Antivirals and Disinfectants Flashcards
NRTIs
abacavir (ABC) • didanosine (ddI) • emtricitabine (FTC) • lamivudine (3TC) • stavudine (d4T) • tenofovir (TDF) – nucleotide reverse transcriptase inhibitor • zidovudine (AZT)
NNRTIs
non nucleoside transcriptase inhibitors
delavirdine (DLV) • efavirenz (EFV) • etravirine (ETV) • nevirapine (NVP) • rilpivirine (RPV)
PIs
Protease Inhibitors
amprenavir (APV) • atazanavir (ATV) • fosamprenavir (f-APV) • indinavir (IDV) • lopinavir/ritonavir (LPV/r) • nelfinavir (NFV) • ritonavir (RTV or r) • saquinavir (hard gel capsule and tablet formulations) (SQV) • tipranavir (TPV) • darunavir (DRV)
Additional Agents for secondary treatment
Fusion inhibitor – enfuvirtide (T20) • CCR5 antagonist – maraviroc (MVC) • Integrase inhibitor – raltegravir – elvitegravir – dolutegravir
Tenofovir Disoproxil Fumarate (Viread)
• Take without regard to food • Adverse effects - renal insufficiency • Special considerations – renal dosing – use with emtricitabine for pre-exposure prophylaxis (PrEP) and post- exposure prophylaxis (PEP)
Emtricitabine (Emtriva)
• Take without regard to food
• Adverse effects
– Hyperpigmentation of the palms
– Skin discoloration
Well tolerated and does not usually have any adverse effects
*looks like secondary syphilis
Zidovudine (Retrovir)
• Taken without regard to food
• Adverse effects
– hyperpigmentation of nails and toes (next slide)
– bone marrow suppression
Used as an IV infusion peripartum in women who have viral loads > 400
** drug of choice for pregnant women
Lamivudine (Epivir)
• Taken without regard to food • Adverse effects – diarrhea – malaise, fatigue – headache • Special considerations – Epivir HBV! • Caution! – Renal dosing requirements **paired with Zidovudine and used for pregnant women
Combination Products
• emtricitabine + tenofovir (Truvada®) – 1 tablet PO daily
emtricitabine + tenofovir + efavirenz (Atripla®) – 1 tablet PO daily
emtricitabine + tenofovir + elvitegravir + cobicistat (Stribild®) – 1 tablet PO daily
Efaviranz (Sustiva)
• Avoid taking with high-fat foods – increases serum concentrations by 39-79% – take on empty stomach • Adverse effects – central nervous system (CNS) effects • 52% of patients in clinical trials • subside after 2-4 weeks – rash – elevated liver function tests (LFTs) – teratogenic – false-positive cannabinoid test! • Drug interactions – Mixed CYP450 3A4 inducer and inhibitor
- needs to be taken right before bed
- *cannot be used for pregnant women
Rilpivirine (Edurant)
non nucleoside • Not for use in high viral loads Drug interactions – CYP450 inducer – Avoid use with proton pump inhibitors
Nevirapine (Viramune)
• Take without regard to food
Adverse Effects:
– hepatitis, including fatal hepatic necrosis
– higher frequency in women with CD4 > 250, men with CD4 > 400
» avoid initiation in these populations
PIs Class Issues
– Drug interactions • Emphasize importance of using same pharmacy for all prescriptions – Metabolic syndrome • Insulin resistance/hyperglycemia • Increased cholesterol and triglycerides • Lipodystrophy/fat redistribution – Heptatotoxicity – GI intolerance – Osteopenia and osteoporosis
Ritonavir (Norvir)
pharmacokinetic booster with other protease inhibitors • 100-400mg/dayin1-2divided doses • Do NOT refrigerate oral solution • Adverse effects – GI upset – taste perversion – circumoral tingling
Atazanavir (Reyataz)
• Take with food
• Special considerations
– separate dosing from antacids and H2-blockers – proton pump inhibitors
• when to avoid
• Adverse effects
– indirect hyperbilirubinemia – prolonged PR interval on EKG – nephrolithiasis
– lack of effect on lipids!
Darunavir (Prezista)
• Take with food
• Special considerations
– Must take darunavir and ritonavir at the same time – Caution in sulfa-allergic patients
– New 600 mg tablet arrived in late spring 2008
• Adverse effects – Rash
Lopinavir/ritonavir (Kaletra)
• Take without regard to meals • Special considerations – Melt-extrusion technology • No refrigeration needed!! – Drug of choice in pregnancy • Adverse effects – asthenia – as with ritonavir
Integrase Inhibitor Raltegravir (Isentress)
• Take without regard to food • Special considerations – metabolized by glucuronidation • Adverse effects – headache – nausea – diarrhea – increased creatine kinase
Integrase Inhibitor Stribild®
• Take with food • Special considerations • “Quad Pill” – Drug interactions – Elevations in serum creatinine – Increased creatine kinase
Initial Treatment Considerations
– Results from resistance testing – Dosing convenience/adherence issues – Adverse effects – Drug interactions – Pregnancy potential/CD4 count – Comorbidities