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Drug profile of pharmacology ( Naloxone ) - Essay Example

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Naloxone 1. Introduction: Opium, derived from the poppy seeds was used as early as the 3rd century. In the 19th century, morphine, a derivative of opium, was used as a narcotic agent. Opioids bind to the opioid receptors that are present in the central nervous system and peripheral nervous system and produce their therapeutic effects…
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Download file to see previous pages They also reverse the effect of the exogenous and endogenous opioid receptors by creating perceptible of opioid withdrawal in the opioid dependent patients. The common Opioid antagonists are naloxone and nalmefene and naltrexone are competitive antagonists for the opioid receptors. Naloxone is used primarily for the patients suffering from respiratory depression. 2. Naloxone – An introduction: Chemical name: “(-)-17-Allyl-4, 5a-epoxy-3, 14-dihydroxymorphinan-6-one.” (Sinatra, Jahr and Watkins-Pitchford, 2010). Generic Name: Naloxone Trade names: “Naloxone hydrochloride Injection (DBL or CSL brands), Naloxone Min-I-Jet Suboxone (in combination with Buprenorphine), Targin (in combination with oxycodone).” (Sinatra, Jahr and Watkins-Pitchford, 2010). Other Names: “L-Naloxone , N- Allylnoroxymorphone, Nalossone, Naloxona, Naloxone HCl, Naloxonum.” (Sinatra, Jahr and Watkins-Pitchford, 2010). Similar Ligands of Naloxone: Nalmefene, naltrexone, (+) – Naloxone, Naloxonazine, nalbuphine, naltriben and naltrindole, naloxone benzoylhydrazone, TRK820, beta – FNA, etorphine, diprenorphine, buprenorphine, nor-binalto and BNTX .(Sinatra, Jahr and Watkins-Pitchford, 2010). ...
It is mainly used for managing opiate dependence syndrome and respiratory depressions caused by overdose of Opioids. The paramedic indications are: 1. Antinarcotic agents. 2. Narcotic antagonists. 3. Depressants. 4. Opiate Antagonists. 5. Reverse sedations caused by Opioids. 6. Respiratory depressants in neonatal care. 3. Mechanism of Action: Naloxone reverses the effect of the opioid overdose. Naloxone competitively binds to the opioid receptors and replaces the opioid molecules. By doing so, it reverses the effect of the agonists such as heroin. Naloxone is competitive antagonists at the mu, kappa and delta receptors. They have 10 fold greater affinity for the mu receptors. (Harvey and Champe 2008). Naloxone does not have any effect on the normal individuals but they precipitate the withdrawal symptoms at the abuse users. Animal studies have suggested that Naloxone inhibits GABA release and stimulates the cholinergic activity. Similarly they do not reverse the effects of ethanol. Naloxone first increases the local blood flow. (Harvey and Champe 2008). Then the drug crosses the cellular membrane and increases the cellular metabolism. Finally it aids in cell repair. Fig 2: competition of Naloxone with the opioid agonists. (Harvey and Champe 2008). Pharmacology: Naloxone is a pure competitive antagonist for the mu receptors. Mu receptors are responsible for miosis, euphoria, feeding, sedation and respiratory depression. Naloxone binds to the competitive receptors such that their antagonists or partial antagonists or mixed agonist- antagonist binding without any independent action. (Flomenbaum et al. 2006). The pharmacokinetics of naloxone differs from the other antagonists. Some studies have also found that extreme low doses of naloxone (0.25 micrograms per ...Download file to see next pagesRead More
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