Chemicals / Complex Chemical Agents/ Chemical:
Meloxicam (with special reference to Ruminants, Bears and Lagomorphs)

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 
A COX-2 receptor preferential NSAID. (B263)

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Names and Formulae
Type
  • COX-2 receptor preferential NSAID in the oxicam class, with anti-inflammatory, analgesic and antipyretic activity. (B263)
Alternative Names Metacam (Boehringer Ingelheim). (B350)
Chemical Formula C14H13N3O4S2 (W324)
Chemical Structure --
Molecular Weight 351.3944 (W324)
Related Chemicals Piroxicam. (B263)

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Physical Properties / Chemistry
Appearance

Pale yellow powder. (B263) The commercial oral formulation is a viscous yellowish suspension with the odour of honey. (J289.27S1.w1)

Melting point --
Boiling point --
Density --
Water solubility
  • Practically insoluble. (J289.27S1.w1)
Other solubility
  • Insoluble in strong acids and bases. Slightly soluble in methanol. (J289.27S1.w1)
Acid/Base

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Pharmacology & General Information
Pharmacology
  • Anti-inflammatory, analgesic and antipyretic properties probably through the inhibition of cyclooxygenase, phospholipidase A2 and inhibition of prostaglandin synthesis. (B263)
  • Meloxicam is considered to be COX-2 preferential (not COX-2 specific) as at higher dosages its COX-2 specificity is diminished. (B263)
Storage / Stability Store at room temperature. (B263)
Legal Category (In UK) POM (B266)

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References

Associated Techniques

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ORGANISATIONS

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

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Authors Debra Bourne (V.w5); Penny Cusdin (V.w60)
Referees Suzanne I. Boardman (V.w6)

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Therapeutic Information

Uses/Indications
Activity --
Appropriate Use
  • Inflammation and pain. (B201.10.w10)
  • An anti-inflammatory, analgesic and antipyretic agent. (B263)
  • Principally used for the symptomatic treatment of osteoarthritis in dogs. (B263)
  • Also has anti-exudative effects and reduces leucocyte infiltration into the inflamed tissue. (B350)
Limitations --
Notes --

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Pharmacokinetics and Drug Interactions
Absorption /Bioavailability
  • Well absorbed in dogs after oral administration. Peak blood levels occur about 7-8 hours after administration. (B263)
  • In rabbits: After a single oral dose of 0.3 or 1.5 mg/kg, maximal plasma concentrations of 0.14 μg/mL and 0.3 μg/mL, respectively occurred at six to eight hours. (J495.56.w1)
Distribution
  • In dogs, the volume of distribution is 0.3 l/kg. (B263)
Plasma Protein binding / Storage
  • In the dog, about 97% is bound to plasma proteins. (B263)
  • In cattle and pigs, more than 98% of meloxicam is bound to plasma proteins. (B350)
  • The highest concentrations are found in the kidney and liver, with relatively low levels in skeletal muscle and fat. (B350)
Elimination Route
  • "In all species studied, meloxicam undergoes extensive hepatic metabolism into 4 inactive metabolites that are excreted in both urine and feces." (J495.56.w1)
  • Extensively biotransformed to several different metabolites in the liver, none of which appear to have pharmacologic activity. (B263)
  • The majority of the metabolites, and the unchanged drug, are eliminated in the faeces. (B263)
  • A significant amount of enterohepatic recirculation occurs. (B263)
  • In cattle and pigs, approximately half the administered dose is eliminated in the urine and the remainder in the faeces. (B350)
  • In dogs, approximately 75% of the administered product is eliminated in the faeces; the remainder in the urine. (B350)
Elimination half-life / Clearance Rate Elimination half-lives are species specific:
  • Dogs: 12 to 36 hours (average 24 hours) (B263)
  • Pigs: 4 hours (B263) / 2.5 hours (B350)
  • Horses: 3 hours (B263)
  • Cattle: 13 hours (B263)
    • After SC administration in young cattle: 26 hours (B350)
    • After SC administration in lactating cows: 17.5 hours. (B350)
  • In rabbits: 
    • After a single oral dose of 0.3 or 1.5 mg/kg, concentrations of drug in plasma decreased rapidly to near-undetectable levels by 24 hours after administration; the elimination half-life was about eight hours. (J495.56.w1)
    • After five days of administration at 0.3 or 1.5 mg/kg daily, no accumulation was noted at either dose rate and elimination was rapid once dosing stopped. (J495.56.w1)
Drug Interactions
  • Can displace, or be displaced by, other highly protein bound drugs such as warfarin and phenylbutazone. (B263)
  • May antagonise the antihypertensive effects of ACE inhibitors. (B263)
  • May cause increased likelihood of bleeding or gastric ulceration if used in conjunction with drugs that affect haemostasis, such as heparin or warfarin, or drugs that may cause gastrointestinal erosion, such as aspirin, flunixin, phenylbutazone, and corticosteroids. (B263)

