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Drugs reference index «Ustekinumab»

Ustekinumab


Ustekinumab

Pronunciation: US-te-KIN-ue-mabClass: Immunomodulator

Trade Names:Stelara- Injection, solution 45 mg per 0.5 mL- Injection, solution 90 mg/mL

Pharmacology

Human immunoglobulin G1 (IgG1) kappa monoclonal antibody that binds with high affinity and specificity to the p40 protein subunit used by both the interleukin (IL)–12 and IL-23 cytokines.

Pharmacokinetics

Absorption

T max was 13.5 days and 7 days after a single subcutaneous administration of 45 mg and 90 mg, respectively.

Distribution

The mean Vd during the terminal phase following a single IV administration ranged from 56.1 to 82.1 mL/kg. Following subcutaneous administration of 45 mg and 90 mg, it was 161 mL/kg and 179 mL/kg, respectively.

Metabolism

Expected to be degraded via catabolic pathways in the same manner as endogenous IgG.

Elimination

The mean systemic Cl following a single IV administration ranged from 1.9 to 2.22 mL/day/kg. The mean half-life ranged from 14.9 to 45.6 days following IV and subcutaneous administration.

Special Populations

Renal Function Impairment

No pharmacokinetic data are available in patients with renal impairment.

Hepatic Function Impairment

No pharmacokinetic data are available in patients with hepatic impairment.

Elderly

There were no apparent changes in pharmacokinetic parameters (Cl and Vd) in subjects older than 65 years of age.

Weight

When given the same dose, subjects weighing more than 100 kg had lower median serum concentrations compared with those subjects weighing 100 kg or less.

Indications and Usage

For the treatment of adults (18 years of age and older) with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.

Contraindications

Standard considerations.

Dosage and Administration

Adults

Weighing 100 kg (220 lb) or less

Subcutaneously 45 mg initially and 4 weeks later, followed by 45 mg every 12 weeks.

Weighing more than 100 kg (220 lb)

Subcutaneously 90 mg initially and 4 weeks later, followed by 90 mg every 12 weeks. 45 mg was also shown to be efficacious; however, 90 mg resulted in greater efficacy in these subjects.

General Advice

  • Administer by subcutaneous injection.
  • Administer each injection at a different anatomic location (such as upper arms, gluteal regions, thighs, or any quadrant of abdomen) than the previous injection, and not into areas where the skin is tender, bruised, erythematous, or indurated.
  • Prior to administration, visually inspect for particulate matter and discoloration. Do not use if discolored or cloudy. The solution is normally colorless to light yellow and may contain a few small translucent or white particles.
  • The injection solution does not contain a preservative; discard any unused portion.

Storage/Stability

Store refrigerated at 36° to 46°F. Do not freeze or shake. Keep in original carton to protect from light until time of use.

Drug Interactions

Bacillus Calmette-Guérin (BCG) vaccine

It is not known whether patients receiving ustekinumab will be vulnerable to dissemination of infection. Do not administer BCG vaccines to patients receiving ustekinumab or for 1 yr prior to initiation or 1 yr following discontinuation of treatment.

CYP substrates

The role for ustekinumab in regulation of CYP-450 isozymes has not been determined. Upon initiating ustekinumab therapy in patients receiving CYP-450 substrates, particularly drugs with a narrow therapeutic index, monitor clinical effects (eg, warfarin) or drug concentrations (eg, cyclosporine) and adjust the dose of the drug as needed.

Immunosuppressive agents, phototherapy

The safety of coadministration of ustekinumab with immunosuppressive agents or phototherapy has not been evaluated.

Live vaccines

It is not known whether patients receiving ustekinumab will be vulnerable to dissemination of infection. Do not administer live vaccines to patients receiving ustekinumab. Use with caution in administering live vaccines to household contacts of patients receiving ustekinumab because of risk for viral shedding from the household contact and transmission to the patient.

Nonlive vaccinations

The immune response to the vaccination may not be sufficient to prevent the disease.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (5%); fatigue (3%); dizziness (2%); depression (1%).

Dermatologic

Pruritus (2%).

EENT

Nasopharyngitis (8%); pharyngolaryngeal pain (2%).

GI

Diarrhea (2%).

Local

Injection-site erythema (2%).

Musculoskeletal

Back pain (2%); myalgia (1%).

Respiratory

Upper respiratory tract infection (5%).

Miscellaneous

Infections (27%).

Precautions

Monitor

Closely monitor for development of signs or symptoms of infection during and after treatment.

Pregnancy

Category B .

Lactation

IgG is excreted in human milk, so it is expected that ustekinumab will be present in human milk.

Children

Safety and efficacy not established.

Immunizations

Psoriatic patients should receive all age-appropriate immunizations prior to the start of treatment.

Infections

May increase the risk of infections and reactivation of latent infections. Serious bacterial, fungal, and viral infections were observed in patients receiving ustekinumab. Ustekinumab should not be given to patients with any clinically important active infection. Individuals genetically deficient in IL-12/IL-23 are particularly vulnerable to disseminated infections from mycobacteria (including nontuberculous, environmental mycobacteria), salmonella (including nontyphi strains), and BCG vaccinations.

Malignancies

Because many immunosuppressants have the potential to increase the risk of malignancies, use with caution in patients at high risk for malignancy or history of malignancy.

Reversible posterior leukoencephalopathy syndrome

May occur during treatment. If suspected, discontinue ustekinumab and administer appropriate treatment.

Tuberculosis

Evaluate patients for tuberculosis infection prior to initiating treatment; do not administer to patients with active tuberculosis.

Overdosage

Symptoms

No data available.

Patient Information

  • Instruct patients to notify their health care provider if they develop any symptoms of infection.
  • Counsel patients about the risk of malignancies while receiving ustekinumab.

Copyright © 2009 Wolters Kluwer Health.

  • Ustekinumab MedFacts Consumer Leaflet (Wolters Kluwer)
  • ustekinumab Subcutaneous Advanced Consumer (Micromedex) - Includes Dosage Information
  • Stelara Prescribing Information (FDA)
  • Stelara Consumer Overview

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