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What is Allopurinol?
The drug Allopurinol is one of the most important drugs in elevated levels of uric acid in the blood (hyperuricemia) and its sequelae such as chronic gout. He is generally well tolerated, however, interactions must be considered with other medications depending on Allopurinol dose. Here you can read everything about the effect of Allopurinol, side effects and use.
A drug that interferes with the synthesis of uric acid. It is a structural analogue of hypoxanthine. It inhibits the enzyme xanthine oxidase, which is involved in the conversion of hypoxanthine to xanthine and xanthine into uric acid. This explains that they can not be used to protect against infection and prevent their infection in tissues and kidneys. When taking Allopurinol, the excretion of urine hypoxanthine and xanthine increases.
After oral administration, almost completely (by 90%) is absorbed from the digestive tract. Metabolized with the formation of alloxanthin, which retains the ability to inhibit xanthine oxidase long enough. Cmax of Allopurinol in blood plasma, after an average of 1.5 hours, alloxanthin – 4.5 hours after a single dose.
T1 / 2 Allopurinol is 1-2 hours, alloxanthin is about 15 hours. About 20% of the dose is taken through the intestine, the rest – by the kidneys.
Treatment and prevention of gout and hyperuricemia of various genesis (including in combination with nephrolithiasis, renal insufficiency, urate nephropathy). Recurrent mixed oxalate-calcium kidney stones in the presence of hyperuricosuria. Increased urate formation after enzymatic disorders. Prophylaxis of acute nephropathy in cytostatic and radiation therapy of tumors and leukemia, as well as with complete medical starvation.
Established individually, controlled by the concentration of urate and uric acid in the blood and urine. Adults with oral administration – 100-900 mg / day, depending on the severity of the disease. The frequency of taking 2-4 times / day after eating. Children under the age of 15 years – 10-20 mg / kg / day or 100-400 mg / day.
Maximum doses: for violations of kidney function (including those caused by urate nephropathy) – 100 mg / day. An increase in the dose is possible in those cases when, on the background of the therapy, an increased concentration of urate in the blood and urine remains.
From the cardiovascular system: in isolated cases – arterial hypertension, bradycardia.
From the digestive system: dyspeptic phenomena (including nausea, vomiting), diarrhea, transient increase in the activity of transaminases in the blood serum; rarely – hepatitis; in isolated cases – stomatitis, violations of the liver (transient increase in the activity of transaminases and alkaline phosphatase), steatorrhea.
From the side of the central nervous system and the peripheral nervous system: in isolated cases – weakness, fatigue, headache, dizziness, ataxia, drowsiness, depression, coma, paresis, paresthesia, convulsions, neuropathies, visual impairment, cataracts, changes in the papillae of the optic nerve, Feel.
On the part of the hematopoiesis system: in some cases – thrombocytopenia, agranulocytosis and aplastic anemia, leukopenia (most probabilities in patients with impaired renal function).
From the urinary system: rarely – interstitial nephritis; in single cases – edema, uremia, hematuria.
On the part of the endocrine system: in single cases – infertility, impotence, gynecomastia, diabetes mellitus.
From the side of metabolism: in isolated cases – hyperlipidemia.
Allergic reactions: skin rash, hyperemia, itching; in some cases – angioimmunoblastnaya lymphadenopathy, arthralgia, fever, eosinophilia, fever, Stevens-Johnson syndrome, Lyell’s syndrome.
Dermatological reactions: in isolated cases – furunculosis, alopecia, hair discoloration.
How does Allopurinol work?
The structure of the drug Allopurinol is very similar to that of hypoxanthine, a degradation product of nucleic acid metabolism (nucleic acids are the building blocks of the genetic material). This hypoxanthine is converted by an enzyme, xanthine oxidase, into uric acid, which is excreted through the kidneys into the urine.
