Showing posts with label Slow-Acting Antirheumatic Agent. Show all posts
Showing posts with label Slow-Acting Antirheumatic Agent. Show all posts

Levamisole (Ergamisol)

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Name: Levamisole (Ergamisol)

Class: Slow-Acting Antirheumatic Agent (Veterinary Anti-Helminthic Agent)

Mechanism: Enhances cell-mediated immune responses (­ chemotaxis & phagocytosis of PMNs and Mfs, ­ T cell fxn). How these effects ameliorate RA is unknown.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Rash (most common), leukopenia, agranulocytosis, thrombocytopenia, influenza-like illnesses, mouth ulcers, n/v.

Utility: Treat rheumatoid arthritis (off-label use).

Special Features:

 

Hydroxychloroquine (Plaquenil)

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Name: Hydroxychloroquine (Plaquenil)

Class: Slow-Acting Antirheumatic Agent (Anti-Malarial Agent)

Mechanism: Unknown. Inhib. nucleic acid synth, stabilizes lysosomal membranes, traps free radicals.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: GI upset, pruritis, headaches, visual disturbances, discoloration of nail beds and mucous membranes.

Utility: Treat rheumatoid arthritis that has been unresponsive to NSAIDs. Also used to treat rheumatoid arthritis in conjunction w/an NSAID (allows use of lower dose of hydroxychloroquine).

Special Features:

 

Methotrexate (Rheumatrex)

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Name: Methotrexate (Rheumatrex)

Class: Slow-Acting Antirheumatic Agent (AntiMetabolismolite)

Mechanism: Inhib. dihydrofolate reductase ® inhib. of formation of tetrahydrofolic acid ® ¯ synth of purines, thymidylic acid, methionine, and serine ®
¯ DNA/RNA/protein synth. ® eventual cell death.

Absorption: Oral, IV, IM, IT.

Dist.: No CNS unless administered IT.

Metabolism.: Excretion, t½:

Toxicity/S.E.s: Stomatitis, myelosuppression, erythema, rash, urticaria, alopecia, n/v/d. Long term use may ® hepatic fibrosis. High doses may ® crystalluria. Patient must be well hydrated and have alkaline urine to avoid renal toxicity. Also pulmonary toxicity in children. IT admin. ® subacute meningeal irritation, stiff neck, headache, fever; rarely seizures, encephalopathy, paraplegia. C/i w/pregnancy (teratogenic).

Utility: Low doses useful in treating rheumatoid arthritis and severe psoriasis. Effective against acute lymphocytic leukemia, choriocarcinoma, Burkitt’s lymphoma, breast cancer, head/neck carcinomas. High doses are curative for osteogenic sarcoma and choriocarcinoma.

 

D-penicillamine (Cuprimine)

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Name: D-penicillamine (Cuprimine)

Class: Slow-Acting Antirheumatic Agent

Mechanism: Unknown. Suppresses/modifies immune system & interacts w/leukocyte membrane receptors. Also chelates heavy metals (e.g., Pb, Hg, As, Cu).

Absorption: Oral.

Dist.: 80% protein bound.

Metabolism.:

Excretion, t½: Urine.

Toxicity/S.E.s: Mucocutaneous—pruritis, dermatitis. Renal—proteinuria,
nephrotic synd. Hematologic—thrombocytopenia, aplastic anemia. Pulmonary—hemorrhagic pneumonitis.

Utility: Treatment of patients w/rheumatoid arthritis who are unresponsive to NSAIDs or whose symptoms persist despite maximal tolerated doses of NSAIDs.

Special Features:

 

Gold (Auranofin, Aurothioglucose)

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Name: Gold (Auranofin, Aurothioglucose)

Class: Slow-Acting Antirheumatic Agent

Mechanism: Unknown. May involve alteration of macrophage fxn.

Absorption: Auranofin—oral. Aurathioglucose—IM.

Dist.: 95% protein bound.

Metabolism.:

Excretion, t½: 65% in urine, 35% feces. 5-6 days.

Toxicity/S.E.s: Affects about 1/3 of patients. Mucocutaneous—pruritis & dermatitis. Renal—proteinuria, nephrotic synd., hematuria. Hematologic—eosinophilia, thrombocytopenia, aplastic anemia.

Utility: Treatment of patients w/rheumatoid arthritis who are unresponsive to NSAIDs or whose symptoms persist despite maximal tolerated doses of NSAIDs.

Special Features: