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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Medication Safety Issues
Sound-alike/look-alike issues:
Timolol may be confused with atenolol, Tylenol®
Timoptic® may be confused with Betoptic® S, Talacen®, Viroptic®
Bottle cap color change:
Timoptic®: Both the 0.25% and 0.5% strengths are now packaged in bottles with yellow caps; previously, the color of the cap on the product corresponded to different strengths.
International issues:
Betimol® may be confused with Betanol® which is a brand name for metipranolol in Monaco
Pronunciation
(TIM oh lol)
U.S. Brand Names
Index Terms
Generic Available
Yes: Excludes hemihydrate ophthalmic solutions. gel-forming ophthalmic solutions, and preservative free maleate ophthalmic solutions
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Ophthalmic: Treatment of elevated intraocular pressure such as glaucoma or ocular hypertension
Oral: Treatment of hypertension and angina; to reduce mortality following myocardial infarction; prophylaxis of migraine
Pregnancy Risk Factor
C (manufacturer); D (2nd and 3rd trimesters - expert analysis)
Pregnancy Considerations
Timolol was shown to cross the placenta in an in vitro perfusion study. Beta-blockers have been associated with bradycardia, hypotension, hypoglycemia, and intrauterine growth rate (IUGR); IUGR is probably related to maternal hypertension. Available evidence suggests beta-blockers are generally safe during pregnancy (JNC 7). Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding. Bradycardia and arrhythmia have been reported in an infant following ophthalmic administration of timolol during pregnancy.
Lactation
Enters breast milk/use caution (AAP rates “compatible”)
Breast-Feeding Considerations
Timolol is excreted in breast milk following oral and ophthalmic administration, and is considered compatible by the AAP. It is recommended that the infant be monitored for signs or symptoms of beta-blockade (hypotension, bradycardia, etc) with long-term use.
Contraindications
Hypersensitivity to timolol or any component of the formulation; sinus bradycardia; sinus node dysfunction; heart block greater than first degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; uncompensated cardiac failure; bronchospastic disease; pregnancy (2nd and 3rd trimesters)
Warnings/Precautions
Boxed warnings:
• Abrupt withdrawal: See “Other warnings/precautions” below.
Concerns related to adverse events:
• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.
Disease-related concerns:
• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring.
• Conduction abnormality: Consider pre-existing conditions such as sick sinus syndrome before initiating.
• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.
• Heart failure: Use with caution in patients with compensated heart failure and monitor for a worsening of the condition.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis; can worsen.
• Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's).
• Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker.
• Psoriasis: Beta-blocker use has been associated with induction or exacerbation of psoriasis, but cause and effect have not been firmly established.
• Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.
• Renal impairment: Use with caution in patients with severe renal impairment; marked hypotension can occur in patients maintained on hemodialysis.
Concurrent drug therapy issues:
• Anesthetic agents: Use with caution in patients receiving anesthetic agents which decrease myocardial function.
• Calcium channel blockers: Use with caution in patients on concurrent verapamil or diltiazem; bradycardia or heart block can occur.
Special populations:
• Contact lens wearers: Some product do contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.
Dosage form specific issues:
• Ophthalmic: Systemic absorption and adverse effects may occur, including bradycardia and/or hypotension. Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Multidose vials have been associated with development of bacterial keratitis; avoid contamination.
Other warnings/precautions:
• Abrupt withdrawal: [U.S. Boxed Warning]: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia.
