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Pharmacology Exam 3: Antimicrobials 3
Pharm exam 3 antimicrobrials 3
209
Anatomy
Graduate
02/27/2011
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Term
Fungal infections are called _____.
 Definition
mycoses
Term
Mycoses are ___ in nature and thus very difficult to treat.
 Definition
chronic
Term
Superficial mycoses infections include infections of the ___, __, __, and ___ ___.
 Definition
- skin
- nails
- scalp
- mucous membranes
Term
Systemic mycoses infections are infections of ___ ___ and ___.
 Definition
- deeper tissues and organs
Term
name two causes of fungal infections:
 Definition
- use of broad spectrum antibiotics
- AIDs
Term
How does use of broad spectrum antibiotics contribute to causing fungal infections?
 Definition
- broad spectrum antibiotics, such as TETRACYCLINE, eliminate or decrease non-pathological bacterial populations. These non-pathologic bacteria compete with fungi.
Term
Use of broad spectrum antibiotics, such as ____, can lead to fungal infections b/c these medicines decrease/eliminate ___ ____. Normally the ____ ___ compete with ___, so without the ___ ___, one is more prone to fungal infections.
 Definition
- Tetracycline
- non-pathological bacteria
- non-pathological bacteria compete with fungi
- so without the non-pathological bacteria, one is more prone to fungal infections
Term
With AIDs, there is a decreased immune response, which leads to increased prevalence of ____ infections with fungi, like ____ ___ ____ (KNOW THIS FOR TEST).
 Definition
- opportunistic
- Pneumocystis carinii pneumonia
Term
What type of fungal infections are people with AIDs more prone to getting? TEST
 Definition
- opportunistic
- Pneumocystis carinii pneumonia
Term
LOOK AT SLIDE 4 OF ANTIMICROBIALS II LECTURE. MAY NEED TO KNOW THIS. NOT SURE.
 Definition
Term
What antifungal drugs are used for subcutaneous and systemic mycoses?
 Definition
- Amphotericin B
- Flucytosine
- Ketoconazole, Miconazole
- Fluconazole
- Itraconazole

A Funny Kitten Might Find Insects.
Term
What antifungal drugs are for superficial mycoses?
 Definition
- Grisiofulvin (ORAL)
- Nystatin (TOPICAL)(ORAL)
- Miconazole (TOPICAL)
- Clotrimazole (TOPICAL)
- Ketoconazole (ORAL)
Term
What two anti-fungal drugs are used for subcutaneous and systemic infections as well as for superficial infections?
 Definition
- Ketoconazole (ORAL)
- Miconazole (TOPICAL)
Term
What are ketoconazole and Miconazole used for and what is their main difference?
 Definition
- they are both antifungals that can be used for systemic, subcutaenous, or superficial fungal infections
- Ketoconazole= ORAL
- Miconazole= TOPICAL
Term
What 3 antifungals are used for superficial infections and administered orally?
 Definition
- Griseofulvin
- Nystatin
- Ketoconazole
Term
What is Nystatin used for and what is so special about it?
 Definition
- Nystatin is an antifungal used for superficial infections
- it can be administered orally or topically
Term
What three drugs are used for superificial fungal infections and are administered topically?
 Definition
- Nystatin
- Miconazole
- Clotrimazole
Term
Common fungi of clinical interest:
 Definition
- Candida albicans
- Histoplasma capsulatum
- Cryptococcus neoformans
- Coccidioides immitis
- Aspergillus spp.
- Blastomyces dermatitidis
Term
Amphotericin B is a ____ ___ ___. This is the drug of choice for ___ ___, such as ___ ___ (TEST).
 Definition
- polyene macrolide antibiotic
- systemic mycoses
- Fungal meningitis
Term
Amphotericin B binds ____ in fungal cell membranes, which causes an ____ in permeability by forming ____ __ ____ ___ in the cell membrane. The pores allow the leakage of ___ ___ and ____, which leads to cell death.
 Definition
- ergosterol
- increase
- amphotericinn B associated pores
- intracellular ions and macromolecules
Term
Amphoterin B should be admistered ___ and ____.
 Definition
- slowly
- parenterally
Term
Severe side effects of Amphotericin B:
 Definition
- Febrile response
- Delayed nephrotoxicity
Term
Amphotericin B clinical uses:
 Definition
- nearly all life-threatening fungal infections
- often used for initial induction to rapidly reduce fungal burden, and then is replaced by a newer azole drug for chronic therapy/prevention of relapse
- intrathecal (subarachnoid )therapy for fungal meningitis
- micotic corneal ulcers and keratitis (topical drops and direct subconjunctival injection)
- fungal arthritis (adjunctive local injection directly into joint)
Term
what antimicrobial is used to treat micotic corneal ulcers and keratitis?
 Definition
- Amphotericin B (topical trops or direct subconjunctival injection)
Term
what drug is used to treat fungal arthritis?
 Definition
Amphotericin B
Term
briefly summarize clinical uses of Amphotericin B:
 Definition
- fungal meningitis
- micotic corneal ulcers or keratitis
- fungal arthritis
- intial treatment to reduce fungal burden in life threatening fungal infections
Term
Ketoconazole is an anti-fungal azole that interferes with ___ ___. It is a ___ that can be given ____.
 Definition
- ergosterol synthesis
- Fungistatic
- orally
Term
Ketoconazole may cause ___.
 Definition
hepatoxocity
Term
Ketoconazole interacts with ___, an anticoagulant/antithrombotic. Ketoconazole inhibits ___ ___ of ___.
 Definition
- Warfarin
- inhibits metabolic transformation of Warfarin
Term
Ketoconazole has endocrine effects. It blocks ___ and ___ ____ ____, which can lead to ____, __ ___, ____, and __ ___.
 Definition
- blocks androgen and adrenal steroid synthesis
- gynecomastia
- decreased libido
- impotence
- menstrual irregularities
Term
Ketoconazole is the CLASSIC EXAMPLE of a drug that ____ ___ ___, thus increasing concentrations of other drugs.
 Definition
INHIBITS CYTOCHROME P450

