Alternative Complementary Medicine
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10 lecture 10.pdf
Summary
# Herbal treatment of acute catarrhal rhinitis
Acute catarrhal rhinitis, a common respiratory ailment characterized by inflammation of the nasal and throat lining leading to swelling and mucus production, can be effectively managed with various herbal remedies. These treatments often focus on counteracting inflammation and stimulating the immune system, with a combination of remedies proving particularly useful [2](#page=2).
### 1.1 Treatment guidelines for acute catarrhal rhinitis
The treatment of acute catarrhal rhinitis generally follows a multi-pronged approach, incorporating both conventional and herbal therapies. Key guidelines include [2](#page=2):
1. **Nasal douches** with isotonic saline solution [2](#page=2).
2. **Antiphlogistics** (anti-inflammatory agents) [2](#page=2).
3. **Cold receptor stimulators** (decongestants) [2](#page=2).
### 1.2 Antiphlogistic agents: German chamomile
German chamomile (*Matricaria recutita*) is a key herbal remedy employed for its anti-inflammatory properties [2](#page=2).
#### 1.2.1 Constituents of German chamomile
The primary constituents of German chamomile that contribute to its therapeutic effects include:
* **Volatile oil** (0.4-1.5%): Major components are (-)-alpha-bisabolol (levomenol), bisabolol oxide A, bisabolol oxide B, bisabololone oxide A, beta-trans-farnesene, trans-en-yne-dicycloether (polyyne spiroether), and chamazulene. Chamazulene, which is blue in color, is formed from the non-volatile precursor matricin during steam distillation [2](#page=2).
* **Flavonoids and highly methoxylized flavonoids** [3](#page=3).
* **Hydroxycoumarins** [3](#page=3).
* **Mucilages** (approximately 10% in mucilage ribs, including fructans like rhamanogalacturonane) [3](#page=3).
#### 1.2.2 Pharmacological effects of German chamomile
German chamomile exhibits several significant pharmacological actions:
* **Anti-inflammatory effects:** Chamazulene plays a role by inhibiting leukotriene B4 formation. The enyne dicycloether component works by preventing mast cell degranulation and subsequent histamine release. Apigenin, a flavonoid, effectively reduces the upregulation of intercellular adhesion molecule-1 and leukocyte adhesion in response to cytokines, through a mechanism independent of free radical scavenging or leukocyte formation [3](#page=3).
* **Antioxidant effects:** Chamazulene, as part of the volatile oil, contributes to antioxidant effects by inhibiting lipid peroxidation. It also inhibits the chemical peroxidation of arachidonic acid, thereby providing both antioxidant and anti-inflammatory benefits [3](#page=3).
#### 1.2.3 Indications and usage of German chamomile
Commission E has approved German chamomile for the following indications:
* Cough and bronchitis [3](#page=3).
* Fevers and colds [3](#page=3).
* Inflammation of the mouth and pharynx [3](#page=3).
#### 1.2.4 Contraindications and precautions for German chamomile
* **Contraindications:** Individuals with a known allergy to chamomile or other plants in the Compositae family should avoid its use [3](#page=3).
* **Precaution & Adverse Reaction:** Ingestion of chamomile tea infusions has, in rare instances, precipitated anaphylactic reactions [3](#page=3).
* **Mode of administration:** It can be administered via inhalation, nasal drops, or as a cream [3](#page=3).
### 1.3 Cold receptor stimulators
Cold receptor stimulators, often used in combination with camphor, are vital for alleviating nasal congestion and improving breathing during acute catarrhal rhinitis [4](#page=4).
#### 1.3.1 Actions of cold receptor stimulators
These agents possess multiple beneficial actions:
1. They stimulate cold receptors in the nose, which facilitates easier breathing due to their decongestant properties [4](#page=4).
2. They act as secretolytic agents, helping to thin and loosen mucus [4](#page=4).
3. They exhibit antimicrobial and antiseptic effects [4](#page=4).
#### 1.3.2 Mode of administration for cold receptor stimulators
Cold receptor stimulators are typically administered as:
* Chest rubs [4](#page=4).
* Steam inhalations [4](#page=4).
* Nasal sprays [4](#page=4).
#### 1.3.3 Mint oil
Mint oil, particularly peppermint oil, is a primary example of a cold receptor stimulator.
##### 1.3.3.1 Constituents of mint oil
The chief components of mint oil include:
* Menthol (35-45%) [4](#page=4).
* Menthone (15-20%) [4](#page=4).
* Menthyl acetate (3-5%) [4](#page=4).
##### 1.3.3.2 Pharmacological effects of mint oil
Mint oil demonstrates the following pharmacological effects:
* Antimicrobial activity [4](#page=4).
* Secretolytic action [4](#page=4).
* A cooling sensation on the skin [4](#page=4).
##### 1.3.3.3 Indications and usage of mint oil
Commission E has approved mint oil for:
* Common colds, coughs, bronchitis, and fevers [4](#page=4).
* Inflammation of the mouth and pharynx [4](#page=4).
* Catarrhs of the respiratory tract and inflammation of the oral and pharyngeal mucosa [4](#page=4).
##### 1.3.3.4 Contraindications and adverse reactions of mint oil
* **Contraindications:** Menthol should be avoided in infants and small children, as it can lead to severe respiratory distress [4](#page=4).
* **Adverse reactions:** Allergic skin reactions and unpleasant local sensations (irritation) can occur with mentholated nasal ointments [4](#page=4).
---
# Herbal treatment of acute sinusitis and cold & flu
This section details herbal approaches to managing acute sinusitis by focusing on immune stimulants and extends to treatments for common cold and flu symptoms, incorporating diaphoretics and vitamin C sources.
### 2.1 Herbal treatment of acute sinusitis
Acute sinusitis, also known as rhinosinusitis, is a brief inflammation of the sinuses, often involving a sinus infection and swelling of the nasal tissue. The treatment regimen for acute sinusitis involves measures similar to those for rhinitis, supplemented with immune stimulants [6](#page=6).
#### 2.1.1 Echinacea (Echinaceae spp.)
Echinacea is a key immune stimulant used in the treatment of acute sinusitis. It is available in various species, including *E. purpurea*, *E. angustifolia*, and *E. pallida*, with different parts of the plant (herb or root) yielding distinct constituents [6](#page=6).
##### 2.1.1.1 Constituents
* **E. purpurea:**
* Herb: Water-soluble immuno stimulating polysaccharides, volatile oil, flavonoids (ferulic acid derivatives, cichoriic acid), alkamides, polyenes [6](#page=6).
* Root: Water-soluble immunostimulating polysaccharides, volatile oil (0.2%), caffeic and ferulic acid derivatives (0.6-2.1% including cichoriic acid), alkamides (0.01-0.04%) [6](#page=6).
* **E. angustifolia:**
* Herb: Volatile oil, flavonoids, caffeic acid derivatives (cichoriic acid, echinacoside), alkamides, polyynes [7](#page=7).
* Root: Water-soluble, volatile oil (under 1%), flavonoids, caffeic acid derivatives (0.3-1.3% including echinacoside, cynarin), alkamides (0.01%), polyynes [7](#page=7).
* **E. pallida:**
* Herb: Volatile oil (0.1%), flavonoids (rutin), caffeic acid derivatives (cichoriic acid), alkamides, polyynes [7](#page=7).
* Root: Water-soluble immunostimulating polysaccharides, volatile oil (0.2-2%), caffeic acid derivatives (echinacoside), alkamides, polyynes [7](#page=7).
##### 2.1.1.2 Pharmacological Effects
Echinacea's primary action is on the nonspecific cellular immune system, exhibiting anti-inflammatory, immuno stimulating, bactericidal, and wound healing properties, which vary by species [7](#page=7).
1. **Immunostimulating:** Ethanolic root extracts of *E. purpurea*, *E. pallida*, and *E. angustifolia* have demonstrated a significant enhancement of phagocytosis in granulocyte smears in vitro. Ethanolic extracts from the aerial parts of *E. angustifolia* and *E. purpurea* also stimulate peritoneal macrophages and can increase spleen weight [7](#page=7).
2. **Anti-Inflammatory:** Polyunsaturated alkamides found in *Echinacea angustifolia* exert anti-inflammatory effects by inhibiting cyclooxygenase and 5-lipoxygenase. The polysaccharide fraction from *Echinacea purpurea* can induce an acute phase reaction [7](#page=7).
3. **Antiviral:** *Echinacea purpurea* herb has shown short-term resistance against influenza, herpes, and vesicular stomatitis viruses, attributed to an interferon-like effect [7](#page=7).
##### 2.1.1.3 Indication and Usage
* **Herb (*E. purpurea*):** Approved by Commission E for common cold, cough/bronchitis, fevers and colds, urinary tract infections, inflammation of the mouth and pharynx, tendency to infection, wounds, and burns [8](#page=8).
* **Root (*E. angustifolia*):** Unproven uses include acute and chronic respiratory tract infections (viral and bacterial), increased susceptibility to infection due to lowered resistance, and treatment of leukopenia following radio and cytostatic therapy, supporting anti-infectious chemotherapy [8](#page=8).
* **Both Herb and Root (*E. pallida*):** Folk medicine applications by Native Americans include external use for burns, swollen lymph nodes, and insect bites. Internally, it has been used for headaches, stomach aches, measles, coughs, and gonorrhea. It has also been used for rattlesnake bites. Currently used for prophylaxis and treatment of flu, sepsis, and mild to moderate cold infections. Externally, it aids in treating poorly healing wounds [8](#page=8).
* **Root (*E. pallida*):** Approved by Commission E as supportive therapy for influenza-like infections [8](#page=8).
##### 2.1.1.4 Precautions and Adverse Reactions
* **General:** Parenteral administration may cause dose-dependent fever, nausea, and vomiting. Caution is advised when administering parentally to individuals with diabetes. Hypersensitivity reactions, including anaphylaxis, have been reported. Rashes, itching, facial swelling, breathing difficulties, dizziness, and a drop in blood pressure have been observed [8](#page=8).
* **Fertility:** High concentrations of Echinacea have shown adverse effects on oocytes in animal models [8](#page=8).
* **Pregnancy:** Parenteral administration should be avoided during pregnancy [8](#page=8).
##### 2.1.1.5 Contraindications
* **Autoimmune Conditions:** Should not be administered in the presence of multiple sclerosis, leukosis, collagen disease, AIDS, or tuberculosis due to potential activation of autoimmune aggressions and overreactive immune responses [9](#page=9).
* **Allergies:** Parenteral administration should not be used in patients prone to allergies, especially to members of the composite family (Asteraceae) [9](#page=9).
* **Pregnancy:** Echinacea should not be used during pregnancy [9](#page=9).
##### 2.1.1.6 Drug Interactions
The immuno-stimulating effect of echinacea may interact with:
1. Drugs with immunosuppressant effects, such as cyclosporine or other anti-rejection medications [9](#page=9).
2. Corticosteroids, potentially interfering with their chemotherapeutic effects [9](#page=9).
### 2.2 Herbal treatment of cold & flu
The treatment regimen for cold and flu involves a multi-faceted approach using immune stimulants, diaphoretics, and vitamin C sources [9](#page=9).
#### 2.2.1 Treatment Regimen
1. **Immuno stimulant:** Purple Echinacea (*E. purpurea*) is an example of an immune stimulant used for cold and flu [9](#page=9).
