Peringatan Keamanan

The oral TDLo of gabapentin in humans is 2.86 mg/kg and the LD50 in rats has been found to be >8000 mg/kg.L8765 Symptoms of overdose are consistent with the drug's adverse effect profile and involve CNS depression (e.g. dizziness, drowsiness, slurred speech, lethargy, loss of consciousness) and gastrointestinal symptoms such as diarrhea.L8726,L8720 Management of overdose should involve symptomatic and supportive treatment. Gabapentin can be removed by hemodialysis - this may be of benefit in some patients, such as those with impaired renal function.L8741

Multi-drug overdoses involving gabapentin, particularly in combination with other CNS depressants such as opioids, can result in coma and death - this possibility should be considered when managing overdosage.L8720

Gabapentin

DB00996

small molecule approved investigational

Deskripsi

Gabapentin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) that was first approved for use in the United States in 1993.L8717 It was originally developed as a novel anti-epileptic for the treatment of certain types of seizuresA186277,A186143 - today it is also widely used to treat neuropathic pain.A14097,A186179 Gabapentin has some stark advantages as compared with other anti-epileptics, such as a relatively benign adverse effect profile, wide therapeutic index, and lack of appreciable metabolism making it unlikely to participate in pharmacokinetic drug interactions.A186143,A185981,L8717. It is structurally and functionally related to another GABA derivative, pregabalin.

Struktur Molekul 2D

Berat 171.2368
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination t<sub>1/2</sub> of gabapentin in patients with normal renal function is 5-7 hours.[L8717,L8720,A186143] In patients with reduced renal function, the elimination t<sub>1/2</sub> may be prolonged - in patients with a creatinine clearance of <30 mL/min, the reported half-life of gabapentin was approximately 52 hours.[L8717,L8720]
Volume Distribusi The apparent volume of distribution of gabapentin after IV administration is 58±6 L.[L8717,L8720] The drug is found in the CSF in concentrations approximately 9-20% of the corresponding plasma concentrations and is secreted into breast milk in concentrations similar to that seen in plasma.[L8717,L8720,A186143]
Klirens (Clearance) Both the plasma clearance and renal clearance of gabapentin are directly proportional to the patient's creatinine clearance due to its primarily renal elimination.[L8717,L8720,A186143]

Absorpsi

Absorption of gabapentin is thought to occur solely via facilitated transport by the LAT1 transporter within the intestines.A186143 As this process is saturable, the oral bioavailability of gabapentin is inversely proportional to the administered dose - the oral bioavailability of a 900mg/day regimen is approximately 60%, whereas a 4800mg/day regimen results in only 27% bioavailability.L8717,L8726 The Tmax of gabapentin has been estimated to be 2-3 hours.L8720,A186143 Food has no appreciable effect on gabapentin absorption.L8717,L8726

Metabolisme

Gabapentin is not appreciably metabolized in humansL8717,L8720 - in humans, metabolites account for less than 1% of an administered dose, with the remainder being excreted as unchanged parent drug in the urine.A186143

Rute Eliminasi

Gabapentin is eliminated solely in the urine as unchanged drug.L8717,L8720 Cimetidine, an inhibitor of renal tubular secretion, reduces clearance by approximately 12%, suggesting that some degree of tubular secretion is involved in the renal elimination of gabapentin.A186143

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Gabapentin possesses CNS depressant activity that may be potentiated by co-administration with alcohol.
  • 2. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

823 Data
Buprenorphine Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Magnesium sulfate The therapeutic efficacy of Gabapentin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Gabapentin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Mirtazapine Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Orphenadrine Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Pramipexole Gabapentin may increase the sedative activities of Pramipexole.
Ropinirole Gabapentin may increase the sedative activities of Ropinirole.
Rotigotine Gabapentin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Gabapentin.
Sodium oxybate Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Thalidomide Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Gabapentin can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Gabapentin can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Gabapentin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Gabapentin may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Gabapentin.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Gabapentin.
Ethanol Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Gabapentin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Zimelidine The risk or severity of adverse effects can be increased when Gabapentin is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Gabapentin is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Gabapentin is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Gabapentin is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Gabapentin is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Gabapentin is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Gabapentin is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Gabapentin is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Gabapentin is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Gabapentin is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Gabapentin is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Gabapentin is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Gabapentin is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Gabapentin is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Gabapentin is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Gabapentin is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Gabapentin is combined with Alaproclate.
Trazodone The risk or severity of adverse effects can be increased when Gabapentin is combined with Trazodone.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Gabapentin.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Gabapentin.
Gallamine triethiodide The risk or severity of CNS depression can be increased when Gallamine triethiodide is combined with Gabapentin.
Rocuronium The risk or severity of CNS depression can be increased when Rocuronium is combined with Gabapentin.
Doxacurium The risk or severity of CNS depression can be increased when Gabapentin is combined with Doxacurium.
Mivacurium The risk or severity of CNS depression can be increased when Gabapentin is combined with Mivacurium.
Metocurine The risk or severity of CNS depression can be increased when Gabapentin is combined with Metocurine.
Pancuronium The risk or severity of CNS depression can be increased when Gabapentin is combined with Pancuronium.
Pipecuronium The risk or severity of CNS depression can be increased when Gabapentin is combined with Pipecuronium.
Rapacuronium The risk or severity of CNS depression can be increased when Gabapentin is combined with Rapacuronium.
Cocaine The risk or severity of methemoglobinemia can be increased when Gabapentin is combined with Cocaine.
Quinidine The therapeutic efficacy of Gabapentin can be decreased when used in combination with Quinidine.
Zopiclone The risk or severity of adverse effects can be increased when Gabapentin is combined with Zopiclone.
Efavirenz The risk or severity of CNS depression can be increased when Efavirenz is combined with Gabapentin.
Melatonin The risk or severity of CNS depression can be increased when Gabapentin is combined with Melatonin.
Dantrolene The risk or severity of CNS depression can be increased when Gabapentin is combined with Dantrolene.
Alprenolol The risk or severity of CNS depression can be increased when Alprenolol is combined with Gabapentin.
Pindolol The risk or severity of CNS depression can be increased when Pindolol is combined with Gabapentin.
Penbutolol The risk or severity of CNS depression can be increased when Gabapentin is combined with Penbutolol.
Periciazine The risk or severity of CNS depression can be increased when Gabapentin is combined with Periciazine.
Thioproperazine The risk or severity of CNS depression can be increased when Gabapentin is combined with Thioproperazine.
Urapidil The risk or severity of CNS depression can be increased when Gabapentin is combined with Urapidil.
Metocurine iodide The risk or severity of CNS depression can be increased when Metocurine iodide is combined with Gabapentin.
Cisatracurium The risk or severity of CNS depression can be increased when Cisatracurium is combined with Gabapentin.
Atracurium besylate The risk or severity of CNS depression can be increased when Atracurium besylate is combined with Gabapentin.
Tubocurarine The risk or severity of CNS depression can be increased when Gabapentin is combined with Tubocurarine.
Vecuronium The risk or severity of CNS depression can be increased when Gabapentin is combined with Vecuronium.
Atracurium The risk or severity of CNS depression can be increased when Gabapentin is combined with Atracurium.
Gallamine The risk or severity of CNS depression can be increased when Gabapentin is combined with Gallamine.
Alcuronium The risk or severity of CNS depression can be increased when Gabapentin is combined with Alcuronium.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Gabapentin.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Gabapentin.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Gabapentin.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Gabapentin.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Gabapentin.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Gabapentin.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Gabapentin.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Gabapentin.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Gabapentin.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Gabapentin.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Gabapentin.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Gabapentin.
Codeine The risk or severity of CNS depression can be increased when Codeine is combined with Gabapentin.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Gabapentin.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Gabapentin.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Gabapentin.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Gabapentin.
Chlorzoxazone The risk or severity of CNS depression can be increased when Chlorzoxazone is combined with Gabapentin.
Thiethylperazine The risk or severity of CNS depression can be increased when Thiethylperazine is combined with Gabapentin.

Target Protein

Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1
Gamma-aminobutyric acid type B receptor subunit 2 GABBR2
Gamma-aminobutyric acid type B receptor subunit 1 GABBR1
Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2
Voltage-dependent N-type calcium channel CACNA1B
Adenosine receptor A1 ADORA1
Potassium voltage-gated channel subfamily KQT member 3 KCNQ3
Potassium voltage-gated channel subfamily KQT member 5 KCNQ5

Referensi & Sumber

Synthesis reference: Donald E. Butler, Barbara J. Greenman, "Gabapentin mohohydrate and a process for producing the same." U.S. Patent US4960931, issued May, 1978.
Artikel (PubMed)
  • PMID: 22240839
    Yagi T, Naito T, Mino Y, Umemura K, Kawakami J: Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects. Drug Metab Pharmacokinet. 2012;27(2):248-54. Epub 2012 Jan 13.
  • PMID: 15638774
    Czapinski P, Blaszczyk B, Czuczwar SJ: Mechanisms of action of antiepileptic drugs. Curr Top Med Chem. 2005;5(1):3-14. doi: 10.2174/1568026053386962.
  • PMID: 18397299
    Patsalos PN, Berry DJ, Bourgeois BF, Cloyd JC, Glauser TA, Johannessen SI, Leppik IE, Tomson T, Perucca E: Antiepileptic drugs--best practice guidelines for therapeutic drug monitoring: a position paper by the subcommission on therapeutic drug monitoring, ILAE Commission on Therapeutic Strategies. Epilepsia. 2008 Jul;49(7):1239-76. doi: 10.1111/j.1528-1167.2008.01561.x.
  • PMID: 26844734
    Abou-Khalil BW: Antiepileptic Drugs. Continuum (Minneap Minn). 2016 Feb;22(1 Epilepsy):132-56. doi: 10.1212/CON.0000000000000289.
  • PMID: 20818832
    Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P: A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinet. 2010 Oct;49(10):661-9. doi: 10.2165/11536200-000000000-00000.
  • PMID: 16141215
    Goto M, Miyahara I, Hirotsu K, Conway M, Yennawar N, Islam MM, Hutson SM: Structural determinants for branched-chain aminotransferase isozyme-specific inhibition by the anticonvulsant drug gabapentin. J Biol Chem. 2005 Nov 4;280(44):37246-56. Epub 2005 Sep 1.
  • PMID: 23567998
    Dickens D, Webb SD, Antonyuk S, Giannoudis A, Owen A, Radisch S, Hasnain SS, Pirmohamed M: Transport of gabapentin by LAT1 (SLC7A5). Biochem Pharmacol. 2013 Jun 1;85(11):1672-83. doi: 10.1016/j.bcp.2013.03.022. Epub 2013 Apr 6.
  • PMID: 17067834
    Maneuf YP, Luo ZD, Lee K: alpha2delta and the mechanism of action of gabapentin in the treatment of pain. Semin Cell Dev Biol. 2006 Oct;17(5):565-70. Epub 2006 Sep 24.
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