Sergoline Mechanism of Action

Pharmacology: Pharmacodynamics: Nicergoline, an ergoline derivative, has arteriolar vasodilating activity. Nicergoline acts by increasing cerebral blood circulation and consumption of oxygen and glucose. It appears to have effect on reducing the cerebrovascular resistance, enhancing catecholaminergic neurotransmitter function and inhibitory effect on platelet aggregation. Moreover, Nicergoline also promotes arterial vasodilation of the limbs by reducing vascular resistances. This can be helpful to correct abnormal blood flow in patients. The therapeutic dose has no effect to systemic arterial pressure.
Pharmacokinetics: Nicergoline is rapidly and almost completely absorbed after oral administration. The drug is metabolized by cytochrome P450 2D6 isozyme. Maximum plasma concentration occurs within 3 hours. More than 90% of the drug bound to human plasma protein (with high affinity for α₁-acid glycoprotein). The major metabolites are 1-methyl-10-methoxy-dihydrolysergol (MMDL) and 10-methoxy-dihydrolysergol (MDL). Nicergoline has linear pharmacokinetics following oral administration. Approximately 70% of drug is excreted in urine.