Everything about Noscapine totally explained
Noscapine (also known as
Narcotine or
Anarcotine) is an
alkaloid opioid agonist from plants of the
Papaveraceae family, without significant
painkilling properties. It is grouped as part of the
benzylisoquinolines, of which
papaverine is also included. This agent is primarily used for its
antitussive (cough-suppressing) effects. It has also been shown to have anticancer activity (
PDF file
).
Structure analysis
Naturally it occurs as alpha enantiomer. It can be converted in the beta enantiomer when it's dissolved in alkaline water-ethanol solvutions.
The lacton ring is unstable and it opens in basic media. The oposit reaction is presented in acidic media.
The bond C1-C3' is unstable also. This is the bond connecting the two optical active carbon atoms. In water solution of sulphuric acid and heating it dissociats into Cortarnin (4-methoxy-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinoline) and Opic acid (6-formyl-2,3-dimethoxybenzoic acid). When Noscapine is reduced with Zn/HCl the bond C1-C3' saturates and the molecule dissociates into Hydrocortarin (2-hydroxycortarin) and Merconine (6,7-dimethoxyisobenzofuran-1(3H)-one).
Mechanism of action
Noscapine's antitussive effects appear to be primarily mediated by its
sigma receptor agonist activity. Evidence for this mechanism is suggested by experimental evidence in rats. Pretreatment with
rimcazole, a sigma specific
antagonist, causes a dose-dependent reduction in antitussive activity of noscapine.
Cancer and stroke treatment
Noscapine is currently under investigation for use in the treatment of several
cancers and hypoxic
ischemia in
stroke patients. In cancer treatment, noscapine appears to interfere with
microtubule function, and thus the division of cancer cells in a way similar to the
taxanes. Early studies in treatment of
prostate cancer are very promising.
In stroke patients, noscapine blocks the
bradykinine b-2 receptors. A 2003 study in Iran showed a dramatic decrease in mortality in patients treated with noscapine.
Studies are currently underway to assess the effectiveness of this drug in cancer and stroke treatment. Noscapine is non-addictive, widely available, has a low
side-effect incidence, and is easily administered orally, thus it has great potential for use, especially in developing countries.
Noscapine Abuse
Noscapine (Nospen) has a history of
Over-the-counter drug abuse in a several countries being readily available from local pharmacies as a prescription drug.
The effects, beginning around 45 to 120 mins after consumption, are similar to
dextromethorphan and
alcohol intoxication. Abuse of noscapine and other cough suppressants (
dextromethorphan,
codeine,
antihistamines, and
xylometazoline nasal drops) has been reported to cause chronic cough lasting over one month upon withdrawal. Unlike dextromethorphan, noscapine isn't an
NMDA receptor antagonist.
Noscapine in Heroin
Noscapine can survive the manufacturing processes of
heroin and can be found in street heroin. This is useful for law enforcement agencies, as the amounts of contaminants can identify the source of seized drugs. In 2005 in Liege,
Belgium, the average noscapine concentration was around 8%.
Noscapine has also been used to identify drug users who are taking street heroin at the same time as prescribed
diamorphine. Since the diamorphine in street heroin is the same as the pharmaceutical diamorphine, examination of the contaminants is the only way to test whether street heroin has been used. Other contaminants used in
urine samples alongside noscapine include
papaverine and
acetylcodeine. Noscapine is metabolised by the body, and is itself rarely found in urine, instead being present as the primary metabolites,
cotarnine and
meconine. Detection is performed by
gas chromatography-mass spectrometry or Liquid Chromatography-Mass Spectrometry (LCMS) but can also use a variety of other analytical techniques.
Possible side-effects
The effects shown above are not permanent, the user may experience spasms the following day after yawning. It is possible to over dose (20+ pills) and avoid taking any other drug in combination to this medication.
WARNING: Do not take noscapine with any
MAOIs (monoamine oxidase inhibitors), unknown and potentially fatal effects may occur. There are no significant contraindications listed for this drug but caution should be exercised.
Further Information
Get more info on 'Noscapine'.
|
External Link Exchanges
Do you know how hard it is to get a link from a large encyclopaedia? Well we're different and will prove it. To get a link from us just add the following HTML to your site on a relevant page:
<a href="http://noscapine.totallyexplained.com">Noscapine Totally Explained</a>
Then simply click through this link from your web page. Our crawlers will verify your link, extract the title of your web page and instantly add a link back to it. If you like you can remove the words Totally Explained and embed the link in article text.
As long as your link remains in place, we'll keep our link to you right here. Please play fair - our crawlers are watching. Your site must be closely related to this one's topic. Any kind of spamming, dubious practises or removing the link will result in your link from us being dropped and, potentially, your whole site being banned. |
