Agonists and Antagonists

Agonists activate receptors to produce the desired response.

Conventional agonists increase the proportion of activated
receptors. Inverse agonists stabilize the receptor in its inactive
conformation and act similarly to competitive antagonists. Many
hormones, neurotransmitters (eg, acetylcholine, histamine,
norepinephrine), and drugs (eg, morphine, phenylephrine,
isoproterenol, benzodiazepines, barbiturates) act as agonists.
Antagonists prevent receptor activation. Preventing activation has many
effects. Antagonists increase cellular function if they block the action of a
substance that normally decreases cellular function. Antagonists
decrease cellular function if they block the action of a substance that
normally increases cellular function.

Receptor antagonists can be classified as reversible or irreversible.

Reversible antagonists readily dissociate from their receptor; irreversible
antagonists form a stable, permanent or nearly permanent chemical bond
with their receptor (eg, by alkylation).
In competitive antagonism, binding of the antagonist to the receptor prevents binding
of the agonist to the receptor.

In noncompetitive antagonism, agonist and antagonist can be bound simultaneously,

but antagonist binding reduces or prevents the action of the agonist.

In reversible competitive antagonism, agonist and antagonist form short-lasting bonds

with the receptor, and a steady state among agonist, antagonist, and receptor is reached.
Such antagonism can be overcome by increasing the concentration of the agonist. For
example, naloxone (an opioid receptor antagonist that is structurally similar to morphine),
when given shortly before or after morphine, blocks morphine’s effects. However,
competitive antagonism by naloxone can be overcome by giving more morphine.
Categories of Drug Action
The five categories of drug action include:
1. Stimulation
- In drug action that stimulates, the rate of cell activity of the
secretion from a gland increases.
- It refers to selective enhancement of the level of activity of
specialized cells.
Stimulant Drug Types, Effects & Addiction Signs
Stimulants are a group of drugs that result in increased activity in
the body. Sometimes referred to as “uppers,” these drugs are
frequently abused due to their performance-enhancing and
euphoric effects. Generally, those who abuse stimulants
experience heightened energy levels and enhanced focus.
Stimulants speed up mental and physical processes, which can produce
desirable effects in the short-term by increasing levels of dopamine in the
brain. While users may feel great due to the short-term effects of stimulants,
long-term abuse of these drugs can have significant consequences, which is
why it is so important for those who abuse the drugs to get help as quickly
as possible.
There are both legal and illicit stimulants, and both categories are commonly
abused. Some of the most commonly abused stimulants include cocaine,
methamphetamine, and prescription stimulants, like Ritalin, Adderall and
Concerta.
Cocaine

Cocaine is one of the most well-known stimulants in the world.

A highly addictive drug, it is made from and named for the South
American coca plant. Cocaine usually comes in the form of a fine
white powder, though the popular “crack” form comes as
crystallized rocks. Cocaine and crack cocaine can be used via a
multitude of methods; the most common form of ingestion for
powdered cocaine is snorting the drug, and the most common
method for crack cocaine is to smoke it.
Signs of cocaine use include but are not limited to:

üExcitability
üDilated pupils
üRunny nose
üWeight loss
üNosebleeds
Methamphetamine

Methamphetamine is a highly addictive stimulant, more

commonly known simply as “meth.” It is usually found in either
powder or crystal form, and it can be used in a multitude of
fashions, from smoking the drug to injecting it intravenously. Its
popularity as a recreational drug is due to the initial rush of
euphoria that accompanies it. However, once that initial rush
has passed, emotions generally get more negative, with feelings
of anger and fear being common during the “crash.”
According to the U.S. National Library of Medicine, medical issues that
can arise due to methamphetamine use include:

ü Extremely high body temperatures that can result in fainting

ü Severe itching
ü Broken teeth and dry mouth, commonly referred to as “meth mouth”
due to poor dental hygiene and nutrition associated with use of the
drug
ü Cognitive issues
ü Users of methamphetamine can easily overdose, which can lead to
extreme physical problems and death.
Prescription Stimulants
Illicit drugs are not the only stimulants out there, as prescription amphetamines have
become popular drugs of abuse in recent years. These drugs include Ritalin,
Adderall, and Concerta. They are often prescribed to treat attention deficit
hyperactivity disorder (ADHD), a condition that affects an individual’s ability to focus
and control impulses.

