Isosorbide mononitrate

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Available since: 2019-09-19

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Clinical Pharmacology

Antianginal drug, organic nitrate. Peripheral vasodilator with a predominant effect on the venous vessels.

Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes the activation of intracellular guanylate cyclase, resulting in an increase in cGMP (vasodilation mediator).

Reduces the oxygen demand of the myocardium by reducing preload and afterload (reduces the end-diastolic volume of the left ventricle and reduces the systolic stress of its walls). It has a coronary expanding action.

Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema. Contributes to the redistribution of coronary blood flow in areas with reduced blood circulation.

Increases exercise tolerance in patients with coronary artery disease, angina.

Expands the vessels of the brain, dura mater, which may be accompanied by headache.

Like other nitrates, cross-tolerance develops. After cancellation (interruption of treatment), sensitivity to it is quickly restored.

Antianginal effect occurs within 30-45 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics

Suction

After ingestion, isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract. Bioavailability - 90-100%. C_max reached after 30 minutes and is 100 ng / ml.

Distribution

Binding to plasma proteins - less than 4%.

Metabolism

Isosorbide mononitrate is almost completely metabolized in the liver to form pharmacologically inactive metabolites.

Removal

T_1/2 is about 4-5 hours. It is excreted by the kidneys almost exclusively in the form of metabolites, 2% - unchanged.

Indications

Prevention of angina attacks in patients with coronary artery disease, including after myocardial infarction.

Chronic heart failure (as part of combination therapy).

Composition

1 tablet contains:

Active substances: isosorbide mononitrate 20 mg.

Excipients: lactose monohydrate 151.7 mg, talc 7 mg, colloidal silicon dioxide 3.5 mg, potato starch 27 mg, microcrystalline cellulose 33 mg, aluminum stearate 2.8 mg.

Isosorbide mononitrate is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
			pills
Monocinque retard	Berlin-Chemie/Menarini	Germany	capsules
Monocinque	Berlin-Chemie/Menarini	Germany	pills
Effox long	UCB Pharma	Belgium	pills
Effox long	UCB Pharma	Belgium	capsules
Pectrol	Krka dd Novo mesto AO	Slovenia	pills
Monosan	PRO.MED.CS Praha a.s	Czech	pills

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Dosage and Administration

The dose of the drug and the frequency of administration set individually depending on the severity of the disease. It is advisable to start therapy with small doses of the drug: 10 mg 2 times / day. Then gradually increase the dose to therapeutic - 20-40 mg in 1-2 doses. If necessary, the dose is increased to 60 mg / day. The maximum daily dose is 80 mg. The duration of treatment and repeated courses - as recommended by the doctor.

pills should be taken orally, after meals, swallowing whole, not chewed and washed down with a small amount of liquid.

Adverse reactions

Since the cardiovascular system: at the beginning of treatment, a headache ("nitrate" headache) may occur, which usually decreases after several days of therapy; dizziness, flushing of the skin, sensation of heat, tachycardia. Sometimes at the first dose of the drug or after increasing the dose, there is a decrease in blood pressure and / or orthostatic hypotension, which may be accompanied by a reflex increase in heart rate, lethargy, as well as dizziness and a feeling of weakness. In rare cases - increased angina attacks (paradoxical reaction to nitrates), orthostatic collapse. Cases of collaptoid states have been reported, sometimes with bradyarrhythmia and syncope.

Use of the drug Effox 20 can lead to transient hypoxemia due to the relative redistribution of blood flow in the hypoventilated alveolar segments. This may be the trigger of ischemia in IHD.

From the digestive system: nausea, vomiting, the appearance of a slight burning sensation of the tongue, dry mouth.

From the side of the central nervous system: stiffness, drowsiness, blurred vision, reduced ability to quickly mental and motor responses (especially at the beginning of treatment); rarely - cerebral ischemia.

Allergic reactions: skin rash.

Dermatological reactions: in some cases, exfoliative dermatitis (severe cases of erythema multiforme exudative, common impetigo and toxicoderma).

Other: development of tolerance (including cross to other nitrates). To prevent the development of tolerance, continuous intake of high doses of the drug should be avoided.

Contraindications

With caution should use the drug for: hypertrophic obstructive cardiomyopathy; constrictive pericarditis; tamponade pericardium; reduced filling pressure of the left ventricle, for example, in acute myocardial infarction (the risk of reducing blood pressure and tachycardia, which can increase ischemia), reducing the function of the left ventricle (left ventricular failure). You should not allow a decrease in systolic blood pressure <90 mm="" hg="" aortic="" and="" or="" mitral="" stenosis="" tendencies="" to="" arterial="" hypotension="" orthostatic="" disturbances="" in="" the="" regulation="" of="" blood="" circulation="" heart="" failure="" with="" low="" left="" ventricular="" filling="" pressure="" glaucoma="" risk="" elevated="" intraocular="" diseases="" accompanied="" by="" an="" increase="" intracranial="" previously="" was="" observed="" only="" iv="" injection="" high="" doses="" nitroglycerin="" incl="" hemorrhagic="" stroke="" recent="" head="" injury="" severe="" anemia="" renal="" liver="" developing="" methemoglobinemia="" p="">

Drug interactions

It is possible to enhance the hypotensive effect while taking it with other vasodilators, antihypertensives, beta-blockers, slow calcium channel blockers, diuretics, ACE inhibitors, antipsychotics (neuroleptics) and tricyclic antidepressants, novocainamide, ethanol, phosphodiestech inhibitors, and tricyclic antidepressants. sildenafil, vardenafil, tadalafil).

The simultaneous use of isosorbide mononitrate with dihydroergotamine can lead to an increase in plasma dihydroergotamine concentration and, thus, increase its antihypertensive effect.

When combined with amiodarone, propranolol, blockers of slow calcium channels (verapamil, nifedipine), an antianginal effect may be enhanced.

Under the influence of beta-adrenomimetics, alpha-blockers (dihydroergotamine), a decrease in the severity of antianginal effect (tachycardia, excessive decrease in blood pressure) is possible.

Barbiturates speed up metabolism and reduce the concentration of isosorbide mononitrate in the blood.

Reduces the effect of vazopressorov.

In combined use with m-anticholinegic (atropine) increases the likelihood of increased intraocular pressure.

Adsorbents, binders and coating agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.

The therapeutic effect of norepinephrine (norepinephrine) is reduced while taking it with nitro compounds.

It must be borne in mind that the drug interactions described above are possible even if the indicated drugs were used shortly before treatment with Effox 20 began.

Pregnancy and Lactation

During pregnancy and during breastfeeding, the drug should be used very carefully, only after a thorough assessment of the benefits and possible risks, since there is not enough experience with its use during these periods.

In experimental animal studies, no damaging effects on the fetus were found.

Special instructions

Effox 20 is not used for the relief of acute attacks of stenocardia and acute myocardial infarction.

During the period of therapy, control of blood pressure and heart rate is necessary.

With prolonged use of Effox 20, tolerance may develop, and therefore it is recommended that after 3-6 weeks of regular use of the drug, a break of 3-5 days be taken, replacing Effox with 20 other antianginal drugs.

When taking Effox 20, temporary hypoxemia is possible due to the relative redistribution of blood flow to the hypoventilated alveolar zones. In patients with coronary artery disease, this can lead to a temporary myocardial hypoxia.

If necessary, the use of the drug Effox 20 on the background of arterial hypotension should be simultaneously administered drugs that have a positive inotropic effect.

With the development of intolerance symptoms are not allowed to re-appointment of the drug.

You can not abruptly stop treatment with Effox 20. It is necessary to cancel the drug gradually to avoid the development of withdrawal syndrome.

During the period of drug treatment should be excluded alcohol.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

During the period of treatment it is not recommended to drive vehicles or engage in other potentially dangerous activities that require rapid psychomotor reactions.

Overdosage

Symptoms: pronounced decrease in blood pressure with orthostatic dysregulation, palpitations, weakness, dizziness, lethargy, headache, skin redness, nausea, vomiting, diarrhea, collapse, syncope, hyperthermia, convulsions, sweating, methemoglobinemia (cyanosis, anoxia, hypochia, seizures, hypoxia, anoxia, hypochidia (hypoxia, anoxia, hypochondria, cramps, sweating, anoxia, anoxia, hypochondria, anoxia, hypochondria, hypochondria, hypertension, cramps, swelling, methohemoglobinemia (cyanosis, anoxic) pressure, paralysis, coma.

Treatment: gastric lavage; in case of a pronounced decrease in blood pressure and / or a state of shock, liquid should be injected; in exceptional cases, norepinephrine and / or dopamine can be infused to improve blood circulation. The 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 by mouth or in the form of sodium salt IV.
methylene blue - up to 50 ml of 1% solution IV.
toluidine blue - first 2–4 mg / kg body weight IV, then, if necessary, repeated administrations of 2 mg / kg body weight are possible with an interval between administrations at 1 hour. 4. oxygen therapy, hemodialysis, exchange blood transfusion.