Pharma antimicrob cards

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Pharma antimicrob cards

  1. 1. Name: Sulfisoxazole (Gantrisin) Name: Sulfamethoxazole (Gantanol)Class: Sulfonamide Class: SulfonamideMech.: Comp. inhib. of PABA incorp. into dihydropteric acid → inhib. of folic acid. Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid → inhib. of folic Bacteriostatic. acid. Bacteriostatic.Absorption: Rapidly absorbed in GI tract. Parenteral. Absorption: Rapidly absorbed in GI tract (slower than isoxazole). Parenteral.Distribution: Widely distrib; CSF. Crosses placenta. Distribution: Widely distrib; limited CSF. Crosses placenta.Metab.: Acetylated in liver Metab.: Acetylated in liverExcretion, t_: Renal filtration, secretion Excretion, t_: Renal filtration, secretionToxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT disturbances— Toxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT deposition of crystalline aggregates; hematopoetic disturbances— deposition of crystalline aggregates; disorders—dyscrasias hematopoetic disorders—dyscrasiasUtility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, Utility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, suppressing recurring UTIs, rheumatic fever) suppressing recurring UTIs, rheumatic fever)Special Features: Spectrum—gram +, gram -. Less renal toxicity than other Special Features: Spectrum—gram +, gram -. sulfas. Protoype.Name: Sulfadiazine Name: Sulfasalazine (Azulfidine)Class: Sulfonamide Class: SulfonamideMech.: Comp. inhib. of PABA incorp. into dihydropteric acid → inhib. of folic acid. Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid → inhib. of folic Bacteriostatic. acid.Absorption: Rapidly absorbed in GI tract. Parenteral. Absorption: Poorly absorbed in GI tract.Distribution: Widely distrib; good CSF. Crosses placenta. Distribution: GI tractMetab.: Acetylated in liver Metab.: Hydrolized to active form by intest. bacteria.Excretion, t_: Renal filtration, secretion Excretion, t_: fecesToxicity/S.E.s: Hypersensitivity—fever, rash, photosensitivity; UT disturbances— Toxicity/S.E.s: Interferes w/normal flora → ↓ vit. K synth. deposition of crystalline aggregates; hematopoetic disorders—dyscrasias Utility: Active in bowel lumen. Used prior to surgery to reduce microbe population. Treat inflammatory bowel disease, rheumatoid arthritisUtility: Uncomplicated UTIs, trachoma (contag. disease of eyelid, conjunct, cornea), nocardiosis (tuberculosis-like infect.), prophylaxis (burnt skin, Special Features: Broken down in intestines to liberate 5-aminosalicylate (anti- suppressing recurring UTIs, rheumatic fever) inflammatory).Special Features: Spectrum—gram +, gram -. www.brain101.info 1
  2. 2. Name: Silver Sulfadiazine (Silvadene) Name: Sulfacetamide sodium (Sulamyd Sodium)Class: Sulfonamide Class: SulfonamideMech.: Releases silver → toxicity for bacteria and fungi. Mech.: Comp. inhib. of PABA incorp. into dihydropteric acid → inhib. of folicAbsorption: acid.Distribution: Topical Absorption:Metab.: Distribution: Ophthalmic application. Penetrates into ocular fluids at high conc.Excretion, t_: Metab.:Toxicity/S.E.s: Excretion, t_:Utility: Used topically to reduce infection of burns, but not to treat established Toxicity/S.E.s: infections. Utility: Ophthalmic infectionsSpecial Features: Special Features: High aqueous concentrations are not irritating.Name: Trimethoprim-Sulfamethoxazole (Bactrim, Septra) Name: Chloramphenicol (Chloromycetin)Class: Class:Mech.: Acts on two sequential steps in synth of folic acid. PABA competitive Mech.: Bacteriostatic. Inhib protein synth by binding to 50S subunit.inhib, dihydrofolate reductase inhib. Bacteriostatic. Absorption: Rapid oral absorptionAbsorption: Oral, IV Distribution: Body fluids, good CSF. Crosses placenta. Milk.Distribution: Metab.: Liver (glucuronyl transferase)Metab.: Excretion, t_: Urine (filtration, secretion), 1.5-3.5 hr.Excretion, t_: Toxicity/S.E.s: Bone marrow depression (anemia, leukopenia, thrombocytopenia,Toxicity/S.E.s: Megaloblastic anemia, leukopenia, granulocytopenia (prevented prob. due to inhib. of mitoch. protein), aplastic anemia by admin. of folic acid) (allergic/idiosync, rare, irreversible, often fatal), Gray BabyUtility: Uncomp. UTIs, otitis media, acute exacerbations of chronic bronchitis, Syndrome (neonate overdose due to reduced ability to conjuate various pneumonias. DOC for Travelers’ diarrhea, P. carinii pneumonia, CA and secrete metabolites), superinfection (S. aureus, Shigella enteritis, systemic Salmonella infects, prostatitis. Pseudomonas, fungi, can be life threatening).Special Features: Trimethoprim = highly selective inhib. of bacterial dihydrofolate Utility: DOC for severe Bacteroides infects (esp. CNS), backup for memingitis, reductase. rickettsial infects, brucellosis. Special Features: Never use if safer antibiotic avail. Never use for mild infects. www.brain101.info 2
  3. 3. Name: Tetracycline (Achromycin V) Name: Doxycycline (Vibramycin)Class: Tetracycline Class: TetracyclineMech.: Active uptake into bacteria →inhib protein synth by binding to 30S Mech.: Active uptake into bacteria →inhib protein synth by binding to 30S ribosome. Bacteriostatic ribosome. BacteriostaticAbsorption: Oral adequate, but incomplete. Impaired by divalent cations. IM Absorption: Good oral absorption. Impaired by divalent cations. IM painful. IV painful. IV may cause thrombophlebitis. Never intrathecal. may cause thrombophlebitis. Never intrathecal.Distribution: Good CSF. Conc. in liver → enterohepatic circ. Penetrates most Distribution: Good CSF. Conc. in liver → enterohepatic circ. Penetrates most tissues and fluids. Crosses placenta. tissues and fluids. Crosses placenta.Metab.: Metab.:Excretion, t_: filtration (1°), bile Excretion, t_: bile; doesn’t require renal excretionToxicity/S.E.s: GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad Toxicity/S.E.s: GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. brown discoloration of teeth; slowing of bone growth; phototoxicity; thrombophlebitis; discoloration of teeth; slowing of bone growth; phototoxicity (more than others); hematopoetic changes; rare hypersens. rxns. thrombophlebitis; hematopoetic changes; rare hypersens. rxns.Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for rickettsia, spirochetes. No effect on viruses or fungi. Also used for acne, prophylaxis for Travelers’ diarrhea. acne, prophylaxis for Travelers’ diarrhea.Special Features: Broad spectrum. Decreased effect of oral contraceptives. Special Features: Broad spectrum. Decreased effect of oral contraceptives.Name: Minocyclin (Minocin) Name: Penicillin GClass: Tetracycline Class: Penicillin (Penicillin G-related)Mech.: Active uptake into bacteria →inhib protein synth by binding to 30S ribosome. Bacteriostatic Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages ofAbsorption: Good oral absorption. Impaired by divalent cations. IM cell wall formation. Bactericidal. painful. IV may cause thrombophlebitis. Never intrathecal. Absorption: Erratic (30%). Usu. not used orally. I.M or I.V. Prolonged effectDistribution: Good CSF. Conc. in liver → enterohepatic circ. Penetrates most with repository preparations (procaine, benzathine (longest)) deep tissues and fluids. Also enters tears and saliva. Crosses placenta. IM.Metab.: Liver, but not critical. Distribution: Widely distributed, little CSF unless meninges inflamed.Excretion, t_: bile; doesn’t require renal excretion Metab.:Toxicity/S.E.s: Vestibular toxicity; GI — burning, discomfort, nausea, vomitiing; superinfection — due to broad spectrum, candida albicans (1°), staph enterocolitis, pseudomemb. Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. colitis; hepatotoxicity (esp. in pregnancy); renal toxicity; Fanconi synd.; perm. in bile. brown discoloration of teeth; slowing of bone growth; phototoxicity; Toxicity/S.E.s: hypersensitivity (1-10%), painful injection, epilepsy, thrombophlebitis; hematopoetic changes; rare hypersens. rxns. superinfection.Utility: gram - cocci, gram - bacilli, acid fast bacilli, chlamydiae, mycoplasma, rickettsia, spirochetes. No effect on viruses or fungi. Also used for Utility: Many gram +, anaerobes, and a few gram -. Most staph. and gram - acne, prophylaxis for Travelers’ diarrhea. resistant. Prophylactic use (rheumatic fever, strep. infections).Special Features: Broad spectrum. Decreased effect of oral contraceptives. Special Features: Narrow spectrum. www.brain101.info 3
  4. 4. Name: Penicillin V Name: Nafcillin (Nafcil)Class: Penicillin (Penicillin G-related) Class: Penicillin (Penicillinase-resistant)Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: Acid stable → good oral absortption. Absorption: Poor oral. Usu. IV for seious infections. IM.Distribution: Widely distributed, little CSF unless meninges inflamed. Distribution: Widely distributed, little CSF unless meninges inflamed.Metab.: Metab.:Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile. in bile.Toxicity/S.E.s: : hypersensitivity (1-10%), superinfection. Toxicity/S.E.s: hypersensitivity (1-10%), superinfection.Utility: Mild to moderate infections only: Many gram +, anaerobes, and a few gram Utility: Penicillinase-producing staph. infections. Gram +. -. Most staph. and gram - resistant. Same spectrum as Pen. G, but less Special Features: Narrow spectrum. Prob. most effective penicillinase-resist. active.Special Features: Narrow spectrum.Name: Methicillin (Staphcillin) Name: Oxacillin (Bactocill)Class: Penicillin (Penicillinase-resistant) Class: Penicillin (Penicillinase-resistant)Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: Usu. IV for seious infections. IM. Absorption: Acid stable. Absorbed orally. IM, IV.Distribution: Widely distributed, little CSF unless meninges inflamed. Distribution: Widely distributed, little CSF unless meninges inflamed.Metab.: Metab.:Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile. in bile.Toxicity/S.E.s: hypersensitivity (1-10%), superinfection. Toxicity/S.E.s: hypersensitivity (1-10%), superinfection.Utility: Penicillinase-producing staph. infections. Gram +. Utility: Penicillinase-producing staph. infections. Mild infections.Special Features: Narrow spectrum. Special Features: Narrow spectrum. www.brain101.info 4
  5. 5. Name: Ampicillin (Omnipen, Polycillin) Name: Amoxicillin (Amoxil)Class: Penicillin (Aminopenicillin) Class: Penicillin (Aminopenicillin)Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: Acid stable. Good oral, but food interferes. IM, IV. Absorption: Acid stable. Good oral (better than ampicillin).Distribution: Widely distributed, little CSF unless meninges inflamed. Distribution: Widely distributed, little CSF unless meninges inflamed.Metab.: Metab.:Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. in bile. in bile.Toxicity/S.E.s: diarrhea, non-allergy skin rash, hypersensitivity (1-10%), Toxicity/S.E.s: diarrhea (less than ampicillin), hypersensitivity (1-10%), superinfection. superinfection.Utility: More effective against gram -s (esp. Proteus, H. influenzae, E. coli, P. Utility: More effective against gram -s (esp. Proteus, H. influenzae, E. coli, P. mirabilis). Less active than Pen. G against gram+ cocci. mirabilis). Less active than Pen. G against gram+ cocci.Special Features: Broad spectrum. Special Features: Broad spectrum.Name: Ticarcillin (Ticar) Name: Clavulanic acidClass: Penicillin (Extended spectrum) Class: β-Lactamase InhibitorMech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: inhibits some β-lactamases cell wall formation. Bactericidal.Absorption: IM, IV. Absorption:Distribution: Widely distributed, little CSF unless meninges inflamed. Distribution:Metab.: Metab.:Excretion, t_: Rapidly elim. by kidneys (probenecid blocks excretion), small amt. Excretion, t_: in bile. Toxicity/S.E.s:Toxicity/S.E.s: hypersensitivity (1-10%), superinfection., coagulation disorders. Utility: Combined with amoxicillin (Augmentin) to increase efficacy againstUtility: Gram -. Effective against Pseudomonas, Proteus mirabilus, often used penicillinase-producing bacteria (i.e., staph.) w/aminoglyc. Special Features:Special Features: Narrow spectrum. Resistance develops quickly. www.brain101.info 5
