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Chemistry and the
     Brain
By Patrick Halks, Jesse Hall and Jordan Hammuck
Chemistryandthe brain
Psychotropic Drugs
   and The Brain
Psychotropic Drugs
        and The Brain
A psychotropic drug is one that targets the central nervous system

The brain acts as the control center sending signals through nerve cells
which transmit messages via neurotransmitters.

Some drugs interfere with this process by changing the amount of
neurotransmitters via agonists which bind to a receptor and enhance
neurotransmitter activity and antagonists which bind to a receptor to
decrease neurotransmitter activity.

The more these drugs are used the higher your tolerance becomes which
results in more of the drug for the same effects.
Chemistryandthe brain
The Blood Brain Barrier
The Blood Brain Barrier

The blood brain barrier are the cells that line the blood vessels of the
brain and are squeezed together to prevent materials from coming in or
out

This barrier makes it difficult to construct a pharmaceutical drug to
help with CNS disorders, because many of these drugs can not pass the
Barrier

Parkinson’s disease is a result of loss of neurons that produce
dopamine, treatment with dopamine is ineffective because it can not
cross the Blood-Brain Barrier.
Chemistryandthe brain
Different types of
 “Brain Drugs”
Different types of
     “Brain Drugs”

Pain Relievers
Depressants
Stimulants
Chemistryandthe brain
Pain Relievers
Pain Relievers


Narcotic- an addictive drug that dulls
your senses and encourages sleep
Nonprescription Pain Relief
Chemistryandthe brain
Narcotics
Narcotics
These drugs are created from a plant
called opium poppy. The main
function is to bind to opiate receptors
which target the body’s pain relievers.


Agonists-bind to receptors and
activate them creating a dream-like
state and pain relief


Antagonists-bind to the receptors
and block the response to opiates,
these are normally used in drug
overdose


Narcotics include
Morphine,OxyContin, and Heroin
Narcotics
These drugs are created from a plant
called opium poppy. The main
function is to bind to opiate receptors
which target the body’s pain relievers.


Agonists-bind to receptors and
activate them creating a dream-like
state and pain relief


Antagonists-bind to the receptors
and block the response to opiates,
these are normally used in drug
overdose


Narcotics include
Morphine,OxyContin, and Heroin
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics

•   Examples include, morphine,
    heroin, Dilaudid, and fentanyl,
    as well as Oxycodone and
    numerous other oral medications
    containing opioid compounds
    and derivatives
•   High potential for addiction
    (habit forming)
     – Can cause withdrawal symptoms
        if stopped abruptly
          • Early Symptoms
               – Agitation, anxiety, muscle aches,
                 increased tearing, insomnia, Rhinorrhea
                  (runny nose), diaphoresis (sweating)
                 , yawning
Side effects of Narcotics

•   Examples include, morphine,
    heroin, Dilaudid, and fentanyl,
    as well as Oxycodone and
    numerous other oral medications
    containing opioid compounds
    and derivatives
•   High potential for addiction
    (habit forming)
     – Can cause withdrawal symptoms
        if stopped abruptly
          • Early Symptoms
               – Agitation, anxiety, muscle aches,
                 increased tearing, insomnia, Rhinorrhea
                  (runny nose), diaphoresis (sweating)
                 , yawning
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics
• Respiratory Depression
  (i.e. hypoventilation,
  hypoxemia, respiratory
  acidosis)!
  – Potentially life-threatening
  – More likely to occur in those
     who haven’t had morphine
    before, as well as in elderly
    or
    debilitated patients
Side effects of Narcotics
• Respiratory Depression
  (i.e. hypoventilation,
  hypoxemia, respiratory
  acidosis)!
  – Potentially life-threatening
  – More likely to occur in those
     who haven’t had morphine
    before, as well as in elderly
    or
    debilitated patients
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics

– Equally, or perhaps more devastating than death, is the common
  phenomenon of anoxic brain injury resulting from respiratory
  depression, whereby the person who (typically overdoses) has a
  long-term depravation of oxygen from their blood supply,
  including that which goes to their brain
   • This results in a myriad of vegetative states or even total brain death
   • Even though these patients are able to be resuscitated, they usually have
     severe limitations in their cognitive and physical functionality, and
     either:
      – Are chronically hospitalized from anywhere from months to years or a period of a few
        years
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics

• Cardiovascular Effects
  – Bradyarrhythmias (slow heart rates leading to aberrant rhythms),
    cardiac arrest, circulatory depression (dangerously low blood
    pressure), hypertension, palpitations, peripheral edema (swelling),
    shock, syncope (passing out), or tachycardia
• Dermatologic Effects
  – Pruritis (itching), rash, recurrent herpes simplex (in someone
    already infected), sweating, urticaria (localized swollen ‘wheals’,
    similar to those induced by a positive PPD, or tuberculin skin test)
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics
• Endocrine/Metabolic Effects
   – Alterations in body temperature
   – Hypogonadism (low testosterone or gonadotropin and libido)
• Gastrointestinal effects
   – Abdominal pain
   – Biliary Colic (caused by contraction of the sphincter of Oddi – controlling the flow of
     bile into the duodenum)
   – Constipation
        • This can cause something called parylitic ileus, whereby GI motility ceases, and this can lead to
          bowel ischemia, which can be quite deadly
   –   Diarrhea
   –   Loss of appetite
   –   Nausea and vomiting
   –   Xerostomia (dry mouth)
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics

• Hematologic effects
  – In patients with Sickle Cell Disease, sickle-cell ‘crisis’ may
    ensue
• Hepatic effects
  – Liver toxicity
  – Abnormal liver function tests
• Immunologic effects
  – Anaphylaxis (leading to anaphylactic shock)
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics
•   Musculoskeletal effects
     – Backache
     – Myoclonus (brief, shock-like jerking)
•   Neurologic effects
     –   Asthenia (lack of strength / muscular control)
     –   Confusion & dizziness
     –   Increased intracranial pressure
     –   Headache
     –   Insomnia
     –   Lightheadedness
     –   Meniere’s Disease (lead to motion sickness & migraines)
     –   Paresthesia (lack of sensation)
     –   Unwanted sedation
     –   Seizure
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics
• Opthalmic effects
  – Amblyopia (lazy eye)
  – Miosis (pupillary constriction)
• Psychiatric effects
  – Anxiety
  – Capgras’ Syndrome (delusion of family-imposter conspiracy
    against the patient)
  – Delirium
  – Dysphoric / Euphoric mood
  – Hallucinations & Psychotic disorder
Chemistryandthe brain
Side effects of Narcotics
Side effects of Narcotics

• Renal effects
   – Nephrotoxicity
   – Urinary retention
• Reproductive effects!
   – sexual dysfunction
   – Withdrawal symptoms in the newborn
• Respiratory effects (besides respiratory depression)
   – Pulmonary edema
   – Irregular breathing
   – Cough suppression
Chemistryandthe brain
Side effects FYI
Side effects FYI
•   Opioid Strength comparison
•   Done in relation of various pain medicine’s strength to that of morphine, i.e., 1mg morphine = 1
    ‘standard unit’
•   Just a few comparisons follow, with most commonly prescribed / abused drugs discussed
•   1mg oral morphine is equivalent to…
     – 100mg codeine or Tramadol
     – 20mg methadone
     – 16.67mg hydrocodone
•   These medications in 1mg dosages are equivalent to the specified dosage of oral morphine
     – 1mg oxycodone = 5-6mg morphine
     – IV morphine = 2.5mg oral morphine
     – Heroin = 2.25mg morphine
     – Hydromorphone (dilaudid) = 2mg morphine
•   Fentanyl, a commonly used pain medicine within the intensive care / hospital environment is
    50-100 times stronger than morphine, and is given in dosages of micrograms/hour!
Chemistryandthe brain
Nonprescription Pain
      Relief
Nonprescription Pain
       Relief
Aspirin-salicylic acid, belongs to a group known as non-steroid anti-
inflammatory drugs (NSAIDs). In this group is also ibuprofen, Advil,
and Motrin

These drugs inhibit synthesis of prostaglandins, or the chemical
messengers that mediate pain, blood clotting, fever and inflammation.

Tylenol- acetaminophen, is a pain and fever reducer that lacks any
anti-inflammatory benefit.
Chemistryandthe brain
Side effects of OTC
Side effects of OTC
• NSAIDS (non-steroidal anti-inflammatory drugs):
  targeting the COX-1 enzyme
  – Include: aspirin, ibuprofen
  – Cox-2 inhibitors
       • Vioxx
• Aspirin (NSA)
  –   Gastrointestinal ulceration and bleeding
  –   Tinnitus (persistent ringing in ears)
  –   Bronchospasm
  –   Angioedema, Reye’s syndrome (usually in children with existing
      viral illnesses)
Chemistryandthe brain
Side effects of OTC
Side effects of OTC

• Ibuprofen
  – (relatively) Common adverse effects (many these only reported
    with IV/intramuscular administration)
     • Hypotension (mild)
     • Rash
     • Hypernatremia, hypoalbuminemia, hypoproteinemia (high blood sodium
       and low blood protein respectively)
     • Heartburn, nausea / vomiting, flatulence
     • Thrombocytosis (elevated platelet levels)
     • Dizziness, headache
     • Urinary retention and elevated blood urea nitrogen
Chemistryandthe brain
Side effects of OTC
Side effects of OTC

• Ibuprofen
   – Serious effects (except for neutropenia, all < or = to 1% chance)
      •   Congestive heart failure, hypertension, heart attack
      •   Stevens-Johnson syndrome, toxic epidermal necrolysis
      •   Gastrointestinal ulceration, perforation, and hemorrhage
      •   Pancreatitis
      •   Anemia, neutropenia (low white blood cell counts), thrombocytopenia
      •   Hepatitis, jaundice, and liver failure
      •   Anaphylactic shock
      •   CVA, aseptic meningitis
      •   Amblyopia
      •   Hearing loss
      •   Depression
Chemistryandthe brain
Side effects of OTC
Side effects of OTC

• Acetaminophen (Tylenol)
  – Common
     •   Pruritis
     •   Constipation, nausea / vomiting
     •   Headache
     •   Agitation
     •   Atelectasis (partial closure / closing of pulmonary alveoli)
  – Serious
     • Stevens-Johnson Syndrome & Toxic epidermal necrolysis
           – Two very similar diseases involving progressive decay and sloughing off of skin tissue.
             This can involve anywhere from 50% to 100% of a patients’ skin. Quite rare, but can result
             in death.
Chemistryandthe brain
Depressants
Depressants
Depressants- Slow physical
and mental activity,
producing relaxation

Barbiturates-Induce
sedation

Benzodiazepines- treat
insomnia, anxiety and
panic disorders
Depressants
Depressants- Slow physical
and mental activity,
producing relaxation

Barbiturates-Induce
sedation

Benzodiazepines- treat
insomnia, anxiety and
panic disorders
Chemistryandthe brain
Barbituates/
Benzodiapines
(depressants)
Barbituates/
Benzodiapines
(depressants)
   Tranquilizers- reduce
   anxiety, while increasing
   GABA (the
   neurotransmitter that
   normally counteracts the
   signals that cause fear and
   anxiety)
Barbituates/
Benzodiapines
(depressants)
   Tranquilizers- reduce
   anxiety, while increasing
   GABA (the
   neurotransmitter that
   normally counteracts the
   signals that cause fear and
   anxiety)
Chemistryandthe brain
Side effects of
 Depressants
Side effects of
               Depressants
• Including: Barbiturates & Benzodiazepines
• Barbiturates
  – Modern use is almost solely for suppression or prevention of
    seizures
  – Include: phenobarbital, phenytoin (Dilantin), phosphenytoin,
    levetiracetam, and Gabapentin
Chemistryandthe brain
Side effects of
 Depressants
Side effects of
                     Depressants
• Barbiturate side effects include
   – Somnolence, ataxia (inappropriate gait), dizziness, headache, insomnia,
     paresthesia, slurred speech, nystagmus (‘typewriter-like’ gaze)
   – Syncope, drug-induced coma
   – Osteomalacia (abnormal bone weakness)
   – Anemia, leukopenia, thrombocytopenia
   – Dermatologic alterations, rash, eczema, Stevens-Johnson syndrome, toxic
     epidermal necrolysis
   – Liver damage
   – Immune hypersensitivity reaction
   – Hallucinations, confusion, nervousness, hostile behavior, suicidal ideation
Chemistryandthe brain
Side effects of
 Depressants
Side effects of
               Depressants
• Benzodiazepines include…
  – Valium (diazepam)
  – Ativan (lorazepam)
  – Versed (midazolam)
  – Xanax (alprazolam)
  – Klonopin (Clonazepam)
  – Also including date-rape drugs such as rohypnol, GHB, and
    Ketamine
  – Side effects are very similar for all of these
Chemistryandthe brain
Side effects of
 Depressants
Side effects of
                       Depressants
• Benzodiazepine side effects ( much more dangerous when
  combined with other drugs acting on the brain & CNS)
  – With high doses, Central nervous system depression potentially
    leads to…
     •   Respiratory depression / arrest
     •   Coma
     •   Hypotension
     •   Hypothermia
     •   Rhabdomyolysis (condition in which Fe / Iron is released from
         intracellular fluid / tissues into bloodstream, causing acute renal failure
         when becoming clogged in the kidneys’ circulation
Chemistryandthe brain
Side effects of
 Depressants
Side effects of
                      Depressants
• Benzodiazepine side effects also include (at ‘therapeutic doses’)
   – Nystagmus, tachycardia, bradycardia, hypotension
   – Decreased respiratory rate (sometimes good!)
   – Drowsiness, slurred speech, dyskinesia (jittery movement), disorientation
   – Nausea / vomiting
   – Teratogenic effects (cause fetal abnormalities & spontaneous abortion)
   – Habit forming / addictive, leading to withdrawal
• Benzos’ are relied on heavily within the context of ICU and OR patient care, for
  their calming action, but also for their side effect of memory loss, which is a good
  thing for many ICU patients!
Chemistryandthe brain
Stimulants and side
      effects
Stimulants and side
•
                                         effects
    Include cocaine (and derivatives such as crack)
    and amphetamines (such as Methamphetamine)


