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Core Concepts in Pharmacology Second Edition

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Nonbenzodiazepine CNS depressants - zalepon (Sonata), zolpidem (Ambien) ... Zaleplon (Sonata) - insomnia. Zolpidem (Ambien) Drugs for Emotional and Mood Disorders ... – PowerPoint PPT presentation

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Title: Core Concepts in Pharmacology Second Edition


1
Drugs for Anxiety and Insomnia
2
Factors that Contribute to Anxiety
  • Stressful environment events
  • Abnormal fear of a specific situation or object
  • Reexperiencing a traumatic life event

3
Nonpharmacological Therapies to Cope with Anxiety
  • Behavioral therapy
  • Biofeedback techniques
  • Meditation

4
CNS Agents Used to Treat Anxiety and Sleep
Disorders
  • Antidepressants
  • Benzodiazepines
  • Barbiturates
  • Nonbarbiturates and nonbenzodiazepines

5
Three Types of Antidepressants
  • Selective serotonin-reuptake inhibitors (SSRIs)
  • Tricyclic antidepressants (TCAs)
  • Monoamine oxidase inhibitors (MAOIs)

6
Benzodiazepines
  • Short-term treatment of anxiety and sleep
    disorders
  • Excessive amounts do not produce
  • Respiratory depression
  • Coma

7
Barbiturates - Schedule II Drugs
  • Rarely used for anxiety or sleep disorders
  • Significant side effects
  • High risk of psychological and physiological
    dependence

8
Nonbenzodiazepines and Nonbarbiturates
  • Anxiety disorders
  • Antiseizure medication - valproate (Depakote)
  • CNS depressant - buspirone (Buspar)
  • Beta blockers - atenolol (Inderal), propanolol
    (Tenormin)
  • Insomnia
  • Nonbenzodiazepine CNS depressants - zalepon
    (Sonata), zolpidem (Ambien)
  • Antihistamines - diphenhydramine (Benadryl),
    hydroxyzine (Vistaril)

9
CNS Depressants
  • Slow neuronal activity in the brain
  • Low doses cause relaxation to sedation
  • High doses cause sleep to anesthesia

10
Antidepressants
  • Tricyclic antidepressants - TCAs
  • Amitriptyline (Elavil) - depression
  • Imipramine (Tofranil) - depression, generalized
    anxiety
  • Monoamine oxidase inhibitors - MAOIs
  • Phenelzine (Nardil) - social anxiety, depression
  • Tranylcypromine (Parnate) - depression

11
Antidepressants (contd)
  • Selective serotonin reuptake inhibitors - SSRIs
  • Fluoxetine (Prozac) - depression, panic, social
    anxiety
  • Paroxetine (Paxil) - depression, panic, social
    anxiety
  • Atypical antidepressants
  • Trazodone (Desyrel) - depression, generalized
    anxiety
  • Venlafaxine (Effexor) - depression, social
    anxiety, generalized anxiety

12
Benzodiazepines
  • Panic disorders
  • Alprazolam (Xanax) - generalized anxiety,
    phobias, social anxiety
  • Anxiety
  • Diazepam (Valium) - panic
  • Oxazepam (Serax) - phobias
  • Insomnia
  • Estazolam (Prosom)
  • Flurazepam (Dalmane)
  • Triazolam (Halcion)

13
Barbiturates for Sedation and Insomnia
  • Short acting
  • Pentobarbital sodium (Nembutal)
  • Secobarbital (Seconal)
  • Intermediate acting
  • Amobarbital (Amytal)
  • Butabarbital sodium (Butisol)
  • Long acting
  • Mephobarbital (Mebaral)
  • Phenobarbital (Luminal)

14
Nonbenzodiazepines, Nonbarbiturates, CNS
Depressants
  • Antiseizure medication
  • Valproate (Depakote) - panic
  • CNS depressants (mild tranquilizers)
  • Buspirone (BuSpar) - generalized anxiety, OCD
  • Beta blockers
  • Atenolol (Tenormin) - performance anxiety, social
    anxiety
  • Nonbenzodiazepines
  • Zaleplon (Sonata) - insomnia
  • Zolpidem (Ambien)

