Description

Simple

A medication used to treat a variety of painful conditions caused by nerve damage and fibromyalgia and to treat some types of seizures.

Clinical

An anticonvulsant drug used to treat neuropathic pain conditions and fibromyalgia, and for the treatment of partial onset seizures in combination with other anticonvulsants.

Overview

Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.[13] It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.[20] Although as per the FDA Label the mechanism of action has not been definitively defined, there is evidence that pregabalin exerts its effects by binding to the α2δ subunit of voltage-dependent calcium channels.[20][22] Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).[21][22] It may have dependence liability if misused but the risk appears to be highest in patients with current or past substance use disorders.[Read more

Pharmacology

Indication

Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury, and as adjunctive therapy for the treatment of partial-onset seizures in patients 1 month of age a... Read more

Pharmacodynamic

Although the structure of pregabalin is similar to gamma-aminobutyric acid (GABA), it does not bind to GABA receptors.[ Read more

Mechanism of action

Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.[ Read more

Absorption

After oral dosing administered in the fasted state, pregabalin absorption is rapid, and extensive.[ 8] Pregabalin oral bioava... Read more

Protein binding

Pregabalin is not plasma protein bound.[8][22 Read more

Volume of distribution

After oral administration of pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg.[22]Although pregabalin is not very lipophilic, it is able to cross the blood brain barrier(BBB).[ Read more

Clearance

In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min.[22] Given pregabalin's lack of plasma protein binding, this clearance rate suggests that renal tubular reabsorption is invol... Read more

Half life

The elimination half life of pregabalin is 6.3 hours.[22]

Route of elimination

Pregabalin is almost exclusively eliminated in the urine.[17][ Read more

Toxicity

In a systematic review that included 38 randomized controlled trials, there were 20 identified adverse effects that were significantly associated with pregabalin, most of which involve the central nervous system and cognition. The identified adverse effects include vertigo, dizziness, balance disor... Read more

Adverse Effects

Contraindications

  • Sex Group: all
  • Regions: US
  • Patient Conditions:
      • Name: Pregabalin hypersensitivity
      • Drugbank Id: DBCOND0123241

