Oragrafin

597.95723

597.96

226-992-7

F604ZKI910

DTXSID0023167

CRYSTALS

2925290090

52.90000

3.73900

2.31g/cm3

168-169 °C

579.8ºC at 760mmHg

304.4ºC

1.715

1.81g/L(temperature not stated)

IT SHOULD BE STORED @ ROOM TEMP IN A TIGHTLY CLOSED CONTAINER PROTECTED FROM LIGHT. /CALCIUM & SODIUM SALTS/

4.8None

4.8

DECOMPOSES @ 225 °C; ESTIMATED PK: 5-5.5|CRYSTALS; MP: 298-302 °C; SOL IN CHLOROFORM, DIMETHYLFORMAMIDE, HOT PROPYLENE GLYCOL; IN WATER @ 20 °C 0.1% /CALCIUM SALT/|VERY FREELY SOL IN WATER, METHANOL, ETHANOL; PRACTICALLY INSOL IN ACETONE, ETHER; SOLUBILITY IN DIMETHYLFORMAMIDE & DIMETHYL SULFOXIDE ABOUT 33 G/100 ML; IN DIMETHYLACETAMIDE ABOUT 66 G/100 ML; LEAFLETS FROM WATER + ACETONE; MP: 303-304 °C (DECOMP WITH EVOLUTION OF IODINE); BITTER LEAFLETS /SODIUM SALT/|ODORLESS; CHALKY, VERY BITTER TASTE /CALCIUM SALT/|ODORLESS /SODIUM SALT/|WHITE TO OFF-WHITE, CRYSTALLINE POWDER /CALCIUM & SODIUM SALTS/

IRRITANT

|Danger|H318 (100%): Causes serious eye damage [Danger Serious eye damage/eye irritation]|P280, P305+P351+P338, and P310|Aggregated GHS information provided by 24 companies from 1 notifications to the ECHA C&L Inventory.

Iopodic acid is cathegorized as one of the top 10 linked to skin reactions.

The absence of a substituent at position 5 allows the compound to bind to serum albumin. This is the reason why immediately after absorption, iopanoic acid enters the bloodstream it binds to albumin and it is transported to the liver.

Iopodic acid is available as a cholecystographic agent. This denomination indicates the iopodic acid is a radiopaque substance that can be used to visualize the gallbladder and biliary channels in abdominal X-ray. An abdominal X-ray uses a minimal amount of ionizing radiation to produce pictures of the inside of the abdominal cavity. It is commonly used to evaluate the stomach, liver, intestines, and spleen. Iopodic acid has also been indicated for the treatment of hyperthyroidism such as Graves disease. Hyperthyroidism refers to any condition where there is too much thyroid hormone produced in the body (overactive thyroid). When the overactivity involves the entire thyroid gland, it is known as Grave's disease.

Contrast Media|...ADMIN ORALLY FOR CHOLECYSTOGRAPHY & MAY BE USED FOR CHOLANGIOGRAPHY. /IPODATE CALCIUM & SODIUM/|...ABSORBED FROM GI TRACT & EXCRETED IN BILE IN SUFFICIENT QUANTITY TO OUTLINE BILIARY DUCTS WITHIN 30 MIN AFTER ADMIN; OPTIMAL OPACIFICATION OF DUCTS OCCURS 1-3 HR AFTER INGESTION. MAX VISUALIZATION OF GALL BLADDER OCCURS 10 HR AFTER ADMIN... /IPODATE CALCIUM & SODIUM/|EXPTL USE: IPODATE [ORAGRAFIN]...SUPPRESS THYROID FUNCTION IN EUTHYROID & HYPERTHYROID INDIVIDUALS. IPODATE...HAS BEEN USED TO TREAT HYPERTHYROIDISM... THE USE OF IPODATE & SIMILAR AGENTS IS INVESTIGATIONAL BUT APPEARS PROMISING FOR SHORT-TERM EARLY TREATMENT OF HYPERTHYROIDISM OR AS AN ADJUNCT TO THIOAMIDE DRUGS.

