Herbal And THM

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Herbal and traditional herbal medication

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Herbal And THM

  1. 1. Herbal and traditional medicinesDr Liesl BrownDepartment of PharmacyUniversity of Limpopo(Medunsa Campus)Module 4.2: Health SystemsPharmacy (2011)
  2. 2. Saint John’s Wort (Hypericumperforatum)
  3. 3. Saint John’s Wort (Hypericum perforatum)Preparation and dosage Medicinal uses• Half cup of boiling water poured • Antidiarroheals over two teaspoons of coarsely • Rheumatism powdered drug, -> strained after • Gout 10 min • Anti-depressant • Treatment of wounds & 1st degreeActive ingredients burns• Naphthodianthrone hypericum • Supportive rx of nervous• Hypericum-like substances excitement + sleep disorders• Flavanoids (Germany) – Rutin • Back pain, groin pain, fevers and – Hyperin rx of wounds (H. aethiopicum) – Isoquercetrin – Bioflavonoids Pharmacological effects – Up to 3% of hyperforin (antibac.) • Antidepressant (? Linked to MAO inhibition) ?? Hypericin • Antiviral activity
  4. 4. Ginkgo (Ginkgo biloba)
  5. 5. Ginkgo (Ginkgo biloba) isiphemba, isiqumama (Zulu)Preparation and dosage Medicinal uses• Roots are smoked • Dried roots, smoked -> asthma• ?? Methods of administration relief • Smoke of whole plant -> nose bleedingActive ingredients • Stem bark (X. spekei) -> general• Chemical compounds are aches and pains, anti-inflam., post poorly known partum haemorrhage• Bioflavonoids have been reported Pharmacological effects• Amento flavone (dimer ofginkgo extract) • ?? Flavanoids response -> effects ??• Dipenteroids • Capillary fragility – Cleistanthatetraenes – Cleistanthateranols • Antispasmodic • Anti-allergic
  6. 6. Valerian (Valeriana officinalis and Valeriana species)
  7. 7. Valerian (Valeriana officinalis and Valeriana species)Preparation and dosage Pharmacological effects• Dried roots/root extracts • Terpenoids & Valepotriates = GABA-A activity (V. officialis) -> sedative effectsActive ingredients • Sesquiterpenoids -> sedatives• Sesquiterpenoids (incl. • Terpenoid & valepotriate -> valerenic acid & valeranone) spasmolytical activity• Iridoids (aka valepotriates) • Insomnia – Forms complex mixtures with valerate as the main comp. • Symptoms of neurotonic disordersMedicinal uses• Nervous disorders• Hysteria• Epilepsy• Mixed with other plant materials e.g.. ‘kattekruie’
  8. 8. Kava-kava (Piper methysticum)
  9. 9. Kava-kava (Piper methysticum) Ava. Intoxicating Pepper. Ava PepperPreparation and dosage Pharmacological effects• The peeled, dried and divided rhizome • Effect on the nerve centres -> used stimulating, -> depressing, -> paralysis• Fluid extract, ½ - 1 drachm. Powdered of the respiratory centre root, 1 drachm. Solid extract, 1 - 15 • Local anesthetic (relieves pain; grains aphrodisiac effect)• The capsules contain 0.3 g; 2-4 caps. • Gonorrhea (acute and chronic), several times per day vaginitis • Leucorrhoea, nocturnal incontinenceActive ingredients • other ailments of the genitourinary• Greenish-yellow resin – kawine tract (strongly aromatic and acrid) • A 20% oil of Kava resin/oil of• Kavaine Methysticcum yangonin – Sandalwood (= gonosan) - internally volatile oil and alkaloid (< active than for gonorrhea kawine) • Urine antiseptic • Strong diuretic it is useful for gout,Medicinal uses rheumatism, bronchial and other• It resembles pepper in local action ailments, resulting from heart trouble• Fermented liquor (rhizome - upper portion) & base of the stems) - narcotic & stimulant (drunk before important religious rites)• The root of the plant chewed & mixed with the saliva, (->intoxicating juice, mixed with pure H20/H20 of coco-nut)
  10. 10. Cola nut (Dombeya rontundiflora)inhlizya enkulu (Zulu); motubane (Tswana); mulanga (Venda); mohlabaphala (N. Sotho)
  11. 11. Cola nut (Dombeya rontundiflora) inhlizya enkulu (Zulu); motubane (Tswana); mulanga (Venda); mohlabaphala (N. Sotho)Preparation and dosage Medicinal uses• Infusions / deconcotions of the • Internal ulcers -> infusions (orally / bark (rarely roots) enemas) – Give: orally / injected enemas • Haemorrhoids – Sometimes mixed with other • Diarrhoea ingredients • Stomach problems• Powdered root -> burnt and • ?? Nausea – pregnant women smoke inhaled where after the powder is used as snuff • When labour is delayed->• decoctions of bark is given to Bark is chewed hasten birth • Chest complaintsActive ingredients• No published info. on chemical Pharmacological effects composition of Dombeya sp. • No details about pharmacological• Other members: activity – Purine bases e.g. caffeine
