Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Lovastatin
Drug ID BADD_D01325
Description Lovastatin, also known as the brand name product Mevacor, is a lipid-lowering drug and fungal metabolite derived synthetically from a fermentation product of _Aspergillus terreus_.[A174550] Originally named Mevinolin, lovastatin belongs to the statin class of medications, which are used to lower the risk of cardiovascular disease and manage abnormal lipid levels by inhibiting the endogenous production of cholesterol in the liver.[A174553] More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,[A181421] which catalyzes the conversion of HMG-CoA to mevalonic acid and is the third step in a sequence of metabolic reactions involved in the production of several compounds involved in lipid metabolism and transport including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very low-density lipoprotein (VLDL). Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD, such as those with Type 2 Diabetes. The clear evidence of the benefit of statin use coupled with very minimal side effects or long term effects has resulted in this class becoming one of the most widely prescribed medications in North America.[A181087, A181406] Lovastatin and other drugs from the statin class of medications including [atorvastatin], [pravastatin], [rosuvastatin], [fluvastatin], and [simvastatin] are considered first-line options for the treatment of dyslipidemia.[A181087, A181406] Increasing use of the statin class of drugs is largely due to the fact that cardiovascular disease (CVD), which includes heart attack, atherosclerosis, angina, peripheral artery disease, and stroke, has become a leading cause of death in high-income countries and a major cause of morbidity around the world.[A181084] Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.[A181087,A181553] Use of statins to target and reduce LDL levels has been shown in a number of landmark studies to significantly reduce the risk of development of CVD and all-cause mortality.[A181090,A181093,A181096,A181427,A181475,A181538] Statins are considered a cost-effective treatment option for CVD due to their evidence of reducing all-cause mortality including fatal and non-fatal CVD as well as the need for surgical revascularization or angioplasty following a heart attack.[A181087, A181406] Evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within 5 years) statins cause a 20%-22% relative reduction in major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks.[A181397, A181403] While all statin medications are considered equally effective from a clinical standpoint, [rosuvastatin] is considered the most potent; doses of 10 to 40mg [rosuvastatin] per day were found in clinical studies to result in a 45.8% to 54.6% decrease in LDL cholesterol levels, while lovastatin has been found to have an average decrease in LDL-C of 25-40%.[A174580,A181409,A181535,A181538,A1793] Potency is thought to correlate to tissue permeability as the more lipophilic statins such as lovastatin are thought to enter endothelial cells by passive diffusion, as opposed to hydrophilic statins such as [pravastatin] and [rosuvastatin] which are taken up into hepatocytes through OATP1B1 (organic anion transporter protein 1B1)-mediated transport.[A181424,A181460] Despite these differences in potency, several trials have demonstrated only minimal differences in terms of clinical outcomes between statins.[A181438, A181427]
Indications and Usage 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.
Marketing Status Prescription; Discontinued
ATC Code C10AA02
DrugBank ID DB00227
KEGG ID D00359
MeSH ID D008148
PubChem ID 53232
TTD Drug ID D06WTZ
NDC Product Code 68001-316; 63629-7687; 55289-881; 71205-993; 68071-4271; 70518-0194; 70934-547; 70518-2009; 70518-0113; 63187-194; 0185-0072; 70934-750; 58623-0021; 68645-567; 70518-3064; 68071-1880; 43063-548; 51407-251; 71335-0819; 54458-844; 63629-3583; 71205-440; 68788-7056; 55289-692; 70515-630; 61919-676; 68788-9668; 20076-0402; 70934-755; 73309-139; 63629-8091; 50090-3396; 68071-3127; 71335-1633; 51927-5161; 51655-558; 63187-765; 51407-253; 63629-7688; 68071-2653; 0093-0928; 68254-0001; 50090-3216; 43063-493; 50090-3881; 53002-5701; 61442-142; 70518-2727; 0093-0576; 61919-941; 68001-314; 68001-315; 71205-994; 51846-1040; 71335-0045; 68180-467; 54458-846; 63187-090; 63629-1178; 67544-225; 71052-668; 70515-629; 61919-311; 61919-547; 0615-8152; 68645-566; 68180-468; 50090-0762; 68071-4955; 0185-0074; 63629-1018; 50090-0757; 63629-1464; 68788-9667; 54458-938; 0093-0926; 43063-939; 71205-992; 50090-0761; 66267-506; 63629-1191; 63187-345; 43063-983; 51846-1014; 70518-0706; 70515-628; 71205-199; 0615-8151; 51407-252; 71610-396; 43353-995; 50090-0759; 61442-141; 66267-561; 54458-845; 43063-692; 68180-469; 61442-143; 54458-936; 63187-814; 53002-1385; 54458-937
Synonyms Lovastatin | Mevinolin | Monacolin K | 6-Methylcompactin | 6 Methylcompactin | MK-803 | MK 803 | MK803 | Mevacor | Lovastatin, (1 alpha(S*))-Isomer | Lovastatin, 1 alpha-Isomer | 1 alpha-Isomer Lovastatin | Lovastatin, 1 alpha Isomer | alpha-Isomer Lovastatin, 1
Chemical Information
Molecular Formula C24H36O5
CAS Registry Number 75330-75-5
SMILES CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
ApoptosisCaspase-9P55211T9390315180944; 12576463; 16054126; 15922728
ApoptosisCaspase-8Q14790T1570015180944; 12576463; 16054126; 15922728
ApoptosisCaspase-3P42574T5794315180944; 12576463; 16054126; 15922728
ApoptosisApoptosis regulator BAXQ07812T8925115180944; 12576463; 16054126; 15922728
Cataract3-hydroxy-3-methylglutaryl-coenzyme A reductaseP04035T535851757025; 8302530; 1998274; 2488025; 2100182; 8628597; 3662274; 2393325; 2307197; 12677170; 2405804; 11833826; 2404052; 1950033; 3056429
HepatotoxicityAlanine aminotransferase 1P24298Not Available2918466; 2077527; 12848586
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.001--Not Available
Abdominal pain07.01.05.0020.000179%
Aggression19.05.01.0010.000179%Not Available
Alopecia23.02.02.001--
Amnesia19.20.01.001; 17.03.02.001--
Anaphylactic shock10.01.07.002; 24.06.02.004--Not Available
Angioedema23.04.01.001; 10.01.05.009--Not Available
Anxiety19.06.02.002--
Arthralgia15.01.02.0010.000268%
Arthritis15.01.01.001--
Asthenia08.01.01.0010.000268%Not Available
Back pain15.03.04.005--
Blood creatine phosphokinase increased13.04.01.001--
Body temperature increased13.15.01.001--Not Available
Cataract06.06.01.001--
Chest pain22.02.08.003; 08.01.08.002; 02.02.02.011--Not Available
Chills15.05.03.016; 08.01.09.001--
Confusional state19.13.01.001; 17.02.03.0050.000179%
Constipation07.02.02.001--
Death08.04.01.001--
Dehydration14.05.05.0010.000179%
Depression19.15.01.0010.000179%
Dermatitis23.03.04.002--Not Available
Dermatomyositis23.03.02.001; 15.05.01.002; 10.04.02.001--Not Available
Diarrhoea07.02.01.0010.000179%
Discomfort08.01.08.003--Not Available
Dizziness24.06.02.007; 17.02.05.003; 02.01.02.0040.000179%
Drug hypersensitivity10.01.01.0010.000179%Not Available
Dry mouth07.06.01.002--
Dysgeusia07.14.03.001; 17.02.07.003--
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