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Causes of Nonlinearity

1) Nonlinearity in drug absorption, distribution, metabolism, and excretion can occur due to various physiological factors like saturation of transport systems, plasma protein binding sites, metabolic enzymes, and excretory pathways. 2) Specific examples where nonlinearity occurs include water soluble vitamins that saturate carrier systems at high doses and drugs like phenytoin that saturate metabolism due to enzyme or cofactor limitations. 3) Changes in gastric emptying, blood flow, or other biological factors can also influence drug absorption in a nonlinear manner.

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Hritik Chaubey
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2K views

Causes of Nonlinearity

1) Nonlinearity in drug absorption, distribution, metabolism, and excretion can occur due to various physiological factors like saturation of transport systems, plasma protein binding sites, metabolic enzymes, and excretory pathways. 2) Specific examples where nonlinearity occurs include water soluble vitamins that saturate carrier systems at high doses and drugs like phenytoin that saturate metabolism due to enzyme or cofactor limitations. 3) Changes in gastric emptying, blood flow, or other biological factors can also influence drug absorption in a nonlinear manner.

Uploaded by

Hritik Chaubey
Copyright
© © All Rights Reserved
Available Formats
Download as PDF, TXT or read online on Scribd
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Brophomouhes PhamorokinuHu GP 60YT

Uni5
austs Nonbinuorit Dr. Parjanya Shukla
&
Druq absorpHon Singh dases
pr. M. P.

NonLbinuority con ocwn


in Orug dishrikuhion
Dru' matahoism and
Dra Ax (YAHon
Drug Absarpian- oriss
Nonlinaviky in drug abro»pHon con
rom -

(A)When abuorphon i btlubility or dmoluhon


Hal -imitad e.g Griauofilvin
AH highur doaks » 0 salwrahd solukon d drug i
dormud in GIT oT af ony "okar
dxkovas wlor 6lt

So t t a d absonphon oHains a comstant valu

(B)Whun abrorphon involues COrTiy-md'alid transpert


6ybtam absophon d uiboflavin, ascorkic aid
Cyonocobalamin et.
Saturahon o tranapot syshem a ighr doxs
dthest Vitomins resulth nonbinuovwty.
C)hun TAAyatemic qut wall oY kapahic makabalism
atainsalurahich e:1: propronalol, hydrodozin and
VErOamil.
dahraion cdos
prayshamicto matabalinm d kus drugs
a high ad intTIaMd bioavailabiby.
#Th boTometaTa of{chad will bL F, Ka, Cmax and AUC
i n case A and B
in casl
ORr Causs onan.untarity n drug absoaph'on
Dr. Parjanya Shukla

chonge in gatric emphying, 1 blood {Wouo and Dr. M.P. Singh Classes
otfu bhyaiologieal doctora.

DrugDishibuion
Non linuariky in drug dishbubm al kigh doses may bu du to

(A) dahnahon d bindig Bttos on plasma protains


e9. phenylbuhazonu and naproxen

Thu th o deinits number od binding aitas foro banhwor


drug On plosmo prote'na and

as Ka conunkahm xaihid, froch'm unbound to hat

(Sahuralion hauu binding Altus


9 thiopental and fenfany. Aentanyl
Wih Joq Angl doss or mulipl doainq, bakurahm a
HM storog Aitas Can OCwY.

Tn Cans A plasma drug tonunrakm , Vd.


Tn Cas Vd.

)Drug Melaboism -
ww mnm

ts myoY Aounu q lorge intersubjac vartablliky i


phammatological suspomA
x Two imprtant Causas ononlinuariky in mutabol'sm ors -

(D Cabouy -bimitad mglabolism duu fo enzymt and /or Cofocor


salunaion e. Phenytoin, alcohal, hiophyllin th.
(B) Enzymi induchon e. COTbamo zehina
Dr. Parjanya Shukla
&
whu a datraasa in
plak plasmo comunhaHon Dr. M. P.Stngh Clases
has bun obanvad on apahkv odminishrakan
hm
oVAY OeTiod oHimu.
aturahm o eh2y mes uAults în
RovaTA in
dereased H 60 mcraassd Css eh2ymi induchon.

9Drug kruhon
)Achu Hubulor sacTahin eg paniuillin G
A saturahan coriT dyaBam - a deorsass dR ocu.

b) Achva tubuwor xuabaovpHon


e9. wateT A0lublu vitamins and glutohL

Aakurahom h orrier 8ystem > a încriass in Ug ocum


AHter
OKur sounas ononlinuarity in unal excra Hon intuds

torud diurAAis, chonges in urin ph, nuphrotoxiu'


and sakurahom d bindng aits.

Cy-Dr. Mohundra PraBab Singb

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