General Pharmacology 01 Class Notes PDF

1 Routes of drug Administration 2 Bioavailability and Bioequivalence 3 Distribution  P H A R M A C O L O G Y S y s...

1 Routes of drug Administration 2 Bioavailability and Bioequivalence 3 Distribution  P H A R M A C O L O G Y S y s te m pich a r m a c o lo g y G e n e r a l Ph a rm a c o lo g y A N S - PK R e s p. s y st em PD C V S - D R U G B lo o d 9 1T A u t a c o id s E n d o cr in e A n t im i c r o b ia l A n t i c a n c er  G e n e r a P lh a r m a c o lo g y d o e s D R U G. o D R U G + m o v e m en t in s id e B o d y t o o P h a r m a c o k in et i c s B o d y d o e s B o d y D R U G + e f fe ct p r o d u c e D R U G t o ② P h a r m a co d y n a m ic s ③ D R U G S D e v el o p m e nt T y p es A D R e t c  H E A D M E S t u d y P H A R M A C O K IN E T I C S c a lc ul a t e O R A L A ① A B S O R P T IO N B A P K > P R IM A R Y D 2 D IS T R IB U T I O N V d ④ p a r a m e t e r s M ③ M E T A B O LI S M C L ① ÷ B lo o d E 4 E X C R E T IO N c a l c u la t e l o a d di n o gs e : m a in t e n a n c E L I M I N A T IO N t ''2 o 0 o E m u n n e w a t er s o lu bl e §  : C el l u l a r b a r r ie r s a d r u g h a st o cro s s t o A B S O R P T I O N r e a c Sh y s te m i c C i r c u l a ti o n ( V E IN S ) ③ C a l c u la t e 0 T y p e so f C el l u l a r ② R o u te of D R U G B i o a v a i l a b il i t y B a r ri e r s D I S T R IB U T IO N L S H ig h c on c. H O IN T O C R O S S C el l u l a r B a r r ie r s C el l m e m b. m o s t D R U G S ① S IM P /L E P A S S I V E D I F F U S : IO N PH O S P H OP PID S ✓ cr o s s L ow con c. * L IP ID s o lu b le D R U G S * N O A T P r e q u ir e d * A lo n g t h e C on c -g r a d i e n t s  10 0 % L ip id s o lu b le 10 0 % w a t e r s o lu b le ① N on - i o n i c S T R O I oN n i c G N on - p o la r. H IG H L Y P o la r I S ⑤ W E A K - Io n ic Y E S C ro s s N ot cr o s s D R U G S ✓ Ab s or be d Or a l ✗ n o t a b s o r b e d or a l e.g H E P A R IN Q A m in o g l y co si d e P K V A L U E Q. T h a t p H a t w h ic h a d r u g s PK V A L U E DR U G p k b e co m 5 e 0s 1. Io n ic S l i o n i c 501. W ☑ + 5 0 /. L S n o n- i o n i c 5 0 1. n o n - i o n i c M E D IA ( P H )  c a l c u la t ed : H e n d e r s o n H a s s el b a ch e g n L o g io n ic con c. → 5 01. L o g s = p H + p k = n o n - io n ic c on c ] 5/0 1. 10 % c h a n g e s io n ic / n o n cico n c b y ⊛ ♀ ch a n g e of p H b y 1 ( m e d ia ) M O R P H IN E ¥ : A S P IR IN Q PK b = 8.5 Pk a = 3.5 W S W E A K A ci d i c w e a k B A S IC B A S IC A u dic L S L S m e d ia M e d ia p H s c a l e O 3.5 7 " s 14 n e u tr a l " % 5 07. 