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PubMedDate not supplied

Cocaine's use in ophthalmology: our 100-year heritage.

One hundred years ago the fledgling ophthalmologist Carl Koller demonstrated that the alkaloid cocaine was a local anesthetic suitable for rendering the eye temporarily insensible to pain. It was an event of historical significance, as his discovery opened the door not only to a new era in ophthalmic surgery, but to surgery in general. In this paper we review the ancient uses of the coca leaf, the historical events leading up to and following Koller's discovery, and the present day uses of cocaine in ophthalmology and medicine.

Anesthesia, Local↗
PubMed1994

Tissue distribution of human acetylcholinesterase and butyrylcholinesterase messenger RNA.

Cholinesterase inhibitors occur naturally in the calabar bean (eserine), green potatoes (solanine), insect-resistant crab apples, the coca plant (cocaine) and snake venom (fasciculin). There are also synthetic cholinesterase inhibitors, for example man-made insecticides. These inhibitors inactivate acetylcholinesterase and butyrylcholinesterase as well as other targets. From a study of the tissue distribution of acetylcholinesterase and butyrylcholinesterase mRNA by Northern blot analysis, we have found the highest levels of butyrylcholinesterase mRNA in the liver and lungs, tissues known as the principal detoxication sites of the human body. These results indicate that butyrylcholinesterase may be a first line of defense against poisons that are eaten or inhaled.

Acetylcholinesterase↗
PubMed1987

Oral self-administration of cocaine: chronic excessive intake by schedule induction.

Rats were exposed to daily 3-hr schedule-induced polydipsia sessions (fixed-time 1 min food-pellet delivery) with a cocaine hydrochloride solution as the available session fluid. Cocaine intake level (mg/kg) was a direct function of solution concentration (0.02-0.2 mg/ml). In a second experiment with 0.15 mg/ml cocaine solution available, mean daily session cocaine intake remained constant at about 40 mg/kg over the 5-week period of the experiment. Post-session serum samples of animals drinking either 0.15 or 0.2 mg/ml cocaine solution yielded serum cocaine values that were similar to those producing subjective "highs" in coca-leaf chewers and experienced users of cocaine. The schedule-induction technique can be used to induce the intake of drug solutions, including those which perhaps taste bitter, so that chronic and pharmacologically significant consequences ensue.

Animals↗
PubMed1982

Antigenic and allergenic changes during storage of a pollen extract.

The changes that occur in the antigens and allergens of a timothy grass pollen extract during storage were measured by radioallergosorbent test (RAST) inhibition, isoelectric focusing, (IEF), crossed immunoelectrophoresis (CIE) and crossed radioimmunoelectrophoresis (CRIE) and a dye-binding protein assay. Storage intervals varied from 7 to 92 days at temperatures of 4 degrees, 22 degrees, and 35 degrees C and the freeze-dried extract was rehydrated and stored in either phosphate-buffered saline with 50% glycerol (PBSG) or Coca's solution (CS). For extracts stored in CS at 35 degrees C, allergenic activity as measured by RAST inhibition dropped by almost one half at 7 days and certain of the IEF, CIE, ad CRIE bands were no longer visible, showing that these properties correlated with allergenic activity. After 65 dys, no IEF bands were visible but three CIE bands could be visualized. At 22 degrees the changes were slower and at 4 degrees C no changes were observed for the 92-day storage time. Extracts stored in PBSG showed some of the same changes but were much more stable at all temperatures. During storage, the protein content as measured by dye binding was also reduced, showing tha proteins were fragmenting. Because some of the allergenic proteins disappeared more rapidly than others, there was not only a loss in total allergenic activity but also a change in specificity. This raises serious questions concerning the use of such extracts, especially for diagnosis.

Allergens↗
PubMed1979

Convention on psychotropic substances, 1971. The role and responsibilities of the World Health Organization.

1. The world community has realized as early as the beginning of this century that collective action between nations is to be more effective in controlling drugs of abuse. A number of international drug control treaties including the Single Convention on Narcotic Drugs, 1961, controls drugs primarily obtained from plant material (opium, coca leaves and cannabis) and synthetic analogues of morphine. The Convention on Psychotropic Substances, 1971, is aimed at controlling psychotropic substances and was formulated in Vienna in 1971. 2. The Convention on Psychotropic Substances, 1971, lays a great responsibility on the World Health Organization to recommend to the United Nations Commission on Narcotic Drugs notifications initiated by the World Health Organization, or by a party to the Convention, regarding international control.

International Cooperation↗
PubMedDate not supplied

Cocaine pharmacokinetics in humans.

Cocaine was given by intravenous administration to human subjects and the concentrations in plasma were measured by gas chromatography--mass spectrometry. Many pharmacokinetic parameters were found to have a strong dose dependence over the range 1 - 3 mg/kg. The terminal plasma half-life in minutes is given by the equation t1/2(beta) = 13.5 + 24.5 dose (r = 0.946). The total plasma clearance in liters/kg per h is 2.51--0.67 dose (r = -0.973). From analysis of previously published data the absorption half-life t1/2(ab) is approximately 8 min for gastrointestinal and for nasal inhalation absorption. The bioavailability for nasal inhalation is approximately 60%. While routes of administration for modern recreational use could lead to unexpected drug accumulation in the blood it is not likely to occur from chewing coca leaves.

Adult↗
PubMedDate not supplied

The ambulatory treatment of noncompulsive users of psychoactive substances.

This paper presents the experience of "La Casa" Programme, a center of the University of Los Andes (Bogotá, Colombia) aimed at prevention, treatment, and research in the fields of drug addiction and AIDS. The multimodal strategy at "La Casa", ambulatory and almost free of charge, has constituted a unique approach in Colombia. The country has a heavy and specific drug consumption problem: in the last ten years the number of regular consumers of a mixture of alcohol, coca paste ("basuco")/cocaine and marihuana has increased to almost 500,000 people; state facilities and human resources are scarce, thus the importance of an appropriate use of them and search for alternatives.

Adolescent↗
PubMedDate not supplied

History of anesthesia in Germany.

The first ether anesthetic was administered in Germany by J.F. Heyfelder (1798-1869) at the Erlangen University Hospital on January 24, 1847. Thereafter, famous discoveries occurred in the field of pharmacology. Albert Niemann isolated cocaine from the coca shrub in 1860; Emil Fischer synthesized the first barbiturate, Veronal, in 1902; and Helmut Weese promoted the first ultra-short-acting barbiturate, hexobarbital (Evipan), in 1932. The local anesthetic effect of cocaine was reported by Koller at the Congress of the German Society for Ophthalmology on September 15, 1884, in Heidelberg. Many new techniques were tried first in German hospitals. Friedrich Trendelenburg carried out, by tracheotomy, the first operation with endotracheal intubation in 1869, and Franz Kuhn promoted and clinically practiced endotracheal intubation in Heidelberg beginning in 1900. August Bier performed the first operation under spinal anesthesia at the Kiel University Hospital on August 16, 1898. Carl Ludwig Schleich (1859-1922) standardized the methods of infiltration anesthesia by using a cocaine solution in sufficient dilution. The development of anesthesia machines was greatly influenced by Heinrich Dräger (1847-1917) and his son Bernhard Dräger (1870-1928). The Dräger Company in Lübeck built the first anesthesia machine with a carbon dioxide (CO2) absorber and circle system in 1925. Paul Sudeck and Helmut Schmidt worked with this system at the Hamburg University Hospital and reported their results in 1926. The first Dräger anesthesia machine was produced in 1902 and introduced into clinical use by Otto Roth (1863-1944) in Lübeck. Before the Second World War, three universities in Germany carried out research in the field of anesthesia: the University of Freiburg with H. Killian, the University of Hamburg with P. Sudeck and H. Schmidt, and the University of Würzburg with C.G. Gauss. Killian and Gauss established the first journals, Der Schmerz and Narkose und Anaesthesie, in 1928. After the Second World War, the field of anesthesia in Germany rapidly regained international standards. The journal Der Anaesthesist was founded in 1952, and the German Society for Anesthesiology and Intensive Medicine was established in 1953.

Anesthesia, General↗
PubMed2006

The potential for sodium hexametaphosphate (SHMP) found in common children drinks to limit acid production in the oral biofilm.

OBJECTIVE: Sodium hexametaphosphate (SHMP) is a widely used industrial preservative commonly found in children's drinks. In this paper we examined the effect of SHMP incorporated into children's drinks on acid production by the oral biofilm by monitoring salivary concentrations of lactic acid. MATERIALS AND METHOD: Twelve healthy adult subjects with an average age 36 years (range 26-54 years) consumed 10 ml from four children's beverages (Coca Cola and three types of Sunny Delight supplemented with SHMP) and a standard solution of sucrose. Saliva was collected at intervals following exposure of the oral biofilm to the drinks and the clearance of carbohydrates and the appearance of lactate was measured using standard enzymatic techniques. RESULTS: All the carbohydrates derived from the drinks were cleared from saliva within 15 min of consumption. Comparison of two drinks [Sunny D Normal and Sunny C] with the same carbohydrate, but different SHMP concentrations suggested that SHMP in these beverages had no significant effect on acid production. CONCLUSIONS: In this clinical study the role of SHMP, incorporated in common beverages, did not inhibit acid production from carbohydrates.

