Pilocarpus jaborandi

Botanical Name : Pilocarpus jaborandi
Family: Rutaceae
Genus: Pilocarpus
Kingdom: Plantae
Order: Sapindales

Synonym: Pilocarpus cearensis, P. officinalis

Common Name :Jaborandi, indian hemp, jaborandi-do-norte, catai-guacu, ibiratai, pimenta-de-cachorro, arruda do mato, arruda brava, jamguarandi, juarandi

Habitat:  Pilocarpus jaborandi is native to the neotropics of South America. Various species are important pharmacologically. Many of the species have the common name Jaborandi.(There are about 13 species of plants belonging to the family Rutaceae)

Selected species are:
*Pilocarpus jaborandi (Pernambuco Jaborandi)
*Pilocarpus microphyllus (Maranham Jaborandi)
*Pilocarpus racemosus (Guadeloupe Jaborandi)
*Pilocarpus pennatifolius (Paraguay Jaborandi)
*Pilocarpus spicatus (Aracati Jaborandi)

Description:
Jaborandi refers to a three to seven meter high shrubby tree with smooth grey bark, large leathery leaves and thick, small, reddish-purple flowers. The leaves contain an essential oil which gives off an aromatic balsam smell when they are crushed. Jaborandi is native to South and Central America and to the West Indies. Several Pilocarpus species are called jaborandi and used interchangeably in commerce and herbal medicine, including the main Brazilian species of commerce: P. jaborandi, and P. microphyllus, and the Paraguay species P. pennatifolius. All three tree species are very similar in appearance, chemical constituents and traditional herbal medicine uses. The word jaborandi comes from the Tupi Indians and it means “what causes slobbering” describing its ancient use in their rainforest herbal pharmacopeia.

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Constituents:  Pilocarpine, jaborine, volatile oil, tannic acid, volatile acid, potassium chloride.

Jaborandi is a perfect example of a plant which made the transition from Amazonian indigenous tribal use, to folklore use, and then into modern medicine based upon natural chemicals found in the plant. In 1875, two researchers independently discovered an alkaloid in jaborandi leaves which was named pilocarpine. Tests revealed that pilocarpine was responsible for much of the biological activity of the plant-especially it’s ability to induce sweating and salivation, as well as to lower intraocular pressure in the eyes (making it an effective treatment in certain types of glaucoma). In 1876, the isolated pilocarpine alkaloid was introduced into conventional ophthalmology for the treatment of glaucoma. The mixture of pilocarpine and another natural product, physostigmine, remains to this day one of the mainstay drugs in ophthalmology. Interestingly, scientists have never been able to fully synthesize the pilocarpine alkaloid in the laboratory; the majority of all pilocarpine drugs sold today are derived from the natural alkaloid extracted from jaborandi leaves produced in Brazil.

Pilocarpine eye drops are still sold as a prescription drug worldwide for the treatment of glaucoma and as an agent to cause constriction of the pupil of the eye (useful in some eye surgeries and procedures). In the treatment of glaucoma, pilocarpine causes the iris of the eye to contract, which leads to the opening of the space between the iris and the cornea and, in effect, relieves narrow-angle glaucoma. It is even being used as a tool for the diagnosis of Alzheimer’s disease in early stages; the eye constriction response to pilocarpine was found to be greater in Alzheimer’s patients than in controls. Tablets of pilocarpine are also manufactured and prescribed to cancer patients to treat dryness of the mouth and throat caused by radiation therapy as well as to patients with Sjogren’s syndrome (an autoimmune disease in which immune cells attack the moisture-producing glands causing dry mouth and eyes). So as history shows; the Indian’s “slobber-mouth” plant made it out of the jungles of the Amazon and into mainstream medicine and pharmaceutical use (for the identical uses the Indians employed it for). As usual, however, the Indians never realized any profits from the resulting manufacture and sales of several drugs over the last 50 years that made use of their plant knowledge.

In addition to pilocarpine, jaborandi leaves contain terpenes, tannic acids and other alkaloids. The natural leaf contains an average of 0.5% pilocarpine, plus similar amounts of other alkaloids such as isopilocarpine, jaborine, jaboridine and pilocarpidine. The alkaloids in jaborandi (including pilocarpine) are a rather rare and unique type of alkaloid that are derived from histidine (an amino acid) and classified as imidazole alkaloids. The main chemicals found in jaborandi include: 2-undecanone, alpha-pinene, isopilocarpidine, isopilocarpine, isopilosine, jaborine, jaborandine, jaboric, limonene, myrcene, pilocarbic acid, pilocarpidine, pilocarpine, pilosine, sandaracopimaradiene, and vinyl-dodecanoate.

