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Carteolol

S01E - Antiglaucoma preparations and miotics ATC S01ED05 Small molecule approved 1988 Oral Topical Natural product

JFDA label: Opti-tens LP 2% ED

Indications

Approved

  • Cardiovascular Diseases — cardiovascular disease
  • Glaucoma — glaucoma

Contraindications

Source: openFDA

  • Carteolol is contraindicated in those individuals with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS ); sinus bradycardia; second- and third-degree atrioventricular block; overt cardiac failure (see WARNINGS ); cardiogenic shock; or hypersensivity to any component of this product. 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 (5)

Not Known Arrhythmia · Atrioventricular block · Bradycardia · Cardiac failure congestive · Palpitations

Vascular disorders (1)

Not Known Hypotension

Nervous system disorders (6)

Not Known Cerebral ischaemia · Cerebrovascular accident · Dizziness · Headache · Loss of consciousness · Syncope

Immune system disorders (1)

Not Known Hypersensitivity

Metabolism and nutrition disorders (2)

Not Known Diabetes mellitus · Hypoglycaemia

Gastrointestinal disorders (1)

Not Known Nausea

Skin and subcutaneous tissue disorders (1)

Not Known Rash generalised

Psychiatric disorders (3)

Not Known Depression · Insomnia · Photophobia

Eye disorders (7)

Not Known Conjunctivitis · Diplopia · Eye irritation · Eyelid ptosis · Lacrimation increased · Vision blurred · Visual impairment

Infections and infestations (1)

Not Known Sinusitis

General disorders and administration site conditions (8)

Not Known Asthenia · Conjunctival hyperaemia · Dysgeusia · Keratitis · Night blindness · Oedema · Shock · Vital dye staining cornea present

Respiratory, thoracic and mediastinal disorders (3)

Not Known Bronchospasm · Dyspnoea · Respiratory failure

Dosing

Source: openFDA

The usual dose is one drop of Carteolol Hydrochloride Ophthalmic Solution 1% in the affected eye(s) twice a day. If the patient's IOP is not at a satisfactory level on this regimen, concomitant therapy with pilocarpine and other miotics, and/or epinephrine or dipivefrin, and/or systemically administered carbonic anhydrase inhibitors, such as acetazolamide, can be instituted.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Carteolol has not been detected in plasma following ocular instillation. However, as with other topically applied ophthalmic preparations, Carteolol may be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported with topical application of beta-adrenergic blocking agents (see CONTRAINDICATIONS ). Cardiac Failure: Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe failure. 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. At the first sign or symptom of cardiac failure, Carteolol Hydrochloride should be discontinued. Non-Allergic Bronchospasm: In patients with non-allergic bronchospasm or with a history of non-allergic bronchospasm (e.g., chronic bronchitis, emphysema), Carteolol Hydrochloride Ophthalmic Solution should be administered with caution since it may block bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta 2 receptors. Major Surgery: The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. Beta-adrenergic receptor blockade impairs the ability of the heart to respond to beta-adrenergically mediated reflex stimuli. This may augment the risk of general anesthesia in surgical procedures. Some patients receiving beta-adrenergic receptor blocking agents have been subject to protracted severe hypotension during anesthesia. For these reasons, in patients undergoing elective surgery, gradual withdrawal of beta-adrenergic receptor blocking agents may be appropriate. If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of such agonists as isoproterenol, dopamine, dobutamine or levarterenol (see OVERDOSAGE ). Diabetes Mellitus: Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiv

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

No data are available for the use of carteolol during breastfeeding.

Chemistry & Properties

2D structure
FormulaC16H24N2O3
Molecular weight292.38 g/mol
IUPAC name5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
CAS51781-06-7
PubChem CID2583
InChIKeyLWAFSWPYPHEXKX-UHFFFAOYSA-N
logP1.7 (XLogP 1.0)
Polar surface area70.59 Ų
H-bond acceptors / donors4 / 3
Drug-likeness (QED)0.77
Lipinski violations0
SMILESCC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes (logBB -0.4)

Enzyme interactions

EnzymeRoleDetail
CYP2C19Substrate
CYP2D6Substrate
CYP3A4Substrate

Transporters

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

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Aminophylline major
Ceritinib major
Dolasetron major
Dyphylline major
Epinephrine major
Fingolimod major
Formoterol major
Indacaterol major
Iobenguane (I-131) major
Olodaterol major
Orciprenaline major
Pirbuterol major
Salbutamol major
Salmeterol major
Siponimod major
Terbutaline major
Theophylline major
Vilanterol major
Aldesleukin moderate
Alectinib 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
Chlorpropamide moderate
Cimetidine moderate
Clidinium moderate
Corticotropin moderate

Showing 40 of 100+.

Registered Products (1)

BrandForm / strengthPackAgentCitizen (JOD)
Opti-tens LP 2% ED Injection 20 mg/ml 3 ml Dar Al Dawa Development and Investment Co Ltd/Jordan 4.920