Term
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Definition
| benzodiazepine; anxiolytic; PO; intermediate-acting; No active metabolites |
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Term
| chlordiazepoxide (Librium) |
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Definition
| benzodiazepine; anxiolytic, anticonvulsant, withdrawal suppressant; LONG-acting; PO, IM, IV; HAS ACTIVE metaoblites; |
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Term
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Definition
| benzodiazepine; used for induction of anesthesia; IV; short duration; NO active metabolites |
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Term
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Definition
| benzodiazepine, centrally-acting muscle relaxant, anxiolytic, anticonvulsant, anesthesia supplement, withdrawal suppressant; relief of skeletal muscle spasm & spasticity (GOLD STANDARD); LONG-acting; HAS ACTIVE metabolites; PO, IM, IV |
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Term
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Definition
| benzodiazepine; hypnotic, axiolytic, anesthesia supplement, withdrawal suppressant; PO, IM, IV; intermediate duration of action; No active metabolites; NOT oxidized in liver --> appropriate if pt has liver impairment |
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Term
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Definition
| benzodiazepine; hypnotic - tx of sleep disorders; Intermediate duration - PO - NO active metabolites |
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Term
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Definition
| benzodiazepine; hypnotic - tx of sleep disorders; PO - short-acting, NO active metabolites |
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Term
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Definition
| competitive benzodiazepine antagonist; used to reverse CNS depressant effects of benzodiazepines, especially midazolam (Versed) during surgical anesthesia; also used to tx benzodiazepine poisoning; Major ADEs: triggers seizures (epileptics or those currently dependent on benzodiazepines, barbiturates, or alcohol); can precipitate symptoms of withdrawal in addicted individuals |
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Term
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Definition
| barbiturate; short/intermediate-acting; used in HA preparations |
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Term
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Definition
| barbituate; long-acting; 2nd-line anticonvulsant for partial and generalized tonic-clonic seizures |
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Term
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Definition
| barbituate; very-short acting; "truth serum"; action is terminated by REDISTRIBUTION in body - very lipid soluble, crosses BBB easily, redistributes from brain to body fat; |
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Term
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Definition
| barbiturate; short/intermediate-acting; used mainly as sedative-hypnotic |
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Term
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Definition
| centrally-acting muscle relaxant; analog of GABA, agonist of GABA B receptors --> inhibits release of excitatory transmitters --> inhibit spasmogenic reflexes; Tx: spasticity resulting from MS, spinal cord injuries; SEs: CNS depression (sedation, drowsiness, ataxia, muscle weakness), euphoria, hallucinations, tremors, seizures |
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Term
| carisoprodol (Soma), metaxolone (Skelaxin) |
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Definition
| centrally-acting muscle relaxants similar to cyclobenzaprine |
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Term
| cyclobenzaprine (Flexeril) |
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Definition
| centrally-acting muscle relaxant; related to TCAs; acts at brainstem to inhibit both gamma & alpha motor systems; Tx: muscle spasms due strains, pulls, etc.; SEs: CNS depression (sedation, drowsiness, loss of coordination), anticholinergic effects (dry mouth, etc) |
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Term
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Definition
| centrally-acting muscle relaxant; alpha-2 adrenergic agonist approved for use as skeletal muscle relaxant; SEs: hypotension, very sedating |
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Term
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Definition
| anxiolytic, sedative-hypnotic; graded depression of CNS (release of inhibitions --> anxiolytic effect --> sedation --> hypnosis --> anesthesia --> respiratory depression --> coma --> death; Other actions: CV - flushing of skin, increased heat loss --> HPN, Increased diuretic effect, increase HDL & decrease LDL (moderate amts), stimulate appetite (small amts) & suppress appetite (large amts); Chronic: hepatotoxicity (fatty liver), anemia, folic acid deficiency, electrolyte imbalances, endocrine disturbances (gynecomastia, testicular atrophy), increased risk of cancer, organic brain dysfunction; Teratogenic - Fetal Alcohol Syndrome |
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Term
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Definition
| mainly anxiolytic, very mild sedative-hypnotic; Tx: mild-moderate anxiety with minimal sedative-hypnotic, muscle relaxant, or respiratory depressant effects; MoA: partial serotonin (5-HT1A) agonist; very low abuse potential; DOES NOT exhibit cross-tolerance or cross-dependence; DRUG OF CHOICE for tx of anxiety in pts w/ hx of alcohol or sedative abuse that have been brought through acute withdrawal phase; |
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Term
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Definition
| non-benzodiazepine sedative-hypnotic, less so anxiotytic, anticonvulsant, or muscle relaxant; enhances effects of GABA with subtype of receptor-Cl channel complex by interacting with subtype of benzodiazepine receptor; longer acting (6-8 hrs); SEs: CNS depression (sedation, amnesia, impaired cognitive & motor function), REPORTS of people performing complex behaviors (eating, driving) with no memory of event; Causes less suppression of REM sleep & to produce less rebound insomnia; LONG-term use only |
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Term
| gammahydroxybutyrate (GHB - Liquid Ecstasy, Organic Quaalude, Liquid X, Easy Lay, Cherry Meth, Georgia Home Boy) |
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Definition
| analog of GABA that can cross BBB; has ergogenic effect (enhancement of athletic performance) & abused by atheletes; widely abused b/c of CNS effects (sedation, euphoria, amneisa) --> "date-rape drug"; high dose chronic use --> development of seizures, severe CNS depression --> coma, death; causes physical dependence |
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Term
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Definition
| hormone produced by pineal gland; used as an OTC sleep aid; little potential for abuse or dependence; helpful in pts that have sleep problems due to travel (jet lag) |
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Term
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Definition
| sedative/hypnotic that is a melatonin receptor agonist; little to NO abuse potential; useful in tx of travel-related sleep problems (jet lag); |
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Term
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Definition
| non-benzodiazepine sedative-hypnotic, less so anxiotytic, anticonvulsant, or muscle relaxant; enhances effects of GABA with subtype of receptor-Cl channel complex by interacting with subtype of benzodiazepine receptor; longer acting (6-8 hrs); SEs: CNS depression (sedation, amnesia, impaired cognitive & motor function), REPORTS of people performing complex behaviors (eating, driving) with no memory of event; Causes less suppression of REM sleep & to produce less rebound insomnia; short-term use only |
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Term
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Definition
| non-benzodiazepine sedative-hypnotic, less so anxiotytic, anticonvulsant, or muscle relaxant; enhances effects of GABA with subtype of receptor-Cl channel complex by interacting with subtype of benzodiazepine receptor; shorter acting (2-4 hrs); SEs: CNS depression (sedation, amnesia, impaired cognitive & motor function), REPORTS of people performing complex behaviors (eating, driving) with no memory of event; Causes less suppression of REM sleep & to produce less rebound insomnia; short-term use only |
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Term
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Definition
| tx of alcoholism; inhibitor of aldehyde dehydrogenase --> blocks conversion of acetalaldehyde to acetate; If pt on drug takes EtOH --> severe rxn --> flushing, HA, nausea, confusion results; VERY UNPLEASANT!; interacts with many drugs, potentially HEPATOTOXIC |
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Term
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Definition
| tx of alcoholism; decreases craving for alcohol & may maintain abstinence in recovering alcoholics; MoA: is unclear; SEs: diarrhea, anxiety, incomnia, depression; HEPATOTOXICITY |
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Term
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Definition
| tx of alcoholism; long-acting opioid antagonist reduces craving for alcohol in alcoholics; ADRs: hepatotoxicity |
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Term
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Definition
| drugs that decrease activity, reduce excitement, and calm pt |
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Term
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Definition
| drugs that produce drowsiness & facilitate onset & maintenance of sleep from which pt can be aroused |
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Term
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Definition
| drugs that act in CNS to alleviate anxiety |
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Term
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Definition
| drugs that reduce frequency & severity of seizure activity in CNS |
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Term
| centrally-acting muscle relaxants |
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Definition
| drugs that act in CNS to cause relaxation of skeletal muscle, useful in treating muscle spasms & spasticity |
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Term
| Therapeutic Effects of Benzodiazepines - alprazolam, chlordiazepoxide, midazolam, diazepam, lorazepam, temazepam, triazolam |
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Definition
| anxiolytic effect (limbic system); sedative-hypnotic effect (reticular activating system - decrease levels of arousal, wakefulness); anticonvulsant effect - inhibits spread & propagation of seizure activity in cerebral cortex; muscle relaxation - modify internuncial polysynaptic reflexes in brainstem, spinal cord --> relaxation of skeletal muscle |
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Term
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Definition
| drug facilitate/enhance effects of inhibitory GABA; interacts with GABA sub A receptor at Cl channels, opening and allowing influx of Cl into cell --> hyperpolarization --> decreases neuronal firing |
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Term
| Side Effects & Toxicities of Benzodiazepines |
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Definition
| sedation, drowsiness, light-headedness; menatl clouding, confusion, psychomotor impairment, slurred speech, ataxia; anterograde amnesia; disinhibition of suppressed behavior (pronounced in elderly); euphoria; hangover (long-acting especially); rebound anxiety (short-acting); respiratory depression; tolerance; dependence; possible teratogenicity |
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Term
| Withdrawal Effects of Benzodiazepines |
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Definition
| agitation, anxiety, irritability, insomnia, abdominal cramps, sweating, & seizures |
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Term
| Tx of Benzodiazepine Withdrawal |
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Definition
