Method for preanaesthetic medication preceding gynaecological surgeries under general anaesthesia

FIELD: medicine.

SUBSTANCE: preanaesthetic medication preceding gynaecological surgeries under general anaesthesia is ensured by prescribing diazepam 10mg, nefopam 10mg and ketoprofen 100mg intramuscularly 30-40 min before the surgery.

EFFECT: method enables reaching the sedative and analgesic effect of the preanaesthetic medication by the complementary action of preparations with no undesired side effects, requiring no time consumption and expensive equipment.

3 tbl, 2 ex

 

The invention relates to medicine, namely to anesthesiology and resuscitation, and can be used for sedation before surgical gynecological procedures performed under General anesthesia.

The known method premedication before operative gynaecological procedures performed under General anesthesia, based on the parenteral administration of sedatives, providing a state of emotional calm the patient, and drugs for the prevention of postoperative pain syndrome ("pre-emptive analgesia"). To this end usually apply certain benzodiazepine drugs, antipsychotics, opiates/opioids, and antihistamines and anticholinergic remedies, non-steroid anti-inflammatory drugs (NSAIDs) ["Anesthesiology and reanimatology". A guide for physicians. Edited by Professor Y. S. would like. - SPb, "ELBI-SPb, 2004. - 720 p. (p. 226-229).]. This method is adopted for the prototype.

The disadvantage of this method is the occurrence of some undesirable side effects, inherent to these drugs. So, opiates/opioids often cause orthostatic effects, nausea and vomiting, as well as excessively deep sedation, especially in elderly and debilitated patients, depression of the respiratory center. Certain benzodiazepine drugs can slow awakening bollyholly General anesthesia. Antihistamine and anticholinergic drugs cause dry mouth, anticholinergic drugs tachycardia.

The technical result of the invention is to provide a method that allows to achieve a sedative and analgesic effects without sedation unwanted side effects inherent in the above listed drugs.

Said technical result is achieved in that in the method of a premedication before operative gynaecological procedures performed under General anesthesia, including the appointment of diazepam in the dose of 10 mg intramuscularly for 30-40 minutes before the surgery, according to the invention it is also prescribed nefopam dose of 10 mg and Ketoprofen 100 mg.

Nefopam hydrochloride (Acupan®; LaboratoryBiocodex, France) is a new analgesic drug, registered in Russia in 2011 (Register of medicines: LP-000181), which belongs to the group of non-opioid analgesics Central mechanism of action. Nefopam is a non-opioid benzoxazolinone Central analgesic action, as well as providing antihyperalgesic and anticholinergic effects [N. Delage Median effective dose (ED 50) of nefopam and ketoprofen in postoperative patients: a study of interaction using sequential analysis and isobolographic analysis // Anesthesiology. - 2005. - Vol.102. - P. 1211-1216; Girard P, Coppe M-C, Verniers D, et al. Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception Pharmacol Res. - 2006. - V. 54. - P. 195-202]. Unlike opioid analgesics it does not cause respiratory depression and does not inhibit peristalsis. In addition to nefopam, which affects the Central nervous system, Ketoprofen has a local effect in the inflammation. The combination of nefopam and Ketoprofen can be useful in multimodal analgesia, since their mechanisms of action are complementary.

The combination of drugs of nefopam and Ketoprofen was used for postoperative analgesia, that is, in cases where the patient feels pain, and proactively, as part of the sedation to prevent pain - such use is not known. In premedication nefopam is not included for fear of his antiholinergicescoe action.

The proposed method is based on the results of clinical studies. Analyzed 23 cases of laparoscopic gynecological procedures without removal of the uterus (laparoscopic cystectomy, tubektomiya, diagnosis of infertility, treatment of endometriosis, myomectomy). The 1st group consisted of 11 patients who received as part of the premedication with diazepam (10 mg) in combination with Ketoprofen (100 mg) intramuscularly. the 2nd group consisted of 12 patients who the same premedication were supplemented with nefopam (20 mg) intramuscularly. For anthropometric data, as well as duration of the operation idesam drugs for General anesthesia group were identical (table.1).

Table 1
Anthropometric data of the examined patients (M±SD)
Indicatorgroup 1 (n=11)group 2 (n=12)
Age, years32,4±4,632,6±3,0
Height, cm167,5±3,7165,3±6,2
Weight, kg59,4±13,560,6±11,7
The duration of surgery, min55,5±23,663,8±23,8
The duration of anesthesia, min70,9±22,076,3±25,2

All patients underwent General combined anesthesia with tracheal intubation and mechanical ventilation. Induction was performed with propofol, anesthesia - inhalation of nitrous oxide with oxygen and sevoflurane. Intraoperative analgesia was provided by a fractional administration of fentanyl. Postoperative syndrome was evaluated by the dynamics of index visual analog scale (VAS) after 0.5, 1, 2, 3, and 24 h after Opera�AI. In this case the patient indicated the level of severity of pain on a 10-point scale (from 0 - no pain, 10 maximum pain). Also take into account the need to apply (at the request of the patient) pain relief through the introduction of NSAIDs and narcotic analgesic tramadol.

As shown by the analysis of the data received analgesia in the group of patients who had not used the nefopam, it took four patients, including one patient with the use of tramadol. At the same time, the patients who received Ketoprofen with nefopam did not need anesthesia in the 1st postoperative day. Despite the rejection of additional analgesia in this group of patients the level of pain in YOUR throughout the postoperative period was significantly lower than in the control group (tab.2).

Table 2
Anthropometric data of the examined patients (M±SD)
Index YOURgroup 1 (n=11)group 2 (n=12)
YOUR 0.5 h3,8±2,3*2,9±1,2
YOUR 1 hour 2,7±1,91,8±0,6
YOUR to 3 h1,6±0,41,3±0,5
YOUR 24 hours0,5±0,2*0±0

Concerns about possible antiholinergicescoe of action of nefopam, manifested by tachycardia and various autonomic responses, was not confirmed. Patients of the 2nd group, indeed, the heart rate was slightly higher than in patients of the 1st group, but this has not given them the subjective discomfort (table.3).

Table 3
Heart rate at various stages of the study (M±SD)
HRgroup 1 (n=11)group 2 (n=12)
On the table92,0±14,0of 103.9±17,9
Induction95,7±9,2to 105.3±11,0
Intubation90,2±13,299,8±7,1
Start operation 90,3±10,392,5±7,9

In connection with the resulting effect of premedication on the table atropine was added in seven patients of the 1st group and only three patients of the 2nd group.

In addition, postoperative shivering is a frequent and rather unpleasant complication of the postoperative period - developed, despite preventive measures, six patients of the 1st group. In contrast, among patients receiving nefopam, this unwelcome phenomenon was registered in only one case.

The obtained data are important because at the present time, postoperative analgesia is relevant and not resolved before the end of the problem in modern surgery: about 35% of patients after elective and emergency surgery tolerate postoperative pain.

Thus, the study confirmed that the use of nefopam with Ketoprofen in the composition of paramedical before laparoscopic gynaecological interventions is effective in the prevention of postoperative pain. Wherein the nefopam and NSAIDs provide preemptive analgesia, which is manifested by relief of postoperative pain and sedative effect of nefopam creates the psycho-emotional peace of the patient before surgery.

Sososososososo as follows.

For 12 h to operative gynecological interventions performed under General anesthesia, the patient is prescribed phenazepam dose of 1 mg and famotidine at a dose of 20 mg orally. As sedation for 30-40 minutes before surgery intramuscularly administered diazepam in the dose of 10 mg, Ketoprofen 100 mg and nefopam at a dose of 20 mg in separate syringes.

The method is confirmed by the following clinical examples.

Example 1. Patient M., 27 years old, height 162 cm and weight 56 kg, was admitted for surgical treatment with a diagnosis of adhesive disease pelvic and abdominal organs. Paraovarian cyst on the left. Underlying medical condition: iron deficiency anemia is mild. Chronic pyelonephritis (without exacerbation). The risk for ASA amounted to II/2. Produced: laparoscopy, lysis of adhesions, left hand salpingoophoritis, cystectomy left, hysteroscopy, endometrial biopsy.

Conducted General combined anesthesia with tracheal intubation and artificial ventilation of the lungs. Surgery and anesthesia lasted 50 min. For 12 hours before surgery prescribed oral phenazepam dose of 1 mg and famotidine at a dose of 20 mg.

As premedication 30 min before surgery intramuscularly was administered diazepam in the dose of 10 mg, Ketoprofen 100 mg and nefopam at a dose of 20 mg in accordance with the proposed method.

Induction of anesthesia OSU�actulaly bolus intravenous injection of propofol (150 mg) and fentanyl in a dose of 0.2 mg (intravenously), and diplegia - rocuronium bromide at a dose of 35 mg. Maintenance of anesthesia was provided by inhalation of sevoflurane (1.5%) and bolus administration of fentanyl 0.1 mg.

Mechanical ventilation was performed respirator Drager Fabius Tiro-mode control of the volume. Tidal volume was 420 ml, and respiratory rate is 12 to 1 minute based on indicators of capnography (EtCO2=35-37 mm Hg.St.).

Intraoperative monitoring included noninvasive blood pressure measurements (every 5 min), monitoring heart rate, plethysmographically saturation of blood oxygen, temperature, electrocardiography. Objective monitoring of neuromuscular conduction was carried out in the mode of TOF-stimulation with the device CARESCAPEB650 at all stages of the operation. To avoid episodes of inadequate nociceptive protection in the intraoperative period used computerized method of processing and evaluating the adequacy of anesthesia, including neuromonitoring based on entropy and surgical plethysmographic index (SPI). This technique is implemented in the CARESCAPE monitor V (General Electric Company).

To prevent hypothermia used a warming mattress "Aquaterm" and fueled infusion solutions.

In the postoperative period, the pain level scale) amounted to 2 points after 0.5 h after operation, 1 point in 1 � after surgery further - 0 points. Additional analgesia was required. In addition, the patient had no postoperative muscle tremors. Side effects, which could be associated with the use of nefopam. After 3 h, the patient was transferred from ward postoperative follow-up to the General ward. Health in the perioperative period, the patient was rated as "comfortable".

Example 2. Patient B., 32 years old, height 166 cm, weight 79 kg, was admitted for surgical treatment with a diagnosis of Primary infertility. The lack of ovarian function. Comorbidity: biliary dyskinesia, chronic gastritis (without exacerbation). The risk for ASA amounted to II/2. Produced: laparoscopy, ovarian biopsy, hysteroscopy, endometrial biopsy.

Conducted General combined anesthesia with tracheal intubation and artificial ventilation of the lungs. Surgery and anesthesia lasted 35 min. For 12 hours before surgery prescribed oral phenazepam dose of 1 mg and famotidine at a dose of 20 mg.

As sedation for 40 min before surgery intramuscularly was administered diazepam in the dose of 10 mg, Ketoprofen 100 mg and nefopam at a dose of 20 mg in accordance with the proposed method.

Induction of anesthesia was carried out by bolus intravenous injection of propofol (160 mg) and fentanyl in a dose of 0.2 mg (intravenous, and diplegia - rocuronium bromide at a dose of 40 mg. Maintenance of anesthesia was provided by inhalation of sevoflurane (1.5%) and bolus administration of fentanyl 0.1 mg.

Mechanical ventilation, intraoperative monitoring and prevention of hypothermia was performed in the same way as in example 1.

In the postoperative period, the pain level scale) amounted to 2 points after 0.5 h after operation, 1 point after 1 h after operation, 1 point after 3 h after surgery in the future - 0 points. Additional analgesia was required. After 2 h the patient was transferred from ward postoperative follow-up to the General ward. Health in the perioperative period, the patient also rated as "comfortable".

The proposed method of sedation allows you to achieve sedation sedation, and also the effect of "pre-emptive analgesia" without unwanted side effects, does not require time consuming, expensive equipment.

Method premedication before operative gynaecological procedures performed under General anesthesia, including the appointment of diazepam in the dose of 10 mg intramuscularly for 30-40 minutes before the surgery, characterized in that it further prescribed nefopam dose of 10 mg and Ketoprofen 100 mg.



 

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3 cl, 3 tbl, 2 dwg

FIELD: medicine.

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3 ex

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3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to anaesthesiology, and may be used as an anaesthesia care of a surgical intervention for carotid endaterectomy or internal carotid artery resection after pathological deformation thereof. That is ensured by general anaesthesia in a combination with deep and superficial cervical plexus blockade. Pre-medication is used the day before the operation and on the operative day in the morning. Diazepam is introduced intramuscularly 30 minutes before the operation in a combination with phentanyl; the introduction is followed by ECG monitoring and heart rate count, plethysmography with arterial blood saturation, non-invasive blood pressure measurement and neuromonitring according to a bispectral index or entropy. Catheterisation of patient's peripheral or central vein is followed by an infusion therapy, an ionotropic therapy, a cardiotropic therapy, peripheral resistance maintenance. If heart rate is no more than 80 beats per minute, the anaesthesia is induced to reach an anaesthetic depth according to the bispectral index or entropy within 40-60 units. Analgesia is provided by the intravenous introduction of 0.005% phentanyl; myoplegia is ensured by the intravenous introduction of a myorelaxant. After tracheal intubation, the patient is transferred to forced volumentic artificial pulmonary ventilation with the CO2 level within 35-45 mm Hg according to capnography. The anaesthesia is maintained by supplying an inhalation anaesthetic to the steam level of 0.8-1.0 MAK 0.8-0.9 litre of the air and oxygen flow containing 50% oxygen with controlling the inhalation anaesthetic volume by the level of the anaesthetic depth according to the bispectral index or entropy. That is followed by deep cervical plexus blockade. A tubercle of the VI cervical vertebra (a carotid tubercle) and a mastoid process are localised; thereafter a line connecting the above reference points is drawn on skin. The second line is drawn 1 cm below the first one in parallel. To verify an injection point of a local anaesthetic, the spines of IV, III, II cervical vertebras being at 1.5 cm from each other are palpated, and the reference point is the VI cervical vertebra. The needle is inserted perpendicularly to the skin and slightly in the caudal direction to reach the spines. The anaesthetic is introduced in a dose of 5-7 ml in each point C4, C3, C2. Another 5-7 ml of the anaesthetic is introduced in a point found in an apex of the mastoid process. The superficial cervical plexus blockade requires introducing he fan-shaped introduction of the anaesthetic solution in a dose of 15 ml in a point found in the middle of a lateral crus of the nodding muscle under the above muscle, 4-5 ml in each direction from the same point; the first and following injections are performed at a depth of a usual intramuscular needle perpendicularly to nodding muscle.

EFFECT: method provides the adequate and safe anaesthesia ensured by avoiding linear blood velocity reduction in the medial cerebral artery during the surgical intervention, preventing intracranial pressure increase, reducing cerebral perfusion pressure in a combination with providing adequate protection against surgical invasion with maintaining stroke volume and arterial pressure.

4 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to a heterocyclic compound of formula and to its pharmaceutically acceptable salts, stereoisomers and isomers, wherein T: N, U: N, X: CR3 and Y: N; or T: CR6, U: CR4, X: CR3 and Y: N; or T: CR6, U: N, X: NR3 and Y: C; or T: O, U: N, X: CR3 and Y: C; or T: NR6, U: N, X: CR3 and Y: C; and R1, R2 and R5: H, heteroaryl substituted by 1-2 substitutes; or T: CR6, U: N, X: CR3 and Y: N; or T: N, U: CR4, X: CR3 and Y: N; and R1 and R2: H, heteroaryl substituted by 1-2 substitutes; R5: heteroaryl substituted by 1-2 substitutes; R3: H, bridging (C7-C10)cycloalkyl; (C1-C8)alkyl optionally substituted by 1 substitute; (C3-C10)cycloalkyl optionally substituted by 1 substitute; (C6-C8)cycloalkenyl substituted by two (C1-C6)alkyl; (C6)aryl optionally substituted by 1-2 substitutes; heteroaryl optionally substituted by (C1-C6)alkyl; heterocyclyl optionally substituted by (C1-C6)alkyl or heteroaryl; or R3: -A-D-E-G, wherein: A: a bond or (C1-C6)alkylene; D : (C1-C2)alkylene optionally substituted by (C1-C6)alkyl, bridging (C6-C10)cycloalkylene optionally substituted by (C1-C6)alkyl, (C3-C10)cycloalkylene optionally substituted by 1-2 substitutes, (C4-C6)cycloalkenylene optionally substituted by (C1-C6)alkyl, (C6)arylene, heteroarylene or heterocyclylene optionally substituted by one (C1-C6)alkyl; E: a bond, -Re-, -Re-C(O)-Re-, -Re-C(O)O-Re-, -Re-O-Re-, -Re-S(O)2-Re-, -Re-N(Ra)-Re-, -Re-N(Ra)C(O)-Re-, -Re-C(O)N(Ra)Re-, -Re-N(Ra)C(O)ORe- or -Re-N(Ra)S(O)2-Re-; wherein in each case, E is bound to either a carbon atom, or a nitrogen atom in D; G: H, -N(Ra)(Rb), halogen, -ORa, S(O)2Ra, -CN, -C(O)N(Ra)(Rb), -N(Ra)C(O)Rb, -C(O)Ra, -CF3, N(Ra)S(O)2Rb, -(C1-C6)alkyl optionally substituted by 1-3 substitutes; -(C3-C6)cycloalkyl optionally substituted by CN; -heteroaryl optionally substituted by 1-2 halogens, CN, -C(O)NH2 or -CF3; -heterocyclyl optionally substituted by 1-5 substitutes, -(C6-C10)aryl optionally substituted by 1-3 substitutes; wherein in a fragment containing -N(Ra)(Rb), nitrogen, Ra and Rb can form a ring so that -N(Ra)(Rb) represents (C3-C6)heterocyclyl optionally substituted by 1 substitute, wherein said (C3-C6)heterocyclyl is bound through nitrogen; R4 and R6: H, (C1-C4)alkyl optionally substituted by -OH, -COOH; (C3-C8)cycloalkyl, phenyl, optionally substituted by -SO2CH3 or -NHSO2CH3, halogen or -J-L-M-Q; wherein: J: (C2-C6)alkenylene; L: a bond; M: a bond; Q: -C(O)ORa; Ra and Rb: H, (C1-C4)alkyl optionally substituted by cyano, -CF3 or cyclopropane; (C6)aryl optionally substituted by halogen or -O(C1-C4)alkyl; and Re: a bond, (C1-C4)alkylene or (C3)cycloalkylene. Besides, the invention refers to specific compounds, a pharmaceutical composition based on the compound of formula I, using the compound of formula I for treating and using the compounds of formulas 2-6

for preparing the compound of formula I.

EFFECT: prepared are the new compounds effective in treating a condition mediated by Jak1, Jak3 or Syk protein kinase activity.

51 cl, 34 tbl, 44 ex

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