LYCEUM OF THE PHILIPPINES UNIVERSITY

(BATANGAS)
A DRUG COMPLETION FOR THE REQUIREMENTS OF
COLLEGE OF NURSING

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SUBMITTED BY:
MARA VIVIENNE DOCTOR- HERRERA
BSN IV-1 OSP

DEFINITION

There are three known types of beta receptor, designated β1, β2 and β3. β -
adrenergic receptor are all located on postsynaptic effector cells. The β₁- adrenergic
receptors are located in the heart and kidney; β₂-Adrenergic receptors are located
mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle,
and skeletal muscle. β₃- receptors are located in fat cells.
Beta-adrenergic blocking agents, beta-adrenergic or beta antagonists may also
referred to as beta- blockers. (sometimes written as β-blocker).

Beta blockers inhibit these normal epinephrine-mediated sympathetic actions, but

have minimal effect on resting subjects. That is, they reduce the effect of
excitement/physical exertion on heart rate and force of contraction, dilation of blood
vessels and opening of bronchi, and also reduce tremor and breakdown of glycogen.

It is therefore expected that non-selective beta blockers have an antihypertensive

effect. The antihypertensive mechanism appears to involve reduction in cardiac
output (due to negative chronotropic and inotropic effects), reduction in renin
release from the kidneys, and a central nervous system effect to reduce
sympathetic activity (for those β-blockers that do cross the blood-brain barrier, e.g.
Propranolol).(1)

The nonselective beta-blockers, including propranolol, oxprenolol, pindolol, nadolol,

timolol and labetalol, each antagonize both b1 - and b2-adrenergic receptors. For
the selective antagonists, including metoprolol, atenolol, esmolol, and acebutolol,
each has much greater binding affinity for the b1 adrenergic receptor. The selective
beta-blockers are normally indicated for patients in whom b2-receptor antagonism
might be associated with an increased risk of adverse effects. Such patients include
those with asthma or diabetes, or patients with peripheral vascular disease or
Raynaud's disease. (2)

Antianginal effects result from negative chronotropic and inotropic effects, which
decrease cardiac workload and oxygen demand. Negative chronotropic properties of
beta blockers allow the lifesaving property of Heart rate control. Beta blockers are
readily titrated to optimal rate control in many pathologic states.

The antiarrhythmic effects of beta blockers arise from sympathetic nervous system
blockade – resulting in depression of sinus node function and atrioventricular node
conduction, and prolonged atrial refractory periods. Sotalol, in particular, has
additional antiarrhythmic properties and prolongs action potential duration through
potassium channel blockade.

Blockade of the sympathetic nervous system on renin release leads to reduced

aldosterone via the renin angiotensin aldosterone system with a resultant decrease
in blood pressure due to decreased sodium and water retention.(1)

PHARMACOKINETICS

Stimulation of β1 receptors by epinephrine induces a positive chronotropic and

inotropic effect on the heart and increases cardiac conduction velocity and
automaticity. Stimulation of β1 receptors on the kidney causes renin release.
Stimulation of β2 receptors induces smooth muscle relaxation, induces tremor in
skeletal muscle, and increases glycogenolysis in the liver and skeletal muscle.
Stimulation of β3 receptors induces lipolysis. (1)

There are no general pattern in the degree and/or direction of stereoselectivity

among different beta-blockers. This is perhaps because β-adrenergic antagonists
encompass a wide spectrum of pharmacokinetic properties, with low to high
degrees of plasma protein binding, extent of excretion into urine as unchanged
drug, and hepatic extraction ratios. Additionally, the degree and direction of
stereoselectivity in the pharmacokinetics of these drugs are susceptible to change
because of patient and/or disease characteristics. Because of the significant
enantioselectivity in the pharmacologic effects of beta-blockers, a stereoselective
change in the pharmacokinetics of these drugs may be associated with an altered
pharmacodynamic profile. (2)

The pharmacokinetics of beta-blocking drugs can also be influenced by race, age,

cigarette smoking and concomitant drug therapy. The wide interpatient variability in
plasma drug concentration observed with beta-blockers makes this parameter
unreliable in routine patient management. Despite the pharmacokinetic differences
among the beta-blockers, these drugs should always be titrated in the individual
patient to achieve the desired clinical response. (3)

PHARMACODYNAMICS

β – adrenergic blockers also have a profound effect on the conduction system of the
heart. The AV node normally receives impulse stimulation from the SA node and
slows it down so that the ventricles have time to fill before they are stimulated to
contract. Conduction in the SA node, which spontaneously depolarizes at the most
frequent rate, is slowed by β – adrenergic blockers, which results in a decreased
heart rate. These drugs also slow conduction through the AV node. These effects of
β – adrenergic blockers on the conduction system of the heart make them useful
drug in the treatment of various type of irregular heart rhythms, called
dysrhythmias.

Their ability to reduce SNS stimulation of the heart, including reducing heart rate
and the force of myocardial contraction (systole), renders β – adrenergic blockers
useful in treating hypertension. Traditionally β – adrenergic blockers were thought to
worsen heart failure. However, recent studies have shown benefit to the use of β –
adrenergic blockers. Certain β – adrenergic blockers such as carvedilol and
metoprolol have produced the best results to date. The form of heart failure that
includes a diastolic dysfunction component responds especially favorably to β –
adrenergic blockers.(4)
INDICATION
Beta blockers are a class of drugs used for various indications, but particularly for
the management of

• cardiac arrhythmias,

• cardioprotection after myocardial infarction (heart attack),

• hypertension.

