Lodoz tabs 2.5mg + 6.25mg #30

Instruction for use of Lodoz

You can buy Lodoz here

Lodoz is a combined drug with a diuretic, hypotensive effect, used in the treatment of arterial hypertension of mild to moderate severity.

Release form and composition

Dosage form of Lodoz release - film-coated tablets: biconvex, round, engraved on one side in the form of a heart; 2.5 mg + 6.25 mg - yellow, engraving on the other side "2.5"; 5 mg + 6.25 mg - pastel pink, engraved on the other side "5"; 10 mg + 6.25 mg - white, engraving on the other side "10" (in a cardboard box 3, 5 or 10 blisters of 10 pcs. In each).
Active ingredients in 1 tablet:
    bisoprolol hemifumarate 2.5; 5 or 10 mg;
    hydrochlorothiazide - 6.25 mg.
Additional components (2.5 mg + 6.25 mg / 5 mg + 6.25 mg / 10 mg + 6.25 mg): anhydrous calcium hydrogen phosphate, fine powder - 75 / 136.25 / 131.25 mg; magnesium stearate vs - 1/2/2 mg; anhydrous colloidal silicon dioxide - 0 / 0.5 / 0.5 mg; microcrystalline cellulose - 37.5 / 10/10 mg; corn starch, fine powder - 6.75 / 10/10 mg; crospovidone - 3/0/0 mg; pregelatinized corn starch - 6.75 / 0/0 mg.
Film sheath:
    2.5 mg + 6.25 mg: yellow Opadry (hypromellose 2910/3 - 1.102 5 mg; polysorbate 80 vs - 0.035 mg; dye iron oxide yellow - 0.089 mg; macrogol 400 - 0.28 mg; titanium dioxide - 0.891 mg ; hypromellose 2910/6 - 1.102 5 mg) - 3.5 mg;
    5 mg + 6.25 mg: pastel pink Opadry [dye iron oxide red (E172) - 0.045 mg; hypromellose 2910/3 - 1.352 25 mg; titanium dioxide - 1.332 9 mg; polysorbate 80 vs - 0.045 mg; dye iron oxide yellow (E172) - 0.012 6 mg; macrogol 400 - 0.36 mg; hypromellose 2910/5 - 1.352 25 mg] - 4.5 mg;
    10 mg + 6.25 mg: white Opadry (titanium dioxide - 1.406 25 mg; macrogol 400 - 0.36 mg; polysorbate 80 vs - 0.045 mg; hypromellose 2910/3 - 1.344 38 mg; hypromellose 2910/5 - 1.344 38 mg ) - 4.5 mg.

Pharmacodynamics

Lodoz is one of the combined drugs with antihypertensive action.
The main properties of active substances:
    bisoprolol: a highly selective β1-blocker without membrane stabilizing and sympathomimetic activity. The mechanism of its action in arterial hypertension is mainly associated with a decrease in the level of renin in the blood plasma and in the heart rate;
    hydrochlorothiazide: a thiazide diuretic with an antihypertensive effect. The diuretic effect of the substance is due to inhibition of the transport of sodium ions from the renal tubules into the blood, which prevents its reabsorption.

Pharmacokinetics

Bisoprolol

Almost in full (more than 90%) is absorbed from the gastrointestinal tract. The time to reach Cmax (maximum concentration of the substance) in blood plasma varies within 1–4 hours. Has a high bioavailability (88%) with a very low first pass effect through the liver. Food intake has no effect on this indicator. The kinetics for doses in the range of 5–40 mg is linear.
The connection with blood plasma proteins is about 30%, Vd (volume of distribution) is about 3 l / kg.
Approximately 40% of bisoprolol is metabolized in the liver to form inactive metabolites.
T1 / 2 (half-life) from blood plasma - 11 hours. Hepatic and renal clearance of a substance is approximately comparable. 50% of the dose is excreted unchanged by the kidneys, as well as metabolites. The total ground clearance is approximately 15 l / h.

