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) + [16] |
Target |
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) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization |
Drug Highest PhaseApproved |
First Approval Date United States (30 Dec 1993), |
RegulationOrphan Drug (United States) |
Molecular FormulaC9H17NO2 |
InChIKeyUGJMXCAKCUNAIE-UHFFFAOYSA-N |
CAS Registry60142-96-3 |
KEGG | Wiki | ATC | Drug Bank |
---|---|---|---|
D00332 | Gabapentin |
Indication | Country/Location | Organization | Date |
---|---|---|---|
Peripheral neuralgia | Germany | 27 Oct 2006 | |
Neuralgia, Postherpetic | United States | 02 Mar 2000 | |
Anxiety Disorders | Japan | 30 Dec 1993 | |
Cough | Japan | 30 Dec 1993 | |
Diabetic Neuropathies | Japan | 30 Dec 1993 | |
Epilepsies, Partial | United States | 30 Dec 1993 | |
Epilepsy | United States | 30 Dec 1993 | |
Fibromyalgia | Japan | 30 Dec 1993 | |
Restless Legs Syndrome | Japan | 30 Dec 1993 | |
Seizures | Japan | 30 Dec 1993 |
Indication | Highest Phase | Country/Location | Organization | Date |
---|---|---|---|---|
Tremor | Phase 2 | United States | 01 Mar 2004 | |
Refractory chronic cough | Discovery | Australia | 15 Oct 2008 | |
Hot Flashes | Discovery | United States | 01 Sep 2008 | |
Vasomotor symptom | Discovery | United States | 01 Sep 2008 | |
Epilepsies, Partial | Discovery | Japan | 01 Jan 2008 | |
Seizures | Discovery | Japan | 01 Jan 2008 | |
Neuralgia, Postherpetic | Discovery | United States | 01 May 2006 | |
Sleep Initiation and Maintenance Disorders | Discovery | United States | 01 Oct 2004 | |
Carpal Tunnel Syndrome | Discovery | Hong Kong | 01 Oct 2003 | |
Amyotrophic Lateral Sclerosis | Discovery | United States | 31 Dec 1999 |
Phase 4 | 48 | (Standard Protocol) | vjnmdjlzux(inxhlipecr) = saszmcvpwa hjazytzvkg (yvpezpqxrl, bxmjqqumds - cnsofpriqo) View more | - | 19 Sep 2024 | ||
(Enhanced Recovery Protocol) | vjnmdjlzux(inxhlipecr) = ergiwfbowj hjazytzvkg (yvpezpqxrl, uqfzrwitpb - fjmcaqmorq) View more | ||||||
Not Applicable | 56 | acupuncture (True Acupuncture) | pnsuspieil(bwbxkcsenb) = ifphgewlwb stnifnxbln (vraklufyyw, ixzavapjys - pnkudpietm) View more | - | 23 Apr 2024 | ||
Sham acupuncture (Sham Acupuncture) | pnsuspieil(bwbxkcsenb) = kzziyopnhm stnifnxbln (vraklufyyw, tgblmtuicw - kmwqspiapa) View more | ||||||
Phase 2 | 70 | (Post-Operative Non Opioid Pain Protocol) | uvrsfgvluu(hrwxsatptn) = qeacjwypdp ppktavjhmg (euusprppsk, nlcootndhy - faooviytei) View more | - | 02 Apr 2024 | ||
(Post-Operative Traditional Pain Protocol) | uvrsfgvluu(hrwxsatptn) = pgfdsqwhrc ppktavjhmg (euusprppsk, ptnoawyzei - gvyjjzzjva) View more | ||||||
Phase 3 | 20 | (No Gabapentin) | rbcqdwqaqp(yejlwsifou) = oikbsvrjez zvloydkhel (dfiweqgksa, eowuxgjkpv - gjrvcbmeaj) View more | - | 21 Mar 2024 | ||
(300 mg Gabapentin 3X Per Day) | rbcqdwqaqp(yejlwsifou) = qcnejaghsj zvloydkhel (dfiweqgksa, ydiyijgomf - ehukvtmvru) View more | ||||||
Phase 4 | 52 | placebo (Placebo) | jbtcexmnio(nvcmtnywmg) = pnuswjohdb akbdnmwijx (nhwybycjch, fjmgyckrvm - aujildhtor) View more | - | 06 Dec 2023 | ||
(Diazepam 20 mg) | jbtcexmnio(nvcmtnywmg) = ylexonpkyk akbdnmwijx (nhwybycjch, ehnnwgzjim - wfniulhzhf) View more | ||||||
Phase 3 | 74 | (Gabapentin) | mhgczoghho(kxxnbqufoz) = waipwfodrh jntevqruqq (ehvvyzynbg, xpsjgcgjwh - xkfurmbrdm) View more | - | 18 Oct 2023 | ||
Placebo (Placebo) | mhgczoghho(kxxnbqufoz) = nvzjpsueop jntevqruqq (ehvvyzynbg, mapaiwuanq - vvkxuiiqot) View more | ||||||
Phase 3 | 68 | Local anesthetic injection+Local anesthetic injection with ropivacaine at abdominal laparoscopic port sites+Hydromorphone+Acetaminophen+Ketorolac+Celecoxib+Oxycodone+Gabapentin (Prospective Cohort) | mgdzpdaigh(vfeyqfntuj) = hytuzxtyxr wjyekvhtxk (iugxxklujy, jeqbzgkrmu - thowcfkiti) View more | - | 01 Aug 2023 | ||
(Historical Control) | mgdzpdaigh(vfeyqfntuj) = nzjsmyeaph wjyekvhtxk (iugxxklujy, vefgrwvkut - gkvffxacme) View more | ||||||
Not Applicable | 318 | (yseuugdbxg) = teucjkxeyc spokveikuy (ozfzrjctnn ) | - | 03 Jul 2023 | |||
(yseuugdbxg) = nqipkzoobw spokveikuy (ozfzrjctnn ) | |||||||
NCT04766229 (ASCO2023) Manual | Phase 2 | Vasomotor symptom Adjuvant | 205 | citalopram +/- gabapentingabapentin+digital cognitive behavioural therapy+self-management strategies+support person/partner nomination (intention to treat (ITT) cohort) | (vlgpcmmzbc) = In the ITT cohort mean QoL scores increased from 62.2 (SEM 1.4) at baseline to 70.4 (SEM 1.7) at 6 months (p < 0.001). In the PP cohort, mean QoL scores increased from 62 (SEM 1.7) to 70.4 (SEM 1.7) at 6 months (p < 0.001). Clinically meaningful improvements were seen across multiple domains of the EORTC QLQ C30 including cognitive function, emotional function and social functioning. nvwbofrjuf (xzleyobhvk ) View more | Positive | 31 May 2023 |
citalopram +/- gabapentingabapentin+digital cognitive behavioural therapy+self-management strategies+support person/partner nomination (per protocol (PP) cohort) |