2. **Diaphoretics (Sweat inducers):** Elder flower, yarrow flower and leaf, and linden flower are diaphoretics that promote sweating. They possess antipyretic and anti-inflammatory effects due to the inhibition of prostaglandins by their flavonoid constituents. Linden flower tea also contributes to the nonspecific activation of the immune system [9](#page=9).
3. **Vitamin C supplements:** Black currant and rose hip peel are sources of Vitamin C. These supplements increase vitamin C stores and enhance the nonspecific immune system, proving beneficial for both prevention and treatment of upper respiratory tract infections [9](#page=9).
---
# Herbal treatment of acute bronchitis and dry cough
This section details herbal remedies used to manage acute bronchitis, focusing on their actions as demulcents, secretolytics, expectorants, and bronchospasmolytics, and also explores antitussive herbs for dry cough.
### 4.1 Herbal treatment of acute bronchitis
Acute bronchitis is typically caused by a viral infection, though irritant bronchitis can result from inhaling toxic or allergic substances. The primary pathological features include abnormal mucus production and impaired clearance from the bronchi, leading to obstruction due to thick secretions and inflammation. Coughing and phlegm production are characteristic symptoms, often prolonged by smoking, and chronic adenovirus infection can also be a contributing factor [10](#page=10).
The treatment regimen for acute bronchitis involves several categories of herbal remedies:
* **Demulcents:** These herbs soothe irritated mucous membranes. Marshmallow is a key example [10](#page=10).
* **Secretolytics & Expectorants:** These agents promote the secretion of thinner mucus and facilitate its expulsion. This category includes aromatic herbs like anise, thyme, and fennel, as well as essential oils such as eucalyptus oil. Herbs containing saponins, like Primula (Cowslip) and Liquorice, also exhibit mucolytic and expectorant effects [10](#page=10).
* **Bronchospasmolytics:** These herbs help to relieve spasms in the bronchial muscles. Thyme, Ivy leaf, Primula root, and Liquorice are noted for this action [10](#page=10).
* **Antiphlogistics:** These remedies possess anti-inflammatory activity. English Ivy (Hedera helix), Primula root, Liquorice, and Iceland moss are examples [10](#page=10).
#### 4.1.1 Demulcents: Marshmallow
* **Botanical Name:** *Althea officinalis* (flowers, leaves & root) [10](#page=10).
* **Key Constituents:** Mucilages (colloidally soluble polysaccharides like galacturonic rhamnans, arabinogalactans, arabans, and glucans), pectins, and starch [10](#page=10).
* **Pharmacological Effects:** Marshmallow alleviates local irritation, can inhibit mucociliary activity, stimulates phagocytosis, and possesses anti-inflammatory, immune-stimulating, and hypoglycemic properties. Its efficacy as a gargle for inflammation of the mouth and throat mucous membranes has been demonstrated [11](#page=11).
* **Indications & Usage:** Approved by Commission E for cough and bronchitis [11](#page=11).
* **Drug Interactions:** May delay the absorption of other simultaneously administered drugs [11](#page=11).
* **Note:** Diabetics should be mindful of the sugar concentration in marshmallow syrup [11](#page=11).
#### 4.1.2 Expectorants: Cowslip
* **Botanical Name:** *Primula* (flowers & root) [11](#page=11).
* **Constituents:**
* Flowers: Flavonoids (3%), Primine, and triterpene saponins [11](#page=11).
* Root: Phenol glycosides (0.2 to 2.3%) and triterpene saponins (5 to 10%), with primulic acid A being a chief component [11](#page=11).
* **Pharmacological Effects:**
* Flowers: Exhibit an expectorant effect attributed to their flavonoid and saponin content. Animal experiments have shown an increase in bronchial secretion volume [11](#page=11).
* Root: The saponin content provides expectorant and diuretic effects, possibly through vagal stimulation [11](#page=11).
* **Indications & Usage:** Approved by Commission E for cough and bronchitis [11](#page=11).
#### 4.1.3 Expectorant and Bronchospasmolytic: English Ivy
* **Botanical Name:** *Hedera helix* (leaves & berries) [12](#page=12).
* **Constituents:** Triterpene saponins, volatile oils, polyynes, steroids, and flavonoids [12](#page=12).
* **Pharmacological Effects:** English Ivy acts as an expectorant and antispasmodic. Hedera saponin C has demonstrated antiviral, antibacterial, antimycotic, anthelmintic, molluscicidal, and anti-flagellate activity. The fresh leaves can be an irritant to skin and mucosa and may cause allergic reactions [12](#page=12).
* **Indications & Usage:** Approved by Commission E for cough and bronchitis. It is used for the symptomatic treatment of chronic inflammatory bronchial conditions and respiratory catarrh [12](#page=12).
### 4.2 Herbal treatment of dry cough
Dry cough is often managed with antitussives, which aim to suppress the cough reflex. While effective for relief in cases of nervous cough, tumors, or severe non-productive cough, antitussives are not ideal if they hinder lung cleansing [12](#page=12).
Antitussive herbs include:
1. **Herbs containing cyanogenetic glycosides:** Examples include Wild Cherry (*Prunus serotina*) [12](#page=12).
2. **Opiates and Opium-like substances:** This includes codeine and gentler alternatives like Lactuca (wild lettuce) [12](#page=12).
3. **Ma-Huang (*Ephedra sinica*)** [12](#page=12).
#### 4.2.1 Antitussive and Bronchodilator: Ma-Huang
* **Botanical Name:** *Ephedra sinica* (young canes collected in autumn, and dried rhizome with roots) [13](#page=13).
* **Constituents:** Alkaloids of the 2-aminophenylpropane type, primarily L-(-)-ephedrine (lR,2S-(-)-ephedrine) and D-pseudoephedrine (lS,2S-(+)-ephedrine), with lesser amounts of L-norephedrine and D-norpseudoephedrine [13](#page=13).
* **Pharmacological Effects:** The concentration of active principles can vary significantly. Ephedrine functions by indirectly stimulating the sympathomimetic nervous system and the central nervous system. The herb exhibits bacteriostatic, positively inotropic, and positively chronotropic effects [13](#page=13).
* **Indications & Usage:** Approved by Commission E for cough and bronchitis [13](#page=13).
* **Precautions & Adverse Reactions:**
* Common side effects include headache, irritability, motor restlessness, nausea, sleeplessness, tachycardia, urinary disorders, and vomiting [13](#page=13).
* Higher doses may lead to blood pressure and cardiac rhythm disorders [13](#page=13).
* Dependence can develop with prolonged use. Due to the risk of tachyphylaxis and dependence, the drug should be administered for short durations only [13](#page=13).
* Ma-Huang should not be used during pregnancy [13](#page=13).
---
## Common mistakes to avoid
- Review all topics thoroughly before exams
- Pay attention to formulas and key definitions
- Practice with examples provided in each section
- Don't memorize without understanding the underlying concepts
Glossary
| Term | Definition |
|------|------------|
| Phytotherapy | The use of plants or plant extracts for medicinal purposes. It involves treating diseases or ailments by employing various parts of plants like flowers, leaves, roots, and bark. |
| Acute Catarrhal Rhinitis | An inflammation of the mucous membrane lining the nose, characterized by swelling and the production of mucus, often triggered by infections or irritations. |
| Antiphlogistic | A substance that counteracts inflammation; an anti-inflammatory agent. These agents work to reduce swelling, redness, and pain associated with inflammatory processes. |
| Chamazulene | A blue-colored volatile compound found in German chamomile, derived from matricin. It possesses significant anti-inflammatory and antioxidant properties. |
| Flavonoids | A class of plant compounds, also known as vitamin P, that have antioxidant effects and can help reduce inflammation. They are abundant in many fruits, vegetables, and herbs. |
| Hydroxycoumarins | A group of chemical compounds found in plants that can have various pharmacological effects, including anticoagulant and antioxidant activities. |
| Mucilages | Gelatinous substances derived from plants, typically soluble in water, that can swell and form a gel. They are often used for their soothing and protective properties, especially for mucous membranes. |
| Cold Receptor Stimulators | Agents that activate cold receptors in the nasal passages, leading to a sensation of improved breathing and acting as decongestants. |
| Secretolytic | A substance that promotes the liquefaction and reduction of viscosity of secretions, such as mucus in the respiratory tract, making them easier to expel. |
| Antimicrobial | An agent that destroys or inhibits the growth of microorganisms, including bacteria, fungi, and viruses. |
| Antiseptic | A substance that inhibits the growth of microorganisms on living tissue, used to prevent infection, particularly on the skin and mucous membranes. |
| 1,8-cineol (Eucalyptol) | The primary active constituent of eucalyptus oil, known for its expectorant, secretolytic, and mild anti-inflammatory effects. |
| Prostaglandin Biosynthesis | The process by which prostaglandins, which are lipid compounds with hormone-like effects, are synthesized in the body. Inhibiting this process can reduce inflammation and pain. |
| Hyperemic | Relating to or causing hyperemia, which is an excess of blood in a part of the body. In topical applications, it can promote healing and reduce inflammation. |
| Expectorant | A drug that helps to loosen and expel mucus from the lungs and respiratory passages. |
| Acute Bronchitis | An inflammation of the bronchial tubes, typically caused by a viral infection, leading to coughing and mucus production. |
| Demulcents | Substances that relieve irritation of the mucous membranes, especially the digestive tract and respiratory tract, by forming a protective film. |
| Secretolytics | Agents that promote the flow of secretions, such as mucus, making them thinner and easier to expel from the body. |
| Saponins | Naturally occurring compounds found in many plants, known for their foaming properties and their expectorant and sometimes diuretic effects. |
| Bronchospasmolytics | Medications or substances that relieve spasms of the bronchial muscles, helping to open the airways and ease breathing. |
| Antipyretic | A drug that reduces fever. |
| Antitussives | Substances that suppress or relieve coughing by acting on the cough reflex. |
| Cyanogenetic Glycosides | Organic compounds that release hydrogen cyanide when hydrolyzed. Certain plant-derived cyanogenetic glycosides have been used for their antitussive properties. |
| Opiates | Narcotic drugs derived from or chemically related to opium, often used for pain relief and cough suppression, though with potential for dependence. |
| Ephedrine | An alkaloid found in plants of the genus Ephedra, acting as a stimulant to the central nervous system and a decongestant. |
| Tachyphylaxis | Rapidly diminishing response to a drug after administration of a few doses. |
| Immunosuppressant | A drug or substance that reduces the activity of the immune system. |
| Autoimmune Aggressions | An immune system response where the body attacks its own healthy tissues. |
| Leukosis | A general term for diseases of the blood or bone marrow characterized by an increase in white blood cells. |
| Collagen Disease | A group of disorders characterized by inflammation and damage to connective tissues throughout the body, such as lupus or rheumatoid arthritis. |
| Asteraceae | A large and widely distributed family of flowering plants, commonly known as the daisy, aster, or sunflower family. |
| Diaphoretics | Substances that promote sweating. |
| Antihypertensive | A drug that lowers blood pressure. |
| MAO-inhibitors (Monoamine Oxidase Inhibitors) | A class of drugs primarily used to treat depression and anxiety disorders. They can interact significantly with sympathomimetic substances. |
| Cardiac Heart Glycosides | A class of drugs derived from plants that are used to treat heart conditions like heart failure and arrhythmias. |
| Secale Alkaloid Derivatives | Compounds derived from the ergot fungus, often affecting blood pressure and uterine contractions. |
| Oxytocin | A hormone and neurotransmitter that plays a role in social bonding, childbirth, and milk ejection. Synthetic forms are used medically. |
Cover
7 lecture Seven.pdf
Summary
# Herbal treatments for diarrhea
This section outlines herbal medicinal approaches to treating diarrhea, focusing on rehydration strategies and the use of tannin-containing remedies [2](#page=2).
