This document discusses adrenergic and cholinergic agents that act on the autonomic nervous system. It begins by introducing the autonomic nervous system and its divisions - the sympathetic and parasympathetic nervous systems. Acetylcholine is described as the neurotransmitter of the parasympathetic system. Cholinergic agonists and antagonists are then discussed, including bethanicol and anticholinesterases. Next, adrenergic drugs acting directly on receptors or indirectly by inhibiting norepinephrine storage are covered. Specific drugs like propranolol, prazosin, and methyldopa are explained in terms of their mechanisms and structure-activity relationships.
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.
The content includes the general introduction of enzymes their basic classification. Enzyme kinetics is described with a short view of Michaelis menten constants. Factors affecting the kinetics of enzymes are also discussed. Principles of enzyme inhibition are discussed with a few examples.
The contents is prepared by the help of books, internet sources, as well as other presentations. I am thankful to all of you.
THE NEUROMUSCULAR BLOCKING DRUGS HERE ARE PRESENTED WITH DEPOLARIZING AND NON DEPOLARIZING ALSO KNOWN AS COMETATIVE AND NON COMPETATIVE, WITH ITS DETAIL ACCOUNT ARE DISCUSSED HERE.
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
THE BERNTHSEN ACRIDINE SYNTHESIS IS THE SYNTHESIS OF ACRIDINE FIRSTLY PERFORMED BY BERNTHSEN THEREFORE KNOWN AS BERNTHSEN ACRIDINE SYNTHESIS. THIS PRESENTATION INCLUDES THE SYNTHESIS WITH ITS MECHANISM AND APPLICATION AS ASKED IN EXAMS.
A drug or other substance that affects how the brain works and causes changes in mood, awareness, thoughts, feelings, or behavior.
Depending on the substance, psychoactive drugs can cause euphoria, increased energy, sleepiness, hallucinations, and more.
Examples of psychoactive substances include alcohol, caffeine, nicotine, marijuana, and certain pain medicines.
Many illegal drugs, such as heroin, LSD, cocaine, and amphetamines are also psychoactive substances. Also called psychotropic substance.
Introduction
parasympathetic nervous system
cholinergic drugs
Anticholinergic agents
Divisions of Autonomous nervous system
Drugs acting on adrenergic nervous system
Adrenergic agents
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.
The content includes the general introduction of enzymes their basic classification. Enzyme kinetics is described with a short view of Michaelis menten constants. Factors affecting the kinetics of enzymes are also discussed. Principles of enzyme inhibition are discussed with a few examples.
The contents is prepared by the help of books, internet sources, as well as other presentations. I am thankful to all of you.
THE NEUROMUSCULAR BLOCKING DRUGS HERE ARE PRESENTED WITH DEPOLARIZING AND NON DEPOLARIZING ALSO KNOWN AS COMETATIVE AND NON COMPETATIVE, WITH ITS DETAIL ACCOUNT ARE DISCUSSED HERE.
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
THE BERNTHSEN ACRIDINE SYNTHESIS IS THE SYNTHESIS OF ACRIDINE FIRSTLY PERFORMED BY BERNTHSEN THEREFORE KNOWN AS BERNTHSEN ACRIDINE SYNTHESIS. THIS PRESENTATION INCLUDES THE SYNTHESIS WITH ITS MECHANISM AND APPLICATION AS ASKED IN EXAMS.
A drug or other substance that affects how the brain works and causes changes in mood, awareness, thoughts, feelings, or behavior.
Depending on the substance, psychoactive drugs can cause euphoria, increased energy, sleepiness, hallucinations, and more.
Examples of psychoactive substances include alcohol, caffeine, nicotine, marijuana, and certain pain medicines.
Many illegal drugs, such as heroin, LSD, cocaine, and amphetamines are also psychoactive substances. Also called psychotropic substance.
Introduction
parasympathetic nervous system
cholinergic drugs
Anticholinergic agents
Divisions of Autonomous nervous system
Drugs acting on adrenergic nervous system
Adrenergic agents
slide consist of cholinergic system, neuronal transmission, receptors of cholinergic system, anti cholinergic drugs its classification, Mechanism of action and organophosphate poisoning and treatment approaches
The medicinal chemistry aspect of the drugs affecting cholinergic nerve transmission of the autonomic nervous system are briefly explained in the slides.
