What is Wellbutrin used for. How does bupropion work as an antidepressant. What are the potential side effects of taking Wellbutrin. Who should avoid using bupropion. How should Wellbutrin be taken properly. What drug interactions are possible with bupropion. When should you consult a doctor about Wellbutrin.

What is Wellbutrin and How Does it Work?

Wellbutrin is the brand name for the medication bupropion, an antidepressant used to treat depression and seasonal affective disorder (SAD). It is also prescribed as a smoking cessation aid under the brand name Zyban. Bupropion works differently from other antidepressants – instead of affecting serotonin levels, it acts on the neurotransmitters norepinephrine and dopamine in the brain.

How exactly does bupropion improve mood and help with depression? Bupropion inhibits the reuptake of norepinephrine and dopamine, allowing these neurotransmitters to remain active in the brain for longer periods. This boost in norepinephrine and dopamine activity is thought to alleviate depressive symptoms and improve mood.

Key Facts About Wellbutrin:

• Drug class: Norepinephrine-dopamine reuptake inhibitor (NDRI)
• Available as immediate-release, sustained-release (SR), and extended-release (XL) tablets
• Typically takes 4-6 weeks to reach full antidepressant effect
• Also used off-label for ADHD, bipolar depression, and sexual dysfunction

Indications and Uses for Wellbutrin

The FDA has approved Wellbutrin for the following uses:

1. Major Depressive Disorder (MDD)

Wellbutrin is primarily prescribed to treat major depressive disorder in adults. It can help alleviate symptoms like persistent sadness, loss of interest in activities, changes in appetite or sleep, and difficulty concentrating.

2. Seasonal Affective Disorder (SAD)

Bupropion XL is approved to prevent episodes of major depressive disorder in patients with a history of seasonal affective disorder. It is typically started in the fall before symptoms of SAD begin and continued through winter.

3. Smoking Cessation

Under the brand name Zyban, bupropion is used as part of a comprehensive smoking cessation program. It can help reduce cravings and withdrawal symptoms associated with quitting smoking.

Are there any off-label uses for Wellbutrin? Yes, doctors sometimes prescribe bupropion for other conditions not officially approved by the FDA, including:

• Attention deficit hyperactivity disorder (ADHD)
• Bipolar disorder (depressive phase)
• Sexual dysfunction caused by other antidepressants
• Obesity (for its potential appetite-suppressing effects)

Potential Side Effects and Risks of Taking Wellbutrin

While Wellbutrin can be an effective treatment for depression, it’s important to be aware of potential side effects. Common side effects of bupropion include:

• Dry mouth
• Nausea
• Insomnia
• Agitation or anxiety
• Constipation
• Headache
• Dizziness
• Increased sweating

Can Wellbutrin cause more serious side effects? In rare cases, bupropion may lead to more severe adverse reactions, including:

Seizures

Bupropion can lower the seizure threshold, especially at higher doses. The risk is higher in people with a history of seizures or eating disorders.

Psychiatric Effects

Some patients may experience worsening depression, suicidal thoughts, or unusual changes in behavior, particularly when first starting the medication or during dose adjustments.

Cardiovascular Effects

Bupropion can cause an increase in blood pressure and heart rate in some individuals.

Allergic Reactions

While rare, some people may experience severe allergic reactions to bupropion, including symptoms like rash, itching, swelling, severe dizziness, or trouble breathing.

Who Should Avoid Taking Wellbutrin?

Wellbutrin is not suitable for everyone. Certain individuals should avoid taking bupropion or use it with caution under close medical supervision. These include:

• People with a history of seizures or epilepsy
• Individuals with eating disorders like anorexia or bulimia
• Those with bipolar disorder, as bupropion may trigger manic episodes
• People with severe liver or kidney disease
• Individuals taking monoamine oxidase inhibitors (MAOIs)
• Pregnant or breastfeeding women (unless the benefits outweigh the risks)

Is Wellbutrin safe for children and adolescents? The safety and efficacy of bupropion have not been established in individuals under 18 years of age. The FDA has issued a black box warning about an increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults taking antidepressants.

Proper Usage and Dosage Guidelines for Wellbutrin

To maximize the benefits of Wellbutrin while minimizing potential side effects, it’s crucial to take the medication exactly as prescribed by your healthcare provider. Here are some general guidelines for taking bupropion:

Dosage Forms

Wellbutrin is available in three formulations:

• Immediate-release tablets (taken 3 times daily)
• Sustained-release (SR) tablets (taken twice daily)
• Extended-release (XL) tablets (taken once daily)

Starting Dose

The typical starting dose for depression is:

• Immediate-release: 100 mg twice daily
• Sustained-release: 150 mg once daily
• Extended-release: 150 mg once daily

How should the dose be adjusted? Your doctor may gradually increase your dose based on your response and tolerability. The maximum recommended dose varies depending on the formulation and indication.

Timing of Doses

Take Wellbutrin at the same time(s) each day. For the extended-release version, it’s often recommended to take it in the morning to minimize sleep disturbances.

Duration of Treatment

Antidepressant treatment typically continues for at least 6-12 months after symptom improvement. Never stop taking Wellbutrin abruptly without consulting your doctor, as this can lead to withdrawal symptoms.

Potential Drug Interactions with Wellbutrin

Wellbutrin can interact with various medications, potentially altering their effectiveness or increasing the risk of side effects. Some important drug interactions to be aware of include:

Monoamine Oxidase Inhibitors (MAOIs)

Combining bupropion with MAOIs can lead to potentially life-threatening reactions. A gap of at least 14 days is required between stopping an MAOI and starting Wellbutrin, or vice versa.

Other Antidepressants

Using bupropion with other antidepressants, especially SSRIs or SNRIs, may increase the risk of serotonin syndrome.

Antipsychotics

Bupropion may affect the metabolism of certain antipsychotic medications, potentially altering their effectiveness or side effect profile.

Seizure Threshold Lowering Drugs

Combining Wellbutrin with other medications that can lower the seizure threshold (e.g., tramadol, theophylline) may increase seizure risk.

CYP2D6 Substrates

Bupropion inhibits the CYP2D6 enzyme, which can affect the metabolism of various drugs including certain antidepressants, antipsychotics, beta-blockers, and opioids.

Are there any food interactions with Wellbutrin? While there are no significant food interactions, excessive alcohol consumption should be avoided as it may increase the risk of seizures.

Monitoring and Follow-up While Taking Wellbutrin

Regular monitoring is essential when taking Wellbutrin to ensure its effectiveness and safety. Your healthcare provider will likely schedule follow-up appointments to assess your progress and any potential side effects.

Initial Weeks of Treatment

During the first few weeks of treatment, you may need more frequent check-ins. Your doctor will monitor for any worsening of depression or emergence of suicidal thoughts, particularly in younger patients.

Blood Pressure and Heart Rate

Regular monitoring of blood pressure and heart rate is important, especially if you have pre-existing cardiovascular conditions.

Symptom Improvement

Your doctor will assess the effectiveness of the medication in improving your depressive symptoms. It may take 4-6 weeks to experience the full benefits of Wellbutrin.

Side Effect Management

Any side effects you experience will be evaluated and managed. This may involve adjusting the dosage or considering alternative treatments if necessary.

Long-term Use

For patients on long-term Wellbutrin therapy, periodic reassessment of the need for continued treatment is recommended.

When should you contact your doctor immediately while taking Wellbutrin? Seek immediate medical attention if you experience severe side effects such as seizures, severe allergic reactions, significant changes in mood or behavior, or any signs of serotonin syndrome (e.g., agitation, hallucinations, rapid heart rate, fever, excessive sweating, shivering, or muscle stiffness).

Wellbutrin vs. Other Antidepressants: Comparative Efficacy and Side Effect Profiles

Wellbutrin (bupropion) differs from other commonly prescribed antidepressants in its mechanism of action and side effect profile. Understanding these differences can help patients and healthcare providers make informed decisions about treatment options.

Mechanism of Action

Unlike selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs), Wellbutrin primarily affects the neurotransmitters norepinephrine and dopamine. This unique mechanism may make it more effective for certain symptoms of depression, such as fatigue and lack of motivation.

Efficacy

Studies have shown that Wellbutrin is generally as effective as SSRIs in treating depression. It may be particularly beneficial for patients who haven’t responded well to SSRIs or who experience specific symptoms like low energy or difficulty concentrating.

Side Effect Comparison

Wellbutrin tends to have a different side effect profile compared to SSRIs:

• Less likely to cause sexual dysfunction or weight gain
• More likely to cause insomnia, agitation, or seizures (at higher doses)
• Less likely to cause gastrointestinal side effects like nausea or diarrhea

How does Wellbutrin compare to specific antidepressants? Here’s a brief comparison with some commonly prescribed medications:

Wellbutrin vs. Prozac (fluoxetine)

Prozac is an SSRI that may be more sedating than Wellbutrin. It’s more likely to cause sexual side effects and weight gain but less likely to cause insomnia or agitation.

Wellbutrin vs. Zoloft (sertraline)

Zoloft, another SSRI, may be more effective for anxiety symptoms compared to Wellbutrin. It’s more likely to cause gastrointestinal side effects and sexual dysfunction.

Wellbutrin vs. Effexor (venlafaxine)

Effexor is an SNRI that affects both serotonin and norepinephrine. It may be more effective for pain symptoms associated with depression but can cause more significant withdrawal symptoms if stopped abruptly.

The choice between Wellbutrin and other antidepressants depends on individual factors such as specific symptoms, medical history, potential drug interactions, and personal preferences regarding side effects. Always consult with a healthcare provider to determine the most appropriate treatment option.

Bupropion (Oral Route) Description and Brand Names

Description and Brand Names

Drug information provided by: IBM Micromedex

US Brand Name

1. Aplenzin
2. Budeprion SR
3. Budeprion XL
4. Buproban
5. Forfivo XL
6. Wellbutrin
7. Wellbutrin SR
8. Wellbutrin XL
9. Zyban

Descriptions

Bupropion is used to treat depression and to prevent depression in patients with seasonal affective disorder (SAD), which is sometimes called winter depression. It is also used as part of a support program to help people stop smoking.

Bupropion is sold under different brand names. If you are already taking medicine for depression or to help you stop smoking, discuss this with your doctor before taking bupropion. It is very important that you receive only one prescription at a time for bupropion.

This medicine is available only with your doctor’s prescription.

This product is available in the following dosage forms:

• Tablet, Extended Release, 24 HR
• Tablet, Extended Release, 12 HR
• Tablet
• Tablet, Extended Release

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Bupropion tablets (Depression/Mood Disorders)

What is this medicine?

BUPROPION (byoo PROE pee on) is used to treat depression.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Wellbutrin

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:

• an eating disorder, such as anorexia or bulimia
• bipolar disorder or psychosis
• diabetes or high blood sugar, treated with medication
• glaucoma
• heart disease, previous heart attack, or irregular heart beat
• head injury or brain tumor
• high blood pressure
• kidney or liver disease
• seizures
• suicidal thoughts or a previous suicide attempt
• Tourette’s syndrome
• weight loss
• an unusual or allergic reaction to bupropion, other medicines, foods, dyes, or preservatives
• breast-feeding
• pregnant or trying to become pregnant

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You can take it with or without food. If it upsets your stomach, take it with food. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not stop taking this medicine suddenly except upon the advice of your doctor. Stopping this medicine too quickly may cause serious side effects or your condition may worsen.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is less than four hours to your next dose, take only that dose and skip the missed dose. Do not take double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:

• linezolid
• MAOIs like Azilect, Carbex, Eldepryl, Marplan, Nardil, and Parnate
• methylene blue (injected into a vein)
• other medicines that contain bupropion like Zyban

This medicine may also interact with the following medications:

• alcohol
• certain medicines for anxiety or sleep
• certain medicines for blood pressure like metoprolol, propranolol
• certain medicines for depression or psychotic disturbances
• certain medicines for HIV or AIDS like efavirenz, lopinavir, nelfinavir, ritonavir
• certain medicines for irregular heart beat like propafenone, flecainide
• certain medicines for Parkinson’s disease like amantadine, levodopa
• certain medicines for seizures like carbamazepine, phenytoin, phenobarbital
• cimetidine
• clopidogrel
• cyclophosphamide
• digoxin
• furazolidone
• isoniazid
• nicotine
• orphenadrine
• procarbazine
• steroid medicines like prednisone or cortisone
• stimulant medicines for attention disorders, weight loss, or to stay awake
• tamoxifen
• theophylline
• thiotepa
• ticlopidine
• tramadol
• warfarin

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Tell your doctor if your symptoms do not get better or if they get worse. Visit your doctor or healthcare provider for regular checks on your progress. Because it may take several weeks to see the full effects of this medicine, it is important to continue your treatment as prescribed by your doctor.

This medicine may cause serious skin reactions. They can happen weeks to months after starting the medicine. Contact your healthcare provider right away if you notice fevers or flu-like symptoms with a rash. The rash may be red or purple and then turn into blisters or peeling of the skin. Or, you might notice a red rash with swelling of the face, lips or lymph nodes in your neck or under your arms.

Patients and their families should watch out for new or worsening thoughts of suicide or depression. Also watch out for sudden changes in feelings such as feeling anxious, agitated, panicky, irritable, hostile, aggressive, impulsive, severely restless, overly excited and hyperactive, or not being able to sleep. If this happens, especially at the beginning of treatment or after a change in dose, call your healthcare provider.

Avoid alcoholic drinks while taking this medicine. Drinking excessive alcoholic beverages, using sleeping or anxiety medicines, or quickly stopping the use of these agents while taking this medicine may increase your risk for a seizure.

Do not drive or use heavy machinery until you know how this medicine affects you. This medicine can impair your ability to perform these tasks.

Do not take this medicine close to bedtime. It may prevent you from sleeping.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• breathing problems
• changes in vision
• confusion
• elevated mood, decreased need for sleep, racing thoughts, impulsive behavior
• fast or irregular heartbeat
• hallucinations, loss of contact with reality
• increased blood pressure
• rash, fever, and swollen lymph nodes
• redness, blistering, peeling, or loosening of the skin, including inside the mouth
• seizures
• suicidal thoughts or other mood changes
• unusually weak or tired
• vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

• constipation
• headache
• loss of appetite
• nausea
• tremors
• weight loss

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F), away from direct sunlight and moisture. Keep tightly closed. Throw away any unused medicine after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

Side Effects, Withdrawal, Dosage, and Interactions

Wellbutrin, also known by the trade name bupropion, is an antidepressant medication. The XL version is an extended-release formula and is usually taken once daily. This prescription is often used to treat seasonal affective disorder, a form of depression occurring during the fall and winter months. It is also a standard treatment for major depression in adults. Zyban, a low-dose form of bupropion, has demonstrated effectiveness for smoking cessation and it has been licensed in the United States and the United Kingdom for this purpose.

Dosage

Doctors typically start people on low doses of the medication and increase it until the ideal dosage is achieved. The full effects of the medication may not be felt for up to four weeks. When stopping the medication, doctors may tell people to taper doses downward for two weeks before complete termination.

Important Considerations Before Use

Before use, talk with your doctor about your medical history. Your doctor will need to know if you have ever had a heart attack, had high blood pressure, diabetes, heart disease, or substance abuse problems. Alcohol can increase the side effects of Wellbutrin, particularly drowsiness.

Tell your doctor about all of your medication allergies. Additionally, tell your doctor and pharmacist which prescription and nonprescription drugs you currently take. Even herbal products like St. John’s Wort can lead to unwanted drug interactions. Wellbutrin, like many antidepressants, can have a dangerous interaction with a class of drugs called monoamine oxidase inhibitors (MAOIs). If you currently take a MAOI or have stopped taking one within the last two weeks, your doctor will likely not prescribe Wellbutrin. Examples of these drugs include Marplan (isocarboxazid), Nardil (phenelzine), and Emsam (selegiline).

Wellbutrin is not approved for use in people younger than 18.

Important Information During Use

• Let your doctor know if you are breastfeeding, pregnant, or plan to become pregnant.
• Be mindful of worsening depression or thoughts of suicide. There is a small risk of suicide or self-harm with any antidepressant.
• Take this medication exactly as prescribed. Do not double up in the event of a skipped dose, and do not take more than your prescribed dosage. Do not chew or crush the tablets because this causes the drug to be released too quickly.
• Taking Wellbutrin with food will prevent stomach upset.
• You may see something that looks like a tablet in your stool. This is actually the empty casing for the medicine and does not mean that you did not get your dosage.

Side Effects

Rare, adverse psychiatric side effects of this medication may include anger, paranoia, hallucinations, and hostility. Other serious effects may include:

• Seizures
• Irrational fears
• Fever
• Rash, blisters, or hives
• Itching
• Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• Hoarse voice
• Trouble breathing or swallowing
• Chest pain
• Muscle or joint pain
• Rapid, pounding, or irregular heartbeat

Less serious side effects of this drug can include:

• Drowsiness
• Excitement
• Dry mouth
• Dizziness
• Headache
• Nausea or vomiting
• Weight loss
• Constipation
• Excessive sweating

Withdrawal

Withdrawal from Wellbutrin is usually not considered dangerous. Gradual tapering of the dose minimizes any withdrawal effects while allowing faster reinstatement of the medication should symptoms of depression return. Possible symptoms of withdrawal may include:

• Nausea or vomiting
• Intense and frequent dreams
• Headache
• Vertigo
• Changes to senses and perception
• Numbness of extremities

References:

1. Medication Guide Wellbutrin XL. (June 2011). Retrieved from http://www.fda.gov/downloads/Drugs/DrugSafety/UCM172744.pdf
2. Use of Psychiatric Medications for Mental Health Concerns. (n.d.). Retrieved from https://www.uhs.uga.edu/caps/medications.html
3. Wellbutrin XL – bupropion hydrochloride tablet, extended release. (December 2009). Retrieved from http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=14812

Page content reviewed by James Pendleton, ND

Naltrexone/Bupropion (Contrave) for Weight Loss – STEPS

Naltrexone/bupropion (Contrave) combines an opioid receptor antagonist (naltrexone) with a dopamine and norepinephrine reuptake inhibitor (bupropion) in an extended-release tablet. It is labeled as an adjunct to increased physical activity and a reduced-calorie diet for chronic weight management in adults who have a body mass index (BMI) of at least 30 kg per m² or who have a BMI of at least 27 kg per m² with one or more weight-related comorbidities such as type 2 diabetes mellitus, hyperlipidemia, or hypertension.

SAFETY

Safety concerns with bupropion include depression, hypertension, and risk of seizures, whereas acute opioid withdrawal and opioid overuse have been associated with naltrexone.1 Naltrexone/bupropion is labeled as increasing the risk of depression and suicidal behavior, based on studies of bupropion alone that showed an increase in the incidence of these events. However, clinical trials of the combination compared with placebo found no increase in depression and no increase in suicidality.2–4 Naltrexone/bupropion should not be given to children or adolescents. Because it may raise blood pressure and heart rate, it should not be used in patients with uncontrolled high blood pressure. It also should not be prescribed to patients with a known seizure disorder or those already taking opioids. The total daily dosage of naltrexone/bupropion should not exceed two tablets twice a day.1

Although one of the goals of weight loss is to decrease the risk of cardiovascular outcomes, patients with active cardiovascular disease, including significant heart failure, history of myocardial infarction, angina, or stroke, were excluded from premarketing studies. A large cardiovascular outcomes study that includes these patients is now ongoing. Bupropion is metabolized in the liver and its use may increase serum levels of some antidepressants, antipsychotics, beta blockers, and antiarrhythmics. Lower doses of these medications may be needed with concomitant use.1

Naltrexone/bupropion is pregnancy category X. Both components are excreted in breast milk and the medication should not be taken by breastfeeding mothers.1

TOLERABILITY

Gastrointestinal symptoms are common with naltrexone/bupropion. Up to one in three patients will report nausea and 19% will experience constipation, especially early in treatment. Headache, dizziness, and sleep disorders are also common.1 In premarketing studies, about 20% of patients discontinued treatment because of adverse effects.2–5

EFFECTIVENESS

Naltrexone/bupropion has been evaluated in three studies that enrolled more than 4,000 overweight or obese patients with hyperlipidemia or hypertension, and in one study of 505 patients with diabetes. In all studies, naltrexone/bupropion combined with a diet and exercise program for one year resulted in greater weight loss than placebo combined with a diet and exercise program.2–5 About four patients need to be treated with naltrexone/bupropion instead of placebo for one additional patient to achieve at least a 5% weight loss (number needed to treat = 4).2–4 Clinically significant weight loss was also achieved with placebo plus an intensive program of behavior modification, which supports the implementation of intensive interventions when these resources exist. 4 In settings where these resources are not available, naltrexone/bupropion combined with less intensive lifestyle interventions may also achieve clinically significant weight loss for obese patients.2,3

Naltrexone/bupropion has not been compared with other pharmacologic approaches. It is unknown if weight gain occurs after stopping the medication, and patient-oriented outcomes such as the development of osteoarthritis, diabetes, hypertension, cardiovascular disease, and mortality have not been studied.

