Pharma

Antivirals and Antifungals Tabulated

1 week of 4th Shift

Antifungals

MYCOTIC INFECTIONS In the mouth:

Four General Types Oral candidiasis or thrush
Cutaneous New born infants & immunocompromised
Subcutaneous patients have increased frequency of oral
Can be superficial but may not be in the skin thrush
Superficial
Systemic* Vaginal Cadidiasis
“yeast infections”
*Can be life threatening Pregnancy, DM, OCP
*usually occur in immunocompromised May occur to both male and females (urethritis
and balanitis)
Candida Albicans
Antiviral Agents
Due to antibiotic therapy, antineoplastics, or Broken Down into 4 major grps based on their chem’l
immunosuppresants (steroids) structures
May result in overgrowth & systemic infections (1) Polyenes: amphoterincin B , nystatin
Opportunistic organism, may multiply in number (2) Flucytosine
because of the decline in the normal flora (3) Imidazoles: ketoconazole, miconazole,
clotrimazole, fluconazole
(4) Griseofulvin
Drug MOA Indication ADR
Polyenes: Fever
Amphotericin B & Malaise
Nystatin IV: fatal systemic mycotic Ms and jt pain
Binds to sterols in cell infections Chills
membrane lining Aspergillosis Nausea
Allowing K+ & Mg2+ to leak out, Blastomycosis Headache
altering fungal cell Coccidiomycosis, Hypertension
metabolism Paracoccidiodomycosi Anaphylaxis
Result: fungal cell death Histoplasmosis Anorexia
Sporotrichosis Tachycardia
Renal Toxicity
Neurotoxicity
Flucytosine Nausea, vomiting,
anorexia
Alone or in combination Confusion,
aka 5-fluorocytosine with amphotericin B for hallucination,
serious systemic headache, sedation
Taken up by fungal cells &
infections caused by
interferes with DNA synthesis Agranulocytosis (dec
susceptible strains of
Result: fungal cell death Cryptococcus & candida WBC)
species Elevated BUN &
creatinine
Elevated transaminases
Imidazoles

maro03267 + maltaaiko = 1 of 4
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Ketoconazole Rash (if topical),

Fluconazole anaphylaxis
N & V, liver cirrhosis
Gynecomastia, uterine
bleeding, loss of libido,
impotence,
oligospermia, hair loss
Interferes with synthesis of Acute
ergosterol hypoaldosteronism,
Increase in cell permeability & renal hypofunction
ultimately inhibition of fungal
Headache
cell growth
Nausea and vomiting
Abdominal pain
Diarrhea
Increase AST in Px w/
cryptococcal meningitis
& AIDS
Rash
Miconazole Vulvovaginal burning
when used as ointment,
inhibit uptake of components cream and vaginal
essential for cell reproduction suppository
& growth as well as cell wall Itching
structures, thus promoting cell Irritation
death of fungi Maceration
Allergic contact
dermatitis
Clotrimazole Abnormal liver function
Altering fungal cell membrane tests
permeability
Stinging, erythema,
Permeating loss of P cmpds, K edema
& other essential intracellular
Cystitis, urethritis
constituents w/ consequent
loss of ability to replicate Vaginal soreness during
intercourse
Griseofulvin Disrupts cell division Rash, urticaria
Result: inhibited fungal Headache
mitosis (reproduction) Nausea/Vomiting &
Deposits in keratin precursor anorexia
cells & has special affinity for Leukopenia
diseased tissue. It is tightly Nephrotoxicity
bound to new keratin of skin, Hepatotoxicity
hair, & nails, w/c becomes Overgrowth of
highly resistant to fungal nonsusceptible
invasion organisms (Candida)

Antivirals
Understanding Viruses:
• Viral replication: Viral Infections
- A virus cannot replicate on its own Competent immune system
- It must attach to and enter a host cell • Best response to viral infection
- It then uses the host’s cell energy to • A well functioning immune system will eliminate
synthesize protein, DNA and RNA (genetic or effectively destroy virus replication
parasites) • Immunocompromised patients have frequent viral
- Spread is fast infections
• Viruses are difficult to kill because they live inside - Cancer patients
our cells - Transplant patients
• Any drug that kills a virus may also kill ourselves - AIDS patients
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• Influenza A Virus (Flu)

Viruses Affected by Current Antiviral Therapy • Respiratory Synctial Virus (RSV)
• Cytomegalovirus (CMV) retinitis • Hepatitis B Virus (HBV)
• Herpes Simplex Virus (HSV)
o HSV 1: oral aphthous ulcers Antivirals
o HSV 2: genital ulcers • Synthetic purine nucleoside analogs
• Varicella Zoster Virus (VZV) • Two types of nucleosides
- Chickenpox, shingles a. Purine – Guanine, Adenosine
• Human Immunodeficiency Virus (HIV) b. Pyrimidine – Thymidine, Cytosine

Drug MOA Antiviral Activity ADR

Purine Nucleoside Analogs: Guanines
Acyclovir (Prototype) Acyclovir Acyclovir
monoPO4 rash, nausea & vomiting,
Cellular enzymes headache, lethargy,
dizziness, seizures,
HSV1, HSV2, VZV
Acyclovir triPO4 confusion, agitation,
- Competes with DGTP thereby impaired renal function
inhibiting DNA synthesis and
consequently viral replication
Ganciclovir CMV retinitis, systemic CMV bone marrow toxicity, fever,
infection nausea, anorexia, vomiting
Ribavirin Influenza A & B, RSV

Purine Nucleoside Analogs: Adenosine

Prototype: zidavudine
Didanosine (ddI) Interferes with the HIV RNA- pancreatitis (9%),
dependent DNA polymerase HIV peripheral neuropathies
(reverse transcriptase), thus (35%), seizures, retinal
preventing replication of the virus depigmentation
Vidaribine (Ara-A) burning, itching,
inhibits DNA polymerase HSV, VZV, CMV, EBV
lacrimation, photophobia
Pyrimidine Nucleoside Analogs: Cytosine
Prototype: zidavudine
Lamovidine Inhibition of HIV reverse
transcriptase Headache
The monophosphate is Insomnia
incorporated into the viral
HIV, HBV Malaise
DNA by HBV polymerase
Pain
resulting in DNA chain
Nausea & Vomiting
termination
Peripheral neuropathy
Zalcitabine HIV
Pyrimidine Nucleoside Analogs: Thymidine
Zidovudine (AZT) Converted to a triPO4 (the Bone marrow
active form) by thymidine suppression
kinase and other cellular Nausea
enzymes HIV Anorexia
Incorporated into growing Headache
DNA chain by viral reverse Fever
transcriptase, thereby Cough
terminating viral replication Rash
Other Antivirals
Amantadine As antiviral Influenza A Orthostatic
(Symmetrel) - blocks uncoating of Other Uses: hypotension
Influenza A virus preventing - Idiopathic Parkinson’s Peripheral edema
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Disease
- Postencephalitic
viral replication
Parkinsonism Insomnia
Antiparkinsonism activity:
- Drug induced Anorexia
- blocks reuptake of dopa into
extrapyramidal Nausea
presynaptic neurons
reactions and Xerostomia
- increased dopa release from
symptomatic
presynaptic fibers
Parkinsonism
associated with _______
Foscarnet (Foscavir) Headache (26%), seizures
(10%), acute renal failure
Inhibits the replication of all
CMV (retinitis and systemic) (27%), nausea (47%),
known herpes virus in vitro
diarrhea (35%), anemia
(33%)
Indinavir Protease inhibitor
HIV protease is required for
cleaving viral polyprotein
precursors into individual final Nausea, dyslipedemia, mild
proteins found in infectious HIV-1 discoloration of indirect
HIV. Inhibition prevents bilirubin
cleavage of these polyproteins
resulting in the formation of
immature non-infectious viral
particles
Oseltamivir (Tamiflu) Neuraminidase inhibitor Fatigue
- Preventing the release of
Dizziness
nearly formed virus form Influenza A & B
Headache
the surface of the infected
Nausea & Vomiting
cells

Ang galing naming magtrans db. =p