Cardiotropics

Digoxin
 Half-life 38 hours average size adult
 PEAK ASSESMENT : Conducted after 8 hours
 Digoxin is excreted as digoxigenin in the urine
 Measurement pf Digoxin by immunoassay
o Cardiac effects: Premature ventricular contraction (PVC)
Atrio-ventricular node blockage

o Toxic effects : Nausea, Vomiting, Visual Distrubances

Lidocaine
 Action : Correct ventricular arrhythmia
Prevent ventricular fibrillation
Treat Acute myocardial infarction
 Acid glycoprotein and is metabolized in the liver, producing active metabolites,
monoethylglycinexylidide and glycinexylide
 Serum Concentration
o Therapeutic range: 1.5 – 4ug/ml
o Toxic Range:
 4-8ug: Central nervous system depression, seizures,
 >8ug: Severe decrease in BP and Cardiac output
 The toxic effect are due to the parent drug and the additive
Monoethylglycinexylidide(MEGX)
 Measurement is through chromatography and immunoassay

Quinidine
 PREPARATION: Quinidine sulfate, Quinidine gluconate
 Naturally occurring drug that treat cardiac arrhythmia
 Is a myocardial depressant that decreases the hearts ability to _____ ( di ko mabasa)

Note: If Quinidine is added to a digoxin therapy regime, an ________( di ko mabasa) an increase

in digoxin concentration

 Serum concentration
o Therapeutic Range: 2-5 ng/ml
o Toxic range Range:
 >5ng/Ml : Nausea, Vomitting, abdominal discomfort, Toxicity
o Peak assessment:
 Quinidine Sulfate : After 2 hours
 Quinidine Gluconate : After 4-5 hours
o Measurement is through chromatography and immunoassay

Procainamide
 Is used to treat inappropriate ventricular contractions and tachycardia.
 This drug is metabolized in the liver to form an active metabolite,
 N-acetylprocainamide, which produces the same effect as its parent drug. Therefore, serum
levels of both drugs must be analysed
Disopyramide
 Stabilizes the heartbeat
 Is both excreted by the renal system as the unchanged drug, metabolized in the liver to form
an inactive metabolite
 _____ for quinidine

Propanolol
 Prescribe for atrial and ventricular arrhythmias and hypertension
 It is considered to be a beta-blocker

THERAPEUTIC DRUG MONITORING

1.2 ANTIBIOTICS
 Antimicrobial drugs must be selectively toxic to infectious microorganism without causing
excessive damage to human cells

Aminoglycosides
 Used to treat infections caused by gram-negative bacteria;
 Include gentamicin, tobramycin, kanamycin, and amikacin
 The aminoglycosides are administered IV or IM because gastrointestinal absorption is poor
 Elimination is via kidney filtration
 Measurement: Chromatography and Immunoassay
 Associated with NEPHROTOXICITY AND OTOTOXICITY
o NEPHROTOXICITY
 Impairs proximal tubule function
 Electrolyte imbalance, proteinuria
 High levels of exposure – KIDNEY Necrosis and Failure
o OTOTOXICITY
 Disrupts the inner cochlea of the ear and vestibular membranes, hearing
and balance impairment

Vancomycin
 Used to treat infections caused by gram-positive bacteria
 Administered by IV because of poor gastrointestinal absorption.
 Measurement: Chromatography and Immunoassay
 May be measured with nephrotoxicity, ototoxicity, and “red man syndrome” (erythemic
flushing of extremities)

1.3 ANTI-EPILEPTIC DRUG

 Function to alter transmission of nerve impulses within the brain to minimize the seizures of
epilepsy.
 Epilepsy, convulsions and seizures are prevalent neurologic disorders
 These drugs are used as prophylactics, therapeutic ranges are considered guidelines
 Most AEDs are analysed by immunoassay or chromatography and measure the free or
bound drug in a serum or plasma sample. Collected at the end of the dosing internal
 First-Generation Antiepileptic drug
o Phenobarbital
o Phenytoin ( Dilantin)
o Valproic Acid (Depakene)
o Carbamazepine (Tegretol)
o Ethosuximide (Zarontin)

 Second-generation antiepileptic drugs

o Gabapentin (Neurontin)
o Felbamate
o Levetiracetam
o Oxarbazpine
o Lamotrigine
o Tiagabine
o Topiramate
o Zonisamide

 Seizures may be classified as:

o Partial seizures:
 Simple Partial, Complex Partial, Partial Becoming Generalized
o Generalized Seizures
 Absence (Petit Mal) Myoclonic
 Clonic seizure Tonic seizure
 Tonic-clonic (Grand Mal) atonic

Note: Seizures are usually self-limiting

A. Myoclonic seizures or twitches

 Are brief contractions, or relaxations, of a muscle or muscle group, resulting in a
sudden, jumpy movement
B. Clonic seizure
 The individual’s muscle begin to spasm and jerk.
C. Tonic seizure
 During a tonic seizure, the person’s muscles initially stiffen and they lose
consciousness
 The person’s eyes roll back into their head as the muscles ( including those in
the chest, arms and legs) contract and the back arches
D. Tonic-clonic (Grand Mal) Seizure
 It is a rare to experience on without the other
 When both are experienced at the same time, this is known as a tonic-clonic
seizure (formerly known as a grand mal seizure).
E. Atonic Seizures ( also called Drop Seizure, Akinetic Seizure, or Drop Attacks0
 Are a type of seizure that consist of a brief lapse in muscle tone that are caused
by temporary alterations in brain function. The seizures are brief –usually less
than fifteen seconds.
Phenobarbital
 A hydantoin-derivative anticonvulsant.
 A long-acting barbiturate that control Grand mal or clonic seizure and focal epileptic; not
used for petit mal seizure
 It is used for treating withdrawal symptoms in infants - mothers are addicted to opiates
 It is used to treat cases of Congenital Hyperbilirubinemia – drug enhances bilirubin
metabolism
 Absorption is slow but complete; 50% Protein Bound

 Marjority is store in the brain

 Renal impairment slows down elimination process.
 Elimination: Hapatic metabolism
 Inactive Proform: Primidone (Mysoline)
Half-life: 70-100 hours
 Peak serum level: 10 hours after oral dose
 Therapeutic level: 20-40 ug/ml(Phenobarbital)
5-12 ug/ml (Primidone)
 Toxic effect Nystagmus, Stupor, Ataxia, Respiratory depression

Phenytoin (Dilantin)
 It controls seizures ( Tonic-Clonic, Simple Partial Seizuer); a short term prophylactic agent in
brain injury
 It is not used for petit mal and atomic seizures
 Administer INTRAVENOUSLY
 MUECTABLE PROFORM: FOSPHENYTOIN
 Decreased Na+ and Ca+ influx into hyperexcitable neuron.
 87-97% protein Bound

 Therapeutic range: 10-20 ug/ml (free form)

 Major Toxicity: Initiation of seizures
Teratogenic action (Cleft lip, palate)
Andnystagmus
 Toxic Level: >20 ug/ml