2/28/2021

Gastrointestinal
Tract Drugs
Pharmacist
Marwan Qasim

GIT Drugs
H2 Proton Anti-
Anti-
Antacids receptor pump Laxatives Diarrheal
emetics
blockers inhibitors agents

Spasmolytic
agent

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Antacids
Aluminum hydroxide Magnesium hydroxide

Calcium carbonate Sodium bicarbonate

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Antacids
• Mechanism of action: Antacids are weak
bases that react with gastric acid to form
water and a salt to diminish gastric acidity.
Because pepsin is inactive at a pH greater than
4, antacids also reduce pepsin activity.

• Indications: Heartburn, Dyspepsia.

Adverse effects
• Aluminum hydroxide tends to cause
constipation, whereas magnesium hydroxide
tends to produce diarrhea. Preparations that
combine these agents aid in normalizing
bowel function.

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Examples
Generic name Calcium carbonate Generic name sodium alginate +
+ Magnesium sodium
carbonate bicarbonate +
Mother name Rennie calcium carbonate

Brand names Antacid Awa

Mother name Gaviscon
Dosage forms chewable tablet
(550mg/110mg, Brand names Enoxan
675mg/135mg,
1000mg/200mg), Dosage forms Tablets (250mg+
oral suspension 80mg+133mg), Oral
(400mg/135mg)/5 suspension
ml, (250mg+
(550mg/110mg)/5 80mg+133mg)
ml, 5mg)\5ml)
(1000mg/200mg)/5
ml).
Doses Four times daily
Doses Four times daily

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H2 receptor blockers

Cimetidine Ranitidine

Nizatidine Famotidine

H2 receptor blockers
• Mechanism of action: H2RAs decrease
gastric acid secretion by reversibly binding to
histamine H2 receptors located on gastric
parietal cells, thereby inhibiting the binding
and action of the endogenous ligand
histamine.

• Indications: Peptic ulcers, Acute stress

ulcers, Gastroesophageal reflux disease
(GERD).

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Examples
Generic name Ranitidine Generic name Famotidine

Mother name Zantac Mother name Pepcid

Brand names Histac Brand names Famodar
Dosage forms injection solution Dosage forms injection solution
(25mg/mL), (10mg/mL,
Syrup (15mg/mL) 0.4mg/mL), oral
Tablet (75mg, suspension
150mg, 300mg) (40mg/5mL)
Capsule (150mg, Tablet (10mg,
300mg) 20mg, 40mg),
Chewable tablet
(10mg, 20mg)
Doses Twice daily. Doses Twice daily.

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Proton Pump inhibitors

Dexlansoprazole Esomeprazole

Lansoprazole Omeprazole

Rabeprazole Pantoprazole

Proton Pump inhibitors

• Mechanism of action: Proton pump
inhibitors act by irreversibly blocking the
enzyme system (the H+/K+ ATPase), or, more
commonly, the (gastric proton pump) of the
gastric parietal cells. The proton pump is the
terminal stage in gastric acid secretion.

• Indication: GERD, erosive esophagitis, active

duodenal ulcer, and pathologic hyper-
secretory conditions.

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Adverse
effects

Examples
Generic name Omeprazole Generic name Lansoprazole
Mother name Prilosec
Mother name Prevacid
Brand names Gasec
Dosage forms packet (2.5mg, Brand names Lanzotec
10mg), suspension
(2mg/ml), tablet Dosage forms capsule (15mg,
(20mg), capsule 30mg), tablet
(10mg, 20mg, (15mg, 30mg), oral
40mg), oral suspension
disintegrating tablet (3mg/ml).
(20mg).
Doses One to two times Doses One to two times
daily. daily.

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Antiemetics

Serotonin Dopamine 1st generation Neurokinin-1

Antagonists Antagonists Antihistamine Antagonists

Ondansetron Domperidone Diphenhydramine Aprepitant

Dolasetron Metoclopramide Dimenhidrinate Netupitant
Granisetron Prochlorperazine Meclizine Cosapitant
Palonosetron Chlorpromazine Rolapitant
Tropisetron Droperidol Fosaprepitant
Haloperidol

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Serotonin Antagonists
• Mechanism of action: These agents
selectively block 5-HT3 receptors in the
periphery (visceral vagal afferent fibers) and in
the brain (CTZ).

• Adverse effects: Headache, malaise, and

constipation.

• Indications: chemotherapeutic induced and

postoperative nausea and vomiting.

Examples
Generic name Ondansetron
Mother name Zofran
Brand names No-vomit
Dosage forms injectable solution
(2mg/mL), tablet
(4mg, 8mg, 24mg)
oral solution (4mg/5mL)
orally disintegrating tablets (4mg, 8mg)
Doses For chemotherapeutic induced nausea
and vomiting and postoperative nausea
and vomiting 2 tablets 1 hour before
chemotherapy and procedure 8mg IV
injection 20 min Before chemotherapy,
and 4mg IV injection immediately before
procedure.

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Dopamine antagonists
• Mechanism of action: Those drugs act by
blocking dopamine receptors in the brain
(CTZ) and in the gastrointestinal tract (vagus
nerves).

• Side effects: Extrapyramidal symptoms

(EPS), sedation, lethargy, diarrhea, and CNS
depression.

• Indications: Nausea and vomiting.

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Extrapyramidal symptoms

Examples
Generic name Domperidone Generic name Metoclopramide

Mother name Motilium Mother name Reglan

Brand names Premosan

Brand names Costi
Dosage forms injectable solution
(5mg/mL), syrup
Dosage forms 10mg Tablets,
(5mg/5mL,
1mg\ml Oral
10mg/10mL
suspension
Tablet (5mg, 10mg)
Dispersible tablets
(5mg, 10mg).
Doses Every 6 hours. Doses Every 6 hours.

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Laxatives
Bulk Stool
Stimulants Osmotic Lubricants
forming softeners

Bisacodyl Methylcellulose Magnesium citrate Docusate Glycerin

Senna Psyllium Magnesium hydroxide Mineral oil
Castor oil Ispaghula husk Polyethylene
Lactulose

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Stimulant laxatives
• Mechanism of action: They have a
selective action on the nerve plexus of intestinal
smooth leading to muscle stimulation of fluid
secretion and colonic contraction results in
enhanced bowel motility.

• Caution: Avoid chronic use may cause laxative

dependence. Ingestion should be avoided within
1 to 2 hours of antacids, H2-receptor antagonists,
proton pump inhibitors, and milk.

Bulk-Forming Laxatives
• Mechanism of action: Bulk-forming laxatives
exert their effect by swelling in the bowel forming
a gel and increasing fecal mass. In addition they
also encourage the proliferation of colonic
bacteria, and this helps further increase fecal bulk
and stool softness.

• NOTE: They are well tolerated in pregnancy and

breastfeeding. Patients should be advised to
increase their fluid intake while taking bulk-
forming medicines. Their effect is usually seen in
12 to 36 hours.

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Examples
Generic name Bisacodyl Generic name Ispaghula husk

Mother name Dulcolax Mother name Fybogel

Brand names Ispagel

Brand names Laxocodyl
Dosage forms 3.5g\Sachet.

Dosage forms 5mg, 10mg Tablets,

5mg, 10mg
Suppository

Doses Put granules in

Doses Two tablets before 150ml of water
bed time. twice daily.

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Anti-Diarrheal agents
Loperamide
Diphenoxylate + atropine
Bismuth subsalicylate

Anti-Diarrheal agents
• Mechanism of action: It prolongs intestinal
transit time, thereby reducing the amount of
fluid lost in the stool.

• Adverse effects: Dizziness, Fatigue,

Abdominal pain and Constipation.

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Examples
Generic name Loperamide Generic name Diphenoxylate +
atropine
Mother name Imodium
Mother name Lomitil

Brand names Vacontil

Brand names enterostop

Dosage forms Oral suspension Dosage forms (2.5mg+0.025mg)\5

(1mg/7.5mL) ml Oral solution
Tablet (2mg), 2.5mg +
Capsule (2mg) 0.025mg Tablets
tablet chewable
(2mg).
Doses Two tablets initially,
then one tablet
after each
subsequent loose Doses 2 tablets every 6
stool up to 8 tablets hours
in 24 hours.

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Spasmolytic agents
Mebeverinic acid
Drotaverine
Hyoscine butylbromide
Papaverine
Otilonium bromide
Dicyclomine
hyoscyamine
Propantheline
Methscopolamine

Spasmolytic agents
• Mechanism of action: Antispasmodic agents
relaxe the smooth muscle of the
gastrointestinal, biliary and urinary tracts. It is
believed to act predominantly at the
parasympathetic ganglia in the walls of the
viscera of these organs.

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Adverse effects
Phototoxicity

Examples
Generic name Mebeverinic acid Generic name Hyoscine
butylbromide

Mother name Duspatalin Mother name Buscopan

Brand names Scopinal

Brand names Colospasmin, Meva
Dosage forms Tablets (10mg,
Dosage forms Tablets (100mg, 20mg), Oral
135mg), Extended solution (0.1%),
release capsules Injection solution
(200mg) (20mg\ml).

Doses Two to three times Doses Three times daily.

daily.

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