Dosing & Uses
Dosage Forms & Strengths
tablet
- 2mg
- 4mg
Type 2 Diabetes Mellitus
Initial 4 mg PO qDay or divided q12hr
If inadequate response afer 8-12 weeks, may increase dose to 8 mg PO qDay or divided q12hr
Monitor: ALT at start of treatment, qMonth for 12 months then q3Months thereafter
Dosage Modifications
Active liver disease (ALT >2.5 x ULN): Do not inititate rosiglitazone
Renal impairment: No dosage adjustments required
Coadministration with sulfonylurea: Adjust sulfonylurea dose if hypoglycemia occurs
Safety and efficacy not established
See Adult dosing
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (4)
- eluxadoline
rosiglitazone increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .
- ethanol
ethanol, rosiglitazone. Other (see comment). Contraindicated. Comment: Excessive EtOH consumption may alter glycemic control. Some sulfonylureas may produce a disulfiram like rxn.
- gemfibrozil
gemfibrozil will increase the level or effect of rosiglitazone by decreasing metabolism. Avoid or Use Alternate Drug.
- tucatinib
rosiglitazone will increase the level or effect of tucatinib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of tucatinib (a CYP2C8 substrate) with a strong or moderate CYP2C8 inhibitors increases tucatinib plasma concentrations and risk of toxicities.
Monitor Closely (75)
- albiglutide
albiglutide, rosiglitazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Concurrent use may increase risk of hypoglycemia; monitor glucose levels.
- aripiprazole
aripiprazole, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- asenapine
asenapine, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- atazanavir
atazanavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- atorvastatin
rosiglitazone increases toxicity of atorvastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- bexarotene
bexarotene increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Based on the mechanism of action, bexarotene capsules may increase the action of insulin enhancing agents, resulting in hypoglycemia. Hypoglycemia has not been associated with bexarotene monotherapy.
- bitter melon
bitter melon increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypoglycemia.
- cannabidiol
cannabidiol will increase the level or effect of rosiglitazone by decreasing metabolism. Modify Therapy/Monitor Closely. Cannabidiol may potentially inhibit CYP2C8 activity. Consider reducing the dose when concomitantly using CYP2C8 substrates.
- cholic acid
rosiglitazone increases levels of cholic acid by decreasing elimination. Modify Therapy/Monitor Closely. Avoid concomitant use of inhibitors of the bile salt efflux pump (BSEP). May exacerbate accumulation of conjugated bile salts in the liver and result in clinical symptoms. If concomitant use is necessary, monitor serum transaminases and bilirubin.
- cinnamon
cinnamon increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Potential for hypoglycemia.
- ciprofloxacin
ciprofloxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Hyper and hypoglycemia have been reported in patients treated concomitantly with quinolones and antidiabetic agents. Careful monitoring of blood glucose is recommended.
- clarithromycin
clarithromycin increases levels of rosiglitazone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. May result in hypoglycemia; monitor glucose levels closely.
- darunavir
darunavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- dulaglutide
dulaglutide, rosiglitazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- exenatide injectable solution
exenatide injectable solution, rosiglitazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Concurrent use may increase risk of hypoglycemia; monitor glucose levels.
- exenatide injectable suspension
exenatide injectable suspension, rosiglitazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Concurrent use may increase risk of hypoglycemia; monitor glucose levels.
- fleroxacin
fleroxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Quinolone antibiotic administration may result in hyper- or hypoglycemia. Gatifloxacin is most likely to produce dysglycemia; moxifloxacin is least likely.
- fluvastatin
rosiglitazone increases toxicity of fluvastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- fosamprenavir
fosamprenavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- gemifloxacin
gemifloxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Quinolone antibiotic administration may result in hyper- or hypoglycemia. Gatifloxacin is most likely to produce dysglycemia; moxifloxacin is least likely.
- glecaprevir/pibrentasvir
rosiglitazone will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- iloperidone
iloperidone, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- indinavir
indinavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- insulin aspart
insulin aspart increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin aspart. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin aspart protamine/insulin aspart
rosiglitazone, insulin aspart protamine/insulin aspart. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin degludec
rosiglitazone, insulin degludec. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin degludec/insulin aspart
rosiglitazone, insulin degludec/insulin aspart. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin detemir
insulin detemir increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin detemir. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin glargine
insulin glargine increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin glargine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin glulisine
insulin glulisine increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin glulisine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin inhaled
rosiglitazone, insulin inhaled. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin isophane human/insulin regular human
rosiglitazone, insulin isophane human/insulin regular human. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin lispro
insulin lispro increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin lispro. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin lispro protamine/insulin lispro
rosiglitazone, insulin lispro protamine/insulin lispro. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents.
