Active ingredient: Sufentanil - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anesthetics, Intravenous
• Narcotics
• Adjuvants, Anesthesia
• Analgesics, Opioid
• Opiate Agonists

Dosage Forms

• Liquid
• Solution

Brands / Synonyms

Chronogesic; Dea No. 9740; Sufenta; Sufentanil Base; Sufentanil Citrate; Sufentanil [Usan:Ban:Inn]; Sufentanilum [Inn-Latin]; Sufentanyl; Sulfentanil Citrate

Indications

Used as an analgesic adjunct in anesthesia and as a primary anesthetic drug in procedures requiring assisted ventilation and in the relief of pain.

Pharmacology

Sufentanil is a synthetic opioid analgesic. Sufentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Sufentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Sufentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.

Mechanism of Action

Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Sufentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.

Absorption

Not Available

Toxicity

LD₅₀: 18.7 mg/kg (IV in mice)

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

Contraindicated in the following: abdominal problems, brain tumor, head injury, gallbladder disease, heart disease, kidney disease, liver disease, lung disease, prostate disease, thyroid disease, and urinary tract disease. Narcotic analgesics may make these conditions or the symptoms of these conditions worse.

Drug Interactions

May interact with the following: any other medicine, prescription or nonprescription (over-the-counter [OTC]), or street drugs, such as amphetamines, barbiturates, cocaine, marijuana, phencyclidine, and heroin or other narcotics (serious side effects may occur if anyone gives you an anesthetic without knowing that you have taken another medicine), benzodiazepines, central nervous system (CNS) depressants (the CNS depressant and other effects of either these medicines or the narcotic analgesics may be increased), buprenorphine or similar medicines (the narcotic analgesics may not work if you are taking buprenorphine or other similar medicines), cimetidine, erythromycin (increased chance of side effects with some narcotic analgesics), and naltrexone (the narcotic analgesics will not work if you are taking naltrexone).