Term
| Acyclovir Mech. of Action |
|
Definition
Nucleoside analog
Guanosine derivative
3 phosphorylation steps
-thymidine kinase
Inhibition viral DNA synthesis |
|
|
Term
-HSV—fever blisters,
-1* and recurrent genital herpes
-VZV—higher doses
-DOC—herpes simplex encephalitis and neonatal HSV infection |
|
Definition
|
|
Term
| Acyclovir Absorption/Interactions |
|
Definition
-Oral, IV, topical
-Poor oral bioavailability (22%)
-Keep well hydrated—prevents renal damage
+ probenecid—decrease renal clearance |
|
|
Term
Contra—Allergies
Cleared by kidneys
Monitor renal function
Nephrotoxicity
NVD
Headache |
|
Definition
| Acyclovir Contraindications/Adverse Effects |
|
|
Term
| valacyclovir mech. of action |
|
Definition
Nucleoside analog
Pro-drug to acyclovir |
|
|
Term
| valacyclovir absorption/interaction |
|
Definition
Oral ingestion converts to acyclovir
Serum levels 3-5x acyclovir
Oral bioavailability 55% |
|
|
Term
NV
Rash
High doses—confusion, hallucinations, seizures
High doses in AIDS—GI problems, TTP, and HUS associated events |
|
Definition
| Valacyclovir contraindications/adverse effects |
|
|
Term
| Famciclovir mech. of action |
|
Definition
Nucleoside analog
Guanine derivative
3 phosphorylation steps
-thymidine kinase
Competitive inhibition of viral DNA polymerase block DNA synthesis
Pro-drug to penciclovir |
|
|
Term
|
Definition
Acute herpes zoster—shingles
Tx/suppression recurrent genital herpes
Tx recurrent mucocutaneous herpes simplex in HIV pts |
|
|
Term
| + probenecid—increase serum levels |
|
Definition
|
|
Term
Contra—Hypersensitivity
Headache
• Nausea
• Diarrhea |
|
Definition
| Famciclovir contraindications/adverse effects |
|
|
Term
| Penciclovir mech. of action |
|
Definition
Nucleoside analog
Guanosine analog, active metabolite of Famciclovir |
|
|
Term
|
Definition
| Topical tx recurrent herpes labilais (fever blisters) |
|
|
Term
Contra—Hypersensitivity
Headache
Anesthesia at site |
|
Definition
| Penciclovir contraindications/adverse reactions |
|
|
Term
| trifluridine (viroptic) mech. of action |
|
Definition
Nucleoside analog
Fluorinated pyrimidine nucleoside
Inhibits viral DNA synthesis incorporated into viral DNA instead of thymidine |
|
|
Term
| Trifluridine (Viroptic) indications |
|
Definition
Keratoconjunctivitis from HSV I/II
***dendrites finding in eye!! |
|
|
Term
| Trifluridine (viroptic) absorption/interactions |
|
Definition
Only as eye drop
No significant interactions |
|
|
Term
| Ganciclovir mech of action |
|
Definition
Nucleoside analog
Acyclic guanosine analog
3 phosphorylation steps
-thymidine kinase
Broader spectrum |
|
|
Term
|
Definition
CMV
CMV retinitis in AIDS pts
Prevent CMV in organ transplant/AIDS pts
HSV
VZV
EBV
HHV-8 |
|
|
Term
| Ganciclovir absorption/interactions |
|
Definition
IV
Orally—prophylaxis end-organ CMV dz in AIDS pts
+ imipenem-cilastatin—seizures |
|
|
Term
Contra—neutropenia & thrombocytopenia
Can depress bone marrow
myelosuppression |
|
Definition
| Gamciclovir contraindications/adverse effects |
|
|
Term
| valganciclovir mech of action |
|
Definition
L-valyl ester prodrug of Ganciclovir
2 diastereomers |
|
|
Term
| valganciclovir indications |
|
Definition
CMV retinitis
CMV prophylaxis in organ transplants |
|
|
Term
| valganciclovir absorption/interactions |
|
Definition
Well absorbed/rapidly metabolized in intestinal wall and liver
Oral replaced oral ganciclovir 2* to lower dosing |
|
|
Term
|
Definition
Phosphonoformic acid
Pyro-phosphate compound inhibit viral DNA/RNA polymerase & HIV reverse transcriptase without phosphorylation
**differs: 2nd line drug |
|
|
Term
|
Definition
CMV retinitis
Colitis
Esophagitis
Acyclovir resistant HSV/VZV |
|
|
Term
| foscarnet absorption/interactions |
|
Definition
+ Take with water to prevent renal failure
+ cyclosporine, Amphotericin B, aminoglycosides additive nephrotoxicity |
|
|
Term
Contra—impaired renal function
Renal failure |
|
Definition
| foscarnet contraindications/adverse reactions |
|
|
Term
| NRTI’s, NNRTI’s, Protease Inhibitors, Fusion Inhibitors, CCR5 receptor antagonists, Integrase Inhibitors |
|
Definition
| 6 classes of anti-retroviral drugs |
|
|
Term
| Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI's) |
|
Definition
Nucleoside analogs, Nucleotide Analogs
Competitive inhibition of HIV-1 reverse transcriptase; incorporation into growing viral DNA chain premature chain termination b/c inhibition of binding with incoming nucleotide
Require intracytoplasmic activation via phosphorylation to triphosphate
Toxicity: associated with lactic academia and severe hepatomegaly w/steatosis (fatty liver infiltrate) |
|
|
Term
| Zidovudine (AZT) mech of action |
|
Definition
NRTI
Thymidine analog
Form nucleotide to inhibit reverese transcriptase to terminate viral DNA
One of 1st drugs with activity against HIV |
|
|
Term
| Zidovudine (AZT) indications |
|
Definition
Prophylaxis after needle sticks
Prophylaxis to prevent vertical transmission |
|
|
Term
| Zidovudine Absorption/Interactions |
|
Definition
Well absorbed orally
Penetrates CNS
+ myelosuppressives (ganciclovir)—additive BM suppression
+ drugs that under glucuronidation—increase AZT levels
+ azoles/protease inhibitors—inhibit metabolism
+ Rifampin—increases clearance
+ usually combined with lamivudine or didanosine
+ stavudine—antagonistic |
|
|
Term
Contra—resistance common in advanced AIDS
Hypersensitivity
Hepatic/renal metabolism
Bone marrow suppression
Book adverse effects Macrocytic anemia, neutropenia, nausea, headache, insomnia, asthenia |
|
Definition
| Zidovudine contraindications/advderse effects |
|
|
Term
|
Definition
NRTI
Acyclic nucleoside phophonate analog of adenosine
Competitively inhibits HIV reverse transcriptase—chain termination |
|
|
Term
|
Definition
|
|
Term
| Tenofivir absorption/interactions |
|
Definition
+ acyclovir/ganciclovir—additive renal toxicity
+ emtricitabine—coformulated—preferred dual NRTI regimen
Take with food |
|
|
Term
Contra—hypersensitivity
Renal impairment
Headache
NVD |
|
Definition
| Tenofivir contraindications/adverse effects |
|
|
Term
| Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI's) |
|
Definition
Bind directly to site on the viral reverse transcriptase that is distinct from nucleoside binding site
Do not require phosphorylation and do not compete with nucleoside triphosphates
Not used alone due to resistance development
Orally/good bioavailability
Extensive hepatic metabolism with renal/fecal excretion
Synergistic w/NRTI’s and protease inhibitors against HIV
Most common side effect: skin rashes! |
|
|
Term
|
Definition
| List Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI's) |
|
|
Term
| Nevirapine, Efavirenz Mech of Action |
|
Definition
Directly inhibit reverse transcriptase
Not nucleotide analogs |
|
|
Term
|
Definition
200 mg dose prevent vertical transmission given at onset of labor
Followed by 2 mg/kg dose to neonate within 3 days |
|
|
Term
| Neviparine absorption/interactions |
|
Definition
Excellent oral bioavailability
Combination therapy with 2 NRTI’s
Induces CYP3A drug metabolism—decreases indinavir, ritonavir, saquinavir, and oral BC
+ ketoconazole—don’t give together!!!! |
|
|
Term
| Nevirapine contraindications/adverse effects |
|
Definition
Toxicity—SJS and toxic epidermal necrolysis, fulminant hepatitis
Book adverse effects
Rash, hepatitis (occasionally fulminant), nausea, headache
Adjust dose for hepatic insufficiency |
|
|
Term
|
Definition
| Preferred NNRTI except in pregnancy! |
|
|
Term
| Efavirenz absorption/interactions |
|
Definition
+ 2 NRTI’s + 1 PI—good starting treatment for HIV!
