Isosorbide mononitrate
Isosorbide mononitrate: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Conditions for dispensing pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Isosorbide mononitrate
ATX code: C01DA14
Active ingredient: Isosorbide mononitrate (Isosorbide mononitrate)
Manufacturer: Unitary Enterprise "Minskinterkaps" (Republic of Belarus); CJSC "Biocom" (Russia)
Description and photo update: 2019-11-07
Prices in pharmacies: from 55 rubles.
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Isosorbide mononitrate is a vasodilating drug of the nitrate group, with antianginal and vasodilating effects.
Release form and composition
Dosage forms:
- capsules: gelatinous, hard, size No. 1, white shell, inside filled with white or almost white odorless powder (in a cardboard box 3 blisters containing 10 capsules);
- tablets: flat-cylindrical, round, color from white to white with a grayish tint; 20 mg each - with a chamfer, 40 mg each - with a line and a chamfer (in a cardboard box 1, 2, 3 or 5 blisters containing 10 tablets).
Each pack also contains instructions for the use of Isosorbide Mononitrate.
Composition of 1 tablet (20/40 mg):
- active substance: isosorbide mononitrate 60%, diluted in lactose - 33.33 / 66.67 mg (corresponds to the content of isosorbide mononitrate - 20/40 mg);
- auxiliary components: magnesium stearate - 1.6 / 3.4 mg; talc - 3.2 / 6.8 mg; primellose (croscarmellose sodium) - 0.8 / 10.2 mg; microcrystalline cellulose - 16 / 47.6 mg; lactose monohydrate - 105.07 / 205.33 mg.
Composition of 1 capsule (20/40 mg):
- active substance: isosorbide mononitrate - 20/40 mg (corresponds to the content of isosorbide mononitrate 40%, diluted with lactose - 50/100 mg);
- auxiliary components: potato starch - 40 mg; magnesium stearate - 2 mg; lactose - in an amount sufficient to obtain the contents of a capsule weighing 200 mg;
- shell: titanium dioxide - 0.873 mg; sodium lauryl sulfate - 0.044 mg; purified water - 10.585 mg; glycerin - 0.095 mg; gelatin - 61.404 mg.
Pharmacological properties
Pharmacodynamics
Isosorbide mononitrate belongs to peripheral vasodilators, mainly affecting the venous vessels. The drug has antianginal and vasodilating properties. Its pharmacological actions include:
- decrease in pressure in the pulmonary circulation;
- decrease in myocardial oxygen demand;
- redistribution of coronary blood flow to ischemic areas;
- expansion of the coronary arteries and improvement of coronary blood flow;
- decrease in preload (through expansion of peripheral veins) and afterload (through a decrease in total peripheral vascular resistance);
- increased exercise tolerance in ischemic heart disease (CHD);
- a decrease in the end diastolic volume of the left ventricle and a decrease in the systolic tension of its walls;
- relaxation of the muscles of the large and small intestine, including the sphincters, esophagus, biliary tract, gallbladder muscles, urinary tract and bronchi;
- promoting regression of manifestations in pulmonary edema.
Isosorbide mononitrate acts at the molecular level by decreasing calcium content in smooth muscle cells, forming cyclic guanosine monophosphate (cGMP) and nitric oxide (NO). When taken orally, its antianginal effect appears after 30 minutes and lasts from 2 to 6 hours.
Pharmacokinetics
- absorption: after oral administration of isosorbide, mononitrate is absorbed quickly and completely. Its bioavailability ranges from 90 to 100%. After approximately 1–1.5 hours, the maximum concentration of the substance in the blood plasma is reached. After 30 minutes, its therapeutic concentration is reached and is 250 ng per 1 ml, during the 4th hour, its value rises to 414 ng per 1 ml, and within 12 hours it drops to 199 ng per 1 ml;
- metabolism: the substance is completely metabolized in the liver without being exposed to the effect of primary origin through the liver. Its metabolites have no pharmacological activity;
- excretion: almost completely in the form of metabolites is excreted by the kidneys and only about 2% unchanged. The half-life of isosorbide mononitrate varies from 4 to 5 hours, and the renal clearance is 1.8 liters per minute;
- tolerance: even in the absence of changes in doses of isosorbide mononitrate and a constant level of nitrate in the blood, a decrease in its effectiveness is noted. Within 24 hours of continuation of treatment, the observed tolerance decreases. When taking the drug intermittently, the development of tolerance is not observed.
