1. THE HISTORY OF THE DRUG : Stimulants
Stimulants are drugs that stimulate the central nervous system to increase levels of mental and
physical energy and alertness and produce an elevated mood. Which is also known as
psychostimulants. “The first amphetamine was synthesized by the German pharmacologist L.
Edeleano in 1887”. Later, in 1910 it was tested on animals and then in 1927 Gordon Alles
self-administered amphetamine and recorded his findings. They could be inhaled or taken orally
and as an effect it reduced fatigue, made alert, and gave confidence. The original purpose of this
drug was “Nonprescription medication in drug stores across the us. The Benzedrine inhaler,
marketed for nasal congestion.” Because of lack of restriction, amphetamines were sold to treat
variety of ailments: obesity, alcoholism,depression, schizophrenia, morphine and codeine
addiction, heart block and head injuries. Stimulants are self medicated over the counter drugs.
Meaning you can buy them at local pharmacy or drug stores. The most common drugs in this
category are caffeine, nicotine, cocaine and methamphetamine. Caffeine and nicotine are
classified as secondary stimulants because, unlike drugs such as amphetamines and cocaine, they
affect the sympathetic nervous system more than the central nervous system. Unlike stimulants
that are abused for recreational purposes, caffeine and nicotine produce only an increased energy
level but not a feeling of intoxication or delusional thoughts or behavior. Caffeine is the most
commonly used stimulant and most widely consumed drug in the United States, and is found in
coffee, tea, soft drinks, energy drinks, chocolate, and drugs. Caffeine may also be an ingredient
in pain relievers, diet pills, and cold and allergy medications.Caffeine belongs to a family of
drugs called methylxanthines, and it works by disrupting the action of a neurotransmitter called
adenosine. Since caffeine is usually consumed in food, it normally enters the body through the
gastrointestinal system, passing from the intestines into circulating blood, which carries it
throughout the body. Another widely ingested stimulant is the nicotine consumed in tobacco
products. Nicotine acts mostly as a stimulant in new users, but long-term users claim that it
relaxes them. The Centers for Disease Control and Prevention report that approximately 9.2% of
teenagers reported smoking cigarettes in 2014, a decrease from 15.8% in 2011. The use of
hookahs has increased in the same time period from 4.1% to 9.4%. The use of multiple tobacco
products by teenagers is reported to increase the risk for nicotine dependence and is predictive of
use in adulthood. Nicotine withdrawal symptoms include anxiety, irritability, insomnia,
depression, headaches, mood swings, difficulty concentrating, and changes in appetite. Cocaine
Cocaine is one of the strongest and shortest-acting stimulants and has a high potential for abuse
owing to its euphoric and habit-forming effects. Street names for these drugs include cigs,
smokes, tabs, blow, lines.
Amphetamines used to help ADHD: Scientist have pointed out that recent
meta-analyses of stimulant medications in substance-dependent patients with ADHD
did not find an overall reduction in substance use among amphetamine a
stimulant-dependent individuals, although most of the studies in the meta analysis did
not examine the use of an amphetamine or methylphenidate product. They stated that
while their study did show a positive effect from aggressive dosing of an amphetamine
formulation on both ADHD symptoms and cocaine use, these findings need to be
replicated in future research.
3. THE VARIOUS FORMS
This drug can be administered by inhalation and orally. The effect of different dosages of
caffeine. The threshold dose of this drug is 10 - 20 mg. And the lethal dose is 3-20 grams orally.
3.3. Calculation of margin of internal exposure (MOIE). The MOIE was first calculated
assuming that the parent chemical (caffeine) is the toxic moiety (parent chemical mode of
action) and then assuming that the major metabolite (paraxanthine) formed is the toxic
moiety.Amphetamine and closely related compounds such as methamphetamine have been used
as central nervous system stimulants for many years, but numerous undesirable side reactions
accompany their administration. For instance, they cause more or less pronounced rise in blood
pressure and there is a tendency toward developing tolerance upon continual use. The
herein-described compound does not have these serious side-effects and thus is markedly
superior to the amphetamines. The compound of this invention is also, even at high doses, free
from the undesirable adrenergic and cardiovascular actions characteristic of the amphetamines.
As increasing doses of the amphetamines are given, convulsions are usually observed. The
compound of this invention does not cause convulsions as the doses are increased. The
compound possesses a low order of toxicity and a desirable spread between effective and lethal
doses; i.e.,.a safe therapeutic index. The compound has a greater margin of safety than"pipradrol
which shows a rather narrow range between effective and toxic doses.
4. THE EFFECTS / THE SIDE EFFECTS
These drugs work by facilitating the release of the neurotransmitter norepinephrine to
improve alertness, attention span, and ability to focus. By boosting levels of glutamate,
the excitatory neurotransmitter of the brain. These drugs tend to increase energy and
alertness, elevate mood, and suppress appetite; They raise blood pressure, heart rate,
and respiration. Caffeine constricts blood vessels of the brain; for this reason it is often
a component of headache remedies .When taking these drugs in high doses, they can
cause heart arrhythmias and seizures. The prolonged or compulsive use of cocaine in
any of its purified forms can cause severe personality disturbances, inability to sleep,
and loss of appetite. Cocaine is an irritant, however, and acts to constrict blood vessels,
causing a chronic runny nose or, in severe cases, ulcerations in the nasal cavity.
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