• Topical beta-blockers that reduce elevated and normal IOP, with or without glaucoma. (medscape.com)
  • They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers"), inhibiting the downstream cellular signaling pathways of adrenergic receptors. (wikipedia.org)
  • There is clear evidence from many controlled trials in the past 25 years that beta blockers are effective in anxiety disorders, though the mechanism of action is not known. (wikipedia.org)
  • Some people have used beta blockers for performance type social anxiety, or "stage fright. (wikipedia.org)
  • In particular, musicians, public speakers, actors, and professional dancers, have been known to use beta blockers to avoid stage fright and tremor during public performance and especially auditions. (wikipedia.org)
  • Stutterers also use beta blockers to avoid fight/flight responses, hence reducing the tendency to stutter. (wikipedia.org)
  • Since they promote a lower heart rate and reduce tremor, beta blockers have been used by some Olympic marksmen to enhance performance, though beta blockers are banned by the International Olympic Committee (IOC). (wikipedia.org)
  • By administering beta blockers which can cross the blood brain barrier immediately following a traumatic event, as well as over the next couple weeks, the formation of PTSD has been reduced in clinical studies. (wikipedia.org)
  • Researchers tested the capacity of adrenergic antagonists, drugs such as alpha and beta blockers, to disrupt the receptor's sensing ability. (sciencedaily.com)
  • Just before finishing my course of Lymecycline, doc and I discussed using beta-blockers, as they can be very effective on redness (spoiler: my biggest problem re. (bybi.com)
  • Beta-blockers aren't created as a treatment for rosacea, but a result of using them is that they can minimise redness because it slows down your heart rate and relaxing your blood vessels. (bybi.com)
  • Instead of beta-blockers, we went with an alpha-blocker (alpha 2 adrenergic receptor antagonist). (bybi.com)
  • Four drug classes were evaluated in the trials: thiazides (21 trials), beta-adrenergic blockers (5), calcium-channel blockers (4) and angiotensin-converting-enzyme (ACE) inhibitors (1). (cmaj.ca)
  • In 5 drug-drug trials comparing thiazides with beta-blockers, the former were associated with a significantly lower rate of withdrawal due to adverse effects (relative risk [RR] 0.69, 95% confidence interval [CI] 0.63-0.76). (cmaj.ca)
  • The same cannot be said for high-dose thiazide therapy, beta-blockers, calcium-channel blockers or ACE inhibitors. (cmaj.ca)
  • 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)
  • 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)
  • Alpha blockers , which counter a different set of noradrenaline effects, are used to treat several cardiovascular and psychiatric conditions. (wikipedia.org)
  • Nonselective beta-blockers (eg, timolol maleate, levobunolol) are controversial because as visual-field progression is possibly due to secondary aggravated nocturnal arterial hypotension. (medscape.com)
  • In General, antihypertensive drugs (diuretics, beta-blockers, ACE inhibitors, antagonists of angiotensin II receptors blockers, vasodilators and Central acting), adrenergic blockers, calcium antagonists and blockers of alpha-adrenergic receptors did not reveal differences in the profile of side effects in patients receiving pay for Forzest with bitcoin compared to placebo. (edbitcoin.com)
  • Alpha-1 blockers constitute a variety of drugs which block α1-adrenergic receptors in arteries and smooth muscles. (absoluteastronomy.com)
  • Beta blockers or beta-adrenergic blocking agents, beta-adrenergic antagonists, beta-adrenoreceptor antagonists or beta antagonists, are a class of drugs used for various indications. (absoluteastronomy.com)
  • In the United Kingdom, the June 2006 "Hypertension: management of hypertension in adults in primary care" [6] guideline of the National Institute for Health and Clinical Excellence , downgraded the role of beta-blockers due to their risk of provoking type 2 diabetes . (wikidoc.org)
  • Although beta blockers lower blood pressure, they do not have as positive a benefit on endpoints as some other antihypertensives. (wikidoc.org)
  • [9] However, beta blockers have an important role in the prevention of heart attack in people who have already had a heart attack. (wikidoc.org)
  • Despite lowering blood pressure, alpha blockers have significantly poorer endpoint outcomes than other antihypertensives, and are no longer recommended as a first-line choice in the treatment of hypertension. (wikidoc.org)
  • Beta-blockers: May decrease effectiveness of PROAIR RESPICLICK and produce severe bronchospasm. (nih.gov)
  • Patients with asthma should not normally be treated with beta-blockers. (nih.gov)
  • Beta-blockers and alpha-adrenergic agonists impair thermoregulatory processes and should be modified (1). (shmabstracts.org)
  • AlphaAdrenergic Blockers - Alpha-Adrenergic Blockers. (powershow.com)
  • Careful preoperative treatment with alpha and beta blockers is required to control blood pressure and prevent intraoperative hypertensive crises. (medscape.com)
  • In rats treated with atropine plus hexamethonium, intravenous phentolamine (non-selective alpha-adrenergic receptor antagonist) plus propranolol (non-selective beta-adrenergic receptor antagonist) completely blocked the BIMP-induced increases in blood pressure and heart rate. (inra.fr)
  • The alpha and beta adrenoreceptor inhibitors, phentolamine and propranolol, inhibited the initial spike and the sustained phase, respectively, suggesting a contribution of adrenergic receptors. (nih.gov)
  • 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)
  • We studied right vagally innervated Langendorff-perfused guinea pig hearts, beta-blocked with propranolol, 5 × 10−7 M. Heart rate and QT interval were measured from bipolar epicardial electrodes. (aspetjournals.org)
  • These include the alpha-2 adrenergic agonists clonidine and guanfacine, the nonselective beta-adrenergic agent propranolol, and most promising prazosin, which is an alpha-1 adrenergic receptor antagonist that blocks the actions of NE on alpha-1 receptors(Petrakis, 2016). (duepapers.net)
  • [ 8 ] There is also evidence that intranasal cationic adrenergic decongestant drugs may be trapped into cellular endomembrane compartments caused by V-ATPase-dependent sequestration that results in a tissue reservoir of these drugs, influencing the toxicity and pharmacology of these agents. (medscape.com)
  • Prostaglandin F2-alpha analog and selective FP prostanoid receptor agonist. (medscape.com)
  • ICI-118,551 Highly selective β2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to its strong receptor specificity. (wikipedia.org)
  • In rats pretreated with the non-selective muscarinic-receptor antagonist atropine, BIMP significantly increased both heart rate and blood pressure. (inra.fr)
  • Clenbuterol is a beta-agonist, while Albuterol is a selective beta-agonist. (profhim.kz)
  • Furthermore, it's partially adrenolytic, as it is less selective than yohimbine on the adrenergic system, partially antagonizing alpha-1- adrenoreceptors. (anabolicminds.com)
  • Selective alpha2-receptor that reduces aqueous humor formation and may increase uveoscleral outflow or inhibit inflow. (medscape.com)
  • Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral outflow. (medscape.com)
  • These include agonists capable of selectively activating β1-, β2- or β3-adrenoceptors, as well as antagonists selective for each of the three subtypes. (sigmaaldrich.com)
  • β-Adrenoceptor antagonists, either non subtype-selective or selective for the β1-adrenoceptor, are widely used as antihypertensives, although the mechanism for this action is still not clearly understood. (sigmaaldrich.com)
  • A beta-2 selective adrenergic antagonist. (lookformedical.com)
  • The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. (citizendium.org)
  • One of two major pharmacologically defined classes of adrenergic receptors. (lookformedical.com)
  • 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)
  • The contractile mechanism of skeletal muscles entails the binding of acetylcholine to nicotinic receptors on the membranes of muscle fibres. (britannica.com)
  • In atropine-treated rats, hexamethonium (antagonist of ganglionic nicotinic receptors) greatly attenuated the BIMP-induced increase in blood pressure without changing the BIMP-induced increase in heart rate. (inra.fr)
  • The effectiveness of angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II receptor blocker AT-1 (ARBs) in reducing the systemic hypertension (SH) is widely known. (intechopen.com)
  • Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart. (aspetjournals.org)
  • 1,4,5-IP3 (significant at 10 microM) and both IP4 isomers (significant at 1 microM) increased after alpha-adrenoceptor stimulation, whereas 1,3,4,5,6-IP5 and IP6 remained unaffected. (aspetjournals.org)
  • Increased inositol polyphosphate turnover may be involved in the mechanism(s) whereby alpha 1-adrenoceptor stimulation produces an increase in myocardial force of contraction. (aspetjournals.org)
  • It has been widely established that dopamine and its agonists play an important role in cardiovascular, renal, hormonal, and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. (biopsychiatry.com)
  • Stimulation of the beta 1 receptors increases myocardial contractility and heart rate. (basicmedicalkey.com)
  • Most β-adrenoceptor mediated actions involve stimulation of adenylyl cyclase via interaction of the agonist-receptor complex with G s . (sigmaaldrich.com)
  • While it was initially thought that cardiac stimulation involved primarily the β1-adrenoceptor, it now appears that all of the receptor subtypes may be involved. (sigmaaldrich.com)
  • 284 AB - Alpha-1 adrenergic stimulation modulates ventricular automaticity via an alpha-1 adrenoceptor (AR) subtype blocked by the alpha-1B antagonist chloroethylclonidine (CEC) and alters repolarization via receptor subtype(s) (alpha-1A and alpha-1D) blocked by WB4101. (aspetjournals.org)
  • The actions of epinephrine resemble the effects of stimulation of adrenergic nerves. (drugs-library.com)
  • Nonselective beta-adrenergic receptor blocking with intrinsic sympathomimetic activity. (medscape.com)
  • Other short-acting sympathomimetic aerosol bronchodilators and adrenergic drugs: May potentiate effect. (nih.gov)
  • Epinephrine, USP is a sympathomimetic (adrenergic) agent designated chemically as 4-[1-hydroxy-2 (methylamino) ethyl]-1,2 benzenediol, a white, microcrystalline powder. (drugs-library.com)
  • Nonselective beta-adrenergic receptor blocking agent. (medscape.com)
  • Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous humor production and possibly increasing outflow of aqueous humor. (medscape.com)
  • Intra-ocular administration of nonselective β-adrenoceptor antagonists is a common treatment for glaucoma. (sigmaaldrich.com)
  • Cardioselective beta1-adrenergic receptor blocking agent with minimal effect on pulmonary and cardiovascular parameters. (medscape.com)
  • Selectively blocks beta1-adrenergic receptors with little or no effect on beta2-receptors. (medscape.com)
  • Clonidine uniquely stimulates α 2 receptors, yet affects the heart rate which is normally affected by beta receptors. (proprofs.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)
  • Brimonidine tartrate is an alpha-adrenergic receptor agonist that reduces IOP. (medscape.com)
  • Brimonidine works by improving the redness of rosacea by stimulating the alpha-receptors on the skin, causing the blood vessels to contract and narrow which reduces the blood flow. (bybi.com)
  • Used as adjunct to miotic or beta-blocker therapy. (medscape.com)
  • In a study made available online this week and in an upcoming issue of the Proceedings of the National Academy of Sciences, researchers describe how they used phentolamine, an alpha blocker drug used to treat hypertension, to successfully impede signaling to the receptor. (sciencedaily.com)
  • High-dose thiazide therapy, beta-blocker therapy and calcium-channel blocker therapy did not significantly reduce the risk of death or coronary artery disease. (cmaj.ca)
  • Several randomized controlled trials have found that the alpha-1 blocker prazosin is effective in reducing symptoms of posttraumatic stress disorder (PTSD) among active-duty soldiers(Roundup, 2017). (duepapers.net)
  • 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)
  • Accordingly, the compensatory reflex mechanisms that come into play with a pronounced increase in blood pressure do not antagonize the direct cardiac actions of epinephrine as much as with catecholamines that have a predominant action on alpha receptors. (drugs-library.com)
  • 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)
  • 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)
  • To a variable degree it acts on both alpha and beta receptor sites of sympathetic effector cells. (drugs-library.com)
  • Neurotransmitters diffuse across the synaptic cleft and bind briefly to specific receptors on the adjoining neuron or effector cell. (msdmanuals.com)
  • The alpha 1-agonist methoxamine and the alpha 1-antagonist prazosin were injected into the DPT of freely moving, unanaesthetized cats. (nih.gov)
  • All effects were antagonized by the alpha 1-adrenoceptor antagonist prazosin (0.1 microM), indicating receptor-mediated effects. (aspetjournals.org)
  • They found that phentolamine binds to the QseC receptor and occupies the pocket that the receptor would use to recognize the host epinephrine and norepinephrine signals - thus blocking the QseC receptor from sensing the signals and preventing it from being able to express its virulence genes in cells. (sciencedaily.com)
  • Our objective was to determine alpha-1 AR subtype specific effects and vagal interactions on heart rate and ventricular repolarization. (aspetjournals.org)
  • A receptor subtype blocked by WB4101 (alpha-1A or alpha-1D) is responsible for the QT and QTc shortening. (aspetjournals.org)
  • In previous studies we investigated the role of beta- and alpha 2-adrenergic receptors through local microinjections of various drugs into the dorsal pontine tegmentum (DPT) of the cat. (nih.gov)
  • Some drugs for the treatment of asthma block the binding of leukotrienes to their receptor. (britannica.com)
  • Because this mechanism is relatively insensitive to drug action, the most important group of drugs that affect the neuromuscular junction act on (1) acetylcholine release, (2) acetylcholine receptors, or (3) the enzyme acetylcholinesterase (which normally inactivates acetylcholine to terminate muscle fibre contraction). (britannica.com)
  • Neuromuscular blocking drugs act on acetylcholine receptors and fall into two distinct groups: nondepolarizing (competitive) and depolarizing blocking agents. (britannica.com)
  • Competitive neuromuscular blocking drugs act as antagonists at acetylcholine receptors, reducing the effectiveness of acetylcholine in generating an end-plate potential . (britannica.com)
  • Which drugs select α 1 receptors and indicate whether agonistically or antagonistically. (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)
  • For reasons that are still unclear, some Alpha-2 drugs, such as guanfacine , have also been shown to be effective in the treatment of anxiety disorders and ADHD . (wikipedia.org)
  • Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. (citizendium.org)
  • 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)
  • phenylephrine decreases effects of iobenguane I 123 by receptor binding competition. (medscape.com)
  • Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in heart rate, sympathetic tone, and activity of the renin aldosterone system. (biopsychiatry.com)
  • If you combine any of these alpha 2 antagonists with caffeine or beta-agonists (aka synergists), the necessary dose decreases quite a bit. (anabolicminds.com)
  • Total peripheral resistance decreases by action of epinephrine on beta receptors of the skeletal muscle vasculature and blood flow is thereby enhanced. (drugs-library.com)
  • The beta 1 receptors are located primarily in the heart but are also found in the kidney. (basicmedicalkey.com)
  • It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS. (lookformedical.com)
  • Another way to inhibit adrenergic receptor signaling is by blocking the synthesis of catecholamines. (wikipedia.org)
  • This means that they block or inhibit the activity of the α1 receptors. (proprofs.com)
  • The signal may stimulate or inhibit the receiving cell, depending on the neurotransmitter and receptor involved. (msdmanuals.com)
  • Alpha-2 antagonists synergize with anything that potentiates catecholamine release. (anabolicminds.com)
  • Coop's Corner #4: Alpha-2 Antagonism? (anabolicminds.com)
  • Furthermore, because alpha-2 antagonism can increase insulin release, these compounds are best taken fasted. (anabolicminds.com)
  • 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)
