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Alfentanil
drug data and news
Alfentanil drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Alfentanil | ||
| Brand Names/Synonyms | Alfenta; Alfentanil; Alfentanilum [Inn-Latin]; Alfentanyl; Dea No. 9737; HSDB 6789 | ||
| Indication | For the management of postoperative pain and the maintenance of general anesthesia | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Alfentanil is a synthetic opioid analgesic. Alfentanil 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. Alfentanil 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. Alfentanil 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. Alfentanil'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. | ||
| Alfentanil News (When available) |
EEG During Anesthesia Is Not a Linear Random Process Feb 22, 2006 EEG During Anesthesia Is Not a Linear Random Process Feb 21, 2006 TIVA, Awareness, and the Brice Interview Feb 21, 2006 Routine Inhaled Induction in Adults: A Safe Practice? Jan 29, 2006 The Influence of Gender on Loss of Consciousness with Sevoflurane ... Jul 21, 2005 The Influence of Gender on Loss of Consciousness with Sevoflurane ... Jul 21, 2005 Assessment of the Onset and Persistence of Amnesia during ... Jun 1, 2005 Awake craniotomy has an edge over general anaesthesia May 27, 2005 Electroencephalogram Monitoring During Anesthesia with Propofol ... Apr 20, 2005 The Short-Acting ß 1 -Adrenoceptor Antagonists Esmolol and ... Feb 22, 2005 | ||
| Dosage Forms | SOLUTION, INJECTION | ||
| Drug_Category | Anesthetics; Narcotics; Analgesics; Opiate Agonists; ATC:N01AH02 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Alfentanil: Both the magnitude and duration of central nervous system and cardiovascular effects may be enhanced when ALFENTA is administered in combination with other CNS depressants such as barbiturates, tranquilizers, opioids, or inhalation general anesthetics. Postoperative respiratory depression may be enhanced or prolonged by these agents. In such cases of combined treatment, the dose of one or both agents should be reduced. Limited clinical experience indicates that requirements for volatile inhalation anesthetics are reduced by 30 to 50% for the first sixty (60) minutes following ALFENTA induction The concomitant use of erythromycin with ALFENTA can significantly inhibit ALFENTA clearance and may increase the risk of prolonged or delayed respiratory depression. Cimetidine reduces the clearance of ALFENTA. Therefore smaller ALFENTA doses will be required with prolonged administration and the duration of action of ALFENTA my be extended. Perioperative administration of drugs affecting hepatic blood flow or enzyme function may reduce plasma clearance and prolong recovery. | ||
| Toxicity | Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | N-[1-[2-(4-ethyl-5-oxo-1,4-dihydrotetrazol-1-yl)ethyl]-4-(methoxymethyl)-4-piperidyl]-N-phenyl-propanamide | ||
| Chemical Formula | C21H32N6O3 | ||
| Molecular Weight | 416.517 g/mol | ||
| Smiles String | CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCN3C(=O)N(N=N3)CC)COC | ||
| Melting Point | 140.8 °C | ||
| Water Solubility | 34.6 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 0.006 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | The liver is the major site of biotransformation. | ||
| Half Life | 90-111 minutes | ||
| Protein Binding [%] | 92% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Alfentanil.html http://www.rxlist.com/cgi/generic2/alfent.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00726 | ||
| CAS Registry Number | 71195-58-9 | ||
| KEGG Compound ID | C08005 | ||
| PubChem ID | SID:189496 | ||
| PharmGKB ID | PA448084 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2248181 |
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