London: “Magic Medicine” Naloxone Can Bring Comatose Heroin Addicts Back To Life ?: UPDATED

16 Apr

A “magic medicine” that can save drugs users’ lives should be rolled out across the UK to stop hundreds of heroin addicts dying unnecessarily, the Government’s drugs advisers have said.

“Magic medicine” can save drug users’ lives Enlarge photo

Professor Les Iversen, the chief drugs adviser, said a single injection of the rescue medicine naloxone can bring heroin addicts who have gone into a coma back to life.

But plans to roll the drug out across the UK are being hampered by laws which say that, as an injectable medicine, it must be prescribed to a particular individual.

The Advisory Council on the Misuse of Drugs is lobbying the regulatory authorities and wants a situation akin to diabetes drugs, where significant others are allowed to administer the drugs if the person who has collapsed is not able to do so, he said.

“If you make a prescription (to) a person, and that person keels over, they’re not in any position to inject themselves,” he said.

“They’re going to have to be injected by someone who’s a friend or a family member who’s been trained in the use of the rescue medication.

“Getting it as widely available as possible is the name of the game.”

Prof Iversen said: “A heroin overdose person could keel over and go into a coma and a single injection of naloxone can bring them back to life again.

“It is really a magic medicine.”

(Editor’s note: WHY BOTHER ?)

UPDATE: INFO:

Naloxone Hydrochloride 0.4 mg/mL Injection, USP 1 mL Carpuject

Description

 Opioid Antagonist
Rx only

Naloxone hydrochloride, an opioid antagonist, is a synthetic congener of oxymorphone. In structure it differs from oxymorphone in that the methyl group on the nitrogen atom is replaced by an allyl group. It is known chemically as 17-allyl-4,5a-epoxy,3-14- dihydroxymorphinan-6-one hydrochloride. It has a molecular weight of 363.84, and the followingstructural formula:

Naloxone hydrochloride occurs as a white to slightly off-white powder, and is soluble in water, in dilute acids, and in strong alkali; slightly soluble in alcohol; practically insoluble in ether and in chloroform. Naloxone hydrochloride injection is available as a sterile solution for intravenous, intramuscular, and subcutaneous administration. Each mL contains 0.4 mg of Naloxone hydrochloride. Each mL contains 8.9 mg of sodium chloride. The pH is adjusted between 3.0 to 6.5 with hydrochloric acid or sodium hydroxide. The air in the cartridges has been displaced by nitrogen gas.

Clinical Pharmacology

Naloxone prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone is an essentially pure opioid antagonist, i.e., it does not possess the “agonistic” or morphine-like properties characteristic of other opioid antagonists. When administered in usual doses in the absence of opioids or agonistic effects of other opioid antagonists, it exhibits essentially no pharmacologic activity. Naloxone has not been shown to produce tolerance or cause physical or psychological dependence. In the presence of physical dependence on opioids, Naloxone will produce withdrawal symptoms. However, in the presence of opioid dependence, withdrawal symptoms will appear within minutes of Naloxone administration and will subside in about 2 hours. The severity and duration of the withdrawal syndrome are related to the dose of Naloxone and to the degree and type of dependence. While the mechanism of action of Naloxone is not fully understood, in vitro evidence suggests that Naloxone antagonizes opioid effects by competing for the mu, kappa, and sigma opiate receptor sites in the CNS, with the greatest affinity for the mu receptor. When Naloxone hydrochloride is administered intravenously (I.V.), the onset of action is generally apparent within two minutes; the onset of action is slightly less rapid when it is administered subcutaneously (S.C.) or intramuscularly (I.M.). The duration of action is dependent upon the dose and route of administration of Naloxone hydrochloride. Intramuscular administration produces a more prolonged effect than intravenous administration. Since the duration of action of Naloxone may be shorter than that of some opiates, the effects of the opiate may return as the effects of Naloxone dissipate. The requirement for repeat doses of Naloxone will also be dependent upon the amount, type and route of administration of the opioid being antagonized.

Adjunctive Use in Septic Shock
Naloxone has been shown in some cases of septic shock to produce a rise in blood pressure that may last up to several hours; however this pressor response has not been demonstrated to improve patient survival. In some studies, treatment with Naloxone in the setting of septic shock has been associated with adverse effects, including agitation, nausea and vomiting, pulmonary edema, hypotension, cardiac arrhythmias, and seizures. The decision to use Naloxone in septic shock should be exercised with caution, particularly in patients who may have underlying pain or have previously received opioid therapy and may have developed opioid tolerance. Because of the limited number of patients who have been treated, optimal dosage and treatment regimens have not been established.

Pharmacokinetics

Distribution
Following parenteral administration, Naloxone is rapidly distributed in the body and readily crosses the placenta. Plasma protein binding occurs but is relatively weak. Plasma albumin is the major binding constituent but significant binding of Naloxone also occurs to plasma constituents other than albumin. It is not known whether Naloxone is excreted into human milk.

Metabolism and Elimination
Naloxone is metabolized in the liver primarily by glucuronide conjugation with Naloxone-3-glucuronide as the major metabolite. In one study, the serum half-life in adults ranged from 30 to 81 minutes (mean 64 ± 12 minutes). In a neonatal study, the mean plasma half-life was observed to be 3.1 ± 0.5 hours. After an oral or intravenous dose, about 25-40% of the drug is excreted as metabolites in urine within 6 hours, about 50% in 24 hours, and 60-70% in 72 hours.

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