Pharmacology of Psychostimulant Misuse Flashcards
Describe the current trends in stimulant overdose deaths
overdose deaths is continually trending upward
Describe the primary clinical effects of psychostimulants with escalating dose
as dose escalates so do the addiction and cognitive deficits
more negative effects
Ex:psychosis confusion coma and circulatory collapse
Discuss the effect of chronic psychostimulant use on the CNS dopaminergic system.
Downregulation of dopamine receptors
Similar changes occur with NE and 5-HT with antidepressant therapy
Receptor downregulation believed to mediate withdrawal symptoms
DA downregulation is not evidence of a broken brain
Recovery of DA receptors shows ability to return to homeostasis (abstinence)
Describe why pseudoephedrine is regulated to reduce methamphetamine abuse
Pseudoephedrine’s OH group can be reduced to Hydrogen to create methamphetamine. Phenylephrine has two OH groups
identify the primary manifestations of sympathomimetic toxidrome
MATHS
what do Psychostimulants do?
activate the CNS resulting inalertness, excitation, and elevated mood
Nicotine MOA
Nicotine activates acetylcholinergic receptor
Na enters cell K exits= action potential
heterogenetiy of subunits determines how many molecules of Ach bind to receptor
variation in receptor composition at different sites may influence physiological response
What are the similarities between nicotine and ACh
charged amino groups and hydrogen bond acceptor groups
T or F: nicotine is membrane penetrable at physiological pH (weak base)
T
T or F nicotine is degraded by acetylcholinesterase
False it is not degraded
what is Partial Agonist Therapy
causes release of dopamine
highly addictive
Nicotine replacement therapy relatively ineffective alone
varenicline partial agonist increases quit rate success (blocks receptors but still releases DA)
what are commonly abused psychostimulants
MDMA (ecstasy)
Methamphetamine (crystal meth)
Methylphenidate(ritalin)
Cocaine
NE
dopamine
Cocaine MOA
Antagonist of amine transporters
DAT>SERT>NERT
Prevents DA reuptake
Increases DA concentration
Increase duration of DA action
what is the MOA of Methamphetamine, Ecstasy and bath salts
they compete for reuptake
resemble endogenous DA,
block DA reuptake and push DA from vessicles increasing extra vesicular DA
reverse transport (gradient) amphetamines are MAOis
Activate trace amine-associated receptor phosphorylate DAT induces reverse transport function
What is catha edulis
mild euphoria excitement similar to strong coffee (ingredient from Khat)
What are common synthestic cathinones
bath salts,plant foods, molly,flakka,scarface
What is the common neurologic effect of methamphetamine abuse
delirium tremor
What is the common psych effect of methamphetamine abuse
Anxiety,paranoia,hallucinations,delusions, and repetitive behavior
What is the common ENT effect of methamphetamine abuse
profuse dental decay
What is the common skin effect of methamphetamine abuse
diaphoresis
Stimulants in the use of cognitive enhancement
there is increasing use of stimulants with the goal of cognitive enhancement but it is not well supported by research and can progress to stimulant use disorder
What does MATHS stand for
M: mydriasi
A: agitation, arrythmia and angina
T: tachycardia
H: HTN hyperthermia
S: seizure and sweating
T or F agitation HTN and seizures can be treated with alpha agonism
False can be treated with benzodiazepines
avoid pure BB due to unapposed alpha agonism
HTN responds to sedation
What does nicotine target in the VTA
DA and glutamate
