DIZAC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DIZAC (DIZAC).
Dizac is a benzodiazepine that enhances the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA_A receptor, resulting in increased chloride ion influx, neuronal hyperpolarization, and inhibition of neuronal excitability.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2C19 isoenzymes; active metabolite N-desmethyldiazepam has a long half-life. |
| Excretion | Renal (70-80% as unchanged drug and metabolites, primarily via glomerular filtration and active tubular secretion), biliary/fecal (15-20%) |
| Half-life | Terminal elimination half-life: 2.5-4 hours in adults; prolonged in renal impairment (up to 20 hours in anuria), neonates, and elderly. Clinical context: Repeated dosing recommended every 4-6 hours. |
| Protein binding | 90-97% bound to serum proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 1.4-2.4 L/kg. High Vd indicates extensive tissue distribution, crossing blood-brain barrier and placenta. |
| Bioavailability | Intramuscular: 80-90%; Oral: 40-60% (due to extensive first-pass metabolism). |
| Onset of Action | Intravenous: 1-5 minutes; Intramuscular: 5-15 minutes; Oral: 30-60 minutes. |
| Duration of Action | Intravenous: 3-6 hours; Intramuscular: 4-6 hours; Oral: 3-6 hours. Duration is dose-dependent and may be shorter with lower doses or in patients with rapid clearance. |
10 mg IV/IM every 4-6 hours as needed; max 40 mg/day.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-50 mL/min: no adjustment; GFR <30 mL/min: administer 50% of normal dose every 6-8 hours. |
| Liver impairment | Child-Pugh Class B: reduce dose by 50%; Class C: contraindicated or use with extreme caution, reduce dose by 75%. |
| Pediatric use | 0.1-0.2 mg/kg/dose IV/IM every 4-6 hours; max 10 mg/dose. |
| Geriatric use | Initiate at 5 mg IV/IM every 6-8 hours; titrate cautiously due to increased risk of sedation and anticholinergic effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DIZAC (DIZAC).
| Breastfeeding | Contraindicated; excreted in breast milk (M/P ratio unknown). Potential for infant sedation and extrapyramidal effects. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: limb reduction defects reported. Second/third trimester: risk of extrapyramidal symptoms, jaundice, hypotonia. Avoid in third trimester due to neonatal effects. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and extrapyramidal signs. Fetal ultrasound for growth and anomalies. Neonatal monitoring for withdrawal and EPS. |
■ FDA Black Box Warning
DIZAC should not be used in neonates or premature infants due to the risk of severe hypotension, bradycardia, and respiratory depression. Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death.
| Serious Effects |
Hypersensitivity to benzodiazepines; myasthenia gravis; severe respiratory insufficiency; acute narrow-angle glaucoma; sleep apnea syndrome; infants under 30 days of age.
| Precautions | Risk of respiratory depression, especially with high doses or in elderly patients; risk of dependence and withdrawal; caution in hepatic or renal impairment; use with caution in patients with acute narrow-angle glaucoma. |
| Food/Dietary | Grapefruit and grapefruit juice may increase diazepam levels and risk of adverse effects; limit or avoid consumption. Caffeine may reduce the sedative effect; monitor for decreased efficacy. High-fat meals may slow absorption of extended-release formulations; take consistently with or without food. |
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| Fertility Effects | May cause hyperprolactinemia leading to menstrual irregularities, anovulation, and reduced fertility. Reversible upon discontinuation. |
| Clinical Pearls | DIZAC (diazepam) is a benzodiazepine with rapid onset for acute anxiety, seizures, and muscle spasms. Use with caution in elderly due to fall risk; avoid abrupt discontinuation to prevent withdrawal. Monitor respiratory depression when co-administered with opioids or alcohol. Injectable form must be administered slowly intravenously (5 mg/min) to avoid phlebitis. For status epilepticus, rectal gel is an alternative when IV access is unavailable. |
| Patient Advice | Do not drive or operate heavy machinery until you know how this medication affects you, as it causes drowsiness and dizziness. · Avoid alcohol and other central nervous system depressants (e.g., opioids, sleep aids) as they can worsen side effects and lead to dangerous sedation. · Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. Abruptly stopping can cause withdrawal symptoms such as anxiety, insomnia, and seizures. · Do not chew or crush extended-release capsules; swallow them whole. · Inform your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding, as diazepam may harm the fetus or pass into breast milk. · Store at room temperature away from moisture and heat. Keep out of reach of children. |