Usage
- Cilnidipine + Olmesartan Medoxomil is prescribed for the treatment of hypertension (high blood pressure). It is also used to lower the risk of cardiovascular events such as heart attacks and strokes in patients with hypertension. Some formulations in combination with Chlorthalidone are indicated for the management of chronic kidney disease (CKD) associated with hypertension.
- Pharmacological Classification: Antihypertensive (a combination of a calcium channel blocker and an angiotensin II receptor blocker).
- Mechanism of Action: Cilnidipine, a dihydropyridine calcium channel blocker, inhibits calcium influx into vascular smooth muscle and cardiac muscle, leading to vasodilation. Olmesartan Medoxomil, an angiotensin II receptor blocker (ARB), blocks the binding of angiotensin II to its receptors, preventing vasoconstriction and promoting vasodilation. The combined effect results in a significant reduction in blood pressure.
Alternate Names
- No widely recognized alternate generic names exist.
- Brand Names: Several brand names are available depending on the manufacturer and country. Examples include Olkem Cl, Cilidin O, Olmistrum LN, and others. Brand names containing Chlorthalidone include Olkem Trio, Nulong-Trio, and Olnyd Trio.
How It Works
- Pharmacodynamics: Cilnidipine reduces peripheral vascular resistance by blocking calcium channels, while Olmesartan Medoxomil blocks the vasoconstricting and aldosterone-secreting effects of angiotensin II. This dual action effectively lowers blood pressure.
- Pharmacokinetics: Both drugs are orally administered. Cilnidipine is well-absorbed, extensively metabolized by the liver (CYP3A4), and has a half-life of approximately 6-8 hours. Olmesartan Medoxomil is rapidly converted to its active metabolite, olmesartan, during absorption from the gastrointestinal tract. It is primarily excreted unchanged in bile and feces, with a half-life of 10-15 hours.
- Mode of Action: Cilnidipine primarily blocks L-type calcium channels in vascular smooth muscle, leading to vasodilation. Olmesartan blocks the AT1 subtype of angiotensin II receptors, inhibiting vasoconstriction and the release of aldosterone.
- Elimination Pathways: Cilnidipine is primarily metabolized by the liver’s CYP3A4 enzymes and eliminated in the urine and feces. Olmesartan is excreted mainly unchanged through the biliary route into the feces, with minimal renal excretion.
Dosage
Standard Dosage
Adults:
- The starting dose is typically Olmesartan Medoxomil 20 mg + Cilnidipine 10 mg once daily. The dose can be increased to Olmesartan Medoxomil 40 mg + Cilnidipine 10 mg if needed.
Children:
- Not recommended for children under 18 years of age.
Special Cases:
- Elderly Patients: Dose adjustment may be needed based on renal function.
- Patients with Renal Impairment: Lower starting doses are recommended and caution is advised.
- Patients with Hepatic Dysfunction: Dose adjustment may be required for Cilnidipine due to its hepatic metabolism.
- Patients with Comorbid Conditions: Careful monitoring is advised in patients with diabetes, heart failure, or other cardiovascular conditions.
Clinical Use Cases
Dosage in specific medical settings is determined based on patient-specific factors and overall clinical assessment. There are no established fixed dosages for clinical use cases such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments are based on individual patient response, renal/hepatic function, and co-administered medications.
Side Effects
Common Side Effects:
- Headache
- Dizziness
- Fatigue
- Nausea
- Peripheral edema (swelling of ankles/feet)
- Diarrhea
Rare but Serious Side Effects:
- Angioedema (swelling of face, lips, tongue)
- Hypotension (low blood pressure)
- Renal impairment
Long-Term Effects:
Long-term complications are rare when the drug is used as directed and monitored appropriately.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include angioedema, severe hypotension, and acute renal failure, requiring immediate medical attention.
Contraindications
- Hypersensitivity to Cilnidipine or Olmesartan Medoxomil
- Biliary obstruction
- Pregnancy (especially second and third trimesters)
- Concurrent use with aliskiren in patients with diabetes
Drug Interactions
- Other antihypertensives (additive hypotensive effect)
- Potassium supplements or potassium-sparing diuretics (risk of hyperkalemia)
- NSAIDs (may reduce antihypertensive effect)
- Grapefruit juice (may increase Cilnidipine levels)
- St. John’s wort (may interact with Olmesartan Medoxomil)
- CYP3A4 inhibitors or inducers (may alter Cilnidipine metabolism)
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated, especially during the second and third trimesters, due to potential fetal harm.
- Breastfeeding: Not recommended as both drugs can pass into breast milk.
Drug Profile Summary
- Mechanism of Action: Cilnidipine: Calcium channel blocker; Olmesartan Medoxomil: Angiotensin II receptor blocker.
- Side Effects: Headache, dizziness, fatigue, nausea, peripheral edema.
- Contraindications: Hypersensitivity, biliary obstruction, pregnancy.
- Drug Interactions: Other antihypertensives, potassium supplements, NSAIDs, grapefruit juice.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy; not recommended during breastfeeding.
- Dosage: Adults: Start with 20 mg Olmesartan + 10 mg Cilnidipine once daily.
- Monitoring Parameters: Blood pressure, renal function, electrolyte levels.
Popular Combinations
- Sometimes combined with Chlorthalidone, a thiazide diuretic, for enhanced antihypertensive effect.
Precautions
- Monitor renal function, especially in elderly patients and those with renal impairment.
- Monitor blood pressure regularly.
- Caution in patients with hepatic impairment.
- Avoid alcohol as it can exacerbate dizziness and hypotension.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cilnidipine + Olmesartan Medoxomil?
A: The initial recommended dose is Olmesartan Medoxomil 20mg + Cilnidipine 10mg once daily. This may be adjusted to a maximum of Olmesartan Medoxomil 40mg + Cilnidipine 10mg once daily as needed.
Q2: What are the common side effects?
A: Common side effects include headache, dizziness, fatigue, nausea, and peripheral edema.
Q3: Can this drug be used in pregnant or breastfeeding women?
A: No, it is contraindicated during pregnancy, particularly in the second and third trimesters. It is also not recommended for breastfeeding mothers.
Q4: Are there any significant drug interactions?
A: Yes, it can interact with other antihypertensives, potassium supplements, NSAIDs, and certain medications metabolized by CYP3A4. Grapefruit juice and St. John’s Wort can also interact with this drug. Always check for potential interactions.
Q5: What should patients do if they miss a dose?
A: If a dose is missed, they should take it as soon as they remember. However, if it is close to the time for the next dose, skip the missed dose and continue with their regular schedule. Do not double the dose.
Q6: How long does it take for this medication to work?
A: The medication can start to lower blood pressure within a few hours, but the full effects may take several weeks to be seen.
Q7: What if the medication is not effectively controlling blood pressure?
A: If blood pressure remains uncontrolled, the dose may need to be increased, or other antihypertensive medications might be added to the treatment regimen. Consultation with the physician is essential.
Q8: Are there any dietary restrictions while taking this medication?
A: Patients should reduce their intake of high-sodium foods and avoid grapefruit juice. Maintaining a healthy weight, regular exercise, and proper hydration are also recommended.
Q9: Can this medication be stopped abruptly?
A: No, patients should not discontinue this medication suddenly without consulting their physician. Abrupt cessation may lead to a rebound increase in blood pressure.
Q10: What are the monitoring parameters for this combination?
A: Regular monitoring of blood pressure, renal function, and electrolyte levels is essential.
