Term
| Major Effects of Cholinesterase Inhibitors |
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Definition
| increased GI motility & secretion; contraction of bladder & relaxation of urinary sphincter; bradycardia & hypotension; increased secretions; decreased intraocular pressure; stimulation of skeletal muscle (therapeutic doses) & paralysis of skeletal muscles (toxic doses); bronchoconstriction |
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Term
| Toxic Effects of Cholinesterase Inhibitors |
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Definition
| SLUDGE (salivation, lacrimation, urination, defecation, GI distress, emesis); skeletal muscle fasciculations; bradycardia, hypotension, shock; severe miosis; CNS stimulation & seizures followed by coma; demyelination of axons & neuropathies after chronic exposure |
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Term
| Treatment of Acute Cholinesterase Inhibitor Poisoning |
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Definition
| administer high doses of atropine (GOLD STANDARD); administer pralidoxime to reactivate enzyme (effective onlye with organo-phosphates); diazepam is useful for controlling seizures |
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Term
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Definition
| a disease characterized by fatigue and weakness of skeletal muscle progressing to complete paralysis; involves an autoimmune process directed against nicotinic receptors of motor end plate |
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Term
| Therapeutic Uses for edrophonium (Tensilon) |
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Definition
| diagnosis of myasthenia gravis; treatment of atony of bladder or GI tract (e.g. urine retention, paralytic ileus) |
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Term
| Therapeutic Uses for neostigmine (Prostigmin) |
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Definition
| treatment of myasthenia gravis; reversal of neuromuscular blockade by nondepolarizing neuromuscular blockers; treatment of atony of bladder of GI tract |
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Term
| Therapeutic Uses for pyridostigmine (Mestinon) |
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Definition
| treatment of myasthenia gravis; reversal of neuromuscular blockade by nondepolarizing neuromuscular blockers; used by Military to protect personnel against nerve aganets used in chemical warfare ("Pre-exposure Antidotal Enhancement") |
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Term
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Definition
| a test using edrophonium, a short-acting cholinesterase inhibitor, that helps in diagnosing myasthenia gravis; a transient improvement in muscle strength indicates a diagnosis of myasthenia gravis |
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Term
| Therapeutic Uses for echothiophate |
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Definition
| treatment of glaucoma; contracts ciliary muscle, putting tension on trabecular meshwork & increases outflow of aqueous humor through the canal of Schlemm |
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Term
| Therapeutic Uses for rivastigmine (Exelon), donepezil (Aricept), and galantamine (Reminyl) |
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Definition
| treatment of Alzheimer's Disease; raises levels of ACh and reverses cholinergic deficit, providing a modest improvement in cognitive ability |
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Term
| Therapeutic Uses for physostigmine (Eserine) |
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Definition
| treatment of poisoning with atropine or other antimuscarinic drugs |
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Term
| Contraindications in the Use of Cholinesterase Inhibitors |
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Definition
| asthma; bradycardia, hypotension, coronary artery disease; peptic ulcer disease; urinary or intestinal obstruction |
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Term
| edrophonium (Tensilon), neostigmine (Prostigmin), and pyridostigmine (Mestinon) |
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Definition
| reversible cholinesterase inhibitors; quaternary ammonium compounds that don't enter CNS; E is short acting (< 10 min) and is used in diagnosis of myasthenia gravis; N & P are longer acting and are used in treatment of myasthenia gravis; P also used by military to protect troops against nerve agents used in chemical warfare |
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Term
| physostigmine/eserine (Antilirium) |
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Definition
| reversible cholinesterase inhibitor, nonquaternary so it can enter CNS; treats poisoning with atropine or other antimuscarinic agents |
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Term
| organophosphate insecticides (parathion, malathion) |
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Definition
| used mainly in farming for insects but has toxic effects on humans; treat poisoning with atropine, pralidoxime |
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Term
| carbaryl (Carbamate Insecticides) |
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Definition
| very widely used insecticide; not absorbed through skin; signs & symptoms similar to cholinesterase inhibitors; treat poisoning with atropine - NOT pralidoxime (not useful)! |
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Term
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Definition
| very potent & toxic irreversible cholinesterase inhibitors; S&S's are typical of cholinesterase inhibitors; treat poisoning with atropine & pralidoxime |
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Term
| pralidoxime/2-PAM (Protopam) |
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Definition
| cholinesterase reactivator, chemically binds to phosphate group that inhibits enzyme and regenerates enzyme; antidote for organophosphate poisoning; MUST be used within 2 hrs following exposure; it DOES NOT work with carbamate insecticides (carbaryl) |
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Term
| Mechanism of Action of sildenafil (Viagra), vardenafil (Levitra), and tadalafil (Cialis) |
