Character; Role; letter
This product is a pale yellow to grayish white suspension. The liquid medicine is packed in a pressure-resistant aluminum bottle. When the button of the valve is pressed, the liquid medicine is sprayed out in mist.
Pharmacology and toxicology
1. Pharmacology
Budesonide is a glucocorticoid with high local anti-inflammatory effect.
Local anti-inflammatory effect
The exact mechanism of glucocorticoid in the treatment of asthma is still unclear. The anti-inflammatory effects of glucocorticoid, such as inhibiting the release of inflammatory mediators and immune response mediated by cytokines, may play an important role in the treatment of asthma. Compared with the affinity of hormone to glucocorticoid receptor, budesonide
The intrinsic vitality of prednisolone is about 15 times higher than that of prednisolone.
A clinical study comparing the efficacy of inhaled budesonide and oral budesonide on asthma confirmed that the efficacy of inhaled budesonide was significantly different from that of placebo, but there was no significant difference between oral budesonide and placebo. Therefore, the therapeutic effect of inhaled budesonide can only be released through its direct effect on respiratory tract.
Induction tests on animals and patients show that budesonide has anti-allergic and anti-inflammatory effects, and can alleviate bronchial obstruction caused by immediate and delayed allergic reactions.
Effect on the exacerbation of asthma
Studies have found that inhaling budesonide once or twice a day can effectively prevent the exacerbation of asthma in children and adults.
Effect on Exercise-induced Asthma
Inhalation of budesonide can effectively prevent exercise asthma.
Effect on airway responsiveness
In patients with hyperresponsiveness, budesonide can reduce the airway response to direct and indirect stimuli.
Effect on hypothalamus-pituitary-adrenal axis function
ACTH test showed that the effect of inhaled budesonide with recommended dose on adrenal function was significantly lower than that of 10mg prednisone. The daily dose for adults is as high as 1600ug.
Children's daily dose is as high as 800ug, which is used continuously for 3 months. No plasma cortisol level and its response to ACTH stimulation were found.
Changes in the meaning of bed. Up to 52 weeks of follow-up confirmed that HPA axis inhibition did not occur.
Effect on growth
Children inhale budesonide aerosol for 2 ~ 6 years, and the daily dose is as high as 600ug. Compared with non-steroid treatment, there is no evidence that this drug is harmful to children.
Growth has an impact.
2. Toxicology
Acute, subacute and long-term toxicity studies show that the systemic effects of budesonide, such as weight loss, atrophy of lymphatic tissue and adrenal cortex, are superior to other sugar skins.
Sex hormones are weak or equivalent to other glucocorticoid.
After six different experimental testing systems, budesonide has no mutagenic and mutagenic effects.
In the experiments of mice and rats, the oral test dose was as high as 200 and 50 ug/kg per day, respectively, to observe the carcinogenicity of budesonide. It turns out that it is.
Rats have no carcinogenic effect. A study pointed out that the incidence of glioma in male SD rats increased after taking budesonide, but the results showed that
Is considered uncertain. Further research in male SD and Fischer rats showed that the incidence of glioma was higher in budesonide treatment group.
The birth rate is very low, and there is no difference between glucocorticoid control group and blank control group. It has been concluded that budesonide treatment will not increase the brain of rats.
The incidence of glioma.
The existing clinical experience shows that there is no evidence that budesonide or other glucocorticoids can induce human glioma and primary hepatocellular carcinoma.
pharmacokinetics
absorb
The drug deposited in the lung after inhalation is about 10- 15% of the labeled amount.
After inhaling a single dose of budesonide lmg, the maximum blood concentration reached 2nmol/L after about 10 minutes. The systemic bioavailability of budesonide inhaled by aerosol is about 26% of the labeled amount, of which 2/5 comes from the oral part.
Be distributed
The apparent distribution volume of budesonide is about 3L/ kg. The average plasma protein binding rate is 85-90%.
biotransformation
The first-pass metabolism of budesonide through the liver is very high (about 90%), and the glucocorticoid activity of the metabolite is low. The activities of the main metabolites, 6β- hydroxybudesonide and 16α- hydroxyprednisolone, were lower than those of budesonide 1%. Budesonide is mainly metabolized by CYP3A, a subgroup of cytochrome P450.
eliminate
The metabolites of budesonide are excreted through the kidney in their original or combined forms. Budesonide was not detected in urine. The systemic clearance rate of budesonide is high, about 65438±0.2L/min, and the average plasma half-life of intravenous administration is about 2-3 hours.
Pharmacokinetic linearity
At the clinical therapeutic dose, the pharmacokinetics of budesonide is directly proportional to the dose.
indicate
It is used for patients with bronchial asthma and asthmatic chronic bronchitis who do not rely on glucocorticoid stimulation or glucocorticoid.
dosage
Inhale people. The dosage of budesonide aerosol should be individualized.
For patients with severe asthma and patients who stop or reduce the use of oral hormones, the dose of budesonide aerosol is:
Adults: 200- 1600 ug daily, divided into 2-4 times (200-800 ug daily for mild patients and 800- 1600 ug daily for severe patients).
Generally 200ug at a time, once in the morning and once in the evening, * * * 400 ug a day, once in severe cases, 4 times a day ***800ug.
Children aged 2-7 years: 200-400 ug daily, divided into 2-4 times.
Children over 7 years old: 200-800 ug daily, divided into 2-4 times.
Taking medicine twice a day (morning and evening) is usually enough. When severe asthma and asthma get worse, it is beneficial to take it 3-4 times a day. while
When the clinical effect is achieved, the maintenance dose should be gradually reduced to the lowest dose that can control the symptoms.
For patients who need to strengthen the therapeutic effect, the dose of budesonide aerosol can be increased, because the former is systemic compared with oral hormone therapy.
The incidence of side effects is very small.
Non-hormone dependent patients. Generally, the therapeutic effect is achieved within ten days. For patients with excessive bronchial mucus secretion, short-term (about
2 weeks) oral hormone therapy.
Hormone-dependent patients: when oral hormone is switched to budesonide aerosol, patients should be in a relatively stable period, and high-dose budesonide aerosol should
When combined with the previous oral hormone for about ten days, the oral hormone can be gradually reduced to the minimum dose (for example, prednisolone is reduced by 2.5mg or the same amount every month).
Budesonide aerosol can completely replace oral hormones in many cases.
counteraction
Clinical trials, literature reports and post-marketing experience show that the following adverse reactions may occur:
1. Mild throat inflammation, cough and hoarseness.
2. Candida infection in oropharynx
3. Immediate or delayed allergic reactions, including rash, contact dermatitis, urticaria, angioneurotic edema and bronchospasm.
4. Mental symptoms, such as nervousness, anxiety, depression and behavioral disorders.
Very few cases reported skin congestion after treatment with human glucocorticoid. In rare cases, bronchospasm will occur after taking human glucocorticoid.
Unknown system; Very few cases have symptoms and signs of systemic drug action after inhaling glucocorticoid, including adrenal hypofunction and slow growth rate.
This may be related to dosage, time, hormone combination, previous hormone use and personal sensitivity.
taboo
People who are allergic to any component of this product.
Matters needing attention
1. We should not try to relieve the acute attack of asthma quickly by inhaling budesonide. At this time, we still need to inhale short-acting bronchodilator. If the patient is found to be ineffective in using short-acting bronchodilators, or needs a higher inhalation dose than usual, he should see a doctor. At this time, we should consider strengthening anti-inflammatory treatment, such as inhaling higher dose of budesonide or taking oral glucocorticoid for a course of treatment.
2. Patients who transition from systemic administration to inhalation administration need special observation. During HPA inhibition, patients may have symptoms and signs of adrenal insufficiency in the case of injury, operation, infection (especially gastroenteritis) or serious loss of other electrolytes. At this time, the symptoms of asthma can be controlled by inhaling human budesonide, but the amount of glucocorticoid reaching the whole body after inhaling the recommended dose is lower than the normal physiological amount, and it cannot provide the necessary mineralocorticoid activity in these emergencies.
During drug withdrawal, some patients have nonspecific discomfort, such as myalgia and joint pain. If individual patients have fatigue, headache, nausea or vomiting, systemic glucocorticoid dysfunction should be suspected. For these patients, it is sometimes necessary to temporarily increase the oral hormone dose.
Inhalation therapy instead of systemic corticosteroids sometimes fails to control allergic diseases that require systemic medication, such as rhinitis and eczema. These allergic diseases require systemic antihistamines and/or topical dosage forms to control symptoms.
3. The decrease of liver function can affect the clearance of glucocorticoid, but the pharmacokinetics of budesonide in patients with liver cirrhosis after intravenous administration is similar to that of healthy volunteers.
The pharmacokinetics of absorbed budesonide is affected by liver function damage, which shows that the systemic utilization rate increases, but it is of great significance to pulmicort aerosol.
Slightly, because when administered by inhalation, the oral absorption part contributes very little to the systemic utilization rate.
4. Patients with pulmonary tuberculosis may need careful consideration when using this product.
5. The local and systemic effects of long-term use of pulmicort aerosol are not completely clear. Once asthma is controlled, the dose should be determined as the minimum effective dose. Doctors should closely monitor the growth and development of children who use glucocorticoid in any way, and weigh the advantages and disadvantages of hormone therapy and its benefits to asthma control and possible growth inhibition.
Medication for pregnant and lactating women
A large number of prospective epidemiological studies and worldwide post-marketing experience have not found that inhalation budesonide during pregnancy will have adverse effects on embryos and newborns.
Like other drugs, the potential harm of budesonide to the mother's mouth and fetus should be weighed during pregnancy. If glucocorticoids are needed, inhaled glucocorticoids can be used. Because compared with oral hormones, when the equivalent dose of anti-asthma is reached. The systemic side effects of inhaled corticosteroids are low.
Whether budesonide can enter human breast milk is unknown.
Children's medication
Children under 2 years old should use it with caution or not.
Medication for elderly patients
With adults.
drug interaction
At present, there is no report on the clinical interaction between budesonide and other drugs for asthma.
As a strong inhibitor of cytochrome P450 CYP 3A, the main metabolic enzyme of corticosteroid metabolism, ketoconazole can increase the systemic exposure of budesonide. At the recommended dose, cimetidine has a slight effect on the pharmacokinetics of oral budesonide, but it has no obvious clinical significance.
excessive
symptom
In most inert cases, occasional overdose will not produce any obvious symptoms, but it will reduce the plasma cortisol level and increase the number and percentage of neutrophils in the blood circulation. The number and percentage of lymphocytes and eosinophils will decrease simultaneously. Habitual overdose can cause adrenal cortex hyperfunction and hypothalamic-pituitary-adrenal suppression.
treat cordially
Stop budesonide or reduce the dose. But the recovery of hypothalamus-pituitary-adrenal axis is a slow process, so the disappearance of these symptoms is also a slow process.
Specification (1) 5ml: 20ml, 200 ug// spray (2)10ml:10mg.50ug/spray.
The storage valve is facing the tripod, protected from light, sealed and stored in a cool place.
Packaging aluminum bottles with metering valves.
50ug// spray: 20O spray/bottle, 1 bottle/box.
200 ug// spray: 10O spray/bottle, 1 bottle/box.
Valid for 2 years 5 Hold your breath as long as possible, preferably 10 second, and then exhale.
Approval number (1) 5ml: 20mg
200ug/ spray: National Medicine Zhunzi H200304 10 \
(2) 10m: 10mg
50ug/ spray: national medicine standard word H20Q304 1 1
Production enterprise
Enterprise name: AstraZeneca Pharmaceutical Co., Ltd.
Address: No.2 Huangshan Road, Wuxi, Jiangsu
Postal code: 2 14028
Quality Tel: 05 10-522000
Fax number: 05 10-5228520
Medical consultation telephone: 02 1-52564555
Fax number: 02 1-52984474
Website:. exist
Usage of budesonide aerosol
Contains budesonide 50 micrograms/spray, 200 micrograms/spray.
Please read the detailed instructions carefully and take the medicine according to the following steps:
1. Remove the protective cover and shake it sufficiently to make its contents fully mixed.
2. Double lips wrap the interface end.
3. Breathe out calmly through the interface.
4. While inhaling, press the aerosol bottle to spray the medicine once, and slowly and deeply inhale people through the mouth.
5. Hold your breath for as long as possible, preferably 10 second, and then exhale.
If further medication is needed, shake the aerosol again and repeat the above steps 2-5.
Rinse your mouth after each medication.
Important matters:
Budesonide acts on the lungs, so the drug release should start at the same time as you inhale, so that the drug can enter the depths of the human lungs as much as possible. Patients can
Ensure that the atomized aerosol liquid does not leak from the mouth or container through the mirror.
Precautions:
Follow the doctor's advice and don't exceed the prescribed amount. Sometimes in order to achieve the best results, it takes two weeks of formal treatment. If you find that the efficacy is obviously reduced, please
See a doctor.
Children; Children should take medicine under the guidance of doctors and supervision of adults.
Warning: This product is a sealed pressure vessel. Do not damage the valve. Avoid direct sunlight and high temperature above 40℃.
Cleaning: regularly remove the aerosol bottle, clean the plastic shell (at least once a week), and wash it with warm water instead of hot water, and add weak cleaning agent if necessary.
After drying, put on a spray bottle.
The patient can put the medicine bottle into a bowl of clear water to detect the remaining amount of liquid medicine.
Be sure to carry a new bottle of budesonide aerosol with you.