Pharmacology - Autonomic drugs

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jknell
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Pharmacology - Autonomic drugs
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2013-03-31 20:20:59
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Pharmacology - Autonomic drugs
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    • 1. Parasympathetic: Cardiac and smooth muscle, gland cells, nerve terminals
    • 2. Sympathetic: sweat glands
    • 3. Sympathetic: Cardiac and smooth muscle, gland cells, nerve terminals
    • 4. Sympathetic: Renal vasculature, smooth muscle
    • 5. Somatic: skeletal muscle
  1. Sympathetic nervous system
    cholinergic fibers
    Adrenal medulla and sweat glands are SNS but are innervated by cholinergic fibers
  2. Botulinum toxin
    Prevents release of neurotransmitter at all cholinergic terminals
  3. ACh receptors
    • Nicotinic ACh Receptors:
    • -Ligand-gated Na+/K+ channels
    • -NN (found in autonomic ganglia)
    • -NM (found in neuromuscular junction)

    • Muscarinic ACh Receptors:
    • -G-protein-coupled receptors that act through 2nd messengers
    • -M1, M2, M3, M4, and M5
  4. Sympathetic receptors: α1
    G-protein class, major function
    • α1q 
    • ↑ vascular smooth muscle contraction

    • ↑ pupillary dilator muscle contraction (mydriasis)
    • ↑ intestinal and bladder sphincter muscle contraction
  5. Sympathetic receptors: α2
    G-protein class, major function
    • α2i
    • ↓ sympathetic outflow
    • ↓ insuliln release
    • ↓ lipolysis
    • ↑ platelet aggregation
  6. Sympathetic receptors: β1
    G-protein class, major function
    • β1s
    • ↑ heart rate
    • ↑ contractility
    • ↑ renin release
    • ↑ lipolysis
  7. Sympathetic receptors: β2
    G-protein class, major function
    • β2: s
    • Vasodilation
    • Bronchodilation
    • ↑ heart rate
    • ↑ contractility
    • ↑ lipolysis
    • ↑ insulinn release
    • ↓ uterine tone (tocolysis)
    • Ciliary muscle relaxation
    • ↑ aqueous humor production
  8. Parasympathetic receptors: M1
    G-protein class, major function
    • M1: q
    • CNS
    • Enteric nervous system
  9. Parasympathetic receptors: M2
    G-protein class, major function
    • M2: i
    • ↓ heart rate
    • ↓ contractility of atria
  10. Parasympathetic receptors: M3
    G-protein class, major function
    • M3: q
    • ↑ exocrine gland secretions (e.g. lacrimal, gastric acid)
    • ↑ gut peristalsis
    • ↑ bladder contraction
    • Bronchoconstriction
    • ↑ pupullary schincter muscle contraction (miosis)
    • Ciliary muscle contraction (accommodation)
  11. Dopamine receptors
    G-protein class, major function
    • D1s - relaxes renal vascular smooth muscle
    • D2i - modulates transmitter release, especially in brain
  12. Histamine receptors
    G-protein class, major function
    • H1: q - ↑ nasal and bronchial mucus production, contraction of bronchioles, pruritis, and pain
    • H2: s - ↑ gastric acid secretion
  13. Vasopressin receptors
    G-protein class, major function
    • V1: q - ↑ vascular smooth muscle contraction
    • V2: s - ↑ H2O permeability and reabsorption in the collecting tubules of kidney (V2 is found in the 2 kidneys)
  14. Gq receptors
    intermediate, overall action
    • Gq: H1, α1, V1, M1, M3
    • **HAVe 1 M&M
    • Intermediate: Phospholipase C, PIP2
    • Result: smooth muscle contraction
  15. Gi and Gs receptor
    intermediate, major function
    • Gs: β1, β2, D1, H2, V2
    • Gi: M2, α2, D2
    • Intermediate: Adenylyl cyclase, cAMP
    • Result: inhibit smooth muscle, ↑ [Ca2+]in (heart)
    • Noradrenergic nerve terminal
    • Release of NE from a sympathetic nerve ending is modulated by NE itself
    • Acts on presynaptic α2-autoreceptors, and by ACh, angiotensin II, and other substances
  16. Cholinomimetic agents
    Direct vs indirect (anticholinesterases)
    • Direct:
    • -Bethanechol
    • -Carbachol
    • -Pilocarpine
    • -Methacholine

