Drugs two last time Flashcards
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Bacteriostatic Inhibitors of protein synthesis function, and 8 classes included
Inhibit growth and replication, do not kill bacteria, include
- tetracyclines
- macrolides
- clindamycin
- chloramphenicol
- dalfopristin/quinipristin
- Linezolid
- Retamulin/mupirocin
- Tigecycline
Tetracyclines spectrum (including 9 specific ones)
Broad speectrum including
1) rickettsia
2) spirochettes
3) brucella
4) chlamydia
5) mycoplasma
6) vibrio cholerae
7) helicobacter pylori
8) borrelia burgdorferi
9) bacillus anthracu
3 common uses of tetracyclines
1) acne
2) peptic ulcers
3) peridontal disease
3Tetracycline ADRs
Photosensitivty, bone and teeth discoloration, suprainfection
Tetracycline mech of action
Bind 30s ribosome preventing protein synthesis, actively transported into cell via energy dependent process only present in bacterial cells
Tetracycline resistance
Decreased uptake, increased exclusion of tetracyclines
Tetracycline absorption
GI absorption limited because of chelates (with any metal ion), topical use too
4 tetracyclines available
1) tetracycline (short acting, no food)
2) denecocycline (medium acting, no food)
3) doxyxcline(long acting, no food)
4) minocycline (long acting, food okay)
Fanconi syndrome
Ingestion of outdated tetracycline can cause renal tubular dysfunction leading to renal failure
Macrolides spectrum
Broad spectrum
Macrolides include 3 drugs
1) erythromycin
2) azithromycin
3) clarithromycin
Macrolides resistance
Pumping out macrolides or modifying target ribosomes
Macrolide mechanism of action
Bind 50S ribosome subunit to prevent protein synthesis
Erythromycin spectrum
Most gram + and few gram -, first choice for bordatella pertussis and cornybacterium diptheria
Erythromycin is often seen as an alternative for ____ in those with an allergy
PCN G
Erythromycin ADRs
- suprainfection
- QT prolongation and sudden cardiac death (torsades de pointes)
Clarithromycin spectrum
Most gram + and few gram -, more active than erythromycin in certain situations
Clarithromycin ADRs
- Very few
- Potential QT prolongation
Clarithromycin and azithromycin are often prescribed over erythromcyin because of one distinct advantage
They do not typically cause nausea and diarrhea
Azithromycin spectrum
Less active than erythromycin on strep/staph, more active on gram - bacterium
Azithromycin ADR’s
- Cannot be taken with food
- Increased risk of heart arrhythmias
Clindamycin mechanism of action
Inhibition of the 50S ribosome to prevent protein synthesis
Clindamycin absorption
-Parenterally/IV, topical, oral
Clindamycin excretion
Mostly hepatic metabolism
Clindamycin treats
Gram + and -, DOC for Bacteroides
Clindamycin ADR
Can cause psudomembranous colitis from Cdiff
Chloramphenicol mechanism of action
Inhibit protein synthesis through binding the 50s ribosomal subunit
Chloramphenicol spectrum
Broad spectrum but often last resort, DOC for typhoid fever and effective against bacterial meningitis
Chloramphenicol absorption
GI route
Chloramphenicol ADRs
- Pancytopenia (aplastic anemia)
- Gray baby syndrome
Dalflopristin/Quinipristin mechanism of action
Streptogamins, together become bactericidal
Dalflopristin/Quinipristin treats…
VRE and MRSA
Dalfopristin/Qunipristin ADR’s
- Hepatotoxicity
- Thrombophlebitis
Linezolid mechanism of action
Binds 23s portion of 50s subuinit of ribosome, cross resistance therefore unlikely
Linezolid treats
VRE and MRSA
Linezolid ADR
Myelosuppression
Tigecycline spectrum
Gram + and -, drug resistant strains, no pseudomonas
Tigecycline mechanism of action
Binds to 30s ribosome
Tigecycline absorption
IV antibiotic
Tigecycline ADRs
Stained teeth in children and photosensitivity
Retapamulin/mupirocin function
Topical antibiotics indicated for impetigo
Fluoroquinolones are designated not to be used…
…in simple and acute infections
Fluoroquinolones spectrum
Broad spectrum, most gram neg and some gram pos including MRSA
Fluorquinolones abosrption
PO administration
Fluoroquinolones ADRs
Tendon rupture/peripheral neuropathy/hypogllycemia/mental illness
Fluoroquinolones include these 8
1) ciprofloxacin
2) norfloxacin
3) ofloxacin
4) Levofloxacin
5) Moxifloxacin
6) gemifloxacin
7) gatifloxacin
8) delafloxacin
Fluoroquinolones mech of action
Enter bacterium by passive diffusion and inhibit replication of baterial DNA by inhibiting bacterial DNA gyrase and toposiomerase IV
Fluorquinolones have a poor activity against….
…anaerobes
Fluorquinolone resistance (2)
1) alterations in DNA gyrase
2) reduced ability of drug to cross bacterial membranes
Cipro is often given prophylactically for patients exposed to these 2 pathogens
1) anthrax exposure
2) meningococcal disease
Cipro ADR
Phototoxicity
Cipro absorption
Gut, must be taken apart from food to prevent chelate formation
Norfloxacin indication
UTI caused by P aeruginosa
Ofloxacin indication
Less effective against P. aeruginosa
Levofloxacin
More effective against gram +
Moxifloxacin
CAP
Gemifloxacin
CAP
Gatifloxacin
Topical use only
Delafloxacin
Acute bacterial skin infection from MRSA
Metronidazole spectrum
Protozoa or anaerobic bacteria, DOC for Cdiff, amoeba, and trichomonas vaginalis
Metronidazole mechanism of action
Taken up passively, converted to active form in anaerobic bacteria, break up DNA helical structure
Metronidazole ADRs
Neurologic effect, urine darkening
Rifampin spectrum
Broad, often for myobacterial infection
Rifampin mech of action
Inhibit RNA poly
Rifampin ADR
Hepatotoxicity, body fluid discoloration
Bacitracin absorption
Topical only (unless life threatening)
Bacitracin mech of action
Inhibit synthesis of cell wall
Bacitracin spectrum
Gram pos
Sulfonamides mech of action
Inhibition of synthesis of folic acid by binding where PABA does to be bacteriostatic
Sulfonamide resistance (3 methods)
R factor
1) Increase synthesis of PABA
2) Prevent sulfonamide binding
3) Reduce uptake of sulfonamide
Sulfonamide spectrum
Broad, gram + including MRSA and some gram neg, DOC for acute UTI
Sulfonamide ADRs
- Photosensitivity
- drug fever
- Steven Johnson syndrome (widespread lesions)
- acute hemolytic anemia
- Kernicterus (bilirubin buildup in newborn brain
Trimethoprim spectrum
Gram - bacilli, some gram +, some protozoa, DOC for uncomplicated UTI
Trimethoprim-Sulfamethoxazole (bactrim) spectrum
UTI, pneumocytis pneumonia, others
