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Wellbutrin Clinical Trials
Inhibition of Human CYP2B6-Catalyzed Bupropion
Hydroxylation by Ginkgo biloba Extract: Effect of Terpene Trilactones and
Flavonols.
Lau AJ, Chang TK.
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print]
PMID: 19487249 [PubMed - as supplied
by publisher]
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Ascorbic acid administration produces an
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Binfaré RW, Rosa AO, Lobato KR, Santos AR,
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LT, Young AH, Alda M, Milev R, Vieta E, Calabrese JR, Berk M, Ha K, Kapczinski
F.
Bipolar Disord. 2009 May;11(3):225-55.
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[Combining Antidepressants: a Useful Strategy for
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Schmauß M, Messer T.
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print]
PMID: 19405782 [PubMed - as supplied
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[No authors listed]
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Efstathiou SP, Skeva II, Dimas C, Panagiotou A,
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MEDLINE]
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Llosa T.
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CYP2B6.
Lin HL, Zhang H, Hollenberg PF.
J Pharmacol Exp Ther. 2009 Apr;329(1):26-37. Epub
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PMID: 19168709 [PubMed - indexed for
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Eur Arch Psychiatry Clin Neurosci. 2009
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A, Modell J.
J Psychopharmacol. 2009 Jan 22. [Epub ahead of
print]
PMID: 19164492 [PubMed - as supplied
by publisher]
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MEDLINE]
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Prescribing during pregnancy. Prenatal drug exposure
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[No authors listed]
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MEDLINE]
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A survey of tobacco dependence treatment services in
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Drug Alcohol Depend. 2009 Jan 7. [Epub ahead of
print]
PMID: 19135319 [PubMed - as supplied
by publisher]
Related Articles
[Specific program for smoking cessation: thus your
patients become nonsmokers]
Hering T.
MMW Fortschr Med. 2008 Nov 13;150(46):42-3. German.
No abstract available.
PMID: 19133359 [PubMed - indexed for
MEDLINE]
Related Articles
A 51-year-old woman with bipolar disorder who wants
to quit smoking.
Schroeder SA.
JAMA. 2009 Feb 4;301(5):522-31. Epub 2009 Jan 6.
PMID: 19126801 [PubMed - indexed for
MEDLINE]
Related Articles
Pharmacotherapy for smoking cessation.
Carrozzi L, Pistelli F, Viegi G.
Ther Adv Respir Dis. 2008 Oct;2(5):301-17. Review.
PMID: 19124379 [PubMed - indexed for
MEDLINE]
Related Articles
Smoking cessation treatment in a real-life setting:
the Greek experience.
Rovina N, Nikoloutsou I, Dima E, Michailidou M,
Roussos C, Gratziou C.
Ther Adv Respir Dis. 2007 Dec;1(2):93-104.
PMID: 19124351 [PubMed - indexed for
MEDLINE]
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Tardive dyskinesia associated with long-term
administration of escitalopram and itopride in major depressive disorder.
Park YM, Lee HJ, Kang SG, Choo CS, Cho JH.
Prog Neuropsychopharmacol Biol Psychiatry. 2009 Mar
17;33(2):380-1. Epub 2008 Dec 13. No abstract available.
PMID: 19121360 [PubMed - indexed for
MEDLINE]
Related Articles
Helping smokers quit: understanding the barriers to
utilization of smoking cessation services.
Gollust SE, Schroeder SA, Warner KE.
Milbank Q. 2008 Dec;86(4):601-27.
PMID: 19120982 [PubMed - indexed for
MEDLINE]
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Use of mRNA expression to detect the induction of
drug metabolising enzymes in rat and human hepatocytes.
Richert L, Tuschl G, Abadie C, Blanchard N,
Pekthong D, Mantion G, Weber JC, Mueller SO.
Toxicol Appl Pharmacol. 2009 Feb 15;235(1):86-96.
Epub 2008 Dec 10.
PMID: 19118567 [PubMed - indexed for
MEDLINE]
Related Articles
Bupropion-associated QRS prolongation unresponsive
to sodium bicarbonate therapy.
Wills BK, Zell-Kanter M, Aks SE.
Am J Ther. 2009 Mar-Apr;16(2):193-6.
PMID: 19114875 [PubMed - indexed for
MEDLINE]
Related Articles
A review of co-morbid depression in pediatric ADHD:
etiology, phenomenology, and treatment.
Daviss WB.
J Child Adolesc Psychopharmacol. 2008
Dec;18(6):565-71. Review.
PMID: 19108661 [PubMed - indexed for
MEDLINE]
Related Articles
Effect of increasing intraperitoneal infusion rates
on bupropion hydrochloride-induced seizures in mice.
Silverstone PH, Williams R, McMahon L, Fleming R,
Fogarty S.
Ann Gen Psychiatry. 2008 Dec 23;7:27.
PMID: 19105845 [PubMed - in process]
Related Articles
Free article in PMC
Review: varenicline, bupropion, and nicotine
replacement therapies are effective for smoking cessation at 6 or 12 months.
Lamarche K.
Evid Based Nurs. 2009 Jan;12(1):10. No abstract
available.
PMID: 19103828 [PubMed]
Related Articles
Behavioural and pharmacological mechanisms of
bupropion's anti-smoking effects: recent preclinical and clinical insights.
Paterson NE.
Eur J Pharmacol. 2009 Jan 28;603(1-3):1-11. Epub
2008 Dec 16. Review.
PMID: 19101536 [PubMed - indexed for
MEDLINE]
Related Articles
Nicotine exposure during adolescence induces a
depression-like state in adulthood.
Iñiguez SD, Warren BL, Parise EM, Alcantara LF,
Schuh B, Maffeo ML, Manojlovic Z, Bolaños-Guzmán CA.
Neuropsychopharmacology. 2009 May;34(6):1609-24.
Epub 2008 Dec 17.
PMID: 19092782 [PubMed - in process]
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Pavlovian drug discrimination with bupropion as a
feature positive occasion setter: substitution by methamphetamine and nicotine,
but not cocaine.
Wilkinson JL, Li C, Bevins RA.
Addict Biol. 2009 Apr;14(2):165-73. Epub 2008 Dec
12.
PMID: 19076926 [PubMed - in process]
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Induction of cytochrome P450 2B6 activity by the
herbal medicine baicalin as measured by bupropion hydroxylation.
Fan L, Wang JC, Jiang F, Tan ZR, Chen Y, Li Q,
Zhang W, Wang G, Lei HP, Hu DL, Wang D, Zhou HH.
Eur J Clin Pharmacol. 2009 Apr;65(4):403-9. Epub
2008 Dec 9.
PMID: 19066872 [PubMed - indexed for
MEDLINE]
Related Articles
Tobacco smoking cessation management: integrating
varenicline in current practice.
Galanti LM.
Vasc Health Risk Manag. 2008;4(4):837-45. Review.
PMID: 19066000 [PubMed - indexed for
MEDLINE]
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Free article in PMC
Evidence for the involvement of the monoaminergic
system in the antidepressant-like effect of magnesium.
