Rational Use of Drugs Part II - How Do Drugs Get Into the Bo

7/24/2019 Rational Use of Drugs Part II - How Do Drugs Get Into the Bo

1/24

HOW DO DRUGS GET

INTO THE BODY?


2/24

WHY BE CONCERNED ABOUT

HOW DRUGS GET INTO BODY?

Bioavailability - % of dos t!at "ts i#to body

Bio$ival#& - si'ila(ity bt)# t)o fo('latio#s of sa' d("

S*d of D(" O#st - !o) lo#" it ta+s t! d(" to b"i# )o(+i#"

Dosi#" I#t(val - !o) oft# t! d(" s!old b "iv#

Sit of A&tio# - )!t!( t! d(" stays lo&al o( a&ts syst'i&ally

T!is iss i'*o(ta#tly aff&ts,


3/24

HOW DO DRUGS GET

INTO THE BODY?

U#lss i#&td di(&tly i#to t! blood st(a'.

d("s 'st b abso(bd/


4/24

WHAT IS DRUG ABSOR0TION?

T! 'ov'#t of d(" 'ol&ls a&(oss biolo"i&al

ba((i(s 1'ostly lay(s of &lls2 f(o' t! sit of

ad'i#ist(atio# to t! blood st(a'/

BIO3OG

ICA3BARRIER 4as&la( Syst'Sit of Ad'i#ist(atio#

DRUG


5/24

WHAT A55ECTS DRUG ABSOR0TION?

Rat of (las of d(" f(o' *!a('a&ti&al *(*a(atio#

6'b(a# *('ability of d("

S(fa& a(a i# &o#ta&t )it! d("

Blood flo) to sit of abso(*tio#

Dst(&tio# of d(" at o( #a( sit of abso(*tio#

T! (at of d(" abso(*tio# )ill b aff&td by,


6/24

WHAT DETER6INES RATE O5

RE3EASE O5 DRUG 5RO6

0HAR6ACEUTICA3

0RE0ARATION?

Soltio#s, No Dlay. I''diat Rlas

Ca*sls 7 Tabls, Dlay 1Dissoltio#2 5ollo)d by Ra*id Rlas

C(a's. Oi#t'#ts 7 S**osito(is, No Dlay. bt Slo) Rlas

A, DOSAGE 5OR6


7/24



0HAR6ACEUTICA3

0RE0ARATION?

D&(as Rat of

Dissoltio#

Bi#d(s

3b(i&a#tsCoati#" A"#ts

B, ADDITI4ES 1E8CI0IENTS2

I#&(as Rat of

Dissoltio#

Disi#t"(a#ts

4a(iabl Eff&ts o#

Rat of Dissoltio#

Dil#ts

Colo(i#" A"#ts5lavo(i#" A"#ts


8/24



0HAR6ACEUTICA3

0RE0ARTAION?

Tablt Co'*(ssio# - Ha(d tablts dissolv 'o( slo)ly

Tablt S!a* - Ro#d tablts dissolv 'o( slo)ly

Tablt Si9 - 3a(" tablts dissolv 'o( slo)ly

C, 6ANU5ACTURING 0ARA6ETERS


9/24



0HAR6ACEUTICA3

0RE0ARATION?

E#t(i& Coati#" - Dissolv i# i#tsti#s. #ot sto'a&!

D, DE3AYED RE3EASE 0RE0ARATIONS


10/24



0HAR6ACEUTICA30RE0ARATION?

Reservoir Diffusion Products- D(" diffss f(o' *ill &o(t!(o"! ''b(a# s!ll

Matrix Diffusion Products- D(" diffss t!(o"! 'at(i:

i# )!i&! it is 'bddd

Matrix Dissolution Products- D(" (lasd as 'at(i: dissolvs

Osmotic Tablets- D(" *'*d ot of tablt by os'oti& fo(&sIon-Exchange Products- D(" bo#d to (si# :&!a#"s

)it! #do"#os io#s

E, SUSTANED RE3EASE 0RE0ARATIONS


11/24

WHAT DETER6INES 6E6BRANE

0ER6EABI3ITY O5 DRUGS?

0(s#& of Ali*!ati& a#d A(o'ati& St(&t(s

Abs#& of 0ola( G(o*s

A, 3I0O0HI3ICITY i#&(ass ''b(a#

*('ability


12/24

WHAT DETER6INES 6E6BRANE

0ER6EABI3ITY O5 DRUGS?

Wa+ a&ids i# i#tsti#s a( 'ostly io#i9d

1i#tsti#al *H (a#"s f(o' ;/; to to 2

B, IONI@ATION d&(ass ''b(a#

*('ability


13/24

WHAT DETER6INES SUR5ACE

AREA 5OR ABSOR0TION?

