Primidone

Mechanism of action:
Primidone is a deoxybarbiturate derivative. Primidone is metabolized in the liver to phenobarbital, which accounts for the major pharmacological effect, and to PEMA (phenylethylmalonamide). Phenobarbital binds to the barbiturate binding site on the GABA_A receptor complex, prolongs the opening time of the chloride channel, and increases Cl- influx, causing neuronal hyperpolarization. This reduces neuronal excitability, produces sedation and relaxation, and influences central nervous system regulation related to tension headache.
Reference(s):
1. Rajput AH et al. (2014). Medical treatment of essential tremor. J Cent Nerv Syst Dis.
2. Schneider SA et al. (2014). The treatment of tremor. Neurotherapeutics.
3. Haidukewych D et al. (1981). Serial free and plasma valproic acid and phenytoin monitoring and drug interactions. Ther Drug Monit.