Cardoso CC, Lobato KR, Binfaré RW, Ferreira PK,
Rosa AO, Santos AR, Rodrigues AL.
Prog Neuropsychopharmacol Biol Psychiatry. 2009 Mar
17;33(2):235-42. Epub 2008 Nov 27.
PMID: 19059299 [PubMed - indexed for
MEDLINE]
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Mechanism-based inhibition of human cytochrome P450
2B6 by ticlopidine, clopidogrel, and the thiolactone metabolite of prasugrel.
Nishiya Y, Hagihara K, Ito T, Tajima M, Miura S,
Kurihara A, Farid NA, Ikeda T.
Drug Metab Dispos. 2009 Mar;37(3):589-93. Epub 2008
Dec 1.
PMID: 19047469 [PubMed - in process]
Related Articles
Wellbutrin - Alert from the F.D.A.
FDA ALERT [07/2005]: Suicidal Thoughts or Actions in
Children and Adults
Patients with depression or other mental illnesses often
think about or attempt suicide. Closely watch anyone taking antidepressants,
especially early in treatment or when the dose is changed. Patients who become
irritable or anxious, or have new or increased thoughts of suicide or other
changes in mood or behavior (or their care givers) should contact their
healthcare professional right away.
Children
Taking antidepressants may increase suicidal thoughts and actions in about 1
out of 50 people 18 years or younger. FDA has approved Zoloft for use in
children only if they have obsessive-compulsive disorder.
Adults
Several recent scientific publications report the possibility of an increased
risk for suicidal behavior in adults who are being treated with antidepressant
medications. Even before these reports became available, FDA began a complete
review of all available data to determine whether there is an increased risk of
suicidal thinking or behavior in adults being treated with antidepressant
medications. It is expected that this review will take a year or longer to
complete. In the meantime, FDA is highlighting that adults being treated with
antidepressant medication, particularly those being treated for depression,
should be watched closely for worsening of depression and for increased suicidal
thinking or behavior.
This information reflects FDA’s preliminary
analysis of data concerning this drug. FDA is considering, but has not reached a
final conclusion about, this information. FDA intends to update this sheet when
additional information or analyses become available.
Wellbutrin
withdrawal Body
Wellbutrin
withdrawal
Dry Mouth
- The
usual amount to moisture in the mouth is noticeably less.
Wellbutrin
withdrawal
Sweating
Increased -
A large
quantity of perspiration that is medically caused.
Wellbutrin
withdrawal
Cardiovascular (Involving the heart and the blood
vessels)
Wellbutrin
withdrawal
Palpitation
- Unusual and not normal heartbeat,
that is sometimes irregular, but rapid and forceful thumping or fluttering. It
can be brought on by shock, excitement, exertion, or medical stimulants. A
person is normally unaware of his/her heartbeat.
Wellbutrin withdrawal
Hypertension
- is high blood pressure, which is a
symptom of disease in the blood vessels leading away from the heart.
Hypertension is known as the “silent killer”. The symptoms are usually not
obvious, however it can lead to damage to the heart, brain, kidneys and eye, and
even to stroke and kidney failure. Treatment includes dietary and lifestyle
changes.
Wellbutrin withdrawal
Bradycardia
-
The heart rate is slowed from 72 beats per minute,
which is normal, to below 60 beats per minute in an adult.
Wellbutrin
withdrawal
Tachycardia
- The heart rate is speeded up to
above 100 beats per minute in an adult. Normal adult heart rate is 72 beats per
minute.
Wellbutrin
withdrawal
ECG Abnormal
-
A test
called an electrocardiogram (ECG) that records the activity of the heart. It
measures heartbeats as will as the position and size of the heart’s four
chambers. It also measures if there is damage to the heart and the effects of
drugs or mechanical devices like a pacemaker on the heart. When the test is
abnormal this means that one or more of the following are present: heart
disease, defects, beating too fast or too slow, disease of the blood vessels
leading from the heart or of the heart valves, and/or a past or about to occur
heart attack.
Wellbutrin
withdrawal
Flushing
- The skin all over the body turns red.
Wellbutrin withdrawal
Varicose Vein - Unusually swollen veins
near the surface of the skin that sometimes appear twisted and knotted, but
always enlarged. They are called hemorrhoids when they appear around the
rectum. The cause is attributed to hereditary weakness in the veins aggravated
by obesity, pregnancy, pressure from standing, aging, etc. Severe cases may
develop swelling in the legs, ankles and feet, eczema and/or ulcers in the
affected areas.
Wellbutrin
withdrawal
Gastrointestinal
(Involving
the stomach and the intestines)
Wellbutrin withdrawal
Abdominal Cramp/Pain
-
Sudden, severe, uncontrollable and painful shortening and
thickening of the muscles in the belly. The belly includes the stomach as well
as the intestines, liver, kidneys, pancreas, spleen, gall bladder, and urinary
bladder.
Wellbutrin withdrawal
Belching
- Noisy release of gas from the stomach through the mouth; a burp.
Wellbutrin
withdrawal
Bloating
- Swelling of the belly caused by excessive intestinal gas.
Wellbutrin withdrawal
Constipation -
Difficulty in having a bowel movement where the material in the bowels is
hard due to a lack of exercise, fluid intake, and roughage in the diet, or due
to certain drugs.
Wellbutrin withdrawal
Diarrhea - Unusually frequent and excessive, runny bowel movements that may
result in severe dehydration and shock.
Wellbutrin
withdrawal
Dyspepsia - Indigestion. This is the discomfort you experience after eating. It
can be heartburn, gas, nausea, a bellyache or bloating.
Wellbutrin withdrawal
Flatulence
- More gas than normal in the digestive organs.
Wellbutrin withdrawal
Gagging
- Involuntary choking and/or involuntary throwing up.
Wellbutrin withdrawal
Gastritis
- A severe irritation of the mucus lining of the stomach either short in
duration or lasting for a long period of time.
Wellbutrin withdrawal
Gastroenteritis
-
A condition where the membranes
of the stomach and intestines are irritated.
Wellbutrin
withdrawal
Gastroesophageal
Reflux - A
continuous state where stomach juices flow back into the throat causing acid
indigestion and heartburn and possibly injury to the throat.
Wellbutrin
withdrawal
Heartburn
- A burning pain in the area of the breastbone caused by stomach juices flowing
back up into the throat.
Wellbutrin withdrawal
Hemorrhoids - Small rounded
purplish swollen veins that either bleed, itch or are painful and appear around
the anus.
Wellbutrin withdrawal
Increased Stool frequency
-
Diarrhea.
Wellbutrin
withdrawal
Indigestion
- Unable to properly consume and absorb food in the digestive tract causing
constipation, nausea, stomach ache, gas, swollen belly, pain and general
discomfort or sickness.
Wellbutrin withdrawal
Nausea - Stomach irritation with a queasy sensation similar to
motion sickness and a feeling that one is going to vomit.
Wellbutrin
withdrawal
Polyposis Gastric
- Tumors that grow on stems in the lining of the stomach, which usually become
cancerous.
