Efox long tablet prolong 50 mg pack cont cell/pack card x30

Compound

• Retard tablets

1 tablet

Isosorbide mononitrate – 50 mg

Excipients: lactose 1H2O; methylhydroxypropylcellulose; calcium hydrogen phosphate 2H2O; MCC; polyvidone; talc; highly cyclic partial glyceride; magnesium stearate; highly dispersed silicon dioxide

10 pcs in blister; There are 3 blisters in a cardboard pack.

• Extended release capsules

1 capsule

Isosorbide mononitrate – 50 mg

Excipients: sucrose; corn starch; lactose monohydrate; magnesium hydrosilicate (talc); ethylcellulose; polyethylene glycol (macrogol); hyprolose

Capsule shell: titanium dioxide (E171); iron oxide red (E172); iron oxide black (E172); gelatin

There are 10 pcs in a blister; There are 3 blisters in a cardboard pack.

• Efox 20

Pills

1 tablet

Isosorbide mononitrate – 20 mg

Excipients: lactose monohydrate; talc; colloidal silicon dioxide; potato starch; MCC; aluminum stearate

There are 10 pcs in a blister; There are 5 blisters in a cardboard pack.

Composition and release form

Efox® long

10 pcs in blister; There are 3 blisters in a cardboard pack.

10 pcs in blister; There are 3 blisters in a cardboard pack.

Efox® 20

10 pcs in blister; There are 5 blisters in a cardboard pack.

Description of the dosage form

Efox long, capsules: hard gelatin capsule, size No. 3, cap - brown opaque; the body is pink, opaque.

The contents of the capsules are white or almost white pellets.

Efox long, retard tablets: white or almost white, round, with a bevel and a notch for breaking on one side, odorless. Minor marbling is allowed.

Efox 20: round white tablets, on one side - flat with a chamfer, a notch for breaking and engraving above the notch “E”, under the notch - “20”, on the other side - convex.

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 exercise tolerance in patients with coronary artery disease.

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.

Pharmacological properties

Pharmacodynamics.
Like all organic nitrates, isosorbide mononitrate (ismn) acts as a nitric oxide (NO) donor. no causes relaxation of vascular smooth muscles by stimulating guanylate cyclase and further increasing the concentration of intracellular cGMP. In this way, cGMP-dependent protein kinase is stimulated, as a result of which the phosphorylation of various proteins in vascular smooth muscle cells changes. in turn, this leads to dephosphorylation of myosin light chains and a decrease in myocardial contractility. ISMN causes relaxation of vascular smooth muscles, which determines vasodilation. Dilation of the veins promotes blood deposition and reduces the volume of venous blood that returns to the heart; thus reducing ventricular end-diastolic pressure and volume (preload). The effect on the arteries, and in high doses on the arterioles, leads to a decrease in systemic vascular resistance (afterload). This in turn improves heart function. The effect on both pre- and afterload leads to a decrease in oxygen consumption by the heart muscle.

In addition, ISMN causes a redistribution of blood flow to the subendocardial parts of the heart in conditions of atherosclerotic lesions. This effect may be explained by selective dilatation of large coronary vessels. Nitrate-induced dilatation of collateral arteries may improve myocardial perfusion in vascular stenosis. In addition, nitrates counteract the occurrence and eliminate coronary spasm. In patients with heart failure, which is accompanied by congestion, nitrates improve hemodynamics at rest and during exercise. This beneficial effect occurs through a number of mechanisms, including a decrease in valvular regurgitation (due to decreased left ventricular chamber dilatation) and a decrease in myocardial oxygen consumption. In addition to its effect on the cardiovascular system, ISMN causes relaxation of the muscles of the bronchi, as well as the muscles of the gastrointestinal tract, biliary and urinary tracts.

