Benzodiazepine; anxiolytic, anticonvulsant

• Tabs: 2, 5, 10 mg

• Oral solution: 1 mg/mL, 5 mg/mL (contains 19% alcohol)

• Injection: 5 mg/mL (contains 40% propylene glycol, 10% alcohol, 5% sodium benzoate, and 1.5% benzyl alcohol)

• Pediatric rectal gel (Diastat): 2.5, 5 mg (5 mg/mL concentration with 4.4 cm rectal tip delivery system; contains 10% alcohol, 1.5% benzyl alcohol, and propylene glycol); in twin packs.

• Pediatric/Adult rectal gel (Diastat AcuDial):

  • 4.4 cm rectal tip delivery system (Pediatric/Adult): 10 mg (5 mg/mL, delivers set doses of either 5, 7.5, or 10 mg); contains 10% alcohol, and 1.5% benzyl alcohol; in twin packs.

  • 6 cm rectal tip delivery system (Adult): 20 mg (5 mg/mL, delivers set doses of either 10, 12.5, 15, 17.5, 20 mg); contains 10% alcohol, and 1.5% benzyl alcohol; in twin packs.

Sedative/muscle relaxant:

• Child:

  • IM or IV: 0.04–0.2 mg/kg/dose Q2–4 hr; max. dose: 0.6 mg/kg within an 8-hr period.

  • PO: 0.12–0.8 mg/kg/24 hr ÷ Q6–8 hr

• Adult:

  • IM or IV: 2–10 mg/dose Q3–4 hr PRN

  • PO: 2–10 mg/dose Q6–12 hr PRN

Status epilepticus:

• Neonate: 0.3– 0.75 mg/kg/dosis IV cada 15–30 min × 2–3 dosis; max. total dose: 2 mg.

• Child >1 mes : 0.2–0.5 mg/kg/dosis IV  cada 15–30 min; max. total dose: < 5 yr : 5 mg ; ≥ 5 yr : 10 mg. May repeat dosing in 2–4 horas si se requiere.

• Adult: 5–10 mg/dose IV Q10–15 min; max.total dose: 30 mg in an 8-hr period. May repeat dosing in 2–4 hr as needed.

• Rectal dose (using IV dosage form): 0.5 mg/kg/dose followed by 0.25 mg/kg/dose in 10 min PRN.

• Rectal gel: all doses rounded to the nearest available dosage strength; repeat dose in 4–12 hr PRN

  • 2–5 yr: 0.5 mg/kg/dose

  • 6–11 yr: 0.3 mg/kg/dose

  • ≥12 yr and adult: 0.2 mg/kg/dose

Hypotension and respiratory depression may occur. Use with caution in hepatic and renal dysfunction, glaucoma, shock, and depression. Do not use in combination with protease inhibitors. Concurrent use with CNS depressants, cimetidine, erythromycin, itraconazole, and valproic acid may enhance the effects of diazepam. Diazepam is a substrate for CYP 450 2B6, 2 C8, 2 C9, and 3A5–7; and minor substrate and inhibitor for CYP 450 2 C19 and 3A3/4. The active desmethyldiazepam metabolite is a CYP 450 2 C19 substrate.

Administer the conventional IV product undiluted no faster than 2 mg/min. Do not mix with IV fluids.

In status epilepticus, diazepam must be followed by long-acting anticonvulsants. Onset of anticonvulsant effect: 1–3 min with IV route; 2–10 min with rectal route.

For management of status epilepticus, see Chapter 1 , Table 1-5. For additional information, see Chapter 20 , Table 20-7 .

Various generics; previously available as Versed

Benzodiazepine

Injection: 1, 5 mg/mL; some preparations may contain 1% benzyl alcohol

Oral syrup: 2 mg/mL; contains sodium benzoate

Titrate to effect under controlled conditions.

See Chapter 6 for additional routes of administration.

Sedation for procedures:

• Child:

  • IV:

    • 6 mo–5 yr: 0.05–0.1 mg/kg/dose over 2–3 min. May repeat dose PRN in 2–3 min intervals up to a max. total dose of 6 mg. A total dose up to 0.6 mg/kg may be necessary for desired effect.

    • 6–12 yr: 0.025–0.05 mg/kg/dose over 2–3 min. May repeat dose PRN in 2–3 min intervals up to a max. total dose of 10 mg. A total dose up to 0.4 mg/kg may be necessary for desired effect.

    • >12–16 yr: Use adult dose; up to max. total dose of 10 mg.

  • PO:

    • ≥ 6 mo: 0.25–0.5 mg/kg/dose × 1; max. dose: 20 mg. Younger patients (6 mo–5 yr) may require higher doses of 1 mg/kg/dose, whereas older patients (6–15 yr) may require only 0.25 mg/kg/dose. Use 0.25 mg/kg/dose for patients with cardiac or respiratory compromise, concurrent CNS depressive drug, or high-risk surgery.

• Adult:

  • IV: 0.5–2 mg/dose over 2 min. may repeat PRN in 2–3 min intervals until desired effect. Usual total dose: 2.5–5 mg. Max. total dose: 10 mg.

Sedation with mechanical ventilation:

• Intermittent:

  • Infant and child: 0.05–0.15 mg/kg/dose Q1–2 hr PRN

• Continuous IV infusion (initial doses, titrate to effect) :

  • Neonate:

    • < 32 wk of gestation: 0.5 mcg/kg/min

    • ≥ 32 wk of gestation: 1 mcg/kg/min

  • Infant and child: 1–2 mcg/kg/min

Refractory status epilepticus:

• ≥ 2 mo and child: Load with 0.15 mg/kg IV × 1 followed by a continuous infusion of 1 mcg/kg/min and titrate dose upward Q5 min to effect (mean dose of 2.3 mcg/kg/min with a range of 1–18 mcg/kg/min has been reported).

Contraindicated in patients with narrow-angle glaucoma and shock. Use with caution in CHF, renal impairment (adjust dose; see Chapter 31 ), pulmonary disease, hepatic dysfunction, and in neonates. Causes respiratory depression, hypotension and bradycardia. Cardiovascular monitoring is recommended. Use lower doses or reduce dose when given in combination with narcotics or in patients with respiratory compromise.

Drug is a substrate for CYP 450 3A4. Serum concentrations may be increased by cimetidine, clarithromycin, diltiazem, erythromycin, itraconazole, ketoconazole, and protease inhibitors. Sedative effects may be antagonized by theophylline. Effects can be reversed by flumazenil. For pharmacodynamic information, see Chapter 6 .