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Transcript of ΦΑΡΜΑΚΕΥΤΙΚΗΧΗΜΕΙΑ ΡΑ∆ΙΟΦΑΡΜΑΚΑusers.auth.gr/papagd/Farmakeutiki...
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Tel. 2310-998680
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(Radiopharmaceutical) , .
, , , .
, ,
:
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He2+
--- e-
+--e+
--
-
N N
NN
Tc
OH
O
O
99mTc-D,L-HMPAO
N N
NS
O
O
O
COOH
99mTc-MAG3
Tc
O
-
S
N N
S
N
Cl
Tc
O
99m Tc-TRODAT-1
NIn
N
O
N
O
OO
O
O
O
O
HN
O
D-Phe
Cys
Trp-DLys
Thr
Cys
Thr(ol)
S S
-
[131I]NaI
-
-
- , .
- ( DNA, )
-
-
-
( )
(e+)- (2 , 511 keV)
(e+)
-
(, ) 80-300 keV ( ) (, -)
/
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95%
(~ 10-10 )
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PETSPECT
15O(+, 123s)15N
13N(+, 9.9m)13C
11C(+, 20.3m)11B201Tl (EC, 74h) 201Hg
18F(+, 109.7m)18O111In(EC, 2.8d, 173keV)111Cd
82Rb (+, 1.2m) 82Kr123I (EC, 13.3h, 159keV)123Te
68Ga (+, 68.3m)68Zn99mTc (IT, 6h, 140keV)99Tc
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( ) (SPECT, PET)
SPECT
PET
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-
-
-
-
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/
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:
( )
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65 m-,6.8 7.2 h211t70 m-,7.8 1h212Bi12 mm-, 2.282.67 d 90Y
11 mm0.155, 2.1316.95 h 188Re
8.7 mm-, 1.7114.3 d 32P
5 mm0.131, 1.083.7 d 186Re
3 mm0.103, 0.81.95 d153Sm
2 mm0.36, 0.68.04 d 131I
1.9 mm0.32, 0.571.48 d105Rh
1.8 mm0.185, 0.542.58 d67Cu
1.5 mm0.21, 0.496.7 d 177Lu
(MeV)
(MeV)
-
, Auger.
LET /
DNA
(> 0.4 Gy/h). 10 h t1/2.
(carrier free)
,
-
DNA
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,
: , , , , , ,
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Ammonia (13N) injectionChromium (51Cr) edetate injectionCyanocobalamin (57Co) capsulesCyanocobalamin (58Co) capsulesFludeoxyglucose (18F) injectionFlumazenil (N-(11C) methyl) injectionGallium (67Ga) citrate injectionHuman albumin injection, iodinated (125I)Indium (111In) pentetate injectionIobenguane (123I) injectionIobenguane (131I) injection for diagnostic useIobenguane (131I) injection for therapeutic useKrypton (81Kr) inhalation gasL-Methionine (11C-methyl) injectionNorcholesterol injection, iodinated (131I)Raclopride (11C-(methyl) injectionSodium acetate (1-11C) injectionSodium fluoride (18F) injectionSodium iodide (123I) injectionSodium iodide (131I) capsules for diagnosti use
Sodium iodohippurate (123I) injectionSodium iodohippurate (131I) injectionSodium pertechnetate (99mTc) injection (fission)Sodium pertechnetate (99mTc) injection (non-fission)Sodium phospate (32P) injectionStrontium (89Sr) chloride injectionTechnetium (99mTc) colloidal rhenium sulphide injectionTechnetium (99mTc) colloidal sulphur injectionTechnetium (99mTc) colloidal tin injectionTechnetium (99mTc) etifenin injectionTechnetium (99mTc) exametazime injectionTechnetium (99mTc) gluconate injectionTechnetium (99mTc) human albumin injectionTechnetium (99mTc) macrosalb injectionTechnetium (99mTc) medronate injectionTechnetium (99mTc) mertiatide injectionTechnetium (99mTc) microspheres injectionTechnetium (99mTc) pentetate injectionTechnetium (99mTc) sestamibi injectionTechnetium (99mTc) succimer injectionTechnetium (99mTc) tin pyrophospate injectionThallous (201Tl) chloride injectionWater (15O) injectionXenon (133Xe) injection
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>95%
. :
: ) , ) , ) , )
-
( +
)
( , , )
-
: , , .
(Instant Thin Layer Chromatography, ITLC) silica
(HPLC)
ITLC
PLC
Rf= cm /cm %
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99mTc:
140 kev
6h
99Mo-99mTc
To 85% -99m , , , , , , ..
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Mo-99/Tc-99m
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Sn2+ +99mTcO4- + H+ 99mTc4+ + Sn4+ + H2O S2O42- + 99mTcO4- + OH- 99mTc4+ + SO32- + H2O
Tc(VII)TcO4-
Tc(V)Tc(IV)Tc(III)Tc(I)
SnCl2, Na2S2O4, HCl, Fe(II), NaBH4,, PPh3
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M -99m
1) :99mTcO4- + + L [99mTc-L]
L= , = SnCl2, NaBH4
2) M ) 99mTcO4- + + L [99mTc-L]
L= ) [99mTc-L] + L [99mTc-L] + L
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99mTc
-
: 99mTc ,
().
:
: .
-
: dl-99mTc-HMPAO
(99mTc-exametazime)
N N
NN
OH
O
Tc
O ~5%
: , [TcO(V)]3+
dl : ( )
(, , Alzheimer )
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99mTc-dl-HMPAO
99mTc-d,l-HMPAO
99mTc-meso-HMPAO
99mTc-d,l-HMPAO
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dl-99mTc-HMPAO >80% : 2 hr ( ), 4-6 hr
( , ) -
3-5% 5 min 50% 3-4 24 . 12%
( )
41% 48
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dl-99mTc-HMPAO 99mTc-d,l-- , . , , - .
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dl-99mTc-HMPAO , , ...
Alzheimer
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S
N N
N
O
O
O
OH
O
Tc-MAG3
Tc
O
Tc-DTPA
. 1-2 .
90% 24 h 5%-10% 1h.
TcN
N N
O
O
O
O-
O
O
O
O
-O
O
Tc(V), ,
3-5 min
.
-
- , -, , .
-
'
.
-
99mTc-Sestamibi
C
CC
CC
N
Tc
C
N
NN
N N
OCH3
OCH3
OCH3
OCH3
H3CO
H3CO
+ , Tc +1 1,5% 1,2%
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SPECT Imaging of Heart
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Cardiac Ischemia
Tc-99m-sesta-mibi stress test
Tl-201 rest
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O/ , 99mTc-MDP
70% .. Ca10(PO4)6(OH)2
P
P
OH
OH
O
OP
P
OH
OH
O
O
TcO
O O
O
OH
OH
HO P O P OH
O O
OH OH
HO P C P OH
O O
OH OH
X
Z
,
, =, MDP, =, =, HDPX=OH, Z=Me, HEDP
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Tc-99m-MDP
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99mTc-MDP
PP
OOHOHHO
O
OH 40-50% 3-4 hrs
: , , .
: , ,
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186/188186/188ReRe--HEDPHEDP
(69% ): Ca10(PO4)6(OH)2
186Re: (t1/290,6 h, - =1, 075eV, 137 eV) 185Re(n,) 186Re188Re: (t1/217 h, - =2,11eV, 155 eV) 188W/188Re
186/188186/188ReRe--HEDPHEDP::186/188186/188ReOReO44-- + SnCl+ SnCl22 + HEDP + HEDP 186/188186/188ReRe--HEDPHEDP
:
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710 710 keVkeV --/ / 103 103 keVkeV (5 %)(5 %)TT1/21/2: 46 hrs : 46 hrs 47-77% 153Sm-EDTMP . 16:1. Sm-153-EDTMP , 88-90% 98% 4 . QUADRAMET QUADRAMET . . 3 3--4 4 QUADRAMET. QUADRAMET.
QUADRAMET 153153SmSm--EDTMPEDTMP
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: Na99mTcO4 99Mo-99mTc. 12
, Tc-99.
. :
-: 15-20 min iv .
70-80% , 20-30% , , . .
. : 18.5-80 q.
a131 p.o. 6-24 h .
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:
I-123 EC (100%), T1/2= 13.2 hr, = 159 KeV (83%)
I-125 EC (100%), T1/2= 60 d, = 35 KeV(7%)
I-131- (100%), T1/2= 8 d, = 284 (6%), 364 (81%), 637(7%)
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aa123/131123/131I.I.
Na131I , Natrii iodidi (131I) capsulae ad usumdiagnosticum, Natrii iodidi (131I) capsulae ad usum therapeuticium, Natrii iodidi (131I) solutio
> 99.9% .
: -133, -135, a3 Per os :
3 hr. 90% , 50% 24 h 10-35 % 24 h pi
X: , , .
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[[1818F]F]--FDGFDG
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[[1818FF]]--FDGFDG
, , ,
, , , ,
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[[1818F]F]--FDGFDG