Nicergoline

Nicergoline, sold under the brand name Sermion among others, is an ergot derivative used to treat senile dementia and other disorders with vascular origins. Internationally it has been used for frontotemporal dementia as well as early onset in Lewy body dementia and Parkinson's dementia. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Unlike many other ergolines, such as ergotamine, nicergoline is not associated with cardiac fibrosis.
It is used for vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs, Raynaud's disease, vascular migraines, and retinopathy.
Nicergoline has been registered in over fifty countries and has been used for more than three decades for the treatment of cognitive, affective, and behavioral disorders of older people.

Medical uses

Nicergoline is used in the following cases:

Acute and chronic cerebral metabolic-vascular disorders. Acute and chronic peripheral metabolic-vascular disorders, Raynaud's disease and other syndromes caused by altered peripheral irrigation.
Migraines of vascular origin
Coadjutant therapy in clinical situations accompanied by platelet hyper-aggregability, arterial tension.
Corio-retinal vascular disorders: diabetic retinopathy, macular degeneration and retinal angiosclerosis
Oto-vestibular problems of a vascular nature: dizziness, auditory hallucinations, hypoacusis.

Dosages for known conditions are usually administered at 5–10 mg three times a day, however anti-aging preventative purposes may want to consider 5 mg once or twice a day more adequate.

Contraindications

Persons suffering from acute bleeding, myocardial infarction, hypertension, bradycardia or using alpha or beta receptor agonists should consult with their physician before use.
Although toxicology studies have not shown nicergoline to have any teratogenic effect, the use of this medicine during pregnancy should be limited to those cases where it is absolutely necessary.
On 28 June 2013, the European Medicines Agency recommended restricting the use of medicines containing ergot derivatives, including nicergoline. They stated that "these medicines should no longer be used to treat several conditions involving blood circulation problems or problems with memory and sensation, or to prevent migraine headaches, since the risks are greater than the benefits in these indications. This is based on a review of data showing an increased risk of fibrosis and ergotism with these medicines." However, only a subset of ergolines are associated with fibrosis and evidence suggests that nicergoline does not carry the same fibrotic risk like other ergoline derivatives such as ergotamine.
Nicergoline is considered unsafe in porphyria.

Side effects

The side effects of nicergoline are usually limited to nausea, hot flushes, mild gastric upset, hypotension and dizziness. At high drug dosages, bradycardia, increased appetite, agitation, diarrhea and perspiration were reported. Most of the available literature suggests that the side effects of nicergoline are mild and transient.

Interactions

Nicergoline is known to enhance the cardiac depressive effects of propranolol. At high dosages, it is advisable to seek one's physician's guidance if combining with potent vasodilators such as bromocriptine, Ginkgo biloba, picamilon, vinpocetine or xantinol nicotinate.

Pharmacology

Pharmacodynamics

Nicergoline is an ergot alkaloid derivative that acts as a potent and selective α_1A-adrenergic receptor antagonist. The IC₅₀ of nicergoline in vitro has been reported to be 0.2 nM. The primary action of nicergoline is to increase arterial blood flow by vasodilation. Furthermore, it is known that nicergoline inhibits platelet aggregation. Studies have shown that nicergoline also increases nerve growth factor in the aged brain. In addition to the α_1A-adrenergic receptor, nicergoline is an antagonist of the serotonin 5-HT_1A receptor and shows moderate affinity for serotonin 5-HT₂ and α₂-adrenergic receptors and low affinity for the dopamine D₁ and D₂ and muscarinic acetylcholine M₁ and M₂ receptors. The major metabolites of nicergoline, MMDL and MDL, show low or no affinity for adrenergic, serotonin, dopamine, or acetylcholine receptors.

Society and culture

Generic names

Nicergoline is the generic name of the drug and its,,, and.

Brand names

In some countries, Sermion is marketed by Viatris after Upjohn was spun off from Pfizer.