Naloxone chemical structure
Find information on thousands of medical conditions and prescription drugs.

Narcan

Naloxone is a drug used to counter the effects of overdosing on opioids such as heroin and morphine. Specifically, naloxone is used in opioid overdoses for countering life-threatening depression of the central nervous system and respiratory system. It is marketed under trade names including Narcan, Nalone, and Narcanti. more...

Home
Diseases
Medicines
A
B
C
D
E
F
G
H
I
J
K
L
M
N
Nabilone
Nadolol
Nafarelin
Nafcillin
Nalbuphine
Nalidixic acid
Nallpen
Naloxone
Naltrexone
Nandrolone
Naphazoline
Naprelan
Naprosyn
Naproxen
Naratriptan
Narcan
Nardil
Naropin
Nasacort
Nasalcrom
Nascobal
Natamycin
Navane
Navelbine
Nebcin
Nebracetam
Nefazodone
Nefiracetam
Nelfinavir
Nembutal
Neoarsphenamine
Neomycin
Neoral
Neosporin
Neulasta
Neupogen
Neurontin
Nevirapine
Nexium
Nialamide
Niaspan
Niclosamide
Nicoderm
Nicorette
Nicotinamide
Nicotine
Nicotinic acid
Nicotrol
Nifedipine
Nifehexal
Nikethamide
Nilstat
Nilutamide
Nimesulide
Nimodipine
Nimotop
Nitrazepam
Nitrofurantoin
Nix
Nizatidine
Nizoral
Nocodazole
Nolvadex
Nomifensine
Norco
Nordazepam
Nordette
Norepinephrine
Norethin
Norfloxacin
Norgestimate
Norgestrel
Norinyl
Noritate
Normodyne
Norplant
Norpramin
Nortriptyline
Norvasc
Norvir
Noscapine
Novafed
Novobiocin
Novocain
Novrad
Nuprin
Nysert
Nystaform
Nystatin
Nystex
Nystop
O
P
Q
R
S
T
U
V
W
X
Y
Z

The drug is derived from thebaine and has an extremely high affinity for μ-opioid receptors in the central nervous system. Naltrexone can be described as a substituted oxymorphone—here the tertiary amine methyl substituent is replaced with but-2-enyl. 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.

Naloxone is injected, usually initially intravenously for fastest action. The drug acts after about two minutes, and its effects may last about 45 minutes. Naloxone has been distributed as part of emergency kits to heroin users, and has been shown to reduce rates of fatal overdose.

The drug also blocks 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. In one experiment, women treated with naloxone reported higher pain levels during childbirth than women not so treated; in another experiment, the pain lowering effect of placebos was blocked if the placebos were administered along with naloxone.

While naloxone is still often used in emergency treatments for 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.

The patent for Naloxone has expired and it is manufactured by various companies. 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 has CAS 51481-60-8.

Naloxone has sometimes been mistakenly called "naltrexate."

Enteral naloxone has been successfully used in the reduction of gastritis and oesophagitis associated with opioid therapy in mechanically-ventilated acute care patients. (Meissner et al., 2004)

Read more at Wikipedia.org


[List your site here Free!]


What's behind runner's high? Is it endorphins, adrenaline or simply a sense of accomplishment? Here, we explain the chemical link between exercise and
From Shape, 2/1/05 by Gwenda Blair

Why do people feel good after they exercise? Thirty years ago, scientists thought they'd come up with the answer: endorphins, hormones that the body produces during exercise that have opiate, or morphinelike, properties. This explanation for what's known as "runner's high"--the euphoric feeling some people get from exercise--soon became the stuff of sports legend. But just how these natural chemicals affect us--and what other body systems might be at play-is an ongoing debate. Here, we sort through the latest theories.

The big breakthrough

Endorphins were discovered when researchers looked into a well-known phenomenon--our ability to get intoxicated from morphine and heroin. They reasoned that we evolved this capacity not to get high from these synthetic drugs but to benefit from endogenous compounds--that is, substances our bodies produce naturally. In the mid-1970s, scientists identified several such opiatelike chemicals that act as messengers throughout the body. Combining the words endogenous and morphine, they coined a new word, endorphin.

Some 25,000 studies later, researchers have yet to figure out whether the increases in endorphin levels in the bloodstream produced by exercise have any impact on endorphin levels in the brain, which would be necessary to improve mood. Because of their particular chemical makeup, synthetic opiates like morphine and heroin can enter the bloodstream and pass through the blood-brain barrier, the semipermeable tissue that protects the brain from potential toxins. By contrast, endorphins in the bloodstream cannot penetrate this barrier, which throws their role in any true runner's high into question.

Defining runner's high

The notion of runner's high itself has its critics, in part because what any one person means by "high" is impossible to quantify. Although some people feel euphoric after their daily workout, others find the experience gratifying but hardly exhilarating. People who feel especially good may simply be releasing more endorphins; on the other hand, their state of bliss could also be related to improved body image, a sense of accomplishment and a host of other factors ranging from an enhanced immune system to oxygen deprivation.

Most likely, credit for the feel-good effect--reportedly prompted not just by running, but by cycling, tennis and nearly any other intense cardio exercise--has to do with a number of body chemicals and systems that constantly interact. For example, feeling a rush points to the involvement of the hormone adrenaline, says Murali Doraiswamy, M.D., chief of the biological psychiatry division at Duke University School of Medicine in Durham, N.C. "Adrenaline evolved as part of our fight-or-flight response to stress, and it's what gives us that geared-up feeling."

The satisfaction associated with exercise probably also involves dopamine. This chemical messenger turns on the brain's reward system and makes people want to repeat enjoyable experiences, everything from munching chocolate or having sex to running, drinking or using illicit drugs.

Exercise and addiction

Regardless of exactly which neurotransmitters are involved in runner's high, perhaps the more important question is whether the need for a buzz can cause dependency. Traditionally the measure of addiction to any substance has been whether withdrawal from it makes you physically sick, but some researchers now think that the true test is how it affects you mentally and emotionally.

"You might not actually be physically ill if you don't run," says George Koob, Ph.D., a professor in the Department of Neuropharmacology at The Scripps Research Institute in La Jolla, Calif. "But if you feel miserable when you're not running even though you're damaging your body and wrecking your work and personal life [by doing so], you've crossed the line into addiction."

If your level of exercise is wreaking havoc on your life, clearly it's time to cut back and perhaps to seek counseling. But it seems unlikely that most of us need to worry about such a fate, if only because for most people exercise simply doesn't produce enough opiatelike substances to be dangerous or, apparently, to make us feel stoned. For this large majority, the high of exercise doesn't come from doing it, but from the feelings generated by health and fitness benefits that occur afterward. "If exercise was truly addicting, no one would put it off," says Duke's Doraiswamy. "Gym wait lists would be longer than those at the hottest restaurants, and doctors would go out of business from lack of patients. Everyone would be rail-thin."

RELATED ARTICLE: Don't feel like going for a jog? Other endorphin producers.

Although endorphins were "discovered" 30 years ago, scientists are still puzzling out which foods and activities stimulate the release of these naturally produced feel-good chemicals, also known as endogenous opioids. Here's an update:

Working with animals, some researchers have found several intriguing connections to touch, sex and play, according to Jaak Panksepp, M.D., Ph.D., head of affective neuroscience at Northwestern University's Falk Center for Molecular Therapeutics in Evanston, Ill. He reports endogenous opioid levels rose in monkeys during rough-and-tumble play. Also, rats conditioned to associate a certain physical location with sex lost their apparent preference for that place after being given naloxone (Narcan), a drug that blocks the release of endorphins.

Steven Feldman, M.D., Ph.D., a dermatology professor at Wake Forest University Baptist Medical Center in Winston-Salem, N.C., has proposed a new candidate for endorphin stimulation: ultraviolet (UV) exposure. His recent study in the Journal of the American Academy of Dermatology links the popularity of sunbathing and tanning studios to the soothing feeling people experience when UV rays hit their skin, likely spiking endorphin levels.--G.B.

Gwenda Blair, a freelance science writer in New York City, enjoys the effects of running more than actually doing it.

COPYRIGHT 2005 Weider Publications
COPYRIGHT 2005 Gale Group

Return to Narcan
Home Contact Resources Exchange Links ebay