You are on page 1of 12

6/16/2014 Gabapentin - Wikipedia, the free encyclopedia

http://en.wikipedia.org/wiki/Neurotin 1/12
Gabapentin
Systematic (IUPAC) name
2-[1-(aminomet hyl)cyclohexyl]acet ic acid
Clinical data
Trade names Fanatrex, Gabarone, Gralise,
Neurontin, Nupentin, Neogab
AHFS/Drugs.com monograph
MedlinePlus a694007
Licence data US Daily Med:link
Pregnancy cat. B1 (AU) C (US)
Legal status Prescription Only (S4) (AU) -
only (CA) POM (UK) -only (US)
Routes Oral
Pharmacokinetic data
Bioavailability 27-60% (inversely proportional
to dose; a high fat meal also
increases bioavailability)[1][2]
Protein binding Less than 3%[1][2]
Metabolism Not significantly
metabolised[1][2]
Gabapentin
From Wikipedia, the free encyclopedia
(Redirected from Neurotin)
Gabapentin (Neurontin) is a pharmaceutical drug,
specifically a GABA analog. It was originally developed to
treat epilepsy, and currently is also used to relieve
neuropathic pain. It is recommended as a first line agent for
the treatment of neuropathic pain arising from diabetic
neuropathy, post-herpetic neuralgia, and central neuropathic
pain.
[3]
It is also commonly prescribed by doctors for many off-label
treatments, such as restless leg syndrome, insomnia, and
bipolar disorder. There are, however, concerns regarding the
quality of the trials conducted for a number of conditions.
[4]
Contents
1 Medical uses
1.1 Pain
1.2 Seizures
1.3 Other
2 Adverse effects
2.1 Suicide
2.2 Overdosage
3 Pharmacology
4 Mechanism of action
5 Society and culture
5.1 Sales
5.2 FDA approval
5.3 Legal action
5.4 Off label promotion
5.5 Brand names
5.6 Forms
5.7 Related drugs
6 Veterinary use
7 See also
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 2/12
Half-life 5 to 7 hours[1][2]
Excretion
Renal
[1][2]
Identifiers
CAS number
60142-96-3

