Drug information of Diazepam

Diazepam

Drug group:

Diazepam is a benzodiazepine (ben-zoe-dye-AZE-eh-peens). It affects chemicals in the brain that may become unbalanced and cause anxiety. Diazepam is used to treat anxiety disorders, alcohol withdrawal symptoms, or muscle spasms. Diazepam is sometimes used with other medications to treat seizures.

Mechanism of effect

As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Pharmacodynamic

Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory.

Pharmacokinetics

Absorption: Essentially complete, with a bioavailability of 93%.Protein binding: 98.5%.Metabolism: Hepatic via the Cytochrome P450 enzyme system. Diazepam and its metabolites are excreted mainly in the urine

Dosage

Usual Adult Dose for Anxiety Oral: 2 to 10 mg 2 to 4 times a day. IM or IV: 2 to 5 mg (moderate anxiety) or 5 to 10 mg (severe anxiety) for one dose. May repeat in 3 to 4 hours, if necessary. Usual Adult Dose for Seizures Oral: 2 to 10 mg 2 to 4 times a day. Rectal gel: 0.2 mg/kg, rounded up to the nearest available unit dose. A supplemental dose of 2.5 mg may be added for more precise titration or if a portion of the first dose is expelled. May repeat in 4 to 12 hours. Maximum of 1 episode every 5 days, or 5 episodes per month. Usual Pediatric Dose for Seizures Rectal gel: Infants less than 6 months old: Not recommended; product contains benzoic acid, benzyl alcohol, ethanol 10%, propylene glycol, and sodium benzoate. Prolonged CNS depression has been reported in neonates receiving diazepam. Infants and Children 6 months to 2 years: Dose not established 2 to 5 years: 0.5 mg/kg, rounded up to the nearest available unit dose. 6 to 11 years: 0.3 mg/kg, rounded up to the nearest available unit dose. 12 years or greater: 0.2 mg/kg, rounded up to the nearest available unit dose. A supplemental dose of 2.5 mg may be added in 10 minutes for more precise titration or if a portion of the first dose is expelled. May repeat in 4 to 12 hours. Maximum of 1 episode every 5 days, or 5 episodes per month. Usual Pediatric Dose for Anxiety 1 to 12 years: Oral: 0.12 to 0.8 mg/kg/day in divided doses every 6 to 8 hours as needed. IM: 0.04 to 0.3 mg/kg every 2 to 4 hours as needed, up to a maximum of 0.6 mg/kg in 8 hours. Febrile seizure prophylaxis in children: Oral: 1 mg/kg/day orally in divided doses every 8 hours. Initiate therapy at first sign of fever and continue for 24 hours after fever resolves.

Alerts

Extreme care must be used in administering Diazepam Injection, particularly by the I.V. route, to the elderly, to very ill patients and to those with limited pulmonary reserve because of the possibility that apnea and/or cardiac arrest may occur. Concomitant use of barbiturates, alcohol or other central nervous system depressants increases depression with increased risk of apnea. Resuscitative equipment including that necessary to support respiration should be readily available. 2-When diazepam is used with a narcotic analgesic, the dosage of the narcotic should be reduced by at least one-third and administered in small increments. In some cases the use of a narcotic may not be necessary. 3-Diazepam Injection should not be administered to patients in shock, coma, or in acute alcoholic intoxication with depression of vital signs. 4-Efficacy and safety of parenteral diazepam has not been established in the neonate (30 days or less of age).

Points of recommendation

1-Should be used with caution in patients with renal or hepatic impairment. 2-Do not increase the dose even if you think the medication "does not work anymore" without consulting your physician. 3-Do not stop taking this medication abruptly or decrease the dose without consulting your physician, since withdrawal symptoms can occur.

Pregnancy level

D


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