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At least 19 recordsLinked to original sources
PubMed1984

Local anesthetic effects of cocaine and several extracts of the coca leaf (E. coca).

Cocaine and a number of different fractions of a crude ethanol extract of the coca leaf (E. coca) were subjected to a local anesthetic screen using rat tail withdrawal from electric shock. Following an intradermal injection of 0.1 ml of a 2.0% (w.v) solution of cocaine HCl, an immediate response was observed. Two of the coca fractions also produced some local anesthesia. An alkaloidal fraction, containing an equivalent amount of cocaine, produced a maximum effect that was approximately 20% less than that observed with cocaine. The only other fraction producing any effect, a water soluble cocaine-free fraction, showed a maximum response that was approximately 30% of that observed with cocaine.

Anesthetics, Local↗
PubMedDate not supplied

Constituents of Erythroxylon coca. II. Gas-chromatographic analysis of cocaine and other alkaloids in coca leaves.

A gas-chromatographic procedure is outlined for the analysis of cocaine and cis- and trans-cinnamoylcocaines in coca leaves. The procedure was applied to the determination of these alkaloids in coca leaves collected from three different locations in Peru. The extraction of alkaloids from plant material was accomplished following the procedure we previously outlined. Recovery of cinnamoylcocaines was quantitative and the average coefficient of variation was 6.8%. Using androst-4-ene-3,17-dione as the internal standard, the correlation coefficient (r2) as determined from the calibration curve of trans-cinnamoylcocaine was 0.99 and the response factor 0.72. Observable differences in relative proportions of cis and trans isomers of cinnamoylcocaine were found among samples from different locations. In addition, the relative proportions of the total cinnamoylcocaine concentration to cocaine varied with sample origin. We have also examined coca extracts using a nitrogen detector and by gas chromatography--mass spectrometry. The nature and identity of other nitrogenous peaks in the chromatograms are also discussed.

Alkaloids↗
PubMed1981

Comparative stimulus properties of two fractions of the coca leaf (E. coca).

Male and female Wistar rats were trained to discriminate 5.0 mg/kg cocaine from 2.0 ml/kg saline using a two-bar food reinforcement (FR 30) drug discrimination paradigm. Once discrimination behavior had stabilized the subjects were tested (in extinction) with several doses of two different fractions of the coca leaf and four doses of cocaine HCl (1.0, 2.5, 7.5, 10 mg/kg). The fractions were prepared by extracting powdered coca leaves with 95% ethanol and then partitioning the residue between chloroform and water. Two doses of the water fractions (480, 960 mg/kg) and five doses of the chloroform fraction (7.5, 15, 30, 60 120 mg/kg) were tested. The water fractions was devoid of cocaine while the five doses of the chloroform fraction contained cocaine equivalent to 0.4, 0.83, 1.65, 3.3 and 6.6 mg/kg, respectively, as determined by gas chromatographic analysis. The 2.5, 7.5, and 10.0 mg/kg cocaine doses generalized to cocaine. The 1.0 mg/kg dose of cocaine generalized to saline. The water fraction at 480 mg/kg generalized to saline; however following pretreatment with the 960 mg/kg dose of this fraction, the animals failed to respond. The two largest doses of the chloroform fraction (60 and 120 mg/kg) generalized to cocaine while the other three doses did not. The 7.5 mg/kg generalized to saline; the 15 and 30 mg/kg doses engendered an intermediate level of responding on both the cocaine and saline lever.

Animals↗
PubMedDate not supplied

Systematic anatomy of Erythroxylum P. Browne: practical and evolutionary implications for the cultivated cocas.

Preliminary study of the pantropical Erythroxylaceae indicates that anatomical features can provide valuable insight into the generic, infra-generic and specific affinities of unidentified specimens. Combinations of qualitative and quantitative anatomical data are most reliable when considered in conjunction with relevant ecological and plant morphological data. Extreme caution is advised in such taxonomic applications due to the intergrading patterns of anatomical variation exhibited within the family. Careful consideration must be given to the potential influence on anatomy of factors such as plant age, habit, leaf morphology and environmental conditions. Although a few species of Erythroxylum are identifiable solely on the basis of unique wood anatomical features, the majority of species can be identified only through a combination of morphological and vegetative anatomical features. Closely related species and species of similar habitats are often very similar in their wood and leaf structure. Anatomical differences are more subtle among the cultivated cocas and their closest neotropical relatives than among most taxa of Erythroxylaceae. A typological concept of foliar venation patterns among the cultivated cocas permits the varietal identification of isolated coca leaves. Several neotropical relatives of the cultivated cocas represent potential adulterants in commercial samples of coca leaf as a result of their striking similarity to genuine coca in leaf form, venation and anatomy. Due to the broad and overlapping range of leaf structural variation exhibited among the cultivated cocas and their nearest relatives, identifications of isolated leaves or leaf fragments are ill-advised in the absence of relevant ecological data. Patterns of wood and leaf anatomical variation within the Erythroxylaceae are most readily explicable as the result of evolutionary diversification in plant habit, leaf size, form and relative duration. Significant correlations among wood and leaf structure reveal various "adaptive strategies" among species of Erythroxylaceae. Redundant patterns of structural evolution, evident among the different species and genera of Erythroxylaceae, help to elucidate the probable evolutionary origins of the cultivated cocas. Comparative anatomical data support the hypothesis that Bolivian coca (E. coca) represents the most primitive of the cultivated cocas. The Colombian and Trujillo varieties of coca (E. novogranatense) appear to have been derived from a Bolivian-like ancestral coca as a result of long-term cultivation, geographic isolation and human selection for increased flavor, palatability and drought resistance.

Coca↗
PubMedDate not supplied

Coca-paste smoking in some Latin American countries: a severe and unabated form of addiction.

Coca paste is an intermediary product in the chemical extraction of cocaine from coca leaves. Abusers smoke coca paste in a dried form, which contains from 40 to 91 per cent cocaine. Over the past 10 years, this pattern of drug abuse has attained epidemic proportions in some Latin American countries, particularly in Bolivia, Colombia and Peru. Addiction to coca paste develops in a few months and has serious health, social and economic consequences. The problem is particularly acute in Latin American countries because of the high doses of coca paste involved. The smoking of coca paste causes four distinct successive phases of mental disorder: euphoria, dysphoria, hallucinosis and paranoid psychosis. It can produce severe intoxication, prolonged or relapsing psychosis and, in some cases, death. Cocaine has been found in the blood of coca-leaf chewers, coca-paste smokers and users of cocaine hydrochloride. Excessive coca-paste smoking is often resistant to therapeutic interventions and there is a high rate of relapse after treatment and rehabilitation.

Adolescent↗
PubMedDate not supplied

Study of the concentration of the herbicide (2,4-dichlorophenoxy)-acetic acid in coca leaves and paste obtained from plants treated with this herbicide.

The herbicide (2,4-dichlorophenoxy)-acetic acid (2,4-D) is considered to be the most cost-effective for eradicating illicit coca plants. Since coca leaves are chewed by the natives of coca producing areas, and, since coca paste and cocaine are widely abused, a study was undertaken to determine whether 2,4-D is translocated into the leaves and transferred to coca paste when coca plants are treated with this herbicide. The study concluded that basal treatment of coca plants with 2,4-D ester resulted in translocation of 2,4-D into the leaves, and this herbicide was detected in high concentrations one week after treatment. Coca paste prepared from leaves obtained from basally treated plants did not contain 2,4-D. Foliage spraying resulted in extremely high concentrations of 2,4-D in the leaves, with significantly high concentrations of the herbicide found one week after spraying. Trace amounts of 2,4-D were detected in coca paste prepared from plants sprayed by the foliage method.

2,4,5-Trichlorophenoxyacetic Acid↗
PubMed1986

Effect of Erythroxylum coca, cocaine and ecgonine methyl ester as dietary supplements on energy metabolism in the rat.

