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Chemistry

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Also known as: 54-31-9, Frusemide, Lasix, Furosemid, Furanthril, Errolon
Molecular Formula
C12H11ClN2O5S
Molecular Weight
330.74  g/mol
InChI Key
ZZUFCTLCJUWOSV-UHFFFAOYSA-N
FDA UNII
7LXU5N7ZO5

Furosemide
A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.
Furosemide is a Loop Diuretic. The physiologic effect of furosemide is by means of Increased Diuresis at Loop of Henle.
1 2D Structure

Furosemide

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
4-chloro-2-(furan-2-ylmethylamino)-5-sulfamoylbenzoic acid
2.1.2 InChI
InChI=1S/C12H11ClN2O5S/c13-9-5-10(15-6-7-2-1-3-20-7)8(12(16)17)4-11(9)21(14,18)19/h1-5,15H,6H2,(H,16,17)(H2,14,18,19)
2.1.3 InChI Key
ZZUFCTLCJUWOSV-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1=COC(=C1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl
2.2 Other Identifiers
2.2.1 UNII
7LXU5N7ZO5
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Errolon

2. Frusemid

3. Frusemide

4. Furanthril

5. Furantral

6. Furosemide Monohydrochloride

7. Furosemide Monosodium Salt

8. Fursemide

9. Fusid

10. Lasix

2.3.2 Depositor-Supplied Synonyms

1. 54-31-9

2. Frusemide

3. Lasix

4. Furosemid

5. Furanthril

6. Errolon

7. Fusid

8. Aisemide

9. Beronald

10. Desdemin

11. Frusemin

12. Fuluvamide

13. Furanthryl

14. Furantril

15. Fursemide

16. Lowpstron

17. Macasirool

18. Prefemin

19. Rosemide

20. Trofurit

21. Fulsix

22. Furesis

23. Katlex

24. Lasilix

25. Radonna

26. Seguril

27. Transit

28. Lasex

29. Salix

30. Urex

31. Marsemide

32. Eutensin

33. Frusetic

34. Fursemid

35. Logirene

36. Oedemex

37. Promedes

38. Frusid

39. Lazix

40. Mirfat

41. Frusemid

42. Frusenex

43. Furanturil

44. Furosedon

45. Profemin

46. Urosemide

47. Aluzine

48. Diural

49. Dryptal

50. Impugan

51. Nicorol

52. Rusyde

53. Uremide

54. Uresix

55. Yidoli

56. Disal

57. Laxur

58. Urian

59. Apo-frusemide

60. Hydro-rapid

61. Anfuramaide

62. Arasemide

63. Bioretic

64. Disemide

65. Diurapid

66. Diurolasa

67. Diusemide

68. Durafurid

69. Fluidrol

70. Frusedan

71. Fuluvamine

72. Furobeta

73. Furodiurol

74. Furodrix

75. Furorese

76. Furosemidum

77. Furosemix

78. Furoside

79. Furosifar

80. Furovite

81. Fursemida

82. Hissuflux

83. Hydroled

84. Jenafusid

85. Lasiletten

86. Lowpston

87. Moilarorin

88. Novosemide

89. Protargen

90. Radisemide

91. Selectofur

92. Sigasalur

93. Spirofur

94. Synephron

95. Zafimida

96. Aldalix

97. Aquarid

98. Aquasin

99. Cetasix

100. Dirine

101. Discoid

102. Diurin

103. Diusil

104. Diuzol

105. Dranex

106. Edemid

107. Edenol

108. Endural

109. Farsix

110. Franyl

111. Frumex

112. Frumide

113. Frusema

114. Furetic

115. Furfan

116. Furmid

117. Furocot

118. Furomen

119. Furomex

120. Furosan

121. Furose

122. Furosix

123. Furoter

124. Fursol

125. Hydrex

126. Kofuzon

127. Kolkin

128. Kutrix

129. Lasemid

130. Liside

131. Luscek

132. Nelsix

133. Odemase

134. Odemex

135. Promide

136. Puresis

137. Radouna

138. Salinex

139. Salurex

140. Salurid

141. Uridon

142. Uritol

143. Aldic

144. Depix

145. Desal

146. Eliur

147. Fluss

148. Furex

149. Furix

150. Golan

151. Hydro

152. Nadis

153. Retep

154. Rosis

155. Vesix

156. Mita

157. Apo-furosemide

158. Furo-puren

159. Lasix Retard

160. Polysquall A

161. 4-chloro-n-furfuryl-5-sulfamoylanthranilic Acid

162. Less Diur

163. Neo-renal

164. Furo-basan

165. Furosemidu

166. Urex-m

167. Nephron

168. Furomide M.d.

169. Furosemida

170. 4-chloro-n-(2-furylmethyl)-5-sulfamoylanthranilic Acid

171. Lb 502

172. 5-(aminosulfonyl)-4-chloro-2-[(2-furylmethyl)amino]benzoic Acid

173. 2-furfurylamino-4-chloro-5-sulfamoylbenzoic Acid

174. Lb-502

175. Nci-c55936

176. Lasix (tn)

177. Benzoic Acid, 5-(aminosulfonyl)-4-chloro-2-[(2-furanylmethyl)amino]-

178. 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic Acid

179. Diumide-k

180. 4-chloro-5-sulfamoyl-n-furfuryl-anthranilic Acid

181. 4-chloro-2-(furan-2-ylmethylamino)-5-sulfamoylbenzoic Acid

182. Chlor-n-(2-furylmethyl)-5-sulfamylanthranilsaeure

183. Anthranilic Acid, 4-chloro-n-furfuryl-5-sulfamoyl-

184. Chembl35

185. 4-chloro-2-((furan-2-ylmethyl)amino)-5-sulfamoylbenzoic Acid

186. Nsc-269420

187. Benzoic Acid, 5-(aminosulfonyl)-4-chloro-2-((2-furanylmethyl)amino)-

188. 7lxu5n7zo5

189. Chebi:47426

190. Furosemidu [polish]

191. 5-(aminosulfonyl)-4-chloro-2-((2-furanylmethyl)amino)benzoic Acid

192. 5-(aminosulfonyl)-4-chloro-2-[(2-furanylmethyl)amino]benzoic Acid

193. Cas-54-31-9

194. Furosemidum [inn-latin]

195. Furosemida [inn-spanish]

196. Ncgc00016241-06

197. Sal Diureticum

198. 4-chloro-2-{[(furan-2-yl)methyl]amino}-5-sulfamoylbenzoic Acid

199. Dsstox_cid_648

200. Dsstox_rid_75710

201. Dsstox_gsid_20648

202. Furosemide "mita"

203. Fun

204. Furosemide Mita

205. Furosemide Oral

206. 5-(aminosulfonyl)-4-chloro-2-([2-furanylmethyl]amino)benzoic Acid

207. 5-(aminosulfonyl)-4-chloro-2-[(furan-2-ylmethyl)amino]benzoic Acid

208. Smr000058202

209. Ccris 1951

210. Furosemide ''mita''

211. Hsdb 3086

212. Sr-01000765380

213. Einecs 200-203-6

214. Hoe-058a

215. Unii-7lxu5n7zo5

216. Nsc 269420

217. Brn 0840915

218. Neosemid

219. Zafurida

220. Chlor-n-(2-furylmethyl)-5-sulfamylanthranilsaeure [german]

221. 5-(aminosulfonyl)-4-chloro-2-((2-furylmethyl)amino)benzoic Acid

222. Furosemide, 4

223. Urex M

224. Furosemide (lasix)

225. Prestwick_752

226. Frumil (salt/mix)

227. Mfcd00010549

228. Furosemide [usan:usp:inn:ban:jan]

229. Spectrum_001100

230. 1z9y

231. 4-chloro-2-[(2-furylmethyl)amino]-5-sulfamoylbenzoic Acid

232. Furosemide [mi]

233. Furosemide [inn]

234. Furosemide [jan]

235. Prestwick0_000341

236. Prestwick1_000341

237. Prestwick2_000341

238. Prestwick3_000341

239. Spectrum2_001005

240. Spectrum3_000437

241. Spectrum4_000560

242. Spectrum5_000744

243. Furosemide [hsdb]

244. Furosemide [iarc]

245. Furosemide [usan]

246. F0182

247. Furosemide [vandf]

248. Upcmld-dp022

249. Furosemide [mart.]

250. Schembl9811

251. Furosemide [usp-rs]

252. Furosemide [who-dd]

253. Furosemide [who-ip]

254. Oprea1_667724

255. Bspbio_000401

256. Bspbio_002054

257. Kbiogr_001259

258. Kbioss_001580

259. 5-18-09-00555 (beilstein Handbook Reference)

260. Mls001066374

261. Mls001306403

262. Mls002548896

263. Bidd:gt0139

264. Divk1c_000575

265. Spectrum1500310

266. Spbio_001129

267. Spbio_002322

268. Bpbio1_000443

269. Furosemide (jp17/usp/inn)

270. Gtpl4839

271. Furosemide [green Book]

272. Dtxsid6020648

273. Furosemide [orange Book]

274. Upcmld-dp022:001

275. Bdbm25902

276. Hms501m17

277. Kbio1_000575

278. Kbio2_001580

279. Kbio2_004148

280. Kbio2_006716

281. Kbio3_001274

282. Zinc35804

283. 4-chloro-2-(2-furylmethylamino)-5-sulfamoyl-benzoic Acid

284. Furosemide [ep Monograph]

285. Ninds_000575

286. Furosemide [usp Monograph]

287. Hms1569e03

288. Hms1920b03

289. Hms2090k06

290. Hms2091h05

291. Hms2096e03

292. Hms2233h03

293. Hms3259m03

294. Hms3370j22

295. Hms3655e09

296. Hms3713e03

297. Hms3874g03

298. Pharmakon1600-01500310

299. Furosemide 1.0 Mg/ml In Methanol

300. Furosemidum [who-ip Latin]

301. Albb-019200

302. Hy-b0135

303. Tox21_110322

304. Tox21_202213

305. Tox21_302971

306. Bbl027780

307. Ccg-40223

308. Nsc269420

309. Nsc757039

310. Stk177334

311. Wln: T5oj B1mr Cg Fvq Dszw

312. Akos000266625

313. Furosemide 100 Microg/ml In Methanol

314. Tox21_110322_1

315. Bcp9000708

316. Cs-1915

317. Db00695

318. Ks-1226

319. Nc00453

320. Nsc-757039

321. Idi1_000575

322. Smp1_000129

323. Ncgc00016241-01

324. Ncgc00016241-02

325. Ncgc00016241-03

326. Ncgc00016241-04

327. Ncgc00016241-05

328. Ncgc00016241-07

329. Ncgc00016241-08

330. Ncgc00016241-10

331. Ncgc00016241-11

332. Ncgc00090893-01

333. Ncgc00090893-02

334. Ncgc00090893-03

335. Ncgc00090893-05

336. Ncgc00090893-06

337. Ncgc00256523-01

338. Ncgc00259762-01

339. Ac-11067

340. Bf166384

341. Bp-13261

342. Sbi-0051389.p003

343. Db-052536

344. Ab00052001

345. Sw196894-3

346. 54f319

347. C07017

348. D00331

349. D87719

350. Ab00052001-10

351. Ab00052001-11

352. Ab00052001_12

353. Ab00052001_13

354. A830094

355. Q388801

356. Sr-01000765380-2

357. Sr-01000765380-3

358. Sr-01000765380-7

359. Brd-k78010432-001-05-8

360. Brd-k78010432-001-10-8

361. Z275128584

362. 4-chloro-2-(2-furanylmethylamino)-5-sulfamoylbenzoic Acid

363. Furosemide, British Pharmacopoeia (bp) Reference Standard

364. Furosemide, European Pharmacopoeia (ep) Reference Standard

365. 4-chloranyl-2-(furan-2-ylmethylamino)-5-sulfamoyl-benzoic Acid

366. Furosemide, United States Pharmacopeia (usp) Reference Standard

367. 4-chloro-n-furfuryl-5-sulfamoylanthranilic Acid Furosemide

368. 4-chloro-n-furfuryl-5-sulfamoylanthranilic Acid??furosemide

369. 5-(aminosulfamyl)-4-chloro-2-[(2-furanylmethyl)amino]benzoic Acid

370. 5-(aminosulfonyl)-4-chloro-2-[(2-furylmethyl)amino]benzoic Acid #

371. 4-chloro-n-furfuryl-5-sulfamoylanthranilic Acid Pound>>furosemide

372. Furosemide, Pharmaceutical Secondary Standard; Certified Reference Material

373. Furosemide For Peak Identification, European Pharmacopoeia (ep) Reference Standard

374. Furosemide Solution, 1.0 Mg/ml In Methanol, Ampule Of 1 Ml, Certified Reference Material

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 330.74 g/mol
Molecular Formula C12H11ClN2O5S
XLogP32
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count7
Rotatable Bond Count5
Exact Mass330.0077203 g/mol
Monoisotopic Mass330.0077203 g/mol
Topological Polar Surface Area131 Ų
Heavy Atom Count21
Formal Charge0
Complexity481
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 6  
Drug NameFurosemide
PubMed HealthFurosemide
Drug ClassesCardiovascular Agent
Drug LabelThe CAS Registry Number is 54-31-9.It has a molecular formula of C12H11ClN2O5S and a molecular weight of 330.75.The molecular structure is as follows:...
Active IngredientFurosemide
Dosage FormTablet; Injectable; Solution
RouteInjection; Oral
Strength40mg/5ml; 10mg/ml; 80mg; 40mg; 20mg
Market StatusPrescription
CompanyVintage Pharms; Wockhardt; Excellium; Hospira; Sun Pharm Inds; Sandoz; Roxane; Ivax Sub Teva Pharms; Emcure Pharms; Fresenius Kabi Usa; Ipca Labs; Claris Lifesciences; Luitpold; Mylan

2 of 6  
Drug NameLasix
PubMed HealthFurosemide
Drug ClassesCardiovascular Agent
Drug LabelLASIX is a diuretic which is an anthranilic acid derivative. LASIX tablets for oral administration contain furosemide as the active ingredient and the following inactive ingredients: lactose monohydrate NF, magnesium stearate NF, starch NF, talc US...
Active IngredientFurosemide
Dosage FormTablet
RouteOral
Strength80mg; 40mg; 20mg
Market StatusPrescription
CompanySanofi Aventis Us

3 of 6  
Drug NameUrex
Active IngredientMethenamine hippurate
Dosage FormTablet
RouteOral
Strength1gm
Market StatusPrescription
CompanyCnty Line Pharms

