Betaxolol

C07A - Beta blocking agents ATC S01ED02 Small molecule approved 1985 Oral Topical Natural product

JFDA label: Apixol eye drops

Indications

Approved

Cardiovascular Diseases — cardiovascular disease
Glaucoma — glaucoma

Off-label

Glaucoma, Open-Angle
Ocular Hypertension

Contraindications

Source: openFDA

Betaxolol tablets, USP is contraindicated in patients with known hypersensitivity to the drug. Betaxolol tablets, USP is contraindicated in patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure (see Warnings ). Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (7)

Very Common Bradycardia

Common Palpitations

Rare Arrhythmia · Atrioventricular block · Cardiac disorder · Cardiac failure · Tachycardia

Vascular disorders (1)

Rare Hypotension

Nervous system disorders (5)

Very Common Dizziness · Headache

Common Paraesthesia

Rare Loss of consciousness · Syncope

Immune system disorders (2)

Rare Hypersensitivity · Immune system disorder

Endocrine disorders (1)

Rare Hyperthyroidism

Metabolism and nutrition disorders (1)

Rare Hypoglycaemia

Gastrointestinal disorders (5)

Common Diarrhoea · Dyspepsia · Nausea

Rare Gastrointestinal disorder · Vomiting

Skin and subcutaneous tissue disorders (6)

Common Dermatitis · Rash

Rare Alopecia · Erythema of eyelid · Eye pruritus · Skin disorder

Musculoskeletal and connective tissue disorders (3)

Common Arthralgia · Musculoskeletal discomfort · Myalgia

Psychiatric disorders (11)

Common Abnormal dreams · Depression · Insomnia

Rare Anxiety · Confusional state · Hallucination · Libido decreased · Mental disorder · Nightmare · Photophobia · Sleep disorder

Eye disorders (17)

Rare Abnormal sensation in eye · Conjunctivitis · Dry eye · Endophthalmitis · Eye discharge · Eye disorder · Eye irritation · Eye pain · Eyelid margin crusting · Foreign body sensation in eyes · Lacrimation increased · Ocular discomfort · Ocular hyperaemia · Panophthalmitis · Vision blurred · Visual acuity reduced · Visual impairment

Reproductive system and breast disorders (2)

Common Erectile dysfunction

Rare Breast disorder

Infections and infestations (7)

Common Rhinitis · Upper respiratory tract infection

Rare Bronchitis · Infection · Influenza · Nasopharyngitis · Sinusitis

Investigations (1)

Rare Feeling abnormal

General disorders and administration site conditions (27)

Very Common Asthenia · Fatigue

Common Chest pain · Lethargy · Nervousness · Oedema · Peripheral coldness · Tension

Rare Angiopathy · Asthenopia · Blepharitis · Blepharospasm · Cataract · Conjunctival disorder · Conjunctival oedema · Disturbance in sexual arousal · Dysgeusia · Infestation · Intermittent claudication · Keratitis · Mediastinal disorder · Nervous system disorder · Periorbital oedema · Psychotic disorder · Punctate keratitis · Refraction disorder · Shock

Respiratory, thoracic and mediastinal disorders (5)

Common Dyspnoea

Rare Asthma · Bronchospasm · Cough · Rhinorrhoea

Dosing

Source: openFDA

The initial dose of betaxolol tablets, USP in hypertension is ordinarily 10 mg once daily either alone or added to diuretic therapy. The full antihypertensive effect is usually seen within 7 to 14 days. If the desired response is not achieved the dose can be doubled after 7 to 14 days. Increasing the dose beyond 20 mg has not been shown to produce a statistically significant additional antihypertensive effect; but the 40-mg dose has been studied and is well tolerated. An increased effect (reduction) on heart rate should be anticipated with increasing dosage. If monotherapy with betaxolol tablets, USP does not produce the desired response, the addition of a diuretic agent or other antihypertensive should be considered (see PRECAUTIONS, Drug Interactions ). Dosage Adjustments For Specific Patients: Patients with renal failure: In patients with renal impairment, clearance of betaxolol declines with decreasing renal function. In patients with severe renal impairment and those undergoing dialysis, the initial dose of betaxolol tablets, USP is 5 mg once daily. If the desired response is not achieved, dosage may be increased by 5 mg/day increments every 2 weeks to a maximum dose of 20 mg/day. Patients with hepatic disease: Patients with hepatic disease do not have significantly altered clearance. Dosage adjustments are not routinely needed. Elderly patients: Consideration should be given to reduction in the starting dose to 5 mg in elderly patients. These patients are especially prone to beta-blocker-induced bradycardia, which appears to be dose related and sometimes responds to reductions in dose. Cessation of therapy: If withdrawal of betaxolol tablets, USP therapy is planned, it should be achieved gradually over a period of about 2 weeks. Patients should be carefully observed and advised to limit physical activity to a minimum.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Cardiac Failure: Sympathetic stimulation may be a vital component supporting circulatory function in congestive heart failure, and beta-adrenergic receptor blockade carries the potential hazard of further depressing myocardial contractility and precipitating more severe heart failure. In hypertensive patients who have congestive heart failure controlled by digitalis and diuretics, beta-blockers should be administered cautiously. Both digitalis and beta-adrenergic receptor blocking agents slow AV conduction. 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. Therefore, at the first sign or symptom of cardiac failure, discontinuation of betaxolol tablets, USP should be considered. In some cases beta-blocker therapy can be continued while cardiac failure is treated with cardiac glycosides, diuretics, and other agents, as appropriate. Exacerbation of Angina Pectoris Upon Withdrawal: Abrupt cessation of therapy with certain beta-blocking agents in patients with coronary artery disease has been followed by exacerbations of angina pectoris and, in some cases, myocardial infarction has been reported. Therefore such patients should be warned against interruption of therapy without the physician’s advice. Even in the absence of overt angina pectoris, when discontinuation of betaxolol tablets, USP is planned, the patient should be carefully observed and therapy should be reinstituted, at least temporarily, if withdrawal symptoms occur. Bronchospastic diseases: PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD NOT IN GENERAL RECEIVE BETA-BLOCKERS. Because of its relative ß 1 selectivity (cardioselectivity), low doses of betaxolol tablets, USP may be used with caution in patients with bronchospastic disease who do not respond to or cannot tolerate alternative treatment. Since ß 1 selectivity is not absolute and is inversely related to dose, the lowest possible dose of betaxolol tablets, USP should be used (5 to 10 mg once daily) and a bronchodilator should be made available. If dosage must be increased, divided dosage should be considered to avoid the higher peak blood levels associated with once-daily dosing. Major Surgery: Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anest

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

Because of its relatively extensive excretion into breastmilk and minimal reported experience during breastfeeding, other beta-blocking agents may be preferred for systemic use, especially while nursing a newborn or preterm infant.

Chemistry & Properties

Formula	C18H29NO3
Molecular weight	307.43 g/mol
IUPAC name	1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
CAS	63659-18-7
PubChem CID	2369
InChIKey	`NWIUTZDMDHAVTP-UHFFFAOYSA-N`
logP	2.39 (XLogP 2.8)
Polar surface area	50.72 Å²
H-bond acceptors / donors	4 / 2
Drug-likeness (QED)	0.62
Lipinski violations	0

SMILES

CC(C)NCC(O)COc1ccc(CCOCC2CC2)cc1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB 0.39)

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2C19	Substrate	—
CYP2D6	Inhibitor	IC₅₀ 65.99999999999994 µM
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Aminophylline	major
Ceritinib	major
Dolasetron	major
Dyphylline	major
Fingolimod	major
Methacholine	major
Oxtriphylline	major
Siponimod	major
Theophylline	major
Acetohexamide	moderate
Aldesleukin	moderate
Alectinib	moderate
Alimemazine	moderate
Amifostine	moderate
Atropine	moderate
Betamethasone	moderate
Brigatinib	moderate
Brimonidine (ophthalmic)	moderate
Brimonidine (topical)	moderate
Budesonide	moderate
Bupropion	moderate
Calcium Phosphate	moderate
Calcium acetate	moderate
Calcium carbonate	moderate
Calcium citrate	moderate
Calcium glubionate anhydrous	moderate
Calcium gluconate	moderate
Calcium lactate	moderate
Canagliflozin	moderate
Celecoxib	moderate
Chlorphenesin	moderate
Chlorpropamide	moderate
Cimetidine	moderate
Clidinium	moderate
Codeine	moderate
Corticotropin	moderate
Crizotinib	moderate
Dapagliflozin	moderate
Deflazacort	moderate
Dexamethasone	moderate

Showing 40 of 100+.

Registered Products (2)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Apixol eye drops	Ophthalmic Solution as Hcl 0.5 %	5 ml	Amman Pharmaceutical Indusries	3.640
Betac	Tablet 20 mg	30 tab	Al Hilal Drug Store	4.400