The effects of dietary supplements of cocaine, ecgonine methyl ester, a coca leaf extract and powdered coca leaves on body weight and overall body metabolism were studied in the rat. Respiratory quotient was measured to assess the relative utilization of fats, carbohydrates and protein. The effect of cocaine and ecgonine methyl ester on protein metabolism was also assessed in terms of changes in the relative state of nitrogen balance. Rats maintained on a low protein/high carbohydrate diet containing cocaine (1 mg/g) exhibited normal body weight gain on normal food intake. Rats on the same diet with 2 mg/g cocaine as the hydrochloride or as coca dextrin lost weight, which was apparently related to diminished food intake. In contrast, rats received the same high level of cocaine as coca leaf powder in the same diet had minimal weight gain in spite of a high food intake. In contrast, rats receiving the same high level of cocaine as ly, rats receiving the same high level of cocaine (2 mg/g) in a high protein diet had normal food intake and body weight gain. An adequate protein diet appears to compensate for whatever inhibiting effect is imposed on the body by the high levels of cocaine. Ecgonine methyl ester appears to have no significant effect on food intake or body weight. Rats fed the low protein/high carbohydrate diet containing either the low (1 mg/g) or the high (2 mg/g) cocaine level exhibited significantly depressed respiratory quotients (near 0.75) suggesting increased fat utilization. The magnitude of the reduction appeared to be dose-related. Yet, the respiratory quotient of the rats receiving the high level of cocaine in a high protein diet remained at normal control values. Also, in a separate nitrogen balance-type of experiment, rats receiving the low level of cocaine (1 mg/g low protein/high carbohydrate diet) exhibited a normal ability to accumulate body nitrogen, presumably protein. These results support the idea that under conditions of protein deprivation cocaine helps spare amino acids through the preferential utilization of fat. Coca leaf in the low protein/high carbohydrate diet equivalent to 2 mg/g cocaine had a small but significant positive effect on respiratory quotient possibly due to the availability of utilizable nitrogenous components in the coca leaf. The respiratory quotient effects were less obvious with an extract of coca leaf incorporated in the diet as coca-dextrin, but showed the same trend.(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMed1989

Coca-leaf production in the countries of the Andean subregion.

The estimated areas under coca-bush cultivation in 1988 are expected to total 44,300 hectares in Bolivia, 25,000 hectares in Colombia, 400 hectares in Ecuador and 114,400 hectares in Peru. The estimated projections for 1989 indicate that coca-leaf production may amount to 68,200 tonnes in Bolivia, 20,000 tonnes in Colombia, 300 tonnes in Ecuador and 120,100 tonnes in Peru. Of all the Andean countries, Venezuela is the only one that has no coca-leaf production problem. According to estimates for the period from 1985 to 1989, coca-leaf production will increase by 43.3 per cent in Bolivia, by 13.6 per cent in Colombia and by 26.2 per cent in Peru. Coca-leaf production in Ecuador has consistently followed a downward trend. According to estimates, since 1985 coca-leaf production in Peru has accounted for more than one half of the total amount produced in the Andean subregion, while production in Colombia, though it has increased in the same period, has accounted for a relatively small share. In 1987, estimated coca-leaf production in Bolivia amounted to 30.2 per cent of the total amount produced in the subregion.

Bolivia↗
PubMed1992

Cocaine problems in the coca-growing countries of South America.

The problems of cocaine present a rather particular profile in the Central Andes region from which this drug originates. On the one hand there is a relatively harmless pattern of use (coca leaf chewing) in the countries concerned which minimizes the drug's most hazardous properties. On the other hand the region suffers from some of the most severe cocaine-related problems to be observed anywhere: (a) easy access to the newer, highly toxic preparations of the drug (such as coca paste) and a rapid growth in the number of new users; (b) the abandonment of certain traditional and essential agricultural activities in favour of the more profitable coca leaf production; (c) the severe ecological damage being caused in the coca growing areas; and (d) the establishment of a powerful coca trade economy which is subverting the very fabric of society and is creating corruption, lawless violence and political anarchy.