TEST!!
Term
What is the clinical use of Ketoconazole?
 Definition
- effective therapy for superficial fungal infections
Term
Fluconazole and Itraconazole also an azole antifungal. Name three ways fluconazole is different than ketoconazole.
 Definition
1. Fluconazole's oral absorption is NOT affected by pH
2. Fluconazole can be given I.V.
3. Fluconazole has better CSF penetration
Term
Amphotericin B is drug of choice for fungal meningitis, but what "azole" can also be used to treat fungal meningitis?
 Definition
- Fluconazole given I.V.
Term
What are the two oral azoles for VAGINAL CANDIDIASIS/MUCOCUTANEOUS CANDIDIAS?
 Definition
- Fluconazole
- Itraconazole

TEST KNOW THIS
Term
What can both fluconazole and itraconazole be used for?
 Definition
- oral azoles for Vaginal candidiasis/mucocutaneous candidiasis
Term
Clotrimazole, Miconazole, and Econazole can only be administered ____, they are too toxic for systemic use and thus are only used for ____ infections.
 Definition
- topically
- superficial
Term
Clotrimazole, Miconazole, and Econazole have a mechanism like ____ in that they inhibit the synthesis of ____ and are ___.
 Definition
- Ketoconazole
- ergosterol
Term
Clinical uses of Clotrimazole, Miconazole, and Econazole?
 Definition
- topical treatment of superficial mycoses
- vaginitis
- athlete's foot
Term
ALL AZOLES INHIBIT SYNTHESIS OF ERGOSTEROL AND ARE FUNGALSTATICS.
 Definition
Term
Systemic application of what drug is used to treat superficial ring worm infection?
 Definition
Griseofulvin
Term
Main use for Griseofulvin (TEST):
 Definition
- systemic application for superficial ring worm infections
Term
Griseofulvin is the topical for ____ fungal infections. It inhibits ____. It has drug interactions with ____.
 Definition
- resistant
- inhibits microtubules
- warfarin
Term
So far what two antibiotics have drug interactions with warfarin?
 Definition
- Amphotericin B
- Griseofulvin
Term
Nystatin is a topical treatment for ___ and other superfical infections. It also used as swish and swallow drug for ___ ___.
 Definition
Candida
Oral candida
Term
What azole is given for intravaginal topical use of Vaginal candidiasis?
 Definition
- clotrimazole
Term
According to slides all azoles just used for superficial infections, but chart on slide 5 of antimicrobials 2 says otherwise?
 Definition
Term
Viruses consist of ___ __, either __ or __, and a ___ __ or ___.
 Definition
- nucleic acid, either RNA or DNA
- protein coat or capsid
Term
Some viruses contain ___ ___ ___, ___ for ___, __ or ___ __ ____ ___.
 Definition
- antigenic viral glycoproteins
- enzymes for replication
- single or double stranded nucleic acid
Term
A virus particle, aka a ____, from outermost to innermost structures, contains a ___ envelope and a ___. The ___ has a coat made of ____. The ____ had __ ___ in its core.
 Definition
- virion
- lipoprotein envelope
- nucleocapsid
- nucleocapsid has a coat made of capsomeres
- nucleocapsid had a core of nucleic acid
Term
Virion:

lipoprotein envelope> capsomere coat of nuclecapsid> nucleic acid inside nucleocapsid

(see slide 14 of antimicrobials II for picture)
 Definition
Term
Examples of DNA viruses:
 Definition
- poxvirus (small pox)
- herpes viruses (chicken pox, shingles, herpes)
- adenovirus (sore throat, conjunctivitis)
- papillomavirus (warts)
- CYTOMEGALOVIRUS (CMV): UBIQUITOUS DNA HERPES VIRUS
Term
What type of virus is the cytomegalovirus, the ubiquitous DNA herpes virus?
 Definition
DNA virus

