Pharmacology

Anti-Virals (College Sec)

1 week of 4th Shift

Understanding Viruses:
• Viral replication:
- A virus cannot replicate on its own
- It must attach to and enter a host cell
- It then uses the host’s cell energy to MOA
synthesize protein, DNA and RNA (genetic Acyclovir Acyclovir monoPO4
parasites) Cellular enzymes
- Spread is fast
• Viruses are difficult to kill because they live inside Acyclovir triPO4
our cells Acyclovir triPO4
• Any drug that kills a virus may also kill ourselves - Competes with DGTP thereby inhibiting DNA
synthesis and consequently viral replication
Viral Infections
Competent immune system Side Effects
• Best response to viral infection • Acyclovir: rash, nausea & vomiting, headache,
lethargy, dizziness, seizures, confusion, agitation,
• A well functioning immune system will eliminate
impaired renal function
or effectively destroy virus replication
• Ganciclovir: bone marrow toxicity, fever, nausea,
• Immunocompromised patients have frequent viral
anorexia, vomiting
infections
- Cancer patients
Purine Nucleoside Analogs: Adenosine
- Transplant patients
Agent Antiviral Activity
- AIDS patients
Didanosine (ddI) HIV
Vidaribine (Ara-A) HSV, VZV, CMV, EBV
Viruses Affected by Current Antiviral Therapy
(prototype: zidavudine)
• Cytomegalovirus (CMV) retinitis
• Herpes Simplex Virus (HSV) MOA
o HSV 1: oral aphthous ulcers • Didanosine: Interferes with the HIV RNA-
o HSV 2: genital ulcers dependent DNA polymerase (reverse
• Varicella Zoster Virus (VZV) transcriptase), thus preventing replication of the
virus
- Chickenpox, shingles
• Vidaribine: inhibits DNA polymerase
• Human Immunodeficiency Virus (HIV)
• Influenza A Virus (Flu) Side Effects
• Respiratory Synctial Virus (RSV) • Didanosine: Pacreatitis (9%), peripheral
• Hepatitis B Virus (HBV) neuropathies (35%), seizures, retinal
depigmentation
Antivirals • Vidaribine: Burning, itching, lacrimation,
• Synthetic purine nucleoside analogs photophobia
• Two types of nucleosides
Pyrimidine Nucleoside Analogs: Cytosine
a. Purine – Guanine, Adenosine
Agent Antiviral Activity
b. Pyrimidine – Thymidine, Cytosine Lamovidine HIV, HBV
Zalcitabine HIV
Purine Nucleoside Analogs: Guanines (Prototype: zidovudine)
Agent Antiviral Activity
Acyclovir(prototype) HSV1, HSV2, VZV MOA (Lamovidine)
Ganciclovir CMV retinitis, systemic CMV
• Inhibition of HIV reverse transcriptase
infection
Ribavirin Influenza A & B, RSV
malta aiko (yin) + mrose (yang) 1 of 3
 Pharma – Antivirals Dr. Biag Page 2 of 3

• The monophosphate is incorporated into the viral - increased dopa release from presynaptic
DNA by HBV polymerase resulting in DNA chain fibers
termination
Side Effects
• Orthostatic hypotension
• Peripheral edema
• Insomnia
Side Effects • Anorexia
• Headache • Nausea
• Insomnia • Xerostomia
• Malaise 2. Foscarnet (Foscavir)
• Pain Indication: CMV (retinitis and systemic)
• Nausea & Vomiting
• Peripheral neuropathy MOA
• Inhibits the replication of all known herpes
Pyrimidine Nucleoside Analogs: Thymidine virus in vitro
Agent Antiviral Activity
Zidovidine (AZT) HIV Side Effects
• Headache (26%), seizures (10%), acute renal
MOA failure (27%), nausea (47%), diarrhea (35%),
• Converted to a triPO4 (the active form) by anemia (33%)
thymidine kinase and other cellular enzymes
• Incorporated into growing DNA chain by viral 3. Indinavir
reverse transcriptase, thereby terminating viral • Antiretroviral agent, protease inhibitor
replication • HIV-1

Side Effects Side Effects

• Bone marrow suppression • Nausea, dyslipedemia, mild discoloration of
• Nausea indirect bilirubin
• Anorexia
• Headache MOA
• Fever • Protease inhibitor
• Cough • HIV protease is required for cleaving viral
polyprotein precursors into individual final
• Rash
proteins found in infectious HIV. Inhibition
prevents cleavage of these polyproteins
Other Antivirals
resulting in the formation of immature non-
1. Amantadine (Symmetrel)
infectious viral particles
Indication: Influenza A
Other Uses:
4. Oseltamivir (Tamiflu)
- Idiopathic Parkinson’s Disease
- Postencephalitic Parkinsonism • Neuraminidase inhibitor
- Drug induced extrapyramidal reactions - Preventing the release of nearly formed
and symptomatic Parkinsonism associated virus form the surface of the infected cells
with _______ • Indication: Influenza A & B

MOA Side Effects:

• As antiviral • Fatigue
- blocks uncoating of Influenza A virus • Dizziness
preventing viral replication • Headache
• Antiparkinsonism activity: • Nausea & Vomiting
- blocks reuptake of dopa into presynaptic
neurons
 Pharma – Antivirals Dr. Biag Page 3 of 3

Just to let u know, 4 weeks na lang, end na ang school

year 2007-2008

Wala lang, just so you have something to look forward

to… (cause I am SURELY looking forward to see this
year end, *sigh)

Hapi bday ulit sa mga January celebrants 