Pravastatin/Mevalotin CAS No. 81093-37-0
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CAS No.81093-37-0
Chemical Name:Pravastatin
SynonymsELISOR;KOPOSTAT;MEVALOTIN;PRAVACHOL;Pravatatin;PRAVASELECT;PRAVASTATIN;Pravastatin-D9;PRAVASTATIN(RG);EPTASTATIN SODIUM
CBNumber:CB6317122
Molecular Formula:C23H36O7
Formula Weight:424.53
Pravastatin Properties
Melting point:171.2-173 °C
storage temp.: 2-8°C
solubility H2O: 19 mg/mL
form: powder
color: white
New Hypolipidemic drugs
Pravastatin is a derivative of Vastatin. It is a new type of hypolipidemic drug. It is especially suitable for primary hypercholesterolemia which is still not controlled by dietary restriction. The drug is statins, developed by Japan Sankyo Pharmaceutical Co. Ltd. and AmericanBristo1-Myers Sguibb Company. It was listed in Japan for the first time in 1989. It is a new drug of Category 4 of western medicine in China, which has a broad market prospect.
Pharmacological action
Pravastatin is a cholesterol lowering drug and is a competitive inhibitor of the Hydroxymethyl glutaryl coenzyme A reductaseh (HMG-CoA reductase). The mechanism of action is the same with lovastatin. It can inhibit the synthesis of cholesterol, increase the metabolism of low density lipoprotein (LDL) and reduce the cholesterol. It can also increase the high density lipoprotein (HDL) and reduce triglyceride. The efficacy of this product is the same as lovastatin and statins. It is used for heterozygous familial, non familial hypercholesterolemia and mixed hyperlipidemia, familial hyperlipoproteinemia type III and serum hypertriglyceridemia (type IV).
Pravastatin is an open - ring active substance, and its sodium salt is used clinically. Like other statins, this product competitively inhibits HMG-CoA reductase, reduces serum TC, LDL-C and ApoB, also decreases serum VLDL and TG, and increases HDLC and Apo-A, which is similar to lovastatin.
Pharmacokinetics
This product is absorbed orally, and its bioavailability is about 17%. The concentration of the blood drug peak is reached 1 to 1.5 hours after taking the medicine. It can be selectively distributed in liver cells. It is metabolized in the liver, the active metabolite is TK 2.5% ~ 10%. It excretes rapidly. After one oral administration, 20% and 71% is discharged through urine and feces within 96 hours. The half-life is 1.5 to 2 hours.
Adverse reaction
The occasional adverse reaction includes diarrhea, abdominal pain, and gastrointestinal discomfort as well as the rise of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, gamma glutamyl transpeptidase. Other occasional adverse reaction includes the increase of CPK and urea nitrogen and the phenomenon of urine occult blood.
Precaution
The curative effect of homozygous family hypercholesterolemia is poor. During the treatment, the liver function should be checked regularly. If the increase of SGPT and SGOT is equal to or more than three times the normal upper limit and is persistent, the treatment should be stopped. Patients with the history of liver disease or drinking history should be careful in use.
The use of HMG-COA reductase inhibitor class lipid lowering drugs can cause the increase of CPK. If the rise value is 10 times the normal limit, it should be stopped. In the course of use, if the patient has unexplained myalgia, pain, weakness, especially those with discomfort and fever, they should be reported to the doctor immediately.
Other HMG-COA reductase inhibitors such as cyclosporin, fibrinic acid derivatives, nicotinic acid, etc. can increase the incidence of myositis and myopathy.However, if pravastatin is used simultaneously with the above drugs, clinical trials indicates that the incidence of myositis and myopathy will not be increased.
Chemical Properties
Off-white Crystal