Top Gene Interactions
- Metabolism: The liver is the major site of biotransformation. Route of Elimination: Only 1.0% of the dose is excreted as unchanged drug; urinary excretion is the major route of elimination of metabolites. Half Life: 90-111 minutes
- Uses/Sources: For the management of postoperative pain and the maintenance of general anesthesia.
- Health Effects: Medical problems can include congested lungs, liver disease, tetanus, infection of the heart valves, skin abscesses, anemia and pneumonia. Death can occur from overdose.
- Symptoms: Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils.
- Treatment: Intravenous administration of an opioid antagonist such as naloxone should be employed as a specific antidote to manage respiratory depression. The duration of respiratory depression following overdosage with ALFENTA may be longer than the duration of action of the opioid antagonist. Administration of an opioid antagonist should not preclude immediate establishment of a patent airway, administration of oxygen, and assisted or controlled ventilation as indicated for hypoventilation or apnea. If respiratory depression is associated with muscular rigidity, a neuromuscular blocking agent may be required to facilitate assisted or controlled ventilation. Intravenous fluids and vasoactive agents may be required to manage hemodynamic instability. (L1712)
- Route of Exposure: For intravenous injection or infusion only.
Mechanism of Action
|Target Name||Mechanism of Action||References|
|Kappa-type opioid receptor||
Cytochrome P450 3A5
Multidrug resistance protein 1
Mu-type opioid receptor
Alpha-1-acid glycoprotein 1
|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 Interacts with Diseases
|Disease||Inference Score||References/Inference Genes|
|Methemoglobinemia Type IV||6.35||
|Epilepsy, Idiopathic Generalized||5.02||
|Respiratory Distress Syndrome, Adult||4.02||