Wellbutrin withdrawal
Swallowing Difficulty
- A feeling that food is stuck in the throat or upper chest area and won’t go
down, making it difficult to swallow.
Wellbutrin withdrawal
Toothache
- Pain in a tooth above and below the gum line.
Wellbutrin withdrawal
Vomiting
- Involuntarily throwing up the contents of the stomach and usually getting a
nauseated, sick feeling just prior to doing so.
Wellbutrin
withdrawal
General
Wellbutrin withdrawal
Allergy -
The extreme
sensitivity of body tissues triggered by substances in the air, drugs, or foods
causing a reaction like sneezing, itching, asthma, hay fever, skin rashes,
nausea and/or vomiting.
Wellbutrin withdrawal
Anaphylaxis
- A violent, sudden, and severe drop
in blood pressure caused by a re-exposure to a foreign protein or a second
dosage of a drug that may be fatal unless emergency treatment is given right
away.
Wellbutrin withdrawal
Asthenia
-
A physically
weak condition.
Wellbutrin
withdrawal
Chest Pains
-
Severe discomfort in the chest caused by not enough oxygen going to the heart
because of narrowing of the blood vessels or spasms.
Wellbutrin
withdrawal
Chills
-
Appearing
pale while cold and shivering; sometimes with a fever.
Wellbutrin withdrawal
Edema of
Extremities
-
Abnormal
swelling of the body’s tissue caused by the collection of fluid.
Wellbutrin withdrawal
Fall
- To suddenly lose your normal
standing upright position as if you were shot.
Wellbutrin
withdrawal
Fatigue
- Loss of normal strength so as to
not be able to do the usual physical and mental activities.
Wellbutrin
withdrawal
Fever
- Abnormally high body temperature,
the normal being 98 degrees Fahrenheit or 37 degrees Centigrade in humans, which
is a symptom of disease or disorder in the body. The body is affected by
feeling hot, chilled, sweaty, weak and exhausted. If the fever goes too high,
death can result.
Wellbutrin
withdrawal
Hot Flashes
-
Brief,
abnormal enlargement of the blood vessels that causes a sudden heat sensation
over the entire body. Women in menopause will sometimes experience this.
Wellbutrin
withdrawal
Influenza-like
Symptoms -
Demonstrating irritation of the respiratory tract (organs of breathing) such as
a cold, sudden fever, aches and pains, as well as feeling weak and seeking bed
rest, which is similar to having the flu.
Wellbutrin
withdrawal
Leg Pain
- A
hurtful sensation in the legs that is caused by excessive stimulation of the
nerve endings in the legs and results in extreme discomfort.
Wellbutrin withdrawal
Malaise -
The somewhat
unclear feeling of discomfort you get when you start to feel sick.
Wellbutrin
withdrawal
Pain in Limb
-
Sudden, sharp and uncontrolled leg discomfort.
Wellbutrin
withdrawal
Syncope
-
A short
period of light headedness or unconsciousness (black-out) also know as fainting
caused by lack of oxygen to the brain because of an interruption in blood
flowing to the brain.
Wellbutrin withdrawal
Tightness of
Chest -
Mild or sharp discomfort, tightness
or pressure in the chest area (anywhere between the throat and belly). The
causes can be mild or seriously life-threatening because they include the heart,
lungs and surrounding muscles.
Wellbutrin
withdrawal
Hemic and Lymphatic Disorders
(Involving
the blood and the clear fluids in the tissues that contain white blood cells)
Wellbutrin withdrawal
Bruise
- Damage to the skin resulting in a
purple-green-yellow skin coloration that’s caused by breaking the blood vessels
in the area without breaking the surface of the skin.
Wellbutrin
withdrawal
Anemia
-
A condition
where the blood is no longer carrying enough oxygen, so the person looks pale
and easily gets dizzy, weak and tired. More severely, a person can end up with
an abnormal heart, as well as breathing and digestive difficulties. The causes
of anemia are not enough protein in the red blood cells, or missing and
chemically destroyed red blood cells, as well as diseased or destroyed bone
marrow.
Wellbutrin withdrawal
Nosebleed
- Blood lost from the part of the
face that has the organs of smell and is where the body takes in oxygen.
Wellbutrin
withdrawal
Hematoma
- Broken blood vessels that cause a
swelling in an area on the body.
Wellbutrin
withdrawal
Lymphadenopathy
Cervical
-
The lymph
nodes in the neck, which are part of the body’s immune system get swollen and
enlarge by reacting to the presence of a drug. The swelling is the result of
the white blood cells multiplying in order to fight the invasion of the drug.
Wellbutrin
withdrawal
Metabolic and Nutritional Disorders
(Energy
and health)
Wellbutrin
withdrawal
Arthralgia
-
Sudden sharp
nerve pain in one or more joints.
Wellbutrin
withdrawal
Arthropathy
- Having joint disease or abnormal
joints.
Wellbutrin
withdrawal
Arthritis
-
Painfully inflamed and swollen joints. The reddened
and swollen condition is brought on by a serious injury or shock to the body
either from physical or emotional causes.
Wellbutrin
withdrawal
Back Discomfort
- Severe physical distress in the area from the neck to the pelvis along the
backbone.
Wellbutrin withdrawal
Bilirubin Increased
- Bilirubin is a waste product of the breakdown
of old blood cells. Bilirubin is sent to the liver to be made water-soluble so
it can be eliminated from the body through emptying the bladder. A drug can
interfere with or damage this normal liver function creating liver disease.
Wellbutrin withdrawal
Decreased Weight
- Uncontrolled and measured loss of heaviness or weight.
Wellbutrin
withdrawal
Gout
- A severe arthritis condition that is caused by the dumping of a waste product
called uric acid in the tissues and joints. It can become worse and cause the
body to develop a deformity after going through stages of pain, inflammation,
severe tenderness, and stiffness.
Wellbutrin withdrawal
Hepatic Enzymes Increased - An increase in the amount of paired liver proteins that
regulate liver processes causing a condition where the liver functions
abnormally.
Wellbutrin withdrawal
Hypercholesterolemia
- Too much cholesterol in the blood cells.
Wellbutrin
withdrawal
Hyperglycemia
- An unhealthy amount of sugar in the blood.
Wellbutrin withdrawal
Increased Weight - A concentration and storage of fat in the body
accumulating over a period of time caused by unhealthy eating patterns, that can
predispose the body to many disorders and diseases.
Wellbutrin withdrawal
Jaw Pain - The pain due to irritation and swelling of the nerves associated with
the mouth area where it opens and closes just in front of the ear. Some of the
symptoms are pain when chewing, head aches, losing your balance, stuffy ears or
ringing in the ears, and teeth grinding.
Wellbutrin withdrawal
Jaw Stiffness
- The result of squeezing and grinding the teeth while asleep that can cause
your teeth to deteriorate as well as the muscles and joints of the jaw.
Wellbutrin
withdrawal
Joint Stiffness
- A loss of free motion and easy flexibility where any
two bones come together.
Wellbutrin withdrawal
Muscle Cramp - When muscles contract uncontrollably without warning and do not
relax. The muscles of any of the body’s organs can cramp.
