Zanidip

The joint Italian-Irish company Recordati Industries Chemica e Pharmaceuticals SpA The drug Lercanidipine (the international name for the drug), a calcium channel blocker, has been released to the pharmacological market. In our pharmacies it can be found under the name Zanidip. He is known to doctors as an excellent antihypertensive drug.

This material comes as an introductory and should not become an instruction for self-treatment. Any medicine must appoint a doctor based on the clinical picture of the disease. The drug Zanidip is an effective antihypertensive drug, but it should be taken only for the intended purpose and under the constant supervision of the specialized doctor.

Indications of the zanidipa

This drug is a directed action. Therefore, indications for Zanidip are not as extensive as many other pharmacological medicines, but this in no way begs for its effectiveness.

The main, and only, indication for the application of Zanidip can be called essential hypertension, the severity of which can be stated as mild or moderate (moderate). 

[1],

Release form

Active active substance Zanidip - lercanidipine hydrochloride, auxiliary chemical compounds can be named: lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch, povidone K30 and magnesium stearate.

The form of release - tablets on which the thin layer of a cover is put. The pharmacy market offers blisters with a different number of pieces (7,14,15,25,28,30 pieces respectively).

Tablets are produced in a light yellow color and have a dosage of active chemical compound lercanidipine hydrochloride - 10 mg, tablets shade from pink to dark pink - 20 mg of active ingredient. The quantitative composition of the auxiliary elements, respectively, in pink tablets is twice as concentrated. 

[2], [3]

Pharmacodynamics

Active active substance Zanidip - lercanidipine, which is a fairly strong calcium antagonist, belonging to the dihydropyridine group of chemical compounds. Lercanidipine depresses the intermembrane transport of this chemical element to the inner region of cardiomyocytes and vascular cells of smooth muscle.

Pharmacodynamics Zanidip with its active substance lercanidipine differs direct directional relaxing effect on the smooth muscles of blood vessels, this makes it possible to reduce the overall peripheral resistance of blood vessels (RPPS). The drug starts working within five to seven hours after the drug is administered, and the positive therapeutic effect persists for the next 24 hours.

High vascular selectivity (selectivity) of the drug can adequately affect the entire cardiovascular system of a person without creating a negative inotropic lesion. Zanidip (as opposed to a small T1 in blood serum), due to its high membrane distribution coefficient, is able to provide a prolonged effect on the antihypertensive characteristic of the patient's body. Lercanidipine gradually acts on the process of vasodilation, which helps to avoid sudden severe attacks of arterial hypotension with reflex tachycardia.

The results of laboratory and clinical observations showed that after the administration of Zanidip, 40% of patients with acute arterial hypotension had normal arterial pressure (the drug was prescribed to the patient once a day at a dosage of 20 mg). When taking 10 mg of lercanidipine twice a day, this percentage was higher - 56% of patients.

In the process of conducting a duplicated blind randomized monitoring study, the results of effective reduction of systolic blood pressure (BP) from figures of 172.6 ± 5.6 to indices of 140.2 ± 8.7 mm Hg were obtained. Art.

Lercanidipine behaves selectively in blocking the current of calcium ions that are transported between the cell membranes. This feature allows you to control the flow of internal calcium penetration into the cardiac and vascular walls of cells, as well as into smooth muscle cells.

[4], [5]

Pharmacokinetics

Suction. Due to its biochemical characteristics, the pharmacokinetics of Zanidip allows the active substance to be fully absorbed from the gastrointestinal tract into the human blood channels. In plasma, the peak amount of lercanidipine is observed even after the expiration of one and a half to three hours after the injection and shows figures of 3.3 ng / ml (if the patient took 10 mg twice daily) and 7.66 ng / ml (after injecting 20 mg once Zanidip).

