Comparative Pharmacology
Head-to-head clinical analysis: LOTREL versus TEKAMLO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LOTREL versus TEKAMLO.
LOTREL vs TEKAMLO
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lotrel is a combination of amlodipine (a calcium channel blocker) and benazepril (an ACE inhibitor). Amlodipine inhibits calcium ion influx across cardiac and vascular smooth muscle cells, causing vasodilation and reduced blood pressure. Benazepril inhibits angiotensin-converting enzyme, reducing angiotensin II formation, leading to vasodilation and decreased aldosterone secretion.
Combination of aliskiren (direct renin inhibitor) and amlodipine (dihydropyridine calcium channel blocker). Aliskiren inhibits renin, reducing angiotensin I and II formation; amlodipine inhibits calcium ion influx across cardiac and vascular smooth muscle, causing vasodilation.
Oral: 1 capsule (amlodipine 2.5 mg/benazepril 10 mg) once daily, titrate to maximum 10 mg/40 mg once daily.
One tablet (40 mg telmisartan/5 mg amlodipine) orally once daily; maximum dose: 80 mg telmisartan/10 mg amlodipine per day.
None Documented
None Documented
Amlodipine: 30-50 hours (terminal); steady state in 7-10 days. Benazeprilat: 10-11 hours (terminal); effective half-life 22-24 hours with once-daily dosing.
Amlodipine terminal half-life: 30-50 hours (mean 35 hours), allowing once-daily dosing; steady-state achieved after 7-8 days. Valsartan terminal half-life: ~6 hours, but pharmacodynamic effect persists due to tight AT1 receptor binding.
Amlodipine: 60% renal, 20-25% fecal. Benazeprilat: 85% renal (as benazeprilat and conjugated metabolites), 15% biliary/fecal.
TEKAMLO (amlodipine/valsartan) excretion: amlodipine is extensively metabolized in the liver with 60% of metabolites excreted renally and 20-25% via feces; unchanged drug in urine <10%. Valsartan is primarily excreted unchanged in feces (70-80%) via biliary elimination, and 13% in urine as unchanged drug.
Category C
Category C
Antihypertensive combination
Antihypertensive combination