Rational Use of Drugs Part II - How Do Drugs Get Into the Bo
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Transcript of Rational Use of Drugs Part II - How Do Drugs Get Into the Bo
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7/24/2019 Rational Use of Drugs Part II - How Do Drugs Get Into the Bo
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HOW DO DRUGS GET
INTO THE BODY?
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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,
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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/
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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
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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,
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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
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WHAT DETER6INES RATE O5
RE3EASE O5 DRUG 5RO6
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
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WHAT DETER6INES RATE O5
RE3EASE O5 DRUG 5RO6
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
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WHAT DETER6INES RATE O5
RE3EASE O5 DRUG 5RO6
0HAR6ACEUTICA3
0RE0ARATION?
E#t(i& Coati#" - Dissolv i# i#tsti#s. #ot sto'a&!
D, DE3AYED RE3EASE 0RE0ARATIONS
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WHAT DETER6INES RATE O5
RE3EASE O5 DRUG 5RO6
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
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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
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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
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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
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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
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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
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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
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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
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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
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3o)Hi"!
DlaydI''diat
WHAT ARE THE AD4ANTAGES AND DISAD4ANTAGES O5
ORA3. I4. I6 AND SC AD6INISTRATION?
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
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3o)Hi"!
3o)Hi"!
WHAT ARE THE AD4ANTAGES AND DISAD4ANTAGES O5
ORA3. I4. I6 AND SC AD6INISTRATION?
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
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3o)Hi"!
WHAT ARE THE AD4ANTAGES AND DISAD4ANTAGES O5
ORA3. I4. I6 AND SC AD6INISTRATION?
A4AI3ABI3ITY O5 SUSTAINED RE3EASE
DOSAGE 5OR6S
Hi"! 3o)I6 O(al SC I4
TO3ERANCE TO 5UNFY 4EHIC3ES
O(al I6 SC I4
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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#
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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
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No) yo +#o)
HOW DO DRUGS GET
INTO THE BODY?