Hypertension is the most common cardiovascular disease determined by increase blood pressure (pressure exerted by blood against the wall of a blood vessel )in arteries.
The onset of hypertension is defined as having a blood pressure of 140/90 mm Hg or greater .
Hypertension is the major risk factor for coronary artery disease, heart failure, stroke and renal failure.
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.
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
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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.
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
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
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- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
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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.
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.
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
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Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
1. Presenting by,
Mr. PURUSHOTHAM K N
Assistant Professor
Department of Ph. Chemistry
SACCP
B. G. Nagar
2021-2022
ADRENERGIC & CHOLINERGIC AGENTS
2. Introduction
AUTONOMIC NERVOUS SYSTEM
The autonomic nervous system is a control system that acts largely
unconsciously and regulates body functions such as the heart rate, digestion,
respiratory rate, pupillary response, urination.
The ANS is part of the peripheral nervous system and it also controls some of
the muscles within the body. We are often unaware of the ANS because it
functions involuntary and reflexively.
For example, we do not notice when blood vessels change size or when our heart
beats faster.
3. Divisions OF Autonomous Nervous System
I.SYMPATHETIC NERVOUS SYSTEM:
The sympathetic nervous system primary process is to stimulate the body's fight-or-flight
response.
For example-the sympathetic nervous system can accelerate heart rate,
widen bronchial passages, decrease motility of the large intestine, constrict
blood vessels, cause pupillary dilation.
2. PARASYMPATHETIC NERVOUS SYSTEM:
The parasympathetic nervous system is one of three divisions Of the autonomic nervous
system. Sometimes called the rest and digest system, the parasympathetic system
conserves energy as it slows the heart rate, increases intestinal and gland activity
4.
5. PARASYMPATÄOC NERVOUS SYSTEM
Acetyl choline (Ach) is neurotransmitter which propagates impulse transmission in
parasympathetic division. Ach also function as a neurotransmitters . Ach causes contraction
of smooth muscles, cardiac inhibition in man or laboratory animals. Parasympathetic nerve
fibers liberates acetylcholine hence this system is also called cholinergic nervous system .
Ach is biosynthesized by acetylation of choline molecule in nerve terminals. The free
acetylation present in blood and other tissues, get quickly hydrolysed by cholinesterase
enzyme into acetic acid and choline as shown below:-
8. CHOLINERGIC AGONIST
Choline esters
Acetyl Choline
1. Any change in the ethylene bridge may affect the chemical stability of Ach
molecule.
2. A quaternery ammonium group is essential for manifestation of both
muscarinic and nicotinic receptors.
3. If one or more methyl group is present on nitrogen atom are replaced by
hydrogen or ethyl group then both the activities Le muscarinic and nicotinic
activity is reduced.
4. Quaternary nitrogen atom may be replaced by Arsenic, antimony ,
phosphorous or sulphur atom without the loss of Ach like activities.
9. Bethanicol
Mode of action-
a) It has more selective muscarinic action on GIT and urinary bladder.
b) It increases tone of contraction of intestine
c) It causes emptying of urinary bladder due to contraction of muscle of bladder and
relaxation of sphincter muscle.
❑ Use-
It is used to get relief from abdominal distension (stress) after surgery.
10. 2. ANTICHOLINETERASE
These enzymes causes inhibition of cholinesterase enzyme which is
responsible for hydrolysis of acetylcholine into acetic acid and choline.
a. Reversible anticholinesterase - They having structural similarities with
Ach hence they are combined with anionic and esteric sites. -They
having a great affinity towards active sites but no intrensic activity.
example- i. Physostigmine
SAR-
1.The distance between other oxygen & nitrogen appproximately same as
that of distance between other oxygen and nitrogen present in Ach.
2.Two heterocyclic rings are not essential for anticholinesterase activity
during hydrolysis the phenolic fragment of these drug is eliminated .
leaving the carbonyl group attach to the enzyme.
