naloxone
American Heritage Dictionary:
Top
nal·ox·one
(năl'ək-sōn', nə-lŏk'sōn) 
n.
A drug, C19H21NO4, used as an antagonist to narcotic drugs, such as morphine.
n.
A drug, C19H21NO4, used as an antagonist to narcotic drugs, such as morphine.
[Short for N-allyldihydrohydroxynormorphinone, its chemical name.]
Drug Info:
Top
Naloxone
Brand names: Narcan®
Chemical formula:
Naloxone Hydrochloride Solution for injection
What is this medicine?
NALOXONE (nal OX one) is a narcotic blocker. It is used to treat narcotic drug overdose.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•drug abuse or addiction
•an unusual or allergic reaction to naloxone, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
This medicine is for injection into a muscle, injection under the skin, or infusion into a vein. It is given by a health care professional in a hospital or clinic setting.
Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as newborn for selected conditions, precautions do apply.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•narcotic medicines for pain
•nalbuphine
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Your condition will be monitored carefully while you are receiving this medicine.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•fast, irregular heartbeat
•high blood pressure
•pain that was controlled by narcotic pain medicine
•seizures
•stomach cramps
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•aches and pains
•diarrhea
•fever or chills
•irritable, nervous, restless
•nausea, vomiting
•runny nose
•sweating
•trembling
•weak
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
This drug is given in a hospital or clinic and will not be stored at home.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford Dictionary of Biochemistry:
Top
naloxone
1-N-allyl-7,8-dihydro-14-hydroxynormorphinone; one of the most effective opiate antagonists. It binds tightly to opiate receptors in the nervous system, its action depending on the 3-carbon side-chain substitution on the nitrogen. It is used as an antidote to overdosage of narcotics.
| nalidixic acid, nactin, nRNA | |
| naltrexone, nano+, nanogram |
Saunders Veterinary Dictionary:
Top
naloxone
A narcotic antagonist structurally related to oxymorphone used as the hydrochloride to reverse the effects of previously administered narcotics.
Wikipedia on Answers.com:
Top
Naloxone
Not to be confused with the related chemical naltrexone.
 |
|
|---|---|
 |
|
| Systematic (IUPAC) name | |
| (1S,5R,13R,17S)- 10,17-dihydroxy- 4-(prop-2-en-1-yl)- 12-oxa- 4-azapentacyclo [9.6.1.01,13.05,17.07,18] octadeca- 7(18),8,10-trien- 14-one | |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| Pregnancy cat. | B (USA) B1 (Aus) |
| Legal status | Prescription Only (S4) (AU) |
| Routes | IV, IM |
| Pharmacokinetic data | |
| Bioavailability | 2% (Oral, 90% absorption but high first-pass metabolism) |
| Metabolism | Liver |
| Half-life | 1-1.5 h |
| Excretion | Urine, Biliary |
| Identifiers | |
| CAS number | 465-65-6  |
| ATC code | V03AB15 |
| PubChem | CID 5284596 |
| IUPHAR ligand | 1638 |
| DrugBank | DB01183 |
| ChemSpider | 4447644 |
| UNII | 36B82AMQ7N |
| KEGG | D08249 |
| ChEBI | CHEBI:7459  |
| ChEMBL | CHEMBL80 |
| Synonyms | 17-allyl- 4,5α-epoxy- 3,14-dihydroxymorphinan- 6-one |
| Chemical data | |
| Formula | C19H21NO4 |
| Mol. mass | 327.37 g/mol |
| SMILES | eMolecules & PubChem |
|
|
 (what is this?) (verify) |
|
Naloxone is an opioid antagonist drug developed by Sankyo in the 1960s.[1] Naloxone is a drug used to counter the effects of opiate overdose, for example heroin or morphine overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory system. Naloxone is also experimentally used in the treatment for congenital insensitivity to pain with anhidrosis (CIPA), an extremely rare disorder (1 in 125 million) that renders one unable to feel pain. It is marketed under various trademarks including Narcan, Nalone, and Narcanti, and has sometimes been mistakenly called "naltrexate." It is not to be confused with naltrexone, an opioid receptor antagonist with qualitatively different effects, used for dependence treatment rather than emergency overdose treatment.
|
Contents
|
Pharmacodynamics
Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system. Naloxone is a μ-opioid receptor competitive antagonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- and δ-opioid receptors.
