THERAPEUTIC DRUG MONITORING

1. GUIDE:
SRAVAN SIR
PRESENTED BY:
K.PRIYA DARSHINI
PHARMD
Y12PHD0415
HINDU COLLEGE OF
PHARMACY,AMARAVATHI ROAD,GUNTUR

2. INTRODUCTION
 Amiodarone isaniodinatedBenzofuran.
 StructurallysimilartoTHYROXINEand PROCAINAMIDE.
 Itisa class-3antiarrhythmicdrugs
 It was used initally as a treatment for angina pectoris.–
coronary vasodilation.
 Used for the prevention and treatment of serious atrial and
ventricular arrhythmias

3. MECHANISM OF ACTION
 Increases the refractory period in all cardiac tissues
 Decreases automaticity of fibres in the Purkinje
system
 Prolongs AV conduction
 Can block potassium, sodium and calcium channels
and β receptors

4. BRAND NAMES:
 CORDARONE
 PACERONE

5. PHARMACOKINETIC PARAMETERS:
 Highly lipid soluble compound.
 DESETHYL AMIODARONE is the active metabolite.
ON ORAL ADMINISTRATION
 Slowly absorbed
 Bioavailability: 20-55%
 Large volume of distribution: 0.9-148L/Kg
 Protein binding: <96%
 Half life: 58days

6. ON INTRAVENOUS
ADMINISTRATION
 100% bioavailability
 Large volume of distribution
 Variable t½ ranging from 4.8hr to 68.2hrs

7. INDICATIONS
 It is primarily indicated for atrial fibrillations and
flutter.
 Effective in maintaining sinus rhythm.
 Not useful as prophylactic in Pt. with risk of sudden
cardiac death after MI.
 It is indicated when other treatments are ineffective
or have not been tolerated esp. in recurrent life
threatening venticular arrhythmias.

8. DOSAGE AND ADMINSTRATION
 Loading dosage varies from 600 to 1400 mg/day for 2
to 21 days.
 Usual maintenance dose varies from 200 to 600
mg/day
 Plasma concentrations of AMIDARONE are usually
b/w 1 to 2mcg/ml during effective therapy.
 Levels of drug >3-4mcg/ml, for prolonged periods
of time are associated with adverse effects.

9. ADVERSE DRUG REACTION:
Dizziness
Bitter taste
Headache
Flushing
Nausea and Vomiting
Constipation
Ataxia
Weight loss
Tremor
Photosensitivity
Blue-grey skin discolouration
Pulmonary fibrosis and pneumonitis
Cough, fever
Allergic reaction
Blurred vision

10. DRUG INTERACTIONS
 Amiodarone increases the plasma concentration of
digoxin
 Amiodarone can result in increased plasma
concentration of Phenytoin
 Amiodarone increase anticoagulant effect by
inhibiting metabolism of Warfarin.

11. ASSAY PROCEDURE:
 HIGH PERFORMANCE LIQUID CHROMATOGRAPHY:
PRINCIPLE:
The separation of a substance depend on the
relative distribution of mixture constituents between
2 phases, a mobile phase and a stationary phase.
VOLUME USED: 0.5 -1 mL.
ADVANTAGES: Speed,efficacy, accuracy.
DISADVANTAGES: Costly, complex.

12. CONCLUSION:
 Use with caution in patients with heart failure and
liver or thyroid function impairment
 Avoid in patients with second or third degree AV block
and bradycardia