Updated: 12/16/2018

Cholinomimetic Agents

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Direct agonists
  • Most direct agonists are resistant to acetylcholinesterase (AChE)  
    • thereby prevents breakdown of agonist
    • increases cholinergic effect
Direct Agonists Uses Mechanism of Action
Methacholine • Challenge test for bronchial airway hyperactivity/asthma 
• Rapid onset of contraction of smooth muscles in the airways and increases tracheobronchial secretions
• Slightly resistant to acetylcholine-esterase (AChE)
Pilocarpine • Management of glaucoma
• Contracts the pupillary sphincter (miosis) and ciliary muscle (improved accommodation)
• Lowers intraocular pressure by reducing resistance to aqueous humor outflow
• Resistant to AChE
Bethanechol  • Acute postoperative and postpartum urinary retention
• Neurogenic ileus
• Causes bladder contractions which initiates urination
• stimulates gastric motility and tone restoring peristalsis
• Resistant to AChE
Carbachol • Lowers intraocular pressure treating glaucoma
• Pupillary contraction
• Stimulates muscarinic receptors causing miosis 
• Resistant to AChE

 

Indirect Agonists (Cholinesterase Inhibitors)
  • Mechanism of action
    • all work by inhibiting ACHE 
    • thereby preventing the degradation of ACH prolonging its effects
Indirect Agonist
Uses
Notes

Physostigmine 

• Glaucoma
• Atropine overdose or Atropa belladonna (deadly nightshade) ingestion
• CNS penetration
• Absorbs well on all bodily surfaces 
Neostigmine • Postoperative and neurogenic ileus and urinary retention
• Myasthenia gravis
• Reversal of neuromuscular junction blockade (postoperative)

• No CNS penetration
Pyridostigmine  • Myasthenia gravis
• No CNS penetration
Edrophonium • Diagnosis of myasthenia gravis 
• Ileus
• Arrhythmias
• Extremely short lived (5 - 15 min)
Echothiophate • Glaucoma
• Long-lasting (100 hours)
• No CNS penetration
• Insecticides: malathion is safe in humans but parathion is harmful and both can penetrate the CNS
 
Cholinesterase Inhibitor Poisoning
  • Cholinesterase poisoning symptoms 
    • due to ingestion of parathion or cholinesterase inhibitors
    • symptoms result from the overstimulation of systemic cholinergic receptors
      • Glands: sweating, salivation, and lacrimation
      • GI and GU: diarrhea, abdominal cramping, urination
      • Heart: bradycardia
      • Respiratory: bronchospasm
      • Musculoskeletal: skeletal muscle overexcitation
      • Eye: miosis
    • Mnemonic: Diarrhea, Urination, Miosis, Bradycardia, Emesis, Lacrimation, Lethargy, and Salivation
  • Treatment
    • atropine: blocks muscarinic receptors
    • pralidoxime: regenerated AChE
 

