LANOPHYLLIN
Clinical safety rating
cautionComprehensive clinical and safety monograph for LANOPHYLLIN (LANOPHYLLIN).
Lanophyllin is a xanthine derivative that inhibits phosphodiesterase, leading to increased intracellular cyclic AMP levels. It also antagonizes adenosine receptors, resulting in bronchodilation, respiratory stimulation, and anti-inflammatory effects.
| Metabolism | Primarily hepatic via CYP1A2, with minor contributions from CYP2E1 and CYP3A4. Metabolites include 3-methylxanthine, 1-methyluric acid, and 1,3-dimethyluric acid. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 10% of elimination; hepatic metabolism accounts for 90%, with metabolites excreted in urine. Biliary/fecal excretion is negligible (<2%). |
| Half-life | Terminal elimination half-life is 7-9 hours in healthy adults; increases to 20-30 hours in congestive heart failure, cirrhosis, or severe COPD; decreases to 3-5 hours in smokers (tobacco or marijuana) due to enzyme induction. |
| Protein binding | Approximately 40% bound to albumin; binding is nonlinear and decreases at higher serum concentrations. |
| Volume of Distribution | 0.4-0.7 L/kg, approximating total body water (0.45 L/kg in adults). Vd is increased in neonates (0.6 L/kg) and decreased in obesity (0.3-0.4 L/kg) due to reduced lean body mass. |
| Bioavailability | Oral immediate-release: 90-100%; Oral sustained-release: 80-100% relative to immediate-release; Rectal solution: 100%; Rectal suppository: 60-80% (erratic). |
| Onset of Action | Oral (immediate-release): 30-60 minutes; Oral (sustained-release): 1-2 hours; Intravenous: 5-10 minutes; Rectal (solution): 30-60 minutes. |
| Duration of Action | Oral (immediate-release): 6-8 hours; Oral (sustained-release): 12-24 hours depending on formulation; Intravenous: 4-6 hours; Rectal (solution): 6-8 hours. Duration is primarily limited by redistribution and metabolism. |
| Molecular Weight | 180.17 |
5-6 mg/kg IV loading dose over 20-30 minutes, then 0.4-0.6 mg/kg/hour continuous IV infusion; maintenance oral dose 300-600 mg/day in divided doses every 8-12 hours.
| Dosage form | ELIXIR |
| Renal impairment | For GFR <30 mL/min: reduce maintenance dose by 50%; consider monitoring serum concentrations. |
| Liver impairment | Child-Pugh Class A: reduce dose by 50%; Child-Pugh Class B: reduce dose by 75%; Child-Pugh Class C: avoid use or use with extreme caution with 80% dose reduction. |
| Pediatric use | IV loading dose: 5-7 mg/kg over 20-30 minutes; maintenance IV infusion: 0.5-1 mg/kg/hour for ages 1-9 years, 0.4-0.7 mg/kg/hour for ages 9-16 years; oral: 10-20 mg/kg/day in divided doses every 6-8 hours, maximum 600 mg/day. |
| Geriatric use | Elderly patients: reduce loading dose to 4-5 mg/kg; maintenance dose 0.2-0.3 mg/kg/hour IV or 200-400 mg/day oral; monitor serum theophylline levels closely due to decreased clearance. |
| 1st trimester | Limited human data; animal studies show fetal harm. Use only if benefit outweighs risk. |
| 2nd trimester | Limited human data; monitor for fetal tachycardia. Use only if clearly needed. |
| 3rd trimester | May cause neonatal irritability, tachycardia, and apnea. Avoid during labor due to potential for neonatal toxicity. |
Clinical note
Comprehensive clinical and safety monograph for LANOPHYLLIN (LANOPHYLLIN).
| Placental transfer | Readily crosses the placenta achieving fetal serum concentrations similar to maternal levels. |
| Breastfeeding | Theophylline is excreted into breast milk in small amounts (about 1% of maternal dose). Monitor infant for irritability or insomnia. Consider alternative if infant has concurrent illness or prematurity. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Insufficient human data; animal studies show no evidence of teratogenicity at clinically relevant doses. First trimester: no known increase in major malformations. Second and third trimesters: no known adverse fetal effects. However, use only if clearly needed. |
| Fetal Monitoring | Monitor maternal serum drug levels (therapeutic range 5-15 mcg/mL), especially in late pregnancy due to reduced clearance. Monitor fetal heart rate and growth if used near term. Assess for maternal signs of toxicity (nausea, vomiting, tachycardia, arrhythmias, seizures). |
| Fertility Effects | No significant effects on human fertility reported. Animal studies show no impairment of fertility at therapeutic doses. |
■ FDA Black Box Warning
None explicitly required by FDA, but use with caution due to narrow therapeutic index and potential for severe toxicity.
| Serious Effects |
Hypersensitivity to theophylline or xanthine derivativesActive peptic ulcer diseaseUncontrolled seizure disorder
| Precautions | Narrow therapeutic index; monitor serum concentrations regularly. Risk of arrhythmias, seizures, and gastrointestinal bleeding. Use lower doses in heart failure, liver disease, and elderly. Avoid abrupt discontinuation due to withdrawal symptoms. |
| Food/Dietary | Avoid grapefruit and grapefruit juice due to CYP3A4 inhibition increasing theophylline levels. Limit caffeine intake (coffee, tea, cola) as it may add to theophylline's stimulant effects. High-fat meals may delay absorption; take consistently with or without food. |
| Clinical Pearls | LANOPHYLLIN is a fixed-dose combination of lansoprazole, a proton pump inhibitor, and theophylline, a methylxanthine bronchodilator. Monitor serum theophylline levels due to lansoprazole's potential to inhibit CYP1A2, increasing theophylline toxicity risk. Avoid in patients with hepatic impairment or acute asthma exacerbation. Taper theophylline to prevent withdrawal seizures. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily in the morning. · Swallow the capsule whole; do not crush or chew. · Avoid drinking alcohol or consuming grapefruit products while on this medication. · Report symptoms like nausea, vomiting, palpitations, or seizures immediately. · Do not stop abruptly; consult your doctor for gradual dose reduction. |
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