Cephalothin (Keflin)

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Name: Cephalothin (Keflin)

Class: First Gen. Cephalosporin

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: IV. IM rarely used due to pain.

Distribution: Poor CSF.

Metab.:

Excretion, t½:

Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, renal damage (worse if comb. w/aminoglycs.)

Utility: Usu not DOC. Serious Klebsiella infects., strep/staph infects, some penicillinase-producing bacteria.

Special Features: Narrow spectrum. Greater gram - activity than pen. G. More gram+ activity than gram - activity. Less susceptible to b-lactamase than most penicillins.

 

Probenecid

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Name: Probenecid

Class:

Mech.: Interferes w/renal excretion of drugs that undergo tubular secretion. Inhib. glucuronide conjugation of other drugs.

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility:

Special Features: Decreases renal excretion of methotrexate — possible toxicity. Decreases renal excretion of penicillin.

 

Sulbactam

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Name: Sulbactam

Class: b-Lactamase Inhibitor

Mech.: inhibits some b-lactamases

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Combined with ampicillin (Unasyn-sulbactam) to increase efficacy against penicillinase-producing bacteria (i.e., staph).

Special Features:

 

Clavulanic acid

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Name: Clavulanic acid

Class: b-Lactamase Inhibitor

Mech.: inhibits some b-lactamases

Absorption:

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Combined with amoxicillin (Augmentin) to increase efficacy against penicillinase-producing bacteria (i.e., staph.)

Special Features:

 

Ticarcillin (Ticar)

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Name: Ticarcillin (Ticar)

Class: Penicillin (Extended spectrum)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: IM, IV.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), superinfection., coagulation disorders.

Utility: Gram -. Effective against Pseudomonas, Proteus mirabilus, often used w/aminoglyc.

Special Features: Narrow spectrum. Resistance develops quickly.

 

Minocyclin (Minocin)

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Name: Minocyclin (Minocin)

Class: Tetracycline

Mech.: Active uptake into bacteria ®inhib protein synth by binding to 30S ribosome. Bacteriostatic

Absorption: Good oral absorption. Impaired by divalent cations. IM painful. IV may cause thrombophlebitis. Never intrathecal.

Distribution: Good CSF. Conc. in liver ® enterohepatic circ. Penetrates most tissues and fluids. Also enters tears and saliva. Crosses placenta.

Metab.: Liver, but not critical.

Excretion, t½: bile; doesn’t require renal excretion

Toxicity/S.E.s: Vestibular toxicity; GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown discoloration of teeth; slowing of bone growth; phototoxicity; thrombophlebitis; hematopoetic changes; rare hypersens. rxns.

Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for acne, prophylaxis for Travelers’ diarrhea.

Special Features: Broad spectrum. Decreased effect of oral contraceptives.

 

Amoxicillin (Amoxil)

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Name: Amoxicillin (Amoxil)

Class: Penicillin (Aminopenicillin)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Acid stable. Good oral (better than ampicillin).

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: diarrhea (less than ampicillin), hypersensitivity (1-10%), superinfection.

Utility: More effective against gram -s (esp. Proteus, H. influenzae, E. coli, P. mirabilis). Less active than Pen. G against gram+ cocci.

Special Features: Broad spectrum.

 

Ampicillin (Omnipen, Polycillin)

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Name: Ampicillin (Omnipen, Polycillin)

Class: Penicillin (Aminopenicillin)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Acid stable. Good oral, but food interferes. IM, IV.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: diarrhea, non-allergy skin rash, hypersensitivity (1-10%), superinfection.

Utility: More effective against gram -s (esp. Proteus, H. influenzae, E. coli, P. mirabilis). Less active than Pen. G against gram+ cocci.

Special Features: Broad spectrum.

 

Oxacillin (Bactocill)

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Name: Oxacillin (Bactocill)

Class: Penicillin (Penicillinase-resistant)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Acid stable. Absorbed orally. IM, IV.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), superinfection.

Utility: Penicillinase-producing staph. infections. Mild infections.

Special Features: Narrow spectrum.

 

Methicillin (Staphcillin)

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Name: Methicillin (Staphcillin)

Class: Penicillin (Penicillinase-resistant)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Usu. IV for seious infections. IM.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), superinfection.

