Taxonomic Class

Rutaceae

Common Trade Names

Multi-ingredient preparations: Jaborandi, Origin Hair and Scalp Therapy, Wonder Gel, X-Tablets

Common Corms

The leaves from the jaborandi tree are available as essential oil, fluidextract, a powder, and tincture. Combination products are found as gels and tablets. Pilocarpine, the main active ingredient, is available in many prescription products:

Ocular insert: 20 mcg, 40 mcg

Ophthalmic gel: 4%

Ophthalmic solution: 0.25%, 0.5%, 1 %,2%,3%,4%,5%,6%,8%, 10%

Tablets: 5 mg

Source

Pilocarpus, or jaborandi, consists of the leaves of Pilocarpus jaborandi (Pernambuco jaborandi), Pilocarpus microphyllus (Maranham jaborandi), or Pilocarpus pinnatifolius (Paraguay jaborandi). The plant is native to the northern and northeastern parts of Brazil.

Chemical Components

Three alkaloids are found in jaborandi: pilocarpine, pilocarpidine, and isopilocarpine. Also reported are jaborine, pilosine, volatile oils (including dipentene), and jaboric, pilocarpic, and tannic acids.

Actions

When applied topically to the eye, pilocarpine stimulates muscarinic receptors; this causes the pupil to constrict and the ciliary body to contract, thus improving the outflow of aqueous humor. Muscarinic alkaloids, when administered orally, stimulate the smooth muscles of the GI tract, increasing motility and tone. The tone and motility of other organs or organ systems (such as the ureter, bladder, gallbladder, and biliary ducts) may also be increased. Pilocarpine causes increased sweating and salivation in humans. It acts on the CV and respiratory systems as well (decreases blood pressure, heart rate, and vital capacity). In cats, pilocarpine has caused cortical stimulation .

Jaborine, a component found in the leaves, may actually be antagonistic to pilocarpine. Tannic acid has local astringent properties that act on the GI mucosa and has shown anti ulcerative and antisecretory effects within the GI tract.

Reported Uses

Although jaborandi has several reported uses, pilocarpine is usually extracted and used to stimulate saliva secretion or as a diaphoretic or myotic . Pilocarpine is primarily used to treat glaucoma or xerostomia. Other reported uses of the jaborandi plant include treatment of Bright’s disease, deafness, diabetes, edema, intestinal atony, jaundice, nausea, nephritis, pleurisy, psoriasis, rheumatism, syphilis, and tonsillitis. A decoction of the leaf applied locally has been used as a treatment for baldness.

Dosage

For glaucoma, 1 or 2 gtt applied t.i.d. or q.i.d. Refer to package insert for pilocarpine for specific dosing information.

For xerostomia, 15 to 30 mg P.O. daily; a dose of 100 mg P.O. is considered fatal.

The following daily doses have been suggested: powdered leaves, 5 to 60 grains (0.324 to 3.9 g); fluidextract, 10 to 30 gtt; tincture, Y, to 1 dram (1.75 to 3 ml).

Adverse Reactions

CNS: headache.

CV: bradycardia.

EENT: increased salivation, lacrimation, visual changes.

GI: nausea, vomiting.

Skin: sweating.

Interactions

Anticholinergics (atropine, ipratropium, scopolamine, other belladonna­type alkaloids): May decrease effects of these drugs. Avoid administration with jaborandi.

Beta blockers: May cause conduction problems. Monitor the patient.

Glycosides, iron-containing compounds, other alkaloids: Tannic acid may interact with these drugs. Do not use together.

Other prescription products containing pilocarpine, other muscarinic agonists (arecoline, methacholine, muscarine), cholinesterase inhibitors (do­nepezil, edrophonium, physostigmine): May have additive effect when used concomitantly. Use cautiously to avoid toxicity.

Contraindications And Precautions

Jaborandi is contraindicated in patients who are hypersensitive to pilocarpine and in those with uncontrolled asthma, acute iritis, and angleclosure glaucoma. Avoid use in pregnant or breast-feeding patients. Avoid large doses of jaborandi because hepatic injury can occur, especially in patients with preexisting hepatic disease. Use cautiously in patients with significant CV disease, biliary tract or urogenital abnormalities (cholelithiasis, nephrolithiasis), and preexisting cognitive or psychiatric disorders.

Special Considerations

Monitor intraocular pressure in patients at risk for glaucoma.

Monitor liver transaminase levels; if they increase, the product should be discontinued immediately.

Inform the patient that excessive sweating may lead to dehydration if fluids are not replenished.

Alert Signs of pilocarpine toxicity include exaggerated muscarinic effects. Extreme cases may lead to severe bronchospasm, hypotension, pulmonary edema, and shock. Treatment consists of atropine administration and general support of the CV and respiratory systems to counteract the effects from pulmonary edema .

Urge the patient to immediately report symptoms associated with pilocarpine toxicity (excessive sweating, lacrimation, increased salivation, nausea, vomiting, hypotension, and bradycardia) or hepatic dysfunction (fever, jaundice, and pain in right upper quadrant). Instruct him to discontinue use of the product if they occur.

Caution the patient that pilocarpine may cause visual changes, especiallyat night, which may impair his ability to drive.

Advise the pregnant or breast-feeding patient not to use jaborandi.

Commentary

The jaborandi tree is regarded as a source for pilocarpine. Much information exists about the use of pilocarpine for treating glaucoma and xerostomia. No human studies are available that support the use of jaborandi leaves for any medicinal purpose. Patients with glaucoma, xerostomia, or other potentially treatable conditions should seek medical advice because self-medication with jaborandi is not advised.


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