Ohl and Williamson - Drugs Flashcards
Which drug’s MOR is from a herpes UL97 protein kinase mutation (CMV), herpes TK deficiency and DNA Pol mutation?
Gangciclovir
Cycle Gang Uniform- Ultra Leather Jackets ‘97.
Your patient has severe CMV retinitis. Which drug should you use? What form is this in?
Valganciclovir (P/O)
Which two drugs offer herpes coverage PLUS CMV coverage?
Ganciclovir and Valganciclovir
An immunocompromised patient has CMV retinitis, GI CMV. What do you give him? How?
Gangciclovir (IV)
Which drug is preferred for severe CMV only, do to toxicity?
Gangciclovir
What drug covers severe CMV, and acyclovir resistant/TK mutation resistant HSV and VZV?
Foscarnet
What drug treats severe CMV and CMV retinitis, but causes myelosuprresion? Which one is IV only?
Ganciclovir and Valganciclovir Ganciclovir is IV only.
What should you give someone with Whitlows?
P/O Acyclovir
How does acyclovir work?
Acyclovir is converted by viral thymidine kinase to acyclovir monophosphate, which is then converted by host cell kinases to acyclovir triphosphate (ACV-TP). ACV-TP, in turn, competitively inhibits and inactivates HSV-specified DNA polymerases preventing further viral DNA synthesis without affecting the normal cellular processes.
What is the MOR of acyclovir?
Herpes TK deficiency, DNA mutation
What would you give for severely disseminated HSV?
Acyclovir (IV)
How many times do you give acyclovir orally? What is a better (but more expensive) drug to use?
3-5x a day.You can give famciclovir or valaciclovir instead 1-2x a day, however, it is very expensive.
What are some side effects of Foscarnet?
Nephrotoxicity and electrolyte imbalance
When would you use Foscarnet? How do you administer it?
IV. For severe HSV infections that are Acyclovir or Ganciclovir resistant and CMV
How does Foscarnet work?
It binds and inhibits herpes DNA pol DIRECTLY.
What drug would you give for papillomavirus, poxviruses, acyclovir-ganciclovir resistant HSV and VZV, CMV
Cidofovir
What are some side effects of cidofovir?
Nephortoxicity
Which drug has a long intracellular 1/2 life which allows for single wkly dose and is an alternate to foscarnet? How do you administer it?
Cidofovir.It is used as an injection for the eye.
___ is an acyclic cytosine analog. ___ is a pyrophosphate mimic.
CidofovirFoscarnet
How do you administer Valganciclovir? What do you give it for? What are some side effects?
P/OFor severe CMV retinitis.Myelosupression. It is an esterfied prodrug that gets de-estered by the host.
What can you give topically for HSV labialis?
Pencyclovir (OTC)
What drugs block the M2 channel of Influenza? Which influenza strain does it not work on?
Amantadine, Rimantadine
What are some side effects of Amantadine and Rimantadine?
Neurotoxicity (confusion, anxiety, insomnia), especially in elderly patients and renal insufficient patients. Amantadine is more toxic than Rimantadine.
_____ and ____ prevents acidification of viral interior necessary for uncoating. Influenza B virus M2 channel is unaffected. Inhibits release of RNP and uncoating of viruses entering the cell. Which one is more toxic?
Amantadine and Rimantadine. Amantadine is more toxic.”A’man to blocking M2!”
____ aka tamiflu is a ____ inhibitor
NA. Sialic acid mimics that prevent release of new viruses from cells (block NA from cleaving sialic acid receptor). Both inhibit pinching off of new viral progeny. Zana blocks the active site of NA while Oselta competitively binds sialic acid, blocking NA.
Out of oseltamivir and zanamavir, which does has no resistance?
Zana –> no resistance. Oselta –> resistant to most H1N1 strains.
What are the side effects of Oseltamavir?
Nausea and vomiting (10%)
What are the side effects of Zanamavir?
bronchospasm (contraindicated for asthmatics)
Out of Oselta and Zanamavir, which one works only if given within 48 hours?
Oseltamivir
Which drug inhibits viral entry of influenza at the membrane fusion step?
Umifenovir.
