This document summarizes information on various drugs used to treat glaucoma, including apraclonidine hydrochloride, befunolol hydrochloride, brimonidine tartrate, and bimatoprost. It provides details on their chemical structures, pharmacological classification, indications for use, adverse effects, and proprietary products containing each drug. Caution is advised when using apraclonidine and brimonidine in patients with cardiovascular disease or depression due to potential adverse effects from systemic absorption. Brimonidine should also be used cautiously in children due to risk of serious systemic effects.
This document summarizes information on various drugs used to treat glaucoma, including apraclonidine hydrochloride, befunolol hydrochloride, brimonidine tartrate, and bimatoprost. It provides details on their chemical structures, pharmacological classification, indications for use, adverse effects, and proprietary products containing each drug. Caution is advised when using apraclonidine and brimonidine in patients with cardiovascular disease or depression due to potential adverse effects from systemic absorption. Brimonidine should also be used cautiously in children due to risk of serious systemic effects.
This document summarizes information on various drugs used to treat glaucoma, including apraclonidine hydrochloride, befunolol hydrochloride, brimonidine tartrate, and bimatoprost. It provides details on their chemical structures, pharmacological classification, indications for use, adverse effects, and proprietary products containing each drug. Caution is advised when using apraclonidine and brimonidine in patients with cardiovascular disease or depression due to potential adverse effects from systemic absorption. Brimonidine should also be used cautiously in children due to risk of serious systemic effects.
This document summarizes information on various drugs used to treat glaucoma, including apraclonidine hydrochloride, befunolol hydrochloride, brimonidine tartrate, and bimatoprost. It provides details on their chemical structures, pharmacological classification, indications for use, adverse effects, and proprietary products containing each drug. Caution is advised when using apraclonidine and brimonidine in patients with cardiovascular disease or depression due to potential adverse effects from systemic absorption. Brimonidine should also be used cautiously in children due to risk of serious systemic effects.
Pharmacopoeias. In US. Befunolol Hydrochloride (rINNM) ⊗ Preparations
USP 31 (Apraclonidine Hydrochloride). A white to off-white, Proprietary Preparations (details are given in Part 3) Béfunolol, Chlorhydrate de; Befunololi Hydrochloridum; BFE-60; odourless to practically odourless powder. Soluble 1 in 34 of wa- Arg.: Lumigan; Austral.: Lumigan; Austria: Lumigan; Belg.: Lumigan; ter, 1 in 74 of alcohol, and 1 in 13 of methyl alcohol; insoluble in Hidrocloruro de befunolol. 7-[2-Hydroxy-3-(isopropylami- Braz.: Lumigan; Canad.: Lumigan; Chile: Lumigan; Cz.: Lumigan; Denm.: chloroform, in ethyl acetate, and in hexanes. pH of a 1% solution no)propoxy]-2-benzofuranyl methyl ketone hydrochloride. Lumigan; Fin.: Lumigan; Fr.: Lumigan; Ger.: Lumigan; Gr.: Lumigan; Hong in water is between 5.0 and 6.6. Store in airtight containers. Pro- Kong: Lumigan; Hung.: Lumigan; India: Lumigan; Irl.: Lumigan; Israel: Lu- Бефунолола Гидрохлорид migan; Ital.: Lumigan; Malaysia: Lumigan†; Mex.: Lumigan; Neth.: Lumi- tect from light. C 16 H 21NO 4 ,HCl = 327.8. gan; Norw.: Lumigan; NZ: Lumigan; Philipp.: Lumigan; Pol.: Lumigan; C AS — 39552-01-7 (befunolol); 39543-79-8 (befunolol Port.: Lumigan; S.Afr.: Lumigan; Singapore: Lumigan; Spain: Lumigan; Swed.: Lumigan; Switz.: Lumigan; Thai.: Lumigan; Turk.: Lumigan; UK: Adverse Effects and Precautions hydrochloride). Lumigan; USA: Lumigan; Venez.: Lumigan. Adverse effects after perioperative instillation of apra- ATC — S01ED06. Multi-ingredient: Cz.: Ganfort; Gr.: Ganfort; Port.: Ganfort; UK: Gan- clonidine into the eye include hyperaemia, lid retrac- ATC Vet — QS01ED06. fort. tion, and mydriasis. Some patients may develop an ex- aggerated reduction in intra-ocular pressure. On O regular instillation an ocular intolerance reaction may H3C H Brimonidine Tartrate (BANM, USAN, rINNM) occur, characterised by hyperaemia, ocular pruritus, in- N CH3 AGN-190342-LF; Brimonidin Tartrat; Brimonidine, Tartrate de; creased lachrymation, ocular discomfort, and oedema O Brimonidini Tartras; Tartrato de brimonidina; UK-14304-18. 5- of the lids and conjunctiva; treatment should be O CH3 Bromo-6-(2-imidazolin-2-ylamino)quinoxaline D-tartrate. stopped if these symptoms occur. Other adverse effects OH Бримонидина Тартрат reported include dry mouth and nose, conjunctivitis, C 11 H 10BrN 5 ,C 4 H 6 O 6 = 442.2. conjunctival blanching, blurred vision, asthenia, head- C AS — 59803-98-4 (brimonidine); 79570-19-7 (brimoni- ache, and taste disturbances. (befunolol) dine tartrate). Systemic absorption can occur after application to the ATC — S01EA05. eye and may result in adverse effects similar to those of ATC Vet — QS01EA05. Profile clonidine (p.1247). Cardiovascular effects have been Befunolol is a beta blocker (p.1225). It is used as the hydrochlo- reported; therefore apraclonidine should be used with ride in the management of ocular hypertension and open-angle glaucoma (p.1873). Eye drops containing befunolol hydrochlo- Br caution in patients with severe cardiovascular disease, H ride 0.25%, 0.5%, or 1% are instilled twice daily. N N including hypertension, and in patients with a history N of vasovagal attacks. Drowsiness may also occur. De- Preparations pression has rarely been associated with use of apraclo- Proprietary Preparations (details are given in Part 3) NH Austria: Glauconex†; Gr.: Thilonium†; Ital.: Betaclar; Jpn: Bentos; Mon.: N nidine and it should be used with caution in depressed Bentos. patients. (brimonidine)
Interactions Bimatoprost (BAN, USAN, rINN)
Systemic absorption may occur after topical applica- Adverse Effects and Precautions AGN-192024; Bimatoprostum. (Z)-7-{(1R,2R,3R,5S)-3,5-Dihy- As for Apraclonidine Hydrochloride, p.1878. tion of apraclonidine to the eye and there is a theoreti- droxy-2-[(1E,3S)-3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl}- cal possibility of interactions similar to those reported N-ethyl-5-heptenamide. In children. Systemic adverse effects, occasionally severe,1 with clonidine (p.1248). Since the effects of apracloni- have been reported in children treated with brimonidine eye Биматопрост drops. In one study2 adverse effects were reported in 70 of 83 dine on circulating catecholamines are unknown, li- C 25 H 37NO 4 = 415.6. children given adjunctive brimonidine, the most common effects censed product information recommends that MAOIs C AS — 155206-00-1. being lethargy and excessive sleepiness; other effects included should not be given with apraclonidine; tricyclic and ATC — S01EE03. ocular irritation and blurred vision. Hypothermia occurred in a related antidepressants and systemic sympathomimet- ATC Vet — QS01EE03. few cases, mainly in older children. Effects suggesting CNS de- ics should also be avoided or used with caution. pression, such as cyanosis and breathing difficulty, were rare, and were most likely in children less than 6 years of age or HO H weighing less than 20 kg. Alternative medication should be con- Uses and Administration H N CH3 sidered in this group. In the UK, licensed product information Apraclonidine is an alpha2-adrenoceptor agonist de- contra-indicates use in neonates and infants under 2 years of age; rived from clonidine (p.1247). It reduces intra-ocular use in children under 12 years of age is not recommended. O 1. Sztajnbok J. Failure of naloxone to reverse brimonidine-induced pressure when instilled into the eye and is used in pa- coma in an infant. J Pediatr 2002; 140: 485–6. tients undergoing eye surgery, and as an adjunct in the H 2. Al-Shahwan S, et al. Side-effect profile of brimonidine tartrate HO HO H management of glaucoma (p.1873). The reduction in in children. Ophthalmology 2005; 112: 2143–8. intra-ocular pressure begins within an hour of instilla- tion and is maximal after about 3 to 5 hours. Interactions As for Apraclonidine Hydrochloride, p.1878. Apraclonidine is used as the hydrochloride, but the strength of an ophthalmic solution is usually expressed Adverse Effects and Precautions Uses and Administration in terms of the base. Apraclonidine hydrochloride As for Latanoprost, p.1882. Ocular pruritus is common. Hyper- Brimonidine is an alpha2-adrenoceptor agonist with 11.5 mg is equivalent to about 10 mg of apraclonidine. tension and headache also commonly occur. actions and uses similar to those of apraclonidine To control or prevent a postoperative increase in intra- Pharmacokinetics (p.1878). It is used to lower intra-ocular pressure in pa- Small amounts of bimatoprost are absorbed from eye drops, with tients with open-angle glaucoma or ocular hyperten- ocular pressure in patients undergoing anterior seg- peak blood concentrations seen within 10 minutes of dosing. Bi- ment laser surgery, a 1% solution is instilled into the matoprost is metabolised by oxidation, de-ethylation and glu- sion (p.1873), as an alternative or adjunct to topical eye one hour before surgery and again immediately curonidation and is excreted mainly in the urine with about 25% beta blocker therapy. It may also be used as adjunctive upon completion of surgery. appearing in the faeces. The elimination half-life is 45 minutes. therapy in patients with raised intra-ocular pressure not Uses and Administration controlled by topical monotherapy with other drugs For short-term adjunctive therapy in patients with Bimatoprost is a synthetic prostamide, a fatty-acid amide that is such as latanoprost and travoprost. The reduction in in- raised intra-ocular pressure not controlled by conven- structurally related to dinoprost (prostaglandin F2 ). It is used to tra-ocular pressure is maximal about 2 hours after top- tional therapy, a 0.5% solution may be instilled three reduce intra-ocular pressure in the treatment of open-angle glau- ical use. times daily. coma and ocular hypertension (p.1873). Reduction in pressure starts about 4 hours after instillation and is maximal within 8 to In the management of glaucoma or ocular hyperten- There is a loss of effect over time (tachyphylaxis) with 12 hours; the effect lasts for at least 24 hours. It is given once sion, eye drops containing brimonidine tartrate 0.1, apraclonidine and the benefit in most patients lasts for daily in the evening as a 0.03% ophthalmic solution. 0.15, or 0.2% are instilled two or three times daily. less than a month. ◊ References. Glaucoma. References to the use of brimonidine in glaucoma Preparations 1. Sherwood M, et al. Six-month comparison of bimatoprost once- and raised intra-ocular pressure. daily and twice-daily with timolol twice-daily in patients with 1. Adkins JC, Balfour JA. Brimonidine: a review of its pharmaco- USP 31: Apraclonidine Ophthalmic Solution. elevated intraocular pressure. Surv Ophthalmol 2001; 45 (suppl logical properties and clinical potential in the management of 4): S361–S368. open-angle glaucoma and ocular hypertension. Drugs Aging Proprietary Preparations (details are given in Part 3) 2. Brandt JD, et al. Comparison of once- or twice-daily bimatoprost 1998; 12: 225–41. Arg.: Iopidine†; Austral.: Iopidine; Austria: Iopidine; Belg.: Iopidine; with twice-daily timolol in patients with elevated IOP: a 3-month 2. Cantor LB. The evolving pharmacotherapeutic profile of brimo- Braz.: Iopidine†; Canad.: Iopidine; Chile: Iopidine†; Cz.: Iopidine†; clinical trial. Ophthalmology 2001; 108: 1023–31. nidine, an alpha 2-adrenergic agonist, after four years of contin- Denm.: Iopidine; Fin.: Iopidine; Fr.: Iopidine; Ger.: Iopidine; Gr.: Iopidine; Hong Kong: Iopidine; India: Alfadrops; Irl.: Iopidine; Israel: Iopidine; Ital.: 3. Whitcup SM, et al. A randomised, double masked, multicentre uous use. Expert Opin Pharmacother 2000; 1: 815–34. Iopidine; Jpn: Iopidine†; Malaysia: Iopidine†; Mex.: Iopidine; Neth.: Iopi- clinical trial comparing bimatoprost and timolol for the treat- 3. David R. Brimonidine (Alphagan): a clinical profile four years dine; Norw.: Iopidine; NZ: Iopidine†; Port.: Iopidine; S.Afr.: Iopidine; Sin- ment of glaucoma and ocular hypertension. Br J Ophthalmol after launch. Eur J Ophthalmol 2001; 11 (suppl 2): S72–S77. gapore: Iopidine; Spain: Iopimax; Swed.: Iopidine; Switz.: Iopidine; Turk.: 2003; 87: 57–62. 4. Lee DA, Gornbein JA. Effectiveness and safety of brimonidine Iopidine; UK: Iopidine; USA: Iopidine; Venez.: Iopidine†. 4. Cantor LB, et al. Intraocular pressure-lowering efficacy of bi- as adjunctive therapy for patients with elevated intraocular pres- matoprost 0.03% and travoprost 0.004% in patients with glauco- sure in a large, open-label community trial. J Glaucoma 2001; ma or ocular hypertension. Br J Ophthalmol 2006; 90: 1370–3. 10: 220–6. Befunolol Hydrochloride/Cyclopentolate Hydrochloride 1879 5. Katz LJ. Twelve-month evaluation of brimonidine-purite versus Carbachol (BAN, rINN) Glaucoma and ocular hypertension. Carbachol is some- brimonidine in patients with glaucoma or ocular hypertension. J times used as an alternative to pilocarpine in the management of Glaucoma 2002; 11: 119–26. Carbach.; Carbacholi Cloridum; Carbacholine; Carbacholum; glaucoma (p.1873) when resistance or intolerance to pilocarpine 6. Sherwood MB, et al. Twice-daily 0.2% brimonidine-0.5% Carbacholum Chloratum; Carbacol; Choline Chloride Car- develops. It is also instilled into the anterior chamber of the eye timolol fixed-combination therapy vs monotherapy with timolol bamate; Karbachol; Karbacholis; Karbakol; Karbakoli; Karbamino- or brimonidine in patients with glaucoma or ocular hypertension: (intracameral instillation) to minimise postoperative rises in in- a 12-month randomized trial. Arch Ophthalmol 2006; 124: choliny chlorek. O-Carbamoylcholine chloride; (2-Carbamoy- tra-ocular pressure associated with ocular surgery, and some1,2 1230–8. loxyethyl)trimethylammonium chloride. have found it to be more effective than acetylcholine. 7. Fung AT, et al. Meta-analysis of randomised controlled trials Карбахол 1. Ruiz RS, et al. Effects of carbachol and acetylcholine on intra- comparing latanoprost with brimonidine in the treatment of muscular pressure after cataract extraction. Am J Ophthalmol open-angle glaucoma, ocular hypertension or normal-tension C 6 H 15 ClN 2 O 2 = 182.6. 1989; 107: 7–10. glaucoma. Br J Ophthalmol 2007; 91: 62–8. C AS — 51-83-2. 2. Hollands RH, et al. Control of intraocular pressure after cataract Preparations ATC — N07AB01; S01EB02. extraction. Can J Ophthalmol 1990; 25: 128–32. ATC Vet — QA03AB92; QN07AB01; QS01EB02. Preparations Proprietary Preparations (details are given in Part 3) Arg.: Alphagan; Brimo-Klonal; Brimopress; Oftalmotonil; Austral.: Alpha- USP 31: Carbachol Intraocular Solution; Carbachol Ophthalmic Solution. gan; Enidin; Austria: Alphagan; Belg.: Alphagan; Braz.: Alphagan; Canad.: Alphagan; Chile: Agglad Ofteno; Alphagan; Brimopress; Cz.: Alphagan; CH3 Proprietary Preparations (details are given in Part 3) Denm.: Alphagan; Fin.: Alphagan; Fr.: Alphagan; Ger.: Alphagan; Gr.: Al- O Arg.: Miostat; Austral.: Miostat; Belg.: Miostat; Braz.: Miostat†; Canad.: + CH3 − Carbastat†; Miostat; Cz.: Jestryl†; Miostat; Fin.: Doryl†; Ger.: Carbamann; phagan; Benil; Brimodine; Brinal; Brinidin; Hong Kong: Alphagan; Hung.: Alphagan†; India: Brimodin; Iobrim; Irl.: Alphagan; Israel: Alphagan; Ital.: N Cl Doryl†; Jestryl†; Hong Kong: Miostat†; Hung.: Miostat; Israel: Miostat; Alphagan; Malaysia: Alphagan; Mex.: Agglad; Alphagan; Nor-Tenz; Neth.: H 2N O CH3 Ital.: Mioticol; Malaysia: Miostat; Neth.: Miostat; Philipp.: Miostat; Pol.: Alphagan; Norw.: Alphagan; NZ: Alphagan; Philipp.: Alphagan; Pol.: Al- Miostat; S.Afr.: Miosys†; Singapore: Miostat; Swed.: Isopto Karbakolin; Mi- phagan; Port.: Alphagan; S.Afr.: Alphagan; Singapore: Alphagan; Spain: ostat; Switz.: Doryl†; Miostat; Thai.: Miostat; Turk.: Miostat; USA: Carb- Alphagan; Swed.: Alphagan; Switz.: Alphagan; Thai.: Alphagan; Turk.: Al- NOTE. CAR is a code approved by the BP 2008 for use on single astat; Miostat; Venez.: Miostat†. phagan; UK: Alphagan; USA: Alphagan; Venez.: Agglad Ofteno; Alphagan. unit doses of eye drops containing carbachol where the individ- Multi-ingredient: Ital.: Mios. Multi-ingredient: Arg.: Combigan; Austral.: Combigan; Braz.: Com- ual container may be too small to bear all the appropriate label- bigan; Canad.: Combigan; Chile: Combigan; Cz.: Combigan; Gr.: Com- ling information. bigan; Hung.: Combigan; India: Brimodin P; Irl.: Combigan; Mex.: Com- Pharmacopoeias. In Chin., Eur. (see p.vii), and US. bigan-D; NZ: Combigan; Port.: Combigan; Switz.: Combigan; UK: Combigan; USA: Combigan. Ph. Eur. 6.2 (Carbachol). A white or almost white, crystalline, Cyclopentolate Hydrochloride hygroscopic powder. Very slightly soluble in water; sparingly soluble in alcohol; practically insoluble in acetone. Store in air- (BANM, rINNM) tight containers. Protect from light. Ciklopentolát-hidroklorid; Ciklopentolato hidrochloridas; Clorid- Brinzolamide (BAN, USAN, rINN) ⊗ USP 31 (Carbachol). A white powder. Freely soluble in water; sparingly soluble in alcohol; practically insoluble in chloroform rato de Ciclopentolato; Cyclopentolate, chlorhydrate de; Cy- clopentolati hydrochloridum; Cyklopentolát hydrochlorid; AL-4862; Brintsolamidi; Brinzolamid; Brinzolamida; Brinzolami- and in ether. Store in airtight containers. Cyklopentolathydroklorid; Hidrocloruro de ciclopentolato; Siklo- dum. (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H- Incompatibility. Chlorocresol (0.025 to 0.1%) and chlorobuta- pentolat Hidroklorür; Syklopentolaattihydrokloridi. 2-Dimethyl- thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide. nol (0.5%) were both found to be incompatible with a solution of aminoethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate hydro- Бринзоламид carbachol (0.8%) and sodium chloride (0.69%), very slight pre- chloride. C 12 H 21N 3 O 5 S 3 = 383.5. cipitates forming on heating and increasing on standing.1 Циклопентолата Гидрохлорид C AS — 138890-62-7. 1. PSGB Lab Report No.911 1962. C 17 H 25 NO 3 ,HCl = 327.8. ATC — S01EC04. Adverse Effects, Treatment, and Precautions C AS — 512-15-2 (cyclopentolate); 5870-29-1 (cyclopen- ATC Vet — QS01EC04. As described for choline esters under Acetylcholine Chloride, tolate hydrochloride). p.1877. Carbachol has substantial nicotinic activity which may be unmasked by the use of atropine to counteract muscarinic ef- ATC — S01FA04. fects. ATC Vet — QS01FA04. H2N O Carbachol also produces adverse effects and requires precautions S similar to those of other miotics such as pilocarpine (p.1885) O CH3 when used in the eye, but may produce more ciliary spasm than O H pilocarpine. S N CH3 N Effects on the gastrointestinal tract. Fatal oesophageal O rupture has been reported1 after subcutaneous injection of carba- CH3 O OH S chol to relieve urinary retention. N 1. Cochrane P. Spontaneous oesophageal rupture after carbachol O therapy. BMJ 1973; 1: 463–4. CH3 O Overdosage. Life-threatening attacks of profuse sweating, in- testinal cramps, explosive defaecation, hypothermia, hypoten- (cyclopentolate) Pharmacopoeias. In US. sion, and bradycardia occurred in a 36-year-old man after delib- USP 31 (Brinzolamide). A white or almost white powder. Insol- erate poisoning with 30 to 40 mg of carbachol.1 The patient’s 10- NOTE. CYC is a code approved by the BP 2008 for use on single year-old son had died after poisoning with a similar dose of car- unit doses of eye drops containing cyclopentolate hydrochloride uble in water; slightly soluble in alcohol and in methyl alcohol. bachol. where the individual container may be too small to bear all the 1. Sangster B, et al. Two cases of carbachol intoxication. Neth J appropriate labelling information. PHNCYC is a similar code Adverse Effects and Precautions Med 1979; 22: 27–8. approved for eye drops containing phenylephrine hydrochloride As for Dorzolamide, p.1880. Interactions and cyclopentolate hydrochloride. Effects on the eyes. Corneal oedema has been noted in the Pharmacopoeias. In Eur. (see p.vii), Jpn, and US. NSAIDs. Licensed UK product information for acetylcholine Ph. Eur. 6.2 (Cyclopentolate Hydrochloride). A white or almost eyes of 2 patients after the long-term use of brinzolamide 1% eye chloride ophthalmic preparations states that there have been re- drops;1 both patients recovered after brinzolamide was stopped. white, crystalline powder. Very soluble in water; freely soluble in ports that acetylcholine and carbachol were ineffective when alcohol. A 1% solution in water has a pH of 4.5 to 5.5. 1. Zhao JC, Chen T. Brinzolamide induced reversible corneal de- used in patients treated with topical (ophthalmic) NSAIDs. compensation. Br J Ophthalmol 2005; 89: 389–90. USP 31 (Cyclopentolate Hydrochloride). A white crystalline Uses and Administration powder, which develops a characteristic odour on standing. Very Uses and Administration Carbachol, a choline ester, is a quaternary ammonium parasym- soluble in water; freely soluble in alcohol; insoluble in ether. pH pathomimetic with the muscarinic and nicotinic actions of ace- of a 1% solution in water is between 4.5 and 5.5. Store at a tem- Brinzolamide is a carbonic anhydrase inhibitor with tylcholine (p.1877). It is not inactivated by cholinesterases so its perature not exceeding 8° in airtight containers. actions and uses similar to those of dorzolamide actions are more prolonged than those of acetylcholine. (p.1880). It is used to reduce intra-ocular pressure in Carbachol has a miotic action and is usually given intra-ocularly Adverse Effects, Treatment, and Precau- the management of open-angle glaucoma and ocular to produce miosis in ocular surgery and to reduce postoperative tions hypertension (p.1873), either alone or as adjunctive rises in intra-ocular pressure; up to 0.5 mL of a 0.01% solution is As for Atropine Sulfate, p.1219. therapy with a topical beta blocker. A 1% suspension is instilled into the anterior chamber of the eye (intracameral instil- lation). The maximum degree of miosis is usually obtained with- Eye drops of cyclopentolate hydrochloride may cause instilled into the eye two or three times daily. in 2 to 5 minutes of intra-ocular instillation and miosis lasts for temporary irritation. Glaucoma. References. 24 hours. 1. Cvetkovic RS, Perry CM. Brinzolamide : a review of its use in Eye drops containing up to 3% of carbachol have also been used Abuse. Cyclopentolate eye drops have been abused.1 One of 2 the management of primary open-angle glaucoma and ocular hy- patients who did so had been instilling 200 to 400 drops of cy- to lower intra-ocular pressure in glaucoma, usually three times pertension. Drugs Aging 2003; 20: 919–47. clopentolate into both eyes daily for about 4 months, presumably daily with other miotics (see below). Miosis occurs within 10 to 20 minutes of instillation and lasts for 4 to 8 hours; reduction in for its CNS effects, and experienced intense nausea, vomiting, Preparations weakness, and tremors on withdrawal. intra-ocular pressure lasts for 8 hours. USP 31: Brinzolamide Ophthalmic Suspension. 1. Sato EH, et al. Abuse of cyclopentolate hydrochloride (Cyc- Carbachol has been used for the treatment of urinary retention logyl) drops. N Engl J Med 1992; 326: 1363–4. Proprietary Preparations (details are given in Part 3) Arg.: Azopt; Austral.: Azopt; Austria: Azopt; Belg.: Azopt; Braz.: Azopt; including postoperative urinary retention. It has also been used in some countries for the treatment of decreased gastrointestinal Hypersensitivity. Two children developed hypersensitivity re- Canad.: Azopt; Chile: Azopt; Cz.: Azopt; Denm.: Azopt; Fin.: Azopt; Fr.: Azopt; Ger.: Azopt; Gr.: Azopt; Hong Kong: Azopt; Hung.: Azopt; In- motility. actions shortly after the instillation of 1% cyclopentolate hydro- don.: Azopt; Irl.: Azopt; Israel: Azopt; Ital.: Azopt; Malaysia: Azopt; chloride eye drops into each eye.1 Both children initially had a Mex.: Azopt; Neth.: Azopt; Norw.: Azopt; NZ: Azopt; Philipp.: Azopt; Dry mouth. Carbachol has been used as an alternative to pilo- facial rash but in one of them the rash later spread to include the Pol.: Azopt; Port.: Azopt; Rus.: Azopt (Азопт); S.Afr.: Azoptic; Singa- carpine in the treatment of radiation-induced xerostomia.1 The arms and legs and was accompanied by mild breathlessness. pore: Azopt; Spain: Azopt; Swed.: Azopt; Switz.: Azopt; Thai.: Azopt; overall treatment of dry mouth is discussed on p.2140. Turk.: Azopt; UK: Azopt; USA: Azopt; Venez.: Azopt. 1. Jones LWJ, Hodes DT. Possible allergic reactions to cyclopen- 1. Joensuu H. Treatment for post-irradiation xerostomia. N Engl J tolate hydrochloride: case reports with literature review of uses Med 1994; 330: 141–2. and adverse reactions. Ophthalmic Physiol Opt 1991; 11: 16–21.
The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii)