Non HIV Drugs Med chem Flashcards

(74 cards)

1
Q

viral entry, replication and possible site for anti viral

A

viral attachment
cell entry
transcription
translation
viral assembly

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2
Q

what is a dominant factor for infectious disease

A

aging

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3
Q

what kind of analogs are antivirals

A

purines or pyrimidine

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4
Q

what kind of drugs are antivirals and how do they become active?

A

prodrugs

must be phosphorylated by viral or cellular enzymes

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5
Q

what do antivirals inhibit?

A

active replication so the viral growth resumes after drug removal

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6
Q

anti-viral agents do not eliminate

A

non replicating or latent virus

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7
Q

what is important for the prevention of and recovery from a number of viral infections

A

effective host immune response

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8
Q

what are herpes virial infection and disease structure

A

a linear double stranded virus, all similar and known to cause latent infections

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9
Q

herpes simplex virus 1

A

infections above the waist, gingivostamatitis, herpes labialis, encephalitis

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10
Q

herpes simple virus 2

A

infection below the waist, herpes genitals

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11
Q

varicella zoster virus

A

causes varicella (chickenpox) or zoster (shingles)

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12
Q

epstein barr virus

A

infectious mononucleosis and development of nasopharyngeal carcinoma

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13
Q

cytomegalovirus

A

congenital infections, mononucleosis

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14
Q

human herpes virus type 8

A

kasposi sarcoma

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15
Q

oral agents for herpes virus

A

acyclovir
valacyclovir
famciclovir

MOA: inhibition of viral synthesis of DNA

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16
Q

topical agents for herpes

A

acyclovir
dococanol
peniciclovir

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17
Q

ophthalmic agents for herpes

A

trifluridine

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18
Q

Acyclovir MOA

A

uptake of infected cell
-thymidine kinase phosphorylates to acyclovir monophosphate
-converted to acyclovir triphosphate

completes with deoxygusnosine triphosphate for viral DNA polymerase
-lacks 3 hydroxyl group –> chain termination
-inactivates the viral DNA polymerase-guanosine analog

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19
Q

acyclovir fomulations and spectrums

A

-oral, topical, IV formulas
-spectrum: Herpes simplex 1 and 2, varicella , possibly the epstein barr virus

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20
Q

valacyclovir

A

-L-valyl ester prodrug
-rapidly and almost converted to acyclovir
-spectrum: Herpes simplex 1 and 2, varicella , possibly the epstein barr virus
- oral only

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21
Q

what are three basic resistance mechanisms of acyclovir resistance

A

reduced or absent thymidine kinase
altered TK substrate specificity
alterations in DNA polymerase

cross resistance to famciclovir& valacyclovir

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22
Q

famciclovir

A

-cyclic adenine analog
-converted to penciclovir in the liver and intestine
-oral only
-spectrum: Herpes simplex 1 and 2, varicella ,epstein barr virus (less)
-AE: HA, GI

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23
Q

famciclovir resistance

A

-mutations in viral TK or DNA polymerase
-cross resistance w acyclovir in TK negative strain
-may still have activity in TK altered strains

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24
Q

topical agents for orolabial herpes

A

Penciclovir
-inhibit DNA synthesis
-topical guanine analog similar to acyclovir*
-apply every 2 hrs

Docosanol
-active against a broad range of lipid envelop virus **
-MOA: interferes with viral fusion to host *

