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Four process of pharmacokinetics: Drugs in liquid form are more rapidly absorbed than
solid drugs
1. Absorption
Takes place in the mucosal lining Pain, stress, and foods that are solid, hot or high in fat
makes drugs remain in the stomach longer because
Tablets are example- not 100% drug it is with
these causes a slow gastric emptying time.
excipient. This is for the drug to take a particular
size and shape and to enhance drug dissolution. Poor circulation to stomach hampers absorption, du to
A. Disintegration- it has to be broken down into shock or diseases.
small particles
B. Dissolution- a process where broken down Drugs given rectally are absorbed slower than drugs
particles combine with liquid administered by mouth.
C. Absorption- happens in the mucosal lining of
Suppository-based drug affects the absorption.
the small intestine. Movement of drug into the
blood stream after administration. Drugs that are administered intramuscularly are
Drugs are both disintegrated and dissolve faster absorbed faster in muscles that have increase blood
in acidic fluids (ph 1-2) than in alkaline fluids flow like deltoid than those that do not.
The very young and older adults have less
gastric activity- drug absorption Is slower Subcutaneous have decreased blood flow compared
Enteric coated drug are meant to be absorbed with muscle, slower absorption.
in the small intestine.
Absorption of Oral Drugs
NURSING IMPLICAITON-do NOT crush the
medication. It will not be absorbed in the GI tract > intestinal lumen > liver (via the portal vein)
intended site.
Drugs are absorbed in the mucosal lining of the First pass metabolism or first-pass effect
small intestine through:
- in the liver some drugs are metabolised in
a. Passive transport (diffusion and facilitated
an inductive form and are excreted, thus,
diffusion)
reducing the drug available to exert a
- no energy needed
pharmacologic effect.
diffusion drug moves across the cell membrane
- Lidocaine and nitroglyceride should not be
from higher to lower concentration
given orally because it will be inactivated by
facilitated diffusion
the liver.
b. Active transport (needs enzyme or protein)
- energy required Bioavailability
c. Pinocytosis
- Refers to the percentage of adminestered
drug available for activity. Two drugs are administered together they
- For orally administered drug bioavailability compete for protein bounding sites in which
is affected by absorption and first-pass drug accumulation will occur and drug toxicity
metabolism may result.
- Oral dug less than 100%
- Intravenous is 100% Low plasma protein level, decreases the number of
- FACTORS that alter BioA: available binding sites and can lead in an increase of
amount of free drug available resulting in drug accu and
1. Drug form
2. Route of administration toxicity.
3. Gastric mucosa and motility Drugs taken during pregnancy:
4. Administration with food and other
drugs 1st trimester- spontaneous abortion
5. Changes in liver metabolism
2nd trimester- spontaneous abortion, teratogensis, or
> decreased of liver meta increased of
other subtler effects
bioavailability
2. Distribution 3rd trimester- fetal growth and development
-refers to the movement of drug from the
circulation to the body tissues 3. Metabolism or biotransformation
- drug affinity to protein binding - Is the process in which the body chemically
> highly protein-bound drugs changes drug into a form that can be
-90% bound to protein excreted
>weakly protein-bound drugs - Liver is a primary site of metabolism
-less than 10% bound to protein - Cytochrome P450 system
TAKE NOTE - liver enzyme
The portion of the drug that is bounded to the - metabolized lipid-soluble drugs to water-
protein is inactive because it is not available to soluble drug for renal excretion
interact with tissue receptor, thus, no
Factors that alter drug metabolism
pharmacologic effect.
1. Liver disease (cirrhosis and hepatitis)- inhibits
The portion that remains unbound is free active drug-metabolizing enzymes in the liver
drugs. Free drugs can exit blood vessel and
reach their site of action, thus, with Decreased drug metabolism > excess drug accumulation
pharmacologic response. > toxicity
1. Lower albumin levels (hypoalbuminemia) - Is the time it takes for the amount of drugs
With liver and kidney disease into the body to be reduced by half.
Malnourished - Amount of administered, amount of drug
Older adults (mas naa hypoalbuminemia) remaining in the body from the previous
2. Lower plasma protein level dose, and elimination can affect half- life.
- Example: 500 mg paracetamol was
Patients with kidney or liver disease may have administered at 0800H. 4 hours half-life.
significantly lower albumin levels. 0800H- 500 mg
1200H- 250 mg
NURSING IMPLICATION- check patient’s protein
0400H- 125 mg
and albumin level when administering drugs.
ss
Loading Dose
- The administration of a large initial dose
used to ensure quick therapeutic response,
for a lower maintenance dose. Drugs with
LONG half-lives
- Example: Phenytoin, half-life 22 hours
4. Elimination or excretion
- Main route is through the kidneys
- Drugs are also excreted through bile, lungs,
saliva, sweat and breast milk.
- Urine PH influences drug excretion
Acidic urine- elimination of weak based drug
Alkaline urine- elimination of weak acidic based
drug
> prerenal
(profusion of blood towards the kidney),
(dehydration and haemorrhage)
-intrarenal
(within the kidneys/ formation of urine)
(glomerulonephritis, chronic kidney dis), and
-postrenal
(outflow of urine form the kidneys)
(prostatic hypertrophy, stones, and urogenic
bladder) affects excretion.
NURSING IMPLICATION:
Planning
Implementation
patient teaching
- general, side effects, self-administered,
diet, cultural considerations
other interventions
Evaluation
- documentation
- Antiseptic, antinflammatory,
antipasmodial, anti-cough, anti-spasmodic,
10 MEDICINAL IN THE PHILIPPINES antioxidant hepatoprotective, antidiabetic,
1. Akapulko antigenotoxic in folklore med.
- Tinea infections, insect bites, ringowrms,
eczema, scabies and itchiness.
5. Lagundi
- Used to reat cough, colds, fever
- Relief for asthma & pharyngitis,
rheumatism, dyspepsia, boils, and diarrhea
2. Ampalaya
- Treatment of diabetes (mellitus),
haemorrhoids, coughs, burns, and calds,
neing studied for anti-cancer
6. Niyog-niyogan
- Intestinal parasite
3. Bawang or garlic
- Used to treat infection
- Antibacterial, antiinflamatory, anticancer,
and anti-hypertensive
- Reduce cholesterol level
7. Sambong
- Treat kidney stones, wounds, cuts,
rheumatism, anti-diarrhea, anti spasm,
colds and coughs and hypertension
4. Bayabas or Guava
10 HERBAL PLANTS IN THE PHILIPPINES
1. Astralagus
- used as an adjunct to boost immune
system
8. Tsaang gubat
- Treat skin allergies including eczema,
scabies, and itchiness wounds in childbirth.
2. Chamomile
-for sleeplessness, anxiety, stomach and
intestinal ailments
9. Ulasimang bato
-athritis
3. Cinnamon
- Bronchitis, GI problems, anorexia, and
diabetes
4. Echinacea
- For cold, flue, and infection.
8. Ginseng
- Used to boost immune system. Increase a
5. Garlic
person’s sense of well-being and increase
-used to lower cholesterol, blood pressure, and
stamina
reduce heart disease.
9. Hawthorn
6. Ginger - Heart disease
- Nausea, motion sickness and diarrhea
-
10. Licorice root
7. Gingko - Stomach ulcer, bronchitis, sore throat, and
-asthma, bronchitis, fatigue, and tinnitus viral hepatitis.
11. Mil thistle 14. Turmeric
- Cirrhosis, chronic hepatitis, and gall bladder -heartburn, stomach ulcer, gallstone,
disorder. inflammation and caer.
15. Valerian
- Insomnia, anxiety, headache, depression,
irregular heartbeat, and tremors.
12. Peppermint
- Nausea, indigestion, irritable bowel
syndrome, cold, headaches, muscle and
nerve pain.
MENINGES
- outer layer - dura mater
- middle layer - arachnoid mater
- inner layer - pia mater
SUBARACHNOID SPACE
- space between the arachnoid and pia mater is filled with cerebrospinal fluid
BRAIN
- located @ the cranium of skull
- has 3 main parts (cerebrum, cerebellum, and medulla oblongata)
CEREBRUM
- largest part of brain
- divided into Left and Right hemispheres
- concerned with learning, memory, interpretation, and personality
CEREBELLUM
- located @ the back of brain below cerebrum
- controls balance, movement, and coordination
BRAIN STEM
- located beneath cerebrum, in front of cerebellum
- connects brain with spinal cord
- composed of Midbrain, Pons, and Medulla oblongata
- controls a number of autonomic functions including respiration and blood pressure
SPINAL CORD
- extends from Medulla oblongata and down the back
- protected by the vertebral column
- a hollow tube containing cerebrospinal fluid
- 31 pairs of spinal nerves arise from spinal cord, these nerves transmit info from body organs to
brain, and from brain to organs
NURSING CARE OF CLIENTS WITH CNS AND PSYCHOTHERAPEUTIC DRUGS
(Care of clients with Drugs affecting the Central and Peripheral System)
PART 1
Nervous System
-Composed of all nerve tissue:
▪ Brain
▪ Spinal cord
▪ Nerves
▪ Ganglia
-receives stimuli and transmits information to nerve centers for an appropriate
response
2 types: CNS and PNS
Group of Medications
STIMULANTS
Indications:
Attention-Deficit/Hyperactivity Disorder
- dysregulation of the transmitter’s serotonin, norepinephrine and dopamine
- may occur before 7yrs of age and may continue through teenage years
Characteristics: inattentiveness, inability to concentrate, restlessness, hyperactivity,
inability to complete tasks and impulsivity
Narcolepsy
- characterized by falling asleep during normal waking activities
*Sleep paralysis usually accompanies narcolepsy and affects the voluntary muscles
Respiratory Distress
- refers to a condition in which the person is having trouble breathing which often
show signs that they are not getting enough O2
- this condition prevents the body organs from getting the O2 they need to fxn
2. Amphetamine-like Drugs
- used for ADHD or narcolepsy
Examples: Methylphenidate HCl
Modafinil
Dexmethylphenidate HCl
Armodafinil
- more effective in treating ADHD than Amphetamines
- classified as Controlled Substance Schedule (CSS) II drug.
