timolol ophthalmic (Timoptic, Timoptic in Ocudose, Timoptic XE, Tim Ak, Betimol, Istalol)

Dosing and uses of Timoptic, Timoptic XE (timolol ophthalmic)

• Adult
• Pediatric

 

Adult dosage forms and strengths

ophthalmic solution

• 0.25%
• 0.5%

gel forming solution

• 0.25%
• 0.5%

 

Ocular Hypertension

1 gtt affected eye(s) q12hr 0.25%, if not effective increase 0.5% 1 gtt q12hr THEn

Decrease to 1 gtt/day if IOP controlled

XE formulation (0.25% or 0.5%): 1 gtt qDay

 

Pediatric dosage forms and strengths

Safety & efficacy not established

 

Timoptic, Timoptic XE (timolol ophthalmic) adverse (side) effects

>10%

Burning or stinging (38%)

 

>1%

Blurred vision (4-10%)

Cataract (4-10%)

Conjunctivitis (4-10%)

Decreased visual acuity (4-10%)

Headache (4-10%)

Hypertension (4-10%)

Infection (4-10%)

Itching (4-10%)

 

Frequency not defined

Ocular irritation

Blepharitis

Keratitis

Ocular pain

Discharge (e.g., crusting)

Foreign body sensation

Dry eyes

Eyelid erythema

Blepharoptosis

Decreased corneal sensitivity

Diplopia

Cystoid macular edema

Pseudopemphigoid

Choroidal detachment following filtration surgery

Epiphora

Photophobia

Conjunctival injection

Corneal fluorescein staining

Retinal vascular disorder

Ptosis

 

Warnings

Contraindications

Hypersensitivity to any component of this product; bronchial asthma; history of bronchial asthma; severe chronic obstructive pulmonary disease; sinus bradycardia; second or third degree atrioventricular block; overt cardiac failure; cardiogenic shock

 

Cautions

Observe patients receiving topical timolol and a systemic ß-adrenergic blocking agent concomitantly for potential additive effects on IOP and/or systemic effects of ß-adrenergic blockade

Severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, reported following systemic or ophthalmic administration of timolol maleate

Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition of beta-adrenergic receptor blockade may precipitate more severe failure

In Patients Without a history of cardiac failure continued depression of myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure; at first sign or symptom of cardiac failure, therapy should be discontinued

Patients with chronic obstructive pulmonary disease (e.g., chronic bronchitis, emphysema) of mild or moderate severity, bronchospastic disease, or a history of bronchospastic disease (other than bronchial asthma or a history of bronchial asthma, in which timolol is contraindicated) should, in general, not receive beta-blockers

Some authorities recommend gradual withdrawal of beta-adrenergic receptor blocking agents in patients undergoing elective surgery; if necessary during surgery, effects of beta-adrenergic blocking agents may be reversed by sufficient doses of adrenergic agonists

Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents; beta-adrenergic receptor blocking agents may mask signs and symptoms of acute hypoglycemia

Beta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism; patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents that might precipitate thyroid storm

Because of potential effects of beta-adrenergic blocking agents on blood pressure and pulse, these agents should be used with caution in patients with cerebrovascular insufficiency; if signs or symptoms suggesting reduced cerebral blood flow develop following initiation of therapy, alternative therapy should be considered

There have been reports of bacterial keratitis associated with use of multiple-dose containers of topical ophthalmic products; these containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of ocular epithelial surface

Choroidal detachment after filtration procedures has been reported with the administration of aqueous suppressant

In patients with angle-closure glaucoma, the immediate objective of treatment is to reopen the angle; this requires constricting the pupil; timolol maleate has little or no effect on the pupil; timolol should not be used alone in the treatment of angle-closure glaucoma

While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens; such patients may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions

Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness); timolol has been reported rarely to increase muscle weakness in some patients with myasthenia gravis or myasthenic symptoms

Remove contact lens prior to administration

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Secreted in breast milk; Mfr advises against breast feeding (AAP Committee states compatible with breast feeding)

 

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 Timoptic, Timoptic XE (timolol ophthalmic)

Mechanism of action

Nonselective beta-adrenergic receptor blocker; reduces IOP by reducing production of aqueous humor

 

Pharmacokinetics

Absorption: Minimal systemic absorption detected

Onset: 30 min

Peak effect: 1-2hr

Duration: <24 hr