Drug profile of pharmacology ( Naloxone ) Essay

Drug profile of pharmacology ( naloxone ) - establish ExampleThey also reverse the cause 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 worthless 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 name 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). quasi(prenominal) Ligands of Naloxone Nalmef ene, 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 paramedical 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 ca-ca 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 showtime 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 overtone 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