Autonomic Nervous System Drugs

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AUTONOMIC NERVOUS SYSTEM Pharmacodynamics

DRUGS
 Mimics the action of acetylcholine on the
neurons in certain target organs in the body.
 They combine with receptors on the cell
CHOLINERGIC DRUGS membranes of target organs, then stimulate the
 Promote the action of the neurotransmitter muscle and produce:
 Salivation
 Acetylcholine.
 Bradycardia
 Also called parasympathomimetic drugs
 Vasodilatation
because they produce effects that imitate
 Bronchoconstriction
parasympathetic nerve stimulation.
 Increased activity of the GIT
 Enhance the action of acetylcholine, stimulating  Increased tone and contraction of the
the parasympathetic nervous system. muscles of the bladder
Two major classes:  Pupillary constriction

1. Cholinergic Agonists – “mimickers” Pharmacotherapeutics


 Mimic the action of acetylcholine  Cholinergic agonists are used to:
2. Anticholinesterase Drugs – “inhibitors”  Treat atonic or weak urinary bladder and
 Inhibits the destruction of acetylcholine at post- operative and postpartum urine
the cholinergic receptor sites. retention
Cholinergic Agonists  Treat GI disorders: postoperative
abdominal distention and GI atony
a. By directly stimulating cholinergic receptors,  Reduce eye pressure in patients with
they mimic the action of acetylcholine. glaucoma and during eye surgery
b. Include the following drugs:  Treat salivary gland hypofunction caused by
 Acetylcholine – rarely used clinically radiation therapy.
 Bethanecol
 Pilocarpine Adverse Reactions
 Carbachol  Nausea and vomiting
Major Uses:  Cramps and diarrhea
 Blurred vision
 Treatment of glaucoma, myasthenia gravis, and  Bradycardia
urinary retention.  Hypotension
 Shortness of breath
Route of Administration
 Urinary frequency
 Topically with eye drops  Increased salivation and sweating

