Diazepam

Question 1

MOA

Answer 1

Inhibition of neurotransmitter in the central nervous system

Bind to receptors in various regions of the brain and spinal cord. This binding increases the inhibitory effects of gamma-aminobutyric acid (GABA). GABAs functions include CNS involvement in sleep induction.

Question 2

Indications for use

Answer 2

Panic disorders, severe anxiety, alcohol withdrawal, and seizures.

Question 3

Pharmacological effects

Answer 3

sedative, muscle-relaxant, enhance memory (amnesia) effect

Question 4

Pharmacokinetics (way of administration, metabolism, elimination, T1/2)

Answer 4

IM, IV, Rectal, Oral 2-10 mg/ met. In liver/elim. Urine/ half-life (88 vs 41 h)

Question 5

Overdose effects

Answer 5

ataxia, drowsiness, dysarthria, sedation, muscle weakness, profound sleep, hypotension, bradycardia.

Extreme overdosage may lead to coma, areflexia, cardio-respiratory depression and apnoea.

Overdose of benzodiazepines in combination with other CNS depressants (including alcohol) may be fatal.

Question 6

Side effects

Answer 6

Drowsiness, headache, dizziness, diarrhea, hypotension, black stool, chills, dark urine, ataxia

Question 7

Contraindications for use

Answer 7

Hypersensitivity, open angle glaucoma, sleep apnea, myasthenia gravis

Question 8

Drug interactions

Answer 8

When used simultaneously with drugs that have a depressant effect on the central nervous system (including neuroleptics, sedatives, hypnotics, opioid analgesics, anesthesia),

the depressive effect on the central nervous system, on the respiratory center, and severe arterial hypotension are enhanced.

Opioid agonist, smoking decrease the action

Question 9

Interactions with products (meal), drinks

Answer 9

In the presence of food mean lag times are approximately 45 minutes as compared with 15 minutes when fasting. Avoid alcohol

Question 10

Children

Answer 10

+ 6 months agr. The clearance of diazepam is 20 to 30 mL/min in young adults

Question 11

Elderly patients

Answer 11

half-life of diazepam is prolonged in neonates, in the elderly, and in patients with kidney or liver disease. In elderly patients, dosage be limited to the smallest effective amount

Question 12

Pregnant women

Answer 12

Category C , the patient should be apprised of the potential hazard to the fetus. when diazepam is used during labor and delivery, as high single doses may produce irregularities in the fetal heart rate. Diazepam passes into breast milk

Question 13

Overdose Treatment

Answer 13

induction of vomiting and administration of activated charcoal (if the patient is conscious), gastric lavage through a tube (if the patient is unconscious), symptomatic therapy, monitoring vital functions, intravenous administration of fluids (to enhance diuresis), and, if necessary, mechanical ventilation . If agitation develops, barbiturates should not be used. The benzodiazepine receptor antagonist flumazenil is used as a specific antidote (in a hospital setting)