AKRIDILOL

Active material: Karvedilol
When ATH: C07AG02
CCF: Beta₁-,beta₂-adrenoblokator. Alpha₁-adrenoblokator
ICD-10 codes (testimony): I10, i20, I50.0
Manufacturer: Chemical-pharmaceutical plant AKRIKHIN JSC (Russia)

Pharmaceutical form, composition and packaging

Pills Valium, a facet and Valium, from white to white with Valium a color shade, Slight marbling.

Excipients: ludipress LTSE (lactose, povidone), sodium starch glycolate (sodium carboxymethyl), magnesium stearate.

10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.

Pills square with rounded corners, lenticular, with Phillips a notch on one side and engraving “Al1” – another, from white to white with Valium a color shade, Slight marbling.

Excipients: ludipress LTSE (lactose, povidone), sodium starch glycolate (sodium carboxymethyl), magnesium stearate.

10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.

Pills Oval, lenticular, with partial notch on both sides and engraved “AL2” on one side, from white to white with Valium a color shade, Slight marbling.

Excipients: ludipress LTSE (lactose, povidone), sodium starch glycolate (sodium carboxymethyl), magnesium stearate.

10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.

Pharmacological action

Alpha- and beta-8th. Akridilol^® blocks β₁-, b₂– и a₁-adrenoreceptory. Provides vazodilatirtee, antianginalnoe and antiaritmicescoe action. The drug has no internal sympathomimetic activity, has membrane stabilizing properties. Thanks to β-adrenoceptor blockade hearts may decline ad, reduced cardiac output and decrease HEART RATE. Akridilol^® inhibits Renin-angiotensin-al′dosteronovuû system by β-adrenoceptor blockade kidneys, causing a decrease in Renin activity plasma. Inhibiting α-adrenergic receptor, the drug may cause peripheral vessels, that leads to a decrease in the ROUND.

Through a combination of β-adrenoceptor blockade and vasodilation drug reduces ad in hypertension; the disease has a protivojishemicescoe and antianginalnoe action; When left ventricular dysfunction and circulatory failure improves haemodynamic indicators, increases left ventricular ejection fraction and reduces its size.

There has expressed influence on lipid metabolism and potassium content, sodium and magnesium in plasma.

Has an antioxidant effect, eliminating the oxygen free radicals.

Pharmacokinetics

Absorption

After oral administration, carvedilol is rapidly absorbed from the gastrointestinal tract. High lipophilicity. C_max plasma levels achieved after 1-1.5 no. Bioavailability – 24-28%. Eating does not affect the bioavailability of carvedilol.

Distribution

Plasma protein binding is 95-99%.

Carvedilol penetrates through the placental barrier, excreted in breast milk.

Metabolism

Metabolised in the liver with the formation of a number of active metabolites; 60-75% absorbed drug is metabolized in “first pass” through the liver. Metabolites have a pronounced anti-oxidant and adrenoblokirutm action.

Deduction

T_1/2 is 6-10 no.

Excretion of the drug from the body mainly jelchew.

Pharmacokinetics in special clinical situations

If any of the kidneys carvedilol significantly the pharmacokinetic parameters do not change. In patients with impaired liver system bioavailability carvedilol improves by lowering metabolism when “first pass” through the liver.

In case of serious violations of the liver carvedilol is contraindicated.

Testimony

- Arterial hypertension (as monotherapy and in combination with diuretics);

- Congestive heart failure (in a combination therapy);

- CHD: stable angina.

Dosage regimen

At hypertension initial dose for Adult is 6.25-12.5 mg / day for 2 days. Then appoint 25 mg / day 1 time / day in the morning. Through the if necessary 14 days you can further increase the dose in 2 times. The maximum daily dose is 50 mg 1 time / day (Perhaps in 2 admission).

At CHD at the beginning of treatment, the drug is prescribed for 12.5 mg 2 times/day for the first 2 days of treatment, then – by 25 mg 2 times / day. In case of insufficiency antianginalnogo effect through 2 weeks of therapy dose can be increased in 2 times. The maximum daily dose is 100 mg (by 50 mg 2 times / day).

At chronic heart failure treatment is initiated with dosages 3.125 mg 2 times / day for 2 weeks. With good endurance dose increase at intervals of not less than 2 weeks before 6.25 mg 2 times / day, then to 12.5 mg 2 times/day and then to 25 mg 2 times / day. The dose should be increased to a maximum of, which is well tolerated by patients. In Patients weighing less than 85 kg the target dose of 50 mg / day; in patients weighing more 85 kg the target dose of 75-100 mg / day.

The drug should be taken regardless of mealtimes, drinking a small amount of liquid.

Side effect

From the central and peripheral nervous system: dizziness, headache (usually, not strong and early treatment), loss of consciousness, myasthenia (more often at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia.

Cardio-vascular system: bradycardia, orthostatic hypotension, AV-blockade II and III degrees; rarely – violation of periferičeskoû circulation, progression of heart failure (at a time of increased doses), edema of the lower extremities, angina, marked reduction in blood pressure.

From the digestive system: dry mouth, nausea, diarrhea or constipation, vomiting, stomach ache, loss of appetite, increase in liver transaminases.

From the hematopoietic system: rarely – thrombocytopenia, leukopenia.

Metabolism: weight gain, violation of carbohydrate metabolism.

Allergic reactions: allergic skin reactions (rash, hives, itch, rash), exacerbation of psoriasis, nasal congestion.

The respiratory system: Dyspnea and bronchospasm (prone patients).

Other: blurred vision, decrease in lacrimation, flu-like symptoms, chikhaniye, myalgia, arthralgia, pain in the limbs, intermittent claudication; rarely – violation of urination, impairment of renal function.

Contraindications

-acute or Decompensated chronic heart failure, requiring in/with the introduction of inotropic funds;

- Severe hepatic impairment;

— AV-blockade II and III degrees;

- Vыrazhennaya bradycardia (less 50 u. / min);

- SSS;

- Hypotension (systolic blood pressure less than 85 mm Hg. Art.);

- Cardiogenic shock;

- COPD;

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

-hypersensitivity to karvedilolu or other components of the drug.

FROM caution the preparation should be applied to strokes prinzmetala, thyrotoxicosis, occlusive peripheral vascular disease, pheochromocytoma, psoriaze, renal failure, AV-blockade I degree, extensive surgical interventions and general anesthesia, diabetes, gipoglikemii, depression, myasthenia.

Pregnancy and lactation

Adequate and well-controlled studies of application of carvedilol during pregnancy did not take place, Therefore, use of the drug in this category of patients is possible only in cases, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Breastfeeding is not recommended during treatment with carvedilol.

Cautions

Therapy should be long and not stop dramatically, especially in IBS, tk. This can lead to poor flow of main disease. If necessary dose should be reduced gradually, during 1-2 weeks.

At the beginning of therapy Akridilolom^® or if the dose of the drug in patients, particularly the elderly, There may be an excessive decline ad, mainly to stand up. In such cases, there is a need for dose adjustment.

In the treatment of chronic heart failure in the selection of doses may increase symptoms of congestive heart failure, the appearance of edema. However, do not increase the dose Akridilola^®, recommended appointment dioretikov in higher doses up to stabilize the patient's condition.

Recommended constant monitoring of ECG and hell while appointing Akridilola^® and blocking slow calcium channels, derived fenilalkilamina (verapamil) and benzotiazepina (diltiazem), and antiaritmicakimi means also I class.

It is recommended to monitor kidney function in patients with chronic renal insufficiency, arterial gipotenziei and chronic heart failure.

In the case of surgery using general anesthesia should notify anesthesiologist prior therapy of Akridilolom^®.

Akridilol^® does not affect the concentration of glucose in the blood and causes no changes in glucose tolerance test in patients with non-insulin-dependent diabetes mellitus.

Patients with pre-treatment feohromotsytoma, you must assign Alpha-adrenoreceptor antagonists.

Patients, using contact lenses, should be considered, that the drug may cause reduction of slezootdeleniâ.

During treatment should avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

It is not recommended to drive the car at the beginning of therapy and when increasing doses of Akridilola^®. Should refrain from other activities, related to high concentration and psychomotor quick reactions.

Overdose

Symptoms: decrease in blood pressure (accompanied by dizziness or fainting, systolic BP below 80 mmHg.), bradycardia. Possibly wheezing due to bronchoconstriction and vomiting. In severe cases there may be cardiogenic shock, respiratory failure, confusion, conduction disorders.

Treatment: symptomatic therapy. Monitoring and correction of the vital indicators, if necessary – in the intensive care unit. Appropriate in/with the introduction of m-holinoblokatorov (atropyn), adrenomimetikov (epinephrine, norepinephrine).

Drug Interactions

Together with the use of carvedilol may potentiate the effects of other antigipertenziveh funds or drugs, which have gipotenzivny effect (nitrates).

When coupled with enalapril and diltiazem can develop violations conductivity heart and hemodynamics.

Inhibitors of microsomal oxidation (cimetidine) increase, and inductors (phenobarbital, rifampicin) weaken gipotenzivny effect of carvedilol.

While receiving carvedilol and digoxin increases the concentration of the latter and may increase time AV-holding.

Carvedilol may potentiate the action of insulin and oral gipoglikemicakih funds, When the symptoms of hypoglycemia (especially the tachycardia) can camouflage, Therefore, in patients with diabetes it is recommended that regular monitoring of blood glucose levels.

Preparations, reduced catecholamine (reserpine, MAO inhibitors), increase the risk of arterial hypotension and bradycardia.

While the application of Cyclosporine increases the concentration of the latter (correction is recommended daily dose of Cyclosporine).

The simultaneous appointment of clonidine may potentiate the hypotensive and negative hronotropony effects of carvedilol.

General anesthetics are deepening the negative inotropy and hypotensive effects of carvedilol.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in a dry, protected from light, reach of children, at a temperature no higher than 25 ° C. Shelf life – 3 year.