Sympatholytic drugs (Adrenergic blockers) bind to the adrenergic receptors and prevent the action of adrenergic drugs.
These are drugs which block the actions of sympathetic division or catecholamines (adrenaline and noradrenaline).
They are competitive antagonists at both α and β adrenergic receptors.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
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.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
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.
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 term “opiate” refers only to substances with morphine-like activity that are structurally related to morphine. Opioids are sometimes referred to as “narcotic analgesics” and opioid receptor antagonists as “narcotic antagonists”
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
Neurohumoral transmission in CNS ,special emphasis on importance of various neurotransmitters like with GABA, Glutamate, Glycine, serotonin and dopamine
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 term “opiate” refers only to substances with morphine-like activity that are structurally related to morphine. Opioids are sometimes referred to as “narcotic analgesics” and opioid receptor antagonists as “narcotic antagonists”
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
Neurohumoral transmission in CNS ,special emphasis on importance of various neurotransmitters like with GABA, Glutamate, Glycine, serotonin and dopamine
Antihypertensives | Classes of Drugs | Baro ReceptorChetan Prakash
This Presentation provides a knowledge about Antihypertensives, types of blood pressure, hypertension types, normal blood pressure regulation, baro receptors, classes of antihypertensive drugs,recent discovery on hypertension. This is an assignment for the subject, Advanced Pharmacology-I, 1st year M.Pharm, 1st semester.
This presentation contains a brief introduction of Adrenergic and cholinergic systems and their function in our body.
And a brief description of some adrenergic and cholinergic agents along with their mechanism of action along with their respective Structures.
General introduction about hypertension and structure activity relationship of Different types of antihypertensive drugs, and related questions that were asked in exams.
detailed SAR and mode of action of ACE inhibitors
About pharmacological classification of sympathetic nervus system both sympathomimetics and sympatholytics drug and all about his pharmacokinetics and pharmacodynamics action on body
Pharmacology Experiment based Questions With Answer KeysA M O L D E O R E
MSBTE Pharmacology Practical Exam for Diploma in pharmacy students in Maharashtra.
Experimental pharmacology for D. Pharmacy Students
Pharmacology Experiment based Questions
PCI New Syllabus ER2020
Course Code: 20056
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting
Anatomy and physiology are two of the most basic terms and areas of study in the life sciences. Anatomy refers to the internal and external structures of the body and their physical relationships, whereas physiology refers to the study of the functions of those structures.
Animal cells are typical of the eukaryotic cell, enclosed by a plasma membrane and containing a membrane-bound nucleus and organelles. Unlike the eukaryotic cells of plants and fungi, animal cells do not have a cell wall. This feature was lost in the distant past by the single-celled organisms that gave rise to the kingdom Animalia. Most cells, both animal and plant, range in size between 1 and 100 micrometers and are thus visible only with the aid of a microscope.
All living organisms are made of cells and cellular products. The cell is the smallest structural, functional, and biological unit of all living organisms. It can capable of biosynthesis, replication and energy transformation. All cellular organelles carry out specific functions that are necessary for the normal functioning of the cell. Animal cells work together and function interdependently. Human cells vary in size, shape, and function. Most animal cells are so small they can only be seen with the aid of a microscope. Based on function, there are more than 200 different kinds of animal cells that help each system contribute to the homeostasis of the entire body. Despite their many differences, human cells have several similar structural features: a cell membrane, a nucleus, and cytoplasm and cell organelles.
Your sympathetic nervous system is best known for its role in responding to dangerous or stressful situations.
In these situations, your sympathetic nervous system activates to speed up your heart rate, deliver more blood to areas of your body that need more oxygen or other responses to help your get out of danger.
Its nerve fibers arise from the thoracic and lumbar regions of the spinal cord.
The autonomic ganglia are the synapses between preganglionic and postganglionic neurons. The postganglionic axons then go to the visceral effectors.
Acetylcholine is a neurotransmitter releases in the preganglionic nerve endings and Noradrenaline at postganglionic nerve endings.
The drugs which mimic the action sympathetic division are called sympathomimetics.
They show similar actions as that of catecholamines.
Sympathomimetic
They act by either by directly interacting with adrenergic receptors (alpha or beta) or stimulation of the adrenergic nerve endings.
The digestive system is made up of the gastrointestinal tract—also called the GI tract or digestive tract—and the liver, pancreas, and gallbladder. ... The hollow organs that make up the GI tract are the mouth, esophagus, stomach, small intestine, large intestine, and anus.
