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Pregabalin



Pregabalin
Systematic (IUPAC) name
(S)-3-(aminomethyl)-5-methylhexanoic acid
Identifiers
CAS number 148553-50-8
ATC code N03AX16
PubChem 5486971
DrugBank APRD01198
Chemical data
Formula C8H17NO2 
Mol. mass 159.23 g.mol-1
Pharmacokinetic data
Bioavailability ≥90%
Protein binding Nil
Metabolism Negligible
Half life 5–6.5 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B3 (Au), C (U.S.)

Legal status

S4 (Au), POM (UK), Schedule V (U.S.)

Routes Oral

Pregabalin (INN) (pronounced /prɨˈgæbəlɨn/) is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica.

Recent studies have shown that pregabalin is effective at treating chronic pain in disorders such as fibromyalgia[1] and spinal cord injury[2]

It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the U.S.[3]

Additional recommended knowledge

Contents

History

Pregabalin was initially developed 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. Food and Drug Administration (FDA) approval for use in treating epilepsy, diabetic neuropathy pain and post-herpetic neuralgia pain in June 2005, and appeared on the U.S. market in fall 2005.

Pharmacology

Like gabapentin, pregabalin binds to the α2δ subunit of the voltage-dependent calcium channel in the central nervous system. However, the exact mechanism of action is unknown.

Clinical use

Indications

Pregabalin is indicated for:

  • Treatment of neuropathic pain in adults
  • Adjunctive therapy in adults with partial seizures with or without secondary generalization
  • Fibromyalgia pain. The FDA has approved Pregabalin as an indicated use on June 21, 2007[4].
  • Generalized anxiety disorder (approved in the European Union).[5]

Adverse effects

Adverse drug reactions associated with the use of pregabalin include:[6][7]

  • Very common (>10% of patients): dizziness, drowsiness
  • Common (1–10% of patients): visual disturbance (including blurred vision, diplopia), ataxia, dysarthria, tremor, lethargy, memory impairment, euphoria, weight gain, constipation, dry mouth, peripheral edema, loss or decrease of libido, erectile dysfunction
  • Infrequent (0.1–1% of patients): depression, confusion, agitation, hallucinations, myoclonus, hypoaesthesia, hyperaesthesia, tachycardia, excessive salivation, sweating, flushing, rash, muscle cramp, myalgia, arthralgia, urinary incontinence, dysuria, thrombocytopenia, Kidney calculus
  • Rare (<0.1% of patients): neutropenia, first degree heart block, hypotension, hypertension, pancreatitis, dysphagia, oliguria, rhabdomyolysis

Drug interactions

No pharmacokinetic interactions have been demonstrated in vivo. The manufacturer notes some potential pharmacological interactions with oxycodone, lorazepam and ethanol (alcohol). Concurrent use may increase the central nervous system effects of these medications (e.g. drowsiness, effects on concentration).[6]

References

  1. ^ http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/10-25-2002/0001827864&EDATE=
  2. ^ http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/11-28-2006/0004480854&EDATE=
  3. ^ Drug Enforcement Administration, Department of Justice. Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist 2005;70(144):43633-5. PMID 16050051
  4. ^ FDA Approves First Drug for Treating Fibromyalgia. Retrieved on 2007-07-04.
  5. ^ "Pfizer's Lyrica Approved for the Treatment of Generalized Anxiety Disorder (GAD) in Europe". Press release. Retrieved on 2007-07-04.
  6. ^ a b Pfizer Australia Pty Ltd. Lyrica (Australian Approved Product Information). West Ryde: Pfizer; 2006.
  7. ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Pregabalin". A list of authors is available in Wikipedia.
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