CN1329887A - Application of clonidine as analgesic - Google Patents
Application of clonidine as analgesic Download PDFInfo
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- CN1329887A CN1329887A CN 01113739 CN01113739A CN1329887A CN 1329887 A CN1329887 A CN 1329887A CN 01113739 CN01113739 CN 01113739 CN 01113739 A CN01113739 A CN 01113739A CN 1329887 A CN1329887 A CN 1329887A
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- clonidine
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Abstract
An application of clonidine as analgesis is disclosed. Said clonidine is originally used as antihypertensive medicine. When it is used as analgesic, it is peridurally or intrathecally applied individually or in conjuction with opium analgesic. Its advantages include sure analgesic effect, no suppression to respiration, no complications (nausea, emesis, itching and urinary retention), no addition, no carcinogenesis, and less by-effect.
Description
The present invention relates to a kind of analgesics, particularly depressor is used as a kind of analgesics.
Before the present invention made, pain was the content of medical research and therapeutic treatment as a big problem of medical science always.Ache in late cancer and intractable pain bring the human body and spiritual misery to the patient, make the patient lose people's dignity, lose the courage and the holding capacity that continue treatment.Therefore, analgesia as one independently subject be subjected to medical investigator and medical personnel's attention, also be subjected to the attention of medical product manufacturing enterprise simultaneously.At present, opioid drug is in analgesia, still occupy mastery reaction in the pain relieving, clinically by in whole body, the sheath or epidural give opioid drug, can produce analgesic activity by opiate receptor.But long-term prescription can cause such as the side effect of feeling sick, vomiting, constipation, respiration inhibition etc. can not tolerate, and main is to produce severe dependency and addiction, easily causes abuse, thereby causes the failure for the treatment of.So the pain of eradicating the patient is the problem that the medical research personnel need to be resolved hurrily.
Purpose of the present invention just is to overcome above-mentioned defective, works out a kind of new analgesia, analgesic medicine.
Technical scheme of the present invention: its major technique is characterised in that epidural or intrathecal drug delivery, dosage 2ug/kg/ days or more than.
Clonidine is as the application of analgesics, and its dose controlled was built in 2ug/kg/ days-12ug/kg/ days.
Advantage of the present invention and effect are by having significant analgesia role with clonidine in the canalis spinalis, apnea suppresses, feels sick, vomits, disturbs complication such as scabies and urine retention, can produce definite analgesic effect by epidural or intrathecal drug delivery, be better than morphine, side effect reduces, do not produce drug resistance, more do not have addiction.With the opiates administering drug combinations, the analgesic onset time is short, prolongs the analgesia effective time of opiates, reduces the consumption of opiates medicine, thereby reduces or avoid the generation of the untoward reaction of opiates medicine.
Clonidine is a synthetic imidazolidine derivatives of early 1960s, is α
2-receptor stimulating agent is widely used in hypertensive clinical treatment as central depressor.
We use α by discovering in whole body or the canalis spinalis
2-receptor stimulating agent has analgesic activity, can alleviate the behavior reaction of animal to pain stimulation, and only by spinal cord α
2Receptor-mediated, realize by activating spinal cord epinephrine descending inhibitory system.
The present invention just is being based on this discovery and is realizing.
Embodiment 1;
The analgesia of operation back, epidural administration, dosage is 2.5ug/kg/ days, in 2-12ug/kg/ days scopes, calculate with adult's body weight 60kg, the cloudy local anaesthetics that stagnates of perspective study canalis sacralis adds the analgesic effect 50 routine caudal block persons of improving that clonidine strengthens adult's anal operation of postop., all accept 1: 20 ten thousand adrenergic 2% lignocaine and 0.5% bupivacaine etc. capacity mixed liquor 30ml, wherein 25 examples add clonidine 150ug, and analgesic activity obviously prolongs.
Experiment showed, that analgesic effect is strengthened gradually, but has surpassed this scope, only prolongs the time of analgesic activity, no longer increases the intensity of analgesic activity in this 2-12ug/kg/ days dosage ranges, as can surpass this amount restriction for time expand.Intrathecal injection also produces same purpose and effect.
Embodiment 2:
Clonidine and opiates administering drug combinations, adopt patient's (pernicious cancer pain) controlled analgesia, epidural clonidine and morphine administering drug combinations, the clonidine dosage is 30ug/h, be no more than 40ug/h at most, have analgesic activity, compare with morphine with single, under same analgesic activity, can reduce the consumption of morphine effectively.
The general pharmacology test:
At pig epidural space injection clonidine 3ug/kg, do not influence the regional flow of spinal cord or any organ; Dosage is 10ug/kg when above, causes that the local vascular of breast, waist section spinal cord shrinks, and blood flow reduces 25-35%, and brain and cervical part of esophagus blood flow obviously do not change, and the kidney blood flow does not have significant change yet.
The effect of clonidine respiration inhibition is very slight.Behind the oral clonidine, tidal volume, respiratory frequency and minute ventilation volume no change.
In the administration of epidural Canis familiaris L., do not damage motor function, skin is the corresponding relation of dosage and effect to the thermostimulation tic response latency; Under high dose 160ug/h and 320ug/h, bradycardia, calmness, respiratory frequency minimizing appear.
In the administration of epidural clonidine sheep, do not bring high blood pressure down and the rhythm of the heart.
The quiet notes of rat 5ug/kg clonidine reduces heartbeat rule and arteriotony, dosage 11.3 ± 5.6vs2.1kg ± 0.9mg/kg that QRS changes for the first time.
Acute toxicity test:
Canis familiaris L. epidural injection dosage 4ml/ days, at 0 (normal saline), 80,200 and administration in 320ug/h28 days in, the concentration of clonidine reaches 1920ug/ml, dead animal do not occur.
Clonidine rat oral administration LD50 is 465mg/kg;
Clonidine mice oral administration LD50 is 206mg/kg.
Long term toxicity test:
The toxicity test of 28 days epidural administrations of clonidine Canis familiaris L. does not have death; All there be not to take place special the variation in normal saline group and clonidine group Canis familiaris L. body weight; Breathing rate, heart rate and blood pressure reduce, and produce calm; At three days infusion clonidines of beginning, the Canis familiaris L. systolic pressure reduces; At the 3rd day infusion clonidine of beginning, Canis familiaris L. mean systolic arterial pressure 87VS70mmHg, diastolic pressure 76VS57mmHg all reduces.
Hematology and serum chemistry evaluation are not different especially between clonidine group and matched group and clonidine group.
Matched group and clonidine group CSF change of blood sugar are 67.8 ± 4.3VS82 ± 7.8mg/dl.
Evidence does not have mutagenesis, and is no carcinogenic, has no drug resistance no addiction.
Claims (3)
1. clonidine is characterized in that epidural or intrathecal drug delivery as the application of analgesics, dosage 2ug/kg/ days or more than.
2. clonidine according to claim 1 is as the application of analgesics, it is characterized in that dose controlled was built in 2ug/kg/ days-12ug/kg/ days.
3. clonidine according to claim 1 and 2 is characterized in that and can unite use with opioid analgesic as the application of analgesics.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01113739 CN1329887A (en) | 2001-06-29 | 2001-06-29 | Application of clonidine as analgesic |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01113739 CN1329887A (en) | 2001-06-29 | 2001-06-29 | Application of clonidine as analgesic |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1329887A true CN1329887A (en) | 2002-01-09 |
Family
ID=4660446
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 01113739 Pending CN1329887A (en) | 2001-06-29 | 2001-06-29 | Application of clonidine as analgesic |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1329887A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108307631A (en) * | 2015-04-17 | 2018-07-20 | 莫诺帕医疗公司 | The clonidine and/or clonidine derivative of adverse side effect for preventing and/or treating chemotherapy |
| CN114796448A (en) * | 2022-05-06 | 2022-07-29 | 延安大学 | Application of clonidine and Gap26 in preparation of analgesic |
-
2001
- 2001-06-29 CN CN 01113739 patent/CN1329887A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108307631A (en) * | 2015-04-17 | 2018-07-20 | 莫诺帕医疗公司 | The clonidine and/or clonidine derivative of adverse side effect for preventing and/or treating chemotherapy |
| CN114796448A (en) * | 2022-05-06 | 2022-07-29 | 延安大学 | Application of clonidine and Gap26 in preparation of analgesic |
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