Bupropion is a racemic mixture. The pharmacological activity and pharmacokinetics of the individual enantiomers have not been studied. However, it appears likely that only a small proportion of any orally administered dose reaches the systemic circulation intact. Exposure AUC to bupropion was equivalent for both formulations. Bioequivalence was also demonstrated for all three major active metabolites i. The food effect is not considered clinically significant.
The extent of protein binding of the hydroxybupropion metabolite is similar to that for bupropion; whereas, the extent of protein binding of the threohydrobupropion metabolite is about half that seen with bupropion. Bupropion is extensively metabolized in humans. In vitro findings suggest that CYP2B6 is the principal isoenzyme involved in the formation of hydroxybupropion, while cytochrome P enzymes are not involved in the formation of threohydrobupropion.
The potency and toxicity of the metabolites relative to bupropion have not been fully characterized. However, it has been demonstrated in an antidepressant screening test in mice that hydroxybupropion is one-half as potent as bupropion, while threohydrobupropion and erythrohydrobupropion are 5-fold less potent than bupropion.
This may be of clinical importance because the plasma concentrations of the metabolites are as high as or higher than those of bupropion. The times to peak concentrations for the erythrohydrobupropion and threohydrobupropion metabolites are similar to that of the hydroxybupropion metabolite. Only 0. Factors or conditions altering metabolic capacity e. The elimination of the major metabolites of bupropion may be affected by reduced renal or hepatic function because they are moderately polar compounds and are likely to undergo further metabolism or conjugation in the liver prior to urinary excretion.
Renal Impairment: There is limited information on the pharmacokinetics of bupropion in patients with renal impairment. An inter-trial comparison between normal subjects and subjects with end-stage renal failure demonstrated that the parent drug C max and AUC values were comparable in the 2 groups, whereas the hydroxybupropion and threohydrobupropion metabolites had a 2. Bupropion is extensively metabolized in the liver to active metabolites, which are further metabolized and subsequently excreted by the kidneys.
The elimination of the major metabolites of bupropion may be reduced by impaired renal function. Hepatic Impairment: The effect of hepatic impairment on the pharmacokinetics of bupropion was characterized in 2 single-dose trials, one in subjects with alcoholic liver disease and one in subjects with mild-to-severe cirrhosis. In subjects with severe hepatic cirrhosis, significant alterations in the pharmacokinetics of bupropion and its metabolites were seen Table 5. Table 5. T max a. Left Ventricular Dysfunction: During a chronic dosing trial with bupropion in 14 depressed subjects with left ventricular dysfunction history of CHF or an enlarged heart on x-ray , there was no apparent effect on the pharmacokinetics of bupropion or its metabolites, compared with healthy volunteers.
These data suggest there is no prominent effect of age on bupropion concentration; however, another single- and multiple-dose pharmacokinetics trial suggested that the elderly are at increased risk for accumulation of bupropion and its metabolites [see Use in Specific Populations 8. The clinical significance of this finding is unknown. Smokers: The effects of cigarette smoking on the pharmacokinetics of bupropion were studied in 34 healthy male and female volunteers; 17 were chronic cigarette smokers and 17 were nonsmokers.
In addition, in vitro studies suggest that paroxetine, sertraline, norfluoxetine, fluvoxamine, and nelfinavir inhibit the hydroxylation of bupropion. This effect is thought to be due to the inhibition of the CYP2B6-catalyzed bupropion hydroxylation. Cimetidine: The threohydrobupropion metabolite of bupropion does not appear to be produced by cytochrome P enzymes.
The effects of concomitant administration of cimetidine on the pharmacokinetics of bupropion and its active metabolites were studied in 24 healthy young male volunteers. Following oral administration of bupropion mg with and without cimetidine mg, the pharmacokinetics of bupropion and hydroxybupropion were unaffected. Citalopram: Citalopram did not affect the pharmacokinetics of bupropion and its three metabolites. Carbamazepine, Phenobarbital, Phenytoin: While not systematically studied, these drugs may induce the metabolism of bupropion. Animal data indicated that bupropion may be an inducer of drug-metabolizing enzymes in humans.
