Pectrol tablets p / o prolonged action 60mg, No. 30

Prevention of angina attacks. Chronic heart failure (as part of combination therapy), some forms of pulmonary hypertension and cor pulmonale (as part of combination therapy).

The tablets should be taken orally, whole, with water 1 hour before or 2 hours after a meal.
The initial dose is 1 tablet (40 mg) once a day, in the morning.
If necessary, the dose can be increased to 60 mg once a day. In case of nocturnal attacks of angina pectoris, the tablet should be taken in the evening. The dose of the drug and the frequency of administration is set 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 - 80 mg (in special cases, up to 80 mg / day - 1 tablet 40 mg 2 times a day).

Treatment of chronic heart failure is usually started in a hospital, where the dose is selected taking into account the therapeutic effect and side effects.
The drug Pectrol must 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 after 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 is at least 12 hours.

Active substance:

isosorbide mononitrate 60 mg

Excipients:

Hypromellose

Carnauba wax

Purified stearic acid

Lactose monohydrate

Colloidal silicon dioxide

Magnesium stearate

Film casing:

Talc

Hypromellose

Titanium dioxide

Magnesium stearate

Macrogol 4000

Iron dye yellow oxide (E172)

Acute circulatory disorders (shock, vascular collapse); cardiogenic shock in cases where high end diastolic pressure in the left ventricle is not provided by using intra-aortic counterpulsation or by administering drugs that have a positive inotropic effect; severe arterial hypotension (systolic blood pressure less than 90 mm Hg, diastolic - less than 60 mm Hg); concomitant use of sildenafil (PDE inhibitor); hypersensitivity to nitrates.

Description
Tablets 40 mg.
Round, slightly biconvex tablets, film-coated, white with a yellowish sheen, engraved on one side of the tablet '1M 40', with possible inclusions.
Cross-sectional view of the tablet: yellowish-white rough mass with white blotches with a shell of white with a yellowish tinge.

Tablets 60 mg.
Oval, slightly biconvex tablets, film-
coated, white with a yellowish tinge, scored on both sides,
engraved on one side of the tablet '60', with possible inclusions.
Cross-sectional view of the tablet: yellowish-white rough mass with white
blotches with a shell of white with a yellowish tinge.

Pharmacotherapeutic group: vasodilating agent - nitrate

Pharmacological properties
Pharmacodynamics
Peripheral vasodilator with a predominant effect on the venous vessels. Stimulates the formation of nitric oxide (an endothelial relaxing factor) in the vascular endothelium, which causes the activation of intracellular guanylate cyclase, resulting in an increase in cyclic guanosine monophosphate (cGMP) (a mediator of vasodilation). Reduces myocardial oxygen demand by reducing preload and afterload (reduces the end diastolic volume of the left ventricle and reduces the systolic tension of its walls). Has a coronary dilating effect. Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema. Promotes redistribution of coronary blood flow in areas with reduced blood circulation.Increases exercise tolerance in patients with coronary heart disease (CHD), angina pectoris. Expands the vessels of the brain, dura mater, which may be accompanied by a headache. Cross-tolerance develops to isosorbide, as to other nitrates. After the cancellation of therapy (a break in treatment), sensitivity to it quickly recovers. The antianginal effect occurs within 30-40 minutes after ingestion and lasts up to 8-10 hours.The antianginal effect occurs within 30-40 minutes after ingestion and lasts up to 8-10 hours.The antianginal effect occurs within 30-40 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics
After oral administration, isosorbide is rapidly and completely absorbed from the gastrointestinal
tract (gastrointestinal tract). Possesses absolute bioavailability (about 100%), since there is no effect of 'primary passage' through the liver. The release of isosorbide from tablets does not depend on food intake, peristalsis, or pH in the lumen of the gastrointestinal tract. Isosorbide has a high volume of distribution; less than 4% binds to blood plasma proteins. The therapeutic concentration (100 ng / ml) is reached within 30 minutes after ingestion. The time to reach the maximum concentration (TCmax) in the blood plasma is 1-1.5 hours. It is subjected to denitration with the formation of isosorbide or combines with glucuronide. The formed inactive 2-glucuronide is excreted through the kidneys. Renal clearance 115 ml / min. The half-life (T1 / 2) is from 4 to 10 hours. In hepatic and renal failure, the pharmacokinetics of isosorbide does not change significantly.

Indications for use

• ischemic heart disease: prevention of attacks of stable angina pectoris;

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

Contraindications
Hypersensitivity to isosorbide mononitrate, other nitro compounds and drug components; severe arterial hypotension and hypovolemia (systolic blood pressure below 100 mm Hg, diastolic blood pressure below 60 mm Hg, central venous pressure below 4-5 mm Hg); 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 (HOCM) , constrictive pericarditis, toxic pulmonary edema, severe anemia, simultaneous use with phosphodiesterase-5 (PDE-5) inhibitors (sildenafil, vardenafil, tadalafil),period of breastfeeding, age up to 18 years (efficacy and safety have not been established), lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

With caution: mitral valve prolapse, aortic and / or mitral stenosis, tendency to orthostatic disorders of vascular regulation, in elderly patients, thyrotoxicosis, angle-closure glaucoma, severe renal failure, liver failure (risk of methemoglobinemia), diseases accompanied by increased intracranial pressure ( including hemorrhagic stroke, traumatic brain injury), hypothyroidism, malnutrition.

Application during pregnancy and during breastfeeding
The drug Pectrol is not recommended during pregnancy.
The use of the drug Pectrol is possible only when the expected benefit to the mother outweighs the potential risk to the fetus and / or child.
If necessary, the use of the drug Pectrol breastfeeding should be discontinued.