| gradual weaning of pt off drug by decreasing dose by 10% every 2-3 days over a period of 2-3 wks |
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Term
| Altered Sleep Patterns due to Benzodiazepines |
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Definition
| decreased sleep latency; increased duration of stage 2 non-REM sleep; decreased duration of stages 3&4; decreased # of awakenings; some decrease in duration of REM sllep; abrupt cessation --> REM rebound |
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Term
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Definition
| tx of anxiety; sedative-hypnotics; tx of acute alcohol withdrawal; tx of convulsive seizures & status epilepticus; relief of skeletal muscle spasm & spasticity; preanesthetic medication & anesthetic supplement; induction of anesthesia |
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Term
| Pharmacologic Effects of Barbiturates |
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Definition
| sedative/hypnotic & anxiolytic effects - distinction between these effects and more CNS depression blurred; sedate/hypnotic: more suppresssion of REM sleep, greater REM rebound effect, more likely to cause "hangover effect"; general anesthetic effect; more serious respiratory depression; good anticonvulsant effects; euphoria |
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Term
| Adverse Effects of Barbiturates |
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Definition
| sedation, drowsiness, lethargy, confusion, ataxia; hangover effect; respiratory depression (high doses, OD); disinhibition of suppressed behavior; NAUSEA & GI UPSET; ALLERGIC RXNs; AGGRAVATION OF ACUTE INTERMITTENT PORPHYRIA (group of rare disorders passed down through families, in which heme is not made properly) |
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Term
| Drug Interactions with Barbiturates |
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Definition
| additive effects with CNS depressants (alcohol, opioids, antihistamines); MAO-I's enhance CNS depression; oral anticoagulant effects greatly reduced b/c of induction of drug metabolizing enzymes |
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Term
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Definition
| insomnia, anxiety, restlessness, irritability, tremors, EEG changes, nausea, vomiting; grand mal seizures; delirium, hallucinations; can be severe enough to be LIFE-THREATENING EMERGENCY! Tx: symptomatic support + benzodiazepine (control seizures) |
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Term
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Definition
| these drugs produce serious problems at doses just above therapeutic levels; Main symptoms: severe CNS depression (coma & depressed respiration) --> hypotension, shock, and circulatory collapse; Tx: symptomatics (ventilation, hydration) -- NO SPECIFIC ANTIDOTES!! |
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Term
| Side Effects of buspirone (Buspar) |
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Definition
| dizziness, HA, irritability, tachycardia, GI disturbances (nausea, diarrhea), fairly safe even at high doses |
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Term
| Drug Interactions with buspirone (Buspar) |
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Definition
| used with MAO-I's --> HTN; inhibitors of CYP3A4 & cimetidine can increase blood levels; complex interactions with antidepressants & antipsychotics |
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Term
| antihistamines - hydroxyzine (Atarax, Vistaril), promethazine (Phenergan), diphenhydramine (Benadryl, Tylenol PM, etc) |
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Definition
| drugs used for other reasons but with side effects of sedation & drowsiness; used as mild sedatives; also some anxiolytic activity; OTC sleep aids |
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Term
| Beta-adrenergic Blockers - propanolol |
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Definition
| drugs that have some anxiolytic effect; useful in pts with pronounced autonomic symptoms (tachycardia, HPN); also used to tx some types of situational anxiety (stage fright) |
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Term
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Definition
| follows zero order kinetics; an adult metabolizes 7-10 grams (1 drink) per hour; Alcohol Dehydrogenase Pathway --> MOST IMPORTANT (liver), metabolized EtOH at low conc., overloaded at higher conc. or chronic use; MEOS --> metabolizes EtOH at higher conc. or chronic use; Aldehyde Dehydrogenase puts it into Krebs Cycle |
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Term
| Alcohol's Effects on Sleep |
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Definition
| reduces sleep latency; reduces time spent in REM sleep; decreases overall quality of sleep |
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Term
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Definition
| result from acetaldehyde buildup; analogs present in beverages; metabolic changes & dehydratoin resulting from acute intoxication; pharmacodynamic changes in brain |
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Term
| Alcohol Withdrawal Syndrome |
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Definition
| symptoms appear 6-24 hrs after drug is stopped, resolves within 5 days; Mild: anxiety, irritability, insomnia, nausea, sweating, tachycardia, palpitations, hypertension; Severe: anxiety, fear, hallucinations, delirium, tremors, grand mal seizures, hypertension, tachycardia, arrhythmias; very serious, life threatening |
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Term
| Management of Alcohol Withdrawal |
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Definition
| Objective: prevent seizures, delirium, & arrhythmias; Benzodiazepines (diazepam, lorazepam, oxazepam) suppress withdrawal symptoms; Use phenytoin to control seizures; Use clonidine to alleviate autonomic effects (tachycardia, HTN); Antipsychotics (haloperidol) should NOT be used to control hallucinations due to increased risk of seizures; Vitamin supplementation (thiamin); Reduce craving for EtOH with naltrexone (ReVIA) or acomprosate (Campral); |
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