Ephedrine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Reversal of spinal or epidural anaesthesia-induced hypotension
Adult: As ephedrine hydrochloride: 3-6 mg (max: 9 mg) via slow IV inj every 3-4 minutes. Max: 30 mg. As ephedrine sulfate: 5-10 mg via IV bolus inj as needed. Max: 50 mg.
Child: >12 years As ephedrine hydrochloride: Same as adult dose.

Nasal
Nasal congestion
Adult: As 0.5% or 1% drops: Instil 1-2 drops into each nostril as needed up to 4 times daily. Max: 7 days. As 0.5% spray: 2-3 sprays into each nostril up to 4 hourly. Max: 3 days.
Child: >12 years As 0.5% or 1% drops: Same as adult dose. 6-<12 years As 0.5% spray: 1-2 sprays up to 4 hourly. Max: 3 days. ≥12 years Same as adult dose.

Oral
Bronchospasm
Adult: 15-60 mg tid.
Elderly: Initial: 50% of adult dose.
Child: 1-5 years 15 mg tid. 6-12 years 30 mg tid.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
Dilute 50 mg/mL vial with 9 mL dextrose 5% solution or 0.9% NaCl to make 5 mg/mL.
Chống chỉ định
CV disease, cardiomyopathy, peripheral vascular resistance, arrhythmias, hyperthyroidism, hyperexcitability, phaeochromocytoma, closed-angle glaucoma, urinary retention, following nasal or sinus surgery (nasal). Ischaemic heart disease, prostatic hyperplasia (oral). Hypertension (nasal/oral). Concomitant use with other sympathomimetics and α-sympathomimetic agents (IV/nasal); β-blockers (nasal). Children <12 years old (nasal).
Thận trọng
Patient with diabetes mellitus. Ischaemic heart disease, arrhythmia, tachycardia, hypertension, angina pectoris (IV). Asthma (oral/nasal). Hyperthyroidism, closed-angle glaucoma (IV/oral). Prostatic hyperplasia (IV/nasal). Renal impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Rebound nasal congestion, mucosal ulceration, epistaxis, discomfort including dryness, stinging, burning (nasal). Hypertension (IV).
Cardiac disorders: Palpitations, cardiac arrhythmias, tachycardia (IV/oral).
Eye disorders: Mydriasis (nasal); closed-angle glaucoma (IV).
Gastrointestinal disorders: Nausea, vomiting; dry mouth (nasal/oral); thirst (nasal); hypersalivation (IV/nasal).
Metabolism and nutrition disorders: Hyperglycaemia (nasal); hypokalaemia, anorexia (IV/nasal).
Musculoskeletal and connective tissue disorders: Muscle weakness (nasal).
Nervous system disorders: Headache, dizziness, insomnia, irritability, tremors, tolerance.
Psychiatric disorders: Anxiety, hallucination.
Renal and urinary disorders: Urinary retention.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Diaphoresis.
Vascular disorders: Hypertension; impaired circulation to the extremities (nasal/oral); vasodilation, flushing (nasal).
IM/IV/Parenteral/SC: C
Chỉ số theo dõi
Monitor blood pressure and pulse. Monitor patients with renal impairment for adverse reactions.
Quá liều
Symptoms: Nausea, vomiting, headache, fever, hypertension, restlessness, ventricular and supraventricular arrhythmias, respiratory depression, convulsion, paranoid psychosis, delusions and hallucinations. Management: Supportive and symptomatic treatment. May administer benzodiazepine or neuroleptic agent for CNS stimulant effects. For severe hypertension, may give parenteral antihypertensives such as nitrates, Ca channel blockers, Na nitroprusside, labetalol or phentolamine. Perform emesis or gastric lavage for severe oral ephedrine overdosage.
Tương tác
May increase risk of arrhythmias with halogenated anaesthetics (e.g. halothane, cyclopropane), cardiac glycosides, quinidine, and TCAs. May block the antihypertensive effect of adrenergic neurone blockers (e.g. guanethidine). Increased risk of vasoconstrictor or pressor effects with ergot alkaloids and oxytocin. May increase the incidence of nausea, insomnia and nervousness with theophylline. May increase clearance of dexamethasone. May potentiate stimulant effect of caffeine.
Potentially Fatal: May enhance the adverse or toxic effect of other indirect sympathomimetics (e.g. phenylephrine, phenylpropanolamine, pseudoephedrine, methylphenidate) and α-sympathomimetic agents. Enhanced hypertensive effect with MAOIs.
Ảnh hưởng đến kết quả xét nghiệm
May cause false-positive amphetamine enzyme multiplied immunoassay technique (EMIT) assay.
Tác dụng
Description:
Mechanism of Action: Ephedrine is a sympathomimetic that has α- and β- adrenergic activity. It stimulates both adrenergic receptors through direct and indirect mechanisms. It raises the blood pressure by increasing cardiac output, releases the stores of norepinephrine, and causes vasoconstriction of the mucosal blood vessels, thereby resulting in decreased thickness of the nasal mucosa.
Onset: Bronchodilation: Within 15-60 minutes (oral).
Duration: Bronchodilation: 2-4 hours; Pressor and cardiac responses: 1 hour (IV); 4 hours (oral).
Pharmacokinetics:
Absorption: Readily and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 90%.
Distribution: Distributed throughout the body and accumulates in the liver, lungs, kidneys, spleen, and brain. Crosses the placenta; enters breast milk.
Metabolism: Minimally metabolised in the liver, producing small amounts of metabolites, p-hydroxyephedrine, p-hydroxynorephedrine, norephedrine.
Excretion: Mainly via urine (approx 77% as unchanged drug and small amount of metabolites). Elimination half-life: Urine pH 5: Approx 3 hours, pH 6.3: Approx 6 hours.
Đặc tính

Chemical Structure Image
Ephedrine

Source: National Center for Biotechnology Information. PubChem Database. Ephedrine, CID=9294, https://pubchem.ncbi.nlm.nih.gov/compound/Ephedrine (accessed on Jan. 22, 2020)

Bảo quản
Store below 25°C. Protect from light.
Phân loại MIMS
Thuốc chống sung huyết mũi & các chế phẩm khác dùng cho mũi / Thuốc kích thích hô hấp / Thuốc co mạch
Phân loại ATC
R03CA02 - ephedrine ; Belongs to the class of adrenergics for systemic use, alpha- and beta-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
C01CA26 - ephedrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of hypotension.
Tài liệu tham khảo
Anon. Ephedrine (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/06/2021.

Anon. Ephedrine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/06/2021.

Anon. Ephedrine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/06/2021.

Bronkaid Max (Foundation Consumer Healthcare LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/06/2021.

Buckingham R (ed). Ephedrine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/06/2021.

Ephedrine Hydrochloride 3 mg/mL Solution for Injection (Aurum Pharmaceuticals Ltd). MHRA. https://products.mhra.gov.uk. Accessed 03/06/2021.

Ephedrine Hydrochloride Tablets BP 60 mg (Kensington Pharma Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 03/06/2021.

Ephedrine Nasal Drops 1% (Thornton & Ross Ltd). MHRA. https://products.mhra.gov.uk. Accessed 03/06/2021.

Ephedrine Sulfate (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/06/2021.

Joint Formulary Committee. Ephedrine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/06/2021.

Rinosan Propo Nasal Decongestant Spray (Bee Right LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/06/2021.

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