Acids↗
PubMed2004

Sensitivity-enhanced IPAP experiments for measuring one-bond 13C'-13Calpha and 13Calpha-1Halpha residual dipolar couplings in proteins.

Sensitivity-enhanced 2D IPAP experiments using the accordion principle for measuring one-bond 13C'-13Calpha and 1Halpha-13Calpha dipolar couplings in proteins are presented. The resolution of the resulting spectra is identical to that of the decoupled HSQC spectra and the sensitivity of the corresponding 1D acquisitions are only slightly lower than those obtained with 3D HNCO and 3D HN(COCA)HA pulse sequences due to an additional delay 2Delta. For cases of limited resolution in the 2D 15N-1HN HSQC spectrum the current pulse sequences can easily be modified into 3D versions by introducing a poorly digitized third dimension, if so desired. The experiments described here are a valuable addition to the suites available for determination of residual dipolar couplings in biological systems.

Algorithms↗
PubMed2004

The set of triple-resonance sequences with a multiple quantum coherence evolution period.

The new pulse sequence building block that relies on evolution of heteronuclear multiple quantum coherences is proposed. The particular chemical shifts are obtained in multiple quadrature, using linear combinations of frequencies taken from spectra measured at different quantum levels. The pulse sequences designed in this way consist of small number of RF-pulses, are as short as possible, and could be applied for determination of coupling constants. The examples presented involve 2D correlations HNCO, HNCA, HN(CO)CA, and H(N)COCA via heteronuclear zero and double coherences, as well as 2D HNCOCA technique with simultaneous evolution of triple and three distinct single quantum coherences. Applications of the new sequences are presented for 13C,15N-labeled ubiquitin.

Carbon Isotopes↗
PubMed2004

Neural correlates of behavioral preference for culturally familiar drinks.

Coca-Cola (Coke) and Pepsi are nearly identical in chemical composition, yet humans routinely display strong subjective preferences for one or the other. This simple observation raises the important question of how cultural messages combine with content to shape our perceptions; even to the point of modifying behavioral preferences for a primary reward like a sugared drink. We delivered Coke and Pepsi to human subjects in behavioral taste tests and also in passive experiments carried out during functional magnetic resonance imaging (fMRI). Two conditions were examined: (1) anonymous delivery of Coke and Pepsi and (2) brand-cued delivery of Coke and Pepsi. For the anonymous task, we report a consistent neural response in the ventromedial prefrontal cortex that correlated with subjects' behavioral preferences for these beverages. In the brand-cued experiment, brand knowledge for one of the drinks had a dramatic influence on expressed behavioral preferences and on the measured brain responses.

Adult↗
PubMed2001

Secondary structure of human apolipoprotein A-I(1-186) in lipid-mimetic solution.

The solution structure of an apoA-I deletion mutant, apoA-I(1-186) was determined by the chemical shift index (CSI) method and the torsion angle likelihood obtained from shift and sequence similarity (TALOS) method, using heteronuclear multidimensional NMR spectra of [u-(13)C, u-(15)N, u-50% (2)H]apoA-I(1-186) in the presence of sodium dodecyl sulfate (SDS). The backbone resonances were assigned from a combination of triple-resonance data (HNCO, HNCA, HN(CO)CA, HN(CA)CO and HN(COCA)HA), and intraresidue and sequential NOEs (three-dimensional (3D) and four-dimensional (4D) 13C- and 15N-edited NOESY). Analysis of the NOEs, H(alpha), C(alpha) and C' chemical shifts shows that apoA-I(1-186) in lipid-mimetic solution is composed of alpha-helices (which include the residues 8-32, 45-64, 67-77, 83-87, 90-97, 100-140, 146-162, and 166-181), interrupted by short irregular segments. There is one relatively long, irregular and mostly flexible region (residues 33-44), that separates the N-terminal domain (residues 1-32) from the main body of protein. In addition, we report, for the first time, the structure of the N-terminal domain of apoA-I in a lipid-mimetic environment. Its structure (alpha-helix 8-32 and flexible linker 33-44) would suggest that this domain is structurally, and possibly functionally, separated from the other part of the molecule.

