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pentobarbital (Nembutal)

 

Classes: Sedative/Hypnotics; Barbiturates

Dosing and uses of Nembutal (pentobarbital)

 

Adult dosage forms and strengths

injectable solution: Schedule II

  • 50mg/mL

 

Hypnotic

Initial: 100 mg IV OR 150-200 mg Im

May give small increments of drug after at least 1 minute to reach full effect

Not to exceed 500 mg

 

Barbiturate Coma

Load: 10-15 mg/kg IV over 30 min; follow by 5 mg/kg IV q1hr for 3 doses

Maintenance: 1 mg/kg/hr IV; may increase to 2-4 mg/kg/hr

 

Renal Failure

Use lower dose

 

Hepatic Failure

Use lower dose

 

Other Indications & Uses

Acute convulsive episodes

 

Pediatric dosage forms and strengths

injectable solution: Schedule II

  • 50mg/mL

 

Hypnotic

2-6 mg/kg IM once; not to exceed 100 mg

 

Pre-procedure Sedation

2-6 mg/kg IM, Or

1-3 mg/kg IV

Not to exceed 100 mg Im

 

Geriatric dosage forms and strengths

Not recommended; use lower dose if use becomes necessary

 

Nembutal (pentobarbital) adverse (side) effects

Frequency not defined

Angioedema (rare)

Bradycardia

Hypotension

Agitation

Ataxia

CNS depression

Confusion

Dizziness

Fever

Headache

Hyperkinesia

Nightmares

Nervousness

Somnolence (frequent)

Syncope

Rash

Stevens-Johnson syndrome

Constipation

Nausea

Vomiting

Agranulocytosis (rare)

Megaloblastic anemia with prolonged use (rare)

Injury of liver with prolonged use (rare)

SLe

Apnea

Hypoventilation

 

Warnings

Contraindications

Barbiturate sensitivity, porphyria liver disease, severe respiratory disease

 

Pregnancy and lactation

Pregnancy category: d

Lactation: secreted in breast milk; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Nembutal (pentobarbital)

Mechanism of action

Depresses sensory cortex & decreases motor activity; produces sedation, drowsiness, and hypnosis

 

Pharmacokinetics

Half-Life: 15-50 hr

Onset: 10-15 min (IM); 3-5 min (IV)

Duration: 3-4 hr

Protein bound: 45-70%

Vd: 0.8 L/kg (children); 1 L/kg (adults)

Metabolism: hepatic microsomal enzymes, glucuronidation

Excretion: Mostly urine

Enzymes induced: CYP1A2, CYP2C9/10, CYP3A4

 

Administration

IV Incompatibilities

Additive: chlorpheniramine, ephedrine, hydrocortisone, hydroxyzine, insulin (regular), levorphanol, norepinephrine, penicillin G potassium, pentazocine, phenytoin, promazine, promethazine, Na bicarb, streptomycin, succinylcholine, thiopental, triflupromazine, vancomycin

Syringe: butorphanol, chlorpromazine, cimetidine, dimenhydrinate, diphenhydramine, droperidol, fentanyl, glycopyrrolate, hydroxyzine, meperidine, midazolam, morphine, nalbuphine, pentazocine, prochlorperazine, promazine, promethazine, ranitdine

Y-site: amphotericin B cholSO4, fenoldopam

Not spec: cefazolin, clindamycin, diazepam, tetracycline

 

IV Compatibilities

Additive: amikacin, aminophylline, CaCl2, chloramphenicol, erythromycin, lidocaine, thiopental, verapamiL

Syringe: aminophylline, atropine (<15 min), ephedrine, hyaluronidase, hydromorphone, neostigmine, scopolamine, Na-bicarb, thiopentaL

Y-site: acyclovir, gatifloxacin, insulin, linezolid, propofoL

 

IV Preparation

Solution: no further prep needed (available form: 50 mg/mL)

 

IV/IM Administration

IV: slow push; NMT 50 mg/min

  • only when other routes not available

IM: NMT 5 mL per site; deep into large muscle

Vials are for multiple use (contains 20 mL=1 g)