Doxofylline


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Bronchial asthma, Chronic obstructive pulmonary disease
Adult: Recommended dose: 400 mg bid-tid. Max: 1,200 mg daily.
Elderly: Reduce dose to 200 mg bid-tid.
Child: As syr: <12 years 6-9 mg/kg bid; ≥12 years 200 mg bid-tid. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Nhóm bệnh nhân đặc biệt
Patient with CHF or concomitant infection: Dose reduction may be required.

Smokers: Dose adjustment may be necessary.
Suy thận
Dose reduction may be required.
Suy gan
Dose reduction may be required.
Chống chỉ định
Acute MI, hypotension. Lactation.
Thận trọng
Patient with CV disease (e.g. cardiac arrhythmias, angina pectoris, chronic right ventricular failure, CHF, hypertension), COPD; active or history of peptic ulcer and/or GERD; hyperthyroidism, hypoxaemia, concomitant infection, inflammation, history of seizure disorder. Smokers (including after cessation of smoking). Hepatic and renal impairment. Children and elderly. Pregnancy.
Tác dụng không mong muốn
Cardiac disorders: Tachycardia, extrasystoles, palpitations.
Gastrointestinal disorders: Nausea, vomiting, epigastric pain.
Metabolism and nutrition disorders: Hyperglycaemia.
Nervous system disorders: Headache. Rarely, seizures.
Psychiatric disorders: Irritability, insomnia.
Renal and urinary disorders: Albuminuria.
Respiratory, thoracic and mediastinal disorders: Tachypnoea.
Chỉ số theo dõi
Monitor heart rate, respiratory rate, and CNS effects (e.g. irritability, insomnia).
Quá liều
Symptoms: Nausea, vomiting, gastrointestinal bleeding, hypotension, seizures, and severe arrhythmia. Management: Symptomatic and supportive treatment. May induce emesis or perform gastric lavage, followed by administration of activated charcoal or cathartic. In case of seizures, establish adequate airway and give IV diazepam and/or phenobarbital.
Tương tác
Increased half-life and decreased clearance with cimetidine, allopurinol, erythromycin, ciprofloxacin, troleandomycin, lincomycin, clindamycin, ranitidine, propranolol, and flu vaccines. Decreased half-life and increased clearance with phenytoin and other anticonvulsants. Increased risk of synergistic toxicity with ephedrine and other sympathomimetics. May potentiate hypokalaemia caused by hypoxia with β2-agonists, corticosteroids, and diuretics.
Tương tác với thức ăn
Caffeine-containing products may enhance the adverse effect of doxofylline; avoid concomitant use.
Tác dụng
Description:
Mechanism of Action: Doxofylline, a theophylline derivative, is a bronchodilator. It inhibits phosphodiesterase enzymes which increase cyclic adenine monophosphate (cAMP), thereby causing bronchial smooth muscle relaxation leading to bronchodilation.
Pharmacokinetics:
Absorption: Rapidly absorbed. Absolute bioavailability: 62.6%. Time to peak plasma concentration: 1.19 hours.
Distribution: Volume of distribution: 1 L/kg. Plasma protein binding: Approx 48%.
Metabolism: Extensively metabolised in the liver (approx 90%) into the inactive metabolite, hydroxyethyltheophylline.
Excretion: Via urine (<4% as unchanged drug). Elimination half-life: 7-10 hours.
Đặc tính

Chemical Structure Image
Doxofylline

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 50942, Doxofylline. https://pubchem.ncbi.nlm.nih.gov/compound/Doxofylline. Accessed Apr. 26, 2022.

Bảo quản
Store below 30°C. Protect from light.
Phân loại MIMS
Thuốc trị hen & bệnh phổi tắc nghẽn mạn tính
Phân loại ATC
R03DA11 - doxofylline ; Belongs to the class of xanthines. Used in the systemic treatment of obstructive airway diseases.
Tài liệu tham khảo
Cazzola M and Mactera MG. The Effect of Doxofylline in Asthma and COPD. Respiratory Medicine. 2020 Feb;164. https://doi.org/10.1016/j.rmed.2020.105904. Accessed 05/04/2022

Goldstein MF and Chervinsky P. Efficacy and Safety of Doxofylline Compared to Theophylline in Chronic Reversible Asthma - A Double-Blind Randomized Placebo-Controlled Multicentre Clinical Trial. Med Sci Monit. 2002;8(4):CR297-304. Accessed 05/04/2022. PMID: 11951074

Anon. Doxofylline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/04/2022.

Buckingham R (ed). Doxofylline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/04/2022.

Doxofix 400 mg Tablet (Amherst Laboratories, Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 05/04/2022.

Doxofree 400 mg Tablet (Lloyd Laboratories, Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 05/04/2022.

Fildox 400 mg Extended-release Tablet (Zydus Healthcare Philippines Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 05/04/2022.

Maxivent 200 mg Tablet, 400 mg Tablet, 100 mg/5 mL Syrup (Ajanta Pharma Limited). MIMS Philippines. http://www.mims.com/philippines. Accessed 05/04/2022.

Puroxan (Eurodrug). MIMS Thailand. http://www.mims.com/thailand. Accessed 05/04/2022.

Puroxan Tablet (Eurodrug Laboratories [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 25/04/2022.

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