Ophthalmic agents

The chemistry of most of the drugs in this family is quite simple, accounting in part for the very large number of analogues which have been made. The foundation for the chemistry in this series was laid long ago by Stolz in his classic synthesis of the ophthalmic agent adrenal one (3) in which he reacted catechol with chloroacetyl chloride and then displaced the reactive chlorine atom with methylamine to complete the synthesis. Borohydride reduction would have given epinephrine (adrenaline). 

Topical anesthesia will increase the bioavailability of ophthalmic agents by decreasing the blink reflex and the production and turnover of tears. 

Systemic agents for detailed information, see group monograph in Cardiovascular section. Topical ophthalmic agent. 

Other drugs that may interact with systemic -adrenergic blocking agents also may interact with ophthalmic agents. 

Mechanism of Action An ophthalmic agent that is a selective alphaj-adrenergic agonist. Therapeutic Effect Reduces intraocular pressure (lOP). 

Mecfianism of Action An ophthalmic agent that increases the outflow of aqueous humor. Therapeutic Effect Decreases intraocular pressure. 

The step 1 product combined with ophthalmic agents and 2,2 -azobis(2-methylpropio-nitrile) was clamped between two silanized glass plates and polymerized by heating to 100°C for 2 hours. The film was isolated and hydrated in deionized water for at least 4 hours and then autoclaved for 30 minutes at 121°C. The cooled films were analyzed for mechanical properties according to ASTM D-1708a and oxygen permeability. 

Yuen J, FisceUa R, Gaynes B. Ophthalmic agents and managed care.JMCP 2002 8 217-223. 

Take an adequate history to determine whether there has been any previous allergic or toxic response to a drug, especially an ophthalmic agent. 

A rabbit model study suggested that topical 0.2% fluconazole has pharmacokinetic properties, low toxicity, and selective MICs that merit further studies as an ophthalmic agent (Yee et al.). 

Note aplastic anemia is also a risk, but risk with topical ophthalmic agents has been grossly overplayed.)... 

Diamond JP. Systemic adverse effects of topical ophthalmic agents. Implications for older patients. Drugs Aging 1997 ll(5) 352-60. 

Shuhnan DG, Amdahl L, Washington C, Graves A. A combined analysis of two studies assessing the ocular comfort of antiaUergy ophthalmic agents. Clin Ther 200325(4) 1096-1106. 

Examples of organophosphates include the insecticides malathion, parathion, diazinon, fenthion, azinphos methyl, terbufos, dichlorvos, and chlorpyr-ifos the nerve gases soman, sarin, tabun, and VX the ophthalmic agent echothiophate the anthelmintic trichlorfon tricresyl phosphate-containing... 

To overcome several of the pharmacological and pharmaceutical shortcomings of EP as an ophthalmic agent, the pro-drug approach has been successfully applied in the form of the 3,4-dipivaloyl ester, Dipivefrin, DPE (Eq. 9.10). 

Carbachol is used as an ophthalmic agent, in the reduction of intraocular pressure. The drug induces miosis, and is therefore also used to counteract the effects of sympathetic agents in the eye. 

Ocular bioavailability is generally accepted to be extremely low compared to bioavailability obtained from conventional oral doses. Indeed, whereas ocular bioavailability is of the order of 1-3% (Lee and Robinson, 1986) a similar oral bioavailability would probably not be commercially acceptable. There is, therefore, a great potential need for improvement of the ocular bioavailability of almost all ophthalmic agents that penetrate the eye for their pharmacological effect. 

Agent for Chronic Obstructive Agent for Transplant Rejection Antihypertensive Agent for Rhinitis I mm unosu ppressant Antidepressant Ophthalmic Agent Antiallergic/Antiasthmatic Other... 

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