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(Parasympathomimetics,
Cholinomimetics)
Assoc. Prof. I. Lambev
E-mail: itlambev@mail.bg
Activation of ocular
parasympathetic
fibers results in narrowing of the pupil
and increased curvature of the lens,
enabling near
objects to be
brought into focus
(accommodation).
CHOLINERGIC NERVES
The NM-receptor
is a macroprotein with
5 subunits, which are
arranged like a rosette
surrounding the Na+
channel. The two alpha
subunits carry two ACh
binding sites with negatively charged groups
which combine with the
cationic group of ACh
and open Na+ channel.
N-receptor: 5 subunits
(2) Alkaloids
a) stimulants of M-receptors:
Pilocarpine, Cevimeline (dry mouth),
Bethanechole, Musacarine, Phalloidin
b) stimulants of N-receptors:
Nicotine, Cytisine (Tabex), Lobeline
4+
Ionization!!!
BBB
M- N-effects of ACh
A 1 min
200
150
100
50
M-
M-
effect
effect
ACh
2 mcg i.v.
ACh
50 mcg
Neffect
ACh
Atropine ACh
2 mg i.v. 50 mcg 5 mg
Pilocarpus
jaborandi
Pilocarpine
- in glaucoma
Pilocarpine Hydrochloride
eye drops (Pilocar)
- sol. 1%, 2%, 4%
- in open angle glucoma
Applied to the eye, it
penetrates cornea and
promptly causes
miosis, ciliary muscle contraction, and fall in intraoccular
tension (< 22 mm) lasting 4-8 h.
Side effect: painful spasm of
accommodation for near vision.
Systemic effects:
sweating, salivation
Cardiovascular effects: in small doses fall in BP, but in high
doses elicits rise in BP and tachycardia, probably due to
ganglionic stimulation (through muscarinic receptors)
Development of
angle closure
glaucoma and
its reversal
by miotics
Autonomic
control
of pupil (A)
and site
of action of
mydriatics (B)
and
miotics (C)
Galantamine is antiChEs
with direct N-action used in:
Myastenia gravis
Alzheimers disease
Poliomyelitis
Postoperative paresis of GIT and bladder
As antagonist of competitive
myorelaxants with less
side effects than neostigmine
Prof. D. Paskov
(19141986)
Galantamine
(Nivalin)
Enlargement ventricles
Diminished hypothalamus
Alzheimer's disease