Antiviral Drugs Flashcards
What are NRTIs
Nucleoside/nucleotide reverse transcriptase inhibitors
How do NRTIs work
Competitively inhibit neucleotides binding to reverse transcriptase and terminate the DNA chain
What’s the difference between nucleosides and nucleotides
Nucleosides need to be phosphorylated to get activated
What are NRTIs side effects
Can cause mitochondrial toxicity and lactic acidosis
Give examples of NRTIs and common ending
Mainly end with - dine
- lamivudine
- zidovudine
- stavudine
- didanosine
- abacavir
Lamivoudine adverse effects
Can cause peripheral neuropathy
What can lamivoudine treat other than HIV
It can also treat hepatitis B, alongside tenofovir (neucleotide)
When is zidovudine used and what are it’s adverse effects
Used during pregnancy and breast feeding to reduce vertical transmission. May cause myelosppression (anemia and granulocytopenia)
Stavudine side effect
Peripheral neuropathy
Didanosine side effect
May cause pancreatitis
Abacavir side effect
Hypersensitivity associated with HLA-B57:01 allele
Delayed rash
What are NNRTIs
non-nucleoside reverse-transcriptase inhibitor
NNRTIs mechanism of action
Bind to reverse transcriptase at different site than NRTIs, doesn’t requires phosphorylation to become active.
Example of NNRTI
Nevirapine
Nevirapine adverse effects
Can cause Rash, hepatoxicity and Steve Johnson syndrome (conjunctivitis and mucosal destination)
HIV protease inhibitors ending suffix and examples
Ends with -Navir
Ritonavir is the most important since it inhibits p450 which enhances other PIs
Which gene codes for HIV proteases
POL gene
HIV protease inhibitors adverse effects
Hyperglycemia, dyslipidemia, lipodystrophy (buffalo hump) and insulin resistance
Integrase inhibitor mechanism of action
Inhibits incorporation if HIV genome in to host cells DNA
Example of integrase inhibitor
Raltegravir
Give examples of fusion inhibitors
Enfuvirtide
Miraviroc
Enfuvirtide path inhibited and way of administration
Enfuvirtide is given IV - it binds to GP41 inhibiting entry
Miravoric path inhibited and way of administration
Miroviric is given orally - binds to CCR5 on Tcells inhibiting entry
What is HAART
Highly active antiretroviral therapy
Example of HAART
Two NRTIs and protease inhibitor or
Two NRRIs and NNRTI
How to prevent mother to child transmission
Test for HIV, C Section, No breast feeding and antiretroviral therapy
What is the antiretroviral therapy used for pregnant women
Two NRTIs backbone(Abacavir and Lamivudine) and ritonavir with any PI
OR
(Tenofovir and emtricitabine) and ritonavir with other PI
Prophylaxis against HIV
Zidovudine and Lamivudine and Indinavir
Drugs against hepatitis B
IFN-alpha, lamivudine (NRTI and DNA polymerase inhibitor)
Also tenofovir and entecavir and adefovir (nephrotoxicity)
Treatment of Hepatitis C
IFN-alpha (pegylated- longer T1/2)) and Ribavirin(interferes with viral mRNA)
Drugs for COVID 19
Remedesivir (prodrug, interferes with RNA-dependent RNA polymerase—> inhibiting viral RNA synthesis
Inhibitors of viral uncoating
Amantadine and rimantadine (active against only influenza A and for prophylaxis)
Neuroamidase inhibitors
Oseltamivir (Oral) and Zanamivir(inhaled or intranasal) (active against influenza A and B)
What are anti herpetic drugs
DNA polymerase inhibitors
How does resistance to acyclovir happen
Mutation in tymidine kinase
What does acyclovir treat
Given for HSV, VZV and EBV treatment of primary and recurrent herpes genitalis—> oral, herpes labialis—> topical(given 4-5x daily while valcyclovir (3x daily)
What is given for HSV infections in immunocompromised, VZV and encephalitis
I.V acyclovir
What is given when herpes is resistant to cyclovir
Foscarnet
What is given in CMV infections
Ganciclovir(can cause myelosuppression)
And Foscarnet
