JPS62111925A - Analgesic and sedative in emergence recovery from anesthesia - Google Patents

Abstract

PURPOSE:The titled sedative containing a water-soluble derivative of acetylsalicylic acid as an active ingredient. CONSTITUTION:A analgesic and sedative in emergence recovery from anesthesia containing a water-soluble derivative of acetylsalicylic acid, e.g. acetylsalicylic acid DL-lysine salt, as an active ingredient. The above-mentioned analgesic and sedative is administered 10-60min before emergence recovery in performing operation while in systemic anesthesia. The dosage form is preferably injection and the above-mentioned active ingredient is dissolved in distilled water for injection, physiological saline solution, etc., in 5-20w/v%, preferably 10w/v% concentration and prepared in use. The dose thereof is 100-1,000mg/time expressed in terms of the acetylsalicylic acid and intravenously administered. EFFECT:The degree of patient's rest is excellent without acting on the consciousness in emergence recovery. Since the analgesic and sedative is injection, administration is very readily carried out without inducing gastrointestinal injury as in the case of solution for internal use.

Description

DETAILED DESCRIPTION OF THE INVENTION (a) Field of Application The present invention relates to a sedative analgesic agent for awakening from anesthesia, which contains a water-soluble derivative of acetyl monolithylic acid as an active ingredient.

(T:1) Conventional technology When the stimulus from a surgical procedure is perceived as a sensation, it excites the sympathetic nerves, causing contraction of smooth muscles such as blood vessels and bronchi, and reflex tension of skeletal muscles.

As a result, upon awakening from anesthesia, a sudden rise in blood pressure, an increase in pulse rate, and suppression of breathing occur.

In this way, postoperative pain is caused by a combination of surgical factors and general anxiety and tension about the surgery, and occurs for several hours after awakening from anesthesia.

GOE [enflurane +
It has been noticed that this can be a problem in the case of laughing gas (nitrous oxide) decaxygen anesthesia and GOF (halogenated laughing gas + oxygen) anesthesia.

(c) Problems to be Solved by the Invention Although sedatives such as penxicin, indomethacin, and ibuprofen have been used to suppress such postoperative pain, satisfactory results have not always been obtained.

Therefore, the present inventors investigated various drugs to suppress this postoperative pain, and found that by appropriately using a water-soluble derivative of acetyl monolithylic acid before the onset of pain in patients,
The present invention was completed after discovering that it is effective in analgesing postoperative pain and calming excitement during awakening.

(d) Means for solving the problem Widely known water-soluble derivatives of acetylsalicylic acid are used in the present invention, but preferably acetylsalicylic acid and an alkaline earth metal (such as NaSK) are used.
, alkali metals (Ca, Mg, etc.) formed into salts with basic substances are used.

Among these, basic amino acids are particularly preferred as the basic substance. These include, for example, lysine, arginine, in particular Dl,,-lysine.

As the water-soluble derivative of acetylsalicylic acid of the present invention, acetylsalicylic acid L) L~lysine salt is particularly preferably used. Furthermore, this acetylsalicylic acid-1)
L-1) The method for preparing gin salt is described in JP-A-56-101.
The method described in Specification No. 10 etc. may be used.

For example, the preparation of the present invention is preferably an injection, in which a water-soluble derivative of acetylsalicylic acid is mixed with distilled water for injection,
It is prepared by dissolving it in physiological saline or other aqueous solvents before use.

Of course, there are additives that are added to regular injections, such as:
It is preferable to include a buffer, a solubilizing agent, an isotonic stabilizer, a preservative, and the like.

In the formulation of the present invention, the water-soluble derivative of acetylsalicylic acid is usually 5 to 20 w/v%, preferably IO
It is prepared into an aqueous solution of about W/V%.

The preparation of the present invention may optionally contain other medicinal ingredients in addition to the water-soluble derivative of acetylsalicylic acid.

The preparation of the present invention may be produced in accordance with known methods.

The preparation of the present invention is applicable to sedating postoperative pain and sedating symptoms during awakening.

The formulations of the invention are typically administered intravenously.

The dosage depends on the degree of anesthesia, age and weight of the patient,
It may be selected appropriately depending on gender, condition, etc., but usually 1.
100-100% as acetylsalicylic acid per serving
0 mg is used.

The administration may be performed from the time of induction of anesthesia to before awakening (preferably from 10 to 60 minutes before awakening).

(e) Effects of the present invention When the preparation of the present invention is used, the patient's level of rest is very good without affecting consciousness during awakening.

Therefore, it was found to be very effective in alleviating pain in patients immediately after surgery.

Furthermore, since it is an injection, it is extremely easy to administer and does not cause gastrointestinal disorders as is known with oral preparations.

Thus, the preparation of the present invention is clinically useful as an analgesic and sedative for post-operative pain.

(f) Clinical Examples Although clinical examples are given to explain the present invention in detail, the present invention is not limited by these in any way.

Clinical example A patient (male, age 26, weight 65 kg) undergoing orthopedic surgery was given 0 astropine as a premedication 60 minutes before surgery.
．． 5 mg of hydroxyzine and 50 mg of hydroxyzine were intramuscularly injected. At the time of induction of anesthesia, after intravenously injecting 200 mg of thiopencour and 50 mg of suxasame 1-nium chloride, GOE (enflurane + laughing gas decaoxygen) [laughing gas 4β/min, oxygen 2β/min, maintaining enflurane concentration 1-2%] was used. Inhalation anesthesia was started, and the surgery was performed as scheduled. Thirty minutes before the end of anesthesia, a vial of venopyrine (acetylsalicylic acid - D L-lysine salt manufactured by Midori Juji Co., Ltd.) (498 mg as acetylsalicylic acid) was injected intravenously.The patient's reactions were normal and he did not complain of pain upon awakening. The patient's rest level was also good.After that, the patient was interviewed every 30 minutes, but there was no particular change.

Also, no serious side effects were observed.

Formulation example Acetylsalicylic acid 900mg -DL-Lysine salt Color inhibitor Aminoacetic acid 100mg Stabilizer Chloride 50mg (anhydride) Total 1050mg Active ingredient Acetylsalicylic acid -DL -IJjinj
fffi90[]mg is 498m acetylsalicylic acid
g and 402 mg of DL, -lysine.

When used, it was dissolved in distilled water for injection IQmI2 to prepare an intravenous injection.

Patent applicant: Midori Juji Procedures In 1
F'tan December 26, 1985 Director-General of the Special Consideration Agency Tono 1, Incident! 1 Indication of Showa 6 (Special IF Application No. 2/190232, Title of invention Anesthesia Awakening 1 [, 'I Analgesic Sedatives 3, Amendment 4 Ministry of Affairs 1'1 Relationship with: Patent 1 Applicant Name: Co., Ltd. Ne1 Midorijuji 6 Number of inventions increased by the amendment: 07 Target of the amendment: Column 8 of “Detailed Description of the Invention” for specifications Contents of the amendment: Mei IBIF 3, page 6, No. 10- Line 11, [The patient's reaction is normal and 1 when awake. 1 When the patient is awake, the patient's reaction is i"
Always correct.

Claims (2)

[Claims] (1) During surgery under general anesthesia, 10 to 10 minutes before awakening
An analgesic and sedative for awakening from anesthesia, characterized in that the analgesic and sedative for awakening from anesthesia, which is administered at 60 minutes, is a water-soluble derivative of acetylsalicylic acid. (2) An analgesic and sedative for awakening from anesthesia, characterized in that the water-soluble derivative of acetylsalicylic acid is acetylsalicylic acid-DL-lysine salt.