Pectrol - instructions for use, dose, side effects, contraindications

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Dosage form: & nbspsustained-release tablets

Composition:1 tablet of prolonged action contains

Active substance: isosorbide-5-mononitrate 40.0 mg or 60.0 mg

Excipients: hypromellose, carnauba wax, stearic acid purified, lactose monohydrate, magnesium stearate, silicon dioxide purified, talc, titanium dioxide, Macrogol 4000, iron oxide red dye.

Description:

tablets 40 mg - round, slightly biconcave tablets, covered with a cream-colored membrane of cream color with the inscription "1M 40" on one side, with possible splotches.

tablets 60 mg - oval, slightly biconcave tablets, covered with a cream-colored film shell, with a notch on both sides and with the inscription "60" on one side, with possible splotches.

Pharmacotherapeutic group:vasodilator - nitrate

Pharmacodynamics:Peripheral vasodilator with predominant effect on venous vessels. Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, which results in an increase in cGMP (a 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 tolerance to physical activity in patients with ischemic heart disease (IHD), angina pectoris. 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:

After oral administration, isosorbide mononitrate is rapidly and completely adsorbed from the gastrointestinal tract (GIT). Has absolute bioavailability - about 100%, since there is no effect of "first passage" through the liver. The release of isosorbide mononitrate from tablets does not depend on food intake, peristalsis or pH in the luminal gut.Isosorbide mononitrate is distributed in the body's total fluid, and only 5% binds to blood plasma proteins. The therapeutic concentration of -100 ng / ml - is achieved 30 minutes after the appointment inward. Isosorbide mononitrate is metabolized by denitrification and conjugation with glucuronic acid. An inactive metabolite is excreted through the kidneys. Kidney clearance 115 ml / min. The half-life is between 4 and 10 hours. With hepatic and renal failure, the pharmacokinetics of isosorbide mononitrate does not change significantly.

Indications:

- Prevention of angina attacks in patients with ischemic heart disease

- Chronic heart failure (as part of combination therapy)

Contraindications:

Hypersensitivity to isosorbide mononitrate, other nitro compounds and components of the drug; severe 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 (including cardiogenic shock), vascular collapse,left ventricular failure with low end-diastolic pressure, acute myocardial infarction (with severe arterial hypotension), severe aortic and / or severe mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), cardiac tamponade, constrictive pericarditis, toxic pulmonary edema, severe anemia, concomitant use with inhibitors of phosphodiesterase-5 (PDE-5) (sildenafil, vardenafil, tadalafil), the period of breastfeeding, the age of 18 years (efficacy and safety not established), lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Carefully:mitral valve prolapse, aortic and / or mitral stenosis, propensity to orthostatic disorders of vascular regulation, elderly patients, thyrotoxicosis, angle-closure glaucoma, severe renal failure, liver failure (risk of methaemoglobinaemia), diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral injury), hypothyroidism, malnutrition.

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 the child.

Dosing and Administration:

Tablets should be taken orally, whole, with water for 1 hour before or 2 hours after eating.

The initial dose is 1 tablet (40 mg) once a day, in the morning.

If necessary, the dose may be increased to 60 mg once a day. In the case of nocturnal attacks of angina pills should be taken in the evening. The dose of the drug and the frequency of admission is determined individually, depending on the severity of the disease. Depending on the severity of the clinical effect from 3 to 5 days of therapy, a single dose can be increased to 60 to 80 mg (in special cases up to 80 mg / day - 1 tablet 40 mg twice a day). Treatment of chronic heart failure is usually initiated in the hospital, where the dose is selected taking into account the therapeutic effect and side effect.

Pectrol® should be taken 1 tablet (40 mg or 60 mg) once a day or 1 tablet (40 mg) twice a day (1 tablet in the morning and the second in about 7 hours). The interval between taking the last dose of the drug in the evening and the first dose of the drug the next morning - at least 12 hours.

Side effects:

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

From the digestive tract: nausea, vomiting, there may be a sensation of slight burning of the tongue, dry mouth;

From 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.

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

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

Overdose:

Symptoms: Headache, dizziness, palpitations, hyperthermia, skin flushing, sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnoea, dyspnea, bradycardia, seizures, visual disturbances, increased intracranial pressure, collapse, fainting, paralysis, coma .

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

Interaction:

Increases the concentration of dihydroergotamine in the blood plasma. Barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in the blood plasma. With simultaneous use with vasodilators, antipsychotic drugs (antipsychotics), tricyclic antidepressants, procainamide, ethanol, quinidine, beta-adrenoblockers, blockers of "slow" calcium channels, diuretics, dihydroergotamine, PDE-5 inhibitors (incl. sildenafil, vardenafil, tadalafil) may increase the hypotensive effect. With the simultaneous use of amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine and others) and isosorbide mononitrate, an antianginal effect may increase. Under the influence of beta-adrenomimetics, alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to reduce the antianginal effect (tachycardia, excessive blood pressure decrease).When used simultaneously with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure. Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.

It is possible to reduce the therapeutic effect of norepinephrine (norepinephrine). With simultaneous use of all vasodilating agents, whose action is associated with nitric oxide, including classical donators of nitric oxide (for example, nitroglycerine, isosorbide dinitrate, isosorbide mononitrate, sodium nitroprusside, molsidomine), etc., with sapropterin (coenzyme of nitric oxide synthetase) is increased risk development of arterial hypotension.

Special instructions:

The drug Pectrol is not intended for relief of angina attacks.

During the therapy, it is necessary to monitor blood pressure and heart rate (heart rate). In case of need of application of a preparation against a background of an arterial hypotension it is necessary to simultaneously apply medicines (ЛС), possessing a positive inotropic effect.

Proper use of Pectrol® provides a period with a low concentration of isosorbide mononitrate, which is necessary to prevent the development of tolerance to nitrates.As for all nitrates, it is important to strictly follow the dosage regimen and a 12-hour interval between the use of Pectrol®. In this case, a period with a low concentration (less than 100 ng / L) is achieved, while a therapeutic effect is maintained. It is necessary to avoid abrupt discontinuation of Pectrol® and reduce the dose gradually. Frequent use and high doses can cause tolerance, in this case it is recommended to cancel the drug for 24-48 h or a break for 3-5 days after 3-6 weeks of regular admission, replacing for this time isosorbide mononitrate by other antianginal JICs. When transferring a patient from isosorbide dinitrate therapy to Pectrol®, the total daily dose should be calculated in advance. It is known that 10 mg of isosorbide mononitrate corresponds to 20 mg of isosorbide dinitrate.

It is possible to develop transient hypoxemia due to the redistribution of blood flow to hypoventilation alveolar segments. During the period of application of the preparation Pectrol® it is necessary to exclude the use of alcohol.

With the simultaneous use of the drug Pectrol® with sapropterin, it is recommended to monitor blood pressure.

Effect on the ability to drive transp. cf. and fur:Perhaps a decrease in the ability to rapid mental and motor reactions, so you should carefully manage vehicles and engage in potentially hazardous activities during drug therapy.

Form release / dosage:Tablets of prolonged action of 40 mg and 60 mg.

Packaging:10 tablets in a blister pack. 3 or 10 blisters in a cardboard box together with instructions for use.

Storage conditions:Store at a temperature not higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011751 / 01

Date of registration:04.03.2010

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

VALPHARMA, S.A. Republic of San Marino

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp16.10.2014

Illustrated instructions

Instructions

Pectrol® (Pektrol®)