  6. 6. Name: Sulbactam Name: ProbenecidClass: β-Lactamase Inhibitor Class: Mech.: Interferes w/renal excretion of drugs that undergo tubular secretion.Mech.: inhibits some β-lactamases Inhib. glucuronide conjugation of other drugs.Absorption: Absorption:Distribution: Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Toxicity/S.E.s:Utility: Combined with ampicillin (Unasyn-sulbactam) to increase efficacy against Utility: penicillinase-producing bacteria (i.e., staph). Special Features: Decreases renal excretion of methotrexate — possibleSpecial Features: toxicity. Decreases renal excretion of penicillin.Name: Cephalothin (Keflin) Name: Cephalexin (Keflex)Class: First Gen. Cephalosporin Class: First Gen. CephalosporinMech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: IV. IM rarely used due to pain. Absorption: Oral.Distribution: Poor CSF. Distribution: Poor CSF.Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, renal damage (worse if comb. w/aminoglycs.) renal damage (worse if comb. w/aminoglycs.)Utility: Usu not DOC. Serious Klebsiella infects., strep/staph infects, some Utility: Usu not DOC. Serious Klebsiella infects., strep/staph infects, some penicillinase-producing bacteria. penicillinase-producing bacteria.Special Features: Narrow spectrum. Greater gram - activity than pen. G. More Special Features: Narrow spectrum. Greater gram - activity than pen. G. More gram+ activity than gram - activity. Less susceptible to β- gram+ activity than gram - activity. Less susceptible to β- lactamase than most penicillins. lactamase than most penicillins. www.brain101.info 6
  7. 7. Name: Cefoxitin (Mefoxin) Name: Cefaclor (Ceclor)Class: Second Gen. Cephalosporin Class: Second Gen. CephalosporinMech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: IV. IM rare due to pain. Absorption: Oral.Distribution: Poor CSF. Distribution: Poor CSF.Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, renal damage (worse if comb. w/aminoglycs.) renal damage (worse if comb. w/aminoglycs.)Utility: Mixed anaerobic infects. Utility: Resp. and middle ear infections (H. influenzae, M. catarrhalis)Special Features: More gram- efficacy than first gen. Less gram+ cocci efficacy Special Features: More gram- efficacy than first gen. Less gram+ cocci efficacy than first gen. ↑ β-lactamase resistance. than first gen. ↑ β-lactamase resistance. Problem w/bacterial resistance.Name: Cefotaxime (Claforan) Name: Cefixime (Suprax)Class: Third Gen. Cephalosporin Class: Third Gen. CephalosporinMech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: IV Absorption: OralDistribution: good CSF Distribution: poor CSFExcretion, t_: Excretion, t_:Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, Toxicity/S.E.s: Hypersensitivity (some cross-sensitivity to pen.), superinfection, renal damage (worse if comb. w/aminoglycs.) renal damage (worse if comb. w/aminoglycs.)Utility: Serious nosocomial gram- sepsis. Meningitis caused by gram- enteric Utility: Serious nosocomial gram- sepsis. Serious Klebsiella infects., strep/staph bacteria or H. influenzae. Serious Klebsiella infects., strep/staph infects, infects, some penicillinase-producing bacteria. Nosocomial infects. some penicillinase-producing bacteria. Nosocomial infects. Often used Often used in comb. w/aminoglycosides. in comb. w/aminoglycosides. Special Features: Decreased efficacy against gram+ cocci. Broader gram-Special Features: Decreased efficacy against gram+ cocci. Broader gram- spectrum. More resistance against β-lactamases than spectrum. More resistance against β-lactamases than second generation. Problem w/bacterial resistance. second generation. Problem w/bacterial resistance. www.brain101.info 7
  8. 8. Name: Imipenem Name: Aztreonam (Azactam)Class: β-lactam (Carbapenem) Class: β-lactam (Monobactam)Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of Mech.: Binds to PBPs, blocks activity of transpeptidases in terminal stages of cell wall formation. Bactericidal. cell wall formation. Bactericidal.Absorption: Oral, IV (painful) Absorption:Distribution: Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: painful injection, allergy, nausea/vomiting, superinfection Toxicity/S.E.s: Gram+ superinfections. (diarrhea), reversible blood disorders. Utility: Infections caused by susceptible orgs. resistant to other drugs.Utility: Combined w/equal amts of cilastatin to block tubular metab. and formation Special Features: Not fused bicyclic. Potent gram-, but limited spectrum (only of nephrotoxic compounds. Treats serious nosocomial infections, aerobics and facultative gram-). Little cross-allergenicity infections of unknown etiology, mixed infections. w/pen. or ceph. Less toxic than aminoglycs. Usu used inSpecial Features: Broadest spectrum of all β-lactams. Resistant to penicillinases combinations (except for UTIs). and most β-lactamases. Resistance develops during treatment.Name: Methenamine Name: Nitrofurantoin (Furadantin)Class: UTI Agent Class: UTI AgentMech.: Decomposes at pH ≤5.5 to NH4+ and formaldehyde (bactericidal). Mech.: Unclear. Baceria activate nitrofurantoin more rapidly than do mammalian cells. Bacteriostatic in low conc., cidal in high conc.Absorption: Oral very good, but ↓ pH of stomach decomposes lots of the drug. Absorption: Rapidly and completely absorbed after oral admin. Enteric-coated tablet solves most of problem. Distribution: Antibact. conc. not achieved in plasma. Active in urine.Distribution: Activated 1° in urine. Metab.:Metab.: NH4+ production requires fxning liver for excretion. Kidneys only Excretion, t_:important if methenamine mandelate or hippurate is used. Toxicity/S.E.s: GI effects, pulm. toxicity (acute pneumoinitis, subacuteExcretion, t_: Excreted in urine. NH4+ reduced requires liver for excretion. interstitial pulonary fibrosis), hypersensitivity rxns. chronicToxicity/S.E.s: GI distress. Long term = rash, hematuria, albuminuria, hepatitis, neuro efffects. Turns urine brown. Not for preg. painful/frequent micturition. women or infants (hemolytic anemia). Not to be mixedUtility: Chronic suppression of UTIs. w/probenecid.Special Features: No resistance formation. Orgs which raise urine pH inhibit Utility: Uncomplicated lower UTIs caused by E. coli, Enteroccus, prevention of formaldehyde formation → ↓ sensitivity. recurrence of UTIs. Special Features: Effect enhanced by urine pH≤5.5. www.brain101.info 8
  9. 9. Name: Cinoxacin (Cinobac) Name: Ciprofloxacin (Cipro)Class: Nonfluorinated quinolone Class: Fluorinated quinoloneMech.: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal. Mech.: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal.Absorption: Oral Absorption: Rapid absorption after oral admin.Distribution: Distribution: Good tissue penetration. Poor CSF.Metab.: Metab.: Partial hepatic metab.Excretion, t_: Excretion, t_: Glomerular filtration, secretion. Also feces, bile, sputum. 4 hrs.Toxicity/S.E.s: Usu. not severe. GI, CNS. Not for pregnant or nursing women Toxicity/S.E.s: Usu. not severe. GI, CNS, arthropathy. Not for pregnant or or prepubertal children. nursing women or prepubertal children.Utility: UTIs due to coliform bacteria Utility: Upper and lower UTIs, DOC for Pseudomonas UTIs. Active againstSpecial Features: aerobic gram- bacilli, H. influenzae, Neisseria. Good alternate. for several causes of infectious diarrhea, osteomyelitis, and patients w/CF. Special Features: Broader spectrum than nonfluorinated quinolones.Name: Norfloxacin (Noroxin) Name: Phenazopyridine (Pyridium)Class: Fluorinated quinolone Class: Analgesic (not an antibiotic)Mech.: Inhib bact. DNA gyrase (topoisomerase II). Bactericidal. Mech.: Analgesic effect on urinary tract mucosa.Absorption: Oral admin. Absorption:Distribution: Good tissue penetration. Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_: 90% excreted in urine w/in 24 hrs.Toxicity/S.E.s: Usu. not severe. GI, CNS. Not for pregnant or nursing women Toxicity/S.E.s: GI, headaches. Not for use w/renal insufficiency or severe or prepubertal children. hepatitis. Hemolytic anemia. Cancer in rats. Stains urine,Utility: UTIs due to Enterobacteriaceae, Enteroccus, Staph, Pseudomonas. skin, sclera, and contact lenses red-orange.Special Features: Broader spectrum than nonfluorinated quinolones. Utility: Relief of dysuria and urethral irritation assoc. w/acute cystitis, trauma, surgery, catheterization, endoscopy. Special Features: When used w/antibacterial agent, should be discontinued after 48 hr. Should never be used on long-term basis to mask undiagnosed urinary tract pain. www.brain101.info 9
  10. 10. Name: Streptomycin Name: Neomycin (Mycifradin)Class: Aminoglycoside Class: AminoglycosideMech.: O2 dependent uptake → inhib. of protein synth by binding to 30S rib. Mech.: O2 dependent uptake → inhib. of protein synth by binding to 30S rib. subunit → leaky membranes. Bactericidal. subunit → leaky membranes. Bactericidal.Absorption: Poor oral absorption. Usu. IM or IV. Absorption: Very little oral absorption. Topical.Distribution: Limited to extracellular space. Poor CSF, ocular. No placenta. Distribution: Limited to extracellular space. Poor CSF, ocular. No placenta.Excretion, t_: glomerular filtration. 2 hrs. Excretion, t_:Toxicity/S.E.s: Ototoxicity. Vestibular toxicity. Low nephrotoxicity. Toxicity/S.E.s: Parenteral → severe ototoxicity and nephrotoxicity.Utility: Used in comb. therapy for tuberculosis. Used alone for bubonic plague Utility: Topical treatment of superf. sensitive skin and eye infections. and tularemia. Preoperative prophylaxis for bowel surgery.Special Features: Resistance 1° due to plasmid-med. mod. of aminoglyc. Also Special Features: Resistance 1° due to plasmid-med. mod. of aminoglyc. Also alter. of transport system, mutation of rib. subunit. alter. of transport system, mutation of rib. subunit.Name: Gentamicin (Garamycin) Name: Tobramycin (Nebcin)Class: Aminoglycoside Class: AminoglycosideMech.: O2 dependent uptake → inhib. of protein synth by binding to 30S rib. Mech.: O2 dependent uptake → inhib. of protein synth by binding to 30S rib. subunit → leaky membranes. Bactericidal. subunit → leaky membranes. Bactericidal.Absorption: Poor oral absorption. Usu. IM or IV. Absorption: Poor oral absorption. Usu. IM or IV.Distribution: Limited to extracellular space. Poor CSF, ocular. No placenta. Distribution: Limited to extracellular space. Poor CSF, ocular. No placenta.Excretion, t_: glomerular filtration. 2 hrs. Excretion, t_: glomerular filtration. 2 hrs.Toxicity/S.E.s: Ototoxicity (aud., vest.), nephtrotoxicity. Toxicity/S.E.s: Ototoxicity (aud., vest.), nephtrotoxicity (less than gentamicin).Utility: Nosocomial aerobic gram- infects, esp. in immunocomp, neutropenics. Utility: Nosocomial aerobic gram- infects, esp. in immunocomp, neutropenics. Often used in synergistic combs to treat P. aeruginosa, enteroccus, life- Often used in synergistic combs to treat P. aeruginosa, enteroccus, life- threatening gram- sepsis. Used in comb. against S. aureus. Ineffective threatening gram- sepsis. Used in comb. against S. aureus. Ineffective against anaerobes. against anaerobes.Special Features: Resistance 1° due to plasmid-med. mod. of aminoglyc. Also Special Features: Resistance 1° due to plasmid-med. mod. of aminoglyc. Also alter. of transport system, mutation of rib. subunit. alter. of transport system, mutation of rib. subunit. www.brain101.info 10
