Viruses consist of a nucleic acid core surrounded by a protein capsid. Some viruses have an outer envelope. There are several stages to viral replication within a host cell, including attachment, entry, uncoating, transcription/translation, replication, assembly and release. Antiviral drugs target different stages of the viral life cycle and can be classified as inhibitors of attachment/entry, nucleic acid synthesis, uncoating/assembly, or immunomodulators. Examples of antivirals for influenza include neuraminidase inhibitors which prevent release and amantadine/rimantadine which inhibit uncoating. Ribavirin is used for RSV. Interferons, lamivudine and entecav
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
This PPT covers Drug therapy for Viral Infection or disease. It includes Viral replication cycle, classification of antiviral drugs, Anti-Herpes drug, Anti Influenza drugs, Anti hepatitis drugs and anti retroviral drugs
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
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.
nalidixic acid, the quinolones, the naphthyridines & the cinnolines, Classification, ISOSTERIC REPLACEMENT
DNA gyrase (Topo II) SAR- substitution variation, Ciprofloxacin
Antiprotozoal drugs are a class of medication used to treat infections caused by protozoa, which are single-cell organisms that belong to the type of parasites. Protozoal infections occur throughout the world and are a major cause of morbidity and mortality in some regions such as Africa and South-East Asia.
Antiviral drugs are a class of medication used specifically for treating viral infections rather than bacterial ones. Most antivirals are used for specific viral infections, while a broad-spectrum antiviral is effective against a wide range of viruses.
medicinal chemistry of Antiviral drugsFatenAlsadek
medicinal chemistry of antiviral drugs with its chemical structures and how they chemically work
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
This PPT covers Drug therapy for Viral Infection or disease. It includes Viral replication cycle, classification of antiviral drugs, Anti-Herpes drug, Anti Influenza drugs, Anti hepatitis drugs and anti retroviral drugs
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
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.
nalidixic acid, the quinolones, the naphthyridines & the cinnolines, Classification, ISOSTERIC REPLACEMENT
DNA gyrase (Topo II) SAR- substitution variation, Ciprofloxacin
Antiprotozoal drugs are a class of medication used to treat infections caused by protozoa, which are single-cell organisms that belong to the type of parasites. Protozoal infections occur throughout the world and are a major cause of morbidity and mortality in some regions such as Africa and South-East Asia.
Antiviral drugs are a class of medication used specifically for treating viral infections rather than bacterial ones. Most antivirals are used for specific viral infections, while a broad-spectrum antiviral is effective against a wide range of viruses.
medicinal chemistry of Antiviral drugsFatenAlsadek
medicinal chemistry of antiviral drugs with its chemical structures and how they chemically work
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
classification of antiviral agents,replication of HIV virus and replication of virus.targets of virus,classification of antiviral agents with structure and mechanism action of antiviral agents
Antiviral Drugs – A Brief (Classification & Mechanism of Actions)Parth Thosani
This presentation gives you an overview of antiviral agents (both retro and non-retro viruses), focusing on the sites of actions, classification and class-wise mechanism of actions.
TREATMENT OF RESPIRATORY VIRUS INFECTIONS
A.Neuraminidase inhibitors
NAIs block the release of the influenza virus from infected host cells and thus reduce the spread of infection in the respiratory tract.
B.Inhibitors of viral uncoating
amantadine and rimantad are example of drug for viral uncoating inhibitors
the drugs effective in both treatment and prevention
Ribavirin
Ribavirin is a synthetic guanosine analog.
It is effective against a broad spectrum of RNA and DNA viruses.
. Lamivudine This cytosine analog
is an inhibitor of both hepatitis B virus (HBV) DNA polymerase and human immunodeficiency virus (HIV) reverse transcriptase.
. Adefovir dipivoxil is a nucleotide analog that is phosphorylated to adefovir diphosphate , which is
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
ABDOMINAL TRAUMA in pediatrics part one.drhasanrajab
Abdominal trauma in pediatrics refers to injuries or damage to the abdominal organs in children. It can occur due to various causes such as falls, motor vehicle accidents, sports-related injuries, and physical abuse. Children are more vulnerable to abdominal trauma due to their unique anatomical and physiological characteristics. Signs and symptoms include abdominal pain, tenderness, distension, vomiting, and signs of shock. Diagnosis involves physical examination, imaging studies, and laboratory tests. Management depends on the severity and may involve conservative treatment or surgical intervention. Prevention is crucial in reducing the incidence of abdominal trauma in children.
Basavarajeeyam is an important text for ayurvedic physician belonging to andhra pradehs. It is a popular compendium in various parts of our country as well as in andhra pradesh. The content of the text was presented in sanskrit and telugu language (Bilingual). One of the most famous book in ayurvedic pharmaceutics and therapeutics. This book contains 25 chapters called as prakaranas. Many rasaoushadis were explained, pioneer of dhatu druti, nadi pareeksha, mutra pareeksha etc. Belongs to the period of 15-16 century. New diseases like upadamsha, phiranga rogas are explained.
Adv. biopharm. APPLICATION OF PHARMACOKINETICS : TARGETED DRUG DELIVERY SYSTEMSAkankshaAshtankar
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Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
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NVBDCP.pptx Nation vector borne disease control programSapna Thakur
NVBDCP was launched in 2003-2004 . Vector-Borne Disease: Disease that results from an infection transmitted to humans and other animals by blood-feeding arthropods, such as mosquitoes, ticks, and fleas. Examples of vector-borne diseases include Dengue fever, West Nile Virus, Lyme disease, and malaria.
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Basavarajeeyam is a Sreshta Sangraha grantha (Compiled book ), written by Neelkanta kotturu Basavaraja Virachita. It contains 25 Prakaranas, First 24 Chapters related to Rogas& 25th to Rasadravyas.
2. Virion
• Virus consists of:
• A core genome of Nucleic acid which may be either double stranded
or single stranded DNA or RNA (but not both), surrounded by a
protein shell or capsid.
• Capsid is composed of capsomeres, which consist of one or two
molecules of polypeptides.
• Capsid and its enclosed nucleic acid is called nucleocapsid
• In some viruses a lipoprotein membrane or envelope surrounds the
nucleocapsid and may contain antigenic viral glycoproteins.
• The whole infective particle is called VIRION.
• Viruses are intracellular parasites which utilize host cell machinery
to synthesize new viral protein and genetic material
5. Replication of Viruses
1. Attachment / Adhesion
2. Penetration
i. Endocytosis
ii. Fusion
iii. Translocation
3. Uncoating
4. Transcription (synthesis of mRNA)
5. Translation
i. Early translation (synthesis of proteins)
ii. Late translation (synthesis of proteins)
6. Replication
7. Assembly (formation of capsomeres, capcid,
Nucleocapcid, envelope)
8. Release
6.
7.
8.
9.
10. Classification
• I. Inhibitors of viral attachment and penetration:
Gamma-globulin (IgG):Neutralize viruses and prevent
attachment and penetration
• II. Inhibitors of viral nucleic acid synthesis.
1. Purine analogues
Acyclovir, Valacyclovir, Ganciclovir,
Penciclovir, Ribavirin etc.
2. Pyrimidine analogues
Zidovudine, Idoxuridine, trifluridine, cytarabine etc.
3. Pyrophosphate analogues
Foscarnet
III. Inhibitors of uncoating and viral assembly:
1. Prevent viral uncoating
Amantadine, Rimantadine
2. Neuraminidase inhibitors
Oseltamivir, Zanamivir
12. Chemotherapy of Viral Infections
• 1. Drugs for respiratory virus infections
• 2. Drugs for Hepatic Viral Infections
• 3. Drugs for Herpes virus infection
• 4. Drugs for HIV Infection
13. Treatment of respiratory virus infections
• A. Neuraminidase Inhibitors: (For type A&B)
• Oseltamivir (Tamiflu)
• Zanamavir (Relenza)
• B. Inhibitors of viral uncoating: (For type A)
• Amantadine
• Rimantadine
C. Ribavirin: (For Respiratory syncytial virus
RSV)
Interference with viral messenger RNA
15. Drugs for Respiratory Virus Infections
• Viral respiratory tract infections for which
treatments exist include those of influenza A
and B and respiratory syncytial virus (RSV).
• A. Neuraminidase inhibitors:
• Neuraminidase is an enzyme found on the virus
which cleaves sialic acid from cell membrane,
leading to a more effective release of viruses.
• Oseltamivir and Zanamivir are effective
against both Type A and Type B influenza
viruses.
• Both drugs are eliminated unchanged in the
urine.
17. Drug Examples
Tamiflu-
• Recently sold to 40
countries to battle avian flu
• It is a neuraminidase
inhibitor, it works on both
influenza A and B
18. B. Inhibitors of viral uncoating
• The therapeutic spectrum of amantadine and
rimantadine is limited to influenza A infections,
equally effective in both treatment and prevention.
• Mode of action: The primary antiviral mechanism
of amantadine and rimantadine is to block the
viral membrane matrix protein, M2, which
functions as a channel for hydrogen ion.
This channel is required for the fusion of the viral
membrane with the cell membrane that ultimately
forms the endosome (created when the virus is
internalized by endocytosis).
