Product Name

  • Name

    Dorzolomide hydrochloride

  • EINECS 620-304-2
  • CAS No. 130693-82-2
  • Article Data13
  • CAS DataBase
  • Density 1.53 g/cm3
  • Solubility
  • Melting Point 265-267 °C
  • Formula C10H16N2O4S3.HCl
  • Boiling Point 575.8 °C at 760 mmHg
  • Molecular Weight 360.907
  • Flash Point 302 °C
  • Transport Information
  • Appearance White off-white crystalline powder.
  • Safety
  • Risk Codes
  • Molecular Structure Molecular Structure of 130693-82-2 (Dorzolomide hydrochloride)
  • Hazard Symbols
  • Synonyms 4H-Thieno[2,3-b]thiopyran-2-sulfonamide,4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, (4S,6S)-(9CI);(S,S)-(-)-5,6-Dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxidemonohydrochloride;L 671152;MK 507;Trusopt;
  • PSA
  • LogP

Synthetic route

(4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide di-p-toluyl-L-tartate salt
1227941-29-8

(4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide di-p-toluyl-L-tartate salt

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Stage #1: (4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide di-p-toluyl-L-tartate salt With sodium hydrogencarbonate In water; ethyl acetate at 25 - 30℃; for 0.25h;
Stage #2: With hydrogenchloride In ethyl acetate; isopropyl alcohol at 25 - 85℃; for 12.5h; Product distribution / selectivity;		100%
With hydrogenchloride In isopropyl alcohol at 80℃; for 0.0833333 - 0.166667h; pH=3 - 4; Product distribution / selectivity; Heating / reflux;
Stage #1: (4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide di-p-toluyl-L-tartate salt With sodium hydrogencarbonate In ethyl acetate at 20℃;
Stage #2: With hydrogenchloride In methanol; isopropyl alcohol for 0.666667h;
5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide maleate salt

5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide maleate salt

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Stage #1: 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide maleate salt With hydrogenchloride; sodium hydroxide In water at 52℃; pH=7.7; Inert atmosphere;
Stage #2: With hydrogenchloride In water; isopropyl alcohol at 20 - 75℃;		99.2%
Stage #1: 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide maleate salt With sodium hydroxide In water at 52℃; Inert atmosphere;
Stage #2: With hydrogenchloride In water; isopropyl alcohol at 75℃;		8.1 g
dorzolamide
120279-96-1

dorzolamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In ethyl acetate pH=1;95%
With hydrogenchloride In water; dimethyl sulfoxide at 5 - 10℃; for 3h; pH=1.0;
5,6-dihydro-4-(S)-ethylamino-6-(S)-methyl-4H-thieno[2,3-b]thiopyran-7,7-dioxide hydrochloride

5,6-dihydro-4-(S)-ethylamino-6-(S)-methyl-4H-thieno[2,3-b]thiopyran-7,7-dioxide hydrochloride

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Stage #1: 5,6-dihydro-4-(S)-ethylamino-6-(S)-methyl-4H-thieno[2,3-b]thiopyran-7,7-dioxide hydrochloride With sulfuric acid; sulfur trioxide at 20℃; for 2 - 3h;
Stage #2: With thionyl chloride for 3 - 6h; Heating / reflux;
Stage #3: With hydrogenchloride; ammonia Product distribution / selectivity; more than 3 stages;		70%
Stage #1: 5,6-dihydro-4-(S)-ethylamino-6-(S)-methyl-4H-thieno[2,3-b]thiopyran-7,7-dioxide hydrochloride With sulfuric acid; sulfur trioxide at -7 - 20℃; for 22h;
Stage #2: With thionyl chloride at 20 - 65℃; for 24h;
Stage #3: With hydrogenchloride; ammonia Product distribution / selectivity; more than 3 stages;
Reaxys ID: 11712783

Reaxys ID: 11712783

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
With (-)-di-p-toluoyl-L-tartaric acid22.48%
trans-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide

trans-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Stage #1: trans-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide; Di-p-toluoyl-L-tartaric acid In propan-1-ol Heating / reflux;
Stage #2: With sodium hydrogencarbonate In water
Stage #3: With hydrogenchloride In ethanol		22.48%
2C10H16N2O4S3*C11H10O7