- To treat glaucoma
11. Irreversible Anti cholinesterase
Irreversible anticholinesterase causes inhibition of anticholinesterase irreversible.
Eg:- methyl parathion
MOA-
Parathion is a organophosphorous compound.
It inhibits cholinesterase enzyme.
Use
It is used to treat glaucoma.
It is used to treat myasthenia gravis.
12. Irreversible Anti cholinesterase
Irreversible anticholinesterase causes inhibition of anticholinesterase irreversibly.
Eg : methyl partition
MOA-
Parathion is a organophosphorous compound.
It inhibits cholinesterase enzyme.
Use
It is used to treat glaucoma.
It is used to treat myasthenia gravis.
15. Cation group
N-atom must be tertiary amine which undergo quaternisation at physiological Ph.
Highly alkyl group on nitrogen causes stearic hinderance.
Quaternisation increases anticholinergic action and decreases cholinergic action.
Hydroxyl group
It is important for affinity and in presence of –OH more active compound.
Eg: amino alcohol ester
In amino alcohol ester , hydroxyl group contain carboixylic acid which having maximum activity.
e. Atropine.
16. Cyclic substitution
At least one cyclic substituent is a common feature in
anticholinergics.
Introduction of large cyclic group decrease activity.
Adverse effects
Tachycardia
Blurred vision.
Dry mouth and skin
Use
It is used to treat parkinsonism disease.
Atropine is specific antidote for mushroom poisioning
17. Drugs Acting on Adrenergic Nervous System
These are the drugs which produces action similar to that of action produced by adrenaline or causes
sympathetic stimulants.
Adrenaline and nor-adrenaline are the two transmitters-
Relaxation of smooth muscles.
Increase in heart activity.
Decrease the gland secreation.
19. Directly Acting Drugs
1. Non-selective beta 1 & beta 2 blockers.
example- propranolol
Propranolol belongs to the group of beta
blocking agents known as acyclopropranol
amine Group has been incorporated into
molecule between aromatic ring and
ethylamine side chain.
MOA-
It blocks the action of epinephrine and nor-
epinephrine on the both beta1 and beta 2
adrenergic receptor.
20. Nature of aromatic ring and its substituents are primary determinant of beta
antagonist activity. Propranolol has high lipid solubility which allows it to
penetrate nerve tissue and shows cardiodepressant effect in addition to
propranolol its beta blocking activity, to avoid this problem use of polar group
like methane sulphonamide.
iii. Alkyl on ortho group position on phenyl ring provides good activity.
e.g.
21. SAR-
Substutional of amino group R3 i.e CH3 Increased selectivity
Substitution if alpha carbon blocks metabolism by MOA.
OH at beta carbon enhances adrenoreceptor properties
22. SYMPATHOLYTIC OR ANTIADRENERGIC AGENTS
They block the release action of catecholamines (epinephrine, norepinephrine,
dopamine) which are released in response to stress.
Centrally acting antiadrenergic agents make the heart beat slower and with less
force, and relax the blood vessels.
23.
24. Prazosin
(i) Prazosin is a selective blocker of postsynaptic al receptors, producing
vasodilation Of both arteries and veins.
Prazosin reduces peripheral vascular resistance and lowers arterial blood pressure.
SAR-
a. Amino group present in the structure is essential for the activity.
b. If five membered ring in structure is removed then activity decreases.
25. Centrally acting sympatholytics
Methyldopa
Mechanism of action
Methyldopa is an α2 adrenergic receptor agonist acts centrally by decreasing the sympathetic outflow
which in turn lowers B.P.
SAR
If methoxy group is removed then sympatholytic activity decreases.
Nitrogen atom present in structure is essential for the activity.
Amine group present in structure shows antiadrenergic activity.
26. Drugs Inhibiting NE Storage
Stimulate NE secreation and inhibit sympathetic activity and reduces BP.
SAR-
If methoxy group is removed than sympatholytic activity decreases.
Nitrogen atom present in structure is essential for activity.
Amine group present in structure shows adrenergic activity.
MOA