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Home , Iotroxic acid, Ioxilan, Ioxitalamic acid, Mangafodipir, Metrizamide

1486 Contrast Media

Iotrolan (BAN, USAN, rINN) Description. iotroxate contains about 47.4% of I. (BAN, USAN, rINN) Iotrol; Iotrolán; Iotrolane; Iotrolanum; Iotrolum; Jotrolaani; Jotro- Adverse Effects, Treatment, and Precautions Acide ioxaglique; Ácido_ ioxáglico; Acidum ioxaglicum; Joksagliini- lan; ZK-39482. N,N′,N′′,N′′′-Tetrakis(2,3-dihydroxy-1-hydroxy- See under the amidotrizoates, p.1475. happo; Joksagliko rugštis; Joxaglinsav; Joxaglinsyra; Kyselina joxa- methylpropyl)-2,2′,4,4′,6,6′-hexaiodo-5,5′-(N,N′-dimethylmalo- glová; P-286. N-(2-Hydroxyethyl)-2,4,6-tri-iodo-5-[2′,4′,6′-tri- nyldi-imino)di-isophthalamide. iodo-3′-(N-methylacetamido)-5′-methylcarbamoylhippuramido]- After intravenous injection, binds to plasma pro- isophthalamic acid. Йотролан teins and is taken up by the liver; plasma-protein binding is about Йоксагловая Кислота C37H48I6N6O18 = 1626.2. 60 to 90%. It is excreted primarily unchanged in the bile; a small CAS — 79770-24-4. amount is metabolised and excreted in the urine. C24H21I6N5O8 = 1268.9. ATC — V08AB06. CAS — 59017-64-0. ATC Vet — QV08AB06. Uses and Administration ATC — V08AB03. Iotroxic acid is an ionic dimeric iodinated radiographic contrast ATC Vet — QV08AB03. medium (see p.1474); it is taken up by the liver and excreted in OH OH bile, and is used in cholecystography and cholangiography. IO OH OH OH Iotroxic acid is given intravenously as a solution containing HO 10.5% of the meglumine salt. The usual dose is 10.5 g of meglu- HO N O HN OH HN mine iotroxate (equivalent to about 5 g of ), given by infu- H I O I O sion over at least 15 minutes. Alternatively, a solution containing CH3 III O HN OH O HC 22.8% of meglumine iotroxate may be used. HN I N I Preparations N O NH HO H Proprietary Preparations (details are given in Part 3) O HO IIN O NH I I OH HC O O Austral.: Biliscopin; Austria: Biliscopin; Ger.: Biliscopin; Gr.: Biliscopin; NZ: Biliscopin; Spain: Bilisegrol†; Swed.: Biliscopin†; Switz.: Biliscopin; UK: Bi- N CH OH 3 liscopin. H3C OH O

Description. contains about 46.8% of I. Description. Ioxaglic acid contains about 60% of I. (BAN, USAN, rINN) Pharmacopoeias. In Eur. (see p.vii). Pharmacopoeias. In Eur. (see p.vii) and US. Ph. Eur. 6.2 (Iotrolan). A white or yellowish-white, hygroscopic Ioversolum; Joversol; Joversoli; MP-328. N,N′-Bis(2,3-dihydroxy- Ph. Eur. 6.2 (Ioxaglic Acid). A white or almost white hygroscop- powder. Very soluble in water; practically insoluble in alcohol; propyl)-5-[N-(2-hydroxyethyl)glycolamido]-2,4,6-tri-iodoisoph- ic powder. Very slightly soluble in water and in dichloromethane; freely soluble in dimethyl sulfoxide. Store in airtight containers. thalamide. slightly soluble in alcohol. It dissolves in dilute solutions of alkali Protect from light. hydroxides. Store in airtight containers. Protect from light. Йоверсол Adverse Effects, Treatment, and Precautions USP 31 (Ioxaglic Acid). Store at a temperature of 25°, excursions As for the amidotrizoates, p.1475. For the adverse effects relat- C18H24I3N3O9 = 807.1. permitted between 15° and 30°. ing to the use of nonionic contrast media such as iotrolan for my- CAS — 87771-40-2. elography, see under , p.1483. ATC — V08AB07. Meglumine Ioxaglate (BANM, rINNM) Pharmacokinetics ATC Vet — QV08AB07. Ioxaglate de Méglumine; Ioxaglate Meglumine (USAN); Ioxaglato Iotrolan is excreted unchanged in the urine. After intrathecal in- de meglumina; Meglumini Ioxaglas; MP-302 (meglumine jection, about 80% is excreted in the urine within 24 hours. ioxaglate with sodium ioxaglate). The N-methylglucamine salt of Uses and Administration OH ioxaglic acid. Iotrolan is a nonionic dimeric iodinated radiographic contrast Меглумина Йоксаглат medium (p.1474). It is given intrathecally for and C24H21I6N5O8,C7H17NO5 = 1464.1. for contrast enhancement in computed tomography, and by in- HO CAS — 59018-13-2. stillation