AS DRUGS: Gastrointestinal Pharmacology (John Waddington)

Drug name Side effects Action Other

!"#$O%A$&!R P'"OR# (Amo)icillin* $larithromycin and acid su++ressant,
% &reatment: use Triple therapy: Two antibiotics (Amo)icillin and $larithromycin) and an acid suppressant
such as Proton pump inhibitor or H
2
antagonist .
PRO&O- PU.P #-#%#&ORS
Uses of Proton Pum+ inhi/itors: Triple therapy for peptic ulcer, gastroesophageal reflux, prophylaxis against
ulcer deelopment.
Ome+ra0ole !iarrhea, nausea, flatulence " #rreersible bloc$ing of
H%&'% (tpase )proton pump*
" prodrug actiated in acid pH

1
R!$!P&OR A-&AGO-#S& ($imetidine* Ranitidine,
#t competitiely bloc$s histamine induced acid release by parietal cells. There is less acid suppression than PP#s
because it only bloc$s histamine component. +lcer relapses once treatment stopped.
$imetidine " ,onfusions&drowsiness,
Headaches, rashese, diarrhea
" Hepatic&renal failure in
elderly
" #t inhibits cytochrome p-./
en0ymes.
" #t has antiandrogenic actiity.
1aises prolactin leels
2ynaecomastia:
enlargement of breasts in
males.
Ranitidine " 3ewer side effects " little&no inhibition of P-./
en0ymes and antiandrogenic
actiity.
$'&OPRO&!$&#2! AG!-&S (.iso+rostol* Sucralfate* %ismuth(
" ,ytoprotectie agents are used for mucosal barrier fortifying agents. (4ncourage mucosal barriers)
.iso+rostol " !iarrhea, uterine
contractions, thus,
contraindicated in pregnancy
" 56(#!s inhibit ,789 to
decrease prostaglandin
formation, thus, promote
ulceration. Therfore, you gie
this to high ris$ 56(#! user
" analogue of
Prostaglandin P249
Sucralfate " #t binds to ulcer base. #t has a
mucosal protecting action
through stimulation of P2 and
bicarbonate
" #t:s a polymer of
aluminium and sucrose
%ismuth " #t binds to ulcer base (inhibits
H.pylori).
" #t precipitates at acid ph to
protect mucosa and stimulates
P2 and bicarbonate production
" ,olloidal tripotassium
dicitratobismuthate
A-&A$#DS (Aluminium hydro)ide* .agnesium hydro)ide* Sodium %icar/onate,
These are wea$ bases used to neutrali0e gastric acid. 7ften used as symptom relief. These are used for non"ulcer
dyspepsia
Aluminum hydro)ide ,onstipation
.agnesium hydro)ide !iarrhea
Sodium /icar/onate (l$alosis
S&#.U"A-&S O3 G#& .O&#"#&' (.etoclo+ramide* Dom+eridone* $isa+ride,
.etoclo+ramide " 4xtrapyramidal side effects " !
2
dopamine antagonist
" #t stimulates gastric emptying
.HT
-
receptor"mediated
(ch release
Dom+eridone " Peripheral !
2
antagonist
" stimulates gastric emptying.
"increases lower esophageal
sphincter tone and increases
prolactin secretion
$isa+ride " 6timulates (ch release in
myenteric plexus of upper 2#T.
" #t stimulates gastric emptying.
; #ncreases lower esophageal
sphincter tone
Drug name Side effects Action Other
A-&#!.!&#$ DRUGS
(Anticholinergics* Antihistamines* Do+amine rece+tor antagonist* Serotin rece+tor antagonist*
$anna/inoid,
Anticholinergics
(yoscine)
(nticholinergic side effects " <uscurainic antagonist at
estibular nuclei (=5)
" <otion sic$ness of short
duration
" >ittle antiemetic effect
Antihistamine
($ycli0ine)
6edation as side effect " H9 antagonist at =5
" <otion sic$ness
" >ittle antiemetic effect
Do+amine rece+tor
antagonist
(Phenothia0ines*
%utyro+henones*
.etoclo+ramide*
Dom+eridone)
" 4xtrapyramidal side
effects to <etoclopramide
" !
2
antagonist used to depress
chemoreceptie trigger 0one
(,T?)
" !ecreases omitting
" !omperidone also
simulates 2#T motility. #t
also does not pass @@@
and increase prolactin
secretion
Serotin rece+tor
antagonist
(Ondansetron)
" ,onstipation and
headache
" #t depress ,T? function and
depress isceral afferents from
2#T
" #t decreases omiting
" ."HT
A
antagonists
" orally or by #.=.
infusion with cytotoxics
$anna/inoids
(-a/ilone)
" !rowsiness
" Pschological effects
" #t acts through cannabinoid
receptor
"#t decreases omiting due to
drugs stimulating ,T?
" BCtetrahydrocannabinol
analogue
#-3"A..A&OR' %OW!" D#S!AS!
(Aminosalicylates* $orticosteroids* #mmunos++resi4e agents* Antimicro/ials* &-3a #nhi/itors
$rohns disease: Transmural inflammationD panenteric (mouth to anus)D T53a
Ulcerati4e colitis: <ucosal and submucosal inflammationD 1ectum (always), colon (ariable)D immunological
mechanisms
%O&: diarrhea and bleeding, infectius factors, genetic factors
Aminosalicylates
(Sulfasala0ine*
.esalamine)
" 2#T disturbance
" Hypersensitiity 1xns
" #ts an anti"inflammatory
agents inhibiting leu$otriene&
prostaglandin formation
" 6ulfasala0ine (prodrug which
gies mesalamine as actie)
" ."aminosalicylates
$orticosteroids
(ydrocortisone*
Prednisolone*
%udesonide)
" typical steroid side effects
limit long"term use
" #t modulations immune system
" #nhibition of cyto$ine
production to induce remission
H,: #.=, topical
P6: orally, topical
@6: orally.
#mmunosu++resi4e
agents
(A0athio+rine*
.erca+to+urine*
$yclos+orine)
" Purine analogues inhibiting
nucleic acid synthesis for long
term maintenance.
" (0athiprine (Prodrug which
gies <ercaptopurine as actie)
" ,yclosporine (#.=. for
seere, resistant
ulceratie colitis)
Antimicro/ials
(.etronida0ole)
" #t interrupt bacterial role in
inflammatory process
&-3a inhi/itors
(#nfli)ima/)
" (ntibodies to inflammatory
effects of T53a in 2+T for
refractory ,rohn:s disease
" #nfliximab (#.=.)
Drug name Side effects Action Other
"A5A&#2!S
(Dietary 3i/re6/ul7 forming la)ati4es* Osmotic la)ati4es* $ontact6stimulant la)ati4es,
" These are the drugs which promote defecation.
<ain ,haracteristics: " They retain water and electrolytes in lumen ia hydrophilic&osmotic proterties: by E transit
ia E bul$. " F mucosal absorption of H
2
7 and electrolytes: E transit ia E bul$. " E intestinal motility: F H
2
7 and
electrolyte absorption ia direct effect to E transit
Dietary 3i/re6 %ul7
forming la)ati4es
(%ran8 methylcellulose*
is+aghula)
(derse effects such as
decrease absorption of
drugs, intestinal impaction
and obstruction, (!ry bul$)
esophageal obstruction.
" #t:s a fibre rich diet
" E stool mass ia component
polysaccharides and E transit
oer 9"G days
Osmotic la)ati4es
(.agnesium sul+hate*
magnesium hydro)ide*
sodium +hos+hate)
("actulose)
" 4ffects of first three are
that little is absorbed
" The first three E transit oer
9"A hours.
" >actulose is osmotically
actie disaccharide. #t E
transit oer 2"A days
$ontact6stimulant
la)ati4es
(Senna)
(%isacodyl)
" they directly stimulate
myenteric plexus&mucosa. #t
E permeability of mucosal
surface. #t coordinates
increase in mass moements
and decrease in
segmentation. E transit oer
H"I hours.
" 6enna: prodrug for
actie anthracine
deriatie
" bisacodyl:
suppository (inserted
into rectum) and E
transit oer 9."A/ mins
A-&#D#ARRO!A AG!-&S
Three main approaches:
9) <aintain fluid&electrolyte balance: oral rehydrationD 5a,l and glucose for infant diarrhea
2) +se of anti"infectie agents
A) +se of constipating agents
(bsorbent compounds: absorb fluids&toxins (9aolin* +ectin* aluminium hydro)ide)
7piates: E muscle tone and F propulsie moements. (lso, F sensory stimulation for defecation
reflex
o 7piate deriaties without ,56 effects and dependence liability of morphine:
Di+heno)ylate and "o+eramide