Malignant disease accounts for many deaths in industrialized countries. Cancer occurs when normal cells are transformed into abnormal cells through genetic alterations. Chemotherapy aims to palliate symptoms, induce remission, or cure cancer by destroying cancer cells. The document discusses the classification, mechanisms of action, indications, and side effects of various classes of anticancer drugs including alkylating agents, antimetabolites, and antibiotics. It also outlines the multi-phase process of clinical trials required to approve new anticancer drugs.
Definition
Anticancer, or antineoplastic, drugs are used to treat malignancies, or cancerous growths. Drug therapy may be used alone, or in combination with other treatments such as surgery or radiation therapy.
Purpose
Anticancer drugs are used to control the growth of cancerous cells. Cancer is commonly defined as the uncontrolled growth of cells, with loss of differentiation and commonly, with metastasis, spread of the cancer to other tissues and organs. Cancers are malignant growths. In contrast, benign growths remain encapsulated and grow within a well-defined area. Although benign tumors may be fatal if untreated, due to pressure on essential organs, as in the case of a benign brain tumor, surgery or radiation are the preferred methods of treating growths which have a well defined location. Drug therapy is used when the tumor has spread, or may spread, to all areas of the body.
Definition
Anticancer, or antineoplastic, drugs are used to treat malignancies, or cancerous growths. Drug therapy may be used alone, or in combination with other treatments such as surgery or radiation therapy.
Purpose
Anticancer drugs are used to control the growth of cancerous cells. Cancer is commonly defined as the uncontrolled growth of cells, with loss of differentiation and commonly, with metastasis, spread of the cancer to other tissues and organs. Cancers are malignant growths. In contrast, benign growths remain encapsulated and grow within a well-defined area. Although benign tumors may be fatal if untreated, due to pressure on essential organs, as in the case of a benign brain tumor, surgery or radiation are the preferred methods of treating growths which have a well defined location. Drug therapy is used when the tumor has spread, or may spread, to all areas of the body.
ANTI CANCER DRUGS[ANTI-NEOPLASTIC DRUGS] MEDICINAL CHEMISTRY BY P. RAVISANKAR.Dr. Ravi Sankar
what is cancer?, History,Malignent tumor, non-malignent tumor(benign tumor),Largest tumor ever removed, tumour growth kinitics, doubling tume, angiogenesis, causes of cancer, drugs, treatment of cancer, classification of anti-cancer agents, mechanism of actions,alkylating agents,anti metabolites, vinka alkaloids, best ways to reducing cancer.
BY P. RAVISANKAR
VIGNAN PHARMACY COLLEGE
VADLAMUDI
GUNTUR
ANDHRA PRADESH
INDIA.
Anti-Neoplastic agents(Anti-cancer drugs)-History-Mechanism of actions-Classifications,SAR,Synthesis and Uses.(Medicinal chemistry)
P.Ravisankar
Vignan Pharmacy College
Vadlamudi. Guntur-A.P. India.
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
It include introduction and history of penicillin, mechanism of action of penicillin, classification of penicillin, structural activity relationship of penicillin, adverse effects of penicillin and therapeutic uses of penicillin.
this presentation cover medicinal chemistry of penicillin.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
ANTI CANCER DRUGS[ANTI-NEOPLASTIC DRUGS] MEDICINAL CHEMISTRY BY P. RAVISANKAR.Dr. Ravi Sankar
what is cancer?, History,Malignent tumor, non-malignent tumor(benign tumor),Largest tumor ever removed, tumour growth kinitics, doubling tume, angiogenesis, causes of cancer, drugs, treatment of cancer, classification of anti-cancer agents, mechanism of actions,alkylating agents,anti metabolites, vinka alkaloids, best ways to reducing cancer.
BY P. RAVISANKAR
VIGNAN PHARMACY COLLEGE
VADLAMUDI
GUNTUR
ANDHRA PRADESH
INDIA.
Anti-Neoplastic agents(Anti-cancer drugs)-History-Mechanism of actions-Classifications,SAR,Synthesis and Uses.(Medicinal chemistry)
P.Ravisankar
Vignan Pharmacy College
Vadlamudi. Guntur-A.P. India.
