Documente Academic
Documente Profesional
Documente Cultură
, SpFK
Faculty of Medicine
UPH
Case
A 22 yo medical student, noted a burning pain in his
upper abdomen since 2 weeks ago. This sensation
occurs 1 to 2 hrs after eating. He is actually in a good
health before, although he smokes approximately 2
packs of cigs & drink 5 cups of coffee a day. He is
currently under stress because of his bachelor exam.
He also been taking 1-2 tabs aspirin daily for the past
2 months because of headache.
The pain frequently awakens him at midnight. His
pain usually relieved by eating and by taking antacid.
What is the most likely problem?
What is the most appropriate treatment?
Anatomy
Meaning of numbers
1. Body of stomach
2. Fundus
3. Anterior wall
4. Greater curvature
5. Lesser curvature
6. Cardia
9. Pyloric sphincter
10. Pyloric antrum
11. Pyloric canal
12. Angular notch
13. Gastric Canal
14. Rugal folds
PGE2
Histamine
ACh
M3
Ranitidine
Gastrin
_
Proglumide
_
Misoprostol
PGE
receptor
Adenyl
cyclase
ATP
Ca++
+
H2
cAMP
Gastrin
receptor
Ca++
+
Protein Kinase
(Activated)
+
+
K
K + H
_
Omeprazole
Proton pump
Gastric acid
Parietal cell
Lumen of stomach
Antacid
Antacids
Weak bases that react with gastric hydrochloric acid
Antacids cont
Antacids cont
Present
day antacids :
Aluminium Hydroxide
Magnesium Hydroxide
React slowly with HCl magnesium chloride
or aluminum chloride and water.
No gas is generated, belching does not occur.
Metabolic alkalosis is also uncommon
because of the efficiency of the
neutralization reaction.
Antacids cont
Duration of action :
30 min when taken in empty stomach
2 hrs when taken after a meal
Side effects :
Al3+ antacids constipation (As they relax gastric smooth
brown algae.
on
(Strocain)
Antacid - Interactions
Adsorb drugs (binding the drug) and form insoluble
(ex.tetracycline, quinolone)
Clinical importance :
Interactions can be avoided by taking antacids
2 hrs before or after ingestion of other drugs .
Histamine H2 Receptor
Antagonist
Reversible competitive inhibitors of H2 receptor
Highly selective, No action on H1 or H3 receptors
Very effective in inhibiting nocturnal acid
Cimetidine
Bioavailability
80
Relative Potency 1
Half life (hrs) 1.5 - 2.3
Duration of
Ranitidine
50
5 -10
1.6 - 2.4
1
400
Famotidine
40
32
2.5 - 4
Nizatidine
>90
5 -10
1.1 -1.6
12
0.1
150
20
150
action (hrs)
Inhibition of
CYP 450
Dose mg(bd)
& increases
conc. of Warfarin, Theophylline, Phenytoin,
Ethanol.
CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4)
new molecules
Esomeprazole
20 - 40 mg o.d.
Lansoprazole
30 mg o.d.
Pantoprazole
40 mg o.d.
Rabeprazole
20 mg o.d.
before meals
Other acid suppressing agents not coadministered
interactions
Answer :
Antacids
Explanation :
Antacids neutralise the already secreted
acid in the stomach. All other drugs act by
stopping acid secretion and so may not relieve
symptoms at least for 45 min.
Sucralfate
Salt of sucrose complexed to sulfated aluminium
hydroxide
In acidic pH polymerizes to viscous gel that
Misoprostol
PGE analogue
Modest acid inhibition Stimulate mucus &
bicarbonate secretion
Enhance mucusal blood flow
Approved for prevention of NSAID induced ulcer
Side effect : Diarrhoea & cramping abd. pain 20 %
Not so popular as P.P.I are more effective & better
tolerated
secretion
Direct antimicrobial activity against H.pylori
May cause blackening of stools & tongue
Not used for long periods bismuth toxicity
Available compounds :
Bismuth subsalicylate in USA (IndScantoma )
Bismuth subcitrate in Europe
Bismuth dinitrate
Answer :
Antacids or Sucralfate
Explanation ;
H2 antagonists cross placenta and are also
secreted in breast milk. Safety of Proton pump
inhibitors not established in pregnancy.
Misoprostol causes abortion .
Eradication of
H.pylori
Triple Therapy
The BEST among all the Triple therapy regimen is
Omeprazole / Lansoprazole
- 20 / 30 mg bd
Clarithromycin
- 500 mg bd
Amoxycillin / Metronidazole
- 1gm / 500 mg bd
Metronidazole
- 250 mg qid
Tetracycline
- 500 mg qid
Tetracycline
- 400 mg bd
- 500 mg bd
Quadruple Therapy
Given when Triple Therapy fails
Omeprazole / Lansoprazole - 20 / 30 mg bd
Bismuth subsalycilate
- 2 tabs qid
Metronidazole
- 250 mg qid
Tetracycline
- 500 mg qid
= Cushings ulcer
Stress induced ulceration after severe burns
= Curlings ulcer
Antiemetics
Pathophysiology of Emesis
Cancer chemotherapy
Opioids
Chemoreceptor
Trigger Zone
(CTZ)
Dopamine D2,
5 HT3,Opioid
Receptors
Cerebral cortex
Smell
Sight
Thought
Anticipatory emesis
Vomiting Centre
(medulla)
Muscarinic, 5 HT3 &
Histaminic H1
Motion
sickness
Vestibular
nuclei
Muscarinic
Histaminic H1
in hepatic insufficiency
Given once or twice daily orally or intravenously.
Drugs Available
Ondansetron
32 mg / day
Granisetron
10 g / kg / day
Dolasetron
1.8 mg / kg / day
Indications
Chemotherapy induced nausea & vomiting given
Adverse Effects
Excellent safety profile
Headache & constipation
All three drugs cause prolongation of QT interval,
Dopamine D2 Antagonist
Antagonise D2 receptors in CTZ.
Drugs available
Metoclopramide
10 mg tid
Domperidone
10 mg tid
cannot.
effects.
But as metoclopramide crosses BBB it has
Prochlorperazine
Promethazine
Phenothiazines are antipsychotics with potent
Droperidol
Droperidol used for post-op. nausea & vomiting,
H1 Antihistaminics
Most effective drugs for motion sickness
Drugs available
Betahistine
Meclizine
Cyclizine
Dimenhydrinate
Diphenydramine
Promethazine Used in pregnancy,
used by NASA for space motion sickness
Anticholinergics
Scopolamine (hyoscine) used as oral or
Cannabinoids
Dronabinol used as adjuvant in chemotherapy
Explanation :
Principle Management :
lifestyle modifications
weight loss and elevating the head of the bed
avoiding eating two hours before bed
Certain foods & lifestyle are considered to promote reflux: