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DRAXMIBI 1 MG KIT FOR RADIOPHARMACEUTICAL PREPARATION

Active substance(s): TETRAKIS COPPER TETRAFLUOROBORATE

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213551

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213551

ENGLISH

ENGLISH

SUMMARY OF PRODUCT CHARACTERISTICS

PACKAGE LEAFLET:
INFORMATION FOR THE USER

1 NAME OF THE MEDICINAL PRODUCT
DRAXMIBI 1 mg kit for radiopharmaceutical preparation

DRAXMIBI 1 mg
Kit for radiopharmaceutical ­preparation
Tetrakis (2-methoxy isobutyl isonitrile) copper(I)
tetrafluoroborate
Read all of this leaflet carefully before you start using
this medicine.
–  Keep this leaflet. You may need to read it again.
–  If you have any further questions, ask your doctor or
pharmacist.
–  This medicine has been prescribed for you. Do not
pass it on to others as it may harm them.
–  If any of the side effects gets serious, or if you notice
any side effects not listed in this leaflet, please tell
your doctor or pharmacist.
In this leaflet:
1.  What DRAXMIBI is and what it is used for
2.  Before you are injected with DRAXMIBI
3.  How to use DRAXMIBI
4.  Possible side effects
5.  How to store DRAXMIBI
6.  Further information

2 QUALITATIVE AND QUANTITATIVE COMPOSITION
1 vial contains:
Active substance
Tetrakis (2-methoxy isonitrile) Copper (I) Tetrafluoroborate �����������������������������������������1 mg
Excipients:
This medicinal product contains 0.61 mg of Sodium per vial.
For a full list of excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Kit for radiopharmaceutical preparation.
Lyophilized, white powder.
To be reconstituted with sodium pertechnetate (99mTc) solution for injection (not included in this kit).
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
This medicinal product is for diagnostic use only.
After reconstitution with sodium technetium pertechnetate (99mTc) solution for injection,
the solution of technetium (99mTc) sestamibi obtained is indicated for:

1. WHAT DRAXMIBI IS AND WHAT IT IS USED FOR
This medicinal product is for diagnostic use only.
DRAXMIBI is used to study the blood circulation,
especially the blood circulation in the heart. It is also
used to determine if any areas of the heart muscle
have been damaged because of an insufficient blood
supply to the heart. DRAXMIBI is also used in the
diagnosis of breast cancer when the results of other
diagnostic methods are unclear. DRAXMIBI can also
be used to check for overactivity of the parathyroid
gland, which may be causing an abnormally high
activity of this organ.
After injecting DRAXMIBI, your doctor will then take
an image (scan) of the concerned organ. The area
where the radioactive compound accumulated will
show up in the scan and help the doctor make the
diagnosis.
2. BEFORE YOU ARE INJECTED WITH DRAXMIBI
Do not use DRAXMIBI
If you are allergic (hypersensitive) to the active substance or any of the other ingredients of DRAXMIBI
(see Section 6 for a list of ingredients).
Take special care with DRAXMIBI
This product is hardly ever used in patients under
18 years because it has not been fully investigated in
this age group. If you are younger than 18 years, the
doctor may still decide to use this product if the risks
are smaller than the benefits. Please tell your doctor,
if you know you are suffering from a kidney and/or
liver disease and/or malformation of your gallbladder. Your doctor will explain to you the details of the
applied doses and procedures.
Please also read the information under ‘Pregnancy
and breastfeeding’.
DRAXMIBI contains a small amount of radioactive
medicine and will be injected in your body. The risk
associated with this procedure is very small. Your
doctor will only carry out the examination if he/she
believes that the risk is smaller than the potential
benefit of the examination.
Using other medicines
Please tell your doctor if you are taking or have
recently taken any other medicines, including medicines obtained without a prescription.
Pregnancy and breastfeeding
Ask your doctor for advice before taking any medicine.
It is important to tell your doctor if you are or may be
pregnant or if you are breast­feeding. The use of
medicinal products which contain radioactivity during pregnancy must be considered carefully. Your
doctor will only administer this product during pregnancy if a benefit is expected that outweighs the
risks.
If you are breastfeeding, please tell your doctor. He/
she may decide either to postpone the examination
until you have stopped breastfeeding or ask you to
stop breastfeeding temporarily.
Breastfeeding should be stopped for 24 hours after
injection and the expressed milk within this period
of time should be discarded.
Driving and using machines
DRAXMIBI does not affect the ability to drive or use
machines.
Important information about some ­ingredients of
DRAXMIBI
This medicinal product contains less than 1 mmol
Sodium (23 mg) per vial. This means that this product is practically ‘sodium-free’.
3. HOW TO USE DRAXMIBI
This product may only be used in accordance with
your doctor’s instructions and under his/her supervision.
DRAXMIBI is administered by injection into a vein.
The doctor may give you 2 injections for heart imaging, one at rest and one with exercise. If 2 injections
are needed, they will be given at least 2 hours apart.
Scans can be made until 6 hours after the injection.
If DRAXMIBI is used to study the blood flow in your
heart, you should not eat for at least four hours prior
to the examination. Your doctor may ask you to have
a light fatty meal or drink one or two glasses of milk
after each injection, prior to making the scan.
Your doctor may advise you to drink a lot of fluid so
that the traces of radioactivity will leave your body
more quickly. This is normal when using medicinal
products which contain radioactivity. Your doctor
will also tell you about any other steps you may need
to take following the use of this product.
Because there are strict laws covering the use, handling and disposal of radioactivity, DRAXMIBI will
always be used in a hospital or in similar settings. It
will only be handled and administered by people
who have been trained and are qualified in the safe
handling of radioactive material.
If you are injected with more DRAXMIBI than you
should
Since DRAXMIBI is administered under strictly controlled circumstances by a doctor, it is unlikely that
you will be given an overdose. Should this happen
nonetheless, the doctor will take appropriate measures.
Your doctor may then also advise you to drink a lot
of fluid so that the traces of radioactivity will leave
your body more quickly.
If you have any further questions on the use of this
product, ask your doctor.
4. POSSIBLE SIDE EFFECTS
Like all medicines, DRAXMIBI can cause side
effects, although not everybody gets them.
The following terms are used to describe how often
side effects have been reported.
very common: affects more than 1 user in 10
common: affects 1 to 10 users in 100
uncommon: affects 1 to 10 users in 1,000
rare: affects 1 to 10 users in 10,000
very rare: affects less than 1 user in 10,000
not known: frequency cannot be ­estimated from
the available data

Assessment of global ventricular function
First-pass technique for determination of ejection fraction and/or ECG-triggered, gated
SPECT for evaluation of left ventricular ejection fraction, volumes and regional wall
motion.
Scinti-mammography for the detection of suspected breast cancer
Detection of suspected breast cancer when mammography is equivocal, inadequate or
indeterminate.
Localisation of hyperfunctioning parathyroid tissue in patients with recurrent or persistent hyperparathyroidism, and in patients scheduled to undergo surgery of the parathyroid glands.
4.2 Posology and method of administration
For intravenous use.
The suggested activity range for intravenous administration to a patient of average weight
(70 kg) is:
Diagnosis of reduced coronary perfusion and myocardial infarction:
400 – 900 MBq
Assessment of global ventricular function:
600 – 800 MBq injected as a bolus.
For diagnosis of ischaemic heart disease two injections (stress and rest) are required in
order to differentiate transiently from persistently reduced myocardial uptake. The recommended activity range for diagnosis of ischemic heart disease according to the
European procedural guideline is
– Two-day protocol: 600 – 900 MBq/study
– One-day protocol: 400 – 500 MBq for the first injection, three times more for the second
injection.
Not more than a total of 2000 MBq should be administered for a one-day protocol and
1800 MBq for a two-day-protocol by these two injections which should be done at least
two hours apart but may be performed in either order. After the stress injection, exercise
should be encouraged for an additional one minute (if possible).
In each country nuclear medicine physicians should respect the diagnostic reference
levels (DRLs) and the rules laid down by the local legislation. The injection of activities
greater than local DRLs should be justified.
For diagnosis of myocardial infarction one injection at rest may be sufficient.
For breast imaging: 740 – 925 MBq injected as a bolus in the arm opposite to the
lesion.
For parathyroid imaging: 185 – 740 MBq injected as a bolus.
(The activity used should in every case be as low as reasonably practical).
Safety and efficacy in children below the age of 18 years have not been established.
Where appropriate and practical, an investigation that does not involve radiation should
be employed.
The use in children and adolescents has to be considered carefully, based upon clinical
needs and assessing the risk/benefit ratio in this patient group. The activities to be
administered for children should be modified according to the recommendations of the
Paediatric Task Group of the EANM (1990). This activity can be determined from the
recommended activity for adults on the basis of body mass, using the following multiplying coefficient:
  3 kg = 0.10

