Stimulants II Flashcards by Chrystel Bamba

Tobacco traditional medicine used to treat

Asthma
Cough
Toothache
Sedative

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Jean Nicot

introduces tobacco to France

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Green Tobacco Sickness

Essentially nicotine poisoning
Occurs in contact with wet tobacco or sweat

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Symptoms of Green Tobacco Sickness

Nausea
Vomiting
Headache
Dizziness

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Nicotine

Major Alkaloid in tobacco
Stored in leaf
Synthesized in root
Derived from aspartic acid

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Wilhelm Posselt and Karl Reinmann (germany)

Isolated nicotine from the tobacco plant and identified it as a poison

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PHYSIOLOGICAL RESPONSES TO NICOTINE

Stimulant, depressant, tranquilizer, narcotic
Analgesic-like effect

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Low nicotine concentrations

Increased blood pressure
Increased heart rate
Nausea, dizziness, general weakness
Muscle relaxant

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High nicotine concentrations

Convulsions
Death by Suffocations
Paralysis of Muscles used in respiration

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Responses to Nicotine in CNS

Suppresses appetite, reduces anxiety, activates dopaminergic reward system

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Toxicity of Nicotine

60 mg

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Nicotine Addiction

15 cigarettes per day

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Fetal effects of Nicotine

can cross the placenta

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Nicotine Withdrawal symptoms

craving, mood changes, cognitive deficits, sleep disturbance

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Respiratory problems connected to Tobacco

Emphysema
Labored breathing, wheezing, chest pain

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Particulates

Nicotine, tobacco tars and resins, Phenolics Nitrosamines, Oils, Formic Acid, butyric acid, acetic acid

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Gases

Nitrogen, carbon dioxide, carbon monoxide, Ammonia, Hydrogen Sulfide, Hydrogen cyanide

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Effects of arecoline

Increased heart rate and blood pressure
Increase memory and speed of mental processing

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Arecoline addiction

Typical symptoms similar to those seen with tobacco

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Coca Plant

Native to Colombia, Ecuador, Bolivia, Western Brazil
Leaves produce cocaine

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Domestication of the Coca Plant

Large scale cultivation in Peru, Bolivia, Colombia

First cultivated in easter Andes of Bolivia 7000 years ago

Growth in other areas more recent
5000 years ago

Often grown on mountain terraces called Cocales
Some cocales under cultivation for 800 years

Vin Mariani

Angelo Mariani produced a beverage that was a mix of red Bordeaux wine and coca leaf extract

Pemberton’s French wine coca

1880s American pharmacist concocts “intellectual beverage” based on Vin Mariani

Flavoured with coca leaf

Father of modern surgery

W.S Halstead

Sigmund Freud

Experiments with cocaine to alleviate depression and overcome withdrawal symptoms

Evo Morales

Bolivian President Wishes to legalize coa Growth for medicinal uses Major concerns for US

aliphatic non-protein amino acid precursor of cocaine

ornithine

Basic structural element of coca alkaloids

Tropane ring Ring may be open or closed

Extraction of Coca Alkaloids

Mash leaves with alkali, kerosine, or gasoline to form soluble free base form of alkaloids Coca paste is converted into water soluble form, cocaine hydrochloride Use medicinally and illegally

Derivatives of ecgonine 3 major alkaloids

Cocaine, Cinnamylcocaine and Truxilline

Derivatives of tropine

Valerie, Tropacocaine

Derivatives of hygrine

Hygroline, Cuschohygrine

Effects of Cocaine according to Freud

Exhilaration and vivid euphoria Greater capacity for work Long lasting mental or physical work without fatigue Complete elimination for food or sleep

CNS stimulant (Cocaine)

Mucous membranes of nose facilitate fast passage to brain Maximum effect in 15-30 minutes The perfect illusion User is more competent and productive Full of energy, smarter, more vigilant, more confident Ego food

Low dosage of Cocaine

Increased heart rate and blood pressure, increased body temperature

Increasing usage of Cocaine: symptoms related to toxicity

Convulsions and respiratory failure Cardiovascular collapse Liver damage

Extreme Use of Cocaine

Euphoria of high is contrasted with depression during withdrawal as drug leaves the system Suicidal thoughts

Medicinal Uses of Cocaine

Acts as local anesthetic and vasoconstrictor Modern: used as local anesthetic occasionally

Cocaine Mechanism of Action

Blocks reuptake transporters of dopamine and norepinephrine Results in increased levels of neurotransmitters in the synapse

Dopamine

brain neurotransmitter Affects limbic system pleasure center Stimulates memory and emotions

Norepinephrine

stimulates heart and muscle contractions More NE = greater endurance

Cocaine affects dopamine reuptake

Dopamine associated with reward system in the brain More dopamine = more reward Leads to psychological and physical dependence

Overdose often fatal

due to norepinephrine effects on vasoconstriction of blood vessels

Qat

Catha edulis

Has powerful stimulant effect

North American Ephedra

Ephedra nevadensis, Ephedra trifuera American Southwest and Mexico

Ephedra alkaloid is isolated from Ephedra by

Yamanashi, Japanese chemist

Schimdt and Chen

Chemists from Eli Lilly Pharmaceutical Co. Showed ephedrine to be an effective decongestant

Sympathomimetic drug

Mimics neurotransmitters that normally activate the sympathetic nervous system

Agonist at alpha and beta adrenergic receptors

Where norepinephrine and epinephrine normally bind Promotes bronchial dilation, increases heart rate and blood pressure

Amphetamines:

Synthetic ephedrine Substitutes for ephedrine Used to dilate bronchial passages Stimulate sympathetic branch of PNS

Benzedrine

first amphetamine used in 1932 to clear nasal passages and for narcolepsy Known for its euphoric effects