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Dr Shahid Saache
JR1, Dept Of Pharmacology
B.J.G.M.C PUNE
INTRODUCTION
ANS also called visceral, vegetative or involuntary
nervous system
Distributed widely through out body
Regulates autonomic function without conscious
control
In periphery nerves, ganglia & plexuses that
innervates heart, BV, glands, other visceral organs & SM
ADRENERGIC BLOCKERS
End of postganglionic
sympathetic synapse-
adrenergic receptors
“Block or decrease the effects of sympathetic nerve
stimulation, endogenous catecholamines and adrenergic
drugs”
Adrenergic receptor blockers antagonize receptor action
of epinephrine & related drugs
Adrenergic neurone blocking agents act by interfering
with release of adrenergic transmitter
Central sympatholytics
Ganglion blockers
Chemical sympathectomy
Neuron blocking drugs
Guanethidine
Act mainly by preventing release of NE at nerve endings
Pharmacological sympathectomy
Uses- HTN, glaucoma, neuropathic pain,& given IM for
htnsive crises, severe pre eclampsia
ADRs- severe postural hypotension, diarrheoa, renal
impairment
Bretylium
Causes initial release of NE→ blocks adrenergic
transmission by preventing NE release from adrenergic
nerve endings
Blocks K+ channels- class III antiarrhythmic activity
Guanadrel
False neurotransmitter- accumulated, stored & released
like NE but is inactive at adrenergic receptors
M/A- Replacement of NE with inactive transmitter
ADRs- hypotension, fatigue ,lassitude, Sexual
dysfunction, Diarrhoea
Reserpine
Inhibit vesicular catecholamine transporter
Sedation, inability to concentrate- MC ADRs occasionally
psychotic depressionsuicide
Recent interest -at low doses, in combination with
diuretics, for hypertension
Metyrosine
Inhibits tyrosine hydroxylase
Adjuvant to phenoxybenzamine & other α adrenergic
blockers for pheochromocytoma & in preoperative
preparation for resection of pheochromocytoma
ADR- crystalluria
Central sympatholytics
α Methyldopa
MOA: Converted to α methyl NE which acts on α2
receptors in brain & causes inhibition of adrenergic
discharge in medulla – ↓PVR & ↓BP
Various adverse effects – cognitive impairment, postural
hypotension, positive coomb`s test etc – Not used
therapeutically now except in Hypertension during
pregnancy (category B drugs)
Clonidine
Imidazoline derivative, partial agonist of central α2
receptor
Not frequently used now because of tolerance and
withdrawal hypertension
ADRENERGIC BLOCKERS
ADRENERGIC BLOCKERS
Alpha Blockers
Prazosin
Well absorbed orally ; bioavailability is 50-70%
Peak concentrations within 1-3 hours after oral dose
Initial dose 1 mg, usually given at bedtime
A maximal effect generally is observed with a total daily
dose of 20 mg in patients with hypertension
Uses- HTN, BPH,nightmares a/w PTSD, scorpion bite
S/E- orthostatic hypotension, syncope, nasal congestion
"first dose response"
Terazosin
Less potent than prazosin but retains high specificity
for α1 receptors
Bioavailability -high (>90%), t1/2 ~12 hours, duration of
action extends beyond 18 hrs
More effective than finasteride for BPH
Interesting aspect of the action of terazosin and
doxazosin for BPH is induction of apoptosis in prostate
SM cells
Initial first dose of 1 mg is recommended
Doses of 10 mg/day may be required for maximal
effect in BPH
Doxazosin
Highly selective antagonist at α1 receptors
T1/2 is 20 hours, duration of action may extend to 36
hrs bioavailability & extent of metabolism is similar
to prazosin
Given initially as a 1mg dose for HTN & BPH
Alfuzosin
Similar affinity at all of the α1 receptor subtypes
Bioavailability is ~64%, t1/2 3-5 hrs
Substrate of CYP3A4 and concomitant administration of
CYP3A4 inhibitors is contraindicated
Avoided in patients at risk for prolonged QT syndrome
One 10-mg extended release tablet daily to be taken
after meal
Used extensively in treating BPH; it is not approved for
treatment of hypertension
Tamsulosin
