tocilizumab (Rx)

Brand and Other Names:Actemra
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injection for IV infusion

  • 20mg/mL in 4, 10, and 20mL vials

single-use prefilled syringe for SC injection

  • 162mg/0.9mL
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Rheumatoid Arthritis

Indicated for adults with moderate-to-severe active rheumatoid arthritis with inadequate response to 1 or more DMARDs as an IV infusion or SC injection

May use alone or in combination with methotrexate or other DMARDs

IV infusion

  • 4 mg/kg IV q4wk initially; may increase to 8 mg/kg q4wk based on clinical response 
  • Not to exceed 800 mg/dose q4wk

SC injection

  • Weight <100 kg: 162 mg SC every other week, followed by an increase to every week based on clinical response
  • Weight ≥100 kg: 162 mg SC every week

Systemic Sclerosis (Orphan)

Orphan designation for treatment of systemic sclerosis

Orphan sponsor

  • Genentech, Inc.; 1 DNA Way; South San Francisco, CA 94080-4990

Dosage Modifications

Renal impairment

  • Mild: No dosage adjustment required
  • Moderate-to-severe: Has not been studied

Hepatic impairment

  • Not recommended with active hepatic disease or hepatic impairment

Do not initiate if

  • ANC <2000/mm³
  • Platelets <100,000/mm³
  • ALT/AST >1.5 times ULN

Transaminase elevations

  • >1 to 3 x ULN: Modify dose of other DMARDs if possible; for persistent increases and receiving IV infusion, reduce dose to 4 mg/kg or discontinue therapy and restart when ALT/AST return to normal; for persistent increases and receiving SC injection, reduce injection frequency to every other week or hold dosing until ALT/AST return to normal, resume at every other week and increase frequency to every week as clinically appropriate
  • >3 to 5x ULN: Discontinue therapy and restart when <3 x ULN and follow above recommendations
  • >5 x ULN: Discontinue therapy

Neutropenia

  • ANC >1000/mm³: Maintain dose
  • ANC 500-1000/mm³: Discontinue therapy until >1000/mm³, for patients receiving IV infusion, restart therapy at 4 mg/kg and increase to 8 mg/kg if clinically warranted; for patients receiving SC injection, restart at 162 mg every other week and increase frequency to every week as clinically appropriate
  • ANC <500/mm³: Discontinue therapy

Thrombocytopenia

  • 50,000-10,0000/mm³: Discontinue therapy until >100,000/mm³ for patients receiving IV infusion, restart therapy at 4 mg/kg and increase to 8 mg/kg if clinically warranted; for patients receiving SC injection, restart at 162 mg every other week and increase frequency to every week as clinically appropriate
  • <50,000/mm³: Discontinue therapy

Dosing Considerations

Monitor neutrophils, platelets, ALT, and AST every 4-8 weeks

Monitor lipids 4-8 weeks following initiation of therapy and then at ~24 week intervals

Use not recommended if

  • ANC <500/mm³
  • Platelets <50,000/mm³
  • ALT or AST >5x ULN

Dosage Forms & Strengths

injection for IV infusion

  • 20mg/mL in 4, 10, and 20mL vials
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Systemic Juvenile Idiopathic Arthritis (SJIA, Still's Disease)

<2 years: Safety and efficacy not established

≥2 years or older (<30 kg): 12 mg/kg IV q2weeks 

≥2 years or older (≥30 kg): 8 mg/kg IV q2weeks

May be administered as monotherapy or with methotrexate

Polyarticular Juvenile Idiopathic Arthritis (PJIA)

<2 years: Safety and efficacy not established

≥2 years or older (<30 kg): 10 mg/kg IV q4weeks 

≥2 years or older (≥30 kg or more): 8 mg/kg IV q4weeks

May be administered as monotherapy or with methotrexate

Dosage Modifications

Dose reduction has not been studied in the PJIA and SJIA populations

Dose interruptions are recommended for liver enzyme abnormalities, low neutrophil counts, and low platelet counts in patients with PJIA and SJIA at levels similar to what is outlined for adults with RA

Dosing Considerations

Monitor neutrophils, platelets, ALT and AST at the time of the second infusion and thereafter every 4-8 weeks for PJIA and every 2-4 weeks for SJIA

Monitor lipids 4-8 weeks following initiation of therapy and then at ~24 week intervals

Increased risk of serious infections in patient ≥65 years of age; caution should be used when treating the elderly

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Interactions

Interaction Checker

and tocilizumab

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            SC injection site reactions (7.1-10.1%)

            1-10%

            Upper respiratory tract infections

            Nasopharyngitis

            Headache

            Hypertension

            Increased ALT

            Infusion related skin reactions (eg, rash, pruritus, urticaria)

            Dose related adverse reactions including decreased neutrophil count <1000/cu.mm, decreased platelets <100,000/cu.mm

            Lipid elevations

            Mouth ulcerations

            Gastritis

            Upper abdominal pain

            Postmarketing reports

            Stevens-Johnson Syndrome

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            Warnings

            Black Box Warnings

            Serious infections leading to hospitalization or death (ie, tuberculosis; bacterial, invasive fungal, viral, or other opportunistic infections) have occurred with use

            Stop therapy if serious infection occurs; can restart if infection is controlled

            Test for latent tuberculosis before initiating; if positive, initiate tuberculosis therapy before starting tocilizumab

            Continue to monitor all patients for active tuberculosis during therapy

            Contraindications

            Hypersensitivity

            Cautions

            Risk for serious infections (see Black Box Warnings)

            If a serious infection develops, interrupt therapy until infection controlled

            Tocilizumab has not been studied in combination with biological DMARDs (eg, TNF antagonists, IL-1R antagonists, anti-CD20 monoclonal antibodies, selective costimulation modulators) and its use should be avoided in combination with these agents because of increased immunosuppression and risk of infection

            Nonmelanoma skin cancers reported; periodic skin examination recommended

            Caution if increased risk for GI perforation

            May cause neutropenia, decreased platelets, elevated liver transaminases, and increased lipid parameters; monitor neutrophils, platelets, lipids, and liver function tests every 4-8 weeks

            Anaphylaxis or serious hypersensitivity reactions have occurred, including fatalities, with or without concomitant arthritis therapies

            Do not coadminister with live vaccines (eg, MMR, intranasal influenza); IL-6 inhibition may interfere with the normal immune response to new antigens, all patients, particularly those with PJIA and SJIA, should be current with their immunizations before initiating therapy

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            Pregnancy & Lactation

            Pregnancy: Pregnancy exposure registry that monitors pregnancy outcomes in women exposed to during pregnancy; physicians are encouraged to register patients and pregnant women are encouraged to register themselves by calling 1-877-311-8972; the limited available data in pregnant women are not sufficient to determine whether there is a drug-associated risk for major birth defects and miscarriage; monoclonal antibodies are increasingly transported across placenta as pregnancy progresses, with largest amount transferred during third trimester; risks and benefits should be considered prior to administering live or live-attenuated vaccines to infants exposed to therapy in utero

            Lactation: No information is available on presence of tocilizumab in human milk, the effects of drug on breastfed infant, or effects of drug on milk production; maternal immunoglobulin G (IgG) is present in human milk; if tocilizumab is transferred into human milk, effects of local exposure in gastrointestinal tract and potential limited systemic exposure in infant to tocilizumab are unknown; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and potential adverse effects on breastfed child from tocilizumab or from underlying maternal condition

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Interleukin-6 receptor antagonist; changes in clinical trials observed include decreased C-reactive protein level to within normal range, decreased values in other pharmacodynamic parameters (eg, rheumatoid factor, erythrocyte sedimentation rate, amyloid A), and increased hemoglobin value

            Absorption

            Peak plasma time: 1 hr

            Distribution

            Vd: 6.4L

            Elimination

            Half-life: up to 11 days (4 mg/kg); up to 13 days (8 mg/kg)

            Cmax: 88.3 mcg/mL (4 mg/kg); 183 mcg/mL (8 mg/kg)

            Clearance: 0.0125 L/hr

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            Administration

            IV Preparation

            Withdraw a volume of 0.9% NaCl from bag/bottle equal to volume of the solution required for the patient's dose

            Adults and children weighing ≥30 kg: Dilute to 100 mL in 0.9% NaCl

            Children <30 kg: Dilute to 50 mL in 0.9% NaCl

            Slowly add dose to infusion bag or bottle and gently invert to mix (prevent foaming)

            IV Administration

            Administer as single IV infusion over 1 hr

            Do NOT administer as bolus or push

            Do not infuse with any other drugs as no compatibility studies have been conducted

            SC Preparation

            Remove prefilled SC syringe from refrigerator 30 minutes before administration

            SC Administration

            Indicated only in adults with rheumatoid arthritis

            Rotate SC injection sites (ie, thighs, abdomen, outer area of upper arm [caregiver only]) and inject full amount of the syringe (0.9 mL)

            Transition from IV to SC: Administer first SC dose instead of next scheduled IV dose

            Storage

            Undiluted vials and prefilled SC syringes: Store refrigerated between 2-8°C (36-46°F) in original container and protect from light

            After dilution for IV administration: Store refrigerated between 2-8°C (36-46°F) or room temperature for up to 24 hr; protect from light

            Do not freeze

            Do not save unused, reconstituted drug in vials because product contains no preservatives

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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