Sport nutritional supplements & drugs interactions

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Herbal Medicines for
Neurologic disorders
Hamid R. Sadeghnia
Department of Pharmacology, School of Medicine, MUMS
US dietary
supplement
market
(Rea & Ooyen 2009)
US $23.7 billion with a predicted
compound annual growth rate of 5%
Outlines
• ANALGESIC AGENTS
• ANTIANXIETY AGENTS, SEDATIVES & HYPNOTICS
• ANTICONVULSANTS
• ANTIDEPRESSANTS
• APPETITE STIMULANTS
• CENTRAL NERVOUS SYSTEM STIMULANTS
• CHOLINESTERASE INHIBITORS &COGNITIVE ENHANCING AGENTS
• MIGRAINE PREPARATIONS
• VERTIGO AGENTS
Barberry (Berberis vulgaris)
• The medicinal part is the fruit and the root bark
• Isoquinoline alkaloids (berberine) & vit. C
• Berberin
• Competitive α1 & α2 adrenergic blocking effects
• Anticonvulsant and antispasmodic effects
• Daily Dosage: up to 2 g
• Opiate withdrawal symptoms
• Barberry root bark
Boswellia (Boswellia serrata)
• The resin gum exuded when incisions are made in the bark of the trunk
• Pentacyclic triterpene acids: Boswellic acids
• Brain vascular insufficiency (memory loss, cognitive decline,
Alzheimer’s disease)
• Increase CBF
• Inflammatory conditions (rheumatoid arthritis, MS, Asthma)
• Anti-inflammatory effect (inhibition of LOX & LTs production)
• Sedative & analgesic properties
Chamomile
• German Chamomile (Matricaria Recutita): the entire flowering herb or only the flowers
• Volatile oil: alpha-bisabolol (levomenol)
• Flavonoids: apigenin, luteolin, quercetin
• Anxiolytic Effects
• Flavonoids: Apigenin is a ligand for the central BDZ receptors
• Daily dosage: 3 g at the main meals
• Caution: Anaphylactic Reactions
• Drug Interactions:
• Coumarin Anticoagulants: additive effects due to the hydroxycoumarins in chamomile
Chamomile
• English Chamomile or Roman Chamomile (Chamaemelum nobile):
flowers & aerial parts
• Sedative
• Daily dosage: 1.5 g at the main meals
• The drug is not to be used during pregnancy
Cinnamon (Cinnamomum verum)
• The dried tree bark, the cinnamon oil extracted from the
bark
• Volatile oil: cinnamaldehyde, cinnamic acid, eugenol
• Diterpenes: cinnzeylanin, cinnzeylanol
• Alzheimer’s disease, Loss of appetite
• Daily Dosage: 2 to 4 g drug
Esfand or Harmal (Peganum harmala)
• CNS stimulant & antidepressant activity
• Harmala alkaloids: harmane, harmine, harmaline,
harmalol
• β-carboline
• Reversible inhibitor of MAO-A (RIMA)
• Acetylcholinesterase inhibitor
• Histamine N-methyltransferase inhibitor (wakefulness-promoting effects)
• Daily dosage: 1 g
Fennel (Foeniculum vulgare)
• Fennel oil extracted from the fruit and seeds
• Trans-anethols, Fenchone, Estragole, Hydroxycoumarins
• Central analgesic effect, memory-strengthening effect (antiacetylcholinestrase activity)
• Daily Dosage: 0.1-0.6 ml of Fennel oil (5-7 g fennel seed)
‫رازیانه‬
Ginger (Zingiber officinale)
• The root
• Volatile oil: zingiberene, zingiberol, linalool
• Gingerols
• Shogaols
• Anti-emetic Effects (Motion Sickness, Postoperative Nausea and Vomiting)
• Local gastrointestinal actions
• Positive inotropic, antithrombotic & platelet aggregation inhibitory (inhibit
thromboxane synthesis), anti-lipidemic effects
• Anti-dyspepsia
‫زنجفيل‬
Ginger (Zingiber officinale)
• Anti-migraine
• Anti-Inflammatory Effects
• Inhibition of COX & 5-LOX
• Immunomodulation (RHEUMATOID ARTHRITIS,
OSTEOARTHRITIS)
• Drug interactions: anticoagulants
• Daily dosage: 2-4 g
Ginkgo (Ginkgo biloba)
• The fresh or dried leaves, and the seeds
• Flavonoids & Biflavonoides: quercetin, ginkgetin
• Trilactonic diterpenes: ginkgolides
• Trilactonic sesquiterpene: bilobalids
• Platelet-activating factor (PAF) receptor antagonist (Ginkgolide B)
• Inhibition of PAF-induced platelet aggregation, inflammation, extravasation, bconchoconstriction
and airway hyperactivity and T-lymphocyte proliferation and cytokine production
• The antioxidant (free radical scavenging), membrane-stabilizing & increase CBF
• Ischemic Dementia
Ginkgo (Ginkgo biloba)
• Indications:
• Dementia & Symptomatic relief of organic brain dysfunction
• Peripheral Occlusive Arterial Disease (Intermittent claudication)
• Vascular Vestibular Disorders (vertigo, tinnitus)
• ADVERSE REACTIONS:
• Subarachnoid hemorrhage and an increase in bleeding time
Ginkgo (Ginkgo biloba)
• Anticoagulants, Antiplatelet Agents, Low Molecular Weight Heparins, and Thrombolytic
Agents/NSAIDs
• Increased risk of bleeding
• Buspirone & SSRI
• Precipitation of hypomanic episodes (serotonin syndrome)
• Insulin
• Ginkgo increase insulin levels
• Monoamine Oxidase Inhibitors (MAOIs)
• Potentiation effect (Ginkgo may inhibit monoamine oxidase)
