Disease modifying agents  (Anti-rheumatic agents)

adalimumab (Humira ®): anakinra (Kineret ®)
auranofin (Ridaura ®) azathioprine (Imuran ®)
etanercept (Enbrel ® ) hydroxychloroquine (Plaquenil ®)
infliximab (Remicade ® ) leflunomide (Arava ®)
methotrexate (Rheumatrex ®) sulfasalazine (Azulfidine ®)

adalimumab  (Humira ®):  top of page icon

A recombinant, anti-tumor necrosis factor (TNF)-alpha monoclonal antibody.

Dosing: rheumatoid arthritis: 40 mg SQ every other week. The drug can be given concomitantly with methotrexate. Whether adalimumab will offer a significant advantage over infliximab or etanercept remains to be determined.

SUPPLIED:
Injection, solution [preservative free]: 40 mg/0.8 mL (1 mL) [prefilled glass syringe; packaged with alcohol preps]

anakinra  (Kineret ®)  top of page icon

A recombinant, nonglycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra).

Dosing (Adults):
Rheumatoid arthritis: 100 mg/day SQ daily. Higher doses did not result in a higher response. The dose should be administered at approximately the same time every day.

SUPPLIED:
Injection, solution [preservative free]: 100 mg/0.67 mL (1 mL) [prefilled syringe]

auranofin  (Ridaura ®)  top of page icon

Oral gold compound.

Dosing (Adults):
Normal dose (rheumatoid arthritis):
Adults: 6 mg/day in 1-2 divided doses; after 3 months may be increased to 9 mg/day in 3 divided doses; if still no response after 3 months at 9 mg/day, discontinue drug

SUPPLIED:
Capsule: 3 mg [29% gold]

azathioprine  (Imuran ®)  top of page icon

An immunosuppressive agent.
Mechanism of Action
Azathioprine is an imidazolyl derivative of mercaptopurine; antagonizes purine metabolism and may inhibit synthesis of DNA, RNA, and proteins; may also interfere with cellular metabolism and inhibit mitosis

Dosing (Adults):
(Rheumatoid arthritis): Initial dose: 1 mg/kg (50-100mg) orally once daily or divided twice daily. In the absence of serious toxicity and if response is unsatisfactory, the dose can be increased, beginning at 6 to 8 weeks and thereafter at 4 week intervals, in increments of 0.5 milligrams/kilogram/day up to a maximum dose of 2.5 milligrams/kilogram/day. Patients who do not improve after 12 weeks of therapy can be considered refractory.

Dosing adjustment in renal impairment:
Clcr 10-50 mL/minute: Administer 75% of normal dose daily
Clcr<10 mL/minute: Administer 50% of normal dose daily

Hemodialysis: Slightly dialyzable (5% to 20%)
Administer dose post hemodialysis: CAPD effects: Unknown; CAVH effects: Unknown

SUPPLIED:
Injection, powder for reconstitution, as sodium: 100 mg
Tablet [scored]: 50 mg
Azasan®: 25 mg, 50 mg, 75 mg, 100 mg
Imuran®: 50 mg

etanercept  (Enbrel ® ) top of page icon

Tumor necrosis factor receptor fused to the Fc fragment of human immunoglobulin G1. Indicated for the reduction of signs and symptoms of moderate to severe, active rheumatoid arthritis in patients who have had an inadequate response to one or more disease-modifying antirheumatic drugs. Can be used in combination with methotrexate for those patients not responding to methotrexate monotherapy.

Dosing (Adults):
Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis:
Once-weekly dosing: 50 mg once weekly

Twice weekly dosing: 25 mg given twice weekly (individual doses should be separated by 72-96 hours)

Note: If the physician determines that it is appropriate, patients may self-inject after proper training in injection technique.

Administration
Administer subcutaneously. Rotate injection sites. New injections should be given at least one inch from an old site and never into areas where the skin is tender, bruised, red, or hard.
Powder for reconstitution: Follow package instructions carefully for reconstitution. Note: The needle cover of the diluent syringe (multidose vial) may contain dry natural rubber (latex) which should not be handled by persons sensitive to this substance. The maximum amount injected at any single site should not exceed 25 mg.

Prefilled syringe: May be allowed to reach room temperature prior to injection.

SUPPLIED:
Injection, powder for reconstitution: 25 mg [diluent contains benzyl alcohol; packaging may contain dry natural rubber (latex)]

Injection, solution: 50 mg/mL (0.98 mL) [prefilled syringe with 27-gauge 1 /2 inch needle]

hydroxychloroquine  (Plaquenil ®)  top of page icon

Antimalarial agent that possesses anti-inflammatory activity.