•   Side effects of cocaine include…


     –   Delusions of grandeur, euphoria, emotional instability,
          insomnia & restlessness, hallucinations, mania and paranoid
         psychosis


     –   Dilated pupils, headache, vertigo / dizziness, loss of
         consciousness, seizures


     –   Nausea / vomiting


     –   Nasal septal defects (from snorting)


     –   Chronic bronchitis, coughing, pulmonary edema, respiratory
         failure and death (esp. with crack)


     –   Chest pain, tachycardia, cardiomyopathy, aortic rupture /
         dissection, myocardial infarction, cardiac arryhthmias,
         palpitations
Stimulants and side
•
                                         effects
    Include cocaine (and derivatives such as crack)
    and amphetamines (such as Methamphetamine)


•   Side effects of cocaine include…


     –   Delusions of grandeur, euphoria, emotional instability,
          insomnia & restlessness, hallucinations, mania and paranoid
         psychosis


     –   Dilated pupils, headache, vertigo / dizziness, loss of
         consciousness, seizures


     –   Nausea / vomiting


     –   Nasal septal defects (from snorting)


     –   Chronic bronchitis, coughing, pulmonary edema, respiratory
         failure and death (esp. with crack)


     –   Chest pain, tachycardia, cardiomyopathy, aortic rupture /
         dissection, myocardial infarction, cardiac arryhthmias,
         palpitations
Stimulants and side
•
                                         effects
    Include cocaine (and derivatives such as crack)
    and amphetamines (such as Methamphetamine)


•   Side effects of cocaine include…


     –   Delusions of grandeur, euphoria, emotional instability,
          insomnia & restlessness, hallucinations, mania and paranoid
         psychosis


     –   Dilated pupils, headache, vertigo / dizziness, loss of
         consciousness, seizures


     –   Nausea / vomiting


     –   Nasal septal defects (from snorting)


     –   Chronic bronchitis, coughing, pulmonary edema, respiratory
         failure and death (esp. with crack)


     –   Chest pain, tachycardia, cardiomyopathy, aortic rupture /
         dissection, myocardial infarction, cardiac arryhthmias,
         palpitations
Chemistryandthe brain
• Amphetamine side effects include…
   – Hypertension, tachycardia, heart failure, aortic dissection, heart attack,
     angina, cardiac arrest
   – Tachypnea, pulmonary hypertension, pulmonary edema, Acute Respiratory
     Distress Syndrome
   – Seizures, coma
   – Agitation, paranoia, delusions, hyperactivity, severe psychosis (acute or
     chronic)
   – Hyperthermia, rhabdomyolysis, coma, metabolic acidosis
   – Renal failure, hepatic injury, coagulopathy, renal tubular necrosis
   – Vomiting, diarrhea, gastrointestinal bleeding
   – Fetal abnormalities & spontaneous abortion (& can be passed via breast milk)
Stimulants and side
                effects
• Amphetamine side effects include…
   – Hypertension, tachycardia, heart failure, aortic dissection, heart attack,
     angina, cardiac arrest
   – Tachypnea, pulmonary hypertension, pulmonary edema, Acute Respiratory
     Distress Syndrome
   – Seizures, coma
   – Agitation, paranoia, delusions, hyperactivity, severe psychosis (acute or
     chronic)
   – Hyperthermia, rhabdomyolysis, coma, metabolic acidosis
   – Renal failure, hepatic injury, coagulopathy, renal tubular necrosis
   – Vomiting, diarrhea, gastrointestinal bleeding
   – Fetal abnormalities & spontaneous abortion (& can be passed via breast milk)
References
•
                                References
    Barbiturate retrieved from Wikipedia, April 10th, 2011 from http://en.wikipedia.org/wiki/Barbiturate
•   EMedicineHealth, retrieved April 9th, 2011 from http://www.emedicinehealth.com/cocaine_abuse/
    page3_em.htm#Cocaine Abuse Symptoms
•   Medline Plus, National Institutes of Health & National Library of Medicine Database. Retrieved April
    9th, 2011. Available from http://www.nlm.nih.gov/medlineplus/ency/article/000949.htm
•   Micromedex 2.0, available via Shands.org ‘VPN’ network from Shands Teaching Hospitals and
    Clinics @ The University of Florida (available to employees only). Retrieved April 10th, 2011 from
    https://vpn.shands.org/micromedex2/librarian/ND_T/evidencexpert/ND_PR/evidencexpert/CS/
    A5B79F/ND_AppProduct/evidencexpert/DUPLICATIONSHIELDSYNC/35310D/ND_PG/
    evidencexpert/ND_B/evidencexpert/ND_P/evidencexpert/
    PFActionId/,DanaInfo=.awxyCxmut0xxsoMq32+pf.HomePage
•   Opioid Comparison, retrieved April 9th, 2011 from http://en.wikipedia.org/wiki/Opioid_comparison
    Millard, J.; Adventures in Chemistry; Houghton Mifflin: 2008; pp. 356-68.Tough, P.; “The
    Alchemy of OxyContin: From Pain Relief to Drug Addiction,” The New York Times Magazine; July
    29, 2001.
    “OxyContin,” Wikipedia. http://en.wikipedia.org/wiki/ Oxycontin (accessed 10 Apr 2011).

