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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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

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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Toxicity

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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Technetium Tc-99m exametazime which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AclidiniumAclidinium may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
AcrivastineTechnetium Tc-99m exametazime may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
Adefovir dipivoxilAdefovir dipivoxil may decrease the excretion rate of Technetium Tc-99m exametazime which could result in a higher serum level.
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Food Interactions
No interactions found.

Products

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Active Moieties
NameKindUNIICASInChI Key
Technetium Tc-99munknown6EW75241VU14133-76-7GKLVYJBZJHMRIY-NJFSPNSNSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CeretecKit0.5 mg/5mLIntravenousMedi-Physics Inc.1988-12-30Not applicableUS flag
CeretecInjection, powder, lyophilized, for solution0.5 mg/5mLIntravenousMedi-Physics Inc. dba GE Healthcare.1988-12-30Not applicableUS flag
Drax ExametazimeInjection, powder, lyophilized, for solution0.5 mg/1IntravenousJubilant DraxImage Inc., dba Jubilant Radiopharma2017-08-17Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CeretecTechnetium Tc-99m exametazime (0.5 mg/5mL) + Cobalt chloride (200 ug/2mL)KitIntravenousMedi-Physics, Inc. dba GE Healthcare2018-09-25Not applicableUS flag

Categories

ATC Codes
V09AA01 — Technetium (99mtc) exametazime
Drug Categories
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
  1. Ui K, Yamaguchi T: [Therapy and diagnosis of emergency shock patients]. Nihon Naika Gakkai Zasshi. 1991 Dec 10;80(12):1892-6. [Article]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
KEGG Drug
D02284
PubChem Substance
347910416
RxNav
1431726
ChEMBL
CHEMBL2111018
RxList
RxList Drug Page
Wikipedia
Technetium_(99mTc)_exametazime
FDA label
Download (114 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous0.5 mg/5mL
KitIntravenous
KitIntravenous0.5 mg/5mL
Injection, powder, lyophilized, for solutionIntravenous0.5 mg/1
Injection, powder, lyophilized, for solutionIntravenous0.18 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

Drug created at October 05, 2015 16:56 / Updated at October 09, 2021 02:48