Other Indications for beta blockers include:

• Angina

• Mitral valve prolapse

• Atrial fibrillation

• Congestive heart failure

• Glaucoma

• Migraine prophylaxis

• Symptomatic control (tachycardia, tremor) in anxiety and hyperthyroidism

• Essential tremor

• Phaeochromocytoma, in conjunction with α-blocker (1)

NURSING MANAGEMENT
1. Administer oral beta-blocker before meals and at a.m. If insomnia occurs.
2. Check client’s apical pulse rate before drug administration, refer if below
60bpm.
3. Hypotensive precautions
4. Warn clients not to drive or operate dangerous machinery until he/she has
adjusted to medications.(5)
5. Monitor vital signs and pulse, observe for signs of bradycardia, heart failure,
orpulmonary edema. (Beta-blockers decrease heart rate and cardiac output.)
 6. Monitor for orthostatic hypotension. (Beta-blockers cause orthostatic
hypotension.)
7. Observe for drowsiness, fatigue, and weakness. (These are side effects of
betablockers.)
8. In diabetic clients, monitor for hypoglycemia. (Some beta-blockers may lower
blood glucose levels.)
9. Monitor for effects on the heart, especially with exertion. (Beta-blockers can
decrease cardiac output.)(6)

CARDIO-SELECTIVE AGENTS

DRUG DOSE/ ROUTE OF ADMINISTRATION

ACEBUTOL ADULT:
OL PO:400-800 mg/day
(Sectral) 600-1200 mg/day divided bid

ATENOLOL ADULT:
(Tenormin) PO: 50-100 mg/day daily or bid
50-200 mg/day or bid
IV: 5 mg over 5 min; repeat in 10 min

ADULT:
ESMOLOL IV: Bolus of 500 mcg/kg over 1 min, followed by 4 min at 50 mcg/kg/min and
(Brevibloc) evaluate
IV: 80 mg bolus over 30 min followed by 150 mcg/kg/infusion

NON- SELECTIVE AGENTS

PROPANOL ADULT:
OL PO: 80-320 mg/day divided bid-qid
(Inderal) 120- 640 mg/day divided bid- tid
10-30 mg tid-qid
20-40 mg tid/qid
120-320 mg/day divided
30-60 mg/day divided for 3 days before surgery with an α-blocker also
IV: 1 mg slow IV push, may repeat every 5 min up to 5 mg
 SOTALOL
(Betapace) ADULT:
PO: 160-320 mg/day divided

CARVEDILO ADULT:
L PO: 3.125 mg bid; may double dose every 2wk to highest tolerated dose,
(Coreg) max 50 mg/day

p.270-293, Liley, Harrington, Synder; Pharmacology and the Nursing Process; Fifth Edition; 2007.

SAMPLE OF (DRUG) IMAGES

ACEBUTOLOL
(Sectral)

ATENOLOL
(Tenormin)
 ESMOLOL
(Brevibloc)

PROPANOLOL
(Inderal)

SOTALOL
(Betapace)
 CARVEDILOL
(Coreg)

SIDE EFFECTS

Low Blood Pressure

Asthma

Low Blood Pressure

Nausea

Slow Heart Rate

Headaches

Impaired Circulation

Dizziness

Loss of Sleep

Muscle Cramps

Heart Failure

Peyronie's disease
ADVERSE REACTION

nausea abnormal vision

diarrhea decreased concentration

bronchospasm hallucinations

dyspnea insomnia

cold extremities nightmares

exacerbation of Raynaud's clinical depression

syndrome

sexual dysfunction
bradycardia

erectile dysfunction and/or

hypotension alteration of glucose

heart failure lipid metabolism

heart block

fatigue
http://en.wikipedia.org/wiki/Beta_blocker

dizziness
 DOCUMENT REFERENCES:

1. http://en.wikipedia.org/wiki/Beta_blocker
2.http://www.ualberta.ca/~csps/JPPS4(2)/R.Mehvar/betablockers.htm
3.http://www.ncbi.nlm.nih.gov/pubmed/1674683
4. p.270-293, Liley, Harrington, Synder; Pharmacology and the Nursing Process; Fifth
Edition; 2007.
5.http://www.scribd.com/doc/10455366/Pharmacology
6.http://wps.prenhall.com/wps/media/objects/3775/3866436/npf_charts/ch23/Beta-
adrenergic%20Antagonist.pdf

IMAGE REFERENCES:
(WEB)

ACEBUTOLOL
(Sectral)
https://members.kaiserpermanente.org/kpweb/image/feature/026drugency/drugphotos/WYE
41790.JPG

ATENOLOL
(Tenormin)
http://ordertenormin.org/images/tenormin.jpg
https://members.kaiserpermanente.org/kpweb/image/feature/026drugency/drugphotos/ZNC
01050.JPG

ESMOLOL
(Brevibloc)
http://www.frca.co.uk/images/esmolol.jpg

PROPANOLOL
(Inderal)
http://www.aclepsa.com/images/prescriptions/inderal_tn.jpg
http://www.drugs.com/images/pills/mmx/t103963f/inderal_la.jpg

SOTALOL
(Betapace)
http://www.peacehealth.org/kbase/media/medical/multum/betapace160mg.jpg

CARVEDILOL
(Coreg)
http://www.patentlyo.com/patent/081208_0235_NoInequitab1.jpg
http://www.drugs.com/images/pills/mtm/Coreg%2012.5%20mg.jpg

VISIT: