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Pharmacology semester 1
Pharm GI
Antidiarrheals
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Antidiarrheal overview
Three main classes of drugs are used for diarrhea
absorbent preparations,
opiates
, and
anticholinergics
Antidiarrheal examples
Absorbents: Pepto-Bismol,
Kaopectate
Opiates:
diphenoxylate-atropine
(Lomotil),
difenoxin-atropine
(Motofen, loperamide (immodium)
anticholinergics:
Alosetron
(
Lotronex
)
Kaolin
clay like powder that attracts and holds onto
bacteria
and
thickens
the stool
Pepto-Bismol
antisecretory effects which causes
less
secretions in the stool
Diphenoxylate-atropine
decreases
secretion and slows
peristalsis
is an
opiate
and can cause
opiate
like efects
Loperamide
slows
peristalsis
reduces
fecal volume and
increases
bulk
reduces
absorption of fluid
Pharmacotherapeutics of antidiarrheals
drugs that delay gastric motility are contraindicated in
liver
and
renal impairment
due to risk of toxic megacolon
Atropine is contraindicated in
narrow angle glaucoma
and down syndrome and
children
Bismuth is contraindicated in
children
who are recovering from
URI
eluxadoline
could cause
pancreatitis
Alosetron
is contraindicated in
constipation
Adverse drug reactions antidiarrheals
constipation
diphenoxylate-atropine can cause anticholinergic symptoms such as
dry mouth
, flushing, tachycardia, and
urinary retention
, dizziness, and drowsiness
nausea
/
vomiting
Use and dosing of antidiarrheals
Absorbents
: taken after each loose stool
chronic diarrhea with IBS:
steroids
and
sulfasalazine
, loperamide
IBS: loperamide
Infantile diarrhea:
bismuth salicylate 2.5
mL q 4 hours for
2-24
months and 5 mL
travelers diarrhea:
bismuth subsalicylate
Education of antidiarrheals
take as
prescribed
, do not double dose or take extra
doses
Adverse reactions of antidiarrheals
Constipation
bismuth
can turn tongue and stool
gray
or black
diphenoxylate
can cause anticholinergic effects
crofelemer
may cause
upper
respiratory infection
Lifestyle changes with
antidiarrheal
adding
fiber
wash hands
fasting
to rest the
GI tract
avoid foods that cause
diarrhea
Crofelemer
is indicated for patients on antiretroviral therapy
Anticholinergic antidiarrheals such as atropine/difenoxin are contraindicated in
narrow
angle
glaucoma
atropine is
contraindicated
in children, especially those with
down-syndrome
bismuth subsalicylate is contraindicated in patients with a history of
asthma
and
aspirin
sensitivity
pancreatitis
is an adverse effect of eluxadoline
alosetron
is contraindicated in patients with
hepatic impairment
and has a black box warning
Kaolin/pectin is
safe
in pregnancy
Bismuth subsalicylate may increase risk of
aspirin
toxicity
diphenoxylate, atropine, and loperamide all have
additive
or
potentiating
CNS effects
Absorbent preparations are commonly used in
acute
diarrhea
Children with severe diarrhea need
oral rehydrating
solutions
Loperamide
is generally given for IBS associated diarrhea
All patients should be cautioned about
rebound constipation
when discontinuing medication
diphenoxylate can cause
anticholinergic
symptoms such as dr y
mouth
,
tachycardia
, and
urinary retention
eluxadoline
may cause pancreatitis