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butorphanol (Stadol)

 

Classes: Opioid Analgesics; Analgesics, Opioid Partial Agonist

Dosing and uses of Stadol (butorphanol)

 

Adult dosage forms and strengths

injectable solution: Schedule IV

  • 1mg/mL
  • 2mg/mL

nasal spray: Schedule IV

  • 10 mg/mL (1mg/spray)

 

Pain

Indicated for pain when use of opioid analgesic is appropriate

IV: 1 mg IV q3-4hr PRN; dosage range 0.5-2 mg q3-4hr

IM: 2 mg IM q3-4 hr; dosage range 1-4 mg q3-4hr

IntranasaL

  • Initial: 1 mg (1 spray in 1 nostril); may repeat once after 60-90 min if inadequate pain relief
  • Depending on pain severity, by give initial dose of 2 mg (1 spray in each nostril); patient must remain recumbant; do not repeat this dose
  • Maintenance: 1 mg (1 spray in 1 nostril) q3-4hr prn

 

Balanced Anesthesia

2 mg IV before induction and/or 0.5-1 mg increments during anesthesia (higher dose may be required, up to 0.06 mg/kg, or 4 mg/70 kg)

Total cumulative dose varies; typically ranges between 4-12.5 mg (0.06-0.18 mg/kg)

 

Labor Pain

Indicated for labor pain in full-term (37 weeks gestation or more) women without fetal distress in early labor

1-2 mg/dose IV/IM; may repeat PRN q4hr

Decrease dose if concomitantly used with other analgesics or CNS depressants

Do not administer within 4 hr of anticipated delivery

 

Preoperative & Preanesthesia

2 mg IM 60-90 minutes preop

This dose is approximately equipotent to morphine 10 mg or meperidine 80 mg

 

Geriatric Dosing

Decrease initial dose by 50% (0.5 mg IV and 1 mg IM)

Increase dose interval from q4hr to q6hr

IntranasaL

  • 1 mg (1 spray in 1 nostril) initially, may repeat once after 90-120 minutes if inadequate pain control
  • Maintenance: 1 mg (1 spray in 1 nostril) q4-6hr prn

 

Renal & Hepatic Impairment

Decrease initial dose by 50% (0.5 mg IV and 1 mg IM)

Increase dose interval from q4hr to q6hr

IntranasaL

  • 1 mg (1 spray in 1 nostril) initially, may repeat once after 90-120 minutes if inadequate pain control
  • Maintenance: 1 mg (1 spray in 1 nostril) q4-6hr prn

 

Pediatric dosage forms and strengths

<18 years old: Not recommended

 

Stadol (butorphanol) adverse (side) effects

>10%

Sedation (43%)

Dizziness (19%)

Nasal congestion (13%)

Nausea and/or vomiting (13%)

Insomnia (11%)

 

1-10%

Anorexia

Anxiety

Blurred vision

Bronchitis

Confusion

Constipation

Cough

Dizziness

Dry mouth

Dyspnea

Ear pain

Epistaxis

Euphoria

Floating feeling

Headache

Lethargy

Nasal irritation

Nervousness

Paresthesia

Palpitations

Pharyngitis

Pruritis

Rhinitis

Sensation of heat

Sinus congestion

Sinusitis

Stomach pain

Sweating/clammy

Taste abnormalities

Tinnitus

Tremor

URI

Vasodilation

 

<1%

Apnea

Increased/decreased Bp

Bradycardia

Chest pain

Respiratory depression

Tachycardia

 

Warnings

Contraindications

Absolute: opioid dependence, respiratory depression, respiratory failure

Relative: cardiac arrhythmias, cardiovascular disease, coronary insufficiency, myocardial infarction, toxin-mediated diarrhea

 

Cautions

Drug abuse, emotional lability, head injury, hepatic/renal impairment, incr ICP, GI/urinary obstruction, BPH, hypothyroidism

Less risk of respiratory sedation than with pure opioid agonist

May produce withdrawal in opioid dependent pts

Avoid alcohoL

 

Pregnancy and lactation

Pregnancy category: C; D if used for prolonged periods or near term

Lactation: excreted in breast milk, but infant likely exposed to insignificant amounts (AAP Committee states compatible w/ nursing)

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Stadol (butorphanol)

Mechanism of action

Narcotic agonist-analgesic of kappa opiate receptors and partial agonist of mu opiate receptors; inhibits ascending pain pathways, which causes alteration in response to pain; produces analgesia, respiratory depression, and sedation

 

Pharmacokinetics

Half-life: 4.6 hr

Onset: <10 min (IV); 5-10 min (IM); within 15 min (nasal)

Duration: 3-4 hr (IV/IM); 4-5hr (nasal);

Peak effect: 0.5-1hr (IM); 4-5min (IV)

Bioavailability: 60-70% (nasal)

Protein Bound: 80%

Vd: 487 L (range: 305-901 L)

Metabolites: hydroxybutorphanol; N-dealkylation & conjugation of butorphanol & its metabolites)

Metabolism: Liver (hydroxylation)

Excretion: Urine (primarily)

 

Administration

IV Compatibilities

Syringe: (partial list) atropine, diphenhydramine, fentanyl, hydroxyzine, meperidine, metoclopramide, midazolam, prochlorperazine, promethazine

Y-site: (partial list) allopurinol, bivalirudin, labetalol, linezolid, propofoL

 

IV Incompatibilities

Syringe: dimenhydrinate, pentobarbitaL

Y-site: amphotericin B cholesteryl SO4, midazolam

 

IV Administration

pH: 3.0-5.5

IM/IV injection

 

Storage

Store at room temp

Protect from freezing