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 Contraindications Hypersensitivity to barbiturates or excipients History of latent porphyria Cautions Too rapid administration may cause respiratory depression, laryngospasm, apnea, or vasodilation with fall in blood pressure Exercise caution when administered to patients with acute or chronic pain; could result in paradoxical excitement or important symptoms could be masked The use of barbiturates as sedatives in the postoperative surgical period and as adjuncts to cancer chemotherapy is well established Administer barbiturates with caution in patients with hepatic damage and at reduced doses initially; barbiturates should not be administered to patients showing the premonitory signs of hepatic coma Concomitant use of alcohol or other CNS depressants may produce additive CNS depressant effects Elderly or debilitated patients may react to barbiturates with marked depression, excitement, and confusion; in some patients, barbiturates repeatedly produce excitement rather than depression Parenteral solutions of barbiturates are highly alkaline; extreme care should be taken to avoid perivascular extravasation or intra-arterial injection; extravascular injection may cause local tissue damage with subsequent necrosis; consequences of intra-arterial injection may vary from transient pain to gangrene of the limb; any complaint of pain in the limb warrants stopping the injection Physical dependence Psychological, tolerance and physical dependence may occur with continued use; patients with psychological dependence on barbiturates may develop a physical dependence on barbiturates by increasing or decreasing the dosage interval without consulting a physician Administration in excess of 400 mg of pentobarbital or secobarbital for approximately 90 days is likely to produce some degree of physical dependence; a dosage of 600-800 mg taken for at least 35 days is sufficient to produce withdrawal seizures To minimize the possibility of overdosage or the development of dependence, limit the prescribing and dispensing of sedative-hypnotic barbiturates, to the amount required for the interval until the next appointment Withdrawal symptoms may occur from abrupt cessation after prolonged use in the dependent person and may result in delirium, convulsions, and possibly death; barbiturates should be withdrawn gradually from any patient known to be taking excessive dosage over long periods of time Therapy should be administered with caution, if at all, to patients who are mentally depressed, have suicidal tendencies, or history of drug abuse Drug interactions overview Barbiturates can induce hepatic microsomal enzymes resulting in increased metabolism and decreased anticoagulant response of oral anticoagulants (eg, warfarin, acenocoumarol, dicumarol, and phenprocoumon); patients stabilized on anticoagulant therapy may require dosage adjustments if barbiturates are added to or withdrawn from their dosage regimen Patients stabilized on corticosteroid therapy may require dosage adjustments if barbiturates are added to or withdrawn from their dosage regimen due to induction of hepatic microsomal enzymes by barbiturates This drug may interfere with the absorption of orally administered griseofulvin, decreasing its blood levels; effects of blood level reduction unknown; preferable to avoid concomitant administration of these drugs Induction of microsomal enzymes by this drug, may shorten the half-life of doxycycline for as long as 2 weeks after barbiturate therapy discontinued; monitor clinical response to doxycycline closely if both drugs administered concurrently Phenytoin and barbiturate blood levels should be monitored more frequently if given concurrently; effect of barbiturates on phenytoin metabolism reported to be variable; sodium valproate and valproic acid appear to decrease barbiturate metabolism; monitor barbiturate blood levels and make appropriate dosage adjustments as necessary Additive CNS effects may result from concomitant use of other CNS depressants; monitor closely Monoamine oxidase inhibitors (MAOI) may inhibit barbiturate metabolism and prolong barbiturate effects; monitor closely This drug may increase the metabolism of estradiol when administered concurrently; patients on oral contraceptives have become pregnant when concurrently treated with antiepileptic drugs; suggest an alternate contraceptive method to women taking this drug General anesthetics and sedation drugs in young children and pregnant women Brain development Prolonged or repeated exposure may result in negative effects on fetal or young children’s brain development Caution with use during surgeries or procedures in children younger than 3 yr or in pregnant women during their third trimester Assess the risk:benefit ratio in these populations, especially for prolonged procedures (ie, >3 hr) or multiple procedures Pregnancy Barbiturates can cause fetal damage when administered to a pregnant woman; retrospective, case-controlled studies have suggested a connection between maternal consumption of barbiturates and a higher-than-expected incidence of fetal abnormalities Following oral or parenteral administration, barbiturates readily cross the placental barrier and are distributed throughout fetal tissues with highest concentrations found in the placenta, fetal liver, and brain; fetal blood levels approach maternal blood levels following parenteral administration Withdrawal symptoms occur in infants born to mothers who receive barbiturates throughout the last trimester of pregnancy If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus Decisions regarding the timing of any elective procedures requiring anesthesia should take into consideration the benefits of the procedure weighed against the potential risks Labor and delivery Hypnotic doses of these barbiturates do not appear to significantly impair uterine activity during labor; full anesthetic doses of barbiturates decrease the force and frequency of uterine contractions; administration of sedative-hypnotic barbiturates to the mother during labor may result in respiratory depression in the newborn Premature infants are particularly susceptible to the depressant effects of barbiturates; if barbiturates are used during labor and delivery, resuscitation equipment should be available Data are currently not available to evaluate effect of barbiturates when forceps delivery or other intervention is necessary; also, data are not available to determine the effect of these barbiturates on the later growth, development, and functional maturation of the child Lactation Exercise caution when a barbiturate is administered to a nursing woman; small amounts of barbiturates are excreted in the milkPregnancy 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. 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 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) No images available for this drug. No images available for this drug.A Patient Handout is not currently available for this monograph.Print FormularyPatient DiscountsAdding plans allows you to compare formulary status to other drugs in the same class.To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.Create Your List of PlansAdding plans allows you to:View the formulary and any restrictions for each plan.Manage and view all your plans together – even plans in different states.Compare formulary status to other drugs in the same class.Access your plan list on any device – mobile or desktop. The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. View explanations for tiers and restrictions Tier Description 1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs. 2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs. 3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs. 4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. NC NOT COVERED – Drugs that are not covered by the plan. Code Definition PA Prior Authorization Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription. 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