Drug Interactions
Specific Drugs
| Drug |
Interaction |
Comments |
| β-Adrenergic blocking agents |
Potential additive effect |
Adjust initial and subsequent atenolol dosage downward based on clinical findings (e.g., blood pressure, heart rate) |
| Anesthetics, general (myocardial depressant) |
Increased risk of hypotension and heart failure |
Use with caution (see Anesthesia and Major Surgery under Cautions) |
| Calcium-channel blockers (e.g., verapamil, diltiazem) |
Additive hypotensive effect; may be used to therapeutic advantage
Potential for bradycardia and heart block, increase in left ventricular end diastolic pressure |
Adjust dosage carefully
Patients with preexisting conduction abnormalities or left ventricular dysfunction particularly susceptible |
| Catecholamine-depleting drugs (e.g., reserpine) |
Potential for additive effects (increased hypotension and marked bradycardia) |
Monitor closely for symptoms (e.g., vertigo, syncope, postural hypotension) |
| Clonidine |
May exacerbate rebound hypertension following discontinuance of clonidine |
Discontinue atenolol therapy several days before clonidine discontinuance. If replacing clonidine, delay initiation of atenolol for several days after stopping clonidine |
| Hydralazine |
Additive hypotensive effect; may be used to therapeutic advantage |
Adjust dosage carefully |
| Methyldopa |
Additive or potentiated hypotensive effect; may be used to therapeutic advantage |
Adjust dosage carefully when used concurrently |
| NSAIAs (e.g., indomethacin, aspirin) |
Potential for decreased atenolol antihypertensive effect |
Studies indicate no clinically important interaction; concomitant administration appears safe and effective |
Pharmacokinetics
Absorption
Bioavailability
50–60% following oral administration.
Onset
1 hour following oral administration. Within 5 minutes following IV administration.
Duration
At least 24 hours following oral administration (antihypertensive and β-adrenergic blocking effects). About 12 hours following IV administration (effect on heart rate).
Special Populations
In geriatric patients, plasma concentrations are increased.
Distribution
Extent
Well distributed into most tissues and fluids except brain and CSF.
Readily crosses the placenta, has been detected in cord blood.
Distributed into milk in concentrations higher than those in serum.
Plasma Protein Binding
Approximately 6–16%.
Elimination
Metabolism
Little or no hepatic metabolism.
Elimination Route
40–50% excreted unchanged in urine following oral administration; remainder in feces, principally as unabsorbed drug.
Half-life
6–7 hours.
Special Populations
In patients with Clcr 15–35 mL/minute per 1.73 m2, plasma half-life is increased to 16–27 hours; in progressive renal impairment plasma half-life is >27 hours.
In geriatric patients, total clearance is decreased by about 50%, plasma half-life is prolonged.
Hemodialysis: 1–12% removed.
Stability
Storage
Oral
Tablets
Tight, light-resistant containers at 20–25°.
Tablets (Atenolol and Chlorthalidone)
Tight, light-resistant containers at 20–25°.
Parenteral
Injection
20–25°.
Protect from light.
Compatibility
Parenteral
Solution Compatibility
Manufacturer states that dilutions in dextrose injection, sodium chloride injection, or sodium chloride and dextrose injection are stable for 48 hours if not used immediately.
Drug Compatibility