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Drugs Acting on the CNS and PNS 2011 Mps

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Pharmacology by karch
15
Major P. Salipot, RN Page 1 of 15 St. Mary’s College Selected Neurotransmitters Acetycholine – communicates between nerve and muscle. Norepinephrine/epinephrine – found in limbic system; involved in arousal Dopamine – involved in coordination of impulses and responses (motor and intellectual) GABA – inhibits nerve activity and impt in preventing overexcitability or stimulation such as seizure Serotonin – found in limbic system, impt for arousal and sleep; prevent depression and promote motivation. ANTIANXIETY A void abrupt discontinuation after prolonged use N ot give if increase BP, renal/hepatic dysfunction or history of drug abuse X anax, Ativa, Serax - a few examples I ncrease in 3 D’s- drowsiness, dizziness, decrease BP E nhances action of GABA T each to rise slowly from supine Y es, alcohol should be avoided Anxiolytic and Hypnotic agents Anxiolytics – prevents feelings of tension or fear Sedatives - calm patients and make them unaware of the environment Hypnotics - cause sleep Minor tranquilizers – causes state of tranquility in anxious patients STATES AFFECTED BY ANXIOLYTIC AND HYPNOTIC DRUGS 1. Anxiety - feeling of tension, nervousness, apprehension, or fear that usually involves unpleasant reactions to a stimulus , whether actual or unknown 2. Sedation - loss of awareness and reaction to environmental stimuli a. For patients who are restless, nervous, irritable or overreacting to stimuli 3. Hypnosis – extreme sedation results in further CNS depression and sleep a. Act on RAS BENZODIAZEPINES - most frequently uses anxiolytic drug - prevents anxiety without much sedation - act on limbic system and RAS to make GABA more effective - peak 30 mins - lipid soluble - cross the placenta/ enters the milk - Schedule IV Indication: anxiety disorders, alcohol withdrawal, hyperexcitability and agitation pre-op relief of anxiety and tension to aid in balanced anesthesia Contraindication: - allergy - acute alcohol intoxication - psychosis - pregnancy - acute narrow-angle glaucoma - shock Adverse Reaction: - headache - dizziness - drowsiness - cognitive impairment - nervousness - lethargy - palpitation - nausea - dry mouth - vomiting Overdose: - hypotension and respiratory depression - somnolence, confusion, coma, diminished reflexes - only if taken with CNS depressants such as alcohol and barbiturates - nursing intervention: do not give syrup of ipecac (this is contraindicated if pt has ingested a medication that can cause sedation) o gastric lavage Flumazenil - treat benzodiazepines overdose - reverse sedation caused by benzodiazepines that are used as adjunct anesthesia - reverse sedation produced for diagnostic tests and other medical procedures 1. diazepam (Valium) - prototype - anxiety, alcohol withdrawal, muscle relaxant, antiepileptic, antitetanus, pre-op anxiolytic - monitor injection sites 2. estazolam (Prosam) - hypnotic, txt of insomia - give with food to minimize GI upset 3. flurazepam (Dalmane) - give 15 – 30 mins before bedtime - causes less REM rebound than any other benzodiazepines 4. halazapam (Paxipam) 5. lorazepam (Ativan) - prototype 6. temazepam (Restoril) - induces sleep within 20 – 40 mins - give 20 – 30 mins before bedtime 7. clonazepam (Klonapin) - seizure, panic attacks, neuralgia 8. clorazepate (Tranxene) - anxiety, alcohol withdrawal, adjunct therapy for Partial seizure 9. chlordiazepoxide (Librium) first benzodiazepene BARBITURATES - 1 st introduced in 1903 - standard drug for tx of insomia and producing sedation
Transcript
Page 1: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 1 of 15 St. Mary’s College

Selected Neurotransmitters

Acetycholine – communicates between nerve and muscle.

Norepinephrine/epinephrine – found in limbic system; involved in arousal

Dopamine – involved in coordination of impulses and responses (motor and

intellectual)

GABA – inhibits nerve activity and impt in preventing overexcitability or

stimulation such as seizure

Serotonin – found in limbic system, impt for arousal and sleep; prevent

depression and promote motivation.

ANTIANXIETY

A void abrupt discontinuation after prolonged use

N ot give if increase BP, renal/hepatic dysfunction or

history of drug abuse

X anax, Ativa, Serax - a few examples

I ncrease in 3 D’s- drowsiness, dizziness, decrease BP

E nhances action of GABA

T each to rise slowly from supine

Y es, alcohol should be avoided

Anxiolytic and Hypnotic agents

Anxiolytics – prevents feelings of tension or fear

Sedatives - calm patients and make them unaware of the environment

Hypnotics - cause sleep

Minor tranquilizers – causes state of tranquility in anxious patients

STATES AFFECTED BY ANXIOLYTIC AND HYPNOTIC DRUGS

1. Anxiety - feeling of tension, nervousness, apprehension, or fear that usually

involves unpleasant reactions to a stimulus , whether actual or unknown

2. Sedation - loss of awareness and reaction to environmental stimuli

a. For patients who are restless, nervous, irritable or overreacting to stimuli

3. Hypnosis – extreme sedation results in further CNS depression and sleep

a. Act on RAS

BENZODIAZEPINES

- most frequently uses anxiolytic drug

- prevents anxiety without much sedation

- act on limbic system and RAS to make GABA more effective

- peak 30 mins

- lipid soluble

- cross the placenta/ enters the milk

- Schedule IV

Indication:

anxiety disorders,

alcohol withdrawal,

hyperexcitability and agitation

pre-op relief of anxiety and tension to aid in balanced anesthesia

Contraindication:

- allergy - acute alcohol intoxication

- psychosis - pregnancy

- acute narrow-angle glaucoma - shock

Adverse Reaction:

- headache - dizziness

- drowsiness - cognitive impairment

- nervousness - lethargy

- palpitation - nausea

- dry mouth - vomiting

Overdose:

- hypotension and respiratory depression

- somnolence, confusion, coma, diminished reflexes

- only if taken with CNS depressants such as alcohol and barbiturates

- nursing intervention: do not give syrup of ipecac (this is contraindicated if pt

has ingested a medication that can cause sedation)

o gastric lavage

Flumazenil

- treat benzodiazepines overdose

- reverse sedation caused by benzodiazepines that are used as adjunct

anesthesia

- reverse sedation produced for diagnostic tests and other medical procedures

1. diazepam (Valium)

- prototype

- anxiety, alcohol withdrawal, muscle relaxant, antiepileptic, antitetanus, pre-op

anxiolytic

- monitor injection sites

2. estazolam (Prosam)

- hypnotic, txt of insomia

- give with food to minimize GI upset

3. flurazepam (Dalmane)

- give 15 – 30 mins before bedtime

- causes less REM rebound than any other benzodiazepines

4. halazapam (Paxipam)

5. lorazepam (Ativan) - prototype

6. temazepam (Restoril)

- induces sleep within 20 – 40 mins

- give 20 – 30 mins before bedtime

7. clonazepam (Klonapin) - seizure, panic attacks, neuralgia

8. clorazepate (Tranxene) - anxiety, alcohol withdrawal, adjunct therapy for Partial

seizure

9. chlordiazepoxide (Librium) first benzodiazepene

BARBITURATES

- 1st introduced in 1903

- standard drug for tx of insomia and producing sedation

Page 2: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 2 of 15 St. Mary’s College

