Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the µ-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys. The most common adverse reactions are nausea, dizziness, vomiting, and somnolence. Constipation is more common in use of the ER formulation. Precautions against concomitant use of central nervous system depressants, including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol, or use of tapentadol within 14 days of the cessation of monoamine oxidase inhibitors, are advised. The safety and efficacy have not been established for use during pregnancy, labor, and delivery, or for nursing mothers, pediatric patients less than 18 years of age, and cases of severe renal impairment and severe hepatic impairment. The major concerns for tapentadol are abuse, addiction, seeking behavior, withdrawal, and physical dependence. The presumed problem for use of tapentadol is to control the ratio of MOR agonist and NRI. In conclusion, tapentadol produces both nociceptive and neuropathic pain relief, but with worries about abuse and dependence.
Absorption ; Acute Pain ; Analgesics, Opioid ; Anesthetics, General ; Behavior, Addictive ; Birds* ; Central Nervous System Depressants ; Chronic Pain ; Constipation ; Dizziness ; Drug-Related Side Effects and Adverse Reactions ; Humans ; Hyperalgesia ; Hypnotics and Sedatives ; Kidney ; Monoamine Oxidase Inhibitors ; Mothers ; Nausea ; Neuralgia ; Nociceptive Pain ; Norepinephrine ; Nursing ; Phenothiazines ; Pregnancy ; Receptors, Adrenergic, alpha ; Receptors, Opioid, mu ; Vomiting

Nowadays in the field of plastic surgery, operations with no general anesthesia have been much increased, using daily surgery center. We used "Propofol TCI system" to control exact target concentration of conscious sedation and to reduce any systemic complication of the other local anesthetics. Twenty of ASA Class I or II patients were scheduled for elective surgery using Diprifusor(R) TCI system at 0.8-1.9 ug/ml target concentration. We estimated the proper target concentration, time of awakening, postoperative patient satisfaction and presence of postoperative amnesia. All the patients was satisfied except one patients who underwent nasal tip plasty. The target concentration of the conscious sedation varies with age and the type of operation but average concentration was 1.4-1.6 ug/ml. The average time of awakening, which we estimated by the time of eye opening was 2.6 minutes. Postoperative systemic complication and unusual vital sign were not present. We present here our satisfactory results using propofol infused by TCI(Target controlled infusion) system. This system is called 'Diprifusor(R)' and has a benefit of excellent sedative effect, low complication rate, safety, and rapid awakening time which enables the patient to return to his normal life cycle.
Amnesia ; Anesthesia, General ; Anesthesia, Intravenous* ; Anesthesia, Local* ; Anesthetics, Local ; Conscious Sedation ; Humans ; Hypnotics and Sedatives ; Life Cycle Stages ; Patient Satisfaction ; Propofol* ; Surgery, Plastic* ; Vital Signs

Preoyerative sedation of children is a difficult problem of great importance, for the psychic trauma comsequent to anticipation of surgery may be as great a hazard to the patient as his original disease. Until now, a number of sedatives have been used commonly for adequate sedation of pediatric patients, but, no method has been universally accepted. At our hospital fifty pediatric patients receiving general anesthesia for minor elective surgery were studied to evaluate the effect of ketamine hydrochloride as a preanesthetic agent. The results were as follows: 1) The onset of drag action was about, about 5min. 2) The induction of anesthesia and maintenances of operation was smooth, because a sedative effect was obtained without cardiovascular and respiratory depression. 3) With a small dosage of ketamine(2mg/kg), patients were free from apprehension. So, perioperative psychic trauma was preventible. 4) The two excitable patients were anesthetized by intravenous anesthetics with ease. 5) Mild complications, accurred but they were not significant.
Anesthesia ; Anesthesia, General ; Anesthetics, Intravenous ; Child* ; Humans ; Hypnotics and Sedatives ; Ketamine* ; Methods ; Respiratory Insufficiency

BACKGROUND: Lidocaine has been used for attenuating cardiovascular responses to endotracheal intubation and thought to have the sedative effect. The sedative effect of lidocaine has not been known well. The BIS (bispectral index) has been used an indicator of the sedative state and has been considered to be related to anesthetic agents and noxious stimulus. The purpose of this study is to evaluate sedative and cardiovascular effects of lidocaine during TCI (target controlled infusion) of propofol by monitoring BIS and hemodynamics. METHODS: Fifty ASA patient status 1 and 2, aged from 20 to 65 years patients (n = 50, 2 groups) undergoing elective surgeries with general anesthesia. These patients were randomly allocated to group C or L. Patients in Group L received 1.5 mg/kg injection and 40microgram/kg/min infusion of lidocaine. Patients in Group C received normal saline. The BIS, blood pressure and heart rate were mesasured before injection of drug, 1, 2 minute after injection of drug, just before intubation, 1, 2, 5 and 10 min after intubation. RESULTS: The BIS of group L more decreased than group C at 1, 2, 5 and 10 min after endotracheal intubation. The blood pressure and heart rate did not show any differences between two groups. CONCLUSIONS: Intravenous injection of lidocaine reduced BIS. Lidocaine had sedative effects under propofol target controlled infusion. But Cardiovascular variables of this study failed to show any differences between two groups (P < 0.05).
Anesthesia, General ; Anesthetics ; Blood Pressure ; Heart Rate ; Hemodynamics* ; Humans ; Hypnotics and Sedatives ; Injections, Intravenous* ; Intubation ; Intubation, Intratracheal ; Lidocaine* ; Propofol*

BACKGROUND: Althogh drug euption refers to a common dermatological condition, there are numerous holdbacks on the diagnosis. OBJECTIVE: This study atternpts to define the clinical features and causavite drug of the patients with drug eruptions, and to evalarate the diagnostic value of various skin tests. METHOD: 130 patients with drug eruptions were reviewed clinically. In 54 patients, intradermal test, patch test, and scratch patch test were performed using suspected drugs. Result : The exanthematous eruption(53.0%), fixed drug eruptior.(29.2%), and urticaria(6.2%) were the common types of the drug eruption. The common causative agenst of drug eruptions were antibiotics/antimicrobials, antipyretics/NSAIDs, and CNS depressants. 28 paitients out of the 54 patients on skin tests with suspected drugs had positive results in at least one slinest. CONCLUSION: In our study, we were able to obtain somewhat meaningfi 1 results based on data from the combination of various skin tests.
Central Nervous System Depressants ; Diagnosis ; Drug Eruptions* ; Humans ; Intradermal Tests ; Patch Tests ; Skin Tests* ; Skin*

BACKGROUND: Although drug eruption refers to a common dermatologieal condition, there are numerous setbacks in the diagnosis. In addition there are no annual average prevalence rates of drug eruptions according to time sequence in Korea. OBJECTIVE: This study attempts to detme the clinical features and causative drugs of drug eruptions, the diagnostic value of various skin tests and to evaluate the dome,stic annual average prevalence rate of drug eruptions according to time sequence. METHOD: 270 patients with drug eruptions were reviewed clinically. In 103 patients, intradennal, patch and scratch-patch tests were performed using suspected drugs. The annual average prevalence rate of drug eruptions was calculated from 10 different general hositals in Korea. RESULT: Exanthematous eruptions(49.3), fixed drug eruptions(30.1), and urticaria(10.0%) were the common types of drug eruptions. The common causative agents were antibiotics/antimicrobials, antipyretics(NSAIDs, and CNS depressants. 52 patients out of 103 had positive results after at least one skin test with suspected drugs. CONCLUSION: In our study, we were ahle to obtain somewhat meaningful results basnl on data from the combination of various skin tests. As a result, physicians need to prescrible drugs with care.
Central Nervous System Depressants ; Diagnosis ; Drug Eruptions* ; Humans ; Korea ; Prevalence ; Skin Tests* ; Skin*

BACKGROUND: Total intravenous anesthesia(TIVA) with various kinds of sedatives and synthetic analgesics has many advantages such as no air pollution, no hepatic or renal toxicity and good postoperative pain relief compared with inhalation anesthesia. METHODS: TIVA with fentanyl and propofol was applied to the 25 patients in ASA class I and II. The changes of hemodynamics, arterial blood gas, blood sugar level, hepatorenal function and complications were evaluated perioperatively. RESULTS: Systolic blood pressure and mean arterial pressure decreased after induction, but intraoperatively systolic blood pressure became preoperative value while mean arterial pressure increased compared with preoperative value. Heart rate increased after induction and intraoperatively. At recovery room there were no clinically significant changes in the data of arterial blood gas. The blood sugar level slightly increased during postoperative period. There were no clinically significant changes in hepatic or renal function test of postoperative 3rd day compared with preoperative one. The chief complications of TIVA during anesthesia were pain on injection site and slight movement, while nausea or vomiting, dizziness and urinary retention were the major complications at postoperative period. CONCLUSIONS: TIVA with fentanyl and propofol is considered to have good controllability and it can be applied as one of the general anesthesia methods in the case of contraindications to N2O and volatile anesthetics, but further study will be required to quantify the appropriate dosage of propofol or fentanyl to minimize perioperative hemodynamic change and respiratory depression.
Air Pollution ; Analgesics ; Anesthesia ; Anesthesia, General ; Anesthesia, Inhalation ; Anesthesia, Intravenous* ; Anesthetics ; Arterial Pressure ; Blood Glucose ; Blood Pressure ; Dizziness ; Fentanyl* ; Heart Rate ; Hemodynamics ; Humans ; Hypnotics and Sedatives ; Nausea ; Pain, Postoperative ; Postoperative Period ; Propofol* ; Recovery Room ; Respiratory Insufficiency ; Urinary Retention ; Vomiting

BACKGROUND: This bispectral index, which is used for intravenous anesthetics and inhalation anesthesia, is a scale of sedation and hypnotic effect, which is widely used in clinics. Atypical changes in BIS are expected due to increased cardiac output, decreased blood albumin concentrations and renal function in severe burn patients undergoing early escharectomy. The aim of this study was to compare BIS according to effected site concentrations of propofol during anesthetic induction using propofol TCI in severe burn and nonburn patients. METHODS: Forty patients were classified as twenty nonburn elective surgical patients (group 1) and twenty burn patients scheduled for escharectomy (group 2). For induction, a propofol TCI device incorporating a prefilled syringe was adjusted to a target concentration of 6mug/ml in flash mode. The bispectral index was checked before induction and at each effect site concentration of propofol (0.5mug/ml interval) until an effect site concentration of 4.5mug/ml. Other suspected contributory factors such as cardiac index, creatinine clearance and albumin were checked simultaneously. The unpaired t-test and repeated measures ANOVA were performed for the statistical analysis. RESULTS: Below an effect site concentration of propofol of 3mug/ml, no BIS difference was evident between group 1 and group 2. However, at 3.5mug/ml, group 1 was 41.1+/-13.5 and group 2 was 54.7+/-16.6 and at 4mug/ml, group 1 was 40.1+/-2.6 and group 2 was 50.1+/-13.1. Among the suspected contributing factors, cardiac index and albumin showed significant differences between groups 1 and 2 (cardiac index: 3.4+/-0.5 L/min/m2 vs 2.7+/-0.3 L/min/m2, albumin: 4.1+/-0.3 g/dl vs 2.6+/-0.3 g/dl, P<0.05). Creatinine clearance showed no significant difference between the groups. CONCLUSIONS: Severe burn patients who are expecting early escharectomy had higher BIS values than nonburn patients from an effect site concentration of propofol of 3.5mug/ml. This study suggest that cardiac index should be considered as a factor that influences propofol.
Anesthesia, Inhalation ; Anesthetics, Intravenous ; Burns* ; Cardiac Output ; Creatinine ; Humans ; Hypnotics and Sedatives ; Propofol* ; Syringes

Induction of general anesthesia with direct laryngoscopy and tracheal intubation is a routine procedure. However, it is accompanied by varying degree of sympathetic stimulation as reflected by significant hypertension, tachycardia, and arrhythmia. These transient hemodynamic responses are undesirable, especially in patients with cardiovascular or intracranial diseases. Many approaches have been tried to attenuate these potentially adverse circulatory responses (topical or i.v. lidocaine, deep anesthesia with inhalation anesthetics, opioids, adrenergic blockers, calcium channel blockers, sedatives, etc), and several trials reduced the hemodynamic effects. This study was done to examine blunting effect of verapamil, labetalol, and fentanyl on the adverse hemodynamic changes following direct laryngoscopy and tracheal intubation. Eighty patients, ASA Physical Status I II, scheduled for elective surgery, were selected randomly. These were divided into four groups. Group 1: Control (saline) (n = 20) Group 2: Verapamil 100 ug/kg (n = 20) Group 3: Labetalol 0.25 mg/kg (n = 20) Group 4: Fentanyl 3 ug/kg (n = 20) These were injected 3 minutes before induction with thiopental sodium (5mg/kg) and succinylcholine (1 mg/kg) i.v. in alI groups. Laryngoscopy and endotracheal intubation were performed 5 minutes after study drugs injection. After the completion of intubation, 50% nitrous oxide in oxygen and 1.5 Vol% halothane were inhaled. The blood pressure and heart rate were measured with automatic noninvasive blood pressure device and E.C.G monitoring every minutes for 10 minutes. The data were analyzed with Student's paired t-test within the groups and unpaired t-test between the groups. Results were considered statistically significant if p < 0.05. All study drugs, verapamil, labetalol, or fentanyl significantly blunted the increase in heart rate, arterial blood pressure, and rate pressure product caused by direct laryngoscopy and endotracheal intubation. There was no significant difference between verapamil and labetalol, but the blunting effects on hemodynamic changes were very significant in fentanyl group. So, verapamil, labetalol, and fentanyl may offer on important role in patients in whom an inaease in blood pressure, heart rate, and/or rate pressure product should be avoided during the endotracheal intubation.
Adrenergic Antagonists ; Analgesics, Opioid ; Anesthesia ; Anesthesia, General ; Anesthetics, Inhalation ; Arrhythmias, Cardiac ; Arterial Pressure ; Blood Pressure ; Calcium Channel Blockers ; Fentanyl* ; Halothane ; Heart Rate ; Hemodynamics* ; Humans ; Hypertension ; Hypnotics and Sedatives ; Intubation ; Intubation, Intratracheal* ; Labetalol* ; Laryngoscopy ; Lidocaine ; Nitrous Oxide ; Oxygen ; Succinylcholine ; Tachycardia ; Thiopental ; Verapamil*

Recently, intravenous sedatives and analgesics are being commonly used in children because of the clinical need for increasing the non-operating room anesthesia and intraoperative neurophysiologic monitoring during surgery and environmental problems. Administration methods (single bolus, intermittent bolus, or continuous infusion) vary according to the clinical request. Continuous intravenous anesthesia based on the weight is still the most commonly used method for administration of intravenous drugs in children. With the newly developed statistical method and medical devices, target controlled infusion of intravenous anesthetics has become possible in pediatric anesthesia, in spite of the difficulty in obtaining the specific pharmacokinetic model using pharmacokinetic parameters. Nowadays, a pharmacokinetic-pharmacodynamic model for complete effect-site target controlled infusion is available for use in children. Several drugs are used for pediatric sedation, such as analgesics or anesthetics such as opioids (remifentanil, sufentanil or alfentanil), neuromuscular blocking agents or sedatives (midazolam, dexmedetomidine). All these drugs have been used in continuous infusion via various methods including target controlled infusion. Many studies have been carried out by researchers to use target controlled infusion for safe and efficient treatment in children according to the increase in clinical demand. Various pharmacokinetic-pharmacodynamic models for commonly used intravenous drugs will be reviewed, with a focus on children in this small discussion.
Analgesics ; Analgesics, Opioid ; Anesthesia ; Anesthesia, Intravenous ; Anesthetics ; Anesthetics, Intravenous ; Child* ; Humans ; Hypnotics and Sedatives ; Intraoperative Neurophysiological Monitoring ; Methods ; Neuromuscular Blocking Agents ; Sufentanil