Paracetamol Infusion 1GM/100ml for Slow Intravenous Infusion

Each 100ml contains:Paracetamol1gmWater for Injectionsq.s.
Composition:
Each 100ml contains:
Paracetamol..................................................1gm
Water for Injections..................................q.s.
Folded physical property
The prismatic crystals of ethanol.Melting point of 169-171 ºC, relative density 1.293 (21/4 ºC).Soluble in ethanol, acetone and hot water, insoluble in water, insoluble in petroleum ether and benzene.No smell, bitter taste.The pH value of saturated aqueous solution is 5.5-6.5.
The preparation methods
This product is made for acetaminophen.
Method 1: adding amino phenol to dilute acetic acid, adding glacial acetic acid, reaction temperature to 150 ºC, 7 h, to join the acetic anhydride, reaction 2 h again, check the finish, qualified after cooling below 25 ºC, rejection filter, washed to acetic acid taste, dry, coarse product.
Method 2: amino phenol, glacial acetic acid and acid with 50% or more of the acid mother liquor distillation, steamed out of dilute acid distillate per hour the speed of one over ten of the total, to stay within the temperature rise to more than 130 ºC, amino phenolic residue sampling inspection for less than 2.5%, in dilute acid content (50%), the cooling crystallization.To filter, wash with a small amount of dilute acid, and then use a large amount of water to get close to colorless.
The yield of method 1 is 90%, and the yield of method 2 is 90-95%.
Refined method: when heated to near boiling, put into coarse products.Heat up to total solution, add water soaked activated carbon, and dilute acetic acid to pH= 4.2-4.6, boiling 10min.Pressure filtration, filtrate and a small amount of heavy sodium sulfite.Cooling below 20 ºC, precipitation crystallization.Shake off, wash, dry with the product of acetaminophen.
Other methods of production include: (1) zinc reduction for nitrophenol in glacial acetic acid and acetylation of acetaminophen;(2) the hydrazone produced by hydroxyacetophenone, in acid solution of sulfuric acid, was added to sodium nitrite and transposed to produce acetaminophen.
Drug pharmacology
Pharmacodynamics is a kind of acetanilide antipyretic analgesics.By inhibiting ring oxidase and selectivity in the hypothalamus of the temperature regulating center, the synthesis of prostaglandins in peripheral vascular expansion, sweating and antipyretic effect, strength of its antipyretic effect similar to aspirin.By inhibiting the synthesis and release of prostaglandin, the pain threshold can be improved to play analgesic effect, which belongs to peripheral analgesic medicine, which is weaker than aspirin, only effective for mild and moderate pain.This product has no obvious anti-inflammatory effect.
Pharmacokinetic from gastrointestinal tract after oral absorption quickly and completely (after high carbohydrate diet medication may reduce absorption), distributed evenly in the body fluids, after absorbing about 25% combined with plasma proteins.Small amount (blood drug concentration <60 mu g/ml) is not obvious in combination with protein, and the combination rate of mass or intoxication is high, which can reach 43 %.90 ~ 95% of the product is metabolized in the liver, mainly in combination with glucuronic acid, sulfuric acid and cysteine.Intermediate metabolites have a toxic effect on the liver.Half-life beta is usually 1 ~ 4 hours to 2 hours (average), kidney function not full-time unchanged, but in some liver disease patients may extend, the elderly and newborns can be extended, children is shorter.The blood drug concentration of 0.5 ~ 2 hours after oral administration was peak, and the blood drug concentration was 5 ~ 20 mu g/ml at the dose under 650mg, and the duration was 3 ~ 4 hours.During lactation, women took 650mg of the product, and the concentration of milk was 10 ~ 15 mu g/ml in 1 ~ 2 hours.The half-life beta is 1.35 to 3.5 hours.The product is mainly excreted from the kidney in the form of the combination with glucuronic acid, and about 3% of the product is excreted in the urine in 24 hours.
To adapt to the symptoms
It can be used for mild to moderate pain, such as fever, headache, joint pain, neuralgia, and pain, etc.The goods can only relieve symptoms, anti-inflammatory effects no or very little, can't eliminate the redness, swelling, arthritis activity obstacle, so can't to replace aspirin or other non-steroidal anti-inflammatory drug treatment of all types of arthritis.But the goods can be used for allergic to aspirin, intolerance, or is not suitable for application cases of aspirin, such as chickenpox, patients with hemophilia and other hemorrhagic diseases (including cases of application of anticoagulant therapy), and peptic ulcer, gastritis, etc.If necessary, the application should be applied to other treatments to relieve pain or fever.
Side effects
1. Adverse reactions of liver: prolonged or overdose can cause liver cell necrosis.Paracetamol cause liver cell necrosis is its direct effects on liver cells, may be an overdose of acetaminophen causes the body to generate a toxic metabolite, when accumulated to a certain amount, cause liver GSH depletion, decreased liver detoxification capacity greatly, toxic metabolite destroy liver cells and produce cell degeneration and necrosis.Due to excessive paracetamol of the heart necrosis of acute hepatic lobules, rapid progression of sudden liver failure and death.
The side reaction of 2, kidney: excessive toxic metabolites generated paracetamol also can damage the kidneys and cause renal cell necrosis, especially share sodium salicylate or caffeine, are more likely to damage the kidneys.
3, the side reaction of blood system: long-term excessive paracetamol, toxic metabolites can be generated by direct effects on bone marrow hematopoietic system, constitute the damage, can also induce thrombocytopenic purpura or leukemia.
4, the side reaction of the nervous system: if children with an overdose of acetaminophen, also can cause the symptoms of the central nervous system, mainly in the brain damage, neurologic impairment, coma, and so on.
Rarely, if allergic reaction should be stopped immediately.
considerations
• take an overdose and call the doctor immediately.
• not to be taken with other drugs containing acetaminophen.
• if there is a severe sore throat and accompanied by fever, headache or nausea or vomiting, please consult a doctor.
• avoid alcoholic beverages while taking the medicine, and the drinker should take the product and other painkillers under the guidance of a doctor.
Taking paracetamol in the following situations can cause liver damage
(1) overdose.
(2) take long and high doses.
(3) drink or drink alcoholic beverages.
(4) small doses of liver disease can also damage the liver.
(5) mix it with other acetaminophen headaches, cold medications and other medications.In a study of 300 patients with severe liver failure, American researchers found that 38 percent of the cases were related to acetaminophen.In another group of 307 adults suffering from severe liver damage, 35 percent of the cases were linked to acetaminophen.Most of these cases are accidental, due to inattention.