Gabapentin: pharmacology and its use in pain management

Anaesthesia - Tập 57 Số 5 - Trang 451-462 - 2002
Michael Rose1, Peter Kam2
1Department of Anaesthesia and Pain Management, University of Sydney at Royal North Shore Hospital, St. Leonards, NSW 2065, Australia
2Associate Professor, Department of Anaesthesia and Pain Management, University of␣Sydney at Royal North Shore Hospital, St Leonards, NSW 2065, Australia

Tóm tắt

Summary Although its exact mode of action is not known, gabapentin appears to have a unique effect on voltage‐dependent calcium ion channels at the postsynaptic dorsal horns and may, therefore, interrupt the series of events that possibly leads to the experience of a neuropathic pain sensation. Gabapentin is especially effective at relieving allodynia and hyperalgesia in animal models. It has been shown to be efficacious in numerous small clinical studies and case reports in a wide variety of pain syndromes. Gabapentin has been clearly demonstrated to be effective for the treatment of neuropathic pain in diabetic neuropathy and postherpetic neuralgia. This evidence, combined with its favourable side‐effect profile in various patient groups (including the elderly) and lack of drug interactions, makes it an attractive agent. Therefore, gabapentin should be considered an important drug in the management of neuropathic pain syndromes.

Từ khóa


Tài liệu tham khảo

Taylor CP, 1993, New Trends in Epilepsy Management: The Role of Gabapentin., 13

Satzinger G, 1994, Antiepileptics from gamma‐aminobutyric acid, Arzneimittelforchung, 44, 261

Bartoszyk GD, 1986, New Anticonvulsant Drugs, 147

10.1016/S0378-4347(00)83818-9

10.1016/S0378-4347(00)84064-5

10.1023/A:1018951214146

Vollmer KO, 1989, Pharmacokinetic model and absolute bioavailability of the new anticonvulsant gabapentin, Advances in Epileptology, 17, 209

Türck D, 1989, Dose‐linearity of the new anticonvulsant gabapentin after multiple oral doses, European Journal of Clinical Pharmacology, 36, A310

Richens A, 1993, New Trends in Epilepsy Management: The Role of Gabapentin, 41

10.1111/j.1365-2125.1991.tb05507.x

Vollmer KO, 1986, Pharmacokinetics and metabolism of gabapentin in rat, dog and man, Arzneimittel-Forschung/Drug Research, 36, 830

10.1016/0920-1211(92)90020-T

Ojemann LM, 1988, Gabapentin concentrations in human brain. Abstract, Epilepsia, 29, 694

Comstock TJ, 1990, Gabapentin pharmacokinetics in patients with various degrees of renal function, Journal of Clinical Pharmacology, 30, 862

Schmidt B, 1989, Antiepileptic Drug, 925

Anhut H, 1988, Drug interaction study of the new anticonvulsant gabapentin with phenytoin in epileptic patients, Abstract Naunyn-Schmiedeberg's Archives of Pharmacology, 337, R127

Graves NM, 1989, Pharmacokinetics of gabapentin in patients treated with phenytoin, Pharmacotherapy, 9, 196

10.1002/j.1552-4604.1995.tb05020.x

Busch JA, 1992, Effect of Maalox TC on single‐dose pharmacokinetics of gabapentin capsules in healthy subjects, Pharmaceutical Research, 9, S

10.1016/0922-4106(93)90156-4

10.1016/0920-1211(93)90078-L

10.1016/0922-4106(93)90155-3

10.1016/0920-1211(93)90070-N

10.1016/0304-3940(91)90249-S

10.1002/ana.410390114

10.1016/0014-2999(83)90425-9

Schlicker E, 1985, Gabapentin decreases monoamine release without affecting acetylcholine release in the brain, Arzneimittel-Forschung, 35, 1347

10.1016/0920-1211(94)90074-4

Abdi S, 1998, The anti‐allodynic effects of amitryptyline, gabapentin and lidocaine in a rat model of neuropathic pain, Anesthesia and Analgesia, 87, 1360, 10.1213/00000539-199812000-00027

Pan HL, 1999, Gabapentin suppresses ectopic nerve discharges and reverses allodynia in neuropathic rats, Journal of Pharmacology and Experimental Therapeutics, 288, 1026

10.1038/sj.bjp.0701320

10.1016/S1098-7339(06)80010-6

10.1097/00000542-199801000-00028

10.1097/00000539-199908000-00034

10.1038/sj.bjp.0703530

10.1097/00000539-199802000-00025

10.1016/S0304-3959(98)00043-8

10.1016/S0920-1211(97)00084-3

10.1016/0920-1211(93)90023-Z

10.1016/0165-6147(90)90238-4

10.1523/JNEUROSCI.14-08-04882.1994

Field MJ, 1997, Evaluation of gabapentin and S‐(+)‐3‐isobutylgaba in a rat model of postoperative pain, Journal of Pharmacology and Experimental Therapeutics, 282, 1242

10.1016/S0006-8993(98)00890-7

10.1016/S0304-3959(98)00239-5

10.1038/sj.bjp.0703380

10.1016/S0304-3940(00)00769-2

Ramsay RE, 1995, Antiepileptic Drugs, 857

10.1111/j.1528-1157.1999.tb00804.x

10.1212/WNL.44.5.982

10.1097/00007691-199912000-00006

Gallay BJ, 2000, Reversible acute renal allograft dysfunction due to gabapentin, Transplantation, 70, 208

