Pharmacology of Psychostimulants Flashcards
- Define psychostimulant.
Induce improved mental or physical performance or both via: mood elevation, locomotor stimulation, alertness, increased ability to concentrate, decreased appetite and decreased fatigue
- Describe the mechanism of action and clinical uses of psychostimulant drugs
Psychostimulants inhibit uptake via monoamine transporters, evoke transporter-mediated monoamine release or both
Therapeutic uses include: ADHD, narcolepsy, prevent and reverse fatigue, appetite suppression
- Describe how cocaine and amphetamine differ in their effects at the monoamine uptake transporters.
Cocaine only blocks reuptake, it does not encourage increased release of NT whereas amphetamine can cause both
- Describe the similarities and differences in the pharmacology and effects of atomoxetine and amphetamine.
Atomoxetine is not a stimulate drug like amphetamine, it does not significantly effect DA
- Describe the pharmacology of modafinil and how it differs from other psychostimulants.
Modafinil does not effect other receptors besides DAT and NET and does not inhibit MAO-B
- Recognize the cathinone chemical structure and state medical and nonmedical uses of these drugs.
commonly as drugs of abuse, similar drugs have a B-keto amphetamine structure
Discuss the use, mechanism, pharmacology, adverse effects and precautions of Amphetamine.
prototype stimulant, of the most potent, first line ADHD tx.
indirect acting sympathomimetic, inhibits NE, DA and 5-HT uptake transporters, evokes MA release
immediate or extended release forms, metabolized by CYPs and MAO, excreted in urine
increased sympathetic tone: CNS, CV, has some reinforcement properties
contraindications: severe anxiety, tension, psychosis, anorexia, CAD, HTN and with MAOI, hyperthyroidism or glaucoma
Discuss the use, mechanism, pharmacology, adverse effects and precautions of Methylphenidate.
tx. for ADHD or narcolepsy
more DA uptake blockade than catecholamine releasing activity
metabolism in liver, metabolites mostly in urine
less motor stimulation than amphetamine and minimal peripheral effects, less reinforcing
contraindications same as amphetamines except no troubles with hyperthyroidism
Discuss the use, mechanism, pharmacology, adverse effects and precautions of Modafinil.
non-amphetamine stimulant, promotes wakefulness for narcolepsy, shift related sleep disorder and OSA (may be useful for cocaine dependance)
unclear mechanism binds to DAT and NET to inhibit DA and NE uptake, increases extracellular glutamate and has week or negligible interactions at NE, 5-HT, DA, GABA, adenosine, histamine and melatonin receptors, does not inhibit MAO-B activity
metabolism mainly by CYP3A4, renal elimination, significant half-life
adverse effects: headaches, restlessness, euphoria, altered moods, ND, increased HR and BP, not as reinforcing as amphetamines
NOT FOR CHILDREN, do not use with MAOI, may inhibit CYP2C9 and CYPC19
Discuss the use, mechanism, pharmacology, adverse effects and precautions of Atomoxetine.
non-stimulant drug for ADHD (variable response
NRI, no appreciable 5-HT or DA transporter affinity for other receptors
side effects diminish with continued dosing, extensive hepatic metabolism
mininamal peripheral effects, BBW for suicidal ideation, CNS, CV, GI and UG effects
caution with hepatic disease, narrow angle glaucoma, MAOI, cerebrovascular disease
Discuss the use, mechanism, pharmacology, adverse effects and precautions of Cathinones.
bathsalts- mostly drugs of abuse
Monoamine alkaloid found in Catha leaf, cathinone stops reuptake but does not increase release of DA
B-keto amphetamine structure, 10x potent than cocaine
locomotor and stereotypical behavior, not officially scheduled by controlled substance
