Product Information
Registration Status: ActiveSIN14487P
BRILLIOR CAPSULE 25MG is approved to be sold in Singapore with effective from 2014-01-16. It is marketed by PFIZER PTE LTD, with the registration number of SIN14487P.
This product contains Pregabalin 25mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by Pfizer Manufacturing Deutschland GmbH in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Pregabalin is an anticonvulsant drug used for neuropathic pain, epilepsy and generalized anxiety disorder.[A31161] It presents antihyperalgesic actions by binding to the α2δ subunit of the voltage-dependent calcium channels without presenting antinociceptive actions.[A31162] Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).[L1006] It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the U.S.[A31161]
Indication
Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy or spinal cord injury, and postherpetic neuralgia. It is not approved for the management of fibromyalgia or as adjuntive therapy for adult partial onset seizures.[FDA label]
Mechanism of Action
Pregabalin binds presynaptically to the alpha2-delta subunit of the voltage-gated calcium channels in central nervous system tissues located in the brain and spinal cord.[A31163] The mechanism of action has not been fully elucidated but studies suggest that pregabalin produces a disruption of calcium channel traficking or a reduction of calcium currents. The inhibition of subunits of voltage-gated calcium channels reduces calcium release which in order inhibits the release of several neurotransmitters [FDA label] Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.[A31165]
Pharmacokinetics
- Absorption
- Pregabalin has linear and dose-proportional absorption with a steady state achieved at 48-72 hours. Nowadays, there are two different formulations of pregabalin with different pharmacokinetic profiles, this is important due to the fact that the newest formulation has a propety of extended release. Pregabalin, in its both forms, presents a rapid absorption at fasting state. Pregabalin has a Cmax of 3.2mcg/ml, Tmax 0.7 hours and AUC 31.5mcg h/ml, while pregabalin CR (extended release) presents a Cmax 2.0mcg/ml, Tmax 8 hours and AUC 29.4mcg h/ml. Pregabalin is absorbed from the small intestine and proximal colon and its AUC values will depend on the type and quantity of meal calories ingested. [A31166]
- Distribution
- Pregabalin does not bind to plasma proteins. The apparent volume of distribution after oral administration is 0.5 L/kg. Pregabalin passage across bloos brain barrier (BBB) is done through the system L. [A31167]
- Metabolism
- Pregabalin undergoes negligible metabolism in humans.[A31168]
- Elimination
Clearance
Mean renal clearance is estimated to be 67 to 80.9 ml/min in young healthy subjects. Due to its lack of plasma protein binding, it is indicated the presence of renal tubular reabsorption.[FDA label]
Toxicity
Most common adverse reactions presented in clinical trials are dizziness, somnolence, peripheral edema, nausea, blurred vision, dry mouth and weight gain.[FDA label]
Active Ingredient/Synonyms
(S)-3-(aminomethyl)-5-methylhexanoic acid | (S)-3-Isobutyl gaba | 3-Isobutyl gaba | CI 1008 | S-(+)-3-isobutylgaba | Pregabalin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.