Vertinex Mechanism of Action

Pharmacotherapeutic group: Antipsychotics. ATC code: N05AB04.
Pharmacology: Pharmacodynamics: Vertinex contains Prochlorperazine which is a potent phenothiazine neuroleptic.
Prochlorperazine has a wide range of activity arising from its depressant actions on the Central Nervous System and its alpha-adrenergic blocking and weaker anticholinergic activities. It is a dopamine inhibitor; it inhibits prolactin-release-inhibitory factory, considered to be dopamine, thus stimulating the release of prolactin. The turnover of dopamine in the brain is also increased.
It has anti-emetic, antipruritic, serotonin-blocking and weak antihistamine properties and slight ganglion-blocking activity. It inhibits the heat regulating centre so that the patient tends to acquire the temperature of his surroundings. It is analgesic and can relax skeletal muscle. Its actions on the autonomic system produce vasodilation, hypotension and tachycardia. Salivary and gastric secretions are reduced.
Pharmacokinetics: Prochlorperazine is readily absorbed from the gastro-intestinal tract but is subject to considerable first-pass metabolism in the gut wall. It is also extensively metabolised in the liver and is excreted in the urine and faeces in the form of numerous active and inactive metabolites; there is evidence of enterohepatic recycling. Although the plasma half-life has been reported to be only a few hours, it has a very prolonged terminal elimination phase of up to about 3 weeks. Its duration of therapeutic effect can range from a few days to several weeks or possibly longer. It is very extensively bound to plasma proteins. It is widely distributed in the body and crosses the blood-brain barrier to achieve higher concentrations in the brain than in the plasma. Its metabolites also cross the placental barrier and are excreted in breast milk. The rate of metabolism and excretion of phenothiazines decreases in old age.