 Orally
 Subcutaneous injection – more rapid than ANTICHOLINESTERASE DRUGS
oral and response is more effective
 Block the action of the enzyme acetyl
cholinesterase, which breaks down
acetylcholine, at cholinergic receptor sites,
Metabolism and Excretion preventing the breakdown of acetylcholine.
 Metabolized by cholinesterase:  As Ach builds up, it continues to stimulate
 At the muscarinic and nicotinic receptor the cholinergic receptors.
sites
 In the plasma Two categories:
 In the liver 1. Reversible
 All drugs in this class are excreted by the 2. Irreversible
kidneys
1. Reversible Nursing Alert
 have a short duration of action (minutes to
 Symptoms of cholinergic crisis
hours) and include:
(cholinergic drug toxicity)
 Ambenonium
 include severe abdominal cramping,
 Donepezil
diarrhea, excessive salivation, muscle
 Edrophonium
weakness, rigidity and spasm, and
 Neostigmine
clenching of the jaw.
 Physostigmine salicylate
 Pyridostigmine Treatment of over-dosage:
 Tacrine
 atropine (usual dosage of atropine is 0.4 to 0.6
Pharmacodynamics mg IV)
 other treatment also may be prescribed.
 Promote action of acetylcholine at receptor
sites. Possible Nursing Diagnoses
 Depending on the site, drug’s dose, and
duration of action, they can produce a stimulant  Disturbed Sensory Perception: Visual
or depressant effect on cholinergic receptors. related to adverse drug reactions or increased
pressure within the eye
Pharmacotherapeutics  Risk for Injury related to muscular weakness,
rigidity, or spasms due to drug overdose
 Reduce eye pressure in patients with glaucoma
 Diarrhea related to adverse drug reaction.
and during eye surgery
 Increase urinary bladder tone
 Improve tone and peristalsis through GIT in
patients with paralytic ileus CHOLINERGIC BLOCKING DRUGS
(ANTICHOLINERGIC DRUGS)
 Promote muscular contraction in patients with
myasthenia gravis  Interrupt parasympathetic nerve impulses in
 Diagnose myasthenia gravis (neostigmine and the CNS and ANS
edrophonium)  Prevent Ach from stimulating cholinergic
 Antidote to anticholinergic drugs, tricyclic receptors.
antidepressants, belladonna alkaloids, and  Do not block all cholinergic receptors, just the
narcotics muscarinic receptor sites.
 Treat mild to moderate Alzheimer’s dementia  Muscarinic receptors are cholinergic receptors
(Donepezil) that are stimulated by the alkaloid muscarine
Adverse Reactions and blocked by atropine.
Major Cholinergic Blockers
 Nausea and vomiting
 Diarrhea 1. Belladonna Alkaloids:
 Shortness of breath  Atropine – the prototype
 Wheezing or tightness in the chest  Belladonna
 Seizures  Homatropine
 Bradycardia  Hyoscyamine sulfate
 Hypotension  Scopolamine hydrobromide
 Respiratory depression
2. Synthetic Derivatives (Quarternary
Nursing Responsibilities: Ammonium drugs)
 Always encourage to change position slowly  Clidinium
to avoid dizziness  Glycopyrrolate
 Should be given as directed and the patient  Propantheline
carefully monitored for toxicity.
3. Tertiary Amines:
 Benztropine
 Dicyclomine Nursing Diagnoses
 Ethopropazine
 Disturbed Sensory Perception: Visual
 Oxybutynin related to adverse drug reaction
 Trihexyphenidyl  Impaired Oral Mucous Membranes
Pharmacotherapeutics related to drug action on mucous
membranes
 All cholinergic blockers are used to treat  Risk for Injury related to effect of drug
spastic or hyperactive GI and urinary  Constipation related to slowing of
tract conditions – relax muscles and peristalsis in the gastrointestinal tract
decrease GI secretions
 Propantheline is the drug of choice Nursing Responsibilities:
 Belladonna alkaloids are used with  Apply pressure to inner canthus for a few
morphine to treat biliary colic due to gallstones. seconds after opthalmic use for mydriasis
 Administered by IV injection to relax the GI  The antidote is physostigmine salicylate
smooth muscle.  Elderly patients to avoid exposure to high
 Atropine is given before surgery to: temperature or strenuous exercise to prevent
 Reduce oral and gastric secretions heat stroke. Encourage them to replace fluid
 Reduce secretions in the respiratory system and sodium intake
 Prevent a drop in heart rate caused by vagal  Encourage wearing of dark glasses if
nerve stimulation during anesthesia experiencing sensitivity to light
 Belladonna alkaloids can affect the brain
by:
1. Scopolamine ADRENERGIC DRUGS
 when given with morphine or meperidine
causes drowsiness and amnesia in the Adrenergic drugs are also called
patient having surgery sympathomimetic drugs
 used to treat motion sickness  They produce effects similar to those produced
2. Cholinergic blockers by the sympathetic nervous system.
 used to treat extrapyramidal (Parkinson-
like) symptoms caused by drugs and in
 Classified into two groups:
treating Parkinson’s disease
 Catecholamines
 Noncatecholamines
 Belladonna alkaloids have important
 Divided according to how they act:
therapeutic effects on the heart by:
a. Direct-acting
1. Atropine is the drug of choice to treat:
 Drug acts directly on the organ or tissue
a. Symptomatic Sinus Bradycardia
innervated by the SNS
b. Arrhythmias resulting from anesthetics
b. Indirect-acting