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Administration
Formulations available UK
  • Metacam Oral Suspension (Boehringer Ingelheim): Oral suspension, Meloxicam 1.5 mg/mL, 32 mL, 100 mL. For dogs. (B201.10.w10)
  • Metacam 0.5% Injection (Boehringer Ingelheim): Injection, Meloxicam 5 mg/mL, 10mL. For dogs. (B201.10.w10)
  • Metacam 5 mg/mL Solution for Injection for Cattle and Pigs (Boehringer Ingelheim): Injection, Meloxicam 5 mg/mL, 100mL. For cattle and pigs. (B350)
Doses / Administration Routes / Frequencies Cattle

Dogs

  • By mouth: 200 g/kg as a single dose for 1 day, then 100 g/kg once daily. Should be given soon after feeding. (B201.10.w10)
  • By subcutaneous injection: 200 g/kg as a single dose. (B201.10.w10)

Bears

  • Has been given subcutaneously at 0.5 mg/kg once then orally at 0.1 mg/kg once daily (mixed with honey) for two weeks. (Used for alleviation of severe joint pain prior to treatment by femoral head and neck excision). (J2.32.w3)

Lagomorphs - Oryctolagus cuniculus domesticus - Domestic rabbit:

  • 100 - 300 micrograms orally once daily. (B373.Guide.w41)
  • 200 - 300 micrograms subcutaneously once daily. (B373.Guide.w41)
  • 0.2 - 0.6 mg/kg orally or subcutaneously. Duration of analgesic action possibly 24 hours. (B601.16.w16)
  • The oral suspension is generally palatable to rabbits. (B601.16.w16)
  • Note: based on a study in New Zealand White rabbits, "Rabbits may require a dose exceeding 0.3 mg/kg given once daily to achieve optimal plasma levels of meloxicam over a 24-h interval." (J495.56.w1)
  • 0.3 - 0.6 mg/kg subcutaneously or orally every 24 hours. "studies have shown that rabbits may require a dose exceeding 0.3 mg/kg every 24 hours to achieve optimal plasma levels of meloxicam over a 24-hour interval and doses of 1.5 mg/kg subcutaneously or orally are well tolerated for 5 days." (B546)
Monitoring parameters

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Withdrawal period / Withholding time
Notes UK 

Cattle

  • Meat and offal - 15 days. (B350)
  • Milk - 5 days. (B350)

Pigs

  • Meat and offal - 5 days. (B350)

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Toxic Information

Toxic effects of Pharmaceutical Products
Contraindications / Precautions
  • Not recommended for use in pregnant or lactating animals or in animals which are less than six weeks old. (B263, B350)
  • Contraindicated for use in individuals known to be hypersensitive to this drug. (B263)
  • Contraindicated in individuals with active gastrointestinal ulceration or bleeding. (B263)
  • Contraindicated in individuals with impaired renal, hepatic or cardiac function. (B263)
  • Contraindicated in individuals with haemorrhagic disorders. (B263)
  • Contraindicated for use in pregnant or lactating bitches. (B201.10.w10)
  • Use with extreme caution in individuals which are dehydrated, hypovolaemic or hypotensive as these conditions may potentially increase the risk of development of renal toxicity. (B263)
Adverse Effects / Side Effects / Warnings
  • Occasional gastrointestinal distress in dogs, usually transient. (B263)
  • Low renal toxicity. (B263)
  • Prolonged use may cause gastro-intestinal lesions, inappetance, vomiting and diarrhoea. (B201.10.w10)
  • Serious side effects, including fatalities, have been recorded very rarely. (B263)
Operator Warnings --
Overdose / Acute Toxicity
  • No specific information. (B263)

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Detailed Toxicological Information
Classification --
Acute Toxicity --
Chronic Toxicity --
Reproductive effects
  • Contraindicated for use in pregnant or lactating bitches. (B201.10.w10)
Teratogenic effects --
Mutagenic effects --
Carcinogenic effects

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

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Nutrient Information

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

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External / Environmental Information

External / Environmental Uses
Use --
Formulation --
Application method --
Application Concentration --
Persistence of Effect / Frequency of Application --

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Sources in the Environment
Natural sources --
Human-associated sources --

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Effects on the Environment
Effects in the aquatic environment

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Effects on land --

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Persistence in the Environment
Breakdown in soil and groundwater

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Breakdown in water --
Breakdown in vegetation --

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