  12. 12. Guarana (Ginseng)
  13. 13. Guarana (Ginseng) Panax quinquefolium Aralia quinquefolia. Five Fingers. Tartar Root. Red Berry. Mans Health, 人参 (ninjin = carrot, Japanese)Preparation and dosage Medicinal uses (cont.)A decoction of 1/2 oz. of the root, boiled in • Western medicine: tea or soup and taken every morning – stomachic tonic – stimulant, useful in loss of appetiteActive ingredients – digestive affections that arise from• Starch (l/s), gum, some resin, volatile mental and nervous exhaustion oil (s/s), sweetish body, Panaquilon (= – lower blood glucose yellow powder, precipitating with water – beneficial effects on immune a white, amorphous substance – function Panacon) Pharmacological effectsMedicinal uses • Adaptogenic effects (e.g. anti-fatigue,• China: well-being, increase vigor, longevity) – dyspepsia, vomiting and nervous • Heart & Circulation (e.g. regulate chol. disorders Level, BP, BG)• Remedy for consumption and other • Immunity enhancer diseases • Reproductive fx (e.g. M+F menopause, impotence)
  14. 14. Chamomile
  15. 15. Ma-huang (Ephedra)
  16. 16. Ma-huang (Ephedra) Sea ephedrine, ephedra, ephedra alkaloids, sea grape, yellow horse, yellow astringent, joint fir, squaw tea, Mormon tea, popotillo, teamsters tea• Reported to cause serious, even fatal, side effects such as heart attack, stroke, irregular heartbeats, and sudden death, the FDA has recommended that consumers not take ma huang• When considering the use of herbal supplements, consultation with a primary health care professional (trained in the uses of herbal/health supplements) is advisable• Ma huang has been used as a stimulant and for weight loss and appetite suppression• Ma huang has not been evaluated by the FDA for safety, effectiveness or purity• All potential risks and/or advantages of ma huang may not be known• No regulated manufacturing standards in place for these compounds• Other uses, not listed here
  17. 17. Feverfew (Tanacetum parthenium)
  18. 18. Feverfew (Tanacetum parthenium) Pyrethrum Parthenium (Sm.). Featherfew. Featherfoil. Flirtwort Bachelors ButtonsPreparation and dosage• Not be used in children < 2 yrs Medicinal uses• Fluid extract: dose, 1 – 2 drachms • hysterical complaints, nervousness,• The cold infusion is made from 1 OZ. lowness of spirits, general tonic, migraine of the herb to a pint of boiling water, cooled, and taken frequently in doses • Coughs, wheezing, asthma and of half a teacupful (125 ml) difficult breathing (decoction with sugar• Preparations to contain > 0.2% or honey) parthenolide • The herb, bruised and heated, or fried• Dosages are calculated on an average with a little wine and oil, -> warm external application for wind and colic of 70 kg adult • Pain and swelling - bites of insects and vermin (pain and swelling),Active ingredients rheumatoid arthritis• Parthenolide (-> relieves smooth • Distressing sensitiveness to pain (in a muscle spasms) highly nervous subject)• Parthenolide (-> inhibits the actions of • Face-ache or earache of a dyspeptic compounds that cause inflammation) or rheumatic personPharmacological effects• Inflammatory pathways; platelet aggregation, vascular smooth muscle contraction, migraine
  19. 19. Drug-herb interactions: -HIV/ARV herb interactions Indinavir, nevirapine and St John’s Wort• Saint John’s Wort (SJW) (Rx depression)1 – ?? SJW enhances metabolism of CYP3A4 substrates1 – -> decrease in the plasma level of indinavir and halving its AUC2 – oral clearance of NVP is elevated -> ineffective if taken concurrently with SJW3 - Induced P-gp expression at low, clinically relevant concentrations may explain the decreased bioavailability of P-gp substrates (e.g. indinavir) when co-administrated with SJWIoannides, (2002:451-478); 2 (Piscitelli et al., 2000:547); 3 (De Maat et al., 2001:420); 4 Hennessy et al., (2002:75)1
  20. 20. Drug-herb interactions Interactions between HIV/ART drugs and grapefruit• Soldner et al., (1999:478) investigated the role of grapefruit juice (GFJ) in P-gp mediated drug transport – ?? GFJ significantly activated P-gp mediated efflux of drugs that were substrates for P-gp, potentially counteracting its CYP3A4 inhibitory effects• Romiti et al., (2004) explained that the inhibitory effect of GFJ in the down regulation of P-gp as well as the inhibition of its functions or related components in tubular cells could have a role in changing disposition of some important therapeutic agents
  21. 21. Drug-herb interactions -HIV/ARV herb interactionsInteractions between HIV/ART drugs and garlic-Foster et al, (2001) found that garlic inhibits cytochrome P450 2C9*1,2C19, 3A4, 3A5 and 3A7 mediated metabolism of marker substrates -The activity of CYP2D6 mediated-metabolism was unaffected -The extracts of garlic exhibited a very low to moderate P-gpinhibition as compared to the + control VER-Saquinavir  displayed a 51% drop in its AUC, probably due toinduction of CYP enzymes by garlic supplementation-Back et al., (2003:S12) warn against the potential interactions of herbs,including garlic, milk thistle and ginseng-Conway & Bartlett (2003:61) reported on interactions between bothNVP and NFV with garlicDe Maat et al, 2003:2731
  22. 22. ReferencesDE MAAT, M.M.R., HOETELMANS R.M.W., MATHÔT R.A.A., VAN GORP, E.C.M., MEENTHORST P.L., MULDER J.W. & BEIJNEN J.H. 2001. Drug interactions between St John’s wort and nevirapine. AIDS, 15:420-421.DE MAAT, M.M.R., EKHART, C.G., HUITEMA, A.D.R., KOKS, C.H.W., MULDER, J.W & BEIJNEN, J.H. 2003. Drug interactions between ARV drugs and comedicated agents. Clin. Pharmacokinet., 42(3):223-282.HENNESSY, M., KELLEHER, D., SPIERS, J.P., BARRY, M., KAVANAGH, P., BACK, D., MULCAHY, F AND FEELY, J. 2002. St John’s Wort increases expression of P-gp: Implications for drug interactions. Brit. J. Clin. Pharmaco., 53:75-82.IOANNIDES, C. 2002. Pharmacokinetic interactions between herbal remedies and medicinal drugs. Xenobiotica, 32(6):451-478.KATZUNG, BG. 2001. Basic & Clinical Pharmacology. 9th edition. Lange Medical Books/McGraw-Hill:New YorkPISCITELLI S.C., BURSTEIN A.H., CHAITT, D, ALFARO, R.M. & FALLOON J. 2000. Indinavir concentrations and St John’s wort. Lancet, 355:547-548.VAN WYK B-E, VAN OUTSHOORN, GERICKE N. 1997. Medicinal plants of South Africa, Briza Publications: Pretoria, South AfricaWONG, AHC, SMITH M, BOON HS. Year unknown. Herbal remedies in: Psychiatric practice. Journal of American Medicine. Volume and edition unknown, pp44-51INTERNET SOURCES - available at request http://www.botanical.com/botanical/mgmh/comindxg.html http://nccam.nih.gov/health/asianginseng/ http://www.eden.rutgers.edu/~piyun/ginseng.htm#Effects http://www.botanical.com/botanical/mgmh/f/feverf10.html http://www.umm.edu/altmed/ConsHerbs/Feverfewch.html#Composition http://www.campbell.edu/faculty/nemecz/George_home/references/Feverfew.html
  23. 23. PhD study: Anti-retroviral drug transport across intestinal epithelial cells: influence of tuberculosis drugs and traditional medicines (L Brown, 2007)HIV/ARV drugs: AZT, NVPTB drug: rifampicinTraditional herbal medicines: Sutherlandia frutescens (Cancer Bush), Hypoxishemerocallidea ( African Potato)Active compound of S. frutescens: L-canavanineP-glycoprotein (efflux drug transporter)
  24. 24. Aim Sutherlandia frutescensRifampicin + L-canavanine(TB drug) Hypoxis hemerocalidea (active of S. frutescens) (Traditional herbal medicines) ? P-gp Nevirapine (HIV ARV drug) Intestinal epithelial cells
  25. 25. Conclusions of the NVP experimentsExperimental group P-gp involvement CommentsNVP 1: (alone) √ NVP substrate Influences F of NVP (effluxed in BL-AP direction, P < 0.05)NVP 2: (NVP + VER) Inhibition (effluxed, Increases NVP F ⇓BL-AP, P < 0.05)NVP 3: (NVP + RIF) Inhibition (effluxed, Increase NVP F ⇓BL-AP, P < 0.05)NVP 4: (NVP + H. h) Inhibition (effluxed, Increase NVP F ⇓BL-AP, P < 0.05)NVP 5: (NVP + S. f) Inhibition (effluxed, Increase NVP F ⇓BL-AP, P < 0.05)NVP 6: (NVP + L- Inhibition (effluxed, Increase NVP F (firstCAV) ⇓BL-AP, P < 0.05) finding documented)

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