Dosing (Adults):
(Rheumatoid arthritis) Initial dose: 400 to 600 mg orally once daily with food or milk. qd--then taper dose (usually after 4 to 12 weeks) to 200-400mg orally once daily. If there is no improvement after 6 months, discontinue drug.

SUPPLIED:
Tablet, as sulfate: 200 mg

infliximab  (Remicade ® ) top of page icon

Dosing (Adults):
Rheumatoid Arthritis
. The recommended dose of Remicade is 3 mg/kg given as an intravenous infusion followed with additional similar doses at 2 and 6 weeks after the first infusion then every 8 weeks thereafter. Should be given in combination with methotrexate. For patients who have an incomplete response, consideration may be given to adjusting the dose up to 10 mg/kg or treating as often as every 4 weeks.

SUPPLIED:
Injection, powder for reconstitution [preservative free]: 100 mg

leflunomide  (Arava ®)  top of page icon

Immunomodulatory agent.
Mechanism of Action
Inhibits pyrimidine synthesis, resulting in antiproliferative and anti-inflammatory effects

Dosing (Adults):
(active rheumatoid arthritis):
Oral: Initial: 100 mg/day for 3 days, followed by 20 mg/day; dosage may be decreased to 10 mg/day in patients who have difficulty tolerating the 20 mg dose. Due to the long half-life of the active metabolite, plasma levels may require a prolonged period to decline after dosage reduction.

Elderly: Although hepatic function may decline with age, no specific dosage adjustment is recommended. Patients should be monitored closely for adverse effects which may require dosage adjustment.

Dosing adjustment in hepatic toxicity: Guidelines for dosage adjustment or discontinuation based on the severity and persistence of ALT elevation secondary to leflunomide have been developed. If ALT elevations >2 times but </= 3 times ULN are noted, reduce dose to 10 mg/day, and monitor closely. If elevations persist or if elevations >3 times ULN are observed, discontinue leflunomide and initiate protocol to accelerate elimination. Cholestyramine (8 g 3 times/day for 1-3 days) or activated charcoal (50 g every 6 hours for 24 hours) may be administered to decrease leflunomide concentrations rapidly. If elevations >3 times ULN persist additional cholestyramine and/or activated charcoal may be required.

SUPPLIED:
Tablet: 10 mg, 20 mg

methotrexate  (Rheumatrex ®)  top of page icon

Antineoplastic agent - can be used for immunosuppressive therapy in severe rheumatoid arthritis, psoriasis, and systemic lupus erythematosus.

Dosing (Adults):
Rheumatoid arthritis: Starting dose: 7.5 milligrams orally once a week. This dosage may be administered as a single dose or as a divided dose of 2.5 mg every 12 hours for 3 doses once a week. Once a response has been achieved, reduce the dosage if possible to the lowest effective dose. Maximum recommended dose: 20 mg/week. Consider folate supplementation.

SUPPLIED:
Injection, powder for reconstitution [preservative free]: 20 mg, 1 g
Injection, solution, as sodium: 25 mg/mL (2 mL, 10 mL)
Injection, solution, as sodium [preservative free]: 25 mg/mL (2 mL, 4 mL, 8 mL, 10 mL)
Tablet, as sodium: 2.5 mg
Rheumatrex®: 2.5 mg
Trexall™: 5 mg, 7.5 mg, 10 mg, 15 mg
Tablet, as sodium [dose pack] (Rheumatrex® Dose Pack): 2.5 mg (4 cards with 2, 3, 4, 5, or 6 tablets each)

sulfasalazine  (Azulfidine ®)  top of page icon

Indicated in the treatment of rheumatoid arthritis in patients who have responded inadequately to salicylates or other non-steroidal anti-inflammatory drugs.

Dosing (Adults):
Rheumatoid arthritis: Enteric coated tablet: Initial: 0.5-1 g/day; increase weekly to maintenance dose of 2 g/day in 2 divided doses; maximum: 3 g/day (if response to 2 g/day is inadequate after 12 weeks of treatment)

Dosing interval in renal impairment:
Clcr 10-30 mL/minute: Administer twice daily
Clcr<10 mL/minute: Administer once daily

Dosing adjustment in hepatic impairment: Avoid use

SUPPLIED:
Tablet (Azulfidine®): 500 mg
Tablet, delayed release, enteric coated (Azulfidine® EN-tabs®): 500 mg
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Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.