Among psychiatric disorders, schizophrenia is a common and frequent disease, which has a greater danger and impact on families and society, so it is particularly important to research, develop and reasonably use drugs for the treatment of schizophrenia. Antipsychotics are also known as nerve blockers. They mainly act on the reticular agonist system of the midbrain; the amygdala, hippocampus, and subthalamus of the limbic system; and the pallidum and striatum of the extrapyramidal system, with complex pharmacological effects. Commonly used antipsychotic drugs are divided into phenothiazines (chlorpromazine, methiodiazine, piperazine palmitate, fenpropizine, fluphenazine, fluphenazine decanoate, trifluoperazine, etc.), thiodiazepines (e.g., Teldene, trifluothione, etc.), butylphenols (e.g., haloperidol, pentafluoridol, haloperidol decanoate, etc.), and other non-classical antipsychotic drugs diphenoxazepines (e.g., clozapine, olanzapine, etc.), and Benzamides (such as sulpiride), risperidone, etc.
Product Name
Specification and packaging
Properties, usage and side effects
1
Chlorpromazine, C.P.Z., alias Dormant
25mg*100
50mg*100
25mg/ml
50mg/2ml
Phenothiazines are used on behalf of the class of drugs. This drug is the earliest used antipsychotic drug, a D2/D1 receptor blocker, and has high affinity for 5-HT6 and 7 receptors. It has a strong sedative effect and is mainly used for the treatment of schizophrenia, manic episodes of affective psychosis, reactive psychosis and other psychiatric disorders with symptoms of hallucinations, delusions, excitement and agitation. t1/2=17h, reaching steady state in 5-10 days, when t1/2=30h. The initial oral dose is 25-50mg, 3 times a day, and later increased as appropriate according to the condition and response. The therapeutic dose is 400-800mg/d in divided doses. The duration of treatment for patients in the acute phase takes 6-8 weeks. After the symptoms are relieved, the dose is gradually reduced. The maintenance dose is 300mg/d or less.
The main side effects include extrapyramidal symptoms (EPS), manifesting acute dystonia, tremor-like paralysis, inability to sit still, delayed dyskinesia (TD); anticholinergic effects, with dry mouth, constipation, blurred vision, difficulty urinating, urinary retention, tachycardia, etc.; postural hypotension, mostly caused by injection administration or overdose; more pharmacogenic liver damage, causing increased transaminases; effects on the endocrine The effects of the endocrine system, occasionally breast enlargement, lactation, menstrual changes; sun dermatitis, drug dermatitis, skin pigmentation; occasional occurrence of granulocytopenia; this product can cause excessive sedation, pharmacogenic depression.
2
Trifluoprozine, alias Stelazine
5mg*100
Phenothiazines, strong D2 and weak D1 receptor blockers, strong antipsychotic and antiemetic effects, fast acting, long duration, also has antihistamine effects. It is mainly used for the treatment of schizophrenia. It has good efficacy in acute hallucinations, delusions, sense of being controlled and disobedience. In chronic schizophrenia, it leads to improvement in emotional indifference, behavioral withdrawal, and increased activity. T1/2=13.3h. The initial oral dose is 5mg, 1 to 2 times a day, and gradually increases thereafter to a maximum of 40-60mg/d in divided doses, with a decreasing dose after 2 to 3 weeks of symptom relief and a maintenance dose of 10-20mg/d.
The main side effects are obvious extrapyramidal reactions (EPS), with tremor-like paralysis, inability to sit still, and dystonia being the most common. It can be reduced by reducing the dose or applying anti-convulsive paralysis drugs. Irritability, dry mouth, blurred eyes, difficulty urinating, tachycardia, and loss of appetite may occur. In contrast, abnormal liver function and blood picture changes are less common than with chlorpromazine.
