Efox Long, 50 mg 30 pcs.

Pharmacodynamics

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 an 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 tolerance to physical activity in patients with coronary artery disease and stenocardia. It dilates the blood 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.

Pharmacokinetics

Absorption

When taken orally absorption of isosorbide mononitrate is high, bioavailability is 100%. Time to reach Cmax – 8 hours.

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

Indications

Prevention of angina attacks and subsequent treatment of angina after 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).

Pharmacological effect

Pharmacodynamics

Peripheral vasodilator with a 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, resulting in an increase in cGMP (a mediator of vasodilation).

Reduces myocardial oxygen demand by reducing preload and afterload (reduces the end-diastolic volume of the left ventricle and reduces the systolic tension of its walls). Has a coronary dilating effect.

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

Increases tolerance to physical activity in patients with coronary heart disease and angina pectoris. Dilates blood vessels in the brain and dura mater, which may be accompanied by headaches.

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

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

Pharmacokinetics

Suction

When taken orally, the absorption of isosorbide mononitrate is high, bioavailability is 100%. Time to reach Cmax – 8 hours.

Distribution

Binding to blood plasma proteins is less than 4%.

Metabolism

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

Removal

T1/2 is about 4-5 hours. It is excreted by the kidneys almost exclusively in the form of metabolites, 2% – unchanged.

Special instructions

Efox Long is not used to relieve acute attacks of angina.

With long-term use of Efox Long, the development of tolerance is possible, and therefore it is recommended that after 3-6 weeks of regular use of the drug, take a break for 3-5 days, replacing Efox Long with other antianginal drugs.

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

If symptoms of intolerance develop, re-prescribing the drug is not allowed.

You should not abruptly stop treatment with Efox Long. It is necessary to discontinue the drug gradually to avoid the development of withdrawal syndrome.

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

Use in pediatrics

To date, there is no experience with the use of the drug Efox Long in children.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

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

Active ingredient

Isosorbide mononitrate

Composition

Active ingredients:

isosorbide mononitrate 50 mg.

Excipients:

pellets (sugar balls containing sucrose (sucrose), corn starch),

lactose monohydrate,

talc,

ethylcellulose,

polyethylene glycol (macrogol),

hyprolose.

Shell composition:

titanium dioxide (E171), red iron oxide (E172), black iron oxide, gelatin.

Pregnancy

During pregnancy and lactation, prescription is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus or infant, since there is currently insufficient data on the consequences of its use in pregnant and lactating mothers.

If a nursing mother still takes Efox Long, it is necessary to monitor the child for the development of possible side effects from the drug.

Contraindications

Hypersensitivity to the drug, organic nitrates;
acute circulatory disorders (shock, vascular collapse);
cardiogenic shock, if it is impossible to correct the end-diastolic pressure of the left ventricle using intra-aortic counterpulsation or through the administration of agents that have a positive inotropic effect;
severe arterial hypotension (systolic blood pressure < 90 mm Hg, and diastolic blood pressure < 60 mm Hg); simultaneous use of phosphodiesterase inhibitors, incl. sildenafil, vardenafil, tadalafil, since they potentiate the hypotensive effect of the drug; acute myocardial infarction with severe arterial hypotension; traumatic brain injury, cerebral hemorrhage; anemia (severe form); hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome; toxic pulmonary edema; children and adolescents under 18 years of age (efficacy and safety have not been established).

The drug should be used with caution for: hypertrophic obstructive cardiomyopathy; constrictive pericarditis; pericardial tamponade; reduced left ventricular filling pressure, for example, in acute myocardial infarction (risk of decreased blood pressure and tachycardia, which can increase ischemia), decreased left ventricular function (left ventricular failure). Systolic blood pressure should not be allowed to fall below 90 mmHg; aortic and/or mitral stenosis; tendency to arterial hypotension (orthostatic dysregulation of blood circulation); heart failure with low left ventricular filling pressure; glaucoma (risk of increased intraocular pressure); diseases accompanied by increased intracranial pressure (previously, increased pressure was noted only with the intravenous administration of high doses of nitroglycerin), incl. with hemorrhagic stroke, recent head injury; severe renal failure; liver failure (risk of developing methemoglobinemia).

Side Effects

From the cardiovascular system: at the beginning of treatment, a headache (“nitrate” headache) may occur, which, as a rule, decreases after a few days of therapy; dizziness, facial flushing, feeling of heat, tachycardia. Sometimes, when first taking the drug or after increasing the dose, a decrease in blood pressure and/or orthostatic hypotension is observed, 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 attacks of angina (paradoxical reaction to nitrates), orthostatic collapse. There have been cases of collaptoid states, sometimes with bradyarrhythmia and fainting.

The use of the drug Efox Long can lead to transient hypoxemia due to the relative redistribution of blood flow into hypoventilated alveolar segments. This may be a trigger for ischemia in coronary artery disease.

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

From the side of the central nervous system: stiffness, drowsiness, blurred vision, decreased ability for rapid mental and motor reactions (especially at the beginning of treatment).

Allergic reactions: skin rash.

Dermatological reactions: in some cases – exfoliative dermatitis (severe cases of exudative erythema multiforme, widespread 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 dosing intervals may result in decreased or loss of effectiveness.

Interaction

The hypotensive effect may be enhanced when taken simultaneously with other vasodilators, antihypertensive drugs, beta-blockers, slow calcium channel blockers, diuretics, ACE inhibitors, antipsychotics (neuroleptics) and tricyclic antidepressants, procainamide, ethanol, phosphodiesterase inhibitors (including sildenafil, vardenafil, tadalafil).

Concomitant use of isosorbide mononitrate with dihydroergotamine may increase the plasma concentration of dihydroergotamine and thus enhance 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-adrenergic agonists, alpha-adrenergic blockers (dihydroergotamine), the severity of the antianginal effect (tachycardia, excessive decrease in blood pressure) may be reduced.

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

Reduces the effect of vasopressors.

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

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

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

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 Long was started.

Overdose

Symptoms: marked decrease in blood pressure with orthostatic dysregulation, palpitations, 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; in case of a marked decrease in blood pressure and/or a state of shock, fluids should be administered; in exceptional cases, infusions of norepinephrine and/or dopamine can be performed to improve blood circulation. Administration 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 orally or in the form of sodium salt intravenously.
methylene blue – up to 50 ml of 1% IV solution.
toluidine blue – first 2-4 mg/kg body weight intravenously, then, if necessary, repeated administrations of 2 mg/kg body weight are possible with an interval of 1 hour between administrations. 4. oxygen therapy, hemodialysis, exchange blood transfusion.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

5 years

Manufacturer

Eisika Pharmaceuticals GmbH, Germany