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Descripción (Español)
El bupropion o bupropión (anfebutamona) es un fármaco antidepresivo con propiedades psicoestimulantes (poco potentes). El bupropion se introdujo en EE. UU. en 1985. En 1986 fue retirado del mercado debido a una alta incidencia de episodios convulsivos. Finalmente, en 1989 volvió a aprobarse su uso, fijándose una dosis máxima de 450 mg por día.
Actualmente, está indicado para el tratamiento de la depresión (su efectividad más allá de las 8 semanas no ha sido evaluada en ensayos controlados), para la deshabituación tabáquica (6-7 semanas) y como fármaco de segunda línea en el Trastorno por déficit de atención con hiperactividad (ADHD), entre otros usos. Particularmente, es de elección en aquellos pacientes que padecen disfunciones sexuales inducidas por otros antidepresivos, puesto que se vincula con un incremento de la libido. Además, muestra ventajas comparativas respecto de los agentes convencionales en el tratamiento de los episodios depresivos comórbidos a la enfermedad de Parkinson y de la depresión con retardo psicomotor.
Químicamente es una fenetilamina, emparentada estructuralmente tanto con las aminoketonas como con las anfetaminas. Es un derivado de la droga dietilpropion, un anorexígeno anfetamínico. Las acciones desinhibitorias o estimulantes del bupropion probablemente estén relacionadas a su analogía estructural con moléculas psicoestimulantes potentes como la metcatinona y la metanfetamina
La eficacia terapéutica del bupropion se basa en su acción como Inhibidor Selectivo de la Recaptación de Dopamina (DA) y Noradrenalina (NA). Se postula que los efectos clínicos sólo parcialmente se deben a la actividad de la droga, ya que el bupropion es además, una pro-droga. Como producto del metabolismo de la droga madre, se sintetizan en el organismo al menos tres metabolitos activos, uno de los cuales sería el responsable de buena parte de los efectos clínicos. La biotransformación del bupropion en el hígado, da como producto al compuesto hidroxibupropion, que es un inhibidor de recaptación de DA y NA equipotente. La vida media de la droga madre y de los metabolitos activos es de 20 a 37 horas.
La administración crónica del bupropion no produce aumento de peso, lo que resulta útil en el tratamiento de la deshabituación tabáquica. Su acción terapéutica en el tabaquismo podría deberse en particular al incremento que induce en los niveles extracelulares de dopamina, neurotransmisor implicado en los mecanismos de recompensa y gratificación. La nicotina, al igual que el bupropion, también produce uina liberación de dopamina en el núcleo accumbens (vía de placer común de opiáceos, anfetamina y cocaína). Asimismo, el bupropion aumenta también los niveles de noradrenalina en las sinapsis neuronales, lo que amortiguaría los síntomas de abstinencia.
Por su propiedad activante (estimulación del sistema dopaminérgico), puede producir agitación e insomnio. Otras reacciones adversas comunes son: sequedad de boca, cefaleas, temblor, supresión del apetito, nerviosismo, euforia, mialgias, palpitaciones, reducción de peso. En general, el perfil de efectos secundarios es muy diferente al de los antidepresivos convencionales (no posee efectos anticolinérgicos, ni sedativos) y más afín al de los psicoestimulantes.
Poco antes de su lanzamiento comercial, en 1986, se reportaron convulsiones en un pequeño grupo de pacientes bulímicos. Sin embargo, se continuó con las investigaciones clínica y se aprobó su uso en EE.UU. La inducción de convulsiones, es un efecto adverso raro pero grave, y se asocia con incrementos rápidos en las dosis o bien con cantidades superiores a los 450 mg/día. De cualquier manera, son factores de riesgo para la aparición de estos episodios: historia previa de convulsiones, abstinencia reciente de alcohol o benzodiazepinas, tratamiento concomitante con otras drogas (que disminuyan el umbral convulsivo), trastornos orgánicos cerebrales, anormalidades electroencefalográficas y bulimia.
Un metabolito del bupropion, la radafaxina (GW353162), está iniciando la fase III de ensayos clínicos para el tratamiento tanto de la depresión como de la obesidad.
Véase también
— Fluoxetina
— Nicotina
— Sertralina
— Tabaco
Note: Your account will be debited in USD when you
order Wellbutrin SR with Boliviano and Bolivian Peso according to your bank's actual exchange rates.
Note: Actual product
may differ from
the image above
Other brand names of Wellbutrin SR are Zyban, Bupropion, Amfebutamone.
Why do some drugs have different names?
These are trade or brand names registered by the manufacturer. In different countries manufacturers will often use different trade names. The medications have the same active ingredients, but may look different and have a different trade name.
Brand names: Wellbutrin XL, Wellbutrin SR, Wellbutrin
Why is Wellbutrin SR prescribed?
Wellbutrin is prescribed to help relieve major depression. Symptoms include a severely depressed mood (for 2 weeks or more) and loss of interest or pleasure in usual activities accompanied by sleep and appetite disturbances, agitation or lack of energy, feelings of guilt or worthlessness, decreased sex drive, inability to concentrate, and sometimes, suicidal thoughts or behavior.
Wellbutrin is thought to work by altering levels of the brain chemicals norepinephrine and dopamine. It is not chemically related to other antidepressants such as tricyclics (Elavil), MAO inhibitors (Nardil, Parnate), or serotonin re-uptake inhibitors (Paxil and Prozac).
Most important fact about Wellbutrin SR
Wellbutrin is associated with an increased risk of seizures. This risk is greater at higher doses (approximately 4 in 1,000 patients at dosages of 300 to 450 milligrams a day). Certain factors increase the risk of seizure, including:
— A history of head trauma or previous seizure
— Central nervous system tumor
— Severe liver disease such as cirrhosis
— A history of eating disorders, including anorexia and bulimia
— Excessive use of alcohol, or abrupt withdrawal from alcohol or sedatives
— Taking medications that lower the seizure threshold (see «Possible food and drug interactions when taking Wellbutrin SR»)
To minimize the risk of seizures, dose increases should be done gradually, and the total daily dose of Wellbutrin should not exceed 450 milligrams. Additionally, the doctor should be aware of all your medical conditions, and you should not take any other medications (both prescription and over-the-counter) unless the doctor approves.
How should you take Wellbutrin SR?
Take Wellbutrin exactly as prescribed by your doctor. The usual dosing regimen is 3 equal doses spaced evenly throughout the day. Allow at least 6 hours between doses. Your doctor will probably start you at a low dosage and gradually increase it; this helps minimize side effects.
You should take Wellbutrin SR, the sustained-release form, in 2 doses, at least 8 hours apart. Wellbutrin XL extended-release tablets should be taken once a day in the morning. Swallow Wellbutrin SR and Wellbutrin XL tablets whole; do not chew, divide, or crush them.
If Wellbutrin works for you, your doctor will probably have you continue taking it for at least several months.
If you miss a dose...
Take it as soon as you remember. If it is within 4 hours of your next dose, skip the one you missed and go back to your regular schedule. Never take 2 doses at the same time.
Storage instructions...
Store at room temperature. Protect from light and moisture.
What side effects may occur?
Side effects cannot be anticipated. If any develop or change in intensity, inform your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking Wellbutrin.
Side effects of Wellbutrin SR may include:
Agitation, constipation, dizziness, dry mouth, insomnia, nausea, rash, sweating, weight loss
Why should Wellbutrin SR not be prescribed?
Do not take Wellbutrin if you are sensitive to or have ever had an allergic reaction to it.
Since Wellbutrin causes seizures in some people, do not take it if you have any type of seizure disorder or if you are taking another medication containing bupropion, such as Zyban, the used to help quit smoking. If you have a seizure while taking Wellbutrin, stop taking the drug and never take it again.
Do not take Wellbutrin while abruptly giving up alcohol or sedatives, including tranquilizers such as Librium, Valium, and Xanax. Rapid withdrawal increases the risk of seizures.
If you have had any kind of heart trouble or liver or kidney disease, be sure your doctor knows about it before you start taking Wellbutrin SR. It must be used with extreme caution if you have severe cirrhosis of the liver. A reduced dosage may be needed if you have any sort of liver or kidney problem.
You should not take Wellbutrin if you currently have, or formerly had, an eating disorder. For some reason, people with a history of anorexia nervosa or bulimia seem to be more likely to experience Wellbutrin-related seizures. Do not take Wellbutrin if, within the past 14 days, you have taken a monoamine oxidase inhibitor (MAO inhibitor) drug, such as the antidepressants Marplan, Nardil or Parnate. This particular drug combination could cause you to experience a sudden, dangerous rise in blood pressure.
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