Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm. II > Exam III Antivirals and Antiretroviral Medications > Flashcards

Exam III Antivirals and Antiretroviral Medications Flashcards

1
Q

What are the mechanisms of antivirals?

A
  • *1) Alter uncaring of virus
  • to begin replication
  • these drugs prohibit this phase so can’t penetrate the host, and therefore can’t replicate

**2) Polymerase inhibitors

**3) Inhibit viral protein synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the indications and mechanism for amantadine (Symmetril) and rimantidine (Flumadine)

A

**Indication= Influenza A

mechanism= blocks uncaring of virus, prevents pretension into host

-rimantidine is significantly MORE active than arantadine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the side effects for amantadine (Symmetril) and rimantidine (Flumadine)

A

1) CNS stimulation
- enhanced by antihistamines
2) Insomnia
3) Grand Mal Seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the indications for oseltamivir (Tamiflu)?

A

Indication= Influenza A and B

  • used for tx and prophylaxis
  • classic PRODRUG= hydrolyzed to active form
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What does the drug oseltamivir (Tamiflu) inhibit ?

A

**Neuraminidase inhibitor: drug is an enzyme inhibitor that cleaves the budding viral progeny form its cellular envelope attachment point just prior to release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the indications and mechanism for ribavirin (Rebetol, Virazole)?

A

**indications= tx of respiratory syncytial virus

  • *Mechanisms= prevents synthesis of virus proteins encoded by viral mRNA
  • Inhibits virus RNA polymerase
  • disrupts transcription, translation or promotes digression of viral RNA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the side effects for ribavirin (Rebetol, Virazole)?

A

1) mutagenic
2) teratogenic
3) carcinogenic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the indications for trifluridine (Viroptic) ?

A

Indications: herpes simplex keratitis (in eye); keratoconjunctivitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the mechanism for trifluridine (Viroptic) ?

A

interferes w/ viral replication by incorporating into viral DNA in place of thymidine, causing formation of defective proteins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the mechanism for acyclovir (Zovirax) ?

A

-inhibits viral DNA polymerase preferentially (cycle specific)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the indications for acyclovir (Zovirax

A
  • **IV drug of choice for HSV encephalitis
  • *PRIMARY and RECURRECT HERPES in IMMUNOCOMPROMISED PATIENTS
  • Herpes zoster
  • Genital HSV infection
  • USED every 3 hrs which is consistent with cycle phases of viruses
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the indication/mechanism for ganciclovir (Cytovene) ?

A

Indication: **Human cytomegalovirus (CMV)
**Used in tx for CMV retinitis

mechanism: inhibits viral DNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Describe famciclovir and valacyclovir

A
  • recurrent genital herpes
  • *CLASSIC PRODRUGS: converted to penciclovir and acyclovir respectively as they pass thru intestine
  • has not been studies for use in herpes labials
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what are interferons?

A
  • Family of naturally occurring inducible glycoproteins that interfere with the ability of viruses to infect cells
  • Antivirals, cytotoxic, immunomodulatory actions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Interferons:
Synthesized by ____________
3 types of interferes: ______, _____, ____
Administered ______, ______, ______.
Antiviral mechanism is __________understood

Induction of host cell enzymes that ______ viral RNA ______, ultimelty leading to the __________ of viral _______ and ______

A
  • recombinant DNA technology
  • alpha, beta, gamma
  • intralesionally, subcutaneously, or IV
  • incompletely
  • *inhibit
  • *translation
  • *degradation
  • *mRNA
  • *tRNA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are 7 known mechanisms for interferon?

A

1) Induce gene transcription
2) Inhibit cellular growth
3) alter sate of cell differentiation
4) Interfere with oncogene expression
5) Alter cell surface antigen expression
6) increase phagocytic activity of macrophages
7) Augment cytotoxicity of lymphocytes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

The most common indication for interferons are ?

A

1) **Hepatitis B and C
2) **Multiple sclerosis
- Also used for some cancers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What are some adverse effects of interferons?

A

1) **Flu-like symptoms -fever,chills, myalgias, arthralgia, GI disorder (nausea, vomit, diarrhea)
2) Rash
3) **Bone marrow suppression -granulocytopenia
4) ** Neurotoxicity - somnolence, behavioral disturbances
5) **CNS Effects -headaches, depression
6) **Severe fatigue
7) **Severe weight loss
8) **Autoimmune disorders - thyroiditis
9) **Cardiovascular - CHF
10) ** Oral -taste changes, reactivation of herpes labials, excessive salivation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are the drugs for Hep C?

