Description: The instructions for nicergoline tablets were issued by National Medical Products Administration in April, 2002 16,No. [2002] 106 "Notice on Publishing the Catalogue of Instructions for the Fourth Batch of Chemicals". The instruction manual published by National Medical Products Administration is a reference sample of the revised specifications. If there are any doubts, enterprises can propose amendments. Indications should be consistent with the original approved content; Adverse reactions, drug interactions and other contents, the instructions provided by the enterprise can not be less than those listed in the sample draft. For empty items or incomplete items in the sample manual, enterprises should be required to fill in according to the actual situation, such as trade names and specifications.
Drug name
Generic name: nicergoline tablets
Former name:
Trade name:
English name: Nicergoline Tablets
Chinese pinyin: Nimaijiaolin Pian
The main component of this product is nicergoline, and its chemical name is 10α methoxy 1, 6 dimethyl ergoline 8β methanol 5 bromo nicotinate.
Its structural formula:
Molecular formula: C24H26 O3N3Br
Molecular weight: 484.392
character
This product 10mg is a white film-coated tablet, and 30mg is a yellow film-coated tablet. After the film-coated tablet is removed, it appears white.
Pharmacology and toxicology
This product is a semi-synthetic ergot derivative. Has alpha receptor blocking effect and vasodilating effect. It can strengthen the energy metabolism of brain cells and increase the utilization of oxygen and glucose. Promote the conversion of neurotransmitter dopamine to increase nerve conduction, strengthen the synthesis of protein in the brain, and improve brain function.
pharmacokinetics
Niergoline is absorbed rapidly and almost completely after oral administration. The absolute bioavailability is less than 5%. The main metabolites of nicergoline are MMDL( 1,6 dimethyl 8β hydroxymethyl 10α methoxyginergoline) and MDL(6 dimethyl 8β hydroxymethyl 10α methoxyginergoline). Most of nicergoline (> 90%) binds to plasma protein, and its affinity for blood α -acid glycoprotein is higher than that of serum protein. In rats, [3 H] labeled nicergoline (5mg/kg) had the highest radioactivity in the liver. Followed by kidney, lung, pancreas, saliva, lymph, spleen, adrenal gland and myocardium. The radioactivity in the brain is lower than that in the blood. After [3 H] and [14 C] labeled nicergoline were given, renal excretion was the main attenuation route of radioactivity (about 80% of the total). The radioactivity in feces only accounts for10 ~ 20% of the total.
The pharmacokinetic parameters of nicergoline were compared among four groups of young volunteers (average 24 ~ 32 years old) and elderly volunteers (average 69 ~ 70 years old). The results showed that the pharmacokinetics of nicergoline was not affected by age. In patients with severe renal insufficiency, the excretion of MDL and MMDL in urine decreased significantly. After a single oral dose of 30mg nicergoline, the urine excretion of patients with mild, moderate or severe renal insufficiency decreased by 32, 32 and 59% on average, respectively, compared with those with normal renal function.
Bioavailability test was carried out in China. The estimated elimination half-life of MDL was 8.11.6 hours, and the peak time and peak concentration were 2.71.6 hours after domestic 10mg/ tablet was taken orally by 2 healthy volunteers. 12 healthy volunteers took domestic 30mg/ tablet of nicergoline film-coated tablets orally. The estimated elimination half-life of MDL was 8.5 2 hours, and the peak time and peak concentration were 2.61.1hour and102.8 30.5 μ g/ml, respectively.
indication
1, improve the low desire and emotional disorders (slow response, inattention, memory decline, lack of ideas, depression, anxiety, etc.) caused by cerebral arteriosclerosis and sequelae of stroke.
2, acute and chronic peripheral circulation disorders (limb vascular occlusive disease, Raynaud's syndrome, other peripheral circulation symptoms).
It is also suitable for vascular dementia, especially for improving cognition and memory in early treatment and reducing the severity of the disease.
dosage
Take orally, don't chew. 20 ~ 60 mg daily, divided into 2 ~ 3 times. Continuous administration for a sufficient period of time, at least six months; It is up to the doctor to decide whether to continue the medication.
adverse effect
No serious adverse reactions were reported. There may be hypotension, dizziness, stomachache, hot flashes, facial flushing, drowsiness and insomnia. In clinical trials, the concentration of uric acid in blood can be observed to increase, but this phenomenon has no correlation with the dosage and time of administration.
contraindication
This product is not suitable for the following situations: recent myocardial infarction, acute bleeding, severe bradycardia, orthostatic dysfunction, bleeding tendency and allergic to nicergoline.
matters need attention
It should be used under the guidance of a doctor. Usually, this product has no effect on blood pressure at therapeutic dose, but it may gradually lower blood pressure for sensitive patients. Use with caution in patients with hyperuricemia or patients with gout history. Renal insufficiency should be reduced. Pregnant women are generally not suitable for use, and the pros and cons should be weighed when necessary. No alcohol is allowed during taking the medicine.
Keep out of reach of children.
Medication for pregnant and lactating women
Toxicity test failed to show the teratogenic effect of nicergoline. The indications of this medicine show that this medicine is not used for pregnant women and lactating women.
Children's medication
According to the current indications, this drug is not used in children.
Medication for elderly patients
Pharmacokinetics and tolerance tests show that there is no difference in dosage and administration method between adults and elderly patients.
drug interaction
Niergoline tablets may enhance the effect of antihypertensive drugs. Because nicergoline is metabolized by CYTP450 2D6, interaction with drugs through the same metabolic pathway is not excluded.
overdose
Intake of high dose of nicergoline may cause a temporary drop in blood pressure. Generally, you don't need treatment, just lie on your back for a few minutes. Rare cases have insufficient blood supply to the brain and heart, so it is suggested to give sympathomimetic drugs under continuous blood pressure monitoring.
specifications
10mg，30mg
store up
Shading, sealed and preserved.
package
term of validity
registered number of approval
Production enterprise
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