bisoprolol

Absorption: Well absorbed after oral administration, but 20% undergoes first-pass hepatic metabolism.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: 50% excreted unchanged by the kidneys; remainder renally excreted as metabolites; 2% excreted in feces.

Half-Life: 9–12 hr.

Time/Action Profile ⬆ ⬇

(antihypertensive effect)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1–4 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Uncompensated HF;
Pulmonary edema;
Cardiogenic shock;
Bradycardia or heart block.

Use Cautiously in:

Renal impairment (dosage ↓ recommended);
Hepatic impairment (dosage ↓ recommended);
Pulmonary disease (including asthma; beta₁ selectivity may be lost at higher doses); avoid use if possible;
Diabetes mellitus (may mask signs of hypoglycemia);
Thyrotoxicosis (may mask symptoms);
History of severe allergic reactions (intensity of reactions may be ↑);
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have sensitivity to beta blockers (initial dosage recommended).

Adv. Reactions/Side Effects ⬆ ⬇

CV: BRADYCARDIA, HF, hypotension, peripheral vasoconstriction

Derm: rash

EENT: blurred vision, stuffy nose

Endo: hyperglycemia, hypoglycemia

GI: ↑liver enzymes, constipation, diarrhea, nausea, vomiting

GU: erectile dysfunction, ↓libido, urinary frequency

MS: arthralgia, back pain, joint pain

Neuro: fatigue, weakness, anxiety, depression, dizziness, drowsiness, insomnia, memory loss, mental status changes, nervousness, nightmares

Resp: bronchospasm, PULMONARY EDEMA, wheezing

Misc: drug-induced lupus syndrome

Interactions ⬆ ⬇

Drug-drug:

General anesthetics, phenytoin, and verapamil may cause additive myocardial depression.
Additive bradycardia may occur with clonidine, digoxin, diltiazem, ivabradine, or verapamil.
Additive hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.
Concurrent use with amphetamine, cocaine, ephedrine, epinephrine, norepinephrine, phenylephrine, or pseudoephedrine may result in unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia).
Concurrent thyroid preparation administration may ↓ effectiveness.
May alter the effectiveness of insulins or oral hypoglycemic agents (dose adjustments may be necessary).
May ↓ the effectiveness of theophylline.
May ↓ the beta₁-cardiovascular effects of dopamine or dobutamine.
Use cautiously within 14 days of MAO inhibitor therapy (may result in hypertension).

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily, may be ↑ to 10 mg once daily (range 2.5–20 mg/day).

Renal Impairment

PO (Adults ): CCr <40 mL/min: Initiate therapy with 2.5 mg/day, titrate cautiously.

Hepatic Impairment

PO (Adults ): Hepatitis/Cirrhosis: Initiate therapy with 2.5 mg/day, titrate cautiously.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 10 mg
In combination with: hydrochlorothiazide (Ziac). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Monitor BP, ECG, and pulse frequently during dosage adjustment period and periodically throughout therapy.
Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of HF (dyspnea, rales/crackles, weight gain, peripheral edema, jugular venous distention).
Monitor frequency of prescription refills to determine adherence.

Lab Test Considerations:

May cause ↑ BUN, serum triglyceride, and uric acid levels.
- May cause ↑ in ANA titers.
- May cause ↑ in blood glucose levels.

Implementation ⬆ ⬇

PO: Take apical pulse before administering. If <50 bpm or if arrhythmia occurs, withhold medication and notify physician or other health care professional.
- May be administered without regard to meals.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication exactly as directed, at the same time each day, even if feeling well; do not skip or double up on missed doses. If a dose is missed, it should be taken as soon as possible up to 4 hr before next dose. Abrupt withdrawal may precipitate life-threatening arrhythmias, hypertension, or myocardial ischemia.
Teach patient and family how to check pulse and BP. Instruct them to check pulse daily and BP biweekly and to report significant changes to health care professional.
May cause drowsiness. Caution patients to avoid driving or other activities that require alertness until response to the drug is known.
Advise patients to change positions slowly to minimize orthostatic hypotension.
Caution patient that this medication may increase sensitivity to cold.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any Rx, OTC, or herbal products, especially cold preparations, concurrently with this medication. Patients on antihypertensive therapy should also avoid excessive amounts of coffee, tea, and cola.
Diabetics should closely monitor blood glucose, especially if weakness, malaise, irritability, or fatigue occurs. Medication does not block dizziness or sweating as signs of hypoglycemia.
Advise patient to notify health care professional if slow pulse, difficulty breathing, wheezing, cold hands and feet, dizziness, light-headedness, confusion, depression, rash, fever, sore throat, unusual bleeding, or bruising occurs.
Instruct patient to inform health care professional of medication regimen before treatment or surgery.
Advise patient to carry identification describing disease process and medication regimen at all times.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Hypertension: Reinforce the need to continue additional therapies for hypertension (weight loss, sodium restriction, stress reduction, regular exercise, moderation of alcohol consumption, and smoking cessation). Medication controls but does not cure hypertension.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