3. Anorexiants
- suppress appetite
Examples: Benzphetamine
Diethylpropion HCl
Phentermine HCl
Phentermine topiramate
Phendimetrazine
Liraglutide
Naltrexone HCl
Bupropion HCl
(cause a similar effect on the hypothalamic and limbic regions of the brain to
suppress appetite. These medications do not have serious side effects associated w/
amphetamines)
*Long term use of this medication results to nervousness, restlessness, irritability,
insomnia, palpitation and hypertension
4. Analeptics
- stimulate respiration
Examples: Caffeine citrate 2 main drugs
Theophylline
Doxapram
*Large dose of caffeine will stimulate respiration
*Theophyllinen is mostly used to relax the bronchioles and used to increase respiration
in newborn
DEPRESSANTS
*Drugs that are CNS depressants cause varying degree of depression or reduction in the
functional activity within the CNS
*The degree of depression depends primarily on the drug and the amount of drug taken
Classifications:
Sedative-hypnotics
Analgesics (opioid/nonopioid)
General Anesthetics
Anticonvulsants
Antidepressant
Antipsychotic
1. Sedative-hypnotics
Examples:
Secobarbital sodium
Butabarbital sodium
Phenobarbital
Pentobarbital
Mephobarbital
*Hypnotic effect is a form of natural sleep
Hypnotic drug therapy should be short term to prevent drug dependence and drug
tolerance
*Interrupting hypnotic therapy can decrease drug tolerance but abruptly discontinuing a
high dose of hypnotic taken over a long perion can cause withdrawal symptoms
General rule:
The lowest dose should be taken to achieve sleep
Patients w/ severe respiratory disorders should avoid hypnotics which could
cause an increase in respiratory depression
Hypnotics are contraindicated during pregnancy
Ramelteon is the only major sedative-hypnotic approved for long term use. This
drug may be used to treat chronic insomnia
Types of Sedative-hypnotics:
• Nonbenzodiazepines
• Melatonin Agonist
PART 2
ANASTHETICS
- Substances that induces insensitivity to pain
Classified as: General and Local
*Monitor vital signs following general and local anesthesia because hypotension and
respiratory depression may result
Balanced Anesthesia
- A combination of drugs each with a specific effect frequently used in general
anesthesia
- Used to minimize cardiovascular problems, decreases the amount of general
anesthetic used
- Reduces possible post-anesthesia nausea and vomiting
- Minimizes the disturbance of organ fxn and decreases pain
Stages of Anesthesia:
1. Analgesia –
• begins with consciousness and ends with loss of consciousness
• speech is difficult
• sensation of smell and pain are lost
• dreams, auditory and visual hallucinations may occur
• “induction stage”
2. Excitement/Delirium
• Produces a loss of consciousness caused by depression of the
cerebral cortex
• Confusion, excitement or delirium occur
• Induction time is short
3. Surgical
• Surgical procedure is performed during this stage
*As anesthesia deepens, respirations become shallower and the respiratory rate is
increased
4. Medullary Paralysis
• “toxic stage of anesthesia” in which respirations are lost and
circulatory collapse occurs, ventilator assistance is necessary
*The patient’s response to anesthesia may differ according to variables related to health
status of the individual. These variables include: Age, A current health disorder,
Pregnancy, History of heavy smoking and Frequent use of Alcohol and Drugs
➢ Local Infiltration – used to block the pain at the site where the drug is
administered by preventing the conduction of nerve impulses
• Dental procedures
• Suturing skin lacerations
• Short term surgery at a localized area
• Block nerve impulses
• Below the insertion of spinal anesthetic
• Diagnostic procedures (such as lumbar puncture and
thoracentesis)
➢ Spinal route
Requires that a local anesthetic be injected into the subarachnoid space:
- Below the first lumbar space (L1) in adults
- The 3rd lumbar space in children (L3)
*A Postdural-puncture headache might result following a spinal anesthesia possibly
because of a decrease of cerebrospinal fluid pressure caused by the leak of fluid at the
needle insertion point.
Nursing Intervention: Increased fluid intake usually decreases the likelihood of leaking
spinal fluid. Encourage the patient to remain flat
• Spinal Block – into the subarachnoid space
• Epidural Block – in the epidural space
• Caudal Block – through the sacral hiatus
• Saddle Block – lower end of spinal column
*Blood pressure should be monitored during administration of these types of anesthesia
➢ Intravenous – may be used for general anesthesia or for the induction stage
of anesthesia
TIVA – Total Intravenous Anesthesia
ANTISEIZURE DRUG
- Used for epileptic seizures, also called as “anticonvulsants/anti-epileptic” drugs
- This medication acts by stabilizing nerve cell membrane and suppress abnormal
electrical impulses in the cerebral cortex
- Prevents seizures but do not eliminate the cause or provide a cure
• Suppresses sodium/calcium influx
• Increases the action of Gamma Aminobutyric Acid (GABA)
1. Hydantoins – act by inhibiting sodium influx, stabilizing cell membranes, reduces
repetitive neuronal firing and limit seizure ; may cause birth defects or congenital
anomalies
• Phenytoin – for the treatment of tonic-clonic seizure, partial
seizures and status epilepticus ; has narrow therapeutic range:
10-20 mcg/mL
(serum level should be monitored)
*Onset of action of PO route is 30mins-2hrs
*Peak of 1.5-6hrs a steady state of serum concentration at 7-10days
*Duration of action dependent on the half-life which could be up to
45hrs
*IV line should always be flushed w/ saline sol’n before and after use to reduce venous
irritation
*This medicatiom may be diluted in saline sol’n and dextrose should be avoided because
of drug precipitation and must not be administered through IM route
*If medication will exceed 20 mcg/mL→ toxic effects
*If medication is below 10 mcg/mL →will not render a desired effect
2. Barbiturates
• Phenobarbital – used to treat tonic-clonic, partial and myoclonic
seizures as well as status epileptic
– therapeutic range: 20-40 mcg/mL
3. Succinimides
• Ethosuximide – acts by decreasing calcium influx through the t-
type calcium channel
- used to treat absence seizure
- Therapeutic range: 40-100 mcg/mL
4. Benzodiazepines
Have antiseizure effects: Clonzepam, Clorazepate dipotassium, Lorazepam,
Diazepam
5. Iminostilbenes
• Carbamazepine – used for psychiatric disorders, trigeminal
neuralgia and alcohol withdrawal. - Therapeutic range: 4-12
mcg/mL
6. Valproate – for tonic-clonic absence and mixed type of seizure
- Therapeutic serum range: 50-100mcg/mL
*Liver enzymes should be monitored
*Hepatoxicity is one of the adverse rxn
PART 3
Parkinson’s Disease
- Caused by an imbalance of the neurotransmitters (DA and ACh) and it is marked by
the degeneration of neurons of the extrapyramidal motor tract in the substantia
nigra of the midbrain
- Chronic, progressive neurologic disorder that affects the extrapyramidal motor tract
which controls posture, balance, locomotion.
- Most common form of Parkinsonism – a syndrome, a recombination of similar
symptoms because of its major features like:
Major Features:
❖ Rigidity (abnormal increased muscle tone) –increases with movement
*Postural changes caused by rigidity and bradykinesia include: chest and head
thrust forward with the knees and hips flexed, shuffling gait and the absence of arm
swing
*Other characteristic symptoms include: masked facies - no facial expressions,
involuntary tremors of the head and the neck, and peel rolling motions of the hands
❖ Bradykinesia (slow movement)
❖ Gait disturbances
❖ Tremors – more prevalent at rest
Neurotransmitters:
Dopamine (DA)
- an inhibitory neurotransmitter
- released from/ produced by : dopaminergic neurons
- maintains and controls Acetylcholine and inhibits its excitatory response
- plays a part in controlling the movements a person makes and their emotional
responses/ TAKE NOTE: Dopamine has a control in the locomotion or movement of a
person
*The right balance of DA is vital for both physical and mental well-being, vital brain
functions that affect mood, sleep, memory, learning, concentration and motor control
are influenced by the levels of DA in a person’s body
Acetylcholine (ACh)
- an excitatory neurotransmitter
- essential for muscles to contract, without it muscles cannot contract
- released from cholinergic neurons
- achieved neurotransmitter of the parasympathetic nervous system that contracts
smooth muscles, dilates blood vessels, increases bodily secretions, and slows heart
rate
*These 2 neurotransmitters (DA and Ach) need to work hand in hand in order to create
a balance ; if one is elevated, there will be a chaos in the body system
1. Anticholinergics
2. Dopamine replacements (dopaminergics)
3. Dopamine Agonists
4. Monoamine Oxidase B (MAO-B) Inhibitors
5. Catechol-O-methyltransferase (COMT) Inhibitors
1.) Anticholinergics
- Can inhibit the release of ACh
*one of the problems in Parkinson’s Disease is the increased number of ACh
Examples:
Benztropine mesylate
Trihexyphenidyl Hydrochloride
Side Effects:
- Dry mouth
- Dry secretions
- Urinary retention
- Constipation
- Blurred Vision
- Increase in heart rate
Assessment:
▪ Obtain a health history (report any history of glaucoma, GI dysfunction, urinary
retention, angina, or myasthenia gravis)
▪ Obtain a drug history (report any probable drug-to-drug interaction such as with
phenothiazine tricyclic antidepressants and antihistamine – can increase effect of
dry hexafenidyl hydrochloride)
▪ Assess baseline vital signs for future comparison
▪ Assess pt’s knowledge regarding the medication regimen
▪ Assess usual urinary output
Nursing Diagnosis:
▪ Impaired mobility related to muscle rigidity
▪ Impaired urinary elimination related to urinary retention
Planning:
▪ Pt will have decreased involuntary symptoms caused by the disease or drug
induced parkinsonism
Nursing interventions:
▪ monitor vital signs urine output and bowel sounds (increased pulse rate urinary
retention and constipation are side effects of anticholinergics)
▪ observe for involuntary movements
Patient teachings:
▪ avoidance of alcohol cigarette caffeine and aspirin (to decrease gastric acidity)
▪ encourage the patient to relieve dry mouth with hard candy ice chips or sugarless
chewing gum (because anticholinergics can decrease salivation)
▪ suggest that patient uses sunglasses in direct sunlight (because of possible
photophobia)
▪ advise patients to void before taking the drug (to minimize urinary retention)
▪ counsel patients who take an anticholinergic for control of symptoms of
parkinson's disease to have routine eye examination (because anti-cholinergics are
contraindicated in patients with glaucoma)
▪ encourage patients to ingest foods high in fiber and to increase fluid intake (to
prevent constipation)
Evaluation:
▪ evaluate the outcomes of the therapy
▪ evaluate the patient's response to trihexyfenidyl or the benztrophine vesilate to
determine whether parkinson's disease symptoms are controlled
2.) Dopaminergics
Examples of Dopaminergics
✓ Carbidopa and Levodopa
✓ Levodopa
❖ the first dopaminergic drug - introduced in 1961 but is no longer available
in the United States
❖ When it was introduced, levodopa was effective in diminishing symptoms
and increasing mobility (this is because the blood brain barrier admits
levodopa but not dopamine)
❖ NOTE: the enzyme dopa decarboxylase - converts levodopa to dopamine in
the brain but this enzyme is also found in the PNS and 99% of levodopa is
converted into dopamine before it reaches the brain
❖ THEREFORE only about 1% of levodopa taken in is converted to dopamine
once it reaches the brain
❖ large doses are needed to achieve a pharmacologic response
❖ these high doses could cause many side effects
o nausea
o vomiting
o Dyskinesia
o orthostatic hypotension
o cardiac dysrhythmia and
o psychosis
❖ the fact that so much levodopa is metabolized before it reaches the brain
an alternative drug carbidopa was developed
✓ Carbidopa
❖ inhibit the enzyme dopa decarboxylase in the PNS
❖ more levodopa reaches the brain
❖ Carbidopa is combined with Levodopa in a ratio of one part carbidopa to 10
parts levodopa (1:10)
Advantages of combining levodopa with carbidopa:
➢ more dopamine reaches the basal ganglia
➢ smaller doses of levodopa are required to achieve the desired effect
Disadvantages of the carbidopa levodopa combination:
➢ more available levodopa = more side effects may occur
➢ the peripheral side effects of levodopa are not as prevalent however
angioedema palpitations and orthostatic hypotension may occur
➢ GI disturbances are also very common in patients who are taking carbidopa
levodopa (because dopamine stimulates the chemoreceptor trigger zone or
the ctc in the medulla which then stimulates the vomiting center)
*taking the drug with food can decrease nausea and vomiting but foods
lose the absorption rate of the medication
Assessment:
▪ Assess vital signs for future comparison
▪ Assess patients for signs symptoms of PD (including stoop forward posture,
shuffling gait, mask facies and resting tremors)
▪ Assess patient history (that includes glaucoma, heart disease, peptic ulcer, kidney
or liver disease and psychosis because severe cardiac renal or psychiatric health
problems are contraindications for levodopa)
▪ Assess drug history (especially if the patient is taking monoamine oxidase
inhibitor or MAO-I)
NOTE: if a MAO-I and carbidopa levodopa are taken concurrently it may result to
hypertensive crisis - a severe increase in the blood pressure that may lead to
stroke
Nursing diagnosis:
▪ Impaired physical mobility related to dizziness
▪ Risk for fall
*do not forget that our main objective of administering dopaminergic or carbidopa
levodopa to a patient is to decrease the signs and symptoms of parkinson's
disease within one to four weeks of drug therapy
Nursing interventions:
▪ Monitoring vital signs (electrocardiogram or ECG because orthostatic hypotension
may occur during early use of carbidopa-levodopa)
▪ Instruct patients to rise slowly to avoid faintness
▪ Observe for weakness, dizziness or syncope (which are symptoms of orthostatic
hypotension)
▪ Administer carbidopa-levodopa with low protein foods (because high protein diets
interfere with drug transport to the CNS)
▪ Observe for symptoms of Parkinson’s dse.
▪ Urge the patient not to abruptly discontinue the medication (because rebound
Parkinson's disease may occur)
▪ Advise patients to avoid chewing or crushing the extended release tablets
▪ Encourage patients to report side effects and symptoms of dyskinesia
▪ Explain that it may take weeks or months before symptoms are controlled
▪ Suggest to patients that taking carbidopa-levodopa with food may decrease GI
upset (but food will slow the rate of drug absorption)
Evaluation:
▪ Do not forget to evaluate the effectiveness of drug therapy
▪ Determine if there is an absence of side effect
▪ Determine if the patient and family have increased knowledge of the drug
regimen
3.)Dopamine Agonist
- also called dopaminergics
- used to stimulate dopamine receptors
Examples:
▪ Amantadine
▪ Bromocriptine
▪ Pramipexole
▪ Ropinirole Hydrochloride
1.) Amantadine
-an antiviral drug that affects the dopamine receptors
-can be taken alone or in combination with carbidopa levodopa or anticholinergic
-produces improvement in symptoms but drug tolerance develops
-patients who cannot tolerate carbidopa-levodopa are given with this medication
Side effects:
▪ nausea
▪ orthostatic hypotension
▪ palpitation
▪ chest pain
▪ lower extremity edema
▪ nightmares
▪ delusion and confusion
Assessment, Nursing Diagnosis and Planning:
▪ for a patient who is taking anticholinergic and carbidopa-levodopa are just the same
for a patient who's taking amantadine and bromocriptine
Patient teachings:
▪ Urge patient taking amanti. to report any signs of skin lesions, seizures, or
depression (a history of these health problems should have been previously
reported to a health care provider)
▪ Advise patients taking bromo. to report symptoms of lightheadedness when
changing positions (because this is a symptom of orthostatic hypotension)
▪ Warn patients to avoid alcohol when taking bromocriptine
▪ Teach patients to check their heart rate and report heart rates that changes or
there will be irregularity noted
▪ Counsel patients not to abruptly stop the medication or the drug without first
notifying a healthcare provider
4.)Monoamine oxidase-B inhibitor (MAO-B inhibitor)
Examples:
▪ Selegiline hydrochloride
▪ Rasagline
-inhibit MAO-B -> prolongs the action of levodopa
Note: the enzyme MAO-B causes catabolism or breakdown of dopamine
➢ Selegiline HCl
- can delay the use of carbidopa-levodopa by one year
*Take note that in parkinson's disease dopamine is actually depleted already
because the production is not enough considering that there is degeneration
of the dopaminergic neurons and so the produced dopamine has to be
preserved but unfortunately the enzyme called MAO-B or monoamine oxidase
b causes catabolism of the dopamine thereby these enzymes will further
deplete or decrease the number of dopamine so Selegiline will inhibit the
MAO-B thus the dopamine will be preserved or the dopamine will not be
catabolized
*Monoamine oxidase A or MAO-A is an enzyme that promotes the metabolism of
tyramine in the GI tract if tyramine is not metabolized it can cause
hypertensive crisis - a severe increase in the blood pressure that may lead to
stroke
TAKE NOTE: Selegiline inhibits both MAO-B and MAO-A, so be wary!
Patient teaching:
▪ Urging him or her to avoid foods high in tyramine such as aged cheese,
red wine, cream, yogurt, chocolate, bananas, raisins, etc. to prevent
hypertensive crisis
▪ Inform the patient that severe drug interaction may occur between
Selegiline and various tricyclic antidepressants or TCAs and Selective
Serotonin Reuptake Inhibitors or SSRIS
▪ can intensify the actions of levodopa which may lead to intense and controllable
urges like sex, gambling, and spending money
▪ suddenly falling asleep (you need to warn patient to avoid driving and other
potentially dangerous activities)
EPILEPSY
- a group of neurological diseases characterized by recurrent seizures.
SEIZURE
- happen as a result of sudden surge in the brain’s electrical activities.
- depends on what part of the brain is affected its symptoms include:
❖ loss of awareness
❖ unusual behaviors/sensations
❖ uncontrollable movements
❖ loss of consciousness
● EXITATORY NEURONS - stimulates others to fire rxn potentials and transmit electrical
messages
● INHIBITORY NEURONS - suppress this process, preventing excessive firing
❏ A balance between excitation and inhibition is essential for normal brain functions.
❏ If this abnormal electrical surge happens within a limited area of the brain, it causes
PARTIAL or FOCAL seizures. Partial seizures subdivide further to:
- Simple partial - depending on the affected brain area, patients may have unusual
feelings, strange sensations, or uncontrollable jerky movements, but remain
conscious and aware of the surroundings .
❏ If the entire brain is involved, GENERALIZED seizures will result. Generalized seizures
subdivide further to:
- Clonic seizures - associatd with rhythmic, jerky muscle movements, are rare
❏ Tonic-clonic seizures, also known as convulsive seizures - The most common and
also most dramatic, are combinations of muscle stiffening and jerking. This type is what
most people relate to when they think of a seizure. It also involves sudden loss of
consciousness and sometimes loss of bladder control. A tonic-clonic seizure that lasts
longer than 5min requires immediate medical treatment.
❏ Generalized seizures that start in childhood are likely to involve genetic factors.
Epilepsy due to a single gene mutation is rare. More often, an interaction of multiple genes and
environmental factors is responsible. Hundreds genes have been implicated.
❏ Examples include genes encoding for GABA receptors – major components of the
inhibitory circuit, and ion channels.
❏ Many genetic disorders that cause brain abnormalities or metabolic conditions have
epilepsy as a primary symptom.
❏ An EEG may also help in differentiating between partial and generalized seizures.
❏ Many anti-epileptic drugs are available which target sodium channels, GABA
receptors, and other components involved in neuronal transmission. Different
medicines help with different types of seizures. Patients may need to try several drugs to
find the most suitable.
❏ Dietary therapy: ketogenic diet has been shown to reduce or prevent seizures in many
children whose seizures could not be controlled with medication.
❏ Ketogenic diet is a special high-fat, low-carbohydrate diet that must be prescribed and
followed strictly. With this diet, the body uses fat as the major source of energy instead
of carbohydrates. The reason why this helps control epilepsy is unclear.
❏ A surgery may be performed to remove part of the brain that causes seizure. This is
usually done when tests show that seizures are originated from a small area that does
not have any vital function.
UNDERSTANDING PARKINSON’S DISEASE (PD)
PATHOLOGY
➢ Patients with PD experience a loss of cells to a region of the brain called SUBSTANTIA
NIGRA
➢ Patients with PD will see a decline in physical, psychological, and neurological funtions.
➢ The disease manifests in a form of slowed movement known as BRADYKINESIA
➢ Resulting in muscle tremors, gait problems, rigidity or stiffness,postural instability, and
cognitive impairment
➢ The disease is both chronic and progressive, patients gradually lose their ability to
perform even the simplest of tasks.
➢ No cure for Parkinsons, a number of treatments are available for the management of
motor and non-motor symptoms to be used in combination of medications.
➢ Currently, the most popular surgical therapy for the treatment of PD is DEEP BRAIN
STIMULATION (DBS)
➢ Targeted exercise that focuses on general mobility and dexterity may slow down the
progression of the disease
➢ Lifestyle modifications, balanced diet, and rest may also slow down symptoms.
➢ An upcoming form of treatment for PD is VIRTUAL REALITY (VR)
DOPAMINE
- a chemical messenger responsible for transferring signals within the brain that
allow coordination of movement.
- when dopamine levels decrease it causes abnormal brain activity, leaving patients less
able to direct or control movements
SYSTEM
- a group of neurons with gaps in between electrical signals pass between these gaps
from one neuron to the next with the help of neurotransmitters
- when acetylcholine binds to the receptor, it opens the receptor and allows sodium to
enter
PIC OF SODIUM
- when sodium enter neuron, its ionic charge allows electrical signal to move from last
neuron to the next
- with acetylcholine bound to the receptor the electrical signal fires until it reaches the
muscle
PIC OF ACETYLCHOLINESTERASE
ACETYLCHOLINESTERASE
- enzyme that breaks down acetylcholine
- breaking down acetylcholine will stop it from being able to open the receptor
- if receptor stays closed---then sodium cannot enter---electrical signal cannot be relayed to the next
nerve
- Acetylcholinesterase Inhibitors WILL BIND to acetylcholinesterase and keep them from breaking
down acetylcholine
- since acetylcholine is NOT broken down, it can BIND to the receptor and ALLOW sodium to ENTER
and allows electrical signal to continue to next neuron
With the nerve impluse continuing to its destination,the muscles can contract and relax. Acetylcholinesterase Inhibitors for
Alzheimer’s Disease
Acetylcholinesterase/Cholinesterase Inhibitor
- is a classification of medication that can be administered to a patient with alzheimer’s disease take note
that one of the theories in alzheimer’s disease poses that there is degeneration of the cholinergic
neuron and there is deficiency in acetylcholine.
- An enzyme called acetylcholinesterase breaks down acetylcholine if this will happen the level of
acetylcholine will further deplete to prevent such from happening.
- Administered which will then inhibit the cholinesterase and preserve the acetylcholine
Ex. Of these medications:
• Donepezil
• Memantine
• Galantamine
• Revastigmine
Rivastigmine
- Increases the amount of Ach at the cholinergic synapses
- Give twice a day
- Contradicted to patients with liver disease because hepatotoxicity may occur.
Assessment
• Assess the patient’s mental and physical abilities.
• Obtain a history that includes any liver or renal disease or dysfunction
• Assess for memory and judgement loss
• Observes for signs of behavioral disturbances
• Examine pt. for signs of aphasia
• Note motor function
• Determine family member’s ability to cope with patient’s mental and physical changes.
Nursing Diagnosis:
• Self care Deficit related to memory loss
• Chronic confusion related to memory loss
Planning:
• Patient’s memory will be improved
• Patient will maintain self care of body functions with assistance
Nursing Interventions
• Assist the patient in ambulation and activity
• Monitor for side effects
• Record Vital signs periodically
• Observe any patient behavioral changes
• Patient teaching:
-Teach family members about safety measures
-Patient should rise slowly to avoid dizziness and loss of balance
-Monitor routine liver function tests
Evaluation
• Evaluate effectiveness of drug regimen
Drugs for Myasthenia Gravis
-is a chronic autoimmune neuro muscular disease that affects approximately 20 in every 100 000 people
Antibodies attack the acetylcholine receptor sites then later on these receptor sites will be obstructed and
eventually destroyed so there will be less acetylcholine receptor sites and so the acetylcholine molecucles are
prevented from binding to the receptors and the stimulation of normal neuromuscular transmission is inhibited
thereby there is ineffective muscular contraction and weakness because take note your acetylcholine is very
important neurotransmitter in order for your muscles to contract so if theres a problem with the transmission so
later on there will be also a problem in relation to muscle contraction.
Manifestations:
• Ptosis
• Diplopia
• Dysphagia
• Dysarthia
• Respiratory muscle weakness
Acetylcholine may also be depleted because of the enzyme Acetylcholine or cholinesterase take note
that this enzyme is responsible for the breakdown of acetylcholine and so to stop that
acetylcholinesterase will be administered in order to inhibit the action of the acetylcholinesterase
and it will prevent the breakdown of acetylcholine thus preserving acetylcholine and this means
that there is more acetylcholine available to activate the cholinergic receptors and promote
muscle contraction.
Ex medications:
Neostigmine
Pyridostigmine
Neostigmine
• Short-acting, with half life of 0.5-1 hour
• Must be given on time to prevent muscle weakness
Pyrodostigmine
• Half-life of oral pyrodostigmine is 3-7 hours and is 2-33 hours for IV
• Given every 4-6 hours
• Increases muscle strength
Take note that overdosing or under dosing of acetylcholinesterase inhibitors has an effect it could be
Myasthenic crisis or cholinergic crisis.it is
Myastheic Crisis
- Underdosage of acetylcholinesterase inhibitor
- Severe complication manifested as generalized muscle weakness that may involve the muscles of
respiration
- Triggered by infection,emotional stress,menses,pregnancy,surgery, trauma,hypokalemia,temperature
extremes and alcohol intake
- Occurs 3-4 hours after taking certain medications like
aminoglycosides,phenytoin,macrolides,fluoroquinolones,quinine,quinidine,magnesium salt,psychotropic
medications and neuromuscular blocking agents.
Cholinergic Crisis
- And overdosage of the acetylcholinesterase inhibitor
- Occurs within 30-60 mins after taking anticholinergic drugs,this complication is due to continuos
depolarization of post synaptic membranes that creates neuromuscular blockade
- Often has severe muscle weakness that can lead respiratory paralysis and arrest accompanying
symptoms include meiosis or abnormal pupil constrictiom,power,sweating,vertigo,excessive
salivation,nausea vomiting,abdominal cramping,diarrhea,bradycardia and fasciculations or
involuntarymuscle twitching.
Endrophonium
- is a ultra short acting cholinesterase inhibitor may be used to distinguish between the myasthenic crisis
from cholinergeic crisis.
- Used to diagnose myasthenia gravis its ultra short duration of 5 to 30 mins. Increases muscle strength
immediately.
Pyrodistigmine
Assesment:
Nursing Diagnosis:
Nursing interventions:
• Monitor effectiveness of drug therapy.
• Administered prescribed AChE inhibitor following dosage recommendation
• Observe for cholinergic crisis
• Have antidote for cholinergic crisis ready: Atroponine Sulfate
Patient teaching:
• Teach patient to take drugs as ordered
• Encourage pt. to wear a medical ID or necklace that indicates health problem
• Teach pt.about side effects
• Inform pts to take the drug meals for best absorption
Evaluation:
• Evaluate effectiveness of drug therapy
• Determine the absence of respiratory distress
• Evaluate the correct use of the drug by the patient
Problems:
• Motor
• Sensory
• Neurologic
• Cerebellar
• Emotional
Immunomodulators
• Are disease-modifying drugs
• The first line of treatment for MS
• Examples:
-Beta interferon
Interferon beta 1-a
Interferon beta 1-b
-Glatiramer acetate
-Teriflunomide
Corticosteroids
- Used to manage exacerbation of MS
antipsychotic agents - are also known as neuroleptics or psychotropics but the preferred name for
this group is either antipsychotics or neuroleptics.
neuroleptic - refers to any drug that modifies psychotic behavior and exerts an antipsychotic effect
Schizophrenia- a chronic psychotic disorder is the major category of psychosis in which many of the
mentioned symptoms are manifested
non-phenothiazine
we have the buterophenones ,the benzoxazipines ,the hydroendolones and the thiosunthenes.
antipsychotic agents block the action of dopamine and thus may be classified as dopaminergic
antagonists specifically it blocks the dopamine receptors
on the other hand atypical antipsychotics have a weak affinity to detail receptors and a stronger affinity
to d receptors and they block the serotonin receptor. these agents cause fewer extra pyramidal
symptoms than typical antipsychotic agents which have strong affinity to detail receptors
phenothiazinegroup
1. Aliphatic -aliphatic medications produce a strong sedative effect decrease blood pressure and may
cause moderate extrapyramidal symptoms. an example of an aliphatic medication is chlorpromazine
hydrochloride thorazine
2. piperazine- piperacin produce more extrapyramidal symptoms dry mouth urinary retention and
aggranocytosis. an example of this medication is the flofenazine and perfinazine
3. Piperidine- has a strong sedative effect few extra pyramidal symptoms has a low to moderate effect
on blood pressure and has no anti-emetic effect. an example of this classification of medication is
thioridazine.
most antipsychotics can be given orally in a form of tablet or liquid. it can also be given intramuscularly
or intravenously. for oral use the liquid form might be preferred because some patients may hide tablets
in their cheek or under their tongue to avoid taking them. mouth checks are necessary for non-compliant
patients.
phenothiazine metabolites may cause a harmless pink to red brown urine color the
Full therapeutic effect of oral antipsychotics may not be evident for three to six weeks following initiation
of their therapy but an observable therapeutic response may be apparent after seven to ten days.
Nonphenothiazine
1. butyrophenone group- a frequently prescribed nonphenothiazine
specifically under butyrophenone is haloperidol (Haldol)
haloperidol's pharmacologic behavior is similar to that of the phenothiazines.
it is a potent antipsychotic drug in which the equivalent prescribed dose is smaller than that of drugs of
lower potency
that is if the medication is administered intramuscularly. because the medication is a viscous liquid a
large gauge needle such as gauge 21 should be used with a z track method for administration in a
deep muscle. the injection site should not be massaged and sites should be rotated
these medications should not remain in a plastic syringe longer than minutes take note
this is true if the medication is administered intramuscularly
there are also capsules or tablet forms of haloperidol
2. Dibenzoxazepine- this classification of medication has moderate sedative and orthostatic
hypotensive effect an example of this medication
is loxapine
3. dihydroindolone -this medication has low sedative and orthostatic hypotensive effect
an example of this classification of medication is molindone
characteristics of akathisia include restlessness, trouble standing still, paces the floor
and feet in constant motion ,rocking back and forth
acute dystonia is characterized by facial grimacing ,involuntary upward eye movement ,muscle
spasms on the tongue face neck and back (the back muscle spasms cause trunk to arch forward)
further in acute dystonia there is
laryngeal spasms
tardive dyskinesia is characterized by protrusion and rolling of the tongue,
sucking and smacking movements of the Lips, chewing motion ,facial dyskinesia And, involuntary
movements of the body and extremities
these extrapyramidal symptoms can begin within-days after initiation of antipsychotic therapy and are
most prevalent with the Phenothiazines, butyrophenones and thiosanthines
tardive dyskinesia may develop in 20% of patients taking antipsychoticsfor long-term therapy
Neuroleptic malignant syndrome is a rare but potentially fatal condition associated with antipsychotic
drugs
neuroleptic symptoms involve muscle rigidity ,hyperthermia altered mental status, profuse diaphoresis,
blood pressure fluctuations, tachycardia ,dysrhythmias, seizure rhabdomyolysis ,acute renal failure,
respiratory failure ,and coma.
atypical antipsychotic agents -these are effective in treating both positive and negative symptoms of
schizophrenia
phenothiazines can decrease the effect of anticonvulsants thus an adjustment on the dosage of the
anticonvulsant may be necessary but take note that it has to be prescribed by the physician so you as
a nurse your responsibility here if and when the patient has seizure and is taking an anti-seizure
medication is that you need to inform the physician right away so that the physician can adjust the
dosage of the medication
assess mental status and cardiac eye and respiratory disorders before starting drug therapy and
continue daily assessment
Possible nursing diagnosis you can formulate are
ineffective relationship related to social withdrawal
risk for loneliness
what is our plan why are we administering phenothiazine or nonphenothiazine medication to our
patients ? it is to improve the psychotic behavior of our patients through medications, psychotherapy
and, adjunct therapy
anxiolytics
- primarily used to treat anxiety and insomnia
Medication: benzodiazepine
-multiple uses such as anticonvulsant , sedative hypnotic ,pre-operative drug
substance abuse withdrawal, and anxiolytic
-mainly for severe or prolonged anxiety examples
Examples of benzodiazepines
⚫ Chlordiazepoxide
⚫ Diazepam
⚫ Clorazepate dipotassium
⚫ Lorazepam- the most frequently prescribed
⚫ Alprazolam
Assessment:
Assess for suicidal ideation
Determine the patients support system
Obtain a drug history
Diagnosis;
Anxiety related to situational crisis
Planning:
aim to reduce the anxiety and stress of the patient through pharmacologic methods like the use of
benzodiazepines or support in group therapy
Nursing interventions:
Observe patient for side effects
Monitor vital signs
Encourage family to be supportive of thepatient
Advise patients not to drive a motorvehicle
Warn patients not to consume alcohol or cns depressants
Inform patients that an effective response may take one to two weeks
Encourage patients to rise slowly from sitting to standing positions to avoid dizziness fro orthostatic
hypotension
Evaluation:
Evaluate the effectiveness of drug therapy
Determine whether the patient is taking the anxiolytic drug as prescribed
ANTIDEPRESSANT AGENTS
-that are used to treat clinical depression or prevent it from recurring
Depression
⚫ most common mental illness
⚫ Characterized primarily by mood changes and loss of interest in normal activities
Types:
1. Reactive
2. Major depression
3. Bipolar Disorder
5 groups of Antidepressants
1.Tricyclic antidepressants or (tca) or trycyclics
2.selective serotonin reuptake inhibitors or (ssris)
3.Serotonin norepinephrine reuptake inhibitor or (snris)
4.atypical antidepressants
5. monoamine oxidase inhibitors (MAOIs)
we've been mentioning anticholinergic effects what is the most common anticholinergic effect that we've mentioned
ever since we started this topic that is urinary retention
Drug examples:
⚫ Amitriptyline HCL
⚫ imipramine
⚫ trimipramine
⚫ Doxepin
⚫ Clomipramine HCL
Alcohol hypnotics sedatives and barbiturates potentiate the cns depression when taken with tca
Drug examples:
⚫ Fluoextine
⚫ Fluvoxamine
⚫ sertraline
⚫ Paroxetine
⚫ Citalopram
⚫ escitalopram
-Many ssris have an interaction with grapefruit juice that can lead to possible toxicity
Side Effects:
⚫ dry mouth
⚫ blurred vision
⚫ Insomnia
⚫ headache
⚫ nervousness
⚫ anorexia
⚫ nausea
⚫ diarrhea
⚫ suicidal ideation
Drug Examples:
⚫ Venlafaxine
⚫ Duloxetine
⚫ Desvenlafaxine
Side Effects:
⚫ drowsiness
⚫ Dizziness
⚫ insomnia
⚫ headache
⚫ euphoria
⚫ amnesia
⚫ blurred vision
⚫ ejaculatory dysfunction
Adverse Reactions:
⚫ Hypertension
⚫ Tachycardia
⚫ angioedema
⚫ seizures
⚫ suicidal ideation
4. atypical antidepressants
-the second generation
antidepressant
-used for major depression reactive depression and anxiety
-affects one or two of the three neurotransmitters which are serotonin,norepinephrin ,and dopamine
Drug Examples:
⚫ amoxipine
⚫ nephazodone
⚫ moprotiline
⚫ trazodone
should not be taken with maois and should not be used within 14 days after discontinuing maoi's
Side Effects:
⚫ agitation
⚫ Restlessness
⚫ Insomnia
⚫ orthostatichypotension
⚫ anticholinergic effects
MOOD STABLIZERS
- used to treat bipolar affective disorder (is a psychological illness that involves severe mood
swings)
these mood swings take the form of depression or mania and may last for several months at a
time
during the time of depression patients often have a great sadness guilt no appetite poor sleep
and cannot enjoy themselves
mania is the opposite of this with patients experiencing erratic and excited behavior
drug examples:
⚫ lithium
⚫ Carbamazepine
⚫ Valproic acid
⚫ Divalproex
⚫ Lamotrigine
These are considered as the first line of drugs for bipolar disorder
Lithium
-is an inexpensive drug that must be closely monitored because it has a narrow therapeutic
serum range of 0.8 to 1.2 ml equivalent per liter
-serum sodium levels also need to be monitored because lithium tends to deplete sodium
side effects:
Dry mouth
Thirst
increased urination
weight gain
bloated feeling
metallic
taste
edema on the hands and ankle
Opioid Analgesic
- narcotic medications that treats severe pain (ex. Headache or muscle)
Indication:
-relief of moderate to severe pain,
-pre-operative medication
-as supplement to anesthesia
Contraindication
-head injury
-shock or very low blood pressure
Assessment:
a. Obtain Medical history
- contraindications for morphine sulfate
include severe respiratory disorders
increased intracranial pressure, seizures may be present when taking these
Nursing Diagnosis
- Acute pain related to surgical tissue injury
-Ineffective breathing pattern related to excess morphine dosage
Planning
- To reduce and alleviate patient’s pain
Interventions:
-Administer morphine sulfate before pain reaches its peak
-Monitor vital signs – fewer than 10 respirations/min can indicate respiratory distress
-Record urine output – should be at least 600ml/day
-Check bowel sounds
-Check for pupil changes and reaction. Pinpoint pupils can indicate morphine overdose
-Have naloxone available
-Encourage patient not to use alcohol or CNS depressants
-Suggest non-pharmacologic measures to relieve pain
-Alert patient that continuous use of morphine sulfate can be addicting
Evaluation
- Evaluate the effectiveness of morphine in lessening or alleviating the pain in using consistent pain scale
-Determine the stability of vital signs
2. Meperidine
- can be given orally, Intramuscularly or IV routes
- primarily effective in GI procedures
-preffered during pregnancy (does not diminish contraction, and causes neonatal respiratory depression)
-not indicated to patients with chronic pain, sever liver dysfunction, sickle cell disease, history of seizure, severe CAD, and
cardiac dysrhythmia
3. Hydromorphone
-6x more potent than morphine
-for relief of moderate or severe pain
-when given IV, dilution of each dose with 5ml sterile water or NSS is preferred
-Direct administration of 2mg or less should be given over 2-3 minutes
Migraine Headaches
- characterized by unilateral throbbing head pain accompanied by nausea, vomiting, photophobia
Mild migraine:
-aspirin
-acetamoniphen
-NSAIDS (ibuprofen and naproxen)
Nonopioid Analgesic – less potent than opioid and used to treat mild to moderate pain
Nursing Diagnosis:
Risk for Injury
Acute pain related to edema from the surgical incision
Planning:
To alleviate the pain from the patient
Interventions:
Check hepatic enzyme tests
Teach patients to keep acetaminophen out of childrens reach
Advice patients not to self-medicate with acetaminophen for more than 10
days
Teach patients to check acetaminophen dosages on the label of OTC drugs.
4g/day
Avoid alcohol ingestion while taking the drug
Antidote for acetaminophen is acetylcysteine
Evaluation
Evaluate the effectiveness of the drug in terms of relieving pain using
consistent pain scale.
Determine whether the patient is taking the recommended dosage
ANTI-INFLAMMATORIES:
1.) NSAIDS
2.) CORTICOSTEROIDS
3.) DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
4.) ANTIGOUT DRUGS
Note: Aspirin should not be taken during last trimester of pregnancy and children
with flu.
Note: indomethacin is very irritating to stomach and should be taken with food,
these types of drugs may also cause sodium and water retention and increase in
BP.
Note: Ketorolac are recommended for short term management of pain, like after
surgery bc its very effective in alleviating pain.
D.) Propionic Acid Derivatives – are aspirin-like but have stronger effects and
creates less GI irritation
Examples: Fenoprofen CA, Flurbiprofen, Ibuprofen, Ketoprofen,
Naproxen, and Oxaprozin
Note: Gastric Irritation is a common side effect, therefore should be taken with
food.
F.) Oxicams – used for long term rheumatoid arthritis and osteo
Examples: piroxicam and meloxicam
Note: It can cause GI problems like ulceration and epigastric distress, it should not
be taken with aspirin and other nsaids.
SUMMARY:
Nonopioid Analgesic – less potent than opioid and used to treat mild to moderate pain
ANTI-INFLAMMATORIES:
1.) NSAIDS
2.) CORTICOSTEROIDS
3.) DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
4.) ANTIGOUT DRUGS
7 Groups of NSAID:
1.) Salicylates
2.) Para-Chlorobenzoic Acid
3.) Phenylacetic Acid Derivatives
4.) Propionic Acid Derivatives
5.) Fenamates
6.) Oxicams
7.) COX-2 Inhibitors
Important note: the first 6 groups of NSAIDs have the same mechanism of action which is to
block COX-1 and COX-2 and the 7th has a mechanism of only blocking COX-2. COX stands for
cyclooxygenase.
⁃ � Sympathetic, SNS
⁃ � Parasympathetic, PSNS
✏️ in situations that requires alertness and energy, such as facing danger or doing physical
activities, the ANS activates its sympathetic division to mobilize the body for action.
� cardiac output
� dilates pupil
✏️ it also inhibits body processes that are less important in emergencies, such as:
✏️On the other hand, during ordinary situations, the parasympathetic division:
� it slows heartbeats, decreases respiratory rate, stimulates digestion, removes waste and stores
energy.
� � The sympathetic division is therefore known as the "FIGHT or FLIGHT" response, while the
parasympathetic division is associated with the "REST and DIGEST" state.
Despite having opposite effects on the same organ the S&S and PS NS are not mutually exclusive
in most organs both systems are simultaneously active producing a background rate of activity
called the autonomic tone a balance between sympathetic and parasympathetic inputs.
This balance shifts one way or the other in response to the body's changing needs some organs,
however receive inputs from only one system, for example the smooth muscles of blood vessels
only receives sympathetic fibers which keep them partially constricted and thus maintaining
normal blood pressure an increase in sympathetic firing rate causes further constriction and
increases blood pressure. While a decrease in firing rate dilates blood vessels lowering blood
pressure.
The autonomic nerve pathways from the control centers in the central nervous system
✏To the target organs are composed of two neurons which meet and synapse in an autonomic
ganglion
Accordingly, these neurons are called pre ganglionic and post ganglionic in the SNS the pre
ganglionic
neurons arise from the thoracic and lumbar regions of the spinal cord their fibers exit by way of
spinal nerves to the nearby sympathetic chain of ganglia.
✏Once in the chain preganglionic fibers may follow any of three routes
ANS 1
Afferent/Sensory Neurons – sends impulses to the CNS where they are interpreted or
integrated
Efferent/Motor Neurons – receives the impulses or informationfrom the brain and transmits
these impulses through the spinal cord to the effector cells
*Both act on the same organ but produce opposite responses to provide homeostasis or balance ;
can act as stimulating agent or a depressing agent
1. Adrenergic Agonists
- Drugs that stimulate the sympathetic nervous system
- Also called as “adrenergics” or “sympathomimetics”
- They mimic the sympathetic neurotransmitters norepinephrine and epinephrine
- They act on one or more adrenergic receptor sites located in the effector cells of muscles
(such as the heart, bronchiole walls, GI tract, urinary bladder and ciliary muscles of the
eyes)
Inactivation of Neurotransmitters:
1. Reuptake of the transmitter back into the neuron (nerve cell terminal)
2 enzymes that inactivates Norepinephrine:
Monoamine Oxidase (MAO) – located inside the neuron
Catechol-O-methyltransferase (COMT) – located outside the neuron
*These medications can prolong the action of neurotransmitter by either inhibiting the reuptake
or inhibiting the degradation by enzymatic action
2. Enzymatic transformation or degradation
3. Diffusion away from the receptor
Classification of Sympathomimetics
Catecholamines
Non-Catecholamines
Ø It blocks the effects of the neurotransmitter either directly by occupying the receptors or
indirectly by inhibiting the release of the neurotransmitters norepinephrine and epinephrine
ANS 2
EPINEPHRINE
Pregnancy category C
Dosage: Adult: subcut/IM: 0.3 mg Epipen Auto injector, may repeat in 5-20 mins
Acts on alpha and beta receptors; promotion of CNS and cardiac stimulation and
bronchodilation, strengthens cardiac contraction, increases cardiac rate and cardiac output;
reduces mucosal congestion by inhibiting histamine release; reverse anaphylactic reactions
Indications:
- Nasal Congestion
- Allergic reaction
- Anaphylaxis
- Asthma
- Bronchospasm
- Angioedema
- Status Asthmaticus (severe type of asthma)
- Cardiac arrest
- Cardiac resuscitation
Contraindications:
- Cardiac tachydysrhythmias
- Cerebral arteriosclerosis
- Labor
- Closed-angle glaucoma
Caution
-Hypertension
-Prostatic hypertrophy
-Hyperthyroidism
-Pregnancy
-Diabetes mellitus
SIDE EFFECTS
-Anorexia
-Restlessness
-Tremors
-Agitation
-Sweating
-Headache
-Pallor
-Insomnia
-Weakness
-Dizziness
-Hyperglycemia
ADVERSE REACTIONS
-palpitations
-tachycardia
-hypertension
-dyspnea
-Ventricular fibrillation
-Pulmonary edema
DRUG INTERACTIONS:
ALBUTEROL SULFATE
Bronchospasm prophylaxis : Immediate release: A/ado: PO: Initially 2-4 mg q6-8h: max 32 mg/d
Extended release: A/adol: PO: 4-8mg q12h; max 32 mg/d C: 6-12y:PO initially 4 mg q12h; max
24 mg/d
MOA: Stimulates beta2 adrenergic receptors in the lungs, which relaxes the bronchial smooth
muscle, thus causing bronchodilation
Albuterol sulfate
Indications:
- To treat Asthma
- For prophylaxis and treatment of acute bronchospasm
Contraindications:
- Hypersensitivity
- Milk protein hypersensitivity
Caution
-Tremor
-Dizziness -nasopharyngitis
-Drowsiness -Insomnia
-Nervousness -Weakness
-Restlessness -Nausea
-Agitation -Diarrhea
-Sweating
-Headache
ADVERSE REACTIONS
-palpitations -tachycardia
-hypertension -infection
- Hyperglycemia -Hypokalemia
LIFE THREATENING
- Cardiac dysrhythmia
- Angioedema
- Bronchospasm
- Steven-Johnson Syndrome
ALBUTEROL SULFATE
Drug-lab Interactions:
Alpha 1 agonist
-Midodrine hydrochloride
-Phenylephrine hydrochloride
- Norepinephrine bitartrate
- Dopamine hydrochloride
Alpha 1, Beta 1 and Beta 2 agonist
- Epinephrine
- Ephedrine hydrochloride
Beta 1 agonist
- Dobutamine hydrochloride
Beta 2 agonist
- Metaproterenol sulfate
- Terbutaline Sulfate
Nursing Assessment
3. Administer antidote, phentolamine mesylate, 5-10 mg, diluted in 10-15 mL, of saline
infiltrated into the areas of IV extravasation of norepinephrine and dopamine.
4. Report patient’s vital sign and check blood pressure every 3-5 mins or as indicated to avoid
severe hypertension
5. Monitor the ECG for dysrhythmia when adrenergic agonists given intravenously.
6. Report side effect of Adrenergic drugs such tachycardia, palpitations, tremors, dizziness,
and increased blood pressure.
9. Evaluate blood glucose levels in patients with diabetes mellitus for potential elevation.
CLIENT TEACHING
General
1. Advise the patient to read labels on all over the counter (OTC) drugs for cold symptoms
and diet pills.
2. Explain continuous use of nasal sprays or drops that contain adrenergic agonists may
result in rebound nasal congestion.
Self- Administration
ANS 3
Alpha 1 Receptor
· Eye – increased pumping of heart can cause reflex tachycardia – can result in constriction of
pupils or miosis
§ Beta 1 blocker with ISA (intrinsic sympathomimetic activity – term used to descibe the ability
of a certain beta blocker to bind with a beta receptor which produces a complete activation) :
acebutolol
· Heart – decreases heart rate and blood pressure, reduces force of contraction – beta adrenergic
blockers useful in treating mild and moderate hypertension, angina, heart failure, and myocardial
infarction
· Kidney – suppresses renin angiotensin aldosterone system (RAAS) – decreases blood pressure
Beta 2 receptor
Atenolol
ü Pregnancy Category D
ü Dosage: Hypertension – Adult: PO: Initially 25-50 mg/d; may increase to 100 mg/d after 7 days;
max of 100 mg/d
ü MOA: selectively blocks beta 1 – adrenergic receptor sites, decreases sympathetic outflow to
periphery, suppresses renin – angiotensin – aldosterone system
ü Contraindications: sinus bradycardia, heart block greater than first degree (exhibits decrease in
heart rate – reason why contraindicated), cardiogenic shock (heart suddenly can’t pump enough
blood to body), pulmonary edema (excess fluid in lungs), acute bronchospasm, pregnancy and
lactation Caution: Renal dysfunction, diabetes mellitus
ü Drug interactions:
o Increased absorption with atropine and other anticholinergics
o Increased risk of hypoglycemia with insulin and sulfonylureas (note medication decreases blood
sugar)
Phentolamine mesylate
ü Pregnancy Category C
ü Dosage: Adult: subcut: 5-10 mg in 10 ml NS injected into extravasation area to prevent dermal
necrosis
ü MOA: Binds to alpha-1 receptors, resulting in a decrease in peripheral vascular resistance and
vasodilation
ü Indications: Pheochromocytoma (rare tumor in adrenal gland tissue, resulting in release of too
much epinephrine and norepinephrine hormones that controls the heart rate, metabolism, and
blood pressure) diagnosis, hypertension in pheochromocytoma surgery, dermal necrosis due to
epinephrine/norepinephrine extravasation (antidote)
ü Side effects: Weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea,
vomiting
Alpha 1 blockers
· Phentolamine mesylate
· Doxazosin mesylate
· Prazosin hydrochloride
· Terazosin hydrochloride
· Carvedilol,
· Labetalol
· Metoprolol tartrate
· Atenolol
· Acebutolol hydrochloride
· Betaxolol
· Bisoprolol fumarate
· Esmolol hydrochloride
· Propanolol hydrochloride
· Nadolol
· Pindolol
· Sotalol
· Timolol maleate
Reserpine
ü Classification: adrenergic neuron antagonist (drugs that blocks the release of norepinephrine
from the sympathetic terminal neurons)
ü Pregnancy Category C
ü Dosage: Hypertension – Adult: PO: initially 0.5 mg/d for 1-2 weeks; maintenance: 0.1 – 0.25
mg/d
ü MOA: an adrenergic neuron antagonist that blocks the release of norepinephrine from the
sympathetic terminal neurons; reduces the serotonin and catecholamine transmitters
ü Also crosses placenta and blood-brain barrier and enters the breast milk, fully absorbed from
GI tract
ü Indications: Hypertension
ü Contraindications: Active peptic ulcer (stimulates HCl secretion in stomach and might cause
further peptic ulcer), history of mental depression, Parkinson’s disease Caution: Myocardial
infarction, cardiac arrhythmias, gallstones, epilepsy, pregnancy, lactation
ü Drug interactions:
Nursing Assessment
Nursing Interventions
2. Report any complaints like dizziness, lightheadedness, early morning insomnia, mental
depression or chest pain
4. Note any complaint of stuffy nose because vasodilation may result and nasal congestion can
occur
Client Teaching
General
Self-administration
1. Teach the pt and the family how to take pulse and blood pressure
2. Encourage pt to take adrenergic neuron antagonists at the same time every day and not to
discontinue it w/o permission from the health care provider (may cause rebound effect)
Side effects
2. Inform pt and family of possible psychological changes when taking adrenergic neuron
antagonist, which occur because of catecholamine depletion
3. Warn pt that med may cause erectile or ejaculation dysfunction which is usually dose related
4. Advise pt not to drive or operate dangerous equipment until drug response is known
Cultural considerations
2. Provide an interpreter with the same ethnic background and gender if possible, especially when
sensitive topics are being addressed
Evaluation
ANS 4
Bethanechol Chloride
Brand name: Urecholine ,urotone
Pregnancy category C
Classification:Direct acting cholinergic agent
Dosage: Urinary retention
Adult: PO: initially 5-10 mg tid/qid; maintenance: 10-50mg
tid/qid;maximum:200mg/d
Adult;subcut: 5mg tid/qid; maximum 40 mg/d
MOA: stimulates the cholinergic(muscarinic) receptors: promotes contraction of the bladder ;
increases GI secretion and peristalsis, pupillary constriction and bronchoconstriction(pporly
absorbed in the GI tract but mostly secreted in the urine)
Indications:
Urinary retention
Neurogenic bladder
Contraindications:
Intestinal or urinary tract obstruction
Irritable bowel syndrome
Bradycardia
Hypotension
COPD
Asthma
Peptic ulcer
Hyperthyroidism
Seizures
parkinsonism
Side effects
Hypotension
Tachycardia
Blurred vision
Excessive salivation
Increase gastric acid secretion
Abdominal cramps
Diarrhea
bronchoconstriction
Adverse reactions:
Tachycardia
weakness
Life threatening:
Bronchospasm
1. Metoclopramide hydrochloride
-prescibed to treat gastroparesis, nausea and GERD.
-in low doses, it enhances gastric motility and thus accelerate gastric
emptying time.
2. Pilocarpine( for the eyes)
- acts on the nicotinic receptor
MOA: constricts the pupil of the eye that results in opening the schelm
canal to promote drainage of aqueous humor
IND: used to treat glaucoma by relieving fluid pressure in the eye and
promote miosis in eye surgery and examinations
-oral form is used to relieve xerostomia(dry mouth)
Side effects:
Hypotension
Bradycardia sweating
Hypersalivation
GI Distress
Contraindications:
Intestinal or urinary obstruction
Give caustion to client with bradycardia, asthma ,peptic ulcer, hyperthyroidism
ANS 5
● CARDIOVASCULAR
● GASTROINTESTINAL
● URINARY TRACT
● CENTRAL NERVOUS SYSTEM-TREMORS OF THE MUSCLE
● BRONCHIAL
● GLANDULAR-DECREASES THE SALIVATION AND BRONCHIAL SECRETIONS
● OCULAR- DILATES PUPIL
ATROPINE
● Dry mouth
● Decreased perspiration
● Nausea
● Head ache
● Amnesia
● Constipation
● Dry skin
● Flushing
● Mydriasis
● Blurred vision
● Anxiety
● Photophobia
● Urinary retention
● Hyperflexia
● Ataxia
●
ADVERSE EFFECT
● Tachycardia
● Paradoxic bradycardia
● Hypertension
● Hypotension
● Angina
● Pulmonary edema
● Seizure
Life threatening:
● Dysrythmias
● Laryngospasm
● Steven johnson syndrome
● Coma
DRUG INTERACTIONS
BENZTROPINE
● Tachycardia
● Cardiac neuropathy
● Prostatic hypertrophy
● Psychosis
●
SIDE EFFECTS
● Nausea
● vomitting
● Dry mouth
● Constipation
● anhidrosis
● headache
● drowsiness
● Blurred vision
● cofusion
● depression
●
ADVERSE EFFECT
● Tachycardia
● Urinary retention
● Ocular hypertension
BENZTROPINE
Drug sample
-scopolamine
NURSING ASSESSMENT
o Anterior pituitary gland Take note: the thyroid hormone levels in the
blood are regulated by the negative feedback; it
Thyroid stimulating hormone is the anterior pituitary gland secretes TSH
which stimulates the thyroid gland to produce
Responds to the presence of thyroid T4 and T3
releasing hormone
Stimulates the release triiodothyronine (T3) Pancreas- exocrine and endocrine gland
and thyroxine (T4) from the thyroid gland
Islets of langerhans (has two important cells)
Adenocorticotropic hormone
Alpha Islet cells- produces glucagon (breaks
It is released in response to the glycogen down to glucose in the liver)
corticotropin releasing hormone in the
hypothalamus. Beta Islet cells- produces insulin (responsible
Stimulates the release of glucocorticoids for the uptake of glucose, amino acids, fatty
(cortisol), mineralocorticosteriod acids to converts them to substances that are
(aldosterone), and androgen from the stored in the body cells)
adrenal cortex.
Gonads
o Posterior pituitary gland- storage for
the hormones Female: Ovaries
No specific target gland, it affects the body Take note: Growth hormone can't be
tissues and bones administered orally because it will be inactivated
Established as a counter regulatory by the gastrointestinal enzymes.
hormone for insulin
Stimulates lipolysis which results free fatty Routes of Administration: Subcutaneous,
acids from the adipose tissue to the Intramuscular
circulation.
Factors to be qualified for growth hormone
o Presence of free fatty acids (FFA) therapy:
can induced insulin resistance,
increased FFA by hepatocytes 1. Growth hormone should be administered
results in oxidation and before it epiphysis or fused because it only
accumulation of key enzymes for acts on newly forming bone.
gluconeogenesis resulting in a
increase blood glucose level Drugs for clients with growth hormone
deficiency:
Clients with increased growth hormone-
increases glucose production through Somatropin or Genatropin- used to treat growth
gluconeogenesis and glycogenesis from failure in children because of pituitary growth
the liver and kidney hormone deficiency
Somatropin
-mimics the natural occurring GH in the
Growth Hormone Therapy body.
-also known as recumbenant growth
-for patients who has excess or deficiency with hormone
growth hormone usually treated with a
replacement hormone. Side effects:
- involves decreased activity of the thyroid gland Formulation: tablet and injection solution
usually due to a tumor in the region of the
Route: oral and intravenous
pituitary which resulting to a decreased thyroid
stimulating hormone in the blood Contains synthetic T3 only and has a short half -
life duration of action
* aside of the diagnostic usage of thyrotropin, it
is also given for clients with thyroid cancer but it Drug of choice for initial treatment of Myxedema
is not used to treat thyroid cancer alone but
rather it is used as an, *not recommended for maintenance therapy but
it is frequently used as initial therapy for treating
Adjunct Therapy for Well Differentiated Thyroid Myxedema because of its rapid onset of action
Cancer:
Liotrix (Thyrolar)
Formulation: tablet Cardiovascular collapse
Route: oral
Formulation: tablet
Route: Oral
Adverse Effects: Inhibits synthesis of thyroid hormones
Tachycardia - Methimazole (Tapazole)
Hypertension
Formulation: tablet
Palpitations
Osteoporosis Route: Oral
Seizure
Thyroid Crisis Does not inhibit synthesis of thyroid
Angina pectoris hormone
Atrial fibrillation
Does not inhibit the peripheral conversion Monitor thyroid function before and during
of T3 to T4 as does PTU but it is 10 times therapy
more potent and has a longer half life than
PTU WBC and differential count should be
monitored periodically
PTU
Advise patient to report sore throat, fever,
- Does not reverse hyperthyroidism rapidly chills, headache, malaise, weakness,
yellowing of eyes or skin and unusual
- More side effects bleeding immediately
- Has potential for liver damage *aside from thiomides, patients with
- Last resort when methimazole is not hyperthyroidism is also given iodine
appropriate Potassium iodide (SSKI)
Methimazole - iodine is necessary component of the
- Reverses hyperthyroidism rapidly thyroid hormone
Examples:
Combination Insulins
Examples:
CONTRAINDICATIONS OF INSULIN
Confusion
Agitation
Tremors
Headache
Flushing
Hunger
Ultra-Long Acting Insulin
Weakness
- Reaches the bloodstream in Lethargy
six hours, DOES NOT peak Fatigue
and last about 36 hrs or longer Urticaria
Irritation at injection site
Examples:
ADVERSE EFFECTS OF INSULIN
Tachycardia
Palpitations
Hypoglycemic reactions
Somogyi effect
Lipodystrophy
Anaphylaxis
Shock
NURSING CONSIDERATIONS
Amylin analogue
- used for type 1 and type 2 Diabetes
Mellitus patients
- administered before meals
- inhibits the release of glucagon while
eating
- slows food emptying in the stomach DRUGS FOR WOMEN’S HEALTH
- has a severe hypoglycemic effect
Side Effects:
- nausea Endometriosis – the abnormal location of
- vomiting the endometrial tissue outside the uterus.
- headache It is the common cause of dysmenorrhea,
chronic pelvic pain, and infertility.
HYPERGLYCEMIC DRUGS
- given to patients who experiences
induced hypoglycemia or other causes of
Ectopic endometrial implant responds to
hypoglycemia
endometrial control; particularly the
Glucagon estrogen. When menstruation occurs, the
- it protects the body cells especially in the ectopic endometrial implant proliferates
brain and retina by providing nutrients and and bleed.
energy needed to maintain body function
Increased Number of menstrual cycle
- available for parenteral use only
- use to treat insulin induced hypoglycemia
when other methods of providing glucose
are not available Inflammation of the surrounding organ
- blood glucose begin to rise in 10 minutes tissue
after administration.
Diazoxide
- it increases blood sugar by inhibiting TREATMENT
insulin release from the beta cells and
stimulating release of epinephrine
The goal of treatment is to decrease the
amount of circulating estrogen and limit or
eliminate estrogen. GN-RH AGONIST
This interrupts internal bleeding and - Potent drugs that inhibit GNRH
irritation associated with the ectopic release
endometrial implant and may even cause - Creates a hypoestrogenic
them to recede. environment
Examples:
Diarrhea
● Microorganisms in the GI tract disrupts epithelium of the intestine
● This results to poor water absorption
● Leading To diarrhea
● Loose, watery stool and possibly more frequent bowel movements
Constipation
● Accumulation of hard fecal material
Ulcer Formation
● Hypersecretion of hydrochloric acid and pepsin which erodes the GI mucosal lining
(Peptic Ulcer)
Nursing problems
● Nausea
● Diarrhea
● Constipation
● Risk for deficient fluid volume
● Pain
● Imbalanced nutrition: less than body requirements
● Anxiety
● Deficient knowledge
Drugs related to the Digestive System
Antiemetics
● Prevents nausea, vomiting, vertigo and motion sickness
● Not recommended during pregnancy
○ If vomiting and nausea threatens the mother and fetus
○ trimethobenzamide (tigan) is given
○ Pregnancy Category C
OTC / Nonprescription Prescription
Antihistamines Antihistamine
Phosphorated Benzodiazepines
Carbohydrate Solution
Serotonin Antagonists
Glucocorticoids
Cannabinoids
Miscellaneous antiemetics
Antihistamines
● MOA: Blocks h1 receptor sites - inhibiting stimulations of CTZ and vestibular
pathways
● Can be OTC or prescribed but differ in length of effect, side and adverse effects.
