Logimax coated pills prolonged N30
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Active ingredients
Metoprolol + Felodipine
Release form
Pills
Composition
Active ingredient: Felodipine (Felodipine), Metoprolol Succin; Concentration of the active substance (mg): 52.5
Pharmacological effect
Antihypertensive drug of combined composition. It has hypotensive, antianginal and antiarrhythmic effects .; The complementary mechanism of action of felodipine, which lowers OPSS, and metoprolol, which reduces cardiac output, leads to a more pronounced antihypertensive effect and better tolerability compared with felodipine and metoprolol monotherapy. When taking Logimax, blood pressure reduction is stable and effective during the entire interval between doses (24 hours) .; Felodipine Felodipine, a dihydropyridine derivative, is a vasoselective blocker of slow calcium channels and is intended for the treatment of arterial hypertension and stable angina pectoris. Felodipine is a racemic mixture .; Conductivity and contractility of vascular smooth muscle is suppressed by affecting the calcium channels of the cell membrane. Due to the high selectivity for smooth muscles of arterioles, felodipine in therapeutic doses does not have a negative inotropic effect on contractility or conductivity of the heart .; The antihypertensive effect of felodipine is due to a decrease in OPS. Felodipine effectively reduces blood pressure in patients with arterial hypertension, both in a horizontal position and in a sitting and standing position, at rest and during exercise. Since felodipine has no effect on the smooth muscles of the veins or adrenergic vasomotor control, the development of orthostatic hypotension does not occur. At the beginning of treatment, as a result of a decrease in blood pressure in patients receiving felodipine, a temporary reflex increase in heart rate and cardiac output can be observed, which is leveled when combined with beta-blockers. The effect of felodipine on AD and OPS correlates with the plasma concentration of felodipine. After reaching a stable equilibrium plasma concentration of felodipine, the antihypertensive effect persists for 24 hours; Felodipine treatment leads to the reverse development of left ventricular hypertrophy .; Felodipine relaxes the smooth muscles of the respiratory tract.Felodipine has been shown to have a negligible effect on gastrointestinal motility. With long-term use, felodipine does not have a clinically significant effect on the content of lipids in the blood. In patients with type 2 diabetes mellitus with felodipine administered for 6 months, there was no clinically significant effect on metabolic processes. Felodipine can also be prescribed to patients with reduced left ventricular function, receiving standard therapy, and patients with bronchial asthma, diabetes, gout, or hyperlipidemia .; Felodipine reduces vascular resistance in the kidneys, has a natriuretic and diuretic effect, and does not have a potassium uretic effect (due to a decrease in tubular reabsorption of sodium and water). Felodipine does not affect glomerular filtration and albumin excretion .; Metoprolol; Metoprolol is a cardio-selective antagonist of β1 -adrenoreceptors, does not affect, in therapeutic doses, on β2 -adrenoreceptors, located mainly in peripheral vessels and bronchi. It has a slight membrane stabilizing effect and does not possess intrinsic sympathomimetic activity .; Beta-blockers have a negative inotropic and chronotropic effect. Metoprolol reduces the stimulating effect of catecholamines on the myocardium and helps to reduce heart rate, cardiac output and blood pressure. Under stress, with increased secretion of adrenaline, metoprolol does not interfere with normal physiological vasodilation .; At therapeutic doses, metoprolol has a smaller contractile effect on the muscles of the bronchi than non-selective beta-blockers .; Metoprolol to a lesser extent than non-selective beta-blockers affects insulin secretion and carbohydrate metabolism, and therefore metoprolol can be administered to patients with diabetes. Metoprolol has a lesser effect on such cardiovascular reactions in hypoglycemia, such as tachycardia. With metoprolol therapy, blood glucose is restored to a normal level faster than with non-selective beta-blockers. Therapy; Metoprolol reduces elevated blood pressure in both standing and horizontal position, as well as during exercise. At the beginning of therapy, metoprolol causes an increase in OPSS.However, with long-term treatment, there is a decrease in blood pressure due to a reduction in OPSS with an unchanged cardiac output. In patients with arterial hypertension, metoprolol reduces mortality from cardiovascular complications .; In patients receiving metoprolol, there are no changes in blood electrolyte balance.