Take on empty stomach
Take at bedtime initially to minimize CNV side effects |
|
|
Term
Adverse CNS effects—abnormal dreams/depression
Neural tube defects if administered in 1st trimester
Rash, increased liver enzymes, headache, nausea |
|
Definition
| Efavirenz contraindications/adverse effects |
|
|
Term
|
Definition
cleaves precursor molecules to produce final structural proteins of mature virion core—prevent assembly of protein coat
Render particle noninfectious—prevent new waves of infections
Adverse effects: syndrome of altered fat distribution, insulin resistance, and hyperlipidemia develop type II diabetes
Given orally, extensively metabolized by cytochrome P450
Renal/fecal excretion
Combined with 2 NRTI’s |
|
|
Term
|
Definition
|
|
Term
| Nelfinavir Mech of Action |
|
Definition
| Protease inhibitor--> inhibits CYP3A system |
|
|
Term
|
Definition
| Ok’d in pregnant women as compared to other PI’s |
|
|
Term
| Nelfinavir absorption/interactions |
|
Definition
+ food—increase absorption
Multiple interactions
+ midazolam (sedative)
+ amiodarone (anti-arrhythmia)
+ quinidine |
|
|
Term
Dose limited diarrhea and flatulence
Hypersensitivity |
|
Definition
| Nelfinavir contraindications/adverse reactions |
|
|
Term
|
Definition
| Potent inhibitory effect of P450 3A4 isoenzyme—add to other PI’s as pharmacokinetic booster to increase drug exposure and ½ life |
|
|
Term
|
Definition
| Doesn’t necessarily treat anything—boosts activity of other drugs |
|
|
Term
| ritonavir absorption/interactions |
|
Definition
Preferred PI regiments
+ atazanavir 1x/day
+ darunavir 1x/day
+ foxamprenavir 2x/day
Loopinavir/ritonavir (corfumalated) 1x/2x/day
Take with food |
|
|
Term
Nausea
Diarrhea
Paresthesias
Hepatitis |
|
Definition
| ritonavir contraindications/adverse reactions |
|
|
Term
|
Definition
| List early inhibitors of the anti-retroviral drugs class |
|
|
Term
| Enfuvirtide mech of action |
|
Definition
Fusion inhibitor blocks entry
Inhibit fusion of viral and cellular membranes
Binds to viral envelop |
|
|
Term
| HIV infections in combination w/other anti-retroviral agents |
|
Definition
|
|
Term
Injection subq BID
No significant interactions |
|
Definition
| Enfuvirtide absorption/interactions |
|
|
Term
Hypersensitivity
Local injection site reactions
Diarrhea
Nausea
Aches, fatigue
Non-specific symptoms |
|
Definition
| enfuvirtide contraindications/adverse effects |
|
|
Term
| Maraviroc mech. of action |
|
Definition
CCR5 receptor antagonist
(genetics pg 186)
2nd line drug |
|
|
Term
|
Definition
Adults w/CCR5-tropic HIV-1
Resistance to other anti-retroviral agents |
|
|
Term
Muscle/joint pain
Diarrhea
Sleep disturbance
Increased liver enzymes |
|
Definition
| maraviroc contraindications/adverse reactions |
|
|
Term
| Raltegravir mech of action |
|
Definition
integrase inhibitor
Pyrimidinone analog
Binds to integrase (essential to replication of HIV-1/2)
Inhibits strand transfer |
|
|
Term
|
Definition
| Adult pts infected with strains of HIV-1 resistant to multiple agents |
|
|
Term
|
Definition
|
|
Term
Diarrhea, nausea, fatigue
Headache, Dizziness
Muscle aches
Increased Creatine kinase |
|
Definition
| raltegravir contraindications/adverse effects |
|
|
Term
| lamivudine, adefovir, interferon alfa, pegylated interferon alfa, ribavirin |
|
Definition
| List Anti-Hepatitis Agents for Hep B and C |
|
|
Term
Nucleoside reverse transcriptase inhibitor
Cytosine analog |
|
Definition
| lamivudine mech of action |
|
|
Term
|
Definition
|
|
Term
+ TMP-SMZ—increase Lamivudine AUC
Oral |
|
Definition
| lamivudine absorption/interactions |
|
|
Term
Hypersensitivity
Headache
Insomnia
Fatigue
Elevated LFT |
|
Definition
| lamivudine contraindications/side effects |
|
|
Term
|
Definition
Adenosine analog monophosphate
Inhibits HBV DNA polymerase--> chain termination |
|
|
Term
|
Definition
|
|
Term
+ ibuprofen—AUC increased
Oral |
|
Definition
| adefovir absorption/interactions |
|
|
Term
Hypersensitivity
Nephrotoxicity, lactic acidosis, hepatomegaly and steatosis |
|
Definition
| adefovir contraindications/adverse effects |
|
|
Term
| interferon alfa mech of action |
|
Definition
Endogenous protein
Antiviral effects through cellular metabolic process involving synthesis of both RNA/proteins |
|
|
Term
|
Definition
| interferon alfa indications |
|
|
Term
Reduces clearance of theophylline—increases levels
Subq or IM |
|
Definition
| interferon alfa absorption/interactions |
|
|
Term
Contra—psychosis, severe depression, neutropenia, thromcytopenia, uncontrolled seizures
Flu-like symptoms
Elevated LFT |
|
Definition
| interferon alfa contraindications/adverse effects |
|
|
Term
| pegylated interferon alfa mech of action |
|
Definition
| Polyethylene glycol (PEG) moiety attached to interferon, reduce clearance and sustained absorption |
|
|
Term
|
Definition
| pegylated interferon alfa indications |
|
|
Term
|
Definition
Unknown mechanism of action!
Broad spectrum anti-viral drug |
|
|
Term
|
Definition
Influenza A, B
Parainfluenza
RSV
Paramyxoviruses
HCV
HIV-1 |
|
|
Term
| ribavirin absorption/interactions |
|
Definition
Aerosol in Rx of chronic hepatitis C
Antagonizes anti-viral activity of Zidovudine
Oral |
|
|
Term
Contra—anemia, end stage renal failure, severe heart disease, pregnancy
Toxicity
Depression
Myelosuppression |
|
Definition
| ribavirin contraindications/adverse effects |
|
|
Term
| amantadine, rimantadine, zanamivir, oseltamivir (tamiflu) |
|
Definition
| List anti-influenza agents |
|
|
Term
| amantadine and rimantadine mech of action |
|
Definition
| 2 drugs that Inhibits uncoating of viral RNA influenza A within infected cell |
|
|
Term
| Prevention/tx of influenza A |
|
Definition
|
|
Term
|
Definition
| + anticholinergic drugs— additive anticholinergic effects |
|
|
Term
Hypersensitivity
Nausea
Vomiting
CNS agitation |
|
Definition
| rimantadine contraindications/adverse effects |
|
|
Term
|
Definition
Prophylaxis and tx of influenza A
Originally developed for Parkinson’s
Doesn’t work against influenza B!! |
|
|
Term
+ cimetidine—inhibits metabolism
+ anticholinergic drugs— additive anticholinergic effects |
|
Definition
|
|
Term
Hypersensitivity
GI intolerance
Nervousness
Lightheadedness
CNS effects more prominent |
|
Definition
| amantadine contraindications/adverse effects |
|
|
Term
| zanamivir and oseltamivir (tamiflu) |
|
Definition
2 drugs mech of action...
Neuraminidase inhibitors
Viral enzyme cleaves sialic acid residues—impedes viral spread |
|
|
Term
|
Definition
|
|
Term
| zanamivir interactions/absorption |
|
Definition
Intranasal
Limits usefulness
No interactions |
|
|
Term
Hypersensitivity
Nasal/throat discomfort
bronchospasm |
|
Definition
| zanamivir contraindications/adverse effects |
|
|
Term
| prevention/tx of influenza A and B |
|
Definition
| oseltamivir (tamiflu) indications |
|
|
Term
| + probenecid—increases serum levels (block kidney excretion) |
|
Definition
| oseltamivir (tamiflu) interactions |
|
|
Term
Hypersensitivity
GI upset
CNS agitation |
|
Definition
| oseltamivir (tamiflu) contraindications/adverse effects |
|
|
Term
| palivizumab mech of action |
|
Definition
| Humanizod monoclonal antibody directed against F glycoproteins on surface of RSV |
|
|
Term
|
Definition
| Prevent RSV in high risk infants/children |
|
|
Term
|
Definition
No interactions
Works well but cost about $1000/month! |
|
|
Term
Hypersensitivity
Injection site reaction
Increased LFT’s |
|
Definition
| palivizumab contraindications/adverse effects |
|
|
Term
|
Definition
| Immune response modifier—activate immune system |
|
|
Term
|
Definition
| Topical tx of external genital/perianal warts |
|
|
Term
|
Definition
| imiquimod administration/interactions |
|
|
Term
Hypersensitivity
Local skin irritation |
|
Definition
| imiquimod contraindications/adverse effects |
|
|
Term
Absorption/penetration into host cell
Uncoating of viral nucleic acid
Synthesis of early regulatory proteins
Synthesis of DNA/RNA
Synthesis of late, structural proteins
Assembly of viral particles
Release from cell |
|
Definition
| viral replication steps (7) |
|
|
Term
| anti-influenza drugs mech of action |
|
Definition
| work by uncoating virus/blocking neuraminidase inhibitors |
|
|
Term
|
Definition
| closely resemble either purines or pyrimidines—get incorporated into a growing DNA chain but they are structurally different so they cause chain termination once incorporated |
|
|
Term
| foscarnet differentiation |
|
Definition
| only anti-viral that doesn’t have purine/pyrmidine type look |
|
|
Term
| acyclovir, penciclovir, and ganciclovir resistance |
|
Definition
| Viruses that mutate and change enzyme thymidine kinase develop resistance to |
|
|
Term
-NRTI’s are picked up by RT and altered structure works to prevent action of RT
-NRTI’s actually bind to different site and block enzyme directly |
|
Definition
| key distinction between NRTI's and NNRTI's mech of action |
|
|
Term
Reduction of moribidity associated with HIV
Prolongation of survival
Improvement of the patient’s quality of life
Restoration/maintenance of immunologic function
Suppression of viral load
Prevention of vertical transmission |
|
Definition
| goals of anti-retroviral therapy |
|
|
Term
| decreased risk of HIV-associated complications, non-opportunistic infections and HIV transmission |
|
Definition
| Benefits of early anti-retroviral tx include |
|
|
Term
| drug-related adverse reactions, resistance, and increased medication time |
|
Definition
| Potential harms of early anti-retroviral tx include |
|
|
Term
Nucleoside analogs:
Acyclovir, cidofovir, famciclovir, ganciclovir, penciclovir, trifluridine, valacyclovir, vidarabine
Others:
foscarnet, fomivirsen |
|
Definition
drugs used for herpes infections...
nucleoside analogs (8)
others (2) |
|
|
Term
|
Definition
acyclic cytosine nucleotide analog with in vitro activity
already has phosphate attached—doesn’t need thymidine kinase |
|
|
Term
|
Definition
CMV retinitis
HSV-1/2
VZV
EBV
HHV-6/8
Adenovirus
Poxviruses
Polyomaviruses
Human papillomavirus |
|
|
Term
| Prehydrate with normal saline—reduce neprhotoxicity |
|
Definition
| cidofovir administration/interactions |
|
|
Term
| Dose-dependent proximal tubular nephrotoxicity |
|
Definition
| cidofovir adverse reactions |
|
|
Term
Abacavir
Didanosine
Emtricitbine
Lamivudine
Stavudine
Tenofovir
Zidovudine– AZT, 1st one developed |
|
Definition
|
|
Term
Atazanavir
Darunavir
Fosamprenavir
Lopinavir
Nelfinavir
Ritonavir |
|
Definition
| Protease Inhibitors list (6) |
|
|