 Cholinergic blockers are used as cycloplegics:  Drug triggers the release of a
a. Paralyze the ciliary muscle of the eye neurotransmitter, usually
b. Alter the shape of the lens of the eye norepinephrine
 Cholinergic blockers are used as mydriatics: c. Dual-acting
a. Dilate the pupils of the eye – easier to  Can act both directly and indirectly
measure refractive errors during an eye  Therapeutic use of adrenergic drugs depend on
exam or to perform eye surgery. which receptors they stimulate and to what
Adverse Reactions degree.
a. Can affect the ff. receptors:
 Dry mouth  Alpha-adrenergic receptors
 Reduced bronchial secretions  Beta-adrenergic receptors
 Tachycardia  Dopamine receptors
 Decreased sweating
 Blurred vision
 Most adrenergic drugs produce their effects by  Norepinephrine has nearly pure alpha
stimulating alpha and beta receptors – mimic activity
the action of epinephrine and norepinephrine.  Dobutamine and isoproterenol have only
 Dopaminergic drugs act primarily on receptors beta- related activity
in the SNS stimulated by dopamine.  Epinephrine stimulates alpha receptors and
beta receptors
Catecholamines  Dopamine primarily exhibits dopaminergic
activity.
 Common properties:
 Stimulate the nervous system  Alpha adrenergic drugs:
 Constrict peripheral blood vessels  Treat hypotension caused by relaxation of
 Increase heart rate the muscles of the blood vessels (loss of
 Dilate the bronchi vasomotor tone) and blood loss due to
 Common catecholamines: hemorrhage.
 Dobutamine ( Dobutrex)  Beta1 adrenergic drugs:
 Dopamine ( Intropin)  Treat bradycardia, heart block, paroxysmal
 Epinephrine ( Adrenaline) atrial or nodal tachycardia, ventricular
 Norepinephrine (Levarterenol, Levophed) febrillation, asystole, and cardiac arrest.
 Isoproterenol ( Isuprel)  Beta2 adrenergic drugs:
 treat acute and chronic bronchial asthma,
Pharmacokinetics emphysema, bronchitis, and acute
hypersensitivity reactions to drugs.
 Cannot be taken orally because they are
 Dopamine:
destroyed by digestive enzymes.
 used in low doses to improve blood flow to
 Rapidly absorbed through the mucous
the kidneys because it dilates the renal
membrane if given sublingually.
blood vessels.
Pharmacodynamics  Manufactured catecholamines:
 have a short duration of action, which can
 Catecholamines are primarily direct-acting. limit their therapeutic usefulness.
 Cause either excitatory or inhibitory effect:
 Activation of alpha receptors generates an Adverse Reactions
excitatory response except for intestinal
 Restlessness
relaxation.
 Anxiety
 Activation of beta receptors mostly
 Dizziness
produces an inhibitory response except in
 Headache
the cells in the heart, where norepinephrine
 Palpitations
produces excitatory effects.
 Arrhythmias
 Clinical effects depend on the dosage and the  Hypotension
route of administration.  HPN and hypertensive crisis
 Catecholamines are potent inotropes – makes  Stroke
the heart contract more forcefully  Angina
 called: inotropic effect.  Hyperglycemia
 Also produce a positive chronotropic effect –  Tissue necrosis at injection site (I.V. dose leaks
cause the heart to have regular rhythm and fast into the surrounding tissue)
rate.
 As catecholamines cause vasoconstriction and Non-Catecholamines
rise of blood pressure, the heart rate can fall as Varied effects on the body:
the body tries to prevent excessive rise in blood
pressure.  Local or systemic vasoconstriction:
 Mephentermine
Pharmacotherapeutics
 Metaraminol
 Therapeutic use depends on the particular  Methoxamine
receptor activity that is activated.  Phenylephrine
 Nasal and eye decongestion and bronchiolar Adverse Reactions
dilation:
 Headache
 Albuterol
 Restlessness
 Ephedrine
 Anxiety or euphoria
 Isoetharine
 Irritability
 Metaproterenol
 Trembling
 Terbutaline
 Drowsiness and insomnia
 Smooth muscle relaxation
 Light-headedness
 Ritodrine
 Incoherence
 Terbutaline
 Seizures
Pharmacokinetics  Hypertension
 Hypotension
Absorption and Distribution  Palpitations
 Inhaled drugs (Albuterol) – gradually absorbed  Bradycardia
from the bronchi of the lungs and result in  Arrhythmias
lower drug levels in the body.  Cardiac arrest
 Oral drugs are absorbed well from the GIT.  Irregular heart rate and blood pressure in
 Ephedrine cross the BBB and can be found in pregnant woman and fetus
high concentrations in the brain and CSF.  Coldness or tingling
 Pallor or flushing
Metabolism  Angina
 Cerebral hemorrhage
 Occur primarily in the liver but can also occur
in the lungs, GIT, and in other tissues. Nursing Diagnoses
Excretion  Ineffective Tissue Perfusion related to
hypovolemia, blood loss, impaired
 Drug and metabolites are excreted primarily in
distribution of fluid, impaired circulation,
the urine.
impaired transport of oxygen across alveolar
 Acidic urine increases excretion
and capillary bed, other (specify)
 Alkaline urine slows excretion
 Decreased Cardiac Output related to
Pharmacodynamics altered heart rate and/or rhythm
 Imbalanced Nutrition: Less Than Body
 Can be direct-acting, indirect-acting, or dual-
Requirements related to adverse reaction
acting
(anorexia) to the drug
 Direct-acting that stimulates alpha activity:
 Disturbed Sleep Pattern related to
 Methoxamine and phenylephrine
adverse reactions (insomnia, nervousness)
 Selective to Beta2 activity: to the drug
 Albuterol, isoetharine, metaproterenol,
ritodrine, and terbutaline Nursing Responsibilities:
 Indirect-acting:
 Monitor v/s
 Phenylpropanolamine
 Monitor urinary output and assess bladder for
 Dual-acting: distention
 Ephedrine, mephentermine, metaraminol  Report S/E
 Pseudoepherine  Offer foods to avoid nausea & vomiting
Pharmacotherapeutics  With dopamine, check IV site frequently
because infiltration causes necrosis [antidote –
 Metaraminol causes vasoconstriction – used to Regitine (Phentolamine Mesylate)]
treat hypotension in severe shock
 Ritodrine is used to stop preterm labor
ADRENERGIC BLOCKING DRUGS  Bradycardia or tachycardia
 Edema
 Also called sympatholytic drugs
 Difficulty of breathing
 Used to disrupt the SNS function
 Light-headedness
 Blocks impulse transmission at adrenergic
 Flushing
neurons or adrenergic receptor sites by:
a. Interrupting the action of adrenergic drugs  Arrhythmias
b. Reducing available norepinephrine  Angina
c. Preventing the action of cholinergic drugs  Heart attack
 Classified according to their site of  Vasospasms
action:  Shock-like state
1. Alpha-adrenergic blockers
Nursing Responsibilities:
2. Beta-adrenergic blockers
 Encourage to take as prescribed & not to
Alpha-Adrenergic Blockers
abruptly stop taking the medication
 Interrupt the actions of epinephrine and  Avoid over the counter medications
norepinephrine at alpha receptors.  Avoid alcohol ingestion
 Results in:  Avoid hazardous activities until stable blood
 Relaxation of the smooth muscle in the levels are achieved
blood vessels  Report weight gain of more than 1 kg / week
 Increase vasodilatation Beta-Adrenergic Blockers
 Decrease blood pressure
 Representative drugs:  Most widely used adrenergic blockers
 Ergoloid mesylates  Prevent stimulation of the SNS by inhibiting the
 Ergotamine action of catecholamines at beta- adrenergic
 Phenoxybenzamine receptors
 Phentolamine  Commonly called Beta Blockers
 Prazosin  Can be selective or non-selective
 Ergotamine is a mixed alpha agonist and  Nonselective drugs affect:
antagonist and acts as an alpha blocker at high  Beta1 receptor sites – located mainly in the
doses. heart
 Beta2 receptor sites – located in the
Pharmacodynamics
bronchi, blood vessels, and uterus
 Alpha blockers interfere with the synthesis,  Include: Carvedilol, Labetalol, Levobunolol,
storage, release, and reuptake of Penbutolol, Pindolol, Sotalol, Nadolol,
norepinephrine by neurons. Propranolol, and Timolol.
 They antagonize epinephrine, norepinephrine,  Selective beta blockers primarily affect
or adrenergic drugs at alpha receptor sites. the Beta-1 sites only:
 Acebutolol
Pharmacotherapeutics  Atenolol
 Alpha blockers cause smooth muscles to relax  Betaxolol
and blood vessels to dilate, thus, increase local  Bisoprolol
blood flow to the skin and other organs and  Esmolol
reduce blood pressure.  Metoprolol tartrate
 Used to treat: Pharmacodynamics
1. Hypertension
2. Peripheral vascular disorders  Beta blockers have widespread effects in the
3. Pheochromocytoma body
 Produce blocking action not only at adrenergic
Adverse Reactions nerve endings but also in the adrenal medulla
 Orthostatic hypotension  Effects on the heart:
 Severe hypertension  Increased peripheral vascular resistance
 Decreased blood pressure
 Decreased force of cardiac contraction
Nursing Responsibilities:
 Decreased oxygen consumption of the heart
 Slowed conduction of impulses between  Encourage to always take meds as prescribed,
atria and ventricles of the heart no more, no less
 Decreased cardiac output  Instruct to never abruptly stop the medication
 Selective beta1 blockers are cardio-selective  Change position slowly or avoid sudden change
beta blockers because they reduce stimulation of position
of the heart.  Report constipation, urinary hesitancy or
 Nonselective beta blockers not only reduce bladder distention
stimulation of the heart but also cause
bronchiolar constriction – leading to
bronchospasms, especially in patients with
COPD. –which is not seen with cardio-selective
beta blockers.
Pharmacotherapeutics

 Clinical usefulness of beta blockers is based


largely on how they affect the heart.
 Clinical indications:
 Angina pectoris
 Hypertension
 Open-angle glaucoma
 Hypertrophic cardiomyopathy
 Supraventricular arrhythmias
 Cardiovascular symptoms of thyrotoxicosis
 Migraine headache
 Pheochromocytoma
 Essential tremors
 Anxiety

Adverse Reactions
 Hypotension
 Bradycardia
 Heart failure
 Peripheral vascular insufficiency
 Bronchospasm
 Diarrhea or constipation
 Nausea and vomiting
 Abdominal distention and flatulence
 Anorexia
 Skin rashes
 Respiratory distress due to allergic reaction
Nursing Diagnoses

 Ineffective Tissue Perfusion: Peripheral


related to adverse drug response
(hypotension)
 Risk for Injury related to vertigo,
dizziness, weakness, and syncope
secondary to orthostatic hypotension

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