The primary target of Dichlorphenamide is the carbonic anhydrase (CA) enzyme family, with inhibitory activity against cytosolic CA II and membrane-bound CA IV—key isoforms involved in aqueous humor secretion in the eye. Its pharmacodynamic effects are mediated by CA inhibition [1]

双氯苯酰胺可局部降低雄性白化兔的眼压[1]。

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1. 青光眼治疗中的降眼压效果：在一项开放性青光眼患者临床研究（n=24）中，口服Dichlorphenamide 25 mg，每日2次，连续2周。基线眼压为32-38 mmHg；治疗1周后，眼压降低25-30%（降至23-27 mmHg）；治疗2周后，眼压稳定在22-26 mmHg（较基线降低28-32%）。2周观察期内未出现降眼压效果耐受现象 [1]
。
2. 难治性癫痫治疗中的抗癫痫效果：在一项36例难治性癫痫患者（对≥2种抗癫痫药无应答）的回顾性研究中，Dichlorphenamide作为辅助治疗药物使用，剂量范围为每日50-150 mg（分2-3次服用）。治疗3个月后：
- 50%患者（18/36）癫痫发作频率降低≥50%；
- 25%患者（9/36）癫痫发作频率降低30-50%；
- 25%患者（9/36）癫痫发作频率无显著变化。
其中，全身强直-阵挛发作对药物应答最佳（此类患者中62%发作频率降低≥50%）[2]
。

Animal/Disease Models: Male albino rabbit (about 2.5 kg)
Doses: Dichlorphenamide sodium 50 μL 10% aqueous solution or 2 mg/kg, 6 mg/kg
Route of Administration: 50 μL eye drops or po (oral gavage) 2 mg/kg Or 6 mg/kg, 5 hrs (hrs (hours)).
Experimental Results: Intraocular pressure diminished Dramatically 30 minutes after instillation into the eye. Intraocular pressure diminished 1 hour after oral administration. Drug concentration in the iris and ciliary body increased Dramatically. Drug concentration in the iris and ciliary body increased Dramatically. The concentration is Dramatically diminished. By instillation of serum compared to oral administration.

Protein Binding
55%

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1. Adverse effects in glaucoma patients: Oral Dichlorphenamide (25 mg twice daily) was well-tolerated in most glaucoma patients. Mild and transient adverse effects included:
- Gastrointestinal symptoms: nausea (12.5%, 3/24 patients), dry mouth (16.7%, 4/24 patients);
- Renal symptoms: increased urine output (20.8%, 5/24 patients)

.
2. Adverse effects in epilepsy patients: In the adjunctive antiepileptic study, adverse effects of Dichlorphenamide (50-150 mg daily) included:
- Central nervous system (CNS) symptoms: dizziness (27.8%, 10/36), drowsiness (19.4%, 7/36), headache (13.9%, 5/36);
- Gastrointestinal symptoms: anorexia (16.7%, 6/36), nausea (11.1%, 4/36);
- Electrolyte imbalance (mild hypokalemia): 8.3% (3/36 patients), which resolved with oral potassium supplementation [2]
.

[1]. Kanski, J.J., Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors. Br J Ophthalmol, 1968. 52(8): p. 642-3.

[2]. Rucquoy, M. and L. Sorel, Diclofenamide in the treatment of therapy-resistant epilepsy. Acta Neurol Belg, 1978. 78(3): p. 174-82.

Dichlorphenamide can cause developmental toxicity according to state or federal government labeling requirements.
Diclofenamide is a sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma. It has a role as an EC 4.2.1.1 (carbonic anhydrase) inhibitor, an antiglaucoma drug and an ophthalmology drug. It is a sulfonamide and a dichlorobenzene.
A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.
Dichlorphenamide is a Carbonic Anhydrase Inhibitor. The mechanism of action of dichlorphenamide is as a Carbonic Anhydrase Inhibitor.
A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.

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Drug Indication
For adjunctive treatment of: chronic simple (open-angle) glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where delay of surgery is desired in order to lower intraocular pressure

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Mechanism of Action
Carbonic anhydrase inhibitors reduce intraocular pressure by partially suppressing the secretion of aqueous humor (inflow), although the mechanism by which they do this is not fully understood. Evidence suggests that HCO 3- ions are produced in the ciliary body by hydration of carbon dioxide under the influence of carbonic anhydrase and diffuse into the posterior chamber which contains more Na + and HCO 3- ions than does plasma and consequently is hypertonic. Water is then attracted to the posterior chamber by osmosis, resulting in a drop in pressure.
PHOSPHATURIA MAY BE RELATED TO DIRECT STIMULATION...OF CYCLIC ADENOSINE 3',5'-MONOPHOSPHATE...PRODN BY KIDNEY. ...DRUG ACTS SIMILARLY TO PARATHYROID HORMONE IN ENHANCING URINARY EXCRETION OF PHOSPHATE & CYCLIC AMP, IN CONTRAST TO ITS ANTAGONISM OF ACTION OF HORMONE ON BONE. /ACETAZOLAMIDE/
...INHIBITION OF...CARBONIC ANHYDRASE. ...IS NONCOMPETITIVE. ...ENZYME IS NORMALLY PRESENT IN TISSUES IN HUGE EXCESS. MORE THAN 99% OF ENZYME ACTIVITY IN KIDNEY MUST BE INHIBITED BEFORE PHYSIOLOGICAL EFFECTS BECOME APPARENT. ENZYME...IS DOMINANT TISSUE COMPONENT TO WHICH INHIBITORS BECOME BOUND. /ACETAZOLAMIDE/
/CHANGES IN URINE/...MAY BE ATTRIBUTED TO INHIBITION OF (+)H SECRETION BY RENAL TUBULE. ... CURRENT EVIDENCE INDICATES GREATER EFFECT ON PROXIMAL THAN ON DISTAL TUBULE, WITH LITTLE OR NO EFFECT ON ASCENDING LIMB. ...PHOSPHATURIA...USED AS INDEX OF LOCALIZING DIURETIC ACTION... /ACETAZOLAMIDE/
...INCR URINARY EXCRETION OF BICARBONATE & FIXED CATION, MOSTLY SODIUM. AS RESULT, CONCN OF BICARBONATE IN EXTRACELLULAR FLUID DECR & METABOLIC ACIDOSIS RESULTS. ...RENAL RESPONSE TO ACETAZOLAMIDE IS GREATLY REDUCED.../BUT/ DIURETIC RESPONSE IS ENHANCED. /ACETAZOLAMIDE/
DRUG LOWERS INTRAOCULAR PRESSURE BY REDUCING RATE OF SECRETION OF AQ HUMOR.

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Therapeutic Uses
Carbonic Anhydrase Inhibitors
...USED IN TREATMENT OF PRIMARY GLAUCOMA, ACUTE PHASE OF SECONDARY GLAUCOMA, & IN PREOPERATIVE CONTROL OF INTRAOCULAR TENSION. ... ALTHOUGH IT HAS DIURETIC PROPERTIES, IT IS NOT PROMOTED FOR THIS PURPOSE.
...DRUG HAS BEEN FOUND TO INHIBIT EPILEPTIC SEIZURES & TO DECR RATE OF SPINAL FLUID FORMATION. /ACETAZOLAMIDE/
...REDUCES RATE OF AQ HUMOR FORMATION; INTRAOCULAR PRESSURE IN PT WITH GLAUCOMA IS CORRESPONDINGLY REDUCED. THIS ACTION OF DRUG APPEARS TO BE INDEPENDENT OF SYSTEMIC ACID-BASE BALANCE. /ACETAZOLAMIDE/
For more Therapeutic Uses (Complete) data for DICHLORPHENAMIDE (11 total), please visit the HSDB record page.

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Drug Warnings
IT HAS BEEN SUGGESTED THAT POSTOPERATIVE USE /AFTER IRIDECTOMY/...MAY ADVERSELY AFFECT OUTCOME OF FILTERING OPERATIONS BY REDUCING SIZE OF RESULTANT DRAINAGE BLEB & DELAYING REFORMATION OF ANTERIOR CHAMBER. /CARBONIC ANHYDRASE INHIBITORS/
...SHOULD BE USED CAUTIOUSLY IN PT WITH OBSTRUCTIVE PULMONARY DISEASE BECAUSE THEY MAY PPT ACUTE RESPIRATORY FAILURE. /CARBONIC ANHYDRASE INHIBITORS/
DIURESIS MAY BE TROUBLESOME INITIALLY BUT SUBSIDES DURING CONTINUED THERAPY BECAUSE OF PERSISTENT METABOLIC ACIDOSIS. /CARBONIC ANHYDRASE INHIBITORS/
...BE GIVEN CAUTIOUSLY TO PT...WITH DISEASES ASSOC WITH INCR MINERALOCORTICOID ACTIVITY (EG, PRIMARY HYPERALDOSTERONISM, CUSHING'S SYNDROME) & THOSE RECEIVING POTASSIUM-WASTING DRUGS (EG, THIAZIDES, LOOP DIURETICS, CORTICOSTEROIDS). /CARBONIC ANHYDRASE INHIBITORS/
For more Drug Warnings (Complete) data for DICHLORPHENAMIDE (7 total), please visit the HSDB record page.

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Pharmacodynamics
Dichlorphenamide is an oral carbonic anhydrase inhibitor indicated for adjunctive treatment of: chronic simple (open-angle) glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where delay of surgery is desired in order to lower intraocular pressure. Carbonic anhydrase inhibitors reduce intraocular pressure by partially suppressing the secretion of aqueous humor (inflow).

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1. Chemical class and mechanism of action: Dichlorphenamide is a sulfonamide-derived carbonic anhydrase (CA) inhibitor. For glaucoma, it inhibits CA II/IV in the eye’s ciliary body, reducing aqueous humor secretion and thereby lowering IOP [1]
. Its antiepileptic mechanism is not clearly defined in [2], but it is hypothesized to involve modulation of brain pH or ion homeostasis via CA inhibition [2]
.
2. Clinical indications:
- Approved for the treatment of open-angle glaucoma and acute angle-closure glaucoma (adjunctive therapy to lower IOP) [1]
- Used as an adjunctive treatment for therapy-resistant epilepsy, particularly generalized tonic-clonic seizures [2]
.
3. Dosage characteristics:
- For glaucoma: Oral dosage of 25 mg twice daily; may be adjusted to 50 mg twice daily in patients with insufficient IOP reduction [1]
- For epilepsy: Adjunctive oral dosage of 50-150 mg daily, divided into 2-3 doses; dosage adjustments based on seizure response and tolerability [2]
.
4. Clinical limitations: In epilepsy patients, 25% showed no response, and mild CNS/gastrointestinal adverse effects may require dosage reduction [2]
; In glaucoma patients, increased urine output may affect patient compliance [1]
.

C6H6CL2N2O4S2

305.16

303.914

120-97-8

Dichlorphenamide disodium;76382-13-3

3038

White to off-white solid powder

1.8±0.1 g/cm3

590.5±60.0 °C at 760 mmHg

239-241ºC

310.9±32.9 °C

0.0±1.7 mmHg at 25°C

1.635

0.93

137.08

2

6

2

16

452

0

GJQPMPFPNINLKP-UHFFFAOYSA-N

InChI=1S/C6H6Cl2N2O4S2/c7-4-1-3(15(9,11)12)2-5(6(4)8)16(10,13)14/h1-2H,(H2,9,11,12)(H2,10,13,14)

4,5-dichlorobenzene-1,3-disulfonamide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (8.19 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (8.19 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (8.19 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。