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Dr. Bob is Robert Hsiung, MD,
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Posted by ed_uk on February 16, 2006, at 14:33:34
Trifluoperazine (Stelazine) is a typical neuroleptic. Here is an interesting study........
Neurosci Lett. 2005 Dec 24
Trifluoperazine, an orally available clinically used drug, disrupts opioid antinociceptive tolerance.Tang L, Shukla PK, Wang ZJ.
Department of Biopharmaceutical Sciences, College of Pharmacy, University of Illinois, 833 South Woods Street, Chicago, IL 60612, USA.
Calcium/calmodulin dependent protein kinase II (CaMKII) has been shown to play an important role in the generation and maintenance of opioid tolerance. In this study, trifluoperazine was studied for its effect on morphine tolerance in mice. Acute treatment with trifluoperazine (0.5mg/kg, i.p.) completely reversed the established antinociceptive tolerance to morphine. Pretreatment with trifluoperazine also significantly attenuated the development of antinociceptive tolerance (p<0.01). Morphine induced a significant up-regulation of supraspinal and spinal CaMKII activity in tolerant mice, which was abolished after the pretreatment or acute treatment with trifluoperazine. These data suggested that trifluoperazine was capable of suppressing opioid tolerance, possibly by the mechanism of inhibiting CaMKII. Since trifluoperazine has been safely used as an antipsychotic drug, we propose that the drug should be studied in humans for the prevention and treatment of opioid tolerance and addiction.
Posted by ed_uk on February 16, 2006, at 14:35:44
In reply to Trifluoperazine (Stelazine) and opioid tolerance, posted by ed_uk on February 16, 2006, at 14:33:34
Interestingly, Stelazine has been used as an antiemetic during the first few days of opioid treatment (for severe pain). Low doses are normally used eg. 1-2mg twice a day.
Ed
Posted by med_empowered on February 18, 2006, at 13:47:30
In reply to Re: Trifluoperazine (Stelazine) and opioid tolerance » ed_uk, posted by ed_uk on February 16, 2006, at 14:35:44
I'd hate to be "treated" for addiction with Stelazine...even low-dose antipsychotics can cause problems, and I think the last thing recovering drug user's need is a chemical lobotomy. As for "preventing" tolerance...I don't see what the big deal is with "tolerance" in pain management. As long as the doses aren't high enough to impair a person (and stimulants can help undo some of the painkiller-induced fog), I think "tolerance" should be a minor concern, one placed long after patient comfort.
Are there any non-phenothiazine anti-emitic drugs? Here in the US we have Marinol--the over-priced "safe" synthetic THC...but usually its only used in cancer or AIDS patients.
Posted by ed_uk on February 18, 2006, at 14:56:17
In reply to Re: Trifluoperazine (Stelazine) and opioid tolerance, posted by med_empowered on February 18, 2006, at 13:47:30
Hi Med
>I'd hate to be "treated" for addiction with Stelazine
Me too! I did think the article was interesting though.
>Are there any non-phenothiazine anti-emetic drugs?
Yes, there are many........
Domperidone (Motilium) - a selective D2 antagonist which doesn't cross the blood brain barrier. As a result, extrapyramidal side effects are very uncommon. Domperidone is not available in the US.
Metoclopramine (Reglan, Maxolon) - a drug related to the antipsychotics sulpiride and amisulpride.
Ondansetron (Zofran) and granisetron (Kytril). These drugs act at 5-HT3 receptors and are very useful for chemotherapy-induced nausea and vomiting.
Cyclizine (Valoid, Marezine) - an antihistamine and anticholinergic.
There are many more.......
Kind regards
Ed
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