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Timolol is a
beta blocker Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms ( arrhythmia), and to protect the heart from a second heart attack after a first heart attack ( secondary prevention ...
medication used either
by mouth Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administ ...
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 Hypertension, also known as high blood pressure, is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms itself. It is, however, a major ri ...
, chest pain due to insufficient blood flow to the heart, to prevent further complications after a
heart attack A myocardial infarction (MI), commonly known as a heart attack, occurs when Ischemia, blood flow decreases or stops in one of the coronary arteries of the heart, causing infarction (tissue death) to the heart muscle. The most common symptom ...
, and to prevent migraines. 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 Shortness of breath (SOB), known as dyspnea (in AmE) or dyspnoea (in BrE), is an uncomfortable feeling of not being able to breathe well enough. The American Thoracic Society defines it as "a subjective experience of breathing discomfort that con ...
. Other side effects include masking the symptoms of low blood sugar in those with
diabetes Diabetes mellitus, commonly known as diabetes, is a group of common endocrine diseases characterized by sustained high blood sugar levels. Diabetes is due to either the pancreas not producing enough of the hormone insulin, or the cells of th ...
. Use is not recommended in those with
asthma Asthma is a common long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wh ...
, uncompensated
heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome caused by an impairment in the heart's ability to Cardiac cycle, fill with and pump blood. Although symptoms vary based on which side of the heart is affected, HF ...
, or chronic obstructive pulmonary disease (COPD). It is unclear if use during pregnancy is safe for the fetus. Timolol is a non-selective beta blocker. Timolol was patented in 1968, and came into medical use in 1978. It is on the World Health Organization's List of Essential Medicines. Timolol is available as a generic medication. In 2022, it was the 155th most commonly prescribed medication in the United States, with more than 3million prescriptions.


Medical uses


By mouth

In its by mouth or oral form, it is used: * to treat
high blood pressure Hypertension, also known as high blood pressure, is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms itself. It is, however, a major ri ...
* to prevent
heart attack A myocardial infarction (MI), commonly known as a heart attack, occurs when Ischemia, blood flow decreases or stops in one of the coronary arteries of the heart, causing infarction (tissue death) to the heart muscle. The most common symptom ...
s * to prevent migraine headaches The combination of timolol and the
alpha-1 blocker Alpha-1 blockers (also called alpha-adrenergic blocking agents or alpha-1 antagonists) constitute a variety of drugs that block the effect of catecholamines on alpha-1 adrenergic receptors, alpha-1-adrenergic receptors. They are mainly used to tr ...
prazosin has
sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...
effects.


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
beta blocker Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms ( arrhythmia), and to protect the heart from a second heart attack after a first heart attack ( secondary prevention ...
approved for topical use in treatment of glaucoma in the United States (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 people. That is, tolerance develops. It may reduce the extent of the daytime IOP curve up to 50%. The IOP is higher during sleep. Efficacy of timolol in lowering IOP during the sleep period may be limited. It is a 5–10× more potent beta blocker than
propranolol Propranolol is a medication of the beta blocker class. It is used to treat hypertension, high blood pressure, some types of cardiac dysrhythmia, irregular heart rate, thyrotoxicosis, capillary hemangiomas, akathisia, performance anxiety, and ...
. Timolol is light-sensitive; it is usually preserved with 0.01% benzalkonium chloride (BAC), but also comes BAC-free. It can also be used in combination with pilocarpine, carbonic anhydrase inhibitors or prostaglandin analogs. A Cochrane review compared the effect of timolol versus brimonidine in slowing the progression of open angle glaucoma in adults but found insufficient evidence to come to conclusions.


On the skin

In its gel form it is used on the skin to treat infantile hemangiomas.


Contraindications

The medication should not be taken by individuals with: * An allergy to timolol or any other beta-blockers *
Asthma Asthma is a common long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wh ...
or severe chronic obstructive bronchitis * A slow heart rate (bradycardia), or a heart block *
Heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome caused by an impairment in the heart's ability to Cardiac cycle, fill with and pump blood. Although symptoms vary based on which side of the heart is affected, HF ...


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 Erectile dysfunction (ED), also referred to as impotence, is a form of sexual dysfunction in males characterized by the persistent or recurring inability to achieve or maintain a Human penis, penile erection with sufficient rigidity and durat ...
. 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 sold under many
brand name A brand is a name, term, design, symbol or any other feature that distinguishes one seller's goods or service from those of other sellers. Brands are used in business, marketing, and advertising for recognition and, importantly, to create and ...
s worldwide. Timolol eye drops are sold under the brand names Timoptic and Istalol among others.


References


External links

* {{Authority control 4-Morpholinyl compounds Beta blockers Ethers Ophthalmology drugs Secondary alcohols Thiadiazoles Wikipedia medicine articles ready to translate World Health Organization essential medicines