1484 Contrast Media myelography, see under , p.1483; for specific references, to or to other contrast media, severe , hy- Profile see below. peruricaemia, or cholangitis. Because of its cholinergic action, is a nonionic monomeric iodinated radiographic con- Effects on the nervous system. Reports of serious neurolog- premedication with atropine has been suggested in some coun- trast medium (see p.1474). It may be given intravenously, intra- ical sequelae to lumbar myelography with . tries for patients with coronary heart disease. Iodine-containing arterially, orally, or by instillation into body cavities, and is used contrast media may interfere with -function tests and with in procedures including angiography, arthrography, endoscopic 1. Wallers K, et al. Severe meningeal irritation after intrathecal in- jection of iopamidol. BMJ 1985; 291: 1688. some blood and urine tests. retrograde cholangiopancreatography, hysterosalpingography, urography, and visualisation of the gastrointestinal tract. It is also 2. Robinson C, Fon G. Adverse reaction to iopamidol. Med J Aust Breast feeding. No adverse effects have been observed in 1986; 144: 553. used for contrast enhancement in computed tomography. breast-feeding infants whose mothers were receiving iopanoic 3. Bell JA, McIlwaine GG. Postmyelographic lateral rectus palsy 1 associated with iopamidol. BMJ 1990; 300: 1343–4. acid and the American Academy of Pediatrics considers that it Iopentol is usually available as solutions containing 32.9 to 4. Mallat Z, et al. Aseptic meningoencephalitis after iopamidol my- is therefore usually compatible with breast feeding. 76.8% of iopentol (equivalent to 150 to 350 mg/mL of iodine) elography. Lancet 1991; 338: 252. 1. American Academy of Pediatrics. The transfer of drugs and oth- and the dose and strength used vary according to the procedure 5. Bain PG, et al. Paraplegia after iopamidol myelography. Lancet er chemicals into human milk. Pediatrics 2001; 108: 776–89. and route. 1991; 338: 252–3. Correction. ibid.; 1029. Also available at: 6. Klein KM, et al. Status epilepticus and seizures induced by iopa- http://aappolicy.aappublications.org/cgi/content/full/ Preparations midol myelography. Seizure 2004; 13: 196–9. pediatrics%3b108/3/776 (accessed 27/03/06) Proprietary Preparations (details are given in Part 3) Pharmacokinetics Pharmacokinetics On intravascular use, iopamidol is rapidly eliminated, with up to Austria: Imagopaque; Fr.: Ivepaque; Ger.: Imagopaque; Gr.: Imagopaque; is variably absorbed from the gastrointestinal tract Ital.: Imagopaque; Spain: Imagopaque†; Switz.: Imagopaque†. 50% of the dose recovered unchanged in the urine within 2 and is strongly and extensively bound to plasma proteins. It is hours; the elimination half-life is about 2 hours. It is not signifi- conjugated in the liver to the glucuronide and excreted largely in cantly bound to plasma proteins. the bile and the remainder (about one-third of the dose) in the Uses and Administration urine. It appears in the gallbladder about 4 hours after a dose is Iopodic Acid (BANM, rINNM) Iopamidol is a nonionic monomeric iodinated radiographic con- taken and maximum concentrations occur after about 17 hours. trast medium (see p.1474). It may be given intravenously, intra- About 50% of a dose is excreted in 24 hours, but elevated pro- Acide Iopodique; Ácido iopodico; Acidum Iopodicum; Ipodic arterially, intrathecally, intra-articularly, orally, or rectally and is tein-bound iodine concentrations may persist for several months. Acid. 3-(3-Dimethylaminomethyleneamino-2,4,6-tri-iodophe- used in radiographic procedures including angiography, arthrog- nyl)propionic acid. raphy, myelography, urography, and imaging of the gastrointes- Uses and Administration tinal tract. Iopamidol is also used for contrast enhancement dur- Iopanoic acid is an ionic monomeric iodinated radiographic con- Йоподовая Кислота ing computed tomography. trast medium (p.1474). It has been given orally for cholecystog- C H I N O = 598.0. raphy and cholangiography in usual doses of 3 g, given with 12 13 3 2 2 Iopamidol is usually available as solutions containing 30.62 to plenty of water, about 10 to 14 hours before X-ray examination. CAS — 5587-89-3. 