- habit forming; low therapeutic index

- Category D

Mechanism of Action

- acts on reticular formation

- reduces nerve impulse traveling to the cortex

- potentiate GABA

- raises seizure threshold

- enzyme- inducer (stimulates enzyme responsible for metabolism and

breakdown in the liver of many drugs causing quick biotransformation

Contraindicaiton: drug allergy, respiratory difficulty, liver disease

Adverse reaction: drowsiness, lethargy, dizziness, excitement

Overdose: respiratory depression to respiratory arrest

- sleep, profound coma, death

- cold clammy skin

- fever, areflexia, tachycardia, hypotension

- TX: symptomatic, supportive

o Activated charcoal ( pulls drug from the circulation and eliminating it

by GIT

o Forced diuresis

Drug Interaction:

- alcohol, antihistamine, benzodiazepines, opioids, tranquilizers

- MAOI prolonged barbiturate effect

- Anticoagulant decrease coagulation and possible clot formation

- Oral contraceptives increase metabolism of contraceptive drug

pentobarbital (Nembutal)

- principally used pre-op to relieve anxiety and provide sedation

phenobarbital (Luminal)

- most commonly prescribed

- prototype

- long-acting

- prevents generalized tonic-clonic seizures

- for fever-induced convulsions

- for neonatal hyperbilirubinemia

amobarbital (Amytal sodium)

- sedative/hypnotic; convulsions; manic reactions

secobarbital (Seconal)

- preanesthetic sedation; convulsive seizure of tetanus

Nursing interventions:

1. give slow IV.

2. provide standby life support facilities

3. taper dosage gradually

4. provide comfort measures

5. provide thorough patient teachings

6. do not administer these drugs intra-arterially

7. do not mix IV drugs in solution with other drugs

OTHER ANXIOLYTIC AND HYPNOTIC DRUGS

1. chloral hydrate (Aquachloral)

a. Oldest non-barbiturate sedative-hypnotic

b. Frequently used to produce nocturnal sedation

c. Can cause tachyphylaxis (rapid appearance of a progressive

decrease in response to a pharmacologically or physiologically

active substance after its repetitive administration)

2. antihistamine (promethazine [Phenergan], diphenhydramine [Benadryl])

a. used to decrease need for narcotics

b. monitor for thickened respiratory secretion

3. buspirone (Buspar)

a. No sedative, anti-convulsant or muscle relaxant properties

ANTIDEPRESSANTS OR MOOD ELEVATORS

used to treat depressive disorders caused by emotional or environmental

stressors, losses, drugs, disease states such as cerebrovascular accidents or

depression that cannot be related to identifiable cause

these drugs are classified as:

o tricyclic antidepressants (TCAs)

o monoamine oxidase inhibitors (MAOI)

o selective serotonin reuptake inhibitors (SSRI)

TRICYCLIC ANTISEPRESSANTS (TCA)

for patients with insomnia, decreased libido, loss of appetite, feelings of

worthlessness

increases the levels of neurotransmitters serotonin or norepinephrine in the

space between nerve endings

1. nortriptyline (Pamelor)

2. amitriptyline (Elavil)

3. clomipramine (Anafranil)

4. desipramine ( Norpramin)

5. imipramine (Tofranil)

6. doxepin ( Sinequan)

Nursing responsibilities:

1. Asses the patients level or severity of depression, including the presence of

suicidal ideation

2. identify usual coping mechanism

3. Observe for side effects ( dry mouth, blurred vision, tachycardia, urinary

retention, constipation)

4. Observe for drug interaction

5. Observe for therapeutic effects of TCAs 2 to 3 weeks after the initial dose -

therapeutic window (serum plasma level)

If no therapeutic response occurs in 4 weeks to 8 weeks, another drug is prescribed.

Patient education:

1. Take drug as prescribed.

Page 3: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 3 of 15 St. Mary’s College

2. Avoid taking OTC cold remedies or drugs without the physician’s knowledge.

Antihistamine and narcotic analgesics will increase the effect.

3. Avoid excessive exercise and high temperature because anticholinergic

effects of these agents block perspiration.

MONOAMINE OXIDASE INHIBITORS (MAOI)

Well known for their multiple drug and food interactions because they inhibit

the enzyme that breaks down amino acid tyramine and tryptophan

An accumulation of these substances triggers the release of norepinephrine

and a HYPERTENSIVE CRISIS can occur

Clinical symptoms:

i. Elevated Bp

ii. Headache

iii. Diaphoresis

iv. Dilation of pupil

v. Rapid heart rate and arrhythmia

vi. Intracerebral hemorrhage

DIET RESTRICTIONS FOR PATIENTS ON MAOI THERAPY

High tyramine content

(avoid while on MAOI

therapy)

Moderate tyramine

content

(May eat occasionally

while on MAOI therapy)

Low tyramine Content

(Limited quantities

permissible while on

MAOI therapy)

Aged cheese (cheddar,

Swiss, camembert, blue

cheese, parmesan,

provolone, Romano, brie)

Raisins, fava beans, flat

Italian beans, Chinese

pea pods

Red wines (Chianti,

burgundy, sauvignon)

Smoked and processed

meats (salami. Bologna,

pepperoni, summer

sausage)

Caviar, pickled herring,

corned beef, chicken of

beef liver

Soy sauce, brewer’s

yeast, meat tenderizer

Gouda cheese,

processed American

cheese, mozzarella

Yogurt, sour cream

Avocados, banana

Beer, white wine, coffee,

colas, tea, hot chocolate

Meat extracts, such as

bouillon

Chocolate

Pasteurized cheese 9

cream cheese, cottage

cheese, ricotta)

Figs

Distilled spirits (in

moderation)

1. tranylcypromine (Parnate)

2. isocarboxazid (Marplan)

3. phenelzine (Nardil)

Maximum therapeutic effect: 2 – 6 weeks of therapy

Medication for overdose:

phentolamine (Regitine) for excessive response

diazepam ( valium) for excessive agitation

Patient Education:

1. take drugs as prescribed.

2. avoid ingestion of tyramine-containing foods

3. report any symptoms indicative of hypertensive crisis, such as headache and

palpitations

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI)

became popular because of its advantageous safety profile and its broad

spectrum of potential indications

depend on neuronal release of serotonin for their action, which is blocking

of neuronal uptake of serotonin

the inhibition of serotonin reuptake into the nerve terminal by an SSRI

increases synaptic transmitter levels to exert a clinically significant

antidepressant effect

used in treatment of depression alone or in the presence of concurrent

disorders such as anxiety, panic attacks, eating disorders, sleep

disorders, alcoholism, or schizophrenia

Generic name Trade name

Sertraline Zoloft

Fluoxetine Prozac

Fluvoxamine Luvox

Paroxetine Paxil

cetaprolam Celexa

Client education:

1. Take the dugs as prescribed. Avoid altering the dosage of the medication.

Contact the physician before discontinuing use of the drug.

