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Alpha Adrenergic Antagonist

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161. Post-retrieval disruption of a cocaine conditioned place preference by systemic and intrabasolateral amygdala β2- and α1-adrenergic antagonists (PubMed)

the effects of beta(1) and beta(2), as well as alpha(1)-adrenergic receptor antagonism following retrieval of a cocaine conditioned place preference (CPP). We found that rats administered the beta(2) antagonist ICI 118,551 (8 mg/kg intraperitoneal [IP]) or the alpha(1) antagonist prazosin (1 mg/kg IP) following a drug-free test for CPP showed attenuated preference during a subsequent test, while the beta(1) antagonist betaxolol (5 or 10 mg/kg IP) and a lower dose of prazosin (0.3 mg/kg IP) had no effect (...) Post-retrieval disruption of a cocaine conditioned place preference by systemic and intrabasolateral amygdala β2- and α1-adrenergic antagonists Previous work has demonstrated post-retrieval impairment in associative learning paradigms, including those mediated by drugs of abuse, using nonspecific beta-adrenergic receptor (beta-AR) antagonists. Remarkably little is known about the role of the specific beta-AR subtypes, or other adrenergic receptors, in these effects. The current study examined

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2009 Learning & Memory

163. Treatment of Hypertension in Association With Left Ventricular Hypertrophy

with a decrease in left ventricular mass index of 13.3% (95%CI, 9.9%–16.8%), calcium channel blockers (CCBs) 9.3% (95%CI, 5.5%–13.1%), diuretics 6.8% (95%CI, 3.0%–10.7%) and beta-adrenergic antagonists (β-blockers) 5.5% (95%CI, 2.3%–8.6%) . However, this meta-analysis was small (1200 patients received active treatment; 189 received placebo), and mean duration of therapy was only 25 weeks. Subsequent studies have shown similar degrees of LVH regression with other agents, including alpha-blockers (ɑ-blockers (...) . Langenfeld MR, Gatzka CD, Weidinger G, Schobel HP. Impact of alpha- versus beta-blockers on hypertensive target organ damage: results of a double-blind, randomized, controlled clinical trial. Am J Hypertens 1997;10:985-91. Thurmann PA, Kenedi P, Schmidt H, Rietbrock N. Influence of the Angiotensin II antagonist valsartan on left ventricular hypertrophy in patients with essential hypertension. Circulation 1998;98:2037-42. Tedesco MA, Ratti G, Aquino D, et al. Effects of losartan on hypertension and left

2018 Hypertension Canada

164. Choice of therapy for Adults With Hypertension Without Compelling Indications for Specific Agents

supporting use of beta-adrenergic antagonists (β-blockers) in this age group consists of four trials including the placebo-controlled Medical Research Council on Mild Hypertension trial , comparing thiazides with β-blockers, which failed cumulatively to detect any significant difference in occurrence of cardiovascular endpoints (RR, 0.95; 95%CI, 0.82 to 1.11), although number of events in these trials was insufficient to prove equivalence, thus justifying a Grade B rating . Additionally, β-blockers may (...) be noted that LIFE used a control regimen with suboptimal efficacy in older patients with hypertension (i.e., β-blockers) . However, data from the ONTARGET Trial supports the equivalence of ARBs to ACE inhibitors in high-risk patients and is the basis of the caution not to combine ACE and ARB therapy given the unfavourable risk benefit profile demonstrated . Alpha-blockers Alpha-blockers were inferior to diuretics in the ALLHAT trial and this resulted in early termination of the alpha-blocker arm

2018 Hypertension Canada

165. Diagnosis & Assessment of Hypertension - Endocrine Hypertension

these conversion values with their local laboratories. Uncorrected hypokalemia (K + <3.3mmol/L), severe sodium restriction, and administration of renin-angiotensin inhibitors, diuretics and DHP-calcium channel antagonists may cause false-negative ratios and beta-blockers can cause a false positive . Other factors that can interfere with interpretation include renal dysfunction, oral contraceptives, NSAIDs, and in particular mineralocorticoid receptor antagonists. If possible, alpha blockers, hydralazine (...) adrenal adenoma, idiopathic hyperaldosteronism/bilateral adrenal hyperplasia, unilateral hyperplasia, and less commonly adrenal carcinoma and familial hyperaldosteronism (glucocorticoid remediable or non-remediable). Differentiation between unilateral and bilateral forms of aldosterone hypersecretion has important treatment implications. Unilateral forms might be amenable to improvement or even cure with adrenalectomy. In contrast, mineralocorticoid receptor antagonists are the treatment of choice

