Anti-viral drugs Flashcards
DNA viruses
- HSV, HBV
- genome replication takes place in the cell nucleus
- they are dependent on the host cell’s DNA and RNA synthesizing machinery
RNA viruses
- HCV, influenza virus
- replication usually takes place in the cytoplasm
- use their own enzymes to replicate RNA and create copies of their genomes
RNA retroviruses
- HIV
- integrate the DNA copy of viral RNA produced by reverse transcriptase into the host genome as a provirus
Which type of therapy has a greater clinical effectiveness?
Combination therapy
Viral replication
-steps
- Attachment of the virus to the receptors on the host cell surface
- Entry of the virus through the host cell membrane
- Uncoating of viral nucleic acid
- Synthesis of early regulatory proteins
- Synthesis of new viral RNA or DNA
- Integration into the nuclear genome
- Synthesis of late, structural proteins
- Assembly (maturation) of viral particles)
- Release from the cell
Drugs for herpes
- names
- mechanism of action
Acyclovir
Ganciclovir
Valaciclovir
-inhibits the synthesis of new viral DNA
Acyclovir
- mechanism of action
- pharmacokinetics
- indications
-acts as a competitive substrate for DNA polymerase (inhibits synthesis) and chain termination after its incorporation into viral DNA
- topica, oral, i/v, renal excretion
- herpes simplex virus and varicella zoster virus
- mucocutaneous and genital herpes lesions
- prophylaxis in AIDS and in other immunocompromised patients
- i/v: severe herpes disease
Acyclovir
- effect on which phase of viral replication?
- unwanted effects
- in comparison to Valacyclovir?
- Synthesis of new viral DNA
- nephrotoxicity
- Valacyclovir has a longer duration of action
Gancyclovir
- mechanism of action
- pharmacokinetics
- indications
-same as Acyclovir
- i/v, penetrates well into tissues, renal elimination, oral bio-availability less than 10%
- cytomegalovirus (HSV-5), HSV
-prophylaxis and treatment of cytomegalovirus infections in immunocompromised patients
Gancyclovir
- unwanted effects
- in comparison to Valganciclovir?
- bone marrow depression (neutropenia)
- high oral bio-availability and decrease use of i/v gancilovir in CMV
Drugs for influenza
-names
Amantadine
Rimantadine
Oseltamivir
Zanamivir
Amantadine and Rimantadine
- mechanism of action
- indications
- inhibit an early step in replication of the influenza A (but not influenza B) virus
- prevent uncoating by binding to proton channel
- used for prophylaxis, they have no effect if you are already sick
- can reduce the duration of symptoms if given within 48h after contact
Amantadine and Rimantadine
- effect on which phase of viral replication?
- unwanted effects
- Uncoating of viral nucleic acid
- GI irritation, dizziness, ataxia, slurred speech
Oseltamivir and Zanamivir
- mechanism of action
- pharmacokinetics
- indications
-inhibitors of neuraminidases produced by influenza A and B –> inhibit viral release from the cell
- Oseltamivir: oral, Zanamivir: inhalation
- should be used only if you already have symptoms
- decrease the time to alleviation of influenza symptoms; are more effective if used within 24h after onset of symptoms
- prophylatically decrease incident of influenza
Oseltamivir and Zanamivir
- effect on which phase of viral replication?
- unwanted effects
- release from the cell
- GI symptoms (Oseltamivir)m bronchospasms in asthmatic patients (zanamivir)