      Document 0002
 DOCN  DRG0002
 UNIQUE IDENTIFIER        DRG-0245
 NAME OF SUBSTANCE        Levamisole hydrochloride [USAN 1996]
 REGISTRY NUMBER          16595-80-5
 STANDARD CHEMICAL NAME   Imidazol[2,1-b]thiazole, 2, 3, 5,
                          6-tetrahydro-6-phenyl-, monohydrochloride,
                          (S)- [USAN 1996]
 SYNONYMS                 Ergamisol [USAN 1996]
 PROTOCOL ID NUMBERS      NCI 95 C-184
 SECONDARY SOURCE ID      R 12,564 [USAN 1996]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Appears to act as an
                          immunorestorative agent in the presence of
                          immunosuppression resulting from recent
                          surgery and chemotherapy, but does not
                          stimulate the immune response to above normal
                          levels. May be related to T-cell activation
                          and proliferation, augmentation of monocyte
                          and macrophage activity, and increases in
                          neutrophil mobility, adherence, and
                          chemotaxis. Does not have cytotoxic effects.
                          Rapidly absorbed from the gastrointestinal
                          tract. The plasma half-life is between 3-4
                          hours for levamisole and 16 hours for its
                          metabolites. It is extensively metabolized by
                          the liver and the metabolites excreted mainly
                          by the kidneys. [USP DI 1996] [Physicians
                          GenRx 1996]
 DISEASES STUDIED/TREATED Enhancement of immune function in HIV
                          infection [Physicians GenRx 1996]
 CLASSIFICATION CODE      Immunomodulator [Physicians GenRx 1996]
 OTHER MAJOR USES         Indicated, in combination with fluorouracil,
                          for treatment of Dukes C adenocarinoma of the
                          colon following complete resection of primary
                          tumor [USP DI 1996]
 SUBSTANCE INTERACTIONS   May interact with alcohol to produce
                          Antabuse-like side effects. May also
                          interact with fluorouracil to increase plasma
                          levels of phenytoin. [Physicians GenRx 1996]
 ADVERSE EFFECTS          Adverse effects (in combination with
                          fluorouracil) may include nausea, vomiting,
                          diarrhea, stomatitis, anorexia, rash,
                          pruritus, flu-like symptoms, fever, chills,
                          dizziness, ataxia, depression, confusion,
                          memory loss, weakness, inability to
                          concentrate, headache, reversible
                          neutropenia, sepsis, thrombocytopenia, and
                          hyperbilirubinemia. Adverse effects when
                          administered alone may include rash,
                          arthralgia/myalgia, fever, neutropenia,
                          urinary infection, and cough. Other adverse
                          effects reported in worldwide experience with
                          levamisole hydrochloride include exfoliative
                          dermatitis, periorbital edema, vaginal
                          bleeding, anaphylaxis, convulsions,
                          hallucinations, renal failure,
                          hyperlipidemia, elevated serum creatinine,
                          and increased alkaline phosphatase.
                          [Physicians GenRx 1996]
 CONTRAINDICATIONS        Contraindicated in patients with known
                          hypersensitivity to the drug or its
                          components. [Physicians GenRx 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C11H12N2S.HCl [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 240.76 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   STABILITY: Stable in acid aqueous media;
                          hydrolyzes in alkaline or neutral solutions.
                          [Physicians GenRx 1996]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White to pale cream
                          colored crystalline powder that is almost
                          odorless. [Physicians GenRx 1996]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 50 mg tablets. [Physicians GenRx
                          1996]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [Physicians GenRx
                          1996]
 SUBSTANCE DELIVERY DATA  STORAGE INSTRUCTIONS: Store at 15-30 C (59-86
                          F). Protect from moisture. [Physicians GenRx
                          1996]
 MANUFACTURERS            Janssen Research Foundation
 REFERENCES               ICA8/92401191. Laane H, Eussen R, Graafmans
                          J. The effects of levamisole on HIV-infected
                          patients. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B163 (abstract no. PoB 3456).
 ENTRY MONTH              9605
 LAST REVISION DATE       960612
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
