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DRUG ACTION:
Pharmaceutic,
Pharmacokinetic &
Pharmacodynamic Phases
A. Pharmaceutic Phase
- is the first phase of drug action
The first phase of drug action
Drug becomes a solution so that it can be
absorbed
2 Pharmaceutic phases: Disintegration &
Dissolution
Disintegration is the breakdown of a
tablet/capsule into smaller particles
Dissolution is the dissolving of the smaller
particles in the GI fluid before absorption
- Drugs in liquid form are more rapidly
available for GI absorption than are solids
- Enteric-coated drugs resist disintegration in
the gastric acid of the stomach, so
disintegration does not occur until the drug
reaches the alkaline environment of the
small intestine (enteric-coated tablets or
capsules and sustained release capsules
should not be crush, crushing would alter
the place and time of absorption of the drug
B. Pharmacokinetic Phase
The of drug movement to achieve drug
action
The Process are: ABSORPTION, DISTRIBUTION,
METABOLISM (BIOTRANSFORMATION) &
EXCRETION
ABSORPTION
Is the movement of drug particles from the
GI tract to body fluids by passive
absorption, active absorption, or Pinocytosis
Most oral drugs are absorbed into the
surface area of the small instestine through
the action of extensive mucosal villi
Passive absorption occurs mostly by
diffusion (movement from higher
concentration to lower concentration)
Active absorption requires a carrier such
as enzyme or protein to move the drug
against a concentration agent (energy is
required for active absorption)
Pinocytosis is a process by which cells
carry a drug across their membrane by
engulfing the drug particles
FACTORS AFFECTING ABSORPTION
BLOOD FLOW poor circulation as a result
of shock, vasoconstrictor drugs, or disease
hampers absorption
Dosages
Remaining
(mg)
Percenta
ge Left
(%)
325
50
162
25
81
12.5
12
40
6.25
15
20
3.1
18
10
1.55
EXCRETION
Refers to the elimination of drugs from the
body
KIDNEY is the main route of drug
elimination
Other routes: hepatic metabolism, bile,
feces, lungs, saliva, sweat & breast milk
Protein-bound drugs cannot be filtered
through the kidneys, once the drug is
released from the protein, it is a free drug
and is eventually excreted in the urine
Factors affecting Excretion
Urine pH urine pH ranging from 4.5 to 8.
Acid urine promotes elimination of weak
base drugs and alkaline urine promotes
elimination of weak acid drugs (aspirin)
Kidney disease that results in decreased
glomerular filtration rate (GFR) or
decreased renal tubular secretion (drug
excretion is slowed or impaired)
A decreased in blood flow to the kidneys
can alter drug excretion
THERAPEUTIC INDEX
Therapeutic Index (TI) estimates the
margin of safety of a drug through the use
of a ratio that measures the effective
(therapeutic) dose and lethal dose
Important Terms:
LOADING DOSE a large initial dose to initiate
immediate drug response
SIDE EFFECTS are physiologic effects not
related to desired drug effects
ADVERSE REACTIONS are more severe than
side effects, undesirable effects of drugs that cause
mild to severe side effects
TOXIC EFFECTS or TOXICITY drug level
exceeds the therapeutic range resulting from
overdosing or drug accumulation
TOLERANCE refers to a decreased
responsiveness over the course of therapy
PLACEBO EFFECT is a psychologic benefit from
a compound that may not have the chemical
structure of a drug effect
DRUG-DRUG INTERACTION the effects of a
combination of drugs may be greater than, equal to,
or less than the effects of a single drug
FOOD-DRUG INTERACTION the effects of
selected foods may speed, delay or prevent
absorption of specific drugs
PRINCIPLES OF DRUG ADMINISTRATION
- Administration of medications is a basic
activity in nursing practice
- Nurses must be knowledgeable about the
specific drugs and their administration,
client response, drug interactions, client
allergies
- Nurses are accountable for the safe
administration of medications
- Nurses must know all the components of a
drug order and questions those orders that
are not complete, unclear, outside the
recommended range,
- Nurses are legally liable if they give a
prescribed drug and the dosage is incorrect
or the drug is contraindicated for the client
The Five-Plus-Five Rights of Drug
Administration
To provide safe drug administration, the
nurse should practice the Rights of drug
administration
1. RIGHT CLIENT
- Verify client by checking the identification
band
- Distinguish between two clients with the
same last name
Transdermal
Transdermal medication is stored in a patch
laced on the skin and absorbed through
skin, thereby having systemic effect
Transdermal patches should be rotated to
different sites and not reapplied over the
next exact same area when changed
The area should be thoroughly cleaned prior
to administration of a new transdermal
patch
Topical
Topical medication can be applied to the
skin with glove, tongue blade or cottontipped applicator
Use appropriate technique to remove the
medication from the container and apply it
to the clean, dry skin
Instillations
Administration of Eye Drops
Remove any discharge by gently wiping out
from inner canthus. Use separate cloth for
each eye
Gently draw the skin down below the
affected eye to expose the conjunctival sac
Administer the prescribed number of drops
into the center of the sac (not directly on the
cornea)
Gently press on the lacrimal duct with sterile
cotton ball or tissue for 1-2 min. after
instillation to prevent systemic absorption
Client should keep eyes closed for 1-2 min.
to promote absorption
Administration of Eardrops
Medication should be at room temperature
Client should sit up with head tilted slightly
toward the unaffected side
CHILD: pull down and back on auricle.
AFTER 3 YEARS OF AGE/ADULT: pull up
and back on auricle
Instill prescribed number of drops
Have client maintain position for 2-3 min
Administration of Nose Drops & Sprays
- Have the client blow the nose
Have the client tilt head back for drops to
reach frontal sinus and tilt head to affected
side to reach ethmoid sinus
Intramuscular
Systemic effect
Usually more rapid effect of drug than with
SQ
Sites: Ventrogluteal, Dorsogluteal, Deltoid
and Vastus Lateralis (pediatrics)
Equipment: 20-23 gauge, 18 g for blood
transfusion, 1-1.5 inches in length
Flatten the skin area using the thumb and
index finger and inject between them
Insert the needle at 90 degree angle
Ventrogluteal site volume of drug
administration is 1-3ml (slightly angle the
needle toward the iliac crest)
Dorsogluteal site - volume of drug
administration is 1-3ml, place the needle at
a 90 degree angle to the skin with the client
prone
Deltoid site - volume of drug administration
is 0.5 to 1ml, place the needle at a 90
degree angle to the skin or slightly toward
acromion
Vastus lateralis - volume of drug
administration is less than 0.5ml in infants, 1
ml in pediatrics, 1-1.5 ml in adults (direct the
needle at the knee at 45 to 60 degree angle
to the lateral middle thigh)
Z-Tract Injection technique
Prevents the medication from leaking back
into the subQ tissue
Used for medications that cause visible
permanent skin discolorations (e.g. iron
dextran)
Gluteal site is preferred
STEPS:
a. pull the skin to one side and hold
b. insert needle
c. Hold skin to side
d. inject medication
Intravenous
Systemic effect
More rapid than the IM or subQ routes
Site: accessible peripheral veins such as
cephalic vein of the arm, dorsal vein of
hand for direct IV
Acetylcholinesterase Inhibitors or
Cholinesterase Inhibitors
Prototypes:
- Neostigmine (Prostigmine) - first drug used
to manage MG, a short-acting
acetylcholinesterase inhibitor with a half-life
of 0.5 to 1 hour (given every 2-4 hours on
time to prevent muscle weakness)
- Pyridostigmine bromide (Mestinon) has an
intermediate action and given every 3-6
hours
- Edrophonium CL (Tensilon) for diagnosing
myasthenia gravis, ptosis should be absent
in 1-5 min. increase muscle strength for 520 min.
Mode of action: transmission of neuromuscular
impulses by preventing destruction of acetylcholine,
increasing muscle strength
Side effects/ Adverse reaction: GI disturbances
(nausea/vomiting, diarrhea, abdominal cramps),
increased salivation and tearing
Underdosing myasthenia crisis (muscle
weakness)
Overdosing cholinergic crisis (severe muscle
weakness, dyspnea)
Nursing interventions (Acetylcholinesterase
Inhibitors)
1. Monitor effectiveness of drug therapy
muscle strength should be increased
2. Observe client for signs and symptoms of
cholinergic crisis caused by overdosing i.e.
severe muscle weakness, increased
salivation, sweating, tearing
3. Have readily available antidote for
cholinergic crisis (atropine sulfate)
4. All doses of AChE inhibitors should be
administered ON TIME, because late
administration of the drug could result in
muscle weakness
SKELETAL MUSCLE RELAXANTS
Prototype:
Muscle Relaxants
1. Baclofen (Lioresal) for muscle spasms
caused by multiple sclerosis and spinal cord
injury, overdose can cause CNS
depression, drowsiness, dizziness,
hypertension
2. Dantrolene sodium (Dantrium) for chronic
neurologic disorders causing spasm i.e.
SCI, stroke, avoid taking with alcohol and
CNS depression
3. Pancronium bromide (Pavulon) used in
surgery for relaxation of skeletal muscle
4. Succinylcholine CL (Anectine) used in
surgery with anesthesia for skeletal muscle
relaxation
Side effects/Adverse Reactions:
Nausea, vomiting, dizziness, weakness, insomnia,
tachycardia, hypotension
Nursing Interventions (Muscle relaxants)
1. Monitor and report elevated liver enzymes
2. Observe for CNS side effects i.e. dizziness
3. Instruct client not to abruptly stop taking
muscle relaxant to avoid rebound spasms
4. Advise client not to drive or operate
dangerous machinery because of sedative
effect of drug i.e. drowsiness
5. Teach client to avoid alcohol and CNS
depressants
6. Contraindicated for pregnant mothers
ANTIDYSRHYTHMIC DRUGS
Cardiac Dysrhythmias (arrhythmia)
Defined as any deviation from the normal
rate or pattern of the heartbeat, includes
heart rates that are too slow (bradycardia),
too fast (tachycardia) or irregular.
