Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To evaluate the therapeutic value of various antihypotensive agents we investigated amezinium (AMZ; CAS 30578-37-1), dihydroergotamine (DHE; CAS 511-12-6), midodrine (MDD; CAS 42794-76-3), and oxilofrine (OXF; CAS 365-26-4) in volunteers during passive orthostasis in a randomized double-blind study against placebo (PCB). Blood pressure, heart rate, and circulating catecholamines were determined before and after i.v. injections of the mentioned agents before and during 10 min of passive orthostasis. Echocardiographic and venous plethysmographic data were obtained during resting before and after the administration of the drugs. Resting heart rate decreased after injection of PCB, AMZ, DHE, and MDD. During tilting no significant changes in heart rate could be observed. Blood pressure remained unchanged at rest and during orthostasis after all agents injected. DHE and MDD lowered circulating noradrenaline. Echocardiographic parameters were changed after administration of AMZ (increase in stroke volume index (SVI) and ejection fraction (EF)), MDD (increase in enddiastolic volume index and SVI), and OXF (increase in SVI, EF, and cardiac index). The venous capacity of the lower left leg was only significantly decreased after injection of DHE, indicating an increased venous tone of the leg veins. The observed changes in sympathetic and cardiovascular parameters are in agreement with their sympathomimetic actions and allow a differential therapeutic classification: DHE and MDD are suitable agents for patients with sympathotonic orthostatic reaction; if asympathotonic orthostatic reaction occurs MDD, AMX and OXF should be recommended to those patients.
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PMID:Cardiovascular parameters and catecholamines in volunteers during passive orthostasis. Influence of antihypotensive drugs. 153 Jun 77

The beta 2-sympathomimetic drug fenoterol (fenoterol hydrobromide, CAS 1944-12-3, Partusisten) is routinely used to inhibit uterine contractions (tocolysis). Investigations of plasma concentrations of those receiving i.v. or oral tocolysis often show different results, both within particular groups of pregnant women and in comparison with non-pregnant persons. The aim of this study was to determine the pharmacokinetics of fenoterol in pregnant women, an important factor which so far had not been known. Four healthy pregnant women with similar weight and gestational age and all with premature labor were administered a continuous intravenous infusion of 4 micrograms fenoterol/min. During and up to 24 hours after the end of the infusion, venous blood samples were taken in order to determine the fenoterol plasma concentrations by radioimmunoassay. From a steady state concentration (css) of 2242 +/- 391 pg/ml (x +/- S.E.), a non-linear two-phased plasma elimination was seen with half-lives t1/2 of 11.40 min and 4.87 h. The area under the plasma concentration-time curve (AUC0-12h) was 6.27 ng/ml x h. The total clearance (Cltot) was 114.8 l/h. These data are nearly the same as the data already known for healthy non-pregnant (male) volunteers. The deviations which are seen in the plasma concentrations in pregnant women in comparison to non-pregnant persons during or after continuous i.v. infusion can therefore not be caused by differences in the pharmacokinetics. Other factors, however, such as body weight and/or gestational age, might influence the results.
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PMID:Pharmacokinetics of fenoterol in pregnant women. 771 Apr 46

Atenolol (CAS 29122-68-7) and metoprolol (CAS 37350-58-6) are beta 1-selective adrenoceptor antagonists without intrinsic sympathomimetic activity. beta-Receptor blockers influence carbohydrate- and lipid metabolism. Liver is a central organ of these processes. The metabolic fate of a single oral atenolol and metoprolol dose and their actions on carbohydrate- and lipid parameters have been investigated. Healthy male rats received a dose reducing heart beat/min by 25% (atenolol: 6 mg/kg; metoprolol: 10 mg/kg). About 9% of atenolol is metabolized by cytochrome P-450 (P-450). P-450-dependent functions (aminopyrine-N-demethylase, hexobarbital biotransformation time) were not inhibited. Serum bilirubin was normal. Triglyceride (TG), total cholesterol and HDL-cholesterol levels of the plasma were not affected. Transient blood glucose increase was measured returning to initial value at 120 min. Metoprolol is metabolized by hepatic monooxygenases. P-450-dependent functions were inhibited correlating to the lowered P-450-content of the microsomes. High TG level and decreased HDL-cholesterol content were measured. Blood glucose was significantly high. The liposoluble metroprolol affected the hepatic functions more than the hydrophilic atenolol. The monitoring of blood glucose during beta-receptor antagonist treatment may be suggested.
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PMID:Metabolic actions of a single atenolol and metoprolol dose. 784 28

The aim of this study was to compare the decongestant properties and tolerability of the sympathomimetic xylometazoline hydrochloride 0.1% (CAS 1218-35-5, XMZ) and an oral formulation of cetirizine hydrochloride 5 mg and pseudoephedrine hydrochloride 120 mg (CAS 83881-51-0 and 90-82-4, CTZ/PSE; Cirrus). Thirty-six asymptomatic patients suffering from perennial allergic rhinitis from house dust mite were randomized to this open two-period crossover study. Patients received the study medications for four days each. In each period, treatments were taken twice a day. On day 1 in each period, immediately after the first dose of medication, patients were challenged with Dermatophagoides pteronyssinus extract 1 in the Vienna Challenge Chamber for 5 h. Primary efficacy parameters were nasal congestion evaluated by digital analysis of nasal cavity photographs and nasal airflow. Furthermore amounts of nasal secretions, nasal and ocular symptoms were recorded. In addition, 5 independent Ear-Nose-Throat specialists also assessed nasal cavity photographs. Statistical analyses were conducted at the 5% level of significance. Digital analysis of the nasal cavity photographs as well as nasal airflow measurements did not differentiate XMZ from CTZ/PSE. Ratings of the photographs of the nasal cavity emphasized the rapid onset of XMZ. No clinically relevant adverse events were recorded. This rapid onset of action but short-lived effect of topical xylometazoline 0.1% should be balanced against the consistent and prolonged effect of systemic cetirizine/pseudoephedrine combination in the treatment of perennial allergic rhinitis as no significant differences between these 2 medications were noted regarding their decongestant properties. With the exception of nasal obstruction, all subjective symptoms as well as the global condition were significantly better under CTZ/PSE. Amounts of nasal secretions during these sessions were significantly lower with CTZ/PSE.
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PMID:Efficacy and safety of an oral formulation of cetirizine and prolonged-release pseudoephedrine versus xylometazoline nasal spray in nasal congestion. 1176 92

Ritodrine hydrochloride ((R,S)-4-hydroxy-alpha-[1-[2-((4-hydroxyphenyl)ethyl]amino)ethyl]benzenemethanol, CAS 26652-09-5) is a direct-acting sympathomimetic agent with a predominant beta-adrenergic activity and a selective action on beta2-receptors. A clinical trial was carried out to investigate the pharmacokinetics, pharmacodynamics and safety of ritodrine hydrochloride administered at the doses of 10, 20 and 30 mg p.o. and 10 mg by i. m. route. A four-way randomised crossover design was adopted on 12 healthy female volunteers with a wash-out of at least 14 days. Concentrations of ritodrine and of the pool of ritodrine in plasma and concentrations of the pool of ritodrine in urine of volunteers were bioassayed with tandem mass spectrometry. The following pharmacokinetic parameters were calculated, using the non-compartmental model: Cmax, AUC0-t, AUC0-INF, t1/2, Vd/f, and Aet after each administration. The distribution volume of ritodrine proved to be about 3 times higher than that of the pool of ritodrine after i. m. injection, confirming the good permeability of ritodrine that massively enters tissue compartments. Statistical analyses of pharmacokinetic parameters ascertained that the p. o. absorption of ritodrine hydrochloride was linearly related with the doses administered in the 10-30 mg range. The pharmacodynamic parameters evaluated complied with the mechanism of action of this drug.
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PMID:Pharmacokinetics and pharmacodynamics of ritodrine hydrochloride administered orally and intramuscularly to female healthy volunteers. 2086 8