Food Interactions

  • Avoid alcohol. Alcohol may increase CNS effects.
  • Take with or without food. Food alters drug absorption, but not to a clinically significant extent.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Pregabalin is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of 2,5-Dimethoxy-4-ethylthioamphetamine can be increased when used in combination with Pregabalin.
3-isobutyl-1-methyl-7H-xanthine
Pregabalin may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of 4-Bromo-2,5-dimethoxyamphetamine can be increased when used in combination with Pregabalin.
4-Methoxyamphetamine
The therapeutic efficacy of 4-Methoxyamphetamine can be increased when used in combination with Pregabalin.
5-methoxy-N,N-dimethyltryptamine
The therapeutic efficacy of 5-methoxy-N,N-dimethyltryptamine can be increased when used in combination with Pregabalin.
6-O-benzylguanine
Pregabalin may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Deazaguanine
Pregabalin may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Nitroindazole
The therapeutic efficacy of 7-Nitroindazole can be increased when used in combination with Pregabalin.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The therapeutic efficacy of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be increased when used in combination with Pregabalin.
7,9-Dimethylguanine
Pregabalin may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine
Pregabalin may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-chlorotheophylline
Pregabalin may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
9-Deazaguanine
Pregabalin may increase the excretion rate of 9-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
9-Methylguanine
Pregabalin may increase the excretion rate of 9-Methylguanine which could result in a lower serum level and potentially a reduction in efficacy.
Abacavir
Pregabalin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abexinostat
The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Abexinostat.
Acarbose
Pregabalin may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acebutolol
Pregabalin may increase the arrhythmogenic activities of Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Pregabalin which could result in a higher serum level.
23 References
  1. 1 . Authors unspecified: Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist. 2005 Jul 28;70(144):43633-5.PubMed: 16050051
  2. 2 . Su TZ, Feng MR, Weber ML: Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther. 2005 Jun;313(3):1406-15. Epub 2005 Mar 15.PubMed: 15769862
  3. 3 . Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, Cui M, Hoffman D, Donevan S: Pregabalin is a potent and selective ligand for alpha(2)delta-1 and alpha(2)delta-2 calcium channel subunits. Eur J Pharmacol. 2011 Sep 30;667(1-3):80-90. doi: 10.1016/j.ejphar.2011.05.054. Epub 2011 Jun 1.PubMed: 21651903
  4. 4 . Bonnet U, Scherbaum N: How addictive are gabapentin and pregabalin? A systematic review. Eur Neuropsychopharmacol. 2017 Oct 5. pii: S0924-977X(17)30897-0. doi: 10.1016/j.euroneuro.2017.08.430.PubMed: 28988943
  5. 5 . Field MJ, Oles RJ, Lewis AS, McCleary S, Hughes J, Singh L: Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents. Br J Pharmacol. 1997 Aug;121(8):1513-22.PubMed: 9283683
  6. 6 . Rajappa GC, Vig S, Bevanaguddaiah Y, Anadaswamy TC: Efficacy of Pregabalin as Premedication for Post-Operative Analgesia in Vaginal Hysterectomy. Anesth Pain Med. 2016 May 14;6(3):e34591. doi: 10.5812/aapm.34591. eCollection 2016 Jun.PubMed: 27642577
  7. 7 . Bender G, Florian JA Jr, Bramwell S, Field MJ, Tan KK, Marshall S, DeJongh J, Bies RR, Danhof M: Pharmacokinetic-pharmacodynamic analysis of the static allodynia response to pregabalin and sildenafil in a rat model of neuropathic pain. J Pharmacol Exp Ther. 2010 Aug;334(2):599-608. doi: 10.1124/jpet.110.166074. Epub 2010 May 5.PubMed: 20444880
  8. 8 . Ben-Menachem E: Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8.PubMed: 15315511
  9. 9 . Prompila N, Eiamart W, Jumroen Y, Sayankuldilok N, Chariyavilaskul P, Ketchat W, Wittayalertpanya S: Pharmacokinetics and bioequivalence of a pregabalin 150-mg capsule in healthy Thai subjects. Int J Clin Pharmacol Ther. 2017 Oct;55(10):811-817. doi: 10.5414/CP202954.PubMed: 28513426
  10. 10 . Hong T, Han S, Lee J, Jeon S, Yim DS: Comparison of oral absorption models for pregabalin: usefulness of transit compartment model. Drug Des Devel Ther. 2016 Dec 7;10:3995-4003. eCollection 2016.PubMed: 27994441
  11. 11 . Rodriguez J, Castaneda G, Munoz L: Direct determination of pregabalin in human urine by nonaqueous CE-TOF-MS. Electrophoresis. 2013 May;34(9-10):1429-36. doi: 10.1002/elps.201200564. Epub 2013 Apr 16.PubMed: 23463484
  12. 12 . Randinitis EJ, Posvar EL, Alvey CW, Sedman AJ, Cook JA, Bockbrader HN: Pharmacokinetics of pregabalin in subjects with various degrees of renal function. J Clin Pharmacol. 2003 Mar;43(3):277-83.PubMed: 12638396
  13. 13 . Gajraj NM: Pregabalin: its pharmacology and use in pain management. Anesth Analg. 2007 Dec;105(6):1805-15. doi: 10.1213/01.ane.0000287643.13410.5e.PubMed: 18042886
  14. 14 . Zaccara G, Gangemi P, Perucca P, Specchio L: The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials. Epilepsia. 2011 Apr;52(4):826-36. doi: 10.1111/j.1528-1167.2010.02966.x. Epub 2011 Feb 14.PubMed: 21320112
  15. 15 . Toth C: Pregabalin: latest safety evidence and clinical implications for the management of neuropathic pain. Ther Adv Drug Saf. 2014 Feb;5(1):38-56. doi: 10.1177/2042098613505614.PubMed: 25083261
  16. 16 . Takahashi Y, Nishimura T, Higuchi K, Noguchi S, Tega Y, Kurosawa T, Deguchi Y, Tomi M: Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line. Pharm Res. 2018 Oct 29;35(12):246. doi: 10.1007/s11095-018-2532-0.PubMed: 30374619
  17. 17 . Stump P: [Pregabalin--profile of efficacy and tolerability in neuropathic pain]. Drugs Today (Barc). 2009 Oct;45 Suppl C:19-27.PubMed: 20087482
  18. 18 . Lee DW, Lee HJ, Kim HJ, Chang SH, Park DJ: Two cases of pregabalin neurotoxicity in chronic kidney disease patients. NDT Plus. 2011 Apr;4(2):138. doi: 10.1093/ndtplus/sfq219.PubMed: 25984138
  19. 19 . Wood DM, Berry DJ, Glover G, Eastwood J, Dargan PI: Significant pregabalin toxicity managed with supportive care alone. J Med Toxicol. 2010 Dec;6(4):435-7. doi: 10.1007/s13181-010-0052-3.PubMed: 20373065
  20. 20 . Cross AL, Sherman Al: Pregabalin .PubMed: 29261857
  21. 21 . Pfizer Link
  22. 22 . FDA Label Pregabalin Link
  23. 23 . Pfizer Medical Information - Lyrica Link