2. Report any unusual symptoms such as tremors, nausea and vomiting, anorexia,

weight loss, nervousness, or sexual dysfunction

3. Avoid the use diazepam, alcohol and tryptophan.

4. Inform the physician if taking anticoagulant or theophylline

5. Avoid operating hazardous machinery, including automobile if drowsiness

occurs.

6. have the blood pressure and pulse monitored initially and after each dosage

change to detect hypotension, hypertension, and irregular heart rates

ANTIPSYCHOTICS

Action: Blocks dopamine receptor sites in the brain. There is a depression of the limbic

system and cerebral cortex that controls aggression. Antiemetic effects by inhibiting the

chemoreceptor trigger zone in the medulla. May inhibit anticholinergic, antihistamine

and/or sedative effects.

Page 4: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 4 of 15 St. Mary’s College

Indications: Schizophrenic disorders, mania, agitated organic disorders, delusional

disorders, antiemetic, intractable hiccups. Preoperative sedation (i.e. Compazine,

Phenergan)

Warnings: Alcoholism, other CNS depression, hepatic, renal or coronary disease,

cerebral insufficiency, severe hypotension, glaucoma, bone marrow depression, blood

dyscrasias; young children. Use cautiously in elderly debilitated clients.

Undesirable effects: STANCE on the next page will help you remember these effects.

Other specific information: Alcohol, CNS depressants may increases CNS and respiratory

depression, TCA and MAOI may increase sedation, hypotensive and anticholinergic

effects. Decrease levodopa effects. Lithium, antacids, and antidiarrheals may decrease

absorption.

Interventions: Monitor periodic liver function tests. WBC, serum glucose, VS and

psychological testing during therapy. Orthostatic hypotension is likely to occur, rise

slowly with assistance and initiate safety measures. Suicidal precautions, if necessary. Do

not mix parenteral solutions with other drugs in same syringe. Give deep IM injections.

Following parenteral route, remain in supine position for at least 30 minutes/ Liquids

should be protected from light and should be diluted with fruit juice before

administering. Avoid skin contact with oral suspension solution. Treat extrapyramidal

symptoms with anticholinergics (i.e. Cogenin0. Discontinue at least 48 hours prior to

surgery.

Education: teach that urine may urn pink or reddish brown. Advise that he medication

may take 6 weeks or linger to achieve a therapeutic effect. Instruct to give the daily

dose 1-2 hours before bedtime. Oral concentrate must be diluted in 2- 3 oz. fluid (water,

fruit juice, carbonated drink or milk). Avoid sun exposure, (use sunblock). Caution

against driving a car. Explain the importance of reporting sore throat, fever or symptoms

of infection. Undesirable effects usually subside approximately 2 weeks of therapy

decrease by dose adjustment. Inform other providers when taking these drugs. Advise

client to wear an ID bracelet indication medication therapy.

Evaluation: The client is able to cope with performance of activities of daily living

independently.

Drugs: Phenothiazines: chlorpromazine (Thorazine); fluphenazine (Prolixin); mesoridazine

(Serentil); Perphenazine (Trifalon); prochlorperazine (Compazine); promazine (Sparine);

thioridazine (Mellaril); trifluoperazine (Stelazine); triflupromazine (Vesprin);

Non phenothiazine: clozapine (Clorazil); haloperidol ( haldol); loxapine (Loxitane);

molindone (Moban); olanzapine (Zyprexa); pimozide (Orap); quetiapine (Seroquel);

risperidone ( Risperdal); thiothixene (Navane)

S edation

unlight

T ardive dyskenesia

achycardia

remors

A nticholinergic

granulocytosis

ddiction

N euroleptic malignant syndrome

C ardiac arrhythmias (orthostatic hypotension)

E xtrapyramidal (Akathesia)

ndocrine (change in libido)

EPS? Remember PANAT: Psuedoparkinsonism, Akathisia, Neuroleptic Malignant

Syndrome (Fever, Encephalopathy, Vital signs unstable, Elevated enzymes esp CPK,

Rigidity of muscles), Acute Dystonic Reactions, Tardive Dyskinesia

MOOD STABILIZERS

given during the manic phase of manic-depressive phase

treatment of choice for the manic phase of the bipolar disorder and for long-

term prophylaxis of this bipolar disorder

level out the activity of neurotransmitter in the area of the brain that controls

emotions, thus preventing a decreased activity of nerve impulses, resulting in

depression or an increased activity of nerve impulses, resulting in MANIA.

Thought to maintain a constant Na concentration in the brain, regulating

impulses along the nerve cells as well as mood swings

The body does not metabolized Lithium; approximately 80% of a Lithium dose is

reabsorbed in the proximal convoluted tubules and excreted by the kidneys

Lithium Toxicity:

The usual range of therapeutic serum concentrations are:

For therapeutic mania: 1.0 to 1.5 mEq/L

For maintenance: 0.6 to 1.2 mEq/L

Symptoms include:

At serum levels of 1.5 to 2.0 mEq/L

o Blurred vision, ataxia, tinnitus, persistent nausea and vomiting, severe

diarrhea

At serum levels of 2.0 to 3.5 mEq/L

o Excessive output of diluted urine, increasing tremors, muscular

irritability, psychomotor retardation, mental confusion

At serum levels above 3.5 mEq/L

o Impaired consciousness, nystagmus, seizure, coma, oliguria, anuria,

arrhythmia, myocardial infarction, cardiovascular collapse

MOOD STABILIZING AGENTS

classification Generic name Trade name

antimanic Lithium carbonate

Lithium citrate

Eskalith,Lithane. Lithobid,

Eskalith CR

Cibalith-S

Anticonvulsants Clonazepam

Carbamazepine

Valproic acid

Gabapentin

Lamotrigine

Topiramate

Klonopin

Tegretol

Depakene, Depakote

Neurontin

Lamictal

Topamax

Page 5: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 5 of 15 St. Mary’s College

Calcium Channel Blockers verapamil Calan, isoptin

Give after meal to avoid gastric irritation

Cautions:

o Heart disease

o Sodium restricted diet

o Hypotension

o Epilepsy

o Parkinsonism

Lithium level: taken 2x/ week during initiation of therapy and before stability of

manic episode

o Serum levels taken q 12 hours after dose

Drugs that increase effect of lithium :

o Diuretics

o Anti inflammatory

Drugs that decrease effects of lithium

o Azetazolamide ( Diamox)

o Na bicarbonate

o Drugs with theophylline components

L evel - therapeutic (0.6 to 1.2 mEq/L)

I ncreased urination

T hirst increased

H eadache

H and tremor

I ncrease fluids

U nsteady

M onitor Salt - adequate intake

CNS Stimulants

Used to clinically tx attn deficit dos and narcolepsy.

Paradoxically, calm hyperkinetic children and keep them focus on one activity for

a longer period.

methylphenidate (Ritalin, Concerta): tx of attn deficit, other behavioral syndromes

assoc with hyperactivity, narcolepsy

dexmethylphenidate (Focalin): tx of attn deficit for 6 y/o +

dextroamphetamine (Dexedrine): adjunct therapy for exogenous obesity (short

term)

modafinil (Provigil): tx narcolepsy, improving wakefulness in people with obstructive

sleep apnea/hypopneas syndrome

MOA/Indication

Possibly increase the release of catecholamines from presynaptic neurons, leading

to increase in stimulation of the postsynaptic neurons.

