Allopurinol is a drug that can effectively reduce the concentration of uric acid. This prevents the deposition of uric acid salts in the kidneys, bladder and joints. One of the most well-known ailments of the genitourinary system is urolithiasis. This disease is very diverse, since stones in the kidneys and bladder can be of a very different nature and, accordingly, require different treatments. Allopurinol is a drug that prevents the deposition and increase of urate.
Causes of the disease
To treat the disease, medicinal components are used that affect both the individual symptoms of gout and the pathogenetic process as a whole. One such drug is allopurinol. It is used to treat hyperuricemia, the main cause of gout.
The human body contains purines. These are colorless crystals that form salts with mineral acids. Their basic element is xanthine, which is present in all tissues of the body. These crystals are highly soluble in alkaline and acidic solutions.
The body also contains the enzyme xanthine oxidase, which acts as a catalyst in the oxidation of hypoxanthine - a natural derivative of purines - into xanthine. The end product of this metabolism (metabolism) is uric acid. Its significant increase in the body is called hyperuricemia, and the resulting complications are called gout. This happens due to blood circulation throughout the body, which is involved in supplying nutrients to the joints. Thus, uric acid salts enter there and are deposited, causing disease.
Reviews
Considering the fact that the period of accumulation of this medicinal substance in the blood (in sufficient concentration to provide a therapeutic effect) is on average one week, patients suffering from gout should use Allopurinol almost for life. Reviews from doctors are clear: the drug has proven itself well. But this is not a “miracle pill” that you can take and forget about your illness. Gout is more of a lifestyle choice than a chronic disease. But it is “Allopurinol” that helps control the level of lactic acid and prevent exacerbation of the disease and its further progression.
From the point of view of the convenience of prescribing the drug "Allopurinol", reviews from doctors are also positive, because in most cases the patient needs to take the medicine once a day. This minimizes the likelihood of missing a medication dose and, therefore, increases the effectiveness of the therapy.
Metabolic processes
Allopurinol, entering the body, is transposed into oxypurinol during metabolism under the influence of xanthine oxidase . It is an analogue of xanthine that does not oxidize. This happens within two hours after taking the pill. That is, the drug serves as an enzyme inhibitor. Thus, the growth of uric acid in the body is inhibited. The metabolite is then excreted by the kidneys within 24 hours. Therefore, oxypurinol is responsible for the effectiveness of treatment. The drug disrupts the synthesis of uric acid, reduces its amount in the body and promotes the dissolution of its salts.
With a decrease in hyperuricemia, the formation of urate in the joints and urinary system stops. The rapid action of the drug leads to the resorption of nodes and a decrease in pain. Increases joint mobility. The drug is especially effective for chronic manifestations of arthropathy.
Indications
The drug is used for almost all forms of primary - gouty, and secondary hyperuricemia, and sometimes even for preventive purposes with high levels of uric acid. The list of indications for use is quite impressive:
- gout – prescribed even against the background of renal failure;
- kidney stones - with the formation of urates;
- lymphosarcoma, acute leukemia,
- chronic myeloid leukemia;
- traumatic injuries;
- cytostatic and radiation therapy;
- Lesch-Nien syndrome;
- massive glucocorticoid therapy;
- uric acid nephropathy.
pharmachologic effect
When the medicine is taken orally (by mouth), it dissolves and is absorbed in the digestive tract. Reaches peak plasma concentrations within 1.5 hours. Then the drug is absorbed in the small and duodenal intestines. Due to the long period of elimination of components, accumulation (cumulation) of the drug in the body is possible.
Oxypurinol can be eliminated from the body from 18 to 70 hours. The oxypurinol metabolite has the same effect as the main component, but binds longer to enzymes that accelerate chemical reactions in the body.
Allopurinol and oxypurinol are excreted by the kidneys, with almost no binding to plasma proteins . A fifth of the substance is excreted by the intestines within two to three days. If the patient has impaired renal function, the withdrawal period of the drug increases.
In addition to gout, it is prescribed if there are:
- hyperuricemia;
- urate urolithiasis;
- urate nephropathy;
- reperfusion injury of the myocardium;
- kidney stone disease;
- protozoal infection;
- hyperexcretion of uric acid;
- tophi in subchondral bone and soft tissues;
- nephrolithiasis;
- signs of gouty nephropathy;
Therapeutic properties
Reviews from patients indicate that allopurinol does not relieve pain in gout, but is used as a means of preventing attacks . Its main action is aimed at the root cause of the disease, that is, hyperurecemia, to reduce the amount of uric acid in the blood plasma.
