Pregabalin

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Information about Pregabalin

Pregabalin is an inhibitor of neuronal activity used for therapy of neuropathy and as an anticonvulsant. 

Liver safety of Pregabalin

Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare. 

Mechanism of action of Pregabalin

Pregabalin (pre gab' a lin) is a structural analogue of gamma-aminobutyric acid (GABA) but is novel in its activity, having no effects on GABA-A or GABA-B receptors.  Instead, the neuronal acitivity of pregabalin appears to be mediated by its binding to the alpha-2-delta subunit of the presynaptic voltage-gated calcium channel whcih leads to a decrease in release of neuroexcitatory neurotransmitters by hyperexcited neurons.  Pregabalin has been shown to be effective in reducing neuropathic pain from diabetic and postherpetic neuropathy and is an effective anticonvulsant. 

FDA approval information for Pregabalin

Pregabalin was approved for use in the United States in 2004.  Current indications include diabetic and post-herpetic neuropathy and as adjunctive therapy of partial onset seizures.  Pregabalin is also used for fibromyalgia and off-label for generalized anxiety disorders and migraine. 

Dosage and administration for Pregabalin

Pregabalin is available in capsules in varying concentrations from 25 to 300 mg under the brand name of Lyrica.  The recommended initial dose for neuropathic pain is 50 to 75 mg two to three times daily, the maximum dose being 300 mg daily.  Higher doses are used in treating seizures.  The dose should be increased and tapered gradually. 

Side effects of Pregabalin

The most common side effects of pregabalin are dose related and include peripheral edema, weight gain, dizziness, somnolence, confusion, headache, blurred vision, tremor and ataxia.

Anticonvulsants

Generic Name / Brand Name Liver Toxicity Score Approval Year Major Indications
Brivaracetam / Briviact E 2016 Partial seizures
Carbamazepine / Tegretol A 1968 Partial, mixed and generalized seizures, trigeminal neuralgia
Clobazam / Onfi E 2011 Seizures assocated with Lennox-Gastaut syndrome
Clonazepam / Klonopin D 1975 Absence and myoclonic seizures, anxiety and panic disorders
Clorazepate / Tranxene E 1972 Partial seizures, anxiety disorders, and alcohol withdrawal
Diazepam / Valium E 1963 Convulsions, anxiety disorders, muscle spasms
Eslicarbazepine / Aptiom D 2013 Partial seizures
Ethosuximide / Zarontin E 1960 Absence seizures
Ezogabine / Potiga E 2011 Partial seizures
Felbamate / Febatol B 1993 Refractory or severe epilepsy
Fosphenytoin / Cerebyx A 1996 Tonic-clonic seizures, status epilepticus
Gabapentin / Neurontin C 1993 Partial seizures, post-herpetic neuralgia
Lacosamide / Vimpat D 2008 Partial seizures
Lamotrigine / Lamictal B 1994 Partial and generalized tonic-clonic seizures, bipolar disorder
Levetiracetam / Keppra C 1999 Partial, generalized tonic-clonic, and myoclonic seizures
Methsuximide / Celontin E 1957 Absence seizures
Oxcarbazepine / Trileptal D 2000 Partial seziures
Perampanel / Fycompa E 2012 Partial and generalized tonic-clonic seizures
Phenobarbital / Luminal A 1916 Partial and generalized seizures, anxiety, and irritable bowel syndrome
Phenytoin / Dilantin A 1938 Generalized tonic-clonic and partial onset seizures, status epilepticus
Pregabalin / Lyrica C 2004 Partial seizures, fibromyalgia, and neuropathic pain
Primidone / Mysoline E 1954 Partial and generalized tonic-clonic seizures
Rufinamide / Banzel E 2008 Seizures associated with Lennox-Gastaut syndrome
Tiagabine / Gabitril E 1997 Partial seizures
Topiramate / Topamax C 1996 Partial and generalized tonic-clonic seizures, migraine headaches
Valproate / Depakene A 1978 Absence and complex partial seizures
Vigabatrin / Sabril D 2009 Refractory, complex partial seizures, and infantile spasms
Zonisamide / Zonegran D 2000 Partial seizures

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