Drug Information

Drug Interaction:

Angiotensin II Receptor Antagonists-

Candesartan, Eposartan, Irbestan, Losartan metabolite, Olmesatran, Telmistran, Valsartan

Prior treatment with diuretics increases risk of excessive hypotension, use a lower initial dose.

Potassium, potassium-sparing diuretics, cyclosporin may increase risk of hyperkalaemia, monitor potassium.

NSAIDs (including COX-2 inhibitors) may reduce antihypertensive response risk of hyperkalaemia or acute renal failure.

Excretion of lithium may be reduced; monitor lithium concentration

Indication:

Hypertension

Approved by (DCI) Drug Controller GENERAL - India For Marketing

(Ref- IDMA Publication)

Name of Drug Indication Date of Approval

Candesartin Antihypertensive 31-08-2000

FIXED DOSE COMBINATIONS APPROVED BY DCG(I)

FROM JANUARY 1961 TILL NOVEMBER 2014

Name of Drug Indication Date of Approval

1.Candesartan Cilexetil 16mg+ 13-01-2002

Hydrochlorthiazide 12.5mg tablet

Essential hypertension (not for initial therapy)

Angiotensin II Receptor Antagonists-

Candesartan, Eprosartan, Irbestan, Losartan metabolite, Olmesatran, Telmistran, Valsartan

Adverse Reaction:

Angiotensin II Receptor Antagonists-

Candesartan, Eprosartan, Irbestan, Losartan metabolite, Olmesatran, Telmistran, Valsartan

Adverse Reactions-

CANDESARTAN-

CNS-

Dizziness 4% , Headache,Fatigue, Anxiety/nervousness Depression < 1%

GI -

Diarrhea > 1% Dyspepsia/heartburn > 0.5%, Nausea/vomting >1% Adominal pain >1%

Musculoskeletal-

Arthalgia >1% Pain 3% Myalgia >0.5%

Respiratory -

Upper Res tract infn 6 % Cough >1 % Sinusitis >1% Pharyngitis 2%, Bronchitis >1%

Miscellaneous -

Chest pain >1% Rash > 0.5%Tacycardia > 0.5%   Peripheral edema >1%
  Albuminurea > 1%   Hypertriglyceridemia > 0.5%
   Creatinine phosphokinase increase > 0.5% .Hypperglycemia   > 0.5%
   Hematuria > 0.5%

Contra-Indications:

Hypersensitivity reactions. Patients with a history of angioedema, including angioedema following use of ACE inhibitors.

Special precautions:

Patients with sodium depletion and aortic or mitral valve stenosis, hypertrophic obstructive cardiomyopathy as severe hypotension may occur.

Patients with renal artery stenosis, there is a risk of impaired renal function and precipitation of acute renal failure.

Patients with primary hyperaldosteronism may poorly respond to anyihypertensive effect of the drug.

Women of reproductive potential, avoid use of this drug in women who are likely to become pregnant

Dosages/ Overdosage Etc:

Date of approval August 2000

Indication-

Hypertension

Dosage

Blood pressure response is dose related over a range of 2 to 32mg once daily

Most of the anti-hypertensive effect is present within 2 weeks amd maximal blood pressure reduction obtained wihin 4 to 6 weeks of treatment with candesartan

Patient Information:

1.Women of reproductive potential, avoid use of this drug in women who are likely to become pregnant

2.Food does not affect the bioavailability of candesartan

Pharmacology/ Pharmacokinetics:

Angiotensin II Receptor Antagonists-

Candesartan, Eprosartan, Irbestan, Losartan metabolite, Olmestaran, Telmistran, Valsartan

Ref- Drug Facts and Comparison (2010)

Pharmacology:

Candesartan blocks the binding of angiotension II to type I angiotension (AT) receptors and

therefore blocks the effects of angiotensin more selectively than do the ACE inhibitors, reduces angiosin-induced vassoconstriction, sodium readsorption and aldosterone release.

Pharmacokinetics:

After oral administration, candesartan cilexetil is rapidly and completely metabolised to the active compound candesartin during absorption from gastro-intestinal tract. Peak plasma concentration reaches at approx 3 to 5 hours. Food does not affect the bioavailability. Within 72 hours about 90% of the dose is excreted. The terminal half-life ranged from approx 9 to 13 hours.

Angiotensin II Receptor Antagonists Pharmacoknetics

Parameters Candesartran Eprosartan Irbesartan Losartan

metabolite

Bioavailability 15% ~13% 60% to 80% ~ 33%

Food effect no effect <25% no effect 10% 14%

AUC /Cmax)

Plasma bound >99% ~ 98% 90% 98.7% (99.8%)

Tmax 3 to 4h 1to 2 1.5 to 2h 1h(3 to 4h)

Volume 0.13L/kg 308L 53to 93L ~34L(~12L)

distribution

Converted to minor minor <20% ~14%

metabolite

Metabolism O-demeth glucoron CYP2C9 CYP2C9/

lation idation CYP3A4

Terminal ~9hr 5 to 9h 11 to 15h ~2h(6 to 9h)

half-life

Total Plasma 0.37mL/ ~130mL/min 157 to ~600mL/min

clearance min/kg 176mL/min (~50mL/min)

Renal 0.19mL/ ~30 to 40 3 to 3.5 ~75mL/min

clearance min/kg mL/min mL/min (~25mL/min)

Recovered ~33% ~7% ~20% ~45/~35%

in urine (IV/oral)

Recovered ~67% ~90% ~80% ~50~60%

in feces (IV/oral)

Olmesartan Telmisartan Valsartan

Bioavailability ~26% 42% /58% ~25%

(40mg/160mg)

Food effect no effect 6%/20% 40%/50%

(AUC/Cmax) (40mgAUC/

160mg AUC)

Plasma 99% >99.5% 95%

bound

Tmax 1 to 2 0.5 to 1h 2 to 4h

Volume of ~17L ~500L 17L

distribution

Convereted none ~11% ~20%

to metabolite

Metabolism none conjugation unknown

Terminal ~13hr ~24hr ~6hr

half life

Total plasma 1.3L/h >800mL/min ~2L/h

clearance

Renal 0.6L/h nd 0.62L/h

clearance

Recovered 35% to 50% 0.91%/ ~13%

in urine 0.49%(IV/oral)

Recovered 50% to65% >97% ~83%

in feces

Interaction with Food:

Food does not affect the bioavailability of candesartan

Pregnancy and lactation:

Insufficient information available on pregnancy and lactation.

Women of reproductive potential, avoid use of this drug in women who are likely to become pregnant

Candesartan Cilexetil - Angiotensin II Receptor Antagonists- (FDC-List) (2000)

Drug Interaction

Indication

Adverse Reaction

Contra-Indications

Dosages/ Overdosage Etc

Patient Information

Pharmacology/ Pharmacokinetics

Interaction with Food

Pregnancy and lactation

Drug Interaction:

Indication:

Adverse Reaction:

Contra-Indications:

Dosages/ Overdosage Etc:

Patient Information:

Pharmacology/ Pharmacokinetics:

Interaction with Food:

Pregnancy and lactation:

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