Antidepressants mainly act on the mesencephalon of the central nervous system, especially the hypothalamus, followed by the limbic system, with complex pharmacological effects. Commonly used antidepressants include tricyclics (such as amitriptyline, doxepin, promethazine, chlorpromazine, etc.), tetracyclics (such as maprotiline), monoamine oxidase inhibitors (such as phenelzine, moclobemide), selective pentraxin reuptake inhibitors (such as fluoxetine, paroxetine, sertraline, triazolone), etc.
Product Name
Specification and packaging
Properties, usage and side effects
1
Promethazine Imipramine
10mg*100
25mg*100
Tricyclic antidepressant (TCA), an NE/5-HT reuptake inhibitor, mainly blocks the reuptake of NE by the presynaptic membrane and blocks M, H1, and α1 receptors. It is used for various types of depression, especially those in which psychomotor retardation symptoms predominate. It is virtually ineffective in depressive states associated with schizophrenia and can worsen motor and anxiety depression. It is also used in pediatric enuresis, attention deficit hyperactivity syndrome, phobic states, and obsessive-compulsive disorder. It is readily absorbed orally and has a first-pass effect, with a Tmax of 1-4 h and a T1/2 of 19-24 h. The effective blood concentration is 150-225 ng/ml. The biologically active metabolites are desipramine, 2-hydroxyprometamol, and 2-hydroxydesipramine, which are inactivated when combined with glucuronide. Both the active metabolites and the prodrug can cross the blood-brain barrier and placental barrier and be excreted from milk. 70% is excreted from urine and 22% from feces.
Dry mouth, excessive sweating, constipation, blurred vision, urinary retention, intestinal paralysis, and electrocardiographic changes are common. A few appear hyperactive or induce mania and occasionally cause seizures. It can cause malformations in newborns. Contraindicated in patients with severe heart, liver, kidney disease, epilepsy. Use with caution in the elderly, patients with glaucoma, hypertension, and prostatic hypertrophy. Not to be used with monoamine oxidase inhibitors (MAOI), anticholinergics, and antihypertensives.
2
Clomipramine, alias Clomipramine, trade name Anafranil
10mg*30
25mg*30
25mg*48
Tricyclic antidepressant, an NE/5-HT reuptake inhibitor. It has antidepressant, anti-anxiety and anti-compulsive effects. It can eliminate depressed state of mind, arouse interest in work and social activities, uplift mood and rejuvenate. It is indicated for the treatment of depression, obsessive-compulsive disorder, phobias, and anxiety disorders. It is the drug of choice for obsessive-compulsive neurosis. Also used for phobias, anxiety disorders, panic attacks, chronic pain, etc. Easily absorbed orally with Tmax=4h and T1/2 of 17-28h (mean 21h). The effective blood concentration is 250-700ng/ml. the active metabolite is desmethylchlorpromazine. 2/3 is excreted in the urine and 1/3 in the feces. Oral 25-75mg/d, may be increased gradually, maximum not exceeding 300mg/d, divided into 2-3 doses.
The main side effects are slight weakness, drowsiness, dizziness, dry mouth, bitter mouth, constipation, poor appetite, blurred vision, and difficulty in urination. There may be postural hypotension, electrocardiographic changes, occasional skin allergy, abnormal liver function. Use with caution in advanced age, glaucoma, prostate hypertrophy; not to be combined with MAOI and anticholinergic drugs.
3
Amitriptyline, trade name Amitril
25mg*100
This product is a tricyclic, NE/5-HT reuptake inhibitor with strong antidepressant and sedative effects, and also enhances the effects of central depressants. It is suitable for depression of affective psychiatric disorder, menopausal depression, neurotic depression and depressive state of organic psychosis, and has satisfactory effect on depression with insomnia. It has the clinical characteristics of strong antidepressant effect and short effect time. It is easily absorbed orally, with Tmax of 8-12 h and T1/2 of 9-25 h. The effective blood concentration is 120 ng/ml. The active metabolite is nortriptyline. Excretion is slow, with 60% of the administered dose excreted in urine and feces in 72h. 70% is excreted in urine and 22% in feces. The dose of nortriptyline is 25-50mg/d orally at the beginning, divided into 3 doses, gradually increasing the dose to 150-250mg/d therapeutically and 50-150mg/d as a maintenance dose. The dosage for the elderly is generally 1/3 of that for adults.
The main side effects are dry mouth, drowsiness, dizziness, constipation, urinary distress, blurred vision, cardiac arrhythmia, postural hypotension, and some patients may have abnormal liver function. It is contraindicated in patients with severe heart disease, glaucoma, urinary retention and prostatic hypertrophy; it should not be combined with anticholinergic drugs and MAOI.
4
Doxepin Doxpine, alias Doxepin
25mg*100
Tricyclic antidepressant, an NE reuptake inhibitor. It has strong antidepressant, anxiolytic, sedative and hypnotic effects. Used for all types of depression, anxiety and depressive states. Antidepressant effect is inferior to promethazine and amitriptyline, but the sedative effect is obvious. The anti-anxiety effect mostly takes effect within 1 week, and the antidepressant effect mostly takes effect in 7 to 10 days. It is easily absorbed orally, with T1/2 ranging from 8 to 24h (mean 17h). The effective blood concentration is 100ng/ml, and the active metabolite is desoxepin, with T1/2 of 31-81h. It is rapidly metabolized, and most of it is excreted in the urine within 24h. The starting dose is mostly at 25mg, 2-3 times a day, and the commonly used dose is 150-300mg/d.
The main side effects include dry mouth, constipation, urinary retention, blurred vision, dizziness, palpitations, hypotension, nausea, vomiting, sweating, drug rash, photosensitivity, local edema, hypogonadism, etc. It is prohibited for patients with severe heart, liver and kidney diseases and epilepsy; it should not be used with anticholinergic drugs, antihypertensive drugs and MAOI.
5
Maprotilne, trade name Ludiomil
25mg*30
25mg*48
Tetracyclic antidepressant, inhibits the reabsorption of NE in presynaptic neurons and inhibits a small amount of 5-HT reabsorption, also has antihistamine effect and moderate anticholinergic and sedative effect. It has strong antidepressant effect and is a broad-spectrum antidepressant. It has a rapid effect and can relieve anxiety, depression and psychomotor block, and is suitable for various depressions. Oral absorption is slow but complete, with Tmax of 4-16h and T1/2 of 27-58h (mean 43h). Oral dose of 150mg/d reaches steady-state effective blood concentration of 100-400ng/ml in 2 weeks. metabolites are combined with glucuronide and about 2/3 are excreted from urine and 1/3 from feces. The starting dose is 50mg/d, and the therapeutic dose is 75-150mg/d, which can be taken in one dose or divided into 2-3 doses. Individual patients can increase to 300mg/d.
Side effects include dry mouth, constipation, blurred vision, tachycardia, dizziness, tremor, sleep disorders, skin irritation, and occasionally mania. 200mg/d or more has a high rate of seizure induction and should be monitored by EEG. Use with caution in patients with glaucoma, epilepsy, prostatic hypertrophy and cardiac, hepatic and renal dysfunction. May enhance the cardiovascular effects of NE, epinephrine, central depressants and anticholinergic drugs, and care should be taken when co-administered. Not suitable to be combined with MAOI.
6
Mianserin, alias Mianserin, trade name Tolvon Tolvan
60mg*30
Tetracyclic antidepressant, selectively blocks presynaptic membrane α2 receptors, also has strong 5-HT2, H1 receptor antagonism. Fast-acting, with antidepressant, sedative-hypnotic and anxiolytic effects. Used in various depressions, but less effective in endogenous bipolar depression. It has a sleep improving effect and is also used for anxiety and obsessive-compulsive disorders. It is readily absorbed orally, with Tmax=3h and T1/2 of 14-33h (33±15h over 60 years). Steady-state blood concentrations are reached in 6 days of oral administration, with effective blood concentrations of 25-70 ng/ml. 95% of the metabolites are metabolized by the liver, and the metabolites are 8-hydroxylation, 8-hydroxydemethylation, and N-oxidation, the first two of which are active. The metabolites are combined with glucuronide and excreted quickly, mainly from the urine, and 1%-2% are excreted in the form of prodrug. Oral dose starts at 30mg/d and can be increased to 60-150mg/d, taken once at bedtime. Maintenance dose 60mg/d.
Compared with tricyclics, cardiovascular toxicity is small, anticholinergic adverse reactions are mild, and adverse reactions such as dry mouth, constipation, and sleepiness are generally tolerated. Occasionally, a transient increase in ALT is seen, and a few elderly people may experience T-wave changes and ST-segment reduction.
