Histamine and bradykinin are important autacoids or local hormones that act near their site of synthesis to exert physiological effects. Histamine is released from mast cells and basophils during allergic reactions and binds to H1, H2, H3 and H4 receptors, causing effects like vasodilation, increased vascular permeability, and bronchioconstriction. It is involved in allergic diseases. Bradykinin is produced from kininogen and acts on B1 and B2 receptors to cause vasodilation, smooth muscle contraction, increased vascular permeability and pain. Both histamine and bradykinin are inactivated by enzymatic degradation and their effects can be blocked by receptor antagonists.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
Detailed information of all terms like Thyroid gland, Thyroxine, Triidothyronine, Calcitonine, growth and development , propylthiouracil, Calorigenesis, tadpole to frog, Oligomenorrhoea, snehal chakorkar, pharmacology, Cretinism, Myxoedema coma, Graves disease, Thiocynates, Perchlorate, Nitrates.
Radioactive iodine, I131
H1-antihistamines are used to treat allergy symptoms. Within this group are two generations called the first generation and second generation antihistamines. H2-antihistamines are used to treat gastrointestinal conditions.
The H2 receptor antagonists are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells, where they inhibit acid secretion. They are highly selective, do not affect the H1 receptors, and are not anticholinergic agents.
The key difference between H1 and H2 receptors is that the H1 receptor couples with Gq/11 stimulating phospholipase C while the H2 receptor interacts with Gs to activate adenylyl cyclase. Histamine is an organic nitrogenous compound that involves local immune responses.
5-Hydroxytryptamine & it’s Antagonist is a Topic in Pharmacology which will defiantly Help You in pharmacy field All information is related to pharmacology drug acting and it's effect on body. it is collage project given by our department i would like to share with you.
Detailed information of all terms like Thyroid gland, Thyroxine, Triidothyronine, Calcitonine, growth and development , propylthiouracil, Calorigenesis, tadpole to frog, Oligomenorrhoea, snehal chakorkar, pharmacology, Cretinism, Myxoedema coma, Graves disease, Thiocynates, Perchlorate, Nitrates.
Radioactive iodine, I131
H1-antihistamines are used to treat allergy symptoms. Within this group are two generations called the first generation and second generation antihistamines. H2-antihistamines are used to treat gastrointestinal conditions.
The H2 receptor antagonists are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells, where they inhibit acid secretion. They are highly selective, do not affect the H1 receptors, and are not anticholinergic agents.
The key difference between H1 and H2 receptors is that the H1 receptor couples with Gq/11 stimulating phospholipase C while the H2 receptor interacts with Gs to activate adenylyl cyclase. Histamine is an organic nitrogenous compound that involves local immune responses.
5-Hydroxytryptamine & it’s Antagonist is a Topic in Pharmacology which will defiantly Help You in pharmacy field All information is related to pharmacology drug acting and it's effect on body. it is collage project given by our department i would like to share with you.
Outline:
What is the antihistamines.
What is histamine.
What is the receptors.
What is the clinical uses of antihistamines.
Side effects of antihistamines.
What is the contraindications.
pharmacology of Histamines , Serotonin and its antagonistibrahimussa
Histamine is an organic nitrogenous compound involved in local immune responses, as well as regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Histamine is involved in the inflammatory response and has a central role as a mediator of itching
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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.
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
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
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
3. “An organic substance, such as a hormone, produced
in one part of organism and transported by the
blood or lymph to another part of the organism
where it exerts a physiologic effect on that part”.
7. INTRODUCTION
• Imidazole ethylamine
• Formed from the amino acid Histidine
• Important inflammatory mediator
• Potent biogenic amine and plays an
important role in inflammation,
anaphylaxis, allergies, gastric acid
secretion and drug reaction
• As part of an immune response to
foreign pathogens, produced by
Basophils and mast cells found in
nearby connective tissues.
8. SITES OF HISTAMINE RELEASE
1) Mast cell site:
• Pulmonary tissue (mucosa of bronchial tree)
• Skin
• GIT(intestinal mucosa)
Conc. Of histamine is particularly high in these tissues
9. 2) Non-mast cell sites:
• CNS (neurons)
• Epidermis of skin
• GIT(gastric cells)
• Cells in regenerating or rapidly growing tissues
• Basophils (in the blood)
10. SYNTHESIS
• Decarboxylation of amino acid L-histidine catalyzed by L-
histidine decarboxylase.
• Storage sites:
• perivascular tissue – mast cell
• circulation – basophil (bound to chondroitin SO4)
• others – GIT, lungs, skin, heart, liver, neural tissue, reproductive
mucosa, rapidly growing tissues and body fluids
11. METABOLISM
Major pathways
• Deamination – small intestine, liver, kidney and monocytes
• Methylation – small intestine, liver, skin, kidney, thymus &
leukocytes
12.
