ANTI VIRAL DRUGS

ANTI VIRAL DRUG

Anti-Herpes drugs
• Herpes is mainly caused by Herpes Simplex Virus
[HSV], it is a DNA virus
• Herpes is also known as Shingle's disease
• Chickenpox is produced by Varicella Zoster Virus
[VZV]
• It is not treated properly VZV will be transformed
to Herpes Zoster Virus [HZV]
Drugs

• Acyclovir
• Vidarabine
• Valacyclovir
• Idoxuridine
• Famciclovir
• Trifluridine
• Ganciclovir
• Fomivirsen
• Cidofovir
• Docosanol
• Foscarnet
1- ACYCLOVIR
• It is effective against HSV and VZV
• It is not effective against Cyto Megalo Virus
• It is administered 4-5 times daily due to very short half-life.
• They are applied topically, orally and IV.

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 Acyclovir
↓Thymidine kinase
Acyclovir Monophosphate
↓
Acyclovir Diphosphate
↓
Inhibition of DNA Replication

Acyclovir is converted to Acyclovir Monophosphate with the help of

Thymidine kinase enzyme.
It gets converted to Acyclovir Diphosphate which results in inhibition of
DNA replication of the virus
2- Valacyclovir and Famciclovir

• These are prodrugs of Acyclovir

• Which increase the t1/2 of Acyclovir

ADR:
 Nephrotoxicity
 Dehydration (major ADR)
 Bone marrow suppression
3- Ganciclovir
Effective against HSV and CMV
ADR:
• Myelosuppression
• Headache
• Seizures
4- Cidofovir
It is effective against HSV and CMV, Adeno virus
and Papilloma virus
ADR: Nephrotoxicity
5- Foscarnet
Given IV for CMV
ADR:
• Nephrotoxicity
• Hypokalemia
• Headache
• Seizures
6- Vidarabine, Idoxuridine, Trifluridine
• These are all used topically for the treatment Kerato-
conjunctivitis
• Idoxuridine is most preferred
7- Fomivirsen
• Used in retinitis caused by CMV

8- Docosanol

• It is an Alcohol found in breast milk, used

topically for Herpes infection.
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 ANTI- INFLUENZA DRUGS
• They are 2 types of influenza. Influenza A & Influenza B.
• Amantadine and Rimantadine is effective only against
influenza A.
• Oseltamivir (Tamiflu) & Zanamivir (Relenza) are effective
against Influenza A and B
• O and Z are the preferred agents in treatment of H1N1
(Swine flu) & H5N1 (Bird flu) H- Attachment of virus to the
host cell for replication. It is known as Hemagglutinins
N- It is responsible for the release of new virus after replication.
 ANTI-HEPATITIS DRUGS
Hepatitis A
• Hepatitis A is transmitted by fecal-oral route for the
treatment no Anti-viral drugs are used
• The agents which improve liver function, like liver
supplements are generally given.

Hepatitis B
• Hepatitis B is transmitted by sexual route
• It is treated with Antiviral agents
1- Oral agents
• Entecavir
• Lamivudine
• Adefovir
• Tenofovir
• Telbivudine
2- Parental agents
• Interferon a- 2b
• Peg INF a- 2a

Vaccination for Prevention: Immunoglobulin + Hepatitis B vaccine

Hepatitis C

• It is transmitted through contaminated syringes and

needles.
• Ribavirin (Oral route)
• Peg INF a (SC route)
 ANTI HIV DRUGS
• AIDS is caused by HIV retrovirus which contains RNA as the
genetic material.
• The major cell concern with attack of HIV virus is CD4 Cells
(Cluster of differential cells)
• Diagnosis of AIDS, Normal CD4 count: 500-1200 cells/ mm3
• CD4 count < 350 cell/ mm3 - AIDS patient
• CD4 count < 200 cell/ mm3 - The patient is at high risk
• ELISA test
• Western blot test
PATHOPHYSIOLOGY OF AIDS
 DNA replication
DNA
Reverse transcription↑ ↓ Transcription
RNA
↓ Translation
Viral proteins
1- Binding - HIV virus will be attached to CD4 receptors
located in the host cell.

2- Fusion - It allows the HIV virus to enter the host CD4 cell.

3- Reverse transcription - The HIV virus converted from RNA

to DNA with the help of Reverse transcriptase enzyme to
form HIV DNA.