If accumulates too much uric acid in the body due to disease or malnutrition (meat-rich diet), this crystallizes. The crystals are deposited mainly in the joints, where they cause inflammation, a movement restriction and pain – doctors speak then of gout. Also in the kidney are uric acid crystals can deposit (gout kidney). There you can kidney stones “grow up” and increasingly interfere with the function of the kidneys – the way to renal failure.
Allopurinol blocks the enzyme xanthine oxidase, and thus the degradation of hypoxanthine to uric acid. The precursors of uric acid can also be excreted via the kidneys, however: they do not tend to form crystals.
In the body Allopurinol is almost completely converted within two hours after ingestion in oxypurinol, but both forms inhibit the enzyme in question. Oxypurinol is excreted very slowly for 18 to 43 hours via the kidneys in the urine.
What is Allopurinol used for?
The drug Allopurinol is used in adults as a drug of first choice for the treatment of hyperuricemia (elevated uric acid levels in the blood) used, which makes usually only by secondary diseases such as gout, kidney stones and other kidney ailments noticeable. However, initiation of therapy should always be tried before that to get high purine or uric acid levels by diet under control, such as a meat-free diet.
The therapy with Allopurinol is usually long term, provided that the uric acid levels do not normalize by the change in diet. Allopurinol but is only suitable as a preventive measure of acute gout attacks (sudden severe, inflammatory), but not for the treatment of a seizure – taking during a seizure may increase the acute pain.
How to take Allopurinol?
Allopurinol is applied in the form of tablets. Based on the levels of uric acid in the blood, the doctor determines the individual Allopurinol dosage. For this purpose, usually once a day started with a hundred milligrams of Allopurinol and then gradually increased if needed. The maximum Allopurinol dose per day is eight hundred milligrams, which in several doses (morning, noon, evening) is split.
Because Allopurinol inhibits the formation of uric acid, it is referred to as Urikostatikum. In severe cases, a uricosuric can additionally be given a drug that promotes the excretion of uric acid (eg, probenecid or benzbromarone). There are also tablets that already contain both active substances (Allopurinol and uricosuric).
What are the special instructions for taking Allopurinol?
For patients with existing liver or kidney disease specific dosage recommendations apply.
When and heart failure (congestive heart failure) Allopurinol may only be used very carefully, as this may renal function is limited. Is due to the increased levels of uric acid the kidney already involved (so-called “gouty kidney” kidney stones), attention must be paid to the fact that at least two liters of urine per day are produced. This can be achieved by adding sufficient liquid is drunk.
Allopurinol may interact with various medications. Examples:
- In combination with antibiotics such as Ampicillin and can increasingly rashes occur.
- anticoagulant coumarin-type can be enhanced in its effect, which is why initially there should be a close monitoring of blood coagulation.
- asthma medications such as Theophylline are inhibited in their degradation and may need to be dosed less to avoid poisonous (toxic) effects.
- With simultaneous application of cytostatics (cancer drugs) occur more frequently blood disorders. This must be especially monitored.
- Allopurinol can the degradation of drugs such as Phenytoin (at), chlorpropamide inhibit (in diabetes) and ciclosporin (for autoimmune diseases and after transplants). Their dose must therefore possibly be reduced by the doctor.
During pregnancy and lactation Allopurinol should not be used, since this requires the data are insufficiently. In addition, the drug has been shown in animal studies as a reproductive prejudicial (toxic for reproduction).
How to buy medication with Allopurinol?
All medicines containing the active substance Allopurinol require a prescription because of the wide-ranging interactions with other drugs and to apply only through the pharmacy. But you can buy Allopurinol tablets online from UK.
Since when Allopurinol is known?
Allopurinol was first approved in the US in the year 1966th After the patent had expired, numerous generic preparations of the original (generic) came on the market.
In 1977, the active ingredient of the World Health Organization (WHO) has been added to the list of essential medicines. This list includes all active ingredients that are needed to provide the most urgent needs of the population to health care satisfied.