Exam 7: CNS Stimulants Flashcards
(23 cards)
Name the three amphetamine classes?
DL-amphetamine, Dextroamphetamine, methamphetamine
What are the pharmacological effects of amphetamines?
release monoamines, primarily NE and DA, from nerve terminals in the brain
What are the mechanismms of amphetamines that increase NE and DA?
1) competitive inhibition of DA and NE reuptake 2) enter sympathetic nerve ending and displace stored NE and DA (reverse NE transport) 3) inhibit MAO breakdown of DA and NE
What are the main central effects of amphetamine-like drugs?
locomotor stimulation, euphoria and excitement, insomnia, increased stamina, anorexia, adverse effects of amphetamines include feelings of anxiety, irritability and restlessness
What feelings follow after the stimulant effect wears off from amphetamines?
depression and anxiety
What can occur with prolonged use of amphetamines? describe
amphetamine psychosis; resembles acute schizophrenic attack (hallucinations, paranoia, aggressive behavior)
What occurs after the prolonged use of amphetamines is stopped after a few days?
period of deep sleep, upon awaking subject is lethargic, depressed, anxious and hungry
What transporters are inhibited by methylphenidate (ritalin)
NET and DAT. [SERT a little bit]
Does methylphenidate facilitate NE or DA release? AKA enter into the neuron?
No; blocks NET and DAT reuptake processes
What does modafinil do?
increase extracellular DA levels in striatum and nucleus accumbens
What diseases do we treat with modafinil?
narcolepsy, shift work, ADHD
T/F: MDMA (ecstasy) is a stimulant and mild hallucinogenic?
true
What are the pharmacoligical effects of MDMA?
inhibits monoamine transporters, mostly 5-HT transporter, also releases 5HT
What are the negative effects of MDMA?
sudden illness and death, acute hyperthermia (dmg to skeletal muscle and renal failure), excess water intake and retention, heart failure
What are pharmacological effects of cocaine?
binds to and inhibits the transporters of NET, DAT, SERT
what are the sympathomimetic actions?
tachycardia, vasoconstriction, increase in blood pressure, increase in body temp
What do the euphoric effects of cocaine involve?
inhibition DA and 5-HT reuptake
What are adverse effects of cocaine?
toxic effects common in cocaine abusers, serious cardiovascular events, dependence, in utero impact during pregnancies
what are major pharmacological actions of methylxanthines?
CNS stimulation, diuresis, stimulation of cardiac muscle, relaxation of smooth muscle
What do methylxanthines resemble with their effects on cardiac and smooth muscle?
Beta-adrenoceptor stimulation
What are the intracellular effects of methylxanthines (caffeine and theophylline)?
block PDE, increase intracellular cAMP –> effects that mimic those of mediators that stimulate adenylyl cyclase
What type of adenosine receptors do methylxanthine act on?
A1 and A2 adenosine receptors
What are the clinical uses of methylxanthines?
aspirin in some preps, ergotamine, mildly agreeable sense of alertness, respiratory stimulants, theophylline is used as a bronchodilator
