The main component that is the basis of the drug is leflunomide. It is contained in a volume of 10, 20, and 100 mg and helps to reduce inflammation. The active component inhibits the production of dehydrogenase dehydrogenase and does not allow the affected tissues to grow. Leflunomide does not allow excessive activity of mitogen proliferation and DNA synthesis of T-lymphocytes.
Arava is available exclusively in tablet form.
The drug is very well absorbed, the bioavailability percentage is an average of 89 percent. Pills are not tied to a meal schedule; they can be drunk both before and after meals. The maximum content of the main component in the blood occurs in different ways, at times this time is an hour, but can reach 24 hours.
The active component breaks down into several metabolites, the main of which is A771726, and it is he who is responsible for the main therapeutic properties of the drug. The same metabolite exhibits antiproliferative activity, due to which the growth of lymphocytes is reduced.
The components of the drug are removed from the body for a very long time. The average clearance is 31 ml / h. It is excreted through the kidneys for two weeks, can be excreted along with feces.
Indications for taking the drug
The reason for the appointment of Arava is rheumatoid arthritis in the acute stage. It is prescribed for psoriatic arthritis, also in the stage of exacerbation of the disease.
- In no case should you prescribe a remedy for an allergic reaction to the main component or any other that is part of the composition;
- It should not be used in patients with impaired liver function;
- These tablets are strictly contraindicated for AIDS patients or in the presence of other immunodeficiency diseases, especially in severe manifestations;
- With violations of bone marrow hematopoiesis or with a strong decrease in hemoglobin, white blood cells, platelets, if the cause was not rheumatoid arthritis, taking the drug is strictly contraindicated;
- In the presence of severe infections that are difficult to treat;
- In moderate to severe renal failure, Arava is also not recommended;
- A severe form of lowering the level of total protein in the blood;
- It is impossible to take the drug during pregnancy, during the entire period of bearing a child, since the components actively penetrate the placenta, exerting a negative effect on the fetus;
- You can not take pills at the time of breastfeeding, it will also negatively affect the health of the baby;
- Admission of Arava negatively affects the quality of sperm in men, therefore it should not be allowed for a man to have sex without reliable contraception while taking the pills;
- The drug is not prescribed for children under 18 years of age; it is intended for use only by adult patients.
Do not take Arava to women of childbearing age who are not strictly monitoring contraception. Such prudence is needed in order to avoid an unplanned pregnancy during the treatment period.
Even after the cancellation of Arava, it is impossible to immediately conceive a child, about two years must pass before all toxic substances are eliminated from the body and do not affect the development of the future baby. To do this, a woman must pass special tests that will show at what level the toxic element in her body is currently located.
The value of the indicator should not be more than 0,02 mg / l. After two weeks, the analysis must be passed again, if the level is the same, you can safely proceed to the conception of the baby.
To accelerate the excretion of the active component, you can carry out the “washing” procedure.
For this purpose, Colestyramine in an amount of 11 g is introduced into the patient’s body for 8 days three times a day. This drug can be replaced with Activated Carbon. It should also be taken for 11 days, but four times a day, a single dosage of 50 mg. For better assimilation of the tablets, it is worth crushing.
This procedure is designed to reduce the overestimated content of the main ingredient in the patient’s body to an acceptable level of 0,02 mg. It is worth considering that during the “laundering” the effectiveness of oral contraceptives is significantly reduced.
It doesn’t matter which of the two drugs a woman chooses. Therefore, for the duration of the procedures it is advisable to use also mechanical protective equipment – for example, condoms.
Instructions for use
In the case of rheumatoid arthritis in the first days of administration, the highest dosage is prescribed – 100 mg once a day. At this dosage, the drug is taken for three days, no longer. This dose is called loading and allows you to quickly begin to act the active component, accelerating its effect on the body.
In the future, the dose is reduced to 20 mg per day, you need to take the drug for a long time, the exact term is determined by the doctor.
In some cases, if there is a risk of provoking adverse reactions, especially from the gastrointestinal tract, the loading dose is excluded from the course, proceeding immediately to the maintenance one.
If the patient does not tolerate even 20 mg, it makes sense to switch to a dosage of 10 mg per day. From reducing the dosage in the first days, the effectiveness of treatment does not decrease, but the moment of onset of relief comes later.
With psoriatic arthritis, the treatment regimen is the same, first there is three days of stress treatment, after which they go to the stage of maintenance treatment. The first positive result occurs in one and a half to two months. In the future, the effect intensifies and increases over the course of six months.
- Quite often, against the background of taking the drug, an increase in blood pressure occurs, hypertensive patients should especially carefully monitor the indicators;
- There are also often adverse reactions from the gastrointestinal tract, they manifest themselves in the form of diarrhea, vomiting, nausea, if you do not take timely measures, anorexia is likely;
- Aphthous stomatitis and other lesions of the mucous membrane in the mouth are likely;
- Pain in the abdomen is not excluded, the activity of hepatic transaminases increases, taste buds may malfunction, the likelihood of hepatitis is not ruled out, pancreatitis, acute liver necrosis are extremely rare;
- Not often, but still there is a possibility of interstitial lung disease, sometimes this s >
In view of the large list of contraindications and adverse reactions, Arava begins to be taken only after a comprehensive examination. For the same reason, with great care, they introduce it to patients older than 65 years.
We must not forget the fact that even after the cessation of the therapeutic course due to the long half-life, there is still a chance of adverse reactions. The possibility of the onset of severe forms of allergies is not excluded.
If for some reason there is a need for urgent removal of traces of the drug, you need to use the “laundering” system based on activated carbon or Colestyramine (described in the “Contraindications” section).
Due to the fact that the main metabolite of leflunomide has a sufficiently high toxicity and is excreted by the liver, it may have too severe an effect on this organ. For this reason, in the presence of liver diseases, it is better to refuse the use of Arava, choosing a more suitable drug from analogues.
With liver diseases, severe damage to this organ can occur, up to a fatal outcome. Such a development of events most often happens in the first six months of drug therapy. Such consequences can be avoided by strictly following the doctor’s recommendations in compliance with all dosages.
To reduce the risk of adverse reactions from the liver, it is worthwhile to determine the level of ALT activity before starting a therapeutic course. In the future, this analysis also makes sense at least once every two months. This will avoid problems in the future.
If the analysis reveals an increase in ALT at least a couple of times, it makes sense to reduce the dosage to the minimum – 10 mg per day, if even in this case the level does not stabilize, the drug should be completely abandoned. Taking the drug can only be continued if the indicator stabilizes.
If in the past the patient has had a decrease in hemoglobin, white blood cells or platelets, the risk of hematological reactions increases. The same problem can happen with those patients who have abnormalities in bone marrow function or are at high risk of suppressing bone marrow function.
To prevent the occurrence of such a reaction, before the start of therapy, it is necessary to determine the number of platelets, in the future it is necessary to regularly conduct this analysis at least every two months.
Requires constant monitoring of platelet count and in the following cases:
- If the patient has recently taken hematotoxic drugs, or these drugs were taken in tandem with immunosuppressive drugs. Such control is also required when the “laundering” period has not been carried out;
- In the presence of blood discharge in terms of;
- Control is also required if these indicators are constantly not in a stable state and are not connected with this inflammation of the joints.
In case of serious adverse reactions, the drug should be stopped immediately and proceed with the “laundering” procedure.
Despite the fact that the drug has long been actively used in the treatment of arthritis, there is still no full-fledged study of its combination with many drugs. In particular, there is no data on how leflunomide-based agents with antimalarial drugs behave quite often in rheumatology, such as chloroquinone, hydroxychloroquinone.
Also, the interaction with gold preparations, D-penicillamine, Azathioprine, administered both orally and intramuscularly, has not been studied.
For the simple reason that leflunomide is very difficult to remove from the body and for a long time remains in a sufficiently high concentration, it is not so easy to switch from it to another medication.
In most cases, a “laundering” procedure is required, which will allow the body to be freed of traces of the Arava drug as much as possible and allow other drugs to work fully. However, it should be taken into account that even with the correctly carried out “laundering” procedure, the risk of adverse reactions persists for a long time to come.
In the event of the appearance of dermatological reactions, especially ulcerative stomatitis, the intake of Arava should be stopped immediately. In the event of adverse reactions in the form of Stevens-Johnson syndrome or with the appearance of toxic epidermal necrolysis, it is necessary to immediately stop taking the drug and proceed with the “washing” procedure
It has been established that agents with immunosuppressive actions can have a negative effect on infectious diseases. A person becomes susceptible to various fungal infections. It is noted that such infectious diseases occur in a more severe, intense form, are difficult to treat and often give complications.
In case of infection of this kind of infection, the patient must immediately stop taking the drug Arava and proceed with the “laundering” procedure.
If the patient is prone to frequent colds or is at risk due to tuberculin reactivity, he should be closely monitored. At the first symptoms, refuse further treatment.
During therapy, occasionally there are cases of interstitial pulmonary process. The high-risk group includes those patients in whom this disease is in a quiet stage. This disease can dramatically go into the stage of exacerbation.
As a result, the patient may die. To avoid death, you should be more careful about symptoms such as cough and dyspnea. At the first signs, it is necessary to immediately stop the therapy and proceed to the stage of “washing.” After this, emergency treatment of the interstitial pulmonary process is required.
Situations were noted when peripheral neuropathy occurred in those receiving Arava, after the end of the administration, this side effect passed by itself without outside help. However, there were cases when, at the end of taking the drug, the side effect continued to persist.
In patients older than 65 years with diabetes mellitus taking immunosuppressive drugs, in particular Arava, the risk of peripheral neuropathy increases. In this case, it is worth completely abandoning treatment on the basis of this medication and proceed with the “laundering” procedure.
Overdose cases were noted in those patients who were five times the daily dose. Other common symptoms were diarrhea, severe pain in the lower abdomen, there were cases of a decrease in leukocytes, hemoglobin, and platelets, while, on the contrary, the liver function tests were overestimated.
The first thing to do in case of an overdose, to carry out the “laundering” procedure with Coletiramine or activated carbon, this will speed up the process of naturally removing the active component from the body.
Conducting a standard procedure for gastric lavage using warm salt water will not give the desired result.
Colestyramine should be taken three times a day for 8 g. Already after a day, the content of the active metabolite will decrease by about 40%. After two days, this level is already reduced by 65%.
Activated charcoal in the form of crushed tablets should be taken every 6 hours, then after the first day the level of the active component of Arava will be reduced by 37% in the blood, after another day the initial indicator will drop by half.
However, such an effective “laundering” procedure can be carried out only according to the doctor’s testimony. Doing this yourself should not be. The dialysis procedure does not reduce the active component, since leflunomide is thus not excreted.
Arava’s interaction with other drugs and diagnostic tests
The combined use of hematoxic and immunosuppressive drugs with each other can lead to increased adverse reactions. Taking other hepototoxic drugs, including alcohol, will lead to the same consequences. Switching to other means without the necessary “washing off” procedure in this case also leads to the fact that adverse reactions will manifest themselves with greater force.
You should not combine the intake of Arava and Coletiramine, such a tandem will lead to a significant decrease in the concentration of leflunomide and, as a result, the therapeutic effect of taking these funds. The same reaction will be from taking Activated Carbon.
There were no negative reactions from the combined use of Arava and Methotrexatom, so both drugs are often included in the general course of treatment for rheumatoid arthritis.
With caution, take drugs such as Phenytoin, Tolbutamide, Warfarin in the complex in Arava. The reason is simple, leflunomide significantly reduces the activity of their main components, as a result, the effect of their use becomes many times less than expected. In the case of Warfarin, an increase in prothrombin time also occurs.
The combined use of oral contraceptives and Arava does not have any consequences on the effectiveness of both drugs.
There is no evidence of the efficacy and safety of treatment using live vaccines. It is impossible not to take into account the long half-life of the drug.
Arava is produced in Germany and France, its cost in Russia is quite high, for packaging from a German manufacturer you will have to pay from 2800 rubles, for the French version and even more – from 3100 rubles. Given that this is a means of long-term use, this cost can not be called budgetary, so doctors often resort to analogues of this drug.
Shishkevich Vladimir, orthopedic and traumatologist, project editor-in-chief ExpertNews.
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At the heart of this drug is the same leflunomide. It is available in the form of tablets with a dosage of 10, 20 and 100 mg of the content of the active component. The drug is often prescribed as the main one in the treatment of rheumatoid arthritis, it effectively reduces the symptoms of the disease and helps inhibition of structural damage to the joints. Leflyde is well established in the treatment of psoriatic arthritis.
The therapeutic effect of taking the drug occurs after two weeks and can persist for up to six months from the end of the dose. Tablets should be taken starting with a loading dose for the first three days. After they switch to support mode. The dosage at this time is 10 or 20 mg.
Due to the fact that Leflyde is a structural analogue of Arava, the list of contraindications, adverse reactions, overdoses and interactions with other drugs is completely the same.
The main difference between Leflyde and Arava in price, the first costs from 1800 rubles, which is much cheaper than European counterparts. This difference in cost is due to the fact that Leflyde is a Russian-made drug.
In this preparation, leflunomide is also based. The tool is an active immunomodulating agent, has anti-inflammatory and antiproliferative properties. It interferes with the proliferation and formation of T-lymphocyte DNA.
The properties of the drug are fully consistent with previous structural analogues. The same dosage regimen, adverse reactions and contraindications. Leflunomide also has three dosage forms – 10, 20 and 100 mg.
The cost of the drug starts from one and a half thousand rubles for the packaging of the minimum dosage.
The basis of the drug was mycophenolate mofitel, which is an active non-competitive inhibitor of inosine monophosphate dehydrogenase. Cellsept is not the main treatment for arthritis, it is prescribed in combination with corticosteroids. It helps the body take corticosteroids more easily, preventing medication from being rejected.
Cellsept’s contraindications are minimal – in addition to the standard allergic reaction, this is the period of pregnancy and lactation. A large number of adverse reactions from taking the drug also can not be expected – diarrhea, vomiting, sometimes sepsis and leukopenia.
The cost of the funds can not be called budgetary, you will have to pay at least 3000 rubles for packaging the medicine.
This drug is a structural analogue of Arava, since it is based on the same leflunomide. Often prescribed as a baseline in the treatment of rheumatoid arthritis. As in the case of Arava, there are a number of contraindications that you should pay attention to before you start taking the drug. Adverse reactions are also available. According to the reception scheme, it completely coincides with the analogue.
Elafra is a German drug, so the price is not inferior to its counterpart – in pharmacies for the packaging of tablets they will ask from 3000 rubles.
Despite the fact that all these agents are analogs and many are based on the same substance, it is impossible to change the drugs on their own in any case, this can only be done by the attending physician.
Methotrexate or Arava: which is better?
These drugs are often compared, as both are essential in the treatment of rheumatoid arthritis. But methotrexate is also prescribed for acute lymphocytic leukemia, trophoblastic disease, skin cancer, cervix, vulva, esophagus and other diseases. Moreover, he effectively copes with arthritis in the late stages of the course.
As the main component in the drug is methotrexate. It is an antitumor agent, a folic acid antagonist.
The main effect is associated with inhibition of the production of purines, nucleotides and thymidylate. It does not allow the affected cells to grow, preventing this process.
For ease of administration, the drug has several forms of release – tablets with a dosage of 2,5, 5 and 10 mg, ampoules – 1, 5 10 ml. Available in the form of concentrate – 5, 10 and 50 ml. The drug is prescribed orally, intravenously, intramuscularly, injected into the spinal canal. Such a variety of release forms and dosages allows the use of this drug even in young children up to a year. Which, undoubtedly, is a big plus.
Like Arava, the drug has many contraindications, including pregnancy and the period of breastfeeding, it is prescribed with caution to patients with kidney and liver disease. The list of adverse reactions is also considerable, which must be taken into account. Taking the drug can provoke severe toxic reactions, which is not the best property.
Unlike its predecessor, it has a narrow focus. This is not to say that one drug is much superior to another, each has its own advantages and disadvantages, which the attending physician relies on when making an appointment.
In terms of price, Methotrexate looks much more profitable than Arava, the first one costs only 100 rubles per pack of tablets. Which is much cheaper than Arava.
Natalia “My husband was diagnosed with rheumatoid arthritis. The doctor warned that he would now have to constantly take drugs. They appointed MethodJect as the basis. But he did not fit her husband – there was severe nausea, and the pain only became stronger. Of course, the drug was canceled, Arava was prescribed, it has been taking for more than a month, it is too early to talk about real results, but the state of health has become much better. We hope that our trials will end there. One minus, a very high cost, but nothing can be done, we will take it. ”
Sergey “For twenty years I’ve been suffering from rheumatoid arthritis, I tried all kinds of medicines, schemes, very little, which from all this gave a real result. Because of the gold preparations, jade developed, on Methotrexate I had such vomiting that I could not drink water calmly. Some of the received ones worked for a while, then the effect passed, and the pain returned. About 5 years ago I was discharged from Arava. Also, not everything was so smooth with these pills. At first I had terrible anemia, I had to take Fenyuls. But this is literally in the first month of treatment. then it all went away. Now only they are saved. I take it regularly. ”
Anna “I have been suffering from arthritis for a long time, I have rheumatoid. The pains are getting stronger every year, I don’t know what to take. Long injected methotrexate. It seemed to help not bad, but, probably, the body got used to it or something, and it stopped saving me. My head began to spin, nausea appeared. Today I went to the reception, they wrote me Arava, and I’m just in dismay. It seems that the drug is not cheap, and they produce it abroad, but there are so many side effects from it that I am afraid to drink it. Moreover, the woman in line scared that he did not help at all, only a waste of money. Of course, I’ll buy it anyway, try it, but I don’t really hope for anything. ”