Pharmacology Mnemonics - Flash Cards

Name: Buspirone (Bu Spar)

Class: Antianxiety-Sedative-Hypnotic Agents (Selective Antianxiety Agent)

Mechanism: Agonist for 5-HT 1A and D₂ receptors.

Absorption: Oral ® rapid absorption.

Dist.:

Metabolism.: Extensive 1st-pass Metabolism. (hepatic hydroxylation & dealkylation) ® Metabolismolites that may have slight activity.

Excretion, t½: 2-4 hr.

Toxicity/S.E.s: Wide safety margin. Dizziness, insomnia, nervousness, nausea, headache, myoclonic jerks, chest pain, tinnitus, fatigue. Lower incidence of CNS S.E.s than w/BZDs, but higher incidence of GI S.E.s. Coadmin. w/haloperidol ® ­ serum haloperidol. W/MAO inhib. may cause ­ BP.

Utility: Short-term relief of anxiety w/o signif. sedation, drowsiness, or amnesia.

Special Features: No synergistic/additive effect w/other antianxiety or hypnotic agents. No CNS depression. No known potential for tolerance, dependence, abuse, or withdrawal. May take more than a week for anxiolytic effects to develop.

Name: Flumazenil (Romazicon)

Class: Benzodiazepine Antagonist

Mechanism: Competitive antagonist for BZD receptor ® antagonism of BZD CNS effects, including respiration depression.

Absorption: IV

Dist.: CNS

Metabolism.:

Excretion, t½: Duration of action 1-4 hr. \ repeated admin. often required.

Toxicity/S.E.s: Can precipitate severe abstinence synd. in BZD-dependent patients.

Utility: Treat CNS depressant effects of BZD overdose.

Special Features:

Name: Flurazepam (Dalmane)

Class: Antianxiety-Sedative-Hypnotic Agent (Benzodiazepine)

Mechanism: Acts on BZD receptors closely coupled to GABA_A receptors ® enhancement of GABA inhib. action via ­ freq. of Cl^- channel opening.

Absorption: Oral ® rapid absorption (large variability in indiv. responsiveness).

Dist.: Protein binding ³50%. CNS.

Metabolism.: Liver microsomal N-dealkylation/hydroxylation, then conjug ® inactive glucuronides. No induction of hepatic microsomal enzymes.

Excretion, t½: Urine—mostly Metabolismolized. Long—24-100 hr. Active Metabolismolites.

Toxicity/S.E.s: Acute—excessive depression of CNS fxns (drowsiness, sleep, confusion, disorientation, ataxia, slurred speech, nystagmus, mild amnesia, dementia). May also cause aggression, hyperactivity, delirium, insomnia. Large doses or mixture w/depressants (e.g., EtOH) may cause resp. depression, coma, hallucinations, nightmares, confusion. Chronic—impaired thinking/memory, weight gain/loss. Habituation & physical dependence ® w/drawal syndrome. Abrupt discontinuation ® risk for convulsion (less risk than w/newer BZDs). Metabolism. ¯ in elderly and by cimetidine. Overdose ® serious resp. depression (rarely fatal w/support). ALL BZDs—Use caution w/­ age, pregnancy, EtOH/subst. abuse, depression, driving/dangerous machinery, use of other CNS depressants, narcolepsy, hypersensitivity, chronic use > 1 wk- 1 month (except for epilepsy). Psych & phys dependence.

Utility: Anxiety, insomnia, alcohol w/drawal. Sedation—all BZDs are DOCs for sedation.

Special Features: Older BZD (longer t½, less potency).

Name: Isoflurane (Forane)

Class: General Anesthetic (Halogenated Hydrocarbon)

Mechanism: Stabilizes membranes of excitable tissue ® inhibition of action potential (primarily pre-synaptic blockade of synaptic transmission).

Absorption:Inhaled. Interm. blood solubility®Interm. onset of effect (BGPC = 1.4). MAC = 1.40.

Dist.: Dissolves in blood. Organs w/high perfusion are most affected.

Metabolism.: Very little liver Metabolism. (2%).

Excretion, t½:

Toxicity/S.E.s: Moderately irritating. Low level of cardiac depression. Depresses circulation. Low potential for arrhythmia.

Utility: Induces general anesthesia.

Special Features: Lowest toxicity of the volatile liquids. Non-flammable. Satisfact. analgesia, good relaxation.

Name: Desflurane (Suprane)

Class: General Anesthetic (Halogenated Hydrocarbon)

Mechanism: Stabilizes membranes of excitable tissue ® inhibition of action potential (primarily pre-synaptic blockade of synaptic transmission).

Absorption: Inhaled. Low blood solubility®Rapid onset of effect (BGPC = 0.42). MAC = 6-7.

Dist.: Dissolves in blood. Organs w/high perfusion are most affected.

Metabolism.: Some liver Metabolism.

Excretion, t½:

Toxicity/S.E.s: Moderately irritating. Low level of cardiac depression. Depresses circulation. Low potential for arrhythmia.

Utility: Induces general anesthesia.

Special Features: Produces rapid induction/awakening. Non-flammable. Satisfact. analgesia, good relaxation.