PRICE

Naltrexone/bupropion costs approximately $212 for a one-month supply.

SIMPLICITY

The dosing of naltrexone/bupropion must be titrated. In week 1, patients should take one 8/90-mg tablet once a day in the morning with a low-fat meal. In week 2, they should increase the daily dosage to one tablet in the morning and one tablet in the evening. During week 3, patients should increase the daily dosage to two tablets in the morning and one tablet in the evening, and in week 4 patients will reach the maximum recommended dosage of two tablets twice a day. 1 Patients with moderate to severe renal impairment should be limited to one tablet twice daily, and patients with moderate hepatic impairment should be limited to one tablet daily.1 If patients do not lose 5% of their baseline body weight after 12 weeks, further treatment is unlikely to be beneficial and therapy should be discontinued.1 If patients achieve clinically significant weight loss after 12 weeks, therapy should be continued for up to one year. Naltrexone/bupropion has not been studied beyond 56 weeks.2–5

Is Wellbutrin a Narcotic?

While Wellbutrin isn’t a narcotic, that doesn’t mean it doesn’t have the potential for misuse. For the most part, Wellbutrin is considered to be a relatively safe antidepressant. However, since Wellbutrin affects the “feel-good” brain neurotransmitters norepinephrine and dopamine, it is sometimes taken to achieve a stimulant-like high. When Wellbutrin is taken in high doses or in dangerous ways, such as intravenously, it may act similarly to a stimulant. People who use Wellbutrin recreationally may have doses up to 1200 mg at a time, while the maximum daily dose of the drug is 450 mg for prescription use.

Along with injecting Wellbutrin, some recreational users will crush the tablets to snort them. This provides all of the effects of the drug directly into the bloodstream at one time and bypasses the time-release elements of Wellbutrin. It’s extremely dangerous, however, and can cause serious health problems. For example, Wellbutrin can be caustic when it’s injected. It can damage tissues significantly as a result. In some places, such as Canada, recreational Wellbutrin use has led to the rise of the nickname “poor man’s cocaine.”

Another reason Wellbutrin is often confused with or compared to narcotics is because it does cause physical dependence in many users. Physical dependence isn’t the same as a psychological addiction. Dependence means the person’s body depends on the presence of the drug. If someone is dependent on Wellbutrin and tries to stop using it suddenly, they may go through withdrawal. The potential for withdrawal makes it important that the person taking the drug doesn’t stop taking Wellbutrin suddenly without speaking to their healthcare professional. As with other antidepressants, a doctor will usually recommend patients taper down their dosage of Wellbutrin gradually.

For the most part, Wellbutrin is considered a relatively safe and well-tolerated antidepressant. It’s not a narcotic, but there has been a rise in misuse of the drug, especially lately. When taken in high doses or illicit ways such as injecting dissolved tablets, some people may experience a stimulant-like high. Taking Wellbutrin in this way can be dangerous or deadly, however. Wellbutrin isn’t a narcotic, and it’s not especially addictive, but it can lead to physical dependence, so patients should be aware of this when taking it. As with any prescription drug, it should be taken only as directed by a physician.

If you or a loved one is struggling with the weight of an addiction to prescription drugs or anything else, get in touch with The Recovery Village. Whether you just want to ask questions, learn more, or get specific information about going to treatment and how to pay for it, we’re here to provide you with answers.

Facts about Wellbutrin, an anti-depression medicine | | Expert help for your emotional health

By Dr. Ho Anh, 07/22/2020

Chances are, you know someone who takes some sort of psychiatric medicine. According to the National Center for Health Statistics, 12.7% of the U.S. population over age 12 in 2017 took antidepressants in the past month and one in six Americans take some sort of psychiatric drug.

With the prevalence of antidepressants, how do we distinguish between the many types? Wellbutrin is a norepinephrine-dopamine reuptake inhibitor (NDRI) that stands out among the host of selective serotonin reuptake inhibitors (SSRIs), which are the most common drug for depression treatment. SSRIs are known to come with side effects like nausea, insomnia, diarrhea, weight changes, and nervousness.

While SSRIs are also notorious for their unwanted influence on libido and orgasms, Wellbutrin is an antidepressant alternative that has been shown to cause fewer sexual side effects and can even improve sexual function in some cases.

What is Wellbutrin?

Wellbutrin, or bupropion, is an NDRI antidepressant that is FDA approved to treat major depressive disorder (MDD) and seasonal affective disorder (SAD). The drug is prescribed off label to help with bipolar disorder and attention deficit hyperactivity disorder (ADHD).

Because it has also been known to help people quit smoking, the drug could be a good choice for those who are affected by mood disorders and want to quit smoking. Wellbutrin comes in the form of an oral tablet.

What is treatment with Wellbutrin like?

Much like most medication for mood disorders, Wellbutrin works most effectively to decrease the symptoms of depression over the course of a few weeks. In the first 1-2 weeks, physical symptoms related to energy levels, sleep, or appetite tend to improve first, followed by mood improvement and renewed interest in activities in 4-6 weeks.

For long-term improvement, it’s important to keep using bupropion even after symptoms have subsided to ensure depressive symptoms don’t return. However, if you’re taking Wellbutrin to quit smoking, the period of use may be shorter. Please consult your provider on the length of your treatment and do not stop taking or change the dosage without asking your healthcare provider first.

What are some best practices for taking Wellbutrin?

When taking medication that may affect your mood and behavior, it’s important to be diligent about how and when you’re taking it. Here are some best practices for taking Wellbutrin:

1. If you miss a dose, take it as soon as you remember. Never take two doses at once.
2. Avoid alcohol consumption and illegal drug use. It may reduce the effectiveness of the medication and increase the risk of seizures.
3. Do not stop taking Wellbutrin abruptly. The risk of seizure from stopping abruptly is four times greater with Wellbutrin than other depressants.

What are the dosages?

There are three formulations and dosing variations. Please consult your doctor to find the appropriate treatment:

• Immediate release: Wellbutrin is immediate release for MDD, which means it takes effect shortly after the tablet is taken. Dosage can be up to three times a day. A dose usually starts at 100mg twice a day up to three times a day at max 150mg per dose.
• Sustained-release: Treats MDD. Dosage is typically 150mg once a day, potentially 150mg (max 200mg) per day.
• Extended-release: Treats MDD and SAD, starting at 150mg (max 300mg or 450mg) once a day.

What are some possible side effects?

Side effects are usually resolved in the first 1-2 weeks of treatment and are typically mild. Unlike many antidepressants, Wellbutrin does not typically lower libido or cause sexual side effects and is often prescribed along with other antidepressants to counter the sexual side effects other drugs might have. For those with bipolar disorder, Wellbutrin may lead to manic episodes.

The most common side effects are:

• Headaches
• Dry mouth
• Stomach pain
• Sleep difficulties
• Weight loss
• Reduced appetite
• Nausea and dizziness
• Constipation
• Weakness

Rare side effects occur in less than 10% of patients and include:

• Aggressiveness
• Agitation
• Muscle pain
• Skin rash
• Ringing in the ears
• Angle-closure glaucoma
• Skin rash

What are some other drug interactions?

Other drugs may influence how Wellbutrin works or increase side effects:

• Adderall
• Blood thinners
• Diabetes medications (Glucophage)
• Monoamine oxidase inhibitors
• OTC pain relieves (e.g. ibuprofen)

Please consult a medical professional to see if Wellbutrin is a good fit for your condition.

—-

Dr. Ho Anh

Chief Medical Officer at Cerebral

Bupropion (Wellbutrin)

How does this medicine work?

Bupropion (bu-pro-pee-on) is an antidepressant. It regulates the mood by increasing specific brain chemicals. It may be used for:

• depression
• attention deficit and hyperactivity disorders
• anxiety
• quitting smoking

It may also be used to treat other conditions as determined by your doctor.

Bupropion may take up to 12 weeks to build up in the body and produce its fullest effect.

How should I give it?

Bupropion comes in pill form. Your child should take this medicine exactly as prescribed. Give it at regular times every day to keep a steady level in the bloodstream.

Do not stop this medicine without checking with your doctor or nurse practitioner. It should be stopped over a period of time.

___ If your child is taking a short-acting pill, and cannot swallow pills:

• Crush it in a tablet crusher or between 2 spoons, inside a plastic bag, or in folded paper.
• Mix the powder with a very small amount (about 1 teaspoon) of soft food, such as applesauce, chocolate syrup, ice cream, jelly, or yogurt. Make sure your child takes all of the mixture.

___ If the medicine is an extended-release (SR or XL) product, it should be swallowed whole. Tablets should not be cut in half, crushed or chewed.

Are there any precautions about food or other medicines?

Follow the directions for using this medicine provided by your doctor.

Give this medicine with food if it upsets your child’s stomach.

Warning! There are certain medicines that interact with bupropion. Please check with the doctor or pharmacist before giving any other prescription or non-prescription medicine, vitamins, or herbs.

Avoid alcohol-containing foods or beverages while taking this medicine.

What should I do if a dose is missed?

Take the missed dose as soon as you remember, but do not give doses closer than 8 hours apart for extended-release and 6 hours for short-acting. This can cause seizures or convulsion (muscles stiffening and shaking). If it is too close to the next dose, skip the missed dose and continue with the regular schedule. Never give a double dose. If your child misses two doses, call the clinic.

If your child vomits within 30 minutes after a dose, please call the clinic for instructions.

What are the side effects?

Common

• drowsiness
• lightheadedness, dizziness
• headache
• constipation
• dry mouth
• nausea (upset stomach)
• vomiting (throwing up)

Occasional

• tiredness or weakness
• muscle twitching
• possible weight loss
• blurred vision
• trouble sleeping

The person taking this medicine should not drive, operate machinery, or do anything else that could be dangerous until it is known if he or she has any side effects to this medicine.

When should I call the clinic?

• suicidal thinking
• significant worsening of depression
• dizziness, lightheadedness, or fainting
• severe headache
• irregular (fast or pounding) heartbeat
• rash or hives
• confusion or hallucinations (hearing or seeing things that do not exist)
• seizures or convulsions (uncontrollable muscle stiffening and shaking)
• vomiting (if due to this medicine)
• trouble breathing – call 911

What else do I need to know?

This medicine should not be used in children with a history of eating disorders or seizures.

While taking the extended-release form of this medicine, part of the tablet may pass in a bowel movement. This is normal.

You and your child should know the names of all the medicines he or she is taking. Share this information with anyone involved in your child’s care. Please bring the medicine container when your child comes to the clinic or emergency department.

Check the label and expiration date before giving each dose. Ask your pharmacist what to do with outdated or unused medicines. If there is no “take-back” program empty them into the trash.

Store all medicines in their original container and away from direct sunlight or heat. Do not store in humid places such as the bathroom. Keep them out of children’s reach, locked up if possible.

Always make sure you have enough medicine on hand. Each time you refill your prescription, check to see how many refills are left. If no refills are left, the pharmacist will need 2 or 3 days to contact the clinic to renew the prescription.

If too much or the wrong kind of medicine is taken, call the Poison Control Center at 1-800-222-1222. If your child is unconscious or has a seizure, call 911.

Questions?

This is not specific to your child but provides general information. If you have any questions, please call your clinic or pharmacy.

Last reviewed 8/2015 ©Copyright

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90,000 Bupropion gave criminal complications – Newspaper Kommersant No. 29 (6750) dated 18.02.2020

Kommersant learned about a new criminal case related to the drug bupropion – recall that the police and customs of the Russian Federation call it a “drug derivative”, and psychiatrists consider it a legal antidepressant. Astrakhan customs opened a case of drug smuggling on an especially large scale against Olga Kalinovskaya, who is suffering from a psychiatric illness, who received pills by mail.The woman claims that she did not even order the medicine – the package was allegedly a New Year’s gift from a friend who advised her about treatment. Experts point out that bupropion is not banned in Russia, but this does not interfere with judging for its purchase.

Olga Kalinovskaya has lived in Ukraine since 2008, where she was diagnosed with depressive personality disorder. In 2012, a friend of hers, a teacher working with special children, suggested that a woman might also have attention deficit hyperactivity disorder (ADHD).She advised to contact an acquaintance from Norway, who himself lives with ADHD and remotely consults other patients. He confirmed the diagnosis of Olga Kalinovskaya and recommended bupropion for treatment; she several times ordered the drug to Ukraine from an Indian pharmaceutical company without any problems.

Abroad bupropion is absolutely legal and prescribed by doctors as an antidepressant or a remedy to help quit smoking. Foreign pharmaceutical companies produce bupropion tablets under different names: Zyban, Elontril, Wellbutrin.Until 2016, it was sold in Russia, and the Ministry of Health even included it in the standards for the provision of medical care. But then the manufacturer left the Russian market and revoked the license from the State Register of Medicines. By law, such drugs can be bought and sold as dietary supplements without a license.

In 2017, Olga Kalinovskaya with her husband and child returned to Volgograd to look after her elderly mother. The woman went through a psychiatric commission, but Russian doctors did not confirm ADHD. She was given a different diagnosis (she asked not to disclose it to the media) and prescribed treatment.Ivan Martynikhin, a member of the executive committee of the Russian Society of Psychiatrists, told Kommersant that ADHD is poorly diagnosed in Russia: “Doctors do not know that it persists in adults as well. I see patients who come in with a depressive disorder and ADHD is at the root of it. ”

At the same time, the psychiatrist emphasized that one should not engage in self-examination: “Only half of the patients who came to see me and complained of ADHD, the syndrome was actually confirmed. ”

At the end of December 2019, Kalinovskaya received a notification about the delivery of an unknown parcel from India.She was detained at the post office – it turned out that there were 300 bupropion tablets in the package. According to Ms. Kalinovskaya, this was a complete surprise for her. Later, the woman found out that the drug was sent by the same patient-consultant from Norway. “He didn’t warn me, he sent me pills for his money. He explained that he knew about my problem and just wanted to help, ”Olga Kalinovskaya said. As a result, the Astrakhan customs opened a criminal case against Mrs. Kalinovskaya under Part 3 of Art. 229.1 of the Criminal Code of the Russian Federation (drug smuggling on an especially large scale, the maximum punishment is up to 20 years in prison).Customs experts believed that the tablets contained “derivatives” of the illicit drug ephedrone.

As Kommersant has already told, at the beginning of 2019, Russian law enforcement agencies began to arrest citizens who order drugs with bupropion in foreign online stores. The fact is that since 2012 in Russian legislation there is the concept of “derivatives of narcotic drugs” – this is the name for substances created by a slight change in the chemical formula of a drug. “Derivatives” are not included in the list of prohibited substances, but are still considered a drug.This formulation appeared in the framework of the fight against new types of drugs, primarily “spice” – manufacturers quickly changed parts of the formula, which allowed for some time to sell the drug without the threat of punishment. However, lawyers and narcologists even then criticized the idea of ​​“derivatives” for legal uncertainty: they warned that sooner or later legal pharmaceuticals would be banned.

About ten criminal cases of bupropion smuggling are now known, at least two people are in jail.

At the same time, the Russian Society of Psychiatrists (ROP) in August 2019 published an official conclusion that bupropion is not a drug and does not lead to dependence. Ivan Martynikhin, a member of the ROP executive committee, said that patients had contacted the community with a request to add bupropion to the clinical guidelines. The psychiatrist told Kommersant that the drug has practically no analogues and “kills two birds with one stone: bupropion is not bad in treating depression and affects the cause – attention deficit hyperactivity disorder.”Ivan Martynikhin noted that bupropion has no severe side effects, which is important for patients with bipolar depression. Moreover, the drug can be prescribed in addition to the main drugs to correct side effects.

Legal consultant on drug-related cases, expert of the Institute of Human Rights Arseny Levinson draws attention to the fact that no Russian legal act fixes the prohibition of bupropion for circulation in the Russian Federation, nowhere is it officially stated that it is considered a drug.“If a person does not read the news, then they have no place to know that bupropion is recognized by the police as a derivative of ephedrone,” says Mr. Levinson. “Obviously, such a person cannot commit smuggling, a crime involving direct intent. In other words, the person must know that he is committing a crime and be willing to do so. How could Olga Kalinovskaya know that a medicine that she freely bought in Ukraine suddenly turned out to be a drug in Russia? ” According to him, “the authorities stubbornly ignore” the problem of criminal liability for “derivatives”.Mr. Levinson participates in the work of the Duma working group on improving anti-drug legislation; in the summer of 2019, he talked there about the bupropion situation. “The representative of the Ministry of Internal Affairs said that they are aware of the problem, that the police are humanly sorry for those who are persecuted for purchasing drugs for medical reasons, but nothing needs to be changed,” said Arseniy Levinson.

“As a result, I face 20 years in prison for inaccuracies in the legislation,” says Olga Kalinovskaya.

Recall that the first criminal case of bupropion smuggling was initiated in April 2019 by the Ural customs against Daria Belyaeva, who ordered an antidepressant from Poland. As the girl’s lawyer Irina Ruchko told Kommersant, in January 2020 the case was returned for the third time for further investigation – with the wording that the investigation “did not specify the circumstances of socially dangerous acts”. According to her, now the investigator intends to send several inquiries: “At least, to the medical institution where Daria was treated – to find out what drugs she was prescribed in connection with the disease.And in the Ministry of Health – to find out the attitude of the department to bupropion. ”

The lawyer said that the investigator himself became the subject of a departmental audit: “Initially, the defense was familiarized with the decree on the appointment of an examination on bupropion, where the expert was asked five questions. And then the same decision appeared in the materials of the case, only with three questions. In simple terms, this means that the investigator changed one decision for another. ” The lawyer sent a petition, after which the ICR conducted a check on the actions of the investigator.“The results are not yet known to me, but I very much doubt that a criminal case will be opened,” she said.

During the investigation, Daria Belyaeva was assigned an additional psychiatric examination – the girl was declared insane. “If the court concludes that she is guilty, then she will be sent for compulsory outpatient treatment,” the lawyer explained. “That is, she is not threatened with a colony now. But this situation puts pressure on her – after all, she already had a serious illness.Of course, it is not easy for her to endure. ” “Let’s hope that the case will be dismissed without trial on exonerating grounds,” says Arseniy Levinson. “It is clear that there is no public danger in the actions of a patient who acquires a medicine that is legal all over the world for use on medical grounds.”

Elizaveta Lamova, Alexander Chernykh

90,000 On the narcogenic potential of bupropion – News

On the narcogenic potential of bupropion

26 August 2019, 06:27
Ivan Martynikhin

In 2019, Russia opened several criminal cases against persons who purchased the antidepressant bupropion abroad and imported into Russia (for example, this, this, etc.). Due to the factual equating of bupropion with narcotic drugs, a significant number of people with mental disorders in Russia who used it for therapeutic purposes were forced to refuse to take it (about this, for example, here and here).

Below are the answers of the ROP to the questions formulated in the lawyer’s request received by the ROP from the lawyer of one of the accused in a criminal case related to the purchase of bupropion.

1.Are there any data on scientific studies of the efficacy and safety of Bupropion conducted in Russia? Did they show the addictive potential of the drug?

In the GRLS database (http://grls.rosminzdrav.ru/default.aspx) there is no data on the studies of bupropion in Russia. The drug had a registration certificate LSR-008003/10 from 08/12/2010 to 08/22/2016 with the trade name Wellbutrin (CJSC GlaxoSmithKline Trading).

In open sources in English (https: // clinicaltrials.gov) there are 3 completed large multicenter RCTs of bupropion, in which centers from Russia participated.

In the 2 published studies, there is no indication that bupropion has addictive potential or provokes abuse in research subjects.

In addition, these two RCTs found no critical tolerability or safety issues.The reported AEs [adverse events] are consistent with more than 30 years of international post-marketing surveillance experience that demonstrates a favorable tolerability and safety profile for therapeutic doses of bupropion.

2. Is there scientific evidence for the development of Bupropion drug dependence syndrome?

There is currently no reliable [evidence] data indicating the addictive potential of bupropion.

3. Is it possible to assert that the drug Bupropion has a low addictive potential – i.e. does not cause euphoria and addiction syndrome or is it extremely rare?

Yes, according to available data (national pharmacopoeias, official documents of the FDA and EMA, APA, NIMH and NICE guidelines, instructions for the drug with different trade names from Europe, Asia and America, etc.) bupropion does not cause euphoria, addiction syndrome and not subject to massive abuse.

4. Can the agent Bupropion, registered in many countries of the world as an antidepressant, included in the state register of medicines of the Ministry of Health of the Russian Federation as a therapeutic agent and which has been in existence since 2010? to 2016 in the public domain (civil circulation in the Russian Federation) without any restrictions, contain a narcotic component that would allow it to be included in the list of narcotic and / or potent drugs, the circulation of which in the Russian Federation is limited by law?

From the standpoint of clinical pharmacology and narcology, bupropion cannot be classified as a narcotic drug solely because of its structural chemical affinity for the stimulant ephedrone / methcathinone.

From the formal standpoint of the current regulatory document, such a classification is possible ( Decree of the Government of the Russian Federation of June 30, 1998 . N 681 “On approval of the list of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation” with amendments and additions dated 6 February, 17 November 2004, 8 July 2006, 4 July 2007, 22 June, 21, 31 December 2009, 21 April, 3, 30 June, 29 July, 30 October, 27 November, 8 December 2010 r., February 25, March 11, July 7, October 6, December 8, 2011, February 22, March 3, April 23, May 18, September 4, October 1, November 19, 23, 2012, February 4, 26, June 13, July 10, September 9, November 7, December 16, 2013, March 22, May 31, June 23, October 25, December 9, 2014, February 27, April 9, May 8, July 2, October 12 2015, 1 April 2016, 18 January, 21 February, 25 May, 12, 29 July 2017, 28 March, 22 June, 19 December 2018 )

Definition of derivatives of narcotic drugs and psychotropic substances according to the Decree of the Government of the Russian Federation No. 681:

6.Derivatives of narcotic drugs and psychotropic substances are substances of synthetic or natural origin that are not included in independent positions in the state register of medicines or in this list, the chemical structure of which is formed by the replacement (formal substitution) of one or more hydrogen atoms, halogens and (or) hydroxyl groups in the chemical structure of the corresponding narcotic drug or psychotropic substance into other monovalent and (or) divalent atoms or substituents (with the exception of hydroxyl and carboxyl groups), the total number of carbon atoms in which should not exceed the number of carbon atoms in the initial chemical structure of the corresponding narcotic drug or psychotropic substances.

If one and the same substance can be classified as a derivative of several narcotic drugs or psychotropic substances, it is recognized as a derivative of a narcotic drug or psychotropic substance, the change in the chemical structure of which requires the introduction of the smallest number of substituents and atoms.

5. Is Bupropion registered and is Bupropion still being used in the treatment of patients in other countries? Are there any restrictions on its circulation in other countries?

Bupropion is registered for several indications (depression, tobacco addiction, etc.)) and is used in many countries of the near and far abroad (USA, European countries, Turkey, India, countries of Southeast Asia).

Existing restrictions apply to the ability to prescribe bupropion by doctors of other specialties (in particular, in the UK and some other countries of Western and Northern Europe, a prescription for bupropion can be prescribed by general practitioners at the first visit of people with mild to moderate depressive and neurotic conditions), as well as insurance coverage and the availability of the drug on the “preferential lists”.

6. Does the drug for which the Russian Federation issued an unlimited passport of the drug LSR-008003/10 for medical use, which has an international non-proprietary, grouping or chemical name – Bupropion, however, is currently excluded from the state register of drugs of the Russian Federation – the status “unregistered medicinal product (preparation) “?

Yes, from 22.08.2016 bupropion does not have a registration certificate valid in Russia.

8. Is Bupropion included in the List of narcotic drugs and psychotropic substances, the circulation of which in the Russian Federation is prohibited in accordance with the legislation of the Russian Federation, international treaties?

No, at present bupropion is not included in the “List of narcotic drugs, psychotropic substances and their precursors, the circulation of which in the Russian Federation is prohibited in accordance with the legislation of the Russian Federation and international treaties of the Russian Federation ( list I )”, “The list of narcotic drugs and psychotropic substances, the circulation of which in the Russian Federation is limited and in respect of which control measures are established in accordance with the legislation of the Russian Federation and international treaties of the Russian Federation ( list II )”, as well as the “List of psychotropic substances, the circulation of which in The Russian Federation is limited and in respect of which the exclusion of certain control measures is allowed in accordance with the legislation of the Russian Federation and international treaties of the Russian Federation ( list III ) “

9.Can it be a derivative of a narcotic drug – a drug previously registered in the Russian Federation as a medicinal product, introduced into the GRLS without any restrictions on its circulation?

The broad interpretation of “Definitions of derivatives of narcotic drugs and psychotropic substances according to the Decree of the Government of the Russian Federation No. 681” makes it possible to classify as a derivative of a narcotic drug even drugs available on the market and having unlimited circulation , for example, sumatriptan and zolmitriptan (as derivatives of psychotomimetic N, N- dimethyltryptamine).

10. Have any restrictions been established by the board of the Eurasian Economic Commission on the import or export of Bupropion on the territory of the member states of the Eurasian Economic Union?

Currently, there are no EEC restrictions in the public domain regarding the import or export of bupropion in the territory of the EAEU countries.

11. Does Bupropion have the same addictive (narcogenic) properties with Ephedrone, to call it an analogue of Ephedrone, i.e.?That is, classify it as a narcotic drug, if so, which ones?

See the answer to question 3. Currently, from the standpoint of evidence-based medicine, bupropion lacks addictive (narcogenic) properties, incl. properties, ephedrone.

The psychostimulating effect of bupropion does not allow users of stimulants to use it for recreational purposes – at doses higher than therapeutic, its tolerance is noticeably impaired, and in therapeutic doses the specific stimulating effect does not reach the effect of even the “weak” illegal stimulants.

12. Can some (partial) structural similarity of one drug to another with addictive potential be a sufficient basis for attributing addictive properties to the first drug?

See the answer to questions 4 and 9. “Definition of derivatives of narcotic drugs and psychotropic substances in accordance with the Decree of the Government of the Russian Federation No. 681” leaves a lot of space for public and professional discussion, i.This norm was developed without cooperation with the expert community (psychiatrists, narcologists, clinical pharmacologists, specialists in organic synthesis, etc.).

13. Is Bupropion included in the list of narcotic and / or potent drugs, the circulation of which in the Russian Federation is limited by law?

See answer to question 8.

One of the documents that explains the use (but not circulation) of bupropion is the Order of the Ministry of Sports of Russia dated 03.12.2018 N 976 “On approval of the lists of substances and (or) methods prohibited for use in sports” (Registered in the Ministry of Justice of Russia on 26.12.2018 N 53177)

Section II (Substances and Methods Prohibited in Competition), clause 9. Stimulants (S6) states that bupropion is not included in the list of prohibited substances :

Clonidine, topical / ophthalmic imidazole derivatives, as well as stimulants included in the 2019 monitoring program (bupropion, caffeine, nicotine, phenylephrine, phenylpropanolamine, pipradrol and synephrine) are allowed.

Tags:

drugs (8) criminal code (2) bupropion (1)

Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^® , contains all the information you need to know about the drug, including the indications, route of administration, side effects and when you should contact your healthcare provider.

Trade names: USA

Aplenzin; Forfivo XL; Wellbutrin SR; Wellbutrin XL; Zyban [DSC]

Trade names: Canada

MYLAN-BuPROPion XL; ODAN Bupropion SR; PMS-BuPROPion SR; RATIO-BuPROPion SR [DSC]; TARO-Bupropion XL; TEVA-Bupropion XL; Wellbutrin SR; Wellbutrin XL; Zyban

Warning

• Drugs like this have increased the likelihood of suicidal thoughts or actions in children and young people.This risk may be higher in people who have attempted suicide or have had suicidal thoughts in the past. All people taking this drug must be closely monitored. Call your doctor right away if you have signs such as depressed mood (depression), nervousness, anxiety, grumpiness, or anxiety attacks, or if other mood or behavior changes occur or worsen. Call your doctor immediately if you have suicidal thoughts or attempted suicides.

What is this drug used for?

• The drug is used to treat depression.
• Used to prevent seasonal affective disorder (SAD).
• It is used for smoking cessation.
• This medicinal product may be used for other indications. Consult your doctor.

What do I need to tell my doctor BEFORE taking this drug?

• If you are allergic to this drug, any of its ingredients, other drugs, foods or substances.Tell your doctor about your allergy and how it manifested itself.
• If you have ever had a seizure.
• If you abuse alcohol and suddenly stop using it.
• If you are taking certain other drugs, such as anticonvulsants or tranquilizers, and you stop using them abruptly.
• If you have ever had an eating disorder such as anorexia or bulimia.
• If you have any of the following health conditions: kidney disease or liver disease.
• If you have taken a drug for depression or Parkinson’s disease in the past 14 days. These include isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline. An episode of very high blood pressure may occur.
• If you are taking any of the following drugs: linezolid or methylene blue.
• If you are taking another drug that contains the same drug.

This list of drugs and diseases that may be adversely associated with this drug is not exhaustive.

