Abaggio - Instructions For The Use Of Tablets, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Abagio

Abaggio: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Aubagio

ATX code: L04AA31

Active ingredient: teriflunomide (Teriflunomide)

Producer: Sanofi-Winthrop Industry (France)

Description and photo updated: 2018-29-11

Prices in pharmacies: from 53,500 rubles.

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Abagio is an immunosuppressive drug for suppressing unwanted immune responses in multiple sclerosis.

Release form and composition

The drug is produced in the form of film-coated tablets: pentagonal, pale blue, on one side there is an engraving of the company logo, on the other - "14" (14 pcs. In blisters, 2 blisters in packages of the "sleeve" type, cardboard box 1 or 3 packages and instructions for use Abagio).

1 film-coated tablet contains:

• active substance: teriflunomide - 14 mg;
• auxiliary components: corn starch, sodium carboxymethyl starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, hydroxypropyl cellulose;
• film casing: macrogol, hypromellose, titanium dioxide (E171), indigo carmine-based aluminum varnish (E132), talc.

Pharmacological properties

Pharmacodynamics

Abagio is an immunosuppressive drug intended for use in multiple sclerosis in order to suppress unwanted immune reactions of the body. Its active substance, teriflunomide, has immunomodulatory and anti-inflammatory properties, which are realized by selective and reversible inhibition of the mitochondrial enzyme dihydroorotate dehydrogenase (DHO-DH), which is necessary for the de novo synthesis of pyrimidine. Therefore, it blocks the proliferation of stimulated lymphocytes, which requires de novo synthesis of pyrimidine. It is believed that the mechanism of action of teriflunomide in multiple sclerosis may be due to a decrease in the number of circulating lymphocytes.

Taking teriflunomide in a daily dose of 14 mg has little effect on the change in the number of immune cells in the blood. During the first 12 weeks of therapy, the decrease in the number of lymphocytes is less than 0.3 x 10 ⁹ / L, until the end of treatment, the achieved levels are maintained.

Mean equilibrium drug concentrations do not cause clinically significant lengthening of the QT interval.

There is a decrease in the level of uric acid concentration and the content of phosphorus in serum. It can be assumed that this is not due to changes in glomerular functions, but is associated with an increase in tubular excretion.

The clinical efficacy and safety was assessed based on the results of a study in which patients with relapsing multiple sclerosis (RMS) took daily teriflunomide at a dose of 7 or 14 mg for 108 weeks. For the study, patients with a diagnosis of multiple sclerosis, recurrent course, with or without progression were randomized. The patients had 1 relapse (or more) during the year preceding the study. The average age of the patients was 37.9 years; when included in the study, the mean Extended Disability Scale (EDSS) score was within 5.5. The majority (67.2%) of patients did not take drugs affecting the disease within two years before enrollment in the study.

When comparing the effectiveness of teriflunomide (at a dose of 14 mg once a day) with the effectiveness of interferon beta-1a (subcutaneously at a dose of 0.044 mg three times a week) after 95 weeks of therapy, the number of patients with a confirmed failure of treatment according to the Kaplan-Meier method was: teriflunomide - 41.1%, against the background of interferon beta-1a - 44.4%. According to the results of the study, 19.8% of patients completely stopped using the drug, of which 3.6% - due to the lack of a sufficient effect, 10.8% - due to the development of adverse events.

The efficacy and safety of using teriflunomide under the age of 18 has not been established.

Pharmacokinetics

After repeated oral administration, the maximum plasma concentration (C _max) of teriflunomide is reached on average after 1–4 hours. The bioavailability of Abagio is approximately 100%. Simultaneous food intake has no clinically significant effect on the pharmacokinetics of teriflunomide.

The equilibrium concentration (C _ss) in plasma is observed after about 100 days and exceeds the initial total concentration of teriflunomide by about 34 times.

Plasma protein binding is more than 99%. Teriflunomide binds, most likely, to albumin and is actively distributed in plasma.

V _d (volume of distribution) is low.

Teriflunomide is metabolized moderately, the first stage of biotransformation is hydrolysis, the second is oxidation.