22 kg = 0.50

42 kg = 0.78

  4 kg = 0.14

24 kg = 0.53

44 kg = 0.80

  6 kg = 0.19

26 kg = 0.56

46 kg = 0.82
48 kg = 0.85

  8 kg = 0.23

28 kg = 0.58

10 kg = 0.27

30 kg = 0.60

50 kg = 0.88

12 kg = 0.32

32 kg = 0.62

52 – 54 kg = 0.90

14 kg = 0.36

34 kg = 0.64

56 – 58 kg = 0.92

16 kg = 0.40

36 kg = 0.66

60 – 62 kg = 0.96

18 kg = 0.44

38 kg = 0.68

64 – 66 kg = 0.98

20 kg = 0.46

40 kg = 0.70

68 kg = 0.99

Cardiac Imaging
If possible, patients should fast for at least four hours prior to the study. It is recommended that patients eat a light fatty meal or drink a glass or two of milk after each
injection, prior to imaging. This will promote rapid hepatobiliary clearance of technetium
(99mTc) sestamibi resulting in less liver activity in the image.
Imaging should begin approximately after 60 min after injection to allow for hepatobiliary
clearance. Longer delay can be required for resting images and for stress with vasodilatators alone because of the risk of higher subdiaphragmatic 99mTc activity. There is no
evidence for significant changes in myocardial tracer concentration or redistribution,
therefore imaging for up to 6 hours post injection is possible. Test may be done in a one
day or two days protocol.
Tomographic imaging (SPECT) with or without ECG gating should be performed according
to current international guidelines.
Breast imaging is optimally initiated 5 to 10 minutes post injection with the patient in the
prone position with breast freely pendant. A 10 minute lateral image of the breast suspected of containing cancer should be obtained with the camera face as close to the
breast as practical.
The patient should then be repositioned so that the contralateral breast is pendant and
a lateral image of it should be obtained. An anterior supine image may then be obtained
with the patient’s arms behind her head.
Parathyroid imaging depends on whether subtraction technique or wash-out technique
is used. For the subtraction technique either 123I, 99mTc or Tl-201 can be used and should
be performed according to literature, guideline and recommended activites:
If double phase technique is used, 370 to 740 MBq of technetium (99mTc) sestamibi are
injected and the first neck and thorax image obtained 10 minutes later. After a wash-out
period of 1 to 2 hours, neck and thorax imaging is again performed.
Between the two images SPECT or SPECT/CT can be performed.
In case of kidney failure, exposure to ionising radiation can be increased. This must be
taken into account when calculating the activity to be administered.
In general, activity selection for patients with a decreased hepatic function should be
cautious, usually starting at the low end of the dosing range.
For the instruction for preparation and control of the radiochemical purity of the radiopharmaceutical, see section 12.
4.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients.
4.4 Special warnings and precautions for use
Pregnancy, see section 4.6.
Contents of the vial are intended only for use in the preparation of technetium (99mTc)
sestamibi and are not to be administered directly to the patient without first undergoing
the preparative procedure.
Newborns, infants, children and adolescents, see section 4.2.
In myocardial scintigraphy investigations under stress conditions, the general contraindications and precautions associated with the induction of ergometric or pharmacological
stress should be considered.
Because of potential tissue damage extravasal injection of this radioactive product has to
be strictly avoided.
In patients with reduced hepatobiliary function, a very careful consideration is required
since an increased radiation exposure is possible in these patients.
Breast lesions less than 1 cm in diameter may not all be detected with scintimammography as the sensitivity of technetium (99mTc) sestamibi for the detection of these lesions
is 25% relative to histological diagnosis. A negative examination does not exclude breast
cancer especially in such a small lesion.
Proper hydration and frequent urination are necessary to reduce bladder irradiation.
Radiopharmaceutical agents should be used only by qualified personnel with the appropriate government authorisation for use and manipulation of radionuclides. Its receipt,
storage, use, transfer and disposal are subject to the regulations and/or appropriate
licences of the local competent official organisation.
For each patient, exposure to ionising radiation must be justified on the basis of likely
benefit.
The activity administered must be such that the resulting radiation dose is as low as
reasonably achievable bearing in mind the need to obtain the intended diagnostic or
therapeutic result.

