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DRUGS ACTING ON THE GASTRO INTESTINAL TRACT

A. DRUG USED FOR TREATMENT OF PEPTIC ULCER
Peptic Ulcer is characterized by various degree of erosion of gut wall. Ulcer develops
when aggressive factors out weighs the mucosal resistance to ulceration. Aggressive
factors out weighs the mucosal resistance to ulceration.
Pathophysiology may be due to
- Increase in Gastric acid Secretion
- H. pylori infection
- NSAIDS
Pyloric sphincter - control movement of acid stomach content into the duodenum
Viscoid mucous - prevent gastric mucosa from acid stomach content
Cardiac sphincter - prevent reflex into the oesophagus
Factor for opening of cardiac sphincter
- Tight clothing
- Over eating
- Abdominal pressure owing to pregnancy
- Obesity
Common Symptom of PUD
- Epigastric pain which comes 90min - 3hr after eating (main)
- Right upper Quadrant pain
- Abdominal fullness
- Nausea (Vomiting)
Dietary regimen & drug therapy are the corner stone of the treatment
The treatment is aimed at
- Withdrawal of the offending agent such as NSAIDs
- Improve life style (avoid smoking, alcohol, spicy foods, caffeine containing beverage)
- All Stimulants which increase gastric acid secretion
- Relief of pain
- Acceleration of ulcer healing
Pharmacotherapy of peptic Ulcer
1. Antacids
2. H2 - receptor antagonist
3. Proton pump inhibitors
4. Antibiotic, bismuth, antimuscarinic
1. Antacid
-Weak bases and react with acid to form salt with H2O
- Act locally in the stomach
MOA: - neutralize the acid in the stomach and indirectly inhibiting activity of pepsin
(pepsin is inactive above PH4)

GIT DRUGS-RATHEESH

Antacid

Neuralizing
Capacity
NaHCa3(systemic) High

Salt
Formed
Nacl

Solubility
of Salt
High

CaCa3

Moderate

CaC12

Moderate

AlOH)3

High

AlCl3

Moderate

MgCl2

Low

Mg (OH)2

High

Adverse
Effect
- Systemic alkalosis
- Fluid Retention
- Hypercalcemia
- Nephrolithiasis
- Constipation
- Interfere with the
Bio availability of
many drug.
- Diarrhea
- Hyper magnesia

Drug Interactions
- Antacid decrease gastric absorption of tetracycline and oral iron products
- With enteric coated products
Use
1. To Neutralize meal Stimulated gastric acid secretion
- Usually taken 1 hour after meal
2. Beneficial in healing duodenal ulcer
- Often used in conjunction with H2 - receptor antagonist
3. Dyspepsia (epigastric discomfort)
2.Anti-Secretary Drugs
H2-receptor antagonist
MOA: - They competitively inhibit the action of histamine on the H2 - receptor that
trigger parietal cell response to chemical stimulation.
These are the most popular drugs for the treatment of peptic ulcer.
They bring about symptomatic relief & ulcer healing
A. Cimetidine
- Inhibit stimulated acid secretion (e.g. histamine, insulin)
- Inhibit meal stimulated acid secretion
Use - 1. Prophylaxis of duodenal ulcer
2. Short term treatment of gastric ulcer
Dose: - 400mg po bid
300mg IV
Adverse Effect
- Hepatotoxicity
- Diarrhea, Dizziness
- Inhibit P450 enzymes
- Sexual dysfunction (antiandrogenic effect)
Kinetics
- Following oral administration, 80% is absorbed
- Mostly excreted unchanged in urine
B. Ranitidine
- 5 times more potent than cimetidine
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- Action is more selective and long duration of action
Dose: - 150mg Bid or 300mg at bed time
Advantage
- Doesn't produce sexual dysfunction
- Doesn't interfere with hepatic Metabolism
C. Famotidine
- About 40 times more potent than cimetidine
- Well tolerated and posses fewer side effect
- Doesn't interfere with Hepatic drug metabolism
Doses: - 20mg bid or 40mg once a day at bed time
Proton-Pump inhibitor
Parietal cells secrete H+ ions which is accomplished by an enzyme H+, K+- ATPase (serve
as a proton pump, exchanging K+ for H+ ions). It is required for HCl secretion
Omeprazole
MOA: - bind to H+-K+ ATPase enzyme and inactivate it
Effect
- More potent than H2 - blocker
- Has longer duration of action
- No rebound increase in gastric acid secreation
Dose: 20mg once a day (best if taken before break fast)
Adverse effect
- Inhibit drug metabolizing enzyme
- Hyper gastremia
- Prolonged complete suppression of the acid barrier to bacteria entry into the body
3. Anti-Muscarinic agent
Pirenzepine
MOA: - M1- receptor antagonist
Effect: - Beneficial in treatment of duodenal ulcer than gastric ulcer
SE: - anticholinergic side effect: dryness, dizziness, headache
4. Mucosal Protective Agent
Bismuth
-Form white precipitate in gastric acid
MOA - PPt (antacid-glyco protien complex) coats the ulcer site
- Drug may cause constipation and black stool
Carbenoxolone sodium(ulcer healing)
MOA - Increase production and viscosity of mucous
S.E. - Aldosterone like effect (hypertension, fluid retention and hypokalemia)
5. Antibiotics-against H.Pylori infection:doxorubicin,ampicillin
B. DRUGS USED AS LAXATIVES (Purgatives,Cathartics)
Constipation is difficult to define. In general, it may be defined as infrequent or
seemingly incomplete evacuation
Diagnosis: - Clinical
Non - drug treatment:
- Removal of underlying cause
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- More fiber diet intake
- Increase fluid intake
Phatology; change in diet ,exercise,GI motility
Laxatives: - drug which produce soft formed stool
Purgative: - Produce sever action, watery stool
laxative are not usually recommended for children under 4 years of age
1. Stimulant or irritant Laxative
Castor Oil
- Castor Oil is obtained from seed of ricinus communis
- By itself, it is not irritant
MOA: - when ingested
Castor Oil Pancreatic Ricinoleic acid
Lipase
- Ricinoleic acid causes stimulation of small intestine and thereby increases peristalisis
and result in laxative action.
Dose: 5-30ml
- Effect quickly seen in 2-3 hr
CI ; pancreatic disease
Bisacodyl
- Structurally similar to phenolphthalein (color indicator)
- Can be used orally or rectally
- Stimulate the large intestine
Dose 10mg in the night
10mg rectally in the morning.
children 5mg rectally in the morning (4yrs)
2. Osmotic Laxatives
Salt: - Mg S04, Mg citrate
MOA: - when given orally, not absorbed from GIT. They exert osmotic effect on the GIT
there by holding considerable amount of water.
ses in bulk which exert mechanical effect thereby ses motility and facilitating
evacuation of faces.
- These drug act both in small intestines and large intestines
- Onset of action is fast and hence given before meals (breakfast) in the morning.
- Patient should be advised to take plenty of water
- Small amount of these drug which are absorbed may produce toxic effect especially in
renal insufficiency.
Mg - Market CNS depression
Na - aggravate CHF(congestive heart failure)
3. Bulk Laxatives
Lactose
- Non-absorbable disaccharide act by its stomach effect
MOA
1.Natural and Synthetic Polysacharide and cellulose derivative which when administered
Are not absorbed and increase the bulk of indigestible residue.
2. These drug absorb water and swell up, producing mechanical stimulation of evacuation
- Action is mild and stable 12-36hr
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4. Lubricant laxative
Liquid Paraffin
MOA 1. Oil retard the reabsorption of water from rectal mass in the colon
2. Oil also act as lubricant ,facilitating stool passage
Dose 10ml po every night for 3 days
Glycerin
1 gm rectally at night after moistening with water
C. ANTI-EMETICS
Nausea refers to the feeling of an imminent desire to vomit
Vomiting; refers to the forceful oral expulsion of gastric content
These are drugs which oppose or counter act nausea and vomiting.
Vomiting may triggered by a variety of stimuli.
Vomiting range from the physiologic state of pregnancy to serious pathology.
Pain
Bad taste
Bed Sight
Rotation

CTZ
VC

Emetic Substance (ipecac)

Pregnancy ( specially multiple pregnancy
Post Operative Vomiting
Anticancer Drug
Electrolyte Disturbance

VC= Vomiting Center

CTZ= Chemoreceptor trigger zone
The vomiting center has mainly muscarinic receptor
E.g. D2= Dopamine (D2) receptor
H1= Histamine (H1) receptor
Non-drug treatment of N/V
- Correction of the underling cause
- Hydration
1.H1-receptor antagonist
These have little or no effect against vomiting produced by substance acting directly on
the CTZ but are effective in motion sickness & against vomiting caused by substances
which act locally in the stomach.
Promethazine
Therapeutic category: - Anti-emetic, Antihistamine
Use: - Symptomatic treatment of various allergic conditions, antiemetic, motion sickness
pregnancy implication; possible respiratory depression if drug is delivered near time of
delivery.
MOA: - compete with histamine for H1-receptor; reduce stimuli to the brainstem reticular
system
SE bradycardia
Dosage: - Adults
Oral - 25mg at bed time - Allergic
IM/IV - 25mg
- antiemetic Oral, IM/IV 12.5 - 25mg every 4-6 hours
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motion sickness 25mg 30-60minute before departure.
Administration: - IM is the preferred route of administration
: - Due to the possibility of orthostatic hypotension IV route is not usually
Preferred.
Solution for injection may be diluted in 25-100ml NS or D5W (max one at
25mg/ml) and infused over 15-30minute.
Meclizine
therapeutic category;-antihistamine;antiemetics
Use;- prevention and treatment of motionsickness
SE;- slight to moderate drowsiness
thickening of bronchial secreation
Dosage;-12.5-25mg ,1hr before travel,repeat the dose every 12to 24 hr if needed
2.Muscarinic receptor antagonist
Hyoscine
Therapeutic category: - Anticholinergic, Antisposmodic
use ;-motionsickness,spasm
hyocine is the most potent agent available for prevention of motion sickness,though it is
less useful once sickness occurs
MOA: - block the action of Acetyl Choline at parasympathetic sites in smooth muscle,
Secretary Glands and the CNS; and hence dries secreation, antagonize histamine.
Dietry Consideration: - should be taken before meal or food
Dosage: - adults 10mg 2 tab prn
3.Dopamine antagonist
Metoclopromide
Therapeutic category: - Antiemetic; Dopamine antagonist
MOA: - block the dopamine receptor in chemo receptor trigger zone of the CNS
SE ;- disorder of movement,drowsiness,fatigue
occulogyric crisis(rapid involuntary eye movement)
disorder of menstruation(due to prolactin release)
PK;-half life -4hr
excreation;-urine
Dosage:- Adults:- 10-15mg/dose up to four times a day 30 minute before meal
Children: - 0.1-0.2mg/kg/dose up to four times a day
Administration: - injection solution may be given IM, direct IV push or infusion.
Lower doses (<10mg) of metocloprsmide can be given IV push undiluted
Over 1-2 minutes.
Dosage Form: - 5mg/ml (2ml, 10ml, 30ml) - injection
Syrup: 5mg/5ml
Tablet: 5mg, 10mg
phenothiazine
Chlorpromazine
Therapeutic category: - Anti-emetic, Antipsychostic agent
MOA - block Dopaminergic receptor in the brain
- Non-selective Dopomine antagonist
Dosage
Adults oral 10-25mg every 4-6 hours
IM, IV 25-50mg every 4-6hours
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Children oral 0.5-1mg/kg/dose every 4-6 hour as needed
IM/IV 0.5-1mg/kg/dose every 4-6 hour as needed
Dosage form: - injection 25mg/ml (10ml)
Oral: - 10mg, 25mg, 50mg, 100mg
Non-drug treatment of NIV
- Correction of the underling cause
- Hydration
D.ANTI -DIARHEAL AGENTS
Diarhea is the frequent passage of liquid faeces.
Cause - infections agents, toxins, drugs
They can range from discomfort and inconvenience in a healthy well nourished adults to
a medical emergency requiring hospitalization and parentral fluid & electrolyte therapy.
There are different approaches in the treatment of diarrhea:1. Maintainance of fluid with electrolyte balance
A. ORS (oral rehydration salt)
- Glucose
- Nacl
- Kcl
1. Sachet in 1 lit of H2O
2. Anti-infective agent
- Depending on the problem (i.e. type of infectious agent), d/t antibiotics can be
Given
E.g. Ciprofloxacin,
3. Anti motility agents
The main pharmacological agent which decrease motility are opiates like codeine,
diphenoxylate and loperamide.
Loperamide
Therapeutic category: - antidiarheal
Dosage: - 4mg initially, followed by 2mg after each loose stool (max 16mg/day)
Other use: - Traveler's diarrhea
Dosage
4mg after first loose followed by 2mg after each loose stool to a max of 8mg/day.
Loperamide is an opiate analogue with major peripheral opioid agonist
Advantage: - no abuse potential
But in over dose it may occur
Diphenoxylate (2.5mg)+ tatropine (0.25mg) or Lomotil
- It is an opiod chemically related to pethidine
Use: - constipating agent
Action: - is similar to codeine
Action (antidiarheal) is most prominent, but because it is absorbed systemically and
cross BBB CNS effect do occur.
Atropine is added in non-pharmacologic doses to discourage abuse.
Dose: -10mg followed by 2.5-5mg 6 hourly.

GIT DRUGS-RATHEESH