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2012-01-14 14:19:49
D3 Autonomic Pharmacology

D3 Autonomic Pharmacology
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  1. Which drug class is Epinephrine in?
    Sympathetic Agonists - ­Nonspecific
  2. List the indications for Epinephrine
    • Local Vasoconstriction
    • Hypotension and Shock
    • Bronchodilation
    • Allergy
  3. What is the mechanism of action of Epinephrine?
    Direct stimulation of α and β adrenergic receptors
  4. How is Epinephrine used in dentistry?
    Vasoconstriction—less bleeding and makes the analgesia last longer
  5. Use of Epinephrine could result in complications/ adverse effects in patients with what types of medical conditions?
    • Cardiac disease
    • Cerebrovascular disease
    • Diabetes
    • Parkinson's disease
    • Thyroid disease
  6. What is the impact of Epinephrine on the heart?
    β1 stimulation increases the work of the heart and decreases cardiac efficiency
  7. What effects of Epinephrine are of concern in the diabetic patient?
    • Increases in circulating blood glucose from stimulation of liver glycogenolysis and glucagon secretion
    • Inhibition of insulin secretion
  8. Why is the use of Epinephrine a cause for concern in patients with Parkinson's disease?
    May cause temporary worsening of symptoms
  9. What is the upper limit of Epinephrine that can be used, per procedure, in patients taking β-Blockers?
    Upper Limit: 0.04 mg total per procedure
  10. Epinephrine can adversely interact with what types of medications?
    • Tricyclic Antidepressants
    • β-Blockers
  11. What adverse effects can be seen if Epinephrine is given to a patient on Tricyclic Antidepressants?
    Tricyclic Antidepressants block reuptake and degradation of epi, leading to more cardiac adverse effects
  12. What adverse effects can be seen if Epinephrine is given to a patient on Non-Selective β-Blockers?
    Block β receptors in the peripheral blood vessels, epi acts as a pure α agonist and blood pressure rises
  13. What adverse effects can be seen if Epinephrine is given to a patient on Selective β-Blockers?
    Selective Block β1 receptors in heart, at high doses block β 2 receptors in peripheral blood vessels
  14. Name two α Sympathetic Agonists┬×
    • Methylphenidate (Ritalin) ┬×
    • Amphetamine (Adderall)
  15. What is the mechanism of action of α Sympathetic Agonists?
    Release of Norepi from synaptic vesicle
  16. What are α Sympathetic Agonists used for?
    • ADHD
    • Narcolepsy
  17. What is the risk for abuse and addiction of α Sympathetic Agonists?
    Schedule 2 (Ritalin and Adderall)
  18. What are the adverse effects of α Sympathetic Agonists?
    • Dyskinesia, muscle tightness, bruxism
    • The FDA asked the Drug Safety and Risk Management advisory committee to look into studying the cardiac risk in both adult and children taking ADHD drugs
  19. Which drug class is Clonidine (Catapres) in?
    Presynaptic α2 Agonist
  20. What is Clonidine (Catapres) used for?
    • Used in hypertension (oral tablet and patch)
    • Used with opiates to relieve the pain associated with end-stage cancer (Epidural Injection)
  21. What is the mechanism of action of Clonidine (Catapres)?
    • Inverse Agonist
    • Binds to α2 medullary receptors in the brain which inhibit sympathetic outflow to the body and α receptors in blood vessels are inhibited
  22. What are the Dental Adverse Effects of Clonidine (Catapres)?
    • Dry mouth
    • Orthostatic hypotension
  23. What dosage forms is Clonidine (Catapres)
    available in?
    Oral Tablet: Used for HTN

    Patch: Used for HTN (Catapres TTS)

    Epidural Injection: Used with opiates to relieve the pain associated with end-stage cancer
