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Antibiotics and Antibacterials, General B. Sulfamethoxydiazine (Sulfameter, Sulla) IX. TOXICITY AND SIDE EFFECTS: C. Sulfadimethoxine (Madribon) A. Fever D. Sulphormethoxine-Very long-acting; thera- B. Rash, urticaria peutic blood levels for 1 week. C. Cyanosis, methemoglobinemia D. Nausea, vomiting, diarrhea V. POORLY ABSORBED SULFONAMIDES: E. Hepatitis, jaundice for local use in the intestinal tract only. F. Hematuria, albuminuria, crystalluria, toxic A. Succinylsulfathiazole (Sulfasuxidine): nephritis. 1. Dosage-3.0 Gm q 4 h p.o. G. Headache, mental depression, psychosis, 2. Maximum effect usually not achieved un- peripheral neuritis. til 7th day of therapy. H. Leukopenia, agranulocytosis, purpura, aplas- B. Phthalylsulfathiazole (Sulfathalidine): tic anemia, hypoprothrombinemia, hemolytic ane- 1. Dosage-1.5 Gmq4hp.o. mia. 2. Double this dosage in the presence of I. Severe hypersensitivity reactions - anaphy- diarrhea. laxis, periarteritis nodosa and other collagen dis- 3. Effect produced in 5-7 days. eases, Stevens-Johnson syndrome. C. Para-nitrosulfathiazole (Nisulfazole): Used X. only for intrarectal instillation in treatment of PRECAUTIONS: proctitis or non-specific colitis. A. Keep careful record of urine output - try to maintain output of at least 1200-1500 ml/24 VI. TOPICAL SULFONAMIDES: hrs. B. Alkalinization of urine-sodium bicarbonate A. Mafenide (Sulfamylon): Used on skin as (12-15 Gm/day) may be used for this purpose 10% cream. Unlike other sulfonamides, effective when full systemic doses of sulfonamides are used, in presence of pus and necrotic tissue and does not when there is difficulty in being sure of adequate sensitize readily when used topically. Of value in fluid intake and output, and when such adjunctive prevention and therapy of burn infection due to therapy is not contraindicated. Pseudomonas. C. Check fresh urine specimens for RBC's, B. Ophthalmic preparations: Sodium sulfaceta- albumin and sulfa crystals. mide (Sulamyd) and sulfisoxazole diolamine are the only products suitable for topical use in the eye; D. Weekly blood counts. they are available as solutions (30%) and oint- ments (10%). ANTIBIOTICS AND ANTIBACTERIALS, C. Vaginal preparations: These include sulfi- GENERAL soxazole and triple sulfonamide combinations SYDNEY M. FINEGOLD, M.D., AND ALVIN DAVIS, M.D. made up as creams or tablets. They are used in nonspecific vaginitis and cervicitis. I. PENICILLIN G (Benzylpenicillin): 1. Spectrum and Uses: Highly active against VII. SULFAPYRIDINES: Gram-positive cocci other than beta lactamase- A. Sulfapyridine: Too toxic for general use, but producing staphylococci; Gram-negative cocci; best drug available for dermatitis Gram-positive bacilli; fusiforms and some other herpetiformis. Gram-negative anaerobic bacilli; and (in high dos- B. Salicylazosulfapyridine (Azulfidine): Ofvalue age) Proteus mirabilis. Oral penicillin G is useful in ulcerative colitis, particularly in preventing re- in many urinary tract infections due to E. coli and lapse. Value in regional enteritis less well estab- P. mirabilis. lished. 2. Types of Preparations, Route of Administra- tion and Dosage: VIII. SULFONAMIDES IN GENERAL: a. Crystalline aqueous penicillin G: A. Desired peak blood level-8-15 mg/100 ml (1) Peak blood levels - generally 1-2 (except poorly absorbed compounds). units/ml for each one million units intra- B. Mode of action-bacteriostatic. muscular/day. 364 NOVEMBER 1969 * II I* 5 (2) Probenecid (Benemid) 0.5 Gm q 6 h million units supplies 975 mg (25 mEq) of will usually raise levels 11/2 to 2 times. potassium. b. Procaine penicillin G suspended in oil or c. Allergic reactions ranging from minor skin water: reactions to anaphylactic shock and death occur. (1) With single intramuscular dose of The best prophylaxis is a careful history com- 300,000 to 600,000 units, peak serum levels bined with discriminate use of this drug. The are usually 0.75 unit/ml or less and serum usual skin tests and conjunctival tests with peni- concentrations of at least 0.04 unit/ml (ad- cillin G are unreliable. Use of penicillinase equate for highly sensitive organisms such as (Neutrapen) for treatment of penicillin allergy pneumococci and Group A beta-hemolytic should be condemned because there is no proof streptococci) persist for from 20 to 24 hours. of its effectiveness and because it may actually Frequency of administration depends on increase the hazard. preparation and dosage used. d. Hemolytic anemia, neutropenia. (2) Increasing dosage primarily prolongs 4. Mode of Action: Bactericidal. duration of blood level rather than raising peak level; the usual daily maximum should II. ALPHA-PHEENOXY-PENICILLINS:* be 1.2 million units. A. Phenoxymethyl penicillin (penicillin V, Pen- c. Procaine penicillin G in sesame oil and Vee, V-Cillin): This compound is better absorbed 2 % aluminum monostearate: on oral administration than penicillin G and is A single 200,000 unit dose behaves much more acid stable. The antibiotic spectrum of the like procaine penicillin, but 600,000 unit two agents is similar. Both are susceptible to doses result