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25
HSV ocular keratoconjuctivitis
Trifluridine inhibits dna synthesis
26
anti-cmv agents
ganciclovir valganciclovir foscarnet cidofovir
27
ganciclovir MOA
inhibits DNA polymerase -complets with deoxyguanosin triphosphate -viral encoded phosphotransferase converts to ganciclovir -more effective than acyclovir
28
ganciclovir formulation and spectrum
oral, IV, Intraocular CMV EBV HSV/VZV very effective in treating CMV retinitis in AIDS patients
29
Valganciclovir MOA
Inhibition of viral synthesis of DNA L-valyl prodrug of ganciclovir
30
Valganciclovir formula and spectrum
available orally only CMV EBV HSV/VZV
31
valganciclovir resistance
-mutation in the viral protein kinase responsible for monophosphrylation -responsible for monophosphorylation --confers resistance to ganciclovir alone -mutation in the viral polymerase gene --may show cross resistance to similar antivirals
32
foscarnet MOA
Inhibition of viral synthesis of DNA does not require thymine kinase -- works on HSV strains deficient in this enzyme selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerase noncompetitive inhibitor does not affect cellular DNA polymerse
33
resistance of foscarnet
not caused by thymidine kinase alterations
34
Foscarnet formulation and spectrum
IV only - controlled infusions CMV including ganciclovire strains acyclovir resistant HSV or VZV, EBV
35
Foscarnet structure
phosphonomethanoic acid
36
Cidofovir structure
cytosine analog
37
Cidofovir MOA
Inhibition of viral synthesis of DNA -acyclic nucleoside phosphonate derivative -phosphorylation not dependent on viral kinase -may enhance activity to TK deficient strains
38
Cidofovir formula
IV only
39
Cidofovir must be avoided in
preexisting renal impairment
40
Cidofovir AE
nephrotoxicity (dose-limiting), neutropenia, metabolic acidosis
41
cidofovir resistance
mutation in viral DNA polymerase in CMV, pox, and adenovirus confers resistance to CMV Foscarnet activity not affected by cidofovir resistance
42
what is shingles ( herpes zoster) caused by ?
reactivation of varicella zoster (VZV), initial infection causes chicken pox effective vaccine available
43
Antiviral therapy for Shingles (herpees zoster)
acyclovir, famciclovir, and valaciclovir reduces severity of shingles in Administration begins within 72hours of beginning of symptoms
44
Zoster Immune globin
useful for prevention of chickenpox and shingles but typically not for treatment
45
Human Papilloma virus
non enveloped double stranded DNA virus associated with the development of carcinoma, cervix, anus, and penis
46
What can human papilloma cause
cervical, vaginal, vulvar cancers in women penile cancer in men anal and throat cancer, and genital warts in both men and women
47
papillomavirus treatment options
no specific treatment available Imiquimod* Podofilox Trichloroacetic acid*
48
imiquimod
Immunomodulator* - activates immune cells (monocytes, macrophages, NK cells) produces antiviral cytokines indirectly activates antigen presenting cells including langerhan cells and T helper cells
49
Podofilox
AKA podophyllotoxin main ingredient in podophyllin exact mechanism not known
50
trichloroacetic acid
keratolytic agent given topically crypto therapy burning off HPV wart with liquid nitrogen
51
lopinavir
experimental for HPV but approved for HIV as a protease inhibitor
52
vaccines against HPV
Gardasil- against types 6,11,16, and 18 Cervarix- against types 16 and 18 both non living vaccines
53
influenza vireuses
majority respiratory virus that can cause considerable mortality and in some cases mortality converted with 2 different type of spikes - neuraminidase -hemagglutinin
54
influenza agents
oseltamivir zanamivir amantadine rimantadine
55
what are the two large glycoproteins on the outside of the viral particles
neuraminidase (NA) hemagglutinin( HA)
56
hemagglutinin (HA)
a lectin that mediates binding of the virus to target cells and entry of the viral genome into the target cell
57
neuraminidase (NA)
involved in the release of progeny virus from infected cells by cleaving sugars that bind the mature viral particles
58
oseltamivir MOA
oral neuraminidase inhibitor * cleaves terminal sialic acid residues on glycoconjugates and destroys receptors newly formed virions adhere to cell surface and limit spread
59
Oseltamivir spectrum and AE
Influenza A and B avian influenza H5N1 disease AE: HA, N/V
60
zanamivir MOA
Neuraminidase inhibitor given inhalation
61
zanamivir spectrum and AE
Uncomplicated influenza A and B some strains of avian influenza possible effective fo H5N1 AE: nasal and throat discomfort, btanchospasm
62
Amantadine and Rimantadine MOA
prevents the release of viral nucleic acid into host cell blocks M2 protein channel (type A only) disrupts hydrogen transport, viral uncaring in host cell and therefore viral RNA transcription not currently used in US
63
Amantadine and Rimantadine spectrum and AE
Influenza A (not influenza B) , resistance is frequent AE: Seizures, anticholinergic , CNS, edema , blurry vision
64
Influenza Vaccines (best way to control flu infections)
-inactivated or recombinant (conventional) ----IM ----Trivalent or Quadrivalent* -LAIV- live attenuated prep --FLUMIST ----administered intranasally ----not recommended due to lack of efficacy
65
moneypox
viral zoonosis and symptoms are similar to small pox patients
66
viral structure of of monkeypox
-double stranded DNA virus -belongs to the orthopoxvirus genus of the poxvirdae family -central african and west african cascade
67
Central african strain
more transmissible more severe
68
west african strain
only sporadic cases hypothesis- may be little propensity for human to human transmission
69
what are the natural host for monkey pox
exact natural reservoir unknown rodents ( dormice, squirrels, and rats) eating inadequately cooked meals from infected animals
70
transmission of monkeypox
human close contact with infected animal or human person to person through lesions, bodily fluid, respiratory droplets, contaminated material (beddings)
71
symptoms of monkey pox
invasion period: fever, chills, HA, backache ( last 0-5 days ) skin eruption: development of rash including lesions and pustules (begin 1-3 days, most contagious) symptoms last 2-4 weeks
72
diagnosis of monkey pox
Polymerase chain reaction (PCR) -samples from skin lesions, liquid from pustules or dry crust biopsy
73
treatment for monkeypox
no treatment same as small pox and cytomegalovirus Tercovirimat ( not FDA approved) -limited to pts who are at risk for severe disease such as immunocompromised conditions and younger than 8 yo
74
what is the vaccines available for monkey pox
ACAM2000 -replication competent vaccine that protects against smallpox -contain the vaccinia virus which is live and infectious JYNNEOS -live virus and is replication-deficient vaccine -18 or older and with immune deficiencies can receive the vaccine