Chemistry
Naloxone is synthesized from thebaine. The chemical structure of naloxone resembles that of oxymorphone, the only difference being the substitution of the N-methyl group with an allyl (prop-2-enyl) group. The name naloxone has been derived from N-allyl and oxymorphone.
Administration
Naloxone is most commonly injected intravenously for fastest action. The drug generally acts within a minute, and its effects may last up to 45 minutes. It can also be administered via intramuscular or subcutaneous injection. Use of a wedge device (nasal atomizer) attached to a syringe to create a mist delivering the drug to the nasal mucosa[2] may also be utilized, although this solution is more likely utilized outside of a clinical facility. Naloxone is used orally along with Oxycontin Controlled Release and it helps in reducing the constipation associated with opioids. Enteral administration of Naloxone blocks opioid action at the intestinal receptor level, but has low systemic bioavailability due to marked hepatic first pass metabolism. [3]
Uses
 |
This section needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (July 2008) |
Counteracting opiate overdose and addiction
Naloxone has been distributed as part of emergency overdose response kits to heroin and other opioid drug users, and this has been shown to reduce rates of fatal overdose. Projects of this type are under way in many US cities, including San Francisco, New Mexico, Philadelphia, New York State, Baltimore, Boston, Los Angeles, Milwaukee, and Chicago.[4][5] CDC estimates that US programs for drug users and their caregivers prescribing take-home doses of naloxone and training on its utilization are estimated to have reversed 10,000 opioid overdose deaths.[6] Healthcare institution-based naloxone prescription programs have also helped reduce rates of opioid overdose in North Carolina, and have been replicated in the US military.[7][8] Nevertheless, scale-up of healthcare-based opioid overdose interventions is limited by providers' insufficient knowledge and negative attitudes towards prescribing take-home naloxone.[9] Programs training police and fire personnel in opioid overdose response using naloxone have also shown promise in the US.[10][11]
Pilot projects were also started in Scotland in 2006 {{(http://www.scotland.gov.uk/Topics/Justice/law/Drugs-Strategy/drugrelateddeaths/NationalNaloxone)}. Also in the UK, in December 2008 the Welsh Assembly Government announced intention to establish demonstration sites for 'take home' Naloxone.[12] While naloxone is still the standard treatment in emergency reversal of opioid overdose, its clinical use in the long-term treatment of opioid addiction is being increasingly superseded by naltrexone. Naltrexone is structurally similar but has a slightly increased affinity for κ-opioid receptors over naloxone, can be administered orally, and has a longer duration of action.
Enteral naloxone has been successfully used in the reduction of gastritis and esophagitis associated with opioid therapy in mechanically-ventilated acute care patients.
The combination oxycodone/naloxone is used for the prophylaxis of opioid-induced constipation in patients requiring strong opioid therapy under the trade name Targin and in the Netherlands under Targinact.[13]
Preventing opioid abuse
Naloxone is used as a secondary chemical in the drug Suboxone. Suboxone and Subutex were created to help opiate-addicted patients detox. Suboxone contains four parts buprenorphine and one part naloxone, while Subutex contains only buprenorphrine. Naloxone was added to Suboxone in an effort to dissuade patients from injecting the tablets, due to naloxones ability to block opioid receptors and send the user into immediate withdrawal. Users with a high tolerance however may still be able to abuse Suboxone via injection given that buprenorphine has a higher affinity for opioid receptors than naloxone. Oral or sublingual administration affects only the gastrointestinal tract, and has the added benefit of helping to reverse constipation and lowered bowel motility caused by chronic medical use, or abuse, of a variety of opioids. Because of possible side effects of naloxone in some patients, chemical detox can begin with Suboxone's sister drug, Subutex, which does not contain naloxone. It is common for Suboxone film to be used in all cases unless pregnancy is a concern.
Depersonalization disorder
A 2001 Russian study has shown that naloxone can be used to treat depersonalization disorder. According to the study: "In three of 14 patients, depersonalization symptoms disappeared entirely and seven patients showed a marked improvement. The therapeutic effect of naloxone provides evidence for the role of the endogenous opioid system in the pathogenesis of depersonalization."[14]
Side-effects
Possible side effects include: change in mood, increased sweating, nausea, nervousness, restlessness, trembling, vomiting, allergic reactions such as rash or swelling, dizziness, fainting, fast or irregular pulse, flushing, headache, heart rhythm changes, seizures, sudden chest pain.[15]
Naloxone has been shown to block the action of pain-lowering endorphins which the body produces naturally. The likely reason for this is that these endorphins operate on the same opioid receptors that Naloxone blocks. Naloxone is capable of blocking a placebo pain-lowering response, both in clinical and experimental pain, if the placebo is administered together with a hidden or blind injection of naloxone.[16] Other studies have found that placebo alone can activate the body's μ-opioid endorphin system, delivering pain relief via the same receptor mechanism as morphine.[17]
Legal status
Patent status
The patent for naloxone has expired. It is available in generic forms.
Prescription status
In the US, naloxone is classified as a prescription medication, though it is not a controlled substance. ,[18] Dispensing the drug by medical professionals (including physicians or other licensed prescribers) at the point of service is subject to rules that vary state to state. [19] Naloxone distribution programs utilize licensed prescribers to distribute the drug, sometimes relying on “standing orders” mechanisms[20][21] to increase scale-up.
Shortage and Pricing
Naloxone has been periodically under FDA shortage designation since 2001 and was recently re-verified as being in shortage due to a manufacturing delay. [22] Twenty-one out of 48 naloxone prescription programs surveyed in 2010 reported they had experienced challenges in obtaining naloxone in the months leading up to the survey, mainly due either to cost increases that outstripped allocated funding or the suppliers’ inability to fill orders.[23] The approximate cost of a 1ml ampoule of naloxone in the United States is estimated to be significantly higher than in most Western countries; on average, the price for naloxone supply has increased precipitously in recent years. [24]
Identification
The CAS number of naloxone is 465-65-6; the anhydrous hydrochloride salt has CAS 357-08-4 and the hydrochloride salt with 2 molecules of water, hydrochloride dihydrate, has CAS 51481-60-8. Nalaxone
See also
References
- ^ US Patent 3254088 - Morphine Derivative
- ^ "Journal of Emergency Nursing". http://www.jenonline.org/article/PIIS0099176704000078/fulltext?browse_volume=30&issue_key=TOC%40%40JOURNALS%40YJENU%400030%400002&issue_preview=no&select1=no&select1=no&vol=#section7.
- ^ (PMID: 10601678 [PubMed - indexed for MEDLINE])
- ^ "OD Prevention Program Locator.". Overdose Prevention Alliance. http://www.overdosepreventionalliance.org/p/od-prevention-program-locator.html. Retrieved 15 May 2012.
- ^ "Community-Based Opioid Overdose Prevention Programs Providing Naloxone — United States, 2010". Centers for Disease Control and Prevention. 2010 Dec. http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6106a1.htm.
- ^ "Community-Based Opioid Overdose Prevention Programs Providing Naloxone — United States, 2010". Centers for Disease Control and Prevention. 2010 Dec. http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6106a1.htm.
- ^ Albert S, Brason FW 2nd, Sanford CK, Dasgupta N, Graham J, Lovette B. (2011 Jun). "Project Lazarus: community-based overdose prevention in rural North Carolina". Pain Medicine. http://www.ncbi.nlm.nih.gov/pubmed/21668761.
- ^ Beletsky L, Burris S, and Kral AH. (2009 Jul). "Closing Death's Door: Action Steps to Facilitate Emergency Opioid Drug Overdose Reversal in the United States". Center for Health Law, Policy and Practice, Temple University School of Law. http://papers.ssrn.com/sol3/papers.cfm?abstract_id=1437163. Retrieved 2012-05-12.
- ^ Beletsky L, Ruthazer R, Macalino GE, Rich JD, Tan L, Burris S. (2007 Jan). "Physicians' knowledge of and willingness to prescribe naloxone to reverse accidental opiate overdose: challenges and opportunities". Journal of Urban Health. http://www.ncbi.nlm.nih.gov/pubmed/17146712.
- ^ Beletsky L, Moroz E.. "The Quincy Police Department: Pioneering Naloxone Among First Responders.". Overdose Prevention Alliance. http://www.overdosepreventionalliance.org/2012/05/quincy-police-department-pioneering.html. Retrieved 15 May 2012.
- ^ Lavoie D. (2012 April). "Naloxone: Drug-Overdose Antidote Is Put In Addicts' Hands". Huffington Post.
- ^ "IHRA 21st International Conference Liverpool, 26th April 2010 - Introducing 'take home' Naloxone in Wales". http://www.ihra.net/files/2010/08/26/Danny_Morris.pdf. Retrieved 9 March 2011.
- ^ Simpson K, et al. (2008 Dec). "Fixed-ratio combination oxycodone/naloxone compared with oxycodone alone for the relief of opioid-induced constipation in moderate-to-severe noncancer pain". Curr Med Res Opin 24 (12): 3503–3512. DOI:10.1185/03007990802584454. PMID 19032132. http://www.informapharmascience.com/doi/abs/10.1185/03007990802584454. Retrieved 2009-04-09.
- ^ Nuller YL, Morozova MG, Kushnir ON, Hamper N (June 2001). "Effect of naloxone therapy on depersonalization: a pilot study". J. Psychopharmacol. (Oxford) 15 (2): 93–5. DOI:10.1177/026988110101500205. PMID 11448093. http://jop.sagepub.com/cgi/pmidlookup?view=long&pmid=11448093.
- ^ http://www.drugs.com/sfx/naloxone-side-effects.html
- ^ Sauro, Marie D; Greenberg, Roger P. (Feb 2005), "Endogenous opiates and the placebo effect: A meta-analytic review", Journal of Psychosomatic Research 58 (2): 115–120, PMID 15820838, http://maccurtain.com/psych/Sadistic%20Ben%20Mark2/Sauro%20and%20greenburg%202004%20endogenous%20opiates%20and%20the%20placebo%20effect.pdf
- ^ http://www.jyi.org/news/nb.php?id=429
- ^ 21 U.S.C.A. §§801-904; see e.g., LA Rev Stat. Ann. §40:964 (specifically excluding Naloxone from the schedule of controlled substances.)
- ^ Burris S, Beletsky L, Castagna CA, Coyle C, Crowe C, McLaughlin JM. (July 2009). "Stopping an Invisible Epidemic: Legal Issues in the Provision of Naloxone to Prevent Opioid Overdose". Center for Health Law, Policy and Practice, Temple University School of Law. PMID 1434381. http://papers.ssrn.com/sol3/papers.cfm?abstract_id=1434381.
- ^ Beletsky L, Burris S, and Kral AH. (2009 Jul). "Closing Death's Door: Action Steps to Facilitate Emergency Opioid Drug Overdose Reversal in the United States". Center for Health Law, Policy and Practice, Temple University School of Law. http://papers.ssrn.com/sol3/papers.cfm?abstract_id=1437163. Retrieved 2012-05-12.
- ^ Burris S, Beletsky L, Castagna CA, Coyle C, Crowe C, McLaughlin JM. (2009 Jul). "Stopping an Invisible Epidemic: Legal Issues in the Provision of Naloxone to Prevent Opioid Overdose". 1 Drexel L. Rev. http://papers.ssrn.com/sol3/papers.cfm?abstract_id=1434381. Retrieved 2012-05-12.
- ^ "Current Drug Shortages, US Food and Drug Administration". http://www.fda.gov/Drugs/DrugSafety/DrugShortages/ucm050792.htm. Retrieved 12 May 2012.
- ^ "Community-Based Opioid Overdose Prevention Programs Providing Naloxone — United States, 2010". Centers for Disease Control and Prevention. 2010 Dec. http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6106a1.htm.
- ^ Beletsky L, Burris S, and Kral AH. (2009 Jul). "Closing Death's Door: Action Steps to Facilitate Emergency Opioid Drug Overdose Reversal in the United States". Center for Health Law, Policy and Practice, Temple University School of Law. http://papers.ssrn.com/sol3/papers.cfm?abstract_id=1437163. Retrieved 2012-05-12.
External links
- Chicago Recovery Alliance's naloxone distribution project
- Report on Naloxone and other opiate antidotes, by the International Programme on Chemical Safety
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
Post a question - any question - to the WikiAnswers community:
Copyrights:
American Heritage Dictionary
The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.
Read more
Oxford Dictionary of Biochemistry
Oxford University Press. Oxford Dictionary of Biochemistry and Molecular Biology © 1997, 2000, 2006 All rights reserved.
Read more
Saunders Veterinary Dictionary
Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.
Read more
