Pilocarpus jaborandi

Examples of alkaloid of relative pharmaceutical usefulness so far characterized from Rutaceae are pilocarpine from Pilocarpus jaborandi Holmes. This imidazole alkaloid is occasionally used to treat glaucoma. 

The choline ester, carbachol, activates M-cholinoceptors, but is not hydrolyzed by AChE. Carbachol can thus be effectively employed for local application to the eye (glaucoma) and systemic administration (bowel atonia, bladder ato-nia). The alkaloids, pilocarpine (from Pilocarpus jaborandi) and arecoline (from Areca catechu betel nut) also act as direct parasympathomimetics. As tertiary amines, they moreover exert central effects. The central effect of muscarinelike substances consists of an enlivening, mild stimulation that is probably the effect desired in betel chewing, a widespread habit in South Asia. Of this group, only pilocarpine enjoys therapeutic use, which is limited to local application to the eye in glaucoma... 

Pilocarpine (15) Pilocarpus jaborandi Holmes (jaborandi), and related species Cholinergic (parasympathomimetic)... 

The basic alkaloid in Pilocarpus jaborandi (Rutaceae) is pilocarpine, a molecule of which contains an imidazole nucleus and is also used as a clinical drug. During alkaloid synthesis, L-histidine can produce the manzamine nucleus (Figure 27). These alkaloids are quite widespread, though they were first isolated in the late 1980s in marine sponges. They have an unusual polycyclic system and a very broad range of bioactivities. Common alkaloids with this nucleus include manzamine A, manzamine B, manzamine X, manzamine Y, sextomanzamine A and so on. 

Source leaflets of South American shrub Pilocarpus jaborandi Uses treatment of open-angle glaucoma... 

Histidine is a precursor of a very limited number of alkaloids. The most well-known is pilocarpine from Pilocarpus jaborandi. The plant was formerly used as a truth serum (diaphoretic activity), and the alkaloid is used to counter the mydriatic effects of atropine. 

Pilocarpine Cholinergic agent used for glaucoma Pilocarpus jaborandi Jaborandi tree... 

The leaves of Pilocarpus species, including Pilocarpus jaborandi (jaborandi) and Pilocarpus racemosus (acei-tillo), contain pilocarpine or isopilocarpine as major alkaloids as well as a variety of minor alkaloids. Pilocarpine (see separate monograph) is an agonist at acetylcholine receptors, which enhances salivary flow, sweating, and gastrointestinal motility. It can interfere with asthma therapy and the effect of anticholinergic drugs. 

Limonis Cortex Outer rind of ripe fruit Citrus medica Northern India Limonum Pilocarpus Jaborandi ... 

Pilocarpine Hydrochloride, USP. Pilocarpine mono-hydrochloride is the hydrochloride of an alkaloid oblaineil from the dried leaflets of Pilocarpus jaborandi or P. micro-pliylltis, in which it occurs to the extent of about 0.39 together with other alkaloids. 

Pilocarpine, the salt of an alkaloid obtained from Pilocarpus Jaborandi, is an example of a muscarinic agonist that does not adhere to the traditional SAR. In 1876, Langley reported that extracts containing the alkaloid stimulated the end organs of parasympathetic neurons. The structure of pilocarpine was reported in 1901. 

Pilocarpus jaborandi leaf Pilocarpus microphyllus leaf Pilocarpus pennatifolius leaf Piper longum fruit Piper methysticum rhizome, root Piper nigrum fruit Scutellaria baicalensis root... 

CiiHi NjOa, Mr 208.26, oily liquid or crystals, mp. 34 °C (as hydrochloride 193-205 °C, nitrate I74°C), bp. 260°C (0.7 kPa), [a] > +106° (HjO), soluble in water, ethanol, chloroform forms well crystallizing salts with acids. P. is the main alkaloid of the South American jaborandi tree (Pilocarpus jaborandi). It is isolated from the leaves. P. is also easily accessible by synthesis and is used as its salts in medicine as a cholinergic parasympathicomimetic, miotic (for glaucoma) agent and as an atropine antagonist it is also used in veterinary medicine for colics and constipation. Detection by means of Helch s reaction. Pilocarpus species contain further imidazole alkaloids (see table). 

Jaborandi is the name of the crude drug prepared from the evergreen plants Pilocarpus jaborandi and Pilocarpus pinnatifolius, which grow wild in South America, especially in Brazil. In South America, 13 plants in this genus are known, and all are used as the material for Jaborandi, which is important as the material for the extraction of pilocarpine. 

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