Isosorbide mononitrate sustained-release capsules (Ⅱ)

Pharmacological action Organic nitrates mainly release nitric oxide (NO), which is the same as the relaxing factor released by the endothelium. It stimulates guanylate cyclase, increases cyclic guanosine monophosphate (cGMP) and causes vasodilation. Isosorbide mononitrate has a direct relaxant effect on vascular smooth muscle, which can cause vasodilation. It has a stronger dilating effect on venous blood vessels, thereby reducing the amount of blood returning to the heart and reducing the preload of the heart. In patients with angina pectoris, the reduction of preload can reduce the already elevated filling pressure of the left and right ventricles, thereby reducing the ventricular diameter and ventricular wall tension and reducing myocardial oxygen demand. Isosorbide mononitrate can also dilate arteries, reduce afterload, and cause a decrease in blood pressure. Isosorbide mononitrate also has a dilating effect on coronary arteries. Toxicological action Acute toxicity Isosorbide mononitrate LD50 (mg/kg body weight) Single oral dose Intravenous push Intravenous drip Rat 291018101820 Mouse 201017601750 Long-term toxicity/subacute toxicity Long-term toxicity experiments in rats have shown no toxic effects. When dogs were given isosorbide mononitrate orally at a dose of 191 mg/kg body weight, the methemoglobin level increased by 2.6% compared to before administration, the concentration of nitrite in plasma was within the detection limit (less than 0.02 mg/l), and there was no change in alkaline phosphate and GPT. Mutagenicity and carcinogenicity In multiple mutagenicity tests (including in vivo and in vitro tests), it was not found to be mutagenic. Long-term rat studies also did not find it to be carcinogenic. Reproductive toxicity In studies of animal embryos, prenatal and postnatal development, isosorbide mononitrate was not found to have teratogenic effects. However, there is no experience of safe use of the drug for pregnant and lactating women.

Isosorbide mononitrate

This product is a capsule, and the contents are white or slightly yellow spherical pellets.

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

Unless otherwise prescribed, take one capsule (40 mg isosorbide mononitrate) once daily. In special cases, the dose may be increased to one capsule (40 mg isosorbide mononitrate) twice daily. Note: When the dose is one capsule twice daily, equivalent to 40 mg isosorbide mononitrate twice daily, the second capsule should be taken no more than 8 hours after the first capsule to fully exert the drug's effect. Dosage form and schedule: The sustained-release capsules should be swallowed whole with an appropriate amount of water after meals and should not be chewed. When discontinuing this product, the dose should be reduced gradually and not stopped suddenly because rebound phenomenon may occur. This drug should not be taken after the expiration date.

Headaches often occur at the beginning of medication (so-called nitrate headaches); experience has shown that they usually disappear after a few days of continued medication. When the drug is first administered or the dose is increased, there is often a decrease in blood pressure accompanied by a reflex increase in heart rate and a feeling of dizziness and sluggishness. Sometimes there is nausea, vomiting, transient redness and heat of the skin, and allergic skin reactions. In rare cases, there may be a severe decrease in blood pressure accompanied by an aggravation of angina symptoms (paradoxical effect of nitrates) and/or a significant paradoxical bradycardia. Collapse and syncope (sudden loss of consciousness) have been reported occasionally, and in individual cases exfoliative dermatitis (inflammatory skin disease) may occur. Tolerance to isosorbide mononitrate and cross-resistance with other nitro compounds have been described with continuous long-term use of high doses. Continuous high doses should be avoided to prevent

--Allergic to nitro compounds or any other ingredients--Acute myocardial infarction with low filling pressure--Left ventricular dysfunction with low filling pressure--Shock state--Severe hypotension (systolic blood pressure less than 90 mmHg)--Myocardial disease with limited cardiac volume (hypertrophic obstructive cardiomyopathy)--Constrictive pericarditis--Cardiac tamponade--Combined use of sildenafil (VIAGRA), because sildenafil can significantly enhance the antihypertensive effect of isosorbide mononitrate.

Precautions for children: No toxic effects on embryos were observed in animal experiments, and it is not clear whether ISMN is excreted through breast milk, but due to the lack of experience with pregnant and lactating women, it should be used with caution. Precautions for pregnancy and lactation: No toxic effects on embryos were observed in animal experiments, and it is not clear whether ISMN is excreted through breast milk, but due to the lack of experience with pregnant and lactating women, it should be used with caution. Precautions for the elderly: Elderly patients may be more sensitive to this type of drug and are more likely to experience dizziness and other reactions.

The concomitant use of blood pressure lowering drugs (antihypertensives), beta-blockers, calcium antagonists, other vasodilators, diazepam or tricyclic antidepressants or alcohol may increase the blood pressure lowering effect of this product. The concomitant use of nitric oxide donors, such as the active ingredient in this product and sildenafil (VIAGRA), can significantly enhance the antihypertensive effect. The concomitant use of this product can increase the blood pressure raising effect of dihydroergotamine. The concomitant use of nonsteroidal antirheumatic drugs cannot be ruled out as a possible reduction in the effect of this product.

Keep away from light and sealed.

40mg

24 months

Beijing Honglin Pharmaceutical Co., Ltd.

• Founded in:

  1993-12-07

• Address:

  Yanqi Industrial Development Zone, Huairou District, Beijing

• Tax NO.:

  91110000621702873B

• Registered Funds:

  $15.8 million

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