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39 Cards in this Set
- Front
- Back
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What are the prototype stimulants?
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Caffeine
Modafinil Amphetamines Cocaine Nicotine |
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What are the clinical indication for stimulant use?
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Headache
Fatigue Narcolepsy ADHD Obesity |
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What methylxanthines has greatest amount of CNS stimulant properties?
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Caffeine
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What are the therapeutic uses for caffeine?
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Fatigue and restore alertness
Headaches |
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What is the mechanism of caffeine action?
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1. Adenosine A1 and A2 receptor blocker. Adenosine can inhibit neuronal activity.
2. PDE inhibitor 3. glycine receptor blocker |
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What is caffeine withdrawal syndrome?
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Headache
Fatigue Difficulty with concentration Irritability |
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Describe caffeine overdose and treatment.
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> 1 gram = mild delirium, alternating states of consciousness and arrhythmias
>5 grams = seizures Treat with diazepam and support |
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What are the therapeutic uses for modafinil?
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Narcolepsy
Shift workers Fatigue in pts with OSA |
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What is the purposed action of modafinil?
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effects of DM reuptake
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What are the pronounced symptoms of modafinil overdose and how is it treated?
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CV effects
Treated with support |
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What are the methylphenidates used for?
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ADHD
Narcolepsy |
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Where is modafinil metabolized? How does it effect its own metabolism?
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In the liver, thought to induce its own metabolism
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Why could withdrawal of methylphenidates cause severe depression?
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Chronic use can have psychic dependence and psychotic episodes
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What are the therapeutic uses of amphetamines?
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ADHD
Narcolepsy formerly obesity |
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What it the difference between dextoamphetamine and amphetamine?
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d-isomer only. More selective for CNS
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What is lisdexamphetamine?
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extended formulation of dextroamphetamine
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Why was amphetamine discontinued for obesity treatment?
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Tolerance and high abuse potential
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What is the mechanism of action for amphetamines?
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Indirect sympathomimetic: release of NE from synaptic vesicles and at higher doses increases DM release
Blocks neuronal amine reuptake |
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How can renal excretion of amphetamines be enhanced?
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Acidify urine (Vitamin C)
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Amphetamine and MAOI should not be used in combination. Why?
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Can cause hypertensive crisis
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What non-stimulant is used to treat ADHD?
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Atomoxetine
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What is the mechanism of action for atomoxetine?
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NE reuptake inhibitor
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Why should atomoxetine be used with caution in pediatric pts?
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Increases suicidal ideation
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What stimulants are currently used in the management of obesity? What are the mechanisms?
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Sibutramine: NE, 5HT, DM reuptake inhibitor
Phentermine: NE, DM release Diethylpropion: NE release Mazindol: NE reuptake inhibitor |
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What is the mechanism of action for sibutramine?
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NE, 5HT, and DM reuptake inhibitor
Suppresses appetite Thermogenic |
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Where is sibutramine metabolized?
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In the liver into two active metabolites
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What drug classes are contraindicated with sibutramine?
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MAOI
SSRI TCA anything that is serotonergic, such as ergots and triptans too. |
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What is phenylephrine used for?
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nasal decongestant
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What is the mechanism of cocaine?
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DM, 5HT, NE reuptake inhibitor
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What is the difference between cocaine and amphetamine tolerance?
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Tolerance does not develop to euphoria
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How is cocaine OD treated?
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Diazepam
Nitroglycerin Calcium channel blocker |
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What is the mechanism of nicotine?
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agonist for nAChR perdominantly on presynaptic neurons. Causes release of DM, opioids, and others.
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What causes nicotine dependence?
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central DM release
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What is bupropion?
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an atypical antidepressant and smoking cessation aid. It acts as a norepinephrine and dopamine reuptake inhibitor (NDRI), as well as α3β4-nicotinic receptor antagonist.
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Bupropion is contraindicated for what pts?
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Psychotics
Epileptics Pts with eating disorders |
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What is the most effect smoking cessation drug?
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Varenicline
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What is mechanism for varenicline?
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partial nicotinic receptor agonist increasing mesolimbic DM levels to stop cravings
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What is the presentation with large nicotine overdose?
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Prostration
Hypotension Respiratory failure Convulsions |
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How is nicotine overdose treated?
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Support and diazepam
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