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Another name: dioxy dimethylpurine; 1, 3-dimethyl-3, 7-dihydro-1h-purine-2, 6-diketone; 1, 3-dimethyl xanthine; Hydrated tea base; The tea base; Theophylline /1, 3-dimethyl xanthine; 1, 3-dimethylxanthine
1, 3-dimethyl -3, 7-dihydro-1h-purine-2,6-dione; 1, 3 - dimethyl - xanthin; 1 h - Purine - 2, 6 - dione, 3, 7 - dihydro - 1, 3 - dimethyl -; 3, 7 - dihydro - 1, 3 - dimethyl - 1 h - purine - 6 - dione. 3 h) - dione, 1, 3 - dimethyl - purine - 6 (1 h, 6 - dione, 3, 7 - dihydro - 1, 3 - dimethyl - 1 h - Purine - 2; accurbron; Acet-theocin
The CAS number: 58-55-9
Moleclar formula: C7H8N4O2
Molecular weight: 180.16
EINECS no. : 200-385-7
Danger Category code :22-39/23/24/25-23/24/25-11-36/37/38
Safety Instructions :7-16-36/37-45-36-26
Dangerous Goods Transport Number :UN 2811 6.1/PG 3
The nature of the
Melting point: 271-273 °C
Flash: 11 ° C
Storage conditions: 2-8°C
Solubility: 0.1M HCl: soluble
Water solubility :8.3 g/L (20 º C)
Appearance: White crystalline or crystalline powder, odorless, bitter taste.
Solubility: Dissolved in water (1:120), ethanol (1:18), chloroform (1:86), hydroxide lye, ammonia, dilute hydrochloric acid and dilute nitric acid, slightly dissolved in ether at room temperature.
The main purpose
Theophylline is a methylpurine drug. It can strengthen heart, diuresis, dilate coronary artery, relax bronchial smooth muscle and excite central meridian system. Mainly used in the treatment of bronchial asthma, emphysema, bronchitis, cardiac dyspnea.
Theophylline drug toxicology
The pharmacological action of theophylline depends on blood concentration. However, the safe range of its effective blood concentration is very narrow. For example, when the blood concentration is 10-20 μg/ml, the bronchial dilation can cause toxic reactions if the blood concentration exceeds 20μg/ml. Oral absorption is not stable, its clearance in vivo influencing factors, and individual differences are large, blood concentration is difficult to control, so easy to occur poisoning. Excessive dosage at one time, or the speed of intravenous injection is too fast, or the accumulation of repeated drug use, there is the possibility of overdose poisoning. And sometimes the symptoms of poisoning are not easy to be found, or even misdiagnosed as the original disease itself; And therefore mistakenly further increase theophylline dosage, resulting in serious poisoning. Infection can affect theophylline metabolism and increase blood concentrations to toxic levels. Other factors that can increase theophylline levels are liver disease, congestive heart failure, respiratory failure, chronic obstructive pulmonary disease, kidney failure, metabolic acidosis, high fever, female, young, old and obesity. Some people stress that intravenous aminophylline is easy to poison the elderly, so it is not appropriate to give the elderly intravenous injection of this drug.
(1) Mild poisoning: nausea, vomiting, headache, restlessness, insomnia and excitable etc.
(2) Moderate poisoning: In addition to the above reactions, precardiac discomfort, palpitation, arrhythmia or irregular breathing, etc.
(3) Severe poisoning: there may be ventricular tachycardia, mental disorders, convulsions, seizures, coma, and even respiratory and cardiac arrest.
The poisoning symptoms of infants and the elderly are more serious. Fifteen cases of children (aged 12 days to 16 months) were reported to have misused aminophylline more than 10 times the normal dose. Among them, 11 cases were given intravenously and intravenously respectively, and the rest were given orally. The main manifestations after medication were central nervous system overexcitement, crying disturbance, muscle tremor, convulsion and delirium, rapid respiration, failure, arrhythmia, and rapid and frequent vomiting. Two cases died. Cardiac accidents are common in the elderly with poisoning. Six cases of acute left heart failure were reported after intravenous injection of 0.25-0.5 g aminophylline diluted by 20 ~ 40ml 50% glucose solution. In 4 cases, dyspnea, orthostatic and sinus tachycardia occurred within 1 ~ 2 minutes. The other two fainted at 2 minutes. After symptomatic treatment, the symptoms were relieved 15 ~ 20 minutes later.
Some patients develop allergic corpora shortly after intravenous injection, presenting with sweating, irritability, cyanosis, shortness of breath, tingling of the mouth, and decreased blood pressure. This should be distinguished from the toxic reactions caused by intravenous injection, as the two treatments are not the same.
Plasma drug concentration determination All patients receiving theophylline therapy should have their plasma drug concentration measured when available. The measurement time should be selected in: ① input load before; 1 ~ 2 hours after input; ③ 24 hours after medication; ④ Critical patients should be measured once every 12 hours during medication. When the plasma concentration of theophylline was less than 5 mg/L, there was almost no efficacy. 5 ~ 10mg/L effective; 10 ~ 20mg/L is the best curative effect. > 20mg/L, the toxic reaction showed. 30 ~ 40mg/L can cause severe toxic reactions.
First aid treatment
There is no special detoxification therapy, mainly supportive therapy and symptomatic therapy.
1. Remove toxins
(1) Gastric lavage as soon as possible for those poisoned by oral administration. The gastric lavage solution can be 1:5000 potassium permanganate solution; Catharsis, a large amount of fluids, drinking diuretics, to promote the excretion of toxins.
(2)Hemodialysis or peritoneal dialysis is feasible for patients with life-threatening poisoning; Resin blood perfusion is also effective, perfusion can be 2 ~ 2.5 hours, the curative effect is faster than hemodialysis.
(3) Repeated large dose of oral activated carbon, 40g for the first time, and then take 20g for 2 ~ 3 hours, and take 20% sorbitol solution 50 ~ 70ml each time after taking, this method can accelerate the clearance of theophylline in the body 1 times.
2. Symptomatic treatment
(1) Patients with abdominal distension and vomiting can receive intramuscular injection or intravenous injection of neostigmine 1 mg; Metoclopramide 10mg can also be injected intramuscular.
(2) Diazepam, phenobarbital or bentoin sodium and other tranquillizer can be used when excited, agitated, delirium or convulsion.
(3) arrhythmias should be selected according to specific types of drugs, such as lidocaine for ventricular arrhythmias, verapamil for atrial arrhythmias, and propafenone, etc.
(4) hypotension can be intramuscular injection or intravenous infusion of the pressor known interhydroxyamine.
(5) Oxygen inhalation.
3. Adenosine triphosphate should be prohibited during treatment of poisoned patients.
Method of production of theophylline
(1)1, 3-dimethyl-4-amino-5-formamide ureacil reacted with sodium hydroxide solution at 90-95℃ to obtain theophylline crude product, which was recrystallized by hot water and decolorized by activated carbon.
(2) Using ethyl cyanoacetate and dimethyl urea as raw materials, through condensation, nitrification, reduction, formylation, cyclization reaction to obtain crude product, recrystallization.