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30 Cards in this Set
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Nystatin (Mycostatin)
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Class: Polyene
MOA: Stops ergosterol synthesis. Ergosterol is part of the fungal cell membrane. Forms a pore in the membrane so contents leak out and cell bursts. Indication: Drug of choice for fungal infections of the oral cavity Broad spectrum of activity- Candida, Histoplasmosis, Cryptococcus Used prophylactically in immunocompromised patients Not absorbed from skin or mucosal membranes (GI Tract) Too toxic for parenteral use, only used topically Drug of choice for pts with liver disease or alcoholism For extensive disease: Ketoconazole or fluconazole with Nystatin Dosage forms: Oral Suspension 100,000 u/mL -5mL S and S 5x/day Lozenges 200,000 units -Dissolve completely in mouth (do not chew or swallow whole) 5x/day NPO ½ hour after use -Both treatments usually last 14 days -Patients say it has a bitter, foul taste |
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Clotrimazole (Mycelex)
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Class: Imidazole
MOA: Stops ergosterol synthesis. Ergosterol is part of the fungal cell membrane Binds to the oral mucosa, gradually released, fungistatic concentrations for several hours Indication: Candidiasis, fungal infections Dosage: Troches 10 mg Dissolve completely in mouth (do not chew or swallow whole) 5 times per day NPO ½ hour after use Only used topically because not absorbed from the GI tract ^Binds to the oral mucosa, gradually released, fungistatic concentrations for several hours^ Patients report that it tastes better than nystatin |
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Ketoconazole (Nizoral)
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Class: Imidazole
MOA: Stops ergosterol synthesis. Ergosterol is part of the fungal cell membrane Binds to the oral mucosa, gradually released, fungistatic concentrations for several hours Indication: Candidiasis, fungal infections Dosage: Can be used topically (cream 2 %) or orally (tablets 200 mg) Well absorbed from the GI tract in conditions of low pH Drug interaction with drugs that increase the pH of the stomach Dose: 1 tab qd with orange juice or a meal for 14 days Adverse Effects: hepatoxicity (0.01 %) Inhibits synthesis of testosterone and estradiol Inhibitor of Cytochrome p450 3A4 -Cyclosporin -Phenytoin -Sulfonylureas -Warfarin |
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Fluconazole (Diflucan)
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Class: Triazole
MOA: A triazole derivative: more selective inhibitor of fungal cell membrane p450 Adverse Effects: GI upset, less hepatoxicity than ketoconazole Weak inhibitor of p450 3A4: fewer drug interactions Uses: Candidemia, osteomyelitis, meningitis -Therapy for 3-6 months -Life long in HIV patients -Prophylaxis in bone marrow transplant Dosage: Tablets 100 mg -2 tabs stat, then 1 qd for 13 days Suspension 50 mg/5 mL -Rinse mouth with 20 mL on day 1 for 1 minute then swallow Repeat with 10 mL qd for 14 days total IV form: Uses: Candidemia, osteomyelitis, meningitis -Therapy for 3-6 months -Life long in HIV patients -Prophylaxis in bond marrow transplant Resistance Decreased susceptibility -correlate with treatment failure in HIV positive patients Fluconazole resistant fungi are cross resistant to other azole antifungal agents |
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Itraconazole (Sporanox)
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Class: Triazole
MOA: Significant inhibitor of p450 3A4 If infection is resistant to nystatin, ketoconazole, fluconazole Resistance in Candida species isolated from patients on prolonged therapy Dosage: Capsules 100 mg and suspension 10 mg/mL Take 1 capsule bid Rinse mouth with 20 mL for 1 minute qd then swallow and continue for 14 days |
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Iodoquinol
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Class: hydroxyquinoline
Halogenated hydroxyquinoline with amebicidal, antitrichomonal, antibacterial and antifungal activity MOA: Chelates trace metals at bacterial surfaces that are essential for growth Indications: angular cheilitis Dosage forms: 1 % topical cream with 1 % hydrocortisone Apply to affected areas after each meal and hs |
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Oral Candidiasis in immunocompetent patients
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1. Clotrimazole Lozenges 10 mg
2. Nystatin Lozenges 200,000 units -Dissolve slowly in mouth (do not chew or swallow whole) 5 times per day -NPO ½ hour after use 3. Fluconazole tablets 150 mg -Take one tablet po stat |
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Oral Candidiasis in immunocompromised patients or mucocutaneous candidiasis
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1. Fluconazole Oral Suspension 50 mg/5 mL
2. Itraconazole Oral Suspension 10 mg/ mL -Rinse mouth with 20 mL for 1 minute then swallow qd and continue for 14 days 3. Fluconazole tablets 100 mg -Take 2 tablets stat, then 1 tablet qd for 13 days |
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Chronic atrophic candidiasis associated with a denture
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1. Nystatin Cream 100,000 u/g
2. Clotrimazole Cream 1 % 3. Ketoconazole Cream 2 % -Apply thin coat of medicine to entire inner surface of denture after each meal for 14 days Full strength bleach: only for dentures without metal -Soak for 10 minutes once a week then rinse well Anti-fungal Vaginal tablets -Dissolve tablet in water, soak denture for 10 minutes |
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Amphotericin
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Class: Polyene
Mechanism is identical to Nystatin Binds to cholesterol in plasma membranes Most toxic antibiotic in current use: given over a period of 2-6 hours Adverse Effects: Hypotension, delirium, fever, nausea, vomiting, abdominal pain, anorexia, headache, nephrotoxicity AKA “amphoterrible” Premedicate with Benadryl, Tylenol, and dexamethasone |
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Caspofungin
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Class: Echinocandin
Inhibition of glucan synthase Enzyme is present in fungal cells not mammalian cells Inhibition synthesis of 1,3-β-D-glucan -Essential component of fungal cell walls Candidemia, invasive aspergillus, candida abscesses, deep tissue infections, refractory or invasive infections |
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Anidulafungin
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Class: Echinocandin
Inhibition of glucan synthase Enzyme is present in fungal cells not mammalian cells Inhibition synthesis of 1,3-β-D-glucan -Essential component of fungal cell walls Candidemia, invasive aspergillus, candida abscesses, deep tissue infections, refractory or invasive infections |
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Micafungin
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Class: Echinocandin
Inhibition of glucan synthase Enzyme is present in fungal cells not mammalian cells Inhibition synthesis of 1,3-β-D-glucan -Essential component of fungal cell walls Candidemia, invasive aspergillus, candida abscesses, deep tissue infections, refractory or invasive infections |
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Flucytosine
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Class: antimetabolite
Po only Metabolized to 5-FU, cancer drug Then to 5-F-dump: inhibits DNA synthesis Then to 5-FUTP: inhibits RNA synthesis Cryptococcal endocarditis or meningoencephalitis |
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Posaconazole
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Class: triazole
Your future Once itraconazole is resistant Same mechanism of other triazole anti-fungals Candida prophylaxis in immunocompromised patients Treatment of refractory or invasive fungal infections |
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Voriconazole
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Class: triazole
Your future Once itraconazole is resistant Same mechanism of other triazole anti-fungals Candida prophylaxis in immunocompromised patients Treatment of refractory or invasive fungal infections |
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Acyclovir
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Class: Polymerase inhibitor
MOA: Guanosine analog (2 carbon atoms missing from ribose, no –OH for polymerase rxn) Selective phosphorylation: Basis for selectivity of drug for virus infected cells 3000 fold greater concentration required to inhibit non-infected cell growth Dosage: Ointment: -Symptomatic relief of recurrent herpes labialis Oral Prophylaxis and treatment primary and recurrent of genital herpes Preventing reactivation in immunosuppressed patients Bioavailability: 20 % dose is 200 mg 5 x’s/day Drug resistance: Loss of viral thymidine kinase activity Elaboration of a viral thymidine kinase with altered substrate specificity Expression of altered DNA polymerase activity |
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Valacyclovir
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Class: Polymerase inhibitor
Greater bioavailability than Acyclovir MOA: Guanosine analog (2 carbon atoms missing from ribose, no –OH for polymerase rxn) Selective phosphorylation: Basis for selectivity of drug for virus infected cells 3000 fold greater concentration required to inhibit non-infected cell growth Indications: Herpetic gingivostomatitis Recurrent intraoral herpes simplex Herpes labialis Herpes zoster Dosage: Ointment: -Symptomatic relief of recurrent herpes labialis Oral Prophylaxis and treatment primary and recurrent of genital herpes Preventing reactivation in immunosuppressed patients Bioavailability: 54 % dose is 2G q12h |
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*Ganciclovir (Cytovene)
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Same mechanism as acyclovir
Same specificity for viral thymidine kinase Inhibits viral DNA polymerase More potent than acyclovir against HSV, CMV and VZV Used for acyclovir resistant HSV infections Adverse effects: aspermatogenesis, carcinogenic and teratogenic Ganciclovir: always iv Valganciclovir: oral form 900 mg once daily with food |
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Penciclovir (Denavir)
