Alfentanyl
Alfentanyl Uses, Dosage, Side Effects, Food Interaction and all others data.
A short-acting opioid anesthetic and analgesic derivative of fentanyl. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanyl is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.
Alfentanyl is a synthetic opioid analgesic. Alfentanyl 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, alfentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Alfentanyl 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. Alfentanyl depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
| Trade Name | Alfentanyl |
| Availability | Prescription only |
| Generic | Alfentanil |
| Alfentanil Other Names | Alfentanil, Alfentanilo, Alfentanilum, Alfentanyl |
| Related Drugs | Buprenex, aspirin, acetaminophen, tramadol, naproxen, Tylenol, oxycodone, fentanyl, lidocaine, ketamine |
| Type | |
| Formula | C21H32N6O3 |
| Weight | Average: 416.5172 Monoisotopic: 416.25358892 |
| Protein binding | 92% |
| Groups | Approved, Illicit |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alfentanyl is an opioid agonist used to induce and maintain anesthesia, as well as an analgesic.
For the management of postoperative pain and the maintenance of general anesthesia.
Alfentanyl is also used to associated treatment for these conditions: General Anesthesia, Induction of anesthesia therapy, Maintenance of anesthesia therapy, Monitored anesthesia care sedation, Perioperative analgesia
How Alfentanyl works
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. Alfentanyl's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Toxicity
Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils.
Food Interaction
No interactions found.Alfentanyl Alcohol interaction
[Moderate] GENERALLY AVOID:
Ethanol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics.
Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.
In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.
Concomitant use of opioid analgesics with ethanol should be avoided.
Alfentanyl Drug Interaction
Moderate: meperidine, meperidine, hydromorphone, hydromorphone, metoprolol, metoprololUnknown: epinephrine, epinephrine, amoxicillin, amoxicillin, multivitamin, multivitamin, calcium / vitamin d, calcium / vitamin d, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, prednisone, prednisone, acetaminophen, acetaminophen
Volume of Distribution
- 0.4 to 1 L/kg
Elimination Route
For intravenous injection or infusion only.
Half Life
90-111 minutes
Clearance
- 5 mL/kg/min
Elimination Route
Only 1.0% of the dose is excreted as unchanged drug; urinary excretion is the major route of elimination of metabolites.
Innovators Monograph
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