Dosage and administration
Tablets should be taken orally, whole, washed down with water 1 hour before or 2 hours after meals.
The initial dose is 1 tablet (40 mg) once a day, in the morning.
If necessary, the dose can be increased to 60 mg once a day. In case of nocturnal attacks of angina pectoris, the tablet should be taken in the evening. The dose of the drug and the frequency of administration is set 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 - 80 mg (in special cases, up to 80 mg / day - 1 tablet 40 mg 2 times a day).

Treatment of chronic heart failure is usually started in a hospital, where the dose is selected taking into account the therapeutic effect and side effects.
The drug Pectrol must 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 after 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 is at least 12 hours.

Side effect
Classification of the incidence of side effects of the World Health Organization (WHO):
very often> 1/10
often from> 1/100 to <1/10
infrequently from> 1/1000 to <1/100
rarely from> 1/10000 to <1/1000
very rarely from <1/10000, including isolated reports.

From the side of the cardiovascular system:
often: 'nitrate' headache, dizziness, transient flushing of the facial skin, a feeling of heat, tachycardia, a marked decrease in blood pressure (BP); rarely: transient hypoxemia, increased angina attacks (paradoxical reaction), orthostatic collapse;
On the part of the digestive system:
infrequently: nausea, vomiting, a slight burning sensation of the tongue may appear, dryness of the oral mucosa; From the nervous system:
often: stiffness, drowsiness, blurred vision, decreased ability to quick mental and motor reactions (especially at the beginning of treatment);
rarely: cerebral ischemia;
Allergic reactions:
infrequently: angioedema, skin rash, urticaria;
very rare: exfoliative dermatitis, Stevens-Johnson syndrome;
Others:
infrequently: development of tolerance (including cross-over to other nitrates).

Overdose
Symptoms: marked decrease in blood pressure with orthostatic vasodilation, reflex tachycardia and headache. Weakness, dizziness, flushing of the skin, nausea, vomiting, diarrhea may appear. At high doses (more than 20 mg / kg of body weight), the appearance of methemoglobinemia, cyanosis, dyspnea and tachypnea should be expected due to the formation of nitrite ions due to the metabolism of isosorbide mononitrate. At very high doses of the drug, intracranial pressure may increase with cerebral symptoms. With chronic overdose, an increase in mettemoglobin is detected.
Treatment:gastric lavage; with methemoglobinemia, depending on the severity, intravenous ascorbic acid in the form of sodium salt is used (previously methylthionium chloride (methylene blue) was used at 0.1-0.15 ml / kg of 1% solution up to 50 ml); oxygen therapy, hemodialysis, exchange blood transfusion.
Symptomatic therapy with a pronounced decrease in blood pressure (epinephrine and related compounds are ineffective).

Interaction with other medicinal products
Increases the concentration of dihydroergotamine in blood plasma.
Barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in the blood.
With simultaneous use with vasodilators, antipsychotics (antipsychotics), tricyclic antidepressants, novocainamide, ethanol, quinidine, beta-blockers, blockers of 'slow' calcium channels, diuretics, dihydroergotamine, inhibitors of PDCH. tadalafil), an increase in the hypotensive effect is possible

With the simultaneous use of amiodarone, propranolol, blockers of 'slow' calcium channels (verapamil, nifedipine, etc.) and isosorbide mononitrate, an increase in the antianginal effect is possible.
Under the influence of beta-adrenergic agonists, alpha-blockers (dihydroergotamine, etc.), it is possible to reduce the severity of the antianginal effect (tachycardia, excessive decrease in blood pressure).

With simultaneous use with m-anticholinergics (atropine, etc.), the likelihood of an increase in intraocular pressure increases.
Adsorbents, astringents and coating agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.
It is possible to reduce the therapeutic effect of norepinephrine (norepinephrine).

With the simultaneous use of all vasodilating agents, the action of which is associated with nitric oxide, including classical donors of nitric oxide (for example, nitroglycerin isosorbide dinitrate, isosorbide mononitrate, sodium nitroprusside molsidomine), etc., with sapropterin (coenzyme of nitric oxide synthetase), the risk of
arterial hypotension increases ...

Special instructions
The drug Pectrol is not intended to relieve angina attacks.
During the period of therapy, it is necessary to control blood pressure and heart rate (HR). If it is necessary to use the drug against the background of arterial hypotension
, drugs with a positive inotropic effect should be used simultaneously.

Correct use of the Pectrol drug ensures the presence of a period with a low concentration of isosorbide mononitrate, which is necessary to prevent the development of nitrate tolerance. As with all nitrates, it is important to strictly adhere to the dosage regimen and the 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 the therapeutic effect remains.
It is necessary to avoid abrupt withdrawal of the Pectrol drug and gradually reduce the dose. Frequent use and high doses can cause the development of tolerance; in this case, it is recommended to cancel the drug for 24-48 hours or a break for 3-5 days after 3-6 weeks of regular intake, replacing at this time isosorbide mononitrate with other antianginal drugs.

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.
The development of transient hypoxemia is possible, due to the redistribution of blood flow to the hypoventilated alveolar segments.
During the period of application of the drug Pectrol, it is necessary to exclude the use of alcohol.
With the simultaneous use of the drug Pectrol with sapropterin, it is recommended to control blood pressure.

Influence on the ability to drive vehicles and other technical devices: when using the drug Pectrol, you must be careful when driving and working with complex technical devices due to the possibility of side effects.

Release form
Tablets of prolonged action, film-coated, 40 mg and 60 mg. 10 tablets are placed in a blister strip made of combined PVC / PVDC material and aluminum foil.
3 or 10 blisters are placed in a cardboard box along with
instructions for use.

Storage conditions
At a temperature not exceeding 25 ? —.
Keep out of the reach of children.

Shelf life is
3 years.
Do not use after the expiration date.

Terms of dispensing
Prescription.