Pilocarpine

208.26

208.26

202-128-4

01MI4Q9DI3

DTXSID1021162

C62068

OIL OR CRYSTALS|NEEDLES

S01EB01|N - Nervous system|S - Sensory organs

2939800000

44.1

1.1

Solid

1.2±0.1 g/cm3

34 °C

260 °C

215.0±21.2 °C

1.585

2.07e+00 g/L

KEEP WELL CLOSED & PROTECTED FROM LIGHT. /HCL/

D18 +106° (c = 2)

6.78None

6.78|PK1= 7.15; PK2= 12.57 @ 20 °C

WHITE CRYSTALS; SLIGHTLY BITTER; MP: 195-198 °C; ALSO GIVEN AS 204-205 °C; 1 G DISSOLVES IN 0.3 ML WATER, 3 ML ALCOHOL, 366 ML CHLOROFORM; INSOL IN ETHER; /HCL/|ODORLESS, FAINTLY BITTER CRYSTALS; SOLN ACID TO LITMUS; PKA1= 6.8, PKA2= 1.3 /HCL/|MP: 173.5-174.0 °C DECOMP; SPECIFIC OPTICAL ROTATION: +77 DEG TO +83 °FOR D (SODIUM) LINE (10%); 1 G DISSOLVES IN 4 ML WATER, 75 ML ALCOHOL; INSOL IN CHLOROFORM, ETHER /NITRATE/|SOL ARE ACID TO LITMUS /NITRATE/|WHITE POWDER OR CRYSTALS FROM ALC /NITRITE/

III

6.1(b)

1544

3

26/28

25-45

TK1400000

T+

STABLE IN AIR BUT AFFECTED BY LIGHT. /NITRATE/

P260-P264-P284-P301 + P310-P310

H300 + H330

|Danger|H300: 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|H300+H330 (97.44%): Fatal if swallowed or if inhaled [Danger Acute toxicity, oral; acute toxicity, inhalation]|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|P260, P262, P264, P270, P280, P301+P310, P302+P350, P307+P311, P310, P321, P322, P330, P361, P363, P405, and P501

In clinical trials of pilocarpine, serum enzyme elevations were uncommon and no more frequent than with placebo. Despite, wide scale use, there have been no published reports of acute liver injury attributable to pilocarpine.

PILOCARPINE IS CHIEF ALKALOID OBTAINED FROM LEAFLETS OF SOUTH AMERICAN SHRUBS OF GENUS PILOCARPUS. ...IT WAS LONG KNOWN BY NATIVES THAT CHEWING OF LEAVES OF PILOCARPUS PLANTS CAUSED SALIVATION, 1ST EXPT WERE...PERFORMED IN 1874 BY BRAZILIAN PHYSICIAN NAME COUTINHOU.|FROM PILOCARPUS JABORANDI HOLMES, RUTACEAE: PETIT, POLANOVSKI, BULL SOC CHIM (3) 17, 557, 702 (1897).

For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.|FDA Label

Pilocarpine is an orally available cholinergic agonist that is used to treat symptoms of dry mouth in patients with keratoconjunctivitis sicca (Sjögren syndrome) or with xerostomia (dry mouth) due to local irradiation. Pilocarpine has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent liver injury.

Sjögren Syndrome Agents

Miotics; Muscarinic Agonists; Parasympathomimetics|PILOCARPINE IS USED IN TREATMENT OF GLAUCOMA... IT CAN ALSO BE GIVEN IN OINTMENT OR AS LAMELLAE. ...MIOTIC ACTION OF PILOCARPINE IS USEFUL IN OVERCOMING MYDRIASIS PRODUCED BY ATROPINE; ALTERNATED WITH MYDRIATICS...EMPLOYED TO BREAK ADHESIONS BETWEEN IRIS & LENS.|PILOCARPINE IS BETTER TOLERATED THAN ANY OTHER MIOTIC. /HCL/|PILOCARPINE IS MIOTIC OF CHOICE FOR INITIAL & MAINTENANCE THERAPY IN PRIMARY OPEN-ANGLE GLAUCOMA & MOST OTHER CHRONIC GLAUCOMAS. ...USED FOR EMERGENCY TREATMENT OF ACUTE ANGLE-CLOSURE GLAUCOMA.|For more Therapeutic Uses (Complete) data for PILOCARPINE (6 total), please visit the HSDB record page.

/PILOCARPINE/...SHOULD NOT BE USED FOR LONG PERIODS IN SUCH CASES TO AVOID OR POSTPONE IRIDECTOMY BECAUSE ANY MIOTIC MAY TIGHTEN PUPIL AGAINST LENS & BLOCK FLOW OF AQUEOUS THROUGH PUPIL.

IF RESISTANCE TO PILOCARPINE DEVELOPS DURING LONG-TERM THERAPY, RESPONSIVENESS MAY SOMETIMES BE RESTORED BY SUBSTITUTING ANOTHER AGENT, SUCH AS CARBACHOL, FOR PERIOD OF TIME.

Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.

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.)

There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers|LITTLE DEFINITIVE INFORMATION IS AVAIL ON FATE & ELIMINATION OF PILOCARPINE. IT IS PARTLY DESTROYED IN BODY, BUT LARGER FRACTION IS EXCRETED IN URINE IN COMBINED FORM.|PILOCARPINE PENETRATES EYE WELL; AFTER TOPICAL INSTILLATION...|POISONING HAS OCCURRED FROM CUTANEOUS ABSORPTION.

Possibly occurs at the neuronal synapses and in the plasma|Pilocarpine has known human metabolites that include 3-hydroxypilocarpine.

0.76 hours

Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.|...ACT PRIMARILY @ MUSCARINIC RECEPTORS OF AUTONOMIC EFFECTOR CELLS, GANGLIONIC EFFECTS CAN ALSO BE OBSERVED. THIS IS PARTICULARLY TRUE OF PILOCARPINE, ALTHOUGH ITS GANGLIONIC ACTION ALSO INVOLVES STIMULATION OF MUSCARINIC RECEPTORS...|...AFTER TOPICAL INSTILLATION, MIOSIS BEGINS IN 15 TO 30 MIN & LASTS 4 TO 8 HR. REDUCTION OF INTRAOCULAR PRESSURE IS MAXIMAL IN 2 TO 4 HR, WHICH CORRELATES WITH MAX DECR IN OUTFLOW RESISTANCE. EFFECT ON INTRAOCULAR PRESSURE OUTLASTS EFFECT ON OUTFLOW FACILITY...PILOCARPINE...MAY DECR AQUEOUS PRODUCTION.|...PILOCARPINE /HAS AS/...PRINCIPAL ACTION STIMULATION OF SAME AUTONOMIC EFFECTOR CELLS AS THOSE ACTED UPON BY CHOLINERGIC POSTGANGLIONIC NERVE IMPULSES.|...PILOCARPINE...PRINCIPAL ACTION STIMULATION OF SAME AUTONOMIC EFFECTOR CELLS AS THOSE ACTED UPON BY CHOLINERGIC POSTGANGLIONIC NERVE IMPULSES. IN THIS RESPECT...RESEMBLE CHOLINE ESTERS...

TREATMENT CONSISTS IN PARENTERAL ADMIN OF ATROPINE, & ADEQUATE MEASURES TO SUPPORT RESP & CIRCULATION & TO COUNTERACT PULMONARY EDEMA.

LOCAL IRRITATION, ALLERGIC REACTIONS, & SYSTEMIC EFFECTS ARE UNCOMMON. 1 CASE OF MALFUNCTION IN EUSTACHIAN TUBE & DISTURBANCE IN MIDDLE EAR HAS BEEN REPORTED AFTER USE OF 4% SOLN /OF PILOCARPINE/.|HAZINESS OF CORNEAL EPITHELIUM & SUPERFICIAL CORNEAL VASCULARIZATION WITH REDNESS OF CONJUNCTIVA HAVE BEEN OBSERVED...IN 2 PT AFTER LONG-CONTINUED USE OF PILOCARPINE EYEDROPS.|ADVERSE SIDE EFFECTS FROM TOPICAL USE ON EYE ARE FEW, CONSISTING OF SENSATION OF DIMNESS OF VISION...ENFORCED ACCOMMODATION FOR NEAR, CAUSING PSEUDOMYOPIA & IMPROPER FOCUSING...BY PEOPLE BELOW AGE OF PRESBYOPIA. ACHING DISCOMFORT IN EYE FROM CONTRACTION OF CILIARY MUSCLE...@ START OF TREATMENT WITH...EYEDROPS.|SALIVARY, LACRIMAL, GASTRIC, PANCREATIC, & INTESTINAL GLANDS, & MUCOUS CELLS OF RESP TRACT ARE...STIMULATED BY.../PILOCARPINE/. ...AFTER PILOCARPINE, COMPOSITION OF SALIVA TENDS TO APPROACH...ULTRAFILTRATE OF PLASMA. ... GASTRIC GLANDS...SECRETE JUICE...ESP ABUNDANT IN PEPSIN & MUCIN...|For more Human Toxicity Excerpts (Complete) data for PILOCARPINE (12 total), please visit the HSDB record page.

Hydrochloride, Pilocarpine

ADSORBOCARPINE (BURTON, PARSONS)...ALMOCARPINE (AYERST)...ISOPTO CARPINE (ALCON)...MI-PILO (BARNES-HIND)...MISTURA P (LEDERLE)...PILOCAR (SMP)...PILOCEL (SOFTCON PRODUCTS)...PILOMIOTON (SMP)... /HCL/; PV CARPINE LIQUIFILM (ALLERGAN)...PILOFRIN LIQUIFILM (ALLERGAN)... /NITRATE/|OCUSERT PILO-20, PILO-40 /(ALZA)/

2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, (3S,4R)-: ACTIVE|/PILOCARPINE/ HAS CIS CONFIGURATION; ISOPILOCARPINE IS TRANS: ZAV'VANOL, DOKLADY ADAD NAUK SSSR 82, 257 (1952). ABSOLUTE CONFIGURATION: HILL, BARCZA, TETRAHEDRON 22, 2889 (1966).|INCOMPATIBILITIES: SILVER NITRATE, MERCURY BICHLORIDE, IODIDES, GOLD SALTS, TANNIN, CALOMEL, POTASSIUM PERMANGANATE, ALKALIES.|/OCUSERT/...IS ELLIPTICALLY SHAPED UNIT...OF PILOCARPINE-CONTAINING RESERVOIR SURROUNDED BY PERMEABLE MEMBRANE. FOLLOWING PLACEMENT BY PT, DIFFERENT FORMS OF UNIT ARE DESIGNED TO RELEASE PILOCARPINE @ RATE OF EITHER 20 OR 40 UG/HR FOR 1 WK. INTRAOCULAR PRESSURE IS REDUCED CONTINUOUSLY...WITH...LESS TOTAL DRUG...|PILOCARPINE HYDROCHLORIDE & PILOCARPINE NITRATE ARE OFFICIAL IN USP BOTH AS SALTS & AS OPHTHALMIC SOLN. AVG ORAL OR HYPODERMIC DOSE OF PILOCARPINE, NOW RARELY USED, IS 5 TO 10 MG. DEVICE FOR ACHIEVING SUSTAINED RELEASE OF PILOCARPINE INTO CUL-DE-SAC OF EYE IS ALSO AVAIL (OCUSERT).

DETERMINATION OF PILOCARPINE HCL THROUGH THE FORMATION OF POLYIODINE COMPLEXES.|HIGH SPEED LIQUID CHROMATOGRAPHY DETERMINATION OF PILOCARPINE IN PHARMACEUTICAL PREPARATIONS.|MODIFIED HIGH PRESSURE LIQUID CHROMATOGRAPHIC DETERMINATION OF PILOCARPINE HCL IN OPHTHALMIC SOLUTION.|DETERMINATION OF PILOCARPINE IN PHARMACEUTICAL PREPARATIONS BY LIQUID CHROMATOGRAPHY.

GLC METHOD FOR DETERMINATION OF PILOCARPINE WAS DEVELOPED & TESTED ON AQUEOUS HUMOR OF RABBIT EYES FOLLOWING OCULAR INSTILLATION.|ELECTRON CAPTURE GAS CHROMATOGRAPHIC METHOD FOR DETERMINING PILOCARPINE IN BLOOD & AQUEOUS HUMOR IS DISCUSSED.

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