`
`Optician; the British optical and instrument
`v. 223, no. 5853 (May 31 2002)
`General Collection
`W1 OP861
`2002-06-12 12:05:49
`
`•
`
`May 31 2002 £3.25
`
`~e~urnal for OPTOMETRISTS & DISPENSING OPTICIANS
`
`M-vw.optometryonline.net
`
`'Fresh~
`cool ·
`than
`myop
`
`Recommend Refresh® eye drops
`to your customers -
`they'll thank you .for it.
`
`This week's front cover features Allergan. For further details please telephone 01494 444722
`
`2 2>
`
`9 770030 396114
`
`A Reed Business Information Publication
`
`LUPIN EX1036, Page 1
`
`
`
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`j
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`MAY 31, 2002 No 5853 Vol 223
`
`Contents
`
`Features
`Opportunity knocks
`8
`John WilfiltsoJ/ says get ready for the new NHS.
`
`16
`
`The making of a modern practice
`Rob Moss reports on Cambridge-based optometrist Angela
`Gould's progress as she establishes herself as owner of one
`of the university town's oldest practices.
`
`18 Medicines Update - Part 11
`Professonl1ichael Doughty provides an overview of eye
`medicines and other eve care products introduced in the
`last three months.
`
`23 Ocular pharmacokinetics
`Dr fohn Lawrenson discusses ocular pharmacokinetics and
`the significance it has for drug delivery and toxicity.
`
`2 6 Drugs database
`OPTICIAN describes the City Ocular Adverse Reactions to
`Drugs database.
`
`27 Effects of anti-epileptic drugs on visual performance
`Emma Rolf Hilton, Sarah Hosking and Tim Betts describe the
`impact that drugs prescribed to treat epilepsy can have on a
`patient's vision.
`
`31 Clinical Audit Patient Survey
`Dale Harris and Bob Hutchinson look at the dispensing
`process in practice.
`
`32 OPTICIAN Index
`April sa"v slower growth than is usual for spring.
`
`Regulars
`4
`News
`10
`Products
`12
`letters/Comment
`How to contact OPTICIAN
`14 Omen
`35 Appointments
`43 Optical Suppliers' Guide
`47 A-Z of anterior eye disease
`
`Next Issue
`Contact lens monthly
`• John Mev!er and Cristina Sch11ider discuss the dangers of
`ultraviolet light and suggest UV-blocking contact lenses as
`protection.
`• The second part of our pilot CET series on Visual Recognition
`in Contact Lens Practice covers fitting characteristics.
`• Lyndon Jones takes a look at equipping your practice ready for
`contact lens practice.
`
`This week's front cover
`features Allergan.
`llhr.lhllft For further details please
`E~~::':._-~~~~ telephone 01494 444722
`
`LUPIN EX1036, Page 2
`
`
`
`Medicines Update
`for optical practitioners Part 11
`
`MEDICINES UPDATE for optical
`practitioners is designed to keep the UK
`optometrist up to date with all aspects of
`eye medicines and other eye products that
`can be used to manage a range of minor(cid:173)
`to-moderate non sight-threatening
`conditions or diseases that can affect the
`external eye.
`In addition, the series is designed to
`keep the optometrist fully informed of
`the availability and developments of
`ophthalmic medicines for the manage(cid:173)
`ment of severe eye diseases and in
`systemic medicines that could have an
`impact on the eye or vision, including
`those medications likely encountered in
`shared-care schemes.
`This part includes several new products
`
`Professor Michael Doughty provides an overview of eye medicines
`and other eye care products introduced in the past three months
`
`and a brief review of rhe role of oral
`antihistamines in the management of
`seasonal allergic conjunctivitis.
`
`TEN NEW OPHTHALMIC PRODUCTS
`This quarter sees the introduction of
`another option in re-wetting solutions, a
`generic carbomcr gel, several options for
`management of seasonal allergic conjunc(cid:173)
`tivitis (including a new topical ocular
`multiple-acting 'antihistamine, another
`generic mast cell stabiliser, and several
`
`products containing the oral antihistamine
`cetirizine), a new gel formulation oftimolol
`and third prostaglandin analogue for
`management of open-angle glaucoma
`(Table 1). Some changes in product
`availability have also occurred (Table 2).
