Harman Patil (Editor)

Timolol

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Trade names
  
Betimol, others

MedlinePlus
  
a602022

AHFS/Drugs.com
  
Monograph

Timolol

Pregnancy category
  
AU: C US: C (Risk not ruled out)

Routes of administration
  
By mouth, topical (eye drop)

ATC code
  
C07AA06 (WHO) S01ED01 (WHO)

Timolol is a medication used either by mouth or as eye drops. As eye drops it is used to treat increased pressure inside the eye such as in ocular hypertension and glaucoma. By mouth it is used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines.

Contents

Common side effects with the drops is irritation of the eye. Common side effects by mouth include tiredness, slow heart beat, itchiness, and shortness of breath. Other side effects include masking the symptoms of low blood sugar in those with diabetes. Use is not recommended in those with asthma, heart failure, or COPD. It is unclear if use during pregnancy is safe for the baby. Timolol is in the non-selective Beta blocker family of medication.

Timolol was patented in 1968 and came into medical use in 1978. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Timolol is available as a generic medication. The wholesale cost in the developing world is about 0.86 to 2.29 USD per 5 ml bottle. In the United States it costs 25 to 50 USD per month.

By mouth

In its by mouth form, it is used:

  • to treat high blood pressure
  • to prevent heart attacks
  • to prevent migraine headaches
  • Eye drops

    In its eye drop form it is used to treat open-angle and, occasionally, secondary glaucoma. The mechanism of action of timolol is probably the reduction of the formation of aqueous humor in the ciliary body in the eye. It was the first β blocker approved for topical use in treatment of glaucoma in the USA (1978). When used by itself, it depresses intraocular pressure (IOP) 18–34% below baseline within first few treatments. However, there are short-term escape and long-term drift effects in some patients. That is, tolerance develops. It may reduce the extent of diurnal IOP curve up to 50%. IOP higher during sleep. It is 5–10× more potent β blocker than propranolol. Timolol is light-sensitive; it is usually preserved with 0.01% benzalkonium chloride (BAC), but also comes BAC-free. Can also be used in adjunctive therapy with pilocarpine or carbonic anhydrase inhibitors.

    A Cochrane Systematic Review compared the effect of timolol versus brimonidine in slowing the progression of open angle glaucoma in adult participants.

    Side effects

    The most serious possible side effects include cardiac arrhythmias and severe bronchospasms. Timolol can also lead to fainting, congestive heart failure, depression, confusion, worsening of Raynaud's syndrome and impotence.

    Side effects when given in the eye include: burning sensation, eye redness, superficial punctate keratopathy, corneal numbness.

    Formulations

    It is available in tablet and liquid formulations.

    For ophthalmic use, timolol is also available combined:

  • with carbonic anhydrase inhibitors:
  • timolol and brinzolamide
  • timolol and dorzolamide
  • with α2 agonists:
  • timolol and brimonidine
  • with prostaglandin analogs:
  • timolol and latanoprost
  • timolol and travoprost
  • Brand names

    Timolol is marketed under many trade names worldwide.

    References

    Timolol Wikipedia