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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↗

PubMed2005

Molecular cloning and functional characterization of the dopamine transporter from Eloria noyesi, a caterpillar pest of cocaine-rich coca plants.

Cocaine is produced by coca plants as a chemical defense to deter feeding by insects. It has been shown that cocaine sprayed on tomato leaves reduces insect feeding, causes abnormal behaviors at low doses and kills feeding insects at doses equivalent to that in coca leaves [Nathanson, J.A., Hunnicutt, E.J., Kantham, L., Scavone, C., 1993. Cocaine as a naturally occurring insecticide. Proc. Natl. Acad. Sci. U. S. A. 90, 9645-9648.]. Most insects avoid coca leaves except the larvae of Eloria noyesi, a caterpillar pest of coca plants, which feeds preferentially on coca leaves. In the current study, we cloned and characterized the dopamine transporters (DATs) from caterpillars of E. noyesi (enDAT) and the silkworm, Bombyx mori (B. mori, bmDAT). The two insect DATs shared 88% amino acid sequence homology and functional similarity. Although enDAT and bmDAT showed the highest affinity for dopamine among endogenous amines, they were more sensitive to mammalian NET-selective inhibitors than to mammalian DAT-selective inhibitors. Despite a high cocaine content in the food source for E. noyesi, cocaine sensitivity of enDAT was similar to that of bmDAT, suggesting that mechanisms other than DAT insensitivity to cocaine, such as cocaine sequestration, might be responsible for cocaine resistance in this species. Given the significant differences in pharmacological profile from mammalian DATs, invertebrate DATs provide excellent tools for identifying regions and residues in the transporters that contribute to high-affinity binding of psychostimulants and antidepressants.

Amino Acid Sequence↗

PubMedDate not supplied

Attitudes and values of Peruvian coca growers.

This study uses semi-structured interviews to examine the attitudes and values of Peruvian coca growers toward coca leaf and cocaine basic paste (CBP) consumption and its distribution. The subjects of the study were 186 coca growers from Peruvian jungle valleys who are involved in illegal commercialization of coca leaf and cocaine paste production. Data collected in 1994 reveal that growers consider coca leaf to be a most profitable product and a unique opportunity to improve their quality of life. Although growers acknowledge that a problem exists among local users, they do not assume any responsibility for CBP consumption and dissemination in rural areas. This leads to the conclusion that awareness of a CBP consumption problem is not enough for growers to stop drug production; they need consistent training in social values, as well as support in legal and economic alternatives.

Adult↗

PubMed2006

Coca tea consumption causes positive urine cocaine assay.

BACKGROUND: Coca tea, derived from the same plant that is used to synthesize cocaine, is commonly consumed in South America and easily obtained in the United States. OBJECTIVES: To determine whether consumption of coca tea would result in a positive urine toxicology screen for cocaine metabolites. METHODS: Five healthy adult volunteers consumed coca tea and underwent serial quantitative urine testing for cocaine metabolites by fluorescence polarization immunoassay. The cutoff for a positive assay was chosen at 300 ng/ml, the National Institute on Drug Abuse standard. RESULTS: Each participant's urine cocaine assay was positive (level exceeding 300 ng/ml) by 2 h after ingestion. Three out of five participants' samples remained positive at 36 h. Mean urine benzoylecgonine concentrations in all postconsumption samples was 1777 ng/ml (95% confidence interval: 1060-2495). CONCLUSIONS: Coca tea ingestion resulted in a positive urine assay for cocaine metabolite. Healthcare professionals should consider a history of coca tea ingestion when interpreting urine toxicology results.

Adult↗

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↗

PubMed1993

Oesophageal and gastric potential difference and pH in healthy volunteers following intake of coca-cola, red wine, and alcohol.