Adverse Reactions
Ophthalmic:
>10%: Ocular: Burning, stinging
1% to 10%:
Cardiovascular: Hypertension
Central nervous system: Headache
Ocular: Blepharitis, blurred vision, cataract, conjunctival injection, conjunctivitis, foreign body sensation, hyperemia, itching, tearing, visual acuity decreased
Miscellaneous: Infection
Systemic:
1% to 10%:
Cardiovascular: Bradycardia
Central nervous system: Fatigue, dizziness
Respiratory: Dyspnea
Frequency not defined (reported with any dosage form):
Cardiovascular: Angina pectoris, arrhythmia, bradycardia, cardiac arrest, cardiac failure, cerebral ischemia, cerebral vascular accident, edema, heart block, hypotension, palpitation, Raynaud's phenomenon
Central nervous system: Anxiety, confusion, depression, disorientation, dizziness, hallucinations, insomnia, memory loss, nervousness, nightmares, somnolence
Dermatologic: Alopecia, angioedema, pseudopemphigoid, psoriasiform rash, psoriasis exacerbation, rash, urticaria
Endocrine & metabolic: Hypoglycemia masked, libido decreased
Gastrointestinal: Anorexia, diarrhea, dyspepsia, nausea, xerostomia
Genitourinary: Impotence, retoperitoneal fibrosis
Hematologic: Claudication
Neuromuscular & skeletal: Myasthenia gravis exacerbation, paresthesia
Ocular: Corneal sensitivity decreased, cystoid macular edema, diplopia, dry eyes, keratitis, ocular discharge, ocular pain, ptosis, refractive changes, visual disturbances
Otic: Tinnitus
Respiratory: Bronchospasm, cough, dyspnea, nasal congestion, pulmonary edema, respiratory failure
Miscellaneous: Allergic reactions, cold hands/feet, Peyronie's disease, systemic lupus erythematosus
Metabolism/Transport Effects
Substrate of CYP2D6 (major); Inhibits CYP2D6 (weak)
Drug Interactions
Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Alpha-/Beta-Agonists (Direct-Acting): Beta-Blockers may enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Epinephrine used as a local anesthetic for dental procedures will not likely cause clinically relevant problems. Management: Cardioselective beta-blockers and lower doses of epinephrine may confer a more limited risk. Patients who may require acute subcutaneous epinephrine (e.g., bee sting kits) should probably avoid beta blockers. Exceptions: Dipivefrin. Risk D: Consider therapy modification
Alpha1-Blockers: Beta-Blockers may enhance the orthostatic effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Risk D: Consider therapy modification
Alpha2-Agonists: Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the alpha2-agonist is abruptly withdrawn. Exceptions: Apraclonidine; Brimonidine. Risk D: Consider therapy modification
Amifostine: Antihypertensives may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, antihypertensive medications should be withheld for 24 hours prior to amifostine administration. If antihypertensive therapy can not be withheld, amifostine should not be administered. Risk D: Consider therapy modification
Aminoquinolines (Antimalarial): May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Amiodarone: May enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers. Risk C: Monitor therapy
Anilidopiperidine Opioids: May enhance the bradycardic effect of Beta-Blockers. Anilidopiperidine Opioids may enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy
Antihypertensives: May enhance the hypotensive effect of other Antihypertensives. Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Beta-Blockers. Beta-Blockers may decrease the metabolism of Antipsychotic Agents (Phenothiazines). Antipsychotic Agents (Phenothiazines) may decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Barbiturates: May decrease the serum concentration of Beta-Blockers. Risk C: Monitor therapy
Beta2-Agonists: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Beta2-Agonists. Risk D: Consider therapy modification
Calcium Channel Blockers (Nondihydropyridine): May enhance the hypotensive effect of Beta-Blockers. Bradycardia and signs of heart failure have also been reported. Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Beta-Blockers. Risk C: Monitor therapy
Cardiac Glycosides: Beta-Blockers may enhance the bradycardic effect of Cardiac Glycosides. Risk C: Monitor therapy
CYP2D6 Inhibitors (Moderate): May decrease the metabolism of CYP2D6 Substrates. Risk C: Monitor therapy
CYP2D6 Inhibitors (Strong): May decrease the metabolism of CYP2D6 Substrates. Risk D: Consider therapy modification
Darunavir: May increase the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Dipyridamole: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Disopyramide: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Dronedarone: May enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6. Management: Use lower initial beta-blocker doses; adequate tolerance of the combination, based on ECG findings, should be confirmed prior to any increase in beta-blocker dose. Risk D: Consider therapy modification
Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Hypotensive Agents: May enhance the adverse/toxic effect of other Hypotensive Agents. Risk C: Monitor therapy
Insulin: Beta-Blockers may enhance the hypoglycemic effect of Insulin. Risk C: Monitor therapy
Lidocaine: Beta-Blockers may decrease the metabolism of Lidocaine. Risk C: Monitor therapy
MAO Inhibitors: May enhance the orthostatic effect of Orthostasis Producing Agents. Risk C: Monitor therapy
Methacholine: Beta-Blockers may enhance the adverse/toxic effect of Methacholine. Risk X: Avoid combination
Methylphenidate: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Midodrine: Beta-Blockers may enhance the bradycardic effect of Midodrine. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Beta-Blockers. Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
Pentoxifylline: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Propafenone: May increase the serum concentration of Beta-Blockers. Propafenone possesses some independent beta blocking activity. Risk C: Monitor therapy
Propoxyphene: May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
QuiNIDine: May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Reserpine: May enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy
Rifamycin Derivatives: May decrease the serum concentration of Beta-Blockers. Exceptions: Rifabutin. Risk C: Monitor therapy
RiTUXimab: Antihypertensives may enhance the hypotensive effect of RiTUXimab. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Exceptions: Fluvoxamine. Risk C: Monitor therapy
Sulfonylureas: Beta-Blockers may enhance the hypoglycemic effect of Sulfonylureas. Cardioselective beta-blockers (eg, acebutolol, atenolol, metoprolol, and penbutolol) may be safer than nonselective beta-blockers. All beta-blockers appear to mask tachycardia as an initial symptom of hypoglycemia. Ophthalmic beta-blockers are probably associated with lower risk than systemic agents. Risk C: Monitor therapy
Theophylline Derivatives: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Theophylline Derivatives. Risk D: Consider therapy modification
Yohimbine: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Storage
Ophthalmic drops: Store at room temperature; do not freeze. Protect from light.
Timolol GFS: Store at 2°C to 25°C (36°F to 77°F). Protect from light.
Timoptic® in OcuDose®: Store in the protective foil wrap and use within 1 month after opening foil package.
Mechanism of Action
Blocks both beta1- and beta2-adrenergic receptors, reduces intraocular pressure by reducing aqueous humor production or possibly outflow; reduces blood pressure by blocking adrenergic receptors and decreasing sympathetic outflow, produces a negative chronotropic and inotropic activity through an unknown mechanism
Pharmacodynamics/Kinetics
Onset of action:
Hypotensive: Oral: 15-45 minutes
Peak effect: 0.5-2.5 hours
Intraocular pressure reduction: Ophthalmic: 30 minutes
Peak effect: 1-2 hours
Duration: ~4 hours; Ophthalmic: Intraocular: 24 hours
Absorption: Oral: Rapid and complete (~90%); Timolol is measurable in the serum following ophthalmic use
Distribution: Vd: 1.7 L/kg
Protein binding: 60%
Metabolism: Extensively hepatic; extensive first-pass effect
Bioavailability: 50%
Half-life elimination: 2-2.7 hours; prolonged with renal impairment
Time to peak, plasma: Oral: 1-2 hours
Excretion: Urine (15% to 20% as unchanged drug)
Dosage
Ophthalmic:
Children and Adults:
Solution: Initial: Instill 1 drop (0.25% solution) into affected eye(s) twice daily; increase to 0.5% solution if response not adequate; decrease to 1 drop/day if controlled; do not exceed 1 drop twice daily of 0.5% solution
Gel-forming solution (Timolol GFS, Timoptic-XE®): Instill 1 drop (either 0.25% or 0.5% solution) once daily
Adults: Solution (Istalol®): Instill 1 drop (0.5% solution) once daily in the morning
Oral: Adults:
Hypertension: Initial: 10 mg twice daily, increase gradually every 7 days, usual dosage: 20-40 mg/day in 2 divided doses; maximum: 60 mg/day
Prevention of myocardial infarction: 10 mg twice daily initiated within 1-4 weeks after infarction
Migraine headache: Initial: 10 mg twice daily, increase to maximum of 30 mg/day
Administration: Other
Ophthalmic: Administer other topically-applied ophthalmic medications at least 10 minutes before Timoptic-XE®; wash hands before use; invert closed bottle and shake once before use; remove cap carefully so that tip does not touch anything; hold bottle between thumb and index finger; use index finger of other hand to pull down the lower eyelid to form a pocket for the eye drop and tilt head back; place the dispenser tip close to the eye and gently squeeze the bottle to administer 1 drop; remove pressure after a single drop has been released; do not allow the dispenser tip to touch the eye; replace cap and store bottle in an upright position in a clean area; do not enlarge hole of dispenser; do not wash tip with water, soap, or any other cleaner. Some ophthalmic solutions contain benzalkonium chloride; wait at least 10 minutes after instilling solution before inserting soft contact lenses.
