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180 Cards in this Set

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cholinergic antagonist
drug that interfers with ACh at cholinergic receptors
antagonist
a compound that has an affinity for the receptor but lacks intrinsic activity
binds but will not produce a response
2 types of nicotinic antagonists
ganglionic blockers
neuromuscular blocking agents
muscarinic antagonists aka (7)
antimuscarinic
anticholinergic
cholinergic antagonist
cholinergic blocker
parasympatholytics
*parasympathetic postganglionic blocking agent
antispasmodic
muscarinic antagonist clinical manifestations: heart
tachycardia
muscarinic antagonist clinical manifestations: lungs
dilation of bronchioles
muscarinic antagonist clinical manifestations: GI tract
decr secretion & motility
muscarinic antagonist clinical manifestations: bladder
urinary retention
muscarinic antagonist clinical manifestations: eyes
mydriasis
cycloplegia
mydriasis
pupil dilation
cycloplegia
temporary paralysis of ciliary muscle
muscarinic antagonist clinical manifestations: skeletal muscle
relaxation
muscarinic antagonist clinical manifestations: CNS
CNS stimulation or depression
muscarinic antagonist clinical manifestations: mucous membrane
decr salivation and perspiration
clinical significance of antimuscarinics (uses, effects)
incr cardiac output
antispasmodic effect
antisecretory effect
mydriatic & cycloplegia
PD
asthma
cholinergic poisoning
how can an antimuscarinic treat bradyarrythmia?
incr heart rate
what significance does the antispasmodic effect of antimusc have?
used to treat diahrrea - tone & motility of GIT
what significance does the antisecretory effect of antimusc have?
can be used prior to surgery
antisialoqoque (prevent drooling)
antihydrotic (prevent excessive perspiration)
why can an antimuscarinic be used to treat asthma or COPD
b/c antimusc cause bronchodilation
what are the most common side effects of antimuscarinics?
dry mouth
mydriasis
urinary retention
precipitate glaucoma
how do antimusc precipitate glaucoma?
pupils dilate -> ciliary muscle thickens -> anterior chamber narrows -> obstruct outflow of aq humor -> incr intraocular pressure
what are the 6 classes of antimuscarinics
solanaceous alkaloids
aminoalcohol esters
aminoalcohol ethers
amino alcohols
aminoamides
miscelleneous
give 2 examples of solanaceous alkaloids
atropine
scopolamine
atropine is derived from what plants?
atropa belladona (deadly nightshade)
datura stramonium (jimsonweed, thorn apple)
what plant is scopolamine derived from?
hyoscymus niger (black henbane)
another name for atropine
hyoscyamine
what bicyclic ring does atropine contain? what 2 rings make up the bicyclic ring?
tropane
piperidine
n-methyl pyrrolidine
what position must the 3 alpha hydroxy group be in for atropine to be active?
axial position
neurotropic effect
interfering with nerve impulse transmission
musculotropic effect
direct depression of smooth muscle, esp of the GIT
standard - papavarine
atropine sulfate is used primarily for?
mydriatic effect during eye exams/refraction studies
other effects of atropine sulfate?
tachycardia
constipation
xerostomia
dry eyes
CNS stimulation
decr GIT secretions
atropine sulfate is contraindicated in patients with:
open angle glaucoma
BPH
severe hypertension
scopolamine is AKA
hyoscine
can scopolamine penetrate the CNS?
yes b/c it has no charge
what important group is found in scopolamine
beta-epoxy group
what is scopolamine used for?
to prevent motion of sickness - drug of choice
what are side effects of scopolamine?
sedation
dry mouth
homatropine HBr is similar to what other drug?
atropine
homatropine HBr is an ester of what 2 acids
tropine acid
mandelic acid
what is the potency of homatropine compared to atropine?
1/2 as potent as atropine
homatropine is used primarily for what properties?
mydriatic and cycloplegic proterties
what is the brand name for ipratropium br?
atrovent
how is ipratropium related to atropine?
it is a semi-synthetic derivative of atropine
what is the mechanism of action of ipratropium bromide
produces bronchodilation by competitive inhibition of cholinergic receptors bound to smooth muscles of bronchioles
ipratroium br is used to treat:
asthma (as an adjuvant) & COPD
list of 9 drugs that are aminoalcohol esters
clidinium br
cyclopentolate HCl
dicyclomine HCl
eucatropine HCl
glycopyrrolate
mepenzolate br
methantheline br
oxyphencyclamine hcl
propantheline br
brand name for clidinium bromide
quarzan
clidinium bromide contains what kind of nucleus?
quinuclidine
clidinium bromide is used for which effects?
its antispasmodic & antisecretory effects
clidinium br is used in combination with chlordiazepoxide to treat
peptic ulcers & other GI secretory diseases
brand name for clidinium br & chlordiazepoxide combo
librax
librax has more affinity for which receptors?
