      Document 0183
 DOCN  DRG0183
 UNIQUE IDENTIFIER        DRG-0064
 NAME OF SUBSTANCE        Nystatin [USAN 1996]
 REGISTRY NUMBER          1400-61-9
 STANDARD CHEMICAL NAME   Nystatin [USAN 1996]
 SYNONYMS                 Candio-Hermal [Merck Index 1989]
 SYNONYMS                 Diastatin [Merck Index 1989]
 SYNONYMS                 Fungicidin [Merck Index 1989]
 SYNONYMS                 Moronal [Merck Index 1989]
 SYNONYMS                 Mykostatyna [CHEMLINE]
 SYNONYMS                 Myconystatin [CHEMLINE]
 SYNONYMS                 Mycostatin [USAN 1996]
 SYNONYMS                 Mycostatin 20 [CHEMLINE]
 SYNONYMS                 Nilstatin [USAN 1996]
 SYNONYMS                 Nistatina [CHEMLINE]
 SYNONYMS                 Nystan [Merck Index 1989]
 SYNONYMS                 Nastatine [CHEMLINE]
 SYNONYMS                 Nystatinum [CHEMLINE]
 SYNONYMS                 Nystavescent [Merck Index 1989]
 SYNONYMS                 Nystex [USAN 1996]
 SYNONYMS                 O-V Statin [USAN 1996]
 SYNONYMS                 Stamycin [CHEMLINE]
 SYNONYMS                 Zydin E [CHEMLINE]
 SYNONYMS                 Component of Comycin [USAN 1996]
 SYNONYMS                 Component of Mycolog II [USAN 1996]
 SYNONYMS                 Component of Mytrex [USAN 1996]
 SYNONYMS                 Component of Nystaform [USAN 1996]
 SYNONYMS                 Component of Nystaform-HC [USAN 1996]
 SYNONYMS                 Component of Tetrastatin [USAN 1996]
 SYNONYMS                 Biofanal [Merck Index 1989]
 SYNONYMS                 Candex [Merck Index 1989]
 SYNONYMS                 Multilind [Merck Index 1989]
 SYNONYMS                 Nystatin LF I.V. [Merck Index 1983]
 SYNONYMS                 Nilstat [Drug Evaluations Annual 1992]
 SYNONYMS                 Component of Myco-Triacet II [USAN 1996]
 PROTOCOL ID NUMBERS      FDA 026A
 PROTOCOL ID NUMBERS      FDA 026B
 PROTOCOL ID NUMBERS      FDA 103A
 PROTOCOL ID NUMBERS      FDA 042A
 PROTOCOL ID NUMBERS      FDA 012Q
 PROTOCOL ID NUMBERS      FDA 103B
 PROTOCOL ID NUMBERS      FDA 103C
 SECONDARY SOURCE ID      AI3-26526 [CHEMLINE]
 SECONDARY SOURCE ID      Caswell No. 607B [CHEMLINE]
 SECONDARY SOURCE ID      HSDB 3138 [CHEMLINE]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Nystatin is both fungistatic
                          and fungicidal in vitro against a wide
                          variety of yeast and yeast-like fungi.
                          Candida albicans exhibits no significant
                          resistance to nystatin in vitro on repeated
                          subculture in increasing levels of nystatin;
                          other Candida species become quite resistant.
                          Nystatin acts by binding to sterols in cell
                          membranes of susceptible fungi with resulting
                          changes in cell membrane permeability
                          allowing leakage of intracellular components.
                          Nystatin exhibits no activity against
                          bacteria, protozoa, trichomonads or viruses.
                          Gastrointestinal absorption of nystatin is
                          insignificant. Mean nystatin concentrations
                          in excess of those required in vitro to
                          inhibit growth of clinically significant
                          Candida persisted in saliva for 2 hours after
                          oral dissolution of 2 nystatin pastilles
                          (400,000 units). [PDR 1995]
 DISEASES STUDIED/TREATED Treatment of HIV-related candidiasis [AmFAR
                          Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Antifungal [USAN 1996]
 OTHER MAJOR USES         Used topically in an appropriate dosage form
                          for the treatment of cutaneous,
                          mucocutaneous, and oral cavity infections
                          caused by Candida albicans (monilia) such as
                          oral thrush, perleche, paronychia,
                          vulvovaginal candidiasis and diaper rash.
                          Approved for treatment of candidiasis [AHFS
                          Drug Information 1995; AmFAR Tx Dir
                          1995;7(4)]
 ADVERSE EFFECTS          Rarely, oral irritation or sensitization may
                          occur. Large oral doses may cause diarrhea,
                          gastrointestinal distress, nausea, and
                          vomiting. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in patients showing
                          hypersensitivity to this drug. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Nystatin is an amphoteric
                          polyene macrolide that occurs as a
                          hygroscopic, yellow to light tan powder with
                          a cereal-like odor. Each mg of nystatin
                          contains less than 4400 units of activity
                          [AHFS Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C47H75NO17 [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 926.13 [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: Above 250 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY (mg/ml at about 28 C): Water, 4.0;
                          methanol, 11.2; ethanol, 1.2; carbon
                          tetrachloride, 1.23; chloroform, 0.48;
                          benzene, 0.28; ethylene glycol, 8.75. [Merck
                          Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Solutions and aqueous suspensions
                          begin to lose activity soon after
                          preparation; aqueous suspensions are stable
                          for 10 minutes on heating to 100 C at pH 7.0
                          [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Aqueous suspensions stable in
                          moderately alkaline media, but labile at pH 9
                          and pH 2 [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Heat, light, and oxygen accelerate
                          decomposition [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Light yellow powder
                          [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: Gradually decomposed above
                          160 degrees without melting by 250 [Merck
                          Index 1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Aqueous suspension; oral or
                          vaginal tablets; topical powder; cream;
                          ointment. [AHFS Drug Information 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: May be applied topically as
                          cream, ointment, powder, vaginal tablet, or
                          oral lozenge or suspension. [AHDS Drug
                          Information 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store under refrigeration at 2-8 C
                          (36-46 F) in tight, light-resistant
                          container. [PDR 1995]
 MANUFACTURERS            Paddock Laboratories
 REFERENCES               Lloveras S, Macias JR, Masini R, Franchi M,
                          Rodriguez Rios E, Navarro L. Vaginal
                          candidiasis in females HIV+/AIDS, local
                          therapy with nistatin. Int Conf AIDS. 1994
                          Aug 7-12;10(2):144 (abstract no. PB0590).
 REFERENCES               Greensan D. Treatment of oropharyngeal
                          candidiasis in HIV- positive patients. J Am
                          Acad Dermatol. 1994 Sep;31(3 Pt 2):S51-5.
 REFERENCES               Rios A, Brewton G, Crofoot G, Quesada J, Lenk
                          R, Lopez-Berenstein G. A phase I-II clinical
                          study of Nystatin-LF IV in patients with HIV
                          infections. Int Conf AIDS. 1993 Jun
                          6-11;9(1):483 (abstract no. PO-B26-2089).
 REFERENCES               Heinic GS, Greenspan D, MacPhail LA, Dodd CL,
                          Beck C, Greenspan JS. Fluconazole-resistant
                          Candida in eight HIV-seropositive patients.
                          Int Conf AIDS. 1993 Jun 6-11;9(1):436
                          (abstract no. PO-B18-1808).
 REFERENCES               Rios A, Rosenblum M, Crofoot G, Lenk RP,
                          Lopez-Berenstein G. Pharmacokinetics of
                          liposomal nystatin in patients with human
                          immunodeficiency virus infection [letter]. J
                          Infect Dis. 1993 Jul;168(1):253-4.
 REFERENCES               Rios A, Crofoot GE, Lenk R, Hayman A,
                          Rosenblum M, Lopez-Berestein G. A phase 1
                          single dose safety evaluation and
                          pharmacokinetic (Pkc) study of
                          nystatin-liposomal formulation nystatin-LF
                          i.v. in patients with HIV infection. Int Conf
                          AIDS. 1992 Jul 19-24;8(3):127 (abstract no.
                          PuB 7473).
 REFERENCES               Nyst MJ, Perriens JH, Kimputu L, Lumbila M,
                          Nelson AM, Piot P. Gentian violet,
                          ketoconazole and nystatin in oropharyngeal
                          and esophageal candidiasis in Zairian AIDS
                          patients. Ann Soc Belg Med Trop. 1992
                          Mar;72(1):45-52.
 REFERENCES               Nyst M, Perriens J, Lusakumunu K, Kapita B,
                          Piot P. Prospective comparative study of
                          gentian violet, ketoconazole and nystatin to
                          treat oral and oesophageal candidiasis in
                          AIDS patients. Int Conf AIDS. 1990 Jun
                          20-23;6(1):238 (abstract no. Th.B.465).
 REFERENCES               Lemay MD, Cooper ER, Patel DK, Pelton SI.
                          EFFICACY AND SAFETY OF KETOCONAZOLE IN HIV
                          INFECTED INFANTS WITH MUCOCUTANEOUS
                          CANDIDIAISIS. Int Conf AIDS. 1989 Jun
                          4-9;5:496 (abstract no. B.591).
 REFERENCES               Ackerman Z, Zeltser R, Maayan S. AIDS and
                          oropharyngeal candidiasis. Isr J Dent Sci.
                          1989 Oct;2(3):162-6.
 ENTRY MONTH              8911
 LAST REVISION DATE       960604
 

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