Monitoring Parameters
Blood pressure, apical and radial pulses, fluid I & O, daily weight, respirations, mental status, and circulation in extremities before and during therapy; monitor for systemic effect of beta-blockade even when administering ophthalmic product
Dietary Considerations
Oral product should be administered with food at the same time each day.
Patient Education
Oral: Take exact dose prescribed; do not increase, decrease, or discontinue dosage without consulting prescriber. Take at the same time each day. If you have diabetes, monitor serum glucose closely. May cause postural hypotension (use caution when rising from sitting or lying position or climbing stairs); dizziness, drowsiness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); decreased sexual ability (reversible); or nausea or vomiting (small frequent meals or frequent mouth care may help). Report swelling of extremities, respiratory difficulty, or new cough; weight gain (>3 lb/week); unresolved diarrhea or vomiting; or cold blue extremities. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
Ophthalmic: For ophthalmic use only. Apply prescribed amount as often as directed. Wash hands before using. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). Tilt head back and look upward. Gently pull down lower lid and put drop(s) inside lower eyelid at inner corner. Close eye and roll eyeball in all directions. Do not blink for 1/2 minute. Apply gentle pressure to inner corner of eye for 30 seconds. Wipe away excess from skin around eye. Do not use any other eye preparation for at least 10 minutes. Do not share medication with anyone else. Temporary stinging or blurred vision may occur. If using Istalol®, remove contact lenses prior to administration. Lenses may be reinserted 15 minutes following administration. Immediately report any adverse cardiac or CNS effects (usually signifies overdose). Report persistent eye pain, redness, burning, watering, dryness, double vision, puffiness around eye, vision changes, other adverse eye response, worsening of condition or lack of improvement.
Geriatric Considerations
Since bioavailability increased in about twofold in elderly patients, geriatrics may require lower maintenance doses. Also, as serum and tissue concentrations increase beta1 selectivity diminishes. Beta-adrenergic blockade may result in less hemodynamic response than seen in younger adults due to alterations in the beta-adrenergic autonomic system. Studies indicate that despite decreased sensitivity to the chronotropic effects of beta-blockade with age, there appears to be an increased myocardial sensitivity to the negative inotropic effect during stress (ie, exercise). Controlled trials have shown the overall response rate for propranolol to be only 20% to 50% in elderly populations. Therefore, all beta-adrenergic blocking drugs may result in a decreased response as compared to younger adults. Due to propranolol's CNS penetration and nonselective action, it may not be the beta-blocker of choice for use in elderly.
Anesthesia and Critical Care Concerns/Other Considerations
Surgery: Based on available evidence, beta-blockers should be started days to weeks before elective surgery in selected patients when possible and titrated to a heart rate <65 beats per minute. Additional data suggest that long acting beta-blockers may be superior to short acting ones (Redelmeier, 2005). The ACC/AHA 2007 guidelines update on perioperative cardiovascular evaluation and care for noncardiac surgery recommend beta-blockers be continued in patients undergoing surgery who are receiving beta-blockers to treat angina, symptomatic arrhythmias, hypertension, or other ACC/AHA Class I guideline indications (Class I recommendation). The guidelines also recommend that beta-blockers be given to patients undergoing vascular surgery who have myocardial ischemia demonstrated during preoperative testing (Class I recommendation).