Very common (≥1/10)
Common (≥1/100 to <1/10)
Uncommon (≥1/1,000 to <1/100)
Rare (≥1/10,000 to <1/1,000)
Very rare (<1/10,000)
Immune system disorders:
Rare: Severe hypersensitivity reactions such as dyspnoea, hypotension, bradycardia,
asthenia and vomiting (usually within two hours of administration of DRAXMIBI), angioedema.
Nervous system disorders:
Uncommon: Headache
Rare: Seizures (shortly after administration of DRAXMIBI), syncope.
Cardiac disorders:
Uncommon: Chest pain/angina pectoris, abnormal ECG.
Rare: Arrhytmia.
Gastrointestinal disorders:
Uncommon: Nausea
Rare: Abdominal pain.
Skin and subcutaneous tissue disorders:
Rare: Allergic skin and mucosa reactions with exanthema (pruritus, urticaria, oedema),
vasodilatation, local reactions at the injection site, hypoaesthesia and paraesthesia,
flushing.
Very rare: Other hypersensitivity reactions have been described in predisposed patients.
If hypersensitivity reactions occur, the administration of the medicinal product must be
discontinued immediately and, if necessary, intravenous treatment initiated.
Respective medicinal products and equipment (e.g. endotracheal tube and ventilator)
have to be readily available.
General disorders and administration site conditions:
Common: Immediately after injection, a metallic or bitter taste, partly in combination
with dry mouth and an alteration in the sense of smell may be observed.
Rare: Fever, fatigue, dizziness, transient arthritic-like pain.
Other disorders:
Exposure to ionising radiation is linked with cancer induction and a potential for development of hereditary defects. As most diagnostic nuclear medicinal product investigations
are done with low radiation doses of less than 20 mSv these adverse events are expected
to occur with a low probability. The effective dose calculated with an average amount
of activity of 2000 MBq (500 MBq at rest and 1500 MBq at stress) for a 1-day-protocol is
16.4 mSv (4.5 mSv at rest and 11.9 mSv at stress). The effective dose is 8.32 mSv when
the maximal recommended activity of 925 MBq is administered.
4.9 Overdose
In the event of administration of a radiation overdose with technetium (99mTc) sestamibi
the absorbed dose to the patient should be reduced where possible by increasing the
elimination of the radionuclide from the body by frequent micturation and defaecation.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Technetium (99mTc) compounds
ATC code: V09GA01
Pharmacodynamic effects are not expected after administration of technetium (99mTc)
sestamibi.
After reconstitution with Sodium Pertechnetate (99mTc) Injection, the following complex
forms (technetium (99mTc) sestamibi):
99mTc-(MIBI) + Where: MIBI = 2-methoxy isobutyl isonitrile
6
Technetium (99mTc) sestamibi, when administrated in usual doses and by the usual way,
has no pharmacodynamic effects detectable clinically.
5.2 Pharmacokinetic properties
Technetium (99mTc) sestamibi is a cationic complex which accumulates in the viable
myocardial tissue proportional to the regional coronary blood flow.
Technetium (99mTc) sestamibi from the blood is rapidly distributed into the tissue:
5 minutes after injection only about 8% of the injected dose is still in circulation.
The tissue uptake of technetium (99mTc) sestamibi depends primarily on the vascularisation which is generally increased in tumour tissue. Due to its lipophilicity and its positive
charge, the technetium (99mTc) sestamibi complex crosses the cell membrane and concentrates in the most negatively charged compartment of the cell, the mitochondria.
Cardiac indication
Technetium (99mTc) sestamibi binds to the mitochondrial membrane and an intact mitochondrial membrane potential is important for intracellular binding.
The uptake of technetium (99mTc) Sestamibi in the myocardium is proportional to blood
flow in the physiologic flow range. The rate of passive uptake is determined by the membrane permeability of the drug and the surface area of the vascular beds to which it is
exposed. Since the radio­tracer enters the cell via diffusion, it will underestimate blood
flow at high flow rates (>2.0 ml/g/min).
When coronary flow varied from 0.52 to 3.19 ml/g/min, myocardial extraction for technetium (99mTc) sestamibi averaged 0.38 +/– 0.09. Technetium (99mTc) sestamibi from the
blood is rapidly distributed into the tissue. Five minutes after injection only about 8 percent of the injected dose is still in circulation.
Technetium (99mTc) sestamibi undergoes minimal redistribution over time. This may
impact on lesion detection as the differential washout between the normal and ischemic
myocardium may result in a reduction in defect size or severity with time.
Mastology indication
The cellular concentration of technetium (99mTc) sestamibi was demonstrated to be
increased in mammary tumour tissue probably because of the high content of mitochondria in tumour cells and the high membrane potential of tumour cells.
Several in vitro studies demonstrated that technetium (99mTc) sestamibi is a substrate of
P-glycoprotein. A direct correlation between the P-glycoprotein expression and the elimination of technetium (99mTc) sestamibi from tumours has been established. The cellular
over-expression of P-glycoprotein could result in false negative images of tumours,
especially of tumours larger than 1 cm.
Parathyroid indication
In adenoma of the parathyroid glands blood flow and the number of mitochondria are
increased. This fact may explain the elevated uptake and trapping of technetium (99mTc)
sestamibi in parathyroid adenoma.
Localisation of technetium (99mTc) ­sestamibi appears to be dependent on blood flow to the
tissue, the concentration of technetium (99mTc) sestamibi presented to the tissue, and the
size of the parathyroid adenoma.
Myocardial uptake which is coronary flow dependent is 1.5% of the injected dose at stress
and 1.2% of the injected dose at rest.
Animal experiments have shown that uptake is not dependent on the functional capability
of the Sodium-potassium pump. Irreversibly damaged cells however do not take up technetium (99mTc) sestamibi. The myocardial extraction level is reduced by hypoxia.
The clearance of the myocardial fraction is minimal and the redistribution is insignificant
during at least 4 hours after an induced ischemia in the dog. Technetium (99mTc) sestamibi is rapidly distributed from the blood into the tissue: 5 minutes after injection only
about 8% of the injected dose is still in circulation.
However some experimental and clinical studies indicated a redistribution in severely
ischaemic areas. A potential influence on the diagnostic quality of the test has not been
established.

!

Common side effects that have occurred in patients
who have been injected with DRAXMIBI include:
metallic or bitter taste, alteration of smell, and dry
mouth immediately after injection.

Myocardial perfusion scintigraphy
Detection and localisation of coronary artery disease and myocardial infarction.

