SEMINAR

ON
BETA BLOCKERS
AND
CALCIUM CHANNEL BLOCKERS

PRESENTED BY;
UMADEVI.K
IIND YEAR MSc NURSING
THE OXFORD COLLEGE OF NURSING
 INTRODUCTION
 Beta blockers and calcium channel blockers are widely
prescribed for a range of conditions and are now widely used
in the management of cardiovascular disease.

 In 1958, the first beta blocker, dichloroisoproterenol, was

synthesised by Eli Lilly Laboratories.

 Sir James W Black in 1962, found the first clinically

significant beta blockers – Propranolol and Pronethalol

 Calcium channel blockers were first identified in the lab of

German pharmacologist Albrecht Fleckenstein beginning in
1964 and are now widely used and have potent vasodialatory
effect.

 BETA BLOCKERS
Beta
blockers, also known as
beta-adrenergic blocking
agents or beta antagonists,
or beta-adrenergic
antagonists, are
medications that reduce
blood pressure. Beta
blockers work by blocking
the effects of the hormone
epinephrine, also known as
adrenaline.
 BETA RECEPTORS

 Beta receptors are found on cells of the heart

muscles, smooth muscles, airways, arteries,
kidneys, and other tissues that are part of the
sympathetic nervous system and lead to stress
responses, especially when they are stimulated by
epinephrine (adrenaline).
 TYPES OF BETA RECEPTERS
 Three types of beta receptors are known,
designated β1, β2 and β3 receptors.
 β1-adrenergic receptors are located mainly in
the heart and in the kidneys.
 β2-adrenergic receptors are located mainly in
the lungs, gastrointestinal tract, liver, uterus,
vascular smooth muscle, and skeletal muscle.
 β3-adrenergic receptors are located in fat cells.
MECHANISM OF ACTION
 INDICATIONS
 Angina pectoris
 Atrial fibrillation
 Cardiac arrhythmia
 Congestive heart failure
 Essential tremor
 Glaucoma
 Hypertension
 Migraine prophylaxis
 Mitral valve prolapse
 Myocardial infarction
 Phaeochromocytoma, in conjunction with α-
blocker
 Postural orthostatic tachycardia syndrome
 Symptomatic control (tachycardia, tremor) in
anxiety and hyperthyroidism
 Theophylline overdose
 Acute aortic dissection
 Hypertrophic obstructive cardiomyopathy
 Marfan syndrome (treatment with propranolol
slows progression of aortic dilation and its
complications)
 Prevention of variceal bleeding in portal
hypertension
 CONTRAINDICATIONS

 cocaine-induced tachycardia
 sinus bradycardia
 partial AV block
 peripheral vascular diseases
 diabetes mellitus
 chronic obstructive pulmonary disease (COPD)
and
 asthma
 ADVERSE EFFECTS

 Nausea
 diarrhea
 bronchospasm
 dyspnea
 cold extremities
 exacerbation of Raynaud's syndrome
 bradycardia
 hypotension,
 heart failure
 heart block
 fatigue
 dizziness
 alopecia (hair loss)
 abnormal vision
 hallucinations
 insomnia
 nightmares
 sexual dysfunction
 alteration of glucose and lipid metabolism.
 Adverse effects associated with β2-adrenergic
receptor antagonist activity (bronchospasm,
peripheral vasoconstriction, alteration of glucose
and lipid metabolism)
DOSAGE
 EXAMPLES OF BETA BLOCKERS
 Acebutolol (Sectral)
 Atenolol (Tenormin)
 Betaxolol (Kerlone, discontinued)
 Betaxolol (Betoptic, Betoptic S)
 Bisoprolol fumarate (Zebeta)
 Carteolol (Cartrol, discontinued)
 Carvedilol (Coreg)
 Esmolol (Brevibloc)
 Labetalol (Trandate, Normodyne)
 Metoprolol (Lopressor, Toprol XL)
 Nadolol (Corgard)
 nebivolol (Bystolic)
 penbutolol (Levatol)
 pindolol (Visken, discontinued)
 propranolol (Inderal, InnoPran)
 sotalol (Betapace)
 timolol (Blocadren, discontinued)
 timolol ophthalmic solution (Timoptic)
 DRUG INTERACTIONS
 Combining propranolol (Inderal) or pindolol
(Visken) with thioridazine (Mellaril) or
chlorpromazine (Thorazine) may result in low
blood pressure (hypotension) and abnormal heart
rhythms because the drugs interfere with each
others' elimination and result in increased levels
of the drugs.
 Dangerous elevations in blood pressure may occur
when clonidine (Catapres) is combined with a beta
blocker
 Phenobarbital and similar agents may increase the
breakdown and reduce blood levels of propanolol
(Inderal) or metoprolol (Lopressor, Toprol XL). This
may reduce effectiveness of the beta blocker.
 Aspirin and other nonsteroidal antiinflammatory
drugs (NSAIDs) (for example, ibuprofen) may
counteract the blood pressure reducing effects of beta
blockers by reducing the effects of prostaglandins.
Prostaglandins play a role in control of blood
pressure.
 TOXICITY
 Glucagon is the specific antidote for beta-
blocker poisoning, because it increases
intracellular cAMP and cardiac contractility

