optipran

Description : OPTIPRANOLOL® (metipranolol ophthalmic solution) 0.3% containsmetipranolol, a non-selective beta-adrenergic receptor blocking agent optipran. Metipranololis a white, odorless, crystalline powder optipran.

The chemical name of metipranolol is (±)-1-(4-Hydroxy-2,3,5-trimethylphenoxy)-3-(isopropylamino)-2-propanol-4-acetate optipran.

The chemical structure of metipranolol is:

C 17 H 27 NO 4 Mol optipran. Wt optipran. 309.40

Each mL of OPTIPRANOLOL® contains 3 mg metipranolol optipran. INACTIVES: Povidone,Glycerin, Hydrochloric Acid, Sodium Chloride, Edetate Disodium, and PurifiedWater optipran. Sodium Hydroxide and/or Hydrochloric Acid may be added to adjust pH optipran. PRESERVATIVE: Benzalkonium Chloride 0.004% optipran.

Clinical Pharmacology : Metipranolol blocks beta 1 and beta 2 (non-selective)adrenergic receptors optipran. It does not have significant intrinsic sympathomimeticactivity, and has only weak local anesthetic (membrane-stabilizing) and myocardialdepressant activity optipran.

Orally administered beta-adrenergic blocking agents reduce cardiac output inboth healthy subjects and patients with heart disease optipran. In patients with severeimpairment of myocardial function, beta-adrenergic receptor antagonists mayinhibit the sympathetic stimulatory effect necessary to maintain adequate cardiacoutput optipran.

Beta-adrenergic receptor blockade in the bronchi and bronchioles may resultin significantly increased airway resistance from unopposed para-sympatheticactivity optipran. Such an effect is potentially dangerous in patients with asthma orother bronchospastic conditions (see CONTRAINDICATIONS and WARNINGS ) optipran.

OPTIPRANOLOL® Ophthalmic Solution, when applied topically in the eye, hasthe action of reducing elevated as well as normal intraocular pressure (IOP),whether or not accompanied by glaucoma optipran. Elevated intraocular pressure is a majorrisk factor in the pathogenesis of glaucomatous visual field loss optipran. The higherthe level of intraocular pressure, the greater the likelihood of glaucomatousvisual field loss and optic nerve damage optipran.

The primary mechanism of the ocular hypotensive action of metipranolol is mostlikely due to a reduction in aqueous humor production optipran. A slight increase inoutflow may be an additional mechanism optipran. OPTIPRANOLOL Ophthalmic Solution reducesIOP with little or no effect on pupil size or accommodation optipran.

In controlled studies of patients with intraocular pressure greater than 24mmHg at baseline, OPTIPRANOLOL Ophthalmic Solution reduced the average intraocularpressure approximately 20-26% optipran.

The onset of action of OPTIPRANOLOL Ophthalmic Solution, as measured by a reductionin intraocular pressure, occurs within 30 minutes after a single administration optipran. The maximum effect occurs at about 2 hours optipran. A reduction in intraocular pressurecan be demonstrated 24 hours after a single dose optipran. Clinical studies in patientswith glaucoma treated for up to two years indicate that an intraocular pressurelowering effect is maintained optipran.

Animal Pharmacology : In rabbits administered metipranolol in one eye at 2 to4 fold increased concentrations, multi-focal interstitial nephritis was observedin male animals, and lympho-hystiocytic and heterophilic interstitial pneumoniawas observed in female animals optipran. The clinical relevance of these findings inunknown optipran.

Indications And Usage : OPTIPRANOLOL Ophthalmic Solution is indicated in thetreatment of elevated intraocular pressure in patients with ocular hypertensionor open angle glucoma optipran.

Contraindications : Hypersensitivity to any component of this product optipran.

OPTIPRANOLOL Ophthalmic Solution is contraindicated in patients with bronchialasthma or a history of bronchial asthma, or severe chronic obstructive pulmonarydisease; symptomatic sinus bradycardia; greater than a first degree atrioventricularblock; cardiogenic shock; or overt cardiac failure optipran.

Warnings : As with other topically applied ophthalmic drugs, this drug may beabsorbed systemically optipran. Thus, the same adverse reactions found with systemicadministration of beta-adrenergic blocking agents may occur with topical administration optipran. For example, severe respiratory reactions and cardiac reactions, including deathdue to bronchospasm in patients with asthma, and rarely, death in associationwith cardiac failure, have been reported following topical application of beta-adrenergicblocking agents (see CONTRAINDICATIONS ) optipran.

Since OPTIPRANOLOL Ophthalmic Solution had a minor effect on heart rate andblood pressure in clinical studies, caution should be observed in treating patientswith a history of cardiac failure optipran. Treatment with OPTIPRANOLOL Ophthalmic Solutionshould be discontinued at the first evidence of cardiac failure optipran.

OPTIPRANOLOL Ophthalmic Solution, or other beta-blockers, should not, in general,be administered to patients with chronic obstructive pulmonary disease (e.g.,chronic bronchitis, emphysema) of mild or moderate severity (see CONTRAINDICATIONS) optipran. However, if the drug is necessary in such patients, then it should be administeredwith caution since it may block bronchodilation produced by endogenous and exogenouscatecholamine stimulation of beta 2 receptors optipran.

Precautions : General: Because of potential effects of beta-adrenergic receptorblocking agents relative to blood pressure and pulse, these should be used withcaution in patients with cerebrovascular insufficiency optipran. If signs or symptomssuggesting reduced cerebral blood flow develop following initiation of therapywith OPTIPRANOLOL Ophthalmic Solution, alternative therapy shoulld be considered optipran.

Some authorities recommend gradual withdrawal of beta-adrenergic receptor blockingagents in patients undergoing elective surgery optipran. If necessary during surgery,the effects of beta-adrenergic receptor blocking agents may be reversed by sufficientdoses of such agonists as isoproterenol, dopamine, dobutamine or levarterenol optipran.

While OPTIPRANOLOL Ophthalmic Solution has demonstrated a low potential forsystemic effect, it should be used with caution in patients with diabetes (especiallylabile diabetes,) because of possible masking of signs and symptoms of acutehypoglycemia optipran.

Beta-adrenergic receptor blocking agents may mask certain signs and symptomsof hyperthyroidism, and their abrupt withdrawal might precipitate a thyroidstorm optipran.

Beta-adrenergic blockade has been reported to potentiate muscle weakness consistentwith certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness) optipran.

Risk of anaphylactic reaction: While taking beta-blockers, patients with ahistory of severe anaphylactic reaction to a variety of allergens may be morereactive to repeated challenge, either accidental, diagnostic, or therapeutic optipran. Such patients may be unresponsive to the usual doses of epinephrine used totreat allergic reaction optipran.

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