Pregabalin

Actions

• Blocks voltage-gated Ca++ channels.
• Increases glutamic acid decarboxylase, the enzyme that is responsible for making GABA.

Metabolism

Not metabolized

Elimination

Renal >90%

Therapeutic serum concentration range

5-10 μg/ml

Half-life

7-12 hours

Plasma protein binding

0%

Important side-effects

Angioedema and hypersensitivity skin reactions.

Peripheral edema.

Weight gain.

Suicidal behavior and ideation.

PR interval prolongation.

Decreased platelet count.

Indications

Focal seizures with or without generalization.

Dosing recommendation

Start with 50–75 mg/day.

Increase to 150 mg over 2–4 weeks. If indicated, further increase by increments of 75–150 mg every 2 weeks.

Target dose: 150–600 mg/day divided in 2–3 doses.

Renal impairment

Initial and target doses should be adjusted in patients with impaired renal function.

Hepatic impairment

No adjustment is necessary in patients with impaired hepatic function.