What Is Bupropion?

Bupropion belongs to the aminoketone class of antidepressants. Applicable to patients with depressive depression and depression who have no obvious or intolerable effect on other antidepressants. Long-term high-dose administration can produce a down-regulating effect of -adrenergic receptors ^[1] .

Bupropion belongs to the aminoketone class of antidepressants. Applicable to patients with depressive depression and depression who have no obvious or intolerable effect on other antidepressants. Long-term high-dose administration can produce a down-regulating effect of -adrenergic receptors ^[1] .

Drug Name

Bupropion

Foreign name

Bupropion Hydrochloride Tablet

Exterior

Yellow film-coated tablets

Main ingredients

Bupropion

Brief introduction of bupropion compounds

Bupropion Basic Information

common name:

Bupropion

English name: Bupropion Hydrochloride Tablet

Chemical name: (±) -1- (3-chlorophenyl) -2-[(1,1-dimethylethyl) amino] -1-acetone

Chinese alias: 1- (3-chlorophenyl) -2-[(1,1-methylethyl) amino] -1-acetone hydrochloride; bupropion hydrochloride; butylamine acetone; -tert-Butylaminoethylphenylmethanone; 1- (3-chlorophenyl) -2-[(1,1-dimethylethyl) amino] -1-acetone hydrochloride; 1- (3 -Chlorophenyl) -2-[(1,1-methylethyl) amino] -1-acetone

English name: bupropion

English alias: (+/-)-1- (3-CHLOROPHENYL) -2-[(1,1-DIMETHYLETHYL) AMINO] -1-PROPANONE HYDROCHLORIDE; 1- (3-CHLOROPHENYL) -2-[(1,1 -DIMETHYLETHYL) AMINO] -1-PROPANONE, HYDROCHLORIDE; 2-tert-butylamino-1- (3-chlorophenyl) -propan-1-one hydrochloride; AMFEBUTAMONE; AMFEBUTAMONE HCL; AMFEBUTAMONE HYDROCHLORIDE; BUPROPION HCL; BUPROPION HYDROCHLORIDE; DL-1 -(3-CHLOROPHENYL) -2-[(1,1-DIMETHYLETHYL) AMINO] -1-PROPANONE HYDROCHLORIDE; (+-)-1- (3-chlorophenyl) -2-((1,1-dimethylethyl) amino) -1-propanone; 1-dimethylethyl) amino) -1- (3-chlorophenyl) -2-((((+-)-1-propanon; alpha- (tert-butylamino) -m-chloropropiophenone; Wellbutrin1- (3- Chlorophenyl) -2-[(1,1-dimethylethyl) amino) -1-propamone; (a-2- (tert-butylamino) -3 & cent ;; 2-tert-butylamino-1- (3-chlorophenyl) -propan- 1-one; m-chloro-a- (tert-butylamino) propiophenone; BUPROPION / AMFEBUTAMONE; Amfebutamon; Wellbatrin: Wellbutrin

Molecular formula: C ₁₃ H ₁₈ ClNO · HCl

Molecular weight: 276.2

Phytochemical properties of bupropion

Melting point: 233-234 ° C

Form: solid

color: White

Solubility: soluble in methanol, ethanol, acetone, ether or benzene

Solubility: ethanol: 193 mg / mL solutions may be stored for several days at 4 ° C.

Bupropion Safety Terminology

S36 Wear suitable protective clothing.

Wear appropriate protective clothing.

Bupropion Risk Terminology

R22 Harmful if swallowed.

Harmful if swallowed.

Bupropion production method

In a solution of ethyl magnesium bromide, an ethyl ether solution of o-chlorophenylacetonitrile was added for reaction. The reaction solution was hydrolyzed with cold dilute hydrochloric acid. After diethyl ether was distilled off, the remaining aqueous solution was heated for a certain time. Seeds are allowed to cool. The solid was collected by filtration, washed with cold water, and recrystallized from methanol to obtain o-chlorophenylacetone. Dissolve o-chlorophenylacetone in dichloromethane, stir with activated carbon and magnesium sulfate, and filter. A solution of bromine in dichloromethane was added with stirring. When the bromine color completely disappeared, the solvent was removed by concentration in vacuo, and the remaining oil was o-chloro--bromophenylacetone. O-Chloro--bromophenylacetone was dissolved in acetonitrile, and tert-butylamine in acetonitrile was added. Let stand and add water and ether to partition. After treatment, it was finally washed with acetone, and then recrystallized from a mixture of isopropanol and absolute ethanol. Get bupropion hydrochloride.

Bupropion use

New types of antidepressants have aminoketone structures and are chemically unrelated to tricyclic, tetracyclic, and monoamine oxidase inhibitors or other standard drugs. Used for antidepressant ^[2] .

Bupropion Drug Description

Bupropion Application Area

Central nervous system medication

Bupropion traits

This product is a yellow film-coated tablet, which is white after removing the coating. Bupropion is a racemic mixture. The pharmacological activity and pharmacokinetics of individual enantiomers have not been studied. The pharmacokinetic curve of bupropion is a two-compartment model. The average half-life of the terminal phase is 21 hours (± 20%), and the average half-life of the distributed phase is 3 to 4 hours.

Bupropion pharmacological action

Bupropion has a weak inhibitory effect on norepinephrine, 5-HT, and dopamine reuptake, but has no effect on monoamine oxidase. The antidepressant mechanism of this product is not clear, and may be related to noradrenaline and / or dopaminergic effect.

Bupropion toxicology

Genotoxicity : Two of the five strains in the bupropion Ames test showed positive results (mutation rate was 2 to 3 times that of the control group), and one of the three bone marrow cytogenetic tests in rats Increased chromosome aberration rates.

Reproductive toxicity : Oral administration of bupropion up to 300 mg / kg in rats, no damage to fertility was seen. Pregnant rats and rabbits were given bupropion doses of up to 450 mg / kg and 150 mg / kg, respectively (based on body surface area, equivalent to 7-11 times and 7 times the maximum recommended human dose, respectively), and no drug-related effects were found. Fetal Toxicity.

Carcinogenicity : In long-term dosing studies, rats and mice were given bupropion doses of up to 300 and 150 mg / kg (by body surface area, respectively, equivalent to 7 times and 2 times the maximum recommended human dose), For 104 consecutive weeks and 96 weeks, a dose of 100-300 mg / kg can cause nodular hyperplasia of the liver in rats. It is not clear whether the hyperplasia is a precursors of neoplasm. No similar lesions were seen in the mice. There was no increase in the incidence of malignant tumors of the liver and other organs in either trial.

Bupropion pharmacokinetics

Bupropion is a racemic mixture. The pharmacological activity and pharmacokinetics of individual enantiomers have not been studied. The pharmacokinetic curve of bupropion is a two-compartment model. The average half-life of the terminal phase is 21 hours (± 20%), and the average half-life of the distributed phase is 3 to 4 hours. Absorption: Only a small part of bupropion can be absorbed after oral administration, and peak blood concentration can be reached within 2 hours.

Distribution : In vitro tests show that the plasma protein binding rate is 84% when the concentrated drug concentration is 200 g / mL. The metabolite oxybupropion has a protein binding rate similar to that of bupropion, while the other metabolite threonine hydrogenated bupropion has a protein binding rate that is only half that of bupropion. 17 subjects taking a single 150 mg dose showed a bupropion volume of 1950 L (20% CV)

Metabolism : Bupropion is extensively metabolized in the human body, and three active metabolites are produced through tert-butyl hydroxylation and / or reduction of the carboxyl group: oxybupropion, threonine hydrogenated bupropion And erythritol hydrogenated bupropion. The bupropion side chain is oxidized to form a glycine-m-chloroperoxybenzoic acid copolymer, which is the most important metabolite in urine. In vitro tests show that cytochrome P450B6 is the main isoenzyme involved in the formation of oxybupropion, while cytochrome P450 isoenzyme does not participate in the formation of threonine hydrobupropion.

Because bupropion can be extensively metabolized, there may be potential drug-drug interactions, especially with drugs that also require cytochrome P450IIB6 isoenzyme metabolism. Although cytochrome P450IID6 is not involved in the metabolism of bupropion, there is a potential interaction between bupropion and drugs metabolized by cytochrome P450D6 (see Drug Interactions). The peak plasma concentration of oxybupropion reached 6 hours after a single oral administration of bupropion, which was 10 times the peak plasma concentration of the original drug at steady state, and the AUC at steady state was about 17 times that of the original drug. The peak times for other metabolites threonine bupropion and erythritol bupropion are similar to oxybupropion, and the steady-state AUC is 1.5 and 7 times that of bupropion, respectively.

Excretion : After oral administration of 200 mg of 14C-bupropion, 87% and 10% of radioactivity can be detected in urine and feces, respectively. Only 0.5% of the drug was excreted in its original form.

Bupropion indication

Used to treat depression.

Bupropion dosage

Oral, starting with a small dose, the starting dose is 75mg (1 tablet) once, twice a day (once and evening each); after taking it for at least 3 days, the dose can be gradually increased according to clinical efficacy and tolerance 75mg (1 tablet) at a time, 3 times a day (once each morning, middle, and evening); later, you can continue to gradually increase to the usual dose of 300mg daily, as appropriate, 3 times daily (2 tablets each, 1 tablet each during middle and evening hours) ). In the process of increasing the dosage, the increasing dose within 3 days shall not exceed 100 mg per day. As an antidepressant, this product usually takes 4 weeks to show obvious effects. If there is no obvious effect after continuous use for several weeks, you can consider gradually increasing to the maximum daily dose of 450mg, but the maximum daily dose should not exceed 150mg (2 tablets), the interval between two medications should not be less than 6 hours.

Bupropion adverse reactions

According to foreign literature reports, common adverse events in clinical use of bupropion include agitation, dry mouth, insomnia, headache / migraine, nausea / vomiting, constipation, and tremor. About 10% of the 2,400 subjects (including patients and healthy volunteers) discontinued medication due to the occurrence of adverse events. The most common causes are neuropsychiatric disorders (3.0%), mainly agitation and mental disorders; gastrointestinal disorders (2.1%), mainly nausea and vomiting; neurological disorders (1.7%), mainly epilepsy, Headache and sleep disorders; skin discomfort (1.4%). It is worth noting that some adverse events were caused by the dosage above the recommended daily dose.

(I) The following are adverse events observed in daily doses of bupropion between 300 and 600 mg in a placebo-controlled study:

Cardiovascular System:

Arrhythmia: bupropion (n = 323), 5.3; placebo (n = 185), 4.3;

Dizziness: bupropion (n = 323), 22.3; placebo (n = 185), 16.2;

Hypertension: bupropion (n = 323), 4.3; placebo (n = 185), 1.6;

Hypotension: bupropion (n = 323), 2.5; placebo (n = 185), 1.2;

Palpitations: bupropion (n = 323), 3.7; placebo (n = 185), 2.2;

Syncope: Bupropion (n = 323), 1.2; Placebo (n = 185), 0.5;

Bradycardia: bupropion (n = 323), 10.8; placebo (n = 185), 8.6;

Skin system:

Itching: bupropion (n = 323), 2.2; placebo (n = 185), 0.0;

Flushing: bupropion (n = 323), 8.0; placebo (n = 185), 6.5;

Digestive system:

Anorexia: bupropion (n = 323), 18.3; placebo (n = 185), 18.4;

Increased appetite: bupropion (n = 323), 3.7; placebo (n = 185), 2.2;

Constipation: bupropion (n = 323), 26.0; placebo (n = 185), 17.3;

Diarrhea: bupropion (n = 323), 6.8; placebo (n = 185), 8.6;

Indigestion: bupropion (n = 323), 3.1; placebo (n = 185), 2.2;

Nausea / vomiting: bupropion (n = 323), 22.9; placebo (n = 185), 18.9;

Weight gain: bupropion (n = 323), 13.6; placebo (n = 185), 22.7;

Weight loss: bupropion (n = 323), 23.2; placebo (n = 185), 23.2;

Urogenital:

Impotence: bupropion (n = 323), 3.4; placebo (n = 185), 3.1;

Menstrual disorders: bupropion (n = 323), 4.7; placebo (n = 185), 1.1;

