Usage
- Azelnidipine + Telmisartan is prescribed for the management of hypertension (high blood pressure), especially stage 2 hypertension, in patients whose blood pressure is not adequately controlled by monotherapy or who have multiple risk factors or comorbidities.
- Pharmacological Classification: Antihypertensive (a combination of a calcium channel blocker and an angiotensin II receptor blocker).
- Mechanism of Action: Azelnidipine blocks calcium channels in blood vessels, causing vasodilation. Telmisartan blocks angiotensin II receptors, preventing vasoconstriction. The combined effect lowers blood pressure.
Alternate Names
- No widely recognized alternate generic names exist.
- Brand Names: Telma AZ (Glenmark Pharmaceuticals). Other brand names may exist.
How It Works
- Pharmacodynamics: Azelnidipine and Telmisartan both lower blood pressure through different but complementary mechanisms, leading to a synergistic effect. Azelnidipine, a dihydropyridine calcium channel blocker, primarily acts on vascular smooth muscle, causing vasodilation. Telmisartan, an angiotensin II receptor blocker (ARB), inhibits the binding of angiotensin II to its receptor, preventing vasoconstriction. This dual mechanism reduces peripheral vascular resistance and lowers blood pressure without significant reflex tachycardia.
- Pharmacokinetics: Azelnidipine is rapidly and almost completely absorbed after oral administration. It undergoes extensive first-pass metabolism in the liver by CYP3A4 enzymes. Telmisartan also has good oral absorption, but limited bioavailability due to extensive first-pass metabolism, primarily by CYP2C9. Both drugs are highly protein-bound. Azelnidipine is excreted primarily via the biliary route, while Telmisartan is mainly eliminated unchanged in the feces, with a small portion excreted in the urine.
- Mode of Action: Azelnidipine inhibits L-type calcium channels in vascular smooth muscle, reducing calcium influx and causing vasodilation. Telmisartan selectively blocks the AT1 subtype of angiotensin II receptors, preventing angiotensin II-mediated vasoconstriction and aldosterone release.
- Receptor Binding/Enzyme Inhibition: Azelnidipine binds to and inhibits L-type calcium channels. Telmisartan binds to and blocks AT1 angiotensin II receptors. Azelnidipine is metabolized by CYP3A4, and telmisartan primarily by CYP2C9.
- Elimination Pathways: Azelnidipine is primarily excreted in the bile and feces. Telmisartan is predominantly eliminated unchanged in the feces, with a small portion excreted in urine.
Dosage
Standard Dosage
Adults:
- The starting dose is typically Azelnidipine 8 mg + Telmisartan 40 mg once daily. The dose can be titrated up to a maximum of Azelnidipine 16 mg + Telmisartan 80 mg once daily, based on the patient’s blood pressure response and tolerability.
Children:
- Not recommended for use in children due to a lack of safety and efficacy data.
Special Cases:
- Elderly Patients: Initiate therapy with the lower end of the dosing range. Monitor closely for hypotension.
- Patients with Renal Impairment: Start with a lower dose (Azelnidipine 8mg + Telmisartan 40 mg) and monitor renal function regularly.
- Patients with Hepatic Dysfunction: Use with caution and reduce the dosage as needed. Start with a lower dose (Azelnidipine 8mg + Telmisartan 40 mg) and titrate cautiously.
- Patients with Comorbid Conditions: Close monitoring is advised for patients with diabetes, heart failure, or other cardiovascular diseases. Dosage adjustments may be required.
Clinical Use Cases
- Specific dosing guidelines for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations are not available for this combination drug. Individualized management based on blood pressure control and hemodynamic stability is recommended.
Dosage Adjustments
- Dose adjustments may be needed for patients with renal or hepatic impairment.
- Consider interactions with other medications and lifestyle factors.
Side Effects
Common Side Effects:
- Dizziness, headache, peripheral edema (swelling in the ankles, feet, or hands), fatigue, back pain, nasopharyngitis.
Rare but Serious Side Effects:
- Angioedema (swelling of the face, lips, tongue, or throat), severe hypotension, kidney dysfunction, liver injury, allergic reactions.
Long-Term Effects:
- Chronic hypotension and related complications if not properly managed.
Adverse Drug Reactions (ADR):
- Angioedema, severe hypotension, acute renal failure, hepatic injury, severe allergic reactions.
Contraindications
- Hypersensitivity to Azelnidipine or Telmisartan.
- Severe hepatic impairment or biliary obstruction.
- Pregnancy (especially second and third trimesters).
- Concomitant use with aliskiren in patients with diabetes or renal impairment.
Drug Interactions
- Other antihypertensives (additive hypotensive effect).
- Potassium-sparing diuretics (risk of hyperkalemia).
- NSAIDs (may reduce antihypertensive effect).
- Lithium (increased lithium levels).
- CYP3A4 inhibitors or inducers (may affect Azelnidipine metabolism).
- CYP2C9 inhibitors or inducers (may affect Telmisartan metabolism).
- Grapefruit juice (may increase Azelnidipine levels).
- Alcohol (may potentiate hypotensive effect).
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Contraindicated in pregnancy, especially in the second and third trimesters, due to the risk of fetal harm.
- Breastfeeding: Not recommended during breastfeeding. If use is essential, consider an alternative safer option or monitor the infant for potential adverse effects.
Drug Profile Summary
- Mechanism of Action: Azelnidipine blocks calcium channels, while Telmisartan blocks angiotensin II receptors, both leading to vasodilation and lowered blood pressure.
- Side Effects: Dizziness, headache, peripheral edema, fatigue. Rarely, angioedema, hypotension, kidney/liver injury.
- Contraindications: Hypersensitivity, severe hepatic impairment, pregnancy, concomitant use with aliskiren in specific populations.
- Drug Interactions: Other antihypertensives, potassium-sparing diuretics, NSAIDs, lithium, CYP3A4/CYP2C9 inhibitors/inducers, grapefruit juice, alcohol.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy. Not recommended while breastfeeding.
- Dosage: Adults: Starting dose 8/40 mg once daily, titratable up to 16/80 mg. Not for children. Adjust for renal/hepatic impairment.
- Monitoring Parameters: Blood pressure, renal function (creatinine, potassium), liver function tests.
Popular Combinations
- Azelnidipine + Telmisartan is itself a popular combination. Additional combinations with a thiazide diuretic (like hydrochlorothiazide) or a beta-blocker may be used for further blood pressure control if needed.
Precautions
- General Precautions: Assess renal and hepatic function, monitor blood pressure, evaluate for heart failure.
- Specific Populations: Pregnant women (contraindicated), breastfeeding mothers (not recommended), children (not recommended), elderly patients (start with lower dose).
- Lifestyle Considerations: Reduce sodium intake, regular exercise, manage stress, avoid smoking and excessive alcohol consumption.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Azelnidipine + Telmisartan?
A: The starting dose is Azelnidipine 8 mg + Telmisartan 40 mg once daily, titratable up to 16/80 mg based on response and tolerability.
Q2: How does this combination work to lower blood pressure?
A: Azelnidipine blocks calcium channels and Telmisartan blocks angiotensin II receptors, both resulting in vasodilation.
Q3: What are the common side effects?
A: Dizziness, headache, peripheral edema, and fatigue are common.
Q4: Are there any serious side effects?
A: Yes, rarely angioedema, severe hypotension, kidney/liver injury can occur.
Q5: Can this medication be used during pregnancy or breastfeeding?
A: It’s contraindicated in pregnancy, and not recommended while breastfeeding.
Q6: What are the major drug interactions?
A: Other antihypertensives, NSAIDs, lithium, and potassium-sparing diuretics are some important interactions.
Q7: What precautions should be taken with this drug?
A: Monitor blood pressure, renal function, and liver function. Adjust the dose for renal or hepatic impairment.
Q8: How should I counsel my patients on lifestyle modifications?
A: Advise patients to reduce sodium intake, exercise regularly, manage stress, quit smoking, and limit alcohol consumption.
Q9: What should patients do if they miss a dose?
A: Take the missed dose as soon as remembered, unless it is close to the next scheduled dose. Do not double the dose.