7
Trozodone, alias Triazolone, trade name Mesyrel
50mg*20
Triazolopyridine compound, with a wide range of action sites and receptors, is a relatively selective 5-HT reuptake inhibitor, inhibition of DA, histamine receptors have no effect, the anticholinergic effect is slight, with a broad-spectrum antidepressant effect and sedative effect. It is suitable for various depressions and has good effect on symptoms such as sleep disorder, irritability and suicidal ideation, and has some therapeutic effect on impotence and prostatic hypertrophy reported. Tmax=1h, T1/2 is 5-9h, the active metabolite is m-chlorophenylpiperazine, which is excreted from urine in favorable and bound form. For the treatment of depression, the starting dose is 50 mg, 2-3 times a day, and the therapeutic dose is 300-600 mg/d; for depressive states where sleep disorders predominate, 50-150 mg/d can be taken in a single dose or in divided doses. The dose for the treatment of sexual dysfunction is generally greater than 150mg/d.
The main side effects are drowsiness, dizziness, headache, weakness, tremor, dry mouth, constipation, nausea, postural hypotension, cardiac arrhythmia, penile erection, etc. Contraindicated in pregnant and lactating women; may increase the effect of central depressants.
8
Fluoxetine Fluoxetine, trade name Prozac Prozac; Eucerin, Omelan, Eucerin, Fluoxetine capsules, Fluoxetine tablets
10mg*14
20mg*14
20mg*28
It is a representative drug of selective 5-HT reuptake inhibitor (SSRI). It has no down-regulation effect on postsynaptic membrane beta receptors, no affinity for cholinergic receptors, alpha receptors and histamine receptors, thus no anticholinergic side effects, does not cause hypotension, has little effect on the heart and no sedative effect. It has good efficacy in depression and obsessive-compulsive disorder, and can also be used for post-schizophrenic depression, bulimia nervosa and anorexia nervosa. It usually takes effect in 1 to 2 weeks of treatment. It is readily absorbed orally, with a Tmax of 4-6h and a T1/2 of 1-3 days. Hepatic metabolism and strong inhibition of cytochrome enzymes. The active metabolite, desmethyl fluoxetine, has a T1/2 of 7 to 15 days. Most of it is bound to glucuronide, a small amount is excreted as prodrug, 80% is excreted in urine and 15% in feces. It is convenient to take, and because of its long half-life, the effect of missed doses is not significant. The starting dose is usually 20mg, and the elderly can start with 10mg. The therapeutic dose is also 20mg/d, taken in the morning. For the treatment of obsessive-compulsive disorder, the dose is 20 to 80mg/d.
The side effects are mild, mainly nausea, anorexia, tremor, insomnia, anxiety, and can be gradually adapted with continued treatment. The incidence of rash is 3%, and high doses can induce seizures and sometimes mild mania. Long-term treatment is well tolerated, and drug overdose is safe. Combination with tricyclic drugs may increase the blood concentration of the latter, resulting in increased side effects. The “5-HT syndrome” is rare when taking SSRI drugs, including a group of symptoms such as anxiety, impaired consciousness, tremor, and myoclonus, and a high body temperature may indicate the occurrence of symptoms.
9
Paroxetine, trade name Seroxat
20mg*10
SSRI class antidepressant. Antidepressant effect is similar to TCA, with small side effects and some sedative effect. It is suitable for depression, especially depression with significant anxiety symptoms and sleep disorders, panic disorder. It usually takes effect in 1 to 2 weeks of treatment. It is completely absorbed orally and reaches steady-state blood concentration in 10 days after first-pass metabolism. t1/2=24 h. It is metabolized by the liver, metabolites are inactive, excreted by the kidneys, and a small amount is excreted in the feces. Easy to take, starting dose is usually 20mg, elderly people can start from 10mg. The therapeutic dose is also 20mg/d, taken in the morning. The dose can be increased in 10mg increments up to 60mg/d depending on the situation for 2-3 weeks of treatment.
Side effects are mild, mainly dry mouth, nausea, anorexia, constipation, tremor, insomnia, and ejaculation disorder, which can be gradually adapted by continuing treatment. It can sometimes induce mild mania, and should be used with caution in people with a history of epilepsy and mania, and in women during pregnancy and lactation. Long-term treatment is well tolerated, and drug overdose is safe. It inhibits cytochrome P450 isoenzyme, and when combined with tricyclic drugs amitriptyline and promethazine, it may increase the blood concentration of the latter, resulting in increased side effects. Combination with lithium salt is not recommended. Rapid discontinuation may cause sleep disturbance, agitation or anxiety, nausea, sweating, and confusion.
10
Sertraline, trade name Zoloft
50mg*14
SSRI class antidepressant. Antidepressant effect is similar to TCA, with small side effects and certain sedative effect. It is suitable for depressive states, obsessive-compulsive disorder, and especially depression with anxiety symptoms. It usually takes effect in about 7 days of treatment amount. Oral Tmax is 6-8 h, T1/2=26 h. Hepatic metabolism, metabolite desmethylsertraline is inactive, metabolism is complete and excreted from feces and urine. There is moderate intensity of pharmacological enzyme CYP2D6 inhibition. Easy to take, the starting dose is usually 50mg, the therapeutic dose is also 50mg, and the dose can be gradually increased to a maximum of 200mg/d at 50mg each time when the efficacy is poor or well tolerated, and taken in the morning. No special adjustment is needed for the elderly. OCD efficacy may take longer to appear.
Side effects are mild, mainly dry mouth, nausea, loose stools or diarrhea, tremor, delayed ejaculation, increased sweating, and dyspepsia, which can be gradually adjusted with continued treatment. An increase in transaminases may occasionally occur with oral doses of 100 mg/d or more. It can sometimes induce mild mania, and should be used with caution in people with a history of epilepsy or mania, and in women during pregnancy and lactation. Long-term treatment is well tolerated, and overdose is safe. Abrupt discontinuation is not recommended. Combination with lithium, tryptophan and alcohol is not recommended.
11
Fluvoxamine, alias Fluvoxamine, trade name Luvox Lancet
50mg*30
SSRI antidepressant, weak inhibition of NE or DA, weak affinity with Ach receptors in the brain, does not cause central and peripheral anticholinergic effects. It has little effect on neuroendocrine and cardiovascular systems and no antihistamine effect. It is suitable for the treatment of various depressions and related symptoms, especially for patients with obvious suicide attempts, obsessive-compulsive symptoms, and can be used in patients with depression with glaucoma, prostatic hypertrophy, and heart disease. Oral Tmax is 3.5-8h, T1/2 is about 15h, and steady-state blood concentrations are generally reached in about 10d. Hepatic metabolism, metabolites have 11 kinds, no pharmacological activity, its metabolite M2 is a very strong pharmacological enzyme CYP2D6 inhibitor. 90% is excreted from urine. Pharmacokinetic parameters in the elderly are similar to those in the young. The oral starting dose is generally 50mg/night, gradually increasing to an effective, therapeutic dose of 100-200mg/d, which can be increased to a maximum of 300mg/d in divided doses. The maintenance anti-relapse dose is 100mg/d.
The side effects are mild, mainly nausea, drowsiness, constipation, anxiety, tremor, decreased movement and fatigue in the early stage, and the reaction can disappear with continued treatment. Use with caution in epilepsy, hepatic and renal insufficiency, pregnancy and lactation. Overdose is safe. Combination with lithium salt and tryptophan may enhance the effect of 5-HT.
12
Citalopram, trade name Cipramil, Citalopram
20mg*14
SSRI antidepressant, without sedative effect, suitable for various depressive psychiatric disorders. Easily absorbed orally, T1/2 about 36h. hepatic metabolism, almost no or very weak inhibition of hepatic cytochrome P450 enzymes CYP1A2, CYP2C19, CYP2D6, very little inhibition of CYP3A4, especially suitable for elderly patients. It is administered orally and can be taken at any time throughout the day. The starting dose is 20mg/d, depending on the specific response and degree of depression, up to 60mg/d. The recommended dose for elderly patients is 20mg/d, which can be increased to a maximum of 40mg/d in divided doses. The maintenance anti-relapse dose is 100 mg/d. No dose adjustment is required for mild to moderate renal decompensation, and the dose should not exceed 30 mg/d for hepatic decompensation.
Side effects are rare and mild, with no cardiac toxicity. Nausea, dry mouth, drowsiness, increased sweating, diarrhea, and ejaculation disorders are common and usually occur in the first 2 weeks of treatment, and reactions may disappear with continued treatment. No correlation with seizures, but still need to be used with caution in epilepsy, history of mania, hepatic insufficiency, pregnancy and lactating women. Cimetidine may cause a moderate increase in mean steady-state levels of cimeteplane. Cimetoplan has no interaction with lithium salts, carbamazepine, or alcohol, and no pharmacodynamic effects have been found with benzodiazepines, antipsychotics, analgesics, antihistamines, antihypertensives, beta-blockers, and cardiovascular system drugs. Suicide-induced drug overdose can be associated with sleepiness, sleepiness, loss of consciousness, convulsions, tachycardia, nausea, cyanosis, tremors, and sweating.
