Atropine
Pharmaceutics
 Structure
 MOA: competitive
inhibition of mACRs,
no nACR effects
unless high dose
 Route
Pharmacokinetics
 Oral bioavailability
 Onset/duration
 Distribution
 Protein binding
 Metabolism
 T1/2B
Pharmacodynamics
 CNS
 CVS
 Resp
 GIT/GUT
 With reversal of ND
NMBs with ACEis
Glycopyrulate Hyoscine
 Tertiary amine,  Quaternary amine.  Tertiary amine,
racemic mixture only Thus glycopyrulate racemic mixture only
L isomer active cannot cross BBB L active
and placenta,
increased risk of
CNS/ CCS/ ocular
side effects
 IV
 IV  IV, PO, transdermal
 20%, thus not given  5-20%, thus not  50%, can be given
orally given orally oral
 Onset 1 min,  Onset 3 mins,  shorter duration
duration 1 hr, duration 2 hr, better than atropine
therefore better for for medium acting
severe vagal ACEi (neostigmine)
bradycardia, or for
faster acting ACEi
(edrophonium)
 Vd 3L/kg  0.2L/kg
 2L/kg
 50%
 10%
 Extensive  Minimally
 Extensive
metabolism by metabolised 20%, metabolism by
hepatic esterases 80% excreted hepatic esterases
80%, 20% excreted unchanged in urine 99%, 1% excreted in
in urine unchanged (therefore caution in urine unchanged
renal failure)
 2.5hrs  1hr  2.5hrs
 Crosses BBB (tertiary  Does not cross BBB  Crosses BBB (tertiary
amine), mydriasis, (quaternary amine), amine), thus similar
agitation, sedation, no CNS side effects to atropine, more
amnesia, risk of CCS, potent CNS effects
increased IOP and thus more ideal for
risk in closed angle pre medication but
glaucoma increased risk of CCS
 Tachycardia (inhibits  Similar to atropine,
 Similar to atropine,
M2R at SA), minimal but less CVS side
but slower onset
vasodilation. More effects
and less CVS effects
potent and faster
onset CVS effects
than others, thus
most ideal for vagal
bradycardia. At low
dose can cause initial
bradycardia
 Inhibits secretions,
bronchodilates, less  More effective
 More effective
effective than others antisialogogue than
antisialogogue than
atropine, due to CNS
atropine
effects as well, ideal
 Anti-emetic,
premedication
constipation, urinary
retention, dry mouth  Similar to atropine,
 No antiemesis, as commonly used for
does not cross BBB anti emesis and
 Faster onset, ideal
motion sickness
with faster onset
 Not used, as has
ACEi (edrophonium),  Slower onset ideal central side effects,
but has central side with slower onset slower waking from
effects (dose ACEis (neostigmine),
20mcg/kg) no central side GA
effects (dose
8mcg/kg)