A

1) Ledipasvir + sofosbuvir (Harvoni)
- 100k for 12 wks
- 40% of pts take for 8 wks
2) simeprevir (Olysio)
3) sofosbuvir (Sovaldi)
4) boceprevir (Victrelis)
5) telaprevir (Incivek)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What are the challenges with Antiretrovirals?

A

-to kill the virus, host cells, are often harmed

***Anticirals that alter viral replication
processes are often TOXIC to host cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Viral disease:

All circuses must infect cell to __________
***infection begins when virus _________to _________.
Attachment is mediated by viral proteins that bind to _________ on host cell membrane.
Once enter is gained into host cell, virus is available for ______.
**Viral DAN or RNA itself is ______

A 
replicate
attaches
host cell
specific receptors 
replication 
replicated
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the mechanism for Antiretrovirals ?

A
  • Inhibiting viral attachment and entry (limits spread)
  • Alter genome replication = polymerase inhibitors
  • Immunization = provides **antibodies against viral envelope proteins
  • -blocks viral attachment/penetration
  • -virucidal= antibodies destroy or inactive virus before it interacts w/ receptor on target cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What drug is the first antiviral HIV agent that inhibits viral enter into host cells ?

A

enfuvirtide (Fuzeon)

-Fusion protein inhibitor

24
Q

What is a retrovirus?

A

Any virus in the family Retroviridae that has RNA as it n.a

  • Uses enzyme** reverse transcriptase
  • *Essential for HIV replication
  • Virus penetrate lymphocyte by releasing RNA into cytoplasm
  • Reverse transcriptase is a DNA polymerase
  • -Copies RNA retrovirus into DS DNA
  • **TARGER OF ANTIRETROVIRALS: REVERSE TRANSCRIPTASE
25
Q

Retrovirus:

The DNA segment is presently incorporated int to the cell’s DNA within the nucleus, process is called ____________.
The integrated DNA segment = ?
The new RNA synthesizes viral proteins which are eventually incorporated into new _______ which after release from cell to another ______ ***may represent an ____________ ____

A 
integration 
provirus 
virus 
cell (macrophage) 
infectious virion
26
Q

What are the Subtypes (3 primary classes) of antiretroviral drugs for HIV?

A

1) Nucleoside reverse transcriptase inhibitors
2) Protease inhibitors
3) Nonnucleoside reverse transcriptase inhibitors
- integrase inhibitor

27
Q

What is an example of a fusion protein inhibitor?

A

enfuvirtide (Fuzeon)

28
Q

__________ inhibitors were the very first class of HIV inhibitors to be used a s drugs

A

Reverse transcriptase inhibitors

29
Q

What are the drug concepts for HIV?

A

-Drug tragets structural and functional differences btwn viral and human proteins
-Tx of HIV infection requires combo therapy = HAART
(Highly active antiretroviral therapy)
-“Cocktails” (used to improve effect)
-

30
Q

What does a typical cocktail consist of?

ex?

A

nucleoside reverse transcriptase inhibitor, non-nucleoside reverse transcriptase inhibitor and a protease inhibitor

Ex: lamivudine, nevirapine, and sawuinavir

31
Q

TX w/ antiretrovirals:

Started for most HIV infected pts when immunosuppression becomes _________. CD4

A 
pronounced
500
-2 nuceloside reverse transcriptase inhibitors w/ a protease inhibitor 
-resistant
-alternative drug
-opportunist infections
32
Q

What are the side effect of antiretrovirals?

A

1) Anemia
- toxic to bone marrow and blood cells (transfusions)

2) Leukopenia and granulocytopenia
- predispose pt to infections, fatigue, muscle pain, rashes, nausea, diarrhea, headaches.

3) Hepatotoxicity
4) Peripheral neuropathy
5) Pancreatitis

33
Q

What is the goal of antiretrovirals is to what?

A
  • Prevent opportunistic infections

- Vaccines and other drugs are used for immunoprophylaxis for many infections

34
Q

Pt taking anti-infective agents for what 6 conditions?

A

1) Pneumonia
2) infleunza
3) TB
4) Hep B
5) Herpetic infections
6) Candidiasis

35
Q

What is the tx for opportunistic infection in HIV/AIDS, **Pneumocystis carinii?

A 
oral trimethoprimsulfamethoxazole (Bactrim) 
**SULFA DRUG
36
Q

What is the tx for opportunistic infection in HIV/AIDS, **viral infections?

A

gancilovir, foscarnet, acyclovir

37
Q

What is the tx for opportunistic infection in HIV/AIDS, **candidiasis?

A

fluconazole, ketoconazole

38
Q

What is the tx for opportunistic infection in HIV/AIDS, **cryptococcus, histoplasma?

A

(yeast-like fungi= fluconazole, ketoconazole, amphotericin B

39
Q

What is the tx for opportunistic infection in HIV/AIDS, **tuberculosis?

