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Pharma Antivirals and Antifungals Tabulated 1 week of 4 th Shift
Pharma
Antivirals and Antifungals Tabulated
1 week of 4 th Shift

Antifungals

MYCOTIC INFECTIONS

Pharma Antivirals and Antifungals Tabulated 1 week of 4 th Shift Antifungals MYCOTIC INFECTIONS Four General

Four General Types

Cutaneous

Subcutaneous

Can be superficial but may not be in the skin

Superficial

Systemic*

*Can be life threatening

*usually occur in immunocompromised

Cand Candida ida AAlblbicans icans
Cand
Candida
ida AAlblbicans
icans

Due

to

antibiotic

therapy,

antineoplastics, or

immunosuppresants (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 thrush

New

born

infants

&

immunocompromised

patients have increased frequency

thrush

of

oral

Vaginal Cadidiasis

“yeast infections”

Pregnancy, DM, OCP

May occur to both male and females (urethritis

and balanitis)

Antiviral Agents

Broken Down into 4 major grps based on their chem’l

structures

(1) Polyenes: amphoterincin B , nystatin

 

(2) Flucytosine

(3) Imidazoles:

ketoconazole,

miconazole,

clotrimazole, fluconazole

(4) Griseofulvin

Drug

MOA

Indication

ADR

Polyenes:

   

Fever

Amphotericin B & Nystatin

IV: fatal systemic mycotic

Malaise Ms and jt pain

Binds to sterols in cell membrane lining

infections Aspergillosis

Chills Nausea

Allowing K + & Mg 2+ to leak out, altering fungal cell metabolism Result: fungal cell death

Blastomycosis Coccidiomycosis, Paracoccidiodomycosi Histoplasmosis Sporotrichosis

Headache Hypertension Anaphylaxis Anorexia Tachycardia Renal Toxicity Neurotoxicity

Flucytosine

aka 5-fluorocytosine Taken up by fungal cells &

Alone or in combination with amphotericin B for serious systemic

Nausea, vomiting, anorexia Confusion, hallucination, headache, sedation

interferes with DNA synthesis Result: fungal cell death

infections caused by susceptible strains of

Agranulocytosis (dec WBC)

Cryptococcus & candida species

Elevated BUN & creatinine

Elevated transaminases

Imidazoles

 

Antivirals and Antifungals

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Ketoconazole

   

Rash (if topical),

 
 

Fluconazole

Interferes with synthesis of ergosterol

anaphylaxis N & V, liver cirrhosis Gynecomastia, uterine bleeding, loss of libido, impotence, oligospermia, hair loss Acute hypoaldosteronism,

 

Increase in cell permeability & ultimately inhibition of fungal cell growth

 

renal hypofunction Headache 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 essential for cell reproduction

cream and vaginal suppository

& growth as well as cell wall

Itching

structures, thus promoting cell

Irritation

death of fungi

Maceration

Allergic contact

 

dermatitis

 

Clotrimazole

Altering fungal cell membrane permeability Permeating loss of P cmpds, K & other essential intracellular constituents w/ consequent loss of ability to replicate

 

Abnormal liver function tests Stinging, erythema, edema Cystitis, urethritis Vaginal soreness during intercourse

 
 

Griseofulvin

Disrupts cell division Result: inhibited fungal mitosis (reproduction) Deposits in keratin precursor cells & has special affinity for diseased tissue. It is tightly bound to new keratin of skin, hair, & nails, w/c becomes highly resistant to fungal invasion

 

Rash, urticaria Headache Nausea/Vomiting & anorexia Leukopenia Nephrotoxicity Hepatotoxicity Overgrowth of nonsusceptible organisms (Candida)

 

Antivirals

Understanding Viruses :

Viral replication:

 
  • - A virus cannot replicate on its own

 
  • - It must attach to and enter a host cell

  • - then

It

uses

the

host’s

cell

energy

to

synthesize protein, DNA and RNA (genetic

parasites)

 
  • - Spread is fast

Viruses are difficult to kill because they live inside

our cells

Any drug that kills a virus may also kill ourselves

 

Viral Infections

Competent immune system

Best response to viral infection

A well functioning immune system will eliminate

or effectively destroy virus replication

Immunocompromised patients have frequent viral

infections

  • - Cancer patients

  • - Transplant patients

  • - AIDS patients

 

Antivirals and Antifungals

 

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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

Acyclovir

   

monoPO4

rash, nausea & vomiting,

 
Cellular enzymes

Cellular enzymes

headache, lethargy, dizziness, seizures,

Acyclovir triPO4

 

HSV1, HSV2, VZV

confusion, agitation,

-

Competes with DGTP thereby inhibiting DNA synthesis and consequently viral replication

impaired renal function

Ganciclovir

 

CMV retinitis, systemic CMV infection

bone marrow toxicity, fever, nausea, anorexia, vomiting

Ribavirin

 

Influenza A & B, RSV

 

Purine Nucleoside Analogs: Adenosine

 

Prototype: zidavudine

Didanosine (ddI)

Interferes with the HIV RNA- dependent DNA polymerase (reverse transcriptase), thus preventing replication of the virus

HIV

pancreatitis (9%), peripheral neuropathies (35%), seizures, retinal depigmentation

Vidaribine (Ara-A)

inhibits DNA polymerase

 

HSV, VZV, CMV, EBV

burning, itching, lacrimation, photophobia

Pyrimidine Nucleoside Analogs: Cytosine

 

Prototype: zidavudine Lamovidine

 

Inhibition of HIV reverse transcriptase The monophosphate is incorporated into the viral DNA by HBV polymerase resulting in DNA chain termination

 

HIV, HBV

Headache Insomnia Malaise Pain Nausea & Vomiting 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

 

Antivirals and Antifungals

Page 4 of 4

 
 
   

Disease

 
   
  • - Postencephalitic Parkinsonism

Insomnia

viral replication Antiparkinsonism activity:

  • - Drug induced extrapyramidal symptomatic

Anorexia

Nausea

  • - blocks reuptake of dopa into presynaptic neurons

  • - increased dopa release from presynaptic fibers

reactions and

Parkinsonism associated with _______

Xerostomia

 

Foscarnet (Foscavir)

Inhibits

the

replication

of

all

 

Headache (26%), seizures (10%), acute renal failure

(33%)

 
 

known herpes virus in vitro

 

CMV (retinitis and systemic)

(27%), nausea (47%),

 

diarrhea (35%), anemia

 

Indinavir

Protease inhibitor

     
 

HIV protease is required for cleaving viral polyprotein precursors into individual final proteins found in infectious HIV. Inhibition prevents cleavage of these polyproteins resulting in the formation of immature non-infectious viral

HIV-1

Nausea, dyslipedemia, mild discoloration of indirect bilirubin

 
     
 

Oseltamivir (Tamiflu)

particles Neuraminidase inhibitor

   

Fatigue

 
 
  • - Preventing

the

release

of

Dizziness

nearly

formed

virus

form

Influenza A & B

the surface of the infected cells

Headache Nausea & Vomiting

Ang galing naming magtrans db. =p