pentamidine (Rx)

>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

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 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.

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%)

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