Gonzalez‐Sicilia L, 1998, Stevens–Johnson syndrome associated with gabapentin, American Journal of Medicine, 105, 455

10.1002/1097-4598(200008)23:8<1204::AID-MUS7>3.0.CO;2-H

Korn‐Merker E, 1999, Gabapentin in childhood epilepsy. A prospective evaluation of efficacy and safety, Epilepsy Research, 38, 57

10.1111/j.1528-1157.1994.tb05974.x

10.1111/j.1528-1157.1999.tb00927.x

10.1016/S0920-1211(99)00006-6

Saletu B, 1986, Evaluation of encephalotropic and psychotropic properties of gabapentin in man by pharmaco‐EEG and psychometry, International Journal of Clinical Pharmacology, Therapy and Toxicology, 24, 362

10.1017/S0317167100020916

10.1345/aph.19303

10.1016/S0304-3940(99)00057-9

10.1097/00000542-199910000-00021

10.1097/00000542-200002000-00033

10.1097/00002508-199709000-00011

10.1159/000007979

10.1016/S1098-7339(97)80037-5

10.1016/S1098-7339(98)90123-7

Vadivelu N, 1999, Neuropathic pain after anti‐HIV gene therapy successfully treated with gabapentin, Journal of Pain and Symptom Management, 17, 155

10.1016/0896-6974(96)89444-8

Hays H, 1999, Using gabapentin to treat neuropathic pain, Canadian Family Physician, 45, 2109

10.1001/jama.280.21.1831

10.1002/14651858.CD001133

10.1016/S0002-9343(00)00398-3

10.1001/archinte.159.16.1931

10.1016/S0885-3924(00)00181-0

10.1001/jama.280.21.1837

10.1016/S0885-3924(99)00033-0

Valzania F, 1998, Gabapentin in trigeminal neuralgia. Abstract, Neurology, 50, A379

10.1212/WNL.51.2.611

10.1159/000008192

10.1111/j.1600-0404.1991.tb04937.x

10.1016/S0003-9993(00)90135-7

10.1016/S0003-9993(97)90168-4

10.1177/135245859700300407

10.1212/WNL.51.2.609

Solaro C, 2000, Gabapentin is effective in treating nocturnal painful spasms in multiple sclerosis, Multiple Sclerosis, 6, 192, 10.1177/135245850000600310

10.1016/S0003-9993(97)90020-4

Waldman SD, 1990, Reflex sympathetic dystrophy, Internal Medicine Magazine, 11, 62

10.1016/0885-3924(95)00001-F

10.1016/S0887-8994(99)00139-3

Di Trapani G, 2000, Gabapentin in the prophylaxis of migraine: a double‐blind randomized placebo‐controlled study, La Clinica Therapeutica, 151, 145

10.1046/j.1468-2982.2000.00065.x

10.1046/j.1468-2982.2000.00046.x

10.1016/0304-3959(87)90176-X

Mercadante S, 1998, Gabapentin in spinal cord injury pain, Pain Clinics of America, 10, 203

10.1016/S0304-3959(98)00153-5

10.1053/apmr.2000.9166

10.1038/sj.sc.3100366

10.1038/sj.sc.3100481

Gatti A, 1998, Gabapentin in the treatment of distal symmetric axonopathy in HIV infected patients, Neurology, 50, A216

Newshan G, 1998, HIV neuropathy treated with gabapentin (letter), AIDS, 12, 219

10.1016/S0002-8703(38)90693-3

10.1097/00000542-199704000-00029

Zapp JJ, 1996, Postpoliomyelitis pain treated with gabapentin, American Family Physician, 53, 2445

10.1097/00007611-200093020-00021

10.1097/00002826-200001000-00008

10.1200/JCO.1999.17.1.434a

10.1159/000008068

10.1097/00000539-199912000-00026

10.1046/j.1526-4610.1999.3910761.x

10.1046/j.1524-4725.1999.08295.x

10.4088/JCP.v60n0911

10.1055/s-2007-979203

10.1592/phco.19.8.565.31521

10.4088/JCP.v60n0408

Bolts SR, 1999, Gabapentin and lamotrigine in bipolar disorder, American Journal of Health-System Pharmacy, 56, 1939, 10.1093/ajhp/56.19.1939

10.1016/S0165-0327(98)00198-0

10.3109/10401239909147073

10.1055/s-2007-979219

Brannon N, 2000, Gabapentin treatment for post‐traumatic stress disorder (letter), Canadian Journal of Psychiatry, 45, 84

10.1097/00004714-200002000-00015

10.1176/jnp.12.1.40

10.4088/JCP.v61n0114f

10.1016/S0887-8994(98)00166-0

10.1001/archneur.56.4.475

10.1163/156856900750228123

10.1111/j.1468-3083.1999.tb00890.x

10.1016/S0887-8994(99)00104-6

10.1016/S0885-3924(00)00218-9

10.1136/bmj.311.7012.1047

McQuay HJ, 1996, A systematic review of antidepressants in neuropathic pain, British Medical Journal, 68, 217