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Encyclopedia > Furosemide
Furosemide
Systematic (IUPAC) name
5-(aminosulfonyl)-4-chloro-2-
[(2-furanylmethyl)amino]benzoic acid
Identifiers
CAS number 54-31-9
ATC code C03CA01
PubChem 162482
DrugBank APRD00608
Chemical data
Formula C12H11ClN2O5S 
Mol. mass 330.745 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 43-69%
Metabolism hepatic and renal glucuronidation
Half life up to 100 minutes
Excretion renal 66%, biliary 33%
Therapeutic considerations
Pregnancy cat.

C(AU) C(US) IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is an easy way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number chlorine, Cl, 17 Chemical series nonmetals Group, period, block 17, 3, p Appearance yellowish green Standard atomic weight 35. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... This article is about the chemical element and its most stable form, or dioxygen. ... This article is about the chemical element. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... The simplified molecular input line entry specification or SMILES is a specification for unambiguously describing the structure of chemical molecules using short ASCII strings. ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... Example of glucuronidation Glucuronidation of alcohols and acids Glucuronidation is a major inactivating pathway for a huge variety of exogenous and endogenous molecules, including drugs, polluants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids and bile acids. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... For other uses, see Australia (disambiguation). ... For other uses of terms redirecting here, see US (disambiguation), USA (disambiguation), and United States (disambiguation) Motto In God We Trust(since 1956) (From Many, One; Latin, traditional) Anthem The Star-Spangled Banner Capital Washington, D.C. Largest city New York City National language English (de facto)1 Demonym American...

Legal status

Prescription only The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes Oral, IV, IM

Furosemide (INN) or frusemide (former BAN) is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi-Aventis under the brand name Lasix. It has also been used to prevent thoroughbred and standardbred race horses from bleeding through the nose during races. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... Intravenous therapy or IV therapy is the giving of liquid substances directly into a vein. ... Intramuscular injection is the injection of a substance directly into a muscle. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... A British Approved Name (BAN) is the official non-proprietary or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia (BP). ... Loop diuretics are diuretics that act on the ascending loop of Henle in the kidney. ... This page is about the condition called edema. ... Sanofi-aventis (Euronext: SAN, NYSE: SNY), headquartered in Paris, France, is one of the 3 largest pharmaceutical companies in the world, along with Pfizer,GlaxoSmithKline. ... For the processor with the same codename , see Athlon. ... Standardbred harness racing horses are so called because in the early years of the Trotting Registry, the standardbred stud book established in the United States in 1879 by the National Association of Trotting Horse Breeders, only horses who could race a mile in a standard time or better, or whose...


Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs. The World Anti-Doping Agency (WADA) is an independent foundation created through a collective initiative led by the International Olympic Committee (IOC). ... In sports, doping refers to the use of performance-enhancing drugs, particularly those that are forbidden by the organizations that regulate competitions. ...

Contents

Mechanism of action

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The name of lasix is derived from lasts six (hours) -- referring to its duration of action. Like other loop diuretics, furosemide acts by inhibiting the Na-K-2Cl symporter in the thick ascending limb of the loop of Henle. The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone, it also abolishes the corticomedullary osmotic gradient and blocks negative as well as positive free water clearance. The Na-K-2Cl symporter is an ion pump carrier protein that is inhibited by loop diuretics. ... The thick ascending limb of loop of Henle (or distal straight tubule) can be divided into two parts: that in the renal medulla, and that in the renal cortex. ... In the kidney, the loop of Henle is the portion of the nephron that leads from the proximal convoluted tubule to the distal convoluted tubule. ... In the physiology of the kidney, free water clearance (CH2O) is the volume of blood plasma that is cleared of solute-free water per unit time. ...


Additionally, furosemide is a noncompetitive subtype-specific blocker of GABA-A receptors (Korpi et al, 1995, Tia et al, 1996, Wafford et al, 1996). Furosemide has been reported to reversibly antagonize GABA-evoked currents of alpha6 beta2 gamma2 receptors at microM concentrations, but not alpha1 beta2 gamma2 receptors (Korpi et al, 1995; Wafford et al, 1996). During development, the alpha6 beta2 gamma2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide (Tia et al,. 1995).


Clinical use in humans

Furosemide, as a loop diuretic, is principally used in the following indications (Aventis, 1998): Year 1998 (MCMXCVIII) was a common year starting on Thursday (link will display full 1998 Gregorian calendar). ...

It is also sometimes used in the management of severe hypercalcemia in combination with adequate rehydration (Rossi, 2004). This page is about the condition called edema. ... Liver cirrhosis as seen on an axial CT of the abdomen. ... Renal failure is when the kidneys fail to function properly. ... For other forms of hypertension, see Hypertension (disambiguation). ... Cerebral edema (cerebral oedema in British English) is an excess accumulation of water in the intra- and/or extracellular spaces of the brain. ... Pulmonary edema is swelling and/or fluid accumulation in the lungs. ... Diuresis is the production of urine by the kidney. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Hypercalcaemia is an elevated calcium level in the blood. ...


