Drug reference directory
Drug reference

doxofylline

Methylxanthine bronchodilator (dioxolane analog) · Bronchodilator

START
400 mg PO 2–3 times daily after food
TYPICAL MAX
1200 mg/day
STOP IF
Significant arrhythmia, seizure, or severe hypotension
WATCH
ECG/HR, K, GI symptoms; xanthine-class CNS effects
CDSCO approvedATC R03DA11
Dose laddermg/d
400per dose800BID total1.2kmax/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLStandard dosing30REDUCEReduce dose; monitor≥90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
45minONSET1hPEAK6.5ht½12hDURATION
ONSET
45min · absorption
PEAK
1h · Tmax
t½
6.5h · t½
DURATION
12h · BID-TID
EXCRETION
Renal — metabolites; ~4% unchanged
route + CYP
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
Limited data; use only if clearly needed.
FDA category + note
Top interactionssee all 5 →
  • Other XanthinesSevereDatabaseKimi deep-research + Cla

Mechanism

Methylxanthine that inhibits phosphodiesterase III/IV (less adenosine antagonism than theophylline), producing bronchodilation; lower CNS / cardiac toxicity than theophylline.

Indications

Chronic obstructive pulmonary diseaseAsthma (maintenance, regions where licensed)

Dosing

Adult
400 mg PO 2–3 times daily after food.
Pediatric
≥12 y: as adult.
Renal adjustment
Caution in severe impairment; no fixed adjustment.
Hepatic adjustment
Reduce dose in significant impairment.
Geriatric
Reduce dose; tachyarrhythmia risk.
Max dose
1200 mg/day

Pharmacokinetics

Onset
Bronchodilation 30–60 min
Peak effect
~1 h (Tmax)
Duration
~12 h
Half-life
~6–7 h
Bioavailability
Well absorbed orally
Protein binding
~48%
Metabolism
Hepatic
Excretion
Renal (metabolites; ~4% unchanged)

Contraindications

  • Acute myocardial infarction
  • Severe arrhythmia
  • Severe hypotension
  • Hypersensitivity to xanthines
  • Caution: peptic ulcer, seizure disorders

Side effects

Common
Nausea/vomitingHeadachePalpitationsInsomniaTremor
Serious
  • Tachyarrhythmia
  • Seizures (overdose)
  • Severe hypotension
  • GI bleeding (rare)

Pregnancy & lactation

Pregnancy

Limited data; use only if clearly needed.

Lactation

Limited data; caution.

Drug interactions

Other Xanthines
Severe
Database

Additive cardiac/CNS toxicity

Avoid combination

Source: Kimi deep-research + Cla

Ciprofloxacin
Moderate
Database

Increased xanthine levels

Monitor; reduce dose

Source: Kimi deep-research + Cla

Beta Blockers
Moderate
Database

Antagonism of bronchodilation

Use cardioselective β-blocker if needed

Source: Kimi deep-research + Cla

Lithium
Moderate
Database

Increased lithium clearance

Monitor lithium levels

Source: Kimi deep-research + Cla

Smoking
Moderate
Database

Induces xanthine metabolism

Dose adjustments after stopping smoking

Source: Kimi deep-research + Cla

7 additional unreviewed or low-confidence interactions hidden because their provenance or source detail is insufficient.

Related guidelines

Ask House about doxofylline

Continue into a citation-backed clinical answer with the drug context already attached.

Textbook-sourced·Sources: Goodman & Gilman 14e·Updated: 2026-05-20·Cockpit curated: 2026-05-20