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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. Pilocarpine eye drops are still sold as a prescription drug worldwide for the treatment of glaucoma and as an agent to cause constriction (opposite of dilation) 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.
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 human 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, hypotension, 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!
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.
May potentiate cardiac medications.
May potentiate diuretic medications.
May potentiate cholinergic medications.
May potentiate anti-glaucoma medications.
May potentiate diaphoretics.
C11H16N2O2 = 208.148
Pilocarpine is an alkaloid obtained commercially from jaborandi leaves, in which it occurs in very variable quantity, but rarely more than 0.5 per cent., and is associated with a small proportion of its isomer, isopilocarpine. The pure alkaloid is best obtained by adding excess of ammonia to an aqueous solution of one of its salts, and extracting with chloroform, washing the latter to remove ammonia. On evaporation or distillation of the chloroform, a colourless oily liquid remains, which may be freed from the last traces of solvent by exposing to the air in an open dish for several days. All efforts to crystallise the base have so far failed. Pilocarpine occurs as a colourless thick syrupy liquid, which becomes thinner on warming. With acids it forms salts which crystallise well, the most useful medicinally being the nitrate, on account of its stability in the air. The hydrochloride is hygroscopic. Pilocarpine hydrobromide (C11H16N2O2HBr = 289.076) occurs in white crystals. Soluble in water and in alcohol. Melting-point, 185°. It is used for similar purposes, and given in similar doses, to pilocarpine hydrochloride. By the action of heat or alkalies pilocarpine is readily converted into its isomer, isopilocarpine; the conversion is quantitative by heating with water in a scaled tube at 180° for four hours. The isomer is very similar in its chemical properties to pilocarpine; it is a syrup which can be distilled unchanged in vacuo, and forms crystalline salts with acids. It occurs naturally in small quantity in jaborandi leaves, but the greater portion is formed during the process of manufacture.
C11H16N3O5 = 271.166.
Pilocarpine nitrate, C11H16N2O2, HNO3, a salt of the alkaloid pilocarpine, obtained from jaborandi leaves. It is also official in the U.S.P. It may be prepared by neutralising diluted nitric acid with pure pilocarpine and evaporating the neutral aqueous solution thus obtained to dryness on a water-bath. The residue is taken up with boiling alcohol, from which it is allowed to crystallise; 100 parts of the salt contain 76.75 parts of the base. Pilocarpine nitrate occurs in the form of white, distinct crystals, or as a micro-crystalline anhydrous, odourless powder, having a faintly bitter taste; it is permanent in the air. Melting-point not below 173°. A concentrated, aqueous solution gives no precipitate on the addition of solution of ammonia, nor with solutions of sodium or potassium hydroxide (distinction from other alkaloids). If 1 or 2 centigrams of the salt be dissolved in 2 mils of distilled water in a test-tube, 2 mils of a slightly acidified solution of hydrogen peroxide added and a small layer of benzene be carefully poured upon the liquid, then if 3 or 4 drops of a solution of potassium bichromate (1 in 300) be added and the mixture gently shaken, the benzene layer will acquire a violet colour, while the aqueous layer will remain yellow (distinction from other alkaloids). Commercial pilocarpine nitrate is said to contain variable amounts of isopilocarpine nitrate, which lower the melting-point, the chemically pure salt melting at 177° to 178°. Rotation in aqueous solution, not lower than +80°. On ignition it leaves no residue.
Soluble in water (1 in 8), alcohol (1 in 50); almost insoluble in ether or chloroform.
Action and Uses.—Pilocarpine stimulates the terminations of certain nerves supplying unstriped muscle, the heart, and secretory glands. After administration of the drug the secretion of the salivary, sweat, gastric, intestinal, lachrymal, and mucous glands of the mouth, nose, and respiratory tract is augmented. Its action on plain muscle results in increased movements in the alimentary tract, causing perhaps nausea, colic pains, and diarrhoea. The bronchioles are constricted, so that the amount of air entering and leaving the lungs is very much diminished, an "asthmatic" condition resulting. Its action upon the terminations of the third nerve in the eye causes contraction of the pupil, with reduced intra-ocular pressure. Small doses of pilocarpine quicken the heart and raise blood pressure, but large doses have the opposite effect. Pilocarpine nitrate is given by the mouth or hypodermically, principally as a powerful diaphoretic, especially in dropsy due to renal disease and in uraemia, but it is contra-indicated in cardiac dropsy on account of its depressing action. It is sometimes given in bronchitis and in asthma, to stimulate the broncho-dilator fibres when the constrictor fibres are fatigued, and is employed, with potassium bromide, in epilepsy and nervous affections. In ophthalmic surgery, pilocarpine nitrate is employed, like physostigmine, to contract the pupil and reduce intra-ocular pressure in glaucoma, detachment of the retina and intra-ocular haemorrhage. A slight increase of tension at first occurs, and the contraction is less complete, and of shorter duration, than that produced by physostigmine. The action of pilocarpine is in all cases antagonised by atropine. Pilocarpine nitrate is best administered by hypodermic injection in doses of from 1/10 to 1/4 grain. Pills may be prepared with milk sugar and glucose. Larger initial doses than 1/20 grain by the mouth are not well tolerated. For ophthalmic use 0.5 per cent. solutions are suitable. Pilocarpine nitrate has been used with good results in aural vertigo and tinnitus aurium; it has been recommended for use in lotions (1 in 250) to promote the growth of the hair, its effect being attributed to stimulation of the glands of the scalp. In cases of poisoning by pilocarpine the stomach should be emptied, and belladonna given by the mouth or atropine hypodermically.
Dose.—3 to 30 milligrams (1/20 to 1/2 grain).
The action of the fluid extract or tincture of jaborandi and impure pilocarpine is sometimes disappointing, failing entirely to produce their characteristic influence and perhaps producing results contrary to those anticipated. This is due to the presence of the alkaloid, jaborine, which acts antagonistically to pilocarpine, having in its therapeutic influence many of the characteristics of atropine, an antagonist of pilocarpine.
The nitrate and hydrochlorate of pilocarpine carefully prepared are free from jaborine and are thus reliable in their action. Solutions of pilocarpine should be made fresh when needed, as the salts decompose in aqueous solution. They are not permanent but will precipitate at once in alkaline solutions.
Physiological Action—Near the point of the administration of a hypodermic injection of the alkaloid, a few drops of sweat appear within from four to six minutes after the injection, to be immediately followed with moisture on the forehead, neck and chest, and in quick succession the entire body is bathed with a most profuse perspiration.
It is a powerful anti-diphtheritic and sialogogue, acting profoundly as a stimulant upon the secretions of the entire glandular system. No one known remedy stimulates every secretion of the body simultaneously as profoundly as does this agent.
The depression of the agent should not be allowed to progress; after the sweating has continued a few minutes profusely, a little whisky, brandy, tincture of ginger, or tincture of capsicum should be given in hot water, and occasionally repeated while the transpiration progresses. If the heart shows the influence of the depression, a hypodermic of strychnine may be given, or a few drops of the tincture of cactus, strophanthus, digitalis, or nux vomica. If it is desirable to stop the sweating abruptly, atropine hypodermically may be resorted to.
The extreme effects of the agent need not be obtained in many cases, but owing to the susceptibility of some cases a small dose will sometimes produce extreme results. It is safe to obtain these results in extreme sthenic cases—in robust patients. The reaction will be prompt and satisfactory.
Most observers state that it is best to quench the thirst with weak coffee or milk and not with-cold water. It is undesirable that the patient swallow the saliva when the agent is administered after the bite of venomous snakes or in threatened hydrophobia or if given as an antidote to poisons.
When the agent fails to act upon the skin it often expends its force upon the salivary glands, kidneys, stomach, intestines or lungs, producing extreme secretion or excretion from these organs. In some cases this agent produces nausea, vomiting, diarrhea, contracted pupil, extreme weakness, dimness of vision, sighing respiration, palpitation and collapse; but these symptoms of alarming nervous depression rarely occur and are easily combated with atropine.
Specific Symptomatology—The direct indications for this agent are acute suppression of the secretions, especially of those of the skin in sthenic conditions usually with distress, elevation of temperature, sharp, hard pulse, dry skin, dry mucous membranes, constipation, and small quantity of urine with dark color and high specific gravity.
Kinnett gives the specific indications for its use, as dry hot skin, dry parched mouth, pulse full and very strong, patient restless and uneasy, suppression of the secretions, especially of the kidneys, which seem to be unable to act properly. His contra-indications are feebleness, weak pulse, weak heart action, tendency to depression.
Contra-Indication—Jaborandi should be avoided in asthenic conditions, or where there is feeble or dilated heart, and used with care in old people and-young children. Except in its influence on laryngeal and bronchial disorders, and in the sthenic stage of diphtheria when it loosens the membranes.