Pregabalin


Description

Pregabalin is an anticonvulsant drug used for neuropathic pain, epilepsy and generalized anxiety disorder.[

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Pharmacology

Indication

Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neurop... Read more

Pharmacodynamic

Pregabalin is structurally analogous to the inhibitory neurotransmitter gamma-aminobutyric acid (GAB... Read more

Mechanismofaction

Although the mechanism of action has not been fully elucidated, studies involving structurally relat... Read more

Absorption

Absorption of pregabalin is rapid and extensive reflecting it's relatively quick onset of efficacy.... Read more

Proteinbinding

Pregabalin is not plasma protein bound [ Read more

Volumeofdistribution

The apparent volume of distribution after oral administration is 0.5 L/kg. It is also likely that pr... Read more

Clearance

In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min. This r... Read more

Halflife

The elimination half life of pregabalin is roughly 6 hours [FDA Label].

Routeofelimination

Pregabalin is mainly renally excreted with 98% of the drug eliminated unchanged in the urine, while... Read more

Toxicity

In a systematic review that included 38 randomized controlled trials, there were 20 identified adver... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • Kind: experimental
    • Percent: 23-45%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 11-37%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 36%
  • Kind: placebo
    • Percent: 12%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 8-29%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 18-28%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 11-28%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 8-25%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 13-22%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 6-20%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 4-16%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 0-16%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: 5-16%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 7-15%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 10-14%
  • Kind: placebo
    • Percent: 12%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 3-14%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Weight increased US
  • Kind: experimental
    • Percent: 8-14%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 4-12%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 5-12%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Diplopia US
  • Kind: experimental
    • Percent: 5-12%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Vision blurred US
  • Kind: experimental
    • Percent: 7-12%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 3-11%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: 7-11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4-10%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Balance disorder US
  • Kind: experimental
    • Percent: 2-9%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Neuropathy US
  • Kind: experimental
    • Percent: 2-9%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 5-9%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 1-9%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Blurry vision US
  • Kind: experimental
    • Percent: 1-9%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Thinking abnormal US
  • Kind: experimental
    • Percent: 4-9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 6-9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 5-9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nasopharyngitis US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Abnormal Gait US
  • Kind: experimental
    • Percent: 0-8%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 5-8%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Increased appetite US
  • Kind: experimental
    • Percent: 3-7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Euphoric mood US
  • Kind: experimental
    • Percent: 2-7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vision blurred US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 2-7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: 1-7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 1-7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 1-7%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Speech Disorder US
  • Kind: experimental
    • Percent: 1-7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 2-7%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial

    Contraindications

    • Recommended Actions:
      • avoid
    • Regions: US
    • Patient Conditions:
        • Name: Drug Hypersensitivity
        • Drugbank Id: DBCOND0032673

    Food Interactions

    • Avoid alcohol (may increase CNS effects).
    • When taken with food, Cmax decreases, while Tmax is prolonged. Despite these observations, the total absorption of pregabalin is not effected to a clinically relevant degree. Pregabalin can be taken with or without food.

    Interactions

    Type in a drug name to check for interaction with Pregabalin

    The metabolism of (R)-warfarin can be decreased when combined with Pregabalin.
    The metabolism of (S)-Warfarin can be decreased when combined with Pregabalin.
    The risk or severity of hypoglycemia can be increased when Pregabalin is combined with 2,4-thiazolidinedione.
    The therapeutic efficacy of 2,5-Dimethoxy-4-ethylthioamphetamine can be increased when used in combination with Pregabalin.
    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.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Pregabalin.
    The therapeutic efficacy of 4-Bromo-2,5-dimethoxyamphetamine can be increased when used in combination with Pregabalin.
    The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be increased when used in combination with Pregabalin.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Pregabalin.
    The therapeutic efficacy of 4-Methoxyamphetamine can be increased when used in combination with Pregabalin.
    The metabolism of 5-androstenedione can be decreased when combined with Pregabalin.
    The therapeutic efficacy of 5-methoxy-N,N-dimethyltryptamine can be increased when used in combination with Pregabalin.
    The metabolism of Pregabalin can be decreased when combined with 6-Deoxyerythronolide B.
    Pregabalin may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Pregabalin may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of Pregabalin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The therapeutic efficacy of 7-Nitroindazole can be increased when used in combination with Pregabalin.
    The therapeutic efficacy of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be increased when used in combination with Pregabalin.
    Pregabalin may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Pregabalin may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.

    References

    • 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 . 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 . 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 . 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 . 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 . 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 . 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 . Ben-Menachem E: Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8. [PubMed: 15315511]
    • 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 . 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 . 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 . 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 . 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 . 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 . 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 . Pfizer [Link]

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