Lexicomp-martindale-Dorzolamide Hydrochloride

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16/4/2021 Lexicomp

Dorzolamide Hydrochloride (Martindale: The Complete Drug Reference)

Drug Nomenclature
Chemical Name: (4S,6S)-4-(Ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulphonamide 7,7-dioxide hydrochloride
Form and Weight: C10H16N2O4S3,HCl = 360.9
CAS: 120279-96-1 (dorzolamide); 130693-82-2 (dorzolamide hydrochloride)
Note: Use in Sport. Dorzolamide (ophthalmic use of carbonic anhydrase inhibitors is not prohibited) may be restricted in certain sports (see
Refer to ) and competitors should check with the appropriate sports authorities.
Pharmacopoeias: In Eur. (see Refer to ) and US.Ph. Eur. 9 ( Dorzolamide Hydrochloride ). A white or almost white, crystalline powder. Soluble
in water; very slightly soluble in anhydrous alcohol; slightly soluble in methyl alcohol. It exhibits polymorphism.USP 42 ( Dorzolamide
Hydrochloride ). A white to off-white crystalline powder. Soluble in water. Store at 15 degrees to 30 degrees. Protect from light.
Edit Dates: 11-Aug-1997; 07-Aug-1998; 04-Oct-2000; 29-Oct-2001; 27-May-2004; 24-May-2006; 12-Aug-2008; 23-Jul-2010; 21-Jan-2020

Synonyms
Dorzolamid Hidroklorür; Dorzolamida, hidrocloruro de; Dorzolamide, chlorhydrate de; Dorzolamidhydrochlorid; Dorzolamidi
hydrochloridum; L-671152 (dorzolamide); MK-0507; MK-507; ドルゾラミド塩酸塩

United States Adopted Names


Dorzolamide Hydrochloride

British Approved Names


Dorzolamide Hydrochloride [BANM]

International Nonproprietary Names


Dorzolamide Hydrochloride [rINNM (en)]
Dorzolamide, Chlorhydrate de [rINNM (fr)]
Dorzolamidi Hydrochloridum [rINNM (la)]
Hidrocloruro de dorzolamida [rINNM (es)]
Дорзоламида Гидрохлорид [rINNM (ru)]

Anatomic Therapeutic Chemical Classification


S01EC03

ATC Code (veterinary)


QS01EC03

Uses and Administration


Dorzolamide is a carbonic anhydrase inhibitor with actions similar to those of acetazolamide ( Refer to ). It is used in the management of
open-angle glaucoma, pseudo-exfoliative glaucoma, and ocular hypertension ( Refer to ), either alone or as an adjunct to a topical beta
blocker.
Dorzolamide is given as eye drops containing dorzolamide hydrochloride equivalent to 2% of the base. For monotherapy it is usually given
three times daily; a twice-daily regimen is recommended when used with a beta blocker.
(last reviewed 2010-07-23; last modified 2008-08-07)
References.
(last reviewed 2010-07-23; last modified 2010-07-06)
References
1. Lesk MR, et al.. Effectiveness and safety of dorzolamide-timolol alone or combined with latanoprost in open-angle glaucoma or ocular
hypertension.Ann Pharmacother. 2008; 42: 498–504. PubMed
2. Katz LJ, et al.. Efficacy and safety of brimonidine and dorzolamide for intraocular pressure lowering in glaucoma and ocular
hypertension.Curr Med Res Opin. 2007; 23: 2971–83. PubMed

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Adverse Effects, Treatment and Precautions


Adverse Effects and Precautions
Local ocular adverse effects may occur with dorzolamide eye drops and include conjunctivitis, keratitis, burning or stinging, eyelid
inflammation or irritation, and blurred vision. Corneal oedema and irreversible corneal decompensation have been reported in patients with
pre-existing chronic corneal defects and/or a history of intra-ocular surgery. There is also an increased potential for developing corneal
oedema in those with low endothelial cell counts. Hence, dorzolamide eye drops should be used with caution in these patient groups.
Dorzolamide may be absorbed systemically, resulting in adverse effects and precautions similar to those of acetazolamide (see Refer to ).
Other adverse effects reported are headache, bitter taste, epistaxis, fatigue, and nausea.
(last reviewed 2010-07-23; last modified 2010-07-06)
Porphyria
The Drug Database for Acute Porphyria, compiled by the Norwegian Porphyria Centre (NAPOS) and the Porphyria Centre Sweden, classifies
dorzolamide as probably not porphyrinogenic; it may be used as a drug of first choice and no precautions are needed.1
(last reviewed 2010-07-23; last modified 2011-11-14)
References
1. The Drug Database for Acute Porphyria. Available at: Link (accessed 25/10/11)