    • Indirect: (anticholinesterases)
    • -Neostigmine
    • -Pyridostigmine
    • -Edrophonium
    • -Physostigmine
    • -Donepezil
  17. Cholinomimetics
    possible adverse reactions
    Exacerbation of COPD, asthma, peptic ulcer disease
  18. Bethanechol
    uses, action
    • Uses: Postoperative ileus, neurogenic ileus, urinary retention
    • Action: Activates bowel and bladder smooth muscle
    • Resistant to AChE
  19. Carbachol
    uses, action
    • Carbachol
    • Uses: Glaucoma, pupillary contraction, relief of intraocular pressure
    • Action: Carbon copy of acetylcholine
  20. Pilocarpine
    uses, action
    • Uses: Potent stimulator of sweat, tears, saliva
    • Open-angle and closed-angle glaucoma
    • Action: Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE
    • **"You cry, drool, and sweat on your 'pilow'
  21. Methacholine
    uses, action
    • Uses: challenge test for dx of asthma
    • Action: Stimulates muscarinic receptor in airway when inhaled
  22. Neostigmine
    uses, action
    • Uses: Postoperative and neurogenic ileus and urinary retention
    • -myasthenia gravis
    • -reversal of neuromuscular junction blockade (postoperative)
    • Action: ↑ endogenous ACh
    • *Neo CNS = No CNS penetration
  23. Pyridostigmine
    uses, action
    • Uses: Myasthenia gravis (long acting)
    • -Does not penetrate CNS
    • Action: ↑ endogenous ACh
    • -↑ strength
    • **Pyridostigmine gets rid of myasthinea gravis
  24. Edrophonium
    Uses, action
    • Uses: Diagnosis of myasthenia gravis (extremely short acting)
    • Action: ↑ endogenous ACh
  25. Physostigmine
    Uses, action
    • Uses: anticholinergic toxicity (crosses blood-brain barrier)
    • Action: ↑ endogenous ACh
    • **Physostigmine "phyxes" atropine overdose
  26. Donepezil
    Uses, action
    • Uses: Alzheimer's disease
    • Application: ↑ endogenous ACh
  27. Cholinesterase inhibitor poisoning
    • Often due to organophosphates (parathion) - insecticides; poisoning usually seen in farmers
    • irreversibly inhibit AChE
    • Causes: DUMBBELSS
    • Diarrhea
    • Urination
    • Miosis
    • Bronchospasm
    • Bradycardia
    • Excitation of skeletal muscle and CNS
    • Lacrimation
    • Sweating
    • Salivation
    • Antidote: atropine + pralidoxime (regenerates active AChE)
  28. Muscarinic antagonists
    • Atropine, homatropine, tropicamide
    • Benztropine
    • Scopolamine
    • Ipratropium, tiotropium
    • Oxybutynin
    • Glycopyrrolate
  29. Atropine, homatropine, tropicamide
    • Eye
    • Produces mydriasis and cycloplegia
  30. Benztropine
    • CNS
    • Parkinson's disease
    • *"Park my Benz"
  31. Scopolamine
    • CNS
    • Motion sickness
  32. Ipratropium, tiotropium
    • Respiratory
    • COPD, asthma
    • *I pray I can breathe soon!"
  33. Oxybutynin
    • Genitourinary
    • Reduce urgency in mild cystitis and reduce bladder spasms
  34. Glycopyrrolate
    • Gastrointestinal, respiratory
    • Parenteral: preoperative use to reduce airway secretions
    • Oral: drooling, peptic ulcer
  35. Atropine
    organ system, action
    • Muscarinic antagonist; blocks DUMBBeLSS (skm and CNS excitation mediated by nicotinic receptors)
    • Used to treat bradycardia and for ophthalmic applications
    • Eye: ↑ pupil dilation, cycloplegia
    • Airway: ↓ secretions
    • Stomach: ↓ acid secretion
    • Gut: ↓ motility
    • Bladder: ↓ urgency in cystitis
  36. Atropine
    toxicity
    • ↑ body temperature (due to ↓ sweating)
    • Jimson weed (Datura) → gardener's pupil
    • Sx:
    • Rapid pulse
    • dry mouth
    • dry, flushed skin
    • cycloplegia
    • constipation
    • disorientation
    • Acute angle-closure glaucoma in elderly (due to mydriasis)
    • urinary retention in men with BPH
    • hyperthermia in infants
  37. Atropine
    toxicity pneumonic
    • Hot as a hare
    • Dry as a bone
    • Red as a beet
    • Blind as a bat
    • Mad as a hatter
  38. Sympathomimetics
    Direct vs indirect
    • Direct:
    • Epinephrine
    • Norepinephrine
    • Isoproterenol
    • Dopamine
    • Dobutamine
    • Phenylephrine
    • Albuterol, salmeterol, terbutaline
    • Ritodrine