Wellbutrin
withdrawal
Muscle Stiffness
- Tightening of muscles making it difficult to bend.
Wellbutrin
withdrawal
Muscle Weakness
- Loss of physical strength.
Wellbutrin
withdrawal
Myalgia - A general widespread pain and tenderness of the muscles.
Wellbutrin
withdrawal Thirst
- A strong,
unnatural craving for moisture/water in the mouth and throat.
Wellbutrin
withdrawal
Nervous System (Sensory channels)
Wellbutrin withdrawal
Carpal
Tunnel Syndrome - A
pinched nerve in the wrist that causes pain, tingling, and numbing.
Wellbutrin withdrawal
Coordination Abnormal - A lack of normal, harmonious interaction of the parts of
the body when it is in motion.
Wellbutrin withdrawal
Dizziness - Losing one’s balance while feeling unsteady and lightheaded which may
lead to fainting.
Wellbutrin
withdrawal
Disequilibrium
- Lack of mental and emotional balance.
Wellbutrin withdrawal
Faintness - A temporary condition where one is likely to go
unconscious and fall.
Wellbutrin withdrawal
Headache - A sharp or dull persistent pain in the head
Wellbutrin
withdrawal
Hyperreflexia - A not normal and involuntary increased response in the
tissues connecting the bones to the muscles.
Wellbutrin
withdrawal
Light-headed
Feeling –
Uncontrolled and usually brief loss of consciousness caused by lack of oxygen to
the brain.
Wellbutrin
withdrawal
Migraine
- Reoccurring severe head pain usually with nausea, vomiting, dizziness, flashes
or spots before the eyes, and ringing in the ears
Wellbutrin withdrawal
Muscle Contractions Involuntary
- Spontaneous and uncontrollable tightening reaction of the muscles caused by
electrical impulses from the nervous system.
Wellbutrin
withdrawal
Muscular Tone Increased - Uncontrolled and exaggeration muscle tension. Muscles are
normally partially tensed and this is what gives us muscle tone.
Wellbutrin
withdrawal
Paresthesia - Burning, prickly, itchy, or tingling skin with no obvious or
understood physical cause.
Wellbutrin withdrawal
Restless Legs
- A need to move the legs without any apparent reason. Sometimes there is pain,
twitching, jerking, cramping, burning, or a creepy-crawly sensation associated
with the movements. It worsens when a person is inactive and can interrupt
one’s sleep so one feels the need to move to gain some relief.
Wellbutrin
withdrawal
Shaking
- Uncontrolled quivering and trembling as if one is cold and chilled.
Wellbutrin
withdrawal
Sluggishness
- Lack of alertness and energy, as well as being slow to respond or perform in
life.
Wellbutrin withdrawal
Tics - A contraction of a muscle causing a repeated movement not
under the control of the person usually on the face or limbs.
Wellbutrin
withdrawal
Tremor
- A nervous and involuntary vibrating or quivering of the body.
Wellbutrin withdrawal
Twitching - Sharp, jerky and spastic motion sometimes with a
sharp sudden pain.
Wellbutrin
withdrawal
Vertigo
- A sensation of dizziness with disorientation and confusion.
Wellbutrin
withdrawal Psychiatric Disorders (Mental and emotional)
Wellbutrin withdrawal
Aggravated Nervousness
- A progressively worsening, irritated and troubled state of mind.
Wellbutrin
withdrawal
Agitation
- Suddenly violent and forceful, emotionally disturbed state of mind.
Wellbutrin withdrawal
Amnesia - Long term or short term, partial or full memory loss created by
emotional or physical shock, severe illness, or a blow to the head where the
person was caused pain and became unconsciousness.
Wellbutrin
withdrawal
Anxiety Attack
- Sudden and intense feelings of fear, terror, and dread physically creating
shortness of breath, sweating, trembling and heart palpitations.
Wellbutrin withdrawal
Apathy
- Complete lack of concern or interest for things that ordinarily would be
regarded as important or would normally cause concern.
Wellbutrin
withdrawal
Appetite
Decreased - Having a
lack of appetite despite the ordinary caloric demands of living with a resulting
unintentional loss of weight.
Wellbutrin
withdrawal
Appetite
Increased - An
unusual hunger causing one to overeat.
Wellbutrin
withdrawal
Auditory
Hallucination -
Hearing things without the voices or noises being present.
Wellbutrin
withdrawal
Bruxism -
Grinding and clenching of teeth while sleeping.
Wellbutrin withdrawal
Carbohydrate
Craving - A drive
and craving to eat foods rich in sugar and starches (sweets, snacks and junk
foods) that intensifies as the diet becomes more and more unbalanced due to the
unbalancing of the proper nutritional requirements of the body.
Wellbutrin withdrawal
Concentration Impaired
- Unable to easily focus your attention for long periods of time.
Wellbutrin
withdrawal
Confusion
- Not able to think clearly and understand in order to make a logical decision.
Wellbutrin
withdrawal
Crying Abnormal
- Unusual and not normal fits of weeping for short or long periods of time for
no apparent reason.
Wellbutrin withdrawal
Depersonalization
- A condition where one has lost a normal sense of personal identity.
Wellbutrin
withdrawal
Depression
- A hopeless feeling of failure, loss and sadness that can deteriorate into
thoughts of death.
Wellbutrin
withdrawal
Disorientation
- A loss of sense of direction, place, time or surroundings as well as mental
confusion on personal identity.
Wellbutrin
withdrawal
Dreaming Abnormal
- Dreaming that leaves a very clear, detailed picture and impression when awake
that can last for a long period of time and sometimes be unpleasant.
Wellbutrin
withdrawal
Emotional
Lability
- Suddenly breaking out
in laughter or crying or doing both without being able to control the outburst
of emotion. These episodes are unstable as they are caused by things that
normally would not have this effect on an individual.
Wellbutrin withdrawal
Excitability - Uncontrollably responding to stimuli.
Wellbutrin withdrawal
Feeling Unreal - The awareness that one has an undesirable emotion like
fear but can’t seem to shake off the irrational feeling. For example, feeling
like one is going crazy but rationally knowing that it is not true. The quality
of this side effect resembles being in a bad dream and not being able to wake
up.
Wellbutrin
withdrawal
Forgetfulness
- Unable to remember what one ordinarily would remember.
Wellbutrin
withdrawal
Insomnia
- Sleeplessness caused by physical stress, mental stress or stimulants such as
coffee or medications; it is a condition of being abnormally awake when one
would ordinarily be able to fall and remain asleep.
Wellbutrin
withdrawal
Irritability
- Abnormally annoyed in response to a stimulus.
Wellbutrin withdrawal
Jitteriness - Nervous fidgeting without an apparent cause.
Wellbutrin
withdrawal
Lethargy
- Mental and physical sluggishness and apathy that can deteriorate into an
unconscious state resembling deep sleep. A numbed state of mind.
Wellbutrin
withdrawal
Libido Decreased
- An abnormal loss of sexual energy or desire.
