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Dental Therapeutics Exam 2 > Antivirals > Flashcards

Antivirals Flashcards

1
Q

Oral Viral Infections

A

Coxsackie-Type Viruses (Picorna RNA virus) - Herpangina, Acute Lymphonodular Pharyngitis, Hands Foot and Mouth disease; Herpes type viruses (DNA virus), Human papilloma virus (DNA virus)

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2
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTI) - Agents to Treat AIDS

A

Zidovudine (Azidothymine, AZT) (Retrovir), Didanosine (Videx), Zalcitabine (Hivid), Stavudine (Zerit), Lamivudine (Epivir), Abacavir (Zaigen)

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3
Q

DNA (dsDNA) Viruses

A

Poxvirus (smallpox), Herpes (chickenpox, herpes, shingles, CMV), Adeno (sore throat, conjunctivitis, Papilloma (warts), Hep B (dsDNA reverse transcriptase)

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4
Q

RNA Viruses

A

Orthomyxo - ssRNA (inluenza), Avian flu, Swine flu; Filo -ssRNA ebola, marburg; Retro +ssRNA (AIDS, Measles, Mumps), Flavi - +ssRNA (Arthropod host): West Nile, Zika, Dengue (DENV), Chikungunya, Yellow fever etc; Hep C +ssRNA; Picorna +ssRNA polio, echovirus, coxsackie

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5
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTI) and Adverse Effects

A

Agents Used to Treat AIDS Zidovudine (Azidothymine, AZT) (Retrovir) - Anemia, N. anorexia, Hepatotoxicity, Lactic acidosis, Myopathy, Peripheral neuropathy; Didanosine (Videx) - Diarrhea, Pancreatitis and Peripheral neuropathy; Zalcitabine (Hivid) - Peripheral neuropathy, Stomatitis, Pancreatitis, Rash; Stavudine (Zerit) - Lactic acidosis and peripheral neuropathy; Lamivudine (Epivir) - Headache and nausea, Pancreatitis rare; Abacavir (Zaigen) - Hypersensitivity rxn, GI, Neuro complaints;
Phosphorylated AZT accumulates in most dividing cells in body bc its activation is non-selective, Cause bone marrow suppression - Manifest as anemia and neutropenia also myopathy, Adverse effects due to inhibition of cellular polymerases by AZT triphosphate and by inhibition of cellular thymidylate kinase by AZT monophosphate

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6
Q

Zidovudine

A

Azidothymine, AZT - Retrovir
Agent used to treat AIDS - NRTI
Nucleoside analog w/alt sugar moiety similar acyclovir, Contains no 3’hydroxyl so like acyclovir it is a chain terminator, Requires phosphorylation to activate

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7
Q

Zidovudine Mechanism of Action

A

Activated by phosphorylation by host cell thymidine kinase and then by other kinases to the triphosphate, Acts as substrate for reverse transcriptase and competes with thymidine triphosphate for incorporation into DNA, Since NRTIs lack a 3’hydroxyl group, incorporation into DNA terminates chain elongation

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8
Q

Zidovudine Indication

A

Asymptomatic and symptomatic HIV infections

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9
Q

Zidovudine Pharmacokinetics

A

Oral or IV, In combination with other HIV drugs, Well distributed including CNS; Zidovudine and Didanosine are rapidly metabolized and excreted in urine; Large proportion of others excreted unchanged

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10
Q

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)

A

Agents Used To Treat AIDS

Nevirapine (Viramune), Delavirdine (Rescriptor), Efavirenz (Sustiva)

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11
Q

NNRTI Mechanism of Action

A

Inhibit HIV reverse transcriptase directly by binding adjacent to enzyme active site and inducing conformational changes in site, Agents do not require phosphorylation for activity

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12
Q

NNRTI Indications

A

HIV infections, Used in combination with NRTI agents or protease inhibitors; Resistance develops rapidly if used alone or with only one other agent

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13
Q

NNRTI Pharmacokinetics

A

Oral, Metabolized in liver (CYP450), Efavirenz has long elimination half-life of 2d - So once a day admin

