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PHRM 865: Theraputics V > Lecture 23.1: Antivirals > Flashcards

Lecture 23.1: Antivirals Flashcards

1
Q

What is the Mechanism of Action for Acyclovir?

A
  • Inhibition of Viral DNA Replication
  • Prodrug –> Acyclovir Triphosphate
  • Viral Kinases = 1 Phos & Human Kinases = 2 & 3 Phos
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2
Q

What is the spectrum of Activity for Acyclovir?

A
  • Herpes Simplex Virus 1 & 2 [HSV 1 & 2]
  • Varicella Zoster Virus [VZV]
  • HSV-1 > HSV-2 > VZV > EBV&raquo_space; CMV
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3
Q

What is the Pharmacokinetics of Acyclovir?

A
  • Very BAD orally [10-20%]; food dont help; Dose Dependent
  • Widely distributed in body; correlates with Body H20
  • Eliminated Renally by Glom and Tub = Renal Adjustments
  • Removed During Hemodialysis
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4
Q

What are some of the clinical indications for Acyclovir?

A
  • HSV Primary, Recurrent, Chronic
  • HSV Encephalitis 10mg/kg IV [IV gets to brain]
  • Muscocutaneous Disease 5mg/kg IV
  • Shingles
  • Severe VZV 10mg/kg IV

Dose adjust in obese people

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5
Q

What are some of the Adverse Effects for Acyclovir?

A
  • Nausea, Vomiting Diarrhea [Very Common]
  • Nephrotoxicity [Crystals]
  • Neurotoxicity [Reversible]
  • Thrombophlebitis
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6
Q

What is the Mechanism of Action for Valacyclovir?

A
  • L-Valyl ester PRODRUG of Acyclovir
  • Inhibition of Viral DNA Replication
  • Prodrug –> Acyclovir Triphosphate
  • Viral Kinases = 1 Phos & Human Kinases = 2 & 3 Phos
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7
Q

What is the Spectrum of Activity for Valacycolvir?

A
  • HSV-1 & 2
  • VZV
  • HSV-1 > HSV-2 > VZV > EBV&raquo_space;CMV
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8
Q

What is the Pharmacokinetics for Valacyclovir?

A
  • Rapidly absorbed and completely converted to Acyclovir by Intestinal and hepatic metabolism = orally
  • Bioavailability GREATER
  • Removed via hemodialysis

ALL BECAUSE OF THE L-VALYL ESTER

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9
Q

What are hte clinical indications for Valacyclovir?

A
  • Core Sores
  • VZV [preferred over acyclovir]
  • HSV Primary, Recurrent, Chronic

Adjust for renal issues

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10
Q

What are the Adverse Effects for Valacyclovir?

A
  • Nausea, Vomiting Diarrhea [Very Common]
  • Nephrotoxicity [Crystals]
  • Neurotoxicity [Reversible]
  • Thrombophlebitis

same as acyclovir

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11
Q

What is the Mechanism of action for Famciclovir?

A
  • PRODRUG of Penciclovir –> Oral Fam rapidly converts to Pen
  • Pen get Phos by viral kinase to Pen Mono –> cellular kinase to Pen Tri = Inhibition of Viral Replication
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12
Q

What is the Spectrum of Activity for Famciclovir?

A
  • HSV-1
  • HSV-2
  • VZV

same as Acyclovir

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13
Q

What is the Pharmacokinetics for Famciclovir?

A
  • Well Absorbed Orally; Food slows absorption [no need for food]
  • Half Life 2.5h
  • ~90% unchagned in urine
  • Dose reduction in renal issues
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14
Q

What are some of the Clinical indications for Famciclovir?

A
  • Cold Sore 1.5g once
  • HSV Primary 250mg PO TID, Recurrent 125mg PO BID, Suppression 250 PO BID
  • VZV 500mg PO TID
  • HIV 500mg PO BID
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15
Q

What are som eof the Adverse Effects for Famciclovir?

A
  • Well Tolerated
  • Headache, Nausea, Vomiting, Diarrhea

DI: Probenecid decreases renal clearence

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16
Q

What is the Mechanism of Action for Ganciclovir?

A
  • HSV & VZV: Viral Thymidine Kinase phos it
  • CMV: CMV-encoded protein kinase phos it once –> then cellular for 2 & 3 Phos
  • Ganciclovir tri INHIBITS viral DNA poly = inhibits viral replication

CMV Protein = UL97 gene

Resistance = UL97 Gene mutations

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17
Q

What is the Spectrum of Activity for Ganciclovir?

A
  • HSV-1 & HSV-2
  • VZV
  • CMV
  • EBV
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18
Q

What is the Pharmacokinetics for Ganciclovir?

A
  • Low Oral Bioavailability
  • Able to get into the EYE
  • > 90% unchanged renally = DOSE adjust
  • 50% removed during hemo
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19
Q

What is the Clinical indications for Ganciclovir?

A
  • CMV Retinitis
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20
Q

What are some of the adverse effects for Ganciclovir?/

A
  • Bone Marrow Suppression [reversible]
  • Neutropenia is ~40%; can treat that with G-CSF
21
Q

What is the mechanism of action for Valganciclovir?

