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Flashcards in Drugs of Abuse Deck (21):
1

depressant that enhances GABA binding to GABAa receptor and inhibits glutamate binding to NMDA receptor, and facilitates release of endogenous opioids in VTA

acute effect: CNS depression
toxicity: potentially life-threatening respiratory depression
mild withdrawal: sympathetically driven tremors, tachycardia, hypertension, sweating
severe withdrawal: potential life-threatening seizures due to down-regulation of GABAa receptors and upregulation of NMDA receptors

profound addiction and physiological dependence

ethanol

2

depressants that enhance GABA binding to GABAa receptor

acute effect: CNS depression
toxicity: potentially life-threatening respiratory depression when used in combination with other depressants

moderate use withdrawal includes anxiety, paresthesia, sleep disturbance
severe withdrawal: potential life-threatening seizures due to down-regulation of GABAa receptors

profound addiction and physiological dependence

benzodiazepines

3

depressants that enhance GABA binding and directly activate GABAa receptors

toxicity: potentially life-threatening respiratory depression when used in combination with other depressants

severe withdrawal: potential life-threatening seizures due to down-regulation of GABAa receptors

profound addiction and physiological dependence

barbiturates

4

activation of mu opioid receptors in medullary respiratory center, spinal/supraspinal sites mediating analgesia, enteric nerves, and reward pathway

histamine release results in vasodilation, bronchoconstriction, hypotension

potentially life-threatening respiratory depression

withdrawal is uncomfortable but not life-threatening
hyperalgesia, diarrhea, dilated pupils, hypertension, sweating, dysphoria, craving

profound addiction and physiological dependence

heroin (opioids)

5

activation of central and peripheral nicotinic acetylcholine receptors
activation of nicotinic acetylcholine receptors in the reward pathway

stimulant effects - increased arousal, concentration
depressant effects - decreased anxiety

withdrawal: irritability, anxiety, dysphoria, difficulty concentrating, restlessness, increased appetite or weight gain

profound addiction and physiological dependence

nicotine

6

activation of cannabinoid receptors in the brain, spinal cord, and reward pathway

depressant-like effects including relaxation
psychedelic-like effects
sympathomimetic effects
increased appetite

tolerance to acute effects develops rapidly
withdrawal tends to be mild including restlessness, irritability, depression, insomnia

addiction and physiological dependence considered less prominent compared to opioids and ethanol

THC (Cannabinoids)

7

stimulants that enhance synaptic release of dopamine and norepinephrine

acute effects: CNS arousal, alertness, euphoria, sympathomimetic effects (increased HR and BP)

overdose leads to cardiac arrhythmia, MI, stroke, seizures
seizures rarer and due to decrease in seizure threshold by unknown mechanism

chronic use can lead to hallucinations, violent behavior, psychosis

tolerance to euphoric effects develops rapidly
reverse tolerance can be seen with continued use - increased risk of cardiac arrhythmia, cerebral vasoconstriction leading to stroke

withdrawal mild in most patients - dysphoria, sleepiness, bradycardia, craving, depression
with major depression or suicidal ideation treat with antidepressants

addiction can be profound
physiological dependence considered less prominent than with alcohol or opioids

amphetamine and methamphetamine

8

stimulants that block reuptake of dopamine, norepinephrine, and serotonin

acute effects: CNS arousal, alertness, euphoria, sympathomimetic effects (increased HR and BP)

overdose leads to cardiac arrhythmia, MI, stroke, seizures
seizures due to blocking GABAa receptors

chronic use can lead to hallucinations, violent behavior, psychosis

tolerance to euphoric effects develops rapidly
reverse tolerance can be seen with continued use - increased risk of cardiac arrhythmia, cerebral vasoconstriction leading to stroke

withdrawal mild in most patients - dysphoria, sleepiness, bradycardia, craving, depression
with major depression or suicidal ideation treat with antidepressants

addiction can be profound
physiological dependence considered less prominent than with alcohol or opioids

cocaine

9

psychedelics related to serotonin
agonists at 5HT, dopamine, and adrenergic receptors
weak effect in reward pathway

peripheral sympathomimetic effect, altered perception, hallucinations (primarily visual, not all drugs/doses), altered mood

tolerance is minimal in most cases
withdrawal can include craving, confusion, anxiety, and depression

addiction and physiological dependence thought to be minimal in most individuals

LSD and psilocybin

10

psychedelics related to dopamine and amphetamines
induce 5HT and dopamine release
agonists at 5HT, dopamine, and adrenergic receptors

peripheral sympathomimetic effect, altered perception, hallucinations (primarily visual, not all drugs/doses), altered mood

tolerance is minimal in most cases
withdrawal can include craving, confusion, anxiety, and depression

addiction and physiological dependence thought to be minimal in most individuals

MDMA/ecstacy

11

dissociatives that inhibit NMDA receptors (in and outside of reward pathway)
developed as general anesthetic agents

acute effects: analgesia, anesthesia, dissociation, sympathomimetic (increased HR and BP)

toxicities include hallucinations, delusions, psychosis, violent behavior
at higher doses - seizures, coma, death

withdrawal symptoms can include craving, confusion, and depression

addiction and physiological dependence is considered less prominent compared to opioids and ethanol

PCP and ketamine

12

alcohol aversion therapy
prevent relapse in recovering alcoholics

inhibits acetaldehyde dehydrogenase leading to accumulation of acetaldehyde upon alcohol consumption which causes flushing, nausea, headache, vomiting, adn hypotension

hepatotoxic at high doses
can lead to marked respiratory depression, cardiovascular collapse, convulsion, closely monitor patient

effectiveness is limited by failures in adherence

disulfram

13

FDA approved anti-craving medications for alcohol addiction, can also be used as anti-epileptic meds

anti-craving mechanism is unknown
known to increase activity of GABAa receptors and inhibit glutamatergic NMDA receptor activity

combination with disulfram is more effective than either alone
not used to treat alcohol withdrawal

acamprosate and topiramate

14

Narcan challenge test before treatment when recovering alcoholic is suspected of using opioids

used in opioid overdose

inhibits mu opioid receptors in ventral tegmental area of the brain - short acting antagonist

cardiac arrhythmias, hepatotoxicity, pulmonary edema, opioid withdrawal

duration/severity of withdrawal symptoms is less severe

Naloxone

15

anti-craving therapy for alcohol addiction, prevent relapse in recovering alcoholics
limited success in treating opioid dependence by preventing high, does not alleviate craving

inhibits mu opioid receptors in ventral tegmental region of the brain - long acting antagonist

hepatotoxic at high dose

combination with disulfram does not offer substantial advantage for recovering alcoholics
inhibits opioid analgesia

Naltrexone

16

used for both drug maintenance therapy and detoxification of opioid addiction
strong opioid analgesic drug

high efficacy agonist at mu opioid receptor
suppresses symptoms of craving and withdrawal due to slow absorption and long half-life
produces plasma opioid levels that remain stable over time and therefore mitigate cravings and withdrawal symptoms
stable concentration bypasses alternating highs and withdrawals seen in heroin use

cardiac arrest/arrhythmias due to prolonged QT syndrome, respiratory arrest, constipation, nausea, risk of death when combined with other CNS depressants

administered orally on a daily basis, has significant abuse liability

methadone

17

used for both drug maintenance therapy and detoxification of opioid addiction

similar to methadone but longer acting

QT prolongation longer than with methadone
ECG monitoring is recommended

administered orally 2-3 times per week

LAAM

18

used for both drug maintenance therapy and detoxification of opioid addiction

partial agonist at mu opioid receptor and antagonist at kappa opioid receptor - long acting

respiratory depression, hypotension, dizziness, sedation, bradyarrhythmia, tachyarrhythmia

overdose is difficult due to partial agonist property
available in combination with naloxone to prevent elicit drug use (Suboxone)

Buprenorphine

19

smoking cessation aid, reduces craving, prevents withdrawal
multiple forms available - gum, patches, nasal spray

different kinetics than smoking
slower absorption and longer lasting nicotine plasma levels - less rewarding
alleviates craving and is associated with less frequent withdrawal symptoms

limited success (15-20%)

Nicotine replacement therapy (NRT)

20

smoking cessation aid, reduces craving, prevents withdrawal

antidepressants (efficacy not related to depression)
mechanism unknown
non-competitive antagonist of nicotinic acetylcholine receptors in reward pathway
weak inhibitor of dopamine, norepinephrine, and 5HT reuptake in reward pathway

black box warning - suicidal thoughts, erratic/aggressive behavior, exacerbation of underlying psychiatric illness

can be combined with NRT to improve results

exercise caution in patients with preexisting psychiatric illnesses

Bupropion

21

smoking cessation aid, reduces craving, prevents withdrawal

partial agonist at alpha4beta2 nicotinic acetylcholine receptors (nAChRs) in ventral tegmental area and nucleus accumbens
inhibits nicotine full agonist activation at nAChRs

black-box warning - suicidal thoughts, erratic/aggressive behavior, exacerbation of underlying psychiatric illness

exercise caution in patients with preexisintg psychiatric illnesses

Varenicline