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ATV is prescribed as an adjunct to dietary modifications for managing:
- Elevated total cholesterol, LDL-C, Apo B, and triglycerides.
- Heterozygous and homozygous familial hypercholesterolemia.
- Mixed dyslipidemia (Fredrickson Types Ia and Ib).
- Hypertriglyceridemia (Fredrickson Type IV).
- Dysbetalipoproteinemia (Fredrickson Type III).
- Risk reduction of cardiac events in patients with coronary artery disease.
- Hypercholesterolemia related to diabetes mellitus or post-renal transplant.
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✅ Description:
ATV 10 mg Tablet is generally well-tolerated and considered safe. Some individuals may experience side effects like diarrhea, flatulence, or stomach upset—taking the tablet with meals may help reduce these symptoms. Patients should report any unexplained fatigue, muscle pain, or weakness to their doctor promptly.
Liver function tests are usually done prior to starting therapy and monitored periodically thereafter. Notify your physician if you observe symptoms of liver issues such as persistent abdominal pain, dark-colored urine, or yellowing of the skin/eyes.
Inform your healthcare provider if you have a history of liver or kidney disease, or if you have diabetes. Atorvastatin can cause a slight increase in blood glucose levels, so regular monitoring is advisable in diabetic patients.
Do not use this medication during pregnancy, while planning to conceive, or if you are breastfeeding.
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✔️ Pharmacokinetics
- Absorption: Rapidly absorbed with peak plasma levels within 1–2 hours. Bioavailability of the parent drug is around 14%, with about 30% systemic availability of HMG-CoA reductase inhibitory activity.
- Distribution: Large volume of distribution (~381 L). Around 98% bound to plasma proteins. Low blood/plasma ratio (~0.25) suggests limited red blood cell penetration. Likely secreted in human milk.
- Metabolism: Extensively metabolized via CYP3A4 into active metabolites (ortho- and para-hydroxylated forms), which contribute approximately 70% to its cholesterol-lowering effect.
- Excretion: Primarily excreted in bile; minimal urinary excretion (<2%). Plasma half-life is approximately 14 hours, with HMG-CoA reductase inhibitory effects lasting 20–30 hours.
✔️ Mechanism of Action
Atorvastatin is a selective HMG-CoA reductase inhibitor. This enzyme plays a crucial role in converting HMG-CoA to mevalonate, a precursor to cholesterol. Atorvastatin helps lower plasma cholesterol and lipoproteins by inhibiting cholesterol production in the liver and enhancing the uptake of LDL through increased LDL receptor expression on hepatocyte surfaces.
✔️ Dosage & Administration
Adults: Initial dose is 10–20 mg once daily. In cases requiring LDL-C reduction >45%, 40 mg may be started. Dose may be titrated up to 80 mg/day as needed.
Pediatrics (10–17 years): Starting dose is 10 mg/day; max 20 mg/day. Adjust dose at 4-week intervals.
Elderly: No dose adjustment needed.
Can be taken at any time of day, with or without food.
Grapefruit juice should be limited to less than 1 liter/day to avoid drug interaction.
✔️ Drug Interactions
- Increased Risk of Myopathy with: Cyclosporine, fibrates, niacin, erythromycin, azole antifungals.
- Antacids: May reduce plasma levels by ~35%, but the lipid-lowering effect remains unchanged.
- Colestipol: Reduces atorvastatin levels by ~25%, but enhances cholesterol-lowering effects.
- Digoxin: Co-administration raises digoxin levels (~20%). Monitoring recommended.
- Oral contraceptives: May increase hormone levels (norethindrone by ~30%, ethinyl estradiol by ~20%).
- Warfarin: No significant effect observed on prothrombin time.
✔️ Pregnancy & Lactation:
Contraindicated. Potential for fetal harm and adverse neonatal outcomes; discontinue if pregnancy occurs.
✔️ Geriatric:
Slightly higher plasma levels; more pronounced LDL-lowering effect seen.
✔️ Dialysis Patients:
Hemodialysis is unlikely to remove the drug effectively due to high protein binding.
✔️ Renal Impairment:
No dose adjustment needed.
✔️ Liver Disease:
Higher plasma concentrations; use with caution.
✔️ Common Side Effects
Gastrointestinal: Constipation, bloating, indigestion, abdominal discomfort
Others: Headache, back pain, rash, muscle/joint pain, general weakness, infections
✔️ Contraindications
- Hypersensitivity to atorvastatin or any formulation component.
- Active liver disease or persistent unexplained elevation in liver enzymes.
- History of serious adverse effects from HMG-CoA reductase inhibitors.
- Use during pregnancy or breastfeeding.
✔️ Storage:
Store in a cool, dry place away from direct light and heat. Keep out of children’s reach.
⚠️Disclaimer:
At ePharma, we’re committed to providing accurate and accessible health information. However, all content is intended for informational purposes only and should not replace medical advice from a qualified physician. Please consult your healthcare provider for personalized guidance. We aim to support, not substitute, the doctor-patient relationship.
