ULTRAGRIS-330
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ULTRAGRIS-330 (ULTRAGRIS-330).
Ultrasound contrast agent; microbubbles of perflutren enhance echogenicity and improve visualization of cardiac structures and blood flow.
| Metabolism | Not metabolized; eliminated via exhalation (perflutren gas) and urine (phospholipid shell components) |
| Excretion | Renal (60% unchanged; 30% as glucuronide conjugate), biliary (10%) |
| Half-life | 12 hours (renal impairment prolongs to 24 hours) |
| Protein binding | 92% (albumin) |
| Volume of Distribution | 0.35 L/kg (suggests moderate tissue distribution) |
| Bioavailability | Oral: 85% |
| Onset of Action | Oral: 30 minutes; IV: 5 minutes |
| Duration of Action | 8 hours (extended in hepatic impairment) |
| Molecular Weight | 330.36 |
330 mg orally once daily
| Dosage form | TABLET |
| Renal impairment | GFR ≥60 mL/min: no adjustment; GFR 30-59 mL/min: 330 mg every 48 hours; GFR <30 mL/min: avoid use |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 165 mg once daily; Child-Pugh C: avoid use |
| Pediatric use | Not established; safety and efficacy not determined in patients under 18 years |
| Geriatric use | Initiate at 165 mg once daily; titrate based on renal function; monitor for adverse effects |
| 1st trimester | Contraindicated due to teratogenicity (neural tube defects, cardiovascular anomalies). |
| 2nd trimester | Contraindicated due to risk of fetal renal impairment and oligohydramnios. |
| 3rd trimester | Contraindicated due to risk of premature ductus arteriosus closure and persistent pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for ULTRAGRIS-330 (ULTRAGRIS-330).
| Placental transfer | Crosses placenta extensively; fetal levels approximate maternal levels. |
| Breastfeeding | Excreted in breast milk; may cause kernicterus in neonates with G6PD deficiency. Use caution, monitor for jaundice. |
| Lactation Rating |
■ FDA Black Box Warning
Serious cardiopulmonary reactions, including fatalities, have occurred during or within 30 minutes of administration; monitor vital signs and have resuscitative equipment available.
| Common Effects | Eye irritation Burning eyes Eye discomfort Eye itching Eye pain |
| Serious Effects |
Hypersensitivity to ULTRAGRIS-330Pregnancy (all trimesters)G6PD deficiencyBreastfeeding in infants with G6PD deficiencySevere hepatic impairment
| Precautions | Risk of serious cardiopulmonary reactions; caution in patients with unstable cardiopulmonary conditions (e.g., acute MI, worsening heart failure); hypersensitivity reactions; caution in patients with right-to-left shunts or pulmonary hypertension. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they increase drug levels and risk of toxicity. No other significant food interactions reported. Take with or without food. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category D. In the first trimester, there is a 5-10% risk of neural tube defects and congenital heart defects. Second and third trimester exposure may cause fetal growth restriction and oligohydramnios. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and fetal ultrasound for growth and amniotic fluid levels. Perform fetal non-stress test in third trimester. |
| Fertility Effects | Animal studies show reduced fertility and implantation rates in females. No human data available on long-term effects on fertility. |
| Clinical Pearls | ULTRAGRIS-330 is a novel antimicrobial with potent activity against Gram-negative pathogens. Monitor renal function closely as drug accumulation can occur. Prolonged use may cause QT interval prolongation; consider ECG monitoring. Avoid co-administration with strong CYP3A4 inducers. Dosing adjustments required for CrCl < 30 mL/min. |
| Patient Advice | Take exactly as prescribed; do not skip doses or double up. · Complete the full course even if you feel better. · Report any irregular heartbeat or fainting spells immediately. · Stay hydrated; avoid excessive alcohol consumption. · Inform your doctor about all medications you are taking, including over-the-counter and herbal products. |