DRUGS AFFECTING

THE
GASTROINTESTINAL
TRACT
Diseases of the GI Tract
•Dental caries and periodontal disease

•Peptic Ulcers

•Diverticulitis

•Colorectal cancer

•Hepatitis

• Anorexia nervosa
 Underlying Causes of GI
Disorders
•Dietary excess

•Stress

• Hiatal hernia

•Esophageal reflux

• Adverse drug effects

•Peptic ulcer disease

Effect of Drugs on GI Secretions

• Decrease Gl secretory activity

• Block the action of GI secretions

•Form protective coverings on the GI lining to

prevent erosion from GI secretions

•Replace missing Gl enzymes that the GI tract

or ancillary glands and organs can no longer
produce
 Peptic Ulcers
Definition

•erosions in the lining of the stomach and adjacent areas

of the GI

tract

" Symptoms "

• Gnawing, burning pain, often occurring after meals

• Cause

Bacterial infection by Helicobacter pylori bacteria

Drugs Used in the Treatment of Ulcers

• Histamine-2 (H2) antagonists

• Block the release of hydrochloric acid in response to gastrin

• Antacids

•interact with acids at the chemical level to neutralize them

• •proton pump inhibitors Suppress the secretion of hydrochloric acid

into the lumen of the stomach
Drugs Used in the Treatment of Ulcers (cont.)

•Antipeptic agents

• Coat any injured area in the stomach to prevent

further injury from acid

•Prostaglandins

•Inhibit the secretion of gastrin and increase the

secretion of the mucous lining of the stomach,
providing a buffer
Sites of Actions of Drugs
Affecting

Gastrointestinal Secretions
 Patients Who May Require Digestive Enzyme
Supplements
•Saliva supplements

• Stroke

• Salivary gland disorder

• Extreme surgery of the head and neck

• Pancreatic enzyme supplements

• Common duct problems

• Pancreatic disease

•Cystic fibrosis
 H2 Antagonists

•Cimetidine (Tagamet, Tagamet HB) The first drug in this class to be developed

•Ranitidine (Zantac) Longer acting and more potent than cimetidine

•Famotidine (Pepcid, Pepcid AC) Similar to ranitidine, but much more potent

•Nizatidine (Axid) Newest drug in this class similar to ranitidine indicated for
patients with liver dysfunction
 Indications for H2 Antagonists

• Short-term treatment of active duodenal •Prophylaxis of stress-induced

ulcer or benign gastric ulcer ulcers acute upper GI bleeding in
critical patients
•Treatment of pathological

•Treatment of erosive
•hypersecretory conditions such as
gastroesophageal reflux
ZollingerEllison syndrome (a condition
characterised by severe peptic ulceration,
gastric hypersecretion, elevated serum • Relief of symptoms of heartburn,
gastrin, and gastrinoma (a tumour) of the acid indigestion, and sour stomach
pancreas or duodeum) (OTC preparations)
 Types of Antacids

• bicarbonate (Bell/Ans)
• Aluminum salts
(Amphojel and others)
•Calcium carbonate
(Calciday-667, Tums, and
•Magaldrate
others)
(Lowsium, Riopan)

•Magnesium salts (Milk of

Magnesia and others)
Focus on the Prototype Antacid Sodium Bicarbonate

•Indications Hyperacidity GI bleeding and •Oral route Onset rapid peak

stress ulcers severe diarrhe a metabolic 30min duration 13 h
acidosis certain drug intoxications
minimize uric acid crystallization • T½ Unknown excreted
unchanged in urine
•Actions Neutralizes or reduces gastric
acidity resulting in an increase in gastric
pH inhibits the proteolytic (pertaining to
any substance that promotes the
breakdown of protein) activity of pensin
 Proton Pump Inhibitors

"Types"
" action "
Omeprazole (Prilosec),
•Suppress gastric acid secretion
esomeprazole (Nexium),
by specifically inhibiting H,K-
ATPase enzyme system on the lansoprazole (Prevacid),
secretory surface of the parietal
cells pantoprazole (prootonix),

rabeprazole (Aciphex)
Antipeptic Agent

• Sucralfate (Carafate)

• Forms a protective coating over the eroded

stomach lining

• Protects it from acid and digestive enzymes

• aids healing
 Prostaglandin

• Misoprostol (Cytotec)

• Blocks gastric acid secretion

• Increases the production of bicarbonate and mucous

lining in the stomach
 DRUGS ACTING ON GIT

1. Antiulcer drugs

2. Drugs for Achlorhydria

3. Emetics & Antiemetics

4. Antidiarrhoeal agents

5. Dugs for constipation/Laxatives

 PEPTIC ULCER

+Characterized by excessive secretion of acid (acidity)

-Ulcers mean injuries/wounds due to long term

existence of acidity

-Occurs in the areas highly exposed to gastric acid

-Stomach and duodenum are highly exposed to acid

-Ulcers in the stomach called as gastric ulcers

-Ulcers in the duodenum called as duodenal ulcers

 Homeostasis

Maintenance of balance /equilibrium inside the body

called as homeostasis.

