ULTRAGRIS-165
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ULTRAGRIS-165 (ULTRAGRIS-165).
ULTRAGRIS-165 is a combination of the antifungal agent griseofulvin and a synthetic corticosteroid, which inhibits fungal cell mitosis by binding to tubulin and disrupting microtubule function, while the corticosteroid reduces inflammation via glucocorticoid receptor activation.
| Metabolism | Griseofulvin is metabolized in the liver primarily by CYP3A4; the corticosteroid component is metabolized via hepatic enzymes including CYP3A4. |
| Excretion | Primarily renal (70-80% unchanged), with 15-20% biliary/fecal. Total clearance 120 mL/min. |
| Half-life | Terminal elimination half-life of 8–10 hours in healthy adults; prolonged to 15–20 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 95–98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8–1.2 L/kg, indicating distribution into total body water with some tissue binding. |
| Bioavailability | Oral: 85–95% (first-pass metabolism minimal). |
| Onset of Action | Oral: 30–60 min; IV: 5–10 min. |
| Duration of Action | Oral: 6–8 hours; IV: 4–6 hours. Extended by hepatic impairment. |
160 mg orally every 6 hours or 300 mg orally every 12 hours; total daily dose not to exceed 1500 mg.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: 160 mg every 12 hours or 300 mg every 24 hours; GFR 15-29 mL/min: 160 mg every 24 hours; GFR <15 mL/min: 160 mg every 48 hours or 160 mg every 24 hours with close monitoring. |
| Liver impairment | Child-Pugh A: No adjustment; Child-Pugh B: 160 mg every 8 hours; Child-Pugh C: 160 mg every 12 hours or consider alternative therapy. |
| Pediatric use | Weight-based: 5 mg/kg/dose orally every 6 hours; maximum single dose 160 mg; maximum daily dose 1000 mg. |
| Geriatric use | No specific dose adjustment recommended; monitor renal function and consider starting at lower end of dosing range due to age-related renal decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ULTRAGRIS-165 (ULTRAGRIS-165).
| Breastfeeding | ULTRAGRIS-165 is excreted into human breast milk. Milk-to-plasma ratio is 0.8. Potential for serious adverse reactions in nursing infants; therefore, breastfeeding is not recommended during treatment and for 2 weeks after last dose. |
| Teratogenic Risk | ULTRAGRIS-165 is contraindicated in pregnancy due to documented teratogenicity in first trimester (neural tube defects, cardiovascular malformations) based on human data. Second and third trimester use associated with low birth weight and preterm delivery. Use only if benefit outweighs risk and no alternative available. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to griseofulvin or corticosteroids","Severe hepatic impairment","Pregnancy (Category X due to teratogenic effects)"]
| Precautions | ["Hepatotoxicity risk; monitor liver function","Bone marrow suppression with prolonged use","Photosensitivity reactions","May impair immune response"] |
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| Fetal Monitoring | Monitor maternal blood pressure, liver function tests, and renal function monthly. Fetal ultrasound for growth and anatomy in first trimester if exposed; serial growth scans in second and third trimester. Monitor for fetal distress with non-stress testing after 32 weeks. |
| Fertility Effects | ULTRAGRIS-165 may impair female fertility by causing anovulation and menstrual irregularities. In males, reversible oligospermia and decreased sperm motility have been reported. Fertility effects are generally reversible upon discontinuation. |