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121 Cards in this Set
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drugs which effect muscarinic receptors- postsynoptic structures or effectors
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Cholinergic Drugs
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autonomic ganglia, neuromuscular junction
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nicotinic receptors
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available as a drug product- very limited therapeutic purposes
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acetylcholine
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not commonly used, non selective, available at a lot of different sites, will get wide spread effects
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acetylcholine
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inactivation is extremely rapid-very short effect, use topically in the eye
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acetylcholine
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acetyl ester that is fairly rapidly inactivated makes a little more effective
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methacholine
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carbamic acid ester that is very stable and not easily metabolized by choline esterase, much longer acting drug
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carbachol
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not as selective as methacholine and is used topically in the eye
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carbachol
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more selective, long duration of effect because of carbamic acid ester
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uracholine
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topically in eye, used in surgery
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acetylcholine
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glaucome or ocular sugery
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carbachol
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urinary bladder retention
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methacholine
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abdominal retention, build up of gas products
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uracholine
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decreae activity in GIT and bladder
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uracholine
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administered by injection which has a more predictable effect and sometimes orally which is very poor, delays effect and random
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acetylchonine, carbachol, methacholine, and uracholine
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side effect(s) of acethycholine, carbachol, methacholine, and uracholine
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salivation
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administed as D-pantothenyl alcohol and in body is converted to pantothenic acid
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dexpanthenol
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precursor to CoEnzyme A, absorbed better in alcohol form
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Dexpanthenol
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Dexpanthenol
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Ilopan
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take 2 to 3 tabs 3 times a day
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dexpanthenol
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enhances synthesis of acetylcholine, transfer of 2 carbon groups
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Co Enzyme A
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product good for gas retention (anti-flactulant), and also used for laxative withdrawal
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dexpanthenol (50mg) + choline (25mg)
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injection, abdominal retention, bladder retention, laxative
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dexpanthenol
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far fewer than choline estero, diarrhea, dematities, nausea
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adverse effects dexpanthenol
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injection or oral, stimulate GIT, prokinetic agent, doesn't minic ACh and doesn't interact with cholinergic receptors
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Metaclopramide
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Metaclopramide
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Reglan
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stimulate GI tract without significant impact on secretions
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prokinetic agent
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GERD
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gastroesphogeal reflux disease
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causes contraction of lower sphincter which prevents reflux , not best choice for GERD
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mechanism of action for metaclopramide
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removed from general use in 2000
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cisapride
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interacted with other drugs to cause ventricular arrthymias
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cisapride
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prokinetic agent
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cisapride
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tegaserod
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zelnorm
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prokinetic agent
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tegaserod
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5- HT4 receptor agonist
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tegaserod
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relief of abdominal pain and constipation assocaited with irritable bowl syndrome
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tegaserod
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adverse effects of tegaserod
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headache and diarrhea
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natural alkaloids, found in plants stimulate cholinergic receptors
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cholingeric agents
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are lipid soluble and distribute into CNS- expect to penetrate CNS- not a desirable effect
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secondary and tertiary amines
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tertiary amine found in leaves piolcarpus jaborandi
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pilocarpine
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used topically in the eye as a miotic agent in the management of glaucoma
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pilocarpine
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constriction of the pupil
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miotic agent
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contracts the ciliary muscle in the eye- results in blurred vision and dialation of the drainage system for ocular fluid
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pilocarpine
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sustained release- membrane placed into the culdesac of eye-lasts one week
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ocuster
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allows normal neurotransmitter to accumulate
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cholinesterase
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neurons, NMJ, RBC, more specific for acetylcholine
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true of acetylchoinesterase
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plasma, liver, intestines, more vunerable to inhibit drugs, anyting that inhibits cholinesterase
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plasma or pseudo choliesterase
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generally carbamic acid esters
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reversible ChE inhibitors
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tertiary amine found in seeds of physostigma venenosum and gets into CNS, very limited systemic use
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physotigmine
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ocular miotic agent, limited use in Alzheimer's disease, not highly selective , quick acting, use with toxicity to cholinergiv agents and is a cholinesterase inhibitor
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use of physotigmine
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neostigmine
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prostigmine
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onset 10-20 min, duration of 2 to 4 hours
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neostigmine
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stimuates the GIT and bladder, available by injection or oral tabs, cholinergic
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uses of neostigmine
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pyridostigmine
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mestinon
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duration 3-6 hours, given once a day, oral and parent, available in a sustained release product for use in myasthemia
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pyridostigmine
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ambenonium
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mytelase
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duration 4 to 8 hours, has tendency to accumulate at NMJ, administer 2-3 times daily
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ambenonium
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administer IV only, onset 20-30 sec, duration 2-4 min, used in surgery to reverse curvave like drugs, rapidly eliminated by the kidneys
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edrophonium
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edrophonium
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tensilon
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edrophonium
