Efox 20, tablets 20 mg 50 pcs

An antianginal drug, organic nitrate. Peripheral vasodilator with predominant effect on venous vessels.

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

Limits myocardial oxygen demand by reducing preload and postload (decreases left ventricular end-diastolic volume and reduces systolic wall tension). It has coronary dilator effect.

Limits blood flow to the right atrium, decreases the pressure in the small circle of the circulation and regresses the symptoms of pulmonary edema. Helps redistribute coronary blood flow in the area with reduced blood flow.

Enhances exercise tolerance in patients with coronary artery disease and angina pectoris.

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

As with other nitrates, cross-tolerance develops. After withdrawal (interruption of treatment), sensitivity to it quickly recovers.

The antianginal effect occurs 30-45 min after oral administration and lasts up to 8-10 h.

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Indications

Prevention of angina pectoris attacks in CHD patients, including after myocardial infarction.

Chronic heart failure (as part of combination therapy).

Active ingredient

Composition

1 tablet contains:

Active substances:

Isosorbide mononitrate 20 mg.

Associates:

Lactose monohydrate 151.7 mg,

Talc 7 mg,

Silica colloidal dioxide 3.5 mg,
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Potato starch 27 mg,

Microcrystalline cellulose 33 mg,

Aluminium stearate 2.8 mg.

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How to take, the dosage

The dose of the drug and the frequency of administration are 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 a day. Then the dose should be gradually increased to a therapeutic one – 20-40 mg in 1-2 doses. If necessary, the dose is increased to 60 mg/day. The maximum daily dose is 80 mg. Duration of treatment and repeated courses are based on the doctor’s recommendation.

The tablets should be taken orally after a meal, swallowed whole, without chewing and with plenty of fluids.

Interaction

It is possible to increase the hypotensive effect when concomitant administration with other vasodilators, hypotensive agents, beta-adrenoblockers, slow calcium channel blockers, diuretics, ACE inhibitors, antipsychotics (neuroleptics) and tricyclic antidepressants, novokainamide, ethanol, phosphodiesterase inhibitors (including sildenafil, vardenafil, tadalafil and tadalafil).sildenafil, vardenafil, tadalafil).

The concomitant use of isosorbide mononitrate with dihydroergotamine may increase the plasma concentration of dihydroergotamine and thus enhance its antihypertensive effect.

In combination with amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine) the antianginal effect may be increased.

With the influence of beta-adrenomimetics, alpha-adrenoblockers (dihydroergotamine) a decrease of the antianginal effect (tachycardia, excessive BP reduction) is possible.

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

Decreases the effect of vasopressors.

When combined with m-cholinoblockers (atropine), there is an increased likelihood of increased intraocular pressure.

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

The therapeutic effect of norepinephrine (noradrenaline) is reduced when concomitantly taken with nitro compounds.

Please note that the above drug interactions are also possible if the above drugs were used shortly before treatment with Efox 20 was started.

Special Instructions

Efox 20 is not used to stop acute attacks of angina pectoris and acute myocardial infarction.

A BP and HR should be monitored during therapy.

Long use of Efox 20 may lead to tolerance development; therefore it is recommended to take a 3-5 day break after 3-6 weeks of regular use of the drug, replacing Efox 20 with other antianginal drugs.

When taking Efox 20 temporary hypoxemia is possible due to relative redistribution of blood flow to hypoventilated alveolar zones. In patients with CHD, this may lead to temporary myocardial hypoxia.

If it is necessary to use Efox 20 against a background of arterial hypotension, drugs with a positive inotropic effect should be administered simultaneously.

The drug should not be reapplied if symptoms of intolerance develop.

To stop treatment with Efox 20 abruptly, discontinue it gradually to avoid withdrawal symptoms.

Alcohol should be avoided during treatment with the drug.

Impact on ability to drive vehicles and other mechanisms requiring high concentration

When taking the drug, it is not recommended to drive vehicles or engage in other potentially hazardous activities requiring rapid psychomotor reactions.

Features

Isorbide mononitrate is quickly and completely absorbed from the gastrointestinal tract after oral administration. Bioavailability is 90-100%. Cmax is reached after 30 min and is 100 ng/ml.

Distribution

The binding to plasma proteins is less than 4%.

Metabolism

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

The excretion

T1/2 is about 4-5 hours. Excreted by the kidneys almost exclusively as metabolites, 2% unchanged.

Contraindications

Side effects

Cardiovascular system disorders: at the beginning of treatment, headache (“nitrate” headache) may occur, which usually decreases after a few days of therapy; dizziness, facial hyperemia, fever, tachycardia. Sometimes, when taking the drug for the first time or after increasing the dose, a decrease in BP and/or orthostatic hypotension is observed, which may be accompanied by a reflex increase in HR, lethargy, as well as dizziness and a feeling of weakness. In rare cases, increased angina attacks (paradoxical response to nitrates), orthostatic collapse. There have been cases of collaptoid states, sometimes with bradyarrhythmia and fainting.

The use of Efox 20 may lead to transient hypoxemia due to relative redistribution of blood flow to hypoventilated alveolar segments. This can be a trigger mechanism of ischemia in CHD.

In the digestive system: nausea, vomiting, possibly a mild burning sensation of the tongue, dry mouth.

CNS disorders: stiffness, somnolence, blurred vision, decreased ability to quick mental and motor reactions (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, widespread impetigo and toxicoderma).

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

Overdose

Symptoms: marked BP decrease with orthostatic dysregulation, palpitations, weakness, dizziness, lethargy, headache, flushed skin, nausea, vomiting, diarrhea, collapse, syncope, hyperthermia, seizures, sweating, methemoglobinemia (cyanosis, anoxia), hyperpnea, dyspnea, increased intracranial pressure, paralysis, coma.

Treatment: gastric lavage; if there is a marked decrease in BP and/or a state of shock, fluids should be administered; in exceptional cases, infusions of noradrenaline and/or dopamine may be given to improve blood circulation. Administration of epinephrine (adrenaline) and related compounds is contraindicated.

Depending on the severity, in cases of methemoglobinemia the following antidotes are used:

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