Deferasirox - Revision history

ClaireLewis: /* References */

2019-09-20T23:51:36Z

References

← Older revision		Revision as of 23:51, 20 September 2019
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	[[Category:Pharmacology]]		[[Category:Pharmacology]]
			[[Category:Toxicology]]

Mholtz: Text replacement - "qd" to "QD"

2017-07-07T10:55:13Z

Text replacement - "qd" to "QD"

← Older revision		Revision as of 10:55, 7 July 2017
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	==Adult Dosing==		==Adult Dosing==
	===[[Iron toxicity]], chronic transfusional===		===[[Iron toxicity]], chronic transfusional===
	*20-30 mg/kg PO qd		*20-30 mg/kg PO QD
	**Start: 20 mg/kg PO qd		**Start: 20 mg/kg PO QD
	**Max: 40 mg/kg/day		**Max: 40 mg/kg/day
	**Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin		**Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
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	**Hold: Ferritin <500 mcg/L		**Hold: Ferritin <500 mcg/L
	===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===		===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===
	*10-20 mg/kg PO qd		*10-20 mg/kg PO QD
	**Start: 10 mg/kg PO qd		**Start: 10 mg/kg PO QD
	**Max: 20 mg/kg/day		**Max: 20 mg/kg/day
	**Decrease dose 50% if Cr >33% above baseline x2 weeks		**Decrease dose 50% if Cr >33% above baseline x2 weeks
Line 24:		Line 24:
	===[[Iron toxicity]], chronic transfusional===		===[[Iron toxicity]], chronic transfusional===
	*2-15 yo		*2-15 yo
	**20-30 mg/kg PO qd		**20-30 mg/kg PO QD
	***Start: 20 mg/kg PO qd		***Start: 20 mg/kg PO QD
	***Max: 40 mg/kg/day		***Max: 40 mg/kg/day
	***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin		***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
	***Decrease dose 10 mg/kg/day if Cr >33% above baseline and >ULN		***Decrease dose 10 mg/kg/day if Cr >33% above baseline and >ULN
	*16+ yo		*16+ yo
	**20-30 mg/kg PO qd		**20-30 mg/kg PO QD
	***Start: 20 mg/kg PO qd		***Start: 20 mg/kg PO QD
	***Max: 40 mg/kg/day		***Max: 40 mg/kg/day
	***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin		***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
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	===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===		===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===
	*10-15 yo		*10-15 yo
	**10-20 mg/kg PO qd		**10-20 mg/kg PO QD
	***Start: 10 mg/kg PO qd		***Start: 10 mg/kg PO QD
	***Max: 20 mg/kg/day		***Max: 20 mg/kg/day
	***Adjust dose based on serum ferritin trends and liver iron concentration		***Adjust dose based on serum ferritin trends and liver iron concentration
	***Decrease dose 5 mg/kg/day if Cr >33% above baseline and >ULN		***Decrease dose 5 mg/kg/day if Cr >33% above baseline and >ULN
	*16+ yo		*16+ yo
	**10-20 mg/kg PO qd		**10-20 mg/kg PO QD
	***Start: 10 mg/kg PO qd		***Start: 10 mg/kg PO QD
	***Max: 20 mg/kg/day		***Max: 20 mg/kg/day
	***Adjust dose based on serum ferritin trends and liver iron concentration		***Adjust dose based on serum ferritin trends and liver iron concentration

Jonwarren: Creation of page

2017-02-15T03:40:04Z

Creation of page

New page

==Administration==
*Type: [[Antidote]]
*Dosage Forms: 125, 250, 500 mg disperse tab
*Routes of Administration: Oral
*Common Trade Names: Exjade

==Adult Dosing==
===[[Iron toxicity]], chronic transfusional===
*20-30 mg/kg PO qd
**Start: 20 mg/kg PO qd
**Max: 40 mg/kg/day
**Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
**Decrease dose 10 mg/kg/day if Cr >33% above baseline x2 weeks
**Hold: Ferritin <500 mcg/L
===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===
*10-20 mg/kg PO qd
**Start: 10 mg/kg PO qd
**Max: 20 mg/kg/day
**Decrease dose 50% if Cr >33% above baseline x2 weeks
***Interrupt treatment if already at 5 mg/kg/day
**Hold: Ferritin <300 mcg/L or liver iron <3 mg Fe/g

==Pediatric Dosing==
===[[Iron toxicity]], chronic transfusional===
*2-15 yo
**20-30 mg/kg PO qd
***Start: 20 mg/kg PO qd
***Max: 40 mg/kg/day
***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
***Decrease dose 10 mg/kg/day if Cr >33% above baseline and >ULN
*16+ yo
**20-30 mg/kg PO qd
***Start: 20 mg/kg PO qd
***Max: 40 mg/kg/day
***Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
***Decrease dose 10 mg/kg/day if Cr >33% above baseline x2 weeks
===[[Iron toxicity]], chronic non-transfusion-dependent [[thalassemia]]-assoc.===
*10-15 yo
**10-20 mg/kg PO qd
***Start: 10 mg/kg PO qd
***Max: 20 mg/kg/day
***Adjust dose based on serum ferritin trends and liver iron concentration
***Decrease dose 5 mg/kg/day if Cr >33% above baseline and >ULN
*16+ yo
**10-20 mg/kg PO qd
***Start: 10 mg/kg PO qd
***Max: 20 mg/kg/day
***Adjust dose based on serum ferritin trends and liver iron concentration
***Decrease dose 50% if Cr >33% above baseline x2 weeks
****Interrupt treatment if already at 5 mg/kg/day

==Special Populations==
*[[Drug pregnancy categories|Pregnancy Rating]]: C; Caution during pregnancy
*Lactation risk: L3; Safety unknown

===Renal Dosing===
*Adult:
**CrCl 40-60: Decrease start dose 50%
**Cr >2x ULN or CrCL <40: Contraindicated
*Pediatric:
**CrCl 40-60: Decrease start dose 50%
**Cr >2x ULN or CrCL <40: Contraindicated
===Hepatic Dosing===
*Adult:
**Child-Pugh Class B: Decrease start dose 50%
**Child-Pugh Class C: Avoid use
*Pediatric:
**Child-Pugh Class B: Decrease start dose 50%
**Child-Pugh Class C: Avoid use
==Contraindications==
*Allergy to class/drug
*Cr >2x ULN or CrCl <40
*Poor performance status
*High risk [[myelodysplastic syndrome]]
*Advanced malignancy
*[[Thrombocytopenia]] <50,000
*Hepatic impairment, Child-Pugh Class C
*Caution if hepatic impairment, Child-Pugh Class A or B
*Caution if renal impairment
*Caution if concurrent nephrotoxic agent
*Caution if hematologic disorder
*Caution in patients >55yo

==Adverse Reactions==
===Serious===
*Nephrotoxicity
*Hepatotoxicity
*GI hemorrhage
*GI perforation
*GI ulcer
*[[Agranulocytosis]]
*[[Neutropenia]]
*[[Thrombocytopenia]]
*[[Anemia]] exacerbation
*[[Hearing loss]]
*Cataracts
*Lens opacification
*Retinal disorders
*Hypersensitivity reaction
*[[Anaphylaxis]]
*[[SJS]]
*Erythema multiforme
*Leukocytoclastic vasculitis
===Common===
*Cr elevated
*[[Abdominal pain]]
*[[Proteinuria]], intermittent
*[[Diarrhea]]
*[[Nausea]]/[[Vomiting]]
*[[Rash]]
*ALT elevated
*IOP elevated

==Pharmacology==
*Half-life: 8-16h
*Metabolism: Liver; CYP450: minimal (8%); UGT: 1A1 (primary), 1A3 substrate
*Excretion: Feces 84%, Urine 8%

==Mechanism of Action==
*Chelates iron, promoting fecal iron excretion

==Comments==
*Black Box Warning
**Risk for renal failure in pts with comorbidities or advanced hematological disorder
**Risk for hepatic failure in pts with Child-Pugh Class A, B, C disease
**Risk for gastrointestinal Hemorrhage in elderly pts with advanced hematologic malignancies or low platelets

==See Also==
*[[Iron toxicity]]

==References==
<references/>

[[Category:Pharmacology]]