Interactions
Systemic absorption may occur after topical application of dorzolamide to the eye and there is a theoretical possibility of interactions similar
to those reported with acetazolamide (see Refer to ).
(last reviewed 2010-07-23; last modified 2008-08-07)

Pharmacokinetics
Systemic absorption occurs after topical application of dorzolamide to the eye. It accumulates in red blood cells during chronic dosing due to
binding to carbonic anhydrase and is about 33% bound to plasma proteins. Dorzolamide forms a single N-desethyl metabolite that is less
active and also accumulates in red blood cells where it binds mainly to the less active isoenzyme of carbonic anhydrase. Although
dorzolamide is mainly excreted unchanged in the urine, its metabolite is also excreted in the urine.
(last reviewed 2010-07-23; last modified 2011-01-02)
References.
(last reviewed 2010-07-23; last modified 2010-07-06)
References
1. Martens-Lobenhoffer J, Banditt P. Clinical pharmacokinetics of dorzolamide.Clin Pharmacokinet. 2002; 41: 197–205. PubMed

Preparations: Single-Ingredient
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
ARGENTINA: Dorlamida; Poenglausil¤; Trusopt;AUSTRALIA: Trusamide; Trusopt;AUSTRIA: Dorlazept; Dorzo-Vision; Trusopt;BELGIUM:
Trusopt;BRAZIL: Ocupress; Trusopt;CANADA: Trusopt;CHILE: Glaucotensil; Trusopt;CZECH REPUBLIC: Oftidor; Optipres¤; Optodrop¤;
Trusopt;DENMARK: Arzolamid; Dorzostill; Trusopt;FINLAND: Trusopt;FRANCE: Trusopt;GERMANY: Dorlazept; Dorzo-Vision; Trusopt;GREECE:
Dorolad; Odyral; Optodrop; Rezlod; Trusopt;HONG KONG: Dorzo; Trusopt;HUNGARY: Dorzolep; Nodom; Trusopt;INDIA: Dortas; Dorzox;
Ocudor;IRELAND: Trusopt;ISRAEL: Trusopt;ITALY: Dorzostill; Trusopt;MALAYSIA: Trusopt;MEXICO: Dorlenka; Iopzox; Oftilan; Piobaj;
Trusopt;NETHERLANDS: Dorzostill; Trusopt;NORWAY: Trusopt;NEW ZEALAND: Trusopt;PHILIPPINES: Trusopt;POLAND: Adolamid; Dolopt;
Dorzostill; Dropzol; Glautic; Nodofree; Nodom; Oftidor; Rozalin; Trusopt; Vizidor;PORTUGAL: Dorcil; Galax¤; Proglau¤; Trusopt;RUSSIAN
FEDERATION: Dorzolan (Дорзолан); Glaucopt (Глаукопт); Trusopt (Трусопт);SOUTH AFRICA: Glaucopress; Trusopt;SINGAPORE:
Trusopt;SPAIN: Trusopt;SWEDEN: Trusopt;SWITZERLAND: Dorlazept¤; Dorzo-Vision; Trusopt;THAILAND: Trusopt;TURKEY: Dorzamed;
Trusopt;UNITED KINGDOM: Eydelto; Trusopt;UKRAINE: Dorsamed (Дорзамед); Dorzol (Дорзол); Dorzoptic (Дорзоптик); Rezlod (Резлод);
Rozalin (Розалин);UNITED STATES: Trusopt;VENEZUELA: Dorzol; Glaucotensil D; Trusopt;

