Hydroxyzine (pamoate)

Modify Date: 2024-01-03 14:55:18

Hydroxyzine (pamoate) Structure
Hydroxyzine (pamoate) structure
Common Name Hydroxyzine (pamoate)
CAS Number 10246-75-0 Molecular Weight 763.274
Density 1.182g/cm3 Boiling Point 499.2ºC at 760mmHg
Molecular Formula C44H43ClN2O8 Melting Point N/A
MSDS Chinese USA Flash Point 255.7ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Hydroxyzine (pamoate)


Hydroxyzine pamoate is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ug/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].

 Names

Name hydroxyzine pamoate
Synonym More Synonyms

 Hydroxyzine (pamoate) Biological Activity

Description Hydroxyzine pamoate is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ug/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
Related Catalog
References

[1]. Minogiannis, P., et al., Hydroxyzine inhibits neurogenic bladder mast cell activation. Int J Immunopharmacol, 1998. 20(10): p. 553-63.

[2]. Dimitriadou, V., X. Pang, and T.C. Theoharides, Hydroxyzine inhibits experimental allergic encephalomyelitis (EAE) and associated brain mast cell activation. Int J Immunopharmacol, 2000. 22(9): p. 673-84.

[3]. Kan, W.M., et al., Effect of hydroxyzine on the transport of etoposide in rat small intestine. Anticancer Drugs, 2001. 12(3): p. 267-73.

[4]. Morichi, R. and G. Pepeu, A study of the influence of hydroxyzine and diazepam on morphine antinociceptoion in the rat. Pain, 1979. 7(2): p. 173-80.

 Chemical & Physical Properties

Density 1.182g/cm3
Boiling Point 499.2ºC at 760mmHg
Molecular Formula C44H43ClN2O8
Molecular Weight 763.274
Flash Point 255.7ºC
Exact Mass 762.270813
PSA 151.00000
LogP 7.32310
Vapour Pressure 2.13E-17mmHg at 25°C
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
Safety Phrases 36
RIDADR NONH for all modes of transport
WGK Germany 3

 Articles26

More Articles
Microencapsulation of hydroxyzine HCl by thermal phase separation: in vitro release enhancement and in vivo pharmacodynamic evaluation.

Pharm. Dev. Technol. 18(1) , 196-209, (2013)

The systemic effect of hydroxyzine hydrochloride following its oral administration or topical application is associated with non compliant anticholinergic effect. Subsequently, the present study aims ...

Worsening of contact dermatitis by oral hydroxyzine: a case report.

Dermatol. Online J. 19(2) , 4, (2013)

Hydroxyzine is commonly used to treat pruritic skin lesions. Although rare, hydroxyzine can sometimes be linked to worsening dermatitis in patients who have sensitivities to phenothiazines and/or ethy...

Acute generalized exanthematous pustulosis associated with 2 common medications: hydroxyzine and benzocaine.

J. Am. Acad. Dermatol. 71(4) , e147-9, (2014)

 Synonyms

Paxistil {Pamoate}
Equipose {Pamoate}
4,4'-Methylenebis(3-hydroxy-2-naphthoic acid) - 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]-1-piperazinyl}ethoxy)ethanol (1:1)
Paxisitil
4,4'-methanediylbis(3-hydroxynaphthalene-2-carboxylic acid) - 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol (1:1)
Bobsule
Atarax P
Hydroxyzine pamoate salt
4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid,2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol
hydroxyzine pamoate
acide 4,4'-méthanediylbis(3-hydroxynaphtalène-2-carboxylique) - 2-(2-{4-[(4-chlorophényl)(phényl)méthyl]pipérazin-1-yl}éthoxy)éthanol (1:1)
2-Naphthalenecarboxylic acid, 4,4'-methylenebis[3-hydroxy-, compd. with 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethanol (1:1)
Hydroxyzyne pamoate
4,4'-Methandiylbis(3-hydroxynaphthalen-2-carbonsäure)--2-(2-{4-[(4-chlorphenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol(1:1)
EINECS 233-582-1
Hydroxyzine embonate
Hydroxyzine (pamoate)
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