Indication: Indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open angle glaucoma.
Pharmacology: Metipranolol is a beta1 and beta2 (non-selective) adrenergic receptor-blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Metipranolol is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Metipranolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Metipranolol reduces intraocular pressure with little or no effect on pupil size or accommodation in contrast to the miosis which cholinergic agents are known to produce.
Mechanism Of Action: Although it is known that metipranolol binds the beta1 and beta2 adrenergic receptors, the mechanism of metipranolol's action is not known. It has no significant intrinsic sympathomimetic activity, and has only weak local anesthetic (membrane-stabilizing) and myocardial depressant activity. It appears that the ophthalmic beta-adrenergic blocking agents reduce aqueous humor production, as demonstrated by tonography and fluorophotometry. A slight increase in aqueous humor outflow may be an additional mechanism.
Drug Category: Adrenergic beta-Antagonists; Sympatholytics; Antihypertensive Agents; Anti-Arrhythmia Agents; ATC:S01ED04
Brand Names/Synonyms: BRN 2152010; Disorat; METIPRANOLOL HYDROCHLORIDE; Metipranolol; Metipranolol [Usan:Ban:Inn]; Metipranololum [Inn-Latin]; Optipranolol; Trimepranol; VUFB-6453
Dosage Forms: Not Available
Absorption: Not Available
Interactions:
DrugBank: Interactions for Metipranolol
Interactions for Metipranolol:
OptiPranolol® Ophthalmic Solution should be used with caution in patients who are
receiving a beta-adrenergic blocking agent orally, because of the potential for additive effects on systemic
beta-blockade.
Close observation of the patient is recommended when a beta-blocker is administered to patients
receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of
hypotension and/or bradycardia.
Caution should be used in the coadministration of beta-adrenergic receptor blocking agents, such as
metipranolol, and oral or intravenous calcium channel antagonists, because of possible precipitation of left
ventricular failure, and hypotension. In patients with impaired cardiac function, who are receiving calcium channel
antagonists, coadministration should be avoided.
The concomitant use of beta-adrenergic receptor blocking agents with digitalis and calcium channel
antagonists may have additive effects, prolonging atrioventricular conduction time.
Caution should be used in patients using concomitant adrenergic psychotropic drugs.
Ocular
In patients with angle-closure glaucoma, the immediate treatment objective is to re-open the angle by
constriction of the pupil with a miotic agent. OptiPranolol Ophthalmic Solution has little or no effect on the pupil,
therefore, when it is used to reduce intraocular pressur e in angle-closure glaucoma, it should be used only with
concomitant administration of a miotic agent.
Chemical IUPAC Name: [4-[2-hydroxy-3-(1-methylethylamino)propoxy]-2,3,6-trimethyl-phenyl]ethanoate
Chemical Formula: C17H27NO4
Half Life: Not Available
Drug Type: Approved Drug
# Accession No: APRD00668
CAS Registry Number: 22664-55-7
