SUBLIMAZE Dosage & Rx Info | Uses, Side Effects

Sublimaze Generic Name & Formulations

Legal Class

CII

General Description

Fentanyl citrate 50mcg/mL; soln for IV or IM inj; preservative-free.

Pharmacological Class

Opioid agonist.

How Supplied

Ampules (2mL, 5mL)—10, 25; 10mL, 20mL—5; Vials (50mL)—1

Manufacturer

Akorn, Inc.

Mechanism of Action

Fentanyl is an opioid agonist whose principal therapeutic action is analgesia. The precise mechanism of the analgesic action is unknown although fentanyl is known to be a mu opioid receptor agonist. Specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and play a role in the analgesic effects of this drug.

Sublimaze Indications

Indications

Short-term analgesia during anesthetic periods, premedication, induction and maintenance; and in the immediate postoperative periods as need arises. Analgesic supplement in general or regional anesthesia. Concomitantly with neuroleptic as an anesthetic premedication, for anesthesia induction and as an adjunct in the maintenance of general and regional anesthesia. As an anesthetic in combination with oxygen in selected high risk patients (eg, undergoing open heart surgery, complicated neurological or orthopedic procedures).

Sublimaze Dosage and Administration

Adult

Should be administered only by trained persons in IV anesthetics and management of respiratory effects in an adequate facility. Have an opioid antagonist and other resuscitative measures available. Individualize. Premedication: 50–100mcg (1–2mL) by IM inj 30–60 mins prior to surgery. Adjunct to general anesthesia (low dose): 2mcg/kg; (moderate dose): 2–20mcg/kg; (high dose): 20–50mcg/kg; see full labeling. Adjunct to regional anesthesia: 50–100mcg (1–2mL) by IM inj or slow IV (over 1–2 mins), when needed. Post-op: 50–100mcg (1–2mL) by IM inj, may repeat in 1–2 hrs as needed. General anesthetic: 50–100mcg/kg (1–2mL/kg), may administer with oxygen and a muscle relaxant; in certain cases (eg, open heart surgery, complicated neurological or orthopedic procedures), doses up to 150mcg/kg (3mL/kg) may be needed. Elderly, debilitated: reduce dose. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

Children

<2yrs: not established. 2–12yrs (induction and maintenance): 2–3mcg/kg. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

Sublimaze Contraindications

Not Applicable

Sublimaze Boxed Warnings

Boxed Warning

Serious and life-threatening risks from use of Sublimaze: Addiction, abuse, and misuse. Life-threatening respiratory depression. Risks from concomitant use with benzodiazepines or other CNS depressants. Cytochrome P450 3A4 interaction.

Sublimaze Warnings/Precautions

Warnings/Precautions

Abuse potential (monitor). Life-threatening respiratory depression; monitor during initiation or following a dose increase. Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor closely. Opioid-induced hyperalgesia (OIH) and allodynia; consider decreasing dose of current opioid or opioid rotation if OIH is suspected. Monitor for signs of hypotension when initiating or titrating dose. Adrenal insufficiency. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Hypertension. Bradyarrhythmias. Drug abusers. Renal or hepatic impairment. Monitor vital signs routinely. Elderly. Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery: not recommended. Nursing mothers: monitor infants.

Sublimaze Pharmacokinetics

Distribution

Volume of distribution: 4 L/kg. Distribution time: 1.7 minutes; Redistribution time: 13 minutes.

Metabolism

Hepatic.

Elimination

Renal (~75%), fecal (~9%). Half-life: 219 minutes.

Sublimaze Interactions

Interactions

Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT₃ antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and/or precipitate withdrawal symptoms. Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors, grapefruit juice). Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics. Hypertension with concomitant neuroleptics during anesthesia combination use; monitor ECG. Cardiovascular depression with nitrous oxide and high-dose fentanyl. May increase serum amylase.

Sublimaze Adverse Reactions

Adverse Reactions

Respiratory depression, apnea, skeletal muscle rigidity, bradycardia (may be severe); orthostatic hypotension, syncope, OIH and allodynia.

Sublimaze Clinical Trials

See Literature

Sublimaze Note