- insulin NPH
insulin NPH increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin NPH. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - insulin regular human
insulin regular human increases toxicity of rosiglitazone by unknown mechanism. Use Caution/Monitor. Insulin may increase the fluid retention associated with thiazolidinediones (peroxisome proliferator-activated receptor [PPAR]-gamma agonists).
rosiglitazone, insulin regular human. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Antidiabetic agents are often used in combination; dosage adjustments may be required when initiating or discontinuing antidiabetic agents. - ketotifen, ophthalmic
ketotifen, ophthalmic, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Combination may result in thrombocytopenia (rare). Monitor CBC.
- letermovir
letermovir will increase the level or effect of rosiglitazone by unspecified interaction mechanism. Use Caution/Monitor. Monitor glucose concentrations.
- levofloxacin
levofloxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Quinolone antibiotic administration may result in hyper- or hypoglycemia. Gatifloxacin is most likely to produce dysglycemia; moxifloxacin is least likely.
- liraglutide
liraglutide, rosiglitazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Concurrent use may increase risk of hypoglycemia; monitor glucose levels.
- lonapegsomatropin
lonapegsomatropin decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Closely monitor blood glucose when treated with antidiabetic agents. Lonapegsomatropin may decrease insulin sensitivity, particularly at higher doses. Patients with diabetes mellitus may require adjustment of their doses of insulin and/or other antihyperglycemic agents.
- lopinavir
lopinavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- lurasidone
lurasidone, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- marijuana
marijuana decreases effects of rosiglitazone by pharmacodynamic antagonism. Use Caution/Monitor.
- mavacamten
rosiglitazone will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Inititiation of weak CYP2C19 inhibitors may require decreased mavacamten dose.
- mecasermin
mecasermin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Additive hypoglycemic effects.
- mifepristone
mifepristone will increase the level or effect of rosiglitazone by Other (see comment). Use Caution/Monitor. Inhibits CYP2C8/2C9; use smallest recommended doses for substrates and monitor
- moxifloxacin
moxifloxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Quinolone antibiotic administration may result in hyper- or hypoglycemia. Gatifloxacin is most likely to produce dysglycemia; moxifloxacin is least likely.
- nelfinavir
nelfinavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- ofloxacin
ofloxacin increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Quinolone antibiotic administration may result in hyper- or hypoglycemia. Gatifloxacin is most likely to produce dysglycemia; moxifloxacin is least likely.
- olanzapine
olanzapine, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- opuntia ficus indica
opuntia ficus indica increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor.
- paclitaxel
rosiglitazone will increase the level or effect of paclitaxel by Other (see comment). Use Caution/Monitor. Paclitaxel levels/toxicity may increase when coadministered with CYP2C8 inhibitors
- paclitaxel protein bound
rosiglitazone will increase the level or effect of paclitaxel protein bound by Other (see comment). Use Caution/Monitor. Paclitaxel levels/toxicity may increase when coadministered with CYP2C8 inhibitors
- paliperidone
paliperidone, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- pitavastatin
rosiglitazone increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- pravastatin
rosiglitazone increases toxicity of pravastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- quetiapine
quetiapine, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- risperidone
risperidone, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
- ritonavir
ritonavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- rosuvastatin
rosiglitazone increases toxicity of rosuvastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- sacubitril/valsartan
rosiglitazone will increase the level or effect of sacubitril/valsartan by Other (see comment). Use Caution/Monitor. The results from an in vitro study with human liver tissue indicate that valsartan is a substrate of the hepatic uptake transporter OATP1B1; coadministration with OATP1B1 inhibitors may increase valsartan systemic exposure
- saquinavir
saquinavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- selexipag
rosiglitazone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- shark cartilage
shark cartilage increases effects of rosiglitazone by pharmacodynamic synergism. Use Caution/Monitor. Theoretical interaction.
- simvastatin
rosiglitazone increases toxicity of simvastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- somapacitan
somapacitan decreases effects of rosiglitazone by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Growth hormone products may decrease insulin sensitivity, particularly at higher doses. Antidiabetic agents may require dose adjustment after initiating somapacitan. .
