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.

Pharmacological effect

Zanidip-Recordati – Blocker of “slow” calcium channels. Lercanidipine is a racemic mixture of dextro- (R) and levorotatory (S) stereoisomers, a derivative of 1,4-dihydropyridine, capable of selectively blocking the flow of calcium ions into the cells of the vascular wall, cardiac cells and smooth muscle cells.

The mechanism of antihypertensive action is due to a direct relaxing effect on vascular smooth muscle cells. Has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after oral administration and its duration lasts for 24 hours (24 hours). Due to its high selectivity for vascular smooth muscle cells, there is no negative inotropic effect.

Zanidip®-Recordati is a metabolically neutral drug and does not have a significant effect on the content of lipoproteins and apolipoproteins in the blood serum, and also does not change the lipid profile in patients with arterial hypertension.

Pharmacokinetics:

Suction
After oral administration, lercanidipine is absorbed almost completely from the gastrointestinal tract. Cmax in blood plasma is achieved after 1.5-3 hours and is 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%.
Does not accumulate upon repeated use.

Metabolism
Metabolized during the “primary passage” through the liver by biotransformation of CYP3A4 with the formation of a number of metabolites that do not have pharmacological activity.

Removal
It is excreted by the kidneys and intestines after biotransformation. There are 2 phases of elimination of lercanidipine: early (T1/2 – 2-5 hours) and final (T1/2 – 8-10 hours). The drug is practically undetectable in unchanged form in urine and feces.

Pharmacokinetics in special clinical situations

In patients with renal and hepatic insufficiency, plasma protein levels are reduced, so the free fraction of lercanidipine may be increased.

Special instructions

During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Lercanidipine

Composition

1 tab. contains:

Active substances:

lercanidipine hydrochloride 20 mg.

Excipients:

lactose monohydrate – 60 mg,

MCC – 78 mg;

sodium carboxymethyl starch 31 mg;

povidone K30 – 9 mg;

magnesium stearate – 2 mg.

Shell (20 mg dosage):

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

Contraindications

Hypersensitivity,
decompensated CHF, unstable angina, aortic stenosis, recent myocardial infarction (within 1 month),
severe liver dysfunction, kidney dysfunction (creatinine clearance less than 12 ml/min),
women of childbearing age who do not use reliable contraception, pregnancy, lactation,
childhood and adolescence (up to 18 years).

For dosage forms containing lactose (additionally): lactose intolerance, galactosemia, glucose/galactose malabsorption syndrome.

With caution. Renal and/or liver failure, CVS (without pacemaker), ischemic heart disease, LV dysfunction, old age.

Side Effects

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

From the nervous system: rarely – drowsiness; infrequently – headache, dizziness;

From the immune system: very rarely – hypersensitivity;

From the cardiovascular system: not often – tachycardia, palpitations; “flushes” of blood to the skin of the face; rarely – angina pectoris; very rarely – fainting, marked decrease in blood pressure, chest pain, myocardial infarction;

From the digestive system: rarely – nausea, vomiting, diarrhea, abdominal pain, dyspepsia, very rarely – increased activity of liver enzymes (reversible);

From the skin: rarely – skin rash;

From the musculoskeletal system: rarely – myalgia;

From the urinary system: rarely – polyuria;

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

Interaction

Compatible with beta-blockers, diuretics, ACE inhibitors.

When used concomitantly with cardiac glycosides, it is necessary to monitor the symptoms and signs of digoxin intoxication.
Concomitant use with cimetidine does not cause significant changes in the plasma concentration of lercanidipine; at high doses of cimetidine, the bioavailability and, accordingly, the hypotensive effect of lercanidipine increases.

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

Inducers of the CYP3A4 isoenzyme (antidepressants, rifampicin) may reduce the hypotensive effect of the drug.

Grapefruit juice and ethanol may enhance the hypotensive effect of lecarnidipine.

Overdose

Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia, increased frequency and duration of angina attacks, myocardial infarction.

Treatment: symptomatic therapy.

Storage conditions

At a temperature not exceeding 30 °C. Keep out of the reach of children.

Manufacturer

Recordati chemical and pharmaceutical industry, Italy