captopril (Rx)

Brand and Other Names:Capoten, Captoril
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg
  • 50mg
  • 100mg
more...

Acute Hypertension

12.5-25 mg PO; may repeat PRN

Hypertension (Alone or with Thiazide)

Initial: 25 mg PO q8-12hr, increase gradually based on response (may start lower in some patients)

Maintenance: 25-150 mg PO q8-12hr

450 mg/day maximum

Congestive Heart Failure (With Diuretics and Digitalis)

Initial: 6.25-12.5 mg PO q8hr in conjunction with cardiac glycoside and diuretic therapy

Target therapy: 50 mg q8hr

450 mg/day maximum

Left Ventricular Dysfunction After Myocardial Infarction

6.25 mg PO initially followed by 12.5 mg q8hr

Increase to 25 mg PO q8hr over next few days; THEN

Target dose: 50 mg PO q8hr

Diabetic Nephropathy

25 mg PO q8hr

Dosing Considerations

Beneficial for many patients at risk for heart disease; reduces risk of MI, stroke, diabetic nephropathy , microalbuminuria, new onset DM

Consider starting an ACE inhibitor in high-risk patients, even if no HTN or CHF

May prolong survival in CHF, may preserve renal function in DM

May help to prevent migraine HA

Good choice in hyperlipidemia patients

Requires weeks for full effect; to start, use low dose and titrate every 1-2wk

Administration

Take on an empty stomach

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg
  • 50mg
  • 100mg
more...

Hypertension (Off-label)

Neonates: 0.05-0.1 mg/kg/dose q8-24hr, titrate dose up to 0.5 mg/kg/dose q6-24hr 

Infants: 0.15-0.3 mg/kg/dose; titrate dose upward to maximum 6 mg/kg/day in 1-4 divided doses; 2.5-6 mg/kg/day usually required

Children: 0.3-0.5 mg/kg/dose; titrate to maximum 6 mg/kg/day divided q6-12hr

Older children: 6.25-12.5 mg/dose q12-24hr; titrate to no more than 6 mg/kg/day divided q6-12hr

Adolescents: 12.5-25 mg/dose q8-12hr; may increase by 25 mg/dose q1-2Weeks to maximum 450 mg/day

Other Information

Take on an empty stomach

Acute hypertension

12.5-25 mg PO; may repeat PRN

Hypertension (alone or with thiazide)

Initial: 25 mg PO q8-12hr, increase gradually based on response (may start lower in some patients)

Maintenance: 25-150 mg PO q8-12hr

450 mg/day maximum

Congestive heart failure (with diuretics and digitalis)

Initial: 6.25-12.5 mg PO q8hr in conjunction with cardiac glycoside and diuretic therapy

Target therapy: 50 mg q8hr  

450 mg/day maximum

Left ventricular dysfunction after myocardial infarction

6.25 mg PO initially followed by 12.5 mg q8hr

Increase to 25 mg PO q8hr over next few days; THEN

Target dose: 50 mg PO q8hr

Diabetic nephropathy

25 mg PO q8hr

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Interactions

Interaction Checker

and captopril

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Hyperkalemia (1-11%)

            1-10%

            Hypersensitivity rxns (4-7%)

            Skin rash (4-7%)

            Dysgeusia (2-4%)

            Hypotension (1-2.5%)

            Pruritus (2%)

            Cough (0.5-2%)

            Chest pain (1%)

            Palpitations (1%)

            Proteinuria (1%)

            Tachycardia (1%)

            Frequency Not Defined

            Cardiac arrest

            Orthostatic hypotension

            Ataxia

            Confusion

            Depression

            Somnolence

            Angioedema

            Photosensitivity

            Neutropenia

            ARF if renal artery stenosis

            Renal impairment

            Impotence

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            Warnings

            Black Box Warnings

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

            Contraindications

            Hypersensitivity to ACE inhibitors

            Anuria

            History of ACEI-induced angioedema

            Hereditary or idiopathic angioedema

            Bilateral renal artery stenosis

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

            Do not coadminister with aliskiren in patients with diabetes mellitus or with renal impairment (ie, GFR <60 mL/min/1.73 m²)

            Cautions

            Aortic stenosis/hypertrophic cardiomyopathy, hypotension, biliary cirrhosis or biliary obstruction, myelosuppression, electrolyte imbalance, hyperuricemia or gout, SLE, hepatic or renal impairment

            Avoid concomitant use with lithium

            Less effective in African-Americans

            Excessive hypotension if concomitant diuretics or volume-depleted; start with 6.25 mg q8hr

            Risk of hyperkalemia, especially with K+ sparing diuretics

            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

            Blood levels don't correlate with BP response

            Food decreases absorption

            ACE inhibition also causes increased bradykinin levels which putatively mediates angioedema

            Coadministration with mTOR inhibitors (eg, temsirolimus, everolimus, sirolimus) may increase risk for angioedema

            Intestinal angioedema, that presented with abdominal pain, reported in patients treated with ACE inhibitors

            Neutropenia (<1000/mm³ with myeloid hypoplasia reported with captopril; risk is dependent on clinical status of patient

            Causes false positive urine acetone

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            Pregnancy & Lactation

            Pregnancy Category: C; D in 2nd & 3rd trimesters

            Discontinue as soon as pregnancy detected; during the second and third trimesters of pregnancy, drugs that act directly on the renin-angiotensin have been associated with fetal injury that includes hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death

            Lactation: enters breast milk/not recommended (AAP states compatible with nursing)

            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

            Angiotensin converting enzyme (ACE) inhibitors dilate arteries and veins by competively inhibiting the conversion of angiotensin I to angiotensin II (a potent endogenous vasoconstrictor) and by inhibiting bradykinin metabolism; these actions result in preload and afterload reductions on the heart

            ACE inhibitors also promote sodium and water excretion by inhibiting angiotensin-II induced aldosterone secretion; elevation in potassium may also be observed

            ACE inhibitors also elicit renoprotective effects through vasodilation of renal arterioles

            ACE inhibitors reduce cardiac and vascular remodeling associated with chronic hypertension, heart failure, and myocardial infarction

            Pharmacokinetics

            Half-Life: 1.9 hr (healthy); 2.06 (heart failure); 20-40 hr (anuria); significantly increase in CrCl <20 mL/min

            Onset: PO: initial response: 15-30 min; peak response: 60-90 min

            Duration: PO (multiple dose): 8-12 hr

            Peak Plasma Time: PO: 0.5-1.5 hr

            Therapeutic range: 0.05-0.5 mcg/mL

            Bioavailability: 70-75%

            Protein Bound: 25-30%

            Vd: 0.7 L/kg

            Metabolism: liver (50%)

            Metabolites: captopril-cysteine disulfide (inactive)

            Total Body Clearance: 0.8 L/kg/hr

            Renal Clearance: 0.4 L/kg/hr

            Excretion: mainly urine (95%)

            Dialyzable: Yes (HD)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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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