Flashcards in Benzodiazepines 1 Deck (17)
Benzodiazepines - 11 drugs
Benzodiazepines - MOA
Facilitates activity of GABAA receptor-chloride ion channel. Binds receptors with both α1 and α2 subunits. Increases the receptors affinity for GABA, and the frequency of when the channel is open. Increased chloride conductance causes hyperpolarization. GABA dependent.
Also inhibit neuronal reuptake of adenosine. Increases inhibitory effect of adenosine on neurons that release ACh → arousal.
Benzodiazepines - effects
Dose-dependent but limited CNS depression.
Sedative and anxiolytic effect. Hypnosis and anesthesia.
Anterograde amnesia Anticonvulsant effect.
Mild euphoric effect. Pharmacodynamic tolerance, cross-tolerance.
Dilation of coronary arteries and decreased total peripheral resistance (from adenosine reuptake inhibition).
Daytime sedation and hangover.
Suppress slow-wave and REM sleep.
Benzodiazepines - clinical use
Amnesic property for pts undergoing stressful procedures (endoscopy/outpatient surgery).
Occasionally muscle spasm and spasticity.
Benzodiazepines - contraindications
Driving. Use of other CNS depressant
Benzodiazepines - adverse effects
Anterograde amnesia. Motor incoordination, dizziness, excessive drowsiness. Impaired cognitive processing, concentration, judgment, planning. Interfere with driving and psychomotor skills. Drowsiness.
Respiratory depression (IV adm). Mild euphoria. Physical dependence (long-term use).
Benzodiazepines - Withdrawal syndrome
Nonleathal, headache, insomnia, rebound anxiety, irritability, muscle twitches.
Hypotension, arrhythmia (tachy & brady). Fatal massive overdose.
Flumazenil: competitive benzo receptor antagonist.
β-carboline derivatives: inverse agonists
Flumazenil - adverse effects
Seizures, arrhythmias, blurred vision, emotional lability, dizziness.
Medium-acting benzodiazepines - 5 drugs
Short-acting benzodiazepines - 3 drugs
Long-acting benzodiazepines - 3 drugs
Benzos with no active metabolites - 4 drugs
Which benzodiazepines are safer in elderly pts and why? 3 drugs
They bypass phase I oxidation, only phase II conjugation.
Which benzodiazepines are administered only orally? 7 drugs
Benzodiazepines with both oral and parenteral administration - 3 drugs