  11. 11. Name: Amikacin (Amikin) Name: ErythromycinClass: Aminoglycoside Class: MacrolideMech.: O2 dependent uptake → inhib. of protein synth by binding to 30S rib. Mech.: Inhib protein synth by binding to 50S rib. subunit. Bacteriostatic subunit → leaky membranes. Bactericidal. Absorption: Orally effective. Enteric-coated tablets.Absorption: Poor oral absorption. Usu. IM or IV. Distribution: Good tissue penetration, but poor CSF.Distribution: Limited to extracellular space. Poor CSF, ocular. No placenta. Metab.: Hepatic metab.Excretion, t_: glomerular filtration. 2 hrs. Excretion, t_: Secreted in bile as active drug. 1.6 hr.Toxicity/S.E.s: Ototox.(aud., vest.)(>than gent or tobr), nephtrotox.(<than gent.) Toxicity/S.E.s: GI irritation.,rashes, ototoxicity (large parenteral doses), drug interactions due to inhib of hepatic metab.Utility: Nosocomial aerobic gram- infects, esp. in immunocomp, neutropenics. Often used in synergistic combs to treat P. aeruginosa, enteroccus, life- Utility: Alternate to pen. in mild-moderate infects (esp. Strep, H. influenzae). threatening gram- sepsis. Used in comb. against S. aureus. Ineffective DOC for Legionnaire’s disease, Diphtheria carrier state, Mycoplasma against anaerobes. pneumoniae infects, Whooping cough (Bordatella pertussis) Special Features: Not recommended for severe staph. infections or forSpecial Features: Resistance 1° due to plasmid-med. mod. of aminoglyc. Also meningitis. alter. of transport system, mutation of rib. subunit. Least susceptible to resistance of the aminoglycs. Also, broadest spectrum. Most expensive aminoglyc.Name: Azithromycin (Zithromax) Name: Clindamycin (Cleocin)Class: Macrolide (azalide) Class: LincosamideMech.: Inhib protein synth by binding to 50S rib. subunit. Bacteriostatic Mech.: Inhib protein synth by binding to 50S rib. subunit. Bacteriostatic.Absorption: Good oral. Better than erythromycin. Absorption: Nearly complete oral absorption. IV.Distribution: Good tissue penetration. Better than erythromycin. Distribution: Good into most tissues, including bone. Poor CSF.Metab.: Hepatic metab. Metab.: Hepatic metab.Excretion, t_: Bile excretion. 68 hrs. Excretion, t_: Renal excretion. 2.7 hr.Toxicity/S.E.s: fewer than erythromycin, esp. GI. No interference w/cytochrome Toxicity/S.E.s: High incidence of diarrhea. Antibiotic-assoc. pseudomembranous p450 metab. colitis. Skin rashes. Local thrombophlebitis due to IV.Utility: Alternate to pen. in mild-moderate infects (esp. Strep, H. influenzae). Utility: Alternate to pen. or eryth. in susceptible infections. One DOC for non- DOC for Legionnaire’s disease, Diphtheria carrier state, Mycoplasma CNS anaerobic infections. Used topically for acne. pneumoniae infects, Whooping cough (Bordatella pertussis) Special Features:Special Features: Expanded spectrum over classic macrolides (more potent against gram- bacilli, chlamydiae). www.brain101.info 11
  12. 12. Name: Vancomycin (Vancocin) Name: Metronidazole (Flagyl)Class: Polypeptide Class: Nitroimidazole derivativeMech.: Blocks peptidoglycan polymerization → inhib cell wall synth. Bactericidal. Mech.: Inhib. DNA synth, degrades DNA, e- acceptor for reduced substrates.Absorption: Poorly absorbed from GI tract. Usu given IV Absorption: Complete, quick oral absorption.Distribution: Poor CNS Distribution: Well distrib to all tissues and fluids (including CSF)Metab.: Metab.: Hepatic metab.Excretion, t_: Renal excretion Excretion, t_:Toxicity/S.E.s: Ototoxicity, nephrotoxicity, thrombophlebitis (IV). In patients Toxicity/S.E.s: GI, metallic taste, neurotox (vertigo), disulfiram-like effect w/AIDS, “red man” syndrome (diffuse flushing) w/alcohol, neutropenia. Not for first trimester preg (mutagenic). Not for patients w/active CNS disease or hist. of bloodUtility: Last ditch measure against severe MRSA infects. DOC for antibiotic dyscrasias. assoc. pseudomembranous colitis (oral). Utility: IV treatment of anaerobic infects. Oral for amebiasis, giardiasis, andSpecial Features: Narrow spectrum (gram+ cocci), spec. MRSA, C. difficile. genital infects of Trichomonas vaginalis. Special Features: Antiparasitic and antibacterial activity. All anaerobic cocci and anaerobic gram- bacilli, including Bacteriodes. Trichomonasis, amebiasis, giardiasis.Name: Acyclovir (Zovirax) Name: Ganciclovir (Cytovene)Class: Antiviral Class: AntiviralMech.: Inhib. DNA synthase (most selective for herpes virus). Phosphorylated Mech.: Phosph by viral thymidine kinase. Competes w/normal nucleotides. by viral thymidine kinase. Then inhib. viral DNA polymerase by Prevents chain elongation upon incorporation. Also inhib. viral and competing w/deoxyguanosine triphosphate. cellular DNA polymerase.Absorption: Absorption: Poor oral. Usu. given IV.Distribution:some CSF Distribution: Good CSFMetab.: Metab.:Excretion, t_: Renal secretion, 2.5 hr. Excretion, t_: Renal excretion. 4 hr.Toxicity/S.E.s: Topical admin may cause loal irritation. IV may cause local Toxicity/S.E.s: Bone marrow suppression. Teratogenic and mutagenic in phlebitis, rash. Encephalophaty in renal-impaired. experimental animals.Utility: Topical, oral, IV application to treat herpes infections. Utility: CytomegalovirusSpecial Features: Special Features: www.brain101.info 12
