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51 Cards in this Set
- Front
- Back
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Drugs for herpes
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Acyclovir
Gancyclovir Cidofovir Foscarnet |
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Uses for acyclovir
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HSV (esp 1 and 2)
HSV encephalitis (decrease mortality by 50%) prophylaxis against HSV in IC Prophylaxis against CMV sero+ reactivation in IC severe VZV (esp of eye) in IC |
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ADME of acyclovir
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15-30% bioavailibility
CSF = 50% of serum 15% metabolize Renal excretion with T1/2 = 2.5 hours |
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Adverse effect and interaction with acyclovir
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No real side effects unless impaired renal function
Encephalopathy in 1% of IV admin with unexpectedly high levels Probencid inhibits excretion Acyc reduces elimination of methotrexate |
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Use of Gancyclovir
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Only approved for CMV
has effect with HSV 1-2 |
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MOA of ganciclovir
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like acyclovir but better substrate for host phorphorylation (CMV won't phosphorylate acyclovir)
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ADME ganciclovir
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IV only
Good CNS penetration Reneal excretion with T1/2 = 3-4 hours |
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Adverse effect of ganciclovir
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1/3 experience bone marrow suppression and must come off
5-15% CNS toxicity |
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Cidofovir resistance
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Phorphorylated by cellular enzyme so low resistance
No cross-resistance expected |
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Cidofovir ADME
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IV drug
17-65 hour half life (no need for permanent IV) |
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Adverse effect of cidofovir
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1/4 get nephrotoxicity, ocular hypotnia, neutropenia and acidosis
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MOA for foscarnet
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Inhibits DNA polymerase and reverse transcriptase at different site than other HSV drug so no resistance is seen
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Use of Foscarnet
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CMV retinitis
CMV prophylaxis Acyclovir resistant HSV Gancyclovir resistant CMV |
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Your AIDS patient get CMV but is resistant to gancylovir tx. What should you use?
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Foscarnet
Different site of action so no cross-resistance |
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ADME of Foscarnet
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IV, but poorly soluble so large amounts needed
Renally excreted Accumulates in bone |
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Adverse effect of cidofovir
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1/4 get nephrotoxicity, ocular hypotnia, neutropenia and acidosis
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MOA for foscarnet
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Inhibits DNA polymerase and reverse transcriptase at different site than other HSV drug so no resistance is seen
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Use of Foscarnet
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CMV retinitis
CMV prophylaxis Acyclovir resistant HSV Gancyclovir resistant CMV |
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Your AIDS patient get CMV but is resistant to gancylovir tx. What should you use?
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Foscarnet
Different site of action so no cross-resistance |
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ADME of Foscarnet
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IV, but poorly soluble so large amounts needed
Renally excreted Accumulates in bone |
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Adverse effects of Foscarnet
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Causes nephrotoxicity and hypocalcemia
anemia CNS toxicity w/ AMP-B is particularly nephrotoxic w/ Pentamidine is particualrly bad for hypocalcemia |
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Drugs used for HIV Tx
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Zidovudine
Lamivudine Didanosine Nevirapine Tenofovir Ritonavir Indinavir |
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Which two drugs has phosphonate diesters
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Cidofovir
Tenofovir |
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Zidovudine
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AZT
RT inhibitor (nucleoside analog) Recommended only for HIV |
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ADME Zidovudine
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Oral absorbed
Good distribution Some renal, mostly hepatic T1/2 = 1 hour, give every 4 |
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Side effect of Zidovudine
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Granulocytopenia
Anemia 50% of people Dose dependent, limiting |
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Drug interaction with Zidovudine
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Bone marrow supression with Ampho B and TMP/SMX (glucourondiation)
Nephrotoxic (and probenicid may inhibit clearance) |
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Didanosine
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nucleoside analog RT inhibito
for kids or adults in whom Zidovudine isn't working |
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Adverse effects and SE of Didanosine
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30% peripheral neuropathy
10% pancreatitis GI symptoms |
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Lamivudine
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Use with Zidovudine for Ping-Pong resistance, better serum HIV lowering and few additional side effects
Pancreatitis rare additional side effect of Lamivudine |
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Side effects of Lamivudine vs Zidovudine
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Lam has the same ones, but less frequently and not additive when used together
Pancreatitis is rare additional side effect |
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Unusual use for lamviduine
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Hepatitis B
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HIV drug also useful in Hep B
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Lamivudine
Tenofuvir |
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Nevirapine
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NON-nucleoside analog whose use remains to be determined
May cause severe rash |
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Tenofuvir
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Nucleotide analog RT inhibitor
Given once daily and does not require phorphorylation |
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Side effects of Tenofuvir
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Fanconi's syndrome (nephrotoxicity)
Not for kids or pregnant |
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Ritonavir
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PI with ton's of drug interactions!
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Ritonavir ADME and interactions
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Give twie daily with meal in ethyl alcohol solution (disufuram and metronidazole are a problem)
Interacts adversly with any drug metabolized by the P450 3A system |
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Side of effect of Ritonaivr
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Circumoral paresthesia
Elevates liver enzymes, CK's and TG's |
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Use of Ritonavir
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With RT inhibitors for HIV
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ADME of Indinavir
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Take every 8 hours, not three times a day, while fasting
Effects P450, but 20% renal excreted Use with Didanosine inhibits abosorption, use 1 hous apart |
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Indinavir Drug interactions
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Ketoconazole interferes with metabolism
Didanosine inhibits its absorption Effects any drug metabolized by P450, though not as badly as Ritonavir |
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Side Effect of Indinavir
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Renal stones (drink 1.5 L of water)
Gi Distress Elevated Bilirubin |
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Elevates Bilirubin, but not as a sign of hepatitis
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Indinavir
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Causes nephrolithiasis
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Indinavir
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Enfuravirtide
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SC injected fusion inhibitor. Expensive, complicated, and in short supply
but it works! |
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Amantadine for flu prophylaxis
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5 weeks alone
2 weeks with vaccination |
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ADME Amantadine
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Oral
Not metabolized, renal excretion 12-18 hour half life |
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Side effect of Amantadine
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CNS toxicity at high dose. Releases dompamine, which inhibits ACh (used for parkinson's). Anticholinergics make it even worse
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Rimanatdine
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Amantadine but metabolized by liver. Used for Renal imparied patients
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Oseltamavir and Zanamavir
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Neuraminidase inhibitors
Zanamavir make cause brochospasm in asthmatics |
