What Is Butorphanol Tartrate?

Butorphanol tartrate, a major metabolite, excites K-opioid peptide receptors, and has dual effects on agonism and antagonism on U-receptors. It mainly interacts with these receptors in the central nervous system (CNS) to exert its pharmacological effects including analgesic effects indirectly. In addition to the analgesic effects, the effects on the CNS include reducing the spontaneous breathing of the respiratory system, cough, excitement and vomiting center, dilation, and sedation. Its effect may be achieved through non-CNS action mechanisms. Such as changing the resistance and capacitance of the heart blood vessels (nerves), bronchomotor tension, gastrointestinal secretion, motor muscle activity and bladder sphincter activity.

Butorphin tartrate

Butorphanol tartrate, a major metabolite, excites K-opioid peptide receptors, and has dual effects on agonism and antagonism on U-receptors. It mainly interacts with these receptors in the central nervous system (CNS) to exert its pharmacological effects including analgesic effects indirectly. In addition to the analgesic effects, the effects on the CNS include reducing the spontaneous breathing of the respiratory system, cough, excitement and vomiting center, dilation, and sedation. Its effect may be achieved through non-CNS action mechanisms. Such as changing the resistance and capacitance of the heart blood vessels (nerves), bronchomotor tension, gastrointestinal secretion, motor muscle activity and bladder sphincter activity.

Chinese name

Butorphin tartrate injection

Foreign name

Butorphanol Tartrate Injection

Product name

Noyan

Main ingredients

Butorphin tartrate

Drug Name

[Common name]: Butorphin tartrate injection

[Pinyin]: Jiushisuan Butuofeinuo Zhusheye

[Main ingredients] The main ingredients of this product are: Butorphanol tartrate, its chemical name is: L-(-17) -cyclobutylmethyl-3,14-dihydroxy codedranin D-(-)-tartaric acid (1 : 1) Salt.

[Type] central analgesics

Chemical Structure:

[Molecular formula]: C21H29NO2 · C4H6O6

[Molecular weight]: 477.56

[Properties] This product is a colorless clear liquid

[Specifications] 1ml: 1mg

[Packing] Brown vial, 5 bottles / box.

The analgesic effect of this product is generally intravenous injection for several minutes, and the effect of intramuscular injection for 10-15 minutes begins. Intravenous injection, intramuscular injection reaches a peak in 30-60 minutes, and the maintenance time is 3-4 hours, which is equivalent to morphine, meperidine and pentazocine.

This product can be absorbed quickly by intramuscular injection, and reach the peak plasma concentration in 20-40 minutes. The serum protein binding rate is about 80%, and it has a concentration-dependent relationship in a concentration range of not more than 7ng / ml. This product can pass through the blood-brain barrier and placental barrier, can enter human milk, is mainly metabolized in the liver, and the main metabolite is hydroxylated butorphinol. The creatinine clearance of patients with renal dysfunction was <30 ml / min, the half-life was extended by about 10.5 hours, and the body fluid elimination rate was 150 L / H. 70% -80% of the drug is eliminated by urine, and only 15% is eliminated by feces.

It is used to treat various cancerous pains and pains after surgery.

The intramuscular injection dose is 1-2 mg, if necessary, it can be repeated every 3-4 hours. There is no sufficient clinical data to recommend a single dose of more than 4 mg. Or as directed by your doctor.

Mainly doze, dizziness, nausea and / or vomiting.

Occurrence rate is 1% or more, considering reports of adverse reactions that may be related to butorphanol tartrate:

Whole body: weakness, headache, heat.

Cardiovascular system: vasodilation, palpitations.

Digestive system: anorexia, constipation, dry mouth, stomach pain.

Nervous system: anxiety, confusion, euphoria, floating, insomnia, nervousness, paresthesia, tremor.

Respiratory system: bronchitis, cough, dyspnea, epistaxis, nasal congestion, nasal irritation, pharyngitis, rhinitis, sinusitis, sinus congestion, upper respiratory tract infection.

Skin: sweaty / cold, itchy.

Special sensations: blurred vision, ear pain, tinnitus, and abnormal taste.

Incidence rates below 1% consider reports of adverse reactions that may be related to butorphanol tartamate.

Cardiovascular system: hypotension, syncope.

Nervous system: different dreams, anxiety, hallucinations, hostility, symptoms of drug withdrawal.

Skin: Rash / Wind.

Urinary system: dysuria.

[Contraindications] 1. Those who are allergic to this product or other ingredients in this product are prohibited.

2. Due to the antagonistic characteristics of opioids, this product should not be used in patients who rely on narcotine.

3. Patients younger than 18 years are disabled.

1. It should be used with caution in patients who repeatedly use narcotic analgesics and who are resistant to opioids.

2. Patients with brain damage and elevated intracranial pressure should be used with caution or not.

3. The initial dose interval of patients with liver and kidney disease should be extended to 6-8 hours until the response is very good. The subsequent dose is adjusted according to the patient's response instead of fixed administration according to the dosing schedule.

4. Use with caution in patients with myocardial infarction, ventricular dysfunction, and coronary insufficiency. When hypertension develops, the drug should be stopped immediately.

5. This product can cause respiratory depression, especially for patients taking CNS drugs at the same time or suffering from CNS disease or respiratory defects, use with caution.

6. It is forbidden to drink alcohol while taking this product.

The short-term physical dependence potential of rodents after giving this product is lower than that of analgesia after morphine, but it has been reported in recent years that long-term, frequent and large-scale use of butorphin tartrate in animals or humans can also cause physical dependence and abuse.

Medication for pregnant and lactating women

Pregnancy Type C: Studies in mice, rats, and rabbits during reproduction have shown no potential teratogenicity with tube formation using butorphino. However, when rats were administered subcutaneously at 1 mg / kg (5.9 mg / m2) of butorphanol during pregnancy, stillbirth was more frequent than that of the control group. The oral dose for rabbits during pregnancy was 30 mg / kg (5.1 mg / kg). m2) and 60mg / kg, showing a high incidence of failure after implantation. Women who have not taken butorphinol in human pregnancy for 37 weeks have adequate and closely controlled studies, so it is best not to take medications. Women in pregnancy can only use butorphanol when the potential benefits outweigh the potential risks.

Breastfeeding: When breastfeeding women are given intravenous butorphanol injection, butorphanol testing in breast milk shows that a small amount of butorphanol may be clinically irrelevant to the baby (used 4 times a day by the mother, each time 2mg, 4ug / L during milk excretion). The advantages and disadvantages of lactating women should be weighed.

Medication for children

The effectiveness and safety of butorphanol use in people younger than 18 years have not been proven, so it is prohibited to use butorphino in people younger than 18 years.

Medication for elderly patients

It is recommended that when using butorphanol in elderly patients, the initial dose is halved, and the interval period is twice as long as that of normal people. The subsequent dose and interval are determined according to the specific response of the patient.

1. While using butorphinol, the use of central nervous system inhibitors [such as alcohol, barbiturates (hypnotic sedatives), diazepam and antihistamines] will lead to a stronger inhibitory effect on the central nervous system. When combined with these drugs that enhance the opioid effect, the amount of butorphino should be the minimum effective dose, and the subsequent dose should be reduced as much as possible.

2. It is unclear whether the combination with drugs that affect liver metabolism (such as cimetidine, erythromycin, theophylline, etc.) affects the effect of butorphino, but the physician has carefully reduced the initial dose and prolonged Intermittent dosing.

3. Whether the use of butorphino and MAO (monoamine oxidase) blocking drugs interact with each other has not been confirmed.

Clinical Appearance: The clinical symptoms of any series of overdose of synthetic narcotic drugs are mostly hypoventilation, cardiovascular insufficiency and / or coma, and a few overdose symptoms are fatal consequences caused by simultaneous consumption of several other drugs. Leno was not sure.

Treatment: Excessive measures for butorphanol use include adequate ventilation, peripheral perfusion and normal body temperature, and keeping the airway open. Patients are continuously observed by continuously measuring their mental state, responsiveness, and vital signs. Continuous monitoring with a pulse oximeter and tracheal intubation if the patient is unconscious. Proper venous access should be maintained to facilitate the treatment of hypotension caused by vasodilators.

In special methods, opioids (any synthetic anesthetic antagonist) can be used, such as naloxone hydrochloride. Since the tolerance to buprenorphine exceeds the tolerance to naloxone hydrochloride, naloxone hydrochloride should be repeated.