$31.00
Manufacturer: France
Prevention and long-term treatment of angina.
Description
Efox Long Storage
active substance: isosorbide mononitrate, isosorbide 5-nitrate;
1 prolonged-release capsule contains isosorbide mononitrate 50 mg;
Efox Long excipients: lactose, monohydrate, spherical sugar, talc, ethylcellulose, macrogol 20,000, hydroxypropylcellulose;
hard gelatin capsule: titanium dioxide (E 171), iron oxide red (E 172), iron oxide black (E 172), gelatin.
Efox Long Dosage form
Prolonged-release capsules.
Main physical and chemical properties: capsule lid – brown, opaque;
capsule body – pink, opaque; capsule contents – white or almost white granules.
Pharmacotherapeutic group
Vasodilators used in cardiology.
ATX code C01D A14.
Pharmacological properties
Pharmacodynamics.
Isosorbide mononitrate (CCM) causes vascular smooth muscle to relax, thereby causing it to dilate. Postcapillary vessels, as well as large arteries, especially those parts of the coronary arteries that have retained reactivity, are much more affected than resistance vessels. The latter effect promotes blood deposition and reduces the volume of venous blood returning to the heart; thus reducing ventricular end-diastolic pressure and volume (preload).
A decrease in the radius of the ventricle and a decrease in systolic tension of the vascular wall causes a decrease in the consumption of energy and oxygen by the heart.
Reducing the filling pressure of the heart promotes the perfusion of subendocardial areas prone to ischemia, which can improve regional contractions and stroke volume. Dilation of large arteries near the heart leads to a decrease in both systemic resistance (postload) and the output resistance of the pulmonary artery.
Effects on other organ systems include relaxation of the bronchial muscles, urinary tract, gallbladder muscles, as well as the muscles of the bile ducts, esophagus, large and small intestines, including the sphincters.
Mechanism of action.
At the molecular level, nitrates are likely to act through the production of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP), which may mediate relaxation.
Pharmacokinetics.
CCI after oral administration is rapidly and completely absorbed. Systemic bioavailability is 90-100%. Isosorbide mononitrate is almost completely metabolized in the liver. Metabolites are not active.
The half-life from blood plasma is 4-5 hours.
Isosorbide mononitrate is excreted almost exclusively as metabolites through the kidneys. Only about 2% of the compound is excreted unchanged.
Bioavailability.
For Efox® Long, a prolonged-release capsule (50 mg) from a bioavailability study involving 18 healthy male volunteers (on an empty stomach), the following data were established – maximum plasma concentration (Cmax) is 488 ± 129 ng / ml, time to maximum plasma concentration (tmax) – 5 hours, area under the curve (AUC) – 5029 ± 1272 ng • h / ml compared to the reference drug (20 μg, immediate release tablets) 436 ± 138 ng / ml, 1 hour and 5843 ± 1877 ng • h / ml, respectively (results are given as the mean value with standard deviation).
Tolerance.
Despite constant dosing and constant levels of nitrate in blood plasma, there may be a decrease in the effectiveness of the drug. If tolerance develops, it can be overcome by interrupting therapy for 24 hours. Taking the drug intermittently does not lead to the development of tolerance.
Indication
Prevention and long-term treatment of angina.
Contraindication
Hypersensitivity to isosorbide mononitrate, other nitrate compounds or to any of the excipients;
acute circulatory failure (shock, vascular collapse);
acute myocardial infarction with low filling pressure;
cardiogenic shock (unless sufficient left ventricular end-diastolic pressure is maintained through intra-aortic counterpulsation or the use of drugs with a positive inotropic effect);
hypertrophic obstructive cardiomyopathy;
constrictive pericarditis;
cardiac tamponade;
severe hypotension (systolic blood pressure below 90 mm Hg);
severe anemia;
severe hypovolemia.
Phosphodiesterase inhibitors (sildenafil, tadalafil, vardenafil) should not be used during nitrate therapy (see sections 4.4).
“Interaction with other medicinal products and other forms of interaction”).
Soluble guanylate cyclase stimulant riociguate should not be used during nitrate therapy (see Interaction with other medicinal products and other forms of interaction).
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