...SHOULD BE USED WITH CAUTION IN PT WITH RENAL OR HEPATIC DISEASE. /IPODATE CALCIUM/|...CONTRAINDICATED IN PATIENTS...KNOWN TO BE ALLERGIC TO IODINE. IT ALSO INTERFERES WITH THYROID FUNCTION TESTS BASED ON UPTAKE OF RADIOACTIVE IODINE BY THE GLAND. /IPODATE CALCIUM & SODIUM/|TWO CASES OF HYPERTHYROIDISM FOLLOWING CHOLECYSTOGRAPHY ARE REPORTED. ONE PATIENT RECEIVED 3 G OF SODIUM IPODATE (1800 MG IODINE); THE OTHER ONE RECEIVED 6 G OF SODIUM IPODATE.|IOPANOIC ACID ADMINISTRATION RESULTS IN INCREASED BSP /SULFOBROMOPHTHALEIN/ RETENTION, PROBABLY BY COMPETING WITH BSP FOR CONCENTRATION & EXCRETION BY THE LIVER. OTHER CHOLECYSTOGRAPHIC MEDIA SUCH AS SODIUM IPIDATE...HAVE SIMILAR EFFECTS. HOWEVER, SOME FEEL THAT THIS INTERFERENCE WITH BSP EXCRETION WOULD SELDOM CAUSE DIAGNOSTIC CONFUSION.

The thyroid effects of iopodic acid are related to the blocking of the more potent form of the thyroid hormone. It also blocks thyroid hormone release and it can interfere with its synthesis in some patients. The effects of iopopdic acid on some diseases, such as Graves disease, have been shown not to be as effective and to present a relapse after discontinuation. The effects of iopodic acid on thyroid has been proven to produce an inactivation of approximately 80% of the type II deiodinase in pituitary and cerebral cortex.

Substances used to allow enhanced visualization of tissues. (See all compounds classified as Contrast Media.)

The lipophilicity of ipodate is sufficient for passage through the gastrointestinal mucosa. After ingestion, iopodic acid is promptly absorbed by passive diffusion in the small intestinal mucosa. The presence of bile salts in the duodenum is essential for its diffusion through the intestine wall and a high-fat diet is important in order to increase the absorption effectivity. The maximum effect is showed to be attained 5 hours after the initial dosage and the effect were retained for more than 60 hours.|The metabolism products of ipodate are readily excreted into the bile, follow the bile flow to fill up the gallbladder and then excreted by the biliary system in the feces. This mode of excretion accounts for 65% of the eliminated dose whereas the kidneys are responsible for the remaining 35% of the elimination.|...RAPIDLY ABSORBED FROM GI TRACT & EXCRETED IN BILE... /IPODATE CALCIUM/|...SOMEWHAT LESS RAPIDLY ABSORBED FROM GI TRACT.../WHEN COMPARED WITH IPODATE CALCIUM/. /IPODATE SODIUM/

The absence of a substituent at position 5 facilitates for preferential hepatocyte uptake. Once taken in the liver, the metabolism is mainly performed by glucuronide conjugation in the same pathway as bilirubin.

For cholecystography, iopodic acid blocks the X-rays as they pass through the body which allows delineating the body structures that do not contain this compound. The use of iopodic acid in hyperthyroidism is related to the inhibition of 5'-monodeiodinase type I and II; this will later impair the extrathyroidal conversion of thyroxine (T4) to triiodothyronine (T3).|IPODATE /ORAGRAFIN/...GIVEN ONCE DAILY CAUSES RAPID DECLINE IN SERUM T3 & T4, INCREASES RT3, & APPEARS TO BE MORE POTENT THAN PTU IN INHIBITING EXTRATHYROIDAL CONVERSION OF T4 TO T3. ANOTHER MECHANISM PROBABLY INVOLVES THE SLOWER INHIBITION OF THYROID HORMONE SECRETION CAUSED BY RELEASE OF IODINE AFTER METABOLISM OF IPODATE. THE USE OF IPODATE & SIMILAR AGENTS IS INVESTIGATIONAL BUT APPEARS PROMISING FOR SHORT-TERM EARLY TREATMENT OF HYPERTHYROIDISM OR AS AN ADJUNCT TO THIOAMIDE DRUGS. /IPODATE SALTS/|THE INGESTION BY NORMAL SUBJECTS OF 3 G OF SODIUM IPODATE RESULTED IN DECREASES OF SERUM TOTAL & FREE T3 TO A NADIR ON DAY 4 WHICH AVERAGED 43% & 40%, RESPECTIVELY, BELOW INITIAL MEAN VALUES. TOTAL & FREE RT3 INCREASED MARKEDLY TO PEAK ON DAY 3, 244% & 189%, RESPECTIVELY, ABOVE INITAL MEAN VALUES. CHANGES OBSERVED AFTER ADMINISTRATION OF IPODATE WERE CONSISTENT WITH AN EFFECT ON THE PERIPHERAL METABOLISM OF T4.|IPODATE INHIBITED BINDING OF (125)I-LABELED T3 IN VITRO. IT PRODUCED A 50% INHIBITION OF BINDING AT 1.2X10-4 MOLAR. WHEN GIVEN ORALLY IN ACTIVE IN VIVO EXPERIMENTS, IPODATE DID NOT DIMINISH BINDING TO LIVER NUCLEAR RECEPTORS, BUT APPEARED TO INHIBIT IN VIVO METABOLISM OF LABELED T3.|IPODATE IS AN EFFECTIVE, COMPETITIVE IN VITRO INHIBITOR OF (125)I-LABELED T3 BINDING TO RAT HEPATIC NUCLEI RECEPTORS. T3 RECEPTOR BINDING INHIBITION ALSO OCCURRED WHEN IPODATE WAS GIVEN IV TO RATS.|3,3'-DIIODOTHYRONINE (3,3'-T2) SECRETION FROM PERFUSED CANINE THYROID ISOLATED IN SITU, WAS INHIBITED BY IPODATE (10-5 MOLES).