A
  • L-Valyl Ester of Ganciclovir = rapidly converted to Gan by intestinal and hepatic esterases
  • HSV & VZV: Viral Thymidine Kinase phos it
  • CMV: CMV-encoded protein kinase phos it once –> then cellular for 2 & 3 Phos
  • Ganciclovir tri INHIBITS viral DNA poly = inhibits viral replication
22
Q

What is the Spectrum of Activity for Valganciclovir?

A
  • HSV-1 & HSV-2
  • VZV
  • CMV
  • EBV
23
Q

What is the Pharmacokinetics for Valganciclovir?

A
  • Increased bioavailability of GAN when given as Val-GAN
  • Major route of elim = Renal; Adjust Dose
  • Hemo decerases GAN conc.
24
Q

What are the indications for Valganciclovir?

A
  • CMV Retinitis
25
Q

What are the adverse effects of Valganciclovir?

A
  • Bone Marrow Suppression [reversible]
  • Neutropenia is ~40%; can treat that with G-CSF
  • Hemtologic Toxicity
26
Q

What is the mechanism of action for Letermovir?

A
  • Inhibits the pUL56 subunit of the viral terminase complex of CMV
  • Inhibition of CMV replication and prevention of CMV infections
27
Q

What is the spectrum og activity for Letermovir>

A
  • CMV
28
Q

What is the pharmacokinetics for Letermovir?

A
  • Well absorption
  • Half-life 12h
  • IV has hydroxypropyl betadex
  • NO dosage adjustment for CrCl > 10; if CrCl < 50 monitor
29
Q

What are some of the indications for Leteomvir?

A
  • Prophylaxis of CMV; 480 mg IV or PO daily [1/2 this with cyclosporine]
30
Q

What are some of the adverse effects for Leteomvir?

A
  • Nausea, Vomiting, Diarrhea, cough, edema, fatigue, Ab pain
31
Q

What are som eof the Drug Interactions for Leteromvir?

A
  • Its a 3A4 Inhibitor
  • Contraindicated with Pita/Simvastatin when taken with Cyclosporine
  • DO NOT use with Riampin
32
Q

What is the MEchansim of action for Foscarnet?

A
  • Directly inhibits viral DNA Polymerase
  • Does NOT require phosphorylation by Thymidine kinase or other kinases

NOT a PRODRUG

33
Q

What is the spectrum of activity for Foscarnet?

A
  • HSV-1 & HSV-2 [even ACV resistant strains]
  • VZV [even ACV resistant strains]
  • CMV [even GAN resistant strains]
34
Q

What is the pharmacokinetics ofr Foscarnet?

A
  • ONLY IV
  • Bone sequesters 10-20% of a dose [kicking out Phos or Ca]
  • > 80% unchanged renally - Adjust dose
35
Q

What are some of the clinicla indications for Forcasnet?

A
  • CMV Retinitis
  • HSV & VZV resistant
36
Q

What are some of the sdbverse effects for Foscarnet?

A
  • Nephrotoxicity - dose limiting [WILL need to to rehydrate]
  • Metabolic
  • Nausea, Vomiting, Headache, Tremor, Seizures…

Very Toxic = why its a last line

37
Q

What is the Mechanism of action for Amantadine & Rimantadine?

A
  • Inhibits ion channels of the M2 protein = inhibition of uncoating of viral RNA within the host cell
37
Q

What is the Spectrum of Activity for Amantadine & Rimantadine?

A
  • Flu A
  • NOT recommended for treatment OR prophylaxis of Flu A because of the high resistance
38
Q

What is the pharmacokinetics for Amantadine & Rimantadine?

A
  • Well Absorbed
  • Aman: Half life 12-18h; Unchanged in the Urine [Adjust dose in renal issues]
  • Riman: Half life 24-26h; Reduce dose by 50%
39
Q

What are some of the clincial indicaitons for Amantadine & Rimantadine?

A
  • Flu A
40
Q

What are the adverse effects for Amantadine & Rimantadine?

A
  • CNS - more common with Aman
  • GI
41
Q

What are the Neuraminidase Inhibitors that are used?

A
  • Zanamivir, Oseltamivir, Peramivir
42
Q

What is the Mechanism of Action for the Neuraminidase Inhibitors?

A
  • prevents the virus from leaving the cell = decreased spread
  • Neuraminidase helps viruses break through the cell wall and increase replication = increase spread
43
Q

What is the spectrum of activity for the Neuraminidase Inhibitors?>

A
  • Flu A & B
44
Q

What are the Pharmacokinetics for Oseltamivir?

A
  • Rapidly absorbed
  • Half Life 22h when CrCl < 30 = Dose adjust
  • NO DOSE ADJUST for morbid obese people
45
Q

What are the Pharmacokinetics for Zanamivir?

A
  • Inhaled
  • Half Life 2.8h
  • NO real drug interactions
46
Q

What are the clinical indications for Zanamivir?

A
  • Treatment of Flu > 7yo
  • Prophylaxis of Flu > 5yo
  • DO NOT give live vaccine until 48h after stopping Zanamivir
  • DO NOT give Zanamivir until 2w after live vaccine
  • DO NOT GIVE in asthma or COPD

** Symptomatic< 2days**

47
Q

What are the Clinical indications for Oseltamivir?

A
  • Treatment of Flu > 2w old
  • Prophylaxis of Flu > 1yo
  • DO NOT give live vaccine within 2w before or 48h after starting Oseltamivir
  • CAN give inactive vaccine tho

PHRM 865: Theraputics V (42 decks)

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