2C10H16N2O4S3*C11H10O7

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Stage #1: 2C10H16N2O4S3*C11H10O7 With sodium carbonate In water; ethyl acetate
Stage #2: With hydrogenchloride In ethyl acetate; isopropyl alcohol pH=1 - 2;
5,6-dihydro-6-methyl-4-oxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide

5,6-dihydro-6-methyl-4-oxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: dihydrogen peroxide / sodium tungstate (VI) dihydrate / ethyl acetate; water / -20 °C
2.1: water; sodium tetrahydroborate; methanol / ethyl acetate / 10 - 20 °C
3.1: sulfuric acid / 0 - 30 °C
3.2: 10 °C / pH 7 - 8
4.1: sodium tetrahydroborate / tetrahydrofuran / -5 - 5 °C
4.2: 5 - 20 °C
5.1: sodium hydroxide / 20 °C / pH 7.5 - 8
6.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
7.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
7.2: 0.67 h
View Scheme
4-hydroxy-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide

4-hydroxy-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sulfuric acid / 0 - 30 °C
1.2: 10 °C / pH 7 - 8
2.1: sodium tetrahydroborate / tetrahydrofuran / -5 - 5 °C
2.2: 5 - 20 °C
3.1: sodium hydroxide / 20 °C / pH 7.5 - 8
4.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
5.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
5.2: 0.67 h
View Scheme
(+/-)-(4S,6S;4R,6R)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide

(+/-)-(4S,6S;4R,6R)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
2.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
2.2: 0.67 h
View Scheme
(+/-)-(4S,6S;4R,6R)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide maleate

(+/-)-(4S,6S;4R,6R)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide maleate

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: sodium hydroxide / 20 °C / pH 7.5 - 8
2.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
3.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
3.2: 0.67 h
View Scheme
N-(6-methyl-7,7-dioxido-2-sulfamoyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-4-yl)acetamide

N-(6-methyl-7,7-dioxido-2-sulfamoyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-4-yl)acetamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: sodium tetrahydroborate / tetrahydrofuran / -5 - 5 °C
1.2: 5 - 20 °C
2.1: sodium hydroxide / 20 °C / pH 7.5 - 8
3.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
4.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
4.2: 0.67 h
View Scheme
6-methyl-4-oxo-5,6-dihydro-4H-thieno[2.3-b]thiopyran-2-sulfonamide-7,7-dioxide
935289-26-2

6-methyl-4-oxo-5,6-dihydro-4H-thieno[2.3-b]thiopyran-2-sulfonamide-7,7-dioxide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: water; sodium tetrahydroborate; methanol / ethyl acetate / 10 - 20 °C
2.1: sulfuric acid / 0 - 30 °C
2.2: 10 °C / pH 7 - 8
3.1: sodium tetrahydroborate / tetrahydrofuran / -5 - 5 °C
3.2: 5 - 20 °C
4.1: sodium hydroxide / 20 °C / pH 7.5 - 8
5.1: isopropyl alcohol; acetonitrile / 1 h / 70 °C / Reflux
6.1: sodium hydrogencarbonate / ethyl acetate / 20 °C
6.2: 0.67 h
View Scheme
(6S)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-4-one-2-sulfonamide
1383784-43-7

(6S)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-4-one-2-sulfonamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sodium tungstate (VI) dihydrate; oxygen / methanol; water / 6 h / 10 - 50 °C / Inert atmosphere
2.1: sodium tetrahydroborate / water; tetrahydrofuran / 2 h / 15 °C / Inert atmosphere
3.1: methanesulfonic acid / 18 h / 10 - 87 °C / Inert atmosphere
3.2: 4.5 h / 7 - 40 °C / pH 7.3
4.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
4.2: 40 °C
5.1: sodium hydroxide / water / 52 °C / Inert atmosphere
5.2: 75 °C
View Scheme
(6S)-4-oxo-5,6-dihydro-6-methyl-7,7-dioxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide
154716-03-7