Coca↗
PubMed1982

Comparative lethality of coca and cocaine.

The 24 hour lethal effects of cocaine were compared to those of a crude ethanol extract of the coca leaf (Erthroxylon coca) in male, Swiss mice. Various doses of cocaine HCl and coca leaf extracts suspended in a Tween 60, Arlacel 83, and distilled water vehicle were injected IP into groups of 10 mice. The LD50 for cocaine was 95.1 mg/kg. The LD50 for the coca extract was 3450 mg/kg. The LD50 of the extract based on its cocaine content was 31.4 mg/kg. The results clearly indicate that the coca leaf contains constituents other than cocaine that can contribute to a toxic effect of the plant.

Animals↗
PubMed1983

Anorexic activity of cocaine and coca extract in naive and cocaine tolerant rats.

Dose response curves for reducing limited access food consumption were determined for cocaine HCl IP, cocaine HCl PO, and whole Erythroxylum coca extract PO. The ED50's for cocaine HCl in drug naive rats were 19.6 mg/kg (IP) and 34.6 mg/kg (PO). When the dose of E. coca extract was expressed in terms of cocaine HCl content, the ED50 was 52.6 mg/kg (PO). When dose response curves were determined in rats that had received cocaine (45 mg/kg, PO) for 30 days, a shift to the right in the cocaine HCl curve (an ED50 of 98.4 mg/kg PO) indicated tolerance. However, the shift to the right was less for E. coca extract than for cocaine HCl. Although the anorexic activity of E. coca extract was less than that of an equivalent amount of cocaine in naive rats it was often more than that of equivalent doses of cocaine HCl in tolerant rats. Interaction with other constituents of E. coca extract appears to alter the potency of the cocaine content of the extract in different directions in naive and tolerant rats.

Animals↗
PubMedDate not supplied

Amazonian coca.

A general overview of various aspects of Amazonian coca (Erythroxylum coca var. ipadu) is presented. This plant is considered a distinct variety of coca which has been developed as a cultivated plant in the upper Amazon basin. It differs from typical Andean coca in morphological, physiological and chemical features as well as in the method of preparation and use by Amazonian tribes. The main topics here discussed are the history, distribution, botany, chemistry, origin, methods of preparation and use, and the effects of Amazonian coca.

Chemistry↗
PubMedDate not supplied

Analysis of alkaloids in leaves of cultivated Erythroxylum and characterization of alkaline substances used during coca chewing.

Several solvents were tested for the extraction of the alkaloids in Erythroxylum coca. The resulting crude extracts were analyzed by gas chromatography--mass spectrometry. Ethanol extraction was found to be the only quantitative method presenting no artifacts. It was established that cocaine and cis- and trans-cinnamoylcocaine were the endogenous alkaloids in E. coca leaves. From the several breakdown compounds arising during long-term extraction with H2SO4 or CHCl3, ecgonine methyl ester was the only alkaloid fully identified; ecgonine methyl ester was tentatively identified on the basis of its mass spectrum fragmentation pattern. Quantification by mass fragmentography of the three endogenous compounds was performed using a stable-isotope dilution technique on individual leaves of single branches of E. coca, E. novogranatense and E. novogranatense var. truxillense. The relative amounts of these alkaloids changed with leaf age as well as between species and varieties. The variation in alkaloid levels between individual leaves was too great to allow the use of the ratio between cocaine and the cinnamoylcocaine levels as a taxonomic marker. The initial pH value of 17 different alkaline substances traditionally used during coca leaf chewing was measured after dissolution in H2O; values ranged between 10.1 and 12.8. Buffer capacity was determined by titration with HCl. Three types of curve shapes were obtained which could correspond to NaOH, Na2CO3 and NaHCO3 titration curves. One sample of alkaline material had no buffer capacity at all. The recovery and breakdown of the cocaine contained in E. coca leaf power was monitored for one hour at various pHs at 37 degrees C. The levels of cocaine and benzoylecgonine did not change by more than 17% at any of the pHs tested (6.0, 9.0 and 11.5). It was concluded that the alkaline substances are mainly responsible for the transformation of the alkaloids to free bases and not for a major hydrolysis of cocaine.

