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CREANZ 8

Quick Overview

Our aim is to reach out to the globe within shortest possible time frame


To promote this objective, not only we distribute and market our  Cardiovascular range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Creanz 8 which contains Candesartan cilexetil...8 mg.


This Creanz 8 contains same active ingredient as Blopress from Astrazeneca.


 

CREANZ 8

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Details

 Each uncoated tablet contains:

Candesartan cilexetil        8 mg

Excipients                         q.s.

CHEMICAL NAME: 2-ethoxy-1-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-1,3-benzodiazole-6-carboxylic acid.

CATEGORY: Angiotensin II receptor antagonist

DESCRIPTION: A white coloured, round shaped, biconvex, uncoated tablet.

CLINICAL PHARMACOLOGY

Mechanism of Action:

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathways for angiotensin II synthesis.

There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Candesartan has much greater affinity (>10,000-fold) for the AT1 receptor than for the AT2 receptor.

Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because candesartan does not inhibit ACE (kininase II) it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Candesartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of candesartan on blood pressure.

Pharmacokinetic Actions

Absorption:

Candesartan cilexetil is rapidly and completely bioactivated by ester hydrolysis during absorption from the gastrointestinal tract to candesartan, a selective AT1 subtype angiotensin II receptor antagonist.

Distribution:

The volume of distribution of candesartan is 0.13 L/kg. Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells. The protein binding is constant at candesartan plasma concentrations well above the range achieved with recommended doses. In rats, it has been reported that candesartan crosses the blood-brain barrier poorly, if at all. It has also been demonstrated in rats that candesartan passes across the placental barrier and is distributed in the fetus.

Metabolism

It undergoes minor hepatic metabolism by O-deethylation to an inactive metabolite. The elimination half-life of candesartan is approximately 9 hours. After single and repeated administration, the pharmacokinetics of candesartan is linear for oral doses up to 32 mg of candesartan cilexetil. Candesartan and its inactive metabolite do not accumulate in serum upon repeated once-daily dosing.

Excretion

Candesartan is mainly excreted unchanged in urine and feces (via bile). Following an oral dose of 14C-labeled candesartan cilexetil, approximately 33% of radioactivity is recovered in urine and approximately 67% in feces. Biliary excretion contributes to the elimination of candesartan. Total plasma clearance of candesartan is 0.37 mL/min/kg, with a renal clearance of 0.19 mL/min/kg. When candesartan is administered orally, about 26% of the dose is excreted unchanged in urine.

DOSAGE AND ADMINISTRATION:

                                             Starting Dose        Dose Range Target    Maintenance Dose

Adult Hypertension (2.1)    16 mg tablet           8 - 32 mg tablet total             _

                                                once daily               daily dose

 

Pediatric Hypertension        0.20 mg/kg              0.05 - 0.4 mg/kg                  _

   (1 to < 6 years)                oral suspension       oral suspension

                                             once daily                once daily or

                                                                             consider divided

                                                                               dose

Pediatric Hypertension       < 50 kg 4 - 8              > 50 kg 8 - 16            _

   (6 to < 17 years)            mg tablet once          mg tablet once

                                                  daily           daily or consider

                                                                              divided dose

                                            < 50 kg 4 - 16    > 50 kg 4 - 32

                                           mg tablet once   mg tablet once

                                                 daily             daily or consider

                                                                                   divided dose

 

Adult Heart Failure              4 mg tablet                 32 mg tablet

                                               once daily                   once daily

The target dose is 32 mg once daily, which is achieved by doubling the dose at approximately 2-week intervals, as tolerated by patient.

INDICATIONS:

Hypertension: Treatment of hypertension in adults and children 1 to < 17 years of age.

Heart Failure: Treatment of heart failure (NYHA class II-IV) in adults with left ventricular systolic dysfunction (ejection fraction ≤ 40%) to reduce cardiovascular death and to reduce heart failure hospitalizations.

USE IN SPECIFIC POPULATIONS:

Geriatric Use:

•           Hypertension

            No overall differences in safety or effectiveness were             reported between geriatric and younger adult subjects, and other reported clinical experience has not identified             differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

•           Heart Failure

            In patients ≥ 75 years of age, the reported incidence of drug discontinuations due to adverse events was abnormal renal function, hypotension and hyperkalemia.         In addition to monitoring of serum creatinine, potassium, and blood pressure during dose escalation and periodically thereafter, greater sensitivity of some older individuals with heart failure must be considered.

CONTRAINDICATIONS

Contraindicated in patients who are hypersensitive to any component of this product.

WARNING:

USE IN PREGNANCY:

When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, CREANZ should be discontinued as soon as possible.

Drug Interactions-

No significant drug interactions have been reported in studies of candesartan cilexetil given with other drugs such as glyburide, nifedipine, digoxin, warfarin, hydrochlorothiazide, and oral contraceptives in healthy volunteers, or given with enalapril to patients with heart failure (NYHA class II and III). Because candesartan is not significantly metabolized by the cytochrome P450 system and at therapeutic concentrations has no effects on P450 enzymes, interactions with drugs that inhibit or are metabolized by those enzymes would not be expected.

Lithium: Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with ACE inhibitors, and with some angiotensin II receptor antagonists. An increase in serum lithium concentration has been reported during concomitant administration of lithium with CREANZ, so careful monitoring of serum lithium levels is recommended during concomitant use.

PREGNANCY AND LACTATION:

Pregnancy: Pregnancy Categories C (first trimester) and D (second and third trimesters)

Labor and Delivery: The effect of CREANZ on labor and delivery in humans is unknown.

Nursing Mothers

It is not known whether candesartan is excreted in human milk, but candesartan has been shown to be present in rat milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue CREANZ, taking into account the importance of the drug to the mother.

EFFECT TO DRIVE & USE THE MACHINE: None

ADVERSE EFFECTS:

Most common adverse reactions which caused adult patients to discontinue therapy for:

• Hypertension was headache and dizziness.

• Heart Failure was hypotension, abnormal renal function,    and hyperkalemia.

• Most common adverse reactions (incidence ≥ 2% and          greater than placebo) are back pain, dizziness, upper       respiratory tract infection, pharyngitis and rhinitis.

OVERDOSAGE

No lethality was observed in acute toxicity studies in mice, rats, and dogs given single oral doses of up to 2000 mg/kg of candesartan cilexetil. In mice given single oral doses of the primary metabolite, candesartan, the minimum lethal dose was greater than 1000 mg/kg but less than 2000 mg/kg. The most likely manifestation of overdosage with CREANZ would be hypotension, dizziness, and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Candesartan cannot be removed by hemodialysis.

Treatment:

To obtain up-to-date information about the treatment of overdose, consult your Regional Poison Control Center. Telephone numbers of certified poison control centers are listed in the Physicians’ Desk Reference (PDR). In managing overdose, consider the possibilities of multiple-drug overdoses, drug-drug interactions, and altered pharmacokinetics in your patient.

Storage: Store in a cool and dry place below 300C. Protect from light.

Packing: Blister of 10 tablets.

Shelf Life: 30 months from the date of manufacturing.

 

 

 

 

 

 

 
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