metipranolol ophthalmic

Action and Spectrum

Actions and spectrum: 

metipranolol ophthalmic is a beta-adrenergic blocking agent used to lower intraocular pressure with ocular hypertension and open-angle glaucoma. It acts by reducing the production of aqueous humor in the eye, which helps to reduce the pressure inside the eye. 

metipranolol ophthalmic is a non-selective beta blocker, it blocks both beta-1 and beta-2 adrenergic receptors. By blocking these receptors, it reduces the activity of the sympathetic nervous system, which normally stimulates the production of aqueous humor. This results in a reduction in intraocular pressure, which helps to prevent damage to the optic nerve and preserve vision in patients with glaucoma or ocular hypertension. 

The spectrum of activity of metipranolol ophthalmic is similar to other beta-blockers used in the treatment of glaucoma and ocular hypertension. It is most effective in reducing intraocular pressure in patients with open-angle glaucoma and mild-to-moderate ocular hypertension. 

metipranolol ophthalmic is typically administered as eye drops and is available in various strengths and formulations. The specific treatment plan and use of metipranolol ophthalmic may vary depending on individual circumstances and the severity of the condition. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Systemic 

• Reducing systemic adverse effects by placing a finger in the corner of the eye (occluding the punctum) or by gently shutting the eyelids for three minutes without opening and closing them 
• Similar side effects to those caused by systemic beta-blockers include bradycardia, worsening of congestive heart failure (CHF), asthma, nausea, nightmares, tiredness, cough, epistaxis, dyspnea, rhinitis, arthritis, myalgia, and rash 

Ocular 

• Blepharitis 
• Light intolerance 
• Tearing 
• Browache 
• Burning sensation in eye 
• Blurred vision 
• Uveitis 
• Eyelid dermatitis 

Black Box Warning

Black Box Warning: 

metipranolol ophthalmic does not have a black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: metipranolol ophthalmic is contraindicated in individuals with hypersensitivity or allergic reaction to metipranolol or any other component of the medication. Allergic reactions may include itching, rash, swelling, or difficulty breathing. 
• Asthma: metipranolol ophthalmic is contraindicated in individuals with bronchial asthma or severe chronic obstructive pulmonary disease. Beta-blockers, including metipranolol, can potentially worsen respiratory symptoms in these patients. 
• Sinus Bradycardia and Heart Block: metipranolol ophthalmic is contraindicated in individuals with sinus bradycardia (slow heart rate) or heart block (disruption of electrical signals in the heart) unless there is an artificial pacemaker in place. Beta-blockers can further decrease heart rate and worsen these conditions. 
• Cardiogenic Shock: metipranolol ophthalmic is contraindicated in individuals with cardiogenic shock. Beta-blockers can further impair cardiac function and worsen this condition.

Caution: 

• Respiratory Disorders: Patients with a history of mild to moderate chronic obstructive pulmonary disease (COPD) or bronchial asthma should use metipranolol ophthalmic with caution. Beta-blockers can potentially worsen respiratory symptoms in these individuals. Close monitoring of respiratory function is recommended. 
• Cardiovascular Disorders: metipranolol ophthalmic can affect cardiovascular function. Patients with certain cardiovascular conditions, such as congestive heart failure, heart block, bradycardia, or hypotension, should use metipranolol with caution. 
• Diabetes: metipranolol ophthalmic can mask some of the signs and symptoms of hypoglycemia in diabetic patients.  
• Surgical Procedures: If you are scheduled for any surgical procedure, including eye surgery, inform your healthcare provider that you are using metipranolol ophthalmic. Beta-blockers like metipranolol can interact with certain anesthetics and medications used during surgery, potentially affecting cardiovascular function. 
• Contact Lens Wearers: metipranolol ophthalmic contains benzalkonium chloride, which is absorbed by soft contact lenses. 

Comorbidities: 

• Respiratory Disorders: Patients with a history of chronic obstructive pulmonary disease or bronchial asthma may experience worsened respiratory symptoms due to the beta-blocking effects of metipranolol. Close monitoring of respiratory function is advised. 
• Cardiovascular Disorders: metipranolol can affect heart rate and blood pressure. Patients with pre-existing cardiovascular conditions like congestive heart failure, heart block, or bradycardia should use metipranolol with caution. 
• Diabetes: metipranolol may mask some signs of hypoglycemia in diabetic patients, making it more challenging to detect and manage low blood sugar levels.  
• Thyroid Disorders: metipranolol can potentially affect thyroid function. Patients with thyroid disorders should be closely monitored while using metipranolol. 
• Allergic Reactions: Patients with a history of allergic reactions to beta-blockers or other components of metipranolol ophthalmic should avoid its use. 
• Surgery: Prior to any surgical procedures, including eye surgery, inform your healthcare provider about your use of metipranolol ophthalmic. Beta-blockers can interact with certain anesthetics and medications used during surgery, potentially affecting cardiovascular function. 

Pregnancy / Lactation

Pregnancy consideration: Pregnancy Category C 

Lactation: it is unknown whether metipranolol ophthalmic is excreted in human breast milk  

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 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: 

metipranolol ophthalmic acts by reducing the production of aqueous humor in the eye, which helps to decrease intraocular pressure. metipranolol blocks both beta-1 and beta-2 adrenergic receptors, leading to a reduction in sympathetic nervous system activity. By blocking these receptors, it decreases the formation of aqueous humor and improves the outflow of fluid from the eye. The net result is a reduction in intraocular pressure and protection of the optic nerve from damage.  

Pharmacodynamics: 

• Beta-Adrenergic Blocking Activity: metipranolol is a non-selective beta-adrenergic blocking agent. It competitively blocks both beta-1 and beta-2 adrenergic receptors in the eye. 
• Reduction of Aqueous Humor Production: By blocking beta-2 adrenergic receptors in the ciliary body of the eye, metipranolol decreases the production of aqueous humor. This reduces the inflow of fluid into the eye and helps to lower intraocular pressure. 
• Improved Aqueous Humor Outflow: metipranolol also increases the outflow of aqueous humor through a trabecular meshwork, facilitating its drainage from the eye. This further contributes to the reduction of intraocular pressure. 
• Intraocular Pressure Reduction: The primary pharmacodynamic effect of metipranolol is the reduction of intraocular pressure.

Pharmacokinetics: 

Absorption 

When applied topically as eye drops, metipranolol is absorbed through the cornea and conjunctiva into the anterior chamber of the eye. It has limited systemic absorption, resulting in minimal plasma concentrations. 

Distribution 

metipranolol is distributed within the eye tissues, primarily targeting the ciliary body, where it exerts its pharmacological effects. Limited distribution outside the eye minimizes systemic side effects. 

Metabolism 

metipranolol undergoes extensive hepatic metabolism via enzymes such as cytochrome P450 (CYP) isoenzymes, primarily CYP2D6. The metabolites formed are inactive and do not contribute significantly to the drug’s therapeutic effects. 

Elimination and excretion 

The metabolites of metipranolol and a small fraction of the unchanged drug are excreted primarily in the urine. Renal excretion accounts for the elimination of metipranolol from the body. 

Adminstartion

Administration: 

• Wash your hands thoroughly before handling the eye drops.  
• Tilt your head and look up towards the ceiling.  
• Hold the dropper close to the eye, but without touching it.  
• Squeeze the prescribed no. of drops into the pocket formed by the lower eyelid. Usually, one to two drops are used in the affected eye(s).  
• Close eyes for a few seconds to allow the medication to spread evenly across the eye surface.  
• Avoid blinking or squeezing the eye while the drops are being instilled.  
• Replace the cap on the drop bottle and store it according to the manufacturer’s instructions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: metipranolol ophthalmic 

Pronounced: (meh-tee-PRAH-noh-lol off-THAL-mik)  

Why do we use metipranolol ophthalmic? 

metipranolol ophthalmic is a medication used for the treatment of certain eye conditions, such as glaucoma and ocular hypertension. metipranolol eye drops are commonly prescribed to lower intraocular pressure in individuals with open-angle glaucoma or ocular hypertension. metipranolol helps to lower elevated intraocular pressure, which is a risk factor for the development and progression of glaucoma.