      Document 0119
 DOCN  DRG0119
 UNIQUE IDENTIFIER        DRG-0128
 NAME OF SUBSTANCE        Penicillin G [USAN 1996]
 REGISTRY NUMBER          61-33-6
 RELATED REGISTRY NUMBER  113-98-4
 STANDARD CHEMICAL NAME   Monopotassium
                          3,3,-dimethyl-7-oxo-6-(2-phenylacetamido)
                          -4-thia-1-azabicyclo (3.2.0)
                          heptane-2-carboxylate [PDR 1995]
 SYNONYMS                 Pfizerpen [PDR 1995]
 SYNONYMS                 Benzylpenicilin potassium [USAN 1996]
 PROTOCOL ID NUMBERS      NIAID ACTG 145
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Binds to serum proteins,
                          mainly albumin. Exerts a bactericidal action
                          against penicillin-susceptible microorganisms
                          during the stage of active multiplication.
                          Acts through the inhibition of biosynthesis
                          of cell wall mucopeptide, rendering the cell
                          wall osmotically unstable. Not active against
                          penicillinase-producing bacteria, including
                          many strains of staphylococci. About 15-30%
                          of oral doses are absorbed in fasting
                          individuals. Serum levels of 20 mcg/ml were
                          reported following IV infusions of penicillin
                          G potassium or sodium in subjects receiving 2
                          million units every 2 hours or 3 million
                          units every 3 hours. The drug is widely
                          distributed in the body with a volume of
                          distribution of 0.53-0.67 L/kg in normal
                          adults. The serum half-life is 0.4-0.5 hours
                          in adults with normal renal function.
                          Penicillin G and its metabolites are excreted
                          in the urine. [PDR 1995] [AHFS Drug
                          Information 1995]
 DISEASES STUDIED/TREATED Bactericidal action against
                          penicillin-susceptible microorganisms [PDR
                          1995]
 CLASSIFICATION CODE      Antibacterial [PDR 1995]
 OTHER MAJOR USES         Bactericidal action against
                          penicillin-susceptible microorganisms [PDR
                          1995]
 SUBSTANCE INTERACTIONS   Effects are diminished by concurrent
                          administration of aminoglycosides or
                          bacteriostatic antibiotics (e.g.,
                          erythromycin, tetracycline). Probenecid
                          coadministration produces higher and
                          prolonged serum levels of penicillin G.
                          Hyperkalemia may occur with the
                          administration of potassium sparing
                          diuretics. Food decreases the rate and extent
                          of oral absorption. [PDR 1995] [AHFS Drug
                          Information 1995]
 ADVERSE EFFECTS          Adverse effects include hypersensitivity
                          reactions including skin rashes, urticaria
                          and reactions resembling serum sickness
                          (e.g., chills, fever, edema, arthralgia, and
                          prostration). Severe and occasionally fatal
                          anaphylaxis has occurred. Rarely observed
                          adverse reactions include hemolytic anemia,
                          leucopenia, thrombocytopenia, nephropathy,
                          and neuropathy. Cardiac arrhythmias and
                          cardiac arrest may also occur. The
                          Jarisch-Herxheimer reaction has been reported
                          in patients treated for syphilis. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in patients with history of
                          previous hypersensitivity reaction to any
                          penicillin. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Penicillin G is a natural
                          penicillin produced by fermentation of
                          Penicillium chrysogenum in a medium
                          containing phenylacetic acid [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Penicillin G potassium and
                          sodium are frequently referred to as aqueous,
                          crystalline forms of penicillin G [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Colorless or white
                          crystal or a white crystalline powder
                          (potassium form) [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C16H17KN2O4S (potassium)
                          [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 372.49 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   STABILITY: Rapidly inactivated by acids,
                          alkali hydroxides and by oxidizing agents.
                          The reconstituted solution is stable for 7
                          days if refrigerated [USP DI 1995]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Very soluble in water [PDR 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: Moderately hygroscopic; pH
                          of the reconsitituted product is between
                          6.0-8.5 [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 1, 5, 10, and 20 million units
                          (potassium). [USP DI 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous. [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store dry powder below 86 F (30 C).
                          Solutions may be stored for seven days in a
                          refrigerator. [PDR 1995]
 MANUFACTURERS            Pfizer Incorporated, Roerig Division
 REFERENCES               Gordon SM, Eaton ME, George R, Larsen S,
                          Lukehart SA, Kuypers J, Marra CM, Thompson S.
                          The response of symptomatic neurosyphilis to
                          high-dose intravenous penicillin G in
                          patients with human immunodeficiency virus
                          infection [see comments]. N Engl J Med. 1994
                          Dec 1;331(22):1469-73.
 REFERENCES               Kastner RJ, Malone JL, Decker CF. Syphilitic
                          osteitis in a patient with secondary syphilis
                          and concurrent human immunodeficiency virus
                          infection. Clin Infect Dis. 1994
                          Feb;18(2):250-2.
 REFERENCES               Ishii N, Ichiyama S, Nakajima H, Ito A.
                          Sexually transmitted diseases in a HIV
                          infected patient. J Dermatol. 1993
                          Mar;20(3):171-4.
 REFERENCES               Deschenes J, Seamone CD, Baines MG. Acquired
                          ocular syphilis: diagnosis and treatment. Ann
                          Ophthalmol. 1992 Apr;24(4):134-8.
 REFERENCES               Gleich LL, Linstrom CJ, Kimmelman CP.
                          Otosyphilis: a diagnostic and therapeutic
                          dilemma [see comments]. Laryngoscope. 1992
                          Nov;102(11):1255-9.
 REFERENCES               Keeley DJ, Nkrumah FK, Kapuyanyika C.
                          Randomized trial of sulfamethoxazole +
                          trimethoprim versus procaine penicillin for
                          the outpatient treatment of childhood
                          pneumonia in Zimbabwe. Bull World Health
                          Organ. 1990;68(2):185-92.
 REFERENCES               Kinghorn GR, Spencer RC, Smith TK, Wooley PD,
                          Patel R, Robinson AJ. Comparative study of
                          cefuroxime axetil and procaine penicillin in
                          the treatment of uncomplicated gonorrhoea.
                          Int J STD AIDS. 1990 Jul;(4):285-7.
 REFERENCES               Manganoni AM, Graifemberghi S, Facchetti F,
                          Gavazzoni R, De Panfilis G. Effectiveness of
                          penicillin G benzathine for primary and
                          secondary syphilis in HIV infection [letter].
                          L AM Acad Dermatol. 1990 Dec;23(6 Pt
                          1):1185-6.
 REFERENCES               McLeish WM, Pulido JS, Holland S, Culbertson
                          WW, Winward K. The ocular manifestations of
                          syphilis in the human immunodeficiency virus
                          type 1-infected host. Opthalmology. 1990
                          Feb;97(2):196-203.
 REFERENCES               Hook EW 3d. Treatment of syphilis: current
                          recommendations, alternatives, and continuing
                          problems. Rev Infect Dis. 1989 Sep-Oct;11
                          Suppl 6:S1511-7.
 ENTRY MONTH              9111
 LAST REVISION DATE       951213
 

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