PDA Block 3 Week 2 Flashcards

(96 cards)

1
Q

Penicillin

A
Penicillin G and V
Oxacillin
Amipicillin, amoxicillin
Ticarcillin
Piperacillin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Penicillin

A
  • Well distributed to most area of the body: low penetration into CSF but increases during Meningitis
  • 30% hepatic metabolism
  • mostly renal: 80% tubular anionic excretion
  • Time dependent killing
  • Adverse effect: Severe allergic reactions→ anaphylaxis (Pre-Pen for testing); Rash, diarrhea, enterocolitis, elevated liver enzymes, hemolytic anemia, seizures
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Beta lactamase inhibitors

A

Clavulanic acid, tazobactam (beta-lactam analogs that bind irreversibly to beta-lactamase)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Cephalosporin

A

Cefazolin: 1
Cephalexin: 1

Cefuroxime: 2
Cefoxitin: 2

Ceftriaxone: 3
Ceftazidime: 3

Cefepime: 4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Penicillin G and V

A

Oral: Pen V and IV/IV= Pen G(poor Oral- not stable to Acid)
G+ Anaerobes: Clostridium (Not Bacterioides fragilis)

G+: Streptococcus

Limited G-: Some use in Neisseria meningitides
Spiochetes: Syphillis

Good activity against: anthrax, Listeria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Oxacillin

A

“methicillin like drug” Beta lactamase producing staphylococci

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Amipicillin, amoxicillin

A

IV or oral
Amoxicillin: better after oral dose

Ampicillin: IV (for Neisseria, Listeria) and GI infections (keep more drugs in intestinal tract for Shigella infx)

G+ Beta-lactamase negative: listeria, Strep
G-: haemophilus, Neisseria, E. Coli, Salmonella

Amoxicillin: Alternate choice for Lyme disease
High dose amoxicillin is drug of choice for otitis media – Strep. Pneumo strains

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Ticarcillin

A

Retain some G+ against Strep
Anaerobes: ticararillin +Clavulanate

G- to cover pseudomonas ( susceptibile to beta lactamase)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Piperacillin

A

G- including pseudomonas and Klebsiella, including those that are ticarcillin resistant)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Cefazolin

A

Longer half life (1-2 hrs)
Best G+ activity.
Surgical prophylaxis for skin flora

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Cephalexin

A

Oral
Half life: 50 min
Mostly G+
Skin, bone/joint, UTI, respiratory, otitis media

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Cefuroxime

A
  • CSF penetration
    Haemophilus
    Not good against enterics (E. Coli)
  • Good tolerance to many gram negative beta lactamase
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Cefoxitin

A
  • Not for CNS

- Good for anaerobes (Bacteroides) Good tolerance to many G- beta lactamases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Ceftriaxone

A
  • CSF, Long half life
  • G-: Klebsiella, Enterobacter, proteus

Meningitis (Neiserria, S. pneumo, H. influenzae)

Only choice for gonorrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Ceftazidime

A
  • CSF
  • Good for some strains of Pseudomonas
    Not great for Strep
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Cefepime

A
  • CSF
  • Half life 2 hours
  • G- with pseudomonas activity
  • more resistant to type I beta-lactamases
  • Better for G+ (Strep)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Cephalosporin

A
  • Cell- wall agent
  • Bactericidal
  • Inhibit transpeptidases
    (penicillin binding proteins or PBPs) which catalyze cell wall
    crosslinks
  • B- lactam covalently binds to PBPs
  • Time dependent killing
  • Renal clearance
  • Adverse reaction: allergic, N/V/D, enterocolitis, hepatocellular damage
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Beta Lactams

A

-Cell wall agent
- Bactericidal
- Inhibit transpeptidases
(penicillin binding proteins or PBPs) which catalyze cell wall
crosslinks

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Bacterial resistance to B- lactams

A
  • Beta- lactamase: enzyme that cleaves beta-lactam ring
  • altered PBP
  • Beta-lactam agent cannot reach PBP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Imipenem

A
  • Cell wall agent
  • Broad spectrum: resistant to many beta lactamases including extended spectrum beta-lactamase
  • Not for meningitis
  • Not effective for MRSA, pseudomonads
  • Ill defined infections

Adverse effects: - Hypersensitivity, some cross allergies with penicillins/cephalosporins

  • Seizures, dizziness, confusion
  • Nausea, vomiting, diarrhea, colitis, superinfection
  • Given with cilastatin: renal peptidase inhibitor
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Aztreonam

A
  • Used against G- aerobic rods (Haemophilus, Pseudomonas)
  • Adverse: seizures, anaphylaxis, can affect heart= transient EKG changes, cramps, nausea
  • No allergic cross-reactions with beta-lactams. Can be used in those with known hypersensitivities to penicillin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Vancomycin

A
- Bactericidal
G+ only (serious infxn!)
- Staph including MRSA
- Strep. Pneumonia
- Enterococcus (VRE)
- Clostridium difficile enterocolitis ( don’t want to overuse)

Inhibits cell wall synthesis: binds to D-Ala-D-ala → interfers with crosslinking and elongation of peptidoglycan (transglycosylation)

  • Red man or red neck syndrome: head and neck erythema
  • Nephrotoxicity
  • Phlebitis (infusion site)
  • Ototoxicity
  • Hypersensitivity
  • Not absorbed → IV administration for systemic infections
  • Primarily used in serious infection
  • use oral for clostridium diff. enteroocolitis

-Cephalosporin tolerance strains: use vancomycin + 3rd gen cephalosporin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Fosfomycin

A
  • Use: uncomplicated UTIs caused by E.coli, & Enterococcus.
  • inhibits synthesis of peptidoglycan building blocks by inactivating enolpyruvyl transferase, (early cell wall synthesis enzyme)- new cell wall of dividing bacteria → rupture
  • Adverse: headache, diarrhea, nausea, vaginitis
  • Single dose effective for treating UTIs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Bacitracin

