This document discusses antiviral agents for nonretrovirals. It begins by outlining the key learning objectives which are to describe viral infections, classification of antiviral agents, their mechanisms of action and resistance. It then classifies antiviral agents into non-retroviral and antiretroviral categories. Under non-retroviral agents, it describes treatments for influenza, herpes and hepatitis viruses. It provides details on specific drugs for each virus type, including their mechanisms of action, resistance and pharmacokinetics.
Antiviral drugs are a class of medications used to treat viral infections by inhibiting the replication or growth of viruses in the body. These drugs work by targeting specific components of a virus, such as the viral enzymes, proteins, or nucleic acids, and disrupting their ability to infect or replicate inside host cells. This can help reduce the severity of symptoms, prevent complications, and speed up recovery.
There are many types of antiviral drugs available, including:
1. Nucleoside or nucleotide analogues: These drugs mimic the structure of the nucleosides or nucleotides needed for viral replication, thereby interfering with virus replication.
2. Protease inhibitors: These drugs block the activity of viral proteases, which are enzymes that are required for the replication and assembly of some viruses.
3. Interferons: These drugs are naturally occurring proteins that help the immune system fight viral infections by boosting the body's antiviral response.
4. Neuraminidase inhibitors: These drugs block the activity of viral neuraminidase, an enzyme that is required for the release of virus particles from infected cells.
5. Fusion inhibitors: These drugs block the fusion of viral and host cell membranes, which is an essential step in viral entry and replication.
Antiviral drugs can be used to treat a variety of viral infections, including influenza, HIV/AIDS, hepatitis B and C, herpes, and Ebola. However, the effectiveness of these drugs can vary depending on the specific virus and the stage of infection. Antiviral drugs may also have side effects, and it is important to consult with a healthcare provider before taking them.
I have tried to provide an outline regarding the general antivirals available in our country..and discussed regarding MOA,indications and Therapeutic uses.
Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit its development.
Antiviral drugs are a class of medications used to treat viral infections by inhibiting the replication or growth of viruses in the body. These drugs work by targeting specific components of a virus, such as the viral enzymes, proteins, or nucleic acids, and disrupting their ability to infect or replicate inside host cells. This can help reduce the severity of symptoms, prevent complications, and speed up recovery.
There are many types of antiviral drugs available, including:
1. Nucleoside or nucleotide analogues: These drugs mimic the structure of the nucleosides or nucleotides needed for viral replication, thereby interfering with virus replication.
2. Protease inhibitors: These drugs block the activity of viral proteases, which are enzymes that are required for the replication and assembly of some viruses.
3. Interferons: These drugs are naturally occurring proteins that help the immune system fight viral infections by boosting the body's antiviral response.
4. Neuraminidase inhibitors: These drugs block the activity of viral neuraminidase, an enzyme that is required for the release of virus particles from infected cells.
5. Fusion inhibitors: These drugs block the fusion of viral and host cell membranes, which is an essential step in viral entry and replication.
Antiviral drugs can be used to treat a variety of viral infections, including influenza, HIV/AIDS, hepatitis B and C, herpes, and Ebola. However, the effectiveness of these drugs can vary depending on the specific virus and the stage of infection. Antiviral drugs may also have side effects, and it is important to consult with a healthcare provider before taking them.
I have tried to provide an outline regarding the general antivirals available in our country..and discussed regarding MOA,indications and Therapeutic uses.
Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit its development.
Pharmacology and therapeutics of Antiretroviral agentPrajwalGhatol1
Title: Antiretroviral Agents Pharmacology
Introduction:
Antiretroviral agents play a crucial role in the management of human immunodeficiency virus (HIV) infections. HIV is a retrovirus that attacks the immune system, specifically the CD4 cells (T cells), leading to a weakened immune system and increased susceptibility to various infections. Antiretroviral therapy (ART) aims to suppress viral replication, maintain or restore immune function, and improve overall quality of life. This note provides a detailed overview of the pharmacology of antiretroviral agents.
Classification of Antiretroviral Agents:
Antiretroviral agents are classified into several classes based on their mechanism of action:
a. Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs):
- Examples: Zidovudine, Lamivudine, Tenofovir.
- Mechanism: They inhibit reverse transcriptase, an enzyme essential for viral DNA synthesis, by acting as faulty substrates.
b. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs):
- Examples: Efavirenz, Nevirapine, Rilpivirine.
