PEKTROL®

Active material: Izosorʙida mononitrat
When ATH: C01DA14
CCF: Peripheral vasodilators. Antianginal drug
ICD-10 codes (testimony): i20, I50.0
When CSF: 01.06.01.01.03
Manufacturer: KRKA d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Sustained-release tablets, film-coated cream colour, round, slightly biconcave, with an inscription “Im40” on one side, with possible inclusions.

Excipients: gipromelloza, carnauba wax, purified stearic acid, lactose monohydrate, magnesium stearate, purified silicon dioxide, talc, Titanium dioxide, macrogol 4000, iron oxide red dye.

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Sustained-release tablets, film-coated cream colour, Oval, slightly biconcave, with a notch on both sides and with an inscription “60” on one side, with possible inclusions.

Excipients: gipromelloza, carnauba wax, purified stearic acid, lactose monohydrate, magnesium stearate, purified silicon dioxide, talc, Titanium dioxide, macrogol 4000, iron oxide red dye.

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

Peripheral vasodilator with a primary effect on the venous vessels. Antianginalny product of prolonged action.

Stimulates nitric oxide (endothelial relaksirutego factor) in endotelia receptacles, calling the activation of intracellular guanylyl Cyclase, resulting in an increase in cGMP (Mediator of vasodilation). Vasodilation decreases venous return to the heart (preload), reducing the load on the heart, that reduces the need heart of oxygen.

Dilatirujushhij effect of nitrates on the artery and arteriola reduces resistance to release (afterload). Has koronarorasshirjajushhim activity.

Reduces blood flow to the right predserdiu, contributes to the reduction of pressure in the small circle of blood circulation and regression of symptoms oteke light. Promotes the redistribution of coronary blood flow in the area with reduced blood circulation.

Increases tolerance to physical activity in patients with ischemic heart disease.

Dilates blood vessels in the brain, dura mater, that may be accompanied by headache.

It inhibits platelet aggregation, reduces vnutritrombocitarnyj of thromboxane synthesis.

Like other nitrates, develops cross tolerance. After the abolition of the (interruption of treatment) sensitivity to it quickly recovers.

Antianginalny effect comes through 30-40 minutes after administration inwards and continues until 8-10 no.

Pharmacokinetics

Absorption and distribution

After taking the drug inside Isosorbide-5-mononitrate is rapidly and completely absorbed from the digestive tract. C_max plasma (100 ng / ml) achieved through 30 minutes after ingestion.

Has absolute biodostupnostthew – about 100%, Since there is no effect of the first passage through the liver. Release of Isosorbide-5-mononitrate tablets does not depend on the meals, peristalsis or pH in the bowel lumen.

Associated with the plasma protein on 5%.

Metabolism and excretion

Isosorbide mononitrate metabolised denitrizaciej and konjugaciej with glukuronova acid.

Inactive metabolite is excreted in the urine. Renal clearance – 115 ml / min.

T_1/2 It is between 4 to 10 no.

Pharmacokinetics in special clinical situations

When liver and kidney failure farmakokinetika Isosorbide-5-mononitrate does not change significantly.

Testimony

-Prevention of strokes in patients with ISCHEMIC HEART DISEASE;

- Congestive heart failure (in a combination therapy).

Dosage regimen

The tablets should be taken orally, after meal, swallowed whole and drink a glass of water. Dose and frequency reception is established individually depending on the severity of the disease.

The average initial dose of 40 mg 1 time / day (morning). In the case of nocturnal angina attacks tablet should be taken in the evening. If necessary dose can be increased to 60 mg 1 time / day or 40 mg 2 times / day.

Depending on the severity of clinical effect with 3-5 day therapy dose can be increased to 60 mg 1 time / day or 40 mg 2 times / day.

Treatment of chronic heart failure usually begin in the hospital, where dose selected until, until it is determined appropriate maintenance dose. The appropriate dose of the drug should be determined by taking into consideration the clinical effect and side effects.

The recommended dose for both indications is 40 mg or 60 mg 1 time / day or 40 mg 2 times / day (1 tab. in the morning and the second approximately 7 no). The interval between admission and reception evening medication next dose in the morning should not be less than 12 no.

Side effect

Cardio-vascular system: “nitrate” headache, dizziness, passing hyperemia skin, feeling the heat, tachycardia, marked reduction in blood pressure; rarely – increasing angina attacks (paradoxical reaction), Orthostatic hypotension.

