 Home > Encyclopedia > 2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)

2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)

2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1) structure

CAS No:
138982-67-9
Formula:
C21H21ClN4OS.ClH.H2O
Chemical Name:
2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)
Synonyms:
2H-Indol-2-one,5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-,hydrochloride,hydrate (1:1:1);2H-Indol-2-one,5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-,monohydrochloride,monohydrate;5-[2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl)ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride monohydrate;Ziprasidone monohydrochloride monohydrate;Ziprasidone hydrochloride monohydrate
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

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Description

Pale Tan PowderChEBI: The hydrochloride hydrate salt of ziprasidone.

Ziprasidone Hydrochloride is the hydrochloride salt form of ziprasidone, a benzothiazolylpiperazine derivative and an atypical antipsychotic agent with an antischizophrenic property. Ziprasidone hydrochloride functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor. Ziprasidone hydrochloride also inhibits synaptic reuptake of serotonin and norepinephrine. The mechanism of action by which ziprasidone hydrochloride exerts its antischizophrenic effect is unknown but is potentially mediated through a combination of dopamine D2 and serotonin 5-HT2 antagonism. This agent also has antagonistic activity against histamine H1 and alpha-1-adrenergic receptors.

2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1) Basic Attributes

Molecular Weight：

467.42

Exact Mass：

466.099701

UNII：

216X081ORU

DSSTox ID：

DTXSID00160855

NCI Thesaurus Code：

C48031

HScode：

38220010

Characteristics

PSA：

77.7

XLogP3：

4.68760

Appearance：

off-white powder

Melting Point：

300°C

Boiling Point：

554.8°C at 760 mmHg

Flash Point：

289.3ºC

Water Solubility：

DMSO: >10mg/mL

Storage Conditions：

room temp

Vapor Pressure：

2.38E-12mmHg at 25°C

Safety Information

Packing level：

Ⅲ

Transport codes：

UN1230 - class 3 - PG 2 - Methanol, solution

wgk germany：

hazard class code：

6.1

safety instructions：

24/25

RTECS Number：

NM3241200

Marks：

Precautionary statement(s)：

P260-P280

Hazard Statements：

H317-H373

GHS Classification：

|Warning|H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P260, P261, P272, P280, P302+P352, P314, P321, P333+P313, P363, and P501|Aggregated GHS information provided by 32 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)|Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)

MeSH Entry Terms：

5-(2-(4-(3-benzisothiazolyl)piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one

2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1) Use and Manufacturing

Uses

Ziprasidone is the hydrochloride salt of a benzisothiazolylpiperazine analog structurally related to the atypical antipsychotic drug tiospirone that antagonizes both central serotonin 5-HT2A (Ki = 0.42 nM) and dopamine D2 (Ki = 4.8 nM) receptors. It is also a potent agonist at 5-HT1A receptors (Ki = 3.4 nM), increasing cortical dopamine release which may offset negative effects associated with dopamine D2 antagonism, and an inverse agonist at 5-HT1B and 5-HT1D receptors (pKis = 8.8 and 8.6, respectively).[Cayman Chemical]

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:467.4
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:4
Exact Mass:466.0997026
Monoisotopic Mass:466.0997026
Topological Polar Surface Area:77.7
Heavy Atom Count:30
Complexity:573
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

Material

Isopropanol

Drug Function and Efficacy

Zolotin Ziprasidone Hydrochloride Capsules

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Zolotin Ziprasidone Hydrochloride Capsules
Indication	Ziprasidone should not be used with drugs that prolong the QT interval. Ziprasidone acts primarily on the central nervous system and should be used with caution with other centrally acting drugs. Ziprasidone may induce hypotension and therefore may enhance the efficacy of some antihypertensive drugs. Ziprasidone may antagonize the effects of levodopamine and dopamine agonists. Effects of other drugs on ziprasidone: Carbamazepine: Carbamazepine is a CYP3A4 inducer. When patients take 200 mg of carbamazepine twice a day for 21 consecutive days, the AUC of ziprasidone decreases by about 35%. The higher the dose of carbamazepine, the greater the decrease in the AUC of ziprasidone. Ketoconazole: Ketoconazole is a strong CYP3A4 inhibitor. When patients take 400 mg of ketoconazole daily for 5 consecutive days, the AUC and Cmax of ziprasidone increase by about 35-40%. Other CYP3A4 inhibitors have similar effects. Cimetidine: 800 mg of cimetidine, once a day, for 2 days, has no effect on the pharmacokinetics of ziprasidone. Antacids: The co-administration of 30 mL of antacids has no effect on the pharmacokinetics of ziprasidone. In addition, in controlled clinical trials, population pharmacokinetic analysis of schizophrenia patients enrolled showed that the pharmacokinetics of ziprasidone did not change significantly when co-administered with benztropine, propranolol and lorazepam. Effect of ziprasidone on other drugs: In vitro studies have shown that ziprasidone does not interfere with the metabolism of drugs that are mainly cleared by CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4. There is almost no interaction between ziprasidone and other drugs due to displacement. Lithium: Ziprasidone (40 mg bid) and lithium (450 mg bid) co-administered for 7 days will not affect the steady-state blood concentration or renal clearance of lithium. Oral contraceptives: Ziprasidone (20 mg bid) combined with oral contraceptives ethinyl estradiol (0.03 mg) and levonorgestrel (0.15 mg) did not affect the pharmacokinetics of these two oral contraceptives. Dextromethorphan: Consistent with the results of in vitro tests, the results of a study conducted in healthy volunteers showed that ziprasidone did not change the metabolism of dextromethorphan, a substrate of CYP2D6, to its major metabolite, dextrorphan. There was no significant change in the dextromethorphan/dextrphan ratio in urine.

Zolotin Ziprasidone Hydrochloride Capsules

Indication

Ziprasidone should not be used with drugs that prolong the QT interval. Ziprasidone acts primarily on the central nervous system and should be used with caution with other centrally acting drugs. Ziprasidone may induce hypotension and therefore may enhance the efficacy of some antihypertensive drugs. Ziprasidone may antagonize the effects of levodopamine and dopamine agonists. Effects of other drugs on ziprasidone: Carbamazepine: Carbamazepine is a CYP3A4 inducer. When patients take 200 mg of carbamazepine twice a day for 21 consecutive days, the AUC of ziprasidone decreases by about 35%. The higher the dose of carbamazepine, the greater the decrease in the AUC of ziprasidone. Ketoconazole: Ketoconazole is a strong CYP3A4 inhibitor. When patients take 400 mg of ketoconazole daily for 5 consecutive days, the AUC and Cmax of ziprasidone increase by about 35-40%. Other CYP3A4 inhibitors have similar effects. Cimetidine: 800 mg of cimetidine, once a day, for 2 days, has no effect on the pharmacokinetics of ziprasidone. Antacids: The co-administration of 30 mL of antacids has no effect on the pharmacokinetics of ziprasidone. In addition, in controlled clinical trials, population pharmacokinetic analysis of schizophrenia patients enrolled showed that the pharmacokinetics of ziprasidone did not change significantly when co-administered with benztropine, propranolol and lorazepam. Effect of ziprasidone on other drugs: In vitro studies have shown that ziprasidone does not interfere with the metabolism of drugs that are mainly cleared by CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4. There is almost no interaction between ziprasidone and other drugs due to displacement. Lithium: Ziprasidone (40 mg bid) and lithium (450 mg bid) co-administered for 7 days will not affect the steady-state blood concentration or renal clearance of lithium. Oral contraceptives: Ziprasidone (20 mg bid) combined with oral contraceptives ethinyl estradiol (0.03 mg) and levonorgestrel (0.15 mg) did not affect the pharmacokinetics of these two oral contraceptives. Dextromethorphan: Consistent with the results of in vitro tests, the results of a study conducted in healthy volunteers showed that ziprasidone did not change the metabolism of dextromethorphan, a substrate of CYP2D6, to its major metabolite, dextrorphan. There was no significant change in the dextromethorphan/dextrphan ratio in urine.

Ziprasidone hydrochloride
Manufacturer	Chongqing Shenghuaxi Pharmaceutical. Co., Ltd.

Ziprasidone Hydrochloride Capsules
Ingredients	The main ingredient of this product is: Ziprasidone hydrochloride. Chemical name: 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2(1H)-indol-2-one hydrochloride monohydrate.
Indication	1 Ziprasidone should not be used in combination with drugs that prolong the QT interval. 2 Ziprasidone mainly acts on the central nervous system and should be used with caution in combination with other centrally acting drugs. 3 Ziprasidone may induce hypotension and therefore may enhance the efficacy of certain antihypertensive drugs. 4 Ziprasidone may antagonize the effects of levodopamine and dopamine agonists. Effects of other drugs on ziprasidone Carbamazepine: Carbamazepine is a CYP3A4 inducer. When patients take 200 mg of carbamazepine twice a day for 21 consecutive days, the AUC of ziprasidone decreases by approximately 35%. The higher the dose of carbamazepine, the greater the decrease in the AUC of ziprasidone.
Specifications	60 mg

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Registered Holders

MEGAFINE PHARMA P LTD

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Guide of 2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)

Description
Basic Attributes
Characteristics
Safety Information
Drug Information
Use and Manufacturing
Computed Properties
Material
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
Latest News
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2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)

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