Adrenergic agonists and antagonists act on adrenergic receptors. Agonists like epinephrine and norepinephrine directly stimulate receptors, whereas antagonists like prazosin competitively block receptor activation. These drugs have widespread effects throughout the body due to the sympathetic nervous system's role in functions like heart rate, blood pressure, bronchodilation and uterine contraction. Care must be taken with certain drugs that can cause severe side effects like hypotension or bronchospasm.
Lecture covers the pharmacology of anticholinergic drugs. Includes classification, therapeutic uses, adverse effects of anticholinergics. Atropine has been described as prototype drug.
Lecture covers the pharmacology of anticholinergic drugs. Includes classification, therapeutic uses, adverse effects of anticholinergics. Atropine has been described as prototype drug.
New product dedisions provide a dear path to the business. New product development
astep by step process. A Complete idea is required behind new product.
1 1deal Generation: The development of a product starts with the concept and idea.
The remaining process is depending on that idea.
2 Screening of Idea: This step is cruial to ensure that unsuitable ideas, for whatever
reason, are rejected as soon as possible. Ideas need to be considered objectively,
ideally by a group or committee.
3. Concept Development and Testing: After having an idea, next is the sreening
stage. The idea should now convert into concept. It has depth information which can
be visualizing by the consumer.
4. Anaysis of business: After finalization of concept, a business case needs to be kept
algTStogether to consider whether the new service /product will be gainful.
2665.Product Development If the nev product is approved, it will be approved to the
2marketing and technical development step.
6. Test Marketing: Market testing (test marketing or) is different to consumer testing.
in that it introduces the product that follows proposed plan of marketing.
od7. Commercialization: When the concept has been tested and developed, final
0decisions are required to move the product to its introduction into the market.
8. Launch: A detailed plan of launch is required for this step. This is the important
stage for success of a product
New Drug Development
So In present business atmosphere, it is more important to take smart decisions for
business. Innovative approaches and new products can put an organization on proper
pathway and to make a big success if appropriately analyzed and executed. Make it simpler
(Fig.2.1).0
Following parameters should keep in mind for a better decision:
Analyzing existing service and product portfolio frequently.
Knowing the position of functions of business, projects of departments and
initiatives.
Understanding the distribution of funds and assessing efficiency.
Having understanding of market for new opportunities and possible competition.
2.B PRODUCT BRANDING, PACKAGING AND LABELLING DECİSIONs
2.8.1 Branding
Branding has its existence from ancient era. According to Nilson (2000), the first example
of branding is found in the oil lamps' manufacture on the Greek islands thousands of years
back. Brand elements are name, sign, term, symbol, design or distinguishing characteristics.
Brand is not only a graphical design or a logo; it is the unique identity of the product.
By American Marketing Association, Brand can be defined as name, term, sign, symbol
or design, or a combination of them intended to identijy the goods and services of one seller or
group of sellers and to diferentiate them from those of other sellersa54
Branding is a process, where a company generates loyalty among consumers in the
market. Brands are designed with a motive to communicate customers the reason for the
existence of their product. Brand should have a strong connection with customers;
Announcement about my previous presentations - Thank youAreej Abu Hanieh
ANNOUNCEMENT Thank you for all of you, my followers who sent me messages with a lot of love and appreciations, I finally graduated after 6 years of studying in Birzeit University , In doctor of Pharmacy department I hope all of you benefited from all the presentations posted before Thank you a new PharmD GraduatedAreej ^^
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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!
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.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
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.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
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
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
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.
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.
3. Adrenergic neurons release NE as the primary
neurotransmitter
Adrenal medulla NE is converted to epinephrine,
they are both stored and released upon stimulation
in the ratio of 80% epinephrine and 20% NE
Found in the CNS and sympathetic nervous system
Adrenergic receptors located presynaptically on the
neuron or postsynaptically on the effector organ are
the sites of action of adrenergic drugs
4. 1. Synthesis of
norepinephrine
2. Storage of NE in vesicles
3. Release of NE
4. Binding to receptors
5. Removal of NE
6. Metabolism by the
enzymes Catechol O-
methyltransferase
(COMT) and monoamine
oxidase (MAO)
5. α1
◦ Present on postsynaptic membranes of effector organs
◦ Constriction of smooth muscle, vasoconstriction, increased
blood pressure, total peripheral resistance
◦ Subdivided to α1A, α1B, α1C, and α1D
α2
◦ Located on presynaptic nerve endings
◦ Stimulated α2 cause feedback inhibition of NE release
◦ Subdivided to α2A, α2B and α2C
β1 (Heart, Kidney)
◦ Tachycardia, Increased myocardial contractility, Renin release
β2 (Bronchi, blood vessels, uterus)
◦ Vasodilation, Bronchodilation, Relax uterine smooth muscles
β3
6.
7. Desensetization of adrenoceptors: Reduction
in the responsiveness of these receptors due
to prolonged exposure to catecholamines (NE
and epinephrine)
Mechanisms for desentization
◦ Sequestration of the reseptors, so they are not
available for binding
◦ Downregulation of receptors by destruction or
decreased synthesis
◦ Inability to couple to G protein
8. These drugs exert their effects via direct stimulation of
the adrenergic receptors (1, 2, 1, 2) leading to a wide-
range of pharmacological effects.
Endogenous sympathomimetic drugs include:
Epinephrine (adrenaline), norepinephrine (noradrenaline),
dopamine.
Catecholamines: Sympathomimetic amines
(NE, epinephrine, dopamine and isoprotrenol)
Highly potent in stimulating adrenergic receptors
Rapidly inactivated by COMT and MAO
Poor CNS penetration
Non catecholamine adrenergic agonists have longer
duration of action
10. Epinephrine
◦ Commonly used in therapy
◦ Strengthens the contractility of myocardium (β1)
(positive inotrpic effect)
◦ Increases the rate of contraction (β1)
(positive chronotropic effect)
◦ Increase cardiac output (β1)
◦ Promotes renin release, increase blood pressure
(β1 on kidney)
◦ Constriction of arterioles (α1)
◦ Dilation of vessels going to liver and skeletal muscles (β2)
◦ Bronchodilation (β2)
◦ Hyperglycemia (β2 in liver)
11. Therapeutic uses
◦ Bronchospasm, emergency for acute asthma
◦ Anaphylactic shock
◦ Cardiac arrest
◦ Anesthetics, to increase the duration of local anesthesia
(vasoconstriction)
Pharmacokinetics
◦ Rapidly metabolized by COMT and MAO
◦ Administered IV for emergencies
◦ Can be administered IM or SC but not oral
Adverse effects:
◦ cardiac arrhythmia
◦ CNS effects: anxiety, tremor.
12. Acts mostly on α receptors
Effects
◦ Vasoconstriction (α1 effect)
◦ Increase total peripheral resistance
◦ Increase blood pressure
◦ Reflex bradycardia due to stimulation of baroreceptor
Therapeutic uses
◦ Shock, NE increases peripheral resistance and blood
pressure
Administered IV
Adverse effects: similar to epinephrine
13. β1 and β2 agonist, nonselective, rarely used
Increase heart rate and force of contraction,
increasing cardiac output
Used to stimulate the heart in emergencies
(atrioventricular (AV) block or cardiac arrest)
Adverse effects: similar to epinephrine
14. Activates α and β receptors
A neurotransmitter that occurs naturally in the
CNS and adrenal medulla
Increases heart rate and force of contraction
(positive chronotropic and inotropic effects)
Rapidly metabolized by MAO and COMT
Used for
◦ Shock treatment
◦ Hypotension
◦ Severe congestive heart failure
Adverse effects
◦ Hypertension
◦ Arrhythmia
15. Dobutamine
◦ β1 agonist
◦ Increases cardiac rate and output
◦ Uses:
Increase cardiac output in acut congestive hear failuer
For inotropic support after cardiac surgery
◦ Adverse effects:
Similar to epinephrine
16. Oxymetazoline
◦ Stimulates α1 and α2 receptors
◦ Used locally in the eye or nose as a vasoconstrictor
◦ Mechanism: Directly stimulates α receptors on
blood vessels in nasal mucosa and conjunctiva to
reduce blood flow and decrease congestion
◦ Found in many over the counter short-term nasal
spray decongestants
◦ Found in opthalmic solution for relief of redness of
the eye
◦ Rebound congestion and tolerance can occur with
long term use
17. Phenylphrine
◦ Stimulates α1 receptors
◦ Vasoconstrictor
◦ Used in opthalmic solutions for mydriasis
◦ Used as nasal decongestant
◦ Can be used to raise blood pressure and to
terminate episodes of supraventricular tachycardia
18. Clonidine
◦ α2 agonist
◦ Used in essential hypertension to lower blood pressure
because of its action in the CNS
◦ Acts centrally to inhibit sympathetic activity and outflow
to periphery
◦ Side effects
Lethargy
Sedation
◦ Abrupt discontinuation leads to rebound hypertension
19. Albuterol and terbutaline
◦ β2 agonists
◦ Used as bronchodilators, administered by a metered dose
inhaler
◦ Terbutaline is used as uterine relaxant to suppress premature
labor (off label use)
◦ Side effects:
Tremor
Restlessness
Salmeterol and formoterol
◦ β2 agonists
◦ Long acting bronchodilators, administered by a metered dose
inhaler
20. Inhibit reuptake of norepinephrine or cause
norepinephrine release from presynaptic terminal
Amphetamine
◦ CNS stimulant
◦ Can increase blood pressure by stimulation of α1 and β1
receptors
◦ Used in hyperactivity of children, narcolepsy
Cocaine:
◦ Inhibits reuptake of norepinephrine
◦ CNS stimulant
21. Cocaine
◦ Highly addictive
◦ Blocks reuptake of epinephrine, serotonin and dopamine
into presynaptic terminals
◦ Prolongs the peripheral and central actions of these
neurotransmitters
◦ Dopaminergic effects in the brain’s pleasure system
(limbic system) produce the euphoria associated with
cocaine
22.
