• Due to the high penetration across the blood-brain barrier, lipophilic beta blockers such as propranolol and metoprolol are more likely than other less lipophilic beta blockers to cause sleep disturbances such as insomnia, vivid dreams and nightmares. (wikipedia.org)
  • A meta-analysis further supports reduced incidence of heart failure worsening in patients treated with beta-blockers compared to placebo. (wikipedia.org)
  • More lipophilic beta blockers tend to cross the blood-brain barrier more readily, with greater potential for effects in the central nervous system as well as associated neuropsychiatric side effects. (wikipedia.org)
  • Beta blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. (druglib.com)
  • If replacing clonidine by beta-blocker therapy, the introduction of beta blockers should be delayed for several days after clonidine administration has stopped. (druglib.com)
  • Concomitant use of prostaglandin synthase inhibiting drugs, eg, indomethacin, may decrease the hypotensive effects of beta blockers. (druglib.com)
  • Data from several studies, ie, TIMI-II, ISIS-2, currently do not suggest any clinical interaction between aspirin and beta blockers in the acute myocardial infarction setting. (druglib.com)
  • While taking beta blockers, patients with a history of anaphylactic reaction to a variety of allergens may have a more severe reaction on repeated challenge, either accidental, diagnostic or therapeutic. (druglib.com)
  • Beta-blockers have been in use for nearly 50 years. (medscape.com)
  • In addition to their traditional role in treating hypertension and other cardiovascular disorders, beta-blockers are also used for additional purposes such as migraine headaches, hyperthyroidism, glaucoma, anxiety, and various other disorders. (medscape.com)
  • Beta-blockers act as competitive inhibitors of catecholamines, exerting their effects at both central and peripheral receptors. (medscape.com)
  • much of the clinical and overdose experience that exists with beta-blockers was provided by case reports and clinical studies of this drug. (medscape.com)
  • Other nonselective beta-blockers include nadolol, timolol, and pindolol. (medscape.com)
  • Nonselective beta-blockers exert a wider variety of extracardiac manifestations. (medscape.com)
  • Some beta-blockers, such as pindolol and acebutolol, also have beta-agonist properties. (medscape.com)
  • Beta-blockers: May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. (nih.gov)
  • Patients with asthma should not normally be treated with beta-blockers. (nih.gov)
  • Beta-blockers: Use with caution. (nih.gov)
  • This chapter discusses two groups of drugs that affect the sympathetic nervous system-adrenergic agonists, or sympathomimetics , and adrenergic antagonists, also called adrenergic blockers or sympatholytics -along with their dosages and uses. (basicmedicalkey.com)
  • Patients receiving β-adrenergic blockers for an extended period following myocardial infarction have a higher chance of surviving. (benthamscience.com)
  • Beta-blockers in patients without heart failure after myocardial infarction. (benthamscience.com)
  • Harari R, Bangalore S. Beta-blockers after acute myocardial infarction: An old drug in urgent need of new evidence! (benthamscience.com)
  • this agent is a non-selective receptor blockers. (pharmacology2000.com)
  • To assess the effect of cardioselective beta-blockers in patients with asthma or COPD. (nih.gov)
  • Randomized, blinded, placebo-controlled trials of single dose or continued treatment of the effects of cardioselective beta-blockers in patients with reversible airway disease. (nih.gov)
  • Beta1-blockers were divided into those with or without intrinsic sympathomimetic activity (ISA). (nih.gov)
  • Cardioselective beta-blockers given in mild - moderate reversible airway disease or COPD, do not produce adverse respiratory effects in the short term. (nih.gov)
  • Beta-blockers bind to beta-adrenoceptors, which inhibit normal sympathetic effects that act through the receptors norepinephrine and epinephrine. (uspharmacist.com)
  • Nonselective beta-blockers block both beta receptors, whereas cardioselective beta-blockers bind to the beta-adrenoceptor and partially activate the receptor while preventing other receptor agonists from binding. (uspharmacist.com)
  • Beta blockers , which counter some of the effects of noradrenaline by blocking their receptors, are frequently used to treat glaucoma , migraine , and a range of cardiovascular problems. (wikipedia.org)
  • Increased sensitivity to bisoprolol, other components of the drug to other beta-blockers, - acute heart failure or heart failure decompensation requiring holding inotropic therapy - shock (including cardiogenic) - pulmonary edema - atrioventricular (AV) blockade II-III extent without the pacemaker, - sinoatrial block, - sick sinus syndrome, - bradycardia (heart rate less than 60 beats / min. (pharmru.com)
  • These effects are blocked by beta-adrenergic receptor blockers. (pharmacology2000.com)
  • β-adrenergic receptor blockers increase AV conduction time and increase AV nodal refractoriness, thereby helping to terminate nodal reentrant arrhythmias. (pharmacology2000.com)
  • Whether or not this activity is responsible for any relative sparing of beta2-adrenergic receptors, it is suggested that pindolol may be better tolerated in asthma and other obstructive lung diseases than other beta-adrenergic blockers. (onlineasthmainhalers.com)
  • However, Benson et al presented five asthmatic subjects whose FEVi decreased by more than 20 percent after receiving one or more beta-adrenergic blockers. (onlineasthmainhalers.com)
  • The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and asthma, for example. (targetmol.com)
  • This belongs to the group of medicines known as beta-blockers. (pharmacycode.com)
  • Cardiol - Carvedilol information Carvedilol is a blood pressure medication and belongs to the class of drugs known as beta-blockers. (medicatione.com)
  • These beta-blockers affect the circulatory system, which includes the human heart, arteries and veins. (medicatione.com)
  • Beta-blockers: May decrease effectiveness of PROAIR HFA and produce severe bronchospasm. (drugcite.com)
  • Although it is similar to metoprolol, atenolol differs from pindolol and propranolol in that it does not have intrinsic sympathomimetic properties or membrane-stabilizing activity. (druglib.com)
  • Propranolol is the most common beta-blocker involved in severe beta-blocker poisoning. (medscape.com)
  • Propranolol is a nonselective beta-blocker, demonstrating equal affinity for both beta1- and beta2-receptors. (medscape.com)
  • Results from using an in vitro tissue bath technique indicated that propranolol and preferential beta(2)-adrenoceptor antagonists (ICI-118,551 and butoxamine), in a concentration-dependent manner, blocked the relaxation induced by nicotine (100 microM) without affecting the relaxation elicited by transmural nerve stimulation (TNS, 8 Hz). (lookformedical.com)
  • Propranolol, a nonselective beta-adrenergic blocking drug, aggravates bronchospasm in asthmatics . (onlineasthmainhalers.com)
  • Our decrease in mean maximal exercise heart rate with 0.4 mg of pindolol, 26 beats per minute, is close to the 29 beats per minute determined by Epstein et al in normal subjects given 0.15 mg/kg of propranolol intravenously, suggesting a comparable degree of beta-adrenergic blockade. (onlineasthmainhalers.com)
  • In another study this effect was blocked by the coadministration of propranolol, nonselective beta-adrenergic antagonist. (drugcentral.org)
  • Intravenous (IV) adrenergic agonists and antagonists are high-alert medications because they can cause significant harm to a patient in the event of a medication error. (basicmedicalkey.com)
  • This means that it stimulates the beta2-adrenergic receptors in your throat. (fastshop.co.il)
  • Understanding the direct and indirect effects of beta-receptor blockade is crucial to rapid identification and appropriate treatment of beta-blocker toxicity. (medscape.com)
  • Blockade of beta-receptors results in decreased production of intracellular cyclic adenosine monophosphate (cAMP) with a resultant blunting of multiple metabolic and cardiovascular effects of circulating catecholamines. (medscape.com)
  • Beta1-receptor blockade reduces heart rate, blood pressure, myocardial contractility, and myocardial oxygen consumption. (medscape.com)
  • Beta2-receptor blockade inhibits relaxation of smooth muscle in blood vessels, bronchi, the gastrointestinal system, and the genitourinary tract. (medscape.com)
  • Other than the direct effects of the beta-adrenoreceptor blockade, toxicity may result from other mechanisms, including sodium and calcium channel blockade, centrally mediated cardiac depression, and alteration of cardiac myocyte energy metabolism. (medscape.com)
  • Reversible blockade suggests that the inhibitor dissociates from the receptor relatively easily. (pharmacology2000.com)
  • By analyzing specific amino acid mutations of the α 2A - receptor with respect to changes in PB binding, certain sites were identified that may serve as the molecular target for phenoxybenzamine-mediated receptor blockade. (pharmacology2000.com)
  • Antiarrhythmic effects are due mainly to beta-adrenergic receptor blockade. (pharmacology2000.com)
  • β-adrenergic receptor blockade can also help reduce ventricular following rates in atrial flutter and fibrillation, again by acting at the AV node. (pharmacology2000.com)
  • I.V. administration is used for rapid beta-receptor blockade in treatment of atrial fibrillation with high ventricular following rates. (pharmacology2000.com)
  • Acceptable beta-adrenergic antagonists for use in patients with asthma should ideally minimize antagonism of bronchial (beta2) receptors while providing useful cardiac (beta2) blockade. (onlineasthmainhalers.com)
  • We found that pindolol, given in a fixed dose of 0.4 mg intravenously, produced betai-adrenergic blockade as measured by reduction in exercise heart rate, although resting heart rates were not significantly different. (onlineasthmainhalers.com)
  • Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles. (druglib.com)
  • Anticholinergics prevent the increases in intracellular concentration of cyclic guanosine monophosphate (cyclic GMP) which are caused by interaction of acetylcholine with the muscarinic receptor on bronchial smooth muscle. (theodora.com)
  • While it is recognized that beta 2 -adrenergic receptors are the predominant receptors on bronchial smooth muscle, recent data indicate that there is a population of beta 2 -receptors in the human heart which comprise between 10% and 50% of cardiac beta-adrenergic receptors. (theodora.com)
  • In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta 2 -adrenergic receptors compared with isoproterenol. (theodora.com)
  • Isoproterenol (Isuprel, Isoprenaline) is a classical nonselective β-adrenergic agonist, with prominent actions at β 1 and β 2 receptors. (pharmacology2000.com)
  • Mechanism of ActionIn vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has preferential effect on beta 2-adrenergic receptors compared with isoproterenol. (drugcentral.org)
  • It is specifically a selective antagonist of the β1-adrenergic receptor and has no intrinsic sympathomimetic activity. (wikipedia.org)
  • Rezatomidine is a selective antagonist of α2-adrenergic receptor and can be used in studies about chronic pain, including neuropathic pain. (targetmol.com)
  • Metoprolol is a beta blocker, or an antagonist of the β-adrenergic receptors. (wikipedia.org)
  • Metoprolol blocks β1-adrenergic receptors in heart muscle cells, thereby decreasing the slope of phase 4 in the nodal action potential (reducing Na+ uptake) and prolonging repolarization of phase 3 (slowing down K+ release). (wikipedia.org)
  • non-primary source needed] Metoprolol is classified as a moderately lipophilic beta blocker. (wikipedia.org)
  • Like metoprolol, atenolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. (druglib.com)
  • Beta-blocker therapy has mortality benefit in patients with hypertension, heart failure and coronary artery disease, as well as during the perioperative period. (nih.gov)
  • 1 It is estimated that the number of persons aged 65 years and older will increase to 72 million by the year 2030, which will in turn result in an increased rate of hypertension among the elderly. (uspharmacist.com)
  • According to the Seventh Report of the Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC 7), the SBP should be the primary target for diagnosis and treatment of hypertension in the elderly ( TABLE 1 ). (uspharmacist.com)
  • As with other beta 1-blocker mechanism of action in hypertension is unclear. (pharmru.com)
  • When hypertension effect develops after 2-5 days, stable operation is noted after 1-2 months. (pharmru.com)
  • With the advent of antihypertensive agents, the incidence of hypertensive emergencies in the United States has declined from 7% to approximately 1% of patients with hypertension. (medscape.com)
  • In older children, congestive heart failure may be caused by left-sided obstructive disease (valvar or subvalvar aortic stenosis or coarctation), myocardial dysfunction (myocarditis or cardiomyopathy), hypertension, renal failure,[1] or, more rarely, arrhythmias or myocardial ischemia. (medscape.com)
  • It is a selective β1 receptor blocker medication. (wikipedia.org)
  • If the two drugs are coadministered, the beta blocker should be withdrawn several days before the gradual withdrawal of clonidine. (druglib.com)
  • Beta-blocker toxicity in children usually results from exposure to an adult's unattended medications. (medscape.com)
  • Beta-blocker toxicity in adults usually results from a suicide attempt or an accidental overdose of a routine medication. (medscape.com)
  • An example of an 'irreversible' non-selective α-receptor blocker is phenoxybenzamine (Dibenzyline). (pharmacology2000.com)
  • Single dose cardioselective beta-blocker produced a 7.46% (95% CI 5.59, 9.32) reduction in FEV1, but with a 4.63% (95% CI 2.47, 6.78) increase in FEV1 with beta2-agonist, compared to placebo. (nih.gov)
  • Bisoprolol - selective beta 1-blocker, without its own sympathomimetic activity, has no membrane stabilizing action. (pharmru.com)
  • Adverse effects of beta blocker therapy can lead to fatigue, bronchospasm, depression, impotence, and attenuation of hypoglycemic symptoms in diabetic patients and worsening of congestive heart failure. (pharmacology2000.com)
  • A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS. (drugcentral.org)
  • Pindolol (LB-46), a potent beta-adrenergic blocker, does not have selective betai antagonism and is said to have intrinsic sympathomimetic activity. (onlineasthmainhalers.com)
  • Bucindolol Formatel is a blocker of β1-adrenergic receptor. (targetmol.com)
  • Clonidine uniquely stimulates α 2 receptors, yet affects the heart rate which is normally affected by beta receptors. (proprofs.com)
  • What this means, is that it stimulates your beta-2 receptors. (fastshop.co.il)
  • Dobutamine is an example of a drug that selectively stimulates the heart via β 1 receptors, although dobutamine also has activity at α adrenergic receptors as well. (pharmacology2000.com)
  • It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. (lookformedical.com)
  • Although their agonist property is weaker than that of catecholamines, they are capable of stimulating beta-receptors, especially when catecholamine levels are low. (medscape.com)
  • Blocking in low doses of beta 1-adrenergic receptors of the heart, stimulated by catecholamines reduces the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), the current lowers intracellular calcium ions, inhibits all heart functions reduces atrioventricular (AV) conduction and excitability. (pharmru.com)
  • Catecholamine-depleting drugs (eg, reserpine) may have an additive effect when given with beta-blocking agents. (druglib.com)
  • Which drugs select α 1 receptors and indicate whether agonistically or antagonistically. (proprofs.com)
  • These drugs bind to α1 receptors and activate them, leading to vasoconstriction and increased blood pressure. (proprofs.com)
  • Ephedrine and Pseudo-Ephedrine are referred to as mixed acting drugs because they exhibit both antagonistic and stimulatory effects on their receptor simultaneously. (proprofs.com)
  • This dual action of the drugs on the receptor is what classifies them as mixed acting drugs. (proprofs.com)
  • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. (nih.gov)
  • Use with caution in patients sensitive to sympathomimetic drugs and patients with cardiovascular or convulsive disorders. (nih.gov)
  • Phenylephrine and methoxamine are examples of drugs that selectively activate α 1 -adrenergic receptors (adrenomimetic). (pharmacology2000.com)
  • Whereas the above two example drugs show α-adrenergic receptor selectivity (α 1 vs. α 2 ), oxymetazoline activates both α 1 and α 2 adrenergic receptors. (pharmacology2000.com)
  • It should not be used in patients anesthetized with agents such as cyclopropane or halothane as these may sensitize the heart to the arrhythmic action of sympathomimetic drugs. (drugs-library.com)
  • Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. (lookformedical.com)
  • Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lookformedical.com)
  • Drugs that selectively bind to and activate beta-adrenergic receptors. (lookformedical.com)
  • Details of antihypertensive drug therapy and compliance, intake of over-the-counter (OTC) preparations such as sympathomimetic agents, and use of illicit drugs such as cocaine are important elements of the medication history. (medscape.com)
  • Of candidate drugs for PONV, CPZ is the only drug that has activity at the first four of these receptors. (ispub.com)
  • Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes. (guidelinecentral.com)
  • When given by rapid intravenous injection, it produces a rapid rise in blood pressure, mainly systolic, by (1) direct stimulation of cardiac muscle which increases the strength of ventricular contraction, (2) increasing the heart rate and (3) constriction of the arterioles in the skin, mucosa and splanchnic areas of the circulation. (drugs-library.com)
  • The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. (lookformedical.com)
  • Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta 2 -agonist and methylxanthines were administered concurrently. (guidelinecentral.com)
  • Angiotensin II receptor 1(AT1) antagonists are beneficial in focal ischemia/reperfusion (I/R). However, in cases of global I/R, such as cardiac arrest (CA), AT1 blocker's potential benefits are still unknown. (bvsalud.org)
  • By preventing reuptake of 5-HT presynaptically, SSRIs result in more 5-HT to stimulate postsynaptic 5-HT receptors. (msdmanuals.com)
  • The mechanism of action is to enhance the inhibitory effect of endogenous GABA in the CNS by increasing the sensitivity of the GABA-receptor mediator as a result of stimulation of benzodiazepine receptors located in the allosteric center of postsynaptic GABA-receptor activating. (medicatione.com)
  • In addition, beta-adrenergic receptor antagonism inhibits both glycogenolysis and gluconeogenesis, which may result in hypoglycemia. (medscape.com)
  • By binding to α2 receptors in the CNS, clonidine can modulate the release of norepinephrine, resulting in a decrease in sympathetic outflow and ultimately leading to a decrease in heart rate. (proprofs.com)
  • The alpha 2 receptors are located in the postganglionic sympathetic nerve endings. (basicmedicalkey.com)
  • Activation of this receptor type centrally reduces sympathetic outflow, which is the proposed mechanism that accounts for antihypertensive actions noted following clonidine administration. (pharmacology2000.com)
  • To a variable degree it acts on both alpha and beta receptor sites of sympathetic effector cells. (drugs-library.com)
  • Only dopamine can activate these receptors. (basicmedicalkey.com)
  • Five neurotransmitter receptors are of primary importance in PONV: acetylcholine, dopamine-2, histamine-1, serotonin-3, and neurokinin-1. (ispub.com)
  • Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. (targetmol.com)
  • Rotigotine Hydrochloride, a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. (targetmol.com)
  • What does activation of Dopamine D1 receptors do? (brainscape.com)
  • Anti-sialogue (anticholinergic) - reduces salivary and GIT secretions (pre-operative prep) due to widespread location of autonomic receptors side effects are common which both the clinician and patient should be aware of. (emedsa.org.au)
  • The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS. (lookformedical.com)
  • Clen) Clenbuterol (Clen) is a selective beta-2 agonist/antagonist and a bronchodilator. (fastshop.co.il)
  • Albuterol sulfate, chemically known as (1,3-benzenedimethanol, (alpha)'-[[(1,1-dimethylethyl) amino] methyl]-4-hydroxy, sulfate (2:1)(salt), (±)- is a relatively selective beta 2 -adrenergic bronchodilator. (theodora.com)
  • Combivent Inhalation Aerosol is a combination of the anticholinergic bronchodilator, ipratropium bromide, and the beta 2 -adrenergic bronchodilator, albuterol sulfate. (theodora.com)
  • Because it crosses the blood-brain barrier so that the the alpha receptors it binds are ones in the CNS instead of on the effector organ. (proprofs.com)
  • This means that the alpha receptors it binds to are located in the central nervous system (CNS) rather than on the effector organ, which in this case is the heart. (proprofs.com)
  • Desogestrel binds intracellular progesterone receptors in progesterone responsive tissue and the resultant complex interacts with DNA and results in either gene transcription or gene repression. (medindex.am)
  • Pimecrolimus binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. (medindex.am)
  • Clonidine is able to affect the heart rate by stimulating α2 receptors instead of β receptors because it has the ability to cross the blood-brain barrier. (proprofs.com)
  • Clonidine activates another type of adrenergic receptor, designated α 2 . (pharmacology2000.com)
  • Centrally-acting sympatholytic agent/agents (alpha2 adrenergic receptor agonists). (pharmacology2000.com)
  • phenylephrine decreases effects of iobenguane I 123 by receptor binding competition. (medscape.com)
  • Total peripheral vascular resistance at the beginning of the drug in the first 24 hours, is increased (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta-2 adrenergic receptor), after 1-3 days returned to the initial value, and long-term use - is reduced. (pharmru.com)
  • however, little is known concerning whether beta-adrenoceptor-mediated hyperpolarization is altered with aging. (lookformedical.com)
  • In contrast, preferential beta(1)-adrenoceptor antagonists (atenolol and CGP-20712A) did not affect either nicotine- or TNS-induced relaxation. (lookformedical.com)
  • Results of double-labeling studies indicated that beta(2)-adrenoceptor immunoreactivities and NADPH diaphorase reactivities were colocalized in the same nerve fibers in basilar and middle cerebral arteries. (lookformedical.com)
  • Olodaterol is a novel, long-acting β2-adrenergic agonist (EC50s: 97.7 nM for the human β2-adrenoceptor) that exerts its pharmacological effect by binding and act. (targetmol.com)
  • Piperoxan hydrochloride is an α2 adrenoceptor antagonist. (targetmol.com)
  • ST-91 is an agonist of α2-adrenoceptor with a mixed α-adrenergic receptor type/subtype selection profile. (targetmol.com)
  • Plasma levels are usually less than 200 μg/L during therapeutic administration, but can range from 1-20 mg/L in overdose victims. (wikipedia.org)
  • Transmitters are inactivated by (1) reuptake of the transmitter back into the neuron (nerve cell terminal), (2) enzymatic transformation or degradation, and (3) diffusion away from the receptor. (basicmedicalkey.com)
  • Atenolol, a competitive beta(1)-selective adrenergic antagonist, has the lowest lipid solubility of this drug class. (druglib.com)
  • Pressure: Atenolol works by blocking the transmission of messages to the beta receptors in the heart which slows down the activity of the heart, decreasing blood pressure. (pharmacycode.com)
  • Angina: Atenolol works by blocking the transmission of messages to the beta receptors in the heart which slows down the activity of the heart and reduces the heart's need for oxygen. (pharmacycode.com)
  • Activation of beta 2 -adrenergic receptors on airway smooth muscle leads to the activation of adenylyl cyclase and to an increase in the intracellular concentration of cyclic-3',5'-adenosine monophosphate (cyclic AMP). (theodora.com)
  • Albuterol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges. (guidelinecentral.com)
  • In an 18-month study in CD-1 mice, albuterol sulfate showed no evidence of tumorigenicity at dietary doses of up to 500 mg/kg (approximately 1700 times the maximum recommended daily inhalation dose for adults on mg/m basis and approximately 800 times the maximum recommended daily inhalation dose for children on mg/m basis). (drugcentral.org)
  • Phenoxybenzamine (PB) has been used to probe α-adrenergic receptor subtypes. (pharmacology2000.com)
  • This means that while they bind to the receptor in an antagonistic manner, they also stimulate the receptor at the same time. (proprofs.com)
  • They stimulate 5-HT 1 receptors, with antidepressant and anxiolytic effects, but they also stimulate 5-HT 2 receptors, commonly causing anxiety, insomnia, and sexual dysfunction, and 5-HT 3 receptors, commonly causing nausea and headache. (msdmanuals.com)
  • This means that they block or inhibit the activity of the α1 receptors. (proprofs.com)
  • Clenbuterol is a substituted phenylaminoethanol and a long-acting beta-2 adrenergic agonist with sympathomimetic activity. (fastshop.co.il)
  • In some instances peripheral resistance is not altered or may even rise owing to a greater ratio of alpha to beta activity in different vascular areas. (drugs-library.com)
  • A synthetic progestogen with progesterone hormone receptor agonistic activity. (medindex.am)
  • They act on one or more adrenergic receptor sites located in the effector cells of muscles such as the heart, bronchiole walls, gastrointestinal (GI) tract, urinary bladder, and ciliary muscles of the eye. (basicmedicalkey.com)
  • Since all reactions are, by definition, reversible, those reactions in which the inhibitor and receptor complex is so stable that dissociation is unlikely are described as 'irreversible. (pharmacology2000.com)
  • Oxymetazoline is an example of a non-selective α-adrenergic receptor agonist. (pharmacology2000.com)