Benzodiazepines 1 Flashcards Preview

19 Sedative, hypnotic, anxiolytic drugs > Benzodiazepines 1 > Flashcards

Flashcards in Benzodiazepines 1 Deck (17)
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1

Benzodiazepines - 11 drugs

Alprazolam
Chlordiazepoxide
Clonazepam
Diazepam
Estazolam
Flurazepam
Lorazepam
Midazolam
Oxazepam
Tamazepam
Triazolam

2

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.

3

Benzodiazepines - effects

Dose-dependent but limited CNS depression.
Sedative and anxiolytic effect. Hypnosis and anesthesia.
Anterograde amnesia Anticonvulsant effect.
Muscle relaxation.
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.

4

Benzodiazepines - clinical use

Anxiety, insomnia.
Amnesic property for pts undergoing stressful procedures (endoscopy/outpatient surgery).
Seizure disorders.
Occasionally muscle spasm and spasticity.
Alcohol withdrawal.
Preferred short-term.

5

Benzodiazepines - contraindications

Driving. Use of other CNS depressant

6

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).
Fetal malformations

7

Benzodiazepines - Withdrawal syndrome

Nonleathal, headache, insomnia, rebound anxiety, irritability, muscle twitches.
Hypotension, arrhythmia (tachy & brady). Fatal massive overdose.

8

Benzodiazepine antagonist

Flumazenil: competitive benzo receptor antagonist.
β-carboline derivatives: inverse agonists

9

Flumazenil - adverse effects

Seizures, arrhythmias, blurred vision, emotional lability, dizziness.

10

Medium-acting benzodiazepines - 5 drugs

Alprazolam.
Clonazepam.
Estazolam.
Lorazepam.
Temazepam.

11

Short-acting benzodiazepines - 3 drugs

Midazolam
Oxazepam
Triazolam

12

Long-acting benzodiazepines - 3 drugs

Chlordiazepoxide
Diazepam
Flurazepam

13

Benzos with no active metabolites - 4 drugs

Clonazepam
Lorazepam
Oxazepam
Temazepam

14

Which benzodiazepines are safer in elderly pts and why? 3 drugs

Lorazepam.
Oxazepam.
Temazepam.
They bypass phase I oxidation, only phase II conjugation.

15

Which benzodiazepines are administered only orally? 7 drugs

Alprazolam
Clonazepam
Estazolam
Flurazepam
Oxazepam
Temazepam
Triazolam

16

Benzodiazepines with both oral and parenteral administration - 3 drugs

Chlordiazepoxide
Diazepam
Lorazepam

17

Benzodiazepines that are only adm parenterally - 1 drug

Midazolam