Drug Profiles:
STADOL®

CAUTION: Federal law prohibits dispensing without prescription.

PRESCRIPTION: Butorphanol tartrate is a crystalline substance. the dose in expressed as the tartrate salt. One milligram of the salt is equivalant to 0.68 mg of the free base. The n-octanol/aqueous buffer partition coefficient of butorphanol is 180:1 at pH 7.5

STADOL® Injection, USP, is a sterile, parenteral, aqueous solution of butorphanol tartrate for intravenous or intramuscular administration. In addition to 1 or 2 mg of butorphanol tartrate, each mL of solution contains 3.3 mg of citric acid, 6.4 mg sodium citrate, and 6.4 mg sodium chloride, and 0.1 mg benzethonium chloride (in multiple dose vial only) and a preservative.

 STADOL NS® is an aqueous solution of butorphanol tartate for administration as a metered spray to the nasal mucosa. Each bottle of STADOL NS contains 2.5 ml of a 10 mg/ml solution of butorphanol tartate with sodium chloride, citric acid, and benzethonium chloride in purified water with sodium hydroxide and/or hydrochloric acid added to adjust the pH to 5.0.

ACTIONS: Butorphanol and its major metabolites are agonists at k-opioid receptors and mixed agonist-antagonist at µ-opioid receptors.

In addition to analgesia, CNS effects include depression of spontaneous respiratory activity and cough, stimulation of the emetic center, miosis and sedation. Effects possibly mediated by non-CNS mechanisms include alteration in cardiovascular resistance and capacitance, bronchomotor tone, gastrointestinal secretory and motor activity and bladder sphincter activity.

INDICATIONS: STADOL NS® (butorphanol tartrate) is indicated for the management of pain when the use of an opioid analgesic is appropriate.

CONTRAINDICATIONS: STADOL® Injection and STADOL NS® are contraindicated in patients hypersensitive to butorphanlo tartrate or the preservative benzethonium chloride in STADOL NS® or STADOL® Injection in the multi-dose vial.

PRECAUTIONS: Hypotension association with syncope during the first hour of dosing with STADOL NS® has been reported rarely, particularly in patients with past history of similar reactions to opioid analgesics. Therefore, patients should be advised to avaoid activities with potential risks.

ADVERSE REACTIONS: asthenia/lethargy, headache, sensation of heat, dry mouth, nausea and/or vomiting stomach pain, anxiety, dizziness, insomnia, nervousness, cough, nasal congestion and/or irritation, sweating, blurred vision, ear pain, and tinnitus (ringing in ears).

DOSAGE and ADMINISTRATION:

Factors to be considered in determining the dose are age, body weight, physical status, underlying pathological condition, use of other drugs, type of anesthesia to be used, and surgical procedure involved. Use in the elderly, patients with hepatic or renal disease or in labor requires extra caution. The following doses are for patients who do not have impaired hepatic or renal function and who are not on CNS active agents.

Use for Pain

STADOL® Injection

Intravenous: The usual recommended single dose for IV administration is 1mg repeated every 3 to 4 hours as necessary. The effective dosage range depending on the severity of pain is 0.5 to 2 mg repeated every 3 to 4 hours.

Intramuscular: The usual recommended single dose for IM administration is 2 mg in patients who will be able to remain recumbent, in the event drowsiness or dizziness occurs. This may be repeated every 3 to 4 hours, as necessary. The effective dosage range depending on the sverity of pain is 1 to 4 mg repeated every 3 to 4 hours. There are insufficient clinical data to recommend single doses above 4 mg.

STADOL NS®

The usual recommended dose for initial masal administration is 1 mg (1 spray in one nostril). Adherence to this dose reduces the incidence of drowsiness and dizziness. If adequate pain relief is not achieved within 60-90 minutes, an additional 1 mg dose may be given.

HOW SUPPLIED:

STADOL NS® (butorphanol tartrate) Nasal Spray

STADOL NS is supplied in child-resistant prescription vial containing a metered dose spray pump with protective clip and dust cover, a bottle of nasal spray solution, and a patient instruction leaflet. On average, one bottle will deliver 14-15 doses if no repriming in necessary.