Isosorbide mononitrate-Teva (Isosorbide mononitrate-Teva)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbsppills
Composition:1 tablet contains: active substance isosorbide mononitrate 40.0 mg (in the form of trituration - isosorbide mononitrate: lactose monohydrate (40:60) 100.0 mg); Excipients: lactose monohydrate 72.0 mg, corn pregelatinized corn starch 53.2 mg, copovidone 8.0 mg, silicon colloidal dioxide 4.8 mg, magnesium stearate 2.0 mg.
Description:Round biconvex tablets of white color. On one side - the risk and engraving "M4".
Pharmacotherapeutic group:Vasodilating agent - nitrate
Pharmacodynamics:

Peripheral vasodilator with predominant effect on venous vessels. Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, which results in an increase in the content of cyclic guanosine monophosphate. The preload and afterload decrease due to the widening of the peripheral veins due to a decrease in the overall peripheral vascular resistance, reducing the need for myocardium in oxygen. Possesses coronary dilatation. Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of circulation and regression of symptoms with pulmonary edema. Increases exercise tolerance in patients with ischemic heart disease (CHD).It dilates the vessels of the brain, the dura mater, which is accompanied by a headache. Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored.

Antianginal effect occurs 30-40 minutes after ingestion and lasts up to 8-12 hours.

Pharmacokinetics:

After oral administration isosorbide mononitrate quickly and completely absorbed from the gastrointestinal tract (GIT). It has absolute bioavailability (about 100%), since there is no effect of "primary passage" through the liver. The release of isosorbide mononitrate does not depend on the time of ingestion, peristalsis or pH in the lumen of the gastrointestinal tract. Isosorbide mononitrate has a large volume of distribution, communication with plasma proteins is less than 4%. Therapeutic concentration (100 ng / ml) is achieved 30 minutes after ingestion. The time to reach the maximum concentration is 1-1.5 hours. Isosorbide mononitrate completely metabolized in the liver with the formation of pharmacologically inactive metabolites.

The half-life of plasma is 4-5 hours. Isosorbide mononitrate is excreted by the kidneys in the form of metabolites, only about 2% are eliminated unchanged.

Indications:

Ischemic heart disease: prevention of attacks of stable angina, including after a previous myocardial infarction.

Chronic heart failure (as part of combination therapy).

Contraindications:Hypersensitivity to isosorbide mononitrate, other nitro compounds and other components of the drug; acute circulatory disturbances (shock, collapse); cardiogenic shock if it is not possible to correct the final diastolic pressure of the left ventricle with intra-aortic counterpulsation or by introducing agents that have a positive inotropic effect; acute heart failure; severe arterial hypotension (systolic blood pressure (BP) less than 90 mm Hg); cerebral hemorrhage, hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, severe hypovolemia, severe aortic and subaortic stenosis, mitral stenosis; lactose intolerance; deficiency of lactase; glucose-galactose malabsorption; simultaneous administration of inhibitors of phosphodiesterase-5, incl.sildenafil, vardenafil, tadalafil, as they potentiate the hypotensive effect of the drug; acute myocardial infarction with severe arterial hypotension; anemia (severe form); toxic pulmonary edema; children under 18 years of age (efficacy and safety not established).
Carefully:With reduced pressure filling the left ventricle, for example, with acute myocardial infarction (risk of lowering blood pressure and tachycardia, which may increase ischemia). Do not lower the systolic blood pressure below 90 mm Hg. Art. with aortic and / or mitral stenosis; propensity to arterial hypotension (orthostatic disorders of blood circulation regulation); at a closed angle glaucoma; diseases accompanied by increased intracranial pressure (previously increased pressure was noted only with intravenous (IV) high doses of nitroglycerin), including hemorrhagic stroke, a recent head trauma; with severe renal failure; if liver function is inadequate (risk of methaemoglobinaemia); hypothyroidism; pregnancy and during breastfeeding; inadequate and malnutrition.
Pregnancy and lactation:

Isosorbide mononitrate-Teva is not recommended for use during pregnancy and during breastfeeding. The use of the drug is possible only according to the prescription of the doctor, after a thorough evaluation of the benefits to the mother and the possible risk to the fetus / child, as there are currently insufficient data on the consequences of its use in pregnant and lactating mothers.

There is evidence that nitrates are excreted in breast milk and can cause methaemoglobinemia in a child. The amount of excretion of isosorbide mononitrate in breast milk was not determined, so caution should be exercised when using the drug during breastfeeding. If a nursing mother still takes Isosorbide mononitrate-Teva, it is necessary to establish observation of the child for the development of possible side effects from the use of the drug.

Dosing and Administration:

Inside, after eating, swallowing whole, without chewing and washing down with a small amount of liquid.

The dose of Isosorbide mononitrate-Teva preparation and the frequency of reception are determined individually depending on the severity of the disease.The initial dose is -1 tablet (40 mg) once a day.

If necessary, the dose may be increased to 60 mg (1 tablet of 40 mg tablets and 2.1 to 40 mg) once a day.

In the case of nocturnal attacks of angina pills should be taken in the evening.

Depending on the severity of the therapeutic effect of the day 3-5 with single therapy dose can be increased to 60-80 mg (in special cases up to 80 mg / day) for the same multiplicity of reception.

The decision on the duration of therapy is taken by a doctor.

Side effects:

The frequency of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely (including individual reports) - less than 0.01%; frequency is unknown - can not be calculated from available data.

From the central nervous system: very often - "nitrate" headache; often - dizziness (including postural), drowsiness, blurred vision, fatigue, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment); rarely - ischemia of the brain.

From the cardiovascular system: infrequently - hyperemia of the skin of the face, a feeling of heat, "hot flashes" of blood to the skin of the face, tachycardia; frequency unknown - marked decrease in blood pressure; rarely - increased attacks of angina pectoris (paradoxical reaction to nitrates), orthostatic collapse. There were cases of collapoid states, sometimes with bradyarrhythmia and syncope.

From the digestive system: infrequently - nausea, vomiting, there may be a feeling of slight burning of the tongue, dryness of the oral mucosa; very rarely - heartburn.

Allergic reactions: infrequently - a skin rash.

Dermatological reactions: very rarely - angioedema, Stevens-Johnson syndrome; frequency is unknown - exfoliative dermatitis (severe cases exudative erythema multiforme, and impetigo commonly toksikodermiya).

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

For organic nitrates cases of pronounced reduction in blood pressure were observed, accompanied by nausea, vomiting, restlessness, pallor of the skin and sweating.

Long-term use of the Isosorbide mononitrate-Teva preparation can cause transient hypoxemia due to the relative redistribution of blood flow to the hypoventilation alveolar areas. This may be the triggering mechanism of ischemia in IHD.

Overdose:

Symptoms: marked reduction in arterial pressure with orthostatic vasodilation, reflex tachycardia and headache. There may appear pallor of the skin, increased sweating, "threadlike" pulse, weakness, dizziness, flushing of the skin, nausea, vomiting, diarrhea. When taking high doses (more than 20 mg / kg), nitrite ions, formed due to the metabolism of isosorbide mononitrate, can cause methemoglobinemia with cyanosis, dyspnea and tachypnea.

When taking very high doses, intracranial pressure may increase with the development of cerebral symptoms.

With a chronic overdose in the blood, you can find an increased content of methemoglobin, the clinical significance of which is controversial.

Treatment: in addition to general measures such as gastric lavage and providing patients with a horizontal position with raised legs,it is necessary in the conditions of the intensive care unit to ensure the observation of the indicators of vital functions and, if necessary, to correct them.

If there is a pronounced decrease in blood pressure and / or shock, the volume of circulating blood should be replenished; in exceptional cases to normalize blood circulation, you can enter norepinephrine (noradrenaline) and / or dopamine. The introduction of epinephrine (adrenaline) and related compounds is contraindicated. Depending on the severity of methemoglobinemia, the following antidotes are recommended:

1. Ascorbic acid: 1 g inside or in the form of the sodium salt in / in 0.1-0.15 ml / kg 1% solution up to 50 ml.

2. Oxygenotherapy, hemodialysis, exchange blood transfusion.

If there is a stoppage of breathing and the heart, resuscitation should be started immediately.

Interaction:

With simultaneous use with other vasodilators, antihypertensive agents, beta-adrenoblock locators, slow calcium channel blockers, diuretics, angiotensin converting enzyme inhibitors, antipsychotics (antipsychotics) and tricyclic antidepressants, procainamide, ethanol, phosphodiesterase-5 inhibitors (v. h. sildenafil, vardenafil, tadalafil) may increase the hypotensive effect. Simultaneous application of isosorbide mononitrate with dihydroergotamine can lead to an increase in the concentration of dihydroergotamine in the blood plasma and, thus, enhance its hypotensive effect.

With simultaneous use with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine), it is possible to increase the antianginal effect.

Under the influence of beta-adrenomimetics, alpha-adrenoblockers (dihydroergotamine and others), it is possible to reduce the antianginal effect (tachycardia, excessive blood pressure decrease).

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

With simultaneous application of isosorbide mononitrate, the effect of vasoconstrictive drugs is reduced.

When used simultaneously with m-holinoblokatorami (atropine) increases the likelihood of increased intraocular pressure.

Absorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate in the digestive tract.

The therapeutic effect of norepinephrine (norepinephrine) decreases with simultaneous intake with nitrocompounds.

Special instructions:

Isosorbide mononitrate-Teva is not used to stop acute attacks of angina and acute myocardial infarction!

During the period of therapy with Isosorbide mononitrate-Teva, control of blood pressure and heart rate is necessary.

With long-term use, the development of tolerance is possible, in connection with which it is recommended after 3-6 weeks of regular intake of the drug to take a break for 3-5 days, replacing the preparation of Isosorbide mononitrate-Teva with other antianginal drugs.

When taking Izosorbid mononitrate-Teva, temporary hypoxemia is possible due to the relative redistribution of blood flow to the hypoventilation alveolar zone. In patients with IHD, this can lead to temporary myocardial hypoxia.

If it is necessary to use Izosorbid mononitrate-Teva preparation against arterial hypotension, drugs with a positive inotropic effect should be used simultaneously.

With the development of symptoms of intolerance, repeated use of the drug is not allowed.

Therapy with isosorbide mononitrate-Teva drug should be discontinued gradually, in order to avoid the development of the "withdrawal" syndrome.

During the treatment with the drug should be excluded from drinking alcohol.

Effect on the ability to drive transp. cf. and fur:When using the Isosorbide mononitrate-Teva preparation, one should refrain from performing actions that require a high concentration of attention and speed of psychomotor reactions, when driving vehicles and working with complex technical devices.
Form release / dosage:
Tablets of 40 mg.
Packaging:For 10 tablets in a blister of PVC / aluminum foil. By 2, 3, 5 or 10 blisters together with instructions for use in a cardboard box.
Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription
Registration number:LP-002405
Date of registration:19.03.2014
Expiration Date:19.03.2019
The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
Manufacturer: & nbsp
Representation: & nbspTeva Teva Israel
Information update date: & nbsp09.11.2017
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