Presented by Dhanashree Kavhale. M. Pharm.(Pharmaceutical Chemistry) 1st year.
Various organic named reactions are there in Advanced Organic Chemistry I, as some of them are explained along with their mechanism.
Presented by Dhanashree Kavhale. M. Pharm.(Pharmaceutical Chemistry) 1st year.
Various organic named reactions are there in Advanced Organic Chemistry I, as some of them are explained along with their mechanism.
HERE PRESENTATING VITAMINS AS PER SYLLABUS OF MPHARM SUBJECT NATURAL PRODUCTS INCLUDING VITAMIN B2, B12, B3, ITS STRUCTURE ISOLATED FROM CONTENTS AND COMPLETE DETAIL ON IT IN A EASY WAY , THE MOST ASKED VITAMINS.
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
Synthetic reagent and applications OF ALUMINIUM ISOPROPOXIDEShikha Popali
SYNTHETIC REAGENTS AND APPLICATIONS OF ALUMINIUM ISOPROPOXIDE ITS ALTERNATIVE NAMES AND ITS PHYSICAL PROPERTIRS , HANDLING, STORAGE, PRECAUTIONS, PREPARATIONS, SYNTHETIC APPLICATIONS
Analog design is usually defined as the modification of a drug molecule or of any bioactive compound in order to prepare a new molecule showing chemical and biological similarity with the original model compound
There are many ways that drug-resistant infections can be prevented: immunization, safe food preparation, handwashing, and using antibiotics as directed and only when necessary. In addition, preventing infections also prevents the spread of resistant bacteria.The main cause of antibiotic resistance is antibiotic use. When we use antibiotics, some bacteria die but resistant bacteria can survive and even multiply. The overuse of antibiotics makes resistant bacteria more common. The more we use antibiotics, the more chances bacteria have to become resistant to them.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
A. Adrenergic neurotransmitters and their biosynthesis and metabolism, adrenergic receptors their distribution and actions mediated by them
B. Sympathomimetics
1. Direct acting: SAR, Endogenous catecholamines,
a) Alpha adrenergic agonists: Phenylephrines, Methoxamine, Naphazoline, Xylometazolines, Oxymetazoline, Clonidines, Guanabenz, Methyldopa
b) Dual agonist/antagonist: Dobutamine
c) Beta adrenergic agonists: Isoproterenols, Metaproterenol, Terbutalins, Albuterol, Salbuterol, Bitolterol, Ritodrine
2. Indirect acting: Hydroxyamphetamine, Propylhexedrine
3. Mixed acting: Ephedrine, Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers: Phenoxybenzamines
c) Alpha1 blockers: Prazosins, Doxazosin, Tamsulosin
d) Alpha2 blockers: Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers: Propranolols, Nadolol, Pindolol, Timolol, Sotalol
b) Beta1 blockers: Acebutolol, Atenelol, Esmolol, Metaprolols
c) Betablockers with alpha1 antagonistic activity: Labetalol, Carvedilol
HERE PRESENTATING VITAMINS AS PER SYLLABUS OF MPHARM SUBJECT NATURAL PRODUCTS INCLUDING VITAMIN B2, B12, B3, ITS STRUCTURE ISOLATED FROM CONTENTS AND COMPLETE DETAIL ON IT IN A EASY WAY , THE MOST ASKED VITAMINS.
synthesis of hetero-cyclic drugs which act as anti-malarial drugs where you get all information about synthesis, preparation, properties, uses of drugs.
