BUPRENORPHINE

(for veterinary information only)

BRAND NAME: BUPRINEX, CARPUJECT, SIMBADOL

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 receptor 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. While buprenorphine is commonly dispensed for three times daily usage, how long a dose lasts actually depends on the size of the dose. This is possible because of buprenorphine's "ceiling effect" which means that once a maximum effect has been reached (i.e. all the receptors have been bound with drug), giving more buprenorphine does not create a greater effect. Instead, the higher the dose, the longer the effects last.

In the cat (but not the dog), buprenorphine is absorbed into the body directly from the mouth membranes; swallowing is unnecessary. This is called "transmucosal" administration and is how buprenorphine is almost always used in the home setting.

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 because a potentially dangerous blood pressure situation called "serotonin syndrome" can result. 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). Other compounds that could be problematic in this way include tick control products containing amitraz or the pain reliever tramadol.

The following drugs can increase blood levels of buprenorphine: ketoconazole, itraconazole, fluconazole (all antifungals) and erythromycin (an antibacterial antibiotic).

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 debilitated.

Transmucosal delivery of buprenorphine in the cat is as reliable as injection but in the dog only about 50% of the buprenorphine is absorbed into the body from the mouth. This route might still be useful if dose adjustments are taken into consideration.

In 2014, a veterinary labelled product called Simbadol^® was released by Abbott Laboratories. This product is for cats only and is injectable only. The buprenorphine in Simbadol^® has been treated so that one dose can be expected to last for 24 hours. This version of buprenorphine cannot be used orally.

If you skip a dose by accident, do not double up on the next dose. Instead, simply pick up at the next dose as normal.

Buprenorphine is a controlled substance. Special paperwork is necessary for its prescription.

Short version (to help us
comply with "Lizzie's Law")

Page last updated: 5/6/2021