Drugs acting on
Gastrointestinal Tract
Lecture#01
Contents
➢Introduction
➢Brief overview of physiology of
Gastrointestinal Tract
➢Classification of Drugs Acting on
Gastrointestinal Tract
➢Emetics and Anti emetics
Introduction
• Human digestive system is composed of the
Gastrointestinal tract that includes oral cavity,
pharynx, esophagus, stomach, small and large
intestines. Associated with G.I.T are the following
accessory organs: salivary glands, liver, gallbladder,
and pancreas
• Esophageal sphincter and Pyloric sphincter separate
esophagus and stomach, and stomach and small
intestine respectively.
• The gastrointestinal tract is an organ system within
humans and other animals which takes in food,
digests it to extract and absorb energy and nutrients,
and expels the remaining waste as feces
Physiology of Gastrointestinal Tract
Functions of GIT:
• Ingestion
• Transport
• Absorption
• Digestion
• Secretion
• Excretion
Classification of Drugs Acting on G.I.T
➢Emetics and Anti emetics
➢Laxatives or Purgatives
➢Anti-diarrheal agents
➢Drugs for treatment of Peptic and duodenal
ulcers
➢Drugs for treatment of Inflammatory bowel
diseases
➢Drugs affecting bile flow and Cholelithiasis
Emetics and Anti emetics
• Emesis or vomiting: Emesis is the involuntary, forceful expulsion
of the contents of stomach through the mouth
• Nausea: Nausea is a symptom characterized by pronounced
stomach discomfort and the sensation of wanting to vomit.
• Emetics: A medicine or other substance that causes vomiting
• Anti emetics: An antiemetic is a drug that is effective against
vomiting and nausea. Anti emetics are typically used to treat
motion sickness and the side effects of opioid analgesics, general
anesthetics, and chemotherapy directed against cancer.
Pathophysiology of vomiting
• Act of vomiting can be initiated by Stimulants,
that can either act centrally or directly in the
bowel. Following can be triggered to initiate
emesis ;
❑Vomiting center
❑Chemoreceptor trigger zone (CTZ)
❑Vestibular system (Labyrinth)
❑Higher centers of brain
❑Stomach
Vomiting center
❖ The vomiting centre initiates, regulates and controls
the act of emesis.
❖It is located in the medulla oblongata
❖It primarily consists of Muscarinic receptors and also
Histamine-1 receptors
❖Vomiting center receives afferent impulses from CTZ,
vestibular nuclei, abdominal afferents (via the vagus
nerve) and higher centers of brain to initiate physical
act of vomiting (emetic reflex).
Chemoreceptor trigger zone (CTZ)
❖CTZ is located in the medulla oblongata within the area
postrema, which is outside of the blood–brain barrier
❖CTZ communicates with other structures in
the vomiting center to initiate vomiting
❖It is stimulated by endogenous cytotoxic agents
circulating in blood
❖After activation , it stimulates vomiting center which
leads to emesis
❖It has Dopamine (D2) receptors and Serotonin (5-HT3)
receptors
Vestibular system (Labyrinth)
❖The Vestibular system is part of the inner ear. It is a
sensory system that is responsible for providing our
brain with information about motion, head position,
and spatial orientation; it also is involved with motor
functions that allow us to keep our balance, stabilize
our head and body during movement, and maintain
posture.
❖It cause nausea and vomiting due to motion sickness
❖ It send signals to brain via Vestibular cochlear III nerve
(V-III nerve) to an area known as vestibular nuclei, that is
located in pons of brain stem
❖ Vestibular nuclei contains two types of receptors i-e
Histamine-1 (H1) receptors and Muscarinic receptors.
❖ If vestibular nuclei is stimulated due to motion
sickness or morning sickness, it stimulates CTZ, which
then stimulates vomiting center and cause emetic reflex.
Higher centers of brain
❖Afferent impulses from higher centers of brain such
as bad smell, sight, emotional feelings etc sends
signals to vomiting center via muscarinic receptors
and causes emetic reflex.
Stomach
❖Gastric mucosa consists of many cells, one of them is
Enterochromaffin cells, which release serotonin in
response to any cytotoxic agents.
❖Serotonin then activates 5-HT3 receptors located on
sensory nerve fibre (vagus nerve) innervating the
area, which then activates vomiting centre and also
CTZ and cause emetic reflex.
Emetic reflex
• Vomiting center, after being stimulated by
different factors sends signals to GIT and
causes;
❑Relaxation of lower esophageal sphincter
❑Contraction of diaphragm and abdominal muscles
❑Increase intra abdominal pressure
❑Closes epiglottis
Anti emetic Drugs
1. H1 receptor antagonists
2. 5-HT3 receptor antagonists
3. D2 receptor antagonists
4. Muscarinic receptor antagonists
H1 receptor antagonists
Drugs:
➢ Diphenhydramine
➢ Promethazine
➢ Cyclizine
➢ Cinnarzine
Mechanism of action:
These drugs block the H1 receptors in vestibular nuclei and
prevent vomiting caused due to motion sickness and morning
sickness. They also block H1 receptors centrally in vomiting
center and some of the drugs also have anti cholinergic effects
by blocking muscarinic receptors at same sites.
Uses:
1. motion sickness
2. morning sickness in pregnancy
Other uses:
Mainly used in allergic reactions
Side effects:
1. Drowsiness
2. Sedation
3. Anti-cholinergic effects
5-HT3 receptor antagonists
Drugs:
➢ Ondansatron
➢ Dolasatron
➢ Palanosatron
➢ Granisatron
➢ Tropisatron
Mechanism of action:
They antagonize the effects of serotonin by blockade of 5-HT3
receptors at intestinal vagal afferents. And additionally central
blockade of 5-HT3 receptors in the vomiting center and CTZ also
play important role.
Uses:
1. Chemotherapy patients
▪The drugs are most effective when given by i/v
injection 30 minutes prior to administration of
chemotherapy .
2. Radiotherapy patients
3. Post operative nausea and vomiting (PONV)
Side effects:
These drugs are well tolerated with few side effects
➢Headache
➢Dizziness
➢GI upset
Dopamine 2 Receptor antagonist
Drugs:
➢ Chlopramazine Phenothiazines
➢ Droperidol Butyrophenones
➢ Metaclopromide Benzamides
Mechanism of action:
The anti emetic property of these drugs is through binding
and inhibiting the activation of D2 receptors at CTZ
Uses:
1. Chemotherapy patients
2. Radiotherapy patients
3. Used to prevent and treat postoperative nausea and
vomiting.
Other uses:
Mostly used as anti psychotic as most of anti psychotic
drugs are D2 receptors antagonists.
Side effects:
➢Sedation
➢Hypotension
➢Fatigue
➢Extrapyramidal side effects
oDystonia
oAkathesia
oAkinesia
Muscarinic receptor antagonists
Drugs:
➢ Hyoscine (Scopolamine)
Mechanism of action:
Block the effects of ACh by blocking muscarinic receptors in
vestibular nuclei and vomiting center.
Uses:
1. Mostly used in motion sickness
2. PONV
Side effects:
➢ Anti-cholinergic effects
Emetics
• Emetics are drugs or substances used to induce
vomiting
• They are used to treat poisoning
Drugs:
1. Dopamine agonists
❑ E-g- Levodopa
2. Digoxin
3. Chemotherapy
4. Syrup of ipecac
Syrup of ipecac
Mechanism of action :
• It acts both by locally irritating gastric mucosa
and centrally by stimulating CTZ .
Uses:
➢Induce vomiting in poisoning
