SELECTIN ® is a drug based on pravastatin sodium salt
THERAPEUTIC GROUP: Lipid-lowering agents - HMG-CoA reductase inhibitor
Indications SELECTIN ® Pravastatin
SELECTIN ® is used as a pharmacological treatment of mixed dyslipidemia and heterozygous primary or familial hypercholesterolemia, when an appropriate diet and a correct lifestyle have not produced satisfactory therapeutic results.
SELECTIN ® can also be used in the prevention of cardiovascular diseases in patients with a previous clinical history of coronary events, myocardial infarction, cerebrovascular events and various types of diseases of the cardiovascular system.
SELECTIN ® is also used in the treatment of post-transplant hyperlipidaemia in patients undergoing immunosuppressive therapy.
SELECTIN ® mechanism of action Pravastatin
Pravastatin, taken orally, is rapidly absorbed from the gastrointestinal tract, reaching its maximum plasma concentration approximately 1.5 hours after its intake. Much of the drug undergoes first pass hepatic metabolism, with the formation of inactive metabolites, which causes the absolute bioavailability of pravastatin to drop to approximately 17% of the total dose taken.
The active share selectively penetrates into hepatic cells, exerting a "direct inhibition" on the enzyme HMG-CoA reductase, necessary for the hepatic synthesis of cholesterol. The reduction of cholesterol levels inside the hepatocyte, through a positive feedback mechanism, increases the expression of LDL receptors on the cell surface, thus improving the uptake of low density lipoproteins (called LDL). This double action, also accompanied by an "inevitable reduction in the synthesis of VLDL (precursors of LDL), determines an appreciable drop in blood concentrations of LDL cholesterol already after a week of treatment. The therapeutic effect, however, tends to be maximized only at fourth week from the start of treatment.
This biological effect, probably also supported by a pleiotropic action of statins, results in a significant reduction in cardiovascular risk and in the incidence of related diseases.
Approximately one and a half hours after ingestion, pravastatin is largely eliminated in the faeces, while the remainder is excreted in the urine.
Studies carried out and clinical efficacy
1. THE EFFECTIVENESS OF PRAVASTATIN
J Hum Hypertens. 1994 Jul; 8: 525-30.
Efficacy and safety of pravastatin in hypertensive hypercholesterolaemic patients on antihypertensive drug therapy.
Celis H, Lijnen P, Fagard R, Staessen J, Thijs L, Amery A.
This study, conducted on patients with hypercholesterolemia (total cholesterol greater than 250mg / dL) and hypertension, demonstrated how the administration of pravastatin at doses of 20 and 40 mg daily can guarantee a reduction of over 27% in total cholesterol and of approximately 35% of LDL cholesterol, regardless of the type of antihypertensive treatment performed.
2. THE PLEIOTROPIC EFFECTIVENESS OF PRAVASTATIN
Eur J Pharmacol. 2010 Mar 25; 630 (1-3): 107-11. Epub 2010 Jan 5.
In vitro antioxidant activity of pravastatin provides vascular protection.
Kassan M, Montero MJ, Sevilla MA.
Several studies around the world are trying to clarify and identify the non-lipid-lowering effects of provastatin, probably involved in the prevention of cardiovascular diseases. This study, conducted in vitro on cell cultures, demonstrated how provastatin can exert a powerful antioxidant and vasoprotective action, through mechanisms independent of the inhibition of the production of mevalonic acid.
3. ANTI-CANCER STATIN?
Eur J Cancer. 2010 Aug 18. [Epub ahead of print]
The addition of pravastatin to chemotherapy in advanced gastric carcinoma: A randomized phase II trial.
Konings IR, van der Gaast A, van der Wijk LJ, de Jongh FE, Eskens FA, Sleijfer S.
Several studies, still in an experimental phase, support the antitumor action of statins, exerted by inhibiting the synthesis of cholesterol (an element necessary for the constitution of cell membranes). This clinical trial used pravastatin as an adjuvant to chemotherapy in the treatment of advanced gastric cancer, but did not achieve any kind of improvement. The discrepancy existing between the biological hypothesis - supported by in vitro experiments - and clinical practice, does not allow us to express an unambiguous opinion on this usefulness.
Method of use and dosage
SELECTIN ® 20/40 mg pravastatin tablets: the dosage most used in the treatment of primary hypercholesterolemia is between 10 and 40mg per day, taken in a single dose, possibly before going to sleep. The formulation of the specific dosage must be carried out by the doctor after a "careful assessment of the state physio-pathological of the patient, and after excluding possible causes of secondary hypercholesterolemia. According to the therapeutic objective and the results found, it is possible to adjust the dosage after about 4 weeks, the period necessary to obtain the maximum therapeutic effect.
In any case, before undertaking any pharmacological treatment, it would be advisable to adopt a healthy lifestyle and a low-fat diet, to be continued even during the therapeutic process.
In the prevention of cardiovascular diseases, the dose of SELECTIN ® generally used was 40 mg / day, while in post transplant hyperlipidemia the dose of 10 mg / day was generally used, to eventually adjust it in case of reduced therapeutic response.
IN ANY CASE, BEFORE TAKING SELECTIN ® Pravastatin - YOU MUST BE PRESCRIBED AND CHECKED BY YOUR DOCTOR.
Warnings SELECTIN ® Pravastatin
Like other statins, pravastatin therapy requires monitoring of liver function and transaminases. It is in fact necessary to administer this drug with caution to patients with a previous clinical history of liver disease, in order to avoid - albeit rare - unpleasant side effects.
The same caution should be maintained towards patients with a previous history of myopathies, or predisposed to the development of skeletal muscle diseases; in these cases, periodic monitoring of creatine kinase levels would be necessary to avoid episodes of rhabdomyolysis. The same follow-up, on the other hand, is not required for patients without such clinical histories, as long as the absence of muscular pain and persistent weakness is always ascertained.
Given the presence of lactose among the excipients, SELECTIN ® could create gastrointestinal problems in patients with impaired glucose / galactose tolerance, or with lactase enzyme deficiency syndrome.
In light of current studies and the drug's mechanism of action, pravastatin is not expected to affect the patient's normal attention span; therefore, it does not appear to affect the ability to drive or use machines.
PREGNANCY AND BREASTFEEDING
Several studies have shown the absence of teratogenic effects of pravastatin on the fetus; however, the use of SELECTIN ® is strongly contraindicated in pregnancy, given the importance of cholesterol during the phases of embryogenesis and fetal development.
Breastfeeding should also be discontinued in case of treatment with pravastatin, even if the amounts of the active substance found in breast milk are negligible.
Interactions
Unlike many other statins and inhibitors of the HMG-CoA reductase enzyme, the hepatic metabolism of pravastatin is not supported solely by cytochrome P450 3A4. This characteristic therefore reduces the potential interactions with its inhibitors or inducers (acetylsalicylic acid, warfarin, cyclosporine. ..) and keeps its pharmacokinetic profile fairly stable.
A dose adjustment, on the other hand, is required in case of concomitant intake of other lipid-lowering drugs.
Contraindications SELECTIN ® Pravastatin
SELECTIN ® is contraindicated in case of hypersensitivity to one of its components, of various types of liver disease and during the period of pregnancy and lactation.
Undesirable Effects - Side Effects
The various studies carried out on the tolerability and safety of pravastatin have shown that the incidence of side effects is comparable to that observed in the control sample. The most common adverse reactions were all of little clinical significance and generalized, such as diarrhea, nausea, vomiting, flatulence, dizziness and asthenia.
More serious reactions involving the muscular, skeletal, cardiovascular and hepatic systems were decidedly more rare and transient, so much so that they quickly disappeared following the suspension of therapy.
Note
SELECTIN ® can only be sold under medical prescription.
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