Lodoz, pills 2.5mg+6.25mg 30pcs

Composition

of 1 tab. bisoprolol hemifumarate (bisoprolol fumarate (2: 1)) 2.5 mg; hydrochlorothiazide 6.25 mg

Auxiliary substances:

magnesium stearate-1.0 mg,

crospovidone-3.0 mg,

corn starch-6.75

mg, pre-gelatinized corn starch-6.75 mg,

microcrystalline cellulose-37.5 mg,

single-substituted calcium phosphate-75.0 mg.

Shell composition:

polysorbate 80 VS – 0.035 mg, iron oxide yellow-0.089 mg, macrogol 400-0.280 mg, titanium dioxide-0.891 mg, hypromellose 2910/3-1.1025 mg, hypromellose 2910/6-1.1025 mg

Pharmacological action

Combined antihypertensive drug.

Bisoprolol is a highly selective beta-1-adrenoblocker without sympathomimetic and membrane-stabilizing activity. The mechanism of action of bisoprolol in arterial hypertension is primarily associated with a decrease in the level of renin in blood plasma and a decrease in heart rate.

Hydrochlorothiazide is a thiazide diuretic with an antihypertensive effect. Its diuretic effect is due to the inhibition of the transport of sodium ions from the renal tubules to the blood, thereby preventing its reabsorption.

In clinical studies, potentiation of the effects of active substances in this combination was observed. Efficacy for the treatment of mild to moderate arterial hypertension was noted even when used in the lowest doses-2.5 mg + 6.25 mg.

Side effects, such as hypokalemia (when using hydrochlorothiazide) and bradycardia, asthenia and headache (when using bisoprolol), are dose-dependent. Therefore, to reduce undesirable effects, the amount of each active ingredient in Lodose is reduced by 2-4 times.

Indications

Arterial hypertension of mild and moderate severity.

Use during pregnancy and lactation

It is not recommended to use this combination drug during pregnancy, because it contains a diuretic from the thiazide group.

It is currently unknown whether bisoprolol is excreted in breast milk.

Diuretics from the thiazide group are excreted in breast milk, and therefore breast-feeding during treatment with Lodoz is contraindicated.

There are no data on the use of the drug in children, so it is not recommended for use in pediatrics.

Contraindications

-Severe forms of bronchial asthma, COPD. – Chronic heart failure in the stage of decompensation, which does not respond to drug therapy. – Cardiogenic shock. – SSR, including sinoatrial block. -Grade II and III AV block without an artificial pacemaker. – Severe bradycardia (HR-Variant angina pectoris (Prinzmetal angina pectoris). – Pheochromocytoma (without simultaneous use of alpha-blockers). – Severe forms of peripheral circulatory disorders (including Raynaud’s disease). – Arterial hypotension. – Hypokalemia. – Hypovolemia. – Severe renal impairment (creatinine clearance – Severe hepatic impairment. – Concomitant use with floctafenin, sultoprid, antiarrhythmic agents, lithium preparations-Children and adolescents under 18 years of age (efficacy and safety have not been established). – Hypersensitivity to bisoprolol and other components of the drug. – Hypersensitivity to hydrochlorothiazide and other sulfonamides.

It should be used with caution in patients with grade I AV block, psoriasis, CHD, decompensated chronic heart failure, thyrotoxicosis, water and electrolyte disorders (hyponatremia, hypokalemia, hypercalcemia), gout, as well as in elderly patients.

Side effects

From the central nervous system:  sleep disorders, depression; possible – fatigue, tiredness, dizziness, headache (may occur at the beginning of treatment and usually disappear during the first or second week of treatment).

From the cardiovascular system:  bradycardia, impaired AV conduction, exacerbation of chronic heart failure, orthostatic hypotension.

Respiratory system disorders:  bronchospasm in patients with a history of asthma or COPD

From the digestive system:  nausea, vomiting, diarrhea, constipation, hepatitis, jaundice, increased AST and ALT activity.

From the urinary system:  reversible increase in serum creatinine and urea levels.

Musculoskeletal disorders:  feeling of cold and numbness of the extremities, muscle weakness, cramps.

From the side of the senses:  hearing disorders, reduced production of lacrimal glands (should be considered for patients using contact lenses), visual impairment.

