Aritel Plus - instructions for use, doses, side effects, contraindications

excipients for dosage of 5 mg + 6.25 mg: silicon dioxide colloid (aerosil) 2.1 mg, corn pregelatinized corn starch 23.9 mg, lactose (milk sugar) 70 mg, magnesium stearate 0.75 mg, microcrystalline cellulose 32 mg;

film coating: Selekoate AQ-02140/A 4 mg, including: hypromellose (hydroxypropylmethylcellulose) 2.2 mg, macrogol (polyethylene glycol 400) 0.36 mg, macrogol (polyethylene glycol 6000) 0.56 mg, titanium dioxide 0.84 mg, dye sunset yellow 0.04 mg.

excipients for dosage of 10 mg + 6.25 mg: silicon dioxide colloid (aerosil) 3 mg, corn pregelatinized starch 33 mg, lactose (milk sugar) 100 mg, magnesium stearate 1 mg, microcrystalline cellulose 46.75 mg;

composition of film shell: Selekoate AQ-02140/A 6 mg, including: hypromellose (hydroxypropylmethylcellulose) 3.3 mg, macrogol (polyethylene glycol 400) 0.54 mg, macrogol (polyethylene glycol 6000) 0.84 mg, titanium dioxide 1.26 mg, dye sunset yellow 0.06 mg.

Description:

The tablets covered with a film cover of yellow-orange color, round, biconcave. On the cross-section there are two layers: a shell of yellow-orange color, a core of white color.

Pharmacotherapeutic group:Antihypertensive drug combined (beta 1-blocker selective + diuretic)

ATX: & nbsp

C.07.B.B.07 Bisoprolol in combination with thiazides

Pharmacodynamics:

Aritel® Plus is a combined product that includes bisoprolol and hydrochlorothiazide.

Bisoprolol - selective beta₁-adrenoceptor without internal sympathomimetic activity. Has antihypertensive, antiarrhythmic and antianginal action. Blocking in low doses of beta₁(adenosine triphosphate (ATP)), reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect , reduces the excitability and contractility of the myocardium). As the dose increases, beta blocks₂-adrenoceptors.

The total peripheral vascular resistance at the beginning of beta-blockers application increases in the first 24 hours (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of beta stimulation₂-adrenoreceptors), after 1-3 days, returns to the initial, and with a long-term administration decreases.

The hypotensive effect is associated with a decrease in the minute volume of blood, suppression of sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system by inhibiting beta-adrenoreceptors of the juxtaglomerular renal apparatus (which leads to a decrease in renin secretion), restoration of the sensitivity of the aortic arch baroreceptorsactivity in response to a decrease in blood pressure) and influence on the central nervous system. With arterial hypertension, the effect develops after 2-5 days, stable effect - after 1-2 months.

Hydrochlorothiazide - Thiazide diuretic. Reduces the reabsorption of sodium ions in the cortical segment of the Henle loop, without affecting its area passing through the medulla of the kidney. It blocks carbonic anhydrase in the proximal part of the convoluted renal tubules, enhances the excretion of potassium ions, hydrocarbonates and phosphates by the kidneys. Virtually does not affect the acid-base state. Increases the excretion of magnesium ions by the kidneys; It detains calcium ions in the body and inhibits the excretion of urates. The diuretic effect develops after 1-2 hours, reaches a maximum after 4 hours, persists for 6-12 hours. The diuretic effect decreases with a decrease in the glomerular filtration rate and stops at a value of less than 30 ml / min.

Pharmacokinetics:

Bisoprolol

After ingestion, absorption from the gastrointestinal tract is 80-90%. Eating does not affect the degree of absorption. The time to reach the maximum concentration in the blood plasma is 2-4 hours.The connection with plasma proteins is about 30%.

Poorly penetrates the blood-brain and placental barrier. Secretion of breast milk is insignificant. Metabolised in the liver.

The half-life is 9-12 hours. It is excreted by the kidneys (50% in unchanged form), less than 2% by the intestine.

Hydrochlorothiazide

When ingested, absorbed quickly, but incomplete. The time to reach the maximum concentration in the blood plasma is about 4 hours. The bioavailability of hydrochlorothiazide is 60-80%. The connection with plasma proteins is 40%.

It penetrates the placental barrier, and is excreted into breast milk. It is not metabolized. It is excreted by the kidneys mainly unchanged through glomerular filtration and active tubular secretion. The half-life is about 8 hours.

Indications:

Arterial hypertension of mild to moderate severity.

Contraindications:

- Hypersensitivity to bisoprolol and other components of the drug;

- hypersensitivity to hydrochlorothiazide and other sulfonamides;

- bronchial asthma;

- chronic obstructive pulmonary disease;

- cardiogenic shock;

- syndrome of weakness of the sinus node (incl.sinoatrial blockade);

- atrioventricular blockade of II and III degree without artificial pacemaker;

- pronounced bradycardia (heart rate less than 50 beats per minute);

- Variable angina pectoris (Prinzmetal angina);

- pheochromocytoma (without simultaneous use of alpha-blockers);

- hard-to-control diabetes mellitus;

- late stages of peripheral circulatory disorders (including Raynaud's syndrome);

- severe arterial hypotension;

- refractory hypokalemia, hyponatremia, hypercalcemia;

- metabolic acidosis;

- hypovolemia;

- acute renal insufficiency;

- chronic renal failure (creatinine clearance (CK) less than 30 ml / min);

- simultaneous application with floktaphenin, sultopride;

- simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO type B inhibitors);

- age under 18 years (effectiveness and safety not established);

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- pregnancy;

- lactation period.

Carefully:

Carefully should be used in case of atrioventricular blockade of the first degree, ischemic heart disease, hepatic insufficiency,renal failure (QC more than 30 ml / min.); thyrotoxicosis, pheochromocytoma (against the background of treatment with alpha-adrenoblockers), water-electrolyte disorders (hyponatremia, hypokalemia, hypercalcemia); depression (including in the anamnesis), myasthenia gravis, gout, psoriasis, as well as in elderly patients.

Dosing and Administration:

Aritel® Plus is recommended in the morning (during meals). Tablets should be swallowed whole, not liquid, squeezed with a small amount of liquid, once a day.

The dose of the drug should be selected individually.

At the beginning of the treatment should take 1 tablet of the drug Aritel® Plus, containing 5 mg of bisoprolol / 6.25 mg hydrochlorothiazide 1 time / day. If the therapeutic effect is inadequate after 2 weeks, the dose can be increased by taking 1 tablet of the drug Aritel® Plus containing 10 mg of bisoprolol / 6.25 mg of hydrochlorothiazide, 1 time / day.

Patients with impaired liver function, as well as patients of advanced age, do not need to adjust the dosage regimen.

In patients with severe impairment of liver and kidney function (QC more than 30 ml / min), the maximum daily dose of bisoprolol should not exceed 10 mg.

Side effects:

From the central and peripheral nervous system: dizziness, headache, asthenia, sleep disorders, depression; increased fatigue, hallucinations, "nightmarish" dreams, convulsions; feeling of cold and numbness in the limbs.

From the cardiovascular system: bradycardia, orthostatic hypotension, violation of atrioventricular conduction, ventricular extrasystole, exacerbation of chronic heart failure.

From the respiratory system: bronchospasm (in predisposed patients).

From the digestive system: nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa; hepatitis.

From the musculoskeletal system: muscle weakness, spasms of the calf muscles, arthralgia.

From the sense organs: hearing impairment, decreased lacrimal gland production (must be taken into account by patients using contact lenses), visual impairment. On the part of the reproductive system: violation of potency (very rare).

On the part of the hematopoiesis system: leukopenia, thrombocytopenia.

Allergic reactions: skin itch, rash, reddening of the skin of the face, allergic rhinitis.

From the skin: increased sweating, alopecia, exacerbation of psoriasis.

From the laboratory indicators: increased activity of "hepatic" transaminases, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, glucosuria, hyperuricemia, reversible increase in creatinine and urea in the blood plasma.

Overdose:

Symptoms: marked decrease in blood pressure, bradycardia, acute heart failure, ventricular extrasystole, atrioventricular block, convulsions, bronchospasm.

LTreatment: gastric lavage, the appointment of absorbents, symptomatic therapy. In the case of a pronounced decrease in blood pressure, it is necessary to give the patient a horizontal position with elevated legs, to replenish the volume of circulating blood.

When bradycardia is intravenously administered atropine in a dose of 1-2 mg, glucagon in a dose of 1 mg (slowly bolus), if necessary - as an infusion in a dose of 1-10 mg / h. In the subsequent it is appointed epinephrine (epinephrine) at a dose of 15-85 μg (the administration of which can be repeated, but its total amount should not exceed 300 μg) or dopamine in a dose of 2.5-10 μg / kg / min.

In acute heart failure, cardiac glycosides, diuretics, glucagon. If there are no signs of pulmonary edema, then intravenously administered plasma-substituting solutions, if they are ineffective - epinephrine, dopamine, dobutamine.

When ventricular extrasystole is used lidocaine.

With the development of atrioventricular block, intravenous 1-2 mg of atropine, epinephrine, or a temporary pacemaker should be administered.

When convulsions are recommended diazepam intravenously.

When bronchospasm is inhaled, beta is injected₂-adrenomimetics.

Interaction:

With the simultaneous use of the drug Aritel® Plus with phenytoin (with intravenous administration) and drugs for inhalation of general anesthesia (derivatives of hydrocarbons), the cardiopepressive effect and the likelihood of excessive reduction in blood pressure (due to the content of bisoprolol) may increase.

The clearance of lidocaine and xanthine may decrease due to a possible increase in their concentrations in the blood plasma, especially in patients with initially elevated clearance of theophylline (due to the content of bisoprolol in the formulation).

With the simultaneous use of calcium and / or vitamin preparations D in high doses, hypercalcemia may develop and the risk of metabolic acidosis (due to the content of the drug hydrochlorothiazide) increases.

Aritel® Plus is contraindicated for use in combination with floktaphenin, sultopride, MAO inhibitors (with the exception of MAO type B inhibitors).

It is possible to increase the antihypertensive effect of the drug Aritel® Plus when used with antidepressants, antipsychotics, slow calcium channel blockers (amlodipine, felodipine, nifedipine, nicardipine, nimodipine, nitrendipine), angiotensin-converting enzyme inhibitors (incl. captopril, enalapril), irbesartan, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive agents.

It is possible to reduce the antihypertensive effect of the drug Aritel® Plus with simultaneous administration with glucocorticosteroids (for systemic administration), estrogens, nonsteroidal anti-inflammatory drugs (indomethacin, piroxicam, naproxen, phenylbutazone) and tetracosactide.

When used simultaneously with the drug Aritel® Plus, the effects of nondepolarizingmuscle relaxants and anticoagulant effect of coumarin derivatives.

Cardiac glycosides, methyldopa, reserpine, guanfacine, BCCC (verapamil, diltiazem, amlodipine, felodipine, nifedipine, nicardipine, nimodipine, nitrendipine), antiarrhythmics, as well as agents that can initiate arrhythmias such as pirouettes (astemizole, beprideil, erythromycin, halofantrine, pentamidine, sparfloxacin, terfenadine), increase the risk of developing and / or strengthening bradycardia, atrioventricular blockade and chronic heart failure. With simultaneous application with sotalol hypokalemia and development of ventricular arrhythmia such as "pirouette" is possible.

With the simultaneous use of the drug Aritel® Plus with lithium salts, it is possible to increase the concentration of the latter in the blood to a toxic level.

The effectiveness of insulin and hypoglycemic agents for oral administration may be reduced.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

With the simultaneous use of the preparation Aritel® Plus with allergens used for immunotherapy, or with extracts of allergens for skin tests,as well as with allopurinol or with iodine-containing radiopaque diagnostic agents for intravenous administration, the risk of allergic reactions increases.

With the simultaneous administration of the drug Aritel® Plus with mefloquine, bradycardia may develop; with carbamazepine - hyponatremia; with cyclosporine - an increase in serum creatinine is possible.

Sulfasalazine increases the concentration of bisoprolol in the blood plasma; rifampicin - shortens the half-life of bisoprolol.

Special instructions:

During the therapy with Arilit® Plus, heart and blood pressure control is necessary (at the beginning of treatment - every day, then - once every 3-4 months), for the glucose content in the blood in patients with diabetes mellitus (1 every 4-5 months). In elderly patients, it is recommended to monitor kidney function (1 every 4-5 months). It is necessary to teach the patient how to calculate heart rate. It is necessary to reduce the dose of the drug Aritel® Plus (by reducing the content of bisoprolol) from 10 to 5 mg, if the heart rate at rest does not exceed 50-55 beats / min.

In the period of therapy with the drug Aritel® Plus, it is also necessary to monitor the parameters of the acid-base state and the level of electrolytes (potassium, sodium, calcium).

In patients with impaired peripheral circulation, caution should be exercised when prescribing Arilit® Plus.

In thyrotoxicosis, Aritel® Plus (due to the bisoprolol content in it) can mask the clinical signs of the disease (for example, tachycardia).

Patients with pheochromocytoma should not be prescribed Aritel® Plus until treatment with alpha-blockers is prescribed. In this case, it is necessary to monitor blood pressure.

It is recommended to stop therapy with the drug Aritel® Plus with the development of depression caused by taking a beta-blocker (due to the content of bisoprolol in it).

In elderly patients, treatment with Arilit® Plus should be started with a dosage form containing a low dose of bisoprolol (5 mg). At the same time, regular monitoring of the patients' condition is necessary.

Particular attention is required in cases of surgical intervention under general anesthesia in patients taking beta-blockers. Such patients should cancel Arilit® Plus 48 hours prior to surgery, alert the anesthetist that the patient is taking Arilit® Plus.As a means for general anesthesia, a drug with a minimum negative inotropic effect should be chosen.

On the background of therapy with beta-blockers, the exacerbation of psoriasis is possible. Patients with this disease Aritel® Plus should be administered with caution.

If anamnesis is indicated for anaphylactic reactions, regardless of the cause of their occurrence, especially when conducting desensitizing therapy, treatment with Aritel® Plus (due to bisoprolol content) may increase the risk of allergic reactions and promote the development of resistance to epinephrine (adrenaline) treatment in usual doses.

Patients who use contact lenses should be careful when using the drug Aritel® Plus, as beta-blockers can reduce the production of tear fluid.

In patients with hyperuricemia, the risk of developing attacks of gout aggravation is increased. In this case, the dose of the drug Aritel® Plus should be selected individually under the control of the level of uric acid in the serum. Before the study of parathyroid gland function, treatment with Aritel® Plus should be stopped,since on the background of its reception, transitory hypercalcemia may occur.

Athletes should be informed that Aritel® Plus contains bisoprolol, which can give false positive results in the conduct of doping control.

Effect on the ability to drive transp. cf. and fur:

Arylit® Plus should be used with caution when operating vehicles and mechanisms due to the possibility of developing dizziness.

Form release / dosage:

Tablets, film-coated, 5 mg + 6.25 mg and 10 mg + 6.25 mg.

Packaging:

For 10, 15 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

According to 1, 3, 6 contour cell packs of 10 tablets or 2, 4 contour packs of 15 tablets each, or 1.2 circuit packs of 30 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007919/09

Date of registration:06.10.2009 / 18.10.2012

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp12.09.2017

Illustrated instructions

Instructions

Aritel® Plus (Arital® Plus)