Paradoxical effect of calming to attn deficit syndrome is believed to be r/t

increased stimulation of an immature RAS, which leads to the ability to be more

selective in response to incoming stimuli.

CI/Cautions

Presence of known allergy

Marked agitation, anxiety, tension (exacerbation)

Severe fatigue or glaucoma

Cardiac dses

Pregnancy and lactation

Caution: history of drug dependence and hypertension

AE

Nervousness

Insomia

Dizziness

HA

Blurred Vision

Difficulty with accommodation

Anorexia, nausea, weight loss

HTN, arrhythmias, angina

Nursing Implications

Ensure proper dx of behavioral syndromes and narcolepsy

Arrange to interrupt the drug periodically for behavioral syndromes

Arrange to dispense the least amount of drug

Adm before 6 pm

Monitor weight, CBC, ECG

Consult with school nurse and counselor for comprehensive care

Safety measures

Pt teaching (SOP)

ANTIEPILEPTIC AGENTS

Epilepsy

- most prevalent of the neurological disorders, is not a single disease, but a

collection of different syndromes

- all of these conditions are characterized by the same feature: sudden

discharge of excessive electrical energy from nerve cells located within the

brain which leads to a seizure

- in some cases, this release stimulates motor nerve resulting in convulsions, with

tonic-clonic muscle contractions that have potential to cause injury, tics and

spasm

Antiepileptics

- these agents are sometimes called as anticonvulsants, but because all types

of epilepsy do not involve convulsions, this term is generally not acceptable.

Classification of Seizures:

1. generalized seizure

begin in one area of the brain and rapidly spread throughout both

hemisphere of the brain

usually experience a loss of consciousness resulting from massive

electrical activity throughout the brain

a. tonic-clonic seizure (formerly known as grand mal seizure)

Page 6: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 6 of 15 St. Mary’s College

dramatic tonic-clonic muscle contraction, loss of consciousness,

and a recovery period characterized by confusion and

exhaustion

tonic- prolonged muscular contraction

clonic – series of alternating contractions and partial relaxation

of muscle

b. absence seizure (formerly known as petit mal seizure)

involved abrupt, brief ( 3-5 seconds) period of loss of

consciousness

occur commonly in children and frequently disappears at

puberty

c. myoclonic seizure

involve short, sporadic periods of muscle contractions that last

for several minutes. Relatively rare and are often secondary

seizure

d. febrile seizure

related to very high fever and usually involves convulsions

occur in children and are usually self-limiting and do not

reappear

e. status epilepticus

potentially the most dangerous of seizure conditions, is a state in

which seizures rapidly recur again and again

without recover of consciousness

2. partial seizure (also called focal seizure)

involve one area of the brain and do not spread throughout the

entire organ

a. simple partial seizure

occur in a single area of the brain and may involve a single

muscle movement or sensory alteration

b. complex partial seizure

involve complex sensory changes such as hallucinations, mental

distortion, changes in personality loss of consciousness and social

inhibitions

motor changes may include involuntary urination, chewing

motions, and diarrhea

onset usually occurs by late teens

DRUGS FOR TREATING TONIC-CLONIC SEIZURE

1. HYDANTOINS

Stabilize nerve membranes and limit the spread of excitability form the

initiating focus

Less sedating than many other epileptics, they may be the drug of choice

inpatients who are not willing to tolerate sedation and drowsiness

a. phenytoin (Dilantin)

for tonic-clonic seizure and status epilepticus as well as in the

prevention and treatment of seizure following neurosurgery

b. ethotoin (Peganone)

for tonic-clonic seizure and myoclonic seizure

c. fosphenytoin (Cerebyx)

For short-term control of status epilepticus and to prevent seizure

following neurosurgery

d. Mephenytoin (Mesantoin)

For tonic-clonic, myoclonic and partial seizure in patients who do not

respond to less toxic antiepileptic agents

Has been associated with severe hepatic toxicity, bone marrow

suppression and often unacceptable dermatologic reactions

2. BARBITURATES and BARBITURATE-LIKE DRUGS

a. Phenobarbital (Luminal)

Available in oral and parenteral forms

Used for emergency control of status epilepticus and acute seizure

associated with eclampsia and tetanus

b. Primidone ( Mysoline)

Alteranate choice in the treatment of tonic-clonic or partial seizure

Have longer half-life than Phenobarbital and is available only in oral

form

3. BENZODIAZEPINES

THERAPEUTIC ACTION:

- In generael, hydrantoins, barbiturate and benzodiazepine all stabilize nerve

membranes throughout the CNS to decrease excitability and hyperexcitability

to stimulation

CONTRAINDICAITON:

- pregnancy

- lactation

ADVERSE EFFECTS:

- depression, confusion, drowsiness, lethargy, fatigue, constipation, dry mouth,

anorexia, cardiac arrhythmia

- hydrantoins - severe liver toxicity, bone marrow suppression, gingival

hyperplasia, and potentially serious dermatologic reactions ( hirsutism,

coarsening of facial skin) which are all related to cellular toxicity

NURSING RESPONSIBILTIES:

1. discontinue drug at any sign if hyperexcitability reaction or liver dysfunction, or

severe skin rash to limit reaction and prevent potentially serious reactions

2. administer drug with food to alleviate GI irritation if GI upset is a problem

Page 7: Drugs Acting on the CNS and PNS 2011 Mps

Major P. Salipot, RN Page 7 of 15 St. Mary’s College

3. suggest the wearing or a carrying a medic-alert bracelet to alert emergency

workers and healthcare providers about the use of epileptic drug

DRUGS FOR TREATING ABSENCE (PETIT MAL) SEIZURE

1. SUCCINIMIDES

– drugs that modulate the inhibitory neurotransmitter GABA are most

frequently used

a. Ethosuximide ( Zarontin)

Drug of choice for treating absence seizure

Relatively few adverse effects compared to other antiepileptic drug

b. Methsuximide ( celontin)

Oral drug, used to treat absence seizures that are resistant to other

drugs

Associated with bone marrow suppression

c. Phensuximide ( Milontin)

Used for treatment of absence seizure that are resistant to other

agents

Therapeutic action:

- suppress the abnormal activity in the brain associated with absence seizure

Contraindication:

- allergy

- renal or hepatic disease

adverse effects:

- depression,. Drowsiness, fatigue, insomnia, headache, blurred vision

- nausea, vomiting, anorexia, weight loss, GI pain, constipation or diarrhea

- bone marrow suppression and dermatologic reactions such as pruritus,

urticaria, alopecia, Steven-Johnson syndrome may occur as a result of direct

chemical irritation of the skin and bone marrow

Nursing Responsibilities:

1. Administer the drug with food to alleviate GI irritation

2. Monitor CBS prior to and periodically during drug therapy to detect bone

marrow suppression early and provide appropriate intervention

3. discontinue the drug if skin rash, bone marrow suppression or unusual

depression or personality changes occur to prevent the development of

serious adverse effects

4. discontinue the drug slowly and never withdraw the drug quickly because

rapid withdrawal may precipitate absence seizure

OTHER DRUGS FOR TREATING ABSENCE SEIZURES

1. valproic acid ( Depakene)

