Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.Adrenergic beta-Antagonists: 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.Practolol: A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.Receptors, Adrenergic: Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. 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. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.Sympatholytics: Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.Epinephrine: The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Atropine: An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.Dogs: The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)Catecholamines: A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Amino Alcohols: Compounds possessing both a hydroxyl (-OH) and an amino group (-NH2).Receptors, Adrenergic, alpha: One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.Physical Exertion: Expenditure of energy during PHYSICAL ACTIVITY. Intensity of exertion may be measured by rate of OXYGEN CONSUMPTION; HEAT produced, or HEART RATE. Perceived exertion, a psychological measure of exertion, is included.Tremor: Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Sympathomimetics: Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Hemodynamics: The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.Betaxolol: A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.Sympathetic Nervous System: The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.Pulse: The rhythmical expansion and contraction of an ARTERY produced by waves of pressure caused by the ejection of BLOOD from the left ventricle of the HEART as it contracts.Hemangioma: A vascular anomaly due to proliferation of BLOOD VESSELS that forms a tumor-like mass. The common types involve CAPILLARIES and VEINS. It can occur anywhere in the body but is most frequently noticed in the SKIN and SUBCUTANEOUS TISSUE. (from Stedman, 27th ed, 2000)Hemangioma, Capillary: A dull red, firm, dome-shaped hemangioma, sharply demarcated from surrounding skin, usually located on the head and neck, which grows rapidly and generally undergoes regression and involution without scarring. It is caused by proliferation of immature capillary vessels in active stroma, and is usually present at birth or occurs within the first two or three months of life. (Dorland, 27th ed)Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Adrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.Heart: The hollow, muscular organ that maintains the circulation of the blood.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Delayed-Action Preparations: Dosage forms of a drug that act over a period of time by controlled-release processes or technology.Carbimazole: An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.Ethanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.Placebos: Any dummy medication or treatment. Although placebos originally were medicinal preparations having no specific pharmacological activity against a targeted condition, the concept has been extended to include treatments or procedures, especially those administered to control groups in clinical trials in order to provide baseline measurements for the experimental protocol.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Depression, Chemical: The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.Clinical Trials as Topic: Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries.Hypertension, Portal: Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Levobunolol: The L-Isomer of bunolol.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Myocardial Contraction: Contractile activity of the MYOCARDIUM.Celiprolol: A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Cardiac Output: The volume of BLOOD passing through the HEART per unit of time. It is usually expressed as liters (volume) per minute so as not to be confused with STROKE VOLUME (volume per beat).Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.Stimulation, Chemical: The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.

Drug-protein binding and blood-brain barrier permeability. (1/3372)

The permeability surface area (PS) product, an index of permeability of the blood-brain barrier (BBB), was measured by using the in situ perfusion method. In the cerebral circulation, the fraction of drug that permeates into the brain through the BBB is not only the unbound fraction but also the fraction dissociated from the protein in the perfusate. The sum of these two fractions, the apparent exchangeable fraction, was estimated by fitting the parameters of the BBB permeability under the condition of varying BSA concentrations in the perfusate. The unbound fraction of drugs in a buffer containing 0.5 mM BSA was measured by using the ultrafiltration method in vitro, and the apparent exchangeable fraction was measured in vivo by using the intracarotid artery injection method. The apparent exchange fraction was 100% for S-8510, 96.5% for diazepam, 90.9% for caffeine, 38.3% for S-312-d, 33.1% for propranolol, and 6.68% for (+)-S-145 Na, and each of these was higher than the corresponding unbound fraction in vitro in all drugs. The apparent exchangeable fractions, for example, were 8 times higher for diazepam and 38 times for S-312-d than the unbound fractions in vitro. The apparent exchangeable fraction of drugs was also estimated from the parameters obtained with the perfusion method. Because drugs can be infused for an arbitrary length of time in the perfusion method, substances with low permeability can be measured. The apparent exchangeable fractions obtained with this method were almost the same as those obtained with the intracarotid artery injection method.  (+info)

The role of the sympathetic nervous system in the regulation of leptin synthesis in C57BL/6 mice. (2/3372)

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)