Wellbutrin withdrawal
Panic Reaction
- A sudden, overpowering, chaotic and confused mental state of terror resulting
in being doubt ridden often accompanied with hyperventilation, and extreme
anxiety.
Wellbutrin
withdrawal
Restlessness
Aggravated - A
constantly worsening troubled state of mind characterized by the person being
increasingly nervous, unable to relax, and easily angered.
Wellbutrin
withdrawal
Somnolence - Feeling sleepy all the time or having a condition of
semi-consciousness.
Wellbutrin
withdrawal
Suicide Attempt
- An unsuccessful deliberate attack on one’s own life with the intention of
ending it.
Wellbutrin
withdrawal
Suicidal Tendency
- Most likely will attempt to kill oneself.
Wellbutrin withdrawal
Tremulousness
Nervous - Very
jumpy, shaky, and uneasy while feeling fearful and timid. The condition is
characterized by thoughts of dreading the future, involuntary quivering,
trembling, and feeling distressed and suddenly upset.
Wellbutrin withdrawal
Yawning - involuntary opening of the mouth with deep inhalation of
air.
Wellbutrin
withdrawal
Reproductive Disorder Female
Wellbutrin
withdrawal
Breast Neoplasm
-
A tumor or cancer, of either of the two milk-secreting
organs on the chest of a woman.
Wellbutrin
withdrawal
Menorrhagia
- Abnormally heavy menstrual period or a
menstrual flow that has continued for an unusually long period of time.
Wellbutrin
withdrawal
Menstrual Cramps
- Painful, involuntary uterus contractions that women experience around the time
of their menstrual period, sometimes causing pain in the lower back and thighs.
Wellbutrin
withdrawal
Menstrual
Disorder - A disturbance or derangement in the normal function of a woman’s
menstrual period.
Wellbutrin
withdrawal
Pelvic
Inflammation - The reaction of the body to infectious, allergic, or chemical
irritation, which in turn causes tissue irritation, injury, or bacterial
infection characterized by pain, redness, swelling, and sometimes loss of
function. The reaction usually begins in the uterus and spreads to the
fallopian tubes, ovaries, and other areas
in the hipbone region of the body.
Wellbutrin
withdrawal
Premenstrual
Syndrome - Various physical and mental symptoms commonly experienced by women of
childbearing age usually 2 to 7 days before the start of their monthly period.
There are over 150 symptoms including eating binges, behavioral changes,
moodiness, irritability, fatigue, fluid retention, breast tenderness, headaches,
bloating, anxiety, and depression. The symptoms cease shortly after the period
begins, and disappear with menopause.
Wellbutrin
withdrawal
Spotting Between
Menses - Abnormal bleeding between periods. Unusual spotting
between menstrual cycles.
Wellbutrin
withdrawal
RESPIRATORY SYSTEM
(Organs involved in breathing)
Wellbutrin
withdrawal
Asthma
- A disease of the breathing system initiated by and allergic reaction
or a chemical with repeated attacks of coughing, sticky mucus, wheezing,
shortness of breath, and a tight feeling in the chest. The disease can reach a
state where it stops a person from exhaling, leading to unconsciousness and
death.
Wellbutrin
withdrawal
Breath Shortness
-
Unnatural breathing using a lot off effort resulting in not enough air taken in
by the body.
Wellbutrin
withdrawal
Bronchitis
- Inflammation of the two main
breathing tubes leading from the windpipe to the lungs. The disease is marked
with coughing, a low-grade fever, chest pains, and hoarseness, caused by an
allergic reaction.
Wellbutrin
withdrawal
Coughing
- A cough is the response to an
irritation, such as mucus, that causes the muscles controlling the breathing
process to expel air from the lungs suddenly and noisily to keep the air
passages free from the irritating material.
Wellbutrin
withdrawal
Laryngitis
- Inflammation of the voice box
characterized by hoarseness, sore throat, and coughing. It can be cause by
straining the voice or exposure to infectious, allergic or chemical irritation.
Wellbutrin
withdrawal
Nasal Congestion
- The
presence of an abnormal amount of fluid in the nose.
Wellbutrin
withdrawal
Pneumonia
Tracheitis - Bacterial infection of the air passageways and lungs that causes
redness, swelling and pain in the windpipe. Other symptoms are high fever,
chills, pain in the chest, difficulty in breathing, and coughing with mucus
discharge.
Wellbutrin
withdrawal
Rhinitis
- Chemical irritation causing pain,
redness and swelling in the mucus membranes of the nose.
Wellbutrin
withdrawal
Sinus Congestion
- The
mucus-lined areas of the bones in the face that are thought to help warm and
moisten air to the nose. These areas become clogged with excess fluid or
infected.
Wellbutrin
withdrawal
Sinus Headache
- The
abnormal amount of fluid in the hollows of the face bone area especially around
the nose. This excess fluid creates pressure, causing pain in the head.
Wellbutrin
withdrawal
Sinusitis
- The body reacting to chemical
irritation causing redness, swelling and pain in the area of the hollows in the
facial bones especially around the nose.
Wellbutrin
withdrawal SKELETAL
Wellbutrin withdrawal
Neck/Shoulder Pain
- Hurtful sensations
of the nerve endings caused by damage to the tissues in the neck and shoulder
signaling danger of disease.
Wellbutrin
withdrawal
SKIN and APPENDAGES DISORDERS (Skin, legs and arms)
Wellbutrin
withdrawal
Acne
- Eruptions of the oils glands of the
skin, especially on the face, marked by pimples, blackheads, whiteheads, bumps,
and more severely, by cysts and scarring.
Wellbutrin withdrawal
Alopecia -
The loss of hair or baldness.
Wellbutrin
withdrawal
Eczema
- A severe or continuing skin disease
marked by redness, crusting and scaling with watery blisters and itching. It is
often difficult to treat and will sometimes go away only to reappear again.
Wellbutrin
withdrawal
Dermatitis
- Generally irritated skin that can
be caused by any of a number of irritating things such as parasites, fungus,
bacteria, or foreign substances
causing an allergic reaction. It is a general inflammation of the skin.
Wellbutrin
withdrawal
Dry Lips
- The
lack of normal moisture in the fleshy folds that surround the mouth.
Wellbutrin withdrawal
Dry Skin - The lack of normal moisture/oils in the
surface layer of the body. The skin is the body’s largest organ.
Wellbutrin withdrawal
Folliculitis
-
Inflammation of a follicle (small body sac) especially a hair follicle. A hair
follicle contains the root of a hair.
Wellbutrin withdrawal
Furunculosis - Skin boils that show up repeatedly.
Wellbutrin withdrawal
Lipoma - A tumor of mostly fat cells that is not health
endangering.
Wellbutrin withdrawal
Pruritus
- Extreme itching of often-undamaged skin.
Wellbutrin withdrawal
Rash - A skin eruption or discoloration that may or may not be
itching, tingling, burning, or painful. It may be caused by an allergy, an skin
irritation, a skin disease.
Wellbutrin withdrawal
Skin Nodule - A bulge, knob, swelling or outgrowth in the skin
that is a mass of tissue or cells.