4- Integration - HIV DNA is transported across the host cell

and integrated to host DNA with the help of Integrase
enzyme.
5- Replication - HIV DNA undergoes transcription and
translation to release viral proteins.

6- Assembling - The viral protein moves to the surface of the

immature cells.

7- Budding- The newly formed HIV releases Protease enzyme

to breakup long viral protein chain and the smaller proteins
combines to form mature HIV and spread the infection.
 CLASSIFICATION OF DRUGS

1- Fusion inhibitors • Maraviroc

• Vicriviroc

• Zidovudine
• Lamivudine
a) Nucleoside RTI's
• Zalcitabine
2- Reverse • Didanosine
transcriptase • Abacavir
inhibitors
• Efavirenz
b) Non- nucleosides RTI's • Etravirine
• Nevirapine
• Delavirdine
3- Integrase inhibitors: • Raltegravir
• Dolutegravir

• Saquinavir
• Ritonavir
• Indinavir
4- Protease inhibitor • Nelfinavir
• Lopinavir
• Amprenavir
• Atanzavir
• Darunavir
ANTIFUNGAL DRUGS
 ANTIFUNGALS
Classification based on MOA
Drug affecting or altering membrane permeability
• Fluconazole
• Itraconazole [Sporanox]
a) Triazoles • Voriconazole
• Tericonazole
1. Azoles
• Posaconazole
MOA:
• These drugs crosses fungal cell wall
through which K+ like ion are leaved out. • Ketoconazole
• They inhibit fungal cholesterol synthesis • Miconazole
and causes death of fungus. b) Imidazoles • Clotrimazole
• Econazole
• Butoconazole
 • Terbinafine
2. Allylamines • Butenafine
• Naftifine
• Amphotericin B
• Natamycin
3. Polyene Antibiotics
• Hamycin
• Nystatin
• Polymyxin B
• Colistin
4. Polypeptide Antibiotics
• Tyrothricin
II) Drugs inhibiting nucleic acid synthesis Flucytosine

III) Drugs inhibiting microtubule function

• Griseofulvin
[Microtubule - Cells responsible for replication]
• Caspofungin
IV) Drugs inhibiting cell wall synthesis • Micafungin
[Echinocandins] • Anidulafungin
• Nikkomycin
• Cyclopyroxolamine
• Whitefield's ointment
• [Benzoic acid + Salicylic acid]
V) Miscellaneous agent
• Haloprogin
• Tolnaftate
• Undecylenic acid
DRUGS USED FOR THE TREATMENT OF SYSTEMATIC
FUNGAL INFECTION
1. Amphotericin B:

• It is not absorbed by oral route Administered by show IV infusion

• It has a widest Antifungal spectrum
• Drug of choice for the most of the fungal infection
• Effective in treatment of Keratitis, Corneal ulcer, fungal meningitis
etc.
• It is never mixed with Normal saline due to stability problems
ADR:
• Hypokalemia
• Hypomagnesemia
• Anemia
• Renal tubular acidosis
2. Flucytosine:
• Given by Oral route
• Shows maximum activity when gives in
combination with Amphotericin B
ADR:
• Bone marrow depression
• Alopecia
• Liver dysfunction
• Hepatoxicity
3. Azoles
Ketoconazole is an enzyme inhibitor which
increases the plasma concentration of
other drugs avoided with Narrow
therapeutic index drugs like
• Warfarin
• Digoxin
• theophylline etc.
ADR:
• Gynecomastia
• Infertility
• Alopecia
 Drugs Uses
Fluconazole Maximum oral bioavailability among the azoles.

Possess widest antifungal spectrum also used in the treatment

Voriconazole
Aspergillosis (infection by type of mold/fungus affect RS)

Treatment of histoplasmosis and blastomycosis (lung infection

Itraconazole by Hstoplasma capsulatum fungal spore, Inhaling Blastomyces
dermatitidis spores from external sources)

Echinocandins Effective in the treatment of Aspergillosis

Drugs used for superficial or topical fungal
infection by oral route
1- Griseofulvin
• The absorption of Griseofulvin increased in presence of fatty
meal. It causes disulfiram like reaction with alcohol.
• It is an enzyme inducer
2- Allyl mines
• Terbinafine, Butenafine, Naftifine
• Major ADR include Rashes and GI upset
3- AZOLES
• Ketoconazole
• Fluconazole
• Itraconazole
Drugs used for topical or superficial fungal
infection by topical route
• Nystatin
• Cyclopyroxolamine
• White fields ointments
• Tolnaftate
• Undecylenic acid
• Haloprogin
• Allyl amines
Anti Protozoan drugs
 AMOBEIASIS
Caused by Entamoeba hystolytica
Classification
1- Tissue
2- Luminal or
Amebicides / Extra 3- Tissue + Luminal
Intestinal
intestinal Amebicides
Amebicides
Amebicides

