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furosemide (Lasix, Furoscix)
Tradename: Lasix (LAsts for SIX hours).
Indications:
1) hypertension
2) heart failure
3) edema, including peripheral edema & pulmonary edema
4) IV form used to increase renal excretion of Ca+2 in patients with hypercalcemia
5) empiric treatment of oliguria
Contraindications:
- of no benefit in acute renal failure [5]
Dosage:
- 1 mg/kg up to 20-80 mg IV
- IV infusion: 40 mg loading dose, then 2-200 mg/hr
- subcutaneous self-administration (Furoscix) 80 mg dose over 5 hours [7]
- 20-80 mg PO QD/BID
- Max dose:
a) 160 mg/day (hepatic failure),
b) 240 mg/day (nephrotic syndrome)
c) 600 mg/day (CHF with normal renal function) [6]
d) doses as large as 2.5 g/day have been used
Tabs: 20, 40, 80 mg. Solution 10 & 40 mg/5 mL. Furoscix: single-use pre-filled cartridge attaches to the patient's abdomen [7]
Pharmacokinetics:
1) absorption is erratic
2) 96-99% is bound to plasma proteins
3) renal clearance is by active secretion
4) onset of diuresis within 30-60 minutes (PO) 5 min (IV)
5) peak effect in 1-2 hours; reduced & delayed in the elderly
6) duration of action: 6-8 hours
7) 50-80% of IV dose & 20-55% of PO dose is excreted unchanged in the urine
8) 1/2life is about 90 minutes, increased in patients with cirrhosis, CHF & end-stage renal disease (ESRD)
Adverse effects:
1) common (> 10%)
- orthostatic hypotension
2) less common (1-10%)
- electrolyte disorder, blurred vision, diarrhea, headache, photosensitivity, loss of appetite, abdominal pain
3) uncommon (< 1%)
- rash, injection site erythema, hyperuricemia, gout, hepatic dysfunction
- agranulocytosis, leukopenia, anemia, thrombocytopenia
- ototoxicity, pancreatitis, xanthopsia, nausea
- nephrocalcinosis, prerenal azotemia, interstitial nephritis
4) other
- hypocalcemia
- K+ depletion
- Ca+2 & Mg+2 depletion
- hypochloremic alkalosis
- dilutional hyponatremia
- hyperglycemia
- glucosuria
- hypercholesterolemia (mild) total & LDL
- vasculitis
- reaction to sulfa-drugs (cross-sensitivity)
- pseudo-porphyria cutanea tarda
- bullous pemphigoid [8]
Drug interactions:
1) drugs that cause K+ depletion, i.e. beta-2 agonists
2) decreased lithium clearance
3) increased requirements of insulin &/or sulfonylureas
4) probenecid
5) increased risk of renal failure in combination with NSAIDs
6) enhancement of effects of muscle relaxants
Mechanism of action:
1) inhibits resorption of electrolytes in the ascending loop of Henle
2) decreases the reabsorption of Na+ & Cl-
3) increases K+ excretion in the distal renal tubule
4) other electrolytes affected include: Ca+2, Mg+2, NH4+, HCO3- & phosphate
5) Lasix acutely reduces preload via a direct venodilation in addition to its diuretic effect; thus furosemide is particularly useful in the setting of congestive heart failure & pulmonary edema
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with drug (more general classes)
General
loop diuretic
sulfanilamide
Properties
MISC-INFO: elimination route KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed)
Lippincott-Raven, Philadelphia, 1998, pg 473
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Ho KM and Sheridan DJ
Meta-analysis of furosemide to prevent or treat acute renal
failure.
BMJ 2006, 333:420
PMID: 16861256
- Medical Knowledge Self Assessment Program (MKSAP) 15,
American College of Physicians, Philadelphia 2009
- Lou N
FDA Approves At-Home Furosemide for Heart Failure.
Strong diuretic to become available outside the hospital setting.
MedPage Today October 10, 2022
https://www.medpagetoday.com/cardiology/chf/101139
- NEJM Knowledge+ Dermatology
- Lee JJ, Downham TF 2nd.
Furosemide-induced bullous pemphigoid: case report and review of literature.
J Drugs Dermatol. 2006 Jun;5(6):562-4.
PMID: 16774111 Review.
Component-of
amiloride/furosemide