What is Fentanyl citrate - Meaning and definition

Published by Roberto Wenk. Reviewed by Alison Ramsey. Last updated date: November 21, 2018.

The citrate salt of fentanyl, a synthetic opioid related to the phenylpiperidines, with analgesic and anesthetic properties.
Fentanyl exerts its analgesic effect by selectively binding to the mu-opioid receptor in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates.
Stimulation of the mu-receptor inhibits adenyl cyclase activity, induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels, and blocks the opening of N-type voltage-gated calcium channels, resulting in hyperpolarization and reduced neuronal excitability; in addition, neuronal release of neurotransmitters, such as substance P, GABA, dopamine, acetylcholine, and noradrenaline, may decrease.
Additional pharmacological effects of fentanyl include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, and cough suppression.

Fentanyl citrate buccal tablet A tablet formulation containing the citrate salt of the synthetic anilidopiperidine opiate fentanyl with analgesic activity. Upon contact with the buccal mucosa, fentanyl citrate buccal tablet rapidly releases fentanyl, which is quickly absorbed into the systemic circulation.

Fentanyl citrate pectin-based nasal spray A pectin-based, aqueous nasal spray containing the citrate salt of fentanyl. Upon intranasal administration of this agent and contact with the nasal mucosa, pectin in low-viscosity aqueous solution gels in the presence of mucosal calcium ions; from this intranasal gel delivery platform, fentanyl is released into the systemic circulation in a relatively rapid but controlled and sustained manner.

Fentanyl matrix transdermal patch A transdermal formulation containing fentanyl. Upon topical administration, fentanyl diffuses from the transdermal patch through the skin and is transported via the systemic circulation to the central nervous system (CNS).

Fentanyl sublingual spray A sublingual preparation of fentanyl. After rapid sublingual transmucosal absorption, the active ingredient fentanyl is transported via the systemic circulation to the central nervous system (CNS).

Adapted from National Cancer Institute. NCI Drug Dictionary. Internet. September 15, 2009.

Published by Roberto Wenk. Last updated date: February 9, 2016.

Adult
Buccal - Breakthrough cancer pain - Patients already receiving and tolerant to opioid treatment.
As loz - Initial: 200 mcg over 15 min per episode; may repeat once after 15 min if needed. Max: 1.6 mg/dose. No more than 4 unit doses should be taken daily.
As tab - Initial: 100 mcg episode; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode.
As film - Initial: 200 mcg per episode; thereafter, at least 2 hr must elapsed before treating another episode.

Sublingual - Breakthrough cancer pain
As tab - Initial: 100 mcg per episode; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode.
As spray - Initially, 100 mcg per episode; may repeat once after 30 min if needed; wait for at least 4 hr before treating another episode.
Nasal - Breakthrough cancer pain. Initial: Spray 50 or 100 mcg into 1 nostril per episode; may repeat once after 10 min; wait for at least 2 or 4 hr before treating another episode. Max: 4 episodes treated daily.

IV
Adjunct to general anaesthesia
Patients w/ spontaneous respiration: Initial: 50-200 mcg followed by supplements of 50 mcg. Max: 200 mcg. Admin lower infusion rates of 0.05-0.08 mcg /kg/min.
Patients w/ assisted ventilation. Initial: 300-3,500 mcg (up to 50 mcg/kg) followed by supplements of 100-200 mcg depending on response. Loading dose (alternatively via bolus): Approx 1 mcg/kg/min given for the 1st 10 min followed by infusion of approx 100 ng/kg/min.

IM
Premedication before anaesthesia: 50-100 mcg to be given 30-60 min prior to induction.

Transdermal. Intractable chronic pain.
Opioid-naive patients. Initial: Apply patch that delivers ≤25 mcg/hr. Adjust dose according to response.
Patients receiving a strong opioid analgesic: Initial dose should be based on the previous 24-hr opioid requirements. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days.

Adverse drug reactions: reduce pulmonary compliance and/or apnoea, bronchoconstriction, laryngospasm; nausea, vomiting; bradycardia, oedema, CNS depression, confusion, dizziness, drowsiness, headache, sedation, hypotension, peripheral vasodilation, increased intracranial pressure, itching, rash, erythema, pruritus, coughing, urinary retention.

CIMS Drug Information System. Internet. Accessed on January 10, 2016.

Fentanyl citrate

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