Contents 1 Pinyin 2 English Reference 3 Overview 4 Acetazolamide Pharmacopoeia Standard 4.1 Product name 4.1.1 Chinese name 4.1.2 Chinese Pinyin 4.1.3 English name 4.2 Structural formula 4.3 Molecular formula and molecular weight 4.4 Source (name), Content (potency) 4.5 Properties 4.6 Identification 4.7 Inspection 4.7.1 Acidity 4.7.2 Clarity of alkaline solution 4.7.3 Chloride 4.7.4 Sulfate 4.7.5 Related substances 4.7.6 Silver reduction 4.7.7 Weight loss on drying 4.7.8 Ignition residue 4.7.9 Heavy metals 4.8 Content determination 4.9 Category 4.10 Storage 4.11 Preparation 4.12 Version 5 Acetazolamide instructions 5.1 Drug name 5.2 English name 5.3 Alias ??of Demaxi 5.4 Classification 5.5 Dosage form 5.6 Pharmacological effects of acetazolamide 5.7 Pharmacokinetics of acetazolamide 5.8 Indications of acetazolamide 5.9 Contraindications of acetazolamide 5.10 Precautions 5.11 Adverse reactions of acetazolamide 5.12 Usage and dosage of acetazolamide 5.13 Interactions between Demax and other drugs 5.14 Expert Comments 6 Acetazolamide Poisoning 6.1 Clinical Manifestations 6.2 Treatment 7 References This is a redirected entry that shares the content of Acetazolamide. For the convenience of reading, acetazolamide in the following text has been automatically replaced by demax. You can click here to restore the original appearance, or use the note method to display 1 Pinyin
dài mǎ kè sī 2 English reference
< p> Iocamic Acid 3 OverviewDemax is a carbonic anhydrase inhibitor drug, which is white needle-shaped crystals or crystalline powder; odorless and slightly bitter in taste. By inhibiting carbonic anhydrase in renal tubular epithelial cells, the formation of H+ and HC03 is reduced, the exchange of Na+ and H+ is slowed down, Na+ reabsorption is reduced, and the excretion of Na+, K+, H2O and HC03 is increased, resulting in a diuretic effect. Sometimes used to treat cerebral edema and mild cardiogenic edema. This drug inhibits carbonic anhydrase in ciliary body cells, reducing the production of aqueous humor and lowering intraocular pressure, so it is mainly used to treat glaucoma. Also used as an anti-epileptic drug. Mainly damages the central nervous system, blood system, liver, kidney, etc. 4 Daimax Pharmacopoeia Standard 4.1 Product name 4.1.1 Chinese name
Daimax 4.1.2 Chinese Pinyin
Yixian Zuo'an
4.1.3 English Name
Acetazolamide 4.2 Structural formula 4.3 Molecular formula and molecular weight
C4H6N4O3S2 222.25 4.4 Source (name), content (potency)
This product is N (5 ammonia sulfonate Acyl 1,3,4thiadiazole 2yl)acetamide. Calculated on a dry basis, the C4H6N4O3S2 content should be 98.0% to 102.0%. 4.5 Properties
This product is white needle crystal or crystalline powder; odorless and slightly bitter.
This product is slightly soluble in boiling water, very slightly soluble in water or ethanol, almost insoluble in chloroform or ether; easily soluble in ammonia solution. 4.6 Identification
(1) Take about 0.1g of this product, add sodium hydroxide test solution dropwise to dissolve, add 10ml of water and 1 drop of phenolphthalein indicator solution, add dilute hydrochloric acid dropwise until the pink color disappears, add mercury nitrate A few drops of the test solution will form a white precipitate.
(2) Take about 0.2g of this product, put it in a test tube, add 1ml each of ethanol and sulfuric acid, and heat it to produce the aroma of ethyl acetate.
(3) The infrared light absorption spectrum of this product should be consistent with the control spectrum (Figure 9 of "Drug Infrared Spectrum Collection"). 4.7 Inspection 4.7.1 Acidity
Take 1.0g of this product, add 50ml of heated water, shake, let cool, and measure according to the law (2010 edition of Pharmacopoeia, Part II, Appendix VI H). The pH value should be 4.0 to 6.0. 4.7.2 Clarity of alkaline solution
Take 1.0g of this product and add 5ml of 10% sodium hydroxide solution to dissolve it. The solution should be clear.