Hemostasis or haemostasis is a process to prevent and stop bleeding, meaning to keep blood within a damaged blood vessel (the opposite of hemostasis is hemorrhage). It is the first stage of wound healing. This involves coagulation, blood changing from a liquid to a gel.
Aminocaproates.
Antifibrinolytic Agents.
Estrogens, Conjugated (USP)
Hemostatics.
Tranexamic Acid.
Aprotinin.
Deamino Arginine Vasopressin
Sulfonamides (sulphonamides) are a group of man-made (synthetic) medicines that contain the sulfonamide chemical group. They may also be called sulfa drugs. Many people use the term sulfonamide imprecisely to refer only to antibiotics that have a sulfonamide functional group in their chemical structure.
The endocrine system is a messenger system comprising feedback loops of the hormones released by internal glands of an organism directly into the circulatory system, regulating distant target organs. In vertebrates, the hypothalamus is the neural control center for all endocrine systems.
Anticoagulants are used to treat and prevent blood clots that may occur in your blood vessels. Blood clots can block blood vessels (an artery or a vein). A blocked artery stops blood and oxygen from getting to a part of your body (for example, to a part of the heart, brain or lungs).
A tissue is a group of similar cells that are specialized for a particular function.
The four basic fundamental types of body tissues are
1. Epithelial tissue
2. Connective tissue
3. Muscular tissue
4. Nervous tissue
Each type of tissue is characterized by specific functions. These tissues contribute to the overall health and maintenance of the body. These tissues combine to form organs. The various organs make up the systems of the body that allow us to function and survive in our complex world. Histology is the science that deals with the study of tissues.
In biology, the tissue is a cellular organizational level between cells and a complete organ. A tissue is an ensemble of similar cells and their extracellular matrix from the same origin that together carry out a specific function. Organs are then formed by the functional grouping together of multiple tissues.
The English word "tissue" derives from the French word "tissue", meaning that something that is "woven", from the verb tisse, "to weave".
Career scope and opportunities
Pharmacy is the health profession that links the health sciences with the chemical sciences, and it is charged with ensuring the safe and effective use of medication. The scope of pharmacy practice includes compounding and dispensing medications, and it also related to more modern services like patient care, including clinical services, reviewing medications for safety and efficacy, and providing drug information.
The demand for pharma graduates is high in sectors like - healthcare, research, manufacturing, medical marketing, pharmacovigilance etc. As a pharma graduate, you can take up job roles like - drugs inspector, drugs controller, hospital pharmacist etc.
Ever hear the term "bronchial asthma" and wonder what it means? When people talk about bronchial asthma, they are really talking about asthma, a chronic inflammatory disease of the airways that causes periodic "attacks" of coughing, wheezing, shortness of breath, and chest tightness.
According to the CDC, more than 25 million Americans, including 6.8 million children under age 18, suffer with asthma today.
Allergies are strongly linked to asthma and to other respiratory diseases such as chronic sinusitis, middle ear infections, and nasal polyps. Most interestingly, a recent analysis of people with asthma showed that those who had both allergies and asthma were much more likely to have nighttime awakening due to asthma, miss work because of asthma, and require more powerful medications to control their symptoms.
Asthma is associated with mast cells, eosinophils, and T lymphocytes. Mast cells are the allergy-causing cells that release chemicals like histamine. Histamine is the substance that causes nasal stuffiness and dripping in a cold or hay fever, constriction of airways in asthma, and itchy areas in a skin allergy. Eosinophils are a type of white blood cell associated with allergic disease. T lymphocytes are also white blood cells associated with allergy and inflammation.
These cells, along with other inflammatory cells, are involved in the development of airway inflammation in asthma that contributes to the airway hyperresponsiveness, airflow limitation, respiratory symptoms, and chronic disease. In certain individuals, the inflammation results in the feelings of chest tightness and breathlessness that's felt often at night (nocturnal asthma) or in the early morning hours. Others only feel symptoms when they exercise (called exercise-induced asthma). Because of the inflammation, the airway hyperresponsiveness occurs as a result of specific triggers.
These are substances produced by a wide variety of cells in the body, having strong biological activity. Autacoids generally act locally at the site of synthesis and release. So they have also been called ‘local hormones’. They have short duration of action. They usually exert their action at the site of inflammation, lesion and injury.
The autacoids also differ from circulating hormones in that they are produced by many tissues rather than in specific endocrine glands.
The classical autacoids are— Ex.
Histamine, Serotonin
Prostaglandins, Leukotriene, Heparin, Endothelins
Bradykinin, Angiotensin, Eicosanoids
Interleukins, TNFα (tissue necrosis factor),
Platelet activating factor
The cell is the smallest structural, functional, and biological unit of all living organisms. It can capable of biosynthesis, replication and energy transformation.
ANATOMY
Anatomy is the study of the structure or morphology of the body and the physical relationship between body parts.
PHYSIOLOGY
Physiology is the study of the functions of body parts, what they do, and how they do it.
Within the body, there are different levels of structural organization and complexity.
Drug dependence
It is a physical or psychological condition resulting from repeated administration of mood-altering drugs.
It is a state characterized by a compulsion to take the drug on a continuous or periodic basis in order to experience its euphoriogenic effects.
If a mood-altering drug is unavailable, then the individual develops certain withdrawal symptoms.
Physical dependence + Psychological dependence
Drug addiction
Drug habituation
Drug abuse
Habit-forming drug
General anesthesia is a medically induced reversible loss of consciousness and loss of protective reflexes over the entire body, resulting from the administration of general anesthetic agents. The optimal combination of these agents for any given patient and procedure is typically selected by an anesthesiologist.
General anesthesia has many purposes including:
Pain relief (analgesia)
Blocking memory of the procedure (amnesia)
Producing unconsciousness
Inhibiting normal body reflexes to make surgery safe and easier to perform
Relaxing the muscles of the body
Non narcotic analgesics, antipyretics & anti-inflammatory drugsA M O L D E O R E
An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain. Analgesic drugs act in various ways on the peripheral and central nervous systems.
Non-steroidal anti-inflammatory drugs (NSAIDs) are medicines that are widely used to relieve pain, reduce inflammation, and bring down a high temperature. They're often used to relieve symptoms of headaches, painful periods, sprains and strains, colds and flu, arthritis, and other causes of long-term pain.
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Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
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.
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
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.
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
- 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
1. SYMPATHOLYTICS
Prof. Amol B. Deore
• Department of Pharmacology
• MVP’s Institute of Pharmaceutical Sciences, Nashik
2. SYMPATHOLYTICS
•Sympatholytic drugs (Adrenergic blockers) bind to
the adrenergic receptors and prevent the action of
adrenergic drugs.
•These are drugs which block the actions of
sympathetic division or catecholamines (adrenaline
and noradrenaline).
•They are competitive antagonists at both α and β
adrenergic receptors.
3. Adrenergic Receptors
•Adrenaline and noradrenaline are the
neurotransmitters release at the sympathetic post
ganglionic nerve endings.
•The adrenergic receptors are categorized into alpha
and beta adrenergic receptors. Adrenaline acts on both
alpha and beta receptors.
4. Alpha Sympatholytics
• Alpha adrenergic blocking agents
• Alpha receptor antagonists block the adrenergic
responses mediated through alpha adrenergic
receptors.
• Some of them have selectivity for α1 or α2 receptors.
5. • Pharmacological actions of adrenaline and alpha Sympatholytics
Receptor Location
Pharmacological actions
of Adrenaline
Pharmacological actions
of α- Sympatholytics
α1
• Veins, arterioles,
arteries, capillaries
• Urinary sphincter
• Eye Radial muscles
Vasoconstriction and
rise in blood pressure
Contraction
Mydriasis
Vasodilation and fall in
blood pressure
Relaxation
Miosis
α2
• Presynaptic
membrane
• Blood vessels
Control release of NA in
nerve endings
Vasoconstriction and
rise in blood pressure
Increase release of NA
Vasodilation and fall in
blood pressure
7. Pharmacological actions of alpha sympatholytics
• The important effects of α receptor stimulation are α1
mediated vasoconstriction and α2- (presynaptic) receptor
mediated inhibition of NA release.
• α1-blockade—inhibits vasoconstriction --leading to
vasodilation and thereby ↓ BP. This fall in BP is opposed by
the baroreceptor reflexes which tend to ↑ heart rate and
cardiac output.
• α2-blockade—enhances release of NA which stimulates β
receptors (α are already blocked) - β1 stimulation in heart
results in tachycardia and increased cardiac output.
8. Selective α1-blockade—results in hypotension without significant tachycardia.
Selective α2-blockade—↑NA release resulting in hypertension.
α-blockade also results in miosis and nasal stuffiness.
α-blockade in the bladder and prostate leads to decreased resistance to the flow
of urine.
9. Therapeutic uses of alpha sympatholytics
• Hypertension: Selective alpha -blockers like prazosin are used in
the treatment of hypertension. Phenoxybenzamine or
phentolamine can be used in hypertensive crisis.
• Pheochromocytoma: Pheochromocytoma is an adrenal medullary
tumour which secretes large amounts of catecholamines resulting
in hypertension. The tumour has to be removed surgically.
