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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.
Clonidine is an imdiazoline compound, meaning that its main chemistry is of an imidazole ring.
==Pharmacology==
==Pharmacology==
{{pharmacology}}
{{pharmacology}}
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Some studies suggest that clonidine in low doses can boost growth hormone levels.<ref>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</ref>
Some studies suggest that clonidine in low doses can boost growth hormone levels.<ref>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</ref>
Although clonidine overdoses may be reversed by naloxone{{citation needed}} (a controversional claim) as well as clonidine being noted to cause constipation<ref>Boehringer Ingelheim. Catapres (clonidine hydrochloride) tablets prescribing information (2009) https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/017407s034lbl.pdf</ref>, it causes very little to almost no respiratory depression.<ref>Bailey, P. L., Sperry, R. J., Johnson, G. K., Eldredge, S. J., East, K. A., East, T. D., ... & Stanley, T. H. (1991). Respiratory effects of clonidine alone and combined with morphine, in humans. Anesthesiology, 74(1), 43-48.</ref>
Although clonidine overdoses may be reversed by naloxone{{citation needed}} (a controversial claim) as well as clonidine being noted to cause constipation<ref>Boehringer Ingelheim. Catapres (clonidine hydrochloride) tablets prescribing information (2009) https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/017407s034lbl.pdf</ref>, it causes no respiratory depression.<ref>Bailey, P. L., Sperry, R. J., Johnson, G. K., Eldredge, S. J., East, K. A., East, T. D., ... & Stanley, T. H. (1991). Respiratory effects of clonidine alone and combined with morphine, in humans. Anesthesiology, 74(1), 43-48.</ref>
==Subjective effects==
==Subjective effects==
{{EffectStub}}
{{EffectStub}}
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|{{effects/physical|
|{{effects/physical|
*'''[[Effect::Sedation]]''' - Clonidine can be strong in its sedating effect.
*'''[[Effect::Sedation]]''' - Clonidine can be strong in its sedating effect, about equivalent to benzodiazepines. Users can be very tired and can sleep through or ignore prompts to wake up.
** This can lead to atypical walking gait from decreased locomotion coordination. The effect can manifest itself with users tripping over their feet, falling, or passing out (mainly from very low blood pressure).
*'''[[Effect::Decreased heart rate]]'''
*'''[[Effect::Decreased heart rate]]'''
*'''[[Effect::Decreased blood pressure]]''' - Clonidine's sympatholytic effects lower blood pressure and therefore, it is commonly used to treat hypertension.<ref>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</ref>
*'''[[Effect::Decreased blood pressure]]''' - Clonidine's sympatholytic effects lower blood pressure quickly and effectively and therefore, it is commonly used to treat hypertension.<ref>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</ref>
*'''[[Effect::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.
*'''[[Effect::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.
*'''[[Effect::Dry mouth]]'''
*'''[[Effect::Dry mouth]]'''
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*'''Decreased blood pressure upon standing''' - This effect may be overwhelming at higher doses and can be described as a "head rush" or feeling of lightheadedness.
*'''Decreased blood pressure upon standing''' - This effect may be overwhelming at higher doses and can be described as a "head rush" or feeling of lightheadedness.
*'''[[Effect::Physical fatigue]]''' - This general feeling of decreased movement and tiredness is from sedation.
*'''[[Effect::Physical fatigue]]''' - This general feeling of decreased movement and tiredness is from sedation.
*'''[[Effect::Dizziness]]''' - Clonidine can lead to an increased chance of falls due to this. This effect gets stronger with the dose increasing.
*'''[[Effect::Dizziness]]''' - Clonidine can lead to an increased chance of falls due to this. This effect gets stronger with dose increase.
*'''Skin reactions''' - This can happen if clonidine is given in a patch, such as in Catapres-TTS.
*'''Skin reactions''' - This can happen if clonidine is given in a patch, such as in Catapres-TTS.
*'''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, coldness, and numbness.
*'''Raynaud's Phenomenon''' - Raynaud's Phenomenon occurs when the spasm of arteries results in reduced blood flow to the extremities, causing a pale tone, tingling, coldness, and numbness.
*'''[[Effect::Auditory suppression]]''' - According to anecdotal reports, this effect is likely due to very low blood pressure, which is why it is listed as physical. It has been described as a "hollow" type distortion or loss of hearing.
*'''[[Effect::Auditory suppression]]''' - According to anecdotal reports, this effect is likely due to very low blood pressure, which is why it is listed as physical. It has been described as a "hollow" type distortion or loss of hearing.
}}
}}
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===Lethal dosage===
===Lethal dosage===
According to dailymed.nlm.nih.gov's prescribing information page for clonidine, clonidine's oral [[LD50|LD<sub>50</sub>]] in mice is 206 mg/kg and for rats, 465 mg/kg.
According to the NIH prescribing information page for clonidine, clonidine's oral [[LD50|LD<sub>50</sub>]] in mice is 206 mg/kg and for rats, 465 mg/kg.
