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valsartan/amlodipine/hydrochlorothiazide (Rx)Brand and Other Names:Exforge HCT

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

valsartan/amlodipine/hydrochlorothiazide

tablet

  • 5mg/160mg/12.5mg
  • 5mg/160mg/25mg
  • 10mg/160mg/12.5mg
  • 10mg/160mg/25mg
  • 10mg/320mg/25mg
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Hypertension

5-10 mg amlodipine/160-320 mg valsartan/12.5-25 mg hydrochlorothiazide qDay; may titrate dose after 2 weeks

Use in patients not adequately controlled with monotherapy; may use as initial therapy in patients likely to need multiple drugs to achieve blood pressure goals

Indicated for patients not adequately controlled on any 2 of the following antihypertensive classes: calcium channel blockers, angiotensin receptor blockers, and diuretics, OR

Indicated for substitution for the individually titrated drug components

May increase dose after 2 weeks if needed

Not to exceed 10 mg/320 mg/25 mg PO once-daily

Renal & Hepatic Impairment

Renal impairment

  • Mild or moderate (CrCl ≥30 mL/min): No dose adjustment necessary
  • Severe (CrCl <30 mL/min): Safety and effectiveness not established

Hepatic impairment

  • Not recommended for initial therapy; amlodipine 2.5 mg is not an available strength with available dosage forms for this drug combination
  • Amlodipine: Extensively metabolized by liver and half-life increased (56 hr) with impaired hepatic function
  • Valsartan: No dose adjustment necessary with mild-to-severe hepatic impairment
  • Hydrochlorothiazide: Minor alterations of fluid and electrolyte balance may cause hepatic coma in patients with impaired hepatic function

Safety/efficacy not established

Hypertension

Not recommended for initial therapy; amlodipine 2.5 mg is not an available strength with available dosage forms for this drug combination

Initiate with 2.5 mg PO qDay; may titrate dose after 2 weeks

Indicated for patients not adequately controlled on any 2 of the following antihypertensive classes: calcium channel blockers, angiotensin receptor blockers, and diuretics, OR

Indicated for substitution for the individually titrated drug components

May increase dose after 2 weeks if needed

Not to exceed 10 mg/320 mg/25 mg PO once-daily

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Interactions

Interaction Checker

valsartan/amlodipine/hydrochlorothiazide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Amlodipine

            • Edema (1.8-10.8%)

            1-10%

            Amlodipine

            • Headache (7.3%)
            • Fatigue (4.5%)
            • Palpitation (0.7-4.5%)
            • Dizziness (1.1-3.4%)
            • Flushing (0.7-2.6%)
            • Nausea (2.9%)
            • Abdominal pain (1.6%)
            • Somnolence (1.4%)

            Valsartan

            • Hyperkalemia (4-10%)
            • Dizziness (2-8%)
            • Hypotension (1-7%)
            • Fatigue (3%)

            Hydrochlorothiazide

            • Anorexia
            • Epigastric distress
            • Hypokalemia
            • Hypotension
            • Phototoxicity

            <1%

            Hydrochlorothiazide

            • Anaphylaxis
            • Stevens-Johnson syndrome
            • Toxic epidermal necrolysis
            • Disorder of hematopoietic structure
            • Hepatotoxicity
            • Pancreatitis

            Frequency Not Defined

            Valsartan

            • Headache
            • Cough (rare, esp compared to ACE inhibitors)

            Hydrochlorothiazide

            • Confusion
            • Hypomagnesemia
            • Metabolic acidosis
            • Dizziness
            • Fatigue
            • Headach
            • Hypercalcemia
            • Hyperuricemia, Hyperglycemia, Hyperlipidemia, Hypercholesterolemia, Muscle weakness or cramps, Nausea, Purpura, Rash, Vertigo, Vomiting

            Postmarketing Reports

            Valsartan

            • Hypersensitivity: Angioedema (rare)
            • Digestive: Elevated liver enzymes, hepatitis (rare)
            • Renal: Impaired renal function, renal failure
            • Clinical laboratory tests: Hyperkalemia
            • Dermatologic: Alopecia, bullous dermatitis
            • Blood and lymphatic: Thrombocytopenia (rare)
            • Vascular: Vasculitis
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            Warnings

            Black Box Warnings

            Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death

            Contraindications

            Hypersensitivity to valsartan, amlodipine, sulfonamide drugs, or other ingredients

            Pregnancy (2nd and 3rd trimesters): Significant risk of fetal/neonatal morbidity and mortality

            Anuria

            Coadministration with aliskiren in patients with diabetes

            Cautions

            Avoid with severe hepatic impairment or renal impairment (ie, CrCl <30 mL/min)

            Excessive hypotension may occur (rare); caution if volume/salt depleted, initiate cautiously in patients with heart failure, recent MI, or those undergoing surgery or dialysis

            Worsening angina and acute MI may occur after starting or increasing amlodipine dose, particularly with severe obstructive CAD

            Patients whose renal function may depend in part on the activity of the renin angiotensin system (eg, patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, or volume depletion); correct volume depletion prior to initiation

            Dual blockade of the renin angiotensin system with ARBs, ACE inhibitors, or aliskiren associated with increased risk for hypotension, hyperkalemia, and renal function changes (including acute renal failure) compared to monotherapy; closely monitor blood pressure

            Acute transient myopia and acute angle-closure glaucoma has been reported, particularly with history of sulfonamide or penicillin allergy (hydrochlorothiazide is a sulfonamide)

            Hydrochlorothiazide may exacerbate SLE

            Hydrochlorothiazide may alter glucose tolerance and raise serum calcium, cholesterol, and triglycerides

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            Pregnancy & Lactation

            Pregnancy Category: C (1st trimester); D (2nd & 3rd trimesters)

            Lactation: Discontinue drug or do not nurse

            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.

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            Pharmacology

            Mechanism of Action

            Amlodipine: Calcium channer blocker; blocks contractile effects of calcium on cardiac and vascular smooth muscle cells; results in peripheral arterial vasidilation, decreased peripheral vascular resistance, and blood pressure reduction

            Valsartan: Angiotensin receptor blocker; blocks vasoconstriction and sodium retaining effects of angiotensin II on cardiac, vascular smooth muscle, adrenal, and renal cells

            Hydrochlorothiazide: Thiazide diuretic; directly promotes the excretion of sodium and chloride in the kidney leading to reductions in intravascular volume

            Pharmacokinetics

            Bioavailability

            • Amlodipine: 64-90%
            • Valsartan: 10-35%
            • Hydrochlorothiazide: 50-80%

            Peak Concentration Time

            • Amlodipine: 6 hr
            • Valsartan: 3 hr
            • Hydrochlorothiazide: 2 hr

            Half-Life

            • Amlodipine: 30-50 hr (terminal elimination half-life)
            • Valsartan: 6 hr
            • Hydrochlorothiazide: 5.8-18.9 hr

            Vd

            • Amlodipine: 21 L/kg
            • Valsartan: 17 L/kg
            • Hydrochlorothiazide: 3.6-7.8 L/kg

            Protein Bound

            • Amlodipine: 93%
            • Valsartan: 95%
            • Hydrochlorothiazide: 68%

            Metabolism

            • Amlodipine: 90% converted to inactive metabolites via hepatic metabolism
            • Valsartan: 20% metabolized via CYP2C9
            • Hydrochlorothiazide: Not metabolized

            Excretion

            • Amlodipine: 10% parent compound and 60% metabolites excreted in urine
            • Valsartan: 83% (feces); 13% (urine)
            • Hydrochlorothiazide: 61% excreted unchanged in urine
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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