### 1.1 Rehydration therapy in diarrhea
The primary approach to managing diarrhea using herbal medicine is oral rehydration therapy (ORT) [2](#page=2).
#### 1.1.1 Sugar-salt solutions
ORT typically involves sugar-salt solutions, frequently enhanced with the addition of starch [2](#page=2).
#### 1.1.2 Starch as a rehydration agent
Starch-based substances, including rice, potato, wheat, and maize, are utilized either as suspensions or in the form of starch-based foods like gruels for rehydration purposes [2](#page=2).
> **Tip:** The use of starch in rehydration is not merely for energy provision but also plays a crucial role in the absorption of sodium and water.
##### 1.1.2.1 Mechanism of starch in rehydration
The polysaccharides present in starch undergo hydrolysis within the gastrointestinal tract (GIT), yielding sugars that are subsequently absorbed. This process leverages the co-transport mechanism of sugar and sodium ions (Na+) from the GIT lumen into the intestinal cells and mucosa. Consequently, starch suspensions actively shift the balance of Na+ towards the mucosal side, thereby enhancing water absorption and supplying the body with energy [2](#page=2).
### 1.2 Tannin-containing drugs for diarrhea
Following rehydration therapies, tannin-containing drugs represent the second line of treatment for diarrhea [2](#page=2).
#### 1.2.1 Properties of tannins
Tannins are characterized as astringent, polymeric polyphenols that are widely distributed in various plant-derived drugs [2](#page=2).
#### 1.2.2 Key herbs containing tannins
Prominent herbs utilized for their tannin content include Black catechu, Acacia catechu, and Oak bark. Even common beverages like tea and coffee also contain tannins [2](#page=2).
#### 1.2.3 Safety and contraindications of tannins
While generally considered safe, caution is advised when administering tannin-containing herbs concurrently with other medications. Tannins exhibit incompatibility with alkalis and alkaloids, forming complexes with proteins and amino acids [2](#page=2).
> **Tip:** Be mindful of potential drug interactions when using tannin-rich herbs, particularly if the patient is on other medications or supplements.
---
# Herbal treatments for constipation
This section summarizes various plant-derived laxatives used for constipation, categorized into bulk-forming, stimulant, and osmotic types.
### 2.1 Bulk-forming laxatives
These are agents with a high fiber content, often rich in polysaccharides, that swell in the gastrointestinal (GI) tract. They are typically undigested and pass through the GI tract unchanged, providing nutrients for colonic bacteria and influencing gut flora composition and food metabolism, which can lead to increased gas. Bulking agents contain a large amount of fibers, while swelling agents are primarily plant material, often seeds, rich in mucilage. The swelling index serves as a marker for the quality of bulk-forming laxatives, indicating the polysaccharide content. Preparations of these laxatives must always be taken with ample water. Conversely, they can be used to treat diarrhea if taken with very little fluid, allowing them to absorb fluid from the lumen and increase stool consistency [3](#page=3).
#### 2.1.1 Linseed (Flaxseed)
* **Constituents:** Mucilages (3-10%) with high swelling capacity, cyanogenic glycosides (0.05-0.1%), fatty oil (30-45% primarily linolenic, linoleic, and oleic acids), proteins (20-27%), lignans, and phenylpropane derivatives [3](#page=3).
* **Pharmacological Effects:** The laxative effect is attributed to bulk material and mucins. Animal experiments have shown a reduction in liver cholesterol levels due to unsaturated fatty acids and a blood sugar-lowering effect. The antitumor effect is linked to lignans, which possess antimycotic, antioxidative, and anti-estrogenic properties. A potential toxic principle involves cyanogenic glycosides, which can yield HCN, but no signs of poisoning have been observed in humans with high single doses or chronic intake [4](#page=4).
* **Indications & Usage:** Approved for constipation and inflammation of the skin [4](#page=4).
* **Contraindications:** Ileus, esophageal stricture, and acute inflammatory illnesses of the intestine, esophagus, and stomach entrance [4](#page=4).
* **Precautions & Adverse Reactions:** No health hazards or side effects are known with proper therapeutic dosages. Excessive use with insufficient fluid intake can lead to ileus. Cyanogenic glycosides do not pose a danger at therapeutic dosages as they are only partially broken down, and increased cyanide ion or thiocyanic acid levels in blood have not been demonstrated. For inflammatory bowel conditions, pre-swollen flaxseed is recommended [4](#page=4) [5](#page=5).
* **Drug Interactions:** Absorption of other simultaneously taken drugs may be delayed [5](#page=5).
* **Food Interactions:** Absorption of flaxseed oil is facilitated when taken with food [5](#page=5).
#### 2.1.2 Ispagula, Psyllium, Wheat bran
* **Constituents:** Mucilages (10-12% in the seed coat, mainly arabinoxylans), iridoids (e.g., aucubin), pyridine alkaloids, proteic substances, and fatty oil [5](#page=5).
* **Pharmacological Effects:** The mucins exert a laxative and antidiarrheal effect by regulating intestinal peristalsis through swelling [5](#page=5).
* **Indications & Usage:** Approved for constipation and diarrhea [5](#page=5).
* **Contraindications:** Pathologic GI tract constriction, inflammatory GI tract illnesses, impending or present ileus, and severely variable diabetes mellitus [6](#page=6).
* **Precautions & Adverse Reactions:** No health hazards or side effects are known with proper therapeutic dosages. Allergic reactions (rhinitis, conjunctivitis, asthma, urticaria) can occur in isolated cases. Incorrect administration with insufficient fluid can lead to esophageal or intestinal obstruction, especially in the elderly [6](#page=6).
* **Drug Interactions:** Absorption of other simultaneously taken drugs could be delayed [6](#page=6).
### 2.2 Stimulant laxatives
These are typically anthraquinone-containing drugs, often found as glycosides in plants. They are metabolized to anthrone types in the colon and caecum by natural GI flora. Anthranoid drugs act directly on the intestinal mucosa, increasing colonic peristalsis, reducing transit time, and consequently decreasing water reabsorption from the colon. Monomeric aglycones like emodin and aloe emodin have demonstrated genotoxic and mutagenic effects in bacterial and mammalian cell lines. Long-term use may cause blackening of the colon due to metabolite incorporation and is associated with an increased risk of colon carcinoma. They are contraindicated in pregnancy as they can affect the uterus and increase abortion risk [6](#page=6) [7](#page=7).
#### 2.2.1 Examples of Stimulant Laxatives
* **Senna leaves and fruits** [Cassia acutifolia & Cassia angustifolia [7](#page=7).
* **Cascara bark** [Rhamnus purshiana and **Frangula bark** [Rhamnus frangula: These barks contain cascarosides and glucofrangulin, respectively. Fresh bark contains emetic and colicky anthrone and dianthrone glycosides and requires storage for one year for oxidation to less toxic anthraquinones [7](#page=7).
* **Castor Oil:** Contains glycerides that yield irritant ricinoleic acid upon hydrolysis [7](#page=7).
#### 2.2.2 Senna
* **Constituents:** Anthracene derivatives (2.5-3.5%) including sennosides A, A1, B, C, and D; and naphthacene derivatives such as 6-hydroxymusizin glucoside [7](#page=7).
* **Pharmacological Effects:** Senna is an anthranoid stimulant laxative. Its laxative effect is mediated by sennosides and their active metabolite, rhein anthrone, in the colon. It inhibits water and electrolyte absorption from the large intestine, increasing intestinal content volume and pressure, which stimulates colon motility. It also stimulates active chloride secretion, increasing water and electrolyte content, a process dependent on calcium. The secretion is mediated by stimulation of endogenous prostaglandin E2 [7](#page=7) [8](#page=8).
* **Indications & Usage:** Used for constipation and bowel evacuation before diagnostic GI and colorectal tests [8](#page=8).
* **Tip:** Stimulating laxatives should not be used for more than 1 to 2 weeks without medical advice [8](#page=8).
* **Contraindications:** Intestinal obstruction, acute inflammatory intestinal diseases, or appendicitis [8](#page=8).
* **Precautions & Adverse Reactions:**
* **General:** Spasmodic GI complaints can occur due to the purgative effect or overdosage. Prolonged use may rarely lead to cardiac arrhythmias, nephropathies, edema, and accelerated bone deterioration. Senna abuse can cause tetany, aspartyl glucosamine excretion, and hypogammaglobulinemia [8](#page=8).
* **Electrolyte Abnormalities:** Long-term use causes electrolyte loss, particularly potassium ions. Hypokalemia can result in hyperaldosteronism, albuminuria, hematuria, inhibition of intestinal motility, and muscle weakness [8](#page=8).
* **Drug Potentiation:** Hypokalemia can potentiate cardioactive glycosides and antiarrhythmics [8](#page=8).
* **Finger Clubbing:** Observed with senna abuse and is reversible upon discontinuation [9](#page=9).
* **Cathartic Colon:** Anatomic alteration of the colon (loss of haustral folds) seen with chronic use (more than three times weekly for 1 year or longer), suggesting neuronal injury or damage to the colonic longitudinal musculature [9](#page=9).
* **Carcinogenesis:** Carcinogenic activity in the colon following long-term administration of anthracene drugs is not fully clarified [9](#page=9).
* **Melanosis Coli:** Prolonged use may lead to melanosis coli, where melanic substance precursors are derived from anthranoid laxatives [9](#page=9).
* **Occupational Sensitization:** IgE-mediated allergy, asthma, and rhino conjunctivitis have been reported after occupational exposure [9](#page=9).
* **Tissue Damage:** Chronic high-dose treatment can reduce vasoactive intestinal polypeptide and somatostatin levels in the colon, potentially indicating damage to enteric nervous tissue [9](#page=9).
* **Drug Interactions:**
* **Digitalis Glycosides:** Potassium loss from prolonged use or abuse can potentiate digitalis toxicity [9](#page=9).
* **Antiarrhythmics:** Potassium loss may potentiate arrhythmias when given with antiarrhythmics [9](#page=9).
* **Estrogen:** Serum estrogen levels may decrease due to increased intestinal transit affecting absorption [9](#page=9).
* **Indomethacin (NSAIDs):** Can cause dose-dependent inhibition of net fluid transport by inhibiting prostaglandin E2, reducing senna's therapeutic effect [10](#page=10).
* **Nifedipine (calcium channel blocker):** Rhein anthrone's therapeutic effects involve calcium channels, which can be blocked by nifedipine but not verapamil [10](#page=10).
* **Pregnancy:** Should not be used during pregnancy or nursing [10](#page=10).
* **Pediatric Use:** Not for children under 2 years; children aged 2-12 should follow dosage recommendations [10](#page=10).
* **Elderly:** Elderly patients should start with half the normal dose [10](#page=10).