Reduces abnormal electrical activity in the brain and may also

increase GABA activity at inhibitory receptors

Drug of choice in treating myoclonic seizures

2. zonisamide ( Zonegram)

Inhibits voltage-sensitive sodium and calcium channels, thus

stabilizing nerve cell membranes and modulating calcium-

dependent presynaptic release of excitatory neurotransmitters

Patients who take this drug should be very well hydrated; there is a

risk of renal calculi development

DRUGS FOR TREATING PARTIAL (Focal) SEIZURE

1. carbamazepine ( Tegetrol, atretol)

drug of choice for treating partial seizures

2. gabapentin ( Neurontin)

used as adjunct therapy in the treatment of focal seizure

3. Lamotrigine (Lamictal)

4. Tiagabaine (Gabritil)

5. Topiramate ( Topamax)

Adjunct therapy for partial seizure in adults

Therapeutic actions:

- stabilize nerve membranes by:

o directly by allowing sodium and calcium channels

o indirectly by increasing the activity of GABA

Contraindications:

- allergy

- bone marrow suppression

- severe hepatic dysfunction

ANTIPARKINSONIAN DRUGS

PARKINSON’S DISEASE

- a chronic neurologic disorder that affects the extrapyramidal motor tract(

which controls posture, balance and locomotion)

- three major features: rigidity, bradykinesia and tremors

- postural changes: chest and head thrust forward with knees and hips flexed

- with shuffling gait and absence of arm swing, with masked fasci. Involuntary

movement of head and neck and pill-rolling motion of the hands

- first described by James Parkinson in 1817

Pathophysiology

- caused by imbalance of the dopamine and acetylcholine

- marked by degeneration of the neurons in the substancia nigra and at the

basal ganglia

- there is an unexplained degeneration of the dopaminergic neurons

- drugs that are used to treat Parkinson’s Disease

1. anticholinergics

2. dopaminergics

3. dopamine agonist

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4. MAO-B inhibitor

5. COMT inhibitors- inhibits catechol-O-methyltranferase enzyme

ANTICHOLINERGICS

- drugs that oppose the effects of acetylcholine receptor sites in the substancia

nigra and corpus striatum

- has greater affinity for cholinergic receptors site sin the CNS

- block the action of acetylcholine in the CNS t help normalize acetylcholine-

dopamine imbalance

- reduce rigidity and to a lesser extent, tremor but have minimal effect on

bradykinesia

- are parasymphatolytics

- first used to treat Parkinson’s Disease before levodopa and dopamine agonist

were introduced

- peak in 1 – 4 hours

- cross the placenta

contraindications:

- allergy

- narrow angle glaucoma

- GI obstruction

- GU obstruction

- Prostatic hypertrophy

Side effects:

- dry mouth

- blurred vision

- constipation

- paralytic ileus

o rare but potentially very serious side effect. Monitor for abdominal

distension, absent bowel sounds, nausea, vomiting, epigastric pain.

Report immediately to the physician if these are present.

- urinary retention

- tachycardia, decreased sweating, elevated temperature

Nursing interventions:

1. arrange to decrease dosage.

2. arrange for a decrease in dosage in hot weather

3. give the drug with meal if GI upset occurs, before meals if dry mouth is a

problem

4. monitor bowel function

5. ensure that the patient voids before taking the drug if urinary retention is a

problem

6. provide thorough patient teaching

anticholinergic drugs:

1. benztropine mesylate ( Cogentin) – larger dose at bedtime

2. biperiden ( Akineton) - prototype

a. with prolonged use tolerance may occur

b. avoid taking with other CNS depressant and alocohol

c. start at 2mg/day in 1-4 divided doses

3. ethopropazine ( Parsidol)

4. Procyclidine (Kemadrin)

5. trihexyphenidyl ( Artane)

DOPAMINERGICS

- increases the amount of dopamine and enhances transmission of dopamine

- more effective than anticholinergics in treating Parkinson’s Disease

- directly stimulates the dopamine receptors

- after neurodegeneration has progressed to the extent that the nerves are

damaged or gone, these drugs are not effective

- levodopa is the first drug to be invented in 1961, it is a precursor to dopamine

that can cross blood-brain-barrier

- this increases mobility

- dopa decarboxylase converts levodopa to dopamine in the brain

Side effects:

- anxiety, nervousness, headache, malaise, fatigue, confusion, mental changes

- anorexia, nausea, vomiting, dysphagia, constipation

Drug-drug interactions:

1. with MAOI – increases the risk of hypertensive crisis

2. with Vit B6 and phenytoin may lead to decrease efficacy

1. levodopa (Dopar)

a. Prototype

b. Can cross the BBB

c. Immediate precursor of dopamine\loss of effectiveness after 3-5

years

d. Twitching of eyelids is an early sign of dug toxicity

e. Common side effects: fatigue, weakness, drowsiness, dizziness,

fainting, increased sweating darkening of the urine

f. If given with carbidopa ( SINEMET) more effective

i. Carbidopa inhibits the enzyme dopa decarboxylase

diminishing the metabolism of levodopa

3. amantadine (Symmetrel)

a. Antiviral drug that increases levels of dopamine

4. bromocriptine (Parlodel)

5. pergolide (Permax)

a. Inhibits prolactin secretion and rise in growth hormone

6. ropinirole (Requip)

Adjunct to levodopa therapy

1. entacapone (Comtan)

a. Increase the plasma concentration and duration of action of

levodopa

b. Inhibits catecholamine O-methyl transferase (COMT)

2. tolcapone (Tasmar)

a. Works in similar ways with carbidopa-levodopa

b. Blocks COMT

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c. Used in later stage of the disease when the effectiveness of

cerbidopa-levodopa decreases

3. selegiline (Carbex, Eldepryl)

a. Inhibits MAO

Muscle Relaxants

Muscle Spasm

Often result from injury to musculoskeletal system

Violent and painful involuntary muscle contraction

Flood of sensory stimuli – stimulate intense muscle contraction – cut off blood

supply – increase lactic acid – pain

Muscle Spasticity

Result of injury to CNS rather than at the periphery

Permanent

Result from increase in excitatory influence or decrease in CNS control

Hypertonia – excessive stimulation of opposing muscle groups which may

cause contractures

CENTRAL ACTING MUSCLE RELAXANTS

Interfere with the reflexes that causes muscle spasm

MOA/Indication

Unknown but believed to be involved in action in the upper or spinal

interneurons.

Relief of discomfort assoc with acute, painful musculoskeletal condition as an

adjunct to rest, physical therapy etc.

CI/Cautions

Presence of known allergy

Baclofen shld not be used to treat spasticity that contributes to locomotion or

increased function

Caution: history of epilepsy, cardiac dysfunction, any condition marked by

muscle weakness, hepatic/renal dysfunction, pregnancy/lactation

AE

CNS Depression: drowsiness, fatigue, weakness, confusion, HA, insomnia

GI: nausea, dry mouth, anorexia, constipation

Hypotension, arrhythmias

Urinary frequency, enuresis, urgency

Chlorzoxazone may discolor urine (orange-purple red)

Nursing Implications

Provide additional comfort measures (heat, rest, NSAIDS, positioning)

Discontinue if + hypersensitivity reactions or liver dysfunctions

Taper baclofen slowly over 1-2 weeks

If baclofen is adm by delivery pump: pt should understand the pump, reason

for frequent monitoring, how to adjust dose and program.