into body ducts or cavities for procedures including HN ATC — V08AB03. lymphography, arthrography, hysterosalpingography, cholangio- ATC Vet — QV08AB03. I O pancreatography, and for visualisation of the mammary ducts. It Description. Meglumine ioxaglate contains about 52% of I. may also be given orally for imaging of the gastrointestinal tract. Iotrolan is usually available as solutions containing 51.3% or HO N I Sodium Ioxaglate (BANM, rINNM) 64.1% of iotrolan (equivalent to 240 or 300 mg/mL of iodine, Ioxaglate de Sodium; Ioxaglate Sodium (USAN); Ioxaglato sódico; respectively) and the dose and strength used vary according to O HO the procedure and route. MP-302 (sodium ioxaglate with meglumine ioxaglate); Natrii I NH Ioxaglas; Natriumjoksaglaatti; Natriumjoxaglat. Preparations HO O Натрий Йоксаглат Proprietary Preparations (details are given in Part 3) OH C24H20I6N5NaO8 = 1290.9. Austral.: Isovist†; Austria: Isovist; Canad.: Osmovist†; Cz.: Isovist†; CAS — 67992-58-9. Denm.: Isovist; Fin.: Isovist†; Ger.: Isovist; Hung.: Isovist; Neth.: Isovist; NZ: Isovist; S.Afr.: Isovist; Switz.: Isovist; UK: Isovist. ATC — V08AB03. Description. Ioversol contains about 47.2% of I. ATC Vet — QV08AB03. Pharmacopoeias. In US. Description. Sodium ioxaglate contains about 59% of I. USP 31 (Ioversol). Store at a temperature of 25°, excursions per- Iotroxic Acid (BAN, USAN, rINN) Adverse Effects, Treatment, and Precautions mitted between 15° and 30°. See under the amidotrizoates, p.1475. Acide Iotroxique; Ácido iotróxico; Acidum Iotroxicum; Jotroksi- happo; Jotroxsyra; SH-213AB. 3,3′-(3,6,9-Trioxaundecanedioyl- Adverse Effects, Treatment, and Precautions Pharmacokinetics di-imino)bis(2,4,6-tri-iodobenzoic acid). See under the amidotrizoates, p.1475. On intravascular use, ioxaglates are rapidly distributed through- out the extracellular fluid. Protein binding is reported to be very Йотроксовая Кислота Pharmacokinetics low. They are mainly excreted unchanged in the urine, although C22H18I6N2O9 = 1215.8. When given intravascularly, ioversol is rapidly eliminated biliary may predominate in renal impairment. With CAS — 51022-74-3. unchanged in the urine, with a half-life of about 1.5 hours; more normal renal function, about 90% of a dose is excreted in the ATC — V08AC02. than 95% of a dose is eliminated within 24 hours. Binding to urine within 24 hours; an elimination half-life of about 90 min- ATC Vet — QV08AC02. plasma or serum proteins is very low. utes has been reported. Ioxaglates cross the placenta and are dis- Uses and Administration tributed into breast milk. They are removed by haemodialysis and peritoneal dialysis. O Ioversol is a nonionic monomeric iodinated radiographic con- HO I O I trast medium (p.1474) that is given intra-arterially or intrave- Uses and Administration O nously for angiography and urography. It is also used for contrast Ioxaglic acid is an ionic dimeric iodinated radiographic contrast I NH O I enhancement during computed tomography. It is usually availa- medium (p.1474). It is given intravenously, intra-arterially, intra- O O OH ble as a solution containing 34 to 74% of ioversol (equivalent to articularly, or by instillation into body ducts and cavities and is I NH I 160 to 350 mg/mL of iodine). The dose and strength used vary used in diagnostic procedures including angiography, arthrogra- O according to the procedure and route. phy, hysterosalpingography, and urography. It is also used for contrast enhancement during computed tomography. ◊ References. Description. Iotroxic acid contains about 62.6% of I. Ioxaglic acid is usually available as solutions containing a mix- 1. Floriani I, et al. Clinical profile of ioversol: a metaanalysis of 57 ture of the sodium and meglumine salts. Commonly used solu- Pharmacopoeias. In Int. and Jpn. randomized, double-blind clinical trials. Invest Radiol 1996; 31: tions contain 39.3% of meglumine ioxaglate and 19.6% of sodi- 479–91. um ioxaglate (equivalent to 320 mg/mL of