009- Pharmacology of Stimulants, Depressants and Hallucinogens

 
 
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Stimulants, Depressants and Hallucinogens are available by prescription, in over the counter medications and as illicit substances.  Learn more about the effects of these types of drugs, how they impact your brain chemistry and signs and symptoms of intoxication and withdrawal.

Show Notes

2. In this Episode, we will: Define stimulants, depressants and hallucinogens  Discuss their ◦ Mechanism of action ◦ Symptoms of intoxication ◦ Symptoms of withdrawal ◦ Short and long term effects ◦ Common street names  Explore the process of differential diagnosis
3.  Method of administration greatly effects the intensity and duration of onset for various drugs ◦ Oral (slowest) ◦ Inhalation/Snorting ◦ Inhalation/Smoking ◦ Injection ◦ Rectal suppository ◦ Skin patches
4.  Drugs affect everyone differently, based on: ◦ Size, weight and health ◦ Whether the person is used to taking it ◦ Whether other drugs are taken concurrently ◦ The amount taken ◦ The strength of the drug (varies from batch to batch with illegally produced drugs)
5.  Stimulants are substances that act to excite the central nervous system ◦ Caffeine ◦ Amphetmines ◦ Cocaine
6.  Stimulants increase alertness, attention, and energy, as well as elevate blood pressure, heart rate, and respiration.  Used to treat asthma and other respiratory problems, obesity, neurological disorders, ADHD, narcolepsy, and occasionally depression
7.  Stimulants enhance norepinephrine and dopamine.  Increase in dopamine can induce a feeling of euphoria when stimulants are taken nonmedically.  Norepinepherine also increases blood pressure and heart rate, constricts blood vessels, increases blood glucose, and opens up breathing passages.
8.  Mechanism of action ◦ Increase noradrenaline/norepinepherine & dopamine in the brain in 4 ways  Bind to the presynaptic membrane causing the release of dopamine  Interact with dopamine containing synaptic vesicles, releasing free dopamine into the nerve terminal
9.  Mechanism of action ◦ 4 ways cont…  Bind to monoamine oxidase in dopaminergic neurons and prevent the degradation of dopamine, leaving free dopamine in the nerve terminal  Bind to the dopamine re-uptake transporter, causing it to act in reverse and transport free dopamine out of the nerve terminal.
10.  Generalized State Of Euphoria  Increased Energy  Confidence  Mental Alertness  Sexual Arousal  Itching And Scratching  Large Pupils  Dry Mouth  Fast Heart Beat And Breathing  Teeth Grinding  Reduced Appetite  Excessive Sweating
11.  In the 4 to 6 days after stimulant use, the following effects may be experienced: ◦ Restless sleep and exhaustion ◦ Headaches ◦ Dizziness and blurred vision ◦ Paranoia, hallucinations and confusion ◦ Irritability, mood swings and depression ◦ Anxiety ◦ Insomnia
12.  Methamphetamine has a substantially longer half-life than cocaine, thus leading to more intense and protracted withdrawal.  Chronic methamphetamine users may have episodes of violent behavior, paranoia, anxiety, confusion, and insomnia.