  13. 13. Name: Foscarnet (Foscavir) Name: Trifluridine (Viroptic)Class: Antiviral Class: AntiviralMech.: Phosph by viral thymidine kinase. Competes w/normal nucleotides. Mech.: Pyrimidine analog. Competes with TTP for incorp into viral DNA. Inhib. Prevents chain elongation upon incorporation. Also inhib. viral and viral DNA synth. cellular DNA polymerase. Absorption:Absorption: Poor oral. Usu. given IV. Distribution: 1% soln applied to cornea. Not given systemicallyDistribution: Good CSF Metab.:Metab.: Excretion, t_:Excretion, t_: Renal excretion. 4 hr. Toxicity/S.E.s: Mutagenic and teratogenic activity in experimental tests.Toxicity/S.E.s: Renal dysfxn #1. Nausea, vomiting, headache, fatigue, anemia. Utility: Topical treatment for keratoconjunctivitis.Utility: Cytomegalovirus Special Features:Special Features: 3x more expensive than gancyclovir.Name: Interferon alpha 2b (Intron A) Name: Amantadine (Symmetrel)Class: Antiviral Class: Antiviral/Antiparkinsonian AgentMech.: Bind to cell-surface receptors and inhibit viral penetration or uncoating, Mech.: Blocks a late stage in assembly of influenza A virus synth or methylation of mRNA, translation of viral proteins, viral Absorption: Well absorbed orally. assembly or release, and degrade mRNA. → Inhib. viral protein synth. Distribution: Also induce a protein kinase that inactivates protein eIF-2 which is Metab.: necessarty for protein synth initiation. Excretion, t_: Excreted unchanged in urine.Absorption: Low oral activity. Usu. given IM or SC Toxicity/S.E.s: CNS toxicity (nervousness, confusion, hallucinations, insomnia,Distribution: depression, confusion). Overdose → toxic psychosis. Freq. livedoMetab.: Rapid degradation. reticularis (skin mottling). Peripheral edema, freq. nausea. C/I w/hist. of seizures or congestive heart failure. Amantadine>rimantadineExcretion, t_: 40 min.Toxicity/S.E.s: influenza-like illness. Bone marrow suppression Utility: Treat influenza A. Treat Parkinson’s Disease symptoms → improvement w/granulocytopenia and thrombocytopenia. Antibodies develop o akinesia, rigidity, tremor, gait disturbances, & total disability in ~ 50% of patients (mech. unknown). Use alone or w/L-Dopa for PD. w/continued use. Continued nasal admin → mucosal damage. Features: Can be used prophylactically for influenza A. For PD, sustainedUtility: Treat hepatitis B and C improvement may last up to 30 months, but may also be short lived (1-3 months). For PD, as good as or better than anticholinergics. www.brain101.info 13
  14. 14. Name: Rimantadine (Flumadine) Name: Ribavirin (Virazole)Class: Antiviral Class: AntiviralMech.: Blocks a late stage in assembly of influenza A virus Mech.: Purine analog. After phosphorylation, inhibits enzymes involved inAbsorption: Well absorbed orally. guanine nucleotide synth. After further phosph, inhib several viral- specific enzymes involved in DNA synth.Distribution: Absorption: Oral bioavail 45%. IV. Aerosol.Metab.: Hepatic metab. Distribution:Excretion, t_: Metab.:Toxicity/S.E.s: CNS toxicity (nervousness, confusion, hallucinations, insomnia) amantadine>rimantadine Excretion, t_: 40 daysUtility: Treat influenza A Toxicity/S.E.s: Accumulates in erythrocytes → hemolytic anemia. Bone marrowSpecial Features: Can be used prophylactically. suppression. GI, CNS aggravation. Teratogenic and mutagenic in animals. Toxicity avoided w/aerosol admin (for RSV). Antagonizes AZT activity. Utility: Aerosol form used to treat respiratory syncytial virus. Most important drug for treatment of hemorrhagic fever. Special Features:Name: Azidothymidine (Zidovudine, AZT) Name: Dideoxyinosine (Didanosine, Videx, DDI)Class: Antiviral Class: AntiviralMech: Thymidine analog. After phosph, inhib. viral RNA-dependent DNA Mech.: Inhib reverse transcriptase. polymerase (reverse transcriptase). Causes chain termination after Absorption: incorporation. Distribution:Absorption: Oral bioavail 60-65%. Metab.:Distribution: good CSF Excretion, t_:Metab.: Metab. to glucuronide. Antag. by ribavirin Toxicity/S.E.s: Peripheral neuropathy, rash, stomatitis, esophageal ulceration,Excretion, t_: 1 hr. pancreatitis, fever.Toxicity/S.E.s: Granulocytopenia (45%), anemia (transfusions necessary 30%), Utility: Treat HIV. Strains resistant to AZT may be susceptible. After treatment, headache, nausea, insomnia, myalgia. may become susceptible again to AZT. Alternating treatment superior toUtility: Treatment of HIV. Decreases plasma HIV RNA, increases CD4 cells, either alone. decreases # of opportunistic infects, prolongs survival. Reduces risk of Special Features: transmission by pregnant women to fetuses from 28% to 8%.Special Features: www.brain101.info 14
  15. 15. Name: Dideoxycytosine (Zalcitabine, Hivid, DDC)) Name: Indinavir (Crixivan)Class: Antiviral Class: AntiviralMech.: Inhib reverse transcriptase. Mech.: Inhib HIV protease activityAbsorption: Absorption: OralDistribution: Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Peripheral neuropathy, rash, stomatitis, esophageal ulceration, Toxicity/S.E.s: pancreatitis, fever. Utility: Treat HIVUtility: Treat HIV. Strains resistant to AZT may be susceptible. After treatment, Special Features: Active against strains resistant to reverse transcriptase may become susceptible again to AZT. Alternating treatment superior to inhibitors. either alone.Special Features:Name: Ritonavir (Norvir) Name: Saquinavir (Invirase)Class: Antiviral Class: AntiviralMech.: Inhib HIV protease activity Mech.: Inhib HIV protease activityAbsorption: Oral Absorption: OralDistribution: Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Toxicity/S.E.s:Utility: Treat HIV Utility: Treat HIVSpecial Features: Active against strains resistant to reverse transcriptase Special Features: Active against strains resistant to reverse transcriptase inhibitors. inhibitors. www.brain101.info 15
