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Phytopharmaceuticals
- 2. CONTENT • Ephedra • Ginger • Garlic • Kava kava • Ginkgo biloba • Valerian • Chamomile • Echinacea • Ginseng • Cranberry • Acorus • Comfrey • Tomato • Liquorice • Senna • Cascara
- 3. EPHEDRA • Source: dried stem of • Ephedra sinica, E. equisentina (China) • E. gerardiana, E. intermedia, E. major (India, Paskistan) family Ephedraceae • Constituents: Ephedrine, pseudo ephedrine, methyl ephedrine • (norephedrine does not occur naturally, its presence is proof of adulteration) • Label claim: 10 or 11 mg ephedrine
- 4. EPHEDRA • Pharmacology: CVS & Respiratory effects • MOA: alpha 2, beta 1, 2, 3 receptor stimulator • Release of norepinephrine from nerve ending due to alpha2 & beta 1 • Not preferred for Asthma: downregulation quickly occurs and the bronchodilator effects are lost • No significant action on BP • Weight loss: Beta 3 (adipose tissue) receptor agonist
- 5. EPHEDRA • Clinical studies: • Asthma : no good result • Weight loss: ephedrine/caffeine combination showed good result • Athletic performance: ephedrine/caffeine combination showed good result • Pharmacokinetic: pure from is easily absorbed compared herbal extracted form
- 6. EPHEDRA • Toxicity: Neurological, Renal • Drug interactions: MAO • Therapeutic uses:Weight loss (ephedrine→ reduce body fat), • Athletic performance (increase dopamine → increase free fatty acids) • Dose: NMT 32 mg/day • Regulatory status: prohibiting the sale of dietary supplements containing ephedrine alkaloids (ephedra)
- 7. GINGER • Source: dried rhizomes of Zingiber officinale, Z. capitatum • Family: Zingiberaceae • Constituents: 6-Gingerol, Shagol • Pharmacology: • GIT effect: motion sickness (inhibition of 5HT3 receptors) • Anti inflammatory • Migraine prevention (inhibition of arachidonic acid metabolism)
- 8. GINGER • Pharmacokinetic: no human studies • Drug interactions:Antiplatelet, anticoagulants • Therapeutic uses: Nausea,Anti-inflammatory & analgesic • Recommended dose: 170 mg to 1 g → 3to4 times daily • Market preparation: Halls ginger, Himalaya Ginger digestive comfort • Regulatory status: official monograph USPNF and dietary supplement, OTC product for motion sickness
- 9. GARLIC • Source: dried bulbs of Allium sativum • Family: Liliaceae • Constituents: Sulphur containing compounds • Allicin, DAS, DADS, DATS,Ajoene • Pharmacology • CVS: reduce fibrinolytic activity, reduce LDL-cholesterol, antihypertensive, antiplatelet (inhibit HMG-CoA reductase and other lipogenic enzymes) • GI: relieve abdominal discomfort, gas, antibacterial (H.pylori)
- 10. GARLIC • Antifungal: topical garlic -1% ajoene • Pharmacokinetic: rapidly and easily absorbed in the gastrointestinal tract and distributed mainly in plasma, liver, and kidney • Adverse effects: if not refrigerated, contact dermatitis • Drug interactions:Antiplatelet,Anticoagulants,Anti HIV • Therapeutic uses: CVS,Antifungal • Recommended dose: up to 2.5 g fresh raw garlic • Market preparation: Himalaya lasuna cardiac wellness, Nutralite garlic heartcare
- 11. GARLIC • Regulatory status: GRAS (generally recommended as safe) • food
- 12. KAVA KAVA • Source: dried roots & rhizomes of Piper methysticum • Family: Piperaceae • Constituents: Kava lactones: Kawain, Methysticin,Yangonin, dihydrokawain • Pharmacology: • Neurological effects: antidepressant, anti-anxiety, anxiolytic (GABA binding in amygdala by Kavapyrone) • Sedation: (inhibition of noradrenaline uptake) • Anxiolytic, euphoric (mesolimbic dopaminergic pathway)
