Tekturna Hct (aliskiren hemifumarate/hydrochlorothiazide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Aliskiren is a nonpeptide renin inhibitor.
Hydrochlorothiazide is a thiazide diuretic and antihypertensive agent.
Aliskiren is a nonpeptide renin inhibitor. Renin catalyzes the conversion of angiotensinogen to angiotensin I, the initial and rate-limiting enzymatic reaction of the renin-angiotensin-aldosterone (RAA) system; angiotensin I is subsequently cleaved to angiotensin II by angiotensin-converting enzyme (ACE). Angiotensin II has vasoconstrictor and aldosterone-secreting effects, which increase blood pressure.
All drugs that inhibit the RAA system, including renin inhibitors, suppress feedback inhibition of renin secretion, leading to a compensatory increase in plasma renin concentrations. When this increase occurs during therapy with ACE inhibitors or angiotensin II receptor antagonists, the result is increased plasma renin activity (PRA). Because aliskiren binds with high affinity to plasma renin, aliskiren inhibits effects of increased renin concentrations and conversion of angiotensinogen to angiotensin I, resulting in reduced PRA and reduced concentrations of angiotensin I, angiotensin II, and aldosterone; whether aliskiren affects other RAA system components (e.g., ACE, non-ACE pathways) is not known.
Oral bioavailability of aliskiren is low (about 2.5%). Based on in vitro studies, aliskiren appears to be metabolized by cytochrome P-450 (CYP) isoenzyme 3A4. The amount of the absorbed dose that is metabolized has not been established; however, aliskiren appears to undergo minimal hepatic metabolism.
In addition, aliskiren is a substrate for P-glycoprotein and organic anion transport protein (OATP) 2B1. Unabsorbed aliskiren is excreted principally in feces as unchanged drug, and absorbed drug is eliminated principally in feces via hepatobiliary clearance as unchanged drug and minimally in urine; approximately 25% of an absorbed oral dose of aliskiren is eliminated in urine as unchanged drug.
Generic name: aliskiren hemifumarate/hydrochlorothiazide
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Tekturna Hct:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Dosage of aliskiren hemifumarate is expressed in terms of aliskiren.
Dosage of hydrochlorothiazide should be individualized according to the patient's requirements and response. The lowest dosage necessary to produce the desired clinical effect should be used. If hydrochlorothiazide is added to the regimen of a patient stabilized on a potent hypotensive agent, dosage of the hypotensive agent should initially be reduced to avoid the possibility of severe hypotension.
Aliskiren is administered orally. The manufacturer recommends that patients establish a routine pattern for taking aliskiren with regard to meals; administration with a high-fat meal substantially decreases absorption of the drug.
Hydrochlorothiazide is administered orally.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Concomitant use of aliskiren and an angiotensin-converting enzyme (ACE) inhibitor or angiotensin II receptor antagonist in patients with diabetes mellitus. (See Use in Combination with Angiotensin-converting Enzyme Inhibitors or Angiotensin II Receptor Antagonists under Warnings/Precautions: Other Warnings/Precautions, in Cautions.)
Known hypersensitivity to aliskiren or any ingredient in the formulation.
Use in pediatric patients younger than 2 years of age. (See Pediatric Use under Warnings/Precautions: Specific Populations, in Cautions.)
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects reported in hypertensive patients receiving aliskiren include diarrhea, headache, dizziness, fatigue, cough, back pain, flu-like symptoms, rash, hyperkalemia, small increases in BUN or serum creatinine concentration, and increased serum creatine kinase (CK, creatine phosphokinase, CPK) concentrations.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety of aliskiren therapy has been evaluated in pediatric patients 6-17 years of age receiving the drug for up to 52 weeks. (See Uses: Hypertension in Pediatric Patients.) In these studies, no unanticipated adverse effects were observed; adverse effects in pediatric patients 6 years of age or older are expected to be similar to those observed in adults. Preclinical studies in rats indicate a potential for a substantial increase in exposure to aliskiren in pediatric patients. The manufacturer states that aliskiren is contraindicated in children younger than 2 years of age and should not be used in children 2 to younger than 6 years of age or in children who weigh less than 20 kg.
If oliguria or hypotension occurs in neonates with a history of in utero exposure to aliskiren, blood pressure and renal function should be supported; exchange transfusions or dialysis may be required. (See Fetal/Neonatal Morbidity and Mortality under Warnings/Precautions: Warnings, in Cautions.)
Aliskiren can cause fetal harm when administered to a pregnant woman. (See Fetal/Neonatal Morbidity and Mortality under Warnings/Precautions: Warnings, in Cautions.)
Aliskiren is distributed into milk in rats; it is not known whether the drug is distributed into human milk. Breast-feeding is not recommended during treatment with aliskiren.
When the total number of patients studied in clinical trials of aliskiren is considered, 19% were 65 years of age or older, while 3.4% were 75 years of age or older. In clinical trials of aliskiren in fixed combination with hydrochlorothiazide, 19.6% of patients were 65 years of age or older and 3.2% were 75 years of age and older. Although no overall differences in efficacy or safety were observed between geriatric and younger patients and other clinical experience revealed no evidence of age-related differences, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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