Methylphenobarbital

An anticonvulsant and sedative drug

Methylphenobarbital
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Methylphenobarbital, also known as mephobarbital, is a barbiturate derivative that is primarily used as an anticonvulsant and sedative. It is a central nervous system depressant that works by enhancing the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain.

Pharmacology

Methylphenobarbital is a GABA receptor agonist, which means it increases the effect of GABA, leading to increased inhibitory effects in the central nervous system. This action helps to stabilize neuronal activity and prevent seizures.

Medical uses

Methylphenobarbital is primarily used in the treatment of epilepsy, particularly in the management of generalized tonic-clonic seizures and partial seizures. It may also be used as a sedative in certain medical situations.

Side effects

Common side effects of methylphenobarbital include drowsiness, dizziness, and ataxia. Long-term use can lead to tolerance and dependence.

Mechanism of action

Methylphenobarbital enhances the inhibitory effects of GABA by binding to the GABA_A receptor and increasing the duration of chloride ion channel opening, which hyperpolarizes the neuron and reduces neuronal excitability.

Synthesis and metabolism

Methylphenobarbital is metabolized in the liver to phenobarbital, which is also an active anticonvulsant. This conversion contributes to its long duration of action.

History

Methylphenobarbital was first synthesized in the early 20th century and has been used clinically for many decades. It was developed as a derivative of phenobarbital to provide similar anticonvulsant effects with potentially fewer side effects.

Related pages

• Barbiturate
• Phenobarbital
• Anticonvulsant
• Sedative