Wellbutrin withdrawal
SPECIAL SENSES
Wellbutrin withdrawal
Conjunctivitis
- Infection of the membrane that covers the eyeball and lines the eyelid, caused
by a virus, allergic reaction, or an irritating chemical. It is characterized
by redness, a discharge of fluid and itching.
Wellbutrin withdrawal
Dry Eyes - Not enough moisture in the eyes.
Wellbutrin withdrawal
Earache - Pain in the ear.
Wellbutrin withdrawal
Eye Infection
- The invasion of the eye tissue by a bacteria, virus, fungus, etc, causing
damage to the tissue, with toxicity. Infection spreading in the body progresses
into disease.
Wellbutrin withdrawal
Eye Irritation
- An inflammation of the eye.
Wellbutrin withdrawal
Metallic Taste
- A range of taste impairment from distorted taste to a complete loss of taste.
Wellbutrin withdrawal
Pupils Dilated
- Abnormal expansion of the blace circular opening in the center of the eye.
Wellbutrin withdrawal
Taste alteration
- Abnormal flavor detection in food.
Wellbutrin withdrawal
Tinnitus - A buzzing, ringing, or whistling sound in one or
both ears occurring from the internal use of certain drugs.
Wellbutrin withdrawal
Vision Abnormal
- Normal images are seen differently by the viewer.
Wellbutrin withdrawal
Vision Blurred
- Eyesight is dim or indistinct and hazy in outline or appearance.
Wellbutrin withdrawal
Visual Disturbance
- Eyesight is interfered with or interrupted. Some disturbances are light
sensitivity and the inability to easily distinguish colors.
Wellbutrin
withdrawal URINARY SYSTEM
DISORDER
Wellbutrin
withdrawal
Blood in Urine
-
Blood is present when one empties liquid waste product of the kidneys through
the bladder by urinating in the toilet turning the water pink to bright red. Or
you could see pots of blood in the water after urinating.
Wellbutrin
withdrawal
Dysuria
- Difficult or painful urination.
Wellbutrin
withdrawal
Kidney Stone
- Small hard masses of salt deposits that the kidney forms.
Wellbutrin
withdrawal
Urinary Frequency - Having to urinate more often than usual or between unusually short
time periods.
Wellbutrin
withdrawal
Urinary Tract
Infection - An invasion of bacteria, viruses, fungi, etc., of the
system in the body that starts with the kidneys and eliminates urine from the
body. If the invasion goes unchecked it can injure tissue and progress into
disease.
Wellbutrin
withdrawal
Urinary Urgency
- A sudden compelling urge to urinate, accompanied by discomfort in the bladder.
Wellbutrin
withdrawal
UROGENITAL (Urinary tract and genital structures or functions)
Wellbutrin
withdrawal
Anorgasmia
- Failure to experience an orgasm.
Wellbutrin
withdrawal
Ejaculation
Disorder - Dysfunction of the discharge of semen during orgasm.
Wellbutrin
withdrawal
Menstrual
Disorder - Dysfunction of the discharge during the monthly menstrual cycle.
Wellbutrin withdrawal
Acute Renal
Failure - The kidneys
stop functioning properly to excrete wastes.
Wellbutrin withdrawal
Angioedema
- Intensely itching and swelling welts on the skin called hives caused by an
allergic reaction to internal or external agents. The reaction is common to a
food or a drug. Chronic cases can last for a long period of time.
Wellbutrin
withdrawal
Toxic Epidermal
Necrolysis - An abnormal condition where a large portion of skin
becomes intensely red and peels off like a second-degree burn. Often the
symptoms include blistering.
Wellbutrin
withdrawal
Gastrointestinal
Hemorrhage - Stomach and intestinal excessive internal bleeding.
Wellbutrin withdrawal
Grand Mal
Seizures (or Convulsions)
- A recurring sudden violent and involuntary attack of muscle spasms with a loss
of consciousness.
Wellbutrin withdrawal
Neuroleptic Malignant Syndrome
- A life threatening, rare reaction to an anti-psychotic drug marked by fever,
muscular rigidity, changed mental status, and dysfunction of the autonomic
nervous system.
Wellbutrin withdrawal
Pancreatitis - Chemical irritation with redness, swelling, and
pain in the pancreas where digestive enzymes and hormones are secreted.
Wellbutrin withdrawal
QT Prolongation
- A very fast heart rhythm disturbance that is too fast for the heart to beat
effectively so the blood to the brain falls causing a sudden loss of
consciousness and may cause sudden cardiac death.
Wellbutrin withdrawal
Rhabdomyolysis
- The breakdown of muscle fibers that releases the fibers into the circulatory
system. Some of the fibers are poisonous to the kidney and frequently result in
kidney damage.
Wellbutrin withdrawal
Serotonin Syndrome
- A disorder brought on by excessive levels of serotonin caused by drugs and can
be fatal as death from this side effect can come very rapidly.
Wellbutrin withdrawal
Thrombocytopenia
- An abnormal decrease in the number of blood platelets in the circulatory
system. A decrease in platelets would cause a decrease in the ability of the
blood to clot when necessary.
Wellbutrin withdrawal
Torsades de Pointes
- Unusual rapid heart rhythm starting in the lower heart chambers. If the short
bursts of rapid heart rhythm continue for a prolonged period it can degenerate
into a more rapid rhythm and can be fatal.
Wellbutrin
withdrawal. How to avoid
Wellbutrin withdrawal side
effects
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Description
Antidepressant
Bupropion hydrochloride, an antidepressant of the aminoketone class, is chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. Its structure closely resembles that of diethylpropion; it is related to phenylethylamines. It is designated as (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone
hydrochloride. The molecular weight is 276.2. The emperical formula is C13H18CINO*HCl. Bupropion powder is white, crystalline, and highly soluble in water. It has a bitter taste and produces the sensation of local anesthesia on the oral mucosa.
Bupropion is supplied for oral administration as 75 mg (yellow-gold) and 100 mg (red) film-coated tablets. Each tablet contains the labeled amount of bupropion hydrochloride and the inactive ingredients: 75 mg tablet - D&C Yellow No. 10 Lake, FD&C Yellow No. 6 Lake, hydroxypropyl cellulose, hydroxypropyl
methylcelluose,
microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide; 100 mg tablet - FD&C Red No. 40 Lake, FD&C Yellow No. 6 Lake, hydroxypropyl cellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide.
Clinical Pharmacology
Pharmacodynamics and Pharmacological Actions:
The neurochemical mechanism of the antidepressant effect of bupropion is not known. Bupropion does not inhibit monoamine oxidase. Compared to classical tricyclic antidepressants, it is a weak blocker of the neuronal uptake of serotonin and norepinephrine; it also inhibits the neuronal re-uptake of dopamine to some extent.
Bupropion produces dose-related CNS stimulant effects in animals, as evidenced by increased locomotor activity, increased rates of responding in various schedule-controlled operant behavior tasks, and, at high doses, induction of mild stereotyped behavior.
Bupropion causes convulsions in rodents and dogs at doses approximately tenfold the dose recommended as the human antidepressant dose.
Absorption, Distribution, Pharmacokinetics, Metabolism, and Elimination:
Oral bioavailability and single-dose pharmacokinetics:
In humans, following oral administration of bupropion, peak plasma bupropion concentrations are usually achieved within 2 hours, followed by a biphasic decline. The average half-life of the second (post-distributional) phase is approximately 14 hours, with a range of 8 to 24 hours. Six hours after a single dose, plasma bupropion
concentrations are approximately 30% of peak concentrations. Plasma bupropion concentrations are dose-proportional following single doses of 100 to 250 mg; however, it is not known if the proportionality between dose and plasma level is maintained in chronic use.
The absolute bioavailability of bupropion tablets in humans has not been determined because an intravenous formulation for human use is not available.
However, it appears likely that only a small proportion of any orally administered dose reaches the systemic circulation intact. For example, the absolute bioavailability of bupropion in animals (rats and dogs) ranges from 5% to 20%.
Metabolism:
Following oral administration of 200 mg of 14C-bupropion, 87% and 10% of the radioactive dose were recovered in the urine and feces, respectively. However, the fraction of the oral dose of bupropion excreted unchanged was only 0.5%, a finding documenting the extensive metabolism of bupropion.
Several of the known metabolites of bupropion are pharmacologically active, but their potency and toxicity relative to bupropion have not been fully characterized. However, because of their longer elimination half-lives, the plasma concentrations of at least two of the known metabolites can be expected, especially in chronic use, to be
very much higher than the plasma concentration of bupropion. This is of potential clinical importance because factors or conditions altering metabolic capacity (e.g., liver disease, congestive heart failure, age, concomitant medications, etc.) or elimination may be expected to influence the degree and extend of accumulation of these
active metabolites.
Furthermore, bupropion has been shown to induce its own metabolism in three animal species (mice, rats, and dogs) following subchronic administration. If induction also occurs in humans, the relative contribution of bupropion and its metabolites to the clinical effects of bupropion may be changed in chronic use.
Plasma and urinary metabolites so far identified include biotransformation products formed via reduction of the carbonyl group and/or hydroxylation of the tert-butyl group of bupropion. Four basic metabolites have been identified.
They are the erythro- and threo-amino alcohols of bupropion, the erythro-amino diol of bupropion, and a morpholinol, metabolite (formed from hydroxylation of the tert-butyl group of bupropion).
The morpholinol metabolite appears in the systemic circulation almost as rapidly as the parent drug following a single oral dose. Its peak level is three times the peak level of the parent drug; it has a half life on the order of 24 hours; and its AUC 0 to 60 hours is about 15 times that of bupropion.
The threo-amino alcohol metabolite has a plasma concentration time profile similar to that of the morpholinol metabolite. The erythro-amino alcohol and the erythro-amino diol metabolites generally cannot be detected in the systemic circulation following a single oral dose of the parent drug. The morpholinol and the
threo-amino alcohol metabolites have been found to be half as potent as bupropion in animal screening tests for antidepressant drugs.
During a chronic dosing study in 14 depressed patients with left ventricular dysfunction, it was found that there was substantial interpatient variability (two- to five-fold) in the trough steady-state concentrations of bupropion and the morpholinol and threo-amino alcohol metabolites. In addition, the steady-state plasma
concentrations of these metabolites were 10 to 100 times the steady-state concentrations of the parent drug.
The effect of other disease states and altered organ function on the metabolism and/or elimination of bupropion has not been studied in detail. However, 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
conjugation in the liver prior to urinary excretion. The preliminary results of a comparative single-dose pharmacokinetic study in normal versus cirrhotic patients indicated that half-lives of the metabolites were prolonged by cirrhosis and that the metabolites accumulated to levels two to three times those in normals.
The effect of age on plasma concentrations of bupropion and its metabolites has not been characterized.
In vitro tests show that bupropion is 80% or more bound to human albumin at plasma concentrations up to 800 micromolar (200 mcg/mL).
Bupropion is indicated for the treatment of depression. A physician considering bupropion for the management of a patient's first episodes of depression should be aware that the drug may cause generalized seizures with an approximate incidence of 0.4% (4/1000). This incidence of seizures may exceed that of other marketed antidepressants
by as much as fourfold. This relative risk is only an approximate estimate because no direct comparative studies have been conducted.
The efficacy of bupropion has been established in three placebo-controlled trials, including two of approximately 3 weeks duration in depressed inpatients, and one of approximately 6 weeks duration in depressed outpatients. The depressive disorder of the patients studied corresponds most closely to the Major Depression category of the
APA Diagnostic and Statistical Manual III.
Major Depression implies a prominent and relatively persistent depressed or dysphoric mood that usually interferes with daily functioning (nearly every day for at least 2 weeks); it should include at least four of the following eight symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest
in usual activities or decrease in sexual drive, increased fatigability, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and suicidal ideation or attempts.
Effectiveness of bupropion in long-term use, that is, for more than 6 weeks, has not been systematically evaluated in controlled trials. Therefore, the physician who elects to use bupropion for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient.
Bupropion is contraindicated in patients with a seizure disorder. Bupropion is also contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in such patients treated with bupropion. The concurrent administration of bupropion and a monoamine oxidase (MAO)
inhibitor is contraindicated. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of treatment with bupropion. Bupropion is contraindicated in patients who have shown an allergic response to it.
Seizures:
Bupropion is associated with seizures in approximately 0.4% (4/1000) of patients treated at doses up to 450 mg/day. This incidence of seizures may exceed that of other marketed antidepressants by as much as fourfold. This relative risk is only an approximate estimate because no direct comparative studies have been conducted. The estimate
seizure incidence for bupropion increases almost tenfold between 450 and 600 mg/day, which is twice the usually required daily dose (300 mg) and one and one-third the maximum recommended daily dose (450 mg). Given the wide variability among individuals and their capacity to metabolize and eliminate drugs, this disproportionate increase in
seizure incidence with dose incrementation calls for caution in dosing.
During the initial development, 25 among approximately 2400 patients treated with bupropion experienced seizures. At the time of seizure, seven patients were receiving daily doses of 450 mg or below for an incidence of 0.33% (3/1000) within the recommended dose range. Twelve patients experienced seizures at 600 mg per day (2.3%
incidence); six additional patients has seizures at daily doses between 600 and 900 mg (2.8% incidence).
A separate, prospective study was conducted to determine the incidence of seizure during an 8-week treatment exposure in approximately 3200 additional patients who received daily doses of up to 450 mg. Patients were permitted to continue treatment beyond 8 weeks if clinically indicated. Eight seizures occurred during the initial 8-week
treatment period and five seizures were reported in patients continuing treatment beyond 8 weeks, resulting in a total seizure incidence of 0.4%.
The risk of seizure appears to be strongly associated with dose and the presence of predisposing factors. A significant seizure, CNS tumor, concomitant medications that lower seizure threshold, etc.) was present in approximately one-half of the patients experiencing a seizure. Sudden and large increments in dose may contribute to
increased risk. While many seizures occurred early in the course of treatment, some seizures did occur after several weeks at fixed dose.
