Dosing & Uses
Dosage Forms & 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
Dosage Forms & 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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse 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 & 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
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
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
