3-[3-[[(ジメチルアミノ)メチレン]アミノ]-2,4,6-トリヨードフェニル]プロパン酸

Insoluble

SLIGHTLY SOL IN ETHANOL; METHANOL /CALCIUM SALT/

VERY SOL IN CHLOROFORM /SODIUM SALT/

PRACTICALLY INSOL IN WATER; VERY SOL IN METHANOL, ETHANOL, CHLOROFORM, ACETONE, DILUTE SULFURIC ACID

168-169ºC

168-169 °C

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/

Danger

H318 (100%): Causes serious eye damage [Danger Serious eye damage/eye irritation]

P264+P265, P280, P305+P354+P338, and P317 (click each P-code to see the statement)

Aggregated GHS information provided per 24 reports by companies from 1 notifications to the ECHA C&L Inventory.

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/

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.

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.