Cholescor Uses

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What is Cholescor?

Cholescor is in a group of drugs called HMG CoA reductase inhibitors, or "statins." Cholescor reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

Cholescor is used to lower the risk of stroke, heart attack, and other heart complications in people with diabetes, coronary heart disease, or other risk factors

Cholescor is used in adults and children who are at least 10 years old.

Cholescor may also be used for other purposes not listed in this medication guide.

Cholescor indications

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Therapy with Cholescor™ (Cholescor) Extended-Release Tablets should be a component of multiple risk factor intervention in those individuals with dyslipidemia who are at risk for atherosclerotic

vascular disease. Cholescor™ (Cholescor extended-release tablets) should be used in addition to a diet restricted in saturated fat and cholesterol as part of a treatment strategy to lower Total-C and LDL-C to target levels when the response to diet and other nonpharmacological measures alone has been inadequate to reduce risk.

Cholescor™ (Cholescor extended-release tablets)

Primary Prevention of Coronary Heart Disease

In individuals without symptomatic cardiovascular disease, average to moderately elevated Total-C and LDL-C, and below average HDL-C, Cholescor™ (Cholescor extended-release tablets) is indicated to reduce the risk of:

Coronary Heart Disease

Cholescor™ (Cholescor extended-release tablets) is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower Total-C and LDL-C to target levels.

Hyperlipemia

Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for artherosclerotic vascular disease due to hypercholesterolemia

Cholescor™ (Cholescor extended-release tablets) is indicated as an adjunct to diet for the reduction of elevated Total-C, LDL-C, Apo B, and TG, and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb, see Table VI) when the response to diet restricted in saturated fat and cholesterol and to other non-pharmacological measures alone has been inadequate.

General Recommendations

Prior to initiating therapy with Cholescor™ (Cholescor extended-release tablets), secondary causes for hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism) should be excluded, and a lipid profile performed to measure Total-C, HDL-C, and TG. For patients with TG less than 400 mg/dL ( < 4.5 mmol/L), LDL-C can be estimated using the following equation:

LDL-C = Total-C - [0.2

How should I use Cholescor?

Use Cholescor extended-release tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Ask your health care provider any questions you may have about how to use Cholescor extended-release tablets.

Uses of Cholescor in details

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Cholescor is used to decrease the amount of fatty substances such as low-density lipoprotein (LDL), bad cholesterol and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL), good cholesterol in the blood.

Cholescor description

Cholescor is a cholesterol-lowering agent that belongs to the class of medications called statins. It was the second agent of this class discovered. It was discovered by Alfred Alberts and his team at Merck in 1978 after screening only 18 compounds over 2 weeks. The agent, also known as mevinolin, was isolated from the fungi Aspergillus terreus. Research on this compound was suddenly shut down in 1980 and the drug was not approved until 1987. Interesting, Akira Endo at Sankyo Co. (Japan) patented Cholescor isolated from Monascus ruber four months before Merck. Cholescor was found to be 2 times more potent than its predecessor, mevastatin, the first discovered statin. Like mevastatin, Cholescor is structurally similar to hydroxymethylglutarate (HMG), a substituent of HMG-Coenzyme A (HMG-CoA), a substrate of the cholesterol biosynthesis pathway via the mevalonic acid pathway. Cholescor is a competitive inhibitor of HMG-CoA reductase with a binding affinity 20,000 times greater than HMG-CoA. Cholescor differs structurally from mevastatin by a single methyl group at the 6’ position. Cholescor is a prodrug that is activated by in vivo hydrolysis of the lactone ring. It, along with mevastatin, has served as one of the lead compounds for the development of the synthetic compounds used today.

Cholescor dosage

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The patient should be placed on a standard cholesterol-lowering diet before receiving Cholescor™ (Cholescor extended-release tablets) and should continue on this diet during treatment with Cholescor™ (Cholescor extended-release tablets).

The usual recommended starting dose is 20, 40, or 60 mg once a day given in the evening at bedtime. The recommended dosing range is 10-60 mg/day, in single doses. Doses should be individualized according to the recommended goal of therapy. A starting dose of 10 mg may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more.

Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of Cholescor™ (Cholescor extended-release tablets) if cholesterol levels fall significantly below the targeted range.

Dosage in Patients Taking Cyclosporin

In patients taking cyclosporin concomitantly with Cholescor™, therapy should begin with 10 mg of Cholescor™ (Cholescor extended-release tablets) and should not exceed 20 mg/day.

Dosage in Patients Taking Amiodarone or Verapamil

In patients taking amiodarone or verapamil concomitantly with ALTOCORTM, the dose should not exceed 40 mg/day.

Concomitant Lipid-Lowering Therapy

Use of Cholescor™ (Cholescor extended-release tablets) with fibrates or niacin should generally be avoided. However, if Cholescor™ (Cholescor extended-release tablets) is used in combination with gemfibrozil, other fibrates, or lipid-lowering doses ( ≥ 1 g/day) of niacin, the dose of Cholescor™ should not exceed 20 mg.

Dosage in Patients with Renal Insufficiency

In patients with severe renal insufficiency (creatinine clearance < 30 mL/min), dosage increases above 20 mg/day should be carefully considered and, if deemed necessary, implemented cautiously.

How supplied

Cholescor™ (Cholescor) Extended-Release Tablets are supplied as round, convex shaped tablets containing 10 mg, 20 mg, 40 mg and 60 mg of Cholescor.

NDC 62022-760-30: 10 mg extended-release dark orange-colored tablets imprinted with Andrx logo and 10 on one side, bottles of 30.

NDC 62022-770-30: 20 mg extended-release orange-colored tablets imprinted with Andrx logo and 20 on one side, bottles of 30.

NDC 62022-780-30: 40 mg extended-release peach-colored tablets imprinted with Andrx logo and 40 on one side, bottles of 30.

NDC 62022-781-30: 60 mg extended-release light peach-colored tablets imprinted with Andrx logo and 60 on one side, bottles of 30.

Storage

Store at controlled room temperature 20°- 25° C (68°- 77°F) Avoid excessive heat and humidity.

Distributed by: Andrx Laboratories, Inc. Weston, Florida 33331. Rev. date: 7/03.

Cholescor interactions

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What other drugs will affect Cholescor?

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Drug interaction studies have not been performed with Cholescor™ (Cholescor extended-release tablets). The types, frequencies and magnitude of drug interactions that may be encountered when Cholescor™ (Cholescor extended-release tablets) is administered with other drugs may differ from the drug interactions encountered with the Cholescor immediate-release formulation. In addition, as the drug exposure with Cholescor™ 60 mg is greater than that with Cholescor immediate-release 80 mg (maximum recommended dose), the severity and magnitude of drug interactions that may be encountered with Cholescor™ (Cholescor extended-release tablets) 60 mg are not known. It is therefore recommended that the following precautions and recommendations for the concomitant administration of Cholescor immediate-release with other drugs be interpreted with caution, and that the monitoring of the pharmacologic effects of Cholescor™ (Cholescor extended-release tablets) and/or other concomitantly administered drugs be undertaken where appropriate.

CYP3A4 Interactions

Cholescor is metabolized by CYP3 A4 but has no CYP3A4 inhibitory activity; therefore it is not expected to affect the plasma concentrations of other drugs metabolized by CYP3A4. Potent inhibitors of CYP3A4 (below) increase the risk of myopathy by reducing the elimination of Cholescor. See WARNINGS, Myopathy/Rhabdomyolysis, and CLINICAL PHARMACOLOGY, Pharmacokinetics.

Itraconazole

Ketoconazole

Erythromycin

Clarithromycin

HIV protease inhibitors

Nefazodone

Cyclosporine

Large quantities of grapefruit juice ( > 1 quart daily)

Interactions with lipid-lowering drugs that can cause myopathy when given alone

The risk of myopathy is also increased by the following lipid-lowering drugs that are not potent CYP3A4 inhibitors, but which can cause myopathy when given alone.

Other drug interactions

Amiodarone or Verapamil: The risk of myopathy/rhabdomyolysis is increased when either amiodarone or verapamil is used concomitantly with a closely related member of the HMG-CoA reductase inhibitor class.

Coumarin Anticoagulants: In a small clinical trial in which Cholescor was administered to warfarin treated patients, no effect on prothrombin time was detected. However, another HMG-CoA reductase inhibitor has been found to produce a less than two seconds increase in prothrombin time in healthy volunteers receiving low doses of warfarin. Also, bleeding and/or increased prothrombin time has been reported in a few patients taking coumarin anticoagulants concomitantly with Cholescor. It is recommended that in patients taking anticoagulants, prothrombin time be determined before starting Cholescor and frequently enough during early therapy to ensure that no significant alteration of prothrombin time occurs. Once a stable prothrombin time has been documented, prothrombin times can be monitored at the intervals usually recommended for patients on coumarin anticoagulants. If the dose of Cholescor is changed, the same procedure should be repeated. Cholescor therapy has not been associated with bleeding or with changes in prothrombin time in patients not taking anticoagulants.

Antipyrine: Cholescor had no effect on the pharmacokinetics of antipyrine or its metabolites. However, since Cholescor is metabolized by the cytochrome P450 isoform 3A4, this does not preclude an interaction with other drugs metabolized by the same isoform.

Propranolol: In normal volunteers, there was no clinically significant pharmacokinetic or pharmacodynamic interaction with concomitant administration of single doses of Cholescor and propranolol.

Digoxin: In patients with hypercholesterolemia, concomitant administration of Cholescor and digoxin resulted in no effect on digoxin plasma concentrations.

Oral Hypoglycemic Agents:

In pharmacokinetic studies of Cholescor immediate-release in hypercholesterolemic non-insulin dependent diabetic patients, there was no drug interaction with glipizide or with chlorpropamide.

Endocrine Function

HMG-CoA reductase inhibitors interfere with cholesterol synthesis and as such might theoretically blunt adrenal and/or gonadal steroid production. Results of clinical trials with drugs in this class have been inconsistent with regard to drug effects on basal and reserve steroid levels. However, clinical studies have shown that Cholescor does not reduce basal plasma cortisol concentration or impair adrenal reserve, and does not reduce basal plasma testosterone concentration. Another HMG-CoA reductase inhibitor has been shown to reduce the plasma testosterone response to HCG. In the same study, the mean testosterone response to HCG was slightly but not significantly reduced after treatment with Cholescor 40 mg daily for 16 weeks in 21 men. The effects of HMG-CoA reductase inhibitors on male fertility have not been studied in adequate numbers of male patients. The effects, if any, on the pituitary-gonadal axis in premenopausal women are unknown. Patients treated with Cholescor who develop clinical evidence of endocrine dysfunction should be evaluated appropriately. Caution should also be exercised if an HMG-CoA reductase inhibitor or other agent used to lower cholesterol levels is administered to patients also receiving other drugs (e.g., ketoconazole, spironolactone, cimetidine) that may decrease the levels or activity of endogenous steroid hormones.

CNS Toxicity

Cholescor produced optic nerve degeneration (Wallerian degeneration of retinogeniculate fibers) in clinically normal dogs in a dose-dependent fashion starting at 60 mg/kg/day, a dose that produced mean plasma drug levels about 30 times higher than the mean drug level in humans taking the highest recommended dose (as measured by total enzyme inhibitory activity). Vestibulocochlear Wallerian-like degeneration and retinal ganglion cell chromatolysis were also seen in dogs treated for 14 weeks at 180 mg/kg/day, a dose which resulted in a mean plasma drug level (Cmax) similar to that seen with the 60 mg/kg/day dose.

CNS vascular lesions, characterized by perivascular hemorrhage and edema, mononuclear cell infiltration of perivascular spaces, perivascular fibrin deposits and necrosis of small vessels, were seen in dogs treated with Cholescor at a dose of 180 mg/kg/day, a dose which produced plasma drug levels (Cmax) which were about 30 times higher than the mean values in humans taking 80 mg/day.

Similar optic nerve and CNS vascular lesions have been observed with other drugs of this class. Cataracts were seen in dogs treated for 11 and 28 weeks at 180 mg/kg/day and 1 year at 60 mg/kg/day.

Cholescor side effects

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What are the possible side effects of Cholescor?

Cholescor™ (Cholescor extended-release tablets)

Cholescor™ (Cholescor extended-release tablets) Clinical Studies

In clinical studies with Cholescor™ (Cholescor extended-release tablets), adverse reactions have generally been mild and transient. In controlled studies with 467 patients who received Cholescor™ (Cholescor extended-release tablets), < 3% of patients were discontinued due to adverse experiences attributable to Cholescor (Cholescor extended-release tablets) ™. This was similar to the discontinuation rate in the placebo and Cholescor immediate-release treatment groups. Pooled results from clinical studies with Cholescor™ (Cholescor extended-release tablets) show that the most frequently reported adverse reactions in the Cholescor™ (Cholescor extended-release tablets) group were infection, headache and accidental injury. Similar incidences of these adverse reactions were seen in the Cholescor and placebo groups. The most frequent adverse events thought to be related to Cholescor™ (Cholescor extended-release tablets) were nausea, abdominal pain, insomnia, dyspepsia, headache, asthenia, and myalgia. In controlled trials (e.g., vs. placebo and vs. Cholescor immediate-release), clinical adverse experiences reported as ≥ 5% in any treatment group are shown in Table VII below.

Table VII: Pooled Controlled Studies TESS by Body System and COSTART Term, Most Common ( ≥ 5% in Any Group)

Randomized Patients Treatment
n = Placebo 34 Cholescor™ 467 Cholescor™ 329
Body System COSTART Term
Body as a Whole Infection 3 (9) 52 (11) 52 (16)
Accidental Injury 3 (9) 26 (6) 12 (4)
Asthenia 2 (6) 12 (3) 6 (2)
Headache 2 (6) 34 (7) 26 (8)
Back Pain 1 (3) 23 (5) 18 (5)
Flu Syndrome 1 (3) 24 (5) 18 (5)
Pain 0 14 (3) 17 (5)
Digestive Diarrhea 2 (6) 15 (3) 8 (2)
Musculoskeletal Arthralgia 2 (6) 24 (5) 20 (6)
Myalgia 5 (15) 14 (3) 11 (3)
Nervous Dizziness 2 (6) 10 (2) 5 (2)
Respiratory Sinusitis 1 (3) 17 (4) 20 (6)
Urogenital Urinary Tract Infection 2 (6) 8 (2) 9 (3)

Cholescor Immediate-Release

Cholescor Immediate-Release Phase III Clinical Studies

In Phase III controlled clinical studies involving 613 patients treated with Cholescor immediate-release, the adverse experience profile was similar to that shown below for the 8,245-patient EXCEL study. Persistent increases of serum transaminases have been noted. About 11% of patients had elevations of CK levels of at least twice the normal value on one or more occasions. The corresponding values for the control agent cholestyramine was 9 %. This was attributable to the noncardiac fraction of CK. Large increases in CK have sometimes been reported.

Expanded Clinical Evaluation of Cholescor (EXCEL) Study

Cholescor immediate-release was compared to placebo in 8,245 patients with hypercholesterolemia [Total-C 240-300 mg/dL (6.2-7.8 mmol/L)] in the randomized, double-blind, parallel, 48-week EXCEL study. Clinical adverse experiences reported as possibly, probably or definitely drug-related in ≥ 1% in any treatment group are shown in the table below. For no event was the incidence on drug and placebo statistically different.

Table VIII: Clinical Adverse Events Reported as Possibly, Probably or Definitely Drug-Related in ≥ 1% in Any Treatment Group in the EXCEL Study

Placebo

(N=1663)

%

Cholescor IR

20 mg q.p.m.

(N=1642)

%

Cholescor IR

40 mg q.p.m.

(N=1645)

%

Cholescor IR

20 mg b.i.d.

(N=1646)

%

Cholescor IR

40 mg b.i.d.

(N=1649)

%

Body As a Whole
Asthenia 1.4 1.7 1.4 1.5 1.2
Gastrointestinal
Abdominal pain 1.6 2.0 2.0 2.2 2.5
Constipation 1.9 2.0 3.2 3.2 3.5
Diarrhea 2.3 2.6 2.4 2.2 2.6
Dyspepsia 1.9 1.3 1.3 1.0 1.6
Flatulence 4.2 3.7 4.3 3.9 4.5
Nausea 2.5 1.9 2.5 2.2 2.2
Musculoskeletal
Muscle cramps 0.5 0.6 0.8 1.1 1.0
Myalgia 1.7 2.6 1.8 2.2 3.0
Nervous System/Psychiatric
Dizziness 0.7 0.7 1.2 0.5 0.5
Headache 2.7 2.6 2.8 2.1 3.2
Skin Rash 0.7 0.8 1.0 1.2 1.3
Special Senses
Blurred vision 0.8 1.1 0.9 0.9 1.2

Other clinical adverse experiences reported as possibly, probably or definitely drug-related in 0.5% to 1.0% of patients in any drug-treated group are listed below. In all these cases the incidence on drug and placebo was not statistically different. Body as a Whole: chest pain; Gastrointestinal: acid regurgitation, dry mouth, vomiting; Musculoskeletal: leg pain, shoulder pain, arthralgia; Nervous System/Psychiatric: insomnia, paresthesia; Skin: alopecia, pruritus; Special Senses: eye irritation.

In the EXCEL study, 4.6% of the patients treated up to 48 weeks were discontinued due to clinical or laboratory adverse experiences which were rated by the investigator as possibly, probably or definitely related to therapy with Cholescor immediate-release. The value for the placebo group was 2.5%.

Air Force/Texas Coronary Atherosclerosis Prevention Study (AFCAPS/TexCAPS)

In AFCAPS/TexCAPS involving 6,605 participants treated with 20-40 mg/day of Cholescor immediate-release (n=3,304) or placebo (n=3,301), the safety and tolerability profile of the group treated with Cholescor immediate-release was comparable to that of the group treated with placebo during a median of 5.1 years of follow-up. The adverse experiences reported in

AFCAPS/TexCAPS were similar to those reported in EXCEL.

Concomitant Therapy

In controlled clinical studies in which Cholescor immediate-release was administered concomitantly with cholestyramine, no adverse reactions peculiar to this concomitant treatment were observed. The adverse reactions that occurred were limited to those reported previously with Cholescor or cholestyramine. Other lipid-lowering agents were not administered concomitantly with Cholescor during controlled clinical studies. Preliminary data suggests that the addition of gemfibrozil to therapy with Cholescor is not associated with greater reduction in LDL-C than that achieved with Cholescor alone. In uncontrolled clinical studies, most of the patients who have developed myopathy were receiving concomitant therapy with cyclosporine, gemfibrozil or niacin (nicotinic acid)

The following effects have been reported with drugs in this class. Not all the effects listed below have necessarily been associated with Cholescor therapy.

Skeletal: muscle cramps, myalgia, myopathy, rhabdomyolysis, arthralgias.

Neurological: dysfunction of certain cranial nerves (including alteration of taste, impairment of extra-ocular movement, facial paresis), tremor, dizziness, vertigo, memory loss, paresthesia, peripheral neuropathy, peripheral nerve palsy, psychic disturbances, anxiety, insomnia, depression.

Hypersensitivity Reactions: An apparent hypersensitivity syndrome has been reported rarely which has included one or more of the following features: anaphylaxis, angioedema, lupus erythematous-like syndrome, polymyalgia rheumatica, dermatomyositis, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia, positive ANA, ESR increase, eosinophilia, arthritis, arthralgia, urticaria, asthenia, photosensitivity, fever, chills, flushing, malaise, dyspnea, toxic epidermal necrolysis, erythema multiforme, including Stevens-Johnson syndrome.

