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TEMGESIC 400 MICROGRAM SUBLINGUAL TABLETS

Active substance(s): BUPRENORPHINE HYDROCHLORIDE / BUPRENORPHINE HYDROCHLORIDE / BUPRENORPHINE HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS
1

NAME OF THE MEDICINAL PRODUCT
Temgesic 400 microgram Sublingual Tablets

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Buprenorphine hydrochloride
buprenorphine base.

3

432µg/tablet,

equivalent

to

400µg

PHARMACEUTICAL FORM
Sublingual tablet
White to creamy white, circular, biconvex tablets, embossed on one side with
“H”.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
As a strong analgesic for the relief of moderate to severe pain.

4.2

Posology and method of administration
Administration by the sublingual route.
Adults and children over 12:
1-2 tablets (200-400 micrograms) to be dissolved under the tongue every 6-8
hours or as required. The recommended starting dose for moderate to severe
pain of the type typically presenting in general practice is 1 to 2 tablets, 8
hourly.
Elderly:
There is no evidence that dosage needs to be modified for the elderly.
Children under 12 years:
Temgesic Sublingual is suitable for use in children under 12 as follows:
16 - 25 kg (35 - 55lb)
½ tablet
25 - 37.5 kg (55 - 82.5lb)
½-1 tablet
37.5 - 50 kg (82.5 - 110lb) 1-1½ tablets
The recommended dose should be administered every 6 to 8 hours.
Sublingual administration is not suitable for children under the age of six
years.
Temgesic sublingual may be used in balanced anaesthetic techniques at a dose
of 400 micrograms.

Special populations
Hepatic impairment:
The effects of hepatic impairment on the pharmacokinetics of buprenorphine
were evaluated in a postmarketing study. Buprenorphine is extensively
metabolised in the liver, and plasma levels were found to be higher for
buprenorphine in patients with moderate and severe hepatic impairment
compared to healthy subjects. Patients should be monitored for signs and
symptoms of toxicity or overdose caused by increased levels of
buprenorphine. Temgesic should be used with caution in patients with
moderate to severe hepatic impairment (See section 5.2).

4.3

Contraindications
Not to be given to patients who are known to be allergic to Temgesic or other
opiates.
Hypersensitivity to any of the constituents.

4.4

Special warnings and precautions for use
Temgesic occasionally causes significant respiratory depression and, as with
other strong centrally acting analgesics, care should be taken when treating
patients with impaired respiratory function or patients who are receiving drugs
which can cause respiratory depression. Although volunteer studies have
indicated that opiate antagonists may not fully reverse the effects of Temgesic,
clinical experience has shown that Naloxone may be of benefit in reversing a
reduced respiratory rate. Respiratory stimulants such as Doxapram are also
effective. The intensity and duration of action may be affected in patients with
impaired liver failure.
Controlled human and animal studies indicate that buprenorphine has a
substantially lower dependence liability than pure agonist analgesics. In
patients abusing opioids in moderate doses substitution with buprenorphine
may prevent withdrawal symptoms. In man limited euphorigenic effects have
been observed. This has resulted in some abuse of the product and caution
should be exercised when prescribing it to patients known to have, or
suspected of having, problems with drug abuse.
Diversion:
Diversion of Temgesic has been reported. Diversion refers to the introduction
of buprenorphine into the illicit market either by patients or by individuals
who obtain the medicinal product through theft from patients or pharmacies.
This diversion may lead to new addicts using buprenorphine as the primary
drug of abuse, with the risks of overdose, spread of blood borne viral
infections and respiratory depression.
Hepatic impairment:
The effects of hepatic impairment on the pharmacokinetics of buprenorphine
were evaluated in a postmarketing study. Since buprenorphine is extensively
metabolised, plasma levels were found to be elevated for buprenorphine in
patients with moderate and severe hepatic impairment. Patients should be
monitored for signs and symptoms of toxicity or overdose caused by increased

levels of buprenorphine. Temgesic sublingual tablets should be used with
caution in patients with moderate to severe hepatic impairment (See section
5.2).
Athletes must be aware that this medicine may cause a positive reaction to
‘anti-doping’ tests.

4.5

Interaction with other medicinal products and other forms of interaction
There is evidence to indicate that therapeutic doses of buprenorphine do not
reduce the analgesic efficacy of standard doses of an opioid agonist and that
when buprenorphine is employed within the normal therapeutic range,
standard doses of opioid agonist may be administered before the effects of the
former have ended without compromising analgesia. However, in individuals
on high doses of opioids buprenorphine may precipitate abstinence effects due
to its properties as a partial agonist.
Temgesic may cause some drowsiness which may be potentiated by other
centrally acting agents, including alcohol, tranquillisers, sedatives and
hypnotics. Temgesic should be used with caution in patients receiving
monoamine oxidase inhibitors, although animals studies have given no
evidence of interactions.
Although interaction studies have not been performed, since this drug is
metabolised by CYP3A4 (see section 5.2 pharmacokinetic properties), it is
expected that gestodene, troleandomycin, ketoconazole, norfluoxetine,
ritonavir, indinavir and saquinavir inhibit its metabolism. Alternatively,
inducers of this enzyme such as phenobarbital, carbamazepine, phenytoin and
rifampicin may reduce the levels of the drug. Since the magnitude of an
inducing or inhibitory effect is unknown, such drug combinations should be
avoided.
Temgesic has no known effects on diagnostic laboratory tests.