13. MECHANISM OF ACTION
Histamine is an autacoid, which means it acts similarly to a local
hormone, near its site of synthesis. It is produced as part of the
local immune response to invading bodies and triggers
inflammation.
Histamine exerts its effects by binding to histamine receptors on
cells’ surfaces.
14. There are four types of histamine receptor: H1, H2, H3 and H4. The
binding of histamine to these receptors stimulates them to
produce functional responses:
• The H1 histamine receptor plays an important role in allergic
response and is widely distributed throughout the peripheral
nervous system, particularly the smooth muscle. Activation of the
H1 receptor causes blood vessel dilation, increased vessel
permeability, stimulation of sensory nerves in the airways and
bronchoconstriction. In addition, activation of this receptor
promotes the chemotaxis of eosinophils, which can lead to nasal
congestion, sneezing and rhinorrhea.
15. • The H2 receptor is found on the parietal cells within the stomach,
heart and to a limited extent, in immune cells and vascular smooth
muscle. Activation of the H2 receptor stimulates vasodilation and
release of the gastric acids required for digestion.
16. • The H3 histamine receptor is a presynaptic autoreceptor found on
nerve cells that contain histamine. It is widely distributed
throughout the central nervous system, with the greatest
expression found in the cortex, caudate nucleus, thalamus,
hypothalamus, olfactory tubercle and hippocampus. The diverse
distribution of the H3 receptor throughout the cortex suggests this
receptor is able to modulate many neurotransmitters such as
dopamine, GABA, acetylcholine and norepinephrine in the central
and peripheral nervous systems.
17.
18. • The H4 histamine receptor is mainly found on immune cells and
tissues including peripheral blood leukocytes, the spleen, bone
marrow and thymus. It is also found in the colon, lung, liver and
epicanthus. Stimulation of this receptor also mediates the
chemotaxis of eosinophils and upregulates adehsion of molecules.
19. ROLE IN ALLERGY:
• Allergies are caused by a hypersensitivity reaction of the antibody class IgE (which are
located on mast cells in the tissues and basophils in the blood)
• When an allergen is encountered, it binds to IgE, which excessively activates the mast
cells or basophils, leading them to release massive amounts of histamines
20.
21. • These histamines lead to inflammatory responses ranging from
runny nose to anaphylactic shock
• If both parents have allergies, you have a 70% chance of having
them, if only one parent does, you have a 48% chance, statistics
suggested by American Academy of Asthma, Allergies and
Immunology.
22. HISTAMINE ANTAGONISTS
Anithistamines are drugs used to block the activity of histamines, by
preventing the ability of histamine to bind to histamine receptors.
These agents are therefore referred to as histamine antagonists.
23. HISTAMINE ANTAGONISTS
H1 receptor antagonist
1) Sedative (first generation) antihistamines: Highly lipid soluble and easily enters into the CNS:
a) Potent and marked sedative:
• Promethazine (phenergan) widely used • Diphenhydramine Dimenhydrinate
b) Potent and moderate sedative:
• Chloryclizine • Chlorpheniramine • Tetrahydeoxy carboline
c) Less potent and less sedative: • Mepyramine • Pheniramine(avil)
2) Non-sedative (second generation ) antihistamines: Less lipid soluble therefore cannot enter into the CNS:
• Cetrizine • Terfenadine • Astemizole • Ketotifen • Cyclizine
27. H2 RECEPTOR ANTAGONISTS
H2 blockers are a group of medicines that reduce the amount of
acid produced by the cells in the lining of the stomach. They are
commonly called H2 blockers. They include cimetidine, famotidine,
nizatidine and ranitidine.
28. INDICATIONS
H2-antagonists are used by clinicians in the treatment of acid-
related gastrointestinal conditions, including:
• Peptic ulcer disease (PUD)
• Gastroesophageal reflux disease (GERD/GORD)
• Dyspepsia
• Prevention of stress ulcer (ranitidine)
29. DRUG INTERACTIONS:
• Cimetidine inhibits cyto p-450 – accumulation of warfarin,
phenytoin, theophylline, propanolol, diazepam & phenobarbital
• Ranitidine – weak inhibitor
• Nizatidine & famotidine – do not inhibit
cyto P – 450
30. H3 RECEPTOR ANTAGONIST
• An H3 receptor antagonist is a classification of drugs used to block the
action of histamine at the H3 receptor.
• Unlike the H1 and H2 receptors which have primarily peripheral actions,
H3 receptors are primarily found in the brain and are inhibitory
autoreceptors located on histaminergic nerve terminals, which
modulate the release of histamine. Histamine release in the brain
triggers secondary release of excitatory neurotransmitters such
as glutamate and acetylcholine via stimulation of H1 receptors in
the cerebral cortex.
31. • Consequently, unlike the H1 antagonist which are sedating,
H3antagonists have stimulant effects, and are being researched as
potential drugs for the treatment of neurodegenerative conditions
such as Alzheimer's disease.
