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GUIDE:
SRAVAN SIR
PRESENTED BY:
K.PRIYA DARSHINI
PHARMD
Y12PHD0415
HINDU COLLEGE OF
PHARMACY,AMARAVATHI ROAD,GUNTUR
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
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
BRAND NAMES:
 CORDARONE
 PACERONE
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
ON INTRAVENOUS
ADMINISTRATION
 100% bioavailability
 Large volume of distribution
 Variable t½ ranging from 4.8hr to 68.2hrs
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.
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.
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
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.
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.
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
TDM of amiodarone BY Dr.PRIYA

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TDM of amiodarone BY Dr.PRIYA

  • 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
  • 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