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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
What are the adverse effects of Valganciclovir?
- **Bone Marrow Suppression** [reversible] - Neutropenia is ~40%; can treat that with G-CSF - **Hemtologic Toxicity**
26
What is the mechanism of action for Letermovir?
- Inhibits the **pUL56** subunit of the viral terminase complex of CMV - **Inhibition of CMV replication and prevention of CMV infections**
27
What is the spectrum og activity for Letermovir>
- CMV
28
What is the pharmacokinetics for Letermovir?
- Well absorption - Half-life 12h - **IV has hydroxypropyl betadex** - **NO dosage adjustment for CrCl > 10; if CrCl < 50 monitor**
29
What are some of the indications for Leteomvir?
- Prophylaxis of CMV; 480 mg IV or PO daily [1/2 this with cyclosporine]
30
What are some of the adverse effects for Leteomvir?
- Nausea, Vomiting, Diarrhea, cough, edema, fatigue, Ab pain
31
What are som eof the Drug Interactions for Leteromvir?
- Its a **3A4 Inhibitor** - Contraindicated with Pita/Simvastatin when taken with Cyclosporine - DO NOT use with Riampin
32
What is the MEchansim of action for Foscarnet?
- **Directly** inhibits viral DNA Polymerase - **Does NOT require phosphorylation by Thymidine kinase or other kinases** ## Footnote **NOT a PRODRUG**
33
What is the spectrum of activity for Foscarnet?
- HSV-1 & HSV-2 [even ACV resistant strains] - VZV [even ACV resistant strains] - CMV [even GAN resistant strains]
34
What is the pharmacokinetics ofr Foscarnet?
- ONLY **IV** - **Bone sequesters 10-20% of a dose** [kicking out Phos or Ca] - > 80% unchanged renally - **Adjust dose**
35
What are some of the clinicla indications for Forcasnet?
- CMV Retinitis - HSV & VZV resistant
36
What are some of the sdbverse effects for Foscarnet?
- **Nephrotoxicity - dose limiting** [WILL need to to rehydrate] - **Metabolic** - Nausea, Vomiting, Headache, Tremor, Seizures... ## Footnote **Very Toxic = why its a last line**
37
What is the Mechanism of action for Amantadine & Rimantadine?
- Inhibits ion channels of the M2 protein = inhibition of uncoating of viral RNA within the host cell
37
What is the Spectrum of Activity for Amantadine & Rimantadine?
- Flu A - **NOT recommended for treatment OR prophylaxis of Flu A** because of the high resistance
38
What is the pharmacokinetics for Amantadine & Rimantadine?
- 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
What are some of the clincial indicaitons for Amantadine & Rimantadine?
- Flu A
40
What are the adverse effects for Amantadine & Rimantadine?
- CNS - more common with Aman - GI
41
What are the Neuraminidase Inhibitors that are used?
- Zanamivir, Oseltamivir, Peramivir
42
What is the Mechanism of Action for the Neuraminidase Inhibitors?
- **prevents the virus from leaving the cell = decreased spread** - Neuraminidase helps viruses break through the cell wall and increase replication = increase spread
43
What is the spectrum of activity for the Neuraminidase Inhibitors?>
- Flu A & B
44
What are the Pharmacokinetics for Oseltamivir?
- Rapidly absorbed - Half Life 22h when CrCl < 30 = **Dose adjust** - **NO DOSE ADJUST for morbid obese people**
45
What are the Pharmacokinetics for Zanamivir?
- Inhaled - Half Life 2.8h - NO real drug interactions
46
What are the clinical indications for Zanamivir?
- **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 ## Footnote ** Symptomatic< 2days**
47
What are the Clinical indications for Oseltamivir?
- **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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