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Butorphanol

Kappa-opioid agonist and mu antagonist

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Butorphanol

Butorphanol is a mixed-action opioid with analgesic, sedative and antitussive properties. It is used alone for selected purposes and commonly with other sedatives for restraint or anesthetic premedication. Analgesia is generally shorter and less robust than that provided by full mu-opioid agonists, especially for severe somatic or postoperative pain.

Its veterinary roles include equine visceral pain, combination sedation and suppression of selected nonproductive cough in dogs. The relative contributions of analgesia, sedation and cough suppression vary with species, exposure and the clinical setting.

Group

Kappa-opioid agonist and mu antagonist

Mechanism of Action

Butorphanol acts principally as a kappa-opioid receptor agonist with weak antagonist or low-efficacy activity at mu receptors. Kappa signaling modifies nociceptive processing and contributes to sedation, with useful visceral analgesia in some species. The receptor profile produces a different maximal effect from a full mu agonist.

Central suppression of the cough reflex underlies its antitussive use. This effect can occur independently of the degree of analgesia, explaining why usefulness for cough does not establish adequate control of a severe painful procedure.

Its relatively short analgesic action and mixed receptor behavior influence combination use. It can modify or partially oppose effects of a full mu agonist, while combination with sedatives can deepen restraint without proportionately improving all forms of pain control. Redosing based only on apparent wakefulness can therefore misjudge its clinical effect.

Dose Rates

Dogs

Use / stageDoseRouteScheduleInstructions
Cough suppression0.055 mg/kgSCEvery 6–12 h
Cough suppression0.011 mg/kgIM
Cough suppression0.5–1 mg/kgPOEvery 6–12 h
Sedation and premedication0.2–0.4 mg/kgIV, IM, SCMay be combined with acepromazine or another sedative.
Analgesia0.2–0.4 mg/kgIV, IM, SCEvery 2–4 h
Analgesia1–4 mg/kgPOEvery 6 h
Analgesic infusion — Loading0.2–0.4 mg/kgIVOnce
Analgesic infusion — Maintenance0.1–0.2 mg/kg/hourIVContinuous
Cough suppression0.055–0.11 mg/kgSCEvery 6–12 hUp to 7 days
Cough suppression0.55–1.1 mg/kgPOEvery 6–12 hUp to 7 days
Cough suppression0.05–1 mg/kgPOEvery 6–12 hTitrate to cough control without excessive sedation.
Cough suppression0.55–1.1 mg/kgPOAs needed
Alternative analgesia0.1–0.5 mg/kgIV, IM, SCSedation may outlast analgesia; effect on pain can last an hour or less.
Epidural analgesia0.25 mg/kgEPIDURALUse preservative-free diluent/local anesthetic in a procedure-specific epidural plan; reported onset under 30 minutes and duration 2–4 hours.
Partial reversal of full mu agonists0.05–0.1 mg/kgIVMay reduce sedation/respiratory depression while retaining some analgesia; monitor clinical response.
Immobilization combinationReference onlyIMIM butorphanol 0.2 mg/kg plus medetomidine 0.001–0.01 mg/kg and midazolam 0.05–0.2 mg/kg. A higher medetomidine alternative uses 0.01–0.02 mg/kg; additional anesthetic or analgesic choices depend on the procedure.
Analgesic infusion0.1–0.4 mg/kg/hourIVContinuous
Cisplatin-associated emesis prevention0.4 mg/kgIMOnceAdminister 30 minutes before cisplatin infusion.

