Harpagin F.c. Tablets
Composition:
Each film-coated tablet contains:
Benzbromarone 20.0 mg
Allopurinol 100.0 mg
Active Ingredients:
Benzbromarone 20 mg
Allopurinol 100mg
Inactive Ingredients:
Sodium Starch Glycolate, Tween® 80, Polyvinylpyrrolidone,Titanium dioxide, Magnesium stearate, Talc, Colloidal Silicon-dioxide, Polyaminomethacrylate
(Eudraigt E) dry substance, Polyethylene glycol 6000, Isopropanol, Purified water.
Pharmaceutical form:
Film-coated tablet
Pharmacological action:
Allopurinol acts on purine catabolism without disrupting the biosynthesis of purines. It reduces the production of uric acid by inhibiting the biochemical reactions immediatly preceding its formation. The degree of this decrease is dose dependent. Allopurinol is a structure analogue of the natural purine base, hypoxanthine.
It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and xanthine to uric acid, the end product of purine
metabolism in man. Allopurinol is metabolised to the corresponding xanthine analogue, oxypurinol (alloxanthine) which also is an inhibitor of xanthine oxidase.
Allopurinol reduces both the serum and urinary uric acid levels by inhibiting the formation of uric acid. Benzbromarone, uricosuric agent, lowers the serum uric
acid level by increasing urinary excretion of uric acid this is done by inhibiting the proximal tubular reabsorption of uric acid in nephrons.
Pharmacokinetics:
Allopurinol is absorbed rapidly after its ingestion and between 30 to 60 minutes, it reaches its highest plasmatic concentrations. In avarage, 20% is excreted through the feces in a lapse of 48 to 72 hours, as a non absorbed medication Allopurinol is rapidly eliminated from the plasma, it has a mean life of 2 to 3 hours as it is converted to alloxanthine. Less than 10% of a single dose or an average of 30% of the medicine taken for longer periods is excreted through urine. Allopurinol and its metabolite alloxanthine are distributed along the total tissular water, except on the cerebrum, where its concentration is 33% of the concentration observed in the rest of the tissues. Neither compound is linked to plasmatic proteins. their concentrations in plasma have no direct relation with their therapeutic or toxic effects.
Benzbromarone is only partially absorbed from the gastrointestinal tract reaching peak plasma concentration about 2 to 4 hours after a dose by mouth.
Benzbromarone is extensively bound to plasma proteins. It is metabolized in the liver, and is excreted mainly in the feces, a small amount appears in the urine.
Indications:
– All forms of uric acid accumulation in blood (primary and secondary hyperuricemia).
– Harpagin is not suitable for use in acute attacks of gout.
Dosage and administration:
Unless otherwise prescribed by the physician, swallow 1 film-coated tablet once or twice per day as a whole after meals with plenty of liquid.
Contraindications:
Severe disturbances of renal function (creatinine clearance below 5ml/min gouty nephropathy), pregnancy, and lactation period. hypersensitivity to Harpagin,
haemochromatosis, children under 14 years.
Side effects:
Transient gastrointestinal disturbances, and allergic skin reactions may sporadically appear.
Exfoliative dermatitis, cholestasis, cephalgia, tiredness, and dizziness seldom appear. Such complaints disappear when therapy is over. It is also possible for
the therapy to go ahead by declining dose. Leucopenia and thrombocytopenia seldom can appear.
Drug interactions:
The metabolism of 6-Mercaptopurine is inhibited by Harpagin thus the dose of Azathioprine or 6-Mercaptopurine should be reduced to the quarter when the
drugs are given concomitantly.
Harpagin may interfer with the hepatic inactivation of oral anticoagulants, Harpagin may delay the elimination of probenecid and increase its concentration in
plasma.
Pregnancy and lactation:
Harpagin should not be used during pregnancy or breastfeeding.
Warnings and precautions:
Harpagin (allopurinol) should be discontinued at the first appearance of skin rash or other signs which may indicate an allergic reactions. In some instance a
skin rash may be followed by more severe hypersensitivity reactions such as exfoliative, urticarial and purpuric lesions as well as Steven’s Johnson syndrome
(erythema multiform exsudativum), and/or general vasculitis, irreversible hepatotoxicity .
Package & Storage:
Carton box containing 2&3 strips each of 10 film-coated tablets & insert leaflet
Store below 30’c and protect from light
Keep all drugs out of reach of children
Manufactured by:
Marcyrl Pharmaceutical Industries