 Patients who experience Bronchospasm due to

the Beta2 blocking effects of nonselective beta
blockers may be treated with anticholinergic
drugs, such as Ipratropium, which are safer than
beta agonists in patients with cardiovascular
disease. Another antidote for beta blocker
poisoning are Salbutamol and Isoprenaline.
 CALCIUM CHANNEL BLOCKERS

 A calcium channel blocker

(CCB) is a chemical that
disrupts the movement of
calcium (Ca2+) through calcium
channels. Calcium channel
blockers are used as
antihypertensive drugs.
DRUG ACTION
MECHANISM OF ACTION
 CCBs used as medications primarily have three
effects:

 by acting on vascular smooth muscle they reduce

contraction of the arteries and cause an increase in
arterial diameter, a phenomenon called vasodilation
(CCBs do not work on venous smooth muscle)

 by acting on cardiac muscles (myocardium), they

reduce the force of contraction of the heart

 by slowing down the conduction of electrical activity

within the heart, they slow down the heart beat.
 CLASSIFICATIONS
1. Dihydropyridine
 Dihydropyridine calcium channel blockers are
derived from the molecule dihydropyridine and
often used to reduce systemic vascular resistance
and arterial pressure, but are not used to treat
angina
 This CCB class is easily identified by the suffix
"-dipine"
 Amlodipine (Norvasc)
 Aranidipine (Sapresta)
 Azelnidipine (Calblock)
2.Non-dihydropyridine
 Phenylalkylamine
 Phenylalkylamine calcium channel blockers
are relatively selective for myocardium, reduce
myocardial oxygen demand and reverse coronary
vasospasm, and are often used to treat angina
 EXAMPLES ARE:
 Verapamil (Calan, Isoptin)
 Gallopamil
 Fendiline
3.Benzothiazepine

 Benzothiazepine calcium channel blockers belong

to the benzothiazepine class of compounds and are
an intermediate class between phenylalkylamine and
dihydropyridines in their selectivity for vascular
calcium channels.
 EXAMPLE :Diltiazem (Cardizem) (also used
experimentally to prevent migraine)
4.Nonselective
 While most of the agents listed above are relatively
selective, there are additional agents that are
considered nonselective. These include mibefradil,
bepridil, flunarizine
5. Ziconotide
 Ziconotide, a peptide compound derived from the
omega-conotoxin, is a selective N-type calcium
channel blocker that has potent analgesic properties.
 EXAMPLES OF CALCIUM CHANNEL
BLOCKERS
 AMLODIPINE (NORVASC)
 CLEVIDIPINE (CLEVIPREX)
 DILTIAZEM (CARDIZEM),
 FELODIPINE (PLENDIL),
 ISRADIPINE (DYNACIRC),
 NIFEDIPINE (ADALAT, PROCARDIA),
 NICARDIPINE (CARDENE),
 NIMODIPINE (NIMOTOP),
 NISOLDIPINE (SULAR), AND
 VERAPAMIL (CALAN, ISOPTIN).
 INDICATIONS
 CCBs are used for treating high blood pressure,
angina, and abnormal heart rhythms.
 They also may be used after a heart attack
 They also are used for treating:
 pulmonary hypertension,
 Raynaud's syndrome,
 cardiomyopathy, and
 subarachnoid hemorrhage.
 CCBs are also used in the prevention of migraine
headaches
 COMMON DRUGS AND DOSAGES

 AMLODIPINE (NORVASC®):
 Adult (usual) Angina: 5-10 mg po qd.
 BEPRIDIL (VASCOR®):
 usual dose: 300 mg/day; maximum daily dose:
400 mg
 CLEVIDIPINE -CLEVIPREX ®
 Intravenous infusion of Cleviprex at 1-2 mg/hour.
 DILTIAZEM (CARDIZEM ®):
 Adult (usual) Oral:usual dose 180-360 mg po
daily (ANGINA)
 usual dose 120-180 mg bid (HYPERTENSION)
 FELODIPINE (PLENDIL®):
 Adults: hypertension: Oral: 2.5-10 mg once
daily.
 NIFEDIPINE (PROCARDIA®):
 10-30 mg 3 times/day as capsules
 SIDE EFFECTS
 Constipation
 nausea
 Headache
 Rash
 edema (swelling of the legs with fluid)
 low blood pressure
 drowsiness and dizziness
 sexual dysfunction.
 DRUG INTERACTIONS
 Verapamil and diltiazem decrease the
elimination of a number of drugs by the liver.
Through this mechanism, verapamil and
diltiazem may reduce the elimination and
increase the blood levels of carbamazepine
(Tegretol), simvastatin (Zocor), atorvastatin
(Lipitor), and lovastatin (Mevacor). This can
lead to toxicity from these drugs.
 TOXICITY
 Mild CCB toxicity is treated with supportive care
 For severe overdoses, treatment usually includes
close monitoring of vital signs and the addition of
vasopressive agents and intravenous fluids for
blood pressure support. IV calcium gluconate (or
calcium chloride if a central line is available) and
atropine are first-line therapies.
 CONCLUSION
 Cardiovascular disease remains the leading cause
of morbidity and mortality among transplant
recipients. Therefore, antihypertensive therapy
should focus on those agents with proven benefit in
reducing the progression of cardiovascular disease.
Despite their effectiveness, CCB's often have a
high mortality rate over extended periods of use,
and have been known to have multiple side effects.
Beta-blockers, however, have been, are, and will
remain the cornerstone for the treatment of heart
failure
THANK UUUUUUUUUUUUUUUUUU……