13.  A study in April, 2015 analyzed 21 supplements labelled as containing Acacia rigidula, a type of shrub native to Texas. ◦ Eleven of them were found to contain beta- methylphenylethylamine, or BMPEA, an isomer of amphetamine whose effect on humans has never been studied. ◦ Only 3 in which the chemical was found indicated its presence on their labels, and none of them specified the amount of BMPEA in each pill, according to the study. http://onlinelibrary.wiley.com/doi/10.1002/dta.1793/abstract  DoD list of Supplements to Avoid
14.  Toxic doses, over 5 grams per day for an adult, ◦ A cup of coffee contains 80–175 mg of caffeine, depending on the bean and preparation method ◦ Redbull: 80mg ◦ Monster: 86mg ◦ Starbucks (short) brewed coffee 8oz: 180mg ◦ Stacker II (1capsule) 200mg ◦ Vivarin (1 tablet) 200mg
15.  Possible side effects for stimulants, include: ◦ Hostility ◦ Paranoia ◦ Psychotic symptoms ◦ Unsafely elevated body temperature ◦ Irregular heartbeat, heart failure ◦ Seizures ◦ Exacerbation of existing anxiety
16.  Reduced appetite  Restless sleep  Dry mouth/dental problems  Reduced immunity  Trouble concentrating  Difficulty breathing  Muscle stiffness  Anxiety and paranoia  Depression & Suicidal Ideation  Heart/kidney problems  Increased risk of stroke  Tolerance  Confusion  Sexual dysfunction  Chest pain or palpitations  Seizures and delirium
17.  Amphetamines ◦ R-ball ◦ Skippy ◦ The smart drug ◦ Vitamin R ◦ Kibbles and bits ◦ Speed ◦ Truck drivers ◦ Bennies ◦ Black beauties ◦ Crosses ◦ Hearts ◦ LA turnaround ◦ Uppers ◦ Amps ◦ Pick-me-ups  Cocaine and Crack ◦ coke ◦ Snow ◦ 8-ball ◦ flake ◦ powder ◦ dust ◦ candy ◦ white ◦ kryptonite ◦ cookies ◦ strong ◦ Speedball is cocaine + heroin
18.  Depressants exert the opposite effect of stimulants. ◦ They s-l-o-w everything down
19.  Mechanism of Action ◦ Depressants exert their effects through a number of different pharmacological mechanisms, the most prominent of which include facilitation of GABA, and inhibition of glutamatergic or monoaminergic (dopamine, noradrenaline and serotonin) activity
20.  Types include ◦ Barbiturates (Sedatives, -barbitals) ◦ Benzodiazapines (-lam, -pam) ◦ Inhalants (Aerosols, paint, gasoline, glue) ◦ Muscle relaxants ◦ Non-Benzodiazapine hypnotics (Lunesta, Sonata) ◦ Opiates
21.  Americans use ◦ 80% of global opioid supply ◦ 99% of global hydrocodone  Direct healthcare costs are 8.7x higher for opiate abusers  Annual cost of opioid abuse ◦ 2001: $8.6 Billion ◦ 2007: $55.7 Billion
22.  Class of Drugs: Analgesic (pain killer); CNS Depressant, antitussive (cough suppressant)  Types of Drugs ◦ Natural ◦ Synthetic ◦ Semi-synthetic.
23.  Opiates may be detected in urine for 2-4 days  Heroin contains acetylcodeine  Codeine is metabolized to morphine, both substances may appear in the urine following codeine ingestion  Oxycodone does not produce a positive response to routine screens for opiates, which generally target morphine and/or codeine
24.  If patients are taking opiates or benzos for a medical purpose, send urine to the lab and monitor levels.  Buprenorphine can be abused, although it has a ceiling effect.  Buprenorphine needs to have it’s own test as it produces a unique metabolite.  Suboxone is buprenorphine + naloxone and is harder, but not impossible to abuse
25.  Short term impact (up to 5 hours) ◦ Depends heavily on the dose of morphine or heroin, the route of administration, and previous exposure ◦ Including  Psychological: Euphoria, feeling of well-being, relaxation, drowsiness, sedation, disconnectedness, delirium.  Physiological: Analgesia, depressed heart rate and respiration depression, constipation, flushing of the skin, sweating, pupils fixed and constricted, diminished reflexes
26.  Complications and Side Effects ◦ Medical complications among abusers arise primarily from adulterants and in non-sterile injecting practices ◦ Include skin, lung and brain abscesses, collapsed veins, endocarditis, hepatitis and HIV/AIDS.
27.  Complications and Side Effects ◦ Alcohol or depressants such as benzodiazepines, hypnotics, and antihistamines increase the CNS effects of opiates such as:  Sedation/drowsiness  Decreased motor skills.  Respiratory depression, hypotension
28.  Long term impact ◦ Vein collapse ◦ Depression ◦ Brain changes/damage ◦ Reduction of the production of natural pain killers
29.  Symptoms of intoxication ◦ Constricted pupils ◦ Agitation ◦ Scratching and picking
30.  Symptoms of withdrawal ◦ Begin within 6-12 hours; last 5-10 days; peak between 48-72 hours ◦ Yawning ◦ Drug Craving ◦ Irritability/dysphoria/depression ◦ Flu like Symptoms: Runny nose, sweating. vomiting, chills, abdominal cramps, body aches, muscle and bone pain, muscle spasms, insomnia.
31.  Detoxification Issues ◦ Tolerance decreases rapidly, so overdosing during relapse is easy ◦ Biggest focus during opiate withdrawal is to provide palliative care ◦ In general, opiate withdrawal is not life threatening
32.  Current state of Use/Abuse ◦ Fentanyl is 30-50x stronger than heroin. Overdose rates are ◦ Difficulty getting prescription opioids has led to increases in demand for heroin ◦ Nearly 6% of 12th graders report using narcotics other than heroin for recreational purposes
33.  Class of Drugs: Antianxiety/Depressant ◦ Sedative, hypnotic (sleep-inducing), anxiolytic (anti- anxiety), anticonvulsant, and muscle relaxant properties.  Types of Drugs ◦ Short acting ◦ Long Acting  Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor
34.  Ingestion of therapeutic dosages may be detectable for 1-3 days while extended usage over a period of months or years can extend excretion times up to 4- 6 weeks after cessation of use  Different tests are required to identify different benzos  benzodiazepines such as alprazolam (Xanax®), lorazepam (Ativan®), and clonazepam (Klonopin®) do not share this metabolic pathway
35.  Due to individual differences between people and drugs, a standard therapeutic level is often hard to identify  Many abusers accentuate the effects of benzodiazepines by the using alcohol or other CNS depressants
36.  Short term impact ◦ Drowsiness ◦ Blurred vision ◦ Poor coordination ◦ Amnesia ◦ Hostility/Irritability ◦ Disturbing dreams ◦ Reduced inhibition ◦ Impaired judgment
37.  Short term impact in the elderly ◦ Confusion ◦ The appearance of dementia ◦ Benzodiazepine overdose  Combining with other depressants has an exponential additive effect  Rohypnol is a benzodiazepine
38.  Long term impact ◦ Impairment in several cognitive domains, such as visuospatial ability, speed of processing, and verbal learning J Clin Psychiatry. 2005;66 Suppl 2:9-13. ◦ Benzodiazepine use for 3 months or more was associated with an increased risk of Alzheimer's disease of up to 51%. Benzodiazepine use and risk of Alzheimer’s disease: case-control study BMJ 2014; 349
39.  Symptoms of withdrawal ◦ Sleep disturbance ◦ Irritability, increased tension and anxiety, panic attacks, hand tremor, sweating, palpitations ◦ Difficulty in concentration ◦ Dry heaves and nausea, headache, muscular pain and stiffness ◦ Seizures ◦ Psychosis
40.  Detoxification Issues ◦ Symptoms appear around the end of the half-life period ◦ Rebound anxiety and insomnia peak within a couple of days ◦ Withdrawal symptoms can last for 2-4 weeks depending on the drug ◦ Protracted withdrawal is not uncommon in heavy and/or long-term users.
41.  Detoxification Issues ◦ “A grand mal seizure may occur in as many as 20-30% of individuals undergoing untreated withdrawal from these substances.” Diagnostic and Statistical Manual of Mental Disorders, 5th Ed. ◦ Flumazenil (Romazicon) is a competitive antagonist that can reverse the sedative and overdose effects of benzodiazepines but not of alcohol or other sedative- hypnotics. (SAMHSA TIP 45)
42.  Current state of Use/Abuse  Most frequently used class of drugs for anxiety disorders. An estimated past year prevalence of use in the USA has been reported at 12.9% Archives of Clinical Neuropsychology Volume 19, Issue 3, April 2004, Pages 437–454
43.  GHB (gamma-Hydroxybutyric acid) ◦ Acts on GHB and GABAB Receptors ◦ Some athletes also use GHB, as GHB has been shown to elevate human growth hormone ◦ Date-rape drug
44.  Non-benzodiazepine sleep medications, such as Ambien, Lunesta, and Sonata, have a different chemical structure, but act on some of the same brain receptors as benzodiazepines.  Barbiturates (-barbitals) i.e. phenobarbital are used to reduce anxiety or to help with insomnia. ◦ Readily available in many hospice-involved patients
45.  Inhalants ◦ Types  Paint and paint thinners  Markers  Glues  Shoe polish  Gasoline  Cleaning fluids  Aerosols
46.  Herbs and Supplements ◦ Valerian ◦ Melatonin ◦ Passion Flower ◦ GABA  Muscle relaxants (Flexeril)  Atypical antipsychotics (Seroquel, trazadone)  Mood stabilizers (Depakote)
47. Barbs Candy Downers Phennies Reds Red Birds Sleeping pills Tooies Tranks Yellows Yellow Jackets
48.  Hallucinogens are a class of drugs that cause hallucinations—profound distortions in a person’s perceptions of reality.  Hallucinogens can be found in some plants and mushrooms (or their extracts) or can be man- made  Commonly divided into two broad categories ◦ classic hallucinogens (such as LSD) ◦ dissociative drugs (such as PCP).