Alkalies↗
PubMed1978

Coca leaf as a therapeutic agent.

South American Indians have used coca leaf as a remedy for thousands of years. Coca might be useful as a treatment for gastrointestinal ailments and motion sickness, as a fast-acting antidepressant medication, as a substitute stimulant for coffee in certain cases, and as an adjunct in programs of weight reduction and physical fitness. In leaf form, coca does not produce toxicity or dependence. Its effects are distinct from those of cocaine, which is but one of a number of active compounds in the leaf. Coca can be administered as a chewing gum containing a whole extract of the leaf, including alkaloids, natural flavors, and several nutrients. Legal mechanisms exist for importing, distributing, and dispensing coca, and experimentation with it by interested physicians would be valuable.

Chewing Gum↗
PubMed1979

Deleterious effect of short-term exposure to Coca-Cola on rats.

Semiacute toxicity of cola fluid, Coca-Cola, conducting for approximately a month in rats, was studied. A trend of cariogenicity of Coca-Cola was strongly indicated. When the fluid was given ad libitum, decarbonized Coca-Cola and carbohydrate solution, consisted 8% of glucose and 3.5% of sugar and then adjusted pH to 2.4 with oxalic acid, were consumed 2 to 3 times greater than the control (water). A hyperuresis was observed as the result of great consumption of liquid, but no liver nor kidney degeneration was observed by histopathological examination. The diet consumption of the groups of Coca-Cola and carbohydrate solution was approximately a half of the control, water. However, when a complete diet was given, no physiological difference in time was observed, except in diarrhea and depression of hair gloss in Coca-Cola group.

Animals↗
PubMed1991

[Archeological and artistic sources of coca consumption in pre-hispanic America].

The use of coca in pre-hispanic America is confirmed by archeological and artistic sources, such as sculptures, ceramics, fabrics and pictures. The historical and geographical diffusion of these pieces of evidence seems to point to the fact that coca has been a strong element in the union of the different cultures of this continent. Those pieces of evidence were mostly found in a religious bond and indicate towards the divine character awarded to this plant; this divinity will, later on, be confirmed by the Inca's, who will raise it to a god. Owing to its many properties such as its use in the course of initiation rituals and of important celebrations, and seeing its fundamental importance in economy, coca was allowed a manifold value. The investigation of as well the technical (materials, workmanship,...) as the esthetic factors (form, style,...) of the works of art, combined with the study of the cultural background, shows that the use of coca seems to have been a privilege of the upper social classes. It is just from the Inca period (1450-1530) that the whole people could reach to coca, so that its stimulating properties outweighed the symbolic meaning.

Art↗
PubMed1991

[Consumption of coca in history].

The first consumers of coca were the Aymara Indians of the Andes mountains. At the beginning, the consumption of coca-leaves was reserved to princes and priests during religious ceremonies. This habit was later extended to the common people. The Spanish invaders judged that this practice was the expression of a "pagan cult" and therefore banned the cultivation of the coca-plant. In the XIXth century, coca and cocaine were used once more in Europe. Freud made self-experiments with cocaine, but he was promptly discouraged by reading about the cases of cocaine mania reported in the American scientific literature. In 1870 Angelo Mariani brought on the market a kind of wine, based on coca extract, which enjoyed a great success in Europe. Hereafter Pemberton produced, in the USA, a competitive drink under the name "Vin français cola", wherein he replaced the wine by a cola extract and where from he finally vanished cocaine. The medical use of cocaine for the treatment of hayfever and asthma (Dr. Tücker's elixir) had in between officially been agreed by the famous scientific societies in America. This treatment was finally abandoned.

Ceremonial Behavior↗