ONSET OF ACUTE IODIDE POISONING MAY OCCUR IMMEDIATELY OR SEVERAL HR AFTER ADMIN. ANGIOEDEMA IS OUTSTANDING SYMPTOM, & SWELLING OF LARYNX MAY LEAD TO SUFFOCATION. MULTIPLE CUTANEOUS HEMORRHAGES MAY BE PRESENT. ALSO MANIFESTATIONS OF SERUM-SICKNESS TYPE HYPERSENSITIVITY, SUCH AS FEVER, ARTHRALGIA, LYMPH NODE ENLARGEMENT, & EOSINOPHILIA, MAY APPEAR. THROMBOTIC THROMBOCYTOPENIC PURPURA & FATAL PERIARTERITIS NODOSA ATTRIBUTED TO HYPERSENSITIVITY TO IODIDE HAS BEEN DESCRIBED. /IODINE PREPN/|MEDIA USED FOR GI ROENTGENOGRAPHY & AGENTS ADMIN ORALLY MAY CAUSE NAUSEA, VOMITING, & DIARRHEA. ACUTE TUBULAR NECROSIS HAS BEEN REPORTED TO BE THE CONSEQUENCE OF INGESTION OF CERTAIN GALLBLADDER DYES. /IODINATED CONTRAST MEDIA/|THE WATER-SOLUBLE COMPOUNDS ARE RESPONSIBLE FOR 2 TYPES OF SEVERE REACTIONS: (1) INFREQUENTLY...SEVERE RESPIRATORY DIFFICULTY WITH WHEEZING, BRONCHIAL & LARYNGEAL SPASM, SWELLING OF LIPS & EYELIDS, & GIANT URTICARIA. ... (2) SOMEWHAT MORE FREQUENT IS...CARDIOVASCULAR COLLAPSE IN WHICH THERE IS FALL IN BLOOD PRESSURE, TACHYCARDIA, DYSPNEA, & CONFUSION & CYANOSIS PROGRESSING TO UNCONSCIOUSNESS. /WATER-SOLUBLE IODINATED CONTRAST MEDIA/|UNTOWARD EFFECTS REPORTED INCL ABDOMINAL CRAMPING, DIARRHEA, NAUSEA, VOMITING, DYSURIA, URTICARIA, HEADACHE, HEARTBURN, & EPIGASTRIC PAIN. ALTHOUGH RARE, HYPOTENSION & CIRCULATORY COLLAPSE HAVE BEEN REPORTED. /IPODATE CALCIUM & SODIUM/

3-(3-(Dimethylaminomethylideneamino)-2,4,6-triiodophenyl)propanoic acid

SODIUM IPODATE, BILOPTIN, ORAGRAFIN-SODIUM. /SODIUM IPODATE/; CALCIUM IPODATE, SOLUBILOPTIN, ORAGRAFIN-CALCIUM. /CALCIUM IPODATE/.|/IPODATE CALCIUM/...CONTAINS 61.7% IODINE... /IPODATE SODIUM/...CONTAINS 61.4% IODINE... /IPODATE CALCIUM & SODIUM/

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients