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Bupropion

Bupropion

Overview

Even before Prozac, there was Wellbutrin (bupropion). It was the first of a new generation of antidepressants and was introduced in 1985, almost two years before Prozac received FDA approval.

The company started shipping Wellbutrin to pharmacies around the country, but before prescriptions could actually be filled, a problem arose. A small study involving 50 women with an eating disorder uncovered an alarming statistic.

Four out of the fifty (8 percent) had suffered a seizure. This unexpected and alarming discovery created consternation at the FDA and the feds had the drug pulled off pharmacy shelves.

The FDA demanded additional tests, but the company resisted, maintaining that the bulimic subjects in the study were not representative of depressed patients. Prior research suggested that the seizure incidence was similar to that for other antidepressants.

For more than a year the company and the FDA argued. Eventually the company capitulated and studied an additional 3,000 patients.

The results redeemed Wellbutrin: The seizure incidence turned out to be 0.4 percent, not that different from other antidepressants and nowhere near the 8 percent seen in the small bulimia study.

Finally, in August 1989, Wellbutrin returned to pharmacy shelves, but it was almost too late. Prozac, introduced in 1987, had become a shooting star. Its incredible popularity made Wellbutrin an also-ran.

Although Wellbutrin works differently from Prozac and similar drugs (Paxil and Zoloft), doctors seemed to remember only the initial concern about seizures.

Despite its initial lack of success in the marketplace, Wellbutrin is roughly comparable to Prozac-like drugs in effectiveness.

Unlike traditional antidepressants, Wellbutrin does not cause weight gain, drowsiness, blurred vision, mental confusion, cardiovascular problems or impaired memory.

And it has one huge advantage over Prozac and other SSRI antidepressants. It does not lower libido, produce impotence or impair orgasms. If anything, Wellbutrin may actually stimulate sexuality for some people.

Side Effects and Interactions

Side effects associated with Wellbutrin include headache, dry mouth, agitation, insomnia, tremor, sweating, skin rash, nausea and constipation.

Other possible side effects include dizziness, nervousness, confusion, weight loss and blurred vision. Report any symptoms to your physician promptly.

Certain other medications may change the metabolism of Wellbutrin: The AIDS drug ritonavir can lead to large increases in the blood levels of the antidepressant, while the antiseizure medicine Tegretol lowers blood concentrations of Wellbutrin.

Taking antipsychotics, antidepressants, theophylline, or oral corticosteroids in combination with Wellbutrin may increase the risk of a seizure. So can sudden discontinuation of anti-anxiety pills like Ativan, Halcion or Xanax.

Other possible interactions may occur in combination with levodopa, phenelzine and tricyclic antidepressants such as amitrityline.

Because of a concern that ginkgo biloba could possibly make a person more vulnerable to seizures, it probably should not be taken together with drugs known to increase the risk of seizures. Antidepressants such as Wellbutrin belong in this category.

Interactions between the herb St. John’s wort and Wellbutrin are possible. Switching between antidepressants and herbal treatment calls for medical guidance (physicians can find a suggested protocol for gradual substitution of St. John’s wort in Hyla Cass’s book, St. John’s Wort: Nature’s Blues Buster).

Animal experiments indicate that compounds that act on dopamine in the brain, such as Wellbutrin, may affect or be affected by the herb chaste tea berry.

Check with your pharmacist and physician to make sure Wellbutrin is safe in combination with any other medicines and herbs you take.

Special Precautions

Even though the seizure risk with Wellbutrin is not as high as originally feared, a 0.4% incidence must not be ignored. The dosing schedule is extremely important in reducing this risk.

The maximum daily dose of 450 mg should not be exceeded. In the case of the sustained release (SR) formulation, the total daily dose should not exceed 400 mg.

Alcohol and certain other drugs (oral decongestants, other antidepressants, theophylline, oral corticosteroids) may potentiate the risk of seizures, so please check with a physician before consuming alcoholic beverages or taking any other medications.

Some drugs, such as Ativan, Halcion or Xanax, should be used cautiously, if at all, with Wellbutrin, because stopping them suddenly may make some people more vulnerable to seizures.

Wellbutrin may cause an exaggerated sun reaction, so people taking this antidepressant should stay out of the sun, wear protective clothing and use a broad spectrum sun block.

Taking the Medicine

Wellbutrin can be somewhat more complicated to take than other medications.

The SR (slow-release) formula is usually given as 150 mg twice a day with at least eight hours between the two doses. If the dose needs to be increased, this must be done gradually with medical supervision.

The SR (slow-release) formulation should not be chewed, crushed or split, as this might alter the absorption of this medicine.

The immediate-release tablets are usually given three times daily. No single dose should exceed 150 mg.

Dosing is usually started at 200 mg a day, given as 100 mg twice a day. This can be gradually increased to a total of 300 mg a day total. The daily dose should not be increased by more than 100 mg in a three-day period.

To minimize insomnia, the last dose of the day should not be taken at bedtime. However, immediate-release tablets should be spaced approximately six hours apart.

Food does not appear to have a significant effect upon  absorption, so it may be taken with or without food.

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About the Author
Joe Graedon is a pharmacologist who has dedicated his career to making drug information understandable to consumers. His best-selling book, The People’s Pharmacy, was published in 1976 and led to a syndicated newspaper column, syndicated public radio show and web site. In 2006, Long Island University awarded him an honorary doctorate as “one of the country's leading drug experts for the consumer.” .
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