Hey all SWIF is relatively unfamiliar with cocaine use however is asking the following question for a friend. Excuse any obvious lack of knowledge that he presents.
Here is my issue
SWIF has a good friend who once used cocaine pretty heavily she hasnt used in 3 years and wants to start using on a rare special occasion basis she is worried however that she'll go overboard on the night becuase once she starts on that night she cant stop she wondered whether if she took diazepam after she'd taken so much it would stop cocaines effects regardless of whether she took more. Similar to how a Heroin user might take Nalaxone to stop him using anymore.
If not what other drugs would force the cocaine experience to end?
Ionotropic glutamate receptors have been implicated in the behavioral effects of cocaine in animal studies. For example, these receptors are involved in cocaine self-administration, reinstatement of drug seeking, and behavioral sensitization. Recently, an important role for metabotropic glutamate receptors (mGluRs) has been identified, following reports that mice lacking the mGluR5 subtype do not self-administer cocaine; and that a selective mGluR5 antagonist (2-methyl-6(phenyethynyl)-pyridine or MPEP) attenuates cocaine self-administration at doses not affecting food reinforced operant behavior. While these observations suggest that MPEP may be acting as a functional cocaine antagonist, these prior studies have been conducted in rodent models. The present study by Dr. Roger Spealman and colleagues examined MPEP effects on squirrel monkeys responding for i.v. cocaine, and compared these effects with the NMDA antatongist, dizocilpine. Animals self-administered cocaine under a second-order schedule and were then withdrawn so that responses were no longer reinforced by i.v. cocaine. Once responding on the drug lever was extinguished (i.e., responding on the lever no longer produced cocaine injections), drug seeking was measured following a cocaine "priming" injection to reinstate the behavior. In a separate study, monkeys were trained to discriminate cocaine from saline by making responses on a drug- or saline-appropriate lever, after injection of either the drug or the vehicle. Other animals were observed following MPEP or dizocilpine to assess antagonist effects on a number of spontaneous behaviors including locomotion, object exploration, foraging, self-grooming, and vocalizations. The data show that pretreatment with either 0.1 to 1.0 mg/kg MPEP, or 0.003 to 0.03 mg/kg dizocilpine, to animals responding for 0.1 to 0.3 mg/kg cocaine, produced dose-related decreases in response rates. When MPEP pretreatment was tested before cocaine priming in animals extinguished from lever pressing, with either 0.3 or 1.0 mg/kg cocaine as the prime, both 0.3 and 1.0 mg/kg MPEP significantly attenuated reinstatement. However, higher doses of MPEP were required to reduce seeking primed with 1.0 mg/kg cocaine, suggesting that the cocaine-antagonist effects of this mGluR5 drug are surmountable. Surmountable antagonism was also observed for the attenuation of discriminative cue properties of cocaine, as MPEP produced an overall rightward shift in the cocaine dose-response function in this paradigm. In contrast, the NMDA antagonist had little effect on drug seeking in the test for reinstatement, and rather than blocking discriminative cue properties of cocaine, had either no effect or enhanced cocaine discrimination. Behavioral observations revealed that MPEP significantly reduced overall locomotion but was without effects on foraging, exploration or grooming, whereas dizocilpine had no behavioral effects except that it increased muscle resistance. As MPEP did not disrupt spontaneous behavior, and also did not disrupt operant responding in drug discrimination testing, this mGluR5 antagonist may be a promising candidate to explore for the treatment of cocaine addiction. Moreover, the observed differences between this antagonist and dizocilpine suggest that the observed antagonism is independent from MPEP's interaction with the glutamate NMDA receptor. Lee, B., Platt, D.M., Rowlett, J.K., Adewale, A. and Spealman, R.D. Attenuation of Behavioral Effects of Cocaine by the Metabotropic Glutamate Receptor 5 Antagonist 2-methyl-6-(phenylethynyl)-pyridine in Squirrel Monkeys: Comparison with Dizocilpine. The Journal of Pharmacology and Experimental Therapeutics, 312, pp. 1232-1240, 2005.
2-methyl-6(phenyethynyl)-pyridine or MPEP has proven to be a effective antagonist in rodents, though SWIM doesn't know of the effectivity in humans or with test on humans.
The only problem is to aquire it.Because of the amounts of heroin overdoses on the streets, some states or citys freely provide nalexon to decrease the numbers of deaths.
This is not the case with any cocaine antagonist, only hospitals have them, SWIM isn't even sure if paramedics have them.
Actually, SWIM did just think of something... it's *possible* Neurontin (gabapentin) or Lyrica (pregabalin) would do the trick. These drugs work by inhibiting brain synapses, and apparently inhibiting excitatory neurotransmitter release (at least in some areas of the brain). Basically, they dampen brain activity. So a moderate dose of either substance at some point could throw a big wet blanket on the party, although not exactly forcing the end of coke's activity in the body.
Actually, SWIM did just think of something... it's *possible* Neurontin (gabapentin) or Lyrica (pregabalin) would do the trick. These drugs work by inhibiting brain synapses, and apparently inhibiting excitatory neurotransmitter release (at least in some areas of the brain). Basically, they dampen brain activity. So a moderate dose of either substance at some point could throw a big wet blanket on the party, although not exactly forcing the end of coke's activity in the body.
SWIF has access to both of these medications, is the polypharmacology of this combination dangerous at all. SWIF would hate to be trying to help his friend as cause her major health complications.
11-09-2006, 16:32
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