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 C_max is 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 excretion

T_1/2 is about 4-5 hours. It is excreted by the kidneys almost exclusively as metabolites, 2% unchanged.

Indications

Heart failure, Dyspnea, Angina pectoris, Cardialgia (heart pain), Edema

• Prevention of angina attacks and subsequent treatment of angina after myocardial infarction

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• pulmonary hypertension (as part of combined therapy);
• treatment of chronic heart failure (as part of combined therapy with cardiac glycosides, diuretics, ACE inhibitors).

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Active ingredient

Isosorbide mononitrate

Composition

Active substances:

Isosorbide mononitrate 50 mg.

Auxiliary substances:

lactose monohydrate,

hydroxypropyl methylcellulose (hypromellose),

calcium hydrophosphate dihydrate,

Microcrystalline cellulose,

povidone,

talk,

glyceryl distearate,

Magnesium stearate,

High dispersed silicon dioxide.

How to take, the dosage

Appoint orally in a dose of 50 mg once a day. Duration of treatment and repeated courses are according to the doctor’s recommendation.

The drug is taken after a meal, without chewing and with small amounts of liquid.

Interaction

It is possible to increase the hypotensive effect when concomitant administration with other vasodilators, hypotensive agents, beta-adrenoblockers, slow calcium channel blockers, diuretics, ACE inhibitors, antipsychotics (neuroleptics) and tricyclic antidepressants, novokainamide, ethanol, phosphodiesterase inhibitors (including sildenafil, vardenafil, tadalafil and tadalafil).sildenafil, vardenafil, tadalafil).

The concomitant use of isosorbide mononitrate with dihydroergotamine may increase the plasma concentration of dihydroergotamine and thus enhance its antihypertensive effect.

In combination with amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine) the antianginal effect may be increased.

With the influence of beta-adrenomimetics, alpha-adrenoblockers (dihydroergotamine) a decrease of the antianginal effect (tachycardia, excessive BP reduction) is possible.

Barbiturates accelerate metabolism and decrease the concentration of isosorbide mononitrate in blood.

Decreases the effect of vasopressors.

When combined with m-cholinoblockers (atropine), there is an increased likelihood of increased intraocular pressure.

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

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

Please note that the above drug interactions are also possible if the above drugs were used shortly before starting treatment with Efox Long.

Special Instructions

Efox Long is not used to stop acute attacks of angina pectoris.

Long use of Efox Long may lead to development of tolerance, therefore it is recommended to take a 3-5 day break after 3-6 weeks of regular use of the drug, replacing Efox Long with other antianginal drugs.

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

The drug should not be reapplied if symptoms of intolerance develop.

The treatment with Efox Long should not be stopped abruptly. It is important to stop the drug gradually to avoid developing withdrawal symptoms.

At the time of treatment with the drug the use of alcohol should be avoided.

Pediatric use

To date there has been no experience with the use of Efox Long in children.

Impact on the ability to drive vehicles and other mechanisms requiring high concentration

During treatment, it is not recommended to drive vehicles and engage in other potentially hazardous activities requiring rapid psychomotor reactions.

Contraindications

• High sensitivity to the drug, organic nitrates;
• acute circulatory disorders (shock, vascular collapse);
• expressed arterial hypotension (systolic BP < 90 mmHg.st, and diastolic BP < 60 mm Hg);
• current use of phosphodiesterase inhibitors, including sildenafil, var. sildenafil, vardenafil, tadalafil, because they potentiate the hypotensive effect of the drug;
• cranial trauma, cerebral hemorrhage;
• anemia (severe form);
• hereditary galactose intolerance, lactase deficiency, or glucose and galactose malabsorption syndrome;
• toxic pulmonary edema;
• child and adolescent age below 18 years (effectiveness and safety not established).

The drug should be used with caution in: hypertrophic obstructive cardiomyopathy; constrictive pericarditis; pericardial tamponade; decreased left ventricular filling pressure, such as in acute myocardial infarction (risk of lower BP and tachycardia, which may worsen ischemia), decreased left ventricular function (left ventricular failure). Decreased systolic BP < 90 mmHg; aortic and/or mitral stenosis; susceptibility to arterial hypotension (orthostatic circulatory dysregulation); heart failure with low left ventricular filling pressure; glaucoma (risk of increased intraocular pressure); diseases accompanied by increased intracranial pressure (previously increased pressure has been observed only with high doses of nitroglycerin administered by injection), including.including hemorrhagic stroke, recent head trauma; significant renal insufficiency; hepatic insufficiency (risk of methemoglobinemia).

Side effects

Cardiovascular system disorders: at the beginning of treatment, headache (“nitrate” headache) may occur, which usually decreases after a few days of therapy; dizziness, facial hyperemia, fever, tachycardia. Sometimes, when taking the drug for the first time or after increasing the dose, a decrease in BP and/or orthostatic hypotension is observed, which may be accompanied by a reflex increase in HR, lethargy, as well as dizziness and a feeling of weakness. In rare cases, increased angina attacks (paradoxical response to nitrates), orthostatic collapse. There have been cases of collaptoid states, sometimes with bradyarrhythmia and fainting.

The use of Efox Long may lead to transient hypoxemia due to relative redistribution of blood flow to the hypoventilated alveolar segments. This can be a trigger mechanism of ischemia in CHD.

In the digestive system: nausea, vomiting, possibly a mild burning sensation of the tongue, dry mouth.

CNS disorders: 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 erythema multiforme exudative, widespread 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 efficacy.

Overdose

Symptoms: marked BP decrease with orthostatic dysregulation, palpitations, weakness, dizziness, lethargy, headache, flushed skin, nausea, vomiting, diarrhea, collapse, syncope, hyperthermia, seizures, sweating, methemoglobinemia (cyanosis, anoxia), hyperpnea, dyspnea, increased intracranial pressure, paralysis, coma.

Treatment: gastric lavage; if there is a marked decrease in BP and/or a state of shock, fluids should be administered; in exceptional cases, infusions of noradrenaline and/or dopamine may be given to improve blood circulation. Administration of epinephrine (adrenaline) and related compounds is contraindicated.

Depending on the severity, in cases of methemoglobinemia the following antidotes are used:

1. vitamin C – 1 g orally or in sodium salt form IV.
2. methylene blue – up to 50 ml of 1% solution w/v.
3. toluidine blue – first 2-4 mg/kg body weight w/v, then if necessary, repeated injections of 2 mg/kg body weight with an interval of 1 hour between injections are possible. 4. oxygen therapy, hemodialysis, exchange blood transfusion.
   

Similarities

Monochinqué, Monochinqué retard, Efox, Monosan, Pectrol