Cilnidipine + Telmisartan

Usage

• Cilnidipine + Telmisartan is primarily prescribed for the treatment of essential hypertension (high blood pressure). It is used when monotherapy with either drug alone does not adequately control blood pressure. This combination also indirectly helps to reduce the risk of cardiovascular events like heart attacks and strokes.
• Pharmacological Classification: This combination includes two classes: a calcium channel blocker (Cilnidipine) and an angiotensin II receptor blocker (ARB) (Telmisartan).
• Mechanism of Action: Cilnidipine blocks calcium channels in vascular smooth muscle, leading to vasodilation and reduced peripheral resistance. Telmisartan blocks the angiotensin II receptor, preventing vasoconstriction and aldosterone release, further contributing to lower blood pressure.

Alternate Names

• No widely recognized alternate generic names exist.
• Several brand names are available, varying by region and manufacturer (e.g., Cilacar T, Telma LN, etc. - Note that brand names are subject to change and vary by location. Always verify locally available brands).

How It Works

• Pharmacodynamics: Cilnidipine acts by inhibiting calcium influx into vascular smooth muscle cells, resulting in vasodilation and decreased peripheral vascular resistance. Telmisartan blocks the effects of angiotensin II, a hormone that causes vasoconstriction and aldosterone release, thus preventing these effects and promoting vasodilation.
• Pharmacokinetics: Cilnidipine is well-absorbed orally, with peak plasma concentration reached within 2-4 hours. It is extensively metabolized by the liver (primarily CYP3A4 enzyme) and has a half-life of approximately 6-8 hours. Telmisartan is also well-absorbed orally but undergoes minimal hepatic metabolism and is primarily excreted unchanged in bile. It has a longer half-life of around 24 hours.
• Mode of Action: Cilnidipine blocks L-type calcium channels, which are crucial for vascular smooth muscle contraction. Telmisartan competitively binds to the angiotensin II type 1 (AT1) receptor, preventing the binding of angiotensin II and its subsequent vasoconstrictive effects.
• Elimination Pathways: Cilnidipine is primarily metabolized by the liver, with metabolites and unchanged drug excreted in feces and urine. Telmisartan is predominantly excreted unchanged in bile.

Dosage

Standard Dosage

Adults:

• The standard dose is one tablet (usually Cilnidipine 10mg + Telmisartan 40mg) orally once daily.
• The dose can be increased (e.g., to Cilnidipine 20mg + Telmisartan 40/80mg) based on individual blood pressure response and tolerability after 2-4 weeks. Maximum daily doses for individual components (Cilnidipine 20mg and Telmisartan 80mg) should not be exceeded.

Children:

• Not recommended for use in children under 18 years of age. Safety and efficacy have not been established.

Special Cases:

• Elderly Patients: A lower starting dose may be considered in elderly patients due to the increased likelihood of impaired hepatic, renal, or cardiac function. Dose titration should be done cautiously.
• Patients with Renal Impairment: Dose adjustment may be required depending on the degree of impairment. Careful monitoring of renal function is advisable.
• Patients with Hepatic Dysfunction: Use with caution in patients with mild to moderate hepatic impairment. Dose adjustment may be needed. Contraindicated in severe hepatic impairment and biliary obstructive disorders.
• Patients with Comorbid Conditions: Careful monitoring and dose adjustments may be necessary in patients with diabetes, cardiovascular disease, or other comorbidities.

Clinical Use Cases

• Cilnidipine + Telmisartan is not specifically indicated for use in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like cardiac arrest. Its primary indication is chronic hypertension management.

Dosage Adjustments

• Dose adjustments should be based on patient response, tolerability, renal function, hepatic function, and concomitant medications. Genetic polymorphisms affecting drug metabolism might also warrant dose modifications.

Side Effects

Common Side Effects

• Dizziness, headache, peripheral edema, flushing, fatigue, back pain, gastrointestinal disturbances (nausea, diarrhea).

Rare but Serious Side Effects

• Hypotension, angioedema, hyperkalemia, acute renal failure, hepatic dysfunction, allergic reactions.

Long-Term Effects

• Potential long-term effects include electrolyte imbalances, renal impairment, cardiovascular events if blood pressure is not adequately controlled.

Adverse Drug Reactions (ADR)

• Clinically significant ADRs requiring immediate attention include angioedema, severe hypotension, acute renal failure, and allergic reactions.

Contraindications

• Hypersensitivity to cilnidipine or telmisartan.
• Cardiogenic shock, severe aortic stenosis, recent history of unstable angina or acute myocardial infarction, heart failure, severe hypotension.
• Second and third trimesters of pregnancy.
• Severe hepatic impairment and biliary obstructive disorders.
• Concomitant use with aliskiren in patients with diabetes or renal impairment (GFR < 60 ml/min/1.73 m2).

Drug Interactions

• Cilnidipine: Antipsychotics, antidiabetics, antiepileptics (phenytoin, carbamazepine), rifampicin, quinidine, erythromycin, other antihypertensives, aldesleukin.
• Telmisartan: Aliskiren, digoxin, lithium, NSAIDs (including COX-2 inhibitors).
• Other Interactions: Potassium-sparing diuretics, potassium supplements, alcohol, grapefruit juice.

Pregnancy and Breastfeeding

• Pregnancy Safety Category: Contraindicated in the second and third trimesters. Not recommended in the first trimester. Angiotensin II receptor blockers can cause fetal harm.
• Breastfeeding: Excretion in breast milk is unknown, but potential for adverse effects in infants exists. Use is generally not recommended.

Drug Profile Summary

• Mechanism of Action: Calcium channel blockade (Cilnidipine) and angiotensin II receptor blockade (Telmisartan).
• Side Effects: Dizziness, headache, edema, flushing, fatigue, gastrointestinal upset. Rarely: hypotension, angioedema, renal impairment.
• Contraindications: Hypersensitivity, pregnancy, severe hepatic/renal impairment, certain cardiovascular conditions.
• Drug Interactions: Multiple drug interactions, including with antihypertensives, antidiabetics, and NSAIDs.
• Pregnancy & Breastfeeding: Contraindicated in second and third trimesters of pregnancy, not recommended during breastfeeding.
• Dosage: One tablet daily (typically 10mg/40mg), adjustable based on individual response.
• Monitoring Parameters: Blood pressure, renal function, electrolyte levels, liver function tests (as needed).

Popular Combinations

• While Cilnidipine + Telmisartan is itself a combination, it may sometimes be used with other antihypertensives like hydrochlorothiazide or a beta-blocker if blood pressure control remains inadequate. The rationale is to target multiple pathways involved in blood pressure regulation.

Precautions

• General Precautions: Assess for allergies, liver/kidney function, other medical conditions before initiating therapy.
• Specific Populations:
  • Pregnant Women: Avoid use.
  • Breastfeeding Mothers: Not recommended.
  • Children & Elderly: Not recommended in children, cautious use in elderly.
• Lifestyle Considerations: Avoid alcohol, limit potassium intake, avoid operating machinery if experiencing dizziness.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Cilnidipine + Telmisartan?

A: The usual starting dose is one tablet (Cilnidipine 10mg/Telmisartan 40mg) once daily. The dose can be adjusted based on individual blood pressure response, up to a maximum of Cilnidipine 20 mg and Telmisartan 80 mg daily.

Q2: How long does it take for Cilnidipine + Telmisartan to work?

A: Blood pressure reduction begins within a few hours of the first dose, but optimal blood pressure control might take 2-4 weeks to achieve.

Q3: Can Cilnidipine + Telmisartan be taken at night?

A: Yes, it can be taken at any time of day, preferably at the same time each day for consistent blood pressure control.

Q4: What are the most common side effects?

A: The most frequently reported side effects are dizziness, headache, peripheral edema, flushing, and fatigue.

Q5: Is Cilnidipine + Telmisartan safe during pregnancy?

A: No, it is contraindicated during the second and third trimesters of pregnancy and generally not recommended during the first trimester or while breastfeeding.

Q6: What should I do if I miss a dose?

A: Take the missed dose as soon as you remember, unless it’s almost time for the next dose. Do not double the dose to catch up.

Q7: Can Cilnidipine + Telmisartan affect kidney function?

A: Telmisartan can potentially affect kidney function, especially in patients with pre-existing renal impairment. Monitoring kidney function is important during treatment.

Q8: What are the serious side effects to watch out for?

A: Serious side effects, though rare, can include significant hypotension, angioedema, hyperkalemia, and renal impairment. Seek immediate medical attention if these occur.

Q9: Can I drink alcohol while taking this medicine?

A: It’s best to avoid or limit alcohol consumption, as it can exacerbate the blood pressure-lowering effects and increase the risk of side effects like dizziness and lightheadedness.

Q10: What other medications should I avoid while taking Cilnidipine + Telmisartan?

A: Several medications interact with this combination. Inform your doctor about all other medications you are taking, including over-the-counter drugs and supplements, to prevent potential interactions. Common interacting drugs include NSAIDs, certain antidiabetics, and some antidepressants.