Apolipoprotein A-I↗
PubMed2000

Chemotaxonomy and geographical distribution of tropane alkaloids.

This review illustrates the distribution of tropane alkaloids within the families Solanaceae, Erythroxylaceae, Proteaceae, Euphorbiaceae, Rhizophoraceae, Convolvulaceae and Cruciferae. Whereas tropane alkaloids are characteristic of the genera Datura, Brugmansia (tree datura) and Duboisia of the Solanaceae, the distribution is more widespread with novel tropane derivatives in families not traditionally associated with these bases. The chemical nature of more recently discovered water-soluble calystegines and the di- and trimeric forms from the Convolvulaceae (e.g. schizanthines from Schizanthus spp.), truxillines from Bolivian coca leaves and moonines of Erythroxylum moonii are highlighted. Where possible and appropriate, links between the phytochemistry and taxonomy are discussed.

Brassicaceae↗
PubMed1986

Epidemic free-base cocaine abuse. Case study from the Bahamas.

Beginning in 1983, a sharp increase was noted in the number of new admissions for cocaine abuse to the only psychiatric hospital and to the primary outpatient psychiatric clinic in the Bahamas. For the two facilities combined, new admissions for cocaine abuse increased from none in 1982 to 69 in 1983 and to 523 in 1984. Although there was some evidence for a rise in cocaine use during this time, as the drug became cheaper and more available, a primary cause of this medical epidemic seemed to be a switch by pushers from selling cocaine hydrochloride, which has a low addictive potential, to almost exclusive selling of cocaine free base, which has a very high addictive potential and causes medical and psychological problems. Although the use of free cocaine base is rising around the world, this is the first report of a nationwide medical epidemic due almost exclusively to this form of the drug, although similar problems are reported with smoking coca paste in South America.

Adolescent↗
PubMed1980

Plant hallucinogens, shamanism and Nazca ceramics.

The ceramics of the ancient Nazca, an extinct people that lived on the south coast of Peru from 100 to 800 AD, are examined. It is suggested that plant hallucinogens and stimulants including Trichocereus pachanoi, Erythroxylon coca, Datura spp., and Anadenanthera peregrina were utilized in religious ritualism connected with shamanism, stressing personal ecstasy as a means of contact with the supernatural on the part of regional religious-political leaders. Shamanic themes linked to world-wide plant hallucinogenic ingestion are identified and summarized, and their representation in Nazca ceramic art delineated.

Ceramics↗
PubMed1997

A case with coincidence of aberrant right subclavian artery and common origin of the carotid arteries.

An aortic arch variant was found in a 63 year-old male cadaver during routine dissection. An aberrant right subclavian artery (ARSA) arose from the distal aortic arch after the left subclavian artery and coursed to the right and upward behind the trachea and esophagus. A common origin for the carotid arteries (COCA) accompanied this variant of the right subclavian artery.

Carotid Arteries↗
PubMed2006

Isolation and characterization of a thermally stable recombinant anti-caffeine heavy-chain antibody fragment.

We have isolated and characterized a caffeine-specific, heavy-chain-only antibody fragment (V(HH)) from llama that is capable of being utilized to analyze caffeine in hot and cold beverages. Camelid species (llama and camel) were selected for immunization because of their potential to make heat-stable, heavy-chain-only antibodies. Llamas and camels were immunized with caffeine covalently linked to keyhole limpet hemocyanin, and recombinant antibody techniques were used to create phage displayed libraries of variable region fragments of the heavy-chain antibodies. Caffeine-specific V(HH) fragments were selected by their ability to bind to caffeine/bovine serum albumin (BSA) and confirmed by a positive reaction in a caffeine enzyme-linked immunosorbent assay (caffeine ELISA). One of these V(HH) fragments (VSA2) was expressed as a soluble protein and shown to recover its reactivity after exposure to temperatures up to 90 degrees C. In addition, VSA2 was able to bind caffeine at 70 degrees C. A competition caffeine ELISA was developed for the measurement of caffeine in beverages, and concentrations of caffeine obtained for coffee, Coca-Cola Classic, and Diet Coke agreed well with high performance liquid chromatography (HPLC) determination and literature values. VSA2 showed minimal cross reactivity with structurally related methylxanthines.

Animals↗