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Monday, September 15, 2008

Cholinergic Blockers Updates (Nclex Pharmacology Summaries & WorkSheets)

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Cholinergic Blockers Updates (Pharmacology Summaries & WorkSheets) Slideshow Transcript
Slide 1: Drugs Affecting the Autonomic Nervous System Cholinergic Agents and Cholinergic Blocking Agents Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 2: Cholinergic Agents • Drugs that stimulate the parasympathetic nervous system (PSNS) • The PSNS is the opposing system to the SNS Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 3: Cholinergic Agents Also known as • cholinergic agonists or • parasympathomimetics Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 4: Instructors may wish to use EIC Image #56: The Parasympathetic and Sympathetic Nervous Systems and Their Relationships to One Another Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 5: Cholinergic Agents • Mimic the effects of the PSNS neurotransmitter • Acetylcholine (ACh) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 6: Cholinergic Receptors Two types, determined by: • Location • Action once stimulated Nicotinic receptors and Muscarinic receptors Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 7: Nicotinic Receptors • Located in the ganglia of both the PSNS and SNS • Named “nicotinic” because can be stimulated by the alkaloid nicotine Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 8: Muscarinic Receptors • Located postsynaptically: – Smooth muscle – Cardiac muscle – Glands of parasympathetic fibers – Effector organs of cholinergic sympathetic fibers • Named “muscarinic” because can be stimulated by the alkaloid muscarine Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 9: Instructors may wish to insert EIC Image #57: The Sympathetic, Parasympathetic, and Somatic Nervous Systems This slide illustrates location of the nicotinic and muscarinic receptors within the PSNS. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 10: Lisa L. HHS: Hernandez: HHS: Adrenergic Agents: Is there copy missing at the Mechanism of Action end? Inhibiting what? • Direct-acting (agonist) – Bind to cholinergic receptors, causing stimulation Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 11: Adrenergic Agents: Mechanism of Action • Indirect-acting – Inhibit the enzyme “cholinesterase” Result: more ACh is available at the receptors Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 12: Indirect-Acting Cholinergic Agents (Cholinesterase Inhibitors) • Reversible – Bind to cholinesterase for a period of minutes to hours • Irreversible – Bind to cholinesterase and form a permanent covalent bond – The body must make new cholinesterase Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 13: Drug Effects of Cholinergic Agents • Effects seen when the PSNS is stimulated. • The PSNS is the “rest and digest” system. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 14: Drug Effects of Cholinergic Agents “SLUDGE” • Salivation • Lacrimation • Urinary incontinence • Diarrhea • Gastrointestinal cramps • Emesis Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 15: Drug Effects of Cholinergic Agents • Stimulate intestine and bladder – Increased gastric secretions – Increased gastrointestinal motility – Increased urinary frequency • Stimulate pupil – Constriction (miosis) – Reduced intraocular pressure • Increased salivation and sweating Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 16: Drug Effects of Cholinergic Agents • Cardiovascular effects – Decreased heart rate – Vasodilation • Respiratory effects – Bronchial constriction, narrowed airways Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 17: Drug Effects of Cholinergic Agents • At recommended doses, the cholinergics primarily affect the MUSCARINIC receptors. • At high doses, cholinergics stimulate the NICOTINIC receptors. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 18: Drug Effects of Cholinergic Agents • DESIRED EFFECTS: from muscarinic receptor stimulation • Many undesirable effects are due to stimulation of the nicotinic receptors Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 19: Cholinergic Agents: Therapeutic Uses Direct-Acting Agents • Reduce intraocular pressure • Useful for glaucoma and intraocular surgery Examples: acetylcholine, carbachol, pilocarpine Topical application due to poor oral absorption Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 20: Cholinergic Agents: Therapeutic Uses Direct-Acting Agent—bethanechol • Increases tone and motility of bladder and GI tract • Relaxes sphincters in bladder and GI tract, allowing them to empty • Helpful for postsurgical atony of the bladder and GI tract Oral dose or SC injection Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 21: Cholinergic Agents: Therapeutic Uses Indirect-Acting Agents • Cause skeletal muscle contractions • Used for diagnosis and treatment of myasthenia gravis • Used to reverse neuromuscular blocking agents • Used to reverse anticholinergic poisoning (antidote) Examples: physostigmine, pyridostigmine Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 22: Cholinergic Agents: Therapeutic Uses Indirect-Acting Agent—donepezil (Aricept) • Used in the treatment of mild to moderate Alzheimer’s disease. • Helps to increase or maintain memory and learning capabilities. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 23: Cholinergic Agents: Side Effects Side effects are a result of overstimulation of the PSNS. • Cardiovascular: – Bradycardia, hypotension, conduction abnormalities (AV block and cardiac arrest) • CNS: – Headache, dizziness, convulsions • Gastrointestinal: – Abdominal cramps, increased secretions, nausea, vomiting Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 24: Cholinergic Agents: Side Effects Side effects are a result of overstimulation of the PSNS. • Respiratory: – Increased bronchial secretions, bronchospasms • Other: – Lacrimation, sweating, salivation, loss of binocular accommodation, miosis Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 25: Cholinergic Agents: Interactions • Anticholinergics, antihistamines, sympathomimetics • Antagonize cholinergic agents, resulting in decreased responses Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 26: Cholinergic Agents: Nursing Implications • Keep in mind that these agents will stimulate the PSNS and mimic the action of ACh. • Assess for allergies, presence of GI or GU obstructions, asthma, peptic ulcer disease, or coronary artery disease. • Perform baseline assessment of VS and systems overview. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 27: Cholinergic Agents: Nursing Implications • Medications should be taken as ordered and not abruptly stopped. • The doses should be spread evenly apart to optimize the effects of the medication. • Overdosing can cause life-threatening problems. Patients should not adjust the dosages unless directed by the physician. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 28: Cholinergic Agents: Nursing Implications • Encourage patients with myasthenia gravis to take medication 30 minutes before eating to help improve chewing and swallowing. • When donepezil is prescribed for Alzheimer’s disease, be honest with caregivers and patients that the drug is for management of symptoms, not for a cure. • Therapeutic effects of donepezil may not occur for up to 6 weeks. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 29: Cholinergic Agents: Nursing Implications • Atropine is the antidote for cholinergics. It should be available in the patient’s room for immediate use if needed. • Patients should notify their physician if they experience muscle weakness, abdominal cramps, diarrhea, or difficulty breathing. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 30: Cholinergic Agents: Nursing Implications Monitor for side effects, including: Increased respiratory Abdominal cramping secretions Bronchospasms Dysrhythmias Difficulty breathing Hypotension Nausea and vomiting Bradycardia Diarrhea Increased sweating Increase in frequency and urgency of voiding patterns Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 31: Cholinergic Agents: Nursing Implications Monitor for therapeutic effects: • Alleviated signs and symptoms of myasthenia gravis • In postoperative patients with decreased GI peristalsis, look for: – Increased bowel sounds – Passage of flatus – Occurrence of bowel movements • In patients with urinary retention/hypotonic bladder, urination should occur within 60 minutes of bethanecol administration Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 32: Cholinergic Blocking Agents • Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system (PSNS) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 33: Cholinergic Blocking Agents: Mechanism of Action • Competitive antagonists • Compete with ACh • Block ACh at the muscarinic receptors in the PSNS – As a result, ACh is unable to bind to the receptor site and cause a cholinergic effect. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 34: Cholinergic Blocking Agents: Mechanism of Action • Once these drugs bind to receptors, they inhibit nerve transmission at these receptors. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 35: Instructors may wish to use EIC Image #58: Site of Action of Cholinergic Blockers Within the PSNS Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 36: Cholinergic Blocking Agents: Chemical Class Natural Synthetic/Semisynthetic atropine anisotropine clidinium belladonna dicyclomine glycopyrrolate hyoscyamine hexocyclium homatropine scopolamine ipratropium isopropamide oxybutynin propantheline tolterodine tridihexethyl Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 37: Drug Effects of Cholinergic Blocking Agents • Cardiovascular – Small doses: decrease heart rate – Large doses: increase heart rate • CNS – Small doses: decrease muscle rigidity and tremors – Large doses: drowsiness, disorientation, hallucinations Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 38: Drug Effects of Cholinergic Blocking Agents • Eye – Dilated pupils (mydriasis) – Decreased accommodation due to paralysis of ciliary muscles (cycloplegia) • Gastrointestinal – Relax smooth muscle tone of GI tract – Decrease intestinal and gastric secretions – Decrease motility and peristalsis Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 39: Drug Effects of Cholinergic Blocking Agents • Genitourinary – Relaxed detrusor muscle – Increased constriction of internal sphincter – Result: urinary retention • Glandular – Decreased bronchial secretions, salivation, sweating • Respiratory – Decreased bronchial secretions – Dilated bronchial airways Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 40: Cholinergic Blocking Agents: Therapeutic Uses CNS Decreased muscle rigidity and muscle tremors • Parkinson’s disease • Drug-induced extrapyramidal reactions Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 41: Cholinergic Blocking Agents: Therapeutic Uses Cardiovascular Affect the heart’s conduction system • Low