15
Drugs for Emotional and Mood Disorders
16
Categories of Mood Disorders
  • Depression
  • Bipolar disorder

17
Antidepressants Combat Depression
  • Enhance mood
  • Boost neurotransmitters
  • Norepinephrine
  • Serotonin
  • Four primary classes
  • Tricyclic antidepressants (TCAs)
  • Selective serotonin reuptake inhibitors (SSRIs)
  • Monoamine oxidase inhibitors (MAOIs)
  • Atypical antidepressants

18
Several Drugs May Be Used to Manage Bipolar
Disorder
  • Mood stabilizers to manage manic phase
  • Some antiseizure drugs to stabilize mood
  • TCAs and atypical antidepressants used during
    depressive stage
  • Benzodiazepines during manic phase to moderate
    manic symptoms
  • Antipsychotic agents used for extreme agitation,
    delusions, or hallucinations

19
To Manage Attention Deficit-Hyperactivity
Disorder (ADHD)
  • CNS stimulants are drug of choice
  • Non-CNS stimulants less effective
  • Atypical antidepressants and TCAs
  • Second choice drugs
  • When CNS stimulants fail
  • When CNS stimulants are contraindicated

20
Symptoms of ADHD
  • Easy distractability
  • Failure to receive or follow instructions
    properly
  • Inability to focus on one task at a time and
    tendency to jump from one activity to another
  • Difficulty remembering

21
Symptoms of ADHD (contd)
  • Frequent loss or misplacing of personal items
  • Excessive talking and interrupting other children
    in a group
  • Inability to sit still when asked repeatedly
  • Impulsiveness
  • Sleep disturbances

22
Atypical Antidepressants
  • Action - inhibit the reuptake of serotonin and
    affect the activity of norepinephrine and
    dopamine
  • Primary use - depression
  • Examples
  • Bupropion (Wellbutrin)
  • Nefazodone (Serzone)

23
CNS Stimulants - Schedule II Controlled Substance
  • Action - stimulate specific areas of CNS that
    heighten awareness and increase focus
  • Primary use - ADHA
  • Adverse effects
  • Insomnia
  • Nervousness anorexia
  • Weight loss
  • Examples
  • Methylphenidate (Ritalin)
  • Pemoline (Cykert)

24
Nonstimulants
  • Action - inhibit reuptake of norepinephrine
  • Primary use - ADHD
  • Adverse effects
  • Headache
  • Insomnia
  • Upper abdominal pain
  • Decreased appetite
  • Cough
  • Example - atomoxetine (Strattera)

25
Drugs for Psychoses and Degenerative Diseases of
the Nervous System
26
Imbalance of Neurotransmitters in Specific Areas
of the Brain
  • Too much dopamine produced
  • Stimulates dopamine type 2 (D2) receptors on the
    postsynaptic neurons

27
Parkinsonism Symptoms
  • Tremor
  • Muscle rigidity
  • Stooped posture
  • Shuffling gait

28
Most Common Degenerative Diseases of the CNS
  • Alzheimers disease
  • Amyotrophic lateral sclerosis (ALS)
  • Huntingtons chorea
  • Multiple sclerosis (MS)
  • Parkinsons disease

29
Parkinsons Disease Pharmacological Management
  • Agents do not cure the disease
  • Increase ability to perform normal daily
    activities
  • Reduce symptoms of the disease
  • Know the side effects of the agents

30
Alzheimers Disease Pharmacological Management
  • Do not cure the disease
  • Slow progression of disease in mild to moderate
    stages (not severe stage)
  • Limited effectiveness in improving
  • Functions in activities of daily living
  • Behavior
  • Cognition
  • Know the side effects of the different agents

31
Multiple Sclerosis Pharmacological Management
  • Do not cure the disease
  • Reduce inflammation during exacerbations
  • Prevent attacks on the nervous system
  • Relieve symptoms
  • Know the side effects of different agents

32
Drugs for Parkinsons Disease
  • Dopaminergic agents
  • Example - levodopa (Larodopa)
  • Action - increase dopamine levels in the corpus
    striatum
  • Primary use - Parkinsons disease
  • Adverse effects - involuntary movements,
    headache, insomnia, nausea, vomiting, orthostatic
    hypotension

33
Drugs for Parkinsons Disease (contd)
  • Anticholinergics
  • Example - benzotropine (Cogentin)
  • Action - acts on CNS
  • Primary use - Parkinsons disease
  • Adverse effects - dry mouth, blurred vision,
    tachycardia, urinary retention, constipation

