Pregabalin
Chemical
Structural analogue of GABA
Use
Neuropathic pain
Postherpetic neuralgia
Fibromyalgia
Partial onset seizures
Presentation
Capsule, Tablets ER, Solution
Dose
Requires dose titration
50mg in divided doses to start
Max 300mg/day
Route
po
MoA
Binds a2δ subunit of presynaptic voltage gated calcium channels in CNS
Modulating the release of excitatory neurotransmitters glutamate, subs-P, norepinephrine
PD
(systems)s
PK
A
OBA > 90%
D
Not lipophilic but crosses BBB
Facilitated by L transporters which transport a-acids across BBB
No PPB
M
<2% metabolism
E
Excreted unchanged in urine
t1/2β 6hrs
Adverse Effects
Dependence
Vertigo, dizziness, balance disorder, incoordination, ataxia, blurry vision, diplopia, somnolence, confusion, tremor, attention disturbance, peripheral oedema, dry mouth, constipation