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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|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>



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Clonidine
Chemical Nomenclature
Common names Catapres, Catapres-TTS, Kapvay, Nexiclon XR
Substitutive name Clonidine
Systematic name N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
Class Membership
Psychoactive class Depressant
Chemical class Imidazoline
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 25 μg
Light 50 - 75 μg
Common 75 - 100 μg
Strong 100 - 300 μg
Heavy 300 μg +
Duration
Total 6 - 8 hours
Onset 15 - 45 minutes
Peak 60 - 90 minutes
Offset 6 - 8 hours









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.

Interactions
Stimulants
Depressants
Dissociatives

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 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

This pharmacology section is incomplete.

You can help by adding to it.

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]

Binding Sites Binding Affinity Ki (nM)[3]
α1A 316.23
α1B 316.23
α1D 125.89
α2A 42.92
α2B 106.31
α2C 233.1

Clonidine also binds to the Imidazoline I1 receptor as an agonist.[citation needed]

Some studies suggest that clonidine in low doses can boost growth hormone levels.[4]

Subjective effects

This subjective effects section is a stub.

As such, it is still in progress and may contain incomplete or wrong information.

You can help by expanding or correcting it.

''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 PsychonautWiki contributors. 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

Cognitive effects


Toxicity and harm potential

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.[7]

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]

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.[9]

Legality

This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

United States: In the US, clonidine is only available through prescription.[citation needed]

See also

References

  1. Brayfield, A, ed. (13 January 2014). "Clonidine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 28 June 2014.
  2. Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management.". Current Clinical Pharmacology. 6 (4): 280–7. PMID 21827389.
  3. 3.0 3.1 Isaac, L. (1980). Clonidine in the central nervous system: site and mechanism of hypotensive action. Journal of Cardiovascular Pharmacology, 2, S5-20. PMID: 6154837
  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
  5. 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
  6. Hoehn-Saric R, Merchant AF, Keyser ML, Smith NVK. Effects of Clonidine on Anxiety Disorders. Arch Gen Psychiatry.
  7. Reversal of clonidine toxicity by naloxone. Niemann, James T et al. Annals of Emergency Medicine, Volume 15, Issue 10, 1229 - 1231
  8. Koski, A., Ojanperä, I., & Vuori, E. (2002). Alcohol and benzodiazepines in fatal poisonings. Alcoholism: Clinical and Experimental Research, 26(7), 956-959.
  9. Revisiting clonidine: an innovative add-on option for attention-deficit/hyperactivity disorder. Childress AC, Sallee FR. (2012) https://www.ncbi.nlm.nih.gov/pubmed/22462040

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