Desbutal
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| Combination of | |
|---|---|
| Methamphetamine | Stimulant |
| Pentobarbital | Barbiturate |
| Clinical data | |
| Trade names | Desbutal |
| Routes of administration | By mouth |
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Desbutal was the brand name of a fixed-dose combination formulation composed of 5mg of the central nervous system (CNS) stimulant ("upper") amphetamine derivative, methamphetamine hydrochloride (HCl) and 30 mg of the CNS depressant ("downer") barbiturate, pentobarbital sodium. Manufactured by Abbott Laboratories as a scored tablet to be taken orally.
Marketed as an antidepressant, as well an anorectic for treating obesity, a treatment for narcolepsy, parkinsonism, alcoholism, and some off-label uses, Desbutal had a high potential for abuse and dependence, consequently being discontinued.[1]
Desbutal was designed as round biphasic tablets, with the two active ingredients visibly partitioned between the two faces of the tablet to control their rates of dissolution and achieve a more preferable pharmacokinetic profile. Each tablet featured a yellow half which contained an immediate-release formulation of pentobarbital sodium, and a blue half which contained a sustained-release formulation of methamphetamine hydrochloride (Desoxyn Gradumet). The three dosages of tablets that were manufactured included 5 mg, 10 mg, and 15 mg of methamphetamine hydrochloride with 30 mg, 60 mg, and 90 mg of pentobarbital sodium, respectively. Abuse of Desbutal often involved physical separation of these two halves by sawing with a razor or fingernails, followed by the consumption of each active ingredient independently rather than concurrently. Typically abusers would ingest the blue half containing methamphetamine for stimulation and wakefulness, followed by future ingestion of the yellow half containing pentobarbital as a hypnotic for counteracting stimulant-induced insomnia whenever sleep was desired.
Overdose
Desbutal overdose was typically life-threatening as a result of acute toxicity from pentobarbital poisoning, since the oral median lethal dose (LD50) of pentobarbital sodium is reached significantly sooner than the oral LD50 of methamphetamine hydrochloride when consumed as dosage units with the mass ratio present in Desbutal. Barbiturate overdose is a medical emergency which was treated with immediate gastric lavage, mechanical ventilation, and intermittent intravenous bolus administration of multiple different drugs, since no selective barbiturate binding site receptor antagonists were clinically available as an antidote, and dosages were dependent on individual patient response. These drugs often included picrotoxin, amiphenazole (Daptazile), bemegride (Megimide), and methamphetamine sulfate (Methedrine) in dosages sometimes exceeding 250 mg over the first 24-hour period of being admitted into an intensive care unit (ICU). While a quantitative relationship between the blood levels of barbiturate derivatives and the depression of the central nervous system (CNS) had become established by researchers in 1955, they also emphasized that the accurate correlation of these factors is complicated by the presence of tolerance to the drug, intercurrent disease and senility, as well as the concurrent administration of other noxious substances.