Radiopharmaceuticals should be prepared by the user in a manner which satisfies both
radiation safety and pharmaceutical quality requirements. Appropriate aseptic precautions should be taken, complying with the requirements of Good Manufacturing Practice
for pharmaceuticals.
This medicinal product contains less than 1 mmol Sodium (23 mg) per dose, i.e. essentially
‘Sodium-free’.
If hypersensitivity reactions occur, the administration of the medicinal product must be
discontinued immediately and intravenous treatment initiated, if necessary. To enable
immediate action in emergencies, the necessary medicinal products and equipment such
as endotracheal tube and ventilator must be immediately available.
4.5 Interaction with other medicinal products and other forms of interaction
No drug interactions have been described to date. Medicinal products which affect myocardial function and/or blood flow may cause false negative results in the diagnosis of
coronary arterial disease. For this reason, concomitant medication should be taken into
consideration when interpreting the results of the scintigraphic examination.
4.6 Pregnancy and lactation
Women of childbearing potential
When it is necessary to inject radiopharmaceuticals to women of childbearing potential,
information should always be sought about pregnancy. Any woman who has missed
a period should be assumed to be pregnant until proven otherwise. Where uncertainty
exists it is important that radiation exposure should be the minimum consistent with
achieving the desired clinical information. Alternative techniques, which do not involve
ionising radiation, should be considered.
Pregnancy
Radionuclide procedures carried out on pregnant women also involve radiation to the
foetus. Only imperative investigations should therefore be carried out during pregnancy,
when the likely benefit far exceeds the risk incurred by the mother and foetus.
Lactation
Before administering a radiopharmaceuticals to a mother who is breastfeeding consideration should be given as to whether the investigation could be reasonably delayed until
after the mother has ceased breastfeeding and as to whether the most appropriate choice
of radio­pharmaceuticals has been made, bearing in mind the secretion of activity in
breast milk.
If the administration is considered necessary, breastfeeding should be interrupted for
24 hours and the expressed feeds discarded. Close contact with infant should be restricted during this period.
4.7 Effects on ability to drive and use machines
DRAXMIBI has no influence on the ability to drive and use machines.
4.8 Undesirable effects
The following table presents how the frequencies are reflected in this section:

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  5.3 Preclinical safety data
In acute intravenous toxicity studies in mice, rats and dogs, the lowest dose of tech­netium
(99mTc) sestamibi that resulted in any deaths was 7 mg/kg (expressed as Cu(MIBI)4BF4
content) in female rats. This corresponds to 500 times the maximal human dose (MHD) of
0.014 mg/kg for adults (70 kg). Neither rats nor dogs exhibited treatment related effects at
technetium (99mTc) sestamibi doses of 0.42 mg/kg (30 times MHD) and 0.07 mg/kg
(5 times MHD) respectively for 28 days. At repeated dose administration, the first toxicity
symptoms appeared during the administration of 150 times the daily dose during 28 days.
Studies on reproductive toxicity have not been conducted.
Cu(MIBI)4BF4 showed no genotoxic activity in the Ames, CHO/HPRT and sister chromatid exchange tests. At cytoxic concentrations, an increase in chromosome aberration
was observed in the in vitro human lymphocyte assay. No genotoxic activity was
observed in the in vivo mouse micronucleus test at 9 mg/kg.
Studies to assess the carcinogenic potential of DRAXMIBI have not been conducted.
  6 PHARMACEUTICAL PARTICULARS
  6.1 List of excipients
Sodium Citrate Dihydrate
L-Cysteine Hydrochloride Monohydrate
Mannitol
Stannous Chloride Dihydrate
Hydrochloric Acid (for pH-adjustment)
Sodium Hydroxide (for pH-adjustment)
  6.2 Incompatibilities
The technetium labelling reactions involved depend on maintaining the stannous level
in the reduced state. Hence, Sodium Pertechnetate (99mTc) Injection containing oxidants should not be employed.
This medicinal product must not be mixed with other medicinal products except those
mentioned in section 12.
  6.3 Shelf life
Before reconstitution: 15 months.
After reconstitution: 10 hours. Do not store above 25°C. Do not refrigerate or freeze.
  6.4 Special precautions for storage
Store in the original package in order to protect from light.
Unlabelled product: Do not store above 25°C. Do not refrigerate or freeze.
For storage conditions of the reconstituted medicinal product, see section 6.3.
Storage should be in accordance with national regulations for radioactive material
  6.5 Nature and contents of container
10 ml glass vials, type 1 borosilicate glass sealed with a butyl rubber stopper.
Pack sizes: 2, 5 and 10 vials in a carton.
Not all pack size may be marketed.
This product is in multi-dose vials.
  6.6 Special precautions for disposal
Any unused product or waste material should be disposed of in accordance with local
requirements.
  7

MARKETING AUTHORISATION HOLDER
DRAXIMAGE (UK) Limited
125 Old Broad Street, 26th Floor, London
United Kingdom EC2N 1AR

  8

MARKETING AUTHORISATION NUMBER(S)
PL 29620/0003

  9 DATE OF FIRST AUTHORISATION
6 May 2009
10

DATE OF REVISION OF THE TEXT
1 February 2013

11

DOSIMETRY
Technetium (99mTc) is produced by means of a (99Mo/99mTc) generator and decays
with the emission of gamma radiation with mean energy of 140 keV and half-life of
6.02 hours to technetium (99mTc) which, in view of its long half-life of 2.13 x 105 years
can be regarded as quasi stable.
The data listed below are from ICRP 80 and are calculated according to the following
assumptions: After intravenous injection the substance is rapidly cleared from the
blood and accumulates mainly in muscular tissues (including heart), liver, kidneys, and
a smaller amount in salivary glands and thyroid. When the substance is injected in conjunction with a stress test, there is a considerable increase of the uptake in organs and
tissues. The substance is excreted by the liver and kidneys in the proportions 75% and
25%, respectively.
Dose absorbed per activity administered
[mGy/MBq] (resting test)
Organ

