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19. Drugs used in

GIT Disorders
Acid peptic disease.
Drugs used in acid peptic disease are Hy papa

hy • H2 inhibitors

P • Proton pumb inhibitors

A • Ant acids

P • Protectivegents

A • Antibiotics

H2 inhibitors
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Mechanism
Blockage action of histamine on parietal cells
Uses

Proton pump inhibitors

OLPER + parazole
O  Ome + prazole  Omeprazole
L  Lenzo + prazole  Lenzoprazole
P  Pento + prazole  Pentoprazole
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E  esmo + prazole  Esmoprazole
R  Rabe + prazole  Rabeprazole
Mechanism
Lipophilic weak bases that diffuses into parietal cell canaliculi.
 Irreversibly inhibit the parietal cells H/K ATPase the transporter
that is primarily responsible producing stomach acid.
Uses

In GERD and peptic ulcer these agents are more potent than H2 receptor
antagonists
Pharmacokinetics
 Oral formulations are enteric coated to prevent destruction in
stomach
 Half-life of 1-2 hours and effects last for 1 day and 3-4 days are re-
quired to achieve full effectiveness
Adverse effects
TIDA proton
T  Vit B twelve (B12) deficiency  because of decrease absorp-
tion (need acidity for absorption)
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I  inc risk of respiratory and enteric tract infections
D  Diarrhoea and sar dard (headache)
A  Abdominal pain
Antacids
Al(OH)3 and Mg(OH)2
 These are weak bases that react with protons in GIT
 Also stimulate protective function of gastric mucosa
Mg(OH)2  this is also found in syrup milk of magnesia that is a laxative
So this causes strong laxative effect
Al(OH)3 show constipating effect opposite to Mg(OH)2
CaCO3 and NaHCO3 can also be used they are also weak bases
Uses
GPS dr with burning hurt
G  GERD
P  Peptic ulcer
S  Stress related gastroenteritis (less used)
Dr  Dyspepsia
Burning hurt  heart burn
Adverse effects
 Excess Calcium absorption from milk and Calcium rich foods  re-
sult in milk alkali syndrome
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 Regular intake may lead to alkalosis
 Chemical reaction between antacid
and acid  production of CO2
distended abdomen
 May cause headache
 Al(OH)3  constipation
 Mg(OH)2  laxative
 Al(OH)3  neurotoxic and contrain-
dicated in pregnancy
 Mg(OH)2  in renal failure patients
body Mg level increase Mg  hypermagnecemia
Protective agents
Protective MSc
Protective  protective agents
M  misoprostol
S  sucralfate
C  colloidal bismuth
Misoprostol
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 Inc. mucosal protection
 Dec. acid secretion
Uses
 Effective in Ulcers by NSAIDS
Not used widely because of multiple doses and poorly tolerated adverse
effects
Side effects diarrhoea + GIT upset
 Should not be taken by pregnant women  increase uterine con-
tractions may cause abortion
 With mifepristone used vaginally  to terminate pregnancy
Sucralfate
 Aluminium sucrose sulphate
o Poorly soluble molecule that polymerise in acidic environ-
ment of stomach and bind to injured tissue
 form protective covering over ulcer beds
 accelerate healing of the ulcer
 Reduce reoccurrence rate
o Systemic effects are very less  too insoluble
 Toxicity very low
Colloidal bismuth
 Formation of protective covering on the ulcerative tissue
 Stimulation of mucosal protection mechanism
Antibiotics
Chronic infection with H-Pylori (present in most of the patients with reoc-
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currence, Non NSAID induced peptic ulcer.

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Dosage regime
Proton pump inhibitor + Clarithromycin + amoxicillin
 Metronidazole is given for penicillin allergic persons.

Motility Promoters
Mnemonic for this is MMDC (Multan medical and dental college)

M • motility promoters

M • Metocloperamide

D • Domperidone

C • Cholinomimetics (Neostigmine)

Metoclopramide and Domperidone

Dopamine D2 antagonist that increase the GIT motility
 Prevent emesis after surgical anaesthesia
 Chronic use of metoclopramide causes symptoms of parkinsonism
and other extrapyramidal side effects
Cholinomimetics
Neostigmine  is used for GERD and Gastropresis.

Drugs used in irritable bowel syndrome

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Sir Alu said to aunty chalo chalain lubi k pas irritation ho rhi hay.
Sir  serotonin antagonist  alosteron
Aunty  anticholinergics
Chalo chalain  chloride channel activator  Lubiproston
Serotonin antagonists
Alosteron
 Potent 5HT3 antagonist

Used in treatment of women with severe IBM and diarrhoea

Side effect  constipation and colitis
Anticholinergics
Hayoscyamine  also known as dhaturine (an antispasmodic drug)
Antispasmodic  drug or herb that depress muscle spasm and re-
lieve abdominal pain
Hayoscyamine  is an anti-muscarinic drug
Uses
 Peptic ulcer
 Irritable bowel syndrome
 Pancreatitis and colitis
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Side effects same as of atropine but weaker
Chloride channel activators
Lubiproston  Chloride channel activator type 2
 Treatment of women with IBS and constipation

Drugs for inflammatory bowel disease

Central intelligence agency of America

central • Corticosteron

intelligence • immunosuppresants

agency • 5-aminosalisalic drugs

america • anti TNF drugs

Corticosteroids
Glucocorticoids are used
 Inhibit prostaglandin synthesis
 Inhibit leukotriene synthesis
Immunosuppressants
Methotrexate’ azathioprine are used
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Depress immune system
5-aminosalisalate inhibitor drugs
Used for topical therapy of inflammatory bowel disease
Mechanism
 inhibit synthesis of prostaglandins
 inhibit synthesis of inflammatory mediators
 interfere with the production of inflammatory cytokines
Generic name for 5ASA is Mesalamine
Adverse effects  GIT upset, headache, nausea, bone marrow suppres-
sion and hypersensitivity reactions
Anti TNF drugs
 Natalizumab
Block integrins on circulatory leukocytes
 Used in severe Crohn’s disease

Antiemetic drugs
H2Canada
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H • 5HT3 blocers

H • H1 blockers

C • corticosteroids

A • anti-muscarinics

N • Nurokinin receptor antagonists

A • aaaaaaaaa

D • D2 blockers

A • aaaa

5 HT3 antagonists
Go to 5HT3 antagonists in chapter of histamine and serotonin
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H1 blockers
Go to chapter of histamine and serotonin for more details
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Corticosteroids
Dexamethasone is used  anti-inflammatory and immunosuppressant
For further readings read in Corticosteroids chapter
Anti-muscarinics  scopolamine

Neurokinin receptor antagonists  apirepitant

 Chemotherapy induced nausea vomiting used
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D2 blockers  prochlorperazine

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Antiemetic treatment of nausea and vomit

Antidiarrheal drugs
 Loperamide
 Colloidal bismuth compounds
 Pectin and Kaolin absorbent compounds
Loperamide
Activate opioid mu receptors  decrease tone of longitudinal mus-
cles.
Colloidal bismuth compounds
Subsalicylate and citrate salts  effective in travellers’ diarrhoea
Pectin and Kaolin  absorbent compounds

Laxatives

Mg(OH)2 and other nonabsorbant s

Bulk forming compds  methyl cellulose and psyllium

Stool surfactants  mineral oils

Stimulants  cenna

chloride channel activators lubiprostone

Opiod receptor inhibitors

Contents

Pharmacology Mnemonics and Short Notes By Muhammad Ramzan Ul Rehman