Pharm1E1 Cholinergic Antagonists & NM Drugs Flashcards
atropine has high affinity for ? receptors and little to no affinity for ?
muscarinic- NONSELECTIVE for M1-M5
nicotine» little to no effect at ganglia
tissues most sensitive to atropine? 3
salivary
bronchial
sweat
? is 5 times more selective for M1 over ? receptors
pirenzepine
M2
common s/e of musc. ant
dry mouth
sites with little cholinergic control i.e. ? wont respond significantly
blood vessels
antimuscarinics that enter the CNS can cause ? and ?
drowsiness
amnesia
treats motion sickness; s/e include dry mouth & ?
scopolamine
sedation
high doses of atropine results in?
tachycardia
low doses of atropine.. initially causes ? b/c
the ? receptors aka ? on the ? terminals are blocked; these receptors normally reduce synaptic release of ? so when they are blocked more Ach is released, resulting in bradycardia
bradycardia presynaptic muscarinic autoreceptors vagal nerve Ach
blockade of atrial muscle M2 receptors = no clinical significance except in ? or ?
atrial flutter, fibrillation
overall antimuscarinic effects on heart not dramatic: ? and little to no change in ?
tachycardia, blood pressure
atropine - respiratory - bronchodilation and reduction in?
bronchial secretions
in RS primary use is ? and ?
reduce secretions and prevent laryngospasm (inhalation anesthesia)
elevation of body temperature in infants aka?
atropine fever
antimuscarinics reduce ? but have little effect on ?
tremor, bradykinesia
drugs for PD? 3
cogentin
artane
norflex
aka CAN
topical app- eye
aids in measurement of ? and facilitates ?
refractive error
eye exam of retina
antimuscarinics for the eye? PACS TH
paremyd- combo of antimusc & sym-mimetic atropine cyclopentoate scopolamine tropicamide homatropine
? is the longest acting on the eye
atropine
? is best for eye exams; shortest acting
tropicamide
respiratory- inhibit airway secretions & cause bronchodilation (5)
atropine hyoscyamine ipratropium combivent tiotropium
best for asthma?
combivent- activates B2!
1st line for COPD
ipratropium
GI- peptic ulcer 3
rarely used- PPIs more common
atropine
anaSPAZ
rubinol
Diarrhea drug- additive to ? to discourage abuse
lomotil, opioid
antispasmodics - 2
treats IBS & spastic colon
atropine
bentyl
only one for heart?
low dose =?
high dose=?
atropine
bradycardia (presynaptic inhibition)
tachycardia (may extend an infarct)
atropine can reverse ? in the heart and ? attacks aka ? can be blocked
bradycardia
vaso-vagal, syncope
GU- relieve urinary urgency/incontinence
s/e include ? and ?
name 6
ditropan XL detrol LA sanctura toviaz enablex vesicare **last two are M3 selective-detrusor muscle- overactive bladder
atropine very safe but CI in ? and ?
GLC, especially narrow angle closure
BPH- can precipitate urinary retention
ganglionic blockade- all ganglia blocked bc all are ?, so the ? in ANS is prevented; drug?
nicotinic
reflex activity
inversine- DOES access the CNS
effect of inversine is opposite to the ?
all tone is PNS except for ?
dominant ANS tone
arterioles (S), veins (S), sweat glands (S), and G/U (both)
bv are dominant via SNS vasoconstrictor actions so mecamylamine (inversine) results in ? bc ?
postural/orthostatic hypotension
the postural reflexes that prevent venous pooling are blocked
on heart vagal tone dominates so ganglionic blockade»_space; ?
moderate tachycardia
mecamylamine (inversine) indicated for moderate to severe ? and is an orphan drug by FDA for ?
Htn
Tourette’s
*also used for ADHD, drug withdrawal, reducing bleeding during surgery
inversine rarely used by can lower BP in emergency cases of ?
acute dissecting aortic aneurysm
NM blocking drugs are used as adjuncts to ?
general anesthesia
nicotinic receptor antagonists are ? agents
nondepolarizing
depolarizing agents activate ? i.e. ?
nicotinic receptors, succinylcholine
non depolarizing are given either ? or ? but are inactive if given?
IM, IV, orally
longer actings non depolarizing blockade drugs?
**difficult to reverse blockade!
tubocurarine (80-120hrs)
PANcuronium (120-180hrs)- pan = all so it needs a long time!
shorter acting non depolarizing blockade drugs?
atracurium (30-60 min), mivacurium (12-18 min)
rapid onset, low potency, intermediate duration?
rocuronium
nondepolarizing blocking drugs produce flaccid paralysis of muscle by inhibiting the ?
binding of ACh to nAChRs on muscle fibers
? can slightly block ganglionic neuronal nicotinic Ach receptors
tubocurarine
used in patients w/ multi system organ failure b/c their metabolism is independent of renal and hepatic function
atricurium, cisatracurium
has the fastest onset and is a useful alternative to succinylcholine for tracheal intubation?
rocuronium
tubocurarine produces ? due to stimulation of ? release and at high concentrations ganglionic blockade
hypotension
histamine
has a moderate increase in HR and CO due to blockade of cardiac muscarinic receptors?
pancuronium
? and ? can be used to ANTAGONIZE NM blockade
neoSTIGmine
pyridoSTIGmine
drugs:
? and ? can increase NM blockade
Ca channel blockers, anesthetics i.e. isoflurane
two molecules of Ach bind to the receptors a ? in the receptor results in the opening of an ion channel which allows the passage of ? into the cell causing membrane depolarization
conformational change
sodium ions
in succinylcholine initially the muscles display disorganized ? which is followed by ?
contractions
flaccid paralysis
despite repolarization the membrane cannot be ? as long as succinylcholine is present- resembles ? of the nAChRs
depolarized
sensitization
With succinylcholine, ? results if a second dose is given ? minutes after the first
bradycardia
five
during prolonged muscle depolarization, excessive ? is lost and significant Na, Cl, and Ca are gained by the muscle. excessive damage to the soft tissue the K released can cause significant ? occasionally causing cardiac arrest
potassium
hyperkalemia
halothane followed by administration of ? results in ?
malignant hyperthermia