There are case reports that show [[naloxone]] may be a useful antidote in treating clonidine overdoses. However, this is not in widespread clinical use.<ref> Reversal of clonidine toxicity by naloxone. Niemann, James T et al. Annals of Emergency Medicine, Volume 15, Issue 10, 1229 - 1231</ref>
There are case reports that show [[naloxone]] may be a useful antidote in treating clonidine overdoses. However, this is not in widespread clinical use.<ref> Reversal of clonidine toxicity by naloxone. Niemann, James T et al. Annals of Emergency Medicine, Volume 15, Issue 10, 1229 - 1231</ref>
===Tolerance and addiction potential===
===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 is dangerous due to concurrent use of depressants.{{citation needed}}
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 is reported to have potentiating effects, but this has not been studied and may be dangerous or risky due to oversedation.{{citation needed}}
===Dangerous interactions===
===Dangerous interactions===
Revision as of 22:27, 14 November 2017
Pharmacology and legality should be expanded before publication. Please help by contributing.
It may contain incorrect information, particularly with respect to dosage, duration, subjective effects, toxicity and other risks. It may also not meet PW style and grammar standards.
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
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, substance withdrawal (from either alcohol, opioids, or smoking tobacco), migraine, menopausal flushing, diarrhea, and certain pain conditions.[1] It is classified as a centrally acting α2adrenergicagonist and imidazoline receptoragonist. It has been in clinical use for over 40 years.[2]
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.[3]
Clonidine also binds to the imidazoline I1 receptor as an agonist.[4]
Some studies suggest that clonidine in low doses can boost growth hormone levels.[5]
Although clonidine overdoses may be reversed by naloxone[citation needed] (a controversial claim) as well as clonidine being noted to cause constipation[6], it causes no respiratory depression.[7]
''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, about equivalent to benzodiazepines. Users can be very tired and can sleep through or ignore prompts to wake up.
Decreased blood pressure - Clonidine's sympatholytic effects lower blood pressure quickly and effectively and therefore, it is commonly used to treat hypertension.[8]
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.
Decreased blood pressure upon standing - This effect may be overwhelming at higher doses and can be described as a "head rush" or feeling of lightheadedness.
Physical fatigue - This general feeling of decreased movement and tiredness is from sedation.
Dizziness - Clonidine can lead to an increased chance of falls due to this. This effect gets stronger with dose increase.
Skin reactions - This can happen if clonidine is given in a patch, such as in Catapres-TTS.
Raynaud's Phenomenon - Raynaud's Phenomenon occurs when the spasm of arteries results in reduced blood flow to the extremities, causing a pale tone, tingling, coldness, and numbness.
Auditory suppression - According to anecdotal reports, this effect is likely due to very low blood pressure, which is why it is listed as physical. It has been described as a "hollow" type distortion or loss of hearing.
Cognitive effects
Cognitive fatigue - Clonidine behaves this way due to the fact that user is usually so sedated that all they want to do is sleep, making cognitive tasks difficult.
Anxiety suppression - Clonidine has relatively strong anxiolytic effects and is sometimes used clinically to treat anxiety.[9]
Focus suppression - This usually occurs at higher doses. The effect is also usually from the sedated state.
Irritability - One can feel very agitated and annoyed at things. This especially happens when the medicine is suddenly stopped, which is an incorrect practice; clonidine should be tapered off of the user.
It is strongly recommended that one use harm reduction practices when using this substance. Caution should be used when used in combination with other depressants.
Lethal dosage
According to the NIH prescribing information page for clonidine, clonidine's oral LD50 in mice is 206 mg/kg and for rats, 465 mg/kg.
There are case reports that show naloxone may be a useful antidote in treating clonidine overdoses. However, this is not in widespread clinical use.[10]
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 is reported to have potentiating effects, but this has not been studied and may be dangerous or risky due to oversedation.[citation needed]
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.
Stimulants (Lisdexamfetamine, amphetamine, propylhexedrine, others) - This combination could potentially increase the chance of an abnormal heartbeat.[citation needed] Caution should be exercised and physical activity should be avoided. However, in clinical use, this combination has a positive effect on the mind, especially in ADHD, and can be used for focusing or memory retention. Still, it is not wise to combine high doses of each substance.[12]
↑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.
↑ 3.03.1Isaac, L. (1980). Clonidine in the central nervous system: site and mechanism of hypotensive action. Journal of Cardiovascular Pharmacology, 2, S5-20. PMID: 6154837
↑Bricca, G., Greney, H., Zhang, J., Dontenwill, M., Stutzmann, J., Belcourt, A., & Bousquet, P. (1994). Human brain imidazoline receptors: further characterization with [3 H] clonidine. European Journal of Pharmacology: Molecular Pharmacology, 266(1), 25-33. DOI: https://doi.org/10.1016/0922-4106(94)90205-4
↑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
↑Bailey, P. L., Sperry, R. J., Johnson, G. K., Eldredge, S. J., East, K. A., East, T. D., ... & Stanley, T. H. (1991). Respiratory effects of clonidine alone and combined with morphine, in humans. Anesthesiology, 74(1), 43-48.
↑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.
What will get this page published? I assume dangerous interactions needs the templates, cite flags, etc. --Corticosteroid (talk) 03:10, 31 August 2017 (CEST)
@corticosteroid: Do you want me to give you instructions or just demonstrate it by completing it myself? Clarity (talk) 22:03, 31 August 2017 (CEST)