2018 Hypertension Canada

166. Lack of alpha 1b-adrenergic receptor protects against epileptic seizures. (PubMed)

Lack of alpha 1b-adrenergic receptor protects against epileptic seizures. The role of alpha 1b-adrenergic receptor (alpha 1b-AR) in relation with neuronal degeneration, drug addiction, and seizure susceptibility has recently emerged. In particular, mice that overexpress alpha 1b-AR undergo spontaneous epileptic seizures and progressive neuronal loss in a variety of brain areas. Therefore, one should expect that the blockade of alpha 1b-AR leads to anticonvulsant and neuroprotective effects (...) . However, the lack of alpha 1b-AR antagonists does not allow testing of this hypothesis.The development of alpha 1b-AR knockout (KO) mice led us to measure seizure susceptibility and neurodegeneration following systemic excitotoxins in these mice.We found that alpha 1b-AR KO mice are markedly resistant to kainate- and pilocarpine-induced seizures. Moreover, when marked seizure duration and severity are obtained by doubling the dose of chemoconvulsants in alpha 1b-AR KO, neuronal degeneration never

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2009 Epilepsia

167. Surgical Management of Lower Urinary Tract Symptoms Attributed to Benign Prostatic Hyperplasia

). Traditionally, the primary goal of treatment has been to alleviate bothersome LUTS that result from BPO. More recently, treatment has also been focused on the alteration of disease progression and prevention of complications that can be associated with BPH/LUTS, such as acute urinary retention. 16 A variety of pharmacologic classes of medications are employed to treat LUTS attributed to BPH, including alpha- adrenergic antagonists (alpha-blockers), beta adrenergic agonists, 5-alpha- reductase inhibitors (5

2018 American Urological Association

168. CRACKCast E151 – Antidepressants

: Phentolamine 2 – 3 mg increments every 10 – 15 minutes until BP close to 140 systolic Beta-adrenergic blockers are contraindicated due to the risk of unopposed alpha-agonist stimulation. Life threatening serotonin toxicity: Requires paralysis, intubation and ventilation to prevent multi organ failure Supportive Care Agitation and tachycardia: Increasing anxiety, sweating, tremor, tachycardia and mydriasis may herald the onset of seizures. Titrated doses of benzodiazepines are effective e.g. diazepam 2.5 (...) Hot as hell The bladder keeps its tone and the heart runs alone 5HT & NE reuptake inhibition (ie extra serotonin and norepinephrine) They look like sympathomimetic Tachycardia / hyperthermia, agitation, ALOC & Seizures GABA Blockade Seizures Alpha – 1 blockade Hypotension [2] What are the ECG findings associated with TCA toxicity and what are their implications As per Interventricular conduction delay — QRS > 100 ms in lead II Right axis deviation of the terminal QRS: Terminal R wave > 3 mm in aVR

2018 CandiEM

169. CRACKCast E161 – Antipsychotics

) Undesired clinical effects occurring in therapeutic use such as extrapyramidal syndromes Idiosyncratic effects such as NMS D2 receptor antagonism Reducing positive symptoms of schizophrenia EPS symptoms NMS Common “off- target” effects include: Alpha-1 adrenergic receptor antagonism Orthostatic hypotension Muscarinic acetylcholine receptor antagonism Anticholinergic toxicity Histamine H1 receptor antagonism Sedation Fast voltage-gated sodium channel blockade Wide complex dysrhythmias Delayed potassium (...) . Pupils may be of variable size Anticholinergic effects promote mydriasis, whereas miosis, resulting from alpha-antagonism, may mimic opioid toxicity. Mild orthostatic hypotension is also a common finding from alpha-adrenergic blockade Seizures EPS symptoms [3] Compare typical and atypical antipsychotic adverse effect profile Please refer to Box 155.1 in Rosen’s 9 th Edition for a comprehensive table outlining the various classifications of low/medium potency antipsychotics and atypical antipsychotics

2018 CandiEM

170. CRACKCast E195 – Procedural Sedation and Analgesia

Semisynthetic Mu Opioid Receptor Agonist Analgesic IV 0.1-0.15 mcg/kg/min infusion; supplement boluses of 1-2 mcg/kg increments Dexmedetomidine Alpha-2 Adrenergic Agonist Analgesic, sedative IV 1 mcg/kg over 10 min, then 0.2-0.7 mcg/kg/hr [9] What are our reversal agents for opioids and benzodiazepines, and how are they dosed? Opioid Reversal Agent: Naloxone Competitive antagonist of opioids Reverses opioid-related respiratory depression Rapid onset, half life of 45 minutes Clinical effects only for 15-30 (...) minutes – MAY NEED TO RE-DOSE Can be dosed IV/IM Should only dose enough to reverse opioid respiratory depression Consider initial IV doses of 0.04-0.1 mg q 1-2 minutes Complete reversal usually occurs with 1-2 mg IV Risks Few, largely rare complications Pulmonary edema, seizure, and dysrhythmias have been described Benzodiazepine Reversal Agent: Flumazenil Competitive antagonist of benzodiazepines Reverses sedation, but is NOT EFFECTIVE for reversing respiratory depression Rapid onset, peak effect

2018 CandiEM

172. Hypofractionated Radiation Therapy for Localized Prostate Cancer

ratio. Classically, the probability of cell survival following a dose of ionizing radiation is governed by the linear-quadratic model. In this model, curves of cell survival as a function of dose have an initial linear component followed by a steeper quadratic component. The relative weighting of each component, and thus the sensitivity to fractionation of the irradiated tissue, is characterized by a parameter called the alpha-beta ratio. The alpha-beta ratio of adenocarcinoma of the prostate (...) is considered low compared to most other neoplasms, with several estimates derived from large populations in the range of 100 to 200 cGy. 5-7 Unlike other solid tumors with higher alpha-beta ratios, the alpha-beta ratio of the adjacent dose-limiting normal structure, namely the rectum, has been estimated to be greater than that of prostate cancer itself. 8,9 An implication of this relationship is that hypofractionation - daily delivery of EBRT with fraction sizes >200 cGy - may further improve

2018 American Urological Association

173. Hypofractionated Radiation Therapy for Localized Prostate Cancer

survival as a function of dose have an initial linear component followed by a steeper quadratic component. The relative weighting of each component, and thus the sensitivity to fractionation of the irradiated tissue, is characterized by a parameter called the alpha-beta ratio. The alpha-beta ratio of adenocarcinoma of the prostate is considered low compared to most other neoplasms, with several estimates derived from large populations in the range of 100 to 200 cGy. - Unlike other solid tumors (...) with higher alpha-beta ratios, the alpha-beta ratio of the adjacent dose-limiting normal structure, namely the rectum, has been estimated to be greater than that of prostate cancer itself. , An implication of this relationship is that hypofractionation—daily delivery of EBRT with fraction sizes > 200 cGy—may further improve the therapeutic ratio of EBRT in localized prostate cancer. Specifically, according to the model, for courses of conventionally fractionated and hypofractionated EBRT

2018 American Society of Clinical Oncology Guidelines

174. Management of specific situations in polycythaemia vera and secondary erythrocytosis

(Landolfi et al , ). Low‐dose aspirin, which describes various doses (e.g. 75, 81 or 100 mg) used in different countries, is the only dose to have been assessed in recent clinical trials. The risk of major bleeding, particularly gastro‐intestinal, increases with age, and proton pump inhibitors should be given to patients over 75 years of age as well as to those a with high bleeding risk. The role of the ADP‐receptor antagonist, clopidogrel, in the long‐term prevention of MPN‐related thrombosis has (...) should be undertaken if it is not controlled at the time of acute thrombosis. For arterial thrombosis, low dose aspirin should be offered to all patients, and specialist advice should be sought. For venous thromboembolism (VTE), anticoagulation should be commenced. Low molecular weight heparin (LMWH) remains the first choice in the acute setting, followed by vitamin K antagonists (VKA) as per guidelines (NICE, ). Direct oral anticoagulants (DOACs) are increasingly used in the non‐MPN population

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2018 British Committee for Standards in Haematology

