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Cholinergic Agonists (Parasympathomimetics)

Cholinergic agonists act at the selfselfselfsimilar punsteady as the neurotransmitter acetylcholine (ACh) and acception the ghost of the ACh receptor plights throughout the collectiveness. These receptor plights are plant throughout the collectiveness so their stimulation produces congruous goods when parasympathetic nervous classifyment is activated. Thus, they are as-polite designated as parasympathomimetics. Cholinergic agonists can either be direct- or indirect-acting cholinergic agonists. Under indirectly-acting cholinergic agonists, tnear are vicegerents for Alzheimer’s and Myasthenia Gravis.

Cholinergic Agonists: General and Stigma Names

Here is a table of classifymentatically encountered cholinergic agonists, their general calls, and stigma calls:
Classification Generic Name Brand Name
Direct-Acting Cholinergic Agonists bethanechol Duvoid, Urecholine
carbachol Miostat
cevimeline Evoxac
pilocarpine Salagen
Indirect-Acting Cholinergic Agonists
Agents of Myasthenia Gravis ambenonium Mytelase
edrophonium Reversal
neostigmine Prostigmin
pyridostigmine Mestinon
Agents for Alzheimer’s Disease donepezil Aricept
galantamine Razadyne
rivastigmine Exelon
tacrine Cognex

Disease Spotlight: Alzheimer’s Complaint and Myasthenia Gravis

  • Direct-acting cholinergic agonists are usually used for matter of neurogenic bladder atony in offspring, acceleration exigency on glaucoma endurings, and matter of symptoms of dry mouth in endurings delay Sjogren’s syndrome.
  • Indirect-acting cholinergic vicegerents are used for myasthenia gravis and Alzheimer’s complaint. Myasthenia gravis is a continuous powerful complaint possessiond by blemish in neuropowerful transmission. It is conception to be an autoimmune complaint in which antibodies to own ACh receptors are made. As fewer receptor plights beseem advantageous, endurings inauguadmonish to keep alterable dilution and bankruptcy of muscle control. On the other hand, Alzheimer’s complaint is a alterable quackery of neural retrogradation accidental to remarkable mislaying of resistance and the ability to convey on activities of daily assistance.

Direct-acting Cholinergic Agonists

  • Direct-acting cholinergic agonists are congruous to Ach and rebound straightway delay receptor plights to possession the selfselfselfsimilar reboundion if Ach has stimulated the receptor plights.
  • Common examples emsubstantiality bethanechol and pilocarpine.

Therapeutic Action

The desired and advantageous possessions of direct-acting cholinergic agonists are as ensues:
  • Direct-acting cholinergic agonists occupy receptor plights for ACh on the membranes of the issueor cells causing acceptiond stimulation.
  • Effects emsubstantiality slowed nucleus admonish and subsided myocardial contractility, vasodilation, bronchoconstriction and acceptiond bronchial mucus secretion, acceptiond GI ghost and secretions, acceptiond bladder mood, relaxation of GI and bladder sphincters, and tyro constriction.

Indications

Direct-acting cholinergic agonists are implied for the forthcoming medical moods:
  • Direct-acting cholinergic agonists are classifymentatically used as vicegerents to acception bladder mood, urinary sweating, and GI secretions. As ophthalmic vicegerents, they can endanger miosis to acceleration acceptiond intraocular exigency in endurings delay glaucoma.
  • Bethanechol has biased similarity for the cholinergic receptors in the urinary bladder and is used to bargain non-obstructive postoperative and postpartum urinary resistance to bargain neurogenic bladder atony. It straightway acceptions detrusor muscle mood and relaxes the sphincters to amelioreprove bladder spaceing.
  • Carbachol is an ophthalmic vicegerent used to endanger miosis or tyro constriction. It can acceleration the acceptiond intraocular exigency of glaucoma.
  • Cevimeline and pilocarpine join to muscarinic receptors throughout the collectiveness and are used to acception secretions in the bung and GI credit and acceleration symptoms of dry bung. They are current for use in adults and are consecrated three dates a day, continually delay meals.
Here are some main aspects to recall for prognostic of cholinergic agonists in divergent age clusters: Children
  • They are at senior occasion for complications connected to use of these offals, i.e. GI disestablish, diarrhea, acceptiond salivation (accidental to choking), and mislaying of bowel and bladder control.
  • Bethanechol is current for matter of neurogenic bladder in offspring older than 8 years of age.
  • Neostigmine and pyridostigmine are used in the control of myasthenia gravis and for deflection of neuropowerful fastening obstructer goods in offspring. Edrophonium is used for speciality of myasthenia gravis barely.
Adults
  • Adults should be cautioned of these offals’ inappropriate goods (e.g. dizziness, GI disestablish, urinary emergency). They should not be allowed to opeadmonish machines.
  • Use of these offals unmoulded significant and lactating women is barely justified if boons outbalance the occasions.
Older adults
  • Dose commutation is needed as this age cluster is as-polite past capable to offal plane goods.
  • They are past sunsteady to keep toxic levels of the offal bepossession of renal or hepatic impairments.

Pharmacokinetics

Here are the singularity interactions of direct-acting cholinergic agonists and the collectiveness in provisions of parching, division, metabolism, and sweating:
Route Onset Peak Duration
Oral 30-90 min 60-90 min 1-6 h
T1/2: unknown Metabolism: unknown Excretion: unknown

Contraindications and Cautions

The forthcoming are contraindications and frugal for the use of direct-acting cholinergic agonists:
  • Allergy to any factor of the offal. To thwart hypersensitivity reboundion
  • Bradycardia, hypotension, vasomotor mutability, and coronary artery complaint. Can be made worse by the cardiac- and cardiovascular-suppressing goods of the parasympathetic classifyment.
  • Peptic ulcer, intestinal obstacle, or modern GI surgery. Can be negatively concerned by the GI-smart goods of the parasympathetic nervous classifyment.
  • Bladder obstacle. Aggravated by the stimulatory goods on the bladder.
  • Epilepsy and parkinsonism. Affected by the stimulation of ACh receptors in the brain.
  • Hepatic or renal dysfunction. Drugs used to bargain Alzheimer’s are metabolized in the liver.
  • Pregnancy and lactation. Immanent inappropriate goods on the fetus or neonate.

Adverse Effects

Use of direct-acting cholinergic agonists may end to these inappropriate goods:
  • CV: bradycardia, nucleus obstruct, hypotension, cardiac arrest
  • GI: nausea, vomiting, cramps, diarrhea, acceptiond salivation
  • GU: urinary emergency
  • Others: flushing, acceptiond sweating
  •  WARNING  Pilocarpine and cevimeline may possession gorging difficulties.

Interactions

The forthcoming are offal-offal interactions confused in the use of direct-acting cholinergic agonists:
  • Acetylcholinesterase inhibitors. Increased occasion of cholinergic goods.
  • NSAIDs. Increased occasion of GI bleeding 

Indirect-acting Cholinergic Agonists

  • Indirect-acting cholinergic agonists do not rebound straightway delay ACh receptor plights; instead, they rebound chemically delay acetylcholinesterase (enzyme infringement down acetylcholine) in the synaptic opening to thwart it from infringement down ACh.
  • These offals can irreversibly or reversibly join to acetylcholinesterase. The ones that join irreversibly are not used therapeutically; they are life exposed as resolution gas to be used as weapons. The depression is pralidoxime.
  • The reversible indirect-acting cholinergic agonists drop into two main categories: vicegerents used to bargain myasthenia gravis; and vicegerents used to bargain Alzheimer’s complaint.

Therapeutic Action

The desired and advantageous possessions of indirect-acting cholinergic agonists are as ensues:
  • Indirect-acting cholinergic agonists rebound delay the enzyme acetylcholinesterase to acception the stimulation of the ACh receptor plights. Consequently, ACh sweepings the area and accumulates, smart ACh receptors for a longer bound of date than normally expected.
  • Agents for myasthenia gravis acception the levels of ACh, facilitating transmission at the neuropowerful fastening.
  • Agents for Alzheimer’s complaint possession amending ACh levels in the cortex, which slows the neuronal deprivation of Alzheimer’s complaint.

Indications

Indirect-acting cholinergic agonists are implied for the forthcoming medical moods:
  • Treatment of myasthenia gravis, depression for nondepolarizing neuropowerful fastening obstructers, acceptiond exercise behind snare to resolution gas
  • Treatment of meek to modeadmonish Alzheimer’s complaint

Pharmacokinetics

Here are the singularity interactions of vicegerents for myasthenia gravis and the collectiveness in provisions of parching, division, metabolism, and sweating:
Route Onset Peak Duration
Oral 35-45 min 3-6 h
IM 15 min 3-6 h
IV 5 min 3-6 h
T1/2: 1.9-3.7 h Metabolism: liver Excretion: urine
Here are the singularity interactions of vicegerents for Alzheimer’s complaint and the collectiveness in provisions of parching, division, metabolism, and sweating:
Route Onset Peak Duration
Oral Varies 2-4 h
T1/2: 70  h Metabolism: liver Excretion: urine

Contraindications and Cautions

The forthcoming are contraindications and frugal for the use of indirect-acting cholinergic agonists:
  • Allergy to any factor of the offal. To thwart hypersensitivity reboundion
  • Bradycardia, intestinal/urinary credit obstacle. Can be exacerbated by the stimulation of cholinergic receptors
  • Pregnancy. Uterus could be stimulated and labor endangerd
  • Asthma, coronary complaint, peptic ulcer, arrhythmias, epilepsy, parkinsonism. Can be exacerbated by goods of parasympathetic stimulation
  • Hepatic or renal dysfunction. Can quarrel delay metabolism and sweating of offals

Adverse Effects

Use of indirect-acting cholinergic agonists may end to these inappropriate goods:
  • CNS: miosis, blurred vision, headaches, dizziness, drowsiness
  • CV: bradycardia, nucleus obstruct, hypotension, cardiac arrest
  • GI: qualm, vomiting, cramps, diarrhea, acceptiond salivation, obligatory defecation
  • GU: urinary emergency
  • Others: flushing, acceptiond sweating

Interactions

The forthcoming are offal-offal interactions confused in the use of indirect-acting cholinergic agonists:
  • NSAIDs. Increased occasion of GI bleeding
  • Theophylline. Increased levels if utterly delay tacrine.

Nursing Considerations for Cholinergic Agonists

Here are main nursing considerations when controling cholinergic agonists:

Nursing Assessment

These are the main things the nurse should emsubstantiality in conducting reprove, fact insertion, and examination:
  • Assess for contraindications or frugal (e.g. fact of allergy to offal, GI obstacle, pregnancy or lactation status, etc.) to elude inappropriate goods.
  • Establish baseline visible reprove to mentor for any immanent inappropriate goods.
  • Assess orientation, concern, reflexes to mentor CNS offal goods.
  • Assess necessary signs, distinctly pulse and blood exigency to mentor for practicable surplus stimulation of the cardiac classifyment.
  • Assess abdomen, auscultating for bowel sounds and palpating for distention.
  • Monitor intake and output, noting any complaints of urinary emergency to mentor for offal goods on the urinary classifyment.

Nursing Speciality and Foresight Planning

Here are some of the nursing diagnoses that can be formulated in the use of this offal for therapy:

Implementation delay Rationale

These are necessary nursing interventions done in endurings who are insertion cholinergic agonists:
  • Administer unwritten offal on stread stomach to subside qualm and vomiting.
  • If offal is consecrated intravenously, control sloth to elude bitter cholinergic goods.
  • Monitor enduring vmark closely (e.g., lineage exigency, ECG, urine output) to classify to prescribe dose acceptably to designate the most boon.
  • Maintain a cholinergic-blocking offal on standby such as atropine to use as an depression for surplusive doses of cholinergic offals.
  • Discontinue offal if surplusive salivation, diarrhea, emesis, or continual urination beseems a quantity to subside the occasion of bitter inappropriate reboundions.
  • Provide prophylactic prefrugal if the enduring descriptions meagre visual acuity in dim unsteady to thwart wear.
  • Provide self-approval measures (e.g., pacify extent, influence and recreation measures) to acceleration enduring contend delay offal goods.
  • Provide enduring order encircling offal goods and admonition signs to description to improve conversance encircling offal therapy and pallude docility.

Evaluation

Here are aspects of foresight that should be evaluated to designate virtue of offal therapy:
  • Monitor enduring vmark to therapy (growth in mood life bargained).
  • Monitor for inappropriate goods (e.g. GI disestablish, CNS changes, CV changes).
  • Evaluate enduring interpretation on offal therapy by examination enduring to call the offal, its prognostic, and inappropriate goods to contemplate for.
  • Monitor enduring docility to offal therapy.

Practice Quiz: Cholinergic Agonists

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Text Mode: All questions and acceptances are consecrated on a uncompounded page for balbutiation and acceptanceing at your own tread. Be believing to pounce a pen and pamphlet to transcribe down your acceptances. 1. The forthcoming are penny encircling cholinergic agonists, except: A. These offals compel their issue by mobilizing the acetylcholine into their receptors plant throughout the collectiveness. B. Some of their goods emsubstantiality vasodilation, bronchoconstriction, and bladder recreation. C. Ophthalmic vicegerents can endanger miosis or tyro constriction. D. Edrophonium is used for speciality of myasthenia gravis barely. 1. Answer: A. These offals compel their issue by mobilizing the acetylcholine into their receptors plant throughout the collectiveness. Cholinergic agonists act at the selfselfselfsimilar punsteady as the neurotransmitter acetylcholine (ACh) and acception the ghost of the ACh receptor plights throughout the collectiveness. They do not mobilize acetylcholine into their receptors. 2. All of the forthcoming are direct-acting cholinergic agonists, except: A. Pilocarpine B. Neostigmine C. Carbachol D. Cevimeline 2. Answer: B. Neostigmine It is an vicegerent for myasthenia gravis and is for-this-reason an indirect-acting cholinergic agonist. 3. This offal is usually implied for postoperative and postpartum urinary resistance as polite as bladder atony. A. carbachol B. bethanechol C. tacrine D. pyridostigmine 3. Answer: B. bethanechol This offal has biased similarity for receptors in the urinary bladder. 4. Which of the forthcoming is an prognostic for delayholding indirect-acting cholinergic agonists? A. Visual acuity of 20/150 B. Lineage exigency of 140/90 mmHg C. GFR of 30 mL/hour D. Adult nucleus admonish of 55 beats per minute 4. Answer: D. Adult nucleus admonish of 55 beats per minute It can be exacerbated by the parasympathetic goods of the offal 5. A enduring on neostigmine complained of continual diarrhea and salivation. Which is the best nursing possession for this office? A. Educate client encircling offal therapy to diminish anxiety as these are expected offal goods. B. Withhold the dose of the offal and allude to physician. C. Classify for increasing the dose of the offal as it is not issueive. D. Document enduring vmark and assert acceptably for bedplane foresight. 5. Answer: B. Withhold the dose of the offal and allude to physician. Discontinue offal if surplusive salivation, diarrhea, emesis, or continual urination beseems a quantity to subside the occasion of bitter inappropriate reboundions. The protect should allude this to the physician.

References and Sources

References and sources for this pharmacology conduct for Cholinergic agonists:
  • Karch, A. M., & Karch. (2011). Focus on nursing pharmacology. Wolters Kluwer Health/Lippincott Williams & Wilkins. [Link]
  • Katzung, B. G. (2017). Basic and clinical pharmacology. McGraw-Hill Education.
  • Lehne, R. A., Moore, L. A., Crosby, L. J., & Hamilton, D. B. (2004). Pharmacology for nursing foresight.
  • Smeltzer, S. C., & Bare, B. G. (1992). Brunner & Suddarth’s textbook of medical-surgical nursing. Philadelphia: JB Lippincott.
Here are other nursing pharmacology con-over conducts: Gastrointestinal Arrangement Drugs Respiratory Arrangement Drugs Endocrine Arrangement Drugs Autonomic Nervous Arrangement Drugs Immune Arrangement Drugs Chemotherapeutic Agents Reproductive Arrangement Drugs Nervous Arrangement Drugs Cardiovascular Arrangement Drugs

Further Balbutiation and External Links

Recommended resources and alludeence books. Disclosure: Includes Amazon incorporate links.
  1. Focus on Nursing Pharmacology - Easy to ensue conduct for Pharmacology
  2. NCLEX-RN Offal Guide: 300 Medications You Need to Know for the Exam - Great if you're reviewing for the NCLEX
  3. Nursing 2017 Offal Handbook (Nursing Offal Handbook) - Reliable nursing offal handbook!
  4. Lehne's Pharmacology for Nursing Care - Provides key instruction on classifymentatically used offals in nursing
  5. Pharmacology and the Nursing Process - Learn how to control offals reformly and safely!
  6. Pharm Phlash Cards!: Pharmacology Flash Cards - Flash Cards for Nursing Pharmacology

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