Cats

Use / stageDoseRouteScheduleInstructions
Analgesia0.2–0.8 mg/kgIV, SCEvery 2–6 h
Analgesia1.5 mg/kgPOEvery 4–8 h
Sedation0.2–0.5 mg/kgIV, IMUse the lower 0.2 mg/kg dose when combined with other agents for short procedures.
Analgesic infusion — Loading0.2–0.4 mg/kgIVOnce
Analgesic infusion — Maintenance0.1–0.2 mg/kg/hourIVContinuous
Alternative analgesia0.1–0.5 mg/kgIV, IM, SCSedation may outlast analgesia; effect on pain can last an hour or less.
Epidural analgesia0.25 mg/kgEPIDURALUse preservative-free diluent/local anesthetic in a procedure-specific epidural plan; reported onset under 30 minutes and duration 2–4 hours.
Partial reversal of full mu agonists0.05–0.1 mg/kgIVMay reduce sedation/respiratory depression while retaining some analgesia; monitor clinical response.
Immobilization combinationReference onlyIMIM butorphanol 0.2 mg/kg plus medetomidine 0.001–0.015 mg/kg and midazolam 0.05–0.2 mg/kg. A higher-sedation alternative uses medetomidine 0.015–0.02 mg/kg; ketamine 1–5 mg/kg may be added if needed.
Postoperative infusion with ketamineReference onlyIVButorphanol loading 0.1–0.2 mg/kg IV followed by 0.1–0.2 mg/kg/hour; ketamine loading 0.1 mg/kg IV followed by 0.4 mg/kg/hour is a separate concurrent component.

Horses

Use / stageDoseRouteScheduleInstructions
Analgesia0.2–0.4 mg/kgIVEvery 3–4 h
Lower-dose analgesia0.02–0.1 mg/kgIVLower doses, including 0.1 mg/kg, may limit intestinal hypomotility.
Lower-dose analgesia0.04–0.2 mg/kgIM
Sedation0.01–0.06 mg/kgIV
Analgesic infusion13–24 mcg/kg/hourIVContinuous
Analgesia0.1 mg/kgIVEvery 3–4 hUp to 2 days
Abdominal pain0.01–0.02 mg/kgIVMay be used alone or with a separate xylazine regimen.
Foal analgesia0.1–0.2 mg/kgIV, IMFoals only.
Postoperative analgesic infusionReference onlyIVA reported regimen loads 17.8 mcg/kg then infuses 23.7 mcg/kg/hour; the loading route is not independently specified. Another regimen infuses 13 mcg/kg/hour without an assigned loading dose.
Cough suppression0.02 mg/kgIMEvery 8–12 h
Field anesthesia adjunctReference onlyIVGive xylazine 1 mg/kg IV or 2 mg/kg IM and allow 5–10 minutes or longer for IM effect. Only after adequate sedation, ketamine 2 mg/kg IV may be used. Butorphanol 0.02–0.04 mg/kg IV can supplement inadequate sedation before ketamine; alternatives include diazepam 0.03 mg/kg IV or 5% guaifenesin to effect. Do not induce with ketamine in an inadequately sedated horse.

Ruminants

Use / stageDoseRouteScheduleInstructions
Analgesia0.05–0.2 mg/kgIV

Cattle

Use / stageDoseRouteScheduleInstructions
Sedation with xylazine0.01–0.02 mg/kgIVOnly in the stated xylazine combination.
Analgesia0.02–0.25 mg/kgIV, SC
Adult surgical analgesia20–30 mg/animalIVAdult cattle; optional pretreatment with 10 mg xylazine is described.

Ferrets

Use / stageDoseRouteScheduleInstructions
Sedation and analgesia0.05–0.1 mg/kgIM, SC
Analgesia0.05–0.5 mg/kgSC, IMEvery 4 h
Injectable anesthetic combinationsReference onlyIMAlternatives include butorphanol 0.2 mg/kg with xylazine 2 mg/kg IM; or butorphanol 0.1 mg/kg, ketamine 5 mg/kg and medetomidine 80 mcg/kg IM; or butorphanol 0.2 mg/kg, tiletamine/zolazepam 1.5 mg/kg and xylazine 1.5 mg/kg IM. Do not merge the alternatives.
Postoperative analgesic infusionReference onlyIVLoading 0.1–0.2 mg/kg followed by 0.1–0.2 mg/kg/hour; the excerpt does not explicitly assign the loading route, so the full instruction is retained as a protocol.