(TEST)
Term
Examples of RNA viruses:
 Definition
- retroviruses (AIDs, T-cell leukemia)
- arenaviruses (meningitis, Lassa fever)
- hepadnaviruses (serum hepatitis)
- arbovirus (arthropod borne encephalitis)
- orthomyxoviruses (influenza)
- paramyxovirus (measles, mumps)
- rubella virus (German measles)
- rhabdovirus (rabies)
Term
not sure if we need to know this:

process of viral infection:
 Definition
attachment> penetration by pinocytosis mechanisms> uncoating and transfer of viral DNA to nucleus> early transcription into viral mRNA> early translation of viral mRNA into enzymes for viral DNA synthesis> synthesis of viral DNA and late transcription of viral mRNA> late translation of mRNA into viral proteins> assembly of virus particles in nucleus> budding from nucleus and release of virions
Term
Some anti-viral drugs work by blocking ___ ___ ___. They do this by inhibiting __ ___ ___.
 Definition
- nucleic acid synthesis
- inhibiting viral-DNA polymerase
Term
Other antiviral drugs, like interferon, work by inhibiting ___ of __ ____ .
 Definition
- inhibiting translation of viral mRNA
Term
what is interferon and how does it work?
 Definition
- antiviral drug
- works by inhibiting translation of viral-mRNA
Term
Viruses share the ____ ___ of host cells, thus it is hard to find ___ antiviral drugs.
 Definition
- metabolic processes
- selective
Term
Generally, by the time viral infections are diagnosed ___ ___ is advanced and ____ is difficult.
 Definition
- viral replication
- chemotherapy is difficult
Term
For many life-threatening viral infections, there is __ ___ and the antiviral drugs just improve quality of life (AIDs and Herpes).
 Definition
- no cure
Term
The best strategy with viruses is ____.
 Definition
prevention
Term
remember HIV is an ___ virus.
 Definition
RNA
Term
The HIV virus uses ___ ___ ___. Explain how this works.
 Definition
- RNA retrovirus replication

virion contains reverse transcriptase> viral encoded DNA integrates into the host genome as a provirus> virally coded DNA is transcribed to genomic RNA and mRNA> translation of viral proteins> virus is released by budding> virus replicates without killing host cell> some RNA retrovirus transforms normal cells to malignant cells
Term
What are the 4 classes of Anti-AIDs drugs?
 Definition
1. Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI or NtRTI)
2. Non-nucleoside reverse transcriptase inhibitors (NNRTI)
3. Protease Inhibitors
4. Fusion Inhibitors
Term
what is a nucleoside:
 Definition
nucleoside= nucleobase + ribose/deoxyribose sugar
Term
what is a nucleotide?
 Definition
nucleotide= nucleoside + phosphate

