Alias Metformin; Tai Gumi; Cimetidine ,Cimetidine Foreign Name Cimetidine Character White or off-white crystalline powder; almost odorless, bitter taste. Soluble in methanol, soluble in ethanol, slightly soluble in isopropanol, slightly soluble in water, soluble in dilute hydrochloric acid. Pharmacological action It is a kind of H2 receptor antagonist, which can significantly inhibit gastric acid secretion caused by food, histamine or pentagastrin stimulation and reduce its acidity. It has preventive and protective effects on corrosive gastritis caused by chemical stimulation, and also has obvious curative effects on stress ulcers and upper gastrointestinal bleeding. This product has anti-androgenic effect, which is valuable in the treatment of hirsutism. This product can attenuate the activity of immunosuppressive cells and enhance the immune response, thus inhibiting tumor metastasis and prolonging the survival period. Indications This product is suitable for duodenal ulcer, gastric ulcer, reflux esophagitis, upper respiratory tract bleeding. Dosage and Administration Oral: At the beginning, 1.2~1.6g per day, divided into 4 times. After the symptoms are reduced (about 10 days), take 0.2g each time, 3 times a day to maintain, can be taken for several months. After stopping the drug, if the symptoms recur, the drug is still effective. Static injection: 200mg, diluted with saline and slowly injected, 4-6h once, should not exceed 2g / d. The course of treatment are 4-6 weeks. Precautions 1.Digestive system reactions: the more common are diarrhea, abdominal distension, bitter mouth, dry mouth, mild elevation of aminotransferases, etc. Occasionally, there are severe hepatitis, hepatic necrosis, hepatic steatosis. Abrupt discontinuation of the drug can cause chronic peptic ulcer perforation, which is estimated to be caused by rebound hyperacidity after discontinuation. Therefore, it is necessary to continue to take the drug (400mg per night) for 3 months after completing the treatment. Patients with acute pancreatitis, pregnant and lactating women should not apply. 2. Urinary system reaction: in recent years, there are many reports of acute interstitial nephritis caused by this product, resulting in renal failure. However, this toxic reaction is reversible, and renal function can be normalized after stopping the drug. In order to avoid nephrotoxicity, attention should be paid to checking renal function during the use of the drug. 3. Hematopoietic reactions: the product has a certain inhibitory effect on the bone marrow, a small number of patients can occur reversible moderate granulocytopenia, thrombocytopenia and autoimmune hemolytic anemia, the incidence of which is 0.02% of the drug users. It has also been reported to cause aplastic anemia. Attention should be paid to check the blood picture during the use of the drug. 4. Central nervous system reaction: this product can pass the blood-brain barrier, with a certain degree of neurotoxicity, the more common are dizziness, headache, fatigue, drowsiness and other symptoms. A small number of patients may experience restlessness, dullness of sensation, slurred speech, sweating, localized convulsions or epileptic-like seizures, as well as hallucinations, delusions and other symptoms. 5. Cardiovascular system reaction: there may be bradycardia, facial flushing and so on. When injected intravenously, there are occasional sudden drop in blood pressure, atrial premature beats, cardiac and respiratory arrest. 6. Effects on endocrine and skin: due to the anti-androgenic effect, a large dose of the drug (more than 1.6g per day) can cause gynecomastia, female breast-feeding, decreased libido, impotence, reduced sperm count, etc., which can disappear after stopping the drug. It can inhibit sebum secretion and induce exfoliative dermatitis, dry skin, sebum deficiency dermatitis, alopecia, oral ulcers. Rash, giant urticaria, drug fever, etc. also occur from time to time. 7. Aluminum hydroxide, magnesium oxide or metoclopramide (Gastrofen) can reduce the blood concentration of this product when taken together with this product. 8. Since aluminum sulfate needs to be hydrolyzed by gastric acid to be effective, and this product is to inhibit gastric acid secretion, the combination of the two may reduce the efficacy of aluminum sulfate. 9. Combining with benzodiazepines (Valium, Nitrovalium, Flunitrazepam, Librium) may increase the blood concentration of Valium, aggravate sedation and other central nervous system depressing symptoms, and may develop into respiratory and circulatory failure. When the combination must be used, it can be changed to hydroxyvalium or chlorhydroxyvalium, and the elimination of the latter two is not affected by this product. 10. When patients take digoxin and quinidine at the same time, it is not suitable to use this product. Because this product can inhibit the metabolism of quinidine, and the latter can displace digoxin from its binding site, resulting in an increase in the blood concentration of both quinidine and digoxin. Blood levels should be monitored. 11. This product can delay the metabolism of caffeine, so when used in combination with it, it can enhance the latter's effect and is prone to toxic reactions. Caffeine is contraindicated in patients with gastric ulcer, and caffeine and caffeine-containing beverages should be contraindicated when taking this product. 12. Combined with warfarin anticoagulants, it can reduce the rate of the latter's excretion from the body and lead to bleeding tendency. 13. Due to the increase in pH of gastric juice, when combined with tetracycline, the dissolution rate of tetracycline can be reduced, absorption is reduced, and the effect is weakened (but the enzyme inhibition of this product may increase the blood concentration of tetracycline); if combined with acetylsalicylic acid, the opposite result occurs, and acetylsalicylic acid can enhance the effect. 14. Combining with ketoconazole can interfere with the absorption of the latter and reduce its antifungal activity, but the above changes can be avoided by taking some acidic beverages together. 15. Combining this product with captopril may cause psychotic symptoms. 16. Since this product has a myoneural blocking effect similar to that of aminoglycosides, this effect is not counteracted by neostigmine but only by calcium chloride. Therefore, when combined with aminoglycoside antibiotics, it may cause respiratory depression or respiratory arrest. Drug Interactions 1. Aluminum hydroxide, magnesium oxide, or metoclopramide (Gastroflex) may decrease the blood concentration of this product when taken concurrently with this product. 2. It may reduce the efficacy of aluminum thioglycollate. 3. This product is a hepatic enzyme inhibitor. Combining with Pranolol will increase its serum concentration and slow down the heart rate at rest; combining with phenytoin sodium or other beta-lactone ureas may increase the blood concentration of the latter and lead to phenytoin sodium poisoning. 4. Combination with opioids has been reported to produce respiratory depression, mental confusion, disorientation and other adverse reactions in patients with chronic renal failure. 5. This product may increase the absolute utilization of verapamil (ibogaine), which should be noted because of the rare but serious side effects that can occur with verapamil. 6. When combined with theophylline, it can reduce the demethylation clearance of the latter by 20%-30% and increase its blood concentration. 7. Combined with benzodiazepine tranquilizers, it may increase the blood concentration of diazepam, aggravate sedation and other central nervous system inhibition symptoms, and may develop into respiratory and circulatory failure. 8. When patients take digoxin and quinidine at the same time, it is not advisable to use this product, because this product can inhibit the metabolism of quinidine, and the latter can displace digoxin from its binding site, resulting in an increase in the blood concentration of both quinidine and digoxin. 9. This product can delay the metabolism of caffeine, and when used in combination with it, it can enhance the effect of the latter, and is prone to toxic reactions. 10. Combined with warfarin anticoagulants, it can reduce the rate of the latter's excretion from the body, leading to bleeding tendency. 11. Combined with tetracycline, tetracycline dissolution rate can be reduced, absorption is reduced, the effect is weakened; aspirin and vice versa. 12. Combination with ketoconazole can interfere with the absorption of the latter and reduce its antifungal activity, but the above changes can be avoided by taking some acidic drinks together. 13. Combining this product with captopril may cause psychotic symptoms. 14. Since this product has similar myoneurotic blocking effect to aminoglycosides, this effect is not counteracted by neostigmine, but only by calcium chloride. Therefore, the combination with aminoglycoside antibiotics may lead to respiratory depression or respiratory arrest. Specifications Tablet: 0.2g, 0.8g per tablet. Capsule: 0.2g per capsule. Injection: 0.2g (2ml) per injection.

Morpholine

Pharmacology and toxicology This product is a peripheral dopamine receptor blocker, directly acting on the gastrointestinal wall, can increase the lower esophageal sphincter tone, prevent gastro-esophageal reflux, enhance gastric peristalsis, promote gastric emptying, coordinate gastric and duodenal motility, inhibit nausea and vomiting, and effectively prevent bile reflux without affecting gastric juice secretion. It is not easy to pass the blood-cerebrospinal fluid barrier, and has no inhibitory effect on dopamine receptors in the brain, so there is no extrapyramidal system and other neurological and psychiatric adverse reactions.

Pharmacokinetics Rapid absorption after oral administration, peak blood concentration can be reached in 15-30 minutes. Distribution is highest in the gastrointestinal local drug concentration, followed by plasma, and almost none in the brain. The product is almost entirely metabolized in the liver, half-life (t1/2) is 7 hours, the total excretion through the urine is 31.23%, the prototype of the drug accounted for 0.4%; fecal excretion of the total 65.7%, the prototype of the drug accounted for 10%.

Indications 1.Relief of dyspeptic symptoms caused by delayed gastric emptying, gastrointestinal reflux, esophagitis, such as: epigastric flatulence, bloating, epigastric pain, belching, flatulence, heartburn in the mouth with or without refluxed gastric contents. 2. Treatment of nausea and vomiting caused by functional, organic, infectious, dietary, radiotherapy or chemotherapy.

Dosage Oral: 1. Adults: 10mg 3 to 4 times a day, the dose can be doubled if necessary or as prescribed by the doctor. 2.Children: 3～4 times a day, 0.3mg per kilogram of body weight each time, this product should be taken 15～30 minutes before meals.

Adverse reactions 1.Occasionally transient, mild abdominal cramps. 2. Sometimes serum prolactin levels are elevated, but normalize after discontinuation of the drug. The effect is similar to that seen with many other drugs.

Precautions

Pregnant and Nursing Women Use with caution in pregnancy.

Children The possibility of central side effects in infants under 1 year of age cannot be ruled out due to the imperfect development of their blood-cerebrospinal fluid barrier.

Drugs for elderly patients

Drug interactions Anticholinergic drugs may counteract the antidyspeptic effect of this product, so the two should not be combined.