Preparations: Multi-Ingredient
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
ARGENTINA: Aliviapres; Cosopt; Dor-Timolol¤; Dorlamida T; Dorzoflax; Dorzolamida T; Glaucotensil TD; Press Out T; Timed D; Zopirol
DM;AUSTRALIA: Cosdor; Cosopt; Cozdol;AUSTRIA: Cosopt; Dorzastad; DorzoComp-Vision; Dorzolamide comp; Duokopt; Timsopt¤;BELGIUM:
Cosopt; Dualkopt; TensocMylan; Timoglaucon¤;BRAZIL: Cosopt; Drusolol; Glalfital; Glaucoftal¤; Pressaliv; Timosopt;CANADA: Apo-Dorzo-
Timop; Cosopt;CHILE: Cosopt; Doblefect; Dorsof T¤; Dortim; Dorzine¤; Glaucotensil T; Glausolets Plus; Tiof Plus;CZECH REPUBLIC: Amiptic;
Batidor¤; Cosopt; Dortimpos¤; Dorzogen Combi; Dozotima; Dualkopt; Optodrop Combi¤;DENMARK: Arzotilol¤; Cosopt; Costad; Dorzo Tim;
Duokopt; Timosopt¤;FINLAND: Cosopt; Duokopt; Glaukostad;FRANCE: Cosidime; Cosopt; Dualkopt;GERMANY: CosDuo; Cosopt; Dorzo Plus
T¤; DorzoComp-Vision; Dorzolamid comp¤; Duokopt;GREECE: Arutidor¤; Cosopt; Dorzoptic Plus; Dorzotim¤; Dotiz; Duokopt; Mardozia;

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Ophtha-biotic; Optodrop-Co; Phardinol; Tesol¤;HONG KONG: Apo-Dorzo-Timop; Cosopt; Mardozia;HUNGARY: Cosopt; DorzolEP Komb;
Dozopres Combi; Dozopticum Duo; Glamzolid; Kiranol;INDIA: Misopt; Ocudor-T;IRELAND: Claropt¤; Cosopt; Dortim¤;ISRAEL: Cosopt;
Dorzatol-Avenir; Timodor;ITALY: Cosopt;MALAYSIA: Cosopt;MEXICO: Anhigot; Besser¤; Cosopt; Eliptic; Krytantek; Trovost;NETHERLANDS:
Cosopt; Dortim; Dualkopt;NORWAY: Cosopt; Duokopt;NEW ZEALAND: Cosopt¤; Dortimopt; Dorzolatim¤;PHILIPPINES: Cosopt;POLAND:
Candotim; Cosopt; Dolopt Plus; Dortim; Dotiteva; Dozopres Combi; Dropzol Tim; Duokopt; Nodofree Combi; Nodom Combi; Oftidorix;
Rozacom; Tymolamid; Vizidor Duo;PORTUGAL: Cosopt; Duokopt; Protizol; Timosopt¤; Zycopt;RUSSIAN FEDERATION: Cosopt (Косопт);
Dortimol (Дортимол); Dorzolan Extra (Дорзолан Экстра); Dorzopt (Дорзопт); Dorzopt Plus (Дорзопт Плюс);SOUTH AFRICA: Cosopt; Glaumide
Co; Glauopt Co;SINGAPORE: Cosopt;SPAIN: CosDuo; Cosopt; Duokopt;SWEDEN: Cosopt; Costad¤; Duokopt;SWITZERLAND: Co-Dorzolamid¤;
Cosopt; DorzoComp-Vision; Duokopt;THAILAND: Cosopt;TURKEY: Arudor; Cosopt; Dorzasopt; Dorzotim; Oftomix; Tidomix¤; Tomec;
Xolatim;UNITED KINGDOM: Cosopt; Eylamdo;UKRAINE: Cosopt (Косопт); Dorzitim (Дорзітім); Dorzoptic Combi (Дорзоптик Комбі); Dorzotimol
(Дорзотимол); Rozacom (Розаком);UNITED STATES: Cosopt;VENEZUELA: Cosopt; Dobet; Glaucotensil T; Tidor; Tiof Plus;

Preparations: Pharmacopoeial
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
BP 2019: Dorzolamide and Timolol Eye Drops; Dorzolamide Eye Drops;USP 42: Dorzolamide Hydrochloride and Timolol Maleate Ophthalmic
Solution; Dorzolamide Hydrochloride Ophthalmic Solution;

Therapeutic Use
Miotics Mydriatics and Antiglaucoma Drugs

Last Updated 1/18/21

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