iodine) or 24.6% of Meglumine Iotroxate (BANM, rINNM) Preparations meglumine ioxaglate and 12.3% of sodium ioxaglate (equivalent to 200 mg/mL of iodine). The dose and strength used depend Dimeglumine Iotroxate; Iotroxate de Méglumine; Iotroxate Meg- USP 31: Ioversol Injection. lumine; Iotroxato de meglumina; Meglumine Iotroxinate; Meglu- upon the procedure and route. mini Iotroxas. The di(N-methylglucamine)salt of iotroxic acid. Proprietary Preparations (details are given in Part 3) Preparations Arg.: Optiray; Austral.: Optiray; Austria: Optiray; Belg.: Optiject; Optiray; Меглумина Йотроксат Canad.: Optiray; Cz.: Optiray; Denm.: Optiray; Fin.: Optiray; Fr.: Opti- USP 31: Ioxaglate Meglumine and Ioxaglate Sodium Injection. C22H18I6N2O9,2C7H17NO5 = 1606.2. ject; Optiray; Ger.: Optiray†; Gr.: Optiray; Hung.: Optiray; Israel: Optiray; Proprietary Preparations (details are given in Part 3) CAS — 68890-05-1. Ital.: Optiray; Neth.: Optiray; Norw.: Optiray; Port.: Optiray; Spain: Arg.: Hexabrix; Austral.: Hexabrix; Austria: Hexabrix; Belg.: Hexabrix; Optiray; Swed.: Optiray; Switz.: Optiray; UK: Optiray; USA: Optiray. Braz.: Hexabrix†; Canad.: Hexabrix; Chile: Hexabrix; Cz.: Hexabrix; ATC — V08AC02. Denm.: Hexabrix; Fin.: Hexabrix; Fr.: Hexabrix; Ger.: Hexabrix; Gr.: ATC Vet — QV08AC02. Hexabrix; Hung.: Hexabrix; Israel: Hexabrix; Ital.: Hexabrix; Neth.: Iotrolan/ 1487

Hexabrix; Norw.: Hexabrix; NZ: Hexabrix; Port.: Hexabrix; Spain: Sodium Ioxitalamate (rINNM) Pharmacokinetics Hexabrix; Swed.: Hexabrix; Switz.: Hexabrix; UK: Hexabrix; USA: Ioxitalamate de Sodium; Ioxitalamate Sodium; Ioxitalamato sódi- After intravenous injection, is dephosphorylated Hexabrix; Venez.: Hexabrix. and manganese is exchanged for zinc leading to the release of co; Natrii Ioxitalamas. free manganese ions and the formation of 2 inactive metabolites. Натрий Йокситаламат Manganese is rapidly taken up by the liver, pancreas, kidney and (USAN, rINN) C12H10I3N2NaO5 = 665.9. spleen; about 15 to 20% is excreted in the urine within 24 hours, Ioxilán; Ioxilane; Ioxilanum. N-(2,3-Dihydroxypropyl)-5-[N-(2,3- CAS — 33954-26-6. with most of the remainder excreted in the faeces over about 4 dihydroxypropyl)acetamido]-N′-(2-hydroxyethyl)-2,4,6-triidoiso- ATC — V08AA05. days. The metabolites are almost entirely excreted in the urine phthalamide. ATC Vet — QV08AA05. within 24 hours. Йоксилан Description. Sodium ioxitalamate contains about 57.2% of I. Uses and Administration C18H24I3N3O8 = 791.1. Profile Mangafodipir is a manganese chelate that is used as a magnetic CAS — 107793-72-6. is an ionic monomeric iodinated radiographic resonance contrast medium (p.1474) for imaging of the liver and ATC — V08AB12. contrast medium (p.1474) with actions similar to those of the pancreas. Manganese has paramagnetic properties that increase ATC Vet — QV08AB12. amidotrizoates (p.1475). It is given intravenously or by instilla- the relaxivity of hydrogen ions, leading to signal enhancement. tion into body cavities for procedures including angiography, Free manganese is released from mangafodipir in the body and cholangiography, cystography, hysterosalpingography, and is taken up by normal liver and pancreatic tissue, increasing the OH degree of contrast. H urography; it may be given orally or rectally for imaging of the O N OH gastrointestinal tract. It is also used for contrast enhancement in Mangafodipir is given intravenously as the trisodium salt. computed tomography. Ioxitalamic acid is usually available as a solution containing 21% In the UK, a solution containing mangafodipir trisodium II of the sodium salt (equivalent to 120 mg/mL of iodine), 55.1 to 7.57 mg/mL (10 micromol/mL) is used. Usual doses for imaging are: H 66% of the meglumine salt (equivalent to 250 to 300 mg/mL of N iodine), or as a mixture of both salts. The dose and strength used • liver: 0.5 mL/kg (5 micromol/kg) given by intravenous infu- HO N OH vary according to the procedure and route. sion at a rate of 