75.5% of iopamidol (equivalent to 150 to 370 mg/mL of iodine) and the dose and strength used vary according to the procedure Iopanoic acid has also been used in the management of hyperthy- ATC — V08AC08; V08AC10. and route. roidism (see below). ATC Vet — QV08AC08; QV08AC10. Preparations Hyperthyroidism. Iopanoic acid and other iodinated oral USP 31: Iopamidol Injection. cholecystographic agents reduce conversion of thyroxine to tri- iodothyronine, as well as inhibiting release of O Proprietary Preparations (details are given in Part 3) 1 Arg.: Hemoray; Iopamiron; Opacrile; Austral.: Isovue; Austria: Gastromi- from the thyroid gland, and they have been used in the manage- ro; Jopamiro; Scanlux; Braz.: Iopamiron; Chile: Radiomiron; Cz.: Gas- ment of hyperthyroidism (p.2165). Iopanoic acid has been used HO I CH tromiro†; Iopamiro†; Scanlux; Denm.: Iopamiro; Fr.: Iopamiron; Ger.: So- successfully for pre-operative preparation in severe hyperthy- 3 lutrast; Unilux; Gr.: Iopamiro; Scanlux; Hung.: Gastromiro†; Iopamiro; roidism,2-4 and for control of hyperthyroidism before radio- N N Scanlux; Irl.: Gastromiro†; Niopam†; Israel: Gastromiro†; Iopamiro; Ital.: 5 CH Gastromiro; Iopamiro; Iopasen; Mex.: Pamiray; Neth.: Gastromiro; Io- iodine treatment. It has a rapid effect but rebound hyperthyroid- 3 pamiro; Scanlux; Norw.: Iopamiro; NZ: Iopamiro; Isovue; Port.: Gastromi- ism may occur and it is not generally suitable for long-term use.1 ro; Iopamiro; Scanlux; Spain: Iopamiro; Swed.: Iopamiro; Switz.: Iopamiro; 1. Braga M, Cooper DS. Oral cholecystographic agents and the thy- I I Scanlux; UK: Gastromiro; Niopam; Scanlux; USA: Isovue; Venez.: Iopami- roid. J Clin Endocrinol Metab 2001; 86: 1853–60. ron. 2. Pandey CK, et al. Rapid preparation of severe uncontrolled thy- rotoxicosis due to Graves’ disease with iopanoic acid—a case report. Can J Anesth 2004; 51: 38–40. Calcium Iopodate (BANM, rINNM) Iopanoic Acid (BAN, rINN) 3. Dhillon KS, et al. Treatment of hyperthyroidism associated with thyrotropin-secreting pituitary adenomas with iopanoic acid. J Calcii Iopodas; Calcium Ipodate; Iopodate Calcique; Iopodato Acide iopanoïque; Ácido iopanoico; _Acidum iopanoicum; Iodo- Clin Endocrinol Metab 2004; 89: 708–11. cálcico; Ipodate Calcium; Kalciumjopodat; Kalsiumjopodaatti. panoic Acid; Jopaanihappo; Jopano rugštis; Jopánsav; Jopansyra; 4. Panzer C, et al. Rapid preoperative preparation for severe hyper- Кальций Йоподат Kyselina jopanoová. 2-(3-Amino-2,4,6-tri-iodobenzyl)butyric ac- thyroid Graves’ disease. J Clin Endocrinol Metab 2004; 89: 2142–4. id. (C12H12I3N2O2)2Ca = 1234.0. 5. Bal CS, et al. Effect of iopanoic acid on radioiodine therapy of Йопаноевая Кислота hyperthyroidism: long-term outcome of a randomized controlled CAS — 1151-11-7. C11H12I3NO2 = 570.9. trial. J Clin Endocrinol Metab 2005; 90: 6536–40. ATC — V08AC10. CAS — 96-83-3. ATC — V08AC06. Preparations ATC Vet — QV08AC10. ATC Vet — QV08AC06. BP 2008: Iopanoic Acid Tablets; Description. Calcium iopodate contains about 61.7% of I. USP 31: Iopanoic Acid Tablets. Proprietary Preparations (details are given in Part 3) (BAN, rINN) NH2 Arg.: Colesom†; Ital.: Cistobil†; Spain: Colegraf; Venez.: Colepak†. Sodium Iopodate Iopodate de Sodium; Iopodato de sodio; (USAN); H3C I I Natrii Iopodas; Natriumjopodaatti; Natriumjopodat; NSC- 106962; Sodium Ipodate. HO Iopentol (BAN, USAN, rINN) Compound 5411; Iopentolum; Jopentol; Jopentoli. N,N′-Bis(2,3- Натрий