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'''Clonidine''' (also known by the trade names '''Catapres''', '''Kapvay''', '''Nexiclon''', '''Clophelin''', and others) is a medication used to treat [[increased blood pressure|high blood pressure]], attention deficit hyperactivity disorder, [[anxiety]] disorders, tic disorders, [[drug withdrawal|substance withdrawal]] (from either [[alcohol]], [[opioids]], or smoking tobacco), migraine, menopausal flushing, [[diarrhea]], and certain pain conditions.<ref>Brayfield, A, ed. (13 January 2014). "Clonidine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 28 June 2014.</ref> It is classified as a centrally acting α2 [[adrenergic]] [[agonist]] and imidazoline [[receptor]] [[agonist]]. It has been in clinical use for over 40 years.<ref>Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management.". Current Clinical Pharmacology. 6 (4): 280–7. PMID 21827389.</ref>
'''Clonidine''' (also known by the trade names '''Catapres''', '''Kapvay''', '''Nexiclon''', '''Clophelin''', and others) is a medication used to treat [[increased blood pressure|high blood pressure]], attention deficit hyperactivity disorder, [[anxiety]] disorders, tic disorders, [[drug withdrawal|drug withdrawal]] (from either [[alcohol]], [[opioids]], or smoking tobacco), migraine, menopausal flushing, [[diarrhea]], and certain pain conditions.<ref>Brayfield, A, ed. (13 January 2014). "Clonidine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 28 June 2014.</ref> It is classified as a centrally acting α2 [[adrenergic]] [[agonist]] and imidazoline [[receptor]] [[agonist]]. It has been in clinical use for over 40 years.<ref>Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management.". Current Clinical Pharmacology. 6 (4): 280–7. PMID 21827389.</ref>
==Chemistry==
==Chemistry==
Revision as of 22:48, 16 July 2017
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Template:SubstanceBox/clonidineClonidine (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, drug withdrawal (from either alcohol, opioids, or smoking tobacco), migraine, menopausal flushing, diarrhea, and certain pain conditions.[1] It is classified as a centrally acting α2 adrenergicagonist and imidazoline receptoragonist. It has been in clinical use for over 40 years.[2]
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.
Binding affinities:
Clonidine shows agonism at the following receptors, namely the alpha (α) receptors. It lowers blood pressure by stimulating the α2 receptors in the brain.[citation needed]
α1A receptor: 316.23 nM
α1B receptor: 316.23 nM
α1D receptor: 125.89 nM
α2A receptor: 42.92 nM
α2B receptor: 106.31 nM
α2C receptor: 233.1 nM
Clonidine also binds to the Imidazoline I1 receptor as an agonist.
Some studies suggest that clonidine in low doses can boost growth hormone levels.[3]
''Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.''
Physical effects
Sedation - Clonidine can be strong in its sedating effect. This can lead to atypical walking gait from decreased locomotion coordination.
Decreased blood pressure - Clonidine's sympatholytic effects lower blood pressure and is commonly used to treat hypertension.[4]
Abnormal heartbeat - Clonidine's chance of causing this is relatively low, but caution should be taken if clonidine is taken with other drugs that can cause this. Intense physical activity should be avoided.
Raynaud's Phenomenon - Raynaud's Phenomenon occurs when the spasm of arteries results in reduced flood flow to the extremities, causing a pale tone, tingling, and numbness.
Auditory suppression - According to anecdotal reports, this effect is likely due to very low blood pressure. It has been described as a "hollow" type distortion or loss of hearing.
It is strongly recommended that one use harm reduction practices when using this drug, especially concurrently with other depressants. According to drugs.com, clonidine's maximum medical dose for hypotension is 2.4 miligrams in divided doses.
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.
There are studies that show naloxone may be a useful antidote in treating clonidine overdoses. However, this is not in widespread clinical use.[6]
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 and may be dangerous due to concurrent use of depressants.
Dangerous interactions
Warning:Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
↑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.
↑Effect of clonidine on growth hormone, prolactin, luteinizing hormone, follicle-stimulating hormone, and thyroid-stimulating hormone in the serum of normal men. (1990). Lal S, Tolis G, Martin SB, Brown GM, Guyda H. https://www.ncbi.nlm.nih.gov/pubmed/1184719
↑Mitchell A, Bührmann S, Opazo Saez A, Rushentsova U, Schäfers RF, Philipp T, et al. Clonidine lowers blood pressure by reducing vascular resistance and cardiac output in young, healthy males. Cardiovasc Drugs Ther 2005;19:49–55. pmid:15883756
↑Hoehn-Saric R, Merchant AF, Keyser ML, Smith NVK. Effects of Clonidine on Anxiety Disorders. Arch Gen Psychiatry.
↑ Reversal of clonidine toxicity by naloxone. Niemann, James T et al. Annals of Emergency Medicine, Volume 15, Issue 10, 1229 - 1231
↑Koski, A., Ojanperä, I., & Vuori, E. (2002). Alcohol and benzodiazepines in fatal poisonings. Alcoholism: Clinical and Experimental Research, 26(7), 956-959.