5 0 1. ↘ 5 0 9  m o r e L S n o n - i o n ic : A ci d i c W e a k a ci d ic D R U G m e d l e * 0 - 1 W S Io n ic : B a s ic m e d i a 8 - 9 I S n o n - io n ic : B A S I C m e c h e m o r e * w e a k B a s ic D R U G S ↳ i s / ' m : ic A ci d i c m e d i s IN S p H 8 n o t in f lu en c e d b y ? S t r o n g A n d /B a s ic D R U G 5 01. Al w a y s i o n ic 10 t i m es l o g o  Q Q A S P IR IN I TO R A NP P IN G in s id e S t om a ch C el l s B lo o d 3.5 c ro s s 3.5 G A S T R IC u lc er s v o n - io n i c S le : 7 4 - H Cl : 0 - 1 10 N i c M A T H S T im e : R ed u c e A b s o r p tio n ? D R U G S f r o m stom a ch ② A n t a c id s A S P IR IN pk = 3.5 B B A S IC I o n ic N o n - Io n ic R ed u ce a ci d i t y n A ci d i c D R U G S 5 01. D R U G P H = 3.5 5 0 % of st o m a ch L o gs - 1 10 /. 9 01. pH = 2.5 Log to ✓ 9 91. M A X A b s o r p ti o n L o g - 1 1 ). l p H = 1.5 0 - 1 B A S IC D R U GS : SI > > > > S tom a ch f u n c t io n 0. If. 9 9.9 1. 4 0 1 = 0.5 ( D u o d en u m ) 10 0 L o g to 3 A C ID IC D R U G S : SI > St om a ch @ 8- 9 10 A ll D R U G S f r o m G R E A T E R s u rf a c eA r e a SI 1 0.1  O T H E R M e t h o d s of C r o s s in g C el l s IN S PL 2 A q u e o u s D if f u s io n → W a t e r s o lu b le / i o n icD R U G cro s s A Q U A P O R I N → N o A T P ¥. L it h iu m ( 4 ) G lo m e r u l u f is lt er a t i o n ③ F IL T E R A T IO N A T h r o u gh P a r a c el l u la r s p a c es 0 P o d o c y te ¥ N e p h r on [ G F ] g lo m e r u l ac a p p i r l l a r y. B o w m a n n ep h r o n u r in e s u b cu t a n e o u i n sj e c t i o n ( in s u li n ) ⑦ c a p il l a r y B lo o d  E n d o c y t o s is ( P in o c y t o s) is 4 L a rg e ↳ # C el l D r in k in g P ro t ein ☁ B o t u l in u m t o x i→ n A b s o r b ed o r a l ¥ B (1 v i t a m i n ) Q Q : H el p of T r a n s p o r t e r s ⑤ C A R R IE R M e d ia t e d T r a n s p o r t F A C I L I T A T E D D if f u s i o n A C T I V E T R A N S P O R T c an C H ig h Low D c on c. m m A T P a s e L o w co n c. H ig h a n e. T r a n s p o r t er T r a n s p o r t er  N o A T P r e q u ir e d * T A P r e q u ir e d * A g a i n s t c o n c. g r a d i e n t A t h ce o n c g r a d ie n t ong e g. L e v o d o p a / m e t hd oy l p a F l u - u or ar c il o * N a t K + A T P a s e e. g T r a n s p o rt e rs : G L U T Q * P - G L coprtein Q C A S EI T E ¥ A T P b in di n g 2 0 2 3 A B C IN GET 2 0 2 2  Functio Locatin - - P - Placent Kidney GIT B : GLYCOPRTEIN ( intes EFLUX : : Remov : /liver ) : Transpote DRUG out excrtion Absorptin entry of organs Body Q /fetus D 4s Multi P - gp MRP DRUG - Transpute Resitan entr - protein Body MDR  Substrae ↓ ↑ Activy Activy of of of Pgp P - gp P - gp : P P - - gp gp. inhbtors inducers Digoxn : > CLARITHOMYN Rifampcn Erythomcin Ketocnazl AMIODRNE VERAPMIL Quinde Q. Q LO OPID = , DERAMI → → not not : Absored entr Non - B adicton GIT  Q Q se Clarithomyn Rifampcn you al : tomrw Reduc Increas excrtion Thanks ) ② l efct Routes efct Bioavlbty of of of Digoxn Digoxn Toxicty DRUG. NET 20 Anythmia ABSaphm INCET 20  2° Atpase 10 ATPase active active use Transpot Transt DISTRBUON PIN - med EP Multi AP - Resitan Protein MRP DRUG Resitanc Dry multi MDR.