Ustekinumab - instructions for use, reviews, analogs and forms of release (injections in ampoules for injections in solution) drugs for the treatment of psoriasis and psoriatic arthritis in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Ustekinumab. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of experts on the use of Ustekinumab in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Ustekinumab Analogues in the presence of existing structural analogs. Use for the treatment of psoriasis and psoriatic arthritis in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Ustekinumab - an interleukin inhibitor, a fully human monoclonal antibody of the class of immunoglobulins G. Ustekinumab has a high affinity and specificity for the p40 subunit of IL-12 and IL-23 human interleukins (IL).

IL-12 and IL-23 are heterodimeric cytokines. Ustekinumab blocks the effects of IL-12 and IL-23 on the activation of immune cells, in particular, the intracellular signaling and secretion of cytokines caused by these cytokines. Thus, it is believed that the drug interrupts the cascade of signal transduction and cytokine secretion, which play a key role in the development of psoriasis.

Ustekinumab leads to a significant weakening of histological manifestations of psoriasis, including hyperplasia and proliferation of epidermal cells. These data are consistent with clinical efficacy. It has no significant effect on the ratio of circulating immune cells in the blood, including memory cells and non-activated T cells, as well as the concentration of cytokines in the blood.

Analysis of the matrix ribonucleic acid (mRNA), isolated from biopsy samples of skin lesions of psoriasis initially and after 2 weeks of treatment,that the use of ustekinumab led to a decrease in the expression of genes encoding its molecular targets-IL-12 and IL-23, as well as genes encoding inflammatory cytokines and chemokines. These data are consistent with the significant clinical effect of treatment.

The clinical effect, namely the improvement of index prevalence and severity of psoriasis (PASI), apparently depends ustekinumab concentration in blood plasma. In patients with the best result in PASI average value of ustekinumab concentration in blood plasma was higher than in patients with less clinical effect. In general, the proportion of patients with improvement in PASI scale reached 75%, increased with increasing ustekinumab concentration in blood plasma.

In patients with psoriatic arthritis who achieved an ACR score of 20 (according to the criteria for improvement of the American College of Rheumatology (ACR), it means an improvement of at least 20%), there is a higher average concentration of ustekinumab in plasma compared to patients who did not respond to treatment. The number of patients with psoriatic arthritis, reached improvement on a scale ACR 20 and ACR 50, increased with increasing ustekinumab concentration in blood plasma.

Composition

Ustekinumab + auxiliary substances.

Pharmacokinetics

After a single subcutaneous administration at a dose of 90 mg in healthy volunteers the mean time of maximum accumulation in the plasma was 8.5 hours. In patients with psoriasis, this quantity of the drug at doses of 45 mg or 90 mg was comparable with that in healthy volunteers. Cumulation in serum was not observed during treatment for a duration of 12 weeks. The metabolic path of ustekinumab is not known. The concentration in the blood plasma depends on the patient's body weight. When administered in similar doses (45 mg or 90 mg) in patients weighing more than 100 kg ustekinumab mean concentration in the plasma was less than in patients weighing less than 100 kg. However, the average minimum concentration ustekinumab in blood plasma of patients body weight over 100 kg at a dose of 90 mg, was comparable to that in patients weighing less than 100 kg at a dose of 45 mg.

Indications

• plaque psoriasis moderate or severe in the ineffectiveness or contraindications or intolerance other systemic therapy, including cyclosporin, methotrexate or psoralen with ultraviolet irradiation;
• active psoriatic arthritis - as a monotherapy or in combination withmethotrexate with insufficient response to previous therapy with non-biological disease-modifying antirheumatic drugs.

Forms of release

A solution for subcutaneous administration of 45 mg in 0.5 ml and 90 mg in 1 ml (injections in ampoules for injection).

Instructions for use and dosing regimen

Ustekinumab is administered subcutaneously.

The recommended dose is 45 mg. The second injection is done 4 weeks after the first application, then every 12 weeks.

For patients with a body weight of more than 100 kg, the recommended dose is 90 mg.

If the therapy is ineffective for 28 weeks, it is recommended to consider the advisability of using Ustekinumab.

If the clinical effect is not sufficiently pronounced, a dose adjustment according to a special scheme should be performed.

Side effect

• upper respiratory tract infections, including viral infections;
• inflammation of subcutaneous fat;
• diverticulitis (inflammatory bowel disease);
• osteomyelitis (a purulent-necrotic process that develops in the bone and bone marrow, as well as in surrounding soft tissues);
• gastroenteritis (inflammatory process in the stomach and small intestine);
• pneumonia (inflammation of the lung tissue);
• urinary tract infections;
• dizziness, headache;
• depression, fatigue;
• pain in the throat and larynx;
• nasal congestion;
• diarrhea;
• itching;
• Myalgia (pain in the muscle);
• backache;
• rashes and hives;
• malignant neoplasms;
• reaction at the injection site (pain, swelling, itching, tightness, bleeding, hemorrhage, irritation).

Contraindications

• severe infectious diseases in the acute phase, including tuberculosis;
• malignant neoplasms;
• pregnancy;
• lactation period (breastfeeding);
• children and adolescents under 18;
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

Contraindicated use Ustekinumaba during pregnancy and lactation (breastfeeding).