doses: slow the heart rate • High doses: block inhibitory vagal effects on the SA and AV node pacemaker cells – Result: increased heart rate Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 42: Cholinergic Blocking Agents: Therapeutic Uses Atropine Used primarily for cardiovascular disorders • Sinus node dysfunction • Symptomatic second-degree heart block • Sinus bradycardia with hemodynamic compromise (advanced life support) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 43: Cholinergic Blocking Agents: Therapeutic Uses Respiratory Blocking the cholinergic stimulation of the PSNS allows unopposed action of the SNS. • Results: – Decreased secretions from nose, mouth, pharynx, bronchi – Relaxed smooth muscles in bronchi and bronchioles – Decreased airway resistance – Bronchodilation Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 44: Cholinergic Blocking Agents: Therapeutic Uses Respiratory agents are used to treat: • Exercise-induced bronchospasms • Chronic bronchitis • Asthma • Chronic obstructive pulmonary disease Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 45: Cholinergic Blocking Agents: Therapeutic Uses Gastrointestinal PSNS controls gastric secretions and smooth muscles that produce gastric motility. • Blockade of PSNS results in: – Decreased secretions – Relaxation of smooth muscle – Decreased GI motility and peristalsis Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 46: Cholinergic Blocking Agents: Therapeutic Uses Gastrointestinal agents are used to treat: • Peptic ulcer disease • Irritable bowel disease • GI hypersecretory states Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 47: Cholinergic Blocking Agents: Therapeutic Uses Genitourinary • Relaxed detrusor muscles of the bladder • Increased constriction of the internal sphincter • Reflex neurogenic bladder • Incontinence Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 48: Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Cardiovascular Increased heart rate, dysrhythmias CNS CNS excitation, restlessness, irritability, disorientation, hallucinations, delirium Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 49: Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Eye Dilated pupils, decreased visual accommodation, increased intraocular pressure Gastrointestinal Decreased salivation, decreased gastric secretions, decreased motility Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 50: Cholinergic Blocking Agents: Side Effects Body System Side/Adverse Effects Genitourinary Urinary retention Glandular Decreased sweating Respiratory Decreased bronchial secretions Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 51: Cholinergic Blocking Agents: Interactions • Antihistamines, phenothiazines, tricyclic antidepressants, MAOIs • When given with cholinergic blocking agents, cause ADDITIVE cholinergic effects, resulting in increased effects Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 52: Cholinergic Blocking Agents: Nursing Implications • Keep in mind that these agents will block the action of ACh in the PSNS. • Assess for allergies, presence of BPH, glaucoma, tachycardia, MI, CHF, hiatal hernia, and GI or GU obstruction. • Perform baseline assessment of VS and systems overview. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 53: Cholinergic Blocking Agents: Nursing Implications • Medications should be taken exactly as prescribed to have the maximum therapeutic effect. • Overdosing can cause life-threatening problems. • Blurred vision may cause problems with driving or operating machinery. • Patients may experience sensitivity to light and may want to wear dark glasses or sunglasses. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 54: Cholinergic Blocking Agents: Nursing Implications • When giving ophthalmic solutions, apply pressure to the inner canthus to prevent systemic absorption. • Dry mouth may occur; can be handled by chewing gum, frequent mouth care, and hard candy. • Check with physician before taking any other medication, including OTC medications. • ANTIDOTE for atropine is physostigmine salicylate (Antilirium). Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 55: Cholinergic Blocking Agents: Nursing Implications • Anticholinergics may lead to higher risk for heat stroke due to effects on heat-regulating mechanisms. • Teach patients to limit physical exertion, and avoid high temperatures and strenuous exercise. • Emphasize the importance of adequate fluid and salt intake. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 56: Cholinergic Blocking Agents: Nursing Implications • Patients should report the following to their physician: urinary hesitancy and/or retention, constipation, palpitations, tremors, confusion, sedation or amnesia, excessive dry mouth (especially if they have chronic lung infections or disease), or fever Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 57: Cholinergic Agents: Nursing Implications • Monitor for therapeutic effects: • For patients with Parkinson’s disease: fewer tremors and decreased salivation and drooling • For patients with peptic ulcer disease: decreased abdominal pain Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Slide 58: Cholinergic Blocking Agents: Nursing Implications Monitor for side effects, including: Constipation Tachycardia Tremors Confusion Hallucinations Sedation Urinary retention Hot, dry skin Fever CNS depression (occurs with large doses of atropine) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.





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