Anxiolytics mainly act on the limbic system of the brain. They are mainly used to eliminate or reduce tension, anxiety, panic, stabilize mood and have a sedative-hypnotic effect. Commonly used anxiolytics mainly include benzodiazepine diazepam, nitrazepam, eszopiclone, alprazolam, clonazepam, lorazepam; new anxiolytics such as buspirone. Sedative-hypnotic drugs include scobarbital, chloral hydrate, etc.
Name
Specification and packaging
Character, usage and side effects
1
Diazepam, alias Valium, Valium
2.5mg*100
(Class II psychotropic drug, limited to 100 tablets)
It has sedative, hypnotic, anti-anxiety, anticonvulsant and muscle relaxation effects. Tmax is 60-90min, T1/2 is 35-50h. It is metabolized by the liver, partially converted into active norethindrone, and then combined with glucuronide and excreted in urine. Intravenous Valium is the drug of choice for the control of persistent epilepsy and is also used for alcohol withdrawal treatment. Injections for the treatment of anxiety and panic attacks can be injected 10-20 mg, and for the treatment of epilepsy can be immediately pushed 10-20 mg intravenously. oral anti-anxiety is generally 5-10 mg once, 3 times a day; for sleep can be 5-20 mg.
Side effects are mild, mainly drowsiness, vertigo, ataxia, tachycardia, etc. Note that alcohol should be avoided when taking the drug; contraindicated in patients with glaucoma and myasthenia gravis; prolonged use can lead to dependence and cognitive dysfunction. Benzodiazepine overdose can be treated by intravenous administration of benzodiazepine antagonist Advil.
2
Nitrozepam, alias Nitrozepam
5mg*100
(Class II psychotropic drug, limited to 100 tablets)
It has sedative, hypnotic, anti-anxiety and anti-epileptic effects. The hypnotic effect approximates physiological sleep, with fewer after-effects. It also has good effect on petit mal seizures and infantile spasms. Tmax is 0.5~5h, T1/2 is 21~30h. 5~20mg per night for hypnosis, 10~30mg per night for antiepilepsy, divided into doses.
The main side effects are occasional drowsiness, irritability, ataxia, vertigo, headache, constipation leukopenia, etc. Alcohol should be avoided while taking the drug, and prolonged use can lead to dependence.
3
Estazolam, alias Deprenyl Alprazolam Surazepam
1mg*20
1mg*100
(Class II psychotropic drug, limited to 100 tablets)
It has sedative, hypnotic, anti-anxiety and anticonvulsant effects, with weak central skeletal muscle relaxation effects. Mainly used for insomnia, anxiety, tension, fear and other disorders. Sedative-hypnotic effect is 2.5 to 4 times stronger than nitrazepam. Bitter taste, insoluble in water used. tmax is 1 to 2h, T1/2 about 17h. hepatic metabolism, metabolites are active, renal excretion is slow. Orally, for sedation, 1 to 2mg/d, 1 to 3 times/d; for insomnia, 1 to 4mg at bedtime.
The main side effects are slight weakness, dry mouth, drowsiness and dizziness. Use with caution in patients with hypertension, pregnant women, infants, and hepatic and renal insufficiency. Prolonged use can lead to dependence.
4
Alprazolam, alias Jiajing Valium Xanax
0.4mg*20
0.4mg*100
(Class II psychotropic drug, limited to 100 tablets)
It has sedative and hypnotic effects, and also has certain tricyclic antidepressant effects, with fast action, small dose and small side effects. It also has a central muscle relaxation effect. It is suitable for anxiety, depression, intractable insomnia, epilepsy and preoperative sedation. Tmax is 1~2h, T1/2 is 12~15h. The main metabolites are 3-hydroxymethyltriazolium and 3-hydroxy-5-methyltriazolium, the former activity is half of the original drug, the latter inactive. 80% is excreted from urine, can pass the placental barrier and excreted from breast milk. For hypnosis, 0.4-0.8mg at bedtime; for anxiety and depression, 0.4-0.8mg/time, 3 times/d, maximum daily dose 4-5mg/d.
Adverse reactions are low, mainly fatigue, dizziness, headache, dry mouth, constipation, nausea, excessive sweating, tachycardia, hypotension, tremor, etc. Pregnant women, nursing mothers, glaucoma patients are prohibited or cautious to use, and prolonged use may lead to dependence.
5
Clonazepam, alias Clonazepam
2mg*100
1mg/ml
(Class II psychotropic drug, limited to 100 tablets)
It has strong sedative, hypnotic, muscle relaxation, control of psychomotor excitement, antiepileptic and anxiolytic effects. It can be used as an adjunctive treatment for anti-mania and tic obscura syndrome. Slightly soluble in water, rapidly absorbed orally, Tmax is 1~2h, T1/2 is 19~30h duration of action 5~7h. Hepatic metabolism to acetamide derivatives, excreted from urine in the form of glucuronide sulfate conjugate. For hypnosis, take 1-4mg at bedtime. 1-2mg for excitement control by sedation or intramuscular injection, reduce for elderly. For anti-epilepsy, take 4-8mg/d orally in divided doses up to 20mg/d; 1-4mg/d by sedative injection, slowly pushed over 30sec, or by sedative dosing if necessary.
The main side effects are drowsiness, ataxia, fatigue, vertigo, slurred speech, decreased muscle tone, salivation, and gastrointestinal reactions. Transinfusion has an inhibitory effect on heart rate and respiration. It is teratogenic and is contraindicated in pregnant women. Forbidden in patients with hepatic and renal insufficiency and glaucoma. Long-term use may lead to drug dependence. Sudden discontinuation of the drug may cause seizures.
6
Flurazepam, alias Fluazepam, trade name Toluenda
15mg*100
(Class II psychotropic drug, limited to 100 tablets)
It mainly acts on the parts of the limbic system related to emotion, and has a weak inhibitory effect on the brainstem reticular activating system. It has good efficacy in insomnia caused by anxiety. Used to improve sleep and sedation, the effect is 1/4 of that of Valium, but the anxiety relief effect is 8 times that of Valium, applicable to anxiety and various types of insomnia, can shorten sleep induction time and prolong sleep, maintain sleep for 7-8h. easily soluble in water, Tmax=1h, T1/2 about 23h. because of the long T1/2, the hypnotic effect is enhanced on the 2nd to 3rd day of continuous use, and still has a hypnotic effect 1 to 2 days after stopping the drug Hypnotic effect. It is rapidly metabolized by the liver and the main metabolite, N-1-Hydroxyethylfluprednisolone, has a T1/2 of 47-100 h. The metabolites are excreted in the urine. Take 15-30mg/time orally, before bedtime. 15mg/dose for the elderly and infirm.
Common side effects are drowsiness, vertigo, dizziness and ataxia. There may also be gastrointestinal reactions, chest pain, arthralgia, palpitations and urinary tract reactions. Contraindicated with pregnant women, adolescents under 15 years of age, deep use in patients with severe depression, hepatic and renal insufficiency. Note that alcohol should be avoided when taking the drug; prolonged use can lead to dependence.
7
Triazolam Triazolam, trade name Helocin Soundexin
0.25mg*50
(Class I psychotropic drug, limited)
It has significant sedative, anti-anxiety and hypnotic effects. It has rapid sleep-inducing effect, short half-life, fast excretion, no accumulation effect and no drowsiness effect. The hypnotic effect is 45 times stronger than that of Valium, which can shorten the waking period and prolong the stage I sleep, and has less effect on stage II and III sleep. It is mainly used for anxiety and insomnia, especially for those who have difficulty in falling asleep. It is easily absorbed orally, difficult to dissolve in water, Tmax is 1.5±0.7h, T1/2 is about 2.7h. It is metabolized by liver, there are six kinds of metabolites, but only 7α-hydroxytriazolam is active, mainly excreted by kidney, 8% has fecal excretion. It can be excreted through the placental barrier and from breast milk. Anxiolytic treatment oral 0.25-0.5mg/dose, 3 times/d. High dose use for no more than 2 consecutive weeks.
The main side effects are fatigue, weakness, dizziness, drowsiness, blurred vision, etc. Use with caution in the elderly and in patients with hepatic or renal insufficiency. Easy to develop drug dependence and drug seeking behavior.
8
Lorazepam Lorazepam, alias Chlordiazepoxide Lorazepam, trade name Lola
0.5mg*20
0.5mg*100
(Class II psychotropic drug, limited to 100 tablets)
It has central sedation, anticonvulsant and muscle relaxation effects, and has strong anxiolytic and hypnotic effects. Mainly used for anxiety, insomnia, has a significant sleep-inducing effect, can make sleep last 8h. easily absorbed orally, insoluble in water, Tmax = 2h, T1/2 about 10-18h. hepatic metabolism, metabolites combined with glucuronic acid, excreted by the kidneys, renal disease generally does not affect the clearance rate. Anxiolytic treatment oral 0.5-2mg/dose, 3 times/d. High dose use for no more than 2 consecutive weeks.
The main side effects are fatigue, dizziness, drowsiness, etc. No cardiovascular system adverse reactions, there is a mild respiratory depression effect. Use with caution in pregnant women, children, and those with hepatic or renal insufficiency. Long-term use may lead to drug dependence.
9
Midazolam, alias Imipramine, trade name Lixin
15mg*20
(Class II psychotropic drug, limited to 100 tablets)
Short-acting sedative with sedative, anti-anxiety, hypnotic, muscle relaxation and anticonvulsant effects. Fast acting, fast metabolic inactivation, short duration, with obvious sleep-inducing effects. It is mainly used for insomnia and sleep rhythm disorders. It is easily absorbed orally, dissolved in water, Tmax=0.5h, first pass effect 40%, T1/2 about 2h. Hepatic metabolism, metabolite α-hydroxyimidazolam rapidly combined with glucuronide inactivation, excreted by kidney. After 7h of administration, there is no residual effect in the body, so it has almost no effect on hepatic insufficiency and the elderly. It is administered orally 7.5 to 15 mg/dose at bedtime.
Side effects are rare, but amnesia may occur at the beginning of the dosing period, and drug dependence may occur in susceptible patients.
10
Buspirone, trade name Bespar
Yishu Kibit
5mg*20
Aromatic piperazine anxiolytics. It mainly acts on hippocampal 5-HT1A receptors and D1 receptors, reducing the ability of 5-HTergic neurons and producing anxiolytic effects. It can also reduce the sensitivity of 5-HT2 receptors in the body, so it also has an antidepressant effect. It is a highly selective anxiolytic drug and does not have sedative-hypnotic effects. It has no effect on neuroendocrine function and is suitable for acute and chronic anxiety states. It has good effect on anxiety agitation, inner instability and nervousness, and is also effective for anxiety with mild depression. It is easily absorbed orally, Tmax is about 0.5~1h, T1/2 is about 2~11h. Most of it is metabolized by the liver, the main metabolites are 5-hydroxybutanedione and 1-pyrimidinopiperazine, the latter is partially active. 60% is excreted by urine, 40% by feces. It is taken orally at a dose of 5mg/d, 3 times/d, gradually increasing to 20-30mg/d, with a maximum dose of 60mg/d. In the elderly, the dose should not exceed 15mg/d.
The main side effects are gastrointestinal discomfort, nausea, diarrhea, headache, vertigo, agitation, insomnia. Contraindicated in severe liver and kidney disease, glaucoma, myasthenia gravis, and pregnant women. It should not be used with alcohol, antihypertensive drugs, hypoglycemic drugs, anticoagulants, contraceptives, MAOI.
It does not produce synergistic effects with other hypnotic drugs, nor does it enhance the effects of alcohol. It does not eliminate withdrawal reactions to addictive drugs, nor does it produce drug dependence and withdrawal reactions.
11
Zolpidem Zolpidem, trade name Synthroid Lotan Norbine
5mg*40
10mg*6
10mg*20
(Class II psychotropic drug, limited to 100 tablets)
Acts selectively on the ω1 receptor subtype for the short-term treatment of insomnia. In small doses, it shortens the time to fall asleep and prolongs the duration of sleep; in large doses, the duration of second, third and fourth phase sleep and REM latency are prolonged and REM time is shortened. Tmax of zolpidem is about 0.3-3h, T1/2 is about 2.4h (0.7-3.5h), the effect can be maintained for 6h, and the hepatic first pass effect is 35%. Urinary excretion 56%, fecal excretion 37%. The recommended dose for adults is 10mg at bedtime, not exceeding 20mg, starting from 5mg for the elderly or those with hepatic insufficiency. The course of treatment can be from a few days to 1 year.
Effects on the central nervous system and gastrointestinal motility are most likely to occur in the elderly. They include sleepiness, dizziness, headache, nausea, diarrhea, vertigo, and rarely, memory impairment (paracrine amnesia), nocturnal irritability, depression, disturbance of consciousness, diplopia, tremor, and choreographic gait. Contraindicated in obstructive sleep apnea syndrome, myasthenia gravis, severe hepatic insufficiency, acute respiratory insufficiency with respiratory depression, pregnancy and lactation.
12
Zopiclone, trade name Imovan 忆梦返
Sanchen
7.5mg*10
7.5mg*20
Zopiclone is a piperazine carboxylate anti-anxiety drug. It can bind to BZ receptors and has anxiolytic, anticonvulsant and muscle relaxant effects similar to BZ class. It can improve sleep and make sleep prolonged to reduce the number of awakenings. Used in the treatment of insomnia. tmax is about 1.5-2h, T1/2 is about 5h, can be prolonged to 8h in cirrhosis and elderly patients, T1/2 is not prolonged in renal failure patients. Hepatic metabolism, the main metabolites are N-desmethyl and N-oxidation derivatives, with low activity. Urinary excretion 80%, fecal excretion 10%. Taken at bedtime, the recommended dose for adults is 7.5-15mg/dose, taken 30min before bedtime.
Adverse reactions are rare, commonly morning drowsiness, bitter mouth, dry mouth, muscle weakness, etc. Withdrawal symptoms may occur when the drug is suddenly stopped after long-term use. Severe respiratory insufficiency and hypersensitivity to this drug are prohibited, and it is not recommended for pregnant and lactating women. The dose should be reduced in patients with hepatic insufficiency.
13
Chlormezanone, alias Fenaluron
200mg*20
Thiazide and thiazole derivatives anxiolytic, intramedullary polysynaptic reflex inhibitor. Has weak sedative and muscle relaxing effects. Used for sleep disorders, anxiety and tension. Also used in the treatment of migraine. Slightly soluble in water, T1/2 about 29h. 200mg/dose orally for adults, 2-3 times/d.
There are side effects such as drowsiness, flushing, drug rash, anorexia and depression. Not suitable to be combined with phenothiazines and MAOI.
14
Hydroxyzine, alias Atarax Antalax Antalax
25mg*100
Diphenylmethane derivative anxiolytic, subcortical activity inhibitor, with weak anxiolytic, sedative-hypnotic, central muscle relaxation, anticholinergic (antispasmodic) and antihistamine effects. Used for nervousness, anxiety, agitated neurosis and anxiety associated with gastrointestinal disorders, also for hypnosis and psychosomatic disorders, such as chronic allergic skin diseases. It is easily absorbed orally, Tmax=3h, T1/2 14-33h for young adults, 18-48h for over 60 years old. 95% is metabolized in the liver, the main metabolites are demethylated, 8-hydroxylated and N-oxidized derivatives, the first two are active and mainly excreted in the urine. It is administered orally 25-50mg/dose, 2-3 times/d.
Adverse effects include drowsiness and dizziness. Use with caution under 6 years of age.
15
Phenobarbital, alias Luminal
30mg*100
500mg/ml
(Class II psychotropic drug, limited to 100 tablets)
Long-acting barbiturate antiepileptic drugs. Used for grand mal seizures, persistent status and limited seizures. Poor efficacy for petit mal seizures. Also has sedative and hypnotic effects and can be used for anxiety, hyperthyroidism, hypertension, nausea, etc. Oral Tmax2～18h, injection Tmax about 15min, T1/2 about 72～96h, children about 40h, part of the liver metabolism, converted into inactive products, 30% in the form of prodrug through the kidney excretion, can be reabsorbed by the renal tubules, so that the action time is prolonged. The concentration in breast milk is 10%-30% of blood concentration. Oral 15~100mg/time, 30~200mg/d, up to 250mg/time or 500mg/d in divided doses. Intramuscular or sedative injection, 100-250mg/d, 1 to 2 times/d, up to 250mg/d or 500mg/d. For grand mal seizures commonly used, easy to change from intramuscular to oral.
Side effects include drowsiness, irritability, ataxia, drug-related liver damage, rash, respiratory depression, and coma. Long-term application can lead to drug dependence, and sudden discontinuation of the drug can cause seizures. Toxicity can be excreted through blood and peritoneal dialysis.
16
Secobarbital, alias Seconol
0.1g*10
(Class I psychotropic substance, limited to 10 tablets)
Short-acting barbiturates are sedative-hypnotics. Fast-acting, can fall asleep in 15-20 min, and the duration is also short. Mainly used for patients who have difficulty sleeping. Slightly soluble in water, easily soluble in ethanol. Mainly metabolized by the liver and excreted by the kidneys. Take 0.1~0.2g orally before bedtime.
Adverse reactions mainly include dizziness, drowsiness, a few patients may have rash, drug fever and other allergic reactions, can inhibit breathing, overdose can lead to poisoning. It is easy to cause drug dependence, and long-term use should not be suddenly discontinued to avoid withdrawal reactions. Use with caution in patients with reduced liver and kidney function.
17
Chloral Hydrate, simple C.H.
10％*100ml
(Psychotropic drug, limited to 200ml)
It has strong hypnotic and anticonvulsant effects, safe and effective, and not easy to accumulate poisoning. It can be taken for 10-20min to fall asleep, and can last for 6-8h without discomfort after waking up. It is mostly used for severe insomnia, h