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pentoxifylline (Trental, Pentoxil, Pentoxifylline SR)

 

Classes: Hemorheologic Agents

Dosing and uses of Trental, Pentoxil (pentoxifylline)

 

Adult dosage forms and strengths

tablet, extended release

  • 400mg

 

Intermittent Claudication

400 mg PO q8hr

Recommended duration of treatment: ≥8 weeks

 

Dosage modifications

Digestive or CNS side effects: Decrease dose to 400 mg BID; discontinue if adverse effects persist

Renal impairment (CrCl <30 mL/min): Decrease dose to 400 mg/day

Hepatic impairment: No information

 

Administration

Take with meals

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Trental, Pentoxil (pentoxifylline) adverse (side) effects

1-10%

Nausea

Vomiting

 

<1%

Angina

Anaphylaxis

Anorexia

Aplastic anemia

Pancytopenia

Conjunctivitis

Angioedema

Aseptic meningitis

Chest pain

Leukemia

Leukopenia

Cholecystitis

Hepatitis

Seizure

Scotoma

Thrombocytopenia

Increased live enzyme

 

Warnings

Contraindications

Hypersensitivity to pentoxifylline or xanthine derivatives

Recent retinal or cerebral hemorrhage

 

Cautions

Use caution with risk factors for hemorrhage

Discontinue at first sign of anaphylaxis

Use with caution in renal impairment; exposure to pentoxifylline and/or active metabolites may increase; significance unknown

Use with caution in the elderly due to potential for renal impairment

Use with caution in hepatic impairment; exposure to pentoxifylline and/or active metabolites may increase; significance unknown

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Drug excreted in breast milk; discontinue therapy, or do not nurse

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Trental, Pentoxil (pentoxifylline)

Mechanism of action

Improves blood flow by decreasing blood viscosity and increasing red blood cell (RBC) flexibility

May increase tissues oxygenation through enhanced blood flow

 

Absorption

Bioavailability: 10-30%

 

Distribution

RBC binding: Parent drug, 45%; 5-hydroxyhexyl metabolite, 40%

 

Metabolism

Extensively metabolized in liver (first pass); also metabolized in erythrocytes

Metabolites: 5-hydroxyhexyl, 3-carboxypropyL

 

Elimination

Half-life: 24-48 min (Parent drug); 60-96 min (metabolites)

Excretion: Urine (50-80%, principally as metabolites), feces (<4%)