Monitor respiratory status

DIRECT-ACTING SKELETAL MUSCLE RELAXANTS

dantrolene (Dantrium) currently available in market in treating spasticity that

directly affect peripheral muscle contraction.

Used primarily for cerebral palsy, MS, muscular dystrophy, polio, tetanus,

quadriplegia, amyotrophic lateral sclerosis (ALS)

Not used for tx of muscle spasm assoc with musculoskeletal injury or rheumatic

dos

MOA/Indication

Dantrolene acts within skeletal muscle fibers, interfering with release of calcium

from muscle tubules.

Dantrolene is indicated for the control of spasticity resulting from upper motor

neuron disorders and prevention of malignant hyperthermia

Botulinum toxin type B (Myobloc) approved for the reduction of the severity of

abnormal head position and neck pain assoc with cervical dystonia.

Botulinum toxin type A (Botox Cosmetic) approved for cervical dystonia,

strabismus, blepharospasm and primary maxillary hyperhidrosis

CI/Cautions

Presence of known allergy

Spasticity that contributes to locomotion, upright position or increased function

Active hepatic dses

Lactation

Caution with the use of dantrolene: in women and all patients 35 y/o +, history

of liver dse or dysfunction, respi depression, cardiac dse, pregnancy

Caution for botulinum toxins: with peripheral neuropathic dse, neuromuscular

disorders, pregnancy and lactation

AE

CNS depression: drowsiness, fatigue, weakness, confusion, HA, insomnia, visual

disturbances

GI: irritation, diarrhea, constipation, abd cramps

Dantrolene: direct hepatocellular damage, urinary frequency, enuresis,

urgency, crystalline urine with pain or burning

Botulinum: anaphylactic reactions, HA, dizziness, muscle pain, paralysis,

redness and edema at injection site.

Nursing Implications

Discontinue at signs of liver dysfunction

Monitor for possible extravasation

Institute for supportive care for malignant hyperthermia (cooling blankets,

ventilation, anticonvulsants as needed)

Periodically discontinue (2-4 days) to monitor therapeutic effects

Discontinue if severe diarrhea

NARCOTICS

- Opioid, derived from opium

Opioid Receptors

- respond to naturally occuring peptins, endorphins, and enkephalin

- BRAINSTEM: control BP, pupil diameter, GI secretions, chemoreceptor trigger

zones (regulates nausea and vomiting, cough and respiration)

- SPINAL CORD AND THALAMUS: integrate and relate incoming info about pain

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- PERIPHERAL NERVE SITES: block release of neurotransmitters that are related to

pain and inflammation

4 types:

1. mu – analgesia, respiratory depression, feeling of euphoria, decrease GI activity, pupil

constriction, development of physical dependence

2. kappa – analgesia, pupil constriction, sedation

3. beta – react with enkephalins to modulate pain transmission

4. Sigma – pupil dilation, hallucination

Narcotic Agonist

- react with opioid receptor

Indication: analgesia, sedation, and sense of well-being, antitusssives

- severe acute and chronic pain, pre-op medication, analgesia during

anesthesia

- given IVTT, IM, SC

Contraindication: Allergy, pregnancy, labor, lactation

- diarrhea caused by poisons

- biliary surgery

Adverse reaction:

- apnea, cardiac arrest, shock

- orthostatic hypotension

- nausea and vomiting, constipation and biliary spasm

- lightheadedness, dizziness, anxiety, fear, hallucinations, pupil constriction,

impaired mental processes

- ureteral spasm, urinary retention, hesitancy, loss of libido

Nursing Interventions:

1. provide narcotic antagonist and equipment for assisted ventilation on standby

during IV administration.

2. Monitor site for irritation and extravasation

3. Monitor timing of analgesic doses

4. use extreme caution when injecting a narcotic into any body area that is

chilled or has poor perfusion

Drugs:

1. morphine ( Roxanol) – prototype

2. codeine – for mild to moderate pain; coughing

3. fentanyl ( Duragesic)

4. hydrocodone ( Hycodan) - relief of cough, for moderate pain

5. meperidine ( Demerol) – obstetrical anesthesia

6. opium ( Paregoric) – treatment of diarrhea, relief of moderate pain

7. oxycodone ( OxyContin)

Narcotic Agonist- Antagonist

- stimulates certain opioid receptor but block other such receptor

- less abuse potential than pure narcotic agonist

- like morphine, causes sedation, respiratory depression, constipation

1. Buprenorphine (Buprenex)

2. Nalbuphine (Nubain)

a. For moderate to severe pain, adjunct for general anesthesia

b. To relieve pain during labor and delivery

c. Should not be given to patients allergic to sulfites

3. Pentazocine ( Talwin)

a. Prototype

Narcotic Antagonist

- useful in blocking unwanted adverse effects associated with narcotics

- play a role in treatment of narcotic overdose

Adverse effect:

- Narcotic abstinence Syndrome characterized with nausea, vomiting,

sweating, tachycardia, hypertension, feelings of anxiety

Drugs:

1. Nalmefene ( Revex)

2. Naloxone ( narcan) – used to diagnose suspected narcotic overdose

3. Baltrexone (ReVita) – orally for alcohol or narcotic dependence

NON-OPIOID ANALGESIC

- includes acetaminophen, NSAID, cyclo-oxygenase 2 (COX-2)

ACETAMINOPHEN

- most widely used nonopioid analgesic

- action similar to salicylate

- blocks peripheral pain impulses by inhibition of prostaglandin synthesis

- lowers febrile body temperature

- for mild to moderate pain and fever

Contraindication:

- allergy

- glucose-6-phosphate dehydrogenase (G6PD) deficiency

Adverse effects:

- rash, nausea, vomiting

- can cause hepatotoxicity

- nephropathy

Acetylcysteine - recommended antidote for acetaminophen toxicity

- prevents the hepatotoxic metabolites of acetaminophen from forming

TRAMADOL HYDROCHLORIDE

- forms weak bond to sigma receptors

- inhibits re uptake of both norepinephrine and serotonin

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Major P. Salipot, RN Page 11 of 15 St. Mary’s College

- for moderate to severe pain

Adverse effects:

- drowsiness, dizziness, headache, nausea , constipation and respiratory

depression

Contraindication:

- allergy

- acute alcohol intoxication, centrally acting analgesic, opioids

- can cause seizure to patients taking MAOI, TCA and neuroleptics

ANTIMIGRAINE DRUGS

Migraine

- term used to describe several syndromes usually includes severe, throbbing

headaches on one side of the head. Affects personality, GI, CNS, and mood.

- types include: Common and Classic

- Common migraine is without aura, cause severe unilateral, pulsating pain

frequently accompanied by nausea, vomiting, sensitivity to light and sound.

- Classic migraine is usually preceded by aura or sensation involving sensory or

motor disturbances which usually occurs 10 mins before the pain begins

- has two drugs, ergot derivatives and triptans.

Ergot Derivatives

- cause constriction of the cranial blood vessels and decrease the pulsation of the

cranial arteries. Reduces hyperperfusion.

- because of many side-effects, has limited use in some patients.

- dihydroergotamine(Migranal) is IV or IM form or as nasal spray which provide rapid

relief.

- ergotamine (generic) prototype which is usually given SL. Cafergot is popular

(ergotamine+caffeine) because of rapid absorption at GI tract.

MOA/Indication

-block alpha-adrenergic and serotonin receptor sites to cause a constriction of

cranial blood vessels, a decrease in cranial artery pulsations, and a decrease in the

hyperperfusion of basilar artery bed.

-for prevention, abortion of migraine or vascular HA.

CI

-CAD, HTN Peripheral Vascular Dse

-impaired liver function

-Pregnancy and lactation

-Caution: pruritus (exacerbation), malnutrition (cause severe GI reactions)

AE

-numbness, tingling of extremities, muscle pain

-pulselessness, weakness, chest pain arrhythmia, localized edema, itching, MI may

occur

-GI upset, Nausea, vomiting, diarrhea

-Ergotism: syndrome which is manifested by nausea, vomiting, severe thirst,

hypoperfusion, chest pain, BP changes, confusion, drug dependency, drug withdrawal

D-D

-beta-blockers + ergotamine = risk for peripheral ischemia and inc. gangrene

Nsg Implementation

-avoid prolonged use

-use of atropine or phenothiazine if NV is severe

-provide comfort measures

-assess extremities carefully because of decrease in perfusion especially those with

decubitus ulcer or gangrene

-provide supportive measure to ensure patient safety if acute OD.

Triptans

-new drugs cc cause cranial vasoconstriction

-not assoc with all vascular and GI effects of ergot

-triptan of choice depends on personal experience

Sumatriptan (Imitrex) – used to tx migraine attacks; PO, SQ, nasal spray; effective

against cluster HA; CI for elderly

Naratripan (Amerge) - PO; tx of acute migraine; assoc with several birth defects; CI

for severe hepatic/renal dysfunction

Rizatriptan (Maxalt) – PO; tx of migraine with/out aura; have more angina effects so

CI for CAD

Zolmitriptan (Zomig) – PO; tx of migraine with/out aura in adults

Almotriptan (Axert) – tx of tx of migraine with/out aura

Frovatriptan (Frova) – has advantage of long-life; PO tx for acute migraine with/out

aura; prevents rebound HA

Eletriptan (Relpax) – PO; tx of migraine with/out aura

MOA/Indications

- triptans bind to SSR sites to cause vasoconstriction of cranial blood vessels,

relieving s/sx of migraine HAs.

-used as tx not prevention

-sumatriptan injection is also indicated for cluster HA

CI

-allergy

-pregnancy

-active CAD

-caution: elderly, lactation, renal/hepatic dysfunction

D-D Interaction

-triptans + ergot = prolonged vasoaction effect

-triptans + MAOI = increase vasoconstriction, must be avoided; more than two

weeks not receiving MAOI before use

AE

-numbness, tingling, burning sensation, feelings of coldness or strangeness, dizziness,

weakness, myalgia, vertigo

-dysphagia, abd discomfort

-BP alterations, tightness or pressure in the chest

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Nsg Implementation

- adm to relieve acute migraine

- arrange safety precautions for CNS or visual changes

- provide comfort measures such as environmental controls and stress reduction

- monitor: BP if with history of CAD; D/C if there is sign of angina or prolonged

HTN

- patient teaching

ANESTHETICS -drugs that can cause complete or partial loss of sensation

General anesthetics

CNS depressants used to achieve the ff goals:

Analgesia, unconsciousness and amnesia

- blocks body reflexes

- depresses the RAS and cortex

- lipid soluble

- metabolized in the liver

- cross the placenta

Contraindication:

1. status asthmaticus

2. absence of suitable veins for intravenous administration

Risk Factors:

- CNS Factors; Presence of underlying neurological disease

- Cardiovascular factors: CAD, hypotension

- Respiratory factor: COPD

- Renal and hepatic factor: conditions that interfere with the metabolism of and

excretion of anesthetics

Balanced Anesthesia

- use of combination drugs, each with specific effect, to achieve analgesia,

muscle relaxation, unconsciousness and amnesia, rather than the use of single

drug

- involves the ff:

1. Pre-op medication: which may include the use of anticholinergics that

decrease secretions to facilitate intubations and prevent bradycardia

associated with mental depression

2. sedative/hypnotic to relax patient, facilitate amnesia and decrease

sympathetic stimulation

3. Antiemetics to decrease nausea and vomiting associated with GI depression

4. Antihistamine to decrease the chance of allergic reaction and to help dry

secretion

5. Narcotics to aid analgesia and sedation

Stages of Anesthesia

Stage 1 (Analgesia)

- begins with consciousness and ends with loss of consciousness. Speech is

difficult, sensation of smell and pain are lost. Dreams and auditory and visual

hallucinations may occur. This stage may be called the induction stage.

Stage 2 (Excitement or delirium)

- produces loss of consciousness caused by depression of the cerebral cortex.

Confusion, excitement, or delirium occurs. Short induction time.

Stage 3 (Surgical)

- Surgical procedure is performed during this stage. There are 4 phases. The

surgery is usually performed on phase 2 and upper phase 3. As anesthesia

deepens, respirations become more shallow and respiratory rate increases.

Stage 4 (Medullary paralysis)

- toxic stage of anesthesia. Respirations are lost and circulatory collapse occurs.

Ventilatory assistance is necessary.

Induction – from beginning until stage 3; danger is in stage 2 because of systemic

stimulation

Maintenance – stage 3 until completion of surgery

Recovery – from time of D/C of anesthesia until patient regains consciousness

Types of GA

1. Barbiturate Anesthetics are IV drugs used to induce rapid anesthesia which is

then maintained by inhaled drugs.

b. Thiopental (Pentothal)

i. Most widely used of the IV anesthetics

ii. Rapid onset and ultra short recovery period

iii. Has no analgesic property

c. Methotexital ( Brevital)

i. Rapid onset and shorter recovery period

ii. Cannot come in contact with silicon

iii. Lacks analgesic property

iv. Causes respiratory depression and apnea

2. Nonbarbiturate Anesthetics given IV

a. Midazolam (Versed)

i. Prototype

ii. Rapid onset with peak effectiveness for 30 to 60 mins.

