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active ingredient in st. john's wort
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Pharmacologic effects of hypericin
monoamine oxidase a and b inhibitor
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MAO-A deaminates
- serotonin
- melatonin
- epinephrine
- norepinephrine
- dopamine
-
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invitro studies of hydroalcoholic extract have shown
inhibition of serotonin, NE and DA reuptake
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Chronic administration of st. john's wort has shown ____ in mice
- down regulation of cortical adrenoreceptors
- up regulation of 5ht2 receptors
- reduction of interleukin 6 production
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a randomized trial comparing citalopram 20mg to st. john's wort 900mg showed
equivalence in reducing symptoms of moderate to severe depression over 6 weeks.
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Antiviral and anti-carcinogenic effects of SJW
hypericin is photolabile, when activated it inhibits enveloped and non-enveloped viruses as well as growth of some neoplastic tissues
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ADEs with st. johns wort
photosensitization
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Drug interactions with SJW
- antidepressants = additive effects
- may induce cyp450 => numerous interactions
- induction of p-glycoprotein drug transporter
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most common formulation of SJW
dried hydroaclcoholic extract
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onset of action with SJW
2-4 weeks
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Coenzyme Q10
potent antioxidant used for hypertension and prevention of statin-induced myopathy
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effects of coenzyme q10 on coronary artery disease and chronic stable angina
modest but appear promising
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ADEs with coenzyme q10
- rarely has any ADEs even at high doses
- GI upset/diarrhea/nausea/heartburn and anorexia in <1%.
- maculopapular rash and thrombocytopenia are rare
- irritability, dizziness, headache
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Drug interactions with CoQ10
structural similarity to vitamin K which decreases effectiveness of warfarin
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Glucosamine uses
pain associated with knee osteoarthritis
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Available forms of glucosamine
- sulfate and hydrochloride
- hydrochloride is ineffective
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Endogenous glucosamine is used for
production of glycosaminoglycans and other proteoglycans in cartilage
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Studies with glucosamine
have shown improvements in pt with osteoarthritis
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ADEs with glucosamine
- very well tolerated
- mild diarrhea and nausea
- may cause allergy in people with shellfish allergies
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Drug interactions with glucosamine
may increase the INR in patients taking warfarin resulting in increased risk of bruising or bleeding
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Results when taking glucosamine
- may take 1-2 months
- no direct analgesic effects
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Melatonin
- serotonin derivative produced by the pineal gland
- regulation of sleep wake cycle
- release coincides with darkness (9pm-4am)
- release is suppressed by daylight
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Other uses studied for melatonin
- contraception
- protection against oxidants
- prevention of aging
- treatment of depression
- HIV
- cancer
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Current uses of melatonin
prevention of jet lag and induction of sleep
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sleep maintenance insomnia
- pt older than 65 who have low melatonin levels
- treatable with melatonin sustained release
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Melatonin receptors have been identified in
- granulosa cell membranes in the female reproductive tract
- associated with midcycle suppression of LH
- may result in partial inhibition of ovulation
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melatonin may be used with _____ days 1-21 of the menstrual cycle to lower LH levels
progestin
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melatonin in men
- decreased sperm quality
- possibly due to aromatase inhibition
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ADEs with melatonin
- next day drowsiness
- changes in BP
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Drug interactions with melatonin
- concentrations of melatonin are altered with NSAIDs, antidepressants, adrenoreceptor agonists/antagonists, scopolamine and sodium valproate
- increases effects of nifedipine
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Melatonin is metabolized by ____ and may interact with ____.
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Melatonin for jet lag
- take on the evening of departure and for 1-3 nights after arrival in new time zone
- exposure to daylight is also important
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