Aminoglycosides

 and  
tetracycline  as  well
 M1,3,5 are stimulatory, M2&4 are inhibitory on adenylyl cyclase

Receptor Name Typical Locations Result of Ligand Binding

Cholinoceptors
Muscarinic M1 CNS neurons, sympathetic postganglionic Formation of IP3 and DAG, increased intracellular calcium
neurons, some presynaptic sites
Muscarinic M2 Myocardium, smooth muscle, some Opening of potassium channels, inhibition of adenylyl cyclase
presynaptic sites; CNS neurons
Muscarinic M3 Exocrine glands, vessels (smooth muscle Like M1 receptor-ligand binding
and endothelium); CNS neurons
Muscarinic M4 CNS neurons; possibly vagal nerve endings Like M2 receptor-ligand binding

Muscarinic M5 Vascular endothelium, especially cerebral Like M1 receptor-ligand binding

vessels; CNS neurons
Nicotinic NN Postganglionic neurons, some presynaptic Opening of Na+,K+ channels, depolarization
cholinergic terminals
Nicotinic NM Skeletal muscle neuromuscular end plates Opening of Na+,K+ channels, depolarization

Adrenoceptors
Alpha1 Postsynaptic effector cells, especially Formation of IP3 and DAG, increased intracellular calcium
smooth muscle
Alpha2 Presynaptic adrenergic nerve terminals, Inhibition of adenylyl cyclase, decreased cAMP
platelets, lipocytes, smooth muscle
Beta1 Postsynaptic effector cells, especially heart, Stimulation of adenylyl cyclase, increased cAMP
lipocytes, brain; presynaptic adrenergic and
cholinergic nerve terminals, juxtaglomerular
apparatus of renal tubules, ciliary body
epithelium
Beta2 Postsynaptic effector cells, especially Stimulation of adenylyl cyclase and increased cAMP. Activates
smooth muscle and cardiac muscle cardiac Gi under some conditions.

Beta3 Postsynaptic effector cells, especially Stimulation of adenylyl cyclase and increased cAMP
lipocytes; heart
Dopamine
receptors
D1 (DA1), D5 Brain; effector tissues, especially smooth Stimulation of adenylyl cyclase and increased cAMP
muscle of the renal vascular bed
D2 (DA2) Brain; effector tissues, especially smooth Inhibition of adenylyl cyclase; increased potassium conductance
muscle; presynaptic nerve terminals
D3 Brain Inhibition of adenylyl cyclase

D4 Brain, cardiovascular system Inhibition of adenylyl cyclase

Cholinergic effects
Target Receptor Response
Sphincter M3 Contraction-miosis
Eye
Ciliary muscle M3 Contraction-accommodation for near vision

SA node M2 Heart rate (HR)-negative chronotropy

Heart Conduction velocity-negative dromotropyNo effects on ventricles, Purkinje
AV node M2
system
Bronchioles M3 Contraction-bronchospasm
Lungs
Glands M3 Secretion
Stomach M3 Motility-cramps
GI tract Glands Ml Secretion
Intestine M3 Contraction-diarrhea, involuntary defecation
Contraction (detrusor), relaxation (trigone/sphincter), voiding, urinary
Bladder M3
incontinence
Sphincter M3 Relaxation, except lower esophageal, which contracts
Glands M3 Secretion-sweat ( thermoregulatory),salivation, and lacrimation
Dilation (via NO/endothelium-derived relaxing factor )-no innervation, no
Blood vessels (endothelium) M3
effects of indirect agonists
 Drugs of the ANS

Drug type Drug Mechanism Clinical Use Side Effects

Cholinergic Methacholine Agonist of muscarine only used in bronchial SPLUDS-BBB or DUMBELS
Agonist It has β -methyl group in its receptor reactivity testing -Salivation, Miosis, Lacrimation,
Muscarinic structure which reduces the Urination, Defacation, Sweating,
Agonists potency at nicotinic Bronchoconstriction, Emesis,
receptors. Bradycardia.
Sweating is the only
Sympathetic action here
Carbechol Direct stimulant of Rarely used
muscarine & nicotinic Therapeuticaly.
receptor
NOT degraded by
ACh-esterase
Bethanechol Muscarinic only Rx-ileus (postop/ Generalized ACh-esterase
It has β -methyl group in its Not degraded by ACh- neurogenic), urinary stimulation
structure which reduces the esterase retention
potency at nicotinic
receptors.
Pilocarpine Stimulates muscarine Rx-glaucoma (topical), CNS – disturbances
receptor xerostomia Stimulates sweating
Crosses the BBB
Suscep. To AchC is
negligebile.
Nicotine Agonist at nicotinic Smoking cessation
receptors. programs
Resistant to hydrolysis
by Ache.
 Cevimeline synthetic direct-acting Treatment of dry mouth
muscarinic receptor and dry eyes in patients
agonist who have had radiation
therapy for head and
neck cancer and in
those with Sjögren's
syndrome (dry eyes, dry
mouth, and arthritis).
Varenicline partial agonist at the The drug is used as an
nicotinic receptor aid to smoking
subtype cessation and has
been found to reduce
both the craving and
withdrawal effects
caused by the absence
of nicotine.
Reversible Physostigmine Reversible inhibition of Decreases intra ocular Generalized ACh stimulation
Anticholineste ACh-esterase pressure (glaucoma) Hi dose
rase Acts on all ACh Overdose tx CNS – convulsion
Can be labeled receptors Atropine,
as Indirectly Paralysis of skeletal muscle (too
Tertiary amine, so phenothiazine, TCA much Ach resulting in depolarizing
acting drugs crosses the BBB and
and require NM block)
have central actions
the presence
Neostigmine Reversible inhibition of Tx for myasthenia Generalized ACh stimulation
of Ach to bring
ACh-esterase gravis
about their
effect. Quaternary amine so Reverses the effect of
Doesn’t cross BBB competitive NM
NO Pupil constriction blockers ( Curari like
drugs)
orally active
Pyridostigimine Similar to neostigmine. Similar to neostigmine.
 Edrophonium Similar to neostigmine Used in dx of Generalized ACh stimulation
Much Shorter half life myasthenia gravis / Cholinergic crisis – antidote is
differentiating b/w Atropine
myasthenic crisis and
cholinergic crisis.
tests: better =MG
worse= cholinergic
crisis
Agents for Tacrine, donepezil, Are centrally acting, Alzheimer's disease Tacrine less used due to short half
Alzheimer’s galantamine, and rivastigmine reversible life and hepatotoxicity.
disease cholinesterase
inhibitors that readily
cross the blood-brain
barrier and act to
increase the
concentration of
acetylcholine at central
cholinergic synapses.
Irreversible Organophosphates Covalently binds to Glaucoma only in very DUMBELS
Ache DFP/Echothiphaate ACh-esterase to form very dilute solutions convulsions, coma, respiratory
inhibitors. phosphorylated Ache. (echothiophate) but paralysis, death.
Malathion, parathion, soman,
tabun, sarin Phosphorylated Ache rarely used now due to Antidote – Pralidoxime /
require nearly 100 hrs risk of retinal ATROPINE
for hydrolysis. detachment and
cataract. Chronic exposure to the
organophosphates leads to a
delayed neurotoxicity due to
demyelinization of motor
neurons
ACh-esterase Pralidoxime It is an AChE Overdose of -Only effective in short time period
re-activator (2-PAM) reactivatior, but must organophosphates after AchE conversion. New nerve
be administered IV Blocks SLUD gases have very short window of
within minutes after (salivation, lacrimation, opportunity.
exposure as it is only Urination, Defecation)
effective prior to
aging. Ineffective in
the CNS and against
carbmylated AChE.
Drugs Sildenafil, tadalafil and Phosphodiesterase Erectile dysfunction. Headache, nasal congestion,
augmenting vardenafil. inhibitor (5-PDE). dyspepsia, myalgia, back pain,
effect of Ach These drugs potentiate and visual disturbances.
the vasodilative effect Concurrent administration of 5-
of acetylcholine PDE inhibitors and nitroglycerin
released from sacral can cause profound
parasympathetic hypotension, reflex tachycardia,
neurons and thereby and worsening of angina
increase penile blood pectoris.
flow and facilitate
penile erection during Can also augment the
sexual stimulation. hypotensive effects of other
Mediators involved are vasodilators, including α-
Nitric oxide and Cyclic adrenoceptor antagonists
GMP.
Cholinergic Atropine Competitive antagonist Eye AntiCholinergics Dry up every
Antagonist to muscarinic receptor. -Cycloplegic & thing –Decreases sweat/
Effects (Atropine myadriatic (near salivation/lacrimation
effects in order of accommodation/dilation Acid secretions are inhibited at
increasing dose) but effect on ciliary very high doses.
Decreased secretions muscle persists for 72 -Dilated pupil w/ loss of
( salivary, bronchial, hours) accommodation
sweat) GI/GU -Flushing of skin
Mydriasis and -Antispasmodic -Hot (no sweat i.e. no
cycloplegia -Decrease acid thermoregulation)
Hyperthermia productin (peptic ulcer -Delusions & toxic psychosis
Tachycardia and tx)?
-initial bradycardia followed by
decrease in PR Antidiarrheal (in sustained tachycardia.
interval. combination with
diphenoxylate) -Urinary retention and
Sedation constipation.
Urinary retention and Lung
Never given in patients of GERD
constipation -Antisecretory for as causes opening of the lower
Behavioral excitation surgery esophageal sphincter.
and hallucinations Anesthetic – decreases
secretions
-Tx of parkinsons
-Antidote for
organophosphates
-Sinus Bradycardia,
-Symptomatic AV
Block (Glycopyrrolate
more suited)

Dose-dependent effects of atropine

Scopolamine -Competitive blocker of muscarin DOC-Motion Atropine-like ADR
receptors Sickness Causes sedation and
-Greater action on CNS w/ longer (prophylactic) short term memory
duration loss.
Tropicamide and Competitive antagonist to Eye examination Atropine-like ADR
cyclopentolate. muscarinic receptor. Short duration -Cycloplegic&
of action. myadriatic
Ipratropium and Tiotropium Quaternary amine derivatives of Administered by Because these drugs
atropine,Competitive antagonist to inhalation to patients are not well absorbed
muscarinic receptor with obstructive lung from the lungs into the
diseases. systemic circulation,
Do not impair the they produce few
ciliary clearance of adverse effects.
secretions from the
airways.
Pirenzepine Ulcer tx
Benztropine, trihexyphenidyl, Penetrates CNS Parkinson’s Disease
biperden. (central effects)
 Oxybutynin, glycopyrrolate, To treat transient
dicyclomine, tolterodine, cystitis, post-op
darifenacin, solifenacin, and bladder spasms, or
trospium incontinence.
Glycopyrrolate, dicyclomine, To reduce transient GI
methscopolamine. hypermotility
Antihistaminics NOTE: Remember the
TCAs benefits and toxicities
related to the
Antipsychotics anticholinergic activities
Quinidine and related drugs of of these drugs.
Other drug the same group
groups with Amantadine
anticholinergic
properties. Mepridine
Botulinum toxin Acts by blocking the release of Cervical dystonia
acetylcholine from the neuron by Blepharospasm
preventing the vesicle where the
Acetylcholine is stored from Severe primary axillary
binding to the membrane. hyperhidrosis.
Achalasia
Spastic disorders
associated with injury
or disease of the
central nervous system
including trauma,
stroke, multiple
sclerosis, Parkinson's
disease, or cerebral
palsy
Cosmetic Use
(wrinkles)
NOTE: Both anticholinergics and phenylephrine, an α1-adrenoceptor agonist, induce mydriasis, but phenylephrine will not
induce cycloplegia (loss of accommodation).
Cholinergic Trimethaphan Short-acting blocker Good for emergency Blocks all autonomic
antagonist : lowering of blood responses
Nicotinic / pressure ( in Final effect will depend
Ganglionic hypertension caused on the predominant
Blockers by pulmonary edema tone on that particular
or dissecting aortic system (see the table
aneurysm) below)
Stimulates histamine
release, can cause
flushing, dizziness, and
headache.
Mecamylamine long acting rarely used.
Hexamethonium Experimental only

Effector   System   Effect of ganglion blockade

Arterioles   SANS  Vasodilation, hypotension
Veins   SANS  Dilation, decreased venous return, decreased CO
Heart   PANS   Tachycardia
Iris   PANS   Mydriasis
Ciliary muscle  PANS   Cyclplegia
GI tract   PANS   Decreased tone and motility-constipation
Bladder   PANS   Urinary retention
Salivary glands   PANS   Xerostomia
Sweat glands  SANS  Anhydrosis
Adrenomimetic Drugs:
Adrenomimetic / Sympathomimetic drugs mimic
the effect of sympathetic nerve stimulation on
sympathetic effectors.
Divided into two major groups on the basis of
their chemical structure:
Catecholamines: Norepinephrine, epinephrine,
dopamine, dobutamine, isoproterenol.
Noncatecholamines:These drugs differ from the
basic catecholamine structure primarily by
having substitution on their benzene ring,
phenylephrine, ephedrine, amphetamine.
Receptor subtype and the
responses mediated by them.

RECEPTOR SELECTIVITY
 Control drug effect

Increased diastolic Increased TPR (Increased α1)

Decreased diastolic
Increased Heart rate
Decreased Heart rate
Increased pulse pressure
decreased TPR (increased β2, decreased α1,
directly acting vasodilators and cholinomimetics.
increased β1 (May be reflex *)
Increased Cholinergic (May be a reflex)
increased β1 (increased inotropic activity)
Effect of α1 activators on Heart rate and blood
pressure
Alpha 1 Agonists
Systemically , increase mean blood pressure via
vasoconstriction.
Increased BP may elicit a reflex bradycardia.
Cardiac output may be decreased but also offset by
increased venous return.
No change in pulse pressure.
Phenylephrine: nasal decongestant and
opthalmologic use ( mydriasis without cycloplegia)
Methoxamine: paroxysmal atrial tachycardia through
vagal reflex.
Alpha 2 Agonists
Stimulate prejunctional receptors in the CNS to
decrease sympathetic outflow. Primary use is mild to
moderate hypertension. Eg. Clonidine and
Methyldopa
Effect of β activators on Heart rate and blood
pressure
Systemically, decrease mean BP via vasodilation
(β2) and increased HR (β1)
Increased Pulse pressure.
Isoproterenol (β1= β2)Uses are bronchospasm, heart
block, and bradyarrhythmias. Side effects include
flushing , angina, arrhythmias.
Dobutamine (β1>>> β2)CHF
Selective β2: Salmeterol, albuterol, and terbutaline
used in asthma and ritodrine used in premature labor.
Effect of Norepinephrine on Heart rate and blood
pressure
Effect of Epinephrine on Heart rate and blood
pressure
Dose dependent effects
• Low dose: β1 ,β2 stimulation.
• High dose: α1, β1 (β2).
Β2 specific effects:
• Smooth muscle relaxation.
• Metabolic effects:
• Increased glycogenolysis
• Increased gluconeogenesis
• Increased mobilization and use of fat.

Exercise: Effect of epinephrine after pre-treatment α1

with blocker.
Adrenergic Epinephrine Interacts with both alpha & Beta DOC – bronchospasm/ CNS – anxiety, fear,
receptors anaphylaxis tension, tremor
Agonist
Vasoconstriction and Eye Marked elevation in BP,
increased blood pressure Glaucoma – decrease increased cardiac work,
(α1), cardiac stimulation (β1), pressure via ischemia, failure.
and bronchodilation (β2) vasoconstriction of ciliary Hemorrhage – cerebral
Low dose, MAP stays the same blood vessels via hi BP
(increase sys, decrease dias) hi Increase duration of Cardiac arrhythmia
dose MAP increase local anesthetics via Pulmonary edema
vasoconstriction
cardiac arrest, ventricular
fibrillation, reduction in
bleeding during surgery
Norepinephrine α1 = α2 , β1>>>>β2. Shock and Hypotension Similar to epi
Negligible Pulmonary action. –powerful vasoconstrictor

Isoproterenol β1=β2 Asthma, atrioventricular Similar to epi

-i.e. non selective beta-agonist block, and bradycardia
Cardiac stimulation(β1) and
bronchodilation (β2)
Decreases peripheral
resistance
Dopamine Precursor for NE Cardiogenic shock, ADR similar to epi
septic shock, heart DA converted to HVA
DA> β1> α1
failure, and adjunct to which can cause
Renal vasodilation (D1), fluid administration in Nausea/hypertension/
cardiac stimulation(β1), and hypovolemic shock arrhythmia
increased blood pressure (β1 Enhances perfusion to
and α1) renal (SPARING),
splanchnic & coronary
arteries.
Beta 1 agonist Dobutamine β1 selective agonist
Dobutamine exerts a greater
effect on the contractile force of
the heart relative to its effect on
the heart rate than does
dopamine.
Dobutamine increases the
oxygen demands on the heart
to a lesser extent than does
dopamine.
Beta 2 Metaproterenol β2 agonist
selective Little effect on heart
agonists
Resistant to COMT methylation/
degradation
Terbutaline /Albuterol β2 agonist
-More selective than
metaproterenol
Resistant to COMT methylation/
degradation
Ritodrine Same but mainly used for its
uterine effects.
CHF tx – increase CO DOBUTAMINE –
with little change in HR NORMOTENSIVE
Shock/resucitation – DOPAMINE –
increases force more than HYPOTENSIVE
rate Use withcaution in
cardiac stimulation patients in A-fib
during heart surgery
Bronchodilator – asthma Skeletal muscle
Uterine relaxation tremor, restlessness,
tachycardia, arrhythmia,
pulmonary edema in
pregnancy.
Same as M. Same as M.
Primarily against CAUTION:
premature labor Hyperglycemia in
mother & reactive
hypoglycemia in
newborn
Contraindicated in
IDDM pt.
 Phenylephrine, Metaraminol, Vasoconstriction, increased Nasal and ocular
and Methoxamine blood pressure, and mydriasis decongestion, mydriasis,
(α1) maintenance of blood
Phenylephrine is not a pressure and treatment of
Alpha 1 substrate for COMT. shock.
Selective
agents Metaraminol, and Methoxamine The reflex bradycardia
are not metabolized by COMT induced by their rapid IV
& MAO. administration has been
used to terminate attacks
of PAT.
Midodrine Is a prodrug that is Indicated in the treatment May cause
enzymatically hydrolyzed to of postural hypotension, hypertension when the
desglymidodrine, an α1- typically due to impaired subject is supine
receptor-selective agonist. autonomic nervous
system function.
Xylometazoline and Activates α adrenergic Used as topical Oxymetazoline may
oxymetazoline receptors but has a liking for decongestants (nasal and cause hypotension,
α1 . ocular) because of their because of central
ability to promote clonidine like effect
vasoconstriction by (Oxymetazoline has
activating α1 receptors. significant affinity for
α2A receptors)
Clonidine, methyldopa, Decreased sympathetic outflow Hypertension, opioid CNS depression.
guanfacine, guanabenz. from central nervous system dependence. Withdrawal of clonidine
Alpha 2 (α2)
Selective Methydopa used for after longterm use
agents Pregnancy induced HT. results in severe
Clonidine available as rebound.
transdermal patch. Methy Dopa causes a
positive coombs test.
Dexmedetomidine Centrally acting α2-selective Indicated for sedation of
agonist initially intubated and
mechanically ventilated
patients during treatment
in an intensive care
setting.
 Apraclonidine and Decreased aqueous humor Short-term control of High rate of
brimonidine. formation (α2) intraocular pressure. tachyphylaxis (rapid
development of
tolerance)
Amphetamine Increase in norepinephrine Narcolepsy, attention- CNS toxicities.
release, central nervous system deficit disorder
stimulation. Resists
Indirect metabolism by COMT and
sympathomim MAO.
etics Cocaine Inhibition of norepinephrine Local anesthesia Convulsions, cerebral
uptake Only local anesthetic hemorrhage,
that is vasoconstrictor arrhythmias, myocardial
in nature. infarction.
Methamphetamine (N-methylamphetamine) is very similar to amphetamine with an even higher ratio of central to
peripheral actions.
Phenmetrazine is a variant phenylisopropylamine with amphetamine-like effects. It has been promoted as an
anorexiant and is also a popular drug of abuse.
Methylphenidate and pemoline are amphetamine variants whose major pharmacologic effects and abuse potential
are similar to those of amphetamine .
Modafinil is a new drug with both similarities to and differences from amphetamine. It has significant effects on
central α1B receptors but in addition appears to affect GABAergic, glutaminergic, and serotonergic synapses as
well.
Ephedrine Vasoconstriction (α1) Nasal decongestion Tachycardia, increased
Mixed Ephiedrine has a direct blood pressure, and
sympathomim stimulatory effect on urinary retention,
etics bronchodilatory receptors also. Central nervous system
stimulation and
Resists metabolism by COMT insomnia.
and MAO.
Pseudoephedrine Vasoconstriction (α1) Used as a nasal
decongestant in the
treatment of colds and
allergies.
Adrenergic Antagonists.
 Beta Adrenoceptor Blocking
Alpha Adrenoceptor Blocking Agents Beta Adrenoceptor Blocking Agents
Agents
Non-Selective Non-Selective
With partial agonist activity
• Phentolamine • Propranolol • Acebutolol
• Phenoxybenzamine • Nadolol • Carteolol
Alpha-one Selective • Timolol • Penbutolol
• Prazosin • Pindolol • Pindolol
• Terazosin • Carteolol • Celiprolol
• Doxazosin Cardioselective
• Tamsulosin (α1A) • Atenolol
With membrane stabilizing activity
Alpha-two Selective • Acebutolol • Propranolol (+)
• Yohimbine • Metoprolol • Pindolol (slight)
Ergot Alkaloids • Betaxolol • Metoprolol (slight)
• Ergotamine Alpha and Beta Blocker • Betaxolol (slight)
• Ergonovine • Labetalol, Carvedilol • Acebutolol (+).
Very Short Acting • Labetalol (+).
• Esmolol

Alpha Adrenoceptor Blocking Agents

Non selective Phenoxybenzamine
α Blockers
Irreversible , non-competitive Tx for
Non selective (but shows
liking for α1 receptors).
Binds covalently to α1 post
synaptic & α2 presynaptic
receptors
Venodilation is prominent
Postural hypotension
pheochromocytoma- Tachycardia
induced hypertension.
Nasal stuffiness
Clonidine w/drawal
Miosis
Raynaud’s phenomena
Failure of ejaculation
Peripheral vascular
disease, BPH, (shooting blanks)
Acrocyanosis from frost Nausea, vomiting
bite.
 Phentolamine/Tolazoline Equilibrium competitive
antagonism.
Non selective.
Venodilation is prominent
Selective α Prazocin/Terazocin/ Equilibrium competitive
Blockers Doxazocin/Trimazosin antagonism.
Selective for α1.
Veins less susceptible to
antagonism than arteries,
thus postural hypotension is
less of a problem.
Cardiac stimulation is less
because release of
norepinephrine is not
enhanced.
Favorable effect on plasma
lipids: increase HDL/LDL
ratio
Tamsulosin and Silodosin α1A selective
Selective α2 Yohimbine, Mirtazapine
blockers
Same but reversible Same
Direct penile injection of
Phentolamine with
Papaverine have been
tried in men with Erectile
Dysfunction (ED).
Primary hypertension, 1st dose phenomenon
BPH. (sudden fall of BP with
first dose)
Vertigo
Nasal congestion
Drowsiness
BPH Immunologic: It
contains a sulfa moiety,
thus causing typical
reactions to sulfa drugs.
Ophthalmologic:
Patients taking
tamsulosin are prone to
a complication known
as floppy iris syndrome
during cataract surgery.
Retrograde ejaculation
Other α
receptor
related drugs

Alfuzosin
Is an α1 selective quinazoline derivative that has also been shown to be efficacious in BPH. Not currently available
in the USA.
Indoramin
Is an α1 selective antagonist, has efficacy as an antihypertensive.
Urapidil
α1 antagonist, weak α2 agonist and 5HT1A agonist action and weak antagonist action at β1. Used in Europe as an
antihypertensive agent and for BPH.
Beta Blockers Beta 1 blockade Cardioselectivity (β1) • Bradycardia,
• Dec. HR, SV, CO Less effect on atrioventricular
vasculature, bronchioles, blockade, and
• Dec. AV nodal conduction congestive heart
uterus, and metabolism
• Dec. renin release failure.
Safer in asthma, diabetes,
• Dec. aqueous humor production peripheral vascular
• Plasma lipid
disease profile is altered
Beta 2 blockade on long term
• May precipitate bronchospasm (in asthmatics) and Intrinsic use.
vasospasm (in patients with vasospastic diseases) sympathomimetic
activity (ISA)
• Patients with
• Metabolic effects : Blocks glycogenolysis, airway disease
gluconeogenesis. Dec. HDL and inc. VLDL Act as partial agonist may suffer
Less bradycardia severe asthma
Effect on Blood vessels.
attacks.
• Slow developing decrease in peripheral resistance. Slight vasodilation or
bronchodilation • Premonitory
Possibly due to: central reduction in sympathetic tone
symptoms of
and reduction in renin release (beta-1 effect) Minimal change in plasma hypoglycemia
Effects on the Eye lipids from insulin
• Several β-blocking agents reduce intraocular pressure, Combined alpha 1 and overdosage, eg,
especially in glaucomatous eyes. The mechanism usually Beta blocking activity tachycardia,
reported is decreased aqueous humor production. tremor, and
Labetalol and carvedilol
anxiety, may be
Used in CHF masked, and
Potassium channel mobilization of
blockade and beta glucose from the
blockade liver may be
impaired.
Sotalol (class III
antiarrhythmic)
• Sedation,
fatigue, and
sleep
alterations.
• Purpura, rash
and fever have
also been
reported.
Nonselective Propanolol NonSelective β Blockers.
Beta Blockers Caution: don’t give to pt.
with: heart failure, asthma,
diabetes
Naldol Longer acting pure antagonist
-No CNS involvement
Timolol More potent than propranolol
lowers IOP in glaucoma
reduces aqueous humor
production
Pindolol partial agonist; partial blockade
Carvedilol It blocks of α1, β1 and β2-
receptors
It also possesses antioxidant
property
Angina pectoris – All general toxicities.
reduction of O2 Contraindicated in
requirement of heart and acute CHF Rebound
an increase in exercise tachycardia if suddenly
capacity. removed
MI-reinfarct protection ASTHMA IS
Essential Hypertension, ABSOLUTE
Migraines – blocks CONTRAINDICATION.
catechlamine induced Use with extreme
vasodilation in brain caution in Diabetes
Performance / stage and patients with
Anxiety partial heart block.
Hypethyroidism – blocks Combination with
periphera conversin of T4 Non-dihyderopyridine
to T3?, decrease Ca channel blockers
sympathetic stimulation is also dangerous.
mediated symptoms in
hyperthyroidism.
Glaucoma
once-per-day dosing
Glaucoma Systemic effects if
HT absorbed in large
quantities.
Migraine
less incidence of
rebound hypertension
less bradycardia
HT
Stable CHF (class II &III)
 Labetalol It blocks of α1, β1 and β2- Hypertension w/o reflex Orthostatic hypotension
receptors tachycardia Dizziness
Selective Beta Metaprolol/ atenolol All are much more potent at β1 Angina Similar to propanolol
1 Blockers than β2 receptors at higher Hypertension
doses may block β2 as well.
Lesser risk of bronchospasm Rest similar to
Propranolol.
and do not prolong
hypoglycemia Metaprolol also indicated
for Post MI arrhythmias
Acebutolol Partial agonist hypertension,
dysrhythmias
Esmolol Very rapid onset & short Used as IV infusion for
duration of action peri-operative
tachycardia and
hypertension,
arrhthymias
Used in electroconvulsive
therapy
Betaxolol Glaucoma
Always remember about Autonomic Control of Heart
Cholinergic innervation found only in atrial and nodal cells.
Adrenergic innervation is found throughout the heart.
More symp to AV node than SA node.
Remember

Disease Contraindicated Reason

COPD, asthma B-blockers Induction of bronchospasm
ACE-I Induction of cough, use AT1
Bradycardia Clonidine Aggravation, risk of Adams-Stokes
B-blocker syndrome

Verapamil/diltiazem
Diabetes Thiazides Reduced glucose tolerance
B-blockers Blunt sx of hypoglycemia
Gout Thiazides Reduced excrfetion of uric acid
Low dose Aspirin
CAD Hydralazine Provocation of angina (reflex tachycardia)
Prazosin
Minoxidil
Peripheral artery occlusive disease B-blockers Aggravation/manifestation
CHF Ca++ antagonist Negative inotrope
B-blockers
Renal failure Amiloride, Triamterene May cause hyperkalemia
Spironolactone
ACE-I Plasma concentration up, side effects