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121 Cards in this Set

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