Peringatan Keamanan

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 disorder, incoordination, ataxia, blurred vision, diplopia, amblyopia, somnolence, confusional state, tremor, disturbance in attention, abnormal thinking, asthenia, fatigue, euphoria, edema, peripheral edema, dry mouth, and constipation A175876.

The most common symptoms of pregabalin toxicity (dose range includes 800 mg/day and single doses up to 11,500 mg) include somnolence, confusion, restlessness, agitation, depression, affective disorder and seizures.L9052

Since there is no antidote for pregabalin overdose, patients should receive general supportive care. If appropriate, gastric lavage or emesis may help eliminate unabsorbed pregabalin (healthcare providers should take standard precautions to maintain the airway).L9052

Pregabalin pharmacokinetic properties suggest that extra-corporeal elimination methods including haemodialysis, may be useful in situations of severe toxicity.A187105 However, there are cases where patients have presented with very high serum levels of pregabalin and have been successfully managed with supportive care alone.A187105

Pregabalin

DB00230

small molecule approved investigational

Deskripsi

Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.A173995 It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.A187190 Although as per the FDA Label the mechanism of action has not been definitively characterized, there is evidence that pregabalin exerts its effects by binding to the ?2? subunit of voltage-dependent calcium channels.A187190,L7066 Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).L1006,L7066 It may have dependence liability if misused but the risk appears to be highest in patients with current or past substance use disorders.A31161

Struktur Molekul 2D

Berat 159.2261
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 half life of pregabalin is 6.3 hours.[L7066]
Volume Distribusi After oral administration of pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg.[L7066] Although pregabalin is not very lipophilic, it is able to cross the blood brain barrier(BBB).[A175894] System L transporters facilitate the transport of large amino acids across the BBB and it has been confirmed that pregabalin is a substrate.[L7066,A175894] This information suggests that system L transporters are responsible for pregabalin uptake into the BBB.[A175894] In rat models, pregabalin has been shown to cross the placenta.[L7066]
Klirens (Clearance) In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min.[L7066] Given pregabalin's lack of plasma protein binding, this clearance rate suggests that renal tubular reabsorption is involved.[L7066]

Absorpsi

After oral dosing administered in the fasted state, pregabalin absorption is rapid, and extensive.A31165 Pregabalin oral bioavailability is reported to be ?90% regardless of the dose.A31165 Cmax is attained within 1.5 hours after single or multiple doses, and steady state is attained within 24-48 hours with repeated administration.A31165,L7066 Both Cmax and AUC appear to be dose proportional.A31165 Food decreases the rate of pregabalin absorption and as a result, lowers the Cmax by an estimated 25-30% and increases the Tmax to approximately 3 hours.L7066 However, the effect of food does not appear to impact the total absorption of pregabalin in a way that is clinically relevant. As a result, pregabalin can be administered with or without food.L7066

Metabolisme

Less than 2% of pregabalin is metabolized and it is excreted virtually unchanged in the urine.A31165,L7066

Rute Eliminasi

Pregabalin is almost exclusively eliminated in the urine.A187093,A187096 Further, based on preclinical studies, pregabalin does not appear to undergo racemization to the R enantiomer in the body.A31168

Interaksi Makanan

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

Interaksi Obat

1789 Data
Ceritinib Pregabalin may increase the bradycardic activities of Ceritinib.
Ivabradine Pregabalin may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Pregabalin.
Buprenorphine Pregabalin 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 Pregabalin.
Magnesium sulfate The therapeutic efficacy of Pregabalin can be increased when used in combination with Magnesium sulfate.
Metyrosine Pregabalin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.
Pramipexole Pregabalin may increase the sedative activities of Pramipexole.
Ropinirole Pregabalin may increase the sedative activities of Ropinirole.
Suvorexant Pregabalin 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 Pregabalin.
Thalidomide Pregabalin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Pregabalin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Pregabalin can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Pregabalin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Pregabalin 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 Pregabalin.
Troglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Troglitazone.
Rosiglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Rosiglitazone.
Pioglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Pioglitazone.
Lobeglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Lobeglitazone.
Netoglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Netoglitazone.
Rivoglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Rivoglitazone.
Ciglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Ciglitazone.
Balaglitazone The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Balaglitazone.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Pregabalin.
Ethanol Pregabalin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Pregabalin 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 Pregabalin.
Benzatropine The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Benzatropine.
Buclizine The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Buclizine.
Propantheline Pregabalin may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Pregabalin may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Tolterodine The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Tolterodine.
Flavoxate Pregabalin may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Pregabalin may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Solifenacin The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Solifenacin.
Fesoterodine Pregabalin may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Pregabalin may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Imidafenacin Pregabalin may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Pregabalin may decrease the excretion rate of Propiverine which could result in a higher serum level.
Disopyramide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Disopyramide.
Hyoscyamine The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Hyoscyamine.
Atropine The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Atropine.
Nicardipine Pregabalin may increase the bradycardic activities of Nicardipine.
Trimebutine Pregabalin may increase the bradycardic activities of Trimebutine.
Otilonium The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Otilonium.
Insulin pork The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin pork.
Acetohexamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Acetohexamide.
Phenformin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Phenformin.
Gliquidone The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Gliquidone.
Mitiglinide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Mitiglinide.
Glisoxepide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Glisoxepide.
Glymidine The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Glymidine.
AICA ribonucleotide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with AICA ribonucleotide.
Buformin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Buformin.
Voglibose The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Voglibose.
NN344 The risk or severity of hypoglycemia can be increased when Pregabalin is combined with NN344.
Glibornuride The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Glibornuride.
Benfluorex The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Benfluorex.
Albiglutide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Albiglutide.
Dulaglutide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Dulaglutide.
Insulin beef The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin beef.
Insulin degludec The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin degludec.
Insulin peglispro The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin peglispro.
Insulin tregopil The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin tregopil.
Ipragliflozin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Ipragliflozin.
Tofogliflozin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Tofogliflozin.
2,4-thiazolidinedione The risk or severity of hypoglycemia can be increased when Pregabalin is combined with 2,4-thiazolidinedione.
Sotagliflozin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Sotagliflozin.
Remogliflozin etabonate The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Remogliflozin etabonate.
Carbutamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Carbutamide.
Guar gum The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Guar gum.
Metahexamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Metahexamide.
Semaglutide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Semaglutide.
Taspoglutide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Taspoglutide.
Englitazone The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Englitazone.
Tirzepatide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Tirzepatide.
Gastric inhibitory polypeptide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Gastric inhibitory polypeptide.
Insulin human The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin human.
Insulin lispro The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin lispro.
Insulin glargine The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin glargine.
Miglitol The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Miglitol.
Gliclazide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Gliclazide.
Exenatide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Exenatide.
Mecasermin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Mecasermin.
Pramlintide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Pramlintide.
Insulin aspart The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin aspart.
Insulin detemir The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin detemir.
Insulin glulisine The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Insulin glulisine.
Liraglutide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Liraglutide.
Acarbose The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Acarbose.
Metformin The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Metformin.
Sulfadiazine The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Sulfadiazine.
Chlorpropamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Chlorpropamide.
Nateglinide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Nateglinide.
Tolazamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Tolazamide.
Glipizide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Glipizide.
Tolbutamide The risk or severity of hypoglycemia can be increased when Pregabalin is combined with Tolbutamide.

Target Protein

Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1

Referensi & Sumber

Synthesis reference: Mark Burk, "Asymmetric synthesis of pregabalin." U.S. Patent US20030212290, issued November 13, 2003.
Artikel (PubMed)
  • PMID: 16050051
    Authors unspecified: Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist. 2005 Jul 28;70(144):43633-5.
  • PMID: 15769862
    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.
  • PMID: 21651903
    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.
  • PMID: 28988943
    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.
  • PMID: 9283683
    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.
  • PMID: 27642577
    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.
  • PMID: 20444880
    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.
  • PMID: 15315511
    Ben-Menachem E: Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8.
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