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Fentanyl information from DrugsUpdate  

See Available Brands of Fentanyl in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *

Fentanyl, brand names including Actiq, Duragesic, Fentora, Onsolis, Sublimaze and Instanyl is a synthetic primary μ-opioid agonist commonly used to treat chronic breakthrough pain and is commonly used in pre-procedures. It is approximately 100 times more potent than morphine, with 100 micrograms of fentanyl approximately equivalent to 10 mg of morphine and 75 mg of pethidine (meperidine) in analgesic activity.

Pharmacodynamics

Pharmacokinetics

Fentanyl is a potent opioid analgesic that increases pain threshold, alters pain reception and inhibits ascending pain pathways by binding to stereospecific receptors within the CNS. Onset Rapid. Duration Short. Distribution Rapidly into tissues; appears in the CSF, crosses the placenta and small amounts enter the breast milk. Protein-binding: 80% Metabolism Hepatic via N-dealkylation and hydroxylation. Excretion Urine (as metabolites and unchanged drug); 4 hrs (elimination half-life).

Fentanyl Indications / Fentanyl Uses

Information Not Available

Fentanyl Adverse Reactions / Fentanyl Side Effects

Nausea, vomiting; bradycardia, oedema, CNS depression, confusion, dizziness,drowsiness, headache, sedation, transient hypotension, peripheral vasodilation; increased intracranial pressure. High IV dose may cause chest wall rigidity. Transdermal: Rash, erythema and itching. Potentially Fatal: Respiratory depression, trunk rigidity, laryngospasm, bronchoconstriction.

Precautions

Fentanyl transdermal system should not be used to initiate opioid therapy in patients who are not opioid-tolerant. Children converting to Fentanyl transdermal system should be opioid-tolerant and 2 years of age or older. Patients, family members, and caregivers should be instructed to keep patches (new and used) out of the reach of children and others for whom Fentanyl transdermal system was not prescribed. A considerable amount of active Fentanyl remains in Fentanyl transdermal system even after use as directed. Accidental or deliberate application or ingestion by a child or adolescent will cause respiratory depression that could result in death.

Special Precautions

Myasthaenia gravis. Head injury; increased intracranial pressure; intracranial lesions; renal or hepatic impairment; neonates; opioid-nontolerant patients. Increased risk of respiratory depression in elderly, debilitated patients, patient with hypoxia or hypercapnia. Hypothyroidism, prostatic hyperplasia, inflammatory bowel disorders, bradycardia or bradyarrhythmias. Rapid IV infusion may cause skeletal muscle and chest wall rigidity, impaired ventilation or respiratory distress/arrest. Prolonged use may cause tolerance, psychological and physical dependence. Abrupt withdrawal after prolonged admin may lead to withdrawal symptoms. Lactation. Pregnancy (avoid high doses or prolonged usage).

Other Drug Interactions

Depressant effects may be enhanced by other CNS depressants e.g. alcohol, anaesthetics, anxiolytics, hypnotics, TCAs and antipsychotics. Ammonium chloride may increase excretion of fentanyl. Phenothiazines may increase hypotensive effect of opioid analgesics. Serum levels may be increased by CYP3A4 inhibitors (e.g. azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin and verapamil). May reduce the efficacy of pegvisomant. Serum levels may be reduced by rifamycin derivatives. May increase serotonergic effect of SSRIs and sibutramine.

Other Interactions

Food Interactions: Avoid valerian, kava-kava and gotu kola. Serum levels may be reduced by St John's wort.

Dosage

Oral Breakthrough cancer pain Adult: For patients who are already receiving and tolerant to opioid treatment: As a loz: Initially, 200 mcg over 15 minutes for an episode of breakthrough pain; may repeat once after 15 minutes if needed. Titrate subsequent doses based on response up to 1.6 mg per dose. Once the effective dose has been identified, no more than 4 unit doses should be taken daily. Elderly: and debilitated patients: Dose reduction may be needed. Intravenous Adjunct to general anaesthesia Adult: For patients with spontaneous respiration: Initially, 50-200 mcg followed by supplements of 50 mcg. To be injected over 3-5 minutes. Possible increased risk of resp depression following doses >200 mcg. For patients with assisted ventilation: Initially, 300-3,500 mcg (up to 50 mcg/kg) followed by supplements of 100-200 mcg depending on the patient's response. To be injected over 3-5 minutes. Child: For patients with spontaneous respiration: >2 yr: 3-5 mcg/kg IV, supplements of 1 mcg/kg may be given. For patients with assisted ventilation: >2 yr: Initially, 15 mcg/kg with supplements of 1-3 mcg/kg. Elderly: and debilitated patients: Dose reduction may be needed. Intramuscular Premedication before anaesthesia Adult: 50-100 mcg, to be given 30-60 minutes before induction of anaesthesia. Elderly: and debilitated patients: Dose reduction may be needed. Transdermal Intractable chronic pain Adult: Patches deliver fentanyl in doses that range from 12-100 mcg/hr. Doses should be individually titrated based on previous use of opioids. For opioid-naive patients: Initiate with patches that deliver not more than 25 mcg/hr of fentanyl. Recommended for opioid-naive patients to start with low doses of short-acting opioids before starting on fentanyl patches. For patients who have been receiving a strong opioid, the initial dose should be based on the previous 24-hr opioid requirement. During transfer to fentanyl patches, previous opioid treatment should be phased out gradually. If patient requires doses >100 mcg/hr, >1 patch may be used; consider alternative or additional therapy if doses >300 mcg/hr are required. 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. Elderly: and debilitated patients: Dose reduction may be needed. Incompatibility Thiopental sodium and methohexital sodium.

Food(before/after)

Information Not Available

List of Contraindications

Fentanyl and Pregnancy

Caution when used during pregnancy Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. If prolonged use/high doses at term: Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Fentanyl and Lactation

Caution when used during lactation

Fentanyl and Children

Fentanyl transdermal system was not studied in children under 2 years of age. Fentanyl transdermal system should be administered to children only if they are opioid-tolerant and 2 years of age or older. To guard against accidental ingestion by children, use caution when choosing the application site for Fentanyl transdermal system and monitor adhesion of the system closely.

Fentanyl and Geriatic

Data from intravenous studies with Fentanyl suggest that the elderly patients may have reduced clearance and a prolonged half-life. Moreover elderly patients may be more sensitive to the active substance than younger patients. A study conducted with the patch in elderly patients demonstrated that Fentanyl pharmacokinetics did not differ significantly from young adult subjects, although peak serum concentrations tended to be lower and mean half-life values were prolonged to approximately 34 hours. Respiratory depression is the chief hazard in elderly or debilitated patients, usually following large initial doses in non-tolerant patients or when opioids are given in conjunction with other agents that depress respiration. Fentanyl transdermal system should be used with caution in elderly, cachectic, or debilitated patients as they may have altered pharmacokinetics due to poor fat stores, muscle wasting or altered clearance.

Fentanyl and Other Contraindications

Hypersensitivity.

Storage

Intramuscular Store between 20-25 ℃ Intravenous Store between 20-25 ℃ Oral Store between 20-25 ℃ Transdermal Store between 20-25 ℃

Lab interference

Intramuscular Store between 20-25 ℃ Intravenous Store between 20-25 ℃ Oral Store between 20-25 ℃ Transdermal Store between 20-25 ℃

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