Histamine is released during allergic reactions and binds to four types of histamine receptors (H1-H4) throughout the body. H1 receptors are responsible for many allergic symptoms and are targeted by antihistamines. First generation antihistamines like diphenhydramine are sedating but newer second generation ones like loratadine are less sedating. Antihistamines treat allergies, nausea, and insomnia. H2 receptor blockers like ranitidine reduce stomach acid and treat ulcers. Mast cell stabilizers prevent histamine release for asthma prevention.
The parasympathetic division typically acts in opposition to the sympathetic autonomic nervous system through negative feedback control.
This action is a complementary response, causing a balance of sympathetic and parasympathetic responses.
Overall, the parasympathetic outflow results in the conservation and restoration of energy, reduction in heart rate and blood pressure, facilitation of digestion and absorption of nutrients, and excretion of waste products.
These are drugs that produce actions similar to that of Acetylcholine hence known as parasympathomimetics.
They act either by directly interacting with cholinergic receptors or by increasing the availability of Acetylcholine at these sites.
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
The parasympathetic division typically acts in opposition to the sympathetic autonomic nervous system through negative feedback control.
This action is a complementary response, causing a balance of sympathetic and parasympathetic responses.
Overall, the parasympathetic outflow results in the conservation and restoration of energy, reduction in heart rate and blood pressure, facilitation of digestion and absorption of nutrients, and excretion of waste products.
These are drugs that produce actions similar to that of Acetylcholine hence known as parasympathomimetics.
They act either by directly interacting with cholinergic receptors or by increasing the availability of Acetylcholine at these sites.
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
Parasympatholytics are the drugs that block or inhibit the actions of acetylcholine at postganglionic nerve endings and cholinergic receptors. They are also referred to as anticholinergics or cholinergic blocking agents or antispasmodics.
Anticholinergic drugs include atropine and related drugs- atropine is the prototype. Atropine is obtained from the plant Atropa belladonna. Atropine and scopolamine (hyoscine) are the belladonna alkaloids. They compete with acetylcholine for muscarinic receptors and block this receptors-they are muscarinic antagonists.
THIS ppt explains in brief about general anesthesia for under graduates. It includes brief classification, mechanism of action, side effects of some important drugs. concepts like diffusion hypoxia, second gas effect, balanced anesthesia and pre- anaesthetic medication are discussed.
Acetylcholine (ACh):- is an organic chemical that functions in the brain
and body of many types of animals, including humans, as a
neurotransmitter—a chemical released by nerve cells to send signals
to other cells.Its name is derived from its chemical structure: it is an
ester of acetic acid and choline. Parts in the body that use or are
affected by acetylcholine are referred to as cholinergic.
Acetylcholine is the neurotransmitter used at the neuromuscular
junction—in other words, it is the chemical that motor neurons of
the nervous system release in order to activate muscles.
.Acetylcholine is also used as a neurotransmitter in the autonomic
nervous system, both as an internal transmitter for the sympathetic
nervous system and as the final product released by the
parasympathetic nervous system.
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
Parasympatholytics are the drugs that block or inhibit the actions of acetylcholine at postganglionic nerve endings and cholinergic receptors. They are also referred to as anticholinergics or cholinergic blocking agents or antispasmodics.
Anticholinergic drugs include atropine and related drugs- atropine is the prototype. Atropine is obtained from the plant Atropa belladonna. Atropine and scopolamine (hyoscine) are the belladonna alkaloids. They compete with acetylcholine for muscarinic receptors and block this receptors-they are muscarinic antagonists.
THIS ppt explains in brief about general anesthesia for under graduates. It includes brief classification, mechanism of action, side effects of some important drugs. concepts like diffusion hypoxia, second gas effect, balanced anesthesia and pre- anaesthetic medication are discussed.
Acetylcholine (ACh):- is an organic chemical that functions in the brain
and body of many types of animals, including humans, as a
neurotransmitter—a chemical released by nerve cells to send signals
to other cells.Its name is derived from its chemical structure: it is an
ester of acetic acid and choline. Parts in the body that use or are
affected by acetylcholine are referred to as cholinergic.
Acetylcholine is the neurotransmitter used at the neuromuscular
junction—in other words, it is the chemical that motor neurons of
the nervous system release in order to activate muscles.
.Acetylcholine is also used as a neurotransmitter in the autonomic
nervous system, both as an internal transmitter for the sympathetic
nervous system and as the final product released by the
parasympathetic nervous system.
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
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).
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.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Read| The latest issue of The Challenger is here! We are thrilled to announce that our school paper has qualified for the NATIONAL SCHOOLS PRESS CONFERENCE (NSPC) 2024. Thank you for your unwavering support and trust. Dive into the stories that made us stand out!
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptxEduSkills OECD
Andreas Schleicher presents at the OECD webinar ‘Digital devices in schools: detrimental distraction or secret to success?’ on 27 May 2024. The presentation was based on findings from PISA 2022 results and the webinar helped launch the PISA in Focus ‘Managing screen time: How to protect and equip students against distraction’ https://www.oecd-ilibrary.org/education/managing-screen-time_7c225af4-en and the OECD Education Policy Perspective ‘Students, digital devices and success’ can be found here - https://oe.cd/il/5yV
The Art Pastor's Guide to Sabbath | Steve ThomasonSteve Thomason
What is the purpose of the Sabbath Law in the Torah. It is interesting to compare how the context of the law shifts from Exodus to Deuteronomy. Who gets to rest, and why?
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
3. Type Location Function
Causes:
vasodilation
Bronchoconstriction
bronchial smooth muscle
contraction separation of
endothelial cells
Found on: (responsible for hives),
H1 histamine • Smooth muscle and pain and itching due
receptor • Endothelium to insect stings;
• CNS tissue
the primary receptors
involved in allergic rhinitis
symptoms and motion
sickness;
sleep regulation.
4. H2 histamine Located on parietal Primarily stimulate
receptor cells gastric acid secretion
Decreased
Found on central
neurotransmitter
H3 histamine nervous system and
release: histamine,
to a lesser extent
receptor acetylcholine,
peripheral nervous
norepinephrine,
system tissue
serotonin
Found primarily in
the basophils and in
H4 histamine the bone marrow. It
Plays a role in
is also found on
receptor chemotaxis.
thymus, small
intestine, spleen, and
colon.
5. B. Release of histamine can occur by two
processes:
1. Energy- and Ca2+-dependent
degranulation reaction. The release of
histamine from mast cells is induced by:
A. immunoglobulin E (IgE) fixation to
mast cells (sensitization) and
subsequent exposure to a specific
antigen;
B. complement activation (mediated by
immunoglobulin G or immunoglobulin
M) may also induce degranulation.
6.
7. 2. Energy- and Ca2+-independent release
(displacement).
• Displacement is induced by:
A. drugs such as morphine, tubocurarine,
guanethidine, and amine antibiotics.
B. mast cell damage, which is caused by noxious
agents such as venom or by mechanical
trauma, can release histamine.
8. Mechanism of action
A. Histamine (H1)-receptors
– H1-receptors are found in the brain, heart,
bronchi, gastrointestinal tract, vascular
smooth muscles, and leukocytes.
– H1-receptors are membrane bound and
coupled to G-proteins, specifically Gq/11, and
their activation causes:
– increase in phospholipase A2 and D activity
– increases in diacylglycerol and intracellular Ca2+
– increased cyclic guanosine 5′-monophosphate (cGMP)
9. – Activation of H1-receptors in the brain
increases wakefulness.
– Activation of H1-receptors in vessels causes
vasodilation and an increase in permeability.
– Activation of H1-receptors typically stimulates
nonvascular smooth muscle.
10. B. Histamine (H2)-receptors
1. H2-receptors are membrane bound; they are
found in the brain, heart, vascular smooth
muscles, leukocytes, and parietal cells.
2. The response of H2-receptors is coupled via
Gαs to increased cyclic AMP (cAMP)
production.
3. Activation of H2-receptors:
• increases gastric acid production
• causes vasodilation
• generally relaxes smooth muscles.
11. C. Histamine (H3)-receptors
1. H3-receptors are found in the central nervous
system (CNS) and peripheral nervous system
(PNS) at presynaptic nerve terminals.
2. H3-receptors are membrane bound and
coupled to Gi/o; their activation increases
intracellular Ca2+ and decreases cAMP.
12. 3. Stimulation of H3-receptors
– on nerve cells causes a decrease in
histamine release
– in the CNS, stimulation of H3 modulates the
release of dopamine, acetylcholine,
serotonin, and norepinephrine.
– Activation of H3-receptors on the vagus
nerve decreases acetylcholine (ACh) release.
13. D. Histamine (H4)-receptors
1. H4-receptors are found on hematopoietic cells
and in the spleen, thymus, and colon.
2. Stimulation of H4 receptors increases
chemotaxis of mast cells and leukocytes cells
toward sites of inflammation.
3. H4 receptors are coupled to Gi/Go and thereby
inhibit the production of cAMP and increase
intracellular Ca2+
14. Histamine agonists
• Histamine, betazole, and impromidine.
– Betazole has approximately tenfold greater
activity at H2-receptors than at H1-receptors.
– Impromidine is an investigational agent; its
ratio of H2 to H1 activity is about 10,000.
– Methimepip is an H3-specific agonist.
15. • The uses of histamine agonists are primarily
diagnostic.
• These agents are used:
1. in allergy testing to assess histamine sensitivity
2. in the test of gastric secretory function
16. • The adverse effects of these agents can
be quite severe; they include:
• flushing
• a burning sensation
• hypotension
• tachycardia
• bronchoconstriction.
20. First-generation agents
1.Alkylamines
– Alkylamines include
– Chlorpheniramine
– Brompheniramine
– These agents produce slight sedation.
21. 2. Ethanolamines
– Include
– diphenhydramine
– doxylamine
– clemastine
– dimenhydrinate
(combination of diphenhydramine and 8-
chlorotheophylline)
– Ethanolamines produce marked sedation;
– doxylamine is marketed only as a sleeping
aid.
– Ethanolamines also act as antiemetics.
22. 3. Ethylenediamines
– Include:
– pyrilamine and antazoline.
– Ethylenediamines produce
moderate sedation and can cause
gastrointestinal upset.
23. 4. Piperazines
– include meclizine and cyclizine.
– Piperazines produce marked adverse
gastrointestinal effects and moderate
sedation.
– These agents have
A.antiemetic
B.antivertigo activities.
24. 5. Phenothiazines
– include promethazine.
– Phenothazines produce marked sedation.
– These agents have antiemetic activity.
– Phenothiazines are also weak α-
adrenoceptor antagonists.
25. 6. Methylpiperidines
– include cyproheptadine.
– have antihistamine, anticholinergic, and
antiserotonin activities.
26. 2. Second-generation agents
2. Piperidines
Loratadine [Claritin]
Desloratadine [Clarinex]
– Poor CNS penetration: reduced sedation
– Little or no anticholinergic activity
– Desloratadine:
• is the active metabolite of loratadine
• has about 15-fold greater affinity for the H1
receptor than the parent compound
27. Fexophenadine
– is structurally different than the other
piperidine antihistamines,
– sedative activity is low but dose dependent.
28. 2. Clemastine
• is a second-generation ethanolamine
• longer duration of action than
dimenhydramine
• it has some antiemetic activity.
3. Alkylamines:
A. acrivastine.
• Acrivastine is not associated with cardiac
effects.
29. B. Cetirizine [Zyrtec]
– Cetirizine is not associated with cardiac
abnormalities.
– Cetirizine has poor penetration into the
CNS.
– Cetirizine is less sedating;
– it is ineffective for motion sickness or
antiemesis.
30. Pharmacologic properties
of Histamine (H1)-receptor antagonists
• well absorbed after oral administration.
1st 2nd
generation generation
Onset 30 min 30 min
Duration 3-8 hrs 3-24 hours
31. • H1-receptor antagonists are lipid soluble; most first-
generation agents cross the blood— brain barrier.
• H1-receptor antagonists are metabolized in the liver;
• many induce microsomal enzymes and alter their own
metabolism and that of other drugs.
32. Pharmacologic Actions
• Many H1-receptor antagonists, especially the
ethanolamines, phenothiazines, and
ethylenediamines, have muscarinic—cholinergic
antagonist activity.
• Most of these agents are effective local anesthetics,
probably because of a blockade of sodium channels in
excitable tissues.
• Dimenhydrinate and promethazine are potent local
anesthetics.
33. • H1-receptor antagonists relax histamine-induced
contraction of bronchial smooth muscle and have some
use in allergic bronchospasm.
• These agents block the vasodilator action of histamine.
• H1-receptor antagonists inhibit histamine-induced
increases in capillary permeability.
• These agents block mucus secretion and sensory nerve
stimulation.
34. • H1-receptor antagonists, especially the first-generation
agents, frequently cause CNS depression (marked by
sedation, decreased alertness, and decreased appetite).
• In children and some adults, these agents stimulate the
CNS.
35. Therapeutic Uses
1. Treatment of allergic rhinitis and conjunctivitis.
• Clemastine is approved for the treatment of rhinorrhea.
• Many antihistamines are used to treat the common cold,
based on their anticholinergic properties, but they are
only marginally effective for this use.
• Diphenhydramine also has an antitussive effect not
mediated by H1-receptor antagonism.
36. 2. Treatment of urticaria and atopic dermatitis,
including hives
3. Sedatives. Several (doxylamine, diphenhydramine)
are marketed as over-the-counter (OTC) sleep aids.
4. Prevention of motion sickness
5. Appetite suppressants
37. Adverse effects
• (significantly reduced with second-generation agents)
• Sedation, dizziness, and loss of appetite.
• These agents can cause gastrointestinal upset, nausea,
and constipation or diarrhea.
• H1-receptor antagonists produce anticholinergic effects
(dry mouth, blurred vision, and urine retention).
• Two second-generation H1 antagonists, astemizole and
terfenadine (a prodrug of fexofenadine) were
discontinued or removed from the market because they
were associated with Q-T prolongation and ventricular
tachycardias.
38.
39. Histamine (H2)-receptor antagonists
• Cimetidine [Tagamet]
• Ranitidine [Zantac]
• Famotidine [Pepcid AC]
• Nizatidine [Axid]
Competitive antagonists at the H2-receptor,
which predominates in the gastric parietal cell.
40.
41. • Used in the treatment of:
1. Gastrointestinal disorders, including
heartburn and acid-induced indigestion.
2. These agents promote the healing of gastric
and duodenal ulcers.
3. Used to treat hypersecretory states such as
Zollinger-Ellison syndrome.
42. Pharmacokinetics
• The bioavailability of H2-antagonists goes from
50% for ranitidine and famotidine to
approximately 90% for nizatidine and advised
dosages take this into account.
• They are taken especially in the evening to
reduce night gastric acidity.
• Their elimination is primarily renal.
• Cimetidine inhibits cytochrome P-450 and
increases the concentrations and the effects of
many other drugs.
43. Adverse effects
• H2 antagonists are generally well-tolerated, except for
cimetidine where all of the following adverse drug
reactions (ADRs) are common.
• Infrequent ADRs include hypotension.
• Rare ADRs include: headache, tiredness, dizziness,
confusion, diarrhea, constipation, and rash.
• Additionally, cimetidine may also cause gynecomastia in
males, loss of libido, and impotence, which are
reversible upon discontinuation.
45. • These are administered by inhalation.
• They inhibit the release of histamine and other
autocoids from the mast cell.
• Each is used prophylactically in the treatment of
asthma
• they do not reverse bronchospasm.
46. • Adverse effects:
– confined to the site of application
– Include:
–sore throat
–dry mouth.
• Nedocromil sodium
– more effective in reducing bronchospasm
caused by exercise or cold air.