Usage
This combination medication is primarily prescribed for managing high homocysteine and cholesterol levels, thus reducing the risk of cardiovascular diseases. It also addresses nutritional deficiencies, particularly those related to B vitamins and vitamin D.
Alternate Names
This combination is often marketed under various brand names like Rosycap HC and Athrovas HC. It may also be referred to as Rosuvastatin + L-Methylfolate + Methylcobalamin + Pyridoxal-5-Phosphate + Vitamin D3.
How It Works
Pharmacodynamics:
- Rosuvastatin: Inhibits HMG-CoA reductase, an enzyme crucial for cholesterol synthesis in the liver. This action lowers total cholesterol, LDL cholesterol, and triglycerides, while increasing HDL cholesterol.
- L-Methylfolate, Methylcobalamin, and Pyridoxal-5-Phosphate: These vitamins are essential cofactors in homocysteine metabolism, helping reduce elevated homocysteine levels, a known risk factor for cardiovascular disease.
- Vitamin D3: Promotes calcium absorption, crucial for bone health and immune function. It may also have a role in cardiovascular health.
Pharmacokinetics:
- Rosuvastatin: Undergoes hepatic metabolism and biliary excretion.
- L-Methylfolate: Converted to tetrahydrofolic acid, the active form of folate, and is excreted renally.
- Methylcobalamin: Converted to active coenzyme forms and stored in the liver. Primarily excreted in bile.
- Pyridoxal-5-Phosphate: Converted to pyridoxal phosphate, its active form, and excreted renally.
- Vitamin D3: Metabolized in the liver and kidneys, with excretion primarily through bile.
Dosage
Dosage should be individualized based on the patient’s specific needs and clinical response. It’s important to note that this combination medication is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its primary use is for chronic management of hyperlipidemia and associated nutritional deficiencies.
Standard Dosage
Adults:
The standard dosage is typically one tablet per day, taken orally with food. However, the exact dose of rosuvastatin can range from 5mg to 40mg depending on the individual’s lipid profile and response to therapy. The vitamin components are usually present in fixed doses.
Children:
This combination is generally not recommended for children under 18 years of age due to safety and efficacy concerns, particularly regarding rosuvastatin’s effects on growth and development.
Special Cases:
- Elderly Patients: Dosage adjustments may be necessary based on renal function and potential drug interactions.
- Patients with Renal Impairment: Dose reduction of rosuvastatin may be needed in patients with moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Rosuvastatin should be used with caution, and dose adjustment might be necessary.
- Patients with Comorbid Conditions: Dosage considerations may apply for patients with diabetes, hypothyroidism, or other conditions.
Side Effects
Common Side Effects:
Nausea, constipation, stomach pain, dizziness, headache, muscle pain, weakness, and increased blood glucose levels.
Rare but Serious Side Effects:
Myopathy, rhabdomyolysis (muscle breakdown), liver dysfunction, and allergic reactions.
Long-Term Effects:
Potential long-term effects of rosuvastatin include muscle-related issues and liver enzyme abnormalities. Regular monitoring is recommended.
Contraindications
- Hypersensitivity to any component of the medication.
- Active liver disease.
- Pregnancy and breastfeeding (especially Rosuvastatin).
- Myopathy or rhabdomyolysis.
- Concomitant use of certain medications like cyclosporine.
Drug Interactions
- CYP3A4 inhibitors and inducers: These can affect rosuvastatin metabolism.
- Fibrates (gemfibrozil, fenofibrate): Increased risk of myopathy.
- Anticoagulants (warfarin): Enhanced anticoagulant effect.
- Antacids: Reduced rosuvastatin absorption.
- Alcohol: Increased risk of liver damage.
Pregnancy and Breastfeeding
This combination, especially rosuvastatin, is contraindicated in pregnancy and breastfeeding due to the potential for fetal harm and infant exposure through breast milk.
Drug Profile Summary
- Mechanism of Action: Rosuvastatin inhibits HMG-CoA reductase; B vitamins lower homocysteine; Vitamin D3 aids calcium absorption.
- Side Effects: Nausea, constipation, muscle pain, myopathy, liver dysfunction.
- Contraindications: Pregnancy, breastfeeding, active liver disease, hypersensitivity.
- Drug Interactions: CYP3A4 inhibitors/inducers, fibrates, anticoagulants, antacids.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Individualized, usually one tablet daily with food.
- Monitoring Parameters: Lipid profile, liver function tests, blood glucose, creatine kinase (for muscle health).
Popular Combinations
This specific combination is itself considered a popular combination for managing hyperlipidemia with concurrent B vitamin and vitamin D deficiencies.
Precautions
- Monitor liver function and creatine kinase levels.
- Evaluate for drug interactions.
- Encourage lifestyle modifications (diet, exercise).
- Caution in patients with renal or hepatic impairment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for this combination?
A: The recommended dosage is individualized based on the patient’s condition and response to therapy. Typically, one tablet daily taken with food is prescribed, with the rosuvastatin component ranging from 5mg to 40mg as per clinical assessment.
Q2: What are the common side effects?
A: Common side effects include nausea, constipation, stomach pain, dizziness, headache, muscle aches, weakness, and elevated blood glucose.
Q3: Is this combination safe during pregnancy or breastfeeding?
A: No, this combination, particularly rosuvastatin, is contraindicated during pregnancy and breastfeeding due to potential risks to the fetus or infant.
Q4: What are the serious side effects I should watch out for?
A: Rare but serious side effects include myopathy, rhabdomyolysis, and liver damage. Patients should report any unexplained muscle pain or weakness immediately.
Q5: Are there any drug interactions I should be aware of?
A: Yes, several drug interactions exist, notably with CYP3A4 inhibitors/inducers, fibrates, some anticoagulants, and antacids. It is essential to review the patient’s medication list for potential interactions.
Q6: How does this medication work to lower cholesterol?
A: Rosuvastatin inhibits HMG-CoA reductase, an enzyme crucial for cholesterol production in the liver. This lowers LDL cholesterol and triglycerides while raising HDL cholesterol.
Q7: Why are the B vitamins and vitamin D included in this combination?
A: The B vitamins (L-Methylfolate, Methylcobalamin, and Pyridoxal-5-Phosphate) help lower homocysteine levels, a risk factor for heart disease. Vitamin D3 promotes calcium absorption and may also contribute to cardiovascular health. These components address potential deficiencies and support overall health.
Q8: What monitoring is necessary while taking this medication?
A: Regular monitoring of lipid profile, liver function tests, blood glucose levels, and creatine kinase (to assess muscle health) is recommended, especially in patients with comorbidities or those on higher rosuvastatin doses.
Q9: Can I consume alcohol while on this medication?
A: Alcohol should be limited or avoided while taking this medication, particularly due to the increased risk of liver-related side effects from rosuvastatin.
