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Antimicrobial Drugs > Antivirals > Flashcards

Antivirals Flashcards

1
Q

Ganciclovir

A

Similar to acyclovir except monophosphate is put on by CMV protein kinase and host enzymes make it a triphosphate and inhibits DNA synthesis and elongation
Uses: CMV retinitis, CMV prophylaxis for transplant recipients
Side effect: bone marrow suppression

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2
Q

Enfuvirtide

A

Use: For HIV-1 and HIV treatment-experienced patients who have failed multiple regimens
MOA: binds to gp41 subunit of HIV glycoprotein and blocks conformational changes required for membrane fusion to CD4+ cells
Side effects: local injection site reactions, diarrea, nausea, fatigue, later option when other regimens have failed

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3
Q

Non-nucleoside reverse transcriptase inhibitors

A

Efavirenz
bind at different site distinct from enzyme catalytic site
All are active as given

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4
Q

Maraviroc

A

chemokine CCR5 antagonist (on human cells to prevent interaction with HIV gp120)–> blocks entry into HIV cells
Use: treatment of CCR5-tropic HIV-1
effective for strains resistant to other drugs (CCR-5 tropic strains tend to predominate early in infection)
Side effects: hepatotoxicity, CV events

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5
Q

Oseltamivir

A

Influenza A and B treatment/ prophylaxis (greatest benefit if given in first 48 hours of symptoms)
Mechanism: prodrug given orally and activated in liver and compettively inhiits influenza neuraminidases (interfere with viral release and penetration)
side effects: nausea, vomiting, diarrhea, bronchitis

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6
Q

Hepatitis B

A

Lamivudine
Tenofovir
Interferon alpha

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7
Q

Tenofivir

A

MoA: monophosphate prodrug phosphorylated by cell enzymes to triphosphate form and compet inhibitor of reverse transcriptase domain of hep B polymerase so cause DNA chain termination
Use: Hep B
Side effects: GI upset

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8
Q

Cytomegalovirs Prophylaxis/Infection

A

Ganciclovir

Foscarnet

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9
Q

HIV therapeutic failure

A

failure to maintain adherence

resistant strains

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10
Q

Ribavirin

A

Interfere with viral mRNA synthesis by :
Mono-P form inhibits inosine 5’-P dehydrogenase and thus GMP and GTP synthesis
Tri-P form inhibits GTP dependent capping of viral mRNA (so gets degraded)
Uses: aerosol use for young children with severe RSV infections and oral capsules for hepatitis C (combined with PEG interferon alpha and other drugs)
Side effects: aerosol use precipitates and clog resp equipment and pulmonary function deterioration and rash
also anemia and bone marrow suppression with Oral and IV use

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11
Q

Inhibition of Nucleic Acid Synthesis

A

Trifluridine
Acyclovir
Famciclovir
Penciclovir

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12
Q

Protease Inhibitors

A

Lopinavir
Ritonavir
Use: in combination with inhibitors of RT (HIV 1 and HIV 2)
and significantly decrease viral blood load
MOA: prevent viral aspartic protease from cleaving Gag-pol polypeptide into separate functional proteins
competitive inhibitor
results in non-infectious viral particles
Toxicity: diabetes, alterations in lipid metabolism (increased triglycerides and cholesterol), fat redistribution, alters metabolism of many other drugs (potent CYP3A inhibitors)

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13
Q

Acyclovir

A

Guanosine analog without cycle of ribose
activated only in virus infected cells and phosphorylates the acyclovir 40-100X faster in infected cells
Inhibits herpes DNA polymerase 10-30X more effectively than host cell DNA polymerase
Competes with doxy-GTP for DNA polymerase (chain termination)
Side Effects: generally well tolerated, rash, itching, nausea, vomiting, headache, fatigue

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14
Q

Abacavir

A

NRTI
Nucleoside Analog
Triphosphorylated form inhibits RT and cause DNA chain termination
Adverse effects: hypersensitivity (associated with HLA-B*57-1 allele) and if develops then stop drug immediately

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15
Q

Amantadine

A

Influenza A prophylaxis
Therapy: reduces fever in 50% of patients and illness duration by 1-2 days
resistance is common
Best in crowded environments
MOA: blocks viral uncoating by interfering with influenza A M2 protein (ion channel)
Side Effects: CNS effects

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16
Q

Penciclovir

A

Similar to acyclovir
Use: recurrent herpes of lips and face
topical administration

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17
Q

Lamivudine (3TC)

A

Nucleoside analog inhibitor of RT and in triphosphate form competitively inhibits RT and cause DNA chain termination (AZT resistance strains are 3TC sensitive and 3TC resistant strains are AZT sensitive)
Use: synergisitic with AZT against HIV
Side effects: nausea, diarrhea, rash