Alcohol causes gastroesophageal reflux and mucosal damage in the oesophagus and the stomach. The transmucosal electrical potential difference gives information on gastric mucosal integrity and function, while the validity of oesophageal measurements have been discussed. Baseline oesophageal potential difference measurements were performed three times with an interval of at least one week. We found oesophageal potential difference measurements reliable with an acceptable reproducibility. Oesophageal and gastric potential difference and pH were measured by use of a new microelectrode principle in 10 healthy volunteers following intake of coca-cola, wine and alcohol. Oesophageal and gastric potential difference decreased after intake of 250 ml coca-cola, 250 ml 11 vol% red wine and 60 ml 43 vol% whisky. Gastric potential difference decreased after intake of 250 ml ethanol 11 vol% and 60 ml ethanol 43 vol%. Intake of red wine and whisky resulted in a significant greater gastric potential difference decrease compared to similar concentrations and volumes of ethanol. The time until the potential difference had regained baseline level was longer after intake of red wine compared to coca-cola, whisky and ethanol. Oesophageal pH decreased after intake of coca-cola and red wine, but was unchanged after whisky. Gastric pH was unchanged after intake of all the drinks. In conclusion, the gastric potential difference reduction was not correlated to alcohol concentration. Red wine seems to affect the gastric potential difference more than coca-cola, whisky and ethanol. The observed changes in oesophageal and gastric potential difference might be due to changes in Cl- secretion and/or due to a damaging effect of the additives of the beverages.

Adult↗

PubMed2006

Results of long-term carcinogenicity bioassays on Coca-Cola administered to Sprague-Dawley rats.

Coca-Cola was invented in May 1886 in Atlanta, Georgia by a pharmacist who, by accident or design, mixed carbonated water with the syrup of sugar, phosphoric acid, caffeine, and other natural flavors to create what is known as "the world's favorite soft drink." Coca-Cola is currently sold in more than 200 countries and in early 2000, the company sold its 10 billionth unit case of Coca-Cola branded products. Given the worldwide consumption of Coca-Cola, a project of experimental bioassays to study its long-term effects when administered as substitute for drinking water on male and female Sprague-Dawley rats was planned and executed. The objective of the project was to study whether and how long-term consumption of Coca-Cola affects the basic tumorigram of test animals. The bioassays were performed on rats beginning at different ages, namely: (a) on males and females exposed since embryonic life or from 7 weeks of age; and (b) on males and females exposed from 30, 39, or 55 weeks of age. Overall, the project included 1999 rats. During the biophase, data were collected on fluid and feed consumption, body weight, and survival. Animals were kept under observation until spontaneous death and underwent complete necropsy. The results indicate: (a) an increase in body weight in all treated animals; (b) a statistically significant increase of the incidence in females, both breeders and offspring, bearing malignant mammary tumors; (c) a statistically significant increase in the incidence of exocrine ademonas of the pancreas in both male and female breeders and offspring; and (d) an increased incidence, albeit not statistically significant, of pancreatic islet cell carcinomas in females, a malignant tumor which occurs very rarely in our historical controls. On the basis of the results of this study, excessive consumption of regular soft-drinks should be generally discouraged, in particular for children and adolescents.

Animals↗

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↗

PubMed1989

Epidemiology of coca and alcohol use among high-altitude miners in Argentina.

A medical survey of 107 high-altitude miners was conducted in Argentina in 1976-1977. Daily chewing of coca leaves was reported by 70 (65%) respondents. Another 15 (14%) used coca occasionally. Weekly alcohol drinking was reported by 36 (34%) respondents, and 14 (14%) drank occasionally. Thirty-five of the weekly drinkers were also daily users of coca. Habitual users did not differ from other workers in mean age or total number of years worked. Daily use of coca was significantly higher among miners with a heavy work load as compared with those having a moderate-to-light work load (unadjusted odds ratio [OR] 4.24); it was also higher among those who had worked only underground rather than always or ever aboveground (OR 7.25), among those working as drillers or cart pushers as opposed to other tasks (OR 6.56), and among Mestizos and Indians compared with whites (OR 3.33). Weekly alcohol use was significantly higher among miners with a heavy work load (OR 6.49), those always working underground (OR 5.57), and those working as drillers or cart pushers (OR 3.67). Adjusting for possible confounding effects of these parameters on each other, the significant associations with habituation were clearly work site, work load, and task.

Alcoholism↗

PubMedDate not supplied

Coca and cocaine as medicines: an historical review.

Coca has been used in folk medicine in South America for thousands of years both as a general stimulant and for more specific medical purposes. It remains one of the most commonly used medicines in some areas of Bolivia and Peru. The medical use of coca and cocaine in the industrial world has a more dramatic and varied history. Coca extract and cocaine were introduced as pancreas for a wide variety of complaints in the late 19th century. Cocaine was the first effective local anesthetic; prescription drugs, patent medicine, and soda drinks containing it were also popular. When its dangers became apparent and substitutes became available, its medical use went into decline, especially when, in the 1930s, amphetamine began to replace it for some purposes. Today its only generally accepted medical use is as a topical anesthetic in certain kinds of minor surgery and other clinical procedures. There are, however, some recent and so far uncertain signs of reviving interest in cocaine and even coca itself for other medical purposes, in research as well as in diagnosis and treatment.

Anesthetics, Local↗

PubMedDate not supplied

The therapeutic value of coca in contemporary medicine.

Coca appears to be a useful treatment for various gastrointestinal ailments, motion sickness, and laryngeal fatigue. It can be an adjunct in programs of weight reduction and physical fitness and may be a fast-acting antidepressant. It is of value in treating dependence on stronger stimulants. Coca regulates carbohydrate metabolism in a unique way and may provide a new therapeutic approach to hypoglycemia and diabetes mellitus. With low-dose, chronic administration it appears to normalize body functions. In leaf form coca does not produce toxicity or dependence. Coca can be administered as a chewing gum or lozenge containing a whole extract of the leaf, including alkaloids, natural flavors, and nutrients.

Anesthetics, Local↗

PubMed1984

Biological activity of the alkaloids of Erythroxylum coca and Erythroxylum novogranatense.

The cultivated Erythroxylum varieties E. coca var. coca, E. coca var. ipadu, E. novogranatense var. novogranatense and E. novogranatense var. truxillense contain 18 alkaloids, identified so far, belonging to the tropanes, pyrrolidines and pyridines, with cocaine as the main alkaloid. The biological activity of the following alkaloids has been reported in the literature: cocaine, cinnamoylcocaine, benzoylecgonine, methylecgonine, pseudotropine, benzoyltropine, tropacocaine, alpha- and beta-truxilline, hygrine, cuscohygrine and nicotine. The biological activity of cocaine and nicotine is not reviewed here, because it is discussed elsewhere in the literature. Hardly anything is known about the biological activity of the other alkaloids present in the four varieties mentioned. The biosynthesis of the coca alkaloids has been outlined.

Alkaloids↗

PubMed2000

Coca leaf chewing as therapy for cocaine maintenance.

Major ethnic groups in Bolivia (Aymaras and Quechuas) have chewed the coca leaf for generations upon generations without health problems. The effects of coca leaf chewing produce a level of social and economic adaptation that is beyond what is normally possible. This was a major factor during the Spanish colonization of Bolivia, when forced native labor was used extensively. The cocaine base, or "pasta", may be seen as a type of South American crack. Its obligatory method of administration is smoking. A primary condition of the "pasta" smoker is compulsive drug-search behavior and addiction to cocaine base destroys emotional and mental balance. Socio-economic maladjustment is the norm amongst "pasta" addicts. Since 1984 I have recommended the chewing of the coca leaf, between 100 to 200 grams of coca leaf per week for the treatment of cocaine dependence. Since this treatment was dispensed on an ad hoc basis, it was not possible to measure the relapses. However, an assessment was conducted on the basis of mental condition and level of social and economic adaptation before and after treatment. The patent's level of social acceptance, before treatment, only reached 60% at most, and after treatment, 26% improved their level of adaptation. Four patients among 50 reached an adaptation level of 100%. Upon final assessment, the level of social adaptation prior to treatment was only 28%, after treatment as many as 48.8% of the patients were socially adapted.

Animals↗

PubMedDate not supplied

Use of coca leaf in southern Peru: adaptation or addiction.

Use of coca leaves among the Quechua Indians of the Peruvian altiplano is considered from the biological and social perspectives. Biologically, coca use seems to reduce the loss of body heat in the cold and to enhance working ability to a small degree. It may also have nutritional value. Socially, coca is well integrated into the economic and social systems, providing functions in both spheres. The equation of coca use with cocaine addiction is also considered and a simple equivalence is rejected.

Adaptation, Physiological↗