Neuroregulation by vasoactive intestinal peptide (VIP) of mucus secretion in ferret trachea: activation of BK(Ca) channels and inhibition of neurotransmitter release. (3/3372)

1. The aims of this study were to determine: (1) whether vasoactive intestinal peptide (VIP) regulates cholinergic and 'sensory-efferent' (tachykininergic) 35SO4 labelled mucus output in ferret trachea in vitro, using a VIP antibody, (2) the class of potassium (K+) channel involved in VIP-regulation of cholinergic neural secretion using glibenclamide (an ATP-sensitive K+ (K(ATP)) channel inhibitor), iberiotoxin (a large conductance calcium activated K+ (BK(ca)) channel blocker), and apamin (a small conductance K(ca) (SK(ca)) channel blocker), and (3) the effect of VIP on cholinergic neurotransmission using [3H]-choline overflow as a marker for acetylcholine (ACh) release. 2. Exogenous VIP (1 and 10 microM) alone increased 35SO4 output by up to 53% above baseline, but suppressed (by up to 80% at 1 microM) cholinergic and tachykininergic neural secretion without altering secretion induced by ACh or substance P (1 microM each). Endogenous VIP accounted for the minor increase in non-adrenergic, non-cholinergic (NANC), non-tachykininergic neural secretion, which was compatible with the secretory response of exogenous VIP. 3. Iberiotoxin (3 microM), but not apamin (1 microM) or glibenclamide (0.1 microM), reversed the inhibition by VIP (10 nM) of cholinergic neural secretion. 4. Both endogenous VIP (by use of the VIP antibody; 1:500 dilution) and exogenous VIP (0.1 microM), the latter by 34%, inhibited ACh release from cholinergic nerve terminals and this suppression was completely reversed by iberiotoxin (0.1 microM). 5. We conclude that, in ferret trachea in vitro, endogenous VIP has dual activity whereby its small direct stimulatory action on mucus secretion is secondary to its marked regulation of cholinergic and tachykininergic neurogenic mucus secretion. Regulation is via inhibition of neurotransmitter release, consequent upon opening of BK(Ca) channels. In the context of neurogenic mucus secretion, we propose that VIP joins NO as a neurotransmitter of i-NANC nerves in ferret trachea.  (+info)

Wavelet transform to quantify heart rate variability and to assess its instantaneous changes. (4/3372)

Heart rate variability is a recognized parameter for assessing autonomous nervous system activity. Fourier transform, the most commonly used method to analyze variability, does not offer an easy assessment of its dynamics because of limitations inherent in its stationary hypothesis. Conversely, wavelet transform allows analysis of nonstationary signals. We compared the respective yields of Fourier and wavelet transforms in analyzing heart rate variability during dynamic changes in autonomous nervous system balance induced by atropine and propranolol. Fourier and wavelet transforms were applied to sequences of heart rate intervals in six subjects receiving increasing doses of atropine and propranolol. At the lowest doses of atropine administered, heart rate variability increased, followed by a progressive decrease with higher doses. With the first dose of propranolol, there was a significant increase in heart rate variability, which progressively disappeared after the last dose. Wavelet transform gave significantly better quantitative analysis of heart rate variability than did Fourier transform during autonomous nervous system adaptations induced by both agents and provided novel temporally localized information.  (+info)

Assessment of cardiac sympathetic regulation by respiratory-related arterial pressure variability in the rat. (5/3372)

1. Mechanical ventilation evokes a corresponding arterial pressure variability (APV) which is decreased by beta-adrenoceptor antagonism. Therefore, in this study we set out to determine whether the respiratory-related APV can be used to assess cardiac sympathetic tone. 2. Computer-generated broad-band mechanical ventilation (0-3 Hz) was applied to Sprague-Dawley rats that had been anaesthetized with ketamine and paralysed with pancuronium. APV and its relationship to lung volume variability (LVV-APV) was systematically quantified with auto- or cross-spectral frequency domain analysis. 3. APV and LVV-APV transfer magnitudes between 0.5 and 1.5 Hz showed dose-dependent suppression by propranolol from 0.01 to 1 mg kg-1, while the static value of arterial pressure remained unchanged. Stroke volume variability, assessed by the use of a pulse contour method, exhibited a similar pattern of suppression by propranolol. In contrast, heart rate variability was not lowered with propranolol. 4. The effect of propranolol on respiratory-related APV persisted even in the presence of combined alpha-adrenoceptor and muscarinic receptor blockade by phentolamine and atropine. 5. The frequency range of 0.5-1.0 Hz was optimal for LVV-APV transfer magnitude to correlate with cardiac sympathetic tone. 6. We conclude that respiratory-related APV may provide a valid assessment of cardiac sympathetic regulation which is independent of parasympathetic and vascular sympathetic influences in ketamine-anaesthetized and positive pressure-ventilated rats.  (+info)

