ANTIDIARRHEALS

DR.dr.Asep Sukohar, M.Kes

Or, If You Prefer, These 4 Flavors
Viral Protozoan
CMV, Rota, adeno,
enterovirus, Norwalk

Giardia, Amy the
Ameba, Cryptosporidium
Invasive Toxicogenic/Secretory
E. Coli 0157:H7, Shigella
Salmonella, Vibrios,
Campy Low-Backed Her,
Your Sin Yee-Hah
Staph, noninvasive E.
Coli, Be Serious, C.
Difficile, Cholera
*lumps together invasive, inflammatory, non-amebic dysenteries, etc.
Invasive vs. Noninvase
INVASIVE NONINVASIVE
Heme Positive Heme Negative
Shigella and Salmonella ETEC, EPEC
Campylobacter Cholera (V. cholerae)
Entameba histolytica Other Vibrios
Yersinia enterocolitica Clostridium perfringens
EHEC Be Serious!
Norwalk Giardia
Cryptosporidia
Rota, parvovirus, weird
protists
Anti diarrheal drugs include :
anti motility agents
adsorbents
drugs that modify fluid and electrolyte
transport
Antimotility and antisecretory agents

Loperamide
an orally active antidiarrheal agent
40-50 x > potent than morphine as an
antidiarrheal agents and penetrates the CNS
poorly
has antisecretory activity against cholera toxin
and some forms of E.coli toxin
effective and safe marketed for OTC
distribution and is available in capsule,
solution, chewable forms
Pharmacokinetic :
its act quickly following an oral use, Tmax = 3-5
hours,
t1/2 = 11 hours, extensive hepatic metabolism
Therapeutic uses :
effective against traveler's diarrhea, used either alone
or in combination with antimicrobial agents
(trimethoprim, cotrimoxazole , fluoroquinolone).
If clinical improvement in acute diarrhea does not
occur within 48 hours, loperamide should be
discontinued.
adjunct treatment in almost all forms of chronic
diarrheal disease.
should not be used in children younger than 2 years
of age
- Side effects & overdosage :

lacks significant abuse potential
overdosage CNS depression and paralytic
ileus
children > sensitive than adults to the CNS-
depressants effects of loperamide
in patients with active inflammatory disease of
the colon, loperamide should be used with great
caution to prevent development of toxic
megacolon.
Diphenoxylate and Difenoxin
structurally related to meperidine
difenoxin is the active metabolite of diphenoxylate and
also is used as such to treat diarrhea
as antidiarrheal agents, diphenoxylate and difenoxin >
potent than morphine
Pharmacokinetic :
- extensively absorbed after oral administration, Tmax = 1-2 hours
deesterified
diphenoxylate -----------------> difenoxin , t
1/2
=12 hours
- higher doses (40-60 mg per day) CNS effects
potential for abuse and/or addiction
- available in preparations containing small doses of
atropine to discourage abuse and deliberate overdosage
Adsorbents

Adsorbent agents such as kaolin, pectin,
methylcellulose and activated attapulgite,
magnesium aluminum silicate widely
used to control diarrhea.
These agents act by adsorbing intestinal
toxins or microorganisms, or by coating or
protecting the intestinal mucosa.
Less effective than antimotility agents and
can interfere with absorption of other
drugs.
Agents that modify fluid and electrolyte
transport

NSAIDs :
Acetosal and indomethacin are effective
in controlling diarrhea This
antidiarrheal action is probably due to
inhibition of prostaglandin synthesis.
Bismuth subsalicylate
(PEPTO-BISMOL) :
Antisecretory, antiinflammatory, and
antimicrobial effects, nausea and
abdominal cramps also may be relieved.

effectively for the prevention and
treatment of traveler's diarrhea , but it
also may be effective in other forms of
nonsyndromic, episodic diarrhea.