This document summarizes various in vivo and in vitro screening methods used to evaluate potential antiulcer drugs. Some key in vivo methods include pylorus ligation in rats, which induces gastric ulcers, and stress ulcer models like restraint-induced ulcers and cold water immersion-induced ulcers. Important in vitro assays are the [125I] gastrin binding assay to evaluate gastrin receptor antagonism, the tiotidine binding assay, and the H+/K+-ATPase inhibition assay to measure inhibition of acid secretion. These screening methods allow evaluation of antiulcer drug candidates and determination of their mechanisms of action, such as antisecretory or cytoprotective effects.
In this slide contains diabetics, classification, symptoms, complication, invivo and invitro screening models of anti diabetics.
Presented by: GEETHANJALI ADAPALA (Department of pharmacology).
RIPER, anantapur
Introduction to Screening Models Of Anti Cancer Drugs
Need for novel anti cancer drugs, In - vitro methods, In - vivo methods, Advantages and disadvantages
Presented by
T. Niranjan Reddy
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Assignment on Preclinical Screening of ImmunomodulatorsDeepak Kumar
Assignment on Preclinical screening of new substances for the pharmacological activity using in vivo, in vitro, and other possible animal alternative models
Extrapolation of in vitro data to preclinical and.pptxARSHIKHANAM4
Extrapolation of in vitro data to preclinical.
the topic is included in m.pharmacy 1st sem syllabus. which is essential for the study and that include the details about how you deal with the preclinical data that will help to decide the NOEAL and LOEAL, the humane dose of the drug can be calculated and further formation is also done.
Preclinical Screening of Antiasthmatic DrugsShubham Kolge
Bronchial asthma is characterized by both bronchoconstriction and airway inflammation which leads to bronchial hyperresponsiveness to various stimuli. Different mediators are implicated in asthma. As the precise etiology is not known and multiple biochemical processes are triggered by different causative factors, it is difficult to have a single drug which can effectively and simultaneously act upon different mediators. This led to an intense search for potent and safe antiasthmatic drugs. This presentation intends to compile different screening methods for the evaluation of new candidate drugs with potential for the treatment of asthma. These include in vitro, in vivo, receptor binding and enzymatic methods.
Screening methods of immunomodulators by shivam diwakerShivam Diwaker
Immune Modulators are the substances or drugs or chemical compounds that are used for the modification in the Immune system such as stimulate and suppress.
Introduction to Screening Models of Anti-Atherosclerosis
Atherosclerosis, Screening models, In vitro models, In vivo models
Presented by
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Department of Pharmacology
This power point presentation include the definition of the peptic ulcer, formation of peptic ulcer, regulation of gastric acid secreation, sign and symptomes, etiology of chronic ulceration, acid- pepsin vs mucosal resistance, gastric hyper secreation, disease complication, infection and obstruction, different factors related to acid secreation, classification of drugs used in peptic ulcer animal models in experimental peptic ulcer in both in-vivo and in- vitro
In this slide contains diabetics, classification, symptoms, complication, invivo and invitro screening models of anti diabetics.
Presented by: GEETHANJALI ADAPALA (Department of pharmacology).
RIPER, anantapur
Introduction to Screening Models Of Anti Cancer Drugs
Need for novel anti cancer drugs, In - vitro methods, In - vivo methods, Advantages and disadvantages
Presented by
T. Niranjan Reddy
Department of Pharmacology
Assignment on Preclinical Screening of ImmunomodulatorsDeepak Kumar
Assignment on Preclinical screening of new substances for the pharmacological activity using in vivo, in vitro, and other possible animal alternative models
Extrapolation of in vitro data to preclinical and.pptxARSHIKHANAM4
Extrapolation of in vitro data to preclinical.
the topic is included in m.pharmacy 1st sem syllabus. which is essential for the study and that include the details about how you deal with the preclinical data that will help to decide the NOEAL and LOEAL, the humane dose of the drug can be calculated and further formation is also done.
Preclinical Screening of Antiasthmatic DrugsShubham Kolge
Bronchial asthma is characterized by both bronchoconstriction and airway inflammation which leads to bronchial hyperresponsiveness to various stimuli. Different mediators are implicated in asthma. As the precise etiology is not known and multiple biochemical processes are triggered by different causative factors, it is difficult to have a single drug which can effectively and simultaneously act upon different mediators. This led to an intense search for potent and safe antiasthmatic drugs. This presentation intends to compile different screening methods for the evaluation of new candidate drugs with potential for the treatment of asthma. These include in vitro, in vivo, receptor binding and enzymatic methods.
Screening methods of immunomodulators by shivam diwakerShivam Diwaker
Immune Modulators are the substances or drugs or chemical compounds that are used for the modification in the Immune system such as stimulate and suppress.
Introduction to Screening Models of Anti-Atherosclerosis
Atherosclerosis, Screening models, In vitro models, In vivo models
Presented by
SHAIK FIRDOUS BANU
Department of Pharmacology
This power point presentation include the definition of the peptic ulcer, formation of peptic ulcer, regulation of gastric acid secreation, sign and symptomes, etiology of chronic ulceration, acid- pepsin vs mucosal resistance, gastric hyper secreation, disease complication, infection and obstruction, different factors related to acid secreation, classification of drugs used in peptic ulcer animal models in experimental peptic ulcer in both in-vivo and in- vitro
A Brief Introduction to Ulcers: What are ulcers, its causes, and symptoms. Classification of Antiulcer drugs and their adverse effects.
List of all the screening models available for Antiulcer drugs.
Few of the models are explained with their Principle, procedures, Evaluation, and assessment.
Screening models for evaluation of anti ulcer activitySIVASWAROOP YARASI
A sore that develops on the lining of the oesophagus, stomach or small intestine.
Ulcers occur when stomach acid damages the lining of the digestive tract. Common causes include the bacteria H. Pylori and anti-inflammatory pain relievers including aspirin.
Upper abdominal pain is a common symptom.
Treatment usually includes medication to decrease stomach acid production. If it is caused by bacteria, antibiotics may be required.
Screening method of peptic ulcer disease.pptxTUSHARUNDHAD3
Screening method of peptic ulcer disease.pptx
1.Introduction
2.Causes
3.Symptoms
4.Classification of antiulcer drugs
Screening model
(A) In vitro model
(B) In vivo model
A. IN VITRO MODEL
1. H+/K+ ATPase inhibition assay
2. Tiotidine binding assay
3. Gastrin binding assay
B. In Vivo model
1. Pylorus ligation in rats
2. NSAIDs induced gastric ulcer
3. Ethanol induced gastric ulcer in rats
4. Histamine induced gastric ulcer
5. Acetic acid induced gastric ulcer
6. Cysteamine induced duodenal ulcer
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Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
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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
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ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
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.
3. INTRODUCTION
• Peptic ulcer is one of the most prevalent chronic gastrointestinal
disorder.
• It is a sore that develops on the lining of the stomach or small
intestine.
• More common in middle- age to older age
• Site : duodenum/ stomach, in a ratio of about 4:1
• Male/ Female ratio is 3:1
9. PYLORUS LIGATION IN RATS
• PRINCIPLE:
Pyloric ligation in rats leads to accumulation of gastric acid in the
stomach leading to acute gastric ulceration.
• REQUIREMENTS:
Albino Wistar Rats (150-200g)
Drugs: Ether (Anesthetic)
Saline (control)
Omeprazole (standard) / Test drug
11. PROCEDURE
Albino Wistar Rat (150-200gm) is taken
Rats are divided into two groups
Control Group Test Group
Both Groups being fasted for 24h before ligation
Vehicle is administered Test drug is administered
Once for 2days and 30minutes before ligation
12. Both group rats are anesthetized with ether
Pyloric ligation procedure done
19 hrs after pyloric ligation,
animals sacrificed by decapitation
Abdomen opened and stomach dissected out
Contents of the stomach collected
Stomach opened along greater curvature
Ulcers observed under 10x magnification
13. Cont…
• Ulcer severity is graded as:
0- normal stomach 1- superficial ulcder 2- deep ulcer 3- penetrated
or perforated ulcer
• The Ulcer Index (U1 )is calculated by the following equation:
U1 = UN +US +UP X 10-1
Where UN = Average no. of Ulcers/animal
US = Average of Severity scores
UP = Percentage of animals with ulcers
14.
15. Cont…
Contents of the stomach analyzed for :-
• Volume
• pH : pH of it is noted with pH meter
• Free acidity & total acidity
• Mucin & prostaglandin levels can be estimated to detect
cytoprotective effects.
INFERENCE:
• Ulcer index of test drug compared with control group to detect
anti- ulcer effect of test drug.
16. Cont.…
• Other parameters help to infer the mechanism of ulcer protection.
e.g. Decrease in vol of gastric acid: antisecretory action
Rise in pH : acid neutralising action
Increase in mucin, PGs : cytoprotective effect
17. NSAIDs INDUCED GASTRIC LESIONS
• Gastric ulceration is produced in rats by certain drugs i.e NSAIDs like
Aspirin, Indomethacin, Ibuprofen.
• The ability of the test drug to protect against the ulceration is observed.
• PRINCIPLE:-
Inhibition of endogenous prostaglandin production and consequent loss of
gastric mucosal defence.
• Important model for identifying drugs that could be effective in NSAID
induced gastropathy
18. Procedure
Wistar Rats (150-200g)
Rats are divided into two groups
Control group Test group
Both Groups being fasted for 24-36 h before ligation
Vehicle administered Test agent (1% carboxymethyl cellulose)
via gastric intubation.
19. Cont…
Administration of Ulcerogenic i.e. NSAIDs
intraperitoneally.
Placing the rats in cages and immersed in water upto the level
of xiphoid process at 23 C for 7h.
Animals are sacrificed
Stomach removed and evaluated for Ulcer Index
20. Stress Ulcer Models
• Stress plays a significant role in the pathogenesis of gastric ulcers in human
being.
• The involvement of psychogenic factors and the ease of production of
gastric ulcers using these models is a real advantage over the pyloric
ligation method of gastric ulcer production.
• 2 type of Stress Ulcer Model
Restraint Induced Ulcers
Cold Water Immersion-Induced Ulcers
21. Procedure Of Restraint induced ulcers
Albino Rat (either sex of 150-200g)
Animals are fasted for 36 h and divided into 2 groups:
Test Group Control Group
Test agent administered saline administered
Both limbs of the rats are tied in pair so that they cannot move
22. Cont…
Animals are subjected to restraint by molding
galvanized steel window around rats
Animal kept under restraint for 24h
Animals are sacrificed and stomach are
dissected out.
Stomach opened along greater curvature
Ulcer index, Ulcer severity & gastric content of the test group is determined
and compared with control group.
23. Cold Water Immersion Induced Ulcers
Wistar rats (150-200g)
Fasting the animal for 16h
Test compound is administered orally to test group
Saline is administered to Control group
Animals are placed individually in restraint
cages vertically and then immersed in water
at 22 C for 1h
Rats are removed from restraint
Evan’s blue injected IV via tail vein
v
24. Cont…
10min Later, Animals are sacrificed
Stomach is removed and filled with formol saline & kept overnight
Next day, stomach is opened along greater curvature, washed in warm water
examined for ulcerative lesions and compared with control group
26. [125I] Gastrin Binding Assay
• PRINCIPLE:
Gastrin (G cells of gastric antrum)
1. Binds to (Cholecystokinin) CCK2 receptors on parietal cells, release HCl
2. Binds to CCK2 receptors on ECL cells Histamine act on H2
receptors of parietal cells release HCl
• Compounds with gastrin receptor antagonistic activity can be potential
antiulcer agent
27. Procedure
• Fundic gland suspension is obtained from Guinea Pig stomach.
The gland suspension is incubated with
50µ𝑙 of [125I] Gastrin Unlabeled Gastrin In the presence of
in the presence of buffer for non specific test compound
(for total binding) binding
for 90 minutes at 37 C
• In microcentrifuge tube, ice cold buffer+ incubated mixture is taken and
centrifuged for 5min at 10,000g
• Radioactivity is quantified in pellet after discarding the supernatant.
28. Evaluation
• Total binding, non- specific binding & specific binding are determined
• Percentage of specifically bound [125I]Gastrin displaced by a given
concentration of the test compound calculated.
• The higher the displaced [125I] Gastrin, more is the gastrin antagonistic
activity of test compound.
29. H⁺ / K⁺- ATPase Inhibition Assay
• H⁺/K⁺ - ATPase or proton pump is the final step in the synthesis of acid by
parietal cells.
• Procedure:
Microsomal gastric H⁺/K⁺ - ATPase obtained from pig gastric mucosa
Incubated with buffer, ATP and Test compound
After 30min.of incubation, Add malachite green to stop the reaction
30. Cont…
After 10 seconds, Add 15% sodium citrate for 45min
Release of orthophosphate from ATP is quantified by calorimeter
EVALUATION:-
• Percentage inhibition of H⁺/K⁺ - ATPase is calculated
• Lesser the orthophosphate release, more is the inhibition of H⁺/K⁺ - ATPase
by test compound
31. REFERENCES
• K.D Tripathi, Drugs for Peptic Ulcer: Essentials of Medical
Pharmacology.2014; Eight edition: 647-649.
• SK Gupta et al, Screening Of Antiulcer Agents: Drug screening
methods.2016;3rd edition: 527-539.
• https://www.google.com/url?sa=i&url=https%3A%2F%2Fwww.resear
chgate.net%2Ffigure%2FThe-cold-restraint-stress-induced-acute-
gastric-injury-model-in-mice-A-A-
simple_fig9_300001236&psig=AOvVaw0qbWy3GY3fn69_5DS-
ddsH&ust=1703859165928000&source=images&cd=vfe&opi=899784
49&ved=0CBQQjhxqFwoTCJD0rPbMsoMDFQAAAAAdAAAAABAD