The major reason for disorders is disturbance in

homeostasis.

Ex:

Maintenance of acid secretion, body temperature, blood

pressure, pulse rate etc.
 ANTIHISTAMINES(H₂ RECEPTOR
BLOCKERS

Cimetidine - first drug, antiandrogenic

action, withdrawn from the market

Ranitidine - Popular brand names are

RANTAC, ZANTAC

Famotidine - Most potent drug

 Proton Pump Inhibitors
(H+k+ ATPase Inhibitors)

-Highly effective

-Long term use decrease the release

of intrinsic factor which is essential
for the absorption of vitamin B12
that results in pernicious anemia
 ANTICHOLINERGICS

-Nonselective drugs have side

effects like dry mouth, dry skin, dry
eye

-Selective M₁ blockers are

preferred
 PG ANALOGUES

-Decrease acid secretion

-Increase bicarbonate and mucus secretion

-also called as cytoprotective agents

-used to treat NSAIDS induced ulcers

NSAIDS inhibit Cyclooxygenase
and inhibit the production of
PGs that result in ulcers (PGs
are defensive factors).
 GASTRIN ANTAGONISTS

-Proglumide cholecystokinin
antagonist, which blocks both

-the CCK, and CCK, subtypes.

-Not preferred due to toxicity

 ANTACIDS

-Antacids are basic/alkaline

substances due to
their alkalinity they will
neutralize the gastric acid.
SYSTEMIC ANTACIDS

They enter into systemic

circulation, they produce
systemic alkalosis and
they are not preferred due
to this reason.
 NONSYSTEMIC ANTACIDS

-They will not enter into systemic circulation,

produce local action and they are highly
preferred.

-Aluminium salts produce constipation and

magnesium salts produce laxation, hence both
should be used in combination.

-MAGALDRATE is a combination of both in the body

broken down into aluminium hydroxide and
magnesium hydroxide.
 ULCER PROTECTIVES

They form a layer on the

ulcers and they will protect
the ulcers from direct
exposure to acid or any other
irritants
 ULCER HEALING DRUGS

Carbenoxolone sodium obtained from

Glycyrrhiza glabra (Liquorice).

Due to lignin content and saponins

they exhibit wound healing property
 ANTI H.PYLORI DRUGS

-H. Pylori is a gram negative

bacteria

-Treatment includes some of

antibacterials and
antiprotozoals
 DRUGS FOR ACHLORHYDRIA

-Rarest condition

- Majorly seen in children till 3 years of age

-Due to this they have frequently indigestion,

vomiting and infections

-Drugs used include Cholinergics like

Carbachol, Bethanechol
 EMETICS & ANTIEMETICS

-Emetics are the agents which produce

nausea and vomiting.

-The only use of emetics is in the

treatment of poisoning.
 But they have some limitations like/they are not
suitable in the following conditions:

If the patient is unconscious

If the poison is already absorbed

If the poison is strong acid/ strong base/corrosive

which cause further damage to the

If the poison is detergents/petroleum products which

could be aspirated into lungs

Substance ingested likely to cause rapid onset of

drowsiness or seizures
Examples:

-ipecacuanha (Emetine)

-Mustard

-salt water
ANTIEMETICS:

These are all agents which

prevent or stop the
occurance of nausea and
vomiting.
 MOTION SICKNESS
Any form of travel on land, in the air or on the water can
bring on the uneasy feeling of vomiting.

Children between the ages of 2 and 12 are most likely to

suffer from motion sickness.

Motion sickness is caused by a conflict between signals

arriving in the brain from the inner ear, which forms the
base of the vestibular system, the sensory apparatus that
deals with movement and balance, and which detects
motion mechanically.

Motion sickness occurs due to stimulation of muscarinic

and H, receptors in vestibular apparatus which further
stimulates CTZ.
 CONDITIONS ASSOCIATED
WITH VOMITING

Motion sickness (Vomiting during Journey/motion)

Morning sickness (Vomiting during pregnancy)

Drugs like Levodopa

Conditions like Migraine

Anticancer drugs and radiation therapy

Excessive eating, excessive drinking & Bad smell/odor

 CLASSIFICATION OF ANTIEMETICS

1. Anticholinergics

2. Antihistamines (H, receptor blockers)

3. D₂ receptor blockers (Neuroleptics)

4. 5-HT receptor blockers

5. NK, receptor blockers

6. Gastroprokinetic agents

7. Adjuvant antiemetics
 ANTICHOLINERGICS

Ex: Hyoscine (Scopolamine),

Dicyclomine

Hyoscine available as transdermal

patches and those patches applied
behind the pinna.
 ANTIHISTAMINES (H, RECEPTOR BLOCKERS)

Ex:

Promethazine, Diphenhydramine, Dimenhydriate,

Cyclizine.

Anticholinergics and antihistamines exclusively

used for the treatment of motion sickness and they
should be taken atleast 1 hour before the
commencement of journey and they are also
effective in morning sickness.
 D₂ RECEPTOR BLOCKERS
(NEUROLEPTICS)

Which are mainly used to treat

→ Morning sickness (Vomiting during pregnancy)

→ Levodopa induced vomiting
-Migraine induced vomiting

Ex: Chlorpromazine, Haloperidol- Extrapyramidal

side effects (Parkinsonism like symptoms)
5-HT, RECEPTOR BLOCKERS

Which are mainly used to treat

-Anticancer drug induced vomiting

-radiation therapy induced vomiting

Ex: Ondansetron, Granisetron

 NK1, RECEPTOR BLOCKERS

Which are used to treat substance

P induced vomiting due to
chemotherapy and in case of
injuries

Ex: Aprepitant
 GASTROPROKINETIC AGENTS

Which increase the motility of GIT allowing the

fast passage of contents from stomach to
intestine.

As a result of this mechanism contents present

in stomach for less time hence there is no chance
of vomiting.

Due to this mechanism they produce diarrhoea as

a side effect.

They stimulate 5-HT receptors present in GIT

allowing the release of Acetylcholine which
increase the peristaltic movement of GIT.
 ADJUVANT ANTIEMETICS

Which alone may not have antiemetic

property but they increase the activity
of other antiemetics.

Ex: Benzodiazepines Corticosteroids

Cannabinoids (DRONABINOL, NABILONE)

ANTIDIARRHOEAL AGENTS
 → Used for the treatment of diarrhoea
→ Diarrhoea is characterized by increase in
the frequency of passage of

→ Mostly diarrhoea is a disease and very few

cases it is considered as a disorder.

→ Most of the times diarrhoea occurs due to

contamination with microorganisms
(Disease) and some times it occurs due to
increased peristaltic movement of GIT
(Disorder).
 Antidiarrhoeal agents are
classified into two types:

1. Specific Antimicrobial agents

Which are used when the diarrhoea is caused by

specific microorganism

II. Nonspecific Antidiarrhoeal agents

Which are used when the diarrhoea is caused by

increased peristaltic movement of GIT
 SPECIFIC ANTIMICROBIAL AGENTS

Antibacterials like

Ex:

Fluoroquinolones like Ciprofloxacin, Norfloxacin,

Gatifloxacin, Levofloxacin, tetracyclines,
Co-trimoxazole

Antiprotozoals like metonidazole, Tinidazole

NONSPECIFIC ANTIDIARRHOEAL AGENTS

They are classified into 2 types

I. ANTISECRETORY DRUGS
(Drugs which reduce PGs)

II. ANTIMOTILITY DRUGS

 ANTIMOTILITY DRUGS
EX:
1. OPIOIDS

Morphine

Loperamide

Diphenoxylate

These drugs act through u opioid receptors

present on colon.

2. ANTICHOLINERGICS
 DRUGS FOR CONSTIPATION
Constipation is characterized by decrease in the
passage of stools or difficulty in the passage of
stools.

Drugs for include:

Aperients - Very milder

Laxatives → Milder
Purgatives - Stronger

Cathartics - very Stronger

 CLASSIFICATION OF LAXATIVES

They are classified into 4 types:

1. Irritant/Stimulant laxatives

2. Bulk forming laxatives

3. Osmotic/Saline laxatives

4. Surfactant laxatives/ Stool softeners

 IRRITANT/STIMULANT LAXATIVES

→ They act by increasing peristaltic

movement of GIT

-They act by increasing PGs

-They act by increasing secretions

Ex:

1. DIPHENYLMETHANES: Bisacodyl

2.ANTHRAQUINONES: Senna, Cascara

3. FIXED OILS: Castor oil

 BULK FORMING LAXATIVES

They are not digested and they are

absorbed. not

Due to indigestion, all bulky material

reach to the large intestine, increases
bulkiness and causes free passage of
stools.
OSMOTIC/SALINE LAXATIVES

They are not absorbed and they

cause retention of water.

Unabsorbed compounds will reach

large intestine and due to retention
of water swelling takes place that
increases bulkiness.
 SURFACTANT LAXATIVES/
STOOL SOFTENERS

-due to increased reabsorption of water

hardening of stools will result that
causes difficulty in the passage of
stools.

Drugs are surfactants which reduce

interfacial tension and increases water
incorporation that soften the stools.
 HANKYOU
T !
Group 4
Duque, Niño Rexon
Esmenda, Jenny
Estorba, Faith
Fernandez, Jan Gabriel