Drugs Used in Gastrointestinal Diseases

7/24/2019 Drugs Used in Gastrointestinal Diseases

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Dr. Francisca Diana A,M.Sc

DRUGS USED INGASTROINTESTINAL DISEASES


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OutlineDrugs used in acid-peptic diseasesPr !inetic agentAntie"etic

Antidiarr#ea$sLa%ati&esAntispas" dicDrug used ' r "isce$$ane us GI dis rder


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DRUG USED IN ACID-PEPTICDISEASE Acid neutralizing agents

Acid production inhibitor H2 antagonist

Proton-pump inhibitorsMucosal protective agentsOther acid suppressant


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GASTERTerdiri atas

BodiKardiaFundusKorpusPilorus

Cekun anKur!atura "inorKur!atura "a#or


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Mu! sa $a"(ung di(agi "en)adi tigadaera# e!s!resi *

Area g$andu$a !ardia "ense!resi"u!us dan pepsin gen.

Area g$andu$a !sinti! +parieta$"ense!resi i n , pepsin gen dan(i!ar( nat.

Area g$andu$a pi$ ri! "ense!resigastrin dan "u!us.


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Pepsin gen di!ata$isis $e# $ )adi pepsin,/aitu en0i" pr te $iti!U$!us pepti! di es 'agus, $a"(ung dandu denu" ter)adi apa(i$a pr du!si asa"$a"(ung dan pepsin tida! (eri"(ang dgnsiete" perta#anan gastr du dena$


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Schematic model for physiologic control of hydrogen ion (acid)secretion by the parietal cells of the gastric fundic glands


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A$id neutrali%in a ents&Anta$ids

Antacid tida! "engurangi & $u"e $ /angdi!e$uar!an $a"(ung tetapi peninggian P#a!an "enurun!an a!ti&itas pepsin.Antasid di(agi d$" 1 g $ ngan *

a. Antasid siste"i! * Natriu" (i!ar( nat+Na O 2 dia(s rpsi di d$" usus #a$usse#ingga "en/e(a(!an urin (ersi'at a$!a$is.

(. Antasid n nsiste"i! * Al(OH) 3, Mg(OH) 2,

a O 3 hampir tida! diabsorpsi dlm usus sehinggatida! menimbul!an al!alosis metaboli!"


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ombination o# Al(OH) 3 , Mg(OH) 2 , a O 3 ($simethicone)Pharmacod%namics&

'orm salt and ater

Promote mucosal de#ense b% stimulation o# Pproduction

*rug interaction&+nhibit absorption o# digoxin, phenytoin, cimetidine,

fluoroquinoloneome Al can be absorbed


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' ( re$eptor anta onistsimetidine, ranitidine, nizatidine, #amotidine

Pharmacod%namic&

educe acid secretion in 2 a%s : competitiveinhibition H2 receptor & modulate !"sresponse to gastrin & #ch

educe ./0 (at night) and 1/- /0 (da%time)


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' ( re$eptor anta onistsPharmaco!inetic&

rapidl% absorbed in intestinal lumenndergo 4 st pass metabolism ' 5 6/0

7 482 & 4-9 hrs, and d"o"a depend on dose, 4/ hrs inrecommended dose:limination& hepatic metab", glomerular #iltration#iltration ; renal tubular secretion

ross the placenta, secreted into breast mil!


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' ( re$eptor anta onistsa#et%&

:P&$arfarin, theophylline, phenitoin, lidocaine, quinidine, b%bloc ers, !a%channel bloc ers, ben'odia'epines

ompete ith procainamide f or renal tubular secretion


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' ( re$eptor anta onists


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Proton-pu"p in)i*itorsOmeprazole, esomeprazole, lansoprazole,

pantoprazole, rabeprazolePharmacod%namic&

Protonated ; concentrated in P canaliculi7he reactive cation binds covalentl% ith H8? A7Pase

educe /-.60, needs 3-9 da%s to return


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Proton-pu"p in)i*itorsPharmaco!inetic& absorbed in intestinal lumen