From the side of metabolism:  hypertriglyceridemia, hypercholesterolemia, hyperglycemia, glucosuria, hyperuricemia, violation of the water-electrolyte state, metabolic alkalosis.

From the hematopoietic system:  leukopenia, thrombocytopenia.

Dermatological reactions:  beta-blockers can cause or exacerbate the course of psoriasis or cause psoriasis-like rashes, alopecia.

Other services:  impotence, allergic rhinitis.

The drug is usually well tolerated. Side effects are described in less than 10% of cases.

Interaction

The drug is contraindicated for use in combination with floctafenin, sultoprid.

The drug is not recommended for use in combination with amiodarone, lithium or with agents that can initiate arrhythmias (astemizole, bepridil, erythromycin, halofantrine, pentamidine, sparfloxacin, terfenadine, vincamycin).

Caution is required when using the drug concomitantly with baclofen, inhaled halogenated general anesthetics, slow calcium channel blockers (bepridil, diltiazem, verapamil), antiarrhythmic agents (propafenone, quinidine, hydroquinidine, disopyramide), insulin, urea preparations, lidocaine, iodine – containing contrast agents, anticholinesterase agents, high doses salicylates, drugs that cause hypokalemia-amphotericin (iv use) and mineralocorticoids (systemic use), tetracosactide, laxatives; cardiac glycosides, diuretics that cause hyperkalemia (amiloride, canrenone, spironolactone, triamterene); ACE inhibitors, metformin.

It is possible to increase the hypotensive effect with the simultaneous use of tricyclic antidepressants (including imipramine), neuroleptics, slow calcium channel blockers with dihydropyridine derivatives (including amlopidine, felopidine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine).

The use of Lodoz simultaneously with tricyclic antidepressants, including MAO inhibitors, as well as neuroleptics, is not a contraindication. At the same time, their combined use should be taken into account, since it may be necessary to reduce the dose of the antihypertensive agent due to the additive antihypertensive effect.

When co-administered with mefloquine, bradycardia may develop.

When co-administered with calcium preparations, hypercalcemia may develop.

When co-administered with cyclosporine, it is possible to increase the content of serum creatinine.

It is possible to weaken the hypotensive effect of Lodoz when co-administered with corticosteroids (for systemic use), NSAIDs and tetracosactide.

How to take, course of use and dosage

Lodoz is recommended to be taken in the morning (during meals). Tablets should be swallowed whole with a small amount of liquid and not chewed.

The initial dose corresponds to 1 tablet (2.5 mg bisoprolol/6.25 mg of hydrochlorothiazide) 1 time/ In case of insufficient effectiveness of treatment, the dose is increased to 1 tablet (5 mg bisoprolol/6.25 mg of hydrochlorothiazide) 1 time/ If necessary, the dose can be increased to 1 tablet (10 mg bisoprolol/6.25 mg of hydrochlorothiazide) 1 time/

No dose adjustment is required in patients with hepatic impairment or moderate renal impairment (creatinine clearance>30 ml / min).

Overdose

Symptoms:  excessive lowering of blood pressure, bradycardia. Newborns from mothers treated with beta-blockers may develop overdose, which is manifested by decompensation of cardiac activity.

Treatment:  in the case of severe bradycardia or an excessive decrease in blood pressure, the following medications are administered intravenously: atropine at a dose of 1-2 mg; glucagon in a dose of 1 mg bolus slowly and then, if necessary, in the form of infusion in a dose of 1-10 mg/h; further, if necessary, enter either epinephrine (adrenaline) in the 15-85 mcg dose, the introduction can be repeated, the total number should not exceed 300 µg, or dopamine at a dose of 2.5-10 µg/kg/min.

In case of overdose in newborns, manifested by decompensation of cardiac activity, glucagon is prescribed at the rate of 0.3 mg / kg; epinephrine (epinephrine) and dobutamine (usually in high doses) should be monitored in the ICU of newborns. Long-term treatment is carried out under the supervision of a specialist.

Special instructions

Treatment should not be abruptly discontinued, especially in patients with CHD. It is recommended to reduce the dose gradually over 2 weeks. If necessary, appropriate therapy should be initiated simultaneously to prevent angina attacks. If it is necessary to prescribe the drug to patients with bronchial asthma or COPD, start treatment with the minimum initial dose. Functional breath tests are recommended before starting therapy. If bronchospasm develops during therapy, beta-adrenomimetics should be prescribed.

In patients with chronic heart failure, the drug should be prescribed with caution and under the supervision of a doctor, in minimal doses.

Taking into account the negative dromotropic effect of beta-blockers, they should be prescribed with caution to patients with grade I AV blockade.

In patients with peripheral circulatory disorders (Raynaud’s disease), beta-blockers can cause an exacerbation of the course of the disease.

Patients with pheochromocytoma should not be prescribed Lodoz until they are treated with alpha-blockers. Blood pressure monitoring is required.

In elderly patients, treatment should begin with a low dose of the drug, and careful monitoring of the patient’s condition is necessary.

Patients taking Lodoz should be warned about the possibility of hypoglycemia and the need for regular monitoring of blood glucose levels. Bisoprolol may mask the symptoms of hypoglycemia (tachycardia, palpitations, and increased sweating).

Against the background of therapy with beta-blockers, an exacerbation of the course of psoriasis is possible. Bisoprolol should be prescribed only when necessary.

If a history of anaphylactic reactions is indicated, regardless of the cause of their occurrence, especially when taking floctafenin, or during desensitizing therapy, treatment with beta-blockers can exacerbate the occurrence of these reactions and cause the development of resistance to treatment with epinephrine (epinephrine) in normal doses. Athletes should be informed that Lodoz contains an Active ingredient that can give positive results during doping tests.

Precautions related to the use of hydrochlorothiazide:

Before starting treatment, regularly during therapy and monitoring of blood sodium levels is necessary. A decrease in sodium levels at the beginning of treatment may be asymptomatic, so regular monitoring is necessary. Special attention is required in the presence of risk factors, for example, senile patients, patients with cirrhosis of the liver.

It is necessary to monitor blood potassium in high-risk patients, for example, in elderly patients, in patients receiving thiazide and thiazide-like diuretics, as well as in patients with cirrhosis accompanied by edema, ascites, in patients with coronary artery disease or with heart failure, an extended QT interval.

Hypokalemia increases the risk of arrhythmias, toxicity of cardiac glycosides. The first determination of the level of potassium in the blood should be carried out during the first week of therapy with Lodosis.

Thiazide diuretics may reduce urinary calcium excretion, resulting in minor and temporary hypercalcemia. Temporary hypercalcemia may be associated with undiagnosed hyperparathyroidism. Treatment with thiazides should be discontinued before parathyroid function is evaluated.

It is necessary to monitor blood glucose levels in patients with diabetes mellitus, especially in the case of hypokalemia.

Patients with hyperuricemia have an increased risk of developing gout attacks: the dose of the drug should be selected individually. Thiazide diuretics are effective in patients with normal renal function or slightly reduced renal function (creatinine clearance 220 mmol / l). In elderly patients, serum creatinine can be calculated based on the age, body weight, and gender of the patient using the Cockcroft formula:

For men:Creatinine clearance (ml / min)= [140-age] x body weight (kg)/72 x serum creatinine (mg / dl)

For women: obtained value x 0.85 Hypovolemia (loss of fluid and sodium), which occurs due to the use of diuretics at the beginning of therapy, leads to a decrease in glomerular filtration, which leads to an increase in blood urea and creatinine levels in patients with normal renal function.

Temporary renal impairment occurs without consequences in patients with normal renal function. In patients with impaired renal function, existing disorders may increase.

If the drug is prescribed with another antihypertensive agent, it is recommended to reduce the dose at the beginning of treatment.

Use in pediatrics: The efficacy and safety of the drug in children and adolescents under 18 years of age have not been established, so the use of the drug is contraindicated.

Influence on the ability to drive motor vehicles and manage mechanisms:

use with caution when driving a car and working with mechanisms due to the possibility of developing dizziness.

Form of production

Coated tablets.

Storage conditions

At a temperature of 18-25 °C

Shelf life

3 years

Active ingredient

Bisoprolol, Hydrochlorothiazide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Arrhythmia