Buprenol (Canada)

Company: Champion Alstoe

Buprenorphine Injection, Manufacturer

Buprenorphine (as buprenorphine hydrochloride) 0.3mg/mL

Veterinary Use Only

Sterile Injection

For use in cats

Description

Buprenol contains buprenorphine, which is a potent long-acting analgesic acting at opioid receptor sites in the central nervous system. Each mL contains 0.3 mg buprenorphine (as buprenorphine hydrochloride). Non-medicinal ingredients include dextrose (50mg), hydrochloric acid (to adjust pH), para-chloro-meta-cresol (1.35 mg) as preservative and water for injection.

THERAPEUTIC CLASSIFICATION:

Opioid analgesic.

Buprenol Indications

Buprenol is indicated for the relief of post-operative pain in cats.

Dosage and Administration

To ensure that analgesia is present during surgery and immediately on recovery, Buprenol should be administered pre-operatively as part of premedication.

An appropriately graduated syringe should be used to ensure accurate dosing.

If additional analgesia is subsequently required, this may be achieved by administration of a further dose of Buprenol two hours after the first dose or use of a suitable injectable NSAID.

Shake well before use. As with all parenteral drug products, the vial should be inspected visually for clarity, particulate matter, precipitate, discolouration, and leakage prior to administration, whenever the solution and container permit. Solutions showing haziness, particulate matter, precipitate, discolouration and leakage should not be used.

Contraindications

Do not administer by intrathecal or epidural route.

Do not use pre-operatively for caesarean section, due to the risk of respiratory depression in the offspring.

CAUTIONS:

Buprenorphine injection may cause respiratory depression and care should be taken when treating animals with impaired respiratory function or animals that are receiving drugs that can cause respiratory depression.

Buprenorphine injection may cause sedation, which may be potentiated by other centrally acting agents including tranquilizers, sedatives, and hypnotics. It is recommended that Buprenol not be used in conjunction with morphine or other opioid type analgesics e.g., etorphine, fentanyl, pethidine, methadone, papaveretum and butorphanol.

As animals treated with opioids may show variable responses, the response of individual animals should be monitored. In some cases, the repeat dose may fail to provide additional analgesia. In these cases, consideration should be given to use of an analgesic from an alternative class.

Buprenorphine injection should be used with caution in animals with impaired liver function, as the substance is metabolized by the liver and its intensity and duration of action may be affected in these animals.

Safety has not been evaluated in clinically compromised cats. In case of renal, cardiac, or hepatic dysfunction, or shock there may be a greater risk associated with the use of the product.

The safety of buprenorphine injection has not been established in breeding, pregnant or lactating cats. The safety of buprenorphine injection has not been established in cats less than 7 weeks of age.

Repeated administration earlier than the recommended repeat interval given under Dosage and Administration of the label is not recommended.

Warnings

As buprenorphine injection has opioid-like activity, care should be taken to avoid accidental self-injection. Following accidental self-injection or ingestion, seek medical advice taking the vial and the insert with you. Following eye contamination or skin contact, wash thoroughly with cold running water. Seek medical advice if irritation persists. Wash hands and the affected area thoroughly after any accidental spillage.

Keep out of reach of children.

Adverse Reactions

Although all adverse reactions are not reported, the following adverse reactions are based on voluntary post-approval adverse drug experience reporting. It is generally recognized that this method of reporting results in significant underreporting of adverse drug reactions. The most frequently reported adverse reactions are injection site pain and injection site reaction. Respiratory depression and tachypnea have been reported.

Mydriasis and signs of euphoria (excessive purring, pacing, rubbing) commonly occur in cats and will usually resolve within 24 hours.

OVERDOSE:

In case of an overdose, supportive measures should be instituted and if appropriate, naloxone may be used. Because the duration of naloxone may be shorter than that of buprenorphine injection, cats that are being treated for an overdose or with symptoms of respiratory depression should be closely monitored as additional doses of naloxone and/or ventilatory support may be required. Naloxone may not be beneficial in reversing buprenorphine injection related hyperthermia in cats.

Clinical Pharmacology

Buprenorphine injection is a potent, long-acting analgesic acting at opiate receptors in the central nervous system. Buprenorphine injection exerts its analgesic effect via high affinity binding to various subclasses of opiate receptors, particularly µ, in the central nervous system.

At clinical dose levels for analgesia, buprenorphine binds to opiate receptors with high affinity and high receptor avidity; such that its disassociation from the receptor is slow, as demonstrated in in vitro studies. This unique property of buprenorphine could account for its duration of activity.

Buprenorphine injection is rapidly absorbed after intramuscular injection. It is highly lipophilic and the volume of distribution in body compartments is large. Pharmacological effects (e.g., mydriasis) may occur within minutes after injection. Analgesic effects appear around 30 minutes after injection with peak effects usually within 1 - 1.5 hours.

Following intramuscular injection in cats, the mean terminal half-life was 6.3 hours, and the clearance was 23 mL/kg/min; however, there was considerable inter-cat variability in pharmacokinetic parameters.

Combined pharmacokinetic and pharmacodynamic studies have demonstrated a marked hysteresis between plasma concentrations and analgesic effect.

Buprenorphine is metabolized in the liver. The major route of excretion is in the faeces. Buprenorphine undergoes N-dealkylation and glucuronide conjugation by the intestinal wall and the liver and its metabolites are excreted via the bile into the gastro-intestinal tract.

Storage

Store between 15 - 30°C. Keep vial in the carton to protect from light. Discard contents 28 days after first dose is removed.

PRESENTATION:

Buprenol Injection is supplied in cartons of one 10 mL amber glass vial.

Manufactured by Labiana Life Sciences S.A. Terrasa, (Barcelona) 08228, Spain

Imported/Distributed by:

Champion Alstoe Animal Health Inc., Whitby, Ontario, L1N 4V1

Label identifier Version CDN 7, July 19, 2022

DIN 02531143

52070986/001

CPN: 1238059.0