Selectivity for α1a (and α1d) subtypes
Efficacious in treatment of BPH & little effect on BP
Well absorbed, t1/2 of 5-10 hrs
0.4 mg starting dose, a dose of 0.8 mg will be more
efficacious
ADR- Abnormal ejaculation (experienced by 18%)
Silodosin
Selectivity for the α1a, over the α1b adrenergic
receptor
Approved for the treatment of BPH and is reported,
as is tamsulosin, to have lesser effects on BP than the
non-α1 subtype selective antagonists
Chief side effect- retrograde ejaculation (in 28%)
Adverse effects
Marked postural hypotension & syncope seen 30-90
mins after an initial dose of prazosin & 2-6 hours after
an initial dose of doxazosin
Syncopal episodes also have occurred with a rapid ↑ in
dosage or with the addition of a 2nd antihypertensive
with prazosin
Nonspecific ADRs- headache, dizziness & asthenia
rarely limit treatment with prazosin
Therapeutic Uses
Hypertension
Prazosin and its congeners -used successfully in the
treatment of essential HTN
These drugs improve rather than worsen lipid profiles
and glucose-insulin metabolism who are at risk for
atherosclerotic disease
Congestive Heart Failure
α receptor antagonists have been used in the treatment
of CHF, as have other vasodilating drugs
Due to dilation of both arteries & veins → reduction of
preload & afterload, which ↑cardiac output &
↓pulmonary congestion
Benign Prostatic Hyperplasia (BPH)
Prazosin ↓ resistance in some patients with impaired
bladder emptying caused by prostatic obstruction or spinal
injury
Finasteride and dutasteride- inhibit conversion of
testosterone to DHT & can ↓ prostate volume in some
patients, approved as monotherapy & in combination with α
receptor antagonists
Tamsulosin ( 0.4 mg daily) & silodosin (0.8 mg) less likely to
cause orthostatic hypotension than others
Combination therapy with doxazosin and finasteride
significantly better than either drug alone
Other Disorders
Variant angina (prinzmetal's angina)
Vasospastic disorders
↓ Ventricular arrhythmias induced by coronary
artery ligation or after reperfusion in animals
Mitral or aortic valvular insufficiency
α2 Receptor Antagonists
Yohimbine
Competitive antagonist
May benefit some patients with psychogenic erectile
dysfunction
Useful for diabetic neuropathy and in the treatment of
postural hypotension
Approved in veterinary medicine for the reversal of
xylazine anesthesia
Non-Selective α Adrenergic
Antagonists:
Phenoxybenzamine & Phentolamine
Referred to as "classical" α blockers
Postural hypotension is a prominent feature can
precipitate cardiac arrhythmias
Therapeutic Uses
Pheochromocytoma
Phenoxybenzamine is often used in preparing the
patient for surgery
Controls episodes of severe HTN and minimizes other
ADRs of catecholamines
Dose 40-120 mg given in two or three divided
portions
Useful for the treatment of hypertensive crises that
follow withdrawal of clonidine or ingestion of
tyramine-containing foods during the use of non-
selective MAO inhibitors
Direct intracavernous injection of phentolamine (in
combination with papaverine) for male sexual
dysfunction but may cause orthostatic hypotension
& priapism
FDA approved the use of phentolamine to reverse
or shorten the duration of soft-tissue anesthesia
Phenoxybenzamine has been used off-label to
control the manifestations of autonomic
hyperreflexia in patients with spinal cord
transection
Toxicity and Adverse Effects
Hypotension -major adverse effect
Alarming tachycardia, cardiac arrhythmias, and
ischemic cardiac events, including myocardial
infarction
Reversible inhibition of ejaculation
Phentolamine should be used with caution in
patients with a history of peptic ulcer
Additional α Adrenergic Receptor Antagonists
Ergot Alkaloids
Indoramin
selective, competitive α1 receptor antagonist that is used
for the treatment of hypertension, BPH, and in the
prophylaxis of migraine
↓ BP with minimal tachycardia
↓ incidence of attacks of Raynaud's phenomenon.
