Efox Long
Efox Long: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Effox long
ATX code: C01DA14
Active ingredient: isosorbide mononitrate (Isosorbide mononitrate)
Producer: Aesica Pharmaceuticals GmbH (Germany)
Description and photo updated: 2020-30-04
Prices in pharmacies: from 199 rubles.
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Efox Long is a vasodilating drug.
Release form and composition
Efoksa long dosage forms:
- prolonged-release tablets: white or almost white, round, convex on one side, on the other side there is a chamfer and risk (10 pcs. in blisters made of polypropylene film, in a cardboard box 3 blisters together with instructions for use of the drug);
- Sustained-release capsules: gelatinous, hard, opaque, size No. 3, body - pink, cap - brown; the contents of the capsules are white or almost white, odorless pellets (10 pcs. in blisters made of polypropylene film, 3 blisters in a cardboard box and instructions for use of Efoksa Long).
1 tablet contains:
- active substance: isosorbide mononitrate - 50 mg;
- auxiliary components: lactose monohydrate, microcrystalline cellulose, hypromellose, glyceryl distearate, povidone, calcium hydrogen phosphate dihydrate, colloidal anhydrous silicon dioxide, magnesium stearate, talc.
1 capsule contains:
- active substance: isosorbide mononitrate - 50 mg;
- auxiliary components: sugar grits [sucrose (sucrose), corn starch], talc, macrogol 20,000, lactose monohydrate, ethyl cellulose, hyprolose;
- capsule cap and body: gelatin, titanium dioxide, iron oxide red; additionally for the capsule cap - iron oxide black dye.
Pharmacological properties
Pharmacodynamics
Efox Long is a vasodilating drug. Its active ingredient, isosorbide mononitrate (nitrate), is a peripheral vasodilator that affects mainly the venous vessels. By stimulating the formation of nitric oxide (an endothelial relaxing factor) in the vascular endothelium, it promotes the activation of intracellular guanylate cyclase, and, as a result, an increase in the content of cyclic guanosine monophosphate (cGMP) (a mediator of vasodilation).
Reducing the total peripheral vascular resistance, it causes the expansion of peripheral veins, which leads to a decrease in pre- and afterload, a decrease in myocardial oxygen demand.
It has a coronary dilating effect, reduces blood flow to the right atrium. Promotes a decrease in pressure in the pulmonary circulation, redistribution of coronary blood flow in the area with reduced blood circulation, regression of symptoms in pulmonary edema.
In patients with ischemic heart disease while taking isosorbide mononitrate, exercise tolerance increases.
When taken orally, the antianginal effect of Efoks Long occurs after 1 / 4–1 / 2 hours, its duration is up to 8–12 hours (after taking extended-release tablets) or up to 17 hours (after taking extended-release capsules).
Taking the drug may be accompanied by a headache caused by the expansion of the vessels of the brain and dura mater. Efox Long is a nitrate drug, so cross-tolerance develops to it. To quickly restore sensitivity to the active substance, it is recommended to take a regular break in treatment.
Pharmacokinetics
The degree of absorption of isosorbide mononitrate after oral administration is high. Bioavailability is 80–90%. The maximum concentration in blood plasma is reached within 5 hours.
Plasma protein binding is less than 4%.
It should be borne in mind that nitrates pass into breast milk, causing the risk of developing methemoglobinemia in a child.
The substance is metabolized in the liver almost completely. As a result of denitration, isosorbide is formed, which has no pharmacological activity.
The half-life when taking Efox Long in the form of tablets is 4-5 hours, in the form of capsules - 5-6 hours. It is excreted through the kidneys almost completely in the form of metabolites, only about 2% of the dose taken is excreted unchanged.
Indications for use
- chronic heart failure - as part of combination therapy;
- prevention of angina attacks in ischemic heart disease or after myocardial infarction.
Contraindications
Absolute:
- cerebral hemorrhage;
- acute circulatory disorders (shock, collapse);
- cardiogenic shock - only in cases where the end diastolic pressure of the left ventricle cannot be corrected by introducing agents that have a positive inotropic effect, or by using intra-aortic counterpulsation;
- severe arterial hypotension - systolic (upper) blood pressure (BP) below 90 mm Hg (Hg);
- hypertrophic obstructive cardiomyopathy;
- constrictive pericarditis;
- severe stage of mitral, aortic and subaortic stenosis;
- cardiac tamponade;
- severe anemia;
- severe hypovolemia;
- concomitant therapy with phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil;
- syndrome of glucose-galactose malabsorption, lactase deficiency or hereditary lactose intolerance;
- breast-feeding;
- age up to 18 years;
- established hypersensitivity to nitrate compounds;
- individual intolerance to the components of the drug.
Efox Long 50 mg tablets and capsules should be used with caution in case of aortic and / or mitral stenosis, reduced left ventricular filling pressure (including acute myocardial infarction, left ventricular failure), a tendency to arterial hypotension (orthostatic circulatory disorders), angle-closure glaucoma, pronounced renal insufficiency, hepatic failure, hypothyroidism, malnutrition and malnutrition of the patient; for diseases accompanied by an increase in intracranial pressure (including a condition after a recent head injury); during pregnancy.
Efoks long, instructions for use: method and dosage
Efox Long capsules and tablets are taken orally, swallowed whole and washed down with a sufficient amount of water or other liquid.
The tablets cannot be divided or chewed!
The dose and duration of treatment is determined by the attending physician, taking into account clinical indications.
Recommended dosage for tablets and capsules: 1–2 pcs. Once a day, in the morning.
The smallest effective dose of Efoks Long should be taken.
Side effects
The adverse reactions listed below are classified according to the following scale 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 1/10 000 and less than 1/1000; very rarely - less than 1/10 000; frequency not established - it is not possible to estimate the frequency from the available data.
Possible side effects when taking Efox Long:
- from the heart: often - tachycardia; infrequently - a paradoxical increase in angina attacks;
- from the side of the vessels: often - orthostatic hypotension; infrequently - collapse, accompanied by bradyarrhythmia and fainting; frequency not established - hypotension;
- from the gastrointestinal tract: infrequently - nausea, vomiting; very rarely - heartburn;
- from the nervous system: very often - nitrate headache; often - drowsiness, dizziness (including postural);
- from the skin and subcutaneous tissues: infrequently - allergic reactions (including rash), flushing of the skin of the face; very rarely - Stevens-Johnson syndrome, angioedema; frequency not established - exfoliative dermatitis;
- general disorders: often - asthenia;
- others: with continuous intake of high doses of Efoksa Long - the development of tolerance (including cross-tolerance to other nitrates); the frequency has not been established - a marked decrease in blood pressure (BP), accompanied by increased sweating, nausea, vomiting, pallor and anxiety; with prolonged use of the drug - transient hypoxemia (with ischemic heart disease can lead to myocardial hypoxia).
Overdose
Symptoms: headache, weakness, dizziness, pallor of the skin, increased sweating, a pronounced decrease in blood pressure with orthostatic vasodilation, reflex tachycardia, threadlike pulse, nausea, vomiting, diarrhea, skin flushing. An overdose of more than 20 mg per 1 kg of body weight can cause methemoglobinemia, cyanosis, tachypnea, dyspnea, anxiety, loss of consciousness, and cardiac arrest.
While taking very high doses of Efox Long, an increase in intracranial pressure with cerebral symptoms should be expected.
Chronic overdose is accompanied by an increase in methemoglobin.
Treatment: immediate gastric lavage, intake of activated charcoal. With a significant decrease in blood pressure and / or a state of shock, it is necessary to give the patient's body a horizontal position with raised legs. It is shown that measures are taken to replenish the volume of circulating blood. In order to improve blood circulation in exceptional cases, it is allowed to prescribe norepinephrine (norepinephrine) and / or dopamine in the form of infusion. The administration of epinephrine, epinephrine and related compounds is contraindicated. With methemoglobinemia, ascorbic acid (1000 mg orally or in the form of sodium salt intravenously), hemodialysis, oxygen therapy, exchange blood transfusion are prescribed.
In case of respiratory arrest and cardiac arrest, appropriate resuscitation measures must be taken immediately.
special instructions
Efoks Long cannot be prescribed for the relief of acute myocardial infarction and angina attacks! It is impossible to allow a decrease in blood pressure below 90 mm Hg. Art.
Treatment is recommended to be accompanied by regular monitoring of blood pressure and heart rate.
