Pharma5 CNS Drugs

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DRUGS AFFECTING THE

AUTONOMIC & CENTRAL


NERVOUS SYSTEM
Merchie Lissa T. Alabat, RN
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The Nervous System
Center of thinking, memory, judgement,
sensation, movement, cognition,
communication, behavior, and personality
Innervates many other body systems and
indirectly influences their actions

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Nervous system is divided into:

Central Nervous System (CNS)
Brain
Spinal cord
Peripheral Nervous System (PNS)
Cranial nerves
Spinal nerves
Autonomic NS
Sympathetic
Parasympathetic NS
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Nervous System Cells
There are two main types of brain cells:
Neurons
Neuroglial cells
- Provide protection, structure and nutrition to the
neurons
4 types:
1. Astroglial
2. Ependymal
3. Oligodendrocytes
4. Microglial

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Neurons

Basic structural and functional units of the
nervous system
Cannot divide by mitosis
Respond to physical and chemical stimuli
Produce and conduct electrochemical impulses
Release chemical regulators

*The brain contains approximately more than 20
billion nerve cells, or Neurons

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Cell body (perikaryon)
Nutrition center
Cell bodies within CNS clustered into nuclei, and
in PNS in ganglia

Axons
Transmits impulses from its cell body to other
neurons

Dendrites
Provide receptive area
Transmit electrical impulses to cell body

Parts of a Neuron
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Synapses

Impulses are transmitted to their final
destination through synapses
Types:
Neuron to neuron
Neuron to gland


Conduction of impulse across synapse:
Pre-synaptic neuron

release neurotransmitter

synaptic cleft

neurotransmitter interacts with receptor

neurotransmitter-receptor complex initiates a
sequence of events (open ion channel)

modulate the electrical activity of the
postsynaptic neuron
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Neurotransmitters

Chemical substances manufactured in the
neuron that aid in the transmission of
information throughout the body.
Chemicals that take a nerve signal across
the synaptic gap between a sending
neuron, and a receiving one.
Excitatory or inhibitory
Neurotransmitters
Dopamine(DA) Monoamines- Catecholamines
Norepinephrine (NE)
Serotonin (5HT) Monoamines- Indolamines
Acetylcholine (Ach) Cholinergics
Glutamate (Glu) Amino Acids
Gamma-Aminobutyric Acid
(GABA)
Amino Acids
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NAME LOCATION(S)
DOPAMINE Brain, smooth muscle
SEROTONIN Brain
NORADRENALINE/
NOREPINEPHRINE
Brain, smooth muscle
ACETYLCHOLINE (ACH)
Parasympathetic nervous system,
brainstem, neuromuscular
junction
GABA Brain
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Mechanism of Drugs on CNS
(1)Axon: Slow/block axonal electrical conduction
e.g. Antiepileptics
Anaesthetics

(2)Synapse: most drugs

1. Affect transmitter:
- synthesis, storage, release, reuptake.
e.g. antidepressants
2. Affect receptor: activation/inhibition(block)
e.g. benzodiazepines, antipsychotics
3. Directly act on ion channels
e.g. phenytoin
Blood Brain Barrier
(1) Structure

3 parts:
barrier between blood and brain cell;
barrier between blood and cerebrospinal fluid
barrier between brain cell and cerebrospinal fluid.

(2) Function: restrict passage of polar compounds and
macromolecules from blood into brain
(3) Pharmacological significance: prerequisite
e.g. Penicillinmeningitis
AUTONOMIC NERVOUS
SYSTEM DRUGS
CHOLINERGIC DRUGS
Promote the action of the neurotransmitter
acetylcholine
Called parasympathomimetic drugs
because they produce effects that imitate
parasympathetic nerve stimulation
2 Major Classes
CHOLINERGIC AGONISTS- mimic the
action of neurotransmitter acetylcholine

ANTICHOLINISTERASE DRUGS-work by
inhibiting the destruction of acetylcholine
at the cholinergic receptor sites
CHOLINERGIC AGONISTS
INCLUDE DRUGS SUCH AS:
Bethanecol
Carbachol
Cevimiline
Pilocarpine
PHARMACOKINETICS
No IM or IV
Usually: orally, topically (eye drops), subQ

METABOLISM/EXCRETION
Metabolized at muscarinic and nicotinic
recepetor sites
In the plasma portion of blood
In the liver
ALL DRUGS IN THIS CLASS ARE
EXCRETED BY THE KIDNEYS

PHARMACODYNAMICS
Work by mimicking the action of acetycholine on
the neurons in certain organs of the body called
target organs. When they combine with receptors
on the cell membranes of target organs, they
stimulate the muscle and produce:
Salivation
Bradycardia
Dilation of blood vessels
Constriction of bronchioles
Increased activity of the GI tract
Increased tone and contraction of the bladder muscles
Constriction of the pupils
PHARMACOTHERAPEUTICS
Cholinergic drugs are used to:
Treat atonic (weak) bladder conditions and
post-op and post-partum urine retention
Treat GI disorders, such as post-op
abdominal distention and GI atony
Reduce eye pressure in patients with
glaucoma and during eye surgery
Treat salivary gland hypofucntion caused by
radiation therapy or Sjogrens syndrome
ADVERSE EFFECTS
Side effects to
expect:
Nausea
Vomiting
Abdominal
cramping
Dizzines
Hypotension
Side effects to
report:
Bronchospasm
Wheezing
Bradycardia

NURSING RESPONSIBILITES
Take baseline VS of
HR and BP

ANTICHOLINISTERASE
DRUGS
Also known cholinergic-blocking agents
Block the action of the enzyme
acetylcholinisterase (which breaks down
the neurotransmitter acetylcholine) at
cholinergic receptor sites, preventing the
breakdown of acetylcholine
As acetylcholine builds up, it continues to
stimulate the cholinergic receptors
2 CATEGORIES
REVERSIBLE
Edrophonium
Neostigmine
Pyridostigmine

IRREVERSIBLE


PHARMACOKINETICS
Generally absorbed by the GI tract, subQ
and mucous membranes
METABOLISM- by enzymes in the plasma
EXCRETED in the urine
PHARMACODYNAMICS
Promote the action of acetycholine at
receptor sites
Depending on the site and the drugs dose
and duration of action, they can produce a
stimulant or depressant effect on
cholinergic receptors
PHARMACOTHERAPEUTICS
- To reduce eye pressure
in patients with glaucoma
during eye surgery
- To increase bladder tone
- To improve tone and
peristalsis through the GI
tract in patients with
reduced motility or
paralytic ileus
- To promote muscle
contraction in patients
with myasthenia gravis
To diagnose myasthenia
gravis (NEOSTIGMINE &
EDROPHONIUM)
As an antidote to
cholinergic blocking
agents, TCA, belladona
and narcotics
To treat mild to moderate
dementia and enhance
cognition in patients wih
Alzheimers disease
ADVERSE EFFECTS
Side effects to expect:
Blurred vision
Constipation
Urinary retention,
dryness of the mucosa
of the mouth, nose
and throat
Side effects to report:
Confusion
Depression
Nightmares
Hallucinations
Palpitations
Orthostatic
hypotension
Arrythmias
Glaucoma
NURSIING
RESPONSIBILITIES
All patients should be
screened for the
presence of closed-
angle glaucoma
Check for history of
enlarged prostate
Take baseline VS of
HR and BP
Sucking on candy or
ice chips for dry
mouth
Give stool softeners
as prescribed for
constipation.
Encourage adequate
fluid intake and privde
sufficient bulk
Promote saferty for
blurring of vision

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