SUBUTEX SUBLINGUAL TABLETS 0.4 mg

Country: Singapore

Language: English

Source: HSA (Health Sciences Authority)

Active ingredient:

BUPRENORPHINE HCl EQV BUPRENORPHINE

Available from:

ZUELLIG PHARMA PTE. LTD.

ATC code:

N02AE01

Dosage:

0.4 mg

Pharmaceutical form:

TABLET

Composition:

BUPRENORPHINE HCl EQV BUPRENORPHINE 0.4 mg

Administration route:

ORAL

Prescription type:

Prescription Only

Manufactured by:

RECKITT BENCKISER HEALTHCARE (UK) LTD

Authorization status:

ACTIVE

Authorization date:

2000-02-03

Patient Information leaflet

SUBUTEX* SUBLINGUAL TABLET 
Brand of buprenorphine 
FOR SUBLINGUAL ADMINISTRATION 
_ _
_DESCRIPTION:  _Each SUBUTEX* Sublingual Tablet contains
buprenorphine hydrochloride equivalent to 
0.4mg, 2mg or 8mg buprenorphine base.  _Inactive ingredients:_ 
Monohydrated lactose, mannitol, maize 
starch, povidone excipient K30, citric acid, sodium citrate, magnesium
stearate. 
_ _
_ACTIONS:  _Buprenorphine is an opioid partial agonist/antagonist
which attaches itself to the µ (mu) and 
κ 
(kappa) receptors of the brain.  Its activity in
opioid maintenance treatment is attributed to its slowly 
reversible link with the µ receptors which, over
a prolonged period, minimizes the need of the addicted 
patient for drugs. 

Buprenorphine has a wide margin of safety due to its partial
agonist/antagonist activity, which limits its 
depressant effects, particularly on cardiac and respiratory
functions. 
_ _
_PHARMACOKINETIC PROPERTIES: _
_Absorption:_  When taken orally,
buprenorphine undergoes first-pass hepatic metabolism with N-
dealkylation and glucuroconjugation in the small
intestine and the liver.  The use of this medication by the 
oral route is therefore inappropriate. 

Peak plasma concentrations are achieved 90 minutes after sublingual
administration and the maximal 
dose-concentration relationship is linear, between 2 mg and 16 mg. 
_ _
_Distribution:_  The absorption of buprenorphine is followed by a
rapid distribution phase and a half-life of 2 
to 5 hours. 
_ _
_Metabolism and elimination:_ Buprenorphine is metabolized by 14-N
dealkylation and glucuroconjugation 
of the parent molecule and the dealkylated metabolite.  The
N-dealkybuprenorphine is a 
µ (mu) agonist 
with weak intrinsic activity. Preclinical data suggest that CYP3A4
is responsible for the N-dealkylation of 
buprenorphine. 

Elimination of buprenorphine is bi- or tri-exponential, with a long
terminal elimination phase of 20 to 25 
hours, due in part to reabsorpti

Summary of Product characteristics

Page 1 of 14
1. NAME OF THE MEDICINAL PRODUCT
SUBUTEX SUBLINGUAL TABLETS 0.4 mg
SUBUTEX SUBLINGUAL TABLETS 2 mg
SUBUTEX SUBLINGUAL TABLETS 8 mg
Brand of buprenorphine
FOR SUBLINGUAL ADMINISTRATION
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Buprenorphine hydrochloride equivalent to buprenorphine base: 0.4mg, 2
mg or 8 mg.
For a full list of excipients, see section 6.1
3. PHARMACEUTICAL FORM _ _
Each SUBUTEX contains buprenorphine hydrochloride equivalent to 0.4mg,
2mg or 8mg
buprenorphine base.
SUBUTEX 8mg sublingual tablets are uncoated oval white flat bevelled
edged tablets, nominal
dimensions 14 mm x 7 mm, debossed on one side with “B8”.
SUBUTEX 2 mg sublingual tablets are uncoated oval white flat bevelled
edged tablets, nominal
dimensions 10 mm x 5 mm, debossed on one side with “B2”.
SUBUTEX 0.4 mg sublingual tablets are uncoated oval white flat
bevelled edged tablets, nominal
dimensions 8 mm x 4 mm, debossed on one side with “04”.
The sublingual formulation is not designed to be split or broken.
4. CLINICAL PARTICULARS_ _
4.1 THERAPEUTIC INDICATIONS: _ _
Substitution treatment for opioid drug dependence, within a framework
of medical, social and
psychological treatment.
4.2 POSOLOGY AND METHOD OF_ _ADMINISTRATION: _ _
Treatment with SUBUTEX is intended for use in adults and children over
15 years of age who have
agreed to be treated for addiction.
When initiating SUBUTEX treatment, the physician should be aware of
the partial agonist profile
of the buprenorphine molecule. Buprenorphine binds to the µ (mu) and
κ (kappa) opiate
receptors, and may precipitate withdrawal symptoms in opioid-dependent
patients.
Administration is sublingual. Physicians must advise patients that the
sublingual route is the
Page 2 of 14
only effective and safe route of administration for this drug. The
tablet should be kept under the
tongue until dissolved, which usually occurs within five to ten
minutes.
_Induction therapy: _
The initial dose is from 0.8 to 4 mg, administered as a single daily
dose.
•
_for opioid-dep