Hydrochlorothiazide

After oral administration, about 80% of hydrochlorothiazide is absorbed from the gastrointestinal tract. Its bioavailability is in the range of 60-80%. Tmax (time to reach the maximum concentration of a substance) in blood plasma varies in the range of 1.5-5 hours (usually about 4 hours).
Communication with blood plasma proteins - 40%.
Hydrochlorothiazide is not metabolized and is almost completely excreted through active tubular secretion and glomerular filtration unchanged. T1 / 2 - approximately 8 hours.
Renal clearance of hydrochlorothiazide in cases of renal and heart failure decreases, T1 / 2 increases. In elderly patients, an increase in plasma Cmax is also possible.
The substance crosses the placenta and is excreted in breast milk.

Indications for use

Lodoz is prescribed for the treatment of mild to moderate arterial hypertension.

Contraindications

Absolute:
    cardiogenic shock;
    bronchial asthma and chronic obstructive pulmonary disease in severe forms;
    acute heart failure or chronic heart failure in the stage of decompensation, which requires inotropic therapy;
    sinoatrial blockade;
    sick sinus syndrome;
    AV block II and III degree without an artificial pacemaker;
    symptomatic bradycardia (with a heart rate of <50 beats / min);
    arterial hypotension (with systolic pressure <100 mm Hg);
    severe peripheral circulatory disorders, including Raynaud's syndrome;
    pheochromocytoma (without the simultaneous use of α-blockers);
    refractory hypokalemia;
    metabolic acidosis;
    liver dysfunction in severe course;
    renal dysfunction in severe course (in patients with creatinine clearance <30 ml / min);
    combined use with sultopride;
    age under 18;
    pregnancy and lactation;
    individual intolerance to any component of the drug, as well as other thiazides and sulfonamides.
Relative (Lodoz is prescribed under medical supervision):
    diabetes mellitus with significant fluctuations in blood glucose concentration;
    chronic heart failure;
    Prinzmetal's angina;
    AV block I degree;
    hypovolemia;
    peripheral circulatory disorders;
    hyperuricemia;
    impaired hepatic function;
    thyrotoxicosis;
    psoriasis;
    water-electrolyte disturbances (hypokalemia, hyponatremia, hypercalcemia);
    pheochromocytoma (during therapy with α-blockers);
    myasthenia gravis;
    depression, including a burdened history;
    angle-closure glaucoma;
    myopia;
    adherence to a strict diet;
    elderly age.

Instructions for use Lodoz: method and dosage

Lodoz tablets are taken orally, once a day, preferably in the morning before, during or after breakfast. The tablets should be swallowed without chewing, whole, washed down with a small amount of liquid.
The dose of the drug is determined individually.
Usually at the beginning of use, 1 tablet Lodoz 2.5 mg + 6.25 mg per day is prescribed. If necessary, it is possible to use a drug containing 5 or 10 mg of bisoprolol.
Lodoz is intended for continuous therapy.

Side effects

Possible adverse reactions (> 10% - very often;> 1% and <10% - often;> 0.1% and <1% - infrequently;> 0.01% and <0.1% - rarely; <0, 01%, including individual messages - very rare):
    metabolism and nutrition: infrequently - violation of water and electrolyte balance (including hyponatremia, hypokalemia, hypochloremia, hypomagnesemia, hypercalcemia), loss of appetite, hyperuricemia, hyperglycemia; very rarely, metabolic alkalosis;
    blood and lymphatic system: rarely - thrombocytopenia, leukopenia; very rarely - agranulocytosis;
    nervous system: often - dizziness, headache;
    psyche: infrequently - insomnia, depression; rarely - nightmares, hallucinations;
    organ of hearing and labyrinthine disorders: rarely - hearing impairment;
    organ of vision: rarely - visual impairment, decreased production of lacrimal fluid (must be taken into account when wearing contact lenses); very rarely - conjunctivitis;
    cardiovascular system: often - a feeling of coldness or numbness in the limbs; infrequently - bradycardia, violation of atrioventricular conduction, aggravation of symptoms of chronic heart failure, orthostatic hypotension; rarely - fainting;
    digestive system: often - diarrhea, nausea, vomiting, constipation; infrequently - abdominal pain; very rarely - pancreatitis;
    respiratory system: infrequently - bronchospasm in patients with a history of bronchial asthma / airway obstruction; rarely - allergic rhinitis; with an unknown frequency - interstitial pulmonary disease;
    liver and biliary tract: rarely - jaundice, hepatitis;
    skin and subcutaneous tissues: rarely - hypersensitivity reactions (including photodermatitis, sudden flushing of the face, skin rash / itching, purpura, urticaria); very rarely - alopecia, cutaneous lupus erythematosus; bisoprolol can cause a psoriasis-like rash or exacerbate the course of psoriasis;
    genitals and mammary gland: rarely - violation of potency;
    musculoskeletal system: infrequently - muscle cramps / weakness;
    laboratory / instrumental studies: infrequently - an increase in the concentration of amylase, triglycerides and cholesterol, a reversible increase in the concentration of serum creatinine and urea, glucosuria; rarely - an increase in the activity of aspartate aminotransferase and alanine aminotransferase;
    others: often - increased fatigue; infrequently - asthenia; very rarely - chest pain.

Overdose

The most common symptoms of an overdose of β-blockers include bradycardia, bronchospasm, a marked decrease in blood pressure, atrioventricular block, hypoglycemia, and acute heart failure.
The sensitivity to a single dose of high-dose bisoprolol varies widely among individual patients, and patients with chronic heart failure are likely to have increased sensitivity.
The most common symptoms of hydrochlorothiazide overdose are hypokalemia, hypovolemia, dizziness, drowsiness, nausea, hypotension. The clinical manifestations of acute / chronic overdose are due to significant loss of electrolytes or fluid.
In cases of overdose, first of all, you should stop taking Lodoz. Shows gastric lavage, the use of adsorbing agents and supportive symptomatic therapy.
Other activities (depending on symptoms):
    severe arterial hypotension: the appointment of vasopressors and intravenous administration of plasma-substituting solutions;
    severe bradycardia: intravenous administration of atropine; with insufficient efficiency, it is possible to carefully administer drugs with a positive chronotropic effect; in some cases, temporary installation of an artificial pacemaker is required;
    exacerbation of chronic heart failure: intravenous administration of vasodilators, diuretics, drugs with a positive inotropic effect;
    atrioventricular block II – III degree: therapy with β-adrenergic agonists under constant medical supervision; possibly the appointment of epinephrine; if necessary, the setting of an artificial pacemaker is shown;
    hypoglycemia: intravenous administration of a glucose solution (dextrose);
    bronchospasm: the use of bronchodilators, aminophylline and / or β2-adrenergic agonists.
There is limited information confirming that bisoprolol is excreted only to a small extent during hemodialysis. The degree of elimination of hydrochlorothiazide by hemodialysis has not been established.

Special instructions

Precautions related to bisoprolol

You should not suddenly interrupt therapy, especially in patients with coronary artery disease. The dose of Lodoz should be reduced gradually over a period of 14 days. If necessary, in order to prevent attacks of angina pectoris, the simultaneous implementation of appropriate therapy is indicated.
In case of bronchial asthma or chronic obstructive pulmonary disease in a mild course, Lodoz should be used at the beginning of therapy in a minimum dose. Functional breathing tests must be performed beforehand. In cases of symptomatic manifestation of these diseases, bronchodilating agents are simultaneously prescribed.
In patients with bronchial asthma, airway resistance may increase, while higher doses of β2-adrenergic agonists are required.
With compensated chronic heart failure, in which β-blockers are indicated, treatment should be started with the minimum doses of Lodoz, gradually increasing them under medical supervision.
If the patient's heart rate is less than 50–55 beats / min at rest, as well as in the presence of symptoms associated with bradycardia, the dose of the drug should be reduced.
Bisoprolol may increase the frequency and duration of vasospastic episodes in patients with Prinzmetal's angina. With mild / mixed manifestations of the disease, it is possible to use Lodoz in combination with vasodilators.
With violations of peripheral circulation or Raynaud's syndrome, taking bisoprolol can exacerbate the course of the disease.
The appointment of Lodoz to patients with pheochromocytoma is not recommended until therapy with α-blockers is performed. Patients need careful monitoring of blood pressure.
Therapy in elderly patients should be carried out under medical supervision.
In diabetes mellitus, the likelihood of developing hypoglycemia should be considered. At the beginning of treatment, you need to regularly monitor the concentration of glucose in the blood. Tachycardia, excessive sweating, palpitations and other symptoms of hypoglycemia (a pronounced decrease in glucose concentration) can be masked.
In patients with psoriasis, an exacerbation of its course is possible, and therefore bisoprolol can be prescribed only when necessary.
In the presence of a burdened history of anaphylactic reactions, regardless of the cause of their occurrence, especially when using iodine-containing contrast agents or conducting desensitizing treatment, taking bisoprolol can exacerbate the occurrence of these reactions and the emergence of resistance to the use of conventional doses of epinephrine (adrenaline).
Bisoprolol during general anesthesia reduces the risk of arrhythmia and myocardial ischemia during induction of anesthesia and intubation, as well as in the postoperative period. At present, it is recommended to continue taking β-blockers intraoperatively. The anesthesiologist should take into account the likelihood of β-adrenergic receptor blockade due to potential interactions with other drugs / substances, which can lead to bradyarrhythmias, suppression of reflex tachycardia and a decrease in the reflex ability to compensate for blood loss. In cases where therapy must be discontinued, the dose of Lodoz should be reduced gradually. Therapy should be completely completed no later than 48 hours before general anesthesia.
Symptoms of thyrotoxicosis during treatment with bisoprolol can be masked.
Combined use with verapamil, bepridil or diltiazem requires careful monitoring of the patient's condition and ECG, especially this warning applies to elderly patients and the period of initiation of therapy.

Hydrochlorothiazide-Related Precautions

Taking hydrochlorothiazide in patients with impaired hepatic function may cause the development of hepatic encephalopathy. In such cases, Lodoz should be canceled immediately.
Against the background of long-term treatment, it is recommended to regularly monitor the content of electrolytes in the blood serum (especially sodium, potassium, calcium), urea, creatinine, serum lipids (triglycerides and cholesterol), glucose and uric acid.
Long-term therapy can cause imbalance in water and electrolyte balance.
Before prescribing the drug and in the future, regular monitoring of the sodium content in the blood is required. Taking Lodoz can cause hyponatremia, sometimes with serious consequences.
A decrease in sodium content at the beginning of therapy may be asymptomatic, which requires regular monitoring; patients at high risk need special attention, for example, patients with cirrhosis of the liver, elderly patients.
The greatest risk associated with taking hydrochlorothiazide is potassium loss (<3.5 mmol / L) leading to hypokalemia. Frequent monitoring of blood potassium is necessary in high-risk patients. The first determination of the plasma potassium content in the blood should be carried out during the first week of therapy.
Hydrochlorothiazide can reduce urinary calcium excretion, resulting in temporary and minor hypercalcemia. With significant hypercalcemia, undiagnosed hyperparathyroidism can be assumed. Before conducting a study of the function of the parathyroid glands, taking Lodoz should be discontinued.
In patients with diabetes mellitus, especially in the case of hypokalemia, monitoring of the concentration of glucose in the blood is required.
With hyperuricemia, the likelihood of gout attacks increases, therefore, for this group of patients, the dose of Lodoz should be selected individually.
Hydrochlorothiazide is effective in normal / slightly reduced renal function (in adults, creatinine clearance> 25 mg / ml or 220 μmol / l).
Hypovolemia, in combination with the loss of fluid and sodium, resulting from the use of diuretics at the beginning of therapy, can lead to a decrease in glomerular filtration, which in turn causes an increase in serum urea and creatinine in the blood in patients with intact renal function. In patients with impaired renal function, existing impairments may worsen; with normal renal function, temporary impairments usually proceed without consequences.
In the case of the appointment of Lodoz with another antihypertensive agent, a dose reduction is recommended, at least at the beginning of therapy.
Taking hydrochlorothiazide may cause photosensitivity reactions. When they appear, protect sensitive areas from artificial UV / sunlight. In severe cases, Lodoz is canceled.
Hydrochlorothiazide, like sulfonamide, can cause idiosyncratic reactions that manifest as acute angle-closure glaucoma / short-term myopia. Symptoms include eye pain or a sharp drop in visual acuity. The duration of the disturbance can vary from a few hours to several weeks from the start of Lodoz. Lack of therapy for angle-closure glaucoma can cause permanent vision loss. First of all, hydrochlorothiazide should be discontinued as soon as possible. In severe cases, it is possible to prescribe an operative surgical or medical treatment. Risk factors for the development of angle-closure glaucoma include a burdened history of allergic reactions to penicillin or sulfonamide derivatives.