Synthetic reagent and applications OF ALUMINIUM ISOPROPOXIDEShikha Popali
SYNTHETIC REAGENTS AND APPLICATIONS OF ALUMINIUM ISOPROPOXIDE ITS ALTERNATIVE NAMES AND ITS PHYSICAL PROPERTIRS , HANDLING, STORAGE, PRECAUTIONS, PREPARATIONS, SYNTHETIC APPLICATIONS
Analog design is usually defined as the modification of a drug molecule or of any bioactive compound in order to prepare a new molecule showing chemical and biological similarity with the original model compound
There are many ways that drug-resistant infections can be prevented: immunization, safe food preparation, handwashing, and using antibiotics as directed and only when necessary. In addition, preventing infections also prevents the spread of resistant bacteria.The main cause of antibiotic resistance is antibiotic use. When we use antibiotics, some bacteria die but resistant bacteria can survive and even multiply. The overuse of antibiotics makes resistant bacteria more common. The more we use antibiotics, the more chances bacteria have to become resistant to them.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
A. Adrenergic neurotransmitters and their biosynthesis and metabolism, adrenergic receptors their distribution and actions mediated by them
B. Sympathomimetics
1. Direct acting: SAR, Endogenous catecholamines,
a) Alpha adrenergic agonists: Phenylephrines, Methoxamine, Naphazoline, Xylometazolines, Oxymetazoline, Clonidines, Guanabenz, Methyldopa
b) Dual agonist/antagonist: Dobutamine
c) Beta adrenergic agonists: Isoproterenols, Metaproterenol, Terbutalins, Albuterol, Salbuterol, Bitolterol, Ritodrine
2. Indirect acting: Hydroxyamphetamine, Propylhexedrine
3. Mixed acting: Ephedrine, Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers: Phenoxybenzamines
c) Alpha1 blockers: Prazosins, Doxazosin, Tamsulosin
d) Alpha2 blockers: Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers: Propranolols, Nadolol, Pindolol, Timolol, Sotalol
b) Beta1 blockers: Acebutolol, Atenelol, Esmolol, Metaprolols
c) Betablockers with alpha1 antagonistic activity: Labetalol, Carvedilol
Epilepsy is a neurological disorder characterized by recurrent and unprovoked seizures. Seizures occur due to abnormal electrical activity in the brain, which leads to temporary disruptions in normal brain function. These disruptions can result in various physical, sensory, emotional, and cognitive symptoms.
Seizures in epilepsy can manifest in different ways and can vary in intensity and duration. Some common seizure types include:
1. Generalized seizures: These seizures involve both sides of the brain and typically result in loss of consciousness. Examples of generalized seizures include tonic-clonic seizures (previously known as grand mal seizures), absence seizures (previously known as petit mal seizures), and atonic seizures.
2. Focal seizures: Formerly known as partial seizures, these seizures are localized to a specific area of the brain. Focal seizures can be further categorized as focal onset aware seizures (previously simple partial seizures), where the person remains conscious during the seizure, or focal onset impaired awareness seizures (previously complex partial seizures), where the person experiences an altered level of consciousness.
Epilepsy can have various causes, including genetic factors, brain injuries, infections, developmental disorders, and brain tumors. However, in many cases, the exact cause remains unknown.
Diagnosis of epilepsy typically involves a thorough medical history review, neurological examination, and various diagnostic tests, such as electroencephalogram (EEG), brain imaging (MRI or CT scan), and blood tests. Treatment options for epilepsy aim to control seizures and may involve the use of antiepileptic medications. In some cases, surgery or other interventions may be considered.
It's important for individuals with epilepsy to work closely with healthcare professionals to manage their condition effectively. With proper medical care and lifestyle adjustments, many people with epilepsy are able to lead fulfilling lives and have their seizures well controlled.
Epilepsies are a group of disorders of the CNS characterized by paroxysmal cerebral dysrhythmia seizures and convulsions .
This ppt includes types of seizures according to lippincott , classification of antiepileptic drugs according to KD tripathi book .
Mechanism of action of classified drugs , choice of drugs and thier adverse effects + side effects .
This ppt aims to give summary of antiepileptic drugs .
this presentation is based on anticonvulsants which are used to cure or to control the disturbance created in brain by abnormal discharging of neurons which is termed as epilepsy.
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
e-content of Stereochemistry for Pharmacy and Chemistry students.
contents includes Isomerism, Chirality, Stereoisomers, Enantiomer, Diastereomer, Cis And Trans Configuration ,L And D Configuration ,R And S Configuration and Importance of the chirality in drugs ,Intravenous anaesthetics , etc.
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
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
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
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
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
micro teaching on communication m.sc nursing.pdfAnurag Sharma
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.
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
Anti ulcer drugs and their Advance pharmacology ||
Anti-ulcer drugs are medications used to prevent and treat ulcers in the stomach and upper part of the small intestine (duodenal ulcers). These ulcers are often caused by an imbalance between stomach acid and the mucosal lining, which protects the stomach lining.
||Scope: Overview of various classes of anti-ulcer drugs, their mechanisms of action, indications, side effects, and clinical considerations.
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
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.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...
02.Anticonvulsant and H1 and H2 receptor antagonist.pptx
1. ANTI-CONVULSANT AND
H1 & H2 RECEPTOR ANTAGONIST
Presenting by:
Mr. PURSHOTHAM K N
Asst. Professor,
Dept. of Pharmaceutical Chemistry
SAC College of Pharmacy.
2021-2022
2. DEFINATION:
• Epilepsy is a brain disorder in which clusters of nerve cells, or neurons,
in the brain sometimes signal abnormally.
• Neurons normally generate electrochemical impulses that act on other
neurons, glands, and muscles to produce human thoughts, feelings, and
actions.
• In epilepsy, the normal pattern of neuronal activity becomes disturbed,
causing strange sensations, emotions, and behavior, or sometimes
convulsions, ,and loss of consciousness.
3. TYPES OF SEIZURES:
1) Generalised seizures: affects both sides of the brain.
a. Absence seizures.
b. Tonic-clonic seizures.
a. Absence seizures,
sometimes called petit mal seizures, can cause rapid blinking
or a few seconds of staring into space.
b. Tonic-clonic seizures.
also called grand mal seizures, can make a person. Cry out,
Lose consciousness, Fall to the ground, Have muscle jerks or spasms.
4. 2) Focal seizures:
are located in just one area of the brain. These seizures are also called
partial seizures
a. Simple focal seizures affect a small part of the brain. These seizures
can cause twitching or a change in sensation, such as a strange taste or
smell.
b. Complex focal seizures can make a person with epilepsy confused or
dazed. The person will be unable to respond to questions or direction for
up to a few minutes.
c. Secondary generalized seizures begin in one part of the brain, but then
spread to both sides of the brain. In other words, the person first has a
focal seizure, followed by a generalized seizure.
5. ANTI-CONVULSANT DRUG
• These drugs that is used to prevent or treat seizures or convulsions by
controlling abnormal electrical activity in the brain.
• Are used to treat epilepsy and other seizure disorders.
6. CLASSIFICATION OF ANTIEPILEPTIC DRUGS
a. Hydantoins: phenytoin, phosphenytoin.
b. Barbiturates: phenobarbitone.
c. Iminostilbenes: carbamazepine, oxcarbazepine.
d. Succinimides: ethosuximide.
e. Aliphatic carboxylic acid: Valproic acid, divalproex
f. Benzodiazepines: clonazepam, diazepam, lorazepam.
g.Newer compounds: gabapentin, lamotrigine, tiagabine, topiramate,
vigabatrin, zonisamide, felbamate.
9. Mechanism Of Action Barbiturates
• Barbiturates are general depressants of all cell of the body, acting as a
cellular histotoxic agent. But the cell of the CNS are more sensitive to
barbiturate action.
1.Barbiturate induce sleep by selectively depressing RAS inthe brain stem.
2.Barbiturate selectively depress neuronal activity in posterior
hypothalamus, amygdaloid nucleus& limbic structure (CNS depression)
3.Barbiturates depress monosynptic pathway of spinalcord (anticanvulsion)
Barbiturates have also GABA like activity or enhance GABA activity.
10. MECHANISM OF ACTION BENZODIAZEPINES
• Benzodiazepines work by increasing the efficiency of a natural brain
chemical, GABA, to decrease the excitability of neurons. This reduces
the communication between neurons and, therefore, has a calming effect
on many of the functions of the brain.
• GABA controls the excitability of neurons by binding to the GABA
receptor. GABA receptors contain an ion channel that conducts chloride
ions across neuronal cell membranes, GABAa receptor complexes also
contain a single binding site for benzodiazepines.
• Binding of benzodiazepines to this receptor complex promotes binding
of GABA, which in turn increases the conduction of chloride ions across
the neuronal cell membrane. This increased conductance raises the
membrane potential of the neuron, resulting in inhibition of neuronal
firing.
11. Mechanism of action of Gabapentin:
• Enhances GABA activity.
