Clobazam
Brand name:- Frisium , Lobazam, Clobazam 5,10,20mg cap.
Clobazam is a benzodiazepine. It works by increasing the action of a chemical messenger (GABA) which suppresses the abnormal and excessive activity of the nerve cells in the brain.
Pharmacodynamic:-
Clobazam belongs to the benzodiazepine class of drugs. Clobazam acts on the GABAA receptor to increase GABA nergic transmission, particularly chloride conductance in neurons. This causes neuronal hyperpolarization, resulting in an increase in the action potential threshold and reducing neuron firing frequency. Consequently, the general neuronal activity of the central nervous system is depressed; therefore, clobazam can be used to treat diseases caused by excessive excitatory action potentials.
The effect of clobazam 20 mg and 80 mg administered twice daily on QTc interval was evaluated in a randomized, evaluator-blinded, placebo-, and active-controlled (moxifloxacin 400 mg) parallel thorough QT study in 280 healthy subjects. In a study with demonstrated ability to detect small effects, the upper bound of the one-sided 95% confidence interval for the largest placebo-adjusted, baseline-corrected QTc based on the Fridericia correction method was below 10 ms, the threshold for regulatory concern. Thus, at a dose two times the maximum recommended dose, clobazam did not prolong the QTc interval to any clinically relevant extent.
Mechanism of action:-
The exact mechanism of action for clobazam, a 1,5-benzodiazepine, is not fully understood but is thought to involve the potentiation of GABAergic neurotransmission resulting from binding at the benzodiazepine site of the GABAA receptor.Specifically, clobazam binds to the interface of the α 2 and γ 2-subunit of the GABAA receptor.It has a great affinity for the α2 subunit than the α1 subunit compared to other 1,4‐benzodiazepines.Binding of clobazam to the GABAA receptor causes chloride channels to open, resulting in an influx of chloride and thus hyperpolarization of neurons.
Used:-
Used in the treatment of epilepsy/seizures and severe anxiety.
Side effects:-
Constipation, Sleepiness, Depression, Dizziness, Dryness in mouth, Fatigue, Headache, Nausea, Sedation, Speech disorder, Decreased appetite, Irritability, Aggression, Restlessness, Drug tolerance, Difficulty in paying attention, Tremors, Abnormality of voluntary movements.
Comments
Post a Comment