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ANTURAN TABLETS 100MG

Active substance(s): SULFINPYRAZONE / SULFINPYRAZONE / SULFINPYRAZONE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
ANTURAN® Tablets 100 mg
Sulfinpyrazone 100 mg Tablets

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION
The active ingredient is 1,2-Diphenyl-3,5-dioxo-4-(2-phenylsulphinylethyl)pyrazolidine (= sulfinpyrazone B.P.)
Each coated tablet contains 100 mg sulphinpyrazone.

3.

PHARMACEUTICAL FORM
Coated tablets.

4.

CLINICAL PARTICULARS

4.1.

Therapeutic Indications
Chronic, including tophaceous gout; recurrent gouty arthritis; hyperuricaemia.

4.2.

Posology and Method of Administration
Anturan is administered orally in tablet form with meals or milk.
Adults: 100-200mg daily increasing gradually (over the first two or three
weeks) to 600mg daily (rarely 800mg), and maintained until the serum urate
level has fallen within the normal range. Subsequent dosage should be
reduced, to the lowest level which maintains serum urate within the normal
range. Maintenance dose may be as low as 200mg daily. Reduced dose
required in renal impairment. Not to be used in severe renal impairment.
Children: Paediatric usage not established.

4.3.

Contra-Indications
Acute attacks of gout. Treatment with Anturan should not be initiated during
an acute attack of gout.
Gastric and duodenal ulcer (overt or case-history).
Known hypersensitivity to sulfinpyrazone and other pyrazolone derivatives.
Sulfinpyrazone is contra-indicated in patients in whom attacks of asthma,
urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or by other
drugs with prostaglandin-synthetase inhibiting activity.
Severe parenchymal lesions of the liver or kidneys (also in the case history).
Porphyria. Blood dyscrasias (also in the case history). Haemorrhagic
diatheses (e.g. blood coagulation disorders).
In the treatment of chronic gout salicylates antagonise the action of Anturan
and should not be given concurrently.

4.4.

Special Warnings and Special Precautions for Use
Warnings
During the early stages of treatment in patients with hyperuricaemia or gout,
acute attacks of gout may be precipitated. To help prevent episodes of
urolithiasis or renal colic, ensure adequate fluid intake and alkalinisation of the
urine during initial stages of therapy.
Since Anturan may cause salt and water retention, caution is called for in
patients with overt or latent heart failure.
For the early detection of a haematological abnormality, careful clinical
supervision and full blood count should be done before and at regular intervals
during treatment.
Precautions
Use with caution in patients with impaired renal function.
In patients with an elevated plasma uric acid level and/or with a history of
nephrolithiasis or renal colic, and also when resuming treatment after
interruption of the medication, a cautious incremental dosage schedule should
be adopted. As with any form of long-term uricosuric medication, renal
function tests should be performed regularly, particularly in cases where there
is pre-existing evidence of renal failure.

4.5.

Interaction with other Medicinal Products and other Forms of Interaction
Since Anturan may potentiate the action of coumarin-type anticoagulants,
frequent estimation of prothrombin time should be undertaken when these
drugs are given concurrently, and the dosage of anticoagulant adjusted
accordingly.
Anturan may also potentiate the action of other plasma protein binding drugs
such as hypoglycaemic agents and sulphonamides, which may necessitate a
modification in dosage.
Penicillins (e.g. penicillin G): Inhibition of tubular secretion may raise the
plasma concentrations of penicillins.
Theophylline: Activation of microsomal liver enzymes and resultant
acceleration of metabolism lowers the plasma concentration of theophylline.
Phenytoin: Displacement of phenytoin from its plasma protein-binding sites as
well as inhibition of microsomal liver enzymes delays the metabolism of
phenytoin, thus prolonging its half-life and raising its plasma concentration.
Substances affecting haemostasis: Such substances, e.g. non-steroidal
antirheumatic drugs, may exert a synergistic effect on the blood coagulation
system and thus increase the risk of haemorrhage.

4.6.

Pregnancy and Lactation
Anturan should be used with caution in pregnant women, weighing the
potential risk against the possible benefits.
It is not known whether the active substance of Anturan and/or its
metabolite(s) pass into breast milk. For safety reasons mothers should refrain
from taking the drug.

4.7.

Effects on Ability to Drive and Use Machines
None known.

4.8.

Undesirable Effects
Gastro-intestinal tract:
Frequent: mild transient gastro-intestinal upsets, such as nausea, vomiting,
diarrhoea.

In isolated cases: gastro-intestinal bleeding and ulcers.
Urogenital system:
Rare: acute renal failure (mostly reversible), especially with high initial
dosages.
In isolated cases: salt and water retention.
Skin:
Rare: allergic skin reactions (e.g. drug rash, urticaria).
Blood:
In isolated cases: leucopenia, thrombocytopenia, agranulocytosis, aplastic
anaemia.
Liver:
In isolated cases: hepatic dysfunction (increase in transaminases and alkaline
phosphatase), jaundice, and hepatitis.

4.9.

Overdose
Signs and symptoms
Nausea, vomiting, abdominal pains, diarrhoea, hypotension, cardiac
arrhythmias, hyperventilation, respiratory disorders, impairment of
consciousness, coma, epileptic seizures, oliguria or anuria, acute renal failure,
renal colic.
Treatment
Immediate treatment consists of forced emesis to recover undigested tablets.
This is followed by gastric lavage preferably with mild alkaline solution such
as sodium bicarbonate solution and supportive therapy as indicated.
Note that forced diuresis is of no value.

5.

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic Properties
Mode of action: Anturan lowers serum urate levels by blocking tubular
reabsorption, thereby increasing renal excretion of uric acid. As a result of
increased excretion, serum urate deposits are mobilised and tophi are no longer
formed.

5.2

Pharmacokinetic Properties
Pharmacokinetics: After oral administration the active substance is absorbed
rapidly and almost completely (> 85%).
Following a single oral dose of 100mg or 200mg, sulfinpyrazone, peak plasma
concentrations of 5-6μg/ml or 13-22μg/ml, respectively, are attained after 1-2
hours. Sulfinpyrazone has a half-life of 2-4 hours.
Following repeated administration of sulfinpyrazone in a dosage of 400mg bid
for 23 days, a significant decrease in the AUC values and an increase in the
drug's clearance was observed as compared with the values recorded after a
single dose. After multiple dosing with 400mg bid, the mean steady-state
concentration of sulfinpyrazone amounts to 5.1μg/ml, which corresponds to
only half of the calculated value after a single dose (9.6μg.ml). The reason for
this is an increase in total clearance brought about by the fact that the drug
induces its own metabolism.
Sulfinpyrazone is metabolised by reduction to the sulphide and by oxidation to
the sulphone and to hydroxy-compounds. The sulphide metabolite inhibits
platelet aggregation in vitro about 12 times more strongly than sulfinpyrazone
itself. In comparison with sulfinpyrazone the plasma concentrations of the
sulphide metabolite are low. Peak sulphide concentrations are reached approx.
19 hours after administration of a single dose.

5.3

Pre-clinical Safety Data
Animal experimental findings indicate that Anturan is neither mutagenic nor
carcinogenic or teratogenic.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose, maize starch, aerosil 200, magnesium stearate, gelatin, sodium starch
glycollate, sucrose, talc, povidone, titanium dioxide (E 171), polyethylene glycol,
avicel, yellow iron oxide (E 172), red iron oxide (E172), black iron oxide (E172),
ammonium hydroxide, shellac glaze, and propylene glycol (E490/E1520).

6.2

Incompatibilities

None known.

6.3

Shelf-Life
Five years.

6.4

Special precautions for storage
Do not store above 25°C. Store in the original container in a dry place.

6.5

Nature and Contents of Container
Containers and blister packs of 84 tablets.

6.6

Instruction for Use, Handling and Disposal
None.

7

MARKETING AUTHORISATION HOLDER
Amdipharm UK Limited
Capital House, 85 King William Street,
London EC4N 7BL, UK

8.

MARKETING AUTHORISATION NUMBER(S)
PL 20072/0024

9.
DATE OF FIRST AUTHORISATION/RENEWAL OF
AUTHORISATION
1st January 2005

10

DATE OF REVISION OF THE TEXT
03/08/2016

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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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