Linton: Introduction to Medical-Surgical Nursing, 4th Edition Pharmacology Tutorial Chapter 16: Cholinergics

The parasympathetic nervous system (PNS) is called the cholinergic system because its primary neurotransmitter is acetylcholine (ACh). Drugs that mimic acetylcholine are called cholinergic drugs, or parasympathomimetics. They are cholinergic agonists because they initiate a cholinergic response. Anticholinergic drugs, or parasympatholytics, block the effect of acetylcholine. They are also called cholinergic antagonists because they inhibit the effect of acetylcholine at the receptor sites. Functions stimulated by the PNS are described as resting, reparative, or vegetative: rest and digest. These functions include digestion, excretion, cardiac deceleration, and near vision. Drugs that affect the PNS act not only on target receptors but also on nearly all PNS receptors. For this reason, most of the side and adverse effects are either normal responses to autonomic stimulation or exaggerations of normal responses. If you are thoroughly familiar with the bodys response to parasympathetic stimulation, you will be able to predict certain side effects and adverse reactions. This will enable you to determine correct nursing actions and provide appropriate patient teaching (refer to Linton and Maebius text, Table 26-2, p. 370). There are two types of cholinergic receptors: nicotinic and muscarinic. Nicotinic activation causes skeletal muscle contraction and, in the brain, promotes the release of acetylcholine in the cerebral cortex. Activation of muscarinic receptors can stimulate or suppress cells in the heart and blood vessels, gastrointestinal tract, respiratory tract, urinary tract, and the eye. Cholinergic drugs mimic the effects of acetylcholine, or increase the concentration of acetylcholine by stimulating its production or preventing its breakdown. Table 16-1 lists the cholinergic drugs, their uses, and specific considerations.

Elsevier items and derived items 2007 by Saunders, an imprint of Elsevier Inc.

Table 16-1 Cholinergic Drugs Drug bethanechol (Urecholine) Uses Treats urinary retention and postoperative decrease in gastrointestinal activity. Specific Considerations Routes: PO or SC only (NOT IM or IV). Administer before meals to reduce gastrointestinal distress. Can cause central nervous system stimulation and circulatory collapse. Expect urination within 1 hour. Anticipate need for catheterization if not effective. Give with milk or food. If patient has trouble swallowing, give 30-45 minutes before meals. IV form must be given very slowly. Check pulse before parenteral dose. If pulse is <60, anticipate order for atropine to increase heart rate before giving neostigmine. Routes: IM, IV. Have atropine available as an antidote. Monitor for extreme muscle weakness related to cholinergic crisis. Routes: PO, IM, IV. Give PO drug with food or milk. If patient has difficulty swallowing, give 30-45 minutes before meals. Atropine may be ordered with pyridostigmine to reduce side effects. Schedule largest dosage to coincide with times of greatest fatigue.

neostigmine (Prostigmin)

Long-term treatment of myasthenia gravis, to reverse neuromuscular blocking agents, and to relieve urinary retention.

edrophonium (Tensilon)

Used to diagnose myasthenia gravis, to differentiate myasthenic crisis from cholinergic crisis, and to reverse effects of neuromuscular blockers. Preferred drug for long-term treatment of myasthenia gravis.

pyridostigmine (Mestinon)

Pharmacology Tutorial Table 16-1 Cholinergic Drugscontd Drug tacrine (Cognex) Uses Used to delay progression of symptoms in early Alzheimers disease.

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donepezil (Aricept)

Used to delay progression of symptoms in early Alzheimers disease.

Specific Considerations Risk of liver toxicity. Monitor liver function results. Evaluate mental status. Effects reduced by smoking; enhanced by cimetidine. Take at regular intervals; can be taken with meals. Advantage over tacrine is lack of liver toxicity. May aggravate chronic pulmonary disease.

ACTIONS AND USES Cholinergic drugs are classified as direct-acting or indirect-acting. Directing-acting cholinergic drugs are synthetic substances that have longer durations of action than acetylcholine. Their target organs and actions as summarized earlier include: Heart: decreased rate Blood vessels: dilation Gastrointestinal tract: increased tone and contractility, increased salivary and gastrointestinal secretions, sphincter relaxation Bladder: increased tone and contractility, sphincter relaxation Bronchi: increased tone and contractility Lungs: increased secretions Eye: miosis (pupil constriction), contraction of ciliary muscle Examples of direct-acting cholinergics are bethanechol (Urecholine) and pilocarpine (IsoptoCarpine, Ocusert). Bethanechol is used to treat urinary retention by causing contraction of the bladder muscle and relaxing the urinary sphincter. Topical or implanted pilocarpine is used in the treatment of glaucoma (see Chapter 30). Indirect-acting cholinergics are also called anticholinesterase agents because they work by preventing the breakdown of acetylcholine by cholinesterase (an enzyme). Normally, excessive accumulation of acetylcholine is prevented by cholinesterase. Effects of indirect-acting drugs are as follows: Skeletal muscle: improved force of contraction Brain: enhanced transmission of nerve impulses Indirect-acting cholinergics are used to reverse the neuromuscular blocking effects of some drugs used in surgery, and in the treatment of myasthenia gravis and Alzheimers disease.

Elsevier items and derived items 2007 by Saunders, an imprint of Elsevier Inc.

SIDE AND ADVERSE EFFECTS Side and adverse effects of cholinergic drugs are related to parasympathetic stimulation. They may include the following: Cardiovascular: bradycardia, dysrhythmias, hypotension Central nervous system: headache, drowsiness, seizures, loss of consciousness Respiratory: bronchospasm, increased secretions, respiratory failure Gastrointestinal: increased salivation, nausea, vomiting, diarrhea, abdominal cramping Bladder: increased frequency and urgency of urination Other: increased sweating, pupil constriction, rash Cholinergic crisis is related to overdose and is manifested by severe weakness that affects the muscles of chewing, swallowing, and breathing. Paralysis of leg muscles occurs as well. Overdose is treated with atropine sulfate. INTERACTIONS AND CONTRAINDICATIONS Drugs that decrease the effects of cholinergic agents are anticholinergics and antihistamines. Quinidine and procainamide can also antagonize the drug effects. Cholinergics are contraindicated with mechanical obstruction of the gastrointestinal or urinary tract. NURSING ACTIONS Monitor vital signs, respiratory status, mental status, muscle strength, and elimination. Have atropine available as an antidote for cholinergic overdose. PATIENT TEACHING Report any palpitations, dizziness, difficulty breathing, or gastrointestinal distress. You may notice increased salivation and sweating.