A hydrocarbon used as an industrial solvent. It has been used as an aerosal propellent, as a refrigerant and as a local anesthetic. (From Martindale, The Extra Pharmacopoeia, 31st ed, p1403)
An antidepressive agent that has also been used in the treatment of movement disorders. The mechanism of action is not well understood.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
A colorless and flammable gas at room temperature and pressure. Ethylene oxide is a bactericidal, fungicidal, and sporicidal disinfectant. It is effective against most micro-organisms, including viruses. It is used as a fumigant for foodstuffs and textiles and as an agent for the gaseous sterilization of heat-labile pharmaceutical and surgical materials. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p794)
A strong corrosive acid that is commonly used as a laboratory reagent. It is formed by dissolving hydrogen chloride in water. GASTRIC ACID is the hydrochloric acid component of GASTRIC JUICE.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
A broad class of substances encompassing all those that do not include carbon and its derivatives as their principal elements. However, carbides, carbonates, cyanides, cyanates, and carbon disulfide are included in this class.
A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions.
Activity involved in transfer of goods from producer to consumer or in the exchange of services.
The addition of descriptive information about the function or structure of a molecular sequence to its MOLECULAR SEQUENCE DATA record.
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.
Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
A congenital cardiovascular malformation in which the AORTA arises entirely from the RIGHT VENTRICLE, and the PULMONARY ARTERY arises from the LEFT VENTRICLE. Consequently, the pulmonary and the systemic circulations are parallel and not sequential, so that the venous return from the peripheral circulation is re-circulated by the right ventricle via aorta to the systemic circulation without being oxygenated in the lungs. This is a potentially lethal form of heart disease in newborns and infants.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.
Contractile activity of the MYOCARDIUM.
The hollow, muscular organ that maintains the circulation of the blood.
Solutions prepared for exchange across a semipermeable membrane of solutes below a molecular size determined by the cutoff threshold of the membrane material.
An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.
Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.
Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property.
Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.
The study of the effects of drugs on mental and behavioral activity.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Drugs that bind to and activate excitatory amino acid receptors.
The gradual destruction of a metal or alloy due to oxidation or action of a chemical agent. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A tough, malleable, iron-based alloy containing up to, but no more than, two percent carbon and often other metals. It is used in medicine and dentistry in implants and instrumentation.
A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic.
A neurological condition that is characterized by uncontrolled rapid irregular movements of the eye (OPSOCLONUS) and the muscle (MYOCLONUS) causing unsteady, trembling gait. It is also known as dancing eyes-dancing feet syndrome and is often associated with neoplasms, viral infections, or autoimmune disorders involving the nervous system.
Macrocyclic polyethers with the repeating unit of (-CH2-CH2-O)n where n is greater than 2 and some oxygens may be replaced by nitrogen, sulfur or phosphorus. These compounds are useful for coordinating CATIONS. The nomenclature uses a prefix to indicate the size of the ring and a suffix for the number of heteroatoms.
A family of hexahydropyridines.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade.
An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.
A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.

Evidence for beta3-adrenoceptor subtypes in relaxation of the human urinary bladder detrusor: analysis by molecular biological and pharmacological methods. (1/1629)

The purpose of the present study was to confirm the presence of beta3-adrenoceptor subtype in the relaxation of human urinary bladder detrusor tissue by reverse transcription-polymerase chain reaction (PCR); direct sequencing of the PCR product, in situ hybridization; and isometric contraction. Using reverse transcription-PCR, the mRNAs of three receptor subtypes (beta1, beta2, and beta3) were expressed in the human urinary bladder detrusor tissue. Direct sequencing of the PCR product of the above beta3-adrenoceptor revealed no mutation in the amplified regions. In situ hybridization with digoxygenin-labeled oligonucleotide probe revealed the presence of the mRNA of beta3-adrenoceptor subtype in the smooth muscle of the urinary bladder. The relaxant effects of isoproterenol (a nonselective beta-adrenoceptor agonist); ZD7114, BRL37344, and CGP12177A (putative selective beta3-adrenoceptor agonists); and SR59230A (a putative selective beta3-adrenoceptor antagonist) were tested using an isometric contraction technique. Isoproterenol in either the presence or absence of both atenolol (a beta1-adrenoceptor-selective antagonist) and butoxamine (a beta2-adrenoceptor-selective antagonist) revealed a relaxant effect on the carbachol-induced contraction of the human urinary bladder detrusor. Both BRL37344 and CGP12177A also revealed relaxant effects on the human urinary bladder detrusor, but ZD7114 did not elicit any relaxation. These results suggest that beta3-adrenoceptor may have some role in urine storage in the human urinary bladder.  (+info)

The role of the sympathetic nervous system in the regulation of leptin synthesis in C57BL/6 mice. (2/1629)

The objectives of this study were to determine whether leptin synthesis is regulated by the sympathetic nervous system and if so whether beta-adrenergic receptors mediate this effect. We show that sympathetic blockade by reserpine increases leptin mRNA levels in brown but not white adipose tissue, while acute cold-exposure decreases leptin expression 10-fold in brown adipose tissue and 2-fold in white adipose tissue. The cold-induced reduction in leptin mRNA can be prevented by a combination of propranolol and SR 59230A but not by either antagonist alone, indicating that beta3-adrenergic receptors and classical beta1/beta2-adrenergic receptors both mediate responses to sympathetic stimulation. Circulating leptin levels reflect synthesis in white adipose tissue but not in brown adipose tissue.  (+info)

Long-term suppression of synaptic transmission by tetanization of a single pyramidal cell in the mouse hippocampus in vitro. (3/1629)

1. The consequences of stimulating a single pyramidal cell in the CA1 area of the hippocampus for synaptic transmission in the stratum radiatum were investigated. 2. Tetanic activation of single pyramids caused by depolarizing current injection, but not an equal number of distributed action potentials, reduced excitatory transmission by 20 %, with a delayed onset, for more than 1 h. 3. EPSPs in the tetanized pyramidal cells were increased for equally long periods but this was not the cause of the field EPSP reduction. Spontaneous somatic IPSPs were not affected; evoked IPSPs were decreased in the tetanized cell. 4. Paired pulse facilitation of the field EPSPs was unchanged. 5. The field EPSP reduction was markedly diminished by a knife cut along the base of pyramidal cells in CA1. 6. The addition of antagonists of GABA, NMDA and metabotropic glutamate receptors blocked or diminished the field EPSP slope reduction evoked by intracellular stimulation. 7. Simultaneous recordings revealed long-lasting excitations of interneurons located in the outer oriens layer as a result of single pyramid tetanization. 8. Intense firing of small numbers of pyramidal cells can thus persistently inhibit mass transmission through the hippocampus. This effect involves activation of interneurons by glutamate receptors.  (+info)

Effects of beta2-adrenergic stimulation on single-channel gating of rat cardiac L-type Ca2+ channels. (4/1629)

Cardiac L-type Ca2+ channels can be stimulated by activation of beta2-adrenoceptors. We intended to determine how the gating behavior at the single-channel level (cell-attached configuration) is affected after selective stimulation of beta2-adrenoceptors. Rat cardiomyocytes were exposed to zinterol, a beta2-agonist (n = 7), isoproterenol (n = 6), a nonselective agonist, 8-bromo-cAMP (n = 6), and a combination of isoproterenol and ICI-118551 (n = 8), a selective beta2-receptor antagonist, or isoproterenol and CGP-20712A, a beta1-selective antagonist (n = 7). In all groups the ensemble-average current and the availability of the channels to open on depolarization were increased in a similar fashion. In addition, the open probability (Po) within active sweeps was elevated. However, zinterol exerted this effect in a unique manner. It elevated Po not by shortening closed times but solely by reducing active sweeps with very low Po and a short burst duration. All zinterol effects were abolished by ICI-118551 (n = 5) and mimicked by isoproterenol plus CGP-20712A (n = 7). We conclude that beta2-adrenoceptor activation of L-type channels differs qualitatively from the classical cAMP-dependent mechanism.  (+info)

Facilitatory beta2-adrenoceptors on cholinergic and adrenergic nerve endings of the guinea pig trachea. (5/1629)

Using electrical field stimulation of epithelium-denuded intact guinea pig tracheal tube preparations, we studied the presence and role of prejunctional beta2-adrenoceptors by measuring evoked endogenous acetylcholine (ACh) and norepinephrine (NE) release directly. Analysis of ACh and NE was through two HPLC systems with electrochemical detection. Electrical field stimulation (150 mA, 0.8 ms, 16 Hz, 5 min, biphasic pulses) released 29.1 +/- 2.5 pmol ACh/g tissue and 70.2 +/- 6.2 pmol NE/g tissue. Preincubation for 15 min with the selective beta2-adrenoceptor agonist fenoterol (1 microM) increased both ACh and NE overflow to 178 +/- 28 (P < 0.01) and 165 +/- 12% (P < 0.01), respectively, of control values, increases that were abolished completely by the selective beta2-adrenoceptor antagonist ICI-118551 (1 microM). Further experiments with increasing fenoterol concentrations (0.1-100 microM) and different preincubation periods (1, 5, and 15 min) showed a strong and concentration-dependent facilitation of NE release, with maximum response levels decreasing (from nearly 5-fold to only 2.5-fold of control value) with increasing agonist contact time. In contrast, sensitivity of facilitatory beta2-adrenoceptors on cholinergic nerves to fenoterol gradually increased when the incubation period was prolonged; in addition, a bell-shaped concentration-response relationship was found at 15 min of preincubation. Fenoterol concentration-response relationships (15-min agonist preincubation) in the presence of atropine and yohimbine (1 microM each) were similar in the case of NE release, but in the case of ACh release, the bell shape was lost. The results indicate a differential capacity and response time profile of facilitatory prejunctional beta2-adrenoceptors on adrenergic and cholinergic nerve terminals in the guinea pig trachea and suggest that the receptors on adrenergic nerves are more susceptible to desensitization.  (+info)

Pharmacological characterization of beta2-adrenoceptor in PGT-beta mouse pineal gland tumour cells. (6/1629)

