Naloxone for overdose

Strang J, Kelleher M, Best D, Mayet S Manning V (2006). Emergency naloxone for heroin overdose. British Medical Journal, 333, 614-5... 

Action on receptors provides numerous examples. Beneficial interactions are sought in overdose, as with the use of naloxone for morphine overdose (opioid receptor), of atropine for anticholinesterase, i.e. insecticide poisoning (acetylcholine receptor), of isoproterelol (isoprenaline) for overdose with a P-adrenoceptor blocker (p-adrenoceptor), of phentolamine for the monoamine oxidase inhibitor-sympathomimetic interaction (a-adrenoceptor). 

Pain-relieving action is not superior to that of codeine Response to naloxone in overdose may be unreliable This drug, which does not activate opioid receptors, has been proposed as a maintenance drug in treatment programs for opioid addicts a single oral dose will block the effects of injected heroin for up to 48 hours (A) Amphetamine Buprenorphine Naloxone Naltrexone Propoxyphene... 

Strang J, Manning V, Mayet S, Best D, Titherington E, Santana L, et al. Overdose training and take-home naloxone for opiate users prospective cohort study of impact on knowledge and attitudes and subsequent management of overdoses. Addiction October 2008 103(10) 1648-57. 

Opiate overdose is a medical emergency that can result in respiratory and CNS depression. The opioid receptor antagonist naloxone immediately reverses cardiorespiratory depression. However, repeated naloxone administration is required, since the effects of naloxone last for 30 min, while opioid agonists can remain at potentially lethal blood levels for several hours. 

This drug is used for complete or partial reversal of narcotic depression, including respiratory depression. Narcotic depression may be due to intentional or accidental overdose (self-administration by an individual), accidental overdose by medical personnel, and drug idiosyncrasy Naloxone also may be used for diagnosis of a suspected acute opioid overdosage. 

Naltrexone (Trexan) is the only opioid antagonist currently in use for treatment of addiction. Naloxone is used to treat opioid overdose and to test for opioid addiction but has a short half-life and is relatively ineffective orally cyclazocine s dysphoric side effects make it unacceptable (Resnick et al. 1980). Patients who are likely to continue to use naltrexone and to benefit from treatment are those who have established careers (e.g., health professionals) and family support and are well motivated. Up to 70% of such clients are abstinent at 1-year follow-up (Washton et al. 1984). Programs that utili2e additional rehabilitative services have better results than those that provide minimal services. Successful treatment is also associated with taking naltrexone... 

The opioid antagonists naloxone and naltrexone bind to aU three opioid receptors, p, K, and 8. These compounds are antagonists due to their inability to elicit downstream effects of these receptors once bound (Sarton et al. 2008 Yaksh and Rudy 1977). Interestingly, both antagonists have a high binding affinity for MORs. Naloxone is used to reverse the effects of an acute opioid overdose because of its rapid onset of action. Naltrexone elicits similar actions, but has a longer onset and duration of action and hence, is used for the maintenance of treatment for opioid addicts. 

Naloxone (Narcan). Naloxone, like naltrexone, is a potent opioid receptor blocker. Its primary use has been to reverse opiate toxicity after an overdose. However, some physicians have found it is also useful for a process known as rapid opiate detoxification. Although opiate withdrawal is not life threatening, it can be extremely unpleasant. Most opiate addicts are fearful of the withdrawal symptoms therefore, it usually requires a slow, deliberate detoxification to keep the withdrawal symptoms in check. Rapid opiate detoxification is an alternative approach that keeps the taper and detoxification as brief as possible. In this approach, naloxone is used in conjunction with general anesthesia or a nonopiate sedative such as the benzodiazepine mid-... 

Only one antagonist is known, naloxone, which is used clinically to treat opiate overdoses and, experimentally, to investigate whether physiological or biochemical actions are opiate-mediated. One example of its use is to support the hypothesis that P-endorphin is responsible for the analgesic effects of acupuncture. Not only does low frequency electroacupuncture increase p-endorphin levels in cerebrospinal fluid but naloxone nullifies the analgesic effect of this treatment. 

Strang, J., Darke, S., Hall, W. Farrell, M. AN, R. (1996). Heroin overdose the case for take-home naloxone. British Medical Journal, 312 1435-1436. http //bmj.bmjjournals.com/cgi/content/full/312/7044/1435 (for full text) Darke, S. Hall, W. (1997). The distribution of naloxone to heroin users. Addiction, 92. 1195-1199.http-//www.blackwell-synergy.com/links/ doi/10.1046/j. 1360-0443.1997.929119520.x/abs/ iot abstract)... 

I hebaine (46) Naloxone (48) Benzyltetrahydro-isoquinoline alkaloid Antidote for opiate overdose... 

It is worth mentioning that iV-allylic substitution in a number of morphine derivatives, as a rule, leads to antagonistic properties. Naloxone is a few times stronger than nalorphine as an antagonist. It blocks opiate receptors. It eliminates central and peripheral action of opioids, including respiratory depression. Naloxone is used upon overdose of narcotic analgesics.Synonyms for this drug are narkan, talwin, and others. 

Adverse effects and drug interactions with codeine are similar to those reported for morphine, although they are less intense. Overdose in children results in the same effects as overdose of morphine, such as respiratory depression, miosis, and coma these symptoms are treated with naloxone administration. 

The most common side effect of pentazocine is sedation resulting from an interaction with the K-receptor. Also observed are sweating, dizziness, psychotomimetic effects, anxiety, nightmares, and headache. Nausea and vomiting are less frequent than with morphine. Respiratory depression and increased heart rate, body temperature, and blood pressure accompany overdose. Naloxone is effective in reducing the respiratory depression but requires the use of higher doses than for morphine overdose. 

Because of its fast onset (minutes), naloxone (Narcan) administered IV is used most frequently for the reversal of opioid overdose. However, it fails to block some side effects of the opioids that are mediated by the ct-receptor, such as hallucinations. The rapid offset of naloxone makes it necessary to administer the drug repeatedly until the opioid agonist has cleared the system to prevent relapse into overdose. The half-life of naloxone in plasma is 1 hour. It is rapidly metabolized via... 

Naloxone is approved for use in neonates to reverse respiratory depression induced by maternal opioid use. In addition, naloxone has been used to improve circulation in patients in shock, an effect related to blockade of endogenous opioids. Other experimental and less well documented uses for naloxone include reversal of coma in alcohol overdose, appetite suppression, and alleviation of dementia from schizophrenia. Side effects of naloxone are minor. 

Overdosing causes stupor and coma. Pulmonary edema occurs, and froth can be seen coming from the nose and mouth. An antidote for an opioid overdose is naloxone (Nar-can ), which can rapidly displace the opioid from the receptor. Overuse of dextromethorphan can induce euphoria, sedation, ataxia, increased awareness, sweating, elevated blood pressure, arrhythmia, hallucinations, and coma. Some of the dextromethorphan effects resemble those of phencyclidine. 

It is inactive orally because of high first pass metabolism in liver. Metabolised by glucuronidation in liver. The main use of naloxone is in the treatment of acute opioid overdose (acute morphine poisoning). It also precipitates withdrawal syndrome when administered to morphine addicts. The constricted pupils of addicts dilate after administration of naloxone. This has been used as a diagnostic tool for opioid addiction. 

The first drug in this class was nalorphine (/V-allylmorphine). Nalorphine is equipotent with morphine but produced severe psychotomimetic activity, which precluded its use as an analgesic. Until the discovery of naloxone it was widely used for its antagonist properties in the treatment of opioid overdose. The dysphoric side effects of some of this class of drugs is thought to be due to binding to the non-opioid a receptor. 

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