Distribution. Metabolism of lercanidipine in all systems, organs and tissues of the patient from the blood is sufficiently mobile. The active substance shows a high percentage of interaction (more than 98%) in the process of binding to plasma proteins. If the medicine was taken after a meal, the bioavailability of the active ingredient is determined by 10%, while in the case of drug administration not later than two hours after eating a very high fat content, bioavailability increases fourfold. Proceeding from this, it follows that to obtain a greater effect, the Zanidip drug should be used in conjunction with food (that is, during or immediately after eating). When you re-enter, it does not accumulate in the body. The active substance is metabolized quite easily through the liver, biotransforming a certain amount of metabolites that do not have high pharmacological activity.

Excretion. After biotransformation, lercanidipine metabolites are excreted by the body of the patient through the kidneys through urine and intestines, together with fecal formations. Two stages of withdrawal are divided:

• The phase of early excretion. The half-life of Zanidip is two to five hours.
• Phase of the terminal excretion. The half-life of Zanidip is eight to ten hours.

Clinical analyzes show that there is practically no medication in its original form in either urine or feces.

Clinically, it has been established that the pharmacokinetics of Zanidip is practically not different in its manifestations, that people who have a history of liver and kidney pathology that have a history of elderly patients.

[6],

Dosing and administration

Most often, the method of administration and dose of Zanidip is unambiguous. The medicine is taken in by squeezing a lot of liquid. A tablet should not be chewed.

The starting daily dosage of the drug is 10 mg and taken once a 15 minutes before meals. If for two weeks the therapeutic effect does not come, the daily dose can be brought up to 20 mg, taking it once or divorced in two ways.

Correct the dosage for elderly patients is not necessary, but it is necessary to constantly monitor the patient's general well-being and, if necessary, cancel or correct the entry of Zanidip.

 If a history of the patient has a mild or moderate degree of liver and / or kidney function pathology, then dosage adjustment is not necessary, in acute forms, this medication should not be prescribed. The starting dose in this case is 10 mg, afterwards it is very accurately adjusted to 20 mg.

If the antihypertensive effect is too pronounced, the amount of medication taken must be reduced.

[10], [11], [12]

Use of the zanidipa during pregnancy

In the light of the fact that there is no complete data on the use of Zanidip during pregnancy and breastfeeding, it is not recommended to use this drug during this period.

There are data on animal testing of other dihydropyridines. The results show that preparations of this group are capable of exerting a destructive effect on the fetus in the womb of the mother, manifesting subsequently all kinds of vices and ugliness (teratogenic effect). Therefore, whenever possible, it is not necessary to use women not only during pregnancy and lactation, but also during the period when it is planned.

Due to the high degree of lipophilicity of the active substance Zanidip, the probability of its entry into breast milk is high. Therefore, it is not necessary to drink the drug during this period, in case of the medical necessity of taking it, it is necessary to stop feeding the newborn with the breast.

Contraindications

Based on the pharmacokinetics and pharmacodynamics of lercanidipine, contraindications to the use of Zanidip are sufficiently extended:

• Unstable angina.
• Heart failure of a chronic nature at the stage of decompensation.
• Violations in the functioning of the kidneys. Glomerular filtration is reduced and is less than 39 ml / min.
• If not passed a month after the happened myocardial infarction.
• Acute form of hepatic insufficiency.
• The pathology of the left cardiac ventricle and the associated vascular obstruction.
• The safety of the drug for children and adolescents has not been established. Age limit is 18 years.
• Pregnancy and lactation.
• Deficiency in the body or complete intolerance of such an enzyme as lactose.
• Contraindicated in the use of Zanidip and in conjunction with potent inhibitors (for example, such as erythromycin, itraconazole, cyclosporin, ketoconazole). Do not drink grapefruit juice while taking the medicine.
• Individual intolerance to lercanidipine or other components of the drug.
• Representatives of the fair sex of childbearing age who are planning a pregnancy in the near future.
• Heart failure in chronic form.
• Very carefully, you need to take Zanidip in conjunction with digoxin and beta-blockers.
• During the course of treatment, it is necessary to be especially careful when driving a vehicle and moving machinery.

[7], [8]

Side effects of the zanidipa

Despite the high efficiency, there are also side effects of Zanidip:

• Dizziness and headaches.
• Hypersensitivity.
• Drowsiness.
• Nausea with vomiting.
• Myocardial infarction.
• Rashes on the skin.
• Sometimes there is tachycardia and angina.
• Diarrhea.
• Flushes of blood to the facial epidermis.
• It is rare enough, but nevertheless there are faints and chest pains.
• Falling blood pressure.
• Myalgia is a muscle pain.
• Polyuria - increased urine formation.
• Increased fatigue.

[9]

Overdose

Considering pharmacokinetics and pharmacodynamics of lercanidipine and referring to the clinical monitoring of the treatment of essential hypertension, it can be argued that an overdose of Zanidip is accompanied by such symptoms:

• Peripheral vasodilation.
• reflex tachycardia.
• Falling blood pressure.
• The increase in the time of the course and frequency of manifestations of angina attacks.
• Myocardial infarction.

When these deviations occur, the attending physician ascribes drugs that are able to cure the symptoms.

[13]

Interactions with other drugs

Only an experienced doctor is able to properly assign the drug and choose the dosage. It is especially necessary to be cautious in the complex use of medicines, because the interactions of Zanidip with other drugs are not always fully understood.

 For example, it would seem, elementary grapefruit juice in combination with Zanidip stimulates the growth of the quantitative component of lercanidipine in the blood. For the same reason, you should not take this drug with inhibitors, such as itraconazole, erythromycin and others. Joint administration of cyclosporine with Zanidip provokes a surge in the concentration of both drugs in the plasma.

It is necessary to adhere to the accuracy when the patient is injected into the body with such drugs as quinidine, amiodarone, astemizole, terfenadine.

The level of lercanidipine may drop with its tandem admission with anticonvulsant medications (this group is called carbamazepine, phenytoin, rifamycin). This is due to the fact that the antihypertensive efficacy of the active substance of the Zanidip drug decreases.

Joint use of lercanidipine with midazolam in an elderly person can cause an increase in the volume of absorbed lercanidipine, while the clearance of absorption is reduced. If there was a medical need for simultaneous admission with digoxin, it is worthwhile, without stopping, to monitor the patient's condition for the manifestation of intoxication symptoms last.

Half of the bioavailability of the active substance Zanidip decreases when working in pairs with metoprolol, while its characteristics remain unchanged. Such consequences can appear due to beta-blockers, which are able to block or partially block the flow of blood through the liver. A similar situation can arise when "cooperating" with other medicinal forms of this group.

 Complex pairing with such drugs as fluoxetine or warfarin does not significantly affect the pharmacokinetics of lercanidipine. If cimetidine is administered to a patient at doses not exceeding the daily threshold of 800 mg, no significant changes in the clinic of the process are observed. While at higher dosages of the drug, the antihypertensive effect of lercanidipine can increase.

Zanidip is better to drink in the morning, and simvastatin in the evening. This will be enough to minimize mutual negative impact. If necessary, the effect of the drug under consideration is capable of ethanol.

During the period of Zanidip drug treatment, it is necessary to minimize the intake of any type of alcohol. Otherwise, this can negatively affect the pharmacodynamics of the drug, enhancing the vasodilator effect.

[14]

Storage conditions

The room temperature in which Zanedip is stored should not exceed 25 ° C - 30 ° C. The place must be chosen so that it is not accessible to young children. The storage conditions of Zanidip are quite simple and do not require much effort.

[15], [16]

Shelf life

The period of validity of the drug under consideration Zanidip is three years. The deadline for use is reflected in the package, and it should not be exceeded. If the expiration date has expired, further use of this drug is not recommended.

[17], [18]