Name | 5-(N-dhp-acetamido)-2,4,6-triiodo-N,N'-B is-dhp-isophthalami |
Synonyms | Iohexal IOHEXOL Iohexol NYCODENZ histodenz solution 6-triiodo-ydroxypropyl)-4 5-(N-2,3-dihydroxypropylacetamido)-*2,4,6-triiodo 5-(n-dhp-acetamido)-2,4,6-triiodo-n,n'-bis-dhp-isophthalami 5-(N-dhp-acetamido)-2,4,6-triiodo-N,N'-B is-dhp-isophthalami 1,3-benzenedicarboxamide,5-(acetyl(2,3-dihydroxypropyl)amino)-n,n'-bis(2,3-dih 5-(N-2,3-DIHYDROXYPROPYLACETAMIDO)-2,4,6-TRIIODO-N,N'-BIS(2,3-DIHYDROXYPROPYL)ISOPHTHALAMIDE N,N'-BIS(2,3-DIHYDROXYPROPYL)-5-[N-(2,3-DIHYDROXYPROPYL)ACETAMIDO]-2,4,6-TRIIODOISOPHTHALAMIDE 5-(N-2-3-DIHYDROXYPROPYL-ACETMIDO)-2,4,6-TRIIODO-N,N'-BIS-(2,3-DIHYDROXYPROPYL)-ISOPHTHALAMIDE 5-[N-(2,3-Dihydroxypropyl)acetamido]-2,4,6-triiodo-N,N-bis(2,3-dihydroxypropyl)isophthalamide solution 5-[acetyl(2,3-dihydroxypropyl)amino]-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodobenzene-1,3-dicarboxamide |
CAS | 66108-95-0 |
EINECS | 266-164-2 |
InChI | InChI=1/C19H26I3N3O9/c1-8(29)25(4-11(32)7-28)17-15(21)12(18(33)23-2-9(30)5-26)14(20)13(16(17)22)19(34)24-3-10(31)6-27/h9-11,26-28,30-32H,2-7H2,1H3,(H,23,33)(H,24,34) |
InChIKey | NTHXOOBQLCIOLC-UHFFFAOYSA-N |
Molecular Formula | C19H26I3N3O9 |
Molar Mass | 821.14 |
Density | 1.078g/mL±0.002g/mLat 25°C(lit.) |
Melting Point | 254-2560C |
Boling Point | 891.5±65.0 °C(Predicted) |
Flash Point | 493°C |
Solubility | Soluble in water (50 mg/ml), methanol, and DMSO. |
Vapor Presure | 3.95E-34mmHg at 25°C |
Appearance | neat |
Color | White |
Merck | 14,5052 |
BRN | 2406632 |
pKa | 11.35±0.46(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,Room Temperature |
Sensitive | Sensitive to light |
Refractive Index | 1.724 |
MDL | MFCD00077732 |
Physical and Chemical Properties | White or pale gray-white powder, with hygroscopicity. |
Use | Non-ionic X-CT contrast medium |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 1 |
RTECS | CZ2205000 |
HS Code | 2924296000 |
Toxicity | LD50 in male, female rats, mice (g Iodine/kg): 15.0, 12.3, 24.3, 25.1 i.v. (Salvesen) |
Reference Show more | 1. Wu Bin, Li Yang, Li Yang, Xia Zhiyuan, Hu Xiaofei, Wu Yongbo, Li yateng, Wu Bin, He Guanglong, Li Jianjun. A preliminary study on the method of cerebral angiography in cadavers [J]. Chinese Journal of Forensic Medicine, 2020,35(06):567-571. 2. Liu Kunliang, Jin Zhicheng, Hu Xiaolong, Yan Dan, Zhang Yu, Zhu Haidong, Teng Gaojun, Xiong Fei, A biodegradable multipolar sphere for promoting imageable trans-arterial chemoembolization, International Journal of B 3. [IF=4.784] Liu Kunliang et al."A biodegradable multifunctional porous microsphere composed of carrageenan for promoting imageable trans-arterial chemoembolization."Int J Biol Macromol. 2020 Jan;142:866 |
LogP | -0.5 |
EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
Introduction | iohexol is the raw material of a contrast agent, which is usually injected into a vein for angiography before CT angiography, urography of urinary system, spinal cord, femoral joint and lymphatic system has the advantages of low contrast density, low toxicity and good tolerance. It is one of the best contrast agents at present, developed countries have completely used it to replace the ionic contrast agent, but also diagnostic drugs. |
mechanism of action | the chemical structure of the nonionic contrast agent is triiodobenzene ring with three hydrophilic groups. Iohexol, iodinol, iophorol have 6 hydroxyl groups, there are 5 iopamidol. Iopromide has 4. Because of the iodine, for high-density contrast agent, in the X-ray film or 17 "film containing the local density of contrast agent increased, so that contrast enhancement, contribute to the diagnosis. Non-ionic contrast agent because of low osmotic pressure, molecular intrinsic toxicity is also low, so that the incidence of adverse drug reactions than the ionic contrast agent greatly reduced. |
function and purpose | 1. Intravascular application clinical application of this product in adults and children's urinary tract imaging and cardiovascular imaging, as well as adult cerebral angiography, peripheral and various arterial angiography, venography, digital subtraction and CT enhanced scan, 2. The subarachnoid space is suitable for myelography in adults and children, and is applied to the subarachnoid space, and CT scan of brain cistern is performed after injection. 3. The application of body cavity is suitable for all kinds of body cavity examination, including oral, such as arthrography, endoscopic retrograde cholangiopancreatography (ERCP), hernia sac radiography, urography, hysterosalpingography, sialography. And various gastrointestinal examinations using an oral water-soluble contrast agent. |
Non-ionic contrast agent | iohexol is a non-ionic contrast agent, pure white or light gray-white powder, hygroscopic. The trade names are known as eukaryote, iohexol, iodohexanol, and the like. In the early 80 s of last century, it was successfully developed by nekomin, Norway. It was first listed in Norway and Sweden in 1982, and was approved by the US Food and Drug Administration (FDA) in 1985, the German company and Japan first Pharmaceutical Co., Ltd. were assigned to the production, products sold in Europe and Asia-Pacific countries. The six hydroxyl groups in the molecule are evenly distributed around the benzene ring, which effectively shields the fat-soluble iodobenzene ring in the molecule, so that it has high hydrophilicity, low viscosity and low permeability than the common ionic contrast agent, it has the advantages of low toxicity to the nervous system. It is the raw material for the production of water-soluble, non-ionic X-CT contrast agent in pharmaceutical factories, and iohexol is also one of the best contrast agents at present, it has been completely replaced by ionic contrast agents in developed countries. Suitable for myelography, cardiovascular, arteriovenous, lymphatic system, urography and enhanced CT scan. The general dosage is as follows: the site of the spinal canal is determined, the lumbar thoracic vertebra 24% solution 8 ~ 12ml, the neck 24% solution 10 ~ 15ml,CT scan brain cisternography 8 ~ 12ml. |
pharmacological action | iohexol contrast agent is a non-ionic water-soluble contrast agent with osmotic pressure close to plasma, moderate viscosity and easy to inject. Clinical angiography and urography have demonstrated that it is less toxic than ionic contrast agents and can be safely used for myelography. The reason is that the non-ionic contrast medium has weak stimulation to mast cells, less histamine release and less allergic reaction. This product has weak vasodilator effect and is not easy to cause hypotension. It has little damage to vascular endothelium and is not easy to form thrombus. The toxicity was lower than that of amippac. This product almost does not penetrate the cell membrane, intravenous injection is mainly distributed in the interstitial cavity, organ tissue is not absorbed, the body is not metabolized, most of the urine in the original form of discharge. PBP<20%. Non-ionic intravascular contrast agents: iodinol, iohexol, iopamidol, iopromide, Iodixanol. FIG. 1 shows the molecular structure of iohexol. |
Clinical application | Cardiovascular angiography, urography, cerebral angiography, peripheral and various arteriography, venography, digital subtraction and CT enhanced scan. Myelography, as well as CT scan of the brain cistern after application to subarachnoid injection. Various body cavity examinations. |
subarachnoid application | ① before use, the iodine allergy test should be performed, and those who are positive are contraindicated. It is contraindicated in patients with history of epilepsy. (2) If you have a history of allergy or are suspected to be allergic to this product, and you must use this product for radiography, you can use adrenocortical hormones and antihistamines before angiography, but adrenal cortical hormone drugs are contraindicated in the spinal canal. (3) when there is local or systemic bacterial infection, do not perform lumbar puncture, of course, do not use this product imaging. ④ sedatives such as diazepam can be given preoperatively if necessary, and analgesics can be given if severe pain is present. (5) Good body fluid status, can reduce the incidence of adverse reactions, it should prevent patients from dehydration. (6) after the imaging, the patient should be placed in a supine bed, with the head raised for at least 6 hours and maintained in a supine position for 24 hours. The patient should not move or bend down his back to prevent the residual contrast agent from flowing to the brain, and can reduce cerebrospinal fluid leakage. 7 if the patient Nausea, Vomit, should be intravenous infusion instead of fluid food, if necessary, to give antiemetics. if myelography fails, repeat myelography should not be performed immediately. In case of epileptic seizure, the patient was relieved immediately by intravenous injection of 10mg diazepam. To prevent recurrence of epilepsy, can stop the onset of 20 to 30 minutes after the intramuscular injection of 0.2g of sodium phenobarbital. The relative density of ↑ Omnipaque (lohexol lnjectlon) was higher than that of cerebrospinal fluid. |
intravascular application | ① allergy test should be performed before use, and it is contraindicated if positive. (2) have a history of allergy, iodine allergy, have asthma patients disabled or used with caution. ③ severe liver and kidney dysfunction, severe thyroid disease, myelogenous leukemia patients should be used with caution; These patients dehydration should be disabled, serum creatinine concentration of more than 0.5mmol/L in patients with diabetes should be disabled. ④ use with caution in pregnant women, if necessary, when using the lowest dose. (5) This product can interfere with the thyroid function test, so that the ability of thyroid tissue combined with iodine is reduced, and it takes several days or even 2 weeks to fully recover. (6) contrast agent should not be mixed with other drugs, special syringe should be used. |
usage and dosage | intraspinal injection: the dosage is determined according to the examination items and the technique used, please refer to the following table: application Project concentration (mg/ml) dosage (ml/time) waist, CT cisternography 1802400~158~24018024010~12 children <2 years 2~6 years> 6 years 125~64~86~86 years Ct ~ 12 for cardiovascular, in arterial, venous and urography, the concentration and dosage of iodine used are generally the same as other vascular contrast agents currently used. |
drug interaction | 1. Simultaneous injection of iohexol contrast agent in patients treated with metformin can lead to lactic acidosis and acute renal failure. 2. Intrathecal injection of the drug with tricyclic antidepressants or monoamine oxidase inhibitors can reduce the threshold of seizures and cause seizures. patients treated with interleukin-2 within 3 and 2 weeks are at increased risk for delayed response (cold-like symptoms and skin reactions). 4, Class III antiarrhythmic drugs such as amiodarone in the recommended dose can prolong the QT interval, combined with the goods to extend the QT interval additive effect. This information has been edited by The Chemical Book et al (2015-08-03). |
adverse reactions | 1. Adverse reactions after subarachnoid application are roughly the same as those after receiving lumbar puncture, but are mostly mild. Head Pain incidence is less than after the use of meglumine, continued several days of intense Head Pain may occur intermittently. Others may have Nausea, Vomit, dizziness, neck and back pain, limb pain, paresthesia, EEG showed unclear short slow waves. 2. The frequency and severity of adverse reactions after intravascular application were significantly lower than those of other ionic contrast agents, and the adverse reactions were similar to those of meglumine. A small number of patients had mild reactions, such as warm feeling, red face, Nausea, Vomit, mild chest pain, skin itching, urticaria, lower limb numbness and so on. |
precautions | 1. Those with history of iodine allergy and allergy should be used with caution. 2, liver and kidney dysfunction, heart and circulatory system dysfunction, physical weakness, cerebral arteriosclerosis, diabetes, goiter, leukemia with caution. 3. Severe hyperthyroidism was contraindicated. 4, emergency treatment should be prepared for acute allergic reaction. |
Use | iohexol is a raw material for pharmaceutical manufacturers to produce water-soluble, non-ionic X-CT contrast media. The trade name of the contrast agent is known as onepack. This contrast agent is usually injected into the vein before CT angiography diagnosis, for angiography, urinary system, spinal cord and femoral joint, lymphatic system, with low contrast density, low toxicity, it is one of the best contrast agents at present, and has completely replaced the ionic contrast agent in developed countries. It is also a diagnostic drug. Non-ionic X-CT contrast media Cardiovascular angiography, coronary angiography, urography, enhanced CT scan and myelography, etc. |