In one trial, following chronic administration of bupropion mg three times daily to 8 healthy male volunteers for 14 days, there was no evidence of induction of its own metabolism. Nevertheless, there may be potential for clinically important alterations of blood levels of co-administered drugs. The effect was present for at least 7 days after the last dose of bupropion.
Concomitant use of bupropion with other drugs metabolized by CYP2D6 has not been formally studied. Lamotrigine: Multiple oral doses of bupropion had no statistically significant effects on the single-dose pharmacokinetics of lamotrigine in 12 healthy volunteers. Digoxin: Literature data showed that digoxin exposure was decreased when a single oral dose of 0. These doses are approximately 7 and 2 times the MRHD, respectively, on a mg per m 2 basis. The question of whether or not such lesions may be precursors of neoplasms of the liver is currently unresolved. Similar liver lesions were not seen in the mouse study, and no increase in malignant tumors of the liver and other organs was seen in either study.
Table 6. For Trial 1, it refers to the mean score at the endpoint visit; for Trials 2 and 3, it refers to the mean change from baseline to the endpoint visit. Protect from light and moisture. Instruct patients, their families, and their caregivers to read the Medication Guide and assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have.
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The complete text of the Medication Guide is reprinted at the end of this document. Advise families and caregivers of patients to observe for the emergence of such symptoms on a day-to-day basis, since changes may be abrupt. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in the medication. Inform patients that some patients have experienced changes in mood including depression and mania , psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation and suicide when attempting to quit smoking while taking bupropion.
Instruct patients to discontinue bupropion and contact a healthcare professional if they experience such symptoms [see Warnings and Precautions 5. Advise patients to minimize or avoid use of alcohol. Pre-existing glaucoma is almost always open-angle glaucoma because angle-closure glaucoma, when diagnosed, can be treated definitively with iridectomy. Open-angle glaucoma is not a risk factor for angle-closure glaucoma. Patients may wish to be examined to determine whether they are susceptible to angle closure, and have a prophylactic procedure e. In addition, there are a number of generic bupropion HCl products for the immediate-, sustained-, and extended-release formulations.
Advise patients to notify their healthcare provider if they become pregnant or intend to become pregnant during therapy. Do not chew, divide, or crush tablets; they are designed to slowly release drug in the body.
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Instruct patients if they miss a dose, not to take an extra tablet to make up for the missed dose and to take the next tablet at the regular time because of the dose-related risk of seizure. The other brands listed are trademarks owned by or licensed to their respective owners and are not owned by or licensed to the GSK group of companies. The makers of these brands are not affiliated with and do not endorse the GSK group of companies or its products. This section of the Medication Guide is only about the risk of suicidal thoughts and actions with antidepressant medicines.
What is the most important information I should know about antidepressant medicines, depression and other serious mental illnesses, and suicidal thoughts or actions? Call your healthcare provider right away if you or your family member has any of the following symptoms, especially if they are new, worse, or worry you:. What else do I need to know about antidepressant medicines?
This section of the Medication Guide is only about the risk of changes in thinking and behavior, depression and suicidal thoughts or actions with drugs used to quit smoking. When you try to quit smoking, with or without bupropion you may have symptoms that may be due to nicotine withdrawal, including:. Some people have even experienced suicidal thoughts when trying to quit smoking without medication. Sometimes quitting smoking can lead to worsening of mental health problems that you already have, such as depression.
Some people have had serious side effect while taking bupropion to help them quit smoking, including:. New or worse mental health problems, such as changes in behavior or thinking, aggression, hostility, agitation, depression, or suicidal thoughts or actions. Some people had these symptoms when they began taking bupropion, and others developed them after several weeks of treatment, or after stopping bupropion. These symptoms happened more often in people who had a history of mental health problems before taking bupropion than in people without a history of mental health problems.
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It is important for you to follow-up with your healthcare provider until your symptoms go away. You should also tell your healthcare provider about any symptoms you had during other times you tried to quit smoking, with or without bupropion. Tell your healthcare provider if you have ever had depression, suicidal thoughts or actions, or other mental health problems. Tell your healthcare provider about all the medicines you take , including prescription, over-the-counter medicines, vitamins, and herbal supplements.
If you have nausea, take your medicine with food. If you have trouble sleeping, do not take your medicine too close to bedtime. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. It may harm them. If you would like more information, talk with your healthcare provider.
Inactive ingredients: carnauba wax, cysteine hydrochloride, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, and titanium dioxide. The tablets are printed with edible black ink. The other brands listed are trademarks owned or licensed to their respective owners and are not owned by or licensed to the GSK group of companies. Leaving GSK Source. Approval: Observe patients attempting to quit smoking with bupropion for the occurrence of such symptoms and instruct them to discontinue bupropion and contact a healthcare provider if they experience such adverse events.
Can minimize risk by gradually increasing the dose and limiting daily dose to mg. Discontinue if seizure occurs. Monitor blood pressure before initiating treatment and periodically during treatment. Consider dose reduction when using with bupropion. Monitor digoxin levels. Table 1. Table 2. Table 3. Table 4. Body General Arthralgia, myalgia, and fever with rash and other symptoms suggestive of delayed hypersensitivity. Cardiovascular Complete atrioventricular block, extrasystoles, hypotension, hypertension in some cases severe , phlebitis, and pulmonary embolism.
Digestive Colitis, esophagitis, gastrointestinal hemorrhage, gum hemorrhage, hepatitis, intestinal perforation, pancreatitis, and stomach ulcer. Endocrine Hyperglycemia, hypoglycemia, hyponatremia, and syndrome of inappropriate antidiuretic hormone secretion. Hemic and Lymphatic Anemia, leukocytosis, leukopenia, lymphadenopathy, pancytopenia, and thrombocytopenia. Metabolic and Nutritional Glycosuria. Nervous System Abnormal electroencephalogram EEG , aggression, akinesia, aphasia, coma, completed suicide, delirium, delusions, dysarthria, euphoria, extrapyramidal syndrome dyskinesia, dystonia, hypokinesia, parkinsonism , hallucinations, increased libido, manic reaction, neuralgia, neuropathy, paranoid ideation, restlessness, suicide attempt, and unmasking tardive dyskinesia.
Respiratory Pneumonia. Skin Alopecia, angioedema, exfoliative dermatitis, hirsutism, and Stevens-Johnson syndrome. Special Senses Deafness, increased intraocular pressure, and mydriasis. Urogenital Abnormal ejaculation, cystitis, dyspareunia, dysuria, gynecomastia, menopause, painful erection, salpingitis, urinary incontinence, urinary retention, and vaginitis.
Inhibitors of CYP2B6 Ticlopidine and Clopidogrel: Concomitant treatment with these drugs can increase bupropion exposure but decrease hydroxybupropion exposure. Clinical Considerations Consider the risks of untreated depression when discontinuing or changing treatment with antidepressant medications during pregnancy and postpartum. Human Data Data from the international bupropion Pregnancy Registry first trimester exposures and a retrospective cohort study using the United Healthcare database 1, first trimester exposures did not show an increased risk for malformations overall.
Animal Data In studies conducted in rats and rabbits, bupropion was administered orally during the period of organogenesis at doses of up to and mg per kg per day, respectively approximately 11 and 7 times the MRHD, respectively, on a mg per m 2 basis.
Animals Studies in rodents and primates demonstrated that bupropion exhibits some pharmacologic actions common to psychostimulants. Metabolism Bupropion is extensively metabolized in humans. Population Subgroups Factors or conditions altering metabolic capacity e. Pregnancy Advise patients to notify their healthcare provider if they become pregnant or intend to become pregnant during therapy. Antidepressant medicines may increase the risk of suicidal thoughts or actions in some children, teenagers, or young adults within the first few months of treatment.
Depression or other serious mental illnesses are the most important causes of suicidal thoughts and actions. Some people may have a particularly high risk of having suicidal thoughts or actions. These include people who have or have a family history of bipolar illness also called manic-depressive illness or suicidal thoughts or actions. How can I watch for and try to prevent suicidal thoughts and actions in myself or a family member? Pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings.
