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49 Cards in this Set

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Penetration and Uncoating: AMANTADINE, RIMANTADINE

propylaxis in Influeza A, and reduce sx if tx w/in initial 48 hrs.

Inhibits viral uncoating by blocking viral membrane protein, M2 proton channel.

Rapidly adsorption, secreted unmetabolized in urine T1/2 20hrs


15% resistance.
Penetration and Uncoating: DOCOSANOL
saturated fatty alcohol, INHIBITS FUSION OF VIRAL ENVELOPE to cell membrane

Effective for tx of HERPES LABIALIS (HSV 1)
Penetration and Uncoating: ENFUVIRTIDE
36 residue synth peptide, based on seq of HIV gp41, BLOCKS FUSION OF THE HIV VIRION TO LYMPHOCYTE.

Adverse eff: hypersensitivity and pneumonia
Assembly and Release: Neuraminidase inhibitor: Zanamivir and Oseltamivir (Tamiflu)
prophylaxis and tx of Influenza A and B ifxn. Reduce sx if given within 48 hrs.
Assembly and Release: Neuraminidase inhibitor: Zanamivir and Oseltamivir (Tamiflu)-- Mech of action
inhibits viral neuraminidase, thereby inhibiting cleavage of sialic aid from glycoproteins, glycolipids and oligosaccharides.

So, end result is: blocks budding of new virus, slows viral spread through respiratory tract

Zanamivir: inhalation; may cause bronchospasm and decrease lung funxn.

oseltamivir: a prodrug, oral admin; nausea and vomiting in >10% pts

Humanized Monoclonal Ab: PALIVIZUMAB
against the F PROTEIN of RSV

approved for prophylactic tx of RSV infxn in high-risk infants
Side effects: Fever, Pneumonia
Viral Nucleic Acid Synthesis: TRIFLURIDINE
thymidine analogue, in which 3 H in the 5-methyl group been replaced with fluorines, which inhibits THYMIDYLATE SYNTHETASE and feedback inhibits other steps in PYRIMIDINE BIOSYNTHESIS
Viral Nucleic Acid Synthesis: TRIFLURIDINE -- Pharmacology
rapidly metabolized by nucleotideases, so useful in METABOLICALLY INACTIVE sites i.e. eye

For tx of Herpetic Conjuctive Keratitis

Selectivity due to differential rate of viral and DNA cellular synthesis
Viral Nucleic Acid Synthesis: RIBAVIRIN
synthetic nucleoside containing 1,2,4 traizole carboxamide fused to a ribose ring moiety.

The phosphorylated form pertub intracellular nucleotide pools; monophophate inhibit INOSINE monophosphate dehydrogenase (essential for synthesis of GMP).

Tx: for RSV infxn in children (inhalation) and combo with IFN in Hep C.

Adv: some incidence of reversible anemia
Viral Nucleic Acid Synthesis: ACYCLOVIR, VALACYCLOVIR (valtrex), Penciclovir, famciclovir
guanosine analogue, having acyclic side chain instead of ribose moiety.

Effective: HSV1, HSV2, VZV

Drug of choice for herpes encephalitis, and varicella (chickenpox) in adolescents and adults.
Viral Nucleic Acid Synthesis: ACYCLOVIR, VALACYCLOVIR (valtrex), Penciclovir, famciclovir -- Mech of Action
Acyclovir is phosphorylated by THYMIDINE KINASE (TK). The triphosphate form is an extremely potent INHIBITOR of VIRAL DNA POLYMERASE.

Acyclovir also doesn't have 3'-OH, so incorporation in nascent DNA would result in chain termination.
Viral Nucleic Acid Synthesis: ACYCLOVIR, VALACYCLOVIR (valtrex), Penciclovir, famciclovir -- Selectivity
drug phosphorylated by TK which cellular enzymes lack. Thus only infected cells accumulate the triphosphate
Viral Nucleic Acid Synthesis: ACYCLOVIR, VALACYCLOVIR (valtrex), Penciclovir, famciclovir -- Pharmacology
Valacyclovir (Valtrex) is a prodrug form of acyclovir: Converted to acyclovir during first pass. Thus, oral admin yeiled 5x greater conc. REDUCES TRANSMISSION OF HSV-2 BY 50%.

Penciclovir: acyclovir analogue, for Herpes labialis (cold sores). It has prodrug form too (FAMCICLOVIR) for tx of herpes labialis and genital herpes.
Viral Nucleic Acid Synthesis: ACYCLOVIR, VALACYCLOVIR (valtrex), Penciclovir, famciclovir -- Toxicity
Oral: GI distress
IV: cause renal dysfunction.
Viral Nucleic Acid Synthesis: Ganciclovir, valganciclovir
also a acyclic guanine nucleoside analog, cosely related to cylcovir.

FOR CMV: inhibits CMV DNA Polymerase.

Catalyzed by CMV encoded UL97 PHOSPHOTRANSFERASE. Also, phosphorylated to some extent by cellular kinase (so more toxic)

Therefore, cause granulocytpenia and thrombocytopenia.

Limit use to severe infxn in immunosuppressive pts and CMV retinits.

Ganciclovir can be given as OCULAR implant.

valganciclovir is a PRODRUG form that is orally active.
Nucleoside Reverse Transcriptase Inhibitor: Zidovudine (AZT)
A synthetic thymidine analog in which 3'-OH replaced with azido group. Prolongs lives of AIDS pts and decrease mother to fetus transmission.
Nucleoside Reverse Transcriptase Inhibitor: Zidovudine (AZT) -- Mech of action
Triphosphate competes w/ dTTP for binding to RT, when incorporated into viral DNA, nascent chains are terminal due to absence of 3'-OH.

Selectivity based on 100x greater affinity of viral RT for AZT than thymidine than is host DNA POL
Nucleoside Reverse Transcriptase Inhibitor: Zidovudine (AZT) -- Pharmacology
well oral absorbtion, cleared rapidly (hepatic) t1/2 One hr.

Can slow metab and excretion with PROBENICID, ACETAMINOPHEN, and ASPIRIN.

Effective conc. in CNS reached.
Nucleoside Reverse Transcriptase Inhibitor: Zidovudine (AZT) -- Toxicity and Resistance
Resistance to AZT and other NRTIs due to mutations in HIV RT gene.

Tox: anemia, neutropenia. POTENTIAL TO INDUCE LACTIC ACIDOSIS as a result of mitochondrial toxicity.
Nucleoside Reverse Transcriptase Inhibitor: OTHER NRTI's.
didanosine (ddl): deoxyadenosine analog

lamivudine (3TC), emtricitabine: approved for Hep B tx

stavudine (d4T), zalcitabine (ddC):

abacavir: guanosine analog, less toxic than AZT

Entecavir: guanine nucleoside analog; Telbivudine: a thymidine analog ;; Inhibit Hep B RT and HBV DNA POL. Not effective against HIV.
Nucleotide reverse transcriptase inhibitor: TENOFOVIR DISOPROXIL
acyclic nucleoside phophonate that when converted to the 'diphosphate' inhibits HIV RT.

The lack of req't for nucleoside kinase activity provides for antiviral activity in RESTING CELLS.

Can increase conc. of didanosine , so when used in combo, increased risk of pancreatitis
Nucleotide reverse transcriptase inhibitor: CIDOFOVIR
another acyclic nucleoside phosphonate.

For tx of ganciclovir and foscarnet-resistant CMV retinitis.

Highly nephrotoxic , may be used for tx of small pox for small pox vaccine reactions
Nucleotide reverse transcriptase inhibitor: ADEFOVIR
for tx of Hep B, nephrotoxic.
Non-nucleoside reverse transcriptase inhibitors: DELAVIRIDINE
rash, fatigue, nausea etc
Non-nucleoside reverse transcriptase inhibitors: NEVIRAPINE
hepatotoxicity, epidermal necrolysis, STEVEN'S JOHNSON
Non-nucleoside reverse transcriptase inhibitors: efavirenz
nightmares, neuropsychological effects. NOT USED DURING PREGNANCY.
Non-nucleoside reverse transcriptase inhibitors: delviridine, nevirapine, efavirenz
These are all used in combo chemotherapy.
Other inhibitors of viral DNA Synthesis: FORSCARNET
inhibits HSV and CMV encoded DNA PL and HIV encoded RT

Effective against ganciclovir-resistant CMV retinitis in AIDS pts

acyclovir-resistant herpes simplex in AIDS pts

Nephrotoxic and symp hypocalcemia
Protein Synthesis/proteolysis inhibition: HIV PROTEASE INHIBITORS
Long List: amprenavir/fosamprenavir, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir
Protein Synthesis/proteolysis inhibition: HIV PROTEASE INHIBITORS
bind to the catalytic site of the HIV encoded Protease cleavage of multiprotein gag-pol precursor into mature viral protein products
Protein Synthesis/proteolysis inhibition: HIV PROTEASE INHIBITORS ... Pharmacology
should only be used in combo which includes one or more nucleoside analogs. Use of two different PI is more effective than a single inhibitor.

Inducers of CYP3A4 i.e. rifampin signif. decrease serum conc. of PIs.
Protein Synthesis/proteolysis inhibition: HIV PROTEASE INHIBITORS -- drug Resistance
result of mutation in HIV protease gene.
Protein Synthesis/proteolysis inhibition: HIV PROTEASE INHIBITOR -- Toxicities
Use of PI assoc. w/ LIPODYSTROPHIES. Increased total LDL, TGs and decreased HDL. Increase Hyperglycemia and MI.

Ritonavir-containing combo of protease inhibitors if used with Rifampin, can lead to drug induced HEPATITIS.
Protein Synthesis Inhibitor: INTERFERON
a glycoprotein with broad in vitro spectrum antiviral activity.