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Questions (5)
Lab Values
Blood, Plasma, Serum Reference Range
ALT 8-20 U/L
Amylase, serum 25-125 U/L
AST 8-20 U/L
Bilirubin, serum (adult) Total // Direct 0.1-1.0 mg/dL // 0.0-0.3 mg/dL
Calcium, serum (Ca2+) 8.4-10.2 mg/dL
Cholesterol, serum Rec: < 200 mg/dL
Cortisol, serum 0800 h: 5-23 μg/dL //1600 h:
3-15 μg/dL
2000 h: ≤ 50% of 0800 h
Creatine kinase, serum Male: 25-90 U/L
Female: 10-70 U/L
Creatinine, serum 0.6-1.2 mg/dL
Electrolytes, serum  
Sodium (Na+) 136-145 mEq/L
Chloride (Cl-) 95-105 mEq/L
Potassium (K+) 3.5-5.0 mEq/L
Bicarbonate (HCO3-) 22-28 mEq/L
Magnesium (Mg2+) 1.5-2.0 mEq/L
Estriol, total, serum (in pregnancy)  
24-28 wks // 32-36 wks 30-170 ng/mL // 60-280 ng/mL
28-32 wk // 36-40 wks 40-220 ng/mL // 80-350 ng/mL
Ferritin, serum Male: 15-200 ng/mL
Female: 12-150 ng/mL
Follicle-stimulating hormone, serum/plasma Male: 4-25 mIU/mL
Female: premenopause: 4-30 mIU/mL
midcycle peak: 10-90 mIU/mL
postmenopause: 40-250
pH 7.35-7.45
PCO2 33-45 mmHg
PO2 75-105 mmHg
Glucose, serum Fasting: 70-110 mg/dL
2-h postprandial:<120 mg/dL
Growth hormone - arginine stimulation Fasting: <5 ng/mL
Provocative stimuli: > 7ng/mL
Immunoglobulins, serum  
IgA 76-390 mg/dL
IgE 0-380 IU/mL
IgG 650-1500 mg/dL
IgM 40-345 mg/dL
Iron 50-170 μg/dL
Lactate dehydrogenase, serum 45-90 U/L
Luteinizing hormone, serum/plasma Male: 6-23 mIU/mL
Female: follicular phase: 5-30 mIU/mL
midcycle: 75-150 mIU/mL
postmenopause 30-200 mIU/mL
Osmolality, serum 275-295 mOsmol/kd H2O
Parathyroid hormone, serume, N-terminal 230-630 pg/mL
Phosphatase (alkaline), serum (p-NPP at 30° C) 20-70 U/L
Phosphorus (inorganic), serum 3.0-4.5 mg/dL
Prolactin, serum (hPRL) < 20 ng/mL
Proteins, serum  
Total (recumbent) 6.0-7.8 g/dL
Albumin 3.5-5.5 g/dL
Globulin 2.3-3.5 g/dL
Thyroid-stimulating hormone, serum or plasma .5-5.0 μU/mL
Thyroidal iodine (123I) uptake 8%-30% of administered dose/24h
Thyroxine (T4), serum 5-12 μg/dL
Triglycerides, serum 35-160 mg/dL
Triiodothyronine (T3), serum (RIA) 115-190 ng/dL
Triiodothyronine (T3) resin uptake 25%-35%
Urea nitrogen, serum 7-18 mg/dL
Uric acid, serum 3.0-8.2 mg/dL
Hematologic Reference Range
Bleeding time 2-7 minutes
Erythrocyte count Male: 4.3-5.9 million/mm3
Female: 3.5-5.5 million mm3
Erythrocyte sedimentation rate (Westergren) Male: 0-15 mm/h
Female: 0-20 mm/h
Hematocrit Male: 41%-53%
Female: 36%-46%
Hemoglobin A1c ≤ 6 %
Hemoglobin, blood Male: 13.5-17.5 g/dL
Female: 12.0-16.0 g/dL
Hemoglobin, plasma 1-4 mg/dL
Leukocyte count and differential  
Leukocyte count 4,500-11,000/mm3
Segmented neutrophils 54%-62%
Bands 3%-5%
Eosinophils 1%-3%
Basophils 0%-0.75%
Lymphocytes 25%-33%
Monocytes 3%-7%
Mean corpuscular hemoglobin 25.4-34.6 pg/cell
Mean corpuscular hemoglobin concentration 31%-36% Hb/cell
Mean corpuscular volume 80-100 μm3
Partial thromboplastin time (activated) 25-40 seconds
Platelet count 150,000-400,000/mm3
Prothrombin time 11-15 seconds
Reticulocyte count 0.5%-1.5% of red cells
Thrombin time < 2 seconds deviation from control
Volume  
Plasma Male: 25-43 mL/kg
Female: 28-45 mL/kg
Red cell Male: 20-36 mL/kg
Female: 19-31 mL/kg
Cerebrospinal Fluid Reference Range
Cell count 0-5/mm3
Chloride 118-132 mEq/L
Gamma globulin 3%-12% total proteins
Glucose 40-70 mg/dL
Pressure 70-180 mm H2O
Proteins, total < 40 mg/dL
Sweat Reference Range
Chloride 0-35 mmol/L
Urine  
Calcium 100-300 mg/24 h
Chloride Varies with intake
Creatinine clearance Male: 97-137 mL/min
Female: 88-128 mL/min
Estriol, total (in pregnancy)  
30 wks 6-18 mg/24 h
35 wks 9-28 mg/24 h
40 wks 13-42 mg/24 h
17-Hydroxycorticosteroids Male: 3.0-10.0 mg/24 h
Female: 2.0-8.0 mg/24 h
17-Ketosteroids, total Male: 8-20 mg/24 h
Female: 6-15 mg/24 h
Osmolality 50-1400 mOsmol/kg H2O
Oxalate 8-40 μg/mL
Potassium Varies with diet
Proteins, total < 150 mg/24 h
Sodium Varies with diet
Uric acid Varies with diet
Body Mass Index (BMI) Adult: 19-25 kg/m2
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(M1.PH.218) A 16 year-old female is being evaluated for shortness of breath. For the last year she has had shortness of breath and subjective wheezing with exercise and intermittent coughing at night. She reports waking up from sleep coughing 1-2 times per month. She now skips gym class because of her symptoms. She denies any coughing, chest tightness, or shortness of breath on the day of her visit. On exam, her lungs are clear to auscultation bilaterally, with normal inspiratory to expiratory duration ratio. Her pulmonary function tests (PFTs) show normal FEV1 and FVC based on her age, gender, and height. She is told to inhale a medication, and her PFTs are repeated, now showing a FEV1 79% of her previous reading. The patient is diagnosed with asthma. Which of the following medications was used to diagnose the patient? Review Topic

QID: 101884
1

Methacholine

84%

(94/112)

2

Pilocarpine

1%

(1/112)

3

Bethanechol

8%

(9/112)

4

Carbachol

3%

(3/112)

5

Physostigmine

3%

(3/112)

M1

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