THEOCLEAR L.A.-130
Clinical safety rating: caution
Comprehensive clinical and safety monograph for THEOCLEAR L.A.-130 (THEOCLEAR L.A.-130).
Theophylline is a methylxanthine that inhibits phosphodiesterase, increasing intracellular cAMP, and blocks adenosine receptors, leading to bronchodilation and anti-inflammatory effects.
| Metabolism | Primarily hepatic via CYP1A2, CYP2E1, and CYP3A4 (major); also N-demethylation and oxidation. Exhibits non-linear pharmacokinetics. |
| Excretion | Approximately 90% of theophylline is eliminated hepatically via CYP1A2 and CYP3A4 metabolism; renal excretion of unchanged drug accounts for about 10% in adults, but may increase to 50% in neonates. Biliary/fecal elimination is negligible. |
| Half-life | Terminal elimination half-life is 3-8 hours in healthy adults (mean 5-6 hours). It is prolonged in patients with hepatic cirrhosis, heart failure, or COPD (up to 30 hours) and in neonates (20-30 hours). Smoking induces metabolism, reducing half-life to 1-4 hours. |
| Protein binding | Approximately 40% bound to plasma proteins, primarily albumin. Binding is reversible and independent of concentration within therapeutic range. |
| Volume of Distribution | Vd of 0.3-0.7 L/kg (average 0.5 L/kg) approximates total body water. This indicates extensive distribution into tissues, with higher concentrations in tissues than plasma. |
| Bioavailability | Oral bioavailability of the sustained-release formulation approaches 100% due to complete absorption. However, food can affect absorption rate; with Theoclear L.A.-130, high-fat meals may increase peak concentration and rate of absorption. |
| Onset of Action | For oral sustained-release (Theoclear L.A.-130): onset of bronchodilation occurs within 1-2 hours; peak effect at 4-6 hours after a single dose. |
| Duration of Action | Duration of bronchodilator effect from a single sustained-release dose is typically 8-12 hours due to the slow-release formulation. Therapeutic serum levels (5-15 mcg/mL) are maintained for the dosing interval. |
130 mg orally every 12 hours; extended-release tablet.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | No specific adjustment required; monitor serum concentrations and adjust dose based on clinical response and trough levels. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: reduce dose by 75% and monitor levels closely. |
| Pediatric use | Not recommended for children under 6 years; for children 6-12 years: 130 mg once daily initially, titrate based on weight and serum levels (target 5-15 mcg/mL). |
| Geriatric use | Initiate at lower end of dosing range (130 mg once daily) and titrate slowly; monitor for toxicity due to reduced clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for THEOCLEAR L.A.-130 (THEOCLEAR L.A.-130).
| Breastfeeding | Theophylline is excreted into breast milk with a milk-to-plasma (M/P) ratio of approximately 0.6-0.7. Infant exposure is about 1-10% of maternal weight-adjusted dose. Adverse effects in nursing infants (irritability, sleep disturbance) have been reported. Caution advised; monitor infant for toxicity. |
| Teratogenic Risk | Theophylline (THEOCLEAR L.A.-130) is not associated with major teratogenic effects in humans. First trimester exposure does not increase risk of congenital malformations above baseline. Third trimester use may cause neonatal irritability, tachycardia, and vomiting due to transplacental transfer. Risk of fetal respiratory depression is low at therapeutic maternal levels. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to theophylline or any component","Pre-existing cardiac arrhythmias (e.g., tachyarrhythmias)","Uncontrolled seizure disorder","Active peptic ulcer disease"]
| Precautions | ["Risk of seizures and arrhythmias at high serum levels (therapeutic range 10-20 mcg/mL)","Monitor serum theophylline levels regularly","Use caution in patients with peptic ulcer disease, hyperthyroidism, or seizure disorders","May exacerbate arrhythmias; ECG monitoring recommended","Drug interactions with CYP1A2 inhibitors (e.g., cimetidine, fluoroquinolones) and inducers (e.g., smoking, rifampin)"] |
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| Fetal Monitoring | Monitor maternal serum theophylline levels (target 5-15 mcg/mL), heart rate, respiratory status, and signs of toxicity (nausea, vomiting, palpitations). Fetal monitoring: assess fetal heart rate and movements; consider non-stress test in third trimester if signs of fetal distress or maternal toxicity. |
| Fertility Effects | No conclusive evidence of adverse effects on human fertility. Animal studies show no impairment of fertility at therapeutic doses. Theophylline may affect sperm motility in vitro, but clinical significance is unknown. |