Chemicals / Complex Chemical Agents/ Chemical:

Cimetidine 

INFORMATION AVAILABLE

GENERAL CHEMICAL INFORMATION THERAPEUTIC INFORMATION [DOSE, FREQUENCY & ROUTE]

NUTRITIONAL INFORMATION

TOXICITY INFORMATION ENVIRONMENTAL INFORMATION
Information in this page has been entered to support the current volumes of Wildpro and further information will be added as new volumes are completed. This page is not intended to substitute for the manufacturer's data sheet and the information is not yet complete for all species, or for all contra-indications etc.

CAUTION: Before any pharmaceutical product is used, the manufacturer's data sheet, containing information on uses, dosage and administration, contra-indications, warnings etc., should always be consulted. It is important to remember that licensing of pharmaceutical products for use in a particular species/condition, as well as mandatory meat and milk withdrawal times for food-producing animals, varies between countries and changes with time. Withdrawal times also may vary between different pharmaceutical formulations and depending on route of administration. In the EU, the prescription cascade must be followed (see LCofC1.2H and W564.Apr05.w1); note that specific restrictions apply for food-producing animals. In the USA, FARAD may be consulted regarding residues and meat and milk withdrawal times.

General Chemical Information

Summary 

Histamine-2 receptor antagonist, used to decrease release of gastric acid in the stomach.

Return to Top of Page

Names and Formulae

Type Histamine-2 (H2) receptor antagonist. (B263, B373.3.w3) 
Alternative Names Cimetidine HCl (B263)
Chemical Formula --
Chemical Structure --
Molecular Weight --
Related Chemicals --

Return to Top of Page

Physical Properties / Chemistry

Appearance
  • Cimetidine: Crystalline powder, white to off-white, with an unpleasant odour. (B263)

  • Cimetidine HCl: crystalline powder, white. (B263)

Melting point --
Boiling point --
Density --
Water solubility
  • Cimetidine: sparingly soluble. (B263)
  • Cimetidine HCl: very soluble. (B263)
Other solubility
  • Cimetidine: 
    • Alcohol: soluble. (B263)
  • Cimetidine HCl:
    • Alcohol: soluble. (B263)
Acid/Base Cimetidine: 

Cimetidine HCl:

Return to Top of Page

Pharmacology & General Information

Pharmacology  
Storage / Stability
  • Store at room temperature, protect from light. (B263)
  • Injectable formulations should not be refrigerated due to the risk of precipitation. (B263)
  • Store oral formulations in tight containers. (B263)
Legal Category (In UK) --

Return to Top of Page

References

Associated Techniques

--

ORGANISATIONS

--

ELECTRONIC LIBRARY
(Further Reading)
Click image for full contents list of ELECTRONIC LIBRARY

--
Authors Debra Bourne MA VetMB PhD MRCVS (V.w5)
Referees Nikki Fox BVSc MRCVS (V.w103)

Return to Top of Page

Therapeutic Information

Uses/Indications

Activity
  • Cimetidine competitively inhibits histamine at the H2 receptors of the parietal cells in the stomach, reducing gastric acid secretion (both basal levels and in response to stimulation by food, histamine, insulin or pentagastrin). Because it reduces gastric juice production, it also decreases pepsin secretion. It does not alter gastric emptying time, pancreatic secretion, biliary secretion or pressure in the lower oesophagus. (B263, B373.3.w3)
  • Cimetidine appears to have an immunomodulating effect, reversing immune suppression due to suppressor T cells. (B263)
  • Cimetadine has weak anti-androgenic activity. (B263)
Appropriate Use
  • Treatment or prevention of gastric, abomasal or duodenal ulceration, reflux oesophagitis, uraemic gastritis, stress-related or drug-induced erosive gastritis (stress-releated or drug-induced) and duodenal gastric reflux. (B263, B373.3.w3) "It has also been employed to treat hypersecretory conditions associated with gastrinomas and systemic mastocytosis." (B263)
  • In the treatment of exocrine pancreatic insufficiency, cimetidine can be used as an adjunct, reducing acid peptic breakdown of pancreatic enzyme supplements. (B373.3.w3)
  • In dogs, cimatidine has been used investigationally as a immunomodulating agent. (B263)
Limitations --
Notes --

Return to Top of Page

Pharmacokinetics and Drug Interactions

Absorption /Bioavailability Dogs: Oral bioavailability reported as about 95%. (B263)

Humans: Following oral administration, rapidly and well absorbed but with a small first-pass effect (metabolism in the liver); oral bioavailability 70-80%. (B263)

  • If given with food, absorbtion may be delayed, and the amount absorbed slightly decreased.
    cimetidine from the body. (B263)
Distribution Dogs: 
  • Volume of distribution 1.2 L/kg. (B263)

Humans:

  • Well distributed, only 15-20% plasma protein-bound. (B263)
  • Cimetidine both enters milk and crosses the placenta. (B263)
Plasma Protein binding / Storage --
Elimination Route
  • Both renal and hepatic. (B263)
    • For parenterally-delivered cimetidine, 75% is eliminated by the kidneys; following oral administration, 48% is eliminated via the kidneys. (B263)
Elimination half-life / Clearance Rate Dogs: Serum half-life 1.3 hours. (B263)

Humans: serum half-life average 2 hrs, longer in elderly individuals and those with hepatic or renal disease. 

