PULMOLITE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PULMOLITE (PULMOLITE).
PULMOLITE is a leukotriene receptor antagonist (LTRA) that selectively and competitively inhibits the cysteinyl leukotriene (CysLT1) receptor in the human airway, thereby reducing bronchoconstriction, mucus secretion, and eosinophilic infiltration.
| Metabolism | Primarily metabolized by cytochrome P450 (CYP) enzymes, specifically CYP2C9 and CYP3A4, to inactive metabolites excreted in bile and urine. |
| Excretion | Primarily renal (80%) as unchanged drug; 15% fecal via biliary excretion; 5% metabolized. |
| Half-life | Terminal elimination half-life: 12 hours (range 10–14 h) in adults with normal renal function (CrCl >90 mL/min); prolonged to 24–30 h in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8 L/kg (range 0.6–1.0 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral: 70% (range 65–75%); IV: 100%. |
| Onset of Action | IV: 2–5 minutes; Oral: 30–60 minutes on empty stomach. |
| Duration of Action | IV: 6–8 hours; Oral: 8–12 hours. Sustained-release formulation extends to 24 hours. |
Adults: 200 mg intravenously every 12 hours over 30 minutes.
| Dosage form | INJECTABLE |
| Renal impairment | GFR >=60 mL/min: no adjustment. GFR 30-59 mL/min: reduce dose to 100 mg every 12 hours. GFR 15-29 mL/min: 100 mg every 24 hours. GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50% (100 mg every 12 hours). Child-Pugh C: contraindicated. |
| Pediatric use | Children 1 month to 12 years: 5 mg/kg intravenously every 12 hours, max 200 mg per dose. Children >12 years: same as adult dosing. |
| Geriatric use | No specific dose adjustment based on age alone; use with caution and monitor renal function; adjust dose per renal function as per renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PULMOLITE (PULMOLITE).
| Breastfeeding | Pulmolite is excreted in human breast milk with an estimated M/P ratio of 2.5. Due to potential serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for 2 weeks after the last dose. |
| Teratogenic Risk | Pulmolite is contraindicated in pregnancy due to demonstrated teratogenicity in animal studies. First trimester exposure is associated with neural tube defects and cardiovascular malformations. Second and third trimester exposure may cause fetal growth restriction and oligohydramnios. |
■ FDA Black Box Warning
No FDA boxed warning exists for PULMOLITE.
| Serious Effects |
Hypersensitivity to PULMOLITE or any component of the formulation. Safety not established for acute asthma exacerbations. Use with caution in patients with severe hepatic impairment.
| Precautions | Neuropsychiatric events (e.g., agitation, aggression, depression, suicidal behavior) have been reported; discontinue if such symptoms occur. Eosinophilia, vasculitis (Churg-Strauss syndrome) may present as systemic eosinophilia. Do not use for acute asthma attacks. Rare cases of hepatic eosinophilic infiltration. Monitor for hypersensitivity reactions. |
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| Fetal Monitoring |
| Monitor maternal blood pressure, renal function, and hepatic enzymes every 4 weeks. Perform fetal ultrasound at 18-20 weeks and 28 weeks to assess growth and anatomy. Monitor amniotic fluid volume monthly after 24 weeks. |
| Fertility Effects | Pulmolite may impair female fertility by disrupting ovarian function and reducing oocyte quality. In males, it may cause reversible oligospermia and reduced sperm motility. Fertility effects may persist for up to 6 months after discontinuation. |