      Document 0156
 DOCN  DRG0156
 UNIQUE IDENTIFIER        DRG-0091
 NAME OF SUBSTANCE        Chlorhexidine gluconate [USAN 1996]
 REGISTRY NUMBER          18472-51-0
 RELATED REGISTRY NUMBER  55-56-1
 STANDARD CHEMICAL NAME   2,4,11,13-Tetraazatetradecanediimidamide,
                          N,N'-bis(4-chlorophenyl)-3,12-diimino-,di-D-g-
                          luconate [USAN 1996]
 SYNONYMS                 Peridex [FDA 050A]
 SYNONYMS                 Hibiclens [USAN 1996]
 SYNONYMS                 Hibistat [USAN 1996]
 SYNONYMS                 Bacticlens [Merck Index 1989]
 SYNONYMS                 Corsodyl [Merck Index 1989]
 SYNONYMS                 Hibidil [Merck Index 1989]
 SYNONYMS                 Hibiscrub [Merck Index 1989]
 SYNONYMS                 Hibitane [Merck Index 1989]
 SYNONYMS                 Orahexal [Merck Index 1989]
 SYNONYMS                 pHisoMed [Merck Index 1989]
 SYNONYMS                 Plac Out [Merck Index 1989]
 SYNONYMS                 Plurexid [Merck Index 1989]
 SYNONYMS                 Rotersept [Merck Index 1989]
 SYNONYMS                 Unisept [Merck Index 1989]
 SYNONYMS                 1,1'-Hexamethylenebis(5-(p-chlorophenyl)bigua-
                          nide)di-D-gluconate [USAN 1996]
 PROTOCOL ID NUMBERS      FDA 050A
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Because of its positive
                          charge, chlorhexidine is adsorbed during oral
                          rinsing on the surfaces of teeth, plaque, and
                          oral mucosa, which have a net negative
                          charge. Subsequently, the adsorbed medication
                          is gradually released from these sites by
                          diffusion for up to 24 hours as the
                          concentration of chlorhexidine in the saliva
                          decreases. This release provides a continuing
                          bacteriostatic effect. Chlorhexidine is
                          adsorbed onto the cell walls of
                          microorganisms, which causes leakage of
                          intracellular components. At low
                          concentrations, chlorhexidine is
                          bacteriostatic; at higher concentrations,
                          chlorhexidine is bactericidal.
                          Pharmacokinetic studies indicate that
                          approximately 30 percent of chlorhexidine is
                          retained in the oral cavity following rinsing
                          and subsequently is slowly released into the
                          oral fluids. Studies using humans and animals
                          have shown that chlorhexidine is poorly
                          absorbed in the gastrointestinal tract. In
                          humans, the mean plasma level of
                          chlorhexidine reached a peak of 0.206 mcg per
                          gram 30 minutes following an oral dose of 300
                          mg. Following oral doses of 30 mg, excretion
                          was primarily through feces (approximately 90
                          percent); less than 1 percent of the
                          medication was excreted in the urine. In
                          addition, 12 hours after chlorhexidine was
                          administered, it was not detectable in the
                          plasma. [PDR 1995] [USP DI 1995]
 DISEASES STUDIED/TREATED Oral candidiasis [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Antimicrobial [USAN 1996]
 CLASSIFICATION CODE      Topical antibacterial [Merck Index 1989]
 OTHER MAJOR USES         Gingivitis, acute necrotizing ulcerative
                          gingivitis; postoperative (prophylaxis) mouth
                          infections; mouth infections in cancer
                          patients (prophylaxsis and treatment);
                          denture stomatitis; aphthous stomatitis and
                          dental plaque; topical preparations are used
                          as bactericidal skin wound cleansing agents
                          [USP DI 1995] [PDR 1995]
 ADVERSE EFFECTS          May cause an increase in staining of teeth
                          and other oral surfaces; an increase in
                          calculus formation and an alteration in taste
                          perception. Less frequent or rare are
                          superficial desquamative lesions (mouth
                          irritation) - reported mainly in children
                          ages 10 to 18 (the lesions are transient and
                          may be painless); tongue tip irritation and
                          parotitis (inflammation or swelling of
                          salivary glands). [PDR 1995] [USP DI 1995]
 CONTRAINDICATIONS        Front-tooth fillings having rough surfaces or
                          margins may develop permanent discoloration
                          from chlorhexidine, necessitating replacement
                          for cosmetic reasons. May be contraindicated
                          in those patients with intolerance to
                          chlorhexidine. May be contraindicated in
                          those patients with periodontitis since it is
                          not known whether the use of chlorhexidine
                          results in an increase in subgingival
                          calculus and since gingival inflammation and
                          bleeding may occur with both periodontitis
                          and gingivitis and chlorhexidine oral rinse
                          may reduce these signs, the presence or
                          absence of these signs should not be used as
                          indicators of periodontitis after the patient
                          has been treated with chlorhexidine. The oral
                          rinse should not be used by patients who are
                          known to be sensitive to chlorhexidine
                          gluconate. [USP DI 1995] [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C22H30Cl2N10.2C6H12O7
                          [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 897.77 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 134 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C52.28%, H5.98%,
                          Cl14.03%, N27.71% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY:  In water at 20 C. Miscible with
                          water, with up to 5 parts alcohol, and with
                          up to 3 parts acetone [USP DI 1990]
 CHEMICAL/PHYSICAL DATA   STABILITY: Avoid excessive heat (above 104 F)
                          with Hibiclens and Hibistat products [PDR
                          1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Bisbiguanide with
                          bacteriostatic activity [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Oral rinse (Peridex),
                          hand rinse (Hibistat germicidal handwipe
                          towelettes), skin cleanser (Hibiclens) [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Oral rinse, topical skin
                          cleanser. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral rinses not intended
                          for ingestion and should be expectorated
                          after use. Topical preparations for skin
                          cleansing [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store above freezing at a
                          temperature not exceeding 25 C (77 F) unless
                          otherwise specified by manufacturer. Protect
                          from light. [PDR 1995] [USP DI 1995]
 MANUFACTURERS            Proctor and Gamble
 REFERENCES               Buckner RY, Kayrouz GA, Briner W. Reduction
                          of oral microbes by a single chlorhexidine
                          rinse. Compendium. 1994 Apr;15(4):512, 514,
                          516 passim; quiz 520.
 REFERENCES               Ciancio S. Expanded and future uses of
                          mouthrinses. J Am Dent Assoc. 1994 Aug;125
                          Suppl 2:29S-32S.
 REFERENCES               Fishcman SL. A clinician's perspective on
                          antimicrobal mouthrinses. J Am Dent Assoc.
                          1994 Aug;125 Suppl 2:20S-22S.
 REFERENCES               Modak S, Sampath L, Miller HS, Millman I.
                          Rapid inactivation of infectious pathogens by
                          chlorhexidine-coated gloves. Infect Control
                          Hosp Epidemiol. 1992 Aug;13(8):463-71.
 REFERENCES               Rowan C. Peridex decreases oral mucositis.
                          Oncol Nurs Forum. 1992 Jul;19(6):939.
 REFERENCES               Russell AD, Furr JR. Inactivation of human
                          immunodeficiency virus by chlorhexidine: the
                          possible role of neutralizers [letter]. J
                          Hosp Infect. 1991 Jul;18(3):249-51.
 REFERENCES               Persson RE, Truelove EL, LeResche L,
                          Robinovitch MR. Therapeutic effects of daily
                          or weekly chlorhexidine rinsing on oral
                          health of a geriatric population. Oral Surg
                          Oral Med Oral Pathol. 1991 Aug;72(2):184-91.
 REFERENCES               Montefiori DC, Robinson WE Jr, Modliszewski
                          A, Mitchell WM. Effective inactivation of
                          human immunodeficiency virus with
                          chlorhexidine antiseptics containing
                          detergents and alcohol. J Hosp Infect. 1990
                          Apr;15(3):279-82.
 REFERENCES               Bernstein D, Schiff G, Echler G, Prince A,
                          Feller M, Briner W. In vitro virucidal
                          effectiveness of a 0.12%-chlorhexidine
                          gluconate mouthrinse. J Dent Res. 1990
                          Mar;69(3):874-6.
 REFERENCES               Harbison MA, Hammer SM. Inactivation of human
                          immunodeficiency virus by Betadine products
                          and chlorhexidine. J Acquir Immune Defic
                          Syndr. 1989;2(1):16-20.
 ENTRY MONTH              9007
 LAST REVISION DATE       951031
 

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