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USMLE - Pharm

Kaplan Section 4 Chapter 1 CNS Pharm - Drugs of Abuse

QuestionAnswer
Name 2 drugs of abuse that are CNS stimulants Cocaine, Amphetamines
What is the mechanism of cocaine? In CNS, blocks reuptake of DA, NE, and 5HT; local anesthetic action from Na+ channel blockade
What is the mechanism of amphetamines? 1. block the reuptake of DA and NE; 2. releases DA and NE from mobile pool --> more available; 3. weak MAO inhibitors --> less DA and NE inactivation --> more DA and NE available.
What is the effect of increased NE action when abusing CNS stimulants? 1. inc HR and contractility, 2. BP changes, 3. mydriasis, 4. central excitation, 5. hyperactivity
What is the toxicity of excess NE? 1. cardiac arrhythmias, 2. generalized ischmia with possible MI and strokes, 3. acute renal and hepatic failures
What is the effect of increased DA action when abusing CNS stimulants? 1. psychotic episodes, 2. paranoia, 3. hallucinations, 4. possible dyskinesias, 5. endocrine disturbances
What is the toxicity of excess DA? 1. Major psychosis, 2. cocaine delirium
What is the effect of increased 5HT action when abusing CNS stimulants? 1. behavioral changes, 2. aggressiveness, 3. dyskinesias, 4. dec appetite
What is the toxicity of excess 5HT? 1. possible serotonin syndrome
What is the toxicity of excess NE, DA, and 5HT? 1. convulsion, 2. hyperpyrexia (excessive and unusual elevation of set body temperature greater than or equal to 41.1° Celsius (106°F) -- diff from hyperthermia, in which body's temp is way above nl set point), 3. death
What are the sx's of withdrawal from CNS stimulants? 1. craving, 2. severe depression, 3. anhedonia (inability to experience joy), 4. anxiety
How would you manage withdrawal sx's from CNS stimulants? Give anti-depressants
Name 3 groups of CNS depressants that people can abuse 1. BZ's, 2. barbiturates, 3. EtOH
What is the mechanism of BZ's? potentiates GABA binding to GABAa receptors at the BZ1 and BZ2 sites
What is the mechanism of barbiturates? prolongation of GABA (imitates GABA at high doses) action on GABAa receptors
What is the mechanism of EtOH? prolongation of GABA (imitates GABA at high doses) action on GABAa receptors
What is the effect of BZ's? light-to-moderate CNS depression
What is the toxicity of BZ's? sedation and anterograde amnesia (can't remember things after the insult/injury)
How do you treat BZ overdose? Reverse with flumazenil
What are the withdrawal sx's of BZ's? 1. rebound insomnia, 2. rebound anxiety
What is the effect of barbiturates? CNS depression
What is the toxicity of barbiturates? 1. severe CNS depression, 2. respiratory depression, 3. death
What is the effect of EtOH? CNS depression
What is the toxicity of EtOH? 1. severe CNS depression, 2. respiratory depression, 3. death
What are the withdrawal sx's of barbiturates? 1. agitation, 2. anxiety, 3. hyperreflexia, 4. life-threatening seizures
What are the withdrawal sx's of EtOH? 1. agitation, 2. anxiety, 3. hyperreflexia, 4. life-threatening seizures, 5. delirium tremens (delusions/hallucinations, associated with tactile hallucinations such as sensations of something crawling on subject - phenomenon known as formication)
What do morphine, heroin, methadone, and fentanyl have in common? all are opioids
What is the mechanism of opioids? 1. activate opioid receptors (mu, kappa, delta)
For opioids, the involvement of which receptor has the most intense abuse and dependence liability? mu -- inc in DA transmission in the mesolimbic tracts
What is the effect of opioids? 1. euphoria, 2. analgesia, 3. sedation, 4. cough suppression, 5. constipation, 6. strong miosis (not with meperidine)
What are the sx's of opioid toxicity? 1. severe respiratory depression, 2. nausea, 3. vomiting
How do you treat respiratory depression caused by opioid toxicity? give naloxone (a μ-opioid receptor competitive antagonist)
What type of drug is marijuana? hallucinogen
What is the mechanism of marijuana? Marijuana stimulates the dopamine pathway from the ventral tegmental area to the nucleus accumbens. Binds to cannabinoid receptors CB1 (CNS) and CB2 (periphery).
What is THC? THC is the primary psychoactive component in marijuana.
How is THC metabolized in the body? CYP450 system
What is the effect of marijuana? 1. sedation, 2. euphoria, 3. inc HR, 4. conjunctival hyperemia (engorgement of the conjunctival vessels), 5. delusions, 6. hallucinations
What is the toxicity of marijuana? Smoking --> possible flashbacks
What are the sx's of marijuana withdrawal? irritability and anxiety
What is the mechanism of action of hallucinogens? interaction with 5HT receptors
What is the effect of hallucinogens? 1. hallucinations, 2. sympathomimetic, 3. dysesthesias (tactile hallucinations)
What is the toxicity of hallucinogens? flashbacks likely
What is the toxicity of PCP? 1. horizontal and vertical nystagmus, 2. paranoia, 3. rhabdomyolysis
What is the danger of PCP? extremely toxic, OD is common, with convulsions and death
What is the toxicity of Ketamine? more mild than PCP: 1. horizontal and vertical nystagmus, 2. paranoia, 3. rhabdomyolysis PLUS 4. hallucinations
What is the effect of ecstasy? (MDMA, MDA, MDEA) amphetamine-like (stimulant) with strong 5HT activation --> hallucinogenic; neurotoxic
Created by: Missy Kratz Missy Kratz on 2008-03-17



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