While prescription stimulants can be necessary for those who actually suffer from
ADHD, they are commonly abused by those without the disorder in an effort to
improve focus or cognitive capabilities. They are often referred to as “study drugs”
and abused by high school and college students who take them before cramming for
finals or in an effort to manage the many demands of an active academic,
extracurricular, and social schedule.
Like other stimulants, Adderall, Ritalin, and Concerta can all
be habit-forming drugs, leading to addiction over time. While
each of these drugs is most commonly used to treat ADHD, they
have other uses as well. Adderall is a combination of
amphetamine and dextroamphetamine that can also be used to
treat narcolepsy. Ritalin contains methylphenidate and is also
used to treat mild depression and narcolepsy. Concerta also
contains methylphenidate.
While abuse of these drugs is most common among teens and young
adults, once addiction takes hold, that use often continues for years.
Students who are dependent on these drugs to manage robust schedules
often continue to rely on them as adults to manage heavy workloads,
family responsibilities, and busy social calendars.

Long-term effects from continued abuse of these prescription stimulants

include depression, cardiovascular complications, nausea, insomnia,
s t u n t e d g r o w t h i n c h i l d r e n a n d t e e n s , a n x i e t y, h y p e r t e n s i o n ,
aggressiveness, and manic states.
Other Stimulant examples:

1. Adrenaline stimulates heart

2. Pilocarpine stimulate salivary glands
3. Pictrotoxine stimulates CNS
2. Depression
In drug action that depresses, cell activity and function of a
specific organ are reduced.
Sometimes called “downers,” these drugs come in
multicolored tablets and capsules or in liquid form.
Some drugs in this category, such as Zyprexa, Seroquel and
Haldol, are known as “major tranquilizers” or “antipsychotics,”
as they are supposed to reduce the symptoms of mental illness.
Depressants such as Xanax, Klonopin, Halcion and Librium
are often referred to as “benzos” (short for benzodiazepines).
Other depressants, such as Amytal, Numbutal and Seconal,
are classed as barbiturates—drugs that are used as
sedatives and sleeping pills.
DEPRESSANTS: SHORT-
TERM EFFECTS
ü Slow brain function ü Fever
ü Slowed pulse and breathing ü Sluggishness
ü Lowered blood pressure ü Visual disturbances
ü Dilated pupils
ü Poor concentration
ü Disorientation, lack of
ü Confusion coordination
ü Fatigue ü Depression
ü Dizziness ü Difficulty or inability to urinate
ü Slurred speech ü Addiction
Higher doses can cause impairment of mem o ry, j u d g m e n t a n d
coordination, irritability, paranoia and suicidal thoughts. Some people
experience the opposite of the intended effect, such as agitation or
aggression.
Using sedatives (drugs used to calm or soothe) and tranquilizers with
other substances, particularly alcohol, can slow breathing and the heart
rate and even lead to death.
A tranquilizer refers to a drug which is designed for the treatment of
anxiety, fear, tension, agitation, and disturbances of the mind, specifically
to reduce states of anxiety and tension.
DEPRESSANTS: LONG-TERM EFFECTS
Tolerance to many depressants can develop rapidly, with larger doses needed to
achieve the same effect. The user, trying to reach the same high, may raise the dose
to a level that results in coma or death by overdose.

Long-term use of depressants can produce depression, chronic fatigue, breathing

difficulties, sexual problems and sleep problems. As a dependency on the drug
increases, cravings, anxiety or panic are common if the user is unable to get more.

Withdrawal symptoms include insomnia, weakness and nausea. For continual and
high-dose users, agitation, high body temperature, delirium, hallucinations and
convulsions can occur. Unlike withdrawal from most drugs, withdrawal from
depressants can be life-threatening.
DEPRESSANTS
Brand Names Street Names
ü Xanax ü Barbs
ü Candy
ü Valium
ü Downers
ü Halcion ü Phennies
ü Librium ü Reds
ü Ativan ü Red Birds
ü Klonopin ü Sleepsing pills
ü Tooies
ü Amytal
ü Tranks
ü Nembutal ü Yellows
ü Seconal ü Yellow Jacket
ü Phenobarbital
3. Replacement
- Replacement drugs such as insulin replace essential
body compounds.
For examples:
1. Levodopa in Parkinsonism
2. Insulin in Diabetes Mellitus
3. Iron in anemia
4. Inhibition or killing of organisms (Cytotoxic Action)
- Drugs that inhibit or kill organisms interfere with bacterial
cell growth.
For examples:
ü Penicillin exerts its bactericidal effects by blocking the
synthesis of the bacterial cell wall.
ü Zidovudine, also known as azidothymidine, is an antiretroviral medication
used to prevent and treat HIV/AIDS.

5. Irritation
- Drugs also can act by the mechanism of irritation
- Laxatives irritate the inner wall of the colon, thus increasing
peristalsis and defecation.