Universal reference book for medicines
Product name: LODOZ (LODOZ)

Active substance: bisoprolol, hydrochlorothiazide

Type: Antihypertensive drug

Manufacturer: MERCK SANTE (France)
Composition, form of production and packaging
The tablets covered with a cover of
yellow color, film;
round, biconcave, with engraving in the form of the heart on one side and the number "2.5" on the other.
1 tab.

bisoprolol hemifumarate (bisoprolol fumarate (2: 1)) 2.5 mg

hydrochlorothiazide 6.25 mg

Excipients: magnesium stearate 1.0 mg, crospovidone 3.0 mg, corn starch 6.75 mg, corn starch, pre-gelatinized 6.75 mg, microcrystalline cellulose 37.5 mg, calcium phosphate monosubstituted 75.0 mg.

The composition of the shell: 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.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
The tablets covered with a cover of pink color, film;
round, biconcave, with engraving in the form of the heart on one side and the number "5" on the other.
1 tab.

bisoprolol hemifumarate (bisoprolol fumarate (2: 1)) 5 mg

hydrochlorothiazide 6.25 mg

Excipients: silicon dioxide colloid - 0.5 mg, magnesium stearate - 2 mg, corn starch - 10 mg, microcrystalline cellulose - 10 mg, calcium phosphate monosubstituted - 136.25 mg.

The composition of the shell: polysorbate 80 VS 0.045 mg, iron oxide yellow 0.0126 mg, iron oxide red 0.045 mg, macrogene 400 0.36 mg, titanium dioxide 1.3329 mg, hypromellose 2910/3 1.35225 mg, hypromellose 2910/5 1.35225 mg.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
The tablets covered with a cover of white color, film;
round, biconcave, with engraving in the form of the heart on one side and the number "10" on the other.
1 tab.

bisoprolol hemifumarate (bisoprolol fumarate (2: 1)) 10 mg

hydrochlorothiazide 6.25 mg

Excipients: silicon dioxide colloid - 0.5 mg, magnesium stearate - 2 mg, corn starch - 10 mg, microcrystalline cellulose - 10 mg, calcium phosphate monosubstituted - 131.25 mg.

The composition of the shell: polysorbate 80 VS - 0.045 mg, macrogol 400 - 0.36 mg, titanium dioxide - 1.40625 mg, hypromellose 2910/3 - 1.34438 mg, hypromellose 2910/5 - 1.34438 mg.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

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 associated, first of all, with a decrease in the level of renin in the blood plasma and a decrease in heart rate.
Hydrochlorothiazide is a diuretic from the group of thiazides with an antihypertensive effect.
Its diuretic effect is due to the inhibition of the transport of sodium ions from the renal tubules into the blood, thus preventing its reabsorption.
In clinical studies, potentiation of the effects of the active substances of this combination was observed.
Efficacy for the treatment of mild to moderate degree of hypertension was noted even when used in the lowest doses - 2.5 mg + 6.25 mg.
Side effects such as hypokalemia (with hydrochlorothiazide) and bradycardia, asthenia and headache (with bisoprolol) are dose-dependent.
Therefore, to reduce unwanted effects, the amount of each active ingredient in Lodose is reduced by a factor of 2-4.
PHARMACOKINETICS

Bisoprolol

Suction and distribution

T max in blood plasma ranges from 1 to 4 hours. Binding to plasma proteins is about 30%.

Metabolism and excretion

40% of bisoprolol is metabolized in the liver.
Metabolites are inactive.
T 1/2 of blood plasma is 11 hours. Kidney and liver clearance are equivalent.
Half of the administered dose is excreted in the urine both in unchanged form and in the form of metabolites. The total ground clearance is about 15 l / h.
Hydrochlorothiazide

Suction and distribution

Bioavailability of hydrochlorothiazide ranges from 60% to 80%.
T max in blood plasma is about 4 hours (from 1.5 to 5 hours). Binding to plasma proteins - 40%.
Hydrochlorothiazide penetrates the placental barrier, excreted in breast milk.

Metabolism and excretion

Hydrochlorothiazide is not metabolized and almost completely eliminated in unmodified form by glomerular filtration and active tubular secretion.
T 1/2hydrochlorothiazide is about 8 hours.
Pharmacokinetics in special clinical cases

In the case of renal and heart failure, in elderly patients renal clearance of hydrochlorothiazide decreases, T 1/2 increases.

INDICATIONS

- Arterial hypertension of mild and moderate severity.

DOSING MODE

Lodose 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 dose of the drug should be selected individually, using the following dosages of the drug Lodose:

- 2.5 mg of bisoprolol / 6.25 mg of hydrochlorothiazide;

- 5 mg of bisoprolol / 6.25 mg of hydrochlorothiazide;

- 10 mg of bisoprolol / 6.25 mg of hydrochlorothiazide.

The initial dose corresponds to 1 table.
(2.5 mg bisoprolol / 6.25 mg hydrochlorothiazide) 1 time / day. In case of insufficient effectiveness of treatment, the dose is increased to 1 tab. (5 mg of bisoprolol / 6.25 mg of hydrochlorothiazide) 1 time / day. If necessary, the dose can be increased to 1 tab. (10 mg of bisoprolol / 6.25 mg of hydrochlorothiazide) 1 time / day.
In patients with impaired hepatic function or moderate renal dysfunction (CK> 30 mL / min), dose changes are not required.

SIDE EFFECT

The drug is usually well tolerated.
Side effects are described in less than 10% of cases.
From the side of the central nervous system: sleep disorders, depression;
possible - fatigue, fatigue, dizziness, headache (may occur at the beginning of treatment and usually take place during the first or second week of treatment).
From the cardiovascular system: bradycardia, violation of AV-conduction, exacerbation of chronic heart failure, orthostatic hypotension.

On the part of the respiratory system: bronchospasm in patients with bronchial asthma or COPD in anamnesis.

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

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

From the musculoskeletal system: a feeling of cold and numbness of the limbs, muscle weakness, convulsions.

From the sense organs: hearing impairment, decreased production of lacrimal glands (must be taken into account by patients using contact lenses), visual impairment.

On the part of the metabolism: hypertriglyceridemia, hypercholesterolemia, hyperglycemia, glucosuria, hyperuricemia, disturbance of the water-electrolyte state, metabolic alkalosis.

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

From the skin: beta adrenoblockers can cause or aggravate the course of psoriasis or cause psoriasis-like rashes, alopecia.

Other: impotence, allergic rhinitis.

CONTRAINDICATIONS

- severe forms of bronchial asthma, COPD;

- Chronic heart failure in the stage of decompensation, not amenable to drug therapy;

- cardiogenic shock;

- SSSU, incl.
sinoatrial blockade;
- AV blockade II and III degree without artificial pacemaker;

- pronounced bradycardia (heart rate <50 bpm);

- Variable angina (Prinzmetal angina);

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

- severe forms of peripheral circulation disorders (including Raynaud's disease);

- arterial hypotension;

- hypokalemia;

- hypovolemia;

- severe renal dysfunction (CK <30 ml / min);

severe hepatic impairment;

- simultaneous use with floktaphenin, sultopride, antiarrhythmics, lithium preparations;

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

- hypersensitivity to bisoprolol and other components of the drug;

- hypersensitivity to hydrochlorothiazide and other sulfonamides.

With caution should be used with AV-blockade I degree, psoriasis, IHD, chronic heart failure in the stage of decompensation, thyrotoxicosis, water-electrolyte disorders (hyponatremia, hypokalemia, hypercalcemia), gout, in elderly patients.

PREGNANCY AND LACTATION

It is not recommended to use Lozose during pregnancy, because it contains a diuretic from the group of thiazides.

At present, it is not known whether bisoprolol is excreted in breast milk.
Diuretics from the thiazide group are excreted in breast milk. Breastfeeding during treatment with Lodose is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with moderate renal dysfunction (CK> 30 mL / min), dose changes are not required.

The drug is contraindicated in cases of severe impairment of kidney function (CK <30 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with impaired liver function, dose changes are not required.

The drug is contraindicated in severe violations of liver function.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

Caution should be used in elderly patients.

SPECIAL INSTRUCTIONS

Precautions associated with the use of bisoprolol

Do not suddenly stop treatment, especially in patients with ischemic heart disease.
The dose is recommended to be reduced gradually within 2 weeks. If necessary, simultaneous initiation of appropriate therapy to prevent angina attacks should be started.
If it is necessary to prescribe the drug to patients with bronchial asthma or COPD, treatment should begin with a minimum initial dose.
Before the start of therapy, functional respiratory tests are recommended. In the case of development of bronchospasm during therapy, beta-adrenomimetics should be prescribed.
Patients with chronic heart failure drug should be administered with caution and under the supervision of a doctor, in minimum doses.

It is necessary to reduce the dose of the drug at a heart rate at rest <50-55 bpm and in the presence of clinical symptoms of bradycardia.

Given the negative dromotropic effect of beta-blockers, they should be administered with caution to patients with grade I AV blockade.

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

Patients with pheochromocytoma should not be prescribed Lodose until treatment with alpha-blockers is performed.
Need control of blood pressure.
In elderly patients, treatment should begin with a low dose of the drug, careful monitoring of the patient's condition is necessary.

Patients taking Lodose should be warned about the possibility of hypoglycemia and the need for regular monitoring of blood glucose levels.
Bisoprolol may mask symptoms of hypoglycemia (tachycardia, palpitation, and increased sweating).
On the background of therapy with beta-blockers, the exacerbation of psoriasis is possible.
Bisoprolol should only be prescribed if necessary.
If anamnesis is indicated for anaphylactic reactions, regardless of the cause of their occurrence, especially with fllctafenin, or with desensitizing therapy, treatment with beta-blockers may aggravate the occurrence of these reactions and cause the development of resistance to epinephrine (adrenaline) treatment in usual doses.

Athletes should be informed that Lodose contains an active substance that can give positive results in doping tests.

Precautions associated with the use of hydrochlorothiazide

Before starting further regularly during therapy and monitoring the level of sodium in the blood.
Decrease in the level of sodium at the beginning of treatment can be asymptomatic, therefore regular monitoring is necessary. Particular attention is required in the presence of risk factors, for example, patients of senile age, patients with cirrhosis of the liver.
Control of potassium in blood is required in patients at high risk, 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, extended QT interval.

Hypokalemia increases the risk of arrhythmias, the toxicity of cardiac glycosides.
The first determination of the level of potassium in the blood should be done during the first week of Lodose therapy.
Thiazide diuretics can reduce the excretion of calcium in the urine, which leads to minor and temporary hypercalcemia.
Temporary hypercalcemia may be associated with undiagnosed hyperparathyroidism. Before the study of parathyroid function, treatment with thiazides should be discontinued.
It is necessary to control the blood glucose level in patients with diabetes mellitus, especially in the case of hypokalemia.

In patients with hyperuricemia, the risk of developing gout attacks is increased: the dose of the drug must be selected individually.

Thiazide diuretics are effective in normal kidney function or a slightly reduced renal function (CC <60 mL / min, serum creatinine> 2.5 mg / dl or> 220 μmol / L).
In elderly patients, QC can be calculated taking into account the age, body weight and sex of the patient according to the Cockcroft formula:
For men: CK (ml / min) = [140-age]?
body weight (kg) /0.814? serum creatinine (μmol / L)
For women: the value obtained?
0.85
Hypovolemia (loss of fluid and sodium), resulting from the use of diuretics at the beginning of therapy, leads to a decrease in glomerular filtration, which leads to an increase in the level of urea and creatinine in the blood in patients with normal renal function.

Temporary impairment of kidney function occurs without consequences in patients with normal renal function.
In patients with impaired renal function, there may be an increase in existing disorders.
In case of prescribing with another antihypertensive drug, a dose reduction at the beginning of treatment is recommended.

Use in Pediatrics

The effectiveness and safety of the drug in children and adolescents under the age of 18 years are not established, so the use of the drug is contraindicated.

Impact on the ability to drive vehicles and manage mechanisms

Use with caution when driving and working with machinery in connection with the possibility of developing dizziness.

OVERDOSE

Symptoms: excessive decrease in blood pressure, bradycardia.
In newborns from mothers who received treatment with beta-blockers, it is possible to develop an overdose, manifested by cardiac decompensation.
Treatment: in the case of severe bradycardia or excessive reduction of blood pressure in / inject the following medicines: atropine in a dose of 1-2 mg;
glucagon in a dose of 1 mg slowly bolus and then, if necessary, in the form of an infusion at a dose of 1-10 mg / h; further, if necessary, enter either epinephrine (adrenaline) at a dose of 15-85 mcg, the administration can be repeated, its total amount should not exceed 300 mcg, or dopamine at a dose of 2.5-10 mcg / kg / min.
When an overdose in newborns, manifested by cardiac decompensation, appoint glucagon at a rate of 0.3 mg / kg;
epinephrine (adrenaline) and dobutamine (usually in high doses) it is necessary to ensure observation in the ICU of newborns. Long-term treatment is carried out under the supervision of a specialist.
DRUG INTERACTION

The drug is contraindicated for use in combination with floktaphenin, sultopride.

The drug is not recommended 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 with baclofen, inhaled halogenated general anesthetics, slow calcium channel blockers (bepridil, diltiazem, verapamil), antiarrhythmics (propafenone, quinidine, hydroquinidine, disopyramide), insulin, urea preparations, lidocaine, iodine-containing contrast agents, anticholinesterase drugs, high doses of salicylates, drugs that cause hypokalemia - amphotericin (iv) and mi
non-corticoid (systemic administration), tetracosactide, laxatives; cardiac glycosides, diuretics causing hyperkalemia (amiloride, canrenone, spironolactone, triamterene); ACE inhibitors, metformin.
It is possible to intensify the hypotensive effect with simultaneous use of tricyclic antidepressants (including imipramine), neuroleptics, slow calcium channel blockers with dihydropyridine derivatives (including amlopidine, felopidine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine).

Application of Lodose simultaneously with tricyclic antidepressants, incl.
inhibitors of MAO, as well as neuroleptics, is not a contraindication. At the same time, their combined use should be taken into account, since a reduction in the dose of the antihypertensive agent due to additive hypotensive effect may be required.
With a joint appointment with mefloquine, bradycardia may develop.

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

When co-administered with cyclosporine, an increase in serum creatinine is possible.

It is possible to reduce the hypotensive effect of Lodose with simultaneous administration with SCS (for systemic administration), NSAIDs and tetracosactide.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of 18 ° to 25 ° C.
Shelf life - 3 years.
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