Although disputed,[1] it is considered ototoxic: "usually with large parenteral doses and rapid administration and in renal impairment"[2] Ototoxicity is damage of the ear (oto), specifically the cochlea or auditory nerve and sometimes the vestibulum, by a toxin (often medication). ...


The tendency, as per all loop diuretics, to cause low potassium levels (hypokalaemia) has given rise to combination products, either with potassium itself (e.g. Lasix-K) or with the potassium sparing diuretic of amiloride (Co-amilofruse). Hypokalemia is a condition in which the body fails to retain sufficient potassium to maintain health. ... Amiloride is an antihypertensive, a potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. ...


Use in horses

The diuretic-effects are put to use most commonly in horses to prevent "bleeding" during a race. Sometime in the early 1970s, furosemide's ability to prevent, or at least greatly reduce, the incidence of "bleeding" (EIPH) by horses during races was discovered accidentally. Pursuant to the racing rules of most states, horses that bleed from the nostrils three times are permanently barred from racing (for their own protection). Clinical trials followed, and by decade's end, racing commissions in some states began legalizing its use on race horses. On September 1, 1995, New York became the last state in the United States to approve such use, after years of refusing to consider doing so. Some states allow its use for all racehorses; some allow it only for confirmed "bleeders." However, its use for this purpose is still prohibited in many other countries, and veterinarians dispute its use for this problem. The 1970s decade refers to the years from 1970 to 1979, also called The Seventies. ... Exercise Induced Pulmonary Hemorrhage (EIPH) also known as bleeding or a bleeding attack has been known to occur in horses that engage in short periods of strenuous exercise. ... is the 244th day of the year (245th in leap years) in the Gregorian calendar. ... Year 1995 (MCMXCV) was a common year starting on Sunday. ... State nickname: Empire State Other U.S. States Capital Albany Largest city New York Governor George Pataki Official languages None Area 141,205 km² (27th)  - Land 122,409 km²  - Water 18,795 km² (13. ...


Furosemide is also used in horses for pulmonary edema, congestive heart failure (in combination with other drugs), and allergic reactions. Despite the fact that it increases circulation to the kidneys, it does not help kidney function, and is not recommended for kidney disease.


Precautions, side-effects, and administration

Furosemide is injected either intramuscularly (IM) or intravenously (IV), usually 0.5-1.0 mg/lb 2x/day, although less before a horse is raced. As with many diuretics, it can cause dehydration and electrolyte imbalance, including loss of potassium, calcium, sodium, and magnesium. It is especially important to prevent potassium loss, as it can cause serious problems. The drug should therefore not be used in horses that are dehydrated or experiencing kidney failure. It should be used with caution in horses with liver problems or electrolyte abnormalities. Overdose may lead to dehydration, change in drinking patterns and urination, seizures, GI problems, kidney damage, lethargy, collapse, and coma. Intramuscular injection is the injection of a substance directly into a muscle. ... Intravenous therapy or IV therapy is the giving of liquid substances directly into a vein. ... Dehydration (hypohydration) is the removal of water (hydro in ancient Greek) from an object. ... Electrolyte disturbance refers to an abnormal change in the levels of electrolytes in the body. ... General Name, symbol, number potassium, K, 19 Chemical series alkali metals Group, period, block 1, 4, s Appearance silvery white Standard atomic weight 39. ... For other uses, see Calcium (disambiguation). ... For sodium in the diet, see Salt. ... General Name, symbol, number magnesium, Mg, 12 Chemical series alkaline earth metals Group, period, block 2, 3, s Appearance silvery white solid at room temp Standard atomic weight 24. ...


Furosemide should be used with caution when combined with corticosteriods (as this increases the risk of electrolyte imbalance), aminoglycoside antibiotics (increases risk of kidney or ear damage), and trimethoprim sulfa (causes decreased platelet count). It may also cause interactions with anesthesics, so its use should be related to the veterinarian if the animal is going into surgery, and it decreases the kidney's ability to excrete aspirin, so dosages will need to be adjusted if combined with that drug. This article is about the drug. ...


Furosemide may cause Digoxin toxicity due to hypokalemia. Digoxin (INN) (IPA: ) is a purified cardiac glycoside extracted from the foxglove plant, Digitalis lanata. ...


The drug is best not used during pregnancy or in a lactating mare, as it has been shown to be passed through the placenta and milk in studies with other species. It should not be used in horses with pituitary pars intermedia dysfunction (Cushings). Cushings syndrome (also called hypercortisolism or hyperadrenocorticism) is an endocrine disorder caused by high levels of cortisol in the blood from a variety of causes, including primary pituitary adenoma (known as Cushings disease), primary adrenal hyperplasia or neoplasia, ectopic ACTH production (e. ...


Furosemide is detectible in urine 36-72 hours following injection. Its use is prohibited by most equestrian organizations.


Drug Interactions

Furosemide has potential interactions with the following medications:[1]

Aminoglycosides are a group of antibiotics that are effective against certain types of bacteria. ... An antibiotic is a drug that kills or slows the growth of bacteria. ... Gentamicin is an aminoglycoside antibiotic, and can treat many types of bacterial infections, particularly Gram-negative infection. ... This article is about the drug. ... Ethacrynic acid (Edecrin®) is a loop diuretic medication used to treat high blood pressure and the swelling caused by diseases like congestive heart failure, liver failure, and kidney failure. ... Hydrochlorothiazide (Apo-Hydro®, Aquazide H®, Microzide®, Oretic®), sometimes abbreviated HCT, HCTZ, or HZT is a popular diuretic drug that acts by inhibiting the kidneys ability to retain water. ... Indomethacin (USAN) or indometacin (INN) is a non-steroidal anti-inflammatory drug commonly used to reduce fever, pain, stiffness, and swelling. ... This article discusses the pharmacological uses of lithium salts; for information on the chemistry of individual lithium salts, see Category:Lithium compounds. ... Antihypertensives are a class of drugs that are used in medicine and pharmacology to treat hypertension (high blood pressure). ... Doxazosin mesylate, a quinazoline compound sold by Pfizer under the brand name Cardura®, is an alpha blocker used to treat high blood pressure and benign prostatic hyperplasia. ... Sucralfate is a prescription medication used to treat peptic ulcers. ...

Brand names

Some of the brand names under which furosemide is marketed include: Aisemide, Beronald, Desdemin, Discoid, Diural, Diurapid, Dryptal, Durafurid, Errolon, Eutensin, Frusetic, Frusid, Fulsix, Fuluvamide, Furesis, Furix, Furo-Puren, Furosedon, Hydro-rapid, Impugan, Katlex, Lasilix, Lasix, Lodix, Lowpston, Macasirool, Mirfat, Nicorol, Odemase, Oedemex, Profemin, Rosemide, Rusyde, Salix, Trofurit, Urex, Frudix


Founded around 1964.


References

  1. ^ Rais-Bahrami K, Majd M, Veszelovszky E, Short B (2004). "Use of furosemide and hearing loss in neonatal intensive care survivors.". Am J Perinatol 21 (6): 329-32. doi:10.1055/s-2004-831887. PMID 15311369. 
  2. ^ BNF 45 March 2003

A digital object identifier (or DOI) is a standard for persistently identifying a piece of intellectual property on a digital network and associating it with related data, the metadata, in a structured extensible way. ... Otherwise known as the doctors prescribing Bible the British National Formulary (BNF) contains a wide spectrum of information on prescribing and pharmacology, among others indications, side effects and costs of the prescription of all medication drugs available on the National Health Service. ...

Further reading

  • Aventis Pharma (1998). Lasix Approved Product Information. Lane Cove: Aventis Pharma Pty Ltd.
  • Forney, Barbara C, MS, VMD. Equine Medications, Revised Edition. Blood Horse Publications. Lexington, KY. Copyright 2007.
  • Rossi S (Ed.) (2004). Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
  • Korpi ER, Kuner T, Seeburg PH, Lüddens H (1995). "Selective antagonist for the cerebellar granule cell-specific gamma-aminobutyric acid type A receptor". Mol. Pharmacol. 47 (2): 283-9. PMID 7870036. 
  • Tia S, Wang JF, Kotchabhakdi N, Vicini S (1996). "Developmental changes of inhibitory synaptic currents in cerebellar granule neurons: role of GABA(A) receptor alpha 6 subunit". J. Neurosci. 16 (11): 3630-40. PMID 8642407. 
  • Wafford KA, Thompson SA, Thomas D, Sikela J, Wilcox AS, Whiting PJ (1996). "Functional characterization of human gamma-aminobutyric acidA receptors containing the alpha 4 subunit". Mol. Pharmacol. 50 (3): 670-8. PMID 8794909. 

The Australian Medicines Handbook or AMH is a medical reference text commonly used in practice by health professionals (particularly general practitioners and pharmacists) in Australia. ...

External links

Prazosin, brand name Minipress®, is a medication used to treat high blood pressure (hypertension). ... Guanethidine is an antihypertensive drug. ... Indoramin BARATOL® is a piperidine antiadrenergic agent. ... Doxazosin mesylate, a quinazoline compound sold by Pfizer under the brand name Cardura®, is an alpha blocker used to treat high blood pressure and benign prostatic hyperplasia. ... A vasodilator is a drug or chemical that relaxes the smooth muscle in blood vessels, which causes them to dilate. ... Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. ... Hydralazine hydrochloride (1 -hydrazinophthalazine monohydrochloride; Apresoline®) is a medication used to treat high blood pressure. ... Minoxidil is a vasodilator and originally was exclusively used as an oral drug (Loniten®) to treat high blood pressure. ... Sodium nitroprusside is the chemical compound Na2[Fe(CN)5NO]. It is a potent peripheral vasodilator that affects both arterioles and venules. ... Phentolamine is a competitive nonselective alpha adrenergic receptor antagonist. ... A serotonin antagonist acts to inhibit the action at serotonin receptors. ... Ketanserin is a serotonin receptor antagonist. ... A endothelin receptor antagonist (ERA) is a drug which blocks endothelin receptors. ... Bosentan is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). ... Ambrisentan is a drug being researched for use in the treatment of pulmonary hypertension. ... Sitaxsentan or sitaxsentan sodium (to be marketed as Thelin®) is a small molecule sodium salt that blocks the action of endothelin on the endothelin-A receptor selectively (by a factor of 6000 compared to the ERB), and is undergoing FDA approval for treating pulmonary hypertension. ... Thiazides are a class of drug that promote water loss from the body ((diuretics)). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. ... Bendroflumethiazide, (formerly known as bendrofluazide), is a thiazide diuretic, used to treat hypertension. ... Chlorothiazide sodium (Diuril®) is a diuretic used within the hospital setting or for personal use to manage excess fluid associated with congestive heart failure. ... Hydrochlorothiazide (Apo-Hydro®, Aquazide H®, Microzide®, Oretic®), sometimes abbreviated HCT, HCTZ, or HZT is a popular diuretic drug that acts by inhibiting the kidneys ability to retain water. ... Chlortalidone (formerly spelt chlorthalidone in the UK) is a thiazide diuretic, used to treat hypertension. ... Indapamide is a diuretic drug, usually used in the treatment of hypertension. ... Quinethazone (brand name Hydromox®) is a thiazide diuretic used to treat hypertension. ... Mersalyl acid (Mersal) is a mercurial diuretic. ... Metolazone is an oral diuretic drug, commonly classified with the thiazide diuretics, and marketed under the brand names Zaroxolyn and Mykrox. ... Theobromine, also known as xantheose,[1] is a bitter alkaloid of the cacao plant. ... Cicletanine is a furopyridine low-ceiling diuretic drug, usually used in the treatment of hypertension. ... Loop diuretics are diuretics that act on the ascending loop of Henle in the kidney. ... Bumetanide is a loop diuretic of the sulfamyl category to treat heart failure. ... Torasemide (rINN) or torsemide (USAN) is a pyridine-sulfonylurea type loop diuretic mainly used in the management of edema associated with congestive heart failure. ... Potassium-sparing diuretic refers to diuretic drugs that do not promote the secretion of potassium into the urine. ... Sodium channels (also known as voltage-gated sodium channels) are integral membrane proteins that are localized in and conduct sodium ions (Na+) through a cells plasma membrane. ... Amiloride is an antihypertensive, a potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. ... Triamterene is a potassium-sparing diuretic used in combination with thiazide diuretics for the treatment of hypertension. ... Aldosterone antagonist refers to drugs which antagonise the action of aldosterone at mineralocorticoid receptors. ... Spironolactone (marketed under the trade names Aldactone, Novo-Spiroton, Spiractin, Spirotone, or Berlactone) is a diuretic and is used as an antiandrogen. ... Eplerenone (INN) (IPA: ) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. ... Potassium canrenoate (or canrenoate potassium) is an aldosterone antagonist. ... Canrenone is an aldosterone antagonist. ...

  Results from FactBites:
 
furosemide (Lasix) - drug class, medical uses, medication side effects, and drug interactions by MedicineNet.com (403 words)
Furosemide works by blocking the absorption of salt and fluid in the kidney tubules, causing a profound increase in urine output (diuresis).
Furosemide is used to treat excessive fluid accumulation and swelling (edema) of the body caused by heart failure, cirrhosis, chronic kidney failure, and nephrotic syndrome.
Furosemide may increase the toxic effect of aminoglycoside antibiotics on the ear, especially in patients with kidney dysfunction.
Furosemide (970 words)
Furosemide can also be used to remove fluid from body cavities or peripheral tissues even when the cause is not heart failure.
Furosemide can also be helpful in reducing dangerously high potassium blood levels and has been used in the horse to treat excercise induced pulmonary hemorrhage (nose bleeds).
Furosemide is associated with an increase in blood sugar levels.
  More results at FactBites »

 
 

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