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Ординатура / Офтальмология / Учебные материалы / Color Atlas of Ophthalmology The Quick-Reference Manual for Diagnosis and Treatment

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14 Ophthalmic Pharmacology 411

Antiinflammatories

An in flam m ator y respon se result s w h en cells are dam aged by m icrobes, p hysical agen ts, or ch em ical agen t s an d can be ch aracterized by redn ess, pain , h eat , an d sw elling (Fig. 14.3).

Corticosteroids

Cor t icosteroids com m on ly u sed in oph th alm ic pract ice are sh ow n in Table 14.7, an d are divided in to su bt ypes (sh ort-act ing, in term ediate-act ing, an d long-act ing) based on th eir durat ion of act ion .

Fig . 14.3 Antiinflammatories are given to suppress inflammation in patients with uveitis.

412 Color Atlas of Ophthalm ology

Table 14.7 To pical Corticosteroids

 

Generic Nam e

Concen -

Trade

Typical Adult

 

 

and Preparation

tration

Nam e

Dosage

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Dexam ethasone

0.1%

Generic

1–2 drops every hour

 

 

sodium phosphate

 

 

 

 

during the day and

 

 

solution

 

 

 

 

every 2 h during the

 

 

 

 

 

 

 

night

 

 

Dexam ethasone

0.1%

Maxidex

Mild disease: 1–2 drops

 

 

ophthalm ic suspension

 

 

 

 

4–6 times per day.

 

 

or ointment

 

 

Severe disease: apply

 

 

 

 

 

 

 

drops hourly

 

 

Fluorom etholone

0.1%

Flarex

1–2 drops 2–4 times

 

 

acetate suspension

 

 

 

 

daily

 

 

Fluorom etholone

0.1%

FML and

1 drop 2–4 times daily

 

 

ophthalm ic suspension

 

available

 

 

 

 

 

 

 

generically

 

 

 

 

 

 

0.25%

FML Forte

1 drop 2–4 times daily

 

 

Fluorom etholone

0.1%

FML S.O.P.

 

1

-inch ribbon into the

 

 

2

 

 

ophthalm ic ointment

 

 

conjunctival sac 1–3

 

 

 

 

 

 

 

 

 

 

 

 

 

times/day

 

 

Loteprednol etabonate

0.5%

Lotemax

1–2 drops 4 times daily

 

 

suspension

0.2%

Alrex

1 drop 4 times daily

 

 

 

 

 

Medrysone ophthalmic

1%

HMS

1 drop every 4 h

 

 

suspension

 

 

 

 

 

 

 

Prednisolone acetate

1%

Pred Forte and

1–2 drops 2–4 times

 

 

ophthalmic suspension

 

available

 

 

daily

 

 

 

 

generically

 

 

 

 

 

 

1%

Econopred Plus

2 drops 4 times daily

 

 

 

0.125%

Econopred

2 drops 4 times daily

 

 

 

0.12%

Pred Mild

1–2 drops 2–4 tim es

 

 

 

 

 

 

 

daily

 

 

Prednisolone sodium

1.0%

amase

1–2 drops up to every

 

 

phosphate ophthalm ic

 

Forte and

 

 

hour

 

 

solution

 

available

 

 

 

 

 

 

 

generically

 

 

 

 

 

 

0.125%

amase Mild

1–2 drops up to every

 

 

 

 

and available

 

 

hour

 

 

 

 

generically

 

 

 

 

 

Rimexolone

1%

Vexol

1–2 drops 4 times daily

 

 

ophthalm ic suspension

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Periocular inject ion s are also u sed to deliver cor t icosteroids w h en in flam m a- tor y con dit ion s are u n respon sive to topical t reat m en ts. Th e m ain in dicat ion s for periocular inject ion s are t reat m en t of in term ediate or posterior uveit is an d cystoid m acu lar edem a. Th e cor t icosteroids t ypically u sed are m ethylpredn isolon e (Depo-Medrol), t riam cin olon e aceton ide (Ken alog-40), betam eth ason e (Celeston e Solusp an ), dexam eth ason e (Decadron Ph osph ate), or available gen eric equivalen ts as sh ow n in Table 14.8.

14 Ophthalmic Pharmacology 413

Table 14.8 Injectable Co rticosteroids

 

Generic Nam e and Preparation

Concentration

Trade Nam e

 

 

 

 

 

 

 

 

 

 

 

 

Betamethasone sodium

6 mg/mL

Celestone Soluspan

 

 

Phosphate and betamethasone

 

 

 

 

acetate injectable suspension

 

 

 

 

Dexamethasone sodium

4 mg/m L

Decadron and

 

 

phosphate injection

 

available generically

 

 

Methylprednisolone acetate

40 mg/mL and

Depo-Medrol and

 

 

injectable suspension

80 mg/mL

available generically

 

 

Triamcinolone acetonide

40 mg/mL

Kenalog -40

 

 

injectable suspension

 

 

 

 

 

 

 

 

 

 

 

 

 

Topical Nonsteroidal Antiinflammatory Drugs (NSAIDs)

Topical NSAIDs cu rren tly u sed in oph th alm ology are sh ow n in Table 14.9 an d can be classed as acet ic acids, propion ic acids, an d a prodrug ar ylacet ic acid .

Table 14.9 To pical Nonsteroidal

am m atory Drugs

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Generic Nam e

Trade

 

 

 

Dosing/

 

and Preparation

Nam e

Indication

 

Concentration

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Brom fenac sodium

Xibrom

Postoperative

ammation

One drop t wice

 

solution

 

 

in patients who have

a day/0.09%

 

 

 

 

undergone cataract

 

 

 

 

 

 

extraction

 

 

 

 

Diclofenac sodium

Voltaren

Postoperative

amm ation

One drop four

 

solution

 

 

following cataract

times a day/

 

 

 

 

extraction and for the

0.1%

 

 

 

 

 

temporary relief of pain

 

 

 

 

 

 

and photophobia following

 

 

 

 

 

 

corneal refractive surgery

 

 

 

Flurbiprofen

Ocufen

Inhibition of interoperative

One drop every

 

sodium½hoursolution2

and

 

miosis

 

 

 

 

 

generic

 

 

 

h prior to

 

 

 

 

 

 

surgery/0.03%

 

Ketorolac

Acular

Postoperative

amm ation

One drop four

 

trom ethamine

and

 

in patients who have

times a day/

 

solution

generic

 

undergone cataract

0.5%

 

 

 

 

 

extraction and for relief of

 

 

 

 

 

 

ocular itching due to

 

 

 

 

 

 

seasonal allergic conjunctivitis

 

 

 

 

Acular PF

Reduction of ocular pain and

One drop four

 

 

 

 

photophobia following

tim es a day/

 

 

 

 

incisional refractive surgery

0.5%

 

 

 

Acular LS

For the reduction of ocular

One drop four

 

 

 

 

pain and burning/stinging

times a day/

 

 

 

 

following corneal refractive

0.4%

 

 

 

 

 

surgery

 

 

 

 

Nepafenac

Nevanac

For pain

ammation

One drop three

 

ophthalm ic

 

 

associated with cataract

times a day/

 

suspension

 

 

surgery

 

0.1%

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

414 Color Atlas of Ophthalm ology

Drug Combinations (Corticosteroids/Antibiotics)

Th e com bin at ion t reat m en t s are m u lt iple-dose su spen sion s, solu t ion s, an d oin t- m en ts for topical applicat ion th at in clu de cor t icosteroids com bin ed w ith an t ibiotics su ch as gen tam icin , polym yxin B, n eom ycin , tobram ycin , an d sulfacetam ide. Th e various cor t icosteroid/an t ibiot ic com bin at ion s are sh ow n in Table 14.10.

Mydriatics and Cycloplegics

Mydriat ic an d cycloplegic agen ts h ave been used in th e pract ice of oph th alm ology sin ce th e m id -n in eteen th cen t u r y. Trade n am es, st rength s, an d dosages are sh ow n in Table 14.11.

Glaucoma

Medicat ion s can preven t vision loss due to glau com a by slow ing or preven t ing in t raocular pressu re (IOP)-related dam age to th e opt ic n er ve (Fig. 14.4). Th e m a- jorit y of glau com a agen ts w ere developed for th e m ore com m on , in sidiou s form of th e disease, prim ar y open -angle glau com a (POAG). IOP plays an im por tan t role in th e n europath ology of POAG. Prevalen ce an d in ciden ce of POAG in crease as IOP in creases. Th erefore, if pat ien t s w ith in creased IOP or sign s of opt ic n er ve dam age are star ted early on m edicat ion s th at decrease IOP, vision can often be preser ved in th e long term . Seven classes of glaucom a drugs are u sed; th e n am es, adm in ist ra- t ion , an d con cen t rat ion s are listed in Table 14.12.

14 Ophthalmic Pharmacology 415

416 Color Atlas of Ophthalm ology

14 Ophthalmic Pharmacology 417

418 Color Atlas of Ophthalm ology

Fig . 14.4 Cupping of the disk in glaucoma.

Beta-Adrenergic Blocking Agents

Mechanism

A disru pt ion in th e physiological product ion of aqu eou s h u m or n at urally resu lts in flu ct u at ion s in IOP. Th e m ajor site of aqueou s h u m or produ ct ion is in th e ciliar y body an d is part ially con t rolled by β-adren ergic receptors. Act ivat ion of th ese receptors cau ses an in crease in th e product ion of aqu eous h u m or w ith in th e ciliar y body. A β-an tagon ist reduces th e form at ion of aqueous h um or result ing in a low er IOP.

Indications

Th is agen t is u sed as a first-lin e t reat m en t of POAG. Prim ar y angle closure glau - com a (PACG) is also an in dicat ion , bu t th e agen t s th at supp ress aqu eou s h um or for- m at ion m ay be less effect ive in th is form of glau com a becau se th e ciliar y body m ay be isch em ic, ren dering th e β-receptors n on fun ct ion al. Never th eless, β-an tagon ist s are st ill in dicated in PAC because of th e redu ct ion in IOP-en h an cing relaxat ion of th e an terior ch am ber angle.

Contraindications/Adverse Effects

Th e sam e β-adren ergic receptors in th e ciliar y body are fou n d in oth er organ s, an d system ic side effect s m ay in clu de decreased h ear t rate, d ecreased blood p ressu re, an d exacerbat ion of in t r in sic bron ch ial asth m a an d ch ron ic obst r u ct ive pu lm o- n ar y disease du e to bron ch osp asm . Th is topical m edicat ion sh ou ld be u sed w ith cau t ion in p at ien t s w ith cardiac or lu ng d isease. Bet a xolol is a cardioselect ive β-1- adren ergic an t agon ist develop ed to avoid t h e p u lm on ar y com p licat ion of t im olol, th e n on select ive classic top ical β-adren ergic an t agon ist . Th e select ive an t agon ist m ay be as effect ive in low er ing IOP as t h e n on select ive, bu t p u lm on ar y sid e effect s h ave occasion ally been n oted . Th erefore, becau se of th e severit y of p u lm o- n ar y com p licat ion s in th e u se of th is class of glau com a agen t , cau t ion sh ou ld be u sed w h en con sid ering th is dr ug in th e p at ien t w ith excessive im p air m en t of pu lm on ar y fu n ct ion . Also, t h e effect s of system ic m edicat ion s su ch as β-block- ers, d igit alis, an d reserp in e can be en h an ced w it h th e u se of top ical β-ad ren ergic an t agon ist s.

14 Ophthalmic Pharmacology 419

420 Color Atlas of Ophthalm ology

Prostaglandin Analogues

Mechanism

Th e prostaglan din class of glau com a agen t s at tem pts to alter th e IOP by en h an cing th e outflow of aqu eou s h um or. Th e classic route of aqu eou s outflow is th rough th e t rabecu lar m esh w ork in to th e can al of Sch lem m . Th e prostaglan din s also take advan tage of a sup plem en tal rou te of aqueous outflow th rough th e uveoscleral path w ay by in creasing th e por t ion of aqu eou s th at th e path w ay n orm ally drain s.

Indications

Lat an oprost w as th e first syn th et ic prostaglan din an alogue th at form ed a n ew class of drugs developed specifically for glau com a. A single daily dose h as been sh ow n to be m ore effect ive in redu cing IOP th an t im olol 0.5%adm in istered t w ice daily, establish ing th e prost aglan din class as a first-lin e t reat m en t for POAG. Th e prostaglan din s are adm in istered topically on ly.

Contraindications/Adverse Effects

Th ere h ave been n o m ajor system ic toxic effects of topical prost aglan din an a- logue use in glaucom a th us far, bu t th ese drugs are w ell kn ow n for som e com m on , un iqu e ocu lar effect s. Pat ien t s frequen tly acqu ire perm an en t darken ing of th e iris, conju n ct ival hyperem ia, conju n ct ival flush ing, red eye, an d a hyper t rich osis of th e eyelash es th at rem its w h en th e m edicat ion is stopped . Th ere are rare adverse effects in cluding cystoid m acu lar edem a, dam age to th e blood –ret in al barrier, an d a periocu lar pigm en t at ion of cosm et ic con cern .

Carbonic Anhydrase Inhibitors

Mechanism

Like th e β-adren ergic blocking agen t s, th is class suppresses aqueou s h u m or produ ct ion . Th e m ech an ism involves decreasing th e form at ion an d secret ion of aqu e- ous at an in t racellu lar level. Carbon ic an hydrase in h ibitors (CAIs) are th e on ly class of glau com a m edicat ion s th at ut ilize a system ic route of deliver y th rough oral m edicat ion s. A topical form , dorzolam ide, is also available an d is m ore com m on ly used th an th e system ic form .

Indications

Oral CAIs are u sually used to su pplem en t various topical agen t s w h en IOP is n ot being adequ ately low ered . Becau se of th eir system ic effect s an d in abilit y to low er IOP in depen den tly, CAIs are usu ally n ot u sed as a first-lin e or sole prim ar y t reat- m en t of glau com a. A com bin at ion of dorzolam ide an d topical t im olol, a β-an t ago- n ist , is available (Cosopt).

Contraindications/Adverse Effects

Th e p ossible adverse effect s of th e system ic CAIs, acetazolam ide, m eth azolam ide, an d dich lorph en am ide, in clude paresth esias, an orexia, gast roin test in al dist u r- ban ces, h eadach es, altered taste an d sm ell, sodium an d p otassiu m deplet ion , a predisposit ion to form ren al calculi, an d rarely bon e m arrow sup pression . Th ese side effect s are p ossible w ith th e topical CAIs bu t h ave a m uch low er in ciden ce. With dorzolam ide an d brin zolam ide th e m ost com m on side effect is altered taste sen sat ion .