Йоподат O I dihydroxypropyl)-5-[N-(2-hydroxy-3-methoxypropyl)acetami- C12H12I3N2NaO2 = 619.9. do]-2,4,6-tri-iodoisophthalamide. CAS — 1221-56-3. Description. Iopanoic acid contains about 66.7% of I. Йопентол ATC — V08AC08. Pharmacopoeias. In Chin., Eur. (see p.vii), Int., and US. C20H28I3N3O9 = 835.2. ATC Vet — QV08AC08. Ph. Eur. 6.2 (Iopanoic Acid). A white or yellowish-white pow- CAS — 89797-00-2. der. Practically insoluble in water; soluble in dehydrated alcohol ATC — V08AB08. Description. Sodium iopodate contains about 61.4% of I. and in methyl alcohol; dissolves in dilute solutions of alkali hy- droxides. Protect from light. ATC Vet — QV08AB08. Pharmacopoeias. In US. USP 31 (Iopanoic Acid). A cream-coloured powder, with a faint USP 31 (Ipodate Sodium). A fine, white or off-white, odourless, characteristic odour. Insoluble in water; soluble in alcohol, in crystalline powder. Soluble 1 in less than 1 of water, 1 in 2 of al- chloroform, in ether, and in solutions of alkali hydroxides and OH cohol, 1 in 2 of dimethylacetamide, and 1 in 3.5 of dimethylfor- carbonates. Store in airtight containers. Protect from light. mamide and of dimethyl sulfoxide; very slightly soluble in chlo- roform; freely soluble in methyl alcohol. Store in airtight Adverse Effects HO containers. Gastrointestinal disturbances such as nausea, vomiting, abdomi- nal cramp, and diarrhoea are reported to occur in up to 40% of HN Profile patients but are usually mild and transient. Mild stinging or burn- O I O Iopodic acid is an ionic monomeric iodinated radiographic con- ing on micturition, and skin rashes and flushing have occurred trast medium (see p.1474). It has similar properties to iopanoic occasionally. Acute renal failure, thrombocytopenia, and hyper- H3C acid (p.1484) and has been used orally as the sodium or calcium sensitivity reactions have been reported. HO N I salt for cholecystography and cholangiography. It has also been Iopanoic acid has potent uricosuric and anticholinesterase ef- tried in the management of hyperthyroidism. HO fects. Preparations Precautions O I NH USP 31: Ipodate Sodium Capsules. Iopanoic acid is contra-indicated in severe hepatic or renal dis- H3C O ease; doses higher than 3 g should not be given to patients with OH Proprietary Preparations (details are given in Part 3) renal impairment. It should not be used in the presence of acute Gr.: Biloptin†; UK: Biloptin†; Solu-Biloptin†. gastrointestinal disorders that may impair absorption. It should be used with caution in patients with a history of hypersensitivity Description. Iopentol contains about 45.6% of I. Iopanoic Acid/ 1485

Iopromide (BAN, USAN, rINN) Profile USP 31 (Iothalamic Acid). A white, odourless, powder. Slightly is an iodinated radiographic contrast medium (p.1474) soluble in water and in alcohol; soluble in solutions of alkali hy- Iopromida; Iopromidum; Jopromid; Jopromidi; ZK-35760. N,N′- that has been used with iopydone for bronchography. droxides. Store at a temperature of 25°, excursions permitted be- Bis(2,3-dihydroxypropyl)-2,4,6-tri-iodo-5-(2-methoxyacetami- tween 15° and 30°. do)-N-methylisophthalamide. Йопромид Iopydone (BAN, USAN, rINN) Meglumine Iotalamate (BANM, rINNM) C H I N O = 791.1. 18 24 3 3 8 Iopidona; Iopydonum. 3,5-Di-iodo-4-pyridone. CAS — 73334-07-3. Iotalamate de Méglumine; Iotalamato de meglumina; Iothalamate ATC — V08AB05. Йопидон Meglumine; Meglumine Iothalamate; Meglumini Iotalamas. The N-methylglucamine salt of iotalamic acid. ATC Vet — QV08AB05. C5H3I2NO = 346.9. CAS — 5579-93-1. Меглумина Йоталамат

C11H9I3N2O4,C7H17NO5 = 809.1. OH H CAS — 13087-53-1. N ATC — V08AA04. HO ATC Vet — QV08AA04. HN II I O Description. Meglumine iotalamate contains about 47.1% of I. O O Pharmacopoeias. US includes only as various injections. I CH3 Description. Iopydone contains about 73.2% of I.