  16. 16. Name: Isoniazid (INH) Name: Rifampin (Rifadin)Class: Antitubercular Class: AntitubercularMech.: Tuberculostatic to resting bacilli, tuberculocidal to rapidly dividing cells. Mech.: Inhib. of bact. DNA-dependent RNA polymerase. Resist develops rapidly. Enters cells via active uptake. Interferes w/DNA synth, glycolyis, Absorption: Orally effective synth of mycolic acid (unique component of mycobacteria) Distribution: Diffuses freely into tissues and fluidsAbsorption: Rapidly absorbed after oral admin. Metab.: LiverDistribution: Distributes in total body water. Retained in infected tissue. Excretion, t_: 30% excreted in urine (50% active). T1/2= 1.5-5 hrs. ↓ in slowMetab.: Acetylated in liver. acetylaters.Excretion, t_: Urine. 75-90% in urine as metabolites in 24 hrs. Toxicity/S.E.s: Low incidence. Jaundice (can be fatal). Use w/cautionToxicity/S.E.s: Direct—inactivation/depletion of pyridoxine → peripheral neuritis w/impaired liver fxn. Induces hepatic microsomal enzymes. GI (treat prophylactically w/supplemental pyridoxine). distress, diarrhea, CNS complaints, hypersensitivity. Influenza- Hypersensitivity rxns. Hepatitis (can be fatal) due to toxic like syndrome. metabolites. Convulsions, optic neuritis, toxic encephalopathy, Utility: Rapidly improves TB patients to non-infectious state. Always used reversible psychotic episodes. w/other agents. Esp. useful in serious cases of TB. AsymptomaticUtility: Most important and widely used drug for tuberculosis. Prob. w/resistance. carriers of N. meningitis, eryth-resist. Legionella pneumophila infects.Special Features: Only drug approved for prophylaxis of tuberculosis. DOC for prophylaxis of H. influenza meningitis.Name: Ethambutol (Myambutol) Name: PyrazinamideClass: Antitubercular Class: AntitubercularMech.: Tuberculostatic, mech. unknown, may involve inhib of mycolic acid synth. Mech.: Bactericidal. Unknown mech.Absorption: Well absorbed orally. Not affected by food. Absorption: Well absorbed orally. Not affected by food.Distribution: Distribution: Dist. in total body water.Metab.: Metab.: Partially metabolized — hydrolyzed, hydroxylatedExcretion, t_: Renal excretion (50% unchanged and 15% inactive metab. in 24 hr) Excretion, t_: Glomerular filtration. 8 hrs.Toxicity/S.E.s: Few. Decreased visual acuity and ability to perceive color green Toxicity/S.E.s: Liver necrosis, hyperuricemia, nausea, vomiting, complication of (usually reversible). Gout. diabetes management.Utility: Treat TB. Resistance develops is used alone. Usu. used with isoniazid. Utility: Used to treat TB when there is resistance to other agents. Requires 3Special Features: additional effective agents. Special Features: www.brain101.info 16
  17. 17. Name: Amphotericin B (Fungizone) Name: NystatinClass: Antifungal (Polyene) Class: Antifungal (Polyene)Mech.: Assoc. w/ergosterol in fungal membrane → 4-5 Å pores. Fungistatic at low conc. Fungicidal at high conc. Mech.: Assoc. w/ergosterol in fungal membrane → 4-5 Å pores. Fungistatic atAbsorption: Insoluble in water. Colloidal preparation injected IV. Not absorbed low conc. Fungicidal at high conc. orally, IM, or after bladder irrigation. Used topically. Absorption: Poor oral absorption. Topical admin.Distribution: Bound to cholesterol and lipoprotiens. Poor CSF. Intrathecal may Distribution: be necessary to treat meningitis.Excretion, t_: Excreted very slowly as inactive metabolite by kidney. Metab.:Toxicity/S.E.s: Nephrotoxicity (80%) requires hospitalization for administration. Excretion, t_: Chills (50%), fever, nausea, vomiting, diarrhea, headache, Toxicity/S.E.s: No side effects when topically applied phlebitis, suppression of RBC synth. IT → headache, radiculitis, Utility: Superficial candidiasis (GI, cutaneous, oropharyngeal, vulvovaginal) via paresis, paresthesias, visual impairment. topical, oral, or vaginal admin.Utility: 1° drug used against serious systemic infections. DOC for 1° amebic Special Features: Safe during pregnancy. meningoencephalitis caused by Naegleria. Alt. for American cutaneous or mucocutaneous leishmoniasis. Weekly injections for chronic suppression of Histoplasmosis in AIDS patients.Special Features: No problem w/resistance development. Increases fungal permeability to other agents.Name: Flucytosine (Ancobon) Name: Ketoconazole (Nizoral)Class: Antifungal Class: Antifungal (Imidazole)Mech.: Converted to 5-fluorouracil in fungi (enzyme not in humans). 5-fluorouracil Mech.: Interferes w/ergosterol synth → altered fungal membrane permeability. → phosph deoxyribose that inhibits thymidylate synth. Fungistatic. Absorption: Absorbed well from GI if contents are sufficiently acidic.Absorption: Well absorbed orally. Distribution: Poor CSF at recommended doses. Ok CSF w/high doses.Distribution: Passes BBB (75%) → good CSF. Aqueous humor, bronchial Metab.: Degraded by liver. secretions. Poorly bound by serum proteins. Excretion, t_: Excreted mostly into bile. Only 10-15% appears unchanged inMetab.: urine. Excreted in milk. Toxicity/S.E.s: Fewer than Amphoter. or flucytosine. Rare fatal hepaticExcretion, t_: 1° glomerular filtration (unmetab. product). 3-4 hr → 200 hr w/renal necrosis. Dose-dependent decrease in testosterone. Toxicities failure. Dose must be adjusted if renal fxn compromised. for nursing infants. Rare anaphylactic shock. Can’t be usedToxicity/S.E.s: Bone marrow depression with anemia, thrombocytopenia, w/astemizole, terfenadine, loratadine due to inhib. of leukopenia. Nausea, rashes, eosinophilisa, severe diarrhea, reversible hepatic dysfxn. Confusion, hallucinations, headache, metabolism. Coadmin. w/ketoconazole → ↑ conc. of vertigo, possibly fatal enterocolitis (esp. in comb. w/Amphoter.). cyclosporin. Increases anticoag. response of anticoag drugs.Utility: DOC for Chromomycosis. Used in comb. w/Amph for systemic Candida Coadmin w/isoniazid or rifampin → ↓ ketoconazole. Albicans. Utility: DOC for Pseudoallescheria boydii. Alternate for C. albicans, H.Special Features: Narrower spectrum than Amphotericin B. Resistance develops capsulatum, B. dermatidis, Paracoccidiodes, C. immitis. rapidly, so usu. used in comb., except to treat Special Features: Very broad spectrum. Being phased out and replaced with Chromomycosis itraconazole and fluconazole. www.brain101.info 17
