Plant Stimulants: Amphetamines and Convulsants Flashcards
What are the two species of Ephedra that are low perennial shrubs native to Eastern Asia?
Ephedra major and E.sinica.
Are other members of the genus occurring both in Asia and North America used medicinally?
No.
What is unique to ALL Ephedra species?
They all have wiry stiff trigs, and highly reduced leaves, both adaptations to grow in dry, desert like habitats.
What is another name for the ephedras?
“Joint Firs”.
What are the ephedras an ancient lineage to?
Gymnosperms of uncertain evolutionary origin and ancestry.
What is the ancient Chines name for the important ephedra medicinal planst?
Ma Huang.
When fo written records of Ephedra date back to in China?
4000 years.
What are stimulant ephedra tonics and teas used for in china?
To improve circulation, increase blood pressure, promote perspiration, and reduce fevers.
Also used as an antihistamine to treat asthma and allergies and as a natural decongestant-good cough remedy.
What did the ancient greeks and romans refer to ephedra as?
Pliny (79 CE).
Who described ephedra in 510 CE?
Dioscorides.
When did ephedra become noticed by two American pharmacologists?
1924.
What is the active secondary product of ephedra?
Ephedrine, an amphetamine like compound.
Who isolated ephedrine?
Japanese chemist, Yamanashi in 1885.
What is the effects of ephedrine?
Powerful CNS stimulant that increases blood pressure and raises the heart rate.
Also found to have anti-histaminic properties, making it useful in treating asthma, hay fever, and common colds.
When did high demands of ephedrine peak?`
1927.
How was ephedra used in western medicine?
To dilate the pupil, increase blood pressure, treat asthma and hay fever, and to counteract overdoses of depressant drugs such as alcohol, barbiturates and morphine.
By which time did synthetic amphetamines replace the ephedrine natural product?
1950s.
What are amphetamines?
Stimulants that reduce fatigue by temporarily increasing overall mental and physical activity, speech and concentration.
What do amphetamines mimic?
Neurotransmitters such as dopamine, stimulating the CNS, and serotonin.
What is pseudoephedrine?
A stereoisomer of ephedrine, a common ingredient of many over the counter preparations, including nasal-sinus decongestants and various cough-cold influenza remedies.
How is pseudoephedrine obtained?
Is contained in Ephedra but usually obtained by yeast fermentation of dextrose in the presence of enzymes and benzaldehyde.
What is pseudoephedrine reduced or oxidized to respectively?
Methamphetmaine, or methcathinone.
When did Ephedra become a popular herbal remedy and nutritional supplement in Western communities?
1990s.
What was it (ephedra) used to promote?
Weight loss by increasing body metabolism and temperature and to improve athletic performance.
What are the adverse effects of ephedrine?
Hypertension, heart palpitations, and rapid heartbeat (tachycardia), and strokes and seizures. Even psychosis.
Who banned ephedra the natural product due to adverse health effects and when?
American Food and Drug Administration in 2004.
Canadian Advisory also wanted awareness.
What are amphetamine or benzedrine?
Ephedrine based semi-synthetic drugs introduced commercially in 1932.
When was amphetamine or benzedrine widely used?
During WWII by German troops (after 1938) and later Allied soldiers to enhance and extend performance.
Also by Japanese troops and factory workers during WWII.
What was advertised about benzedrine after the war?
“Will eliminate drowsiness and repletion of the spirit”.
What was the result of this benzedrine advertisement?
The result was the first recorded stimulant abuse epidemic, in the early 1950s.
When was the benzedrine addiction problems finally eliminated and how?
In 1958 through strong government action against the illegal manufacture and sale of benzedrine.
What was benzedrine used for in western medicine?
A decongestant in nasal inhalers in 1950s and 60s but was banned in 60s over addictive properties.
What IS benzedrine used for in western medicine?
Oral decongestants, diet pills, and bodybuilding aids.
What is methamphetamine (MA) or “speed”?
A semi-synthetic amphetamine first produced in 1929 through the simple reduction of ephedrine.
