GLOFIL-125
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GLOFIL-125 (GLOFIL-125).
GLOFIL-125 (pentoxifylline) is a xanthine derivative that improves erythrocyte flexibility by inhibiting phosphodiesterase, leading to increased intracellular cAMP. It also reduces blood viscosity and platelet aggregation, improving microcirculation.
| Metabolism | Hepatic via erythrocyte and hepatic cytosol enzymes (not cytochrome P450); metabolites include metabolites I (5-hydroxyhexyl) and V (carboxypropyl), which are excreted renally. |
| Excretion | Renal excretion of unchanged drug >90%; biliary/fecal <5%. |
| Half-life | Terminal elimination half-life: 2.5–3.5 hours (prolonged in renal impairment; up to 20–30 hours in severe chronic kidney disease). |
| Protein binding | ~35%, primarily to albumin. |
| Volume of Distribution | 0.3–0.5 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 85–95%. |
| Onset of Action | Oral: 30–60 minutes; Intravenous: immediate. |
| Duration of Action | Oral: 6–8 hours; Intravenous: 4–6 hours (depends on renal function). |
125 mg orally twice daily.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-60 mL/min: 125 mg once daily. GFR <30 mL/min: 125 mg every 48 hours. |
| Liver impairment | Child-Pugh A: 125 mg twice daily. Child-Pugh B: 125 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | 2.5-5 mg/kg orally twice daily; maximum 125 mg per dose. |
| Geriatric use | Initiate at 125 mg once daily and titrate cautiously based on renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GLOFIL-125 (GLOFIL-125).
| Breastfeeding | Excretion into human milk is unknown. M/P ratio not established. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for 5 half-lives after last dose. |
| Teratogenic Risk | GLOFIL-125 is classified as Pregnancy Category D. First trimester: Associated with increased risk of cardiovascular and neural tube defects based on animal studies. Second and third trimesters: Risk of fetal renal impairment, oligohydramnios, and premature closure of ductus arteriosus. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to pentoxifylline or other xanthines (e.g., caffeine, theophylline)","Cerebral hemorrhage or retinal hemorrhage","Concurrent use with strong inhibitors of phosphodiesterase (e.g., dipyridamole) due to increased bleeding risk","Severe coronary artery disease or recent myocardial infarction"]
| Precautions | ["May increase the risk of bleeding, especially in patients with risk factors or on anticoagulants/antiplatelets.","Use with caution in patients with renal impairment (creatinine clearance <30 mL/min).","Monitor liver function in patients with hepatic impairment."] |
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| Fetal Monitoring |
| Monitor maternal renal function (serum creatinine, BUN) and electrolytes monthly. Assess amniotic fluid volume via ultrasound every 4 weeks. Fetal echocardiography at 18-22 weeks. Monitor for signs of premature labor. |
| Fertility Effects | In animal studies, GLOFIL-125 caused reduced spermatogenesis and ovarian follicular depletion at therapeutic doses, potentially impairing fertility in both sexes. Reversibility upon discontinuation is uncertain. |