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Guanfacine Extended-Release is a brand name for Guanfacine. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: 1 INDICATIONS AND USAGE Guanfacine extended-release tablets are indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) as monotherapy and as adjunctive therapy to stimulant medications [see Clinical Studies (14 )] . Guanfacine extended-release tablets are a central alpha 2A -adrenergic receptor…
Verbatim from this product's FDA label. Tap a section to expand.
2 ). 2 ). 1 ). 1 ). 3 ). 3 ). 5 ). 1 General Instruction for Use Swallow tablets whole. Do not crush, chew, or break tablets because this will increase the rate of guanfacine release. Do not administer with high fat meals, due to increased exposure.
2 Dose Selection Take guanfacine extended-release tablets orally once daily, either in the morning or evening, at approximately the same time each day. Begin at a dose of 1 mg/day, and adjust in increments of no more than 1 mg/week.
In monotherapy clinical trials, there was dose- and exposure-related clinical improvement as well as risks for several clinically significant adverse reactions (hypotension, bradycardia, sedative events). 12 mg/kg/day (total daily dose between 1 to 7 mg) (see Table 1).
12 mg/kg/day range. Doses above 4 mg/day have not been studied in adjunctive trials. 3 Switching from Immediate-Release Guanfacine to Guanfacine Extended-Release Tablets If switching from immediate-release guanfacine, discontinue that treatment, and titrate with guanfacine extended-release tablets following above recommended schedule.
Do not substitute for immediate-release guanfacine tablets on a milligram-per-milligram basis, because of differing pharmacokinetic profiles. 3) ] . 4 Maintenance Treatment Pharmacological treatment of ADHD may be needed for extended periods.
Healthcare providers should periodically re-evaluate the long-term use of guanfacine extended-release tablets, and adjust weight-based dosage as needed. 12 mg/kg/day range. Doses above 4 mg/day have not been evaluated in children (ages 6 to 12 years) and above 7 mg/day have not been evaluated in adolescents (ages 13 to 17 years) [see Clinical Studies ( 14 )] .
4 ) and Adverse Reactions (6) ]. Patients/caregivers should be instructed not to discontinue guanfacine extended-release tablets without consulting their health care provider. Monitor blood pressure and pulse when reducing the dose or discontinuing the drug.
Taper the daily dose in decrements of no more than 1 mg every 3 to 7 days to minimize the risk of rebound hypertension. 6 Missed Doses When reinitiating patients to the previous maintenance dose after two or more missed consecutive doses, consider titration based on patient tolerability.
, carbamazepine) (Table 2) [see Drug Interactions ( 7 )] .
1 ). 1 ). To report SUSPECTED ADVERSE REACTIONS, contact Apotex Corp. gov/medwatch. 1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The data described below reflect clinical trial exposure to guanfacine extended-release tablets in 2,825 patients. This includes 2,330 patients from completed studies in children and adolescents, ages 6 to 17 years and 495 patients in completed studies in adult healthy volunteers.
The mean duration of exposure of 446 patients that previously participated in two 2-year, open-label long-term studies was approximately 10 months.
Fixed Dose Trials Table 3:
Percentage of Patients Experiencing Most Common (≥5% and at least twice the rate for placebo) Adverse Reactions in Fixed Dose Studies 1 and 2 Guanfacine Extended-Release Tablets (mg) Adverse Reaction Term Placebo (N=149) 1mg* (N=61) 2mg (N=150) 3mg (N=151) 4mg (N=151) All Doses of Guanfacine Extended-Release Tablets (N=513) Somnolence a 11% 28% 30% 38% 51% 38% Fatigue 3% 10% 13% 17% 15% 14% Hypotension b 3% 8% 5% 7% 8% 7% Dizziness 4% 5% 3% 7% 10% 6% Lethargy 3% 2% 3% 8% 7% 6% Nausea 2% 7% 5% 5% 6% 6% Dry mouth 1% 0% 1% 6% 7% 4% *The lowest dose of 1 mg used in Study 2 was not randomized to patients weighing more than 50 kg.
a: The somnolence term includes somnolence, sedation, and hypersomnia. b: The hypotension term includes hypotension, diastolic hypotension, orthostatic hypotension, blood pressure decreased, blood pressure diastolic decreased, blood pressure systolic decreased.
Table 4:
5 WARNINGS AND PRECAUTIONS Hypotension, bradycardia, syncope: Titrate slowly and monitor vital signs frequently in patients at risk for hypotension, heart block, bradycardia, syncope, cardiovascular disease, vascular disease, cerebrovascular disease or chronic renal failure.