18
Q

Hepatitis C

A 
Ribavirin
Interferon alpha
Simeprevir
Sofosbuvir
Ledipasvir

Treat: interferon alpha +ribavirin for Hep C treatment

19
Q

HCV drug combinations

A

2 or more drugs with different mechanisms
avoid Interferon alpha when possible

Genotype appropriate therapy
Side Effects Tolerance

20
Q

Lamivudine

A

MOA: nucleoside analog (no phosphates) and phosphorylated by cell enzymes to triphosphate form and competitively inhibits reverse transcriptase domain of hep B polymerase (CAUSE DNA CHAIN TERMINATION)
Use: hepatitis B
Side effects: nausea, diarrhea

21
Q

Famciclovir

A

Prodrug activation to penciclovir-triP (active) which is very similar to acyclovir and inhibits viral DNA polymerase
Uses: acute herpes zoster (shingles which is latent chickenpox virus) localized and

22
Q

Foscarnet

A

Inhibits CMV DNA polymerase by biding to pyrophosphate binding site
Does not require conversion to triphosphate form to be active
Uses: CMV retinitis, acyclovir resistant herpes virus (thymidine kinase mutations)
Side Effects: renal damage, electrolyte imbalance, seizures

23
Q

Emtricitabine (FTC)

A

NRTI
Analog of lamivudine
Same mechanism and resistance as 3TC

24
Q

Zidovudine

A

NRTI
Thymidine nucleoside analog phosphorylated by cell enzymes to AZT-triphosphate which competitively inhibits RT and acts as a chain terminator
Side Effects: bone marrow suppression (neutropenia and anemia), avoid drugs which inhibit glucoronyltransferases, myopathy

25
Q

Raltegravir

A

Inhibitor of HIV integrase
Use: HIV-1 treatment and works on virus resistant to other drugs
Mechanism: HIV-1 integrase activity inhibited so HIV-1 DNA can’t integrate into chromosomes
Side effects: potential for severe/fatal skin and hypersensitivity reactions

26
Q

Strategies to inhibit viral adsorption and penetration

A

Immunization
Amantadine
Oseltamivir

27
Q

Fusion Inhibitors

A

Enfuvirtide

28
Q

Efavirenz

A

NNRTI- binds at different site than NRTI and disrupt RT
Multi-drug therapy for HIV
Side effects: rash, CNS/psychiatric symptoms, nightmares, vivid dreams

29
Q

Tenofovir

A

NRTI
unlike AZT: adenosine monophosphate prodrug hydrolyzed to tenofovir phosphonate
similariity to AZT: triphosphate form inhibits RT by competing for incorportate into DNA, causing chain temrination
Uses: combination therapy for HIV
side effects: overall, well tolerated

30
Q

Trifluridine

A

Thymidine analog
Interferes with DNA synthesis
Use: Opthalmic use and treatment of herpes simplex type 1 and 2

31
Q

Integrase Inhibitors

A

Raltegravir

32
Q

Interferon alpha

A

Approved use: condyloma acuminata (venereal warts), hepatitis B and C and given with other drugs (pegylation decreases clearance) with better kinetics and less frequent dosing
Side effects: flu-like syndrome, leukopenia, bone marrow suppression, neurotoxicity, myalgia

33
Q

Lopinavir

A

Protease Inhibitor

Protease inhibitor

34
Q

Immunization

A

active- vaccination

passive- injection of immune globulin (antibodies)

35
Q

Simeprevir

A

Better pharmacokinetics and side effects (new generation)
Reversible inhibitor of hepatitis C NS3/NS4A protease (cleavage of polyprotein to make individual proteins) so no cleavage of polyprotein and infectious virus not made
Use: hepatitis C genotype 1 and in combination with other drugs
Side effects: rash, nausea, itching, CYP3A interactions

36
Q

Nucleoside analtog reverse transcriptase inhibitors (NRTI)

A 
Zidovudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine 
Side effects: lactic acidosis, hepatic steatosis
37
Q

Ledpasvir

A

Inhibits NS5A phosphoprotein

Use: Given with sofosbuvir for HCV genotypes (1,4,5,6)

38
Q

Three forms of Acyclovir

A

Intravenous–> systemic HSV (disseminated neonatal, encephalities) and severe genital herpes
Oral–> primary genital herpes and primary herpetic gingivostomatis
Topical–> primary genital herpes

39
Q

CCR5 Antagonists

A

Maraviroc

40
Q

Sofosbuvir

A

Nucleoside (uridine) analog prodrug
Triphosphate form inhibits HCV NS5B RNA polymerase and is incorporated into viral RNA to cause chain termination
Uses: all hep C genotypes, given with anti-HCV drugs
Side effects: substrate of P-glycoprotein so avoid potent inducers of this

41
Q

Ritonavir

A

Protease Inhibitor Booster
Used to boost levels of other protease inhibitors (blocks metabolism by CYP3A by inhibiting it)
avoid other drugs metabolized by CYP3A

Antimicrobial Drugs (5 decks)

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