ATC code N03AX12
PubChem CID 3446
DrugBank DB00996
ChemSpider
3328

UNII
6CW7F3G59X

KEGG
D00332

ChEBI
CHEBI:42797

ChEMBL
CHEMBL940

PDB ligand ID GBN (PDBe, RCSB PDB)
Chemical data
Formula
C
9
H
17
NO
2

Mol. mass 171.237 g/mol
(what is this?) (verify)
8 References
9 External links
Medical uses
Gabapentin is used primarily to treat seizures, neuropathic
pain, including concussions, and hot flashes.
[5]
There are,
however, concerns regarding the quality of the research on its
use to treat migraines, bipolar disorders, and pain.
[4]
Pain
Gabapentin provides significant pain relief in about a third of
people who take it for fibromyalgia or chronic neuropathic
pain; however, there are side effects in two thirds of
people.
[6]
It is effective in reducing narcotic usage post
operatively
[7]
and is helpful in neuropathic pain due to
cancer.
[8]
It has not been shown useful for HIV-associated
sensory neuropathy.
[9]
When used for neuropathic pain it
does not appear superior to carbamazepine.
[10]
It appears as
effective as pregabalin and costs less.
[11]
It does not appear
to provide benefit for complex regional pain syndrome
[12]
or
to be useful for migraine prevention.
[13]
Seizures
Gabapentin is approved for treatment of focal seizures in a number of countries
[14]
and evidence supports its use
for treating partial and mixed seizure disorders however there is insufficient evidence for its use in generalized
epilepsy.
[15]
Other
There is some evidence of benefit in acquired pendular nystagmus and infantile nystagmus but not in periodic
alternating nystagmus.
[16][17]
Gabapentin may help with menopausal symptoms.
[18][19]
It may be effective in
reducing pain and spasticity in multiple sclerosis.
[20]
Gabapentin is not supported for alcohol withdrawal,
[21]
and
treatment of smoking cessation has had mixed results.
[22][23]
Gabapentin helps with itching (pruritus) associated
with renal failure (uremic pruritus)
[24]
and other conditions.
[25]
Other off-label uses include treatment for mental health disorders. Numerous trials show that it is not effective alone
as a mood-stabilizing treatment for bipolar disorder and so has no therapeutic advantage in having fewer side
effects over better established bipolar drugs such as lithium and valproic acid. Gabapentin is useful in the treatment
SMILES
InChI
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 3/12
of anxiety associated with bipolar disorder and restless leg syndrome and for insomnia, but has limited usefulness in
disorders such as social anxiety disorder and obsessive-compulsive disorder, and in treatment-resistant
depression.
[26]
Gabapentin does not appear effective for the treatment of tinnitus.
[27]
Adverse effects
Gabapentin's most common side effects in adult patients include dizziness, fatigue, weight gain, drowsiness, and
peripheral edema (swelling of extremities);
[28]
these mainly occur at higher doses in the elderly. Also, in children 3
to 12 years of age, researchers observed susceptibility to mild-to-moderate mood swings, hostility, concentration
problems, and hyperactivity. Though rare, the literature reports several cases of hepatotoxicity.
[29][30]
Gabapentin
should be used carefully in patients with renal impairment due to possible accumulation and toxicity.
[31][32]
An increase in formation of adenocarcinomas was observed in rats during preclinical trials; however, the clinical
significance of these results remains undetermined. Gabapentin is also known to induce pancreatic acinar cell
carcinomas in rats through an unknown mechanism, perhaps by stimulation of DNA synthesis; these tumors did not
affect the lifespan of the rats and did not metastasize.
[33]
May cause adverse effects to patient decision making ability.
Suicide
In 2009 the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal
thoughts and behaviors in patients taking gabapentin, along with other anticonvulsant drugs
[34]
modifying the
packaging insert to reflect this.
[28]
In July 2009 the manufacturer of gabapentin (Pfizer) went to trial regarding the
association between gabapentin and the increased risk of suicide.
[35]
Overdosage
Persons who accidentally or intentionally ingested overdoses have manifested drowsiness, sedation, blurred vision,
slurred speech and somnolence or coma. Serum gabapentin concentrations may be measured to confirm
diagnosis.
[36]
Pharmacology
Gabapentin was initially synthesized to mimic the chemical structure of the neurotransmitter gamma-aminobutyric
acid (GABA), but is not believed to act on the same brain receptors.
Some of its activity may involve interaction with voltage-gated calcium channels. Gabapentin binds to the 2
subunit (1 and 2) and has been found to reduce calcium currents after chronic but not acute application via an effect
on trafficking
[37]
of voltage-dependent calcium channels in the central nervous system.
[38]
Another possible
mechanism of action, reported by Ben Barres and colleagues in Cell in 2009, is that gabapentin halts the formation
of new synapses.
[39]
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 4/12
Mechanism of action
Gabapentin interacts with voltage-sensitive calcium channels in cortical neurons. Gabapentin increases the synaptic
concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the
release of mono-amine neurotransmitters. One of the mechanisms implicated in this effect of gabapentin is the
reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1
area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors. Other studies have
shown that the antihyperalgesic and antiallodynic effects of gabapentin are mediated by the descending
noradrenergic system, resulting in the activation of spinal alpha-2 adrenergic receptors. Gabapentin has also been
shown to bind and activate the adenosine A1 receptor.
Society and culture
Sales
Gabapentin is best known under the brand name Neurontin manufactured by Pfizer subsidiary Parke-Davis. A
Pfizer subsidiary named Greenstone markets generic gabapentin.
In December 2004 the FDA granted final approval to a generic equivalent to Neurontin made by the Israeli firm
Teva.
Neurontin began as one of Pfizer's best selling drugs; however, Pfizer has come under heavy criticism and serious
litigation for its marketing of the drug. They face allegations that, behind the scenes, Parke-Davis marketed the drug
for at least a dozen supposed uses that the FDA had not approved.
[40][41]
Today it is a mainstay drug for
migraines, even though it was not approved for such use in 2004.
[42]
FDA approval
Gabapentin was originally approved by the U.S. Food and Drug Administration (FDA) in 1994, for use as an
adjuvant medication to control partial seizures (effective when added to other antiseizure drugs). In 2002, an
indication was added for treating postherpetic neuralgia (neuropathic pain following shingles).
[43]
Legal action
Off label promotion
Although some small, non-controlled studies in the 1990smostly sponsored by gabapentin's manufacturer
suggested that gabapentin treatment for bipolar disorder may be promising,
[20]
the preponderance of evidence
suggests that it is not effective.
[44]
Subsequent to the corporate acquisition of the original patent holder, the
pharmaceutical company Pfizer admitted that there had been violations of FDA guidelines regarding the promotion
of unproven off-label uses for gabapentin in the Franklin v. Pfizer case.
Reuters reported on March 25, 2010, that "Pfizer Inc violated federal racketeering law by improperly promoting
the epilepsy drug Neurontin ... Under federal RICO law the penalty is automatically tripled, so the finding will cost
Pfizer $141 million."
[45]
The case stems from a claim from Kaiser Foundation Health Plan Inc. that "it was misled
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 5/12
A capsule of
gabapentin
into believing Neurontin was effective for off-label treatment of migraines, bipolar disorder and other conditions.
Pfizer argued that Kaiser physicians still recommend the drug for those uses."
[46]
Bloomberg News (3/26/10, Van Voris, Lawrence) added that "during the trial, Pfizer argued that Kaiser doctors
continued to prescribe the drug even after the health insurer sued Pfizer in 2005. The insurer's website also still lists
Neurontin as a drug for neuropathic pain, Pfizer lawyers said in closing argument."
[47]
The Wall Street Journal (3/26/10, Kamp) noted that Pfizer spokesman Christopher Loder said, "We are
disappointed with the verdict and will pursue post-trial motions and an appeal."
[48]
He would later add that "the
verdict and the judge's rulings are not consistent with the facts and the law."
[45]
Franklin v. Pfizer case
By some estimates, off-label prescriptions account for roughly 90 percent of Neurontin sales.
[49]
While off-label
prescriptions are common for a number of drugs and are legal, marketing of off-label uses of a drug is illegal.
[40]
In
2004, Warner-Lambert agreed to plead guilty and pay $430 million in fines to settle civil and criminal charges
regarding the illegal marketing of Neurontin for off-label purposes, and further legal action is pending. The 2004
settlement was one of the largest in U.S. history, and the first off-label promotion case brought successfully under
the False Claims Act. The courts of New York State, for example, have refused to certify a class of injured parties
who took Neurontin for off-label use, finding that they had failed to state that they had any injury.
[50]
The University of California, San Francisco (UCSF) has archived
[51]
and studied
[52]
the documents made public by
this case, which opens a window into the illegal promotion and marketing of pharmaceuticals. However, Pfizer
maintains that the illegal activity originated in 1996, well before it acquired Parke-Davis (through its acquisition of
Warner-Lambert) in 2000. Several lawsuits are underway after people who had been prescribed gabapentin for
off-label treatment of bipolar disorder later attempted or committed suicide.
Brand names
Various suppliers of gabapentin market it under a number of brand names, including Neurostil, Neurontin, Fanatrex,
Gabarone, Gralise, Nupentin, Gabrion,
[53]
Penral, Gabapin.
Forms
Gabapentin comes as:
100 mg, 300 mg, and 400 mg capsules
300 mg, 600 mg, and 800 mg tablets
a 250 mg/5 mL oral (by mouth) solution.
Inactive ingredients in the capsules include lactose, cornstarch, and talc.
The 100-mg capsule shell also contains: gelatin and titanium dioxide.
The 300-mg capsule shell also contains: gelatin, titanium dioxide, and yellow iron oxide.
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 6/12
The 400-mg capsule shell also contains: gelatin, red iron oxide, titanium dioxide, and yellow iron oxide. The
imprinting ink contains FD&C Blue No. 2 and titanium dioxide.
Inactive ingredients in the tablets include poloxamer 407, copolyvidonum, cornstarch, magnesium stearate,
hydroxypropyl cellulose, talc, candelilla wax, and purified water.
Inactive ingredients in the oral solution include glycerin, xylitol, purified water, and artificial flavor.
[54]
Related drugs
Parke-Davis developed a drug called pregabalin as a successor to gabapentin.
[55]
Pregabalin was brought to
market by Pfizer as Lyrica after the company acquired Warner-Lambert. Pregabalin is related in structure to
gabapentin.
[56]
Another new drug atagabalin has been trialled by Pfizer as a treatment for insomnia.
[57]
Veterinary use
Gabapentin is also used for some animal treatments, but formulations (especially liquid forms) for human use may
contain the sweetener Xylitol, which is toxic to dogsso veterinary use of the human version requires caution.
[58]
See also
Gabapentin enacarbil
Pregabalin
Atagabalin
Phenibut
Baclofen
References
1. ^
a

