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, substance withdrawal (from either alcohol, opioids, or smoking tobacco), migraine, menopausal flushing, diarrhea, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist. It has been in clinical use for over 40 years.

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.

• α_1A receptor: 316.23 nM
• α_1B receptor: 316.23 nM
• α_1D receptor: 125.89 nM
• α_2A receptor: 42.92 nM
• α_2B receptor: 106.31 nM
• α_2C 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.

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

• • Sedation - Clonidine can be strong in its sedating effect. This can lead to atypical walking gait from decreased locomotion coordination.
  • Decreased heart rate
  • Decreased blood pressure
  • 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 probably be avoided.
  • Dry mouth
  • Constipation
  • Decreased blood pressure upon standing - This effect may be overwhelming at higher doses and can be called a "head rush."
  • Physical fatigue
  • Dizziness
  • Skin reactions - This can happen if clonidine is given in a patch, such as in Catapres-TTS.
  • Anxiety
  • 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.

Cognitive effects

• • Cognitive fatigue
  • Irritability
  • Focus suppression - This usually occurs at higher doses. The effect is also usually from the sedated state.
  • Thought deceleration

Toxicity and harm potential

It is strongly recommended that one use harm reduction practices when using this drug, especially concurrently with other depressants. Clonidine is a central nervous system depressant and combining these drugs, especially in high doses, may be fatal. According to drugs.com, clonidine's maximum medical dose for hypotension is 2.4 miligrams in divided doses. It is likely not dangerous to take a strong dose (300 micrograms) at once with tolerance, but you should use harm reduction practices and not do as mentioned with no tolerance.

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.

There have been studies that show naloxone may be a useful antidote in treating clonidine overdoses, however this is not in widespread clinical use.

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.

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.

See also

• Responsible use
• Depressant

References

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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