Usage
- Efonidipine + Telmisartan is prescribed for the management of Stage II hypertension (high blood pressure). It may also help reduce the risks associated with hypertension, such as heart attack, stroke, and angina (chest pain).
- Pharmacological Classification: This combination drug includes two classes: a calcium channel blocker (Efonidipine) and an angiotensin II receptor blocker (ARB) (Telmisartan).
- Mechanism of Action: Efonidipine works by relaxing the blood vessels, which lessens the heart’s workload. Telmisartan blocks the action of angiotensin II, a hormone that constricts blood vessels. The combined effect lowers blood pressure.
Alternate Names
- While no direct alternate names exist for the combination itself, the individual components are sometimes known by other names.
- Brand Names: The combination is marketed under various brand names like Efnocar-T and Efonta-T.
How It Works
- Pharmacodynamics: Efonidipine, a dihydropyridine calcium channel blocker, inhibits calcium influx into vascular smooth muscle cells, causing vasodilation. Telmisartan, an ARB, blocks the binding of angiotensin II to its receptors, preventing vasoconstriction. This dual action results in a synergistic lowering of blood pressure.
- Pharmacokinetics: Both drugs are orally administered. Efonidipine is well-absorbed, metabolized by the liver (CYP3A4 enzyme), and primarily excreted in the feces. Telmisartan also has good oral absorption, undergoes minimal metabolism, and is mainly excreted unchanged in the bile.
- Mode of Action: Efonidipine acts on L-type calcium channels, while Telmisartan specifically targets angiotensin II type 1 receptors (AT1 receptors). The combination doesn’t involve enzyme inhibition or neurotransmitter modulation as its primary mechanisms.
- Elimination Pathways: Efonidipine is primarily eliminated through hepatic metabolism and fecal excretion, while Telmisartan is eliminated mainly through biliary excretion.
Dosage
Standard Dosage
Adults:
- The usual starting dose is one tablet daily containing 20 mg of Efonidipine and 40 mg of Telmisartan. This may be increased to a maximum of two tablets daily based on blood pressure response. Individual component doses can go up to 80 mg/day.
Children:
- This combination is not recommended for children as safety and efficacy have not been established.
Special Cases:
- Elderly Patients: Start with a low dose (20 mg Efonidipine/40 mg Telmisartan) and monitor closely for hypotension. Dosage adjustments should be made cautiously.
- Patients with Renal Impairment: Caution is advised, especially in those with severe renal impairment or on hemodialysis. A lower starting dose might be considered.
- Patients with Hepatic Dysfunction: Caution is advised, particularly with moderate to severe hepatic impairment. Patients should be closely monitored, and dose titration should be gradual.
- Patients with Comorbid Conditions: Consider individual patient factors like congestive heart failure and other cardiovascular diseases when adjusting the dose.
Clinical Use Cases
- The provided sources don’t list dosage recommendations for specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. The drug is intended for chronic hypertension management.
Dosage Adjustments
- Dosage adjustments may be necessary based on patient factors like renal/hepatic function, other medical conditions, and response to therapy. Close monitoring of blood pressure is essential during dose adjustments.
Side Effects
Common Side Effects:
- Headache, dizziness, flushing, fatigue, swelling of ankles/feet/hands.
Rare but Serious Side Effects:
- Severe hypotension, allergic reactions, liver dysfunction.
Long-Term Effects:
- The provided sources do not detail specific long-term side effects.
Adverse Drug Reactions (ADR):
- Angioedema, severe hypotension, and other allergic reactions require immediate medical attention.
Contraindications
- Hypersensitivity to efonidipine or telmisartan, pregnancy, severe hepatic impairment, concomitant use of ACE inhibitors.
Drug Interactions
- Other antihypertensive agents, cimetidine, grapefruit juice, tacrolimus, digoxin, quinidine, phenytoin, rifampicin, erythromycin, potassium-sparing diuretics, potassium supplements, lithium, alcohol, and smoking. CYP450 interactions are primarily mediated by CYP3A4 for Efonidipine.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Contraindicated during pregnancy, especially the second and third trimesters.
- Fetal Risks: May cause fetal harm, including fetotoxicity.
- Drug excretion in breast milk: Unknown for the combination, but Telmisartan has been detected in rat milk. Efonidipine should be avoided during breastfeeding.
- Safer Alternatives: Other antihypertensive agents with established safety profiles during pregnancy and lactation should be considered.
Drug Profile Summary
- Mechanism of Action: Calcium channel blockade and angiotensin II receptor blockade leading to vasodilation and lowered blood pressure.
- Side Effects: Headache, dizziness, flushing, fatigue, edema. Rarely: hypotension, angioedema, liver dysfunction.
- Contraindications: Hypersensitivity, pregnancy, severe hepatic impairment, concomitant ACE inhibitor use.
- Drug Interactions: Numerous drug interactions exist (see Drug Interactions section).
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: starting dose 20 mg Efonidipine/40 mg Telmisartan once daily, titratable up to two tablets per day based on blood pressure control. Not for pediatric use.
- Monitoring Parameters: Blood pressure, renal function, hepatic function, signs of angioedema.
Popular Combinations
- While information specifically on Efonidipine + Telmisartan combinations is limited, the combination itself represents a popular strategy to manage hypertension using two different mechanisms.
Precautions
- Screen for allergies, liver/kidney dysfunction, and heart problems.
- Pregnant Women: Avoid use.
- Breastfeeding Mothers: Avoid use.
- Children & Elderly: Not recommended for children; caution in elderly patients.
- Lifestyle Considerations: Limit alcohol, avoid smoking, and be cautious about activities requiring alertness, like driving.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Efonidipine + Telmisartan?
A: The usual starting dose for adults is 20 mg Efonidipine/40 mg Telmisartan once daily, which may be increased to two tablets per day depending upon the blood pressure control or as directed by the physician. It is not recommended for pediatric use.
Q2: What are the major side effects of Efonidipine + Telmisartan?
A: Common side effects include headache, dizziness, flushing, fatigue, and swelling in the ankles, feet, or hands.
Q3: Can Efonidipine + Telmisartan be used during pregnancy?
A: No, it’s contraindicated during pregnancy due to potential harm to the fetus.
Q4: How does Efonidipine + Telmisartan work to lower blood pressure?
A: Efonidipine relaxes blood vessels by blocking calcium channels, while Telmisartan blocks the action of angiotensin II, a hormone that narrows blood vessels. This combined action lowers blood pressure.
Q5: Are there any drug interactions I should be aware of with Efonidipine + Telmisartan?
A: Yes, numerous drug interactions are possible. It’s crucial to inform your doctor about all medications you are taking, including OTC drugs and supplements. Some key interactions include those with other antihypertensives, cimetidine, grapefruit juice, tacrolimus, and digoxin.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. However, if it’s almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not double the dose.
Q7: What precautions should be taken in elderly patients using this combination?
A: Start with a low dose and monitor closely for hypotension. Dose adjustments should be made cautiously.
Q8: Are there any dietary restrictions while taking Efonidipine + Telmisartan?
A: While no strict dietary restrictions apply, limiting alcohol intake is generally recommended. Grapefruit juice can interact with Efonidipine and should be avoided. A balanced diet, low in sodium, is also beneficial for managing hypertension.
Q9: Can I take Efonidipine + Telmisartan if I have liver or kidney problems?
A: Caution should be exercised in patients with hepatic or renal impairment. Dosage adjustments may be necessary. Consult your doctor before starting this medication if you have any liver or kidney problems.