b

c

d

e
"Neurontin, Gralise (gabapentin) dosing, indications, interactions, adverse effects, and more"
(http://reference.medscape.com/drug/neurontin-gralise-gabapentin-343011#showall). Medscape Reference.
WebMD. Retrieved 6 April 2014.
2. ^
a

b

c

d

e
Goa, KL; Sorkin, EM (September 1993). "Gabapentin. A review of its pharmacological properties and
clinical potential in epilepsy.". Drugs 46 (3): 40927. doi:10.2165/00003495-199346030-00007
(http://dx.doi.org/10.2165%2F00003495-199346030-00007). PMID 7693432
(https://www.ncbi.nlm.nih.gov/pubmed/7693432).
3. ^ Attal N, Cruccu G, Baron R, et al. (September 2010). "EFNS guidelines on the pharmacological treatment of
neuropathic pain: 2010 revision". Eur. J. Neurol. 17 (9): 1113e88. doi:10.1111/j.1468-1331.2010.02999.x
(http://dx.doi.org/10.1111%2Fj.1468-1331.2010.02999.x). PMID 20402746
(https://www.ncbi.nlm.nih.gov/pubmed/20402746).
4. ^
a

b
Vedula, SS; Bero L; Scherer RW; Dickersin K (November 2009). "Outcome reporting in industry-sponsored
trials of gabapentin for off-label use". The New England Journal of Medicine 361 (20): 196371.
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 7/12
trials of gabapentin for off-label use". The New England Journal of Medicine 361 (20): 196371.
doi:10.1056/NEJMsa0906126 (http://dx.doi.org/10.1056%2FNEJMsa0906126). PMID 19907043
(https://www.ncbi.nlm.nih.gov/pubmed/19907043).
5. ^ "Gabapentin" (http://www.drugs.com/monograph/gabapentin.html). The American Society of Health-System
Pharmacists. Retrieved 3 April 2011.
6. ^ Moore, RA; Wiffen PJ; Derry S; McQuay HJ (2011-03-16). "Gabapentin for chronic neuropathic pain and
fibromyalgia in adults". In Moore, R Andrew. Cochrane database of systematic reviews (Online) (3): CD007938.
doi:10.1002/14651858.CD007938.pub2 (http://dx.doi.org/10.1002%2F14651858.CD007938.pub2).
PMID 21412914 (https://www.ncbi.nlm.nih.gov/pubmed/21412914).
7. ^ Ho, KY; Gan TJ; Habib AS (2006-12-15). "Gabapentin and postoperative pain--a systematic review of
randomized controlled trials". Pain 126 (13): 91101. doi:10.1016/j.pain.2006.06.018
(http://dx.doi.org/10.1016%2Fj.pain.2006.06.018). PMID 16846695
(https://www.ncbi.nlm.nih.gov/pubmed/16846695).
8. ^ Bar Ad, V (September 2010). "Gabapentin for the treatment of cancer-related pain syndromes". Reviews on
Recent Clinical Trials 5 (3): 1748. doi:10.2174/157488710792007310
(http://dx.doi.org/10.2174%2F157488710792007310). PMID 20482492
(https://www.ncbi.nlm.nih.gov/pubmed/20482492).
9. ^ Phillips, TJ; Cherry CL; Cox S; Marshall SJ; Rice AS (2010-12-28). "Pharmacological treatment of painful HIV-
associated sensory neuropathy: a systematic review and meta-analysis of randomised controlled trials"
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3010990). In Pai, Nitika Pant. Plos One 5 (12): e14433.
Bibcode:2010PLoSO...514433P (http://adsabs.harvard.edu/abs/2010PLoSO...514433P).
doi:10.1371/journal.pone.0014433 (http://dx.doi.org/10.1371%2Fjournal.pone.0014433). PMC 3010990
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3010990). PMID 21203440
(https://www.ncbi.nlm.nih.gov/pubmed/21203440).
10. ^ Wiffen, P; Collins S; McQuay H; Carroll D; Jadad A; Moore A (2005-07-20). "Anticonvulsant drugs for acute
and chronic pain". In Wiffen, Philip J. Cochrane database of systematic reviews (Online) (3): CD001133.
doi:10.1002/14651858.CD001133.pub2 (http://dx.doi.org/10.1002%2F14651858.CD001133.pub2).
PMID 16034857 (https://www.ncbi.nlm.nih.gov/pubmed/16034857).
11. ^ Finnerup, NB; Sindrup SH; Jensen TS (September 2010). "The evidence for pharmacological treatment of
neuropathic pain". Pain 150 (3): 57381. doi:10.1016/j.pain.2010.06.019
(http://dx.doi.org/10.1016%2Fj.pain.2010.06.019). PMID 20705215
(https://www.ncbi.nlm.nih.gov/pubmed/20705215).
12. ^ Tran de, QH; Duong S; Bertini P; Finlayson RJ (February 2010). "Treatment of complex regional pain syndrome:
a review of the evidence". Can J Anaesth 57 (57(2)): 14966. doi:10.1007/s12630-009-9237-0
(http://dx.doi.org/10.1007%2Fs12630-009-9237-0). PMID 20054678
(https://www.ncbi.nlm.nih.gov/pubmed/20054678).
13. ^ Linde, M; Mulleners, WM; Chronicle, EP; McCrory, DC (Jun 24, 2013). "Gabapentin or pregabalin for the
prophylaxis of episodic migraine in adults.". The Cochrane database of systematic reviews 6: CD010609.
doi:10.1002/14651858.CD010609 (http://dx.doi.org/10.1002%2F14651858.CD010609). PMID 23797675
(https://www.ncbi.nlm.nih.gov/pubmed/23797675).
14. ^ Johannessen, SI; Ben-Menachem E (2006). "Management of focal-onset seizures: an update on drug treatment".
Drugs 66 (13): 170125. doi:10.2165/00003495-200666130-00004 (http://dx.doi.org/10.2165%2F00003495-
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 8/12
200666130-00004). PMID 16978035 (https://www.ncbi.nlm.nih.gov/pubmed/16978035).
15. ^ French, JA; Kanner AM; Bautista J; Abou-Khalil B; Browne T; Harden CL; Theodore WH; Bazil C; Stern J;
Schachter SC; Bergen D; Hirtz D; Montouris GD; Nespeca M; Gidal B; Marks WJ; Turk WR; Fischer JH;
Bourgeois B; Wilner A; Faught RE; Sachdeo RC; Beydoun A; Glauser TA (May 2004). "Efficacy and tolerability of
the new antiepileptic drugs, I: Treatment of new-onset epilepsy: report of the TTA and QSS Subcommittees of the
American Academy of Neurology and the American Epilepsy Society". Epilepsia 45 (5): 4019.
doi:10.1111/j.0013-9580.2004.06204.x (http://dx.doi.org/10.1111%2Fj.0013-9580.2004.06204.x).
PMID 15101821 (https://www.ncbi.nlm.nih.gov/pubmed/15101821).
16. ^ McLean, RJ; Gottlob I (August 2009). "The pharmacological treatment of nystagmus: a review". Expert opinion
on pharmacotherapy 10 (11): 180516. doi:10.1517/14656560902978446
(http://dx.doi.org/10.1517%2F14656560902978446). PMID 19601699
(https://www.ncbi.nlm.nih.gov/pubmed/19601699).
17. ^ Strupp, M; Brandt T (July 2009). "Current treatment of vestibular, ocular motor disorders and nystagmus"
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3002631). Therapeutic Advances in Neurological Disorders 2
(4): 22339. doi:10.1177/1756285609103120 (http://dx.doi.org/10.1177%2F1756285609103120). PMC 3002631
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3002631). PMID 21179531
(https://www.ncbi.nlm.nih.gov/pubmed/21179531).
18. ^ Toulis, KA; Tzellos T; Kouvelas D; Goulis DG (February 2009). "Gabapentin for the treatment of hot flashes in
women with natural or tamoxifen-induced menopause: a systematic review and meta-analysis". Clinical
therapeutics 31 (2): 22135. doi:10.1016/j.clinthera.2009.02.006
(http://dx.doi.org/10.1016%2Fj.clinthera.2009.02.006). PMID 19302896
(https://www.ncbi.nlm.nih.gov/pubmed/19302896).
19. ^ Cheema, D; Coomarasamy A; El-Toukhy T (November 2007). "Non-hormonal therapy of post-menopausal
vasomotor symptoms: a structured evidence-based review". Archives of Gynecology and Obstetrics 276 (5): 463
9. doi:10.1007/s00404-007-0390-9 (http://dx.doi.org/10.1007%2Fs00404-007-0390-9). PMID 17593379
(https://www.ncbi.nlm.nih.gov/pubmed/17593379).
20. ^
a

b
Mack, Alicia (2003). "Examination of the evidence for off-label use of gabapentin"
(http://www.amcp.org/data/jmcp/Contemporary%20Subject-559-568.pdf). Journal of Managed Care Pharmacy 9
(6): 55968. PMID 14664664 (https://www.ncbi.nlm.nih.gov/pubmed/14664664).
21. ^ Prince V, Turpin KR; Turpin, K. R. (June 2008). "Treatment of alcohol withdrawal syndrome with
carbamazepine, gabapentin, and nitrous oxide". Am J Health Syst Pharm 65 (11): 103947. doi:10.2146/ajhp070284
(http://dx.doi.org/10.2146%2Fajhp070284). PMID 18499876 (https://www.ncbi.nlm.nih.gov/pubmed/18499876).
22. ^ Sood, A; Ebbert JO; Schroeder DR; Croghan IT; Sood R; Vander Weg MW; Wong GY; Hays JT (February
2007). "Gabapentin for smoking cessation: a preliminary investigation of efficacy". Nicotine & Tobacco Research 9
(2): 2918. doi:10.1080/14622200601080307 (http://dx.doi.org/10.1080%2F14622200601080307).
PMID 17365760 (https://www.ncbi.nlm.nih.gov/pubmed/17365760).
23. ^ Sood, A; Ebbert JO; Wyatt KD; Croghan IT; Schroeder DR; Sood R; Hays JT (March 2010). "Gabapentin for
smoking cessation" (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2825098). Nicotine & Tobacco Research 12
(3): 3004. doi:10.1093/ntr/ntp195 (http://dx.doi.org/10.1093%2Fntr%2Fntp195). PMC 2825098
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2825098). PMID 20081039
(https://www.ncbi.nlm.nih.gov/pubmed/20081039).
24. ^ Berger, TG; Steinhoff, M (June 2011). "Pruritus and renal failure.". Seminars in cutaneous medicine and surgery
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 9/12
24. ^ Berger, TG; Steinhoff, M (June 2011). "Pruritus and renal failure.". Seminars in cutaneous medicine and surgery
30 (2): 99100. doi:10.1016/j.sder.2011.04.005 (http://dx.doi.org/10.1016%2Fj.sder.2011.04.005).
PMID 21767770 (https://www.ncbi.nlm.nih.gov/pubmed/21767770).
25. ^ Anand S (March 2013). "Gabapentin for pruritus in palliative care". American Journal of Hospice and Palliative
Medicine 30 (2): 192196. doi:10.1177/1049909112445464 (http://dx.doi.org/10.1177%2F1049909112445464).
26. ^ Chouinard, G (May 2006). "The search for new off-label indications for antidepressant, antianxiety,
antipsychotic and anticonvulsant drugs" (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1449873). J Psychiatry
Neurosci 31 (3): 168176. ISSN 1180-4882 (https://www.worldcat.org/issn/1180-4882). PMC 1449873
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1449873). PMID 16699602
(https://www.ncbi.nlm.nih.gov/pubmed/16699602).
27. ^ Aazh, H; El Refaie, A; Humphriss, R (December 2011). "Gabapentin for tinnitus: a systematic review.".
American journal of audiology 20 (2): 1518. doi:10.1044/1059-0889(2011/10-0041)
(http://dx.doi.org/10.1044%2F1059-0889%282011%2F10-0041%29). PMID 21940981
(https://www.ncbi.nlm.nih.gov/pubmed/21940981).
28. ^
a

