Efficacy and Safety

Ethiqa XR® (buprenorphine extended-release injectable suspension) 1.3 mg/mL CIII is the only commercial pharmaceutical-grade extended-release buprenorphine FDA-indexed for the control of post-procedural pain in mice, rats, and ferrets.1  

  • Proven long-acting extended-release technology1
  • Delivers up to 3-days or up to 72 hours of demonstrated clinical analgesia in mice, rats, and ferrets with one subcutaneous injection1
  • 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
  • Not compounded, not diluted
  • Favorable viscosity for easy administration
  • Simple to order
  • Complies with FDA GFI #256 “Compounding Animal Drugs from Bulk Drug Substances” and is available through national distributors
*current Good Manufacturing Practices regulated by the FDA

Up to 3 Days of Continuous Pharmaceutical Grade Relief

Tail Flick and PK Data Prove Efficacy following 1 Dose

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

The Peace of Mind from a Product that is FDA-Indexed and Promotes Animal Welfare

Pharmaceutical grade, endotoxin-free

Demonstrated safety in mice1

  • 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

References:
1. FDA Expert Panel Report MIF Z-9000008-A-0000, p.3-53.
2. FDA Expert Panel Report—Rat Efficacy and Safety, p. 1-3.

Demonstrated safety in rats2

  • 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.

Demonstrated safety in ferrets

  • 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.

An Ethical Imperative

The Essential Need for Effective Pain Management in Laboratory Mice, Rats, and Ferrets The appropriate use of anesthetics, tranquilizers, analgesics, and nonpharmacologic interventions in research animals is an ethical and scientific imperative. Pain and distress are undesirable variables in most scientific research projects, and if not relieved, can result in unacceptable animal welfare and invalid scientific outcomes. (emphasis added) — American College of Laboratory Animal Medicine (ACLAM), Position Statement on Pain and Distress in Research Animals

Pharmaceutical Grade Medications Help Limit Risks—Use When Available “The use of pharmaceutical grade chemicals and other substances ensures that toxic or unwanted side effects are not introduced into studies conducted with experimental animals. They should therefore be used, when available, for all animal-related procedures (USDA 1977b). (emphasis added) — NIH Guide for the Care and Use of Laboratory Animals

Achieve Industry Welfare Standards

  • Leading lab animal medicine authorities increasingly recognize the ethical and scientific importance of protecting the welfare of research animals by providing rat and mouse analgesia at the highest level of quality.
  • Many industry organizations, including ACLAM, AALAS, and ASLAP, have developed official position statements recognizing the need to reduce the discomfort of lab animals with effective pain management.

LEARN MORE: For more information about laboratory industry associations and their positions regarding ethics and lab animal pain management, visit their websites at the links below:

American College of Laboratory Animal Medicine (ACLAM)
American Society of Laboratory Animal Practitioners (ASLAP)
Institute for Laboratory Animal Research (ILAR)
American Association for Laboratory Animal Science (AALAS)

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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, and Ferrets:

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.

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.