Assignment: Effects of E-Adrenoceptor Antagonists on Exercise

Discuss about the Effects of E-Adrenoceptor Antagonists on Exercise Induced Cardiovascular Changes.

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Introduction

Beta – adrenoceptors are binded  by beta blockers drugs which block the binding of norepinephrine and epinephrine receptors. These cause inhibition of the effects which act on the receptors. Beta blockers act as drugs which are sympatholytic. Often beta blockers bind to beta-adrenoceptors which partially activates the receptors which activates them while offering prevention of norepinephrine from binding the receptor. The partial agonists thus provide backgrounds for sympathetic activity while offering prevention of normal and enhanced sympathetic activity. The beta blockers possess aspect of intrinsic sympathomimetic activity while others produce stabilizing activity, thus producing similar activites as observed on membrane stabilization activity by sodium channels blockers.[i]

Beta blockers bind themselves to beta adrenoceptors which are located in cardiac area surrounding the nodal tissue, which conduct the system and offers contraction of myocytes. The beat has been shown to have both β₁ and β₂ adrenoceptors, which the common is β₁ adrenoceptors. It offers binding effect on the norepinephrine which releases itself to sympathetic nerves located in adrenergic area. Beta blockers in this case offer binding protection to normal ligand β-adrenoceptors through competing itself on the binding sites.[ii]

Beta adrenoceptors are coupled by the Gs protein which offers activation of adenyl cyclase forming Camp located in the ATP which increases the Camp and thus activated the dependent protein kinase. With the general level of sympathetic tone in the heart, these beta blockers are able to lower down the sympathetic influence which offers stimulation of the heart rate, contractility, electrical conduction and relaxation. This leads to reduction in heart rate, contractility, velocity conduction and relaxation. These kinds of drugs have been shown to have an effect on the elevated levels of sympathetic activity.[iii]

With concern of cardiovascular health, beta blockers often offer little vascular effect due to the β₂ adrenoceptors having small function of the modulator in the basal vascular tone. Blockage of β₂ adrenoceptors is linked to smaller degree of vasoconstriction in the vascular beds.[iv]

Studies have shown that β₁ and β₂ adrenoceptor receptors are associated increased intensity of vascular activity, it stimulates in response to the constriction and relaxation of the arteries and veins.[v] Endothelial cells are not produced through mediation of β₁ and β₂ adrenoceptors, rather they play a key role in influcneing blood vessel activity, further the role played the vascular activity is key in prevention and treatment of vascular disease, thus assessing the different morphology of cardiac function is relevant in establishing effects of β₁ and β₂ adrenoceptors. [vi]

Beta-adrenoceptor antagonists function in cardiovascular management by lowering elevated blood pressure. Compounds such as Atenol selectively apply to Beta 1-adrenoceptor which possess intrinsic sympathomimetic activity. [vii] Pindol on the other hand has non selective ability of beta-adrenoceptor which possesses sympathomimetic activity. These study evaluates its application when used in two body states that is during rest and exercise activities, medical and therapeutic effects of both drugs is being tested. The study is a double blind using vitamin B6 as a placebo control.

This study thus seeks to examine the effects of orally administered β adrenoceptors antagonists, Atenolol and Pendolol on the blood pressure effects, heart rate and lung function during two critical phases of rest and after exercise activity. Assignment: Effects of E-Adrenoceptor Antagonists on Exercise

Methods and materials

The study experiment was submitted to the University of New South Wales, health science department for ethical approval. This experimental study employed double blind design , where subjects were blinded and utilized placebo and control usage. The subject participants involved students aged between 18-65 years of the University of New South Wales.

The materials need for this study included Perceived Exertion Scale, heart rate monitor having watch, strap and polar, blood pressure monitor, peak flow meter and a timer. The experimental phase involved two stages; pre drug and post drug . at the pre drug phase, the start the timer at 0 minutes and time adjusted to resistance level to obtain the KP level, then hold KP level at 50rpm for 2 minutes. During the last 10 seconds, recording of the heart rate, (EHR) and exertion level are undertaken. At 15 minutes recoding s of resting heart rate (RHR) is taken, while at 30 minutes, RHR, oxygen saturation, blood pressure and lung function is undertaken. Then bike exercise undertaken while the KP levels is set at 2 minutes repeat the assessment of EHR, oxygen saturation and exertion levels.

At post drug level, drug is consumed and measurements taken at 15 minutes rest, record thee RHR, oxygen saturation, blood pressure and lung function test for the participant, again the assessments are undertaken at 30 minutes , rest, 45 minutes rest, 60 minutes rest, 75 minutes rest  and 90 minutes rest post drug ingestion rest level . after 90 minutes start the bike then set at KP levels  for 2 minutes then take the assessments of HER, oxygen saturation and exertion level.

Results

Pre drug treatment results

Time/min	Resting heart rate beats/min	BP- dbp/sbp mmHg	PEFR L/min	ROS SpO2 %	EOS	EHR Beats/min	Fatigue
	Rest				Exercise
0	82	115/76	434	98	97	399	10.6
15	87	116/75	441	97
30	86	113/74	445	97	95	114	11
Average	84	117/75	440	97	97	215	11.2

Table 1 showing the pre drug assessment of the various assessment indicators.

Key ; PEFR(Peak expiratory flow rate), ROS( rate of oxygen saturation ), EOS(Exercise oxygen saturation), HER- (Heart exercise rate)

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Post drug treatment results

Time/min	SBP/DBP mmHg
	Vit B6	Atenolol	Pendalol
60	117/72	113/69	106/70
90	118/70	107/67	104/65
120	115/69	108/70	101/64
Average	116/71	109/68	103/66

Table 2 showing the blood pressure assessment

Time/min	RHR beats/min
	Vit B6	Atenolol	Pendalol
60	79	79.5	71
90	79	79	72
120	82	82	71
Average	80	80	71.

Table 2 : showing resting heart rate

Time/min	PEFRL/min
	Vit B6	Atenolol	Pendalol
60	475	451	415
90	460	456	450
120	480	457	451
Average	471	451	438

Table 3 showing the rate of peak expiratory rate

Time/min

ROS SpO2%

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