11 & 12 Flashcards by JULIA MARIE GUINTO

Similar to p-aminobenzoic acid
(PABA)
● Weakly acid compounds
● Modest tissue absorption

SULFONAMIDES

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SULFONAMIDES excretion and metabolization sites

Metabolized in the liver
Excretion: urine

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Triple Sulfa

Sulfisozaxole: short-acting
Sulfamethosaxole: intermediate acting
Sulfadoxine: long-acting

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ROA SULFONAMIDES

Oral absorbable, Oral non-absorbable, Topical

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Sulfonamide is a _____ inhibitor of Dihydropteroate synthase and folate production

Competitive or Selective

Competitive

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SULFONAMIDES are usually given in combination with

Trimetophrim or Pyrimethamine

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Sulfonamides are Bacteriostatic or Bactericidal

Bacteriostatic (when given alone)

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T/F: Is sulfonamide plasmid-mediated

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Resistance in Sulfonamide: accumulation of drug
Increase or Decrease

Decreased

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Resistance in Sulfonamide: production of PABA by bacteria
Increase or Decrease

Increase

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Resistance in Sulfonamide: sensitivity of
dihydropteroate synthase
Increase or Decrease

Decrease

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CLINICAL APPLICATIONS:
Gram (+)
Gram (-)
Klebsiella pneumoniae
Salmonella
Shigella
Enterobacter sp.
Nocardia sp.
Chlamydia trachomatis

SULFONAMIDES

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Poor against anaerobes

SULFONAMIDES

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Not active against: Ricketssiae & P. aeruginosa

SULFONAMIDES

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Clinical application of Oral triple sulfa, sulfisoxazole

Simple UTI

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Nephrotoxicity
- Crystalluria and hematuria

SULFONAMIDES

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Drug interactions with Warfarin & methotrexate

SULFONAMIDES

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TOXICITY:
Hypersensitivity
- Skin rash & fever (common)
- Exfoliative dermatitis (rare)
- Polyarteritis nodosa (rare)
- Stevens-Johnson syndrome (rare)
- Cross-allergenicity

SULFONAMIDES

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ROA TRIMETHOPRIM

PO, IV

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Toxicity of Sulfonamide which is in the 3rd trimester of pregnancy

Kernicterus

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TRIMETHOPRIM excretion site

Excretion: urine (unchanged)

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Structurally similar to folic acid
● Weak base
● Trapped in acidic environments
● High conc: prostatic and vaginal fluids

TRIMETHOPRIM

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TRIMETHOPRIM is a _____ inhibitor of bacterial dihydrofolate reductase

Competitive or Selective

Selective

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Resistance in TRIMETHOPRIM: cell permeability

Increase or Decrease

Decrease

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Resistance in TRIMETHOPRIM: production of dihydrofolate reductase Increase or Decrease

Increase

Clinical application of Oral Trimethoprim

Acute UTIs

CLINICAL APPLICATIONS: P. jirovecii UTIs Prostatitis Shigella Salmonella Nontuberculous mycobacteria

Oral Trimethoprim-Sulfamethoxazole (TMP-SMZ)

TOXICITY: Megaloblastic anemia, Leukopenia, & Granulocytopenia - Supplementary folinic acid

TRIMETHOPRIM

CLINICAL APPLICATIONS: Toxoplasmosis

Oral Pyrimethamine with Sulfonamide

CLINICAL APPLICATIONS: Moderately severe to severe pneumocystis pneumonia

IV Trimethoprim-Sulfamethoxazole

TOXICITY: HIV patients given ____ - Fever - Rashes - Leukopenia - Diarrhea

TRIMETHOPRIM

Mild elevation of blood creatinine

TRIMETHOPRIM

CLINICAL APPLICATIONS: Sinus infections caused by - H. influenzae - M. catarrhalis

TMP-SMX (TRIMETHOPRIM & SULFAMETHOXAZOLE)

CLINICAL APPLICATIONS: DOC of: - Pneumocystis pneumonia - Toxoplasma - Nocardiosis

TMP-SMX (TRIMETHOPRIM & SULFAMETHOXAZOLE)

Treatment of infections - MR staphylococci - L. monocytogenes

TMP-SMX (TRIMETHOPRIM & SULFAMETHOXAZOLE)

TOXICITY: - Nausea - Vomiting - Drug fever - Vasculitis - Renal damage - CNS disturbances - HIV: Fever, Rashes, Leukopenia, Diarrhea

TMP-SMX (TRIMETHOPRIM & SULFAMETHOXAZOLE)

CLINICAL APPLICATIONS: - Ulcerative colitis (oral) - Rheumatoid arthritis (oral) - Enteritis - Other Inflammatory Bowel Diseases (IBDs)

SULFASALAZINE (SALICYLAZOSULFAPYRINE)

CLINICAL APPLICATIONS: ● Opthalmic solution or ointment ● Bacterial conjunctivitis ● Ocular infection

SODIUM SULFACETAMIDE

CLINICAL APPLICATIONS: ● First line for Acute Toxoplasmosis

SULFADIAZINE + PYRIMETHAMINE

CLINICAL APPLICATIONS: ● P. jirovecii pneumonia ● Toxoplasmosis ● Nocardiosis

SULFAMETHOXAZOLE

CLINICAL APPLICATIONS: ● Topical ● Burn wounds - For prevention of infection

SILVER SULFADIAZINE

CLINICAL APPLICATIONS: ● Topical ● Burn wounds - Can cause metabolic acidosis

MAFENIDE ACETATE

CLINICAL APPLICATIONS: ● Marketed in some countries ● Second-line antimalarial agent

