Bisoprolol Fumarate (Page 3 of 4)

PEDIATRIC USE

Safety and effectiveness in pediatric patients have not been established.

GERIATRIC USE

BISOPROLOL FUMARATE has been used in elderly patients with hypertension. Response rates and mean decreases in systolic and diastolic blood pressure were similar to the decreases in younger patients in the U.S. clinical studies. Although no dose response study was conducted in elderly patients, there was a tendency for older patients to be maintained on higher doses of bisoprolol fumarate.

Observed reductions in heart rate were slightly greater in the elderly than in the young and tended to increase with increasing dose. In general, no disparity in adverse experience reports or dropouts for safety reasons was observed between older and younger patients. Dose adjustment based on age is not necessary.

ADVERSE REACTIONS

Safety data are available in more than 30,000 patients or volunteers. Frequency estimates and rates of withdrawal of therapy for adverse events were derived from two U.S. placebo-controlled studies.

In Study A, doses of 5, 10, and 20 mg bisoprolol fumarate were administered for 4 weeks. In Study B, doses of 2.5, 10, and 40 mg of bisoprolol fumarate were administered for 12 weeks. A total of 273 patients were treated with 5 to 20 mg of bisoprolol fumarate; 132 received placebo.

Withdrawal of therapy for adverse events was 3.3% for patients receiving bisoprolol fumarate and 6.8% for patients on placebo. Withdrawals were less than 1% for either bradycardia or fatigue/lack of energy.

The following table presents adverse experiences, whether or not considered drug related, reported in at least 1% of patients in these studies, for all patients studied in placebo-controlled clinical trials (2.5 to 40 mg), as well as for a subgroup that was treated with doses within the recommended dosage range (5 to 20 mg). Of the adverse events listed in the table, bradycardia, diarrhea, asthenia, fatigue, and sinusitis appear to be dose related.

Body System/Adverse Experience All Adverse Experiences (%a) Bisoprolol Fumarate
Placebo (n=132) % 5 to 20 mg (n=273) % 2.5 to 40 mg (n=404) %
Skin
increased sweating 1.5 0.7 1.0
Musculoskeletal
arthralgia 2.3 2.2 2.7
Central Nervous System
dizziness 3.8 2.9 3.5
headache 11.4 8.8 10.9
hypoesthesia 0.8 1.1 1.5
Autonomic Nervous System
dry mouth 1.5 0.7 1.3
Heart Rate/Rhythm
bradycardia 0 0.4 0.5
Psychiatric
vivid dreams 0 0 0
insomnia 2.3 1.5 2.5
depression 0.8 0 0.2
Gastrointestinal
diarrhea 1.5 2.6 3.5
nausea 1.5 1.5 2.2
vomiting 0 1.1 1.5
Respiratory
bronchospasm 0 0 0
cough 4.5 2.6 2.5
dyspnea 0.8 1.1 1.5
pharyngitis 2.3 2.2 2.2
rhinitis 3.0 2.9 4.0
sinusitis 1.5 2.2 2.2
URI 3.8 4.8 5.0
Body as a Whole
asthenia 0 0.4 1.5
chest pain 0.8 1.1 1.5
fatigue 1.5 6.6 8.2
edema (peripheral) 3.8 3.7 3.0

a percentage of patients with event. The following is a comprehensive list of adverse experiences reported with bisoprolol fumarate in worldwide studies, or in postmarketing experience (in italics):

Central Nervous System

Dizziness, unsteadiness , vertigo, syncope , headache, paresthesia, hypoesthesia, hyperesthesia, somnolence, sleep disturbances , anxiety/restlessness, decreased concentration/memory.

Autonomic Nervous System

Dry mouth

Cardiovascular

Bradycardia, palpitations and other rhythm disturbances, cold extremities, claudication, hypotension, orthostatic hypotension, chest pain, congestive heart failure, dyspnea on exertion

Psychiatric

Vivid dreams, insomnia, depression.

Gastrointestinal

Gastric/epigastric/abdominal pain, gastritis, dyspepsia, nausea, vomiting, diarrhea, constipation, peptic ulcer

Musculoskeletal

Muscle/joint pain, arthralgia , back/neck pain, muscle cramps, twitching/tremor.

Skin

Rash, acne, eczema, psoriasis , skin irritation, pruritus, flushing, sweating, alopecia, dermatitis , angioedema , exfoliative dermatitis , cutaneous vasculitis

Special Senses

Visual disturbances, ocular pain/pressure, abnormal lacrimation, tinnitus, decreased hearing , earache, taste abnormalities.

Metabolic

Gout

Respiratory

Asthma/bronchospasm, bronchitis, coughing, dyspnea, pharyngitis, rhinitis, sinusitis, URI.

Genitourinary

Decreased libido/impotence, Peyronie’s disease , cystitis, renal colic, polyuria.

Hematologic

Purpura.

General

Fatigue, asthenia, chest pain, malaise, edema, weight gain, angioedema.

In addition, a variety of adverse effects have been reported with other beta-adrenergic blocking agents and should be considered potential adverse effects of BISOPROLOL FUMARATE:

Central Nervous System

Reversible mental depression progressing to catatonia, hallucinations, an acute reversible syndrome characterized by disorientation to time and place, emotional lability, slightly clouded sensorium.

Allergic

Fever, combined with aching and sore throat, laryngospasm, respiratory distress.

Hematologic

Agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

Gastrointestinal

Mesenteric arterial thrombosis, ischemic colitis.

Miscellaneous

The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with BISOPROLOL FUMARATE during investigational use or extensive foreign marketing experience.

Laboratory Abnormalities

In clinical trials, the most frequently reported laboratory change was an increase in serum triglycerides, but this was not a consistent finding.

Sporadic liver test abnormalities have been reported. In the U.S. controlled trials experience with bisoprolol fumarate treatment for 4-12 weeks, the incidence of concomitant elevations in SGOT and SGPT from 1 to 2 times normal was 3.9%, compared to 2.5% for placebo. No patient had concomitant elevations greater than twice normal.

In the long-term, uncontrolled experience with bisoprolol fumarate treatment for 6-18 months, the incidence of one or more concomitant elevations in SGOT and SGPT from 1 to 2 times normal was 6.2%. The incidence of multiple occurrences was 1.9%. For concomitant elevations in SGOT and SGPT of greater than twice normal, the incidence was 1.5%. The incidence of multiple occurrences was 0.3%. In many cases these elevations were attributed to underlying disorders, or resolved during continued treatment with bisoprolol fumarate.

Other laboratory changes included small increases in uric acid, creatinine, BUN, serum potassium, glucose, and phosphorus and decreases in WBC and platelets. These were generally not of clinical importance and rarely resulted in discontinuation of bisoprolol fumarate.

As with other beta-blockers, ANA conversions have also been reported on bisoprolol fumarate. About 15% of patients in long-term studies converted to a positive titer, although about one-third of these patients subsequently reconverted to a negative titer while on continued therapy.

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