A
  • Gram + Cocci and bacilli
  • Mechanism: interferes with a cell wall synthesis by interfering with lipid carrier that exports early wall components through cell membranes
  • Toxicity: allergic dermatitis
  • Use: topical use only (very nephrotoxic)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Cell- wall agents
``` Penicillin G and V Oxacillin Amipicillin, amoxicillin Ticarcillin Piperacillin Cefazolin Cephalexin Cefuroxime Cefoxitin Ceftriaxone Ceftazidime Cefepime Imipenem Aztreonam Vancomycin Fosfomycin Bacitracin ```
26
Cell Membrane agents
Polymyxin & Daptomycin
27
Polymyxin B
Bind LPS in outer membrane of G- - G- spectrum (pseudomonas) - Topical use
28
Daptomycin
Binds to bacterial cytoplasmic membrane - bactericidal - G+ ONLY - Staph aureus (MSSA, MRSA) - Strep pyogenes - Enterococcus - Staph bacteremia Adverse: - Nausea, diarrhea, GI flora alteration - muscle pain and weakness (monitor CK levels) - Used for complicated skin and skin structure infections - not for lung infections
29
Nucleic Acid agents
``` Norfloxacin Ciprofloxacin Moxifloxacin Nitrofurantoin Rifampin Fidaxomicin Metronidazole ```
30
Quinolones
- Bactericidal - inhibits alpha subunit of DNA gyrase (interfers with control of DNA unwinding) Adverse effects - N/V/abdominal pain, enterocolitis - dizziness, headache, restlessness, depression - seizure - rash- photosensitivity - EKG irregularities, arrhythmia - peripheral neuropathy - arthorpathy/tendon rupture Precautioned: seizure disorder, pregnancy, children
31
Fluorinated Quinolones
Norfloxacin Ciprofloxacin Moxifloxacin
32
Non Fluorinated Quinolones
- used for Enterobacteriacea in urinary tract
33
norfloxacin
urinary tract infections: Enterobacteriaceae
34
Ciprofloxacin
- UTI - infectious diarrhea (shigella, campylobacter), - bone and joint infection (enterobacter) - Skin infections - Chlamydia
35
Moxifloxacin
G+ activity - respiratory infections (p. pneumonia, mycoplasma, legionella) - not for strep throat - Community acquired pneumonia - bacterial bronchitis
36
Nitrofurantoin
- Nitroreductase enzyme converts them to reactive compounds→ damage DNA - UTI Adverse effects: - nausea, vomiting, diarrhea - peripheral neuropathy - hypersensitivity, fever, chills - acute/ chronic pulmonary reactions, - acute and chronic liver damage - Granulocytopenia, leukopenia, megaloblastic anemia - acute hemolytic anemia
37
Rifampin
- inhibits bacterial RNA synthesis by binding RNA pol B - Bactericidal - used for treatment of pulmonary Tuberculosis - prophylaxis for meningococcal meningitis - prophylaxis of H. influenza type b meningitis Adverse: - serious hepatotoxicity - induces hepatic enzymes ( many CYPs), - orange color ( urine, saliva)—very lipophilic
38
Fidaxomicin
- Non-competitive inhibitor of RNA polymerase (inhibits RNA synthesis) - Bactericidal - oral, poorly absorbed Use: C. Diff infection Adverse: GI upset, GI bleeding
39
Metronidazole
Anaerobes reduce the nitro group of metraonidazole→ disrupts DNA - bactericidal Use: Anaerobes, C. Diff, combo therapy for H, pylori, gardenerella vaginalis Adverse: - n.v. anorexia, diarrhea, transient leukopenia, neutropenia, thrombophlebitis after IV infusion, bacterial and fungal superinfections (candida)
40
Protein Synthesis inhibitors
``` Gentamicin Tobramycin Amikacin Doxycycline Minocycline Tigecycline Chloramphenicol Erythromycin Clarithromycin Azithromycin Clindamycin Linezolid ```
41
Aminoglycoside drugs
Gentamicin Tobramycin Amikacin
42
Aminoglycosides Properties
- Only Bactericidal protein synthesis inhibitor - Not absorbed orally, given IV or IM - Glomerular filtration - concentration dependent killing Mechanism: - Penetrate pores of outer membrane - Bind to transport molecule on outer of surface of cytoplasmic membrane - Transported into cell - Bind to several ribosomal sites→ stops initiation→ causes pre-mature release of ribosome from mRNA and mRNA misreading -Primary for G- aerobic bacilli (Enterobacteriaceae, Pseudomonas) ``` Adverse: - Nephrotoxicity: usually reversible - Ototoxicity: both auditory and vestibular damage Related to dose of therapy - Neuromuscular blockage ```
43
Gentamicin
Pseudomonas, Klebsiella, Enterobacter
44
Tobramycin
Pseudomonas, Klebsiella, Enterobacter
45
Amikacin
For some gentamicin & tobramycin resistant strains
46
Tetracycline
- transported into the cell by a protein carrier system - Bind to 30S ribosomal subunits, prevent attachment of aminoacyl-tRNA to the acceptor site on the MRNA-ribosomal complex→ amino acid cannot be added to the protein being synthesized - Bacteriostatic - Use: Rickettsia, Chlamydia, mycoplasma, Ureaplasma, Borrelia (Lyme) - calcium (bivalent cation) binds to tetracycline→ inhibits absorption (do not take with antacids and Ca2+ containing foods) Adverse: - Gastrointestinal disturbance: pseudomembranous enterocolitis - Candida superinfection in colon - Photosensitization with rash—sunlight makes rash worse - Teeth discoloration—avoid use in children (<8) - Contraindicated in pregnancy
47
Doxycycline
- Tetracycline Use: Patients with impaired renal function Alternative for - PenG sensitive syphilis - Uncomplicated N. gonorrhoea -Least affinity for calcium
48
Minocycline
Use: Prophylaxis of Neiss. meningitidis Alternative for - PenG-sensitive syphilis; - uncomplicated gonorrhea - Calcium binding: moderate
49
Tigecycline
- Bacteriostatic - Binds 30S ribosomal subunit and blocks aminoacyl-tRNA entry Use - Skin/Skin structure infections - Complicated intraabdominal infections - Community acquired pneumonia (CAP) 1. G- :E. coli, Citrobacter, Klebsiella, Enterobacter NOT pseudomonas 2. G+: Staphylococcus (MSSA and MRSA) 3. Anaerobes: Bacteroides & Clostridium perfingens 4. CAP: S. pneumonia, Haemophilius Adverse - N/V - increase risk of death
50
Chloramphenicol
Interferes with binding of aminoacyl-tRNA to 50S subunit and inhibits peptide bond formation - Broad spectrum of activity - Alternate agent for treatment of meningitis in beta lactam allergic patients (cephalosporin) - Brain abscesses (anaerobes) Adverse reactions: - Bone marrow depression→ can progress to a fatal aplastic anemia (can be delayed) - Grey baby syndrome: vomiting, pallor, cyanosis, circulatory collapse - high levels of unmetabolized drug due to lack of phase II enzymes - Optic neuritis and blindness hypersensitivity- GI effects (enterocolitis)
51
Macrolides
- Bind to a 50S ribosomal subunit→ block protein synthesis by blocking translocation along ribosome - Bacteriostatic
52
Erythromycin
- Macrolid - Primarily against G+ (strep in penicillin-allergic pts); Also good for atypical bugs: chlamydia, mycoplasma, Legionella, Bordetella - Very fast N/V (due to enhanced motility); inhibits CYP 3A4 metabolism/excretion of many drugs; increase risk of arrhythmia and cardiac arrest (esp with CYP3A4)
53
Clarithromycin
- Macrolid - Alternative to erythromycin for treatment of pharyngitis, respiratory infections. Also: like erythromycin: mycoplasma, legionella, Bordetella. Haemophilus, Moraxella, penicillin-resistant Strep pnemo. Helicobacter & atypical mycobacterial infections. 3 drugs combos: 2 ABX +acid blocker - Less GI effects than Erythromycin. Some CV risk (Prolonged QT) interval
54
Azithromycin
- Macrolid - Respiratory infections (strep pneumo, Haemophilis, mycoplasma, Moraxella & chlamydia, Neisseria gonorrhoae (Ceftriaxone + azithromycin) - Less GI effects than Erythromycin. Some CV risk (Prolonged QT) interval Fewer GI disturbances than w/ erythromycin, fewer drug interactions, Cardiac (prolonged QT)
55
Clindamycin
macrolide-like mechanism: binds to 50S ribosomal subunit - Inhibits most G+ cocci (Strep & MSSA) and many anaerobes including Bacteriodes fragilis - Not for hospital acquired MRSA, enterococcus, or G- aerobes Adverse Rxn - Antibiotic-associated enterocolitis—Associated with C. diff - GI irritation, diarrhea - Hepatotoxicity
56
Linezolid
- Macolid - interferes with protein synthesis, binds 50S subunit→ interferes with 70s initiation complex - Use: G+ spectrum - VRE: vancomycin resistant Enterococcus - s taphylococcus auerus (MRSA, MSSA- alterative to vancomycin) - Streptococcus, group A and B - Streptococcus pneumonia (including multi-drug resistant) Side effects - Non-selective inhibitor of MAO (avoid foods with tyramine)-Contraindicated in SSRI, tricyclics - Diarrhea, headache, n/v, bone marrow suppression
57
Anti-folates agents
Sulfamethoxazole sulfadiazine Tripmethoprim
58
Sulfonamide
- Anti-folate - inhibit folate synthesis by competitive inhibition of dihydropteroate synthase - Sulfamethoxazole + Trimethoprim for UTI,
59
sulfadiazine
- Anti-folate ( dihydropteroate synthase) | - Silver sulfadiazine: topical for burn patients
60
Tripmethoprim
- inhibits folate synthesis by competitively inhibiting dihydrofolate reductase - sulfamethoxazole (Bactrim)= synergistic effect is bactericidal-- Uncomplicated urinary infections—most common use Adverse effects of trimethoprim-sulfa combination 1. Sulfonamide side effects 2. N/V, diarrhea, rashes 3. Eosinophilia, neutropenia, bone marrow suppression 4. Especially pronounced in AIDS patients
61
Hospital acquired MRSA Treatment
``` IV Vancomycin linezolid daptomycin tigecycline ```
62
Community Acquired MRSA
``` Oral Linezolid doxycyclin minocycline clindamycin TMP-SMX ```
63
Tuberculosis Treatment
- Caused by M. tuberculosis | - Rx: isoniazid, Rifampin, Ethambutol, Pyrazinamide, Streptomycin
64
Isoniazid (INH)
Bactericidal for actively growing cells, -static for resting cells. - inhibits synthesis of mycolic acids. - pro-drug that is activated by catalase-peroxide (KatG protein) of tubercle bacillus. Activated drug targets enoyl-acyl carrier protein reductase InhA protein ( important for FA elongation and interferes with DNA synthesis. Resistance: results from mutations in KatG or InhA - Primary TB drug. Patients with INH-sensitive strain should receive INH if possible. - Give in combination with other agent - oral - antacids interfere with absorption - N- acetylation is under genetic control: Slow= half-life: 2-5 hours. Fast half life= 70 min -Neurotoxicity (peripheral neuritis)- impoved with B6 Adverse - hepatotoxicity: correlated with increased age. Possible caused by metabolite of IHN
65
Rifampin
- Inhibits bacterial DNA-dependent RNA polymerase (suppresses RNA synthesis). - Bactericidal for intra and extracellular organisms - Used with INH. Not used alone - limited penetration into CSF - metabolized in liver by deacetylation Adverse: - Hepatotoxicity: can be severe in alcoholics - inducer of CYPs (increase metabolism of other drugs—oral contraceptives, digoxin, warfarin) - orange/red color to urine, feces, saliva, tears, sweat, sputum
66
Ethambutol
- interferes with arabinosyl transferase→ blocks cell wall synthesis - Tuberculostatic: spontaneous resistance occurs 1 in 106 -Use in conjunction with other drugs (INH) - well absorbed, adequate levels in CNS - half life: 3-4 hours - Adverse: well-tolerated -not hepatotoxic -optic neuritis→ decrease in visual acuity, loss ability to differentiate red from green
67
Pyrazinamide
- Blocks mycolic acid synthesis by inhibiting fatty acid synthase I - Bactericidal -combo therapy - important part of short term multi-drug therapy -widely distributed including CSF Adverse: -Hepatic damage: may be fatal w/rifampin
68
Streptomycin
-binds to several ribosomal sites: stops initiation and causes mRNA misreading -reserved for most serious forms of TB (disseminated disease) - IM administration - No CNS penetration - Adverse: - ototoxicity - nephrotoxicity
69
MAC Rx
M. avium-intracellulare Ex: Rifabutin & Clarithromycin
70
Rifabutin
- Rifampin analog for single agent prophylaxis of MAC in AIDs pts. (rec. for low CD4 counts) - multi-drug treatment of MAC Adverse: - similar to rifampin but less frequent ( Hepatotoxicity, inducer of CYPs, orange/red body fluids)
71
Clarithromycin
- part of multi-drug regimen for MAC - MAC prophylaxis - Bactericidal
72
Leprosy Rx
Dapsone Clofazimine Rifampin
73
Dapsone
- structural analog of p-aminobenzoic acid (PABA)→ inhibits synthesis of folic acid - bacteriostatic - used in combination with other drugs (ie. Rifampin) - prophylaxis (&treatment) of Pneumocysitis jiroveci in AIDS pts. - oral - metabolized by same enzymes that acetylates INH: slow and fast acetylators Adverse: - Hemolytic anemia - methemoglobinemia
74
Clofazimine
- binds to mycobacterial DNA interfering with reproduction and growth - used in combo chemotherapy (often for sulfone resistant leprosy -oral - highly lipophilic (long half life: ~2 mo) Adverse: - generally well tolerated - cause red/brown pigmentation of skin, sweat
75
Systemic Fungal Infections Rx
``` Amphotericin B Flucytosine Caspofungin Fluconazole Itraconazole Voriconazole ```
76
Superficial Fungal Rx
``` Fluconazole Miconazole Clotrimazole Itraconazole Nystatin Amphotericin B ```
77
Ophthalmic Fungal Rx
Natamycin
78
Dermatophytic infections Oral Rx
Terbinafine Griseofulvin Itraconazole
79
Amphotericin B