It is important to carefully select the correct dosage of allopurinol, as an acute attack of gout or its transition to a chronic form may occur.
Depending on the stage of the disease, an individual set of treatment measures is prescribed. Therapy is as follows:
• it is necessary to stop the attack;
• measures to prevent relapse;
• preventive measures are prescribed to avoid repeated exacerbations.
It is necessary to ensure that the disease does not become chronic.
The use of allopurinol in the chronic course of the disease is based on the prevention of attacks and reducing the level of uric acid in the blood. Basic therapy is carried out in cases where arthritis reminds itself 3-4 times a year, and if there are gouty nodes.
Anti-gout treatment is based on allopurinol. Also, tablets are prescribed if persistent hyperuricemia has been observed, and there has been at least one attack of arthritis in the past.
Allopurinol analogs
Almost any drug has analogs on the market that differ in price or composition. Allopurinol is no exception. There are a number of remedies designed to be taken for gout. The most famous analogues of Allopurinol are Allopurinol-Egis, Allopurinol Sandoz and Purinol.
The drug called Allopurinol-Egis differs slightly in the composition of the auxiliary components. Its dosage, indications and contraindications are the same as Allopurinol.
The same can be said about other analogues. Most often, drugs differ in cost. However, replacing Allopurinol with a similar drug should under no circumstances occur without consulting your doctor.
Features of the course of treatment
When treating the disease, you must follow the following precautions:
- It is better to start gout therapy with small medicinal doses, 100 mg per day. This approach will prevent the development of allergic reactions and possible acute attacks of arthritis that may occur at the initial stage of treatment. It will also reduce adverse reactions from the drug. You can control the selected dose by the rate of decrease in uric acid. Hyperuricemia should decrease by a tenth of the initial values within one month when taking the tablets.
- Uric acid levels rise very quickly when the drug is discontinued, within 3–4 days.
- If there is a painful attack in the joint, it is first recommended to stop it, and then start treatment with allopurinol. If pain develops during treatment, it is necessary to reduce the prescribed dose of the drug. It is not recommended to completely cancel it, since any treatment is based on the principle of an initial deterioration in health, and only then positive progress.
- At the beginning of treatment, to avoid an acute attack of gout caused by the drug, drugs such as colchicine or NSAIDs are prescribed in small doses.
- The level of uric acid during an exacerbation of arthritis, manifested by attacks, is lower than in the period between attacks, therefore it is necessary to control urates over time, that is, after the exacerbation has ceased.
Dangerous consequences
Side effects include the following:
- partial loss of concentration, attention, vision;
- perverted sense of taste;
- drowsiness, apathy, depression;
- increase or decrease in blood pressure;
- anemia;
- swelling;
- infertility;
- decreased potency;
- dermatitis and other skin lesions;
- dehydration;
- furunculosis and other side effects.
Side effects after taking the drug can be avoided if the instructions for use are initially followed. Under no circumstances should the dosage of the drug be increased without the consent or advice of the attending physician.
Treatment effectiveness
After 2–3 days, a decrease in the level of uric acid in the blood is observed, and on days 7–10 the levels return to normal. When uricemia levels decrease, it is also necessary to reduce the dose of the drug. Persistence of normal results occurs after six months, or a little earlier. After this, the patient is transferred to a maintenance dose of 100 mg/day to prevent relapses.
Treatment must be continuous. Reviews show that it takes up to a year to reduce attacks. Over time, the intensity of the disease decreases, and compactions of the subcutaneous tissue begin to dissolve. After long-term use of the medicine, complete disappearance of the joint manifestations of the disease is possible. The use of allopurinol continues continuously for many years.
Dosages and administration
The drug is available in the form of tablets of 0.1 and 0.3 g. It is recommended to take allopurinol after meals to reduce the side effect of intestinal upset. During treatment, it is necessary to drink a lot of fluid to ensure urine output in a volume of 2–2.5 liters, unless there are contraindications from the blood vessels and heart. When analyzed, the urine reaction should be slightly alkaline. This will prevent the formation of stones. To do this, you need to include in your diet the consumption of sour berries, vegetables, and fruits, which will cause alkalization of urine.