3o) S(fa& A(a,ys. #asal &avity. b&&al &avity. (&t'. sto'a&!. la(" i#tsti#s

Hi"! S(fa& A(a

s'all i#tsti#s. l#"s

ANATO6Y


14/24

WHAT DETER6INES

TISSUE B3OOD 53OW?

3o) Blood 5lo),ys. sto'a&!. la(" i#tsti#s.

(&t'. sb&ta#os tiss

Hi"! Blood 5lo)

s'all i#tsti#s. l#"s. 's&l. b&&al &avity. #asal &avity

A/ 0HYSIO3OGY


15/24

WHAT DETER6INES

TISSUE B3OOD 53OW?

So' D("s A( 4aso&o#st(i&to(s

So' D("s A( Co-Ad'i#ist(d Wit! 4aso&o#st(i&to(s

So' D("s A( 4asodilato(s

B/ 0HAR6ACO3OGY


16/24

WHAT DETER6INES

WHETHER A DRUG IS DESTROYED

AT OR NEAR SITE O5 AD6INISTRATION?

3iv( - !*ati& #9y's 1fi(st *ass ff&t2

Colo# - i#tsti#al 'i&(oflo(a

Sto'a&! - di"stiv #9y's a#d a&ids

BIOCHE6ISTRY


17/24

WHAT ARE THE ROUTES O5

AD6INISTRATION 5OR DRUGS?

O(al

Sbli#"al

R&tal

ENTERA3

I#t(av#os 1I42

I#t(a-a(t(ial 1IA2Sb&ta#os 1SC2

I#t(ad('al 1ID2

I#t(a's&la( 1I62

I#t(a*(ito#al 1I02

3#"s 1I#!alatio#2S+i# 1To*i&al2

0ARENTERA3

Nos 1I#t(a#asal2

Ey 1O*t!al'i&2 Ea( 1Oti&2

4a"i#a

U(t!(a

U(i#a(y Bladd(

I#t(at!&alE*id(al

Di(&tly I#to Ta("t Tiss


18/24

3o)Hi"!

Hi"!

WHAT ARE THE AD4ANTAGES AND DISAD4ANTAGES O5

ORA3. I4. I6 AND SC AD6INISTRATION?

SA5ETY

Hi"! 3o)O(al SC I6 I4

O(al SC I6 I4

CON4ENIENCE

3o)

COSTI4 I6 SC ORA3


19/24

3o)Hi"!

DlaydI''diat



BIOA4AI3ABI3ITY

Hi"! a#d Rliabl 3o) a#do( 4a(iablI4 I6 SC ORA3

I4 I6 SC O(al

ONSET O5 ACTION

0ATIENT CO603IANCEI4 I6 SC O(al


20/24

3o)Hi"!

3o)Hi"!



INTERACTIONS WITH 5OOD

Ris+ No Ris+ O(al I4 I6 SC

O(al I6 SC I4

CO66ERCIA3 A4AI3ABI3ITY O5 DOSAGE 5OR6S

4O3U6E O5 DRUGO(al I4 I6 SC


21/24

3o)Hi"!



A4AI3ABI3ITY O5 SUSTAINED RE3EASE

DOSAGE 5OR6S

Hi"! 3o)I6 O(al SC I4

TO3ERANCE TO 5UNFY 4EHIC3ES

O(al I6 SC I4


22/24

WHY CONSIDER OTHER ROUTES O5

AD6INISTRATION?

Sbli#"al - Ra*id abso(*tio#

t!at by*asss liv(

R&tal - G(at fo( *ati#t t!at

is vo'iti#" o( &a##ot 1)ill #ot2

s)allo) 'di&atio#


23/24

WHY CONSIDER OTHER ROUTES O5

AD6INISTRATION?

3#"s 1I#!alatio#2S+i# 1To*i&al2

Nos 1I#t(a#asal2

Ey 1O*t!al'i&2

Ea( 1Oti&2

4a"i#a

U(t!(a

U(i#a(y Bladd(

I#t(at!&al

E*id(al

Di(&tly I#to Ta("t Tiss

IS O5TEN DESIRAB3E TO CONCENTRATE

6EDICATION AT TARGET SITE TO

INCREASE E55ICACY AND

DECREASE TO8ICITY

1T! *(*os !( is to li'it syst'i& abso(*tio#2


24/24

No) yo +#o)

HOW DO DRUGS GET

INTO THE BODY?

Rational Use of Drugs Part II - How Do Drugs Get Into the Bo

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