iii. Causes nausea and vomiting

b. Droperidol( Inapsime)

i. Use cautiously in patients with renal and hepatic failure

ii. Causes hypotension, chills, hallucination and drowsiness

during recovery period

c. Etomidate ( Amidate)

i. Sometimes used for sedation of patients on ventilators

ii. May experience myoclonic and tonic movements as well as

nausea and vomiting

iii. Not recommended for children younger than 10 years old

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d. Ketamine ( Ketalar)

i. Patient appears to be awake but is unconscious and

cannot feel pain

ii. Causes sympathetic stimulation

iii. Crosses the BBB

iv. Cause hallucinations, dreams and psychotic episode

e. Propofol (Diprivan)

i. Short-acting; rapid onset

ii. For short procedures

iii. Causes local burning sensation

iv. Cause bradycardia, hypotension, extreme: pulmonary

edema

3. Anesthetic gases

- enter the bronchi and alveoli

- very high affinity to fats

a. Nitrous oxide ( blue cylinder)

i. Prototype

ii. Potent analgesic

iii. Weakest pf the gas anesthetic and least toxic

b. cylopropane ( orange cylinder)

i. experience of pain, headache, nausea, vomiting, and

delirium during recovery phase

c. Ethylene ( red cylinder)

i. Leave patient with headache and unpleasant taste

4. Volatile Liquids

- inhaled anesthetic

- most are halogenated hydrocarbons

a. Halothane (Fluothane)

i. Prototype

ii. Vomiting, bradycardia and hypotension

iii. Increased risk for hepatic failure

iv. Recovery syndrome: fever, anorexia, nausea and vomiting

eventual hepatitis

b. Desflurane ( Suprane)

i. With respiratory reactions: cough, increased secretions,

laryngospasm

ii. Not recommended for pediatric patients

c. Enflurane ( Ethrane)

i. Associated with renal toxicity,cardiac arrhythmia and

respiratory depression

d. Isoflurane ( generic)

i. Associated with hypotension, hypercapnia, muscle soreness

and bad taste in the mouth

ii. Does not cause cardiac arrhythmia or respiratory irritation

e. Methoxyflurane ( Penthrane)

i. Can cause renal toxicity, respiratory depression and

hypotension

ii. Rarely used except during labor and delivery, because it

does not relax the uterus

f. Sevoflurane ( Ultane)

i. Newest

Nursing responsibilities:

1. must be administered by a trained personnel

2. have equipment standby to maintain airway and provide mechanical

ventilation

3. Monitor temperature for prompt detection and treatment of malignant

hyperthermia have dantrolene on standby.

4. Monitor VS ECG, cardiac output during administration

5. monitor patient until recovery phase is complete and patient is conscious and

able to move and communicate

6. provide comfort measures

7. provide thorough pre-op teachings

LOCAL ANESTHETICS

- cause loss of sensation in limited areas of the body

- very powerful nerve blockers

- are either esters and amides

- esters are broken down by plasma esterases

- amides are metabolized by the liver

- temporary interrupt the production and conduction of nerve impulses

- prevents sodium ions from entering the nerve they stop the nerve from

depolarizing

- used for: infiltration anesthesia, peripheral nerve block, spinal anesthesia , relief

of local pain

- Contraindication: allergy, heart block, shock, decrease plasma esterase

Modes of Administration:

1. Topical

2. Infiltration

a. Involves injecting the anesthesia directly into the tissues to be treated

3. Field Block

a. Injecting the anesthetic all around the area that will be affected by

the operation

b. Often used for tooth extraction

4. Nerve Block

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a. Injecting the anesthetic at some point along the nerve or nerves that

run to and from the region to which loss of pain sensation or muscle

paralysis is required.

b. Could be a peripheral nerve block (Blocks the sensory and motor

aspects of a particular nerve for relief of pain or diagnostic

procedure) or a central nerve block ( injected through a roots of the

nerves in the spinal cord)

c. Epidural anesthesia, the drug is injected into the space where the

nerve emerge from the spinal cord

d. Caudal block, injection into the sacral canal below the epidural area

5. Intravenous Regional Anesthesia

a. Carefully draining all the blood from the patient’s arm or leg, securing

a tourniquet to prevent anesthesia from entering the general

circulation, and then injecting the anesthesia into the vein of arm or

leg.

Adverse reaction:

- headache, restlessness, anxiety, dizziness

- tremors, blurred vision, backache

- nausea and vomiting, peripheral vasodilation, myocardial depression

- arrhythmia, BP changes

Nursing Interventions:

1. Have equipment standby.

2. Ensure drugs for hypotension, cardiac arrest and CNS alteration

3. Ensure patient receiving spinal anesthesia are well hydrated and remain lying

down for up to 12 hours.

4. Establish safety precaution

5. Provide comfort measure

6. Provide thorough patient teaching

Drugs:

Esters: 1. benzocaine (Dermoplast)

2. Procaine ( Novocain)

Amides: 1. bupivacaine ( Marcaine)

2. Lidocaine ( Xylocaine)

3. Mepivacaine ( Isocaine)

Neuromuscular Junction Blocking Agents

- divided into 2: nondepolarizing and depolarizing

- Nondepolarizing acts as antagonist to Ach while nondepolarizing acts as

agonist for Ach

- Cause paralysis during surgical procedure or facilitation of mechanical

ventilation

Nondepolarizing NMJ Blockers

-curare: first discovered NNMJB which is a poison

-destroyed in cooking

-clinical usage: tubocurarine

-occupies muscular cholinergic receptor sites which prevents Ach from reacting

with the receptor

-effect is more long-lasting

- used when muscle paralysis is required.

Depolarizing NMJ Blockers: Succinylcholine

-attaches to the Ach receptor site of muscle causing stimulation of the muscle and

muscle contraction and can’t be broken down instantly causing prolonged contraction

-hydrophilic that’s why not readily cross BBB

-rapid onset and short duration bec it is broken down by cholinesterase

- indicated for:

a. to serve as adjunct therapy for GA during surgery when reflex when reflex

muscle movement could interfere with procedure or delivery of gas

anesthetics

b. to facilitate mechanical intubation by preventing resistance to passing ET

and in instances in which patient fight or resist the respirator.

c. to facilitate ECT therapy when intense skeletal muscle contractions as a

result of electric shock could cause the patient broken bones or other injuries.

CI

-know allergy

-myasthenia gravis

-hepatic/renal dses

-pregnancy/lactation

-caution:

History of malignant hyperthermia

Pulmonary/CV dysfunction

Altered Fluids and Electrolyte imbalances

Respiratory condition

Fractures

Narrow-angle glaucoma

SCI, paraplegia

-extreme caution:

Dse conditions causing low plasma cholinesterase levels such as:

Cirrhosis, metabolic dos, carcinoma, thyroid toxicosis, collagen

diseases, burns, DHN, hyperpyrexia, exposure to neurotoxic

insecticides

AE

-assoc with muscle paralysis:

Apnea

Histamine release causes wheezing and bronchospasm

Hypotension, cardiac arrhythmias

Constipation, vomiting, regurgitation, aspiration

Decubitus ulcer

Hyperkalemia

Muscle pain (aspirin after procedure)

Malignant hyperthermia (massive muscle contraction, sharp elevated temp,

severe acidosis, death); tx with dantrolene

D-D Interaction

-DNMJB + halothane = increased effect

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Major P. Salipot, RN Page 15 of 15 St. Mary’s College

-DNMJB + aminoglycoside antibiotics = increased neuromuscular blockage

-DNMJB + calcium channel blockers = increased effect

-DNMJB + cholinesterase inhibitors = decreased effect

-DNMJB + xanthines = reversal effect

Nsg Implementation

-adm by trained personnel

-supplies and equipments, peripheral stimulator, cholinesterase inhibitors are on

standby

-do not mix with alkaline sol’n such as barbi

-test pt response and recovery periodically

-monitor temp

-maintain dantrolene for malignant hyperthermia

-adm small dose of NNMJB to decrease adverse effect of succinylcholine

-provide comfort measures

-monitor VS

-drug teaching


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