Which drug binds and inhibits PB2 cap-binding domain (prevents PB2 from stealing 5’ cap from host)?
VX-787 (Pimodivir)
Which drugs work on influenza strains A and B?
Oseltamavir and Zanamavir
Ribavirin is used for what?
It works against several RNA and DNA viruses. Inhaled for RSV (infants and immunocompromised adults), and co-administered p/o with IFN-alpha for chronic HepC.Broad spectrum, RSV and HepC.
If you need to treat chronic HepC, what would you give?
Ribavirin in combination with IFN-alpha.
What are the side effects of Ribavirin?
It is teratogenic (contraindicated in pregnancy). It also can cause hemolytic anemia.
You are trying to treat an infant that comes to your clinic with RSV. What do you prescribe?
Ribavirin (inhaled)
You are trying to treat a pregnant women with chronic hepC. What do you NOT want to give?
You do not want to with Ribavirin p/o with IFN-alpha to a pregnant woman, since it is a teratogenic and can cause hemolytic anemia.
LATTE drugs are used for what?Which is most potent?
Hep BLamivudine, Adefovir, Tenofovir, Telbivudine, and Entecavir. Entecavir is most potent of all HepB drugs and the main drug used against HepB.
____ is the main drug used for HepB and is a nucleoside analog.
EntecavirIf you eat too much Honey Bee, you can get a dENTalCavity (entercavir)
NS5A/B inhibitors are ___ ____ inhibitors and are used for which disease?
RNA replication inhibitorsHepCNS5A (NBA) of Chess
What drug targets CCR5? What disease does it treat?
Maraviroc, a CCR5 co-receptor antagonist treats HIV.
What drug offers a 97% cure rate for HepC?
NS5A/B inhibitors (RNA replication inhibitors)
____ is considered an alternative therapy for naive patients or as salvage (not first-line treatment) for HIV
Maravciroc
Before you give Maraviroc, what should you do?
You should do a tropism assay to make sure that the HIV virus uses CCR5 and not CXCR4.
What HIV drug targets gp41, a fusion entry inhibitor?
Enfuvirtide
Name the NRTI’s
Zidovudine, Tenofovir, Lamivudine, Emtricitabine, Abacavir.
A patient comes to your clinic, co-infected with HIV and HepB. What do you give?
Tenofovir.
What can be used as a prophylaxis for pts who are at risk of HIV?The True Tricky Tenor was PREPPING for his concert.
PrEPTT’sTruvada = and Tenofovir and Emtricitabine
What are the two versions of tenofovir? Which one is better?
Tenofovir disoproxil fumarate (TDF)Tenofovir alafenamide (TAF)TAF is better because is is less toxic and more efficient. A is better than D.
What is the standard treatment for HIV?
Standard treatment requires 2 nukes that are analogues of different nucleotides. Triple therapy (standard treatment) = 2 nukes and 3rd drug (e.g. integrase inhibitor, NNRTI)
If you were to give triple therapy to an HIV patient, which combination would not work?A. Abacavir and Emtricitabine + PIB. Tenofovir and Zidovudine + PIC. Emtricitabine and Lamuvudine + PI
C. They are both cytosine analogs.
You gave a drug to an HIV patient a certain drug. All of a sudden, you see flu-like symptoms and a rash. What happened?
Patient has a B5701 HLA type. You gave abacavir and the patient has an abacavir hypersensitivity. HIV Abacus Airline flies a B5701
Name the NNRTIs. What do they do?Which one is not effective in treating patients with advanced disease?Which NNRTI would you give to a patient if they are resistant to Efavirenz?
Never Ever eat Real PieNevirapine, Efavirenz, Etravirine, RilpivirineAll these non-competitively bind to and inhibit reverse transcriptase. Rilpivirine is not effective for ppl with advanced HIV –> HIV has become a RIL PILL. Do not use Rilpivirine for patients with a high viral load (>100,000) or severely low CD4 (<200). For patients that are resistant to efavirine, give ETRAvirine. (TRY this instead)
What are the INSTI drugs? Integrase Strand Inhibitors
Dolutegravir, Elvitegravir, RaltegravirLow threshold for resistance. The delusion elf, ralph, on instigram
What would you boot elvitegravir with?
Boost is with cobicistat (stribild and genvoya), otherwise must be adminited multiple times per day.
Of all the INTSI’s, which two are the first line treatments, but have a low threshold for resistance?
Elvit and DoluteDelusional Elf (they are the first two words in the mnemonic sentence).
What is Triumeq?
Abacavir/dolutegravir/lamivudine is a fixed-dose combination drug for the treatment of HIV/AIDS. Harry Truman sold his Abacus and bought Dolly the Lamb
Protease Inhibitors are
FosamMy DarlingLets have a lovely pinot at our ATANZANIAN weddingRITON from my TYPwriterFosamprenavirDarunavirLopinavirirAtazanavirRitonavirTipranavir
atazanavir and darunavir is given with a ___
booster –> cobicistatA daring jazz tap dancer (TAZ) always needs a boost of confidence
Lopinavir is boosted with what?
Lopinavir ritanavirLopinaviritanavir
Which PI is given as a salvage therapy?
Tipanovir At the “TIPPING PoInt”Tipanovir
How do PI’s work?
inhibits cleavage of precursor polyproteins by protease
What are the HIV boosters? How do they work?
Cobicistat and RitonavirInhibits Cyp450, preventing metabolism of PI’s and elvitegravir by the liver. Boosting increases concentrations (allows drugs to make it through liver untouched), reducing dosing frequency and pill count.
Amphotericin B (IV) and Amphotericin B (liposomal preparation) are part of which drug family? How does it work?
PolyeneBinds to ergosterol, disrupting cell membrane of yeasts and some molds (increases permeability)
What is the MOR of Amphotericin B?
Uncommon, but structurally altered ergosterol
Amphotericin is a ____ spectrum drug.
broad
A patient comes to your clinic with deep-seated/systemic candida infections. What do you give?
Amphotericin
A patient comes to your clinic with a deep seeded cryptococcus infection. What do you give?
Amphotericin
A patient comes to your clinic with a deep seeded, dimorphic (“environmental”) fungal infection (histoplasmosis, blastomycosis, coccidioidomycosis, sporotrichosis). What do you give?
Amphotericin
A patient comes to your clinic with a deep seeded aspergillus infection. Another patient comes with a deep seeded mucormycosis. what do you give?
Amphotericin B
A patient comes to you with crytococcus, azole-resistant infection. What do you give?
Amphotericin B
What are some side effects from Amphotericin?
“Ampho-terrible”Flu-like symptoms from infusion: fever (esp. in cancer pts/ neutropenics), chills, HoTN (hypotension), HA (hemolytic anemia), n/v, and tachypneaNephrotoxicity – can put pts w/ kidney problems into renal failure!Anemia
A patient came to your clinic after taking mystery drug A.
She now has:
Flu-like symptoms from infusion: fever (esp. in cancer pts/ neutropenics), chills, HoTN (hypotension), HA (hemolytic anemia), n/v, and tachypnea
Nephrotoxicity and Anemia.
What did she take?
Amphotericin B
Which is more toxic, amphotericin B in IV form or liposomal prepared form?
IV form.Similar to Ampho IV, but decreased prevalence and severity. Compared to Ampho IV, more $$$, comparable or slightly better efficacy. Theory: packaging ampho into lipid vehicle means that more drug will be delivered to fungal cell membrane (and to liver and areas of potential deep-seeded mold infection)
You are trying to pick out a drug that will inhibit fungal RNA and DNA synthesis. What do you choose?
A pyrimidine (cytosine analog) - Flucytosine
You have a patient that comes to you with a cryptococcal infection (e.g. crypto-meningitis). What do you prescribe?
Amphotericin B + Flucytosine
What is the MOA of flucytosine?
It inhibits fungal RNA and DNA synthesis/
You have an HIV patient that comes to you with a cryptococcal infection. What do you give?Limit your therapy to ___ weeks due to toxicity, then switch to an ____.
Flucytosine + Amphotericin BLimit therapy to 2 weeks (“induction phase”) due to toxicity; then switch to azole (Itra, Iso, Vori, Fluc, Posa). Doesn’t work well alone. Always used w/ Ampho (works synergistically because these have different MOAs)
What does flucytosine work synergistically with?
Ampho B
Which drug inhibits fungal Cyp450 and synthesis of ergosterol (interfere with permeability and synthesis of fungal cell membranes)?
Imidiazole - AZOLES
What should you NEVER mix imadazole with?
*NEVER used w/ Ampho (MOAs antagonize each other)!IMA AM = NO!
What are all the Imadazoles?
Itraconazole, Isaconazole, Voriconazle, Flucaznole, Posaconazole, Itra IsA Very Fluky PoserIsavuconazole and Posaconazle are both P/OVoricanazole and Fluconazole (IV and PO)
Your patient comes to your clinic but does NOT have an aspergillus infection. What drug do you NOT give?
Fluconazole (IV/PO).Fluc does not work on Apsergillus
What drug treats:Candida, Cryptococcus, CoccidioidomycosisNO MOLDS (e.g., aspergillus)
Fluconazole (IV/PO)
Flucanazole treats all candida except for ____
C. Krusei
What are the side effects of fluconazole?
None. Generally well tolerated.
What drug is this?Excellent CSF penetration (given to treat crypto-meningitis after 2 wk induction period w/ Ampho+Flucyt.; drug of choice for Coccidioidal meningitis). Renal excretion; oral form very bioavailable. Don’t treat for asymptomatic candiduria (candida in distal urethra, urine, or foley cath) shows up as positive urine culture but person is NOT actually infected; Summary: use for indicated infections you want to treat ORALLY or if you need to cross blood-brain barrier
Flucanazole
Excellent CSF penetration (given to treat crypto-meningitis after 2 wk induction period w/ Ampho+Flucyt.; drug of choice for Coccidioidal meningitis). Renal excretion; oral form very bioavailable. Don’t treat for asymptomatic candiduria (candida in distal urethra, urine, or foley cath) shows up as positive urine culture but person is NOT actually infected; Summary: use for indicated infections you want to treat ORALLY or if you need to cross blood-brain barrier
Your patient has HIV and has a disseminated cryptococcus meningitis infection. What do you give?You have another HIV patients that has coccidioidal meningitis. What do you give?
Fluconazole + AmphoFluconazole + Ampho
Your patients has a coccidioidomycosis infection –> Coccidioidal meningitis. What is your drug of choice?
Fluconazole
Fluconazole will NOT treat acquired ____
C. Albicans
____ will not treat C. Glabrata and C. Krusei
Fluconazole
How does Fluconazole work?
Inhibits fungal CYP450 and synthesis of ergosterol (interfere with permeability and synthesis of fungal cell membranes)*NEVER used w/ Ampho (MOAs antagonize each other)
Which fungal drug offers excellent CSF penetration?
Fluconazole
This drug inhibits ergosterol synthesis and thus, fungal membrane synthesis by inhibiting squalene epoxidase (different than azoles – no Cyp450!)
Terbinafine
Your patient comes to the clinic with a C. krusei infection. What do you give?
Voriconazole (IV/PO)Don’t give Fluconazole, since C. krusei is resisstant to Fluc.
How is Voriconazole administered?
IV/PO
Your patient comes with an aspergillus infection. What is your first DOC?
Voriconazole
Voriconazole (IV/PO) has expanded activity to molds over fluconazole (its parent) and itraconazole while keeping most candida and cryptococcus activity
What do you treat for endemic mycosis? (dimorphics/ “environmentals”): Blastomycosis, histoplasmosis, sporotrichosis,Trichophyton, onychomycosis??
Itraconazole
____ is a drug that is used for endemic mycoses but it is poorly absorbed orally (better if given as liquid). There islittle CSF penetration (Fluconazole is better); for severe indicated infections, start w/ Ampho first and then switch to this.
Itraconazole
List the Imadazole drugs from smallest spectrum to largest spectrum:
FIV PI
Fluconazole (least spectrum, but a great yeast drug, bioavailable, use for yeasts)
Itraconazole (increased spectrum, use mainly for dimorphic fungi (Histo, Blasto, Sporo, Cocc)
Voriconazole (increased spectrum even more, more molds, used mainly for ASPERGILLUS
Posaconazole & Isavuconazole (increased spectrum for even MORE complex molds like bread molds, rhizopus, and mucomycosis)
What is the main drug used for Aspergillus infections?
