pharmacopeia
GET
/api/v1/drug/timolol
2D structure
(2S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
SMILES CC(C)(C)NC[C@@H](COC1=NSN=C1N2CCOCC2)O
InChIKey BLJRIMJGRPQVNF-JTQLQIEISA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Adrenergic beta1-Antagonists; Adrenergic beta2-Antagonists.

Indications

Sourced from openFDA
  • Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE may be used when a patient is sensitive to the preservative in Timolol Maleate Ophthalmic Solution, benzalkonium chloride, or when use of a preservative-free topical medication is advisable.ICD-10: H40.059, H40.9

Contraindications

Sourced from openFDA
  • Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is contraindicated in patients with (1) bronchial asthma; (2) a history of bronchial asthma; (3) severe chronic obstructive pulmonary disease (see WARNINGS ); (4) sinus bradycardia; (5) second or third degree atrioventricular block; (6) overt cardiac failure (see WARNINGS ); (7) cardiogenic shock; or (8) hypersensitivity to any component of this product.contraindicated

Dosage & administration

Sourced from openFDA

Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is a sterile solution that does not contain a preservative. The solution from one individual unit is to be used immediately after opening for administration to one or both eyes. Since sterility cannot be guaranteed after the individual unit is opened, the remaining contents should be discarded immediately after administration. Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is available in concentrations of 0.25 and 0.5%. The usual starting dose is one drop of 0.25% Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE in the affected eye(s) administered twice a day. Apply enough gentle pressure on the individual container to obtain a single drop of solution. If the clinical response is not adequate, the dosage may be changed to one drop of 0.5% solution in the affected eye(s) administered twice a day. Since in some patients the pressure-lowering response to Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE may require a few weeks to stabilize, evaluation should include a determination of intraocular pressure after approximately 4 weeks of treatment with Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE. If the intraocular pressure is maintained at satisfactory levels, the dosage schedule may be changed to one drop once a day in the affected eye(s). Because of diurnal variations in intraocular pressure, satisfactory response to the once-a-day dose is best determined by measuring the intraocular pressure at different times during the day.

Warnings & precautions

Sourced from openFDA

As with many topically applied ophthalmic drugs, this drug is absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported following systemic or ophthalmic administration of timolol maleate (see CONTRAINDICATIONS ). Cardiac Failure Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe failure. In Patients without a History of Cardiac Failure continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of cardiac failure, Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE should be discontinued. Obstructive Pulmonary Disease 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 Maleate Ophthalmic Solution in OCUDOSE is contraindicated [see CONTRAINDICATIONS ]) should, in general, not receive beta-blockers, including Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE.

Adverse reactions

Sourced from openFDA

The most frequently reported adverse experiences have been burning and stinging upon instillation (approximately one in eight patients). The following additional adverse experiences have been reported less frequently with ocular administration of this or other timolol maleate formulations: Body as a Whole Headache, asthenia/fatigue, and chest pain. Cardiovascular Bradycardia, arrhythmia, hypotension, hypertension, syncope, heart block, cerebral vascular accident, cerebral ischemia, cardiac failure, worsening of angina pectoris, palpitation, cardiac arrest, pulmonary edema, edema, claudication, Raynaud’s phenomenon, and cold hands and feet. Digestive Nausea, diarrhea, dyspepsia, anorexia, and dry mouth. Immunologic Systemic lupus erythematosus. Nervous System/Psychiatric Dizziness, increase in signs and symptoms of myasthenia gravis, paresthesia, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances including depression, confusion, hallucinations, anxiety, disorientation, nervousness, and memory loss. Skin Alopecia and psoriasiform rash or exacerbation of psoriasis. Hypersensitivity Signs and symptoms of systemic allergic reactions including anaphylaxis, angioedema, urticaria, and localized and generalized rash. Respiratory Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure, dyspnea, nasal congestion, cough and upper respiratory infections. Endocrine Masked symptoms of hypoglycemia in diabetic patients (see WARNINGS ).

