APO-PREGABALIN pregabalin 50 mg capsule blister pack

Država: Australija

Jezik: engleski

Izvor: Department of Health (Therapeutic Goods Administration)

Aktivni sastojci:

pregabalin

Dostupno od:

Apotex Pty Ltd

INN (International ime):

Pregabalin

Status autorizacije:

Registered

Svojstava lijeka

Product Information – Australia
APO-Pregabalin capsules
Page 1
APO-PREGABALIN CAPSULES
NAME OF THE MEDICINE
Pregabalin.
Chemical Name:
(S)-3-(aminomethyl)-5-methylhexanoic acid
Structural Formula:
Molecular Formula:
C
8
H
17
NO
2
Molecular Weight:
159.23
CAS Registry Number:
148553-50-8
DESCRIPTION
Pregabalin is an analogue of the neurotransmitter gamma-aminobutyric
acid (GABA). It has analgesic and
anticonvulsant activity. Pregabalin is a white to off-white solid. It
is freely soluble in water and basic and
acidic aqueous solutions.
Each capsule contains 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225
mg or 300 mg of pregabalin,
as the active ingredient.
In addition, each capsule contains the following inactive ingredients:
lactose monohydrate, maize starch,
purified talc, gelatin, purified water, titanium dioxide, sodium
lauryl sulfate and TekPrint SW 9008 black ink.
The 75 mg, 100 mg, 200 mg, 225 mg and 300 mg capsules also contain
iron oxide red.
PHARMACOLOGY
PHARMACOLOGICAL ACTIONS
_In vitro_ studies show that pregabalin binds to an auxiliary subunit
(α2δ protein) of voltage-gated calcium
channels in the central nervous system, potently displacing
[3H]-gabapentin. Two lines of evidence indicate
that binding of pregabalin to the α2δ site is required for analgesic
and anticonvulsant activity in animal
models: (1) Studies with the inactive _R_-enantiomer and other
structural derivatives of pregabalin and (2)
Studies of pregabalin in mutant mice with defective drug binding to
the α2δ protein. In addition, pregabalin
reduces the release of several neurotransmitters, including glutamate,
noradrenaline and substance P. The
significance of these effects for the clinical pharmacology of
pregabalin is not known.
Pregabalin does not show affinity for receptor sites or alter
responses associated with the action of several
common drugs for treating seizures or pain. Pregabalin does not
interact with either GABA
A
or GABA
B
receptors; it is not converted metabolically into GABA or a GABA
agonist; it is not an inh