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Beta blockers and calcium channel blockers
1.
2.
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.
.
3. Beta blockers, also known
as
beta-adrenergic
blocking agents or beta
antagonists,
or
betaadrenergic
antagonists,
are
medications
that
reduce
blood pressure.
Beta blockers work by
blocking the effects of the
hormone epinephrine, also
known as adrenaline.
4.
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).
5. 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.
8.
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
15.
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.
16. 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.
17.
Glucagon is the specific antidote for betablocker 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.
18.
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.
19.
20.
21.
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.
22. 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)
24. 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)
25. 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 Ntype calcium channel blocker that has
potent analgesic properties.
27.
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
28.
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.
30. Constipation
nausea
Headache
Rash
edema (swelling of the legs with fluid)
low blood pressure
drowsiness and dizziness
sexual dysfunction.
31.
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.
32. 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.
33.
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