Buprenorphine

(for veterinary information only)

BRAND NAME: BUPRINEX

AVAILABLE as          
INJECTABLE            
but usually prescribed as    
an ORAL SPRAY or LIQUID

BACKGROUND

Opiates have been used since ancient times for their pain relieving and euphoric properties. More recently, neurologic studies have revealed brain receptors which bind opiates, each type of receptors being responsible for different opiate effects. These receptors are named for Greek letters mu, kappa, delta, and sigma. The mu receptor is responsible for the narcotic effects of euphoria, pain relief, addiction, lowering of heart rate, and respiratory depression. Buprenorphine is partially active at the mu receptor.

While buprenorphine is considered approximately 30 times stronger than morphine in many of its effects, because morphine is more active at the mu receptor, morphine is a much a stronger pain reliever. Buprenorphine is best used for mild to moderate pain.

HOW THIS MEDICATION IS USED

This drug can be used as an injectable in the hospital setting but can also be used at home for pain control as an oral drop or spray. One dose lasts approximately 6 hours (in the cat) and the medication does not have to be swallowed; it will simply be absorbed directly from the mouth.

SIDE EFFECTS

  • Approximately 2/3 of people using this medication experienced drowsiness.
     
  • Buprenorphine can cause a drop in heart rate as well as in blood pressure.
     
  • Because respiratory depression is a possible side effect, buprenorphine should not be used in patients with respiratory compromise, including respiratory compromise from heart failure or head trauma. Respiratory depression from buprenorphine would be unusual in normal patients.
     
  • Buprenorphine is removed from the body via the liver. Patients with liver disease will have prolonged effects from this drug.
     
  • Naloxone can be used to reverse side effects of this or any other narcotic.

INTERACTIONS WITH OTHER DRUGS

The sedation side effect is more severe if this medication is used in conjunction with other medications that have a sedating side effect including antihistamines.

Buprenorphine should not be used with seligiline or any other monoamine oxidase inhibitor. A two week waiting period is recommended if buprenorphine or any other narcotic is to be used in a patient on such a drug (usually a dog with canine cognitive dysfunction taking seligiline).

CONCERNS AND CAUTIONS

Buprenorphine should be stored at room temperature and protected from light exposure.

Buprenorphine definitely crosses the placenta to unborn young and is secreted in mother's milk, possibly in a concentrated form. It is thus best not used in pregnancy or lactation.

Opiates should be used with caution in patients with hypothyroidism, hypoadrenocorticism, severe kidney failure, or who are generally debilititated.

Page last updated: 12/1/09