Brand Name : PREGAMAX
Generic Name : Pregabalin
Preparations : 75 mg /150 mg Capsules
Pharmacological Categories : Drug for Neuropathic Pain / Anticonvulsant
Mechanism of Action (MOA)
PREGAMAX (Pregabalin) binds to the α2-δ subunit of voltage-gated Ca2+ channels of axon terminal of the neuron, thus reducing the synaptic release of excitatory neurotransmitters of pain. PREGAMAX may also interact with descending noradrenergic and serotonergic pathways in the brainstem that modulate pain transmission in the spinal cord.
Thus, decrease in neurotransmitter release at many sites within the brain or spinal cord decreases abnormal hyperexcitability and synchronization, preventing seizure and causing analgesic and anxiolytic action.
- Absorption : Rapidly absorbed from the gastrointestinal tract
- Peak Plasma Concentration : 1.5 hours
- Bioavailability : About 90%
- Protein Binding : None
- Metabolism : Liver, negligibly metabolized
- Elimination Half-life : 6.3 hours
- Excretion : Urine (98% unchanged)
Indications and Dosage
- Neuropathic Pain with Cord Injury : One capsule of PREGAMAX 75 mg twice daily. Maximum may be increased up to one capsule of PREGAMAX 150 mg twice daily within 1 week if necessary
- Diabetic Neuropathy : One capsule of PREGAMAX 75 mg twice daily. Maximum may be increased up to one capsule of PREGAMAX 150 mg twice daily within 1 week if necessary
- Postherpetic Neuralgia : One capsule of PREGAMAX 75 mg twice daily. May increase to one capsule of PREGAMAX 150 mg twice daily if necessary. If pain does not subside after taking 1 capsule of PREGAMAX 150 mg twice daily maximum may be increased to 2 capsules of PREGAMAX 150 mg twice daily
- Fibromyalgia : One capsule of PREGAMAX 75 mg twice daily. May increase to one capsule of PREGAMAX 150 mg twice daily within 1 week if necessary. Maximum: One capsule of PREGAMAX 150 mg three time a day
- Adjunct in Partial Seizure with or without Second Generalization: One capsule of PREGAMAX 75 mg twice daily. May increase to maximum dose of PREGAMAX 600 mg per day
Discontinuation : Taper over minimum of 1 week
MOST COMMON : Dizziness and somnolence
COMMON : Blurred vision, diplopia, increased appetite / weight gain, dry mouth, constipation, vomiting, flatulence, euphoria, confusion, reduced libido, erectile dysfunction, irritability, vertigo, ataxia, tremor, dysarthria, paraesthesia, fatigue, oedema
FREQUENT: Disturbance of attention, memory, coordination, gait
LESS FREQUENT : Syncope and congestive heart failure
REPORTED : Stevens-Johnson syndrome
RARELY REPORTED : Reversible renal failure, elevation of creatine kinase concentration, rhabdomyolysis
SEEN : Hypersensitivity reactions (rash, blisters, urticaria, dyspnoea, wheezing)
Hypersensitivity to pregabalin
Warnings and precautions
- Caution in patients with history of angioedema
- Increased risk of suicidal thought or behavior or depression, peripheral edema, dizziness, somnolence and weight gain.
- Abrupt withdrawal may result in increased seizure frequency.
- Possible increase in creatine kinase and rhabdomyolysis
- Risk of ocular effects, thrombocytopenia and PR interval prolongation
- Additive effects on cognitive and gross motor function with CNS depressants (eg. alcohol, lorazepam, oxycodone).
- May increase risk of swelling and hives with ACE inhibitors.
- May increase risk of weight gain and peripheral edema with thiazolidinediones.
Pregnancy Category : C
PREGAMAX 75 mg : A box of 20 blisters, each blister of 10 capsules
PREGAMAX 150 mg : A box of 10 blisters, each blister of 10 capsules