Antivirals lecture Flashcards
6 Classes of Antiretrovirals
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Non-nucleoside reverse transcriptase Inhibitors (NNRTIs)
Protease Inhibitors (PIs)
Fusion Inhibitors
CCR5 Antagonist
Integrase Inhibitor
Initial Treatment for HIV
- Tenofovir/emtricitabine = Dual nucleoside backbone (NRTIs)
- Efavirenz (NNRTI)
- Atazanavir/ritonavir OR Darunavir/ritonavir (PIs)
- Raltegravir (Integrase Inhibitor)
Two major NRTIs
Emtricitabine (FTC), Tenofovir (TDF)
Major NNRTI
Efavirenz (EFV)
Two major PIs
Atazanavir (ATV) Darunavir (DRV)
Major Integrase Inhibitor
Raltegravir
Tenofovir Disoproxil Fumarate
- Category; use
- Adverse effects
- Special considerations
- Other
- NRTI; dual nucleoside backbone w/ emtricitabine
- renal insufficiency (increased serum Crt; check every time you see the pt; urinalysis q1yr); lactic acidosis
- Renal dosing; use with emtricitabine for pre-exposure prophylaxis (PrEP) & post-exposure prophylaxis (PEP)
- Take w/o regard to food; may cause N/V diarrhea/flatulence
Emtricitabine
- Category;use
- Adverse effects
- NRTI; dual nucleoside backbone w/ tenofovir
- Minimal toxicity; hyperpigmentation of the palms (may mimick 2nd syphilis, dot-like); skin discoloration
Zidovudine
- Use
- Adverse effects
- FOR USE IN PREGNANT WOMEN w/ viral loads > 400 + Lamivudine as IV infusion
- Bone marrow suppression (macrosidic anemia)
Lamivudine
- Use
- Adverse effects
- Used for pregnant women w/ viral loads >400 + Zidovudine; 300 mg QD
- Epivir HBV (occasionally used for HBV tx in a much lower dose (100 mg QD)
Major 3 Combination Products
- Generic/Brand names
- Categories
- Frequency
- Emtricitabine +Tenofovir (Truvada) - 1 tablet PO QD
- Emtricitabine + Tenofovir + Efavirenz (NNRTI) (Atripla) - 1 tablet PO HS
- Emtricitabine + Tenofovir + Elvitegravir + Cobicistat (booster + integrase inhibitor) (Stribild) - 1 tablet PO QD
Efaviranz
- Category; frequency
- Considerations
- Adverse effects
- Other
- NNRTI; 600 mg PO HS
- Avoid taking w/ high-fat foods – take on empty stomach (food INCREASES the serum [drug])
- Adverse effects: CNS effects (dizziness, drowsiness, hallucinations/ nightmares) subside w/in 2-4 wks; Rash; Elevated LFTs (MONITOR); TERATOGENIC (okay if she has been on it for a long time; ask about plans for pregnancy); False- + Cannabinoid test
- Drug Interactions: CYP450
Rilpivirine
- Considerations
- Drug Interactions
- Not for use in high viral loads (>100,000)
- Drug interactions: CYP450 Inducer; AVOID USE WITH PPIs!! (needs acidic environment to be absorbed)
Nevirapine
- Use
- Adverse Effects
- Other
- RTI for Pregnancy
- Increased LFTs; hepatitis, including fatal hepatic necrosis: higher frequency in women with CD4 >250 (men CD4 > 400) AVOID INITIATION for people with PRESERVED immune systems (may be initiated w/ increased viral load)
- CYP450 Inducer; counsel pt about mild-moderate rash vs anaphylaxis
Protease Inhibitors: major class issues
- Drug Interactions
- Metabolic syndrome
- Other
- Drug interactions: important to use same pharmacy for all prescriptions
- Metabolic syndrome: insulin resistance/ hyperglycemia; increased cholesterol & TGs, lipodystrophy/ fat redistribution
- Hepatotoxicity, osteopoenia/porosis
Ritonavir
- Use
- Considerations
- Adverse effects
- Used as a pharmacokinetic BOOSTER with other PIs (works on CYP450 in increase [drug])
- Refrigerate capsules but NOT PO sol’n
- Adverse effects: G.I upset, tingling
Atazanavir
- Use
- Special considerations
- Adverse effects
- If used with Atripla, add ritonavir
- Separate dosing from antacids, H2blockers – PPIs: Omeprazole OTC may be used if 12 hours AFTER Atazanavir (only PRN)
- Indirect hyperbiliruminemia (check TBili; most effect may be on sclera: jaundice (rarely systemic)); no effect of lipids (ok for high cholesterol)
Darunavir
- Special considerations
- Adverse effects
-Must take with ritonavir at the same time; CAUTION in sulfa-allergic pts
-Rash (low %)
Hepatotoxicity: primarily with HBV/HCV or with advanced HIV & multiple meds
Lupinavir/ ritonavir
- Use
- Other
Major drug of choice in pregnancy (with DNRTIS)
-Effects: G.I. upset, tingling, asthenia