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Nicergoline
Systematic (IUPAC) name
Ergoline-8-methanol, 10-methoxy-1,6-dimethyl-, 8-(5-bromo-3-pyridinecarboxylate), (8b)
OR
[(2S,4R,7R)-2-methoxy-6,11-dimethyl-6,11-diazatetracyclo[7.6.1.0 2,7.012,16]hexadeca-1(16),9,12,14-tetraen-4-yl]methyl 5-bromopyridine-3-carboxylate
Identifiers
CAS number 27848-84-6
ATC code C04AE02
PubChem 34040
DrugBank APRD00617
Chemical data
Formula C 24H26BrN3O3  
Mol. mass 484.386 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Nicergoline is an ergoloid mesylate derivative used to treat senile dementia and other disorders with vascular origins. It has been found to increase mental agility and enhance clarity and perception. 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.

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.[1]

It is marketed under the trade name Sermion.

Contents

Pharmacological action

Nicergoline is an ergot alkaloid derivative that acts as a potent and selective alpha-1A adrenergic receptor antagonist [2] The IC(50) of nicergoline in vitro has been reported to be 0.2 nM [3] 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.

Use and dosage

Nicerogline is used in the following cases:

  • Acute and chronic cerebral metabolic-vascular disorders (cerebral arteriosclerosis, thrombosis and cerebral embolism, transitory cerebral ischaemia). Acute and chronic peripheral metabolic-vascular disorders (organic and functional arteriopathies of the limbs), 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 5-10mg three times a day, however anti-aging preventative purposes may want to consider 5mg once or twice a day more adequate.[4]

Contraindications and cautions

Persons suffering from acute bleeding, myocardial infarction (heart conditions), 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.

Side effects

Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect. Nicergoline can cause side effects they are usually limited to nausea, hot flushes, mild gastric upset, hypotension and dizziness. At high dosages bradycardia, increased appetite, agitation, diarrhea and perspiration have been known to present themselves. There was a single case of Acute Interstitial Nephritis.[5]

Interactions

Nicergoline is known to enhance the cardiac depressive effects of propranolol (Inderal) - caution is advised. At high dosages, it is advisable to seek one’s physician's guidance if combining with potent vasodilators such as bromocriptine, ginko biloba, hydergine, picamilone, vinpocetine or xanthinol nicotinate.

References

  1. ^ "Fioravanti M, Flicker L. Nicergoline for dementia and other age associated forms of cognitive impairment. Cochrane Database of Systematic Reviews 2001, Issue 4. Art. No.: CD003159. DOI: 10.1002/14651858.CD003159". http://www.cochrane.org/reviews/en/ab003159.html. Retrieved 2008-05-27.  
  2. ^ Alvarez-Guerra M, Bertholom N, Garay RP. Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat. Fundam Clin Pharmacol. 1999;13, 50-8.
  3. ^ Moretti A, Carfagna N, Caccia C, Carpentieri M. Effect of ergolines on neurotransmitter systems in the rat brain. Arch Int Pharmacodyn Ther. 1988, 294, 33-45.
  4. ^ Nicergoline drug insert, Pharmacia & Upjohn, October 2000
  5. ^ Nephron Journal , Vol.92 , October 2002 , Nephron 2002;92:676-679 (DOI: 10.1159/000064096)

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