•   “Alprazolam,” Wikipedia. http://en.wikipedia.org/wiki/Xanax (accessed 10 Apr 2011).
    “Cocaine,” Wikipedia. http://en.wikipedia.org/wiki/Cocaine (accessed 10 Apr 2011).
    Brieter, H.C., et al.; “Acute Effects of Cocaine on Human Brain Activity and Emotion,” Neuron, vol.
    19, no. 3; September 1997; pp. 591-611.

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Chemistryandthe brain

  • 1. Chemistry and the Brain By Patrick Halks, Jesse Hall and Jordan Hammuck
  • 3. Psychotropic Drugs and The Brain
  • 4. Psychotropic Drugs and The Brain A psychotropic drug is one that targets the central nervous system The brain acts as the control center sending signals through nerve cells which transmit messages via neurotransmitters. Some drugs interfere with this process by changing the amount of neurotransmitters via agonists which bind to a receptor and enhance neurotransmitter activity and antagonists which bind to a receptor to decrease neurotransmitter activity. The more these drugs are used the higher your tolerance becomes which results in more of the drug for the same effects.
  • 6. The Blood Brain Barrier
  • 7. The Blood Brain Barrier The blood brain barrier are the cells that line the blood vessels of the brain and are squeezed together to prevent materials from coming in or out This barrier makes it difficult to construct a pharmaceutical drug to help with CNS disorders, because many of these drugs can not pass the Barrier Parkinson’s disease is a result of loss of neurons that produce dopamine, treatment with dopamine is ineffective because it can not cross the Blood-Brain Barrier.
  • 9. Different types of “Brain Drugs”
  • 10. Different types of “Brain Drugs” Pain Relievers Depressants Stimulants
  • 13. Pain Relievers Narcotic- an addictive drug that dulls your senses and encourages sleep Nonprescription Pain Relief
  • 16. Narcotics These drugs are created from a plant called opium poppy. The main function is to bind to opiate receptors which target the body’s pain relievers. Agonists-bind to receptors and activate them creating a dream-like state and pain relief Antagonists-bind to the receptors and block the response to opiates, these are normally used in drug overdose Narcotics include Morphine,OxyContin, and Heroin
  • 17. Narcotics These drugs are created from a plant called opium poppy. The main function is to bind to opiate receptors which target the body’s pain relievers. Agonists-bind to receptors and activate them creating a dream-like state and pain relief Antagonists-bind to the receptors and block the response to opiates, these are normally used in drug overdose Narcotics include Morphine,OxyContin, and Heroin
  • 19. Side effects of Narcotics
  • 20. Side effects of Narcotics • Examples include, morphine, heroin, Dilaudid, and fentanyl, as well as Oxycodone and numerous other oral medications containing opioid compounds and derivatives • High potential for addiction (habit forming) – Can cause withdrawal symptoms if stopped abruptly • Early Symptoms – Agitation, anxiety, muscle aches, increased tearing, insomnia, Rhinorrhea (runny nose), diaphoresis (sweating) , yawning
  • 21. Side effects of Narcotics • Examples include, morphine, heroin, Dilaudid, and fentanyl, as well as Oxycodone and numerous other oral medications containing opioid compounds and derivatives • High potential for addiction (habit forming) – Can cause withdrawal symptoms if stopped abruptly • Early Symptoms – Agitation, anxiety, muscle aches, increased tearing, insomnia, Rhinorrhea (runny nose), diaphoresis (sweating) , yawning
  • 23. Side effects of Narcotics
  • 24. Side effects of Narcotics • Respiratory Depression (i.e. hypoventilation, hypoxemia, respiratory acidosis)! – Potentially life-threatening – More likely to occur in those who haven’t had morphine before, as well as in elderly or debilitated patients
  • 25. Side effects of Narcotics • Respiratory Depression (i.e. hypoventilation, hypoxemia, respiratory acidosis)! – Potentially life-threatening – More likely to occur in those who haven’t had morphine before, as well as in elderly or debilitated patients
  • 27. Side effects of Narcotics
  • 28. Side effects of Narcotics – Equally, or perhaps more devastating than death, is the common phenomenon of anoxic brain injury resulting from respiratory depression, whereby the person who (typically overdoses) has a long-term depravation of oxygen from their blood supply, including that which goes to their brain • This results in a myriad of vegetative states or even total brain death • Even though these patients are able to be resuscitated, they usually have severe limitations in their cognitive and physical functionality, and either: – Are chronically hospitalized from anywhere from months to years or a period of a few years
