Eye Ophthalmic Agents

Acetazolamide (Diamox) Apraclonidine (Iopidine) Betaxolol, Ophthalmic (Betoptic) Brimonidine (Alphagan P) 

Ocupress Ophthalmic) Dipivefrin (Propine) Dorzolamide (Trusopt) 

Teriparatide (Forteo) Zoledronic acid (Zometa, Reclast) 

Echothiophate Iodine (Phospholine Ophthalmic) Epinastine (Elestat) 

Rimexolone (Vexol Ophthalmic) Timolol, Ophtlialmic (Timoptic) 

Testostei one (AndroGel, Andi oderm,. S Irian t, Testim) 

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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. 

Carteolol (Cartrol/ Ocupress Ophthalmic) [Beta Blocker/ Glaucoma Agent] Uses HTN, T lOP, chronic open-angle glaucoma Action Blocks [3-adrenergic receptors (p, 2)1 ISA Dose Ophth 1 gt in eye(s) bid Caution [C (1st tri) D (2nd 3rd tri), /-] Cardiac failure, asthma Contra Sinus bradycardia heart block >lst-degree bronchospasm Disp Ophth soln SE Drowsiness, sexual dysfxn, bradycardia, edema, CHF, ocular conjunctival... 

Chloramphenicol also is widely used for the topical treatment of eye infections. It is a very effective agent because of its extremely broad spectrum of activity and its ability to penetrate ocular tissue. The availability of safer, less irritating instilled ophthalmic antibiotics and the increase in fatal aplastic anemia associated with the use of this dosage form suggest that this agent might best be withdrawn. 

Targeting a drug to its site of action is useful to enhance its effectiveness and reduce toxicity. If accessible this can be achieved by direct local application, e.g. eye drops to treat ophthalmic conditions, inhalers to treat respiratory conditions, but currently strategies such as the development of targeting agents such as monoclonal antibodies or the use of the more permeable nature of tumour capillaries to allow accumulation of macromolecular carriers have also been employed. 

Nadolol is noteworthy for its very long duration of action its spectrum of action is similar to that of timolol. Timolol is a nonselective agent with no local anesthetic activity. It has excellent ocular hypotensive effects when administered topically in the eye. Levobunolol (nonselective) and betaxolol (E -selective) are also used for topical ophthalmic application in glaucoma the latter drug may be less likely to induce bronchoconstriction than nonselective antagonists. Carteolol is a nonselective 13-receptor antagonist. 

Topical local anesthesia is often used for eye, ear, nose, and throat procedures. Satisfactory topical local anesthesia requires an agent capable of rapid penetration across the skin or mucosa, and with limited tendency to diffuse away from the site of application. Cocaine, because of its excellent penetration and local vasoconstrictor effects, has been used extensively for ear, nose and throat (ENT) procedures. Cocaine is somewhat irritating and is therefore less popular for ophthalmic procedures. Recent concern about its potential cardiotoxicity when combined with epinephrine has led most otolaryngology surgeons to switch to a combination containing lidocaine and epinephrine. Other drugs used for topical anesthesia include lidocaine-bupivacaine combinations, tetracaine, pramoxine, dibucaine, benzocaine, and dyclonine. 

Antiviral Efficacy and Clinical Use. Vidarabine (Vira-A) was the first systemic agent used to treat herpesvirus infections, including CMV, herpes simplex virus, and varicella-zoster virus.42 In the past, this drug was administered by continuous intravenous infusion to treat severe systemic infections caused by these viruses, but systemic use of vidarabine has been replaced by safer and less toxic agents. Vidarabine is currently used primarily to treat local viral infections of the eye (e.g., herpes simplex keratoconjunctivitis) it is applied topically by ophthalmic ointment to treat these infections. 

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