Measure heart rate and blood pressure prior to initiation of therapy, following dose increases, and periodically while on therapy. Avoid concomitant use of drugs with additive effects unless clinically indicated. 1 ).
Sedation and somnolence:
Occur commonly with guanfacine extended-release tablets. Consider the potential for additive sedative effects with CNS depressant drugs. 2 ).
Cardiac Conduction Abnormalities:
May worsen sinus node dysfunction and atrioventricular (AV) block, especially in patients taking other sympatholytic drugs. 3 ).
Rebound Hypertension:
Abrupt discontinuation of guanfacine extended-release tablets can lead to clinically significant and persistent rebound hypertension. Subsequent hypertensive encephalopathy was also reported. 4 ). 1 Hypotension, Bradycardia, and Syncope Treatment with guanfacine extended-release tablets can cause dose-dependent decreases in blood pressure and heart rate.
Decreases were less pronounced over time of treatment. 1) ]. Measure heart rate and blood pressure prior to initiation of therapy, following dose increases, and periodically while on therapy. , heart block, bradycardia, cardiovascular disease, vascular disease, cerebrovascular disease, or chronic renal failure.
In patients who have a history of syncope or may have a condition that predisposes them to syncope, such as hypotension, orthostatic hypotension, bradycardia, or dehydration, advise patients to avoid becoming dehydrated or overheated.
4 CONTRAINDICATIONS Guanfacine extended-release tablets are contraindicated in patients with a history of a hypersensitivity reaction to guanfacine extended-release tablets or its inactive ingredients, or other products containing guanfacine.
Rash and pruritus have been reported. History of hypersensitivity to guanfacine extended-release tablets, its inactive ingredients, or other products containing guanfacine ( 4 ).
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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Table 2:
Guanfacine Extended-Release Tablets Dosage Adjustments for Patients Taking Concomitant CYP3A4 Inhibitors or Inducers Clinical Scenarios Starting Guanfacine Extended-Release Tablets while currently on a CYP3A4 modulator Continuing Guanfacine Extended-Release Tablets while adding a CYP3A4 modulator Continuing Guanfacine Extended-Release Tablets while stopping a CYP3A4 modulator CYP3A4 Strong and moderate Inhibitors Decrease guanfacine extended-release tablets dosage to half the recommended level.
(See Table 1) Decrease guanfacine extended-release tablets dosage to half the recommended level. (See Table 1) Increase guanfacine extended-release tablets dosage to recommended level. (See Table 1) CYP3A4 Strong and moderate Inducers Consider increasing guanfacine extended-release tablets dosage up to double the recommended level.
(See Table 1) Consider increasing guanfacine extended-release tablets dosage up to double the recommended level over 1 to 2 weeks. (See Table 1) Decrease guanfacine extended-release tablets dosage to recommended level over 1 to 2 weeks.
(See Table 1)
Adverse Reactions Leading to Discontinuation (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in Fixed Dose Studies 1 and 2 Guanfacine Extended-Release Tablets (mg) Adverse Reaction Term Placebo (N=149) 1mg* (N=61) 2mg (N=150) 3mg (N=151) 4mg (N=151) All Doses of Guanfacine Extended-Release Tablets (N=513) n (%) n (%) n (%) n (%) n (%) n (%) Total patients 4 (3%) 2 (3%) 10 (7%) 15 (10%) 27 (18%) 54 (11%) Somnolence a 1 (1%) 2 (3%) 5 (3%) 6 (4%) 17 (11%) 30 (6%) Fatigue 0 (0%) 0 (0%) 2 (1%) 2 (1%) 4 (3%) 8 (2%) Adverse reactions leading to discontinuation in ≥ 2% in any dose group but did not meet this criteria in all doses combined: hypotension (hypotension, diastolic hypotension, orthostatic hypotension, blood pressure decreased, blood pressure diastolic decreased, blood pressure systolic decreased), headache, and dizziness.
* The lowest dose of 1 mg used in Study 2 was not randomized to patients weighing more than 50 kg. a: The somnolence term includes somnolence, sedation, and hypersomnia.
