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4.4 CNS stimulants
By Dr. Winsauer
39
Pharmacology
Professional
04/04/2012

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Cards

Term
What is NE made from?
Definition
tyrosine (tyrosine hydroxylase)--> DOPA --> DA --> NE
Term
All "psychomotor" stimulants are ____.
Definition
indirect acting sympathomimetics
Term
What is the MOA of cocaine versus amphetamines?
Definition
cocaine prevents reputake, amphetamines enhance release
Term
What drugs can abolish the effects of CNS stimulants that release catecholamines?
Definition
reserpine= prevents monamine transport to allow DA into vesicles
guanethidine= blocks reputake 1
Term
Peripheral effects of sympathomimetics are due to ___________, central effects due to ___________.
Definition
increase NE peripherally; increased DA centrally
Term
Name some CNS stimulants that work by releasing catecholamines.
Definition
amphetamine, methamphetamine, dextroamphetamine, ephedrine, pseudoephedrine, methylphenidate, pemoline
Term
What is the difference between ephedrine and pseudoephedrine?
Definition
pseudoephedrine is also a stereoisomer of ephedrine
Term
Besides being as CNS stimulant by causing the release of catecholamines, ephedrine also...
Definition
is an alpha and beta agonist
Term
What is methylphenidate used to treat?
Definition
ADD
Term
What are the unique characteristics of pemoline?
Definition
long acting; caution due to hepatic complications/failure
Term
Name some CNS stimulants that block the reuptake of catecholamines (NE and DA) and serotonin.
Definition
cocaine, mazindol, sibutramine, modafinil
Term
What is notable about sibutramine?
Definition
a CNS stimulant that blocks the reuptake of catecohlamines and serotonin and has two active metabolites with relatively long half lives
Term
What are the advantages to using modafinil?
Definition
no abuse liability (not self administered by rats), possibly be used to treat stimulant withrawal; used by military
Term
What is the MOA of bupropion?
Definition
blocks reuptake of DA and EPI
Term
If child can not tolerate first line ADD meds, use...
Definition
atomoxetine
Term
What is Atomoxetine?
Definition
a relatively selective NE reuptake inhibitor which is marketed as the first non-stimulant for ADHD
Term
What is the MOA of methylxanthines?
Definition
adenosine receptor antagonists= relaxes vasculature and smooth muscle
Term
Name a short and a long acting methylxanthine.
Definition
short acting= caffeine
long acting= theophylline
Term
What are teh symptoms of methylxanthine withdrawal?
Definition
headaches d/t hypotension
Term
T/F CNS stimulant withdrawal can cause death.
Definition
false
Term
What is theophylline?
Definition
long-acting methylxanthine found in tea and perscribed for nighttime asthma
Term
Drugs that ________________ could also be considered indirect acting adrenergic agonist but they are not traditionally considered to be stimulants.
Definition
MOA and COMT inhibitors
Term
Name a COMT inhibitor.
Definition
entacapone
Term
What is a complication associated witih entacapone administration?
Definition
hepatotoxicity
Term
What are the effects of CNS stimulants?
Definition
cardiovascular responses, CNS, respiratory, dental, anti-SLUDE
Term
What are the cardiovascular effects of CNS stimulants?
Definition
can raise both systolic and diastolic pressure (amphetamine) Hr rate can also be reflexively slowed; with large doses, cardiac arrythmias may occur
Term
What are the effects of CNS stimulants on the CNS?
Definition
main effect includes wakefulness, alertness, decreased sense of fatigue, elevation of mood, increased capacity to concentrate, elation, euphoria and increased motor and speech activities. Many individuals though experience headache, palpitation, dizziness, agitation, confusion and delirium with high doses producing psychotic symptoms
Term
What are the respiratory effects of CNS stimulants?
Definition
have a direct effect on the medullary respiratory center and increase both the depth and rate of respiration. In normal individuals however, therapeutic doses do not increase respiratory rate or minute volume
Term
What causes the dental problems associated with amphetamines abuse?
Definition
vasoconstriction + no salivation
Term
Tolerance almost invariably develops what effects of stimulants?
Definition
anorexigenic effects and mood enhancing effects
Term
Chronic administration with CNS stimulants results in ____.
Definition
extensive psychological dependence but not physical tolerance
Term
T/F It is important to treat symptoms of withdrawal from CNS stimulants.
Definition
false
Term
What are the symptoms of withdrawal from CNS stimulants?
Definition
dysphoria, depression, sleepiness, fatigue, bradycardia and craving
Term
What are the therapeutic uses of CNS stimulants?
Definition
obesity, ADD, narcolepsy
Term
What is differential tolerance?
Definition
tolerance to some but not all effects of a drug
Term
T/F Amphetamine-like drugs have been shown to be more effective than placebo in promoting weight loss in short-term, double-blind controlled studies.
Definition
true
Term
What percent of school-aged kids have ADD/
Definition
12%
Term
How do CNS stimulants treat narcolepsy?
Definition
probably a specific effect on the reticular activating system in the brain
Term
What are the contraindications of CNS stimulants?
Definition
anorexia, insomnia, asthenia, psychopathic personality, or a history of homicidal or suicidal tendencies
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