Drugs of Abuse

jmanderson's version from 2016-03-12 16:12



Question Answer
maladaptive or INAPPROPRIATE USE of a drug that leads to a negative effect on ones life or othersabuse
repeated seeking or WANTING to use a drug to obtain a positive reinforcement or avoid a negative reinforcementaddiction
………. are a strong psychological reinforcer for psychological dependence. (ex- smoking while you gamble)associated cues
patients NEEDING to use a drug based on the principles of tolerance and withdrawaldependence
Are all addictive drugs abused?nope (e.g., etOH)
Are all abused drugs addictive?nope (e.g., LSD)
the need to increase the dose of a drug to get the same result, different than dependencetolerance
drug causes changes in the body such that removal of the drug causes unwanted effects known as ……..withdrawal
vomiting, chills (goose bumps, “cold turkey”), and kicking movements are sx of …….withdrawal
All drugs that produce dependence and addiction increase ............ within the limbic system (esp. nucleus accumbens)!!!!dopamine (DA)!!!
Mesencephalic region that projects to the limbic system supplying the area with dopamine (mesolimbic system) – responsible for pleasure/rewardventral tegmental area (VTA)
Indirect action of drugs rely on ……… meaning to inhibit GABAergic neural transmission to indirectly increase DA releasedisinhibition
Rx for comatose patient with uncertain intoxications?NALOXONE 2 mg, THIAMINE 100 mg, GLUCOSE
Red eyes assoc with ...... toxicitycannabis
pinpoint pupils assoc with ...... toxicityopioids
Neurotransmitter - pleasure, euphoria, mood, motor function (the final activation chemical in all rewards)dopamine - D1 receptors
Neurotransmitter - mood, impulsivity, anxiety, sleep, cognitionserotonin (5HT) - 5HT3 receptors
Neurotransmitter - pain, appetite, memorycannabinoids - CB1, CB2 receptors
Neurotransmitter - painopioid peptiedes (endorphins, enkaphilins) - kapp, mu, delta receptors
Neurotransmitter - decrease anxiety, less panic, relaxationGABA - GABA-A and GABA-B receptors
What abused drug inhibit GABAergic neurons that project to dopaminergic neurons in the VTA?alcohol
What abused drug binds to opioid receptors that inhibit GABAergic neurons that project to dopaminergic neurons in the VTA?heroin (opioids)
What abused drug blocks the function of DAT (by binding to the DAT and slowing transport)?cocaine
What abused drug activates cholinergic neurons that project to dopaminergic neurons of the VTAnicotine
What schedule drug has "high potential for abuse, no currently accepted medical use in tx in the US, lack of accepted safety for use under medical supervision"schedule 1 drug
Benzodiazepine suffix and examples-PAM (most), ex - lunitrezepam, lorazepam, diazepam, clorazepate, alprazolam, triazolam, chordiazepoxide, clonazepam
Barbituates suffix and examples-BARBITAL, ex- phenobarbital, secobarbital, amobarbital

MOA and AE


Question Answer
cocaine addiction MOAInhibits reuptake of monamines by BLOCKING MONAMINE TRANSPORTERS
Most important monamine transporter blocked by cocaineDA transporters (secondarily, NE and 5HT transporters)
Rare OD effect of cocainehypertensive crisis (diastolic BP > 130 mmHg)
Amphetamine addiction MOAdirect action on VTA dopaminergic nerve terminals (REVERSE TRANSPORT and inhibition of neurotransmitter reuptake by monoamine transporters – inhibits vesicular monamine transporter)
MDMA has greater 5HT3 effect than DA effect (hallucinogen) and is a ………… neurotoxinSEROTENERGIC NEUROTOXIN
Methamphetamine is a greater psychostimulant and is a ……… and ….. neurotoxinDOPAMINERGIC and SEROTONERGIC neurotoxin
Number one cause of preventable deathtobacco smoke and nicotine
Ethanol addiction MOApositive allosteric modulator of GABA-A receptor (resulting in DA release)
Physiological withdrawal of etOH (Shaking, confusion, high blood pressure, fever, and hallucinations are some symptoms) is called …..Delerium Tremens
#1 cause of death from acute etOH abuseaspiration of vomit
etOH DI that causes hepatotoxicitydisulfiram
Benzodiazepines therapeutic MOApositive allosteric modulator of GABA-A receptors; increase FREQUENCY of channel opening (increase potency of GABA)
Barbiturates therapeutic MOApositive allosteric modulator of GABA-A receptors; increase DURATION of channel opening (increase efficacy of GABA), higher concentrations can act as direct GABA-A receptor agonist
Chronic Benzo and Barb AEsmaladaptive behaviors, abscess/infections from IV, death from OVERDOSE
Use of benzodiazepines and barbiturates with other ………………… greatly increases the risk of COMA and DEATHdepressants (such as opiates and ethanol)
Benzodiazepines acute AEssedation, ataxia and stupor. Coma, respiratory depression and DEATH RARE WHEN USED ALONE
Barbiturates acute AEsDEATH from respiratory depression, cardiovascular collapse, aspiration pneumonitis and aspiration pneumonia
What can enhance the elimination of phenobarbital but does NOT work for short-acting barbiturates (hepatically eliminated)?Urinary alkalinization

