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30 Cards in this Set
- Front
- Back
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12 Muscarinic Actions
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1 GI secretion & motility
2 decreased heart rate 3 miosis (pupilary constriction) 4 ciliary muscle constriction (for accommodation) 5 bronchial constriction & secretion 6 detrusor contraction 7 sphincter relaxation (except lower esophageal) 8 sweating 9 salivation 10 lacrimation 11 blood vessel dilation 12 memory |
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5 Muscarinic Agonists
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1 Cevimeline
2 Pilocarpine 3 Methacholine 4 Carbachol 5 Bethanechol |
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2 Muscarinic Agonists that cross into CNS
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Cevimeline
Pilocarpine |
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3 Muscarinic Agonists that will not cross BBB
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Methacholine
Bethanechol Carbachol |
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Peripheral Cholinesterase Inhibitors
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Pyridostigmine
Physostigmine (crosses BBB) Ambenonium Neostigmine Demecarium Edrophonium |
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Irreversible Cholinesterase Inhibitors
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Organophosphates: what class are they in and how is it different from others in it's class?
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Clinical Uses of Muscarinic Agonists
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glaucoma
urine retention dx of asthma xerostomia |
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Centrally Acting Cholinesterase Inhibitors & Theory of Action
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What type of drugs are these? The idea was to improve cholinergic activity as to improve memory, not very effective though & hepatotoxicity & some peripheral effects
1. Tacrine 2. Donepezil 3. Rivastigmine 4. Galantamine |
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Cholinesterase Inhibitory Toxicity
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SLUDGE
salivation, lacrimation, urination, defecation, GI upset, emesis |
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Edrophonium: class, indication, and duration of action
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cholinesterase inhibitor - Carbamate?
used to test for myasthenia gravis or see if treatment is inadequate (in stroke, no effect) used for reversal of neuromuscular blockade by non depolarizing muscle relaxants very short duration (minutes) |
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6 Adverse Effects of Muscarinic Agonists
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Adverse effects of what type of agent?
SLUDGE Salivation Lacrimation Defecation GI Distress Emesis-Nausea Diarrhea Miosis Spasm of accomodation --> headache Breathing difficulty Bradycardia |
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8 Contraindications of Muscarinic Agonists
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Contraindications of what type of agent?
1 Gl obstruction 2 Bladder obstruction 3 Asthma 4 Ulcer 5 Coronary artery disease 6 Hyperthyroidism 7 Parkinson's disease 8 Seizures |
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Physostigmine: chemical quality and place of action
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cholinesterase inhibitor
tertiary amine readily penetrates CNS treats antimuscarinic toxicity |
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What saves an enzyme, NOT the patient, after being bound by an organophosphate?
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2PAM (pralidoxime chloride)
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Describe Organophosphate toxicity
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What type of toxicity is described?
1. onset 2 wks following exposure 2. demyelination--> flaccid & spastic paralysis 3. toxicity is independent of inhibition of cholinesterase 4. recovery rare |
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3 Examples of Organophosphates & Indications
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What class of drugs are the following?
1. Echothiophate (tx for open-angle glaucoma) 2. Parathion, malathion (pro-drug instecticides, both(?) safe for humans) 3. Soman-nerve toxins (Vx), very lipid soluble |
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Tx of Cholinesterase Inhibitor Overdose
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1. Support respiration
2. Wash skin, gastric lavage 3. Atropine (anticholinergic) 4. 2PAM (*atropine first!) |
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Cholinesterase should be used with EXTREME caution in what kind of patient and why?
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Heart patients, the decrease in heart rate could be exaggerated
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Muscarinic Antagonists: how they work and 5 examples
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competitively block Ach @ muscarinic receptor
1. ATROPINE 2. Darifenacin 3. Oxybutynin 4. Scopolomine- prevent motion sickness 5. Tolterodine |
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Characteristics of Muscarinic Antagonists/Blockers
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Can't think-sedation & confusion
Can't see-dilated pupils (mydriasis) & blurred vision Can't pee-urinary retention Can't spit-dec salivation Can't sh**-dec GI secretion & motility But these will subside... Tolerance! Elderly- start small! |
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Uses of Musarinic Antagonists/Blockers
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1 Overactive bladder
2 Motion Sickness 3 Adjunct to anesthesia (dec secretion) 4 Organophosphate & mushroom poisoning 5 IBS 6 Bladder spasm 7 To dilate pupils (mydriasis) but --> dec vision |
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Contraindications for Muscarinic Blockers
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Small people (can't accomodate for decreased sweating)
Glaucoma, esp narrow angle (slams trebecular mesh) Prostatic hyperplasia (already have a hard time peeing!) Cardiac disease (response can be unexpected and exagerated!) |
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Cardiac effect of muscarinic blockers
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1. bradycardia (presynaptic receptors sense a dec in Ach so initially, they secrete more Ach, lowering hr)
2. tachycardia (high dose--blocks the Ach that the Vagus secretes) |
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Nicotine Agonist Responses
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1 inc hr & bp via adrenal gland
2 inc GI tone & motility (nausea & diarrhea) 3 CNS stimulation--more w increasing dose up to seizure, then depression due to tachyphylaxis 4 note lack of euphoria that seen w other addictive substances |
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Acute Nicotine Poisoning
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1 salivation, vomiting, diarrhea, headache, disturbed hearing
2 faintness, collapse, dec bp, weak pulse, difficult breathing 3 convulsions 4 depression & death |
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Tx of Acute Nicotine Poisoning
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1 gastric lavage (not ipecac-cardiotoxic)
2 O2 3 tx of shock as needed |
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Botulinum Toxin-indication, action, risk
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migraine, wrinkles, spasticity
inhibits Ach release black box: life threatening w spread from injection site |
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Depolarizing Neuromuscular Blockers: action, use, elimination, warning
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overstimulates neuromuscular junction (tachyphylaxis)
succinylcholine (very short acting--> use for intubation) pseudocholinesterase (some are poor biotransformers--RISK) if having problems, adding a cholinesterase would CAUSE MORE HARM |
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Succinylcholine Adverse Effects
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1 malignant hyperthermia (esp w halothane)
2 muscle fasciculation 3 hyperkalemia 4 prolonged contraction in myotonia and ALS pts |
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Non-depolarizing Neuromuscular Blockers: action, character, route, pattern of action, 6 examples
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Competitive receptor blockers
Long duration, titratable IV use only spare diaphragm, affect head & neck then limbs cholinesterases CAN reverse 1 Atracurium 2 Cisatracurium 3 Pancuronium 4 Rocuronium 5 Tubocurarine 6 Vecuronium |
