Lercatop medicine 10mg Balkanpharma treats hypertension from mild to medium (2 blisters x 14 tablets)

ATC code: c08ca13.

Lercanidipin is a calcium channel blocker of the dihydropyridine group, inhibiting the calcium ions into myocardial and smooth muscle cells. Its mechanism of lowering blood pressure is due to the direct relaxation of blood vessels, thus reducing peripheral resistance. Although the half -life in the plasma of Lercanidipin is short, Lercanidipin has a prolonged lowering effect due to the high water distribution coefficient and has a selective dilatation effect on blood vessel smooth muscles.

Due to the vasodilation effect caused by lercanidipin, it is slowly onset, so acute hypotension with reflex tachycardia is rarely observed in patients with hypertension using Lercanidipine.

Like other asymmetry 1, 4 - Dihydropyridin, the hypotension effect of lercanidipin is mainly due to the isomorphic S.In addition to clinical studies conducted to support treatment indications, an uncontrolled, random study on patients with severe hypertension (on average ± sd of diastolic blood pressure is 114.5 ± 3.7 mmHg) shows that the blood pressure has been normal in 40% of 25 patients taking 20 mg lercanidipin once a day and 56% of the 25 mg LERCANIDIPIN patients every day two mg twice. In a double, random, controlled study compared to the placebo in patients with solitary hypertension, Lercanidipin is effective in reducing the initial systolic blood pressure 172.6 ± 5.6 mmHg to 140.2 ± 8.7 mmHg.

Dynamic pharmacokinetics

Lercanidipin 10 mg and 20 mg are completely absorbed after taken with peak in plasma of 3.30 ng/ml ± 2.09 and 7.66 ng/ml ± 5.90, after about 1.5 - 3 hours after taken medication.

Due to the high first metabolism, Lercanidipin's bioavailability when taking the drug with a meal is about 10%, although it is reduced to 1/3 when used for healthy volunteers to drink when hungry.

Lercanidipine distribution from plasma to tissues and organs quickly and widely. Linking with plasma proteins is 98%higher. Because the level of protein in plasma decreases in patients with severe renal impairment or liver dysfunction, the free drug in these patients may increase.

Lercanidipin is metabolized mainly by CYP3A4; No mother medicine is found in urine or feces. Lercanidipin is mainly converted into inactive metabolites, about 50% of the dose is excreted in the urine.

Elimination is mainly by biological metabolism, half-life except for 8-10 hours, treatment activity lasts up to 24 hours because of its ability to attach to high lipid arrays. No accumulation is observed when used continuously.

In elderly patients and patients with renal dysfunction or mild to moderate liver dysfunction, lercanidipin pharmacokinetics similar to the common patient group. In patients with severe renal dysfunction or the prime patient shows that the pharmacokinetics of the drug are higher (about 70%). In patients with medium to severe liver failure, the systemic bioavailability of Lercanidipine may increase because this drug is mainly metabolized through the liver.

Caution when using

Pathological sinus syndrome:

Need to take special care when using lercanidipin in patients with pathological sinus button syndrome (if a pacemaker is not in situ printing). Although hemodynamic control studies show that there is no impairment of ventricular function, also cautious in patients with left ventricular dysfunction. It has been suggested that some short -acting dihydropyridine may be associated with an increase in cardiovascular risk in local heart anemia patients. Although Lercanidipin is a long -lasting effect, it is also necessary to be cautious in this patient group.

Angina:

Some dihydropyridine is very dangerous when leading to angina or a pain before the heart. It is very rare for patients to have angina that may increase the frequency, time or severity of the pain. The special case of myocardial infarction can be observed.

Used in patients with kidney or liver dysfunction:

Be cautious when starting treatment in patients with kidney or mild to medium liver dysfunction. Although the usual dose regimen is recommended to be tolerated in this patient group, the dosage increase to 20 mg of Lercanidipin daily should be carefully approached. The low voltage effect can be enhanced in patients with liver failure and the consequence of a dose adjustment to be considered.

Lercanidipin is not recommended for patients with severe liver failure or severe renal failure (creatinine clearance

CYP3A4 induction drug:

CYP3A4 induction drugs such as anti -convulsions (eg phenytoin, carbamazepin) and rifampicin may reduce lercanidipine levels in plasma and thus reduce the effect of lercanidipine than expected.

This drug contains lactose monohydrate and therefore should not be used for patients with lactase enzyme deficit, galactosaemia or glucose - galactose malabsorption syndrome.

