Exam 3: Abuse Dependence

Front 1

Ethanol Pharmacology

Back 1

main effects in CNS (mostly depressant activities)
Increases GABA-mediated inhibition
Increases inhibition of Ca++ channels
Increases inhibition of NMDA-receptor function

Front 2

Disulfiram (Antabuse)

Back 2

blocks aldehyde dehydrogenase ALDH, resulting in the accumulation of acetaldehyde.
Treatment requires that patient be free of alcohol for at least 24 h.

Front 3

Acamprosate (Campral)

Back 3

It is thought to minimize drinking by acting on GABA and/or NMDA receptors.
Trials comparing acamprosate vs. naltrexone found naltrexone to be superior.

Front 4

Topiramate (Topamax)

Back 4

It blocks Na+channels (+ Ca++ channels & GluR) - potentiates GABA.
It induces P450

Front 5

Naltrexone (ReVia, Depade)

Back 5

An opioid receptor antagonist. It blunts craving or pleasure derived from drinking alcohol. Not to be used in combination with disulfiram => hepatotoxicity

Front 6

Lorazepam (Ativan), oxazepam(Serax) & Chlordiazepoxide (Librium)
Treating alcohol withdrawal is best accomplished with benzodiazepines

Back 6

are preferred for patients with significant liver disease because the half-lives of other benzodiazepines can be prolonged significantly. Metabolized Outside The Liver

Front 7

Other drugs that have been used in the treatment of withdrawal include:

Back 7

Beta-blockers (propranolol (Inderal))
Clonidine (α-adrenergic agonist)
Antipsychotics (phenothiazines(e.g., chlorpromazine))
Other antiepileptics (e.g., phenytoin (Dilantin))

Front 8

Opiates & Opioids
Direct acting drugs

Back 8

Naltrexone (ReVia)
Naloxone (Narcan)
Methadone (Dolophine)
Buprenorphine “Bupe” (Subutex)
Buprenorphine + Naloxone (Suboxone)

Front 9

Opiates & Opioids
Indirect acting drugs

Back 9

Clonidine (Catapres)
Lofexidine (Britlofex)
Opiates (or narcotics) appear to interact with specific receptors interfering with pain impulses.

Front 10

Naltrexone (ReVia) & Naloxone (Narcan)
μOR antagonist (high affinity)

Back 10

Naltrexone can only be used after withdrawal is complete
Naloxone is primarily used to counteract opiate overdoses

Front 11

Methadone (Dolophine)
μOR agonist

Back 11

It prevents euphoria if heroin is taken
Blunts effects of other opioids

Front 12

Buprenorphine “Bupe” (Subutex)
μOR partial agonist and κOR antagonist

Back 12

Blocks effects of pure agonists like heroin
Buprenorphine + Naloxone (Suboxone) use
Low potential for overdose & long duration of action
While on Suboxone, addicts can function/work as members of society

Front 13

Clonidine (Catapres)
α adrenergic receptor agonist

Back 13

blocks symptoms of opioid withdrawal by decreasing sympathetic tone. Methadone, buprenorphine and α adrenergic receptor agonists(clonidine, lofexidine) are commonly used for opioid detoxification.

Front 14

Nicotine (tobacco smoking)
Pharmacological effects

Back 14

CNS: complex effects driven by nicotinic Ach receptors
PNS: Stimulant effects at peripheral ganglia (nicotinic Ach receptors).

Front 15

Nicotine agonists
Nicotine Replacement Therapy (NRT):

Back 15

Nicotine polacrilex chewing gum (Nicorette); lozenges (Commit)
Nicotine transdermal patches (Nicoderm CQ, Nicotrol)
Nicotine inhaler (Nicotrol inhaler): Nicotine nasal spray (Nicotrol NS)

Front 16

Varenicline (Chantix, Champix)
Nicotine partial-agonist

Back 16

reduce cravings for and decrease the pleasurable effects of smoking.
increased risk for certain cardiovascular side effects in patients with cardiovascular disease

Front 17

Bupropion (Zyban) (Wellbutrin)
Atypical Antidepressants

Back 17

reduces the carvings for and nicotine withdrawal effects. It may be a dopamine & NE reuptake inhibitor. It may also be a dopamine & NE releaser. Contraindication: Past or current history of an eating disorder

Front 18

Tablet formulations that reduce the potential for abuse

Back 18

Tablets contain drug + niacin: if tablet is crushed niacin gives an unpleasant taste and GI discomfort.
Tablets that contain drug + an antagonist: the antagonist is released only if tablet is crushed.

Front 19

Amphetamine (abuse & dependence)

Back 19

Indirect acting agonist: (ultimately) releases intracellular stores of catecholamines. Although not a MAOI, amphetamine may inhibit MAO. CNS (behavioral) effect due to release of dopamine rather than NE.

Front 20

Fenfluramine + Phentermine cocktail (“Fen Phen”)

Back 20

Fenfluramine (Pondimin) inhibits serotonin reuptake (SSRi) leading to CNS effects including a feeling of satiety.
Phentermine (Fastin) is an appetite suppressant of the amphetamine class
excess of serotonin => pulmonary hypertension

Front 21

Sibutramine (Meridia)
appetite suppressant (oral anorexiant)

Back 21

serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines but acts more like TCAs
used in combination with a reduced calorie diet and exercise to obtain and keep weight loss.
Increases the risk of cardiovascular events (heart attacks and strokes)

Front 22

Anabolic (Androgenic) Steroid Abuse

Back 22

Used to increase protein anabolism and muscle mass (with exercise). Used to improve appetite and sexual drive.
Effects are dramatic in young females (masculinization). Genitalia of infants are affected when mothers use androgens. Females may have spotting due to progestin activity of testosterone analogs.

Front 23

Volatile Substance Abuse (VSA) (glue sniffing, solvent sniffing abuse)

Back 23

Inhalation of volatile substances occurs mainly among adolescents. VSA gives rise to dose-dependence similar to hypnotic sedatives. Small doses lead to euphoria and other behavior similar to those caused by ethanol. Higher doses may produce convulsions, coma and death.