This document discusses the autonomic nervous system. It begins by defining the somatic and autonomic nervous systems, and their components. It then compares the somatic and autonomic nervous systems. The functions of the sympathetic and parasympathetic nervous systems are described. Cholinergic and adrenergic receptors are explained. The document concludes by discussing cholinergic and adrenergic drugs, including their classifications, mechanisms of action, uses and side effects.
The presentation describes the mechanism action of diuretics with the class of Carbonic anhydrase inhibitors, loop diuretics, thiazides, osmotic and potassium diuretics.
The presentation describes the mechanism action of diuretics with the class of Carbonic anhydrase inhibitors, loop diuretics, thiazides, osmotic and potassium diuretics.
Sympathomimetics or Adrenergic Agonists (Introduction, Classification, Adenor...Ahmad Naeem
Sympathomimetics or adrenergic agonists (introduction, classification, adenoreceptors, neurtransmission, direct acting, indirect acting, mixed action agonists, summary)
Drugs that partially or completely mimic the effects of transmitter substances of the sympathetic nervous system. On the basis of chemical structure we divide Sympathomimetics into
1. Catecholamine
2. Non-Catecholamine
Adrenergic drugs that activate adrenergic receptors are termed
as sympathomimetics, Some sympathomimetics directly activate
adrenergic receptors (direct-acting agonists), while others act
indirectly by enhancing release or blocking reuptake of norepinephrine (indirect-acting agonists). Adrenergic transmission is restricted to the sympathetic division of the ANS. There are three closely related endogenous catecholamine's (CAs).
1. Noradrenaline (NA): It acts as transmitter at postganglionic sympathetic sites (except sweat glands, hair follicles and some vasodilator fibers) and in certain areas of brain.
2. Adrenaline (Adr) It is secreted by adrenal medulla and may have a transmitter role in the brain.
3. Dopamine (DA) It is a major transmitter in basal ganglia, limbic system, CTZ, anterior pituitary, etc. and in a limited manner in the periphery
Mechanism of Action , Therapeutic uses and adverse effects of Adrenergic Agonists
1. Direct-acting agonists:
These drugs act directly on α or β receptors, producing effects similar to those that occur following stimulation of sympathetic nerves or release of epinephrine from the adrenal medulla.
Examples of direct-acting agonists include epinephrine,
norepinephrine, isoproterenol, and phenylephrine.
2. Indirect-acting agonists:
These agents may block the reuptake of norepinephrine or cause the release of norepinephrine from the cytoplasmic pools or vesicles of adrenergic neuron. The norepinephrine then traverses the synapse and binds to α or β receptors.
Examples of reuptake inhibitors and agents that cause norepinephrine release include cocaine and amphetamines,
respectively.
3. Mixed-action agonists:
Ephedrine and its stereoisomer, pseudoephedrine, both stimulate adrenoceptors directly and release norepinephrine
from the adrenergic neuron.
Oriel (Levocetirizine Dihydrochloride Tablets) is used in the symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and urticaria in adults and children aged 6 years and above.
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones
Sympathomimetics or Adrenergic Agonists (Introduction, Classification, Adenor...Ahmad Naeem
Sympathomimetics or adrenergic agonists (introduction, classification, adenoreceptors, neurtransmission, direct acting, indirect acting, mixed action agonists, summary)
Drugs that partially or completely mimic the effects of transmitter substances of the sympathetic nervous system. On the basis of chemical structure we divide Sympathomimetics into
1. Catecholamine
2. Non-Catecholamine
Adrenergic drugs that activate adrenergic receptors are termed
as sympathomimetics, Some sympathomimetics directly activate
adrenergic receptors (direct-acting agonists), while others act
indirectly by enhancing release or blocking reuptake of norepinephrine (indirect-acting agonists). Adrenergic transmission is restricted to the sympathetic division of the ANS. There are three closely related endogenous catecholamine's (CAs).
1. Noradrenaline (NA): It acts as transmitter at postganglionic sympathetic sites (except sweat glands, hair follicles and some vasodilator fibers) and in certain areas of brain.
2. Adrenaline (Adr) It is secreted by adrenal medulla and may have a transmitter role in the brain.
3. Dopamine (DA) It is a major transmitter in basal ganglia, limbic system, CTZ, anterior pituitary, etc. and in a limited manner in the periphery
Mechanism of Action , Therapeutic uses and adverse effects of Adrenergic Agonists
1. Direct-acting agonists:
These drugs act directly on α or β receptors, producing effects similar to those that occur following stimulation of sympathetic nerves or release of epinephrine from the adrenal medulla.
Examples of direct-acting agonists include epinephrine,
norepinephrine, isoproterenol, and phenylephrine.
2. Indirect-acting agonists:
These agents may block the reuptake of norepinephrine or cause the release of norepinephrine from the cytoplasmic pools or vesicles of adrenergic neuron. The norepinephrine then traverses the synapse and binds to α or β receptors.
Examples of reuptake inhibitors and agents that cause norepinephrine release include cocaine and amphetamines,
respectively.
3. Mixed-action agonists:
Ephedrine and its stereoisomer, pseudoephedrine, both stimulate adrenoceptors directly and release norepinephrine
from the adrenergic neuron.
Oriel (Levocetirizine Dihydrochloride Tablets) is used in the symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and urticaria in adults and children aged 6 years and above.
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
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
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
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
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.
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
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
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!
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.
2. Nervous System
Peripheral nervous Central nervous
system (PNS) system (CNS)
Afferent Efferent Brain Spinal
(sensory) (motor) cord
Somatic nervous Autonomic nervous
system (SNS) system (ANS)
Sympathetic Parasympathetic Enteric nervous system
(thoraco-lumbar) (Cranio-sacral)
2
3. Difference between Somatic NS and ANS
Somatic NS
concerned with
consciously controlled
functions
e.g. Movement , Respiration
Innervate skeletal muscle
consist of a single motor
neuron
Has no peripheral ganglia
Effect is always excitation
Autonomic NS
activities are not under conscious
control
*concerned primarily with visceral
functions: Regulation of the heart,
temp., secretary glands, digestion,
metabolism
Innervate visceral organs
consist of two motor neurons in
series
Has ganglia b/n pre-synaptic and
post synaptic
Effect is both excitatory &
inhibitory 3
4. ANS Functions
Sympathetic nervous system functions
1. Regulating the cardiovascular system
Increase cardiac output
Causes vasoconstriction
2. Regulate body temperature
By regulating blood flow to the skin
By promoting secretion of sweat, thereby helping the body
to cool
By inducing piloerection (erection of hair) can promote
heat conservation
4
5. Sympathetic nervous system functions……..
3. Implementing the “ fight – or – flight” reaction which consists
Increasing heart rate and blood pressure
Shunting blood away from the skin and viscera into skeletal
muscles
Dilating the bronchi to improve oxygenation
Dilating the pupil to enhance visual acuity
Mobilizing stored energy
thereby providing glucose for the brain and fatty acids for
muscles
5
7. Parasympathetic nervous system functions
maintains essential bodily functions
• such as digestive processes, elimination of wastes and is
required for life
usually acts to oppose or balance the actions of the sympathetic
division
– Is dominant over the sympathetic in “rest and digest”
situations
7
8. Functions of parasympathetic nervous system
• Slowing the heart rate
• Increase gastric secretion
• Emptying of the bladder
• Emptying of the bowel
• Focusing the eye for near vision
• Constricting the pupil
• Contracting bronchial smooth muscle
8
10. Important terminology
Cholinergic neurons
– are neurons which synthesis, store & release Ach
Cholinomimetics
– are those agents which mimic the activity of Ach
– Are also called parasympathomimetics
Chlinoreceptors
– are binding site for Ach & cholinomimetics
Cholinoreceptor antagonists (anticholinergic or parasympatholytics)
– are agents which block/ oppose the actions of Ach
10
11. Adrenergic neurons
– are neurons which synthesis, store & release EP and NE
Adrenomimetics
– are agents which mimic the activities of NE
– Are also called sympathomimetics
Adrenoceptors
– are binding sites for NE, EP & adrenomimetics
Adrenoceptor antagonists
– are agents which antagonize the activities of NE, EP
– are also called sympatholytics/sympathoplegics
11
12. Autonomic receptors
• Includes cholinergic and adrenergic receptors
Cholinergic receptors
• Two types: muscarinic & nicotinic cholinoceptors
Muscarinic receptors
• Are activated by muscarine (plant alkaloid)
• Found in many visceral organs such as smooth muscle cells,
cardiac cells, exocrine glands, CNS, Autonomic ganglia
• Further classified into M1, M2, M3, M4 & M5
12
15. Cholinergic receptors ………..
Nicotinic receptors
• Activated by nicotine (tobacco alkaloid)
• Based on their location nicotinic Ach receptors are grouped
into two types
– Nn (at ganglia)
– Nm (at neuromuscular junction)
15
16. Adrenoceptors
– Interact with NE, EP & other related drugs
– Two types
1. α-adrenoceptors (α-1, α-2)
2. β-adrenoceptors (β-1, β-2, β-3)
16
19. Steps in cholinergic neurotransmission
1. Synthesis of acetyl choline (ACh)
From choline and acetyl CoA which catalyzed by choline
acetyl transferase
2. Up take to storage vesicle
3. Release of acetyl choline by exocytosis
4. Binding to receptor
5. Degradation of acetyl choline by acetylcholinesterase /AChE
To acetate & choline
6. Recycling of choline
19
22. Cholinergic Drugs
1. Cholinomimetic drugs
• Similar effects to acetylcholine (Ach)
• Elicit all or some of the effects of Ach
• Classified as
1. Direct acting
Cholinergic receptor agonists
2. Indirect acting
Acetyl cholinesterase enzyme inhibitors (AchEIs) also
called anticholinesterase
22
24. Direct Cholinergic Agonists
Choline esters: Methacholine, Carbachol, Bethanechol
Alkaloids: Muscarine, Pilocarpine, Arecholine
Differ from Ach
Have longer duration of action
Effective orally & parenterally
Relatively more selective in their actions
But, still less potent than Ach
24
25. Cholinomimetic drugs: therapeutic use
a) Pilocarpine
• Use: Glaucoma, xerostomia, reverse mydriatic effects of
atropine
• Dose: 1–2 gtts TID in eye 1–6 times/d
• SE: Temporary reduction in visual acuity, headache
b) Bethanecol
• Use:
1) Urinary retention - because relax urinary sphincter
2) Gastric atony
3) Paralytic ileus
• CI: gastric ulcer, recent surgery of the bowel, asthma
• Dose: 10-15mg po tid or QID, 5mg SC QID
25
29. 29
Treatment
– Maintenance of respiration
– Atropine parenterally in large doses
– Pralidoxime chloride (2-PAM, or 2-
pyridine aldoxime methyl chloride)
effective as an antidote for
poisoning by phosphate ester
AChEIs
30. Contraindication to cholinomimetics
– Bronchial asthma
– GIT hyper-motility
– Peptic ulcer disease
– Coronary artery disease
– Hypotension
– Bradycardia
– Hyperthyroidism: may cause atrial fibrillation
30
32. 2. Cholinergic antagonists
Cholinergic blockers or anti-cholinergic drugs
Bind to cholinergic receptor but do not trigger the usual
receptor mediated intracellular effects
These drugs are classified as:
– Anti-muscarinic agents
– Ganglionic blockers (Nn)
– Neuromuscular blocking drugs (Nm)
32
33. 33
Target Effect Use Drug
Glands secretion PUD Pirenzepine, Telenzepine
Eye Mydriasis Ophthalmic
examination
Atropine, Tropicamide,
Cyclopentolate
Urinary
bladder
tone with
constriction
Urinary
incontinency
Tolferodine, Darifenacin,
Fesoterodine
GI smooth
muscle
motility with
tone
Hyper motility Hyoscine
CNS Block all
muscarnic
-motion sickness
-parkinsonism
-Hyoscine/ scopolamine
-Benzotropine
Respiratory Relaxation Asthma Ipratropium, Tiotropium
Antimuscarinics…
34. Neuromuscular blocking drug
• Succinyl choline, Vecuronium, Mivacurium, Pancuronium,
Rapacurium, Gallamine
• These drugs generally block the action of acetylcholine and
produce different effect.
1) Adjuvant in general anesthesia: muscle relaxation
2) Control ventilation i.e. facilitation of endotracheal intubation
3) Prevention of trauma in electro shock therapy of psychiatric
disorder E.g. Succinyl choline
34
36. Adrenergic drugs
1. Adrenomimetics
• Drugs which activate the effects of adrenergic SN
stimulation
• Also called sympathomimetics
• Have a wide range of effects
36
38. – Adrenomimetics can be classified into three groups
1. Direct acting adrenomimetics
– Directly interact & stimulate adrenoceptors
– Their effects are not reduced by prior treatment with
reserpine or guanethidine
– Prior treatment with reserpine or guanethidine can increase
their effects due to receptor upregulation
Examples: NE, EP, DA, IP, Dobutamine, phenylephrine,
albuterol, salmeterol, metaraminole, terbutalin, clonidine,
oxymethazoline
38
39. 2. Indirect acting adrenomimetics
• Don’t interact with the adrenoceptors
• Increase availability of NE/EP to stimulate the adrenoceptors
• Their action emanates from one of the following
– Displace stored neurotransmitters from the vesicles
E.g. amphetamine, tyramine, methamphetamine
– Inhibit reuptake of neurotransmitters into the neuron
E.g. cocaine, TCAs
– Inhibit the metabolizing enzymes (MAO & COMT)
E.g. selegiline, rasagiline, entacapone, tolcapone
• Their response is abolished by prior administration of reserpine or
guanethidine
39
40. 3. Mixed acting adrenomimetics
– Work by both direct & indirect mechanisms
– Increase release of NE & also activate adrenoceptors
E.g. ephedrine
– Their responses are blunted but not abolished by prior
treatment with reserpine or guanethidine
40
42. Catecholamines
Derivatives of β-phenyl ethylamine
When 3,4 OH is added to phenyl ring (3,4 OH)→ catechol ring
Hence, catechol ethyl amine→catecholamines
Phenyl ring
42
Ethyl amine
43. Catecholamines…..
These compounds share the following properties:
High potency: by activating α or β receptors
Rapid inactivation: metabolized (MAO&COMT)
- have a brief of action when given parentrally, and are
ineffective when administered orally because of
inactivation
Poor penetration into the CNS
- Catecholamines are polar & do not cross BBB
- Nevertheless have some clinical effects that are
attributed to the action of CNS.
