timolol maleate

(tye moe' lole)

Apo-Timol (CAN), Betimol, Blocadren, Timoptic, Timoptic-XE

Pregnancy Category C

Drug classes
Beta-adrenergic blocker
Antihypertensive
Antiglaucoma drug

Therapeutic actions
Competitively blocks beta-adrenergic receptors in the heart and juxtaglomerular
apparatus, decreasing the influence of the sympathetic nervous system on these tissues
and decreasing the excitability of the heart, decreasing cardiac output and oxygen
consumption, decreasing the release of renin, and lowering BP; reduces IOP by
decreasing the production of aqueous humor and possibly by increasing aqueous humor
outflow.

Indications
• Hypertension, used alone or in combination with other antihypertensives,
especially thiazide-type diuretics
• Prevention of reinfarction in MI patients who are hemodynamically stable
• Prophylaxis of migraine
• Ophthalmic solution: Reduction of IOP in chronic open-angle glaucoma, some
patients with secondary glaucoma, aphakic patients with glaucoma ocular HTN

Contraindications and cautions

• Contraindicated with sinus bradycardia (HR < 45 beats/min), second- or third-
degree heart block (PR interval > 0.24 sec), cardiogenic shock, CHF, asthma,
COPD, pregnancy, lactation.
• Use cautiously with diabetes or thyrotoxicosis (timolol can mask the usual cardiac
signs of hypoglycemia and thyrotoxicosis).

Available forms
Tablets—5, 10, 20 mg; ophthalmic solution, gel—0.25%, 0.50%

Dosages
ADULTS
Oral
• Hypertension: Initially, 10 mg bid. Increase dosage at 1-wk intervals to a
maximum of 60 mg/day divided into 2 doses, as needed. Usual maintenance dose
is 20–40 mg/day.
• Prevention of reinfarction in MI (long-term prophylaxis in patients who survived
the acute phase): 10 mg bid PO.
 • Migraine: 10 mg PO bid; during maintenance, the 20 mg/day may be given as a
single dose. May be increased to a maximum of 30 mg/day in divided doses or
decreased to 10 mg/day. Discontinue if satisfactory response is not obtained after
6–8 wk.
Ophthalmic
Initially, 1 drop of 0.25% solution bid into the affected eye or eyes. Adjust dosage on
basis of response to 1 drop of 0.5% solution bid or 1 drop of 0.25% solution daily. When
replacing other agents, make change gradually and individualize dosage.
PEDIATRIC PATIENTS
Safety and efficacy not established.

Pharmacokinetics
Route Onset Peak
Oral Varies 1–2
hr
Ophthalmologic Rapid 1–5
hr
Metabolism: Hepatic; T1/2: 3–4 hr
Distribution: Crosses placenta; enters breast milk
Excretion: Urine

Adverse effects
Oral
• Allergic reactions: Pharyngitis, erythematous rash, fever, sore throat,
laryngospasm, respiratory distress
• CNS: Dizziness, vertigo, tinnitus, fatigue, emotional depression, paresthesias,
sleep disturbances, hallucinations, disorientation, memory loss, slurred speech
• CV: CHF, cardiac arrhythmias, sinoatrial or AV nodal block, peripheral vascular
insufficiency, claudication, CVA, pulmonary edema, hypotension
• Dermatologic: Rash, pruritus, sweating, dry skin
• EENT: Eye irritation, dry eyes, conjunctivitis, blurred vision
• GI: Gastric pain, flatulence, constipation, diarrhea, nausea, vomiting, anorexia,
ischemic colitis, renal and mesenteric arterial thrombosis, retroperitoneal fibrosis,
hepatomegaly, acute pancreatitis
• GU: Impotence, decreased libido, Peyronie's disease, dysuria, nocturia, frequent
urination
• Musculoskeletal: Joint pain, arthralgia, muscle cramp
• Respiratory: Bronchospasm, dyspnea, cough, bronchial obstruction, nasal
stuffiness, rhinitis, pharyngitis (less likely than with propranolol)
• Other: Decreased exercise tolerance, development of antinuclear antibodies
(ANA), hyperglycemia or hypoglycemia, elevated serum transaminase
Ophthalmic
• Local: Ocular irritation, decreased corneal sensitivity, visual refractive changes,
diplopia, ptosis

Interactions
Drug-drug
• Increased effects with verapamil
• Increased risk of orthostatic hypotension with prazosin
• Decreased antihypertensive effects with NSAIDs, clonidine
• Decreased elimination of theophyllines with resultant decrease in expected
actions of both drugs when taken concurrently
• Peripheral ischemia and possible gangrene with ergotamine, methysergide,
dihydroergotamine
• Increased risk of hypoglycemia and masked signs of hypoglycemia with insulin
• Hypertension followed by severe bradycardia with epinephrine
• All of the above may occur with ophthalmic timolol; in addition, additive effects
are possible with oral beta-blockers
Drug-lab test
• Possible false results with glucose or insulin tolerance tests (oral)

Nursing considerations
Assessment
• History: Sinus bradycardia, second- or third-degree heart block, cardiogenic
shock, CHF, asthma, COPD, pregnancy, lactation, diabetes or thyrotoxicosis
• Physical: Weight, skin condition, neurologic status, P, BP, ECG, respiratory
status, kidney and thyroid function, blood and urine glucose

Interventions
• Do not discontinue drug abruptly after long-term therapy (hypersensitivity to
catecholamines may have developed, causing exacerbation of angina, MI, and
ventricular arrhythmias). Taper drug gradually over 2 wk with monitoring.
• Consult with surgeon about withdrawal if patient is to undergo surgery
(withdrawal is controversial).

Teaching points
• Do not stop taking this drug unless instructed to do so by a health care provider.
• Avoid driving or dangerous activities if dizziness or shaking occurs.
• Report difficulty breathing, night cough, swelling of extremities, slow pulse,
confusion, depression, rash, fever, sore throat.
• If using ophthalmic form, administer eye drops properly to minimize systemic
absorption.

Adverse effects in Italic are most common; those in Bold are life-threatening.