- Mechanism: They bind directly to reverse transcriptase, causing conformational changes that inhibit its activity.
c. Protease Inhibitors (PIs):
- Examples: Atazanavir, Darunavir, Ritonavir.
- Mechanism: PIs interfere with the protease enzyme, hindering the cleavage of viral polyproteins and preventing the maturation of infectious viral particles.
d. Integrase Strand Transfer Inhibitors (INSTIs):
- Examples: Raltegravir, Elvitegravir, Dolutegravir.
- Mechanism: INSTIs block the integrase enzyme, preventing the integration of viral DNA into the host genome.
e. Entry Inhibitors:
- Examples: Enfuvirtide, Maraviroc.
- Mechanism: Enfuvirtide inhibits the fusion of viral and cellular membranes, while Maraviroc blocks the CCR5 receptor, preventing viral entry into the cell.
Pharmacokinetics:
a. Absorption:
Antiretroviral drugs can be taken orally, and their absorption may be affected by food. For instance, some PIs are better absorbed with food, while others should be taken on an empty stomach.
b. Distribution:
Antiretrovirals distribute widely in the body, including the central nervous system. Some drugs have specific formulations to enhance their penetration into sanctuary sites.
c. Metabolism:
Many antiretrovirals undergo hepatic metabolism, primarily through the cytochrome P450 system. Drug interactions may occur, influencing the metabolism of co-administered medications.
d. Excretion:
Renal excretion is a significant route for some antiretrovirals. Dosing adjustments are necessary in patients with renal impairment.
Resistance:
a. Mechanisms:
HIV has a high mutation rate, leading to the emergence of drug-resistant strains. Resistance can result from mutations in the viral genome, reducing drug binding or increasing the efficiency of viral replication.
b. Prevention:
Combination therapy, or highly active antiretroviral therapy (HAART), is employed to reduce the risk of resistance. This involves using
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
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Pharmacology and therapeutics of Antiretroviral agentPrajwalGhatol1
Title: Antiretroviral Agents Pharmacology
Introduction:
Antiretroviral agents play a crucial role in the management of human immunodeficiency virus (HIV) infections. HIV is a retrovirus that attacks the immune system, specifically the CD4 cells (T cells), leading to a weakened immune system and increased susceptibility to various infections. Antiretroviral therapy (ART) aims to suppress viral replication, maintain or restore immune function, and improve overall quality of life. This note provides a detailed overview of the pharmacology of antiretroviral agents.
Classification of Antiretroviral Agents:
Antiretroviral agents are classified into several classes based on their mechanism of action:
a. Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs):
- Examples: Zidovudine, Lamivudine, Tenofovir.
- Mechanism: They inhibit reverse transcriptase, an enzyme essential for viral DNA synthesis, by acting as faulty substrates.
b. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs):
- Examples: Efavirenz, Nevirapine, Rilpivirine.
- Mechanism: They bind directly to reverse transcriptase, causing conformational changes that inhibit its activity.
c. Protease Inhibitors (PIs):
- Examples: Atazanavir, Darunavir, Ritonavir.
- Mechanism: PIs interfere with the protease enzyme, hindering the cleavage of viral polyproteins and preventing the maturation of infectious viral particles.
d. Integrase Strand Transfer Inhibitors (INSTIs):
- Examples: Raltegravir, Elvitegravir, Dolutegravir.
- Mechanism: INSTIs block the integrase enzyme, preventing the integration of viral DNA into the host genome.
e. Entry Inhibitors:
- Examples: Enfuvirtide, Maraviroc.
- Mechanism: Enfuvirtide inhibits the fusion of viral and cellular membranes, while Maraviroc blocks the CCR5 receptor, preventing viral entry into the cell.
Pharmacokinetics:
a. Absorption:
Antiretroviral drugs can be taken orally, and their absorption may be affected by food. For instance, some PIs are better absorbed with food, while others should be taken on an empty stomach.
b. Distribution:
Antiretrovirals distribute widely in the body, including the central nervous system. Some drugs have specific formulations to enhance their penetration into sanctuary sites.
c. Metabolism:
Many antiretrovirals undergo hepatic metabolism, primarily through the cytochrome P450 system. Drug interactions may occur, influencing the metabolism of co-administered medications.
d. Excretion:
Renal excretion is a significant route for some antiretrovirals. Dosing adjustments are necessary in patients with renal impairment.
