Dosing and uses of NebuPent, Pentam (pentamidine)
Adult dosage forms and strengths
powder for injection
- 300mg
powder for nebulizer solution
- 300mg
Pneumocystis Jiroveci Pneumonia
Treatment: 4 mg/kg IV/IM qDay for 14-21 days
Prophylaxis: 4 mg/kg IV/IM q2-3Weeks Or
Nebulized 300 mg q4Weeks
African Trypanosomiasis (Off-label)
4 mg/kg IM qDay x10 days
Leishmaniasis (Off-label)
Visceral: 2-4 mg/kg IM q24-48hr x 15-30 doses
Cutaneous: 2 mg/kg IV/IM qODay x7 doses OR 3 mg/kg IM qODay x4 doses
Orphan Designations
Pancreatic cancer
Liver and intrahepatic bile duct cancer
Ovarian cancer
Orphan sponsor
- Oncozyme Pharma, Inc; 555 Rene-Levesque West - 9th Floor; Montreal, Quebec H2Z 1B1, Canada
Renal Impairment
CrCl >10 mL/min: No adjustment necessary
CrCl <10 mL/min: 4 mg/kg IV/IM q24-36hr
Other Information
Monitor: Renal function
Pediatric dosage forms and strengths
powder for injection
- 300mg
powder for nebulizer solution
- 300mg
Pneumocystis Jiroveci Pneumonia
<4 months
- Safety and efficacy not established
>4 months
- Treatment: 4 mg/kg IV/IM qDay for 14-21 days
- Prophylaxis: 4 mg/kg IV/IM q2-3Weeks OR
- Nebulized 300 mg q4Weeks
African Trypanosomiasis (Off-label)
4 mg/kg IM qDay x10 days
Leishmaniasis (Off-label)
Visceral: 2-4 mg/kg IM q24-48hr x 15-30 doses
Cutaneous: 2 mg/kg IV/IM qODay x7 doses OR 3 mg/kg IM qODay x4 doses
Renal Impairment
CrCl >30 mL/min: No adjustment necessary
CrCl 10-30 mL/min: 4 mg/kg IV/IM q36hr
CrC<10 mL/min: 4 mg/kg IV/IM q48hr
Hemodialysis: 4 mg/kg IV/IM q48hr after dialysis on dialysis day
NebuPent, Pentam (pentamidine) adverse (side) effects
>10%
Injection
- Increased SCr (23%)
- IM site reactions (11%)
- Leukopenia (10.3%)
Nebulizer
- Cough (1-63%)
- Wheezing (32%)
- Fever (51%)
- Decreased appetite (50%)
- Bronchospasm (48%)
- Fatigue (66%)
- Infection (15%)
1-10%
Injection
- Anemia
- Confusion/hallucinations
- Hypoglycemia
- Hypotension
- Elevated LFT's
- Fever
- BUN increased
- Azotemia
- Anorexia/Nausea/Vomiting
- Rash
- Thrombocytopenia
Nebulizer
- Bitter/metallic taste
- Headache
- Diarrhea
- Nausea
- Oral Candida
- Anemia
- Pharyngitis
- Night sweats
- Upper respiratory tract infection
<1%
Anxiety
Arthralgia
Blepharitis
Dizziness
Neuralgia
Anemia
Bronchitis
Chest tightness
Colitis
Blurred vision
Neutropenia
Pleuritis
Rales
Thrombocytopenia
Warnings
Contraindications
Hypersensitivity
Cautions
Hypotension, QT prolongation, and Stevens-Johnson syndrome reported with use
Use caution in patients with history of pancreatitis, hyperglycemia, hypoglycemia, hypocalcemia, leukopenia, thrombocytopenia, anemia, hepatic/renal dysfunction
Risk of nephrotoxicity with parenteral administration
Risk of sudden, severe hypotension with parentera administration-keep patient supine
Pregnancy and lactation
Pregnancy category: C
There are no adequate and well controlled studies of aerosolized pentamidine in pregnant women; a literature report indicated that pentamidine 4 mg/kg/day IV administered to pregnant rats was embryolethal; teratogenicity was not observed in this study. It is unknown whether aerosolized pentamidine crosses the placenta at clinically significant concentrations
Lactation: Not known if distributed in breast milk, discontinue drug 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 NebuPent, Pentam (pentamidine)
Mechanism of action
Inhibits synthesis of DNA, RNA, phospholipids, protein by inhibiting oxidative phosphorylation and/or interfering with incorporation of nucleotides and nucleic acids into RNA and DNA
Pharmacokinetics
Half-Life: 5.8 hr (IV); 7-11 hr (IM)
Metabolism: Liver
Vdss: 286-1356 L (IV); 1658-3790 (IM)
Excretion: Urine (12%)
Administration
IV Incompatibilities
Y-site: aldesleukin, cefazolin, cefoperazone, cefotaxime, cefoxitin, ceftazidime, ceftriaxone, fluconazole, foscarnet, linezolid
IV Compatibilities
Solution: D5W, Ns
Y-site: diltiazem, gatifloxacin, zidovudine
IV Preparation
Reconstitute w/ 3-5 mL SWI or D5W (do not use NS)
Reconstituted solutions (60-100 mg/mL) stable for 48 hr at room temp; keep between 22-30°C to prevent crystallization
For IV infusion, dilute in 50-250 mL D5W (stable at room temp for 24 hr)
IV/IM Administration
IM: deep IM using Z-track technique
IV: Slow infusion over 60-120 min
Pts should be in supine position
