Pharm – drugs that decrease ACh – Flashcards
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Antimuscarinics
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DG's are BATSHIT Crazy! - D icyclomine - G lycopyrrolate - B enztropine - A tropine - T ropicamide - S copolamine - H omatropine - I pratropium - T olterodine - C yclopentolate
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Scopolamine
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Motion sickness Patch AE: drowsiness
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Tropicamide, cyclopentolate, homatropine
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Fast but short acting mydriatic agents
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Ipratropium
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quarternary amine Inhalation for bronchodilation [COPD] Tiotropium = similar but longer acting
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Tolterodine
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For overactive bladder [urinary frequency, urgency, nocturia, incontinence] AE: dry mouth, blurred vision Contraindicated: narrow angle glaucoma
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Dicyclomine
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Relaxes intestinal smooth muscle for irritable bowel symptoms
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Glycopyrrolate
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Inhibit secretions pre-op Prevent excessive sweating Prevent muscarinic AE's if given neostigmine to reverse neuromuscular block
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Benztropine
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For EPS symptoms in Parkinson's or antipsychotics
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Other drugs with anti-muscarinic properties
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Antihistamines Antidepressants Phenothiazine antipsychotics
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Ganglionic blockers
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Depolarizing - nicotinic agonists Non-depolarizing - curare No longer used - Hexamethonium -Trimethaphan - Mecamylamine
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Hexamethonium
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First effective anti HTN No longer used Poor absorption, ANS AE's
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Trimethaphan
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Used for acute aortic dissection - lowers BP - prevents sympathetic reflex no longer used
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Mecamylamine
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Orally active CNS side effects Was used for HTN, to improve GI symptoms For Tourettes syndrome
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Neuromuscular blockers
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Antagonize nAChR's [eye muscles --> extremities --> trunk --> intercostal muscles --> diaphragm] Depolarizing - Succinylcholine Non depolarizing
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Succinylcholine
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Slow inactivation Prolonged duration of action Phase I = initial activation causes persistent depolarization that leads to receptor blockade and Na+ channel inactivation Phase 2 = nicotinic receptors inactivate
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Succinylcholine AEs
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- Apnea - Hyperkalemia [K+ release from muscle via nAChR upregulation] - increased IOP - Increased gastric pressure - Malignant hyperthermia
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Neuromuscular blocker pharmacokinetics
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Eliminated by kidney = long T1/2 and duration Eliminated by liver = shorter T1/2 and duration Hydrolyzed by plasma esterase = shortest T1/2 and duration
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Long acting neuromuscular blockers (5)
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1-2 hours - Tubocurarine = blocks autonomic ganglia - metocurine = blocks autonomic ganglia - Pancuronium = cardiostimulatory - Pipecuronium - Doxacurium
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Intermediate acting neuromuscular blockers (4)
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20-60 min - Vecuronium - Atracuronium - Cisatracuronium - Rocuronium
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Short acting neuromuscular blockers (2)
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5-15 min - Succinylcholine = stimulates autonomic ganglia - Mivacurium
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Neuromuscular blockers with histamine release
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High - Tubocurarine Moderate - Metocurine Low - Atracuronium - Mivacurium Slight - Cisatracurium - Succinylcholine
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Neuromuscular blockers with significant metabolism
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Kidney deacetylation - Pancuronium - Pipecuronium Liver and kidney deacetylation - Vecuronium Spontaneous hydrolysis - Atracurium - Cisatracurium Liver elimination - Rocuronium
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Reversal of neuromuscular blockade
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Cholinesterase inhibitor [neostigmine] To prevent overshoot: antimuscarinic [atropine or glycopyrrolate] BUT - give antimuscarinic first, THEN AChEI