Women of childbearing age should use effective methods of contraception during treatment with the drug and 15 weeks after it.

Use in children

Contraindicated for children and adolescents under 18 years.

Application in elderly patients

Caution should be used in elderly patients.

special instructions

Caution should be used in patients with chronic or recurrent parasitic and infectious diseases of a viral, fungal or bacterial nature; malignant tumors in the anamnesis; in elderly patients.

Do not use in patients with clinically relevant, active infections. With caution should be used in patients with chronic infections or the presence of recurrent infections in the anamnesis. Ustekinumab is a selective immunosuppressant and may increase the risk of infections and the reactivation of infections in the latent phase.

Before starting the test, the patient should be tested for tuberculosis. In the presence of latent or active tuberculosis, including in the history, it is necessary to begin its treatment before the application of utekinumab. Also, it is necessary to begin treatment of tuberculosis in patients who have not had sufficient effect from the previous treatment. During the treatment with usekinumab and after this, patients should be closely monitored to identify signs and symptoms of active tuberculosis.

With the development of anaphylactic and other serious allergic reactions, the use of ustekinumab should be stopped immediately and appropriate treatment prescribed.

Ustekinumab is a selective immunosuppressant. Immunosuppressants can increase the risk of developing malignant tumors. In some patients who received ustekinumab in clinical studies, malignant neoplasms (cutaneous and non-dermal forms) were observed. The use of ustekinumab has not been studied in patients with malignant tumors in the anamnesis. Caution should be exercised when using ustekinumab in patients with malignant tumors in an anamnesis, as well as when deciding whether to continue treatment with ustekinumab in patients with diagnosed malignant neoplasms.

In all patients over the age of 60 years, as well as in patients who received long-term therapy with immunosuppressants or ultraviolet radiation, it is necessary to conduct a test for the presence of non-melanoma skin cancer.

During the period of treatment it is not recommended to use vaccines,containing weakened pathogens of infectious (viral or bacterial) diseases, as well as 15 weeks before the vaccination (after the last dose of ustekinumab) and 2 weeks after vaccination. Together with ustekinumab, vaccines containing inactivated microorganisms can be used.

The safety and efficacy of ustekinumab in combination with immunosuppressive drugs and phototherapy has not been studied. Caution should be exercised when considering the possibility of simultaneous use of other immunosuppressants and utekinumab, as well as during the transition from therapy with another antipsoriasis biological agent to ustekinumab therapy.

Impact on the ability to drive vehicles and manage mechanisms

Studies of the influence of Ustekinumab on the ability to drive vehicles and other potentially hazardous activities were not conducted.

Drug Interactions

Special studies of the drug interaction of Ustekinumab were not conducted.

Do not use vaccines containing weakened pathogens of infectious diseases, concomitantly with ustekinumab.

With the joint use of the drug Ustekinumab and such drugs as Paracetamol (acetaminophen), ibuprofen, acetylsalicylic acid, metformin, atorvastatin, naproxen, levothyroxine and hydrochlorothiazide interaction was not detected.

The safety and efficacy of the joint use of the drug with other immunosuppressants (methotrexate, cyclosporine) or biological agents for the treatment of psoriasis have not been studied.

Analogues of the drug Ustekinumab

Structural analogs for the active substance:

• Stelara.

Analogues of the drug Ustekinumab on the pharmacological group (immunosuppressants):

• Abaggio;
• Azathioprine;
• Actemra;
• Antiliphosphine;
• Arava;
• Arresto;
• Atgam;
• Benlist;
• Gilenia;
• The festival;
• Grafalon;
• Delagil;
• Zenapax;
• Ilaris;
• Imuran;
• Consuprene;
• Xolar;
• Kuprenil;
• Leflunomide;
• MabThera;
• Misept;
• Mayforth;
• The methodical;
• Mycophenolate;
• Necklair;
• Nulogix;
• Orgosporin;
• Orensia;
• Othello;
• Pantograph;
• Plaquenil;
• Raleph;
• Raptiva;
• Redditus;
• Rituximab;
• Sandimmun;
• Sertikan;
• Simponi;
• Simulect;
• Soliris;
• Stelara;
• Suprema;
• Tacrolimus;
• Tacrose;
• Tauredon;
• Teriflunomide;
• Tizabry;
• Timoglobulin;
• Timodepressin;
• Femoriks;
• Fingolimod-native;
• Flammages;
• Humirah;
• Cyclosporin;
• Ecological;
• Elafra;
• Enbrel;
• Antivio;
• Yaqurinus.

Response of a therapist

In my practice, there have been patients suffering from psoriasis. Not all, but some of them are prescribed the drug Ustekinumab. Against the backdrop of treatment, the skin symptoms of psoriasis subsided in them, the symptoms of joint inflammation associated with this disease go away. But the side effects of Ustekinumab therapy are observed in almost all cases. Most often it is fatigue, dizziness, pain in the muscles. But there were cases of gastroenteritis, urticaria, urinary tract infection. Often there are reactions to the injection of the drug at the injection site, manifested by redness, swelling and soreness.

Similar medicines:

Other medicines: