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19 Cards in this Set
- Front
- Back
ACETYLCHOLINE
physiological activity |
direct acting cholinergic agonist
CARDIOVASCULAR SYSTEM - vasodilation - decrease heart rate - decrease in force of contraction SMOOTH MUSCLE: contraction - increase GI motility - constriction of Bronchioles - contraction of ureter, bladder and uterine contraction - miosis of eye, accomidation for near vision GLANDS: secrections - increase salivation, sweating, lacrimation, GI secretions, bronchiolar secretions NEUROMUSCULAR (nicotinic) - stimulation of motor end plate |
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ACETYLCHOLINE
pharmocologic activity |
therapeutic action is due to muscarinic activity
THERAPEUTIC USES: - used to acheive miosis during eye surgery ADVERSE EFX: "DUMBELS" Diarrhea and Decreased BP Urination Miosis Bronchoconstriction Excitation of skeletal muscle Lacrimation Salivation |
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BETHANOCHOL
CARBOCHOL Methacholine choline esters |
RECEPTOR: muscarinic and nicotinic (Bethanichol- muscarinic)
PHYSIOLOGICAL AXN(s): Activation of muscarinic receptors increases cGMP and potassium flux, accelerates phosphatidyl inositol turnover ---> increase in intracellular Ca or inhibition of adenyl cyclase activity THERAPEUTIC USES: - Bethanechol stimulates GI motility and is used to treat urinary retention (remember BBB) - Carbachol is rarely used but may be used for glaucoma or to induce miosis ADVERSE EFX: "DUMBELS" * Methacholine is used to test the severity of bronchial hyperreactivity |
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PILOCARPINE
MUSCARINE "the natural alkaloids" |
RECEPTOR: primarily muscarinic
PHYSIOLOGICAL AXN(s): - miosis and contraction of the ciliary muscle - decreases heart rate - causes bronchial SM contraction THERAPEUTIC USES: - xerostomia, to induce salivation - glaucoma, onset of action 15-30 min, 4-8 duration ADVERSE EFX: - CNS disturbances such as hallucinations and convulsions along with DUMBELS - contraindicated in pts w/ peptic ulcers, asthma, hyperthyroidism, parkinsons * Muscarine is an alkaloid present in wild mushrooms, not used clinically; interest is due to accidental intoxication, treated w/ atropine |
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EDROPHONIUM
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cholinesterase inhibitor
RECEPTOR: nicoinic receptors PHYSIOLOGICAL AXN(s): binds reversibly to AChE preventing access by ACh THERAPEUTIC USES: used in the diagnosis of Myasthemia Gravis b/c of its short duration of action (5-15 min). It is also used to differentiate btwn MG and cholinergic crisis - administration of Edrophonium helps MG but makes cholinergic crisis worse. ADVERSE EFX: excessive cholinergic stimulation |
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PHYSOSTIGMINE
PYRIDOSTIGMINE NEOSTIGMINE |
Carbamates Esters
RECEPTOR: nicotinic (not Physos.) PHYSIOLOGICAL AXN(s): binds active site of AChE making nzm resistant to hydrolysis THERAPEUTIC USES: Physostigmine (0.5-2h; inj,top)- glaucoma, atropine or trycylic depressant intoxication Neostigmine (0.5-2h; PO,inj)- Myasthemia gravis, urinary retention, paralytic ileus Pyridostigmine (3-6h; PO,inj)- Myasthemia Gravis ADVERSE EFX: "DUMBELS" tremors, convulsions pyrido and neostig have CNS effects |
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ECHOTHIOPHATE
MALATHION PARATHION SARIN soman |
Organophosphates
PHYSIOLOGICAL AXN(s): "irreversible inhibitor" bind to AChE yeilding phosphorylated nzm, nzm undergoes aging and new nzm must be sythesized THERAPEUTIC USES: Echothiophate- used topically for glaucoma, duration is greater than 100 hours Malathion/ Parathion - agricultural pesticides, frequent accidental intoxication Soman/ Sarin - nerve gases, used in chemical warfare ADVERSE EFX: "DUMBELS" tremors convulsions death due to respiratory depression * treat toxicities w/ O2, atropine, pralodoxime, and benzodiazapines (to reduce siezure activity |
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PRALODOXIME
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RECEPTOR: cholinesterase reactivator
PHYSIOLOGICAL AXN(s): has strong affinity for phosphorylated enzyme, oxime gets phosphorylated, thus regenerating free enzyme THERAPEUTIC USES: antidote to organophosphates; not effective once aging has taken place ADVERSE EFX: |
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DONEPEZIL
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Non competitive reversible cholinesterase inhibitors
PHYSIOLOGICAL AXN(s): selective AChE of the brain THERAPEUTIC USES: treatment of cognitive deficits associated with Alzheimers Disease, selective for memory loss ADVERSE EFX: |
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NICOTINE
physiological actions |
RECEPTOR: binds a subunit of nicotinic receptorscusing increase Na influx
CNS: - small doses increase rate and depth of respiration - tremors; convulsions at toxic doses - irritability, nausea and vomiting, antidiuretic, increase in alertness and memory CARDIOVASCULAR: increased heart rate, CO, TPR, and blood pressure GI TRACT: increases secretions and motility; excaberates peptic ulceration |
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NICOTINE
pharmacologic properties |
Nicotine is highly soluble and well absorbed from all routes of administration
THERAPEUTIC USES: nicotine gum, inhaler, nasal spray, and transdermal patch to aid in smoking cessation ACUTE INTOXICATION: respiratory failure, CV collapse, nausea, vomiting, headache, dizziness, palpitations and convulsions CHRONIC TOXICITY: - tolerance and physical dependence - respiratory and CV disease - cancer * BUPORPION and antidepressant, used as an aid in smoking cessation * CLONIDINE releives the symptoms of withdrawal |
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ATROPINE
physiological characteristics |
RECEPTOR: competative, reversible antagonists of ACh at muscarinic receptors; no intrinsic activity (natural alkaloid of the plant Atropa belladona)
CARDIOVASCULAR SYSTEM: - low doses reduce heart (transient brachycardia) thru vagal stimulation - high doses elevate heart rate GI TRACT: reduces salivary gland secretion PULMONARY SYS: reduces bronchial secretions and stimulates bronchodilation EYE: paralysis of muscles --> mydriasis and cyclopegia URINARY BLADDER: bladder wall relaxation SECRETIONS: reduces salivation and inhibits sweating |
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ATROPINE
IPRATROPIUM pharmocologic characteristics |
THERAPEUTIC USES:
- bradycardia/ MI in pts with excessive vagal activity - mydriasis and cyclopegia - treatment of organophosphate poisoning - to dry salivary secretions - diarrhea, gastrointestinal, bladder spasms - COPD and bronchial asthma (IPRATROPIUM, used by B inhalaltion) ADVERSE EFX: dry as a bone hot as a hare red as a beet blind as a bat mad as a hatter * contraindicated in patients with glaucoma, prostatic hyperplasia, and in elderly men |
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SCOPOLAMINE
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belladonna alkaloid
RECEPTOR: muscarinic PHSIOLOGICAL AXN(S):nonselective blockade of receptors; competes with ACh THERAPEUTIC USES: - prevention of motion sickness-"lotion for motion" - long duration of action w/ potent CNS effects; given transdermally ADVERSE EFX: dry as a bone hot as a hare red as a beet blind as a bat mad as a hatter |
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HOMATROPINE
CYCLOPENTOLATE TROPICAMIDE |
RECEPTOR: muscarinic
PHSIOLOGICAL AXN(S): semi/synthetic compounds nonselectively block muscarinic receptors THERAPEUTIC USES: given topically to induce mydriasis and cyclopegia; have much shorter duration of action than atropine and scopolamine ADVERSE EFX: similar to atropine but much milder |
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DICYCLOMINE
GLYCOPYRROLATE |
Synthetic anti-cholinergic agents
RECEPTOR: muscarinic PHYSIOLOGICAL AXN(s): block muscarinic receptors THERAPEUTIC USES: - reduce gastrointestinal spasm gastrointestinal motility - reduce acid secretion in peptic ulceration - (glycopyrrolate) dries salivary secretions ADVERSE EFX: at high doses can lead to constipation in the elderly |
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BENZTROPINE
TRIHEXYPHENIDYL |
semi synthetic anti muscarinic agents
RECEPTOR: muscarinic PHYSIOLOGICAL AXN(s): blockade of muscarinic receptors THERAPEUTIC USES: treatment of drug induced Parkinson's disease to lower relative excess in cholinergic activity ADVERSE EFX: delirium, mental confusion, and memory loss |
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OXYBUTANIN
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RECEPTOR:muscarinic
PHYSIOLOGICAL AXN(s): blockade of muscarinic receptors THERAPEUTIC USES: relieve urgency of transient cystisitis and bladder spasms due to infection of after urologic surgery ADVERSE EFX: |
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MECAMYLAMINE
Trimethaphan |
Anti-nicotinics, Ganglionic blockers; all synthetic amines
RECEPTOR: nicotinic PHYSIOLOGICAL AXN(s): non depolarizing, competitive blocker; binds to the ACh nicotinic receptor site but has no intrinsic activity CNS: sedation, tremor, mental abberation EYE: cyclopegia, loss of accom., moderate pupil dilation CV SYS: decresed arteriolar and venomotor tone, leading to hypotension; moderate tachycardia THERAPEUTIC USES: limited; hypertensive emergency ADVERSE EFX: |