176. Gastroesophageal Reflux Disease (GERD) - Guidelines for Prescribing H2RAs and PPIs

, hypercalcemia Use of medications which reduce lower esophageal pressure can induce or worsen GERD – alpha-adrenergic antagonists, anticholinergics, beta-agonists, benzodiazepines (diazepam), calcium channel blockers (nifedipine, felodipine, amlodipine), nicotine, progesterone, theophylline For more information go to: CTC - Gastroesophageal Reflux - Available at . American Gastroenterological Association Medical Position Statement on the Management of Gastroesophageal Reflux Disease. Available online at GERD (...) -The-Counter Drug Options Antacids, alginates; over-the-counter dose H2 receptor antagonists (H2RAs); OTC-dose H2RAs/alginate combination mild, infrequent symptoms Esomeprazole 20 mg or omeprazole 20 mg (14 days) mild and frequent symptoms (if daily treatment is preferred) or moderate symptoms. PPIs are considered first line. Grade A recommendation (consistent high-quality evidence) on-demand therapy for recurrent symptoms appearing 3 months after resolution of last episode esomeprazole or omeprazole

2018 medSask

177. British Association for Psychopharmacology consensus statement on evidence-based treatment of insomnia, parasomnias and circadian rhythm disorders: An update

arousal systems. The same is true for any drug which blocks one of the other arousal systems; they produce a degree of sedation but are not generally e?ective hypnotics. However, someagentshavespeci?cactionsoncertainsleepparameters; for instance, drugs which block 5HT2 receptors (such as ritanserin or eplivanserin) can increase slow-wave sleep (Idzikowski et al., 1988; Landolt et al., 1999) whereas the alpha-1 adrenergic blocker prazosin is useful in post-trau- matic stress disorder-related nightmares (...) of proteins with bind- ing sites for a number of sleep-promoting drugs, in particu- lar benzodiazepines, so-called Z-drugs and barbiturates, all of which enhance the e?ects of GABA’s actions at the GABA A receptor. There are a number of subtypes of this receptor which are relevant for sleep, not only because of their di?erent location in the brain but also because of the fact that some hypnotic drugs are selective for a particular subtype. The alpha-1 subtype is highly expressed in the cortex and probably

2019 British Association for Psychopharmacology

179. Urolithiasis

., et al. Alpha blockers for treatment of ureteric stones: systematic review and meta-analysis. BMJ, 2016. 355: i6112. 106. Guercio, S., et al. Randomized prospective trial comparing immediate versus delayed ureteroscopy for patients with ureteral calculi and normal renal function who present to the emergency department. J Endourol, 2011. 25: 1137. 107. Ramsey, S., et al. Evidence-based drainage of infected hydronephrosis secondary to ureteric calculi. J Endourol, 2010. 24: 185. 108. Lynch, M.F., et (...) , 1994. 152: 1095. 114. Porpiglia, F., et al. Effectiveness of nifedipine and deflazacort in the management of distal ureter stones. Urology, 2000. 56: 579. 115. Dellabella, M., et al. Medical-expulsive therapy for distal ureterolithiasis: randomized prospective study on role of corticosteroids used in combination with tamsulosin-simplified treatment regimen and health-related quality of life. Urology, 2005. 66: 712. 116. Campschroer, T., et al. Alpha-blockers as medical expulsive therapy

2018 European Association of Urology

180. Male Sexual Dysfunction

Hypertens, 2004. 17: 1135. 199. Kloner, R.A., et al. Interaction between the phosphodiesterase 5 inhibitor, tadalafil and 2 alpha-blockers, doxazosin and tamsulosin in healthy normotensive men. J Urol, 2004. 172: 1935. 200. McCullough, A.R., et al. Achieving treatment optimization with sildenafil citrate (Viagra) in patients with erectile dysfunction. Urology, 2002. 60: 28. 201. Forgue, S.T., et al. Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol, 2006. 61: 280. 202. Nichols, D.J (...) with injection therapy: long-term dropout parameters. J Urol, 2000. 163: 467. 251. Buvat, J., et al. Double-blind multicenter study comparing alprostadil alpha-cyclodextrin with moxisylyte chlorhydrate in patients with chronic erectile dysfunction. J Urol, 1998. 159: 116. 252. Mulhall, J.P., et al. Intracavernosal forskolin: role in management of vasculogenic impotence resistant to standard 3-agent pharmacotherapy. J Urol, 1997. 158: 1752. 253. Bechara, A., et al. Comparative study of papaverine plus

2018 European Association of Urology

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