TEKTURNA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TEKTURNA (TEKTURNA).

How it works

Direct renin inhibitor that binds to renin, inhibiting the conversion of angiotensinogen to angiotensin I, thereby reducing angiotensin II levels and decreasing vasoconstriction and aldosterone secretion.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; minor metabolism via other pathways. Excreted in feces (78%) and urine (22%).
Excretion	Primarily renal (88% as unchanged drug and metabolites, 33% as unchanged aliskiren); biliary/fecal elimination accounts for approximately 12%.
Half-life	Terminal elimination half-life is approximately 24 hours (range 20–40 hours), supporting once-daily dosing.
Protein binding	Approximately 50% bound to plasma proteins (primarily albumin).
Volume of Distribution	Volume of distribution is approximately 1.7 L/kg, indicating extensive distribution into tissues.
Bioavailability	Oral bioavailability is approximately 2.5% (low due to limited absorption and high first-pass metabolism); absorption is reduced by high-fat meal (by up to 50%).
Onset of Action	Oral: Reduction in blood pressure occurs within 2 hours, with maximal effect observed by 2–4 weeks of continuous therapy.
Duration of Action	Dosing interval is 24 hours; blood pressure reduction is maintained over 24 hours with once-daily administration.

Classification & Brands

Dosing & administration

150 mg orally once daily, starting dose; may increase to 300 mg once daily after 2-4 weeks if blood pressure not controlled, with or without food.

Dosage form	TABLET
Renal impairment	Contraindicated in GFR <30 mL/min/1.73 m². For GFR ≥30 mL/min/1.73 m², no dose adjustment required.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh Class A or B). Not studied in severe hepatic impairment (Child-Pugh Class C).
Pediatric use	Not approved for use in pediatric patients under 18 years of age due to lack of safety and efficacy data.
Geriatric use	No dose adjustment required in elderly patients; initiate therapy at 150 mg once daily and monitor renal function and blood pressure closely due to increased risk of hypotension and renal impairment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TEKTURNA (TEKTURNA).

Breastfeeding	No data on presence in human milk; manufacturer advises against breastfeeding due to potential adverse effects in nursing infants, including hypotension and renal impairment.
Teratogenic Risk	Drugs acting directly on the renin-angiotensin system (RAS) can cause fetal injury and death when used during the second and third trimesters. Risks include oligohydramnios, fetal renal dysfunction, skull ossification defects, and neonatal renal failure. First trimester exposure may also carry increased risk but is less well-defined.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Pregnancy","History of angioedema with previous renin-angiotensin system inhibitors","Concomitant use with aliskiren in patients with diabetes (age- and renal-specific restrictions)"]

Clinical Precautions

Precautions

["Fetal toxicity (avoid in pregnant women; discontinue if pregnancy detected)","Hypotension in volume-depleted patients","Renal impairment (monitor renal function; risk of acute renal failure in patients with bilateral renal artery stenosis)","Hyperkalemia (especially in patients with renal impairment, diabetes, or on potassium-sparing diuretics)","Angioedema (discontinue immediately and manage appropriately)"]

Clinical Tips & Counseling

Drug interactions

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TEKTURNA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TEKTURNA (TEKTURNA).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; minor metabolism via other pathways. Excreted in feces (78%) and urine (22%).
Excretion	Primarily renal (88% as unchanged drug and metabolites, 33% as unchanged aliskiren); biliary/fecal elimination accounts for approximately 12%.
Half-life	Terminal elimination half-life is approximately 24 hours (range 20–40 hours), supporting once-daily dosing.
Protein binding	Approximately 50% bound to plasma proteins (primarily albumin).
Volume of Distribution	Volume of distribution is approximately 1.7 L/kg, indicating extensive distribution into tissues.
Bioavailability	Oral bioavailability is approximately 2.5% (low due to limited absorption and high first-pass metabolism); absorption is reduced by high-fat meal (by up to 50%).
Onset of Action	Oral: Reduction in blood pressure occurs within 2 hours, with maximal effect observed by 2–4 weeks of continuous therapy.
Duration of Action	Dosing interval is 24 hours; blood pressure reduction is maintained over 24 hours with once-daily administration.

Classification & Brands

Dosing & administration

150 mg orally once daily, starting dose; may increase to 300 mg once daily after 2-4 weeks if blood pressure not controlled, with or without food.

Dosage form	TABLET
Renal impairment	Contraindicated in GFR <30 mL/min/1.73 m². For GFR ≥30 mL/min/1.73 m², no dose adjustment required.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh Class A or B). Not studied in severe hepatic impairment (Child-Pugh Class C).
Pediatric use	Not approved for use in pediatric patients under 18 years of age due to lack of safety and efficacy data.
Geriatric use	No dose adjustment required in elderly patients; initiate therapy at 150 mg once daily and monitor renal function and blood pressure closely due to increased risk of hypotension and renal impairment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TEKTURNA (TEKTURNA).

Breastfeeding	No data on presence in human milk; manufacturer advises against breastfeeding due to potential adverse effects in nursing infants, including hypotension and renal impairment.
Teratogenic Risk	Drugs acting directly on the renin-angiotensin system (RAS) can cause fetal injury and death when used during the second and third trimesters. Risks include oligohydramnios, fetal renal dysfunction, skull ossification defects, and neonatal renal failure. First trimester exposure may also carry increased risk but is less well-defined.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Pregnancy","History of angioedema with previous renin-angiotensin system inhibitors","Concomitant use with aliskiren in patients with diabetes (age- and renal-specific restrictions)"]