  • 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)
  • When the receptor binds to signaling molecules, the bacterium can infect cells. (sciencedaily.com)
  • This is a first-generation antihistamine with anticholinergic effects that binds to H1 receptors in the CNS and the body. (medscape.com)
  • since this receptor is located presynaptically, agonism at this receptor inhibits the presynaptic release of adrenaline and noradrenaline, preventing postsynaptic adrenergic receptor activation and downstream signaling. (wikipedia.org)
  • Noradrenaline is involved in the regulation of the sleep/waking cycle by acting through various receptor types. (nih.gov)
  • The -Adrenergic Receptors and the Control of Adipose Tissue Metabolism and Thermogenesis. (sigmaaldrich.com)
  • In conclusion, in the setting of betaadrenergic blockade, an alpha-1B receptor appears responsible for the alpha-1 adrenergic decrease in heart rate and facilitation of vagal responsiveness. (aspetjournals.org)
  • The alpha-2 receptor is an autoreceptor, meaning it is located NOT on the postsynaptic neuron chiefly, but on the pre-synaptic neuron. (anabolicminds.com)
  • In such cases, the dendrites (a neuron's receiving branches) on the postsynaptic neurons release neurotransmitters that affect receptors on the presynaptic neurons. (msdmanuals.com)
  • Neurotransmitters that are released bind to receptors on another neuron. (msdmanuals.com)
  • From a therapeutic point of view, the above-mentioned agonists are used for treating Parkinson's disease, acting over DA 2 dopaminergic receptors of the nigrostriatal system. (biopsychiatry.com)
  • Bromocriptine and the other dopaminergic agonists mentioned act over DA 2 receptors of the tuberoinfundibular system, inhibiting prolactin release and decreasing hyperprolactinemia and tumor size. (biopsychiatry.com)
  • Other adrenergic receptors are dopaminergic and are located in the renal, mesenteric, coronary, and cerebral arteries. (basicmedicalkey.com)
  • 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)
  • More adrenaline production can lead to what we wrongfully refer to as "CNS fatigue" either by depleting dopamine (adrenaline is made from dopamine) or a desensitization of the adrenergic receptors due to overstimulation. (t-nation.com)
  • Only dopamine can activate these receptors. (basicmedicalkey.com)
  • Presynaptic beta(2)-adrenoceptors mediate nicotine-induced NOergic neurogenic dilation in porcine basilar arteries. (lookformedical.com)
  • Beta-adrenoceptor signaling pathways mediate cardiac pathological remodeling. (sigmaaldrich.com)
  • Inhibition of binding of [3H]batrachotoxinin A 20-alpha-benzoate to sodium channels by local anesthetics. (aspetjournals.org)
  • Characterization of a functional thrombin receptor. (jci.org)
  • The IUPHAR compendium of receptor characterization and classification. (sigmaaldrich.com)
  • Purification and characterization of a bungarotoxin polypeptide which blocks nicotinic receptor function in primary culture of adrenal chromaffin cells. (aspetjournals.org)
  • Three β-adrenoceptor proteins have been cloned, and the characteristics of these recombinant receptors correspond with those of the three well characterized β-adrenoceptors on native tissues, designated as β1, β2 and β3. (sigmaaldrich.com)
  • However, in contrast to the prejunctional α 2 -adrenoceptors, these prejunctional receptors do not appear to have major physiologic significance. (sigmaaldrich.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)
  • What this means is that Clen will stimulate both the beta- and alpha-adrenergic receptors. (profhim.kz)
  • This means that while they bind to the receptor in an antagonistic manner, they also stimulate the receptor at the same time. (proprofs.com)
  • Yohimbine possess extreme affinity for the alpha-2-adrenoreceptor, but due to receptor homology with various 5-HT receptors, yohimbine HCl is highly anxiogenic and is clinically used to model panic disorder. (anabolicminds.com)
  • The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
  • Time-dependent changes in the affinity of the receptor for agonists. (aspetjournals.org)
  • The beta 2 receptors are found mostly in the smooth muscles of the lung and GI tract, the liver, and the uterine muscle. (basicmedicalkey.com)