A

isoniazid (INH), rifampin, ethambutol, streptomycin

40
Q

What is the tx for opportunistic infection in HIV/AIDS, **CMV?

A

ganciclovir

41
Q

What is the tx for opportunistic infection in HIV/AIDS, **EBV?

A

acyclovir, ganciclovir

42
Q

What are nucleoside reverse transcriptase inhibits?

A
  • drugs are chemically nucleosides
  • **Must be biotransformed/bioactivated to work
  • drug integrated into DNA polymerase so DNA terminated

**INHIBTING VIRLA ENUME REVERSE TRANSCRIPTASE

-without reverse transcriptase viral RNA can’t be made into DNA segment and integration doesn’t occur.

43
Q

Nucleoside reverse transcriptase inhibitors:

Reverse transcriptase of HIV is _______ times more susceptible to _____ than normal human cells.
Drugs have _______ on cells already ________

A

1100 X
inhibition
no effect
containing HIV

44
Q

What are examples of Nucleoside reverse transcriptase inhibitors?

A

1) abacavir (Ziagen)
2) **didanosine (Videx)
3) emtricitabine (Emtriva)
4) lamivudine (Epivir)
5) stavudine (Zerit)
6) zalcitabine (Hivid)
7) **zidovudine (Retrovir) = “AZT”

45
Q 
Zidovudine (Retrovir) = AZT:
inhibits HIV \_\_\_\_\_reduces \_\_\_\_\_ from AIDS and AIDS related complex.
Very \_\_\_\_\_\_ = bone marrow depression 
-patient often require \_\_\_\_\_\_\_
Side effects? \_\_\_\_\_\_, \_\_\_\_, \_\_\_\_\_, \_\_\_\_\_
A 
synthesis
morbidity/mortality 
toxic 
transfusions
-CNS,
 -**nausea (FREQUENT), 
-ORAL EFFECT (taste, tongue edema, bleeding gingiva, mouth ulcers) 
-drug interactions inhibit metabolism of drug = potentiates toxicity of both agents
46
Q

What are the drug interactions of Zidovudine (Retrovir) = AZT?

A
  • acetaminophen
  • aspirin
  • indomethacin (NSAID)
47
Q

Nonnucleoside reverse transcriptase inhibitors:
Also block reverse ____________
Drugs inhibit the ______ reaction of reverse transcriptase that is ________ of nucleotide binding.
**DO NOT REQUIRE _________

A

transcriptase
catalytic
independent
***BIOACTIVATION

48
Q

Resistance of Nonnucleoside reverse transcriptase inhibitors develops if used alone (4) list them

A

1) delavirdine (Rescriptor)
2) efavirenz (Sustiva)
3) etravirine (Intelence)
4) nevirapine (Viramune)

49
Q

What are protease inhibitors?

A

-suppress viral replication by inhibiting protease, responsible for cleaving viral precursor peptides into infective virions

***preventing maturation of HIV-infected cells

***PRIMARY DIFFERENCE OF THESE DRUGS = INTERFERENCE W/ ACTION OF HIV INFECTED CELLS

50
Q

List 8 protease inhibitors

A

1) atazanavir (Reyataz)
2) darunavir (Prezista)
3) fosamprenavir (Lexiva)
4) **indinavir (Crixivan)
5) **nelfinavir (Viracept)
6) ritonavir (Norvit)
7) **sawuinavir (Invirase)
8) tipranavir (Aptivus)

51
Q

Nucleotide Reverse Transcriptase Inhibitors :
interfere with HIV viral RNA ________ DNA _________ resulting in ______ of viral replication
Ex: ___________

A

dependent
polymerase
inhibition
tenofovir (Viread)

52
Q

Integrase inhibitors:

Inhibits _________, the enzyme that helps to insert viral _______strand into __________
-prevents ______ of proviral gene into human DNA.
Examples: __________ , ___________

A

integrase
cDNA
human genome
integration

  • raltegravir (Isentress)
  • dolutegravir (Tivicay)
53
Q

What is the NEW HIV medication approved?

Use?

A
  • *Complera
  • COMBO drug used for initial tx of HIV

Use: tx of HIV-1 (complete regiment) with HIV-1 RNA

54
Q

What are the 3 medication from different classes in **Complera ?

A

1) emtricitabine
2) rilpivirine
3) tenofovir disoproxil fumarate

55
Q

What are the adverse events from **Complera ?

A

lactic acidosis/severe hepatomegaly w/ steatosis; post tx acute exacerbation of hep B

56
Q

What are 3 oral complications seen in the gums with Complera ?

A
  • linear gingival erythema
  • NUP
  • Periodontitis

Pharm. II (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions