      Document 0236
 DOCN  DRG0236
 UNIQUE IDENTIFIER        DRG-0011
 NAME OF SUBSTANCE        Clindamycin [USAN 1995]
 REGISTRY NUMBER          18323-44-9
 STANDARD CHEMICAL NAME   L-threo-alpha-D-galacto-Octopyranoside,
                          methyl 7-chloro-
                          6,7,8-trideoxy-6-(((1-methyl-4-propyl-2-pyrro-
                          lidinyl) carbonyl) amino)-1-thio-,
                          (2S-trans)- [USAN 1995]
 SYNONYMS                 Cleocin [USAN 1995]
 SYNONYMS                 Dalacin C [Merck Index 1989]
 SYNONYMS                 Sobelin [Merck Index 1989]
 SYNONYMS                 7(S)-Chloro-7-deoxylincomycin [USAN 1995]
 SYNONYMS                 7-Deoxy-7(S)-chlorolincomycin [Merck Index
                          1989]
 SYNONYMS                 Dalactine (hydrochloride monohydrate) [Merck
                          Index 1983]
 SYNONYMS                 U-21251 [Merck Index 1989]
 SYNONYMS                 Antirobe [Merck Index 1989]
 SYNONYMS                 Klimicin [Merck Index 1989]
 SYNONYMS                 Methyl 7-chloro-6,7,8-trideoxy-6-
                          (1-methyl-trans-4-propy1-L-2-pyrrolidinecarbo-
                          xamido)-1-thio-L-threo-alpha-D-galacto-octopy-
                          ranoside [USAN 1995]
 PROTOCOL ID NUMBERS      NIAID ACTG 044
 PROTOCOL ID NUMBERS      NIAID ACTG 077 Pilot
 PROTOCOL ID NUMBERS      NIAID ACTG 108
 PROTOCOL ID NUMBERS      NIAID CPCRA 001
 PROTOCOL ID NUMBERS      FDA 021A
 SECONDARY SOURCE ID      U-21,251 [USAN 1995]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Clindamycin hydrochloride is
                          rapidly absorbed after oral administration,
                          reaching a mean peak serum  level of 2.50
                          mcg/ml in 45 minutes, with  a reduction
                          thereafter to 1.51 and 0.70 mcg/ml in 3 and 6
                          hours respectively. Clindamycin is widely
                          distributed  in body fluids and tissue
                          (including bone); but no significant levels
                          are attained in cerebrospinal fluid.
                          Approximately 10% of the bio-activity is
                          excreted in the urine and 3.6% in the feces;
                          the remainder is excreted as bio-inactive
                          metabolites. Clostridia toxin(s) appear to be
                          the primary cause of clindamycin-associated
                          colitis. Cholestyramine and colestipol resins
                          have been shown to bind the toxin in vitro.
                          [PDR 1995]
 DISEASES STUDIED/TREATED Pneumocystis carinii pneumonia (PCP) and
                          toxoplasmosis [PDR 1993; AHFS 1995]
 CLASSIFICATION CODE      Antibacterial [PDR 1995]
 OTHER MAJOR USES         Treatment of serious infections by
                          susceptible anaerobic bacteria. Used against
                          infections due to streptococci, pneumococci,
                          and staphylococci, should be reserved for
                          penicillin-allergic patients [PDR 1995]
 SUBSTANCE INTERACTIONS   Antagonism has been demonstrated between
                          clindamycin and erythromycin. Clindamycin has
                          been shown to have neuromuscular blocking
                          properties that may enhance the action of
                          other neuromuscular blocking agents.
                          Therefore it should be used with caution in
                          patients receiving  such agents. [PDR 1995]
                          The following drugs are physically
                          incompatible with clindamycin phosphate(IV
                          preparation): ampicillin sodium, phenytoin
                          sodium, barbiturates, aminophylline, calcium
                          gluconate, and magnesium sulfate. [PDR 1995]
                          Combination therapy with clindamycin and
                          quinine has been reported as beneficial in
                          the treatment of cryptosporidiosis;
                          clindamycin with pyrimethamine has been used
                          against cerebral and/or ocular toxoplasmosis
                          in immunocompromised patients. [AHFS Drug
                          Information 1995]
 ADVERSE EFFECTS          Has been associated with severe colitis
                          (usually characterized by severe persistent
                          diarrhea and severe abdominal cramps and may
                          be associated with the passage of blood and
                          mucus), which may end fatally; also may cause
                          esophagitis, nausea, vomiting, rashes,
                          jaundice and liver function abnormalities,
                          renal dysfunction, transient neutropenia
                          (leukopenia) and eosinophilia, and
                          agranulocytosis and thrombocytopenia. LD-50
                          (mice: 361 mg/kg; 245 mg/kg (IV); LD-50
                          (rats): 2,618 mg/kg (oral). [PDR 1995]
 CONTRAINDICATIONS        Should not be used in patients with a history
                          of hypersensitivity to preparations
                          containing clindamycin or lincomycin. [PDR
                          1995] Use of clindamycin may cause overgrowth
                          of nonsusceptible organisms, particularly
                          fungi. Patients with preexisting candida
                          infection should receive concomitant
                          antifungal treatment. Clindamycin should be
                          used with caution in patients with a history
                          of GI disease, and with severe renal and/or
                          hepatic impairment. [AHFS Drug Information
                          1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: A lincomycin derivative;
                          Lincosamine antibiotic [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C18H33C1N2O5S [USAN 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 424.99 [USAN 1995]
 CHEMICAL/PHYSICAL DATA   PERCENT ELEMENTAL COMPOSITION: C50.87%;
                          H7.83%; Cl8.34%; N6.59%; O18.82%; S7.54%
                          [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 141-143 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Water, pyridine, ethanol,
                          dimethylformamide [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Yellow amorphous solid;
                          white crystals from ethanol-ethyl acetate
                          [Merck Index 1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Vial of sterile solution of
                          clindamycin phosphate, equivalant to 150 mg
                          clindamycin/ml; clindamycin hydrochloride
                          (75, 150, and 300 mg capsules). [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Clindamycin palmitate
                          hydrochloride granules for oral (15 mg/ml)
                          solution; topical solution (10 mg/ml). [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Topical gel, lotion, solution
                          and vaginal cream [AHFS Drug Information
                          1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Clindamycin hydrochloride
                          and clindamycin palmitate hydrochloride are
                          administered PO; the phosphate is
                          administered by IM injection or IV infusion.
                          [AHFS Drug Information 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Solution (clindamycin phosphate, IV)
                          and capsules and granules: Store at
                          controlled room temperature, 15-30 C (59-86
                          F). [PDR 1995]
 MANUFACTURERS            Upjohn
 REFERENCES               Caumes E, Bocquet H, Guermonprez G, Rogeaux
                          O, Bricaire F, Katlama C, Gentilini M.
                          Adverse cutaneous reactions to
                          pyrimethamine/sulfadiazine and
                          pyrimethamine/clindamycin in patients with
                          AIDS and toxoplasmic encephalitis. Clin
                          Infect Dis. 1995 Sep;21(3):656-8.
 REFERENCES               Behbahani R, Moshfeghi M, Baxter JD.
                          Therapeutic approaches for AIDS-related
                          toxoplasmosis. Ann Pharmacother. 1995
                          Jul-Aug;29(7-8):760-8.
 REFERENCES               Winstanley P. Drug treatment of toxoplasmic
                          encephalitis in acquired immunodeficiency
                          syndrome. Postgrad Med J. 1995
                          Jul;71(837):404-8.
 REFERENCES               Rabaud C, May T, Amiel C, Katlama C, Leport
                          C, Ambroise-Thomas P, Canton P. Extracerebral
                          toxoplasmosis in patients infected with HIV.
                          A French National Survey. Medicine
                          (Baltimore). 1994 Nov;73(6):306-14.
 REFERENCES               Black JR, Feinberg J, Murphy RL, Fass RJ,
                          Finkelstein D, Akil B, Safrin S, Carey JT,
                          Stansell J, Plouffe JF, et al. Clindamycin
                          and promaquine therapy for mild-to-moderate
                          episodes of Pneumocystis carinii pneumonia in
                          patients with AIDS: AIDS Clinical Trials
                          Group 044. Clin Infect Dis. 1994
                          Jun;18(6):905-13.
 REFERENCES               Toma E, Fournier S, Dumont M, Bolduc P,
                          Deschamps H. Clindamycin/primaquine versus
                          trimethoprim-sulfamethoxazole as primary
                          therapy for Pneumocystis carinii pneumonia in
                          AIDS: a randomized, double-blind pilot trial.
                          Clin Infect Dis. 1993 Aug;17(2):178-84.
 REFERENCES               Petit N, Bonnet E, Gallais H.  Pneumocystis
                          carinii pneumonia successfully treated by a
                          clindamycin-dapsone combination in a
                          HIV-infected patient. Int Conf AIDS. 1993 Jun
                          6-11;9(1):379 (abstract no. PO-B10-1463).
 REFERENCES               Toma E, Tremblay C, Passerini L.
                          Clindamycin/primaquine for severe
                          Pneumocystis carinii pneumonia (PCP). Int
                          Conf AIDS. 1993 Jun;9(1):62 (abstract no.
                          WS-B19-6).
 REFERENCES               Gatti G, Flaherty J, Bubp J, White J, Borin
                          M, Gambertoglio J. Comparative study of
                          bioavailabilities and pharmacokinetics of
                          clindamycin in healthy volunteers and
                          patients with AIDS. Antimicrob Agents
                          Chemother. 1993 May;37(5):1137-43.
 ENTRY MONTH              8906
 LAST REVISION DATE       960501
 

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