4 of 6  
Drug NameFurosemide
PubMed HealthFurosemide
Drug ClassesCardiovascular Agent
Drug LabelThe CAS Registry Number is 54-31-9.It has a molecular formula of C12H11ClN2O5S and a molecular weight of 330.75.The molecular structure is as follows:...
Active IngredientFurosemide
Dosage FormTablet; Injectable; Solution
RouteInjection; Oral
Strength40mg/5ml; 10mg/ml; 80mg; 40mg; 20mg
Market StatusPrescription
CompanyVintage Pharms; Wockhardt; Excellium; Hospira; Sun Pharm Inds; Sandoz; Roxane; Ivax Sub Teva Pharms; Emcure Pharms; Fresenius Kabi Usa; Ipca Labs; Claris Lifesciences; Luitpold; Mylan

5 of 6  
Drug NameLasix
PubMed HealthFurosemide
Drug ClassesCardiovascular Agent
Drug LabelLASIX is a diuretic which is an anthranilic acid derivative. LASIX tablets for oral administration contain furosemide as the active ingredient and the following inactive ingredients: lactose monohydrate NF, magnesium stearate NF, starch NF, talc US...
Active IngredientFurosemide
Dosage FormTablet
RouteOral
Strength80mg; 40mg; 20mg
Market StatusPrescription
CompanySanofi Aventis Us

6 of 6  
Drug NameUrex
Active IngredientMethenamine hippurate
Dosage FormTablet
RouteOral
Strength1gm
Market StatusPrescription
CompanyCnty Line Pharms

4.2 Therapeutic Uses

Diuretics; Sodium Potassium Chloride Symporter Inhibitors

National Library of Medicine's Medical Subject Headings. Furosemide. Online file (MeSH, 2017). Available from, as of April 10, 2017: https://www.nlm.nih.gov/mesh/2017/mesh_browser/MBrowser.html


Oral Lasix may be used in adults for the treatment of hypertension alone or in combination with other antihypertensive agents. Hypertensive patients who cannot be adequately controlled with thiazides will probably also not be adequately controlled with Lasix alone. /Included in US product labeling/

NIH; DailyMed. Current Medication Information for Lasix (Furosemide Tablet) (Updated: April 2016). Available from, as of April 19, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2c9b4d8f-0770-482d-a9e6-9c616a440b1a


Lasix is indicated in adults and pediatric patients for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome. Lasix is particularly useful when an agent with greater diuretic potential is desired. /Included in US product labeling/

NIH; DailyMed. Current Medication Information for Lasix (Furosemide Tablet) (Updated: April 2016). Available from, as of April 19, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2c9b4d8f-0770-482d-a9e6-9c616a440b1a


IV furosemide has been found useful as an adjunct to hypotensive agents in the treatment of hypertensive crises, especially when associated with acute pulmonary edema or renal failure. In addition to producing a rapid diuresis, furosemide enhances the effects of other hypotensive drugs and counteracts the sodium retention caused by some of these agents. /NOT included in US product labeling/

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2828


For more Therapeutic Uses (Complete) data for Furosemide (11 total), please visit the HSDB record page.


4.3 Drug Warning

/BOXED WARNING/ Lasix (furosemide) is a potent diuretic which, if given in excessive amounts, can lead to a profound diuresis with water and electrolyte depletion. Therefore, careful medical supervision is required and dose and dose schedule must be adjusted to the individual patient's needs.

NIH; DailyMed. Current Medication Information for Lasix (Furosemide Tablet) (Updated: April 2016). Available from, as of April 19, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2c9b4d8f-0770-482d-a9e6-9c616a440b1a


Excessive diuresis may cause dehydration and blood volume reduction with circulatory collapse and possibly vascular thrombosis and embolism, particularly in elderly patients. As with any effective diuretic, electrolyte depletion may occur during Lasix therapy, especially in patients receiving higher doses and a restricted salt intake. Hypokalemia may develop with Lasix, especially with brisk diuresis, inadequate oral electrolyte intake, when cirrhosis is present, or during concomitant use of corticosteroids, ACTH, licorice in large amounts, or prolonged use of laxatives. Digitalis therapy may exaggerate metabolic effects of hypokalemia, especially myocardial effects.

NIH; DailyMed. Current Medication Information for Lasix (Furosemide Tablet) (Updated: April 2016). Available from, as of April 19, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2c9b4d8f-0770-482d-a9e6-9c616a440b1a


Patients receiving furosemide must be carefully observed for signs of hypovolemia, hyponatremia, hypokalemia, hypocalcemia, hypochloremia, and hypomagnesemia. Patients should be informed of the signs and symptoms of electrolyte imbalance and instructed to report to their physicians if weakness, dizziness, fatigue, faintness, mental confusion, lassitude, muscle cramps, headache, paresthesia, thirst, anorexia, nausea, and/or vomiting occur. Excessive fluid and electrolyte loss may be minimized by initiating therapy with small doses, careful dosage adjustment, using an intermittent dosage schedule if possible, and monitoring the patient's weight. To prevent hyponatremia and hypochloremia, intake of sodium may be liberalized in most patients; however, patients with cirrhosis usually require at least moderate sodium restriction while on diuretic therapy. Determinations of serum electrolytes, BUN, and carbon dioxide should be performed early in therapy with furosemide and periodically thereafter. If excessive diuresis and/or electrolyte abnormalities occur, the drug should be withdrawn or dosage reduced until homeostasis is restored. Electrolyte abnormalities should be corrected by appropriate measures.

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2830


Furosemide should be used with caution in patients with hepatic cirrhosis because rapid alterations in fluid and electrolyte balance may precipitate hepatic precoma or coma.

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2830


For more Drug Warnings (Complete) data for Furosemide (29 total), please visit the HSDB record page.


4.4 Drug Indication

Furosemide is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome, in adults and pediatric patients. Oral furosemide is indicated alone for the management of mild to moderate hypertension or severe hypertension in combination with other antihypertensive medications. Intravenous furosemide is indicated as adjunctive therapy in acute pulmonary edema when a rapid onset of diuresis is desired.


Treatment of fluid retention


5 Pharmacology and Biochemistry
5.1 Pharmacology

Furosemide manages hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome. Furosemide is a potent loop diuretic that works to increase the excretion of Na+ and water by the kidneys by inhibiting their reabsorption from the proximal and distal tubules, as well as the loop of Henle. It works directly acts on the cells of the nephron and indirectly modifies the content of the renal filtrate. Ultimately, furosemide increases the urine output by the kidney. Protein-bound furosemide is delivered to its site of action in the kidneys and secreted via active secretion by nonspecific organic transporters expressed at the luminal site of action. Following oral administration, the onset of the diuretic effect is about 1 and 1.5 hours, and the peak effect is reached within the first 2 hours. The duration of effect following oral administration is about 4-6 hours but may last up to 8 hours. Following intravenous administration, the onset of effect is within 5 minutes, and the peak effect is reached within 30 minutes. The duration of action following intravenous administration is approximately 2 hours. Following intramuscular administration, the onset of action is somewhat delayed.


5.2 MeSH Pharmacological Classification

Sodium Potassium Chloride Symporter Inhibitors

Agents that inhibit SODIUM-POTASSIUM-CHLORIDE SYMPORTERS which are concentrated in the thick ascending limb at the junction of the LOOP OF HENLE and KIDNEY TUBULES, DISTAL. They act as DIURETICS. Excess use is associated with HYPOKALEMIA and HYPERGLYCEMIA. (See all compounds classified as Sodium Potassium Chloride Symporter Inhibitors.)


Diuretics

Agents that promote the excretion of urine through their effects on kidney function. (See all compounds classified as Diuretics.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
FUROSEMIDE
5.3.2 FDA UNII
7LXU5N7ZO5
5.3.3 Pharmacological Classes
Loop Diuretic [EPC]; Increased Diuresis at Loop of Henle [PE]
5.4 ATC Code

C03CA01

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


C - Cardiovascular system

C03 - Diuretics

C03C - High-ceiling diuretics

C03CA - Sulfonamides, plain

C03CA01 - Furosemide


5.5 Absorption, Distribution and Excretion

Absorption

Following oral administration, furosemide is absorbed from the gastrointestinal tract. It displays variable bioavailability from oral dosage forms, ranging from 10 to 90%. The oral bioavailability of furosemide from oral tablets or oral solution is about 64% and 60%, respectively, of that from an intravenous injection of the drug.


Route of Elimination

The kidneys are responsible for 85% of total furosemide total clearance, where about 43% of the drug undergoes renal excretion. Significantly more furosemide is excreted in urine following the I.V. injection than after the tablet or oral solution. Approximately 50% of the furosemide load is excreted unchanged in urine, and the rest is metabolized into glucuronide in the kidney.


Volume of Distribution

The volume of distribution following intravenous administration of 40 mg furosemide were 0.181 L/kg in healthy subjects and 0.140 L/kg in patients with heart failure.


Clearance

Following intravenous administration of 400 mg furosemide, the plasma clearance was 1.23 mL/kg/min in patients with heart failure and 2.34 mL/kg/min in healthy subjects, respectively.


Significantly more furosemide is excreted in urine following the IV injection than after the tablet or oral solution. There are no significant differences between the two oral formulations in the amount of unchanged drug excreted in urine.

NIH; DailyMed. Current Medication Information for Lasix (Furosemide Tablet) (Updated: April 2016). Available from, as of April 19, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2c9b4d8f-0770-482d-a9e6-9c616a440b1a


After oral administration of furosemide to 18 pregnant women on the day of delivery, substantial concentrations of the drug were detected in umbilical cord vein plasma as well as in amniotic fluid. The ratio between the furosemide concentrations in maternal vein plasma and in umbilical cord plasma increased with time and approximated unity at 8 to 10 hr after administration of the drug. The plasma half-life of furosemide appeared to be longer in the mothers than in nonpregnant healthy volunteers. In one patient the plasma level of furosemide was constant during 5 hr of observation.

PMID:699480 Beermann B et al; Clin Pharmacol Ther 24 (5): 560-2 (1978)


In one study in patients with normal renal function, approx 60% of a single 80 mg oral dose of furosemide was absorbed from the GI tract. When admin to fasting adults in this dosage, the drug appeared in the serum within 10 min, reached a peak concn of 2.3 ug/mL in 60-70 min, & was almost completely cleared from the serum in 4 hr. When the same dose was given after a meal, the serum concn of furosemide increased slowly to a peak of about 1 ug/ml after 2 hr & similar concns were present 4 hr after ingestion. However, a similar diuretic response occurred regardless of whether the drug was given with food or to fasting patients. In another study, the rate & extent of absorption varied considerably when 1 g of furosemide was given orally to uremic patients. An avg of 76% of a dose was absorbed, & peak plasma concns were achieved within 2-9 hr (avg 4.4 hr). Serum concns required to produce max diuresis are not known, & it has been reported that the magnitude of response does not correlate with either the peak or the mean serum concns.

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2831


The diuretic effect of orally administered furosemide is apparent within 30 minutes to 1 hr and is maximal in the first or second hour. The duration of action is usually 6-8 hr. The maximum hypotensive effect may not be apparent until several days after furosemide therapy is begun. After iv administration of furosemide, diuresis occurs within 5 min, reaches a maximum within 20-60 min, and persists for approximately 2 hr. After im administration, peak plasma concentrations are attained within 30 min; onset of diuresis occurs somewhat later than after iv administration. In patients with severely impaired renal function, the diuretic response may be prolonged.

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2831


For more Absorption, Distribution and Excretion (Complete) data for Furosemide (15 total), please visit the HSDB record page.


5.6 Metabolism/Metabolites

The metabolism of furosemide occurs mainly in the kidneys and the liver, to a smaller extent. The kidneys are responsible for about 85% of total furosemide total clearance, where about 40% involves biotransformation. Two major metabolites of furosemide are furosemide glucuronide, which is pharmacologically active, and saluamine (CSA) or 4-chloro-5-sulfamoylanthranilic acid.


It would appear that frusemide glucuronide is the only or at least the major biotransformation metabolite in man. 2-amino-4- chloro-5-sulfamoylanthranilic acid has been reported in some studies but not in others; and is thought to be an analytical artifact.

International Programme on Chemical Safety (IPCS); Poisons Information Monograph (PIM) No. 240, Furosemide (July 1997). Available from, as of April 18, 2017: https://www.inchem.org/pages/pims.html


In patients with normal renal function, a small amount of furosemide is metabolized in the liver to the defurfurylated derivative, 4-chloro-5-sulfamoylanthranilic acid. ...

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2831


5.7 Biological Half-Life

The half-life from the dose of 40 mg furosemide was 4 hours following oral administration and 4.5 hours following intravenous administration. The terminal half-life of furosemide is approximately 2 hours following parenteral administration. The terminal half-life may be increased up to 24 hours in patients with severe renal failure.


To study the pharmacokinetics of furosemide (fursemide; Lasix) and its acyl glucuronide and to analyze the pharmacodynamic response, a study was conducted in 7 healthy subjects, mean age 34 yr, who received a single oral 80 mg dose of furosemide in tablet form. Two half-lives were distinguished in the plasma elimination of furosemide and its conjugate, with values of 1.25 and 30.4 hr for furosemide and 1.31 and 33.2 hr for the conjugate. ...

Vree TB et al; J Pharm Pharmacol (Nov): 964-9 (1995)


In dogs, ... the elimination half life /is/ approximately 1-1.5 hours.

Plumb D.C. Veterinary Drug Handbook. 8th ed. (pocket). Ames, IA: Wiley-Blackwell, 2015., p. 644


Various investigators have reported a wide range of elimination half-lives for furosemide. In one study, the elimination half-life averaged about 30 minutes in healthy patients who received 20-120 mg of the drug IV. In another study, the elimination half-life averaged 9.7 hours in patients with advanced renal failure who received 1 g of furosemide IV. The elimination half-life was more prolonged in 1 patient with concomitant liver disease.

American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda, MD. 2016, p. 2831


The serum half-life in therapeutic doses is 92 minutes; increasing in patients with uremia; congestive heart failure and cirrhosis as well as in the neonate and aged patients. In such patients the half-life may be extended to 20 hours.

International Programme on Chemical Safety (IPCS); Poisons Information Monograph (PIM) No. 240, Furosemide (July 1997). Available from, as of April 18, 2017: https://www.inchem.org/pages/pims.html


5.8 Mechanism of Action

Furosemide promotes diuresis by blocking tubular reabsorption of sodium and chloride in the proximal and distal tubules, as well as in the thick ascending loop of Henle. This diuretic effect is achieved through the competitive inhibition of sodium-potassium-chloride cotransporters (NKCC2) expressed along these tubules in the nephron, preventing the transport of sodium ions from the lumenal side into the basolateral side for reabsorption. This inhibition results in increased excretion of water along with sodium, chloride, magnesium, calcium, hydrogen, and potassium ions. As with other loop diuretics, furosemide decreases the excretion of uric acid. Furosemide exerts direct vasodilatory effects, which results in its therapeutic effectiveness in the treatment of acute pulmonary edema. Vasodilation leads to reduced responsiveness to vasoconstrictors, such as angiotensin II and noradrenaline, and decreased production of endogenous natriuretic hormones with vasoconstricting properties. It also leads to increased production of prostaglandins with vasodilating properties. Furosemide may also open potassium channels in resistance arteries. The main mechanism of action of furosemide is independent of its inhibitory effect on carbonic anhydrase and aldosterone.


Though both in vivo and in vitro studies have demonstrated an anticonvulsant effect of the loop diuretic furosemide, the precise mechanism behind this effect is still debated. The current study investigates the effect of furosemide on Cs-induced epileptiform activity (Cs-FP) evoked in area CA1 of rat hippocampal slices in the presence of Cs(+) (5mM) and ionotropic glutamatergic and GABAergic receptor antagonists. As this model diverges in several respects from other epilepsy models it can offer new insight into the mechanism behind the anticonvulsive effect of furosemide. The present study shows that furosemide suppresses the Cs-FP in a dose-dependent manner with a near complete block at concentrations = 1.25 mM. Because furosemide targets several types of ion transporters we examined the effect of more selective antagonists. Bumetanide (20 uM), which selectively inhibits the Na-K-2Cl co-transporter (NKCC1), had no significant effect on the Cs-FP. VU0240551 (10 uM), a selective antagonist of the K-Cl co-transporter (KCC2), reduced the ictal-like phase by 51.73 +/- 8.5% without affecting the interictal-like phase of the Cs-FP. DIDS (50 uM), a nonselective antagonist of Cl(-)/HCO3(-)-exchangers, Na(+)-HCO3(-)-cotransporters, chloride channels and KCC2, suppressed the ictal-like phase by 60.8 +/- 8.1% without affecting the interictal-like phase. At 500 uM, DIDS completely suppressed the Cs-FP. Based on these results we propose that the anticonvulsant action of furosemide in the Cs(+)-model is exerted through blockade of the neuronal KCC2 and Na(+)-independent Cl(-)/HCO3(-)-exchanger (AE3) leading to stabilization of the activity-induced intracellular acidification in CA1 pyramidal neurons.

PMID:26301821 Uwera J et al; Brain Res 1625: 1-8 (2015)


Sodium chloride reabsorption in the thick ascending limb of the loop of Henle is mediated by the Na(+)-K(+)-2Cl(-) cotransporter (NKCC2). The loop diuretic furosemide is a potent inhibitor of NKCC2. However, less is known about the mechanism regulating the electrolyte transporter. Considering the well-established effects of nitric oxide on NKCC2 activity, cGMP is likely involved in this regulation. cGMP-dependent protein kinase I (cGKI; PKGI) is a cGMP target protein that phosphorylates different substrates after activation through cGMP. We investigated the potential correlation between the cGMP/cGKI pathway and NKCC2 regulation. We treated wild-type (wt) and cGKIa-rescue mice with furosemide. cGKIa-rescue mice expressed cGKIa only under the control of the smooth muscle-specific transgelin (SM22) promoter in a cGKI deficient background. Furosemide treatment increased the urine excretion of sodium and chloride in cGKIa-rescue mice compared to that in wt mice. We analyzed the phosphorylation of NKCC2 by western blotting and immunostaining using the phosphospecific antibody R5. The administration of furosemide significantly increased the phosphorylated NKCC2 signal in wt but not in cGKIa-rescue mice. NKCC2 activation led to its phosphorylation and membrane translocation. To examine whether cGKI was involved in this process, we analyzed vasodilator-stimulated phosphoprotein, which is phosphorylated by cGKI. Furosemide injection resulted in increased vasodilator-stimulated phosphoprotein phosphorylation in wt mice. We hypothesize that furosemide administration activated cGKI, leading to NKCC2 phosphorylation and membrane translocation. This cGKI-mediated pathway could be a mechanism to compensate for the inhibitory effect of furosemide on NKCC2.

PMID:26183401 Limmer F et al; FEBS J 282 (19): 3786-98 (2015)


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04-Jan-2022
30-May-2025
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DOSAGE - TABLET;ORAL - 20MG

USFDA APPLICATION NUMBER - 16273

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DOSAGE - TABLET;ORAL - 40MG

USFDA APPLICATION NUMBER - 16273

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DOSAGE - TABLET;ORAL - 80MG

USFDA APPLICATION NUMBER - 16273

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DOSAGE - INJECTABLE;INJECTION - 10MG/ML **Fed...DOSAGE - INJECTABLE;INJECTION - 10MG/ML **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

USFDA APPLICATION NUMBER - 18579

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ABOUT THIS PAGE

Looking for 54-31-9 / Furosemide API manufacturers, exporters & distributors?