Drug Interactions
  • May inhibit the hepatic microsomal enzyme system; metabolism of other drugs may therefore be reduced, resulting in prolonged serum half-life and increased serum concentrations. Additionally, hepatic blood flow may be reduced, reducing the first-pass effect on some drugs. (B263)
    • Drugs whose metabolism may be affected by cimetidine include: "beta-blockers (e.g., propranolol), lidocaine, calcium channel blockers (e.g., verapamil), diazepam (and other benzodiazepines), ethanol, metronidazole, phenytoin, quinidine, theophylline, and warfarin." (B263)
    • It may be necessary to adjust dosages and/or increase therapeutic monitoring of the effects of affected drugs. (B263)
  • May decrease renal clearance of procainamide. (B263)
  • "May exacerbate leukopenias when used with other agents that can cause this problem." (B263)
  • If any antacids, metoclopramide, sucralfate, digoxin or ketoconazole are also being used in the same individual, then avoid giving at the same time - preferably administer at least two hours apart. (B263)

Physical interactions

Cimetidine Injectable product is reported physically compatible with: "acetazolamide sodium, amikacin sulfate,
atropine sulfate, carbenicillin disodium, cefoxitin sodium, chlorothiazide sodium, clindamycin phosphate, colistimethate sodium, dexamethasone sodium phosphate, digoxin, epinephrine, erythromycin lactobionate, furosemide, gentamicin sulfate, heparin sodium, insulin (regular), isoproterenol HCl, lidocaine HCl, lincomycin HCl, methylprednisolone sodium succinate, nafcillin sodium, norepinephrine bitartrate, penicillin G potassium/sodium, phytonadione, polymyxin B sulfate, potassium chloride, protamine sulfate, quinidine gluconate, sodium nitroprusside, tetracycline HCl, vancomycin HCl, verapamil HCl, and vitamin B complex (w/ or w/o C)
" also with commonly used solutions for intravenous infusions (including amino acid (total parenteral nutrition) solutions), if used within 48 hours of dilution. (B263)

Reported physically incompatible with (or conflicting data on comptability): "amphotericin B, ampicillin sodium, cefamandole naftate, cefazolin sodium, cephalothin sodium, and pentobarbital sodium." (B263)

Note: Physical compatibility is affected by factors such as concentration, pH, temperature and diluents; specialized references should be consulted for more specific information. (B263)

Return to Top of Page

Administration

Formulations available --
Doses / Administration Routes / Frequencies
  • Dogs: Orally, intramuscularly or intravenously, 5 - 10 mg/kg, three times daily. (B373.3.w3)
  • Cats:  Orally, intramuscularly or intravenously, 2.5 - 5.0 mg/kg, three times daily. (B373.3.w3)
  • Horses: Foals, for gastric ulceration, orally 20 mg/kg one to three times daily, or intravenously 8 - 10 mg/kg, four to six times daily. (B373.3.w3)

Lagomorphs - Oryctolagus cuniculus domesticus - Domestic rabbit:

  • 5.0 - 10.0 mg/kg orally every 6 -12 hours. (B601.15.w15)
  • 5.0 - 10.0 mg/kg orally, subcutaneously, intramuscularly or intravenously every 8 - 12 hours. (B602.41.w41)

Ferrets - Mustela putorius furo - Ferret:

  • 10 mg/kg orally, subcutaneously, intramuscularly or intravenously every eight hours. (B602.41.w41)
  • (B626.App.w22)
  • 5.0 - 10.0 mg/kg orally, subcutaneously, intramuscularly or by slow intravenous injection every eight hours. (B631.21.w21)
  • 5 - 10 mg/kg orally, subcutaneously, intramuscularly or intravenously three times daily. In the treatment of stress-induced gastric ulcers. (J213.3.w1)

Great Apes

Monitoring parameters --

Return to Top of Page

Withdrawal period / Withholding time

Notes --

Return to Top of Page

Toxic Information

Toxic effects of Pharmaceutical Products

Contraindications / Precautions
  • Contraindicated in patients with known hypersensitivity to cimetidine. (B263)
  • Use with caution in geriatric individuals and individuals with significantly decreased renal or hepatic function. (B263)
    • Consider reducing the dose in such individuals. (B263)
  • Use with caution in individuals receiving concurrent drug therapy, because cimetadine blocks microsomal metabolism of drugs in the liver. (B373.3.w3)
Adverse Effects / Side Effects / Warnings
  • Rarely seen in animals at normal dosages. (B263)
  • Potentially (based on human data), mental confusion, headache (when the drug is discontinued), gynecomastia and decreased libido may occur. Very rarely, agranulocytosis. Rapid intravenous injection may result in transient cardiac arrhythmias. (B263)
  • If given intramuscularly, there may be pain at the injection site. (B263)
  • May inhibit the hepatic microsomal enzyme system, thereby affecting the metabolism of some other drugs (see above - Drug Interactions). (B263)
Operator Warnings --
Overdose / Acute Toxicity --

Return to Top of Page

Detailed Toxicological Information

Classification --
Acute Toxicity --
Chronic Toxicity --
Reproductive effects --
Teratogenic effects --
Mutagenic effects --
Carcinogenic effects

--

Organ toxicity --
Bird Toxicity --
Aquatic organism activity --
Other organism toxicity --

Return to Top of Page

Nutrient Information

Nutritional Data

Sources --
Biological Use --
Recommended Daily Allowance / Recommended level in food --
Stability in food (Storage time) --
Interactions --

Return to Top of Page

External / Environmental Information

External / Environmental Uses

Use --
Formulation --
Application method --
Application Concentration --
Persistence of Effect / Frequency of Application --

Return to Top of Page

Sources in the Environment

Natural sources --
Human-associated sources

--

Return to Top of Page

Effects on the Environment

Effects in the aquatic environment

--

Effects on land --

Return to Top of Page

Persistence in the Environment

Breakdown in soil and groundwater

--

Breakdown in water --
Breakdown in vegetation --

Return to Top of Page