Gastrointestinal: pancreatitis, hepatitis, including chronic active hepatitis, cholestatic jaundice, fatty change in liver; and rarely, cirrhosis, fulminant hepatic necrosis, and hepatoma; anorexia, vomiting.

Skin: alopecia, pruritus. A variety of skin changes (e.g., nodules, discoloration, dryness of skin/mucous membranes, changes to hair/nails) have been reported.

Reproductive: gynecomastia, loss of libido, erectile dysfunction.

Eye: progression of cataracts (lens opacities), ophthalmoplegia.

Laboratory Abnormalities: elevated transaminases, alkaline phosphatase, y-glutamyl transpeptidase, and bilirubin; thyroid function abnormalities.

Cholescor contraindications

See also:
What is the most important information I should know about Cholescor?

Hypersensitivity to any component of this medication. Active liver disease or unexplained persistent elevations of serum transaminases.

Pregnancy and Lactation

Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hypercholesterolemia. Moreover, cholesterol and other products of the cholesterol biosynthesis pathway are essential components for fetal development, including synthesis of steroids and cell membranes. Because of the ability of inhibitors of HMG-CoA reductase such as Cholescor™ (Cholescor extended-release tablets) to decrease the synthesis of cholesterol and possibly other products of the cholesterol biosynthesis pathway, Cholescor™ (Cholescor extended-release tablets) is contraindicated during pregnancy and in nursing mothers. Cholescor™ (Cholescor extended-release tablets) should be administered to women of childbearing age only when such patients are highly unlikely to conceive. If the patient becomes pregnant while taking this drug, Cholescor™ (Cholescor extended-release tablets) should be discontinued immediately and the patient should be apprised of the potential hazard to the fetus.



Active ingredient matches for Cholescor:

Lovastatin in Pakistan.


Unit description / dosage (Manufacturer)Price, USD
Cholescor 400 mg x 30's$ 19.22
Cholescor 400 mg x 60's$ 31.87

List of Cholescor substitutes (brand and generic names):

Cholstatin 20 mg x 3 Blister x 10 Tablet
Cholvastin 20 mg x 3 x 10's (Sanbe)$ 30.13
Tablet; Oral; Lovastatin 20 mg
Tablet; Oral; Lovastatin 40 mg
Delipic 20 mg x 3 Blister x 10 Tablet
Delipic 20 mg x 30's
Delipic 20 mg x 300's
Tablet; Oral; Lovastatin 20 mg
Tablet; Oral; Lovastatin 40 mg
Dom-lovastatin tablet 20 mg (Dominion Pharmacal (Canada))
Dom-lovastatin tablet 40 mg (Dominion Pharmacal (Canada))
Ellanco 20 mg x 1's (Duopharma)
Ellanco 20 mg x 100's (Duopharma)
Ellanco 20 mg x 250's (Duopharma)
Ellanco 20 mg x 500's (Duopharma)
10 mg x 10's (Glenmark)$ 0.60
20 mg x 10's (Glenmark)$ 0.96
Elstatin 10mg TAB / 10 (Glenmark)$ 0.60
Elstatin 20mg TAB / 10 (Glenmark)$ 0.96
Elstatin 20 mg x 10 x 10's (Glenmark)
ELSTATIN 20 MG TABLET 1 strip / 10 tablets each (Glenmark)$ 0.96
ELSTATIN tab 10 mg x 10's (Glenmark)$ 0.60
ELSTATIN tab 20 mg x 10's (Glenmark)$ 0.96
Elstatin 20mg Tablet (Glenmark)$ 0.10
Elstin 10mg TAB / 10 (East West)$ 0.63
Elstin 20mg TAB / 10 (East West)$ 0.89

References

  1. DailyMed. "LOVASTATIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. PubChem. "lovastatin". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
  3. DrugBank. "lovastatin". http://www.drugbank.ca/drugs/DB00227 (accessed September 17, 2018).

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