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Class: Polymerase inhibitor
MOA: Inhibits HSV polymerase competitively with deoxyguanosine triphosphate Indicated for HSV-1 and HSV-2 Off-label varicella-zoster Dose- Apply every 2 hours while awake for 4 days. Treatment should be started as early as possible (during prodrome phase) ½ day shorter duration of disease |
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Valganciclovir
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Class: Polymerase inhibitor
Same mechanism as acyclovir Same specificity for viral thymidine kinase Inhibits viral DNA polymerase More potent than acyclovir against HSV, CMV and VZV Used for acyclovir resistant HSV infections Adverse effects: aspermatogenesis, carcinogenic and teratogenic Ganciclovir(Cytovene): always iv Valganciclovir: oral form 900 mg once daily with food |
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Abreva
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Class: Fusion inhibitor
Over the counter so you can recommend MOA: inhibits fusion between the human cell membrane and HSV— Prohibits entry into human cell Directions for use: apply 5 x’s/day starting at the early stage (redness) to stop progressing to the blister stage One day shorter Use a maximum of 10 days |
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Enfuvirtide (Fuzeon)
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Class: entry inhibitor
MOA: Gp41 initiates fusion of the virus into the lymphocyte cell surface Binds to the first heptad repeat in the gp41 subunit of the viral glycoprotein Prevents conformational changes Evidence of HIV-1 replication despite ongoing antiretroviral therapy Resistance: Substitutions in the aa’s in the gp41 protein Indication: HIV |
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Maraviroc (Selzentry)
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Class: entry inhibitor
MOA: Selectively and reversibly binds to the CCR5 coreceptor located on human CD4 cells Prevents interaction between the human CCR5 coreceptor and the gp120 subunit of the viral envelope glycoprotein Inhibits gp120 conformational change required for CCR5 HIV-1 fusion with the CD4 cell and subsequent cell entry Indication: HIV |
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Amantadine (Symmetrel)
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Class: Ion channel blockers
Prevents the release of infectious viral nucleic acid into the host cell Interferes with the influx of protons through a transmembrane domain of the viral M2 protein Indication: influenza Reduces infection rates by 50 % and illness rates by 60 % CNS depression |
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Oseltamivir (Tamiflu)
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Class: Neuro amidase inhibitor
Neuraminidase -present on the surface of influenza virus particles -enables the virus to separate itself from cells Uses: -uncomplicated acute illness due to influenza A and B virus -adults and pediatric patients 1 year of age and older -symptomatic for no more than 2 days -Prophylaxis Not Recommended -Underlying airway disease (asthma or COPD) |
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Zidovudine
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Class: NRTI (polymerase inhibitor)
MOA: Inhibit the reverse transcriptase enzyme by mimicking naturally occurring nucleotides Have to be phosphorylated to be active Incorporated into viral complementary DNA Terminates chain elongation HIV reverse transcriptase 100 times more susceptible to inhibition than mammalian DNA polymerase Significantly reduces the incidence of neonatal infection from 30 % to 1 % Indication: HIV |
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Efavirenz (Sustiva)
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Class: NNRTI (polymerase inhibitor)
MOA: Inhibit the reverse transcriptase by binding directly to the enzyme adjacent to the active site Low resistance barrier 5% of treatment naïve patients initially present with resistance Single mutation confers resistance Al exhibit cross resistance Many drug interaction via P450s False positive cannabinoid test Indication: HIV |
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Saquinavir (Invirase)
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Class: Protease inhibitor
MOA: Inhibit the HIV protease enzyme Cuts proteins into usable portions to make new functional virions Uncut proteins means that the virions leave the cells without the ability to infect other cells Combination therapy -Many are given with a low dose of another PI (Ritonavir(strong inhibition of CYP3A4, Used in small doses (100 mg) to “boost” other Pis, Inhibits their metabolism, Other Pis can be given in higher concentrations for longer period of time), or Norvir) Indication: HIV Interactions: Substrates -Diazepam (Valium) -Alprazolam(Xanax) Triazolam (Halcion) is contraindicated Inhibitors -Fluconazole -Itraconazole -Ketoconazole |
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Raltegravir (Isentress)
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Class: integrase inhibitor
Integrase: Creates available ends on viral DNA Splices viral DNA into the host DNA inside the nucleus Indication: HIV |
