Rheumatology Book

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Hydroxychloroquine

Aka: Hydroxychloroquine, Plaquenil
  1. Indications
    1. Early Rheumatoid Arthritis
      1. Especially Antinuclear Antibody positive
    2. Systemic Lupus Erythematosus
  2. Mechanism
    1. Antimalarial agent used in rheumatic disease
    2. Modified Chloroquine to reduce retinopathy risk
  3. Efficacy
    1. Response in 70-80% of cases
    2. Response occurs in 3-6 months
    3. Highest efficacy when used early in disease process
  4. Dose
    1. Initial: 200 mg PO bid
    2. Taper after 1-2 years when stable: 200 mg PO qd
  5. Adverse Effects
    1. Retinopathy
      1. Rare (contrast with Chloroquine)
    2. Neurologic adverse effects
      1. Early toxicity (subsides within 2 weeks)
        1. Irritability
        2. Insomnia
        3. Headache
      2. Late toxicity requires medication discontinuation
        1. Tinnitus
        2. Decreased hearing acuity
      3. Very rare toxicity
        1. Myopathy or muscular weakness
    3. Gastrointestinal adverse effects
      1. Increased stool frequency
      2. Diarrhea
      3. Bloating
      4. Nausea
    4. Cardiovascular adverse effects
      1. Palpitations
      2. Premature Atrial Contractions
      3. Conduction defects
  6. Monitoring
    1. Routine eye exam every 6-12 months
  7. References
    1. Matteson (2000) Mayo Clin Proc 75:669-74
    2. Pincus (1999) Clin Rheumatol 17(6 Suppl 18):S2-S124

Hydroxychloroquine (C0020336)

Definition (NCI) A 4-aminoquinoline with immunosuppressive, antiautophagy, and antimalarial activities. Although the precise mechanism of action is unknown, hydroxychloroquine may suppress immune function by interfering with the processing and presentation of antigens and the production of cytokines. As a lysosomotropic agent, hydroxychloroquine raises intralysosomal pH, impairing autophagic protein degradation; hydroxychloroquine-mediated accumulation of ineffective autophagosomes may result in cell death in tumor cells reliant on autophagy for survival. In addition, this agent is highly active against the erythrocytic forms of P. vivax and malariae and most strains of P. falciparum but not the gametocytes of P. falciparum.
Definition (MSH) A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970)
Definition (NCI) A substance that decreases immune responses in the body. It is used to treat some autoimmune diseases, and is being studied as a treatment for graft-versus-host disease. Hydroxychloroquine belongs to the family of drugs called antiprotozoals.
Definition (PDQ) A 4-aminoquinoline with antimalarial and immunosuppressive properties. Although its precise mechanism of action is unknown, hydroxychloroquine may suppress immune function by interfering with the processing and presentation of antigens and the production of cytokines. This agent is highly active against the erythrocytic forms of P. vivax and malariae and most strains of P. falciparum but not the gametocytes of P. falciparum. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38571&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38571&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C557" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D006886
SnomedCT 373540008, 83490000
English Hydroxychlorochin, Hydroxychloroquine, Oxychlorochin, Oxychloroquine, hydroxychloroquine, ethanol, 2-((4-((7-chloro-4-quinolinyl)amino)pentyl)ethylamino)-, Hydroxychloroquine [Chemical/Ingredient], Hydroxychloroquine (product), Hydroxychloroquine (substance), HCQ, HYDROXYCHLOROQUINE
Swedish Hydroxiklorokin
Czech hydroxychlorochin
Finnish Hydroksiklorokiini
Russian GIDROKSIKHLOROKHIN, OKSIKHLOROKHIN, PLAKVENIL, ГИДРОКСИХЛОРОХИН, ОКСИХЛОРОХИН, ПЛАКВЕНИЛ
Polish Hydroksychlorochina
Japanese オキシクロロキン, ヒドロキシクロロキン
Spanish hidroxicloroquina (producto), hidroxicloroquina (sustancia), hidroxicloroquina, Hidroxicloroquina, Oxicloroquina
French Hydroxychloroquine
German Hydroxychlorochin, Hydroxychloroquin, Oxychlorochin, Oxychloroquin
Italian Idrossiclorochina
Portuguese Hidroxicloroquina, Oxicloroquina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Plaquenil (C0699177)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D006886
English Plaquenil Sulfate, plaquenil sulfate, plaquenil, Plaquenil
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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