Composition, form of production and packaging
Long-acting tablets coated with a film membrane , coated with a white white film with a yellowish hue, oval, slightly biconcave, with a risk on both sides, with an engraving "60" on one side, with possible splotches; on a cross-section - a yellowish-white rough mass with white impregnations with a shell of white with a yellowish shade of color.
1 tab.
isosorbide mononitrate 60 mg
Excipients: hypromellose - 102.333 mg, carnauba wax - 51.167 mg, stearic acid purified - 51.167 mg, lactose monohydrate - 38.167 mg, silicon dioxide colloid - 2 mg, magnesium stearate - 1.5 mg.
The composition of the film shell: talc - 2.8 mg, hypromellose - 2.167 mg, titanium dioxide - 2.1 mg, magnesium stearate - 4 mg, macrogol 4000 - 0.45 mg, iron oxide oxide yellow (E172) - 0.05 mg.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
Tablets of prolonged action , covered with a film coating of white with a yellowish hue of color, round, slightly biconcave, with engraving "IM40" on one side, with possible impregnations; on a cross-section - a yellowish-white rough mass with white impregnations with a shell of white with a yellowish shade of color.
1 tab.
isosorbide mononitrate 40 mg
Excipients: hypromellose - 68.266 mg, carnauba wax - 34.133 mg, stearic acid purified - 34.133 mg, lactose monohydrate - 25.446 mg, silicon dioxide colloid - 1.333 mg, magnesium stearate - 1 mg.
Composition of the film shell: talc - 1.866 mg, hypromellose - 1.44 mg, titanium dioxide - 1.4 mg, magnesium stearate - 2.666 mg, macrogol 4000 - 0.3 mg, ferric oxide yellow oxide (E172) - 0.033 mg.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Peripheral vasodilator with predominant effect on venous vessels. Antianginal drug of prolonged action.
Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in cGMP (mediator of vasodilation). Vasodilatation reduces the venous return to the heart (preload), reducing the burden on the heart, which reduces the need for myocardium in oxygen.
Dilating effect of nitrates on arteries and arterioles reduces resistance to ejection (postload). Possesses coronary dilatation.
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 exercise tolerance in IHD patients.
It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.
Inhibits platelet aggregation, reduces intra-platelet synthesis of thromboxane.
Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored.
Antianginal effect occurs 30-40 minutes after ingestion and lasts up to 8-10 hours.
PHARMACOKINETICS
Suction and distribution
After taking the drug inside isosorbide-5-mononitrate quickly and completely absorbed from the digestive tract. The therapeutic concentration in plasma (100 ng / ml) is achieved 30 minutes after ingestion.
Has an absolute bioavailability - about 100%, since there is no effect of the first passage through the liver. The release of isosorbide-5-mononitrate from tablets is not dependent on food intake, peristalsis or pH in the lumen of the intestine.
It binds to blood plasma proteins by 5%.
Metabolism and excretion
Isosorbide mononitrate is metabolized by denitrification and conjugation with glucuronic acid.
An inactive metabolite is excreted in the urine. Renal clearance - 115 ml / min.
T 1/2 is between 4 and 10 hours.
Pharmacokinetics in special clinical cases
With hepatic and renal failure, the pharmacokinetics of isosorbide-5-mononitrate does not change significantly.
INDICATIONS
- prevention of angina attacks in patients with IHD;
- chronic heart failure (as part of combination therapy).
DOSING MODE
Tablets should be taken orally, after eating, swallowed whole and washed down with a glass of water. The dose of the drug and the frequency of reception is determined individually, depending on the severity of the disease.
The average initial dose is 40 mg 1 time / day (in the morning). In the case of nocturnal attacks of angina pills should be taken in the evening. If necessary, the dose of the drug can be increased to 60 mg 1 time / day or 40 mg 2 times / day.
Depending on the severity of the clinical effect from 3-5 days of therapy, the dose can be increased to 60 mg 1 time / day or 40 mg 2 times / day.
Treatment of chronic heart failure usually begins in the hospital, where the dose is selected until the appropriate maintenance dose is determined. The appropriate dose of the drug should be determined taking into account the clinical effect and side effects.
The recommended maintenance dose for both indications is 40 mg or 60 mg 1 time / day or 40 mg 2 times / day (1 tablet in the morning and the second approximately 7 hours later). The interval between taking the drug in the evening and taking the next dose in the morning should be at least 12 hours.
SIDE EFFECT
From the side of the cardiovascular system: "nitrate" headache, dizziness, transient hyperemia of the skin of the face, sensation of heat, tachycardia, marked decrease in blood pressure; in rare cases - increased attacks of angina (paradoxical reaction), orthostatic collapse.
On the part of the digestive system: nausea, vomiting, there may be a feeling of slight burning 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); in rare cases - ischemia of the brain.
Dermatological reactions: skin rash, in some cases - exfoliative dermatitis.
Other: development of tolerance (including cross-over to other nitrates).
CONTRAINDICATIONS
- arterial hypotension and hypovolemia (systolic blood pressure below 100 mmHg, diastolic blood pressure below 60 mmHg, central venous pressure below 4-5 mmHg);
- acute heart failure;
- shock;
- Vascular collapse;
- left ventricular failure with low end-diastolic pressure;
- Acute myocardial infarction (with severe arterial hypotension);
- cardiac tamponade;
- toxic pulmonary edema;
- diseases accompanied by increased intracranial pressure (including the number of hemorrhagic stroke, craniocerebral injury);
- lactation period;
- age under 18 years (effectiveness and safety not established);
- Hypersensitivity to nitrates or other components of the drug.
With caution , the drug should be prescribed for mitral valve prolapse, aortic and / or mitral stenosis, a tendency to orthostatic disorders of vascular regulation, constrictive pericarditis, severe anemia, thyrotoxicosis, hypertrophic cardiomyopathy (possibly an increase in angina attacks), severe renal failure, liver failure methemoglobinemia), as well as elderly patients.
PREGNANCY AND LACTATION
The use of the drug in pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus or child.
If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be given to the drug with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure (risk of development of methaemoglobinaemia).
APPLICATION FOR CHILDREN
Safety and effectiveness of the drug in children are not established. Contraindicated: age to 18 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
SPECIAL INSTRUCTIONS
Pectrol В® is not intended for relief of angina attacks.
Proper use of Pectrol В® guarantees the presence of a period with a low concentration of nitrate, which is necessary to prevent the development of tolerance to nitrates.As for all nitrates, it is important to strictly follow the instructions for the dosage regimen of Pectrol В® and observe the 12-hour interval between doses. In this case, a period with a low concentration (less than 100 ng / l) is achieved, while the therapeutic effect remains.
It is necessary to avoid the abrupt withdrawal of the drug and reduce the dose gradually.
During the therapy, it is necessary to monitor blood pressure and heart rate.
When transferring patients taking isosorbide dinitrate to isosorbide-5-mononitrate, the total daily dose should be calculated in advance. It is known that 10 mg of isosorbide-5-mononitrate corresponds to 20 mg of isosorbide dinitrate.
Use in Pediatrics
Safety and effectiveness of the drug in children are not established.
Impact on the ability to drive vehicles and manage mechanisms
There may be a decrease in the ability for rapid mental and motor reactions, so it is necessary to carefully manage vehicles and engage in potentially hazardous activities during the period of therapy with Pectrol В® .
OVERDOSE
Symptoms: headache, dizziness, palpitations, hyperthermia, skin hyperemia, sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnoea, dyspnoea, bradycardia, seizures, visual disorders, increased intracranial pressure, collapse, fainting, paralysis, coma.
Treatment: gastric lavage, with methemoglobinemia - inside or in / in ascorbic acid - 1 g, i / v 1% methylene blue solution 1-2 mg / kg; with severe arterial hypotension - intravenous phenylephrine (mezaton). Epinephrine and related compounds are ineffective.
DRUG INTERACTION
Pectrol В®, when used at the same time, increases the concentration of dihydroergotamine in the blood plasma.
Barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in the blood.
When combined with antihypertensive agents, vasodilators, antipsychotic agents (antipsychotics), tricyclic antidepressants, novocainamide, ethanol, quinidine, beta-adrenoblockers, slow calcium channel blockers, dihydroergotamine and sildenafil, hypotensive effect may increase.
When a combination of amiodarone, propranolol, slow calcium channel blockers (including verapamil, nifedipine), acetylsalicylic acid and Pectrol, an antianginal effect may increase.
Under the influence of beta-adrenostimulyatorov, alpha-adrenoblokatorov (including dihydroergotamine) is possible a decrease in the severity of the antianginal effect (tachycardia, excessive decrease in blood pressure).
When combined with m-holinoblokatorami (including atropine) increases the likelihood of increased intraocular pressure.
Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide-5-mononitrate in the digestive tract.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