beta2-adrenergic receptor-selective agonist clenbuterol prevents Fas-induced liver apoptosis and death in mice. (6/3372)

Stimulation of the cAMP-signaling pathway modulates apoptosis in several cell types and inhibits Jo2-mediated apoptosis in cultured rat hepatocytes. No information is yet available as to whether the hepatic beta2-adrenergic receptor (AR) expression level, including beta2-AR-dependent adenylyl cyclase activation, modulates hepatocyte sensitivity to apoptosis in vivo or whether this sensitivity can be modified by beta2-AR ligands. We have examined this using C57BL/6 mice, in which hepatic beta2-AR densities are low, and transgenic F28 mice, which overexpress beta2-ARs and have elevated basal liver adenylyl cyclase activity. The F28 mice were resistant to Jo2-induced liver apoptosis and death. The beta-AR antagonist propranolol sensitized the F28 livers to Jo2. In normal mice clenbuterol, a beta2-AR-specific agonist, considerably reduced Jo2-induced liver apoptosis and death; salbutamol, another beta2-AR-selective agonist, also reduced Jo2-induced apoptosis and retarded death but with less efficacy than clenbuterol; and propranolol blocked the protective effect of clenbuterol. This indicates that the expression level of functional beta2-ARs modulates Fas-regulated liver apoptosis and that this apoptosis can be inhibited in vivo by giving beta2-AR agonists. This may well form the basis for a new therapeutic approach to diseases involving abnormal apoptosis.  (+info)

Endothelin antagonists block alpha1-adrenergic constriction of coronary arterioles. (7/3372)

We have previously observed that intracoronary administration of the alpha1-adrenergic agonist phenylephrine (PE) over a period of minutes induced both an immediate and long-lasting (2 h) vasoconstriction of epicardial coronary arterioles. Because it is unlikely that alpha1-adrenergic constriction would persist for hours after removal of the agonist, this observation supports the view that another constrictor(s) is released during alpha1-adrenergic activation and induces the prolonged vasoconstriction. Therefore, we hypothesized that the prolonged microvascular constriction after PE is due to the production of endothelin (ET). We focused on ET not only because this peptide produces potent vasoconstriction but also because its vasoconstrictor action is characterized by a long duration. To test this hypothesis, the diameters of coronary arterioles (<222 micrometers) in the beating heart of pentobarbital-anesthetized dogs with stroboscopic intravital microscopy were measured during a 15-min intracoronary infusion of PE (1 microgram. kg-1 . min-1) and at 15-min intervals for a total of 120 min. All experiments were performed in the presence of beta-adrenergic blockade with propranolol. At 120 min, arterioles in the PE group were constricted (-23 +/- 9% change in diameter vs. baseline). Pretreatment with the ET-converting enzyme inhibitor phosphoramidon or the ETA-receptor antagonist FR-139317 prevented the PE-induced constriction at 120 min (-1 +/- 3 and -6 +/- 3%, respectively, P < 0.01 vs. PE). Pretreatment with the selective alpha1-adrenergic antagonist prazosin (Prz) also prevented the sustained constriction (0 +/- 2%, P < 0.01 vs. PE) but Prz given 60 min after PE infusion did not (-13 +/- 3%). In the aggregate, these results show that vasoconstriction of epicardial coronary arterioles via alpha1-adrenergic activation is blocked by an ET antagonist and an inhibitor of its production. From these data, we conclude that alpha1-adrenergic activation promotes the production and/or release of ET, which produces or facilitates microvascular constriction of epicardial canine coronary arterioles.  (+info)

beta2-adrenoceptor agonists reduce the decline of rat diaphragm twitch force during severe hypoxia. (8/3372)