overdose treatments


Question Answer
Rx for comatose patient with uncertain intoxications?NALOXONE 2 mg, THIAMINE 100 mg, GLUCOSE
What can be used with cocaine OD to reduce anxiety, agitation, seizures, hypertension, tachyarrhythmias?IV lorazepam
Tx and order of tx for hypertensive crisis of cocaine ODphentolamine (Alpha-1-blocker) or labetalol IV (beta-blocker) => block A before B
What drug can tx MALIGNANT HYPERTHERMIA from MDMA overdose?DANTROLENE (Ryanodine receptor antagonist)
Chronic use of tobacco/nicotine AEDEATH (risk factor for chronic illness)
Tx of nicotine abuse?nicotine replacement therapy, BUPROPION (antidepressant), varenicline (partial nicotinic R agonist)
Buproprion for tobacco tx MOAinhibits reuptake of DA, NE, and 5HT in the CNS. Is a non-competitive nicotine receptor antagonist, and at high concentrations inhibits the firing of NE neurons in the locus coeruleus.
Bupropion for tobacco tx AEsdry mouth, nausea, HA, increase risk of SEIZURES
Rx to prevent Wernicke-Korsoakoff syndrome in etOH overdoseTHIAMINE
etOH addiction Rx (3)?naltrexone (blocks mu opioid receptor), acomprosate, disulfiram (deterrent)
When combined with etOH, this causes building up of acetaldehyde, leading to severe vomiting flushing of the skin, increased HR, SOB, N/V, throbbing headache, visual disturbance, mental confusion, postural syncope, and circulatory collapseDisulfiram
Benzodiazepine for etOH tx AEssedation and DRUG DEPENDENCY
Buprenorphine/naloxone (Suboxone®) and Methadone for opioid tx AEsConstipation, nausea, vomiting, sedation and DRUG DEPENDENCY
Heroin addiction txmethadone, buprenorphine (activates opioid receptors)
First line tx for opidoid overdose (mu-opioid receptor antagonists)naloxone
tx of opioid withdrawalclonidine (alpha-2 receptor agonist)
tx of opioid abuseBuprenorphine/naloxone (Suboxone®) and Methadone

withdrawal, tolerance, addiction level


Question Answer
cocaine withdrawal severitymild
cocaine tolerance severityvariable
amphetamine withdrawal severityHIGH
amphetamine tolerance severityHIGH
tobacco withdrawal severitymild
tobacco tolerance severityHIGH
etOH withdrawal severityHIGH
etOH tolerance severityHIGH
opioids withdrawal severityHIGH
opioids tolerance severityHIGH
benzodiazepines withdrawal severityHIGH
benzodiazepines tolerance severityHIGH
What drug is very addictive and is most often abused concomitant with other drugs (esp. opioids)?benzodiazepines
Barbituates withdrawal severityHIGH
Barbituates tolerance severityHIGH
LSD withdrawal severityNONE
LSD tolerance severityyes (but rapid and short lived)
Does LSD increase dopamine in the nucleus accumbens?NO!
Is LSD addictive?NO
Are dissociative agents (e.g., ketamine and dextromethorphan) addictive?No
Do dissociative agents (e.g., ketamine and dextromethorphan) cause withdrawal and tolerance?no
Does Cannabis affect the nucleus accumbens?NO (there is no CB1 receptors in the NAc)
Cannabis withdrawal severityunknown
Cannabis tolerance severityREVERSE TOLERANCE (the more you smoke, the less you need)

route of administration


Question Answer
cocaine route of administrationchewing leaves, snorting/sniffing, IV, inhalation
amphetamines route of administrationoral, IV, smoked, snorted
tobacco route of administrationsmoked, inhaled, chewed
opioid route of administrationoral (prescriptioin), IV (parenteral prescription, crushing oral prescriptions, heroin)
Benzo and Barb route of administrationoral, IV (more addictive than PO)
decrease half life of benzo/barb does what to addiction potential?increases
LSD route of adminpaper tabs or drops on tongue
ketamine and dextromethorphan route of admincrystalline powder, liquid, capsule, pill (snorted, ingested, injected, smoked)
Cannibis route of adminsmoking, vaporizing, tea, edibles