Antimanic drugs mainly refer to drugs with therapeutic and preventive effects on mania. Lithium salt is the most common antimanic drug, in addition to the commonly used antipsychotics chlorpromazine, haloperidol, clozapine, quetiapine and the antiepileptic drugs carbamazepine, sodium valproate, and magnesium valproate also have antimanic effects. In addition, the calcium channel blockers valproate (isoptinin) and colistin have also been reported for the treatment of mania.
Name
Specification and packaging
Properties, usage and side effects
1
Lithium Carbonate or Li2CO3
0.25g*100
0.3g*100 (controlled release tablets)
This drug has the effect of stabilizing emotion, its mechanism of action is not clear, from the clinical efficacy, there is a significant anti-manic effect, used for the treatment of manic episodes, bipolar affective psychosis manic phase and depressive phase, mixed phase, split affective psychosis. It is the drug for maintenance treatment of mania in remission. It also has the effect of raising white blood cell, and is used for the adjuvant treatment of granulocytopenia. It is easily absorbed orally, Tmax is 2~4h, T1/2 is 12~24h, and it takes 5~7 days to reach steady state in serum, and even slower to reach steady state concentration in cerebrospinal fluid. 95% is excreted in urine, and a small amount is excreted in feces, sweat, saliva and breast milk. The rate of excretion of lithium is positively correlated with sodium salt. Start with one oral dose of 0.25g, three times a day, and gradually increase the dose according to the blood lithium concentration and response to dosing. The therapeutic dose is 0.5-2.0g/d, divided into 2-3 doses. The dose should be increased slowly, and the highest therapeutic dose should not exceed 2 to 3 weeks. Ask the patient to eat more salt-containing diet and drink more water. The maintenance dose is 0.5-1.0g/d, divided into 2-3 doses. Since the effective therapeutic amount of lithium salt is very close to the toxic amount, the future high or low should be determined during treatment according to the patient’s age, weight, blood lithium concentration, side effects, and therapeutic effect. Therefore, the blood lithium concentration should be measured frequently during treatment, and its therapeutic blood lithium concentration is 0.6 to 1.2 mmol/L, maintenance blood lithium concentration is 0.4 to 0.8 mmol/L. Blood lithium concentration >1.5 mmol/L can show symptoms of toxicity, and 0.5 mmol/L can show symptoms of toxicity in elderly or susceptible patients.
The main side effects are nausea, vomiting, abdominal pain, diarrhea, anorexia, fine hand tremor, weakness, thirst, frequent urination, swelling, weight gain, goiter, decreased blood pressure, abnormal ECG (T-wave hypotension, inversion, etc.). Symptoms of toxicity such as tremor, hyperreflexia, seizures, and in severe cases, impaired consciousness in the form of acute organic brain syndrome should be strictly guarded against. Lithium salt taken with digoxin and quinidine can increase the toxic effect, taken with chlorpromazine reduces the blood concentration of chlorpromazine, taken with antipyretics, diuretics and laxatives can increase the blood concentration of lithium. It can be excreted from breast milk, so nursing women should not breastfeed when taking it. Long-term application may lead to impaired renal tubular function and hypothyroidism. Use with caution in the elderly and in patients with renal insufficiency.
2
Sodium Valproate
Trade name (extended-release tablets for Depakene)
200mg*100
Valproate is an antiepileptic drug of the valproic acid class. It acts through GABAergic system and inhibits GABA aminotransferase. It has efficacy on all personality seizures, with the best effect on petit mal seizures. It is used in epilepsy and affective mental disorders. It is often used in combination with schizophrenic patients with certain affective symptoms. t1/2 is about 15h. for the treatment of epilepsy, adults take 200-400mg/dose orally, 2-3 times/d. the initial dose tolerated for the treatment of mania is 500-1000mg/d, after which the dose is gradually increased until the effective blood concentration of 50-150μg/ml is reached, and the dose can reach 2000mg/d. after 1 week, the symptoms are significantly increased. There is a significant improvement in symptoms 1 week thereafter.
Common side effects are gastrointestinal reactions, such as anorexia, nausea and vomiting. A small number of patients develop hepatotoxicity with elevated serum alkaline phosphatase and transaminases. Rarely, lymphocytosis, thrombocytopenia, alopecia, somnolence, weakness, and ataxia occur. It can inhibit the metabolism of sodium phenytoin, phenobarbital and clonidine, which may cause toxicity.
3
Magnesium valproate valpamag
200mg*60
Anti-epileptic spectrum is wide, and can be used as an emotional stabilizer. Used for the treatment of affective mental disorders. Easily absorbed orally, Tmax is 1.7-2h, T1/2 about 8.3h, high bioavailability, mostly excreted by urine in the form of glucuronide. Adults 200-400mg/dose, 3 times a day, maximum amount 1800mg/d.
Adverse reactions commonly include nausea, vomiting, decreased appetite, loose stools, drowsiness, dizziness, etc. It also has an effect on liver function.
4
Carbamazepine
Trade name: Deltamethrin
100mg*100
200mg*30
Aminostilbene antiepileptic drug, suitable for partial seizures, especially complex partial seizures, generalized tonic-clonic seizures. It is particularly suitable for patients with personality changes and psychiatric symptoms, and is not effective for akathisia myoclonic and dystonic seizures. It can also be used for abnormal behavior, impulsivity, and mood instability during acute psychotic episodes. The Tmax of single dose is about 4~8h, T1/2 is about 36h, and T1/2 decreases to 10~25h after 3~4 weeks of continuous dosing. there is enterohepatic circulation, 98% hepatic metabolism. Oral 200～600mg/d, increase once every 5 days, gradually increase to therapeutic amount 600～1200mg/d or blood concentration reaches 4～15μg/ml, divided into 3～4 times. Acute mania 600～1200mg/d, rapid circulation type 1200～2000mg/d. Generally, good effect is achieved within 1～2 weeks. When treating mania, other antipsychotic drugs can be combined and the dose can be reduced as appropriate.
Sleepiness, dizziness, diplopia, ataxia are common. Gastrointestinal discomfort, nausea, vomiting, abdominal pain, diarrhea, constipation, anorexia, and dry mouth are common. Hepatic impairment is occasionally seen, and skin lesions, such as rash, photosensitivity dermatitis, skin pigmentation, occur in 10%. Transient leukopenia occurs in 10% and other hematologic changes are occasionally seen. It has antidiuretic hormone-like effects and may reduce asymptomatic hyponatremia. Regular blood and liver function checks are required for long-term use. Abrupt discontinuation of the drug may cause seizures.
5
Topiramate, trade name Topamax
25mg*60
50mg*60
100mg*60
New antiepileptic drug for the additive treatment of partial seizures with or without secondary generalized seizures. It can also be applied in the treatment of affective psychiatric disorders. t1/2 is about 21h and plasma steady-state concentrations are reached at 4-8h. Prototypes and metabolites are excreted mainly through the kidneys and can cross the placental barrier with potential reproductive toxicity. The initial dose is 50mg/night, and the dose is gradually increased after 1 week to 50-100mg/week in 2 doses. The therapeutic dose is generally 200-400mg/week, with a maximum dose of 1600mg/week. Blood concentration monitoring is generally not necessary. Topiramate is added to the application of phenytoin sodium, and only rarely does the dose of phenytoin sodium need to be adjusted. Topiramate generally has no effect on the blood concentrations of other antiepileptic drugs, but rarely has an effect on the blood concentrations of phenytoin sodium, and blood concentrations should be monitored when clinical signs of toxicity occur. The dose should be increased to 1.5 times during hemodialysis, and the supplemental dose should be divided at the beginning and end of hemodialysis.
Adverse reactions include ataxia, impaired concentration, confusion, dizziness, fatigue, abnormal sensation, drowsiness, and abnormal thinking, as well as anxiety, amnesia, loss of appetite, aphasia, depression, diplopia, emotional instability, nausea, nystagmus, dysphasia, taste inversion, visual abnormalities, and weight loss.