      Document 0049
 DOCN  DRG0049
 UNIQUE IDENTIFIER        DRG-0198
 NAME OF SUBSTANCE        Benztropine mesylate [USAN 1996]
 REGISTRY NUMBER          132-17-2
 STANDARD CHEMICAL NAME   8-Azabicyclo(3.2.1)octane,
                          3-(diphenylmethoxy)-8-methyl-, endo,
                          methanesulfonate [USAN 1996]
 SYNONYMS                 Cogentin [USAN 1996]
 SYNONYMS                 Benzatropine methanesulfonate [CHEMLINE]
 SYNONYMS                 Benztropine mesilate [CHEMLINE]
 SYNONYMS                 Benzotropine mesylate [CHEMLINE]
 SYNONYMS                 Benzotropine methanesulfonate [CHEMLINE]
 SYNONYMS                 Cogentin methanesulfonate [CHEMLINE]
 SYNONYMS                 Tropine benzohydryl ether methanesulfonate
                          [CHEMLINE]
 SYNONYMS                 lalphaH,5alphaH-Tropane,
                          3alpha-(diphenylmethoxy)-, methanesulfonate
                          [CHEMLINE]
 SYNONYMS                 Cobrentin methanesulfonate [Merck Index 1989]
 SYNONYMS                 3-Diphenylmethoxytropane mesylate [CEHMLINE]
 SYNONYMS                 Cogentinol [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID ACTG 242
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: The anticholinergic activity
                          of benztropine is about equal to that of
                          atropine. The antihistaminic activity is
                          similar to that of pyrilamine maleate.
                          Benztropine does not produce as much central
                          stimulation as does trihexyphenidyl.
                          Benztropine effects are cumulative and may
                          not be evident until 2 or 3 days after start
                          of treatment. [AHFS Drug Information 1995]
 DISEASES STUDIED/TREATED As an active placebo to mimic the side
                          effects of study drugs [NIAID ACTG 242]
 CLASSIFICATION CODE      Anticholinergic [PDR 1995]
 CLASSIFICATION CODE      Antiparkinsonian [USAN 1996]
 OTHER MAJOR USES         Adjunct in therapy for parkinsonism; useful
                          in control of extrapyramidal disorders
                          (except tardive dyskinesia) due to
                          neuroleptic drugs [PDR 1995]
 SUBSTANCE INTERACTIONS   Interacts with antipsychotic drugs such as
                          phenothiazines or haloperidol, and with
                          tricyclic antidepressants. [PDR 1995]
 ADVERSE EFFECTS          Possible adverse effects include tachycardia,
                          paralytic ileus, constipation, vomiting,
                          nausea, dry mouth, toxic psychosis (including
                          confusion, memory impairment, and visual
                          hallucinations), nervousness, depression,
                          listlessness, numbness of fingers, blurred
                          vision, dilated pupils, urinary retention,
                          dysuria, allergic reaction, heat stroke,
                          hyperthermia, and fever. [PRD 1995]
 CONTRAINDICATIONS        Contraindicated in children under 3 years of
                          age and in patients with hypersensitivity to
                          the drug. Use with caution in older children.
                          [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Parasympatholytic [MeSH]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C21H25NO.CH4O3S [USAN
                          1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 403.54 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 143 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMP: C65.48%, H7.24%, N3.47%,
                          O15.86%, S7.95% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in water [Merck Index
                          1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pH 6 [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Crystalline white
                          powder [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 0.5, 1, and 2 mg tablets; 1
                          mg/ml sterile solution for injection. [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral; intravenous;
                          intramuscular. [PDR 1995]
 MANUFACTURERS            Merck and Company Incorporated
 REFERENCES               Holmes VF. Rapid progression of organic
                          delusional syndrome to dementia in AIDS. Int
                          Conf AIDS. 1989 Jun 4-9;5:499 (abstract no.
                          B.611).
 ENTRY MONTH              9403
 LAST REVISION DATE       951024
 

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