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Barbiturates

Barbiturates Fact Card

  • Drug Class:
    CNS Depressant, Sedative, Hypnotic, Anxiolytic, Preanesthetic, Anticonvulsant
  • DEA Class:
    Schedule 2: Amobarbital, Pentobarbital, Secobarbital
  • DEA Class:
    Schedule 3: Amobarbital with Noncontrolled Active Ingredient, Amobarbital Suppository Dosage Form, Aprobarbital, Barbituric Acid Derivative (Barbiturates not Specifically Listed), Butabarbital (Secbutabarbital), Butalbital, Butobarbital (Butethal), Pentobarbital with Noncontrolled Active Ingredient, Pentobarbital Suppository Dosage Form, Secobarbital with Noncontrolled Active Ingredient, Secobarbital Suppository Dosage Form, Talbutal, Thiamylal, Thiopental, Vinbarbital
  • DEA Class:
    Schedule 4: Barbital, Methohexital, Methylphenobarbital (Mephobarbital), Phenobarbital
  • Availability in US:
    Prescription Forms
  • Synonyms:
    Depressants, Sedatives, Sleeping Pills, Tranquilizers
  • Brand Names:
    Amytal (Amobarbital), Allzital (Butalbital), Brevital (Methohexital), Butapap (Butalbital), Butisol (Butabarbital), Fioricet (Butalbital), Fiorinal (Butalbital), Lanorinal (Butalbital), Luminal (Phenobarbital), Nembutal (Pentobarbital), Seconal (Secobarbital)
  • Street Names:
    Barbs, Downers, Tranks, Bute (Butabarbital), Phennies (Phenobarbital), Reds (Seconal), Seggies (Secobarbital)

What are barbiturates?

Barbiturates are a class of potent CNS depressant drugs derived from barbituric acid, the original compound developed in the 19th century — most notably secobarbital, phenobarbital, butalbital, pentobarbital, amobarbital, and butabarbital. Others include aprobarbital, barbital, butobarbital (butethal), metharbital, methohexital, methylphenobarbital (mephobarbital), talbutal, thiamylal, thiopental, and vinbarbital. The majority of the latter list are either no longer manufactured or not available in the US.

Barbiturates are prescribed for a number of medical purposes: as sedatives, as hypnotics for treating insomnia, as anticonvulsants, and as preanesthetics to reduce anxiety prior to surgery — most notably under the brand names Seconal, Luminal, Nembutal, Fioricet, Fiorinal, Amytal, and many generic labels. Barbiturates are powerfully addictive and are misused for their euphoric effects and their ability to induce sleep.

Barbiturates Types

Barbiturates are produced commercially, available only by prescription and for use by licensed medical facilities. They are found in the form of oral tablets and capsules, in a variety of shapes and colors — also found in the form of oral solutions and injectable forms. Street barbiturates are licitly manufactured barbiturates that are either diverted prescriptions or the subjects of another form of diversion.

Barbiturates
Barbiturates

Onset and Duration of Action

Barbiturates are commonly divided into groups based on the onset and duration of their action. [1]

  • Short-acting barbiturates — Onset of action: 10–15 minutes, duration of action: 3–4 hours: Secobarbital (Seconal), Pentobarbital (Nembutal).

  • Medium-acting barbiturates — Onset of action: 45–60 minutes, duration of action: 6–8 hours: Amobarbital (Amytal), Aprobarbital, Butabarbital (Butisol).

  • Long-acting barbiturates — Onset of action: 60 minutes or longer, duration of action: 10–12 hours: Mephobarbital, Metharbital, Phenobarbital (Luminal).

Short-acting and medium-acting barbiturates are more attractive to recreational users because they provide quicker results. In cases of barbiturate overdose, those related to long-acting barbiturates, such as phenobarbital, can be more problematic to treat — due to the long half-life and elimination of the drug. These cases often require aggressive interventions, such as ventilatory support and admission to an intensive care unit.

What are the effects of barbiturates?

Barbiturates produce varying levels of relaxation, euphoria, drowsiness, and/or unconsciousness, depending on the specific drug and dose. In general, lower doses or less potent barbiturates may produce euphoric or sedative effects — while higher doses or more potent barbiturates may produce hypnotic, sleep-inducing effects. When high doses are consumed, the threat of death by barbiturate overdose is a strong concern. Consequently, barbiturates have been prominently used in cases of physician-assisted or geriatric suicide.

Barbiturate Abuse and Addiction

The euphoric and sedative properties of barbiturates make them an attractive choice for recreational users. Such users typically procure the drug, directly or indirectly, from individuals possessing legitimate prescriptions. The hypnotic properties of barbiturates make them attractive to those seeking help with sleeping. Barbiturates are often abused in combination with CNS stimulant drugs, such as cocaine, amphetamine, or methamphetamine, either to help neutralize the effects of the stimulant drug or to expedite sleep. [2]

Barbiturates Abuse
Barbiturates Abuse

Barbiturates are powerfully addictive and prone to a very high degree of physical dependence. For the barbiturate addicted attempting abstinence, withdrawal symptoms can be debilitating and long lasting, often requiring professional assistance. Tolerance to barbiturates occurs quickly and physical dependence poses a threat, so medical treatments are typically limited to the short-term. Barbiturates were commonly prescribed until the 1970s, when for the most part, they were replaced by the relatively safer benzodiazepines. Today, barbiturates are prescribed sparingly. [2]

Urine Testing for Barbiturates

Barbiturates urine tests target secobarbital, with possible cross-reactivity for a lengthy list of different barbiturates, including phenobarbital, butalbital, and aprobarbital. Secobarbital is prominent as unchanged parent drug in the urine of those ingesting secobarbital[1] Phenobarbital is prominent as unchanged parent drug in the urine of those ingesting phenobarbital — or as a metabolite in the urine of those ingesting methylphenobarbital (mephobarbital)[1] Butalbital is prominent as unchanged parent drug in the urine of those ingesting butalbital[3] Aprobarbital is prominent as unchanged parent drug in the urine of those ingesting aprobarbital[1]

Barbiturates Drug Test
Barbiturates Drug Test

Approximately 5% of a secobarbital dose is recovered in the urine as unchanged secobarbital, while 25–50% of a phenobarbital dose is recovered in the urine as unchanged phenobarbital, and 25–50% of an aprobarbital dose is recovered in the urine as unchanged aprobarbital. [1] Approximately 3.6% of a butalbital dose is recovered in the urine as unchanged butalbital. [3]

In a study published in Therapeutic Drug Monitoring, volunteers received single doses of secobarbital, phenobarbital, or butalbital, and subsequently submitted to urinalysis screening. Maximum urine concentrations were reported as follows: secobarbital: mean: 406 ng/mL, range: 232–653 ng/mL; phenobarbital: mean: 1,275 ng/mL, range: 665–2,138 ng/mL; butalbital: mean: 798 ng/mL, range: 497–1,888 ng/mL. [4]

Alkalinization of the urine (higher pH) increases renal excretion of some barbiturates, primarily phenobarbital, aprobarbital, and methylphenobarbital (mephobarbital). [1]

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