What are the characteristics of MA in comparison to ephedrine?
It is more potent and addictive than ephedrine, producing an immediate rush of energy, sense of power and well being.
What are the cycle affects of MA?
Leads to binging and withdrawal (sometimes sleeping for days).
What is MDMA or ecstasy?
A powerful derivative of methamphetamine, high dosages of which may lead to depression, memory loss, and acute insomnia.
What results in a severe overdoes of MDMA?
Impaired breathing, heart attack, and kidney failure.
What was MDMA originally advocated for in 1970s?
A psychotherapeutic agent, but by 1980s became a popular illicit street drug.
What have more recent studies found in regard to MDMA?
Smaller, controlled doses of MDMA are useful in treating severe cases of post-traumatic stress disorder.
Investigating therapeutic uses as of 2016.
What is ketamine?
An amphetamine derivative, widely used as a general anesthetic.
It is a dissociative drug, inducing a trance like state with associated sedative and analgesic effects.
True or False.
Ketamine is a N-methyl-D-aspartate (NMDA) receptor antagonist that results in rapid increase in neurotransmitter glutamate?
True.
Does ketamine increase dopamine activity in the brain?
Yes.
How is ketamine used recreationally?
To induce a potentially dangerous dissociative state known as the “K-hole”, with accompanying visual and auditory hallucinations.
How may ketamine actually be medicinally useful?
In low doses administered intravenously, it may be useful in treating severe, treatment-resistant depression and suicidal thoughts.
What example has shown these positive ideas about ketamine as a medicinal drug?
In some patients, a single dose results in rapid and relatively sustained reduction in depression symptoms and suicidal thoughts. Trials currently underway for how to treat depression used ketamine.
What is methylphenidate and what is it used for?
Another ephedrine like synthetic used to calm hyperactive children, popular in the US.
What is the drug combination of methylphenidate and what was it used for?
Fenfluramine-phentermine, widely used in the early 1990s to promote weight loss-both drugs, F and P, are ephedrine like synthetics.
When and why were these combinations banned?
In 1997, when studies showed that fen-then users developed serious heart valve problems, also due to addiction and psychoses.
What is the convulsant strychnine?
A small deciduous tree with shiny elliptical leaves, native to southern Asia and Australia, and it is in the same genus as South American curare.
What genus does strychnine and curare belong to?
Strychnos toxifera.
What is the difference between strychnine and curare?
Strychnine is a powerful muscle convulsant while curare drugs are a potent muscle relaxant.
What is the alkaloid that occurs in all part of the strychnine plant?
Strychnine.
Where is strychnine alkaloid most potent?
Seeds, bark and whole fruit.
What is dangerous about the strychnine alkaloid?
It is highly poisonous and can be deadly. Was used as a homicide poison in 1800s Europe and as an arrow poison in Southeast Asia.
What are symptoms of strychnine poisoning?
Initial agitation followed by uncontrolled muscle spasms and convulsions.
At high doses, these convulsions result in collapse of vital organ function causing death.
What type of poison was strychnine sold as in 1800s and early 1900s?
Rat poison.
How was strychnine used medicinally?
Effective as nervous system stimulant at low doses. It was recommended as a cure for fever and snakebites, to stimulate the GI tract, to improve blood circulation, and in the treatment of nervous conditions.
Also used to treat overdoses of depressants.
True or False.
Strychnine is an effective antagonist that prevents the failure of vital organ function
True.
What does strychnine implementation in mice demonstrate?
The facilitation of both short and long term memory, significantly increasing learning ability.
Why is strychnine an important drug in pharmacological research?
It shows high specificity in labeling the glycine receptor.
Crude extracts of strychnine plant have also shown to be powerfully analgesic (1000x as potent as morphine).
What are the two potent anti-malarial agents that are strychnine like alkaloids isolated from two African Strycnos species?
1) Sungucine.
2) Isostrychnopentamine.
What are the two African Strycnos species?
1) S.icaja
2) S.usambarensis
