DRUGS ACTING ON
GASTROINTESTINAL SYSTEM
FLOW OF PRESENTATION
Composition
Action
Dosage
Route
Indications
Contraindications
Drug Interactions
Side effects
Adverse effects
Toxicity & Role of nurse Proton pump inhibitors
CLASSIFICATION OF DRUGS ACTING ON GI SYSTEM
Antiemetic's
Emetics
Purgatives
Antacids
Cholinergic
Anticholinergic
Fluid and Electrolyte therapy
Antidiarrheal
Histamines
Antiemetics
Antiemetics are the Drugs which prevent or control the
Vomiting/Nausea.
• CLASSIFICATION
5HT3 Antagonists: Ondansetron , Granisetron, Dolasetron
Prokinetics / Dopamine Antagonists: Domperidone,
Olanzapine , Metoclopramide
Antihistamines: Cyclizine , Diphenhydramine , Meclozine ,
Promethazine , Hydroxyzine
Anticholinergic: Hyoscine , Dicyclomine
Mechanism of action
5HT3 Antagonists: They block serotonin receptors in CNS and
Gastrointestinal tract So they can be used to treat post operative and
cytotoxic (Chemotherapy) drugs nausea/ vomiting.
Prokinetics (Dopamine Antagonists): They block the dopamine
neurotransmitter also they promote gastrointestinal motility &
quicken gastric emptying.
Antihistamines: They block the histamine neurotransmitter and they
act by an effect on vomiting center and by producing sedation.
Anticholinergics: An Anticholinergic agents block the neurotransmitter
Acetyl choline in central and peripheral nervous system.
Drug example and doses
1. Hyoscine 200-600mg (SC)
2. Diclomine 40mg 6hourly
3. Cyclizine 50mg 4-6 hour
4. Meclizine 25mg/day.
5. Metoclopramide 10mg
6. Domperidone 10-20 mg 4-6hours
7. Ondansetron 8-16mg
Indications / Uses
5HT3 antagonists are used in management of nausea
vomiting associated with chemotherapy.
Antihistamine such as diphen hydramine is used for
motion sickness and morning sickness.
Metoclopramide is used for gastric emptying in patient’s
receiving tube feeding.
Anticholinergic such as hyoscine, Dicyclomine are useful
in travel sickness.
Contraindication/ Precautions
Diphenhydramine is contraindicated in hypertensive
patients.
Metoclopramide is contraindicated in suspected
gastrointestinal problem.
Use cautiously and reduced dose in renal impairment
conditions.
Anti emetics
Adverse effects •Hypotension. •Constipation. •Dryness of mouth.
•Blurred vision. •Pain in IM injection site. •Drowsiness. •Rectal
irritation. •Photo sensitivity reaction.
Drug interactions •Use antihistamine, other CNS depressants
including opioids and sedative – hypnotic drugs causes additive CNS
depression. •Metoclopramide affects GI motility and alter GI
absorption of other drugs such as salicylates, levodopa, diazepam,
lithium, tetracycline.
Nursing Responsibilities
Assess the patient for nausea/vomiting and fluid and electrolyte
imbalances.
Decrease metoclopramide dose 50% of usual recommended dose
if creatinine clearance is less than 40ml/min.
Instruct the patient not to consume alcohol when taking an
antiemetic drugs.
Advise the patient to take oral antiemetics 1hour before exposures
to conditions causing motion sickness or before travelling.
Emetics
Emetics are drugs which produce vomiting.
Mechanism of action -They stimulate the
chemoreceptor trigger zone and gastric
mucosa to induce vomiting.
Drug example and doses
1. Apomorphine 5mg IM
2. Copper sulfate Given in water every 5 min. until emesis
occur.
3. Sodium chloride (NaCl) 2 table spoon of NaCl in glass of
warm water
4. Ipecac syrup 15-30ml (followed by 200ml of water.
Emitics
Indications / Uses - •To induce vomiting. •To treat
poisoning. •Treatment of overdose of drug.
Contraindication / Precautions - •History of
seizures. •Semi comatose or unconscious patient.
•Ingested caustic substance or petroleum products.
Adverse effects - •Arrhythmias.
•Cardiotoxicity. •Diarrhea. •Drowsiness.
Drug interactions -•Emetic reduce their
effects when used with activated charcoal.
Nursing Responsibilities
Assess the consciousness level of patient before
administering drug.
Follow administration of Ipecac syrup with one or two passes
of tepid water or other clear liquid.
Obtain a history, to find out caustic substances to determine
possible antidotes.
We should know that lavage is necessary if second dose not
produce vomiting Ipecac may be cardiotoxic if absorbed.
Laxatives/Purgatives
These drugs are combinedly knows as purgatives, which includes laxatives
and cathartics these drugs are used to overcome the constipation and
proper evacuation of bowels.
Mechanism of action
•Osmotic laxatives (Magnesium hydroxide) draw water into the intestine
to increase the mass of stool, stretching musculature which results in
peristalsis.
•Stimulant laxatives result in stimulation of intestinal peristalsis.
•Lubricant laxatives increase water retention in the stool, prevent water
absorption from the stool, and lubricate as well as soften intestinal
contents.
•Stool softener allow more fluid are fat to penetrate the faeces, producing
a softer fecal mass.
Drug example and doses
1. Bilk forming laxatives (Methyl Cellulose) 2 tablets 1000mg orally
with 8oz of liquid up to 6times a day.
2. Lubricant laxatives include mineral oil (Kondremal, Fleet mineral
oil enema.
3. Hyperosmotic laxatives include lactulose. 10mg BD
4. Stimulant laxatives (Bisacodyl, Castor oil) 5-10 mg sodium Pico
sulfate 15-20 ml
5. Stool softener (Docusate Calcium, Docusate potassium) 240mg 50-
400mg orallyb1to 4 equally divided dose each day.
Indications / Uses
To treat or prevent constipation.
To prepare the bowel for radiologic or endoscopic procedures.
Short term treatment of constipation caused high dose of opioid use.
Osmotic laxatives are used to rapid evacuation of the bowel after
ingestion of poison or following anti-helminthic therapy to rid of the
body from dead parasites.
Methyl cellulose and psyllium are used to many chronic diarrhea.
Contraindication / Precautions •Contraindicated if patient with
parasites. Or severe abdominal pain of unknown cause.
Adverse effects
GI irritation.
Rectal burning sensation.
Osmotic laxatives may causes dehydration.
Long term use and abuse of laxatives may cause permanent loss
of colonic motility. Laxative dependence and electrolyte
imbalances.
Nutritional deficiencies (with lubricant laxatives).
Belching (with osmotic laxatives)
Electrolyte imbalance. (with saline laxatives)
Drug interactions - Laxative decrease intestinal transit time
and reduce absorption of orally administer drugs.
Nursing Responsibilities
Assess for abdominal pain, distention, nausea/vomiting,
bowel sounds.
Monitor the patient for fluid electrolyte imbalances.
Evaluate stools for frequency and consistency.
Mix bulk forming laxatives in full glass of water or juice
Antacids
They act by neutralizing Gastric acid in the
stomach.
Mechanism of action - They achieve their effects
by neutralizing gastric acid, inhibiting gastric
acid secretion or protect gastric mucosa.
Drug example and doses
1. Sodium bi carbonate 1-5 gram orally
2. Magnesium hydroxide 0.5-1gm
3. Aluminum Hydroxide Up to 1gm daily
4. Magnesium carbonate 250-500 mg orally
5. Calcium carbonate Up to 1.5gm daily
Indications / Uses •Indigestion. •Reflux esophagitis, •Pain and burning
with peptic ulcer. •Peptic ulcer.
Contraindication / Precautions •Abdominal pain of unknown origin.
•Caution in renal failure because they contain magnesium. •Heart
patient.
Adverse effects •Constipation (Aluminum Hydroxide).
•Hypophosphatemia (with Aluminum Hydroxide). •Hypomagnesemia
(with Magnesium Hydroxide). •Increase sodium can cause edema and
CHF. (Sodium bi carbonate). •Diarrhea (Magnesium Hydroxide)
Drug interactions •Antacids decrease absorption of anticholinergics,
sucralfate, H2 receptor antagonists, Iron, Isoniazid and tetracyclines.
Nursing Responsibilities
Give antacids at least one hour after meal and at least one hour a part from
enteric coated tablets.
Always give combination of aluminum and magnesium hydroxide because
they make a balance (constipation effects of aluminum with laxative effects
of magnesium).
Give pre-cautiously to kidney and heart patient.
Check antacids labels for sodium content and to use only low sodium
preparation.
Teach the patient to avoid gastric irritants such as smoking, alcohols,
Cholinergic
Information for GI system
Parasympathomimetic or cholinomimetics
Stimulate parasympathetic nervous system in same manner as
does acetylcholine
May stimulate cholinergic receptors directly or slow acetylcholine
metabolism at synapses (affect the enzyme acetylcholinesterase)
Useful in treating Alzheimer’s Disease, Myasthenia gravis and to
treatment atony of the smooth muscle of the GI system or urinary
system
Cholinergic
GI effects
Acetylcholine stimulates cholinergic receptors in the gut to
promote normal secretory and motor activity
Cholinergic activity in the gut will increase peristalsis and
facilitates movement of flatus and feces
The secretory functions of the salivary and gastric glands also
stimulated.
Increased tone and contractility in GI smooth muscle, relaxation
of sphincters, increased salivary gland and GI secretions.
Anticholinergic –
Information for GI system
Also called cholinergic blocking agents or parasympatholytics
Again, focus is on the parasympathetic nervous system
Parasympathetic system acts as a resting and reparative function
Functions include digestion, excretion, cardiac decelertion,
anabolism and near vision.
Most anticholinergic drugs interact with the muscarinic receptors
in the brain, secretory glands, heart, and smooth muscle.
A few can also affect the nicotinic receptors. Glycopyrrolate
(Robinul) is an example
Mechanism of action: Act by occupying receptor sites at
parasympathetic nerve endings, thereby leaving fewer
receptor sites free to respond to acetylcholine.
Distribution of receptors is broad so effects of anticholinergics
will be diffuse.
Helpful in treating irritable colon or colitis.
Useful in gastritis, pylorospasm and ulcerative colitis as they
slow motility.
Proton pump inhibitors
These agents are used in patient with peptic ulcers (who
have failed to respond H2 blockers)
Mechanism of Action: It acts by inhibiting proton pump
which is final common step in gastric acid secretion. It also
have antisecretory action.
Drug example and doses :
1. Omeprazole 20mg daily
2. Lansoprazole 30 mg OD.
3. Pantoprazole 40mg 4 Rabeprazole 20mg
Indications / Uses •Peptic ulcer. •Reflux esophagitis. •Zollinger –
elision syndrome. •Prevent and treat NSAID’s related to gastric
ulcer.
Contraindication / Precautions •Hypersensitivity. •Special
precaution in pregnant and breast feeding mothers.
Adverse effects- •Headache. •Abdominal pain. •Chest pain.
•Diarrhea. •Dizziness. •Nausea / Vomiting.
Drug interactions- •Proton pump inhibitor interfere with the
absorption of drugs (Ketoconazole, iron and ampicillin) that
depends on gastric PH absorption.
Nursing Responsibilities
Monitor the patient for diarrhea and abdominal pain.
Teach the patient to swallow capsule whole and not to chew or crush
them.
Teach the patient to avoid gastric irritants, such as smoking alcohol,
aspirin containing products, caffeine, NSAIDs and food that causes
irritation.
Antidiarrheals
Drug used to control diarrhea is called antidiarrheal drugs.
Mechanism of action
Antidiarrheals active opioids receptor in G.I. tract to decrease
intestinal motility and to increase the absorption of fluid and
sodium in the intestine.
Indications / Uses
To treat underlying cause of diarrhea.
To control the relive symptoms of acute and chronic diarrhea.
Drug example and doses
1. Loperamide 2-4mg
2. Diphenoxylate 5-10mg
3. Octreotide 100-250 mcg TID
4. Polycarbophil / Bismuth subsalicylate 60 ml
6hourly suspension
Anti diarroheals
Contraindication / Precautions- •Contraindicated in abdominal
pain of unknown pathology. •There is an increase risk of
megacolon in clients with inflammatory bowel disorders. This
could lead to a serious complication such as perforation of bowel.
Adverse effects - •Constipation. •Abdominal pain. •Pain at the
injection site. •Nausea. •Gall stones. (with octreotide)
•Drowsiness. (with diphenoxylate, and loperamide.
Drug interactions - •Use diphenoxylate or loperamide with similar
acting drugs causes additive anticholinergic effects.
Nursing Responsibilities
Assess for the abdominal pain and distension, nausea, vomiting, and
bowel sounds.
Assess the patients skin turgor and monitor fluid and electrolyte balance
for evidence of dehydration resulting from diarrhea.
Advise patient to avoid drinking plain water because it does not content
necessary electrolytes that have been loss in the stool.
Advise clients to avoid caffeine. Caffeine exacerbate diarrhea by
increasing GI motility.
Nurses responsibility
Client with severe case of diarrhea may be hospitalized
for management of diarrhea.
Know that high dose, long term use of defenoxin or
diphenoxylate may cause dependence
Histamines (Histamine Receptors
Antagonist/H2 blockers)
They are also called as H2 antagonists. These agents
block the action of histamine, thus it reduce the
amount of acid released into the stomach. They also
promote ulcer healing.
Mechanism of action : They inhibit gastric acid
secretion by inhibiting the action of histamine and
histamine 2 receptors in gastric parietal cells.
Histamines
Drug example and doses
1. Cimetidine 400mg B.D.
2. Ranitidine 150mg twice daily.
3. Famotidine 20-40 mg. 4 Nizatidine 150 mg twice daily.
Indications / Uses - •Gastritis. •Reflux esophagitis. •Indigestion. •Peptic ulcer.
•Heart burn.
Contraindication / Precautions - •Hypersensitivity with this drug. •Breast
feeding women. •Cautiously use in pregnant women.
Adverse effects - •Dizziness. •Headache. •Gynecomastia. •Confusion.
•Impotence. •Loss of libido due to antiandrogenic action.
Histamines
Drug interactions - •Antacids may inhibit absorption of H2 receptors
antagonists. •Cigarette smoking increases gastric acid secretions and may
decreases the effectiveness of H2 receptors antagonists.
Nursing Responsibilities
•Don’t give an antacid within 1 hour of administration of H2 receptors
antagonists it may decrease the absorption.
•Teach the patients to avoid gastric irritants, such as smoking alcohol aspirin
containing products, caffeine, NSAID’s and food that cause G.I. irritation.
•Teach the patient that smoking worsens ulcer disorders and counteracts the
effect of H2 blockers.
References
1. Dr. P.K. Panwar, Essentials of pharmacology for nurses, AITBS pub. 2017, India, Pg no. 38
– 48.
2. Dr. Suresh k sharma, Textbook of pharmacology, pathology & genetics for nurses,
Jaypee pub. 2016 India Pg no 132 – 160.
3. Tara v. Shanbhag, Smita shenoy, Pharmacology preparation manual for undergraduate,
Elsevier pub. 2014. Pg no. 259 – 280.
4. Marilyn Herbert – Ashton, Nancy Clarkson, Pharmacology, Jones & Barllet pub 2010
India, Pg no 527 – 550.
5. Govind s. mittal, Pharmacology at a glance, Paras medical book pub. 2009 India 35 – 40.
6. Madhuri Inamdar, Pharmacology in nursing, Vora medical pub. 2006 India 1st edition, Pg
no 99 – 110.