Voriconazole Vori Good Asperigus
What drug inhibits 1-3 beta glucan synthetase?(1-3 beta-glucan is a key cell wall component)
Echinocandins - The FUNGINS(Caspofungin, micafungin)The “E” looks like a 3, and B comes before C”Mainly bloodstream and deep-seated candida infections (particular resistant candida/ fluconazole-resistant strains)NOt FUN.
The fungins will treat mainly bloodstream and deep-seated ____ infections (particular resistant candida/fluconazole-resistant strains). They also treat ____ (but not as well as voriconazole).Fungins can also treat candida (including C. ___ and ___); However, no activity against ______
Mainly bloodstream and deep-seated candida infections (particular resistant candida/ fluconazole-resistant strains) Aspergillus (but not as good as voriconazole), Candida (including C. glabrata and C. krusei); No activity against cryptococcus
____ is the drug of choice for resistant Candida (e.g., C. krusei, C. glabrata) over Ampho due to lower toxicity; Usually, you should start your pt on this for 2-3 days while awaiting MIC results – if infection sensitive to fluconazole, switch over.
Echinocandins (The Fungins)- drug of choice for resistant Candida (e.g., C. krusei, C. glabrata) over Ampho due to lower toxicity; usually start pt on this for 2-3 days while awaiting MIC results – if infection sensitive to fluconazole, switch over.
Your patient comes with a candida infection. You don’t know if it is resistant or not. What do you do?
Start then out with Echinocandins (The fungins) for 2-3 days while awaiting for a MIC result. If the yeast is sensitive to Fluconazole, switch over.
A patient comes with a trichophyton (jock’s itch) infection. What do you give?
Terbinafine (P/O)
Patient comes with onychomycosis (toenail/ fingernail fungus). What do you give?
Terbinafine (P/O)
A patient comes with thrush. What do you give?
Nystatin
A patient comes to your office with a dermatophyte infection such as tinea corporus, pedis and capitus. She also has vulvovaginal candidiases, thrush and esophageal candidiases. What do you give?
Imidazole (Miconazole - monostat, Clotrimazole - lotrmin) - Ketoconazoleor Analyzime (Terbinafine - lamisil)
How does Terbinafine work?
Inhibition of egosterol synthesis
What anti-fungal drug is good for penetrating the BBB
Fluconazole
Side Effects of Terbinafine?
Hepatobiliary dysfunction; many drug-drug interactions
Which antiparasitic drugs target the erythocytic states (non-liver stages)
Chloroquine (p/o), Mefloquine (P/O), Doxycycline, Quinine (P/O), Quinidine (IV), Artemether/lumefantrine (ACT) P/O.
Quincy and Quincy’s Doxin, ArtyLu, sniffed Clara Meth and Chlorine
What drug would you give all the plasmosias?
Chloroquine (P/O)
Chloroquine inhibits ___ polymerase allowing non-detoxified Hb products to build up which are toxic against the organism.
heme
What drug is not active against hepatic schizont or hypozoite?
Chloroquine (PO)
A patient says he is going to Africa next month. What drug should you start on him?
A prophylaxix – chloroquine (PO)
Mefloquine (PO) is active against all ____
plasmodium species, including chloroquine-resistant P. falciparum)
What are the side effects of Mefloquine?
N/V, nightmares or “vivid dreams”CNS stimulation (rare) including anxiety, tremor, hallucincations, psychosis, seizures
Which drug can be given weekly for prophylaxis (long 1/2 life, 5-7 weeks) for all plasmodium species?Note: contraindicated (not give) for patients with history of seizures, depression/psychiatric disorders
Mefloquine
- A patient comes to your clinic with chloroquine/mefloquine resistant malaria. What do you do?2. Another patient comes to your office telling you she wants to for to Africa, where a resistant malaria is endemic. What do you do?
- Give a daily P/O doxycycline dose. For treatment, used with quinine(PO)/quinidine(IV) 2. For prophylaxis, use doxycycline (P/O)
A patient contracted Malaria in the U.S. What do you give? They ask you about the side effects. What do you say?
Quinine (P/O) IV side effects: Arrythmias, hypotension, N/V, tinnitus, hemolytic anemia.
Which drug is rapidly cidal, usually used with doxy, has a short 1/2 life, and a narrow TI: toxicity/ratio?Clue: Alkaloid extracted from a cinchona tree bark; used with doxy for more rapid parasite clearance;
Quinine (PO)Quinidine (IV)
What drug binds iron, breaking down peroxidase bridges leading to the generation of free radicals that damage parasite proteins?
ACT (Artemether/lumefantrine (PO)
What drug do you give for uncomplicated malaria? Clue: it decreases parasitemia the quickest of all antimalarial drugs
ACT (artemether/lumefantrine) POThe WHO mandates combination therapy of malaria with artemether PLUS another antimalarial (lumefantrine, pyramethamine)
Drugs that act on erythrocytic states (non-liver states) interfere with ___ production
schizont
A patient comes to you with NON-SEVERE P. Falciparum, chloroquine-and-mefloquine-resistant P. falciparum. What do you give? Clue: it is not very active against P. vivax/ovale latent liver stages - hypnozoites)
Atovaquone/proguanil (PO) “Malarone)
A patient comes to you needing prophylaxis for malaria in preparation for their trip to Africa. hey do not like getting nightmares. What do you give? How often?
Atovaquone/proguanilA “causal prophylaxis” of malaria (no dream issues.Give this daily (as opposed to wkly for chloroquine/mefloquiine)
What drug works against the hypnozoite and is active only in the liver stage?
Primaquine (PO)
You need to give a patient a “terminal prophylaxis” of P. vivax/ovale (which have relapse potential from hyponzogriote). What do you give, what do you warn them of, and how often do you give it?
Primaquine (PO)Well-tolerated, BUT causes hemolysis in G6PD-deficient patients (must check G6PD in ethnic groups where it prevails). Given daily (PO)
Metronidazole is given to treat what?
Amoeba, Giardia, Trichomonas
Chloroquine (PO) MOR?
Drug efflux (pumps): resistance appears geographically.P. falciparum in most of the world is resistant
What drug is bioavailable, and can be given wkly for prophylaxis (long 1/2 life) or more frequently for P. falciparum from susceptible area and P. vivax/ovale?
Chloroquine (PO)
What is the MOA of chloroquine. What does it treat?
Inhibits heme polymerase allowing non-detoxified Hb prodct to build up which are toxic against the trophozoite. It is active against susceptible p. falciparum (haiti, C. america, Middle East – drug resistance in all other areas limits use for P. falciparum and vivax).Not active against liver stages (Schizont/hypnozoite)
A patient contracted malaria in Africa. You’d like to treat the erythrocytic stage. What drug would you NOT want to give?
Chloroquine (PO)Chloroquine is active against susceptible p. falciparum in haiti, c. america, middle east, but is resistant in all other areas.
Which drugs work against the Liver cycle of malaria only?
Primaquine (hypnozoite)
Which drugs work against the erythrocytic cycle only?
QQ’s CMD-ACTQuinine/Quinidine, chloroquine, mefloquine, doxycycline, ACT
Which drug works on both liver and eryth. cycles?
Atovaquone/proguanil
A 36 yr old male of Lebanese ancestry is being treated for P. Vivax malaria. He experiences sever fatigue, back pain, and darkened urine. Which one of the following antimalarial drugs is most likely to have cause his symptoms?
PrimaquineThe symptoms presented by patients are consistent with hemolytic anemia. The pt is male and from the mediterranean basin, both which are factors associated with G6PD deficincy. Prim. is most likley to cause hemolytic anemia in such people.
Tinnitus, dizziness, blurred vision and headache are indicative of toxicity to which one of the following atimalarial drugs?
Quinine:
Which drug is recommended for life-threatening severe P. falciparum infection>
Arteminsinin is the antimalarial drug rec for life threatning multi drug resistant p. falciparum malaria.
A patient who frequently backpacks in the outdoors complains of diarrhea and fatigue. Examination of stool specimens show binucleate organisms with four flaggae. Which one of the following drugs would be effective?
Metronidazole. Patient has giardiases.
Which drug is a good drug of choice for dermatophytic infections such as athletes foot?
Terbinafine