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14
Q

NNRTI Adverse Effects

A

Rash and various CNS disturbance particularly with efavirenz

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15
Q

HIV Protease Inhibitors

A 
Used to treat AIDS
Agents Saquinavir (Invirase), Ritonavir (Norvir), Indinavir (Crixivan), Nelfinavir (Viracept), Amprenavir (Agenerase)
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16
Q

HIV Protease Inhibitor Mechanism of Action

A

Inhibit HIV protease essential for final step of new virus formation, Active against viral strains resistant to HIV reverse transcriptase inhibitors

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17
Q

HIV Protease Inhibitor Indication

A

Used in combination with zidovudine and/other HIV reverse transcriptase 1 inhibitors to avoid resistance, Ritonavir used with saquinavir to increase retention of latter

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18
Q

HIV Protease Inhibitor Pharmacokinetics

A

Oral, Metabolized in liver

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19
Q

HIV Protease Inhibitor Adverse Effects

A

Many and frequent; Body fat redistribution (buffalo hump), N, V, D; Hyperglycemia, Hyperlipidemia 15%, Hypercholesterolemia, 50% Paresthesias with ritonavir, Kidney stones with Indinavir (Crystalluria), Fatigue, Peripheral neuropathy

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20
Q

Herpes Antivirals

A

Acyclovir (Zovirak), Valacyclovir (Valtrex), Penciclovir (Vectavir), Famciclovir (Prosurx), Ganciclovir (GanGuard)

21
Q

Herpes Antivirals Mechanism of Action

A

Converted to triphosphate w/ viral-specific thymidine kinase, Triphosphate selectivity inhibits virus DNA polymerase and thus inhibits viral DNA replication

22
Q

Herpes Antivirals Indications

A

Useful in treatment of genital herpes simplex, herpes simplex labials (cold sores), herpes zoster (shingles) and varicella zoster (chicken pox), Prophylaxis against herpes viruses in immunocompromised patients, Ganciclovir useful for CMV in immunocompromised patients

23
Q

Herpes Antivirals Pharmacokinetics

A

Orally, Topically or IV, Well distributed and Excreted largely unchanged

24
Q

Herpes Antivirals Adverse Effects

A

Nausea, Vomiting, Diarrhea, Headache and Hallucinations with high dose, Leukopenia and Thrombocytopenia with Ganciclovir, Headache and Arthralgia

25
Q

Herpes Antivirals Mechanism of Resistance

A

Mutation in viral thymidine kinase

26
Q

Herpes Antivirals Avoidance

A

Acyclovir with Amphotericin B, TMP-SMX (Bactrim), Aspirin NSAID, Probenecid, Zidovudine (AZT/Retrovir), Tacrolimus (Prograf)

27
Q

Valacyclovir

A

Herpes Antiviral
Acyclovir chemically bound to Valine moiety, Prodrug form of acyclovir w/greater oral bioavailability, Rapidly converted to Acyclovir after oral administration

28
Q

Valacyclovir Drug Interactions

A

Better bioavailability than acyclovir, Taken less frequent, Some metabolism by alcohol and aldehyde dehydrogenase, Valacyclovir should not be prescribed with SSRI bc SSRI inhibit 2D6 enzyme needed to activate drug; Avoid using Valacyclovir w/ Cimetidine (Tagamet) or Probenecid (Benemid)

29
Q

Herpes Antivirals Prescription

A

Acyclovir Intermitten therapy for cold sores lasting less than one week - 200mg, #25, Take one capsule five times a day for a full 5 days; Acyclovir buccal 50mg, 1, Apply buccal tablet to upper gum until sticks and let dissolve

30
Q

Foscarnet Mechanism of Action

A

Foscavir; Herpes Antivirals; Selectively inhibits viral DNA-polymerase, RNA polymerase and HIV reverse transcriptase at pyrophosphate binding site without affecting human DNA polymerases, Inhibit replication of all known herpes viruses

31
Q

Foscarnet Indication

A

CMV retinitis and acyclovir-resistant mucocutaneous HSV infections in patients with AIDS

32
Q

Foscarnet Pharmacokinetics

A

IV, limited entry into CNS, may accumulate in bone, largely excreted unchanged in urine, Triphasic elimination, Longest t1/2 50hr

33
Q

Foscarnet Adverse Effects

A

Renal impairment, Headache and Seizures

34
Q

Trifluridine

A

Viroptic; Ophthalmic; Herpes Antivirals

Inhibit DNA synthesis by incorporation into viral DNA, Used to treat herpes simplex keratitis topically

