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definition - Pregabalin

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Pregabalin

                   
Pregabalin
Systematic (IUPAC) name
(S)-3-(aminomethyl)-5-methylhexanoic acid
Clinical data
Trade names Lyrica
AHFS/Drugs.com monograph
MedlinePlus a605045
Licence data US Daily Med:link
Pregnancy cat. B3 (Au), C (U.S.)
Legal status S4 (Au), POM (UK), Schedule V (U.S.)
Routes Oral(main), IV, Insufflation
Pharmacokinetic data
Bioavailability ≥90%
Protein binding Nil
Metabolism Negligible
Half-life 5–6.5 hours
Excretion Renal
Identifiers
CAS number 148553-50-8 YesY
ATC code N03AX16
PubChem CID 5486971
DrugBank DB00230
ChemSpider 4589156 YesY
UNII 55JG375S6M YesY
KEGG D02716 YesY
ChEBI CHEBI:64356 YesY
ChEMBL CHEMBL1059 YesY
Synonyms PD-144,723
Chemical data
Formula C8H17NO2 
Mol. mass 159.23 g.mol-1
 YesY (what is this?)  (verify)

Pregabalin (INN) (play /prɨˈɡæbəlɨn/) is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults.[1] It has also been found effective for generalized anxiety disorder and is (as of 2007) approved for this use in the European Union.[1] It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica. Pfizer described in an SEC filing that the drug could be used to treat epilepsy, post-herpetic neuralgia and diabetic peripheral neuropathy, fibromyalgia, et al. Sales reached a record $3.063 billion in 2010.[2]

Recent studies have shown that pregabalin is effective at treating chronic pain in disorders such as fibromyalgia[3] and spinal cord injury.[4] In June 2007, pregabalin became the first medication approved by the U.S. Food and Drug Administration specifically for the treatment of fibromyalgia.[5]

It is considered to have a low potential for abuse, and a limited dependence liability if misused, and is thus classified as a Schedule V drug in the U.S.[6]

Lyrica is one of four drugs which a subsidiary of Pfizer in 2009 pleaded guilty to misbranding "with the intent to defraud or mislead". Pfizer agreed to pay $2.3 billion (£1.4 billion) in settlement, and entered a corporate integrity agreement. Pfizer illegally promoted the drugs and caused false claims to be submitted to government healthcare programs for uses that were not approved by the U.S. Food and Drug Administration (FDA).[7]

Pregabalin is available in 25, 50, 75, 100, 150, 200, 225, and 300 mg capsules, and recently a strawberry-flavoured oral solution has been developed, containing 20 mg/mL with an added sweetening agent (sucrose) to mask the chemical's bitter taste.[8][9] The maximum daily recommended dose for pregabalin is 600 mg. Dosages must be monitored and increases should be based on patient's tolerance.[8]

Contents

  Uses

  A package of 150 mg Lyrica (Finland)

In the United States, the Food and Drug Administration (FDA) has approved pregabalin for adjunctive therapy for adults with partial onset seizures, management of postherpetic neuralgia and neuropathic pain associated with diabetic peripheral neuropathy, and the treatment of fibromyalgia.[10]. Pregabalin has also been approved in the European Union and Russia (but not in US) for treatment of Generalized anxiety disorder.[11][12]

Pregabalin is also used off-label for the treatment of chronic pain, neuropathic pain, perioperative pain, and migraine, though Pfizer was penalized for promoting such uses in US.[10]

Usually physicians will start the patient on a low dose of pregabalin and increase it gradually, depending on the patient's evaluation. Its therapeutic effect appears after 1 week of use and is similar in effectiveness to lorazepam, alprazolam and venlafaxine but pregabalin has demonstrated superiority by producing more consistent therapeutic effects for psychic and somatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance and additionally unlike benzodiazepines it does not disrupt sleep architecture and produces less severe cognitive and psychomotor impairment; it also has a low potential for abuse and dependence and may be preferred over the benzodiazepines for these reasons.[12][13]

There is not enough data to state that it should be used in all neuropathic pain, and it has not been found to be effective for HIV-associated peripheral neuropathy.[14]

  History

Pregabalin was invented by medicinal chemist Richard Bruce Silverman at Northwestern University in the United States. The drug was approved in the European Union in 2004. Pregabalin received U.S. FDA approval for use in treating epilepsy, diabetic neuropathic pain, and post-herpetic neuralgia in December 2004, and appeared on the U.S. market in fall 2005.[15]

In June 2007, the FDA approved Lyrica as a treatment for fibromyalgia. It was the first drug to be approved for this indication and remained the only one until duloxetine (Cymbalta) gained FDA approval for the treatment of fibromyalgia in June 2008.[16]

The patent for Lyrica currently expires in March 2018 (Silverman, R. B.; Andruszkiewicz, R. U. S. Pat. 6,197,819 B1 (March 6, 2001) "Gamma Amino Butyric Acid Analogs and Optical Isomers."). This is the earliest possible date that a generic version of Lyrica could become available. However, there are other circumstances that could come up to extend the exclusivity period of Lyrica beyond 2018. These circumstances could include things such as lawsuits or other patents for specific Lyrica uses. Once Lyrica goes off patent, there may be several companies that manufacture a generic Lyrica drug.

  Adverse effects

Adverse drug reactions associated with the use of pregabalin include:[17][18]

Pregabalin may also cause withdrawal effects after long-term use if discontinued abruptly. When prescribed for seizures, quitting "cold turkey" can increase the strength of the seizures and possibly cause the seizures to reoccur. Withdrawal symptoms include restlessness, insomnia, and anxiety. Pregabalin should be reduced gradually when finishing treatment. Because of complication risk associated with certain common side-effects in patients affected by other health issues, Pregabalin should not be used without regular medical supervision and any side effect should immediately be reported.[citation needed]

  Overdosage

Several renal failure patients developed myoclonus while receiving pregabalin, apparently as a result of gradual accumulation of the drug. Acute overdosage may be manifested by somnolence, tachycardia and hypertonicity. Plasma, serum or blood concentrations of pregabalin may be measured to monitor therapy or to confirm a diagnosis of poisoning in hospitalized patients.[20][21][22]

  Pharmacology

  Pharmacodynamics

Like gabapentin, pregabalin binds to the α2δ (alpha2delta) subunit of the voltage-dependent calcium channel in the central nervous system. Pregabalin decreases the release of neurotransmitters including glutamate, noradrenaline, substance P and calcitonin gene-related peptide.[23] However, unlike anxiolytic compounds (eg, benzodiazepines) which exert their therapeutic effects through binding to GABAA, GABAB, and benzodiazepine receptors, pregabalin neither binds directly to these receptors nor augments GABAA currents or affects GABA metabolism (Pfizer Inc. 2006).[24]

  Pharmacokinetics

Absorption: Pregabalin is rapidly absorbed when administered on an empty stomach, with peak plasma concentrations occurring within one hour. Pregabalin oral bioavailability is estimated to be greater than or equal to 90% and is independent of dose. The rate of pregabalin absorption is decreased when given with food resulting in a decrease in Cmax by approximately 25 to 30% and a delay in Tmax to approximately 2.5 hours. Administration with food, however, has no clinically significant effect on the extent of absorption.[25]

Distribution: Pregabalin has been shown to cross the blood–brain barrier in mice, rats, and monkeys. Pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. In humans, the volume of distribution of pregabalin for an orally administered dose is approximately 0.56 L/kg and is not bound to plasma proteins.[25]

Metabolism: Pregabalin undergoes negligible metabolism in humans.[26] Approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The major metabolite is N-methyl pregabalin.[25]

Excretion: Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug.[25] Renal clearance of pregabalin is 73 mL/minute.[verification needed]

  Drug interactions

No pharmacokinetic interactions have been demonstrated in vivo. The manufacturer notes some potential pharmacological interactions with opioids (pregabalin is synergistic with opioids in lower doses), benzodiazepines, barbiturates, ethanol (alcohol), and other drugs that depress the central nervous system.[17]

  Pregnancy

Pregabalin has been assigned to pregnancy category C by the FDA. Animal studies have revealed increased incidences of fetal structural abnormalities and other manifestations of developmental toxicity including lethality, growth retardation, and both nervous and reproduction system functional impairment. Animal studies have reported that pregabalin crosses the placenta and have shown an increased risk in male-mediated teratogenicity. There are no controlled data in human pregnancy. Pregabalin should only be given during pregnancy when there are no alternatives and benefit outweighs risk.[27]

  Misuse

Pregabalin is a Schedule V drug, classified as a CNS depressant. The potential for abuse of pregabalin is less than the potential with benzodiazepines; additionally the mild euphoric effects of pregablin disappear with prolonged use.[28]

  See also

  References

  1. ^ a b Benkert, Otto; Hippius, Hanns (2006) (in German). Kompendium Der Psychiatrischen Pharmakotherapie (6th ed.). Springer. ISBN 978-3-540-34401-8. 
  2. ^ "Portions of the Pfizer Inc. 2010 Financial Report". Sec.gov (edgar archives). http://www.sec.gov/Archives/edgar/data/78003/000119312511048877/dex13.htm. Retrieved 2011-11-06. 
  3. ^ Crofford, Leslie J., Rowbotham, Michael C., Mease, Philip J. et al. (April 2005). "Pregabalin for the treatment of fibromyalgia syndrome: results of a randomized, double-blind, placebo-controlled trial". Arthritis & Rheumatism 52 (4): 1264–1273. DOI:10.1002/art.20983. PMID 15818684. http://onlinelibrary.wiley.com/doi/10.1002/art.20983/full. Retrieved 2011-11-06. 
  4. ^ Siddall, Philip J.; Cousins, M.J.; Otte, A. et al. (2006). "Pregabalin in central neuropathic pain associated with spinal cord injury: a placebo-controlled trial". Neurology 67 (10): 1792–1800. DOI:10.1212/01.wnl.0000244422.45278.ff. PMID 17130411. http://www.neurology.org/content/67/10/1792. Retrieved 2011-11-06. 
  5. ^ "FDA Approves First Drug for Treating Fibromyalgia" (Press release). U.S. Food and Drug Administration. 2007=06-21. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm108936.htm. Retrieved 2011-11-06. 
  6. ^ Drug Enforcement Administration, Department of Justice (July 2005). "Schedules of controlled substances: placement of pregabalin into schedule V. Final rule". Federal register 70 (144): 43633–5. PMID 16050051. http://www.deadiversion.usdoj.gov/fed_regs/rules/2005/fr0728.htm. Retrieved 2012-01-22. 
  7. ^ "Pfizer agrees record fraud fine". BBC News. 2009-09-02. http://news.bbc.co.uk/2/hi/business/8234533.stm. Retrieved 2011-11-06. 
  8. ^ a b "Lyrica (Pregabalin) Drug Information: Dosage, Side Effects, Drug Interactions and User Reviews". Rxlist.com. 2011-06-10. http://www.rxlist.com/lyrica-drug.htm. Retrieved 2011-11-06. 
  9. ^ "Pregabalin Oral Solution - IPCOM000187748D - IP.com". Priorartdatabase.com. 2009-09-17. http://ip.com/IPCOM/000187748. Retrieved 2012-01-22. 
  10. ^ a b "Pfizer to pay $2.3 billion to resolve criminal and civil health care liability relating to fraudulent marketing and the payment of kickbacks". Stop Medicare Fraud, US Dept of Health & Human Svc, and of Justice. http://www.stopmedicarefraud.gov/pfizerfactsheet.html. Retrieved 2012-07-04. 
  11. ^ "Pfizer's Lyrica Approved for the Treatment of Generalized Anxiety Disorder (GAD) in Europe" (Press release). http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/03-27-2006/0004327379. Retrieved 2011-11-06. 
  12. ^ a b Bandelow, Borwin; Wedekind, Dirk; Leon, Teresa (July 2007). "Pregabalin for the treatment of generalized anxiety disorder: a novel pharmacologic intervention". Expert Review of Neurotherapeutics 7 (7): 769–781. DOI:10.1586/14737175.7.7.769. PMID 17610384. http://www.ingentaconnect.com/content/ftd/ern/2007/00000007/00000007/art00001. Retrieved 2011-11-06. 
  13. ^ Owen, Richard T. (September 2007). "Pregabalin: its efficacy, safety and tolerability profile in generalized anxiety". Drugs of Today 43 (9): 601–10. DOI:10.1358/dot.2007.43.9.1133188. PMID 17940637. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=4&p_RefId=1133188&p_IsPs=N. Retrieved 2012-01-22. 
  14. ^ Simpson, David M.; Schifitto, G.; Clifford, D.B. et al. (February 2010). "Pregabalin for painful HIV neuropathy: a randomized, double-blind, placebo-controlled trial". Neurology 74 (5): 413–420. DOI:10.1212/WNL.0b013e3181ccc6ef. PMC 2816006. PMID 20124207. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2816006. 
  15. ^ Dworkin, Robert H.; Kirkpatrick, Peter (June 2005). "Pregabalin" (PDF). Nature Reviews Drug Discovery 4 (6): 455–456. DOI:10.1038/nrd1756. PMID 15959952. http://www.nature.com/nrd/journal/v4/n6/pdf/nrd1756.pdf. Retrieved 2012-01-22. 
  16. ^ "Living with Fibromyalgia, Drugs Approved to Manage Pain". U.S. Food and Drug Administration. 2008-07-18. http://www.fda.gov/ForConsumers/ConsumerUpdates/ucm107802.htm. Retrieved 2011-11-06. 
  17. ^ a b Pfizer Australia Pty Ltd. Lyrica (Australian Approved Product Information). West Ryde: Pfizer; 2006.
  18. ^ Rossi, Simone, ed. (2006). Australian Medicines Handbook, 2006. Australian Medicines Handbook. ISBN 978-0-9757919-2-9. 
  19. ^ "Medication Guide (Pfizer Inc.)" (PDF). U.S. Food and Drug Administration. June 2011. http://www.fda.gov/downloads/Drugs/DrugSafety/UCM152825.pdf. Retrieved 2011-11-06. 
  20. ^ Murphy, N.G.; Mosher, L. (2008). "Severe myoclonus from pregabalin (Lyrica) due to chronic renal insufficiency". Clinical Toxicology 46: 594. 
  21. ^ Yoo, Lawrence; Matalon, Daniel; Hoffman, Robert S.; Goldfarb, David S. (2009). "Treatment of pregabalin toxicity by hemodialysis in a patient with kidney failure". American Journal of Kidney Diseases 54 (6): 1127–30. DOI:10.1053/j.ajkd.2009.04.014. PMID 19493601. 
  22. ^ Baselt, Randall C. (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Biomedical Publications. pp. 1296–1297. ISBN 978-0-9626523-7-0. 
  23. ^ Micheva KD, Taylor CP, Smith SJ (April 2006). "Pregabalin Reduces the Release of Synaptic Vesicles from Cultured Hippocampal Neurons". Molecular Pharmacology 70 (2): 467–476. DOI:10.1124/mol.106.023309. PMID 16641316. http://molpharm.aspetjournals.org/content/70/2/467.full.pdf. 
  24. ^ Strawn, JR; Geracioti Jr, TD (2007). "The treatment of generalized anxiety disorder with pregabalin, an atypical anxiolytic". Neuropsychiatric disease and treatment 3 (2): 237–43. DOI:10.2147/nedt.2007.3.2.237. PMC 2654629. PMID 19300556. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2654629. 
  25. ^ a b c d "Summary of product characteristics". European Medicines Agency. 19 August 2009. http://www.emea.europa.eu/humandocs/PDFs/EPAR/lyrica/emea-combined-h546en.pdf. Retrieved 8 September 2009. [dead link]
  26. ^ McElroy, Susan L.; Keck, Paul E.; Post, Robert M., eds. (2008). Antiepileptic Drugs to Treat Psychiatric Disorders. INFRMA-HC. p. 370. ISBN 978-0-8493-8259-8. 
  27. ^ "Pregabalin, Prescription Marketed Drugs". Drugs Database. http://drugsdb.eu/drug.php?d=Pregabalin&m=Southeast%20Medical%20Solutions%20Rx%20Llc&id=82ea6330-e914-4741-b642-e42203b92d17.xml. Retrieved 2012-01-22. 
  28. ^ Chalabianloo, F; Schjøtt J (January 2009). "Pregabalin and its potential for abuse". Journal of the Norwegian Medical Association 129 (3): 186–187. DOI:10.4045/tidsskr.08.0047. PMID 19180163. http://www.tidsskriftet.no/index.php?vp_SEKS_ID=1797598. 

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