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
It include introduction and history of penicillin, mechanism of action of penicillin, classification of penicillin, structural activity relationship of penicillin, adverse effects of penicillin and therapeutic uses of penicillin.
this presentation cover medicinal chemistry of penicillin.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
chaemoprevention of cancer using dietary phytochemicals awan867
dietary phytochemicals are natural ,non-nutritive ,secondary metabolites .they are mainly for defense system in plants ,also provide colour ,aroma, flavour .they also have anti mutagenic & anti carcinogenic properties . there are 900 phytochemicals but main phytochemicals like curcumin ,gingerol,ECGC, Capsacin and many more . various cell signalling molecules can act as a target for these phytochemicals .
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
263778731218 Abortion Clinic /Pills In Harare ,sisternakatoto
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Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
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!
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
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
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
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.
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
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
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ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
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
2. Overview
Introduction
Malignant disease accounts for a high proportion
of deaths in industrialised countries.
The treatment of anticancer drug is to give
palliation, induce remission and, if possible, cure.
3. Overview
Introduction
Cancer occurs after normal cells have been
transformed into neoplastic cells through alteration of
their genetic material and the abnormal expression of
certain genes. Neoplastic cells usually exhibit
chromosomal abnormalities and the loss of their
differentiated properties. These changes lead to
uncontrolled cell division and many result in the
invasion of previously unaffected organs, a process
called metastasis.
4. Advances in Cancer Chemotherapy
Treatment options of cancer:
Surgery: before 1955
Radiotherapy: 1955~1965
Chemotherapy: after 1965
Immunotherapy and Gene therapy
5. Advances in Cancer Chemotherapy
The treatment of a patient with cancer may
aim to:
give palliation, for example prompt relief of
unpleasant symptoms such as superior vena cava
obstruction from a mediastinal tumor
induce ‘remission’ so that all macroscopic and
microscopic features of the cancer disappear,
though disease is known to persist
cure, for which all the cells of the clone must be
destroyed.
6. Cancer Chemotherapy
Disease Name 5 Years Survival Rate
Childhood Acute Lymphoblastic Leukemia 50~80%
Adult Acute Lymphoblastic Leukemia 20~60%
Childhood Acute Myeloblastic Leukemia 20~60%
Adult Acute Myeloblastic Leukemia 10~20%
Breast Cancer(Premenopausal) 10~20%
Breast Cancer(Postmenopausal) 0~15%
Hodgkin’ s lymphoma * 40~80%
7. Cancer Chemotherapy
Disease Name 5 Years Survival Rate
Small Cell Lung Cancer (Limited Stage) 10~20%
(Extensive Stage) 0~5%
Non-Hodgkin’ s lymphoma * 40~65%
Ovarian Cancer 40~60%
Children Solid Tumor(Nephroblastoma, Rhabdomyosarcoma、
Lymphoma,Osteosarcoma)* 60~90%
Trophoblastoma (Chorion Epithelioma)** 80~90%
Seminoma of Testis** 60~90%
Embryonic Carcinoma of Testis 60~80%
Note:* Combination with other therapeutics
**Chemotherapy Level of our country is high
8. The Classification of
Anticancer Drugs
According to chemical structure and
resource of the drug;
According to biochemistry mechanisms of
anticancer action;
According to the cycle or phase
specificity of the drug
9. The Classification of
Anticancer Drugs
According to chemical structure and
resource of the drug:
Alkylating Agents, Antimetabolite,
Antibiotics, Plant Extracts,Hormones,
Others
10. The Classification of
Anticancer Drugs
According to biochemistry mechanisms of
anticancer action:
Block nucleic acid biosynthesis
Direct influence the structure and function of
DNA
Interfere transcription and block RNA synthesis
Interfere protein synthesis and function
Influence hormone homeostasis
Others
11. The Classification of
Anticancer Drugs
According to the cycle or phase
specificity of the drug:
cell cycle nonspecific agents (CCNSA)
cell cycle specific agents (CCSA)
12. The Basic Concept of
Cell Generation Cycle
The cycle of cell replication includes:
M(Mitosis)phase
G1(Gap1, period before S)phase
S(DNA synthesis)phase
G2(Gap2,period after S)phase
Growth Fraction (GF)
13.
14. Growth Fraction (GF)
GF=
Proliferating cell group
Total tumor cell group
CCNSA:drugs that are active
throughout the cell cycle.
CCSA: drugs that act during a specific
phase of the cell cycle.
15. Cell cycle specific agents and Cell cycle
Non-specific agents
Cell Cycle Nonspecific Agents (CCNSA)
drugs that are active throughout the cell
cycle
Alkylating Agents
Platinum Compounds
Antibiotics
16. Cell cycle specific agents and Cell cycle
Non-specific agents
Cell Cycle Specific Agents (CCSA)
drugs that act during a specific phase of
the cell cycle
S Phase Specific Drug:
Aantimetabolites, Topoisomerase Inhabitors
M Phase Specific Drug:
Vinca Alkaloids, Taxanes
G2 Phase Specific Drug:
Bbleomycin
17. Mechanism of Anticancer Drugs
Block nucleic acid (DNA, RNA) biosynthesis
Directly destroy DNA and inhibit DNA
reproduction
Interfere transcription and block RNA synthesis
Interfere protein synthesis and function
Influence hormone homeostasis
19. Interfere Protein Synthesis
Antitubulin: vinca alkaloids and taxanes;
Interfere the function of ribosome:
harringtonines;
Influence amino acid supply: L-asparaginase
Bind tubulin, destroy spindle to produce
mitotic arrest.
21. Influence the Structure and
Function of DNA
Alkylating Agent: mechlorethamine,
cyclophosphamide and thiotepa
Platinum: cis-platinium
Antibiotic: bleomycin and mitomycin C
Topoismerase inhibitor: camptothecine and
podophyllotoxin
22. Influence Hormone Homeostasis
These drugs bind to hormone receptors to block
the actions of the sex hormones which results in
inhibition of tumor growth.
Estrogens and estrogen antagonistic drug
Androgens and androgen antagonistic drug
Progestogen drug
Glucocorticoid drug
gonadotropin-releasing hormone inhibitor:
leuprolide, goserelin
aromatase inhibitor: aminoglutethimide,
anastrazole
24. The Main Step of Anticancer
Drug Research
Non-clinical Research:
1.Anticancer Drug Screen:
in vitro:tumor cell culture, tumor
inhibitor/kill test
in vivo:animal xenograft model e.g.Ehrlich
ascites tumor, S180 lymphosarcoma
2. Pharmacodynamics, pharmacokinetics and
toxicology test
25. The Main Step of Anticancer
Drug Research
Clinical Research:
Phase 1 clinical trial
Phase 2 clinical trial
Phase 3 clinical trial
Phase 4 clinical trial
26. The Main Step of Anticancer
Drug Research
Phase 1 clinical trial
In Phase 1 clinical trials, researchers test a new
drug or treatment in a small group of people
(20-80) for the first time to evaluate its
safety, determine a safe dosage range, and
identify side effects.
• TOLERANCE
• PHARMACOKINETICS
27. The Main Step of Anticancer
Drug Research
Phase 2 clinical trial
In Phase 2 clinical trials, the study drug or
treatment is given to a larger group of people
(40-100) to see if it is effective and to further
evaluate its safety.
28. The Main Step of Anticancer
Drug Research
Phase 3 clinical trial
In Phase 3 studies, the study drug or treatment
is given to large groups of people (more than 200)
to further determine its effectiveness, monitor
side effects, compare it to commonly used
treatments, and collect information that will
allow the drug or treatment to be used safely.
29. The Main Step of Anticancer
Drug Research
Phase 4 clinical trial
Phase 4 studies are done after the drug or
treatment has been marketed. These studies
continue testing the study drug or treatment to
collect information about their effect in various
populations and any side effects associated with
long-term use.
31. Alkylating Agents
One of the frightening developments of World
War I was the introduction of chemical warfare.
These compounds were known as the nitrogen
mustard gases. The nitrogen mustards were
observed to inhibit cell growth, especially of
bone marrow. Shortly after the war, these
compounds were investigated and shown to inhibit
the growth of cancer cells.
32. Alkylating Agents
Mechanism of Action
Nitrogen mustards inhibit cell reproduction by
binding irreversibly with the nucleic acids (DNA).
The specific type of chemical bonding involved is
alkylation. After alkylation, DNA is unable to
replicate and therefore can no longer synthesize
proteins and other essential cell metabolites.
Consequently, cell reproduction is inhibited and
the cell eventually dies from the inability to
maintain its metabolic functions.
33. Classification of Alkylating Agents
Bis Chloroethyl Amines:
Cyclophosphamide, Chlormethine,
Chlorambucil, Sarcolysine
Nithrosoureas:
Carmustine,Lomustine
Ethyeneammonium or Aziridines:
Thiotepa,triethylene melamine
Alkysulfonates:Busulfan
34. Resistance of Alkylating Agents
Resistance to alkylating agents has several
causes:
Membrane transport may be decreased.
The drug may be bound by glutathione (GSH)
via GSH-S-transferase or metallothioneins
in the cytoplasm and inactivated.
The drug may be metabolized to inactive
species.
35. Adverse Effects of Alkylating Agents
Myelosuppression is the dose-limiting
adverse effect for alkylating agents.
Nausea and vomiting are common as are
teratogenesis and gonadal atrophy,
although in the latter cases these are
variable, according to the drug, its
schedule, and route of administration.
Treatment also carries a major risk of
leukemogenesis and carcinogenesis.
36. Alkylating Agents——Mustine
Mustine must be injected intravenously
because it is highly reactive. It
disappears very rapidly from the blood,
the activity of Mustine lasts only a few
minutes.
The main indication for Mustine is in
treatment of Hodgkins disease and
lymphomas, but it may also be useful in
other malignancies.
37. Alkylating Agents——
Cyclophosphamide
Cyclophosphamide can also be given orally.
Indications:
It is used in the treatment of chronic lymphocyctic
leukemia, non-Hodgkin’s lymphomas, breast and
ovarian cancer, and a variety of other cancers.
It is also a potent immunosuppressant, it is used in
the management of rheumatoid disorders and
autoimmune nephritis.
Adverse Effects:
Alopecia, nausea, vomiting, myelosuppression, and
hemorrhagic cystitis.
38. Alkylating Agents——Nitrosoureas
Carmustine, Lomustine, Semustine
Pharmacokinetics:
Nitrosoureas are highly lipophilic and
reach cerebrospinal fluid concentrations
that are about 30% of plasma
concentrations.
Indications:
Because of their excellent CNS
penetration, carmustine and lomustine
have been used to treat brain tumors.
39. Alkylating Agents——
Phenylalanine Nitrogen Mustard
Melphalan is a nitrogen mustard that is
primarily used to treat multiple myeloma
(plasma cell myeloma), breast cancer, and
ovarian cancer.
40. Alkylating Agents——
Alkysulfonates
Busulfan [Myleran]
Indications:
Busulfan is administered orally to treat chroic
granulocytic leukemia and other
myeloproliferative disorders.
Adverse Effects:
Busulfan produces advers effects related to
myelosuppression. It only occasionally produces
nausea and vomitting. In high doses, it produces
a rare but sometimes fatal pulmonary
fibrosis, ”busulfan lung”.
41. Alkylating Agents——Thiotepa
Thiotepa is converted rapidly by liver
mixed-function oxidases to its active
metabolite triethylenephosphoramide
(TEPA); it is active in bladder cancer.
42. Antimetabolites
General Characteristics:
Antimetabolites are S phase-specific
drugs that are structural analogues of
essential metabolites and that interfere
with DNA synthesis.
Myelosuppression is the dose-limiting
toxicity for all drugs in this class.
44. Antimetabolites——
Folic Acid Antagonist
Methotrexate (MTX)
Mechanism of Action:
The structures of MTX and folic acid are
similar. MTX is actively transported into
mammalian cells and inhibits dihydrofolate
reductase, the enzyme that normally converts
dietary folate to the tetrahydrofolate form
required for thymidine and purine synthesis.
45. Antimetabolites——
Folic Acid Antagonist
Methotrexate (MTX)
Indications:
The use of MTX in the treatment of
choriocarinoma, a trophoblastic tumor, was the
first demonstration of curative chemotherapy.
It is especially effective for treating acute
lymphocytic leukemia and for treating the
meningeal metastases of a wide range of tumors.
46. Antimetabolites——
Folic Acid Antagonist
Methotrexate (MTX)
Adverse Effects:
MTX is myelosuppressive, producing severe
leukopenia, bone marrow aplasia, and
thrombocytopenia.
This agent may produce severe gastrointestinal
disturbances.
Renal toxicity may occur because of precipitation
(crystalluria) of the 7-OH metabolite of MTX.
47. Antimetabolites——
Purine Antagonists
6-Mercapapurine(6-MP)
The drugs are believed to act similarly to inhibit
purine base synthesis, although their exact
mechanisms of action are still uncertain.
Indications:
Mercaptopurine is used primarily for the maintenance
of remission in patients with acute lymphocytic
leukemia and is given in combination with MTX for
this purpose.
Adverse Effects:
Well tolerate.
Myelosuppression is generally mild with
thioguanine.Long-term mercaptopurine use may cause
hepatotoxicity.
48. Antimetabolites——
Pyrimidine Antagonists
5-Fluorouracil (5-FU)
Mechanism of Action:
Fluorouracil is an analogue of thymine in which the
methyl group is replaced by a fluorine atom. It has
two active metabolites: 5-FdUMP and 5-FdUTP. 5-
FdUMP inhibits thymidylate synthetases and prevents
the synthesis of thymidine, a major building block of
DNA. 5-FdUTP is incorporated into RNA by RNA
polymerase and interferes with RNA function.
50. Antimetabolites——
Pyrimidine Antagonists
5-Fluorouracil (5-FU)
Adverse Effects:
Fluorouracil may cause nausea and vomiting,
myelosuppression, and oral and gastrointestinal
ulceration. Nausea and vomitting are usually mild.
With fluorouracil, myelosuppression is more
problematic after bolus injections, whereas
mucosal damage is dose-limiting with continuous
infusions.
51. Antimetabolites——
Pyrimidine Antagonists
Cytarabine
Indications:
Cytarabine has a narrow clinical spectrum and is
primarily used in combination with daunorubicin or
thioguanine for the treatment of acute
nonlymphocytic leukemia.
Adverse Effects:
High doses of cytarabine can damage the liver,
heart, and other organs.
53. Antibiotics
Adriamycin and Daunorubicin:
Properties:
Adriamycin and Daunorubicin are tetracycline rings
with the sugar daunosamine. They are DNA
intercalating agents that block the synthesis of DNA
and RNA.
These agents are primarily toxic during the S phase
of cell cycle.
These agents imparts a red tinge to the urine.
Adramycin is used to treat acute leukemias, lymphoma,
and a number of solid tumors.
54. Antibiotics
Mitomycin C:
Mechanism:
Mitomycin C is an antineoplastic antibiotic that
alkylates DNA and thereby causes strand
breakage and inhibition of DNA synthesis.
Indications:
It is primarily used in combination with
vinvristine as salvage therapy for breast cancer.
Adverse Effects:
Mitomycin produces delays and prolonged
myelosuppression that preferentially affects
platelets and leukocytes.
55. Antibiotics
Actinomycin D:
Actinomycin D intercalates DNA and thereby
prevents DNA transcription and messenger RNA
synthesis.
The drug is given intravenously, and its clinical
use is limited to the treatment of trophoblastic
(gestational) tumors and the treatment of
pediatric tumors, such as Wilms’ tumor and
Ewing’s sarcoma.
56. Antibiotics
Bleomycin:
Mechanism:
The drug has its greatest effect on neoplastic
cell in the G2 phase of the cell replication
cycle.Although bleomycin intercalates DNA, the
major cytotoxicity is believed to result from
ironcatalyzed free radical formation and DNA
strand breakage.
Indications:
It is useful in Hodgkin’s and non-Hodgkin’s
lymphomas, testicular cancer, and several other
solid tumors.
Adverse Effects:
Bleomycin produces very little myelosuppression.
The most serious toxicities of Bleomycin are
pulmonary and mucocutaneous reactions.
57. Anti-Cancer Plant Allaloids
Tubulin-Binding Agents
Vinca Alkaloids: The cellular mechanism of
action of vinca alkaloids is the prevention of
microtubule assembly, causing cells to arrest
in the late G2 phase by preventing formation
of mitotic filaments for nuclear and cell
division.
58. Anti-Cancer Plant Allaloids
Tubulin-Binding Agents
Vinca alkaloids:
Vinblastine,vincristin, vindesine and vinorelbine are all
alkaloids derived from the periwinkle plant (Vinca rosea).
Indications:
Vinblastine is used in combination with Bleomycin
and Cisplatin for metastatic testicular tumors.
Vincristine is used in combination with prednisone
to induce remission in childhood leukemia.
Vinorelbine is used to treat non-small-cell lung
cancer and breast cancer.
59. Anti-Cancer Plant Allaloids
Tubulin-Binding Agents
Paclitaxel:
Taxanes enhance all aspects of tubulin
polymerization, an action that is the opposite to
that of vinca alkaloids, but they are also
cytotoxic, emphasizing the dynamic importance of
tubulin polymerization as a target for cytotoxic
drugs.
Paclitaxel, Taxotere
60. Interfere the Function of Ribosome:
Cephalotaxus Alkaloids :
Harringtonine
Homoharringtonine
Anti-Cancer Plant Allaloids
61. Platinum Compound
Cisplatin:
Mechanism of Action:
Cisplatin binds to guanine in DNA and
RNA, and the interaction is stabilized by
hydrogen bonding. The molecular
mechanism of action is unwinding and
shortening of the DNA helix.
62. Platinum Compound
Cisplatin:
Indications:
Cisplatin has efficacy against a wide range of
neoplasms. It is given intravenously as a first-
line drug for testicular, ovarian, and bladder
cancer, and it is also useful in the treatment of
melanoma and a number of other soild tumors.
Adverse Effect:
Cisplatin produces relatively little
myelosuppression but can cause severe nausea,
vomiting, and nephrotoxicity.
64. Hormones
Several types of hormone-dependent cancer
(especially breast, prostate, and endometrial
cancer) respond to treatment with their
corresponding hormone antagonists.
Estrogen antagonists are primarily used in the
treatment of breast cancer, whereas androgen
antagonists are used in the treatment of
prostate cancer. Corticosteroids are particularly
useful in treating lymphocytic leukemias and
lymphomas.
65. Hormones
Estrogens:
Estrogens inhibit the effects of endogenous
androgens and androgen-dependent metastatic
prostatic carcinoma. Diethylstilbestrol is usually
the agent of choice.
Cardiac and cerebrovascular complications and
carcinoma of the male breast are potential
adverse effects.
66. Hormones
Progenstins:
Progestins are useful in the management of
endometrial carcinoma and back-up therapy for
metastatic hormone-dependent breast cancer.
67. Hormones
Antiestrogen: Tamoxifen
Tamoxifen is the drug of choice in
postmenopausal women with or recovering from
metastatic breast cancer. It is most effective in
patients who have estrogen receptor-positive
tumors.
Tamoxifen is also used as adjunvctive therapy to
oophorectomy to leuprolide or goserelin in
premenopausal women with estrogen receptor-
positive tumors.
68. Hormones
Androgens:
Androgen activity in breast cancer is similar to
that of estrogens, perhaps for the same
mechanistic reasons.
Virilizing effects and hepatic toxicity make them
unacceptable to most patients.
Fluoxymesterone is the most widely used agent.
Danazol has use in hematology in aplastic anemia
and congenital anemias.
69. Hormones
Glucocorticoids:
They are integral components of curative therapy
for acute lymphoblastic leukemia, non-Hodgkin’s
lymphoma, and Hodgkin’s disease.
Glucocorticoids have essential roles in the
prevention of allergic reaction, emesis control,
relief of intracranial hypertension or spinal cord
compression in neurologic complications, and pain
relief.
71. Drug Resistance
De novo Resistance
Acquired Resistance
Multidrug Resistance (MDR)
72. Drug Resistance
De novo resistance:
De novo resistance can be de novo genetic (i.e.
the cells are initially inherently resistant), or can
arise because drugs are unable to reach the
target cells because of permeability barriers
such as the blood-brain barrier.
73. Drug Resistance
Acquired Resistance:
Acquired drug resistance may result from
genomic mutations, such as the induction or
deletion of enzymes involved in drug inactivation
or drug activation, respectively.
74. Drug Resistance
Multidrug Resistance (MDR):
P-glycoprotein transports many naturally
occurring drugs out of neoplastic cells, and its
induction may lead to multidrug resistance.
As scientific understanding of the mechanisms of
drug resistance increases, new treatments may
be developed to counteract resistance.
75. Drug Toxicity
The most common toxicities of antineoplastic
drugs result from inhibition of cell replication in
the bone marrow, gastrointestinal epithelium, and
hair follicles. Many antineoplastic drugs also
stimulate the chemoreceptor trigger zone in the
medulla and thereby elicit nausea and vomiting.
76. Immunomodulating Drugs
Immunosuppressive Agents:
Act to suppress immune mechanisms and are used
to treat autoimmune diseases or to prevent graft
rejection following tissue transplantation.
Ciclosporin, Tacrolimus, adrenocortical hormones,
antimetabolites, alkylating agent, antilymphocyte
globulin, Mycophenolate Mofetil