To be able to describe:
Hypertension: its prevalence, cardiovascular mortality risks & complications.
Anti hypertensive drugs: classification, mechanism of action & side effects
D) In collecting duct, sodium enters through sodium channels & transferred into interstitial fluid by sodium pump, while potassium is pumped in opposite direction and moves through potassium channels into tubular fluid. Aldosterone stimulates these processes by increasing synthesis of messenger RNA that encodes for sodium channel and sodium pump proteins. The potassium-sparing diuretics exert their effects via two mechanisms: amiloride and triamterene inhibit the entrance of sodium into the principal cells, whereas spironolactone blocks the mineralocorticoid receptor and thereby inhibits sodium reabsorption and potassium secretion.
Introduction to diuretics.
Therapeutic approaches.
Normal physiology of urine formation.
Classification of drugs .
Mechanism of action of Acetazolamide.
Mechanism of action of Thiazides.
Mechanism of action of Loop diuretics.
Mechanism of action of potassium sparing diuretics &aldosterone antagonists.
CONGESTIVE HEART FAILURE
Congestive heart failure is a syndrome that can be caused by a variety of abnormalities
Coronary artery disease
Heart attack
Cardiac myopathy
Conditions that overwork the heart
Hypertension
Valve disease
Thyroid disease
Kidney disease
Congenital birth defects
Diabetes
In the usual form of heart failure, the heart muscle has reduced contractility. This produces a reduction in cardiac output, which then becomes inadequate to meet the peripheral demands of the body.
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.
Introduction to diuretics.
Therapeutic approaches.
Normal physiology of urine formation.
Classification of drugs .
Mechanism of action of Acetazolamide.
Mechanism of action of Thiazides.
Mechanism of action of Loop diuretics.
Mechanism of action of potassium sparing diuretics &aldosterone antagonists.
CONGESTIVE HEART FAILURE
Congestive heart failure is a syndrome that can be caused by a variety of abnormalities
Coronary artery disease
Heart attack
Cardiac myopathy
Conditions that overwork the heart
Hypertension
Valve disease
Thyroid disease
Kidney disease
Congenital birth defects
Diabetes
In the usual form of heart failure, the heart muscle has reduced contractility. This produces a reduction in cardiac output, which then becomes inadequate to meet the peripheral demands of the body.
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.
This Slideshare includes the introduction of congestive heart failure, signs and symptoms, pathogenesis, epidemiology, etiology, pathophysiology, classification of drugs which is used to manage CHF, and recent drugs used to manage CHF.
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)
This slide talks about the different pharmacological properties of Antihypertensive Drugs. The classification and examples of these drugs are also given in detail.
Diuretic and Urinary alkalizes-Dr.Jibachha Sah,M.V.ScDr. Jibachha Sah
Dr.Jibachha Sah,M.V.Sc (Veterinary pharmacology),Lecture,College of Veterinary science,NPI,Bhojard,Chitwan,Nepal.This is part of lecture note on veterinary pharmacologyAUTONOMIC AND SYSTEMIC PHARMACOLOGY, Sixth Semester, B.V.Sc & A.H 6th semester.
Dr.Jibachha sah,Email: jibachhashah@gmail.com,Mobile:00977-9845024121
Ovarian tumors are abnormal growths on the ovaries, the female reproductive organs that produce eggs. Ovarian tumors can be noncancerous (benign) or cancerous (malignant). Many things can make you more likely to develop an ovarian tumor.
Gestational trophoblastic disease (GTD) is a group of rare diseases in which abnormal trophoblast cells grow inside the uterus after conception. In gestational trophoblastic disease (GTD), a tumor develops inside the uterus from tissue that forms after conception (the joining of sperm and egg).
This Slideshare includes the introduction of congestive heart failure, signs and symptoms, pathogenesis, epidemiology, etiology, pathophysiology, classification of drugs which is used to manage CHF, and recent drugs used to manage CHF.