Overdosage

Sourced from openFDA

There have been reports of inadvertent overdosage with Timolol Maleate Ophthalmic Solution resulting in systemic effects similar to those seen with systemic beta-adrenergic blocking agents such as dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest (see ADVERSE REACTIONS ). Overdosage has been reported with timolol maleate tablets. A 30-year-old female ingested 650 mg of timolol maleate tablets (maximum recommended oral daily dose is 60 mg) and experienced second and third degree heart block. She recovered without treatment but approximately two months later developed irregular heartbeat, hypertension, dizziness, tinnitus, faintness, increased pulse rate, and borderline first degree heart block. An in vitro hemodialysis study, using 14 C timolol added to human plasma or whole blood, showed that timolol was readily dialyzed from these fluids; however, a study of patients with renal failure showed that timolol did not dialyze readily.

Approval history

Sourced from openFDA
  • Aug 17, 1978NDANDA018086Bausch And Lomb Inc
  • Nov 5, 1986NDANDA019463Bausch And Lomb Inc
  • Nov 4, 1993NDANDA020330Bausch And Lomb Inc
  • Mar 31, 1995NDANDA020439Thea Pharma
  • Apr 7, 1998NDANDA020869Thea Pharma
  • Oct 21, 1998NDANDA020963Sandoz
  • Jun 4, 2004NDANDA021516Bausch And Lomb
  • Oct 30, 2007NDANDA021398Abbvie

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
35,566 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Treatment Failure3,99911%
  2. 2Drug Ineffective2,3536.6%
  3. 3Eye Irritation2,1085.9%
  4. 4Eye Pain1,7414.9%
  5. 5Ocular Hyperaemia1,6874.7%
  6. 6Fatigue1,6464.6%
  7. 7Vision Blurred1,2833.6%
  8. 8Dizziness1,2563.5%
  9. 9Off Label Use1,2323.5%
  10. 10Intraocular Pressure Increased1,2183.4%
  11. 11Diarrhoea1,1513.2%
  12. 12Dyspnoea1,0873.1%
  13. 13Headache1,0833.0%
  14. 14Nausea1,0813.0%
  15. 15Death1,0372.9%

Literature

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Recent PubMed references pinned to Timolol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 331 ClinicalTrials.gov registrations naming Timolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Timolol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • CYP2D6CPIC B/C (provisional)ClinPGx 3

Frequently asked questions

How does Timolol work?
Mechanism-of-action classes: Adrenergic beta1-Antagonists; Adrenergic beta2-Antagonists.
What is Timolol used for?
According to FDA labeling, Timolol carries indications including: Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE may be used when a patient is sensitive to the preservative in Timolol Maleate Ophthalmic Solution, benzalkonium chloride, or when use of a preservative-free topical medication is advisable.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Timolol?
Timolol is classified as Beta blocking agents, Beta blocking agents, non-selective, Adrenergic beta1-Antagonists, Adrenergic beta2-Antagonists, Decreased Blood Pressure, Decreased Intraocular Fluid Pressure, Negative Chronotropy, Negative Inotropy.
What are the brand names for Timolol?
Timolol is marketed under brand names including Betimol, Combigan, Cosopt, Istalol, Timoptic.
What are the contraindications for Timolol?
Timolol labeling lists contraindications including: Preservative-free Timolol Maleate Ophthalmic Solution in OCUDOSE is contraindicated in patients with (1) bronchial asthma; (2) a history of bronchial asthma; (3) severe chronic obstructive pulmonary disease (see WARNINGS ); (4) sinus bradycardia; (5) second or third degree atrioventricular block; (6) overt cardiac failure (see WARNINGS ); (7) cardiogenic shock; or (8) hypersensitivity to any component of this product.. Always consult the full prescribing information and a clinician.
Note. Data for timolol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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