2 - Topical and Intralesional Antiviral Agents Flashcards
Topical and intralesional agents can be:
(1) viricidal
(2) immune-enhancing
(3) cytodestructive
True
The topical viricidal agents include:
(1) acyclovir
(2) penciclovir
(3) cidofovir
(4) foscarnet
(5) idoxuridine
True
The topical/intralesional immune enhancers include:
(1) topical imiquimod
(2) topical and intralesional interferon
True
The topical/intralesional cytodestructive agents include:
(1) intralesional bleomycin
(2) topical podophyllin/podofilox
(3) topical trichloroacetic acid
(4) topical cantharidin
(5) topical salicylic acid
(6) topical 5-fluorouracil
True
Topical acyclovir 5% cream and ointment are FDA approved for the treatment of HSV
True
Even when acyclovir is applied topically to damaged skin including localised VZV infection, systemic absorption is limited
True
Topical acyclovir is specific for HSV-infected cells because the drug requires phosphorylation by the viral enzyme thymidine kinase
True
Topical acyclovir is most effective against HSV-1 and HSV-2 and less effective against VZV due to less efficient phosphorylation by the VZV viral thymidine kinase
True
Topical acyclovir is not effective against CMV because CMV does not encode for thymidine kinase
True (acyclovir needs to be phosphorylated by viral thymidine kinase to be able to be incorporated into viral DNA by viral-DNA polymerase)
Topical acyclovir 5% ointment is approved of the management of initial genital HSV in immunocompetent patients
True (early application within 24 hours of onset of prodrome is important)
Initial = every 3 hours up to 6 X daily for 7 days
Recurrent = 5 X daily for 4 days
A finger cot or rubber glove should be used when applying the medication to prevent autoinoculation or transmission to other persons
Topical acyclovir 5% ointment/cream is approved of the management of limited non-life threatening mucocutaneous genital HSV and HSV labialis in immunocompetent patients
True (early application within 24 hours of onset of prodrome is important)
Topical acyclovir may cause application site reactions including mild pain and burning, although placebo patients experienced similar adverse effects
True
Both topical acyclovir and penciclovir are classified as pregnancy category B
True
Topical cidofovir and foscarnet are classified as pregnancy category C
True (listed for the injectable version of the drug)
Topical acyclovir has limited use as monotherapy for genital HSV and HSV labialis and when medically tolerable, oral acyclovir is preferred over topical acyclovir for recurrent genital herpes given the greater efficacy in reducing the duration of viral shedding and time to crusting and healing of lesions
True
Penciclovir is only available in topical preparation because of poor oral availability
True (Famciclovir, the prodrug of penciclovir is available in oral form)
Penciclovir is selectively phosphorylated to the monophosphate from by viral thymidine kinase, and then further phosphorylated by human cellular kinases to the active triphosphate for, which inhibits viral replication by competitively binding to viral DNA polymerase
True
Even though acyclovir and penciclovir are qualitatively similar (with similar mode of action), penciclovir exhibits more efficient phosphorylation, a higher affinity to viral DNA polymerase, and increased stability of its active triphosphate form; thus leading to longer duration of activity
True
Penciclovir exhibits inhibitory activity against HSV-1, HSV-2, VZV and EBV
True (limited activity against CMV)
Penciclovir exhibits limited in vitro inhibitory activity against CMV
True
Penciclovir 1% cream is indicated for the treatment of recurrent HSV labialis in immunocompetent individuals 12 years and older
True (Penciclovir 1% cream should be applied at the earliest sign/symptom to all lesions every 2 hours/at least 6X daily for 4 days)
Penciclovir 1% cream reduced pain and viral shedding associated with HSV labialis independent of the timing of medication initiation
True
The most frequently reported adverse effect with topical Penciclovir is headache
True
Given the inconvenience or frequent application of topical Penciclovir (every 2 hours, or at least 6X daily), the expense and the reduction of symptoms of viral shedding by half a day; the clinical benefit of penciclovir over oral antiviral therapy is limited
True
If oral therapy is contraindicated or not available, topical Penciclovir is an alternative option to topical acyclovir for HSV labialis
True (although no head to head studies performed between these 2)
Cidofovir is an acyclic nucleotide that exhibits antiviral activity against a broad range of DNA viruses including HPV, human herpes viruses, and some pox viruses
True
IV Cidofovir is used to treat CMV retinitis in AIDS patients
True
No oral preparations of cidofovir are available, however cidofovir has been compounded in topical formulations for verruca vulgaris (HPV)
True (reported anecdotally or in small studies including children with recalcitrant disease)
Unlike acyclovir and penciclovir, cidofovir does not depend on thymidine kinase for its phosphorylation
True
Cidofovir acts as a competitive inhibitor for incorporation into viral DNA by viral DNA polymerase and blocks viral DNA synthesis
True
No oral preparations of cidofovir are available, however cidofovir has been compounded in topical formulations for condyloma acuminata/genital warts (HPV)
True (reported anecdotally or in small studies in immunocompetent patients)
No oral preparations of cidofovir are available, however cidofovir has been compounded in topical formulations for herpes simplex (HSV)
True (reported anecdotally or in small studies in AIDS patients with acyclovir-resistant HSV as well as immunocompetent patients)
No oral preparations of cidofovir are available, however cidofovir has been compounded in topical formulations for orf (parapox virus)
True (reported anecdotally or in small studies)
No oral preparations of cidofovir are available, however cidofovir has been compounded in topical formulations for molluscum contagiosum (pox virus)
True (reported anecdotally or in small studies in children and adults with HIV with recalcitrant disease)
Topical cidofovir may cause headaches, nausea, and pharyngitis, though with similar frequency to placebo
True
Application site pruritus, rash, pain, paraesthesia and ulceration are increased with higher concentrations of topical cidofovir
True
Foscarnet is a pyrophosphate (not a nucleoside) analog with activity against all herpes viruses
True
Foscarnet is used in the treatment of CMV infection in immunocompromised patients
True
Foscarnet is the oral drug of choice for acyclovir-resistant HSV
True (does not require activation by either cellular or viral enzymes)
Foscarnet does not require activation by either cellular or viral enzymes
True (drug of choice for acyclovir-resistant HSV)
NB. Acyclovir relies on viral thymidine kinase for phosphorylation and subsequent inhibition of viral replication
Foscarnet is not a nucleoside analog, and so nucleoside-resistant viral DNA polymerase are susceptible/sensitive to Foscarnet
True (foscarnet is a pyrophosphate analog instead)
NB. Acyclovir and Penciclovir are nucleoside analogs (Valacyclovir is the prodrug or acyclovir and Famciclovir is the prodrug of Penciclovir)
Idoxuridine is a thymidine analog which has limited efficacy in genital HSV, HSV labialis, and VZV infections
True (only available as an ophthalmic solution for the treatment of herpes keratitis)
Idoxuridine is only available as an ophthalmic solution for the treatment of herpes keratitis
True (has limited efficacy in genital HSV, HSV labialis, and VZV infections)
Imiquimod is a topical immunomodulating agent approved by the FDA for treatment of external genital and perianal warts/condylomata acuminata (HPV) for patients 12 years and older
True
5% cream once daily 3 X weekly application for up to 16 weeks
3.75% cream daily for 8 weeks
5% topical Imiquimod is a topical immunomodulating agent approved by the FDA for treatment of superficial small <2cm non-facial superficial BCC if surgery is inappropriate and patient follow up can be assured
True
5% cream once daily 5 days/week for 6-12 weeks