• Examples of selective H3 antagonists include clobenpropit, ABT-
239, ciproxifan, conessine, A-349,821, and pitolisant.
32. The ability of the H3 receptor to modulate various neurotransmitters
makes this receptor a novel therapeutic target in the relief of
symptoms caused by several conditions including movement
disorders, obesity, schizophrenia, abnormal sleep/wake patterns
and ADHD.
33. H4 ANTAGONIST
• The histamine H4 receptor (H4R) is the newest member of the
histamine receptor family. H4 is highly expressed in bone marrow
and white blood cells and regulates neutrophil release from bone
marrow and subsequent infiltration in the zymosan-
induced pleurisy mouse model. It is also expressed in the colon, liver,
lung, small intestine, spleen, testes, thymus, tonsils, and trachea. By
inhibiting the H4 receptor, asthma and allergy may be treated.
34. The highly selective histamine H4 antagonist VUF-6002 is orally
active and inhibits the activity of both mast cells and eosinophils in
vivo, and has antiinflammatory and antihyperalgesic effects.
36. The recent discovery of a fourth histamine receptor (H4), and the
realization that it is exclusively expressed on hematopoietic cell
types that are most implicated in the development and
symptomatology of allergy and asthma, suggests that
pharmacological targeting of the H4 receptor, either alone or in
combination with H1 receptor antagonists, may prove useful for
treating both allergy and asthma.
37. PEPTIDE DERIVED AUTACOIDS
• THESE ARE DERIVED FROM PROTEINS
• MADE UP OF LONG CHAINS OF POLYPEPTIDES
• MOST IMPORTANT IN THIS CLASS: ANGIOTENSIN, BRADYKININ
38. BRADYKININ
The kinin-kallikrein system makes bradykinin by proteolytic
cleavage of its kininogen precursor, high-molecular-weight
kininogen (HMWK or HK), by the enzyme kallikrein. Moreover,
there is compelling evidence that plasmin, a fibrinolytic enzyme, is
able to generate bradykinin after HMWK cleavage.
39.
40. METABOLISM
In humans, bradykinin is broken down by three kininases:
Angiotensin-converting enzyme (ACE), Aminopeptidase P (APP),
and Carboxypeptidase N (CPN), which cleave the 7-8, 1-2, and 8-9
positions, respectively.
41. BRADYKININ RECEPTORS
• The B1 receptor (also called bradykinin receptor B1) is expressed only as a
result of tissue injury, and is presumed to play a role in chronic pain. This
receptor has been also described to play a role in inflammation. Most
recently, it has been shown that the kinin B1 receptor recruits neutrophil via
the chemokine CXCL5 production. Moreover, endothelial cells have been
described as a potential source for this B1 receptor-CXCL5 pathway.
42. • The B2 receptor is constitutively expressed and participates in
bradykinin's vasodilatory role.
• The kinin B1 and B2 receptors belong to G protein coupled receptor
(GPCR) family.
43. PHARMACOLOGICAL ACTIONS
Bradykinin is a potent endothelium-dependent vasodilator, leading
to a drop in blood pressure. It also causes contraction of non-
vascular smooth muscle in the bronchus and gut, increases
vascular permeability and is also involved in the mechanism
of pain. Bradykinin also causes natriuresis, contributing to the drop
in blood pressure.
44. Overactivation of bradykinin is thought to play a role in a rare
disease called hereditary angioedema, formerly known as
hereditary angio-neurotic edema.
45. BRADYKININ INHIBITORS
• Aprotinin (TRASYLOL), the potent inhibitor of kallikrein, has been
employed clinically to reduce blood loss in patients undergoing
coronary artery bypass surgery, but unfavorable survival statistics
in retrospective and prospective studies have resulted in its
discontinuation.
46. A new class of anti-hypertensive agent was developed to inhibit
major kinin-degrading enzymes, ACE, and the added inhibition of
bradykinin metabolism was expected to enhance therapeutic
effectiveness. In phase III clinical trials, the prototype drug
omapatrilat was an effective antihypertensive agent but was
associated with a 3-fold higher incidence of angioedema than with
an ACE inhibitor alone, causing withdrawal of the drug.
47. More recently, several non-peptide B1 antagonists with in vivo
activity have been developed the most promising of these is
SSR240612, which is orally active and inhibits inflammation and
neuropathic pain in animal studies. None has yet been tested
clinically.
48. BRADYKININ INHIBITORS
• Currently, bradykinin inhibitors are being developed as potential
therapies for hereditary angioedema. Icatibant is one such
inhibitor. Additional bradykinin inhibitors exist. It has long been
known in animal studies that bromelain, a substance obtained
from the stems and leaves of the pineapple plant, suppresses
trauma-induced swelling caused by the release of bradykinin into
the bloodstream and tissues.
49. • Other substances that act as bradykinin inhibitors
include aloe and polyphenols, substances found in red wine and
green tea.
• Bradykinin is also released by carcinoid tumors, and results
in asthma-like symptoms.