[Note: The acidic environment of the endosome
is required for viral uncoating.]
• These drugs may also interfere with the release of
20. C. Ribavirin
• Mode of action: The mode of action of ribavirin
has been studied only for the influenza 1. viruses.
The drug is
first converted to the 5'-phosphate derivatives,
the major product being the compound ribavirin-
triphosphate,
which exerts its antiviral action by inhibiting
guanosine triphosphate formation, preventing viral
mRNA capping,
and blocking RNA-dependent RNA polymerase.
• [Note: Rhinoviruses and enteroviruses, which
contain preformed mRNA and do not need to
synthesize mRNA in the host cell to initiate an
infection, are relatively resistant to the action of
ribavirin.]
• It is used for RSV in infants and children, but not
22. Drugs for Hepatic Viral Infections
• A. Interferon ( for HBV & HCV)
• B. Lamivudine ( for HBV & HIV)
• C. Adefovir (hepatitis B and herpes
simplex virus infection).
• D. Entecavir ( for HBV)
23. Drugs for Herpesvirus infection
• A. Acyclovir
• B. Cidofovir
• C. Fomivirsen
• D. Foscarnet
• E. Ganciclovir
• F. Penciclovir and famcicolvir
G. Vidarabine
H. Trifluridine
31. Treatment for HIV Infection
• Approval of zidovudine in 1987.
• Multi drug regimen is commonly referred to as highly
active antiretroviral therapy,or HAART.
• There are five classes of antiretroviral drugs, each of
which targets one of four viral processes.
• These classes of drugs are:
I. Nucleoside and nucleotide reverse transcriptase
inhibitors (NRTIs)
2. Non-nucleoside reverse transcriptase inhibitors
(NNRTIs),
3. Protease inhibitors,
4. Entry inhibitors .
5. Integrase inhibitors.
• The current recommendation for primary therapy is to
administer two NRTIs with either a protease inhibitor
or an NNRTI.
32. • To enable HIV to be integrated into the
host DNA and so use the cell's genetic
machinery to make new virus, the single-
stranded viral RNA must first be converted
to double-stranded DNA by the viral
enzyme reverse transcriptase, while the
enzyme RNAse-H hydrolyses the RNA
after it has been copied. Nucleoside and
non-nucleoside reverse-transcriptase
inhibitors are two classes of antiretroviral
drugs that suppress HIV replication by
33.
34.
35. • A. Nucleoside reverse-transcriptase
inhibitors are similar in structure to the
building blocks that make up DNA. By
incorporating themselves into the DNA
nucleoside chain being produced by
reverse transcriptase, they stop
attachment of further nucleosides and so
prevent ongoing viral DNA synthesis.
• B. Non-nucleoside reverse transcriptase
inhibitors attach to the reverse
transcriptase and affect the activity of the
enzyme by restricting its mobility and
36. Mechanism of action of nucleoside and non-nucleoside reverse-
transcriptase inhibitors
41. • Nucleoside analog reverse transcriptase
inhibitors (NRTIs) are nucleoside
analogues that act as competitive
inhibitors of HIV-1 reverse transcriptase.
These drugs compete with nucleoside
triphosphates for access to reverse
transcriptase.
• All NRTIs lack a 3-hydroxyl group; thus,
their incorporation into a growing DNA
chain results in its termination. They
require intracytoplasmic activation via
phosphorylation by cellular enzymes to the
42. • List of NRTIs
• Zidovudine or azidothymidine (AZT) (also
called ZDV): first approved drug in its class.
• Didanosine (ddI): second FDA-approved drug
for the treatment of HIV infection.
• Tenofovir (TDF): first nucleotide analog. It has
significant drug interactions.
• Lamivudine (3TC): also used in the treatment
of HBV infection.
• Emtricitabine (FTC): acts as an inhibitor of
HBV and HIV transcriptase.
• Abacavir (ABC): a guanosine analog
47. Protease inhibitors
• After transcription in the nucleus, viral mRNA
enters the cytoplasm and uses the host's
cellular machinery to manufacture virus
proteins. The viral components then gather at
the cell membrane and immature viruses bud
off the cell. Core proteins are produced as
part of long polypeptides, which must be cut
into smaller fragments by the enzyme
protease in order to form mature, functional
proteins.
• Protease inhibitors bind to the site where
protein cutting occurs, and so prevent the
enzyme from releasing the individual core
50. Integrase Inhibitors
Raltegravir (RAL)
Integrase is one of three HIV-1 enzymes
required for viral replication
Results in integration of HIV-1 DNA into host cell
genome
Raltegravir targets viral integrase