Efoks 20 - instructions for use, dose, side effects, contraindications

active substance: isosorbide mononitrate 20 mg; Excipients: lactose monohydrate 151.7 mg, talc 7.0 mg, silicon dioxide colloid 3.5 mg, potato starch 27.0 mg, cellulose microcrystalline 33.0 mg, aluminum stearate 2.8 mg.

Description:Round tablets of white color, on the one hand - flat with a facet, a notch for the fault and an engraving over the notch "E", under the notch - "20", on the other hand - convex.

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

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 (cGMP) (mediator of vasodilation). The preload and afterload decrease due to the expansion of peripheral veins due to a decrease in the total peripheral vascular resistance, the need for myocardium in oxygen decreases. EFox® 20 has a coronary expansive action. 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. Promotes the redistribution of coronary blood flow in the area with reduced blood circulation and increases exercise tolerance in patients with ischemic heart disease.

Efoks® 20 dilates the vessels of the brain, the dura mater, which can be accompanied by a headache. Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored. The antianginal effect develops 30-45 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics:

Absorption - high, bioavailability - 90 - 100%. The time to reach the maximum concentration in the blood plasma is reached 1 hour after ingestion. The connection with blood plasma proteins is less than 4%. Isosorbide mononitrate almost completely metabolized in the liver.

It is subject to denitrification with the formation of isosorbide, which does not possess pharmacological activity. It is excreted by the kidney almost exclusively in the form of metabolites. Approximately 2% is displayed unchanged. The half-life is 4-5 hours.

Indications:

- Coronary heart disease: prevention of angina attacks, including after a previous myocardial infarction;

- Chronic heart failure (as part of combination therapy).

Contraindications:

- Hypersensitivity to isosorbide mononitrate, other nitro compounds or other components of the drug;

- Acute circulatory disorders (shock, collapse);

- Cardiogenic shock if correction of the end diastolic pressure of the left ventricle by means of intra-aortic counterpulsation or through the introduction of agents that have a positive inotropic effect is not possible;

- Severe arterial hypotension (systolic blood pressure (BP) is below 90 mmHg);

- Simultaneous administration of inhibitors of phosphodiesterase-5, including sildenafil, vardenafil, tadalafil, because they potentiate the antihypertensive effect of the drug;

- Hemorrhage in the brain;

- Severe anemia;

- Hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;

- Hypertrophic obstructive cardiomyopathy;

- Constrictive pericarditis;

- Cardiac tamponade;

- Severe hypovolemia;

- Severe aortic and subaortic stenosis;

- Severe mitral stenosis;

- Age to 18 years (effectiveness and safety not established).

Carefully:

- With reduced pressure filling the left ventricle, for example, acute myocardial infarction (risk of lowering blood pressure and tachycardia,which may increase ischemia), a decrease in the function of the left ventricle (left ventricular failure). Do not lower the systolic blood pressure below 90 mm Hg;

- With aortic and / or mitral stenosis;

- With a tendency to arterial hypotension (orthostatic disorders of blood circulation regulation);

- With angle-closure glaucoma (risk of increased intraocular pressure);

- In diseases accompanied by increased intracranial pressure (increased pressure was noted only with intravenous administration of high doses of nitroglycerin);

- In severe renal failure;

- With severe hepatic insufficiency;

- Pregnancy and the period of breastfeeding;

- Hypothyroidism:

- Inadequate and malnutrition.

Pregnancy and lactation:For safety reasons, Efox® 20 may be used during pregnancy and during breastfeeding only strictly as prescribed by the doctor, after a thorough evaluation of the benefits to the mother and the possible risk to the fetus / child, because there is currently insufficient data on the effects of its use in pregnant and lactating mothers.There are data that nitrates penetrate into breast milk and can cause methemoglobinemia in a child. Excretion of isosorbide mononitrate into breast milk has not been studied, so caution should be exercised when using this medication during breastfeeding. If a nursing mother still takes Efox® 20, stop breastfeeding and monitor the child for possible side effects from the drug.

Dosing and Administration:

Efoks® 20 should be taken orally, without chewing and drinking with a sufficient amount of liquid (for example, one glass of water). Tablets can be divided.

The dosage regimen is determined in accordance with the clinical response of the patient. The lowest effective dose should be given.

It is advisable to start therapy with small doses of the drug: 10 mg (1/2 tablet 20 mg).

Take 1 tablet 1 time, twice a day and then follow the text. The maximum daily dose is 60 mg / day. Patients taking the drug twice a day, the second dose should be taken 8 hours after taking the first. When taken three times a day, the dose is taken every 6 hours.Duration of treatment and repeated courses - on the recommendation of a doctor.

Side effects:

Possible side effects are given below for body systems and frequency of occurrence (classification of the World Organization

Health):

Very often - more than 1/10;

Often - more than 1/100 and less than 1/10;

Infrequently - more than 1/1000 and less than 1/100;

Rarely more than 1/10000 and less than 1/1000;

Very rarely - less than 1/10000;

The frequency is unknown - the frequency can not be estimated from the available data.

Heart Disease

Often: tachycardia;

Infrequent: the paradoxical intensification of angina attacks.

Vascular disorders

Often: orthostatic hypotension;

Infrequently: collapse (accompanied by bradyarrhythmia and syncope);

The frequency is unknown: arterial hypotension (lowering blood pressure).

Disorders from the gastrointestinal tract

Infrequent: nausea, vomiting;

Very rarely: heartburn.

Disturbances from the nervous system

Very often: "nitrate" headache;

Often: dizziness (including postural), drowsiness.

Disturbances from the skin and subcutaneous tissues

Infrequently: skin allergic reactions (including rash), "hot flashes" of blood to the skin of the face;

Very rarely: angioedema, Stevens-Johnson syndrome;

The frequency is unknown: exfoliative dermatitis.

General violations and violations at the site of introduction

Often: asthenia;

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, there have been cases of the development of a marked decrease in blood pressure, accompanied by nausea, vomiting, anxiety, pallor and increased sweating.

Prolonged use of the drug may cause a transient hypoxemia due to a relative redistribution of blood flow to hypoventilation alveolar sites (in patients with coronary heart disease - may lead to myocardial hypoxia).

Overdose:

Symptoms: a marked decrease in blood pressure (systolic blood pressure below 90 mm Hg), reflex tachycardia and headache. There may appear pallor of the skin, increased sweating, "threadlike" pulse, postural dizziness, skin hyperemia, nausea, vomiting, diarrhea.In high doses, you should expect the appearance of methemoglobinemia, cyanosis, tachypnea, dyspnea due to the formation of nitrite ions due to the metabolism of isosorbide mononitrate, there may also be a feeling of anxiety, loss of consciousness and cardiac arrest.

At very high doses of the drug, intracranial pressure may increase with cerebral symptoms.

Treatment:

In light cases: transfer of the patient to the "lying" position with raised legs or the lowered head end of the bed;

In more severe cases: with a pronounced decrease in blood pressure - replenishment of the circulating blood volume (BCC).

In exceptional cases for the improvement of blood circulation, it is possible to carry out infusions of norepinephrine (noradrenaline) and / or dopamine.

The introduction of epinephrine (adrenaline) and related compounds is contraindicated!

With methemoglobinemia:

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

2. Oxygenotherapy, hemodialysis, exchange blood transfusion.

If there is a stop of breathing and heart, immediately begin resuscitative measures.

Interaction:

It is possible to increase the antihypertensive effect with simultaneous reception with other vasodilators, antihypertensive drugs, beta-blockers,blockers of "slow" calcium channels (BCCC), antipsychotic drugs (neuroleptics) and tricyclic antidepressants, procainamide, ethanol, inhibitors of phosphodiesterase-5 (including sildenafil, vardenafil, tadalafil).

Simultaneous application of isosorbide mononitrate with dihydroergotamine can lead to an increase in the concentration of dihydroergotamine in the blood and, thus, increase the hypertensive effect of the latter.

Absorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract. It must be taken into account that the drug interactions described above are also possible if these drugs were used shortly before treatment with Efox® 20 was started. Saprotherin cofactor of nitric oxide synthase. It is advisable to use caution while using sapropterine-containing medications with all vasodilating agents whose action is associated with nitric oxide (N0), including classical NO donors (for example, nitroglycerine, isosorbide dinitrate, isosorbide mononitrate), inhibitors of phosphodiesterase-5 and minoxidil.

Special instructions:

EFox® 20 is not used to stop angina attacks and acute myocardial infarction!

During the therapy, it is necessary to monitor blood pressure and heart rate.

With prolonged use of Efox® 20, tolerance may develop, and therefore it is recommended to cancel for 24-48 hours or for 3-5 days, after 3-6 weeks of regular intake, replacing Efox® 20 with other antianginal agents.

You can not abruptly stop treatment with Efox® 20. This should be done gradually to avoid the undesirable consequences of abrupt cessation of treatment (withdrawal syndrome).

The use of Efox®20 can lead to transient hypoxemia due to the redistribution of blood flow to the hypoventilation alveolar segments. This may be the trigger mechanism of ischemia in patients with coronary heart disease. During the treatment with the drug should be excluded from drinking alcohol.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (risk of drowsiness and headache).

Form release / dosage:

Tablets of 20 mg.

Packaging:For 10 tablets in a blister of polypropylene film and foil polypropylene or in a blister of polypropylene film and aluminum foil.

For 5 blisters together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep the drug 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:П N011548 / 01

Date of registration:24.01.2011

The owner of the registration certificate:YUSB Farma SpAYUSB Farma SpA Italy

Manufacturer: & nbsp

AESICA Pharmaceuticals, GmbH Germany

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp09.04.2014

Illustrated instructions

Instructions

Efoks® 20 (Effox® 20)