The aim of the present study was to investigate the in vitro effects of the short-acting beta2-adrenoceptor agonist salbutamol and the long-acting beta2-adrenoceptor agonist salmeterol on hypoxia-induced rat diaphragm force reduction. In vitro diaphragm twitch force (Pt) and maximal tetanic force (Po) of isolated diaphragm muscle strips were measured for 90 min during hyperoxia (tissue bath PO2 83.8 +/- 0.9 kPa and PCO2 3.9 +/- 0.1 kPa) or severe hypoxia (PO2 7.1 +/- 0.3 kPa and PCO2 3.9 +/- 0.1 kPa) in the presence and absence of 1 microM salbutamol or 1 microM salmeterol. During hyperoxia, salbutamol and salmeterol did not significantly alter the time-related decreases in Pt and Po (to approximately 50% of initial values). Salbutamol had no effects on Po or the Pt-to-Po ratio. Salmeterol treatment significantly reduced Po and increased the Pt-to-Po ratio during hyperoxia (P < 0.05 compared with control value). Hypoxia resulted in a severe decrease in Pt (to approximately 30% of initial value) and Po after 90 min. Both salbutamol and salmeterol significantly reduced the decline in Pt during hypoxia (P < 0.05). The reduction in Po was not prevented. Salbutamol increased Pt rapidly but transiently. Salmeterol had a delayed onset of effect and a longer duration of action. Addition of 1 microM propranolol (a nonselective beta-adrenoceptor antagonist) did not alter Pt, Po, or the Pt-to-Po ratio during hypoxia but completely blocked the inotropic effects of salbutamol and salmeterol, indicating that these effects are dependent on beta2-adrenoceptor agonist-related processes.  (+info)

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  • However, it undergoes high first-pass metabolism by the liver and on average, only about 25% of propranolol reaches the systemic circulation. (nih.gov)
  • After liver has processed this (with propranolol, up to 90% of the original drug is not accepted and goes directly to kidney and out of the body without any use! (nomorepanic.co.uk)
  • Autoradiography showed high concentrations of propranolol in the periportal zones of the liver lobule. (aspetjournals.org)
  • Several of these drugs were able to displace small amounts of propranolol from the liver. (aspetjournals.org)
  • Approximately 75% of a dose of galantamine is metabolised in the propranolol stopping liver. (jaimeurrutia.com)
  • Liver the kidney side effects when using protease sodium diclofenac inhibitors inhibit the the u.Monitoramento do propranolol em crianças submetidas a correção cirúrgica da Tetralogia de Fallot através de cromatografia líquida de alta eficiência. (slipcamgirls.ml)
  • Propranolol is propranolol extensively metabolized by the liver. (dresdencodak.com)
  • Neonatal hepatic propranolol elimination: studies in the isolated perfused neonatal sheep liver. (biomedsearch.com)
  • Using the isolated perfused neonatal sheep liver model, we examined the disposition of propranolol (n = 8, age 0.25-10 days) and compared our findings with our previous study from the perfused near-term fetal sheep liver (Ring JA, et al. (biomedsearch.com)
  • Our study shows that propranolol is rapidly eliminated by the neonatal liver to form several metabolites at rates far greater than in the fetal liver, but rates of elimination have not yet reached that reported in the adult sheep liver. (biomedsearch.com)
  • We found that carboxylesterase (CES), especially the rat CES1 isozyme, Hydrolase A, is expressed in rat skin and that the hydrolysis of p -nitrophenyl acyl derivatives and caproyl-propranolol (PL) was 20-fold lower in the 9000 g supernatant fraction of skin homogenate than in liver microsomes. (mdpi.com)
  • Some experimentation has been conducted in other psychiatric areas: Post-traumatic stress disorder (PTSD) and specific phobias (see subsection below) Aggressive behavior of patients with brain injuries Treating the excessive drinking of fluids in psychogenic polydipsia Propranolol is being investigated as a potential treatment for PTSD. (wikipedia.org)
  • Five of the trials are currently enrolling patients, including four randomized comparison trials with propranolol and a trial evaluating the efficacy of nadolol. (medscape.com)
  • The pharmacokinetics of propranolol have not been investigated in patients under 18 years of age. (nih.gov)
  • Propranolol injection is not recommended for treatment of cardiac arrhythmias in pediatric patients. (nih.gov)
  • For Low Income, Uninsured Patients propranolol 40. (spiritofbaraka.com)
  • Primary: To evaluate the efficacy of extended-release propranolol compared to placebo for reducing pain in patients with temporomandibular disorder (TMD). (clinicaltrials.gov)
  • The report comes as national data shows that there was a 34% increase in overdose deaths caused by propranolol between 2012 and 2017, and that by 2016 nearly 4.7 million prescriptions were issued to patients annually. (pharmatimes.com)
  • Dr Stephen Drage, ICU consultant and HSIB's director of investigations said: "Propranolol is a powerful and safe drug, benefitting patients across the country. (pharmatimes.com)
  • Nilsson O, Melander A, Tegler L (1980) Effects and plasma levels of propranolol and metoprolol in hyperthyroid patients. (springer.com)
  • Several scientists across the world have reported similar results since then, testing propranolol on their own patients with angiosarcoma. (cancertutor.com)
  • Four patients with latent obstruction became asymptomatic on propranolol therapy. (bmj.com)
  • The 7 patients with resting obstruction who are still improved on propranolol have had relatively short periods of treatment (average 15 months), and none experienced the degree of improvement that occurred in the patients with latent obstruction. (bmj.com)
  • This study indicates that propranolol is most effective in patients with muscular subaortic stenosis who have latent obstruction. (bmj.com)
  • It is of limited value in patients with resting obstruction because the benefit of propranolol therapy in the majority of these patients is eventually overtaken by progression in the disease. (bmj.com)
  • Uptake of 14C-propranolol by the lungs during a single passage through the pulmonary circulation was measured in ten patients at cardiac catheterisation. (bmj.com)
  • Mean lung uptake of propranolol was 75% in seven patients who were not previously taking the drug and 33% in three patients who were taking it as regular oral treatment. (bmj.com)
  • In this 2011 Subspecialty Day presentation, he reviews the propranolol treatment strategy used at Indiana University and how to optimize safety in these young patients. (aao.org)
  • Patients received propranolol therapy for at least 3 months. (hindawi.com)
  • Here, we evaluated the efficacy of propranolol on proliferation IH in a clinical cohort including 578 patients. (dovepress.com)
  • For example, response rate to propranolol was 98.1% in patients younger than 2 months, compared with 93.3% in patients older than 2 months and younger than 8 months, and 73.7% in patients older than 8 months. (dovepress.com)
