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Constipation
Pharmacotherapy
Rastegarpanah
Clinical pharmacy Department
Shariati GI Research Center
Tehran university of medical sciences
DEFINITION

A Disturbance In Bowel Function.

Stools Too Hard Or Too Small, Defecation
Too Difficult Or Infrequent.

“Normal” 3 Times / Day To 3 Times / Week

A Stool Frequency Of Less Than Three Per
Week
EPIDEMIOLOGY

Prevalence 12-19%

Prevalence Chronic Constipation Rises
With Age, (65 Years Of Age Or Older).

In Old Age, 26% Of Men & 34% Of Women

Common In Pregnancy.
Digestion period
Stomach:
3hours
Small intestine:
4 – 6 hours
Large intestine:
12 – 72 hours
Small intestine
Duodenum
25-30cm
Jejunum
2 metres
Ileum
3 metres
Large intestine
Ascending colon
Transverse colon
Descending colon
Sigmoid colon
Peristalsis
Excretion
1.Muscles work together to propel waste
matter (Peristalsis)
2.substances not absorbed by the body
becomes faeces
3.Faeces arrives in rectum to be expelled
What affects the bowel?
1. Poor diet
2. Lack of fluid
3. Low Mobility
4. Medications
5. Surgery
PATHOPHYSIOLOGY

Constipation = disordered movement of
stool through colon or rectum

Slowing of colonic transit idiopathic or:


Due to diseases
Side effect of drugs
Etiology:

Disease-Induced:
1.
Irritable bowel syndrome
Metabolic disorders (diabetes),
Endocrine disorders (hypothyroidism),
Neurogenic disorders (Diabetes mellitus,
Multiple sclerosis , Spinal cord injury).
Drug-Induced
Psychogenic causes
Life-style factors
Old age
Children
2.
3.
4.
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Drugs associated with constipation
Constipation in Elderly

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Constipation Is Common:
 Improper Diets (Low In Fiber And Liquids)
 Diminished Abdominal Wall Muscular Strength
 Possibly Diminished Physical Activity
Frequency Of Bowel Movements Is Not Decreased
With Aging.
Diseases Such As Colon Cancer And Diverticulitis,
Drugs In Elderly:
Anticholinergics, Aspirin, Furosemide,
Nitroglycerin, Amitriptyline

Signs and Symptoms :
1.
Decrease in frequency of fecal
elimination
Difficult passage of dry hard stools
Straining to have stool
2.
3.
Diagnostic Criteria


Diagnosis Based On Presence Of Following
For
At Least Three Months (With Symptom Onset
At Least Six Months Prior To Diagnosis).
Diagnostic Criteria
Must Have Two Or More Of Following:
1.
2.
3.
4.
Hard Stools In 25% Of Defecations
Sensation Of Incomplete Evacuation For
At Least 25% Of Defecations
Sensation Of Anorectal Obstruction /
Blockage For At Least 25% Of
Defecations
Fewer Than Three Defecations Per Week
CONSTIPATION
Diagnostic Studies:

Colonic Transit Time (CTT):
radio-opaque markers & day 4 Xray.
Ten markers daily for six days
No laxative and drugs
CTT
In Evaluating Patients With
Chronic Idiopathic Constipation.
 It Is Available And Has No
Complication.
 No Surgical Intervention Without
Colonic Transit Study Is
Recommended .

Patient Assessment



Obtain Lifestyle And Medical History Before
Making Any Recommendations
Determine Reason For Use Of A Laxative
1. To Relieve Constipation
2. To Evacuate The Bowel Prior To An
Upcoming Radiologic Or Endoscopic
Examination
Inquire About The Patient’s Current And
Past Use Of Laxative Products
Treatment




If Underlying Disease Is Recognized,
Cause Should Be Correct It.
GI Cancer Removed Via Surgery.
Endocrine And Metabolic Dz Corrected.
If Hypo-thyroidism, Thyroid-replacement
Therapy .
Refer to M.D. When……



Symptoms Have Persisted For More
Than 2 Weeks
Recurred After Previous Dietary Or
Lifestyle Changes Or Laxative Use
Patients With Blood In The Stool
Management
1.
2.
3.
4.
5.
Dietary Modification.
Increase In Daily Fiber.
Exercise (Even By Walking After Dinner)
Bowel Habits, Regular & Adequate Time
To Respond To Urge To Defecate.
Increase Fluid Intake.
Non-drug Treatment
1.
2.
3.
4.
High Fiber Food: Wheat Grains, Oats, Or
Fruits & Vegetables
Adequate Fluid Intake
Exercise
Avoid Foods That Cause Constipation:
(Cheeses & Sweets)
NON-PHARMACOLOGIC THERAPY
Fiber
 Increases Stool Bulk,
 Retention Stool Water & Increases Rate
Transit
 Increase Frequency Of Defecation
 Fruits, vegetables, cereals have highest fiber
 Bran, a by-product of milling of wheat,
 Trial of dietary high-fiber should be for at
least 1 month before effects on bowel
function are determined
Non Prescription Medications
Over The Counter (OTC)
Types of laxatives:
1.
2.
3.
4.
5.
6.
Bulk Forming
Emollient
Lubricant
Saline
Hyper-osmotic
Stimulant
DRUG CLASSES
Most Induce Bowel Evacuation By:



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Active Electrolyte Secretion
Decreased Water And Electrolyte
Absorption
Increased Intraluminal Osmolarity
Increased Hydrostatic Pressure In The Gut
Three Classifications:
1.
Softening Of Feces In 1 To 3 Days (Bulkforming Laxatives, And Lactulose)
2.
Semifluid Stool In 6 To 12 Hours
(Bisacodyl);
3.
Evacuation In 1 To 6 Hours (Magnesium
Hydroxide, Castor Oil, And Polyethylene
Glycol-electrolyte Solution).
Dosage Recommendations for Laxatives and Cathartics
Bulk Forming Laxatives

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Derived From Agar, Or Psyllium Seed
Synthetic, Methylcellulose & Carboxymethyl
Cellulose Sodium
Dissolve In Intestinal Fluid, Thus Creating Emollient
Gels That Increase Passage Of Intestinal Contents
Stimulate Peristalsis
No Systemic Absorption
Bulk Forming Laxatives
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Onset of action is 12-24hrs
physiologic in promoting evacuation
FIRST choice for constipation
Examples are:
Citrucel powder, Metamucil, Mitrolan
Chewable Tablets
Bulk Forming Laxatives
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Caution In Younger Than 6 Yrs Of Age
Avoid In Intestinal Ulcerations, Stenosis
Interact With Anticoagulants, Digitalis
Glycosides, And Salisylates
Not Used For A Fast Clearing Effect Before A
Diagnostic Procedure
Used Daily And Continued In Most Patients,
With Chronic Constipation.
Emollient Laxatives

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Anionic Surfactants, Softening Of Stool
Systemically Absorbed (Solid)
Onset Of Action (Oral) 24-72hrs
As A Stool Softener, & To Prevent
Constipation And Maintain Regularity
Example : Docusate Sodium
Avoid In Pts Who Have Nausea, Vomiting, Or
Undetermined Abdominal Pain
Saline Laxatives


Non-absorbable Cations & Anions - Draw
Water Into Intestine - Increase In Intra-luminal
Pressure, Stimulates Intestinal Motility
Onset Of Action (Oral) 30min-3 Hrs,
(Rectal) 2-5min

ONLY When Fast Clearance Of The Bowel Is Required

Ex: Fleet Phospho-soda
Avoid In Pts With CHF, Ileostomy, Renal Function

Impairment, Or Younger Than 6 Yrs Old
SALINE CATHARTICS

Saline Cathartics Poorly Absorbed Ions
Magnesium Sulfate Effects By Osmotic Action In
Retaining Fluid In GI.

Magnesium Stimulates The Secretion Of Cholecystokinin, A Hormone That Causes Stimulation Of
Bowel Motility And Fluid Secretion.
M.O.M
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May Be Given Orally Or Rectally.
Bowel Movement Within A Few Hours After
Oral Doses And In 1 Hour Or Less After
Rectal
May Cause Fluid And Electrolyte Depletion.
Magnesium Or Sodium Accumulation In
Patients With Renal Dysfunction
Hyper-Osmotic Laxatives
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Combine An Osmotic & Local Effect Of Sodium
Stearate, Draws Water Into Rectum  bowel
Movement
Onset Of Action (Rectal) 30 Min
Suppository Form
Minimal Side Effects
Example: Glycerin Suppositories
Avoid In Pts With Rectal Irritation
GLYCERIN
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Glycerin as a 1 & 3 g suppository and exerts
its effect by osmotic action in the rectum.
onset of action is less than 30 minutes.
Glycerin is very safe infants, children.
Its use is acceptable on for
constipation, in children.
Lubricant Laxatives

Prevent colonic absorption of fecal water,
thus soften the stool
minimally absorbed
Onset of action (oral)6-8 hrs, (rectal) 5-15 min
Avoid prolonged use
cause mal-absorption of fat-soluble vitamins

Example: Mineral oil

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LUBRICANTS

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Mineral oil (Paraffin) only lubricant
laxative
Mechanism


from petroleum, coating stool and
allowing for easier passage
inhibits colonic absorption of water,
increasing stool weight and decreasing
stool transit time
Dose and ADR Mineral Oil

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Orally Or Rectally In A Dose Of 15 To 45 Ml
Effect On Bowel After 2 Or 3 Days Of Use.
In Debilitated Or Recumbent Patients, May
Aspirated, Lipoid-pneumonia
ADR: Decrease Absorption Of Fat-soluble
Vitamins (A, D, E, And K) With Chronic Use
 Even Orally, May Leak From The Anal
Sphincter, Causing Soiling Of Clothing.
LACTULOSE

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Lactulose - Disaccharide, used Orally Or
Rectally
Metabolized By Colonic Bacteria To Lowmolecular-weight Acids, Result In
Osmotic Effect = Fluid Is Retained In The
Colon.
The Fluid Retained In The Colon Lowers
The Ph And Increases Colonic Peristalsis
LACTULOSE

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Not First-line, Not More Effective Than
Sorbitol Or Milk Of Magnesia
Alternative For Acute Constipation,
Useful In Elderly Patients
Lactulose May Result Flatulence, Cramps,
Diarrhea, And Electrolyte Abnormality.
Lactulose Dose


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Initial Dose 5 To 30 Ml Daily PO In A
Single Dose Or In 2 Divided Doses;
Doses Up To 45 Ml Daily
Dose Is Adjusted To Patient's Needs
Children
 5 To 10 Years Initial Doses Of 10 Ml
Twice Daily
 1 To 5 Years, 5 Ml Twice Daily
 Under 1 Year, 2.5 Ml Twice Daily.
Sorbitol

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A Monosaccharide, Osmotic Action,
Primary Agent In Functional
Constipation
As Effective As Lactulose, Less
Expensive.
Sorbitol By Mouth Or Rectally As An
Osmotic Laxative; Doses Of 20 To
50 G.
Stimulant Laxatives
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2 Classes:
- Diphenylmethane (Bisacodyl)
- Anthraquinone (Senna)
Increases Propulsive Peristaltic Activity
By Local Irritation Of Mucosa
Onset Of Action:
Senna (PO) 8-12 Hrs
Bisacodyl: Oral/Rectal 15-60min,
Systemically Absorbed
Major Use: For Evacuation Of Bowel
Prior To GI Surgery Or Examination
Bisacodyl

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Stimulating Mucosal Nerve Plexus Of
Colon
Significant Inter-patient Variability Exists
With Dosing
A Dose That Causes No Effect In One
Patient May Result In Excessive Cramping
And Fluid Evacuation In Others.
Not Recommended For Regular Daily Use.
Bisacodyl
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Acceptable Intermittently (Every Few Weeks)
To Treat Constipation Or As A Bowel
Preparation
Cause Abdominal Cramping
Significant Fluid And Electrolyte Imbalances
With Chronic Use.
Should Not Use In Appendicitis Is A
Possibility (Perforation Of The Appendix May
Result) Or During Pregnancy Or Lactation
ANTHRAQUINONE
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Cascara, Sennosides, And Casanthrol.
Gut Bacteria Metabolizes These Agents To
Their Active Compounds,
Exact Mechanisms Of Action Not
Understood.
Effects Are Limited To The Colon,
Use Of These Agents Are Similar To Those
For The Diphenylmethane Derivatives.
Intermittent Use Is Acceptable; Daily Use
Discouraged
Stimulant Laxatives
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Sennakot, Sennakot S (With Sodium Docusate),
Exlax, Dulcolax, Fijan Syrup (5.85 Mg Sennoside/5 Ml)
Interact With H1 Blockers, Antacids If
Administered Within 1 Hr
Avoid In Pregnancy
Breast Feeding: Senna Laxative Reported Brown
Discoloration Of Breast Milk
Adverse Effects:
Severe Cramping, Electrolyte & Fluid
Deficiencies, Metabolic Acidosis/Alkalosis
CASTOR OIL
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Castor Oil Metabolized In GI To Active
Compound, Ricinoleic Acid,
Stimulates Secretory Processes, Decreases
Glucose Absorption, And Promotes Intestinal
Motility, In Small Intestine.
Castor Oil Results In A Bowel Movement 1 To
3 Hours.
Because Strong Purgative Action, Should
Not Used For Routine Treatment Of
Constipation.
Polyethylene Glycol

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PEG Become Popular For Colon
Cleansing Before Diagnostic Procedures
Or Colorectal Operations.
Four Liters Of This Solution Is
Administered Over 3 Hours
Not Recommended For Routine Treatment
Of Constipation And Should Be Avoided
In Patients With Intestinal Obstruction.
Acute Constipation


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infrequent use (less than every few
weeks) of laxative is acceptable.
Relieved by use of a tap-water enema or a
glycerin suppository;
if ineffective, use of oral sorbitol, low
doses of diphenylmethane or
anthraquinone laxatives, or saline laxative
(e.g., milk of magnesia)
If laxative is required for longer than 1
week, consult a physician
Bedridden or Geriatric patients
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For some bedridden or geriatric patients, or with
chronic constipation, bulk-forming laxatives first
line of treatment,
Use of laxatives may be required frequently.
Lowest effective dose and infrequently as
possible to maintain regular bowel function
(more than three stools per week).
Milk of magnesia, and sorbitol or lactulose.
Mineral oil should be avoided
Patient Counseling


Laxative use to treat constipation
should be only on a temporary
measure
If laxatives are not effective after 1
week, a physician should be
consulted
Management

1-Management of chronic constipation
due to slow transit including:
patient education
behavior modification
dietary changes
drug therapy

2-Management of defecation involves:
biofeedback
sensory training
relaxation exercises
suppository programs
Patient education:
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reassurance
explanation of normal bowel habits
reduce use of laxatives and cathartics
increase fluid and fiber intake
use normal postprandial increases in
colonic motility by instructing patients to
defecate after meals
important in the morning when colonic
motor activity is highest
What Can You Do?

Become more
physically active

A 30 minute walk
every day may
help keep you
more regular
What Can You Do?

Eat more fiber


More beans, whole
grains and bran
cereals, fresh
fruits, vegetables
Limit foods with no
fiber (cheese,
meat, sweets,
processed foods)
What Can You Do?

Fiber supplements are best choice




Absorb water and make stool softer
Safe to use everyday
Be sure to drink at least 8 to 10
glasses of water everyday
Add to diet slowly to prevent
problems with gas
What Can You Do?

Drink more water and
other liquids (8 eightounce glasses a day)


Liquid helps keep the
stool soft
Avoid caffeine or
alcohol which can
dehydrate you
Treatment
algorithm for
normal transit
constipation
Treatment algorithm
for slow-transit
constipation
 Thank
you for your attention
Constipation in Infants & children




Constipation common.
neurologic, metabolic, or
anatomic abnormalities.
Management:
Dietary modification with highfiber foods
Drugs for Constipation:
Fluid & High fibers
Laxatives -osmotic:
Polyethylene glycol (70 g powder)
Lactulose (10g/15 ml syrup)
Sorbitol (5g powder)
Glycerin
Laxatives - stimulant:
Bisacodyl (Dulcolax, Correctol) 5 mg tab;5,10 mg supp.
Castor oil
Senna
Figan syrup (5.85 mg sennoside B/5 ml)
Magnesium Hydroxide (Milk of magnesium
MOM)240cc 8% Susp

Thank you for your attention
Rastegarpanah