nucleotide= nucleobase + ribose/deoxyribose sugar + phosphate
Term
Anti-AIDs drugs are given in combinations. What is the first choice combination?
 Definition
- 2NRTIs + Protease Inhibitor (PI)
Term
What is the second choice combination of Anti-AIDs drugs?
 Definition
- 2 NRTI + NNRTI
Term
What is the third choice combination of anti-AIDs drugs?
 Definition
- NRTI + NNRTI + PI
Term
Nucleoside Reverse Transcrptase Inhibitors (NRTIs) work by ___ ___ of ____ ____ ____ and can be incorporated into the ___ ___ ___ chain to cause ___. List examples of NRTI.
 Definition
- competitive inhibition
- HIV-1 reverse transcriptase
- growing viral DNA chain
- termination
Term
Name 4 NRTI:
 Definition
- Zidovudine (AZT)
- Zalcitabine (ddC)
- Lamivudine (3TC)
- Didanosine (ddI)
Term
Zidovudine aka ____ is an ___ ___ ____.
 Definition
- azidothimidine (AZT)
- azido(N3) thymidine analogue
Term
Name 4 ways Azidothymidine aka Zidovudine is used to treat AIDS and AIDS related symptoms:
 Definition
1. Reduces incidence of opportunistic infections, stabilizes weight, reverses HIV associated dementia, and reduces viral load
2. Delays onset of AIDS in HIV positive patients
3. Reduces risk of transmission of HIV from mothers to fetus (66% reduction in risk)
4. Given as prophylactic treatments with lamivudine and a protease inhibitor after specific exposures to HIV (accidental needle stick)
Term
Azidothimidine aka Zidovudine is ___ tolerated by patients and ___ in late stages of AIDs.
 Definition
- poorly
- ineffective
Term
After specific exposures to the HIV virus, like an accidental needle stick, what is the prophylactic treatment?
 Definition
- azidothimidine aka zidovudine
- lamivudine
- protease inhibitor
Term
what anti-AIDs drug reduces transmission of HIV virus from mom to fetus by 66%?
 Definition
- Zidovudine aka azidothimidine
Term
Azidothymidine/Zidovudine is an analogue of the ___ ____. It gets phosphorylated by the cellular enzymes to the ___ ___ and then inhibits ___ ___.
 Definition
- pyrmidine thymidine
- triphosphate derivative
- inhibits reverse transcriptase
Term
Azidothymidine can be given __ or ___. It has a bioavailability of 60-80%. ____ in the liver causes inactivation.
 Definition
- orally or I.V.
- Glucuronidation
Term
___ inhibits hepatic inactivation and renal excretion of azidothymidine.
 Definition
Probenecid
Term
Agents that undergo ____ may alter azidothymidine metabolims.
 Definition
glucuronidation
Term
Side effects of Azidothymidine (AZT)/ Zidovudine:
 Definition
- anemia
- neutropenia (agranulocytosis) with long term administration
- GI disturbances
- paresthesias due to poor limb circulation
- skin rash
- insomnia
- fever
- headache
- abnormal liver function
- myopathy (muscular disease)
Term
AZT resistance. The therapeutic response to AZT wanes with __ ___ use. There is viral resistance due to __ ___ ___. Resistance leads to an ___ ___ ___ due to ____.
 Definition
- long term
- mutation of reverse transcriptase
- increasing viral load due to mutation
Term
Zalcitabine aka ____ is another ___ ___ ___ ___. It is a ___ ___ ___ analogue.
 Definition
- dideoxycytidine (ddC)
- synthetic cytosine nucleoside analogue
Term
Zalcitabine aka _____ is used in treatment of AIDS and AIDs related symptoms. It used in combination with ____. It works by inhibiting ___ ___.
 Definition
- dideoxycytidine
- azidothymidine (AZT)
- inhibiting reverse transcriptase
Term
Zalcitabine aka ddC is administered ___.
 Definition
orally
Term
side effects of dideoxycytide aka zalcitabine:
 Definition
- dose related neuropathy
- GI disturbances
- headache
- mouth ulcers
- nail changes
- edema of lower limbs
- general malaise
Term
Lamivudine aka _ ___ __ ____ is also a ___ ___ ___ ____. This is given in combination with ____ for AIDS. It works by ___ the synthesis of the __ ____ __ and it ___ ____ ___.
 Definition
2- deoxy-3- thiacytidine (3TC)
- nucleoside reverstriptase inhibitor (NRTI)
- azidothymidine (AZT)
- terminating synthesis of the proviral DNA chain
- inhibits reverse transcriptase
Term
3 thiacytidine aka Lamivudine is given ____
 Definition
orally
Term
Side effects of 3TC aka 2-deoxy 3 thiacytidine aka Lamivudine:
 Definition
- pancreatitis in pediatric patients
Term
Restistance to AZT develops more slowly when given in combination with ____.
 Definition
- 3TC (2-deoxy-3-thiacytadine aka Lamivudine)
Term
Didanosine aka ______ is a ___ ____ analogue. It is also a ___ ___ ___ ___. .
 Definition
- dideoxyinosine (ddI)
- purine dideoxynucleotide analogue
- nucleoside reverse transcriptase inhibitor (NRTI)
Term
Switching to ___ aka ___ after ____ therapy has been shown to be beneficial with AIDs treatment.
 Definition
- Didanosine aka dideoxyinosine (ddI)
- after AZT therapy
Term
Didanosine aka dideoxyinosine (ddI) gets ___ in the host to a ____, it then ___ the chain and inhibits ___ ___ .
 Definition
- phosphorylated
- triphosphate
- terminates the chain
- inhibits reverse trancriptase
Term
Didanosine aka dideoxyinosine (ddI) is given ___ and is ___ absorbed, even more so with ___.
 Definition
- orally
- rapidly
- antacids
Term
Didanosine aka dideoxyinosine can cause ____ ____. (TEST)
 Definition
Clinical toxicity
Term
side effects of Didanosine/dideoxyinosine (ddI):
 Definition
Clinical toxicity:
- dose related peripheral neuropathy
- pancreatitis
- headache
- GI disturbances
- insomnia
- skin rash
- bone marrow depression
- alteration of liver function
Term
Resistance to Didanosine/dideoxyinosine occurs after ___ ___, but not as bad as resistance as with AZT.
 Definition
prolonged therapy
Term
Normally, nucleoside reverse transcripatase inhibitors (NRTI)are nucleoside analogs that are converted to ___ in the body by phosphorylation. Thus, NRTI are ___.
 Definition
- nucleotides
- prodrugs
Term
Nucleotide reverse transcriptase inhibitors do NOT requires ____, or any other modification for activation. Thus, they may be ___ ___.
 Definition
- do NOT require phosphorylation
- less toxic
Term
Tenofovir is an ___ ___ ___ aka ___ analogue of ____.
 Definition
- acyclic nucleoside phosphonate aka NUCLEOTIDE
- adenosine
Term
Tenofovir is a ___ ___ ___ ___.
 Definition
- nucleotide reverse transcriptase inhibitor (NtRTI)
Term
Tenofovir is indicated in combination therapy with other ___ __ for the treatment of ___ infection in ___.
 Definition
- antiretroviral agents
- HIV-1
- adults
Term
name a NtRTI:
 Definition
Tenofovir
Term
Name the NRTI:
 Definition
- Azidothimidine (AZT) = Zidovudine
- Dideoxycytidine (ddC)= Zalcitabine
- 2-deoxy-3-thiacytide (3TC)= Lamivudine
- Dideoxyinosine (ddI)= Didanosine
Term
Name the 3 Non-nucleoside Reverse Transcriptase Inhibitors:
 Definition
Never Dare Elephants.

