Ocular Pharm: L3: Drugs to Treat Ocular Infections Flashcards
What are the main things you should think about when Treating infections?
- Type of Organism
- Location
- Natural course of infection
- Patient’s immune status
- chances that organism is drug resistant
Ideal Antimicrobial Tx Strategy
- First establish what?
- Select drugs that are what to the organism?
- Select drug that is least what?
- Establish effective what at site of infection?
- Use appropriate what?
- Augment therapy with what?
- What do we do with the patient?
- When do you evaluate treatment effectiveness?
a. What if it’s a more severe infection?
- Diagnosis
- sensitive
- Least toxic/safest active drug
- Dose level
- dosing schedule and duration
- w/physical procedures
- educate them!
- about 1 week
a. 3 days if no substantial improvement, and sooner for severe infections
Antibacterial Drugs
- What kinds are there? (5)
- Cell wall inhibitors
- Cell membrane disruptors
- DNA synthesis inhibitors
- Folate Metabolism Inhibitors (Anti-metabolic)
- Protein Synthesis Inhibitors
Bacterial vs. Eukaryotic Cells
- What do bacterial cells have that Eukaryotic cells do NOT?
- Bacterial cells what what kind of membranes?
a. Their membranes are what?
b. What do Eukaryotic cells have?
3. Bacterial Ribosomes differ from what?
- What can enter Eukaryotic Cells but not bacterial Cells?
a. Why is this?
b. What do bacterial cells need to do then? - Bacterial cells have what kind of DNA?
a. Eukaryotic?
b. What do bacterial cells have to do more to their DNA than eukaryotic cells have to do?
- Cell wall
- Inner and Outer membranes
a. They’re ANIONIC
b. 1 inner membrane. They’re ZWITTERIONIC
3. eukaryotic ribosomes
4. Folic Acid
a. Due to bacterial cell wall
b. They have to make it
5. Circular DNA
a. Linear
b. Have to unwind their DNA more
Cell Wall Inhibitors (1)
- Penicillins (Main one he had listed)?
a. Bactericidal/Static?
b. Spectrum range?
c. Sensitive to what? (Except if they’re Given with WHAT?)
d. Problem with the Older drugs?
e. Toxicity level? (high or low)?
f. MAJOR SIDE EFFECT?
- AMOXICILLIN
a. Cidal
b. Gram + to Extended Spectrum
c. Beta Lactamase Sensitive (unless u give it w/a Beta Lactamase Inhibitor, e.g. Clauvanate)
d. Resistance
e. Low
f. Sensitivity
Cell Wall Inhibitors (2)
- Cephalosporins (2 main ones he has listed)
a. Cidal/Static?
b. Range of spectrum?
c. problem w/older drugs?
d. Major side effect?
e. Which generation drugs cross-react w/Penicillin?
- CEFTRIAXONE, and CEPHALEXIN
a. Cidal
b. Gram + in First generation, to Extended Spectrum in Fourth Generation
c. Resistance
d. Sensitivity
e. 1st generation drugs
Cell Wall Inhibitors (3)
- Bacitracin
a. Cidal/Static?
b. Coverage?
c. Administered how? - VANCOMYCIN
a. cidal/Static?
b. Range?
c. USED FOR what?
d. Problems (2)? - ETHAMBUTOL
a. EFFECTIVE against what?
b. Problems?
- Cidal
b. Mainly Gram + coverage
c. Topically (Nephrotoxicity) - a. CIDAL
b. Gram + coverage
c. MRSA
d. Nephro- and Ototoxicity - a. TB Bacteria
b. Optic Neuritis, Color Blindness, Nystagmus, Arthralgia
Cell Membrane Disruptors
- POLYMYXIN B
a. Cidal/Static?
b. Coverage?
c. Used with other Drugs (like what)?
d. Issues? (2) - Gramicidin
a. Cidal/Static?
b. Coverage?
c. Used with other drugs: Substitute for what?
d. How is it administered? Why?
- a. Cidal
b. Gram NEGATIVE
c. like TRIMETHOPRIM as Polytrim
d. Nephro and Oto Toxicity - a. Cidal (but can be static depending on growth phase)
b. Gram + coverage
c. for Bacitracin
d. Topical ONLY; will cause HEMOLYSIS otherwise
Protein Synthesis Inhibitors (1)
- Aminoglycosides (Main one he had highlighted?)
a. What does it inhibit?
b. static/cidal?
c. How are they given?
d. What 2 things can they cause?
e. Coverage - Tetracyclines (What 2)
a. What do they inhibit?
b. Static/cidal?
c. Coverage?
d. High Resistance in what?
e. Toxicities?