It is excreted unchanged, mainly with bile through the intestines.

T _1/2 (half-life) after repeated administration is 19 days.

If it is necessary to reduce the plasma concentration of teriflunomide, its elimination from the bloodstream can be accelerated by prescribing cholestyramine (4 or 8 g 3 times a day, depending on tolerance) or activated carbon (50 g 2 times a day).

Indications for use

Abagio is indicated for the treatment of relapsing-remitting multiple sclerosis in adult patients.

Contraindications

Absolute:

• severe liver failure (class C on the Child-Pugh scale);
• severe immunodeficiency, including acquired immunodeficiency syndrome (AIDS);
• clinically significant anemia, thrombocytopenia, leukopenia, neutropenia and other pronounced disorders of bone marrow hematopoiesis;
• severe hypoproteinemia;
• severe stage of renal failure requiring hemodialysis;
• severe forms of active infections;
• galactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
• childbearing age in women who do not use reliable methods of contraception, with a plasma concentration of teriflunomide above 0.02 mg / l;
• period of pregnancy;
• lactation;
• age up to 18 years;
• hypersensitivity to drug components.

With caution, Abagio should be prescribed to patients who abuse alcohol, elderly patients (65 years and older).

Abaggio, instructions for use: method and dosage

Abagio tablets are taken orally, swallowed whole and washed down with a sufficient amount of water, regardless of the meal.

Recommended dosage: 1 pc. Once a day.

Side effects

• on the part of the immune system: often - mild allergic reactions;
• mental disorders: often - anxiety;
• infectious complications: very often - laryngitis, upper respiratory tract infections, influenza, mycosis of the feet, urinary tract infections; often - periodontal infections, oral herpes, sinusitis, pharyngitis, bronchitis, viral gastroenteritis, cystitis;
• from the lymphatic system and the hematopoietic system: often - neutropenia; infrequently - mild thrombocytopenia, anemia;
• on the part of the cardiovascular system: often - hypertension;
• from the nervous system: very often - paresthesia; often - neuralgia, lumbosacral radiculitis, hyperesthesia, diseases of the carpal tunnel, peripheral neuropathy;
• from the respiratory system: interstitial lung disease;
• from the digestive system: very often - nausea, diarrhea; often - toothache, vomiting; very rarely - pancreatitis;
• on the part of the musculoskeletal system and connective tissue: often - myalgia, musculoskeletal pain;
• from the reproductive system: often - menorrhagia;
• from the urinary system: often - pollakiuria;
• dermatological reactions: very often - alopecia [including thinning hair, decreased hair density, hair loss associated or not associated with changes in hair texture, diffuse or generalized damage to the entire scalp (without complete hair loss)]; often - acne, rash;
• laboratory indicators: very often - an increase in the level of alanine aminotransferase (ALT); often - an increase in the level of gamma-glutamyltransferase and aspartate aminotransferase (AST), a decrease in the number of neutrophils and leukocytes, a decrease in body weight;
• others: often - pain, post-traumatic pain.

Overdose

Overdose symptoms have not been established.

Treatment: if a significant overdose or toxicity is suspected, for the accelerated elimination of teriflunomide, the patient is advised to prescribe colestyramine at a dose of 8 g 3 times a day for 11 days (if tolerance is poor, it can be reduced to 4 g 3 times a day) or activated carbon at a dose of 50 g 2 times a day.

special instructions

Abagio should be treated by a physician experienced in the treatment of multiple sclerosis. When prescribing the drug, one should take into account such indicators as blood pressure, the degree of ALT activity, the results of a general blood test (including leukocyte count, the number of platelets in the blood). Control of these parameters must be regularly performed during the period of use of teriflunomide.