- stiripentol
stiripentol will increase the level or effect of rosiglitazone by Other (see comment). Modify Therapy/Monitor Closely. Stiripentol is a CYP2C8 inhibitor. Consider dosage reduction for CYP2C8 substrates if adverse effects are experienced when coadministered.
- sulfamethoxypyridazine
sulfamethoxypyridazine increases effects of rosiglitazone by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.
- tecovirimat
tecovirimat will increase the level or effect of rosiglitazone by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Tecovirimat is a weak inhibitor of CYP2C8 and CYP2C19. Monitor for adverse effects if coadministered with substrates of these enzymes. Monitor blood glucose and monitor for hypoglycemic symptoms.
- teriflunomide
teriflunomide increases levels of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- tipranavir
tipranavir decreases effects of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Reports of hyperglycemia due to insulin resistance with protease inhibitors. .
- valsartan
rosiglitazone will increase the level or effect of valsartan by Other (see comment). Use Caution/Monitor. The results from an in vitro study with human liver tissue indicate that valsartan is a substrate of the hepatic uptake transporter OATP1B1; coadministration with OATP1B1 inhibitors may increase valsartan systemic exposure
- xipamide
xipamide decreases levels of rosiglitazone by increasing renal clearance. Use Caution/Monitor.
- ziprasidone
ziprasidone, rosiglitazone. Other (see comment). Use Caution/Monitor. Comment: Atypical antipsychotics have been associated with hyperglycemia that may alter blood glucose control; monitor glucose levels closely.
Minor (69)
- agrimony
agrimony increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- American ginseng
American ginseng increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- amitriptyline
amitriptyline increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- amoxapine
amoxapine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- anamu
anamu increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Theoretical interaction.
- bendroflumethiazide
bendroflumethiazide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- budesonide
budesonide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- chlorothiazide
chlorothiazide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- chlorthalidone
chlorthalidone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- chromium
chromium increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- clomipramine
clomipramine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- clonidine
clonidine decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, rosiglitazone. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - cornsilk
cornsilk increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hypoglycemia (theoretical interaction).
- cortisone
cortisone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- cyclopenthiazide
cyclopenthiazide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- damiana
damiana decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Theoretical interaction.
- danazol
danazol increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- deflazacort
deflazacort decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- desipramine
desipramine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- devil's claw
devil's claw increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- dexamethasone
dexamethasone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- doxepin
doxepin increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- elderberry
elderberry increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hypoglycemia (in vitro research).
- eucalyptus
eucalyptus increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Theoretical interaction.
- fludrocortisone
fludrocortisone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- fluoxymesterone
fluoxymesterone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- fo-ti
fo-ti increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- forskolin
forskolin increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Colenol, a compound found in Coleus root, may stimulate insulin release.
- gotu kola
gotu kola increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. (Theoretical interaction).
- guanfacine
guanfacine decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
guanfacine, rosiglitazone. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - gymnema
gymnema increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- horse chestnut seed
horse chestnut seed increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- hydrochlorothiazide
hydrochlorothiazide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- hydrocortisone
hydrocortisone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- imipramine
imipramine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- indapamide
indapamide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- isoniazid
isoniazid decreases effects of rosiglitazone by unspecified interaction mechanism. Minor/Significance Unknown.
- juniper
juniper increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hypoglycemia (theoretical interaction).
- lofepramine
lofepramine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- lycopus
lycopus increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hypoglycemia (theoretical interaction).
- maitake
maitake increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hypoglycemia (animal research).
- maprotiline
maprotiline increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- mesterolone
mesterolone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- methyclothiazide
methyclothiazide decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- methylprednisolone
methylprednisolone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- methyltestosterone
methyltestosterone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- metolazone
metolazone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Thiazide dosage >50 mg/day may increase blood glucose.
- nettle
nettle increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. (Theoretical interaction).
- nortriptyline
nortriptyline increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- ofloxacin
ofloxacin, rosiglitazone. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Potential dysglycemia.
- oxandrolone
oxandrolone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- oxymetholone
oxymetholone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- pegvisomant
pegvisomant increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- potassium acid phosphate
potassium acid phosphate increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Interaction especially seen in the treatment of hypokalemia.
