What is simvastatin ?
Simvastatin is a cholesterol synthesis inhibitor from the group of statins. It is a specific competitive inhibitor of HMG-CoA reductase, an enzyme which plays an essential role in the biosynthesis of cholesterol. Inhibition of this synthesis has, inter alia, increasing the number of LDL receptors in the liver as a result. This results in the lowering of LDL-cholesterol plasma level. It also decreases the VLDL-cholesterol and triglycerides, and slightly increases the HDL-cholesterol and apolipoprotein A in the plasma. Operation:. Within 2 weeks max after 4 to 6 weeks.
History
Simvastatin in 1989 was the first statin that came on the market in the Netherlands. It was for many years the best-selling cholesterol and one of the best-selling drugs. In 2003 it was sold to simvastatin for 127 million euros in the Netherlands, which occupied the second place in the top 10 drug spending in the Netherlands. The patent expired in May 2003, after which there cheaper generic versions came on the market. In 2010, simvastatin took the third place on the list of most supplied drugs to 65s.
Indications
-Treatment of homozygous familial hypercholesterolemia, primary hypercholesterolemia or mixed dyslipidemia if diet and other measures alone are not enough.
-Prevention for atherosclerotic cardiovascular disease or diabetes mellitus, with either normal or increased cholesterol levels, in addition to other measures.
Kinetic data
-Dosage 1x per day in the evening
-Simvastatin is a pro-drug. Absorption: Good. Extensive first-pass effect, which arises principal active metabolite.
-Bioavailability = <5 active="" major="" metabolite="" p="">-Maximum level = 1-2 hours (active metabolites).
-Plasma protein binding:> 95% (simvastatin, principal active metabolite).
-Metabolism: simvastatin: via hydrolysis and CYP3A4 to active and inactive metabolites. Elimination: mainly in the faeces..
-Elimination half-life = approx 2 hours.
What are the side effects of simvastatin ?
Sometimes
-Gastrointestinal disturbances (nausea, abdominal pain, constipation, flatulence, heartburn or diarrhea)
-Headache, dizziness, blurred vision, fatigue, insomnia or a feeling of weakness.
-Skin rash, itching, redness, hair loss, sensitivity to sunlight
Rarely
-Severe hypersensitivity reaction
-Muscle pain, joint pain, muscle weakness, muscle cramps and muscle breakdown
-Anemia
Very rare
-Liver inflammation
-Numbness or tingling in the limbs
-Psychological symptoms such as anxiety or depression
-Sexual disorders, such as decreased interest in sex, hard erection and delayed ejaculation