Alfentanil: profile and news

EEG During Anesthesia Is Not a Linear Random Process Feb 22, 2006
...rejected with the Hinich test in only 6.2%, 9.1%, and 10.62% of the investigated EEG epochs during general anesthesia with isoflurane/alfentanil (3), Isoflurane ... - Anesthesia & Analgesia (subscription),

EEG During Anesthesia Is Not a Linear Random Process Feb 21, 2006
Jeleazcov C, Fechner J, Schwilden H. Electroencephalogram monitoring during anesthesia with propofol and alfentanil: the impact of second order spectral ... - Anesthesia & Analgesia (subscription),

TIVA, Awareness, and the Brice Interview Feb 21, 2006
Nordstrom O, Englstrom AM, Persson S, Sandin R. Incidence of awareness in total iv anaesthesia based on propofol, alfentanil and neuromuscular blockade. ... - Anesthesia & Analgesia (subscription),

Routine Inhaled Induction in Adults: A Safe Practice? Jan 29, 2006
Bailie R, Christmas L, Price N et al. Effects of temazepam premedication on cognitive recovery following alfentanil-propofol anaesthesia. ... - Anesthesia & Analgesia (subscription),

The Influence of Gender on Loss of Consciousness with Sevoflurane ... Jul 21, 2005
...(8) found, in a multicenter trial, that gender was a highly significant, independent predictor for recovery time using a propofol/alfentanil/nitrous oxide ... - Anesthesia & Analgesia (subscription)

Assessment of the Onset and Persistence of Amnesia during ... Jun 1, 2005
Kearse L, Rosow C, Sebel P, Manberg P. Bispectral analysis measures sedation and memory effects of propofol, midazolam, isoflurane, and alfentanil in healthy ... - AEM (subscription)

Awake craniotomy has an edge over general anaesthesia May 27, 2005
Fentanyl (0.7 mgm/kg and infusion 0.01 mg/kg/min). Sufentanil (0.075 mg/kg and infusion 0.0015 mg/kg/min). Alfentanil (7.5 mg/kg and infusion 0.5 mg/kg/min). ... - Express Healthcare Management,

Electroencephalogram Monitoring During Anesthesia with Propofol ... Apr 20, 2005
In this study, we investigated the proportion of EEG epochs with nontrivial bicoherence during surgical anesthesia with propofol and alfentanil as an indicator ... - Anesthesia & Analgesia (subscription),

The Short-Acting ß 1 -Adrenoceptor Antagonists Esmolol and ... Feb 22, 2005
Bispectral analysis measures sedation and memory effects of propofol, midazolam, isoflurane, and alfentanil in healthy volunteers. ... - Anesthesia & Analgesia (subscription),

Other information

Indication
For the management of postoperative pain and the maintenance of general anesthesia

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.

Drug Category
Anesthetics; Narcotics; Analgesics; Opiate Agonists; ATC:N01AH02

Brand Names/Synonyms
Alfenta; Alfentanil; Alfentanilum [Inn-Latin]; Alfentanyl; Dea No. 9737; HSDB 6789

Dosage Forms
SOLUTION, INJECTION

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.

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

Half Life
90-111 minutes

Drug Type
Approved Drug

# Accession No
APRD00726

CAS Registry Number
71195-58-9