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Xylocaine abuse potential

almost-

Bluelighter
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Mar 15, 2006
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Finland
Does anyone know if xylocaine has any abuse potential?

I heard that i.v lidocaine might have some.
 
No, numbing agents in general do not have any abuse potential, except for cocaine. Anyhow, there are always some people who consider kicking a concrete wall with their bare foot recreational.
 
Sorry my mistake xylocaine=lidocaine. :\

Psychiatr Prax. 1996 Mar;23(2):90-1.
[Euphoric effect of lidocaine]
[Article in German]
Blanke J, Wolstein J, Paulus HJ.
A 42 year old drug addict reported on his experiences with intravenous application of scandicaine and lidocaine. Lidocaine led to short-lasting euphoria comparable with former cocaine-induced effects. Pharmacological hypothesis to explain these mental alterations are discussed.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=8657816&dopt=Citation
 
I'll give it a try a bit later :)

Is euphoria a side-effect of lidocaine?

Lidocaine is widely used for local and regional anaesthesia. It is also administered intravenously to control ventricular arrhythmias. The main systemic side-effects of lidocaine are dizziness, drowsiness, coma, seizures, respiratory arrest, muscle twitching, paresthesia, dysarthria, numbness of the tongue, tinnitus, diplopia and other visual disturbances. We report an unusual side-effect which followed lidocaine administration in two patients. A 24-year-old man, ASA I, with no history of epilepsy or CNS disease, was admitted for wound repair of the left forearm. An axillary block was performed
using 35 ml lidocaine 2% without epinephrine. A blood aspiration test was negative. However, after 2 min the patient became talkative and developed a 'high state of happiness'; he started to laugh, sing and tell jokes. Shortly afterwards, the patient complained of severe tinnitus, diplopia and tongue numbness. The euphoria lasted for about 40 min. The next day, the patient recalled the 'wonderful pleasant experience' but was unable to recall the exact details.

A 56-year-old man was admitted for right femoro-popliteal endarterectomy under local anaesthesia. After infiltration of 50 ml lidocaine 1%, he developed an unexplained feeling of exaggerated happiness.
The patient started to laugh and tell jokes. He also reported tinnitus and numbness of the tongue. This euphoric state lasted 50 min. The next day, the patient stated 'I was like a drunken man'. Psychotic reactions have been reported after intravenous lidocaine administration to control ventricular arrhythmias [1]. Most reactions are about fear from death, doom anxiety and delirium [2]. However, euphoria is rarely reported.

Blanke et al. described a short-lasting euphoria after intravenous lidocaine in a patient who was addicted to cocaine [3]. The euphoric properties of cocaine are due primarily to inhibition of catecholamine
reuptake at CNS synapses. Other local anaesthetics do not block the uptake of norepinephrine. Our patients denied any history of cocaine or alcohol abuse. The euphoric effect of lidocaine
can be attributed to its central action. Anaesthetists usually ask about tinnitus, vision alterations, metallic taste and tongue numbness to detect early evidence of lidocaine toxicity. Mood changes
may pass unrecognised if the patient’s personality is unknown to the physician, the behaviour is considered the result of a psychotic personality; or if the behaviour is masked by premedication or sedatives.
In summary, it is possible that mood alterations, especially euphoria, may be an early sign of CNS reaction following lidocaine administration.

A. Zeidan
Sahel General Hospital,
Beirut, Lebanon
E-mail: [email protected]
A. Baraka
American University of Beirut
Medical Center,
Beirut, Lebanon

References
1 Turner WM. Lidocaine and psychotic reactions. Annals of International Medicine 1982; 97: 149–50.
2 Saravay SM, Marke J, Steinberg MD, Rabiner CJ. 'Doom anxiety' and delirium in lidocaine toxicity. American Journal of Psychiatry 1987; 144: 159–63.
3 Blanke J, Wolstein J, Paulus HJ. [Euphoric effect of lidocaine.]. Psychiatrische Praxis 1996; 23: 90–1.

Source:
Anaesthesia. 2004 Dec;59(12):1253-4.
Is euphoria a side-effect of lidocaine?
Zeidan A, Baraka A.
http://www.ncbi.nlm.nih.gov/entrez/..._uids=15550004&query_hl=4&itool=pubmed_DocSum
 
it is widely reported that rats self administer various para amino caines, maybe them damn rodents are getting high off of proocaine
I would guess in the case of the cocaine user lidocaine provided a pharmacological cue that caused remembered effects. a sort of super placebo.
 
Try clicking here if you want some concrete answers to your querie.
94-15-5.gif

Infact this is somewhat similar to a p-amino-benzoic ester of N-methyl-piperidine-4-ol.
 
Last edited:
Lidocaine: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide

Cocaine: methyl 3-benzoyloxy-8-methyl-8-azabicyclo [3.2.1]octane-4-carboxylate

They're not even remotely related chemically -- I think a lot of people get confused because they both end in -caine. Correct me if I'm wrong, but the -caine series of anesthetics aren't even related to cocaine at all as far as I know, except for the fact that Novocaine (procaine) was the first produced in this topical anesthetic class, and named as such because it was a "new cocaine" without the euphoric and addictive properties. (Source: Erowid)
 
You are correct that they aren't related chemically. That patient self-report by almost- is an isolated incident, and patients do lie about things like whether or not they've used cocaine before.
I read a bit of the journal article attached by Smyth, and all I can say is, damn I can see Bactine becomming prescription only.
 
I heard that benzocaine will show up as a false positive for cocaine on some drug tests
 
Symth,

How does the activity profile of dimethocaine change if the Ar-NH2 group is oxidized to Ar-NO2?

I know I've had some minor but real effects from injected procaine before when coadministered with cocaine. Xylocaine lasts longer than procaine.

"I see patterns"
 
Lignocaine (UK name) does have an abuse potential somewhat similar to cocaine, but as the dose that achieves that is very close to the toxic dose (either stopping heart or breathing) it's not gained much value as a recreational drug. Quite a few show similar activity, but are just as, if not more toxic than lignocaine.

About the only local anaesthetic that has cocaine like activity well short of it's toxic dose is tropacocaine (which is cocaine with the 2-methoxycarbonyl group missing). It's not controlled and is about 1/10th the potency of coke (the para-fluoro ester analogue of tropacocaine is 0.4x the potency of coke which would make it on a par with street coke in the UK)

They're all nasty anyway - I like the look on friends faces when I refuse lines of coke (sometimes also telling them I prefer to have some speed!) - as they turn quite a few users into egocentric wankers (me included)
 
Im not sure Helios. It's worth noting that the DARI nomifensine has an arylamino moiety. Also with regard to tropacocaine. The SAR data for this compound is listed in the 2000 review by Satendra Singh which can be found online. Out of cocaine analogs (not phenyltropanes), the o-hydroxyphenyl shows roughly 10x the potency of cocaine. However compounds lacking the side-chain ester are so much weaker than coke alot of hope has died out in this area.
 
Helios. said:
Symth,

How does the activity profile of dimethocaine change if the Ar-NH2 group is oxidized to Ar-NO2?

I know I've had some minor but real effects from injected procaine before when coadministered with cocaine. Xylocaine lasts longer than procaine.

"I see patterns"

as a general rule aromatic Nitro groups are to be avoided as they are toxic and decouple metabolism, good for getting hot and losing weight though
 
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