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Drug used in constipation
Dr.Jannatul Ferdoush
Assistant Professor
Department Of Pharmacology
• Constipation :
Absence of propagating contraction in colon.
• Purgatives:
They are medicine that promote defecation
largely by reducing the viscosity of the content
of the lower colon.
Classification of purgatives
• Luminally active agent:
1.Bulk forming agent- Several days( at least 3 day)
bran
ispagula husk
methylcellulose
2.Osmotic agent- inorganic salt- (with in 3 hours)
magnesium hydroxide
Magnesium sulfate.7H2O
Lactulose
Stool (fecal) softeners( emollients)(reliefs within 1-2 days)
Docusate sodium
Liquid paraffin
Stimulant purgatives:
Bisocodyl ( 6-10 hrs)
glycerol
sinna(8-12 hrs)
Danthron(6-12hr)
Prokinetic agent
5HT4 agonist
opioid antagonist
Enema & suppositories( 1 hrs)
M/A of Bulk & osmotic laxatives
Retain water in the intestinal lumen
↓
↑Bulk of the stool& gives pressure on the lumen
↓
Stimulate enteric nerve plexus
↓
↑Peristalsis
↓
Evacuation of stool
• Indication:
Hemorrhoids
Anal fissure
Diverticular disease
Irritable bowel syndrome
A/E:
Cathertic colon
Malabsorption syndrome
Proteinloosing enteropathy
Paralytic ileus
Osmotic laxatives
• Where a rapid bowel evacuation is required,
magnesium sulphate is still used.
• This should be used in a dose before breakfast or on
an empty stomach, followed by plenty of warm
fluid.
• This treatment usually causes evacuation within 2
hours
Magnesium sulphate (MgSO4) Epsom salt
• MgSO4 dissociate into Mg & SO4. This Mg draws
water from intestine causing softer stool & help in
evacuation
• MgSO4 is usually given in empty stomach
It may cause uremia in patients with renal
insufficiency
Lactulose
• It is a semi synthetic disaccharide of fructose &
galactose.
• Taken orally, it is unaffected by small intestinal
disaccharidase, is not absorbed
• In the colon, bacteria convert it to its two
component sugars, which are poorly absorbed;
when these are fermented, the lactic acid & acetic
acid are formed which function as osmotic
laxatives. It takes 2-3 days to act
• Indication:
–constipation,
–hepatic encephalopathy
• Contraindications:
–galacosaemia,
–intestinal obstruction
• Side effects: flatulence, cramps, & abdominal
discomfort
• Dose: expressed in terms of an eoral solution
containing lactulose 3.35 g/5ml
• Constipation, adults initially 15 ml twice daily,
gradually reduced according to patients needs; child
under 1 year 2.5 ml, 1-5 years 5 ml., 6-12 years 10
ml twice daily, gradually reduced
• Hepatic encephalopathy, 30-50 ml 3 times daily,
subsequently adjusted to produce 2-3 soft stools
daily
• Avolac (solution, 3.35 mg/5ml), D-Lac (syrup),
Laclose (syrup), Osmolax (syrup)
Magnesium hydroxide
• Indication: mild constipation (acts in 2-4 hours)
• Caution: use only occasionally; the elderly; renal
impairment; hepatic impairment
• Contraindication: intestinal obstruction
• Dose: Aqueous suspension containing about 8%
hydrated magnesium oxide, 25-50ml as & when
required
• Magna milk, milk of magnesia (susp 400 mg/5ml)
Fecal softner
• Decusate:
Softening the stool by↓ surface tension of
stool which allows more water to remain in
the feces.
It has bowel stimulant property.
↑ Intestinal fluid secretion, It mix with stool
& stool become soft.
Liquid paraffin
• Chemically inert mineral oil
• Not digested
• Tasteless
• M/A:
• Lubricates the intestinal wall
• Easy & increase rate of passage of gut contents
• Reduce absorption of water in the small intestine
• Retain more water in the gut contents
• Softening of the stool
• Easy evacuation
• Side effects :
Anal leakage following large doses of paraffin cause
physical & social discomfort.
Granulomatous reactions caused by absorption of
small quantities of liquid paraffin (especially from
the emulsion)
Lipoid pneumonia (taken orally for long period,
especially at night, may be aspirated & cause
chronic lipoid pneumonia)
Stimulant purgatives
• Most strong laxatives
• Induces low grade inflammation in small &
large intestine to promote accumulation of
water & electrolyte
• Stimulate gut motility.
• Dependence:
- Stimulant empty the whole colon. But normal
defecation only empties the descending colon .
-Cessation of use after a few weeks is followed by a
few days constipation to collect significant
materials to restore the normal state.
-This delay may convince the patient to continued
need for purgatives.
• Enema:
containing 130 ml of arachis oil (ground-nut
oil) would lubricate & soften impacted faeces
& promote bowel movement.
• For children above 6 years, the dose has to be
reduced in proportion to body-weight; not
recommended for children under 6 years
Cathartic colon
• It is the anatomical and physiological changes
in the colon that occurs with chronic use of
stimulant laxatives.(> 3times/weeks) for 1 yr
• S/S—
Bloating
Feeling of fullness
Abdominal pain
Incomplete fecal evacuation
• Typically female patient.
• Long standing H/O laxative use
• Cause damage to the colonic Nerve.