• Binds to alpha-2-delta subunit of voltage gated calcium channels
• Inhibits high-voltage-activated calcium currents.
• Result is decreased synaptic transmission
13. HYDANTOIN:
• A phenyl or other aromatic substituents at C5 is essential for the
activity.
• Alkyl substituents at position 5 may contribute to sedation, a property
absent in phenytoin.
• Among other hydantoins some exhibits activity against chemically
induced convulsions.
• While remaining are ineffective against electro shock induced
convulsions.
14. BARBITURATES:
• Optimum activity is observed when one of the substituents at C5 is
phenyl.
• The 5, 5-diphenyl derivatives have less activity than phenobarbitone.
• N2 and N3 substituents, in some cases also results in an increased
activity.
• 5,5-dibenzyl barbituric acid causes convulsions.
15. BENZODIAZEPINES:
• The electron withdrawing atom or group at position 7 increases the anti-
epileptic activity while electron donating substituents at 7, 8 or 9
positions decrease it.
• A phenyl group at position 5 is necessary for activity. But only halogen
substituents are allowed in the ortho position.
• The electron withdrawing groups at ortho or di-ortho positions at 5-
phenyl increase the activity while any substituents on meta or para
position at 5-phenyl decreases the activity.
• Methyl substitution at position 1 confirms high activity.
16. VALPROIC ACID:
• Among other relatives of valproic acid, 3, 3, 4-trimethylpentanoic acid
is also as active as valproic acid.
• The anticonvulsant activity increases with increased chain length.
• Introduction of a double bond decreases the activity.
17. SUCCINIMIDES:
• Methsuximide and phensuximide have phenyl substituents which makes
them active against electrically induced convulsion.
• N-Methylation decreases activity against electroshock seizures and
impart more activity against chemically induced convulsion.
19. H1 AND H2 RECEPTORS ANTAGONIST:
• Histamine is a chemical messenger which are synthesized in the mast cells.
• Structurally histamines is 4-(2-amino ethyl)- imidazole.
• The histamines are available in two tautomeric forms.
20. • Generally histamines are found in the animal tissue, venoms of insect,
bacteria and plant.
• Pharmacologically histamine causes the vasodilatation of capillaries
and which increase the rate of flow and this cause edema, increase heart
rate, stimulate gastric fluids and which lead to the formation of ulcers.
• The human body contains histaminic receptor and are divided into three
different types upon their action.
1. H1-receptors.
2. H2-receptors.
3. H3-receptors
21.
22.
23. CLASSIFICATION OF H1 RECEPTOR ANTAGONIST:
• Ethylene diamine derivative:
ex: 1.Meperamine(Pyrilamine)
Uses:
a. Antihistaminic.
b. Antitussive
c. Less sedative.
28. Mechanism of action of Ranitidine:
Ranitidine
competitively block H2 receptor
Histamine cannot act
Decreases cAMP formation
Reduce acid secretion Healing of ulcer.
29. SAR OF H1 RECEPTOR ANTAGONIST:
• In the above general structure, Ar is aryl group and Ar' is aryl or aryl
methyl group.
• In the general structure the X part determines the class of drug to which
that belongs I.e. if X=O (amino alkyl analogue), X-N (Ethylene diamine
derivative).
• Some times two aromatic rings are bridges that constitutes the tricycle
ring derivative.
30. • Most of the H1 antagonist have ethylene chain, extension of this chain
or branching of this chain lead to reduce the activity of the compound.
• Homologation played to improve the drug like tricyclic anti-
depressents, neruroleptics.
• Due to the close resemblance of antihistamine structure to the
cholinergic blocking agent, most of the antihistamines show the activity
of anti- cholinergic activity.
31. SAR OF H2 RECEPTOR ANTAGONIST:
• In the H2 receptor, imidazole structure believed tobe important for
receptor action.
• The imidazole structure exist in two forms.
32. • The form (1) seems to be necessary for maximal H2-antagonist activity.
Where the R is substituted with CH3 the activity becomes potent.
• Chain of four carbon atom is optional for the activity, shorter chain
drastically lowers the activity. The presence of thioether (-S-) in the
methylene place (-CH3-) lead to more activity.
• The presence of terminal N group increase the activity.