• Diloxanide • Nitroimidazoles
furoate • Metronidazole
Chloroquine • Iodoquinol • Tinidazole
• Qunidoclor • Secnidazole
• Tetracyclines •
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Ornidazole
Emetine, Dihydroemetine is used by parenteral route in
treatment of Severe Hepatic Amoebiasis
Metronidazole
Uses:
• Trichomoniasis
• Giardiasis
• Bacterial vaginosis
• Peptic ulcer disease caused by H pyloric bacteria
• Pseudomembraneous Colitis [Other Rx: Vancomycin,
Teicoplanin]
ADR:
• Metallic taste
• Produce Disulfiram like action with Alcohol
Trypanosomiasis
Severe disease in vertebrates caused by Protozoan
trypanosomes
2 types:

1- African Trypanosomiasis
2- South American Trypanosomiasis
 AFRICAN SOUTH AMERICAN
TRYPANOSOMIASIS TRYPANOSOMIASIS
It caused by Trypanosomiasis
gambiense
It caused by Trypanosomiasis
• Sleeping sickness
cruzi
2 stages:
• Chagas's disease Only
1. Early hemolymphatic
hemolymphatic stage.
Stage- Suramin
• Rx: Nifurtimox
2. Late CNS stage Stage-
Melasoprol Pentamidine
 LEISHMANIASIS

It is caused by protozoa, transmitted by sand fly 3 Types

1- Visceral Leishmaniasis
2- Cutaneous Leishmaniasis
3- Mucocutaneous Leishmaniasis
Drugs:
Amphotericin B
• The drug of choice in visceral leishmaniasis

Sodium Stibogluconate
• It is an Antimony compound
• It is the most preferred drug leishmaniasis

• [Effective for all 3 types of Leishmaniasis]

Other drugs
• Fluconazole

• Metronidazole

• Allopurinol

• Mepacrine
 ANTHELMINTHS
1- Nematodes 2- Trematodes 3- Cestodes

■ Round worm
(Ascaris)
■ Hook worm ■ Pork tape worm
■ Blood fluke
(Ancylostoma) ■ Beef tape worm
(Schistosomiasis)
■ Tread worm ■ Fish tape worm
■ Lung fluke
■ Pinworm ■ Dog tape worm
■ Liver fluke
■ Filarial worm (Hydatid disease)
(Wuchereria
bancrofti)
 CLASSIFICATION
Class/ MOA Examples Uses/ DOC

Albendazole is preferred
1- Drug inhibiting polymerization Eg: Albendazole Mebendazole drug in treatment of almost
of Betatubulin Thiabendazole all Nematode infection as
well as Hydatid disease.

2- Drugs causing paralysis of Eg: Pyrantel pamoate Levamisole

helminths Ivermectin

3- Drugs affecting microphilarial Eg: Diethyl Carbamazine Citrate

Drug of choice for filariasis
membrane [DEC]

The drug of choice in

4- Drug causing outflow of Trematode and Cestode
Eg: Praziquantel (Biltricide)
Calcium infection except Hydatid
disease
 ANTIMALARIAL DRUGS
Malaria is caused by the organisms of protozoan species called
Plasmodium.
• Plasmodium vivax
• Plasmodium falciparum
• Plasmodium ovale
• Plasmodium malariae
• Plasmodium falciparum is responsible for Cerebral Malaria
• It is a deadliest species
• Plasmodium falciparum does not have Exoerythrocytic stage.
DEVELOPMENT STAGES OF MALARIAL PARASITE
 CLASSIFICATION OF DRUGS
• Proguanil
1. Primary tissue Schizonticides/
• Primaquine
Pre Erythrocytic Schizonticides
• Tetracycline
• Chloroquine
• Mepacrine
• Quinine
• Mefloquine
• Sulfonamides
2. Erythrocytic Schizonticides
• Tetracycline
• Halofantrine
• Atovaquone
• Artemisinin
• Proguanil
3. Exo Erythrocytic
Schizonticides • Primaquine

• Quinine
• Mepacrine
4. Gametocides
• Primaquine
• Artemisinin