Hydrochlorothiazide + Nebivolol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Diuretics

Beta-blockers

Included in the formulation

Nebilong H

pills inwards

Micro Labs Limited India

АТХ:

C.07.B.B.12 Nebivolol in combination with thiazides

Pharmacodynamics:

Combined antihypertensive.

Hydrochlorothiazide

The benzothiadiazepine derivative selectively blocks the transport system of sodium, potassium and chlorine ions, stopping their transport through the apical membrane into the cells of the epithelium of the thick segment of the ascending section of the Henle loop. The suppression of reabsorption of ions leads to their removal from the body. Simultaneously with ions of sodium, potassium and chlorine ions of calcium and magnesium are deduced. Hypocalcemia does not develop due to active reabsorption in the distal convoluted tubule of the loop of Henle.

Effective with any fluctuations in acid-base balance, retains a diuretic effect in both acidosis and alkalosis.

Nebivolol

The racemate of the dextrorotatory (D-nebivolol) and levorotatory (L-nebivolol) isomers. D-nebivolol is a highly selective competitive β₁-blocker, which does not have internal sympathomimetic activity. L-nebivolol due to interaction with L-arginine / nitric oxide (NO) has a moderate vasodilating effect.

Has antihypertensive, antiarrhythmic, antianginal action.In therapeutic doses, it does not have α-adrenoblocking and membrane-stabilizing action.

Reduces the effect of catecholamines on the heart muscle, thereby reducing the heart rate, minute and stroke volumes of blood.

Eliminates the effects of arrhythmogenic factors: tachycardia, arterial hypertension, increased content of cyclic AMP.

Antianginal action is due to a decrease in myocardial oxygen demand with prolonged diastole and improved perfusion of the heart muscle.

Pharmacokinetics:

Hydrochlorothiazide

After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 40%.

The therapeutic effect develops 2 hours after admission and lasts for 8-12 hours. Penetrates through the blood-brain and placental barrier, excreted in breast milk. Metabolism in the liver.

The elimination half-life is 6.4 hours. Elimination by the kidneys, about 75% in unmodified form.

Nebivolol

After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract.The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 98%.

Therapeutic effect develops in 2-5 days after the beginning of admission. Metabolism in the liver.

The half-life is 10-50 hours, depending on the genetically determined metabolic rate. Elimination by the kidneys.

Indications:

It is used for the treatment of arterial hypertension.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

IX.I10-I15.I15 Secondary Hypertension

Contraindications:

Severe renal and hepatic insufficiency, cardiogenic shock, bronchial asthma, pheochromocytoma, atrioventricular block II-IV degree, bradycardia, pregnancy and lactation, age under 18 years, individual intolerance.

Carefully:

Chronic heart failure, atrioventricular block I degree, chronic bronchitis with an asthmatic component, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category D. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside, 1 tablet (hydrochlorothiazide / nebivolol: 12.5 / 5 mg) once a day.If necessary, the dose can be increased to 2 tablets.

The highest daily dose: 2 tablets, hydrochlorothiazide / nebivolol: 25/10 mg.

The highest single dose: 2 tablets, hydrochlorothiazide / nebivolol: 25/10 mg.

Side effects:

Hydrochlorothiazide

Central and peripheral nervous system: headache, dizziness, depression, sleep disorders, paresthesia.

Respiratory system: pneumonitis, pulmonary edema.

Hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia, hemolytic anemia.

The cardiovascular system: orthostatic hypotension, rarely - arrhythmia.

Musculoskeletal system: spasms of the calf muscles.

Dermatological reactions: photosensitization, rash, rarely - toxic epidermal necrolysis.

Sense organs: visual impairment.

Urinary system: glycosuria, hyperuricemia.

Reproductive system: impotence.

Nebivolol

central nervous system: dizziness, insomnia, asthenia.

Respiratory system: shortness of breath, rarely - bronchospasm.

Hemopoietic system: neutropenia, thrombocytopenia.

The cardiovascular system: bradycardia, atrioventricular blockade, cold extremities.

Digestive system: indigestion, diarrhea, or constipation.

Sense organs: syndrome "dry eye ", transient visual impairment.

Reproductive system: lowering the potency.

Skin: Hyperhidrosis.

Allergic reactions.

Overdose:

Pronounced decrease in blood pressure, electrolyte imbalance, bradycardia, cardiovascular shock, renal failure.

Treatment: Intravenous 1-2 mg atropine, 2.5 μg / kg dobutamine, intravenously bolus 10 mg glucagon, intravenously drip 10-20 μg isoprenaline at a rate of not more than 5 μg / min.

Interaction:

Hydrochlorothiazide

Strengthens the effects of nondepolarizing muscle relaxants.

Patients with diabetes mellitus when using hydrochlorothiazide requires a correction of doses of oral hypoglycemic agents and insulin preparations.

Enhance the hypokalemic effect of glucocorticosteroids, adrenocorticotropic hormone, carbenoxolone, amphotericin, cardiac glycosides.

Anticholinergic drugs increase the bioavailability of hydrochlorothiazide.

With simultaneous use with lithium preparations, a paradoxical antidiuretic effect is possible.

With simultaneous application with vitamin D and calcium preparations may develop hypercalcemia.

With simultaneous use with cyclosporine, the risk of developing gout and hyperuricemia increases.

Nebivolol

Increases the concentration of ethanol in the blood and lengthens its excretion.

Potentiates the effect of lidocaine in systemic application.

The negative dromo-, foreign, chromotropic effect is intensified with simultaneous administration with amiodarone, anesthetics, antiarrhythmics, digoxin, diltiazem, verapamil.

Increases the bioavailability of nebivolol together with cimetidine.

Special instructions:

Discontinue taking the drug gradually (for 8-10 days).

Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Hydrochlorothiazide + nebivolol (Hydrochlorothiazidum + Nebivololum)