Compound acetylsalicylic acid tablets
Function and Efficacy
Pharmacodynamics ① Analgesic effect: It mainly inhibits the synthesis of prostaglandins and other substances that can make pain sensitive to mechanical or chemical stimulation (such as bradykinin, histamine), and is a peripheral analgesic. However, the possibility of central analgesia (possibly acting on the hypothalamus) cannot be ruled out; ② Anti-inflammatory effect: The exact mechanism is still unclear. It may be due to the fact that this product acts on inflamed tissues and inhibits the synthesis of prostaglandins or other substances that can cause inflammatory reactions (such as histamine). Inhibition of the release of lysosomal enzymes and leukocyte activity may also be related to it; ③ Antipyretic effect: It may act on the hypothalamic thermoregulatory center to cause peripheral vasodilation, increased skin blood flow, sweating, and increased heat dissipation to have an antipyretic effect. This central effect may be related to the inhibition of prostaglandin synthesis in the hypothalamus; ④ Anti-rheumatic effect: The anti-rheumatic mechanism of this product, in addition to antipyretic and analgesic effects, is mainly anti-inflammatory; ⑤ Inhibition of platelet aggregation: It works by inhibiting platelet prostaglandincyclooxygenase, thereby preventing the generation of thromboxane A2 (TXA2) (TXA2 can promote platelet aggregation). This effect is irreversible. Pharmacokinetics: After oral administration, it is absorbed rapidly and completely. It has already begun to be absorbed in the stomach, and most of it can be absorbed in the upper part of the small intestine. The absorption rate is related to solubility and gastrointestinal pH. Food can reduce the absorption rate, but it does not affect the amount absorbed. Enteric-coated tablets are absorbed slowly. This product is absorbed faster when taken with sodium bicarbonate. After absorption, it is distributed in various tissues and can also penetrate into the joint cavity and cerebrospinal fluid. The protein binding rate of aspirin is low, but the protein binding rate of hydrolyzed salicylate is 65-90%. The binding rate decreases accordingly when the blood drug concentration is high. The binding rate is also low in renal dysfunction and pregnancy. The half-life is 15-20 hours; the half-life of salicylate depends on the size of the dose and the urine pH. It is about 2-3 hours when taking a small dose at a time; it can reach more than 20 hours when taking a large dose, and it can reach 5-18 hours when taking the drug repeatedly. After taking 0.65g of aspirin orally once, the half-life of salicylate in breast milk is 3.8-12.5 hours. Most of this product is quickly hydrolyzed into salicylates in the gastrointestinal tract, liver and blood, and then metabolized in the liver. The metabolites are mainly salicylic acid and glucuronic acid conjugates, and a small part is oxidized to gentisic acid. The blood drug peak is reached 1 to 2 hours after a single dose. The blood drug concentration is 25 to 50 mu; g/ml when analgesic and antipyretic; 150 to 300 mu; g/ml when anti-humidity and anti-inflammatory. The time required for blood drug concentration to reach a stable state increases with the increase of daily dose and blood drug concentration, and can be as long as 7 days when taking large doses of drugs (such as anti-rheumatic drugs). For patients who take large doses of drugs for a long time, because the main metabolic pathway of the drug is saturated, a slight increase in dose can lead to a large change in blood drug concentration. Most of this product is excreted from the kidneys as conjugated metabolites and a small part as free salicylic acid. When the dosage is large, the excretion of unmetabolized salicylic acid increases. There can be great differences between individuals. The pH of urine affects the excretion rate. In alkaline urine, the excretion rate is accelerated and the amount of free salicylic acid increases, while the opposite is true in acidic urine.
Ingredients
Appearance
This product is white tablets.
Indication
Salicylic acid analgesics, anti-inflammatory, antipyretics, anti-rheumatic and platelet inhibition drugs can be used clinically in the following situations. (1) Analgesics and antipyretics: They can relieve mild or moderate pain, such as headaches, toothaches, neuralgia, muscle pain and menstrual pain. They are also used to reduce fever for colds, flu, etc. This product can only relieve symptoms and cannot treat the causes of pain and fever, so other drugs must be used at the same time for causal treatment. (2) Anti-inflammatory and anti-rheumatic: It is the first choice for the treatment of rheumatic fever. After taking the medicine, it can reduce fever, reduce inflammation, improve joint symptoms, and reduce erythrocyte sedimentation rate, but it cannot eliminate the basic pathological changes of rheumatism, nor can it prevent heart damage and other complications. If there is obvious myocarditis, it is generally recommended to use adrenal cortex hormones first, and then add this product after the rheumatic symptoms are controlled and before the hormone is stopped.
Usage and Dosage
1. Oral dosage for adults. ① Antipyretic and analgesic, 0.3-0.6g once, 3 times a day, once every 4 hours if necessary. ② Anti-rheumatic, 3-5g a day (7-8g can be used for acute rheumatic fever), divided into 4 doses for oral administration. ③ Inhibit platelet aggregation, there is no clear dosage, most advocate the use of small doses, such as 50-150mg, once every 24 hours. ④ Treatment of biliary ascariasis, 1g once, 2-3 times a day, for 2-3 consecutive days; stop using after 24 hours of paroxysmal colic, and then carry out anthelmintic treatment. 2. Oral dosage for children. ① Antipyretic and analgesic, 1.5g/m2 per day, divided into 4-6 times orally, or 5-10mg/kg per day, or 60mg per year, once every 4-6 hours if necessary: ② Anti-rheumatic, 80-100mg/kg per day, divided into 3-4 times. If no effect is achieved in 1-2 weeks, the dosage can be adjusted according to the blood drug concentration. In some cases, it needs to be increased to 130mg/kg per day. Others: For children with mucocutaneous lymph node syndrome (Kawasaki disease), start with 80-100mg/kg per day, divided into 3-4 times. After 2-3 days of fever, change to 30mg/kg per day, divided into 2-4 times, and take it for 2 months or longer. During the period of thrombocytosis and hypercoagulable blood, take 5-10mg/kg per day, once a day. Dosage instructions: ① It should be taken with food or with water to reduce gastrointestinal irritation; ② The whole tablet should be swallowed within 7 days after tonsillectomy or oral surgery to avoid contact with the wound after chewing and causing damage; ③ For patients undergoing surgical operations, it should be discontinued 5 days before surgery. To avoid coagulation disorders; ④ When used to treat arthritis, the dose should be gradually increased until the symptoms are relieved and the effective blood concentration is reached (mild toxic reactions such as tinnitus and headache may occur at this time. In children, the elderly or deaf patients, these symptoms are not reliable indicators) and then the dose is reduced; but the dosage should not be adjusted frequently, generally not more than once a week. Of course, if side effects occur, the dose should be reduced quickly; it usually takes 7 days for the blood concentration of salicylic acid drugs to reach a steady state; ⑤ Patients with dehydration (especially children) should reduce the dose. When taking large amounts of drugs for a long time, the hematocrit, liver function and serum salicylic acid content should be checked regularly.
Adverse Reactions
The doses generally used for antipyretic and analgesic rarely cause adverse reactions. Long-term and large-scale use of the drug (such as treatment of rheumatic fever), especially when the blood concentration of the drug is 200μg/ml, is more likely to cause side effects. The higher the blood concentration, the more obvious the side effects. (1) The more common gastrointestinal reactions include nausea, vomiting, upper abdominal discomfort or pain (caused by direct stimulation of the gastric mucosa by this product) (incidence rate 39%). (2) Less common or rare cases include (incidence rate 3%): ① Gastrointestinal bleeding or ulcer, manifested as bloody or tarry stools, severe stomach pain or vomiting of bloody or coffee-like substances, which are more common in patients taking large doses of the drug; it is reported that 70% of patients taking 46g per day bleed 310ml per day, and those with ulcers may bleed more and may cause hemorrhagic anemia; gastrointestinal irritation reactions are rare after taking enteric-coated tablets; ② Bronchospasm allergic reaction, manifested as shortness of breath, dyspnea or asthma, chest tightness; ③ Skin allergic reaction, manifested as rash, urticaria, skin itching, etc.; ④ Liver and kidney damage, which is related to the dose, especially when the dose is too large and the blood drug concentration reaches 250mu;g/ml. The damage is reversible and can be restored after stopping the drug. (3) Symptoms of overdose or poisoning: ① Mild, namely salicylic acid reaction (salicylism), which is more common in patients with rheumatism treated with this product, manifested as headache, dizziness, tinnitus, deafness, nausea, vomiting, diarrhea, drowsiness, mental disorder, sweating, deep and rapid breathing, thirst, involuntary movements of hands and feet (more common in the elderly), visual impairment, etc.; ② Severe, hematuria, convulsions, hallucinations, severe mental disorder, dyspnea, unexplained fever, etc. may occur; mental and respiratory disorders are more obvious in children; in case of overdose, laboratory tests may show abnormal EEG, changes in acid-base balance (respiratory alkalosis and metabolic acidosis), hypoglycemia or hyperglycemia, ketonuria, hyponatremia, hypokalemia and proteinuria. It may cause gastrointestinal irritation, bleeding or discomfort, hemolytic anemia, interference with platelet function, angioedema, rash, asthma, and overdose may cause dizziness, tinnitus, sweating, nausea, vomiting, mental disorder or confusion, hyperventilation, confusion, cardiac collapse, and dyspnea. Children under 12 years old may cause Reye's syndrome and hyperuricemia, and long-term use may cause liver damage.
Precautions
1. It is contraindicated for patients who are allergic to aspirin or other non-steroidal anti-inflammatory drugs and caffeine, or patients with hemophilia, active peptic ulcer and other causes of gastrointestinal bleeding; 2. It should be used with caution in children under 6 years old and is contraindicated for infants under 3 months old; 3. It should be used with caution in pregnant and lactating women.
Special Population Medication
Precautions for children: Children under 6 years old should use with caution, and infants under 3 months old are prohibited. Precautions for pregnancy and lactation: Pregnant women and lactating women should use with caution. Precautions for the elderly: Elderly patients are prone to toxic reactions due to decreased renal function, so this product should be used with caution or in a reduced dosage.
Drug Interactions
Not yet clear.
Storage
Keep away from light and store in a sealed container.
Packaging Specification
Acetylsalicylic acid 35mg, phenacetin 24mg, caffeine 6mg
Validity Period
24 months
Manufacturer
Tiansheng Pharmaceutical Group Co., Ltd.
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Founded in:
2001-10-16 -
Address:
Chongqing Chaoyang Industrial Park (Dianjiang Guixi) -
Tax NO.:
9150000073397948XL -
Registered Funds:
318 million yuan -
Website:
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Email: