Addiction. 2005 Mar;100 Suppl 1:58-67.
A medication screening trial evaluation of reserpine, gabapentin and lamotrigine pharmacotherapy of cocaine dependence.
Berger SP, Winhusen TM, Somoza EC, Harrer JM, Mezinskis JP, Leiderman DB, Montgomery MA, Goldsmith RJ, Bloch DA, Singal BM, Elkashef A.
Cincinnati VA/UC NIDA MDRU, VA Medical Center, Cincinnati, OH, USA.

ABSTRACT Aims To conduct a preliminary evaluation of the safety and efficacy of reserpine, gabapentin or lamotrigine versus an unmatched placebo control as a treatment for cocaine dependence. Design A 10-week out-patient study using the Cocaine Rapid Efficacy and Safety Trial (CREST) study design. Setting The study was conducted at the Cincinnati Medication Development Research Unit (MDRU). Participants Participants met Diagnostic and Statistical Manual version IV (DSM-IV) criteria for cocaine dependence. Sixty participants were enrolled, with 50 participants completing the final study measures. Intervention The targeted daily doses of medication were reserpine 0.5 mg, gabapentin 1800 mg and lamotrigine 150 mg. All participants received 1 hour of manualized individual cognitive behavioral therapy on a weekly basis. Measurements Primary outcome measures of efficacy included urine benzoylecgonine (BE) level, Cocaine Clinical Global Impression scale-observer and self-report of cocaine use. Safety measures included adverse events, electrocardiograms (ECGs), vital signs and laboratory tests. Findings Subjective measures of cocaine dependence indicated significant improvement for all study groups. Urine BE results indicated a significant improvement for the reserpine group (P < 0.05) and non-significant changes for the other study groups. No pattern of physical or laboratory abnormalities attributable to treatment with any of the medications was identified. There were three serious adverse events reported, none of which were related to study procedures. The medications appeared to be tolerated well. Conclusions The present findings suggest that reserpine may be worthy of further study as a cocaine dependence treatment.

J Pharmacol Exp Ther. 2005 Feb 25.
Comparison of the Antinociceptive Profiles of Gabapentin and 3-Methylgabapentin in Rat Models of Acute and Persistent Pain: Implications for Mechanism of Action.
Urban MO, Ren K, Park KT, Campbell B, Anker N, Stearns B, Aiyar J, Belley M, Cohen C, Bristow L.
Merck Research Laboratories.

The anticonvulsant gabapentin (GBP) has been shown to be effective for the treatment of neuropathic pain, although its mechanism of action remains unclear. A recent report has suggested that binding to the alpha2sigma subunit of voltage gated calcium channels contributes to its antinociceptive effect, based on the stereoselective efficacy of two analogs: (1S,3R)3-MeGBP (IC50=42 nM) which is effective in neuropathic pain models, and (1R,3R)3-MeGBP (IC50>10000 nM) which is ineffective (Field et al., 2000). The present study was designed to further examine the profiles of GBP and 3-MeGBP in rat models of acute and persistent pain. Systemic administration of GBP or (1S,3R)3-MeGBP inhibited tactile allodynia in the spinal nerve ligation model of neuropathic pain, whereas (1R,3R)3-MeGBP was ineffective. The antiallodynic effect of GBP, but not (1S,3R)3-MeGBP, was blocked by i.t. injection of the GABAB receptor antagonist CGP52432. Systemic GBP or (1S,3R)3-MeGBP also inhibited the second phase of formalin-evoked nociceptive behaviors, whereas (1R,3R)3-MeGBP was ineffective. However, both (1S,3R)3-MeGBP and (1R,3R)3-MeGBP, but not GBP, inhibited first phase behaviors. In the carrageenan model of inflammatory pain, systemic GBP or (1R,3R)3-MeGBP failed to inhibit thermal hyperalgesia, whereas (1S,3R)3-MeGBP had a significant albeit transient effect. Systemic (1S,3R)3-MeGBP, but not GBP or (1R,3R)3-MeGBP, also produced an antinociceptive effect in the warm water tail withdrawal test of acute pain. These data demonstrate that GBP and 3-MeGBP display different antinociceptive profiles, suggesting dissimilar mechanisms of antinociceptive action. Thus, the stereoselective efficacy of 3-MeGBP, presumably related to alpha2sigmabinding, likely does not completely account for the mechanism of action of GBP.

Drug information

GENERIC NAME: gabapentin
BRAND NAME: Neurontin

DRUG CLASS AND MECHANISM: Gabapentin is in the class of drugs called anticonvulsants because they are used to treat seizures (epilepsy) and herpes zoster (shingles). Gabapentin is related to the brain chemical gamma aminobutyric acid (GABA) but exactly how it works is unknown.

PREPARATIONS: Capsules are available in 100mg, 300mg, 400mg, and 800mg sizes by Park-Davis labs.

STORAGE: Store in a dry place at 15-30 degrees C (69-86 F)

PRESCRIBED FOR: Gabapentin is used for treating seizure disorders and herpes zoster (shingles).

DOSING: Gabapentin can be taken with or without food at doses specifically directed by your physician. Individual doses vary greatly between individuals. Usually the drug is taken two to three times daily. It is currently not approved under the age of 12 years old. If discontinued, gabapentin should be gradually withdrawn (usually over one week) as directed by the doctor.

DRUG INTERACTIONS: Gabapentin appears to be relatively safe and has not been shown to interact with other drugs except for it's potential of added sedation. Gabapentin should not be taken within 2 hours of Maalox. Gabapentin may interfere with the reading of N- Multistix in detecting urine protein.

SIDE EFFECTS: Neurontin has few side effects which include sleepiness, dizziness, unsteady gait, fatigue and eye twitching.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.

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NEURONTIN - GENERIC (generic - what is it?)

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Dosage	Packing	Price	Pay now
300 mg	100 caps	USD 149.00
400 mg	100 caps	USD 197.00