b
"Neurontin packaging insert"
(http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020235s041,020882s028,021129s027lbl.pdf) (pdf).
U.S. Food and Drug Administration (FDA). 2009-05-01. Retrieved 2010-07-16.
29. ^ Lasso-de-la-Vega, MC; Zapater, P; Such, J; Perez-Mateo, M; Horga, JF (December 2001). "Gabapentin-
associated hepatotoxicity". Am J Gastroenterol 96 (12): 34602. doi:10.1111/j.1572-0241.2001.05357.x
(http://dx.doi.org/10.1111%2Fj.1572-0241.2001.05357.x). PMID 11774985
(https://www.ncbi.nlm.nih.gov/pubmed/11774985).
30. ^ http://www.fdable.com/advanced_aers_query/0b20534305c9d0e50552a188af4a3487
31. ^ Dogukan, A; Aygen, B; Berilgen, MS; Dag, S; Bektas, S; Gunal, AI (April 2006). "Gabapentin-induced coma in a
patient with renal failure". Hemodialysis International 10 (2): 1689. doi:10.1111/j.1542-4758.2006.00089.x
(http://dx.doi.org/10.1111%2Fj.1542-4758.2006.00089.x). PMID 16623669
(https://www.ncbi.nlm.nih.gov/pubmed/16623669).
32. ^ Bookwalter, T; Gitlin, M (December 2005). "Gabapentin-induced neurologic toxicities". Pharmacotherapy 25
(12): 18179. doi:10.1592/phco.2005.25.12.1817 (http://dx.doi.org/10.1592%2Fphco.2005.25.12.1817).
PMID 16305301 (https://www.ncbi.nlm.nih.gov/pubmed/16305301).
33. ^ Gabapentin Official FDA information, side effects and uses (http://www.drugs.com/pro/gabapentin.html)
34. ^ "Suicidal Behavior and Ideation and Antiepileptic Drugs"
(http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm100190.ht
m). U.S. Food and Drug Administration (FDA).
35. ^ Margaret Cronin Fisk; Jef Feeley; Cary OReilly (2009-07-24). "Pfizer Faces First Trial on Neurontin Suicide
Claim (Update1)" (http://www.bloomberg.com/apps/news?pid=newsarchive&sid=a1CYnBA5tGV4). Bloomberg.
Retrieved 2010-07-16.
36. ^ R.C. Baselt, Disposition of Toxic Drugs and Chemicals in Man, 8th edition, Biomedical Publications, Foster City,
CA, 2008, pp. 6778. ISBN 978-0-9626523-7-0.
37. ^ Hendrich, J; Van Minh, AT; Heblich, F; Nieto-Rostro, M; Watschinger, K; Striessnig, J; Wratten, J; Davies, A et
al. (March 2008). "Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin"
(http://www.pnas.org/content/105/9/3628.full.pdf). Proceedings of the National Academy of Sciences of the
United States of America 105 (9): 362833. Bibcode:2008PNAS..105.3628H
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 10/12
(http://adsabs.harvard.edu/abs/2008PNAS..105.3628H). doi:10.1073/pnas.0708930105
(http://dx.doi.org/10.1073%2Fpnas.0708930105). PMC 2265195
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2265195). PMID 18299583
(https://www.ncbi.nlm.nih.gov/pubmed/18299583).
38. ^ Davies, A; Hendrich, J; Van Minh, AT; Wratten, J; Douglas, L; Dolphin, AC (May 2007). "Functional biology of
the alpha(2)delta subunits of voltage-gated calcium channels". Trends Pharmacol Sci 28 (5): 2208.
doi:10.1016/j.tips.2007.03.005 (http://dx.doi.org/10.1016%2Fj.tips.2007.03.005). PMID 17403543
(https://www.ncbi.nlm.nih.gov/pubmed/17403543).
39. ^ Eroglu, ; Allen, NJ; Susman, MW; O'Rourke, NA; Park, CY; zkan, E; Chakraborty, C; Mulinyawe, SB et al.
(October 2009). "The Gabapentin Receptor 2-1 is the Neuronal Thrombospondin Receptor Responsible for
Excitatory CNS Synaptogenesis" (http://www.cell.com/abstract/S0092-8674%2809%2901185-4). Cell 139 (2):
38092. doi:10.1016/j.cell.2009.09.025 (http://dx.doi.org/10.1016%2Fj.cell.2009.09.025). PMC 2791798
(https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2791798). PMID 19818485
(https://www.ncbi.nlm.nih.gov/pubmed/19818485).
40. ^
a

b
Henney JE (August 2006). "Safeguarding patient welfare: who's in charge?"
(http://www.annals.org/content/145/4/305.full.pdf). Annals of Internal Medicine 145 (4): 3057.
doi:10.7326/0003-4819-145-4-200608150-00013 (http://dx.doi.org/10.7326%2F0003-4819-145-4-200608150-
00013). PMID 16908923 (https://www.ncbi.nlm.nih.gov/pubmed/16908923).
41. ^ "WarnerLambert to pay $430 million to resolve criminal & civil health care liability relating to off-label
promotion" (http://www.usdoj.gov/opa/pr/2004/May/04_civ_322.htm) (Press release). Department of Justice. May
13, 2004. Retrieved December 2, 2009.
42. ^ Mathew, NT; Rapoport, A; Saper, J; Magnus, L; Klapper, J; Ramadan, N; Stacey, B; Tepper, S (February
2001). "Efficacy of Gabapentin in Migraine Prophylaxis" (http://onlinelibrary.wiley.com/doi/10.1046/j.1526-
4610.2001.111006119.x/pdf). Headache: the Journal of Head and Face Pain 41 (2): 11928. doi:10.1046/j.1526-
4610.2001.111006119.x (http://dx.doi.org/10.1046%2Fj.1526-4610.2001.111006119.x). PMID 11251695
(https://www.ncbi.nlm.nih.gov/pubmed/11251695).
43. ^ Pfizer: Product MonographNeurontin (http://www.pfizer.com/pfizer/download/uspi_neurontin.pdf) PDF (251 KB)
Retrieved 14 August 2006
44. ^ Reinares M, Rosa AR, Franco C, et al. (March 2013). "A systematic review on the role of anticonvulsants in the
treatment of acute bipolar depression". Int. J. Neuropsychopharmacol. 16 (2): 48596.
doi:10.1017/S1461145712000491 (http://dx.doi.org/10.1017%2FS1461145712000491). PMID 22575611
(https://www.ncbi.nlm.nih.gov/pubmed/22575611).
45. ^
a

