Introduction to Psychopharmacology: How Drugs Interact with the Body and the Brain

Introduction
Psychopharmacology:
- field of medicine that addresses the use of medications to help correct or control mental illnesses and
drug addiction
Psychoactive drugs:
- natural, semi-synthetic, and synthetic substances that directly affect the neurochemistry and anatomy
of the CNS causing mental, emotional, and physical changes (Inaba)
- Focus on opiates and common combinations

History
- Oldest and best documented group of drugs
- Believed to be cultivated as far back as 3400 B.C. in Mesopotamia, Egypt, Greece, and Asia
- Used for medicinal properties, but recreational abuse and addiction common
- Early 1800s morphine isolated from opium and after hypodermic needle invented, new type of drug user appeared
- By 1914 concern began to grow
- Harrison Narcotic Act passed, restricting opioids to only medical use
- Today, prescription opioids are the 2nd most often illicitly abused drug in the U.S.

What are Opiates?
- Opium
- The exuded substance from the poppy Papaver Somniferum
- Opiates
- Natural opium extracts and semi-synthetic opium preparations
- Opioids
- Synthetic opium-like compounds

Common Opiates Used in College
- Morphine
- Codeine
- Oxycodone
- Use to make Percodan and Oxycontin
- Hydrocodone
- Used to make Vicodin
- Hydrocodone most widely prescribed opioid
- Heroin

Effects of Opiates
- Desired Effects vs. Side Effects
- Pain relief
- Suppresses coughs
- Controls diarrhea (constipation)
- Euphoria
- Slurred speech
- Depressed respiration & heart rate
- Miosis

Toxic Effects
- Addiction
- Overdose
- Drug contamination & adulterants > infection
- Abscesses
- STDs
- Fetal effects

How It Works: Neurotransmission
- Neuron: smallest functional unit of the nervous system
- Cell body: contains the nucleus; processes information that is received by the dendrites
- Axon: extension of the cell body that conducts an action potential
- Axon terminal receives action potential from the axon; releases neurotransmitters into synapse in response to
action potential
- Synapse: small space between axon terminal of one neuron & dendrite of another neuron or postsynaptic target

Biological Basis of Pain
- Pain signals damage
- Neurotransmitter called substance P carries pain message
- Natural opioids help protect the body
- Endorphins: enkephalins, dynorphins, beta endorphins
- Exogenous opioids work by reacting with the same receptor sites
- Mu, kappa, delta, nociceptin
- Opioids we are discussing all considered agonists of the mu receptor

Opioid Effects on Pain
- diagram

Opioids and Emotion
- Opioids also effect emotional pain
- Decrease anxiety
- Sense of detachment
- Deadening of unwanted emotions
- Opioid users take the drug for some of these effects
- Reward/control pathway activated telling body to repeat these actions during stressful periods
- Can lead users to become opioid abusers/addicts

Opioid Effects on Pleasure
- Reward/control pathway tells body to repeat actions that are good for survival
- Natural opioids, like endorphins, activate this pathway
- Cells in brain monitor action and when need filled, send signal to stop
- Exogenous opioids mimic endorphins and tell body to repeat use of these drugs
- Strong opiates like heroin disrupt stop switch
- They overload the stop switch causing it to malfunction
- Drug abusers use past the point of pain relief (Inaba)

Pharmacokinetics
- the process by which a drug is absorbed, distributed, metabolized, eliminated, and excreted by the body
(Darryl S. Inaba)













Routes of Administration
- Smoking
7-10 seconds to reach the brain
- Injection
15-30 seconds
- Snorting
5-8 minutes
- Oral
20-30 minutes

The more rapidly a psychoactive drug reaches its target in the central nervous system, the greater its reinforcing
effect
(Karan, McCance-Katz & Zajicek, 2009)

Factors Affecting Distribution
- Properties of drug
- Body weight/size
- Age
- Gender
- Genotype (diabetes example)
- Health condition
- Nutritional status
- Pharmacological state
- Environmental setting
- Psychological disposition
- Personality
- Expectation about drug effects


Drug Interactions
- Students commonly combine opiates with alcohol or anti-anxiety medications
- All are considered depressants:
- depress circulatory, respiratory, and muscular systems
- Control pain, reduce anxiety, promote sleep, lower inhibition, induce euphoria
- Additive effects
- Synergism
more than 150 prescription and OTC medications interact negatively with alcohol (Inaba)
Opiates and Alcohol
- Prescription painkillers (opiates) are often mixed with alcohol
- Both substances depress the respiratory system increasing the risk of:
- Cyanosis, cell death, and coma
- Also, one could simply stop breathing
- Some slow-release opioids can be dissolved by alcohol, releasing a days worth of opioid in a matter of minutes

History of Anxiolytic Medications
- Benzodiazepines first discovered in 1950s
- Came out on the marker in 1960s
- Quickly became popular b/c less toxic than barbiturates and other sedative hypnotics already out
- Today, they are the most widely used sedative-hypnotics in the U.S.
- However, now they are usually only prescribed for short-term and for specific conditions
- Can be very addictive, dangerous withdrawal symptoms
- Anxiety also treated with serotonin-type antidepressants and mood stabilizers


What are Benzodiazepines?
- Used in medicine for:
- Manage anxiety
- Treat sleep problems
- Control muscular spasms and seizures
- Subdue symptoms of alcohol withdrawal
- Taken recreationally for:
- Anxiety relief
- Induce mild euphoria
- Lower inhibitions
- Common benzodiazepines:
- Xanax:
- relieve symptoms of generalized anxiety disorder, panic disorder, and depression resulting from
anxiety
- Valium:
- Treat anxiety, gain relief from musculoskeletal spasms, control seizures such as those that occur
during severe alcohol or barbiturate withdrawal
- Rohypnol
- Produces anxiety relief, sedation, and amnesia, especially when taken with alcohol

Benzodiazepines and Brain Areas
- The anxiolytic effects result from the actions at limbic centers
- Actions at other regions result in side effects such as sedation, cognitive impairment, muscle relaxation, and -
increased seizure threshold
- The amygdala, orbitofrontal cortex, and insula are associated with the production of behavioral responses to
fearful stimuli and the central mediation of anxiety and panic
- Inhibition due to GABA reduces stimulation of these areas leading to decreased anxiety

Mechanism of Action
- A GABA receptor agonist
- Does not directly stimulate GABA receptor
- Binds to an adjacent site and increases the affinity of GABA for the receptor
- This increases the inhibitory synaptic action of GABA, facilitating the influx of chloride ions, causing
hyperpolarization of the postsynaptic neuron, depressing its excitability

Combining Alcohol and Anxiolytics
- Benzodiazepines used alone can have severe consequences after long term use
- Early withdrawal signs include a return of the anxiety symptoms for which drug was originally prescribed
(amplified)
- Also associated with cognitive impairments interfering with learning behaviors and academic function
- The margin of safety diminishes significantly once an individual takes benzodiazepines with alcohol (Inaba)
- Combining these drugs = synergism
- Prioritization of alcohol, Xanax not metabolized
- Increased risk of exaggerated respiratory depression and blackouts

Summary
- Close to $300 billion was spent on prescription drugs in 2009 in the U.S.
- Of the 3.8 billion prescriptions written each year, more than 350 million were for psychoactive drugs
- What can we do about this issue in our community?
- Many factors contribute to an individuals experience with these drugs, but combining alcohol with anti-anxiety
medications or opiates strongly increases risk and can have fatal consequences