    • Indirect:
    • Amphetamine
    • Ephedrine
    • Cocaine
  39. Epinephrine
    • α1, α2, β1, β2
    • Application: Anaphylaxis, glaucoma (open angle), asthma, hypotension
  40. Norepinephrine
    • α1, α2, β1
    • Application: Hypotension (but ↓ renal perfusion)
  41. Isoproterenol
    • β1, β2
    • Application: Torsade de pointes, bradyarrhythmias (but can worsen ischemia)
  42. Dopamine
    • Low dose: D1
    • Medium dose: β1, β2
    • High dose: α1, α2
    • Application: shock (renal perfusion), heart failure; inotropic and chronotropic
  43. Dobutamine
    • Mostly β1
    • Application: heart failure, cardiac stress testing; inotropic and chronotropic
  44. Phenylephrine
    • α1, α2
    • Application: Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)
  45. Albuterol, salmeterol, terbutaline
    • β2 > β1
    • Application:
    • -Metaproterenol and albuterol for acute asthma;
    • -Salmeterol for long-term asthma or COPD control;
    • -Terbutaline to reduce premature uterine contractions
  46. Ritodrine
    • β2
    • Application: Reduces premature uterine contraction
  47. Amphetamine
    • Indirect general agonist, releases stored catecholamines
    • Applications: Narcolepsy, obesity, attention deficit disorder
  48. Ephedrine
    • Indirect general agonist, releases stored catecholamines
    • Application: Nasal decongestion, urinary incontinence, hypotension
  49. Cocaine
    • Indirect general agonist, reuptake inhibitor
    • Application: causes vasoconstriction and local anesthesia;
    • **never give β-blockers if cocaine intoxication is suspected (can lead to unopposed α1 activation and extreme hypertension)
  50. Norepinephrine vs isoproterenol
    • NE:
    • -increases systolic and diastolic pressure (α1-mediated vasoconstriction)
    • - ↑ MAP → bradycardia

    • Isoproterenolno α effects
    • 2 mediated vasodilation
    • - ↓ MAP and ↑ heart rate through β1 and reflex activity
  51. Sympathoplegics
    Clonidine, α-methyldopa
    • Centrally acting α2-agonists
    • ↓ central sympathetic outflow
    • Application: hypertension, especially with renal disease (no decrease in renal blood flow)
  52. α-blockers
    Nonselective, α1 selective, α2 selective
    • Nonselective:
    • -PHenoxybenzamine (irreversible)
    • -Phentolamine (reversible)

    • α1 selective: (-osin ending)
    • -Prazosin, terazossin, doxazosin, tamsulosin
    • α2 selective:
    • -Mirtazapine
  53. Phenoxybenzamine
    • Nonselective α-blocker (irreversible)
    • Applications: pheochromocytoma (use before removing tumor)
    • Toxicity: orthostatic hypotension, reflex tachycardia
  54. Phentolamine
    • Nonselective α-blocker (reversible)
    • Applications: Give to pts on MAO inhibitors who eat tyramine-containing foods
  55. Prazosin, terazosin, doxazosin, tamsulosin
    • α1 - selective blocker
    • Uses: hypertension, urinary retention in BPH
    • Toxicity: 1st-dose orthostatic hypotension, dizziness, headache
  56. Mirtazapine
    • α2-selective blocker
    • Use: depression
    • Toxicity: sedation, ↑ serum cholesterol, ↑ appetite
    • Epi
    • Epi + α blockade
    • Phenylephrine
    • Phenylephrine + α blockade
  57. β-blockers
    • acetubolol
    • betaxolol
    • esmolol
    • atenolol
    • metoprolol
    • propranolol
    • timolol
    • pindolol
    • labetalol
  58. β-blockers
    applications, effects
    • Angina pectoris: ↓ heart rate and contractility, resulting in ↓ O2 consumption
    • MI: β-blockers ↓ mortality
    • SVT (metoprolol, esmolol): ↓ AV conduction velocity (class II antiarrhythmic)
    • Hypertension: ↓ cardiac output, ↓ renin secretion (due to β1-receptor blockade on JGA cells)
    • CHF: slows progression of chronic failure
    • Glaucoma (timolol): ↓ secretion of aqueous humor
  59. β-blockers
    Toxicity
    • Impotence
    • exacerbation of asthma
    • CV adverse effects (bradycardia, AV block, CHF)
    • CNS adverse effects (seizures, sedation, sleep alterations)
    • *Use with caution in diabetics
  60. β1-blockers
    Selectivity
    • β1-blockers: A through M (except cavedilol)
    • -Acebutol (partial agonist)
    • -Betaxolol
    • -Esmolol (short acting)
    • -Atenolol
    • -Metoprolol
    • *Adventageous in patients with comorbid pulmonary disease
    • **A BEAM
  61. Nonselective antagonists (β1 = β2)
    • *P throuh Z
    • Propranolol
    • Timolol
    • Nadolol
    • Pindolol
  62. Nonselective (vasodilatory) α- and β-antagonists
    • Carvedilol
    • Labetalol
  63. Partial β-Agonists
    • Pindolol
    • Acebutolol
    • *PAPAPartial β-Agonists

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