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Pilocarpine hydrochloride

Pilocarpine hydrochloride structure

CAS No:
54-71-7
Formula:
C11H16N2O2.ClH
Chemical Name:
Pilocarpine hydrochloride
Synonyms:
2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,hydrochloride (1:1),(3S,4R)-;Pilocarpine,monohydrochloride;2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,monohydrochloride,(3S-cis)-;2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,monohydrochloride,(3S,4R)-;Pilocarpine hydrochloride;Pilocarpine muriate;Pilocar SMP;Pilocel;Pilovisc;Pilocarpine chloride;Almocarpine;Pilocarpal;Pilocarpinium chloride;(+)-Pilocarpine hydrochloride;Salagen;Isopto Carpine;Adsorbocarpine;NSC 5746;Vistacarpin N;Pilocar;Sanpilo;Pilogel
Categories:
Natural Products > Alkaloids

Description

Pilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

Pilocarpine hydrochloride is the hydrochloride salt of (+)-pilocarpine, a medication used to treat increased pressure inside the eye and dry mouth. It contains a (+)-pilocarpine.|Pilocarpine Hydrochloride is the hydrochloride salt of a natural alkaloid extracted from plants of the genus Pilocarpus with cholinergic agonist activity. As a cholinergic parasympathomimetic agent, pilocarpine predominantly binds to muscarinic receptors, thereby inducing exocrine gland secretion and stimulating smooth muscle in the bronchi, urinary tract, biliary tract, and intestinal tract. When applied topically to the eye, this agent stimulates the sphincter pupillae to contract, resulting in miosis; stimulates the ciliary muscle to contract, resulting in spasm of accomodation; and may cause a transitory rise in intraocular pressure followed by a more persistent fall due to opening of the trabecular meshwork and an increase in the outflow of aqueous humor.|A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

Pilocarpine hydrochloride Basic Attributes

Molecular Weight：

244.72

Exact Mass：

208.121185

EC Number：

200-212-5

UNII：

0WW6D218XJ

NSC Number：

5746

DSSTox ID：

DTXSID2041096

NCI Thesaurus Code：

C748

HScode：

2934999090

Characteristics

PSA：

44.12000

XLogP3：

-0.09

Appearance：

white powder

Density：

1.2±0.1 g/cm3

Melting Point：

204-205 °C

Boiling Point：

431.8±18.0 °C at 760 mmHg

Flash Point：

215.0±21.2 °C

Refractive Index：

1.585

Water Solubility：

H2O: 100 mg/mL

Storage Conditions：

2-8°C

Specific rotation：

89 º (C=5, H2O)

Safety Information

Packing level：

III

Hazard category：

6.1

Transport codes：

UN 1544 6.1/PG 3

wgk germany：

hazard class code：

26/28-25-23

safety instructions：

25-45

RTECS Number：

TK1450000

Marks：

T+,T

Stability/Shelf Life：

Hygroscopic

Precautionary statement(s)：

Missing Phrase - N15.00950417-P260-P304 + P340 + P310-P403 + P233

Hazard Statements：

H300 + H330

GHS Classification：

|Danger|H300 (64.46%): Fatal if swallowed [Danger Acute toxicity, oral]|P260, P264, P270, P271, P284, P301+P310, P304+P340, P310, P320, P321, P330, P403+P233, P405, and P501|Aggregated GHS information provided by 121 companies from 9 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Treatment of presbyopia

MeSH：

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate. (See all compounds classified as Muscarinic Agonists.)|Agents causing contraction of the pupil of the eye. Some sources use the term miotics only for the parasympathomimetics but any drug used to induce miosis is included here. (See all compounds classified as Miotics.)

MeSH Entry Terms：

Hydrochloride, Pilocarpine

Pilocarpine hydrochloride Use and Manufacturing

Uses

(+)-Pilocarpine is a muscarinic M1 and M2 acetylcholine receptor agonist with pKB values of 5 and 3.7, respectively. Systemic administration of (+)-pilocarpine is typically used as an animal model for temporal lobe epilepsy and can mimic the generation of complex partial seizures by producing changes in hippocampal neuron morphology, membrane properties, and synaptic responses.

Manufacturing Info：

2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, hydrochloride (1:1), (3S,4R)-: INACTIVE

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:244.72
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:3
Exact Mass:244.0978555
Monoisotopic Mass:244.0978555
Topological Polar Surface Area:44.1
Heavy Atom Count:16
Complexity:245
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Promotes aqueous humor outflow, and the efficacy is enhanced by the action of timolol

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

Compound timolol eye drops
Ingredients	Timolol maleate 5mg, pilocarpine hydrochloride 20mg/ml also contains additives such as benzalkonium chloride, citric acid monohydrate, sodium citrate, and hypromellose.
Indication	1. Timolol maleate is a non-selective β-adrenergic receptor blocker with no obvious endogenous sympathomimetic activity and local anesthetic effect, and no direct inhibitory effect on the myocardium. 2. This product is timolol maleate eye drops, which can reduce intraocular pressure in patients with high intraocular pressure and normal people. The exact mechanism of reducing intraocular pressure is still unclear. Tonometry and aqueous humor fluorescence studies suggest that the intraocular pressure-lowering effect of this product is related to reducing aqueous humor production. 3. Carcinogenicity: Animal experiments have shown that long-term and large-scale oral administration of timolol maleate can significantly increase the incidence of adrenal pheochromocytoma in male rats, benign and malignant lung tumors in female mice, benign uterine polyps and breast cancer. 4. Reproductive toxicity: Animal experiments have shown that large doses of oral timolol maleate have adverse effects on the reproductive function of both male and female mice.
Specifications	5ml: timolol 25mg and pilocarpine nitrate 100mg

Registered Holders

SPERA NEXUS INC

United States
Active
スペラネクサス株式会社

Japan
Active
ZHEJIANG AUSUN PHARMACEUTICAL CO LTD

United States
Active

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HANGZHOU LEAP CHEM CO., LTD. Contact Supplier

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CAS No.: 54-71-7

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Hangzhou Hyper Chemicals Limited Contact Supplier

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Guide of Pilocarpine hydrochloride

Description
Basic Attributes
Characteristics
Safety Information
Drug Information
Use and Manufacturing
Computed Properties
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
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Pilocarpine hydrochloride

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