Zanidip-Recordati, 20 mg 28 pcs

Zanidip-Recordati is a “slow” calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and left- (S) stereoisomers, a derivative of 1,4-dihydropyridine, is able to selectively block the flow of calcium ions inside the cells of the vascular wall, heart cells and smooth muscle cells.

The mechanism of antihypertensive action is caused by a direct relaxant action on the vascular smooth muscle cells. It has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after oral administration and its duration lasts for 24 hours. Due to high selectivity for vascular smooth muscle cells there is no negative inotropic effect.

Zanidip®-Recordati is metabolically neutral and has no significant effect on serum lipoprotein and apolipoprotein content and does not change lipid profile in patients with arterial hypertension.

Pharmacokinetics:

Intake
Lercanidipine is almost completely absorbed from the GI tract after oral administration. Cmax in plasma is reached after 1.5-3 hours and is 3.3 ng/ml and 7.66 ng/ml after 10 mg and 20 mg administration, respectively.

Distribution
Distribution from plasma to tissues and organs is rapid. Binding to plasma proteins exceeds 98%.
It does not cumulate with repeated use.

Metabolism
Metabolized by “primary passage” through the liver by CYP3A4 biotransformation to form a number of metabolites, which have no pharmacological activity.

Elimination
It is excreted by the kidneys and the intestine after biotransformation. There are 2 phases of excretion of lercanidipine: early (T1/2 – 2-5 hours) and final (T1/2 – 8-10 hours). The drug is practically not found in unchanged form in urine and feces.

Pharmacokinetics in special clinical cases

In patients with renal and hepatic impairment, plasma protein content is decreased, so the free fraction of lercanidipine may be increased.

Indications

Essential hypertension of mild to moderate severity.

Active ingredient

Composition

1 tablet contains:

Active ingredients:

Lercanidipine hydrochloride 20 mg.

Associates:

Lactose monohydrate – 60 mg,

MCC – 78 mg;

Sodium carboxymethyl starch 31 mg;

Povidone K30 – 9 mg;

Magnesium stearate – 2 mg.

Shell (dosage 20 mg):

Opadry pink (02F25077) – 6 mg (hypromellose, talc, titanium dioxide (E171), macrogol 6000, iron oxide red dye (E172).

How to take, the dosage

Zanidip-Recordati is taken orally, in the morning, at least 15 minutes before a meal, without chewing, with plenty of water, 10 mg once a day.

The dose may be increased to 20 mg (depending on individual effect). Increase the dose to 20 mg 2 weeks after starting the drug.

In mild to moderate renal or hepatic impairment, increasing the dose to 20 mg daily should be done with caution.

Interaction

Compatible with beta-adrenoblockers, diuretics, ACE inhibitors.

In concomitant use with cardiac glycosides, symptoms and signs of intoxication with digoxin should be controlled.
Concomitant use with cimetidine does not cause significant changes in plasma concentrations of lercanidipine, at high doses of cimetidine the bioavailability and respectively the hypotensive effect of lercanidipine increases.

With caution, use with CYP3A4 inhibitors (including ketoconazole, itraconazole, erythromycin).

The inducers of CYP3A4 isoenzyme (antidepressants, rifampicin) may decrease the hypotensive effect of the drug.

Grapefruit juice, ethanol may increase the hypotensive effect of drugnidipine.

Special Instructions

During treatment, caution should be exercised when driving vehicles and engaging in potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity,
decompensated CHF, unstable angina, aortic stenosis, recent myocardial infarction (within 1 month),
Significant liver function abnormalities, renal function abnormalities (CK less than 12 ml/min),
women of childbearing age who do not use reliable contraception, pregnancy, lactation,
childhood and adolescence (under 18 years).

For lactose-containing LPs (optional): lactose intolerance, galactosemia, glucose/galactose malabsorption syndrome.

With caution. Renal and/or hepatic insufficiency, CCSU (without pacemaker), CHD, LV dysfunction, advanced age.

Side effects

WHO statistics: very common – 1/10 prescriptions, common – 1/100 prescriptions, not common – 1/1000 prescriptions, rare – 1/10000 prescriptions, very rare – less than 1/10000 prescriptions.

Nervous system disorders: rare – somnolence; infrequent – headache, dizziness;

Immune system disorders: very rare – hypersensitivity;

Cardiovascular system disorders: not frequent – tachycardia, palpitations; “rushes” of blood to the skin of the face; rare – angina pectoris; very rare – fainting, marked decrease in blood pressure, chest pain, myocardial infarction;

Digestive system disorders: rare – nausea, vomiting, diarrhea, abdominal pain, dyspepsia, very rare – increased activity of “liver” enzymes (reversible);

Skin: rare – skin rash;

Musculoskeletal disorders: rarely – myalgia;

Urinary system: rarely – polyuria;

General disorders and local reactions: not often – peripheral edema, rarely – asthenia, increased fatigue; very rarely – gum hyperplasia.

Overdose

Symptoms: peripheral vasodilation with marked BP reduction and reflex tachycardia, increased frequency and duration of angina attacks, myocardial infarction.

Treatment: symptomatic therapy.

Similarities