Adults

 15-yearold

10-yearold

5-yearold

1-yearold

Adrenal glands

0.0075

0.009

0.015

0.022

0.038

Bladder walls

0.011

0.014

0.019

0.023

0.041

Bone surface

0.0082

0.010

0.016

0.021

0.038

Brain

0.0052

0.0071

0.011

0.016

0.027

Breasts

0.0038

0.0053

0.0071

0.011

0.020

Gall bladder

0.039

0.045

0.058

0.10

0.32

Alimentary tract:
Stomach
Small intestine
  Colon
  ULI
  LLI

0.0065
0.015
0.024
0.027
0.019

0.0090
0.018
0.031
0.035
0.025

0.015
0.029
0.050
0.057
0.041

0.021
0.045
0.079
0.089
0.065

0.035
0.080
0.015
0.17
0.12

Heart

0.0063

0.0082

0.012

0.018

0.030

Kidneys

0.036

0.043

0.059

0.085

0.015

Liver

0.011

0.014

0.021

0.030

0.052

Lungs

0.0046

0.0064

0.0097

0.014

0.025

Muscles

0.0029

0.0037

0.0054

0.0076

0.014

Oesophagus

0.0041

0.0057

0.0086

0.013

0.023

Ovaries

0.0091

0.012

0.018

0.025

0.045

Pancreas

0.0077

0.010

0.016

0.024

0.039

Bone marrow

0.0055

0.0071

0.011

0.030

0.044

Salivary glands

0.014

0.017

0.022

0.015

0.026

Skin

0.0031

0.0041

0.0064

0.0098

0.019

Spleen

0.0065

0.0086

0.014

0.020

0.034

Testicles

0.0038

0.0050

0.0075

0.011

0.021

Thymus

0.0041

0.0057

0.0086

0.013

0.023

Thyroid

0.0053

0.0079

0.012

0.024

0.045

Uterus

0.0078

0.010

0.015

0.022

0.038

Other organs

0.0031

0.0039

0.0060

0.0088

0.016

Effective dose
  [mSv/MBq]

0.0090

0.012

0.018

0.028

0.053

Dose absorbed per activity administered
[mGy/MBq] (exercise test)
Adults

15-yearold

10-yearold

5-yearold

1-yearold

Adrenal glands

0.0066

0.0087

0.013

0.019

0.033

Bladder walls

0.0098

0.013

0.017

0.021

0.038

Bone surface

0.0078

0.0097

0.014

0.020

0.036

Brain

0.0044

0.0060

0.0093

0.014

0.023

Breasts

0.0034

0.0047

0.0062

0.0097

0.018

Gall bladder

0.033

0.038

0.049

0.086

0.26

Alimentary tract:
Stomach
Small intestine
  Colon
  ULI
  LLI

0.0059
0.012
0.019
0.022
0.016

0.0081
0.015
0.025
0.028
0.021

0.013
0.024
0.041
0.046
0.034

0.019
0.037
0.064
0.072
0.053

0.032
0.066
0.12
0.13
0.099

Heart

0.0072

0.0094

0.010

0.021

0.035

Kidneys

0.026

0.032

0.044

0.063

0.11

Liver

0.0092

0.012

0.018

0.025

0.044

Lungs

0.0044

0.0060

0.0087

0.013

0.023

Muscles

0.0032

0.0041

0.0060

0.0090

0.017

Oesophagus

0.0040

0.0055

0.0080

0.012

0.023

Ovaries

0.0081

0.011

0.015

0.023

0.040

Pancreas

0.0069

0.0091

0.014

0.021

0.035

Bone marrow

0.0050

0.0064

0.0095

0.013

0.023

Salivary glands

0.0092

0.011

0.0015

0.0020

0.0029

Skin

0.0029

0.0037

0.0058

0.0090

0.017

Spleen

0.0058

0.0076

0.012

0.017

0.030

Organ

213551.indd 2

Testicles

0.0037

0.0048

0.0071

0.011

0.020

Thymus

0.0040

0.0055

0.0080

0.012

0.023

Thyroid

0.0044

0.0064

0.0099

0.019

0.035

Uterus

0.0072

0.0093

0.014

0.020

0.035

Other organs

0.0033

0.0043

0.0064

0.0098

0.018

Effective dose
  [mSv/MBq]