Tell your doctor and pharmacist about all the medicines you take (both prescription and over-the-counter, natural products and vitamins) and your health problems. You need to make sure that this drug is safe for your medical conditions and in combination with other drugs you are already taking. Do not start or stop taking any drug or change the dosage without your doctor’s approval.

What do I need to know or do while taking this drug?

For all patients taking this drug:

• Tell all healthcare providers that you are taking this drug. These are doctors, nurses, pharmacists and dentists.
• Avoid driving or doing other tasks or work requiring attention or sharp eyesight until you know how this drug is affecting you.
• This drug may interfere with some lab tests. Tell all healthcare providers and lab staff that you are taking this drug.
• Do not stop taking this drug suddenly without talking to your doctor. This can increase the risk of side effects. If necessary, this drug should be stopped gradually as directed by your doctor.
• High blood pressure has happened with this drug.Monitor your blood pressure as directed by your doctor.
• This drug may increase the risk of seizures. The risk may be increased in people taking higher doses of the drug, with certain health problems, or in those using certain other drugs. People who abruptly stop drinking large amounts of alcohol or stop taking certain medications (such as drugs used for anxiety, insomnia, or seizures) are also at higher risk.Talk to your doctor to see if you are at increased risk of seizures.
• Avoid drinking alcohol while taking this drug.
• Consult your doctor before using marijuana, other forms of cannabis, prescription or over-the-counter drugs that may slow you down.
• It may take several weeks to achieve full effect.
• This drug is not approved for use in children.Consult your doctor.
• If you are 65 years of age or older, use this drug with caution. You may have more side effects.
• Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. The benefits and risks for you and your child will need to be discussed.

If you smoke:

• Not all drugs are approved for smoking cessation purposes. Check with your doctor to make sure you are getting the right drug.
• New or worsening mental, mood, or behavioral disorders have been reported with bupropion for smoking cessation. These disorders include thoughts of committing suicide or homicide, depression, violent behavior, rage, anxiety, and anger. These disorders were observed in people who had mental and mood disorders in the past, and those who did not have such disorders. Consult your doctor.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, some people with this drug can cause serious and sometimes deadly side effects. Call your doctor or get medical help right away if you have any of the following signs or symptoms, which may be associated with serious side effects:

• Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
• Signs of high blood pressure, such as very severe headache, or dizziness, or loss of consciousness, or blurred vision.
• Feeling confused, unable to concentrate, or changes in behavior.
• Hallucinations (a person sees or hears something that is not in reality).
• If the seizures become more frequent or severe after starting the medication.
• Chest pain, angina pectoris, tachycardia or irregular heart rhythm.
• Inflammation.
• Shortness of breath.
• Change in hearing.
• Ringing in the ears.
• Frequent urination.
• Swelling of the gland.
• Impaired motor function.
• The risk of eye problems may be increased in some patients with this drug. Your doctor may order you to see an ophthalmologist to see if you are at increased risk of developing these eye problems. Call your doctor right away if you have eye pain, change in vision, swelling, or redness around the eye.
• Possible severe skin reaction (Stevens-Johnson syndrome / toxic epidermal necrolysis). This can lead to serious and permanent health problems and sometimes death. Get immediate medical attention if you experience symptoms such as redness, skin swelling with blistering or scaling (with or without a high fever), redness or irritation of the eyes, and ulceration in the mouth, throat, nose, or eyes.

What are some other side effects of this drug?

Any medicine can have side effects. However, many people have little or no side effects. Call your doctor or get medical help if these or any other side effects bother you or do not go away:

All forms of issue:

• Dizziness or headache.
• Constipation, diarrhea, abdominal pain, nausea, vomiting, or decreased appetite.
• Shiver.
• Nervous tension and agitation.
• Strange or unusual dreams.
• Gas.
• Dry mouth.
• Sleep disorders.
• Joint or muscle pain.
• Nose or throat irritation.
• Excessive sweating.
• Unexplained weight fluctuations.

Extended release tablets:

• Some brand name tablets can sometimes be seen in the stool.For these brands, this is normal and not a cause for concern. If you have any questions, please consult your doctor.

This list of potential side effects is not comprehensive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Office.

You can report side effects to the FDA at 1-800-332-1088.You can also report side effects at https://www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your healthcare practitioner. Read all the information provided to you. Follow all instructions strictly.

For all purposes of this preparation:

• Do not take this medicine more often than prescribed. This can increase your risk of developing seizures.Make sure you know at what intervals you need to apply the drug.
• Take in the morning if you are taking this drug once a day.
• Take this medication with or without food.
• If you cannot sleep, do not take this drug before bed. Consult your doctor.
• Swallow whole. Do not chew, break, or crush.
• Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.
• If you have difficulty swallowing, consult your doctor.

To quit smoking:

• You can take this drug for 1 week before you stop smoking.
• Nicotine replacement and counseling can be done at the same time for better results.
• If you have not been able to quit smoking after 12 weeks of taking this drug, talk to your doctor.
• When you are trying to quit smoking, you may have symptoms of nicotine withdrawal, even when using drugs like this drug to help quit smoking.There are many signs of nicotine withdrawal symptoms. People who try to quit smoking have occasional depression and suicidal thoughts. Check with your doctor.

What to do if a dose of a drug is missed?

• Skip the forgotten dose and return to your normal schedule.
• Do not take 2 doses at the same time or an additional dose.

How do I store and / or discard this drug?

• Store at room temperature, protected from light.Store in a dry place. Do not store in the bathroom.
• Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
• Dispose of unused or expired drugs. Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. Your area may have drug recycling programs.

General information on medicinal products

• If your health does not improve or even worsens, see your doctor.
• Do not give your medicine to anyone or take other people’s medicines.
• Some medicines may come with other patient information sheets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• A separate patient instruction sheet is included with the product. Please read this information carefully. Reread it each time you replenish your supply. If you have questions about this drug, talk with your doctor, pharmacist, or other healthcare professional.
• If you think there has been an overdose of a drug, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Consumer Use and Limitation of Liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are appropriate for a particular patient. This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient.Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a guide to treatment and does not replace the information provided to you by your healthcare professional. Check with your doctor for complete information on the possible risks and benefits of taking this drug.Use of this information is governed by the Lexicomp End User License Agreement available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

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© UpToDate, Inc. and its affiliates and / or licensors, 2021. All rights reserved.

instructions, use, analogues of the drug, composition, indications, contraindications, side effects in the reference book of medicines from UNIAN

Application of Wellbutrin

Wellbutrin – composition and release form of the drug

Wellbutrin: how to take the drug

Wellbutrin – contraindications, side effects

Velbutrin’s analogs

Wellbutrin – psychoanaleptic, antidepressant.

Application of Wellbutrin

Indication.

Treatment of major depressive conditions.

Wellbutrin – composition and release form of the drug

Composition:

active substance: 1 tablet contains 150 mg of bupropion hydrochloride;

excipients: microcrystalline cellulose, hypromellose, cysteine ​​hydrochloride monohydrate, magnesium stearate, white dye concentrate (Opadry OY-7300 White or Opadry YS-1-18202-A White), carnauba wax, black food paint.

Dosage form. Sustained-release film-coated tablets.

Wellbutrin: how to take the drug

Method of administration and dosage.

The drug begins to act no earlier than 14 days after the start of therapy. As with other antidepressants, the full effect of the drug is observed only after a few weeks of treatment.

Wellbutrin tablets should be swallowed whole, without splitting, crushing or chewing, as this may increase the risk of side effects, including convulsions.

The maximum single dose should not exceed 150 mg. Wellbutrin tablets should be used 2 doses per day with an interval between doses of at least 8 hours.

Wellbutrin – contraindications, side effects

Contraindications.

Wellbutrin is contraindicated in patients with hypersensitivity to bupropion or to any of the components of the drug.

Wellbutrin is contraindicated in patients with seizures.

Wellbutrin is contraindicated in patients who have now suddenly stopped using alcohol or sedatives.

Wellbutrin tablets contain bupropion, so they should not be prescribed to patients receiving any other drug containing bupropion, since the incidence of seizures is dose-dependent.

Wellbutrin is contraindicated in patients with present or a history of bulimia nervosa or anorexia nervosa, since in this group of patients there was a high incidence of seizures when prescribing a quick-release form of bupropion.

Simultaneous administration of Wellbutrin and monoamine oxidase inhibitors is contraindicated.At least 14 days should elapse between the cancellation of irreversible MAO inhibitors and the start of treatment with Wellbutrin.

Adverse reactions.

From the immune system: hypersensitivity reactions such as urticaria, more severe hypersensitivity reactions, including angioedema, shortness of breath / bronchospasm or anaphylactic shock.

From the side of metabolism and digestive disorders: anorexia, weight loss, impaired blood glucose levels.

From the psyche: insomnia, sleep disturbance, agitation, anxiety, depression, dysphoria, disorientation, aggressiveness, hostility, irritability, anxiety, hallucinations, unusual dreams, depersonalization, delirium, paranoid thinking, suicidal thoughts and suicidal behavior, psychosis , euphoria, mania, hypomania, changes in mental state.

From the central nervous system: headache, tremor, dizziness, taste disturbances, memory disturbances, anxiety, myoclonus, dystonia, migraine, attention disorders, vertigo, akathisia, dysarthria, convulsions, EEG disturbances, dystonia, ataxia, parkinsonism, movement coordination disorder, memory impairment, paresthesia, fainting, coma, delirium, sensitivity disorders, dyskinesia.

From the side of the organs of vision: visual disorder, diplopia, mydriasis, increased eye pressure.

On the part of the hearing organs: ringing in the ears.

From the heart: tachycardia, heart rhythm disturbances, ECG changes, myocardial infarction, increased blood pressure, edema, palpitations.

From the side of the vessels: increase in blood pressure (in some cases significant), redness, vasodilation, postural hypotension.

From the digestive tract: dry mouth, gastrointestinal disorders, including nausea and vomiting, abdominal pain, constipation, dyspepsia, toothache, gum irritation, intestinal perforation.

From the hepatobiliary system: increased levels of liver enzymes, jaundice, hepatitis.

Skin and subcutaneous tissue disorders: rash, itching, sweating, polymorphic erythema and Stevens-Johnson syndrome, exacerbation of psoriasis, alopecia.

Respiratory system: pulmonary embolism, bronchitis.

From the musculoskeletal system and connective tissues: muscle twitching, arthritis, rhabdomyolysis.

From the kidneys, urinary and reproductive system: infections of the urinary system: decreased libido, increased frequency of urination and / or retention, erectile dysfunction, menstrual irregularities, gynecomastia, testicular edema, glucosuria, nocturia.

General disorders: fever, chest pain, asthenia.

From the side of the blood system: leukocytosis, leukopenia, thrombocytopenia.

Analogs of Velbutrin

no

Source: State Register of Medicines of Ukraine. The instructions are published with abbreviations for information only. Before use, consult your doctor and read the instructions carefully. Self-medication can be harmful to your health.

90,000 in the State Duma are asked to deal with criminal cases on the purchase of antidepressants – RT in Russian

The State Duma asks the Prosecutor General’s Office to find out whether the actions of law enforcement officers who initiate criminal proceedings against Russians due to the purchase of drugs based on bupropion abroad are legal. This substance is not included in the list of prohibited drugs and until 2016 was freely sold in Russia, but now experts of the customs services consider it to be a derivative of ephedrone, the circulation of which is prohibited.Experts point out that in many cases it is impossible to find an alternative to bupropion. At the same time, patients say that they are afraid to purchase the drug, despite the fact that their condition worsens without it.

State Duma Deputy Yaroslav Nilov appealed to the Prosecutor General’s Office and the Ministry of Health with a request to find out why criminal cases are being opened against Russians for acquiring and moving across the customs border of the Russian Federation an antidepressant based on bupropion, which is not prohibited in Russia. Customs officers have recently begun to equate it with ephedrone, which is on the list of prohibited substances.

According to the parliamentarian, the reason for the deputy’s request was an appeal to him by an initiative group of citizens who are in dire need of this medicine, which suddenly found itself under an unofficial ban.

In the appeal that RT got acquainted with, the members of the initiative group ask the deputy to find out on what basis criminal proceedings are being instituted for the acquisition of an unlawful drug. They also propose, if necessary, to amend federal legislation so that law-abiding citizens in need of treatment are not prosecuted for drug smuggling.

The circulation also notes that bupropion has no analogues and in many cases there are no alternatives to its use.

“The drug is one of the most frequently prescribed antidepressants in the world due to its high proven efficacy. For many in Russia, it is the only treatment for their mental illness. At the same time, an ordinary person will never be able to guess which substance can be recognized as a derivative and equated to a drug, ”the authors of the appeal write.

Nilov notes that law enforcement officers have opened criminal cases earlier because of drugs that citizens use for medical purposes.

“We need to understand whether criminal cases are being legally initiated against those who buy and consume bupropion,” the deputy said. – Earlier, there were already cases when citizens were tried to be unjustifiably brought to justice. Everyone remembers the resonant story of Ekaterina Konnova, who was accused of drug dealing when she tried to sell surplus of a psychotropic drug not registered in Russia, which her child was taking. “

Found as a derivative

Until 2016, bupropion-based drugs were freely sold in Russian pharmacies, but after that they were excluded from the list of drugs, since the importer did not renew the license. However, no ban was imposed on ordering medicines abroad.

As RT found out, in the spring of 2019, customs officers and law enforcement officers began to prosecute citizens who purchase drugs based on bupropion in foreign online stores, which is not officially included in the lists of drugs prohibited in Russia.

One of the first criminal cases under the article on drug smuggling (according to part 3 of article 229.1 of the Criminal Code) was initiated against a resident of Yekaterinburg, Daria Belyaeva, who suffers from schizotypal personality disorder.

As reported by RT, a criminal case was opened against Belyaeva after she ordered the antidepressant Elontril in Poland, which includes bupropion. The pills themselves and bupropion were not included in the list of substances prohibited for import, but during the examination it was found that it was theoretically possible to make drugs from them.

Thus, the forensic service of the Customs Administration concluded that the product can be considered as a derivative of ephedrone. Whether it is possible to obtain ephedrone from these tablets is not indicated in the conclusion.

For the purchase of one package of the drug (30 tablets), the girl faces up to 20 years in prison.

Belyaeva’s case was not the only one. According to a RT source in law enforcement agencies, such criminal cases are now being investigated in Moscow, the Volgograd region, Sakhalin and other regions.

At the same time, in some cases, the Russians ordered the drug not abroad, but in Russian online stores. They eventually became involved in criminal cases under Part 2 of Art. 228 of the Criminal Code of the Russian Federation (“Acquisition and storage of narcotic drugs without the purpose of selling”). They face imprisonment for up to ten years.

At the same time, supplies of bupropion to Russia practically stopped. Along with the buyers, law enforcement officers also detained one of the largest sellers, who himself ordered the drug abroad in bulk, and then distributed it with a surcharge in Russia.

“What will happen to me next, I don’t know”

The citizens of the Russian Federation who take the drug say that they are in a desperate situation. According to them, other antidepressants do not help them.

“In 2015, I was admitted to a psychiatric hospital with a diagnosis of schizotypal personality disorder,” says Vladislav Lebedev to RT. – Were treated with antipsychotics, tricyclics. However, my condition only worsened: I could not read, work, study. At some point, I decided to be treated with bupropion and have been taking it ever since.During this time, I was even able to master a new profession. Without bupropion, I’ll become a weak-willed vegetable – there is simply nothing to replace it with. ”

The termination of the supply of the drug, according to RT interlocutors, has already led to a deterioration in health.

“For five years now I have been suffering from derealization and fibromyalgia,” Yaroslav Goncharuk explains in an interview with RT. – I constantly feel weak, muscles all over my body often ache. I have tried many antidepressants and other drugs that are used in such cases, but the combination of bupropion, SSRIs (selective serotonin reuptake inhibitors) and lamotrigine turned out to be ideal for me.Now I do not accept bupropion because it has become dangerous to order it. I got worse, and I don’t know what to do. While drugs are freely sold and bought on the Internet, our police are increasing the rate of detection by unfortunate sick people like Daria Belyaeva. ”

“I fell ill in the spring of 2009,” recalls in an interview with RT one of the Muscovite who signed the appeal to Nilov, who asked not to be named. – Over the years I have tried a lot of different drugs – there was no positive effect.On the contrary, there was muscle weakness and burning pain throughout the body. Only a year ago a new psychiatrist recommended bupropion and two more drugs to me, and it finally took my pain away. Now bupropion has begun to disappear from stores, and without it, the whole maintenance regimen is meaningless. The pills ran out, and now I’m flying back into the abyss. What will happen to me next, I do not know. ”

The medicine must be available

Experts point out that it is incorrect to raise the question of searching for analogues of bupropion or another substance if the medicine helps patients.

“When people die because they cannot get painkillers, this is unnatural,” Oleg Zykov, director of the Institute of Narcological Health of the Nation, commented on the situation to RT. – The task of the officials is to make the medicine available and there is no need to look for any analogues. Of course, it is possible to discuss the narcogenicity of various substances, but there is no common sense in this when it comes to helping patients. ”

Head of the Bureau of Independent Expertise, expert of the Constitutional and Supreme Court of the Russian Federation Yuri Gladyshev believes that in order to avoid criminal prosecution of citizens purchasing drugs for treatment, the term “drug derivatives” should be excluded from criminal law.

“Many substances, including bupropion, are not officially banned, but citizens are sued for their purchase on a regular basis,” explains RT Gladyshev. “The very concept of“ derivatives ”is not clarified in the law, which ultimately allows law enforcement officers to consider them derivatives from prohibited ones.”

Bupropion (Wellbutrin, Zyban, Elontril)

Pharmacological properties
Bupropion is a selective inhibitor of neuronal uptake of catecholamines (norepinephrine and dopamine) with minimal effect on the uptake of indolamines (serotonin) and lack of monoamine inhibition.

Pharmacokinetics
Absorption. After oral administration of bupropion tablets to healthy volunteers, the maximum plasma concentration was reached after 3 hours. Bupropion and its metabolites exhibit linear kinetics with prolonged administration at doses ranging from 150 mg to 300 mg per day. The absorption of bupropion is not significantly increased when consumed simultaneously with food. Distribution. Bupropion is widely distributed – its volume of distribution is approximately 2000 liters.Bupropion and hydroxybupropion bind moderately to plasma proteins (84% and 77%, respectively). The degree of binding to proteins of threohydrobupropion is about half that observed for bupropion. Metabolism. Bupropion is extensively metabolized in the human body. Three pharmacologically active metabolites have been identified in plasma: hydroxybupropion and its amino alcohol isomers – treohydrobupropion and erythrohydrobupropion. Elimination. Approximately 87% of bupropion is excreted in the urine (of which less than 10% is in the form of active metabolites), up to 10% is excreted in the feces.In an unchanged state, only 0.5% of bupropion is excreted. The average clearance after oral administration of bupropion is close to 200 L / h, and the average half-life of bupropion is approximately 20 hours. Patients with renal insufficiency. The effect of kidney disease on the pharmacokinetics of bupropion has not yet been studied. Elimination of the major metabolites of bupropion may be reduced with decreased renal function. Patients with hepatic impairment. The pharmacokinetics of bupropion and its active metabolites in patients with mild to moderate cirrhosis differs little from that in healthy volunteers.In patients with severe cirrhosis of the liver, the maximum concentration of bupropion and the area under the concentration-time curve are significantly increased, and the mean half-life is also lengthened in comparison with healthy individuals. Elderly patients. Pharmacokinetic studies of the elderly give mixed results. Clinical experience has not established a difference in the tolerance of the drug between the elderly and young people, however, a greater sensitivity to it in the elderly cannot be excluded.

Indications for use
Bupropion is intended for the treatment of depressive conditions. If the patient responds positively to treatment, continued therapy with Bupropion is effective in preventing relapse and recurrence of depressive episodes in the future.

Route of administration and dosage
Bupropion tablets should be swallowed whole, without breaking or chewing. Adult use. Initial Treatment: The starting dose is 150 mg once daily.The full antidepressant effect of Bupropion, like other antidepressants, may not appear earlier than a few weeks after the start of treatment. Patients for whom the dose of 150 mg per day is insufficient may experience an improvement when the dose is increased to a maximum of 300 mg per day. The maximum single dose should not exceed 150 mg. Doses of Bupropion exceeding 150 mg per day should be taken in two divided doses at least 8 hours apart. Supportive care: Acute episodes of depression require antidepressant treatment for at least 6 months.It has been established that Bupropion at a dose of 300 mg per day is effective over a long (up to 1 year) period of treatment. Application in children and adolescents. The safety and efficacy of Bupropion in patients under 16 years of age has not been established. Use in patients with impaired liver function. In patients with liver disease, Bupropion should be used with caution. Given the increased variability of the pharmacokinetics of the drug in patients with mild and abstinent liver cirrhosis, decisions must be made about long intervals between doses.In patients with severe liver cirrhosis, Bupropion should be used with extreme caution. In such patients, the dose should not exceed 150 mg every other day.

Side effects
General effect on the body: fever, chest pain, asthenia. The cardiovascular system; tachycardia, vasodilation, postural hypotension, increased blood pressure (in some cases significant), redness, loss of consciousness. Effect on the central nervous system: convulsions, insomnia, tremors, attention disorders, headache, dizziness, depression, disorientation, hallucinations, agitation.anxiety, irritability, aggressiveness, depersonalization. Endocrine and metabolic events: anorexia, weight loss. Gastrointestinal tract: dry mouth, gastrointestinal disorders that include nausea and vomiting, abdominal pain, constipation. Skin and hypersensitivity: rash, itching, sweating. Hypersensitivity reactions that range in severity from urticaria to vascular edema, dyspnea / bronchospasm, rarely anaphylactic shock. Arthralgia, myalgia, and fever have also been described in association with rashes and other symptoms of delayed hypersensitivity.These symptoms may mimic serum sickness. Erythema polymorphism and Stevens-Johnson syndrome are also described as rare side effects. Certain disorders: tinnitus, visual and taste disorders.

Contraindications
Bupropion is contraindicated in patients with hypersensitivity to bupropion or to any of the components of the drug. Bupropion is contraindicated in patients with vascular disorders. Bupropion tablets contain bupropion and should not be given to patients receiving any other drug that contains bupropion, as the incidence of seizures is dose-dependent.Bupropion is contraindicated in patients with a current or history of bulimia nervosa or anorexia nervosa, since this group of patients experienced a higher incidence of seizures when the rapid-release form of bupropion was administered. Concomitant use of Bupropion and monoamine oxidase inhibitors is contraindicated. At least 14 days should elapse between the cancellation of MAO inhibitors and the start of treatment with Bupropion.

Interaction with other drugs
In vitro studies show that bupropion is metabolized to its main active metabolite hydroxybupropion mainly by cytochrome P450 IIB6 (CYP2B6).Therefore, it is necessary to prescribe with caution Wellbutrin simultaneously with drugs that affect the isoenzyme CYP2B6 (for example, orphenadrine, cyclophosphamide, ifosfamide). Although bupropion is not metabolized by the CYP2D6 isoenzyme, in vitro studies of P450 in humans have shown that bupropion and hydroxybupropion are inhibitors of the CYP2D6 metabolic pathway. In human pharmacokinetic studies, administration of bupropion increased plasma levels of desipramine. This effect was observed for at least 7 days after the last dose of bupropion.The concomitant administration of Bupropion with other drugs that are metabolized by the CUR2G6 isoenzyme has not yet been studied. So, simultaneous use with drugs that are metabolized mainly by this isoenzyme (such as individual beta-blockers, antiarrhythmics, antipsychotics) should start with the minimum doses of the concomitant drug. If Bupropion is included in the treatment plan of a patient who is already receiving a drug that is metabolized by CYP2O6, the need to reduce the dose of this drug should be assessed, especially for drugs with a narrow therapeutic index.Since bupropion is extensively metabolized, concomitant administration of drugs that increase metabolism (eg, carbamazepine, phenobarbital, phenytoin) or inhibit metabolism may alter its clinical activity. Limited clinical data demonstrate a higher incidence of neuropsychiatric side effects in patients receiving bupropion concomitantly with levodopa or amantadine. The administration of Bupropion to patients receiving levodopa or amantadine should be administered with caution.Concomitant use of Bupropion and the Nicotine Transdermal System (NTS) may cause an increase in blood pressure.

Overdose
A single dose is described that is 10 times higher than the maximum therapeutic dose. In addition to the actions described in the Side Effects section, the overdose caused symptoms that included drowsiness and loss of consciousness. Treatment: in case of overdose, hospitalization is recommended. Ensure adequate airway patency, oxygenation and ventilation.Soon after an overdose, gastric lavage may be helpful. The use of activated carbon is also recommended. The specific antidote for bupropion is unknown.

Peculiarities of application
Special warnings The recommended dose of Bupropion should not be exceeded, as bupropion is characterized by a dose-dependent development of seizures. At doses that do not exceed the maximum recommended daily dose (150 mg Bupropion twice a day), the incidence of seizures is approximately 0.1% (1/1000).The risk of seizures associated with the use of Bupropion is closely correlated with the presence of risk factors. Therefore, Bupropion should be used with extreme caution in patients with one or more factors that contribute to increased seizure readiness. These factors include: • a history of head trauma; • tumors of the central nervous system; • history of seizures; • concomitant administration of other drugs that lower the seizure threshold. In addition, one should be careful in clinical cases associated with an increased risk of seizures.These include alcohol abuse, abrupt cessation of alcohol or sedatives, diabetes treated with hypoglycemic drugs and insulin, and the use of stimulants or anorexants. Bupropion should be discontinued and not re-prescribed to patients who have experienced seizures during treatment. Bupropion should be discontinued if the patient experiences symptoms of hypersensitivity or anaphylaxis during treatment (skin rash, itching, urticaria, chest pain, edema or dyspnea).Bupropion is extensively metabolized in the liver to active metabolites, which are subject to further metabolism. There was no statistically significant difference in the pharmacokinetics of bupropion in patients with mild to moderate liver cirrhosis compared with healthy volunteers, but the plasma levels of bupropion in individual patients were highly variable. Therefore, Bupropion should be used with caution in patients with liver pathology, reducing the frequency of dosing in patients with mild to moderate liver cirrhosis.Bupropion should be used with extreme caution in patients with severe cirrhosis. In these patients, it is necessary to reduce the frequency of dosing, since the peak concentrations of bupropion in them are significantly increased and accumulation of the drug occurs to a much greater extent than usual. All patients with liver disease should be carefully examined for possible side effects (eg, insomnia, dry mouth, seizures) that may indicate high levels of the drug or its metabolites.Bupropion and its metabolites are excreted primarily by the kidneys. Therefore, the treatment of patients with kidney damage should begin with reduced doses, since bupropion and its metabolites accumulate in such patients to a greater extent than usual. Careful monitoring of the patient is necessary, taking into account possible side effects (for example, insomnia, dry mouth, convulsions), which may indicate high levels of the drug or its metabolites. Clinical experience with bupropion has not shown any difference in tolerance in older people compared to other adult patients.However, a greater sensitivity to the drug in some elderly persons cannot be ruled out. Elderly patients are often characterized by reduced renal function, therefore, the dose must be reduced. As with other antidepressants, there is a risk that Bupropion may accelerate the manic phase in patients with manic-depressive psychosis during the depressive phase of the illness, and may also intensify patent psychoses in other susceptible patients. Pregnancy and lactation The safety of using Bupropion during pregnancy has not been established.Evaluation of studies on animals did not show direct or indirect harmful effects on the development of the embryo and fetus, the course of pregnancy, peri- and postnatal development. A reproductive study in rats showed no impairment of fertility. However, since reproductive studies in animals are not always those that can be applied in relation to humans, the appointment of Bupropion during pregnancy is permissible only in cases where the expected benefit is higher than the possible risk. Since bupropion and its metabolites are excreted in breast milk, it is recommended to stop breastfeeding while taking Bupropion.Influence on the ability to drive a car and other mechanisms. Like other drugs that affect the central nervous system, bupropion can interfere with the ability to perform tasks that require increased attention and coordination. Therefore, patients should be careful when driving and other mechanisms until they are convinced that Bupropion does not impair their function.

Conditions of dispensing from pharmacies
The drug is dispensed by prescription.

Doctors will be spotted on the Internet :: Society :: RBK

Photo: EPA

This year, medical device manufacturers paid Louisville, Kentucky, cardiologist John Mandrole, $ 2,000.dollars for the presentation of their products at various events. However, now he will think twice before agreeing to such deals: US regulators have obliged companies to disclose information about any payments to doctors. In turn, patients will be able to see what their doctor ate and where he flew at the expense of the company whose medications he prescribes.

“Now I will weigh the pros and cons when I get the next offer from the company. After all, soon all payments will be published. Nevertheless, I am concerned that doctors who receive money for joint research with companies may be discredited, while there is nothing wrong with such collaboration, ”John Mandrola told The Wall Street Journal.He himself is now trying in every possible way to avoid representatives of pharmaceutical companies who besiege his clinic: Mandrola is sure that he will find out about the new medicine without the seller’s advice.

Fines do not scare

In the United States, unfair marketing is a common practice in the medical industry. Pharmaceutical companies have hundreds of millions of dollars in budgets to reward doctors. For example, the largest pharmaceutical company Pfizer paid almost $ 175 million for various services to doctors last year.To make them more loyal, tickets for concerts, coupons for visits to spa salons, trips to exotic countries are used. Companies often pay for physicians to attend medical conferences by covering accommodation, food and transportation costs. In addition, they are paid to conduct seminars about the company’s products. In exchange, doctors prescribe the company’s medicine and often advertise it as a fairly versatile remedy for many health problems, while keeping silent about the side effects.

Regulators periodically fine companies for this practice.For example, last year the British GlaxoSmithKline paid a record $ 3 billion fine for the illegal promotion of the antidepressants Paxil and Wellbutrin, medicines for diabetes patients Avandia and a number of other drugs. But in comparison with the profit that these drugs brought, 3 billion is quite a feasible amount.