Pharmacology for Dentistry

(Ben Green) #1
Parasympathomimetics (Cholinergic Agents) 157

bladder and increase in the frequency of
ureteral peristaltic waves.


Acetylcholine causes bronchoconstriction
and increase in bronchial secretion and can
precipitate the bronchial asthma.


Effect on secretions: Acetylcholine
increases the salivary, sweat, lacrimal,
nasopharyngeal, gastric and bronchial
secretions. All these secretory effects
are blocked by atropine and enhanced
by cholinesterase inhibitors e.g. phys-
ostigmine.


Effect on eye: After intraconjunctival
instillation, acetylcholine causes miosis, due
to contraction of circular muscles of the iris
and fall in intraocular tension.


Nicotinic Actions


Effect on autonomic ganglia: It can
cause stimulation of sympathetic and
parasympathetic ganglia and stimulation of
adrenal medulla, which leads to rise in
arterial blood pressure due to peripheral
vasoconstriction.


Effect on myoneural junction:
Acetylcholine cause stimulation of skeletal
muscles and in larger concentration at the
myoneural junction can produce paralysis
of skeletal muscles.


Effect on CNS: Acetylcholine when
injected parenterally does not cross blood
brain barrier being a quarternary
ammonium compound and does not have
any central action.


Therapeutic Uses


Because of nonselective actions,
acetylcholine can not be used for any
therapeutic purpose.


CHOLINOMIMETIC DRUGS

METHACHOLINE
It is effective orally and resistant to
pseudo-cholinesterase and possesses longer
duration of action. Its nicotinic action is less
than acetylcholine and actions are more
marked on CVS as compared to GIT and
urinary system. Earlier it was used for CVS
disorders such as peripheral vascular
disease and paroxysmal supraventricular
tachycardia. But now, it is rarely used in
therapeutics.

CARBACHOL
It is resistant to both true and pseudo-
cholinesterase and is more potent than
methacholine and action is more prolonged.
It is used topically for ophthalmic purpose.

BETHANECHOL
It is resistant to hydrolysis by both true
and pseudocholinesterase and has mainly
muscarinic actions. It has been used in
postoperative and postpartum non-
obstructive urinary retention and
gastroesophageal reflux.

PILOCARPINE
It is a natural alkaloid obtained from leaves
of Pilocarpus microphyllus and Pilocarpus
jaborandi. Pilocarpine is direct acting
muscarinic agonist. It acts on M 3 receptor. It
produces contraction of iris to produce miosis.
It also stimulates ciliary muscle resulting in
increased accommodation and improved
outflow of aqueous humor. As a result of
miosis the pressure on canal of Schlemm is
reduced and hence improves drainage and
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