From the digestive system: nausea, vomiting, Perhaps the feeling light stinging language, dry mouth.

CNS: constraint, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment); rarely – golovnogo ischemia mozga.

Dermatological reactions: skin rash, in some cases – exfoliative dermatitis.

Other: the development of tolerance (incl. Cross to other nitrates).

Contraindications

-arterial hypotension and hypovolemia (systolic BP below 100 mmHg., diastolic HELL below 60 mmHg., central venous pressure below 4-5 mmHg.);

- Acute heart failure;

- Shock;

- Vascular collapse;

— levojeludochkovaya failure with low end diastolic pressure;

- Acute myocardial infarction ((c) expressed arterial hypotension);

-Cardiac tamponade;

-toxic pulmonary edema;

- Diseases, accompanied by increased intracranial pressure (incl. the number of hemorrhagic stroke, traumatic brain injury);

- Lactation;

- Up to 18 years (efficacy and safety have not been established);

-hypersensitivity to nitrates or other components of the drug.

FROM caution should designate product in mitral valve prolapse, aortalnom and/or mitralnom stenoze, the trend towards ortostaticheskim vascular regulation violations, constroguom pericardite, severe anaemia, thyrotoxicosis, hypertrophic cardiomyopathy (perhaps showing strokes), renal insufficiency, hepatic insufficiency (risk of methemoglobinemia), and elderly patients.

Pregnancy and lactation

Use of the drug during pregnancy is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus or child.

If necessary, the appointment during lactation breastfeeding should be discontinued.

Cautions

Pektrol^® not designed for short strokes.

Proper use of the drug Pektrol^® ensures that the period of low nitrate concentrations, What is needed to prevent the development of tolerance to nitrates. As with all nitrate, It is important to strictly follow the instructions for the drug's dosing regime Pektrol^® and comply with the 12-hour interval between doses. In this case, the period is achieved with low concentration (less 100 ng/l), This preserves the therapeutic effect.

There is a need to avoid abrupt cancellation of the drug and reduce the dose gradually.

During a therapy monitoring ad and HR.

The transfer of patients, taking Isosorbide dinitrate on Isosorbide-5-mononitrate, the total daily dose should be calculated in advance. Known, what 10 mg Isosorbide-5-mononitrate correspond 20 mg Isosorbide dinitrate.

Use in Pediatrics

The safety and effectiveness of drugs in children are not installed.

Effects on ability to drive vehicles and management mechanisms

May impair the ability to rapid mental and motor reactions, so you must be careful when driving and to engage in potentially dangerous activities in the period of therapy with Pektrol^®.

Overdose

Symptoms: headache, dizziness, heartbeat, hyperthermia, dermahemia, Sweating, nausea, vomiting, diarrhea, metgemoglobinemiâ (cyanosis, anoksija), giperpnoje, dyspnoea, bradycardia, convulsions, visual disturbances, intracranial hypertension, collapse, fainting, paralysis, coma.

Treatment: gastric lavage, if methemoglobinemia – inside or/Ascorbic acid – 1 g, I / 1% methylene blue solution 1-2 mg / kg; with severe arterial hypotension – in/phenylephrine (mezaton). Epinephrine and related compounds are ineffective.

Drug Interactions

Pektrol^® While applying digidroergotamina concentration increases in plasma.

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

When coupled with antigipertenzivei means, vazodilatatorami, antipsychotic drug (neuroleptics), tricyclic antidepressants, novokainamidom, ethanol, xinidinom, beta-blockers, blockers of slow calcium channels, digidroergotaminom and sildenafilom may increase gipotenzivnogo effect.

With a combination of amiodarone, propranolol, blockers slow calcium channels (incl. verapamil, nifedipine), acetylsalicylic acid and Pektrola^® Perhaps increased antianginalnogo effect.

Under the influence of beta-adrenostimuljatorov, alpha-blockers (incl. digidroergotamin) perhaps reduction of expressiveness of antianginalnogo effect (tachycardia, excessive reduction of blood pressure).

The combined application with m-holinoblokatorami (incl. atropyn) the likelihood of increase intraocular pressure.

Adsorbents, cementing and overlying a means to reduce intake of Isosorbide-5-mononitrate in the digestive tract.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.