‫منــارة التعلــيم الصــيدلي فـــي مصــر ومحيطــها اإلقليـــمي‬

‫أول كلية صيدلة معتمدة من الهيئة القومية لضمان جودة التعليم واالعتماد‬

Students working in Groups

Course Name: Pharmacology 1

Course Code: 303
Academic Program: Bachelor of Pharmacy, 3rd year
Academic Year: 2019/2020

Title of Research: Beta blockers

Student (1) Name: ‫طارق محمود سعداوي محمد‬
Student (1) ID: 30279
National ID: 29811142403339
Student Email: Tarek.mah.saadawy@std.pharma.cu.edu.eg
Student (1) Role in the research:Data collection

Student (2) Name: ‫عبدالرحمن احمد دهشان عبدالعال‬

Student (2) ID: 30281
National ID: 29901092102072
Student Email: abdelrahman.ahm.dahshan@std.pharma.cu.edu.eg

Student (2) Role in the research: Data Collection

Student (3) Name: ‫عبدالرحمن حسن محمد عبدالرحمن‬

Student (3) ID: 30284

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National ID: 30002082102393
Student Email: abdelrahman.has.mohamed@std.pharma.cu.edu.eg

Student (3) Role in the research: Data collection

Student (4) Name: ‫عبدالرحمن محمد سعيد عبدالعزيز‬

Student (4) ID : 30286
National ID: 29902060102476
Student Email: Abdelrahman.moh.saeed@std.pharma.cu.edu.eg
Student (4) Role in the research: Data summarization and word

Student (5) Name: ‫عبدالرحمن مصطفى عبدالذاكر احمد‬

Student (5) ID: 30287
National ID: 29908140100731
Student Email: abdelrahman.mou.abdelzakir@std.pharma.cu.edu.eg
Student (5) Role in the research: Data summarization and word

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Abstract:

Beta blockers or adrenergic blocking agents are medications that lowers

blood pressure by working as competitive antagonist on beta adrenergic

receptors β1 and β2 to block effects of the hormone epinephrine, they cause

heart to beat slowly and affect smooth muscles contraction but do they worsen

symptoms of bronchial asthma? Do they cause contraction of smooth muscle’s

air way? The short answer is No as studies have been done and they showed

that in mild and moderate asthma chronic use of cardio selective beta blockers

didn’t precipitate any asthma attacks but it actually improved the response to

medication because of receptor up regulation mediated by the antagonist ,And

so beta blockers aren’t dangerous to be used in case of bronchial asthma in fact

they even safer than non-selective blockers .

Introduction:

Beta blockers is a group of drugs that act as antagonists for beta receptors
and used for treating many conditions such as cardiovascular diseases and other
diseases. Firstly, beta receptors are three types beta 1 receptor, beta 2 receptor
and beta 3 receptor. B1 receptors are located in the heart and affect the activity
of the heart by mediating it. B2 receptors have diverse locations in different sites
in many organs in the body, so it can control various aspects of metabolic
activity and induce relaxation of smooth muscles. B3 receptors have less
clinically relevant importance and they induce fat cells breakdown. So in case
of blockage of these three receptors by beta blockers drugs, we can get benefits
by treating many diseases. Beta blockers as a class of drugs are important and
can be considered as a first line treatment in many chronic and acute conditions.

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Beta blockers have FDA (food and drug administration) approval and are
indicated for the treatment of many conditions such as myocardial infarction,
tachycardia, hypertension, cardiac arrhythmia, coronary artery disease,
congestive heart failure, essential tremors, hyperthyroidism, portal
hypertension, aortic dissection, migraine prophylaxis, glaucoma and other
diseases. They also are used for treating of less common conditions for example
hypertrophic obstructive cardiomyopathy and long qt syndrome. Beta blockers
available in many dosage forms such as ophthalmic, intravenous and oral
dosage forms, but the route of administration often depends on the disease type
(e.g. topical use in glaucoma), chronicity of the disease and disease acuity ( e.g.
parental use in arrhythmia). As beta blockers affect smooth muscle contraction,
we should conclude that beta blockers can cause contraction of smooth muscles
of the airway, so someone may predict that they worsen the symptoms of
bronchial asthma due to making the breathing more difficult by
bronchoconstriction, but is that true?, and if it is necessary to use beta blockers
how to evaluate the case?. (farzam and Jan, 2019)

-Beta blockers: your asthma’s friendly foe.

Mechanism of action:
-Beta blockers act as competitive antagonists on beta adrenergic receptors
β1 and β2 (Gs subtype GPCR) found in the heart and vasculature and
respiratory smooth muscles, so it blocks the sympathomimetic activity induced
by endogenous catecholamines epinephrine and norepinephrine. (Frishman et
al.,2005)

-They affect blood pressure, heart rate and smooth muscles contraction in the
airways. (Frishman et al.,2005)

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Figure[1] Beta Blockers

mechanism of action. (Ladage et al.,2012)

Pharmacokinetics (Johnsson and Regårdh,1976):

1) Absorption: Rapidly and completely absorbed from the GIT with higher rate
in young than elderly patients.
2) t1/2 distribution: 5-30 mins.
3) Vd: above the body physiological fluid amount.
4) Metabolism: The more lipophilic is completely metabolised within the liver,
but the less lipophilic is excreted through the kidneys.
5) Elimination t1/2: 2-4 hrs with higher values for atenolol and sotalol.