23. Induce the release of norepinephrine from
presynaptic terminals and activate adrenergic
receptors on the postsynaptic membrane
Ephedrine and pseudoephedrine
◦ Release stored NE from nerve endings and directly
stimulate α and β receptors
Pseudoephedrine is used orally to treat nasal
and sinus congestion
24. Adrenergic antagonists, adrenergic blockers,
sympatholytics: bind to adrenoceptors but do
not trigger the usual receptor-mediated
intracellular effects.
These drugs bind to receptors reversibly or
irreversibly and prevent the activation of
receptors by epinephrine and norepinephrine.
25. Affect blood pressure
Blocking α-receptors reduces the sympathetic tone
of the blood vessels decreasing the peripheral
vascular resistance
Lowered blood pressure induces reflex tachycardia
27. Nonselective, binds to α1 and
α2
The block is irreversible and
noncompetetive, to overcome
the block, the body has to
synthesize adrenoceptors
(requires a day or longer)
28. Actions
◦ Prevents vasoconstriction of peripheral blood
vessels by endogenous cathecholamines
◦ Reflex tachycardia occurs
◦ α2 receptors are also blocked causing increased
cardiac output
◦ Phenoxybenzamine use for hypertension was
discontinued because it was unsuccessful in
maintaining lower blood pressure due to blockade
of α2 and α1 receptors
29. Uses:
◦ Treatment of pheochromocytoma (a catecholamine
secreting tumor of cells derived from adrenal
medulla)
◦ Used for Raynaud’s disease and frostbite
Adverse effects
◦ Postural hypotension
◦ Nasal stuffiness
◦ Nausea and vomiting
30. Competitively blocks α1 and α2 receptors
Causes reflex tachycardia
Used for pheochromocytoma (adrenal medulla
tumor)
Adverse effects
◦ Postural hypotension
◦ Arrhythmia
31. Selective competitive blockers of α1 receptors
Prazosin, terazosin and doxazosin are useful for
treating hypertension
Tamsulosin and alfuzosin are indicated for
benign prostatic hypertrophy (BPH)
Effects
◦ Decrease peripheral vascular resistance by causing
relaxation of arterial and venous smooth muscle
◦ Cause minimal change in cardiac output
◦ Can cause first dose syncope (fainting)
First dose administered should be adjusted to 1/3 the
regular dose, or given at bedtime
32. Uses:
◦ Congestive heart failure, by dilating the arteries and
veins these drugs reduce the preload and the afterload
leading to increased cardiac output and reduction of
pulmonary congestion
◦ Prazosin, terazosin and doxazosin are useful for
treating hypertension due to blockade of α1 receptors
◦ Tamsulosin (selectivity for α1 on prostate) and
alfuzosin are indicated for benign prostatic
hypertrophy (BPH) because the blockade of α-
receptors decreases the smooth muscle tone of the
bladder neck and prostate and improves urine flow
33. Adverse effects
◦ Dizziness
◦ Lack of energy
◦ Orthostatic hypotension
◦ Tachycardia
◦ Inhibition of ejaculation due to
blockade of α-receptors in the
ejaculatory ducts
36. Non selective β-antagonists
More potent than propranolol
Nadolol has a very long duration of action
Timolol is used topically for glaucoma
◦ Inhibits aqueous humor production
37. Selective β1 antagonists
Cardioselective (at low doses)
No β2 antagonism (no bronchoconstriction)
Little effect on peripheral resistance
Therapeutic use
◦ Hypertension (to lower blood pressure)
◦ Angina (increase exercise tolerance)
38. Antagonists with partial agonist activity
Have intrinsic sympathomimetic activity
Acebutolol is β1 selective antagonist
Pindolol is non selective β-blocker
Used for hypertensive patients with moderate
bradycardia because they cause less heart rate
decrease
39. Antagonists of both α and β
◦ Block α1 receptors causing peripheral vasodilation and
reducing blood pressure
Used for hypertension
Labetalol can be used in pregnancy-induced
hypertension
Intravenous labetalol can be used for
hypertensive emergencies
Adverse effects:
◦ Orthostatic hypotension
40.
41. • In patients with AV conduction defects, β1 blockers may
cause life-threatening bradyarrhythmias.
• Abrupt discontinuation of long-term β1 blockers use in
angina can exacerbate angina and may increase risk of
sudden heart attack.
• β2 receptor blockade can worsen bronchoconstriction in
asthmatic populations.
• β1-selective blockers or non-selective β blockers with partial
β2 agonism produce less bronchoconstriction than non-
selective β blockers.
42. Reserpine
◦ Blocks the transport of the biogenic amines
norepinephrine, dopamine and serotonin from the
cytoplasm into storage vesicles in adrenergic nerves
◦ Causes depletion of biogenic amines
◦ Impairs sympathetic function
◦ Long duration of action
Guanethidine
◦ Blocks the release of stored norepinephrine
◦ Causes orthostatic hypotension