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tretoquinol

R03CC09

Forms & Strengths

Oral tablets 100 mg
Oral tablets 200 mg
Injectable solution 5 mg/mL
Sustained‑release tablets 150 mg

Adult Dosing

Oral: 100‑200 mg 2‑3 times daily, titrated to serum level 10‑20 µg/mL
Injectable: 0.5 mg/kg IV loading dose over 30 min, then 0.25 mg/kg q6h
Adjust dose for hepatic impairment or smoking status
Maximum daily dose 900 mg
Therapeutic drug monitoring recommended after 5 days

Pediatric Dosing

Oral: 5‑7 mg/kg/day divided q8h; max 250 mg/day
Injectable: 0.25 mg/kg IV q6h if needed
Dose reduced 25% in neonates <1 month
Monitor serum levels; target 8‑15 µg/mL
Avoid in children <2 years with viral bronchiolitis

Indications

Chronic asthma refractory to inhaled β2‑agonists
COPD with frequent exacerbations
Exercise‑induced bronchospasm when inhaled therapy insufficient
Adjunct to anti‑inflammatory therapy in severe persistent asthma

Mechanism of Action

Non‑selective phosphodiesterase inhibitor → ↑cAMP in airway smooth muscle
Adenosine receptor antagonism → reduces bronchoconstrictive reflexes
Mild anti‑inflammatory effects via inhibition of leukotriene release

Contraindications

Known hypersensitivity to xanthines
Active cardiac arrhythmia or uncontrolled tachycardia
Severe hepatic impairment (Child‑Pugh C)
Concurrent use of MAO inhibitors

Adverse Reactions

Nausea, vomiting, abdominal discomfort
Headache, insomnia, anxiety
Palpitations, tachyarrhythmias
Elevated transaminases, hepatotoxicity
Seizures at high serum concentrations

Drug Interactions

CYP1A2 inhibitors (cimetidine, fluvoxamine) ↑ serum tretoquinol
CYP1A2 inducers (rifampin, smoking) ↓ serum levels
Concurrent theophylline‑type agents → additive toxicity
β‑blockers may blunt bronchodilatory effect
Macrolide antibiotics (erythromycin) ↑ levels

Curated Content: Needs Vetting Before Put to Clinical Use