      Document 0137
 DOCN  DRG0137
 UNIQUE IDENTIFIER        DRG-0110
 NAME OF SUBSTANCE        Ciprofloxacin [USAN 1996]
 REGISTRY NUMBER          85721-33-1
 STANDARD CHEMICAL NAME   1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-
                          (1-piperazinyl)-3-quinolinecarboxylic acid
                          [Merck Index 1989]
 SYNONYMS                 Ciflox [Merck Index 1989]
 SYNONYMS                 Ciprobay [Merck Index 1989]
 SYNONYMS                 Ciproxan [Merck Index 1989]
 SYNONYMS                 Ciproxin [Merck Index 1989]
 SYNONYMS                 Velmonit [Merck Index 1989]
 SYNONYMS                 Cipro [USAN 1996]
 SYNONYMS                 Cipro IV [USAN 1996]
 PROTOCOL ID NUMBERS      NIAID ACTG 135
 PROTOCOL ID NUMBERS      NIAID ACTG 223
 SECONDARY SOURCE ID      Bay Q 3939 [USAN 1996]
 SECONDARY SOURCE ID      German Patent: 3,142,854 [Merck Index 1989]
 SECONDARY SOURCE ID      U.S. Patent: 4,670,444 [Merck Index 1989]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Antibacterial against a wide
                          range of gram-positive and gram-negative
                          organisms; bactericidal action results from
                          interference with the enzyme DNA gyrase
                          needed for the synthesis of bacterial DNA.
                          [PDR 1995]
 DISEASES STUDIED/TREATED Possible bactericidal activity against some,
                          but not all, Mycobacterium avium complex
                          (MAC) strains [AmFAR Tx Dir 1995;7(4)] [NIAID
                          ACTG 135] [AHFS Drug Information 1995]
 DISEASES STUDIED/TREATED Under investigation for combination therapy
                          of MAC [AmFAR Tx Dir 1995;7(4)] [NIAID ACTG
                          135] [AHFS Drug Information 1995]
 CLASSIFICATION CODE      Antibacterial [USAN 1996]
 OTHER MAJOR USES         Indicated for the treatment of lower
                          respiratory infections; skin and skin
                          structure infections; bone and joint
                          infections; urinary tract infections; and
                          infectious diarrhea caused by susceptible
                          strains of gram positive and gram negative
                          microorganisms [PDR 1995]
 SUBSTANCE INTERACTIONS   Concurrent administration of theophylline may
                          lead to elevated plasma concentrations of
                          theophylline and increase the risk of
                          theophylline adverse reactions. Ciprofloxacin
                          absorption may be decreased by antacids
                          containing magnesium, aluminum or calcium, by
                          sucralfate or by divalent and trivalent
                          cations such as iron in multivitamin and
                          mineral preparations. Some quinolones,
                          including ciprofloxacin, have been associated
                          with transient elevations in serum creatinine
                          in patients receiving cyclosporine
                          concomitantly. Quinolones have also enhanced
                          the effects of warfarin or other coumarin
                          derivatives and therefore prothrombin times
                          should be monitored. Caffeine metabolism may
                          be affected, increasing its serum half-life.
                          In vitro, ciprofloxacin exhibits synergism
                          with aminoglycosides and beta-lactam
                          antibiotics; however, clinical effects vary.
                          Probenecid interferes with renal tubular
                          secretion of ciprofloxacin. [PDR 1995] [AHFS
                          Drug Information 1995]
 ADVERSE EFFECTS          Adverse effects may include nausea, diarrhea,
                          vomiting, abdominal pain/discomfort,
                          headache, restlessness, and rash.
                          Phototoxicity, dizziness, lightheadedness and
                          severe hypersensitivity reactions have been
                          reported. [PDR 1995] [AHFS Drug Information
                          1995]
 CONTRAINDICATIONS        Contraindicated in patients with history of
                          hypersensitivity to ciprofloxacin or other
                          quinolones. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Fluorinated quinolone with
                          the fluorine at the 6-position, a piperazine
                          moiety at the 7-position, and a three carbon
                          ring at the 1-position [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C17H18FN3O3 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 331.35 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C61.62%, H5.48%,
                          F5.73%, N12.68%, O14.49% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Faint to light yellow
                          crystalline powder [PDR 1995]
 CHEMICAL/PHYSICAL DATA   STABILITY: When diluted in an IV infusion
                          solution ciprofloxacin is stable for 14 days
                          in a refrigerator or at room temperature [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Tablets (250, 500, and 750 mg);
                          vials containing 200 or 400 mg. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral; intravenous. [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store tablets below 30 C (86 F) and
                          vials between 5 and 25 C (41 and 77 F).