  • For patients exhibiting telangiectasia and chromatosis after propranolol treatment, administration of a 0.5% solution of timolol maleate or pulse dye laser is an effective therapeutic approach for complete involution. (dovepress.com)
  • Propranolol had failed to prevent inducibility of sustained ventricular tachycardia during previous programmed stimulation studies in three of the four patients, but it reproducibly suppressed drug-induced arrhythmias that appeared only after administration of the IC agents in each patient. (ahajournals.org)
  • Impact of Nicorandil on Renal Function in Patients With Acute Heart Failure and Pre-Existing Renal Dysfunction Masahito Shigekiyo, Kenji Harada, Ayumi Okada, Naho Terada.Propranolol is a sympatholytic non-selective beta blocker. (slipcamgirls.ml)
  • Propranolol 30 mg b.i.d. patients with one "non-kidney" organ failure but with serum creatinine ranging from 1.5 to 1.9 mg/dL and/or mild-to moderate-.We report the first use of propranolol with the aim of limiting the increase in chorioangioma volume and avoiding the associated complications. (slipcamgirls.ml)
  • We retrospectively reviewed the medical records of all patients who were prescribed propranolol in our Medical Surgical ICU from January 1, 2010, to December 31, 2013. (frontiersin.org)
  • Four double-blind, randomized, crossover studies were conducted in a total of 74 patients propranolol with mild or moderately day severe hypertension treated with Propranolol Hydrochloride Extended-Release Capsules, USP, 160 mg once daily or Propranolol 160 mg given either once daily or in two 80 mg doses. (dresdencodak.com)
  • Current guidelines recommend prophylactic treatment with propranolol or endoscopic band ligation (EBL) to prevent variceal bleeding in patients with medium or large varices. (bioportfolio.com)
  • This study is performed to compare the efficacy and safety of EBL, propranolol, and EBL combined with propranolol in patients with medium or large varices. (bioportfolio.com)
  • The addition of isosorbide mononitrate to propranolol treatment in patients with cirrhosis and portal hypertension caused a marked fall in portal pressure, a reduction in hepatic blood flow, cardiac output and mean arterial blood pressure, but no additional change in azygos blood flow. (wikipedia.org)
  • The additional effect of isosorbide mononitrate was especially evident in patients whose portal pressure was not reduced by propranolol. (wikipedia.org)
  • In most clinical settings, however, such as hypertension or angina where there is little correlation between plasma levels and clinical effect, Propranolol Hydrochloride Extended-Release Capsules, USP, have been therapeutically equivalent to the same mg dose of conventional Propranolol as assessed by 24-hour effects on blood pressure and on 24-hour exercise responses of heart rate, systolic pressure, and rate pressure product. (drugs.com)
  • Propranolol is not recommended for the treatment of hypertension by the Eighth Joint National Committee (JNC 8) because a higher rate of the primary composite outcome of cardiovascular death, myocardial infarction, or stroke compared to an angiotensin receptor blocker was noted in one study. (wikipedia.org)
  • Propranolol is used to treat tremors, angina (chest pain), hypertension (high blood pressure), heart rhythm disorders, and other heart or circulatory conditions. (cigna.com)
  • Propranolol is a widely used, non-selective β-adrenergic receptor antagonist with proven efficacy in the treatment of hypertension, in reducing mortality after myocardial infarction, in treatment of other cardiovascular disorders, and in migraine prophylaxis. (frontiersin.org)
  • To counter the harmful effects of stress hormones like adrenaline on memory, Pitman has been experimenting with propranolol, a drug commonly used to treat hypertension . (drugs-forum.com)
  • Propranolol is a Beta-Blocker used in the treatment of hypertension, cardiac arrhythmias, tremor and anxiety. (slipcamgirls.ml)
  • Propranolol is a medicine that is commonly used to treat high blood pressure (hypertension) and heart problems, but it can also be used to prevent migraines. (dokteronline.com)
  • At dosages greater than required for beta blockade, Propranolol also exerts a quinidine-like or anesthetic-like membrane action, which affects the cardiac action potential. (drugs.com)
  • Propranolol exerts its antiarrhythmic effects in concentrations associated with beta-adrenergic blockade, and this appears to be its principal antiarrhythmic mechanism of action. (drugs.com)
  • At plasma concentrations exceeding those required for β-adrenergic receptor inhibition, propranolol also exhibits anti-arrhythmic ("membrane stabilizing") effects that are not fully explained by β-blockade. (frontiersin.org)
  • Growth Attenuation of Cutaneous Angiosarcoma With Propranolol-Mediated β-Blockade. (cancertutor.com)
  • Control rats (n=5) received only water with their food, whereas beta-blockade was produced in another 5 rats by administering 100 mg/kg/day propranolol in their drinking water. (actapress.com)
  • Propranolol adrenergic blockade inhibits. (slipcamgirls.ml)
  • In angina pectoris, Propranolol generally reduces the oxygen requirement of the heart at any given level of effort by blocking the catecholamine-induced increases in the heart rate, systolic blood pressure, and the velocity and extent of myocardial contraction. (drugs.com)
  • The prize was awarded since Dr Black's propranolol was the first drug after many tens of years which was actually able to control the effects of having angina pectoris - a condition following a heart attack when the heart tissue gets worn and tired due to the original heart attack. (nomorepanic.co.uk)
  • Secondary: To determine if extended-release propranolol efficacy varies according to participants' catechol-O-methyltransferase (COMT) genetic diplotype. (clinicaltrials.gov)
  • Do not stop taking propranolol without talking to your doctor first. (medlineplus.gov)
  • ︉ The dosage of propranolol will depend on the condition being treated and will be personalized for each individual. (netdoctor.co.uk)
  • It has been observed that low dosage of propranolol during the active phase of labor can increase the uterine contractions and cause delivery and reduce the cesarean section significantly without causing maternal and no neonatal complications and cesarean rate. (magiran.com)
  • Propranolol er prices buy generic depakote cytotec 200mg abortion dosage cloridrato de propranolol generico generic propranolol er. (chrisroberson.net)
  • Administration of protein-rich foods increase the bioavailability of propranolol by about 50% with no change in time to peak concentration, plasma binding, half-life, or the amount of unchanged drug in the urine. (nih.gov)
  • Because of the variable bioavailability of propranolol, the dose should be individualized based on response. (rxlist.com)
  • These issues raise questions regarding the assumption that propranolol may have the capacity to exert effects on CNS development in young infants [ 8 ]. (hindawi.com)
  • Give propranolol solution at around the same time(s) every day. (medlineplus.gov)
  • Give propranolol exactly as directed. (medlineplus.gov)
  • You may give propranolol with or without food, but try to give it the same way each time. (childrensmn.org)
  • Correct dosage of cytotec for abortion buy propranolol online buy cheap propranolol online which is stronger 2mg xanax or 2mg klonopin xanax or zoloft for anxiety. (chrisroberson.net)
  • The generic Propranolol is manufactured by one company. (medindia.net)
  • Buy generic propranolol online is propranolol available over the counter what is the dosage for cytotec for abortion meclizine generic drug. (chrisroberson.net)
  • Propranolol is a lipophilic nonselective β -adrenergic receptor ( β -AR) blocker and has the ability to easily penetrate the blood-brain barrier [ 5 ]. (hindawi.com)
  • Elevated propranolol plasma concentrations, a longer mean elimination half-life (254 vs. 152 minutes), and decreased systemic clearance (8 vs. 13 mL/kg/min) have been observed in elderly subjects when compared to young subjects. (nih.gov)
  • Clinically, propranolol is administered as a racemic mixture with equal concentrations of R-(+)- and S-(−)-enantiomers. (frontiersin.org)
  • Both uptake and release of propranolol occur within minutes and are temperature dependent, being about 5 times faster at 37°C than at 20°C. The intracellular fluorescence lifetime of propranolol is generally shorter than the value of 9.8 ns determined in dilute neutral aqueous solution, and the difference is ascribed to concentration quenching. (hindawi.com)
  • Propranolol belongs to the class of drugs called adrenergics, i.e. drugs with a direct effect on the adrenalin uptake (I will explain the uptake mechanism below) in our body. (nomorepanic.co.uk)
  • Hepatic uptake of propranolol. (aspetjournals.org)
  • The second, slower phase of uptake was associated with metabolism of propranolol to other compounds and was temperature, oxygen and concentration dependent. (aspetjournals.org)
  • First pass uptake of 14C-propranolol by the lung. (bmj.com)
  • However, Hall and Carter have argued that many such objections are "based on wildly exaggerated and unrealistic scenarios that ignore the limited action of propranolol in affecting memory, underplay the debilitating impact that PTSD has on those who suffer from it, and fail to acknowledge the extent to which drugs like alcohol are already used for this purpose. (wikipedia.org)
  • Isolated rat livers were perfused with propranolol and other drugs in a simplified recirculation system without plasma proteins or erythrocytes. (aspetjournals.org)
  • This may alter the dose response relation for propranolol and a wide range of other drugs when given intravenously. (bmj.com)
  • M-mode echocardiograms and blood pressure were recorded before entry to the trial, twice during each week of treatment with metoprolol or propranolol, and daily for three days and on the seventh day after stopping the drugs. (bmj.com)
  • Secondly, she says, 'anyone who took that medicine could be in trouble in a legal case,' since defense lawyers may say that the victim was so unstable that she needed drugs to cope, or that the propranolol may have altered her memory about the assault. (drugs-forum.com)
  • Currently, propranolol is the first-line treatment for IHs due to its excellent efficacy [ 3 ]. (hindawi.com)
  • In addition, the efficacy and safety of the combination of EBL and propranolol is not still defined. (bioportfolio.com)