  18. 18. Name: Itraconazole (Sporanox) Name: Fluconazole (Diflucan) Class: Antifungal (Triazole)Class: Antifungal (Triazole) Mech.: Inhib. fungal cyt. P450 and sterol C-14 α-demethylation. Normal sterolsMech.: Inhib. cytochrome P450-dependent synth of ergosterol. depleted, 14-α-methyl sterols build up → fungistatic.Absorption: Oral absorption good. Better in presence of food, high gastric acidity. Absorption: Oral absorption ≅ IV absorption (rare phenom.) Distribution: Low plasma protein binding. Vd close to total body water. GoodDistribution: Neglibible CSF, saliva. saliva, good CSF (~80%), conc. in urine and skin.Metab.: Extensively metab. in liver. Metab.:Excretion, t_: Very little active drug remains in urine. Excretion, t_: 80% appears in urine unchanged. Excreted in milk. 30 hr. Toxicity/S.E.s: Rare hepatotoxicity. Rare exfoliative skin disorders (can beToxicity/S.E.s: Nausea, vomiting, headache, rash, loss of libido, impotence, fatal). GI irritation, rash. Affects rat fetal development. gynecomastia. Rare hepatotoxicity. Inhib. metab. of long-acting Increases metabolite levels of some terfenadine metabolits (not antihistamines (sim. to ketoconazole), erythromycin, triazolam, terf. itself). May slow metab. of long-acting antihistamines and cisapride. cyclosporines.Utility: DOC for many superficial and systemic infections. Alternate for many Utility: Candidiasis (oropharyngeal, esophageal, UTI, vaginal, systemic), superf. and systemic infections. Oral treatment of onychomycoses. Cryptococcal meningitis in AIDS patients and otherwise healthy patients. Same indications as ketocon., but also active against lymphocutaneous Coccidiodal meningitis. Chronic suppresion of Crypt. meningitis in AIDS form of sporotrichosis plus Aspergillosis. Usu. preferred to patients. Single-dose therapy for vaginal yeast infections. ketoconazole. Special Features: Oral absorption ≅ IV absorption. Only causes minor changes inSpecial Features: plasma testosterone and corticosteroid concentrations.Name: Griseofulvin (Grifulvin) Name: Miconazole (Monistat, OTC=Micatin)Class: Antifungal Class: Antifungal (Imidazole)Mech.: Binds to microtubules, disrupts mitotic spindle, blocks mitosis. Mech.: Causes leakage of small molecules/ions across plasma membrane. Also Fungistatic. blocks purine uptake. Fungistatic at low conc. Fungicidal at high conc.Absorption: Always given orally. Erratically absorbed. Fatty meals → ↑ absorption. Absorption: Good oral, but not admin due to GI irritation. Topical, IV, IT.Distribution: Binds in high conc. to keratin in areas of skin, hair, nails most Distribution: Good CSF affected by dermatophytes. Toxicity/S.E.s: Topical → occasional burning and irritation. IV/IT may causeMetab.: cardiorespiratory failure, thrombophlebitis.Toxicity/S.E.s: Headache, rare CNS effects (memory lapse, impaired judgment, Utility: Topical against common fungal infections of skin and vagina. Better than blurred vision. Candida superinfection. High doses nystatin for vaginal candidiasis. Esp. useful in mixed skin infections carcinogenic, teratogenic. Disulfiram-like effect with alcohol. featuring dermatophytes and Candida. Best topical agent for Reduces efficacy of some oral contraceptives. dermatophytoses (even severe). Efficacy = 90%. IV/IT as alternativeUtility: Inhibits most dermatophytes and superfic. yeast infections. Treats most for systemic Pseudallescheriasis infection (only non-topical use). types of tinea, ringworm, athletes foot. Special Features: Safe during pregnancy. Broad spectrum against fungi. AlsoSpecial Features: Cures at the base of the problem. When the cured base grow active against gram+ bacteria. completely out, patient is cured. Long eradication time. Poor cure rate. www.brain101.info 18
  19. 19. Name: Clortrimazole (Lotrimin) Name: Ciclopirox (Loprox)Class: Antifungal (Imidazole) (OTC) Class: Antifungal (OTC)Mech.: Causes leakage of small molecules/ions across plasma membrane. Also Mech.: blocks purine uptake. Fungistatic at low conc. Fungicidal at high conc. Absorption: Penetrates dermis, hair follicles, sebaceous glands.Absorption: Good oral, but not admin due to GI irritation. Topical. Distribution:Distribution: Good CSF Metab.:Toxicity/S.E.s: Topical → occasional burning and irritation. Excretion, t_:Utility: Topical against common fungal infections of skin and vagina. Better than Toxicity/S.E.s: nystatin for vaginal candidiasis. Esp. useful in mixed skin infections Utility: 81-94% cure rate for cutaneous candidiasis, tinea corporis, tinea pedis, featuring dermatophytes and Candida. Good topical agent for versicolor. May (one report) be useful in topical treatment of dermatophytoses. Troches esp. recommended for oropharyngeal onychomycosis. candidiasis. Special Features:Special Features: Safe during pregnancy. Broad spectrum against fungi. Also active against gram+ bacteria. At high conc, also trichomonocidal.Name: Tolnaftate (Aftate, Tinactin) Name: Undecylenic Acid (Desenex)Class: Antifungal (OTC) Class: Antifungal (OTC)Mech.: Mech.:Absorption: Absorption:Distribution: Distribution:Metab.: Metab.:Excretion, t_: Excretion, t_:Toxicity/S.E.s: Toxicity/S.E.s:Utility: 80% efficacy against dermatophytes Utility: <50% efficacy against athlete’s footSpecial Features: Special Features: www.brain101.info 19
  20. 20. Name: Iodide Class: Antifungal? Halide? Mech.: Absorption: Distribution: Metab.: Excretion, t_: Toxicity/S.E.s: Utility: Used as alternate treatment for superficial cutaneous Sporotrichosis. Special Features: www.brain101.info20

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