timolol maleate


timolol maleate

Apo-Timol, Betim (UK), Betimol, Dom-Timolol, Gen-Timolol, Istalol, Novo-Timol, NU-Timolol, PMS-Timolol, Rhoxal-Timolol, Sandoz Timolol, Timoptic, Timoptix-XE

Pharmacologic class: Beta-adrenergic blocker (nonselective)

Therapeutic class: Antihypertensive, vascular headache suppressant, antiglaucoma agent

Pregnancy risk category C

FDA Box Warning

Exacerbations of angina pectoris and myocardial infarction (MI) may follow abrupt withdrawal of some beta blockers. When discontinuing long-term therapy, particularly in patients with ischemic heart disease, reduce dosage gradually over 1 to 2 weeks and monitor patient carefully. If angina worsens markedly or acute coronary insufficiency develops, reinstate drug promptly (at least temporarily) and take other appropriate measures to manage unstable angina. Caution patient not to interrupt or discontinue therapy without prescriber's advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue drug abruptly even in patients treated only for hypertension.

Action

Blocks stimulation of beta1-adrenergic (myocardial) and beta2-adrenergic (pulmonary, vascular, uterine) receptor sites. May reduce aqueous production, which decreases intraocular pressure (IOP).

Availability

Ophthalmic gel: 0.25%, 0.5%

Ophthalmic solution: 0.25%, 0.5%

Tablets: 5 mg, 10 mg, 20 mg

Indications and dosages

➣ Hypertension

Adults: Initially, 10 mg P.O. b.i.d., given alone or with a diuretic; may increase at 7-day intervals as needed. Usual maintenance dosage is 10 to 20 mg daily in two divided doses, up to 60 mg/day.

➣ Acute MI

Adults: 10 mg P.O. b.i.d. starting 1 to 4 weeks after MI

➣ To prevent vascular headaches

Adults: Initially, 10 mg P.O. b.i.d. For maintenance, 20 mg may be given as a single daily dose. Total daily dosage may be increased to a maximum of 30 mg in divided doses or decreased to 10 mg/day, depending on response and tolerance. Withdraw drug if satisfactory response doesn't occur after 6 to 8 weeks at maximum dosage.

➣ Elevated IOP in patients with ocular hypertension or open-angle glaucoma

Adults: One drop of 0.25% to 0.5% ophthalmic solution in affected eye b.i.d., or 0.25% to 0.5% ophthalmic gel in affected eye once daily

Off-label uses

• Angina pectoris

• Supraventricular arrhythmias

Contraindications

• Hypersensitivity to drug or other beta-adrenergic blockers

• Uncompensated heart failure

• Bradycardia or heart block

• Cardiogenic shock

• Bronchial asthma (current or previous), severe chronic obstructive pulmonary disease

Precautions

Use cautiously in:

• renal or hepatic impairment, diabetes mellitus, thyrotoxicosis

• elderly patients

• pregnant or breastfeeding patients

• children (safety not established).

Administration

• Measure apical pulse before giving. If patient has significant bradycardia or tachycardia, withhold dose and consult prescriber.

Adverse reactions

CNS: fatigue, dizziness, asthenia, insomnia, headache, vertigo, nervousness, depression, paresthesia, hallucinations, memory loss, disorientation, emotional lability, clouded sensorium

CV: hypotension, angina pectoris exacerbation, bradycardia, atrioventricular or sinoatrial block, arrhythmias, heart failure

EENT: visual disturbances, dry eyes, tinnitus, nasal congestion

GI: nausea, constipation, diarrhea, abdominal discomfort

GU: erectile dysfunction, decreased libido

Metabolic: hyperuricemia, hypoglycemia, hyperkalemia

Musculoskeletal: joint pain

Respiratory: dyspnea, crackles, bronchospasm, pulmonary edema

Skin: itching, rash

Interactions

Drug-drug. Antihypertensives, nitrates: additive hypotension

Insulin, oral hypoglycemics: altered efficacy of these drugs

Nonsteroidal anti-inflammatory drugs: decreased antihypertensive effect of timolol

Quinidine: inhibited timolol metabolism, leading to increased beta-adrenergic blockade and bradycardia

Reserpine: increased risk of hypotension and bradycardia

Theophylline: reduced effects of both drugs

Drug-diagnostic tests. Antinuclear antibodies: increased titer

Blood urea nitrogen, liver function tests, potassium, uric acid: increased values

Glucose, high-density lipoproteins, hematocrit, hemoglobin: decreased values

Drug-herbs. Ephedra (ma huang), St. John's wort, yohimbine: decreased timolol efficacy

Patient monitoring

• Closely monitor vital signs, blood pressure, cardiovascular status, and ECG.

• Assess respiratory status. Check breath sounds for wheezing and bronchospasm.

• Monitor blood glucose level in patient with diabetes mellitus.

Patient teaching

• Teach patient how to measure pulse before each dose. Instruct him to contact prescriber if pulse is outside established safe range.

Caution patient not to stop taking drug abruptly. Dosage must be tapered.

• Teach patient how to administer eye drops. Instruct him to use drops only as prescribed, because they are absorbed systemically. Caution him not to touch dropper tip to eye or any other surface.

Teach patient to recognize and immediately report significant adverse respiratory, cardiac, and neurologic reactions.

• Inform patient that many over-the-counter drugs and herbs may decrease the efficacy of timolol. Advise him to consult prescriber before using these products.

• Advise diabetic patient that drug may lower blood glucose level. Encourage regular blood glucose monitoring.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

timolol maleate

Cardiology An antihypertensive and antiarrhythmic β-blocker, used to treat glaucoma Adverse effects Worsening of lipid profiles–↑ TGs, ↑ LDL, ↓ HDL. See β-blocker.

adrenergic receptors 

Receptors which are stimulated by the catecholamines adrenaline (epinephrine) and noradrenaline (norepinephrine). These receptors belong to a family of G protein coupled receptors and are found in the central nervous system and many tissues innervated by the peripheral nervous system. There are two types of adrenergic receptors: (1) α-receptors, which are mainly excitatory to smooth muscles and gland cells but cause relaxation of intestinal smooth muscles; (2) β-receptors of which there are (at least) two types, β1 and β2. Generally, stimulation of β-receptors produces an inhibitory response, although in some cases the effect is excitatory (e.g. in the heart). Example: the dilator pupillae muscle contains mainly α-adrenergic receptors and stimulation (e.g. with adrenaline) produces mydriasis. On the other hand, there are drugs that block the effect of catecholamines on α- or β-adrenergic receptors and are called α- or β-blockers (or sympatholytic drugs or adrenergic receptor agonists). Example: the ciliary epithelium contains mainly β-receptors and a β-blocker such as timolol inhibits the secretion of aqueous humour, thus reducing intraocular pressure. Syn. adrenoceptor. See alpha-adrenergic agonists; alpha-adrenergic antagonists; beta-blocker; miotics; mydriatic; sympatholytic drugs; sympathomimetic drugs; autonomic nervous system.

beta-blocker 

A drug that blocks or reduces the action of neurotransmitters on beta-adrenergic receptors. It reduces secretion of aqueous humour and consequently intraocular pressure and it is used in the treatment of glaucoma. Common beta-blockers include timolol maleate, betaxolol hydrochloride, carteolol hydrochloride, levobunolol hydrochloride and metipranolol. Timolol is often used together with another agent (combination drugs), e.g. timolol and brimonidine, timolol and dorzolamide, timolol and latanoprost. Syn. beta-adrenergic antagonist; beta-adrenergic blocking agent. See adrenergic receptors; miotics; sympatholytic drugs.