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Pharmacotherapy of gastro instinal

disorder
1. Antasida
2. Antagonis reseptor histamine 2 dan Proton bloker
3. Spasmolytic (anti spasmodic)
4. Laxantia
5. Diare non spesifik
6. Infection located in gastro intestinal
7. Kolelitolytic and Hemorhoid drug
8. Hepatoprotektor and Regulator gastrointestinal tract.

1. Antasida is a group of drug can decrease gaster acidity


Weak alkaline.do not decrese acid production
Decrease acid capacity depends on type of antasida , intake frequency and “
velocity of emptying gaster
Increase Ph causes decrease pepsin activefity

A. Na HCO3
- Antasida sistemik.,urine alkalis,alkalis metabolic
- Poten antasid ,on set of action ,fast and short duration
- Yield CO2 buble ,gaster distension ,Tablet 500 mg,dosis 1-4 gr
B. Al(OH)3
- Non sistemik antasida
- On set of cation slow, long action/ duration
- React with phosphat ( come from food),with protein became
adstrigen
- Pepsin no active, cause constipation
- Decrease adsorbtion vitamin and Tetrasiklin
- Tablet 600 mg dan suspensi 3,6-4,4 %
C. CaCO3
- Poten Antasida, partly absorbtion
- On set of cation fast, long acting
- cause acid rebound, Constipation,nausea,vomiting
- Tablet 600 mg,dosis 1-2 gr

D. Mg(OH)2 and Mg CO3


- Onset of action slow
- Absorbtion 5 -10%, can cause diare
- Ca cause CV.neurologik and neuromuskuler disorder,alkaliuri
- Tablet 325 mg dan suspensi 7-8,5% Mg(OH)2
Mg trisilikat
Mg2Si308 nH20 + H+ ------2Mg++ + 3SiO2 + (n+2) H2O
- SiO2 to form gel covers ulcus, adsorb gas
- Weak antasida ,slow ation and long action/duration
- Absorb protein and Fe from food ,Mg causes alkaliuri,can cause
siliceous nephrolithiasis
- Tablet 500 mg.forming polimer calls simetikon,polisiloksan

2. Antagonis Reseptor Histamin 2 and Proton bloker


If reseptor H2 isfilled with histamine in gaster causes gaster enzym and H+ .Intake
antagonis H2 causes inhibits secretion. Reseptors H2 are found at anather organ ,
cause side effects
- Simetidine ;
Take place reseptor androgen causes gynecomastia dan disfungsi seksual
Ranitidin dan famotidin donot have this effect
Simetidine reacts with sitokrom PP-450 and inhibits metabolism anather drugs
Avaiable Simetidin 200 mg tablet,Ranitidin 150 mg,and famotidin 20 mg
- Omoperazole,
Proton pump inhibitor at gaster
Decrease production HCl and causes sleepy
Granul 20 mg in kapsul

3. ANTISPASMODIK
Anti kolinergik no efek sentral only at perifer. Anti muskarinik.p-simpatikolytik
Protipe Atropin, syntetik drug is compared with Atropin also side effects.
Farmakodinami ; COV : 0,5 mg stimulsi SSP, greater dosage causes depresi.
Skopolamin euphoria, amnesia, sleepy Eyes ; midriasis ,contracted m.constrictor
pupilae,m.ciliaris
CVO : 2 mg inhibit n.vagus GIT tract : relaxns smooth muscle
Urinary tract : Smooth muscle relaxation .m.detrusor dan contract sfingter
Eksokrin gland ; hyposecretion
Anti spasmodic : 1.Papaverin tab 40 mg, 2.Atropin 0,25 mg /tab 3. Ekstrak Belladon
10 mg/tab 4. Skopolamin 1 mg/tab 5. Clidium 2,5 mg tab
6. Butropium Br 5 mg/tab Hiosin n-butilbromida 10 mg/tab
7. Skopolamin metilbromida 1 mg/tab

4. Obat Konstipasi /Laksans


To accelerate defekasi
a. Stimulant laxans , stimulans mukosa, intramural nerve , intestine smooth muscle ,
increase peristaltic.mucus secretion
- Oleum recini ,zat aktip asam resinolat , effect appear after 3 hours (laten time)
- Difenilmektan (p.p) ,antrakinon laten time 6 jam
Come from leaf of cassia angustifolia Tree,bark Rhamnus pursiana
- Bisakodil drags 10 mg laten time 6-12 houres,available in supp preparation.
b. Salt laxans
- Mg SO4, 30 gr
Increase fluid osmotic pressure intestine lumen example disakarida,laktulosa
Avaialble in syrup 10 gr/15 ml
c. Mass Laxans
Absorb water and ion in colon lumen , example. metilcellulosa,effect after 12-
24 jam
Agar agar,coloid hidrofil,hemisellulosa
d. Pencahar emolien
Soften faeces , decrease surface tension , exmp
Dioktil Na sulfosuksinat 24-48 jam
Parafin liquid : Water Reabsorbsi decrease , disturb vitamin absorbtion and lipid
Na lauryl`sulfoasetat ,sorbitol,glyseropolyethylen.use as enema per rectal

5. Diare drug non spesifik


- narkotik effect , example Loperamid 2 mg ,absorbtion in GET, inhibits peristaltic

- Local effect,adsorbsion toksin,adstrigen


* Norit (karbon adsorben),Kaolin derived silikat
* Pektin function as coagulating effect, adsorb water
* Attapulgit

6. Obat infeksi saluran cerna


a. Tetrasiklin b. Kloramfenikol c. Nitromidazol
A. Tetrasiklin
Come from ( original ) fungi Str.aureofaciens produces Klortetrasiklin
Str. Rimosus produces oksitetrasiklin
Example ; tetrasiklin,Doksisiklin,Minosiklin,Demetilklortetrasiklin
MA : inhibit syntesis protein,bakteriostatic.Broad Spektrum antimicroba
Farmacokinetik :30-80 % Tetrasiklin is absorbed in gastrointestinal,
Minosiklin and Doksisiklin
Absorbsion 90 persen, at upper intestine and gaster
Distrub with food, ph high ph and with
Antasida construct compleks (kelat ). exctretion pass ren
Classification : Poor absorbstion half life 6-9 hours: tetrasiklin,Klortetrasiklin
Oksitetrasiklin dosage 4 times 250 -500 mg
Good absorbtion half life 16 hours Dosis 150 mg every 6 jam :
Demetilklortetrasiklin
Excellent absorbtion , half life 17-20 hours:Dosis100 g 2 times daily
Minosiklin,Doksisiklin
Deposie in bone became brown color until gray at teeth
.Damage Tetrasiklin became anhidro 4 epitetrasiklin
Sympton ; poliuri,polidipsia,proteinuria,nausea, vomiting, rens distrubs calls
Fanconi syndrome . using for Shiegella infection bisa juga menggunakan
cotrimoxazole (gabungan tranetophrin dan sulmametahzole)
B. Kloramfenikol
Come from Str. Venezuelae strong anti mikroba , inhibit protein syntetic with
interfere enzyme peptidil transferase. Bakteriosastik , can make anemia
Aplastik. Avaiable in palmintat dan stearat,kapsul 250 mg dan 500 mg.
good absorbsion in GET metabolism in hepar with conyugation acid
Glukoronat. Excretion pass ren
Side effect : 1. Concentration > 25 ug/ml deprsion bone narrow
Healing after drug stop
2. idiosinkrasi like anemiaplasik
3. Sindroma Gray if given in case neonatus premature
indication : salmonella typhi
Thiamphenicol : derivate Chloramphenicol
More safe than Kloramfenikol with out anemia apalstik

9. Hepatoprotektor dan regulator saluran cerna


Example : methionin, lecithine,curcumin as hepatoprotektor
Methionin is amino acid esensiale .make cholin.Cholin + gliserofosfat+ fatty acid
make lecithin one lipoprotein work as fat transport in blood
Efective as lipotropic
Regulator gastro intestinal
Metoclopramid

M.A 1. potensiasi with kolinergik drug


2. direct at smooth muscle intestine
3. Inhibit dopaminergik central
G.I.T : - Enhance tonus sfingter esophagus distal
- Enhance contraction gaster part antrum
- To corect coordination contraction antrum and duodenum
Accelerate gaster move to duodenum
contraction smooth muscle.
Sentral : anti emetic is caused effec central and perifer. Increase ambang
Ambang rangsang vomiting center in CTZ. At perifer decrease
sensivity
Visceral nerve yang menghantar impuls aferen dari sal.cerna ke
pusat muntah
Antagonis dopamine sentral merupakan dasar anti emetic dan gejala
ekxtrapi-
ramidal..Stimulate sekresi prolaktin memperbaiki laktasi.
Not use at obstruction, bleeding ,perforasi GET
Tablet dan injeksi 5 mg,10 mg
Domperidone
Derivated benzimidazolin antagonis dopamine like klorpromazin.
Mekanism anti vomting : inhibit refluks esophagus, increases tonus sfingter
And Esophagus part decendens. There is no central effect
Avaiable as ;tablet 10 mg dan syrup,dan supp.
Cisepride derivate dari domperidone
Kolelitolytik : Chenodeoxycholic acid, ursodeoxycholic acid (Urdaflak)
Obat hemorohoid :
Bismuth sub gallat,Bismuth subnitrat,Cinchonin(Borraginol)
Anusol , Anusol (H) zat adstrigent + Hydocortison
Ultraproct supp. (lidocain + adstrigent + Fluocortolone (steroid0

Drug for virus hepatitis


Hepatitis B chronic : Analog nucleotide : Entecavir (Baraclude), Adefovir
dipivoxil (Hepera) ,Tebivudine (Sebuvo),Lamividine (3TC)

Hepatitis C kronik : Glikoprotein endogen : interferon alfamtive alfa


Drug for Pararasit/Protozoa : Mebendazole

Kristal yellow water soluble, available in oral and parenteral.


Dosage : 3 x daily 500mg. CHILDREN 30-50 /kgBW daily

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