      Document 0097
 DOCN  DRG0097
 UNIQUE IDENTIFIER        DRG-0150
 NAME OF SUBSTANCE        Cimetidine [USAN 1996]
 REGISTRY NUMBER          51481-61-9
 STANDARD CHEMICAL NAME   N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imida-
                          zol-4-yl) methyl)thio)ethyl)guanidine [Merck
                          Index 1989]
 SYNONYMS                 Tagamet [USAN 1996]
 SYNONYMS                 Acibilin [Merck Index 1989]
 SYNONYMS                 Acinil [Merck Index 1989]
 SYNONYMS                 Cimal [Merck Index 1989]
 SYNONYMS                 Cimetag [Merck Index 1989]
 SYNONYMS                 Cimetum [Merck Index 1989]
 SYNONYMS                 Edalene [Merck Index 1989]
 SYNONYMS                 Dyspamet [Merck Index 1989]
 SYNONYMS                 Eureceptor [Merck Index 1989]
 SYNONYMS                 Gastromet [Merck Index 1989]
 SYNONYMS                 Metracin [Merck Index 1989]
 SYNONYMS                 Peptol [Merck Index 1989]
 SYNONYMS                 Tametin [Merck Index 1989]
 SYNONYMS                 Tratul [Merck Index 1989]
 SYNONYMS                 Ulcedin [Merck Index 1989]
 SYNONYMS                 Ulcedine [Merck Index 1989]
 SYNONYMS                 Ulcerfen [Merck Index 1989]
 SYNONYMS                 Ulcimet [Merck Index 1989]
 SYNONYMS                 Ulcofalk [Merck Index 1989]
 SYNONYMS                 Ulcomedina [Merck Index 1989]
 SYNONYMS                 Ulcomet [Merck Index 1989]
 SYNONYMS                 Ulhys [Merck Index 1989]
 SYNONYMS                 Valmagen [Merck Index 1989]
 SYNONYMS                 Venopex [Merck Index 1989]
 PROTOCOL ID NUMBERS      FDA 119A
 SECONDARY SOURCE ID      SK & F 92334 [MeSH]
 SECONDARY SOURCE ID      SKF 92334 [MeSH]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Cimetidine competitively
                          inhibits the action of histamine at the
                          histamine H2 receptors of the parietal cells
                          and thus is a histamine H2-receptor
                          antagonist. Cimetidine inhibits gastric acid
                          secretion stimulated by food, histamine,
                          pentagastrin, caffeine and insulin.
                          Cimetidine may have an immodulatory effect by
                          virtue of its interaction with H2 receptors
                          on cells in the immune system. In clinical
                          studies of the drug significant increases in
                          immunoglobulins, B-lymphocytes, complement
                          C4, and CD4 counts have been reported.
                          Cimetidine is rapidly absorbed after oral
                          administration and peak levels occur in 45-90
                          minutes. Half-life is approximately 2 hours.
                          Principally excreted in the urine. [PDR 1995]
                          [AmFAR Tx Dir 1995;7(4)]
 DISEASES STUDIED/TREATED Enhancement of immune function in HIV
                          infection [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Immunomodulator [AmFAR Tx Dir 1993;6(4)]
 CLASSIFICATION CODE      Histamine (H2) receptor antagonist [USAN
                          1996]
 OTHER MAJOR USES         Treatment of active duodenal ulcer; active
                          benign gastric ulcer; erosive
                          gastroesophageal reflux disease; pathological
                          hypersecretory conditions (e.g.,
                          Zollinger-Ellison Syndrome); and prevention
                          of upper gastrointestinal bleeding in
                          critically-ill patients [PDR 1995]
 SUBSTANCE INTERACTIONS   Interacts with warfarin-like anticoagulants,
                          phenytoin, propranolol, nifedipine,
                          chlordiazepoxide, diazepam, certain tricyclic
                          antidepressants, lidocaine, theophylline, and
                          metronidazole. [PDR 1995]
 ADVERSE EFFECTS          Adverse effects may include diarrhea,
                          dizziness and somnolence (usually mild),
                          headache, reversible confusion states,
                          gynecomastia, reversible impotence, decreased
                          white blood cell counts, increases in serum
                          transaminase, fever and allergic reactions,
                          small increases in plasma creatinine,
                          bradycardia, tachycardia, A-V heart block,
                          reversible arthralgia and myalgia, and
                          various skin reactions. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in persons with known
                          hypersensitivity to cimetidine. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Histamine H2 receptor
                          antagonist. Chemically related to histamine.
                          Contains an imidazole ring [PDR 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Crystals; has a bitter
                          taste and characteristic odor [PDR 1995]
                          [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C10H16N6S [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 252.35 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 141-143 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C47.60%, H6.39%,
                          N33.30%, S12.71% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in alcohol; slightly
                          soluble in water; very slightly soluble in
                          chloroform; insoluble in ether [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Tablets; flavored liquid; or
                          vials for injection. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral, IV, and IM. [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store at controlled room temperature
                          (15-30 C; 59-86 F). [PDR 1995]
 MANUFACTURERS            Smith, Kline and French Laboratories
 REFERENCES               Matsumoto S. Cimetidine and survival with
                          colorectal cancer [letter; comment]. Lancet.
                          1995 Jul 8;346(8967):115.
 REFERENCES               Saville MW, Lietzau J, Pluda JM, Feuerstein
                          I, Odom J, Wilson WH, Humphrey RW, Feigal E,
                          Steinberg SM, Broder S, et al. Treatment of
                          HIV-associated Kaposi's sarcoma with
                          paclitaxel. Lancet. 1995 Jul
                          1;346(8966):26-8.
 REFERENCES               Stashower ME, Yeager JK, Smith KJ, Skelton
                          HG, Wagner KF. Cimetidine as therapy for
                          treatment-resistant psoriasis in a patient
                          with acquired immunodeficiency syndrome. Arch
                          Dermatol 1993 Jul;129(7):848-50.
 REFERENCES               Munnings HA. Cimetidine. Potential for its
                          use in HIV disease [letter]. West Indian Med
                          J. 1992 Sep;41(3):95.
 REFERENCES               Colin-Jones DG, Langman MJ, Lawson DH, Logan
                          RF, Paterson KR, Vessey MP. Postmarketing
                          surveillance of the safety of cimetidine: 10
                          year mortality report. Gut 1992
                          Sep;33(9):1280-4.
 REFERENCES               Smith TJ, Kaplowitz LG. Pilot study of
                          cimetidine in the treatment of Kaposi's
                          sarcoma in patients with acquired
                          immunodeficiency syndrome [letter]. J Natl
                          Cancer Inst. 1991 Jan 16;83(2):139-41.
 REFERENCES               Smith T, Kaplowitz LG. TREATMENT OF EPIDEMIC
                          KAPOSI'S SARCOMA (KS) WITH CIMETIDINE
                          (MEETING ABSTRACT). Proc Annu Meet Am Soc
                          Clin Oncol; 9:A15 1990.
 ENTRY MONTH              9212
 LAST REVISION DATE       960310
 

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