Hepatitis + HIV Treatment PDF

Hepatitis B (HBV) Treatment Drug Classification MOA Metabolism & Excretion Side Effects Lamivudine (DOC) Cytosine analogue Turns into an active Metabolism: minimal, Nausea...

Hepatitis B (HBV) Treatment Drug Classification MOA Metabolism & Excretion Side Effects Lamivudine (DOC) Cytosine analogue Turns into an active Metabolism: minimal, Nausea metabolite when it’s mainly intracellular by - 100 mg PO QD Nucleoside reverse phosphorylated by the sulfotransferase Vomiting transcriptase and host cell using L-TP polymerase inhibitor Excretion: urinary HA This active form is then (mainly unchanged) Also used in HIV incorporated into viral Nephrotoxicity treatment DNA which disrupts the ½ life = 7 hrs process of viral replication CYP450 minimal The fraudulent viral DNA terminates chain elongation by interfering w/ HBV’s DNA polymerase and HIV reverse transcriptase Adefovir dipivoxil Adenosine nucleotide Same as ^ Metabolism: analog which leads to phosphorylation; - Oral termination of HBV prodrug converted to administration of DNA adefovir active form 10 mg once a day Excretion: urine (45% unchanged) ½ life = 7 hrs CYP450 none, prodrug converted to adefovir active form Entecavir (Baraclude) Deoxyguanosine analog Inhibits reverse Metabolism: Minimal HA transcriptase, DNA - Oral admin 1 mg Effective in replication, and Excreted by glomerular Fatigue daily Lamivudine-resistant transcription filtration and tubular HBV secretion Nausea, dizziness Hepatitis C (HVC) Treatment Drug Classification MOA Metabolism & Excretion Side Effects Mavyret A fixed-dose An inhibitor of the HCV Metabolism: Liver failure (Pibrentasivir/Glecaprev combination product NS3/4A protease which Glecaprevir: liver, ir) containing Glecaprevir is necessary for the partially CYP3A4 Angioedema (HCV NS3/4A protease proteolytic cleavage of Indicated for the tx of inhibitor) and the HCV-encoded Metabolism: HVB reactivation patients w/ chronic HCV Pibrentasivir (HCV NS5A polyprotein and for viral Pibrentasivir: none (patients with a hx) genotype 1, 2, 3, 4, 5, or 6 inhibitor) replication infection without HA cirrhosis and with Pibrentasivr is an Excretion: Glecaprevir is compensated cirrhosis inhibitor of HCV NS5A, in the feces versus Nausea (Child-Pugh A) which is essential for Pibrentasivir is in the viral RNA replication urine Diarrhea and virion assembly Rash Epclusa Combination of NS5A polymerase Metabolism: Sofosbuvir: Bradycardia HBV (past Sofosbuvir, an inhibitor inhibitors: interacts w/ liver extensively CYP450 hx) Indicated for genotypes of the HCV NS5B, and viral and host proteins none, a prodrug 1-6; patients with Velpatasvir, an inhibitor converted to active Reactivation decompensated of the HCV NS5A NS5B polymerase metabolite angioedema cirrhosis (Child-Pugh B protein inhibitors: interferes w/ or C) should be the viral RNA Metabolism: Velpatasvir: HA administered with polymerase liver CTYP 2B6, 2C8, 3A4 weigh-based ribavirin Diarrhea dosing Excretion: Sofosbuvir is Rash in the urine (80%) versus Velpatsavir is in Nausea the feces/bile (94%) Vomiting HIV Treatment Class MOA Adverse Reactions Drugs Notes Viral fusion inhibitors Inhibits entry of the viral Enfuvirtide HAART (Highly Active RNA into the host cell Antiretroviral Therapy) by inhibiting GP41 binding to CD4 2 NRTI’s + NNRTI Attachment Inhibits entry of the viral Maraviroc 2 NRTI’s + coreceptor inhibitor RNA into the host cell Integrase by inhibiting GP120 inhibitor binding to CCR5 2 NRTI’s + NRTI’s (ZALES TD) Inhibit the reverse Mitochondrial toxicity* Zidovudine Protease transcriptase from Myopathy inhibitor taking RNA and making Peripheral Abacavir neuropathy Adjuvant therapy DNA by stopping the Hepatic steatosis Lamivudine growing DNA template Lactic acidosis Enfuvirtide By acting like a Emtricitabine Maraviroc nucleotide even Others though it’s not Pancreatitis Stavudine It will terminate Nephrotoxicity the actual Hypersensitivity Tenofovir reaction formation of DNA Didanosine off of this RNA template strain NNRTI’s (-vir) Allosteric inhibitors Hepatotoxicity Nevirapine Binds onto a particular site CNS toxicity (dizziness Efavirenz or mood changes) Inhibiting the Etravirine reverse Rash transcriptase Delaviridine enzyme from Teratogenic effect being able to Rilpivirine function properly Protease Inhibitors Inhibit protease → won’t Crystal-induced Atazanavir (-navir) be able to cleave the nephropathy polyproteins that were Darunavir CYP450 inhibitor translated Indinavir They won’t be able to make any Lopinavir structural and functional Nelfinavir proteins Essentially then Saquinavir can’t make new Tipranavir virus Ritonavir Integrase Inhibitors Inhibit integrase → not Rhabdomyolysis Dolutegravir (-tegravir) allowing for the incorporation of viral Raltegravir DNA with host DNA Elvitegravir Respiratory Syncytial Virus (RSV) Drug MOA Admin Adverse Effects Metabolism & Excretion Amantadine Dopaminergic drug 100 mg PO BID x 3-5 d, Ataxia Metabolism: liver start within 48 hrs of conjugation Tx of Parkinson’s symptoms Seizures Excretion: urine (50-90% disease DOES cross BBB Insomnia unchanged) Dizziness GI intolerance Prolonged QT interval Rimantadine ^ Same dose and admin Fewer SE but seizures, Metabolism: liver as ^ insomnia, dizziness and extensive ataxia can occur Less lipophilic and does Excretion: urine (