SULFADOXINE + PYRIMETHAMINE (FANSINADIR / FANSIDAR)

These were originally developed because of their gram-negative aerobic coverage (with gram+ coverage as well)

FLUOROQUINOLONES

Impaired absorption when combined with antacids, divalent, and trivalent cations (Should be taken 2h before or 4h after)

FLUOROQUINOLONES

Interfere with bacterial DNA synthesis - Topoisomerase II (relaxation) - Topoisomerase IV (separation)

FLUOROQUINOLONES

is Fluoroquinolones Bactericidal or Bacteriostatic

Bactericidal

Resistant organism appears in about every 107-109: o Staphylococci o P. aeruginosa o S. marcesens

FLUOROQUINOLONES

Emerged rapidly for 2nd generation: o C. jejuni and gonococci o Gram (+) cocci (MRSA) o Pseudomonas and Serratia

FLUOROQUINOLONES

CLINICAL APPLICATIONS: * Urogenital and gastrointestinal tract infection * Atypical and intracellular pathogens * Gr (+) bacteria * Gram (-) organisms o Gonococci o E. coli o K. pneumoniae o C. jejuni o Enterobacter o P. aeruginosa o Salmonella o Shigella

FLUOROQUINOLONES

CLINICAL APPLICATIONS: Bacterial diarrhea * Meningococcal carriers * Prophylaxis of bacterial infections w/ neutropenia * Effectiveness is variable due to resistance o Respiratory tract o Skin and soft tissue infection

FLUOROQUINOLONES

TOXICITIES: * Tendinitis and tendon rupture * Superinfection caused by C. albicans and streptococci * Temporary to Permanent Peripheral Neuropathy * Increase levels of theophylline and other methylxanthines

FLUOROQUINOLONES

TOXICITIES: * May damage growing cartilage and cause arthropathy o Not recommended but may be used for patients below 18 years old * Avoid in pregnancy

FLUOROQUINOLONES

Which DNA gyrase inhibitors can cause photosensitivity

Lomefloxacin, Pefloxacin, Sparfloxacin

Derived from nalidixic acid (earliest) * Common pathogens that cause UTI * Does not achieve adequate plasma levels for use in systemic infections

NORFLOXACIN

Least active of the fluoroquinolones against both gram negative and gram positive organisms

NORFLOXACIN

Synthetic fluorinated derivatives Oral bioavailability: 70%

CIPROFLOXACIN

CLINICAL APPLICATIONS: * Gram (-): greater activity o P. aeruginosa * Gram (+) cocci * Gonococcus * Mycobacteria * MSSA * Atypical organisms (M. pneumoniae)

2nd Gen DNA gyrase inhibitors

CLINICAL APPLICATIONS: * N. gonorrhea (single oral doses) - Alternative to 3rd generation cephalosporin ● Anthrax

CIPROFLOXACIN

CLINICAL APPLICATIONS: * Will eradicate accompanying organisms like Chlamydia (7 day course) o Urethritis

OFLOXACIN

3rd GENERATION DNA gyrase inhibitors

LEVOFLOXACIN, GATIFLOXACIN, SPARFLOXACIN

* Synthetic fluorinated derivatives * Oral bioavailability: 95%

LEVOFLOXACIN

CLINICAL APPLICATIONS: * Slightly less active against gram (-) * Greater activity against gram (+) cocci * Streptococci * S. pneumoniae * Staphylococci * MRSA * MSSA * Some strains of enterococc

LEVOFLOXACIN & GATIFLOXACIN

CLINICAL APPLICATIONS: * Community-acquired pneumonia * Atypical pneumonia (M. pneumoniae) * Anthrax prophylaxis

LEVOFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) o S pneumoniae o Some staphylococci

GATIFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) organisms * Penicillin-resistant pneumococci

SPARFLOXACIN

* Enhanced activity against anaerobes

SPARFLOXACIN

TOXICITIES: QT prolongation

LEVOFLOXACIN

TOXICITIES: * QT prolongation * Hypoglycemia when given with oral hypoglycemic agents

GATIFLOXACIN

TOXICITIES: * Risk for cardiac arrhythmia * Photosensitivity

SPARFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) o S pneumoniae o Some staphylococci * Gram (-) organisms * Anaerobic bacteria * Lacks appreciable activity against: o P. aeruginosa * Used in meningococcal carrier state * Tuberculosis * Neutropenia prophylaxis

MOXIFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) * Gram (-) organisms * Anaerobic bacteria * Used in meningococcal carrier state * Tuberculosis * Prophylactic management: neutropenic patients

TROVAFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) o S. pneumoniae o Some staphylococci ● + Azithromycin o Lower RTIs

GEMIFLOXACIN

CLINICAL APPLICATIONS: * Gram (+) o S. pneumoniae o Some staphylococci o Pneumococci o Beta-hemolytic streptococci o MSSA o MRSA * Gram (-): similar to ciprofloxacin o P. aeruginosa * In vitro activity against anaerobes but not proven

DELAFLOXACIN

11 & 12 Flashcards

(76 cards)