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Buprenorphine (Subutex) was licensed in the UK for the treatment of opiate
dependence in 1998 after studies found it to be less addictive than methadone
and much safer in overdosage (1). Buprenorphine has been previously been used
in lower dosage as an analgesic preparation (Temgesic).
There is evidence
that the withdrawal syndrome is milder on discontinuing buprenorphine than methadone,
and also that fewer symptoms emerge during detoxification with buprenorphine (2).
systematic review concluded that buprenorphine is an effective intervention for
use in the maintenance treatment of heroin dependence, but it is not more effective
than methadone at adequate dosages (3).
Buprenorphine has both partial opioid
agonist and opioid antagonist activity, and provides a milder, less euphoric and
less sedating effect than full opioid agonists such as diamorphine or methadone
(although these effects are less pronounced with methadone than with diamorphine)
- in the management of opioid dependence, sublingual tablets are
used at an initial recommended once-daily dose of 0.8-4 mg, adjusted according
to response. In practice, a starting dose of more than 4 mg/day is often used,
with an adequate maintenance dose being in the range 12-24 mg/day. The maximum
daily dose is 32 mg (4)
- buprenorphine also has a relatively good safety
profile. Even higher than normal therapeutic doses rarely result in clinically
significant respiratory depression because of its partial agonist activity at
the opioid receptor involved (mu)
- safety of buprenorphine mixed with high
doses of other sedative drugs such as alcohol or benzodiazepines remains unclear
buprenorphine treatment in opioid-dependent people may precipitate symptoms of
withdrawal because buprenorphine displaces any residual illicit opioid agonists
from receptors and because its partial agonist activity reduces the stimulation
- also, whereas methadone is an agonist, buprenorphine is an
antagonist at the receptor subtype involved in mood (kappa), which may mean that
it produces less dysphoria
- buprenorphine has abuse potential,
as tablets can be crushed and then injected
asthma, respiratory of hepatic insufficiency; perform regular liver function tests
- withdraw if jaundice or hepatic necrosis develop; pregnancy
- severe hepatic or respiratory insufficiency, acute alcoholism,
delirium tremens, patients < 16 years, breast feeding
- alcohol, MAOIs, CNS depressants, other opiods, benzodiazepines,
Side effects include:
insomnia, constipation, asthenia, nausea, drowsiness, orthostatic hypotension,
dizziness, sweating; other possible side effects include withdrawal symptoms,
The summary of product characteristics should be consulted
before prescribing this drug.
- Seivewright N. More
than methadone? The case for other substitute drugs. In: Community treatment of
drug misuse: more than methadone. Cambridge: Cambridge University Press, 2000,
- Bicel WK, Amass L. Buprenorphine treatment of opiod dependence:
a review. Exer Clin Psychopharmacol 1995; 3: 477-89.
RP et al. Buprenorphine maintenance versus placebo or methadone maintenance for
opioid dependence. Cochrane Database Syst Rev 2004; (3): CD002207.
(January 2007).Methadone and buprenorphine for the management of opioid dependence
Last reviewed 01/2018