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atenolol (Tenormin)

 

Classes: Beta-Blockers, Beta-1 Selective

Dosing and uses of Tenormin (atenolol)

 

Adult dosage forms and strengths

tablet

  • 25mg
  • 50mg
  • 100mg

 

Hypertension

25-50 mg/day PO initially; may be increased to 100 mg/day PO

 

Angina Pectoris

50 mg/day PO; after 1 week, may be increased to 100 mg/day PO; some patients may require 200 mg/day

 

Post Myocardial Infarction

Secondary prevention

100 mg PO once daily or divided q12hr for 6-9 days after myocardial infarction (MI)

 

Alcohol Withdrawal Syndrome (Off-label)

50-100 mg/day PO

 

Supraventricular Arrhythmias (Off-label)

Prevention

50 mg/day PO, beginning up to 3 days before surgery and continued until 7 days after surgery; may be increased to 100 mg/day

 

Thyrotoxicosis (Off-label)

25-100 mg PO once daily or divided q12hr

 

Dosing Modifications

CrCl 15-35 mL/min/1.73 m²: Not to exceed 50 mg/day PO

CrCl <15 mL/min/1.73 m²: Not to exceed 25 mg/day PO

CrCl >35 mL/min/1.73 m²: Dose adjustment not necessary  

 

Pediatric dosage forms and strengths

tablet

  • 25mg
  • 50mg
  • 100mg

 

Hypertension (Off-label)

0.5-1 mg/kg/day PO; not to exceed 2 mg/kg/day or 100 mg/day

 

Geriatric dosage forms and strengths

May be necessary to initiate dosing at 25 mg/day PO

 

Hypertension

25 mg/day PO initially; may be increased to 100 mg/day PO

 

Angina Pectoris

25 mg/day PO; after 1 week, may be increased to 100 mg/day; some patients may require 200 mg/day

 

Post Myocardial Infarction

Secondary prevention

100 mg PO once daily or divided q12hr for 6-9 days after MI

 

Tenormin (atenolol) adverse (side) effects

>10%

Tiredness (13%)

 

1-10%

Hypotension (10%)

Bradycardia (8%)

Cold extremities (0.5- 7%)

Postural hypotension (2-4%)

Depression (3%)

Nausea (2-3%)

Dreaming (2%)

Drowsiness (2%)

Diarrhea (1-2%)

Fatigue (1-2%)

Leg pain (1-2%)

Lethargy (1-2%)

Lightheadedness (1-2%)

Vertigo (1-2%)

Dyspnea (0.4-2%)

2°/3° atrioventricular (AV) block (1%)

 

Frequency not defined

Hypotension, severe congestive heart failure (CHF), sick sinus syndrome

Catatonia, disorientation, emotional lability, hallucinations, headache, impaired performance on neuropsychometric tests, psychoses, short-term memory impairment

Purpura, rashes

Nausea

Thrombocytopenia

Elevated serum hepatic enzymes and bilirubin

Impotence, Peyronie disease

Antinuclear antibodies (ANA), lupus syndrome

Visual disturbances, xerophthalmia

Raynaud phenomenon

 

Warnings

Black box warnings

Ischemic heart disease may be exacerbated after abrupt withdrawaL

Hypersensitivity to catecholamines has been observed during withdrawaL

Exacerbation of angina and, in some cases, MI may occur after abrupt discontinuance

When long-term beta blocker therapy (particularly with ischemic heart disease) is discontinued, dosage should be gradually reduced over 1-2 weeks with careful monitoring

If angina worsens markedly or acute coronary insufficiency develops, beta-blocker administration should be promptly reinitiated, at least temporarily (in addition to other measures appropriate for unstable angina)

Patients should be warned against interruption or discontinuance of beta-blocker therapy without physician advice

Because coronary artery disease (CAD) is common and may be unrecognized, beta-blocker therapy must be discontinued slowly, even in patients treated only for hypertension

 

Contraindications

2°/3° heart block in patients without pacemaker

Cardiogenic shock

Sinus bradycardia

Sinus node dysfunction

Hypersensitivity

Uncompensated cardiac failure

Pulmonary edema

 

Cautions

Use with caution in anesthesia or surgery (myocardial depression), bronchospastic disease, cerebrovascular insufficiency, diabetes mellitus, hyperthyroidism or thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease, compromised left ventricular function, advanced age, heart failure

May mask effects of hyperthyroidism

Risk of hypoglycemia and bradycardia in neonates born to mothers who receive the drug at parturition or while breastfeeding, especially in premature infants and those with renal impairment

Use with caution in patients taking calcium-channel blockers or cardiac glycosides or using inhaled anesthetics

Avoid abrupt withdrawal; sudden discontinuance can exacerbate angina and lead to MI

Increased risk of stroke after surgery

In patients receiving clonidine, atenolol should be discontinued several days before withdrawal of clonidine

May cause or exacerbate CNS depression (use with caution in patients with psychiatric illness)

Use in pheochromocytoma (alpha blockade required before use of beta blocker)

Consider preexisting conditions such as sick sinus syndrome before initiating therapy

May potentiate hypoglycemia and may mask its signs and symptoms in patients with diabetes mellitus; use caution

Monitor for worsening of heart failure symptoms in patients with compensated heart failure

Use caution in patients with myasthenia gravis; may precipitate or aggravate symptoms or arterial insufficiency in patients with Raynaut's disease and peripheral vascular disease; use caution and monitor for progression of arterial obstruction

Avoid beta-blockers without alpha1-adrenergic receptor blocking activity in patients with Prinzmetal variant angina; unopposed alpha1-adrenergic receptors mediate coronary vasoconstriction and can worsen anginal symptoms

Exacerbation or induction of psoriasis reported with beta-blocker use; cause and effect not established

 

Pregnancy and lactation

Pregnancy category: d

Lactation: Drug enters breast milk; neonates born to mothers who are receiving atenolol at parturition or breastfeeding may be at risk for hypoglycemia and bradycardia; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Tenormin (atenolol)

Mechanism of action

Blocks response to beta-adrenergic stimulation; cardioselective for beta1 receptors at low doses, with little or no effect on beta2 receptors

 

Absorption

Bioavailability: 46-60%

Onset: Antihypertensive response, 3 hr

Duration: 12-24 hr (normal renal function)

Peak plasma time: 2-4 hr

 

Distribution

Protein bound: 6-16%

Vd: 50-75 L/kg

 

Metabolism

Metabolized to limited extent in liver

Metabolites: No clinically active metabolites

 

Elimination

Half-life: Children, 4.6 hr; adults, 6-7 hr; neonates, <35 hr; end-stage renal disease, 15-35 hr

Dialyzable: Yes (HD)

Excretion: Feces (50%), urine (40-50%)

 

Administration

IV Incompatibilities

Y-site: Amphotericin B cholesteryl sulfate

 

IV Compatibilities

Y-site: Meperidine, meropenem, morphine sulfate

 

IV Administration

Administer by slow IV infusion at 1 mg/min, either directly undiluted or diluted with D5W or Ns

 

Storage

Store intact ampoules at room temperature

Protect from light

Admixture in dextrose and NaCl-containing solution is stable for 48 hours