Actemra

Introduction
Actemra is a medicine used to treat various inflammatory conditions of the joints (rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis), skin (psoriasis), and bowel (ulcerative colitis, Crohn’s disease). It reduces swelling in these conditions by blocking TNF alpha. Actemra is given by a healthcare professional and should not be self-administered. You should use it regularly and at the same time each day to get the maximum benefit from it. Continue using it as recommended by your doctor and complete the dose even if you feel better. The most common side effects seen with this medicine include headache, high blood pressure, upper respiratory tract infection, increased liver enzymes, and nasopharyngitis (pain or irritation in the throat). Consult your doctor if any of the side effects persist or bother you. Your doctor may be able to help with ways to reduce or prevent these symptoms. You may also be more prone to infections when you are being treated with this medicine. Tell your doctor right away if you develop any symptoms of an infection like fever, cough, rash, loose stools, or flu-like symptoms. To make sure the medicine is safe for you, before taking it, let your doctor know if you have any problems with your heart, kidneys, or liver. You should also tell your doctor about all the other medicines you are taking. While on treatment with this medicine, your doctor may monitor your blood counts by taking regular blood tests to make sure the medicine is not affecting your blood counts. It is important for pregnant and breastfeeding women to ask the advice of their doctors before taking this medicine.

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Uses of Actemra
Ankylosing spondylitis
Rheumatoid arthritis
Psoriasis
Ulcerative Colitis
Crohn’s disease
Side effects of Actemra
Common
Headache
High blood pressure
Upper respiratory tract infection
Increased liver enzymes
Nasopharyngitis (inflammation of the throat and nasal passages)
How to use Actemra
Your doctor or nurse will give you this medicine. Kindly do not self administer.
How Actemra works
Actemra blocks the action of certain chemical messengers that are responsible for inflammation, swelling and redness associated with certain joint diseases.
What if you forget to take Actemra?
If you miss a dose of Actemra, please consult your doctor.
Quick Tips
ACTEMRA 400 MG INJECTION is given as a drip (intravenous infusion) or as an injection directly into a vein.
You may be asked for regular blood tests to check blood counts, cholesterol level and liver functioning during the treatment.
It might make you feel dizzy. If this happens, avoid driving or operating on machinery.
It makes it hard to fight with an infection. Inform your doctor if you notice fever, cough or stomach pain.
Inform your doctor if you are pregnant, planning to become pregnant or are breastfeeding.
Do not stop taking medicine without talking to your doctor first.
Brief Description
Indication
Juvenile idiopathic arthritis, Rheumatoid Arthritis (RA)
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 _ Adult Dose Parenteral Adult: 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 Hepatic impairment Not recommended with active hepatic disease or hepatic impairment

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Child Dose
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 (>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 (>30 kg or more): 8 mg/kg IV q4weeks May be administered as monotherapy or with methotrexate

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Renal Dose
Renal impairment Mild: No dosage adjustment required Moderate-to-severe: Has not been studied

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Contraindication
Hypersensitivity
Mode 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
Precaution
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 Lactation: unknown whether distributed in breast milk, do not breast feed

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Side Effect
>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 _ Interaction Interactions with Other Medications and Other Forms of Interaction: Population pharmacokinetic analyses did not detect any effect of MTX, nonsteroidal anti-inflammatory drugs or corticosteroids on tocilizumab clearance. Tocilizumab has not been studied in combination with other biological DMARDs. The expression of hepatic CYP450 enzymes is suppressed by cytokines, eg, IL-6, that stimulate chronic inflammation. Thus, CYP450 expression may be reversed when potent cytokine inhibitory therapy, eg, tocilizumab is introduced. In vitro studies with cultured human hepatocytes demonstrated that IL-6 caused a reduction in CYP1A2, CYP2C9, CYP2C19, and CYP3A4 enzyme expression. Tocilizumab normalizes expression of these enzymes. The effect of tocilizumab on CYP enzymes (except CYP2C19 and CYP2D6) is clinically relevant for CYP450 substrates with a narrow therapeutic index, and/or where the dose is individually adjusted. In a study in RA patients, levels of simvastatin (CYP3A4) were decreased by 57% one week following a single dose of tocilizumab, to the level similar or slightly higher than those observed in healthy subjects. When starting or stopping therapy with tocilizumab, patients taking medications, which are individually dose-adjusted and are metabolised via CYP450 3A4, 1A2, or 2C9 (eg, atorvastatin, calcium channel blockers, theophylline, warfarin, phenytoin, ciclosporin, or benzodiazepines) should be monitored as doses of these products may need to be adjusted to maintain their therapeutic effect. Given its long elimination t½, the effect of tocilizumab on CYP450 enzyme activity may persist for several weeks after stopping therapy. _