I. Tricyclic antidepressants
Selective 5-HT reuptake activator (SSRA) Tianeptine, structurally belongs to the tricyclic antidepressants, but does not differ from the traditional tricyclic antidepressants and has unique pharmacological effects.
Indications: Various depressive disorders and anxiety disorders, especially geriatric depression.
Contraindications: Patients with hypersensitivity to tianeptine or any of the ingredients in the product; combination with monoamine oxidase inhibitors (MAOIs) is prohibited; children under the age of 15.
Dosage and Administration: The recommended dose is 12.5 mg three times daily (37.5 mg/d). The dose should be reduced appropriately in persons with renal impairment and in the elderly, with 25 mg/d recommended.
Adverse reactions: The more common ones are epigastric pain, abdominal pain, dry mouth, anorexia, nausea, vomiting, constipation, flatulence, insomnia/dreaminess, weakness, dizziness, headache, tachycardia, etc.
Drug-drug interactions: Drug-drug interactions may occur between this drug and non-selective monoamine oxidase inhibitors, and the combination of these two drugs increases the risk of episodes of cardiovascular disease or paroxysmal hypertension, hyperthermia, convulsions, and death. When combined with anesthetic drugs, attention should be paid to possible drug interactions, and tianeptine must usually be discontinued 24 or 48 hours prior to surgery.
II. Tetracyclic antidepressants
D2-antagonist and 5-HT1, 5-HT2 antagonist mainly for Mianserin (Mianserin), is a tetracyclic antidepressants.
Pharmacological effects: Unlike tricyclics, it can selectively block presynaptic Or2-adrenergic receptors to increase the concentration of NE in the synaptic gap. It can also block 5-HT2 receptors and H, receptors. It has antidepressant, anxiolytic and sedative effects; no anticholinergic effects; no cardiovascular toxic effects.
Indications: Various depressive disorders, especially for depressed patients with anxiety and insomnia.
Contraindications: Hypotension, patients with low white blood cell count.
Dosage and Administration: 30-90mg/d, may be taken in a single dose at night, starting with small doses.
Adverse reactions: This drug has small anticholinergic and cardiovascular adverse reactions, and small effects on liver and kidney function. The main adverse reactions are dizziness, weakness, and sleepiness. Rare granulocytopenia.
Third, anti-anxiety drugs
(A) Benzodiazepines
Benzodiazepines are used to treat various types of anxiety disorders and depressive disorders with anxiety symptoms in patients with psychological disorders. The most research has been done to treat panic disorder, and the FDA has approved the use of alprazolam in the treatment of panic disorder. There are also studies that support that other benzodiazepines can be effective in the short-term treatment of panic disorder, including: clonazepam, diazepam, and lorazepam.
Dosage and Administration: The usual starting dose of alprazolam is 0.5 mg 2-3 times/day, increasing by 0.5 mg/d every 3-4 days, with a common dose of 0.4-2 mg/d.
Some patients may require a maximum dose of 4-6 mg/d. The therapeutic dose of clonazepam is 1-6 mg/d. Withdrawal symptoms may occur with higher doses. Dose reductions should be gradual|decreases, typically by 0.5 mg/d every 3-4 days or more slowly. Combining benzodiazepines at the beginning of treatment with SSRIs can have a faster onset of action.
Withdrawal symptoms:
Withdrawal symptoms occur in 30%-90% of patients; most symptoms are mild to moderate and tolerable, but seizures may occur (relatively rare) when larger doses of benzodiazepines are abruptly discontinued. It is recommended that medication should be tapered slowly. For patients with panic disorder, tapering takes 8-24 weeks. Short-term treatment or small doses of benzodiazepines may not require such a long withdrawal time.
When a patient discontinues a benzodiazepine, two things may happen:
1. the patient may have a relapse of the original symptoms.
2. Patients may experience withdrawal symptoms, which often occur within a few days of stopping the drug, but usually diminish or disappear within 2-3 weeks.
Common symptoms of benzodiazepine withdrawal syndrome include.
Anxiety, irritability, insomnia, fatigue, headache, muscle tremors or pain, tremor, shaking, sweating, dizziness, difficulty concentrating attention, nausea, loss of appetite, marked depression, depersonalization, dissociation of reality, enhanced sensory perception (smell, sight, taste, touch), and abnormal perception or kinesthesia. Patients and their families should be given supportive education during treatment to guide the correct discontinuation process. Recent studies suggest that group cognitive behavioral therapy may also help patients to discontinue long-term benzodiazepine use.
The efficacy of benzodiazepines in the treatment of generalized anxiety disorder has been demonstrated in several early studies. Among them, diazepam, alprazolam and lorazepam have been studied more frequently. And the US FDA approved alprazolam for the treatment of anxiety disorders similar to the diagnosis of generalized anxiety disorder.
However, benzodiazepines are not currently recommended as first-line medications for the following reasons:
1. benzodiazepines are not effective for depressive symptoms that are often co-morbid with generalized anxiety disorder.
2. susceptibility to adverse effects such as excessive sedation, memory impairment and psychomotor impairment, which can easily lead to traffic accidents
3, prone to tolerance or abuse, dependence, and prone to withdrawal symptoms after discontinuation of the drug. It is usually recommended to consider benzodiazepines at the beginning of treatment when the efficacy of other anxiolytic drugs has not yet been demonstrated. Combined benzodiazepines have better efficacy for patients’ anxiety and somatic symptoms, but it is usually recommended to use them for a maximum of 2-4 weeks, followed by gradual reduction and discontinuation of the drugs.
IV. 5-HT1A receptor partial agonists
(A) Buspirone
The approved indications for buspirone in China are the treatment of various anxiety disorders. The formulation of buspirone is buspirone hydrochloride, available in the form of 5mg tablets, taken orally. The general starting dose for adults is 10-15mg/d in 2-3 doses; it can be increased to 20-30mg/d in 2-3 doses in the second week. The common dose is 20-40mg/d.
(II) Tandospirone
Tandospirone is available in the form of citrate, and the usual adult dose is 10mg per dose, 3 times daily, which can be increased according to clinical efficacy and safety, with a maximum dose of 60mg/d. Elderly people start with a small dose, such as 5mg per dose.