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15 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Sulfonamides (Drugs):
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Sulfacytine - Oral-absorbable
Sulfisoxazole - Oral-absorbable Sulfamethizole - Oral-absorbable Sulfadiazine - Oral-absorbable Sulfamethoxazole - Oral-absorbable Sulfapyridine - Oral-absorbable |
Sulfadoxine - Oral-absorbable
Sulfasalazine - Oral-non-absorbable Sodium sulfacetamide - Topical Mafenide acetate - Topical Silver sulfadiazine - Topical |
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Sulfonamides (MOA):
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Compete with PABA; Inhibit dihydropteroate synthase (DHPS)
PABA analogs Bacteriostatic |
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Sulfonamides (Indications):
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Broad spectrum: Active against G(+), G(-), chlamydia trachomatis and some protozoa
Synergistic (bactericidal) when combined with trimethoprim or pyrimethamine Urinary tract infection Trimethoprim-sulfamethoxazole (TMP-SMZ) is the drug of choice for Pneumocystis jirovecci pneumonia and Toxoplasmosis Sulfasazaline is used in ulcerative colitis and other inflammatory bowel disease |
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Sulfonamides (Kinetics):
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Metabolized in liver; eliminated by kidney
Most are oral with some being topical |
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Sulfonamides (Adverse Reactions):
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Urinary tract disturbances (Crystalluria, hematuria or obstruction)
Crystalluria can be treated by administration of sodium bicarbonate and fluids Hematopoietic disturbances - provoked in patients with glucose-6-phosphate dehydrogenase deficiency Stevens-Johnson syndrome - skin and mucous membrane eruption |
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Sulfonamides (Resistance):
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Mutations that cause overproduction of PABA
Mutations that cause production of a plasmid-encoded DHPS that has a low affinity for sulfonamides Mutations that impair permeability to the drugs |
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Trimethoprim (MOA):
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Selectively inhibits bacterial DHFR
Bacteriostatic |
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Trimethoprim/TMP-SMZ (Indications):
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Trimethoprim - Urinary tract infection
TMP-SMZ - pneumocystis jirovecii pneumonia (PCP) |
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Trimethoprim/TMP-SMZ (Adverse Reactions):
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Trimethoprim - Megaloblastic anemia, granulocytopenia
TMP-SMZ - GI upset, renal damage, CNS disturbances |
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Trimethoprim/TMP-SMZ (Resistance):
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Reduced cell permeability
Overproduction of DHFR Altered DHFR with reduced drug binding |
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Fluoroquinolones (Drugs):
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Norfloxacin
Ciprofloxacin - the most active against G(-) (P. aeruginosa) Enoxacin Ofloxacin Lomefloxacin |
Pefloxacin
Levofloxacin - superior activity against G(+), including S. pneumoniae Moxifloxacin Gemifloxacin |
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Fluoroquinolones (MOA):
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Blocks DNA synthesis by inhibiting topoisomerase II (DNA gyrase) and topoisomerase IV
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Fluoroquinolones (Indications):
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Active against various G(+) and G(-) bacteria
Urinary tract infection and bacterial diarrhea Ciprofloxacin is a drug of choice for prophylaxis and treatment of anthrax Respiratory fluoroquinolones (levofloxacin, gemifloxacin, moxifloxacin) have enhanced activity against G(+) and are used for RTI |
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Fluoroquinolones (Kinetics):
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Oral absorption impaired by divalent cations (e.g., antiacids)
Widely distributed in body fluids and tissues Most are excreted by kidney Moxifloxacin and gemifloxacin are eliminated through nonrenal mechanism Levofloxacin, gemifloxacin, moxifloxacin - once daily dosing possible |
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Fluoroquinolones (Adverse Reactions):
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GI upset (nausea, vomiting, diarrhea)
CNS (headache, dizziness, insomnia) Skin rash, photosensitivity QT prolongation (potential arrhythmia) Arthropathy (not routinely recommended for <18-yr old) Tendinitis, tendon rupture |
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