Transcript Diarrhoea Loperamide

Anti-diarrheals-II
Opioids
Loperamide, Morphine, Codeine
Mode of action:
1. increase tone of both small and large
bowel and reduce intestinal motility
(enhances fluid and electrolyte reabsorption);
2. increase the sphincter tone and
decrease secretory activity along GIT
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Loperamide
It is a synthetic opioid agonist that has a
high affinity for, and exerts a direct action
on  opiate receptors in the gut wall;
also has a high first-pass metabolism so
very little reaches the systemic circulation;
effective in reducing the duration of
diarrhea (25 vs 40 hrs with placebo)
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Loperamide
50 fold more potent than morphine and 23 times more potent than diphenoxylate in
its effect on GI motility, but penetrates the
CNS poorly, thus has lower risk of CNS
side effects;
Other mechanisms: 1. disruption of
cholinergic and non-cholinergic
mechanisms of peristalsis, 2. inhibition of
calmodulin function and 3. inhibition of
voltage dependent Ca channels
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Loperamide
Indications:
traveller’s diarrhoea
non-specific acute diarrhoea
chronic diarrhoea associated with inflammatory
bowel disease
AAP does not recommend use in children < 6
years old
Used when patient is afebrile or have mild fever
and does not have bloody stool
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Loperamide
Dosage & Administration
dosage forms: caplets (2 mg), and liquid
(1 mg/5ml)
Dose: 4 mg initially, then 2 mg after each
loose stool/ Do not exceed 16 mg/day
Consult product instructions for
pediatric dose
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Loperamide
Contraindication
Loperamide should not be used in
patients with fecal leukocytes, high fever,
or blood or mucus in the stool (dysentery);
Loperamide may cause paralytic ileus in
patients with desentery
Paralytic ileus: paralysis or inactivity of the intestine that prohibits the
passage of material within the intestine. May be a result of anticholinergic
drugs, injury or surgery
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Adsorbents
Kaolin, pectin, attapulgite and bismuth
subsalicylate;
Kaolin: a natural hydrated aluminum silicate.
Not absorbed from GIT, 90% metabolized in gut
and excreted in faeces
Attapulgite is another naturally occur clay
mineral, consisting of hydrous Mg-Al-silicate;
kaolin & attapulgite have varying and relatively
weak adsorptive properties in respect to
diarrhoea producing bacteria
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Adsorbents
Mode of action:
1.
adsorb the microbial toxins and microorganisms to their own surfaces
drugs not absorbed from the GIT toxins and
MOs are excreted in stool;
2. Hydrophilic adsorbents (e.g. pectin and bulkforming agents; ispaguala, methylcellulose, and sterculia),
bind water within the intestine causing watery
stool to become more formed
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Adsorbents
the main constituents in the antidiarrhoeal
preparations for young children (whom
opiates and antimuscarinics are
contraindicated);
not absorbed from GIT harmless and
safe to use
Debate: reduce evacuation of faecesprolong presence of pathogens/toxins in
bowel. Adsorption: non-specific process
(medicines)
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PROBIOTICS: AN
UPDATE
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Background
Probiotics are live organisms that are
ingested to provide therapeutic or
preventative benefit for the host. The most
commonly used are the lactic acidproducing bacteria bifidobacteria and
lactobacilli. Probiotics also include the
yeast Saccharomyces boulardii. Probiotics
are commonly promoted to strengthen the
immune defenses.
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Bifidobacteria spp
Saccharomyces
boulardii
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Probiotics, Beneficial
Microbes
Beneficial microbes
such as bifidobacteria
live in the intestinal ecosystem with potentially
pathogenic bacteria. Beneficial microbes
prevent the overgrowth of “bad bacteria” by
producing antimicrobial agents. Additionally,
beneficial
microbes
competitively
limit
pathogenic bacterial overgrowth by occupying
receptor sites and vying for space and
nutrients. Beneficial microbes may also
increase intestinal production of mucin, which
stimulates the production of mucus, forming a
protective barrier on the intestinal lining
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In order to be effective:
• probiotics must be able to withstand a
wide range of pH variation. Many microbes cannot
withstand the protective acid barrier of the stomach and the effects
of bile.
• must also be able to colonize the gut and
be able to attach to the intestinal
epithelium.
• Additionally, the probiotic should
disturb healthy intestinal microbes
not
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Probiotic Bacteria and Yeasts
Bifidobacteria are anaerobic, rod-shaped,
gram-positive bacteria. Bifidobacteria are
the most prominent beneficial microbes in
the
colon.
Bifidobacteria
produce
antimicrobial substances that have a
broad spectrum of antimicrobial activity
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Bifidobacteria that are commonly used
as probiotics include Bifidobacterium
longum, B. breve, B. infantis, B. bifidum, B.
lactis, and B. adolescentis. Bifidobacteria
supplements are most commonly combined
with other probiotics.
Lactobacilli are a group of gram-positive
rods that are obligate and facultative
anaerobes.
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Other bacteria sometimes used as
probiotics
include
Streptococcus
thermophilus and Leuconostoc species.
The yeasts Saccharomyces boulardii and
S. cerevisiae are also used
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Probiotics for Diarrhea
•
Probiotics may be useful as adjunctive treatment
of adults and children with infectious diarrhea.
Several species of Lactobacillus seem to reduce
the duration of diarrhea, particularly in rotaviral
infections.
• For antibiotic-associated diarrhea, Lactobacillus
rhamnosus GG, S. boulardii, and probiotic
mixtures appear to be effective prophylactic
agents. Given along with antibiotics, these
probiotics can reduce the incidence of diarrhea by
about 60% to 65%. The effectiveness of probiotics
on treatment of antibiotic-associated diarrhea is
less clear.
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SAFETY
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SUMMARY
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