Cholinergic Blocking Flashcards
Cholinergic-Blocking Drugs
Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system (PSNS)
Also known as anticholinergics, parasympatholytics, and antimuscarinic drugs
Mechanism of action of cholinergic-blocking drugs
Competitive antagonists
Compete with ACh for binding at muscarinic receptors in the PSNS
- As a result, ACh is unable to bind to thereceptor site and cause a cholinergic effect.
When these drugs bind to receptors, they inhibit nerve transmission at these receptors.
Cholinergic-Blocking Drugs: Natural Plant Alkaloids
- Atropine sulphate
- scopolamine hydropbromide
Cholinergic-Blocking Drugs: Synthetic and semisynthetic
glycopyrrolate
oxybutynin (Ditropan®)
tolterodine (Detrol®)
Drug Effects; Cardiovascular
- Small doses: decreased heart rate
- doses: increased heart rate
Drug Effects; Central nervous system (CNS)
Small doses: decreased muscle rigidity and tremors
Large dose: drowsiness, disorientation, hallucinations
Drug effects; EYE
Dilated pupils (mydriasis)
Decreased accommodation caused by paralysis of ciliary muscles (cycloplegia)
Drug effects; Gastrointestinal (GI)
Relaxed smooth muscle tone of GI tract
Decreased intestinal and gastric secretions
Decreased motility and peristalsis
Drug Effects; Genitourinary (GU)
Relaxed detrusor muscle
Increased constriction of internal sphincter
Result: urinary retention
Drug Effects; Glandular
Decreased sweating
drug effects; Respiratory
Decreased bronchial secretions
Indications: Central Nervous System
Decreasing muscle rigidity and muscle tremors
Parkinson’s disease (becoming less trendy)
Drug-induced extrapyramidal reactions such as those associated with antipsychotic drugs
Indications: Cardiovascular
Affects the heart’s conduction system.
- Low doses: slow the heart rate
- High doses:, block inhibitory vagal effects on sinoatrial and atrioventricular node pacemaker cells
- Results in increased heart rate
Indications: Cardiovascular - atropine
Used primarily for cardiovascular disorders
Diagnosis of sinus node dysfunction
Symptomatic second-degree heart block
Severe sinus bradycardia with hemodynamic compromise (advanced life support)
Indications: Respiratory
Blocking the cholinergic stimulation of the PSNS allows unopposed action of the sympathetic nervous system.
Indications: Respiratory, Results
Decreased secretions from the nose, mouth, pharynx, and bronchi
Relaxed smooth muscles in the bronchi and bronchioles
Decreased airway resistance
Bronchodilation
Indications: Respiratory, Cholinergic blockers are used to treat:
Exercise-induced bronchospasms
Asthma
Chronic obstructive pulmonary disease
Indications: Gastrointestinal
The PSNS controls gastric secretions and smooth muscles that produce gastric motility.
Indications: Gastrointestinal, Blockade of PSNS results in:
Decreased secretions
Relaxation of smooth muscle
Decreased GI motility and peristalsis
Indications: Gastrointestinal, GI drugs are used to treat what?
Irritable bowel disease
GI hypersecretory states
Indications: Genitourinary
- Reflex neurogenic bladder
- Incontinence
Contraindications
Known drug allergy
Angle-closure glaucoma
Acute asthma or other respiratory distress
Myasthenia gravis
Acute cardiovascular instability
GI or GU tract obstruction (e.g., benign prostatic hyperplasia [BPH]) or illness