4.6

Fertility, pregnancy and lactation
Temgesic is not recommended for use during pregnancy. Animal studies
indicate that the amounts of buprenorphine excreted in milk are very low and
in human use are unlikely to be of clinical significance to the baby. There is
indirect evidence in animal studies to suggest that Temgesic may cause a
reduction in milk flow during lactation. Although this occurred only at doses
well in excess of the human dose, it should be borne in mind when treating
lactating women.

4.7

Effects on ability to drive and use machines
If you feel drowsy after taking these tablets do not use machines.
This medicine can impair cognitive function and can affect a patient’s ability
to drive safely. This class of medicine is in the list of drugs included in
regulations under 5a of the Road Traffic Act 1988. When prescribing this
medicine, patients should be told:
• The medicine is likely to affect your ability to drive

• Do not drive until you know how the medicine affects you
• It is an offence to drive while under the influence of this medicine
• However, you would not be committing an offence (called ‘statutory
defence’) if:
o The medicine has been prescribed to treat a medical or dental problem
and
o You have taken it according to the instructions given by the prescriber
and in the information provided with the medicine and
o It was not affecting your ability to drive safely
Details regarding the new driving offence concerning driving after drugs have
been taken in Great Britain may be found here: https://www.gov.uk/drugdriving-law

4.8

Undesirable effects
Nausea, vomiting, dizziness, sweating and drowsiness have been reported and
may be more frequent in ambulant patients. Hallucinations and other
psychotomimetic effects have occurred although more rarely than with other
agonists/antagonists. Elderly patients would be expected to be more
susceptible to these effects. Hypotension leading to syncope may occur.
Rashes, headache, urinary retention and blurring of vision have occasionally
been reported. Rarely, a serious allergic reaction may occur following a single
dose. Temgesic occasionally causes significant respiratory depression (see
section 4.4 Special warnings and precautions for use).
Cases of bronchospasm, angioneurotic oedema and anaphylactic shock have
also been reported.
During use of buprenorphine as substitution treatment the following adverse
reactions have also been observed: hepatic necrosis and hepatitis.

4.9

Overdose
Supportive measures should be instituted and if appropriate Naloxone or
respiratory stimulants can be used. The expected symptoms of overdosage
would be drowsiness, nausea and vomiting; marked miosis may occur.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Buprenorphine is a µ (mu) opioid partial agonist and κ (kappa) antagonist. It is
a strong analgesic of the partial agonist (mixed agonist/antagonist) class.

5.2

Pharmacokinetic properties
Absorption

When taken orally, buprenorphine undergoes first-pass hepatic metabolism
with N-dealkylation and glucuroconjugation in the small intestine. The use of
this medication by the oral route is therefore inappropriate.
Peak plasma concentrations are achieved 90 minutes after sublingual
administration.
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 oxidatively metabolised by 14-N-dealkylation to N-desalkylbuprenorphine (also known as norbuprenorphine) via cytochrome P450
CYP3A4 and by glucuroconjugation of the parent molecule and the
dealkylated metabolite. Norbuprenorphine is a µ (mu) agonist with weak
intrinsic activity.
Elimination of buprenorphine is bi- or tri- exponential, with a long terminal
elimination phase of 20 to 25 hours, due in part to reabsorption of
buprenorphine after intestinal hydrolysis of the conjugated derivative, and in
part to the highly lipophilic nature of the molecule.
Buprenorphine is essentially eliminated in the faeces by biliary excretion of
the glucuroconjugated metabolites (80%), the rest being eliminated in the
urine.

5.3

Preclinical safety data
None stated.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose, mannitol, maize starch, povidone K30, citric acid anhydrous,
magnesium stearate, sodium citrate, purified water and alcohol (96%).

6.2

Incompatibilities
None stated.

6.3

Shelf life
3 years - Nylon/aluminium/uPVC blister strip.
3 years - HDPE bottle.

6.4

Special precautions for storage
Do not store above 30ºC. Store in the original package - Nylon/aluminium/
uPVC blister strip.
Do not store above 30ºC - HDPE bottle.

6.5

Nature and contents of container
Nylon/aluminium/uPVC blister strips of 10 tablets each, packed in cartons of
50 tablets.
HDPE bottle consisting of 50 tablets.

6.6

Special precautions for disposal
To be dissolved under the tongue and not to be chewed or swallowed.

7

MARKETING AUTHORISATION HOLDER
Indivior UK Limited
103 - 105 Bath Road
Slough
Berkshire
SL1 3UH
United Kingdom

8

MARKETING AUTHORISATION NUMBER(S)
PL 36699/0005

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
11/11/1980

10

/

17/05/2002

DATE OF REVISION OF THE TEXT
18/05/2016

Expand Transcript

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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