Table 5:
Other Common Adverse Reactions (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in Fixed Dose Studies 1 and 2 Guanfacine Extended-Release Tablets (mg) Adverse Reaction Term Placebo (N=149) 1mg* (N=61) 2mg (N=150) 3mg (N=151) 4mg (N=151) All Doses of Guanfacine Extended-Release Tablets (N=513) Headache 19% 26% 25% 16% 28% 23% Abdominal Pain a 9% 10% 7% 11% 15% 11% Decreased Appetite 4% 5% 4% 9% 6% 6% Irritability 4% 5% 8% 3% 7% 6% Constipation 1% 2% 2% 3% 4% 3% Nightmare b 0% 0% 0% 3% 4% 2% Enuresis c 1% 0% 1% 3% 2% 2% Affect Lability d 1% 2% 1% 3% 1% 2% Adverse reactions ≥2% for all doses of guanfacine extended-release tablets and >rate in placebo in any dose group but did not meet this criteria in all doses combined: insomnia (insomnia, initial insomnia, middle insomnia, terminal insomnia, sleep disorder), vomiting, diarrhea, abdominal/stomach discomfort (abdominal discomfort, epigastric discomfort, stomach discomfort), rash (rash, rash generalized, rash papular), dyspepsia, increased weight, bradycardia (bradycardia, sinus bradycardia), asthma (asthma, bronchospasm, wheezing), agitation, anxiety (anxiety, nervousness), sinus arrhythmia, blood pressure increased (blood pressure increased, blood pressure diastolic increased), and first degree atrioventricular block.
* The lowest dose of 1 mg used in Study 2 was not randomized to patients weighing more than 50 kg. a: The abdominal pain term includes abdominal pain, abdominal pain lower, abdominal pain upper, and abdominal tenderness. b: The nightmare term includes abnormal dreams, nightmare, and sleep terror.
c: The enuresis term includes enuresis, nocturia, and urinary incontinence. d: The affect lability term includes affect lability and mood swings.
Monotherapy Flexible Dose Trials Table 6:
Percentage of Patients Experiencing Most Common (≥5% and at least twice the rate for placebo) Adverse Reactions in the Monotherapy Flexible Dose Study 4 Guanfacine Extended-Release Tablets Adverse Reaction Term Placebo (N=112) AM (N=107) PM (N=114) All Doses of Guanfacine Extended-Release Tablets (N=221) Somnolence a 15% 57% 54% 56% Abdominal Pain b 7% 8% 19% 14% Fatigue 3% 10% 11% 11% Irritability 3% 7% 7% 7% Nausea 1% 6% 5% 5% Dizziness 3% 6% 4% 5% Vomiting 2% 7% 4% 5% Hypotension c 0% 6% 4% 5% Decreased Appetite 3% 6% 3% 4% Enuresis d 1% 2% 5% 4% a: The somnolence term includes somnolence, sedation, and hypersomnia.
b: The abdominal pain term includes abdominal pain, abdominal pain lower, abdominal pain upper, and abdominal tenderness c: The hypotension term includes hypotension, diastolic hypotension, orthostatic hypotension, blood pressure decreased, blood pressure diastolic decreased, blood pressure systolic decreased.
d: The enuresis term includes enuresis, nocturia, and urinary incontinence.
Table 7:
Adverse Reactions Leading to Discontinuation (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in Monotherapy Flexible Dose Study 4 Guanfacine Extended-Release Tablets Adverse Reaction Term Placebo (N=112) AM (N=107) PM (N=114) All Doses of Guanfacine Extended-Release Tablets (N=221) n (%) n (%) n (%) n (%) Total patients 0 (0%) 8 (7%) 7 (6%) 15 (7%) Somnolence a 0 (0%) 4 (4%) 3 (3%) 7 (3%) Adverse reactions leading to discontinuation in ≥2% in any dose group but did not meet this criteria in all doses combined: fatigue a: The somnolence term includes somnolence, sedation, and hypersomnia.
Table 8:
Other Common Adverse Reactions (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in the Monotherapy Flexible Dose Study 4 Guanfacine Extended-Release Tablets Adverse Reaction Term Placebo (N=112) AM (N=107) PM (N=114) All Doses of Guanfacine Extended-Release Tablets (N=221) Headache 11% 18% 16% 17% Insomnia a 6% 8% 6% 7% Diarrhea 4% 4% 6% 5% Lethargy 0% 4% 3% 3% Constipation 2% 2% 4% 3% Dry Mouth 1% 3% 3% 3% Adverse reactions ≥2% for all doses of guanfacine extended-release tablets and >rate in placebo in any dose group but did not meet this criteria in all doses combined: affect lability (affect lability, mood swings), increased weight, syncope/loss of consciousness (loss of consciousness, presyncope, syncope), dyspepsia, tachycardia (tachycardia, sinus tachycardia), and bradycardia (bradycardia, sinus bradycardia).
a: The insomnia term includes insomnia, initial insomnia, middle insomnia, terminal insomnia, and sleep disorder.