The guidelines also state that beta-blockers are probably recommended in patients undergoing intermediate risk (eg, carotid endarterectomy, prostate surgery) or vascular surgery in whom preoperative assessment identifies coronary heart disease or high cardiac risk (Class IIa recommendation). High cardiac risk is defined as having >1 of the following clinical risk factors: History of ischemic heart disease, compensated or prior heart failure, cerebrovascular disease, diabetes mellitus, or renal insufficiency. The use of beta-blockers is uncertain in patients undergoing intermediate risk or vascular surgery with ?1 clinical risk factor (Class IIb recommendation).
The majority of published trials suggest a benefit of perioperative beta-blocker use during noncardiac surgery especially in high-risk patients; however, more recent clinical trials have not shown a benefit to perioperative beta-blockade for noncardiac surgery (Juul, 2006; Yang, 2006).
Cardiovascular Considerations
It is important to recognize that timolol eye drops may have systemic effects, particularly when patients are also on oral beta-blocker therapy or therapy with other negative chronotropic agents.
Atrial Fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.
Chronic Stable Angina: Beta-blockers are effective in the treatment of chronic stable angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.
Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. According to the 2003 JNC-VII guidelines for the treatment of hypertension, most patients with hypertension will require treatment with at least 2 antihypertensives. First-line therapy for hypertension is a diuretic (eg, hydrochlorothiazide or chlorthalidone). When a diuretic cannot be used or when a compelling indication exists for another drug, other types of antihypertensives may be used (eg, ACEIs, ARBs, beta-blockers, CCBs). Beta-blockers are among the multiple choices of agents that have shown benefit in a number of different patient subtypes. Compelling indications for a beta-blocker include patients with heart failure, postmyocardial infarction, high coronary disease risk, or diabetes. In type 2 diabetic patients, a UK Prospective Diabetes Study Group (UKPDS) trial showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.
Treatment should be targeted to a goal blood pressure of <140/90 mm Hg. If diabetes or renal disease coexists, the blood pressure goal should be <130/80 mm Hg.
ST-Segment Elevation Myocardial Infarction (STEMI): Beta-blockers, without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of STEMI and continued long-term. Oral beta-blockade should be initiated promptly in patients without contraindications (eg, signs of heart failure, evidence of a low output state, risk of cardiogenic shock, or other beta-blocker contraindications) (Class I recommendation). Use of intravenous beta-blockade may be considered and given promptly if the patient is experiencing concomitant hypertension or a tachyarrhythmia (Class IIa recommendation).
Unstable Angina/Non-ST-Segment Elevation MI (UA/NSTEMI): In the treatment of UA/NSTEMI, oral beta-blockade should be initiated within the first 24 hours in patients without contraindications (eg, signs of heart failure, evidence of a low output state, risk of cardiogenic shock, or other beta-blocker contraindications) (Class I recommendation). Use of intravenous beta-blockade should only be considered if the patient is experiencing concomitant hypertension upon presentation (Class IIa recommendation).
Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Timolol is a nonselective beta-blocker and may enhance the pressor response to epinephrine, resulting in hypertension and bradycardia. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
Epinephrine has interacted with nonselective beta-blockers such as propranolol to result in initial hypertensive episode followed by bradycardia. Timolol is also a nonselective beta-blocker. Timolol is available as an eye drop and oral dose form. When administered as an eye drop, the significance of a potential systemic interaction with epinephrine is unknown. However, it is suggested that cautionary procedures be used, particularly if vasoconstrictor is used immediately following an ophthalmic dose of timolol taken by the patient. If patients are taking the oral form of timolol, then the significance of a potential systemic interaction is well known and cautionary use of epinephrine is advised.
Mental Health: Effects on Mental Status
May cause dizziness or fatigue; may rarely cause anxiety, depression, or hallucinations
Mental Health: Effects on Psychiatric Treatment
Barbiturates and carbamazepine may decrease the effects of beta-blockers
Nursing: Physical Assessment/Monitoring
Assess other medications patient may be taking for effectiveness and interactions. Monitor therapeutic effectiveness (according to purpose of therapy) and adverse reactions at beginning of therapy and regularly with long-term therapy. Monitor blood pressure periodically. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Note: Unless otherwise specified, strength expressed as base.
