Zanidip Recordatie coated pills 10mg N56
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Active ingredients
Lercanidipine
Release form
Pills
Composition
Lercanidipine hydrochloride 10 mg Auxiliary substances: lactose monohydrate - 30 mg, microcrystalline cellulose - 39 mg, sodium carboxymethyl starch - 15.5 mg, povidone K30 - 4.5 mg, magnesium stearate - 1 mg. The composition of the shell: opadry yellow (OY-SR-6497) - 3 mg (hypromellose, talc, titanium dioxide (E171), macrogol 6000, iron dye yellow oxide (E172)).
Pharmacological effect
Blocker of "slow" calcium channels. Lercanidipine is a racemic mixture of right- (R) and left-rotating (S) stereoisomers, a derivative of 1,4-dihydropyridine, capable of selectively blocking the flow of calcium ions into the vascular wall cells, heart cells and smooth muscle cells. The mechanism of antihypertensive action is due to a direct relaxing effect on vascular smooth muscle cells. It has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after ingestion and its duration is maintained for 24 hours (24 hours). Due to the high selectivity to vascular smooth muscle cells, there is no negative inotropic effect. Zanidip Recordatio is a metabolically neutral drug and does not have a significant impact on the content of lipoproteins and apolipoproteins in the serum, and does not change the lipid profile in patients with arterial hypertension.
Pharmacokinetics
After ingestion, lercanidipine is almost completely absorbed from the gastrointestinal tract. Cmax in plasma is reached in 1.5-3 hours and amounts to 3.3 ng / ml and 7.66 ng / ml after taking 10 mg and 20 mg, respectively. Distribution Distribution from blood plasma to tissues and organs occurs quickly. Plasma protein binding exceeds 98%. At repeated use does not accumulate. Metabolism Metabolized during the "primary passage" through the liver through CYP3A4 biotransformation with the formation of a number of metabolites that do not possess pharmacological activity. Withdrawal Excreted by the kidneys and intestines after biotransformation. There are 2 phases of elimination of lercanidipine: early (T1 / 2 - 2-5 h) and final (T1 / 2 - 8-10 h). The drug in its unchanged form is practically not detected in the urine and feces. Pharmacokinetics in special clinical situations In patients with renal and hepatic insufficiency, the plasma protein content is reduced, so the free fraction of lercanidipine may be increased.
Indications
- Essential hypertension mild and moderate severity.
Contraindications
- chronic heart failure in the stage of decompensation; - unstable angina; - obstruction of vessels emanating from the left ventricle of the heart; - recent myocardial infarction (within 1 month); - severe abnormal liver function; - impaired renal function (glomerular filtration rate less than 39 ml / min); - simultaneous use with powerful inhibitors of isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine; - Lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome; - children's and teenage age up to 18 years (efficiency and safety are not established); - pregnancy; - lactation period; - women of childbearing age who do not use reliable contraceptives; - hypersensitivity to lercanidipine, other derivatives of the dihydropyridine series or any component of the drug. With care: dysfunction of a liver of easy and moderate severity; sick sinus syndrome (without pacemaker); left ventricular failure and ischemic heart disease; chronic heart failure; simultaneous reception of beta adrenoblockers, digoxin.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
The drug is prescribed 10 mg 1 time / day (in the morning) at least 15 minutes before meals. Depending on the individual effect, the dose of the drug can be increased to 20 mg. The therapeutic dose is adjusted gradually, if necessary, the dose is increased 2 weeks after the start of the drug. Tablets are taken orally, without chewing, with a sufficient amount of water. In elderly patients, dose adjustment is not required, however, when taking the drug requires constant monitoring of patients. In the presence of mild or moderate renal or hepatic insufficiency, as a rule, dose adjustment is not required; the initial dose is 10 mg, then the dose should be carefully increased to 20 mg / day. If the antihypertensive effect is too pronounced, the dose should be reduced.
Side effects
The frequency of occurrence of adverse events was classified as follows: very often (1/10), often (1/100), infrequently (1/1000), rarely (1/10 000), very rare (<1/10 000). On the part of the nervous system: rarely - drowsiness; infrequently - headache, dizziness. On the part of the immune system: very rarely - hypersensitivity.Since the cardiovascular system: infrequently - tachycardia, feeling of heartbeat, rush of blood to the skin of the face; rarely - angina; very rarely - fainting, marked reduction in blood pressure, chest pain, myocardial infarction. On the part of the digestive system: rarely - nausea, vomiting, diarrhea, abdominal pain, dyspepsia; very rarely - a reversible increase in liver enzyme activity. Skin: rarely - skin rash. On the part of the musculoskeletal system: rarely - myalgia. From the urinary system: rarely - polyuria. Other: infrequent - peripheral edema; rarely - asthenia, fatigue; very rarely - gingival hyperplasia.
Overdose
Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia, an increase in the frequency and duration of strokes, myocardial infarction. Treatment: conduct symptomatic therapy.
Interaction with other drugs
The drug should not be taken simultaneously with inhibitors of CYP3A4 (liver cytochrome P450 isoenzyme), such as ketoconazole, itraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect). Concurrent use of lercanidipine with cyclosporine is contraindicated. This leads to an increase in the content of both substances in the blood plasma. Lercanidipine should not be taken together with grapefruit juice, because it leads to the inhibition of lercanidipine metabolism and potentiation of the antihypertensive effect. It is necessary to be careful at simultaneous reception with such drugs as terfenadin, astemizol, quinidine and class III antiarrhythmic drugs (for example, amiodarone). Simultaneous use with anticonvulsant drugs (for example, phenytoin, carbamazepine) and rifamycin can lead to a decrease in the level of lercanidipine in the blood plasma and, therefore, to a decrease in the antihypertensive effect of lercanidipine. While taking digoxin, it is necessary to regularly monitor for signs of digoxin intoxication. Taking the drug with midazolam in old age leads to an increase in the absorption of lercanidipine and a decrease in the rate of absorption. Metoprolol reduces the bioavailability of lercanidipine by 50%, while the bioavailability of metoprolol remains unchanged.This effect may occur due to a decrease in hepatic blood flow, which is caused by beta-blockers, therefore it can also manifest itself when used with other drugs in this group. Cimetidine in a dose of 800 mg / day does not lead to significant changes in the concentration of lercanidipine in the blood plasma, however, special care is required, since with higher doses of cimetidine, the bioavailability of lercanidipine, and, consequently, its antihypertensive effect, may increase. With simultaneous use with simvastatin, the drug should be taken in the morning, and simvastatin - in the evening. Fluoxetine has no effect on the pharmacokinetics of lercanidipine. Reception of lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter. Lercanidipine can be used simultaneously with beta-blockers, diuretics, ACE inhibitors. Ethanol may enhance the antihypertensive effect of pharmacidipine.
special instructions
Caution must be exercised in the appointment of patients with impaired renal function, coronary artery disease (there is a risk of increased angina attacks). Before starting the drug, it is necessary to compensate for chronic heart failure. Special care should be taken at the initial stages of treatment of patients with mild and moderate severity of liver failure. Impact on the ability to drive vehicles and control mechanisms During the period of treatment, care must be taken when performing work requiring increased attention when driving, especially at the beginning of treatment and when increasing the dose of the drug (risk of drowsiness, headache and dizziness).