Pharmacokinetics
Felodipine; Absorption; Felodipine systemic bioavailability index is about 15% and does not depend on food intake. Meal affects the rate of felodipine absorption, resulting in an increase in plasma Cmax by approximately 65%. Cmax in plasma is reached 3-5 hours after taking the drug .; Distribution; Plasma protein binding is approximately 99%. Vd in equilibrium approximately 10 l / kg. Does not accumulate. Css is reached in 5 days .; Metabolism; Felodipine is metabolized in the liver, all metabolites are pharmacologically inactive .; Withdrawal; T1 / 2 felodipine in the final phase - about 25 hours. The total plasma clearance averages 1.2 l / min; About 70% of the taken dose is excreted in the form of metabolites with urine, the rest - with feces. Less than 0.5% is excreted in the urine unchanged .; Pharmacokinetics in special clinical situations; In patients with impaired liver function and the elderly, the concentration of felodipine in the blood plasma increases. However, the age attribute only partially explains the individual changes in the plasma concentration of felodipine .; When kidney function is impaired, the plasma concentration of felodipine does not change, but cumulation of inactive metabolites is observed. Felodipine is not excreted by hemodialysis .; Metoprolol; Absorption and metabolism; Metoprolol is completely absorbed from the gastrointestinal tract after oral administration. It is metabolized in the liver to form 3 major metabolites that do not have pharmacological activity and have no clinical significance .; Withdrawal; About 5% of the metoprolol dose taken is excreted unchanged by the kidneys, the rest is excreted as metabolites .; Felodipine + Metoprolol; Taking Logimax does not change the bioavailability of the components, compared with separate simultaneous administration of felodipine and metoprolol. Absorption rates are independent of food intake.
Indications
Hypertension, symptomatic arterial hypertension.
Contraindications
Hypersensitivity, acute myocardial infarction, unstable stenocardia, severe sinus bradycardia, AV block II-III degree, sick sinus syndrome, severe peripheral circulatory disorders, decompensated heart failure, cardiogenic shock, pregnancy.
Use during pregnancy and lactation
Logimaks; should not be prescribed during pregnancy .; Currently, there is insufficient data on the use of felodipine in pregnant women. Based on animal data, felodipine should not be administered during pregnancy. Slow calcium channel blockers may inhibit uterine contractions in preterm labor, but there is insufficient evidence to support an increase in the duration of physiological labor. The risk of fetal hypoxia is possible if the mother has arterial hypotension and a decrease in perfusion in the uterus due to redistribution of blood flow and peripheral vasodilation .; Metoprolol can be used during pregnancy and lactation only if absolutely necessary. Beta-blockers can cause bradycardia in the fetus, newborns and in breastfed babies. This should be taken into account when deciding on the appointment of the drug in the third trimester of pregnancy and immediately before delivery. Felodipine and metoprolol pass into breast milk. When nursing mother felodipine in therapeutic doses, only a small amount of the drug is administered with breast milk to the baby. Insufficient experience with felodipine in women during lactation does not exclude the risk of the drug being exposed to the child, and therefore felodipine is not recommended for women during lactation. If necessary, continue therapy to achieve a clinical effect should consider stopping breastfeeding.
Dosage and administration
Inside, in the morning, without chewing, drinking water. The initial dose - 1 tab. Once a day, if necessary, double the dose .; There is no need to adjust the treatment regimen in patients with impaired renal function. Usually there is no need to adjust the treatment regimen in patients with impaired liver function, incl. in patients with cirrhosis of the liver.If there are symptoms of severe liver dysfunction (for example, in patients whose history had bypass surgery), the possibility of lowering the dose of the drug should be considered .; In patients of advanced age is usually enough 1 table. Once a day, if necessary - 2 times a day.
Side effects
Decrease in blood pressure; headache, dizziness, peripheral edema, weakness, nausea, vomiting, dry oral mucosa, constipation or diarrhea; gum hyperplasia; ; increased activity of "liver" transaminases; myalgia, arthralgia; allergic reactions (pruritus, angioedema); ; AV blockade Art. I, bradycardia; thrombocytopenia; paresthesia, depression, reduced ability to concentrate, drowsiness, insomnia, anxiety, reduced potency, sexual dysfunction; ; dyspnea, bronchospasm, rhinitis; vision impairment, dryness and / or eye irritation, conjunctivitis, tinnitus, impaired taste sensations; photosensitization .; Rarely - tachycardia, palpitations, gangrene (in patients with severe disorders of the peripheral circulation), amnesia, confusion, hallucinations.
Overdose
Toxicity; When using felodipine in a dose of 10 mg in a 2-year-old child, slight intoxication was noted. Felodipine in a dose of 150–200 mg in a 17-year-old patient and in a dose of 250 mg in an adult caused a slight to moderate intoxication. Felodipine probably has a more significant effect on the peripheral circulation than on the heart, compared with other drugs of this therapeutic group .; Metoprolol in a dose of 7.5 g in an adult caused fatal intoxication. In a 5-year-old child who took 100 mg of metoprolol, after washing the stomach, there were no signs of intoxication. Acceptance of metoprolol in a dose of 450 mg by a 12-year-old child led to moderate intoxication. Acceptance of metoprolol at a dose of 1.4 g and 2.5 g by adults caused moderate and severe intoxication, respectively. Acceptance of metoprolol in a dose of 7.5 g to adults led to extremely severe intoxication .; Symptoms; In case of an overdose with prolonged-action drugs, symptoms of intoxication appear 12-16 hours after administration, severe symptoms may occur several days after ingestion .; With felodipine overdose, the greatest effect on the cardiovascular system is observed: bradycardia (sometimes tachycardia), marked reduction in blood pressure, AV blockade, ventricular extrasystole, atrioventricular dissociation, asystole, ventricular fibrillation, headache, dizziness,impaired consciousness (or coma), convulsions, shortness of breath, pulmonary edema (non-cardiac) and apnea; possible development of respiratory distress syndrome in adults; acidosis, hypokalemia, hyperglycemia, hypocalcemia, hot flashes, hypothermia, nausea and vomiting .; With an overdose of metoprolol, symptoms of the cardiovascular system are the most serious, but sometimes, especially in children and adolescents, symptoms of the central nervous system and suppression of pulmonary function, bradycardia, AV-block I-III degree, asystole, pronounced decrease in blood pressure, weak peripheral perfusion, heart failure, cardiogenic shock, depression of lung function, apnea, and also, increased fatigue, impaired consciousness, loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospas gp, nausea, vomiting, possible esophageal spasm, hypoglycaemia (especially in children) or hyperglycaemia, hyperkalaemia; effects on the kidneys; transient myasthenic syndrome. Concomitant use of alcohol, antihypertensive drugs, quinidine, or barbiturates may worsen the patient's condition. The first signs of overdose can be observed in 20 minutes - 2 hours after taking the drug .; Treatment; Felodipine; Appointment of activated carbon, if necessary, gastric lavage, in some cases, effective even in the late stage of intoxication. Symptomatic therapy is carried out .; Atropine (0.25-0.5 mg IV for adults, 10-20 µg / kg for children) should be prescribed before gastric lavage (due to the risk of stimulating the vagus nerve). Conduct ECG monitoring. If necessary, maintain the airway and ensure adequate ventilation of the lungs. Correction of the acid-base state and serum electrolytes is shown. In the case of bradycardia and AV blockade, atropine 0.5–1 mg is prescribed in / to adults (20–50 µg / kg for children), administration is repeated if necessary, or isoprenaline is initially administered at a dose of 0.05–0.1 µg / kg / min. In case of acute intoxication at an early stage, it may be necessary to install an artificial pacemaker. Hypotension corrected in / in the introduction of fluid. If necessary, adrenaline or dopamine is infused. In acute intoxication, glucagon may be administered. When a cardiac arrest due to an overdose, resuscitation may be necessary for several hours. When convulsions prescribed diazepam.Another symptomatic treatment is being conducted .; Metoprolol; Appointment of activated carbon, if necessary, gastric lavage .; Atropine (0.25-0.5 mg IV for adults, 10-20 µg / kg for children) should be prescribed before gastric lavage (due to the risk of stimulating the vagus nerve). If necessary, maintain the airway (intubation) and adequate ventilation of the lungs. Replenishment of BCC and glucose infusion. Conduct ECG monitoring. Atropine is prescribed in a dose of 1-2 mg IV, and if necessary, repeat the administration (especially in the case of vagal symptoms). In the case of (suppression) myocardial depression, infusion of dobutamine or dopamine is indicated. You can also use glucagon at a dose of 50-50 mg / kg i.v. with an interval of 1 min. In some cases, adding adrenaline to therapy may be effective. For arrhythmias and dilated ventricular (QRS) complex, infusion solutions of sodium chloride or sodium bicarbonate are infused. Installation of an artificial pacemaker is possible. When a cardiac arrest due to an overdose, resuscitation may be necessary for several hours. Terbutaline can be used to relieve bronchospasm (injection or by inhalation). Symptomatic treatment is carried out.