- potassium chloride
potassium chloride increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Interaction especially seen in the treatment of hypokalemia.
- potassium citrate
potassium citrate increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Interaction especially seen in the treatment of hypokalemia.
- prednisolone
prednisolone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- prednisone
prednisone decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- protriptyline
protriptyline increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- sage
sage increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- stevia
stevia increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- testosterone
testosterone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- testosterone buccal system
testosterone buccal system increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- testosterone topical
testosterone topical increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- tongkat ali
tongkat ali increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypoglycemia.
- trazodone
trazodone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- triamcinolone acetonide injectable suspension
triamcinolone acetonide injectable suspension decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown.
- trimipramine
trimipramine increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
- vanadium
vanadium increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.
Adverse Effects
>10%
Increased LDL-cholesterol
Increased HDL-cholesterol
Increased total cholesterol
1-10%
Edema
Hypertension
Heart failure/congestive heart failure
Myocardial ischemia
Diarrhea
Upper respiratory tract infection
Frequency Not Defined
Accidental injury
Anemia
Back pain
Fatigue
Headache
Hypoglycemia
Myalgia
Sinusitis
Weight gain
Warnings
Black Box Warnings
Congestive heart failure risk
Thiazolidinediones, including rosiglitazone, cause or exacerbate congestive heart failure in some patients
After initiation, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema)
If these signs and symptoms develop, the heart failure should be managed according to current standards of care
Furthermore, discontinuation or dose reduction must be considered
Not recommended in patients with symptomatic heart failure
Initiation with established NYHA Class III or IV heart failure is contraindicated
Contraindications
Hypersensitivity to rosiglitazone
Diabetic ketoacidosis
Heart failure NYHA class III-IV
Active liver disease: do not start rosiglitazone if ALT >2.5 x ULN
Cautions
Fluid retention, which may exacerbate or lead to heart failure, may occur; combination use with insulin and use in congestive heart failure NYHA Class I and II may increase risk of other cardiovascular effects
If ALT >3 x ULN stop treatment; if 1.5-3 x normal, retest qWeek until normal or 3 x normal and need to discontinue
Not for use in diabetes mellitus type 1; mechanism requires presence of endogenous insulin; use with insulin may increase risk of heart failure; not recommended
Thiazolidinediones, which are peroxisome proliferator-activated receptor (PPAR) gamma agonists, can cause dose-related fluid retention, particularly when used in combination with insulin; dose-related edema and weight gain may occur
When used in combination with other hypoglycemic agents, a dose reduction of concomitant agent may be necessary to reduce risk of hypoglycemia
Associated with rare cases of new onset or worsening of macular edema
May result in ovulation in some premenopausal anovulatory women; ensure adequate contraception
Increased risk of fractures of upper arm, hand, or foot in female patients
Dose-related decreases in hemoglobin and hemocrit reported
Pregnancy & Lactation
Pregnancy
Limited data in pregnant women are not sufficient to determine drug- associated risk for major birth defects or miscarriage; there are risks to mother and fetus associated with poorly controlled diabetes in pregnancy
Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia-related morbidity
Animal data
- In animal reproduction studies, no adverse developmental effects observed when drug was administered to pregnant rats and rabbits during organogenesis at exposures up to 4 times the maximum recommended human dose (MRHD) of 8 mg daily
Reproductive potential of patients
- Discuss potential for unintended pregnancy with premenopausal women as therapy may result in ovulation in some anovulatory women
Lactation
There are no data on presence of rosiglitazone in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk; however, due to species-specific differences in lactation physiology, animal data may not reliably predict drug levels in human milk; developmental and health benefits of breastfeeding should be considered along with mother's clinical need for therapy and any potential adverse effects on breastfed infant or the underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Lowers glucose by improving target cell response to insulin without increasing pancreatic cell secretion; activates nuclear peroxisome proliferator-activated receptor gamma, which influences the production of gene products involved in glucose and lipid metabolism
Pharmacokinetics
Bioavailability: 99%
Onset of Action: Initial effect delayed; maximum effect may take up to 12 weeks
Peak Plasma Time: 1 hr
Protein Bound: >99%
Half-Life: 3-4 hr
Vd: 17.6 L
Metabolism: by hepatic CYP2C8 & CYP2C9 (minor extent)
Excretion: urine 64%; feces 22%
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Formulary
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