Professional Documents
Culture Documents
Parkinsonism is characterized by a
combination of rigidity, bradykinesia,
tremor, and postural instability that
can occur for a variety of reasons but
is usually idiopathic (Parkinson's
disease or paralysis agitans).
Cognitive decline occurs in many
patients as the disease advances
Cardinal Features
Bradykinesia
Postural instability
Resting tremor (may have postural and
action components)
Rigidity
Motor Symptoms
Decreased dexterity
Dysarthria
Dysphagia
Festinating gait
Flexed posture
Freezing at initiation of movement
Hypomimia
Hypophonia
Micrographia
Slow turning
Autonomic Symptoms
Bladder and anal sphincter disturbances
Constipation
Diaphoresis
Orthostatic blood pressure changes
Paroxysmal flushing
Sexual disturbances
Other
Fatiguability
Oily skin
Pedal edema
Seborrhea
Weight loss
Anticholinergic Medications
Anticholinergic drugs can be effective
for tremor and dystonic features in
some patients but rarely show
substantial benefit for bradykinesia or
other disabilities.
They can be used as monotherapy or
in conjunction with other
antiparkinsonian drugs.
Amantadine
Amantadine is often effective for mild symptoms,
especially tremor. It may also decrease dyskinesia at
relatively high doses (400 mg/day).
Its precise mechanism of action is unknown but may
involve dopaminergic or nondopaminergic mechanisms
such as inhibition of N-methyl-d-aspartate receptors.
Adverse effects include sedation, vivid dreams, dry
mouth, depression, hallucinations, anxiety, dizziness,
psychosis, and confusion. Livedo reticularis (a diffuse
mottling of the skin) is a common but reversible side
effect
Cholinergic nerves are shown in blue; noradrenergic in red; and dopaminergic in green.
Note that some sympathetic postganglionic fibers release acetylcholine or dopamine
rather than norepinephrine. The adrenal medulla, a modified sympathetic ganglion,
receives sympathetic preganglionic fibers and releases epinephrine and norepinephrine
into the blood. ACh, acetylcholine; D, dopamine; Epi, epinephrine; M, muscarinic
Cholinoceptor-Activating &
Cholinesterase-Inhibiting Drugs
Acetylcholine-receptor stimulants and cholinesterase
inhibitors together make up a large group of drugs
that mimic acetylcholine (cholinomimetic agents)
Cholinoceptor stimulants are classified
pharmacologically by their spectrum of action,
depending on the type of receptormuscarinic or
nicotinicthat is activated.
Cholinomimetics are also classified by their
mechanism of action because some bind directly to
(and activate) cholinoceptors whereas others act
indirectly by inhibiting the hydrolysis of endogenous
acetylcholine
Anticholinergic
Cholinergic blocking drugs also are
called anticholinergics or
parasympathomimetic blocking
drugs.
Examples of cholinergic blocking
drugs include atropine, scopolamine,
and propantheline
ACTIONS
Cholinergic blocking drugs inhibit the
activity of acetylcholine in
parasympathetic nerve fibers
When the activity of acetylcholine is
inhibited, nerve impulses traveling
along parasympathetic nerve fibers
cannot pass from the nerve fiber to
the effector organ or structure.
Antimuscarinic Agents
Atropine
a tertiary amine belladonna alkaloid, has a
high affinity for muscarinic receptors,
where it binds competitively, preventing
acetylcholine from binding to those sites .
Atropine acts both centrally and
peripherally.
Pharmacokinetics:
Atropine is readily absorbed, partially
metabolized by the liver, and
eliminated primarily in the urine.
It has a half-life of about 4 hours.
Therapeutic uses
Ophthalmic: In the eye, topical atropine
exerts both mydriatic and cycloplegic
effects
Shorter-acting antimuscarinics
(cyclopentolante and tropicamide) have
largely replaced atropine due to
prolonged mydriasis observed with
atropine (7-14 days versus 6-24 hours
with other agents).
Adverse effects:
Depending on the dose, atropine may
cause dry mouth, blurred vision,
tachycardia, and constipation.
Effects on the CNS include restlessness,
confusion, hallucinations, and delirium,
which may progress to depression, collapse
of the circulatory and respiratory systems,
and death.
Low doses of cholinesterase inhibitors such
as physostigmine may be used to
overcome atropine toxicity.
Scopolamine
Actions:
Scopolamine is one of the most
effective antimotion sickness drugs .
Scopolamine also has the unusual effect
of blocking short-term memory.
In contrast to atropine, scopolamine
produces sedation, but at higher doses
it can produce excitement instead.
Scopolamine may produce euphoria and
is subject to abuse
ADVERSE REACTIONS
Central nervous systemheadache, flushing,
nervousness, drowsiness, weakness, insomnia,
nasal congestion, fever
Eyesblurred vision, mydriasis, photophobia,
cycloplegia, increased ocular tension
Gastrointestinal tractnausea, vomiting, difficulty
in swallowing, heartburn
Urinary tracturinary hesitancy and retention,
dysuria
Cardiovascular systempalpitations, bradycardia
(after low doses of atropine), tachycardia (after
higher doses of atropine)
Otherurticaria, anaphylactic shock, other skin
manifestations
CONTRAINDICATIONS