What is included?
Allopurinol 300 or Allopurinol Sandoz is offered by manufacturers in tablet form. Tablets contain:
- allopurinol - 100 mg or 300 mg;
- auxiliary components in the form of sucrose, potato starch, magnesium stearate, gelatin, lactose monohydrate and others, subject to the brand of the drug itself - analogues may include various auxiliary substances.
Allopurinol is produced in two formulations, where tablets have 100 or 300 mg of the main component, therefore the drug name is distinguished as Allopurinol-100 and Allopurinol-300. Tablets of 100 or 300 mg are offered by manufacturers in dark glass tubes.
Contraindications and precautions
Reasons why the drug should not be used:
The drug destroys the formation of uric acid in the body. Oxypurinol, a derivative of allopurinol, has a positive effect on the organs of the urinary system. In a complex effect, the components of the drug help dissolve urates and reduce uric acid in the body.
Nutrition and diet
An important component of gout treatment is the need to follow a diet . Fasting is not recommended as it can lead to increased uricemia. During therapeutic nutrition, it is necessary to reduce the consumption of foods containing purines, limit the consumption of salt and fats. The diet should be divided, up to six times a day. Drink more fluids in between.
People who gave up drinking alcohol received positive feedback during treatment. It is necessary to give preference to vegetable proteins and introduce vitamins into the diet. It is beneficial to consume alkaline mineral waters. Also allowed from liquids are weak tea, juices, and fruit drinks. Citrus fruits remove uric acid salts from the body. Patients do not need to grind their food. It is advisable to boil or steam it.
Side effects
The drug is usually well tolerated, but rare undesirable effects are possible.
Some reviews indicated the following reactions:
> allergies, manifested by urticaria (skin rash), itching, angioedema;
> drug intolerance;
> fever;
> eosinophilic leukocytosis, leukopenia, aplastic anemia, agranulocytosis, thrombocytopenia were manifested in the hematopoietic system;
> deterioration of kidney function and renal failure;
> hepatitis, increased activity of liver enzymes;
> infertility, erectile dysfunction, gynecomastia;
> dyspeptic disorders;
> development of gout attacks, joint pain;
> hyperlipidemia and hyperglycemia were observed in metabolism.
> changes in taste, decreased vision, cataracts, retinal degeneration;
> decreased blood pressure with mild hypertension, bradycardia;
> peripheral neuritis, headaches, drowsiness, depression, paralysis.
If such listed syndromes develop, you should stop taking the drug and consult a doctor.
special instructions
Allopurinol indirectly affects water balance and promotes dehydration, and therefore the most important requirement during treatment is the consumption of sufficient amounts of water. The volume of daily urine cannot be less than 2 liters - this is an absolute requirement.
The remaining requirements are no less categorical:
- The drug is incompatible with alcohol, so the latter should be avoided.
- Since the drug causes, or rather can cause, drowsiness and dizziness, you should avoid driving while taking the medicine. Only an observing doctor can say how strictly this prohibition must be observed.
- If there are any factors that cause a decrease in renal function - the use of dierutics, old age, hypertensive therapy, it is necessary to carefully calculate the dose and monitor the patient's condition. If any signs of allergy or dysfunction appear, the drug should be discontinued immediately.
- If the drug is prescribed against the background of disorders in the hematopoietic system, then it is necessary to additionally monitor the blood count. For example, take into account the presence of lactose in a 100 mg tablet when preparing a diet for such a patient.
It is necessary to take into account the incompatibility of allopurinol with a number of medications:
- sulfinpyrazone - this reduces the effectiveness of allopurinol;
- indirect anticoagulants – difekin, theophylline. Allopurinol enhances their effects, including negative ones;
- 6-mercaptopurine, azathioprine - the drug increases the toxicity of the drug, so when taken together, the dose of the drugs must be reduced to ¼–1/3 of the usual;
- thiazide diuretics, furosemide, methacrylic acid - increase the concentration of uric acid, which is exactly the opposite of the effect of allopurinol;
- ampicillin, amoxicillin - when taken together, there is a high risk of skin reactions.
Taking 20 g of the drug causes poisoning: vomiting, dizziness, nausea, fever. Against the background of renal failure, poisoning can occur with a lower dose. The substance does not have a specific antidote. Intoxication is dealt with using the usual methods: rinsing, drip with saline, and possibly prescribing dialysis.
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