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Here are short flashcard topics based on the Sulfonamides and Other Synthetic Antimicrobial Drugs PDF:
Sulfonamides
| # | Front (Topic) | Back (Key Point) |
|---|---|---|
| 1 | History of Sulfonamides | First clinically successful antibacterial was Prontosil (1935), containing sulfanilamide |
| 2 | Mechanism of Action | Structurally similar to PABA; block PABA incorporation into folic acid, preventing purine/thymidine/methionine synthesis |
| 3 | Bacteriostatic or Bactericidal? | Bacteriostatic with slow onset of action |
| 4 | Why Selective for Bacteria? | Human cells absorb folic acid (vitamin); most bacteria must synthesize it and cannot take up exogenous folic acid |
| 5 | Resistance Mechanisms | More PABA production; DHPS with low affinity (plasmid-mediated); decreased drug influx |
| 6 | Antibacterial Spectrum | G+/G- bacteria, Nocardia, Chlamydia, E. coli, Klebsiella, Shigella, Salmonella; NOT Rickettsia |
| 7 | Three Categories by Administration | (1) Oral, well-absorbed; (2) Oral, not absorbed (sulfasalazine); (3) Topical |
| 8 | Sulfadiazine | Good CSF levels; combined with pyrimethamine = drug of choice for acute toxoplasmosis |
| 9 | Sulfisoxazole | Very good urine solubility; used for UTI |
| 10 | Sulfamethoxazole | Combined with trimethoprim (TMP-SMX); used for UTI |
| 11 | Sulfadoxine | Long-acting; combined with pyrimethamine = Fansidar (2nd-line malaria treatment) |
| 12 | Sulfasalazine | Oral, not absorbed; used in ulcerative colitis and enteritis |
| 13 | Topical Sulfonamides | Sulfacetamide (conjunctivitis/chlamydia); Mefenide acetate (burns - causes metabolic acidosis); Silver sulfadiazine (burns, less toxic) |
| 14 | Adverse Effect - Crystalluria | Crystals in acidic urine causing kidney damage; prevented by bicarbonate + adequate water intake |
| 15 | Adverse Effect - Stevens-Johnson | Rare (<1%) but potentially fatal severe erythema multiforme |
| 16 | Adverse Effect - Kernicterus | Displaces bilirubin from plasma proteins; neurotoxic in neonates - avoid in neonates and last 2 months of pregnancy |
| 17 | Adverse Effect - Hemolytic Anemia | In G6PD deficiency - low NADPH leads to oxidized glutathione, membrane peroxidation, hemolysis |
| 18 | Other Adverse Effects | GI distress (N/V/D), photosensitivity, allergic rashes, drug fever |
Trimethoprim (TMP) & TMP-SMX (Bactrim/Septra)
| # | Front (Topic) | Back (Key Point) |
|---|---|---|
| 19 | TMP Mechanism | Inhibits dihydrofolate reductase (DHFR); 50,000x more selective for bacterial DHFR than human |
| 20 | TMP-SMX Synergy | Inhibits two sequential steps in tetrahydrofolic acid synthesis - more effective than either drug alone |
| 21 | TMP-SMX Ratio | Combined 1:5 ratio (TMP:SMX) |
| 22 | TMP-SMX Clinical Uses | UTI, otitis media, traveler's diarrhea, Pneumocystis carinii pneumonia (drug of choice) |
| 23 | TMP-SMX - PCP Dosing | IV: 400/80 mg in 125 mL dextrose 5% over 60-90 min |
| 24 | TMP-SMX Adverse Effects | Skin reactions (most common); N/V; folic acid deficiency symptoms in pregnancy/alcoholism/malnutrition |
| 25 | TMP Resistance | Decreased penetration; increased DHFR production; altered DHFR with reduced drug affinity |
Quinolones / Fluoroquinolones
| # | Front (Topic) | Back (Key Point) |
|---|---|---|
| 26 | Quinolone Mechanism | Inhibit topoisomerase II (DNA gyrase) and topoisomerase IV; bactericidal |
| 27 | DNA Gyrase vs Topo IV | Gyrase = inhibits DNA ring cleavage; Topo IV = inhibits chromosomal separation |
| 28 | Spectrum by Generation | Norfloxacin (least effective); Ciprofloxacin (best for G-); Moxifloxacin/Gatifloxacin (best for G+/anaerobes) |
| 29 | Ciprofloxacin | Most effective against G- organisms; also used for COPD, pneumonia, UTI, prostatitis, gonorrhea |
| 30 | Quinolone Resistance | Mutation in target enzyme; E. coli: DNA gyrase changes first, then Topo IV; Staph/Strep: Topo IV first |
| 31 | Quinolone Pharmacokinetics | Good oral bioavailability; mainly excreted in urine; interactions with antacids and bivalent cations |
| 32 | Quinolone Adverse Effects | GI (most common); CNS (headache, dizziness); rash; QTc prolongation (levo, moxi, sparfloxacin); hepatotoxicity (trovafloxacin) |
| 33 | Quinolones & Cartilage | Damage to growing cartilage in children - NOT recommended under 18; tendonitis/tendon rupture in adults; avoid in pregnancy |
| 34 | Nalidixic Acid | Older quinolone; good G- rod activity; mainly for UTI |
Other Urinary Antimicrobials
| # | Front (Topic) | Back (Key Point) |
|---|---|---|
| 35 | Nitrofurantoin Mechanism | Reduced by bacterial reductases forming toxic product; selective because rapidly excreted/broken down in plasma |
| 36 | Methenamine Mandelate | Releases formaldehyde in acidic urine which denatures protein; broad-spectrum bactericidal; used for UTI (especially E. coli) |
These 36 flashcards cover all major topics in the PDF: history, mechanism, spectrum, pharmacokinetics, clinical uses, and adverse effects for sulfonamides, TMP-SMX, quinolones, nitrofurantoin, and methenamine.
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