(available in enteric coated) An acid-labile lipoph%lic prodrug & need acidenvironment to be activated easil% di##use into

acidi#ied compartment (P canaliculi)7o be administered hour before mealHighl% protein bound

ndergo 4 st pass ; hepatic metabolism7 482 & 4,6 hr but acid inhibition last up to 29 hr @o renal elimination


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Proton-pu"p in)i*itorsa#et%&

:


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*rug interaction Alter absorption o# certain drugs Han%a omeprazol %g dpt menghambat a!tivitasenzim >P2 4. serta mengindu!si >P4A2(mening!at!an !lirens beberapa obatantipsi!oti!, ta!rin dan teo#ilin)


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Proton-pu"p in)i*itorsO3AT 3IOA4AILA3ILI

TAS+5

T 6+7AM

D sis $a0i" untu!peptic u$cer atauGERD

OMEPRA8OL 9:-;< :,< = >,< 1:-9: "g > !a$i se#ari

ESOMEPRA8OL ? @: >,1 = >,< 1: = 9: "g > !a$ise#ari

LAN8OPRA8OL @: >,< 2: "g > !a$i se#ari

PANTOPRA8OL >,: = >,B 9: "g > !a$i se#ari

RA3EPRA8OL - 1 1: "g > !a$i se#ari


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+u$osal prote$ti!e a ents

Sucralfate & A comple< o# sucrose salt $ sul#ated AlOH

#orms a paste that selectivel% cover ulcers8erosionsPharmaco!inetic&

Almost unabsorbed=rea!ing do n into sucrose sul#ate ; Al salt

Pharmacod%namic&'orming ph%sical barrier so that prevent #urther causticdamage stimulate mucosal P ; H O3 secretion:nhancing mucosal repair

*rug interaction&+nhibit absorption o# digo


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+u$osal de,ense en)an$ina entsismuth compoundsPharmacod%namic& 5 sucral#ate

timulate P , mucus, bicarbonat secretionrostaglandin analog: misoprostol

A meth%l analog o# P : 4

Pharmaco!inetic& 7 482 & 3/ mnts 3-9 times dail%Pharmacod%namic& stimulates mucus and bicarbonat secretion

:& diarrhea, abdominal cramp (4/-2/0), stimulateuterine contraction

*osis : oral, de asa 2// mg 9 !ali8sehari atau 9// mg 2!ali8hari"

+ndi asi : usia lanCut atau perdarahan saluran cerna a!ibat A+@


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26/44echanism of action of dru used in acid e tic disease


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PROKINETIC AGENTS Agents that enhance coordinated + motilit% and transitsmaterial in the + tract

holinomimetic=ethanechol@eostigmin meth%lsul#ate

*opamine receptor antagonistMetoclopramidedomperidon

erotonin (6-H7 9 ) receptor agonistisapride, prucalopride

Motilin agonistMacrolides& er%throm%cin


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PROKINETIC AGENTSide e##ects&Metoclopramide

:


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PROKINETIC AGENTS

7herapeutic use&: *+mpaired gastric empt%ing

Postvagotom%*iabetic gastroparesis@ 7-ed patients

*%spepsia s%ndrome (non-ulcers)

AntiemeticPersistent hiccup (metoclopramide)


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EAFA7+G:


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timulant la


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timulant la


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=ul! #orming la


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PELEM3E TIN7A3e!er)a dengan "ening!at!an u!uran tin)adan "e$e"(e!!an tin)a tanpa "erangsangperista$ti! usus (ai! $angsung "aupuntida! $angsung se#ingga "uda#di!e$uar!an.

nt # * Para n cair, Na d !usat , g$/cerinsupp, para n cair +"inera$ i$


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Osmotic la


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AE+@: EAFA7+G:Merupa!an gara" n n rgani! /ang"engandung !ati n atau ani n dan tida! segeradia(s rpsi "u! sa usus !arena cenderung(erta#an di sa$uran cerna.Perista$ti! usus "ening!at dise(a(!an pengaru#td! $angsung !arena da/a s" ti!n/a.Air ditari! !e d$" $u"en usus dan tin)a "en)adi

$e"(e! sete$a# 2 = ; )a".A(s rpsi penca#ar gara" "e$a$ui usus(er$angsung $a"(at dan tida! se"purna.

nt # * magnesium citrate, sodium phosphate


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+e$)anis" o, a$tion o, la ati!es


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ANTIE+ETIC

4" erotonin (6-H73) receptors antagonistOndansetron, granisetron, ramosetron, palanosetron,

dolasetron

2" *opamine antagonist& Meto!lopramide, domperidon3" H4-antagonist & %clizine, Promethazine,

prochlorperazine, PK9" Anti!olinergics& copolamine

6" annabioid antagonist& *ronabinol


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ANTIDIARR'EA

4" Opioid agonist2" olloidal bismuth compound

3" ?aolin (h%drated Mg-Al silicate) ; pectin(indigestible ?H)9" =ile salt-binding resin6" Octreotide


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antidiareP)ar"a$od#na"i$ Side e.e$ts

Opi id+L pera"ide,Dip#en %/$ate,

c dein

In#i(it pres/napticc# $inergic ner&e, reduceperista$tic acti&it/

Increase transit ti"e Decrease "ass c $ nic

" &e"ents

c nstipati n, cra"ps,dr siness, para$/tic i$eus,a(d "ina$ ($ ating.

Dip#en %/$ate, (ut n t$ pera"ide, pr duce eup# riadan respirat r/ depressi n

$$ ida$ (is"ut#c "p und

direct anti"icr (ia$e ects and (indsenter t %ins

Dar! st $s, ($ac! staining 't#e t unge

a $in H pectin ads r(ents ' (acteria$t %ins and uid, t#ere(/decreasing st $ $iJuidit/and nu"(er.

a&e n signi cant ad&ersee ect e%cept c nstipati n.S# u$d n t (e ta!en it#in 1# urs ' t#er "edicati n

3i$e sa$t-(inding resin

+ # $estira"ine,$estip $,

c $ese&a$a"

(inds (i$e sa$ts and

increases 'eca$ e%creti n '(i$e acids

3$ ating, atu$ence,

c nstipati nFat "a$a(s rpti nS# u$d n t (e ta!en it#in 1# urs ' t#er "edicati n

S "at statin-$i!e+Octre tide

reduces intestina$ uidsecreti n H pancreatic

secreti n s$ s GI " ti$it/, in#i(it

Steat rr#ea, nausea,($ ating

Fat-s $u($e &ita"inde cienc/


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ANTIPAS+ODIC

4" AnticholinergicH%osc%amine, *ic%clomine

2" erotonin (6-H7 3 ) receptor antagonist

Alosetron+ndication&

to prevent the pain and #ecal urgenc%

inpatient ith += treatment o# diarrhea-predominant +=


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Dru used ,or "is$ellaneous GIdisorder4" Pancreatic enz%mes& pancreatin,

pancrelipasehronic pancreatitis

Malabsorption2" =ile acids& ursodeo


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Re'erencesMc uaid R. Drugs used in t#e treat"ent ' Gastr intestina$diseases. In* Kat%un 3G, Masters S3, and Tre& r A7. 3asicand c$inica$ p#ar"ac $ g/. >> t# ed. Singapure. McGra i$$C1::B. p.>:; -B@.

a$$ace 7L, S#ar!e/ A. P#ar"ac t#erap/ ' gastric acidit/,peptic u$cers, and gastr es p#agea$ re u% disease. In*Good"an / Gil"an0s t#e p#ar"ac $ gica$ (asis 't#erapeutics. >1 t# ed. Ne r!* McGra i$$C 1:>>. p. >2:B-1>.

a$$ace 7L, S#ar!e/ A. Treat"ent ' dis rders ' ( e$" ti$it/ and ater u%C antie"eticsC agents used in (i$iar/ andpancreatic disease. In* Good"an / Gil"an0s t#e

p#ar"ac $ gica$ (asis ' t#erapeutics. >1t#

ed. Ne r!*McGra i$$C 1:>>. p. >212-9B.Page , urtis M, a$!er M, "an 3. Integratedp#ar"ac $ g/. 2 rd ed. Spain. E$se&ier M s(/C 1::;.p.9


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Drugs Used in Gastrointestinal Diseases

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