Hydroxychloroquine (Plaquenil)

Post a comment

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, :

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)

Post a comment

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, :

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)

Post a comment

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, : 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)

Post a comment

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, : 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:

 

Ketorolac (Toradol)

Post a comment

Name: Ketorolac (Toradol)

Class: NSAID

Mechanism: Inhibition of cyclooxygenase ® inhibition of prostaglandin synthesis. Also inhib. of PMN adhesion, aggregation, & activation (ramifications uncertain).

Absorption: Parenteral only.

Dist.: Weak acid (pKa <5). ~90% protein binding. Vd @ albumin Vd.

Metabolism.: 1° = liver. Phase I (oxid.) & Phase II (conjug.).

Excretion, : Metabolismolites in urine. Renal failure ® retention of glucuronide Metabolismolites ® potential for toxic accumulation of orig. compound.

Toxicity/S.E.s: GI—esophagitis & esophageal strictures; gastroduodenal erosions, ulceration, hemorrhage, & perforation; ileal inflammation, strictures, hemorrhage, & perforation; colon hemorrhage and exacerbation of inflammatory bowel disease. Hypersensitivity—possible cross-reaction w/aspirin. Inhib. of platelet aggregation. Kidney—Na+ retention, hemodynamic renal failure, interstitial nephritis. CNS—dizziness, tinnitus, headache, aseptic meningitis. Overdose—Acute is less serious than w/aspirin, but may cause Metabolismolic acidosis & seizures.

Utility: Treat pain, inflammation, dysmenorrhea, patent ductus arteriosis, acute gout. May be as effective as morphine or meperidine for short-term relief of mod.-severe pain.