Antivirals Flashcards
Agents for HSV and VZV
Oral: Zovirax, Valtrex, Famvir, Topical: Denavir (penciclovir), Abreva (Docosanol)
Oral Agent MOA
Nucleoside Analog, Inhibition of viral DNA synthesis
Acyclovir
More potent for HSV 1&2, also covers VZV, ONLY ONE AVAILABLE AS IV, Small F, decrease duration of herpes by 2 days, ADE: ND
Acyclovir ADE
HA!, Nausea, Diarrhea, generally well tolerated, Note: lots of H2O to stop kidney stone formation
Valacyclovir
Much better F, w/ high doses- confusion/hallucinations, More ADE in aids pt’s and transplant pt’s
Famciclovir
converted to pencyclovir, EBV(epstein-Barr), Hep-B, HSV and VZV, does not cause chain termination, generally well tolerated, same side effects as Acyclovir
Acyclovir vs Valacyclovir
valacyclovir has shorter duration of zoster pain followed by famciclovir then acyclovir
Abreva (docosanol)
Penciclovir (Denavir)-metabolite of famciclovir
w/in 12 hours of prodromal symptoms (tingling/numbness) when used 5x’s daily with valacyclovir will shorten cold sores by 18 hours. (abreva- prevents viral entry into cells)
Anti-retroviral Agents
NRTI, NNRTI, PI, Integrase Inhibitors, CCR5 receptor antagonists, Fusion Inhibitors
ART Standard of Care
Combination of 3-4 antiretroviral agents, viral susceptibility to specific agents varies among pt’s
When to Initiate TX
for all HIV infected pt’s
Preferred Regimen
2 NRTI (tenofovir/Emtricitabine)!!!!!, then add on another agent or two that are different (Atripla, Truvada…)
ATR things to consider
Tolerability, convenience, Adherence, Co-morbid conditions, pregnancy, ADE
NRTI
HIV 1&2, inhibits reverse transcriptase (chain termination), BACKBONE OF ART, no food efffect, available in one tab combined (Emtricitabine, Tenofovir, Zidovudine, Abacavir, Lamivudine)
Emtriva (emtricitabine) NRTI
Emtricitabine, ADE: HA, ND, Asthenia, Hyperpigmentation of palms, Lots of combo products available, FOR Hep-B, QD DOSING, no drug-drug interactions
Viread (tenofovir) NRTI
pro-drug, combo products, GI complaints, HA, asthenia, some RENAL IMPAIRMENT, DECR. BONE MINERAL DENSITY AND TOXICITY
Retrovir (zidovudine) NRTI
Zidovudine, GI, Insomia, Lipoatrophy (more when administered w/ other agents, preferred FOR PREGNANT women w/ lamivudine, bid
Epivir (lamivudine) NRTI
can be used in women and infant populations
Ziagen (abacavir) NRTI
hypersensitivity 3-5% of people w/ HLA-B5701 allele, BID, no food effects, use cautiously in CV risk patients
NNRTI
MOA: bind reverse transcriptase (binding site near NRTI site)/(do not require phosphorylation), not effective against HIV-2, base-line genotype testing b/c resistance (2-8%), Disadvant- greater risk of resistance, can have lots of DDI b/c METABOLIZED BY CYP450
Sustiva (efavirenz) NNRTI
not in first trimester!!, CNS EFFECTS mostly which dimisnishes w/ continued tx, SKIN RASH (28%), disadvantages: neural tube defects, neuropsychiatric effects (not w/ high fat meal)
Edurant (rilpivirine) NNRTI
depressive disorders, rash, hyper-lipidemia, must have acidic pH, NO PPI,
Protease Inhibitors
HIV 1&2, prevent processing of viral proteins, LOTS OF METABOLIC COMPLICATIONS (INCREASED TG AND LDL, INSULIN RESISTANCE), fat redistribution worst w/ this group!!, CYP3A4 inhibitors, no phosphorylation needed
Norvir (ritonavir) PI
will increase plasma levels of other PI’s, ADE: GI disturbances, recommended when possible w/ all PI’s
Reyataz (atazanavir) PI
Atazanavir, NO EFFECTS ON LIPIDS, FAT REDISTRIBUTION OR METABOLIC SYNDROME, absorption depends low gastric pH and some food, NO MI OR STROKE RISK, PPI contraindicated!!, to be boosted w/ ritonavir, disad: (HYPEBILIRUBINEMIA)
Prezista (darunavir) PI
Darunavir, dyslipidemia, liver toxicity, boosted w/ ritonavir, CAN BE GIVEN W/ PPI !!!!, MANY DDI, skin rash, food requirements, watch pt’s w/ sulfa allergy
Kaletra (lopinavir) PI
Lopinavir, SHORT TERM USE IN PREGNANCY, elevated TG and cholesterol, BID ideal, High risk of MI
Integrase Inhibitors
block enzyme responsible for replication of HIV 1&2, Raltegravir, elvitegravir, dolutegravir
CCR-5
bind chemokine co-receptor on CD4 cells, prevent HIV entry, Maraviroc
Isentress (raltegravir)
Integrase Inhib.
less DDI than PI’s or NNRTI regimens!!, BID, no food effect, increased CPK = increased rhabdomyolysis
Stribild (elvitegravir)
Integrase Inhib.
CrCl>70ml/min, cobicistat to boost elvitegravir, new onset or worsening renal impairment, food requirement, proximal renal tubulopathy
Tivicay (dolutegravir)
Integrase Inhib.
avoid antacids, qd-bid dosing
Selzentry (maraviroc)
CCR-5
used for R5-HIV, test w/ tropism assay before tx, compared to efavirenz it has less ADE, DDI
Hep-B
we can only suppress NOT treat, 1st line tx: Pegylated interferon alpha-2a, entecavir, tenofovir (KNOW ALL 3!)
Hep-C
most common chronic blood-borne infection in US, 5x’s more common than HIV,
Hep-C
most common chronic blood-borne infection in US, 5x’s more common than HIV
Simeprivir - NS3/4a PI
two forms of birth control for men and women, SUN SENSITIVITY, not for use w/ sulfa aller.
NS5B PI
Sovaldi (sofosbuvir)- two forms of BC to be on, life threatening bradycardia
NS5A replication complex inhibitors
Ledipasvir or ombitasvir,
Interferon and Pegylated Alfa
moa: inhibits viral penetration, translation, and transcription, (pegylated means we give it less often), long half life (up to 160 hrs), ADE: flu like symptoms (30%), Black Box Warnings
Ribavirin
inhibits replication of DNA and RNA viruses, DON’T USE in pregnancy, large spectrum of activity (HIV, RSV, Influenza A and B)
To treat Influzenza A
amantadine, rimantadine, older treatment, not used much
Oseltamivir (tamiflu) and Zanamivir (ralenza)- as an inhaler
neuraminadase inhibitor, for influenza A and B, inhibit release of progeny to new host cells when administerd 36-48 hours after onset of sx, (decrease sx and will decrease overall conditions by 1-2 days)
Osteltamivir
Tamiflu, prodrug, NVD, abdominal pain
Zanamivir
Relenza, ADE: cough bronchospasm, deceased pulmonary function, nasal throat discomfort
ARV
HAART
ART
Anti-retroviral, Highly active anti-retroviral therapy, Anti-retroviral therapy
NS3/4a PI
1st gen- Boceprevir/Telaprevir
2nd gen- simveprevir/paritaprevir/asunaprevir)
