Description
Latin name
EFFOX ® LONG
Release form
Sustained-release tablets.
Packing
30 pcs
Pharmacological action
Pharmacodynamics
Peripheral vasodilator with a primary 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 in cGMP (mediator of vasodilation).
Reduces myocardial oxygen demand 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 coronary expansion effect.
Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema. Promotes redistribution of coronary blood flow in the area with reduced blood circulation.
Increases exercise tolerance in patients with coronary artery disease, angina pectoris. Expands the vessels of the brain, dura mater, which may be accompanied by a headache.
As with other nitrates, cross tolerance develops. After cancellation (interruption of treatment), sensitivity to it is quickly restored.
The antianginal effect occurs 30-45 minutes after ingestion and lasts up to 8-10 hours.
Pharmacokinetics
Absorption
When administered, the absorption of isosorbide mononitrate is high, bioavailability is 100%. The time to reach Cmax is 8 hours.
Distribution of
Binding to blood plasma proteins is less than 4%.
Metabolism
Isosorbide mononitrate is almost completely metabolized in the liver to form pharmacologically inactive metabolites.
Excretion of
T1 / 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 pectoris after myocardial infarction
pulmonary hypertension (as part of combination therapy)
treatment of chronic heart failure (as part of combination therapy with cardiac glycosides, diuretics, inhibitor).
Contraindications
Hypersensitivity to the drug, organic nitrates
acute circulatory disorders (shock, vascular collapse)
cardiogenic shock, if it is not possible to correct the final diastolic pressure of the left ventricle using intra-aortic counterpulsation or by administering drugs that have a positive inotropic effect
severe arterial hypotension (systolic blood pressure <90 mmHg and diastolic blood pressure <60 mmHg) phosphodiesterase inhibitors, including sildenafil, vardenafil, tadalafil, because they potentiate the hypotensive effect of the drug acute myocardial infarction with severe arterial hypotension head injury, cerebral hemorrhage anemia (severe form) hereditary galacto intolerance, lactase deficiency or glucose and galactose malabsorption syndrome toxic pulmonary edema children and adolescents under 18 years of age (efficacy and safety not established). With caution, the drug should be used in case of: hypertrophic obstructive cardiomyopathy, constrictive pericarditis, tamponade of the pericardium, decreased pressure of filling the left ventricle, for example, with acute myocardial infarction (risk of lowering blood pressure and tachycardia, which may increase ischemia), decreased left ventricular function (left ventricular). A decrease in systolic blood pressure <90 mmHg should not be allowed. aortic and / or mitral stenosis, a tendency to arterial hypotension (orthostatic circulatory dysregulation) heart failure with low left ventricular filling pressure glaucoma (risk of increased intraocular pressure) diseases accompanied by an increase in intracranial pressure (previously an increase in pressure was noted only with iv high doses nitroglycerin), including with hemorrhagic stroke, recent head trauma, severe renal failure of liver failure (risk of methemoglobinemia). Use during pregnancy and lactation During pregnancy and lactation, administration is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus or infant, since at present there is insufficient data on the consequences of its use in pregnant and lactating mothers. If the nursing mother still takes Efox Long, it is necessary to establish monitoring of the child for the development of possible side effects from the drug. Composition 1 tablet contains: Active substances: isosorbide mononitrate 50 mg. Excipients: lactose monohydrate, hydroxypropyl methylcellulose (hypromellose), calcium hydrogen phosphate dihydrate, microcrystalline cellulose, povidone, talc, glyceryl distearate, magnesium stearate, highly dispersed silicon dioxide. Dosage and administration Assign inside 50 mg once a day. Duration of treatment and repeated courses – on the recommendation of a doctor. The drug is taken after meals, without chewing and drinking with a small amount of liquid. 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 dizziness therapy, hyperemia of the skin of the face, sensation of heat, tachycardia. Sometimes, at the first dose 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 angina attacks (paradoxical reaction to nitrates), orthostatic collapse. There have been cases of collaptoid states, sometimes with bradyarrhythmia and fainting. The use of the Efox Long preparation can lead to transient hypoxemia due to the relative redistribution of blood flow into the hypoventilated alveolar segments. This may be the trigger of ischemia in coronary artery disease. From the digestive system: nausea, vomiting, a sensation of a slight burning sensation of the tongue, dry mouth. From the side of the central nervous system: stiffness, drowsiness, blurred vision, decreased ability to 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 multiforme exudative erythema, common impetigo and toxicoderma). Others: 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 administration may lead to a decrease or loss of effectiveness. Lekarstvennoe Interaction Perhaps Gain hypotensive the effect with simultaneous standard receiving with the second sosudorasshyryayuschymy funds, antihypertensive funds, beta-blockers, blockers medlenn h kaltsyev h channels, diuretics, ACE inhibitors, antipsychotic assets (neuroleptics) and tricyclic antidepressants, novokaynamydom, ethanol, inhibitors fosfodyÑsteraz ( including sildenafil, vardenafil, tadalafil). Concomitant administration of isosorbide mononitrate with dihydroergotamine can increase the concentration of dihydroergotamine in blood plasma and thus enhance its antihypertensive effect. When combined with amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine), an anti-anginal effect may be enhanced. Under the influence of beta-adrenomimetics, alpha-blockers (dihydroergotamine) it is possible to reduce the severity of the anti-anginal effect (tachycardia, excessive reduction of blood pressure). Barbiturates accelerate metabolism and reduce the concentration of isosorbide mononitrate in the blood. Reduces the effect of vasopressors. When combined with m-cholin blockers (atropine), the likelihood of increased intraocular pressure increases. Adsorbents, binders and envelopes reduce the absorption of isosorbide mononitrate in the gastrointestinal tract. The therapeutic effect of norepinephrine (norepinephrine) is reduced when co-administered with nitro compounds. It should be borne in mind that the drug interactions described above are possible even if these drugs were used shortly before Efox Long treatment was started. Overdose Symptoms: marked decrease in BP with orthostatic dysregulation, palpitations, weakness, dizziness, numbness, headache, skin redness, nausea, vomiting, diarrhea, collapse, fainting, hyperthermia, convulsions, sweating, methemoglobinemia (cyanosis, anoxia), hyperpnoea, dyspnoea, intracranial pressure, paralysis. Treatment: gastric lavage with severe BP and / or shock state should be injected with liquid in exceptional cases to improve blood circulation, noradrenaline and / or dopamine can be given. The introduction 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 inside or in the form of sodium salt in / in. methylene blue – up to 50 ml of 1% solution in / in. toluidine blue – 2-4 mg / kg bw / w at first, then, if necessary, repeated injections of 2 mg / kg body weight with an interval between injections of 1 h are possible. 4. Oxygen therapy, hemodialysis, exchange transfusion. Storage conditions Store in a dry place inaccessible to children at a temperature not exceeding 25 ° C. Expiration 5 years. The active substance Isosorbide mononitrate drugstore terms and conditions prescription Dosage form Dosage form tablets prolong. YUSB Pharma SA, Belgium
