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Biotrans tornaton o drus is defned as the comveston from one
chent cal torm to onother.
| x^ The^ chernftcal changs
ths, the duyni tion adudo themica rnstobility o7 a druq wfthin the
body
caYe uualley afcckd engymteally 0 the body 3
Convesion ok^ penictllin^ to^ penict^ loic^ acid^ by^ the^ bactrial pen?llinase and e^ mommalian^ engymes^ metabolism.^ bud^ Hs Bs
digradaion. by^ the^ Stomach^ add^ to^
ponicitlenic aGd^ B^ che^ mPcal
ostabttihy
t Nomaly^ Resute^ fn^ phanmacoloqie^ nochivaton^ of^ drugs
t nesut^ fa^ tormohon^ of^ metabol:tes^ wth^ (tle^
or) nto^ phan^ matoloq
acdivity
eq convesion^ of^ phenytoin^ hp-hydroy phenyton.
’ ocasfonaly yilds metabolitu^ with^ tqual^ actriy
eqr Conveuion^ of^ phnybutaee^ to^
Bryphenbutazene
Rovely deac^ to^ actvafion^ o^ dugt S usutt^ n^ fomation^ o7 metabolites^ wfth^ high^ fissue uactivi
(onveUsion o^ paralomo^ to^
Ytattive meabolites^ thot^ cauge
hepahic ntorog
DRU6S
+phanmaoloqical Snathvaton
(Active)
Amphetimne phnytoin
(Active)
METABOLUITES AND^ RELATVE^ AcTiviTY^ Of DRUGs
Amttiptg (odeine
o change^ fn^ phavmacloqkal^
Axtivity
Digitoxin Torfcoloqic Acivaion. (Adive)
MEIACOLT TES
Parautamol
(Inathre )
phanyaeonu Hydroyphunobanbakal
(Acive)
Novtriptyln
Morphine
(Reactie Gntamedidia) fissue aylatng mtermediat
îirtdoquinone of N-hydylated
Mtabolitey
polor punchonal qroup. thus undungo phae î Reation o
en (^) unetd by (^) hidnus
ay (^) oxdaton oq (^) AirOmaic (^) Caulbon (^) Afoms (^) (Aromatic (^) Hhydronyotio)
|dhis Reation proceds via tormation o «aitie rtermedlate tne pxideOxide undutyou heoYangenent to yield .anols
epoxi de Asene Hydrane
b Oxdatian
(Arensb)
C.^ oxfdation^ o^ Bengylic^ ,^ allylie^ car
OH.
d orîdatien o aliphati e Corbon oham e oxidati on o aliplie taabon atorn Oxidation o7 Canbon - Heteroatorm lyskres (ai bon - Nitrogen Syetm
?y N-dsalkylation
Dx îdatie deaoloaon its -^ oxide^ tormtion Hydioryleton'
i Desul7uaation
Car bon -sulyur ysthm.
S- eidation
(arbon ato ms
Caskon- bugen satens
Reduche Reocions
Bio nduch ony are (apoble op qnenohing polar tunhonal
Such CLs hytoy 5 onnino (^) wtkh Can (^) undug (^) gurthts (^) biotonatoraof
Ate ehol dehydognaon N- oxidati on
as Redution ot Caukonyu
altehes susptchely
Reducion oy^ aldebydu^ Gketones^ yields^ primony^3 Secnday
ado- keto-ducasu.