Gel-forming solution, ophthalmic, as maleate:
Timolol GFS: 0.25% (2.5 mL [DSC], 5 mL); 0.5% (2.5 mL [DSC], 5 mL)
Timoptic-XE®: 0.25% (5 mL); 0.5% (5 mL)
Solution, ophthalmic, as hemihydrate:
Betimol®: 0.25% (5 mL, 10 mL [DSC], 15 mL [DSC]); 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]
Solution, ophthalmic, as maleate: 0.25% (5 mL, 10 mL, 15 mL); 0.5% (5 mL, 10 mL, 15 mL)
Istalol®: 0.5% (10 mL) [contains benzalkonium chloride and potassium sorbate]
Timoptic®: 0.25% (5 mL); 0.5% (5 mL, 10 mL) [contains benzalkonium chloride]
Solution, ophthalmic, as maleate [preservative free]:
Timoptic® in OcuDose®: 0.25% (0.2 mL); 0.5% (0.2 mL)
Tablet, as maleate: 5 mg, 10 mg, 20 mg [strength expressed as salt]
Pricing: U.S. (www.drugstore.com)
Solution (Betimol)
0.25% (5): $50.55
0.25% (15): $93.56
0.5% (5): $57.66
0.5% (10): $97.28
0.5% (15): $138.40
Solution (Istalol)
0.5% (5): $120.15
Solution (Timolol Maleate)
0.25% (5): $10.99
0.25% (10): $14.99
0.25% (15): $17.97
0.5% (5): $12.99
0.5% (10): $14.99
0.5% (15): $18.99
Solution (Timoptic)
0.25% (5): $43.06
0.5% (5): $44.99
0.5% (10): $44.99
Solution (Timoptic Ocudose)
0.25% (60): $193.97
0.5% (60): $233.98
Solution get-forming (Timolol Maleate)
0.25% (5): $59.71
0.5% (2.5): $46.74
0.5% (5): $55.99
Solution get-forming (Timoptic-XE)
0.25% (5): $65.37
0.5% (5): $70.55
Tablets (Timolol Maleate)
5 mg (60): $22.99
10 mg (60): $25.99
20 mg (60): $41.99
References
“American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
Anderson JL, Adams CD, Antman EM, et al, "ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non-ST-Elevation Myocardial Infarction: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Revise the 2002 Guidelines for the Management of Patients With Unstable Angina/Non-ST-Elevation Myocardial Infarction) Developed in Collaboration With the American College of Emergency Physicians, the Society for Cardiovascular Angiography and Interventions, and the Society of Thoracic Surgeons Endorsed by the American Association of Cardiovascular and Pulmonary Rehabilitation and the Society for Academic Emergency Medicine," J Am Coll Cardiol, 2007, 50(7):e1-e157.
Antman EM, Anbe DT, Armstrong PW, et al, "ACC/AHA Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee to Revise the 1999 Guidelines for the Management of Patients with Acute Myocardial Infarction)," Circulation, 2004, 110(9):e82-292.
Antman EM, Hand M, Armstrong PW, et al, “2007 Focused Update of the ACC/AHA 2004 Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction. A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines,” J Am Coll Cardiol, 2008, 51(2):210-49.
Brauchli YB, Jick SS, Curtin F, et al, “Association Between Beta-Blockers, Other Antihypertensive Drugs and Psoriasis: Population-Based Case-Control Study,” Br J Dermatol, 2008, 158(6):1299-307.
Chobanian AV, Bakris GL, Black HR, et al, “The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report,” JAMA, 2003, 289(19):2560-71.
Fleisher LA, Beckman JA, Brown KA, “2009 ACCF/AHA Focused Update on Perioperative Beta Blockade Incorporated Into the ACC/AHA 2007 Guidelines on Perioperative Cardiovascular Evaluation and Care for Noncardiac Surgery. A Report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines,” J Am Coll Cardiol, 2009 [epub ahead of print]
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