7.ANTIVIRAL DRUGS

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Antiviral drugs are a class of medication used specifically for treating viral infections.Like antibiotics for bacteria, specific antivirals are used for specific viruses. Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit their development. Antiviral drugs are one class of antimicrobials, a larger group which also includes antibiotic (also termed antibacterial), antifungal and antiparasitic drugs,or antiviral drugs based on monoclonal antibodies. Most antivirals are considered relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from viricides, which are not medication but deactivate or destroy virus particles, either inside or outside the body. Antivirals also can be found in essential oils of some herbs, such as eucalyptus oil and its constituents.

Gesundheit & Medizin

BYBY
Dr.Dr. SAMINATHAN KAYAROHANAMSAMINATHAN KAYAROHANAM
M.PHARM, M.B.A, PhDM.PHARM, M.B.A, PhD
ANTIVIRAL DRUGS
1
7

2
NUM CONTENT SLIDE
11 INTRODUCTION TO VIRUS 4
22 THE STRUCTURE OF VIRUSES 5-7
33 VIRUSES SIZE COMPARISON BETWEEN E.COLI 8
44 TYPE OF VIRUS (RNA VIRUS) (DNA VIRUS) 9,10
55 CLASSIFICATION OF ANTIVIRAL DRUGS 11
66 MECHANISM OF ANTIVIRAL AGENTS 12
77 MECHANISM OF SELECTED ANTIVIRAL AGENTS 13-15
88 HIGHLY ACTIVE ANTIRETROVIRAL (HIV) THERAPY
(HAART)
16
99 DRUGS USED TO PREVENT HIV FROM REPLICATING
1010 TOXIC EFFECT OF PROTEASE INHIBITORS/ANTIVIRAL
DRUG
19-22

3 Con…
LEARNING OUTCOME
1. Describe and understand the virus and structure of
virus.
2. Able to understand the types of viruses.
3. List the classification of drugs used to treat virus
infections.
4. Abele to demonstrate the general mechanism of
antivirus drugs.
5. Describe the adverse drug reaction of antiviral drugs.
6. Able to understand the antivirus available drugs and
dose in the market.

4
1.INTRODUCTION TO VIRUS
Virion size range is ~10-400
nm
All virions contain a
nucleocapsid which is
composed of nucleic acid
(DNA or RNA) and a protein
coat (capsid)
Some viruses consist only of
a nucleocapsid, others have
additional components
Envelopes
• virions having envelopes
= enveloped viruses
• virions lacking envelopes
= naked viruses
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

5
2.THE STRUCTURE OF VIRUSES
Con…
CYTOMEGALOVIRUS
Many viruses that infect humans and other animals are
enveloped.
Envelopes form when viral glycoproteins and oligosaccharides
associate with the plasma membrane of the host cell.
All envelopes have a phospholipid bilayer.
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

2.VIRAL ENVELOPES
6
Envelopes vary in:
Size
Morphology
Complexity
Composition
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

2.GENOMIC PACKAGING
7
Genome packaging has an important role
in the infection.
Viral genomes are packaged in one of
three ways:
• Directly in the capsid-inner side of the
protein coat
• Enclosed in special proteins-nucleic acid
binding protein
• Enclosed in proteins from the host cell
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

3.VIRUSES SIZE COMPARISON BETWEEN E.COLI
8
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

9
4.TYPE OF VIRUS (RNA VIRUS)
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

10
4.TYPE OF VIRUS (DNA VIRUS)
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

11
4.TYPE OF VIRUS (DNA VIRUS)
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

12
5.CLASSIFICATION OF ANTIVIRAL DRUGS
1
2
3
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

6.MECHANISM OF ANTIVIRAL AGENTS
13Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

7.MECHANISM OF SELECTED ANTIVIRAL AGENTS
Con…
14
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

15
7.MECHANISM OF SELECTED ANTIVIRAL AGENTS
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

8.HIGHLY ACTIVE ANTIRETROVIRAL (HIV) THERAPY (HAART)
16 4Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

9.DRUGS USED TO PREVENT HIV FROM
REPLICATING
Con…17 Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

9.DRUGS USED TO PREVENT HIV FROM
REPLICATING
18
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

10.TOXIC EFFECT OF PROTEASE INHIBITORS/ANTIVIRAL DRUG
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

20
HYPERSENSITIVITY REACTIONS TO
ABACAVIR
SOME ADVERSE EFFECTS OF
THE HIV PROTEASE INHIBITORS
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

21
ADVERSE REACTIONS OF
EFAVIRENZ
ADVERSE REACTIONS OF
NUCLEOSIDE ANALOGS
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

22
ADMINISTRATION, METABOLISM, AND TOXICITY OF
ZIDOVUDINE (AZT) DIDANOSINE
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

23
11
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

24
2
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

25
3
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

26
4
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

27
4
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

4
28
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

4
29
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

4
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Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

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An antifungal medication is a pharmaceutical fungicide used to treat and prevent mycoses such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually obtained by a doctor's prescription, but a few are available OTC (over-the-counter). Antifungals work by exploiting differences between mammalian and fungal cells to kill the fungal organism with fewer adverse effects to the host. Unlike bacteria, both fungi and humans are eukaryotes. Thus, fungal and human cells are similar at the biological level. This makes it more difficult to discover drugs that target fungi without affecting human cells. As a consequence, many antifungal drugs cause side-effects. Some of these side-effects can be life-threatening if the drugs are not used properly.

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A protein synthesis inhibitor is a substance that stops or slows the growth or proliferation of cells by disrupting the processes that lead directly to the generation of new proteins. All of the antibiotics that target bacterial protein synthesis do so by interacting with the bacterial ribosome and inhibiting its function. The ribosome might not seem like a very good target for selective toxicity, because all cells, including our own, use ribosomes for protein synthesis.The good thing is that bacteria and eukaryotes have ribosomes that are structurally different. Bacteria have so-called 70S ribosomes and eukaryotes have 80S ribosomes. No, not '70s and '80s ribosomes, although that would be pretty entertaining. The S stands for 'Svedberg unit,' and it refers to the rate at which particles sediment down into the tube during high-speed ultracentrifugation. Basically, it tells us about the ribosome's molecular weight and shape. 70S and 80S ribosomes are different enough that antibiotics can specifically target one and not the other. Let's take a closer look at the bacterial 70S ribosome and see where some different kinds of antibiotics act on it. Remember that ribosomes are made of RNA and protein and that they have two subunits, one large and one small. The bacterial 70S ribosome's subunits are the 50S subunit and the 30S subunit. Yes, I know, 50 + 30 = 80, not 70, but this is not a math mistake. Using the Svedberg unit to measure ribosomes means that things don't always add up perfectly, because rates of sedimentation are not additive like molecular weights are. Before we get into the specifics of how antibiotics inhibit bacterial ribosomes, let's briefly review how ribosomes work. First, a tRNA loaded with a particular amino acid enters the ribosome at the A site. The tRNA's anticodon has to match the codon, or group of three nucleotides on the mRNA. Then, at the P site of the ribosome, a peptide bond forms between the previous amino acid and the new amino acid. Finally, the empty tRNA exits at the E site. This process repeats for the whole length of the mRNA, and the polypeptide chain continues to grow.

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The most common mode of action for antibiotics is the inhibition of cell wall synthesis. Antibiotics that inhibit cell wall synthesis work because of the fact that most eubacteria have peptidoglycan-based cell walls but mammals do not. Growth is prevented by inhibiting peptidoglycan synthesis. Thus these antibiotics only work for actively growing bacteria. The cell wall of new bacteria that grew in the presence of cell-wall-synthesis inhibitors is deprived of peptidoglycan. These bacteria will be subjected to osmotic lysis.In addition, gram-negative bacteria generally are less susceptible to inhibitors of cell wall synthesis than are gram-positive bacteria. In the former cell wall synthesis inhibitors fail to reach the cell wall because they are blocked by the gram-negative outer membrane.Penicillin is the classic example of an inhibitor of cell wall synthesis. Other examples include: ampicillin, bacitracin, carbapenems, cephalosporin, methicillin, oxacillin and vancomycin

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