The terms dysrhythmia (disturbed heart
rhythm) and arrhythmia (absence of heart
rhythm) are used interchangeably
Frequently follow an MI or can result from
hypoxia, hypercapnia (increased CO2 in the
blood), coronary artery disease, excess
cathecolamines or electrolyte imbalance
LAXATIVES
Types
A. Stool Softeners or Surfactant Laxatives
Mildest form of cathartic
Detergent action lowers surface
tension, allowing water and fats to
enter and soften stool
Used especially for clients who
should avoid straining
Prototype:
Docusate sodium (Colace)
Docusate calcium (Surfak)
Docusate with casanthranol (Peri-Colace) is
a stool softener combined with a stimulant
Adverse effects: Diarrhea and mild cramps
ANTIDIARRHEALS
Inhibit peristaltic activity by direct action on
intestinal muscles
Inhibit receptors responsible for peristalsis
Prototype:
Kaolin and pectin (Kaopectate)
Loperamide (Immodium)
Diphenoxylate hydrochloride with atropine
sulfate (Lomotil)
Paregoric (camphorated opium tincture)
Bismuth subsalicylate (Pepto-Bismol)
Adverse effects:
Nausea, vomiting, anorexia, abdominal
cramping, diarrhea, mild cramps
Headache, dizziness, drowsiness
Pruritus, rash
EMETICS
Active ingredient is emetine which
stimulates the vomiting reflex located in the
medulla by stimulating the chemoreceptor
trigger zone and irritating gastric mucosa
1. Syrup of Ipecac
used for accidental poisoning
Currently being abused by clients
with bulimia nervosa
Fatal dose is 10-25 mg
Emetine is secreted slowly so a daily
dose of 30 ml is toxic and fatal after
several months
Recommended dose
Children < 1 yr: 5-10 ml followed by to 1
glass of water
Children over 1 year old: 15 ml followed by
1-2 glasses of water
2. Activated Charcoal
Binds and inactivates the poison
until excreted
Recommended to give as soon as
possible after ingestion of poisoning
but not within 1-2 hours of syrup of
ipecac
Given as a powder prepared in an
aqueous slurry to absorb the poison
Recommended dose
Children: not more than 1 dose
Adults: 30-100 mg
Adverse effect
Black tarry stools, diarrhea, constipation
Contraindications & precautions
Unconscious client
Pregnancy
Lactation
Poisoning from caustic substances such as
cyanide
Nursing interventions
Avoid giving within 1-2 hours after ingestion
of syrup of ipecac
Assess vital signs before administration
May give with a laxative to promote
elimination
INSULIN, ANTIDIABETIC AGENTS &
GLUCAGON
Insulin is produced by the beta cells in the
Islets of Langerhans in the pancreas
Key role in the metabolism of CHO, CHOO,
CHON
Glucagon is secreted by the alpha cells
from the Islets of Langerhans in the
pancreas and stimulates hepatic production
of glucose from glycogen stores
MOA of Insulin:
Stimulates the active transport of glucose
into muscle and adipose tissue cells
Regulates the rate at which carbohydrates
are burned by the cells for energy
Promotes the conversion of glucose to
glycogen for storage in the liver
Promotes the conversion of fatty acids into
fat which can be stored as adipose tissue
Promotes conversion of amino acids to
proteins in muscle
Promotes intracellular shifts of K and Mg
Indications
Hormone replacement in the treatment of
DM type 1 and are unable to produce insulin
Antidiabetic agents are used in the
treatment of DM type 2 and who produce an
insufficient amount of insulin
Glucagon, a hyperglycemic agent, is used in
the acute management of severe
hypoglycemia when administration of
glucose is not feasible
Adverse reactions of insulin
Hypoglycemia
Coma
Lipoatrophy and lipohypertrophy of the
injection site
Local allergic reaction at the injection site
Insulin resistance
Allergic reaction
Nursing interventions
Monitor blood glucose frequently when
therapy is initiated and routinely when
stabilized
Monitor for hypoglycemia at peak time of
insulin e.g. apprehension, chills,
perspiration, confusion, double vision,
drowsiness, inability to concentrate,
shakiness, nausea, rapid pulse
Monitor for hyperglycemia e.g. flushed skin,
acetone breath (fruity), polyuria, polydipsia
and anorexia
Monitor weight at frequent intervals
Use only insulin syringes which are
calibrated in units
Before withdrawing the insulin, rotate the
vial between the palms of the hands to
ensure the medication is mixed into the
solution. Do not shake the vial.
When mixing two insulins, draw up the
regular insulin first. This prevents
contamination of the regular insulin.
Insulin should be kept in a cool place and
does not need refrigeration. Opened vials
should not be used after 30 days