- TOBRAMYCIN, gentamycin (Bolded = NB)
a. Protein Synthesis Inhibitor (30S)
b. Can be either
c. Topically or Parenterally (poor oral absorption)
d. Nephro and Oto toxicity
e. Gram + and -
- TETRACYCLINE, DOXYCYCLINE
a. Protein synthesis (30S)
b. Static
c. Broad spectrum
d. in Common Bacteria
e. Many; Discoloration of Developing TEETH (No for kids and pregnant women)
Protein Synthesis Inhibitors (2)
- CLINDAMYCIN
a. What does it inhibit?
b. Static/cidal?
c. Coverage?
d. Side effects? - Macrolides:
a. Inhibit what?
b. Static/cidal?
c. Main coverage use?
d. High sTREP RESISTANCE to OLDER Drugs (like what)?
e. side effects? - Chloramphenicol
a. Inhibitor of what?
b. Static/cidal?
c. Spectrum? Includes what?
d. Toxicity?
- a. Protein synthesis (50S)
b. Static
c. Gram + and -, Anaerobes; Protozoa, Acne, MRSA
d. Diarrhea - (AZITHROMYCIN, Clarithromycin)
a. Protein Synthesis (50S)
b. Static
c. Mostly GRAM +
d. Erythromycin
e. Hypersensitivity; GI Effects; Reversible Hepatitis
- a. Protein Synthesis (50S)
b. Static
c. Broad; Including Non-Bacterial Microorganisms
d. Aplastic Anemia
Folate Metabolism Inhibitors
- Sulfonamides (What 4)
a. Static/cidal?
b. Coverage?
c. Oldest what? Problem?
d. Often used in Combo w/what?; Why?
e. Main USE?
f. SIDE EFFECTS?
- TRIMETHOPRIM
a. Static/cidal?
b. Coverage?
c. Mainly used in what?
d. Toxicities mainly Associated with what?
- (SULFADIAZINE, SULFAMETHOXAZOLE, SULFISOXAZOLE, sulfacetamide)
a. Static
b. Gram + and -
c. Oldest ANTIBACTERIAL DRUGS; Widespread Resistance (The Demon under the Microscope)
d. w/TRIMETHOPRIM (more effective. they work together to block sequential steps in FOLATE SYNTHESIS)
e. Treating TOXOPLASMOSIS
f. Nephrotoxicity and Hypersensitivity (Stevens-Johnson Syndrome)
- a. Static
b. Gram + and -
c. in Combos
d. w/Folic Acid Deficiency
DNA Synthesis Inhibitors
- Fluoroquinolones:
a. Cidal/Static?
b. Coverage?
c. Low TOXICITY when used w/what route of administration?
d. Side Effects?
e. What is NEW and has NO ORAL EQUIVALENT?; Why is this good?
f. Indicated for use in what 2 BACTERIAL INFECTIONS?
- *Don’t use 1st Generation anymore; 2nd Gen: OFLAXACIN and CIPROFLOXAXIN
3rd: LEVOFLOXACIN
4th: MOXIFLOXACIN, GATIFLOXACIN, and besifloxacin
a. CIDAL
b. Gram - w/some Gram + coverage in successive generations
c. Topically
d. Destructive Arthropathy (juvenile animal studies, not observed in humans) and TENDONITIS
e. BesiFloxacin; Less chance to develop resistance (so not given orally and never will be)
f. Bacterial Conjunctivitis and Bacterial Keratitis
Common Topical Antibacterials (1)
- Macrolides:
a. Azithromycin (how is it given)
b. Erythromycin - Fluoroquinolones
a. Besifloxacin
b. Ciprofloxacin
c. Gati-
d. Levo
e. Moxi-
f. Oxy- - Aminoglycosides
a. Gentamycin
b. Tobramycin - Bacitracin
- Combos
a. Neosporin
b. Polysporin
c. Polytrim
- a. Drops
b. Ointment - a. Suspension
b. Drops, Ointment
c-f. DROPS - a. Drops, Ointment
b. Drops, Ointment - Ointment
- a. Polymyxin B, Neomycin, Gramicidin; (OINTMENT)
b. Polymyxin B, Bacitracin (Ointment)
c. Polymyxin B, Trimethoprim (DROPS)
Commonly Used Oral Antibacterials
- Penicillins
a. What 2? - Cephalosporins: What one?
- Macrolides: What one? (What’s the BLACK BOX WARNING for?)
- Tetracyclines: What 1?
- Fluoroquinolones: What one (generation 3)
- a. Augmentin (amoxicillin plus clauvanate) and Dicloxacillin
- Cephalexin
- on Z-pack for FATAL ARRYTHMIA
- Doxycycline
- Levofloxacin
General Rules for Antibacterials
- Don’t kill bugs you don’t need to kill
a. so if infection has high probability of being gram positive but not too severe, use drug with what?
b. What does this AVOID?
c. You can always switch to what if necessary? - Don’t use more powerful treatment than needed
a. For mild infections: What may be acceptable?
b. Use what kind of Drugs when possible, to MINIMIZE SIDE EFFECTS?
- Don’t use a Newer generation than needed.
a. Why?
b. Older drugs are GOOD for what?
- a. with Gram + Coverage
b. Avoids Superinfections
c. to a more broad coverage if needed - a. Cytostatic Drugs
b. TOPICAL - a. more often newer drugs are used, the sooner resistance to them will develop
b. for COVER, mild infections (at least as a starting point), and unusual organisms
Antiviral Drugs
- Topical: 2 types
- Oral: FAV
- ALL of them are what ANALOGS?
- a. TRIFLURIDINE (VIROPTIC)
b. GANCYCLOVIR (Zirgan) - a. Famcyclovir
b. Acyclovir
c. Valacyclovir - are Nucleoside analogs
Antifungal Drugs
- Topical: Only one is currently available.
a. Amphoteracin is a better drug to use, but only approved to be used where? - Oral: 2
- NATAMYCIN
a. Off label: in Europe - a. FLUCONAZOLE
b. Voraconazole
Lids, Lashes, Lacrimal, Adnexia, Orbit
- ALL of them are caused by what type of infection?
- Name the 4 we talked about in class? (BC HD)
- Bacterial
- a. Blepharitis
b. Cellulitis (Preseptal and Orbital)
c. Hordeolum
d. Dacrycystitis
Lids, Lashes, Lacrimal, Adnexia, Orbit
Blepharitis
- What is it?
- Most common Pathogens?
a. So mostly what type?
- Bacterial colonization of lid margin, lid glands, or cilia follicles
(can cause lid changes, conjunctivitis, SPK, corneal infiltrates, and phlyctenules) - Staph Aureus (by far), Strep epidermidis, Proprionibacterium Acnes, Moraxella spp.
a. Mainly G + but minor contribution from Gram -
Lids, Lashes, Lacrimal, Adnexia, Orbit
Blepharitis Treatment (BAD)
- Bacitracin: What is it?
a. Good for coverage of what?
b. Can put directly into what? - Azythromycin 1% (DROP)
a. How many drops per day?
b. Works on what bacteria?
c. May also help restore what? - Doxycycline (100 mg, po, qd), Tetracycline (250 mg, po, qd)
a. Static/Cidal
b. Use this dosage for how long? Then taper to what?
c. Mainly used for what?
d. works on what?
e. Problem?
4. Older macrolides and Tetracyclines can be used, but they have limited effectiveness due to what?
- Ointment (1/2’’, qhs); CWI, CIDAL
a. Gram + and some -
b. onto lids
- Macrolide, PSI, Static
a. 1 drop bid for first 2 days, then once DAILY for next 12 DAYS
b. Gram + and Negative; Covers all major bacterial causes!
c. Lipid in meibomian glands to more normal State (anti-lipase activity)
3. a. Static, PSI
b. 1-2 weeks; then taper to 1/4 dose for 6 MONTHS
c. Anti-Lipase Activity
d. Gram + and Negative Effects, but Significant resistance has developed
e. SEE d.
4. Resistance
Lids, Lashes, Lacrimal, Adnexia, Orbit
Non-Drug Blepharitis Tx
- Lowers Bacterial Burden?
- Decreases VISCOSITY of meibum encouraging outflow and renewal
- Also encourages renewal of meibum
- LID SCRUBS
- WARM COMPRESSES
- EXPRESSION of MEIBOMIAN GLANDS
Lids, Lashes, Lacrimal, Adnexia, Orbit
Hordeolum
- Infection of what?
a. External: Associated with what?
b. Internal: Associated with what? - Most COMMON PATHOGENS? (2)
- Sebaceous glands
a. associated w/Cilia
b. w/Meibomian Glands - Staph Aureus and Staph Epidermidis (GRAM POSITIVE)
Lids, Lashes, Lacrimal, Adnexia, Orbit
Hordeolum Treatment
- Topically treated with 1 of 2 drugs?
a. External Hordeolum: Apply ointment to Lid margin to do what?
b. Internal Hordeolum: Apply Antibiotic Ointment to Cul-De-Sac as what kind of Tx against CONJUNCTIVITIS in case of SPONTANEOUS RUPTURE
c. Older, less potent drugs are useful? If so, Why?
2. If you want to actually treat it, GIVE them ORAL what? (3 things possible)
a. For cases that don’t respond to what Tx?
b. Oral Route will get more drug to what locations?
c. Supply primarily G+ effects (extended for what oral drug)
a. Don’t want to necessarily kill what kind of bacteria in this case?
- Bacitracin (CWI, CIDAL) or Erythromycin (Macrolide, PSI, Static)
a. REDUCE BACTERIAL LOAD
b. PROPHYLAXIS against those things…
c. Resistance is less important so yes…purpose of these is to reduce it…doesn’t actually treat the actual infection! - ORAL DICLOXACILLIN (penicillin, CWI, CIDAL), CEPHALEXIN (Cephalosporin, CWI, CIDAL), or AUGMENTIN (PENICILLIN w/CLAUVANATE, CWI, CIDAL)
a. to Topical Tx
b. to deeper locations
c. a. Gram Negative bacteria (Systemic)
Lids, Lashes, Lacrimal, Adnexia, Orbit
Non-Drug Hordeolum Tx
- Main thing to do?
a. How long?
b. Purpose?
c. If if persists, it may give rise to what 2 things that are harder to treat?
- Warm Compresses, 10 min, qid, w/light massage over hordeolum
a. 10 m qid.
b. get lesion to point and DRAIN
c. Chalazion or Pyogenic Granuloma