Furosemide manufacturers, exporters & distributors 1

38

PharmaCompass offers a list of Furosemide API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Furosemide manufacturer or Furosemide supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Furosemide manufacturer or Furosemide supplier.

PharmaCompass also assists you with knowing the Furosemide API Price utilized in the formulation of products. Furosemide API Price is not always fixed or binding as the Furosemide Price is obtained through a variety of data sources. The Furosemide Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Furosemide

Synonyms

54-31-9, Frusemide, Lasix, Furosemid, Furanthril, Errolon

Cas Number

54-31-9

Unique Ingredient Identifier (UNII)

7LXU5N7ZO5

About Furosemide

A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.

Hydrex Manufacturers

A Hydrex manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Hydrex, including repackagers and relabelers. The FDA regulates Hydrex manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Hydrex API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Hydrex manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Hydrex Suppliers

A Hydrex supplier is an individual or a company that provides Hydrex active pharmaceutical ingredient (API) or Hydrex finished formulations upon request. The Hydrex suppliers may include Hydrex API manufacturers, exporters, distributors and traders.

click here to find a list of Hydrex suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Hydrex USDMF

A Hydrex DMF (Drug Master File) is a document detailing the whole manufacturing process of Hydrex active pharmaceutical ingredient (API) in detail. Different forms of Hydrex DMFs exist exist since differing nations have different regulations, such as Hydrex USDMF, ASMF (EDMF), JDMF, CDMF, etc.

A Hydrex DMF submitted to regulatory agencies in the US is known as a USDMF. Hydrex USDMF includes data on Hydrex's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Hydrex USDMF is kept confidential to protect the manufacturer’s intellectual property.

click here to find a list of Hydrex suppliers with USDMF on PharmaCompass.

Hydrex JDMF

The Pharmaceuticals and Medical Devices Agency (PMDA) established the Japan Drug Master File (JDMF), also known as the Master File (MF), to permit Japanese and foreign manufacturers of drug substances, intermediates, excipients, raw materials, and packaging materials (‘Products’) to voluntarily register confidential information about the production and management of their products in Japan.

The Hydrex Drug Master File in Japan (Hydrex JDMF) empowers Hydrex API manufacturers to present comprehensive information (e.g., production methods, data, etc.) to the review authority, i.e., PMDA (Pharmaceuticals & Medical Devices Agency).

PMDA reviews the Hydrex JDMF during the approval evaluation for pharmaceutical products. At the time of Hydrex JDMF registration, PMDA checks if the format is accurate, if the necessary items have been included (application), and if data has been attached.

click here to find a list of Hydrex suppliers with JDMF on PharmaCompass.

Hydrex CEP

A Hydrex CEP of the European Pharmacopoeia monograph is often referred to as a Hydrex Certificate of Suitability (COS). The purpose of a Hydrex CEP is to show that the European Pharmacopoeia monograph adequately controls the purity of Hydrex EP produced by a given manufacturer. Suppliers of raw materials can prove the suitability of Hydrex to their clients by showing that a Hydrex CEP has been issued for it. The manufacturer submits a Hydrex CEP (COS) as part of the market authorization procedure, and it takes on the role of a Hydrex CEP holder for the record. Additionally, the data presented in the Hydrex CEP (COS) is managed confidentially and offers a centralized system acknowledged by numerous nations, exactly like the Hydrex DMF.

A Hydrex CEP (COS) is recognised by all 36 nations that make up the European Pharmacopoeia Convention. Hydrex CEPs may be accepted in nations that are not members of the Ph. Eur. at the discretion of the authorities there.

click here to find a list of Hydrex suppliers with CEP (COS) on PharmaCompass.

Hydrex WC

A Hydrex written confirmation (Hydrex WC) is an official document issued by a regulatory agency to a Hydrex manufacturer, verifying that the manufacturing facility of a Hydrex active pharmaceutical ingredient (API) adheres to the Good Manufacturing Practices (GMP) regulations of the importing country. When exporting Hydrex APIs or Hydrex finished pharmaceutical products to another nation, regulatory agencies frequently require a Hydrex WC (written confirmation) as part of the regulatory process.

click here to find a list of Hydrex suppliers with Written Confirmation (WC) on PharmaCompass.

Hydrex NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Hydrex as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Hydrex API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Hydrex as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Hydrex and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Hydrex NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Hydrex suppliers with NDC on PharmaCompass.

Hydrex GMP

Hydrex Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Hydrex GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Hydrex GMP manufacturer or Hydrex GMP API supplier for your needs.

Hydrex CoA

A Hydrex CoA (Certificate of Analysis) is a formal document that attests to Hydrex's compliance with Hydrex specifications and serves as a tool for batch-level quality control.

Hydrex CoA mostly includes findings from lab analyses of a specific batch. For each Hydrex CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Hydrex may be tested according to a variety of international standards, such as European Pharmacopoeia (Hydrex EP), Hydrex JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Hydrex USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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