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enlon
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edrophonium
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reversol
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diagnostic antidote for anticholinergics and curare, reversilbe anticholinergic agen, competitive anatagonism, overcome the block
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edrophonium
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organophosphorous compounds, form a stable covalent bond at the esteratic site of ChE
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irreverisble cholinesterase inhibitors
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echothiophate
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echodide
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echothiophate
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phospholine
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used in glaucoma, miotic agent, administer drop application to eye once or twice a day or every other day, comes in powder
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echothiophate
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blurred vision, poor dim light vision, risk of catarracts with long term use, intense miotic effect, may increase IOP
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side effects of echothiophate
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liquid, developed in UK in 1952, increae adhesiveness
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Vx Gas
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penetrate skin and eye, CNS and peripheral effects, effects cholinergic neurons everywhere, miosis, blurred vision, salivation, sweathing, weazing
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symptoms of Vx Gas
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atropine sulfate
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antidote of Vx GAs
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administer 2-4 mg IV every 5 to 10 min until signs of atropine toxicity, antimuscarinic
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antido to Vx gas
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oxime functional group =N-OH
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reactivator of Vx Gas
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pralidoxime
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protopam
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dose 1-2 g IV, dislodge the irreversible ChEI from receptor, effective if administer before 36 horus following exposure,
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pralidoxime
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pyridostigmine
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mestinon
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used to prevent toxicity
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pyridostigmine
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persisted elevated intaocular pressure, increased IOP leads to degeneration of optic nerve and retina
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glaucoma
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obstructed drainage of aqueous humor
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angle closure or narrow angle
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can usually be corrected with surgery
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narrow angle glaucoma
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drainage problem usually due to increase resistance in the canal of schlemm or trobecular meshwork
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wide angle/ open angle/ cronic glaucoma
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some identifiable causes such as tumors or trauma to the eye, not really common
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secondary glaucoma
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infantile, may affect canal of schlemm, may or may not be correctable, extremely rare
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congenital glaucoma
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increase drainage by decreasing the reduction of the filtration angle
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miotice agents in narrow angle glaucoma
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contract the ciliary muscle- dialates the drainage system
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miotic agents in wide angle glaucoma
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direct acting miotic agents
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pilocarpine
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put in eyes once a week
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ocusert
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more viscosity, increase duration, 3 to 4 times daily
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pilogel and piloplex
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blurred vision, poor dim light, night vision
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adverse effects of miotic agents
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decrease IOP by increasing drainage of aqueous humor, may produce slight reaction in formation of aqueous humor, used in combo with pilocarpine
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sympathomimetics agents
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dialate pupils, no good in narrow angle
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adverse effects of sympathomimetics agents
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epinephrine
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sympathomimetics agents
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dipivefrin
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proline
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administer one drop every 12 hours
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dipivefrin
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penetrates 17 times greater into the anterior chamber
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dipivefrin
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alpha 2 adrenergic receptor agonists
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apraclondine and brimonidine
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decrease formation of aqueous humor, may have small effect on drainage,
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alpha 2 adrenergic receptor agonists
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one or tow drips tid
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apraclondine
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adverse effects of apraclondine
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dialate pupil
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apraclondine
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iopidine
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brimonidine
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alphagan
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1 drop tid
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brimonidine
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reduce IOP formation by reducing availability of HCO3-
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carbonic anhydrase inhibitors
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carbonic anhydrase inhibitors
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brinzolamide and dorzolamide
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brinzolamide
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azopt
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1 drop tid
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brinzolamide
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1 drop tid
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dorzolamide
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dorzolamide
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trusopt
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burning senstation, sensation of foreign object in eye, bitter taste, mild conjunctivitis
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adverse effects of carbonic anhydrase inhibitors
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decrease IOP by increasing drainage of aqueous humor
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prostaglandin analogs
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prostaglandin analogs
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latanoprost, travoprost, unoprostone, bimatoprost
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latanoprost
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xalatan
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travoprost
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travatan
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unoprostone
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rescula
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bimatoprost
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lumigan
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administer 1 drop once daily, use in a combination, esters hydrolyzed by esterases in cornea
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prostaglandin analogs
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increase pigmentation, conjunctivitis, increase growth of eyelashes, stimulate formation of melanin, give if another therapy is not working well
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prostaglandin analogs adverse effects
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perservative in eye drop
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benzalkonium chloride
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anticholinergics and corticosteriods
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drugs contraindicated in glaucoma
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dialate pupils, old antidepressents and tranquilizer drugs, narrow angle
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anticholingergics contraindicated in glaucoma
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topical may increase IOP, eye drop cause fluid reterntion, caution in all types of glaucoma
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corticosteriod drugs contraindicated in glaucoma
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chronic autoimmunve disease characterized by skeletal muscle weakness
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myasthenia gravis
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