Isosorbide Mononitrate Tablets

Indications

long-term treatment of coronary heart disease; prevention of angina pectoris; treatment of persistent angina after myocardial infarction; combined with digitalis and / or diuretics, treatment of chronic congestive heart failure.

Clinical pharmacology

Isosorbide mononitrate (ISMN) is the main bioactive metabolite of isosorbide dinitrate. Like other organic nitrates, the main pharmacological action is to relax vascular smooth muscle. ISMN releases nitric oxide (NO), which is the same as endothelium, activates guanylate cyclase, and increases cyclic guanosine monophosphate (cGMP) in smooth muscle cells, thereby relaxing vascular smooth muscle and expanding peripheral arteries and veins. The expansion of the vein is stronger. Venous dilation causes blood to remain in the periphery, reduced blood flow to the heart, reduced left ventricular end-diastolic pressure and pulmonary capillary wedge pressure (pre-load). Arterial dilation reduces peripheral vascular resistance, systolic arterial pressure, and mean arterial pressure (post-load). Coronary artery dilatation increases coronary perfusion. The overall effect is to reduce myocardial oxygen consumption, increase oxygen supply, and relieve angina.

Dosage

oral. 0.5 to 1 tablet at a time, 2 to 3 times a day, 2 tablets for serious cases, 2 to 3 times a day.

Formulation

tablet

specification

20mg

Instruction manual

Approval date:

Date of revision: June 15, 2015 October 20, 2015 December 01, 2017 March 21, 2017

Isosorbide mononitrate tablets instructions

Please read the instructions carefully and use them under the guidance of a physician.

【Drug Name】

Common name: isosorbide mononitrate tablets

Product Name: Xinkang

English name: Isosorbide Mononitrate Tablets

Chinese Pinyin: Danxiaosuan Yishanlizhi Pian

【Ingredients】The main component of this product is isosorbide mononitrate.

Chemical name: 1,4:3,6-dihydro-D-sorbitol-5-mononitrate.

Chemical Structure:

Molecular formula: C6H9NO6           Molecular weight: 191.14

【Properties】 This product is a white film.

【Indications】 long-term treatment of coronary heart disease; prevention of angina pectoris; treatment of persistent angina after myocardial infarction; combined with digitalis and / or diuretics, treatment of chronic congestive heart failure.

【Specification】20mg.

【Usage and dosage】Oral. 0.5 to 1 tablet at a time, 2 to 3 times a day, 2 tablets for serious cases, 2 to 3 times a day.

【Adverse reactions】

At the beginning of the treatment, vasodilatation headache caused by nitrate may occur, and the symptoms may disappear after several days of continuous administration. Facial flushing, dizziness, orthostatic hypotension, and reflex tachycardia may also occur. Occasionally, blood pressure was significantly reduced, bradycardia, angina increased and syncope.

【taboo】

Acute circulatory failure (shock, circulatory collapse); severe hypotension (systolic blood pressure <90mmHg); acute myocardial infarction with low filling pressure (unless under continuous hemodynamic monitoring); hypertrophic obstructive cardiomyopathy; Narrow pericarditis or pericardial tamponade; severe anemia; glaucoma; increased intracranial pressure; allergic to nitro compounds.

【Precautions】

Patients with acute myocardial infarction with low filling pressure should avoid systolic blood pressure below 90 mmHg. Aortic and / or mitral stenosis, orthostatic hypotension and renal insufficiency should be used with caution.

【Pregnant women and lactating women】

No toxic effects on embryos were observed in animal experiments, and it was not clear whether isosorbide mononitrate (ISMN) was excreted by milk. However, due to the lack of experience in the administration of pregnant women and lactating women, it should be used with caution.

【Children's medication】 The study of these drugs is conducted in adults. There is no information on the use of drugs in children and adults, so it is not recommended for children.

【Geriatric Use】Older patients may be more sensitive to this class of drugs, and are more prone to dizziness and other reactions.

【medicine interactions】

Combined with other vasodilators, calcium antagonists, beta blockers, antihypertensives, tricyclic antidepressants and alcohol, it can strengthen the blood pressure lowering effect of this class of drugs.

【Drug overdose】

Responses associated with over-expansion of blood vessels include increased intracranial pressure, dizziness, palpitations, blurred vision, nausea, vomiting, syncope, difficulty breathing, sweating with skin flushing or dampness, conduction block and bradycardia, paralysis, coma, epilepsy Attack or death. No specific antagonists can counteract the vasodilatation of isosorbide mononitrate (ISMN). Epinephrine and other arterial contractions may do more harm than good. Treatment involves raising the lower limbs of the patient to promote venous return and intravenous rehydration. Hemoglobinemia may also occur, and the treatment method is intravenous injection of methylene blue 1-2 mg/kg.

【Pharmacology and Toxicology】

Isosorbide mononitrate (ISMN) is the main bioactive metabolite of isosorbide dinitrate. Like other organic nitrates, the main pharmacological action is to relax vascular smooth muscle. ISMN releases nitric oxide (NO), which is the same as endothelium, activates guanylate cyclase, and increases cyclic guanosine monophosphate (cGMP) in smooth muscle cells, thereby relaxing vascular smooth muscle and expanding peripheral arteries and veins. The expansion of the vein is stronger. Venous dilation causes blood to remain in the periphery, reduced blood flow to the heart, reduced left ventricular end-diastolic pressure and pulmonary capillary wedge pressure (pre-load). Arterial dilation reduces peripheral vascular resistance, systolic arterial pressure, and mean arterial pressure (post-load). Coronary artery dilatation increases coronary perfusion. The overall effect is to reduce myocardial oxygen consumption, increase oxygen supply, and relieve angina.

Carcinogenic and mutagenic phenomena were not observed in animal experiments.

【Pharmacokinetics】

Oral ordinary tablets are completely absorbed in the gastrointestinal tract, no liver first pass effect, bioavailability is nearly 100%, blood concentration peak time is 30 to 60 minutes after taking the drug. The tablet has a working time of 6 hours and an average elimination half-life of 4 to 5 hours. The clearance rate of elderly, liver function or renal dysfunction and cardiac dysfunction is no different from that of healthy young people. ISMN denitrifies in the serum to form isosorbide (about 37%) and dextran (about 7%), which is excreted in the urine, in addition 25% is excreted as glucuronic acid, 2% is excreted as a prototype, feces Exhausted <1%. The metabolites of ISMN have no vasodilator effect.

【Storage】 shading, sealed and stored.

【Packing】 aluminum plastic packaging. 48 pieces / box, 36 pieces / box, 28 pieces / box.

【Validity period】 36 months.

【Executive Standards】 "Chinese Pharmacopoeia" 2015 Edition 2

【Approval No.】 National Drug Standard H10940039

【manufacturer】

Company Name: Lunan Beite Pharmaceutical Co., Ltd.

Production address: No. 243, Yinqueshan Road, Linyi City, Shandong Province

Postal code: 276006

Phone number: 0539-8336336 (Sales) 8336337 (Quality Management Department)

Fax number: 0539-8336029 (Sales) 8336338 (Quality Management Department)

Website: www.LUNAN.com.cn

24-hour customer service hotline: 400-0539-310