* **Preparation:** Infusion: steep 0.5-2 gm of comminuted drug in hot (not boiling) water for 10 minutes, then strain; or steep in cold water for 10-12 hours, then strain. The cold-water method may result in a solution with less resin, reducing abdominal pain. Onset of action is 10-12 hours later [10](#page=10).
### 2.3 Osmotic laxatives
Lactulose and lactose are dimeric sugars derived from milk, useful for treating long-term constipation. Lactose is split into glucose and galactose in the GI tract. Galactose is poorly absorbed and metabolized by colonic bacteria into acids (e.g., lactic, acetic acid) which have an osmotic effect. This also leads to increased bacterial multiplication in the colon, resulting in softer, increased fecal volume and subsequent increased GI peristalsis [10](#page=10).
---
# Main gastrointestinal disorders treated by herbal medicine
This section outlines common gastrointestinal disorders that are addressed using herbal medicinal treatments, detailing the primary approaches and mechanisms of action for each condition [2](#page=2).
### 3.1 Diarrhea
Diarrhea is a prevalent gastrointestinal disorder for which herbal medicine offers distinct treatment lines [2](#page=2).
#### 3.1.1 First-line treatment for diarrhea
The initial approach to managing diarrhea involves oral rehydration therapy (ORT), often incorporating starch-based solutions or foods [2](#page=2).
* **Starch as a therapeutic agent:** Materials such as rice, potato, wheat, and maize are utilized in suspension or as starch-based foods like gruels [2](#page=2).
* **Mechanism of starch in rehydration:** The polysaccharides present in starch are hydrolyzed within the gastrointestinal tract (GIT), yielding sugars that are subsequently absorbed. This process is crucial because the absorption of sugars and sodium ions ($Na^+$) from the GIT lumen into the cells and mucosa occurs via co-transport. Consequently, starch suspensions actively shift the balance of $Na^+$ towards the mucosal side, thereby enhancing water absorption and supplying the body with energy [2](#page=2).
#### 3.1.2 Second-line treatment for diarrhea
Following the initial rehydration phase, tannin-containing herbal drugs are employed as a second-line treatment [2](#page=2).
* **Characteristics of tannins:** Tannins are described as astringent, polymeric polyphenols that are widely distributed in medicinal plants [2](#page=2).
* **Key herbs containing tannins:** Prominent herbs used for their tannin content include black catechu, *Acacia catechu*, and oak bark. Even common beverages like tea and coffee also contain tannins [2](#page=2).
* **Safety and contraindications:** While generally considered safe, caution is advised when administering tannin-rich herbs concurrently with other medications. This is because tannins are incompatible with alkalis and alkaloids, and they can form complexes with proteins and amino acids, potentially affecting the absorption or efficacy of other drugs [2](#page=2).
> **Tip:** When using tannin-containing herbs, be mindful of potential interactions with other medications due to their protein-binding and alkaloid-precipitating properties [2](#page=2).
---
## Common mistakes to avoid
- Review all topics thoroughly before exams
- Pay attention to formulas and key definitions
- Practice with examples provided in each section
- Don't memorize without understanding the underlying concepts
Glossary
| Term | Definition |
|------|------------|
| Phytotherapy | The medicinal use of plants or plant-derived substances to treat or prevent disease and promote well-being. |
| Gastrointestinal Tract (GIT) | The series of organs responsible for digesting food and absorbing nutrients, extending from the mouth to the anus. |
| Oral Rehydration Therapy (ORT) | A treatment for dehydration, especially that due to diarrhea, which involves drinking a solution of sugar and salt in water. |
| Polysaccharides | Complex carbohydrates composed of many monosaccharide units linked together, such as starch and cellulose, often found in plants. |
| Tannins | Astringent, polymeric polyphenolic compounds found in plants that can bind to proteins and other organic compounds, often used for their medicinal properties. |
| Laxative | A substance that aids in the defecation of stools, used to treat constipation. |
| Bulk-forming Laxative | A type of laxative that absorbs water in the intestine to form a gel-like mass, which softens and increases stool bulk, stimulating bowel movements. |
| Fiber | Indigestible plant material that aids digestion by adding bulk to stool and promoting bowel regularity. |
| Mucilage | A gummy substance produced by plants, which swells in water and can be used for its soothing and bulking properties in laxatives. |
| Swelling Index | A measure indicating the amount of polysaccharides present in a plant material, used to assess the quality of bulk-forming laxatives. |
| Cyanogenic Glycosides | Plant compounds that can release hydrogen cyanide (HCN) upon hydrolysis, potentially causing toxicity if ingested in sufficient quantities. |
| Lignans | A class of polyphenolic compounds found in plants, known for their antioxidant, antimycotic, and anti-estrogenic properties. |
| Ileus | A painful condition characterized by the blockage or paralysis of the intestines, preventing normal passage of intestinal contents. |
| Stimulant Laxatives | Laxatives that work by directly stimulating the intestinal lining, increasing peristalsis and promoting bowel movements. |
| Anthraquinones | A group of compounds found in plants, often used as stimulant laxatives, which act on the colonic mucosa to increase motility. |
| Sennosides | Glycosides of anthraquinones found in Senna, acting as potent stimulant laxatives by increasing water and electrolyte secretion in the colon. |
| Cathartic Colon | An anatomical alteration of the colon resulting from chronic use of stimulant laxatives, characterized by loss of haustral folds and potential neuronal damage. |
| Melanosis Coli | A benign pigmentation of the colonic mucosa, appearing dark brown or black, often associated with prolonged use of anthranoid laxatives. |
| Osmotic Laxative | A laxative that works by drawing water into the intestines from surrounding tissues, softening stool and promoting defecation. |
| Lactulose | A synthetic sugar used as an osmotic laxative that is not absorbed in the small intestine and is fermented by colonic bacteria, drawing water into the colon. |
Cover
8 lecture 8.pdf
Summary
# Herbal treatment for inflammatory gastrointestinal conditions
This section details herbal remedies for gastritis and ulcers, focusing on guidelines, constituents, pharmacological effects, and indications for chamomile and liquorice [2](#page=2).
### 1.1 Treatment guidelines for inflammatory GIT conditions
General treatment for inflammatory gastrointestinal (GIT) conditions like gastritis and ulcers typically involves antacids (magnesium and aluminum salts) and demulcents (alginates and mucilage). Phytomedicines such as chamomile and liquorice can also be utilized [2](#page=2).
#### 1.1.1 Helicobacter pylori infection
* *Helicobacter pylori* infection is a known cause of ulceration, with antibiotics being the primary line of treatment [2](#page=2).
#### 1.1.2 Pharmaceutical approaches for mild gastritis
Pharmaceuticals for mild gastritis often combine demulcents to line and soothe the mucosa with carminatives, such as peppermint or anise oil [2](#page=2).
##### 1.1.2.1 Demulcents
Alginates or alginic acid, anionic polysaccharides found in brown algae like Irish moss, function as demulcents. They are prepared from seaweed through washing with acid to remove insoluble ions, dissolution in sodium hydroxide to create a viscous alginate solution, and subsequent filtration to remove debris. The alginate solution binds with water, forming a viscous coating that protects the stomach and esophageal walls [2](#page=2).
### 1.2 German chamomile
* **Botanical Name:** *Matricaria recutita* [2](#page=2).
* **Part Used:** Flower heads [2](#page=2).
#### 1.2.1 Constituents of German chamomile
* **Volatile oil (0.4-1.5%):** Key components include (-)-alpha-bisabolol (levomenol), bisabolol oxide A, bisabolol oxide B, bisabololone oxide A, beta-trans-farnesene, trans-en-yne-dicycloether (polyyne spiroether, adjoining cis-en-yn-dicycloether), and chamazulene (blue due to matricin after steam distillation) [2](#page=2).
* **Flavonoids and highly methoxylated flavonoids** [3](#page=3).
* **Hydroxycoumarins** [3](#page=3).
* **Mucilages (10% in mucilage ribs, fructans):** Including rhamanogalacturonane [3](#page=3).
#### 1.2.2 Pharmacological effects of German chamomile
* **Gastrointestinal Effects:** (-)-alpha-bisabolol reduces the proteolytic activity of pepsin in the GIT and offers protection against gastric toxicity induced by acetylsalicylic acid [3](#page=3).
* **Anti-Inflammatory Effects:** Chamazulene reduces leukotriene B4 formation, while enyne dicycloether inhibits mast cell degranulation and histamine release. Apigenin, a flavonoid, blocks intercellular adhesion molecule-1 upregulation and leukocyte adhesion in response to cytokines, independent of free radical scavenging or leukocyte formation [3](#page=3).
* **Antioxidant Effects:** Chamazulene exhibits antioxidant properties by inhibiting lipid peroxidation and blocking chemical peroxidation of arachidonic acid [3](#page=3).
* **Anxiolytic Effects:** Flavonoids, particularly apigenin, are CNS-active and can exert anxiolytic and mild sedative effects by acting as ligands for central benzodiazepine receptors [3](#page=3).
* **Miscellaneous Effects:** Apigenin has been linked to an increase in atrial rate due to reduced noradrenaline uptake and decreased monoamine oxidase activity [3](#page=3).
#### 1.2.3 Indications and usage of German chamomile
Commission E approves chamomile for internal use in inflammatory GIT diseases associated with spasms, and for irritation of the oral pharyngeal mucous membrane and upper respiratory tract [4](#page=4).
#### 1.2.4 Contraindications for German chamomile
Chamomile should be avoided by individuals with known allergies to its components or other members of the Compositae family [4](#page=4).
#### 1.2.5 Precautions and adverse reactions of German chamomile
Anaphylactic reactions have been reported following the ingestion of chamomile tea infusions [4](#page=4).
### 1.3 Liquorice
* **Botanical Name:** *Glycyrrhiza glabra* [4](#page=4).
* **Part Used:** Roots and rhizomes [4](#page=4).
#### 1.3.1 Constituents of Liquorice
* **Triterpene saponins (3-15%):** The primary components are glycyrrhetic acid (sweet-tasting, aglycone 18beta-glycyrrhetic acid, and its salts, glycyrrhizin) [4](#page=4).
* **Flavonoids:** Including aglycones and isoflavonoids [4](#page=4).
* **Cumestans and hydroxycoumarins** [4](#page=4).
* **Steroids** [4](#page=4).
* **Volatile oil (minimal):** Contains anethole, estragole, eugenol, and hexanoic acid [4](#page=4).
#### 1.3.2 Pharmacological effects of Liquorice
* **Anti-inflammatory and antiplatelet effects** [4](#page=4).
* **Antiulcer effect:** Liquorice provides protective effects against aspirin-induced gastric ulcers and can release endogenous secretin, a potential mediator of these actions. Carbenoxolone, a derivative of glycyrrhetic acid, accelerates ulcer healing. Deglycyrrhizinated licorice is also effective for ulcer healing and lacks the adverse effects associated with carbenoxolone [4](#page=4).
* **Antiviral and antifungal activity** [4](#page=4).
* **Mineral corticoid effect** [4](#page=4).
#### 1.3.3 Indications and usage of Liquorice
Commission E approves liquorice for cough, bronchitis, and gastritis [5](#page=5).
#### 1.3.4 Contraindications for Liquorice
Contraindications include chronic hepatitis, cholestatic liver diseases, liver cirrhosis, severe renal insufficiency, diabetes, arrhythmias, hypertension, hypertonia, hypokalemia, and pregnancy. Tobacco use has been linked to liquorice toxicity [5](#page=5).