Table 9:
Percentage of Patients Experiencing Most Common (≥ 5% and at least twice the rate for placebo) Adverse Reactions in the Monotherapy Flexible Dose Study 5 Adverse Reaction Term Placebo (N=155) All Doses of Guanfacine Extended-Release Tablets (N=157) Somnolence a 23% 54% Insomnia b 6% 13% Hypotension c 3% 9% Dry Mouth 0% 8% Postural Dizziness 2% 5% Bradycardia d 0% 5% a: The somnolence term includes somnolence, sedation, and hypersomnia.
b: The insomnia term includes insomnia, initial insomnia, middle insomnia, terminal insomnia, and sleep disorder. c: The hypotension term includes hypotension, diastolic hypotension, orthostatic hypotension, blood pressure decreased, blood pressure diastolic decreased, blood pressure systolic decreased).
d: The bradycardia term includes bradycardia and sinus bradycardia. There were no specific adverse reactions ≥2% in any treatment group that led to discontinuation in the monotherapy flexible dose study (Study 5).
Table 10:
Other Common Adverse Reactions (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in the Monotherapy Flexible Dose Study 5 Guanfacine Extended-Release Tablets Adverse Reaction Term Placebo (N=155) All Doses of Guanfacine Extended-Release Tablets (N=157) Headache 18% 27% Fatigue 12% 22% Dizziness 10% 16% Decreased Appetite 14% 15% Abdominal Pain a 8% 12% Irritability 4% 7% Anxiety b 3% 5% Rash c 1% 3% Constipation 0% 3% Increased Weight 2% 3% Abdominal/Stomach Discomfort d 1% 2% Pruritus 1% 2% Adverse reactions ≥2% for all doses of guanfacine extended-release tablets and >rate in placebo in any dose group but did not meet this criteria in all doses combined: nausea, diarrhea, vomiting, and depression (depressed mood, depression, depressive symptom).
a: The abdominal pain term includes abdominal pain, abdominal pain lower, abdominal pain upper, and abdominal tenderness. b: The anxiety term includes anxiety and nervousness. c: The rash term includes rash, rash generalized, and rash papular.
d: The abdominal/stomach discomfort term includes abdominal discomfort, epigastric discomfort, and stomach discomfort.
Adjunctive Trial Table 11:
Percentage of Patients Experiencing Most Common (≥5% and at least twice the rate for placebo) Adverse Reactions in the Short-Term Adjunctive Study 3 Guanfacine Extended-Release Tablets + stimulant Adverse Reaction Term Placebo+ stimulant (N=153) AM (N=150) PM (N=152) All Doses (N=302) Somnolence a 7% 18% 18% 18% Insomnia b 6% 10% 14% 12% Abdominal Pain c 3% 8% 12% 10% Fatigue 3% 12% 7% 10% Dizziness 4% 10% 5% 8% Decreased Appetite 4% 7% 8% 7% Nausea 3% 3% 7% 5% a: The somnolence term includes somnolence, sedation, and hypersomnia.
b: The insomnia term includes insomnia, initial insomnia, middle insomnia, terminal insomnia, and sleep disorder. c: The abdominal pain term includes abdominal pain, abdominal pain lower, abdominal pain upper, and abdominal tenderness.
There were no specific adverse reactions ≥2% in any treatment group that led to discontinuation in the short-term adjunctive study (Study 3).
Table 12:
Other Common Adverse Reactions (≥2% for all doses of Guanfacine Extended-Release Tablets and >rate than in placebo) in the Short-Term Adjunctive Study 3 Guanfacine Extended-Release Tablets + stimulant Adverse Reaction Term Placebo (N=153) AM (N=150) PM (N=152) All Doses of Guanfacine Extended-Release Tablets (N=302) Headache 13% 21% 21% 21% Diarrhea 1% 4% 3% 4% Hypotension a 0% 4% 2% 3% Constipation 0% 2% 3% 2% Affect Lability b 1% 3% 2% 2% Dry Mouth 0% 1% 3% 2% Bradycardia c 0% 1% 3% 2% Postural Dizziness 0% 1% 3% 2% Rash d 1% 1% 2% 2% Nightmare e 1% 2% 1% 2% Tachycardia f 1% 2% 1% 2% Adverse reactions ≥2% for all doses of guanfacine extended-release tablets and >rate in placebo in any dose group but did not meet this criteria in all doses combined: irritability, vomiting, asthma (asthma, bronchospasm, wheezing), and enuresis (enuresis, nocturia, urinary incontinence).
a: The hypotension term includes hypotension, diastolic hypotension, orthostatic hypotension, blood pressure decreased, blood pressure diastolic decreased, blood pressure systolic decreased. b: The affect lability term includes affect lability and mood swings.
c: The bradycardia term includes bradycardia and sinus bradycardia. d: The rash term includes rash, rash generalized, and rash papular. e: The nightmare term includes abnormal dreams, nightmare, and sleep terror. f: The tachycardia term includes tachycardia and sinus tachycardia.
5 bpm, respectively, for all doses combined (generally one week after reaching target doses). 2 mmHg. 4 mmHg. 6 bpm. Decreases in blood pressure and heart rate were usually modest and asymptomatic; however, hypotension and bradycardia can occur.
Hypotension was reported as an adverse reaction for 7% of the guanfacine extended-release tablets group and 3% of the placebo group. This includes orthostatic hypotension, which was reported for 1% of the guanfacine extended-release tablets group and none in the placebo group.
These findings were generally similar in the monotherapy flexible dose trials (Studies 4 and 5). In the adjunctive trial, hypotension (3%) and bradycardia (2%) were observed in patients treated with guanfacine extended-release tablets as compared to none in the placebo group.
In long-term, open-label studies, (mean exposure of approximately 10 months), maximum decreases in systolic and diastolic blood pressure occurred in the first month of therapy. Decreases were less pronounced over time. Syncope occurred in 1% of pediatric patients in the clinical program.
The majority of these cases occurred in the long-term, open-label studies. Discontinuation of Treatment Blood pressure and pulse may increase above baseline values following discontinuation of guanfacine extended-release tablets. In five studies of children and adolescents [see Clinical Studies ( 14 )] , increases in mean systolic and diastolic blood pressure averaging approximately 3 mmHg and increases in heart rate averaging 5 beats per minute above original baseline were observed upon discontinuation with tapering of guanfacine extended-release tablets.
In a maintenance of efficacy study, increases in blood pressure and heart rate above baseline slowly diminished over the follow up period, which ranged between 3 and 26 weeks post final dose; the estimated average time to return to baseline was between six and twelve months.
In this study, the increases in blood pressure and pulse were not considered serious or associated with adverse events. However, individuals may have larger increases than reflected by the mean changes. 2 )]. Effects on Height, Weight, and Body Mass Index (BMI) Patients taking guanfacine extended-release tablets demonstrated similar growth compared to normative data.
5 kg compared to those receiving placebo over a comparable treatment period. Patients receiving guanfacine extended-release tablets for at least 12 months in open-label studies gained an average of 8 kg in weight and 8 cm (3 in) in height.
The height, weight, and BMI percentile remained stable in patients at 12 months in the long-term studies compared to when they began receiving guanfacine extended-release tablets. 1, listed by organ system. 2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of guanfacine.
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. 1, include: General: edema, malaise, tremor Cardiovascular: palpitations, tachycardia , rebound hypertension, hypertensive encephalopathy Central Nervous System: paresthesias, vertigo Eye Disorders: blurred vision Musculo-Skeletal System: arthralgia, leg cramps, leg pain, myalgia Psychiatric: confusion, hallucinations Reproductive System, Male: erectile dysfunction Respiratory System: dyspnea Skin and Appendages: alopecia, dermatitis, exfoliative dermatitis, pruritus, rash Special Senses: alterations in taste
Monitor blood pressure and heart rate, and adjust dosages accordingly in patients treated concomitantly with antihypertensives or other drugs that can reduce blood pressure or heart rate or increase the risk of syncope. 1) ]. Before using guanfacine extended-release tablets with other centrally active depressants, consider the potential for additive sedative effects.
Caution patients against operating heavy equipment or driving until they know how they respond to treatment with guanfacine extended-release tablets. Advise patients to avoid use with alcohol. 3 Cardiac Conduction Abnormalities The sympatholytic action of guanfacine extended-release tablets may worsen sinus node dysfunction and atrioventricular (AV) block, especially in patients taking other sympatholytic drugs.
Titrate guanfacine extended-release tablets slowly and monitor vital signs frequently in patients with cardiac conduction abnormalities or patients concomitantly treated with other sympatholytic drugs. 4 Rebound Hypertension In post marketing experience, abrupt discontinuation of guanfacine extended-release tablets has resulted in clinically significant and persistent rebound hypertension above baseline levels and increases in heart rate.
2 )] . In these cases, high-dosage guanfacine was discontinued; concomitant stimulant use was also reported, which may potentially increase hypertensive response upon abrupt discontinuation of guanfacine. Children commonly have gastrointestinal illnesses that lead to vomiting, and a resulting inability to take medications, so they may be especially at risk for rebound hypertension.
5 )] . Blood pressure and heart rate should be monitored when reducing the dose or discontinuing guanfacine extended-release tablets. If abrupt discontinuation occurs (especially with concomitant stimulant use), patients should be closely followed for rebound hypertension.