49.  Hallucinogens interfere with the action serotonin and/or glutamate, which regulate: ◦ Mood ◦ Sensory perception and response ◦ Sleep ◦ Hunger ◦ Body temperature ◦ Sexual behavior ◦ Muscle control ◦ Pain perception ◦ Learning and memory
50. ◦ PCP (Phencyclidine)—  Also known as ozone, rocket fuel, love boat, hog, embalming fluid, or  Usually sold as a liquid or powder.  PCP can be snorted, smoked, injected, or swallowed.
51.  Ketamine—also known as K, Special K, or cat Valium—is odorless and tasteless and has amnesia-inducing and dissociative properties. (Can facilitate sexual assault.)  DXM (Dextromethorphan)—also known as robo—is a cough suppressant and expectorant  Salvia divinorum—also known as diviner’s sage, Maria Pastora, Sally-D, or magic mint—is a psychoactive plant typically ingested by chewing fresh leaves or by drinking their extracted juices.
52.  LSD (d-lysergic acid diethylamide) ◦ AKA: acid, blotter, doses, hits, microdots, sugar cubes, trips, tabs, or window panes ◦ Potent mood & perception-altering hallucinogenic drugs ◦ It is a clear or white, odorless, water-soluble material ◦ Produced as  Tablets known as “microdots”  Thin squares of gelatin called “window panes.”  Diluted with water or alcohol and sold in liquid form.  LSD-soaked paper punched into small individual squares, known as “blotters.”
53.  Peyote (Mescaline) ◦ Also known as buttons, cactus, and mesc— ◦ Is a small, spineless cactus with mescaline as its main ingredient. ◦ The top, or “crown,” of the peyote cactus has disc- shaped buttons that are cut out, dried, and usually chewed or soaked in water to produce an intoxicating liquid.
54.  The effects of hallucinogens can begin within 20 to 90 minutes and can last as long as 6 to 12 hours.  Other short-term general effects include: • Increased heart rate • Nausea • Intensified feelings and sensory experiences • Changes in sense of time (for example, time passing by slowly) • Increased bp, respiration, or body temperature • Loss of appetite • Dry mouth • Sleep problems • Mixed senses (such as “seeing” sounds or “hearing” colors) • Spiritual experiences • Feelings of relaxation or detachment • Uncoordinated movements • Excessive sweating • Panic • Paranoia—extreme and unreasonable distrust • Psychosis—disordered thinking detached from reality
55.  Repeated use of PCP can result in long-term effects that may continue for a year or more after use stops, such as: ◦ speech problems ◦ memory loss ◦ weight loss ◦ anxiety ◦ depression and suicidal thoughts
56.  Though rare, long-term effects of some hallucinogens include the following: ◦ Persistent psychosis—a series of continuing mental problems, including:  visual disturbances  disorganized thinking  paranoia  mood changes  Flashbacks—recurrences of certain drug experiences. hallucinogen persisting perceptual disorder (HPPD).
57.  Stimulants range from caffeine to methamphetamine and “amp up” the system  Opiates, benzodiazepines, barbiturates, alcohol, inhalants are all CNS depressants  Combinations of depressants have an exponential additive effect  Evaluate patients for exposure to all CNS depressants intentional and incidental  Hallucinogens include LSD, PCP, Peyote, Ketamine and Dextromethorphan  Recent research has indicated that HPPD is not due to “traces of the drug being freed up”

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