Cocaine

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Cocaine Medical and Non-Medical Use:

Cocaine Medical and Non-Medical Use Presented by: Amin Younis Medical University of Lodz

Cocaine – What is it ?:

Cocaine – What is it ? Cocaine (benzoylmethylecgonine) is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" in addition to the alkaloid suffix -ine, forming cocaine. It is a stimulant of the central nervous system, an appetite suppressant, and a topical anesthetic.

Systematic Name:

Systematic Name methyl (1R,2R,3S,5S)-3- (benzoyloxy)-8-methyl-8-azabicyclo[3.2.1] octane-2-carboxylate

Forms of Cocaine :

Forms of Cocaine Salt since Cocaine is a weakly alkaline compound and can therefore combine with acidic compounds to form various salts . Basic as the name implies, “freebase” is the base form of cocaine, as opposed to the salt form. It is practically insoluble in water whereas hydrochloride salt is water soluble . Crack is a lower purity form of free-base cocaine that is usually produced by neutralization of cocaine hydrochloride with a solution of baking soda and water.

Appearance :

Appearance Cocaine in its purest form is a white, pearly product. Cocaine appearing in powder form is a salt, typically cocaine hydrochloride. The color of “crack” cocaine will generally range from white to a yellowish cream to a light brown.

Biochemical and Pharmacokinetic Properties:

Biochemical and Pharmacokinetic Properties Serotonin–Norepinephrine–Dopamine reuptake inhibitor Addictive – Mesolimbic Reward Pathway Hydrophilic and Lipophilic Metabolized in the liver by CYP3A4 Excreted by kidneys Half life = 1 hour

Pharmacodynamics :

Pharmacodynamics Cocaine binds tightly at the dopamine transporter forming a complex that blocks the transporter's function . Dopamine accumulates in the synaptic cleft. This results in an enhanced and prolonged postsynaptic effect of dopaminergic signaling at dopamine receptors on the receiving neuron . Prolonged exposure to cocaine, as occurs with habitual use, leads to homeostatic dysregulation of normal (i.e. without cocaine) dopaminergic signaling via down-regulation of dopamine receptors and enhanced signal transduction.

Pharmacodynamics:

Pharmacodynamics

Routes of Administration:

Routes of Administration Oral Many users rub the powder along the gum line “gummers” which numbs the gums and teeth. Another oral method is to wrap up some cocaine in rolling paper and swallow it. Coca leaves are typically mixed with an alkaline substance (such as lime) and chewed into a wad that is retained in the mouth between gum and cheek and sucked of its juices.

Routes of Administration:

Insufflation Nasal insufflation (known as "snorting" "sniffing" ) is the most common method of ingestion of recreational powdered cocaine in the Western world. The drug coats and is absorbed through the mucous membranes lining the sinuses. Routes of Administration

Routes of Administration:

Injection Drug injection provides the highest blood levels of drug in the shortest amount of time. Subjective effects include a ringing in the ears moments after injection (usually when in excess of 120 milligrams) lasting 2 to 5 minutes including tinnitus & audio distortion. Routes of Administration

Routes of Administration:

Inhalation Inhalation or smoking is one of the several means cocaine is administered. Cocaine is smoked by inhaling the vapor by sublimating solid cocaine by heating. Routes of Administration

Routes of Administration:

Suppository This method of administration is commonly administered using an oral syringe. Cocaine can be dissolved in water and withdrawn into an oral syringe which may then be lubricated and inserted into the anus or vagina before the plunger is pushed. Routes of Administration

Medical Effects:

Medical Effects Cocaine is a powerful nervous system stimulant. Its effects can last from 15–30 minutes to an hour, depending upon the method of ingestion. Cocaine is a local vasoconstrictor

Medical Effects Acute:

Medical Effects Acute Cocaine increases alertness, feelings of well-being and euphoria, energy and motor activity, feelings of competence and sexuality. Athletic performance may be enhanced in sports where sustained attention and endurance is required. Anxiety, paranoia and restlessness are also frequent.

Medical Effects Acute:

Medical Effects Acute With excessive dosage, tremors, convulsions and increased body temperature are observed. With excessive or prolonged use, the drug can cause itching, tachycardia, hallucinations, Overdoses cause tachyarrhythmias and a marked elevation of blood pressure, which can be life-threatening.

Medical Effects Chronic:

Medical Effects Chronic

Medical Effects Addiction:

Medical Effects Addiction Cocaine dependency may result in physiological damage, lethargy, psychosis, depression, akathisia , and fatal overdose. cocaine is ranked both the 2nd most addictive and the 2nd most harmful of 20 popular recreational drugs According to Lancet

Medical Use Cocaine as a local anesthetic:

Medical Use Cocaine as a local anesthetic Cocaine blocks sodium channels, thereby interfering with the propagation of action potentials; thus, it acts as a local anesthetic. Medical use is confined primarily to operative procedures of the nose and throat and treatment for dermal lacerations in children.

Medical Use Cocaine in Research:

Medical Use Cocaine in Research Recent research points to an important role of circadian mechanisms and clock genes in behavioral actions of cocaine.

Question 1:

Question 1 A long-term user of cocaine may well develop symptoms of other psychological disorders, such as: a) Major depression b) Social phobia c) Eating disorders d) All of the above

Question 2:

Question 2 When John began snorting cocaine, he would do one line and gain a feeling of euphoria that would last throughout the night. Now John snorts a line every hour or two to get the same euphoric high. In view of this, which statement is most accurate regarding John's use of cocaine ? a) John is experiencing withdrawal symptoms from cocaine. b) John had developed a dependency on cocaine. c) John is addicted to cocaine. d) John has developed a tolerance for cocaine.

Question 3:

Question 3 Which of these local anesthetics is most likely to reduce bleeding during minor surgical procedures: a) Tetracaine b) Lidocaine c) Cocaine d) Prilocaine

PowerPoint Presentation:

Thank You

Reference:

Reference http://www.cnsforum.com/imagebank/item/MAO_cocaine/default.aspx http://www.wellesley.edu/Chemistry/Chem101/addiction/sci-cocaine-addiction.html http://en.wikipedia.org/wiki/Cocaine#Detection_in_biological_fluids http://www.entnet.org/Practice/policyMedicalUseCocaine.cfm

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