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Pilocarpine nitrate

Pilocarpine nitrate structure

CAS No:
148-72-1
Formula:
C11H16N2O2.HNO3
Chemical Name:
Pilocarpine nitrate
Synonyms:
2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,(3S,4R)-,nitrate (1:1);Pilocarpine,mononitrate;2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,(3S-cis)-,mononitrate;2(3H)-Furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-,(3S,4R)-,mononitrate;Pilocarpine nitrate;Pilocarpine subnitrate;Pilagan;(+)-Pilocarpine nitrate
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

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

A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

Pilocarpine nitrate Basic Attributes

Molecular Weight：

271.27

Exact Mass：

271.11700

EC Number：

205-723-7

UNII：

M20T465H6J

NSC Number：

757282

HScode：

2934999090

Characteristics

PSA：

110.17000

XLogP3：

1.33730

Appearance：

white

Melting Point：

178 °C

Boiling Point：

520.5ºC at 760 mmHg

Flash Point：

268.6ºC

Refractive Index：

81 ° (C=2, H2O)

Water Solubility：

H2O: 0.1 g/mL, clear, very faintly yellow

Storage Conditions：

2-8°C

Vapor Pressure：

1.16E-11mmHg at 25°C

Specific rotation：

D +77 to +83° (c = 10)

Collision Cross Section：

146.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3087

wgk germany：

hazard class code：

22-26/28

safety instructions：

1-25-45

RTECS Number：

TK1455000

Marks：

Xn,T+

Precautionary statement(s)：

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

Hazard Statements：

H300 + H330

Drug Information

MeSH：

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.)|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.)

MeSH Entry Terms：

Hydrochloride, Pilocarpine

Pilocarpine nitrate Use and Manufacturing

Uses

Antiglaucoma drug;Cholinergic

Manufacturing Info：

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

Computed Properties

Molecular Weight:271.27
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:3
Exact Mass:271.11682065
Monoisotopic Mass:271.11682065
Topological Polar Surface Area:110
Heavy Atom Count:19
Complexity:270
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Pilocarpine is a direct-acting cholinergic drug that works by directly stimulating muscarinic receptors located on the pupillary sphincter, ciliary body, and secretory glands. Pilocarpine contracts the pupillary sphincter, causing the peripheral iris to leave the anterior wall of the angle, opening the angle and increasing the discharge of aqueous humor. At the same time, this product also contracts the longitudinal fibers of the ciliary muscle, increases the tension of the scleral process, opens the trabecular meshwork gap, reduces the resistance to aqueous humor drainage, increases the discharge of aqueous humor, and reduces intraocular pressure.

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

Pilocarpine nitrate eye drops
Ingredients	The main ingredient of this product is pilocarpine nitrate. Its chemical name is 4-[(1-methyl-1H-imidazol-5-yl)methyl]-3-ethyldihydro-2(3H)-furanone nitrate. Molecular formula: C11H16N2O2HNO3, molecular weight: 271.27
Indication	1. This product has a synergistic effect when used in combination with beta-receptor blockers, carbonic anhydrase inhibitors, beta-adrenergic receptor agonists or hypertonic dehydrating agents. 2. This product combined with latanoprost can reduce the amount of aqueous humor outflow through the uveoscleral pathway and reduce the intraocular pressure lowering effect. 3. Combination with local anticholinergic drugs will interfere with the intraocular pressure lowering effect of this product. Combination with an appropriate amount of systemic anticholinergic drugs usually does not affect the intraocular pressure lowering effect of this product because the concentration of systemic drugs reaching the eye is very low.
Specifications	5ml:100mg
Manufacturer	Jinyao Yongguang (Hebei) Pharmaceutical Co., Ltd.

Pilocarpine nitrate eye drops
Ingredients	Pilocarpine nitrate
Indication	1 This product has a synergistic effect when used in combination with beta-receptor blockers, carbonic anhydrase inhibitors, alpha and beta-adrenergic receptor agonists or hypertonic dehydrating agents. 2 This product combined with latanoprost can reduce the amount of aqueous humor outflow through the uveoscleral pathway and reduce the intraocular pressure lowering effect. 3 Combination with local anticholinergic drugs will interfere with the intraocular pressure lowering effect of this product. Combination with an appropriate amount of systemic anticholinergic drugs usually does not affect the intraocular pressure lowering effect of this product because the concentration of systemic drugs reaching the eye is very low.
Specifications	5ml:25mg
Manufacturer	Anhui Shuangke Pharmaceutical Co., Ltd.

Pilocarpine nitrate eye drops
Ingredients	The main ingredient of this product is pilocarpine nitrate.
Indication	1. This product has a synergistic effect when used in combination with beta-receptor blockers, carbonic anhydrase inhibitors, alpha and beta-adrenergic receptor agonists or hypertonic dehydrating agents. 2. This product combined with latanoprost can reduce the amount of aqueous humor outflow through the uveoscleral pathway and reduce the intraocular pressure lowering effect. 3. Combined use with local anticholinergic drugs will interfere with the intraocular pressure lowering effect of this product. Combined use with an appropriate amount of systemic anticholinergic drugs usually does not affect the intraocular pressure lowering effect of this product because the concentration of systemic drugs reaching the eye is very low.
Specifications	5ml:50mg
Manufacturer	Hangzhou Guoguang Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

Guangzhou Greensyn Pharma Co., Ltd.

China
Active
Guangdong Leawell Pharmaceutical Co., Ltd.

China
Active
ANIDRO DO BRASIL EXTRACOES S.A.

European Union
Active

See More Registered Holders

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