情報リーフレット
ZYPREXA
®
IM
_olanzapine_
CONSUMER MEDICINE INFORMATION
WHAT IS IN THIS LEAFLET
This leaflet is designed to provide
you with answers to some common
questions about this medicine. It does
not contain all the available
information and does not take the
place of talking with your doctor.
The information in this leaflet was
last updated on the date shown on the
final page. More recent information
about this medicine may be available.
Make sure you speak to your
pharmacist or doctor to obtain the
most up to date information on this
medicine. You can also download the
most up to date leaflet from
www.lilly.com.au . The updated
leaflet may contain important
information about ZYPREXA and its
use that you should be aware of.
All medicines have risks and
benefits. Your doctor has more
information about this medicine than
is contained in this leaflet. Also, your
doctor has had the benefit of taking a
full and detailed history from you
and is in the best position to make an
expert judgement to meet your
individual needs.
IF YOU HAVE ANY CONCERNS ABOUT
TAKING THIS MEDICINE, TALK TO YOUR
DOCTOR OR PHARMACIST.
KEEP THIS LEAFLET WITH THIS
MEDICINE.
You may need to read it again.
WHAT ZYPREXA IS
USED FOR
ZYPREXA belongs to a group of
medicines called antipsychotics. It
helps to correct chemical imbalances
in the brain, which may cause mental
illness.
ZYPREXA IM injection is used for
the rapid control of agitation and
disturbed behaviours in patients with
schizophrenia and related psychoses
and in patients with acute mania
associated with Bipolar I Disorder.
Schizophrenia is a mental illness
with disturbances in thinking,
feelings and behaviour. Bipolar I
Disorder is a mental illness with
symptoms such as feeling "high",
having excessive amounts of energy,
needing much less sleep than usual,
talking very quickly with racing
ideas and sometimes severe
irritability.
ZYPREXA IM injection is given
when treatment with ZYPREXA
tablets is not appropriate. Your
doctor will change your treatment to
ZYPREXA tablets or ZYP
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製品の特徴
ZYPREXA (olanzapine) – Product Information v14.0
Page 1 of 21
ZYPREXA
®
(olanzapine)
NAME OF THE MEDICINE
ZYPREXA
®
IM (olanzapine).
Chemically, olanzapine is
2-methyl-4-(4-methyl-1-piperazinyl)-10_H_-thieno[2,3-_b_]
[1,5]benzodiazepine and its empirical formula is C
17
H
20
N
4
S. Olanzapine is a yellow
crystalline solid, practically insoluble in water
with a molecular weight of 312.44. The CAS
number for olanzapine is 132539-06-1.
Olanzapine has the following structural formula:
N
N
S
C H
N
N
C H
H
DESCRIPTION
ZYPREXA IM is a yellow lyophilised powder in a clear
glass vial. It is intended for
intramuscular
use only. The active ingredient in ZYPREXA IM is
olanzapine. ZYPREXA IM
also contains excipients: lactose and tartaric
acid. Hydrochloric acid and/or sodium
hydroxide may have been added during manufacture to adjust pH.
PHARMACOLOGY
Pharmacodynamics
Olanzapine is an atypical antipsychotic, antimanic
and mood stabilising agent that
demonstrates a broad pharmacological profile across a number
of receptor systems.
In preclinical
studies, olanzapine exhibited a range of receptor affinities
(Ki; < 100 nmol) for
serotonin 5HT
2A/2C
, 5HT
3
, 5HT
6;
dopamine D
1
, D
2
, D
3
, D
4
, D
5
; cholinergic muscarinic
receptors m
1
-m
5;
1
adrenergic; and histamine H
1
receptors. Animal behavioural studies
with olanzapine indicated 5HT, dopamine and cholinergic
antagonism, consistent with the
receptor
binding profile. Olanzapine demonstrated a greater _in-vitro_ affinity for
serotonin
5HT
2
than dopamine D
2
receptors and in _in-vivo_ models, greater 5HT
2
than D
2
activity.
Electrophysiological
studies demonstrated that olanzapine selectively reduced the firing of
mesolimbic (A10) dopaminergic
neurons, while having little effect on the striatal (A9)
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