Amlodipine drug interactions
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Common Drug Interactions with Amlodipine
Amlodipine, a widely used antihypertensive, is frequently involved in drug-drug interactions, especially in patients with multiple comorbidities. Studies show that amlodipine is one of the most commonly interacting antihypertensive drugs, with interactions observed in about 20% of hypertensive patient prescriptions. The most frequent interaction is with atenolol, which can lead to reduced heart rate, decreased cardiac contractility, and hypotension. Other drugs that commonly interact with amlodipine include furosemide, enalapril, and digoxin, while interactions with nifedipine and nebivolol are less common. The severity of these interactions ranges from moderate to major, highlighting the need for careful monitoring when amlodipine is prescribed with other medications .
Amlodipine and Antiretroviral Drugs (ARVs)
Amlodipine is metabolized by the CYP3A4 enzyme, making it susceptible to interactions with drugs that inhibit or induce this enzyme. When coadministered with CYP3A4 inhibitors (such as ritonavir-boosted darunavir), amlodipine exposure can nearly double, increasing the risk of side effects. Conversely, CYP3A4 inducers like efavirenz can reduce amlodipine exposure by more than half, potentially decreasing its effectiveness. Dose adjustments are recommended: halve the dose with CYP3A4 inhibitors and double it with inducers, under close clinical supervision .
Amlodipine and Statins (Simvastatin, Atorvastatin, Rosuvastatin)
Amlodipine can increase the blood levels of simvastatin, raising the risk of statin-related side effects. This interaction is significant enough that clinical guidelines recommend limiting simvastatin doses when used with amlodipine . When amlodipine is combined with atorvastatin or rosuvastatin, studies show no significant change in amlodipine or rosuvastatin exposure, but a slight increase (about 23%) in atorvastatin levels may occur. These combinations are generally well tolerated and considered bioequivalent to individual formulations 310.
Amlodipine and Antihypertensive Combinations (Valsartan, Losartan, Atenolol)
When amlodipine is combined with valsartan, there is a decrease in valsartan exposure, but no significant change in amlodipine levels. The combination is well tolerated and does not require dose adjustment for amlodipine or rosuvastatin . With losartan, amlodipine does not significantly affect losartan’s active metabolite, but it does decrease losartan exposure and increase its clearance. The combination produces additive blood pressure-lowering effects and is generally safe . Quantitative modeling also confirms an infra-additive interaction in blood pressure reduction when amlodipine and valsartan are used together .
Amlodipine and Tadalafil
Coadministration of amlodipine and tadalafil (used for erectile dysfunction) leads to a significant increase in tadalafil levels, but amlodipine exposure remains unchanged. The combination is well tolerated, with no significant increase in adverse events compared to monotherapy .
Amlodipine and Curcumin
Curcumin, often used for hyperlipidemia, can significantly increase amlodipine blood levels by inhibiting its metabolism via CYP3A4. This interaction may require dose adjustments and careful monitoring if both are used together .
Amlodipine and Risk of Angioedema
Amlodipine has been associated with angioedema, both alone and in combination with certain renin–angiotensin–aldosterone system inhibitors (RAAS-i), such as specific ACE inhibitors and ARBs. The risk is particularly notable with the combination of amlodipine and trandolapril. Most cases resolve after discontinuing the drug, but monitoring is advised, especially when starting therapy .
Conclusion
Amlodipine is involved in several clinically relevant drug interactions, especially with drugs affecting CYP3A4 metabolism, other antihypertensives, statins, and certain herbal supplements like curcumin. These interactions can alter drug levels, efficacy, and safety, making it essential for clinicians to monitor patients closely and adjust doses as needed. Awareness of these interactions helps ensure safe and effective use of amlodipine in diverse patient populations 12345678+2 MORE.
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