TEKTURNA HCT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEKTURNA HCT (TEKTURNA HCT).
Aliskiren is a direct renin inhibitor that decreases plasma renin activity and inhibits the conversion of angiotensinogen to angiotensin I. Hydrochlorothiazide is a thiazide diuretic that inhibits the sodium-chloride cotransporter in the distal convoluted tubule, reducing sodium and water reabsorption.
| Metabolism | Aliskiren is primarily metabolized by CYP3A4; Hydrochlorothiazide is not metabolized and excreted unchanged in urine. |
| Excretion | Aliskiren: 78-91% unchanged in feces via biliary excretion, <2.4% in urine. Hydrochlorothiazide: ≥95% renal, 50-75% unchanged. |
| Half-life | Aliskiren: terminal half-life 24-31 hours (accumulation supports once-daily dosing). Hydrochlorothiazide: 6-15 hours (correlates with duration of action). |
| Protein binding | Aliskiren: 47-51% (albumin). Hydrochlorothiazide: 40-68% (albumin). |
| Volume of Distribution | Aliskiren: 0.65-2.3 L/kg (extensive tissue distribution due to lipophilicity). Hydrochlorothiazide: 3-7 L/kg (distributes into erythrocytes). |
| Bioavailability | Aliskiren: 2-5% oral (1.6-2.8% at 300 mg). Hydrochlorothiazide: 65-70% oral. |
| Onset of Action | Aliskiren: 2 hours (oral). Hydrochlorothiazide: 2 hours (oral). |
| Duration of Action | Aliskiren: >24 hours (additional effect at 2 weeks). Hydrochlorothiazide: 6-12 hours (antihypertensive effect up to 24 hours). |
Oral: 1 tablet (aliskiren 150 mg / hydrochlorothiazide 12.5 mg) once daily. If blood pressure not controlled, may increase to 1 tablet (aliskiren 300 mg / hydrochlorothiazide 12.5 mg) or 1 tablet (aliskiren 300 mg / hydrochlorothiazide 25 mg) once daily.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with GFR <30 mL/min/1.73m2. For GFR 30-59 mL/min/1.73m2: no dose adjustment required, but monitor serum potassium and creatinine. Discontinue if progressive oliguria or acute renal failure occurs. |
| Liver impairment | Child-Pugh Class A or B: no dose adjustment. Child-Pugh Class C: use with caution; no specific dose guidelines. |
| Pediatric use | Safety and efficacy not established in pediatric patients less than 18 years of age. |
| Geriatric use | Elderly patients may be more sensitive to hypotension and electrolyte imbalances. Start at the lowest dose (150/12.5 mg) and titrate cautiously. Monitor renal function and electrolytes regularly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEKTURNA HCT (TEKTURNA HCT).
| Breastfeeding | Aliskiren: Not known if excreted in human milk. Hydrochlorothiazide: Excreted in breast milk in small amounts; M/P ratio not reported. Use with caution, monitor infant for dehydration, electrolyte imbalance. Consider alternatives if possible. |
| Teratogenic Risk | First trimester: Drugs acting directly on the renin-angiotensin system (aliskiren, the aliskiren component) can cause fetal renal dysfunction, oligohydramnios, and skull ossification defects. Second and third trimesters: Exposure is associated with fetal hypotension, anuria, renal failure, oligohydramnios, skull hypoplasia, and death. Hydrochlorothiazide: Crosses the placenta; risk of electrolyte disturbances, jaundice, and thrombocytopenia in the newborn. Generally avoid in pregnancy, especially second and third trimesters. |
■ FDA Black Box Warning
None
| Serious Effects |
["Pregnancy (risk of fetal harm)","Anuria (due to hydrochlorothiazide component)","Concomitant use with ACE inhibitors or ARBs in patients with diabetes mellitus or moderate-to-severe renal impairment (CrCl < 60 mL/min)","Hypersensitivity to any component (including sulfonamide-derived drugs for hydrochlorothiazide)"]
| Precautions | ["Avoid use in pregnancy (especially 2nd and 3rd trimesters) due to fetal toxicity; discontinue immediately if pregnancy occurs.","Not recommended with ACE inhibitors or ARBs in patients with diabetes or renal impairment (CrCl < 60 mL/min) due to increased risk of renal dysfunction, hyperkalemia, and hypotension.","Symptomatic hypotension may occur, especially in volume-depleted patients; correct volume depletion before use.","Electrolyte imbalances: monitor serum potassium (risk of hyperkalemia), sodium, and magnesium; hydrochlorothiazide may cause hypokalemia, hyponatremia, and hypomagnesemia.","Renal impairment: monitor renal function; may cause acute renal failure; contraindicated with CrCl < 30 mL/min for hydrochlorothiazide component.","Angioedema may occur; discontinue if develops."] |
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| Fetal Monitoring | Monitor maternal blood pressure, renal function, serum electrolytes, and urine output. Perform fetal ultrasound to assess amniotic fluid volume, renal anatomy, and skull development, especially after first trimester exposure. Monitor newborn for hypotension, oliguria, hyperkalemia, and electrolyte disturbances. |
| Fertility Effects | Limited data. No specific adverse effects on fertility reported for aliskiren or hydrochlorothiazide. However, uncontrolled hypertension may affect fertility; control with alternative antihypertensives if pregnancy is planned. |