• Anticonvulsants
• ↓ efficacy (lowering seizure threshold)
• CYP2B 1/2, CYP3A1, and CYP3A2 induction by ginkgo
Ginseng (Panax ginseng)
• The dried root
• Triterpene saponins (25 ginsenosides)
• Improve performance, stamina, cognitive function,
Cerebrovascular deficits
• Used also for loss of appetite, cachexia, anxiety, impotence, neuralgia
and insomnia
• Increase plasma ACTH and corticosteroids
• Stimulate insulin release and increase insulin receptors
Ginseng (Panax ginseng)
• Adverse reactions:
• Insomnia, headache, nervousness
• Hypertension
• Mastalgia
• Pregnancy/Lactation:
• Maternal use of Ginseng has been associated with neonatal
androgenization, thus it is not recommended for use during
pregnancy or lactation
Ginseng (Panax ginseng)
• Drug interactions:
• Anticoagulants (Warfarin, Antiplatelet Agents)/NSAIDS: Increased risk of
bleeding
• Antidiabetic agents/Insulin: Additive hypoglycemic effects
• Estrogens: ↑ estrogenic symptoms such as mastalgia & breakthrough
menstrual bleeding
• Monoamine Oxidase Inhibitors (MAOIs): Manic-type symptoms
(insomnia, tremor, headache, agitation)
• Daily dosage: 1-2 g of root
Siberian ginseng (Eleutherococcus senticosus)
• Dried roots and/or rhizome
• Caffeic acid derivatives
• Hydroxycoumarins
• Triterpene saponins (eleutherosides)
• Immune-stimulating/immune-modulating & antiviral effect
• Hypoglycemic & platelet aggregation-inhibiting effects
• Indications: Lack of stamina, Tendency to infection, tonic
• Daily dosage: 2-3 g of root
Lavender (Lavandula angustifolia)
• The essential oil extracted from the fresh flowers
• Volatile oil: linalool, linalyl acetate
• Hydroxycoumarins: umbelliferone
• Caffeic acid derivatives: rosmaric acid
• Nervousness and insomnia, migraine prophylaxis, Loss
of appetite
Lemon Balm (Melissa officinalis)
• The oil, the dried leaves, the fresh leaves and the whole
plant
• Volatile oil: geranial, linalool, geraniol, eugenol
• Flavonoids & Caffeic acid derivatives: rosmaric acid
• Triterpene acids: ursolic acid
• Nervousness & insomnia
• Daily Dosage: 1.5-4.5 g
‫بادرنجبویه‬
Sweet Orange (Citrus sinensis)
• The fresh and dried fruit peel and the extracted
essential oil
• Volatile oil: Jimonene, citronellal, linalyl acetate
• Flavonoids: naringin, tangeretin
• Nervous tension & sleeplessness, Loss of appetite
Bitter Orange (Citrus aurantium)
• The fresh and dried fruit peel, the flowers, the seeds and
the extracted essential oil
• Volatile oil: linalool, linalyl acetate, limonene
• Limonoids (triterpenoide bitter principles)
• Flavonoids: naringin, tangeretin
• Nervous tension & sleeplessness, Loss of appetite
‫نارنج‬
Passion Flower (Passiflora incarnata)
• The whole dried herb and the fresh aerial parts
• Flavonoids
• Cyanogenic glycosides: gynocardine
• Nervousness and insomnia, depressive states
‫گل ساعت‬
Saffron (Crocus sativus)
• The stigma and style
• Carotinoids: crocins & crocetin
• Picrocrocin
• Volatile oil: safranal (4,5-dehydro-betacyclocitral)
• Antidepressant, anti-anxiety, anti-convulsant
• Daily Dosage: 2 to 4 g drug
St. John's Wort (Hypericum perforatum)
• The entire flowering plant, flowers and aerial parts
• Hypericins (Anthracene derivatives): hypericin, pseudohypericin,
hyperforin
• Flavonoids: hyperoside, quercitrin, rutin
• Xanthones: 1,3,6,7-tetrahydroxyxanthone
• Mild antidepressant, sedative and anxiolytic action
• MAO inhibitory activity: hypericin
• 5-HT, NE & DA re-uptake inhibition: hyperforin
• down-regulation of cortical beta-adrenoceptors and 5HT-2 receptors
‫ هوفاریقون‬،‫علـــف چای‬
St. John's Wort (Hypericum perforatum)
• Side Effects:
• CNS: Restlessness & headache
• GIT: Anorexia, nausea, gastrointestinal pain, dry mouth, Constipation
• Dermatologic: Photosensitization (Hypericism, the hypericum pigments)
• Dosage: 2-4 g (dried herb) or 300 mg (the standardized extract) 3 times
daily
• Drug interactions:
• MAOIs: Hypertensive crisis
• SSRIs: serotonin syndrome
• Induce CYP 450: ↓ bioavailability of cyclosporine, Indinavir, OCP
‫ هوفاریقون‬،‫علـــف چای‬
Valerian (Valeriana officinalis)
• The dried roots
• Alkaloids: Valerine, Valerianine, Valtrate
• Iridoids: valepotriates
• Sesquiterpenes: valerenic acid
• Volatile oil: valerenal, Valerenol, isoeugenyl valerenate, (-)-bornyl
isovalerenate
• Nervousness & insomnia
• Centrally depressive, sedative, anxiolytic, spasmolytic & muscle relaxing
‫سنبل الطیب طبي‬
Valerian (Valeriana officinalis)
• ↑ GABA
• ↓ GABA degradation
• GABA Re-uptake inhibition
• ↑ GABA synthesis & release (glutamine)
• Daily Dosage: 100-3800 mg
‫نبل الطیب طبي‬
Thank you
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