35
Q

Fomivirisen

A

Oligonucleotide that binds to mRNA (antisense) to inhibit human CMV protein synthesis, Indicated in CMV retinitis in patients with AIDS, Occular inflammation is most common adverse effect

36
Q

Agents Used to Treat Viral Respiratory Infections (Influenza)

A

Amantadine

Rimantadine (Less toxic)

37
Q

Viral Respiratory Infection Mechanism of Action
Amantadine
Rimantadine (Less toxic)

A

Inhibitor of viral uncoating, Blocks M2 proton channel in viral envelope, inhibiting acidification of virion interior, dissociation of matrix protein and uncoating, Also cause release of dopamine and NE and blocks NMDA receptor

38
Q

Viral Respiratory Infection Pharmacokinetics
Amantadine
Rimantadine (Less toxic)

A

Readily absorbed from GI tract, well distributed and excreted in urine

39
Q

Viral Respiratory Infection Adverse Effects
Amantadine
Rimantadine (Less toxic)

A

Occasional mild CNS disturbances (Nervousness, Anxiety, Agitation, Insomnia, Difficulty concentrating, Lightheadedness), Exacerbations of pre-existing seizure disorders psychiatric symptoms in PD or schizophrenia

40
Q

Viral Respiratory Infection Indication
Amantadine
Rimantadine (Less toxic)

A

Prophylaxis against and possible treatment of Influenza A infection (Not Influenza B), Reduces length and severity of Influenza A infections; Amantadine used to treat Levodopa-induced dyskinesias that develop late in course of disease. Does this by blocking excitatory NMDA receptors, Due to widespread resistance, use is supplanted by Oseltamivir (Tamiflu) and Zanamivir (Relenza)

41
Q

Agents Used to Treat Viral Respiratory Infections

A

Zanamivir (Relenza) - Powder, Oseltamivir (Tamiflu) - Oral

42
Q

Viral Respiratory Infections Mechanism of Action

Zanamivir (Relenza) - Powder, Oseltamivir (Tamiflu) - Oral

A

Neuraminidase inhibitor, Decrease release of virus from infected cells by inhibiting breakage of bond between virus particles and host cells

43
Q

Viral Respiratory Infections Indications

Zanamivir (Relenza) - Powder, Oseltamivir (Tamiflu) - Oral

A

Influenza A & B to decrease intensity and duration of disease, Also complications; Used as aerosol for respiratory syncytial virus (RSV) infection in children, Oral form for hepatitis

44
Q

Viral Respiratory Infections Pharmacokinetics

Zanamivir (Relenza) - Powder, Oseltamivir (Tamiflu) - Oral

A

Some absorption into blood when used as an aerosol, Readily absorbed from GI tract, Excreted mainly as deribosylated metabolic product in urine;
Zanamivir - Poor bioavailability and administered by inhalation, Less than 20% absorbed systemically, Mostly excreted in urine;
Oseltamivir - Well absorbed orally and excreted largely unchanged in urine

45
Q

Viral Respiratory Infections Adverse Effects

Zanamivir (Relenza) - Powder, Oseltamivir (Tamiflu) - Oral

A

Bronchospasm, Rash, Conjunctivitis, Headache, GI Upset; Uncommon - Oral/Nasal discomfort, Bronchospasm, Delirium, Hallucinations, Other behavior

46
Q

Agents to Treat Viral Respiratory Infections

A

Ribavirin (Virazole)

47
Q

Viral Respiratory Infections Mechanism of Action

Ribavirin

A

Phosphorylated intracellularly and inhibits viral replication of both RNA and DNA viruses partly by interfering with guanosine triphosphate (GTP)_ formation and subsequent viral mRNA capping, hence viral protein synthesis; Though to increase mutagenesis - Hep C

48
Q

Treatment for Viral Hepatitis

A

Interferon (HBV, HCV), Lamivudine (HBV), Tenofovir (HBV), Ribavirin (HCV), Stat-C (HCV) - HCV Protease inhibitors, HCV RNA Poly inhibitors, Combinations for Hep C

Dental Therapeutics Exam 2 (8 decks)

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