Frequent urination: bupropion (n = 323), 2.5; placebo (n = 185), 2.2;

Urinary retention: bupropion (n = 323), 1.9; placebo (n = 185), 2.2;

Skeletal muscle:

Arthritis: bupropion (n = 323), 3.1; placebo (n = 185), 2.7;

nervous system:

Sedentary inability: bupropion (n = 323), 1.5; placebo (n = 185), 1.1;

Bradykinesia: bupropion (n = 323), 8.0; placebo (n = 185), 8.6;

Skin changes: bupropion (n = 323), 1.0; placebo (n = 185), 1.0;

Dry mouth: bupropion (n = 323), 27.6; placebo (n = 185), 18.4;

Sweaty: bupropion (n = 323), 22.3; placebo (n = 185), 14.6;

Headache / migraine: bupropion (n = 323), 25.7; placebo (n = 185), 22.2;

Reduced sleep quality: bupropion (n = 323), 4.0; placebo (n = 185), 0.6;

Increased salivary secretion: bupropion (n = 323), 3.4; placebo (n = 185), 3.8;

Insomnia: bupropion (n = 323), 18.6; placebo (n = 185), 15.7;

Muscle cramps: bupropion (n = 323), 1.9; placebo (n = 185), 3.22;

Pseudo-Parkinson's disease: bupropion (n = 323), 1.5; placebo (n = 185), 1.6;

Sedation: bupropion (n = 323), 19.8; placebo (n = 185), 19.5;

Paresthesia: bupropion (n = 323), 4.0; placebo (n = 185), 3.2;

Tremors: bupropion (n = 323), 21.1; placebo (n = 185), 7.6;

Neuropsychiatric system:

Excitement: bupropion (n = 323), 31.9; placebo (n = 185), 22.2;

Anxiety: bupropion (n = 323), 3.1; placebo (n = 185), 1.1;

Insanity: bupropion (n = 323), 8.4; placebo (n = 185), 4.9;

Decreased libido: bupropion (n = 323), 3.1; placebo (n = 185), 1.6;

Hallucinations: bupropion (n = 323), 1.2; placebo (n = 185), 1.1;

Inattention: bupropion (n = 323), 3.1; placebo (n = 185), 3.8;

Euphoria: bupropion (n = 323), 1.2; placebo (n = 185), 0.5;

Hatred: bupropion (n = 323), 5.6; placebo (n = 185), 3.8;

Non-specific:

Fatigue: bupropion (n = 323), 5.0; placebo (n = 185), 8.6;

Fever / chills: bupropion (n = 323), 1.2; placebo (n = 185), 0.5;

Respiratory system:

Upper respiratory tract discomfort: bupropion (n = 323), 5.0; placebo (n = 185), 11.4;

Special feeling:

Hearing changes: bupropion (n = 323), 5.3; placebo (n = 185), 3.2;

Blurred vision: bupropion (n = 323), 14.6; placebo (n = 185), 10.3;

Taste disorders: bupropion (n = 323), 3.1; placebo (n = 185), 1.1.

Note: The above events are adverse events with an incidence of> 1% in patients treated with bupropion.

(2) In other open and uncontrolled clinical studies, the following adverse events have also been observed, where the common adverse event refers to an incidence of at least 1%, and the occasional adverse event refers to an incidence between 0.1% to 1%. Rare adverse events are those with an incidence below 0.1%.

1. Cardiovascular system: common: edema; occasional: chest pain, abnormal electrocardiogram (premature beats, non-specific ST segment T wave changes), shortness of breath, dyspnea; rare: flushing, paleness, phlebitis, and myocardial injury.

2. Skin system: common: non-specific rash; occasional: hair loss and dry skin; rare: changed hair color, hairy, acne.

3. Digestive system: occasionally: difficulty swallowing, liver damage / jaundice, rectal disease, colitis, gastrointestinal bleeding, intestinal perforation, and gastric ulcer.

4, urogenital system: common: nocturia; occasional: vaginal irritation, testicular enlargement, urinary tract infections, erectile pain, delayed ejaculation; rare: dysuria, enuresis, urinary incontinence, amenorrhea, abnormal ovarian function, pelvic infection , Cystitis, difficulty in sexual intercourse, and pain in ejaculation.

5. Blood / Tumor: Rare: Lymphatic system disease, anemia, and pancytopenia.

6, musculoskeletal system: rare: musculoskeletal chest pain.

7. Nervous system: common: ataxia, epilepsy, muscle cramps, dyskinesia, dystonia; occasional: dilated pupils, dizziness, and difficulty speaking; rare: abnormal EEG, abnormal neurological examination, attention impairment, Sciatica and aphasia.

8, neuropsychiatric system: common: mania / mild mania, decreased libido, hallucinations, decreased sexual function, depression; occasional: memory impairment, personality split, psychosis, pronunciation difficulties, emotional instability, paranoia, Abnormal thinking, coldness; rare: suicidal tendency.

9. Oral diseases: common: stomatitis; occasional: toothache, bruxism, gingival swelling, mucosal edema; rare: glossitis.

10. Respiratory system: occasional: bronchitis and shortness of breath / dyspnea: rare: epistaxis, respiratory rhythm disorder, pulmonary embolism.

11, special feeling: occasional: visual disturbances; rare: diplopia.

12. Non-specific reactions: common: cold-like symptoms; occasional: non-specific pain; rare: abnormal body odor, surgical-related pain, infection.

(3) Volunteers related to bupropion report that the following adverse events may not be related to the drug:

1, the whole body: joint pain, myalgia, rash with fever, and other delayed allergic symptoms, these symptoms are similar to serum disease.

2. Cardiovascular: Hypertension (some cases are more serious), orthostatic hypotension, degree block.

3. Endocrine: abnormal antidiuretic hormone secretion syndrome, hypoglycemia, hyperglycemia, male breast development, diabetes, and unstable hormone levels.

4. Digestive tract: esophagitis, hepatitis, liver damage.

5. Hemolymphatic system: ecchymosis, leukocytosis, leukocytosis, thrombocytopenia.

6, musculoskeletal: joint pain, myalgia, muscle stiffness / fever / rhabdomyolysis, muscle weakness.

7, nerves: coma, delirium, abnormal dreams, bradykinesia with exposure.

8. Skin and accessories: Stevens-Johnson symptoms, angioedema, exfoliative dermatitis, and urticaria.

9, special feeling: tinnitus.

Bupropion contraindications

1. Those with a history of epilepsy should not use this product.

2. This product is contraindicated in patients who are using other drugs containing bupropion.

3. This product is contraindicated in patients with bulimia or anorexia.

4. Those who are allergic to bupropion or any of the ingredients contained in this product are prohibited from using this product.

5. Patients who abstain from alcohol or sedatives are prohibited from using this product.

6. It cannot be used in combination with a monoamine oxidase (MAO) inhibitor. The interval between the monoamine oxidase inhibitor and this product should be at least 14 days.

Bupropion precautions

1. This product cannot be used in combination with other drugs containing bupropion hydrochloride.

2. Epilepsy.

The recommended dose of bupropion is not more than 300 mg / d, and the incidence of epilepsy between 450 and 600 mg / d will increase nearly ten times. It can be seen that the occurrence of epilepsy has a significant correlation with the dose. Sudden administration or an increase in dose will increase the incidence of epilepsy, which can occur during treatment or can occur several weeks after a stable dose is obtained. In addition, many factors can increase the likelihood of seizures. Therefore, individual factors, clinical conditions, and synergistic medication should be considered when applying bupropion.

Individual factors: Due to individual differences, the ability to metabolize and eliminate bupropion is also different, which will increase the incidence of epilepsy. Traumatic brain injury, intermittent epilepsy, central nervous system tumors, and severe liver cirrhosis can reduce the epilepsy threshold and induce epilepsy.

Clinical situation: The surrounding environment can cause epilepsy; Abuse of alcohol, sudden withdrawal of opium, cocaine or other addictive drugs during the use of alcohol and sedatives; excessive use of stimulants or sleeping pills; oral hypoglycemic agents or insulin therapy hypertension.

Synergistic use: At present, some drugs and treatments can lower the threshold and increase the incidence of epilepsy, such as: other antidepressants, sedatives, theophylline, and steroids, etc. Withdrawal.

Suggestions for reducing the incidence of epilepsy: Based on the research progress of bupropion and reviewing the clinical application, the following measures can reduce the incidence of epilepsy:

The daily total amount of bupropion is less than or equal to 450 mg / d; it is taken in three divided doses of less than or equal to 150 mg / d to avoid peak blood concentrations of bupropion and / or metabolites; the dose is gradually increased.

Bupropion should be used with caution in patients with a history of epilepsy, traumatic brain injury, and other patients with an epilepsy-prone constitution; it should be used in combination with other drugs (such as diazepam, antidepressants, theophylline, and steroids). Be cautious; under certain treatments (such as the sudden discontinuation of benzodiazepines), they should be used with caution, as these will reduce the threshold for seizures.

3. Irritability and insomnia. Some patients taking bupropion will experience restlessness, irritability, anxiety, and insomnia, especially shortly after starting treatment. In clinical studies, these symptoms sometimes require sedative / hypnotic treatment. Symptoms in 2% of patients were severe enough to require discontinuation of bupropion.

4. There is currently no clinical experience in the safe dosage of bupropion in patients with myocardial injury or heart disease, so this group of patients should be used with caution. Depression patients with a history of orthostatic hypotension who are receiving tricyclic antidepressants can tolerate bupropion well. The same was true of 36 hospitalized patients with congestive heart failure. However, bupropion caused an increase in supine blood pressure in patients with congestive heart failure, and two patients were removed from the group because they were well above baseline blood pressure.

5. Use with caution in patients with liver damage. Patients with severe cirrhosis should be extremely cautious when applying bupropion, to reduce the dosage and the number of medications. When taking this product, the maximum dose of this part of patients should not exceed 75mg, once a day. Patients with mild to moderate cirrhosis also need to reduce the frequency and / or dose.

All patients with liver damage are closely monitored for adverse reactions reflecting levels of bupropion and its metabolites.

6, with caution in patients with renal dysfunction. No kidney damage has been reported. Bupropion is extensively metabolized, converted into its active metabolites in the liver, and further metabolized in the kidneys and eliminated in vitro. Patients with kidney injury should use bupropion with caution. To reduce the frequency and / or dose, bupropion and its metabolites in this group of patients are more likely to accumulate than healthy people. Adverse reactions reflecting levels of bupropion and its metabolites should be closely monitored.

7. This product may cause allergic reactions. Allergies / allergic reactions requiring treatment such as skin pruritus, urticaria, angioedema, and dyspnea have been reported during bupropion clinical trials. In addition, bupropion-induced lupus erythematosus, Stevens-Johnson syndrome, and anaphylactic shock were reported during the after-sales monitoring period. Patients with a history of allergies or allergic / anaphylaxis symptoms (such as rash, pruritus, urticaria, chest pain, edema, shortness of breath) should discontinue bupropion and consult a doctor.

Delayed allergic reactions (arthralgia, myalgia, fever with rash and other symptoms) caused by bupropion have been reported. These symptoms are very similar to serum sickness.

8. Psychiatry, insanity and other neuropsychiatric symptoms : Patients taking bupropion have reportedly caused more common mental phenomena, such as hallucinations, illusions, difficulty concentrating, paranoia and confusion. Reduce the dose or stop the medicine, the above phenomenon will be reduced, or even disappear.

9. Suicide, suicidal attempts will occur in depression patients themselves, and may continue until there is significant relief. Bupropion should be taken from the smallest dose.

Medication for pregnant and lactating women

At present, there is no sufficient comparative research data used by pregnant women to prove the safety of this product, so pregnant women should not use it. If it must be used, the pros and cons should be fully weighed. Bupropion and its metabolites can be secreted through breast milk. Considering the potential effects of this product on infants, it is not suitable for breastfeeding women. If it is necessary, the necessity of this product for the mother should be fully evaluated to determine whether to stop Use this medication for breastfeeding.

Medication for children

The clinical study of this product does not include people under 18 years of age. Therefore, the effectiveness and safety of the drug in children are not yet clear.

