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Identification
- Summary
Technetium Tc-99m exametazime is a radiopharmaceutical diagnostic agent used as an adjunct for scintigraphy in the detection of altered regional cerebral perfusion in stroke.
- Brand Names
- Ceretec, Drax Exametazime
- Generic Name
- Technetium Tc-99m exametazime
- DrugBank Accession Number
- DB09163
- Background
Technetium Tc-99m exametazime is a radiopharmaceutical sold under the trade name Ceretec used in the detection of altered regional cerebral perfusion in stroke and other cerebrovascular diseases. It can also be used for the labelling of leukocytes to localise intra-abdominal infections and inflammatory bowel disease. Exametazime, also known as hexamethylpropyleneamine oxime or HMPAO, acts as a chelating agent for the Tc-99m radioisotope.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- (99m)Tc HM-PAO
- (99m)Tc HMPAO
- [(99m)Tc] HM-PAO
- Technetium (99mTc) exametazime
- Technetium (99mTc) HMPAO
- Technetium tc 99m exametazime
- Technetium tc 99m HMPAO
- Technetium Tc-99m exametazime
Pharmacology
- Indication
Technetium Tc99m exametazime scintigraphy (with or without methylene blue stabilization) may be useful as an adjunct in the detection of altered regional cerebral perfusion in stroke. Tc99m exametazime without methylene blue stabilization is indicated for leukocyte labeled scintigraphy as an adjunct in the localization of intra-abdominal infection and inflammatory bowel disease.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Inflammatory bowel disease •••••••••••• Diagnostic agent Intra-abdominal infection •••••••••••• Diagnostic agent Altered regional cerebral perfusion in stroke •••••••••••• - Contraindications & Blackbox Warnings
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During the first hour following injection of Tc99m labeled leukocytes, activity is seen in the lungs, liver, spleen, blood pool, bone marrow and the bladder. The kidneys (parenchyma and/or renal pelvis) and gall bladder may also be visualized. Over the first 1-6 hours, the Tc99m is visualized in the bowel. At 24 hours post-injection substantial colonic activity is seen.
- Mechanism of action
- Not Available
- Absorption
Technetium Tc-99m exametazime is rapidly cleared from the blood after intravenous injection. Uptake in the brain reaches a maximum of 3.5-7.0% of the injected dose within one minute of injection. Up to 15% of the activity is eliminated from the brain by 2 minutes post injection, after which little activity is lost for the following 24 hours except by physical decay of technetium Tc99m.
- Volume of distribution
The activity not associated with the brain is widely distributed throughout the body, particularly in muscle and soft tissue.
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
About 30% of the injected dose is found in the gastrointestinal tract immediately after injection and about 50% of this is excreted through the intestinal tract over 48 hours. Also, about 40% of the injected dose is excreted through the kidneys and urine over the 48 hours after injection.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Technetium Tc-99m exametazime which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Active Moieties
Name Kind UNII CAS InChI Key Technetium Tc-99m unknown 6EW75241VU 14133-76-7 GKLVYJBZJHMRIY-NJFSPNSNSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ceretec Injection, powder, lyophilized, for solution; Kit 0.5 mg/5mL Intravenous Medi-Physics Inc. 1988-12-30 Not applicable US 
Ceretec Injection, powder, lyophilized, for solution 0.5 mg/5mL Intravenous Medi-Physics Inc. dba GE Healthcare. 1988-12-30 Not applicable US Drax Exametazime Injection, powder, lyophilized, for solution 0.5 mg/1 Intravenous Jubilant DraxImage Inc., dba Jubilant Radiopharma 2017-08-17 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Ceretec Technetium Tc-99m exametazime (0.5 mg/5mL) + Cobalt chloride (200 ug/2mL) Injection, powder, lyophilized, for solution; Injection, solution; Kit Intravenous Medi-Physics, Inc. dba GE Healthcare 2018-09-25 Not applicable US
Categories
- ATC Codes
- V09AA01 — Technetium (99mtc) exametazime
- Drug Categories
- Amines
- Central Nervous System
- Compounds used in a research, industrial, or household setting
- Diagnostic Radiopharmaceuticals
- Diagnostic Uses of Chemicals
- Drugs that are Mainly Renally Excreted
- Hydroxylamines
- Indicators and Reagents
- Laboratory Chemicals
- Organometallic Compounds
- Organotechnetium Compounds
- Oximes
- Radioactive Diagnostic Agent
- Radiopharmaceutical Activity
- Radiopharmaceuticals
- Technetium (99Mtc) Compounds
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 3B744AG22N
- CAS number
- 99944-78-2
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Ui K, Yamaguchi T: [Therapy and diagnosis of emergency shock patients]. Nihon Naika Gakkai Zasshi. 1991 Dec 10;80(12):1892-6. [Article]
- Weldon MJ, Joseph AE, French A, Saverymuttu SH, Maxwell JD: Comparison of 99m technetium hexamethylpropylene-amine oxime labelled leucocyte with 111-indium tropolonate labelled granulocyte scanning and ultrasound in the diagnosis of intra-abdominal abscess. Gut. 1995 Oct;37(4):557-64. [Article]
- Moretti JL, Defer G, Cinotti L, Cesaro P, Degos JD, Vigneron N, Ducassou D, Holman BL: "Luxury perfusion" with 99mTc-HMPAO and 123I-IMP SPECT imaging during the subacute phase of stroke. Eur J Nucl Med. 1990;16(1):17-22. [Article]
- Van de Wiele C, Philippe J, Van Haelst JP, Van Damme J, Thierens H, Leroux-Roels GE, Dierckx RA: Relationship of decreased chemotaxis of technetium-99m-HMPAO-labeled lymphocytes to apoptosis. J Nucl Med. 1997 Sep;38(9):1417-21. [Article]
- Erba PA, Conti U, Lazzeri E, Sollini M, Doria R, De Tommasi SM, Bandera F, Tascini C, Menichetti F, Dierckx RA, Signore A, Mariani G: Added value of 99mTc-HMPAO-labeled leukocyte SPECT/CT in the characterization and management of patients with infectious endocarditis. J Nucl Med. 2012 Aug;53(8):1235-43. doi: 10.2967/jnumed.111.099424. Epub 2012 Jul 11. [Article]
- Fulgenzi A, Casati R, Colombo FR, Gasparini M, Ferrero E, Bondanza A, Gerundini P, Ferrero ME: Distribution of 99mTc-labeled lymphocytes in control and inflamed rats. Nucl Med Biol. 2004 Jul;31(5):631-8. [Article]
- External Links
- KEGG Drug
- D02284
- PubChem Substance
- 347910416
- 1431726
- ChEMBL
- CHEMBL2111018
- RxList
- RxList Drug Page
- Wikipedia
- Technetium_(99mTc)_exametazime
- FDA label
- Download (114 KB)
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 0.5 mg/5mL Injection, powder, lyophilized, for solution; injection, solution; kit Intravenous Injection, powder, lyophilized, for solution; kit Intravenous 0.5 mg/5mL Injection, powder, lyophilized, for solution Intravenous 0.5 mg/1 Injection, powder, lyophilized, for solution Intravenous 0.18 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at October 05, 2015 16:56 / Updated at October 09, 2021 02:48