lacks a well-defined place in current therapy
Ketanserin
blocks α 1 receptors
Urapidil
a novel, selective α1 receptor antagonist
role in the treatment of hypertension remains to be
determined
Bunazosin
1-selective antagonist ,useful in hypertension
Neuroleptic Agents
Beta blockers
β antagonists can be distinguished by the following
properties:
Relative affinity for β1 and β2 receptors
Intrinsic sympathomimetic activity
Differences in lipid solubility
Capacity to induce vasodilation
Pharmacokinetic parameters
ADRENERGIC BLOCKERS
ADRENERGIC BLOCKERS
MSA ISA Lipid
Solub.
Absorpn
(%)
BA (%) T1/2 Protein
binding
Therapeutic Uses
Cardiovascular Diseases
Hypertension, Angina, Acute Coronary Syndromes &
Congestive Heart Failure
Hypertension
One of the 1st choice drugs because of good pt
acceptability & cardioprotective potential
Myocardial Infarction
Many trials- β receptor antagonists administered
during the early phases of acute MI & continued long-
term may ↓ mortality by ~25%
Angina pectoris
Act by ↓ cardiac work & O2 consumption
C/I in variant angina
Congestive Heart Failure
A number RCTs shows certain β receptor antagonists are
highly effective for pts with all grades of heart failure
secondary to left ventricular systolic dysfunction
Use of β Antagonists in Other Cardiovascular
Diseases
Propranolol- in hypertrophic obstructive
cardiomyopathy and angina, palpitations, and
syncope in patients with this disorder
Pheochromocytoma – should only used after
administering α blockers
Acute dissecting aortic aneurysm
Glaucoma
Useful for open-angle glaucoma
e.g.Carteolol, betaxolol, levobunolol, metipranolol
timolol and levobetaxolol
Have an onset in ~30 mins with a duration of 12-24 hrs
systemic absorption can lead to adverse cardiovascular
and pulmonary effects in susceptible patients
Caution- pts at risk for adverse systemic effects of β
receptor antagonists
Betaxolol- most effective antiglaucoma drug at
reducing Na+/Ca2+ influx
Other Uses
Propranolol, timolol, and metoprolol are effective for
the prophylaxis of migraine
Propranolol- effective in controlling acute panic
symptoms in individuals who are required to perform
in public or in other anxiety-provoking situations
Propranolol also may be useful in the treatment of
essential tremor
Of some value in the treatment of patients
undergoing withdrawal from alcohol or those with
akathisia
Propranolol and nadolol are efficacious in the
primary prevention of variceal bleeding in patients
with portal hypertension
Adverse Effects and Precautions
On Cardiovascular System
β receptor antagonists may induce congestive heart
failure in susceptible patients
Life-threatening bradyarrhythmias
Symptoms of peripheral vascular disease may worsen
Abrupt discontinuation of receptor antagonists after
long-term treatment can exacerbate angina and may
increase the risk of sudden death
Pulmonary function
May cause a life-threatening increase in airway
resistance
CNS
Fatigue, sleep disturbances (including insomnia and
nightmares), & depression
Metabolism
Should be used with great caution in patients with
diabetes who are prone to hypoglycemic reactions
Miscellaneous
Sexual dysfunction
Pregnancy
Drug Interactions
Aluminum salts, cholestyramine, and colestipol may
decrease the absorption of β blockers
Phenytoin, rifampin, and phenobarbital, smoking-
induce hepatic biotransformation enzymes - decrease
plasma concentrations of receptor antagonists (e.g.,
propranolol)
Cimetidine and hydralazine may increase the
bioavailability of agents such as propranolol and
metoprolol by affecting hepatic blood flow
Overdosage
Hypotension, bradycardia, prolonged AV conduction
times, and widened QRS complexes are common
manifestations of overdosage
Non-Selective β Adrenergic Receptor
Antagonists
Propranolol
For HTN & angina, initial oral dose 40-80 mg/day
Uses - supraventricular arrhythmias, ventricular