34
Drugs for Alzheimers Disease
  • Acetylcholinesterase inhibitors
  • Example - donepezil (Aricept)
  • Action - inhibits acetylcholinesterase which
    intensifies effects of acetylcholine at
    cholinergic receptors in order to improve
    function in activities of daily living, behavior,
    cognition
  • Primary use - early stages of Alzheimer's disease
  • Adverse effects - nausea, vomiting, diarrhea

35
Drugs for Multiple Sclerosis
  • Immunostimulants
  • Example - interforon beta la (Avonex)
  • Action - decrease overall relapse rate
  • Primary use - RRMS
  • Adverse effects - redness, pain, swelling,
    itching or lump at injection site, joint pain,
    muscle aches

36
Drugs for Multiple Sclerosis (contd)
  • Miscellaneous drugs for symptoms
  • Modafinil (Provigil) and amantadine (Symmeterel)
    - fatigue, memory loss, progressive weakness
  • Gabapentin (Neurontin) - depression, sensitivity
    to pain
  • Methylprednisolone (Solu-Medrol) - acute
    inflammation of CNS

37
Drugs for Pain Control
38
Successful Pain Management Depends on
  • Accurate assessment of pain experienced
  • Potential disorders causing the pain
  • Selecting the correct therapy

39
Endogenous Opioids Are Neurotransmitters Released
by Descending Neurons
  • Examples - endorphins, dynorphins, enkephalins
  • Block the release of substance P in the spinal
    cord
  • Pain impulses do not reach the brain

40
Acute Opioid Intoxication
  • Medical emergency
  • Respiratory depression

41
Naloxone (Narcan) - Opioid Antagonist - Reverses
Respiratory Depression and Other Acute Symptoms
42
Opioid (Narcotic) Analgesics for Pain Management
  • Opioid agonists
  • Example - morphine
  • Mechanisms of action - bind to both mu and kappa
    receptors and produce analgesia, decrease GI
    motility, euphoria, miosis, sedation
  • Primary uses - treat severe pain
  • Adverse reactions - respiratory depression,
    sedation, nausea and vomiting, and physical and
    psychological dependence

43
Opioid (Narcotic) Analgesics for Pain Management
(contd)
  • Opioid antagonists
  • Example - naloxone (Narcan)
  • Mechanisms of action - inhibit both mu and kappa
    receptors preventing the effects of opioid
    agonists
  • Primary uses - opioid overdose, opioid depression
  • Adverse effect - drowsiness

44
Opioid (Narcotic) Analgesics for Pain Management
(contd)
  • Opioids with mixed agonist-antagonist activity
  • Example - pentazocine (Talwin)
  • Mechanisms of action - activate kappa receptors
    and block mu receptors to produce analgesia,
    decrease GI motility, miosis, sedation
  • Primary uses - treat moderate to severe pain
  • Adverse effects - less intense than opioid
    agonists

45
Nonopioid Analgesics
  • Nonsteroidal anti-inflammatory drugs (NSAIDs)
  • Examples - aspirin and other salicylates,
    ibuprofen and ibuprofen-like drugs, selective
    COX-2 inhibitors
  • Mechanisms of action - aspirin and ibuprofen
    inhibit both COX-1 and COX-2 enzymes which
    inhibit prostaglandins which inhibit pain and
    inflammation selective COX-2 inhibit only COX-2
    enzyme, which produces the prostaglandins that
    cause pain and inflammation
  • Primary uses - treat mild to moderate pain,
    inflammation, fever
  • Adverse effects - GI irritation and bleeding

46
Nonopioid Analgesics (contd)
  • Acetaminophen
  • Example - acetaminophen (Tylenol)
  • Mechanisms of action - inhibit prostaglandin
    production, then block transmission of pain
    impulse peripherally, inhibits prostaglandins in
    hypothalamus
  • Primary uses - treat mild to moderate pain and
    fever
  • Adverse effects - very few with recommended doses

47
Nonopioid Analgesics (contd)
  • Centrally acting drugs
  • Examples - clonidine (Catapres), tramadol
    (Ultram)
  • Mechanisms of action - prevents transmission of
    pain impulses in the spinal cord
  • Primary uses - management of pain
  • Adverse effects - drowsiness, hypotension, nausea
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