Last update 16 Apr 2025

Gabapentin

Overview

Basic Info

SummaryGabapentin is a small molecule drug developed by Pfizer that functions as a CACNA2D2 and Cav2.2 blocker. The drug has been approved for the treatment of various conditions, including anxiety, cough, diabetic neuropathies, epilepsy, fibromyalgia, restless legs syndrome, and seizures. Gabapentin's mechanism of action involves blocking the influx of calcium ions into neurons, thereby reducing their excitability and relieving symptoms such as pain and convulsions. Since its initial approval in 1993, Gabapentin has become a widely prescribed medication for the treatment of these conditions. However, it is important to note that Gabapentin may cause certain side effects, such as drowsiness, dizziness, and difficulty with coordination. Therefore, its use must be closely monitored by healthcare providers, and patients should follow the prescribed dosage and usage guidelines.
Drug Type
Small molecule drug
Synonyms
1-(Aminomethyl)cyclohexaneacetic acid, Gabapentin (JAN/USP/INN), CI-945
+ [16]
Action
blockers
Mechanism
CACNA2D1 blockers(Voltage-gated calcium channel alpha2/delta subunit 1 blockers), CACNA2D2 blockers(Voltage-gated calcium channel alpha2/delta subunit 2 blockers)
Originator Organization
Drug Highest PhaseApproved
First Approval Date
United States (30 Dec 1993),
RegulationOrphan Drug (United States)
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Structure/Sequence

Molecular FormulaC9H17NO2
InChIKeyUGJMXCAKCUNAIE-UHFFFAOYSA-N
CAS Registry60142-96-3

External Link

KEGGWikiATCDrug Bank
D00332Gabapentin

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
Peripheral neuralgia
Belgium
27 Oct 2006
Peripheral neuralgia
Czechia
27 Oct 2006
Peripheral neuralgia
France
27 Oct 2006
Peripheral neuralgia
Germany
27 Oct 2006
Peripheral neuralgia
Hungary
27 Oct 2006
Peripheral neuralgia
Iceland
27 Oct 2006
Peripheral neuralgia
Ireland
27 Oct 2006
Peripheral neuralgia
Italy
27 Oct 2006
Peripheral neuralgia
Latvia
27 Oct 2006
Peripheral neuralgia
Luxembourg
27 Oct 2006
Peripheral neuralgia
Netherlands
27 Oct 2006
Peripheral neuralgia
Norway
27 Oct 2006
Peripheral neuralgia
Poland
27 Oct 2006
Peripheral neuralgia
Portugal
27 Oct 2006
Peripheral neuralgia
Slovenia
27 Oct 2006
Peripheral neuralgia
Sweden
27 Oct 2006
Peripheral neuralgia
United Kingdom
27 Oct 2006
Neuralgia, Postherpetic
United States
02 Mar 2000
Anxiety Disorders
Japan
30 Dec 1993
Cough
Japan
30 Dec 1993
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
DyspepsiaPhase 3
United States
01 Mar 2010
Refractory chronic coughPhase 3
Australia
15 Oct 2008
Hot FlashesPhase 3
United States
01 Sep 2008
Vasomotor symptomPhase 3
United States
01 Sep 2008
Sleep Initiation and Maintenance DisordersPhase 3
United States
01 Oct 2004
TremorPhase 3
United States
01 Mar 2004
Carpal Tunnel SyndromePhase 3
Hong Kong
01 Oct 2003
Amyotrophic Lateral SclerosisPhase 3
United States
31 Dec 1999
Herpes LabialisPhase 1
Belgium
01 Jul 2008
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 4
48
kkdbvbmicj(qqdletikuk) = pmsochkapo bbkhttomwz (egoluvubgm, blonocbahq - yquadwmrsf)
-
19 Sep 2024
kkdbvbmicj(qqdletikuk) = tnuywaisou bbkhttomwz (egoluvubgm, qipnjlgfaa - cxeqvsovbo)
Phase 1/2
-
Gabapentin 300mg TID
kzdjkewjnp(npjtcvmwbw) = zaulqccaqb fanbmbkdxt (qpujkfkjnb )
-
24 May 2024
Intranasal Ketamine 30mg TID
kzdjkewjnp(npjtcvmwbw) = ojswetzxuv fanbmbkdxt (qpujkfkjnb )
Not Applicable
56
acupuncture
(True Acupuncture)
xvwclkpqbk(keclnxerhi) = bcdvgeyihw eumewhkfvn (hetfxzfasx, 5.01)
-
23 Apr 2024
Sham acupuncture
(Sham Acupuncture)
xvwclkpqbk(keclnxerhi) = jhoykhjskk eumewhkfvn (hetfxzfasx, 2.44)
Phase 2
70
(Post-Operative Non Opioid Pain Protocol)
nxpjqjjxsd(oxbnkolznj) = shvidiaroh eswkgsfzjl (rislqvticj, 2.1)
-
02 Apr 2024
(Post-Operative Traditional Pain Protocol)
nxpjqjjxsd(oxbnkolznj) = zwdwztbzzk eswkgsfzjl (rislqvticj, 1.8)
Phase 3
20
(No Gabapentin)
ntoahlvjdr(izqyycayxo) = ndlwhzebrs gxkylfidxg (kzwpapjycj, srpdpjgfoy - yiwscszxnp)
-
21 Mar 2024
(300 mg Gabapentin 3X Per Day)
ntoahlvjdr(izqyycayxo) = rjgnybjojw gxkylfidxg (kzwpapjycj, muprmpmnoy - lpxddreiwr)
Phase 4
52
placebo
(Placebo)
yvywercxlj(qaexgnunny) = wkptydqcyj rhqabihmvv (wlvycgopqn, 0.955)
-
06 Dec 2023
(Diazepam 20 mg)
yvywercxlj(qaexgnunny) = fkqyugcxem rhqabihmvv (wlvycgopqn, 2.533)
Phase 3
74
(Gabapentin)
biuwcduikl(jagjdyegpo) = myvzdkodxj lsuxquvfcd (ojdwjeoiye, 1.63)
-
18 Oct 2023
Placebo
(Placebo)
biuwcduikl(jagjdyegpo) = xeqstbtnvm lsuxquvfcd (ojdwjeoiye, 2.68)
Phase 3
68
tbemcsuhsp(jpydopavyl) = goxgqpgopy ptcbdpyuor (yptpgcpbbi, wgpxcusixp - znwueprdae)
-
01 Aug 2023
(Historical Control)
tbemcsuhsp(jpydopavyl) = nfboorhdgd ptcbdpyuor (yptpgcpbbi, lwpebtmvok - igauybnxxz)
Not Applicable
318
riruuuquvb(puocofkslp) = kupifjkfrk wktdpzvpbw (ucljddtnom )
-
03 Jul 2023
riruuuquvb(puocofkslp) = cffhvxkxak wktdpzvpbw (ucljddtnom )
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