The pharmacokinetics of isosorbide mononitrate is not affected by renal or liver failure. The variability of its effectiveness depends on the individual sensitivity of the patient.
With prolonged therapy at high doses, the development of tolerance and cross-tolerance of isosorbide mononitrate with other nitro compounds was noted. To prevent loss or decrease in effectiveness, it is recommended to avoid continuous administration of high doses of the drug.
Indications for use
Capsules:
- angina pectoris - for prevention and long-term treatment;
- chronic heart failure (CHF) - as part of a combination treatment;
- pulmonary hypertension (increased pressure in the pulmonary circulation).
Tablets:
- attacks of stable angina pectoris, including in the postinfarction period - for prevention;
- CHF - as part of combination therapy.
Contraindications
Absolute:
- acute circulatory disorders (vascular collapse, shock);
- cardiogenic shock (in cases where a sufficiently high end-diastolic blood pressure in the left ventricle is not provided through the administration of drugs that have a positive inotropic effect or the use of intra-aortic counterpulsation);
- severe arterial hypotension (diastolic blood pressure (BP) <60 mm Hg, systolic blood pressure <90 mm Hg);
- combination therapy with phosphodiesterase inhibitors, including tadalafil, vardenafil, sildenafil (due to the fact that they potentiate the antihypertensive effect of nitrates);
- hereditary galactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- age under 18;
- individual intolerance to the components of the drug.
Additionally for tablets:
- cardiac tamponade;
- severe hypovolemia;
- acute myocardial infarction with severe arterial hypotension;
- severe mitral and aortic stenosis;
- hemorrhagic stroke;
- hypertrophic cardiomyopathy;
- constrictive pericarditis;
- severe anemia;
- toxic pulmonary edema;
- lactation period.
Relative (Isosorbide mononitrate is prescribed under medical supervision):
- severe renal failure;
- liver failure (due to the risk of methemoglobinemia);
- low filling pressure against the background of acute myocardial infarction, left ventricular failure (it is important not to allow a decrease in systolic blood pressure <90 mm Hg);
- mitral and / or aortic stenosis;
- tendency to orthostatic reactions of vascular regulation;
- pathologies that are accompanied by an increase in intracranial pressure (a further increase in intracranial pressure has so far been noted only with the introduction of high doses of intravenous nitroglycerin).
Additionally for tablets: malnutrition and malnutrition; hypothyroidism; angle-closure glaucoma (due to the likelihood of increased intraocular pressure); recent traumatic brain injury.
Additionally for capsules: glaucoma; pericardial tamponade, constrictive pericarditis, hypertrophic obstructive cardiomyopathy; thyrotoxicosis; severe anemia; pregnancy and lactation.
Isosorbide mononitrate, instructions for use: method and dosage
Pills
Isosorbide mononitrate tablets are taken orally after meals, without chewing, with water.
The initial dose of the drug is 10–20 mg 2 times a day. In the future, the dose is gradually increased by 2 times (up to 20-40 mg) 2-3 times a day, with an interval between doses of 7-8 hours. The maximum dose should not exceed 120 mg per day.
Before starting therapy, it is required to consult a doctor. The duration of the course and the frequency of administration of Isosorbide mononitrate are set individually. It is important to reduce the dose of the drug gradually and avoid abrupt withdrawal.
If you miss the next dose, you can not take a double dose next time. In such cases, you should continue to adhere to the therapy prescribed by your doctor.
