Guanfacine (Page 3 of 4)

Nursing Mothers

It is not known whether guanfacine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when guanfacine hydrochloride is administered to a nursing woman. Experiments with rats have shown that guanfacine is excreted in the milk.

Pediatric Use

Safety and effectiveness in pediatric patients under 12 years of age have not been demonstrated. Therefore, the use of guanfacine in this age group is not recommended. There have been spontaneous postmarketing reports of mania and aggressive behavioral changes in pediatric patients with attention-deficit hyperactivity disorder (ADHD) receiving guanfacine. The reported cases were from a single center. All patients had medical or family risk factors for bipolar disorder. All patients recovered upon discontinuation of guanfacine HCl. Hallunications have been reported in pediatric patients receiving guanfacine for treatment of attention-deficit hyperactivity disorder.

Geriatric Use

Clinical studies of guanfacine did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy (see CLINICAL PHARMACOLOGY, Pharmacokinetics).

ADVERSE REACTIONS

Adverse reactions noted with guanfacine are similar to those of other drugs of the central α 2 adrenoreceptor agonist class: dry mouth, sedation (somnolence), weakness (asthenia), dizziness, constipation, and impotence. While the reactions are common, most are mild and tend to disappear on continued dosing.

Skin rash with exfoliation has been reported in a few cases; although clear cause and effect relationships to guanfacine could not be established, should a rash occur, guanfacine should be discontinued and the patient monitored appropriately.

In the dose-response monotherapy study described under CLINICAL PHARMACOLOGY, the frequency of the most commonly observed adverse reactions showed a dose relationship from 0.5 to 3 mg as follows:

Adverse Reaction

Placebo

n=59

0.5 mg

n=60

1 mg

n=61

2 mg

n=60

3 mg

n=59

Dry Mouth

0%

10%

10%

42%

54%

Somnolence

8%

5%

10%

13%

39%

Asthenia

0%

2%

3%

7%

3%

Dizziness

8%

12%

2%

8%

15%

Headache

8%

13%

7%

5%

3%

Impotence

0%

0%

0%

7%

3%

Constipation

0%

2%

0%

5%

15%

Fatigue

2%

2%

5%

8%

10%

The percent of patients who dropped out because of adverse reactions are shown below for each dosage group.

Placebo

0.5 mg

1 mg

2 mg

3 mg

Percent dropouts

0%

2%

5%

13%

32%

The most common reasons for dropouts among patients who received guanfacine were dry mouth, somnolence, dizziness, fatigue, weakness, and constipation.

In the 12-week placebo-controlled, dose-response study of guanfacine administered with 25 mg chlorthalidone at bedtime, the frequency of the most commonly observed adverse reactions showed a clear dose relationship from 0.5 to 3 mg as follows:

Adverse Reaction

Placebo

n = 73

0.5 mg

n = 72

1 mg

n = 72

2 mg

n = 72

3 mg

n = 72

Dry mouth

5 (7%)

4 (5%)

6 (8%)

8 (11%)

20 (28%)

Somnolence

1 (1%)

3 (4%)

0 (0%)

1 (1%)

10 (14%)

Asthenia

0 (0%)

2 (3%)

0 (0%)

2 (2%)

7 (10%)

Dizziness

2 (2%)

1 (1%)

3 (4%)

6 (8%)

3 (4%)

Headache

3 (4%)

4 (3%)

3 (4%)

1 (1%)

2 (2%)

Impotence

1 (1%)

1 (0%)

0 (0%)

1 (1%)

3 (4%)

Constipation

0 (0%)

0 (0%)

0 (0%)

1 (1%)

1 (1%)

Fatigue

3 (3%)

2 (3%)

2 (3%)

5 (6%)

3 (4%)

There were 41 premature terminations because of adverse reactions in this study. The percent of patients who dropped out and the dose at which the dropout occurred were as follows:

Dose:

Placebo

0.5 mg

1 mg

2 mg

3 mg

Percent dropouts

6.9%

4.2%

3.2%

6.9%

8.3%

Reasons for dropouts among patients who received guanfacine were: somnolence, headache, weakness, dry mouth, dizziness, impotence, insomnia, constipation, syncope, urinary incontinence, conjunctivitis, paresthesia, and dermatitis.

In a second 12-week placebo-controlled combination therapy study in which the dose could be adjusted upward to 3 mg per day in 1-mg increments at 3-week intervals, i.e., a setting more similar to ordinary clinical use, the most commonly recorded reactions were: dry mouth, 47%; constipation, 16%; fatigue, 12%; somnolence, 10%; asthenia, 6%; dizziness, 6%; headache, 4%; and insomnia, 4%.

Reasons for dropouts among patients who received guanfacine were: somnolence, dry mouth, dizziness, impotence, constipation, confusion, depression, and palpitations.

In the clonidine/guanfacine comparison described in CLINICAL PHARMACOLOGY, the most common adverse reactions noted were as follows:

Adverse Reactions

Guanfacine

(n=279)

Clonidine

(n=278)

Dry Mouth

30%

37%

Somnolence

21%

35%

Dizziness

11%

8%

Constipation

10%

5%

Fatigue

9%

8%

Headache

4%

4%

Insomnia

4%

3%

Adverse reactions occurring in 3% or less of patients in the three controlled trials of guanfacine with a diuretic were:

Cardiovascular — bradycardia, palpitations, substernal pain

Gastrointestinal — abdominal pain, diarrhea, dyspepsia, dysphagia, nausea

CNS — amnesia, confusion, depression, insomnia, libido decrease

ENT disorders — rhinitis, taste perversion, tinnitus

Eye disorders — conjunctivitis, iritis, vision disturbance

Musculoskeletal — leg cramps, hypokinesia

Respiratory — dyspnea

Dermatologic — dermatitis, pruritus, purpura, sweating

Urogenital — testicular disorder, urinary incontinence

Other — malaise, paresthesia, paresis

Adverse reaction reports tend to decrease over time. In an open-label trial of one year’s duration, 580 hypertensive subjects were given guanfacine, titrated to achieve goal blood pressure, alone (51%), with diuretic (38%), with beta blocker (3%), with diuretic plus beta blocker (6%), or with diuretic plus vasodilator (2%). The mean daily dose of guanfacine reached was 4.7 mg.

Adverse Reaction

Incidence of adverse reactions
at any time during the study

n=580

Incidence of adverse reactions
at end of one year

n=580

Dry Mouth

60%

15%

Drowsiness

33%

6%

Dizziness

15%

1%

Constipation

14%

3%

Weakness

5%

1%

Headache

4%

0.2%

Insomnia

5%

0%

There were 52 (8.9%) dropouts due to adverse effects in this 1-year trial. The causes were: dry mouth (n=20), weakness (n=12), constipation (n=7), somnolence (n=3), nausea (n=3), orthostatic hypotension (n=2), insomnia (n=1), rash (n=1), nightmares (n=1), headache (n=1), and depression (n=1).

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