Theophylline can reduce the tension of smooth muscle and dilate the respiratory tract; It can promote the release of endogenous epinephrine and norepinephrine, relax airway smooth muscle; Inhibit the release of calcium ions from the endoplasmic reticulum of smooth muscle, reduce the concentration of intracellular calcium ions and produce respiratory tract dilation. Theophylline has a strong relaxation effect on smooth muscle but is not as good as β Receptor agonists.
Theophylline in the treatment of asthma and COPD
Theophylline is a commonly used drug for the treatment of lung diseases (such as chronic obstructive pulmonary disease, bronchial asthma, etc.) in the elderly, but the effective dose of theophylline is quite close to the toxic dose, and its bioavailability and internal clearance rate vary greatly among individuals, which is vulnerable to various diseases and other drugs. However, the elderly have different degrees of organ dysfunction and weakened internal environment regulation, which makes them more prone to adverse drug reactions. Therefore, theophylline is a very special product; For example, in the treatment of theophylline sustained-release tablets with the same dose, some people are in stable condition, while others are not getting better. The reason may be that there is no personalized customization.
So how do determine the individualized dosage?
As for the problems involved in the above example, you only need to monitor the serum concentration of theophylline. Its principle is to analyze and measure the concentration of drugs in the blood under the guidance of the principle of pharmacokinetics, so as to evaluate the curative effect or determine the administration plan, so as to individualize the administration plan. In general, the concentration of drugs in the blood can indirectly reflect the concentration of drugs in the receptor part, thus indirectly reflecting the intensity of pharmacological effects. When you use it again, the effect will definitely stand up and see the shadow.
Is it necessary to monitor as long as you use drugs?
A. Blood drug concentration should be regularly detected when using drugs by intravenous route. Blood samples were taken after the peak blood concentration reached a steady-state 2-4 hours after administration, and then monitored every 4 hours.
B. Oral theophylline does not always require routine monitoring of serum concentrations, but serum theophylline concentrations should be measured in the following cases: (1) at any time when signs or symptoms of theophylline toxicity appear; (2) For patients with persistent wheezing symptoms, consider that the blood drug concentration may be lower than the treatment concentration and plan to increase the dose before; (3) After administration, from the initial treatment to the adjustment to the final dose; (4) When the treatment plan needs to be changed due to new diseases, deterioration of chronic diseases or possible changes in theophylline clearance rate; (5) The metabolic pathway of theophylline in infants under 1-year-old is immature, so special attention should be paid to the dose and serum theophylline concentration (recommended level B).
So is it necessary to monitor the blood concentration of all drugs in life? The answer is No. If the safety of drugs is high and the efficacy dose is individualized, there is no need for monitoring.
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