Nembutal - General Information:A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Pharmacology:Nembutal, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Nembutal for patients
Practitioners should give the following information and instructions to patients receiving barbiturates.
- The use of barbiturates carries with it an associated risk of psychological and/or physical dependence. The patient should be warned against increasing the dose of the drug without consulting a physician.
- Barbiturates may impair mental and/or physical abilities required for the performance of potentially hazardous tasks (e.g., driving. operating machinery, etc.).
- Alcohol should not be consumed while taking barbiturates. Concurrent use of the barbiturates with other CNS depressants (e.g., alcohol, narcotics, tranquilizers, and antihistamines) may result in additional CNS depressant effects.
Most reports of clinically significant drug interactions occurring with the barbiturates have involved phenobarbital. However, the application of these data to other barbiturates appears valid and warrants serial blood level determinations of the relevant drugs when there are multiple therapies.
Anticoagulants: Phenobarbital lowers the plasma levels of dicumarol (name previously used: bishydroxycoumarin) and causes a decrease in anticoagulant activity as measured by the prothrombin time. Barbiturates can induce hepatic microsomal enzymes resulting in increased metabolism and decreased anticoagulant response of oral anticoagulants (e.g., 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 Patients stabilized on anticoagulant therapy may require dosage adjustments if barbiturates are added to or withdrawn from their dosage regimen.
Corticosteroids: Barbiturates appear to enhance the metabolism of exogeneous corticosteroids probably through the induction of hepatic microsomal enzymes. Patients stabilized on corticosteroid therapy may require dosage adjustments if barbiturates are added to or withdrawn from their dosage regimen.
Griseofulvin: Phenobarbital appears to interfere with the absorption of orally administered griseofulvin, thus decreasing its blood level. The effect of the resultant decreased blood levels of griseofulvin on therapeutic response has not been established. However, it would be preferable to avoid concomitant administration of these drugs.
Doxycycline: Phenobarbital has been shown to shorten the half-life of doxycycline for as long as 2 weeks after barbiturate therapy is discontinued.
This mechanism is probably through the induction of hepatic microsomal enzymes that metabolize the antibiotic. If phenobarbital and doxycycline are administered concurrently, the clinical response to doxycycline should be monitored closely.
Phenytoin, sodium vaiproate, valproic acid: The effect of barbiturates on the metabolism of phenytoin appears to be variable. Some investigators report an accelerating effect, while others report no effect. Because the effect of barbiturates on the metabolism of phenytoin is not predictable, phenytoin and barbiturate blood levels should be monitored more frequently if these drugs are given concurrently. Sodium vaiproate and valproic acid appear to decrease barbiturate metabolism; therefore, barbiturate blood levels should be monitored and appropriate dosage adjustments made as indicated.
Central nervous system depressants: The concomitant use of other central nervous system depressants, including other sedatives or hypnotics, antihistamines, tranquilizers, or alcohol, may produce additive depressant effects.
Monoamine oxidase inhibitors (MAOI): M.O. prolong the effects of barbiturates probably because metabolism of the barbiturate is inhibited.
Estradiol, estrone, progesterone and other steroidal hormones: Pretreatment with or concurrent administration of phenobarbital may decrease the effect of estradiol by increasing its metabolism. There have been reports of patients treated with antiepileptic drugs (e.g., phenobarbital) who became pregnant while taking oral contraceptives. An alternate contraceptive method might be suggested to women taking phenobarbital.
Barbiturates are contraindicated in patients with known barbiturate sensitivity. Barbiturates are also contraindicated in patients with a history of manifest or latent porphyria.
Additional information about NembutalNembutal Indication: For the short-term treatment of insomnia.
Mechanism Of Action: Nembutal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Pentobarbital
Synonyms: Pentobarbital Sodium; Pentabarbitone; Pentabarbital; Pentobarbitone; Pentobarbiturate; Pentobarbituric acid; Sodium Pentobarbital
Drug Category: Adjuvants, Anesthesia; GABA Modulators; Barbiturates; Hypnotics and Sedatives
Drug Type: Small Molecule; Approved
Other Brand Names containing Pentobarbital: Dorsital; Ethaminal; Mebubarbital; Mebumal; Nebralin; Nembutal; Nembutal Sodium; Neodorm; Rivadorm;
Absorption: Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: by hepatic microsomal enzyme system
Half Life: 5 to 50 hours (dose dependent)
Dosage Forms of Nembutal: Solution Intravenous
Chemical IUPAC Name: 5-ethyl-5-pentan-2-yl-1,3-diazinane-2,4,6-trione
Chemical Formula: C11H18N2O3
Pentobarbital on Wikipedia: http://en.wikipedia.org/wiki/Pentobarbital
Organisms Affected: Humans and other mammals
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