Hypertension or high blood pressure is a chronic medical condition in which the blood pressure in the arteries is elevated i.e. 140/90 mmHg systolic /diastolic pressure.
High blood pressure has damaging effect on the heart, brain, kidneys and eyes.
Drugs used to lower blood pressure is known as antihypertensive drugs.
Antihypertensive drug therapy has improved remarkably in the last 50 years.
Before 1950, less effective and less tolerated antihypertensive drugs were available.
Veratrum and sodium thiocyanate could lower BP, but were toxic and difficult to use.
The ganglion blockers that were developed in the 1950s were effective, but inconvenient.
Reserpine was a breakthrough, but produced mental depression.
The therapeutic potential of hydralazine was not tapped fully because of the marked side effects when it was used alone
First choice drug in all grade of essential as well as renovascular hypertension (except renal artery stenosis).
This class of medicine works by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart.
Most patient require low doses which are well tolerated.
Example - Captopril, Enalapril, Lisinopril, Ramipril, Perindopril, Benazepril, Fosinopril, Quinapril, Trandolapril.
Large hydrophobic N-heterocyclic ring increase potency.
Ring showed contain –COOH group to mimic ACE substrate.
The Zn2+binding group may be
sulfhydryl (-CH2SH) like captopril
Di-carboxylate like in enalapril, lisinopril and quinapril
Phosphate like fosinopril
Sulfhydryl group shows superior binding to Zn ion and produces side effect like skin rash, taste disturbance etc.
Esterification of carboxylate or phosphate produce orally bioactive prodrug.
Large heterocyclic ring and hydrophobic ring generally N-containing increase potency and alter pharmacokinetic parameter.
Generally pyrrolidine ring is present (E.g. – Captopril, Enalapril)
The N-group must contain –COOH group to mimic the C-terminal carboxylate of ACE substrate.
X is usually methyl to mimic the side chain of aniline . This type of drug do not require prodrug for oral activity.
Drugs are : Losatran, Candesartan, Irbesartan, Valsartan, Telmisartan
The most prominent action of angiotensin II is vasoconstriction.
The two types of angiotensin II receptors are AT1 and AT2 , most of the action of angiotensin II are mediated by AT1 receptor.
Angiotensin receptor blockers do not affect bradykinin production.
Oral bioavibility – 33% (1st pass metabolism) It is partially carbonylated in liver to an active metabolism (E3174).
All ARB prevent and reverse all known effect of angiotensin-II including slow CNS effect, release of catecholamine, secretion of aldosterone, direct and indirect renal effect.
Telmisartan has additional PPAR-ϒ agonistic activity. This activity can help patient with dysglycemia.
There are thee functional groups that are the most important part f
Medicinal Chemistry of Antihypertensive agents pptxSameena Ramzan
introduction of Hypertension, Pharmacological classification of antihypertensives, Chemical classification, Drug synthesis profile (including every class), Mechanism of Action(including every class), Uses, Adverse Effects, Structure Activity Relationship(including every class)
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
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
The presentation describes the mechanism action of diuretics with the class of Carbonic anhydrase inhibitors, loop diuretics, thiazides, osmotic and potassium diuretics.
Medicinal Chemistry of Antihypertensive agents pptxSameena Ramzan
introduction of Hypertension, Pharmacological classification of antihypertensives, Chemical classification, Drug synthesis profile (including every class), Mechanism of Action(including every class), Uses, Adverse Effects, Structure Activity Relationship(including every class)
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
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,...Dr. Ravi Sankar
ANTI HYPERTENSIVE AGENTS [MEDICINAL CHEMISTRY] BY P.RAVISANKAR, HYPERTENSION,TYPES,CAUSES OF HYPERTENSION, CLASSIFICATION, MECHANISM OF ACTION, SAR, ACE INHIBITORS, ARB , DIURETICS(WATER PILLS), TIPS TO STOP SILENT KILLER.
BY P. RAVISANKAR, VIGNAN PHARMACY COLLEGE, VADLAMUDI, GUNTUR,A.P, INDIA.
The presentation describes the mechanism action of diuretics with the class of Carbonic anhydrase inhibitors, loop diuretics, thiazides, osmotic and potassium diuretics.
Hypertension pharmacotherapy part 2 pptPranatiChavan
First-line medications used in the treatment of hypertension include diuretics, angiotensin-converting enzyme (ACE) inhibitors or angiotensin receptor blockers (ARBs), beta-blockers, and calcium channel blockers (CCBs). Some patients will require 2 or more antihypertensive medications to achieve their BP target. As per special consideration, modified treatment is given in the presentation.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
Adrenergic drugs have many uses. They are used to increase the output of the heart, to raise blood pressure, and to increase urine flow as part of the treatment of shock. Adrenergics are also used as heart stimulants.
Hypertension is the most common cardiovascular disease determined by increase blood pressure (pressure exerted by blood against the wall of a blood vessel )in arteries.
The onset of hypertension is defined as having a blood pressure of 140/90 mm Hg or greater .
Hypertension is the major risk factor for coronary artery disease, heart failure, stroke and renal failure.
Hypertension pharmacotherapy part 2 pptPranatiChavan
First-line medications used in the treatment of hypertension include diuretics, angiotensin-converting enzyme (ACE) inhibitors or angiotensin receptor blockers (ARBs), beta-blockers, and calcium channel blockers (CCBs). Some patients will require 2 or more antihypertensive medications to achieve their BP target. As per special consideration, modified treatment is given in the presentation.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
Adrenergic drugs have many uses. They are used to increase the output of the heart, to raise blood pressure, and to increase urine flow as part of the treatment of shock. Adrenergics are also used as heart stimulants.
Hypertension is the most common cardiovascular disease determined by increase blood pressure (pressure exerted by blood against the wall of a blood vessel )in arteries.
The onset of hypertension is defined as having a blood pressure of 140/90 mm Hg or greater .
Hypertension is the major risk factor for coronary artery disease, heart failure, stroke and renal failure.
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.
Hello friends, This is Akhila Gundabathini!! Here is the detailed information about antihypertensive drugs. Hope this presentation is helpful for you.. Thank You
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
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.
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!
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
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.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
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
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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
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
3. Introduction
Hypertension or high blood pressure is a chronic medical condition in which the blood pressure
in the arteries is elevated i.e. 140/90 mmHg systolic /diastolic pressure.
High blood pressure has damaging effect on the heart, brain, kidneys and eyes.
Drugs used to lower blood pressure is known as antihypertensive drugs.
Blood Pressure Systolic Pressure Diastolic Pressure
Normal < 120 <80
Prehypertension 120-139 80-89
Hypertension stage-I 140-159 90-99
Hypertension stage-I >160 100
Hypertensive Crisis >180 >100
4. History
Antihypertensive drug therapy has improved remarkably in the last 50 years.
Before 1950, less effective and less tolerated antihypertensive drugs were available.
Veratrum and sodium thiocyanate could lower BP, but were toxic and difficult to use.
The ganglion blockers that were developed in the 1950s were effective, but inconvenient.
Reserpine was a breakthrough, but produced mental depression.
The therapeutic potential of hydralazine was not tapped fully because of the marked side
effects when it was used alone
6. ACE Inhibitors
First choice drug in all grade of essential as well as renovascular
hypertension (except renal artery stenosis).
This class of medicine works by causing relaxation of blood vessels as
well as a decrease in blood volume, which leads to lower blood pressure
and decreased oxygen demand from the heart.
Most patient require low doses which are well tolerated.
Example - Captopril, Enalapril, Lisinopril, Ramipril, Perindopril, Benazepril,
Fosinopril, Quinapril, Trandolapril.
11. SAR of ACE inhibitors
Sulfhydryl NH with dicarboxylate Phosphonate group
12. Large hydrophobic N-heterocyclic ring increase potency.
Ring showed contain –COOH group to mimic ACE substrate.
The Zn2+binding group may be
sulfhydryl (-CH2SH) like captopril
Di-carboxylate like in enalapril, lisinopril and quinapril
Phosphate like fosinopril
Sulfhydryl group shows superior binding to Zn ion and produces side
effect like skin rash, taste disturbance etc.
SAR of ACE inhibitors
13. Esterification of carboxylate or phosphate produce orally bioactive prodrug.
Large heterocyclic ring and hydrophobic ring generally N-containing increase
potency and alter pharmacokinetic parameter.
Generally pyrrolidine ring is present (E.g. – Captopril, Enalapril)
The N-group must contain –COOH group to mimic the C-terminal carboxylate of
ACE substrate.
X is usually methyl to mimic the side chain of aniline . This type of drug do not
require prodrug for oral activity.
SAR of ACE inhibitors
14. Angiotensin Receptor Blocker
Drugs are : Losatran, Candesartan, Irbesartan, Valsartan, Telmisartan
The most prominent action of angiotensin II is vasoconstriction.
The two types of angiotensin II receptors are AT1 and AT2
, most of the action of angiotensin II are mediated by AT1 receptor.
Angiotensin receptor blockers do not affect bradykinin production.
Oral bioavibility – 33% (1st pass metabolism)
It is partially carbonylated in liver to an active metabolism (E3174).
16. MOA
All ARB prevent and reverse all known effect of angiotensin-II
including slow CNS effect, release of catecholamine, secretion
of aldosterone, direct and indirect renal effect.
Telmisartan has additional PPAR-ϒ agonistic activity. This
activity can help patient with dysglycemia.
18. SAR
There are thee functional groups that are the most important
part for bioactivity of ARBs.
The first one is the imidazole ring.
The second is bi-phenyl methyl group.
The third one is the tetrazole group.
20. SAR
Most ARBs have same functional groups but the difference in biochemical and
physiological effect is due to its substituents.
Acidic group (Imidazole) group is thought to mimic either phenol or carboxylate of
angiotensin-II.
In the bi-phenyl series the tetrazole and carboxylate group must be in ortho
position for optimal activity(the tetrazole group is superior in term of metabolic
stability, lipophilicity and oral bioavibility).
The n-butyl group provides hydrophobic binding .
N-butyl group can be replaced with either ethyl ether or an propyl group as seen in
Telmisartan, olmestran.
21. Direct Renin Inhibitor
Drugs: Aliskiren, Remikiren and Enalkiren.
Inhibition of function of renin substrate and proposed that inhibition of renin would be
beneficial in treatment of hypertension.
Aliskerin
22. MOA
• Aliskerin directly inhibit renin that stops the formation of
angiotensin-I from angiotensinogen.
• It is a rate limiting step in this pathway.
• Inhibition of renin angiotensin pathway through any of this pathway
shows to cause increase in concentration of renin.
24. Uses
Approved for the treatment of hypertension.
Used as monotherapy with combination of other anti-hypertensive drugs
like hydrochlorothiazide, amlodipine or valsartan.
Aliskerin is available alone or in combination with other hypertensive
agent like diuretics, CCBs, and ARBs.
25. Diuretics
Diuretics are the drugs that induces the urine formation and decrease the
reabsorption.
Diuresis replace plasma and E.F.C. volume by 5-15% and decrease cardiac
output.
26. Thiazide Diuretics
• Thiazides and thiazide-like diuretics reduce the risk of death, stroke,
heart attack, and heart failure due to hypertension
• Chlorothiazide, hydrochlorothiazide, Bendroflumethiazide,
methyclothiazide etc.
27. MOA
It increase the elimination of Na+ and H2O
The blood volume decreases and cardiac output also
decreases.
Chlorothiazide is the longest acting drug of the class.
29. SAR
1 – Sulfonyl group is essential but can be replaced by carbonyl group.
2 - alkyl group form potent drug.
3 – This position decides potency and duration of action. Increased when substituted with
lipophilic group.
4 – Presence of double bond between 3rd and 4th position increases potency.
6 – Substitution with electron withdrawing group like Cl, Br, NO2 are required for activity.
7 – Sulfonyl group is essential for activity. Removal cause decrease in activity.
31. Calcium Channel Blockers (CCBs)
Drugs : Verapamil, Diltiazem, Nifedipine, Amlodipine, Felodipine etc.
Calcium channel blockers (CCBs) are a group of medicines commonly
prescribed to treat conditions of the heart and blood vessels, such as
hypertension (high blood pressure), angina, some abnormal heart
rhythms.
32. MOA
Smooth muscle relaxation – Smooth muscle depolarization by inward Ca2+
through L-type voltage gated ion channel and CCBs blocks the L-type
calcium channels.
Negative chronotropic, Inotropic and dromotropic action on heart.
They lower the B.P. by decreasing peripheral resistance without
compromising cardiac output.
38. SAR
• R1 should be unsubstituted.
• Replacement of R2 with a basic amin ethyl ether chain resulting in increasing
potency of drug
• Replacement of R2 with aryl group causes the loss of activity
• R3 and R5 replacement with alkoxy carbonyl group gives more optimum activity.
• Variation in Alkyl component of easter group (ROOC) decrease in activity.
• R4 position substitution must be phenyl ring