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Phrx 5043- Exam 3 ID
Pediatric & Antifungal
| Question | Answer |
|---|---|
| Which species of fungus typically cause lung infections? | aspergillus fumigatus & pneumocytis jirovecii |
| Which species of fungus typically cause skin, thrush or BSI? | candida albicans & candida glabrata |
| Which species of fungus typically causes meningitis? | cryptococcus neoformans |
| List characteristics of ideal antifungal agents. | i. B.S.A for yeast & molds ii. No cross-resistance /w azoles iii. rapid fungicidal activity iv. low % acquired resistance v. IV & PO form vi. long T1/2 vii. good VD viii. NO D-D iX. No hepa/nephrotoxicity x. No CYP-metab. xi. No variability |
| Which drugs are in the imidazoles antifungals class? | COMET-K Clotrimazole Oxiconazole Miconazole Econazole Tioconazole Ketoconazole |
| Which drugs are in the Triazoles antifungal class? | FIT-VIP Fluconazole Itraconazole Terconazole Voriconazole Isavuconazole Posaconazole |
| What is the MOA of Azole antifungals? | inhibit lanosterol-14a-demethylase (enzyme required to convert lanosterol into ergosterol) |
| What is the MOA of griseofulvin? | inhibits mitosis in dermatophytes. (Ineffectively topically) |
| What is the MOA of flucytosine? | pyrimidine analogue, converted to 5-Fluorouracil (5-FU) which inhibits thymidylate synthase, thus inhibiting the synthesis of DNA and RNA in fungal organisms. |
| Which antifungals are considered polyenes? | NAN Natamycin Amphotericin B Nystatin |
| Which antifungals are considered echinocandins? | CAM Caspofungin Anidulafungin Micafungin |
| Which antifungals are considered allylamines? | ANT Amorolfin Naftifine Terbinafine |
| What is the MOA of allylamines? | inhibit squalene epoxidase |
| What is the MOA of echinocandins? | inhibit cell wall synthesis by targeting glucans (1,3 Beta-glucan synthase) |
| What are 2 evolutionary differences between fungi and mammalian cells that aid in selectivity of antifungal therapeutics? | i. fungi have cells walls v mammalian cells lack cell wall ii. fungi cell membranes contain ergosterol v mammalian cell membranes contain cholesterol |
| What is the MOA of polyene antifungals? | cell membrane disruptor, cause leaking of ions and small molecules leading to apoptosis. |
| Which fungal infections are polyene antifungals used to treat? | severe histoplasmosis cryptococcosis meningitis severe coccidioidomycosis aspergillosis life threatening blastomycosis candidiasis |
| Which polyene cannot be used systemically because of toxicity? | nystatin |
| What are the likely resistance mechanisms of fungi against amphotericin B or nystatin? | decrease in ergosterol increase in chitin |
| Azoles are fungistatic at [i] concentrations but fungicidal at [ii] concentrations | [i] Low [ii] High |
| Which Azole is safer for human tissue? | Triazoles, bind to mammalian P450 enzymes with lower affinity. |
| Which azole has high penetration into CSF and is used to treat fungal meningitis? | fluconazole (water soluble bis-triazole) |
| Which Azole has CYP2C9 interactions with warfarin? | fluconazole, voriconazole (CYP 2C9 inhibitor) |
| Which Azole is orally active and its use has declined since voriconazole & posaconazole use as increased? | itraconazole |
| Which azoles are useful against aspergillosis? | voriconazole (soc), itraconazole, pasconazole,isavuconazole |
| Which azole has the most CYP interactions? | voriconazole (CYP 2C19, 2C9, 3A4) |
| What are the mechanisms of resistance of fungi to Azoles ? | i. mutations in Erg11 gene (code for 14-alpha demethylase) ii. efflux by ATP-binding cassette (ABC-1) |
| Which Azole antifungals is used for serious systemic fungal infections & cutaneous candidiasis? | miconazole |
| What is the MOA of echinocandins? | non-competitive inhibitors of Beta-1,3-glucan synthase (inhibit cell wall biosynthesis) |
| What can be given to a patients determined to be infected by azole-resistant candida spp or aspergillus ? | caspofungin |
| What mechanism of resistance can fungi have against echinocandins? | FKS1 & FKS2 gene mutations (gene code for Beta-1,3-glucan synthase catalytic site) |
| Which antifungals have limited spectrum of activity, and primarily used to treat dermatophytes? | ally amines |
| Which ally amine is available topically only due to extensive first-pass metabolism? | naftifine |
| Which fungi organism typically produce erg11 gene mutations to acquire resistance against azole antifungal? | Candida ablicans & Candida glabrata |
| Which fungal organism commonly over produce ABC-1 efflux pumps to acquire resistant to azoles antifungal? | Candida glabrata |
| Describe the infectious process of viral pathogens. | i. Adsorption ii. Entry iii. Uncoating iv. transcription v. translation vi. Assembly vii. Release |
| List the most common DNA viral pathogens. | Herpesvirus (HSV/CMV/VZV) Adenovirus Papovavirus Poxvirus Parvovirus |
| List the common RNA viral pathogens. | Flavivirus Filovirus Arenavirus Rhabdovirus Reovirus Retrovirus Togavirus Myxovirus Bunyavirus |
| Which viral pathogen causes Herpes Cold Sores? | Herpesviruses (HSV/CMV/VZV) |
| Which viral pathogens causes Polio, Hepatitis A or Rhinovirus? | Picornavirus |
| Which viral pathogen causes Polyoma Warts? | Papovavirus |
| Which viral pathogen causes Rubella, equine encephalitis? | Togavirus |
| Which viral pathogen causes Respiratory infections? | Adenoviruses |
| Which viral pathogen causes Yellow fever, Dengue fever, St Louis encephalitis, Zika? | Flavivirus |
| Which viral pathogen causes Smallpox? | Poxvirus |
| Which viral pathogen causes encephalitis, hemorrhagic fever? | Bunyavirus |
| Which viral pathogen causes canine distemper? | Parvovirus |
| Which viral pathogen causes vesicular stomatitis? | Rhabdovirus |
| Which viral pathogen causes Mumps, Measles? | Myxovirus |
| Which viral pathogen causes Diarrhea? | Reovirus |
| Which viral pathogen causes Ebola or Marburg? | Filovirus |
| Which viral pathogen causes lymphocytic choriomeningitis? | Arenavirus |
| Which viral pathogen causes HIV? | Retrovirus |
| What is the mechanism of resistance against allyl amines by fungi? | increase production of efflux pumps |
| What are the mechanisms of resistance against azoles by fungi? | i. increase production of efflux pumps ii. alteration of membrane sterol composition iii. overproduction of target enzyme iv. mutation of target enzyme |
| what are the mechanisms of resistance against flucytosine by fungi? | i. decrease uptake in C. glabrata ii. mutation in enzyme, UPRT (adds ribose) iii. mutation in cytosine deaminase |
| Which antifungal have low level of evidence supporting resistance against MOA by fungi? | griseofulvin |
| What is the mechanism of action for amantadine & rimantadine as antiviral agents? | interfere with Entry (HA), Uncoating (M2), Replication of influenza A virus. |
| What is the mechanism of action neuraminidase inhibitors? | transition state inhibitor which competes with neuraminidase (NA or sialidase) for sialic acid thus blocking the release of the progeny virus from infected cells. |
| what are the components of influenza virus? | i. Hemmaglutinin (HA) ii. M2 iii. Neuraminidase (NA) or sialidase |
| List some examples of neuraminidase. | zanamivir (Relenza) oseltamivir (Tamiflu) |
| What is a possible mechanism of resistance to zanamivir | mutations in Glu119Gly |
| What is the mechanism of action of baloxavir marboxil (Xofluza)? | inhibit cap-dependent endonuclease (prevent RNA negative viruses like influenza, from stealing guanine 5' cap from host mRNA) |
| list some examples of nucleoside antimetabolites. | idoxuridine cytarabine trifluridine vidarabine acyclovir valacyclovir cidofovir ribavirin |
| Describe the MOA of nucleoside antimetabolites against viral agents. | analogues to physiological nucleosides in terms of uptake and metabolism--> leads to DNA synthesis inhibition & chain termination |
| Which antiviral agents require bioactivation? | i. baloxavir marboxil (Xofluza) ii. oseltamivir (Tamiflu) iii. nucleoside antimetabolites iv. sofosbuvir (for HCV) |
| What is the treatment used against Hepatitis C? | protease inhibitors PEG/RBV + boceprevir/telaprevir |
| list the protease involved in Hepatitis C infection. | NS3/4A NS5A NS5B |
| List some examples of NS5A inhibitors. | ombitasvir daclatasvir ledipasvir |
| What is the MOA of NS5A inhibitors? | modulate IFN & innate immunity |
| What is the MOA of NS5B inhibitors? | inhibit RNA-directed RNA polymerase--> inhibit viral RNA synthesis |
| Which modification of Coronavirus makes ribavirin less effective? | RNA proof-reading exonuclease (nsp14)--> edit out mis-incorporated bases |
| list examples of SARS CoV2 protease inhibitors? | nirmatrelvir & boceprevir |
| What is the MOA of reverse transcriptase nucleoside inhibitors? | inhibits HIV-1 RT via DNA chain termination after incorporation of nucleosi |
| list some examples of nucleoside reverse transcriptase inhibitors (NRTi). | i. zidovudine ii. didanosine iii. stavudine iv. abacavir v. tenofovir vi. lamivudine vii. emtricitabine |
| Which NRTi was FDA approved with lower renal toxicity? | tenofovir alafenamide |
| Which NRTi has no significant D-D interactions? | emtricitabine |
| What causes resistance to non-nucleoside reverse transcriptase inhibitors (NNRTi)? | P236 mutations & Lys103 mutations |
| Which Non-Nucleoside Reverse Transcriptase inhibitor (NNRTi) was developed to overcome resistance? | efavirenz & etravirine |
| list some examples of integrase inhibitors (INSTI). | raltegravir (RAL) elvitegravir (EVG) dolutegravir (ViiV) bictegravir |
| Which integrase inhibitors have Qday dosing? | elvitegravir dolutegravir |
| What is the activity of reverse transcriptase in retroviral infectivity? | converts viral RNA into complimentary DNA-RNA complex & creates dsDNA that is unintegrated. |
| What is the ftn of RNase H in Retroviral infectivity? | RNA chain degradation |
| Which NRTi requires cleavage from tissue & plasma esterases to be active ? | tenofovir |
| Which antiretroviral therapy require phosphorylation to be active? | Nucleoside Reverse Transcriptase inhibitors (NRTi) |
| Which antiretroviral therapy DO NOT require bioactivation via phosphorylation? | Non-Nucleoside Reverse Transcriptase inhibitors (NNRTi) |
| What are the critical viral processing enzymes in HIV infection? | Reverse Transcriptase (RT) Integrase Protease |
| What is the protease involved in HIV infectivity process? | Aspartyl protease |
| What are the monomers present in the aspartyl protease active site? | Asp25-Thr26-Gly27 |
| What is the initial design of protease inhibitors against HIV? | high MW di/tri-peptides low water solubility Low bioavailability short T1/2 (rapid hepatic metabolism) |
| What is the aim for newer protease inhibitors designed to combat HIV? | reduce peptide character reduce MW maintain binding affinity |
| List examples of protease inhibitors (Pi). | saquinavir (lead compound) ritonavir indinavir nelfinivir amprenavir darunavir |
| What is the benefit of 2nd generation protease inhibitors such as amprenavir & darunavir? | i. reduce peptide character ii. reduce number of asymmetric centers iii. enhance solubility iv. enhance binding affinity |
| Describe the mechanism HIV used to gain entry into host cells. | i. HIV surface protein (gp120) binds CD4receptor ii. conformational change in gp120 exposes gp41 iii. binding of gp120 to co-receptor CCR5 or CXCR4 iv. penetration into cell via gp41 |
| Which drugs are develop to prevent HIV from gaining entry into host cells? | maraviroc (block CCR5)& enfuvirtide (block gp41) |
| What is the ftn of integrase in HIV infectivity? | integrate HIV genome into host genome using 2 rxns i. 3' processing to remove 2 nucleotide from 3' end ii. strand transfer |
| Describe the amino acids present in the integrase catalytic site? | Asp64, Asp116, Glu152 |
| Which combinations of ART typically used for Naive HIV patients? | 2 NRTis + Pi w/booster/NNRTi/INSTI |
| List some examples of Non-Nucleoside Reverse Transcritpase Inhibitors (NNRT). | nevirapine (1st gen.) delavirdine (1st gen.) efavirenz (2nd gen.) etravirine (3rd gen.) |
| What is the protease used by SARSCoV2 to release new viral progeny? | C3-like or main protease (Mpro) |
| Which agents are used to overcome SARSCoV2 RNA proof-reading exonuclease (nsp14)? | remdesivir & molnupiravir |
Created by:
daneangelo7
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