#### 1.3.5 Precautions and adverse reactions of Liquorice
* **General:** Prolonged use can lead to hypokalemia, hypernatremia, edema, hypertension, and cardiac complaints [5](#page=5).
* **Endocrine:** Pseudoaldosteronism, characterized by hypertension and hypokalemic metabolic alkalosis, is attributed to glycyrrhetenic acid. This effect is associated with sodium and water retention and suppression of the renin-aldosterone system [5](#page=5).
#### 1.3.6 Drug Interactions of Liquorice
* **Furosemide/Thiazide Diuretics:** Concomitant use is not recommended due to the additive risk of hypokalemia [5](#page=5).
* **Digitalis Glycosides:** Prolonged liquorice use can cause hypokalemia, potentially potentiating digitalis toxicity [5](#page=5).
* **Anti-arrhythmic Agents (procainamide, quinidine):** Concomitant use may potentiate the risk of severe ventricular tachycardia of the torsades de pointes type, as hypokalemia associated with liquorice can increase this risk [5](#page=5).
* **Corticosteroids:** Concurrent use with liquorice can potentiate the effects of corticosteroids due to the prolonged half-life of cortisol [5](#page=5).
---
# Herbal treatment for nausea and vomiting
This section details the use of ginger as a phytomedicine for nausea and vomiting, covering its composition, mechanisms of action, recommended usage, and potential interactions [6](#page=6).
### 2.1 Ginger (Zingiber officinalis; rhizome)
Ginger is a well-established herbal remedy for nausea and vomiting, with its therapeutic properties attributed to a variety of chemical constituents [6](#page=6).
#### 2.1.1 Constituents
The primary active components of ginger include [6](#page=6):
* **Volatile oil (2.5-3.0%)**: The specific composition varies by origin but includes compounds like (-)-zingiberene, arcurcumene, beta-bisabolene, curcumene, neral, geranial, D-camphor, beta-phellandrene, geranial, neral, linalool, (E)-alpha-farnesene, and zingiberol (a mixture of cis- and trans-beta-eudesmol). These are important as aroma carriers [6](#page=6).
* **Aryl alkanes**: These include gingerols and gingerdiols [6](#page=6).
* **Diarylheptanoids**: These are also key active compounds [6](#page=6).
* **Starch (50%)**: A significant component by weight [6](#page=6).
#### 2.1.2 Pharmacological effects
Ginger exhibits a range of pharmacological actions relevant to its use in treating nausea and vomiting, as well as other conditions [6](#page=6) [7](#page=7):
* **Antiemetic effect**: This is primarily attributed to gingerols and shogaols. Unlike many antiemetic drugs that act on the central nervous system (CNS), ginger's antiemetic effect is believed to be due to local actions within the gastrointestinal tract [7](#page=7).
* **Positive inotropic effect**: Ginger can increase the force of heart muscle contractions [6](#page=6).
* **Antithrombotic effect**: Ginger can help prevent blood clot formation [6](#page=6).
* **Antioxidant effects**: It possesses properties that combat oxidative stress [6](#page=6).
* **Anti-migraine effects**: Ginger may be beneficial in managing migraines [6](#page=6).
* **Anti-lipidemic effects**: It can help lower lipid levels [6](#page=6).
* **Promotes secretions**: Ginger promotes the secretion of saliva, gastric juices, and bile [6](#page=6).
* **Anti-inflammatory effects**: These are thought to stem from the inhibition of cyclooxygenase and 5-lipoxygenase enzymes, which reduces leukotriene and prostaglandin synthesis [7](#page=7).
* **Gastrointestinal effects**: In humans, ginger increases intestinal tone and peristalsis [7](#page=7).
* **Immune system stimulation**: Ginger has shown some ability to stimulate the immune system [7](#page=7).
* **Platelet aggregation inhibitory activity**: It can inhibit the clumping of platelets [7](#page=7).
#### 2.1.3 Indications and usage
The German Commission E has approved ginger for the following indications [7](#page=7):
* Loss of appetite [7](#page=7).
* Travel sickness [7](#page=7).
* Dyspeptic complaints [7](#page=7).
> **Tip:** Ginger is commonly used for motion sickness and general nausea due to its local gastrointestinal effects [7](#page=7).
#### 2.1.4 Contraindications
Certain conditions warrant caution or contraindication for ginger use [7](#page=7):
* **Pregnancy**: Large doses of ginger are contraindicated in morning sickness associated with pregnancy [7](#page=7).
* **Gallstone conditions**: Due to its cholagogic effect (promoting bile flow), ginger should not be used in patients with gallstones unless a physician has been consulted [7](#page=7).
* **Hemorrhage risk**: As ginger inhibits thromboxane synthesis, it should be avoided by individuals at risk for bleeding disorders [7](#page=7).
#### 2.1.5 Precautions and adverse reactions
While generally safe at therapeutic doses, certain precautions and potential reactions exist [7](#page=7) [8](#page=8):
* **Gastric epithelial exfoliation**: High doses (6 grams of dried powdered ginger) have been reported to increase the exfoliation of gastric surface epithelial cells, potentially leading to ulcer formation. Therefore, limiting doses to 6 grams on an empty stomach is recommended [7](#page=7).
* **Hypersensitivity reactions**: Ginger can occasionally cause hypersensitivity reactions, manifesting as dermatitis [8](#page=8).
* **Overdose effects**: Large overdoses may lead to central nervous system depression and cardiac arrhythmia [8](#page=8).
#### 2.1.6 Drug interactions
* **Anticoagulants and bleeding disorders**: Patients taking anticoagulant medications or those with existing bleeding disorders should avoid large doses of ginger [8](#page=8).
---
# Herbal treatment for irritable bowel syndrome
This section details the use of various herbal remedies for Irritable Bowel Syndrome (IBS), focusing on their constituents, pharmacological effects, indications, and precautions. Herbal treatments for IBS commonly involve bulk laxatives and antispasmodic carminative agents [8](#page=8).
### 3.1 Bulk laxatives
While not detailed in terms of specific herbs within the provided content, bulk laxatives are mentioned as a foundational treatment approach for IBS [8](#page=8).
### 3.2 Antispasmodic carminative drugs
Antispasmodic carminative drugs, often essential oils, are utilized for their ability to relieve spasms and expel gas from the digestive tract. This category includes mint and umbelliferous fruits [8](#page=8).
#### 3.2.1 Mint leaves & oil (Mentha piperita)
Mint, specifically *Mentha piperita*, is employed for its antispasmodic and carminative properties [8](#page=8).
* **Constituents:**
* Leaves contain volatile oil with chief components such as menthol (35-45%), menthone (15-20%), and menthyl acetate (3-5%), along with caffeic acid and flavonoids [8](#page=8).
* The oil shares similar chief components: menthol (35-45%), menthone (15-20%), and menthyl acetate (3-5%) [8](#page=8).
* **Pharmacological Effects:**
* General effects include spasmolytic action on digestive tract smooth muscle, carminative properties, cholagogue effects, and antimicrobial activity [8](#page=8).
* Leaves also exhibit antiviral, diuretic, and mild sedative effects [9](#page=9).
* The oil is insecticidal, a secretolytic agent, and provides a cooling effect on the skin [9](#page=9).
* **Indications & Usage:**
* **Leaves:** Used for liver and gallbladder complaints, dyspeptic complaints, and convulsive complaints of the gastrointestinal tract [9](#page=9).
* **Oil:** Indicated for common cold, cough, bronchitis, fevers, inflammation of the mouth and pharynx, liver and gallbladder complaints, dyspeptic complaints, tendency to infection, and cramps of the upper gastrointestinal tract and bile ducts, including irritable colon [9](#page=9).
* **Contraindications:**
* Leaves are contraindicated in cases of gallstones [9](#page=9).
* Internal administration of the oil is contraindicated for biliary duct occlusion, gallbladder inflammation, and severe liver damage. Gallstone carriers may experience colic due to the cholagogic effect [9](#page=9).
* **Precautions and Adverse Reactions:**
* No health hazards are known with proper administration at designated therapeutic dosages [9](#page=9).
* Gallstone carriers may experience colic due to the cholagogic effect of the leaves [9](#page=9).
* The oil intake can cause gastric complaints in susceptible individuals [9](#page=9).
* The volatile oil has a weak potential for sensitization due to its menthol content [9](#page=9).
* Administration is advised against in cases of gastroesophageal reflux tendency [9](#page=9).
* Preparations containing mint oil should not be applied to the faces of infants or small children, especially near the nasal area, due to the risk of glottal or bronchial spasm, potentially leading to asthma-like attacks or respiratory failure [10](#page=10).
* **Overdosage:**
* No poisoning cases are recorded. The estimated minimal lethal dose of menthol is 2 grams, though individuals have survived higher doses of 8-9 grams [10](#page=10).
#### 3.2.2 Umbelliferous fruits
This group includes anise, caraway, coriander, and fennel, all of which possess carminative and antispasmodic properties.
##### 3.2.2.1 Anise
* **Constituents:** Volatile oil (anethole), caffeic acid, flavonoids, fatty acids, and proteins [10](#page=10).
* **Pharmacological Effects:** Expectorant, mildly spasmolytic, antibacterial. The oil (trans-anethole) has antibacterial, antiviral, insect repellent, and estrogenic effects [10](#page=10).
* **Indications & Usage:** Common cold, cough, bronchitis, fevers, inflammation of the mouth and pharynx, dyspeptic complaints, and loss of appetite [10](#page=10).
* **Contraindications:** Patients allergic to anise and anethole [10](#page=10).
* **Precautions and Adverse Reactions:** No general health hazards are known with proper administration at designated therapeutic dosages. Sensitization has been observed very rarely [11](#page=11).
##### 3.2.2.2 Caraway
* **Constituents:** Volatile oil (carvone and limonene), fatty oil, polysaccharide, proteins, and furanocoumarin [11](#page=11).
* **Pharmacological Effects:** Spasmolytic effect, antimicrobial, and choleretic effect [11](#page=11).
* **Indications & Usage:** Dyspeptic complaints [11](#page=11).
* **Precautions and Adverse Reactions:** No general health hazards are known with proper administration at designated therapeutic dosages. Overdose can lead to kidney and liver damage [11](#page=11).
##### 3.2.2.3 Coriander
* **Constituents:** Volatile oil (linalool), fatty acids, and hydroxy-coumarins [11](#page=11).
* **Pharmacological Effects:** The oil stimulates gastric juice secretion, and it is carminative, spasmolytic, antibacterial, and antifungal [11](#page=11).
* **Indications & Usage:** Dyspeptic complaints and loss of appetite [11](#page=11).
* **Precautions and Adverse Reactions:** No general health hazards are known with proper administration at designated therapeutic dosages. The drug has a weak potential for sensitization [12](#page=12).
##### 3.2.2.4 Fennel
* **Constituents:** Volatile oil (trans-anethole, fenchone, estragole), pyranocoumarins, flavonoids, fatty oil, and proteins [12](#page=12).
* **Pharmacological Effects:** Stimulates gastrointestinal motility. At higher concentrations, it acts as an antispasmodic. Anethole and fenchone have shown a secretolytic action on the respiratory tract. It is also antimicrobial [12](#page=12).
* **Indications & Usage:** Cough and bronchitis, and dyspeptic complaints [12](#page=12).
* **Precautions and Adverse Reactions:** No general health hazards are known with proper administration at designated therapeutic dosages. Allergic reactions have been observed very rarely. Cross-sensitivity among patients with celery allergy appears possible. Preparations, excluding the drug itself and tea infusions, are not to be administered during pregnancy and to small children [12](#page=12).
### 3.3 Other relevant treatments
* **Tropane alkaloid:** Hyoscine in the form of N-butyl bromide is mentioned as a quaternary ionic compound that is poorly absorbed from the intestine, leading to fewer side effects [8](#page=8).
---
## Common mistakes to avoid
- Review all topics thoroughly before exams
- Pay attention to formulas and key definitions
- Practice with examples provided in each section
- Don't memorize without understanding the underlying concepts
Glossary
| Term | Definition |
|------|------------|
| Phytotherapy | The use of plants or plant extracts for medicinal purposes. It is a form of complementary and alternative medicine. |
| Gastrointestinal Tract (GIT) | The series of organs responsible for digesting food and absorbing nutrients, starting from the mouth and ending at the anus. |
| Antacids | Medications that neutralize stomach acid, providing temporary relief from heartburn and indigestion. They are often composed of salts of magnesium and aluminum. |
| Demulcents | Substances that form a protective coating over mucous membranes, soothing irritation and inflammation. Examples include alginates and mucilage. |
| Alginates | Polysaccharides derived from brown algae, which form a viscous solution when mixed with water, acting as a protective barrier in the stomach and esophagus. |
| Mucilage | A viscous, gummy secretion produced by plants, often used as a demulcent to soothe internal tissues. |
| Carminative | An agent that promotes the expulsion of gas from the digestive tract, relieving bloating and discomfort. Peppermint and anise are common examples. |
| Helicobacter pylori | A bacterium that is a common cause of peptic ulcers and gastritis. It infects the stomach lining and can lead to inflammation. |
| Chamomile | A herb from the Compositae family, known for its anti-inflammatory, antispasmodic, and anxiolytic properties, commonly used for gastrointestinal complaints. |
| (-)-alpha-bisabolol (Levomenol) | A major component of chamomile's volatile oil, known for its gastrointestinal effects, including reducing pepsin activity and protecting against gastric toxicity. |
| Chamazulene | A blue-colored compound found in chamomile, responsible for its anti-inflammatory effects through the inhibition of leukotriene B4 formation. |
| Flavonoids | A diverse group of plant pigments that possess antioxidant and anti-inflammatory properties. In chamomile, they contribute to anxiolytic effects. |
| Apigenin | A flavonoid found in chamomile that acts as a ligand for central benzodiazepine receptors, producing anxiolytic and sedative effects. |
| Liquorice | The root and rhizome of *Glycyrrhiza glabra*, used for its anti-inflammatory, antiulcer, and expectorant properties, though it has potential side effects. |
| Glycyrrhiza glabra | The botanical name for the liquorice plant, from which medicinal extracts are derived. |
| Glycyrrhetic acid | An aglycone and active component of liquorice, responsible for many of its pharmacological effects, including mineralocorticoid activity. |
| Glycyrrhizin | A salt form of glycyrrhetic acid found in liquorice, known for its sweet taste and potent pharmacological effects, but also associated with adverse reactions. |
| Pseudoaldosteronism | A condition mimicking hyperaldosteronism caused by certain substances, like glycyrrhetenic acid from liquorice, leading to fluid retention, hypertension, and hypokalemia. |
| Ginger | The rhizome of *Zingiber officinalis*, widely used for its antiemetic, anti-inflammatory, and digestive properties. |
| Zingiber officinalis | The botanical name for the ginger plant. |
| Gingerols | Pungent compounds found in ginger, believed to be responsible for its antiemetic and anti-inflammatory effects. |
| Shogaols | Compounds formed from gingerols when ginger is dried or heated, also contributing to its antiemetic properties. |
| Antiemetic | An agent that is effective against vomiting and nausea. |
| Irritable Bowel Syndrome (IBS) | A common gastrointestinal disorder characterized by abdominal pain, bloating, and changes in bowel habits, often treated with dietary changes and medications. |
| Bulk laxatives | Dietary fibers that absorb water and increase stool bulk, promoting bowel regularity. |
| Antispasmodic | A drug that relieves or prevents muscle spasms, particularly in the digestive tract. |
| Menthol | A compound found in peppermint oil, known for its cooling sensation, mild anesthetic properties, and spasmolytic effects. |
| Menthone | A ketone found in peppermint oil, contributing to its aroma and some of its pharmacological effects. |
| Menthyl acetate | An ester found in peppermint oil, contributing to its aroma and flavor. |
| Umbelliferous Fruits | Fruits from plants in the Apiaceae family, such as anise, caraway, coriander, and fennel, often used for their carminative and digestive properties. |
| Anethole | A key component of the volatile oil of anise and fennel, known for its expectorant, spasmolytic, and antimicrobial effects. |
| Carvone | A component of caraway seed oil, contributing to its characteristic aroma and spasmolytic properties. |
| Limonene | A cyclic terpene found in the volatile oils of caraway and other citrus fruits, with potential antimicrobial and anti-inflammatory effects. |
| Linalool | An alcohol terpene found in the volatile oil of coriander, known for its carminative and spasmolytic effects. |
| Fenchone | A ketone found in fennel oil, contributing to its aroma and secretolytic action on the respiratory tract. |
| Secretolytic | An agent that promotes the secretion of mucus or other bodily fluids. |
Cover
vptgm-samenvatting-van-plant-tot-geneesmiddelontwikkeling.pdf
Summary
# Plant-derived medicinal compounds
Plant-derived medicinal compounds are natural products or their synthetic derivatives sourced from various botanical origins, classified chemically, and utilized for their diverse therapeutic applications [2](#page=2) [3](#page=3) [4](#page=4) [5](#page=5) [6](#page=6).
### 1.1 Introduction to plant-derived compounds
Plants have historically served as a crucial source of medicines, with many modern pharmaceuticals originating from or being inspired by natural compounds found in flora. These compounds exhibit a wide range of biological activities, making them valuable in treating various ailments [2](#page=2) [3](#page=3) [4](#page=4) [5](#page=5) [6](#page=6).
### 1.2 Carbohydrate-based compounds
Carbohydrates, including monosaccharides, disaccharides, oligosaccharides, and polysaccharides, are derived from plants and have significant medicinal or industrial applications [2](#page=2) [3](#page=3).
#### 1.2.1 Monosaccharides
* **Glucose (Dextrose, druivensuiker):** A fundamental sugar used as an energy source [2](#page=2).
* **Fructose:** Used as a sweetener, particularly for individuals with diabetes [2](#page=2).
* **Mannose (D-mannose):** Utilized in preventing and treating urinary tract infections [2](#page=2).
#### 1.2.2 Disaccharides
* **Lactose:** A sugar found in milk, with intolerances managed by lactase supplements [2](#page=2).
* **Lactulose (semi-synthetic):** A laxative used to treat constipation [2](#page=2).
#### 1.2.3 Oligosaccharides
* **Acarbose:** Derived from *actinoplanes*, this compound inhibits alpha-glucosidase, reducing glucose absorption in the body, and can cause flatulence and diarrhea [2](#page=2).
#### 1.2.4 Polysaccharides
* **Dextran:** A glucose polymer used as a plasma expander to increase blood volume [2](#page=2).
* **Cellulose:** An important precursor for the synthesis of various derivatives [2](#page=2).
* **Hyaluronic acid:** A polymer of N-acetyl-glucosamine and glucuronic acid found in connective tissues and the eye, used in cosmetics for hydration and in eye drops [2](#page=2).
* **Heparin:** A complex polysaccharide derived from animal tissues, used as an anticoagulant to prevent and treat deep vein thrombosis; low molecular weight heparins like enoxaparine and nadroparine are also used [2](#page=2).
* **Gums:** Plant gums from sources like *Aloe Vera*, tragacanth, acacia gum, and agar are used as thickeners, stabilizers, swelling agents, binders, adhesives, and culture media components [3](#page=3).
* **Alginic acid and alginates:** Derived from brown algae, used as thickening agents and to form a protective layer against gastro-oesophageal reflux [3](#page=3).
* **Mucilage:** Obtained from plants like *Althaea officinalis* (marshmallow root), used in cough preparations to soothe the airways [3](#page=3).
* **Psyllium and Flaxseed:** Seeds from *Plantago* and *Linum usitatissimum* respectively, act as bulk-forming laxatives when consumed with sufficient water [3](#page=3).
### 1.3 Flavonoids
Flavonoids, characterized by a C6-C3 structure with acetate units, are found in fruits and vegetables and possess antioxidant properties, contributing to the prevention of cardiovascular diseases and cancer [3](#page=3).
### 1.4 Terpenes
Terpenes are a class of compounds with significant medicinal applications, particularly in oncology [3](#page=3) [5](#page=5).
* **Paclitaxel (Taxol):** Isolated from *Taxus brevifolia* and *Taxus baccata*, it is an antitumoral drug that inhibits mitosis by stabilizing microtubules. Synthetic derivatives and precursors include 10-deacetyl-baccatin III, docetaxel, and cabazitaxel [3](#page=3) [4](#page=4).
* **Artemisinin:** Found in *Artemisia annua* (sweet wormwood), it is highly effective against malaria. Derivatives such as dihydro-artemisinin, artemether, arteether, and artesunate are also used [5](#page=5).
### 1.5 Alkaloids
Alkaloids are a diverse group of nitrogen-containing organic compounds with potent physiological effects [4](#page=4) [5](#page=5) [6](#page=6).
#### 1.5.1 Opium alkaloids
Derived from the opium poppy (*Papaver somniferum*), these include morphine, codeine, thebaine, noscapine, papaverine, and heroin [4](#page=4).
* **Morphine:** A potent analgesic and narcotic, used for severe pain, especially in terminal cancer patients, and has effects similar to endorphins and enkephalins [4](#page=4).
* **Codeine:** A weaker analgesic and cough suppressant derived from morphine, with potential for addiction and constipation [4](#page=4).
* **Thebaine:** A precursor for semi-synthetic analgesics like oxycodone (Oxycontin) and buprenorphine, an addiction treatment [4](#page=4).
* **Noscapine:** A non-addictive cough suppressant with a different structure than morphine [4](#page=4).
* **Papaverine:** A musculotropic spasmolytic that relaxes smooth muscles, historically used for cramps and vasodilation but less common now [4](#page=4).
* **Heroin (diacetylmorphine):** A highly lipophilic derivative of morphine that rapidly enters the central nervous system, making it a potent and addictive drug [4](#page=4).
* **Laudanum:** An opium tincture with saffron, formerly used as an antidiarrheal and antispasmodic [4](#page=4).
#### 1.5.2 Tropane alkaloids
* **Hyoscyamine (atropine) and Hyoscine (scopolamine):** Found in *Atropa belladonna* (deadly nightshade), these are parasympatholytics that relax smooth muscles, used for gastrointestinal and urinary cramps, asthmatic conditions, and scopolamine for motion sickness. Synthetic derivatives include ipratropium bromide and butyl-scopolamine [5](#page=5).