Capsules
Capsules Isosorbide mononitrate are taken orally after meals with water.
The dosage of the drug is 20-40 mg 2-3 times a day, observing the interval between doses of 7-8 hours.
The frequency of admission and the duration of therapy are set individually.
Side effects
Possible adverse reactions [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01%, including isolated messages - very rare]:
- nervous system: very often - nitrate headache (usually, with prolonged use of the drug, it disappears within several days); often - a decrease in the speed of psychomotor reactions (especially at the beginning of therapy), blurred vision, drowsiness, stiffness;
- cardiovascular system: often - orthostatic hypotension or decreased blood pressure, which may be accompanied by pallor of the skin, weakness, dizziness, lethargy, tachycardia, etc. (observed after the first dose or after increasing the dose of the drug); infrequently - against the background of severe arterial hypotension, manifestations of angina pectoris (paradoxical reaction to nitrates) may increase and / or severe paradoxical bradycardia, syncope, methemoglobinemia (with prolonged therapy), collapse, collaptoid states (in some cases with fainting and bradyarrhythmia) may develop;
- gastrointestinal tract: infrequently - dryness of the oral mucosa, possibly a slight burning sensation of the tongue, nausea, vomiting;
- skin and subcutaneous tissues: infrequently - redness of the skin of the face, skin allergic reactions, including rash; very rarely - exfoliative dermatitis, Stevens-Johnson syndrome, angioedema;
- others: an increase in the level of vanillin-succinic acid and catecholamines in the urine, sweating.
Long-term treatment with isosorbide mononitrate can lead to transient hypoxemia through a relative redistribution of blood flow to hypoventilated alveolar areas (with coronary artery disease, myocardial hypoxia may develop).
Overdose
The main symptoms: headache, reflex tachycardia, lowering blood pressure with orthostatic dysregulation. Perhaps the appearance of nausea, diarrhea, vomiting, hot flashes, weakness, dizziness. When taking high doses (> 20 mg per 1 kg of body weight), the development of tachypnea, dyspnea, cyanosis, methemoglobinemia associated with the formation of nitrite ions through the metabolism of the drug should be expected. Reception of very high doses can serve to increase intracranial pressure with the onset of cerebral manifestations.
Chronic overdose can lead to an increase in the level of methemoglobin, but the clinical significance of this phenomenon has not been fully established.
Therapy: gastric lavage, placing the patient in a supine position with raised legs, monitoring of the main indicators of vital functions and their correction (if necessary). Against the background of severe arterial hypotension and / or a state of shock, replenishment of the circulating blood volume is required. In exceptional cases, dopamine and / or norepinephrine (norepinephrine) may be administered to improve blood circulation. Infusion of epinephrine (adrenaline) and related compounds is contraindicated.
With methemoglobinemia, depending on the severity, antidotes are used such as:
- ascorbic acid (oral intake of 1 g of vitamin C or intravenous administration in the form of sodium salt);
- exchange blood transfusion, hemodialysis, oxygen therapy;
- methylene blue (intravenous administration up to 50 ml of 1% methylene blue solution);
- toluidine blue (initially intravenously from 2 to 4 mg per 1 kg of body weight, then repeated administrations (if necessary) of 2 mg per 1 kg of body weight are possible, observing an interval between injections of 1 hour.
special instructions
The drug is not intended for the relief of acute myocardial infarction and acute attacks of angina pectoris.
During the period of taking Isosorbide mononitrate, it is necessary to control the heart rate and blood pressure, When discontinuing therapy, it is important to reduce the dose of the drug gradually. Tolerance can develop to isosorbide mononitrate, and cross-tolerance to other nitro compounds. As a consequence, the effectiveness of the drug after the previous use of other nitro compounds is reduced. In order to avoid the development of tolerance to the action of isosorbide mononitrate, it is important not to allow it to be taken continuously in high doses.
With the lability of blood circulation, taking the first dose of the drug can lead to symptoms of acute circulatory failure. It is possible to prevent the appearance of nitrate headaches by taking 10 mg of isosorbide mononitrate at the beginning of therapy or 20 mg in the morning and evening.
It is recommended to exclude the use of ethanol during the treatment period.
Influence on the ability to drive vehicles and complex mechanisms
Patients during the period of treatment should refrain from driving and conducting potentially hazardous activities.
Application during pregnancy and lactation
Pills
During pregnancy, the use of the drug is possible only as directed by a doctor in cases where the potential benefit of therapy to the mother outweighs the predicted risks to the fetus.
If taking Isosorbide mononitrate tablets is necessary during lactation, stop breastfeeding.
Capsules
The drug during pregnancy and during breastfeeding can be prescribed only after a careful assessment of the possible benefits to the mother and potential risks to the fetus.
When taking capsules during lactation, the child should be monitored for possible side effects from mother's therapy.
Pediatric use
Isosorbide mononitrate is not prescribed for patients under 18 years of age.
With impaired renal function
In severe renal failure, Isosorbide mononitrate is used with caution.
For violations of liver function
Patients with hepatic impairment should take the drug under medical supervision.
Drug interactions
Possible interactions of Isosorbide mononitrate with other drugs / substances:
- antipsychotics (neuroleptics), β-blockers, angiotensin-converting enzyme inhibitors, antihypertensive drugs, other vasodilators, slow calcium channel blockers, tricyclic antidepressants, ethanol, diuretics, phosphodiesterase-5 inhibitors, including tadalafil, sildena effect;
- barbiturates: lower the concentration in the blood and accelerate the metabolism of the substance in the blood;
- vasopressor drugs: Isosorbide mononitrate reduces their effectiveness;
- blockers of slow calcium channels (nifedipine, verapamil and others), propranolol, amiodarone: may enhance the antianginal effect of the drug;
- β-adrenostimulants, α-adrenergic blockers (dihydroergotamine, etc.): can reduce the antianginal effect of the drug (excessive decrease in blood pressure, tachycardia);
- m-anticholinergics (atropine and others): the risk of increased intraocular pressure increases;
- enveloping and astringent drugs, adsorbents: reduce the absorption of isosorbide mononitrate from the gastrointestinal tract;
- norepinephrine (norepinephrine): its therapeutic effect decreases.
Since sapropterin is a coenzyme for the synthesis of nitric oxide, when used in combination with any drugs whose action is associated with nitric oxide, including minoxidil, phosphodiesterase-5 inhibitors and classical donors of nitric oxide (for example, molsidomine, sodium nitroprusside, isosorbide mononitrate, isosorbide dinitrate, nitroglycerin) care should be taken.
Analogs
Analogs of Isosorbide mononitrate are Monosan, Isosorbide mononitrate retard, Efoks long, Monizol, Olikard 40 retard, Monochinque, Mono Mac, Efoks 20, Mono Rom retard, Monolong, Olikard 60 retard, Monocinque retard.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life: tablets - 5 years; capsules - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Isosorbide mononitrate
According to the few reviews about Isosorbide mononitrate, it is impossible to assess the effectiveness and safety of its use. The drug is rarely found in pharmacies.
Isosorbide mononitrate price in pharmacies
The approximate price for Isosorbide mononitrate, for 20 tablets per pack, is: dosage 20 mg - 58 rubles, dosage 40 mg - 136 rubles.
Isosorbide mononitrate: prices in online pharmacies
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Drug name Price Pharmacy |
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Isosorbide mononitrate 20 mg tablets 30 pcs. RUB 55 Buy |
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Isosorbide mononitrate 40 mg tablets 30 pcs. 120 RUB Buy |
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Isosorbide mononitrate 40 mg capsules 30 pcs. RUB 128 Buy |
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Isosorbide mononitrate tab. with prolong. release p / o captivity. 40mg No. 30 184 r Buy |
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Isosorbide mononitrate tab. with prolong. release p / o captivity. 60mg No. 30 255 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
