Simvastatin

Simvastatin
ATC Code C10AA01
Formula C25H38O5
Molar Mass (g·mol−1) 418,57
Physical State solid
Melting Point (°C) 127–132
CAS Number 79902-63-9
PUB Number 54454
Drugbank ID DB00641
Solubility insoluble in water

Basics

Simvastatin belongs to the class of drugs called lipid-lowering agents and statins. Simvastatin is used to lower cholesterol levels in the blood. Too high cholesterol levels (mainly LDL cholesterol) can lead to atherosclerotic diseases such as coronary heart disease or myocardial infarctions.

Simvastatin requires a prescription and is administered in tablet form.

Pharmacology

Pharmacodynamics

The effect of simvastatin results from inhibition of the enzyme HMG-CoA reductase. This enzyme is significantly involved in the synthesis of cholesterol in the liver. The inhibition therefore results in an overall lower cholesterol level in the blood. Indirectly, the reduced synthesis also increases the number of receptors for LDL cholesterol in the body's cells, as a result of which LDL cholesterol in particular is more readily absorbed from the blood into the cells.

Pharmacokinetics

The oral bioavailability of simvastatin is only about 5%. However, this value is irrelevant in the case of simvastatin, since the drug's site of action is the liver. Thus, 100% of the given dose reaches the desired target. The highest plasma concentration is reached after about 1.5-2.5 hours. Approximately 95% of the substance is bound in the blood. The majority of the substance is broken down in the liver via the CYP3A4 and CYP3A5 enzymes and excreted in the urine (40%) and stool (60%). The elimination half-life is approximately 4 hours.

Drug interactions

All drugs interacting with CYP3A4 may lead to increased plasma levels of simvastatin, resulting in serious side effects.

Toxicity

Side effects

Typical side effects include:

  • Upper abdominal discomfort
  • transaminase increase (liver enzymes)
  • myopathies (muscle damage)

These side effects occur rarely and are most common when there is an overdose or interaction with other drugs.

Toxicological data

LD50 (rat, oral): 4438 mg-kg-1

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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