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Winter Quarter, Exam 3
N/A
40
Pharmacology
Post-Graduate
01/09/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Alprazolam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-hypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA-A receptors (associated with opening chloride channels), this decreases neuronal firing. Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
Chlordiazepoxide
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
diazepam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-hypnotic effect, anticonvulsant effect, muscle relaxation  (spasticity, spasms, gold standard) 

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
lorazepam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
midazolam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
ozazepam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
temazepam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
triazolam
Definition

benzodiazepine

Therapeutic effects: anxiolytic effect (relieve anxiety), sedative-ypnotic effect, anticonvulsant effect, muscle relaxation

MoA: enhance inhibitory GABA recetpors (associated with opening chloride channels), Needs GABA also to open channel

ADR: sedation, drowsiness, lightheadedness, mental clouding, confusion, psycomotor impairment, slurred speech, ataxia, memory impairment-anterograde amnesia, disinhibition of suppressed behavior (prounounced in elderly pt), euphoria, hangover, rebound anxiety, respiratory depression, tolerance (partiularly sedative/hypnotic), dependence, possible teratogenicity (avoid during pregnancy, esp 1st trimester)

Regarding sleep: decreased sleep latency (time to fall asleep), decrease in duration of REM sleep

ADME: metabolized by hepatic microsomal enzyme system, do not induce drug metabolizing enzymes

USE: anxiety, sedative/hypnotic, acute alcohol withdrawal,  convulsive sz, status epilepticus, skeletal muscle spasm relief, pre-anesthetic meds, induction of anesthesia

Drug interactions: additvie with alcohol/CNS depressants, cross tolerance/dependence

Term
flumazenil
Definition

benzodiazepine antagonist (competitive) used to reverse CNS depressant effects of benzodiaepines (esp. surgical anesthesia, or benzodiazepine poisoning)

ADR: trigger sz (esp in pt with epilepsy or already currently dependent), ppt s/sx in addicted individuals

Term
butalbital
Definition

intermediate/ short acting barbiturate

USE: sedative-hypnotic mainly

MoA: facilitating action of GABA at GABA-A receptor-chloride channel (interact on site distinct from GABA/benzodiazepine site), can cause opening of Cl channel without GABA

Effects: sediatve/hypnotic, anxiolytic (suppress REM more than benzodiazepines, more likely to produce hangover), anesthetic effect (surgical anesthesia), depression of respiration, anticonvulsants, euphoria

ADME: cross BBB, induces microsomal enzymes, metabolized by liver

ADR: sedation, drowsiness, lethargy, confusion, ataxy, hanover, too much respiratory depression, disinhibition of suppressed havior, nausea/GI upset, allergic reactions

Drug interactions: additive with CNS depressants

Tendency of abuse. 

Term
pentobarbital
Definition

intermediate/ short acting barbiturate

USE: sedative-hypnotic mainly

MoA: facilitating action of GABA at GABA-A receptor-chloride channel (interact on site distinct from GABA/benzodiazepine site), can cause opening of Cl channel without GABA

Effects: sediatve/hypnotic, anxiolytic (suppress REM more than benzodiazepines, more likely to produce hangover), anesthetic effect (surgical anesthesia), depression of respiration, anticonvulsants, euphoria

ADME: cross BBB, induces microsomal enzymes, metabolized by liver

ADR: sedation, drowsiness, lethargy, confusion, ataxy, hanover, too much respiratory depression, disinhibition of suppressed havior, nausea/GI upset, allergic reactions

Drug interactions: additive with CNS depressants

Tendency of abuse. 

Term
thiopental
Definition

ultra short acting barbiturate

USE: induction of surgical anesthesia

MoA: facilitating action of GABA at GABA-A receptor-chloride channel (interact on site distinct from GABA/benzodiazepine site), can cause opening of Cl channel without GABA

Effects: sediatve/hypnotic, anxiolytic (suppress REM more than benzodiazepines, more likely to produce hangover), anesthetic effect (surgical anesthesia), depression of respiration, anticonvulsants, euphoria

ADME: cross BBB, induces microsomal enzymes, metabolized by liver

ADR: sedation, drowsiness, lethargy, confusion, ataxy, hanover, too much respiratory depression, disinhibition of suppressed havior, nausea/GI upset, allergic reactions

Drug interactions: additive with CNS depressants

Tendency of abuse. 

Term
balcofen
Definition

centrally acting muscle relaxant

MoA: analog of GABA that acts as an agonist at certain types of GABA receptors (GABA-B)-- spinal cord

USE: MS, spinal cord injuries for muscle spasticity

ADR: CNS depression, euphoria, hallucinations, tremors, sz, dependence from chronic use 

Term
cyclobenzaprine
Definition

centrally acting muscle relaxant

MoA: related to TCAs, acts at brainstem to inhibit gamma and alpha motor systems

USE: muscle spasms of local origin

ADR: CNS depression, anticholinergic effects

Term
metaxalone
Definition

centrally acting muscle relaxant

 

generally similar to cyclobenzapine

Term
tizanidine
Definition

centrally acting muscle relaxant

MoA: alpha-2 adrenergic agonist

USE: skeletal muscle relaxant

ADR: hypotension, very sedating

Term
Alcohol (ethanol)
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

ADME: passive diffusion, oxidized in liver, follows zero order kinetics (metabolism independent of time/concentration), goes through alcohol dehydrogenase pathway (ethanol to acetaldehyde in the liver, acetaldehyde is toxic), microsomal ethanol oxidizing system (MEOS, high doses/chronic: induces which may lead to alcohol tolerance, raises possibility of numerous drug interactions), aldehyde metabolism (acetaldehyde to aceteate to water and carbon dioxide through aldehyde dehydrogenase) 

Effects: depression of CNS (release inhibitions, anxiolytic, sedation, hypnosis, anesthesia, respiratory depression, coma, death), anterograde amenesia, reduces  sleep latency, reduces time spent in REM, decreases overall quality of sleep. Hangovers from: acetaldehyde buildup, alcohol analogs in beverages, meatgic changes/dehydration, pharmcodynamic changes in the brain

MoA: disordering of membrane lipids, NT/receptor/channel/signal transduction system changes, enhance effects of GABA at receptor chlroide channel

Other effects: CV (flushing), inhibits secretion of ADH (diuretic effect), inc conce of HDL, decrease conc of LDL, stimulates gastric acid secretion, may stimulate appetite (large amounts supppress), chronic use: hepatic function increased initially, then depletes, accumulation of fat in the liver: hepatitis/cirrhosis, teratogenic (fetal alcohol syndrome), anemia, folic acid deficiency, electrolyte imbalances, endocrine disturbances, increased risk of cancer, organic brain dysfunction

Tolerance: pharmacodynamic, cross tolerance

Managing withdrawal: prevent sz, delirium, arrhythmias, benzodiazepines suppress s/sx

Term
buspirone
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

USE: alleviates mild-moderate anxiety with minimal sedative-hypnotic, muscle relxant, or respiratory depressant effects, low abuse potential (drug of choice for tx o anxiety for pt with history of alcohol/sedative abuse)

MoA: does not act through GABA mecchanisms, evidence suggests may act as partial agonist at serotonin (5-HT1A) receptors

ADR: dizziness, HA, irritability, tachycardia,n/d, high doses: CNS depression

Term
zolpidem
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

USE: newer sedative-hypnotic, less anxiolytic, anticonvulsant, muscle relaxant than benzodiazepines

MoA: enhances effects of GABA at benzodiazepeine receptor (omega-1 site)

ADME: metabolized by liver, long acting

ADR: CNS depression, abuse/dependence less likely than benzodiazepine

Term
zaleplon
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

USE: newer sedative-hypnotic, less anxiolytic, anticonvulsant, muscle relaxant than benzodiazepines

MoA: enhances effects of GABA at benzodiazepeine receptor (omega-1 site)

ADME: metabolized by liver, shorter acting

ADR: CNS depression, abuse/dependence less likely than benzodiazepine

Term
eszopiclone
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

USE: newer sedative-hypnotic, less anxiolytic, anticonvulsant, muscle relaxant than benzodiazepines

MoA: enhances effects of GABA at benzodiazepeine receptor (omega-1 site)

ADME: metabolized by liver, long acting

ADR: CNS depression, abuse/dependence less likely than benzodiazepine

Term
gammahydroxybutyrate (GHB)
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

MoA: analog of GABA that crosses BBB

USE: abused because of CNS effects (date-rape drug), NOT approved for general anesthetic, tx of sleep disorders

ADR: chronic: depdnences, sz, coma, death

Term
ramelteon
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

MoA: agonist at melatonin receptors

USE: quantitatively different from other sedative/hypnotics

 

little potential for abuse/dependence, use with caution in pt with impaired hepatic function, may inc levels of prolactin, decrease levels of testosterone

Term
Melatonin
Definition

miscellaneous anxiolytics and sedative hypnotices (non-barbiturates, non-benzodiazepines)

MoA: hormone produced by pineal gland

USE: OTC sleep aid, may help with jet lag (circadian sleep problems), qualitatively different from other sedative/hypnotics 

Term
disulfiram
Definition

tx alcoholism

MoA: inhibits aldehyde dehydrogenase (conversion of acetaldehyde to acetate)

USE: pt consumes alcohol, severe ADR such as flushing, HA, nausea, confusion may result (unpleasant, encourages abstinence)

Drug interactions, potentially hepatotoxic 

Term
acamprosate
Definition

tx alcoholism

USE: decrease craving for alcohol (maintain abstinence)

MoA: unclear, may involve both glutamate, GABA receptors, block NMDA receptors, partially stimulate GABA-A receptors

ADR:  diarrhea, anxiety, insomnia, depression, less potential of hepatotoxicity (may be most effective when combined with naltrexone) 

Term
naltrexone
Definition

tx alcoholism

USE: reduce craving for alcohol

ADR: hepatotoxic 

Term
phenobarbital
Definition

long acting barbiturate

USE: mainly as anticonvulsant

MoA: facilitating action of GABA at GABA-A receptor-chloride channel (interact on site distinct from GABA/benzodiazepine site), can cause opening of Cl channel without GABA

Effects: sediatve/hypnotic, anxiolytic (suppress REM more than benzodiazepines, more likely to produce hangover), anesthetic effect (surgical anesthesia), depression of respiration, anticonvulsants, euphoria

ADME: cross BBB, induces microsomal enzymes, metabolized by liver

ADR: sedation, drowsiness, lethargy, confusion, ataxy, hanover, too much respiratory depression, disinhibition of suppressed havior, nausea/GI upset, allergic reactions

Drug interactions: additive with CNS depressants

Tendency of abuse. 

Term
chlorpromazine
Definition

phenothiazine

USE: tx schizophrenia

Effects: antipsychotic (effects perceived as unpleasant), sedation (tolerance develops), inhibition of conditioned avoidance response in animals, lowering of sz threshold, anti-emetic, poikilothermic, anticholinergic, antihistaminic, CV (orthostatic hypotension, tachycardia, EKG changes, cardiac arrest), sexual dysfunction, endocrine (increased prolactin), weight gain (appetite stimulation), inhibition of Ca/calmoduline-depependned processes, teratogenic effects

Toxic effects: 

Term
fluphenazine
Definition

phenothiazine

Term
prochlorperazine
Definition
phenothiazine
Term
haloperidol
Definition
nonphenothiazine
Term
trifluoperazine
Definition

phenothiazine

Term
clozapine
Definition
"second gen" or "atypical" antipsycotic
Term
olanzapine
Definition

"second gen" or "atypical" antipsycotic

Term
risperidone
Definition

"second gen" or "atypical" antipsycotic

Term
aripirazole
Definition

"second gen" or "atypical" antipsycotic

Term
quetiapine
Definition

"second gen" or "atypical" antipsycotic

Term
ziprasidone
Definition

"second gen" or "atypical" antipsycotic

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