fentaNYL (parenteral) (fen-ta-nil) Sublimaze

 Indications

Analgesic supplement to general anesthesia; usually

with other agents (ultra–short-acting barbiturates,

neuromuscular blocking agents, and inhalation anesthetics)

to produce balanced anesthesia. Induction/

maintenance of anesthesia (with oxygen or oxygen/nitrous

oxide and a neuromuscular blocking agent). Neuroleptanalgesia/

neuroleptanesthesia (with or without

nitrous oxide). Supplement to regional/local anesthesia.

Preoperative and postoperative analgesia. Unlabeled

Use: Continuous IV infusion as part of PCA.

Action

Binds to opiate receptors in the CNS, altering the response

to and perception of pain. Produces CNS depression.

Therapeutic Effects: Supplement in anesthesia.

Decreased pain.

Pharmacokinetics

Absorption: Well absorbed after IM administration.

Distribution: Unknown.

Metabolism and Excretion: Mostly metabolized

by the liver, 10–25% excreted unchanged by the kidneys.

Half-life: Children: Bolus dose—2.4 hr, long-term

continuous infusion—11–36 hr; Adults: 2–4 hr (q

after cardiopulmonary bypass and in geriatric patients).

TIME/ACTION PROFILE (analgesia*)

ROUTE ONSET PEAK DURATION

IM 7–15 min 20–30 min 1–2 hr

IV 1–2 min 3–5 min 0.5–1 hr

*Respiratory depression may last longer than analgesia.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; cross-sensitivity

among agents may occur; Known intolerance.

Use Cautiously in: Geri: Geriatric, debilitated, or

critically ill patients; Diabetes; Severe renal, pulmonary,

or hepatic disease; CNS tumors;qintracranial pressure;

Head trauma; Adrenal insufficiency; Undiagnosed

abdominal pain; Hypothyroidism; Alcoholism; Cardiac

disease (arrhythmias); OB: Use only if the potential

benefit justifies the potential risk to the fetus. Chronic

maternal treatment with opioids during pregnancy may

result in neonatal abstinence syndrome; Lactation: Use

only if the potential benefit of breast feeding justifies

that potential risk to the infant (may cause infant sedation

and/or respiratory depression).

Adverse Reactions/Side Effects

CNS: confusion, paradoxical excitation/delirium, postoperative

depression, postoperative drowsiness.

EENT: blurred/double vision. Resp: APNEA, LARYNGOSPASM,

allergic bronchospasm, respiratory depression.

CV: arrhythmias, bradycardia, circulatory depression,

hypotension. GI: biliary spasm, nausea/vomiting.

Derm: facial itching. Endo: adrenal insufficiency.

MS: skeletal and thoracic muscle rigidity (with rapid

IV infusion).

Interactions

Drug-Drug: Avoid use in patients who have received

MAO inhibitors within the previous 14 days (may

produce unpredictable, potentially fatal reactions).

Concomitant use of CYP3A4 inhibitors including ritonavir,

ketoconazole, itraconazole, clarithromycin,

nelfinavir, nefazodone, diltiazem, aprepitant,

fluconazole, fosamprenavir, verapamil, and

erythromycin may result inqplasma levels andqrisk

of CNS and respiratory depression. Concurrent use with

CYP3A4 inducers including barbiturates, carbamazepine,

efavirenz, corticosteroids, modafinil,

nevirapine, oxcarbazepine, phenobarbital, phenytoin,

rifabutin, or rifampin maypfentanyl levels

and analgesia; if inducers are discontinued or dosage

p,

patients should be monitored for signs of opioid toxicity

and necessary dose adjustments should be made.

Use with benzodiazepines or other CNS depressants

including other opioids, non-benzodiazepine

sedative/hypnotics, anxiolytics, general anesthetics,

muscle relaxants, antipsychotics, and

alcohol may cause profound sedation, respiratory depression,

coma, and death; reserve concurrent use for

when alternative treatment options are inadequate.q

risk of hypotension with benzodiazepines. Nalbuphine, buprenorphine, or pentazocine maypanalgesia.

Drugs that affect serotonergic neurotransmitter

systems, including tricyclic antidepressants, SSRIs,

SNRIs, MAO inhibitors, TCAs, tramadol, trazodone,

mirtazapine, 5–HT3 receptor antagonists,

linezolid, methylene blue, and triptansqrisk of

serotonin syndrome.

Drug-Food: Grapefruit juice is a moderate inhibitor

of the CYP3A4 enzyme system; concurrent use may

qblood levels and the risk of respiratory and CNS depression.

Careful monitoring and dose adjustment is

recommended.

Route/Dosage

Preoperative Use

IM, IV (Adults and Children 12 yr): 50–100 mcg

30–60 min before surgery.

Adjunct to General Anesthesia

IM, IV (Adults and Children 12 yr): Low dose–

minor surgery—2 mcg/kg. Moderate dose–major

surgery—2–20 mcg/kg. High dose–major surgery—

20–50 mcg /kg.

Adjunct to Regional Anesthesia

IM, IV (Adults and Children 12 yr): 50–100 mcg.

Postoperative Use (Recovery Room)

IM, IV (Adults and Children 12 yr): 50–100 mcg;

may repeat in 1–2 hr.

General Anesthesia

IV (Adults and Children 12 yr): 50–100 mcg/kg

(up to 150 mcg/kg).

IV (Children 1–12 yr): 2–3 mcg/kg.

Sedation/Analgesia

IV (Adults and Children 12 yr): 0.5–1 mcg/kg/

dose, may repeat after 30–60 min.

IV (Children 1–12 yr): Bolus—1–2 mcg/kg/dose,

may repeat at 30–60 min intervals. Continuous infusion—

1–5 mcg/kg/hr following bolus dose.

IV (Neonates): Bolus—0.5–3 mcg/kg/dose. Continuous

infusion—0.5–2 mcg/kg/hr following bolus

dose. Continuous infusion during ECMO—5–10

mcg/kg bolus followed by 1–5 mcg/kg/hr, may require

up to 20 mcg/kg/hr after 5 days of therapy.

Availability (generic available)

Injection: 50 mcg/mL.