4.7.3 Chloride
Take 2.0g of this product, add 100ml of water, heat to dissolve, quickly cool, filter, take 25ml of filtrate, check according to law (2010 edition of Pharmacopoeia, Part 2, Appendix VIII A), and Compared with the control solution made from 7.0 ml of standard sodium chloride solution, it must not be more concentrated (0.014%). 4.7.4 Sulfate
Take 25ml of the remaining filtrate under the above chloride item, check it according to the law (Appendix VIII B of Part II of the 2010 edition of the Pharmacopoeia), and compare it with the control solution made of 2.0ml of standard potassium sulfate solution. No more concentrated (0.04%). 4.7.5 Related substances
Take 50 mg of this product, place it in a 100 ml measuring bottle, add 80 ml of water, heat it in an 80°C water bath for 5 minutes, shake to dissolve, let cool, add water to dilute to the mark, shake well , as the test solution; accurately measure 1ml, place it in a 100ml measuring bottle, add water to dilute to the mark, shake well, and use it as the control solution. According to the test of high performance liquid chromatography (Appendix V D of Pharmacopoeia Part 2, 2010), octadecylsilane bonded silica gel was used as filler; 0.43% anhydrous sodium acetate solution-methanol-acetonitrile (95:2:3, Use glacial acetic acid to adjust the pH value to 4.0±0.05) as the mobile phase; the detection wavelength is 265nm. The number of theoretical plates shall not be less than 5,000 based on the generation max peak. Take 20 μl of the control solution and inject it into the liquid chromatograph. Adjust the detection sensitivity so that the peak height of the main component chromatographic peak is approximately 20% of the full scale. Then accurately measure 20 μl each of the test solution and the control solution, inject them into the liquid chromatograph respectively, and record the chromatogram to twice the retention time of the main component peak. If there is an impurity peak in the chromatogram of the test solution, the area of ??a single impurity peak shall not be greater than 0.5 times (0.5%) of the main peak area of ??the control solution, and the sum of the areas of each impurity peak shall not be greater than the main peak area of ??the control solution (1.0%). 4.7.6 Silver reduction substance
Take 5.0g of this product, moisten it with 5ml of absolute ethanol, add 125ml of water and 10ml of nitric acid, accurately add 5ml of silver nitrate titrant (0.1mol/L), and shake well. , place in the dark for 30 minutes, filter through a fused glass funnel, wash the container and funnel with 10ml of water, combine the filtrate and washing liquid, add 5ml of ferric ammonium sulfate indicator solution, and titrate with ammonium thiocyanate titrant (0.1mol/L) To the end point, the consumption of ammonium thiocyanate titrant (0.1mol/L) shall not be less than 4.8ml. 4.7.7 Weight loss on drying
Take this product and dry it at 105℃ to constant weight. The weight loss shall not exceed 0.5% (Appendix VIII L of Pharmacopoeia Part 2, 2010 Edition). 4.7.8 Ignition residue
shall not exceed 0.1% (2010 edition of Pharmacopoeia, Part II, Appendix VIII N). 4.7.9 Heavy metals
Take 0.50g of this product and check it according to the law (Appendix VIII H, Method 3 of the 2010 Pharmacopoeia, Part 2). The heavy metal content should not exceed 20 parts per million. 4.8 Content determination
Take about 0.2g of this product, weigh it accurately, add 400ml of boiling water and stir to dissolve, let it cool, transfer it to a 1000ml measuring bottle, dilute with water to the mark, shake well; accurately measure 5ml , put in a 100ml measuring bottle, add 10ml of 1mol/L hydrochloric acid solution and dilute to the mark with water, shake well, and measure the absorbance at the wavelength of 265nm according to UV-visible spectrophotometry (2010 edition of Pharmacopoeia, Appendix IV A) The absorption coefficient () of C4H6N4O3S2 is calculated as 474, which is obtained. 4.9 Category
Carbonic anhydrase inhibitors. 4.10 Storage
Protect from light and seal. 4.11 Preparations
Daimax Tablets Version 4.12
"Pharmacopoeia of the People's Republic of China and the People's Republic of China" 2010 Edition 5 Daimax Instructions 5.1 Drug Name
Daimax Max 5.2 English name
Acetazolamide, Acetamide, Albox, Diluran, Diurramide, DIAMOX, Edemox 5.3 Alias ??of Max 5.3
Acetazolamide; Acetazolamide; Acetazolamide; Diamox; Acetazolamidum; Acetazolamide; Diamox; Acetazolamidum; Diamox 5.4 Classification
Circulatory system drugs> Antihypertensive drugs> Diuretics and antihypertensive drugs 5.5 Dosage forms
< p> 1. Tablets: 250mg each;2. Injection (powder): 500mg. 5.6 Pharmacological effects of Demax
1. Reduce intraocular pressure. Carbonic anhydrase is present in all tissues in the eye (such as the retina, uvea, and lens), and the largest amount is found in the ciliary body. In glaucoma, the activity of carbonic anhydrase in the ciliary body epithelium increases, resulting in excessive sodium bicarbonate production, which increases the osmotic pressure in the aqueous humor, increases the production of aqueous humor, and increases intraocular pressure.
Demaxi can inhibit the activity of carbonic anhydrase in the ciliary body epithelium, thereby reducing the production of aqueous humor (50% to 60%) and reducing intraocular pressure in patients with glaucoma. Others believe that the intraocular pressure-lowering effect of Demax is due to its reduction in plasma HCO-3 concentration and increase in plasma chloride concentration, which causes metabolic acidosis and decreases blood blood reserve.
2. Cardiogenic edema. Demaxi can be used for cardiogenic edema, but it is not effective for renal and hepatic edema. Demaxi can inhibit carbonic anhydrase in renal tubular epithelial cells, reducing the production of H+ and Na+ reabsorption, and increasing the excretion of Na+, water and bicarbonate, thus producing a diuretic effect. However, Demaxi does not have a strong diuretic effect (it has a good diuretic and antihypertensive effect in patients with eclampsia accompanied by edema), and long-term use can cause drug resistance, so it is rarely used alone for diuresis. When combined with mercury diuretics, they can correct the acid-base balance imbalance caused by each other.
3. Others: Demaxi can also reduce the production of cerebrospinal fluid and inhibit gastric acid secretion. Its mechanism may also be related to the inhibition of carbonic anhydrase. The anti-epileptic mechanism of Demaxi is not fully understood. 5.7 Pharmacokinetics of Daimax
It is easily absorbed after oral administration and has a high protein binding rate. Intraocular pressure begins to decrease 1 to 1.5 hours after oral administration of 500 mg, and the plasma concentration reaches its peak at 12 to 27 μg/ml at 2 to 4 hours. The effect can last for 4 to 6 hours, and the half-life is 24 to 5.8 hours; it begins 2 hours after oral administration of 500 mg of sustained-release capsules. It has an intraocular pressure-lowering effect, the peak time is 8 to 12 hours, the peak serum concentration is 6 μg/ml, and the effect lasts for 18 to 24 hours; it starts to lower intraocular pressure 2 minutes after intravenous injection of 500 mg, and reaches the peak blood concentration in 15 minutes, and the effect lasts for 4 to 5 hours. . Regardless of whether Demaxi is administered orally or intravenously, 90% to 100% of the dose is excreted by the kidneys in unchanged form within 24 hours, but only 47% of the sustained-release capsule is excreted within 24 hours. 5.8 Indications of Demaxi
1. To treat various types of glaucoma and reduce intraocular pressure before anti-glaucoma and certain intraocular surgeries. It is an effective way to control the increase in intraocular pressure in various types of glaucoma in the short term. Adjuvant medications for intraocular pressure.
2. Used for cardiogenic edema. It is also used for cerebral edema and can reduce the production of cerebrospinal fluid.
3. Treat peptic ulcer and inhibit gastric acid secretion.
4. Trial for major and minor epileptic seizures.
5. It can also be used to treat acute mountain sickness and juvenile myoclonic epilepsy.
6. Hypochloremia and hypokalemic periodic paralysis in heart failure. 5.9 Contraindications of Demax
1. Allergy to Demax or other carbonic anhydrase inhibitors, sulfonamides, and thiazide diuretics.
2. Adrenal failure and adrenal insufficiency.
3. Hyponatremia and hypokalemia.
4. Severe liver and kidney dysfunction.
5. Hyperchloric acidosis.
6. Heart failure.
7. Have a history of urinary stones.
8. Patients with chronic non-congestive angle-closure glaucoma. 5.10 Precautions
1. (1) Diabetes; (2) Pulmonary infarction or emphysema.
2. Effects of drugs on the elderly: Elderly patients are more likely to develop drug resistance after long-term use, and may easily cause metabolic acidosis and hypokalemia.
3. Effects of drugs on pregnancy: Animal experiments have confirmed that giving rodents 10 times the regular adult dose of Demax has a higher teratogenic rate, so pregnant women should not use Demax , especially in the first 3 months of pregnancy.
4. The effect of drugs on test values ??or diagnosis: (1) It can interfere with the absorption of the Glenn Nelson method, causing false positive results in the urine 17-hydroxysteroid test; (2) It can alkalinize urine, making the urine False positive results occur in protein measurement (such as bromophenol blue test, etc.); (3) It can increase blood ammonia concentration, serum bilirubin, and urobilinogen concentration; (4) It can increase blood sugar concentration and urine sugar concentration, but in non-diabetic patients Not affected; (5) Plasma chloride concentration may increase and serum potassium concentration may decrease.
5. Check or monitor before and after medication and during medication: For patients with glaucoma: (1) Intraocular pressure should be measured every day during the acute attack, intraocular pressure should be measured regularly during the chronic stage, and vision and visual field should be checked regularly; (2) After intraocular pressure is controlled, the dosage of medication and appropriate anti-glaucoma surgery should be selected based on the type of glaucoma, changes in iridocorneal angle, etc.; (3) Use miotics or timolol eye drops combined with Demax to control Patients with late-stage open-angle glaucoma, congenital glaucoma, and patients who need to postpone anti-glaucoma surgery with unsatisfactory intraocular pressure should not only take additional potassium salts, but also need to have 24-hour intraocular pressure curve, visual acuity, visual field, blood pressure, etc. before treatment. Blood picture and urine routine records are recorded in order to evaluate the efficacy and detect possible adverse reactions during the treatment process.
6. Patients who cannot tolerate sulfa drugs or other sulfonamide derivative diuretics cannot tolerate Demaxi.
7. For angle-closure glaucoma, after using Demaxi in the acute phase, in principle, appropriate anti-glaucoma surgery should be selected based on the iridocorneal angle and intraocular pressure tracings, otherwise the lowered intraocular pressure will give people With the false appearance of safety, angle adhesions will further develop and the timing of surgery will be delayed.
8. Some people who are intolerant to the adverse reactions of Demaxx or who are ineffective after taking Demaxx for a long time can use other carbonic anhydrase inhibitors (such as dichlorphenamide).
9. In order to prevent the occurrence of renal complications, in addition to the general prevention principles of sulfa drugs, potassium salts, magnesium salts, etc. should also be taken. Patients with hypercalciuria should eat a low-calcium diet.
10. For patients with kidney stones (mainly calcium), Demax may induce or aggravate the condition. If abdominal cramps and hematuria occur, the drug should be discontinued immediately.
11. Drink plenty of water during the period of taking. For long-term use, potassium salts should be taken. It is not suitable to combine with calcium, iodine and broad-spectrum antibiotics.
12. It should not be used by patients with pulmonary heart disease, heart failure, Addison syndrome, liver failure, metabolic acidemia and edema associated with hypokalemia. It should not be used by patients with chronic non-congestive angle-closure glaucoma.
13. Demax can cause myopia, loss of eye accommodation function, forward lens shift, retinal edema and other symptoms. If this occurs, the drug should be discontinued in time. 5.11 Adverse reactions of Demaxi
Serious adverse reactions rarely occur during short-term and intermittent use of Demax in ophthalmology. Some adverse reactions are unique to sulfonamide derivatives, and there are also some adverse reactions. It is dose related.
1. Common symptoms include numbness and tingling in the limbs, nausea, lack of appetite, drowsiness, weight loss, depression, metallic taste, diarrhea and polyuria.
2. Occasionally, hearing loss and temporary myopia and sulfonamide-like rash may occur after the first medication.
3. Rare exfoliative dermatitis, granulocytopenia or aplastic anemia.
4. Long-term medication can aggravate symptoms such as hypokalemia, hyponatremia, electrolyte imbalance and metabolic acidosis, as well as renal complications (such as renal colic, stone disease, sulfauria crystals, nephropathy) syndrome, etc.). Long-term use can cause abnormal sensation, gastrointestinal dysfunction, lack of appetite, drowsiness, fatigue, and temporary myopia. Long-term use may easily cause hypokalemia, so potassium salts should be supplemented in time. This drug can reduce the excretion of uric acid and has been reported to aggravate gout during treatment. For diabetic patients with existing kidney disease, kidney function can decrease rapidly. After long-term medication, urine becomes saline and calcium phosphate crystals tend to precipitate, leading to kidney stones and sometimes acute renal failure. Adverse reactions of sulfonamides may also occur, such as rash, crystalluria, agranulocytosis, aplastic anemia, and thrombocytopenia. 5.12 Usage and dosage of Demax
1. Oral administration: (1) Open-angle glaucoma: first dose 250 mg, 1 to 4 times a day. The maintenance dose should be determined based on the patient's response to the drug. Try to use a smaller dose to control the intraocular pressure. Generally, 250mg each time, twice a day, can control the intraocular pressure within the normal range; (2) Secondary glaucoma and Lower intraocular pressure before surgery: 250 mg each time, twice a day; (3) Acute cases: double the first dose to 500 mg, and then switch to a maintenance dose of 125 to 250 mg, once every 4 hours; (4) Treatment of cardiogenic edema : 250 to 500 mg each time, once a day, the best effect is when taken after breakfast; (5) Treatment of cerebral edema: 250 mg each time, 2 to 3 times a day; (6) Treatment of peptic ulcer: 500 mg each time, 3 times a day , 3 weeks is a course of treatment, and the pain disappears in 7 to 9 days. During the medication period, 2g of sodium bicarbonate, 1g of sodium citrate, 1g of potassium bicarbonate, 1.5g of magnesium oxide, and 1500 to 2000ml of water can be used every day to prevent water and electrolyte disorders. Prevention of familial periodic paralysis: Adults take 250 to 750 mg per day, divided into 2 to 3 times.
2. Intravenous injection: For rescue during acute glaucoma attacks and for some patients whose nausea and vomiting prevent oral administration, Demaxi 500 mg can be injected intravenously or intramuscularly, or 250 mg intravenously and 250 mg intramuscularly. Use alternately. For some patients with acute attacks of glaucoma, the above dosage can be used repeatedly within 2 to 4 hours, but continued treatment should be changed to oral dosage according to the patient's condition.
3. Intramuscular injection: the same as intravenous injection.
4. Children: (1) Oral administration: For anti-glaucoma, take 5 to 10 mg/kg orally per day or 300 to 900 mg/m2 per day, taken in divided doses. (2) Intravenous injection: For anti-acute glaucoma, it is usually injected intravenously according to body weight, 5 to 10 mg/kg each time, once every 6 hours. (3) Intramuscular injection: see intravenous injection. 5.13 Drug interactions
1. Combined use with adrenocorticotropic hormone, glucocorticoids, and mineralocorticoids can lead to severe hypokalemia and osteoporosis. Care should be taken to monitor serum potassium concentration and cardiac function when used in combination with the above drugs.
2. When used in combination with amphetamines, anti-M-cholesterol drugs (especially atropine), quinidine, etc., it can form analgesic urine, thereby reducing the excretion of Demax and aggravating the adverse reactions of Demax.
3. Since Demaxi can cause hyperglycemia and urine sugar, the dosage of anti-diabetic drugs should be adjusted when used in combination with anti-diabetic drugs (such as insulin).
4. Combined use with phenobarbital, carbamazepine or phenytoin can lead to an increase in the incidence of osteomalacia.
5. Combined use with digitalis glycosides can increase the toxicity of digitalis and cause hypokalemia.
6. Combined with mannitol or urea, it can increase urine output while enhancing the effect of lowering intraocular pressure. 5.14 Expert comments
Demax is a carbonic anhydrase inhibitor and is a sulfonamide derivative. By inhibiting carbonic anhydrase in ciliary body cells, the formation of carbonic acid is reduced, HCO3- is reduced, and the production of aqueous humor is reduced due to osmotic pressure, thereby reducing intraocular pressure. Clinically, it is often used in combination with miotics or other intraocular pressure-lowering drugs. It is often used to reduce blood pressure before various types of glaucoma and intraocular surgery and to slow the formation of the anterior chamber after surgery. 6. Daimax poisoning
Daimax (acetazolamide, acetazamide) is a carbonic anhydrase inhibitor. Inhibit carbonic anhydrase in renal tubular epithelial cells, reduce the formation of H+ and HC03, slow down the exchange of Na+ and H+, reduce Na+ reabsorption, increase the excretion of Na+, K+, H2O and HC03, and produce a diuretic effect. Sometimes used to treat cerebral edema and mild cardiogenic edema.
This drug inhibits carbonic anhydrase in ciliary body cells, reducing the production of aqueous humor and lowering intraocular pressure, so it is mainly used to treat glaucoma. Also used as an anti-epileptic drug. The oral LD50 for mice is >1.0g/kg, and the intravenous LD50 for dogs is >2g/kg. This drug is completely excreted by the kidneys within 24 hours and has no accumulation effect. The usual dosage for glaucoma and cerebral edema is 0.25g orally, 1 to 2/d. Mainly damages the central nervous system, blood system, liver, kidney, etc. [1] 6.1 Clinical manifestations
Adverse reactions are as follows [2]:
1. Central nervous system
Occasionally numbness and tingling in the face and limbs , drowsiness, fatigue, weakness, dizziness, loss of orientation, depression, muscle weakness, flaccid paralysis, ataxia, etc.
2. Digestive system
Anorexia, nausea, vomiting, dry mouth, thirst, diarrhea, etc.; may cause gastric ulcer, gastrointestinal bleeding, cholestatic jaundice; used in patients with liver cirrhosis This drug can induce hepatic encephalopathy.
3. Blood system
Produce bone marrow suppression, granulocytopenia, leukopenia, thrombocytopenic purpura, bleeding, megaloblastic anemia, aplastic anemia, etc.
4. Urinary system
Frequent urination, polyuria, glycosuria, anuria, hematuria, crystalluria, urinary tract stones, kidney stones, and renal colic.
5. Others
Slowed heart rate, hyperglycemia, hyperuricemia aggravating gout, abnormal liver function, deafness, temporary myopia and increased serum bilirubin, calcium, The excretion of potassium, magnesium, and sodium increases, and the concentration of chlorine increases, resulting in hypokalemia and hyperchloride acidosis. Human body surface area calculator BMI index calculation and evaluation Female safe period calculator Pregnancy date calculator Normal weight gain during pregnancy Safety classification of medication during pregnancy (FDA) Five elements and eight characters Adult blood pressure evaluation Body temperature level evaluation Diabetes diet recommendations Common clinical biochemistry units Conversion to basal metabolic rate Calculate sodium supplementation calculator Iron supplementation calculator Commonly used Latin abbreviations for prescription Quick check Common symbols for pharmacokinetics Quick check Effective plasma osmolality calculator Ethanol intake calculator
Medical encyclopedia, calculate now! 6.2 Treatment
The key points in the treatment of Demaxx poisoning are [3]:
1. Stop taking the drug immediately.
2. Replenish fluids and potassium, correct dehydration and acidosis, and maintain water and electrolyte balance.
3. If bone marrow suppression appears, give glucocorticoids, vitamin B6, inosine, nucleotide tablets, etc., and if necessary, small amounts and multiple blood transfusions.
4. If allergic reaction occurs, provide anti-allergic treatment.