Lodoz pills coated 2.5 mg + 6.25 mg N30
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Active ingredients
Bisoprolol + Hydrochlorothiazide
Release form
Pills
Composition
Active ingredient: Bisoprolol fumarat, Hydrochlorothiazide (Hydrochlorothiazide) Concentration of the active substance (mg): 8.75
Pharmacological effect
Combined antihypertensive drug. Bisoprolol is a highly selective beta1-blocker with no sympathomimetic and membrane stabilizing activity. The mechanism of action of bisoprolol in arterial hypertension is associated primarily with a decrease in the level of renin in the blood plasma and a decrease in heart rate. Hydrochlorothiazide is a diuretic from the thiazide group 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, thereby preventing its reabsorption. In clinical studies, potentiation of the effects of the active substances of this combination was observed. Efficacy for treating mild and moderate arterial hypertension was noted even when used in the smallest 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 Lodoz is reduced by 2-4 times.
Pharmacokinetics
Bisoprolol Absorption and distribution of Tmax in plasma ranges from 1 to 4 hours. Plasma protein binding is about 30%. Metabolism and elimination of 40% of bisoprolol is metabolized in the liver. Metabolites are inactive. T1 / 2 of blood plasma is 11 h. Renal and hepatic clearance are equivalent. Half of the administered dose is excreted in the urine both unchanged and in the form of metabolites. The total clearance is about 15 l / h. Hydrochlorothiazide Absorption and distribution The bioavailability of hydrochlorothiazide ranges from 60% to 80%. Tmax in plasma is about 4 hours (from 1.5 to 5 hours). Plasma protein binding is 40%. Hydrochlorothiazide penetrates the placental barrier, is excreted in breast milk. Metabolism and elimination Hydrochlorothiazide is not metabolized and is almost completely excreted in unchanged form by glomerular filtration and active tubular secretion.T1 / 2 hydrochlorothiazide is about 8 hours. Pharmacokinetics in special clinical situations. In the case of renal and heart failure, in elderly patients the renal clearance of hydrochlorothiazide decreases, T1 / 2 increases.
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 block. - AV block II and III degree without an artificial pacemaker. - Severe bradycardia (HR - Variant angina (Prinzmetal angina). - Pheochromocytoma (without simultaneous use of alpha-adrenergic blockers) .- Severe forms of impaired peripheral circulation (-) h. Raynaud's disease) .- Hypotension .- Hypokalemia .- Hypovolemia .- Severe renal dysfunction (creatinine clearance - Severe dysfunction of the liver.- Simultaneous use with floctafenin, sultridom, antiarrhythmic media. tvami, lithium preparations. - Children and adolescents under 18 years of age (efficacy and safety have not been established). - Increased sensitivity to bisoprolol and other components of the drug. - Increased sensitivity to hydrochlorothiazide and other sulfonamides. With caution should be used with AV block I degree , psoriasis, ischemic heart disease, chronic heart failure in the stage of decompensation, thyrotoxicosis, water and electrolyte disorders (hyponatremia, hypokalemia, hypercalcemia), gout, as well as in elderly patients.
Use during pregnancy and lactation
Precautions associated with the use of bisoprolol Do not suddenly stop treatment, especially in patients with coronary artery disease. It is recommended to reduce the dose gradually over 2 weeks. If necessary, you should simultaneously begin an appropriate therapy to prevent attacks of angina. If necessary, the drug should be prescribed to patients with asthma or COPD, and the treatment should be started with the minimum initial dose. Before starting therapy, it is recommended to conduct functional respiratory tests. If bronchospasm develops during therapy, beta-adrenergic mimics should be prescribed. Patients with chronic heart failure should be prescribed the drug with caution and under medical supervision,in minimal doses. It is necessary to reduce the dose of the drug for heart rate at rest <50-55 beats / min and if there are clinical symptoms of bradycardia. Considering the negative dromotropic effect of beta-adrenergic blockers, they should be administered with caution to patients with an AV block I degree. In patients With peripheral circulatory disorders (Raynaud's disease), beta-blockers can cause an exacerbation of the disease. Patients with pheochromocytoma should not be given Lodoz until treatment with alpha-blockers. Control of AD is necessary. In elderly patients, treatment should begin with a low dose of the drug, 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 can mask the symptoms of hypoglycemia (tachycardia, palpitations and increased sweating). Against the background of therapy with beta-blockers, exacerbation of the course of psoriasis is possible. Bisoprolol should be prescribed only when necessary. With a history of anaphylactic reactions, regardless of the cause of their occurrence, especially when taking floctafenin, or during desensitization therapy, treatment with beta-adrenergic blockers may aggravate the occurrence of these reactions and cause the development of resistance to epinephrine ( adrenaline) in normal doses. Athletes should be informed that Lodoz contains an active substance that can give positive results when held SRI doping testov.Predostorozhnosti associated with start gidrohlorotiazidaPered more regularly and during therapy is necessary to monitor the level of sodium in the blood. Reduction of sodium at the beginning of treatment may be asymptomatic, so regular monitoring is necessary. Special attention is required when there are risk factors, for example, patients of old age, patients with cirrhosis of the liver. Potassium control in the blood is necessary 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, an increased QT interval. Hypopotassemia increases the risk of arrhythmias, cardiac toxicity likozidov.The first determination of the level of potassium in the blood must be carried out during the first week of therapy with Lodoz. 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. Thiazide treatment should be stopped before examining the function of the parathyroid glands. Blood glucose monitoring is necessary 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 must be selected individually. kidney or slightly reduced kidney function (CC <60 ml / min; serum creatinine content> 2.5 mg / dL or> 220 mcmol / L). In elderly patients, CC can be calculated taking into account the patient's age, body weight and gender using the Cockroft formula: For men: CC (ml / min) = [140-age] × body weight (kg) /0.814 × serum creatinine (μmol / l ) For women: the obtained value × 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 of patients with normal renal function. Temporary impairment kidney leakage without consequence in patients with normal renal function. In patients with impaired renal function, it is possible to enhance existing disorders. In the case of the administration of the drug with another antihypertensive agent, a dose reduction is recommended at the beginning of treatment. Use in pediatrics on the ability to drive vehicles and control mechanisms Apply with care when driving and working with mechanisms in connection with the possibility of Itia dizziness.
Dosage and administration
Lodoz should be taken once a day, in the morning before breakfast, during or after it. Tablets should be swallowed whole, not chewed, with a small amount of liquid. The dose of the drug should be selected individually. The initial dose corresponds to 1 tablet containing 2.5 mg of bisoprolol + 6.25 mg of hydrochlorothiazide 1 time per day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet containing 5 mg of bisoprolol + 6.25 mg of hydrochlorothiazide, 1 time per day.If the therapeutic effect is not pronounced, you can increase the dose of the drug Lodoz to 1 tablet containing 10 mg of bisoprolol + 6.25 mg of hydrochlorothiazide, 1 time per day.
Side effects
The drug is contraindicated for use in combination with floktafenin, sultopridom. The drug is not recommended to be used in combination with amiodarone, lithium, or with agents that can initiate arrhythmias (astemizole, bepridil, erythromycin, halofantrine, pentamidine, sparfloxacin, terfenadine, vincomycin, etc.). simultaneous use of the drug with baclofen, halogenated inhalation general anesthetics, slow calcium channel blockers (bepridilom, diltiazem, verapamil), antiarrhythmic drugs with redstvami (propafenone, quinidine, gidrohinidinom, disopyramide), insulin, urea preparations, lidocaine, iodine-containing contrast agents, anticholinesterase agents, high-dose salicylates, drugs that cause hypokalemia - amphotericin (w / administration) and mineralocorticoid (systemic application) tetrakozaktidom laxatives; cardiac glycosides, hyperkalemia-causing diuretics (amiloride, canrenone, spironolactone, triamterene); ACE inhibitors, metformin. It is possible to enhance the hypotensive action while using tricyclic antidepressants (including imipramine), neuroleptics, slow calcium channel blockers derived from the dihydropyridine series (including amlopidine, felopanine, lacidipine, nifedipine, nynepipine, nypidipine, nipedipine, nacidipine, nalipidine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine, nacidipine; nitrendipine). Application of Lodoz simultaneously with tricyclic antidepressants, incl. 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 an antihypertensive agent due to an additive hypotensive effect. If co-administered with mefloquine, bradycardia may develop. If co-administered with calcium drugs, hypercalcemia may develop. When co-administered with cyclosporine possible increase in the content of serum creatinine. It is possible the weakening of the hypotensive action of Lodoz with simultaneous appointment with GCS (for the system Nogo application), NSAIDs and tetrakozaktidom.
Overdose
Headache (may occur at the beginning of treatment and usually disappear during the first or second week of treatment).Since the cardiovascular system: bradycardia, impaired AV conduction, exacerbation of chronic heart failure, orthostatic hypotension. On the respiratory system: bronchospasm in patients with bronchial asthma or COPD in history. 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 the content of serum creatinine and urea. From the musculoskeletal system: feeling cold and ona limb menia, muscular weakness, convulsions. From the sensory organs: hearing impairment, decreased production of the lacrimal glands (it is necessary to take into account patients using contact lenses), visual impairment. Metabolism: hypertriglyceridemia, hypercholesterolemia, hyperglycemia, glucosuria, hyperuricemia, impaired water-electrolyte state, metabolic alkalosis. From the hematopoietic system: leukopenia, thrombocytopenia. Dermatological reactions: beta-blockers can cause or aggravate the course of psoriasis or cause psoriasis-like rashes, alopecia. Others: impotence, allergic rhinitis. The drug is usually well tolerated. Side effects are described in less than 10% of cases.
Interaction with other drugs
Precautionary measures
special instructions
Symptoms: excessive decrease in blood pressure, bradycardia. Newborns from mothers receiving beta-blockers may develop an overdose, which manifests cardiac decompensation. Treatment: in the case of severe bradycardia or an excessive decrease in blood pressure, the following medications are administered: atropine at a dose of 1-2 mg; glucagon at a dose of 1 mg is slowly bolus and then, if necessary, in the form of an infusion at a dose of 1-10 mg / h; then, if necessary, either epinephrine (adrenaline) at a dose of 15-85 mcg is administered, 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. In case of overdose in newborns, manifested by cardiac decompensation activities, prescribe glucagon at the rate of 0.3 mg / kg; epinephrine (adrenaline) and dobutamine (usually in high doses) must be monitored in the ICU of newborns. Prolonged treatment is carried out under the supervision of a specialist.