Interferon Alpha (2a, 2b, n1 and alfacon-1) approved for Chronic Hep B and C and malignancies.

IFN alpha nad n3 used for condyloma acuminata.

Tx of Hep C in combo with Ribavirin.

IFN alfa-2b reduces frequency of chronic infection.
Protein Synthesis Inhibitor: INTERFERON -- Mech of action
effect exerted at level of viral protein synthesis:

Two IFN induced enzymes participate in inhibition of viral protein synth:
1. Induction of DS RNA-dependant protein kinase (PKR) that selectively phosphorylate protein synth factor eIF2.

2. inductin of RNA-dependant 2'-5' oligoadenylate synthetase, which produces enzymes that activate a potent RNase that degrades viral message.

IFN also reduces inflammatory cytokine expression in pts with Hep C.
Protein Synthesis Inhibitor: INTERFERON -- Pharmacology
admin IM or IV; t1/2 if 2 hrs, biologic half life much longer

PegIFN have longer half life (45 hrs) and requires less freq administration
Protein Synthesis Inhibitor: INTERFERON -- Toxicities
bone marrow supression (granulocytopenia, thrombocytopenia) and neurotoxicity, acute toxicities incl. flu like sx, alopecia, depression, and GI distress.
Antisense Oligonucleotides: FOMIVIRSEN
antisense oligonucleotide complementary to immediate-early transcriptional unit (IE2) of CMV.

It binds to IE2 mRNA resulting in decreased expression of IE-encoded proteins.

Administered IV to treat CMV retinitis in AIDS pts.
Antifungal: Polyenes; NYSTATIN, AMPHOTERICIN B
characterized by conjugated double bond system with a macrolide ring. Ring is closed by internal ester or lactone.

Effective against Histoplasma capsulatum, cryptococcus neoformans, blastomyces dermatidis, coccodiodes immitis, candida, and spororthrix schenkii.
Antifungal: Polyenes; NYSTATIN, AMPHOTERICIN B -- Mech of ACtion
polyenes bind tightly to sterols (ergosterol) in serum and cell membrane. This causes membrane disturbance and leakage in the cell components and altered membrane transport.
Antifungal: Polyenes; NYSTATIN, AMPHOTERICIN B --- Selectivity
fungal membrane sterol is ergosterol instead of cholesterol. These drugs have greater affinity for ergosterol than cholesterol
Antifungal: Polyenes; NYSTATIN, AMPHOTERICIN B --Pharmacology
extremely insoluble, and poorly absorbed orally.

Nystatin virtually insoluble; used for superficial and GI infection.

Amp B more potent than nystatin and soluble enough for IV administration and distributed to all body components. Excreted in urine.
Antifungal: Polyenes; NYSTATIN, AMPHOTERICIN B -- Toxicity
Amp B: principal side effect Renal Fxn, decrease in GFR

Liposomal prep are available with decreased toxicity, but more expensive.
Antifungal: AZOLES
This includes fluconazole, itraconazole, ketoconazole, posoconazole, voriconazole

effective in tx of variety of superficial and systemic fungal infxn.
Antifungal: AZOLES -- Mech of action
inhibition of 14-ALPHA-DEMETHYLASE, a Cyt p450 involved in Ergosterol biosynthesis, thus resulting in membrane with altered permeability.

Selectivity: fungal sterol biosynthesis more sensitive to inhibition than mammalian (However, Ketoconazole does inhibit other mammalian p450 and reduce adrenal and gonadal steroid biosynthesis.)
Antifungal: AZOLES -- some specific
Miconazole: exclusively topical form.

Ketoconazole, fluconazole, itraconazole: suitable for oral use

Itraconazole: suitable for nails** and dermatophytosis

Voriconazole: invasive aspergillosis

Fluconazole: good CNS penetration, tx of AIDS associated cryptococcal meningitis, and candida esophagitis.

Posoconazole: for fluconazole and itraconazole-resistant candidiasis.

No renal toxicitiy, metabolism is mainly HEPATIC.
Antifungal: AZOLES -- Toxicities
gynecomastia, Ketoconazole inhibit other mammalian p450s and reduce adrenal and gonadal steroid biosynthesis.

Itraconazole can precipitate CHF in susceptible pts.
Antifungal: AZOLES -- Resistance
overproduction of 14-alpha-demethylase (gene amplification) and efflux via MDR-like efflux pump.
Antifungal: Allylamines: TERBINAFINE
Inhibits fungal SQUALENE EPOXIDE

when used topically, effective against crusi, pedis, corporis.

Orally: efective tx of cutaneous tinea infxn, cutaneous candidiasis.

As effective as GRISEOFULVIN for tx tinea cruris and corporis. MORE effective for onychomycosis and moccasin type tinea pedis.

hepatic metabolism

Tox: alopecia, contact dermatitis, hepatotoxity