The effect of the drug on driving and operating machinery

Lercanidipin does not have or negligible to drive and operate machinery. However, need to be cautious because of dizziness, weakness, fatigue and drowsiness rarely occur.

Using drugs for women during pregnancy and lactation

Pregnancy:

There is no adequate data using lercanidipin in pregnant women. Non -clinical data shows that there is no evidence of the monster effect in rats and rabbits as well as the fertility on the mice is not impaired. Because other dihydropyridine compounds have teratogenicity, should not use lercanidipin for pregnant women or women of reproductive age without effective contraception.

Breastfeeding period:

Because the body's body's body's body's body is high, Lercanidipin can be plentiful in breast milk, should not use lercanidipin for breastfeeding women.

Drug interaction

lercanidipin is metabolized by CYP3A4 enzyme, so the inhibitors or CYP3A4 inhibitors can interact with the metabolism and elimination of Lercanidipin if used simultaneously.

CYP3A4 inhibitors:

Avoid using lercanidipin along with CYP3A4 inhibitors (e.g. ketoconazole, otraconazole, ritonavir, erythromycin, troleandomycin).

A study that interacts with strong inhibitors CYP3A4, Ketoconazole has shown a significant increase in plasma concentrations of lercanidipine (an increase of 15 times the area under the AUC curve, an increase of 8 times the peak concentration of the isomer S - Tercanidipine).

Increased plasma concentrations of both lercanidipin and ciclosporin are observed when used simultaneously. A study in young, healthy volunteers has shown that when using ciclosporin 3 hours after taking lercanidipin, the level of lercanidipin in plasma does not change, while the area under the AUC curve of Ciclosporin increases about 27%. However, the simultaneous use of lercanidipine with ciclosporin causes lymphatic plasma concentrations to increase 3 times, the area under the AUC curve of Ciclosporin increased by 21%. So should not use simultaneously Ciclosporin and Lercanidipin.

As well as other dihydropyridine, lercanidipine is sensitive to the inhibition of metabolism of grapefruit juice, increases the bioavailability of the body and increases the effect of lowering blood pressure. Do not take Lercaridipin with grapefruit juice.

When using Lercanidipin at the same time, oral -dose of 20 mg with oral midazolam in elderly volunteers, Lercanidipin absorption increases about 40% and the absorption rate decreases (the time of reaching the peak concentration is delayed from 1.75 to 3 hours). Midazolam concentration is not changed.

CYP3A4 touch substance:

Simultaneous use of Lercanidipin along with CYP3A4 induction such as anti -convulsions (e.g. phenytoin, carbamazepin) and rifampicin should be careful micro -blood pressure effect may be reduced, need to monitor blood pressure regularly.

CYP3A4 substrate:

Simultaneously used 20 mg of lercanidipin in chronic treatment with B - methyldigoxin indicates no evidence of pharmacokinetic interaction. In healthy volunteers treated with digoxin along with a dose of 20 mg of lercanidipin when hungry indicates the peak concentration of digoxin increases to 33%, while the area under the AUC curve and renal clearance does not change.

Patients who use simultaneously with digoxin should be closely monitored for signs of digoxin poisoning.

A interactive study with fluoxetin (a CYP2D6 and CYP3A4 inhibitor), conducted on volunteers aged 65 ± 7 years old, indicates no change in pharmacokinetics of Lercanidipin.

Simultaneously use 20 mg of lercanidipin at hunger in healthy volunteers does not change the pharmacokinetics of Warfarin.

Be cautious when prescribing lercanidipine simultaneously with the substrates of CYP3A4 such as terfenadin, astemizol, anti -arrhyths group III such as amiodaron, quinidine.

alcohol:

Should avoid using micro -alcohol may increase the vasodilation effect of antihypertensive drugs.

Other interactions:

When using Lercanidipin simultaneously with Metoprolol, a blocker - excreting mainly through the liver, the bioavailability of Metoprolol does not change while the bioavailability of Lercanidipin decreases by about 50%. This effect may be caused by a decrease in the blood flow in the liver by the B and the measurement may occur with other drugs in this group. Therefore, Lercanidipin can be used with sympathetic b blockers but must be adjusted.

When taking a dose of 20 mg of lercanidipin is repeated simultaneously with 40 mg of simvastatin, the area under the AUC curve of Lercanidipin is not changed, while the AUC of Simvastatin increases by about 56% and its active metabolites B - hydroxyacid increases by about 28%. It is not sure that this change is clinically related. There is no interaction when using lercanidipin in the morning and simvastatin in the evening. Lercanidipin is safely used with diuretics and angiotensin transferring enzymes inhibitors.