Biological Activities and Clinical Research:  

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There are well over a thousand clinical studies published on pilocarpine. As with most plant-based drugs, however, the use of the whole natural plant fell out of use as a natural remedy (and failed to attract further research efforts) in favor of the single isolated active ingredient that was turned into a prescription drug. The PDR for Herbal Medicines indicates that the effects of jaborandi leaves are as follows: increases the secretion of saliva, sweat, gastric juices and tears, and stimulates the smooth muscle of the gastrointestinal tract, bronchi, bile duct and bladder. Herbalists and natural health practitioners attribute the same biological activities for the plant as the main activities clinically validated for pilocarpine, but there is no actual clinical research on leaf extracts to support them or qualify them. Another problem is trying to determine effective dosages of leaf extracts (in the absence of clinical research). The pilocarpine content of the leaf can vary – between different “jaborandi” tree species, as well as when different harvesting methods, growth habitats, and even storage, handling and drying methods of the harvested leaves are used. The pilocarpine chemical is fragile; dried jaborandi leaves have shown to lose as much as 50% of their pilocarpine content in as little as a year of storage. Another alkaloid in the leaf, jaborine, has shown to counteract or decrease the effects of pilocarpine, which means that one cannot simply relate the effective dosage of a leaf extract based solely upon the pilocarpine content of the extract.

Finally, one must consider that the longstanding documented use of pilocarpine is not with side effects, toxicity or contraindications. Knowing at least an approximate amount of such an active chemical in a leaf extract is certainly necessary to help determine the extract’s efficacy and safety. The lethal dose of pilocarpine is reportedly 60 mg, which could correspond to as little as 5-10 grams of the leaves. Individuals with cardiac and circulatory problems may even have a lower lethal dosage. Reported side effects for non-lethal dosages of pilocarpine include vomiting, nausea, sweating, convulsions, increased heart rate, difficulty in breathing, and bronchial spasms. Interestingly, a positive side effect of reported use of the pilocarpine eye solution drug was an improvement in sleep apnea and snoring in glaucoma patients using the drug.

Current Practical Uses:

The use of jaborandi is best left in the hands of experienced herbalists and health practitioners since pilocarpine has such pronounced biological activities and it occurs in significant amounts in the natural leaf. (The oral pilocarpine prescription drug, Salagen® is only 5 mg of pilocarpine, so very little is required for a pharmacological effect.) In recent years demand by U.S. consumers for the natural leaf has been increasing, mainly fueled by the high cost of pilocarpine drugs and the rather new uses of it in cancer therapy (as a saliva enhancement agent). However, it still is not recommended to be used by the average lay-person. The natural leaf is not widely available in the U.S. today and importation of it as a natural product is a bit in the grey area since pilocarpine is sold as a regulated prescription drug. In fact, Brazil is the largest producer today of jaborandi leaves. However, 100% of Brazil’s jaborandi leaf production goes into drug manufacture, including Merck Pharmaceuticals who located a manufacturing plant in Brazil specifically for the processing and manufacture their pilocarpine prescription drugs. Current laws in Brazil prohibit the export of jaborandi leaves as a natural product, as they regulate even the leaves as a drug.

Medicinal Uses:
Used internally for psoriasis, itching of the skin, syphilis, chronic excess mucus, and dropsy (leaf extracts).  Internally and externally used for glaucoma and as an antidote to atropine; externally for hair gloss (leaf extracts).

Clinical research is still ongoing today on the isolated alkaloid of Jaborandi leaves, pilocarpine. Some of the latest research is now focused on the topical applications of it as a transdermal penetration agent for other pharmacologic agents since it has the ability to open skin pores and promote capillary blood circulation. These effects are also attributed to its use as a topical agent for baldness.

Precauations:
*Pilocarpine has shown to increase the rate of birth defects in animal studies. Jaborandi should not be taken during pregnancy or while breastfeeding.

*Both jaborandi and pilocarpine may cause headaches and can irritate the stomach and cause vomiting and nausea. An overdose may cause such symptoms as flushing, profuse sweating and salivation, urinary frequency, nausea, rapid pulse, contracted pupils, diarrhea or fatal pulmonary edema.

*The plant may induce bradycardia. Those with cardiac or circulatory conditions should not take jaborandi.

*Jaborandi may induce dehydration due to excessive perspiration and urination. If using jaborandi, electrolyte and fluid status must be monitored and maintained.

Drug Interactions:

*May potentiate cardiac medications.
*May potentiate diuretic medications.
*May potentiate cholinergic medications.
*May potentiate diaphoretics.

Disclaimer : The information presented herein is intended for educational purposes only. Individual results may vary, and before using any supplements, it is always advisable to consult with your own health care provider

Resources:
http://en.wikipedia.org/wiki/Pilocarpus
http://rainforest-database.com/plants/jaborand.htm
http://www.herbnet.com/Herb%20Uses_IJK.htm

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