S ANGAL ANG, RONAL D J OHN A.

THERAPEUTIC DRUG
MONITORING
involves the analysis, assessment, and evaluation of
circulating concentrations of drugs in serum,
plasma, or whole blood
The purpose of these actions is to ensure that a
given drug dosage produces maximal therapeutic
benefit and minimal toxic adverse effects.
ROUTES OF ADMINISTRATION
For a drug to express a therapeutic benefit, it must
be at the appropriate concentration at its site of
action.

Oral
Intravenous
Intramuscular
Subcutaneous
inhalation

Suppository
transcutaneous
PHARMACOKINETIC PROCESSES
L.A.D.M.E
Liberation
Absorption
Distribution
Metabolism
Excretion

LIBERATION
first step in the process by which medication
enters the body and liberates the active
ingredient that has been administered
It is the release of the drug
Applies to a drug given orally

ABSORPTION
The rate at which a drug leaves its site of
administration, and the extent to which absorption
occurs.
Bioavailability- is the fraction of the dose that
reaches the blood
First pass effect- Metabolism of drug by liver before
drug reaches systemic circulation.

DISRIBUTION
The transport of a drug in the body by the
bloodstream to its site of action
METABOLISM
The biologic transformation of a drug into
an inactive metabolite, a more soluble compound,
or a more potent metabolite
Refers to chemical changes that take place in the
drug following administration
EXCRETION
Process by which the drug and its metabolites are
excreted from the body
The rate at which a particular drug is cleared from
the circulation is dependent not only on the type of
drug itself, but also on patients capacity to
metabolize and excrete it.

Excreted mainly through urine and some are
through feces, sweat, saliva.
A. CARDIOACTIVE DRUGS
Class I
(Rapid sodium
channel
blockers)
Class II
(Beta receptor
blockers)
Class III
(Potassium
channel
blockers)
Class IV
(Calcium
channel
blockers)
Quinidine
Disopyramide
Lidocaine
Proicanamide

Propranolol Amiodarone Verapamil
Cardiac glycoside
Digoxin
SODIUM CHANNEL BLOCKERS ARE DRUGS WHICH
IMPAIR CONDUCTION OF SODIUM IONS (NA+) THROUGH
SODIUM CHANNELS. USED IN THE TREATMENT
OF CARDIAC ARRHYTHMIA



Class I
(Rapid sodium channel blockers)

Quinidine
Proicanamide
Lidocaine
Disopyramide

QUINIDINE
A naturally occuring drug for treatment of
arrhythmia.
Orally administrated
Therapeutic range: 2.5-5 g/ml
Toxic range: >5 g/ml

Toxic effects: nausea, vomiting, abdominal
discomfort

DISOPYRAMIDE
Substitute for quinidine and is used to treat cardiac
arrhythmias.
Orally administered
Therapeutic range: 3-5 g/ml
Toxic range: 10 g/ml

Toxic effects: bradycardia and atrioventricular
blockage

PROICANAMIDE
Used to treat cardiac arrhythmia
GIT absorption is rapid and complete
N-acetyl proicanamide(NAPA) is the hepatic
metabolite
Peak serum level occurs one hour after the dose

Toxic effects: reversible lupus like syndrome, nephrotic
syndrome
LIDOCAINE
Used to correct ventricular arrhythmia and to
prevent ventricular fibrilation after myocardial
infarction.
Administered through IV infusion.
Primary product of hepatic metabolism:
monoethylglycineexylidide (MEGX)
Therapeutic range: 1.5-4.0 g/ml
Toxic range: >4.0 g/ml

Toxic effects: seizure, low bp
BETA BLOCKERS ARE KNOWN PRIMARILY FOR THEIR
REDUCTIVE EFFECT ON HEART RATE.
Class II
(Beta receptor blockers)

Propranolol

PROPRANOLOL
Used in the treatment of angina pectoris,
hypertension, coronary artery disease.

Toxic effects: bradycardia, arterial insufficiency,
pharyngitis

POTASSIUM CHANNEL BLOCKERS ARE
AGENTS WHICH INTERFERE WITH CONDUCTION
THROUGH POTASSIUM CHANNELS.
Class III
(Potassium channel blockers)

Amiodarone
AMIODARONE
Blocks potassium channels in the cardiac muscle
and is used for the treatment of ventricular
arrhythmias.
An iodine containing drug which can cause
hyperthyroidism or hypothyroidism
Therapeutic range: 1.0-2.5 g/ml

Toxic effects: bradycardia
DISRUPTS THE MOVEMENT OF CALCIUM(CA
2+
)
THROUGH CALCIUM CHANNELS AND ARE USED AS
ANTI-HYPERTENSIVE DRUGS.
Class IV
(Calcium channel blockers)

Verapamil
VERAPAMIL
For treatment of angina, hypertension and
supraventricular arrhythmias.
Therapeutic range: 80-400 g/ml

Toxic effects: hypotension
CARDIAC GLYCOSIDES ARE A CLASS OF MEDICATIONS
USED TO TREAT HEART FAILURE AND CERTAIN IRREGULAR
HEART BEATS
Cardiac glycoside

Digoxin
DIGOXIN
Used for treatment of congestive heart failure
Peak serum level is 8 hours after an oral dose
Toxic level: >2 g/ml

Toxic effects: nausea, vomiting, visual disturbances
B. ANTIBIOTICS
Aminoglycosides
Vancomycin

AMINOGLYCOSIDES
Used for treatment of gram(-) bacterial infections
Intravenously or intramuscularly administered
Eliminated by renal filtration
May damage the 8
th
cranial nerve at toxic levels

(gentamicin, tobramycin, amikacin, kanamycin,
neomycin, streptomycin)
VANCOMYCIN
Effective against gram(+) cocci and bacilli
Administered through IV infusion
Eliminated by renal filtration
Toxic side effects may occur in the therapeutic
range of 5-10 g/ml

REFERENCES:

Clinical Chemistry: Principles, Techniques, and
Correlations 6
th
ed. by Michael L. Bishop
Henry's Clinical Diagnosis and Management by
Laboratory Methods 22
nd
ed., Mcpherson