Prinzen

Description

Prinzen contains Pitavastatin calcium, a new 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, the main feature of which is to have a synthetic cyclopropyl group as an associated radical. This chemical structure gives pitavastatin several pharmacological benefits relative to other statins, including: a) inhibition of cholesterol synthesis at lower doses than known statins; b) low magnitude metabolism, which contributes to its high bioavailability and prolonged duration of action, c) a metabolic profile that substantially reduces the risk of interactions with food and other drugs. Pitavastatin competitively inhibits HMG-CoA reductase, the enzyme that limits the rate of cholesterol biosynthesis in the liver. As a consequence of this, the number of hepatic LDL receptors increases, which promotes the uptake of circulating LDL from the blood, and reduces the blood concentrations of total cholesterol (C T) and LDL cholesterol (LDL-C). Sustained inhibition of hepatic cholesterol synthesis reduces the secretion of very low-density lipoproteins in the blood, which reduces plasma triglyceride levels.

Pharmacokinetics and pharmacodynamics

The oral absorption of Pitavastatin is 80% and is not affected by concomitant food intake. It is more than 99% bound to plasma proteins, especially albumin and alpha-1 acid glycoprotein, and its bioavailability is the highest of all statins, reaching 50% -60%. Due to its cyclopropyl radical, it is not metabolized by the cytochrome P450 (CYP3A4) or CYP2C9 (only a small fraction is metabolized by this route). Pitavastatin is metabolized to a lactone form through a glucuronidation process. This metabolite is only marginally metabolized via the cytochrome P450 pathway. This characteristic makes Pitavastatin a substance with a low risk of drug interactions. Almost all of the absorbed Pitavastatin is excreted by the hepatocyte in the bile; urinary excretion is less than 5%.

Indications

Prinzen is indicated to reduce elevated levels of Total Cholesterol, LDL, Apo B and Triglycerides and to increase HDL levels in patients with primary hypercholesterolemia or mixed dyslipidemia, when the response to diet and other non-pharmacological treatments is inadequate.


Contraindications

Prinzen is contraindicated in patients with hypersensitivity to Pitavastatin or to any of the excipients or other statins, severe liver failure, active liver disease or persistent and unjustified elevation of serum transaminases, myopathies or concomitant treatment with cyclosporine, pregnancy and lactation.

Side effects

Pitavastatin is a very safe drug, with a low rate of adverse reactions, being the same rare and mild: myalgia, arthralgia, muscle spasms, anorexia, asthenia, fatigue, anemia, insomnia, dizziness, constipation or diarrhea, dyspepsia, nausea, vomiting, abdominal pain, hives and erythema. Liver function test abnormalities.

Drug interactions

Pitavastatin is a drug with minimal interactions, since it is not significantly metabolized by CYP3A4, which is the route used by the other statins. Co-administration of Pitavastatin with cyclosporine, erythromycin, or rifampin is not recommended; since they produce a significant increase in the AUC of Pitavastatin. The use of fibrates alone, niacin, or fusidic acid is associated with myopathies; therefore, co-administration with statins increases the risk of rhabdomyolysis. If systemic treatment with fusidic acid is necessary, the use of Pitavastatin should be suspended for the entire time of its use. Co-administration with ezetimibe has no impact on the plasma concentrations of Pitavastatin. Warfarin, digoxin, itraconazole, and grapefruit juice do not have a significant effect on Pitavastatin concentrations when co-administered.

Cautions

As with other HMG-CoA reductase inhibitors, there is a possibility of developing myalgia, myopathy, and, rarely, rhabdomyolysis; therefore, the patient should be instructed to report any muscle symptoms in order to follow up accordingly. Pitavastatin should be used with caution in patients with a history of liver disease, moderate or severe renal impairment. Pitavastatin does not cause any alteration in the ability to drive and use machinery; but it must be taken into account that cases of dizziness and drowsiness have been reported during treatment with it.

Warning

Keep out of the reach of children. Sale under prescription.

Composition

Prinzen-1

Each coated tablet contains:

Pitavastatin calcium (equivalent to 1mg Pitavastatin)

C.S. excipients

Prinzen-2

Each coated tablet contains:

Pitavastatin calcium (equivalent to 2mg Pitavastatin)

C.S. excipients

Prinzen-4

Each coated caplet contains:

Pitavastatin calcium (equivalent to 2mg Pitavastatin)

C.S. excipients


Administration route

Oral


Posology

Prinzen starting dose is 1 mg once daily, adjustments should be made at intervals of 4 weeks or more. The dose should be individualized based on LDL-C levels, the treatment objective and the patient’s response. Most patients need a dose of 2 mg. The maximum daily dose is 4 mg. The tablet should be taken whole, at the same time each day (preferably at night), with or without food. Elderly: it is recommended to titrate the dose individually according to the goals and the response achieved. Patients with renal impairment: Patients with moderate renal damage or with renal replacement therapy should initially be treated with 1 mg / day of Pitavastatin and receive a maximum dose of 2 mg / day. Prinzen should not be used in patients with severe kidney damage who are not undergoing hemodialysis. Patients with mild to moderate hepatic impairment: they can receive a maximum daily dose of 2 mg, under strict control. Pediatric population: The safety and efficacy of Pitavastatin in children aged 0-18 years have not been established.


Storage Recommendations

Store below 30 °C. Protect  from light and moisture.

 


Presentation

Prinzen 1 mg: Box containing 10 and 30 coated tablets.

Prinzen 2 mg: Box containing 10 and 30 coated tablets.

Prinzen 4 mg: Box containing 10 and 30 coated caplets.