Herbal And THM

Herbal And THM

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  Herbal and traditional medicines Dr Liesl Brown Department of Pharmacy University of Limpopo (Medunsa Campus) Module 4.2: Health Systems Pharmacy (2011)
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  Saint John’s Wort(Hypericum perforatum)
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  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 degree Active 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
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  Ginkgo (Ginkgo biloba)
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  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 bleeding Active 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
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  Valerian (Valeriana officinalisand Valeriana species)
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  Valerian (Valeriana officinalisand Valeriana species) Preparation and dosage Pharmacological effects • Dried roots/root extracts • Terpenoids & Valepotriates = GABA-A activity (V. officialis) -> sedative effects Active 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 disorders Medicinal uses • Nervous disorders • Hysteria • Epilepsy • Mixed with other plant materials e.g.. ‘kattekruie’
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  Kava-kava (Piper methysticum)
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  Kava-kava (Piper methysticum) Ava. Intoxicating Pepper. Ava Pepper Preparation 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 incontinence Active 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)
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  Cola nut (Dombeyarontundiflora) inhlizya enkulu (Zulu); motubane (Tswana); mulanga (Venda); mohlabaphala (N. Sotho)
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  Cola nut (Dombeyarontundiflora) 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 complaints Active ingredients • No published info. on chemical Pharmacological effects composition of Dombeya sp. • No details about pharmacological • Other members: activity – Purine bases e.g. caffeine
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  Guarana (Ginseng)
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  Guarana (Ginseng) Panaxquinquefolium Aralia quinquefolia. Five Fingers. Tartar Root. Red Berry. Man's 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 appetite Active 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 effects Medicinal 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)
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  Chamomile
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  Ma-huang (Ephedra)
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  Ma-huang (Ephedra) Seaephedrine, 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
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  Feverfew (Tanacetum parthenium)
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  Feverfew (Tanacetum parthenium) Pyrethrum Parthenium (Sm.). Featherfew. Featherfoil. Flirtwort Bachelor's Buttons Preparation 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 person Pharmacological effects • Inflammatory pathways; platelet aggregation, vascular smooth muscle contraction, migraine
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  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 SJW Ioannides, (2002:451-478); 2 (Piscitelli et al., 2000:547); 3 (De Maat et al., 2001:420); 4 Hennessy et al., (2002:75) 1
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  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
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  Drug-herb interactions -HIV/ARV herb interactions Interactions 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-gp inhibition as compared to the + control VER -Saquinavir  displayed a 51% drop in its AUC, probably due to induction 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 both NVP and NFV with garlic De Maat et al, 2003:273 1
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  References DE 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 York PISCITELLI 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 Africa WONG, AHC, SMITH M, BOON HS. Year unknown. Herbal remedies in: Psychiatric practice. Journal of American Medicine. Volume and edition unknown, pp44-51 INTERNET 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
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  PhD study: Anti-retroviral drug transport across intestinal epithelial cells: influence of tuberculosis drugs and traditional medicines (L Brown, 2007) HIV/ARV drugs: AZT, NVP TB drug: rifampicin Traditional herbal medicines: Sutherlandia frutescens (Cancer Bush), Hypoxis hemerocallidea ( African Potato) Active compound of S. frutescens: L-canavanine P-glycoprotein (efflux drug transporter)
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  Aim Sutherlandia frutescens Rifampicin + L-canavanine (TB drug) Hypoxis hemerocalidea (active of S. frutescens) (Traditional herbal medicines) ? P-gp Nevirapine (HIV ARV drug) Intestinal epithelial cells
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  Conclusions of theNVP experiments Experimental group P-gp involvement Comments NVP 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 (first CAV) ⇓BL-AP, P < 0.05) finding documented)