Butallylonal

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Butallylonal

Chemical structure of Butallylonal

Butallylonal is a barbiturate derivative that was developed in the early 20th century. It is known for its sedative and hypnotic properties, which made it useful in the treatment of insomnia and as a pre-anesthetic agent. Like other barbiturates, Butallylonal works by depressing the central nervous system.

Chemical Properties

Butallylonal is chemically classified as a barbiturate, which is a class of drugs derived from barbituric acid. The chemical structure of Butallylonal includes a pyrimidine ring, which is characteristic of barbiturates. The presence of various substituents on the ring structure influences its pharmacological activity.

Pharmacology

Butallylonal acts as a central nervous system depressant. It enhances the activity of the gamma-aminobutyric acid (GABA) neurotransmitter by binding to the GABA_A receptor, which increases the duration of chloride ion channel opening, leading to hyperpolarization of the neuron and decreased neuronal activity.

Mechanism of Action

The primary mechanism of action of Butallylonal is through potentiation of GABAergic transmission. By binding to the GABA_A receptor, Butallylonal increases the inhibitory effects of GABA, leading to sedation and hypnosis.

Clinical Uses

Historically, Butallylonal was used as a sedative and hypnotic for the treatment of insomnia and as a pre-anesthetic medication. However, due to the development of safer alternatives, its use has declined.

Side Effects

Common side effects of Butallylonal include drowsiness, dizziness, and ataxia. In higher doses, it can cause respiratory depression, hypotension, and coma.

History

Butallylonal was first synthesized in the early 20th century as part of the development of barbiturate drugs. It was used clinically for several decades before being largely replaced by benzodiazepines and other non-barbiturate sedatives.

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Contributors: Prab R. Tumpati, MD