Medication for elderly patients

There is no significant difference in the safety and effectiveness of this product in elderly patients and young patients, but some elderly patients may be more sensitive to this product and the risk of drug accumulation in the body is increased. Because this product and its metabolites are mainly metabolized by the kidneys, elderly patients should carefully choose the appropriate dose and test their functions at the same time.

Bupropion drug interactions

Drugs metabolized by cytochrome P450B6: In vitro tests show that bupropion is mainly metabolized by P450B6 isoenzymes, so there is a potential interaction with other drugs that affect P450B6 isoenzymes. Bupropion can be widely metabolized, so the combination of other drugs will affect its clinical efficacy. For example, some drugs can induce the metabolism of bupropion (carbamazepine, phenobarbital, phenytoin), and some drugs can inhibit the metabolism of bupropion (such as: cimetidine). Clinical trials involving 24 healthy volunteers have shown that concomitant use of cimetidine can affect the pharmacokinetics of bupropion and its active metabolites. After oral administration of 300 mg of this product, whether or not 800 mg of cimetidine was co-administered had no effect on the pharmacokinetics of the prototype and hydrogenated metabolites, but the AUC and Cmax of threonine hydrobupropion and erythrombohydrobupropion Increased by 16% and 32%, respectively.

Cytochrome P450D6 metabolism drugs: Many drugs (including antidepressants, -blockers, antiarrhythmic drugs and antipsychotic drugs) can be metabolized by CYPD6. In vitro tests have shown that bupropion and oxybupropion are inhibitors of this enzyme. One study involved 15 male subjects, all of whom were extensive metabolizers of the CYPIID6 enzyme. The results showed that after taking bupropion 150 mg twice a day, and then taking desipramine 50 mg once, Will increase the Cmax, AUC, and half-life of desipramine by about 2, 5, and 2.5 times, respectively. Therefore, bupropion should be used with caution in combination with other drugs metabolized by the CYPIID6 enzyme. These drugs include certain antidepressants (eg, nortriptyline, mipamin, dexipramine, paroxetine, fluoxetine, sertraline), antipsychotics (eg, haloperidol, risperidine) Ketones, methiodazine), -blockers (eg, metoprolol), IC antiarrhythmic drugs (eg, propafenone, piperamide), and the minimum dose should be used at the beginning of combined treatment . When taking bupropion in patients who are being treated with CYPIID6 enzyme metabolism drugs, it should be considered to reduce the dose of the original drug, especially those with a narrow therapeutic index.

MAO inhibitors: Animal studies have shown that monoamine oxidase inhibitor (MAOI) acetophenone can increase the acute toxicity of bupropion.

Levodopa: Clinical data indicate that the incidence of side effects may increase after the simultaneous use of ketone and levodopa. Patients taking levodopa should take caution when taking this product at the same time, starting from the minimum dose and then gradually increasing the amount.

Drugs that lower the seizure threshold: When this product is used in combination with drugs that lower the seizure threshold (such as antipsychotics, antidepressants, theophylline, systemic steroids, etc.) or therapy (such as sudden interruption of benzodiazepines) Be extremely careful.

Bupropion overdose

There are very few reports of deaths caused by overdose of this product. Overdose may induce seizures. Other serious reactions include hallucinations, loss of consciousness, and sinus tachycardia. Close ECG monitoring is recommended within the first 48 hours after overdose to maintain airway patency, oxygenation, and ventilation, while providing general supportive therapy and symptom monitoring. It is not recommended to induce vomiting. If necessary, gastric lavage can be given after taking the medicine or when certain symptoms occur, while keeping the airway open.

You should also prepare activated carbon. There are no reports of forced diuresis, dialysis, or blood transfusions during excessive use. No specific antidote is currently available. During the course of treatment, various symptomatic treatments should also be taken, such as benzodiazepine treatment during seizures.

Bupropion Specifications

75mg

Bupropion storage

Store in a sealed, dry place at room temperature (10-30 ° C).

Bupropion Expert Review

Bupropion belongs to the aminoketone class of antidepressants. Applicable to patients with depressive depression and depression who have no obvious or intolerable effect on other antidepressants. Long-term high-dose administration can produce a down-regulating effect of -adrenergic receptors ^[1] .