Clonidine
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Template:SubstanceBox/clonidine Clonidine (also known by the trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions.[1] It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist. It has been in clinical use for over 40 years.[2]
Chemistry
Clonidine is an imdiazoline compound, meaning that its main chemistry is of an imidazole ring. A nitrogen bonded to the imidazole and chlorinated phenyl group makes an amine.
Pharmacology
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Binding affinities:
- Alpha 1A receptor: 316.23 nM
- Alpha 1B receptor: 316.23 nM
- Alpha 1D receptor: 125.89 nM
- Alpha 2A receptor: 42.92 nM
- Alpha 2B receptor: 106.31 nM
- Alpha 2C receptor: 233.1 nM
Subjective effects
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Toxicity and harm potential
It is strongly recommended that one use harm reduction practices when using this drug, especially concurrently with other depressants.
Lethal dosage
According to dailymed.nlm.nih.gov's prescribing information page for clonidine, clonidine's oral LD50 in mice is 206 mg/kg and for rats, 465 mg/kg. Of course, this does not mean one will not die with levels below these. The treatment for clonidine overdose is naloxone.
Tolerance and addiction potential
Clonidine seems to be able to cause addiction and can be tolerated over periods of time. It is used concurrently with prescription pain-killers (opioids) recreationally because it might have potentiating effects, but this has not been studied.
Legal issues
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United States: In the US, clonidine is only available through prescription.
See also
References
- ↑ Brayfield, A, ed. (13 January 2014). "Clonidine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 28 June 2014.
- ↑ Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management.". Current Clinical Pharmacology. 6 (4): 280–7. PMID 21827389.
https://pubchem.ncbi.nlm.nih.gov/compound/clonidine#section=Names-and-Identifiers http://onlinelibrary.wiley.com/doi/10.1002/ddr.430020207/full
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