• Rx – surgery.

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Drug used in constipation

  • 1. Drug used in constipation Dr.Jannatul Ferdoush Assistant Professor Department Of Pharmacology
  • 2. • Constipation : Absence of propagating contraction in colon. • Purgatives: They are medicine that promote defecation largely by reducing the viscosity of the content of the lower colon.
  • 3. Classification of purgatives • Luminally active agent: 1.Bulk forming agent- Several days( at least 3 day) bran ispagula husk methylcellulose 2.Osmotic agent- inorganic salt- (with in 3 hours) magnesium hydroxide Magnesium sulfate.7H2O Lactulose
  • 4. Stool (fecal) softeners( emollients)(reliefs within 1-2 days) Docusate sodium Liquid paraffin Stimulant purgatives: Bisocodyl ( 6-10 hrs) glycerol sinna(8-12 hrs) Danthron(6-12hr) Prokinetic agent 5HT4 agonist opioid antagonist Enema & suppositories( 1 hrs)
  • 5. M/A of Bulk & osmotic laxatives Retain water in the intestinal lumen ↓ ↑Bulk of the stool& gives pressure on the lumen ↓ Stimulate enteric nerve plexus ↓ ↑Peristalsis ↓ Evacuation of stool
  • 6. • Indication: Hemorrhoids Anal fissure Diverticular disease Irritable bowel syndrome A/E: Cathertic colon Malabsorption syndrome Proteinloosing enteropathy Paralytic ileus
  • 7. Osmotic laxatives • Where a rapid bowel evacuation is required, magnesium sulphate is still used. • This should be used in a dose before breakfast or on an empty stomach, followed by plenty of warm fluid. • This treatment usually causes evacuation within 2 hours
  • 8. Magnesium sulphate (MgSO4) Epsom salt • MgSO4 dissociate into Mg & SO4. This Mg draws water from intestine causing softer stool & help in evacuation • MgSO4 is usually given in empty stomach It may cause uremia in patients with renal insufficiency
  • 9. Lactulose • It is a semi synthetic disaccharide of fructose & galactose. • Taken orally, it is unaffected by small intestinal disaccharidase, is not absorbed • In the colon, bacteria convert it to its two component sugars, which are poorly absorbed; when these are fermented, the lactic acid & acetic acid are formed which function as osmotic laxatives. It takes 2-3 days to act
  • 10. • Indication: –constipation, –hepatic encephalopathy • Contraindications: –galacosaemia, –intestinal obstruction
  • 11. • Side effects: flatulence, cramps, & abdominal discomfort • Dose: expressed in terms of an eoral solution containing lactulose 3.35 g/5ml • Constipation, adults initially 15 ml twice daily, gradually reduced according to patients needs; child under 1 year 2.5 ml, 1-5 years 5 ml., 6-12 years 10 ml twice daily, gradually reduced • Hepatic encephalopathy, 30-50 ml 3 times daily, subsequently adjusted to produce 2-3 soft stools daily • Avolac (solution, 3.35 mg/5ml), D-Lac (syrup), Laclose (syrup), Osmolax (syrup)
  • 12. Magnesium hydroxide • Indication: mild constipation (acts in 2-4 hours) • Caution: use only occasionally; the elderly; renal impairment; hepatic impairment • Contraindication: intestinal obstruction • Dose: Aqueous suspension containing about 8% hydrated magnesium oxide, 25-50ml as & when required • Magna milk, milk of magnesia (susp 400 mg/5ml)
  • 13. Fecal softner • Decusate: Softening the stool by↓ surface tension of stool which allows more water to remain in the feces. It has bowel stimulant property. ↑ Intestinal fluid secretion, It mix with stool & stool become soft.
  • 14. Liquid paraffin • Chemically inert mineral oil • Not digested • Tasteless • M/A: • Lubricates the intestinal wall • Easy & increase rate of passage of gut contents • Reduce absorption of water in the small intestine • Retain more water in the gut contents • Softening of the stool • Easy evacuation
  • 15. • Side effects : Anal leakage following large doses of paraffin cause physical & social discomfort. Granulomatous reactions caused by absorption of small quantities of liquid paraffin (especially from the emulsion) Lipoid pneumonia (taken orally for long period, especially at night, may be aspirated & cause chronic lipoid pneumonia)
  • 16. Stimulant purgatives • Most strong laxatives • Induces low grade inflammation in small & large intestine to promote accumulation of water & electrolyte • Stimulate gut motility.
  • 17. • Dependence: - Stimulant empty the whole colon. But normal defecation only empties the descending colon . -Cessation of use after a few weeks is followed by a few days constipation to collect significant materials to restore the normal state. -This delay may convince the patient to continued need for purgatives.
  • 18. • Enema: containing 130 ml of arachis oil (ground-nut oil) would lubricate & soften impacted faeces & promote bowel movement. • For children above 6 years, the dose has to be reduced in proportion to body-weight; not recommended for children under 6 years
  • 19. Cathartic colon • It is the anatomical and physiological changes in the colon that occurs with chronic use of stimulant laxatives.(> 3times/weeks) for 1 yr • S/S— Bloating Feeling of fullness Abdominal pain Incomplete fecal evacuation
  • 20. • Typically female patient. • Long standing H/O laxative use • Cause damage to the colonic Nerve. • Rx – surgery.