• Phenoxybenzamine and phentolamine are used for the
preoperative management of the patient and during the
operation. Inoperable cases are put on long-term treatment with
phenoxybenzamine.
10. Therapeutic uses of alpha sympatholytics
• Raynaud's disease: A patient with Raynaud's disease experiences
pain in the extremities, for example, the fingers, when temperatures
drop. In Raynaud's disease, smaller arteries that supply blood to your
skin undergo vasoconstriction, restrictive blood circulation to
affected areas.
• Migraines are severe, recurring, and painful headaches. Symptoms
may include nausea, vomiting, difficulty speaking, numbness or
tingling, and sensitivity to light and sound.
12. Therapeutic uses of alpha sympatholytics
• Frostbite may occur when skin is exposed to extreme cold, at
times combined with high winds, resulting in vasoconstriction. The
associated decrease in blood flow does not deliver sufficient heat
to the tissue to prevent the formation of ice crystals.
• Benign prostatic hypertrophy (BPH) Blockade of α1 receptors in
the bladder, prostate and urethra reduce resistance to urine
outflow. Prazosin, tamsulosin and alfuzosin are useful in patients
who cannot be operated upon.
16. Adverse effects of α-blockers
•Postural hypotension, palpitation, nasal stuffiness,
miosis, impaired ejaculation and impotence.
Postural hypotension— is when your blood pressure drops when you
go from lying down to sitting up, or from sitting to standing
17. DALES ADRENALINE REVERSAL PHENOMENON
• Henry Dale was demonstrated adrenaline reversal phenomenon in
1906 by using extract of Ergotoxin on anaesthetized experimental
cat. A characteristic series of changes observed in arterial blood
pressure if adrenaline administered intravenously in anaesthetized
cat.
18. • We should also keep in mind that-
• At higher concentration, adrenaline acts on all receptors (α1, α2,
β1,β2, β3).
• But at lower concentration, adrenaline acts selectively on β2 –
receptors (because β2 are more sensitive)
Receptors Location
Pharmacological action of
Adrenaline
α1
Blood vessels (Veins, Arteries,
Arterioles, Capillaries)
Vasoconstrictions
(increases blood pressure)
β2 Blood vessels (Arteries)
Vasodilatation
(fall in blood pressure)
19. Phase 1:
• If adequate dose of adrenaline is given intravenously in anaesthetized
cat, then there will be rise in blood pressure due vasoconstriction
(α1, β2 effect). The cardiac output, heart rate, conduction velocity
and excitability of heart also increased. This is because initially the
concentration of adrenaline is high. So adrenaline will act on both α1,
β2 receptors.
• Within few second level of adrenaline will decrease due to its rapid
metabolism and neuronal re-uptake. At lower concentration only
action of β2 will predominant. So only fall in Blood pressure seen. So
at this level you can observe initially rise in blood pressure and then
after fall in blood pressure. This is called Biphasic response. (refer
figure)
20. Phase 2:
• After biphasic response, if we administer non-selective alpha
blocker-Ergotoxine intravenously in anaesthetized cat, then it
blocks the α1 receptors on blood vessels (veins, arteries,
arterioles, capillaries).
• Hence Ergotoxine shows vasodilation and fall in blood pressure
i.e. hypotensive action. (refer figure)
21.
22. Phase 3:
• After alpha blocking action, if adequate dose of adrenaline is given
intravenously in same anaesthetized cat, then there will be fall in blood
pressure due vasodilation (β2 effect).
• This is because Ergotoxine already blocks the α1 receptors on blood
vessels. So adrenaline will act only on β2 receptors located on blood
vessels (arteries) to show vasodilation and fall in blood pressure i.e.
hypotensive action. (refer figure)
23. So as We have seen in adrenaline reversal phenomenon-
• 1. First give adrenaline and observe biphasic response
2. Second We give non-selective alpha blocker
3. At last We give adrenaline again and observe only
fall in BP due to unopposed β2 action.
28. • β blockers competitively block the actions of adrenaline on beta
receptors innervated organs especialy heart.
• β1 Blocking action reduces heart rate (-ve chronotropic effect),
myocardial contractility (-ve ionotropic effect), conduction velocity and
excitability of the heart.
• Beta blockers decrease myocardial oxygen consumption by decreasing
heart rate, blood pressure and contractility.
29. • β blockers also inhibit the Renin secretion from the kidney nephrons.
Thereby they produce vasodilation and fall in blood pressure.
• β blockers decrease outflow of the sympathetic impulses from
sympathetic nerves.
• β blockers produce resetting of baroreceptors on the aortic body on the
aorta.
• Therefore β blockers shows antihypertensive activity.