Utility: Penicillinase-producing staph. infections. Gram +.

Special Features: Narrow spectrum.

 

Nafcillin (Nafcil)

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Name: Nafcillin (Nafcil)

Class: Penicillin (Penicillinase-resistant)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Poor oral. Usu. IV for seious infections. IM.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), superinfection.

Utility: Penicillinase-producing staph. infections. Gram +.

Special Features: Narrow spectrum. Prob. most effective penicillinase-resist.

 

Penicillin V

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Name: Penicillin V

Class: Penicillin (Penicillin G-related)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Acid stable ® good oral absortption.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: : hypersensitivity (1-10%), superinfection.

Utility: Mild to moderate infections only: Many gram +, anaerobes, and a few gram -. Most staph. and gram - resistant. Same spectrum as Pen. G, but less active.

Special Features: Narrow spectrum.

 

Penicillin G

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Name: Penicillin G

Class: Penicillin (Penicillin G-related)

Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal.

Absorption: Erratic (30%). Usu. not used orally. I.M or I.V. Prolonged effect with repository preparations (procaine, benzathine (longest)) deep IM.

Distribution: Widely distributed, little CSF unless meninges inflamed.

Metab.:

Excretion, t½: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile.

Toxicity/S.E.s: hypersensitivity (1-10%), painful injection, epilepsy, superinfection.

Utility: Many gram +, anaerobes, and a few gram -. Most staph. and gram - resistant. Prophylactic use (rheumatic fever, strep. infections).

Special Features: Narrow spectrum.

 

Doxycycline (Vibramycin)

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Name: Doxycycline (Vibramycin)

Class: Tetracycline

Mech.: Active uptake into bacteria ®inhib protein synth by binding to 30S ribosome. Bacteriostatic

Absorption: Good oral absorption. Impaired by divalent cations. IM painful. IV may cause thrombophlebitis. Never intrathecal.

Distribution: Good CSF. Conc. in liver ® enterohepatic circ. Penetrates most tissues and fluids. Crosses placenta.

Metab.:

Excretion, t½: bile; doesn’t require renal excretion

Toxicity/S.E.s: GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown discoloration of teeth; slowing of bone growth; phototoxicity (more than others); thrombophlebitis; hematopoetic changes; rare hypersens. rxns.

Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for acne, prophylaxis for Travelers’ diarrhea.

Special Features: Broad spectrum. Decreased effect of oral contraceptives.

 

Tetracycline (Achromycin V)

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Name: Tetracycline (Achromycin V)

Class: Tetracycline

Mech.: Active uptake into bacteria ®inhib protein synth by binding to 30S ribosome. Bacteriostatic

Absorption: Oral adequate, but incomplete. Impaired by divalent cations. IM painful. IV may cause thrombophlebitis. Never intrathecal.

Distribution: Good CSF. Conc. in liver ® enterohepatic circ. Penetrates most tissues and fluids. Crosses placenta.

Metab.:

Excretion, t½: filtration (1°), bile

Toxicity/S.E.s: GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown discoloration of teeth; slowing of bone growth; phototoxicity; thrombophlebitis; hematopoetic changes; rare hypersens. rxns.

Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for acne, prophylaxis for Travelers’ diarrhea.

Special Features: Broad spectrum. Decreased effect of oral contraceptives.

 

Chloramphenicol (Chloromycetin)

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Name: Chloramphenicol (Chloromycetin)

Class:

Mech.: Bacteriostatic. Inhib protein synth by binding to 50S subunit.

Absorption: Rapid oral absorption

Distribution: Body fluids, good CSF. Crosses placenta. Milk.

Metab.: Liver (glucuronyl transferase)

Excretion, t½: Urine (filtration, secretion), 1.5-3.5 hr.

Toxicity/S.E.s: Bone marrow depression (anemia, leukopenia, thrombocytopenia, prob. due to inhib. of mitoch. protein), aplastic anemia (allergic/idiosync, rare, irreversible, often fatal), Gray Baby Syndrome (neonate overdose due to reduced ability to conjuate CA and secrete metabolites), superinfection (S. aureus, Pseudomonas, fungi, can be life threatening).

Utility: DOC for severe Bacteroides infects (esp. CNS), backup for memingitis, rickettsial infects, brucellosis.