Recommendations for reducing the risk of seizure:
Retrospective analysis of clinical experience gained during the development of bupropion suggests that the risk of seizure may be minimized if (1) the total daily dose of bupropion does not exceed 450 mg, (2) the daily dose is administered t.i.d., with each single dose not to exceed 150 mg to avoid high peak concentrations of bupropion
and/or its metabolites, and (3) the rate of incrementation of dose is very gradual. Extreme caution should be used when bupropion is (1) administered to patients with a history of seizure, cranial trauma, or other predisposition(s) toward seizure, or (2) prescribed with other agents (e.g., antipsychotics, other antidepressants, etc.) or
treatment regimens (e.g., abrupt discontinuation of a benzodiazepine) that lower seizure threshold.
Potential for Hepatotoxicity:
In rats receiving large doses of bupropion chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of bupropion chronically, various histologic changes were seen in the liver, and laboratory tests suggesting mild hepatocellular injury were noted.
Although scattered abnormalities in liver function tests were detected in patients participating in clinical trials, there is no clinical evidence that bupropion acts as a hepatotoxin in humans.
General:
Agitation and Insomnia: A substantial proportion of patients treated with bupropion experience some degree of increased restlessness, agitation, anxiety, and insomnia, especially shortly after initiation of treatment. In clinical studies, these symptoms were sometimes of sufficient magnitude to require treatment with
sedative/hypnotic drugs. In approximately 2% of patients, symptoms were sufficiently severe to require discontinuation of treatment with bupropion.
Psychosis, Confusion, and Other Neuropsychiatric Phenomena: Patients treated with bupropion have been reported to show a variety of neuropsychiatric signs and symptoms including delusions, hallucinations, psychotic episodes, confusion, and paranoia. Because of the uncontrolled nature of many studies, it is impossible to provide
a precise estimate of the extent of risk imposed by treatment with bupropion. In several cases, neuropsychitric phenomena abated upon dose reduction and/or withdrawal of treatment.
Activation of Psychosis and/or Mania: Antidepressants can precipitate manic episodes in Bipolar Manic Depressive patients during the depressed phase of their illness and may activate latent psychosis in other susceptible patients. Bupropion is expected to pose similar risks.
Altered Appetite and Weight: A weight loss of greater than 5 pounds occurred in 28% of patients receiving bupropion. This incidence is approximately double that seen in comparable patients treated with tricyclics or placebo. Furthermore, while 34.5% of patients receiving tricyclic antidepressants gained weight, only 9.4% of
patients treated with bupropion did. Consequently, if weight loss is a major presenting sign of a patient's depressive illness, the anorectic and/or weight reducing potential of bupropion should be considered.
Suicide: The possibility of a suicide attempt is inherent in depression and may persist until significant remission occurs. Accordingly, prescriptions for bupropion should be written for the smallest number of tablets consistent with good patient management.
Use in Patients with Systemic Illness:
There is no clinical experience establishing the safety of bupropion in patients with a recent history of myocardial infarction or unstable heart disease. Therefore, care should be exercised if it is used in these groups. Bupropion was well tolerated in patients who has previously developed orthostatic hypotension while receiving
tricyclic antidepressants.
Because bupropion HCl and its metabolites are almost completely excreted through the kidney and metabolites are likely to undergo conjugation in the liver prior to urinary excretion, treatment of patients with renal or hepatic, impairment should be initiated at reduced dosage as bupropion and its metabolites may accumulate in such
patients beyond concentrations expected in patients without renal or hepatic impairment. The patient should be closely monitored for possible toxic effects of elevated blood and tissue levels of drug and metabolites.
Information for Patients:
Physicians are advised to discuss the following issues with patients:
Patients should be instructed to take bupropion in equally divided doses three or four times a day to minimize the risk of seizure.
Patients should be told that any CNS-active drug like bupropion may impair their ability to perform tasks requiring judgment or motor and cognitive skills. Consequently, until they are reasonably certain that bupropion does not adversely affect their performance, they should refrain from driving an automobile or operating complex,
hazardous machinery.
Patients should be told that the use and cessation of use of alcohol may alter the seizure threshold, and, therefore, that the consumption of alcohol should be minimized, and, if possible, avoided completely.
Patients should be advised to inform their physician if they are taking or plan to take any prescription or over-the-counter drugs. Concern is warranted because bupropion and other drugs may affect each others metabolism.
Patients should be advised to notify their physician if they become pregnant or intend to become pregnant during therapy.
Drug Interactions:
No systematic data have been collected on the consequences of the concomitant administration of bupropion and other drugs.
However, animal data suggest that bupropion may be an inducer of drug metabolizing enzymes. This may be of potential clinical importance because the blood levels of co-administered drugs may be altered.
Alternatively, because bupropion is extensively metabolized, the co-administration of other drugs may affect its clinical activity. In particular, care should be exercised when administering drugs known to affect hepatic drug-metabolizing enzyme systems (e.g., carbamazepine, cimetidine, phenobarbital, phenytoin).
Studies in animals demonstrate that the acute toxicity of buproprion is enhanced by the MAO inhibitor phenelzine (see CONTRAINDICATIONS).
Limited clinical data suggest a higher incidence of adverse experiences in patients receiving concurrent administration of bupropion and L-dopa. Administration of bupropion to patients receiving L-dopa concurrently should be undertaken with caution, using small initial doses and small gradual dose increases.
Concurrent administration of bupropion and agents which lower seizure threshold should be undertaken only with extreme caution (see WARNINGS). Low initial dosing and small gradual dose increases should be employed.
Carcinogenesis, Mutagenesis, Impairment of Fertility:
Lifetime carcinogenicity studies were performed in rats and mice at doses up to 300 and 150 mg/kg/day, respectively. In the rat study there was an increase in nodular proliferative lesions of the liver at doses of 100 to 300 mg/kg/day; lower doses were not tested. 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.
Bupropion produced a borderline positive response (2 to 3 times control mutation rate) in some strains in the Ames bacterial mutagenicity test, and a high oral dose (300, but not 100 or 200 mg/kg) produced a low incidence of chromosomal aberrations in rats. The relevance of these results in estimating the risk of human exposure to
therapeutic doses is unknown.
A fertility study was performed in rats; no evidence of impairment of fertility was encountered at oral doses up to 300 mg/kg/day.
Pregnancy: Teratogenic Effects:
Pregnancy Category B: Reproduction studies have been performed in rabbits and rats at doses up to 15 to 45 times the human daily dose and have revealed no definitive evidence of impaired fertility or harm to the fetus due to bupropion. (In rabbits, a slightly increased incidence of fetal abnormalities was seen in two studies, but there
was no increase in any specific abnormality.) There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Labor and Delivery:
The effect of bupropion on labor and delivery in humans is unknown.
Nursing Mothers:
Because of the potential for serious adverse reactions in nursing infants from bupropion, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use:
The safety and effectiveness of bupropion in individuals under 18 years old have not been established.
Use in the Elderly:
Bupropion has not been systematically evaluated in older patients.
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