GIAPREZA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GIAPREZA (GIAPREZA).
A synthetic form of human angiotensin II, a vasoconstrictor that increases blood pressure by binding to angiotensin II type 1 receptors (AT1) on vascular smooth muscle, causing vasoconstriction.
| Metabolism | Metabolized by aminopeptidase A and angiotensin-converting enzyme (ACE) to smaller fragments, including angiotensin (1-8). |
| Excretion | Primarily via proteolysis; renal excretion of unchanged drug is negligible (<1%). Fecal excretion is minimal. |
| Half-life | Terminal elimination half-life is approximately 1 hour (range 0.5–2 hours); clinical context: requires continuous intravenous infusion for sustained vasopressor effect. |
| Protein binding | ~70% bound to plasma proteins, primarily to albumin. |
| Volume of Distribution | Approximately 0.5 L/kg; indicates distribution primarily within extracellular fluid and plasma volume. |
| Bioavailability | Intravenous: 100% (only route of administration; oral bioavailability is negligible due to peptide degradation). |
| Onset of Action | Intravenous: Onset of blood pressure increase occurs within 5 minutes of infusion initiation. |
| Duration of Action | Duration of action is short; blood pressure returns to baseline within 15–30 minutes after discontinuation of infusion. Clinical note: continuous infusion is necessary for sustained effect. |
1 mg/kg/min IV continuous infusion, titrated to achieve target mean arterial pressure; maximum dose 10 mg/kg/min.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy not established; no FDA-approved pediatric dosing. |
| Geriatric use | No specific adjustment recommended; use with caution due to potential cardiovascular comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GIAPREZA (GIAPREZA).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or effects on milk production. Consider developmental and health benefits of breastfeeding along with mother's clinical need for angiotensin II and any potential adverse effects on breastfed infant from drug or underlying maternal condition. M/P ratio not available. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal reproduction studies, no adverse developmental outcomes were observed at doses up to 2.1 times the maximum recommended human dose based on AUC. Risk cannot be ruled out; use only if potential benefit justifies potential risk to fetus. First trimester: limited data; second and third trimesters: theoretical risk of fetal hypotension and hypoperfusion due to maternal hypotension. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["No absolute contraindications identified.","Relative contraindications: patients with known hypersensitivity to any component; patients with a history of severe hypertension; patients with a known high risk of arterial or venous thrombosis."]
| Precautions | ["Thromboembolic events (venous and arterial) have been reported; monitor for signs of thrombosis.","Risk of adverse reactions from coadministration with ACE inhibitors (increased response) or angiotensin receptor blockers (increased response).","Concomitant use with vasopressors may require dose adjustment.","Not recommended for patients with high output states (e.g., cardiogenic shock) unless as a rescue therapy."] |
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| Fetal Monitoring | Monitor maternal blood pressure continuously during infusion, fetal heart rate monitoring if gestational age permits, and maternal volume status and electrolytes due to potential for hypokalemia, hyperglycemia, or lactic acidosis. |
| Fertility Effects | No human data on fertility. In animal studies, no effects on male or female fertility at doses up to 2.1 times MRHD based on AUC. |