Precautions related to bisoprolol and hydrochlorothiazide

Athletes should take into account that Lodoz contains active ingredients that can give positive results during doping tests.
Influence on the ability to drive vehicles and complex mechanisms
During therapy, patients need to take into account the likelihood of an individual body reaction to Lodoz, especially at the beginning of therapy, when changing the drug, and also in cases of simultaneous alcohol consumption.

Application during pregnancy and lactation

The use of Lodoz during pregnancy is not recommended, since it contains a diuretic from the thiazide group. The use of diuretics can lead to placental ischemia with a concomitant risk of fetal malnutrition. There is an assumption that hydrochlorothiazide causes thrombocytopenia in newborns.
There is no information about whether bisoprolol is excreted in breast milk. Diuretics from the thiazide group are excreted in breast milk, and therefore breastfeeding while taking the drug is not recommended. Hydrochlorothiazide can suppress the secretion of breast milk.

Childhood use

For patients under the age of 18, Lodoz is not prescribed, since there is no information on the use of the drug in this group of patients.

With impaired renal function

Contraindication: severe renal dysfunction (with creatinine clearance <30 ml / min).

For violations of liver function

Contraindication: severe liver dysfunction.

Use in the elderly

According to the instructions, Lodoz should be used with caution in elderly patients.

Drug interactions

The combined use of Lodoz with sultopride is contraindicated, since bisoprolol may increase the likelihood of ventricular arrhythmias.
Combinations to avoid:
    lithium: an increase in its cardiotoxic and neurotoxic effects, a decrease in excretion from the body (due to hydrochlorothiazide);
    calcium channel blockers such as verapamil and, to a lesser extent, diltiazem: decreased myocardial contractility and impaired AV conduction (due to bisoprolol);
    antihypertensive agents of central action (moxonidine, clonidine, methyldopa, rilmenidine): a decrease in heart rate and a decrease in cardiac output, as well as vasodilation, which is associated with a decrease in central sympathetic tone; you should not interrupt therapy without medical advice; abrupt withdrawal, especially before the withdrawal of β-blockers, can lead to an increase in the risk of rebound arterial hypertension.
Combinations requiring caution:
    calcium channel blockers dihydropyridine derivatives (nifedipine, amlodipine): increased risk of arterial hypotension, patients with chronic heart failure should take into account the risk of subsequent deterioration of the ventricular function of the heart (due to bisoprolol);
    angiotensin-converting enzyme inhibitors (enalapril, captopril), angiotensin II receptor antagonists: an increase in the likelihood of a significant decrease in blood pressure and / or acute renal failure at the beginning of treatment with these drugs in patients with hyponatremia (this is especially true for patients with renal artery stenosis). If during the previous intake of diuretics the development of hyponatremia was observed, it is necessary either to stop taking diuretics 3 days before the use of angiotensin-converting enzyme inhibitors, or to start therapy with low doses with their subsequent gradual increase;
    antihypertensive drugs and other drugs with a possible antihypertensive effect (baclofen, tricyclic antidepressants, phenothiazine derivatives, barbiturates): increased risk of hypotension;
    class I antiarrhythmics (flecainide, quinidine, lidocaine, disopyramide, phenytoin, propafenone): a decrease in AV conduction and an increase in the negative inotropic effect (due to bisoprolol);
    antiarrhythmics (class IA and III, including ibutilide, quinidine, hydroquinidine, amiodarone, dofetilide, disopyramide, sotalol) and other drugs / substances that can cause pirouette-type tachycardia (astemizole, vincamine, terfenadine, erythromycin for intravenous administration, halofantrine, sparfloxacin, pentamidine, some antipsychotics): development of hypokalemia, which can cause ventricular arrhythmias, including pirouette-type tachycardia;
    class III antiarrhythmics (amiodarone): increased AV conduction disturbance (due to bisoprolol);
    m-cholinomimetics: increased impairment of AV conduction and increased risk of bradycardia (due to bisoprolol);
    insulin or oral hypoglycemic agents: increased hypoglycemic action; blockade of β-adrenergic receptors can mask the symptoms of hypoglycemia, for example, tachycardia;
    β-blockers for local use (eye drops for the treatment of glaucoma): increased systemic effects of bisoprolol (lowering blood pressure, slowing heart rate);
    means for conducting general anesthesia: an increase in the risk of the cardiodepressive effect of bisoprolol, which can lead to arterial hypotension;
    non-steroidal anti-inflammatory drugs: a decrease in the antihypertensive effect of bisoprolol; with hypovolemia, it is possible to initiate acute renal failure;
    cardiac glycosides: an increase in the time of the impulse, the development of bradycardia (due to bisoprolol);
    adrenomimetics that affect β- and α-adrenergic receptors (norepinephrine, epinephrine): an increase in their vasoconstrictor effects, which leads to an increase in blood pressure and exacerbation of intermittent claudication (due to bisoprolol); such interactions are most likely with the use of non-selective β-blockers;
    β-adrenergic agonists (dobutamine, isoprenaline): mutual decrease in the effect;
    drugs that promote the excretion of potassium from the body (corticosteroids, carbenoxolone, tetracosactide, amphotericin B, furosemide, drugs with a laxative effect): increased potassium loss;
    methyldopa: hemolysis associated with the formation of antibodies to hydrochlorothiazide (in some cases);
    drugs that lower the plasma concentration of uric acid in the blood: weakening their effectiveness (due to hydrochlorothiazide);
    contrast agents with iodine content: in cases of dehydration caused by taking hydrochlorothiazide, the risk of acute liver failure increases, especially against the background of the use of contrast agents in high doses;
    colestipol, cholestyramine: decreased absorption of hydrochlorothiazide;
    potassium-sparing diuretics: an increase in the likelihood of hyper- or hypokalemia, especially in patients with diabetes mellitus or liver failure (due to hydrochlorothiazide);
    calcium salts: an increase in the likelihood of hypercalcemia (due to hydrochlorothiazide, which is associated with a decrease in calcium excretion by the kidneys).
Combinations to consider:
    monoamine oxidase (MAO) inhibitors, except for MAO-B inhibitors: an increase in the antihypertensive effect, which can cause the development of a hypertensive crisis (due to bisoprolol);
    mefloquine: increased risk of developing bradycardia (due to bisoprolol);
    glucocorticosteroids: a decrease in the antihypertensive effect of Lodoz (due to the retention of water and sodium in the body caused by glucocorticosteroids).

Terms and conditions of storage

Keep out of the reach of children at a temperature of 18-25 ° C.
Shelf life is 3 years.

Reviews about Lodoz

According to reviews, Lodoz is an effective drug used to control blood pressure. Patients indicate the convenience of use, since the drug contains a diuretic that has a mild diuretic effect. The development of adverse reactions is rarely reported.

Terms of sell

A prescription is not required to buy Lodoz.