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Microbiology > Drugs 2 > Flashcards

Drugs 2 Flashcards

1
Q

Amantadine

A

Anti-influenza drug

MOA=uncoating agent

Widespread resistance, so rarely used

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2
Q

Amphotericin B

A

Amphipathic macrolide that binds to ergosterol in fungal cell membrane, forming pores that allow ions to leak out of cell

Broad anti-fungal spectrum

Given for life threatening systemic infections

Insoluble in water, so suspended in deoxycholate

Poorly absorbed by GI tract–>only given orally if problem is in GI tract

Intrinsic resistance in candida lusitaniae and pseudallescheria boydii

Causes bad side effects
Acute/infusion related toxicity=fever, chills, hypotension
Slower toxicity=kidney damage

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3
Q

Imidazoles

A

2N azoles

Older, less potent

Ketoconazole, clotrimazole, miconazole

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4
Q

Dasabuvir

A

HCV RNA polymerase inhibitor

In Viekira Pak

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5
Q

Triazoles

A

3N azoles

Itraconazole, voriconazole, and fluconazole

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6
Q

Griseofulvin

A

Anti-fungal that interferes with microtubules

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6
Q

Itraconazole

A

Most potent triazole

Wide spectrum of action

Widely distributed

Lipid soluble; absorption increased by gastric acid

Toxicity=GI distress, teratogenic

Drug interactions: H2 and proton pump blockers decrease gastric acidity, metabolized by P450 enzymes

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7
Q

5-Fluorocytosine

A

Anti-fungal nucleoside analog that inhibits DNA and RNA synthesis

Soluble in water so can be taken orally with rapid absorption from GI tract

Water soluble–>taken orally and easily absorbed in GI tract

Narrow spectrum

Given in drug combo to avoid resistance

Adverse effects: decrease function of bone marrow, rash, GI effects, renal toxicity

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10
Q

Oseltamivir

A

Anti-influenza drug

MOA=neuraminidase inhibitor

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11
Q

Capsofungin

A

Echinocandins that inhibit beta-glucan synthesis

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13
Q

Fluconazole

A

Triazole

As compared to itraconazole, absorption is not impaired by stomach acid, it has fewer P450 drug interactions, and is widely distributed to include CNS

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14
Q

Echinocandins

A

Anti-fungals that blocks cell wall synthesis by inhibiting beta (1,3)-glucan synthase

Caspofungin

Used for candida, invasive aspergillosis that is resistant to amphotericin B

Minor adverse effects

Resistance from mutation in FKS1 (gene encoding for beta 1,3 glucan synthase)

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15
Q

Zanamivir

A

Anti-influenza drug

MOA=neuraminidase inhibitor

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16
Q

Rimantidine

A

Anti-influenza drug

MOA=uncoating agent

Widespread resistance, so rarely used

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17
Q

Acyclovir

A

Nucleoside analog for herpes and CMV

Guanosine derivative

First phosphorylation by the viral enzyme; second and third by host enzymes

Outcompetes guanosine and is a chain terminator

Oral, topical, IV that is well tolerated

Resistance from HSV thymidine kinase mutation

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18
Q

Terbinafine

A

Inhibits ergosterol biosynthesis by blocking squalene epoxidase

Synthetic allylamine

Used systemically or topically

Accumulates in skin, nail, and fat

Targets tinea

Must be used continuously

Synergistic with triazoles

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19
Q

Peramivir

A

Anti-influenza drug

MOA=neuraminidase inhibitor

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20
Q

Famciclovir

A

Topical nucleoside analog for herpes, CMS

Guanosine derivative that does not cause chain termination

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21
Q

Miltefosine

A

Drug used for leishmaniasis

Inhibits cytochrome c oxidase activity needed for promastigotes and amastigotes, causing apoptosis

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22
Q

Ganciclovir

A

Topical nucleoside analog for herpes, CMS

Guanosine derivative that causes chain termination

Teratogenic

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23
Q

Amantadine

A

Viral entry inhibitor of influenza (adamantanes)

Binds M2 protein on virus to inhibit unsheathing

Resistance when M2 is mutated

Excreted unmetabolized

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24
Q

Rimantadine

A

Viral entry inhibitor of influenza (adamantanes)

Binds M2 protein on virus to inhibit unsheathing

Resistance when M2 is mutated

Excreted as metabolized form

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25
Q

Voriconazole

A

Newest triazole

Given for aspergillus fumigatus

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26
Q

Zanamivir

A

Neuramidase inhibitor for influenza

Sialic acid transition state analog; prevent viral exit

Inhaled

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27
Q

Ribavirin

A

Nucleoside analog as first line treatment for HCV

Guanosine analog that inhibits RNA synthesis, capping, and replication

Side effects: psychiatric, teratogen

28
Q

Ombitasivir

A

HCV NS5A inhibitor

In Viekira Pak

29
Q

Foscarnet

A

Aka foscavir

Binds DNA pol, RNA pol, and HIV RT to inhibit cleavage

Resistance in strands with mutations in DNA pol, but good for strains resistant to ganciclovir and cidofovir

Administered via IV

30
Q

Peramivir

A

Neuramidase inhibitor for influenza

Sialic acid transition state analog; prevent viral exit

Administered as a single IV dose

31
Q

Interferons

A

Given for HCV and HBV as first line treatment

Activate JAK-STAT pathway to initiate human antiviral response which inhibits viral transcription, translation, protein processing, and maturation

MANY adverse side effects, so often have to stop taking

Interferes with P450 metabolism of other drugs

Administered via IV with polyethylene glycol (PEG) to increase half life

31
Q

Entecavir

A

Nucleoside analog as first line treatment for HBV

Guanosine analog that causes steric hindrance in helix, stopping replication

3’ hydroxyl allows for additional bases to be added before termination

Little resistance, little side effects

31
Q

Tenofovir

A

Nucleotide analog used as first line treatment for HBV and HIV

Inhibits reverse transcriptase

Adenosine analog that already has first phosphate to overcome rate limiting step

Chain terminator

Little resistance

Side effects: nephrotoxicity and decrease in bone mineral density

32
Q

Truvada

A

Emtricitabine and tenofovir

35
Q

Viral entry inhibitors for influenza

A

-adine
Amantadine
Rimantadine

36
Q

Cidofovir

A

Nucleoside analog for herpes, CMV

Phosphorylated twice, both times by host kinases

Resistance due to mutations in viral DNA pol
Cross resistance with ganciclovir

Dose dependent nephrotoxicity made worse by probenecid (blocks tubular transport of cidovir so it is not cleared; given to treat gout)

37
Q

Sofosbuvir

A

Nucleotide analog used as first line treatment for HCV

Uridine chain terminator

Prodrug-carries first phosphate to overcome RSL

Daily pill

Little resistance and little side effects

38
Q

Oseltamivir

A

Neuramidase inhibitor for influenza

Sialic acid transition state analog; prevent viral exit

Aka tamiflu

Oral administration

39
Q

Ledipasvir

A

HCV NS5A inhibitor

Binds NS5A tightly

40
Q

Paritaprevir

A

HCV protease inhibitor

In Viekira Pak

41
Q

Simiprevir

A

HCV protease inhibitor

41
Q

Grazoprevir

A

HCV protease inhibitor

42
Q

Azoles

A

Fungistatic

Inhibit ergosterol synthesis by blocking the third step, ERG11 gene

Cause accumulation of toxic membrane methylsterols (more deleterious effect)

Adverse effects: minor GI problems, some liver enzyme abnormality

Resistance mechanisms: efflux pump, change in expression of enzyme to reduce affinity of azole or require more azole, and mutation in ERG3 so no longer make cytotoxic chemicals

Interacts with P450 drugs

42
Q

Elbasvir

A

HCV NS5A inhibitor

43
Q

Viekira Pak

A

Combination for HCV

Includes
Two pills of paritaprevir (protease), ritonavir (booster for paritaprevir), and ombitasvir (NS5A)
One pill of dasabuvir (RNA pol inhibitor)

44
Q

Maraviroc

A

HIV fusion inhibitor

Binds CCR5 to mask it from HIV

Metabolized by p450s

Resistance due to emergence of strains that use CXCR4 to get into CD4+ cells

45
Q

Enfuvirtide

A

HIV fusion inhibitor

Targets p41 on HIV virus

47
Q

HIV integrase inhibitors

A

-gravir

Raltegravir
Elvitegravir
Dolutegravir

48
Q

Emtricitabine

A

HIV nucleoside analog with long half life

Inhibits reverse transcriptase

49
Q

Etravirine

A

Non-nucleotide reverse transcriptase inhibitor

Strategic flexibility allows it to accommodate for mutations in the active site

Reserved for resistant strands

50
Q

Efavirenz

A

Non-nucleoside reverse transcriptase inhibitor

Binds to site adjacent to active site on reverse transcriptase to cause conformational change

51
Q

Raltegravir

A

HIV integrase inhibitor

Binds Mg2+ in active site of Integrase-DNA complex to displace 3’OH

First line therapy; very potent

51
Q

Atazanavir

A

HIV protease inhibitor

Once daily with fewer lipid distribution side effects

52
Q

Elvitegravir

A

HIV integrase inhibitor

Binds Mg2+ in active site of integrase-DNA complex to displace 3’OH

Use cobicistat as a booster

53
Q

Ritonavir

A

HIV protease inhibitor

54
Q

Dolutegravir

A

HIV integrase inhibitor

Part of Triumeq

54
Q

HIV Protease Inhibitors

A

-avir
Atazanavir
Darunavir
Ritonavir

57
Q

HCV protease inhibitors

A

-previr
Simiprevir
Paritaprevir
Grazoprevir

58
Q

Darunavir

A

HIV protease inhibitor

Take twice orally

58
Q

HCV NS5a inhibitors

A

-asvirs

Ledispasvir
Daclatasvir
Elbasvir
Ombitasvir

59
Q

Viral exit inhibitors of influenza

A

-amivir

Zanamivir
Oseltamivir
Peramivir

60
Q

Daclatasvir

A

HCV NS5A inhibitor

Very potent

Microbiology (10 decks)

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