- 13. KAVA KAVA • Pharmacokinetic: excreted in urine • Adverse drug reactions: dermopathy (discoloration of skin, nail) • Drug interactions: alcohol + kava → hypnotic since kava inhibits metabolism of cytochrome • Therapeutic uses:Anxiety • Recommended dose: NMT 250mg (kava lactone), not in children • Market preparation: Kava stress relief, Girnar green tea Desi kaiwa • Regulatory status: worldwide either banned or issued waning, US dietary supplement
- 14. GINKGO BILOBA • Source: dried leaves of Ginkgo biloba (Syn. Maidenhair Tree) • Family: Ginkgoaceae • Constituents: Ginkgolides, Bilobalides, Flavonoids • Pharmacology: • CNS: neuron protection (antioxidant) • Memory/cognition improvement, little effect • Anxiolytic: blockage of 5HT3 receptors • Endocrine effects: increase blood glucose, decrease insulin
- 15. GINKGO BILOBA • Pharmacokinetic: good bioavailability but excreted in urine unchanged • Adverse drug reaction & toxicity: cerebral haemorrhage, increase bleeding time • Drug interactions:Antiplatelet • Therapeutic uses: improve blood flow to brain, improve peripheral circulation so sharpen focus • Recommended dose: 120-240 mg/day • Market products: GERITISIN tab 40 mg FDC • Regulatory status: US dietary supplement, Germany: memory & depression
- 16. VALERIAN • Source: dried roots, rhizomes & stolons of Valeriana wallichii (India), V. officinalis (Europe) • Family:Valerianaceae • Constituents:Valepotriates (Iridoid moiety) • Volatile oil- valerenic acid, valerenal, valerenol • Pharmacology: • Insomnia: improved sleep quality, latency depth (inhibition of enzyme that breakdown GABA) • Antidepressant: reuptake of MAO neurotransmitters
- 17. VALERIAN • Anxiety: reduce Systolic BP • Anxiolytic: due toValepotriates • Pharmacokinetic: • Fast absorption & elimination • Therapeutic uses: Sedative-Hypnotic (sedative),Anxiolytic (restlessness) • Recommended dose: Insomnia (400-600 mg/day 1 hr before bed time for 2-4 week) • Anxiety: 150mg/day in a 3 divided dose/4 week
- 18. VALERIAN • Market preparation: Himalaya Tagara, Natures answer valerian root 500 mg, Relaxul valerian • Toxicity: caution with antifungal & statin • Drug interactions: Barbiturates, Benzodiazepines,Alcohol, CNS depressant • Regulatory status: US does not recommend (due to insufficient data) • Safe as food & used as sleeping aid worldwide
- 19. CHAMOMILE • Source: flowers of Matricaria chamomilla • Family: Compositae • Constituents:Alpha bisabolol,Apigenin (flavonoid), Coumarin • Pharmacology: • Neurologic effect: Chamomile oil vapour (action on GABA) • Sunscreen & Skin cancer: Flavonoids-apigenin (inhibition of protein kinase C) • Anti-inflammatory: mucositis, stomatitis
- 20. CHAMOMILE • Toxicity:Anaphylaxis • Pharmacokinetic; Blood, Urine • Therapeutic uses: Skin & mucous membrane inflammation • Recommended dose: 11 to 15 g/day, topical cream, gel,oil • Market preparation: VLCC neem facewash with chamomile, O3+ chamomile hydrating, Lotus • Regulatory status: chamomile & its oil official in USP, EP • Dietary supplement & GRAS status
- 21. ECHINACEA • Source: roots, leaves & flowers of Echinacea purpurea, E. angustifolia, E. pallida (Syn. Coneflower) • Family: Compositae • Constituents: Echinacoside (caffeic acid derivative)-PHENOL • Unsaturated fatty acid-alkylamide • Pharmacology: • Immunologic effect: Cichoric acid, polysaccharide, alkylamide (phagocytic activity), increase WBC, IL-2 level • Antimicrobial : Upper respiratory Tract infection
- 22. ECHINACEA • Antiviral: Herpes simplex virus (HSV) • Antifungal: polyacetylene increase amount of TNF-alpha so inhibit growth of yeast • Would healing: Echinacoside has antihyaluronidase action • Anti-inflammatory:Alkylamide→COX2 inhibitor • Pharmacokinetic: rapid absorption after single dose
- 23. ECHINACEA • Adverse drug reaction: Immunosuppressant, pyrrolizidine alkaloid→ liver toxicity • Therapeutic uses: 300 mg dry powdered extract (echinacoside 3.5%) • Market preparation: Echinacea immunity (ALLEN) 400 mg, Echinacea plus tonic, Echinaforce cold & flu oral dops (A.Vogel) • Regulatory status: dietary supplement (US), OTC homeopathic drug
- 24. GINSENG • Source: dried roots of Panax ginseng • Family:Araliaceae • Constituents: Pentacyclic triterpene: Ginsenosides • Pharmacology: • Endocrine effects: hypoglycemic, increase hepatic lipogenesis, glycogen storage • Anti fatigue: Ginsenoside (increase ACTH, Cortisol) • Neurologic effect: CNS stimulant, dementia, cognition
- 25. GINSENG • Immunologic effect: • Red ginseng: increase cell mediated immunity • Pharmacokinetic: • Bioavailability 49%, distributed in kidney, excreted in urine • Therapeutic uses: Anti-stress, Adaptogen, Stimulate immunity, mental and physical wellness • Marketed preparation: Revital (212.5 mg), Supractiv capsule • Recommended dose: 1-2 g/thrice upto 3 months
- 26. GINSENG • Contraindications/ Adverse drug reactions: Hypersensitivity,Anaphylaxis, • Inappropriate uses: BP, Diarrhea, Depression, Sleeplessness • Regulatory status: • Germany: non prescription drug, fatigue, debility • US: dietary supplement
- 27. CRANBERRY • Source: fruits ofVaccinium macrocarpon • Family: Ericaceae • Constituents: Flavonoids, Proanthocyanidins • Pharmacology: • Antimicrobial: Fructose + Glycoprotein (inhibiting adherence to mucosal surface) • Mild antiviral (polyphenols) • GIT: large amount (more than 3 to 4 liter/day). Diarrhea, GI symptoms
- 28. CRANBERRY • Renal effects: lower urine pH, reduce urinary complaints, calculus management • Recommended dose: up to 1 liter/ day juice up to 1200 mg/day capsule • Toxicity & Drug interactions:Warfarin, Diabetes • Therapeutic uses: symptomatic relief to UTI, improve odor • Marketed preparation:Tropicana, Real cranberry juice • Cranfit tablet (Cranberry + D-mannose 300 mg) • Regulatory status: Dietary supplement, Food
- 29. ACORUS • Source: dried rhizomes of Acorus calamus (Syn. Sweet flag) • Family:Acoraceae • Constituents: Beta Asarone (volatile oil), Bitter acorine • Pharmacology: • Musculoskeletal: Spasmolytic • CVS effect: In vitro, negative inotropic effect • Pharmacokinetic: • Toxicity: contact dermatitis
- 30. ACORUS • Therapeutic uses: Ulcers, upset stomach • Recommended dose: 250-500 mg powder • Market preparation: Goorganic Vacha powder, Surajbala ancient healer calamus essential oil • Regulatory status: banned in US due to concern over carcinogenicity
- 31. COMFREY • Source: dried leaves of Symphytum officinale (Syn. Bruise wart, Knitback, Knitbone) • Family: Boraginaceae • Constituents: Rosmarinic acid, Mucopolysaccharide, allantoin, mucilage, symphytin • Pharmacology: • GIT effect: peptic ulcer (more release of prostaglandins) • Hepatotoxicity: due to Symphytine • Shorten dermal use not dangerous
- 32. COMFREY • Pharmacokinetic: absorption through skin & GIT • Therapeutic uses: Burn, Swelling, Sprain • Recommended dose: NMT 100 microgram/day, not exceeding 4-6 week/year • Market preparation: Nature’s aid comfrey oil, Comfrey adult diapers, VLCC vitalift comfrey & soy anti-aging serum • Regulatory status: not acceptable as food, External use • US: no internal use
- 33. TOMATO • Source: fruits of Solanum lycopersicon • Family: Solanaceae • Constituents: Carotenoid – lycopene • Pharmacology: • CVS: • Anticancer: interfere with growth factor induce apoptosis cell
- 34. TOMATO • Pharmacokinetic: • Concentration: Liver, adrenal, spleen, lymph node, intestine • Therapeutic uses:Antioxidant, Cancer prevention, CVS prevention • Market preparation: Healthvit lycopene 1000 microgram capsule • Lycored syrup • Zenith nutrition lycopene with multivitamin capsule • Recommended dose: 7 to 75 mg/day • 10-30 mg/ twice with meals
- 35. TOMATO • Contraindications: • Hypersensitive,Acidic stomach ulcer • Adverse drug reactions: diarrhea, dyspepsia, Gas, Nausea • Leaf→ unsafe • Toxicity: not known • Regulatory status: food ingredient
- 36. LIQUORICE • Source: dried roots & stolons of Glycyrrhiza glabra • Family: Leguminosae • Constituents: tri-tepenoid saponin-Glycyrrhizin, • Pharmacology: • Respiratory effect: cough, expectorant (insufficient data) • GIT effects: increase mucous secretion, life span of gastric epithelial cells, inhibition of back diffusion of hydrogen ions • Toxicity & Adverse drug reactions: Hypokalemia, pulmonary edema, hypertension
- 37. LIQUORICE • Source: dried roots & stolons of Glycyrrhiza glabra • Family: Leguminosae • Constituents: tri-tepenoid saponin-Glycyrrhizin, • Pharmacology: • Respiratory effect: cough, expectorant (insufficient data) • GIT effects: increase mucous secretion, life span of gastric epithelial cells, inhibition of back diffusion of hydrogen ions • Toxicity & Adverse drug reactions: Hypokalemia, pulmonary edema, hypertension
- 38. LIQUORICE • Therapeutic uses: Sore throat, cough, gastritis (GI) Complaints • Recommended dose: 760 mg-15 g for ulcer, gastritis 0.2 mg/kg/day • Market preparation: Gutgard (Gastric) Natural remedy • VLCC licorice cold cream, Dabr honitus syrup • Regulatory status: not recommended in potassium deficiency, • US-dietary supplement, food additive • Germany-peptic ulcer
- 39. SENNA • Source: dried leaves & leadflets of Cassia angustifolia, C. acutifolia • Family: Leguminosae • Constituents: Dianthrone (sennoside A, B, C, D) • Pharmacology: • GIT effects: laxative • Pharmacokinetic: high molecular weight → poor absorption • Therapeutic uses: Constipation • Marketed preparation: GNC herbal plus senna leaf ext, Laxa HealthTea
- 40. SENNA • Recommended dose: 172 mg/day • Drug interactions: Digoxin, Diuretic, Blood thinner • Regulatory status: Germany, US approved • From Category 1 to 3 (insufficient data) • Toxicity: Bowels’ disorders, Crohn;s disease, heart
- 41. CASCARA • Source: dried bark of Rhamnus purshiana (Syn. Sacred bark, Buckthorn) • Family: Rhamnaceae • Constituents: Cascaroside • Pharmacology: • GIT effect: laxative (active secretion of H2O, electrolyte within lumen of small intestine,Athrone→ inhibit absorption of H2O, electrolyte in bowel • Strength dilation of pressure in intestine to stimulate peristalsis [ 1 year storage, oxidation to allow harsh constituents, fresh bark → not used intestinal cramps • Contraindications: Crohn’s disease, Ulcerative colitis
- 42. CASCARA • Therapeutic uses: Laxative • Recommended dose: 1 g of bark, 2-6 ml of fluid extract, 100-300 mg of dried bark extract • Regulatory status: • USP monograph, dietary supplement • Category 1 to 3 (more safety data needed)