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Transcript of cimetidine
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Ameer
Hamza
ShaheedSubmitted To:
Sir Irfan Hamid
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Drug name :Cimetidin
Pharmacological class:
Histamine H2 Antagonists
Enzyme Inhibitors
Therapeutic class:
Anti-Ulcer Agents
Cimetidine
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Chemical name:
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Chemical structure:
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Colour: White or off white crystalline powder.
Odour: Unpleasant odour.
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Mechanism of action
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Cimetidine binds to an H2-receptor located on the
basolateral membrane of the gastric parietal cell, blocking
histamine effects. This competitive inhibition results in
reduced gastric acid secretion and a reduction in gastric
volume and acidity.
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Bioavailability:PO: 60-70% (undergoes minimal
1st pass metabolism)
Protein Bound: 15-20%
Half life: 2 hours
Absorption : Oral/I.V 60 %
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Excretion:
Urine: 48-75%
Feces: 2-3%
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Enzymes inhibited:
CYP1A2
CYP2D6
CYP3A4
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Peptic Ulcer:
Peptic ulcers are sores in the lining of the stomach or
duodenum.
Causes :
H.pylori bacteria .
Regular use of pain relievers. NSAID,s
(aspirin, ibuprofen , naproxen , ketoprofen)
(This information taken from book Medical pharmacology by Padmaja
Udaykumar)(page #317))
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Gastroesophageal reflux disease
Reflux Oesophagitis :
Acid from the stomach leaks up into the gullet
(oesophagus)
This information taken from
(http://www.patient.co.uk/health/Acid-
Reflux-and-Oesophagitis.htm)
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Zollinger-Ellison syndrome:
The exact cause of Zollinger-Ellison syndrome remains unknown.
Zollinger-Ellison syndrome are made up of cells (gastrinomas) that secrete large amounts of gastrin, which in turn causes the stomach to produce far too much acid.
(http://www.mayoclinic.com/health/zollinger-ellison-syndrome/DS00461/DSECTION=causes)
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Acid related dyspepsia:
Dyspepsia is sometimes called indigestion.
Discomfort that causes persistent pain or fullness in
the upper abdomen, soon after the meal starts.
(http://www.medindia.net/patients/patientinfo/indigestion.htm)
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Stress ulcer:
Stress can contribute to the development of many
diseases .This includes stomach, or peptic, ulcers.
(http://www.livestrong.com/article/174015-a-stomach-ulcer-from-stress/#ixzz2F8KFZBmc )
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• 200 mg q.i.d
• With meal at bed time
• 200 mg t.d.s
• With meal at bed time
• 400 mg q.i.d upto 12 weeks
• 800 mg/D
• At bed time
Peptic Ulcer
Reflux oesophagitis
Acid related dyspep
sia
Zollinger-Ellison
syndrome
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This information taken from book
Pharmaguid page # 38
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Drug Interactions
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Cimetidine
Theophylline
CYP1A2
Codeine
CYP2D6
Phenytoin
CYP2C9
WarfarineCYP3A4
CYP1A2
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These information taken from,
Pharmaguide page #39.
http://www.merckmanuals.com/professional/clinical_pharmacology/pharmacokinetics/drug_metabolism.html
http://www.aafp.org/afp/2007/0801/p391.html
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Common side
effects:
Headache.
Constipation.
Confusion.
Somnolence.
Rare but
dangerous side
effect:Decrease libido
Decrease sperm count
Impotence
Gynecomastia
(These side effects associated with
high dose of cimetidine)
Lynn wecker page # 200
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Brand
names for
Cimetidine
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B.N: Cimet
M.N: Ferozsons
Tab.: 400 mg
B.N: Tagamet
M.N: GSK
Inj.: 200 mg
Tab.: 200 , 400 mg
B.N: Normacid
M.N: Wilson
Tab.: 400 , 800 mg
B.N: Bacimet
M.N: Davis pharma
Tab.: 200 , 400 mg
Cimetidine
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Any
Question ?
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