Pharmacology of the

GIT system

CIC Ragasa, RN-MD

 Drugs affecting GI secretions
5 types of drugs that affect gastric acid secretions and
are useful for the treatment of peptic ulcer.
1. Histamine (H2) receptor antagonist/blockers
2. Antacids
3. Proton pump inhibitors
4. Mucosal protectants
5. Prostaglandin analogs
General indication of the drugs affecting gastric
acid secretion
• Peptic ulcer
• Gastritis
• Patient on NPO to prevent stress ulcer
 General time of administration of the drugs
affecting gastric acid secretion
Anti-ulcer drugs Prototype Best time to give

Histamine (H2) Cimetidine With FOOD or ONE

receptor
hour after ANTACID
antagonist/blockers

Antacids AlOH and MgOH Usually after meals

Proton pump Omeprazole BEFORE MEALS

inhibitors
Mucosal Sucralfate BEFORE MEALS
protectants
Prostaglandin Misoprostol WITH MEALS
analog
 The H2 Blockers- “tidines”
Prototype: Cimetidine

• 1. Ranitidine
• 2. Famotidine
• 3. Nizatidine
 The H2 Blockers- “tidines”
• Mechanism of Action :
– Decrease gastric acid secretion by blocking H2
receptors
• Uses :
– Prevent & treat gastric duodenal ulcers, GERD &
stress ulcers
– Prevention of ulcer recurrence
 The H2 Blockers- “tidines”
Precautions and Contraindications
• Any known allergy
• Conditions such as pregnancy, lactation, renal
dysfunction and hepatic dysfunction should
warrant cautious use.
• Nizatidine can be used in hepatic dysfunction.
 The H2 Blockers- “tidines”
Dynamics- Side effects/adverse effects
• GIT= diarrhea or constipation
• CNS= Dizziness, headache, drowsiness,
confusion and hallucinations
• Cardio= arrhythmias, HYPOTENSION (related to
H2 receptor blockage in the heart)
• Cimetidine= Gynecomastia and impotence in
males
 The H2 Blockers- “tidines”
Nursing considerations:
• Administer the drug WITH meals at
BEDTIME to ensure therapeutic level
• One hour after Antacids
• Stress the importance of the continued use
for the length of time prescribed
 The H2 Blockers- “tidines”
Nursing considerations
• Monitor the cardiovascular status especially
if the drugs are given IV
• Warn patient of the potential problems of
increased drug concentration if the H2
blockers are used with other drugs or OTC
drugs. Advise consultation first!
 The Antacids
The following are the common antacids that
can be bought OTC:
• Aluminum salts (Amphojel)
• Calcium salts (carbonate)
• Magnesium salts (milk of magnesia)
• Sodium bicarbonate
• Magaldrate (aluminum and magnesium
combination)
 The Antacids
Pharmacodynamics: drug action
• Promote healing of ulcer by neutralizing
hydrochloric acid & reducing pepsin activity.
• They do not affect the rate of gastric acid
secretion.
 The Antacids
Uses
• To treat peptic ulcers by reducing gastric acid
concentration
• To prevent stress ulcersSymptomatic relief of
upset stomach associated with hyperacidity
• Some antacids contains Simethicone (anti-gas
agent) that relieves flatulence.
• Special use of AMPHOGEL (aluminum
hydroxide): to BIND phosphate
 The Antacids
Precautions of Antacid Use
• Known allergy is a clear contraindication
• Caution should be instituted if used in
electrolyte imbalances, GI obstruction and
renal dysfunction.
• Sodium bicarbonate is rarely used because of
potential systemic absorption metabolic
alkalosis!!!
 The Antacids
Pharmacodynamics: Effects of drugs
1. GIT= rebound acidity; alkalosis may occur.
• Calcium salts may lead to hypercalcemia
• Magnesium salts can cause DIARRHEA
• Aluminum salts may cause CONSTIPATION and
Hypophosphatemia by binding with
phosphates in the GIT.
2. Fluid retention due to the high sodium content
of the antacids.
 The Antacids
Nursing Considerations:
• Administer the antacids apart from any other
medications by ONE hour before or TWO
hours after- to ensure adequate absorption
of the other medications
• Tell the patient to CHEW the tablet
thoroughly before swallowing.
Follow it with one glass of water
• Regularly monitor for manifestations of acid-
base imbalances as well as electrolyte
imbalances
 The PPI
These are the newer agents for ulcer treatment
• The “prazoles”
Prototype: Omeprazole
• Lansoprazole
• Esomeprazole
• Pantoprazole
 The PPI
Pharmacodynamics: drug action
• Decrease gastric acid secretion by inhibiting
the enzyme hydrogen/potassium Atpase in
gastric parietal cells.
• The “pump” in the parietal cell is the H-K
ATPase enzyme system on the secretory
surface of the gastric parietal cells
 The PPI
Clinical use of the PPIs
• To prevent & treat gastric & duodenal ulcers,
GERD & stress ulcers.
• Prevention of ulcer recurrence.
 The PPI
Precautions with the use of the PPIs
• Known allergy is a clear contraindication
• Dizziness, headache, rashes, GI disturbance,
fatigue, thirst
 The PPI
Nursing considerations:
• Administer the drug BEFORE meals. Ensure
that patient does not open, chew or crush
the drug.
• Provide safety measures if CNS dysfunction
happens.
• Arrange for a medical follow-up if symptoms
are NOT resolved after 4-8 weeks of therapy.
 The Mucosal Protectant
Sucralfate (Caralfate/ Iselpin)
• This is given to protect the eroded ulcer sites
in the GIT from further damage by acid and
digestive enzymes
 Sucralfate
Action of drug
• It forms an ulcer-adherent complex at
duodenal ulcer sites, protecting the sites
against acid, pepsin and bile.
 Sucralfate
Clinical use of sucralfate
• Short and long term management of
duodenal ulcer.
• NSAIDs induced gastritis
• Prevention of stress ulcer
• Treatment of oral and esophageal ulcers due
to radiation, chemotherapy or sclerotherapy.
 Sucralfate
Precautions on the use of Sucralfate
• known allergy to the drug
• Sleepiness, constipation, dry mouth, rashes,
pruritus, back pain
 The Mucosal Protectant
Nursing Considerations
• Administer drug ON AN EMPTY stomach, 1 hour
before meals , or 2 hour after meals and at
BEDTIME
• Monitor for side-effects like constipation and GI
upset
• Encourage intake of high-fiber foods and increased
fluid intake
 Prostaglandin analogue
Misoprostol
• This agent is a synthetic prostaglandin E1
analog that is employed to protect the lining
of the mucosa of the stomach
 Prostaglandin analogue
Misoprostol: Pharmacodynamics
• Being a prostaglandin analog, it inhibits
gastric acid secretion to some degree
• It INCREASES mucus production in the
stomach lining.
 Prostaglandin analogue
Misoprostol: Clinical use
• NSAIDs-induced gastric ulcers
• Duodenal ulcers unresponsive to H2
antagonists
 Prostaglandin analogue
Precautions of Misoprostol Use
• This drug is CONTRAINDICATED during pregnancy
because it is an abortifacient.
• Women should be advised to have a negative
pregnancy test within 2 weeks of beginning therapy
and should begin the drug on the second or third
day of the next menstrual cycle.
• They should be instructed in the use of
contraceptives during therapy.
 Prostaglandin analogue
Nursing Considerations
• Administer four times daily with meals and at
bedtime
• Obtain pregnancy test within 2 weeks of beginning
therapy.
• Begin the therapy on second or third day of
menstrual period to ensure that the woman is not
pregnant
 Laxatives
• Generally used to INCREASE the passage of
the colonic contents
• The general classifications is as follows:
1. Chemical stimulants- irritants
2. Mechanical stimulants- hyperosmotic
agents and saline cathartics
3. Lubricants and stool softeners
 Laxatives
• Therapeutic Use :
– They promote bowel evacuation by a wide
variety of actions
– To prepare bowel for certain diagnostic
procedures like colonoscopy
 Contraindications in Laxative use
• ACUTE abdominal disorders
– Appendicitis
– Diverticulitis
– Ulcerative colitis
 Chemical Stimulant Cathartics
Prototype: Bisacodyl
Irritant laxatives:
• 1. Castor oil
• 2. Senna
• 3. Cascara
• 4. Phenolphthalein
 Chemical Stimulant Cathartics
Pharmacodynamics
• These agents DIRECTLY stimulate the nerve
plexus in the intestinal wall
• The result is INCREASED movement or
motility of the colon
 Mechanical Stimulant Cathartics
Prototype: LACTULOSE (Cephulac)
Bulk-forming laxatives
• 1. Magnesium (citrate, hydroxide, sulfate)-
saline cathartic
• 2. Psyllium
• 3. Polycarbophil
 Mechanical Stimulant Cathartics
Pharmacodynamics
• These agents are rapid-acting laxatives that
INCREASE the GI motility by
– Increasing the fluids in the colonic material
– Stimulating the local stretch receptors
– Activating local defecation reflex
 Lubricants-Stool softener
Prototype: Docusate

