Usage
- Rosuvastatin + Telmisartan is prescribed for the management of hypertension (high blood pressure) and hypercholesterolemia (high cholesterol). It is also used to reduce the risk of cardiovascular events such as heart attacks and strokes in patients aged 55 or older with a high risk of such events.
- Pharmacological classification: This combination drug belongs to two classes: HMG-CoA reductase inhibitors (Rosuvastatin) and Angiotensin II receptor blockers (Telmisartan).
- Mechanism of action: Rosuvastatin inhibits HMG-CoA reductase, an enzyme in the liver responsible for cholesterol production. This lowers LDL (“bad”) cholesterol and triglycerides while increasing HDL (“good”) cholesterol. Telmisartan blocks the action of angiotensin II, a hormone that narrows blood vessels. This vasodilation lowers blood pressure and improves blood flow.
Alternate Names
- No widely recognized alternate names exist for this specific combination. However, it may sometimes be referred to as a fixed-dose combination (FDC) of Rosuvastatin and Telmisartan.
- Brand Names: This combination is marketed under various brand names depending on the region and manufacturer.
How It Works
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Pharmacodynamics: Rosuvastatin primarily acts on the liver to reduce cholesterol synthesis. Telmisartan acts on the vascular smooth muscle, causing vasodilation and reducing blood pressure.
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Pharmacokinetics:
- Absorption: Both drugs are absorbed orally. Rosuvastatin reaches peak plasma concentration in about 5 hours, while Telmisartan reaches it in about 0.5 to 2 hours.
- Metabolism: Rosuvastatin undergoes limited metabolism, primarily by CYP2C9. Telmisartan is mostly excreted unchanged in the feces.
- Elimination: Rosuvastatin is primarily eliminated in bile, while Telmisartan is eliminated through both biliary and renal routes.
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Mode of action: Rosuvastatin competitively inhibits HMG-CoA reductase, blocking cholesterol synthesis. Telmisartan selectively blocks the binding of angiotensin II to the AT1 receptor, preventing vasoconstriction.
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Receptor binding, enzyme inhibition, or neurotransmitter modulation: Rosuvastatin: enzyme inhibition (HMG-CoA reductase). Telmisartan: receptor blockade (AT1 receptor).
Dosage
Standard Dosage
Adults: The usual starting dose is Rosuvastatin 10 mg + Telmisartan 40 mg once daily. The dose may be titrated up to Rosuvastatin 20 mg + Telmisartan 80 mg once daily, depending on the individual patient’s response and tolerability.
Children: The safety and effectiveness of this combination have not been established in children.
Special Cases:
- Elderly Patients: Dose adjustments may be necessary depending on renal and hepatic function.
- Patients with Renal Impairment: Dose adjustment is required in severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution; dose adjustments may be necessary.
- Patients with Comorbid Conditions: Monitor for potential drug interactions and adverse effects, especially in patients with diabetes, cardiovascular disease, or other conditions.
Clinical Use Cases
This combination is not typically used in acute clinical settings like intubation, surgical procedures, mechanical ventilation, or the ICU. It is primarily intended for chronic management of hypertension and hypercholesterolemia.
Dosage Adjustments
Dosage adjustments may be necessary based on individual patient factors such as renal or hepatic impairment, drug interactions, and other comorbidities. Asian patients may require lower starting doses due to increased rosuvastatin plasma concentrations.
Side Effects
Common Side Effects: Headache, dizziness, fatigue, nausea, muscle pain, back pain, diarrhea, and upper respiratory infections.
Rare but Serious Side Effects: Rhabdomyolysis (muscle breakdown), myopathy (muscle weakness), liver dysfunction, angioedema (swelling of the face, lips, tongue, or throat), and allergic reactions.
Adverse Drug Reactions (ADR): Serious ADRs include hypersensitivity reactions, severe hypotension, hepatotoxicity, rhabdomyolysis, and angioedema.
Contraindications
- Active liver disease or unexplained persistent elevations of liver enzymes.
- Hypersensitivity to rosuvastatin, telmisartan, or any components of the formulation.
- Pregnancy.
- Concurrent use of cyclosporine.
Drug Interactions
- Concomitant use of other antihypertensives may potentiate the blood pressure-lowering effect.
- Medications that affect potassium levels (e.g., potassium supplements, potassium-sparing diuretics) may increase the risk of hyperkalemia, especially in patients with renal impairment.
- CYP2C9 inhibitors (e.g., some antifungals) may increase rosuvastatin levels.
- Gemfibrozil, some antifungals, and protease inhibitors may increase the risk of myopathy when used with rosuvastatin.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: X (Rosuvastatin) and D (Telmisartan). Contraindicated in pregnancy.
- Rosuvastatin can interfere with cholesterol synthesis, which is essential for fetal development. Telmisartan can cause fetal harm, especially during the second and third trimesters.
- It is unknown if these drugs pass into breast milk. The manufacturer recommends avoiding breastfeeding while taking Rosuvastatin + Telmisartan.
Drug Profile Summary
- Mechanism of Action: Rosuvastatin inhibits HMG-CoA reductase; Telmisartan blocks AT1 receptors.
- Side Effects: Headache, dizziness, fatigue, nausea, muscle pain; rarely, rhabdomyolysis, liver dysfunction, angioedema.
- Contraindications: Active liver disease, hypersensitivity, pregnancy, concurrent use of cyclosporine.
- Drug Interactions: Other antihypertensives, potassium-affecting drugs, CYP2C9 inhibitors.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Starting dose 10 mg/40 mg once daily, up to 20 mg/80 mg.
- Monitoring Parameters: Blood pressure, lipid profile, liver function tests, creatinine kinase (for muscle damage), serum potassium.
Popular Combinations
- This fixed-dose combination is itself a popular combination for managing hypertension and hypercholesterolemia concurrently. Other antihypertensives or lipid-lowering medications might be added if necessary.
Precautions
- Monitor liver function tests, renal function, and serum potassium.
- Patients with diabetes should be monitored closely for glycemic control.
- Educate patients about lifestyle modifications (diet, exercise, smoking cessation).
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Rosuvastatin + Telmisartan?
A: The usual starting dose is Rosuvastatin 10 mg + Telmisartan 40 mg once daily. Depending on the individual response and tolerability, the dose may be increased to a maximum of 20 mg/80 mg.
Q2: What are the main contraindications to using Rosuvastatin + Telmisartan?
A: Active liver disease, known hypersensitivity to the components, pregnancy, and concurrent cyclosporine use.
Q3: How does this combination differ from using Rosuvastatin and Telmisartan separately?
A: The fixed-dose combination improves patient compliance due to once-daily dosing.
Q4: What are the key monitoring parameters for patients on this drug?
A: Blood pressure, lipid profile (total cholesterol, LDL, HDL, triglycerides), liver function tests, serum creatinine kinase (to monitor for myopathy), and serum potassium.
Q5: What are the most serious potential side effects of this combination?
A: Rhabdomyolysis, hepatotoxicity, angioedema, and severe hypotension.
Q6: What are the potential drug interactions with Rosuvastatin + Telmisartan?
A: Interactions can occur with other antihypertensives, potassium-affecting drugs, some antifungals, gemfibrozil, and protease inhibitors.
Q7: Can this combination be used during pregnancy or breastfeeding?
A: No, it is contraindicated during pregnancy and breastfeeding.
Q8: Are there any special considerations for elderly patients?
A: Dose adjustments may be necessary based on renal and hepatic function. Start at a lower dose and titrate cautiously.
Q9: What should patients be advised regarding lifestyle modifications?
A: Patients should be encouraged to adopt a heart-healthy lifestyle, including regular exercise, a balanced diet low in saturated fats and cholesterol, and smoking cessation.
Q10: How should a missed dose be managed?
A: If a dose is missed, take it as soon as remembered unless it is close to the next scheduled dose. Do not double the dose.
