Efficacy and Safety
Ethiqa XR® (buprenorphine extended-release injectable suspension) 1.3 mg/mL CIII is the only pharmaceutical-grade extended-release buprenorphine FDA-indexed for the control of post-procedural pain in mice, rats, ferrets, and non-human primates. 1
- Proven long-acting extended-release technology1
- Delivers up to 3-days or up to 72 hours of demonstrated clinical analgesia in mice, rats, ferrets, and non-human primates with one subcutaneous injection
- Administration of a single injection minimizes animal stress and the inconvenience of multiple injections, helping improve animal welfare and reduce the variability of research
- Manufactured in the United States under cGMPs using pharmaceutical-grade ingredients
- FDA-Indexed, not compounded or diluted
- Favorable viscosity for easy administration
- Simple to order; available through national distributors
- Ensures you’re in compliance with FDA GFI #256 “Compounding Animal Drugs from Bulk Drug Substances”
Up to 3 Days of Continuous Pharmaceutical Grade Relief
Tail Flick and PK Data Prove Efficacy following 1 Dose
- Up to 5x dose, repeated 2x
- No remarkable observations
- No signs of pain
- No adverse effect on respiration
- No evidence of pica
- No significant differences in organ weights
- No meaningful differences in hematology and clinical chem values
- No gross pathology findings; no histologic findings
- No significant inflammation or edema
- No adverse effects demonstrated in the TAS studies (repeated SC doses at 2x, 6x, and 10x dose)
- No adverse effects in laboratory parameters (clinical observations, hematology, clinical chemistry, histopathology)
- Rats should be maintained on paper or soft bedding to avoid ingestion of wood chip-type bedding after administration of Ethiqa XR. Pica involving wood chip-type bedding can be lethal in rats.
Buprenorphine plasma concentrations were maintained above established levels for analgesia for up to 3-days or up to 72-hours in both mice and rats
Demonstrated safety in ferrets4
- Pharmacokinetic parameters of Ethiqa XR were studied in 4 adult female ferrets following a single subcutaneous injection of 0.6 mg/Kg body weight. Clinically significant blood levels were observed within 30 minutes up to 72 hours after administration.
Demonstrated safety in cynomolgus
Ethiqa XR is safe and efficacious. No abnormal behaviors or adverse effects at the injection site were observed.5
Demonstrated safety in marmosets
Ethiqa XR has a comparable safety profile to compounded BUP SR in marmosets and injection sites had significantly lower histopathological scores.6
Read the Ethiqa XR Brochure
References:
1. Data on file, Fidelis animal Health
2. FDA Expert Panel Report MIF Z-9000008-A-0000, p.3-53.
3. FDA Expert Panel Report—Rat Efficacy and Safety, p. 1-3.
4. Plunkard J, Jimenez I, Craney M, Villano J. Pharmacokinetics and efficacy of extended-release buprenorphine for post-operative pain management in the domestic ferret (Mustela putorius furo). Submitted for publication; 2024
5. Klein H, Levinson BL, Leary SL, Dobson G. A pharmacokinetic study of extended-release buprenorphine in cynomolgus monkeys (Macaca fasicularis). J Med Primatol. 2023 Dec;52(6):369-373. doi: 10.1111/jmp.12661. Epub 2023 Jul 11. PMID: 37432036.
6. Fabian NJ, Mannion AJ, Jamiel M, Anderson DJ, Rower JE, Reilly CA, Menegas W, Muthupalani S, Ta C, Fox JG, Kramer R, Haupt JL. Evaluation and comparison of pharmacokinetic profiles and safety of two extended-release buprenorphine formulations in common marmosets (Callithrix jacchus). Sci Rep. 2023 Jul 22;13(1):11864. doi: 10.1038/s41598-023-38973-2. PMID: 37481609; PMCID: PMC10363172.
BOXED WARNING
Abuse Potential
ETHIQA XR contains buprenorphine, an opioid that exposes humans to risks of misuse, abuse, and addiction, which can lead to overdose and death. Use of buprenorphine may lead to physical dependence. The risk of abuse by humans should be considered when storing, administering, and disposing of ETHIQA XR. Persons at increased risk for opioid abuse include those with a personal or family history of substance abuse (including drugs or alcohol) or mental illness (e.g., depression).
Life-Threatening Respiratory Depression
Serious, life-threatening, or fatal respiratory depression may occur with accidental exposure to or with misuse or abuse of ETHIQA XR. Monitor for respiratory depression if human exposure to buprenorphine occurs. Misuse or abuse of buprenorphine by swallowing, snorting, or injecting poses a significant risk of overdose and death.
Accidental Exposure
Because of the potential for adverse reactions associated with accidental exposure, ETHIQA XR should only be administered by veterinarians, veterinary technicians, or laboratory staff who are trained in the handling of potent opioids. Accidental exposure to ETHIQA XR, especially in children, can result in a fatal overdose of buprenorphine.
Risks From Concurrent Misuse or Abuse with Benzodiazepines or Other CNS Depressants
Concurrent misuse or abuse of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death.
See HUMAN SAFETY WARNINGS for detailed information.
Important Safety Information
For Rats, Mice, Ferrets, and Non-Human Primates:
Only administer Ethiqa XR® by subcutaneous injection. Ethiqa XR is not intended for intravenous, intra-arterial, intrathecal, intramuscular, or intra-peritoneal injection. Do not use in animals with pre-existing respiratory compromise.
Death has been reported when non-steroidal anti-inflammatory drugs (NSAIDs such as meloxicam and carprofen) and Ethiqa XR have been administered concomitantly in mice.
Do not house rats on wood chip-type bedding after administration of Ethiqa XR. Pica involving wood chip type bedding can be lethal.
Ethiqa XR may cause sedation, decreased blood pressure, decreased heart rate, decreased gastrointestinal mobility, and respiratory depression. Use caution with concomitant administration of Ethiqa XR with drugs that cause respiratory depression. Animals should be monitored for signs of decreased cardiovascular and respiratory function when receiving Ethiqa XR.
The safety of Ethiqa XR has not been evaluated in pregnant, lactating, neonatal, or immune-compromised animals.
For Humans:
Not for use in humans. Keep out of reach of children and pets.
Ethiqa XR contains buprenorphine, a Schedule III controlled substance with an abuse potential similar to other Schedule III opioids, which may lead to overdose and death.
Ethiqa XR should be handled appropriately to minimize the risk of misuse, abuse, addiction, and criminal diversion, including restriction of access, the use of
accounting procedures, and proper disposal methods as appropriate to the laboratory setting and as required by law.
Ethiqa XR should only be handled and administered by a veterinarian, veterinarian technician, or laboratory staff trained in the handling of potent opioids. Wear
protective clothing when administering Ethiqa XR to avoid direct contact with human skin, eyes, oral, or other mucus membranes which could result in absorption of buprenorphine and adverse reactions.
For more information, consult the Prescribing Information including the Boxed Warning.
SA.EthiqaXR.060.04.24