• 1. Glycerin
• 2. Mineral oil
 Lubricants-stool softeners
Pharmacodynamics
• Docusate increases the admixture of fat and
water producing a softer stool
• Glycerin and Mineral oil form a slippery coat
on the colonic contents
 Pharmacokinetics:
Common Side-effects of the Laxatives
• Diarrhea
• Abdominal cramping
• Nausea
• Weakness
• CATHARTIC dependence
 Laxative
IMPLEMENTATION
1. Emphasize that it is use on a SHORT term
basis
2. Provide comfort and safety measures like
ready access to the bathroom, side-rails
3. Administer with a full glass of water
 Laxative
IMPLEMENTATION
4. Encourage fluid intake, high fiber diet and
daily exercise
5. DO NOT administer if acute abdominal
condition like appendicitis is present
6. Advise to change position slowly and avoid
hazardous activities because of potential
dizziness
 The Anti-diarrheals
• Drugs that inhibit peristaltic reflex and
reduce gastrointestinal hypermotility
• Examples :
1. Diphenoxylate Hydrochloride
2. Loperamide (Diatabs)
 The Anti-diarrheals
Type Prototype Action

Local reflex Bismuth Locally coats the lining

of the GIT to soothe
inhibitor subsalicylate irritation

Local anti- Loperamide Directly inhibits the

intestinal muscle
motility activity to SLOW
peristalsis
Central acting Opium Stops GIT spasm by
CNS action
agent derivatives
(paregoric)
 Clinical Indications of drug use
• Relief of symptoms of acute and chronic
diarrhea
• Prevention and treatment of traveler's
diarrhea
Contraindications of anti-diarrheal Use
• Poisoning
• Drug allergy
• GI obstruction
• Acute abdominal conditions
 Side effects
• Constipation
• Nausea, vomiting
• Abdominal distention and discomfort
• TOXIC MEGACOLON
 Emetics and Anti-emetics
Emetic Agent
• Syrup of Ipecac

Anti-emetics
• 1. Phenothiazines
• 2. Non-phenothiazines
• 3. Anticholinergics/Antihistamines
• 4. Serotonin receptor Blockers
• 5. Miscellaneous
 EMETIC
• Prototype: Ipecac Syrup
• Actions :
– Ipecac syrup irritates the GI mucosa locally,
resulting to stimulation of the vomiting center
• Use :
– To induce vomiting as a treatment for drug
overdose and certain poisonings
 EMETIC
Contraindications of Ipecac use
• Ingestion of CORROSIVE chemicals
• Ingestion of petroleum products
• Unconscious and convulsing patient
 EMETIC
Pharmacokinetics: side effects of Ipecac
• Nausea
• Diarrhea
• GI upset
• Mild CNS depression
• CARDIOTOXICITY if large amounts are
absorbed in the body
 ANTI-EMETICS
• These are agents used to manage nausea and
vomiting
• They act either locally or centrally
• In general, they may inhibit the
chemoreceptor trigger zone in the medulla
by blocking DOPAMINE receptor
 ANTIEMETICS
Anti-emetic types Common examples

Phenothiazines Prochlorperazine,
Promethazine
Non-phenothiazines Metoclopramide

Anticholinergics and Meclizine, buclizine

Antihistaminics
Serotonin Receptor “setron”- dolasetron
blockers
Miscellaneous Dronabinol, hydroxyzine
 ANTIEMETICS
Types Pharmacodynamics

Phenothiazines Centrally block the vomiting center in

the medulla

Non-phenothiazine Reduces the responsiveness of the

nerve cell in the medulla; also blocks
the dopamine receptors
Anticholinergics Block the transmission of the impulses
to the medulla

Serotonin receptor Centrally and locally inhibits the

blockers serotonin receptors

Miscellaneous Act in the CNS , either in the medulla or

in the cortex
 ANTIEMETICS
Types Clinical Use

Phenothiazines N/V associated with

anesthesia, intractable
hiccups
Non-phenothiazine N/V associated with chemical
stimulation
Anticholinergics N/V associated with motion
sickness
Serotonin-receptor N/V associated with
Blockers chemotherapy
Miscellaneous N/V associated with
chemotherapy
 ANTIEMETICS
Indications
• 1. Prevention and treatment of vomiting
• 2. Motion sickness
 ANTIEMETICS
Contraindications
• 1. Severe CNS depression
• 2. Severe liver dysfunction
 ANTIEMETICS
Pharmacokinetics: Side-effects
1. PHOTHOSENSITIVITY
2. Drowsiness, dizziness, weakness and tremors
and DEHYDRATON
3. Phenothiazines= autonomic anti-cholinergic
effects like dry mouth, nasal congestion and
urinary retention
Metoclopramide= EPS due to dopamine
receptor blockage
 ANTIEMETICS
IMPLEMENTATION
1. Assess patient’s intake of other drugs that
may cause dangerous drug interaction
2. Emphasize that this is given on a short term
basis
 ANTIEMETICS
IMPLEMENTATION
3. Provide comfort and safety measures
– Advise to change position slowly
– Avoid hazardous activities
– Provide mouth care and ice chips
– Monitor for dehydration and offer fluids if it
occurs
 ANTIEMETICS
IMPLEMENTATION
4. Protect from sun exposure
– Sunscreens
– Protective covering
5. Provide health teaching