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Department of Pharmacology

Faculty of Medicine
University of Lampung
Correction of fluid Treatment should The treatment of
Dehydration is the depletion, shock, always be directed diarrhea: correction
most common and acidosis are of according to the of dehydration,
cause of death in central importance underlying cause as maintenance of
case of diarrhea. to all forms of acute most diarrhea is adequate nutrition,
diarrhea. self-limiting. and drug therapy
Sodium chloride - 3.5 g

Potassium chloride - 1.5 g

Sodium carbonat- 2.5 g

Glucose - 20 g

Water - 1 litre
Rotavirus diarrhea
is generally self-
limiting and does
not need any drug
therapy.
Cholera (tetracyclines co-
trimoxazole),
Antimicrobials Campylobacter (norfloxacin and
other fluroquinolones),
should be regularly Clostridium difficile
used in cases (metronidazole, vancomycin)
Amoebiasis /giardiasis
(metronidazole).
Adsorbents Antisecretory

Antimotility
agents
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.
Octreotide somatostatin

IV T 1.5 hours, SC 6- to 12-hour DoA.

Effective in higher doses for the treatment of diarrhea due to


vagotomy, short bowel syndrome or AIDS.

ADRs: steatorrhea, fat-soluble vitamin deficiency, nausea,


abdominal pain, flatulence, and formation of sludge or gallstones,
hyperglycemia or, less frequently, hypoglycemia (usually mild).
Opioids, eg. opium tincture (paregoric)
containing morphine, diphenoxylate,
difenoxin, codein.

Activation of opioid receptors in the


enteric nerve plexus results in inhibition
of propulsive motor activity.

CNS effects (sedation, respiratory


depression, physical dependence).
Diphenoxylate and Difenoxin

Available in
Extensively Higher doses preparations
absorbed after (40-60 mg per containing
Difenoxin is the
oral day) CNS small doses of
active Potent than
administration, effects atropine to
metabolite of morphine
Tmax = 1-2 potential for discourage
diphenoxylate
hours, T 12 abuse and/or abuse and
hours addiction deliberate
overdosage
40-50 x > potent than
Penetrates the CNS poorly
morphine

Loperamide

Has antisecretory activity


against cholera toxin and Effective and safe
some forms of E. coli toxin
Act quickly following an oral use

PK:

Tmax = 3-5 hours
T = 11 hours
Extensive hepatic metabolism

Effective against traveler's diarrhea, used either alone or in


Therapeutic combination with antimicrobial agents (trimethoprim,
cotrimoxazole, fluoroquinolone).
Adjunct treatment in almost all forms of chronic diarrheal
uses
disease.
Should not be used in children younger than 2 years of age
SE:

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.
AGENTS USED TO TREAT CONSTIPATION

Laxatives/aperients are Purgatives/cathartics are


agents having milder action agents having stronger action
and helps in elimination of resulting in more fluid
soft but formed stools. evacuation.
Bulk forming - dietary fibre, psyllium, ispaghula, methyl
Luminally cellulose
Stool softener - dioctyl sodium sulphosuccinate

Active (Docusates, Doss)


Lubricants - liquid paraffin
Osmotic - magnesium sulphate, magnesium hydroxide,
Agents sodium sulphate, sodium potassium tartarate, lactulose,
sorbitol, mannitol, polyethylene glycol (PEG)

Stimulant Diphenylmethanes - Phenolphthalein, bisacodyl

(Contact) Anthraquinones - Senna, cascara, rhubarb, aloes,


danthron
Fixed oil - Castor oil
Purgatives
Castor oil ricinoleic acid very irritating
peristalsis
OoA >> 0.5 3 hours
Hardly suitable for constipation, but to reduce
absorption of toxin from the gut
Anthraquinone derivatives >> cascara,
senna, aloe contain emodin which stimulates
colonic activity
Inactive >> converted by colon bacteria to the
active free aglycones.
Diphenolmethane derivatives >>
phenolphthalein& bisacodyl potent
stimulant of the colon
OoA delayed 6-8 hours
Indication: GI surgery, MCI, stroke, painful
disease of anus
Classification and Comparison of Representative Laxative
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Laxative Effect and Latency in Usual Clinical Dosage
________________________________________________
Softening of feces, Soft or semifluid stool, Watery evacuation,
1-3 days 6-8 hours 1-3 hours
__________________________________________________________
Bulk-forming laxatives Stimulant laxatives Osmotic laxatives
Bran Diphenylmethane Sod.phosphates
Psyllium prep. derivates MgSO4
Methylcellulose Bisacodyl Milk of magnesia
Calcium polycarbophyl Mg Citrate
Surfactant laxatives Anthraquinone der. Castor oil
Docusates Senna
Poloxamers Cascara sagrada
Lactulose
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