Flashcards in Pharmacology V Deck (25)
Name eight benzodiazepines.
Diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam (p.453)
What is the mechanism of action of benzodiazepines?
To facilitate GABA(a) action by increasing FREQUENCY of Cl- channel opening (p.453)
How do benzodiazepines effect sleep patterns?
Decrease REM sleep (p.453)
Which benzodiazepines have short half lives?
Triazolam, oxazepam, midazolam are short acting (p.453)
What is an important consideration when prescribing short acting vs long acting benzodiazepines?
Short acting benzos are more addictive (p.453)
Name seven clinical uses for benzodiazepines.
Anxiety, spasticity, status epilepticus (lorazepam, diazepam), detoxification (especially alcohol withdrawal- DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia) (p.453)
What toxicities are associated with benzodiazapines?
Dependence, additive CNS depression effects with alcohol (p.453)
Compare the overdose risk of benzodiazepines to barbiturates.
Benzodiazapines have less risk of respiratory depression and coma (p.453)
How is benzodiazepine overdose treated?
What is the mechanism of action of Flumazenil?
Competitive antagonist at GABA benzodiazepine receptor (p.453)
Which three drug classes will bind at the GABA(a) receptor (a ligand gated chloride channel)?
EtOH, benzos, barbiturates (p.453)
Name three nonbenzodiazepine hypnotics.
Zolpidem (Ambien), zaleplon, eszopiclone (p.453)
What is the mechanism of action for nonbenzodiazepine hypnotics?
Act via the BZ1 subtype of the GABA receptor (p.453)
What reverses the effects of nonbenzodiazepine hypnotics?
What are nonbenzodiazepine hypnotics use for?
What toxicities are associated with nonbenzodiazepine hypnotics?
Ataxia, headaches, confusion (p.453)
What is the typical duration of nonbenzodiazepine hypnotics?
Short duration due to rapid metabolism by liver enzymes (p.453)
What advantages do nonbenzodiazepine hypnotics have over other sedative-hypnotic drugs?
They cause only modest day-after psychomotor depression and few amnestic effects; carry lower dependence risk than benzos (p.453)
How do anesthetic drugs enter the CNS?
CNS drugs must be lipid soluble to cross the BBB or must be actively transported (p.453)
What property determines whether an anesthetic drug will have rapid induction and recovery times?
Drugs with decreased solubility in blood wil have rapid induction and recovery times (p.453)
What is true of anesthetic drugs with increased solubility in lipids?
Greater potency (1/MAC) (p.453)
What is MAC for anesthetic drugs?
Minimal alveolar concentration at which 50% of the population is anesthesized. It varies with age (p.453)
Name an anesthetic with low blood and lipid solubility.
N2O; fast induction, low potency (p.453)
Name an anesthetic with high blood and lipid solubility.
Halothane; high potency and slow induction (p.453)