1. The adrenoceptor in a mouse pineal gland tumour cell line (PGT-beta) was identified and characterized using pharmacological and physiological approaches. 2. Adrenaline and noradrenaline, adrenoceptor agonists, stimulated cyclic AMP generation in a concentration-dependent manner, but had no effect on inositol 1,4,5-trisphosphate production. Adrenaline was a more potent activator of cyclic AMP generation than noradrenaline, with half maximal-effective concentrations (EC50) seen at 175+/-22 nM and 18+/-2 microM for adrenaline and noradrenaline, respectively. 3. The addition of forskolin synergistically stimulated the adrenaline-mediated cyclic AMP generation in a concentration-dependent manner. 4. The pA2 value for the specific beta2-adrenoceptor antagonist ICI-118,551 (8.7+/-0.4) as an antagonist of the adrenaline-stimulated cyclic AMP generation were 3 units higher than the value for the betaI-adrenoceptor antagonist atenolol (5.6+/-0.3). 5. Treatment of the cells with adrenaline and forskolin evoked a 3 fold increase in the activity of serotonin N-acetyltransferase with the peak occurring 6 h after stimulation. 6. These results suggest the presence of beta2-adrenoceptors in mouse pineal cells and a functional relationship between the adenylyl cyclase system and the regulation of N-acetyltransferase expression.  (+info)

In vitro and in vivo characterization of intrinsic sympathomimetic activity in normal and heart failure rats. (7/1629)

Clinical studies conducted with carvedilol suggest that beta-adrenoceptor antagonism is an effective therapeutic approach to the treatment of heart failure. However, many beta-adrenoceptor antagonists are weak partial agonists and possess significant intrinsic sympathomimetic activity (ISA), which may be problematic in the treatment of heart failure. In the present study, the ISAs of bucindolol, xamoterol, bisoprolol, and carvedilol were evaluated and compared in normal rats [Sprague-Dawley (SD)], in rats with confirmed heart failure [spontaneously hypertensive heart failure (SHHF)], and in isolated neonatal rat cardiomyocytes. At equieffective beta1-adrenolytic doses, the administration of xamoterol and bucindolol produced a prolonged, equieffective, and dose-related increase in heart rate in both pithed SD rats (ED50 = 5 and 40 microgram/kg, respectively) and SHHF rats (ED50 = 6 and 30 microgram/kg, respectively). The maximum effect of both compounds in SHHF rats was approximately 50% of that observed in SD rats. In contrast, carvedilol and bisoprolol had no significant effect on resting heart rate in the pithed SD or SHHF rat. The maximum increase in heart rate elicited by xamoterol and bucindolol was inhibited by treatment with propranolol, carvedilol, and betaxolol (beta1-adrenoceptor antagonist) but not by ICI 118551 (beta2-adrenoceptor antagonist) in neonatal rat. When the beta-adrenoceptor-mediated cAMP response was examined in cardiomyocytes, an identical partial agonist/antagonist response profile was observed for all compounds, demonstrating a strong correlation with the in vivo results. In contrast, GTP-sensitive ligand binding and tissue adenylate cyclase activity were not sensitive methods for detecting beta-adrenoceptor partial agonist activity in the heart. In summary, xamoterol and bucindolol, but not carvedilol and bisoprolol, exhibited direct beta1-adrenoceptor-mediated ISA in normal and heart failure rats.  (+info)

Tolerability and efficacy of carvedilol in patients with New York Heart Association class IV heart failure. (8/1629)

OBJECTIVES: The purpose of this study was to assess the tolerability and efficacy of carvedilol in patients with New York Heart Association (NYHA) functional class IV symptoms. BACKGROUND: Carvedilol, a nonselective beta-adrenergic blocking drug with alpha-adrenergic blocking and antioxidant properties, has been shown to improve left ventricular function and clinical outcome in patients with mild to moderate chronic heart failure. METHODS: We retrospectively analyzed the outcomes of 230 patients with heart failure treated with carvedilol who were stratified according to baseline functional class: 63 patients were NYHA class IV and 167 were NYHA class I, II or III. Carvedilol was commenced at 3.125 mg b.i.d. and titrated to 25 mg b.i.d. as tolerated. Patients with class IV symptoms were older (p = 0.03), had lower left ventricular fractional shortening (p < 0.001), had lower six-min walk distance (p < 0.001) and were receiving more heart failure medications at baseline compared with less symptomatic patients. RESULTS: Nonfatal adverse events while taking carvedilol occurred more frequently in class IV patients (43% vs. 24%, p < 0.0001), and more often resulted in permanent withdrawal of the drug (25% vs. 13%, p < 0.01). Thirty-seven (59%) patients who were NYHA class IV at baseline had improved by one or more functional class at 3 months, 8 (13%) were unchanged and 18 (29%) had deteriorated or died. Among the less symptomatic group, 62 (37%) patients had improved their NYHA status at 3 months, 73 (44%) were unchanged and 32 (19%) had deteriorated or died. The differences in symptomatic outcome at three months between the two groups were statistically significant (p = 0.001, chi-square analysis). Both groups demonstrated similar significant improvements in left ventricular dimensions and systolic function. CONCLUSIONS: Patients with chronic NYHA class IV heart failure are more likely to develop adverse events during initiation and dose titration when compared with less symptomatic patients but are more likely to show symptomatic improvement in the long term. We conclude that carvedilol is a useful adjunctive therapy for patients with NYHA class IV heart failure; however, they require close observation during initiation and titration of the drug.  (+info)

TY - JOUR. T1 - CON (The window is closed). T2 - In patients with cirrhosis with ascites, the clinical risks of nonselective beta-blocker outweigh the benefits and should NOT be prescribed. AU - Aday, Ariel W.. AU - Rich, Nicole E.. AU - Mufti, Arjmand R.. AU - Tujios, Shannan R.. PY - 2018/5/1. Y1 - 2018/5/1. UR - http://www.scopus.com/inward/record.url?scp=85048328845&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=85048328845&partnerID=8YFLogxK. U2 - 10.1002/cld.699. DO - 10.1002/cld.699. M3 - Review article. C2 - 30992802. AN - SCOPUS:85048328845. VL - 11. SP - 123. EP - 127. JO - Clinical Liver Disease. JF - Clinical Liver Disease. SN - 2046-2484. IS - 5. ER - ...
T44.7X1 is a non-billable code, consider using a code with a higher level of specificity for a diagnosis of poisoning by beta-adrenoreceptor antagonists, accidental (unintentional).
Cardivas is a brand name for Carvedilol, which is a vasodilating non-selective beta-blocking agent with antioxidant properties. Carvedilol reduces the peripheral vascular resistance through...
InChI=1S/C20H27NO4/c1-15-5-4-6-18(11-15)25-14-17(22)13-21-10-9-16-7-8-19(23-2)20(12-16)24-3/h4-8,11-12,17,21-22H,9-10,13-14H2,1-3H3 ...
Professional guide for Esmolol Hydrochloride. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more.
Shahidullah, J, Kettlewell, P, DeHart, K, Ladd, I, Bogaczyk, T, Rooney, K, Signore, A, Larson, S (2016, Nov). Primary Care Behavioral Health Service Delivery: A Psychologist-Delivered Training Curricula for Pediatric Residency Programs. Poster presented at: The National Academies of Sciences, Engineering and Medicine Conference, in Washington, DC.. ...
Although carvedilol, a nonselective beta-blocker with alpha-adrenergic blocking and multiple ancillary activities, has been demonstrated to be superior to metoprolol in chronic heart failure, it remains unclear whether the superiority of carvedilol still exists in myocardial infarction (MI). Therefore, we performed a network meta-analysis of randomized controlled trials (RCTs) to compare the 2 drugs in patients with MI. All RCTs that compared either 2 of the following interventions, carvedilol, metoprolol, and placebo, for the treatment of MI were included. The Cochrane Collaboration Central Register of Controlled Trials, Embase, and PubMed were searched thoroughly for potential eligible studies. Finally, 12 RCTs involving 61,081 patients were included. Pooled results showed that compared with placebo, carvedilol and metoprolol significantly reduced composite cardiovascular events (risk ratio [RR] 0.63; 95% credible interval [CrI] 0.41, 0.85 for carvedilol; RR 0.78; 95% CrI 0.65, 0.93 for metoprolol)
TY - JOUR. T1 - Esmolol infusion versus propranolol infusion. T2 - Effects on heart rate and blood pressure in healthy volunteers. AU - Muller, Matthew D.. AU - Ahmad, Tariq Ali. AU - Pelaez, Alvaro F.Vargas. AU - Proctor, David N.. AU - Bonavia, Anthony S.. AU - Luck, J. Carter. AU - Maman, Stephan R.. AU - Ross, Amanda J.. AU - Leuenberger, Urs A.. AU - McQuillan, Patrick M.. N1 - Funding Information: This project was supported by a grant from the Association of Faculty and Friends of the Penn State Milton S. Hershey Medical Center (M. D. Muller). This project was also supported, in part, by National Center for Advancing Translational Sciences Grants UL1 TR-000127 and KL2 TR-000126 and also under a grant with the Pennsylvania Department of Health using Tobacco CURE funds (M. D. Muller). PY - 2017/3. Y1 - 2017/3. N2 - Despite its widespread clinical use, the β1-adrenergic receptor antagonist esmolol hydrochloride is not commonly used in human physiology research, and the effective dose of ...
Objective: To assess whether chronic treatment with carvedilol can increase myocardial blood flow (MBF) and MBF reserve in idiopathic dilated cardiomyopathy (IDC). Study design: In a double-blind, placebo-controlled trial, 16 consecutive patients with IDC were randomised to treatment with either carvedilol up to 25 mg twice a day (n = 8, 7 men, mean (SD) age 60 (9) years, mean (SD) left ventricular ejection fraction (LVEF) 30% (5%)), or placebo (n = 8 , 6 men, mean (SD) age 62 (9) years, mean (SD) LVEF 28% (6%), NS vs carvedilol group). Before and 6 months after treatment, regional MBF was measured at rest and after intravenous injection of dipyridamole (Dip; 0.56 mg/kg in 4 min) by positron emission tomography and using 13N-ammonia as a flow tracer. Exercise capacity was assessed as the time duration in a maximal bicycle exercise stress test. Results: Carvedilol induced a significant decrease in heart rate at rest and during maximal exercise, and an increase in exercise capacity. Absolute MBF ...
TY - JOUR. T1 - Carvedilol increases ciclosporin bioavailability by inhibiting P-glycoprotein-mediated transport. AU - Amioka, Katsuo. AU - Kuzuya, Takafumi. AU - Kushihara, Hideyuki. AU - Ejiri, Masayuki. AU - Nitta, Atsumi. AU - Nabeshima, Toshitaka. PY - 2007/10/1. Y1 - 2007/10/1. N2 - Carvedilol is often used to treat hypertension and for prophylaxis in vascular sclerosis in renal transplant recipients, who require concomitant treatment with ciclosporin. However, there are few reports regarding the pharmacokinetic interactions between carvedilol and ciclosporin. We have investigated the potential effects of carvedilol on the pharmacokinetics of ciclosporin, and examined the inhibitory effects of carvedilol on P-glycoprotein-mediated transcellular transport using Caco2 cells. Ciclosporin alone or with carvedilol was orally or intravenously administered to rats. The oral administration of carvedilol (10 mg kg-1) with Ciclosporin (10 mg kg-1) increased the whole blood concentration of ...
Penbutolol (brand names Levatol, Levatolol, Lobeta, Paginol, Hostabloc, Betapressin) is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was approved by the FDA in 1987 and was withdrawn from the US market by January 2015. Penbutolol is used to treat mild to moderate high blood pressure. Like other beta blockers it is not a first line treatment for this indication. It should not be used or only used with caution in people with heart failure and people with asthma. It may mask signs of low blood sugar in people with diabetes and it may mask signs of hyperthyroidism. Animal studies showed some signs of potential trouble for women who are pregnant, and it has not been tested in ...
Penbutolol (brand names Levatol , Levatolol , Lobeta , Paginol , Hostabloc , Betapressin ) is a medication in the class of beta blockers , used in the treatment of high blood pressure . Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was approved by the FDA in 1987 and was withdrawn from the US market by January 2015. Medical uses Penbutolol is used to treat mild to moderate high blood pressure . Like other beta blockers it is not a first line treatment for this indication. It should not be used or only used with caution in people with heart failure and people with asthma. It may mask signs of low blood sugar in people with diabetes and it may mask signs of hyperthyroidism. Animal studies showed some signs of potential trouble for women who are pregnant, and it has not
Penbutolol acts on the β1 adrenergic receptors in both the heart and the kidney. When β1 receptors are activated by a catecholamine, they stimulate a coupled G protein which activates adenylyl to convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP) [1]. The increase in cAMP leads to activation of protein kinase A (PKA), which alters the movement of calcium ions in heart muscle and increases heart rate [4]. Penbutolol blocks this and decreases heart rate, which lowers blood pressure. The ability of penbutolol to act as a partial agonist proves useful in the prevention of bradycardia as a result of decreasing the heart rate excessively [2]. Penbutolol binding β1 adrenergic receptors also alters kidney functions. Under normal physiological conditions, the enzyme renin converts angiotensinogen to angiotensin I, which will then be converted to angiotensin II. Angiotensin II stimulates the release of aldosterone from the adrenal gland, causing a decrease in electrolyte and ...
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Histamine can u symptoms of sneezing, itching, spacy eyes, and runny info on carvedilol. Acetaminophen and diphenhydramine is a few medicine used to end headache. This combination product contains 2 years, acetaminophen and an antihistamine. Acetaminophen studies to reduce info on carvedilol andor quickly to moderate pain (such as other, backache, achespains due to person strain, cold, or flu). The antihistamine in this medication may cause drowsiness, and therefore it can also be. Tho interaction with Tylenol PM is not a year with your blood clotting drugs, you also take taking herbs. More:. ...
The purpose of the study is to measure decline in episodic memory in participants with early AD taking carvedilol compared to placebo treatment as evidenced by the Hopkins Verbal Learning Test (HVLT). cerebrospinal fluid levels of Aβ oligomers in early AD, will be measured in participants receiving carvedilol treatment when compared to placebo treatment. Adverse effects will be monitored in participants receiving carvedilol when compared to placebo.. To assess adverse events, routine chemistry and hematology studies, vital signs, and electrocardiographic parameters before and after 6 months randomized placebo-controlled double-blind treatment with carvedilol at a target dose of 25 mg daily, comparing 25 early AD participants taking carvedilol vs. 25 early AD participants taking placebo. ...
The nonselective beta-adrenoceptor and selective alpha1-adrenoceptor blocker carvedilol is widely used in hypertensive and/or cardiac failure patients. However, there have been few studies regarding the effects of carvedilol on cardiac arrest induced by airway obstruction. The present study was performed to evaluate the effects of beta-blocker during cardiopulmonary resuscitation (CPR) in a rat model of cardiac arrest induced by airway obstruction. Twenty-four male Sprague Dawley rats were used. Animals were randomly assigned to one of two groups (n=12 per group), control group: no medication, treatment group: oral administration of beta-blocker (Carvedilol 10 mg/kg/day) for 5 days. After then, all animals were anesthetized with pentobarbital ip. Cardiac arrest was induced by airway obstruction. After 3 minutes of cardiac arrest, animals were received CPR. The rate of chest compressions (CC) was 240 -260/min in all groups. The rate of ventilation was 32 breaths/min in FIO2 0.21. After 5 minutes ...
The Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) study evaluated the effect of carvedilol, an adrenergic blocker, on 2,289 patients with severe congestive heart failure (CHF). While previous studies have shown that beta-blocking agents improve functional status and reduce morbidity in patients with mild to moderate heart failure, their benefits in patients with severe CHF have not been established. The initial study, which was published in May 2001, investigated the effects of carvedilol on patient survival. Packer and colleagues did a follow-up study to examine the effect of carvedilol on morbidity.. Patients were included in the study if they had dyspnea lasting two months or more or fatigue at rest or on minimal exertion, and a left ventricular ejection fraction of less than 25 percent. The subjects could be inpatients or outpatients. Key exclusion criteria were acute illness requiring prolonged hospitalization and use of an intravenous positive inotropic agent or a ...
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Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific literature by Sumitomo Chemical as β-adrenergic blocking, antiarrhythmic compound S-596. It is used in the treatment of high blood pressure and essential tremor. Recommended dosage is 10-30 mg per day. Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes. Can J Physiol Pharmacol. 79 (7): 585-593. doi:10.1139/cjpp-79-7-585. PMID 11478592. Takahashi, H; Yoshida, T; Nishimura, M; Nakanishi, T; Kondo, M; Yoshimura, M (September 1992). Beta-3 Adrenergic Agonist, BRL-26830A, and Alpha/Beta Blocker, Arotinolol, Markedly Increase Regional Blood Flow in the Brown Adipose Tissue in Anesthetized Rats. Japanese Circulation Journal. 56 (9): 936-42. ...
LABETOLOL. Blocks the alpha-1, beta-1 and beta-2 receptors and alpha-1 receptor blokade is responsible for the vasodilator effect. It has a partial agonist effect and is metabolised mainly by the liver.. BUCINDOLOL. Bucindolol is a non-selective and lipophilic beta blocker with a higher affinity then beta receptors. Vasodilator effects seem to be due to direct alpha-1 blockade(2).. BEST (Beta-Blocker Evaluation of Survival Trial) failed to show any benefit of bucindolol for total mortality in Class III-IV heart failure patients when added to the usual care (25). In the Class IV patients bucindolol even increased the composite end point of death and heart failure hospitalisations in six-months follow-up. The annual mortality for Class IV patients in the placebo group of the BEST study was 28 % which was higher than CIBIS (20 %), COPERNICUS (19 %) and MERIT-HF (25 %) studies. It has been suggested that the Class IV patients in BEST study were much sicker than the other studies and this contributed ...
The long term effects of treatment with xamoterol in 14 patients aged 44-73 with mild to moderate heart failure as a result of ischaemic heart disease are reported. After 18 months treatment with xamoterol, patients were assessed in a randomised double blind crossover comparison of xamoterol (200 mg twice a day) and placebo, each given for one month. Compared with placebo, xamoterol significantly increased exercise duration and work done on a bicycle ergometer and reduced the maximum exercise heart rate. Assessment of symptoms and activities at 12 months by visual analogue and Likert scales showed a trend towards the relief of symptoms of breathlessness and tiredness and an improvement in activity. There was an improvement in the clinical signs of heart failure and no haemodynamic deterioration over a 12 month period as assessed by ejection fraction. The improvement in exercise tolerance, symptoms, and activities was sustained for 18 months without side effects or development of tolerance. ...
We prospectively investigated the consequences of adding carvedilol to the typical treatment of ischemic and nonischemic dilated cardiomyopathy (DCM), by measuring the plasma degrees of pro-inflammatory cytokines. In nonischemic individuals on carvedilol, IL-6 and TNF- amounts dropped considerably (P=0.018 and P=0.004, respectively). The remaining ventricular ejection portion more than doubled (P=0.006). In nonischemic individuals on regular treatment, no significant switch occurred in virtually any worth. Carvedilol suppressed the plasma degrees CHIR-99021 manufacture of TNF- and IL-6 both in ischemic and nonischemic individuals. The carvedilol impact was even more pronounced in individuals with nonischemic dilated cardiomyopathy than in people that have ischemic disease. ensure that you the paired-sample check were found in the evaluation of the adjustments that were appropriate with the standard distribution. The Mann-Whitney SFN U and Wilcoxon assessments were used to investigate changes ...
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Actually, considerable heterogeneity in, eg, pharmacokinetic, pharmacological, and physicochemical properties exists across the completely different courses of β-blockers, particularly between the second-generation and newer third-technology brokers. Carvedilol is a vasodilating noncardioselective third-technology β-blocker, without the unfavorable hemodynamic and metabolic effects of conventional β-blockers, which can be used as a cardioprotective agent. Compared with conventional β-blockers, carvedilol maintains cardiac output, has a reduced prolonged impact on coronary heart rate, and reduces blood stress by decreasing vascular resistance. Studies have additionally shown that carvedilol displays favorable effects on metabolic parameters, eg, glycemic management, insulin sensitivity, and lipid metabolism, suggesting that it could be thought of in the treatment of patients with metabolic syndrome or diabetes. Prior to drug initiation, stabilize hemodynamics and minimize fluid retention. ...
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Baseline characteristics were well matched between the treatment groups. Mean body mass index at baseline was 34, and hemoglobin A1c (HbA1c) was 7.2%. Multiple antidiabetic medications were used in 55% of patients, and 8% of patients were insulin-dependent. In addition to 99% of patients taking angiotensin-converting enzyme (ACE) inhibitors or angiotensin-receptor blockers (ARBs) at baseline, 45% were taking a statin. Treatment duration was slightly but significantly longer in the carvedilol group (155 days vs. 147 days for metoprolol, p=0.01 ...
TY - JOUR. T1 - Response-adaptive treatment allocation for survival trials with clustered right-censored data. AU - Su, Pei Fang. AU - Cheung, Siu Hung. PY - 2018/7/20. Y1 - 2018/7/20. N2 - A comparison of 2 treatments with survival outcomes in a clinical study may require treatment randomization on clusters of multiple units with correlated responses. For example, for patients with otitis media in both ears, a specific treatment is normally given to a single patient, and hence, the 2 ears constitute a cluster. Statistical procedures are available for comparison of treatment efficacies. The conventional approach for treatment allocation is the adoption of a balanced design, in which half of the patients are assigned to each treatment arm. However, considering the increasing acceptability of responsive-adaptive designs in recent years because of their desirable features, we have developed a response-adaptive treatment allocation scheme for survival trials with clustered data. The proposed ...
The stress-related catecholamine hormones and the α- and β-adrenergic receptors (α- and β-AR) may affect carcinogenesis. The β-AR GRK/β-arrestin biased agonist carvedilol can induce β-AR-mediated transactivation of the epidermal growth factor receptor (EGFR). The initial purpose of this study was to determine whether carvedilol, through activation of EGFR, can promote cancer. Carvedilol failed to promote anchorage-independent growth of JB6 P+ cells, a skin cell model used to study tumor promotion. However, at non-toxic concentrations carvedilol dose-dependently inhibited EGF-induced malignant transformation of JB6 P+ cells suggesting that carvedilol has chemopreventive activity against skin cancer. Such effect was not observed for the β-AR agonist isoproterenol and the β-AR antagonist atenolol. Gene expression, receptor binding, and functional studies indicate that JB6 P+ cells only express β2-ARs. Carvedilol, but not atenolol, inhibited EGF-mediated activator protein-1 (AP-1) ...
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TY - JOUR. T1 - Carvedilol, a pharmacological antioxidant, inhibits neointimal matrix metalloproteinase-2 and -9 in experimental atherosclerosis. AU - Wu, Tao Cheng. AU - Chen, Yung Hsiang. AU - Leu, Hsin Bang. AU - Chen, Yuh Lien. AU - Lin, Feng Yen. AU - Lin, Shing Jong. AU - Chen, Jaw Wen. PY - 2007/12/1. Y1 - 2007/12/1. N2 - Matrix metalloproteinase (MMP) is critical to the progression of atherosclerosis and neointima hyperplasia after vascular injury. We investigated the effects of carvedilol, a pharmacological antioxidant with α- and β-adrenergic blocking activity, on MMP-2 and MMP-9 expression. Vascular injury was induced with the balloon catheters on abdominal aortas of high-cholesterol-fed rabbits. On Day 21, there was significant aortic neointima formation with increased oxidative DNA damage by immunostaining with 8-hydroxy-2′-deoxyguanosine and enhanced MMP-2 and MMP-9 expressions by Western blotting, which were significantly reduced by oral administration of carvedilol (20 ...
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Results 36% (37/104) of patients showed a HVPG response to propranolol. Among the propranolol non-responders 56% (38/67) eventually achieved a haemodynamic response with carvedilol, while 44% (29/67) patients were finally treated with EBL. The decrease in HVPG was significantly greater with carvedilol (median 12.5 mg/day) than with propranolol (median 100 mg/day): −19±10% versus −12±11% (p,0.001). During a 2 year follow-up bleeding rates for PROP were 11% versus CARV 5% versus EBL 25% (p=0.0429). Fewer episodes of hepatic decompensation (PROP 38%/CARV 26% vs EBL 55%; p=0.0789) and significantly lower mortality (PROP 14%/CARV 11% vs EBL 31%; p=0.0455) were observed in haemodynamic responders compared to the EBL group.. ...
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"Ethanolamines and Propanolamines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ...
"Ethanolamines and Propanolamines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ...
Ethanolamines Aminomethyl propanol Heptaminol Isoetarine Propanolamines Sphingosine Methanolamine (simplest amino alcohol) ... "Ethanolamines and Propanolamines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ...
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The propanolamines include many derivatives where the amine is secondary or tertiary. The parent propanolamines are colorless ... "Ethanolamines and Propanolamines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ...
Propanolamines Aminoaldehydes and aminoketones Nomenclature of Organic Chemistry : IUPAC Recommendations and Preferred Names ...
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Matthias Frauenkron, Johann-Peter Melder, Günther Ruider, Roland Rossbacher, Hartmut Höke "Ethanolamines and Propanolamines" in ...
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... are a class of chemical compounds, many of which are pharmaceutical drugs. They are amino alcohols that are ... Propanolamines include: Acebutolol Atenolol Betaxolol Bisoprolol Metoprolol Nadolol Penbutolol Phenylpropanolamine Pindolol ... "Ethanolamines and Propanolamines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ... Practolol Propranolol Ritodrine Timolol Propanolamine Propanolamines at the US National Library of Medicine Medical Subject ...
Propanolamines are a class of chemical compounds, many of which are pharmaceutical drugs. They are amino alcohols that are ... Propanolamines include: Acebutolol Atenolol Betaxolol Bisoprolol Metoprolol Nadolol Penbutolol Phenylpropanolamine Pindolol ... "Ethanolamines and Propanolamines". Ullmanns Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ... Practolol Propranolol Ritodrine Timolol Propanolamine Propanolamines at the US National Library of Medicine Medical Subject ...
"Ethanolamines and Propanolamines". Ullmanns Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. doi:10.1002/14356007. ...
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Propanolamines / administration & dosage, adverse effects, therapeutic use*. Pulmonary Wedge Pressure / drug effects. Stroke ... 0/Adrenergic beta-Antagonists; 0/Propanolamines; 84057-94-3/esmolol From MEDLINE®/PubMed®, a database of the U.S. National ...
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Tahirovic YA, Geballe M, Gruszecka-Kowalik E, Myers SJ, Lyuboslavsky P, Le P et al. (2008). Enantiomeric propanolamines as ...
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All of the propanolamines showed inhibitory properties in the lubricants. Isopropanolamines were found to have very weak ... Seventeen propanolamines, six diisopropanolamines, and two butanolamines were studied for their antimicrobial properties ...
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Propanolamines [D02.033.100.624]. *Acebutolol [D02.033.100.624.025]. *Phenoxypropanolamines [D02.033.100.624.698]. *Acebutolol ...
2008) Enantiomeric propanolamines as selective N-methyl-d-aspartate 2B receptor antagonists. J Med Chem 51:5506-5521. ... 1B and 5). However, the compounds with para-N-phenylmethanesulfonamide (e.g., propanolamines and compounds 15, 29, 49, 52, and ... The propanolamines show a preference for the amine at position three, the amines being either secondary or tertiary (Tahirovic ... such as dichloro in the case of propanolamines, strongly control potency (Tahirovic et al., 2008). The binding interface ...
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Lakkireddy, D., Vallakati, A., Kanmanthareddy, A., Feldman, T., Gibson, D., Price, M., Rubenson, D. S., Cheng, J., Valderrábano, M., Fernando, R. R., Laing, S. T., Chung, E., Bommana, S., Atkins, D., Pillarisetti, J., Knight, B. P., Evonich, R., Rasekh, A., Gray, J., Sridhar, A. M. & 4 othersEarnest, M., Ferrell, R., Nath, J. & Reddy, Y. M., Jan 1 2015, In : Journal of the American College of Cardiology. 65, 15, p. 1595-1596 2 p.. Research output: Contribution to journal › Letter ...
... propanol-amines, or any other such base providing a salt of the fatty acid being neutralized. The base is added to neutralize ...
Class Antihyperglycaemics; Chlorobenzenes; Heterocyclic bicyclo compounds; Obesity therapies; Propanolamines; Small molecules * ...
TY - GEN. T1 - Reaction kinetics of some important alkanolamines with carbon dioxide in aqueous solutions using stopped flow technique. AU - Al Marri, Jaber. AU - Rongwong, Wichitpan. AU - Benamor, Abdelbaki. PY - 2015/1/1. Y1 - 2015/1/1. N2 - The kinetics of the reactions between aqueous solutions of carbon dioxide and Aminomethylpropanol (AMP), Aminobutanol (AB), Aminopropanol (AP), Diethanolamine (DEA) and Ethanolamine (MEA) were investigated over a temperature range of 293-313 K and different amine concentrations using a stopped flow technique. It was found that at each temperature, MEA reacts faster than AB, which in turn, reacts faster than AMP and DEA respectively. Reactions of MEA, DEA and AB can be explained by the zwitterion mechanism. However, the reaction mechanism of the AMP, a hindered amine, is suggested to be similar to that for tertiary amines, but at a faster rate. The rate constants required to predict reaction rates of these amines with CO2 have been calculated and presented ...
Propanolamines/pharmacology. *Rats. *Rats, Inbred SHR. *Rats, Inbred WKY. *Rats, Wistar. *Receptors, Adrenergic, beta/ ...
Propanolamines/pharmacology. *Pyrrolidines/pharmacology. Substances. *1-phenyl-2-palmitoylamino-3-pyrrolidino-1-propanol ...
  • 2006 ). Glycidyl phenyl ether is a vital drug intermediate for the preparing aryloxy propanolamines (Bala et al. (springeropen.com)
  • Propanolamines are a class of chemical compounds, many of which are pharmaceutical drugs. (wikipedia.org)