* **Cocaine:** Derived from the coca plant (*Erythroxylon coca*), it is a stimulant and highly addictive drug [5](#page=5).
#### 1.5.3 Other alkaloids
* **Colchicine:** From *Colchicum autumnale* (meadow saffron), used to treat acute gout attacks [5](#page=5).
* **Vinblastine and Vincristine:** Iridoid-indol alkaloids from *Catharanthus roseus* (periwinkle), used in cancer therapy [5](#page=5) [6](#page=6).
* **Campothecine:** From the Chinese ornamental tree *Campotheca acuminata*, with semi-synthetic derivatives like topotecan and irinotecan being important anticancer drugs that inhibit DNA replication and transcription [6](#page=6).
* **Kina alkaloids (Quinine):** From the cinchona tree (*Cinchona pubescens*), it was the first antimalarial drug, with derivatives like chloroquine and mefloquine also used [6](#page=6).
* **Ergotamine:** Derived from the ergot fungus (*Claviceps purpurea*), used for acute migraine attacks. LSD, a strong hallucinogen, is also a derivative [6](#page=6).
* **Ephedrine:** A simple alkaloid with a stimulating effect similar to adrenaline, found in nasal drops for vasoconstriction. Related compounds include pseudoephedrine, amphetamine, and MDMA [6](#page=6).
* **Nicotine:** From the tobacco plant (*Nicotiana tabacum*), it has digestive, appetite-suppressing, and anti-diuretic effects, causes vasoconstriction and hypertension, but is not responsible for lung cancer [6](#page=6).
### 1.6 Polyketides, phenylpropanoid derivatives, and their combinations
* **Statins:** Natural products like mevastatin and lovastatin, originally from oyster mushrooms (*Pleurotus ostreatus*), have led to the development of synthetic statins such as simvastatin and pravastatin, used to lower cholesterol and treat cardiovascular diseases [4](#page=4).
* **Salicylic acid:** Found in willow bark (*Salix* species) as salicin, which is converted to salicylic acid in the liver. Its synthetic derivative, acetylsalicylic acid (aspirine), is used for pain relief, fever reduction, and anti-inflammation [5](#page=5).
* **Naphthoquinones:** Lawsone, a red-orange dye from *Lawsonia inermis* (henna), is the basis for atovaquone, an antimalarial drug [5](#page=5).
* **Lignans:** Composed of two C6C3 building blocks, they exhibit inhibitory effects on mitosis but are too toxic. Semi-synthetic derivatives like etoposide and teniposide are important anticancer drugs that inhibit DNA replication and transcription [5](#page=5).
### 1.7 Heart glycosides
* **Digoxin:** A "heart-active glycoside" derived from foxglove plants (*Digitalis purpurea* and *Digitalis lanata*), it strengthens heart contractions and is used for heart insufficiency [5](#page=5).
> **Tip:** When studying plant-derived medicinal compounds, pay close attention to the plant source, the chemical class of the compound, its mechanism of action, and its therapeutic applications, as well as any significant semi-synthetic derivatives [2](#page=2) [3](#page=3) [4](#page=4) [5](#page=5) [6](#page=6).
> **Example:** For Paclitaxel, note its origin from *Taxus* species, its classification as a terpene, its mechanism of inhibiting mitosis by stabilizing microtubules, and its use as an antitumoral drug, along with its synthetic relatives [3](#page=3) [4](#page=4).
---
# Carbohydrate classifications and applications
Carbohydrates are a diverse class of biomolecules with varied structures and significant applications in medicine, industry, and everyday life. This section categorizes carbohydrates into monosaccharides, disaccharides, oligosaccharides, and polysaccharides, detailing their natural sources and functional uses [2](#page=2) [3](#page=3).
### 2.1 Carbohydrate classification
Carbohydrates can be classified based on their molecular size and complexity [2](#page=2) [3](#page=3).
#### 2.1.1 Monosaccharides
Monosaccharides are the simplest form of carbohydrates, consisting of a single sugar unit [2](#page=2).
* **Glucose** (also known as dextrose or grape sugar) [2](#page=2).
* **Fructose** is used as a sweetener for individuals with diabetes [2](#page=2).
* **Mannose** (specifically D-mannose) is used in the treatment of urinary tract infections, often sold under brand names like Femannose® [2](#page=2).
#### 2.1.2 Disaccharides
Disaccharides are formed by the combination of two monosaccharide units [2](#page=2).
* **Lactose** is commonly associated with lactose intolerance, which can be managed with lactase enzyme supplements [2](#page=2).
* **Lactulose** is a semi-synthetic disaccharide with a laxative effect, available under brand names such as Duphalac® and Bifiteral® [2](#page=2).
#### 2.1.3 Oligosaccharides
Oligosaccharides are composed of a short chain of monosaccharide units [2](#page=2).
* **Acarbose** is an oligosaccharide derived from the actinomycete *Actinoplanes*. It acts as an inhibitor of alpha-glucosidase, reducing glucose absorption in the body. Potential side effects include flatulence and diarrhea [2](#page=2).
#### 2.1.4 Polysaccharides
Polysaccharides are complex carbohydrates made up of long chains of monosaccharide units [2](#page=2) [3](#page=3).
##### 2.1.4.1 Glucose polymers
* **Dextran** is a glucose polymer used as a plasma expander to increase blood volume [2](#page=2).
* **Cellulose** is an important component in the synthesis of derivatives and is found in sources like flax fibers and cotton [2](#page=2).
##### 2.1.4.2 Polymers of N-acetylglucosamine and glucuronic acid
* **Hyaluronic acid** is a polymer found in connective tissue and the vitreous humor of the eye. It is utilized in cosmetics for its hydrating properties and in eye drops [2](#page=2).
##### 2.1.4.3 Polymers of uronic acids, D-glucosamine, and sulfate groups
* **Heparin** is derived from animal sources such as bovine lungs and swine intestines. It acts as an anticoagulant, preventing and treating deep vein thrombosis. Modern preparations often involve hydrolysis products like low molecular weight heparins, such as enoxaparin (Clexane®) and nadroparin (Fraxiparine®) [2](#page=2).
##### 2.1.4.4 Gums
Gums are a class of polysaccharides often used as thickening and stabilizing agents [3](#page=3).
* **Tragacanth gum** is used as a swelling agent to create suspensions and prevent precipitation [3](#page=3).
* **Gum arabic** (Acacia gum) serves as a swelling agent for suspensions, a binder, and an adhesive (e.g., in postage stamps) [3](#page=3).
* **Agar** (agar-agar), derived from red algae, is used as a culture medium in bacteriology [3](#page=3).
* **Alginic acid and alginates**, sourced from brown algae, are used as thickening agents in the food industry. They also form a protective layer to alleviate gastro-esophageal reflux when combined with antacids, as seen in products like Gaviscon® [3](#page=3).
##### 2.1.4.5 Mucilages
Mucilaginous preparations are used for their soothing properties.
* **Marshmallow root** (*Althaea officinalis*) yields a mucilage when macerated with cold water, used in cough preparations to soothe the respiratory tract [3](#page=3).
* **Psyllium seeds** (from *Plantago* species) are used as a bulk-forming laxative, requiring consumption with sufficient water [3](#page=3).
* **Flaxseed** (*Linum usitatissimum*) has similar applications to psyllium seed as a laxative [3](#page=3).
### 2.2 Applications of specific plant-derived compounds
Beyond simple carbohydrate structures, various plant compounds and their derivatives have significant medicinal and industrial applications [2](#page=2) [3](#page=3).
#### 2.2.1 Horse tails and ferns
* **Horsetail** (*Equisetum arvense*) is rich in minerals and possesses diuretic and wound-healing properties [2](#page=2).
* **Brake fern** (*Pteridium aquilinum*) is a common plant, with its young leaves (fiddleheads) being edible [2](#page=2).
#### 2.2.2 Ginkgo biloba and sundew
* **Ginkgo biloba** (Japanese nut tree) is a symbol of longevity and is associated with improved blood circulation and potential benefits against age-related dementia [2](#page=2).
* **Sundew** (*Drosera*) contains compounds like droserone, structurally similar to atovaquone, which is a drug used to treat malaria (e.g., Malarone®). The plant's epidermal hairs are adapted for catching insects as a food source [2](#page=2).
#### 2.2.3 Chamomile and devil's claw
* **German chamomile** (*Matricariae flos*) contains chamazulene carboxylic acid, structurally related to ibuprofen. Its dried flower heads are used in anti-inflammatory creams, teas for gastrointestinal issues, and cosmetics (e.g., to lighten hair) [2](#page=2).
* **Devil's claw** (*Harpagophytum procumbens*) root is used for treating inflammation and rheumatism [2](#page=2).
#### 2.2.4 Flavanoids and terpenoids
* **Flavanoids**, found abundantly in fruits and vegetables, are C6C3 compounds with three acetate units. They are recognized for their "healthy" properties, acting as antioxidants and contributing to the prevention of cardiovascular diseases and cancer [3](#page=3).
* **Terpenoids** include compounds like Paclitaxel (Taxol®), originally derived from *Taxus brevifolia* and *Taxus baccata*. Derivatives and precursors, such as 10-deacetyl-baccatin III, are also significant. Paclitaxel is an antitumoral drug that inhibits mitosis by stabilizing microtubules. Related drugs include docetaxel (Taxotere®) and cabazitaxel (Jevtana®) [3](#page=3).
#### 2.2.5 Aloe Vera
* **Aloe Vera** contains parenchyma tissue with mucilaginous compounds. It is widely used in cosmetics for sunburn and other skin conditions [3](#page=3).
#### 2.2.6 Other plant-derived compounds
* **Vlassael and psyllium seeds** are both used as bulk-forming laxatives [3](#page=3).
* **Flaxseed** (*Linum usitatissimum*) shares similar laxative properties with psyllium seed [3](#page=3).
---
# Alkaloids and their pharmacological effects
Alkaloids are a diverse group of naturally occurring compounds, primarily derived from plants, which possess a wide array of pharmacological actions and are used in various therapeutic applications [4](#page=4) [5](#page=5) [6](#page=6).
### 3.1 Classification and examples of alkaloids
Alkaloids can be broadly classified based on their structural origins and the plant sources from which they are derived [4](#page=4) [5](#page=5) [6](#page=6).
#### 3.1.1 Opium alkaloids
Opium alkaloids are derived from the opium poppy, *Papaver somniferum*. This class includes significant compounds like morphine, codeine, thebaine, noscapine, papaverine, and the semi-synthetic derivative, heroin [4](#page=4).
* **Morphine:** A potent analgesic and highly addictive substance, it mimics the action of endogenous endorphins and enkephalins involved in pain perception. It is commonly used for pain relief in terminal cancer patients [4](#page=4).
* **Codeine:** A methylether of morphine, it is a weaker analgesic, a cough suppressant, and a prescription drug with partial addictive potential and an obstipating side effect [4](#page=4).
* **Thebaine:** A precursor to semi-synthetic analgesics like oxycodone (e.g., OxyContin®), which is stronger than morphine. It is also a precursor to buprenorphine (e.g., Temgesic®), used as a withdrawal management agent for addicts [4](#page=4).
* **Noscapine:** A structurally different opium alkaloid, it acts as a cough suppressant without being addictive or narcotic [4](#page=4).
* **Papaverine:** Also structurally distinct, it functions as a musculotropic spasmolytic, relaxing smooth muscle cells. It was historically used for intestinal cramps and vasodilation but is no longer commonly used [4](#page=4).
* **Heroin (diacetylmorphine):** A highly lipophilic derivative of morphine, allowing rapid entry into the central nervous system, making it a potent and highly addictive drug [4](#page=4).
* **Laudanum:** An older preparation, it is an opium tincture with saffron, historically used as an astringent for diarrhea and as a spasmolytic, but is no longer in use [4](#page=4).
#### 3.1.2 Tropane alkaloids
Tropane alkaloids are derived from plants like *Atropa belladonna* (deadly nightshade). Key examples include hyoscyamine (atropine) and hyoscine (scopolamine) [5](#page=5).
* **Hyoscyamine (atropine):** A prototype parasympatholytic, it causes relaxation of smooth muscle cells. It is used for spasms in the gastrointestinal tract or urinary tract and for asthmatic conditions [5](#page=5).
* **Hyoscine (scopolamine):** Primarily used for motion sickness [5](#page=5).
* **Examples of medications:** Ipratropium bromide (Atronase®) for chronic bronchitis and butylscopolamine (Buscopan®) for intestinal cramps are derived from tropane alkaloids [5](#page=5).
* **Cocaine:** Derived from the Coca plant (*Erythroxylon coca*), it is a stimulant, addictive drug [5](#page=5).
#### 3.1.3 Alkaloids derived from L-tyrosine
This group includes alkaloids with a structure originating from the amino acid L-tyrosine [5](#page=5).
* **Colchicine:** Obtained from *Colchicum autumnale* (meadow saffron), it is used to treat acute gout attacks [5](#page=5).
#### 3.1.4 Irido-indol alkaloids
These alkaloids, such as vinblastine and vincristine from *Catharanthus roseus* (Madagascar periwinkle), are crucial in cancer therapy by inhibiting DNA replication and transcription. Etoposide and teniposide, semi-synthetic derivatives related to lignans, also act as important anticancer agents through similar mechanisms [5](#page=5) [6](#page=6).
#### 3.1.5 Campothecine and its derivatives
Campothecin, found in the Chinese ornamental tree *Campotheca acuminata*, has derivatives like topotecan and irinotecan, which are used as anticancer drugs. The L-tryptophan structure is not recognizable in campothecin [6](#page=6).
#### 3.1.6 Kina alkaloids (quinine)
Quinine, isolated from the Cinchona tree (*Cinchona pubescens*), was the first antimalarial drug. Its derivatives, such as chloroquine and mefloquine, are also used to treat malaria. The L-tryptophan structure is not recognizable in quinine [6](#page=6).
#### 3.1.7 Ergotamine
Ergotamine is derived from the ergot fungus (*Claviceps purpurea*). The L-tryptophan structure is recognizable in ergotamine. It is used to treat acute migraine attacks (e.g., Cafergot®). A derivative, LSD, is a potent hallucinogen and drug [6](#page=6).
#### 3.1.8 Simple alkaloids
This category includes alkaloids with simpler structures and significant pharmacological effects [6](#page=6).
* **Ephedrine:** Exhibits a stimulating effect similar to adrenaline. Pseudoephedrine has a different configuration and is less stimulating, used in nasal drops for vasoconstriction and decongestion. Related compounds include amphetamine and MDMA (ecstasy) [6](#page=6).
* **Nicotine:** Found in the tobacco plant (*Nicotiana tabacum*), it stimulates digestion, suppresses appetite, has anti-diuretic effects, causes vasoconstriction, and hypertension. It is not responsible for lung cancer [6](#page=6).
### 3.2 Other natural products with pharmacological effects
While the focus is on alkaloids, the document also mentions other natural product classes with significant medicinal applications, such as statins, salicylates, and terpenoids [4](#page=4) [5](#page=5).
#### 3.2.1 Polyketides, phenylpropane derivatives, and their combinations
* **Statins:** Originally derived from oyster mushrooms (*Pleurotus ostreatus*) as mevastatin and lovastatin, they are now synthetically produced with the same basic structure (e.g., simvastatin, pravastatine). They are cholesterol-lowering drugs used for cardiovascular conditions [4](#page=4).
* **Salicylic acid:** Derived from willow bark (*Salix* species) in the form of salicin, which is converted to salicylic acid in the liver after oral intake. Its synthetic derivative, acetylsalicylic acid (Aspirin®), is used for its analgesic, antipyretic, and anti-inflammatory properties [5](#page=5).
* **Naphthoquinones:** Lawsone, a red-orange dye from *Lawsonia inermis* (Henna plant), is the basis for atovaquone, a drug used against malaria [5](#page=5).
* **Terpenes:** Artemisinin from *Artemisia annua* (sweet wormwood) is highly active against malaria. Derivatives like dihydroartemisinin, artemether, arteether, and artesunate are also used [5](#page=5).
#### 3.2.2 Cardiac glycosides
Also known as "heart-acting glycosides," these are found in plants like foxglove (*Digitalis purpurea*) and woolly foxglove (*Digitalis lanata*). They have a reinforcing effect on the heart, increasing contractility in cases of heart failure, particularly in the elderly. Digoxin is a well-known example [5](#page=5).
---
## Common mistakes to avoid
- Review all topics thoroughly before exams
- Pay attention to formulas and key definitions
- Practice with examples provided in each section
- Don't memorize without understanding the underlying concepts
Glossary
| Term | Definition |
|------|------------|
| Heermoes | Also known as horsetail, this plant is rich in minerals and possesses diuretic and wound-healing properties. |
| Ginkgo biloba | A tree known as the maidenhair tree, its extract is believed to improve blood circulation and combat age-related dementia, symbolizing longevity. |
| Atovaquone | A drug used to treat malaria, derived from the sundew plant (Drosera), which traps insects for nutrients using epidermal hairs. |
| Matricariae flos | The dried flower heads of German chamomile, used in anti-inflammatory creams, teas for gastrointestinal problems, and cosmetics for hair lightening. |
| Chamazulene | A chemical compound found in German chamomile, structurally related to ibuprofen, contributing to its anti-inflammatory effects. |
| Dextrose | Another name for glucose, commonly referred to as grape sugar. |
| Lactulose | A semi-synthetic disaccharide with a laxative effect, used in medications like Duphalac and Bifiteral. |
| Acarbose | An oligosaccharide derived from the actinomycete Actinoplanes, acting as an inhibitor of alpha-glucosidase, thus reducing glucose absorption in the body. |
| Dextran | A glucose polymer used as a plasma expander to increase blood volume. |
| Hyaluronic acid | A polymer of N-acetyl-glucosamine and glucuronic acid found in connective tissue and the vitreous humor of the eye, used in cosmetics for hydration and eye drops. |
| Heparine | A polysaccharide derived from animal organs, acting as an anticoagulant to prevent and treat deep vein thrombosis; low molecular weight heparins like enoxaparin and nadroparin are derivatives. |
| Tragacanth | A type of gum used as a swelling agent to create suspensions and prevent precipitation. |
| Acacia gum | Also known as gum arabic, it is a swelling agent for suspensions, a binder, and an adhesive, historically used on postage stamps. |
| Alginezuur | An alginic acid derived from brown algae, used as a thickening agent in the food industry and to form a protective layer against gastroesophageal reflux when combined with antacids. |
| Heemst | Marshmallow root (althaeae radix) used to prepare mucus solutions through maceration in cold water, acting as an expectorant for cough preparations to soothe the respiratory tract. |
| Vlozaad | Plantago seed, also known as psyllium seed, used as a bulk-forming laxative when taken whole with sufficient water. |
| Flavanoids | Compounds composed of C6C3 units plus three acetate units found in fruits and vegetables, known for their antioxidant properties and role in preventing cardiovascular diseases and cancer. |
| Paclitaxel (Taxol) | An antitumoral drug derived from the yew tree (Taxus brevifolia and Taxus baccata), which inhibits mitosis by stabilizing microtubules. |
| Opium alkaloids | A group of alkaloids derived from the opium poppy (Papaver somniferum), including morphine, codeine, thebaine, noscapine, papaverine, and heroin, with various pharmacological effects. |
| Morphine | A potent opium alkaloid with sedative and addictive properties, used for pain relief, particularly in terminal cancer patients, and structurally similar to endorphins. |
| Codeine | A weaker analgesic and antitussive derived from morphine, requiring a prescription and having a risk of dependence, with an obstipating side effect. |
| Noscapine | An antitussive alkaloid with a different structure from morphine, not causing addiction or sedation. |
| Papaverine | An opium alkaloid with musculotropic spasmolytic properties, relaxing smooth muscle cells, historically used for intestinal cramps and vasodilation, though less common now. |
| Heroine | Diacetylmorphine, a highly lipophilic derivative of morphine that readily enters the central nervous system, known as a strong and addictive drug. |
| Statines | Cholesterol-lowering drugs originally derived from oyster mushrooms (Pleurotus ostreatus), with synthetic versions like simvastatin and pravastatin now widely used. |
| Salicylic acid | A compound originally found in willow bark (Salix species) as salicin, which is converted to salicylic acid in the liver; acetylsalicylic acid (Aspirin) is a synthetic derivative used for pain relief, fever reduction, and anti-inflammatory effects. |
| Lawsone | A red-orange dye from the henna plant (Lawsonia inermis), from which atovaquone, an antimalarial drug, is derived. |
| Lignans | Compounds composed of two C6C3 building blocks, some semi-synthetic derivatives like etoposide and teniposide are important anticancer agents that inhibit DNA replication and transcription. |
| Artemisinine | A potent antimalarial compound derived from Artemisia annua (sweet wormwood), with derivatives like artemether, arteether, and artesunate. |
| Digoxine | A cardiac glycoside from foxglove (Digitalis purpurea and Digitalis lanata) that strengthens heart contractions, used in treating heart insufficiency. |
| Tropane alkaloids | A class of alkaloids including hyoscyamine (atropine) and hyoscine (scopolamine) from plants like Atropa belladonna, acting as parasympatholytics to relax smooth muscles, used for cramps, asthma, and motion sickness. |
| Cocaine | A stimulant and addictive drug derived from the coca plant (Erythroxylon coca). |
| Colchicine | An alkaloid from Colchicum autumnale (meadow saffron) used to treat acute gout attacks. |
| Vinblastine, Vincristine | Iridoid-indole alkaloids derived from Catharanthus roseus (Madagascar periwinkle) used in cancer therapy. |
| Campothecine | A compound from the Chinese ornamental tree Campotheca acuminata, with derivatives like topotecan and irinotecan used as anticancer drugs that inhibit DNA replication and transcription. |
| Kina alkaloids (quinine) | Alkaloids from the Cinchona pubescens tree, historically the first antimalarial drugs, with derivatives like chloroquine and mefloquine also used against malaria. |
| Ergotamine | An alkaloid from the ergot fungus (Claviceps purpurea), used for acute migraine attacks; its derivative LSD is a potent hallucinogen. |
| Ephedrine | A simple alkaloid with a stimulating effect similar to adrenaline, found in nasal drops for vasoconstriction and decongestion. |
| Nicotine | An alkaloid from the tobacco plant (Nicotiana tabacum) with effects on digestion, appetite suppression, and vasoconstriction; it is not responsible for lung cancer. |