`A new option in re-wetting solutions is
`available- Blink-n-clean (Figure 1). The
`idea for this product, as emphasised by
`its name, is that the combination of the
`surfactant (tyloxapol) and the substantial
`quantity
`of
`chemical
`buffer
`(tromethamine) is designed to disperse
`
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`ifJ.iil.E~t New ophthalmic phannaceuticals for UK eMilY 2002)
`c
`Dr:i-Jg name
`SL
`hydroxypropylmethylcellulose 0.15%,
`CE
`ty!oxapol oms%,
`1tromethamine 1.2%, EDTA and
`preserved with polyhexamethylene
`biguanide 0.0001%
`
`cone
`
`Pharmaceutical
`
`COMPLETE
`BLINK-N-CLEAN
`
`2carbomer 980, sorbitol 4%, EDTA
`and preserved with cetrimide 0.01 %
`
`0.2%
`
`SL
`CE
`
`CARBOMER GEL
`
`ketotifen, glycerol and preserved
`with banzalkonium chloride
`
`3Na cromoglycate, sorbitol,
`polysorbate 80, EDTA and
`preserved with benzalkonium chloride
`
`0.025%
`
`PoM
`
`ZADITEN
`
`2%
`
`p
`
`VIVICROM
`EYE DROPS
`
`.CO
`
`32
`
`Presentation
`
`15ml multi-use bottle
`
`65
`
`40
`
`66
`
`67
`
`70
`
`51
`
`68
`
`40
`
`1 Og multi-use tube
`
`5 ml multi-use bottle
`
`10 ml multi-use bottle
`
`7 tablets <GSU
`30 tablets <P)
`
`14 tablets
`
`7 tablets
`
`7 tablets <GSU
`30 tablets <P)
`
`Sg multi-use bottle
`
`10mg
`
`10mg
`
`10mg
`
`10mg
`
`GSL
`p
`
`PIRITIEZE ALLERGY
`TABLETS
`
`p
`
`p
`
`BENADRYL
`ONE-A-DAY
`
`CETIRIZINE
`HAYFEVER RELIEF
`
`GSL
`p
`
`HAYFEVER AND
`ALLERGY RELIEF
`
`0.1%
`
`PoM NYOGEL EYE GEL
`
`cetirizine
`
`cetirizine
`
`cetirizine
`
`cetirizine
`
`timolol, sorbitol, lysine, in a
`carbomer 974P- polyvinyl alcohol gel
`vehicle, preserved with
`benzalkonium chloride 0.008 %
`
`bimataprost, NaCI, citrate and
`phosphate buffers, and preserved
`with benzalkonium chloride
`
`0.03%
`
`PoM
`
`LUMIGAN
`
`32
`
`2.5 ml multi-use bottle
`
`1 also known as trometamol 2 also known as carbopol 3also known as Na cromoglicate
`
`Optician \I.\\ .il. 2002 f\!o5K.i.i ,."' 223
`
`w-.vw.optomerryonline.net
`
`LUPIN EX1036, Page 3
`
`
`
`protein that can accumulate on the surface
`of soft con tact lenses, and so reduce
`discomfort associated with a soiled lens.
`This issue of buffer ingredients has
`been raised before with the inclusion of
`citrate in rewetting solutions to promote
`protein dissolution.l Further comparati1·e
`studies with tromerhamine would be
`useful. The hypromellose should provide
`some comfort as well.
`The first generic carbomer gel, a true
`ocular lubricant,2 for use in the manage(cid:173)
`ment of dry eye is available, Carbomer
`ael (Figure 2). It is not a P Medicine, but
`~ CE 1~1arked. The product is referred to
`by its chemical name, polyacrylic.acid eye
`ointment, in the generic listings. As with
`other products with similar indications, it
`is the new carbomer 980 that is included
`(as opposed to the carbomer 934 that was
`once available in these ocular lubricants).
`This new product is not recommended
`for use while wearing contact lenses, bur
`irs licence is 'to relieve eye discomfort and
`eye dryness in wearers and non-wearers of
`contact lenses'.
`In time for the new allergy season,
`readers should note that the well-known
`P Otrivine-Antistine, listed in the College
`of Optometrists' Formulary, has been
`repackaged (Figure 3).
`The same company has also introduced
`a completely new PoJVl option for manage-
`
`Corporate <~5 identificationfor tables
`1 Ciba Vision Ophth.:limics 2 Typharm,
`3 Rhone-Poulenc~Rorer, 4 Farley,
`5 Martindale,~ APS(Berk 7.C-Pharma,.
`8 Cox Pharms, 9 Hillcross Pharms, 10 Norton
`Healthcare, .11 Stevenden Healthcare,
`12 Cusi, 13 Schering-Piough, 14 Dominion, .
`15 Distriphar, 16 Leo Pharnis, 17 Wyeth Labs,
`18 Chauvin, 19 Hoechst-Marion Roussel,
`20 Crookes Healthcare, 21 Mentholatum,
`22 Alcon, 23 Abbott, 24 Johnson &
`Johnson, 25 ASTA Medical, 26 Norton
`Consumer, 27 Boots; 28,Baker Norton
`Pharms, 29 NuCare, 30 Opus Pharms,
`31 Genus Pharms, 32 Allergan, 33 Stafford(cid:173)
`Miller, 34 Sussex Pharms, 35 Cross-Pharma,
`36 NuMark, 37 Wamer.Lambert Consumer,·
`38 UCB Pharma, 39 .Novartis Consumer
`Health, 40 Novartis Ophthalniics <Pharmsl, . ·
`41 Surgical Designs, 42 Bausch & Lomb
`Surgical, 43 Wellcome, 44 Regent Labs,
`45 Merck Sharpe & Qohme.A6 Bioglan,
`47 Generics UK, 48'/v\edeva:Pharnia,.
`49 Pharmacia .& Upj'ohn, ·50 Mid-Optic, ,
`51 Peach Ethical PharmaceUticals; 52: · ·· · ·
`Chrqme-X, .53 Chenimf:]dica; 54 Fiorizel,
`55 Roche, 56 SSL, 57 Aventis f'harma,
`58 Glaxo-Wellcome, 59 uigap Ptiarma,
`60 Spectrum Ophtl)almic5, 61 Vision
`Pharmaceuticals, 62 VXL, 63 Ophfecs
`<Eurol, 64 Pharmacia, 65 Tubllux Pharma,
`66 Pharma-Giobal, 67 GlaxoSmithKiine
`Consumer, 68 Galpharm, 69 Celltech
`Pharms, 70 Pfizer Consumer Healthcare
`
`Carbomer gel
`r "''~ ~;;- ·,:,..'~;!';, .~g,~ <h~~.t\~: 1,] ~~m
`
`FIGURE 2. Generic carbo mer gel lubricant for dry eye
`
`®
`
`....---;----..
`
`Otnvtne
`Antistin
`
`FiGURE 3.
`Topical decongestanUantihistamine
`for hayfever
`
`Figure 1. Re-wetting drops for
`soft contact lenses
`
`ment of seasonal allergic
`conjunctivitis (SAC), namely
`ketotifen 0.025 per cent (as PoM
`Zadiren, Figure 4).
`Ketotifen is not a new drug
`since
`it was assessed and
`introduced in the 1980s.3 It is
`presented as having three
`mechanisms by which it can
`reduce the signs and symptoms
`of SAC, namely as a histamine
`H 1 blocking drug, as a mast cell
`stabiliser and as an anti(cid:173)
`eosinophil drug.3 More recent studies
`indicate that its affinity for H 1 receptors is
`the highest reported for topical ocular
`antihistamines, with an estimated Ki of
`around lnM,4 although it is not as selective
`for H 1 receptors as some other drugs. Like
`another 'second generation' mast-cell
`stabiliser (ie lodoxamide),S it is considered
`able to reduce histamine release from mast
`cells as well reduce eosinophil recruitment
`and activation (company literature), but
`neither of these other activities appear to be
`very substantiaL6
`Notwithstanding, as an antihistamine,
`it can produce substantial reduction in
`symptoms to an allergen challenge within
`minutes (company literature) and is
`considered as comparing very favourably
`to the use of two other topical ocular
`antihistamines, namely levocabastine,
`available as PoM Livosotin and P Livostin
`Direct,7 and emedastine, available as Po!Vl
`Emadine.s
`In the UK, ketotifen 0.025 per cent
`eyedrops are indicated for use on a bds
`basis, and the only real limitation is that
`the current licence is for individuals over
`12 years of age. There are no limits to the
`time period over which it can be used.
`
`When used as a 0.05 per cent
`solution (as available in the US),
`some 75 per cent of patients
`using the product reported
`adequate control of ocular itching
`and lacrimation within seven
`daYs, with the reduction in eye
`redness (hyperaemia) being
`slightlv less.9
`An issue that has arisen,
`especially in comparative studies,
`IS
`11·hether
`the ketotifen
`evedrops, presumably the vehicle
`characteristics, are as comfortable (ie as
`based on the amount of stinging) as other
`products.tO,II It can be noted, however,
`that while some irritation can be expected,
`this is a general problem with many
`eyedrops and the reported effects with
`ketotifen eyedrops do not appear to be
`really clinically significant, for example
`causing very substantial numbers of
`patients to discontinue therapy.8,9
`Another sodium cromoglycate eyedrops
`product is a,·ailable, P Vivicrom Eye Drops
`(Figure S). As with similar products
`containing this first-generation mast-cell
`stabiliser, it is indicued for use for both
`seasonal and perennial allergic conjunc(cid:173)
`tivitis, but not for contact lens wear-related
`conjunctivitis. It is noteworthy that the
`package insert stresses that the eye drops
`'should be used every day during the hay
`fever season, even when you are not
`suffering from any symptoms'. This use
`should be on a qds basis.
`With the new allergy season, for grass
`pollens etc, now under way, there has been
`a veritable explosion in the options
`available for oral antihistamines for
`seasonal allergic conjunctivitis; all of the
`new products contain cetirizine, a new
`
`Drug name
`
`chloramphenicol
`betamethasone
`
`betamethasorie
`c neomycin
`
`cone
`0.5%
`0.1%
`
`0.1%
`0.5%
`
`c
`PoM
`Pcitvi
`
`Phanmaceutical
`
`SNO-PHENICOL
`BETNESOL
`
`PoM
`
`BETNESOL-N
`
`co
`
`18
`69
`
`69
`
`Presentation
`
`discontinued
`·-
`1Om I multi-use bottle ·
`now available again
`1Om I multi-use bottle
`now available again
`
`www.optometryonline.net
`
`Al.\Y 31. 2002 No 'i:iS3 \'oL 223 Optician
`
`LUPIN EX1036, Page 4
`
`
`
`therapeutics quarterly
`
`MEDICINES UPDATE
`
`FIGURE 4. Topical
`antihistamine/
`mastOcell
`
`Sodium cromoglicate
`eyedrops for hayfever
`and perennial allergic
`conjunctivitis
`
`generation 'non-drowsy' antihistamine.
`These options are the direct result of
`further deregulation on the access to
`'medicines' in that several of these can
`be added to the ever-growing list ofGSL
`options being made available in small pack
`sizes of seven tablets.l2,13
`Cetirizine, a histamine H 1-blocking
`drug, has a well-established efficacy in
`reducing the signs and symptoms of
`seasonal allergic conjunctivitis, as well as
`nasal symptoms.
`Based on both patient reports and
`external eye assessments with grading
`schemes, cetirizine 1 Omg qd treatment
`can produce a clinically significant
`improvement, 14,15 for example on ocular
`irritation, itching, lacrimation and conjunc(cid:173)
`tival redness. Newer research indicates
`that sufficient quantities of cetirizine reach
`the tear film after oral administration
`(lOmg BDS) to have an impact on
`polvmorphonuclear leukocytes reacting
`at the conjunctival surface.l6
`The first two cetirizine products on the
`list should be noted carefully before
`jumping to conclusions abom errors in the
`listings. Now available as both a P
`l'vledicine (30 tablets) and GSL (7 tablets)
`is Piriteze Allergy 1·ablets (Figure 6). The
`product contains cetirizine, and not as
`might be expected, the older generation
`antihistamine chlorpheniramine (as found
`in P Piriton, marketed by the same
`companv).
`As with the other products, they are
`not recommended for use by children
`under the age of 12 vears, but some of the
`package inserts note that use in children
`between the ages of six and 12 years can
`be done under the supervision of a doctor.
`It is left to the reader to decide if 'doctor'
`would include one's 'eve doctor'.
`A ne\\' option from the Benadrvl line,
`
`Optician;-..~:,~ 31. ~OO.! 1\:(J SK~J \·uL 223
`
`a gam contammg cetmz1ne 1 Omg, has
`also been introduced as Benadryl One(cid:173)
`a-day Allergy Relief (Figure 7). It
`should not be confused with Benadryl
`Allergy Tablets that contain acrivastine
`1.3mg. Several generic options
`containing cetirizine are also now
`available. These are an addition to the
`Pollonase line, namely
`P Cetirizine Hayfever
`Relief(Figure 8), and a
`completely new line
`from Galpharm, namely
`Hayfever and Allergy
`Relief (Figure 9). As
`with
`the first new
`option,
`the
`latter
`generic option is also
`available in a small pack
`size as a CSL product
`for
`the
`local
`supermarket.
`At least two other
`generics for cetirizine,
`in pack sizes of 30
`tablets, have also been
`marketed (companies 6 and 46). For all
`these products, while there are still small
`print warnings about the possibility of
`drowsiness as an ADR, when used at the
`recommended doses cetirizine is consid(cid:173)
`ered to have a very low potenrial for such
`side effects.l7 Notwithstanding, should
`optometrists be recommending the use
`of these products to their patients, time
`should still be given to consideration of
`ADRs, and even though some of them
`may well be attributable ro the allergy
`condition itself, IS the anti-histamine could
`still exacerbate the patient's condition.
`
`Pi ri.teze~ allergy
`
`tablers
`.
`Cetirizine Dihydrochloride 10mg
`rehef from hayfever and skin allergies
`one a day
`3D tablets
`
`• ·~ ...
`,...
`
`....... ,.~.
`
`A new option is available for timolol, a
`non-selective beta-blocker, for manage(cid:173)
`ment of open-angle glaucoma. The new
`gel formulation, Po.l'il Nyogel (Figure 10)
`has timolol 0.1 per cent in a carbo mer gel(cid:173)
`polyvinyl alcohol (PYA) mixture. The
`carbomer is carbomer 947P rather than
`980 as used in dry-eye products.
`This new timolol eye 'gel', also known
`as 'T-gel', is also different to the on-eye(cid:173)
`setting gel used as the vehicle PoM
`Timoptol LA that contains timolol 0.5 per
`cent. The gellan gum (also known as
`Gelrite) solution which is the vehicle for
`Timoptol LA interacts with divalent
`cations in the tear film to produce a gel, an
`ophthalmic gel-forming solution or GFS.J9
`The new timolol gel works on a
`different principle by interacting with
`ocular surface mucins. The timolol itself
`is 'trapped' in the carbomer-PVA polymer
`and the interaction with the ocular surface,
`via mucins, is presented as a 'mucoadhe(cid:173)
`sive' ge1.20
`The idea behind the first gel-based
`ophthalmic timolol product (Timoptol LA
`or Timoptic XE outside of the UK), was
`to promote ocular contact time in order to
`increase ocular drug delivery so as to allow
`for routine once-daily dosing.Zl An added
`benefit, partly related to the once-daily
`dosing, was that systemic cardiovascular
`effects might be slightly reduced.22,23The
`new timolol 0.05 per cent ophthalmic gel,
`based on carbomer (polyacrylic acid
`polymer), has been reported to provide
`improved ophthalmic delivery in animal
`models.24 In clinical trials on non-glauco(cid:173)
`matous human eyes, the efficacy ofT-gel
`0.1 per cent as an ocular hypotensive agent
`has been reported to be equivalent to
`timolol 0.5 per cent.25 As with the older
`timolol gel, the new product, PoM Nyogel,
`is indicated for once-daily use, preferably
`in the morning to hopefully avoid night(cid:173)
`time bronchial effects.
`The limitation for use in asthmatics is well
`established, but it should be noted that the
`list of cardiovascular medications under (SIP)
`gets longer and longer and now specifically
`
`FIGURE 6: Branded cetirizine anti-allergy
`tablets for hayfever and perennial allergic
`conjunctivitis
`
`FIGURE 7. Branded cetirizine anti-allergy
`tablets for hayfever and perennial allergic
`conjunctivitis
`
`FIGURE 8: Generic cetirizine anti-allergy
`tablets for hayfever and perennial allergic
`conjunctivitis
`
`lvww,optometryonline.net
`
`LUPIN EX1036, Page 5
`
`
`
`• . ALLERCAN
`
`.......
`'•Ll.JMIGAN®
`
`0.3mg/ml
`EYE DROPS.
`SOLUTION
`
`Brmaloprosl OJ mg/ml
`
`3ml
`
`acceptable for rhe UK (since this is the
`term used in the latest edition of MJMS),27
`but this new drug is being referred to as
`a pwstamide. The question to be asked it
`whether this distinction is important, or
`whether all three drugs (ie latanoprost,
`mn·aprost and bimawprost) can all be
`considered wgcthcr as 'new generation'
`anti-glaucoma medications
`that improve aqueous
`outno11· via the uveoscleral
`route.
`was
`Bimatoprost
`developed as drug AGN
`192024, and was originally
`presented as a unique class
`of drugs caloled OHLs
`(octilar
`hypotensive
`lipids).ZB
`Company-supported
`pre-clinical evaluation
`literature appears to be at
`pains to point out further
`that bimatoprost should not
`be simply considered as
`another alternative
`to
`the other
`prostaglandin analogues.29 Firstly, unlike
`latanoprost (an isopropyl ester form of
`prostaglandin F zcx), bimatoprost is not a
`pro-drug, ie it does not need to be
`converted from the ester into its active
`acid form once absorbed by the anterior
`segment tissues.
`The ester derivatisation, however,
`provides improved corneal penetration.
`
`FIGURE 11. Third option of a
`prostaglandin type drug for
`open-angle glaucoma
`
`includes digoxin, adrenergic neurone blockers
`(such as reserpine), the calcium blockers used
`for angina or high blood pressure or Reynaud's
`syndrome (for example, nifcdipine and
`verapamil), ami-arrhvthmia drugs (eg
`quinidine and disopvramide), as well as other
`beta-blockers.
`In summary, therefore, 'ts with the use
`of other topical ophthalmic
`beta-blockers,
`the ne11·
`timolol gel is generallv not
`for use in patients with anv
`form of significant bronchial
`or cardiovascular disease,
`but with the use of the gel
`formulation
`and
`the
`reduction in timolol concen(cid:173)
`tration to 0.1 per cent, the
`chance of adverse reactions
`in those with borderline
`diseases of these types
`should be reduced. The
`outcome of substantial open(cid:173)
`label clinical trials with Po!\ I
`Nyogel on patients with
`glaucoma have yet to be published.
`A third 'prostaglandin analogue' for
`open-angle glaucoma has been marketed,
`namely bimatoprost 0.03 per cent
`(0.3mg/ml) in Po!\1 Lumigan (Figure 11 ).
`Its introduction will likely re-open the
`debate as to why different prostaglanin(cid:173)
`type substances and/or drugs can have
`different effects on IOP.26 The term
`prostaglandin analogue is presumably still
`
`FIGURE 9. Generic cetirizine anti-allergy
`tablets for hayfever and perennial allergic
`conjunctivitis
`
`NOVAltTIS
`
`FIGURE 10. New eye g'el fonnulation of timolol
`for open-angle glaucoma
`
`,.,. <;.t.~:,pr\_ t..~
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`"Equipment finance is simple
`and keeps cash in the business:'
`Oliver Judge, Optician
`Siemens Financial Services customer
`
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`~'"''" 31, zooz No 5853 VoL 223 Optician
`
`LUPIN EX1036, Page 6
`
`
`
`Bimatoprost actually is a synthetic phenyl
`derivative of a fatty acid amide rather than
`an ester, although both drugs are still 17-
`phenyl derivatiYes of prostaglandin
`F za·26,29 The issue being raised is whether
`bimatoprost not only passively improves
`the non-conventional outflow facility (also
`now being referred to as the pressure(cid:173)
`insensitive aqueous humour outflow
`pathway) but also has an ocular hypoten(cid:173)
`sive effect that is proportionately larger
`for higher lOP values.28,29
`This latter phenomenon is being
`referred to as a pressure-sensitive aqueous
`humour outflow pathway that is indirectly
`linked to the resistance to outflow in
`relation to the actual aqueous production
`and flow rate. This new pathway is,
`however, largely theoretical and cannot
`be directly measured.28 Time will tell as
`to whether this prostaglandin analogue,
`as with the others, will not only offer
`superior control of both daytime and
`nightime lOP to topical ocular beta(cid:173)
`blockers30 but an even greater efficacy as
`a result of a dual effect on outflow.
`Notwithstanding the likely confusion
`and controversy surrounding such a refine(cid:173)
`ment of the possible mechanism of action
`of these types of drugs, the new drug is
`indicated for use as an option in manage(cid:173)
`ment of open-angle glaucoma or ocular
`hypertension when other anti-glaucoma
`medications are either contraindicated (eg
`beta-blockers) or are failing to produce
`the desired effects on lOP. Bimatoprost
`can also be used in combination with
`topical ocular beta-blockers (timolol etc).
`It thus has the same status as the first
`prostaglandin analogue, latanoprost (PoM
`Xalatan) when it was introduced (although
`the indications for latanoprost have now
`been changed- see below).
`In company-supported clinical trials,
`the efficacy of bimaroprost (AGN 192024)
`have been compared to placebo in non(cid:173)
`glaucomatous cyes28 and in patients with
`open-angle glaucoma or ocular hyperten(cid:173)
`sion.J1,32 The Iauer studies have included
`comparisons with latanoprost 0.005 per
`cent qd,'. I and to timolol 0.5 per cem qd or
`bds.-'2 The lOP lowering effects averaged
`between 25 and 35 per cent, making
`bimatoprost clinically comparable to the
`other prostaglandin analogues.33
`It ''as from these studies that it has
`been established that the recommended
`dosing, as with the other two drugs, is
`oncc-dailv and preferably in the evening.
`It should be noted, however, that an (S/P)
`is asthma (respiratory impairment). This
`is mainly because there is inadequate data
`a,·ailablc on the use of this or other topical
`ocular prostaglandin analogues 1n
`asrh marie patients, and not because there
`is considered
`ro be a substantial
`problem.i.i.34 The indications for use of
`the first prostaglandin analogue introduced
`for glaucuma, laranoprost (as Poi\ I Xalatan)
`ha,·e no11· been re,·iscd for it to be used as
`
`Optician \I''" .it. 2011: 'Jo ~KS3 \"or. 22.>
`
`a first line option in management of open(cid:173)
`angle glaucoma and ocular hypertension.
`
`Acknowledgements
`The author wishes to acknowledge the timely
`assistance from the various companies who have
`provided samples for review and answered questions.
`
`REFERENCES
`1 Hong B-S, Bilbault TJ, Chowhan MA eta!.
`Cleaning capability of citrate-containing vs non(cid:173)
`citrate containing lens cleaning solutions: An in
`vitro comparative study. lnt Contact Lens Clinics,
`1994; 21:237-240.
`2 Doughty M]. Drugs, ,)fedications and the Eye, 2002;
`8th Edn (January). Smawcastellane Information
`Services, 23A Henry Bell St, Hclensburgh G84
`7HL, Scotland.
`3 Mikuni I, Fujiwara T, Togawa Keral. Therapeutic
`effects of a new, anti-allergic ophthalmic prepara(cid:173)
`tion. Tokai J Exp Clin Jlfed, 1982: 7: 279-294.
`4 Sharif NA, Su SX, Yanni jl\1. Emedastine: A
`potent, high affinity histamine 1-1 1-receptor(cid:173)
`selective antagonist for ocular use: Receptor binding
`and second messangcr studies. JOcular Pharmacal,
`1994; 10: 653-664.
`5 Bonini S, Schiavone M, Bonini Seta!. Efficacy of
`lodoxamide eye drops on mast cells and eosinophils
`after allergen challenge in allergic conjunctivitis.
`Ophthalmology, 1997; I 04: 849-853.
`6 Yanni JM, Stephens D ], Miller STet a/. The in vitro
`and in vivo ocular pha1111acology of olopatadine (AL-
`4943A), an effective anti-allergic/antihistamin ic agent.
`J Ocul Phannaco! Ther, 1996; 12:389-400.
`7 Doughty M]. Levocabastine, a topical ocular antihis(cid:173)
`tamine available as a Pharmacy Medicine -a literature
`review. The Phannaceutica/J, 2002; 268:367-370.
`8 D'Arienzo PA, Leonardi A, Bensch G. Random(cid:173)
`ized, double-masked, placebo-controlled comparison
`of the efficacy of emedastine difumarate 0.05%
`ophthalmic solution and kerotifen fumarate 0.025%
`ophthalmic solution in the human conjunctival allergen
`challenge model. Clin 7'her, 2002; 24:409-416.
`9 Aguilar A]. Comparative study of clinical efficacy
`and tolerance in seasonal allergic conjunctivitis
`management with 0.1 % olopatadine hydrochloride
`versus 0.05% ketotifen fumarate. :lela Ophrhalmo!
`Scand, 2000; 78:52-55.
`10 Artal MN, Luna JD. Disccpola tv!. A forced
`choice comfort study of olopatidinc hydrochloride
`0.1% versus ketotifcn fumarate 0.05%. Acta
`Ophthalmo! Scand, 2000; 78: 64-65.
`II Kurosawa A, Kuretake Y, Tachihara R el a!.
`Con1parison of eye irritation caused by seven antial(cid:173)
`lergic eyedrops (in Japanese). Folia Ophrhalmo/.Jpn,
`2001; 52: 220-223.
`12 Medicines (Products other than veterinary drugs)
`(General Sale List) Amendment ('\lo 2) Order 2001.
`SI 2001. No 4111.
`13 Chemist & Dn(rzgi<l (2002). Januarv· S. pp 6.
`14 Davies 131-l. Prophylactic treatment of seasonal
`allergic rhinitis. Clin Ther, 1991: 13: 87-91.
`IS Katalin S, Margit V. Foil mann Per a/. The role
`of ceririzine in the out-pati~nt treatment of allergic
`conjunctivitis (in Hungarian). Szwu:szel, 1993; 130:
`111-113.
`16 Kantm A, Oggiano i\:, Coppa G\" tl rtf. Cctirizine
`reduces the primingcapacitv- on neutrophilic polymor(cid:173)
`phonuclear leukocytes ofbcrinl<li lluid from subjects
`with allergic conjuncti\·iris after specific challenge.
`
`ClinDmg!nves!, 1997; 14:346-352.
`17 Volkerts ER, Van Willigenburg APP, Van Laar
`MW eta/. Does cetirizine belong to the new genera(cid:173)
`tion of antihistamines? An investigation into its
`acute and subchronic effects on highway driving,
`psychometric test performance and daytime sleepi(cid:173)
`ness. Human Psychopharmacol, 1992; 7: 227-238.
`18 Spaeth], Klimek L, Mosges R. Sedation in allergic
`rhinitis is caused by the condition and not by antihis(cid:173)
`tamine treatment. Allergy, 1996; 51: 893-906.
`19 Greaves JL, Wilson CG, Rozier A eta/. Scinti(cid:173)
`graphic assessment of an ophthalmic gelling vehicle
`in man and rabbits. Curr l!.)•e Res, 1990; 9: 415-420.
`20 Krishnamoorthy R, Mitra AK. Mucoadhesive
`polymers in ocular drug delivery. In (Mitra AK, ed)
`Ophrholmir Dmg Deli'i.'tt)' Sysrems. Marcel Dekker
`Inc, New York, 1993, pp. 199-221.
`21 Laurence], Holder D, Vogel Ret a/. A double(cid:173)
`masked, placebo-controlled evaluation oftimolol in
`a gel vehicle . .1 C/oumma, I 993; 2: 177-181.
`22 Dickstein K, Hapnes R, Aarsland T Comparison
`of aqueous and gel ian ophthalmic timolol with
`placebo on the 24-hour heart rate response in
`patients on treatment for glaucoma. Am J
`Ophrhalmol, 2001; 132:626-632.
`23 Dickstein K, Aarsland T. Comparison of the
`effects of aqueous and gellan ophthalmic timolol on
`peak exercise performance in middle-aged men. Am
`J Ophrhalmol, 1996; 121:367-371.
`24 von der Ohe N. Stark M, Mayer 1-1 et al. How can
`the bioavailability oftimolol be enhanced? A pha!111a(cid:173)
`cokinetic pilot study of novel hydrogels. Graefes Arch.
`Clin Exp Ophrhalmol, 1996; 234:452-456.
`25 Mayer 1-1, von der Ohe N. Efficacy of a novel
`hydrogel formulation in human Yolunteers. Ophtltal(cid:173)
`mologica, 1'196; 210:101-103.
`26 Camras CB, Biro LZ, Toris CB. Prostaglandins
`and prostaglandin analogues. In (Zimmermann TJ
`eta/ eds) Textbook of Ocular Phammcology. Lippin(cid:173)
`cott-Rave, Philadalphia, 1997; pp. 315-328.
`27 MIMS (2002), ~lay, pp. 14.
`28 Brubaker RE Schoff EO, Nau CB eta!. Effects of
`AGN 192024. a new ocular hypotensive agent, on
`aqueous dynamics. Am.!Ophtha!mol, 2001; 131: 19-24.
`29 Woodward Dl'; Krauss AJ-1-P, Chen] eta/. The
`pharmacology ofbimatoprost (LurniganTl\!). Surv
`Ophthalmo!. 2001:45 (suppl. 4):S337-S345.
`30 DoughtY l\'1]. ilkdicines Update for Optical Practi(cid:173)
`tioners, Parr 10. 01'\"ICIAN, 2002; 223 (no5839): p21-23.
`31 DuBincr 1-lrn Cooke D. Dirks M ct a!. Efficacy
`and safe tv ofbirnatoprost in patients with elevated
`intraocular pressure: A 30-day comparison with
`latanoprost. Sum Ophrhalmol, 2001; 45 (suppl 4):
`S353-S360.
`32 Brandt JD, VanDenburgh Ai'vl, Chen K et ol.
`Comparison of once- nr twice-daily bimacoprost
`with twice-daily tirnolol in patients with elevated
`lOP: a 3-month clinical trial. Ophrhalmology, 2001;
`108:1023-1031.
`33 Alexander CL.l\lillcr SJ, Abel SR. Prostaglandin
`analog trertmcnt of glaucoma and ocular hyperten(cid:173)
`sion. Amt Phaml{ICO!ht7; 2002; 36:504-511.
`34 :lfedicines Compe11dium. Datapharrn Communi(cid:173)
`cations Ltd. 2002.
`
`+ Jlfichae/ 1 Doughty is professor of ocular
`pharmacology a11d physiology at the Depart(cid:173)
`ment of Visio11 Scimces Cfasgow-Cafedonion
`Uuiuersitv. The rmthor ha.r 110 pmp1it:trir)'
`imerests in a11y of the prorlurts mmtiot~erl
`
`wvvw.optometryonline.net
`
`LUPIN EX1036, Page 7