arrhythmias, PVCs, digitalis-induced
tachyarrhythmia's, MI, pheochromocytoma,
essential tremor & prophylaxis of migraine
Nadolol
Long-acting antagonist with equal affinity for 1 and
2 receptors
Distinguishing characteristic of nadolol is its
relatively long t1/2
Timolol
A potent, non-selective β receptor antagonist
Interestingly, the ocular formulation of timolol used
for the treatment of glaucoma, may be extensively
absorbed systemically
Adverse effects can occur in susceptible patients,
such as those with asthma or congestive heart
failure
Pindolol
with intrinsic sympathomimetic activity
Used to treat angina and hypertension
Preferred as antihypertensive in indivisual with
diminished cardiac reserve or propensity to
bradycardia
β1 selective adrenergic receptor antagonists
Metoprolol
Devoid of ISA and MSA
Significant first-pass metabolism
Uses: essential HTN, Angina, tachycardia, CHF,
Adjunct to treat hyperthyroidism
Atenolol
Very hydrophilic
Also used in graves disease
Initial dose is 50 mg/day OD may be ↑100 mg
Less CNS s/e than other β blockers and less
bronchoconstriction
Esmolol
Rapid onset ,short duration
Also class 2 anti arrhythmic
Slow iv injection
Used during surgeries to prevent or treat tachycardia
And SVT
Useful in severe post op HTN
AHA/ACC recommends against using esmolol in
patients already on β blockers, bradycardiac pts and
decompensated heart failure pts
Betaxolol
Mainly used in glaucoma to ↓IOP by↓ production of
aqueous humor
Acebutalol
Have lipophilic properties
Used for HTN, arrhythmias, MI, Smith Magenis
syndrome
Bisoprolol
Higher β1 selectivity than others except Nebivolol
Used in HTN ,CHF
Well tolerated
a/w 34% mortality benefit in CIBIS2
THIRD GENERATION β BLOCKERS
NITRIC OXIDE
PRODUCTION
ALPHA2
RECEPTOR
AGONISM
ALPHA1
RECEPTOR
ANTAGONISM
Ca2+ ENTRY
BLOCKADE
K+ CHANNEL
OPENING
ANTIOXIDANT
ACTIVITY
Celiprolola Celiprolola Carvedilol Carvedilol Tilisolola Carvedilol
Nebivolol Carteolol Bucindolola Betaxolol
Carteolol Bopindolola Bevantolola Bevantolola
Bopindolola Nipradilola
Nipradilola Labetalol
Labetalol
Selective Alpha1 and Nonselective Beta Blocker
↓ BP by ↓ SVR (alpha1)
Vasodilation via α1 blockade & partial beta2 agonist
activity
↓ HR by attenuating reflex tachy via β Blockade
Unchanged C.O.
S/e – postural hypotension
Bucindolol
↑ LV systolic EF, ↓PR hence ↓afterload
↑plasma HDL
Carvidilol
Has antioxidant and anti inflammatory property
Produces vasodilation
FDA approved for HTN, CHF,LV dysfunction following MI
Improves ventricular function and ↓ mortality and
morbidity in mild to severe CHF
Celiprolol
Selective β1 receptor antagonist, but a β2 receptor
partial agonist. It is also a weak α2 receptor antagonist
Recent clinical trial – possible use – vascular
complications of Ehler Danlos syndrome
Nebivolol
Highly selective
NO donorvasodialation, potential to improve
endothelial fuction, no deleterious effect on lipid profile
& carbohydrate metabolism
Use: HTN, CHF
Tissues or organs employed for the study of
Adrenoceptors
 α1 receptor system
1. Rat isolated vas deference (contraction)
2. Rabbit and guinea pig isolated aorta (contraction)
3. Rabbit isolated jejunum (inhibition)
4. Guinea pig isolated ileum (inhibition)
 α2 receptor system
1. Transmurally stimulated rat isolated vas deferens
(inhibition)
2. Electrically stimulated guinea pig isolated ileum
(inhibition)
 β1 receptor system
1. Rabbit isolated perfuse heart (contraction)
2. Rabbit isolated jejunum (inhibition)
 β2 receptor system
1. Guinea pig perfused lungs (brochodilatation)
2. Rat isolated uterus (inhibition)
3. Anaesthetized dog B.P (depression)
 Both α and β receptor system
1. Mouse isolated spleen (α- contraction, β-relaxation)
Conclusion
Thank you

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ADRENERGIC BLOCKERS

  • 1. Dr Shahid Saache JR1, Dept Of Pharmacology B.J.G.M.C PUNE
  • 2. INTRODUCTION ANS also called visceral, vegetative or involuntary nervous system Distributed widely through out body Regulates autonomic function without conscious control In periphery nerves, ganglia & plexuses that innervates heart, BV, glands, other visceral organs & SM
  • 4. End of postganglionic sympathetic synapse- adrenergic receptors
  • 5. “Block or decrease the effects of sympathetic nerve stimulation, endogenous catecholamines and adrenergic drugs” Adrenergic receptor blockers antagonize receptor action of epinephrine & related drugs Adrenergic neurone blocking agents act by interfering with release of adrenergic transmitter Central sympatholytics Ganglion blockers Chemical sympathectomy
  • 6. Neuron blocking drugs Guanethidine Act mainly by preventing release of NE at nerve endings Pharmacological sympathectomy Uses- HTN, glaucoma, neuropathic pain,& given IM for htnsive crises, severe pre eclampsia ADRs- severe postural hypotension, diarrheoa, renal impairment Bretylium Causes initial release of NE→ blocks adrenergic transmission by preventing NE release from adrenergic nerve endings Blocks K+ channels- class III antiarrhythmic activity
  • 7. Guanadrel False neurotransmitter- accumulated, stored & released like NE but is inactive at adrenergic receptors M/A- Replacement of NE with inactive transmitter ADRs- hypotension, fatigue ,lassitude, Sexual dysfunction, Diarrhoea Reserpine Inhibit vesicular catecholamine transporter Sedation, inability to concentrate- MC ADRs occasionally psychotic depressionsuicide Recent interest -at low doses, in combination with diuretics, for hypertension
  • 8. Metyrosine Inhibits tyrosine hydroxylase Adjuvant to phenoxybenzamine & other α adrenergic blockers for pheochromocytoma & in preoperative preparation for resection of pheochromocytoma ADR- crystalluria
  • 9. Central sympatholytics α Methyldopa MOA: Converted to α methyl NE which acts on α2 receptors in brain & causes inhibition of adrenergic discharge in medulla – ↓PVR & ↓BP Various adverse effects – cognitive impairment, postural hypotension, positive coomb`s test etc – Not used therapeutically now except in Hypertension during pregnancy (category B drugs) Clonidine Imidazoline derivative, partial agonist of central α2 receptor Not frequently used now because of tolerance and withdrawal hypertension
  • 13. Prazosin Well absorbed orally ; bioavailability is 50-70% Peak concentrations within 1-3 hours after oral dose Initial dose 1 mg, usually given at bedtime A maximal effect generally is observed with a total daily dose of 20 mg in patients with hypertension Uses- HTN, BPH,nightmares a/w PTSD, scorpion bite S/E- orthostatic hypotension, syncope, nasal congestion "first dose response"
  • 14. Terazosin Less potent than prazosin but retains high specificity for α1 receptors Bioavailability -high (>90%), t1/2 ~12 hours, duration of action extends beyond 18 hrs More effective than finasteride for BPH Interesting aspect of the action of terazosin and doxazosin for BPH is induction of apoptosis in prostate SM cells Initial first dose of 1 mg is recommended Doses of 10 mg/day may be required for maximal effect in BPH
  • 15. Doxazosin Highly selective antagonist at α1 receptors T1/2 is 20 hours, duration of action may extend to 36 hrs bioavailability & extent of metabolism is similar to prazosin Given initially as a 1mg dose for HTN & BPH
  • 16. Alfuzosin Similar affinity at all of the α1 receptor subtypes Bioavailability is ~64%, t1/2 3-5 hrs Substrate of CYP3A4 and concomitant administration of CYP3A4 inhibitors is contraindicated Avoided in patients at risk for prolonged QT syndrome One 10-mg extended release tablet daily to be taken after meal Used extensively in treating BPH; it is not approved for treatment of hypertension