Rabbits

Use / stageDoseRouteScheduleInstructions
Postoperative analgesic infusionReference onlyIVLoading 0.1–0.2 mg/kg followed by 0.1–0.2 mg/kg/hour; the excerpt does not explicitly assign the loading route, so the full instruction is retained as a protocol.
Chemical restraint0.1–0.5 mg/kgIV
Postoperative analgesia0.1–0.5 mg/kgIV, SCEvery 2–4 h
Postoperative analgesia0.4 mg/kgSCEvery 4–6 h

Birds

Use / stageDoseRouteScheduleInstructions
Analgesia and sedation1–4 mg/kgIM, IVEvery 2–3 h
Analgesia and sedation1–4 mg/kgIM, IV, POEvery 4 h

Alpacas

Use / stageDoseRouteScheduleInstructions
Sedation0.1 mg/kgIM
Sedation10 mg/animalIM
Analgesia0.1 mg/kgIV, IM, SCEvery 4–6 h
Injectable anesthesiaReference onlyIMAlternative combinations: butorphanol 0.07–0.1 mg/kg, ketamine 0.2–0.3 mg/kg and xylazine 0.2–0.3 mg/kg IV; or butorphanol 0.05–0.1 mg/kg, ketamine 0.2–0.5 mg/kg and xylazine 0.2–0.5 mg/kg IM. These are component-specific protocols.
Procedural anesthesiaReference onlyIMIM combination: butorphanol 0.046 mg/kg, xylazine 0.46 mg/kg and ketamine 4.6 mg/kg. If needed, half the original ketamine/xylazine doses can extend anesthesia; do not repeat the entire mixture automatically.

Llamas

Use / stageDoseRouteScheduleInstructions
Sedation0.1 mg/kgIM
Sedation10 mg/animalIM
Analgesia0.1 mg/kgIV, IM, SCEvery 4–6 h
Injectable anesthesiaReference onlyIMAlternative combinations: butorphanol 0.07–0.1 mg/kg, ketamine 0.2–0.3 mg/kg and xylazine 0.2–0.3 mg/kg IV; or butorphanol 0.05–0.1 mg/kg, ketamine 0.2–0.5 mg/kg and xylazine 0.2–0.5 mg/kg IM. These are component-specific protocols.
Procedural anesthesiaReference onlyIMIM combination: butorphanol 0.037 mg/kg, xylazine 0.37 mg/kg and ketamine 3.7 mg/kg. Allow quiet induction and adequate onset time.

Reptiles

Use / stageDoseRouteScheduleInstructions
Historical analgesia0.05–1 mg/kgIM, IV, PO, SCEvery 12 hBroad historical reptile/amphibian recommendation; species-specific efficacy varies. Turtles and tortoises may show respiratory depression with limited analgesia.

Indications

Contraindications

Interactions

Adverse effects

Toxicity

Support breathing if depressed; naloxone can reverse serious opioid effects.

Preparations

PreparationFormStrengthRoute
Butorphanol 1 mg tabletTablet1 mg / tabletPO
Butorphanol 5 mg tabletTablet5 mg / tabletPO
Butorphanol 10 mg tabletTablet10 mg / tabletPO
Butorphanol 0.5 mg/mL injectionInjection0.5 mg / mLIV, IM, SC
Butorphanol 1 mg/mL injectionInjection1 mg / mLIV, IM, SC
Butorphanol 2 mg/mL injectionInjection2 mg / mLIV, IM, SC
Butorphanol 10 mg/mL injectionInjection10 mg / mLIV, IM, SC

Monitoring and Administration

Monitor heart rate, breathing and pain frequently; analgesia is often only about an hour.

An approximate ceiling of 0.8 mg/kg is described for routine small-animal use. This is a weight-based ceiling, not a total-mg cap.

Birds may need substantially different doses because of rapid clearance; the cited 2–4 mg/kg every 2–4 hours lacks an administration route and is not generalized into a calculator regimen.

One pharmacogenetic recommendation reduces doses by 25% in heterozygous ABCB1/MDR1 dogs and by approximately 30–50% in homozygous mutants. Monitor sedation and respiration.

Doses are expressed as butorphanol base activity. A human salt-labelled preparation can require conversion: 1 mg tartrate salt corresponds to 0.68 mg base; do not apply this to products already labelled in base equivalents.

Veterinary use

For veterinary reference. Confirm the indication, dose, route, interval, product strength and any applicable withdrawal period before administration.