43
44. Adrenaline/Epinephrine
• Stimulate both α with β receptor
Use:
1) Asthma (β2 - selective are better)
2) Anaphylactic shock
3) Potentiation with prolongation of action of local anesthetic
(by absorption)
4) Restore normal cardiac rhythm in case of cardiac arrest
5) Topical hemostatic agent (control superficial bleeding)
• Dose:
SC, IM 0.1mg - 0.5mg
IV - 0.25mg (in emergency an IV can be used but should be
diluted and given by IV infusion because of cardiac
arrhythmia. 44
45. α1 adrenergic agonists
• Phenylephrine
• Xylomethazoline
• Methoxamine
• Use:
1) Nasal decongestant
2) To raise BP in hypotensive state & shock
45
46. Alpha 2 - adrenergic agonist
Methyldopa (aldomet)
• MOA - sympathetic outflow,
• Use: moderate to severe hypertension in pregnant mom.
• Dose: initial 250mg 2-3X/day
– Usual dose range 250mg -1000mg po bid.
• AE:
– headache, fatigue, sleep disturbance
46
47. β2 Agonist
Include
• Salbutamol/albuterol – rapid acting
• Terbutaline
• Formetrol & Salmetrol – long acting (nocturnal asthma)
• Ritodrine-for Preterm Labour
Use
1) Asthma, albuterol 2 puffs every 4-6 hours as needed (90
mcg/inhalation)
2) Premature labour, terbutaline 2.5-5 mcg/minute over 12hrs
47
48. Ephedrine
• Both α with β agonist (mixed acting)
Use:
1) Asthma - 25-50mg PO 3-4 PRN
2) To treat hypotension
3) Used to relieve broncho-constriction with mucosal
congestion (incorporated in cough syrup)
48
49. 2. Adrenoceptor antagonists
Works by competing with adrenomimetics for access to
adrenoceptors
– Reduce effects produced by both sympathetic nerve
stimulation & exogenous adrenomimetics
• Adrenoceptor antagonists
– Don’t prevent release of NE/EP from adrenergic neurons
– Are not catecholamine depleting agents
– Are also called, sympathoplegics, sympatholytics
49
52. α1 - Blockers
• Use:
– Hypertensive crisis
– Short term control of BP in pheochromocytoma
– Drug choice for HTN with benign prostate hyperplasia
(BPH)
• SE:
orthostatic hypotension, headache, water retention
(relaxation), first dose syncope (fainting)
52
53. -Blockers
A. Non selective -Blockers
– Are also called 1st generation -blockers
– Propranolol, Timolol, Nadolol, Pindolol
B. Cardio selectives [1Blockers ]
– Are called 2nd generation -blockers
– Atenolol, Bisoprolol, Esmolol, Metoprolol
C. Non-selective adrenergic blockers( & Blockers)
– Are also called 3rd generation -blockers
– Carvedilol, Labetalol, Bucindolol, Nebivolol
Longest half life: Nadolol, Cartelol (24 hrs)
Shortest half life: Esmolol (10 min) 53
54. • Some of the β-blockers have some intrinsic activity &
membrane stabilizing activity
– May be considered as partial antagonists
– Examples
• Pindolol
• Acebutolol
• Bucindolol
54
55. β – Blocker: Therapeutic use
Hypertension- alone or with diuretic
For angina treatment: by decreasing cardiac work with
oxygen demand
For chronic heart failure… only metoprolol, bisoprolol & carvedilol
For cardiac arrhythmia
Glaucoma treatment: Timolol
Anti anxiety related to performance: Propranolol
Prophylaxis of migraine
55
60. Assignment
1. Management of Shock (types, pathophysiology of shock
and their management).
2. Pharmacology of anesthetics (local anesthetics and
general anesthetics)
3. Management of Neurodegenerative disorders
(Alzheimer’s disease, Huntington disease, multiple
sclerosis….)
4. New drug development process (preclinical trial and
clinical trials)
5. Management of selrected cardiovascular disorders
(myocardial infraction, ischemic stroke, haemorrhagic
stroke, valvular heart disease).
60