In order to prevent the development of tolerance to the drug with long-term treatment, it is recommended to take a break for 3-5 days after every 21–42 days of regular intake of tablets / capsules, taking other antianginal drugs during this period.
It should be borne in mind that while taking Efoks Long, there is a risk of developing transient hypoxemia. In ischemic heart disease, this can cause ischemia.
The use of alcohol and ethanol-containing drugs during the period of drug therapy is contraindicated.
The use of tablets / capsules of prolonged action with delayed peristalsis of the organs of the gastrointestinal tract may be accompanied by a decrease in the rate of release of the active substance.
Influence on the ability to drive vehicles and complex mechanisms
During the entire period of treatment with Efox Long, patients should refuse to perform all potentially hazardous activities that require an increased concentration of attention and high speed of psychomotor reactions, including driving and complex mechanisms.
Application during pregnancy and lactation
The use of Efox Long capsules and tablets during breastfeeding is contraindicated. If it is necessary to take isosorbide mononitrate during lactation, breastfeeding should be stopped.
The appointment of Efoksa Long during pregnancy is allowed only in special cases, after a thorough assessment by specialists for the ratio of the expected therapeutic effect for the mother and the possible risk for the fetus.
Pediatric use
The appointment of Efoksa Long is contraindicated for the treatment of children under the age of 18 years due to the lack of data on the effectiveness and safety of its use in this category of patients.
With impaired renal function
It is recommended to use Efox Long with caution in patients with severe renal failure.
For violations of liver function
It is recommended to use Efox Long with caution in patients with hepatic insufficiency.
Use in the elderly
Elderly patients do not need dose adjustment.
Drug interactions
- vasodilators, antihypertensive drugs, beta-blockers, slow calcium channel blockers, antipsychotics, tricyclic antidepressants, procainamide, ethanol, phosphodiesterase-5 inhibitors (including sildenafil, vardenafil, tadalafil): concomitant therapy with each of the listed antigens;
- dihydroergotamine: enhances its hypertensive effect;
- verapamil, nifedipine and other blockers of slow calcium channels, amiodarone, propranolol: the combination with these drugs enhances the antianginal effect;
- beta-adrenergic agonists, alpha-blockers (including dihydroergotamine): due to the interaction of isosorbide mononitrate with these substances, a decrease in the severity of the antianginal effect (tachycardia, marked decrease in blood pressure) is possible;
- barbiturates: help to accelerate metabolism, reduce the concentration of isosorbide mononitrate in the blood and the effect of vasopressors;
- atropine and other m-anticholinergics: increase the risk of increased intraocular pressure;
- astringent and coating agents, absorbents: help to reduce the absorption of isosorbide mononitrate in the gastrointestinal tract;
- norepinephrine (norepinephrine): its therapeutic effect decreases;
- preparations containing sapropterin (tetrahydrobiopterin): care should be taken when combining isosorbide mononitrate with these drugs.
Analogs
The analogues of Efoks long are Isosorbide mononitrate, Efoks 20, Monizol, Mono Rom retard, Mono Mac, Monolong, Monosan, Monocinque retard, Monocinque, Olikard 40 retard, Olikard 60 retard, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from moisture.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Efox Long
Reviews about Efox Long are mostly positive.
Price for Efox Long in pharmacies
The price of Efox Long for a package containing 30 extended-release tablets can be 276–425 rubles. The cost of capsules of prolonged action Efox Long 50 mg varies in the range of 280-460 rubles.
Efox long: prices in online pharmacies
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Drug name Price Pharmacy |
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Efox long 50 mg capsules of prolonged action 30 pcs. 199 RUB Buy |
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Efox long 50 mg extended-release tablets 30 pcs. 221 r Buy |
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Efoks Long tablets of prolonged action 50mg 30 pcs. 259 r Buy |
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Efox Long capsules prolonged action 50mg 30 pcs. 275 RUB Buy |
Elena Minkina Doctor anesthesiologist-resuscitator About the author
Education: graduated from the Tashkent State Medical Institute, specializing in general medicine in 1991. Repeatedly passed refresher courses.
Work experience: anesthesiologist-resuscitator of the city maternity complex, resuscitator of the hemodialysis department.
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