- Nevirapine
- Delavirdine
- Efavirenz
Term
NRTIs mechanism summarized:
 Definition
1. Purine and pyrimidine nucleoside reverse
transcriptase inhibitors become active
after conversion to a triphosphate
derivative.
2. The triphosphate derivatives bind
to the substrate binding site.
Term
NNRTI mechanism summarized:
 Definition
1. Do not require phosphorylation to become
active
2. Bind to a lipophilic pocket
distinct from the substrate binding site
Term
NTRTIs bind to the ___ ___ site, while NNRTIs bind to the ___ ___ which is not the same as the substrate binding site.
 Definition
- substrate binding site
- lipophyllic pocket
Term
Nevirapine is a ____ used in treatment of AIDs and AIDs symptoms. It is good for the prevention of transmission of HIV from __ __ to ____.
 Definition
- NNRTI
- infected mothers to newborns
Term
name two anti-AIDS drugs that help prevent spread of infection from infected moms to newborns. Discuss their differences.
 Definition
- AZT: NRTI, less effective and much more expensive

- Nevirapine: NNRTI, more effecive, less expensive
Term
which anti-aids drug is more effective and less expensive at preventing spread of virus from infected mother to baby?
 Definition
- Nevirapine- NNRTI
Term
Nevirapine is a ____ that binds to the ___ ___ of ___ ___ and ___ __ the ___ ___ __. This drug acts ___ with ____.
 Definition
- NNRTI
- lipophyllic pocket
- reverse transcriptase
- allosterically distorts the polymerase active site
- acts synnergistically with NRTIs.
Term
Side effects of Nevirapine a NNRTI:
 Definition
- rash (16%)within 6 weeks of treatment on trunk,face, extremities
- fever
- fatigue
- headache
- nausea
Term
Resistance to Nevirapine is __ if given alone, but has a decreased rate if given with ____.
 Definition
- rapid
- NRTIs
Term
Delavirdine is a ____ that binds to the ___ __ of __ ___ to ___ __ the ___ ___ __. This drug also acts synnergistically with ____.
 Definition
- NNRTI
- lipophyllic pocket
- reverse transcriptase
- allosterically distort
- polymerase active site
- NRTIs
Term
Dilavirdine and Efavirenz (another NNRTI) inhibits the ____ system, so it ___ metabolism of the ___ ___.
 Definition
- inhibits the P450 system
- decreases metabolism of the protease inhibitors
Term
what 2 NNRTI inhibits the P450 system and thus decreases metabolism of the protease inhibitors?
 Definition
Delavirdine
Efavirenz
Term
Side effects of Delavirdine:
 Definition
- rash (but not as severe as with Nevirapine)
Term
Resistance to Delavirdine occurs ___ if given alone, but at a decreased rate if given with NRTIs.
 Definition
rapidly
Term
Efavirenz is ___ that binds the ___ ___ of reverse transcriptase to allostserically distort the polymerase active site. It acts synnergistically with ____.
 Definition
NNRTI
lipophyllic pocket
NRTIs
Term
Efavirenz, like ___, inhibits the ____ system which decreases the metabolism of ___ ___.
 Definition
- Delavirdine
- P450
- protease inhibitors
Term
Side effects of Efavirenz:
 Definition
- CNS effects: 50% of patients in early treatment including dizziness, drowsiness, insomnia, headache, confusion, amnesia, agitation, delusions, depression, and nightmares
- teratogenic in monkeys
- induces the enzyme CYP3ZA4- shown to reduce plasma methadone levels by 50%, known to decrease serum levels of other antiviral/antiAIDs drugs, including the protease inhibitors indinavir and saquinavir
Term
Efavirenz is ____ that induces the metabolic enzyme ____. This is shown to ___ plasma ___ levels by 50%. This also ____ serum levels of other ____ drugs including the ___ ___ indinavir and saquinavir.
 Definition
- NNRTI
- CYP3ZA4
- reduce plasma methadone
- decreases
- anti-AIDs
- protease inhibitors
Term
which NNRTI has CNS effects early on and causes birth defects in monkeys, and decreases levels of plasma methodone and other anti-aids drugs?
 Definition
Efavirenz
Term
Name 5 Protease Inhibitors:
 Definition
- Indinavir
- Nelfinavir
- Ritonavir
- Saquinavir
- Lopinavir100
Term
Protease inhibitors are used to treat ___.
 Definition
HIV
Term
Protease inhibitors work by inhibiting ____ _____, which is a member of the ___ ____ of proteases and is essential for the ___ stage of viral formation.
 Definition
- HIV-1 protease
- aspartyl class
- final
Term
____ precursor protein undergoes autocatalytic cleavage to form _____ ____. These ____ ___ then hydrolyze precursor proteins to generate the proteins required for viral formation. The ___ ___ interfere with this viral formation, leading to ___, ___ virions.
 Definition
- Gag-pol 160-kDA precursor protein
- HIV-1 proteases