2 to 3 mL/minute Monoethanolamine ioxitalamate has also been used. OH I O • pancreas: 0.5 mL/kg (5 micromol/kg) given by intravenous O CH3 Preparations infusion at a rate of 4 to 6 mL/minute Proprietary Preparations (details are given in Part 3) In the USA, a more concentrated preparation is used, containing Description. Ioxilan contains about 48.1% of I. Arg.: Telebrix 30; Telebrix 38; Telebrix Coronario; Telebrix Hystero; Belg.: mangafodipir trisodium 37.9 mg/mL (50 micromol/mL). Usual Telebrix; Telebrix Gastro; Telebrix Hystero; Braz.: Telebrix†; Canad.: Te l - doses are: Pharmacopoeias. In US. ebrix; Chile: Telebrix 30; Telebrix 35; Cz.: Telebrix 30; Telebrix 35; Telebrix USP 31 (Ioxilan). A white to off-white, practically odourless, Gastro; Fr.: Telebrix 12; Telebrix 30; Telebrix 35; Telebrix Gastro; Telebrix • liver: 0.1 mL/kg (5 micromol/kg), given by slow intravenous powder. Soluble in water and in methyl alcohol. pH of a 10% so- Hystero; Ger.: Telebrix Gastro; Telebrix N 180 and 300; Gr.: Telebrix Gas- injection to a maximum dose of 15 mL tro; Telebrix Hystero†; Hung.: Telebrix; Telebrix Gastro; Israel: Telebrix; lution in water is between 5.0 and 7.5. Store at a temperature of Te l e b r ix G as t r o ; Mex.: Te l e b r ix ; Neth.: Telebrix 12; Telebrix 30; Telebrix 25°, excursions permitted between 15° and 30°. Protect from 35; Telebrix Gastro; Telebrix Hystero; Port.: Telebrix 12; Telebrix 30; Tele- Preparations light. brix 35; Telebrix Gastro; Telebrix Hystero; Switz.: Telebrix 12; Telebrix 30; USP 31: Mangafodipir Trisodium Injection. Telebrix 35; Telebrix Gastro; Telebrix Hystero; Venez.: Telebrix 30; Telebrix Adverse Effects, Treatment, and Precautions 35; Telebrix Hystero. Proprietary Preparations (details are given in Part 3) See under the amidotrizoates, p.1475. Austria: Teslascan; Belg.: Teslascan; Cz.: Teslascan; Denm.: Teslascan†; Pharmacokinetics Fin.: Teslascan†; Fr.: Tesl a sca n; Ger.: Teslascan; Gr.: Teslascan; Hung.: Te s la s ca n ; Ital.: Teslascan; Neth.: Teslascan; Norw.: Teslascan; NZ: Te sl a s- After intravascular use, ioxilan is rapidly eliminated unchanged Mangafodipir Trisodium (BANM, USAN, rINNM) can; Port.: Teslascan; Spain: Teslascan; Swed.: Teslascan; Switz.: Teslascan; in the urine; about 94% of a dose is excreted within 24 hours. UK: Teslascan; USA: Teslascan. Protein binding is reported to be very low. Ioxilan is dialysable. Mangafodipir trisódico; Mangafodipir Trisodique; Mangafo- dipirum Trinatricum; MnDPDP (mangafodipir); S-095 (mangafo- Uses and Administration dipir); Win-59010; Win-59010-2 (mangafodipir). Trisodium tri- Ioxilan is a nonionic monomeric iodinated radiographic contrast hydrogen (OC-6-13)-{[N,N′-ethylenebis(N-{[3-hydroxy-5-(hy- Metrizamide (BAN, USAN, rINN) medium (see p.1474). It is given intra-arterially or intravenously droxymethyl)-2-methyl-4-pyridyl]methyl}glycine) 5,5′-bis(phos- for procedures including angiography and urography; it is also phato)](8-)} manganate(6-); Trisodium trihydrogen (OC-6-13)- Metritsamidi; Metrizamid; Metrizamida; Métrizamide; Metrizami- used for contrast enhancement during computed tomography. N,N′-ethane-1,2-diylbis{N-[2-methyl-3-oxido-κO-5-(phospho- dum; Win-39103. 2-[3-Acetamido-2,4,6-tri-iodo-5-(N-methyla- Ioxilan is usually available as solutions containing 62.3 or 72.7% cetamido)benzamido]-2-deoxy-D-glucose. of ioxilan (equivalent to 300 or 350 mg/mL of iodine). The dose natooxymethyl)-4-pyridylmethyl]glycinato(O,N)}manganate(II). and strength used vary according to the procedure and route. Тринатрий Мангафодипир Метризамид Preparations C22H27MnN4Na3O14P2 = 757.3. C H I N O = 789.1. CAS — 155319-91-8 (mangafodipir); 140678-14-4 18 22 3 3 8 USP 31: Ioxilan Injection. (mangafodipir trisodium). CAS — 31112-62-6 (metrizamide); 55134-11-7 (metri- Proprietary Preparations (details are given in Part 3) ATC — V08CA05. zamide, glucopyranose form). Jpn: Imagenil; USA: Oxilan. ATC Vet — QV08CA05. ATC — V08AB01. ATC Vet — QV08AB01.

Ioxitalamic Acid (rINN) O Acide Ioxitalamique; Ácido ioxitalámico; Acidum Ioxitalamicum; HO O O O AG-58107; Ioxithalamic Acid; Joksitalaamihappo; Joxitalamsyra. O O 5-Acetamido-N-(2-hydroxyethyl)-2,4,6-tri-iodoisophthalamic P P O O O acid. O N N O 6H OH Йокситаламовая Кислота Mn O O C12H11I3N2O5 = 643.9. OH OH CAS — 28179-44-4. N O N O NH ATC — V08AA05. CH O HC ATC Vet — QV08AA05. (mangafodipir) II OHO O O Pharmacopoeias. In US. USP 31 (Mangafodipir Trisodium). Pale yellow crystals or crys- I I talline powder. Freely soluble in water; very slightly soluble in H3C N N CH3 O alcohol and in acetone; slightly soluble in chloroform; sparingly H CH3 I H soluble in methyl alcohol. pH of a 1% solution in water is be- N tween 5.5 and 7.0. Store at a temperature not exceeding 8°. H3C N OH H Adverse Effects and Precautions Description. Metrizamide contains about 48.2% of I. I O The most common adverse effects of mangafodipir are injection Profile site discomfort, feelings of warmth or flushing, headache, nau- Metrizamide is a nonionic monomeric iodinated radiographic Description. Ioxitalamic acid contains about 59.1% of I. sea, vomiting, abdominal pain, and taste disturbances. Hypersen- contrast medium (p.1474) that has been used in myelography, Pharmacopoeias. In Fr. sitivity reactions, including anaphylactoid reactions, may occur. angiography, intravenous urography, and arthrography, and also Transient increases in bilirubin and liver transaminase concentra- for contrast enhancement during computed tomography. Meglumine Ioxitalamate (rINNM) tions and decreases in plasma-zinc concentrations have been re- ported. Breast feeding. No adverse effects have been seen in breast- Ioxitalamate de Méglumine; Ioxitalamate Meglumine; Ioxitalama- Mangafodipir should be used with caution in patients with hepat- feeding infants whose mothers were receiving metrizamide and to de meglumina; Meglumini Ioxitalamas. The N-methylglu- 1 ic or renal impairment and should be avoided if impairment is the American Academy of Pediatrics considers that it is there- camine salt of ioxitalamic acid. severe. It should not be given to patients with phaeochromocyto- fore usually compatible with breast feeding. Меглумина Йокситаламат ma. 1. American Academy of Pediatrics. The transfer of drugs and oth- C12H11I3N2O5,C7H17NO5 = 839.2. er chemicals into human milk. Pediatrics 2001; 108: 776–89. CAS — 29288-99-1. ◊ References. Correction. ibid.; 1029. Also available at: ATC — V08AA05. 1. Federle MP, et al. Safety and efficacy of mangafodipir trisodium http://aappolicy.aappublications.org/cgi/content/full/ ATC Vet — QV08AA05. (MnDPDP) injection for hepatic MRI in adults: results of the pediatrics%3b108/3/776 (accessed 27/03/06) U.S. multicenter phase III clinical trials (safety). J Magn Reson Description. Meglumine ioxitalamate contains about 45.4% of I. Imaging 2000; 12: 186–97. The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii)