ANGIOTENSIN ll ACETATE
Clinical safety rating
cautionComprehensive clinical and safety monograph for ANGIOTENSIN ll ACETATE (ANGIOTENSIN ll ACETATE).
Angiotensin II acetate is a synthetic peptide that acts as a potent vasoconstrictor by binding to the angiotensin II type 1 (AT1) receptor on vascular smooth muscle cells, leading to increased intracellular calcium and smooth muscle contraction. It also stimulates aldosterone secretion from the adrenal cortex, promoting sodium and water retention.
| Metabolism | Primarily metabolized by aminopeptidases and other peptidases in plasma and tissues, with minimal hepatic involvement. |
| Excretion | Primarily renal (90-100%) as unchanged drug; minimal biliary/fecal elimination (<10%). |
| Half-life | Terminal elimination half-life is approximately 30-60 minutes; clinical effect is short-lived requiring continuous intravenous infusion. |
| Protein binding | Approximately 30% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.3-0.5 L/kg; indicates distribution mainly in extracellular fluid. |
| Bioavailability | Intravenous: 100%; subcutaneous/intramuscular: not well absorbed due to rapid local metabolism; oral: negligible (<1%) due to extensive first-pass metabolism. |
| Onset of Action | Intravenous: 1-2 minutes; subcutaneous/intramuscular: 5-15 minutes. |
| Duration of Action | Intravenous: 2-4 minutes; subcutaneous: 10-20 minutes; duration is dose-dependent and limited by rapid metabolism and clearance. |
| Molecular Weight | 491.6 |
Intravenous infusion: 1-40 ng/kg/min titrated to achieve target blood pressure. Initial rate: 10 ng/kg/min.
| Dosage form | SOLUTION |
| Renal impairment | No specific dose adjustment required for renal impairment. Use caution in patients with renal artery stenosis. |
| Liver impairment | No specific dose adjustment required for hepatic impairment. |
| Pediatric use | Intravenous infusion: 0.5-20 ng/kg/min titrated to effect. Safety and efficacy not established in neonates. |
| Geriatric use | Start at lower end of dosing range (1-5 ng/kg/min) due to potential for decreased renal function and increased sensitivity. |
| 1st trimester | Contraindicated: risk of oligohydramnios, fetal renal dysfunction, and skull ossification defects in 1st trimester. |
| 2nd trimester | Contraindicated: associated with oligohydramnios, fetal anuria, and renal tubular dysplasia in 2nd trimester. |
| 3rd trimester | Contraindicated: may cause neonatal oliguria, hypotension, and pulmonary hypoplasia in 3rd trimester. |
Clinical note
Comprehensive clinical and safety monograph for ANGIOTENSIN ll ACETATE (ANGIOTENSIN ll ACETATE).
| Placental transfer | Crosses placenta in animal studies; in humans, detected in fetal plasma at 10-70% of maternal levels. |
| Breastfeeding | Minimal excretion into breast milk is expected due to high protein binding and low oral bioavailability; however, use with caution in preterm infants or those with compromised renal function. |
| Lactation Rating | L3 - Moderately Safe |
| Teratogenic Risk | First trimester: Potential for teratogenicity (increased risk of cardiovascular and CNS malformations). Second and third trimesters: Fetal hypotension, anuria, oligohydramnios, skull hypoplasia, pulmonary hypoplasia, and death. Use contraindicated in pregnancy. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, electrolytes. Fetal ultrasound for oligohydramnios, renal function, and skull ossification. Doppler studies for placental blood flow. |
| Fertility Effects | No specific studies. Theoretical risk of altered renin-angiotensin system affecting ovulation or implantation. Use with caution in women attempting conception. |
■ FDA Black Box Warning
No boxed warnings.
| Serious Effects |
Hypersensitivity to angiotensin II or any componentBilateral renal artery stenosisSole functioning kidney with renal artery stenosisHypovolemiaSevere hypotensionConcomitant use with aliskiren in patients with diabetes mellitus
| Precautions | Thrombotic and thromboembolic events: Increased risk of venous and arterial thromboembolic events, including deep vein thrombosis, pulmonary embolism, and myocardial infarction., Ischemic events: May cause cardiac ischemia and reduce cardiac output; use with caution in patients with coronary artery disease., Vascular thrombosis: High risk of vascular thrombosis in patients with a history of thrombosis or hypercoagulable states., Use in hypovolemia: Correct hypovolemia before administration to avoid exacerbation of vasoconstriction., Pregnancy: May cause fetal harm; avoid use in pregnant women unless potential benefit outweighs risk. |
| Food/Dietary | No food interactions specific to angiotensin II acetate. Maintain a balanced diet as tolerated. Avoid excessive salt intake unless directed otherwise, as it may counteract the medication's effect on blood pressure. |
| Clinical Pearls | ANGIOTENSIN II ACETATE is a vasoconstrictor used for refractory hypotension in distributive shock. Administer via central line to avoid extravasation, which can cause severe tissue ischemia. Monitor blood pressure every 5 minutes during titration. Discontinue other vasopressors if possible to avoid additive arrhythmogenic effects. Use with caution in patients with coronary artery disease or previous myocardial infarction due to increased oxygen demand. Taper gradually to avoid rebound hypotension. |
| Patient Advice | This medication is given intravenously in the hospital to raise very low blood pressure. You will be closely monitored during treatment. · Inform your healthcare provider immediately if you experience chest pain, difficulty breathing, or irregular heartbeat. · Avoid sudden position changes to prevent dizziness, as blood pressure may fluctuate. · Report any pain, swelling, or color changes at the injection site, which could indicate medication leakage. · You may need regular blood tests to monitor kidney function and electrolyte levels. |
Loading safety data…