brimonidine and timolol

medtigo

brimonidine and timolol

Brand Name :

Combigan

Synonyms :

brimonidine and timolol

Class :

Antiglaucoma

Action and Spectrum

Mechanism of action

brimonidine is an alpha-2 adrenergic receptor agonist. It works by decreasing the production of aqueous humor in the eye and increasing the outflow of fluid from the eye, which helps to lower IOP. The drug also has a mild vasoconstrictive effect that helps to reduce the size of blood vessels in the eye, further decreasing IOP

timolol is a non-selective beta-blocker that works by reducing the production of aqueous humor in the eye and decreasing the inflow of blood into the eye. This also helps to lower IOP

Spectrum

Both brimonidine and timolol have a broad spectrum of activity, effectively treating a wide range of patients with elevated IOP. However, they may not be effective in all patients, and the IOP-lowering effect can vary from person to person. Additionally, both drugs can cause side effects, such as burning or stinging of the eyes, redness of the eyes, dry mouth, and drowsiness

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined:

5-15%

conjunctival folliculosis

eye pruritis

stinging

allergic conjunctivitis

conjunctival hyperemia

ocular burning

1-5%

blepharitis

depression

eye discharge

eye irritation

eyelid edema

foreign body sensation

hypertension

somnolence

visual disturbance

asthenia

corneal erosion

epiphora

eye dryness

eye pain

eyelid erythema

eyelid pruritis

headache

oral dryness

Black Box Warning

Contraindication / Caution

Contraindications

Contraindications of brimonidine:

Allergic reactions to brimonidine or any of its components
Severe cardiovascular diseases, such as heart failure or unstable angina
Raynaud’s syndrome
Bradycardia (a slow heart rate)
Patients with severe renal or hepatic impairment
Patients who have taken a monoamine oxidase inhibitor (MAOI) in the last two weeks

Contraindications of timolol:

Allergic reactions to timolol or any of its components
Severe bronchial asthma or chronic obstructive pulmonary disease (COPD)
Severe sinus bradycardia (a slow heart rate) or heart block
Cardiogenic shock (a life-threatening condition in which the heart is unable to pump enough blood to meet the body’s needs)
Severely impaired liver function
History of psoriasis

Caution

Drowsiness: It can cause drowsiness, fatigue, and dizziness, especially when first starting treatment. This can impair your ability to perform tasks that require alertness, such as driving or operating heavy machinery.
Dry mouth: It can cause dry mouth, leading to tooth decay and gum disease if not managed properly.
Low blood pressure: It can cause a drop in blood pressure, which can cause symptoms such as dizziness, lightheadedness, and fainting.
Bronchoconstriction: It can worsen bronchoconstriction (narrowing of the airways) in patients with asthma or COPD.
Heart rate and blood pressure: It can slow down your heart rate and lower your blood pressure, which can be dangerous if you already have a slow heart rate or low blood pressure

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

brimonidine and timolol are medications used in the treatment of Glaucoma and other conditions that increase intraocular pressure. brimonidine is an alpha-2 adrenergic agonist that works by reducing aqueous humor production and increasing uveoscleral outflow, which helps to lower intraocular pressure. timolol is a non-selective beta-adrenergic blocker that works by reducing aqueous humor production and improving outflow, which helps to lower intraocular pressure

Pharmacodynamics

Activation of alpha-2 adrenergic receptors by brimonidine led to decreased aqueous humor production and increased uveoscleral outflow, which helps to lower intraocular pressure. brimonidine also has vasoconstrictive effects, which help to reduce the risk of hypotension (low blood pressure) and improve blood flow to the optic nerve

Blocking beta-adrenergic receptors by timolol leads to decreased aqueous humor production and improved outflow, which helps to lower intraocular pressure. timolol also has vasodilatory effects, which help to reduce the risk of adverse cardiovascular effects

Pharmacokinetics

Absorption

brimonidine is rapidly absorbed after topical ocular administration, reaching peak concentrations within 2-4 hours. timolol is rapidly absorbed after oral or topical ocular administration, with peak concentrations reached within 2-4 hours.

Distribution

brimonidine is widely distributed in the body, but only small amounts are found in the bloodstream. timolol is widely distributed in the body, with high concentrations found in the heart and lungs.

Metabolism

brimonidine is metabolized in the liver, primarily by cytochrome P450 3A4 (CYP3A4) enzymes. timolol is metabolized in the liver, primarily by cytochrome P450 2D6 (CYP2D6) enzymes.

Elimination/Excretion

brimonidine is excreted primarily in the urine, with a half-life of approximately 2 hours. timolol is excreted primarily in the urine, with a half-life of approximately 6-10 hours

Adminstartion

Administration

It is administered topically to the eye. The eye drops are instilled in the affected eye(s) one to two times a day, as directed by your doctor. The topical gel is applied to the affected eye(s) once daily, as directed by your doctor

Patient Information Leaflet

Patient information leaflet

Generic Name: brimonidine and timolol

Why do we use brimonidine and timolol?

Ophthalmic brimonidine and timolol is used to treat ocular hypertension or open-angle Glaucoma (high pressure inside the eye)

brimonidine and timolol

No data available for drug.

DRUG INTERACTION

brimonidine and timolol

&

brimonidine and timolol +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

brimonidine and timolol

No data available for drug.

DRUG INTERACTION

brimonidine and timolol

&

brimonidine and timolol +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

brimonidine and timolol

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet

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