Rosiglitazone

AVANDIA

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Pronunciation: roe-si-GLI-ta-zoen (a-VAN-dee-a)

Rosiglitazone ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Rosiglitazone ballicule

Rosiglitazone AVANDIA mascot mnemonic cartoon — Visual mnemonic: Rosiglitazone mascot
**“A van of Rosey glitter zone”**

What it isPPAR-gamma insulin sensitizer; type 2 diabetes.

Why this oneIts legacy is the myocardial-infarction safety signal that sharply curtailed use even after restrictions were eased.

What limits itAvoid in symptomatic heart failure; edema, weight gain, and fractures limit use, and pioglitazone is usually preferred.

Rosiglitazone molecular structure (skeletal formula) — Molecular structure: Rosiglitazone

FDA-approved for

type 2 diabetes (1999)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING CHF: TZDs cause/exacerbate heart failure — monitor after initiation/dose increase; initiation contraindicated in NYHA III/IV HF. Myocardial ischemia: 42-trial meta-analysis showed increased MI/angina risk; overall data inconclusive

FDA dosing	Population	Start	Target	Max
Type 2 diabetes mellitus (monotherapy or with metformin, sulfonylurea, or both)	adult	4 mg QD or 2 mg BID	4-8 mg/day (QD or divided BID); 4 mg BID gave greatest FPG/HbA1c reduction	8 mg/day

Titration May increase to 8 mg/day after 8-12 weeks if inadequate FPG response

Renal No adjustment as monotherapy; combination with metformin contraindicated in renal impairment

Hepatic Do not initiate with clinical evidence of active liver disease or ALT >2.5x ULN; check LFTs before starting and periodically

Pediatric data insufficient to recommend use

Instructions

May take with or without food
Start at lowest recommended dose; monitor for fluid retention with any dose increase
If hypoglycemia on combination therapy, reduce the sulfonylurea dose

Available strengths

tab 2, 4, 8 mg

Contraindications

Initiation in established NYHA Class III or IV heart failure

Cautions

Fluid retention and CHF (boxed) — observe for weight gain, dyspnea, edema; not recommended with symptomatic heart failure
Increased cardiovascular events in NYHA I/II CHF patients
Myocardial ischemia (boxed) — risk greater when added to insulin or with nitrates; initiation not recommended during acute coronary events
Hepatic: measure liver enzymes before initiation and periodically; do not start if ALT >2.5x ULN
Dose-related edema and anemia
Hypoglycemia when combined with sulfonylurea or insulin
Increased fractures in women (upper arm, hand, foot; ADOPT trial)

Adverse reactions

Upper respiratory tract infection
Headache
Back pain
Hyperglycemia
Fatigue
Sinusitis
Edema
Anemia
Hypoglycemia (combination therapy)
Fractures in women

Pregnancy Category C; crosses human placenta; should not be used during pregnancy — most experts recommend insulin monotherapy

Lactation Unknown if excreted in human milk (detected in rat milk); should not be administered to a nursing woman

Cost

Rosiglitazone (AVANDIA)

Strength		#/mo	CostPlus
2 mg	tab	30 qd	not offered
4 mg	tab	30 qd	not offered
8 mg	tab	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Rosiglitazone is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

⚠ BOXED WARNING

Congestive heart failure

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Weight-gain liability2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityFluid retention, heart failure and weight gain

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Memory aids: interaction avatars

CYP2C8 substrate

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