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)
This slide talks about the different pharmacological properties of Antihypertensive Drugs. The classification and examples of these drugs are also given in detail.
Diuretic and Urinary alkalizes-Dr.Jibachha Sah,M.V.ScDr. Jibachha Sah
Dr.Jibachha Sah,M.V.Sc (Veterinary pharmacology),Lecture,College of Veterinary science,NPI,Bhojard,Chitwan,Nepal.This is part of lecture note on veterinary pharmacologyAUTONOMIC AND SYSTEMIC PHARMACOLOGY, Sixth Semester, B.V.Sc & A.H 6th semester.
Dr.Jibachha sah,Email: jibachhashah@gmail.com,Mobile:00977-9845024121
Ovarian tumors are abnormal growths on the ovaries, the female reproductive organs that produce eggs. Ovarian tumors can be noncancerous (benign) or cancerous (malignant). Many things can make you more likely to develop an ovarian tumor.
Gestational trophoblastic disease (GTD) is a group of rare diseases in which abnormal trophoblast cells grow inside the uterus after conception. In gestational trophoblastic disease (GTD), a tumor develops inside the uterus from tissue that forms after conception (the joining of sperm and egg).
A number of medical conditions have high association with kidney stone disease. Any type of chronic diarrhea state (such as Crohn's disease, gastric bypass, inflammatory bowel disorder), primary hyperparathyroidism, obesity, gout, and even diabetes have all been linked to increased risk of kidney stone disease.
The lymph node examination is performed with circular motion, identifying pain, and swollen ganglia or induration. For the anterior cervical lymph node exam, palpate the lymph nodes in the neck using circular motion over the underlying tissues in each area.
Position patient supine, with the hand on the side you're examining behind their head.
Palpate the asymptomatic breast first.
Palpate using the flat palmar surface of your fingers.
Palpate using a systematic technique to ensure you examine all of the breast regions.
The abdominal examination consists of four basic components: inspection, palpation, percussion, and auscultation. It is important to begin with the general examination of the abdomen with the patient in a completely supine position. The presence of any of the following signs may indicate specific disorders.
The lymph node examination is performed with circular motion, identifying pain, and swollen ganglia or induration. For the anterior cervical lymph node exam, palpate the lymph nodes in the neck using circular motion over the underlying tissues in each area.
LOWER LIMB EXAMINATION ,INSPECTION,PALPATION,TONE ,POWER, The neurologic examination is typically divided into eight components: mental status; skull, spine and meninges; cranial nerves; motor examination; sensory examination; coordination; reflexes; and gait and station.
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough
Opioid analgesia is indicated for the treatment of moderate to severe pain. An opioid is a medication that relieves pain by binding to opioid receptors in the central nervous system spinal cord and peripheral nervous system.
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough
Opioid analgesia is indicated for the treatment of moderate to severe pain. An opioid is a medication that relieves pain by binding to opioid receptors in the central nervous system spinal cord and peripheral nervous system.
To explain pathogenesis of Bipolar Disorders
To classify drugs used for treatment of Bipolar Disorders
To describe mechanism of action of drugs used for treatment of Bipolar Disorders
To enlist side effects of drugs used for treatment of Bipolar Disorders.
Indications: Bipolar, cyclothymia, schizoaffective, impulse control and intermittent explosive disorders.
Classes: Lithium, anticonvulsants, antipsychotics
Which you select depends on what you are treating and again the side effect profile.
To explain pathogenesis of Depression
To describe the synthesis, degradation and reuptake mechanism of 5HT
To classify Antidepressant drugs
To describe mechanism of action of Antidepressants.
To enlist side effects of Antidepressants.
The symptoms of depression are feelings of sadness and hopelessness, s well as the inability to experience pleasure in usual activities, changes in sleep patterns and appetite, loss of energy, and suicidal thoughts. Mania is characterized by the opposite behavior: enthusiasm, anger, rapid thought and speech patterns, extreme self-confidence, and impaired judgment.
To explain pathogenesis of Schizophrenia
To classify antipsychotic drugs
To describe mechanism of action of antipsychotics
To enlist side effects of antipsychotic drugs.
Atypical antipsychotics have mixtures of pharmacological properties.
Beyond antagonism of 5HT2A and D2 receptors, they interact with multiple other receptor subtypes for both dopamine and serotonin, and have effects on other neurotransmitter systems as well.
Some of these multiple pharmacological properties can contribute to the therapeutic effects of atypical antipsychotics (e.g., antidepressant, antimanic, and anxiolytic effects), whereas others can contribute to their side effects (e.g,. sedative-hypnotic and cardiometabolic effects).
No two atypical antipsychotics have identical binding properties, which probably helps to explain why they all have distinctive clinical properties.
Learning Objectives:
After completing the topic, the student will be able to:
• Recognize the importance of hemostasis and thrombosis in health and disease.
• Describe the process that leads to platelet aggregation.
• Classify anti-platelets drugs and the mechanism by which they inhibit platelet
aggregation.
• Describe indications, contraindications, drug interactions & adverse effects of anti-
platelets drugs.
• Describe treatment recommendations for antiplatelet agents
Acetylsalicylic Acid (Aspirin)
• Irreversibly inhibits COX1 and, in higher doses, COX2.
• COX1 inhibition (main antithrombotic mechanism); the formation of prostaglandin H2 is blocked, thus
thromboxane A2 cannot be synthesized (TxA2 stimulates platelets aggregation).
Drug interactions
• Co-administration of non-selective COX1 inhibitors may impair its efficacy.
• About one-third of patients receiving aspirin manifest treatment failure (Thrombotic Complication or
Death).
Adverse Events
• Resulting from rebound thrombocyte activation after aspirin withdrawal.
• Single binding site and does not influence other thrombocyte receptors results in aspirin having less
antithrombotic effect than many other agents
Define Angina pectoris, its type and causes
Explain mechanism of action of Nitrates, calcium channel blockers and
Beta Blockers?
3. Describe the clinical uses and adverse effects of anti Anginal drugs
4. Explain why the combination of a nitrate with a beta blocker or a calcium blocker may be more effective than either alone
To be able to describe:
Cholesterol synthesis, source & metabolism
Hyperlipidemia – definition & normal values.
Anti hyperlipidemic drugs: its classification, mechanism of action & side effects.
The natural history of atherosclerosis might involve coronary plaque rupture / erosion, thrombus formation and vessel lumen occlusion, clinically recognized as acute coronary syndrome (ACS). International guidelines strongly recommend early statin administration in patients admitted for ACS. In addition to lowering circulating levels of low-density lipoprotein cholesterol (LDL-c), statin treatment was shown to promote plaque stabilization or regression in several ways, including reduction in necrotic lipid core, anti-inflammatory effects and improvement in endothelial function.
Update on the efficacy of statin treatment in acute coronary syndromes by Rosa, Gian Marco; Carbone, Federico; Parodi, Antonello; Massimelli, Elena A; Brunelli, Claudio; Mach, François (more...) European journal of clinical investigation, 05/2014, Volume 44, Issue 5, 501 - 515
Currently, only one medication has been approved to treat COVID-19. No cure is available for COVID-19. Antibiotics aren't effective against viral infections such as COVID-19. Researchers are testing a variety of possible treatments.
The FDA has approved the antiviral drug remdesivir (Veklury) to treat COVID-19 in hospitalized adults and children who are age 12 and older in the hospital. Remdesivir may be prescribed for people who are hospitalized with COVID-19 and need supplemental oxygen or have a higher risk of serious illness. It's given through a needle in the skin (intravenously).
The FDA has authorized a drug called Paxlovid that includes nirmatrelvir – a drug that blocks the activity of a specific enzyme needed for the virus that causes COVID-19 to replicate – and an antiviral drug called ritonavir that helps slow the breakdown of nirmatrelvir. Paxlovid is authorized to treat mild to moderate COVID-19 in people age 12 and older who are at higher risk of serious illness. The medications are taken by mouth as pills.
The FDA has authorized another drug called molnupiravir to treat mild to moderate COVID-19 in adults who are at higher risk of serious illness and who aren't able to take other treatment options. The medication is taken by mouth as a pill.
The FDA has authorized the rheumatoid arthritis drug baricitinib (Olumiant) to treat COVID-19 in some cases. Baricitinib is a pill that seems to work against COVID-19 by reducing inflammation and having antiviral activity. Baricitinib may be used in people who are hospitalized with COVID-19 who are on mechanical ventilators or need supplemental oxygen.
The U.S. National Institutes of Health has recommended the corticosteroid dexamethasone for people hospitalized with severe COVID-19 who are on supplemental oxygen or need mechanical ventilation. Other corticosteroids, such as prednisone, methylprednisolone or hydrocortisone, may be used if dexamethasone isn't available.
In some cases, the drugs remdesivir, tocilizumab or baricitinib may be given with dexamethasone in hospitalized people who are on mechanical ventilation or need supplemental oxygen.
The FDA has also authorized convalescent plasma therapy with high antibody levels to treat COVID-19. Convalescent plasma is blood donated by people who've recovered from COVID-19. Convalescent plasma with high antibodies may be used to treat some hospitalized people ill with COVID-19 who are either early in their illness or who have weakened immune systems.
Monoclonal antibodies aren't effective against treating COVID-19 caused by the omicron variant. These drugs were previously used to treat mild to moderate COVID-19 in people who had a higher risk of developing serious illness due to COVID-19.
Many people with COVID-19 may have mild illness and can be treated with supportive care. Supportive care is aimed at relieving symptoms and may include:
Pain relievers (ibuprofen or acetaminophen)
Cough syrup or medication
Rest
Fluid intake.
At the end of the lecture, students should be able to:
▶ Classify Antihistamines
Define mechanism of action and uses of Antihistamines
Enlisting the adverse effects of Antihistamines.
Describe the Pharmacology of Expectorants and Mucolytics
Explain the mechanism of action ,clinical uses and toxicity of cough suppressants
▶ Histamine is a chemical messenger mostly generated
in mast cell that mediates a wide range of cellular responses, Including;
-Allergic and inflammatory reactions,
-Gastric acid secretion
- Neurotransmission in parts of the brain
▶ Histamine has no clinical application but antihistamines have important therapeutic applications.
Adverse effects are a significant issue in the treatment of both cytotoxic drugs and newer targeted therapies, leading to dose reductions, dose delays, and treatment discontinuation.
Toxicity can reduce quality of life, jeopardies treatment adherence, and necessitate dose reductions and dose delays, all of which can have a negative impact on treatment response and outcome.
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2. OBJECTIVES
To be able to describe:
Hypertension: its prevalence, cardiovascular mortality risks &
complications.
Anti hypertensive drugs: classification, mechanism of action &
side effects
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 2
4. RISK FACTORS ( NON – MEDICINAL
TREATMENT )
Multifactorial.
Predisposing Factors:
Age, Sex, Gender, Race.
Genetic Factors
Fetal Factors
Lifestyle / Environmental
Factors
Humoral Mechanisms
4
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
5. A) In proximal tubule, carbonic anhydrase catalyzes reversible conversion of hydrogen ion &
bicarbonate to carbon dioxide and water, thereby enabling the reabsorption of sodium
bicarbonate.
This process is inhibited by carbonic anhydrase inhibitors such as
acetazolamide.
B) In thick ascending limb of the loop of Henle, Na + ,K + ,2Cl − symporter transports sodium,
potassium, and chloride ions into tubular cells, and then sodium is transferred to interstitial fluid by
sodium pump. Potassium back-diffuses into lumen and contributes to positive transepithelial potential
that drives paracellular calcium and magnesium reabsorption.
By inhibiting symporter, loop diuretics reduce back-diffusion of
potassium and increases excretion of calcium and magnesium.
Sites and Mechanisms of Action of Diuretics
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 5
6. C) In distal tubule , sodium is transported into tubular epithelial cells
by Na + ,Cl −symporter and then is transferred to interstitial fluid by
sodium pump. Na + ,Cl −symporter is inhibited
by thiazide diuretics.
D) In collecting duct, sodium enters through sodium channels & transferred into interstitial fluid by sodium
pump, while potassium is pumped in opposite direction and moves through potassium channels into tubular
fluid. Aldosterone stimulates these processes by increasing synthesis of messenger RNA that encodes for
sodium channel and sodium pump proteins. The potassium-sparing diuretics exert their effects
via two mechanisms: amiloride and triamterene inhibit the entrance of sodium into the
principal cells, whereas spironolactone blocks the mineralocorticoid receptor and thereby
inhibits sodium reabsorption and potassium secretion.
Sites and Mechanisms of Action of Diuretics
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 6
7. LOOP DIURETICS: FUROSEMIDE
Potent diuretic, to treat
hypertension when thiazide diuretics is
not effective or contraindicated.
In severe hypertension.
In renal insufficiency.
In cardiac failure.
In cirrhosis where sodium retention is
marked.
Spironolactone
Aldosterone receptor antagonists.
The potassium sparing diuretics have a
relatively low natriuretic effect and are
primarily employed in combination with a
thiazide or loop diuretic to reduce
potassium excretion and prevent
hypokalemia.
7
POTASSIUM SPARING DIURETICS
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
9. ß
blocke
rs
Non-selective (ß1, ß2)
blockers:
Pure
Blockers
Sotalol,
Timolol,
Nadolol
With MSA
Propanolol
with ISA*,
MSA**, PA*** can
activate beta
receptors
Pindolol (MSA** ±)
Carteolol
Cardio selective ß1
blockers
Pure
blocker
s
Atenolol,
Bisoprolol (most
selective) Esmolol
(shortest action)
With
MSA
Metaprol
ol
With ISA*
and
MSA**
Acebutol
ol
Drugs that
block both α
and ß
receptors
Labetalol
,
Carvedil
ol
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
9
* ISA – Intrinsic sympathetic activity. ** MSA – Membrane stabilizing activity. *** PA – Partial
agonist
10. Used frequently because they are relatively safe and effective in patients
who suffer from angina or with a history of myocardial infarction.
These drug are cardio protective and rarely causes orthostatic
hypotension.
Relatively safe in hepatic, renal insufficiency or hematopoietic toxicity
10
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
11. BETA BLOCKERS
Relative contraindications
Asthma/COPD
Decompensated CHF
Raynaud’s phenomenon
Peripheral vascular disease
Depression
Side effects
Tiredness
Cold hands and feet
Impotence and sexual
dysfunction
May mask the effect of
hypoglycemia in DM
11
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
12. Angiotensinogen
Angiotensin I
Angiotensin II
Vasoconstriction
Aldosterone
secretion
↑ TPR
↑ Na & water
retention
↑ blood pressure
Angiotensin converting enzyme
Bradykinin
Inactive
metabolites
Vasodilation
↓ TPR
↓ Blood pressure
↑Prostaglandin
synthesis
ACE
Inhibitors
Renin
Aliskiren
ARBs
Spironolactone
12
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
16. ACE INHIBITORS & RECEPTOR BLOCKERS
≈ ACE inhibitors ↓BP by ↓ peripheral vascular resistance without reflex increase of cardiac
output, rate or contractility.
≈ ACE inhibitors ↓ both arterial & venous pressure by ↓ cardiac after & pre load.
≈ Used inpatients with coexisting heart failure, myocardial infarction, diabetes mellitus
≈ By reducing circulating Angiotensin II levels, ACE inhibitors also ↓ the secretion of
Aldosterone, resulting in ↓ sodium and water retention.
The receptor blockers, Blocks the receptors for Angiotensin1
16
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
17. VASODILATORS
17
Examples
Mechanism
of Action
Actions
Adverse
Effects
•Non-selective
block of L-type
calcium channels
•Block vascular
calcium channels
& cardiac calcium
channels
•Causes nitric
oxide release
•Metabolite opens
K channels in
vascular smooth
muscles
•Verapamil
•Diltiazem
•Nifedipine
•Amlodipine
•Felodipine
•Hydralazine
•Minoxidil
•↓cardiac rate &
↓cardiac output
•↓vascular
resistance
•Vasodilation
•↓vascular
resistance
•Reflex
tachycardia
•Constipation
•Dizziness
•Headache
•fatigue
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
19. CALCIUM CHANNEL BLOCKERS: MECHANISM OF ACTION:-
Three types Ca+ channels in smooth
muscles – voltage sensitive, receptor
operated and leak channel
Voltage sensitive are again 3 types – L-
type, T-type and N-type
Normally, L-type of channels admit
Ca+ and causes depolarization
(excitation-contraction) coupling
through phosphorylation of myosin
light chain – contraction of vascular
smooth muscle – elevation of BP
Calcium channel blockers
BLOCK L-type channel
Smooth muscle relaxation
Negative Chrono- tropic effects in heart
19
• ↓ myocardial contraction force, which reduces
myocardial oxygen requirements.
• Causes peripheral vasodilatation.
• ↓ Left ventricular stress & oxygen
requirements of myocardium.
• ↓ heart rate by decreasing activity in Sinoatrial
& Atrioventricular nodal tissues. This gives
additional benefit in controlling
supraventricular tachycardia.
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
20. CALCIUM CHANNEL BLOCKERS:
Nifedipine.
Causes arteriolar vasodilation. Minimal effects
on cardiac conduction or heart rate.
They can cause flushing , headache, hypotension
and peripheral edema.
Verapamil.
Slows cardiac conduction directly and thus
decrease heart rate and oxygen demand but
they are weaker vasodilator.
Causes constipation. Contraindicated in patient
with preexisting depressed cardiac function or AV
conduction abnormalities.
20
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
21. CALCIUM CHANNEL BLOCKERS. SIDE EFFECTS
The calcium channel blockers are generally safe and are as effective as
beta-adrenergic blockers or diuretics in the treatment of mild to moderate
hypertension
Channel blockers are well-tolerated; minor side-effects include dizziness,
headache, flushing, and edema and are most usually associated with the
dihydropyridines
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 21
• Efficacy can be enhanced by combination with other types of antihypertensive.
• Diltiazem or verapamil with beta-adrenergic blockers can lead to
AV block, cardiac depression, bradycardia
Verapamil with digoxin (can increase levels of digoxin, and can cause AV block)
22. CALCIUM CHANNEL BLOCKERS –
CURRENT STATUS
As per JNC 7 CCBs are not 1st line of antihypertensive unless indicated –
ACEI/diuretics/beta blockers
However its been used as 1st line by many because of excellent tolerability and
high efficacy
Preferred in elderly and prevents stroke
They are next to ACE inhibitors in inhibition of albuminuria and prevention of
diabetic nephropathy
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 22
23. VASODILATORS. HYDRALAZINE.
Acts on arteries and arterioles, this results in a decreased peripheral resistance,
which in turn prompts reflex tachycardia and cardiac output.
Indicated for moderately severe hypertension.
Adverse effects include nausea, vomiting, sweating, arrhythmia.
A lupus like syndrome can occur with high dosage, but it is reversible on
discontinuation of drug
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 23
24. VASODILATORS. MINOXIDIL.
Acts by hyperpolarization of smooth muscles and thereby relaxation of Smooth Muscles by acting on potassium
channels
Reflex tachycardia may be severe and may require the concomitant use of a diuretic or β-blocker.
Orally not used any more reserved for severe to malignant hypertension that is refractory to other drugs.
It also causes hypertrichosis (the growth of body hair). This drug is in use topically to treat male pattern baldness.
Topically as 2-5% lotion/gel and takes months to get effects
MOA of hair growth:
Enhanced microcirculation around hair follicles and also by direct stimulation of follicles
Alteration of androgen effect of hair follicles
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 24
25. Αlpha ¹-blockers
are second line of therapy when others agents are
ineffective or contraindicated
25
Examples
Mechanism
of Action
Actions
Adverse
Effects
•Doxazosin
•Prazosin
•Terazosin
•Selectively
blocks a-1
adrenoceptors in
arterioles &
Venules
•Prevents
sympathetic
vasoconstrictio
n
•↓peripheral
vascular
resistance
•↓arterial
pressure
•Reflex
Tachycardia
•↑risks of
congestive
heart failure
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
26. SYMPATHETIC NERVE TERMINAL
BLOCKERS
26
Examples
Mechanism
of Action
Actions
Adverse
Effects
•Reserpine
•Guanethidine
•Blocks vesicular
amine transporter
in noradrenergic
nerves
•Depletes
transmitter stores
•Interferes with
amine release &
replaces
nonepinephrine
in vesicles
•↓All
sympathetic
effects
epically
cardiovascular
•↓Blood
pressure
•Psychiatric
depressions
•GIT
disturbances
•Severe
hypotension
•Sexual
dysfunction
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
27. CENTRALLY ACTING ADRENERGIC DRUGS.
METHYLDOPA.
It diminishes the adrenergic
outflow from central α-2a
receptors to decrease
sympathetic outflow from the
CNS, leading to reduced
peripheral resistance.
Cardiac output is not
decreased and flow to vital
organs is not diminished by
its use.
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE 27
Especially valuable in the treatment
of hypertensive patients with renal
insufficiency & in pregnancy
induced hypertension.
Common side effects include
sedation and drowsiness. Postural
hypotension sometime occurs,
particularly in volume depleted
patients.
28. 28
Hypertension Canada’s 2016 CHEP Guidelines for Blood Pressure Measurement, Diagnosis, Assessment of Risk,
Prevention and Treatment of Hypertension
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE
29. REFERENCE
S:
2014 Hypertension Guideline Stands to Simplify Treatment
https://www.google.com.sa/url?sa=t&rct=j&q=&esrc=s&source=web&cd=4&cad=rja&uact=8&ved=0CEMQFjAD&url
=http%3A%2F%2Fwww.aafp.org%2Fnews%2Fhealth-of-the-public%2F20131218hypertensiongdln.html&ei=O3hoU-
dPIXfOKqmgRA&usg=AFQjCNG0EHrm_MpsPteAvvtZd6Xz49oyPw
2014 Evidence based guidelines for Management of hypertension. American Society of Hypertension
https://www.google.com.sa/url?sa=t&rct=j&q=&esrc=s&source=web&cd=1&cad=rja&uact=8&ved=0CC4QzwIwAA&url=https%3A%2F%2
Fscholar.google.com%2Fscholar%3Fes_sm%3D122%26um%3D1%26ie%3DUTF-8%26lr%26q%3Drelated%3AMwILUs-
KtklAkM%3Ascholar.google.com%2F&ei=O3hoU-PdPIXfOKqmgRA&usg=AFQjCNHqIcse2AhWWafoOr0s7pdhrEaiyQ.
(ACCEPTED MANUSCRIPT) Hypertension Canada’s 2016 CHEP GUIDELINES FOR BLOOD PRESSURE MEASUREMENT,
DIAGNOSIS, ASSESSMENT OF RISK, PREVENTION & TREATMENT OF HYPERTENSION. CANADIAN JOURNAL OF
CARDIOLOGY, REF CJCA 2053
Basic & Clinical Pharmacology : 15th edition by Katzung
Rang & Dale Pharmacology; 8TH EDITION
Lippincott's Pharmacology: 6TH EDITION
For queries: a.mehdi@frpmc.edu.pk
29
THANK
YOU
Department of Pharmacology FAZAIA RUTH PFAU MEDICAL COLLEGE