Resistance:
a. Mechanisms:
HIV has a high mutation rate, leading to the emergence of drug-resistant strains. Resistance can result from mutations in the viral genome, reducing drug binding or increasing the efficiency of viral replication.
b. Prevention:
Combination therapy, or highly active antiretroviral therapy (HAART), is employed to reduce the risk of resistance. This involves using
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
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
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Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
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
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
2. Learning Outcomes
• Outline the main features of viral infections, viral
structure, and steps involved in viral replicative life
cycle.
• Classification of antiviral agents according to their
spectrum of activity.
• Discuss the mechanisms of action of antiviral agents.
• Discuss the mechanisms of resistance of antiviral
agents.
• Explain the:
Pharmacokinetics of antiviral agents.
Adverse effects of antiviral agents.
Drug-drug interactions.
4. Viruses are smaller than bacteria ,and they cannot be observed using a light
microscope.
They lack both a cell wall and a cell membrane, and they do not carry out
metabolic processes.
A virus cannot replicate on its own, they replicate only inside living cells
They contain either DNA or RNA, but not both
. Viruses are difficult to be killed because, and any drug that kills a virus may also kill
the host cells.
Viral diseases are further complicated by the fact that the clinical symptoms appear late
in the course of the disease, at a time when most of the virus particles have replicated.
This contrasts with bacterial diseases, in which the clinical symptoms are usually
coincident with bacterial proliferation.
Viruses are different from other Microbes
5.
6. Key characteristics of antiviral drugs
• Most Antiviral drugs inhibit viral replication.
• They do not eliminate non-replicating or latent virus.
Therefore, the viral growth resumes after drug removal.
• The cure depends on the host immune system to
eradicate.
• Best responses to antiviral drugs are in patients with
competent immune systems.
• Many Antiviral drugs are Prodrugs , They need to be
activated by viral and cellular enzymes to produce the
antiviral effect.
o How do they act ?????
o Antiviral drugs can enter the cells infected with virus
o Interfere with viral nucleic acid synthesis and/or
regulation
o Some drugs interfere with ability of virus to bind to cells
o Some drugs stimulate the body’s immune system
7. Antiviral drug classification
1. Anti HIV
1. Anti-influenza Agents
2. Anti-herpes virus Agents
3. Anti-viral Agents for hepatic viral
infections
B. Antiretroviral Agents
A. Non-Retroviral Antiviral Agents
8. Antiviral drug classification
1. Nucleoside Reverse Transcriptase Inhibitors
(NRTI)
2. Non-nucleoside Reverse Transcriptase
Inhibitors (NNRTI)
3. Protease Inhibitors (PI)
4. Entry Inhibitors
5. Integrase Strand Transfer Inhibitors
1. Anti-influenza Agents
2. Anti-herpes virus Agents
3. Anti-viral Agents for hepatic viral
infections
B. Antiretroviral Agents
A. Non-Retroviral Antiviral Agents
9. Antiviral drug classification
Anti HIV
A. Anti-influenza Agents
B. Anti-herpesvirus Agents
C. Anti-hepatitis Agents
Antiretroviral Agents
Non-Retroviral Antiviral Agents
10.
11. - (found only in Flu A)
Influenza virus, which affects the respiratory tract, is one of the few RNA viruses that replicates in the nucleus of cells.
12. Steps of replication for influenza virus
https://openstax.org/books/microbiology/pages/6-2-the-viral-life-cycle
13. (transcription is the creation of RNA from DNA templet)
(translation is the creation of viral proteins by the m RNA in the ripozome
14. Anti-influenza Agents
Viral respiratory tract infections for
which treatments exist include those
of influenza A and B and respiratory
syncytial virus (RSV).
19. Amantadine & Rimantadine (Pharmacokinetics)
Both drugs are well absorbed orally.
Amantadine distributes throughout the body and readily
penetrates into the central nervous system (CNS), whereas
rimantadine does not cross the blood-brain barrier to the
same extent.
Amantadine is not extensively metabolized. It is excreted
into the urine and may accumulate to toxic levels in
patients with renal failure.
On the other hand, rimantadine is extensively
metabolized by the liver, and both the metabolites and the
parent drug are eliminated by the kidney
20. Amantadine & Rimantadine (Adverse effects)
Insomnia
dizziness
ataxia. More serious side eff ects have
been reported (for example
The drug should be employed
cautiously in patients with CNS
disorders , renal impairment, or
epilepsy.
Rimantadine causes fewer CNS
reactions, because it does not
efficiently cross the blood-brain
barrier.
Both drugs cause GI intolerance.
Amantadine and rimantadine should
be used with caution in pregnant and
nursing mothers, because they have
been found to be embryotoxic and
teratogenic in rats.
21.
22.
23.
24.
25.
26. Antiviral drugs classification
A. anti HIV
A. Anti-influenza Agents
B. Anti-herpes virus Agents
C. Anti-hepatitis Agents
Antiretroviral Agents
Non-Retroviral Antiviral Agents
27. The name is derived from Greek word herpein (to
creep or crawl), referring to latent, recurring infections.
herpes viruses infections - Google Search
Herpes viruses
30. (transcription is the creation of RNA from DNA templet)
(translation is the creation of viral proteins by the m RNA in the ribozom
Hepes virus replication
31. Anti-herpes virus Agents
1. Nucleoside Analogs
2. Non-Nucleoside Analogs
Anti-herpes virus Agents are classified to :
32.
33. Aciclovir is a Guanosine analogue that lacks a true sugar moiety
(containing an acyclic side chain in place of ribose).
34. Aciclovir, Ganciclovir & valganciclovir
Mechanism of action (MOA)
1. Acyclovir is activated
(monophosphorylated) by the viral
thymidine kinase (TK) enzyme to mono-
phosphate.
2. Host enzymes then convert the mono-
phosphate to di- and tri-phosphates
(which is false nucleotide).
3. The false nucleotide will be incorporated
into the viral DNA, causing premature
DNA-chain termination.
4. inhibits viral DNA polymerase activity by
inhibiting DNA chain elongation due to lack
of 3’ –OH group.
Inhibit viral DNA synthesis: Chain termination
35.
36. Mechanism
of resistance
Altered of thymidine kinase
Deficient activity of thymidine kinase
Altered DNA/ mutation in polymerases
Reduction in drug phosphorelation
[Note: Cytomegalovirus (CMV) is resistant,
because it lacks a specific viral thymidine
kinase.
39. Ganciclovir & Valganciclovir
• Ganciclovir is an analog of acyclovir that has 8 to 20 times greater activity against CMV,
which is the only viral infection for which it is approved.
• Valganciclovir is the valyl ester of ganciclovir.
• Like valacyclovir, valganciclovir has high oral bioavailability, because rapid hydrolysis
(metabolism) in the intestine and liver after oral administration leads to high levels of
ganciclovir.
Ganciclovir & valganciclovir are the best agents for Cytomegalovirus (CMV)
treatment
44. Should not be used alone for chronic Hepatitis C (not effective)
45.
46. Because of its teratogenic effects in experimental animals, ribavirin is contraindicated
in pregnancy.
Effective birth control method must be taken to avoide pregnancy during therapy & for
6 months after completetion of treatment in both male and female patients.
(Didanosine (ddI)
47.
48.
49.
50. Lamivudine
This cytosine analog is an inhibitor of both hepatitis B virus (HBV) DNA polymerase and human
immunodeficiency virus (HIV) reverse transcriptase.
Telbivudine
Telbivudine can be used in the treatment of HBV. Telbivudine is not active against HIV or other viruses. The
drug is phosphorylated intracellularly to the triphosphate, which can either compete with endogenous thymidine
triphosphate for incorporation into DNA or else be incorporated into viral DNA, where it serves to terminate
further elongation
of the DNA chain.
Adefovir
Adefovir is used for hepatitis B virus (HBV), it is a nucleotide analog that is phosphorylated to adefovir
diphosphate , which is then incorporated into viral DNA. This leads to termination of further DNA
synthesis and prevents viral replication.
Entecavir
Entecavir is a guanosine analog approved for the treatment of HBV infections. Following intracellular
phosphorylation to
the triphosphate, it competes with the natural substrate, deoxyguanosine triphosphate, for viral reverse
transcriptase. Entecavir has been shown to be effective against lamivudine-resistant strains of
HBV. Liver inflammation and scarring are improved.