Amiodarone by Ayman

Advanced Pharmacology For Critical Care
(amiodarone)
Student : Ayman M Islaimi supervisor : Dr. Sana’ AL Aqqad
jun/2023
OUT LINE
• Introduction
• Pharmacokinetics
• Administration
• Dosing and Indications
• Adverse Reactions
• Contraindications
• Fatal toxicities
• Monitoring Parameters
• Protocols and follow up patient
Introduction
DEVELOPMENT OF AMIODARONE
Amiodarone emanated from the pharmacologic laboratory of Labaz
in Belgium in 1962.5 In the course of the systematic search for potent coronary
dilators, it was one of the many benzofuran derivatives that were synthesized with
the use of the benzofuran moiety present in khellin and its natural
congeners (all of which were coronary dilators
Introduction
Pharmacologic Category
Pharmacologic Category:
• Class III antiarrhythmic agent.
Mechanism of Action:
Inhibits adrenergic stimulation (alpha- and beta-blocking properties),
affects sodium, potassium, and calcium channels, prolongs the action
potential and refractory period in myocardial tissue; decreases AV
conduction and sinus node function
Pharmacokinetics
Absorption
• Bioavailability: Oral: Slow and variable 35-65%.
• Onset:
PO: Initial response 2 days to 3 wk, peak response takes 1 week to 5
months
IV: (electrophysiologic effects) within hours; Antiarrhythmic effects:
2 to 3 days to 1 to 3 weeks.
Peak effect: 1 week to 5 months
• Duration : Variable, 2 weeks to months
• Distribution
Protein bound: 96%
Vd: 66 L/kg
• Metabolism :Liver
• Elimination Half-life: (26-107 days)Not dialyzable by HD or PD.
• Excretion: Feces, and urine .
• Storage :Store at room temp, protect from light and excessive heat.
method of administration
• Amiodacore Injection should only be used when facilities exist for cardiac monitoring, defibrillation, and
cardiac pacing. Amiodacore Injection may be used prior to DC cardioversion
• The standard recommended dose is 5 mg/kg bodyweight given by intravenous On infusion over a period of
20 minutes to 2 hours.
• This should be administered as a dilute solution in 250 ml 5% dextrose.
• This may be followed by repeat infusion of up to 1200 mg (approximately 15 mg/kg bodyweight) in up to
500 ml 5% dextrose per 24 hours,
• the rate of infusion being adjusted on the the basis of clinical response
• In extreme clinical emergency the drug may, at the discretion of the clinician, the be given as a slow injection
of 150-300 mg in 10-20 ml 5% dextrose over a minimum of 3 minutes.This should not be repeated for at least
15 fu minutes.
• Patients treated in this way with Amiodacore Injection must be closely monitored, e.g., in an intensive care
unit
• After dilution in 5% dextrose solution, the diluted solution should be used Ve be immediately Change over
from intravenous to oral therapy As soon as an adequate response has been obtained,
• oral therapy should be initiated concomitantly at the usual loading dose (ie, 200 mg three times a day).
Amiodacore Injection should then be phased out gradually
Ventricular Arrhythmias
PO:
o Load: 800-1600 mg PO qDay for 1-3 weeks until response; once adequate
arrhythmia control achieved, reduce dose to 600-800 mg/day for 1 month
THEN reduce to maintenance dose(400 mg PO qDay)
IV
o 150 mg over first 10 min, followed by 360 mg over next 6 hr ,THEN 540
mg over remaining 18 hr, for a total of 1gm over 24 hr ,
o Duration of therapy: May continue to administer 0.5 mg/min for 2-3
weeks regardless of patient's age, renal function or ventricular function
Conversion to oral amiodarone after IV administration
<1 week IV infusion: 800-1600 mg/day
1-3 week IV infusion: 600-800 mg/day
>3 week IV infusion: 400 mg/day

Adverse Reactions
Increased AST or ALT levels CHF, Hypotension
Dizziness, Headache, Impaired Bradycardia or sinus arrest
memory SA node dysfunction, AV block
Malaise, Fatigue Hepatitis and cirrhosis
Abnormal gait/ataxia Visual disturbances
Involuntary movement Sleep Optic neuritis
disturbances
Hypo/hyperthyroidism
Constipation & Anorexia
Fatal toxicities:
Pulmonary toxicity:
Pneumonitis or interstitial/alveolar pneumonitis
Liver injury:
References
Common but usually mild and evidenced only by abnormal LFT
Overt liver disease can occur and has been fatal in a few cases
Proarrhythmic effect:
Like other antiarrhythmics, can exacerbate the arrhythmia
includes significant heart block or sinus bradycardia
Monitoring Parameters
BP, heart rate ECG, and rhythm throughout therapy.
 History and physical exam every 3 to 6 months: continue monitoring CXR every 3
to 6 months during therapy).
 LFTs (S&S of clinical liver injury, monitor serum electrolytes.
 Assess thyroid function tests before initiation of treatment and then periodically
thereafter (every 3 to 6 months).
Perform regular ophthalmic exams.

References
• Amiodarone: Historical development and pharmacologic profile
Author links open overlay panelBramah N. Singh M.D., D.Phil. a baDepartment of Cardiology, Wadsworth Veterans Administration Medical
Center, Los Angeles, Calif. USAbthe Department of Medicine, University of California at Los Angeles School of Medicine Los Angeles, Calif.
USA. Available online 3 February 2004.
• UpToDate. (n.d.). Evidence-Based Clinical Decision Support System| UpToDate | Wolters Kluwer. https://
www.uptodate.com/contents/amiodarone-adverse-effects-potential-toxicities-and-approach-to-monitoring?search=amiodarone&source=s
earch_result&selectedTitle=2~148&usage_type=default&display_rank=1
• Pacerone, Cordarone (amiodarone) dosing, indications, interactions, adverse effects, and more. (2021, September 17). Medscape Drugs
& Diseases - Comprehensive peer-reviewed medical condition, surgery, and clinical procedure articles with symptoms, diagnosis,
staging, treatment, drugs and medications, prognosis, follow-up, and pictures.
• Amiodarone. (2022). Reactions Weekly, 1908(1), 31-31. https://doi.org/10.1007/s40278-022-15759-5

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Advanced Pharmacology For Critical Care

Student : Ayman M Islaimi supervisor : Dr. Sana’ AL Aqqad

<1 week IV infusion: 800-1600 mg/day

1-3 week IV infusion: 600-800 mg/day

>3 week IV infusion: 400 mg/day

BP, heart rate ECG, and rhythm throughout therapy.

 LFTs (S&S of clinical liver injury, monitor serum electrolytes.

Perform regular ophthalmic exams.

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