Like gabapentin, pregabalin binds to the α2δ (alpha2delta) subunit of the voltage-dependent calcium channel in the central nervous system. This reduces calcium influx into the nerve terminals. Pregabalin also decreases the release of neurotransmitters such as glutamate, noradrenaline, and substance P (Australian Medicines Handbook). Pregabalin increases neuronal GABA levels by producing a dose-dependent increase in glutamic acid decarboxylase activity. Glutamic acid decarboxylase (GAD) is the enzyme that converts the excitatory neurotransmitter glutamate into the inhibitory GABA in a single step. For this reason, pregabalin greatly potentiates benzodiazepines, barbiturates & other depressants.

Pregabalin is an analog of the neurotransmitter GABA. It binds potently to the alpha2-delta subunit resulting in modulation of Ca channels and reduction in the release of several neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P.

Absorption
Rapidly absorbed after oral doses. Peak plasma concentrations are achieved within 1.5 hours.

Distribution
Not bound to plasma proteins.

Metabolism
Negligible metabolism.

Excretion
About 98% excreted unchanged in urine. Elimination half life: about 6.3 hours.

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Dizziness, drowsiness, visual disturbance (including blurred vision, diplopia), ataxia, dysarthria, tremor, lethargy, memory impairment, euphoria, wt gain, constipation, dry mouth, peripheral edema, depression, confusion, agitation, hallucinations, myoclonus, hypoaesthesia, hyperaesthesia, tachycardia, excessive salivation, sweating, flushing, rash, muscle cramp, myalgia, arthralgia, urinary incontinence, dysuria, thrombocytopenia, neutropenia, 1st ° heart block, hypotension, hypertension, pancreatitis, dysphagia, oliguria, rhabdomyolysis.

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Discontinue treatment if patients develop severe angioedema. Withdraw treatment gradually over at least 1 wk. May cause peripheral oedema. Regular vision check is recommended. May decrease platelet count and prolong PR interval.

Concurrent use with oxycodone, lorazepam and ethanol may increase the CNS effects.

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Oral
Postherpetic neuralgia
Adult: 75-150 mg bid. May increase up to 600 mg/day in patients with ongoing pain and can tolerate 300 mg/day.
Renal impairment: Dosage adjustment is required. Patients undergoing haemodialysis should receive a supplementary dose of 25-100 mg immediately after each 4-hours haemodialysis session.
CrCl (ml/min)         Dosage Recommendation
30-60                    Initiate at 75 mg, max dose: 300 mg/day.
15-30                    Initiate at 25-50 mg, max dose: 150 mg/day.
<15                       Initiate at 25 mg, max dose: 75 mg/day.

Oral
Adjunct in partial seizures
Adult: 150-600 mg/day. Should be given in 2-3 divided doses. Max dose: 600 mg/day,
Renal impairment:Dosage adjustment is required. Patients undergoing haemodialysis should receive a supplementary dose of 25-100 mg immediately after each 4-hours haemodialysis session.
CrCl (ml/min)    Dosage Recommendation
30-60               Initiate at 75 mg, max dose: 300 mg/day.
15-30               Initiate at 25-50 mg, max dose: 150 mg/day.
<15                  Initiate at 25 mg, max dose: 75 mg/day.

Oral
Fibromyalgia
Adult: Initiate at 75 mg bid. May increase to 225 mg bid for patients who do not experience sufficient benefit with 300 mg/day.
Renal impairment: Dosage adjustment is required. Patients undergoing haemodialysis should receive a supplementary dose of 25-100 mg immediately after each 4-hours haemodialysis session.
CrCl (ml/min)    Dosage Recommendation
30-60               Initiate at 75 mg, max dose: 300 mg/day.
15-30               Initiate at 25-50 mg, max dose: 150 mg/day.
<15                  Initiate at 25 mg, max dose: 75 mg/day.

Oral
Anxiety
Adult: Initiate at 150 mg daily. May increase at weekly intervals in steps of 150 mg. Max dose: 600 mg daily.
Renal impairment: Dosage adjustment is required. Patients undergoing haemodialysis should receive a supplementary dose of 25-100 mg immediately after each 4-hours haemodialysis session.
CrCl (ml/min)    Dosage Recommendation
30-60               Initiate at 75 mg, max dose: 300 mg/day.
15-30               Initiate at 25-50 mg, max dose: 150 mg/day.
<15                  Initiate at 25 mg, max dose: 75 mg/day.

May be taken with or without food

Contraindicated in pregnancy

Contraindicated in lactation

Safety and efficacy not established

Because of age-related renal function impairment, dosage adjustment may be needed.

Hypersensitivity. Pregnancy, lactation. Driving or working with machines, or do other dangerous activities.

Oral
Store at 25°C

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