The document discusses the structure-activity relationships of various antipsychotic drugs. It begins by describing the dopamine receptor and how drugs like phenothiazines are able to bind to it. It then covers specific structural features of different drug classes that impact their potency and side effect profiles, including phenothiazines, butyrophenones, and atypical antipsychotics. Key structural attributes discussed are the presence of electron-withdrawing groups on phenothiazine rings, different side chains on phenothiazines and butyrophenones, and the chemical structures of atypical antipsychotics. The document concludes that while older structure-function concepts were important, current antipsychotics have diverse mechanisms of action involving
Med chem lecture on Anticholinergic drugs for B.Pharm level in Nepal
Content from Foye's Principle of medicinal chemistry, my own thoughts and some articles
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
Med chem lecture on Anticholinergic drugs for B.Pharm level in Nepal
Content from Foye's Principle of medicinal chemistry, my own thoughts and some articles
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
The presentation will give a brief summary of Barbiturates from the Medicinal chemistry point of view. the contents are not exact, so if there is any discrepancy in it please make corrections. thanks
Amjad Anwar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
MORPHINE AS A LEAD DRUG MOLECULE COMPOUNDShikha Popali
THE ADDICTED DRUG MORPHINE AN ALKALOID USED TO TREAT SOME DISEASE , HERE WE HAVE ATTEMPT ALL DATA ITS STURECTURE MECHANISM OF ACTION, SAR AND APPLICATIONS.
This powerpoint presentation will help to know about introduction of bioisosterism by Biotechnology point of view. Hope this powerpoint presentation will your reference.
The presentation will give a brief summary of Barbiturates from the Medicinal chemistry point of view. the contents are not exact, so if there is any discrepancy in it please make corrections. thanks
Amjad Anwar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
MORPHINE AS A LEAD DRUG MOLECULE COMPOUNDShikha Popali
THE ADDICTED DRUG MORPHINE AN ALKALOID USED TO TREAT SOME DISEASE , HERE WE HAVE ATTEMPT ALL DATA ITS STURECTURE MECHANISM OF ACTION, SAR AND APPLICATIONS.
This powerpoint presentation will help to know about introduction of bioisosterism by Biotechnology point of view. Hope this powerpoint presentation will your reference.
A QSAR is a mathematical relationship between a biological activity of a molecular system and its geometric and chemical characteristics.
QSAR attempts to find consistent relationship between biological activity and molecular properties, so that these “rules” can be used to evaluate the activity of new compounds.
Neuroleptic is an important class of antipsychotic drugs also termed as tranquilizer. It include two types of drug phenothiazine & thioxanthene. The following presentation contain detail structure activity relationship of the same.
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.
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.
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!
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
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
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
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.
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
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
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
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.
5. DOPAMINE RECEPTOR
Anionic site on receptor to
interact with the protonated
nitrogen of dopamine
A flat, hydrophobic area
that interacts with the
phenyl ring and hydrogen
bonding at specific areas
around the phenyl ring to
accommodate the ring
hydroxyls
A two carbon distance
between the anionic site and
the ring site
7. PHENOTHIAZINE BINDING TO D2 RECEPTOR
Protonatable nitrogen that can interact with the anionic
site on the receptor
A phenyl ring to interact with the flat hydrophobic area of
the receptor
The two carbon distance is attained through molecular
bending of the side chain, which contains a three carbon
bridge, toward one of the phenyl rings to approximate a
two carbon distance
Ring geometry is also important in the binding of
phenothiazines to their receptor
11. The most potent position for the electron withdrawing
group is C2 which may help bending the side chain N
through H bond to form dopamine-like conformation
The rank order of potency is position 2>3>4>1
Substitution at C1 has deleterious effect on antipsychotic
activity (which may interfere the bending as in 1) as does
(to a lesser extent) substitution at C4 which may interfere S
binding to receptor
Stronger electron withdrawers are more potent
More than one substitution on the ring system decreases
potency
Oxidizing the ring-sulfur to sulfoxide or sulfone reduces
potency
12. CH3
CH2 CH3
H3C CH3
H CH3 CH2 CH2 CH3 CH3 CH3 CH3 CF3 N CF3
O H O CH3 O C O C O C O S O Cl S O S S O S O O S O CF3
Least potent Most Potent
14. ALKYL SIDE CHAIN
CH3
Increasing or decreasing the
length from 3 carbons N
N CH3
decreases the potency. The
S
further from 3 the less
potent. Two carbon side
Fenethazine
chains increase H1
antagonism (Fenethazine)
Substitutions on the α
carbon decrease potency
CH3
N N
A methyl substituent on the
β carbon can increase or S CH3 CH3
decrease dopamine
antagonism (Trimeprazine) Trimeprazine
15. A methyl substituent on the
β carbon increases H1
antagonism. Substituents CH3
that are larger than methyl N N
decrease antihistaminic S
activity unless they are part
of a heterocycle Methdilazine
(Methdilazine)
Substituents on the γ carbon
decrease dopamine
antagonism but increase N N
anticholinergic activity.
S CH3
These would be expected to
produce less extrapyramidal
CH3
side effects. All the S
piperidines fit this category
Thioridazine
16. Bridging of position 3 of the
side chain to position 1 the
phenothiazine significantly
reduces neuroleptic activity
17. SUBSTITUENTS ON THE γ NITROGEN
There are three classes of phenothiazines based
on the nature of this substituent
1. N,N-Dimethyl (aliphatic)
2. Piperazine
3. Piperidine
18. Thioridazine
S
N S
Piperidine ring
α CH3
Low EPS risk β
Central antimuscarinic
QTc prolongation CH3
N
20. BASIC AMINO GROUP
Maximum neuroleptic potency is observed in
aminoalkylated phenothiazines having a tertiary
amino group.
In general, alkylation of the basic amino group with
groups larger than methyl decreases the
neuroleptic potency.
Quaternization of the terminal nitrogen result in
loss of activity due to inability of these polar
compounds to cross the BBB.
21. POTENCY COMPARISON
Potency at the D2 receptors:
Given equal C2 substituents, ranked from most
potent to least potent - Piperazine > Aliphatic >
Piperidine
Of drugs on the market, however, the rank is -
Piperazine > Piperidine > Aliphatic
Anticholinergic potency: Piperidine > Aliphatic >
Piperazine
22. α Receptor antagonism: Aliphatic > Piperidine >
Piperazine (This may be due to the fact that in
order to get a good antipsychotic effect (D2
antagonism) large doses must be given and so the
α receptor antagonism, although weak, is seen
more)
Extrapyramidal side effects: Piperazine > Aliphatic
> Piperidine (Low anticholinergic potency in the
presence of strong D2 block)
Sedation: Piperidine > Aliphatic > Piperazine
24. METABOLISM
S-oxidation to give sulfoxide derivative inactive.
Terminal N demethylation is still active
C7 hydroxylation inactive compound
Terminal N-oxidation N-oxide derivative is
inactive
28. History/Evolution of Butyrophenone
O
OC2 H5
CH 3 N Meperidine
O O
OC2 H5
N Propophenone
200 x Meperidine as an Analgesic
O
OC2 H5
N Butyrophenone
Analgesia s imilar to Meperidine
O Other activity similar to Chlorpromazine
F OH
N Haloperidol (Haldol)
O Prototype butyrophenone antipsychotic
10x Chlorpromazine
Cl
29. BUTYROPHENONE
R1
O Y
R2
N
X – electron donating group has
highest potency
X
Changing the length of the propyl chain
decreases potency
Replacing the keto oxygen with S, carbon, OH
decreases potency
Y – Replaced with N – Piperazine structure
31. O
F
N NH
N
O
Drope ridol (Inapsine)
Other
Butyrophenone F OH
N
antipsychotics O
CF3
Triflupe ridol
O
F H
N N NH
F
Pimozid e (Orap) "diphenylbu tylpiperidine"
similar to haloperidol, longer duration. Used for Tou rette's Syndrome.
33. Clozapine
7 member central ring
Moderate potency at DA
α1 and α2 adrenergic, 5-HT1A,
5-HT2A, 5-HT2C, M, H1
34. Quetiapine
Lack a substituent on the
aromatic ring
35. Other atypical Resperidone is benzisoxazole and
antipsychotics ziprasidone is the benzisothiazole
containing antipsychotic agents
H3C N
Risperidone is 5-HT2A/D2
F
N
N antagonist with relatively high
O
affinity at histamine H1 and
O N Risperidone adrenergic a1 and a2 receptors. It
Cl H
N has less extrapyramidal side
HCl O
effects
N
N
Ziprasidone is also 5-HT2A/C/D2
S
N Ziprasidone
antagonist with relatively high
affinity at histamine H1 and
adrenergic a1 and a2 receptors. It
can also activate 5-HT1A in brain
and partial D2 agonist activity
37. Aripiprazole
H
O N O
N
N
Cl
Aripiprazole
Cl
It is an arylpiperazine quinoline derivative with complex
pharmacology. Dopamine D2 and serotonin 5-HT1A & 5-
HT2A/C receptor inhibitions are believed to be involved in
its antischizophrenic therapy. It has high affinity partial
agonist effect to some D2 receptors depending on cell
type, which explain its low extrapyramidal side effects.
38. CURRENT CONCEPTS
Presently, antipsychotic agents include many different
chemical structures with a range of activities at different
neurotransmitter receptors (e.g., 5-HT2A antagonism, 5-
HT1A partial agonism).
As a result, structure-function relationships that were relied
upon in the past have become less important.
Instead, receptor-function relationships and functional
assays are more clinically relevant.
Aripiprazole represents a good example of how an
examination of the structure provides little insight into its
mechanism, which is based on dopamine partial agonism.