What Is Fluvoxamine Maleate?

This product is a coated scratch tablet in blister packs. In addition to the active ingredients, it also contains the following excipients: mannitol, corn starch, gelatin starch, sodium stearyl fumarate, colloidal silicon dioxide, hydroxypropyl methylcellulose, polyethylene glycol 6000, talc , Titanium dioxide (E171). This medicine does not contain lactose or sugars (E121). This medicine is a serotonin reuptake inhibitor that acts on brain nerve cells, and has little effect on non-adrenergic processes. At the same time, receptor binding experiments showed that the drug has almost no affinity for -adrenergic, -adrenergic, histamine, muscarinic, dopamine or serum factor receptors.

Fluvoxamine maleate

This product is a coated scratch tablet in blister packs. In addition to the active ingredients, it also contains the following excipients: mannitol, corn starch, gelatin starch, sodium stearyl fumarate, colloidal silicon dioxide, hydroxypropyl methylcellulose, polyethylene glycol 6000, talc , Titanium dioxide (E171). This medicine does not contain lactose or sugars (E121). This medicine is a serotonin reuptake inhibitor that acts on brain nerve cells, and has little effect on non-adrenergic processes. At the same time, receptor binding experiments showed that the drug is effective for -adrenergic, -adrenergic,
Chinese alias: (E) -5-methoxy-1- (4-trifluorotolyl) -O- (2-aminoacetoxime) -1-pentanone maleate
English aliases: 1-Pentanone, 5-methoxy-1- (4- (trifluoromethyl) phenyl)-, O- (2-aminoethyl) oxime, (E)-, (Z) -2-butenedioate (1: 1);
Molecular formula: C15H21F3N2O2 · C4H4O
Molecular weight: 434.409
Completely absorbed after oral administration. The maximum plasma concentration was reached 3-8 hours after taking the drug. The single-dose plasma half-life is 13-15 hours, and the multiple-dose plasma half-life is 17-22 hours. If the maintenance dose is not changed, stable plasma levels can be reached after 10-14 days. This drug is mainly metabolized in the liver, oxidized to 9 metabolites, and excreted by the kidneys. The two major metabolites have little pharmacological activity. In vitro experiments show that 80% of fluvoxamine can bind to human plasma proteins.
Treatment of depression and related symptoms.
The recommended starting dose for depression is 50 mg or 100 mg daily, once a night. Gradually increase until effective. The commonly used effective dose is 100 mg per day and can be adjusted based on individual response. Individual cases can increase to 300 mg per day. If the daily dose exceeds 150 mg, it can be taken in divided doses. The World Health Organization requires that patients continue to take antidepressants for at least 6 months after their symptoms have resolved. The recommended dose of this medicine for preventing the recurrence of depression is 100 mg daily.
The recommended starting dose for obsessive-compulsive disorder is 50 mg daily for 3-4 days, usually the effective dose is between 100-300 mg daily. It should be gradually increased until an effective dose is reached. The maximum daily dose for adults is 300 mg, and the maximum daily dose for children and adolescents over 8 years is 200 mg. A single dose can be taken orally to 150 mg per day, taken before bedtime. If the daily dose exceeds 150 mg, it can be divided into 2-3 times. If a good therapeutic effect has been obtained, the dose adjusted according to individual response can be continued. If symptoms do not improve within 10 weeks of taking the drug, continue to use this product. Although there is no systematic data suggesting the longest duration of continuous treatment with fluvoxamine, since OCD is a chronic disease, the treatment time can be longer than 10 weeks. The dose is carefully adjusted according to the patient's condition so that the patient receives the lowest effective dose possible. It should be regularly evaluated whether to continue treatment. Also consider using behavioral therapy at the same time.
Nausea, sometimes with vomiting, usually disappears 2 weeks after taking the medicine.
Other adverse reactions that occurred in controlled clinical observations at rates greater than 1% or greater than the placebo group were reported as:
Central nervous system: lethargy, dizziness, headache, insomnia, nervousness, agitation, anxiety, tremor;
Digestive system: constipation, anorexia, indigestion, diarrhea, abdominal discomfort, dry mouth;
Skin: sweaty;
Others: weakness, palpitations, tachycardia. Slightly slow heart rate (2-6 beats / min).
Similar to other serotonin reuptake inhibitors, very rarely reported
Depression patients often have suicidal tendencies, which often persist until symptoms improve significantly.
For patients with abnormal liver or kidney function, the starting dose should be lower and closely monitored. Occasionally, patients with no known abnormal liver function developed elevated liver enzymes after taking the drug, and often accompanied by clinical symptoms. If this happens, the drug should be stopped immediately.
Animal experiments have not found that this product can cause convulsions, but patients with a history of epilepsy should be used with caution, if convulsions occur, this product should be discontinued immediately.
There have been reports of abnormal bleeding of the skin and mucous membranes, such as petechiae and purpura, with serotonin reuptake inhibitors. At the same time, drugs that affect platelet function (TCAs, aspirin, non-steroidal anti-inflammatory drugs, etc.), and patients with a history of abnormal bleeding should be used with caution. Healthy volunteers, taking 150 mg of this product daily, have no effect on driving or mechanical operation. However, some reports indicate that drowsiness may occur after medication, and those who drive and operate the machine should pay attention.
Animal reproduction experiments did not find high doses of this drug on the ability of reproduction and teratogenic effects. But usually any medication should be taken with caution during pregnancy. This medicine can be excreted into milk in small amounts, so breastfeeding should be stopped during the medication.
Due to insufficient clinical data, this product is not recommended for children.
There is no significant clinical difference in the conventional dosage of the elderly compared with the young patients. However, dose adjustments should be made slowly in elderly patients.
This product is forbidden to be used in combination with monoamine oxidase inhibitors. If patients change to taking this product, the initial treatment should pay attention to: if it is an irreversible monoamine oxidase inhibitor, it should be stopped for at least 2 weeks; if it is a reversible monoamine oxidase inhibitor (Such as morphobexamide), can be changed to take this product 1 day after discontinuation.
If this product is discontinued, it should be discontinued for at least 1 week before switching to a monoamine oxidase inhibitor.
This product can slow down the decomposition rate of drugs metabolized by the liver. When used equally with warfarin, phenytoin, theophylline, and carbamazei, significant clinical effects can occur. If combined, adjust the dose of these drugs.
This medicine can increase the plasma concentration of phenylalanine through oxidative metabolism. There are reports that this drug can increase the original steady-state plasma concentration of tricyclic antidepressants. It is not recommended to use this product at the same time as tricyclic antidepressants.
This product can increase the plasma level of propranolol, and it is recommended to reduce the dose of propranolol when taking it.
This product is combined with warfarin for two weeks, and the plasma concentration of warfarin increases significantly and the clotting time is prolonged. Patients should monitor clotting time when taking anticoagulants and fluvoxamine orally and adjust the dose of fluvoxamine accordingly.
For severe, drug-resistant depression patients, this product can be combined with lithium. But lithium and tryptophan may aggravate serotoninergic effect of fluvoxamine.
No synergistic reaction was observed between this product and digoxin and atenolol.
As with other psychiatric medications, alcohol intake should be avoided during this medication.
The most common symptoms are gastrointestinal symptoms (nausea, vomiting, diarrhea), lack of energy, and dizziness. Other symptoms such as tachycardia, bradycardia, hypotension, abnormal liver function, convulsions, and coma have also been reported. To date, over 300 cases of overdose of this drug have been reported. The highest dose was 10,000 mg, and the patient fully recovered after symptomatic treatment. Occasionally, patients have a serious comorbidity due to intentional overdose of this drug in combination with other drugs.
There is no specific antagonist of this product for treatment. If overdose, empty stomach contents as soon as possible and treat symptomatically. It is recommended to use activated carbon repeatedly. No good results were seen with diuresis and dialysis.
[Medication]
It should be swallowed with water and should not be chewed.
[Storage / Validity]
This product should be stored in a dry and dark place.
Toxicity data from literature and journals
Numbering
Toxicity type
testing method
Test object
Dosage used
Toxic effect
1
Acute toxicity
oral
Humanity
64286 ug / kg
1. Behavioral toxicity-insomnia 2. Behavioral toxicity-muscle contraction or spasm 3. Biochemical toxicity-Inhibition of transaminase activity and changes in the spatial structure of transaminase
2
Acute toxicity
oral
Adult male
175 mg / kg / 13W-I
1. Behavioral toxicity-muscle contraction or spasm
3
Acute toxicity
oral
Adult woman
10 mg / kg
1. Gastrointestinal toxicity-nausea, vomiting 2. Gastrointestinal toxicity-other changes
4
Acute toxicity
oral
Rat
1500 mg / kg
1. Eye toxicity-dilated pupils 2. Lung, chest or respiratory toxicity-dyspnea 3. Nutrition and metabolic system toxicity-decreased body temperature
5
Acute toxicity
oral
Mouse
1100 mg / kg
1. Eye Toxicity-Mydriasis 2. Behavioral Toxicity-Convulsions or Seizure Thresholds Affected 3. Behavioral Toxicity-Ataxia
6
Acute toxicity
oral
dog
> 464 mg / kg
Detailed effects are not reported other than lethal dose
7
Chronic toxicity
oral
Rat
29120 mg / kg / 13W-I
1. Gastrointestinal toxicity-gastrointestinal ulcer or bleeding 2. Hepatotoxicity-Changes in liver weight 3. Biochemical toxicity-Inhibition or induction of phosphatase
8
Chronic toxicity
oral
dog
6825 mg / kg / 13W-I
1. Liver toxicity-changes in liver weight 2. Kidney, ureter and bladder toxicity-Changes in bladder weight 3. Hematological toxicity-changes in platelet count
[1-6]

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