  • 30. Side effects of Narcotics
  • 31. Side effects of Narcotics • Cardiovascular Effects – Bradyarrhythmias (slow heart rates leading to aberrant rhythms), cardiac arrest, circulatory depression (dangerously low blood pressure), hypertension, palpitations, peripheral edema (swelling), shock, syncope (passing out), or tachycardia • Dermatologic Effects – Pruritis (itching), rash, recurrent herpes simplex (in someone already infected), sweating, urticaria (localized swollen ‘wheals’, similar to those induced by a positive PPD, or tuberculin skin test)
  • 33. Side effects of Narcotics
  • 34. Side effects of Narcotics • Endocrine/Metabolic Effects – Alterations in body temperature – Hypogonadism (low testosterone or gonadotropin and libido) • Gastrointestinal effects – Abdominal pain – Biliary Colic (caused by contraction of the sphincter of Oddi – controlling the flow of bile into the duodenum) – Constipation • This can cause something called parylitic ileus, whereby GI motility ceases, and this can lead to bowel ischemia, which can be quite deadly – Diarrhea – Loss of appetite – Nausea and vomiting – Xerostomia (dry mouth)
  • 36. Side effects of Narcotics
  • 37. Side effects of Narcotics • Hematologic effects – In patients with Sickle Cell Disease, sickle-cell ‘crisis’ may ensue • Hepatic effects – Liver toxicity – Abnormal liver function tests • Immunologic effects – Anaphylaxis (leading to anaphylactic shock)
  • 39. Side effects of Narcotics
  • 40. Side effects of Narcotics • Musculoskeletal effects – Backache – Myoclonus (brief, shock-like jerking) • Neurologic effects – Asthenia (lack of strength / muscular control) – Confusion & dizziness – Increased intracranial pressure – Headache – Insomnia – Lightheadedness – Meniere’s Disease (lead to motion sickness & migraines) – Paresthesia (lack of sensation) – Unwanted sedation – Seizure
  • 42. Side effects of Narcotics
  • 43. Side effects of Narcotics • Opthalmic effects – Amblyopia (lazy eye) – Miosis (pupillary constriction) • Psychiatric effects – Anxiety – Capgras’ Syndrome (delusion of family-imposter conspiracy against the patient) – Delirium – Dysphoric / Euphoric mood – Hallucinations & Psychotic disorder
  • 45. Side effects of Narcotics
  • 46. Side effects of Narcotics • Renal effects – Nephrotoxicity – Urinary retention • Reproductive effects! – sexual dysfunction – Withdrawal symptoms in the newborn • Respiratory effects (besides respiratory depression) – Pulmonary edema – Irregular breathing – Cough suppression
  • 49. Side effects FYI • Opioid Strength comparison • Done in relation of various pain medicine’s strength to that of morphine, i.e., 1mg morphine = 1 ‘standard unit’ • Just a few comparisons follow, with most commonly prescribed / abused drugs discussed • 1mg oral morphine is equivalent to… – 100mg codeine or Tramadol – 20mg methadone – 16.67mg hydrocodone • These medications in 1mg dosages are equivalent to the specified dosage of oral morphine – 1mg oxycodone = 5-6mg morphine – IV morphine = 2.5mg oral morphine – Heroin = 2.25mg morphine – Hydromorphone (dilaudid) = 2mg morphine • Fentanyl, a commonly used pain medicine within the intensive care / hospital environment is 50-100 times stronger than morphine, and is given in dosages of micrograms/hour!
  • 52. Nonprescription Pain Relief Aspirin-salicylic acid, belongs to a group known as non-steroid anti- inflammatory drugs (NSAIDs). In this group is also ibuprofen, Advil, and Motrin These drugs inhibit synthesis of prostaglandins, or the chemical messengers that mediate pain, blood clotting, fever and inflammation. Tylenol- acetaminophen, is a pain and fever reducer that lacks any anti-inflammatory benefit.
  • 55. Side effects of OTC • NSAIDS (non-steroidal anti-inflammatory drugs): targeting the COX-1 enzyme – Include: aspirin, ibuprofen – Cox-2 inhibitors • Vioxx • Aspirin (NSA) – Gastrointestinal ulceration and bleeding – Tinnitus (persistent ringing in ears) – Bronchospasm – Angioedema, Reye’s syndrome (usually in children with existing viral illnesses)
  • 58. Side effects of OTC • Ibuprofen – (relatively) Common adverse effects (many these only reported with IV/intramuscular administration) • Hypotension (mild) • Rash • Hypernatremia, hypoalbuminemia, hypoproteinemia (high blood sodium and low blood protein respectively) • Heartburn, nausea / vomiting, flatulence • Thrombocytosis (elevated platelet levels) • Dizziness, headache • Urinary retention and elevated blood urea nitrogen
  • 61. Side effects of OTC • Ibuprofen – Serious effects (except for neutropenia, all < or = to 1% chance) • Congestive heart failure, hypertension, heart attack • Stevens-Johnson syndrome, toxic epidermal necrolysis • Gastrointestinal ulceration, perforation, and hemorrhage • Pancreatitis • Anemia, neutropenia (low white blood cell counts), thrombocytopenia • Hepatitis, jaundice, and liver failure • Anaphylactic shock • CVA, aseptic meningitis • Amblyopia • Hearing loss • Depression
  • 64. Side effects of OTC • Acetaminophen (Tylenol) – Common • Pruritis • Constipation, nausea / vomiting • Headache • Agitation • Atelectasis (partial closure / closing of pulmonary alveoli) – Serious • Stevens-Johnson Syndrome & Toxic epidermal necrolysis – Two very similar diseases involving progressive decay and sloughing off of skin tissue. This can involve anywhere from 50% to 100% of a patients’ skin. Quite rare, but can result in death.
  • 67. Depressants Depressants- Slow physical and mental activity, producing relaxation Barbiturates-Induce sedation Benzodiazepines- treat insomnia, anxiety and panic disorders
  • 68. Depressants Depressants- Slow physical and mental activity, producing relaxation Barbiturates-Induce sedation Benzodiazepines- treat insomnia, anxiety and panic disorders
  • 71. Barbituates/ Benzodiapines (depressants) Tranquilizers- reduce anxiety, while increasing GABA (the neurotransmitter that normally counteracts the signals that cause fear and anxiety)
  • 72. Barbituates/ Benzodiapines (depressants) Tranquilizers- reduce anxiety, while increasing GABA (the neurotransmitter that normally counteracts the signals that cause fear and anxiety)
  • 74. Side effects of Depressants
  • 75. Side effects of Depressants • Including: Barbiturates & Benzodiazepines • Barbiturates – Modern use is almost solely for suppression or prevention of seizures – Include: phenobarbital, phenytoin (Dilantin), phosphenytoin, levetiracetam, and Gabapentin
  • 77. Side effects of Depressants
  • 78. Side effects of Depressants • Barbiturate side effects include – Somnolence, ataxia (inappropriate gait), dizziness, headache, insomnia, paresthesia, slurred speech, nystagmus (‘typewriter-like’ gaze) – Syncope, drug-induced coma – Osteomalacia (abnormal bone weakness) – Anemia, leukopenia, thrombocytopenia – Dermatologic alterations, rash, eczema, Stevens-Johnson syndrome, toxic epidermal necrolysis – Liver damage – Immune hypersensitivity reaction – Hallucinations, confusion, nervousness, hostile behavior, suicidal ideation
  • 80. Side effects of Depressants
  • 81. Side effects of Depressants • Benzodiazepines include… – Valium (diazepam) – Ativan (lorazepam) – Versed (midazolam) – Xanax (alprazolam) – Klonopin (Clonazepam) – Also including date-rape drugs such as rohypnol, GHB, and Ketamine – Side effects are very similar for all of these
  • 83. Side effects of Depressants
  • 84. Side effects of Depressants • Benzodiazepine side effects ( much more dangerous when combined with other drugs acting on the brain & CNS) – With high doses, Central nervous system depression potentially leads to… • Respiratory depression / arrest • Coma • Hypotension • Hypothermia • Rhabdomyolysis (condition in which Fe / Iron is released from intracellular fluid / tissues into bloodstream, causing acute renal failure when becoming clogged in the kidneys’ circulation
  • 86. Side effects of Depressants
  • 87. Side effects of Depressants • Benzodiazepine side effects also include (at ‘therapeutic doses’) – Nystagmus, tachycardia, bradycardia, hypotension – Decreased respiratory rate (sometimes good!) – Drowsiness, slurred speech, dyskinesia (jittery movement), disorientation – Nausea / vomiting – Teratogenic effects (cause fetal abnormalities & spontaneous abortion) – Habit forming / addictive, leading to withdrawal • Benzos’ are relied on heavily within the context of ICU and OR patient care, for their calming action, but also for their side effect of memory loss, which is a good thing for many ICU patients!
  • 90. Stimulants and side • effects Include cocaine (and derivatives such as crack) and amphetamines (such as Methamphetamine) • Side effects of cocaine include… – Delusions of grandeur, euphoria, emotional instability, insomnia & restlessness, hallucinations, mania and paranoid psychosis – Dilated pupils, headache, vertigo / dizziness, loss of consciousness, seizures – Nausea / vomiting – Nasal septal defects (from snorting) – Chronic bronchitis, coughing, pulmonary edema, respiratory failure and death (esp. with crack) – Chest pain, tachycardia, cardiomyopathy, aortic rupture / dissection, myocardial infarction, cardiac arryhthmias, palpitations
  • 91. Stimulants and side • effects Include cocaine (and derivatives such as crack) and amphetamines (such as Methamphetamine) • Side effects of cocaine include… – Delusions of grandeur, euphoria, emotional instability, insomnia & restlessness, hallucinations, mania and paranoid psychosis – Dilated pupils, headache, vertigo / dizziness, loss of consciousness, seizures – Nausea / vomiting – Nasal septal defects (from snorting) – Chronic bronchitis, coughing, pulmonary edema, respiratory failure and death (esp. with crack) – Chest pain, tachycardia, cardiomyopathy, aortic rupture / dissection, myocardial infarction, cardiac arryhthmias, palpitations
  • 92. Stimulants and side • effects Include cocaine (and derivatives such as crack) and amphetamines (such as Methamphetamine) • Side effects of cocaine include… – Delusions of grandeur, euphoria, emotional instability, insomnia & restlessness, hallucinations, mania and paranoid psychosis – Dilated pupils, headache, vertigo / dizziness, loss of consciousness, seizures – Nausea / vomiting – Nasal septal defects (from snorting) – Chronic bronchitis, coughing, pulmonary edema, respiratory failure and death (esp. with crack) – Chest pain, tachycardia, cardiomyopathy, aortic rupture / dissection, myocardial infarction, cardiac arryhthmias, palpitations
  • 94. • Amphetamine side effects include… – Hypertension, tachycardia, heart failure, aortic dissection, heart attack, angina, cardiac arrest – Tachypnea, pulmonary hypertension, pulmonary edema, Acute Respiratory Distress Syndrome – Seizures, coma – Agitation, paranoia, delusions, hyperactivity, severe psychosis (acute or chronic) – Hyperthermia, rhabdomyolysis, coma, metabolic acidosis – Renal failure, hepatic injury, coagulopathy, renal tubular necrosis – Vomiting, diarrhea, gastrointestinal bleeding – Fetal abnormalities & spontaneous abortion (& can be passed via breast milk)
  • 95. Stimulants and side effects • Amphetamine side effects include… – Hypertension, tachycardia, heart failure, aortic dissection, heart attack, angina, cardiac arrest – Tachypnea, pulmonary hypertension, pulmonary edema, Acute Respiratory Distress Syndrome – Seizures, coma – Agitation, paranoia, delusions, hyperactivity, severe psychosis (acute or chronic) – Hyperthermia, rhabdomyolysis, coma, metabolic acidosis – Renal failure, hepatic injury, coagulopathy, renal tubular necrosis – Vomiting, diarrhea, gastrointestinal bleeding – Fetal abnormalities & spontaneous abortion (& can be passed via breast milk)
  • 97. References Barbiturate retrieved from Wikipedia, April 10th, 2011 from http://en.wikipedia.org/wiki/Barbiturate • EMedicineHealth, retrieved April 9th, 2011 from http://www.emedicinehealth.com/cocaine_abuse/ page3_em.htm#Cocaine Abuse Symptoms • Medline Plus, National Institutes of Health & National Library of Medicine Database. Retrieved April 9th, 2011. Available from http://www.nlm.nih.gov/medlineplus/ency/article/000949.htm • Micromedex 2.0, available via Shands.org ‘VPN’ network from Shands Teaching Hospitals and Clinics @ The University of Florida (available to employees only). Retrieved April 10th, 2011 from https://vpn.shands.org/micromedex2/librarian/ND_T/evidencexpert/ND_PR/evidencexpert/CS/ A5B79F/ND_AppProduct/evidencexpert/DUPLICATIONSHIELDSYNC/35310D/ND_PG/ evidencexpert/ND_B/evidencexpert/ND_P/evidencexpert/ PFActionId/,DanaInfo=.awxyCxmut0xxsoMq32+pf.HomePage • Opioid Comparison, retrieved April 9th, 2011 from http://en.wikipedia.org/wiki/Opioid_comparison Millard, J.; Adventures in Chemistry; Houghton Mifflin: 2008; pp. 356-68.Tough, P.; “The Alchemy of OxyContin: From Pain Relief to Drug Addiction,” The New York Times Magazine; July 29, 2001. “OxyContin,” Wikipedia. http://en.wikipedia.org/wiki/ Oxycontin (accessed 10 Apr 2011). • “Alprazolam,” Wikipedia. http://en.wikipedia.org/wiki/Xanax (accessed 10 Apr 2011). “Cocaine,” Wikipedia. http://en.wikipedia.org/wiki/Cocaine (accessed 10 Apr 2011). Brieter, H.C., et al.; “Acute Effects of Cocaine on Human Brain Activity and Emotion,” Neuron, vol. 19, no. 3; September 1997; pp. 591-611.

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