in levels of 0.03 units/ml or staphylococcal beta lactamase. Most infections higher for more than 90 hours. which will respond to oral therapy can be treated d. Benzathine penicillin G (dibenzylethylene- with 250-500 mg q 8 h. Infections such as osteo- diamine dipenicillin G, DBED, Bicillin): myelitis or subacute bacterial endocarditis (when they can be treated orally) require >50-1,000 mg (1) Very insoluble salt. 300,000 unit dose useful for 0.03 q 4-6 h. Penicillin V is not ordinarily intramuscularly gives levels above unit/ therapy of urinary tract infections. ml for over 5 days with peak levels above 0.15 unit/ml uncommon at any time. Doses B. Phenoxyethyl penicillin (phenethicillin, Syn- of 600,000 units and 1,200,000 units intra- cillin, Maxipen, Chemipen, Broxil, Dargil, Alpen): muscularly result in prolongation of levels This compound is very similar to penicillin V. to 12 and 28 days, respectively. (The oral form is poorly absorbed and should not be III. BETA LACTAMASE-RESISTANT PEN- used.) ICILLINS: * (2) Chiefly useful as a prophylactic agent A. Methicillin (Staphcillin, Celbenin, Dimocil- and in the treatment of early syphilis. lin): (3) Painful on injection. Allergic reac- 1. Spectrum and Uses: Active vs staphylo- tions, when they occur, may be severe and cocci resistant to penicillin G (beta lactamase- prolonged. producers). Distinctly inferior to penicillin G e. Oral penicillin G: vs. other organisms. For urinary tract infections, 400,000 units 2. Routes of Administration and Dosage q6h. a. Intramuscularly 1 Gm q 3-6 h. 3. Toxicity, Side Effects, and Precautions: b. Intravenously 1-4 Gm q 4-12 h (12 Gm a. Central nervous system toxicity may occur or more/day in severe infections). It is best when unusually high doses are used and/or im- given in 50-100 ml over a 30 minute period paired renal function exists. q 4-6 h. (The drug is relatively unstable, par- b. The amount of potassium injected must be ticularly at acid pH's. Make up just before considered when very large doses of crystalline use.) aqueous potassium penicillin are used in the These agents exhibit cross-allergenicity with penicillin G. Probe- presence of impaired renal function. Each 15 necid blocks excretion of all penicillins. All are bactericidal. CALIFORNIA MEDICINE 365 The Western Journal of Medicine 3. Toxicity, Side Effects and Precautions 4. Miscellaneous: Preferred over oral oxacil- a. Sensitivity reactions, as with peni- lin because of better absorption and thus higher cillin G. and more prolonged blood levels. Not suitable b. Renal damage (hypersensitivity?) for treatment of meningitis. fever, albuminuria, pyuria, hematuria, oligu- D. Dicloxacillin (Dynapen, Veracillin): ria to anuria, nitrogen retention, edema, and 1. Spectrum and Uses: Same as for oxacillin. eosinophilia may occur. This is apparently 2. Routes of Administration and Dosage: reversible, but complete recovery may take Available only for oral use. Dosage is 0.25-1.0 months. Gmq6h. c. Bone marrow depression (neutropenia) 3. Toxicity, Side Effects and Precautions: occurs occasionally. Same as for cloxacillin. d. Hemolytic anemia. 4. Miscellaneous: Peak serum levels approx- e. Each 4 Gm of drug supplies 230 mg imately twice those with cloxacillin at compar- (10 mEq) of sodium (drug supplied as so- able dosage. dium salt). E. Nafcillin (Unipen): 4. Miscellaneous. Moderately resistant staph- 1. Spectrum and Uses: Similar to oxacillin. ylococci have been isolated rarely. When other agents are to be administred simultaneously, 2. Routes of Administration and Dosage: they should be given separately rather than be- a. Oral-absorption not reliable. ing mixed with the methicillin. b. Intramuscularly-0.5 Gm q 4-6 h. c. Intravenously-0.5-1.0 Gm q 4 h. May B. Oxacillin (Prostaphlin, Resistopen): be administered by method described for 1. Spectrum and Uses: Similar to methicillin, methicillin. but somewhat more active on a weight basis. 3. Toxicity, Side Effects and Precautions: As There is greater protein binding with this agent. with oxacillin. 2. Routes of Administration and Dosage: 4. Miscellaneous - Significant biliary excre- a. Oral-not recommended (cloxacillin or tion. dicloxacillin are preferred oral agents. b. Intramuscularly-0.5-1.0 Gm q 4 h. IV. BROAD-SPECTRUM PENICILLINS:* c. Intravenously-0.5 Gm or more q 4 h. A. Ampicillin (Penbritin, Polycillin): May be administered by method described for methicillin. 1. Spectrum and Uses: a. Active vs most strains of Proteus mira- 3. Toxicity, Side Effects and Precautions: bilis and occasional strains of other Proteus a. Sensitivity reactions as with penicillin G. species. Active vs most strains of H. influ- b. Neutropenia (rare). enzae, Salmonella and Shigella, and about c. Reversible SGOT elevations are occa- 50% of E. coli strains. sionally noted. b. Similar to penicillin G in its activity vs 4. Miscellaneous - cross-resistance with Gram-positive cocci and vs anaerobes except methicillin. Greater amount of biliary excre- that it is more effective vs many strains of tion than with methicillin. Not suitable for treat- enterococcus.
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