No abstract available.
Propanolamines

OBJECTIVETo study the stereoselective glucuronidation of carvedilol (CARV) by three Chinese liver microsomes.

METHODSThe metabolites of CARV were identified by a hydrolysis reaction with beta-glucuronidase and HPLC-MS/MS. The enzyme kinetics for CARV enantiomers glucuronidation was determined by a reversed phase-high pressure liquid chromatography (RP-HPLC) assay using (S)-propafenone as internal standard after precolumn derivatization with 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosylisothiocyanate.

RESULTSTwo CARV glucuronides were found in three Chinese liver microsomes incubated with CARV. The non-linear regression analysis showed that the values of K(m) and V(max) for (S)-CARV and (R)-CARV enantiomers were (118+/-44) micromol/L, (2 500+/-833) pmol/(min.mg protein) and (24+/-7) micromol/L, (953+/-399) pmol/(min.mg protein), respectively.

CONCLUSIONThese results suggested that there was a significant (P<0.05) stereoselective glucuronidation of CARV enantiomers in three Chinese liver microsomes, which might partly explain the enantioselective pharmacokinetics of CARV.

Carbazoles ; metabolism ; China ; Glucuronic Acid ; metabolism ; Glucuronides ; metabolism ; Microsomes, Liver ; metabolism ; Propanolamines ; metabolism ; Stereoisomerism

BACKGROUND: Rocuronium produces injection pain in 50-80% of treated patients. Therefore, a variety of pretreatments have been attempted to reduce this issue. We evaluated the efficacy of 3 different doses of magnesium on the rocuronium injection pain and following hemodynamic changes by laryngoscopy and tracheal intubation (LTI). METHODS: Two hundreds patients, ASA I and II, undergoing general anesthesia for elective surgery were randomly divided to 4 groups: group 1, 2, 3, 4 received saline 5 ml, magnesium 5, 10 and 20 mg/kg prior to 0.6 mg/kg of rocuronium, respectively. Then, group 1 only was treated with esmolol (20 mg) before LTI. Pain intensity with rocuronium injection was assessed using a four-point scale according to patient's movement. Cardiovascular responses at baseline, after induction, 1 minutes after LTI were determined. RESULTS: Compared to saline, 10 and 20 mg/kg of magnesium significantly reduced the incidence of overall movement after rocuronium injection (34% and 36% in group 3 and 4, respectively vs. 76% in the group 1) (P < 0.0001). Generalized movement was seen in 4% of patients in groups 3 and 4, respectively. Compared to baseline values, diastolic blood pressure (DBP) immediately after LTI significantly increased within groups 1 and 2 (P < 0.001), but not within groups 3 and 4. CONCLUSIONS: Magnesium (10 and 20 mg/kg) prior to rocuronium was effective in attenuating rocuronium associated injection pain and cardiovascular changes by LTI.
Androstanols ; Anesthesia, General ; Blood Pressure ; Hemodynamics ; Humans ; Incidence ; Intubation ; Intubation, Intratracheal ; Laryngoscopy ; Magnesium ; Magnesium Sulfate ; Propanolamines

BACKGROUND: The purpose of this study was to compare the effects of esmolol, esmolol and nicardipine or remifentanil on MBP, HR and recovery in gynecologic laparoscopic surgery. METHODS: Eighty patients scheduled for gynecologic laparoscopic surgery were randomly allocated to four groups: group C (control group, n = 20); group E (esmolol group, n = 20) received esmolol 1 mg/kg, followed by 5microgram/kg/min; group EN (esmolol + nicardipine group, n = 20) received esmolol 1 mg/kg and nicardipine 15microgram/kg, followed by an esmolol infusion 5microgram/kg/min; and group R (remifentanil group, n = 20) received remifentanil 1microgram/kg, followed by 0.05microgram/kg/min. The MBP and HR were measured at preinduction, after induction, at 1, 3, 5 min after intubation, before and after insufflation of CO2 and during surgical procedures. Recovery profiles and postoperative side effects were assessed. RESULTS: The change of MBP after intubation was significantly decreased in group EN. The change of HR after intubation and during surgical procedure were significantly decreased in group E and group R. Recovery profiles were significantly faster in all study groups compared with group C. CONCLUSIONS: The use of esmolol in combination with nicardipine was effective in preventing the increase of MBP after intubation, whereas esmolol or remifentanil had attenuated the acute change of HR to noxious stimuli. Also the use of esmolol, nicardipine or remifentanil as an adjuvant to sevoflurane-N2O anesthesia in gynecologic laparoscopic surgery had facilitated the recovery.
Anesthesia ; Blood Pressure ; Heart ; Heart Rate ; Humans ; Insufflation ; Intubation ; Laparoscopy ; Nicardipine ; Piperidines ; Propanolamines

Although the development of arrhythmias including atrial fibrillation (AF) is common under general anesthesia during surgery, the first episode of AF to occur during this period is rather uncommon. Moreover, most instances of AF are associated with old age, cardiopulmonary diseases as well as metabolic, endocrine, or genetic abnormalities. The occurrence of paroxysmal AF in the perioperative period in an adolescent without any underlying diseases or organic abnormalities has never been reported. Herein, we report a case of a 16-year-old adolescent whose paroxysmal AF was suspected before the anesthesia induction for strabismus surgery and diagnosed after anesthetic induction. Nevertheless, he was managed successfully with esmolol infusions during and after the surgery and thus recovered spontaneously.
Adolescent* ; Anesthesia ; Anesthesia, General ; Arrhythmias, Cardiac ; Atrial Fibrillation* ; Humans ; Perioperative Period* ; Propanolamines ; Strabismus

BACKGROUND: In this prospective, randomized, double-blind, placebo-controlled trial, we investigated the effect of a single dose of esmolol on the bispectral index (BIS) to endotracheal intubation during desflurane anesthesia. METHODS: After induction of anesthesia, 60 patients were mask-ventilated with desflurane (end-tidal 1 minimum alveolar concentration) for 5 min and then received either normal saline, esmolol 0.5 or 1 mg/kg, 1 min prior to intubation (control, esmolol-0.5 and esmolol-1 groups, n = 20/group). BIS, mean arterial pressure, and heart rate were measured prior to anesthesia induction and esmolol administration, immediately preceding intubation (time point 0), and every minute for 5 min after intubation (time point 1 to 5). At time point 0, 1 and 5, 5 ml of arterial blood was taken to measure plasma concentrations of norepinephrine and epinephrine. RESULTS: BIS increased significantly at 1 min after intubation when compared with pre-intubation values in all groups. Both mean arterial pressure and heart rate increased significantly 1 min after intubation when compared with preintubation values for all groups. Plasma epinephrine concentrations did not increase significantly after tracheal intubation in any of the groups. Norepinephrine increased at 1 min after intubation when compared with the preintubation values in the esmolol groups (P < 0.05). CONCLUSIONS: A single bolus of esmolol was unable to blunt the increase in BIS to endotracheal intubation during desflurane anesthesia.
Anesthesia ; Arterial Pressure ; Epinephrine ; Heart Rate ; Humans ; Intubation ; Intubation, Intratracheal ; Isoflurane ; Norepinephrine ; Plasma ; Propanolamines ; Prospective Studies

Pressure overload diseases such as valvular stenosis and systemic hypertension morphologically manifest in patients as cardiac concentric hypertrophy. Preventing cardiac remodeling due to increased pressure overload is important to reduce the morbidity and mortality. A recent clinical study has shown that carvedilol has beneficial effects on the survival rate of patients with heart failure. This may be due to the actions of carvedilol such as beta-adrenoceptor blockade and the alpha1-adrenergic receptor blockade effects. Therefore, we investigated whether carvedilol can reverse preexisting cardiac hypertrophy and we compared the effects of racemic carvedilol and the carvedilol enantiomers. Cardiac hypertrophy was induced in rats by suprarenal transverse abdominal aortic constriction (AC). Fifteen weeks after AC surgery, concentric hypertrophy was identified in the AC group by performing echocardiography. Low dose S- and SR-carvedilol (2 mg/kg/day), which were orally administered for three weeks, caused significant regression of the cardiac hypertrophy, and this most significantly occurred in the rats that received S-carvedilol. However, R-carvedilol did not reduce cardiac hypertrophy. Regression of cardiac hypertrophy by carvedilol was confirmed on the echocardiograms and electrocardiograms. These results suggest that carvedilol could reverse the development of leftventricular concentric hypertrophy that is induced by pressure overload. S-carvedilol is proposed to be superior to SR-and R-carvedilol as a beneficial treatment for cardiac hypertrophy.
Animals ; Carbazoles ; Cardiomegaly ; Constriction ; Constriction, Pathologic ; Echocardiography ; Electrocardiography ; Heart Failure ; Humans ; Hypertension ; Hypertrophy ; Propanolamines ; Rats ; Survival Rate

Esmolol is a cardioselective beta-blocker with a very rapid onset of action and a short half-life. Labetalol is a combined alpha- and beta-adrenoceptor blocking agent. It is a nonselective antagonist at beta-adrenoceptors and a competitive antagonist of postsynaptic alpha 1-adrenoceptors. A 51 year old female patient was transferred to the operating room for performing spinal fusion under general anesthesia. She had no operation and medication history. The initial heart rate was 150 beats/min. Despite administering several bolus injections of esmolol, the heart rate was not decreased to under 130 beats/min. But the heart rate was decreased to 100 beats/min after the administration of labetalol 5 mg and this rate was maintained without an additional injection. The vital signs were stable until the operation was finished and the patient recovered uneventfully in the recovery room. The postoperative laboratory findings revealed that she had hyperthyroidism. We report here on an anesthetic experience of effective labetalol treatment for esmolol-resistant tachycardia in a patient who was under general anesthesia.
Anesthesia, General ; Female ; Half-Life ; Heart Rate ; Humans ; Hyperthyroidism ; Labetalol ; Operating Rooms ; Propanolamines ; Recovery Room ; Spinal Fusion ; Tachycardia ; Vital Signs

A 48-year-old woman was incidentally found to have bilateral adrenal masses, 2.8 cm in diameter on the right, and 2.3 cm and 1.7 cm in diameter on the left, by abdominal computed tomography. The patient had a medical history of hypertension, which was not being controlled by carvedilol, at a dose of 25 mg daily. She presented with signs and symptoms that suggested Cushing Syndrome. We diagnosed adrenocorticotropic hormone (ACTH)-independent Cushing Syndrome based on the results of basal and dynamic hormone tests. Adrenal vein sampling (AVS) was performed to localize a functioning adrenal cortical mass. AVS results were consistent with hypersecretion of cortisol from both adrenal glands, with a cortisol lateralization ratio of 1.1. Upon bilateral laparoscopic adrenalectomy, bilateral ACTH-independent adrenal adenomas were found. The patient's signs and symptoms of Cushing Syndrome improved after surgery just as the blood pressure was normalized. After surgery, the patient was started on glucocorticoid and mineralocorticoid replacement therapy.
Adenoma ; Adrenal Glands ; Adrenalectomy ; Adrenocorticotropic Hormone ; Blood Pressure ; Carbazoles ; Cushing Syndrome ; Female ; Humans ; Hydrocortisone ; Hypertension ; Propanolamines ; Veins

A healthy 35-year-old man who was scheduled for closed reduction of nasal bone fracture developed atrial fibrillation during induction of general anesthesia after intravenous glycopyrrolate injection. During emergence of general anesthesia, atrial fibrillation was suddenly changed to paroxysmal supraventricular tachycardia with 200 beat per minute and lasted for about 10 seconds. Because blood pressure was stable, esmolol was used to reduce ventricular response. At recovery room, ventricular response reduction about 55 beat per minute was observed after intravenous injection of verapamil 5 mg. Thereafter, the rhythm was returned to normal sinus rhythm with bradycardia.
Anesthesia, General ; Atrial Fibrillation ; Blood Pressure ; Bradycardia ; Glycopyrrolate ; Injections, Intravenous ; Nasal Bone ; Propanolamines ; Recovery Room ; Tachycardia, Paroxysmal ; Tachycardia, Supraventricular ; Verapamil