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Definition
| inhibition of cGMP PDE-5 that breaks down cGMP formed by NO-mediated activation of guanylcyclase, causing pronounced vasodilation in the penis, producing an erection |
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Term
| Side Effects & Toxicities caused by sildenafil, vardenafil, tadalafil |
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Definition
| hypotension with a reflex increase in heart rate; increase in heart rate may cause additional problems in pre-existing CVD; visual disturbances - impairment of blue/green color discrimination; auditory disturbances |
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Term
| Drug Interactions with sildenafil, vardenafil, tadalafil |
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Definition
| interacets with drugs that metabolize by CYP3A4 (i.e. erythromycin, ketaconazole, cimetidine); vasodilators, especially nitrates but also Ca-channel blockers; sympathomimetics (cocaine, amphetamines) |
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Term
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Definition
| toxin produced by Clostridium botulinium which prevents the release of ACh from nerve endings - both autonomic nerve endings and neuromuscular junctions; death results from diaphragmatic paralysis; locally injected neuromuscular blocker for treatment of ophthamalogic disorders, wrinkles, dystonia, and excessive sweating |
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Term
| Botulinum toxin poisoning |
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Definition
| lethal doses are very small; treat with aggressive symptomatic support, especially respiratory function plus administration of antibodies to the toxin |
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Term
| Pharmacological Effects of Anticholinergic (antimuscarinic) drugs |
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Definition
| drying of secretions; decrease tone & motility of GI tract; relaxation of bladder and urine retention; bronchodilation; mydriasis (dilation of pupil) with cycloplegia (loss of acomodation) and increase in intraocular pressure; increased heart rate; sedation & amnesia at low doses; excitation & seizures at toxic doses |
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Term
| Common Therapeutic Uses of Anticholinergric Drugs |
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Definition
| treats GI disorders (cramping, diarrhea, IBS); treats urinary incontinence; mydriatic agents; anesthesiology to reduce vagal tone on the heart & to dry secretions; antidote for poisoning with cholinesterase inhibitors or muscarinic agonists; prevention of motion sickness; treatment of Parkinson's disease and Parkinsonism; cardiac stimulation in emergencies; treatment of COPD and asthma; dry respiratory secretions |
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Term
| Side Effects & Toxicities of Antimuscarinic Drugs |
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Definition
| dry mouth; dry, hot skin; constipation, urine retention; visual disturbances, blurred vision, photophobia; CNS effects - sedation, confusion, amnesia |
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Term
| Contraindications in Use of Antimuscarinics |
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Definition
| glaucoma, prostatic hypertrophy, cardiovascular instability, severe ulcerative colitis |
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Term
| Symptoms of Acute Poisoning with Antimuscarinics |
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Definition
| dry, hot skin & hytperthermia; severe mydriasis, blurring of vision, photophobia; CNS stimulation - agitation, hallucinations, seizures progressing to coma & death; cessation of GI motility (no bowel sounds); weak, rapid pulse, tachychardia, arrhythmias |
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Term
| Treatment of Acute Poisoning with Antimuscarinics |
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Definition
| physostigmine/eserine (Antilirium) or other cholinesterase inhibitors; benzodiazepines for the treatment of seizures; ice baths to reduce hyperthermia; keep patient in dark, quiet area to prevent photophobia & excitement |
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Term
| atropine (hyoscyamine & analogs) |
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Definition
| "prototypical" antimuscarinic (anticholinergic) drug that is used for treatment of: some types of MIs where there is an increase in vagal tone resulting in low CO & fall in BP (cardiac stimulation); preop med to reduce secretions & block vagal reflexes on heart; antidote for cholinesterase inhibitor & muscarinic agonist poisoning; dries respiratory secretions in pulmonary medicine; ophthalmologic: mydriatic & cycloplegic agent; antispasmodic for treatment of GI disorders (IBS, biliary colic) |
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Term
| scopolamine (AKA hyoscine, Transderm Scop) |
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Definition
| oral & in patch form; treats the prevention of motion-sickness & vertigo; has a more CNS depressant effect (sedation & amnesia) than atropine |
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Term
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Definition
| nonquaternary antimuscarinic agent used as an intestinal antispasmodic for the treatment of IBS (irritable bowel syndrome) |
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Term
| propantheline (Pro-Banthine) |
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Definition
| antimuscarinic agent used in gastroenterology for its antispasmodic effects (IBS); quaternary compound with few CNS effects |
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Term
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Definition
| quaternary antimuscarinic agent with no CNS effects that is used in anesthesiology as a preop med to dry respiratory secretions & inhibits vagal reflexes; widely used as a generall purpose antimuscarinic agent |
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Term
| ipratropium (Atrovent) & tiatropium (Spiriva) |
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Definition
| antimuscarinic, quaternary salts administered by inhalation for the treatment of asthma & COPD; few systemic effects; one is longer-acting |