Pharmacokinetics. ISMN after oral administration is quickly and completely absorbed into the gastrointestinal tract. ISMN does not undergo first-pass metabolism in the liver and is characterized by high systemic bioavailability (relative bioavailability of the drug is 80–90%). Therapeutic concentration is achieved 15–20 minutes after taking the drug. Thanks to the special technology for manufacturing pellets containing ISMN, the release of the drug is carried out in two stages: 30% of the dose is released immediately, and 70% is released slowly, providing Cmax of ISMN in the blood plasma for 5 hours after administration. T½ is 4–5 hours. ISMN is metabolized in the liver with the formation of NO (active metabolite) and isosorbide (inactive) by denitration, and can interact with glucuronic acid. 2% of isosorbide and ISMN unchanged are excreted by the kidneys.

Contraindications

Hypersensitivity to the drug and other 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 (SBP <90 mm Hg and DBP <60 mm Hg, central venous pressure below 4–5 mm Hg), hypovolemia;

Concomitant use of phosphodiesterase inhibitors, incl. sildenafil, vardenafil, tadalafil, since they potentiate the hypotensive effect of the drug;

Traumatic brain injury, cerebral hemorrhage (Efox long);

Acute myocardial infarction with severe arterial hypotension;

Anemia (severe form);

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

Toxic pulmonary edema;

Age up to 18 years (efficacy and safety have not been established).

Carefully:

Hypertrophic obstructive cardiomyopathy (disease of the heart muscle with narrowing of the heart chambers), 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). SBP should not be allowed to fall below 90 mm Hg. Art.

Aortic and/or mitral stenosis;

Tendency to arterial hypotension (orthostatic disorders of blood circulation regulation);

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 intravenous administration of high doses of nitroglycerin), incl. - with hemorrhagic stroke, recent head injury;

Severe renal failure;

Liver failure (risk of developing methemoglobinemia).

Efox long 50 mg 30 pcs. extended release capsules

pharmachologic effect

Vasodilating agent - nitrate.

Composition and release form Efox long 50 mg 30 pcs. extended release capsules

Capsules - 1 capsule:

• active substance: isosorbide mononitrate - 50 mg;
• Excipients: granulated sugar [sucrose (sucrose) 16.34 - 23.92 mg (62.5 - 91.5%), corn starch 2.22 - 9.80 mg (8.5 - 37.5%)] 26.14 mg , lactose monohydrate 13.42 mg, talc 4.64 mg, ethylcellulose 9.20 mg, macrogol 20000 0.26 mg, hyprolose 1.34 mg;
• Composition of the capsule cap: titanium dioxide (E 171) 0.200 mg, red iron oxide dye (E 172) 0.200 mg, black iron oxide dye (E 172) 0.008 mg, gelatin 19.592 mg;
• Composition of the capsule body: titanium dioxide (E 171) 0.450 mg, red iron oxide dye (E 172) 0.060 mg, gelatin 29.490 mg.

10 capsules per blister made of polypropylene film. 3 blisters along with instructions for use are placed in a cardboard box.

Description of the dosage form

Hard gelatin capsule No. 3. The cap of the capsule is opaque brown, the body of the capsule is opaque pink. The capsule contains white or almost white pellets, odorless.

Directions for use and doses

Efox® Long should be taken orally, without chewing and with a sufficient amount of liquid (for example, one glass of water). Take 1 capsule or, if necessary, 2 capsules at a time, once a day in the morning. The dosage regimen is determined according to the patient's clinical response. The lowest effective dose should be taken. The duration of treatment is as recommended by the doctor.

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 the content of cyclic guanosine monophosphate (cGMP) (a mediator of vasodilation). Preload and afterload are reduced due to the expansion of peripheral veins due to a decrease in total peripheral vascular resistance, and the myocardial oxygen demand decreases. 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 exercise tolerance in patients with coronary heart disease.

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 15-30 minutes after oral administration and lasts up to 17 hours.

Pharmacokinetics

Absorption is high, bioavailability is 80 - 90%. Efox® Long contains pellets that provide immediate release of 30% of the dose taken and gradual release of the remaining 70%. The time to reach maximum concentration in blood plasma is 4 - 5 hours. Communication with blood plasma proteins is less than 4%. Isosorbide mononitrate is almost completely metabolized in the liver. The resulting metabolites are pharmacologically inactive. It is excreted by the kidneys almost exclusively in the form of metabolites. Approximately 2% is excreted unchanged. The half-life is 5 - 6 hours.

Indications for use Efox long 50 mg 30 pcs. extended release capsules

Coronary heart disease: prevention of angina attacks, including after 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 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 below 90 mmHg).
• Concomitant use of phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil, as they potentiate the antihypertensive effect of the drug.
• Brain hemorrhage.
• 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 up to 18 years (efficacy and safety have not been established).

Carefully:

• With reduced left ventricular filling pressure, for example, with acute myocardial infarction (risk of low 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.
• For aortic and/or mitral stenosis.
• With a tendency to arterial hypotension (orthostatic disorders of circulatory regulation).
• With angle-closure glaucoma (risk of increased intraocular pressure).
• For diseases accompanied by increased intracranial pressure, including after a recent head injury.
• With severe renal failure.
• In case of liver failure (risk of developing methemoglobinemia).
• Hypothyroidism.
• Insufficient and unhealthy nutrition.

Application of Efox long 50 mg 30 pcs. extended-release capsules during pregnancy and lactation

For safety reasons, Efox® Long can be used during pregnancy and breastfeeding only strictly as prescribed by a doctor, after a careful assessment of the benefits to the mother and the possible risk to the fetus/child, since there is currently insufficient data on the consequences of its use in pregnant and lactating women mothers. There is evidence that nitrates pass into breast milk and can cause methemoglobinemia in the baby. The excretion of isosorbide mononitrate in breast milk has not been studied, so caution should be exercised when using this drug during breastfeeding. If a nursing mother still takes Efox Long, it is necessary to stop breastfeeding and monitor the child for the development of possible side effects from the drug.

special instructions

Efox® Long is not used to relieve attacks of angina pectoris and acute myocardial infarction!

During the therapy period, control of blood pressure and heart rate is necessary. With long-term use of the drug Efox® Long, the development of tolerance is possible, and therefore it is recommended to discontinue it for 24 - 48 hours or after 3-6 weeks of regular use of the drug, take a break for 3-5 days, replacing the use of the drug Efox Long with other antianginal drugs during this time means.

The use of the drug Efox® Long can lead to transient hypoxemia due to the redistribution of blood flow into hypoventilated alveolar segments. This may be a trigger for ischemia in patients with coronary heart disease. During treatment with the drug, alcohol consumption should be avoided. Treatment with Efox® Long should not be interrupted in order to take phosphodiesterase-5 inhibitors.

There is no information on the need to adjust dosage in elderly patients. In patients with slow gastrointestinal motility, a decrease in the release of the active substance may be observed when using extended-release capsules.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: marked decrease in blood pressure with orthostatic vasodilation, reflex tachycardia and headache. Pallor of the skin, increased sweating, “thready” pulse, weakness, dizziness, skin flushing, nausea, vomiting, and diarrhea may appear. In high doses (more than 20 mg/kg body weight), methemoglobinemia, cyanosis, tachypnea, dyspnea due to the formation of nitrithiones due to the metabolism of isosorbide mononitrate should be expected, and feelings of anxiety, loss of consciousness and cardiac arrest may also occur.

At very high doses of the drug, intracranial pressure may increase with cerebral symptoms. In case of chronic overdose, an increase in methemoglobin is detected.

Treatment: if symptoms of overdose appear, you should stop taking the drug, rinse your stomach, and take activated charcoal.

If there is a pronounced decrease in blood pressure and/or a state of shock, place the patient in a horizontal position with raised legs and take measures to replenish the circulating blood volume (CBV); in exceptional cases, infusions of norepinephrine (norepinephrine) and/or dopamine can be administered to improve blood circulation. Administration of epinephrine (adrenaline) and related compounds is contraindicated. For methemoglobinemia:

1. Ascorbic acid -1 g orally or in the form of sodium salt intravenously - 0.1 4 0.15 ml/kg 1% solution up to 50 ml.
2. Oxygen therapy, hemodialysis, exchange transfusion.

If respiratory and cardiac arrest occurs, immediately begin resuscitation measures.

Side effects Efox long 50 mg 30 pcs. extended release capsules

Possible side effects are listed below by body system and frequency of occurrence: 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 rare (less than 1/10000), frequency unknown (frequency cannot be estimated from available data).

Cardiac disorders - often: tachycardia; infrequently: paradoxical increase in angina attacks.

Vascular disorders - Common: orthostatic hypotension; Uncommon: collapse (accompanied by bradyarrhythmia and syncope); Frequency unknown: hypotension.

Gastrointestinal disorders - Uncommon: nausea, vomiting; Very rare: heartburn.

Nervous system disorders - Very common: “nitrate” headache; Common: dizziness (including postural), drowsiness.

Disorders of the skin and subcutaneous tissues - Uncommon: allergic skin reactions (including rash), flushing of the skin; Very rare: angioedema, Stevens-Johnson syndrome; Frequency unknown: exfoliative dermatitis.

General disorders and disorders at the injection site - Common: asthenia; Other: 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.

For organic nitrates, cases of development of a pronounced decrease in blood pressure, accompanied by nausea, vomiting, anxiety, pallor and increased sweating, have been noted.

Long-term use of the drug can cause transient hypoxemia due to the relative redistribution of blood flow to hypoventilated alveolar areas (in patients with coronary heart disease, this can lead to myocardial hypoxia).

Drug interactions

It is possible to enhance the antihypertensive effect when taken simultaneously with other vasodilators, antihypertensive drugs, beta-blockers, blockers of “slow” calcium channels, antipsychotics (neuroleptics) and tricyclic antidepressants, procainamide, ethanol, phosphodiesterase-5 inhibitors, including sildenafil, vardenafil , tadalafil.

The simultaneous use of isosorbide mononitrate with dihydroergotamine may lead to an increase in the concentration of dihydroergotamine in the blood and, thus, enhance the hypertensive effect of the latter.

When used together with amiodarone, propranolol, blockers of “slow” calcium channels (verapamil, nifedipine, etc.), the antianginal effect may be enhanced.

Under the influence of beta-adrenergic agonists, alpha-adrenergic blockers (dihydroergotamine, etc.), 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 used in combination with M-anticholinergics (atropine, etc.), the likelihood of increased intraocular pressure increases.

Absorbents, astringents and coating 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.

Sapropterin (tetrahydrobiopterin, BH4) is a coenzyme of nitric oxide synthetase. Caution is recommended when coadministering sapropterin-containing drugs with any substances that cause vasodilation by affecting nitric oxide (NO) metabolism or action, including classic NO donors (eg, glyceryl trinitrate (GTN), isosorbide dinitrate (ISDN), isosorbide mononitrate and others).

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.

From the gastrointestinal tract: 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). In rare cases, cerebral ischemia.

Allergic reactions: skin rash.

Other: 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. In some cases, exfoliative dermatitis (severe cases of exudative erythema multiforme, widespread impetigo and toxicoderma).

The use of the drug 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 patients with coronary artery disease.

Increasing the dose and/or changing dosing intervals may result in decreased or loss of effectiveness.

Side effects

The frequency of adverse effects can be defined as very common (10%), common (1 to 10%), uncommon (0.1 to 1%), isolated cases (0.01 to 0.1%), and very rare ( 0.01%). When using the drug, the following undesirable effects may occur:

Neurological disorders: very often - headache; often - slight dizziness in an upright position, dizziness, drowsiness.

Cardiac disorders: often - reflex tachycardia; isolated cases - increased symptoms of angina pectoris (paradoxical reaction).

Vascular disorders: often - orthostatic hypotension when standing up; isolated cases - collaptoid states, sometimes with bradycardia and syncope.

From the gastrointestinal tract: infrequently - nausea, vomiting; very rarely - heartburn.

From the skin and subcutaneous tissue: infrequently - allergic skin reactions (for example, rash), hyperemia of the facial skin; isolated cases - exfoliative dermatitis.

General disorders and reactions at the injection site: often - a feeling of weakness. There are reports of severe hypotensive reactions, which were accompanied by nausea, vomiting, anxiety, pallor and increased sweating when using organic nitrates. The use of the drug may cause temporary hypoxemia due to the relative redistribution of blood flow to the alveolar zones with hypoventilation. In persons with coronary artery disease, this can lead to temporary myocardial hypoxia.

With prolonged use of the drug, tolerance may develop (reduced effectiveness), as well as cross-tolerance with other drugs of the nitrate group (reduced effect in the case of previous therapy with another nitrodrug).

Interaction

It is possible to enhance the hypotensive effect when taken simultaneously with other vasodilators, antihypertensives, beta-blockers, CCBs, diuretics, ACE inhibitors, antipsychotics (neuroleptics) and tricyclic antidepressants, procainamide, ethanol, phosphodiesterase inhibitors, incl. 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, CCBs (verapamil, nifedipine, etc.), the antianginal effect may be enhanced.

Under the influence of beta-adrenergic stimulants, alpha-adrenergic blockers (dihydroergotamine, etc.), the severity of the antianginal effect may decrease (tachycardia, excessive decrease in blood pressure).

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

When used in combination with M-anticholinergics (atropine, etc.), 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 the drug was started.

Efox long tablet prolong 50 mg pack cont cell/pack card x30

Trade name: Effox long International name: Isosorbide mononitrate

Release form: extended-release tablets 50 mg (blisters)

Ingredients: isosorbide mononitrate 50 mg

Pharmacological group: vasodilating agent - nitrate

Pharmacological group according to ATK: C01DA14 (Isosorbide mononitrate)

Pharmacological action: antianginal, venodilating, nitrate, antispasmodic,

Indications: Angina pectoris (prevention). CHF, hypertension in the pulmonary circulation, cor pulmonale (treatment as part of combination therapy). Spasm of peripheral arteries (obliterating endarteritis, angiospastic retinitis).

Dosage regimen: Orally (tablets, capsules), 1 hour before or 2 hours after meals. Take the capsules without chewing with a glass of water. The initial dose is 10-20 mg 2 times a day (for drugs with an average duration of action) or 40-50 mg 1 time a day (for retard capsules and depot tablets). Starting from 3-4 days, the dose can be increased to 20-40 mg 2 times a day (for drugs with an average duration of action), increasing the dose if necessary to 60-80 mg/day. The maximum daily dose is 80 mg.

Contraindications: Hypersensitivity.

Side effects: From the cardiovascular system: headache, dizziness, flushing of the facial skin, feeling of heat, tachycardia, decreased blood pressure. In rare cases, increased angina attacks (paradoxical reaction) and collapse. From the digestive system: nausea, vomiting, a slight burning sensation of the tongue, dry mouth. From the nervous system: stiffness, drowsiness, blurred vision, decreased ability for rapid mental and motor reactions (especially at the beginning of treatment). In rare cases, cerebral ischemia. Allergic reactions: skin rash. Other: development of tolerance (including cross-tolerance to other nitrates), exfoliative dermatitis. Overdose. Symptoms: collapse, fainting, headache, dizziness, palpitations, visual disturbances, hyperthermia, convulsions, skin flushing, increased sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia - usually with chronic overdose), hyperpnea, dyspnea, bradycardia , increased intracranial pressure, paralysis, coma. Treatment: gastric lavage, for methemoglobinemia - orally or IV ascorbic acid 1 g, IV 1% solution of methylthioninium chloride 1-2 mg/kg (up to 50 ml), oxygen therapy, hemodialysis, exchange blood transfusion. Symptomatic therapy for a pronounced decrease in blood pressure is IV phenylephrine (epinephrine and related compounds are ineffective).

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 LV EDV and reduces systolic tension of its walls). Has a coronary dilating effect. Reduces blood flow to the right atrium, helps reduce pressure in the “lesser” 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 a break in use, sensitivity to it is quickly restored. The antiangial effect occurs 30-45 minutes after oral administration and lasts up to 8-10 hours.

Pharmacokinetics: Absorption - high, bioavailability - 100%. The time to reach therapeutic concentration (100 ng/ml) is 30 minutes. TCmax - 1-1.5 hours, for retard forms - 8 hours. Communication with plasma proteins - less than 4%. It undergoes denitration to form isosorbide or combines with a glucuronide. T1/2 - 5 hours. Excreted by the kidneys in the form of glucuronides.

Special instructions: During therapy, monitoring of blood pressure and heart rate is necessary. If it is necessary to use the drug against the background of arterial hypotension, drugs that have a positive inotropic effect should be simultaneously administered or circulatory support devices should be used. Frequent administration and high doses can cause the development of tolerance; in this case, it is recommended to discontinue it for 24-48 hours or after 3-6 weeks of regular use, take a break for 3-5 days, replacing isosorbide mononitrate with other antianginal drugs during this time. Abrupt withdrawal of the drug should be avoided (the dose should be reduced gradually). During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Carefully. For all forms (comparing risk and benefit) - hemorrhagic stroke, recent TBI, acute myocardial infarction (risk of decreased blood pressure and tachycardia, which can increase ischemia), glaucoma (risk of increased intraocular pressure), severe anemia, thyrotoxicosis, arterial hypotension with low systolic blood pressure (can aggravate the condition, causing paradoxical bradycardia and angina attacks), HCM (possibly increased frequency of angina attacks), severe renal failure, liver failure (risk of developing methemoglobinemia), pregnancy, lactation, childhood (safety of use has not been established). For prolonged dosage forms for oral administration - increased gastrointestinal motility, malabsorption syndrome. Category of action on the fetus. C

Interaction: Increases plasma concentrations of dihydroergotamine. Reduces the effect of vasopressors. Barbiturates speed up metabolism and reduce the concentration of isosorbide mononitrate in the blood. When isosorbide mononitrate is used together with antihypertensive drugs, vasodilators, antipsychotic drugs (neuroleptics), tricyclic antidepressants, procainamide, ethanol, quinidine, beta-blockers, BMCC, dihydroergotamine and sildenafil, the hypotensive effect may be enhanced. When combined with amiodarone, propranolol, BMCC (verapamil, nifedipine, etc.), the antianginal effect may be enhanced. Under the influence of beta-adrenergic stimulants, alpha-adrenergic blockers (dihydroergotamine, etc.), the severity of the antianginal effect (tachycardia and excessive decrease in blood pressure) may be reduced. When used in combination with m-anticholinergics (atropine, etc.), the likelihood of increased intraocular pressure increases. Adsorbents, astringents and enveloping drugs reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.

Drug registration number: P No. 013274/01

Date of registration (re-registration) of the drug: December 29, 2006

Directions for use and doses

Orally, after eating, without chewing, with a small amount of liquid (for example, 1 glass of water).

Efox long

1 table each retard or 1 caps. Efox long (50 mg) once a day.

Efox 20

The dose of the drug and the frequency of administration are determined individually depending on the severity of the disease. It is advisable to start therapy with small doses of the drug: 1/2 tablet. (10 mg) Efox 20 2 times a day. Then gradually increase the dose to the therapeutic dose: 1–2 tablets. (20–40 mg) in 1–2 doses. If necessary, the dose is increased to 3 tablets. (60 mg) per day. The maximum daily dose is 80 mg. The duration of treatment and repeated courses are on the recommendation of a doctor.

Note!

Description of the drug Efox Long caps. 50mg No. 30 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

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% solution of methylene blue intravenously;

toluidine blue: first 2–4 mg/kg body weight strictly intravenously; then, if necessary, repeated administrations of 2 mg/kg body weight are possible with an interval of 1 hour between administrations;

Oxygen therapy, hemodialysis, exchange transfusion.

special instructions

During therapy, monitoring of blood pressure and heart rate is necessary.

With long-term use, tolerance may develop, and therefore it is recommended that after 3–6 weeks of regular use of the drug, take a break for 3–5 days, replacing it with other antianginal drugs during this time. If necessary, the drug should be used against the background of arterial hypotension, while simultaneously administering agents that have a positive inotropic effect.

If you become intolerant to the drug, do not take it again.

Do not suddenly stop treatment with the drug. This must be done gradually to avoid the undesirable consequences of abruptly stopping treatment (withdrawal syndrome).

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

There is still no experience in treating children with this drug.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.