Special Features: Never use if safer antibiotic avail. Never use for mild infects.

 

Trimethoprim-Sulfamethoxazole (Bactrim, Septra)

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Name: Trimethoprim-Sulfamethoxazole (Bactrim, Septra)

Class:

Mech.: Acts on two sequential steps in synth of folic acid. PABA competitive inhib, dihydrofolate reductase inhib. Bacteriostatic.

Absorption: Oral, IV

Distribution:

Metab.:

Excretion, t½:

Toxicity/S.E.s: Megaloblastic anemia, leukopenia, granulocytopenia (prevented by admin. of folic acid)

Utility: Uncomp. UTIs, otitis media, acute exacerbations of chronic bronchitis, various pneumonias. DOC for Travelers’ diarrhea, P. carinii pneumonia, Shigella enteritis, systemic Salmonella infects, prostatitis.

Special Features: Trimethoprim = highly selective inhib. of bacterial dihydrofolate reductase.

 

Sulfacetamide sodium (Sulamyd Sodium)

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Name: Sulfacetamide sodium (Sulamyd Sodium)

Class: Sulfonamide

Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid ® inhib. of folic acid.

Absorption:

Distribution: Ophthalmic application. Penetrates into ocular fluids at high conc.

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Ophthalmic infections

Special Features: High aqueous concentrations are not irritating.

 

Silver Sulfadiazine (Silvadene)

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Name: Silver Sulfadiazine (Silvadene)

Class: Sulfonamide

Mech.: Releases silver ® toxicity for bacteria and fungi.

Absorption:

Distribution: Topical

Metab.:

Excretion, t½:

Toxicity/S.E.s:

Utility: Used topically to reduce infection of burns, but not to treat established infections.

Special Features:

 

Sulfasalazine (Azulfidine)

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Name: Sulfasalazine (Azulfidine)

Class: Sulfonamide

Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid ® inhib. of folic acid.

Absorption: Poorly absorbed in GI tract.

Distribution: GI tract

Metab.: Hydrolized to active form by intest. bacteria.

Excretion, t½: feces

Toxicity/S.E.s: Interferes w/normal flora ® ¯ vit. K synth.

Utility: Active in bowel lumen. Used prior to surgery to reduce microbe population. Treat inflammatory bowel disease, rheumatoid arthritis

Special Features: Broken down in intestines to liberate 5-aminosalicylate (anti-inflammatory).

 

Sulfadiazine

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Name: Sulfadiazine

Class: Sulfonamide

Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid ® inhib. of folic acid. Bacteriostatic.

Absorption: Rapidly absorbed in GI tract. Parenteral.

Distribution: Widely distrib; good CSF. Crosses placenta.

Metab.: Acetylated in liver

Excretion, t½: Renal filtration, secretion

Toxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT disturbances— deposition of crystalline aggregates; hematopoetic disorders—dyscrasias

Utility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, suppressing recurring UTIs, rheumatic fever)

Special Features: Spectrum—gram +, gram -.

 

Sulfamethoxazole (Gantanol)

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Name: Sulfamethoxazole (Gantanol)

Class: Sulfonamide

Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid ® inhib. of folic acid. Bacteriostatic.

Absorption: Rapidly absorbed in GI tract (slower than isoxazole). Parenteral.

Distribution: Widely distrib; limited CSF. Crosses placenta.

Metab.: Acetylated in liver

Excretion, t½: Renal filtration, secretion

Toxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT disturbances— deposition of crystalline aggregates; hematopoetic disorders—dyscrasias

Utility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, suppressing recurring UTIs, rheumatic fever)

Special Features: Spectrum—gram +, gram -.

 

Sulfisoxazole (Gantrisin)

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Name: Sulfisoxazole (Gantrisin)

Class: Sulfonamide

Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid ® inhib. of folic acid. Bacteriostatic.

Absorption: Rapidly absorbed in GI tract. Parenteral.

Distribution: Widely distrib; CSF. Crosses placenta.

Metab.: Acetylated in liver

Excretion, t½: Renal filtration, secretion

Toxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT disturbances— deposition of crystalline aggregates; hematopoetic disorders—dyscrasias

Utility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, suppressing recurring UTIs, rheumatic fever)

Special Features: Spectrum—gram +, gram -. Less renal toxicity than other sulfas. Protoype.