cl,C- cHO. H,
- The^ ualton^ i^ catalyzed^ by^ non-ncrosomad^ en3^ yme^ (alled as
(Chloal Hydote)
ob
alohol
OH
poattion Amine oxice Peaon
5 Reducion^ ok^ alcohas^ ,^ Canbon-^
(asbon uble^ bondu;
(Nor ethindhene)
(Tichlorotthanol)
Reduction o^ Norethfnd^ onc^ -^ an^ a,^ B-^ unsaturatd^ Caubonyl^ Lomp',
wesult fo botth^ uduchon^ oh^ C=c^ deuble^ bond^ t,^ tormaton^ os L-CeH
HO
(3p 5p Tehohydno^ novtthind^ ona)
by Hydroluysis^ o)^ Am^ idy
amidauey, nvolves C-N
hutholygt slouoly &the attion s (aBaluged by cleavcge to^ yield^ tonoie^ aud^ eamire
Canbamagpine
CONH, Canbanazepn
lactams
PHASE
C Hydnelti^ deavage^ o,^
Non-Aronmatic Httereyce
Non- anomati^ helerocuels^ alo^
tontain. ami^ cle^ kuncthony
Peniclin G
COOH
REALT20NS:
eKoetable ph'cologncally
Cogtnestilbou
de
(ocH,-i-NH HODC
tnent conjugats
penicilloic aid
ph ase^ seaction^ fovolvo^
ranuheh ob^ Suitdblt^ moeity^ Su^ ch^ au
qlucounonic aud,suhau,^ gycine^ ete. Yn^ presenu^ ob^ enyye oY medabolitu^ oh^ phase^ f^ Tea^ ttiun hanng transterae^ to^ dhg
.S
uadily
coH
Suitable tunctional^ foups^ to^ to1m^
Highty polar,
entgoion sotion w
rnctateim
iput tation^ dud^ urfdine^ dighoçhog^ teuronit^ oud obPG))
3phosphooduno Sin^ -s^ phosphowloa(^ Pnos).^ (or)
-odrn
tonjuqating Ttaqgnty^ mhich^ ar^ derii tonkbchydeot, ot ptin
Certonss with^ duq^ to^ yom^ Confuqa
Ccnfuaaton with^ alucouronic^ Acid^
|8.Trorgen
Gucurond tomation^ c^ urs^ n a^ slepsi
preni ot engme
1 Suntss^ o^ athvOHO^ Co-en3yrme^
oDPGh^ pom^ vDG^ qlucae
(o- enymt^ a^ UbpGA^ ats^ as^ dongr osgouone^ otid
6-UDP
;
eq GuLuTcd^ hahon^ ot^
bezic aid.
UDP- glucuony^ tansjenaæ^ to^
toim Conhuaat
(Begcie aud)
(ooH
qlu caronide o Bergoic atd.
+UDP
Atp hatie acid.
al' cycic acids
anyt acia
dr Conkugaton^ ofth^ glutathfone^ And^
Mercaptepuric acid tormatien
iseprchoxyacute add. cholic ad.
qlutathiane Ps^ a^ trie^ tide^ with^
sthrongly nucleophile.
n Chara er^ due^ to^ preReNepresene^ ofof^ -SM-^ SH^
qn0up nP%^ structue
highly
Salteylic al
A6sH^ Confugat^ dies^
pom other^ tonjugation^ e^ outio na in^ that
he proceys^ doesn't^ rtigui fnftial^ actiration^ of^
Co-eng4mu
Substrate.Sine,^ GsH^ which^ u a^ nudeophile^ s,^
it is
touasdo^ electephiie^
substsate eactive touar d
Congugdk
- The^ fnerad blo Substeate^8 GsM^ B^
CaBalyged by
alutattone -s-^ tansjerase^
to form^ s-^
Substitued
qlutomy
s not^ eyegeted^ by^ in^ urine^ but^ undengo^ es
cleavage, tnst^ by^
y-gultomy tronupeptfdse^ to^
veltae Hee
N-acetylat" o^ t^ gyine^ this^
tongyae by^ N-ouhylae
yields s-9ub:tibuted^ - N-^ aeBy^ cyle ine^ produtk.^ Calle^ d^ Mercap -tunic add
(Subshrat)
eivaties)
(Mocapturicaud
N-autyast
NHCOCH,
HDOC
oH
GONH-CH,-(
th Acetyiation
P AS
NHCO CH, (H,- (H-(o0H (6s4)
Q-S-CH (H
<ysteiny ycn
ale
This yeati^ on.^ Ps^ basfcaly^ an^ aylation Confugahon wtthwth^ amimo^ aud.
-NH, t^ CH,^ (oSCoA^
N-atcky transgrae
R-S - CH,-CH
qlutan
oH
glutathione S- Sttbstrt tanskrale CONH-CH. C00H
HoOC
qlu tahioe^ qConijugat
ayaion vtactton.^ a^ thus^ Stmila^ to
selved n^ Non-^ miAsOMal^ Nat^ transterast
1-gtany! tranueptidaie cONH-CH-C00H
NHCOH,(H, -CHCooH
NH COCH N- actyatd Phs.