  24. Which drug class is Albuterol (Proventil) in?
    β2 Sympathetic Agonist
  25. What is Albuterol (Proventil) used for?
    • Asthma
    • COPD
  26. What is the mechanism of action of Albuterol (Proventil)?
    Stimulation of β2 receptors in lungs to cause bronchodilation
  27. What dosage forms is Albuterol (Proventil) available in?
    • Albuterol Inhalation Aerosol
    • Note: when inhaled, β2 receptors in the lungs will receive most of the drug to decrease the chance for adverse effects
  28. What are the Dental Adverse Effects of Albuterol (Proventil)?
    • unusual taste
    • drying or irritation of the oropharynx
  29. What are the effects of Acetylcholine?
    • Bradycardia
    • Vasodilation
    • Bronchoconstriction
    • Relaxation of urinary sphincter
    • Increase GI secretions
    • Sweating
    • Contraction of iris
    • SLUD Response: Salivation, Lacrimation, Urination, Defecation
  30. What are the therapeutic uses of drugs at Adrenegeric Receptors (Antagonists)?
    • HTN
    • Post myocardial infarction
    • CHF
    • Treatment of arrhythmias
    • Ischemic heart disease
    • Benign prostatic hyperplasia
  31. Which drug class is Terazosin (Hytrin) in?
    α Sympathetic Antagonist
  32. What is Terazosin (Hytrin) used for?
    HTN and benign prostatic hyperplasia
  33. What is the mechanism of action of Terazosin (Hytrin)?
    α1 receptor blockade, leading to smooth muscle relaxation
  34. What are the Dental Adverse Effects of Terazosin (Hytrin)?
    • Dry mouth
    • Dizziness
    • Orthostatic hypotension
  35. Which drug class is Tamsulosin (Flomax) in?
    α Sympathetic Antagonist
  36. What is the mechanism of action of Tamsulosin (Flomax)?
    Blockade of α1A and α1D adrenergic receptor subtypes found only in prostate gland
  37. What is Tamsulosin (Flomax) used for?
    Benign prostatic hyperplasia
  38. List eight effects of β Blockers
    • ↓ the force and rate of myocardial contraction
    • ↓ O2 consumption of the heart
    • ↓ of blood pressure in hypertensive patients
    • CO decreases
    • HR decreases
    • Reduction in plasma renin activity
    • Decrease CNS sympathetic outflow
    • Alteration in baroreceptor responsiveness
  39. Whate are the 2 types of β Blockers?
    • Selective for β1
    • Nonselective
  40. Which drug class is Metoprolol (Toprol XL) in?
    β Blocker (Selective for β1)
  41. What is the mechanism of action of Metoprolol (Toprol XL)?
    Competitive inhibitors of epinephrine and norepi at β1
  42. Which drug class is Propranolol (Inderal) in?
    β Blocker (Nonselective)
  43. What is the mechanism of action of Propranolol (Inderal)?
    Non-selective competitive inhibitor of beta receptors
  44. What is Propranolol (Inderal) used for?
    • Cardiovascular Disease
    • Stage fright
    • Tremor
    • Migraine headache
    • Sexual aggression
  45. What are the Dental Adverse Effects of β Blockers?
    • ­Altered taste ­
    • Lichenoid rxns ­
    • Orthostatic hypotension
  46. What are the Adverse Effects of Non-Selective β Blockers?
    • May enhance the pressor response to epinephrine
    • ­Hypertension
    • Bradycardia
  47. Which drug class is Carvedilol (Coreg) in?
    β Antagonist
  48. What is the mechanism of action of Carvedilol (Coreg)?
    • Antagonist at β1 and α1 receptors
    • Decrease heart rate and contractility and decrease blood pressure through alpha blockade
  49. What is Carvedilol (Coreg) used for?
    CHF (congestive heart failure)
  50. Name the 4 Mechanisms by which Autonomic Nervous System Drugs Act
    • Influence release of the neurotransmitter
    • Influence degradation of the neurotransmitter
    • Influence reuptake of the neurotransmitter
    • Bind (agonist) or block (antagonist) receptor
  51. Name 2 General Therapeutic Uses of Cholinergic Drugs
    • Alzheimer's
    • Salivary Stimulants
  52. Name the 2 mechanisms of Cholinergic Drugs
    • Reversible Cholinesterase Inhibition – Prolong t1/2 of acetylcholine at receptor site
    • Direct Acting – Bind to and stimulate muscarinic receptors
  53. Which drug class is Tacrine (Cognex) in?
    Cholinesterase Inhibitor
  54. What is Tacrine (Cognex) used for?
    • Alzheimer’s
    • Parkinson’s disease with dementia
  55. What is the mechanism of action of Tacrine (Cognex)?
    Idea: Prolong acetylcholine half life in the brain
  56. Name 2 Salivary Stimulants
    • Pilocarpine (Salagen)
    • Cevimeline (Evoxac)
  57. What is the mechanism of action of Salivary Stimulants?
    Agonist at muscarinic receptors
  58. What dosage of Salivary Stimulants is normally prescribed?
    Doses are individualized for desired effects until adverse reactions become intolerable.
  59. Use of Salivary Stimulants could result in complications/ adverse effects in patients with what types of medical conditions?
    • COPD
    • Parkinson’s disease
  60. Use of Cholinergic Drugs could result in complications/ adverse effects in patients with what types of medical conditions?
    Contraindicated in asthma, cardiovascular disease, and ulcer
  61. What adverse effects are associated with Cholinergic Drugs?
    • nausea
    • diarrhea
    • vomiting
    • rhinitis
    • urinary frequency
    • bronchospasm
    • hypotension
    • arrhythmias
    • (parasympathetic reactions)
  62. List seven Effects of Norepinephrine
    • Tachycardia
    • Vasoconstriction
    • Bronchodilation
    • Contraction of urinary sphincter
    • Decreased GI secretions
    • Glycogenolysis
    • Gluconeogenesis
    • Lipolysis
  63. List five Effects of Antimuscarinic Drugs
    • GI:↓ motor and secretory responses
    • Eye: Dilation
    • Urinary Retention
    • Respiratory Tract: Relaxation
    • Salivary Glands: ↓ Secretion
  64. What are the General Therapeutic Uses of Antimuscarinic Drugs?
    • Bronchodilation: Asthma and COPD
    • ­Urinary: antispasmodics
  65. Name 2 Antimuscarinic Drugs used for Bronchodilation (Asthma and COPD)
    • ­Ipratropium (Atrovent)
    • ­Tiotropium (Spiriva)
  66. Name 2 Antimuscarinic Drugs used to treat urinary disfunction (antispasmodics)
    • ­Tolterodine (Detrol)
    • Darifenacin (Enablex)
  67. What is Ipratropium (Atrovent) used for?
    • Bronchodilation
    • By itself, or in combination inhalation product with albuterol (Combivent Inhaler)
  68. What is Tiotropium (Spiriva) used for?
    • Bronchodilation
    • Prolonged T ½ used primarily in COPD
  69. Whate are Tolterodine (Detrol) and Darifenacin (Enablex) used for?
    • Urinary: “antispasmodics”
    • Contracts urinary sphincter muscles used in dysuria, urgency, incontinence
  70. What is a benefit of Darifenacin (Enablex) vs. Tolterodine (Detrol)?
    Darifenacin (Enablex) is a M3 selective agent, less dry mouth and constipation
  71. What drug interactions are associated with Antimuscarinic Drugs?
    • Anticholinergic effects are potentiated by antihistamines. This leads to severe dry mouth.
    • CYP2D6 Inhibitors: may diminish the therapeutic effect of Codeine (Enablex)
  72. List three Therapeutic Uses of Drugs at Nicotinic Receptors
    • Only therapeutic use for nicotine: in smoking cessation programs, gum, patches
    • Neuromuscular junction blockers are used in surgery and intubation –succinylcholine
    • Botulinum toxin type A-Botox
  73. What is the mechanism of action of Nicotine?
    • α4β2 neuronal nicotinic acetylcholine receptors
    • stimulate the central nervous mesolimbic dopamine system
    • neuronal mechanism underlying reinforcement and reward experienced upon smoking
  74. What is the mechanism of action of Varenicline (Chantix)?
    • α4β2 neuronal nicotinic acetylcholine receptors
    • produces agonist activity, while simultaneously preventing nicotine binding to α4β2 receptors
    • stimulates receptor-mediated activity, but at a significantly lower level than nicotine
  75. What are the adverse effects of Varenicline (Chantix)?
    • Nightmares
    • Psychosis
  76. What is the mechanism of action of Botulinum Toxin?
    Prevents synaptic vesicle fusion with membrane
  77. What is Botulinum Toxin used for?
    • Focal dystonias
    • Headache and pain syndromes