Street Drugs
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Drugs are able to work because they mimic internally made substances. For example, the nicotine found in cigarettes activates a certain subclass of acetylcholine receptors called nicotinic receptors, which increases blood pressure and heart rate, improves memory, and causes adrenaline release from the adrenal glands. The receptors throughout the brain and body react to drugs by decreasing in number. This reduces a person’s sensitivity to the drug and greater amounts need to be taken to achieve the same effect. This is the downward spiral of addiction and dependence. After drug abuse stops, receptors do eventually grow back to normal levels. However, this may not be the case for a growing brain which does not fully develop until the age of approximately 25.


NOREPINEPHRINE AND RITALIN
Ritalin (methylphenidate) is an amphetamine (psycho-stimulant) that is used to treat ADHD (attention deficit hyperactivity disorder). Ritalin is chemically similar to cocaine and produces the same behavioral effects as cocaine. Ritalin works mechanically by increasing dopamine and norepinephrine, an effect that causes euphoria, mental alertness, motivation and concentration.

Ritalin (methylphenidate) and Norepinephrine
Ritalin is an amphetamine (behavioral stimulant) that is chemically similar to cocaine and produces the same “high” as cocaine.
Ritalin is used to treat ADHD (attention deficit hyperactivity disorder).
Ritalin produces euphoria, mental alertness and concentration.

Cocaine and Norepinephrine
Cocaine is used as a street drug that causes euphoria and mental alertness.
Cocaine blocks the active breakdown of norepinephrine in the synaptic area resulting in increased norepinephrine activity.

SEROTONIN AND SSRI’S
After serotonin has activated its receptor, the serotonin is broken down and inactivated by enzymes. These enzymes prevent neurotransmitters from overexciting or burning out a neuron. Normally, the serotonin remnants are absorbed back into the original secreting cell, and reassembled back into serotonin. The class of drugs called SSRI’s, (selective serotonin re-uptake inhibitors) prevent the breakdown of serotonin which allows serotonin to activate the receptor for a longer period of time.

MARIJUANA AND CELL RECEPTORS
Marijuana has a similar structure as the neurotransmitter called anandamide. Anandamide, which means “bliss” in Sanskrit, causes a feeling or peace in people get when they smoke marijuana. The quick absorption of inhaled marijuana smoke causes an immediate psychoactive response because there are one thousand times more anandamide receptors in the brain compared to other receptors.

MARIJUANA AND ALCOHOL
Chronic alcohol ingestion causes the release of high amounts of anandamide in the brain which leads to down regulation of our natural marijuana receptors. When an alcoholic stops drinking, a rebound effect causes hyperactive anandamide functioning, which leads to alcohol cravings and relapses.

ACETYLCHOLINE AND NICOTINE
The nicotine found in cigarettes activates a certain subclass of acetylcholine receptors called “nicotinic receptors” which increases blood pressure and heart rate, improves memory, and causes adrenaline release from the adrenal glands.

Natural Hormones vs. Drugs

The actions of natural hormones are regulated because they are rapidly degraded by enzymes soon after they activate a receptor. A drug is unregulated and remains locked into a receptor for a long period of time, which is the same as keeping a light switch turned on. As a result, drugs cause cells to over excite and burn out. Drugs leave the body only after they are detoxified by the liver. Water soluble drugs like cocaine hang around in body for one or two days, and fat soluble drugs like marijuana get stuck in body fat for over a month at a time.

RECEPTOR DOWN REGULATION
Down regulation is when high levels of a hormone or drugs causes receptor shrinkage. The receptors throughout the brain and body react to a high level of hormones (or drugs) by decreasing in number. For example, high levels of insulin in the blood causes a decrease in the number of insulin receptors. Drugs cause greater amounts of receptor down regulation compared than natural hormones because drugs are not broken down as easily as natural hormones. This reduces the person’s sensitivity to the drug and people will need to take greater amounts of the drug to achieve the same effect. This downward spiral is the cause of addiction and dependence. After drug abuse stops, receptors do eventually grow back to normal levels. However, this may not be the case for a growing brain

Too many dietary carbohydrates causes cell receptor down regulation of the insulin receptor. After insulin occupies its receptors, the insulin-receptor complex collapses inside of the cell and is degraded. Some receptors are recycled back to the surface of the cell but others do not make it back so quickly. This process of down regulation is a way the individual cell manages its glucose intake. Chronically ingesting an insulin elevating diet, or a high carbohydrate diet, will cause down regulation of the insulin receptor, and decrease insulin sensitivity. Cells will become less responsive to insulin and excess glucose will collect in the bloodstream. Insulin resistance is the clinical term for this and is considered the “pre-diabetic” state.


RECEPTOR UP REGULATION
When there are low circulating levels of a natural hormone, receptors will up-regulate. For example, on an extreme low carbohydrate diet, when there is little circulating insulin, insulin receptors will grow in number and become more sensitive to insulin. Once carbohydrates are reintroduced into the diet, cells respond rapidly to insulin, and insulin's message will be played out to a greater extent. This usually makes extreme low carb dieters gain their weight back, and then some more. Fat cells are said to become fat magnets after following an extreme low carbohydrate diet. Fat cell receptors have been shown to become as much as 10 times more active in their ability to sequester fat from the bloodstream following an extreme low carbohydrate diet. Receptor up-regulation can also occur after drug abuse stops. Without constant bombardment from a drug, there will be an over-shoot of cell receptors. With many receptors reaching out searching for their drug of choice, relapses and drug cravings become hard to resist.

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