  • 17. Tamsulosin Selectivity for α1a (and α1d) subtypes Efficacious in treatment of BPH & little effect on BP Well absorbed, t1/2 of 5-10 hrs 0.4 mg starting dose, a dose of 0.8 mg will be more efficacious ADR- Abnormal ejaculation (experienced by 18%)
  • 18. Silodosin Selectivity for the α1a, over the α1b adrenergic receptor Approved for the treatment of BPH and is reported, as is tamsulosin, to have lesser effects on BP than the non-α1 subtype selective antagonists Chief side effect- retrograde ejaculation (in 28%)
  • 19. Adverse effects Marked postural hypotension & syncope seen 30-90 mins after an initial dose of prazosin & 2-6 hours after an initial dose of doxazosin Syncopal episodes also have occurred with a rapid ↑ in dosage or with the addition of a 2nd antihypertensive with prazosin Nonspecific ADRs- headache, dizziness & asthenia rarely limit treatment with prazosin
  • 20. Therapeutic Uses Hypertension Prazosin and its congeners -used successfully in the treatment of essential HTN These drugs improve rather than worsen lipid profiles and glucose-insulin metabolism who are at risk for atherosclerotic disease
  • 21. Congestive Heart Failure α receptor antagonists have been used in the treatment of CHF, as have other vasodilating drugs Due to dilation of both arteries & veins → reduction of preload & afterload, which ↑cardiac output & ↓pulmonary congestion
  • 22. Benign Prostatic Hyperplasia (BPH) Prazosin ↓ resistance in some patients with impaired bladder emptying caused by prostatic obstruction or spinal injury Finasteride and dutasteride- inhibit conversion of testosterone to DHT & can ↓ prostate volume in some patients, approved as monotherapy & in combination with α receptor antagonists Tamsulosin ( 0.4 mg daily) & silodosin (0.8 mg) less likely to cause orthostatic hypotension than others Combination therapy with doxazosin and finasteride significantly better than either drug alone
  • 23. Other Disorders Variant angina (prinzmetal's angina) Vasospastic disorders ↓ Ventricular arrhythmias induced by coronary artery ligation or after reperfusion in animals Mitral or aortic valvular insufficiency
  • 24. α2 Receptor Antagonists Yohimbine Competitive antagonist May benefit some patients with psychogenic erectile dysfunction Useful for diabetic neuropathy and in the treatment of postural hypotension Approved in veterinary medicine for the reversal of xylazine anesthesia
  • 25. Non-Selective α Adrenergic Antagonists: Phenoxybenzamine & Phentolamine Referred to as "classical" α blockers Postural hypotension is a prominent feature can precipitate cardiac arrhythmias
  • 26. Therapeutic Uses Pheochromocytoma Phenoxybenzamine is often used in preparing the patient for surgery Controls episodes of severe HTN and minimizes other ADRs of catecholamines Dose 40-120 mg given in two or three divided portions Useful for the treatment of hypertensive crises that follow withdrawal of clonidine or ingestion of tyramine-containing foods during the use of non- selective MAO inhibitors
  • 27. Direct intracavernous injection of phentolamine (in combination with papaverine) for male sexual dysfunction but may cause orthostatic hypotension & priapism FDA approved the use of phentolamine to reverse or shorten the duration of soft-tissue anesthesia Phenoxybenzamine has been used off-label to control the manifestations of autonomic hyperreflexia in patients with spinal cord transection
  • 28. Toxicity and Adverse Effects Hypotension -major adverse effect Alarming tachycardia, cardiac arrhythmias, and ischemic cardiac events, including myocardial infarction Reversible inhibition of ejaculation Phentolamine should be used with caution in patients with a history of peptic ulcer
  • 29. Additional α Adrenergic Receptor Antagonists Ergot Alkaloids Indoramin selective, competitive α1 receptor antagonist that is used for the treatment of hypertension, BPH, and in the prophylaxis of migraine ↓ BP with minimal tachycardia ↓ incidence of attacks of Raynaud's phenomenon. lacks a well-defined place in current therapy
  • 30. Ketanserin blocks α 1 receptors Urapidil a novel, selective α1 receptor antagonist role in the treatment of hypertension remains to be determined Bunazosin 1-selective antagonist ,useful in hypertension Neuroleptic Agents
  • 32. β antagonists can be distinguished by the following properties: Relative affinity for β1 and β2 receptors Intrinsic sympathomimetic activity Differences in lipid solubility Capacity to induce vasodilation Pharmacokinetic parameters
  • 35. MSA ISA Lipid Solub. Absorpn (%) BA (%) T1/2 Protein binding
  • 36. Therapeutic Uses Cardiovascular Diseases Hypertension, Angina, Acute Coronary Syndromes & Congestive Heart Failure Hypertension One of the 1st choice drugs because of good pt acceptability & cardioprotective potential
  • 37. Myocardial Infarction Many trials- β receptor antagonists administered during the early phases of acute MI & continued long- term may ↓ mortality by ~25% Angina pectoris Act by ↓ cardiac work & O2 consumption C/I in variant angina
  • 38. Congestive Heart Failure A number RCTs shows certain β receptor antagonists are highly effective for pts with all grades of heart failure secondary to left ventricular systolic dysfunction
  • 39. Use of β Antagonists in Other Cardiovascular Diseases Propranolol- in hypertrophic obstructive cardiomyopathy and angina, palpitations, and syncope in patients with this disorder Pheochromocytoma – should only used after administering α blockers Acute dissecting aortic aneurysm
  • 40. Glaucoma Useful for open-angle glaucoma e.g.Carteolol, betaxolol, levobunolol, metipranolol timolol and levobetaxolol Have an onset in ~30 mins with a duration of 12-24 hrs systemic absorption can lead to adverse cardiovascular and pulmonary effects in susceptible patients Caution- pts at risk for adverse systemic effects of β receptor antagonists Betaxolol- most effective antiglaucoma drug at reducing Na+/Ca2+ influx
  • 41. Other Uses Propranolol, timolol, and metoprolol are effective for the prophylaxis of migraine Propranolol- effective in controlling acute panic symptoms in individuals who are required to perform in public or in other anxiety-provoking situations
  • 42. Propranolol also may be useful in the treatment of essential tremor Of some value in the treatment of patients undergoing withdrawal from alcohol or those with akathisia Propranolol and nadolol are efficacious in the primary prevention of variceal bleeding in patients with portal hypertension
  • 43. Adverse Effects and Precautions On Cardiovascular System β receptor antagonists may induce congestive heart failure in susceptible patients Life-threatening bradyarrhythmias Symptoms of peripheral vascular disease may worsen Abrupt discontinuation of receptor antagonists after long-term treatment can exacerbate angina and may increase the risk of sudden death
  • 44. Pulmonary function May cause a life-threatening increase in airway resistance CNS Fatigue, sleep disturbances (including insomnia and nightmares), & depression Metabolism Should be used with great caution in patients with diabetes who are prone to hypoglycemic reactions Miscellaneous Sexual dysfunction Pregnancy
  • 45. Drug Interactions Aluminum salts, cholestyramine, and colestipol may decrease the absorption of β blockers Phenytoin, rifampin, and phenobarbital, smoking- induce hepatic biotransformation enzymes - decrease plasma concentrations of receptor antagonists (e.g., propranolol) Cimetidine and hydralazine may increase the bioavailability of agents such as propranolol and metoprolol by affecting hepatic blood flow
  • 46. Overdosage Hypotension, bradycardia, prolonged AV conduction times, and widened QRS complexes are common manifestations of overdosage