This is very important when an antidepressant medicine is started or when the dose is changed. Call your healthcare provider right away to report new or sudden changes in mood, behavior, thoughts, or feelings. Keep all follow-up visits with your healthcare provider as scheduled.
Call the healthcare provider between visits as needed, especially if you have concerns about symptoms. Stopping an antidepressant medicine suddenly can cause other symptoms. It is important to discuss all the risks of treating depression and also the risks of not treating it. Patients and their families or other caregivers should discuss all treatment choices with the healthcare provider, not just the use of antidepressants.
Talk to the healthcare provider about the side effects of the medicine prescribed for you or your family member. Know all of the medicines that you or your family member takes. Keep a list of all medicines to show the healthcare provider. Do not start new medicines without first checking with your healthcare provider. Quitting Smoking, Quit-Smoking Medications, Changes in Thinking and Behavior, Depression, and Suicidal Thoughts or Actions This section of the Medication Guide is only about the risk of changes in thinking and behavior, depression and suicidal thoughts or actions with drugs used to quit smoking.
Some people have had serious side effect while taking bupropion to help them quit smoking, including: New or worse mental health problems, such as changes in behavior or thinking, aggression, hostility, agitation, depression, or suicidal thoughts or actions. If this happens to you, call your healthcare provider. You may want to undergo an eye examination to see if you are at risk and receive preventative treatment if you are. These could be signs of a serious allergic reaction.
Ask your healthcare provider or pharmacist if you are not sure if you take an MAOI, including the antibiotic linezolid. If you do, the medicine will be released into your body too quickly. If this happens you may be more likely to get side effects including seizures. Tell your healthcare provider if you cannot swallow tablets. This is normal. Wait and take your next dose at the regular time. This is very important. If you usually drink a lot of alcohol, talk with your healthcare provider before suddenly stopping.
If you suddenly stop drinking alcohol, you may increase your chance of having seizures. Tell your healthcare provider right away about any side effects that bother you. You may also report side effects to GlaxoSmithKline at Active ingredient: bupropion hydrochloride. Age Range. Increases Compared with Placebo. Decreases Compared with Placebo. Adverse Reaction. Abdominal pain. Chest pain. Hot flashes. Dry mouth. Memory decreased. Fanno la quota massima, circa , m sopra il decollo e poi via verso le vette feltrine e verso la prima boa.
Nessuno riesce a completare la task anzi nessuno riesce ad aggirare la terza boa di Cesio Maggiore. Stessa sorte aspetta anche i fun. Ci si ritrova tutti in atterraggio per la consegna dei gps e per le classifiche dopo essere stati recuperati tutti li attorno. Stesso dicasi per i fun. Quindi con la gara non valida le classifiche che assegnano il titolo Triveneto sono quelle congelate alla task di Bassano.
Siete sempre un esempio. Ma torniamo a bomba! La classifica club vede:. Questo movimento insieme alla nascita della classifica FUN, a livello regionale, ha permesso ai neofiti di boe, start, e lunghi chilometri di maturare una adeguata esperienza con task alla portata di tutti, impegnative, selettive ma sempre in totale sicurezza e divertenti. Migliorarsi divertendosi!
Non dimentichiamo poi che in diverse tappe i club saliti sul podio sono proprio quelli che stanno puntando sui FUN! Hanno subito trovato la giusta sintonia e hanno lavorato per tutta la stagione in modo lodevole trovandosi a dover anche risolvere delle piccole controversie nate ad inizio stagione per una errata interpretazione, da parte di alcuni piloti, del regolamento gare regionale FIVL. Aggiungo un doveroso ringraziamento a tutti coloro che hanno appoggiato, promosso e supportato il nostro sport ed in particolare la riuscita del Campionato Triveneto parapendio Nomi che hanno creduto fermamente nella passione per il volo libero.
Ora concludo questo mio quinto ed ultimo articoletto per il Triveneto.