Hawler medical university college of pharmacy department of Pharmacognosy
prepared by Rawnaq n. al-tabakh Niveen Imad Alyas
Erythroxylum coca Family : erythroxylaceae
Scientific classification is as follow : Kingdom plantae Division magnoliophyta Class magnoliopsida Order malpighiales Family erythroxylaceae Genus Erythroxylum Species E.coca
Geographical source : It's cultivated in Columbia , java , sri lanka , Bolivia , Peru , and India . It's a shrub or small tree , pyramidal in shape , up to 6 m in high , with dark green , ovate leaves .
Habitat : The coca shrub develop well in tropical humid climates , preferably zones such as clearing in forests , or on the wet sides of mountains .
Cultivation : - Coca plant is grown similarly to tea plantation . seeds are sown in rich , light and well drained soil at an altitude of 500 2000 meters - Only the stiff ripe leaves , easily detached , are collected . - Three harvests are collected annually , the first from the pruned twigs , the second in June and the third in November . the leaves are dried and packed in bag
Morphology :The plant resembles a blackthorn bush, and grows to a height of 2 3 m (7 10 ft). The branches are straight, and the leaves, which have a green tint, are thin, opaque, oval, and taper at the extremities.
The flowers are small, and disposed in little clusters on short stalks; the corolla is composed of five yellowishwhite petals, the anthers are heartshaped, and the pistil consists of three carpel's united to form a threechambered ovary
The flowers mature into red berries
Leaves .. are entire 3-8 cm long , 1.5-4 cm wide , shortly petiolated , apex acute , base tapering , lamina brown and glabrous , margin entire , midrib prominent on the lower surface with a ridge on its upper surface , apex acute , surface glabrous , slightly glossy , texture thin , odour distinct , taste bitter . The lower surface shows two , very character , curved lines , one on either side of the midrib. Odour characteristic , taste at first bitter and slightly aromatic , the alkaloids afterwards causing numbness of the tongue and lips
Main active constituents : - The coca leaves contain 0.7 1.5 % of alkaloids which are of three derivatives of : 1.ecgonine ( cocaine , cinnamoylcocaine , alpha and beta truxilline ) 2.tropine ( tropococaine , valerine ) 3.hygrine ( hygroline , suscohygrine - Besides the alkaloids , coca leaves contain an essential oil.
Cocaine : Is the methyl ester of benzoyl ecgonine . cocaine is prepared by semi-synthetic method from plant derived ecgonine . when hydrolyzed it yields , ecgonine , benzoic acid and methyl alcohol .
Cocaine shows central and peripheral nervous system action. it is a psychomotor stimulant with a strong abusing property . the abuse liability is through a prolongation of dopamine in the synapse by blocking dopamine reuptake mechanism .
Cocaine hydrochloride is an ingredient in Bromptom's cocktail , which is used to control severe pain in terminal cancer . it counteract the narcotic induced sedation and respiratory depression together with the narcotic analgesic ingredient like methadone and morphine , used in cocktail . it potentiates the analgesic effects
Extraction of cocaine:Cocaine can be extracted from the leaves with almost any organic solvent. Moisten the dried, powdered leaves with Na carbonate solution and extract with cold benzene or petroleum ether. Extract the organic solution with small amounts of dilute sulfuric acid and basify the extract with Na carbonate (the alkaloids precipitate). Dissolve the precipitate in ether, separate the ether from the aqueous Na carbonate and dry and evaporate in vacuum the ether. Dissolve the residue in methanol and heat with sulfuric acid or methanol HCl; dilute with water and extract with CHCl3. Concentrate and neutralize the aqueous layer and cool to precipitate methylecgonine sulfate, which is converted to cocaine in one step. The alkaloids can also be extracted directly from the powder with dilute sulfuric acid
USES : Cocaine is a local anesthetic . it is the first known local anesthetic from which various other synthetic substitutes with similar activity have been prepared . That it serves as a model for a large number of synthetic local anesthetics that have been produced to increase the stability and reduce the toxicity of the natural product . In general , coca leaves are used as stimulant , restorative , and also in convulsions. Cocaine reduces the sedative and respiratory depressant effect of morphine and allied drugs . due to CNS stimulant properties . it's also used for dental anesthesia
Biosynthesis : It starts with l-ornithin and passes through N-methylputrescine , which is then oxidized to form N-methyl-1-pyrrolinium ion . Addition of 2 acetyl coenzyme A gives 4-acetoacetyl coenzyme A derivative(keto ester) . Pyrrole oxidation and cyclization lead to the tropane derivative( carboxy tropinone )methylation yields carboxy methyl tropinone . Ketone reduction provides ecgonine methyl ester , which is benzoylated to give cocaine . Benzoic acid required for esterification of 10 en route to cocaine is synthesized from phenylalanine via cinnamic acid
Folklore : coca is known in south America since from 500 years ago specially in Bolivia and Peru . pure cocaine isolated from the plant in 1880 by Alfred neiman and was used as local anesthetic in eye , nose and throat surgery because of its role in narrowing blood vessels and preventing bleeding . it has been used in the beginning of the last century as a treatment of depression ( by Sigmund Freud ) , indigestion , crisis and people rely on drugs . coca leaves were also mixed with cola plant for the manufacture of the soft drink coca cola. In 1906 prevent the sale of cocaine in the pharmacy and added to drinks
New updates :Cocaine is crystalline alkaloids obtained from the leaves of the coca plant . it's a stimulant of the central nervous system , suppressing the appetite , create a sense of happiness and beaming the energy increased . although it's often used for the entertainment by this effect. Cocaine is very addictive , and the cultivation , possessing and distribution is illegal for non medical purposes in all parts of the world
People who smoke cocaine suffer from ??? Those who smoke cocaine suffer from shortness of breath and thoracic pain as a result of severe lung injury and bleeding
How long does cocaine take to give it s effect ??
Cocaine reaches the brain in over 3-5 minutes as a smoke and 15 30 minutes intravenously
Effects of cocaine :When a person takes cocaine, it causes a rush. There is between one or two minutes of intense pleasure. This is followed by five to 8 minutes of euphoria, then as the high comes down, an overwhelming urge for more, which may last for a day. When a user is between cocaine doses or halts usage, the opposite effects occur. The user is depressed and tired
Why is cocaine attractive ??? Cocaine is attractive to users because it triggers dopamine. Dopamine is a neurotransmitter that is present in many regions of the brain. In normal mice, the introduction of cocaine increases dopamine by 150 percent. Dopamine regulates movement, emotion, motivation, and the feeling of pleasure.
The first time people use cocaine and its effects fade, they want more. Such is the nature of the drug. The main reason cocaine use continues is the need to experience the "high" and the development of dependence. Dependence is, "the need to maintain a level of the drug in the brain to both satisfy the need and stimulate the reward center, and avoid physical withdrawal symptoms" . There is continual research occurring about dependence and how it can be streamlined.
It was recently discovered through newer imaging techniques that cocaine hinders blood flow. This is why is it can cause brain damage or defects. Recent research demonstrates that if a cocaine user even thinks about cocaine, the blood flow is altered . This suggests that the addictive nature of the drug is stronger than we think, because simply thinking about it produces similar results in addicts' brains' . This is likely to be a result of the way in which cocaine changes the structure of an abuser's brain.
However, even if scientists do identify all of the factors that cause addiction, they are still faced with the dilemma of how exactly to stop the addiction. New hope to end cocaine addiction lies in experimental drugs, such as one that is used to treat epilepsy and holistic approaches such as acupuncture.