H3C N O Profile Sodium Iotalamate (BANM, rINNM) Iopydone is an iodinated radiographic contrast medium (p.1474) I HN that has been used with iopydol for bronchography. Iotalamate de Sodium; Iotalamato de sodico; Iotalamato de so- HO O dio; Iothalamate Sodium; Natrii Iotalamas; Sodium Iothalamate. OH Натрий Йоталамат Iosarcol (pINN) C H I N NaO = 635.9. Description. contains about 48.1% of I. 11 8 3 2 4 Iosarcolum. 3,5-Diacetamido-2,4,6-triiodo-N-methyl-N-{[me- CAS — 17692-74-9; 1225-20-3. Pharmacopoeias. In US. thyl(D-gluco-2,3,4,5,6-pentahydroxyhexyl)carbamoyl]methyl}- USP 31 (Iopromide). A white to slightly yellow powder. Freely benzamide. ATC — V08AA04. soluble in water and in dimethyl sulfoxide; practically insoluble Йозаркол ATC Vet — QV08AA04. in alcohol, in acetone, and in ether. Protect from light. C H I N O = 862.2. 21 29 3 4 9 Description. Sodium iotalamate contains about 59.9% of I. Adverse Effects, Treatment, and Precautions CAS — 97702-82-4. See under the amidotrizoates, p.1475. Pharmacopoeias. US includes only as various injections. Pharmacokinetics OH Adverse Effects, Treatment, and Precautions On intravascular use, iopromide is rapidly distributed in the ex- As for the amidotrizoates, p.1475. tracellular fluid. It is not metabolised and is eliminated HO H HO unchanged in the urine; about 2% of a dose is excreted in faeces. H Incidence of adverse effects. In 40 patients who underwent An elimination half-life of about 2 hours has been reported; CH3 O H OH phlebography with 60% meglumine iotalamate minor adverse about 60% of a dose is excreted in urine within 3 hours and about O N HO H reactions were common despite the use of saline flushing and 92% within 24 hours. Iopromide is not significantly bound to N muscle contraction to clear the veins after examination.1 The plasma proteins. commonest effect was pain at the site of injection, or in the calf I I CH3 Uses and Administration O O and foot; 15 patients of those who had pain in the calf or foot Iopromide is a nonionic monomeric iodinated radiographic con- were found to have venous thrombosis. Major complications of trast medium (see p.1474). It may be given intravenously, intra- phlebography appear to be rare but can cause serious morbidity; H3C N N CH3 examination of 200 case notes and a retrospective study involv- arterially, or by instillation into body cavities, and is used in pro- H H cedures including angiography, arthrography, hysterosalpingog- I ing 3060 patients revealed 4 cases of necrosis in the skin of the raphy, urography, and assessment of dialysis shunt patency. It is foot and gangrene of the foot in 2. also used for contrast enhancement during computed tomogra- Description. Iosarcol contains about 44.2% of I. 1. Thomas ML, MacDonald LM. Complications of ascending phle- phy. bography of the leg. BMJ 1978; ii: 317–18. Iopromide is usually available as solutions containing 31.2 to Profile 76.9% of iopromide (equivalent to 150 to 370 mg/mL of iodine) Iosarcol is an iodinated nonionic monomeric contrast medium Pharmacokinetics and the dose and strength used vary according to the procedure used for a wide range of radiographic imaging procedures. On intravascular use the iotalamates are rapidly distributed; suit- and route. Preparations able concentrations for urography reach the urinary