                          Protect from light, heat, and freezing. [PDR
                          1995]
 MANUFACTURERS            Miles
 REFERENCES               Lucena MI, Marquez M, Velasco JL, Andrade RJ.
                          Acute renal failure attributable to
                          ciprofloxacin in a patient with the acquired
                          immunodeficiency syndrome [letter;comment].
                          Arch Intern Med. 1995 Jan 9;155(1):114-5.
 REFERENCES               Fan-Harvard P, Sanchorawala V, Oh J, Moser
                          EM, Smith SP. Concurrent use of foscarnet and
                          ciprofloxacin may increase the propensity for
                          seizures. Ann Pharmacother. 1994
                          Jul-Aug;28(7-8):869-72.
 REFERENCES               Jacobson MA, Yajko D, Northfelt D, Charlebois
                          E, Gary D, Brosgart C, Sanders CA, Hadley WK.
                          Randomized, placebo-controlled trial of
                          rifampin, ethambutol, and ciprofloxacin for
                          AIDS patients with disseminated Mycobacterium
                          avium complex infection. J Infect Dis. 1993
                          Jul;168(1):112-9.
 REFERENCES               Schurmann D, Eljaschewitsch J, Sandfort J,
                          Stephan R, Pohle HD, Ruf B. Efficacy of
                          ciprofloxacin in treating AIDS-related
                          bacteremic nontyphoidal Salmonella infection.
                          Int Conf AIDS. 1993 Jun 6-11;9(1):51
                          (abstract no. WS-B08-3).
 REFERENCES               Kennedy N, Fox R, Kisyombe GM, Saruni AO,
                          Uiso LO, Ramsay AR, Ngowi FI, Gillespie SH.
                          Early bactericidal and sterilizing activities
                          of ciprofloxacin in pulmonary tuberculosis
                          [see comments]. Am Rev Respir Dis. 1993
                          Dec;148(6 Pt 1):1547-51.
 REFERENCES               de Lalla F, Maserati R, Scarpellini P, Marone
                          P, Nicolin R, Caccamo F, Rigoli R.
                          Clarithromycin-ciprofloxacin-amikacin for
                          therapy of Mycobacterium avium-Mycobacterium
                          intracellulare bacteremia in patients with
                          AIDS. Antimicrob Agents Chemother. 1992
                          Jul;36(7):1567-9.
 REFERENCES               Kemper CA, Meng TC, Nussbaum J, Chiu J,
                          Feigal DF, Bartok AE, Leedom JM, Tilles JG,
                          Deresinski SC, McCutchan JA. Treatment of
                          Mycobacterium avium complex bacteremia in
                          AIDS with a four-drug oral regimen. Rifampin,
                          ethambutol, clofazimine, and ciprofloxacin.
                          Ann Intern Med. 1992 Mar 15;116(6):466-72.
 REFERENCES               Solorzano R. A comparative study of the
                          efficacy of ciprofloxacin and erythromycin in
                          chancroid. Int Conf AIDS. 1992 Jul
                          19-24;8(1):We54 (abstract no. WeB 1050).
 REFERENCES               Balachandran T, Roberts AP, Evans BA, Azadian
                          BS. Single-dose therapy of anogenital and
                          pharyngeal gonorrhoea with ciprofloxacin [see
                          comments]. Int J STD AIDS. 1992
                          Jan-Feb;3(1):49-51.
 REFERENCES               Deamer RL, Prichard JG, Loman GJ.
                          Hypersensitivity and anaphylactoid reactions
                          to ciprofloxacin. Ann Pharmacother. 1992
                          Sep;26(9):1081-4.
 ENTRY MONTH              9104
 LAST REVISION DATE       960314
 

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