GIAPREZA
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 872.9 |
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 | No human data; animal studies not conducted; vasoconstrictive properties may reduce placental perfusion, potentially causing fetal harm. Use only if benefit outweighs risk. |
| 2nd trimester | No human data; theoretical risk of reduced uteroplacental blood flow; consider alternative agents for hypertensive emergencies. |
| 3rd trimester | Same as T2; may cause fetal distress due to maternal hypotension and reduced placental perfusion. |
Clinical note
Comprehensive clinical and safety monograph for GIAPREZA (GIAPREZA).
| Placental transfer | Unknown; peptide molecule with molecular weight >500 Da likely limited placental transfer, but no human data. |
| Breastfeeding | No data on presence in human milk; due to short half-life and intravenous administration, systemic exposure to infant likely negligible; caution if infant has cardiovascular instability. |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to angiotensin II or any excipient
| 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. |
| Food/Dietary | No known food interactions. GIAPREZA is administered intravenously and does not interact with food. |
| Clinical Pearls | GIAPREZA (angiotensin II) is indicated for the treatment of refractory hypotension in adults with distributive shock who have failed adequate volume resuscitation and other vasopressors. Do not administer with angiotensin-converting enzyme (ACE) inhibitors due to risk of excessive hypotension. Monitor blood pressure continuously during administration. Prepare using strict aseptic technique; discard unused portion. Dosage is based on the patient's baseline mean arterial pressure (MAP) and response. Use with caution in patients with severe hypertension or conditions that may be exacerbated by vasoconstriction. |
| Patient Advice | This medication is used to increase your blood pressure if it is dangerously low and not responding to other treatments. · Your blood pressure will be monitored continuously during the infusion. · Inform your healthcare provider if you have a history of high blood pressure, heart disease, or any allergies. · Do not stop or change the dose without consulting your doctor. · Report any symptoms such as chest pain, shortness of breath, or headache immediately. |
Loading safety data…