Fentanyl Citrate

Description

What is fentanyl citrate?

Fentanyl citrate is a potent opioid agonist. A dose of 100 mcg (0.1 mg) (2.0 mL) is approximately equivalent in

analgesic activity to 10 mg of morphine or 75 mg of meperidine. The principal actions of therapeutic value are

analgesia and sedation. Alterations in respiratory rate and alveolar ventilation, associated with opioid analgesics,

may last longer than the analgesic effect. As the dose of fentanyl is increased, the decrease in pulmonary exchange

becomes greater. Large doses may produce apnea. Fentanyl citrate appears to have less emetic activity than either

morphine or meperidine.

Histamine assays and skin wheal testing in man indicate that clinically significant

histamine release rarely occurs with fentanyl. Recent assays in man show no clinically significant histamine release

in dosages up to 50 mcg/kg (0.05 mg/kg) (1 mL/kg). Fentanyl citrate powder preserves cardiac stability, and blunts stress-related

hormonal changes at higher doses.

Fentanyl Citrate Introduction

ChEBI: The citric acid salt of fentanyl, comprising equimolar amounts of citric acid and fentanyl. A mu-opioid receptor agonist, it is a potent opioid analgesic used in the management of labour pain, postoperative pain, and chronic intractable canc r pain. It is also widely used as the analgesic component of balanced anaesthesia.

Fentaz Basic Information

Product Name:	Fentanyl citrate
Synonyms:	fentaz;mcn-jr4263;mcn-jr-4263-49;n-(1-phenethyl-4-piperidinyl)propionanilidedihydrogencitrate;n-(1-phenethyl-4-piperidyl)-propionanilidcitrate(1:1);n-(1-phenethyl-4-piperidyl)propionanilidecitrate;n-(1-phenethyl-4-piperidyl)propionanilidedihydrogencitrate;phentanylcitrate
CAS:	990-73-8
MF:	C28H36N2O8
MW:	528.59
EINECS:	213-588-0
Product Categories:	API; Intermediates & Fine Chemicals; Pharmaceuticals
Mol File:	990-73-8.mol

Phentan Ylcitrate Chemical Structure

Fentanyl citrate

Fentanyl Citrate Chemical Properties

Melting point	153-156°C
Fp	11 °C
storage temp.	2-8°C
solubility	Soluble in water, freely soluble in methanol, sparingly soluble in ethanol (96 per cent).
color	Crystals
CAS DataBase Reference	990-73-8(CAS DataBase Reference)

Fentaz Usage And Synthesis

Chemical Properties	White Powder
Uses	Fentanyl citrate can be used as an analgesic.
Biological Activity	Potent and selective μ -opioid receptor agonist (K i values are 7.0, 151 and 470 nM for μ -, δ – and κ -opioid receptors respectively). Displays antinociceptive activity in vivo .
Clinical Use	A fentanyl citrate patch is available for the treatment of severe chronic pain. This dosage form delivers fentanyl transdermally and provides effective analgesia for periods of up to 72 hours. In 1999, fentanyl also became available in a lollipop dose form for absorption from the oral cavity. Fentanyl’s short duration of action after parenteral dose is caused by redistribution rather than by metabolism or excretion. Repeated doses of fentanyl can result in accumulation and toxicities. Elderly patients usually are more sensitive to fentanyl citrate powder and require lower doses. Opioids have a wide spectrum of P-glycoprotein (P-gp) activity, acting as both substrates and inhibitors, which might contribute to their varying CNS-related effects. Although fentanyl citrate, sufentanil, and alfentanil did not behave as P-gp substrates, they inhibited the in vitro P-gp–mediated efflux of drugs known to be P-gp transported, such as digoxin, increasing their blood levels and the potential for important drug interactions by inhibition of P-gp efflux transporter. Fentanyl citrate powder is utilized to treat advancement torment (abrupt episodes of agony that happen in spite of nonstop therapy with torment medicine) in malignant growth patients no less than 18 years old (or possibly 16 years old assuming utilizing Actiq brand capsules) who are taking routinely planned dosages of another opiate (sedative) torment drug, and who are lenient (used with the impacts of the prescription) to opiate torment meds. Fentanyl is in a class of drugs called opiate (narcotic) analgesics. It works by significantly altering the manner in which the cerebrum and sensory system answer torment.
Safety Profile	Poison by ingestion, subcutaneous, and intravenous routes. When heated to decomposition it emits toxic fumes of NOx. See also PHENTANYL.