-Here is a summary of some controversial studies concerned about these

questions:

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1-In mild and moderate asthma, chronic use of cardio-selective beta
blockers didn’t precipitate asthma attacks, but it actually improved
response to albuterol bronchodilator (Short et al.,2013)
2-This study was done to determine the effect of beta blockers on asthma
severe exacerbation requiring oral steroids and it showed that oral beta
blockers will not produce significant effect in patients on oral steroids.
(Morales et al.,2011)
3-This study describes the safety of using beta blockers in patients with
asthma and cardiovascular disease (CVD) and it shows that cardio-
selective β blockers didn’t produce exacerbation of asthma, but non
selective β
blockers increased the risk of asthma at low doses. (Morales et al.,2017)
4-The study suggests that use of beta blockers is well tolerated by asthma
patients and can reduce airway hyperresponsiveness with long-term use.
(Arboe and Ulrik,2013)
5-The article is concerned about weighing the risks against the benefits of
using β blockers in CHF patients with asthma or COPD and it showed
that the use of cardio-selective blockers is more safe than the non-
selective blockers with improved responsiveness to treatment with β2
agonist due to receptor up regulation mediated by the antagonist.
(Salpeter,2003)
6-Beta blockers should be avoided with asthma patients as they make it worse
due to bronchoconstriction, but in a patient with heart attack and asthma beta
blockers can be used in a selective initial dose that affects only the heart not the
bronchial muscles. (Fanta et al.,2003)

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Conclusion:
As the research showed, cardio-selective beta blockers are safe to be used
in case of asthma patients with cardiovascular diseases, because the studies in
this research showed that cardio-selective beta blockers can improve
responsiveness of the smooth muscles of the airway to bronchodilators.
The studies also revealed selective beta blockers are only to be used in case of
asthma patients with heart diseases, because non-selective beta blockers have
shown higher bronchoconstriction effect to the smooth muscles of the airway
than selective beta blockers, and this effect cannot be tolerated by asthma
patients.

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References:

1)Fanta, C. H., Cristiano, L. M., & Haver, K. E. (2003). when asthma doesn't
get better. In The Harvard Medical School guide to taking control of
asthma: a comprehensive prevention and treatment plan for you and your
family (illustrated, pp. 249–249). essay, New York: Free Press.

2) Farzam K, Jan A. Beta Blockers. [Updated 2019 Nov 21]. In: StatPearls
[Internet]. Treasure Island (FL): StatPearls Publishing; 2020 Jan-..

3)Frishman, W. H., Cheng-Lai, A., & Nawarskas, J. (2011). beta adrenergic

receptors antagonists. In Current cardiovascular drugs (4th ed., pp. 151–
151). essay, Philadelphia, PA: Current Medicine.

4)Johnsson, G., & Regårdh, C.-G. (1976). Clinical Pharmacokinetics of β-

Adrenoreceptor Blocking Drugs. Clinical Pharmacokinetics, 1(4), 233–
263. http://doi.org/10.2165/00003088-197601040-00001

5)Ladage, D., Schwinger, R. H., & Brixius, K. (2012). Cardio-Selective Beta-

Blocker: Pharmacological Evidence and Their Influence on Exercise
Capacity. Cardiovascular Therapeutics, 31(2), 76–83.
http://doi.org/10.1111/j.1755-5922.2011.00306.x

6)Morales, D. R., Guthrie, B., Lipworth, B. J., Donnan, P. T., & Jackson, C.
(2011). Prescribing of -adrenoceptor antagonists in asthma: an
observational study. Thorax, 66(6), 502–507.
http://doi.org/10.1136/thoraxjnl-2011-200067

7)Morales, D. R., Lipworth, B. J., Donnan, P. T., Jackson, C., & Guthrie, B.
(2017). Respiratory effect of beta-blockers in people with asthma and
cardiovascular disease: population-based nested case control study. BMC
Medicine, 15(1). http://doi.org/10.1186/s12916-017-0781-0

8)Salpeter, S. (2003, November 14). Cardioselective Beta Blocker Use in

Patients With Asthma. Retrieved May 24, 2020, from
https://www.medscape.com/viewarticle/464040_4

9)Short, P. M., Williamson, P. A., Anderson, W. J., & Lipworth, B. J. (2013).

Randomized Placebo-controlled Trial to Evaluate Chronic Dosing Effects
of Propranolol in Asthma. American Journal of Respiratory and Critical
Care Medicine, 187(12), 1308–1314. http://doi.org/10.1164/rccm.201212-
2206oc

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10)Ulrik, C., & Arboe, bente. (2013). Beta-blockers: friend or foe in asthma?
International Journal of General Medicine, 6, 549–555.
http://doi.org/10.2147/ijgm.s46592