ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
نسخه الکترونیک
medimedia.ir

Dorzolamide: Drug information

Dorzolamide: Drug information
(For additional information see "Dorzolamide: Patient drug information" and see "Dorzolamide: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Trusopt [DSC]
Brand Names: Canada
  • APO-Dorzolamide;
  • JAMP-Dorzolamide;
  • MED-Dorzolamide;
  • SANDOZ Dorzolamide;
  • Trusopt;
  • Trusopt (Preservative Free)
Pharmacologic Category
  • Carbonic Anhydrase Inhibitor (Ophthalmic);
  • Ophthalmic Agent, Antiglaucoma
Dosing: Adult
Ocular hypertension/glaucoma

Ocular hypertension/glaucoma (open-angle): Ophthalmic: Instill 1 drop in the affected eye(s) 3 times daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling.

CrCl <30 mL/minute: Use is not recommended (has not been studied).

Dorzolamide and its metabolite (N-desethyl: less potent than parent) are excreted renally. Patients with renal impairment, particularly neonates and geriatric patients, should be monitored carefully for untoward effects due to reduced dorzolamide elimination.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling (have not been studied); use with caution.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Dorzolamide: Pediatric drug information")

Intraocular pressure reduction

Intraocular pressure reduction:

Monotherapy: Infants, Children, and Adolescents: Ophthalmic: Instill 1 drop to affected eye(s) 3 times daily (Ref).

Combination therapy (with latanoprost): Limited data available: Infants, Children, and Adolescents: Ophthalmic: Instill 1 drop to affected eye(s) 2 times daily (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling.

CrCl <30 mL/minute: All patients: Use is not recommended (has not been studied).

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.

Dermatologic: Skin rash

Gastrointestinal: Bitter taste (~25% following administration), nausea

Genitourinary: Urolithiasis

Hypersensitivity: Local ocular hypersensitivity reaction (~10%)

Nervous system: Fatigue, headache

Neuromuscular & skeletal: Asthenia

Ocular: Burning sensation of eyes (~33%), eye discomfort (~33%), stinging of eyes (~33%), superficial punctate keratitis (10% to 15%), blurred vision (1% to 5%), conjunctivitis (1% to 5%), eyelid irritation (1% to 5%), eye redness (1% to 5%), lacrimation (1% to 5%), photophobia (1% to 5%), xerophthalmia (1% to 5%), iridocyclitis

<1%, postmarketing and/or case reports: Angioedema, bronchospasm, choroidal detachment (following filtration procedures), contact dermatitis, crusting of eyelid, dizziness, dyspnea, epistaxis, myopia (transient), ocular pain, paresthesia, pruritus, Stevens-Johnson syndrome, throat irritation, toxic epidermal necrolysis, urticaria, xerostomia

Contraindications

Hypersensitivity to dorzolamide or any component of the formulation

Warnings/Precautions

Concerns related to adverse effects:

• Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.

• Ocular effects: Local ocular adverse effects (primarily conjunctivitis and lid reactions) were reported with chronic administration; many resolved upon discontinuation of drug therapy. Choroidal detachment has been reported after filtration procedures.

• Sulfonamide (“sulfa”) allergy: Dorzolamide is a sulfonamide; although administered ocularly, systemic absorption may occur and could result in hypersensitivity. Discontinue use if signs of hypersensitivity or a serious reaction occur.

• Systemic effects: Systemic absorption and adverse effects (similar to sulfonamides) including, blood dyscrasias, Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias may occur with ophthalmic use.

Disease-related concerns:

• Corneal endothelium: Use with caution in patients with low endothelial cell counts; may be at increased risk of corneal edema.

• Hepatic impairment: Use with caution in patients with hepatic impairment (has not been studied).

• Renal impairment: Use is not recommended in patients with severe renal impairment (CrCl <30 mL/minute) (has not been studied).

Special populations:

• Contact lens wearers: Some products contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.

