Effox Long, retard pills 50mg, 30pcs

Composition

Active ingredients:

isosorbide mononitrate 50 mg.

Auxiliary substances:

lactose monohydrate,

hydroxypropylmethylcellulose (hypromellose),

calcium hydrophosphate dihydrate,

microcrystalline cellulose,

povidone,

talc,

glyceryl distearate,

magnesium stearate,

highly dispersed silicon dioxide.

Pharmacological action

Pharmacodynamics

Peripheral vasodilator with a predominant effect on venous vessels.

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

Reduces the oxygen demand of the myocardium by reducing preload and afterload (reduces the final diastolic volume of the left ventricle and reduces the systolic tension of its walls). It has a corona-expanding effect.

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

Increases exercise tolerance in patients with coronary artery disease, angina pectoris. Dilates the blood vessels of the brain, dura mater, which can be accompanied by a headache.

As with other nitrates, cross-tolerance develops. After withdrawal (a break in treatment), sensitivity to it is quickly restored.

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

Pharmacokinetics

Suction

When taken orally, the absorption of isosorbide mononitrate is high, the bioavailability is 100%. The time to reach C_max is 8 hours.

Distribution

Binding to plasma proteins is less than 4%.

Metabolism

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

Elimination

of 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 and subsequent treatment of angina after a previous myocardial infarction;
• pulmonary hypertension (as part of combination therapy);
• treatment of chronic heart failure (as part of combination therapy with cardiac glycosides, diuretics, ACE inhibitors).

Contraindications

• Hypersensitivity to the drug, organic nitrates;
• acute disorders of blood circulation (shock, vascular collapse);
• cardiogenic shock, if not possible correction of end-diastolic pressure of the left ventricle using the intra-aortic pump therapy or due to the introduction of funds, providing a positive inotropic effect;
• severe hypotension (systolic blood pressure < 90 mm Hg. St., and diastolic blood pressure < 60 mm Hg. St);
• concomitant use of phosphodiesterase inhibitors, including sildenafil, vardenafil, tadalafil, since they potentiate the hypotensive effect of the drug;
• acute myocardial infarction with severe hypotension;
• traumatic brain injury, bleeding in the brain;
• anemia (severe form);
• hereditary galactose intolerance, lactase deficiency or malabsorption syndrome of glucose and galactose;
• toxic pulmonary edema,
• childhood and adolescence to 18 years (efficacy and safety not established).

With caution, the drug should be used for: hypertrophic obstructive cardiomyopathy; constrictive pericarditis; pericardial tamponade; reduced left ventricular filling pressure, for example, in acute myocardial infarction (risk of lowering blood pressure and tachycardia, which can increase ischemia), decreased left ventricular function (left ventricular failure). Do not allow a decrease in systolic blood pressure

Side effects

From the cardiovascular system: at the beginning of treatment, a headache (“nitrate” headache) may occur, which usually decreases after a few days of therapy; dizziness, flushing of the facial skin, a feeling of heat, tachycardia. Sometimes, when taking the drug for the first time or after increasing the dose, there is a decrease in blood pressure and/or orthostatic hypotension, which can 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. There have been cases of collaptoid states, sometimes with bradyarrhythmia and syncope.

The use of Effox long may lead to transient hypoxemia due to the relative redistribution of blood flow to hypoventilated alveolar segments. This can trigger ischemia in CHD.

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

From the central nervous system: stiffness, drowsiness, blurred vision, decreased ability to react quickly (especially at the beginning of treatment).

Allergic reactions: skin rash.

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

Other: development of tolerance (including cross-tolerance to other nitrates). To prevent the development of tolerance, long-term treatment with the drug in high doses should be avoided. Increasing the dose and / or changing the intervals of use may lead to a decrease or loss of effectiveness.

Interaction

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

Concomitant use of isosorbide mononitrate with dihydroergotamine may lead to an increase in the concentration of dihydroergotamine in blood plasma and, thus, increase its antihypertensive effect.

When combined with amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine), the antianginal effect may be enhanced.

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

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

Reduces the effect of vasopressors.

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

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

The therapeutic effect of norepinephrine (norepinephrine) decreases when taken concomitantly with nitro compounds.

It should be borne in mind that the drug interactions described above are also possible if these drugs were used shortly before treatment with Effox long was started.

How to take, course of use and dosage

Assign inside at a dose of 50 mg 1 time / day. Duration of treatment and repeated courses – on the doctor’s recommendation.

The drug is taken after a meal, without chewing and drinking a small amount of liquid.

Overdose

Symptoms: marked decrease in blood pressure with orthostatic dysregulation, palpitation, weakness, dizziness, lethargy, headache, redness of the skin, nausea, vomiting, diarrhea, collapse, fainting, hyperthermia, convulsions, sweating, methemoglobinemia (cyanosis, anoxia), hyperpnea, dyspnea, increased intracranial pressure, paralysis, coma.

Treatment: gastric lavage; with a marked decrease in blood pressure and/or a state of shock, fluid should be administered; in exceptional cases, infusions of norepinephrine and/or dopamine can be performed to improve blood circulation. use of epinephrine (epinephrine) and related compounds is contraindicated.

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

Special instructions

Effox Long is not used for relief of acute angina attacks.

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

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

If symptoms of intolerance develop, do not re-prescribe the drug.

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

During treatment with the drug, alcohol consumption should be excluded.

Use in pediatrics

To date, there is no experience of using Effox Long in children.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

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

Form of production

Long-acting tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Isosorbide Mononitrate

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Nursing mothers as prescribed by a doctor

Indications

Heart Failure, Angina