Peripheral vasodilator with a predominant influence on the venous vessels. It has a vasodilating and antianginal effects.
Decreases preload (due to expansion of peripheral veins) and afterload (due to a decrease in total peripheral vascular resistance) reduces myocardial oxygen demand, expanding coronary artery and improves coronary blood flow, facilitates its redistribution in the ischemic area, reduces the end-diastolic volume of the left ventricle and decreases systolic voltage of its walls. Improves exercise capacity in patients with ischemic heart disease, reduces the pressure in the pulmonary circulation.
Isosorbide mononitrate is relaxation of the muscles of the bronchi, the urinary tract, muscle of the gallbladder, biliary tract and esophagus, as well as small and large intestines, including the sphincters.
At the molecular level, nitrates act by formation of nitric oxide (NO) and cyclic guanozilmonofosfata (cGMP), which is considered a mediator of relaxation. The ingestion of isosorbide-5-mononitrate antianginal effect is already apparent after 30 minutes and lasts for 2-6 hours.
It is rapidly and completely absorbed after oral administration. Bioavailability is 90 to 100%. The maximum plasma concentration is reached after about 1-1.5 hours.
Therapeutic concentrations of isosorbide-5-mononitrate in the blood is reached after 30 minutes and 250 ng / ml, for 4 th hour – 414 ngml during the 12th hour -199 ng / mL (i.e., slow drop concentration) . Isosorbide-5-mononitrate is almost completely metabolized in the liver and undergoes de effect of “first pass” through the liver (unlike izosorbuaa dinitrate). Metabolites – pharmacologically inactive.
Isosorbide-5-mononitrate is excreted by the kidneys almost exclusively in the form of metabolites. Approximately 2% is excreted unchanged. The half-life of 4-5 h., which is 8 times higher than that of isosorbide dinitrate.
It describes the development of tolerance and cross-tolerance with other nitro compounds by prolonged continuous treatment with high doses of isosorbide – 5 -mononitrata. To prevent the reduction or loss of effectiveness, to avoid continuous high doses of the drug.
Berlin-Chemie / Menarini Germany
isosorbide-5-mononitrate 40 mg.
lactose monohydrate – 160 mg
Microcrystalline cellulose – 82.5 mg
corn starch – 10 mg,
talc – 5 mg,
Magnesium stearate – 2.5 mg.
Angina, chronic heart failure, acute myocardial infarction
Prevention of angina attacks in patients with coronary artery disease, including after myocardial infarction.
Treatment of chronic heart failure (in a combination therapy).
Hypersensitivity (including to other organic nitrates), the acute phase of myocardial infarction, acute circulatory disorders (shock collapse), hemorrhagic stroke, severe hypotension (less than 90/60 mm Hg. V.), Simultaneous phosphodiesterase inhibitor sildenafil (Viagra), post-traumatic brain injury, angle-closure glaucoma, children up to 18 years.
Headache (in the beginning of treatment, with continued therapy – reduced); after the first dose – lowering blood pressure and / or the development of orthostatic hypotension (accompanied by tachycardia, dizziness, weakness).
Very rarely – nausea, vomiting, flushing, allergic skin reactions.
How to accept, acceptance rate and dosage
Inside, after a meal with water without chewing.
Frequency of administration and duration of treatment are determined individually.
Tselesooobrazno begin therapy at a dose of 20 mg (1/2 tab.) 2 times / day.
Then gradually increase to therapeutic dose – 40 mg (1 tab.) On reception 2-3 times / day at intervals of 7-8 hours.
The maximum daily dose is 120 mg.
Store in the dark, the reach of children at a temperature not higher than 25 ° C.
The hypotensive effect reinforce other vasodilators, antihypertensive agents, beta-blockers, calcium channel blockers, antipsychotics, phosphodiesterase inhibitors (sildenafil) alcohol.
Monochinkve® should not be used for the relief of acute attacks of angina and acute myocardial infarction.
During treatment requires monitoring of blood pressure and heart rate.
abrupt discontinuation should be avoided (the dose reduced gradually).
Perhaps the development of tolerance to Monochinkve® or cross tolerance to other nitro compounds (reducing drug efficacy due to prior use of other nitro compounds). To prevent the development of tolerance to the action Monochinkve® avoid its continuous reception in high doses.
In patients with labile circulation may develop symptoms of acute circulatory failure, already at the first dose.
“Nitrate” Headaches can be largely prevented if at the beginning of therapy, take 1/2 tab. Monochinkve® morning and evening.
In the period of treatment should be to exclude the use of ethanol.
Effects on ability to drive vehicles and other machines that require high concentration of attention
During treatment is not recommended to drive and engage in other potentially hazardous activities that require a rapid psychomotor reactions.
Symptoms: reduction in blood pressure with orthostatic dysregulation, reflex tachycardia, and headache. It may appear weakness, dizziness, hot flashes, nausea, vomiting and diarrhea. At high doses (20 mg / kg body weight) should expect methemoglobinemia, cyanosis, dyspnea and tachypnea from the formation of nitrite ions as a result of metabolism of isosorbide mononitrate. Very high doses can cause increased intracranial pressure with the occurrence of cerebral symptoms. In chronic overdose may cause a higher level of methemoglobin. although the clinical significance of this has not been definitively established.
Treatment: gastric lavage, the patient should be put in a horizontal position with raised legs. Should monitor the main indicators of vital signs and adjust if necessary. Patients with severe arterial hypotension and / or in shock should be administered liquid; in exceptional cases, to improve blood circulation can be performed infusion noradrenaline (norepinephrine), and / or dopamine. Introduction of epinephrine (adrenaline) and related compounds is contraindicated.
Depending on the severity, the following antidotes are used in cases of methemoglobinemia:
- Vitamin C 1 g orally or in the form of the sodium salt / in
- methylene blue: to 50 ml of a 1% solution of methylene blue / in
- toluidine blue: initially 24 mg / kg body weight / in; then, if necessary, may be repeated administration of 2 mg / kg body weight at an interval between doses of 1 h.
Spend as oxygen therapy, hemodialysis, exchange transfusion.