3
Perphenazine, alias Trilafon
2mg*100
4mg*100
5mg/2ml
Phenothiazines, highly effective valence DA receptor blockers, similar in action to chlorpromazine, characterized by low dose, low toxicity and weak sedative effect. It is suitable for all subtypes of schizophrenia. It has better effect on acute hallucinations, victimization, jealousy, relationship delusions, disobedience, improves emotional indifference, and controls excitement and agitation less than chlorpromazine. t1/2=9h, excreted via bile, metabolites excreted in urine and feces. The initial oral dose is 2-4 mg, 3 times a day, and the dose is gradually increased, with a common dose of 20-60 mg/d.
The main side effects include extrapyramidal reactions, dry mouth, constipation, blurred vision, diplopia, nasal congestion, tachycardia, urinary frequency, appetite changes, weight gain and other symptoms. There may be postural hypotension, breast enlargement, and menstrual disorders. Occasionally, rash, electrocardiographic changes, and delayed dyskinesia may occur.
4
Fluphenazine, trade name Anatensol
2mg*100
Phenothiazine, D2/D1 receptor blocker, high affinity for 5-HT6 and 7 receptors, fast acting and long lasting. Mainly used for the treatment of acute and chronic schizophrenia, it can improve the contact of chronic patients, active mood, effective for thought disorder, hallucinatory delusions and nervousness. It is stronger than fenadine for symptoms of reticence, disobedience, impulsivity and indifference and loneliness. T1/2=13h. First dose of 2mg orally, 2-3 times a day, commonly used therapeutic dose 20-30mg/d, maximum dose 60mg/d, maintenance dose 10-20mg/d.
The main side effects are very strong extrapyramidal reactions, among which kinetic eye crisis, spastic squint, torsional spasm, inability to sit still, tremor, and myotonicity are common. Symptoms can be reduced by injection of scopolamine and oral administration of Antan. Occasionally, hypotension, granulocytopenia, and delayed dyskinesia are observed.
5
Fluphenazine Decanoate F.D.
25mg*2pcs
Fluphenazine is a long-acting agent of phenothiazine, T1/2=3.7 days, with an onset of action at 42-72h and the most pronounced effect at 48-96h, and can be maintained for 2-4 weeks. Intramuscular injection, the initial dose is generally 12.5-25mg/dose, once every 2-4 weeks, can be gradually increased to 50-100mg/2 weeks.
Side effects EPS are common, with milder vegetative reactions. Dry mouth and blurred vision may be seen. No significant damage to heart, liver and kidney. Occasional hypotension, granulocytopenia, caution in patients with organic diseases of the heart, liver and brain and in the elderly and infirm.
6
Thioridazine, alias Methiodiazine, trade name Ridazine
25mg*100
50mg*100
Phenothiazines, the pharmacological effect of this drug is approximately the same as that of chlorpromazine, but its sedative effect and extrapyramidal reactions are lighter than those of chlorpromazine. It is used to treat acute and chronic schizophrenia and affective disorders. Because of its anxiolytic and antidepressant effects, it is more effective in depression with hypochondria and delusions. It is widely used in the elderly because it is better tolerated by them. Initial dose 25-50mg, 2-3 times a day. The therapeutic dose is 200-600mg/d and the maintenance dose is 300mg/d or less.
The main side effects are dry mouth, blurred vision, nasal congestion, and postural hypotension. The rate of ECG abnormalities is high, mainly T-wave abnormalities, Q-T prolongation, bundle branch conduction block, which can lead to sudden death and should be taken seriously if it occurs. Long-term application of large amounts can cause retinopathy pigmentosa, which can be recovered after reducing or stopping the drug.
7
Pipotiazine Palmitate, trade name: Pipotiazine or ampicillin
50mg/2ml
Phenothiazines, long-acting agents. DA receptor blockers, weaker hypotensive and hypothermic effects than chlorpromazine. Used for hallucinatory delusions, uncoordinated motor excitement, impulsivity and other symptoms, and has an activating effect on patients with chronic behavioral withdrawal. tmax≈14 days, excretion is slow, 50% excreted after 20 d. 2%-7% excreted from urine, can be excreted by bile for enterohepatic circulation, most excreted from feces. Intramuscular injection, the initial dose is generally 25-50mg/time, once every 4-6 weeks, and the therapeutic amount is 50-200mg/time.
Side effects are EPS, but less than chlorpromazine. Occasionally severe insomnia, jaundice, and granulocytopenia are seen. Use with caution in patients with heart, liver, or kidney disease and in the elderly and infirm. Discontinued in patients with granulocytopenia and closed-angle glaucoma.
8
Chlorprothixene, alias Teldene Tardone
25mg*100
Thiazide, pharmacological action is approximately the same as chlorpromazine. It has some antidepressant effect and is effective in improving anxiety, tension, depression, negativity and sleep disorders. It is commonly used in the treatment of schizophrenia and schizoaffective psychosis with depression and anxiety symptoms. In addition, there are sedative, strengthen the effect of painkillers, ethanol and barbiturates and other hypnotic drugs and relaxation of the transverse muscle, cooling effect. The anticholinergic and antiadrenergic effects are weak and less effective than chlorpromazine in schizophrenia. The initial dose is 25mg, 3 times a day, and the highest therapeutic dose of 50-400mg can reach 800mg, with a maintenance dose of 200mg/d.
The main side effects are postural hypotension, dizziness, drowsiness, fatigue, dry mouth, constipation, tachycardia, and low EPS. Seizures can be caused at high doses. Occasionally, liver damage, granulocytopenia and rash occur. Use with caution in severe heart disease, liver disorders, bone marrow suppression, glaucoma, prostatic hypertrophy, urinary retention, epilepsy; cross-sensitivity with phenazines; acid-control drugs may affect the absorption of this product; sedation and anticholinergic effects are enhanced when used with tricyclic antidepressants.
9
Clopenthixol, trade name Cisordinol High antagonist
10/25mg/tablet
10mg/ml
Thiacetin, a D2/D1 receptor blocker, is less likely to cause increased resistance and DA receptor hypersensitivity with long-term use. It has good effect on psychotic symptoms such as hallucinations and delusions, thought disorders, behavioral disorders, excitability and agitation, and is used in acute and chronic schizophrenia with hallucinations and delusions and thought disorders, manic agitated state, intellectual disorder with psychomotor excitability, aggressive behavior disorder in children and arteriosclerotic dementia in the elderly. t1/2=20h, bioavailability 44%, distribution to the whole body, higher concentration in liver, lung and kidney. Lower concentration in the brain, metabolized by the liver and excreted in the feces and urine. Start with 10~50mg/d, divided into 2~3 doses, increase to 20~75mg/d, up to 150mg/d.
Side effects can be seen as drowsiness, dry mouth, blurred vision, constipation, and EPS. Long-term use is occasionally seen with TD. vertigo, urinary retention, upright hypotension and transient liver damage may also occur. Use with caution in patients with heart, liver and kidney disease and pregnant women.
10
Clothianidin Decanoate
Trade name: Gao Antiin
100mg/ml
200mg/ml
Thiacetin, long-acting formulation. t1/2=19d. for maintenance treatment or chronic schizophrenia. Intramuscular injection, 200-400mg/2 to 4 weeks.
11
Trifloxystrobin Flupentixol, trade name Tropax Rekindled
0.25mg/tablet
0.5mg/tablet
1.5mg/tablet
Thiazoquinone, D1, D2, 5-HT2 receptor blocker. No sedative effect, antipsychotic potency is 4-8 times stronger than Teldene, with uplifting effect. It is used in schizophrenia and is more effective in symptoms such as apathy, hypoactive will and defiance. Small doses have mood stabilizing, anxiolytic and antidepressant effects, also used for post-schizophrenic depression. tmax=4h, bioavailability 40%, significant enterohepatic circulation. Start 1-4mg/d in 2-3 doses, therapeutic dose 10-60mg/d, maintenance dose 5-20mg/d. Anxiety and depression 0.5-3mg/d in 2-3 doses.