- Very lipophilic, binds ergosterol in fungal membranes producing membrane instability/leakage. - effective for most serious systemic mycoses - effective against candida, Histo, crypto, blasto, sporothrix, Coccidiodes - - IV for 6 to 12 weeks - NOT absorbed from GI - Total cumulative dose is impt for renal toxicity - limited CNS penetration - Adverse: Fever, nausea, vomiting, headache, chills, hypotension, hypokalemia, tachypnea, 90% will show non-permanent nephrotoxicity→ enhances toxicity of renally excreted drugs. – can cause permanent renal damage (total drug dose) –reversible hypochromic, normocytic anemia
80
Flucytosine
-fungi contain a cytosine deaminase that converts 5FC→ 5FU. Metabolites of 5FU block nuclei acid synthesis - use: serious infection due to Candida, Cryptococcus - used with amphotericin -oral - when given with amphotericin→ allows reduction of amphotericin dose Adverse: - N/V, diarrhea, enterocolitis, leukopenia, thrombocytopenia - reversible elevated hepatic enzyme - use extreme caution in those with renal insufficiency or bone marrow depression
81
Caspofungin
- inhibits cell wall synthesis by non-comptitively blocking synthesis of Beta (1,3) glucan→ cell lysis - uses: Invasive Aspergillus in pt intolerant of other drugs - Candida, esophageal and systemic - IV - does inhibit P450 - Adverse generally well tolerated -fever, n/v, rash -phlebitis at infection site
82
Imidazole/Triazole Mechanism of action
inhibit sterol 14-alpha sterol demthylase (fungal P450)→ blocks conversion of lanosterol to ergosterol (fungistatic) Fluconazole Itraconazole Voriconazole
83
Fluconazole
- Cryptococcus meningitis - some Candida - oral - Excellent CNS penetration -excreted unchanged in urine Adverse -N/V/rash/Diarrhea/headache -hepatotoxicity: inhibits metabolism of several drugs
84
Itraconazole
- Blastomyces - Histoplasma - Candida, esophageal and oropharyngeal - No CNS penetration - Metabolized in liver Adverse: - N/V/rash/Diarrhea/headache - hepatotoxicity: inhibits metabolism of several drugs - contraindicated w/drugs that inhibit CYP3A4
85
Voriconazole
- invasive Aspergillus (-cidal), scedosporium - extended Candida spectrum - possibly some CNS entry - metabolized in liver - Adverse: N/V/rash/Diarrhea/headache -hepatotoxicity: inhibits metabolism of several drugs -visual disturbances, photosensitive rash -contraindicated with st. johns wort (p450 inducer)
86
Miconazole
- cream/suppository for vaginal candidiasis -topicals—burning, itching, irritation
87
Clotrimazole
- oral or vaginal candidiasis - Topical: oral torches, vaginal tablets, topical creams/solutions -oral form: may cause abnormal liver function test
88
Itraconazole
oropharyngeal and esophageal candidiasis
89
Nystatin
- almost exclusively for Candida of skin, mucous membrane, GI, vaginal - Mechanism similar to amphotericin B -oral: GI distress
90
Amphotericin B
- binds ergosterol - topical for cutaneous or mucodal candida - not effective against dermatophytes - topical: hypersensitivity but no systemic toxicity
91
Natamycin
- Use: fungal eye infections eg. Conjunctivitis - Fusarium, Cephalosporium, Aspergillus Mechanism similar to amphotericin B - Might be used in conjunction with surgical measures Toxicity: conjunctival chemosis and hyperemia
92
Terbinafine
- use: 12 week therapy for nail infections, shorter for other dermatophyte infection - Inhibits fungal squalene eposidase; non-competitively - Accumulation of squalene damages fungal cell membrane - Fungicidal - oral - remains in skin 12 weeks after therapy stopped - Adverse: diarrhea, dyspepsia, abdominal pain
93
Griseofulvin
- recalcitrant infections of skin, hair, nails, beyond scope of topical therapy - therapy for children w/ tinea capitis - Mechanism: slowly deposited into skin, hair, nails→ interferes with microtubule fuciton/mitotic spindle/mitosis (arrest cell cycle) - oral - use with topical Adverse: - contraindicated for pt with porphyria and advanced liver disease - increase metabolism of other drugs (oral contraceptives, warfarin) - Caution: penicillin allergies
94
Itraconazole
- 3 mo therapy for toenail infections - oral - N/V/ rash/diarrhea, headache, edema - discontinue if signs of liver infections appear -inhibits metabolism of many drugs (digoxin, cyclosporine, warfarin)
95
Topical preparations or treatment of common skin, hair, nail infections
- Miconazole - Clotrimazole - Tolnaftate: (tinactin)- cream/solution or foot spray or powder - Terbinafine: topical for dermatophytes - Ciclopirox: lacquer is only topical Rx for fungal nail infections
96
Ciclopirox
lacquer is only topical Rx for fungal nail infections