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Term
| benztropine (Cogentin) & trihexylphyenidyl (Artane) |
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Definition
| centrally acting antimuscarinics used in treatment of Parkinson's disease & Parkinsonism |
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Term
| tolterodine (Detrol), oxybutinin (Ditropan), & solifenacin (VESIcare) |
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Definition
| antimuscarinic agents used in treatment of urinary incontinence due to over-active bladder |
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Term
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Definition
| antimuscarinic agent widely used to dilate pupil for opthamologic examination |
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Term
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Definition
| competitive (nondepolarizing blockers) ACh antagonists at the neuromuscular junction to produce muscle relaxation; used in anesthesia; give a cholinesterase inhibitor (i.e. neostigmine) to reverse muscle relaxation or paralysis after surgery |
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Term
| Sympathetic Effects on the Eye |
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Definition
| pupillary dilation (mydriasis, alpha-1); increase ciliary aqueous humor production (beta-2) |
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Term
| Parasympathetic Effects on Eye |
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Definition
| pupillary constriction (miosis); contraction of ciliary muscle (accomodation for near vision) |
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Term
| Sympathetic Effects on Heart |
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Definition
| increase heart rate (beta-1,beta-2); major increase in contractility (beta-1,beta-2); increase automaticity (beta-1,beta-2); increase conduction velocity (beta-1,beta-2) |
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Term
| Parasympathetic Effects on Heart |
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Definition
| major decrease in heart rate; decrease in contractility; decrease in automaticity; decrease in conduction velocity |
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Term
| Sympathetic Effects on Blood Vessels of Mucosa, Skin, & Splanchnic Beds |
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Definition
| constriction (alpha-1 & alpha-2) |
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Term
| Parasympathetic Effects on Mucosa, Skin, & Splanchnic Beds |
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Definition
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Term
| Sympathetic Effects on Blood Vessels of Skeletal Muscle |
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Definition
| constriction (alpha-1); dilation (beta-2) |
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Term
| Parasympathetic Effects on Blood Vessels of Skeletal Muscle |
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Definition
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Term
| Sympathetic Effects on Airways |
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Definition
| bronchorelaxation (beta-2) |
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Term
| Parasympathetic Effects on Airways |
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Definition
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Term
| Sympathetic Effects on GI Tract |
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Definition
| relaxation (alpha-1,-2 & beta-1,-2); decreased motility |
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Term
| Parasympathetic Effects on GI Tract |
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Definition
| increased motility; increased spasms |
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Term
| Sympathetic Effects on Urinary Bladder Wall, Urinary Sphincter, & Prostate |
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Definition
| relaxation of wall (beta-2) & contraction of sphincter (alpha-1); retention occurs |
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Term
| Parasympathetic Effects on Urinary Bladder Wall, Urinary Sphincter, & Prostate |
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Definition
| constriction of wall; relaxation of sphincters; excretion occurs |
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Term
| Sympathetic Effects on Kidney JG Cells |
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Definition
| increased renin secretion (beta-1) |
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Term
| Parasympathetic Effects on Kidney JG Cells |
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Definition
| no increase or decrease in renin secretion |
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Term
| Sympathetic Effects on Uterus |
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Definition
| contraction (alpha-1) & relaxation (beta-2) during pregnancy |
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Term
| Parasympathetic Effects on Uterus |
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Definition
| no effects before, during, or after pregnancy |
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Term
| Sympathetic Effects on Male Sex Organs |
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Definition
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Term
| Parasympathetic Effects on Male Sex Organs |
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Definition
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Term
| Sympathetic Effects on Liver, Fat Cells |
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Definition
| increased glucose output (beta-2); increased fatty acid output (beta-1) |
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Term
| Parasympathetic Effects on Liver, Fat Cells |
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Definition
| no effects on glucose or fatty acid output |
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Term
| Sympathetic Effects on Skin - pilomotor muscle & sweat glands |
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Definition
| contraction (alpha-1); secretion (muscarinic) |
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