Methylphenobarbital

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A barbiturate derivative used as an anticonvulsant


Chemical structure of Methylphenobarbital

Methylphenobarbital, also known as mephobarbital, is a barbiturate derivative that is primarily used as an anticonvulsant in the treatment of epilepsy. It is a central nervous system depressant and has sedative and hypnotic properties.

Pharmacology[edit | edit source]

Methylphenobarbital is a GABA receptor agonist, which enhances the inhibitory effects of gamma-aminobutyric acid (GABA) in the brain. This action helps to stabilize neuronal activity and prevent the excessive firing of neurons that can lead to seizures.

Medical uses[edit | edit source]

Methylphenobarbital is primarily used in the management of epilepsy, particularly in the control of generalized tonic-clonic seizures and partial seizures. It may also be used in the treatment of anxiety and insomnia due to its sedative effects.

Side effects[edit | edit source]

Common side effects of methylphenobarbital include drowsiness, dizziness, and ataxia. Long-term use can lead to tolerance and dependence, and abrupt discontinuation may result in withdrawal symptoms.

Mechanism of action[edit | edit source]

Methylphenobarbital works by enhancing the activity of GABA, the primary inhibitory neurotransmitter in the central nervous system. By increasing GABAergic activity, it helps to reduce neuronal excitability and prevent seizures.

Synthesis and metabolism[edit | edit source]

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

Legal status[edit | edit source]

Methylphenobarbital is a controlled substance in many countries due to its potential for abuse and dependence. It is classified under various schedules depending on the jurisdiction.

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