Pektrol, retard pills 40mg, 30pcs

Composition

Active ingredient:

Isosorbide-5-mononitrate 40.0 mg.

Auxiliary substances:

Hypromellose;

Carnauba wax;

Purified stearic acid;

Lactose monohydrate;

Magnesium stearate;

Purified silicon dioxide;

Talcum powder.

Titanium dioxide;

Macrogol 4000;

The iron oxide dye is red.

Pharmacological action

Peripheral vasodilator with a predominant effect on venous vessels.

• Pektrol stimulates the formation of nitric oxide (an endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in cGMP (a vasodilation mediator). Vasodilation reduces venous return to the heart (preload), reducing the load on the heart, which reduces the need for oxygen in the myocardium. The dilating effect of nitrates on the arteries and arterioles reduces OPSS (afterload).

• Pektrol has a corona-expanding effect. Reduces blood flow to the right atrium, helps to reduce pressure in the small circle of blood circulation and regression of symptoms in pulmonary edema. Promotes redistribution of coronary blood flow in areas with reduced blood supply.

• Pektrol increases exercise tolerance in patients with CHD and angina pectoris. Dilates the blood vessels of the brain, dura mater, which can be accompanied by a headache. Inhibits platelet aggregation, reduces intraplatelet synthesis of thromboxane.

As with other nitrates, cross-tolerance develops. After withdrawal (a break in treatment), sensitivity is quickly restored.

The antianginal effect occurs 30-40 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics After oral use, isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract (GIT). It has absolute bioavailability – about 100%, since there is no “first pass” effect through the liver. The release of isosorbide mononitrate from tablets does not depend on food intake, peristalsis, or pH in the intestinal lumen. Isosorbide mononitrate is distributed in the general body fluid, and only 5% binds to plasma proteins. The therapeutic concentration of 100 ng / ml is reached 30 minutes after oral use. Isosorbide mononitrate is metabolized by denitrization and conjugation with glucuronic acid. The inactive metabolite is excreted through the kidneys. Renal clearance 115 ml/min. The elimination half-life is 4 to 10 hours. In hepatic and renal insufficiency, the pharmacokinetics of isosorbide mononitrate do not change significantly.

Indications

• Prevention of angina attacks in patients with ischemic heart disease;

• Chronic heart failure (as part of combination therapy).

Use during pregnancy and lactation

The use of isosorbide mononitrate is possible only if the expected benefit to the mother exceeds the potential risk to the fetus and/or child.

Contraindications

• Hypersensitivity to nitrates or other components of the drug.

• 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 hypotension);

• Cardiac tamponade;

• Toxic pulmonary edema;

• Diseases;

• Accompanied by increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury);

• Lactation period;

• Age up to 18 years (efficacy and safety have not been established).

With caution:

• Mitral valve prolapse;

• Aortic and / or mitral stenosis;

• Tendency to orthostatic disorders of vascular regulation;

• Constrictive pericarditis;

• Advanced age;

• Severe anemia.

• Thyrotoxicosis;

• Hypertrophic cardiomyopathy (possibly increased frequency of angina attacks);

• Severe renal failure;

• Hepatic insufficiency (risk of developing methemoglobinemia).

Side effects

From the cardiovascular system:  “nitrate” headache, dizziness, transient hyperemia of the facial skin, a feeling of heat, tachycardia, a marked decrease in blood pressure (BP). In rare cases-increased angina attacks (paradoxical reaction), orthostatic collapse.

From the gastrointestinal tract:  nausea, vomiting, perhaps a slight burning sensation of the tongue, dry mouth;

From the central nervous system:  stiffness, drowsiness, blurred vision, decreased ability to react quickly (especially at the beginning of treatment). In rare cases-cerebral ischemia.

Allergic reactions:  skin rash, in some cases-exfoliative dermatitis.

Other services:  development of tolerance (including cross-tolerance to other nitrates).

Interaction

Concomitant use of Pektrol increases the concentration of dihydroergotamine in blood plasma.

Barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in the blood.

When combined with antihypertensive agents, vasodilators, antipsychotics (neuroleptics), tricyclic antidepressants, novocainamide, ethanol, quinidine, beta-blockers, slow calcium channel blockers, dihydroergotamine and sildenafil, the hypotensive effect may increase. The combination of amiodarone, propranolol, slow calcium channel blockers (including verapamil, nifedipine), acetylsalicylic acid and Pektrol may enhance the antianginal effect.

Under the influence of beta-adrenostimulants, alpha-blockers (including dihydroergotamine), it is possible to reduce 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, binders and enveloping agents reduce the absorption of isosorbide-5-mononitrate in the gastrointestinal tract.

How to take, course of use and dosage

Tablets should be taken orally, after meals, swallowed whole and washed down with a glass of water.

The usual starting dose is 1 tablet of 40 mg per day, in the morning.

If necessary, the dose can be increased to 60 mg per day.

In the case of nocturnal angina attacks, the tablet should be taken in the evening.

The dose of the drug can be increased to 60 mg 1 time a day or up to 2 tablets of 40 mg 2 times a day in 2 divided doses. The dose of the drug and the frequency of use is set individually, depending on the severity of the disease. Depending on the severity of the clinical effect, from 3-5 days of therapy, a single dose can be increased to 40-60 mg (in special cases, up to 80 mg/day) with the same frequency of use.

Treatment of chronic heart failure is usually initiated in a hospital setting, 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.

For both indications, patients should take 1 tablet of 40 mg or 60 mg once a day or a tablet of 40 mg twice a day (1 tablet in the morning and the second in about 7 hours). At least 12 hours should elapse between taking the last dose of the drug in the evening and the first dose of the drug the next morning.

Overdose

Symptoms:  headache, dizziness, palpitations, hyperthermia, skin hyperemia, sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnea, dyspnea, bradycardia, convulsions, visual disturbances, increased intracranial pressure, collapse, fainting, paralysis, coma.

Treatment:  gastric lavage, with methemoglobinemia-inside or in / in ascorbic acid-1 g in / in 1% methylene blue solution 1-2 mg/kg. Symptomatic therapy for severe arterial hypotension – intravenous phenylephrine (mezaton), (epinephrine and related compounds are ineffective).

Special instructions

Pektrol is not intended to stop an attack of angina.

Proper use of mononitrate isosorbide ensures that there is a period with a low nitrate concentration, which is necessary to prevent the development of nitrate tolerance. As with all nitrates, it is important to strictly follow the instructions for dosing Pektrol 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 is preserved.

It is necessary to avoid abrupt discontinuation of the drug and reduce the dose gradually.

During therapy, it is necessary to monitor blood pressure and heart rate.

When transferring patients taking isosorbide dinitrate to isosorbide mononitrate, the total daily dose should be calculated in advance. It is known that 10 mg of mononitrate corresponds to 20 mg of isosorbide dinitrate.

Influence on the ability to drive vehicles and work with mechanisms:

There may be a decrease in the ability to respond quickly to mental and motor reactions, so you should drive vehicles with caution and engage in potentially dangerous activities during therapy with the drug.

Form of production

Pills.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Isosorbide Mononitrate

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Angina, Heart Failure, Myocardial Infarction