tract within 3 to 8 minutes of a bolus intravenous injection. Protein binding Preparations Proprietary Preparations (details are given in Part 3) is reported to be low. The iotalamates are eliminated by the kid- Austria: Melitrast; Ger.: Melitrast. USP 31: Iopromide Injection. neys. In patients with normal renal function more than 90% of the dose injected is excreted in urine within 24 hours; an elimi- Proprietary Preparations (details are given in Part 3) nation half-life of about 90 minutes has been reported. Small Arg.: Clarograf; Austral.: Ultravist; Austria: Ultravist; Belg.: Ultravist; Ca- Iotalamic Acid (BAN, rINN) amounts are reported to be excreted via the bile in the faeces. The nad.: Ultravist†; Cz.: Ultravist; Denm.: Ultravist; Fin.: Ultravist; Fr.: Ul- iotalamates are removed by peritoneal dialysis and haemodialy- travist; Ger.: Ultravist; Gr.: Ultravist; Hung.: Ultravist; Israel: Ultravist; Ital.: Acide iotalamique; Ácido iotalámico; Acidum iotalamicum; Ioth- Ultravist; Jpn: Proscope; Neth.: Ultravist; Norw.: Ultravist; NZ: Ultravist; sis. Port.: Ultravist; Rus.: Ultravist (Ультравист); S.Afr.: Ultravist; Spain: alamic_ Acid (USAN); Jotalaamihappo; Jotalaminsav; Jotalamo Clarograf; Ultravist; Swed.: Ultravist; Switz.: Ultravist; UK: Ultravist; USA: rugštis; Jotalamsyra; Kyselina jotalamová; Methalamic Acid; MI- Uses and Administration Ultravist. 216. 5-Acetamido-2,4,6-tri-iodo-N-methylisophthalamic acid. Iotalamic acid is an ionic monomeric iodinated radiographic Йоталамовая Кислота contrast medium (p.1474) with actions similar to the amidotri- zoates (p.1477). It may be given intravenously, intra-arterially, or C11H9I3N2O4 = 613.9. by instillation into the bladder or uterus, and is used in proce- Iopydol (BAN, USAN, pINN) CAS — 2276-90-6. dures including angiography, arthrography, cholangiography, Iopidol; Iopydolum; Jopydol; Jopydoli. 1-(2,3-Dihydroxypropyl)- ATC — V08AA04. urography and hysterosalpingography. It is also used for contrast 3,5-di-iodo-4-pyridone. ATC Vet — QV08AA04. enhancement in computed tomography. Iotalamates have also been given orally or rectally for imaging of the gastrointestinal Йопидол tract. C H I NO = 421.0. O 8 9 2 3 Iotalamic acid is usually available as solutions containing up to CAS — 5579-92-0. HO I CH3 66.8% of sodium iotalamate or up to 60% of meglumine iotala- ATC — V08AD02. NH mate. The dose and strength used vary according to the proce- ATC Vet — QV08AD02. dure and route. A mixture of the two salts has been given to min- I imise adverse effects. H C O 3 Preparations I NH I USP 31: Iothalamate Meglumine and Iothalamate Sodium Injection; Iotha- O lamate Meglumine Injection; Iothalamate Sodium Injection. O N OH Description. Iotalamic acid contains about 62% of I. Proprietary Preparations (details are given in Part 3) Pharmacopoeias. In Chin., Eur. (see p.vii), Jpn, and US. Arg.: Conray; Cysto-Conray; Austral.: Conray 280; Canad.: Conray; Cys- I HO to-Conray; Ger.: Conray 30†; Conray 60†; Ital.: Conray†; UK: Conray; Ph. Eur. 6.2 (Iotalamic Acid). A white or almost white powder. USA: Conray; Cysto-Conray. Slightly soluble in water and in alcohol; dissolves in dilute solu- Description. Iopydol contains about 60.3% of I. tions of alkali hydroxides. Protect from light. 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)