  • 47. Non-Selective β Adrenergic Receptor Antagonists Propranolol For HTN & angina, initial oral dose 40-80 mg/day Uses - supraventricular arrhythmias, ventricular arrhythmias, PVCs, digitalis-induced tachyarrhythmia's, MI, pheochromocytoma, essential tremor & prophylaxis of migraine
  • 48. Nadolol Long-acting antagonist with equal affinity for 1 and 2 receptors Distinguishing characteristic of nadolol is its relatively long t1/2 Timolol A potent, non-selective β receptor antagonist Interestingly, the ocular formulation of timolol used for the treatment of glaucoma, may be extensively absorbed systemically Adverse effects can occur in susceptible patients, such as those with asthma or congestive heart failure
  • 49. Pindolol with intrinsic sympathomimetic activity Used to treat angina and hypertension Preferred as antihypertensive in indivisual with diminished cardiac reserve or propensity to bradycardia
  • 50. β1 selective adrenergic receptor antagonists Metoprolol Devoid of ISA and MSA Significant first-pass metabolism Uses: essential HTN, Angina, tachycardia, CHF, Adjunct to treat hyperthyroidism Atenolol Very hydrophilic Also used in graves disease Initial dose is 50 mg/day OD may be ↑100 mg Less CNS s/e than other β blockers and less bronchoconstriction
  • 51. Esmolol Rapid onset ,short duration Also class 2 anti arrhythmic Slow iv injection Used during surgeries to prevent or treat tachycardia And SVT Useful in severe post op HTN AHA/ACC recommends against using esmolol in patients already on β blockers, bradycardiac pts and decompensated heart failure pts Betaxolol Mainly used in glaucoma to ↓IOP by↓ production of aqueous humor
  • 52. Acebutalol Have lipophilic properties Used for HTN, arrhythmias, MI, Smith Magenis syndrome Bisoprolol Higher β1 selectivity than others except Nebivolol Used in HTN ,CHF Well tolerated a/w 34% mortality benefit in CIBIS2
  • 53. THIRD GENERATION β BLOCKERS NITRIC OXIDE PRODUCTION ALPHA2 RECEPTOR AGONISM ALPHA1 RECEPTOR ANTAGONISM Ca2+ ENTRY BLOCKADE K+ CHANNEL OPENING ANTIOXIDANT ACTIVITY Celiprolola Celiprolola Carvedilol Carvedilol Tilisolola Carvedilol Nebivolol Carteolol Bucindolola Betaxolol Carteolol Bopindolola Bevantolola Bevantolola Bopindolola Nipradilola Nipradilola Labetalol
  • 54. Labetalol Selective Alpha1 and Nonselective Beta Blocker ↓ BP by ↓ SVR (alpha1) Vasodilation via α1 blockade & partial beta2 agonist activity ↓ HR by attenuating reflex tachy via β Blockade Unchanged C.O. S/e – postural hypotension Bucindolol ↑ LV systolic EF, ↓PR hence ↓afterload ↑plasma HDL
  • 55. Carvidilol Has antioxidant and anti inflammatory property Produces vasodilation FDA approved for HTN, CHF,LV dysfunction following MI Improves ventricular function and ↓ mortality and morbidity in mild to severe CHF Celiprolol Selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist Recent clinical trial – possible use – vascular complications of Ehler Danlos syndrome
  • 56. Nebivolol Highly selective NO donorvasodialation, potential to improve endothelial fuction, no deleterious effect on lipid profile & carbohydrate metabolism Use: HTN, CHF
  • 57. Tissues or organs employed for the study of Adrenoceptors  α1 receptor system 1. Rat isolated vas deference (contraction) 2. Rabbit and guinea pig isolated aorta (contraction) 3. Rabbit isolated jejunum (inhibition) 4. Guinea pig isolated ileum (inhibition)  α2 receptor system 1. Transmurally stimulated rat isolated vas deferens (inhibition) 2. Electrically stimulated guinea pig isolated ileum (inhibition)
  • 58.  β1 receptor system 1. Rabbit isolated perfuse heart (contraction) 2. Rabbit isolated jejunum (inhibition)  β2 receptor system 1. Guinea pig perfused lungs (brochodilatation) 2. Rat isolated uterus (inhibition) 3. Anaesthetized dog B.P (depression)  Both α and β receptor system 1. Mouse isolated spleen (α- contraction, β-relaxation)