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SMUPASPG19-PHARM 1 > Viral RX > Flashcards

Viral RX Flashcards

1
Q 
Herpes
Varicella
Zoster
Virus
Virion
A
  • creep
  • tiny spot
  • girdle
  • poison
  • virus particle, proteins
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2
Q

What are 7 ways Antiviral Target virus?

A
  1. Entry into host cell.
  2. Uncoating of viral nucleic acid.
  3. Synthesis of regulatory proteins.
  4. Synthesis of DNA or RNA
  5. Synthesis of structural proteins.
  6. Assembly of viral particles.
  7. Release of new virus from host cell.
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3
Q

Describe Acyclovir, the 1st antiviral?

A
  1. Structure/Source- guanosine analog (look-alike)
  2. Mechanism of action
    (a) viral kinase adds one phosphorus to acyclovir
    (b) human host white cell adds two (DP) and third (TP) phosphorus which activates acyclovir
    (c) Tri phosphorus acyclovir inhibits DNA synthesis
  3. Pharmacokinetics used po or iv
  4. Active against: HSV-1 and 2, VZ virus
  5. Clinical uses-genital, ocular herpes
  6. ADRs- very few after po up to 10 years
  7. Resistance- viral kinase mutation, target of tri-phosphorus acyclovir, DNA polymerase undergoes mutation
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4
Q

How many Herpes DNA viruses and describe the type?

A
  1. Herpes simplex (cold sores, genital infections)
  2. Varicella-Zoster (chicken pox, shingles)
  3. Cytomegalovirus(CMV)
  4. EpsteinBar(mononucleosis)
  5. Herpes Virus Type 6 (roseola)
  6. Herpes Virus Type 7
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5
Q

MR. HERMERS,
LETS TRY THIS DRUG FOR YOUR COLD SORE. This drug has no effects currently, and effects viral kinase via 1P, you body puts on the DP, and TP?

A

prodrug of acyclovir.
HIGER Cp levels
2. Mechanism of action
(a) viral kinase adds one phosphorus to acyclovir
(b) human host white cell adds two (DP) and third (TP) phosphorus which activates acyclovir
(c) Tri phosphorus acyclovir inhibits DNA synthesis

  1. Pharmacokinetics used po or iv
  2. Active against: HSV-1 and 2, VZ virus
  3. Clinical uses-genital, ocular herpes
  4. ADRs- very few after po up to 10 years
  5. Resistance- viral kinase mutation, target of tri-phosphorus acyclovir, DNA polymerase undergoes mutation
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6
Q

Mr. Ocular,

This drug has longer name with ACETYL AND ESTERR, but similar to Acyclovir?

A

FARMICOLVIR
diacetyl ester prodrug of 6-deoxypenciclovir, a conversion to peniclovir,

  1. Mechanism of action
    (a) viral kinase adds one phosphorus to acyclovir
    (b) human host white cell adds two (DP) and third (TP) phosphorus which activates acyclovir
    (c) Tri phosphorus acyclovir inhibits DNA synthesis
  2. Pharmacokinetics used po or iv
  3. Active against: HSV-1 and 2, VZ virus
  4. Clinical uses-genital, ocular herpes
  5. ADRs- very few after po up to 10 years
  6. Resistance- viral kinase mutation, target of tri-phosphorus acyclovir, DNA polymerase undergoes mutation
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7
Q

Penciclovir

A

active metabolite of famciclovir

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8
Q

WHich drug is different from the others in this class for recurrent HSV?

A

Docosanol- RECURRENT

A 22 carbon alcohol that inhibits the fusion between the HSV envelop and the host cell which blocks entry.

Topical cream for prodromal (onset of s/s)

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9
Q

What are the class of drugs for CMV?

A

Ganciclovir

Foscarnet-

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10
Q

Which drug is unigue and inhibits viral DNA polymerase?

A

Foscarnet
RESISTANT ACYCLOVIR
inorganic pyrophosphate molecule IV only

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11
Q

Mr. Gangi Ul, 97yo
THis drug will help 100x more than acylclovir, and delay your retinis. Its a guanosine, if you care. BUT we will monitor your LFTS

A

GANCICLOVIR
1- guanosine analog.

  1. CMV’s protein kinase phosphotransferase UL97 phosphorylates. Inhibit DNA synthesis.
  2. po, iv or intraocular implant. CSF levels 50% of Cp levels. Clearance related to CrCl.
  3. 100x greater activity against CMV compared to acyclovir.
  4. delay CMV retinitis in AIDS patients, high dose for organ transplant.
  5. neutropenia in 20-40% of patients, ABN LFTS,
  6. mutations in the UL97
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12
Q

What is the Anti-influenza Drug inhibits neuramindase?

A

OSELTAMIVIR
ZANAMIVIRA-SECOND NEURAMINDAASE INHIB
1. Structure-Oseltamivir, analog sialic acid (Anis Star)

  1. MOA-inhibitor of viral neuraminidase on viral surface. Enzymatic cleavage required for release of new virus from host cell.
    . PK- = 80% po dose, cleared UNmetabolized by kidney.
  2. Active against: - INFLU A B
  3. Clinical- reduces illness by 1-2 days. Reduces the incidence of hospitalizations by 50%. reduces incidence of illness by up to 90%.
  4. ADR- GI
  5. Resistance- mutiatin of viral neuraminidase
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13
Q

WHich tricyclic amines drugs block ion channel in virus that blocks replication? MANTA BLOCK PUNCH

A

Rimantadine

Amantadine

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14
Q

Which Anti hepatiis B agent INDUCES ENZYMES and binds to disrupt cell replication?

A

Interferon Alfa-IM or SC, cytokine

  1. MOA- inhibits RNA, mRNA, induc enysmes to chop
  2. PK- IV, IM, SC
  3. Active against:5. Clinical- chronic Hep B, C, warts
  4. ADR- flu like, anemias, neutropenia, thrombo
  5. Resistance- NONE

Pegylated interferon alpha- addition of polyethylene glycol, increases its mw and prolongs the drug’s time in the body

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15
Q

DZ of Hep

A

A- seafood raw
B- sharing needles, Harmful
C- Sex, Treatable

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16
Q

Which HEP drug inhibits DNA Polymerase?

A
  1. Structure- adenine analog by human esterase enyme
  2. MOA- inhibits HBV DNA polymerase, inhibs DNA synthesis
  3. PK-
  4. ADR- Lactic acidosis, inhib mitochondrial DNA polymerase
  5. Resistance- mutiatin of viral neuraminidase
17
Q

Which drug is an analog that is activated by triphosphorylation?

A

Sofosbuvir a nucleotide analog
triphosphorylated
incorporated into viral RNA strand
chain elongation is terminated

18
Q

What other drugs are NS3/4A inhibitors and used in combination for HEP C ?

A 
aclatasvir, 
elbasvir, 
ledipasvir, 
ombitasvir, 
velpatasvir

-tas- or -as-

19
Q

What drug is a Fusion Inhibitors (Entry) and a CCR5 Co-Receptor Blockers?

A

ENFUVIRITIDE- FUsion
1. Structure- synthetic 36 aa peptide (inj <100)

  1. MOA- binds to GP41 of HIV envelop, block confirmation change required for entry
  2. PK- SC injection
  3. Active against: HIV-1
  4. Clinical- Adjucnt HAART
  5. ADR- NONE. Trial sleep, weak, numbness, Bacterial PNA
  6. Resistance- NONE

MARAVIROC- CCR5
1. Structure- synthetic 36 aa peptide (inj <100)

  1. MOA- binds to CCR5 host cell, Block HIV binding and entry. Only good for CD4 w/ this, NOT CXCR4
  2. PK- food ok, dose adj w/ other meds
  3. Active against: HIV-1
  4. ADR- URI, myalgia, sleep. Tropism assay check
  5. Resistance- NONE
20
Q

What drug is a Nucleoside Reverse Transcriptase Inhibitors (NRTIs), the cause insominia?
TIDE-DINE

A

ZIDOVUDINE- VODOO ANALOG
1. Structure- synthetic thymidine analog ATP, CTP, TTP

  1. MOA- inhibit transcriptiase converts viral RNA into cDNA, terminates chain elongation
  2. PK- intracellular kinase phosphorylates drug into active compound
  3. Active against: - specific to viral reverse transcriptase
  4. Clinical- block viral replication
  5. ADR- myelosuppression, insomnia, anxiety, confusion, blood enlarged or dec. Lactic acidosis
  6. Resistance- mutation of reverse transcriptase
Abacavir
Didanosine
Emtricitabine
Lamivudine
Stavudine
Tenofovir
21
Q

What drug is Non-Nucleoside Reverse Transcriptase Inhibitors (NNRITs) and affect CYP3A4 enzymes?
TIDE-DINE

A

DELAVIRDINE- CDONT NEED NUCLEOTIDE
1. Structure- variety, not a nucleotide

  1. MOA-bind to site of reverse transcriptase, induce conformation change, inactivates
  2. PK-take b4 antacids, NO phosphorlation for activation
  3. Active against: -HIV only
  4. Clinical- HAART
  5. ADR- INCUDCES CYP3A4, LEVEL INEFFECTIVE other meds inc and itself
  6. Resistance- mutation of RT
22
Q

What drug is a Protease Inhibitors that is a mimetic and cant chop proteins, but risk are MI?

A

RITONAVIR
1. Structure- peptidomimetic hydroxyalamines

  1. MOA- inhibit viral protease, cannot form the core of viron. HIV Protease cleaves proteins. 2 99 aa monomers, Human have 1. HIV specific
  2. PK- oral, INC. plasma levels of drug P450
  3. Active against: -HIV
  4. Clinical- not a sole agent, booster
  5. ADR- GI, MI inc.
  6. Resistance-

IDINAVIR
1. Structure- peptidomimetic hydroxyalamines

  1. MOA- inhibit viral protease, cannot form the core of viron. HIV Protease cleaves proteins. 2 99 aa monomers, Human have 1. HIV specific
  2. PK- no food
  3. Active against:HIV
  4. Clinical-HAART HIV
  5. ADR- nephrostones, AIN hyperbilirubenia, MI
    ST JOHN wort dec levels. Drink lots of water for stones
  6. Resistance-
23
Q

What drug is a Intergrase Strand Inhibitor?

A

DOLUTEGRAVIR- DILUTE BLOOD LEVELS

  1. MOA- inhibits integration of RT transcribed HIV in the the chromosome of host WBC
  2. PK- food ok
  3. Active against- HIV
  4. Clinical-HAART
  5. ADR- hyperglycemia, elevated ALT

RALTEGRAVIR- RIVER LIVER

  1. ADR- hepatic and pancreatic enzyme dfx
24
Q

Name Five possible causes of drug failure

A
  1. sub-therapeutic Cp (blood) levels fail to suprres viral load
  2. Lack of compliance (>20pills)
  3. Drug resistance
  4. Individual diff in metabolize and clearance
  5. Drug and food interaction
25
Q

HIV entry into host cell mech.

what two receptors on the virus surface does HIV attach to?

A

CD4
spike protein gp120
CCR5
CXCR4

26
Q

HIV entry into host cell mech.

What two receptors are required for virus envelop fusion?

A

CD4 AND CO-RECEPTOR CCR5, CXCR4

27
Q

HIV entry into host cell mech.

What molecule is injected in the cell?

A

RNA

28
Q

HIV entry into host cell mech.

What key enzyme converts viral RNA into DNA?

A

HIV reverse transcriptase

Retro viruse to carry on enzymes

29
Q

HIV entry into host cell mech

What enzyme splices DNA into CD4 host DNA

A

HIV intergrase

30
Q

Which irradiated dz uses similar CD4 and co-receptor?

A

SMallpox Variola major

used now for halting HIV to progress to AIDS

31
Q

Which drug is needed for HAART Therapy?

A

At least 2 diff NRTIs- zidoudine, lamivudine, tenofovir
1 + PIs- idninavir, ritonavir
1 FIs, entry- enfuvirtide, maraviroc
20+ pills/day

32
Q

What are NS3/4A protease inhibitor?

What enzyme split proteins and are required in viruses for viron assembly?

A

Velpatasvira new class of antiviral drug,

Protease enzymes

33
Q

Which drug combination is able to eliminate a virus to ZERO Level?

A

Sofosbuvir + velpatsvir for Hep C 98% cure rate.

34
Q

HIV entry into host cell mech.

Where does mRNA form template for new proteins

A

cytoplasm

CD4(t-helper) converts all of its DNA into mRNA using human enzymes)

35
Q

HIV Drug goals?

A

Dec. viral load
Inc. CD4 cells
Need >200 for stability

36
Q

HIV entry into host cell mech.

What chops proteins required for assembly?

A

Protease

New HIV proeins assemble into new virus particles

37
Q

HIV entry into host cell mech.What happens after partical assembly?

A

Cell bursts
New Particles released
Host cell dies

SMUPASPG19-PHARM 1 (17 decks)

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