Pharmaceutical Bulk Pitavastatin Calcium Powder

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Pitavastatin Calcium Powder Usage and Synthesis.

Among the lipid-regulating drugs, the therapeutic effect of statins is the first, among which pitavastatin has a very obvious effect. Pitavastatin Calcium is a third-generation statin anti-hyperlipidaemia drug, which is known as "super statin" together with rosuvastatin (Rosuvastatin).

Pitavastatin Calcium is one of the more effective statins in the treatment of hypercholesterolemia and familial hypercholesterolemia in the international clinical application. It is highly effective, safe and well-tolerated because its clinical effective dose is 1-2 mg/day, which is significantly lower than that of other marketed statins.

The results of phase I clinical trials showed that pitavastatin calcium at 1, 2 and 4 mg doses had clinical therapeutic significance for hyperlipidemic patients.

Uses and functions of Pitavastatin Calcium.

The main site of absorption after oral administration is the duodenum and the large intestine, the plasma protein binding rate in the human body after absorption is more than 96%, selectively distributed in the liver, and the concentration of the drug in other tissues of the body is lower than or the same as that in plasma.

Pitavastatin calcium is metabolised mainly in the liver, kidneys, lungs, heart and muscles, with metabolite concentrations lower than the drug's prototype concentration, and is excreted via the faeces, with a small amount of the drug excreted in the urine, giving a total excretion rate of almost 100%.

Healthy adult men once oral pitavastatin 0.5 ~ 8mg, t1/2 is about 10h, the plasma drug prototype of the cmax and AUC with the increase in the amount of drug administration and increase, repeated drug did not see drug accumulation.

Pharmacological Effects of Pitavastatin Calcium Raw.

Inhibit HMG-CoA reductase: Pitavastatin Calcium has a potent antagonistic inhibitory effect on HMG-CoA enzyme, with an IC50 value of 6.8nmol/L, and its strength of action is 24 times that of simvastatin and 68 times that of fluvastatin.

Obstruction of cholesterol synthesis: it can efficiently inhibit the process of cholesterol production in HepG2 of human hepatocytes, with an IC50 value of 5.8nmol/L, and its strength of action is 29 times that of simvastatin and 57 times that of atorvastatin.

However, the inhibitory effect of Calcium Pitavastatin on the enzymes involved in cholesterol production after mevalonate production was very weak.

Increase LDL receptor density: Pitavastatin can induce the synthesis of LDS receptor mRNA at an ultra-low concentration of 1 μmol/L to increase its number, leading to an increase in LDL receptor density, thus promoting LDL clearance and reducing plasma LDL-cholesterol concentration and plasma total triglyceride concentration.

Usage and dosage of Bulk Pitavastatin Calcium Powder.

Pitavastatin Calcium dosage may vary between dosage forms and sizes, so please read the specific instructions for use or follow your doctor's advice.

Pitavastatin Calcium Tablets, Pitavastatin Calcium Dispersible Tablets:

Usually, adults take 1-2 mg (i.e. 0.5-1 tablet) of this product orally once a day after dinner. The dose should be increased or decreased as appropriate according to age and therapeutic response, and it may be increased in the case of inadequate reduction of LDL-cholesterol, and the maximum daily dosage is 4 mg (i.e. 2 tablets).

1. When administered to patients with hepatic disease, the initial dosage is 1 mg (i.e., 0.5 tablets) per day and the maximum dosage is 2 mg (i.e., 1 tablet) per day.

2. Since adverse events related to rhabdomyolysis may occur as the dosage (blood concentration) of this preparation increases, due attention should be paid to pre-rhabdomyolysis symptoms such as elevated creatine kinase (phosphocreatine kinase), myoglobinuria, muscle pain, and a feeling of weakness when the dosage is increased to 4mg (i.e., 2 tablets). Administration of more than 8 mg (i.e., 4 tablets) in overseas clinical trials was discontinued due to the occurrence of rhabdomyolysis and related adverse events.

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