APOKYN apomorphine hydrochloride injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

APOMORPHINE HYDROCHLORIDE (UNII: F39049Y068) (APOMORPHINE - UNII:N21FAR7B4S)

Available from:

Tercica, Inc.

INN (International Name):

APOMORPHINE HYDROCHLORIDE

Composition:

APOMORPHINE HYDROCHLORIDE 30 mg in 3 mL

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

APOKYN- APOMORPHINE HYDROCHLORIDE INJECTION
TERCICA, INC.
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APOKYN
APOMORPHINE HYDROCHLORIDE INJECTION
10 MG/ML
FOR SUBCUTANEOUS USE ONLY
NOT FOR IV USE
RX ONLY
DESCRIPTION
APOKYN (apomorphine hydrochloride, USP) is a non-ergoline dopamine
agonist. Apomorphine
hydrochloride is chemically designated as 6aβ-Aporphine-10,11-diol
hydrochloride hemihydrate with
a molecular formula of C
H NO • HCl • 1/2H O. Its structural formula and molecular weight
are:
M.W. 312.79
Apomorphine hydrochloride appears as minute, white or grayish-white
glistening crystals or as white
powder that is soluble in water at 80°C.
APOKYN 10 mg/mL is a clear, colorless, sterile solution for
subcutaneous injection and is available
in 3 mL cartridges. Each mL of solution contains 10 mg of apomorphine
hydrochloride, USP as
apomorphine hydrochloride hemihydrate and 1 mg of sodium
metabisulfite, NF in water for injection,
USP. In addition, each mL of solution may contain sodium hydroxide, NF
and/or hydrochloric acid, NF
to adjust the pH of the solution and 5 mg/mL of benzyl alcohol, NF as
a preservative.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION:
APOKYN is a non-ergoline dopamine agonist with high _in vitro _binding
affinity for the dopamine D
receptor (K = 4.4 nM), moderate affinity for the dopamine D , D , and
D (K = 35-83, 26, and 15 nM,
respectively), and adrenergic α
, α
, α
(K = 65, 66, and 36 nM, respectively) receptors, and low
affinity for the dopamine D , serotonin 5HT
, 5HT
, 5HT
, and 5HT
(K = 370, 120, 120, 130,
and 100 nM, respectively) receptors. Apomorphine exhibits no affinity
for the adrenergic β and β or
histamine H receptors (K > 10,000 nM).
The precise mechanism of action of APOKYN as a treatment for
Parkinson’s disease is unknown,
although it is believed to be due to stimulation of post-synaptic
dopamine D - type receptors within the
caudate-putamen in the brain. Apomorphine has been shown to improve
motor function in an animal
model of Parkinson’s disease. In particular, apomorphine attenuates
the motor