emir
amfepramone
Orlistat
benzotriazole
P-chlorobenzylamine
Fluamphetamine
Fenmei Quqin
Fentamine
Mazindol
Sibutramine
Dexamphetamine
phenbenzamine
amphetamine
The following is a detailed introduction, please have a look and think about it:)
1. Amphetamines:
After the advent of amphetamine, one of its greatest uses is to treat obesity. Some appetite suppressants are mostly related to amphetamines, mostly central nervous system stimulants, and also have metabolic effects. There is a hunger (or eating) center in the hypothalamus with JBOY3 adrenergic receptor, while the satiety center has an adrenergic receptor. Amphetamines and drugs with similar structures directly act on the satiety center, leading to loss of appetite. This effect has been confirmed in animals.
2.Amires Aminorex:
It has been proved that the drug can cause obstructive pulmonary arterial hypertension and lead to death, which is characterized by explosive and rapid development into fatigue dyspnea, chest pain and fatigue collapse, without the usual cause of pulmonary vascular disease. Other appetite suppressants may also be complicated with primary pulmonary hypertension. There are two cases of pulmonary hypertension, of which 1 case used this drug 6 years ago, and 1 case was found after taking it 8 years. Seventy-five patients with symptoms of primary pulmonary hypertension were followed up for an average of 9 years, among which 46 patients had taken appetite suppressants (alone or in combination with other appetite suppressants). There is no difference in their long-term survival rate whether they take appetite suppressants or not. The main symptoms of 22 patients with primary pulmonary hypertension caused by appetite suppressants were dyspnea (22 cases), arrhythmia (20 cases), peripheral edema (18 cases), dizziness (15 cases), cyanosis (14 cases) and chest pain (65438 cases). About 30% patients who have taken appetite suppressants can relieve their long-term symptoms, because patients with primary pulmonary hypertension caused by appetite suppressants adapt better than those who are not caused by drugs.
3. amfepramone, amfepramone: (diethyl acetone)
counteraction
The incidence of adverse reactions of this drug is very inconsistent. The incidence of a group of 90 obese people was similar to that of the placebo group. A group of 95 cases, 25 mg three times a day, with a course of treatment of 65438 06 weeks. The main adverse reaction is nervousness. 12 1 obese patients were given short-acting preparations for an average of 4.4 months and followed up for more than 3 years. The incidence of adverse reactions was less than 9%, 2 cases were nausea and dizziness, 2 cases were nervousness and palpitation, and 3 cases stopped taking drugs because of nausea, insomnia and abnormal sensation. 102 cases were treated with long-acting preparation 16 weeks, and they appeared tension, nervousness, nausea, dizziness and dry mouth. 50 pregnant women were treated with sustained-release preparation by double-blind method. The main adverse reactions were euphoria, sweating, excitement and palpitation. Another group of 75 pregnant women had symptoms of nervousness and insomnia. These reported adverse reactions are not serious, and there is no need to stop taking the drug. It is reported that this drug is addictive and has psychotic symptoms, but it is rare and less common than amphetamine or phenylpentylenetetrazol. A group of 20 overweight women received 6 weeks' diet and 75 mg/d of the drug. There were 65,438+02 cases of dry mouth at least once, 6 cases of headache, 5 cases of nervousness or irritability, 4 cases of constipation and 3 cases of nausea and vomiting. There were 12 cases of urine ketone body positive at least 1 time, 5 cases had no adverse reaction, and only 1 case stopped taking medicine in the third week because of palpitation. The effect of this drug on the central nervous system is not as common as dextroamphetamine. Patients who must stop using amphetamines and benadryl can continue to be treated with this drug. Insomnia is not common if they take it every morning. The drug 75 mg combined with diazepam 10 mg has fewer adverse reactions than any other appetite suppressant. But about 50% patients have adverse reactions, such as dry mouth, nervousness and mild depression.
Prevention and treatment of adverse reactions
(1) Mental depression, epilepsy and pregnant women are prohibited.
(2) Because it has little influence on cardiovascular system, it can be used for obese patients with mild cardiovascular diseases.
(3) Use with caution in patients with hyperthyroidism; Aerial work and careful use by drivers; Use with caution in patients with glaucoma.
(4) Low-calorie diet should be adopted during treatment.
(5) It is not advisable to take medicine intermittently during treatment; Although it is not addictive, long-term use, especially excessive use, will lead to dependence, so you can't stop taking drugs suddenly.
Orlistat Orlistat:
This product is a long-acting and powerful specific gastrointestinal lipase inhibitor. It forms valence bonds with serine sites of gastric lipase and pancreatic lipase in the stomach and small intestine cavity, thus inactivating the enzymes and playing a therapeutic role. Inactivated enzymes cannot hydrolyze fats (mainly triglycerides) in food into absorbable free fatty acids and monoacylglycerol. Undigested triglycerides cannot be absorbed by the body, thus reducing calorie intake and controlling weight. This drug does not need to be absorbed by the whole body to exert its efficacy.
Adverse reactions mainly cause gastrointestinal adverse reactions, which are related to the pharmacological effect of drugs to prevent fat absorption. Common adverse reactions include oil spots, increased gastrointestinal exhaust, urgency of defecation, fatty stool, fatty diarrhea, increased stool frequency and incontinence. With the increase of dietary fat, the occurrence of the above situation also increases accordingly. Patients should be informed of the possibility of gastrointestinal reaction and how to deal with it correctly, such as improving diet structure, especially controlling fat content. Low-fat diet can reduce the possibility of gastrointestinal side effects and help patients detect and adjust their fat intake. These gastrointestinal adverse reactions are usually mild and short-lived, and they appear in the early stage of treatment (the first 3 months). Most patients have only one adverse reaction. Usually, the gastrointestinal reactions of patients taking this medicine are abdominal pain/discomfort, flatulence, watery stool, soft stool, rectal pain/discomfort, and dental and gingival discomfort. Other rare adverse reactions observed include upper respiratory tract infection, lower respiratory tract infection, influenza, headache, menstrual disorder, anxiety, fatigue and urinary tract infection. There are occasional reports of allergic reactions to this product after marketing. The main clinical manifestations are itching, rash, urticaria, angioneurotic edema and allergic reaction.
In the study of animal reproduction of pregnant and lactating women, no embryotoxicity and embryo malformation related to orlistat were observed. No embryo malformation was found in animal research, and it is expected that orlistat will not have teratogenic effect on humans. In any case, it is not recommended to take this product during pregnancy without clinical data. Whether orlistat is secreted in human milk has not been studied. Therefore, this product should not be taken when breastfeeding.
The safety and efficacy of this product for children under 18 years old have not been studied.
Adverse reactions caused by overdose of this product have not been reported. Studies on normal weight and obesity showed that 800mg and 400mg of this product were taken orally three times a day for 15 days, and no obvious adverse reactions were found. And obese people have taken this product 240mg, three times a day for six months, and no obvious adverse reactions have been found. If there is a serious overdose, the patient should be observed for 24 hours. According to human and animal experiments, it is rapid and reversible for orlistat to inhibit the systemic reaction caused by lipase.
Drug Interaction In the pharmacokinetic study, no drug interaction between orlistat and alcohol, digoxin, metformin, nifedipine, oral contraceptives, phenytoin, statins or warfarin was observed. It is observed that the absorption of vitamins D, E and β -carotene will be reduced when taken with this product. If you need to take multivitamins, you should take it at least 2 hours after taking this product or before going to bed. When taking this product at the same time, the plasma concentration of cyclosporine A decreased. Therefore, when this product is administered with cyclosporine A at the same time, the monitoring of the blood concentration of cyclosporine A should be strengthened.
Prevention and treatment of adverse reactions are prohibited for patients with chronic malabsorption syndrome or cholestasis and allergic to this product or any other components in pharmaceutical preparations. After less than two years of orlistat treatment, the levels of vitamins A, E, K and β -carotene in most patients are still within the normal range. In order to ensure adequate nutrition, you can consider supplementing multivitamins. Patients should be educated to follow dietary guidelines. When this product is combined with a high-fat diet (for example, 2000 calories a day, more than 30% is supplied by more than 67g of fat), the possibility of gastrointestinal reaction will increase. The daily fat intake should be distributed among three meals. When this product is taken with a high-fat diet, the possibility of gastrointestinal reaction increases. In patients with type 2 diabetes, this drug can lead to weight loss, often accompanied by improvement of blood sugar control, so it is possible or necessary to reduce the dosage of oral hypoglycemic drugs (such as sulfonylureas).
4. Benzotriazine p-dimethyltetrazine:
The adverse reactions of this medicine include glossitis, stomatitis, dry mouth, nausea, abdominal pain, muscle contracture, constipation, dysuria and headache. This drug is metabolized into phenylhydrazine in human body and abused in some countries.
5. p-Chloropropylamine Chloropropylamine:
The T 1/2 of the drug is about 5 days, and there is a risk of accumulation after continuous administration. The exciting effect of this drug on the central nervous system is not as good as that of dextroamphetamine, and dizziness, tremor, anxiety, tension and insomnia are not common. After taking this medicine, the patient is sleepy and may have pulmonary complications. It can lower systolic blood pressure, while phentermine can increase heart rate. Twenty-five patients took this drug 25mg three times a day, and the incidence of constipation and dry mouth was higher than other appetite suppressants. Another report said that besides insomnia, increased physical activity and increased urination, constipation and dry mouth were more common among volunteers who used Fentamine.
6. Fenfluramine:
(Fluamphetamine, Obedrex, Pinus ponderosa)
Fenfluramine is similar to amphetamine in structure, but the usual dose does not excite the central nervous system. In the double-blind study, the main adverse reactions were sedation and drowsiness, abdominal discomfort and dry mouth, which were generally not serious and rarely needed to be stopped. At high doses, the above reactions are more serious and common, especially drowsiness and abdominal discomfort, including abdominal cramps; Although dizziness, dizziness and headache are not common, they are occasionally serious. No reports of allergic reaction and carcinogenesis were found.
A few patients with cardiovascular system may have increased or aggravated blood pressure, and the blood pressure will return to normal after drug withdrawal. Blood pressure may not necessarily rise again when taking the medicine again.
Two women with respiratory system developed progressive pulmonary hypertension after taking the drug for 8 months, and the symptoms and ECG findings disappeared after stopping taking the drug. Among them, 1 case developed symptoms after re-medication. Therefore, any patient should regularly observe whether the exercise tolerance decreases when using this drug.
Sedation, drowsiness, dizziness and headache are common in the nervous system. Nine healthy people took 80 mg * * * * every day for three weeks. Some people have symptoms such as decreased attention, insomnia, apathy and disintegration in the first week after taking it, but their mood has not changed. Depression can occur during treatment, but it is most common within a few days after sudden withdrawal. About 20% patients will have dizziness, nausea, anxiety and other symptoms after suddenly stopping taking drugs. Depression or excitability may occur after stopping the drug suddenly, which may be caused by the rapid decrease of serotonin, because the central role of this drug is mediated by serotonin. Chronic mental patients go to normal sleep after taking 40 or 80 milligrams of this drug, but wake up a few hours later because of a special feeling of uneasiness and can't fall asleep again until dawn. 1 case took 2 tablets of this medicine during the day and had nightmares at night; The next morning, I switched to 1 film, and the nightmare disappeared. Fifty obese women were treated with this medicine for more than 20 weeks, and gradually increased to 160mg per day, and then decreased, and about half of the patients had more dreams. It is reported that dreams increase with small doses. In susceptible patients, the drug can induce psychosis, and mania and schizophrenia have been reported 1 case. 1 case with a history of schizophrenia was treated with phenothiazine and imipramine for 2 years. In the third week after giving this medicine 40mg every day, schizophrenia broke out, probably because of the interaction between drugs. 1 A 43-year-old woman took this medicine 1 tablet, and her head and neck moved backward, accompanied by tongue and throat muscle spasm; No bronchospasm or other physical abnormalities; Recover immediately after intravenous diphenhydramine injection. Occasionally, it has been reported that male patients have impotence after taking this medicine and disappear after stopping taking it. At high dose (240 mg per day), the incidence of sexual desire loss is very high, especially in women.
Diarrhea, dry mouth and nausea will occur in the digestive system.
Hematopoietic system 1 A 46-year-old female was treated with this drug, and her hemoglobin decreased to 5.1g%, and the direct Coombs test was positive. After prednisone infusion, Combs test turned negative and the patient recovered. There are still 2 cases of anemia caused by the combination of this drug and propranolol in the literature.
Endocrine and metabolism The drug can significantly and slightly improve glucose tolerance, reduce fasting blood cholesterol and 13 lipoprotein. All the metabolic effects of this drug are slight, and its clinical importance is questionable. Occasionally shivering, grinding teeth, baldness. The risk of liver disease will affect the metabolism of this drug. People with endogenous depression tendency had better avoid using this medicine.
The range of overdose is 30 ~ 90 tablets, equivalent to 400 ~ 800 mg, which can cause poisoning. Clinical manifestations, common lethargy, semi-coma with muscle spasm and chills. Other symptoms include dilated pupils, unresponsiveness, nystagmus, hyperreflexia, chin tremor and possible high fever (which may be the main manifestation), which can be recovered quickly and naturally. It is reported that children died of ventricular fibrillation or cardiac arrest caused by poisoning. 1 case 17-year-old girls died 3 hours after taking 1600mg, and some died 3 hours after taking 1200mg sustained-release agent. The main clinical manifestations are agitation, tachycardia (rapidly developing into arrhythmia), convulsion and cardiac arrest.
Among the 438 drug addicts, 60 have a history of drug abuse. In addition, 8 cases were reported to have mental illness, taking 240 mg daily. After using this drug for 6 ~ 12 months, the drug resistance to anorexia may appear, and the tolerance to adverse reactions will soon appear.
In the animal experiment of drug interaction, this drug interacts with halothane. 1 The woman who used the drug died during anesthesia, so the drug should be stopped one week before operation. This product combined with monoamine oxidase inhibitor can produce acute mental disorder.
Prevention and treatment of adverse reactions
(1) Mental depression, epilepsy and pregnant women are prohibited.
(2) Severe arrhythmia, aerial workers, drivers, etc. It should be used with caution.
(3) Don't take the medicine intermittently during the treatment, and gradually reduce it in the last 4 ~ 6 weeks of the course of treatment until the drug is stopped. It is not advisable to stop taking drugs suddenly. Continuous medication time should not exceed 6 months, otherwise drug resistance and dependence will easily occur.
7. Fenmei Quqin Benzachuan:
(Preludin)
The average dose of this drug can be regarded as nervousness, overexcitation, pleasure and insomnia, but it is less common than dextroamphetamine. There are dizziness, headache, nausea, dry mouth and urticaria. Adverse reactions are more obvious at high doses; Paranoid psychosis may happen to addicts; And taking it for a long time sometimes leads to psychotic symptoms. Poisoning by this medicine can cause encephalopathy accidents. Long-term use found 2 cases of central nervous system damage, 1 case of diffuse damage, 1 case of hemiplegia and sensorimotor aphasia. It is reported that pregnant women take this medicine, and in rare cases, newborns have congenital defects. This drug is widely abused or misused in some countries, sometimes through intravenous injection. Taking this drug, former morphine addicts will feel comfortable and overconfident.
8. Fentamine:
(Ponte, Milla)
The adverse reaction of this drug in exciting the central nervous system is less than dextroamphetamine. 177 cases, 16 cases (9%) stopped taking drugs due to adverse reactions. In 13 young healthy volunteers, 2 of them stopped using because of intolerance. Insomnia is the most common adverse reaction, with the incidence of 19.9% in one group and 6.2% in the placebo group. 1 A 26-year-old schizophrenic woman, after taking 240mg once, developed acute mental structure destruction, accompanied by dilated pupils, tachycardia and anxiety. 1 A 32-year-old man took this drug for 4 months (dosage unknown) and developed fatal pulmonary hypertension.
9. Mazindol:
(Sanorex)
Adverse reactions The drug is a tricyclic compound, which has the function of exciting the central nervous system, and is quite similar to amphetamine. 23 cases were given high dose (6 mg/d), and 30% patients had central nervous system reaction. However, 22 amphetamine-dependent patients were given this drug, causing slight amphetamine-like effects. The therapeutic dose does not produce mental pleasure, and its addiction is less than that of amphetamines, and no withdrawal reaction has been reported. The most common adverse reactions in 274 cases were dry mouth, nausea, insomnia, constipation, headache and dizziness. Anxiety and lethargy occurred in 4 cases. The incidence of adverse reactions was high after the drug was started, and gradually decreased after treatment 12 weeks. 50 obese patients were studied by double-blind method. Adverse reactions are mild, such as dry mouth and constipation. Only 1 case had angioneurotic edema, and the rest 1 case had peripheral edema and vomiting. Another group of 60 obese patients were treated with double-blind method 12 weeks, and the adverse reactions were very light, only insomnia and nausea. When drugs are used for a long time and given a low-calorie diet, the incidence of adverse reactions is high and serious. Among 40 obese diabetic patients with stable control, only a few people experienced mild dry mouth and dizziness when treated with this drug. After using this drug for 3 weeks, healthy people showed decreased attention, but their mood was not good. Peripheral adverse reactions were more than central adverse reactions, and had no effect on postural blood pressure and heart rate. However, there are also reports that drug-dependent heart rate increases, which may be due to the role of amphetamine-type drugs. About 5% of women treated with this medicine have aphrodisiac effect, but other researchers have not confirmed it.
Prevention and treatment of adverse reactions
(1) It is forbidden for people who are allergic to this product.
(2) Patients with severe renal, liver and cardiac insufficiency, arrhythmia, severe hypertension, overexcitation and glaucoma are prohibited.
(3) taking antihypertensive drugs such as guanethidine and betaine that are banned at the same time; Do not take monoamine oxidase inhibitors during use or within two weeks after use.
(4) Obesity caused by organic diseases is prohibited.
(5) The use of insulin and hypoglycemic drugs may affect the curative effect of diabetic patients, so the metabolic status of patients should be monitored during the treatment, and the dosage of insulin and hypoglycemic drugs should be adjusted appropriately when necessary. Patients with hypertension should pay attention to blood pressure monitoring when using it.
(6) It may increase the effect of exogenous catecholamine, so the cardiovascular system reaction of patients should be closely monitored when using adrenaline drugs.
(7) It is exciting and should be used with caution by drivers or machine operators.
(8) Do not exceed the prescribed maximum dose to try to increase the curative effect. The normal course of treatment is generally 2 ~ 3 months, and some cases have achieved remarkable results in a short course of treatment. Blood picture and liver and kidney function should be checked before and after taking it.
10. sibutramine
counteraction
(1) The adverse reactions were dry mouth, anorexia, insomnia and constipation.
(2) Other adverse reactions with incidence ≥ 1% include fever, increased heart rate, elevated blood pressure, dyspnea, diarrhea and gastroenteritis.
(3) This product can cause abnormal liver function, which often disappears with further treatment, and there is a clear dose-response relationship.
(4) In addition, limb spasms, increased tension, abnormal thinking, seizures, interstitial nephritis, menstrual disorder and peripheral edema can also be seen; Arthritis, itchy skin, abnormal sensation, amblyopia and other reactions.
Drug Interaction Central Nervous Active Drugs: This product cannot be used together with monoamine oxidase inhibitors. Monoamine oxidase inhibitors should be discontinued for at least 2 weeks before starting to use this drug. Similarly, this product should be stopped for at least 2 weeks before using monoamine oxidase inhibitors.
This product can inhibit the reuptake of 5- hydroxytryptamine, so it is not suitable to be used with other 5- hydroxytryptamine drugs.
Drugs that affect blood pressure and heart rate: Patients who are taking drugs containing norephedrine, ephedrine or pseudoephedrine should use this product with caution.
Drugs for inhibiting cytochrome P450(3A) metabolism: Clinical trials show that this product has potential interaction with ketoconazole and erythromycin, but the effect is not significant.
Prevention and treatment of adverse reactions
(1) Patients receiving monoamine oxidase inhibitor (MAOI) are prohibited.
(2) Patients receiving other central appetite suppressants are prohibited.
(3) Patients with anorexia nervosa are prohibited.
(4) Those who are allergic to the ingredients of this product are prohibited.
(5) Patients with hypertension whose blood pressure cannot be controlled or is not well controlled are prohibited.
(6) Patients with coronary heart disease, heart failure, arrhythmia and stroke are prohibited.
(7) Patients with severe liver and renal insufficiency are prohibited.
(8) The treatment of obesity should focus on diet control and exercise.
(9) Obesity caused by Cushing's syndrome and hypothyroidism should be excluded from the application scope of this product.
(10) Use with caution in patients with a history of hypertension.
(1 1) Because it may increase or aggravate the formation of gallstones, patients with gallstones should use this product with caution.
(12) This product can cause mydriasis, so it should be used with caution in patients with angle-closure glaucoma.
(13) Use with caution in patients with epilepsy, and patients with epilepsy should stop using it.
(14) may affect judgment, thinking or motor skills.
Dexamphetamine:
(dexamethasone, dexamethasone)
This drug is in danger of abuse and addiction, and it is no longer widely used as an appetite suppressant. I felt happy after taking this medicine, but I felt depressed after the efficacy disappeared. Of the 347 cases, 23% were excited. The effect of this medicine on everyone is very different, and even a few people will feel sleepy. Menopausal women are prone to lethargy, irritability and sadness, not euphoria. Adverse reactions caused by excessive excitement of sympathetic nerve are quite common, but they are often not serious. Because it is addictive, we should be careful when using it to treat obesity. It is reported that hyperinsulinemia may occur after long-term use of the drug for several weeks.
Phenyl isopropyl benzylamine:
The medicine can suppress appetite, and can cause anxiety, insomnia and dizziness, gastrointestinal dysfunction (dry mouth and anorexia) and cardiovascular changes due to mental pleasure and other central nervous system excitement.
I hope my answer can help you, and I wish you good health:)