From: "Steve Harris" <sbharris@ix.RETICULATEDOBJECTcom.com> Newsgroups: sci.med Subject: Re: Ziban Date: Tue, 11 Jun 2002 17:00:37 -0700 Message-ID: <ae636s$qvd$1@slb5.atl.mindspring.net> CBI <00doc@mindspring.com> wrote in message ... > > >"Steve Harris" <sbharris@ix.RETICULATEDOBJECTcom.com> wrote in message >news:ae0a89$rac$1@slb0.atl.mindspring.net... >> >> CBI <00doc@mindspring.com> wrote in message ... >> ><Gail@nospam.com> wrote in message >> >news:dn00gu8aa5l0723jq81covsoh73222aalr@4ax.com... >> >> >> >> Wellbutrin is stimulant type anti depressant. >> > >> >Gail, >> > >> >You have no idea what you are talking about. Wellbutrin/Zyban is not speed. >> > >> >-- >> >CBI, MD >> >> >> She didn't say it was. > >Sure she did. Yes, someone pointed out the other message. > >> She said it's a stimulant type antidepressant, and so >> it is. Why do you think it's a seizure risk? Read the PDR (or your Drugdex >> or Nat Med Formulary or whatever you use) on the stuff. >> > >If you say so. It really does not stand out in this regard. COMMENT: Read the experimental literature. It surely DOES stand out in this regard. It's been used as a dopaminergic probe in drug models for years. It's not amphetamine, but it has some similarities in action, cross tolerance, and induction of self-administrative behavior. No, the manufacturers don't really play this up much. To me it quacks (weakly) like a duck. Exp Clin Psychopharmacol 1998 Feb;6(1):32-44 Discriminative-stimulus and participant-rated effects of methylphenidate, bupropion, and triazolam in d-amphetamine-trained humans. Rush CR, Kollins SH, Pazzaglia PJ. Department of Psychiatry and Human Behavior, University of Mississippi Medical Center, Jackson 39219-4505, USA. crush@fiona.umsmed.edu The discriminative-stimulus and participate-rated effects of a range of doses of d-amphetamine (2.5-20 mg), methylphenidate (5-40 mg), bupropion (50-400 mg), and triazolam (0.0625-0.5 mg) were tested in 5 humans trained to discriminate between oral d-amphetamine (20 mg) and placebo. d-Amphetamine and methylphenidate generally dose dependently increased drug-appropriate responding. Bupropion and triazolam on average occasioned less than or equal to 40% drug-appropriate responding. d-Amphetamine, methylphenidate, and bupropion produced stimulant-like participant-rated effects, while triazolam produced sedative-like effects. These results further demonstrate that the acute behavioral effects of d-amphetamine and methylphenidate overlap extensively in humans, which is concordant with preclinical studies. Bupropion produced some d-amphetamine-like, participant-rated drug effects but did not occasion significant levels of d-amphetamine-appropriate responding. These findings are concordant with previous findings of a dissociation between the discriminative-stimulus and participant-rated effects of drugs. Publication Types: Clinical Trial PMID: 9526144 [PubMed - indexed for MEDLINE] ================ Psychopharmacology (Berl) 1997 Nov;134(2):201-12 Dopaminergic mediation of the discriminative stimulus effects of bupropion in rats. Terry P, Katz JL. Psychobiology Section, NIDA Intramural Research Program, National Institutes of Health, Baltimore, MD 21224, USA. Bupropion is a novel, non-tricyclic antidepressant with a primary pharmacological action of monoamine uptake inhibition. The drug resembles a psychostimulant in terms of its neurochemical and behavioural profiles in vivo, but it does not reliably produce stimulant-like effects in humans at clinically prescribed doses. Bupropion binds with modest selectivity to the dopamine transporter, but its behavioural effects have often been attributed to its inhibition of norepinephrine uptake. This experiment examines monoaminergic involvement in the discriminative stimulus effects of bupropion. Rats were trained to press one lever when injected i.p. with bupropion (17.0 mg/kg), and another lever when injected with saline. In substitution tests, dose-response curves were obtained for several monoamine uptake inhibitors. Nine of ten dopamine uptake blockers fully substituted for bupropion; the exception, indatraline (LU 19-005), partially substituted (71% bupropion-appropriate responding). Serotonin and norepinephrine uptake blockers (zimelidine and nisoxetine, respectively) produced negligible or limited substitution, and the anti-muscarinic dopamine uptake blocker benztropine produced limited partial substitution. A series of dopamine D1-like and D2-like receptor agonists were also tested: only the D2-like agonist RU 24213 fully substituted; three other D2-like agonists and four D1-like agonists partially substituted (50% < drug responding < 80%). Antagonism of the discriminative effects of bupropion was obtained with a D1- and a D2-like dopamine antagonist. The results demonstrate strong similarities with those obtained using other dopamine uptake inhibitors as training drugs, and support the view that the behavioural effects of bupropion are primarily mediated by dopaminergic mechanisms. PMID: 9399385 [PubMed - indexed for MEDLINE] ================ J Pharmacol Exp Ther 1989 Oct;251(1):150-5 Effects of cocaine and related drugs in nonhuman primates. III. Self-administration by squirrel monkeys. Bergman J, Madras BK, Johnson SE, Spealman RD. Department of Psychiatry, Harvard Medical School, New England Regional Primate Research Center, Southborough, Massachusetts. The self-administration of cocaine was compared with that of bupropion, 1-(2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine, mazindol, methylphenidate and nomifensine, drugs that displace [3H]cocaine from its binding sites and have monoamine uptake inhibiting effects in common with those of cocaine. Squirrel monkeys responded under a second-order fixed-interval schedule of consequent i.v. drug injection, and dose-effect curves were established by determining stable rates of responding maintained by saline and a range of doses of each drug. Cocaine (0.01-0.56 mg/kg/injection), bupropion (0.1-3.0 mg/kg/injection), 1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-(3- phenylpropyl)piperazine-(0.03-1.0 mg/kg/injection), methylphenidate (0.01-0.3 mg/kg/injection) and nomifensine (0.01-0.3 mg/kg) maintained comparable rates and patterns of responding in all subjects, whereas mazindol (0.03-0.3 mg/kg) maintained self-administration behavior in only half the monkeys studied. The present results in conjunction with those of previous studies in squirrel monkeys reveal a close correspondence between the relative potencies of cocaine and related drugs for maintaining i.v. self-administration and for increasing rates of schedule-controlled responding, suggesting that the reinforcing and psychomotor-stimulant effects of the drugs are mediated similarly. The potency relations observed in the present study also agree generally with those observed for displacement of specifically bound [3H]cocaine in monkey caudate-putamen suggesting that the reinforcing effects of cocaine involve its actions at specific recognition sites in brain.PMID: 2529365 [PubMed - indexed for MEDLINE] ============== J Addict Dis 2002;21(2):1-16 Bupropion treatment for cocaine abuse and adult attention-deficit/hyperactivity disorder. Levin FR, Evans SM, McDowell DM, Brooks DJ, Nunes E. Department of Psychiatry, Columbia University/New York State Psychiatric Institute, New York 10032, USA. fr12@columbia.edu There are few published studies assessing the efficacy of pharmacologic treatments for attention-deficit hyperactivity disorder (ADHD) among substance abusers seeking treatment. Eleven patients who met DSM-IV diagnostic criteria for cocaine dependence and adult ADHD were entered into a 12-week single-blind trial of divided daily doses of bupropion (BPR). All patients received weekly individual standardized relapse prevention therapy. Treatment compliance and retention were good. Patients reported significant reductions in attention difficulties, hyperactivity and impulsivity. Self-reported cocaine use, cocaine craving, and cocaine positive toxicologies, also decreased significantly. In a previously published trial, 12 patients who met similar diagnostic criteria for adult ADHD and cocaine dependence were entered into a 12-week trial of divided daily doses of sustained-release methylphenidate (MPH). Improvements observed on BPR were similar to, and did not differ from those previously observed with MPH. These preliminary data suggest that BPR may be as effective as sustained-release MPH, when combined with relapse prevention therapy, for cocaine abusers with adult ADHD. However, a future study directly comparing BPR to MPH in a double-blind placebo-controlled trial is needed. PMID: 11916368 [PubMed - in process] ================ Eur J Pharmacol 2002 May 17;443(1-3):113-8 Nicotine and bupropion share a similar discriminative stimulus effect. Young R, Glennon RA. Department of Medicinal Chemistry, School of Pharmacy, Box 980540, Virginia Commonwealth University, 23298-0540, Richmond, VA, USA Bupropion is a weakly potent central nervous system (CNS) stimulant that is marketed both as an antidepressant and as an anti-smoking aid. The mechanism(s) by which it produces its effects is not well understood. In the present study, the effect of bupropion was examined in rats trained to discriminate the stimulus effect of 0.60 mg/kg of (-)-nicotine from saline in a two-lever drug discrimination task. In tests of stimulus generalization (substitution), the nicotine (ED(50)=0.17 mg/kg) stimulus completely generalized to bupropion (ED(50)=5.50 mg/kg). In addition, interaction studies were conducted that evaluated the effect of 3.0 mg/kg of bupropion, a dose that when given alone produced saline-appropriate responding, in combination with various doses of nicotine. This application resulted in an enhancement of the potency of nicotine (ED(50)=0.05 mg/kg), as indicated by a leftward shift of the nicotine dose-effect function. In tests of stimulus antagonism, various doses of bupropion were administered prior to the training dose of nicotine and were found to be ineffective as antagonists of the nicotine stimulus. In contrast, the nicotinic acetylcholine receptor (nicotine receptor) antagonist mecamylamine (AD(50)=0.40 mg/kg) completely blocked the stimulus effect of nicotine. Mecamylamine did not attenuate the stimulus generalization of bupropion. The results demonstrated that bupropion can produce a nicotine-like response in nicotine-trained animals, but it does so via a mechanism of action that is unlike that of nicotine. It is speculated that bupropion may be somewhat effective as an anti-smoking treatment in people who are motivated to quit smoking because low doses of bupropion produce a nicotine-like effect(s) that serve as a suitable substitute for nicotine.PMID: 12044800 [PubMed - in process] ================= Sleep Res Online 1998;1(1):49-61 Increased dopaminergic transmission mediates the wake-promoting effects of CNS stimulants. Nishino S, Mao J, Sampathkumaran R, Shelton J. Stanford University School of Medicine, Sleep Disorders Center, Palo Alto, CA 94304, USA. nishino@leland.stanford.edu Amphetamine-like stimulants are commonly used to treat sleepiness in narcolepsy. These compounds have little effect on rapid eye movement (REM) sleep-related symptoms such as cataplexy, and antidepressants (monoamine uptake inhibitors) are usually required to treat these symptoms. Although amphetamine-like stimulants and antidepressants enhance monoaminergic transmission, these compounds are non-selective for each monoamine, and the exact mechanisms mediating how these compounds induce wakefulness and modulate REM sleep are not known. In order to evaluate the relative importance of dopaminergic and noradrenergic transmission in the mediation of these effects, five dopamine (DA) uptake inhibitors (mazindol, GBR-12909, bupropion, nomifensine and amineptine), two norepinephrine (NE) uptake inhibitors (nisoxetine and desipramine), d-amphetamine, and modafinil, a non-amphetamine stimulant, were tested in control and narcoleptic canines. All stimulants and dopaminergic uptake inhibitors were found to dose-dependently increase wakefulness in control and narcoleptic animals. The in vivo potencies of DA uptake inhibitors and modafinil on wake significantly correlated with their in vitro affinities to the DA and not the NE transporter. DA uptake inhibitors also moderately reduced REM sleep, but this effect was most likely secondary to slow wave sleep (SWS) suppression, since selective DA uptake inhibitors reduced both REM sleep and SWS proportionally. In contrast, selective NE uptake inhibitors had little effect on wakefulness, but potently reduced REM sleep. These results suggest that presynaptic activation of DA transmission is critical for the pharmacological control of wakefulness, while that of the NE system is critical for REM sleep regulation. Our results also suggest that presynaptic activation of DA transmission is a key pharmacological property mediating the wake-promoting effects of currently available CNS stimulants. PMID: 11382857 [PubMed - indexed for MEDLINE] -- I welcome email from any being clever enough to fix my address. It's open book. A prize to the first spambot that passes my Turing test. From: ((Steven B. Harris)) Newsgroups: sci.med Date: 12 Jun 2002 17:18:54 GMT Subject: Re: Ziban Message-ID: <20020612131854.09539.00000562@mb-mb.aol.com> >>> Read the experimental literature. >> >>I read your citations. The gist I get from it is that it is weak in this >>regard. I'm not impressed. > >Try taking it at night.. COMMENT: Try taking it *at all*. Again my criticism that most doctors would be a lot better doctors if they actually tried taking THEMSELVES any and all drugs they prescribe, just for a day or two. (Note to anethesiologists-- no, stay away from fentenyl; every rule has a few exceptions). Note sources say Wellbutrin/Ziban isn't a *reliable* simulant at therapeutic doses. The qualification is that it's a pretty reliable if you take more than you're supposed to. Which some people will. Cases of bupropion recreational use have been reported. SBH Steve Harris From: "Steve Harris" <sbharris@ix.RETICULATEDOBJECTcom.com> Newsgroups: sci.med Subject: Re: Ziban Date: Wed, 12 Jun 2002 16:16:21 -0700 Message-ID: <ae8kpk$pa6$1@slb0.atl.mindspring.net> Kurt Ullman wrote in message ... > >>Note sources say Wellbutrin/Ziban isn't a *reliable* simulant at >>therapeutic doses. The qualification is that it's a pretty reliable if >>you take more than you're supposed to. Which some people will. Cases of >>bupropion recreational use have been reported. > > There have also been reports of recreational use of Haldol. I knew a >junkie that used to grind up Contact's little tiny time pills and inject it >for cheap barb high. Thusly, I am less than impressed with most reports of >recreational use. Seems that almost anything can be abused recreationally. I knew somebody was going to say that. Which is why I recommend you try the stuff for yourself. It's not a controlled substance. Get some doc to write you scrip for 20 or 30. Tell him you're trying to quit cocaine. -- I welcome email from any being clever enough to fix my address. It's open book. A prize to the first spambot that passes my Turing test. |
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