(6S)-4-oxo-5,6-dihydro-6-methyl-7,7-dioxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: sodium tetrahydroborate / water; tetrahydrofuran / 2 h / 15 °C / Inert atmosphere
2.1: methanesulfonic acid / 18 h / 10 - 87 °C / Inert atmosphere
2.2: 4.5 h / 7 - 40 °C / pH 7.3
3.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
3.2: 40 °C
4.1: sodium hydroxide / water / 52 °C / Inert atmosphere
4.2: 75 °C
View Scheme
cis-(6S)-4-hydroxy-5,6-dihydro-6-methyl-7,7-dioxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide

cis-(6S)-4-hydroxy-5,6-dihydro-6-methyl-7,7-dioxo-4H-thieno[2,3-b]thiopyran-2-sulfonamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: methanesulfonic acid / 18 h / 10 - 87 °C / Inert atmosphere
1.2: 4.5 h / 7 - 40 °C / pH 7.3
2.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
2.2: 40 °C
3.1: sodium hydroxide / water / 52 °C / Inert atmosphere
3.2: 75 °C
View Scheme
(4S,6S)‑4‑acetamido‑5,6‑dihydro‑6‑methyl‑4H‑thieno[2,3‑b]thiopyran‑2‑sulfonamide‑7,7‑dioxide
147200-03-1

(4S,6S)‑4‑acetamido‑5,6‑dihydro‑6‑methyl‑4H‑thieno[2,3‑b]thiopyran‑2‑sulfonamide‑7,7‑dioxide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
1.2: 40 °C
2.1: sodium hydroxide / water / 52 °C / Inert atmosphere
2.2: 75 °C
View Scheme
(S)-5,6-dihydro-6-methylthieno<2,3-b>thiopyran-4-one
147086-79-1

(S)-5,6-dihydro-6-methylthieno<2,3-b>thiopyran-4-one

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: thionyl chloride; chlorosulfonic acid / 10 h / -3 - 28 °C / Inert atmosphere
2.1: ammonia / methanol; acetone / -10 °C / Inert atmosphere
3.1: sodium tungstate (VI) dihydrate; oxygen / methanol; water / 6 h / 10 - 50 °C / Inert atmosphere
4.1: sodium tetrahydroborate / water; tetrahydrofuran / 2 h / 15 °C / Inert atmosphere
5.1: methanesulfonic acid / 18 h / 10 - 87 °C / Inert atmosphere
5.2: 4.5 h / 7 - 40 °C / pH 7.3
6.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
6.2: 40 °C
7.1: sodium hydroxide / water / 52 °C / Inert atmosphere
7.2: 75 °C
View Scheme
(S)-6-methyl-4-oxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonyl chloride
1083006-59-0

(S)-6-methyl-4-oxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonyl chloride

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: ammonia / methanol; acetone / -10 °C / Inert atmosphere
2.1: sodium tungstate (VI) dihydrate; oxygen / methanol; water / 6 h / 10 - 50 °C / Inert atmosphere
3.1: sodium tetrahydroborate / water; tetrahydrofuran / 2 h / 15 °C / Inert atmosphere
4.1: methanesulfonic acid / 18 h / 10 - 87 °C / Inert atmosphere
4.2: 4.5 h / 7 - 40 °C / pH 7.3
5.1: borane-THF / tetrahydrofuran / 17 h / 38 °C / Inert atmosphere
5.2: 40 °C
6.1: sodium hydroxide / water / 52 °C / Inert atmosphere
6.2: 75 °C
View Scheme
(6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide

(6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide

A

4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride
1417607-96-5

4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride

B

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In acetone at 0 - 5℃; for 2h; pH=1 - 2;A n/a
B n/a
(6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride

(6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
In methanol; water for 2h; Solvent; Reflux;3.2 g
N,N-dimethyl-formamide dimethyl acetal
4637-24-5

N,N-dimethyl-formamide dimethyl acetal

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

(E)-N'-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}-N,N-dimethylmethanimidamide

(E)-N'-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}-N,N-dimethylmethanimidamide

Conditions
ConditionsYield
With triethylamine In N,N-dimethyl-formamide at 20℃; for 3h;80%
1,8-octanediol bis(4-nitrophenylcarbonate)

1,8-octanediol bis(4-nitrophenylcarbonate)

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

8-(((((4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxido-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-yl)sulfonyl)carbamoyl)oxy)octyl (((4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxido-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-yl)sulfonyl)carbamate

8-(((((4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxido-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-yl)sulfonyl)carbamoyl)oxy)octyl (((4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxido-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-yl)sulfonyl)carbamate

Conditions
ConditionsYield
With sodium hydride In N,N-dimethyl-formamide at 20℃; for 2h; Inert atmosphere;56%
dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

N,N-dimethylformamide diethyl diacetal
1188-33-6

N,N-dimethylformamide diethyl diacetal

N'-[(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-2-sulfonyl]-N,N-dimethylmethanimidamide
1034583-83-9

N'-[(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-2-sulfonyl]-N,N-dimethylmethanimidamide

Conditions
ConditionsYield
With triethylamine In N,N-dimethyl-formamide at 20℃; for 3h; Inert atmosphere;

Dorzolomide hydrochloride Chemical Properties

IUPAC Name:(4R,6R)-?4-?(ethylamino)-?6-?methyl-?7,7-?dioxo-?5,6-?dihydro-?4H-?thieno[2,3-?b]thiopyran-?2-?sulfonamide hydrochloride
Molecular Formula:C10H17ClN2O4S3
Molecular Weight:360.900980 g/mol
Appearance:White off-white crystalline powder
Density:1.53 g/cm3
Melting Point:283~285 oC
Boiling Point:575.8 °C at 760 mmHg
Flash Point:302 °C
Synonyms of Dorzolamide hydrochloride(130693-82-2):
3-b)thiopyran-2-sulfonamide,5,6-dihydro-4-(ethylamino)-6-methyl-4h-thieno(;mk-0507;monohydrochloride,(4s-trans)-7-dioxide;(2s,4s)-2-ethylamino-4-methyl-5,5-dioxo-5,7-dithiabicyclo[4.3.0]nona-8,10-diene-8-sulfonamide hydrochloride;DORZOLAMIDE HCL;DORZOLAMIDE HYDROCHLORIDE;dorzolomide hydrochloride;DorzolomideHcl,Usp
Categories of Dorzolamide hydrochloride(130693-82-2):
Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Dorzolamide

Dorzolomide hydrochloride Uses

Dorzolamide hydrochloride(130693-82-2) is used for treatment of glaucoma.

Dorzolomide hydrochloride Toxicity Data With Reference

Toxicity Information of  Dorzolamide hydrochloride(130693-82-2):
1.dog LD50 oral > 250mg/kg (250mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
2.mouse LD50 intravenous 469mg/kg (469mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)LUNGS, THORAX, OR RESPIRATION: DYSPNEA Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
3.mouse LD50 oral 1320mg/kg (1320mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYEBEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
BEHAVIORAL: ATAXIA Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
4.mouse LD50 subcutaneous > 2gm/kg (2000mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE,BEHAVIORAL: ATAXIA,BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
5.rat LD50 intravenous 726mg/kg (726mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY),BEHAVIORAL: TREMOR LUNGS, THORAX, OR RESPIRATION: DYSPNEA Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
6.rat LD50 oral 1927mg/kg (1927mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE
BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)BEHAVIORAL: ATAXIA Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.
7.rat LD50 subcutaneous > 2gm/kg (2000mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE
BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE"
Kiso to Rinsho. Clinical Report. Vol. 28, Pg. 1241, 1994.

Dorzolomide hydrochloride Analytical Methods

TRUSOPT is a sulfonamide and, although administered topically, is absorbed systemically. Therefore, the same types of adverse reactions that are attributable to sulfonamides may occur with topical administration with TRUSOPT. Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitization may recur when a sulfonamide is readministered irrespective of the route of administration. If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation.

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