Today's med: Fluoxetine (brand name: Prozac, Prozac weekly, Sarafem)
Drug Class: Antidepressant, SSRI
Fluvoxamine,Olanzapine/fluoxetine, Nefazodone,Citalopram Hydrobromide, Escitalopram oxalate, Trazodone hydrochloride,Sertraline Hydrochloride, Fluvoxamine Maleate, Paroxetine hydrochloride,Fluoxetine hydrochloride, Paroxetine mesylate, Paroxetine hydrochloride hemihydrate, Nefazodone hydrochloride
Action: Inhibits CNS neuron serotonin reuptake; minimal or no effect on reuptake of norepinephrine or dopamine; does not significantly bind to alpha-adrenergic, histamine, or cholinergic receptors
Indications:
Treatment of major depressive disorder (MDD); treatment of binge-eating and vomiting in patients with moderate-to-severe bulimia nervosa; obsessive-compulsive disorder (OCD); premenstrual dysphoric disorder (PMDD); panic disorder with or without agoraphobia; in combination with olanzapine for treatment-resistant or bipolar I depression
Selective mutism; treatment of mild dementia-associated agitation in nonpsychotic patients; post-traumatic stress disorder (PTSD); social anxiety disorder; fibromyalgia; Raynaud’s phenomenon; treatment of paraphilia/hypersexuality
Contraindications: Hypersensitivity to fluoxetine or any component of the formulation; use of MAO inhibitors intended to treat psychiatric disorders (concurrently, within 5 weeks of discontinuing fluoxetine, or within 2 weeks of discontinuing the MAO inhibitor); initiation of fluoxetine in a patient receiving linezolid or intravenous methylene blue; use with pimozide or thioridazine (Note: Thioridazine should not be initiated until 5 weeks after the discontinuation of fluoxetine)
Adverse Effects:
>10%: Central nervous system: Insomnia (10% to 33%), headache (21%), somnolence (5% to 17%), anxiety (6% to 15%), nervousness (8% to 14%)
Endocrine & metabolic: Libido decreased (1% to 11%)
Gastrointestinal: Nausea (12% to 29%), diarrhea (8% to 18%), anorexia (4% to 17%), xerostomia (4% to 12%)
Neuromuscular & skeletal: Weakness (7% to 21%), tremor (3% to 13%)
Respiratory: Pharyngitis (3% to 11%), yawn (≤11%)
1% to 10%:
Cardiovascular: Vasodilation (1% to 5%), chest pain, hemorrhage, hypertension, palpitation
Central nervous system: Dizziness (9%), abnormal dreams (1% to 5%), abnormal thinking (2%), agitation, amnesia, chills, confusion, emotional lability, sleep disorder
Dermatologic: Rash (2% to 6%), pruritus (4%)
Endocrine & metabolic: Ejaculation abnormal (≤7%), impotence (≤7%), menorrhagia (≥2%)
Gastrointestinal: Dyspepsia (6% to 10%), constipation (5%), flatulence (3%), vomiting (3%), thirst (≥2%), weight loss (2%), appetite increased, taste perversion, weight gain
Genitourinary: Urinary frequency
Neuromuscular & skeletal: Hyperkinesia (≥2%)
Ocular: Vision abnormal (2%)
Otic: Ear pain, tinnitus
Respiratory: Sinusitis (1% to 6%)
Miscellaneous: Flu-like syndrome (3% to 10%), diaphoresis (2% to 8%), epistaxis (≥2%)
<1% (Limited to important or life-threatening): Acne, acute abdominal syndrome, akathisia, albuminuria, allergies, alopecia, amenorrhea, anaphylactoid reactions, anemia, angina, aphthous stomatitis, aplastic anemia, arrhythmia, arthritis, asthma, ataxia, atrial fibrillation, balance disorder, bone pain, bruising, bruxism, bursitis, cardiac arrest, cataract, cerebrovascular accident, CHF, cholelithiasis, cholestatic jaundice, colitis, dehydration, delusions, depersonalization, dyskinesia, dysphagia, dysuria, ecchymosis, edema, eosinophilic pneumonia, erythema multiforme, erythema nodosum, esophagitis, euphoria, exfoliative dermatitis, extrapyramidal symptoms (rare), gastritis, gastroenteritis, GI ulcer, glossitis, gout, gynecological bleeding, gynecomastia, hallucinations, hepatic failure/necrosis, hepatitis, hiccup, hostility, hypercholesteremia, hyperprolactinemia, hypertonia, hyperventilation, hypoglycemia, hypokalemia, hyponatremia (possibly in association with SIADH), hypotension, hypothyroidism, immune-related hemolytic anemia, kidney failure, laryngospasm, laryngeal edema, leg cramps, liver function test abnormalities, lupus-like syndrome, malaise, melena, migraine, misuse/abuse, MI, mydriasis, myoclonus, neuroleptic malignant syndrome (NMS), optic neuritis, orthostatic hypotension, pancreatitis, pancytopenia, paranoid reaction, petechia, photosensitivity reaction, priapism, pulmonary embolism, pulmonary fibrosis, pulmonary hypertension, purpuric rash, QT prolongation, serotonin syndrome, Stevens-Johnson syndrome, suicidal ideation, syncope, tachycardia, thrombocytopenia, thrombocytopenic purpura, toxic epidermal necrolysis, vasculitis, ventricular tachycardia (including torsade de pointes), violent behavior
Standard Dosing:
Note: Upon discontinuation of fluoxetine therapy, gradually taper dose. If intolerable symptoms occur following a dose reduction, consider resuming the previously prescribed dose and/or decrease dose at a more gradual rate.
Children: Depression: 8-18 years: 10-20 mg/day; lower-weight children can be started at 10 mg/day, may increase to 20 mg/day after 1 week if needed
Obsessive-compulsive disorder: 7-17 years: Initial: 10 mg/day; may increase after 2 weeks if inadequate clinical response to 20 mg/day; further increases may be considered after several weeks to recommended range of 20-30 mg/day (lower weight children) or 20-60 mg/day (adolescents and higher weight children)
Selective mutism (unlabeled use): 5-18 years: Initial: 5-10 mg/day; titrate upwards as needed (usual maximum dose: 60 mg/day)
Adults: 20 mg/day in the morning; may increase after several weeks by 20 mg/day increments; maximum: 80 mg/day; doses >20 mg may be given once daily or divided twice daily. Note: Lower doses of 5-10 mg/day have been used for initial treatment.
Indication-specific dosing:
Bulimia nervosa: 60 mg/day
Depression: Initial: 20 mg/day; may increase after several weeks if inadequate response (maximum: 80 mg/day). Patients maintained on Prozac® 20 mg/day may be changed to Prozac® Weekly™ 90 mg/week, starting dose 7 days after the last 20 mg/day dose
Depression associated with bipolar disorder (in combination with olanzapine): Initial: 20 mg in the evening; adjust as tolerated to usual range of 20-50 mg/day. See "Note" below.
Fibromyalgia (unlabeled use): Range: 20-80 mg/day (Arnold, 2002)
Obsessive-compulsive disorder: Initial: 20 mg/day; may increase after several weeks if inadequate response; recommended range: 20-60 mg/day (maximum: 80 mg/day)
Panic disorder: Initial: 10 mg/day; after 1 week, increase to 20 mg/day; may increase after several weeks; doses >60 mg/day have not been evaluated
Post-traumatic stress disorder (PTSD) (unlabeled use): 20-40 mg/day
Premenstrual dysphoric disorder (Sarafem®): 20 mg/day continuously, or 20 mg/day starting 14 days prior to menstruation and through first full day of menses (repeat with each cycle)
Raynaud’s phenomena (unlabeled use): 20 mg/day (Coleiro, 2001)
Social anxiety disorder (unlabeled use): Target dose: 40 mg/day; range 30-60 mg/day (Davidson, 2004)
Treatment-resistant depression (in combination with olanzapine): Initial: 20 mg in the evening; adjust as tolerated to usual range of 20-50 mg/day. See "Note."
Note: When using individual components of fluoxetine with olanzapine rather than fixed dose combination product (Symbyax®), approximate dosage correspondence is as follows:
Olanzapine 2.5 mg + fluoxetine 20 mg = Symbyax® 3/25
Olanzapine 5 mg + fluoxetine 20 mg = Symbyax® 6/25
Olanzapine 12.5 mg + fluoxetine 20 mg = Symbyax® 12/25
Olanzapine 5 mg + fluoxetine 50 mg = Symbyax® 6/50
Olanzapine 12.5 mg + fluoxetine 50 mg = Symbyax® 12/50
Elderly: Depression: Some patients may require an initial dose of 10 mg/day with dosage increases of 10 and 20 mg every several weeks as tolerated; should not be taken at night unless patient experiences sedation
MAO inhibitor recommendations:
Switching to or from an MAO inhibitor intended to treat psychiatric disorders:
Allow 14 days to elapse between discontinuing an MAO inhibitor intended to treat psychiatric disorders and initiation of fluoxetine.
Allow 5 weeks to elapse between discontinuing fluoxetine and initiation of an MAO inhibitor intended to treat psychiatric disorders.
Use with other MAO inhibitors (linezolid or I.V. methylene blue):
Do not initiate fluoxetine in patients receiving linezolid or I.V. methylene blue; consider other interventions for psychiatric condition.
If urgent treatment with linezolid or I.V. methylene blue is required in a patient already receiving fluoxetine and potential benefits outweigh potential risks, discontinue fluoxetine promptly and administer linezolid or I.V. methylene blue. Monitor for serotonin syndrome for 5 weeks or until 24 hours after the last dose of linezolid or I.V. methylene blue, whichever comes first. May resume fluoxetine 24 hours after the last dose of linezolid or I.V. methylene blue.
Administration
Administer without regard to meals.
Bipolar I disorder and treatment-resistant depression: Take once daily in the evening.
Major depressive disorder and obsessive compulsive disorder: Once daily doses should be taken in the morning, or twice daily (morning and noon).
Bulimia: Take once daily in the morning.
Warnings:
Major psychiatric warnings:
• Suicidal thinking/behavior: [U.S. Boxed Warning]: Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (18-24 years of age) with major depressive disorder (MDD) and other psychiatric disorders;consider risk prior to prescribing. Short-term studies did not show an increased risk in patients >24 years of age and showed a decreased risk in patients ≥65 years. Closely monitor patients for clinical worsening, suicidality, or unusual changes in behavior, particularly during the initial 1-2 months of therapy or during periods of dosage adjustments (increases or decreases); the patient’s family or caregiver should be instructed to closely observe the patient and communicate condition with healthcare provider. A medication guide concerning the use of antidepressants should be dispensed with each prescription. Fluoxetine is FDA approved for the treatment of OCD in children ≥7 years of age and MDD in children ≥8 years of age.
• The possibility of a suicide attempt is inherent in major depression and may persist until remission occurs. Patients treated with antidepressants should be observed for clinical worsening and suicidality, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases. Worsening depression and severe abrupt suicidality that are not part of the presenting symptoms may require discontinuation or modification of drug therapy. Use caution in high-risk patients during initiation of therapy.
• Prescriptions should be written for the smallest quantity consistent with good patient care. The patient's family or caregiver should be alerted to monitor patients for the emergence of suicidality and associated behaviors such as anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, and mania; patients should be instructed to notify their healthcare provider if any of these symptoms or worsening depression or psychosis occur.
Concerns related to adverse effects:
• Allergic events and rash: Fluoxetine use has been associated with occurrences of significant rash and allergic events, including vasculitis, lupus-like syndrome, laryngospasm, anaphylactoid reactions, and pulmonary inflammatory disease. Discontinue if underlying cause of rash cannot be identified.
• Anticholinergic effects: Relatively devoid of these side effects
• Bleeding risk: May impair platelet aggregation resulting in increased risk of bleeding events, particularly if used concomitantly with aspirin, NSAIDs, warfarin or other anticoagulants. Bleeding related to SSRI use has been reported to range from relatively minor bruising and epistaxis to life-threatening hemorrhage.
• CNS depression: Has a low potential to impair cognitive or motor performance; caution operating hazardous machinery or driving.
• CNS effects: May cause insomnia, anxiety, nervousness, or anorexia.
• Serotonin syndrome: Potentially life-threatening serotonin syndrome (SS) has occurred with serotonergic agents (eg, SSRIs, SNRIs), particularly when used in combination with other serotonergic agents (eg, triptans, TCAs, fentanyl, lithium, tramadol, buspirone, St John’s wort, tryptophan) or agents that impair metabolism of serotonin (eg, MOA inhibitors intended to treat psychiatric disorders, other MAO inhibitors [ie,linezolid and intravenous methylene blue]). Monitor patients closely for signs of SS such as mental status changes (eg, agitation, hallucinations, delirium, coma); autonomic instability (eg, tachycardia, labile blood pressure, diaphoresis); neuromuscular changes (eg, tremor, rigidity, myoclonus); GI symptoms (eg, nausea, vomiting, diarrhea); and/or seizures. Discontinue treatment (and any concomitant serotonergic agent) immediately if signs/symptoms arise.
• Sexual dysfunction: May cause or exacerbate sexual dysfunction.
• SIADH and hyponatremia: SSRIs and SNRIs have been associated with the development of SIADH; hyponatremia has been reported rarely (including severe cases with serum sodium <110 mmol/L), predominately in the elderly. Volume depletion and/or concurrent use of diuretics likely increases risk.
• Weight loss: May cause anorexia and/or weight loss. Use caution in patients where weight loss is undesirable.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with a history of MI or unstable heart disease; experience in these patients is limited.
• Diabetes: Use with caution in patients with diabetes mellitus; may alter glycemic control and may require adjustment of antidiabetic medication; hypoglycemia and hyperglycemia has been observed during and after cessation of therapy, respectively.
• Hepatic impairment: Use with caution in patients with hepatic impairment; clearance is decreased and plasma concentrations are increased; a lower dosage may be needed in patients with cirrhosis.
• Mania/hypomania: May worsen psychosis in some patients or precipitate a shift to mania or hypomania in patients with bipolar disorder. Monotherapy in patients with bipolar disorder should be avoided. Patients presenting with depressive symptoms should be screened for bipolar disorder. Fluoxetine monotherapy is not FDA approved for the treatment of bipolar depression. Safety and efficacy in children <8 years of age (major depressive disorder) and <7 years of age (OCD) have not been established.
• Ocular effects: May cause mydriasis; use caution in patients at risk of acute narrow-angle glaucoma or with increased intraocular pressure
• Renal impairment: Use with caution in patients with severe renal impairment; a lower dosage or less frequent dosing may be needed.
• Seizure disorders: Use with caution in patients with a previous seizure disorder or conditions predisposing to seizures such as brain damage or alcoholism.
Concurrent drug therapy issues:
• Agents which lower seizure threshold: Use caution with concurrent therapy.
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
• Elderly: Use caution in elderly patients; may cause or exacerbate syndrome of inappropriate antidiuretic hormone secretion or hyponatremia; monitor sodium closely with initiation or dosage adjustments in older adults (Beers Criteria). May also cause agitation, sleep disturbances, and excessive CNS stimulation.
Other warnings/precautions:
• Electroconvulsive therapy: May increase the risks associated with electroconvulsive therapy; consider discontinuing, when possible, prior to ECT treatment.
• Long half-life: Due to the long half-life of fluoxetine and its metabolites, the effects and interactions noted may persist for prolonged periods following discontinuation.
• Withdrawal syndrome: May cause dysphoric mood, irritability, agitation, dizziness, sensory disturbances (eg, electric shock-like sensations), anxiety, confusion, headache, lethargy, emotional lability, insomnia, hypomania, tinnitus, and seizures. Upon discontinuation of fluoxetine therapy, gradually taper dose. If intolerable symptoms occur following a decrease in dosage or upon discontinuation of therapy, then resuming the previous dose with a more gradual taper should be considered.
Mental status for depression, suicidal ideation (especially at the beginning of therapy or when doses are increased or decreased), anxiety, social functioning, mania, panic attacks; signs/symptoms of serotonin syndrome; akathisia, sleep status; blood glucose (for diabetic patients), baseline liver function
C
Drug
interactions:
A total of 971 drugs (5476 brand and generic names) are known to interact with fluoxetine.
- 240 major drug interactions (1629 brand and generic names)
- 689 moderate drug interactions (3626 brand and generic names)
- 41 minor drug interactions (219 brand and generic names)
NSAID (COX-2 Inhibitor): Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of NSAID (COX-2 Inhibitor). NSAID (COX-2 Inhibitor) may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Monitor therapy
NSAID (Nonselective): Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of NSAID (Nonselective). NSAID (Nonselective) may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Management: Consider using alternative analgesics, when appropriate, and/or addition of an gastroprotective agent. Monitor patients closely for signs/symptoms of bleeding, and for evidence of diminished SSRI effectiveness with concurrent use. Consider therapy modification
Omega-3 Fatty Acids: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy
Salicylates: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result. Monitor therapy
Tryptophan: May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Avoid combination
Vitamin E: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy
Vitamin K Antagonists (eg, warfarin): Selective Serotonin Reuptake Inhibitors may enhance the anticoagulant effect of Vitamin K Antagonists.Monitor therapy
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