Less common, but mild EPS is common, with inability to sit still and acute dystonia more prominent. Occasionally may cause insomnia and excitement, and should not be used for excitable and agitated patients. The effects on the vegetative nervous system and cardiovascular system are small. Long-term use may lead to TD, and EPS may be aggravated by the use of gastrofacial and perphenazine; use with caution in pregnancy, hepatic and renal cardiac insufficiency, and in patients with a history of epilepsy.
12
Triflufenthixene decanoate
Trade name Fuconazole
20mg/ml
40mg/ml
A long-acting formulation of thiacetin. For maintenance treatment or chronic schizophrenia. t1/2 is 3~8d, effect lasts 2~3 weeks. Intramuscular injection, 20~40mg/2~4 weeks.
13
Haloperidol Haloperidol, alias Haldol
2mg*100
5mg/ml
Representative of butylphenyl antipsychotics. It has a strong DA receptor effect, mainly acting on D2 as the drug of choice for the treatment of excitatory states. It has strong antipsychotic effect, good efficacy, fast onset of action, low toxicity, weaker sedative effect than chlorpromazine, stronger antiemetic effect, no significant effect on body temperature and blood pressure, weak anticholinergic effect and anti-adrenergic receptor effect. It has a significant effect on hallucinations and delusions, and also has an activating effect on chronic patients. It is mainly used in schizophrenia and is effective in controlling uncoordinated psychomotor excitement, hallucinations, delusions, hostility, and aggression, and is effective in manic episodes of affective psychosis. It is also commonly used in toxic, infectious, somatic and psychogenic psychiatric disorders, and can be effective in certain involuntary movements (chorea, tics). Oral Tmax is 3-4h, intramuscular Tmax=30min, T1/2 is 12-36h, systemic distribution, highest content in the liver. Excretion is slow, excreted from urine and feces, 24h excretion nearly 50%. Oral treatment is generally 8-20mg/d. Rapid haloperidol treatment: 5-10mg/dose by intramuscular injection, repeatable every 0.5-1h until excitement control. For the treatment of Tourette’s syndrome, as such patients are prone to EPS, small doses should be used, usually starting at 0.5 to 1mg/d, once at bedtime, and slowly increasing the dose if necessary, with a dose increase once every 3 to 5 d. The dose for children is 2 to 4mg/d, and for adults is 10 to 16mg/d, which can be divided into 1 to 3 times/d.
Among the major side effects, EPS is the most common, with tremor, motor inability, myotonia, sedentary inability, kinetic eye crisis, spastic squint, and torsional spasm. Injectable drugs have significantly less EPS than oral ones. Long-term use may cause TD. in addition, there is also weakness, dry mouth, constipation, blurred vision, sweating, drowsiness, and loss of appetite. It is generally considered to have low toxicity, less hepatic damage, and milder effects on the cardiovascular system than chlorpromazine, rarely causing ECG changes. It has the potential to cause pharmacogenic depression and can cause acute encephalopathic symptoms such as corkscrewing, spasms, convulsions, coma and myocardial damage at very large doses. Combination with phenobarbital can decrease the concentration of this drug.
14
Haloperidol decanoate Haloperidol decanote, trade name Andrographolide or Halidol
50mg/2ml
Long-acting preparation, Tmax is 4-11h, T1/2 is about 3 weeks. Long-acting, weak sedative effect, used for chronic psychotic schizophrenia and maintenance treatment. Intramuscular injection, 50-200mg/dose, once every 2-4 weeks. The maximum dose is 300mg/4 weeks.
Side effects are similar to those of haloperidol. Long-term use of large doses may cause cardiac rhythm disturbance and myocardial damage, and may also affect liver function. Muscle sclerosis may occur when large amounts are injected at the same site over a long period of time. Use with caution in elderly patients. It has been reported to be teratogenic and should not be used by pregnant women.
15
Penfluridol
10mg/tablet
20mg*24
Butylphenyl, highly effective DA receptor blocker, calcium ion antagonist. Once taken orally, the effect is maintained for 1 week, no anti-adrenergic effect, light sedative effect. It can control hallucinations, delusions, excitement, impulsiveness, etc. In chronic schizophrenia, it can eliminate hallucinations, activate emotions and improve contact. Tmax is 12-24h, T1/2 is 70-230h, stored in fatty tissue and released slowly. It is slow to penetrate and leave the brain tissue, and is stable in the brain with receptor binding. The enterohepatic circulation is the main reason for the long duration of action. Most of it is excreted in its original form in the feces and a small amount in the urine. It is taken once or twice a week with meals, 20mg for the first time, gradually increasing to 40-60mg/week, with a maximum of 120mg/week and a maintenance dose of 20-40mg/week.
Side effects are more common with EPS, in addition to weakness, dizziness, sleep disturbance, anxiety and depression, and gastrointestinal symptoms. Contraindicated in patients with hepatic impairment, contraindicated in elderly patients with tremor palsy, and caution in pregnant women.
16
Clozapine
25mg*100
It is a non-classical antipsychotic drug with a wide range of receptors, including D1, D2, D4, 5-HT, M, α2, H1, etc. It is a strong 5-HT2 receptor blocker, weak for D2 and strong for D4, and has less effect on the DA of black finger striatum. It has the characteristics of high efficacy, fast effect and light extrapyramidal reaction. It has a strong sedative-hypnotic effect. It is suitable for acute and chronic schizophrenia, and has good effects on excitability and agitation, hallucinations, delusions, thought disorders, contact passivity, and behavioral withdrawal. It is the strongest antipsychotic drug available, and the rapid dissociative properties of its action with D2 receptors may be the main reason for its good efficacy. It can also be used for manic episodes and improvement of intractable sleep disorders. tmax varies greatly among individuals, 1.5-6h, plasma protein binding rate is 94%, T1/2 is 3.6-14.3h, and steady-state blood concentration is reached in 7-10 days. The effective blood concentration is 300-600ng/ml. 80% of metabolites are excreted in the feces and 20% in the urine. The starting dose is 25~75mg/d, divided into 2~3 doses, the therapeutic amount is usually 300~400mg/d, and the maintenance amount is 50~200mg/d.
There are many side effects, including drowsiness, dizziness, salivation, constipation, weakness, nausea, abdominal distension, tachycardia, blurred vision, weight gain, etc. The incidence of EPS is low; it is easy to cause ECG changes such as tachycardia and T-wave changes; the anticholinergic effect is strong and causes intestinal paralysis; it has less effect on sexual function; large doses can lead to EEG changes and induce epilepsy; granulocytopenia can occur in individual patients, and it is not related to the dose. The most serious side effect of the drug is not related to the dose. All patients taking clozapine should have their granulocyte count and classification checked regularly, usually once a month in an outpatient clinic. It should not be combined with drugs that induce leukopenia, such as carbamazepine, sulfonamides, chloramphenicol, aminopyrine, etc.
17
Olanzapine Olanzapine, alias Olanzapine, trade name Replac
5mg*20
Olanzapine is a non-classical antipsychotic drug with similar structure and efficacy as clozapine, and also has anxiolytic effect, with less 5-HT1, 5-HT7 and α2 in the receptor spectrum than clozapine, thus reducing side effects. Injectable and long-acting preparations are not yet available in China.
No granulocytopenia side effects were seen, ECG and EEG changes are less, EPS is rare within the therapeutic dose, drowsiness, anticholinergic effect is lighter than clozapine, and there may be transient increase in prolactin.
18
Loxapine, trade name Loxapine
10mg/tablet
D2/D3 receptor blocker, with greater affinity for D3 receptors than D2, chemical structure similar to clozapine. The pharmacological effect is similar to that of chlorpromazine, with rapid onset of action. It is suitable for acute schizophrenia and is effective for thought disorders, anxiety and depression. Treatment of chronic schizophrenia is similar to trifluoperazine. t1/2 is 3-4h, oral bioavailability is reduced for eliciting first-pass effect, easy to pass the blood-brain barrier, mainly excreted by urine. Start 10mg/d, therapeutic dose 100-300mg/d, divided into 2-4 doses.
Side effects EPS common, but also nausea, vomiting, weight gain, ptosis, headache, irritability, anxiety, palpitations, lactation, inhibition of sperm excretion, etc.
19
Quetiapine alias Quetiapine, Quetiapine, trade name Qivi, Seroquel
25mg*28
100mg*30
Dibenzothiazepine class non-classical antipsychotic drugs. Similar to clozapine, it has affinity for D1, D2, 5-HT1A, 5-HT2A, histamine, α1, α2 receptors, and stronger affinity for 5-HT2 receptors than D2 receptors, and also has considerable blocking effect on histamine and adrenergic receptors, with almost no affinity for cholinergic receptors. The incidence of EPS is low, and it is effective and well tolerated in patients prone to EPS, including the elderly, children, and those with pre-existing DA pathology, such as Alzheimer’s disease (AD) and Parkinson’s disease. tmax is 1-1.5 h. It is metabolized in the liver by the cytochrome P450 system and 73% is excreted by the kidneys. The initial dose is 25mg/d twice daily; on the second or third day, the dose is increased by 25-50mg/d twice or three times daily; if tolerated, the dose can be increased to 300-400mg/d on the fourth day, divided into two or three doses. The therapeutic dose for adults was 150 to 750 mg/d, with a mean dose of 478 mg/d in open studies.
EPS occurs similarly to placebo, with mild effects on lactate, ECG, hematology, and body weight, and routine blood and ECG monitoring is not required. Drowsiness and upright hypotension may occur at the beginning of dosing and may resolve within 1 to 2 weeks, and monitoring is required for elderly sick and frail patients at this stage.
20
Sulpiride, alias anti-vomiting agent
100mg*100
Benzamide class, non-classical antipsychotic drug. Selective blockade of DA receptors, its effect does not depend on cAMP. has antipsychotic effect, antiemetic effect, but no, sedative-hypnotic effect. The antiemetic effect is 166 times stronger than that of chlorpromazine. It is suitable for various subtypes of schizophrenia, and has a good effect on symptoms such as xylophobia, hallucinations, delusions, indifference and isolation, and contact passivity. It is no less effective than chlorpromazine in schizophrenia, with significantly fewer extrapyramidal reactions. It has anti-solitary and antidepressant effects in small to medium doses. It can be used for the treatment of depression, depressive neurosis, psychosomatic disorders with depressive states. tmax=2h, T1/2=8h. cannot cross the placental barrier into the umbilical blood circulation. Oral starting dose 50-100mg, 2-3 times a day. Increasing dose, therapeutic dose 600-1200mg/d, maximum amount 1600mg/d, maintenance dose 200-400mg/d. For treatment of tic disorder, starting 50-100mg/d, 2-3 times/d, maximum dose 400-600mg/d.
Side effects include sleep disturbance, thus most of the doses are scheduled in the morning and noon. eps is mild, but there are a few people with severe eps. In addition, there are anxiety, irritability, menstrual disorders, impotence, gynecomastia, lactation, inability to ejaculate, thirst, sweating, difficulty in urination, dyskinesia, gastrointestinal reactions, and hypotension. Electrocardiographic abnormalities are seen with ST-T changes and bundle branch conduction block. Susceptibility to persistent hyperprolactinemia. Contraindicated in patients with hypertension, pheochromocytoma, caution in severe cardiovascular disease and hepatic impairment, minimal combination of anticholinergics, and contraindicated in young children.
21
Tiberium Tiapride
100mg*100
Benzamide, with blocking effect on DAergic receptors in the limbic system of the midbrain, and antagonistic effect on motor disorders caused by DA2 receptor excitation in the striatum, and can block the conduction of painful nerve impulses to the reticular formation via the thalamic tract of the spinal cord. It has stabilizing, sedative, antiemetic, analgesic and excitatory effects on gastrointestinal smooth muscle. Tmax=1h, T1/2 is 3~4h, mainly excreted in urine in original form. For the treatment of Tourette’s syndrome, the initial dose is 50~100mg/d, 2~3 times/d, and the highest dose is 400~600mg/d.
Side effects are mild and are drowsiness, dizziness, weakness, gastrointestinal reactions, followed by overflow of milk and amenorrhea. Individuals may experience excitement and insomnia.
22
Risperidone Risperidone, trade name Risperdal Vistone
1mg*20(White)
2mg*20(Orange)
Strong antipsychotic effect, non-classical antipsychotic drug. 5-HT receptor and DA receptor balance blocker. Rapid action, long and stable maintenance time, light EPS. Indicated for all types of schizophrenia, schizoaffective psychosis and affective disorders. Effective not only for positive symptoms such as hallucinations and delusions in schizophrenia, but also for negative symptoms such as emotional indifference, activity retardation and behavioral withdrawal. It helps to improve and enhance cognitive function. tmax=2h, T1/2 is 2-4h. steady-state blood concentration is reached in 5-6 days. Oral therapeutic dose is usually 2-6mg/d, divided into 1 or 2 doses. The maximum dose does not exceed 20mg/d.
Side effects are mild, with dose-related EPS that predispose to persistent hyperprolactinemia. The main side effects are menstrual disorders, dizziness, palpitations, nystagmus, and a few have difficulty concentrating memory with milder EPS.
23
Ziprasidone
20mg * 20 (tablet/capsule)
60mg*10 (capsule)
Atypical antipsychotic with a different structure from phenothiazines or butalbital benzyl antipsychotics. In vitro studies have shown that ziprasidone has high affinity for dopamine D2, D3, 5-hydroxytryptamine 5HT2A, 5HT2C, 5HT1A, 5HT1D, a-adrenergic receptors, moderate affinity for histamine H1 receptors, and no affinity for other receptors/binding sites tested, including M-cholinergic receptors. Ziprasidone has antagonistic effects on D2, 5HT2A, and 5HT1D receptors and agonistic effects on 5HT1A receptors. Ziprasidone inhibits synaptic reuptake of 5-hydroxytryptamine and norepinephrine.
It is well absorbed orally through the gastrointestinal tract, reaching peak plasma concentration in 6-8 hours and steady-state blood concentration in 1-3 days, with a plasma protein binding rate of >99% and a volume of distribution of 1.5L/kg. The mean terminal half-life (T1/2) is about 7 hours, and the mean apparent systemic clearance is 7.5 ml/min/kg. plasma protein binding rate is about 99%. After oral administration of ziprasidone, it is mainly fully metabolized by the liver, and only a small amount of the prodrug is excreted in the urine (<1%) and feces (<4%). The metabolites are excreted in urine and feces by about 20% and 66%, respectively, and the original form of ziprasidone in serum is about 44%. The enzymes of oxidative metabolism are mainly CYP3A4, CYP1AZ is weak, less than 1/3 of ziprasidone is eliminated by oxidative metabolism of cytochrome P450, and about 2/3 of ziprasidone is cleared by aldehyde oxidase metabolism.
Initial treatment: 20 mg (one tablet) twice a day orally with meals. This may be gradually increased to 80 mg (four tablets) twice a day depending on the condition. To ensure a minimum effective dose, patients should be carefully observed for post-dose response before adjusting the dose. Dose adjustment intervals should generally be no less than 2 days, as oral dosing of this product reaches steady-state blood levels within 1-3 days. Maintenance therapy: Patients should be periodically evaluated and determined if maintenance therapy is required. Although the length of maintenance treatment with ziprasidone has not been determined, the effective dose of ziprasidone for continuous use in patients with schizophrenia in a 52-week clinical trial was 20-80 mg twice a day.
Adverse effects: The side effects of therapeutic doses are similar to those of risperidone, with minor effects on weight and blood glucose; cardiac effects are of concern, especially prolonged QTC. Please refer to the instructions of each drug and ask your treating physician for details.