There is a risk of increased liver enzyme activity, especially during the first 6 months of treatment. Therefore, studies to determine the activity of the patient's liver enzymes must be carried out before starting therapy, then 2 times a month during the first 6 months of treatment, then - with an interval of 2 months. Liver dysfunction may be indicated by clinical symptoms such as abdominal pain, loss of appetite, nausea, vomiting, fatigue, dark urine, and / or jaundice. To continue treatment, a two to threefold increase in ALT in relation to the upper limit of the norm is permissible against the background of regular monitoring. Teriflunomide should be discontinued if liver damage is suspected, including a confirmed increase in liver enzyme activity by more than 3 times the upper limit of normal. Particular attention should be paid to patients with a history of liver disease, taking teriflunomide in this category of patients should be accompanied by careful monitoring of symptoms indicating liver damage.

With an increase in blood pressure, appropriate antihypertensive therapy is indicated.

In acute and chronic infections, treatment with the drug can be started only after a complete cure. If symptoms of infection appear while taking Abagio, you should immediately consult a doctor.

The safety of teriflunomide for latent TB infection has not been established. It is necessary to start taking Abaggio in patients with a positive test for tuberculosis at screening after a course of appropriate therapy.

The risk of developing interstitial lung disease is increased in those patients who have suffered from such diseases during treatment with leflunomide.

If persistent cough and dyspnea appear, discontinuation of therapy and a thorough examination should be considered.

It should be borne in mind that treatment with teriflunomide increases the risk of hematological diseases in patients with anemia, leukopenia, thrombocytopenia, impaired bone marrow function and / or the risk of suppression of bone marrow hematopoiesis. Therefore, when these adverse events appear during therapy, it is necessary to consider discontinuing the use of Abagio and prescribing a procedure for accelerated elimination of the drug to quickly reduce the plasma concentration of teriflunomide.

In the event of ulcerative stomatitis or symptoms indicating the development of a generalized skin reaction (Stevens-Johnson syndrome, Lyell's syndrome), the use of teriflunomide should be discontinued, and the procedure for its accelerated elimination should be started immediately.

Confirmed peripheral neuropathy is the basis for considering discontinuing Abagio and conducting an accelerated elimination procedure.

The use of live attenuated vaccines should be avoided due to the increased risk of infection. The administration of seasonal influenza vaccines during the treatment period produces an immune response that corresponds to the normal response to booster vaccination, the antibody titer is sufficient for seroprotection. The efficacy and safety of primary vaccination against neopathogens has not been established.

Combined use of teriflunomide with leflunomide is not recommended.

The results of a study of the simultaneous use of teriflunomide with glatiramer acetate or with interferon beta for 12 months indicate no problems with the safety of such combinations, but there is a higher frequency of side effects than with monotherapy with teriflunomide. Longer studies have not been conducted on the safety of this combination for the treatment of multiple sclerosis.

Clinical data relating to the co-administration of teriflunomide with glatiramer acetate or interferon beta show that there is no need for a waiting period when starting drug therapy after glatiramer acetate or interferon beta, or, conversely, when starting therapy with glatiramer acetate or interferon beta after treatment with Abagio.

Precautions should be taken when switching from natalizumab therapy to teriflunomide. It is necessary to take into account the half-life of natalizumab and not start Abagio therapy for two to three months, since an increased effect on the patient's immune system is possible.

Care must be taken when switching from fingolimod therapy to avoid combined effects on the immune system. It should be borne in mind that for the elimination of circulating fingolimod from the body, 1.5 months are required without therapy, for the return to the normal number of lymphocytes - from 1 to 2 months.

Against the background of the use of Abagio, the likelihood of embryofetal toxicity from men is considered low.

Influence on the ability to drive vehicles and complex mechanisms

During the period of use of Abagio, patients whose activities are associated with driving vehicles and other potentially hazardous types of work should take into account the possibility of adverse reactions from the nervous system in the form of dizziness.

Application during pregnancy and lactation

The use of Abadzhio is contraindicated during gestation and breastfeeding.

Teriflunomide has reproductive toxicity, therefore, the use of Abaggio should be started only after excluding pregnancy.

Women of childbearing age should use effective contraception throughout the treatment period. They should be informed about the possible risks to the fetus in case of conception during the treatment period. If your period is delayed while taking teriflunomide, you should immediately consult a doctor.

After discontinuation of therapy, conception can be planned only when the plasma concentration of teriflunomide reaches 0.02 mg / l or less. Usually, after the abolition of Abaggio, this requires at least 8 months, but given the individual deviations in drug clearance, it may be necessary to control the plasma concentrations of teriflunomide for two years.

For a more rapid decrease in the plasma concentration of teriflunomide, women can be recommended the procedure for the accelerated elimination of Abagio, which consists in taking cholestyramine at a dose of 8 g (with poor tolerance - 4 g) 3 times a day for 11 days. Alternatively, it is possible to prescribe activated carbon in a dose of 50 g 2 times a day.

When prescribing the drug during lactation, the decision to stop breastfeeding should be made taking into account the degree of need for the drug for the mother.

Impact of Abagio on male and female fertility is unlikely.

Pediatric use

The safety and efficacy of using Abagio in children and adolescents has not been established, therefore, the appointment of the drug under the age of 18 is contraindicated.

With impaired renal function

The use of Abagio is contraindicated for the treatment of patients with severe renal failure, which requires the use of hemodialysis.

In mild, moderate or severe (without hemodialysis) renal failure, dose adjustment is not required.

For violations of liver function

The use of Abagio is contraindicated for the treatment of patients with severe hepatic impairment (class C on the Child-Pugh scale).

For mild to moderate hepatic impairment, dose adjustment is not required.

Use in the elderly

With caution, it is necessary to prescribe Abagio tablets to patients aged 65 years and older due to limited information on the safety and efficacy of the drug for this category of patients.

Drug interactions

• rifampicin, phenobarbital, carbamazepine, phenytoin, St. John's wort and other inducers of cytochrome P ₄₅₀ and carrier proteins: should be prescribed with caution due to the fact that their intake causes a clinically significant decrease in the effect of teriflunomide;
• cholestyramine, activated carbon: contribute to a rapid and significant decrease in the plasma concentration of teriflunomide;
• repaglinide, pioglitazone, paclitaxel, rosiglitazone: drugs metabolized by the CYP2C8 isoenzyme are recommended to be prescribed with caution (since teriflunomide acts as an inhibitor of the CYP2C8 isoenzyme in vivo);
• contraceptives for oral administration: ethinyl estradiol and levonorgestrel in combination with teriflunomide increase the average C _max, this does not adversely affect their effectiveness. When choosing oral contraceptives, their interaction with teriflunomide should be considered;
• caffeine, duloxetine, alosetron, tizanidine, theophylline: these and other drugs metabolized by the CYP1A2 isoenzyme may decrease their effectiveness;
• Warfarin: The pharmacokinetics of S-warfarin are not impaired, but there is a 25% decrease in the peak international normalized ratio (MHO) compared to warfarin monotherapy. MHO should be closely monitored;
• cefaclor, benzylpenicillin, indomethacin, ciprofloxacin, furosemide, cimetidine, ketoprofen, methotrexate, zidovudine [organic anion carrier 3 (POA3) transporter substrates]: caution is advised as teriflunomide is a POA3 inhibitor;
• rosuvastatin: there is a significant increase in the values of C _max and AUC of rosuvastatin, so its dose should be reduced by 50% if necessary in combination with teriflunomide;
• methotrexate, sulfasalazine, daunorubicin, topotecan, doxorubicin, simvastatin, atorvastatin, pravastatin, nateglinide, repaglinide, rifampicin: should be prescribed with caution, accompanying treatment with careful monitoring of signs and symptoms of their increased effects on the body. If necessary, a decrease in the dose of these funds is indicated.

Analogs

The analogues of Abagio are: Femorix, Leflunomid, Elafra, Ralef, Arava, Leflunomid Canon, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at 2-30 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Abagio

Reviews about Abagio are mostly positive. Patients report that while taking the drug for 14 months, no relapses were observed.

Price for Abagio in pharmacies

The price of Abagio for a pack containing 28 tablets can range from 51,748 rubles.

Abagio: prices in online pharmacies

Drug name Price Pharmacy

Abagio 14 mg film-coated tablets 28 pcs. RUB 53,500 Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!