What is Bupropion?
Bupropion, available under the brand names Zyban and Wellbutrin, is an antidepressant medication used in the treatment of smoking cessation therapy. Studies have shown Bupropion to be extremely useful in dealing with nicotine withdrawal and cravings. Chemically, it is an aminoketone and, in addition to alleviating nicotine withdrawal symptoms, helps treat symptoms of depressed mood, irritability, difficulty concentrating, and increased appetite. Bupropion is FDA-approved as a smoking cessation aid for adult depression and seasonal affective disorder and is on the WHO’s list of essential medicines.
How does it work?
Though the exact Bupropion mechanism is still under evaluation, studies have shown that Bupropion exhibits a dual mechanism of action involving norepinephrine and dopamine reuptake, which enables it to have a unique clinical profile in comparison to other medications in the same category. Bupropion exerts its effect primarily through inhibiting dopamine reuptake into neuronal synaptic vesicles, preventing nicotine from attaching to dopamine receptors, and subsequently reducing cravings. It is also a weak noradrenaline reuptake inhibitor. Through its inhibitory effects, it helps treat smoking withdrawal symptoms safely.
At the postsynaptic acetylcholine nicotinic receptors, Bupropion antagonizes the effect of nicotine and blocks its pharmacological effects in addition to inhibiting the nicotine-induced vesicular release of dopamine. These added qualities further help people with chronic nicotine addiction become abstainers and live healthy lives.
How long does it take to work?
Bupropion is available in immediate release, sustained release, and extended release formulations, of which sustained release Bupropion is used in smoking cessation therapy. Bupropion SR attains a peak plasma concentration within 3 hours of ingestion and is unaffected by food intake.
How long does it stay in your system?
The mean elimination half-life of Bupropion after chronic dosing is 21 ±9 hours, and steady-state plasma concentrations of Bupropion are reached within eight days. After completing its half-life, it is eliminated from the body as a metabolic waste.
How to take Bupropion
Immediate Release Bupropion is available in strengths of 75 mg and 100 mg. Extended-release formulations are available in strengths of 100 mg, 150 mg, and 200 mg, and sustained-release formulations are available in a single strength of 150 mg. The medication must be initiated 1-2 weeks before the quit date. You are started on one tablet daily of 150 mg for the first three days, after which you must take two 150 mg tablets daily. Bupropion dosage should not exceed 300 mg a day, while taking care to put a gap of at least 8 hours between either tablet intake.
What are the side effects?
The most common side effects associated with the use of Bupropion are:
- Mild side-effects - nausea, constipation, changes in your sense of taste, frequent urination, drowsiness, and headaches
- Moderate side-effects -dry mouth, ringing in the ears, difficulty falling or staying asleep, stomach pain, uncontrollable shaking of one side of the body, and muscle or joint pain.
- Severe side-effects - fever, hives, hoarseness, swelling of the face, throat, and tongue, chest pain, and difficulty swallowing or breathing.
Because of the moderate dose and safety profile of the medication as a smoking cessation aid, side effects are relatively rare. But if Bupropion side effects persist or increase in intensity, stop using the medication immediately and get urgent medical help.
Drug interactions
Bupropion with Beta blockers : Beta-blockers like Atenolol, Labetalol, and Metoprolol, when used concomitantly with Bupropion, can decrease the metabolism of the beta-blockers and lead to hypotension.
Bupropion with Oral Steroids : Oral Steroids like Dexamethasone and Methylprednisolone, when combined with Bupropion, can increase the patient’s risk of seizures.
Bupropion with Antidepressants :Antidepressants like Citalopram and Desipramine, combined with Bupropion, can increase the risk of seizures and increase the medications’ plasma concentrations.
Bupropion with Sedatives : Sedatives like Tamoxifen and Theophylline, when used simultaneously with Bupropion, can reduce its effectiveness, leading to adverse reactions and delayed treatment.
How to use
Bupropion is a prescription medication and should only be used in conditions of
- Smokers above 18 years of age
- In people with a healthy body and mind
- People who do not respond to other smoking cessation programs.
The dosage of Bupropion is dependent on
- Your age
- Presence of systemic conditions
- Physicians advice
- Tolerance of the drug
- The severity of nicotine addiction
Things to remember when using Bupropion
- Set a date for quitting smoking and start the drug a week or two before the set p.m.
- Avoid using it after 5 pm as the medication can cause trouble sleeping
- The use of the medication can be within 7–12 weeks, extend up to six months, and vary from patient to patient.
- It can be taken with or without food.
- You will not observe immediate results, but it will take a few weeks for the effects to be observed.
- Inform your medical practitioner about any history of seizures, brain tumors, head injuries, or an eating disorder, or if you are taking antipsychotics, tranquilizers, or other antidepressants, before starting Bupropion
FAQ's
Studies regarding the efficacy and tolerability of Bupropion in overweight and obese women have shown the drug to be more effective than a placebo in achieving the desired weight change. It took Bupropion 8 weeks to lose 5% of baseline BMI, and the medication was well tolerated during the entire study. Further studies have found that obese adults who took Bupropion SR in 300 mg or 400 mg doses lost 7.2% to 10% of their body weight over 24 weeks and maintained that weight loss at 48 weeks.
Bupropion is only available on prescription in the UK, and you’ll usually need to see your general practitioner or contact an NHS stop-smoking service to get it. You can even order the medication online through registered smoking cessation aid portals, and have the drug safely delivered to your doorstep.
Clinical studies and Bupropion reviews from patients and health practitioners have proved it is an effective anti-smoking medication. In addition to reducing nicotine cravings, it effectively helps deal with the withdrawal symptoms frequently observed by smokers trying to quit. It is among the very few medications FDA-approved in the US and is said to help 1 in every 5 people trying to quit smoking.
The sleep, energy, and appetite changes as a result of nicotine withdrawal start improving within the first 1-2 weeks of use of Bupropion. This is important because improving physical symptoms show that the drug is working. It takes another 6–8 weeks for the depressed mood and lack of interest in activities to improve and for you to completely get over the withdrawal effects of abstaining from nicotine use.
Bupropion is contraindicated in the following conditions:
⦁ Patients below the age of 18
⦁ Pregnant or breastfeeding ladies
⦁ In patients with a pre-existing seizure disorder
⦁ In patients with neuropsychiatric disorders like intracranial mass, substance disorders, bulimia, and anorexia nervosa
⦁ In patients with severe liver dysfunction
⦁ In patients with a history of alcoholism or those undergoing benzodiazepine withdrawal
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