-Antihistamines
● Examples
○ Cyclizine HCl (Marezine)
○ Dimenhydrinate (Dramamine)
○ Meclizine HCl (Antivert)
● Administer 30-60 minutes before travel
○ Not effective if taken after vomiting has occurred
○ Should be taken after meals
Prescription Antiemetics
-Antihistamines
● Same MOA with OTC
● For postoperative nausea and vomiting and vertigo
● Examples
○ Hydroxyzine (Vistaril)
○ Promethazine (Phenergan)
● Administered preoperatively with narcotics
● Give hydroxyzine deep IM
● Side effects:
○ Drowsiness
○ Dry mouth
○ Blurred vision
○ Constipation
○ Hypertension
○ Transient leukopenia
○ Urinary retention
○ Photosensitivity
-Anticholinergics
● MOA: Act primarily on the vomiting center of the brain by decreasing stimulation of
the CTZ and vestibular pathways
● Scopolamine (Transderm-scop)
○ 3 days efficacy
○ Apply behind ear at least 4 hours before antiemetic effect is required
○ Alternate ears if using for longer than 3 days
○ Wash hands after applying patch
○ Apply no more than 1 patch at the same time
-Dopamine Antagonists
● MOA: block dopamine 2 receptors in the CTZ = suppression of vomiting
● 3 Categories
○ Phenothiazines, Butyrophenones Benzodiazepines
>Phenothiazines
● MOA: inhibit CTZ
● 2 uses:
○ Primary - treatment of severe nausea and vomiting
○ Secondary - reduce anxiety, tension and for psychosis
● Note: For vomiting the dose is smaller than when used for psychiatric problems
● Examples:
○ Prochlorperazine maleate (Compazine)
○ Promethazine (Phenergran)
○ Chlorpromazine (Thorazine)
● Antipsychotic
>Butyrophenone
● MOA: blocks the dopamine 2 receptors in the CTZ used in prevention of nausea and
vomiting during surgical and diagnostic procedures
● Examples:
○ Droperidol (Inapsine)
○ Haloperidol (Haldol)
● Antipsychotic
>Benzodiazepines
● For prevention of nausea and vomiting resulting from cancer chemotherapy together
with metoclopramide
● Example: Lorazepam (Ativan)
● Provides emesis control, sedation, anxiety reduction and amnesia
● Anxiolytic
Adverse effects
● EPS/Extrapyramidal symptoms
○ Antiemetic doses does not cause EPS
○ Used for an extended time may result to EPS
Extrapyramidal Symptoms
● Drug induced movement disorder
● Dystonia - continuous spasms and muscle contractions
● Akathisia - Motor restlessness, rocking feet, rubbing face
● Parkinsonism - rigidity
● Tardive dyskinesia - Irregular jerky movements, involuntary facial movements.
CNS effects
● Restlessness
● Weakness
● Agitation
● Hypotension
● Oral and IV - Administer 30-60 mins before chemo and 12 hrs after chemo
-Glucocorticoids (Corticosteroids)
● Suppress emesis associated with cancer chemo
● Minimized side effects because administered for a short while via IV
● Examples
○ Dexamethasone (Decadron)
○ Methylprednisolone (Solumedrol)
-Cannabinoids
● Active ingredients in marijuana
● Acts as agonists antiemetics via the activation of cannabinoid receptors in both the
brainstem and the enteric nervous system
● For alleviation of nausea and vomiting resulting from cancer treatment
● Prescribed for people in chemo
● Last resort of antiemetic = highly addictive
● Example: Dronabinol (Marinol) CSS III
○ Administer 24 hrs after chemo
○ Make sure the client is not suffering from any psychiatric disorder
● Side effects:
○ Mood changes
○ Euphoria
○ Drowsiness
○ Dizziness
○ Headaches
○ Depersonalization
○ Nightmares
○ Confusion
○ Incoordination
○ Memory lapse
○ Dry mouth
○ Tachycardia
○ Orthostatic hypo or hypertension
● Most common side effects are psychological problems hence assessment is very
important.
-Miscellaneous Antiemetics
● Do not act strictly as antihistamines, anticholinergics or phenothiazines
● MOA: suppress impulses to the CTZ and inhibiting impulses to the vestibular area
● Examples:
○ Diphenidol (Vontrol)
○ Trimethobenzamide (Tigan)
○ Aprepitant (Emend)
○ Metoclopramide HCl (Reglan)
Emetics
● MOA: Stimulate the CTZ in the medulla and acting directly in the gastric mucosa
● Many ways to induce vomiting like putting finger on the back of the throat
● We induce vomiting if clients have ingested dangerous substances
● Only applicable of aspired substance in non-corrosive = Add injury to the GI tract of
emetics are taken
○ Examples of corrosive substance
■ Ammonia
■ Chlorine bleach
■ Lay
■ Toilet cleaners
■ battery acid
-Ipecac syrup
● Should be taken within 60 minutes of poisoning
● Victim should be alert and conscious
● Not given to unconscious individual
● Keep away from patients reach
Antidiarrheals
● For diarrhea and decreasing hypermotility or increased peristalsis
● Should not be used for more than 2 days and if fever is present
>Loperamide (Imodium)
● Structurally related to diphenoxylate
● Causes less CNS depression than the 2 former
● Most common OTC antidiarrheals
● Reduces fecal volume, decreases intestinal fluid and electrolyte losses.
Nursing management
● Continuous monitoring of loose bowel movement
● Administer every after loose stool
-Laxatives
● Soft stool
● Help evacuation of formed fecal matter from the rectum
>Bulk-forming laxatives
● Natural, non absorbable
● MOA: Absorb water in the intestine, increases fecal matter size = distends GI tract
and stimulates peristalsis
● Examples:
○ Polycarbophil (FiberCon)
○ Polyethylene glycol (Miralax)
○ Methylcellulose (Citrucel)
○ Psyllium (Metamucil)
● Mix in a glass of water or juice and consume immediately and drink half to a full glass
of water
● Insufficient fluid intake will result to obstruction
● May take 8-24 hours to take effect
● May take 3 days for stool to be wet and well formed
=Lactulose (Duphalac)
● Commonly found in the area
● Decreases serum ammonia level
● Good clients with liver disease
● Contains glucose and fructose = diabetics should avoid
Note: Monitor serum electrolyte levels for patients taking osmotic laxatives = to avoid
electrolyte imbalance
They contain magnesium or sodium and a small amount is systematically absorbed.
=Castor oil
● Don't administer at bedtime
● Action is quick 2-6 hrs
● Not given in early pregnancy, may stimulate uterine contraction = spontaneous
abortion
=Senna (Senokot)
● Long term use injures the nerves of the colon = loss of intestinal muscular tone
● Side effect is reddish brown urine = secretion phenolphtaleine, senna or cascara
=Bisacodyl (Dulcolax)
● Most abused laxative OTC
● May cause electrolyte imbalance of calcium and potassium
● Absorption is minimal there are minimal side effects
Side effects
● Diarrhea
● Abdominal cramping
● Nausea
● Vomiting
● Weakness
Health teachings
● Proper use of laxatives
● Correct misconceptions of laxative use
-Cathartics
● Soft watery stool with cramping
● Help evacuation of unformed usually watery fecal material from the whole colon
Note: Both serve the same purpose despite different site of action
Antiulcers (TAAHPPP)
● Tranquilizers
● Anticholinergics
● Antacids
● Histamine 2 blockers
● Proton pump inhibitors
● Pepsin inhibitor
● Prostaglandin analogues
● Drugs to treat ulcers
● Tranquilizers and anticholinergics are used infrequently due to potential adverse
effects
>Tranquilizers
● MOA: Reduce vagal stimulation
● Vagus nerves - role in gastric secretions = aroused by taste, sight, odor of food =
cause release of ACh at vagus nerve endings in stomach wall = transmission of
impulses to acid secreting cells
● Examples
○ Chlordiazepoxide (Librium)
○ Clidinium bromide (Quarzan)
● Adverse effects
○ Edema
○ Ataxia
○ Confusion
○ EPS
○ Agranulocytosis
>Antacids
● MOA: Neutralize HCl and reduce pepsin activity
● Calcium carbonate
○ Most effective in neutralizing acid
○ Cause acid rebound
○ ½ of drug can be absorbed systemically
○ Excessive use might lead to Burnett’s syndrome
=Non-systemic antacids
● Compose of alkaline salts such as aluminum and magnesium, aluminum hydroxide,
magnesium hydroxide, magnesium trisilicate
● Magnesium hydroxide
○ Greater neutralizing power than aluminum hydroxide
○ Contraindicated to severe renal impairment = may lead to hypermagnesemia
● Aluminum
○ Small degree of absorption
○ Causes hypophosphatemia
>Histamine 2 blockers
● MOA: Block H2 receptors of parietal cells in stomach = reducing gastric acid
secretion and concentration
● Usually ends with -tidine
○ Cimetidine (tagamet)
○ Famotidine (Pepcid)
○ Nizatidine (Axid)
○ Ranitidine (Zantac)
=Cimetidine (Tagamet)
● 1st H2 blocker
● Short half life and duration of action
● Blocks 70% of acid secretion for 4 hrs.
● 50-80% is excreted unchanged in the urine
● Taken with antacid = ↓ effectiveness
=Nizatidine
● Relieves nocturnal gastric acid secretions for 12 hrs
● Block H2 receptor
● Best given before meals and at bedtime
● 1 hr interval with antacid = maintain efficacy
>Pepsin inhibitor
● Mucosal protective drug
● MOA: Covers the ulcer and protects it from acid and pepsin
● Does not neutralize or inhibit acid secretions
● Sucralfate (Carafate)
● Before meals and at bedtime