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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 75330-75-5
  • AHFC code: 24:06.1
  • Synonyms: 6 alpha-Methylcompactin Lovastatina [Spanish] Lovastatine [French] Lovastatinum [Latin]
  • ATC Code: C10AA02
  • Chemical Formula: C15H29N3O5
  • Molecular Weight: 404.5396
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00227 (APRD00370)
  • SMILES: CC[C,H](C)C(=O)O[C,H]1C[C,,H](C)C=C2C=C[C,H](C)[C,H](CC[C,,H]3C[C,,H](O)CC(=O)O3)[C,,H]12
  • InChl: PCZOHLXUXFIOCF-BXMDZJJMSA-N
  • PubChem: 53232
  • IUPAC: (1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl (2S)-2-methylbutanoate

Additional Details

Indication:
For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia. For primary prevention of coronary heart disease and to slow progression of coronary atherosclerosis in patients with coronary heart disease.
Pharmacodynamics:
The primary cause of cardiovascular disease is atherosclerotic plaque formation. Sustained elevations of cholesterol in the blood increase the risk of cardiovascular disease. Lovastatin lowers hepatic cholesterol synthesis by competitively inhibiting HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step in the cholesterol biosynthesis pathway via the mevalonic acid pathway. Decreased hepatic cholesterol levels causes increased uptake of low density lipoprotein (LDL) cholesterol and reduces cholesterol levels in the circulation. At therapeutic doses, lovastatin decreases serum LDL cholesterol by 29-32%, increases high density lipoprotein (HDL) cholesterol by 4.6-7.3%, and decrease triglyceride levels by 2-12%. HDL cholesterol is thought to confer protective effects against CV disease, whereas high LDL and triglyceride levels are associated with higher risk of disease.
Mode of Action:
Lovastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Lovastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 20,000 times greater affinity than its natural substrate. The bicyclic portion of lovastatin binds to the coenzyme A portion of the active site.
Metabolism:
Undergoes first pass hydrolysis to active metabolites _-hydroxyacid and 6'-hydroxy dervative.
Toxicity:
LD50>1000 mg/kg (orally in mice)
General Reference:
Bobek P, Ozdin L, Galbavy S: Dose- and time-dependent hypocholesterolemic effect of oyster mushroom (Pleurotus ostreatus) in rats. Nutrition. 1998 Mar;14(3):282-6. Pubmed
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