- HIV-1 proteases
- protease inhibitors
- immature, noninfectious
Term
Protease inhibitors interfere with viral formation, leading to ___, ___ virions.
 Definition
- immature, noninfectious
Term
In vitro studies indicate that the combination of ___ ___ ___ and ___ ___ is at least additive and usually synergistic.
 Definition
- reverse transcriptase inhibitors
- protease inhibitors
Term
Lopinavir 100 and Ritonavir 400 are both ___ ___ that are used together.
 Definition
protease inhibitors
Term
A sub-therapeutic dose of ____ inhibits CYP3A-mediated metabolism, thereby increasing ____ concentrations.
 Definition
- Ritonavir
- Lopinavir
Term
Ritonavir increases concentration of Lopinavir by inhibiting ____ mediated metabolism.
 Definition
CYP3A
Term
Using Ritonavir and Lopinavir combination maintains ___ ___ with low emergence ___. This combo also has __ patient compliance.
 Definition
- viral suppression
- resistance
- good
Term
Side effects of Indinavir, a protease inhibitor:
 Definition
- increased bilirubin without other hepatic abnormalities
- nephrolithiasis due to crystalization of drug in urine
Term
Side effects of Nelfinavir, a protease inhibitor:
 Definition
- diarrhea
- asthenia
- headache
- moderate hypertension
Term
Side effects of Ritonavir, a protease inhibitor:
 Definition
- nausea, vomiting, diarrhea
- elevated hepatic aminotransferase and triglyceride levels
- inhibits CYP3A4, leading to decreased metabolism of other drugs
Term
Side effects of Saguinavir:
 Definition
- mild diarrhea
- abdominal discomfort
- nausea
- low bioavailability (4-5%) b/c metabolized by P450 enzymes
- co-administration with rifamycin or cabamazepine further reduces plasma concentrations
Term
It is essential to administer protease inhibitors at ____ tolerated doses and in combination with ___ ___ ___.
 Definition
- maximum
- reverse transcriptase inhibitors
Term
Resistance to Indinavir, a protease inhibitor, emerges ___ at ___ doses.
 Definition
- rapidly
- suboptimal
Term
Resistance to Saquinavir, a protease inhibitor, emerges in ___ of patients after __ __ and appears to be due to a single amino acid mutation at either position 48 or 90.
 Definition
- 45%
- 1 year
Term
Enfuvirtide is a ___ ___ and is the newest ____ ____.
 Definition
- fusion inhibitor
- newest anti-AIDs drug
Term
With AIDs__ ___ glycoprotein binds both ___ and a ___ ____ on the __ ___ surface.
 Definition
- HIV gp120 glycoprotein binds both CD4 and a chemokine co-receptor on the T-cell surface.
Term
The actual fusion process leads to entry of virus into the cell and involves two regions of a ___ ___ ____ called ___ and ___. Enfuvirtide mimics the ___ region.
 Definition
- viral glycoprotein gp41 molecule
- HR1 and HR2
- HR2
Term
The fusion active HIV envelope glycoprotein ___ contains a trimer of identical ___ peptides surrounded by three identical ___ peptides. The drug ___ is a peptide with identical sequence of a region of the __ ___ from ____.
 Definition
- gp41
- N
- C
- Enfuvirtide
- C peptide
- gp41
Term
Enfuvirtide is a ___ ___ used in patients with persistant ___ ___ despite treatment with other anti-viral drugs.
 Definition
- fusion inhibitor
- HIV-1 replication
Term
Enfuvirtide is a 36 amino acid peptide that binds to the ____ subunit of the HIV ___ ___ ___ and ___ entry of virus into the cell.
 Definition
- gp41
- viral envelope glycoprotein
- blocks
Term
With Enfuvirtide ___ does occur, but cross-resistance is __ ___.
 Definition
- resistance
- not occur
Term
Herpes viruses include ___ and ___. These are ___ viruses. ___ are the only host. This is a ___ transmitted disease not seen before puberty. There are ____ cases per year.
 Definition
- HSV-1 and HSV-2
- DNA
- Humans
- sexually
- 500,000
Term
HSV-1 is found in __ __ and __ ___. It is found in ___ ___. This causes recurrent lesions known as __ __ or __ ___. HSV-1 may also have __ ___ and infect the ____ of the eye. The immune
response leads to ___, ___, and ___. __ __ ___ ___ lysis of infected cells of the cornea.
 Definition
- oral mucosa
- oral cavity
- sensory neurons
- cold sores
- fever blisters
- scarring
- cloudiness
- blindness
- antibody dependent complement mediated
Term
HSV-2 is __ herpes. Both HSV-1 and HSV-2 are sexually transmitted, but ___ is main cause of genital herpes. ___ ___ transmission occurs with can occur with HSV-2 during delivery, resulting in ___ and ___ ___ ___.
 Definition
- genital
- HSV-2
- maternal-fetal
- encephalitis
- disseminated herpes infection
Term
4 Anti-herpes drug:
 Definition
1. Acyclovir
2. Valacyclovir
3. Vidarabine
4. Idoxuridine

AVVI
Term
Acyclovir is for ___. It is converted to the ___ by ___ ___ ( a viral enzyme). the monophosphate is then converted to ___ by ___ ___. The ___ __ inhibits ___ ___ ___. This is 30 times more selective for the herpes virus enzymes than at host enzymes.
 Definition
- HSV-1
- monophosphate by thymidine kinase
- triphosphate by mammilian kinases
- Acyclovir inhibits viral DNA polymerase
Term
Side effects of Acylcovir:
 Definition
- local inflammation during I.V. injection
- renal dysfunction if given I.V. too rapidly
- nausea and headache
Term
Immunocompromised patients have ___ ___ __ that are ___ to acyclovir.
 Definition
- herpes simplex isolates
- resistant
Term
Resistance to acyclovir may occur if someone gets ____ in the ___ ___ for __ __ or ___ ___.
 Definition
- mutations
- viral gene
- thymidine kinase
- DNA polymerase
Term
Valacyclovir is similar to ____. Valacyclovir is an _____ ___ of acyclovir. Valacyclovir is almost completely ___ to alocyclovir. It has a ___ bioavailabity than acyclovir.
 Definition
- acyclovir
- L-valyl ester
- metabolized
- higher
Term
Vidarabine clinical uses:
 Definition
- herpes simplex in neonates
- herpes associated encephalitis
- varicella-zoster virus infections in AIDs patients
- second line drug after Acyclovir
Term
Vidarabine is ___ to a ___ by __ ___ to that inhibits viral DNA polymerase.
 Definition
- phosphorylated to a triphosphate by cellular kinase
Term
Administration of Vidarabine:
 Definition
- slow i.v. administration
- topically
Term
administration of valocyclovir:
 Definition
oral
Term
what would you use to treat herpes simplex in a neonate?
 Definition
- Vidarabine
Term
What would you use to treat a varicella-zoster infection in an AIDs patient?
 Definition
Vidarabine
Term
What would you use to treat herpes associated encephalitis?
 Definition
- Vidarabine
Term
Side effects of Vidarabine?
 Definition
- nausea, vomiting, diarrhea
- neurotoxicity in late therapy with high doses, reversible
- bone marrow disturbances
- can be carcinogenic
Term
___ is generally more effective and less toxic treatment for herpes, so it is the __ __ drug for herpes.
 Definition
Acyclovir
first choice
Term
___ is the second choice drug for ___ ___ to acyclovir. ___ is also used in these situations and is more effective and less toxic.
 Definition
- Vidarabine
- HSV resistant
- Foscarnate
Term
Idoxuridine is a ___ ___ of ___ used to treat __ ___ and __ ____ infections in the ___.
 Definition
- pyrimidine analogue of thymidine
- herpes simplex
- varicella-zoster
- eye
Term
Idoxuridine is phosphorylated by to a ___ by a ___ ___. The ___ is then incorporated into both __ and __ ___.
 Definition
- triphosphate
- cellular kinase
- triphosphate
- viral and host DNAa
Term
Administration of Idoxuridine:
 Definition
- topically dissolve in DMSO (dimethylsulfoxide)
Term
Side effects of Idoxuridine:
 Definition
- irritation due to DMSO/contact dermatitis
Term
Idoxuridine is ONLY administered ___ b/c it is a ___ and too toxic for ___ use.
 Definition
- topically
- mutagen
- too toxic for systemic use
Term
Cytomegalovirus (CMV) is a ___ ___ __ __. Most CMV infections during normal childhood and adulthood are ___.
 Definition
- ubiquitous DNA herpes virus
- asymptomatic
Term
In immunosuppressed patients, such as ___ or __ ___ transplants or patients receiving chemotherapy, cyotmegalovirus may be ___ resulting in ___ ___.
 Definition
- organ or bone marrow transplants
- reactivated
- interstitial pneumonia
Term
In AIDs patients, cytomegalovirus often ___ to ___ organs causing ____ (inflammation of the choroid and retina), ____ , and ____ ____.
 Definition
- disseminates to visceral organs
- chorioretinitis
- gastroenteritis
- neurological disorders
Term
2 antiviral agents for Cytomegalovirus:
 Definition
- Ganciclovir
- Foscarnet
Term
Ganciclovir is a ___ ___ ___ ___ analogue that is structurally similar to ___.
 Definition
- synthetic guanosine nucleoside
- acyclovir
Term
Clinical uses of Ganciclovir:
 Definition
- CMV (100 times more effective for CMV than acyclovir is)
- life threatening or sight-threatening CMV infections in immunocompromised patients
- prevents CMV infection in transplantation patients
Term
I want to prevent CMV infection in a transplant patient. What should I use?
 Definition
Ganciclovir
Term
Ganciclovir gets phosphorylated by a __ ___ encoded by ___. It is converetd to a ___and the ___ competes with ___ ___ for incorporation into ___ ___.
 Definition
- protein kinase encoded by CMV
- triphosphate
- triphosphate
- guanosine triphosphate
- viral DNA
Term
Ganciclovir is __ ___ __ rapidly, it persists in cells for __ to __ hours.
 Definition
- is NOT broken down
- 18-20 hours
Term
Administration of Ganciclovir:
 Definition
i.v.
Term
side effects of Ganciclovir:
 Definition
- bone marrow suppression
- severe myelosupression if given with zidovudine
- potentially carcinogenic and teratogenic
Term
GANCICLOVIR CAN CAUSE BIRTH DEFECTS!
 Definition
Term
Foscarnate is a ___ ___ analogue of ____. It is ___.
 Definition
- non-nucleoside analogue of pyrophosphate
- inorganic
Term
Foscarnet clinical uses:
 Definition
- second line drug for CMV eye infection in immunocompromised patients
Term
mechanism of Foscarnet:
 Definition
- inhibits viral DNA polymerase
- binds to the pyrophosphate binding site
Term
Foscarenet administration:
 Definition
i.v.
Term
side effects of Foscarnet:
 Definition
serious nephrotoxicity reversible with kidney dialysis
Term
There are CMV strains reported to be resistant to Foscarnet.
 Definition
Term
Lassa Fever is a West African ___ ___ fever transmitted from rodents to humans. Symptoms include:
 Definition
- arenovirus hemorrhagic fever
- fever associated with hemorrhagic manifestations; neurological disturbances, bradycardia

Diagnosis is suggested by recent travel to West Africa with clinical symptoms. Any pt suspected to have this should be isolated and public health authorities notified.

Due to high risk of the spread of infection from fluids
and excreta, routine laboratory studies are best deferred until diagnosis and specimen disposition is resolved.
Term
Ribavirin is an ____ ____ ____ used to treat ___ ___ ___, including ___ and ___ ___ ___, which is an RNA paramyxovirus. It is also used to treat early stages of __ ___, an arenovirus. It reduces mortalitity of __ __ from 76% to 9%.
 Definition
- adenosine/guanosine analogue
- viral respiratory infections including influenza and respiratory syncytial virus
- Lassa fever
- Lassa fever
Term
clinical uses of Ribavirin:
 Definition
- used to treat viral respiratory infections like flu and respiratory syncytial virus (RNA paramyxovirus)
- early stages of Lassa fever
Term
Hepatitis is a ___ virus and can be caused by 5 different viruses: hepatitis A, B, C, D, or E.
 Definition
- DNA
Term
Hepatitis A is __ __ and ___.
 Definition
- self limiting
- asymptomatic
Term
Hepatitis B is __ and causes __ and ___. It has ___ liver involvement. Patient will be __ and have __ ___. Chronic hepatitis will lead to liver failure.
 Definition
- acute
- fatigue
- nausea
- increasing liver involvment
- jaundice
- dark urine
Term
Hepatitis C has __ symptoms at onset, but long term infection leads to chronic liver disease. It is the ___ ___ reason for liver transplant in the USA.
 Definition
- mild
- most common
Term
Hepatitis C risk factors:
 Definition
- injection of illicit drugs
- sexual partners with HCV
- living in prison or juvenile detention centers
- body piercing or tattoos
- health care workers exposed to HCV blood
- newborns of HCV-infected mothers
Term
Anti-Hepatitis drugs:
 Definition
- HBV interferon a2b + Ribavirin
- HCV interferon a2b + Ribavirin
Term
Interferons are ____ proteins synthesized by ___ ___. They are involved with ___ __, ___ and ___ of the immune response.
 Definition
- inducible proteins
- mammalian cells
- cell growth
- regulation and modulation of the immune response

so interferons are immunomodulators
Term
Clinical uses of a-2b interferon:
 Definition
- hepatitis B
- hepatitis C
- Kaposi sarcomas
- hairy cell leukemia
Term
Interferon a-2b is thought to ___ host enzymes that inhibit ____ of ___ ___. Also receptors of IFN a-2b may be ___ ___ ___, which cause inhibition of ___ ___.
 Definition
- induce
- inhibit translation of viral mRNA
- cell surface gangliosides
- inhibition of viral replication
Term
Side effect of IFN a-2b:
 Definition
- fever
- lassitude
- headache
- myalgia
- bone marrow suppression
- cardiovascular changes
- rashes
- alopecia
- altered thyroid function
- altered renal function
- exacerbate autoimmune diseases like thyroiditis
- acute reversible hearing loss like tinnitus
Term
Antiviral agents used against the influenza virus:
 Definition
- Amantadine
- Rimantadine
Term
Amantadine and Rimantadine are antiviral agents used against __ viruses. They inhibit ___ of viral ___ ___ and inhibit viral ____. These are used as ____ for type A influenza. Treatment is effective if initiated 48 hours after initial appearance of symptoms.
 Definition
- RNA
- uncoating
- viral nucleic acids
- viral replication
- prophylaxis
Term
Oseltamivir aka Tamiflu is taken orally. It inhibits the ____ which results in inhibition of release of viral progeny of influenza _ or _. So this inhibits viral spread. This also works with ____.
 Definition
- neuraminidase
- A or B
- Bird flu= H5N1 strain
Term
Zanamivir aka Relenza is the same thing as ____ except this is in inhaler form. It also used for treatment of influenza A, B, or bird flu.
 Definition
- Oseltamivir
Term
Ribavirin is a synthetic guanosine analoge that is active against a __ ___ of __ and ___ viruses. It inhibits ___ ___ synthesis. It is used for ___ ___ ___ in infants and young children. It can be aerosol form, oral, or i.v.
 Definition
- broad spectrum
- RNA and DNA
- viral mRNA
- Respiratory Syncytial Virus
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