TEKAMLO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEKAMLO (TEKAMLO).
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.
| Metabolism | Aliskiren: minimal metabolism via CYP3A4; amlodipine: extensively metabolized by CYP3A4 |
| Excretion | 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. |
| Half-life | 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. |
| Protein binding | Amlodipine: ~97.5% bound to plasma proteins (albumin). Valsartan: 94-97% bound to serum proteins (mainly albumin). |
| Volume of Distribution | Amlodipine Vd: ~21 L/kg, indicating extensive extravascular distribution. Valsartan Vd: ~5-10 L/kg, indicating moderate distribution into tissues. |
| Bioavailability | Amlodipine: oral bioavailability 64-90% (mean ~64%). Valsartan: oral bioavailability ~23% (range 10-35%). Both are administered orally only. |
| Onset of Action | Amlodipine: gradual onset, with initial antihypertensive effect within 2-6 hours; maximal effect at 6-12 hours. Valsartan: onset within 2 hours; peak effect at 4-6 hours after oral administration. |
| Duration of Action | Amlodipine: duration >24 hours due to long half-life, effective for once-daily dosing. Valsartan: duration 24 hours despite shorter half-life, due to sustained receptor blockade. |
One tablet (40 mg telmisartan/5 mg amlodipine) orally once daily; maximum dose: 80 mg telmisartan/10 mg amlodipine per day.
| Dosage form | TABLET |
| Renal impairment | No adjustment for GFR ≥30 mL/min. Contraindicated if GFR <30 mL/min due to telmisartan component. Amlodipine not dialyzable. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Use lowest available strength, titrate slowly; avoid if severe impairment. |
| Pediatric use | Safety and efficacy not established in patients <18 years. |
| Geriatric use | Start at lowest available strength (40/5 mg); titrate slowly due to increased risk of hypotension and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEKAMLO (TEKAMLO).
| Breastfeeding | No human data; amlodipine excreted in breast milk (M/P ratio ~1.0), telmisartan unknown. Avoid use while breastfeeding due to potential for neonatal hypotension and renal effects. |
| Teratogenic Risk | First trimester: Fetal toxicities (oligohydramnios, renal dysfunction, skull ossification delay) with angiotensin II receptor blocker (ARB) class. Second/third trimester: Oligohydramnios, fetal renal failure, hypotension, hyperkalemia, skull hypoplasia; risk is highest in second and third trimesters. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Concomitant use with aliskiren in patients with diabetes or renal impairment (eGFR <60 mL/min) due to increased risk of renal impairment, hypotension, and hyperkalemia","Pregnancy","History of angioedema with aliskiren"]
| Precautions | ["Risk of hypotension/syncope in volume-depleted patients","Avoid use in pregnancy (potential fetal harm)","Monitor renal function and electrolytes, especially in patients with renal artery stenosis","Peripheral edema (more common in women, dose-dependent)"] |
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| Monitor maternal blood pressure, serum creatinine, potassium, and urine output. Fetal ultrasound to assess amniotic fluid volume and renal function; serial growth scans. |
| Fertility Effects | No specific human data; animal studies show no impairment of fertility with amlodipine or telmisartan at therapeutic doses. |