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Anti-Fungals and Anti-Virals - Table

Anti-Fungals and Anti-Virals - Table

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Published by: sarguss14 on Jan 06, 2009
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Pharma
Antivirals and Antifungals Tabulated
1 week of 4
th
Shift
Antifungals
MYCOTIC INFECTIONS
Four General TypesCutaneousSubcutaneous
Can be superficial but may not be in the skin
SuperficialSystemic**Can be life threatening*usually occur in immunocompromised
Candida AlbicansCandida Albicans
Due to antibiotic therapy, antineoplastics, orimmunosuppresants
(steroids)
May result in overgrowth & systemic infections
Opportunistic organism, may multiply in number because of the decline in the normal flora
In the mouth:Oral candidiasis or thrushNew born infants & immunocompromisedpatients
have increased frequency of oralthrush
Vaginal Cadidiasis
“yeast infections”Pregnancy, DM, OCP
May occur to both male and females (urethritisand balanitis)
Antiviral Agents
Broken Down into 4 major grps based on their chem’lstructures(1)Polyenes: amphoterincin B , nystatin(2)Flucytosine
(3)
Imidazoles: ketoconazole, miconazole,clotrimazole, fluconazole(4)Griseofulvin
DrugMOAIndicationADRPolyenes
:Amphotericin B &NystatinBinds to sterols in cellmembrane liningAllowing K 
+
& Mg
2+
to leak out,altering fungal cellmetabolismResult: fungal cell death
IV
: fatal systemic mycoticinfectionsAspergillosisBlastomycosisCoccidiomycosis,ParacoccidiodomycosiHistoplasmosisSporotrichosisFeverMalaiseMs and jt painChillsNauseaHeadacheHypertensionAnaphylaxisAnorexia TachycardiaRenal ToxicityNeurotoxicity
Flucytosine
aka 5-fluorocytosine Taken up by fungal cells &interferes with DNA synthesisResult: fungal cell deathAlone or in combinationwith amphotericin B forserious systemicinfections caused bysusceptible strains of Cryptococcus & candidaspeciesNausea, vomiting,anorexiaConfusion,hallucination,headache, sedationAgranulocytosis
(decWBC)
Elevated BUN &creatinineElevated transaminases
Imidazoles
 
maro03267 + maltaaiko =1 of 4
 
 Antivirals and Antifungals
Page
2
of 4
KetoconazoleFluconazoleInterferes with synthesis of ergosterolIncrease in cell permeability &ultimately inhibition of fungalcell growthRash (if topical),anaphylaxisN & V, liver cirrhosisGynecomastia, uterinebleeding, loss of libido,impotence,oligospermia, hair lossAcutehypoaldosteronism,renal hypofunctionHeadacheNausea and vomitingAbdominal painDiarrheaIncrease AST in Px w/cryptococcal meningitis& AIDSRashMiconazoleinhibit uptake of componentsessential for cell reproduction& growth as well as cell wallstructures, thus promoting celldeath of fungiVulvovaginal burning
when used as ointment,cream and vaginalsuppository 
ItchingIrritationMacerationAllergic contactdermatitisClotrimazoleAltering fungal cell membranepermeabilityPermeating loss of P cmpds, K & other essential intracellularconstituents w/ consequentloss of ability to replicateAbnormal liver functiontestsStinging, erythema,edemaCystitis, urethritisVaginal soreness duringintercourse
Griseofulvin
Disrupts cell divisionResult: inhibited fungalmitosis (reproduction)Deposits in keratin precursorcells & has special affinity fordiseased tissue. It is tightlybound to new keratin of skin,hair, & nails, w/c becomeshighly resistant to fungalinvasionRash, urticariaHeadacheNausea/Vomiting &anorexiaLeukopeniaNephrotoxicityHepatotoxicityOvergrowth of nonsusceptibleorganisms (Candida)
Antivirals
Understanding Viruses
:
 
Viral replication:-A virus cannot replicate on its own-It must attach to and enter a host cell-It then uses the hosts cell energy tosynthesize protein, DNA and RNA (geneticparasites)-Spread is fast
Viruses are difficult to kill because they live insideour cells
Any drug that kills a virus may also kill ourselvesViral InfectionsCompetent immune system
Best response to viral infection
A well functioning immune system will eliminateor effectively destroy virus replication
Immunocompromised patients have frequent viralinfections-Cancer patients-Transplant patients-AIDS patients
 
 Antivirals and Antifungals
Page
3
of 4
Viruses Affected by Current Antiviral Therapy
Cytomegalovirus (CMV) retinitis
Herpes Simplex Virus (HSV)
o
HSV 1: oral aphthous ulcers
o
HSV 2: genital ulcers
Varicella Zoster Virus (VZV)-Chickenpox, shingles
Human Immunodeficiency Virus (HIV)
Influenza A Virus (Flu)
Respiratory Synctial Virus (RSV)
Hepatitis B Virus (HBV)
Antivirals
Synthetic purine nucleoside analogs
 Two types of nucleosidesa.Purine – Guanine, Adenosineb.Pyrimidine – Thymidine, Cytosine 
DrugMOAAntiviral ActivityADRPurine Nucleoside Analogs: Guanines
Acyclovir (Prototype)Acyclovir AcyclovirmonoPO4Acyclovir triPO4-Competes with DGTP therebyinhibiting DNA synthesis andconsequently viral replicationHSV1, HSV2, VZVrash, nausea & vomiting,headache, lethargy,dizziness, seizures,confusion, agitation,impaired renal functionGanciclovirCMV retinitis, systemic CMVinfectionbone marrow toxicity, fever,nausea, anorexia, vomitingRibavirinInfluenza A & B, RSV
Purine Nucleoside Analogs: Adenosine
Prototype: zidavudineDidanosine (ddI)Interferes with the HIV RNA-dependent DNA polymerase(reverse transcriptase), thuspreventing replication of the virusHIVpancreatitis (9%),peripheral neuropathies(35%), seizures, retinaldepigmentationVidaribine (Ara-A)inhibits DNA polymeraseHSV, VZV, CMV, EBVburning, itching,lacrimation, photophobia
Pyrimidine Nucleoside Analogs: Cytosine
Prototype: zidavudineLamovidineInhibition of HIV reversetranscriptase The monophosphate isincorporated into the viralDNA by HBV polymeraseresulting in DNA chainterminationHIV, HBVZalcitabineHIVHeadacheInsomniaMalaisePainNausea & VomitingPeripheral neuropathy
Pyrimidine Nucleoside Analogs: Thymidine
Zidovudine (AZT)Converted to a triPO4 (theactive form) by thymidinekinase and other cellularenzymesIncorporated into growingDNA chain by viral reversetranscriptase, therebyterminating viral replicationHIVBone marrowsuppressionNauseaAnorexiaHeadacheFeverCoughRash
Other Antivirals
Amantadine(Symmetrel)As antiviral-blocks uncoating oInfluenza A virus preventingInfluenza AOther Uses:-Idiopathic Parkinson’sOrthostatichypotensionPeripheral edema
 
Cellular enzymes

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