Nicergoline

Nicergoline Should be taken on an empty stomach.

Recent MI, acute haemorrhage, orthostatic hypotension, severe bradycardia.

Patient with mild bradycardia, gout, and hyperuricaemia. Renal impairment. Elderly. Pregnancy and lactation.

Significant: CNS depression; reduced systolic or diastolic blood pressure; hyperuricaemia; fibrosis (e.g. pulmonary, cardiac, cardiac valvular, retroperitoneal); ergotism.
Gastrointestinal disorders: Abdominal discomfort, diarrhoea, constipation, nausea.
General disorders and administration site conditions: Feeling hot.
Nervous system disorders: Dizziness, drowsiness, headache.
Psychiatric disorders: Agitation, confusion, insomnia.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Vascular disorders: Flushing.

This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery.

Monitor blood pressure periodically, particularly if given with other antihypertensive agents.

Symptom: Transient reduction in blood pressure, particularly with high doses.

Management: Symptomatic and supportive treatment. May administer sympathomimetics and perform continuous blood pressure monitoring in case of serious blood supply deficiency to the brain and heart.

May potentiate the effects of antihypertensive drugs. May potentiate the cardiac effects of β-blockers (e.g. propranolol). May antagonise the vasoconstrictor effect of sympathomimetic agents. May result in prolonged bleeding period with anticoagulants and aspirin.

Description:
Mechanism of Action: Nicergoline is a semisynthetic ergot derivative with α₁-adrenergic blocking activity to produce vasodilation. It appears to exert additional properties that contribute to its effect on dementia or vascular disorders, such as increasing the cerebral blood circulation and consumption of glucose and oxygen and enhancing catecholaminergic neurotransmitter function. Nicergoline may also have an inhibitory effect on platelet aggregation.
Pharmacokinetics:
Absorption: Rapidly and well absorbed. Bioavailability: 5%. Time to peak plasma concentration: 1.5-3 hours (nicergoline); 3-5 hours (10 α-methoxy-9,10-dihydrolysergol [MDL]); 0.5-1 hour (1-methyl-10 α-methoxy-9,10-dihydrolysergol [MMDL]).
Distribution: Volume of distribution: 224 L. Plasma protein binding: 34.7% (MDL); 14.7% (MMDL).
Metabolism: Metabolised mainly via hydrolysis into MMDL (active metabolite), then via demethylation by CYP2D6 to form MDL (main active metabolite).
Excretion: Via urine (82%); faeces (10%). Elimination half-life: 11-20 hours (MDL).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 34040, Nicergoline. https://pubchem.ncbi.nlm.nih.gov/compound/Nicergoline. Accessed Sept. 25, 2025.

Store below 30°C.

Neurodegenerative Disease Drugs / Peripheral Vasodilators & Cerebral Activators

C04AE02 - nicergoline ; Belongs to the class of ergot alkaloids. Used as peripheral vasodilators.

Brayfield A, Cadart C (eds). Nicergoline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/09/2025.

Nicergoline. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/09/2025.

Sergoline 30 mg Tablet (Siam Bheasach Co., Ltd). MIMS Thailand. http://www.mims.com/thailand. Accessed 19/09/2025.

Sermion Film-coated Tablet 30 mg (Viatris [Thailand] Limited). MIMS Thailand. http://www.mims.com/thailand. Accessed 04/09/2025.

Sermion Sugar-coated Tablet 10 mg (Viatris [Thailand] Limited). MIMS Thailand. http://www.mims.com/thailand. Accessed 01/09/2025.