Ameer

Hamza

ShaheedSubmitted To:

Sir Irfan Hamid

Drug name :Cimetidin

Pharmacological class:

Histamine H2 Antagonists

Enzyme Inhibitors

Therapeutic class:

Anti-Ulcer Agents

Cimetidine

Chemical name:

Chemical structure:

Colour: White or off white crystalline powder.

Odour: Unpleasant odour.

Mechanism of action

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.

Bioavailability:PO: 60-70% (undergoes minimal

1st pass metabolism)

Protein Bound: 15-20%

Half life: 2 hours

Absorption : Oral/I.V 60 %

Excretion:

Urine: 48-75%

Feces: 2-3%

Enzymes inhibited:

CYP1A2

CYP2D6

CYP3A4

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))

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)

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)

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)

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 )

• 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

This information taken from book

Pharmaguid page # 38

Drug Interactions

Cimetidine

Theophylline

CYP1A2

Codeine

CYP2D6

Phenytoin

CYP2C9

WarfarineCYP3A4

CYP1A2

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

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

Brand

names for

Cimetidine

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

Any

Question ?