Interaction with other drugs
Co-administration with substances that interact with the cytochrome P450 enzyme system may affect the concentration of felodipine and metoprolol in the blood plasma. There is no interaction between felodipine and metoprolol, since they are metabolized by various isoenzymes of the cytochrome P450 system; Felodipine; Felodipine is a substrate for CYP3A4. The drugs inducing or inhibiting CYP3A4 have a significant effect on the concentration of felodipine in the blood plasma .; Drugs that induce isoenzymes of the cytochrome P450 system (phenytoin, carbamazepine, phenobarbital, and rifampicin, as well as St. John's wort tincture), increase felodipine metabolism. The combined use of phenytoin, carbamazepine, phenobarbital and rifampicin leads to a decrease in AUC values by 93% and felodipine Cmax by 82%. Avoid co-assignment with inductors CYP3A4 .; Antifungal drugs of the azole series (itraconazole, ketoconazole), macrolide antibiotics (for example, erythromycin) and HIV protease inhibitors are inhibitors of the CYP3A4 enzyme system. With the joint appointment of itraconazole, Cmax felodipine is increased 8 times, AUC - 6 times.With co-administration of erythromycin Cmax and AU, felodipine increases approximately 2.5 times. Co-administration of felidipine and inhibitors of CYP3A4 should be avoided .; Grapefruit juice inhibits the CYP3A4 enzyme system. The use of felodipine with grapefruit juice increases Cmax and AUC of felodipine approximately 2 times. Co-administration should be avoided .; Felodipine may cause an increase in plasma tacrolimus concentration. When used together, it is recommended to control the concentration of tacrolimus in the blood serum; a dose adjustment of tacrolimus may be required .; With the joint appointment of cyclosporine and felodipine, Cmax of felodipine is increased by 150%, AUC is increased by 60%. However, the effect of felodipine on the pharmacokinetic parameters of cyclosporine is minimal .; The combined use of cimetidine and felodipine leads to an increase in Cmax and AUC of felodipine by 55%; Metoprolol; It is necessary to avoid co-administration of Logimax with the following drugs .; Barbiturates (the study was conducted with fenofarbitalom) slightly increase the metabolism of metoprolol, due to the induction of enzymes .; When prescribing propafenone to 4 patients treated with metoprolol, an increase in plasma concentration of metoprolol was noted by a factor of 2-5, while in 2 patients side effects characteristic of metoprolol were noted. This interaction was confirmed during the study on 8 volunteers. Probably, the interaction is due to the inhibition by propafenone, like quinidine, of the metabolism of metoprolol by the isoenzyme CYP2D6. Taking into account the fact that propafenone has the properties of a beta-blocker, the joint appointment of Logimax and propafenone does not seem appropriate .; The combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on AV conductivity and sinus node function .; The combination of Logimax with the following drugs may require dose adjustment .; Class I antiarrhythmic drugs and beta-blockers can result in the summation of a negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. Similar combinations should also be avoided in patients with sick sinus syndrome and impaired AV conduction.The interaction is described on the example of disopyramide .; Diphenhydramine reduces the clearance of metoprolol to β-hydroxymetoprolol 2.5 times. At the same time, there is an increase in the action of metoprolol .; Hypertensive reactions with abrupt cancellation of clonidine may be enhanced when co-receiving beta-blockers. When used together, in the event of clonidine withdrawal, discontinuation of beta-blockers should be started a few days before the withdrawal of clonidine .; Diltiazem and beta-blockers mutually enhance the inhibitory effect on AV conductivity and the function of the sinus node. When metoprolol was combined with diltiazem, there were cases of severe bradycardia .; NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction is most documented for indomethacin. The observed interaction for sulindac was not observed. In studies with diclofenac, the described reaction was not observed .; Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents an increase in blood pressure caused by phenylpropanolamine. However, beta-blockers can cause reactions of paradoxical arterial hypertension in patients receiving high doses of phenylpropanolamine. Reported several cases of hypertensive crisis in patients receiving phenylpropanolamine .; 10 cases of severe hypertension and bradycardia have been reported in patients taking non-selective beta-blockers (including pindolol and propranolol) and receiving epinephrine (adrenaline). Interaction is also noted in the group of healthy volunteers. It is assumed that such reactions can be observed with the use of epinephrine in conjunction with local anesthetics in case of accidental contact with the vascular bed. It is assumed that this risk is much lower when using cardio selective beta-blockers .; Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (in Sweden, about 90% of the population), causing, mainly, a significant increase in the plasma concentration of metoprolol and increased blockade of β-adrenergic receptors.It is believed that this interaction is also characteristic of other beta-blockers, in the metabolism of which the CYP2D6 isoenzyme is involved .; The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Taking into account the extremely long T1 / 2 of amiodarone (50 days), possible interaction should be considered after a long time after the cancellation of amiodarone .; Rifampicin can increase the metabolism of metoprolol, reducing the plasma concentration of metoprolol .; Plasma concentrations of metoprolol may increase with concomitant use with cimetidine, hydralazine, selective serotonin inhibitors, such as paroxetine, fluoxetine and sertraline .; Patients taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors at the same time should be closely monitored .; Against the background of beta-adrenergic blockers, inhalation anesthetics enhance the cardiodepressive effect .; When beta-adrenergic blockers are taken, patients receiving oral hypoglycemic agents may need to adjust the dose of the latter.
special instructions
Care should be taken when co-administered with digitalis preparations .; Logimax; may exacerbate the symptoms of peripheral circulatory disorders .; Precautions should be prescribed for severe renal failure (CC <30 ml / min), aortic stenosis, abnormal liver function, acute myocardial infarction, acute myocardial infarction complicated by heart failure, arterial hypotension, which in susceptible patients can cause myocardial ischemia, acute metabolic acidosis. It is not recommended to start treatment with Logimax in patients who have not previously received antihypertensive therapy .; It is not recommended to prescribe the drug to patients with latent or identified heart failure without appropriate therapy .; The use of Logimax may affect carbohydrate metabolism or mask hypoglycemia, however, when using Logimax, the risk of exposure to carbohydrate metabolism is less than when using non-selective beta-adrenergic blockers .; In some cases, existing AV conduction disturbances may increase, leading to AV blockade .; To patients taking logimax ;,do not enter IV blockers of slow calcium channels like verapamil .; In patients with Prinzmetal angina, the frequency and severity of angina may increase due to spasm of the coronary vessels caused by stimulation of alpha-adrenoreceptors. In this regard, it is not recommended to assign non-selective beta-blockers to this group of patients. Beta-blockers should be used with caution .; Against the background of beta-blockers, anaphylactic shock may take a more severe form. The use of epinephrine (adrenaline) in the commonly used dosage does not always lead to the expected therapeutic effect .; It is recommended that patients with pheochromocytoma be given alpha-blockers simultaneously with Logimax .; The combined use of drugs that induce the CYP3A4 enzyme system leads to a significant decrease in the concentration of felodipine in the blood plasma and an insufficient therapeutic effect from taking the drug. Co-administration of such drugs should be avoided .; The combined use of drugs that inhibit the CYP3A4 enzyme system, leads to a significant increase in the concentration of felodipine in the blood plasma .; You should avoid taking Logimax with grapefruit juice due to a significant increase in the concentration of felodipine in the blood plasma .; It is necessary to avoid abrupt withdrawal of beta-blockers, especially in high-risk patients, due to the possible exacerbation of symptoms of chronic heart failure and an increased risk of myocardial infarction and sudden death. If necessary, the abolition of Logimax should be carried out gradually by reducing the dose within 1-2 weeks .; In the case of surgery, the anesthesiologist should be warned that the patient is taking Logimax; It is not recommended to stop treatment with beta-adrenergic blockers in patients who are to undergo surgery. Impact on the ability to drive vehicles and control mechanisms; When driving vehicles and engaging in potentially hazardous activities that require increased concentration and psychomotor reactions, it should be noted that when using Logimax, dizziness and fatigue can occur.