0.0079

0.010

0.016

0.023

0.045

The effective dose per unit of administered activity has been calculated according to
a voiding frequency of 3.5 hours in adults.
Myocardial perfusion scintigraphy
The effective dose calculated with an average amount of activity of 1800 MBq (900 MBq
at stress and 900 MBq at rest) for a 2-day-­protocol is 15.2 mSv.
The effective dose calculated with an average amount of activity of 2000 MBq (500 MBq
at rest and 1500 MBq at stress) for a 1-day-­protocol is 16.4 mSv.
Evaluation of ventricular function
After injection of 800 MBq, the effective dose is 7.2 mSv at rest. After injection of
800 MBq, the effective dose is 6.3 mSv at stress.
Scinti-mammography
After injection of 925 MBq, the effective dose is 8.32 mSv.
Parathyroid imaging of hyperfunctioning tissue
The effective dose after administration of 740 MBq is 6.7 mSv.
12 INSTRUCTIONS FOR PREPARATION OF RADIOPHARMACEUTICALS
The contents of the kit before preparation are not radioactive. However, after Sodium
Pertechnetate (99mTc) Injection is added, adequate shielding of the final preparation
must be maintained.
The administration of radiopharmaceuticals creates risks for other persons from external radiation or contamination from spill of urine, vomiting etc. Radiation protection
precautions in accordance with national regulations must therefore be taken.
As with any pharmaceutical product, if at any time in the preparation of this product the
integrity of the vial is compromised it should not be used.
The medicinal product should not come into contact with air.
The labelling of the kit should be made according to either method A or method B.
Instructions for Preparation of technetium (99mTc) sestamibi
A. Boiling procedure:
Preparation of technetium (99mTc) sestamibi from DRAXMIBI is to be done according to
the following aseptic procedure:
  1 Waterproof gloves should be worn during the preparation procedure. Remove the
plastic disc from the DRAXMIBI vial and swab the top of the vial closure with alcohol to disinfect the surface.
  2 Place the vial in a suitable radiation shield appropriately labelled with date, time of
preparation, volume and activity.
  3 With a sterile shielded syringe, aseptically obtain additive-free, sterile, non-­
pyrogenic sodium pertechnetate (99mTc) solution (max. 11.1 GBq) in approximately
1 to 3 ml. Not less than 3 ml sodium pertechnetate (99mTc) solution will be use for
the maximum activity of 11.1 GBq.
  4 Aseptically add the sodium pertechnetate (99mTc) solution to the vial in the lead
shield. Without withdrawing the needle, remove an equal volume of headspace to
maintain atmospheric pressure within the vial.
  5 Shake vigorously, about 5 to 10 quick upward-downward motions.
  6 Remove the vial from the lead shield and place upright in an appropriately shielded
and contained boiling water bath, such that the vial is suspended above the bottom
of the bath, and boil for 10 minutes. The bath must be shielded. Timing for the
10 minutes commences as soon as the water begins to boil again.
Note: The vial must remain upright during the boiling step. Use a water bath where the
stopper will be above the level of the water.
  7 Remove the shielded vial from the water bath and allow cooling for fifteen minutes.
  8 Inspect visually for the absence of particulate matter and discoloration prior to
administration.
  9 Aseptically withdraw material using a sterile shielded syringe. Use within ten
(10) hours of preparation.
10 Radiochemical purity should be checked prior to patient administration according
to the Radio-TLC Method as detailed below.
Note: the potential for cracking and significant contamination exists whenever vials
containing radioactive material are heated.
B. Thermal Cycler procedure:
Preparation of technetium (99mTc) sestamibi from DRAXMIBI is to be done according to
the following aseptic procedure:
  1 Waterproof gloves should be worn during the preparation procedure. Remove the
plastic disc from the DRAXMIBI vial and swab the top of the vial closure with alcohol to disinfect the surface.
  2 Place the vial in a suitable radiation shield appropriately labelled with date, time of
preparation, volume and activity.
  3 With a sterile shielded syringe, aseptically obtain additive-free, sterile, non-­
pyrogenic sodium pertechnetate (99mTc) solution (max. 11.1 GBq) in approximately
1 to 3 ml. Not less than 3 ml sodium pertechnetate (99mTc) solution will be use for
the maximum activity of 11.1 GBq.
  4 Aseptically add the sodium pertechnetate (99mTc) solution to the vial in the lead
shield. Without withdrawing the needle, remove an equal volume of headspace to
maintain atmospheric pressure within the vial.
  5 Shake vigorously, about 5 to 10 quick upward-downward motions.
  6 Place the shield in the sample block. While slightly pressing downwards, give the
shield a quarter turn to make certain there is a firm fit between the shield and the
sample block.
  7 Press the proceed button to initiate the program (the thermal cycler automatically
heats & cools the vial and contents). Please see the Recon-o-stat Instruction
Manual for further details.
  8 Inspect visually for the absence of particulate matter and discoloration prior to
administration.
  9 Aseptically withdraw material using a sterile shielded syringe. Use within
ten (10) hours of preparation.
10 Radiochemical purity should be checked prior to patient administration according
to the Radio-TLC Method as detailed below.

Uncommon side effects that have occurred in
patients who have been injected with DRAXMIBI
include: headache, chest pain, abnormal ECG and
feeling sick.
Rare side effects that have occurred in patients who
have been injected with DRAXMIBI include: hypersensitivity reactions, abnormal heart rhythm, oedema, local reactions at the injection site, stomach
pain, vomiting, itching, hives, fever, fainting, seizures, dizziness, flushing, rash, skin numbness or
tingling, fatigue, shortness of breath (dyspnoea), low
blood pressure (hypotension), and joint pains.
Exposure to ionising radiation can cause cancer and
can possibly cause hereditary defects in children
you may later wish to have. However, like most
radioactive medicinal products that are used for
diagnostic examinations, DRAXMIBI has low radiation doses of less than 20 mSv therefore these risks
are very small.
If any of the side effects gets serious or if you notice
any side effects not listed in this leaflet, please tell
your doctor or pharmacist.
5. HOW TO STORE DRAXMIBI
DRAXMIBI will be stored by the hospital pharmacist.
The pharmacist and the doctor will follow the advice
listed below:
Keep out of the reach and sight of children.
Do not use DRAXMIBI after the expiry date which is
stated on the vial and the box after EXP. The expiry
date refers to the last day of that month.
Store in the original package in order to protect from
light. Unlabelled and labelled product: Do not store
above 25°C. Do not refrigerate or freeze.
Storage should be in accordance with national regulations for radioactive material.
Shelf-life after reconstitution: 10 hours.
Do not use DRAXMIBI if you notice cracks or any
other indication that the product is no longer vacuum-sealed.
DRAXMIBI should be disposed according to local
regulations.
6. FURTHER INFORMATION
What DRAXMIBI contains
The active substance is Tetrakis (2 methoxy isobutyl
isonitrile) copper(I) tetrafluoroborate
Each vial contains 1 mg.
The other ingredients are: sodium citrate dihydrate,
L-cysteine hydrochloride mono­hydrate, mannitol,
stannous chloride dihydrate, hydrochloric acid and
sodium hydroxide.
What DRAXMIBI looks like and contents of the pack
DRAXMIBI 1 mg kit for radiopharmaceutical preparation is a white, freeze-dried powder.
Pack sizes: 2, 5 or 10 vials.
Not all pack sizes may be marketed.
This product is in multi-dose vials.
Marketing authorisation holder
DRAXIMAGE (UK) Limited
125 Old Broad Street, 26th Floor
London, EC2N 1AR
United Kingdom
Manufacturer responsible for batch release
Diagnostic Imaging Limited (DIL)
Elkington Lodge
Welford
Northamptonshire
NN6 6HE
United Kingdom
This medicinal product is authorised in the member
states of the EEA under the ­following names:
O Belgium
DRAXMIBI 1 mg trousse pour ­préparation radiopharmaceutique
O Denmark
DRAXMIBI
O Germany
DRAXMIBI 1 mg kit für ein radioaktives
Arzneimittel
O The Netherlands
DRAXMIBI 1 mg kit voor radiofarmaceutisch preparaat
O United Kingdom
DRAXMIBI 1 mg kit for radiopharmaceutical
preparation
This leaflet was last approved in 02/2013.
The following information is intended for healthcare
professionals only:
The complete Summary of Products Charac­teristics is
added as a tear-off section at the end of this package
leaflet.
DRAXIMAGE® is a Registered Trademark of Jubilant
DraxImage Inc.

Radio-TLC Method for the Quantification of technetium (99mTc) sestamibi
1. Materials
1.1 Baker-Flex-Aluminium Oxide plate, # 1 B-F, pre-cut to 2.5 cm x 7.5 cm.
1.2 Ethanol, > 95%.
1.3 Capintec, or equivalent instrument for measuring radioactivity in the
0.74 –11.12 GBq range.
1.4 1 ml syringe with a 22-26 gauge needle.
1.5 Small developing tank with cover, (100 ml beaker covered with Parafilm® is sufficient).
2. Procedure
2.1 Pour enough ethanol into the developing tank (beaker) to have a depth of 3-4 mm of
solvent. Cover the tank (beaker) with Parafilm® and allow it to equilibrate for
approximately 10 minutes.
2.2 Apply 1 drop of ethanol, using a 1 ml syringe with a 22-26 gauge needle on to the
Aluminium Oxide TLC plate, 1.5 cm from the bottom. Do not allow the spot to dry.
2.3 Apply 1 drop of the kit solution on top of the ethanol spot. Dry the spot. Do not
heat!
2.4 Develop the plate a distance of 5.0 cm from the spot.
2.5 Cut the strip 2.5 cm (one third) from the bottom of the strip, and measure each
piece in your dose calibrator.
2.6 Calculate the % radiochemical purity as:
% (99mTc) sestamibi = ( Activity top portion)/
(Activity both pieces) x 100.
2.7 % (99mTc) sestamibi should be ≥ 94%; otherwise the preparation should be discarded.
Note: Do not use material if the radiochemical purity is less than 94%.
After reconstitution the container and any unused contents should be disposed of in accordance with local requirements for radioactive materials.
DRAXIMAGE® is a Registered Trademark of Jubilant DraxImage Inc.

213551

#

Elimination
The major metabolic pathway for clearance of technetium (99mTc) sestamibi is the
hepatobiliary system. Activity from the gallbladder appears in the intestine within one
hour of injection. About 27% of the injected dose is cleared through renal elimination
after 24 hours and approximately 33% of the injected dose is cleared through the faeces
in 48 hours.
Half-Life
The biological myocardial T1/2 is approximately 7 hours at rest and stress. The effective
T1/2 (which includes biological and physical half-lives) is approximately 3 hours.

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2013/06/26 2:14 PM

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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