Butorphanol
Butorphanol Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Butorphanol is a brand name. Its generic name is Butorphanol.
Introduction
Butorphanol, also known as Stadol, is an opioid analgesic drug used to treat moderate to severe pain in adults. It is a synthetic opioid derived from thebaine, and is both an agonist and an antagonist of the mu receptor. It can be administered intranasally, intravenously, intramuscularly, and subcutaneously.Uses for
Butorphanol is used as a continuous or on-demand analgesic for the treatment of moderate to severe pain. It is particularly effective in treating neuropathic pain, with fewer side effects than opioids such as morphine. Additionally, it has been used off-label for the control of postoperative nausea and vomiting, and to potentiate the effects of other analgesics.Mechanism of Action
Butorphanol is a mixed opioid agonist-antagonist. It binds to the mu-opioid receptor, providing both analgesic and anti-emetic effects. It also binds to the kappa-opioid receptor, providing analgesic and sedative effects. At low doses, it acts as a partial agonist at the mu-receptor, while at higher doses it acts as an antagonist.How long does it take to work?
The onset of action of butorphanol is rapid, ranging from 15 minutes after intranasal administration to 45 minutes after intravenous administration. The duration of action is approximately 3-4 hours.Absorption
Butorphanol is rapidly and extensively absorbed after intranasal or intravenous administration. Approximately 50% of an intranasal dose is absorbed.Route of Elimination
Butorphanol is metabolized in the liver by cytochrome P450 enzymes, with the primary metabolites being hydroxy-butorphanol and norbutorphanol. These metabolites are then excreted in the urine.Dosage
Butorphanol is available as a 1mg/ml, 2mg/ml, or 10mg/ml solution for intranasal or injected administration. For continuous analgesia, the usual dose range is 0.15-0.3mg every 4-6 hours. For the treatment of postoperative nausea and vomiting, the initial dose is 0.2mg every 12-24 hours.Administration
Butorphanol can be administered intranasally (using the nasal spray pump), intravenously (by bolus injection), intramuscularly, and subcutaneously.Side Effects
Common side effects of butorphanol include nausea, dizziness, drowsiness, headache, and dry mouth. Rare but serious side effects include severe allergic reactions, muscle rigidity, and respiratory depression.Toxicity
In the case of an overdose of butorphanol, the symptoms include respiratory depression, coma, and severe hypotension. Treatment of an overdose should include supportive care and administration of opioid antagonists, such as naloxone.Precaution
Butorphanol should be used with caution in patients with renal or hepatic impairment, respiratory depression, and in pregnant or breastfeeding women. Patients should be monitored for respiratory depression, particularly when starting or increasing doses.Interaction
Butorphanol can interact with other medications, particularly other central nervous system depressants such as alcohol, benzodiazepines, and other opioids.Disease Interaction
Butorphanol can interact with other diseases, including hepatic and renal impairment, and should be used with caution in patients with these conditions.Drug Interaction
Butorphanol can interact with other medications, particularly CNS depressants such as alcohol, benzodiazepines, and other opioids.Food Interactions
Butorphanol can interact with certain foods, including grapefruit, and should be used with caution in patients who have consumed these foods.Pregnancy Use
Butorphanol is not recommended for use during pregnancy, as there is a risk of adverse fetal effects.Lactation Use
Butorphanol is not recommended for use during lactation, as there is a risk of adverse effects in nursing infants.Acute Overdose
In the case of an overdose of butorphanol, the symptoms include respiratory depression, coma, and severe hypotension. Treatment of an overdose should include supportive care and administration of opioid antagonists, such as naloxone.Contraindication
Butorphanol is contraindicated in patients with known hypersensitivity to opioids, and should not be used in patients with respiratory depression or in patients who have taken monoamine oxidase inhibitors within the last 14 days.Use Direction
Butorphanol should be used as directed by the prescribing physician or pharmacist. The dose should be adjusted as necessary to provide adequate pain relief.Storage Condition
Butorphanol should be stored at room temperature, away from heat and light. It should not be stored in the refrigerator or freezer.Volume of Distribution
The volume of distribution of butorphanol is approximately 4L/kg.Half Life
The half life of butorphanol is approximately 4-5 hours.Clearance
The clearance of butorphanol is approximately 4-7mL/min/kg.Here you find in details version of Butorphanol
Some Frequently Asked Questions About Butorphanol
https://www.medicinesfaq.com/brand/butorphanol,
,
,
http://www.genome.jp/dbget-bin/www_bget?drug:D00837,
http://www.genome.jp/dbget-bin/www_bget?cpd:C06863,
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=6916249,
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507553,
https://www.chemspider.com/Chemical-Structure.16735714.html,
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240437,
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=1841,
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3242,
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL33986,
https://zinc.docking.org/substances/ZINC000003812988,
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000214,
http://www.pharmgkb.org/drug/PA164745398,
http://www.rxlist.com/cgi/generic2/butor.htm,
https://www.drugs.com/cdi/butorphanol-solution.html,
https://en.wikipedia.org/wiki/Butorphanol,