ACTIVE-PAC WITH GABAPENTIN lidocaine hydrochloride menthol

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

GABAPENTIN (UNII: 6CW7F3G59X) (GABAPENTIN - UNII:6CW7F3G59X)

Available from:

Pharmaceutica North America, Inc.

INN (International Name):

GABAPENTIN

Composition:

GABAPENTIN 300 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ACTIVE-PAC WITH GABAPENTIN- GABAPENTIN, LIDOCAINE HYDROCHLORIDE,
MENTHOL
PHARMACEUTICA NORTH AMERICA, INC.
----------
ACTIVE-PAC WITH GABAPENTIN
GABAPENTIN CAPSULES USP
DESCRIPTION
Gabapentin capsules, USP are supplied as imprinted hard shell capsules
containing 100 mg, 300 mg, and
400 mg of gabapentin USP.
The inactive ingredients for the capsules are calcium carbonate,
calcium sulfate dihydrate, glyceryl
behenate, and pregelatinized starch. The capsule shell contains
gelatin, titanium dioxide, sodium lauryl
sulfate, yellow iron oxide (300 mg and 400 mg) and red iron oxide (400
mg). The imprinting ink
contains shellac, dehydrated alcohol, isopropyl alcohol, butyl
alcohol, propylene glycol, strong
ammonia solution, black iron oxide, potassium hydroxide, and purified
water.
Gabapentin is described as 1-(aminomethyl)cyclohexaneacetic acid with
a molecular formula of
C H NO and a molecular weight of 171.24. The structural formula of
gabapentin is:
Gabapentin is a white to off-white crystalline solid with a pK of 3.7
and a pK of 10.7. It is freely
soluble in water and both basic and acidic aqueous solutions. The log
of the partition coefficient (n-
octanol/0.05M phosphate buffer) at pH 7.4 is -1.25.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
The mechanism by which gabapentin exerts its analgesic action is
unknown, but in animal models of
analgesia, gabapentin prevents allodynia (pain-related behavior in
response to a normally innocuous
stimulus) and hyperalgesia (exaggerated response to painful stimuli).
In particular, gabapentin prevents
9
17
2
a1
a2
pain-related responses in several models of neuropathic pain in rats
or mice (e.g. spinal nerve ligation
models, streptozocin-induced diabetes model, spinal cord injury model,
acute herpes zoster infection
model). Gabapentin also decreases pain-related responses after
peripheral inflammation (carrageenan
footpad test, late phase of formalin test). Gabapentin did not alter
immediate pain-related behaviors (rat
tail flick test, formalin footpad acute phase, acetic acid abd