Benzodiazepines Flashcards
Diazepam (Valium)
Helpful in EtOH, barbituate, benzo withdrawl. Don’t give in pregnancy. Contraindicated in children, sleep apnea. Used as muscle relaxant, anticonvulsant, IV for status epilepticus, prevent seizures/DTs/hallucinations in EtOH/Barbituate withdrawal.
Cimetidine will lengthen elimination half life (decrease metabolism)
Benzodiazepines
“pam” “lam”
Intensify actions of GABA(A), only effective when GABA present- therefore has a maximum effect.
Converted to active metabolites.
Metabolized in liver, Slow metabolism. Do not induce liver enzymes. CNS depression very profound w/EtOH. Elderly sensitive to CNS depressive effect. May impair memory and learning. Schedule IV - although tolerance and dependence can develop when used chronically. Abrupt disuse produces rebound effect of greater insomnia/anxiety. Category D in pregnancy (don’t use!), also C/I in children and sleep apnea.
Chlordiazepoxide
Helpful in withdrawal (EtOH/barbs/benzos)
Flurazepam (Dalmane)
Has a long half life itself and then converted to long-acting metabolite. Insomnia (less REM depression). Use for early morning awakening (drug hangover).
Estazolam (Prosom)
Benzodiazepine
Midazolam (Versed)
Very short action (<2 hrs). Brief duration of action: short surgical procedures. Anterograde amnesia.
Temazepam (Restoril)
Insomnia (less REM depression)
Triazolam (Halcion)
Converted to short acting metabolite. May cause rebound insomnia-do not use chronically-produces psychosis. Insomnia (less REM depression), use for trouble falling asleep (but can stay asleep).
Alprazolam (Xanax)
Converted to short acting metabolite.
Chlorazepate (Tranxene)
Long half life. Helpful in EtOH, barbs, benzo withdrawals.
Lorazepam (Ativan)
Intermediate duration of action. Anticonvulsant, IV for status epilepticus, prevent effects of EtOH/barbs withdrawal.
Oxazepam (Serax)
Intermediate duration of action. Conjugated directly to inactive metabolites. Used in EtOH w/liver damage present.
Flumazenil (Romazicon)
Benzo competitive antagonist. IV only. Administer very slowly. Reverses effects of drugs that work on benzo receptors: zolpidem, zaleplon, eszopiclone. Duration is 30 min. Major antagonist: may trigger w/d and seizures in pts dependent on benzos. Must not be used if thre are any signs of seizures disorders. Used in OD on benzos or reverse midazolam.
may cause seizures in pts with barbituate or tricyclic antidepressant overdose
Uses for Benzodiazepines
Anxiety (except OCD, Agoraphobia and panic disorders, PTSD, Anxiety in children and adolescents)
Insomnia (glurazepam, temazepam, triazolam)
Epilepsy and seizures-
Sedation, amnesia, anesthesia
muscle relaxation
WD from barbiturates and alcohol
Clonazepam
Used for prevention of absence seizures