M1 & M3 (CNS & GIT)
brand name for dicyclomine hcl
bentyl
activity of dicylomine as it relates to atropine (neurotropic & musculotropic)
1/8 neurotropic activity & 2x musculotropic activity as atropine
dicyclomine used primarily for its
spasmolytic effet on smooth muscle of GIT; IBS
can dicylomine penetrate the CNS?
yes - no charge
brand name for glycopyrrolate
robinul
can glycopyrrolate penetrate the CNS?
no - quaternary ammonium
what kind of ring does glycopyrrolate have?
pyrrolidine ring
glycopyrrolate used for:
spasmolytic & antisecretory effect
glycopyrrolate has more affinity for which receptor?
M1 (less tachycardia as side effect)
what occurs as a result of high doses of glycopyrrolate
NMJ and ganglionic receptors can be blocked
brand name for propantheline br
pro-banthine
propantheline br is a derivative of what drug?
banthine (methantheline)
-ethyl instead of isopropyl groups
-2-5x more potent
what ring does propantheline br have?
xanthene ring
propantheline br is used for
antispasmodic & antisecretory effects
aminoalcohol esters are mostly used for
antispasmodic & antisecretory effects
aminoalcohol esters - quaternary ammonium derivatives
poorly absorbed
little or no CNS effect
can block ganglionic and NMJ receptors in high doses
aminoalcohol ethers and aminoalcohols are used to
manage symptoms of PD
examples of aminoalcohol ethers
benztropine mesylate
orphenadrine citrate
examples of aminoalcohols
biperidine
procyclidine
trihexyphenidyl HCl
Parkinson's disease first described by who? in what year?
james parkinson
1817
parkinson's disease aka
shaking palsey
4 primary symptoms of PD
fine tremors (pill rolling)
rigidity or stiffness of limbs, trunk
slowness of movement (bradykinesia)
postural instability
other symptoms of PD
oculogyric crisis
mask face
drooling
depression
oculogyric crisis
movement of eyeballs impaired - positioned upward & outward
where does PD orginate
in the midbrain
what does the substantia nigra produce?
dopamine
what is the substantia nigra
deeply pigmented grey cells
pyrimidal tract
excitatory
initiates muscle movement
extrapyrimidal tract
inhibitory
smooths and coordinates muscle movement
what kind of neurotransmittor is dopamine?
inhibitory
in healthy individuals, dopamine relays signals from the substantia nigra to the next relay station, the:
corpus stiatum
what produces purposeful muscle activity
balance of inhibitory dopamine (extrapyrimidal) & excitatory ACh (pyrimidal) mediated neurotransmission
pathophysiology of PD
the dopamine producing neurons in the substantia nigra die
imbalance between dopaminergic & cholinergic activity leaves the patient unable to control movement in a normal manner
primary PD is AKA
paralysis agitans
is the cause of primary PD known?
no (idiopathic)
is primary PD curable?
no - treatment is palliative
what are the causes of secondary PD?
drugs (iatrogenic - reversible)
poisoning
infectious
others
drugs that induce secondary PD
reserpine
haloperidol
chlorpromezine
infectious causes of secondary PD
encephalitis
syphilis
other causes of secondary PD
arterioschlerosis
neurodegenerative processes
objective of PD treatment
to improve quality of life
what are the 2 types of drugs used to treat PD
dopaminergic agonists
cholinergic antagonists (for mild symptoms - tremors)
brand name for diphenhydramine
benadryl
what effect does diphenhydramine have?
antihistaminic
some anticholinergic activity
drowsiness
CNS depression
alleviates some symptoms of PD
brand name for benztropine mesylate
cogentin
what 3 effects does benztropine have?
anticholinergic
antihistaminic
local anaesthetic
benzotropine has similar potency and side effects as what drug?
atropine
benztropine should not be used in patients with:
glaucoma
BPH
benign prostratic hyperplasia
the prostate is enlarged, which pinches the urethra causing painful urination
what are the common structural features of aminoalcohols
bulky groups in the vicinity of hydroxyl and cyclic amino functional groups
gamma-aminopropanol arrangement
tertiary amines used to treat:
quaternary amines used for:
PD
antispasmodic
what is the brand name for biperiden
akineton
what ring structure does biperiden have?
piperidine ring
biperiden is used to treat
all forms of PD
spastic disorders (spinal cord injury, cerebral palsey, multiple schlerosis)
akinesia, rigidity, tremor
brand name for procyclidine HCl
kemadrin
characteristics of procyclidine
pyrrolidine ring
tertiary amine - PD
brand name for trihexyphenidyl HCl
artane
chracteristics of trihexyphenidyl
piperidine ring
used in PD
1/2 as potent as atropine
good margin of safety
brand name for isopropamide iodide
darbid
isopropamide used to treat?
peptic ulcers
DOA of isopropamide
12 hrs
isopropamide is contraindicated for patients with:
glaucoma
BPH
brand name for ethopropazine HCl
parsidol
ring in ethopropazine
phenothiazine
ethopropazine used to treat:
PD (controls rigidity, tremors, sialorrhea, oculogyric crises)
side effects of ethopropazine?
contraindication?
xerostomia
mydriasis
CI: glaucoma
papaverine is a derivative of what plant?
papaver somniferum
papaverine has what kind of structure
benzylisoquinoline
MOA of papaverine
generalized smooth muscle relaxation
papaverine used to treat
peripheral vascular diseases (spasmolytic activity)
male impotency
papaverine not used often b/c?
lack of potency
what is raynaud's disease
vascular disease
cyanosis of fingers, nails b/c of impaired blood flow
what are the 2 types of nicotinic antagonists
ganglionic blocking agents
neuromuscular blocking agents
what are the 3 kinds of ganglionic blocking agents?
depolarizing
nondepolarizing competitive
nondepolarizing noncompetitive
what are the 2 kinds of neuromuscular blocking agents?
nondepolarizing
depolarizing
what was the 1st class of drugs used for hypotensive effect?
neuromuscular blockers
a drug that blocks the sympathetic system is known as:
sympathoplegia
a drug that blocks the parasympathetic system is known as:
parasympathoplegia
what affects do sympathoplegia drugs have?
orthostatic hypotension
sexual dysfunction
what affects do parasympathoplegia drugs have?
constipation
dry mouth
blurred vision
precipitation of glaucoma
in what NS do ganglionic blockers work? neuromuscular blockers?
autonomic
somatic
what stimulant is a depolarizing ganglionic blocking agent?
nicotine
at low doses, nicotine is a _______; at high doses, it is a ________
stimulant (depol & repol)
ganglionic blocker (no repolarization)
what therapeutically useful drugs are there in the depolarizing gangionlic blockers group?
none
MOA of nondepolarizing comkpetitive ganglionic blocking agents
bind to nicotinic receptor but lack intrinsic activity for impulse transmission (unable to depolarize the cell)
name 5 examples of nondepolarizing competitive ganglionic blocking agents
tetramethylammonium salts
hexamethonium
trimethaphan
mecamylamine
what is the difference between hexamethonium and decamethonium
hexa: 6c, strong ganglionic blocker, weak curariform activity
deca: 10c, weak gang blocker, strong curariform activity
brand name for trimethaphan camsylate
arfonad
what ring structure does trimethaphan camselate have?
camphor sulfonate
DOA of trimethaphan
short, 10-30 min
use for trimethaphan
used in emergency room to lower BP (given by iv, inactive orally)
brand name for mecamylamine
inversine
what ring structure does mecamylamine have?
norbornane ring
what is mecamylamine rarely used?
causes severe orthostatic hypotension
curariform activity AKA
neuromuscular blocking activity
what is a NMJ?
specialized synapse between a motor neuron and skeletal muscle
when are neuromuscular blocking agents commonly used?
during surgical procedures as adjuncts to general anesthesia
what are NM blocking agents used during surgery?
induce reversible paralysis
no central activity
what is the prototype for nondepolarizing NMJ blockers?
d-tubocurarine
example of a depolarizing NMJ blocker
succinylcholine
tubocurarine is derived from what plant?
curare (chondodendron tomentosum)
what is the half life of tubocurarine?
90 min
DOA of tubocurarine
2 hrs (binds at receptor for only 1 msec)
uses for tubocurarine
adjunct in general anesthesia
arrow poison
the brand name for atracurium besylate
tracrium
DOA of atracurium?
short - 20min b/c easily hydrolyzed by plasma esterases
what 2 ring structures does atracurium have?
benzyl
tetrahydroisoquinoline
which is more potent: atracurium or tobocurarine?
atracurium, 2.5x
uses for atracurium?
skeletal muscle relaxant for short surgical procedures
paralysis caused by atracurium can be reversed by? how?
AChEI - incr amount of ACh present, competes with drug for receptor
why can atracurium be dangerous if you are on it for a long time?
metabolyte can accumulate in the brain & cause seizures
what is laudanosine?
breakdown product of atracurium
what is the brand name for doxacurium cl?
nuromax
what ring complex does doxacurium have?
benzylterahydroisoquinoline
what is the difference between atracurium & doxacurium?
doxa has an extra methoxy group - hinds access of esterases - longer doa
uses for doxacurium
skeletal muscle relaxant for surgical procedures lasting longer than 90 min
what is the brand name for pancuronium bromide?
pavulon
what ring complex does pancuronium have?
amino steroid
what 2 placess does pancuronium act?
nicotinic receptor
ion channel
which is more potent: tubocurarine or pancuronium?
pancuronium, 5x
uses for pancuronium
skeletal muscle relaxant during surgery
adjunct to anesthesia
what are the possible metabolytes of pancuronium?
3-OH
17-OH
3,17-dihydroxy
brand name for succinyl cl
anectine
what class does succinly cl belong to?
depol NMJ blocker - only useful agent in its class
doa of succinyl cl?
very short acting
succinyl cl is unstable in what kind of soln?
alkaline
uses for succinyl cl
skeletal muscle relaxant in surgery
intratracheal intubation
endoscopic procedures