Proparacaine (PPC) Hydrochloride is a derivative of lidocaine (HY-B0185), with immunomodulatory effect and glucocorticomimetic activity. Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor. Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro[3]. In addition, proparacaine hydrochloride is an ester-type local anesthetic agent that is extensively used in ophthalmic operations[4]. PH (Proparacaine Hydrochloride) has a mydriatic effect of its own. It penetrates through the bare sclera and leads on to skewed dilation of the pupil[5]. 0.5% proparacaine HCl is commonly used for topical anaesthesia in ultrasound pachometry prior to refractive surgery[6].
Proparacaine HCl/盐酸丙美卡因 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Diabetic OLETF rats and non-diabetic LETO rats
Topical application to the eye
0.5%
Single dose
Anesthetize rats for intravitreal injection
Diabetes. 2008 Aug;57(8):2181-90
New Zealand albino rabbits
Anesthetized rabbit model
Topical ocular application
0.5%, 10 μL
Single dose, measurements continued for 5 to 15 minutes
To determine the effect of proparacaine on episcleral venous pressure (EVP). Results showed a significant decrease in EVP (from 12.3 ± 1.1 mm Hg to 8.7 ± 0.9 mm Hg) and a small decrease in intraocular pressure (IOP).
Invest Ophthalmol Vis Sci. 2009 Jun;50(6):2949-52
New Zealand White rabbits
Normal rabbit eye model
Topical ocular administration
0.5%
Single dose or administered 10 minutes before tear collection
To evaluate the effect of anesthesia on basal tear secretion, results showed optimal anesthesia at 10 minutes, effectively suppressing reflex tearing.
Invest Ophthalmol Vis Sci. 2011 Aug 5;52(9):6265-70
BALB/c mice
Allergic rhinitis model
Intranasal administration
75 μg/30 μL
7 consecutive days
PPC significantly decreased nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa. Serum OVA-specific IgE, OVA-specific IgG1, and OVA-specific IgG2a levels were significantly higher in the AR group compared to the control group, but no significant difference was observed between the PPC and AR groups. Serum IL-4 levels were significantly lower in the PPC group compared to the AR group, while IL-5 levels showed no significant difference among all groups. No significant difference in serum cortisol levels was observed among the four groups.
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