13
Venlafaxine, trade name Bolssom Boloxin, Enox
25mg*16
75mg/150mg*14 controlled release
Monocyclic antidepressant, inhibits the reuptake of NE/5-HT, the first drug to inhibit the reuptake of these two transmitters, antidepressant effect is comparable to that of promethazine. Mainly used for depression, but also for obsessive-compulsive disorder, panic attacks, and chronic pain. Oral Tmax is 1 to 2h, T1/2 about 4h, and the active metabolite is O-desmethylvanafloxacin,T1/2 about 10h,. It is a weaker inhibitor of CYP2D6 enzyme. Oral starting dose is generally 25mg/time (50mg/time in severe cases), 2-3 times/d, after that add 75mg every 4d, generally reach 200mg/d, suicidal depression should be rapidly increased to more than 200mg/d within 1 week, the maximum dose is 375mg/d.
Side effects are mild, mainly nausea, drowsiness, dizziness, dry mouth, sweating, hypogonadism, and increased blood pressure. Reduce the dose as appropriate for hepatic and renal insufficiency. Use with caution in patients with epilepsy, blood disorders, pregnancy and lactation. Drug overdose is safer. The dose should be gradually reduced within 1 to 2 weeks when discontinuing the drug.
14
Moclobemine, trade name Long Tian, Kexue
150mg*6
100mg*30
Reversible selective monoamine oxidase inhibitor (A-MAOI). Selective and reversible; improves sleep quality without impairing alertness; less and milder toxic side effects than traditional drugs; almost no toxic side effects on heart and liver; low degree of restriction on tyramine food intake. It is suitable for all kinds of depression, anxiety disorders, bad mood, panic disorder, children’s ADHD, etc. Fast onset of action, generally 2 weeks of effect, 5 to 9 weeks of its efficacy reached the highest point. Oral absorption is safe, Tmax is about 1~2h, T1/2 is about 1~2h, hepatic metabolism, 19 metabolites are produced, the metabolites and 1% of the original drug are excreted through the kidney, 0.06% is excreted from breast milk. There is no significant difference in pharmacokinetic parameters between age groups. Cimetidine prolongs the metabolism of moclobemide. The commonly used therapeutic dose is 300-450 mg/d orally in 2-3 doses after meals, with a maximum dose of 600 mg/d in the second week if necessary. reduce the dose in the elderly. Patients with cirrhosis need to be reduced to half dose, patients with moderate renal impairment generally do not need dose adjustment.
Adverse effects include sleep disturbance, dizziness, headache, mild blood pressure instability, dry mouth, tremor, nausea, sweating, palpitations, reversible disturbance of consciousness.
Contraindications: Hypersensitivity to moclobemide, impaired consciousness, and pheochromocytoma; contraindicated in patients applying the following drugs, such as dulcolax, cocaine, 5-HT reuptake inhibitors (including tricyclic antidepressants), methamphetamine, ephedrine, pseudoephedrine, phenylpropanolamine, classical monoamine oxidase inhibitors; contraindicated with children.
Rarely serious elevated blood pressure reactions occur when taken with meals, but blood pressure should still be monitored regularly; use with caution in pregnant and lactating patients, patients with hepatic impairment (when necessary, 1/3 to 1/2 of the usual dose); avoid taking diets containing high tyramine (e.g., cheese, yeast extract, fermented soy foods); take medications for cough and cold with caution; for those already taking SSRI drugs, if this drug is needed, it is necessary to 4 to 28 days (4 to 5 half-lives) after stopping the above drugs before use; switching from morclobemide to other drugs should generally be stopped for more than 1 day; TCA can be combined with morclobemide or used successively; not recommended to be combined with SSRI.
15
Dimethyl anthracycline, Deanxit, Dextran, alias Dianxin
1 capsule*20
It is a combination of 0.5 mg of trifloxystrobin dihydrochloride (thioxanthines) and 10 mg of tetramethylpropylamine hydrochloride (heterocyclic antidepressant). It produces antidepressant effects and alleviates extrapyramidal side effects through synergy and antagonism of the two drugs. It has a rapid onset of action and is indicated for neurosis, multiple depressive and anxiety states, sleep disorders, plant nerve dysfunction, and various chronic pains. It is rapidly absorbed and reaches its peak concentration in 3-4 hours, and is excreted in urine and feces, with a small amount secreted through the placenta and breast milk. Adults 2 tablets/d, morning dose or morning and afternoon divided; severe cases can be 3 tablets/d, 2 tablets in the morning and 1 tablet in the afternoon; elderly patients 1 tablet/morning; maintenance dose 1 tablet/morning.