Exam 7: CNS Stimulants

Question 1

Name the three amphetamine classes?

Answer 1

DL-amphetamine, Dextroamphetamine, methamphetamine

Question 2

What are the pharmacological effects of amphetamines?

Answer 2

release monoamines, primarily NE and DA, from nerve terminals in the brain

Question 3

What are the mechanismms of amphetamines that increase NE and DA?

Answer 3

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

Question 4

What are the main central effects of amphetamine-like drugs?

Answer 4

locomotor stimulation, euphoria and excitement, insomnia, increased stamina, anorexia, adverse effects of amphetamines include feelings of anxiety, irritability and restlessness

Question 5

What feelings follow after the stimulant effect wears off from amphetamines?

Answer 5

depression and anxiety

Question 6

What can occur with prolonged use of amphetamines? describe

Answer 6

amphetamine psychosis; resembles acute schizophrenic attack (hallucinations, paranoia, aggressive behavior)

Question 7

What occurs after the prolonged use of amphetamines is stopped after a few days?

Answer 7

period of deep sleep, upon awaking subject is lethargic, depressed, anxious and hungry

Question 8

What transporters are inhibited by methylphenidate (ritalin)

Answer 8

NET and DAT. [SERT a little bit]

Question 9

Does methylphenidate facilitate NE or DA release? AKA enter into the neuron?

Answer 9

No; blocks NET and DAT reuptake processes

Question 10

What does modafinil do?

Answer 10

increase extracellular DA levels in striatum and nucleus accumbens

Question 11

What diseases do we treat with modafinil?

Answer 11

narcolepsy, shift work, ADHD

Question 12

T/F: MDMA (ecstasy) is a stimulant and mild hallucinogenic?

Answer 12

true

Question 13

What are the pharmacoligical effects of MDMA?

Answer 13

inhibits monoamine transporters, mostly 5-HT transporter, also releases 5HT

Question 14

What are the negative effects of MDMA?

Answer 14

sudden illness and death, acute hyperthermia (dmg to skeletal muscle and renal failure), excess water intake and retention, heart failure

Question 15

What are pharmacological effects of cocaine?

Answer 15

binds to and inhibits the transporters of NET, DAT, SERT

Question 16

what are the sympathomimetic actions?

Answer 16

tachycardia, vasoconstriction, increase in blood pressure, increase in body temp

Question 17

What do the euphoric effects of cocaine involve?

Answer 17

inhibition DA and 5-HT reuptake

Question 18

What are adverse effects of cocaine?

Answer 18

toxic effects common in cocaine abusers, serious cardiovascular events, dependence, in utero impact during pregnancies

Question 19

what are major pharmacological actions of methylxanthines?

Answer 19

CNS stimulation, diuresis, stimulation of cardiac muscle, relaxation of smooth muscle

Question 20

What do methylxanthines resemble with their effects on cardiac and smooth muscle?

Answer 20

Beta-adrenoceptor stimulation

Question 21

What are the intracellular effects of methylxanthines (caffeine and theophylline)?

Answer 21

block PDE, increase intracellular cAMP –> effects that mimic those of mediators that stimulate adenylyl cyclase

Question 22

What type of adenosine receptors do methylxanthine act on?

Answer 22

A1 and A2 adenosine receptors

Question 23

What are the clinical uses of methylxanthines?

Answer 23

aspirin in some preps, ergotamine, mildly agreeable sense of alertness, respiratory stimulants, theophylline is used as a bronchodilator