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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↗

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↗

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↗

Coca chewing in prehistoric coastal Peru: dental evidence.

In this study, we describe the dental health of four prehistoric human populations from the southern coast of Peru, an area in which independent archaeological evidence suggests that the practice of coca-leaf chewing was relatively common. A repeated pattern of cervical-root caries accompanying root exposure was found on the buccal surfaces of the posterior dentition, coinciding with the typical placement of coca quids during mastication. To further examine the association between caries patterning and coca chewing, caries site characteristics of molar teeth were utilized as indicators for estimating the likelihood of coca chewing for adults within each of the study samples. Likelihood estimates were then compared with results of a test for coca use derived from hair samples from the same individuals. The hair and dental studies exhibited an 85.7% agreement. Thus, we have demonstrated the validity of a hard-tissue technique for identifying the presence of habitual coca-leaf chewing in ancient human remains, which is useful in archaeological contexts where hair is not preserved. These data can be used to explore the distribution of coca chewing in prehistoric times. Simultaneously, we document the dental health associated with this traditional Andean cultural practice.

Coca↗

Brief communication: effect of coca-leaf chewing on salivary progesterone assays.

Although there is evidence for reduced fertility in Andean and Himalayan populations at higher altitudes, factors other than hypoxia may be primarily responsible. A valuable approach in the investigation of these fertility determinants is the use of salivary steroid assays. However, coca-leaf chewing--a ubiquitous practice among high altitude Andean populations--has negative consequences for the accurate measurement of ovarian steroids. This report evaluates the effects of coca-leaf chewing on assays of salivary progesterone. Study participants include naive and habitual users of coca leaf from La Paz and El Alto, Bolivia. Approximately 300 saliva samples were collected immediately before, during, and after coca-leaf chewing. The series includes samples with and without the alkaloid enhancer typically used by coca-leaf chewers. Coca chewing produces false salivary progesterone values that mimic luteal phase values. On the basis of this study, an appropriate protocol is developed for the collection of salivary samples in coca-leaf chewing populations. These results verify the feasibility of salivary assays, even for very difficult field conditions, and highlight the necessity of establishing suitable collection procedures before full field implementation of saliva sampling.

Adult↗

Effects of coca chewing on metabolic and hormonal changes during graded incremental exercise to maximum.

We examined the effects of 1 h of coca chewing on metabolic and hormonal responses during incremental exercise to exhaustion in traditional coca chewers (C; n = 8), and the results were compared with a group of nonchewers (n = 13). For 1 h, C chewed approximately 12 g of coca leaves that resulted in the apparition of cocaine in blood that reached 72 +/- 9 ng/ml. In resting conditions, even though sympathoadrenergic activity (as assessed by norepinephrine and epinephrine plasma levels) was similar in both groups, C displayed a higher level of plasma free fatty acids. Oxygen uptake measured at exhaustion and delta work efficiency during exercise were similar in both groups. During the incremental exercise, C displayed a significantly lower arterial oxygen saturation that cannot be explained by a reduced ventilatory response after coca chewing. In fact, even at maximal exercise, both ventilatory output and ventilatory equivalent were higher in C compared with nonchewers. It is concluded that the beneficial effects of coca chewing on exercise tolerance reported frequently by traditional coca users is not related to either an improved maximal exercise capacity or an increased work efficiency. However, during incremental exercise, coca chewing appeared to result in an increased free fatty acid availability that could be beneficial for prolonged submaximal exercise.

Adult↗

Effects of coca chewing on hormonal and metabolic responses during prolonged submaximal exercise.

The effects of coca chewing on prolonged submaximal exercise responses were investigated in chronic coca chewers and compared with a group of nonchewers. At rest, coca chewing during a 1-h period was followed by a significant increase in blood glucose, free fatty acid, and norepinephrine concentrations and a significant reduction in insulin plasma level. During prolonged (1-h) submaximal (65-70% peak O2 uptake) exercise, chewers displayed a significantly greater adrenergic activation (as evidenced by a higher level of plasma epinephrine) and an increased use of fat (as evidenced by a lower respiratory exchange ratio). The gradual increase in oxygen uptake (O2 drift) commonly observed during prolonged exercise was blunted in coca chewers. This blunting in O2 drift is not related to coca-induced changes in ventilatory or lactate responses to exercise but could possible be related to an enhanced glucose utilization by chewers during the late phase of exercise. The present results provide experimental evidence of the physiological effects of coca chewing that could explain the better ability of coca users to sustain strenuous work for an extended period of time.

Adolescent↗

Storage effects on genomic DNA in rolled and mature coca leaves.

Rolled and mature leaf tissue was harvested from Erythroxylum coca var. coca Lam. (coca) to determine a method for storage that would maintain DNA with high quality and content up to 50 days. Harvesting coca leaf tissue under Andean field conditions often requires storage from 3 to 10 days before extraction where tissue integrity is lost. All samples of rolled and mature coca leaf tissue were harvested and separately stored fresh in RNAlater for 50 days at 4 degrees, -20 degrees, and 23 degrees C, while similar samples were air-dried for 72 h at 23 degrees C or oven-dried for 72 h at 40 degrees C after storage, before extraction. Triplicate samples of each tissue type were extracted for DNA at 10-day intervals and showed that DNA integrity and content were preserved in leaf tissue stored at 4 degrees and -20 degrees C for 50 days. Rolled and mature leaf tissue stored at 4 degrees, -20 degrees, and 23 degrees C showed insignificant degradation of DNA after 10 days, and by day 50, only leaf tissue stored at 4 degrees and -20 degrees C had not significantly degraded. All air- and oven-dried leaf tissue extracts showed degradation upon drying (day 0) and continuous degradation up to day 50, despite storage conditions. Amplified fragment length polymorphism analysis of DNA from rolled and mature leaf tissue of coca stored at 4 degrees and -20 degrees C for 0, 10, and 50 days showed that DNA integrity and content were preserved. We recommend that freshly harvested rolled or mature coca leaf tissue be stored at 4 degrees, -20 degrees, and 23 degrees C for 10 days after harvest, and if a longer storage is required, then store at 4 degrees or -20 degrees C.

Coca↗

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↗

[Effects of coca chewing on the glucose tolerance test].

The effects of coca chewing on the glucose tolerance test were measured. The subjects were 14 habitual coca chewers and 14 non-chewers. All were of Aymara ancestry and came from a rural community from the "Altiplano" close to the city of La Paz. The coca users chewed coca leaves during 3 1/2 hours of the test. The non-chewers showed a significant hypoglycemia at 120 minutes of the test. This effect was not observed in the coca chewers. The hormonal counter-regulation response to hypoglycemia worked perfectly in non-chewers, since glucose levels reached normal values at 180 minutes of the test. These results suggest that coca chewers, at high altitude do not present hypoglycemia, due to an antagonic action of coca metabolites on insulin; allowing a greater availability of glucose in the organism. This would have a positive effect on metabolism in an environment of hypobaric hypoxia, known to lead to situations of hypoglycemia.

Adult↗

Detection and determination of pseudococaine in coca leaves and illicit cocaine samples.

Methodology is presented for the isolation, identification and determination of pseudococaine in coca leaves and illicit cocaine. Coca leaves, crude cocaine base (coca paste), refined cocaine base and refined cocaine hydrochloride, all derived from the same geographic location in Bolivia, were examined. Pseudococaine and other coca alkaloids were isolated from leaf samples using toluene extraction followed by acid/Celite trap and ion-pair column chromatography, and from crude and refined cocaine samples by acid/Celite column ion-pairing chromatography. Mass spectral analysis of coca leaf isolates confirmed the presence of pseudococaine. Pseudococaine was quantified by capillary gas chromatography with flame ionization detection at levels of 0.0001-0.035% (relative to cocaine) in refined illicit cocaine and coca leaves.

Chromatography, Gas↗

Hardness of enamel exposed to Coca-Cola and artificial saliva.

The purpose of this study was to determine the rate of change in indentation hardness of enamel in permanent teeth exposed to Coca-Cola. In a further experiment, the ability of a commercially available artificial saliva to remineralize enamel treated with Coca-Cola was tested. Ten enamel specimens were randomly chosen to be treated with Coca-Cola (experimental groups) and seven with water (control group). The fluids were applied for 1, 2, 3 h and overnight (15 h), washed off with a few drops of water and the moist enamel indentation hardness tested after each interval. With Coca-Cola treatment, the mean enamel hardness was 92.6% (s.d. = 7.9) of the original baseline hardness after 1 h, 93.25% (s.d. = 10.15) after 2 h, 85.7% (s.d. = 12.03) after 3 h and 80.3% after 15 h. The mean indentation hardness of control specimens treated with water was 108.7% (s.d. = 16.09) of the original hardness after 1 h, 99.09% (s.d. = 18.98) after 2 h, 98.97% (s.d. =11.24) after 3 h and 98.42% (s.d. = 22.78) after 15 h. In a separate experiment, the hardness of 9 enamel specimens was tested, as previously described, before and after treatment with Coca-Cola overnight and again after application of artificial saliva for 3 min. Coca-Cola reduced the mean indentation hardness of enamel in the teeth, but the hardness was partially restored with artificial saliva (Salivart) and increased by 18% from the demineralized enamel hardness.

Carbonated Beverages↗

Effect of an acidic beverage (Coca-Cola) on the pharmacokinetics of carbamazepine in healthy volunteers.

The effect of an acidic beverage (Coca-Cola) on the pharmacokinetics of a single dose of carbamazepine was studied. In a two-way cross-over design with a 1 week washout period, 10 healthy volunteers were randomized to received 200 mg carbamazepine orally with 300 ml of Coca-Cola or water. Blood samples were collected at 0, 0.5, 1, 2, 3, 6, 9, 12, 24, 48 and 72 h after drug administration. Plasma carbamazepine levels were higher with Coca-Cola as compared to water. The AUC0-infinity and Cmax of carbamazepine were significantly enhanced after Coca-Cola while tmax was achieved earlier with Coca-Cola. The results of the study indicate that concomitant administration of Coca-Cola enhances the rate and extent of absorption of carbamazepine.

Adult↗

Influence of an acidic beverage (Coca-Cola) on the pharmacokinetics of phenytoin in healthy rabbits.

This study was carried out to evaluate the influence of an acidic beverage (Coca-Cola) on the pharmacokinetics of phenytoin in rabbits. In a cross-over study, phenytoin was given orally at a dose of 30 mg/kg and blood samples were taken at different intervals from 0-24 h. After a washout period of 7 days, Coca-Cola (5 ml/kg) was administered in combination with phenytoin (30 mg/kg) and blood samples were taken at various time intervals from 0-24 h. The same rabbits continued to receive Coca-Cola (5 ml/kg) for another 7 days. On the 8th day, Coca-Cola (5 ml/kg) in combination with phenytoin (30 mg/kg) was administered and blood samples were taken at similar intervals. Plasma was separated and assayed for phenytoin by high performance liquid chromatography (HPLC) and various pharmacokinetic parameters were calculated. It was concluded that an acidic beverage (Coca-Cola) increases the extent of absorption of phenytoin by significantly increasing the Cmax and AUC(o-á) of phenytoin. These results warrant the reduction of phenytoin dose when administered in combination with Coca-Cola to avoid any toxicity.

Administration, Oral↗

Diurnal fluctuations of cocaine and potential precursors in leaves of Erythroxylum coca.

Cocaine is abundant in leaves of Erythroxylum coca var. coca Lam. Consequently, cocaine and two of its early biosynthetic precursors were monitored for 24 h to determine whether they fluctuated diurnally. E. coca was grown under controlled environmental conditions in a growth chamber in soil at pH 3.5. After 17.5 months of growth, leaves not less than 35 days old were harvested every 2 and 4 h for 24 h for arginine, phenylalanine and cocaine content, respectively. The content of cocaine was determined by GC/MS and amino acid content by HPLC. Diurnal fluctuation of cocaine occurred during the 24 h cycle. Cocaine was highest in leaves of E. coca at 8 and 16 h where its content was 7.67 and 9.45 mg.g-1 dry weight, respectively. Arginine and phenylalanine in leaves of E. coca also displayed diurnal rhythmic patterns of fluctuation. The content of arginine declined from hours 6 to 12 and increased to the highest content at 13 h (21.8 mg.g-1 dry weight). Overall, phenylalanine content was lower than arginine, but had two peak periods of accumulation during the 24 h cycle, occurring at 8 and 14 h. The content of phenylalanine in leaves of E. coca during the peak hours was 6.98 and 6.54 mg.g-1 dry weight, respectively.

Alkaloids↗

Influence of acidic beverage (Coca-Cola) on pharmacokinetics of ibuprofen in healthy rabbits.

The study was aimed at determining the effect of Coca-Cola on the pharmacokinetics of ibuprofen in rabbits. In a cross-over study, ibuprofen was given orally in a dose of 56 mg/kg, prepared as 0.5% suspension in carboxymethyl cellulose (CMC) and blood samples (1 ml) were drawn at different time intervals from 0-12 hr. After a washout period of 7 days, Coca-Cola in a dose of (5 ml/kg) was administered along with ibuprofen (56 mg/kg) and blood samples were drawn from 0-12 hr. To these rabbits, 5 ml/kg Coca-Cola was administered once daily for another 7 days. On 8th day, Coca-Cola (5 ml/kg) along with ibuprofen (56 mg/kg), prepared as a suspension was administered and blood samples (1 ml each) were drawn at similar time intervals. Plasma was separated and assayed for ibuprofen by HPLC technique and various pharmacokinetic parameters were calculated. The Cmax and AUC0-alpha of ibuprofen were significantly increased after single and multiple doses of Coca-Cola, thereby indicating increased extent of absorption of ibuprofen. The results warrant the reduction of ibuprofen daily dosage, frequency when administered with Coca-Cola.

Administration, Oral↗

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↗

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↗