Other warnings/precautions:

• Appropriate use: Should be used in combination with therapeutic interventions for the treatment of acute angle-closure glaucoma.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Ophthalmic:

Trusopt: 2% (10 mL [DSC])

Generic: 2% (10 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Dorzolamide HCl Ophthalmic)

2% (per mL): $1.80 - $6.68

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Trusopt: 2% (5 mL) [contains benzalkonium chloride]

Trusopt (Preservative Free): 2% (0.2 mL, 5 mL)

Generic: 2% (5 mL, 10 mL)

Administration: Adult

Ophthalmic: If more than one topical ophthalmic drug is being used, administer the drugs at least 5 minutes apart. Remove contact lens prior to administration and wait 15 minutes before reinserting. Avoid allowing the tip of the dispensing container to contact the eye or surrounding structures. Use eyelid closure or nasolacrimal occlusion when applying topical medications to reduce systemic absorption.

Administration: Pediatric

Ophthalmic: Wash hands before use. Unscrew the cap by turning in the direction of the arrows on top of the cap. Pull lower eyelid down slightly to form a pocket for the eye drop and tilt head back; administer 1 drop. Apply gentle pressure to lacrimal sac immediately following instillation (1 minute) or instruct patient to gently close eyelid after administration to decrease systemic absorption of ophthalmic drops (Ref). Avoid contact of bottle tip with skin or eye; ocular solutions can become contaminated by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may occur from using contaminated solutions. Some solutions contain benzalkonium chloride; remove contact lenses prior to administration and wait at least 15 minutes after instillation before reinserting soft contact lenses. If more than one topical ophthalmic drug is being used, separate administration by at least 5 minutes.

Use: Labeled Indications

Ocular hypertension/glaucoma (open-angle): Treatment of elevated intraocular pressure.

Metabolism/Transport Effects

Substrate of CYP2C9 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Risk C: Monitor therapy

Amantadine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Amantadine. Risk C: Monitor therapy

Carbonic Anhydrase Inhibitors: May enhance the adverse/toxic effect of other Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Risk X: Avoid combination

Pregnancy Considerations

Because information related to dorzolamide use in pregnancy is limited, other agents may be preferred for the treatment of glaucoma in pregnant patients. Use of topical carbonic anhydrase inhibitors may be considered after the first trimester. In general, if ophthalmic agents are needed in pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease exposure to the fetus (Belkin 2020; Strelow 2020).

Breastfeeding Considerations

It is not known if dorzolamide is present in breast milk.

In general, topical carbonic anhydrase inhibitors are considered compatible with breastfeeding. Administering after breastfeeding may help decrease potential exposure to the infant via breast milk (Belkin 2020; Strelow 2020).

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Monitoring Parameters

Ophthalmic exams (optic nerve and visual field assessment), serial measurement of intraocular pressure (IOP). Frequency of follow up based upon whether target IOP achieved, if there is any progression of damage, and how long disease has been controlled (AAO 2019).

Mechanism of Action

Reversible inhibition of the enzyme carbonic anhydrase II and IV in the ciliary epithelium resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor to reduce intraocular pressure.

Pharmacokinetics (Adult Data Unless Noted)

Duration of action: 8 to 12 hours

Absorption: Topical: Reaches systemic circulation where it accumulates in RBCs during chronic dosing as a result of binding to CA-II

Distribution: In RBCs during chronic administration

Protein binding: ~33%

Metabolism: To N-desethyl metabolite (less potent than parent drug)

Half-life elimination: Terminal RBC half-life: 147 days; washes out of RBCs nonlinearly, resulting in a rapid decline of drug concentration initially, followed by a slower elimination phase with a half-life of about 4 months

Excretion: Urine (as unchanged drug and metabolite, N-desethyl)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Apisopt | Trusopt | Xola;
  • (AR) Argentina: Biodrop | Trusopt;
  • (AT) Austria: Dorlazept | Dorzo vision | Trusopt;
  • (AU) Australia: Apo dorzolamide | Trusamide | Trusopt;
  • (BE) Belgium: Dorzolamide Mylan | Trusopt;
  • (BF) Burkina Faso: Ozolamide;
  • (BG) Bulgaria: Dorzopt | Trusopt;
  • (BR) Brazil: Andrum | Cloridrato de dorzolamida | Dorzal | Ocupress | Pert | Trusopt;
  • (CH) Switzerland: Dorzo vision | Dorzolamid Teva | Trusopt;
  • (CI) Côte d'Ivoire: Ozolamide | Proglau | Xola;
  • (CL) Chile: Dorlenka | Dorzolamida | Dorzox | Glaucotensil | Trusopt;
  • (CO) Colombia: Dorzamid | Dorzodel | Dorzolam | Dorzopres | Dorzovision | Glaucotensil d | Trusopt;
  • (CZ) Czech Republic: Dorzolamid olikla | Oftidor | Trusopt | Vizidor;
  • (DE) Germany: Dimaz | Dorzo vision | Dorzolamid 1a pharma | Dorzolamid Actavis | Dorzolamid al | Dorzolamid dr mann | Dorzolamid Heumann | Dorzolamid hexal | Dorzolamid Hormosan | Dorzolamid micro labs | Dorzolamid ratiopharm | Dorzolamid sandoz | Dorzolamid stada | Dorzolamid stulln | Trusopt;
  • (DO) Dominican Republic: Glaucotensil d | Iripress | Trusopt;
  • (EC) Ecuador: Dorlamida | Trusopt;
  • (EE) Estonia: Dorzolamide | Trusopt | Vizidor;
  • (EG) Egypt: Ozolamide | Ozolzmide | Queenzolamide | Xola;
  • (ES) Spain: Dorzolamida | Dorzolamida aristo | Dorzolamida kern pharma | Dorzolamina Colirteva | Trusopt;
  • (ET) Ethiopia: Dorzolamide HCL | Xola;
  • (FI) Finland: Dorzolamid Actavis | Dorzolamid mylan | Dorzolamid ratiopharm | Dorzolamide teva | Trusopt;
  • (FR) France: Dorzolamide Actavis | Dorzolamide biogaran | Dorzolamide Chauvin | Dorzolamide Cristers | Dorzolamide eg | Dorzolamide Mylan | Dorzolamide teva | Trusopt;
  • (GB) United Kingdom: Dorzolamide | Dorzolamide hydrochloride sandoz | Dorzolamide teva | Eydelto | Trusopt | Vizidor;
  • (GR) Greece: Dorolad | Optodrop | Trusopt;
  • (HK) Hong Kong: Dorzo | Trusopt;
  • (HR) Croatia: Dorvis | Dorzol | Trusopt;
  • (HU) Hungary: Dorzolep | Nodom | Trusopt;
  • (IE) Ireland: Dorzolamide Actavis | Trusopt;
  • (IL) Israel: Trusopt;
  • (IN) India: Arodor | Dortas | Dorzotry | Dorzox | Endor | Monosopt | Ocudor | Trusopt;
  • (IQ) Iraq: Dorzimid;
  • (IT) Italy: Dorzoclar | Dorzolamide | Dorzolamide Actavis | Dorzolamide doc generi | Dorzolamide Mylan | Dorzolamide ratiopharm | Dorzolamide tubilux pharma | Dorzostill | Trusopt | Zoliop;
  • (JO) Jordan: Apisopt | Daromed | Optodrop | Ozolamide | Trusopt;
  • (JP) Japan: Trusopt;
  • (KE) Kenya: Xola;
  • (KR) Korea, Republic of: Dozol | Trusopt;
  • (KW) Kuwait: Trusopt | Xola;
  • (LB) Lebanon: Dorzolamide bgr | Trusopt;
  • (LT) Lithuania: Dorzolamide Actavis | Dorzolamide portfarma | Nodofree | Nodom | Oftidor | Trusopt;
  • (LU) Luxembourg: Trusopt;
  • (LV) Latvia: Dorzolamide Actavis | Dorzolamide portfarma | Nodom | Oftidor | Sakor | Trusopt;
  • (MA) Morocco: Trusopt | Xola;
  • (MX) Mexico: Dorlenka | Dorzolamida | Drendor Tec | Iopzox ofteno | Pio Baj | Piobaj | Truglad | Trusopt;
  • (MY) Malaysia: Lamisopt | Trusopt;
  • (NG) Nigeria: Dorsun;
  • (NL) Netherlands: Dorzolamide | Dorzolamide Actavis | Dorzolamide Cf | Dorzolamide Mylan | Dorzolamide Sandoz | Trusmono | Trusopt;
  • (NO) Norway: Dorzolamid ratiopharm | Trusopt;
  • (NZ) New Zealand: Trusopt;
  • (OM) Oman: Xola;
  • (PE) Peru: Atensor | Dorlip | Dorsof | Glaucotensil d | Mersolat D | Sefson | Trusomida | Trusopt | Unidorzo;
  • (PH) Philippines: Trusopt;
  • (PK) Pakistan: Trusopt;
  • (PL) Poland: Adolamid | Dolopt | Dorzolamid stada | Dorzolamid Teva | Dorzolamide genoptim | Dorzostill | Dropzol | Nodom | Oftidor | Rozalin | Trusopt | Vizidor;
  • (PR) Puerto Rico: Dorzolamide HCL | Trusopt;
  • (PT) Portugal: Dorcil | Dorcilfree | Dorzolamida actavis | Dorzolamida Generis | Dorzolamida mylan | Dorzolamida Teva | Trusopt;
  • (PY) Paraguay: Citol dorzo | Dorlamida;
  • (QA) Qatar: Trusopt | Xola | Zolichek;
  • (RO) Romania: Dorzopt;
  • (RU) Russian Federation: Dor antiglau eco | Dorzolamide nativ | Dorzolamide optic | Dorzolamide solopharm | Dorzolan solo | Dorzopt | Glaucopt | Trusopt;
  • (SA) Saudi Arabia: Trusopt | Xola | Zomidor;
  • (SE) Sweden: Dorzolamid mylan | Dorzolamid orifarm | Dorzolamid sandoz | Dorzolamid stada | Trusopt;
  • (SG) Singapore: Trusopt;
  • (SI) Slovenia: Trusopt;
  • (SK) Slovakia: Dorzolamid olikla | Dozotens | Trusopt;
  • (TH) Thailand: Lamisopt | Trusopt;
  • (TN) Tunisia: Alzor | Trusopt;
  • (TR) Turkey: Dorzamed | Trusopt;
  • (TW) Taiwan: Bolano | Dorzomide | Dorzostill | Trusopt;
  • (UA) Ukraine: Dorsamed | Dorsol | Dorzoptic | Rezlod | Rozalin | Trusopt;
  • (UY) Uruguay: Atensor | Beyonas dorzo | Dorzomed | Glaucotensil d | Trusopt;
  • (VE) Venezuela, Bolivarian Republic of: Cofador | Dorzol | Dorzolamida | Glaucotensil d | Trusomida | Trusopt;
  • (ZA) South Africa: Dorzopt | Glaucopress | Glaudor
  1. American Academy of Ophthalmology (AAO) PPP Glaucoma Panel, Hoskins Center for Quality Eye Care. Glaucoma summary benchmarks - 2019. https://www.aao.org/summary-benchmark-detail/glaucoma-summary-benchmarks-2019#PrimaryOpen-AngleGlaucoma(InitialEvaluation). Updated October 2019. Accessed December 23, 2019.
  2. Belkin A, Chen T, DeOliveria AR, Johnson SM, Ramulu PY, Buys YM; American Glaucoma Society and the Canadian Glaucoma Society. A practical guide to the pregnant and breastfeeding patient with glaucoma. Ophthalmol Glaucoma. 2020;3(2):79-89. doi:10.1016/j.ogla.2019.12.004 [PubMed 32672600]
  3. Biollaz J, Munafo A, Buclin T, et al, “Whole Blood Pharmacokinetics and Metabolic Affects of the Topical Carbonic Anhydrase Inhibitor Dorzolamide,” Eur J Clin Pharmacol, 1995, 47(5):455-60. [PubMed 7720769]
  4. Carlsen J, Durcan J, Zabriskie N, Swartz M, Crandall A. Nephrolithiasis with dorzolamide. Arch Ophthalmol. 1999;117(8):1087-1088. doi:10.1001/archopht.117.8.1087. [PubMed 10448757]
  5. Douglass R, Heckman G. Drug-related taste disturbance: a contributing factor in geriatric syndromes. Can Fam Physician. 2010;56(11):1142-1147. [PubMed 21075995]
  6. Dorzolamide [prescribing information]. Bridgewater, NJ: Bausch & Lomb, Inc; July 2016
  7. Hoffmanová I, Sánchez D. Metabolic acidosis and anaemia associated with dorzolamide in a patient with impaired renal function. Br J Clin Pharmacol. 2018;84(4):796-799. doi:10.1111/bcp.13499. [PubMed 29333622]
  8. Lee SJ, Kim M. Allergic contact dermatitis caused by dorzolamide eyedrops. Clin Ophthalmol. 2015;9:575-577. doi:10.2147/OPTH.S74555. [PubMed 25897195]
  9. Maren TH, Conroy CW, Wynns GC, Levy NS. Ocular absorption, blood levels, and excretion of dorzolamide, a topically active carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1997;13(1):23-30. doi:10.1089/jop.1997.13.23. [PubMed 9029437]
  10. Morris S, Geh V, Nischal KK, Sahi S, Ahmed MA. Topical dorzolamide and metabolic acidosis in a neonate. Br J Ophthalmol. 2003;87(8):1052-1053. doi:10.1136/bjo.87.8.1052. [PubMed 12881361]
  11. Ott EZ, Mills MD, Arango S, Getson AJ, Assaid CA, Adamsons IA. A randomized trial assessing dorzolamide in patients with glaucoma who are younger than 6 years. Arch Ophthalmol. 2005;123(9):1177-1186. [PubMed 16157797]
  12. Quaranta L, Biagioli E, Riva I, et al. The Glaucoma Italian Pediatric Study (GIPSy): 3-year results. J Glaucoma. 2018;27(10):856-863. [PubMed 30095601]
  13. Strelow B, Fleischman D. Glaucoma in pregnancy: an update. Curr Opin Ophthalmol. 2020;31(2):114-122. doi:10.1097/ICU.0000000000000641 [PubMed 31922978]
  14. Trusopt (dorzolamide) [prescribing information]. Whitehouse Station, NJ: Merck Sharp and Dohme Corp; July 2021.
  15. Turgut B, Türkçüoğlu P, Güler M, Akyol N, Celiker U, Demir T. Anosmia as an adverse effect of dorzolamid. Acta Ophthalmol Scand. 2007;85(2):228-229. doi:10.1111/j.1600-0420.2006.00857.x. [PubMed 17305746]
  16. Urtti A, Salminen L. Minimizing systemic absorption of topically administered ophthalmic drugs. Surv Ophthalmol. 1993;37(6):435-456. [PubMed 8100087]
  17. Wilkerson M, Cyrlin M, Lippa EA, et al, “Four-Week Safety and Efficacy Study of Dorzolamide, a Novel, Active, Topical Carbonic Anhydrase Inhibitor,” Arch Ophthalmol, 1993, 111(10):1343-50. [PubMed 8216014]
  18. Zimmerman TJ, Kooner KS, Kandarakis AS, Ziegler LP. Improving the therapeutic index of topically applied ocular drugs. Arch Ophthalmol. 1984;102(4):551-553. [PubMed 6704011]
Topic 9386 Version 212.0

آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