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45 Cards in this Set
- Front
- Back
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What does xanthine do? (4)
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- block adenosine receptors
- inhibit phosphodiesterase, enhance cAMP - induce diuresis - translocate Ca2+ at high doses |
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Effects of xanthine: diuresis.
How does xanthine induce diuresis? |
- increase GFR
- inhibit Na+ reabsorption |
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Name two xanthine derivatives.
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- theophylline: may produce convulsion
- throbromine: weak stimulant |
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How does xanthine increase skeletal muscle activity?
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translocate Ca2+ at high doses
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Compare caffeine, theophylline, theobromine in their stimulatory effect.
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- caffeine: increase alertness and concentration.
- theophylline: may produce convulsions. - theobromine: weak stimulant |
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What does theophylline do at high doses?
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- translocate Ca2+
- produce restless, insomnia, tremor and convulsions. |
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What stimulant causes restlessness, insomnia, tremor and convulsions?
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high dose theophylline
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Where is xanthine metabolized?
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liver, some are excreted through kidney.
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What is theophylline useful for?
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- asthma prophylaxis
* can be used in conjunction with beta2 agonist, but need to monitor cardia arrhythmias. |
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Half lives of theophylline in children, adults, heavy smokers.
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children: 3.5 hr
adults: 8-9 hr heavy smoker: 4-4.5 hr (halved) |
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Caffeine adjunct with ___ is a treatment of migraine attacks.
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ergotamine
caffeiene: - enhance effects of ergotamine - enhance absorption of ergotamine |
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How does caffeine treat migraines?
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constriction of cerebral vasculature, release edema and pressure on nerve endings and meninges.
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List some OTCs that contain caffeine. (4)
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- stay awake pills
- diet pills - aspirin preparations - some herbals (kola nut, guarana) |
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Does xanthine treat ADHD?
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No.
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Mechanism of amphtamine.
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release newly synthesized monoamines in the order of NE>DA>5HT
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What is the order of monoamine release by amphetamine?
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NE>DA>5HT
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Effect of amphetamine at low dose.
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release NE
- increase alertness, activity - decrease apetite - increase BP * tolerance |
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Effect of amphetamine at high dose.
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- convulsions
- coma - death |
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Sympathetomimetics that are anorectics.
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- amphetamine (limited use)
- phenylpropanolamine - phen-fen - sibutramine - herbs: mahuang, st. John's wart - methylphenidate |
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Anorectics: phenylpropanolamine.
mechanism. |
suppress appetite so decreases the initiation of eating.
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which drug suppress appetite to decreases the initiation of eating?
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phenylpropanolamine
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Mechanism of drugs that enhance satiety.
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stimulation of 5-HT2C
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Phen-fen is a combination of ___ and ____.
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phenteramine(NE) and fenfulramine(5HT)
* off market because of heart valve damage. |
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mechanism of sibutramine.
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block reuptake of NE and 5-HT.
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How does ma huang work as a anorectic?
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contain ephedrine that release both NE and E.
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How does St. John's wart work as a anorectic?
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block reuptake of NE, DA, and 5-HT.
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Ephedrine is useful for ____ through release of ____. But it is banned because of ___.
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Ephedrine is useful for nasal congetion through release of catecholamines.
Banned because of worse adverse effect: cardiac arrythmia and elevated HR. |
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List some sympathetomimetics that treat narcolepsy.
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- amphetamine
- modafinil - GHB (gamma hydroxy-butyrate) - methylphenidate |
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Orexin (hypocretin) deficiency is the cause of ___.
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narcolepsy
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What is necessary at roughly 6 month intervals to maintain efficacy of amphetamines to treat narcolepsy?
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drug free holidays: because there is no tolerance.
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mechanism of modafinil.
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- reduce GABA release/ altering DA transporter
- increase release of DA and glutamate |
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side effects of modafinil.
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- anxiety
- insomnia - metabolic interactions less common: - ataxia - confusion - emotional instability |
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What is the drug that is used in healthy soldiers to keep them awake without decrement in mental function?
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modafinil
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This drug produces rebound insomnia 4 hours later to alleviate daytime sleepiness when taken at bedtime.
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GHB
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Which drug can treat obesity, narcolepsy, and ADHD?
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methylphenidate
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mechanism of methylphenidate.
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preferential release of NE and DA.
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What is the treatment choice of ADHD?
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methylphenidate or
Adderal (amphetamine and d-amphetamine in different salts) |
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What are some drug choices for ADHD?
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- methylphenidate
- Adderal (amphetamine and d-amphetamine in different salts) - Atomoxetine (Strattera): NE transporter inhibitor. |
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Side effects of methylphenidate.
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- weight loss
- increase HR - increase BP |
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How long does it take for methylphenidate or amphetamine to reach max therapeutic effect?
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2-3 wks
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side effects of amphetamine.
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- weight loss
- heart rate increase - BP increase worse than methlphenidate |
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Which is a better choice of treatment for school age children with ADHD?
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amphetamine salt mixture
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Side effects of atomoxetine.
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- abdominal cramps
- anorexia - increase heart rate - increase BP - constipation - fatigue |
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mechanism of atomoxetine.
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NE transporter inhibitor
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What is the effect of cocaine on NT?
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block the reuptake of NE, DA, and 5-HT.
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