Etacrynic acid


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Acute pulmonary oedema
Adult: 0.5-1 mg/kg or 50 mg via slow inj or infusion over 10 min; a 2nd dose may be given, if required, at a new inj site. Max: 100 mg.

Oral
Oedema
Adult: Initially, 50 mg in the morning, increase if necessary, by 25-50 mg increments daily to min effective dose. Usual effective range: 50-200 mg daily. Severe cases: Up to 400 mg daily. Doses >50 mg should be given in divided doses.
Child: >2 yr Initially, 25 mg daily, increase cautiously if necessary, by 25 mg daily.
Hướng dẫn pha thuốc
Add 50 mL of dextrose 5% or NaCl 0.9% inj to the vial.
Tương kỵ
Incompatible w/ soln w/ pH <5.
Chống chỉ định
Anuria, history of severe watery diarrhoea. Infants.
Thận trọng
Patient w/ advanced hepatic cirrhosis, electrolyte imbalance, hepatic encephalopathy, severe myocardial disease and those undergoing surgery. Renal impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Significant: Fluid/electrolyte loss (e.g. hyponatraemia, hypokalaemia, hypochloraemic alkalosis, hypomagnesaemia), nephrotoxicity, ototoxicity, wt loss, orthostatic hypotension, dehydration.
Nervous: Paraesthesia, dizziness, fainting, headache, fatigue, apprehension, malaise, mental confusion, vertigo.
GI: Thirst, anorexia, abdominal discomfort or pain, dysphagia, nausea, vomiting, diarrrhoea/profuse watery diarrhoea, acute pancreatitis.
Hepatic: Jaundice.
Genitourinary: Reversible hyperuricaemia, decreased urinary urate, interstitial nephritis, increased creatinine concentration.
Endocrine: Metabolic alkalosis, hyperglycaemia, dyslipidaemia, gout.
Musculoskeletal: Weakness, muscle cramps.
Otic: Deafness, tinnitus.
Dermatologic: Exfoliative dermatitis, Stevens-Johnson syndrome, bullous eruptions, rash.
Others: Local irritation, pain, thrombophlebitis.
MonitoringParameters
Monitor BP, renal function, serum electrolytes, CO2, BUN, fluid status including input and output, wt, hearing.
Quá liều
Symptoms: Excessive diuresis w/ electrolyte depletion (e.g. hypokalaemia, hypochloraemia, hyponatraemia) and dehydration. Management: Symptomatic and supportive treatment. Induce emesis or perform gastric lavage. For resp depression, administer oxygen or employ artificial respiration, if necessary.
Tương tác
May increase the ototoxicity and nephrotoxicity of aminoglycoside antibiotics and some cephalosporins. May increase risk of GI bleeding when used w/ other gastric irritants, corticosteroids, anticoagulants. May cause orthostatic hypotension when used w/ other antihypertensive agents. Displaces warfarin from plasma protein. May increase risk of lithium toxicity. Decreased therapeutic effect w/ NSAIDs. May interfere w/ the hypoglycaemic effect of insulin or other antidiabetic agents. May potentiate kaliuresis and natriuretic effect of acetazolamide, dichlorphenamide, methazolamide.
Food Interaction
Enhanced hypokalaemic effect w/ licorice. Diminished antihypertensive effect w/ yohimbine.
Lab Interference
May cause false-negative aldosterone/renin ratio (ARR). Alters glucose tolerance tests.
Tác dụng
Description: Etacrynic acid is a loop diuretic that binds w/ sulfhydryl groups of renal cellular proteins. It inhibits the reabsorption of Na and Cl in the ascending loop of Henle and distal renal tubules, interfering w/ the Cl-binding cotransport system, hence excretion of Na, K, Ca, Mg, and Cl ions are increased and water excretion enhanced.
Onset: Approx 30 min (oral); 5 min (IV).
Duration: 12 hr (oral); 2 hr (IV).
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 2 hr (oral); 30 min (IV).
Distribution: Plasma protein binding: >90%.
Metabolism: Metabolised in the liver (35-40%) to active cysteine conjugate.
Excretion: Via faeces and urine (30-60% as unchanged drug). Elimination half-life: 2-4 hr.
Đặc tính

Chemical Structure Image
Etacrynic acid

Source: National Center for Biotechnology Information. PubChem Database. Ethacrynic acid, CID=3278, https://pubchem.ncbi.nlm.nih.gov/compound/Ethacrynic-acid (accessed on Jan. 22, 2020)

Bảo quản
Store at 25°C.
Phân loại MIMS
Phân loại ATC
C03CC01 - etacrynic acid ; Belongs to the class of high-ceiling aryloxyacetic acid derivative diuretics.
References
Anon. Ethacrynic Acid. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/07/2017.

Buckingham R (ed). Etacrynic Acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/07/2017.

Ethacrynic Sodium Powder, for Soln (Oceanside Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/07/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Ethacrynic Acid, Ethacrynate Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com/. Accessed 03/07/2017.

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