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Azapropazone
Systematic (IUPAC) name
5-dimethylamino-9-methyl-2-prop-2-enylpyrazolo[1,2-a][1,2,4]benzotriazine-1,3-dione
Identifiers
CAS number  ?
ATC code M01AX04
PubChem 5287724
Chemical data
Formula C 16H18N4O2  
Mol. mass 298.33972 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status POM (UK)
Routes  ?

Azapropazone is a non-steroidal anti-inflammatory drug. It is manufacturered by Goldshield under the tradename Rheumox. It is available in the  United Kingdom as a prescription-only drug; with restrictions due to certain contra-indications and side-effects.

Chemistry:

a ketone derivative of pyrazole

Therapeutic uses :

Azapropazone can be used to relieve pain caused by rheumatoid arthritis, ankylosing spondylitis and gout when alternative treatments have failed.

Cautions

Before taking Azapropazone make sure your doctor or pharmacist knows:

if you are pregnant, trying for a baby or breast-feeding if you suffer from liver, kidney or heart problems if you suffer from hypertension (high blood pressure) or systemic lupus erythematosus (SLE) if you suffer from rhinitis, asthma, or breathing problems if you have ever had an unusual reaction after taking aspirin or NSAIDs if you get indigestion or heartburn if you suffer from peptic (stomach) ulcer, inflammatory bowel disease or any other digestive problems if you have ever had blood clotting problems if you suffer from porphyria if you have ever had an allergic reaction to this or any other medicine if you are taking any other medicines, including those available to buy without a prescription, herbal and complementary medicines

Administration:

Take your medication exactly as directed by your doctor. Take Azapropazone with or immediately after food. Azapropazone is for you. Never give it to others even if their condition appears to be the same as yours. If you suspect that you or someone else has taken an overdose of Azapropazone contact your doctor or go to the accident and emergency department of your local hospital at once. Always take the container with you, if possible, even if empty.

Getting the most from your treatment

Before taking any 'over-the-counter' medicines, check with your pharmacist which medicines are safe for you to take alongside Azapropazone. Keep your regular appointments with your doctor so that your progress can be monitored. If you experience indigestion after taking Azapropazone try taking the next dose with a glass of milk.

Dosage:

Azapropazone is available in tablet and capsule form. The usual dose is 1200 mg per day, given as 600 mg twice daily. This may be reduced to 900 mg for maintenance therapy or increased to 1800 mg if required. Azapropazone is principally excreted unchanged by the kidney. In patients over 65 years of age, whose renal function may be reduced, it is therefore suggested that the starting dose be 300 mg in the morning and 600 mg at night. In patients much older than this, a suitable starting regimen is 600 mg at night or 300 mg twice daily. This dosage can be subsequently adjusted since some elderly patients have excellent renal function. In acute gout, 2,4 g may be given in divided doses during the first 24 hours, followed by 1,8 g daily until the attack is resolving, then reduced to 1,2 g daily until symptoms have disappeared. [2]

Side effects:

Along with their useful effects, all medicines can cause unwanted side effects, which usually improve as your body adjusts to the new medicine. Speak with your doctor if any of the following side effects continue or become troublesome.

Azapropazone is likely to cause your skin to become more sensitive to sunlight than it is usually. Avoid direct sunlight and sunbeds and use a sun protection cream higher than factor 15. Feeling or being sick, tummy pain, heartburn, diarrhoea, swelling feet or lower legs, headache, dizziness, nervousness or depression, drowsiness, problems sleeping, numbness in your hands or feet, tiredness, general feeling of being unwell, disturbance in vision, ringing or buzzing in the ears.

Important: If you experience swelling of the lips, mouth and throat; wheezing or breathing problems; yellowing of the skin or whites of the eyes; a high temperature with a sore throat or if you experience black or bloody stools or blood in the urine stop taking this medicine immediately and consult your doctor or accident and emergency department of your local hospital as soon as possible.

This medicine may cause drowsiness and dizziness. Before having any kind of surgery, including dental or emergency treatment, tell the doctor, dentist or surgeon you are taking Azapropazone.

If you experience any other worrying side effects which you think may be due to this medicine, discuss them with your doctor or pharmacist.

Storage:

Keep all medicines out of the reach of children. Store in a cool dry place, away from direct heat and light. Never keep out of date or unwanted medicines. Discard them safely out of the reach of children or take them to your local pharmacist who will dispose of them for you. [1]

References:

[1] http://www.patient.co.uk/showdoc/30002267/ [2] http://home.intekom.com/pharm/cont_eth/rheumox.html








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