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34 Cards in this Set
- Front
- Back
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What are the oldes known anticholinergic drugs?
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Belladonna alkaloids
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What are the belladonna alkaloids?
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Atropine & Scopolamine
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What is the chemistry of atropine & scoploamine?
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Tertiary amines which contain an ester linkage. Levo isomers are active
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What are the synthetic anticholinergics?
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Homatropine & ipratropium
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What is the chemistry of synthetic anticholinergics (homatropine & ipratropium)?
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Related to belladonnas & most are tert or quad amines
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Describe the absorption, distribution, & elimin of natural & tertiary synthetic antichol.
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Well absorbed in GI, Scopolamine through the skin, widely distributed, cross BBB & placenta
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Describe the absorption & distribution of quad amine synthetic antichol.
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Poorly absorbed, doessn't cross BBB (no CNS effects)
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How are antichol metabolized & excreted?
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Metabolized in liver by CYP450 & excreted into urine
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What is the mech of action for antichol?
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Competitive antag; binds to mAChR. mAChR>nAChR
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Generally, how does atropine affect organ systems?
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Not equally sensitive to all systems. Salivary is highly sensitive & gastric is relatively insensitive
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How does atropine affect the CNS?
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Minimal effect @ therapeutic doses. Intermed=drowsiness, impaired memory. Higher=confusion, excitement, hallucination, convulsions. Way higher=paralysis, coma, respiratory fail, & heart fail
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How does scopolamine affect the CNS?
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More CNS effects. Similar to atropine but w/ reduced REM sleep. Used to prevent motion sickness
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How does atropine affect the Pupillary sphincter?
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Mydriasis (pupil dilation)
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How does atropine affect lacrimal glands?
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Dec tear secretion
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How does atropine affect the Ciliary m?
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Cycloplegia (lens fixed for far vision), photophobia, blurred vision, inc resistance to aq outflow
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How does atropine affect the heart?
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Transient dec in HR w/ low dose. Tachycardia w/ no change on BP w/ higher doses
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How does atropine affect the vasculature?
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No affect w/ therapuetic doses. Cutaneous vasodilation w/ toxic doses; atropine flush
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How does atropine affect the respiratory system?
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Bronchodilation (M3)- greater in COPD , reduced secretions (M2)
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How does atropine affect the digestive system?
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Inhibits salivation, reduces gastric, pancreatic, intestinal, biliarysecretion @ larger doses. Also reduces GI tone
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How does atropine affect the urinary tract?
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Dec tone & amplitude of bladder & ureter contractions-> retention
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How does atropine affect sweat glands?
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Lose dose=anhidrosis (hot dry skin). High dose=inc body temp (children sensitive).
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What are the clinical uses of anticholinergics in opthalmology?
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Local application. Atropine/scopolamine have long duration of action (~10d). *Tropicamide lasts ~6hrs. Produces cycloplegia, mydriasis
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What are the clinical uses of anticholinergics in respiratory disorders?
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Ipratropium= combined w/ b2 agonist to use as aerosol for COPD & asthma. Tiotropium=COPD. Longer duration
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What are the clinical uses of anticholinergics in urology?
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Used to treat overactive bladder. Oxybutin, tolterodine, solifenacin. May cause *dry mouth, cognitive impairment, tachy, &urinary retention. Contraindicated for closed angle glaucoma. Tert amines
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What are the clinical uses of anticholinergics in digestive tract?
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Used as adjunct therapy for peptic ulcers, irritable bowel, acute pancreatitis. Methscopolamine & *Pirenzepine
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What are the clinical uses of anticholinergics in CNS system?
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Parkinson's (benztropine) & motion sickness (scopolamine)
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What are the clinical uses of anticholinergics in CV system?
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Limited use. Acute MI- inc HR, BP, CO. Treat bradycardia & syncope
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What are the clinical uses of anticholinergics in anesthesiology?
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Premedication before induction; reduce saliva & respiratory
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What are the clinical uses of anticholinergics as an antidote?
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For anticholinesterase (insecticide, nerve gas) & mushroom poisoning.
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What are the effects of Dicyclomine?
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Dec GI spasm, replaced by oxybutynin
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What are the effects of Glycopyrrolate?
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Oral, dec GI motility. Parenteral, used during surgery
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What are the effects of Propantheline?
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Widely used for ulcer & sometimes bladder. Ganglionic blocker. NMJ blockade
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What are the contraindications & drug interactions for anticholinergics?
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Close angled glaucoma, GI obstruction. Caution w/ open-angled glaucoma, cardiac disease or prostatic hypertrophy. Antihistaminics, phenothiazines, & antidepressants can amplify effects
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What are the adverse effects of anticholinergics?
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From plants of Solanaceae family (Jimson weed, stinkweed, nightshade)-> blind, mad, red, dry, hot
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