Tìm theo
Iobenguane
Các tên gọi khác (6 ) :
  • Adreview
  • Iobenguane
  • Metaiodobenzylguanidine
  • mIBG
  • SID11111341
  • SID90341658
diagnostic agents
Thuốc Gốc
Small Molecule
CAS: 139755-80-9
ATC: V09IX01
CTHH: C8H10IN3
PTK: 275.0896
Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. FDA approved on September 19, 2008.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H10IN3
Phân tử khối
275.0896
Monoisotopic mass
274.991940755
InChI
InChI=1S/C8H10IN3/c9-7-3-1-2-6(4-7)5-12-8(10)11/h1-4H,5H2,(H4,10,11,12)
InChI Key
InChIKey=PDWUPXJEEYOOTR-UHFFFAOYSA-N
IUPAC Name
2-[(3-iodophenyl)methyl]guanidine
Traditional IUPAC Name
2-[(3-iodophenyl)methyl]guanidine
SMILES
NC(N)=NCC1=CC(I)=CC=C1
Độ tan chảy
0°C
Độ sôi
100°C
Độ hòa tan
Soluble
logP
1.64
logS
-3.5
pKa (Strongest Basic)
11.27
PSA
64.4 Å2
Refractivity
58.32 m3·mol-1
Polarizability
21.93 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : AdreView is a diagnostic radiopharmaceutical which contains a small quantity of iobenguane that is not expected to produce a pharmacodynamic effect. Patients with renal insufficiency may experience increased radiation exposure and impaired imaging results.
Cơ Chế Tác Dụng : Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. FDA approved on September 19, 2008. Structure of iobenguane is similar to noradrenaline so it can be taken up by adrenergic tissue in the adrenal medulla, liver, heart, and spleen. Once taken up by noradrenaline transporters in the adrenergic nerve terminals, it is stored in the presynaptic storage vesicles. The radioactive iodine component is responsible for its imaging properties.
Dược Động Học :
▧ Absorption :
Iobenguane rapidly clears from the blood and is highly retained in adrenergic tissues.
▧ Metabolism :
Less than 10% of the dose is metabolized into m-iodohippuric acid (MIHA). However the mechanism in which this metabolite is produced is unknown.
▧ Route of Elimination :
Renally excreted unchanged (70%-90%) via glomerular filtration; Fecal (<1%)
▧ Half Life :
Physical half life = 13.2 hours
Độc Tính : Oral mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50=980 mg/kg. The most common adverse reactions, dizziness, rash, pruritis, flushing, headache, and injection site hemorrhage occurred in < 1.3% of patients.
Chỉ Định : Detection of primary and metastatic pheochromocytoma or neuroblastoma
Tương Tác Thuốc :
  • Amitriptyline May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it inhibits noradrenaline transporter function
  • Cocaine Sympathomimetic that increase chances of producing a false negative imaging result
  • Ephedrine Sympathomimetic that increase chances of producing a false negative imaging result
  • Imipramine May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it inhibits noradrenaline transporter function
  • Labetalol May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it depletes or inhibit reuptake of noradrenaline stores
  • Milnacipran Milnacipran decreases the effects of Iobenguane thus increases the risk of producing a false-negative result. May discontinue milnacipran for at least 5 half-live.
  • Phenylephrine Sympathomimetic that increase chances of producing a false negative imaging result
  • Phenylpropanolamine Sympathomimetic that increase chances of producing a false negative imaging result
  • Pseudoephedrine Sympathomimetic that increase chances of producing a false negative imaging result
  • Reserpine May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it depletes or inhibit reuptake of noradrenaline stores
Liều Lượng & Cách Dùng : Injection, powder, for solution - Intravenous - 0.08 mg and I-123 74 MBq (2 mCi) per mL
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06704
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60860
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04559
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/17156-235-01
Wikipedia
http://en.wikipedia.org/wiki/Iobenguane
RxList
http://www.rxlist.com/adreview-drug.htm
Drugs.com
http://www.drugs.com/mtm/iobenguane-i-123.html
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