Efox Long - instructions for use, dose, side effects, contraindications

Excipients: sugar granules [sucrose (sucrose) 16.34 - 23.92 mg (62.5-1 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, ethyl cellulose 9.20 mg, macrogol 20000 0.26 mg, giprolose 1.34 mg. Composition of cap capsule: titanium dioxide (E 171) 0.200 mg, iron oxide red (E 172) 0.200 mg, ferric oxide black oxide (E 172) 0.008 mg, gelatin 19.592 mg. Capsule body composition: titanium dioxide (E 171) 0.450 mg, iron dye red oxide (E 172) 0.060 mg, gelatin 29.490 mg.

Description:Hard gelatin capsule No. 3. The cap of the capsule is opaque brown, the capsule case is opaque pink in color. The capsule contains pellets of white or almost white color, odorless.

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 overall peripheral vascular resistance, the need for myocardium in oxygen decreases. It has 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 redistribution of coronary blood flow in the area with reduced blood circulation. Increases tolerance to physical activity in patients with coronary heart disease.

It 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. Antianginal effect occurs through 15-30 minutes after ingestion and lasts up to 17 hours.

Pharmacokinetics:Absorption is high, bioavailability is 80 - 90%. EFox® Long contains pellets that provide an immediate release of 30% of the dose and a gradual release of the remaining 70%.Time to reach the maximum concentration in blood plasma 4 - 5 hours. The connection with blood plasma proteins is less than 4%. Isosorbide mononitrate almost completely metabolized in the liver. The metabolites formed are pharmacologically inactive. It is excreted by the kidney almost exclusively in the form of metabolites. Approximately 2% is displayed unchanged. The half-life is 5-6 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 it is impossible to correct the final diastolic pressure of the left ventricle with intra-aortic counterpulsation or through the introduction of agents that have a positive inotropic effect.

- Severe arterial hypotension (systolic blood pressure is lower than 90 mm Pg.).

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

- Hemorrhage in the brain.

- Severe anemia.

- Hereditary intolerance of lactose, fructose or insufficiency of sucrose isomaltase; deficiency of lactase 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 left ventricular filling pressure, for example, with acute myocardial infarction (the risk of lowering blood pressure and tachycardia, which may increase ischemia), lowering 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, including after a recent head injury.

- With severe renal failure.

- With hepatic insufficiency (risk of development of methemoglobinemia).

- Hypothyroidism.

- Inadequate and malnutrition.

Pregnancy and lactation:

For safety reasons, Efox® Long 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, as there is currently insufficient data on the effects of its use in pregnant and lactating women mothers. There are data that nitrates penetrate into breast milk and can cause methemoglobinemia in a child. Excretion of isosorbide mononitrate in breast milk has not been studied, so caution should be exercised when using this medication during breastfeeding. If the nursing mother still takes Efox® long, stop breastfeeding and monitor the child for possible side effects from the drug.

Dosing and Administration:Efox® long should be taken orally, without chewing and washing down with a sufficient amount of liquid (for example, one glass of water). Take 1 capsule or 2 capsules at a time, once a day in the morning. The dosage regimen is determined in accordance with the clinical response of the patient. The lowest effective dose should be taken. Duration of treatment - on the recommendation of a doctor.

Side effects:

Possible side effects are given below for body systems 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 rarely (less than 1/10000), the frequency is unknown (the frequency can not be estimated from 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

Infrequent: 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 transient hypoxemia due to the relative redistribution of blood flow to hypoventilation alveolar sites (in patients with coronary heart disease - may lead to myocardial hypoxia).

Overdose:

Symptoms: marked reduction in arterial pressure with orthostatic vasodilation, reflex tachycardia and headache.There may appear pallor of the skin, increased sweating, "threadlike" pulse, weakness, dizziness, skin flushing, nausea, vomiting, diarrhea. In high doses (more than 20 mg / kg body weight), the appearance of methemoglobinemia, cyanosis, tachypnea, dyspnoea due to the formation of nitrite ions due to the metabolism of isosorbide mononitrate, it is also possible the appearance of anxiety, loss of consciousness and cardiac arrest.

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

Treatment: if you have symptoms of an overdose, you must stop taking the medication, rinse your stomach, take Activated carbon.

If there is a pronounced decrease in blood pressure and / or a shock condition, give the patient a horizontal position with raised legs and take measures to replenish the volume of circulating blood (BCC); in exceptional cases, to improve 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 intensify the antihypertensive effect with simultaneous administration with other vasodilators, antihypertensive drugs, beta-blockers, slow calcium channel blockers, antipsychotic drugs (antipsychotics) and tricyclic antidepressants, procainamide, ethanol, phosphodiesterase-5 inhibitors, 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.

When combined with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect.

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

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

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

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

The therapeutic effect of norepinephrine (norepinephrine) decreases with simultaneous intake with nitrocompounds.

It should be taken into account that the drug interactions described above are also possible if these drugs were used shortly before the treatment with Efox® long was started.

Sapropterin is a coenzyme of nitric oxide synthetase. It is advisable to use caution while using sapropterine-containing medications with all vasodilating agents that are associated with nitric oxide (N0), including classic donors N0 (for example, nitroglycerine, isosorbide dinitrate, isosorbide mononitrate, sodium nitroprusside, molsidomine) and others.

Special instructions:

Efox® long is not used to stop angina attacks and acute myocardial infarction!

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

The use of the drug Efox® long can lead to transient hypoxemia due to the redistribution of blood flow to the hypoventicular 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. Do not interrupt treatment with Efox® long to take phosphodiesterase-5 inhibitors.

Information on the need for dosage adjustment in elderly patients is lacking. In patients with delayed peristalsis of the gastrointestinal tract, a decreaserelease of the active substance with the use of prolonged-action capsules.

Effect on the ability to drive transp. cf. and fur:During the treatment period, 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.

Form release / dosage:Capsules of prolonged action of 50 mg.

Packaging:10 capsules per blister of polypropylene film. For 3 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:In a dry place, 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:P N 013274/02

Date of registration:29.12.2011

The owner of the registration certificate:YUSB Pharma GmbHYUSB Pharma GmbH Germany

Manufacturer: & nbsp

AESICA Pharmaceuticals, GmbH Germany

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp29.12.2011

Illustrated instructions

Instructions

Efox® long (Effox® long)