b
Berkrot, Bill (2010-03-25). "US jury's Neurontin ruling to cost Pfizer $141 mln"
(http://www.reuters.com/article/2010/03/25/pfizer-neurontin-idUSN259778920100325). Reuters.
46. ^ "Pfizer faces $142M in damages for drug fraud"
(http://www.businessweek.com/ap/financialnews/D9ELVKG80.htm). Business Week. 2010-03-25. Retrieved 13
January 2012.
47. ^ Bob Van Voris; Janelle Lawrence (2010-03-26). "Pfizer Told to Pay $142.1 Million for Neurontin Marketing
Fraud" (http://www.bloomberg.com/apps/news?pid=email_en&sid=a_9aVylZQGjU). Bloomberg News. Retrieved
13 January 2012.
48. ^ Jon Kamp (2010-03-25). "Jury Rules Against Pfizer in Marketing Case"
(http://online.wsj.com/article/SB10001424052748704094104575144223583428414.html). The Wall Street Journal.
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 11/12
External links
DrugBank: gabapentin (http://www.drugbank.ca/drugs/DB00996)
Gabapentin information from MedlinePlus
(http://www.nlm.nih.gov/medlineplus/druginfo/meds/a694007.html)
"Gabapentin" (http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000940/) PubMed Health. National Center
for Biotechnology Information (NCBI)
"Suicidal Behavior and Ideation and Antiepileptic Drugs"
(http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm1001
90.htm) U.S. Food and Drug Administration (FDA)
Neurontin (http://topics.nytimes.com/topics/news/health/diseasesconditionsandhealthtopics/neurontin_drug/)
collected news and commentary at The New York Times
"Gabapentin" (http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Gabapentin) Drug Information
Portal. U.S. National Library of Medicine.
Retrieved from "http://en.wikipedia.org/w/index.php?title=Gabapentin&oldid=611623921"
Categories: Amino acids Analgesics Anticonvulsants Anxiolytics GABA analogues Mood stabilizers
(http://online.wsj.com/article/SB10001424052748704094104575144223583428414.html). The Wall Street Journal.
Retrieved 13 January 2012.
49. ^ Tansey, Bernadette (2004-05-14). "Huge penalty in drug fraud, Pfizer settles felony case in Neurontin off-label
promotion" (http://www.sfgate.com/cgi-bin/article.cgi?f=/c/a/2004/05/14/BUGKK6L0LB1.DTL). San Francisco
Chronicle. p. C-1.
50. ^ "Baron v Pfizer, Inc." (http://www.courts.state.ny.us/reporter/3dseries/2007/2007_05813.htm) 2007 NY Slip Op
05813 [42 AD3d 627]. July 5, 2007.
51. ^ Drug Industry Document Archive (http://dida.library.ucsf.edu)
52. ^ Narrative Review: The Promotion of Gabapentin: An Analysis of Internal Industry Documents Steinman et al.
145 (4): 284 Annals of Internal Medicine (http://www.annals.org/cgi/content/full/145/4/284)
53. ^ http://thepharmaguide.com/content/view/5336/31/.
54. ^ Gabapentin Information and Uses - rxwiki.com
55. ^ Baillie, JK; Power, I (January 2006). "The mechanism of action of gabapentin in neuropathic pain". Curr Opin
Investig Drugs 7 (1): 339. ISSN 1472-4472 (https://www.worldcat.org/issn/1472-4472). PMID 16425669
(https://www.ncbi.nlm.nih.gov/pubmed/16425669).
56. ^ Jensen B, Regier LD, editors. RxFiles : Drug comparison charts. 7th ed. Saskatoon, SK: RxFiles, 2010; p.78
57. ^ Kjellsson MC, Ouellet D, Corrigan B, Karlsson MO (June 2011). "Modeling Sleep Data for a New Drug in
Development using Markov Mixed-Effects Models". Pharmaceutical Research 28 (10): 261027.
doi:10.1007/s11095-011-0490-x (http://dx.doi.org/10.1007%2Fs11095-011-0490-x). PMID 21681607
(https://www.ncbi.nlm.nih.gov/pubmed/21681607).
58. ^ Barbara Forney. "Gabapentin for Veterinary Use" (http://www.wedgewoodpetrx.com/learning-
center/professional-monographs/gabapentin-for-veterinary-use.html).
6/16/2014 Gabapentin - Wikipedia, the free encyclopedia
http://en.wikipedia.org/wiki/Neurotin 12/12
Pfizer
This page was last modified on 5 June 2014 at 03:37.
Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply.
By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia is a registered trademark
of the Wikimedia Foundation, Inc., a non-profit organization.