Pilocarpine Hydrochloride

Inquiry

Cat Number

API0231624

CAS Number

54-71-7

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Customer Q&A

CAS Number

54-71-7

EINECS

200-212-5

Storage

Store at room temperature

Synonyms

Pilocarpine HCl; Salagen; Pilocarpine monohydrochloride; Sno pilo; Isopto carpine; Vistacarpin N

Molecular Formula

C11H17ClN2O2

Molecular Weight

244.72

Smiles

CC[C@H]1[C@H](COC1=O)CC2=CN=CN2C.Cl

Appearance

White to off-white crystalline powder

Melting Point

202-205℃

Boiling Point

431.8℃ at 760 mmHg

Relative Density

1.22

General Description

Pilocarpine hydrochloride is a natural alkaloid muscarinic receptor agonist used to treat dry mouth (xerostomia) and dry eyes. It is available as oral tablets for systemic use and as ophthalmic solutions for topical application. The drug has a short duration of action and requires multiple daily dosing.

Mechanism of Action

Pilocarpine directly binds to and activates M1, M2, and M3 muscarinic acetylcholine receptors on salivary, sweat, lacrimal, and gastrointestinal glands. This stimulation increases secretion of saliva, tears, sweat, and digestive juices via intracellular calcium mobilization. In the eye, topical pilocarpine contracts the iris sphincter (miosis) and ciliary muscle, improving aqueous humor outflow and lowering intraocular pressure.

Application

Oral pilocarpine is indicated for xerostomia due to Sjögren's syndrome or radiation therapy for head and neck cancer. Ophthalmic pilocarpine is used for primary open-angle glaucoma, ocular hypertension, and acute angle-closure glaucoma (emergency miosis). It is also employed to reverse mydriasis after ocular examination.

In a retrospective case‑control study (56 patients with unilateral Adie’s tonic pupil, 61 controls), the diagnostic accuracy of the dilute pilocarpine test was compared using two concentrations. The area under the ROC curve was significantly larger for 0.0625% (0.954) than for 0.125% (0.840, P=0.047). A change in maximal pupil diameter of ≥0.5 mm after 0.0625% pilocarpine yielded 100% sensitivity and 82.8% specificity. Digital pupillometry reliably quantified the response. The authors recommend 0.0625% pilocarpine for detecting denervation supersensitivity in Adie’s tonic pupil.

Fig. 1 Representative cases of dilute pilocarpine test in unilateral Adie's tonic pupil. (Yoo YJ, et al., 2021)

References

Yoo YJ, et al. Dilute pilocarpine test for diagnosis of Adie's tonic pupil. Sci Rep. 2021;11(1):10089.

Does Pilocarpine Hydrochloride require protection from light during long-term storage?

Yes, it is photosensitive. UV light can cause photodegradation and racemization at the chiral centers. Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Pilocarpine Hydrochloride?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which accelerates epimerization to isopilocarpine.

Is Pilocarpine Hydrochloride stable in ophthalmic solution formulations?

Formulated solutions require pH control (around 4-5) and preservatives (e.g., benzalkonium chloride) for stability. We provide long-term stability data for ophthalmic presentations.

How is the impurity isopilocarpine (the epimer) monitored during stability?

This primary degradation product is specifically quantified using a stability-indicating chiral HPLC method, ensuring it remains below pharmacopoeial limits.