Ipratropium + Fenoterol

Thông tin thuốc gốc
Chỉ định và Liều dùng
Asthma, Chronic obstructive pulmonary disease
Adult: Available preparations:
Ipratropium 20 mcg and fenoterol 50 mcg/actuation soln for inhalation
Acute asthma attack: 1 puff for prompt relief. If there is no improvement after 5 min, 1 further dose may be given; further doses may be required if there is no relief after 2 admin. Intermittent and long-term treatment: 1 puff up to 4 times daily. Max: 6 puffs daily.

Ipratropium 0.5 mg and fenoterol 1.25 mg/4 mL soln for nebulisation
4 mL (in NaCl soln) via nebuliser as soon as asthma attack starts. A 2nd dose may be required in severe cases.
Child: As soln for inhalation: >6 yr 1 puff, up to Max 3 puffs daily. As soln for nebulisation:  ≥12 yr Same as adult dose.
Chống chỉ định
Hypersensitivity to ipratropium or fenoterol, atropine, or its derivatives. Hypertrophic obstructive cardiomyopathy, tachyarrhythmia.
Thận trọng
Patient w/ CV disease (e.g. recent MI, arrhythmia, HTN, heart failure, vascular disorders), cystic fibrosis, DM, narrow-angle glaucoma, hyperthyroidism, pheochromocytoma, prostatic hyperplasia/bladder-neck obstruction, seizure disorder. Childn. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Hypokalaemia, AF, cardiac arrhythmia, ischemic heart disease, palpitations, QT prolongation, supraventricular tachycardia, tachycardia.
Nervous: Headache, nervousness, tremor, weakness, dizziness.
CV: HTN, palpitation, hot flushes, hypotension.
GI: Glossitis, xerostomia, nausea, stomatitis, constipation, diarrhoea, vomiting, throat irritation.
Resp: Cough, pharyngitis, hoarseness, throat irritation.
Genitourinary: Urinary retention.
Endocrine: Hyperglycaemia.
Musculoskeletal: Muscle cramps, myalgia.
Ophthalmologic: Visual accommodation disturbance, eye pain, increased intraocular pressure, mydriasis, acute angle-closure glaucoma.
Dermatologic: Diaphoresis.
Potentially Fatal: Paradoxical bronchospasm. Rarely, anaphylaxis (e.g. urticaria, angioedema, rash, bronchospasm).
Thông tin tư vấn bệnh nhân
Rinse mouth every after inhalation. This drug may cause dizziness, tremor and visual disturbances, if affected, do no drive or operate machinery. Avoid contact w/ eyes.
Chỉ số theo dõi
Monitor spirometry [e.g. FEV (forced expiratory volume), FVC (forced vital capacity)] and serum K level.
Quá liều
Symptoms: Tachycardia, palpitation, tremor, hypotension, HTN, angina pain, widening of the pulse pressure, arrhythmia, flushing, dry mouth, visual disturbances. Management: Administer sedatives or tranquilisers. For severe cases, employ intensive therapy. β1-selective blockers may be given as specific antidote.
Tương tác
Enhanced bronchodilatory effect w/ β-adrenergic drugs and xanthine derivatives (e.g. theophylline). Increased risk of adverse effects w/ MAOIs or TCAs. Increased risk of CV effects w/ halogenated hydrocarbons (e.g. halothane). Reduced bronchodilatory effect w/ β-blockers. Increased risk of hypokalaemia w/ xanthine derivatives, corticosteroids, diuretics.
Tác dụng
Description: Ipratropium bromide is a nonselective competitive antimuscarinic agent. It causes bronchodilation by blocking the action of acetylcholine induced stimulation of guanyl cyclase hence reducing formation of cyclic guanosine monophosphate (cGMP) at parasympathetic site.
Fenoterol is a direct-acting β2 sympathomimetic agent. It relaxes bronchial smooth muscles via protein phosphorylation (protein kinase A) by stimulating adenylate cyclase, thereby increasing cyclic-3’- 5’-adenosine monophosphate (cAMP) levels.
Onset: Ipratropium: Bronchodilation: W/in 15 min.
Fenoterol: Bronchodilation: 5 min.
Duration: Ipratropium: 4-8 hr.
Fenoterol: 6-8 hr.
Absorption: Ipratropium: 10-30% of a dose is deposited in the lungs while only a small amount reaches systemic circulation. Bioavailability: 7-28%.
Fenoterol: Incompletely absorbed from the GI tract. Bioavailability: 7%.
Distribution: Deposited in lungs (10-39%).
Ipratropium: Plasma protein binding: <20%.
Fenoterol: Enters breast milk. Plasma protein binding: Approx 40-55%.
Metabolism: Ipratropium: Metabolised in the liver to α-phenylacrylic acid, phenylacetic acid-N-isopropylnortropine ester methobromide, N- isopropylnortropine methobromide.
Fenoterol: Undergoes extensive first-pass metabolism via sulfate conjugation.
Excretion: Ipratropium: Via urine and faeces. Elimination half-life: 1.6 hr.
Fenoterol: Via urine and bile (mainly as inactive sulfate conjugate). Elimination half-life: Approx 3 hr.
Đặc tính

Chemical Structure Image
Ipratropium bromide

Source: National Center for Biotechnology Information. PubChem Database. Ipratropium bromide, CID=657308, https://pubchem.ncbi.nlm.nih.gov/compound/Ipratropium-bromide (accessed on Jan. 21, 2020)

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Fenoterol, CID=3343, https://pubchem.ncbi.nlm.nih.gov/compound/Fenoterol (accessed on Jan. 20, 2020)

Bảo quản
Store between 15-25°C. Protect from light and heat.
Phân loại MIMS
Thuốc trị hen & bệnh phổi tắc nghẽn mạn tính
Phân loại ATC
R03AL01 - fenoterol and ipratropium bromide ; Belongs to the class of combination of adrenergics with anticholinergics, that may also include a corticosteroid. Used in the treatment of obstructive airway diseases.
Tài liệu tham khảo
Anon. Ipratropium and Fenoterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/08/2017.

Buckingham R (ed). Fenoterol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/08/2017.

Buckingham R (ed). Ipratropium Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/08/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Ipratropium Bromide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/08/2017.

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