      Document 0135
 DOCN  DRG0135
 UNIQUE IDENTIFIER        DRG-0112
 NAME OF SUBSTANCE        Amikacin sulfate [USAN 1996]
 REGISTRY NUMBER          39831-55-5
 RELATED REGISTRY NUMBER  37517-28-5
 STANDARD CHEMICAL NAME   D-Streptamine,
                          O-3-amino-3-deoxy-alpha-D-glucopyranosyl-(1-
                          6)-O-(6-amino-6-deoxy-alpha-D-glucopyranosyl--
                          (1-
                          4))-N1-(4-amino-2-hydroxy-1-oxobutyl)-2-deoxy-
                          -, (S)- sulfate (1:2) (salt) [USAN 1996]
 SYNONYMS                 Amikin [USAN 1996]
 SYNONYMS                 Amiklin [Merck Index 1989]
 SYNONYMS                 Biklin [Merck Index 1989]
 SYNONYMS                 Fabianol [Merck Index 1989]
 SYNONYMS                 Kaminax [Merck Index 1989]
 SYNONYMS                 Mikavir [Merck Index 1989]
 SYNONYMS                 Novamin [Merck Index 1989]
 SYNONYMS                 Pierami [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID ACTG 135
 PROTOCOL ID NUMBERS      NIAID ACTG 238
 SECONDARY SOURCE ID      BB-K8 [Merck Index 1989]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Antibacterial. Rapidly
                          absorbed after intramuscular injection and
                          well tolerated. Mean serum half-life of
                          slightly over two hours. Excreted primarily
                          by glomular filtration. Following admini
                          stration of recommended dose, therapeutic
                          levels are found in the bone, heart, gall
                          bladder and lung, as well as significant
                          concentrations in urine, bile, sputum,
                          bronchial secretions, interstitial, synovial,
                          and pleural fluids. [PDR 1995]
 DISEASES STUDIED/TREATED Under investigation in combination therapy
                          for Mycobacterium avium complex (MAC) [AmFAR
                          Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Antibacterial [USAN 1996]
 OTHER MAJOR USES         Indicated in the short term treatment of
                          serious infections due to susceptible strains
                          of gram-negative bacteria, including
                          Pseudomonas species, Escherichia coli,
                          species of indole-positive and
                          indole-negative Proteus, Providencia species,
                          Klebsiella-Enterobacter-Serratia species, and
                          Acinetobacter [Mima-Herellea] species [PDR
                          1995]
 SUBSTANCE INTERACTIONS   Concurrent and/or sequential systemic, oral,
                          or topical use of other neurotoxic or
                          nephrotoxic products, particularly
                          bacitracin, cisplatin, amphotericin B,
                          cephaloridine, paromomycin, viomycin,
                          polymyxin B, colistin, vancomycin, or other
                          aminoglycosides should be avoided. Concurrent
                          use with potent diuretics [ethacrynic acid or
                          furosemide) should also be avoided. [PDR
                          1995]
 ADVERSE EFFECTS          May possibly induce auditory/vestibular
                          dysfunction, renal toxicity, and
                          neuromuscular blockade. May cause
                          irreversible deafness in children when given
                          to pregnant women. May cause nausea,
                          vomiting, anemia, and rash. [PDR 1995] [NIAID
                          ACTG 238]
 CONTRAINDICATIONS        Contraindicated in patients with history of
                          hypersensitivity to amikacin or with history
                          of hypersensitivity or serious toxic
                          reactions to aminoglycosides. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Semisynthetic
                          aminoglycoside antibiotic derived from
                          kanamycin A [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C22H43N5O13.2H2SO4 [USAN
                          1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 781.77 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   STABILITY: Stable at room temperature for 24
                          hours at concentrations of 0.25 and 5 mg/ml
                          in certain solutions (e.g., 5% Dextrose
                          Injection, USP) [AHFS Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   STABILITY: Undiluted solutions are stable for
                          2 years [AHFS Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Sparingly soluble in water [AHFS
                          Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Colorless to light
                          straw colored solution [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 203-204 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C45.12%, H7.40%,
                          N11.96%, O35.52% [Merck Index 1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Vials containing 100 and 500
                          mg/2 ml or 1 g/4 ml and disposable syringes
                          containing 50 mg/2 ml. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: IV or IM injection. [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Room temperature. [PDR 1995]
 MANUFACTURERS            Bristol-Myers Squibb
 REFERENCES               Abraham G. Streptococcus pyogenes peritonitis
                          associated with genital swelling and
                          gastroenteritis caused by Cryptosporidium and
                          Salmonella paratyphi B in an HIV infected
                          patient on CAPD [letter]. Nephrol Dial
                          Transplant. 1995;10(1):140-1.
 REFERENCES               Rastogi N, Goh KS, Bryskier A. Activities of
                          roxithromycin used alone and in combination
                          with ethambutol, rifampin, amikacin,
                          ofloxacin, and clofazimine against
                          Mycobacterium avium complex. Antimicrob
                          Agents Chemother. 1994 Jun;38(6):1433-8.
 REFERENCES               Jorup-Ronstrom C, Julander I, Petrini B.
                          Efficacy of triple drug regimen of amikacin,
                          ethambutol, and rifabutin in AIDS patients
                          with symptomatic Mycobacterium avium complex
                          infection. J Infect. 1993 Jan;26(1):67-70.
 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               Benson CA, Kessler HA, Pottage JC Jr,
                          Trenholme GM. Successful treatment of
                          acquired immunodeficiency syndrome-related
                          Mycobacterium avium complex disease with a
                          multiple drug regimen including amikacin.
                          Arch Intern Med. 1991 Mar;151(3):582-5.
 REFERENCES               Chiu J, Nussbaum J, Bozzette S, Tilles JG,
                          Young LS, Leedom J, Heseltine PN, McCutchan
                          JA. Treatment of disseminated Mycobacterium
                          avium complex infection in AIDS with
                          amikacin, ethambutol, rifampin, and
                          ciprofloxacin. Ann Intern Med. 1990 Sep
                          1;113(5):358-61.
 REFERENCES               Benson C, Pottage J, Kessler H. Treatment of
                          AIDS-related disseminated Mycobacterium Avium
                          Complex Disease (D-MAC) with a multiple drug
                          regimen including amikacin. Int Conf AIDS.
                          1990 Jun 20-23;6(1):251 (abstract no.
                          Th.B.517).
 ENTRY MONTH              9104
 LAST REVISION DATE       951213
 

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