Country: Singapore
Language: English
Source: HSA (Health Sciences Authority)
BUPRENORPHINE HCl EQV BUPRENORPHINE
ZUELLIG PHARMA PTE. LTD.
N02AE01
2 mg
TABLET
BUPRENORPHINE HCl EQV BUPRENORPHINE 2 mg
ORAL
Prescription Only
RECKITT BENCKISER HEALTHCARE (UK) LTD
ACTIVE
2000-02-03
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 Read the complete document
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 Read the complete document