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Fosinopril Sodium

Pronunciation

Pronunciation: FAH-sin-oh-PRILL SO-dee-uhm
Class: Antihypertensive, ACE inhibitor

Trade Names

Monopril
- Tablets 10 mg
- Tablets 20 mg
- Tablets 40 mg

Apo-Fosinopril (Canada)
Gen-Fosinopril (Canada)
Novo-Fosinopril (Canada)

Pharmacology

Competitively inhibits angiotensin I-converting enzyme, preventing conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates release of aldosterone. Results in decrease in BP, reduced sodium reabsorption, and potassium retention.

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Pharmacokinetics

Absorption

Absolute bioavailability averages 36%. T max is about 3 h.

Distribution

Protein binding is about 99.4%. Fosinopril does not cross the blood-brain barrier.

Metabolism

The major active metabolite is fosinoprilat.

Elimination

There is approximately equal elimination between the liver and the kidney. The t ½ is about 12 h (fosinoprilat). Cl in hemodialysis is about 2% and about 7% with peritoneal dialysis.

Onset

1 h.

Peak

2 to 12 h.

Duration

24 h.

Indications and Usage

Hypertension; heart failure.

Contraindications

Hypersensitivity to ACE inhibitor; history of angioedema related to previous treatment with an ACE inhibitor and in patients with hereditary or idiopathic angioedema.

Dosage and Administration

Heart Failure
Adults

PO

Initial dose

10 mg every. Increase over several weeks. Usual range is 20 to 40 mg/day. Do not exceed 40 mg/day.

Hypertension
Adults

PO

Initial dose

10 mg every.

Maintenance dose

20 to 80 mg/day; if inadequate response, consider dividing into 2 doses.

Children (weighing more than 50 kg)

PO 5 to 10 mg every as monotherapy.

General Advice

  • Give without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (59° to 89°F). Protect from moisture.

Drug Interactions

Allopurinol

Increased risk of hypersensitivity reactions.

Antacids

May decrease effects of fosinopril.

Capsaicin

Cough may be exacerbated.

Digoxin

May increase or decrease levels of digoxin.

Indomethacin, salicylates (eg, aspirin)

Hypotensive effects may be reduced, especially in low-renin or volume-dependent hypertensive patients.

Lithium

Increased lithium levels and symptoms of lithium toxicity may occur.

Phenothiazines

May increase pharmacologic effect of fosinopril.

Potassium preparations, potassium-sparing diuretics

May increase serum potassium levels.

Laboratory Test Interactions

Measurement of serum digoxin with DigiTab RIA kit may be falsely low. False elevation of liver enzymes or serum bilirubin may occur.

Adverse Reactions

Cardiovascular

Hypotension (4%); orthostatic hypotension (2%); subjective cardiac rhythm disturbance (1%).

CNS

Dizziness (12%); weakness (1%).

GI

Diarrhea (2%); nausea, vomiting (1%).

Hematologic

Transient hemoglobin decrease; neutropenia; leukopenia; eosinophilia.

Metabolic

Hyperkalemia; hyponatremia.

Musculoskeletal

Pain (3%).

Respiratory

Cough (10%); upper respiratory tract infection (2%).

Miscellaneous

Chest pain (2%).

Precautions

Warnings

Pregnancy

When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.


Monitor

Assess heart failure patient for evidence of worsening failure (eg, daily weights, evaluation of peripheral edema, shortness of breath).


Pregnancy

Category D (second, third trimester); Category C (first trimester).

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children weighing less than 50 kg.

Elderly

Use with caution, usually starting at the low end of the dose range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Renal Function

Reduce dose and give less frequently. In renal insufficiency, stable elevations in BUN and serum creatinine may occur because of inadequate renal perfusion; monitor renal function during first few weeks of therapy and adjust dosage.

Hepatic Function

May result in elevated plasma levels; monitor carefully; reduce doses.

Angioedema

May occur. Use extreme caution in patients with hereditary angioedema.

Hepatic failure

Rarely, ACE inhibitors have been associated with a syndrome that starts with cholestatic jaundice and progresses to fulminant hepatic necrosis and sometimes death.

Hypotension/First-dose effect

Significant decreases in BP may occur after first dose, especially in severely salt- or volume-depleted patients or those with heart failure; monitor closely for at least 2 h after initial dose and during first 2 wk of therapy. Minimize risk by discontinuing diuretics, decreasing dose, or increasing salt intake about 1 wk prior to initiating fosinopril.

Neutropenia and agranulocytosis

Have occurred; risk appears greater in patients with renal dysfunction, heart failure, or immunosuppression; monitor WBC counts frequently. Ensure that CBC with differential are evaluated prior to starting therapy, at 2 wk intervals for 3 mo, and periodically thereafter in patient with renal impairment.

Proteinuria

May occur, especially in patients with prior renal disease or those receiving high doses; generally within 6 mo.

Overdosage

Symptoms

Hypotension.

Patient Information

  • Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
  • Advise patient to try to take each dose at about the same time each day.
  • Inform hypertensive patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient to continue taking other medications for the condition as prescribed by health care provider.
  • Instruct patient in BP and pulse measurement skills.
  • Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
  • Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
  • Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
  • Emphasize to hypertensive patient the importance of other modalities on BP control: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
  • Emphasize to heart failure patient the importance of other modalities that can help control heart failure symptoms: weight control, progressive exercise program, smoking cessation, and moderate intake of alcohol and salt.
  • Advise heart failure patient to weigh daily, keep a record of daily weights, and notify health care provider if rapid weight gain (eg, 2 pounds in 1 day or 5 pounds in 1 wk) is noted or if edema or shortness of breath are getting worse.
  • Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to excessive fall in BP, resulting in lightheadedness or fainting.
  • Advise patient that medication may cause dizziness or lightheadedness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
  • Caution patient to avoid unnecessary exposure to UV light (sunlight, tanning booths) and to use sunscreen and wear protective clothing when exposed to UV light to avoid photosensitivity reaction.
  • Instruct women to inform health care provider if pregnant, planning to become pregnant, or breastfeeding.
  • Instruct patient to stop taking drug and immediately report any of the following symptoms to health care provider: sore throat, fever, swelling of the hands or feet, irregular heartbeat, chest pains, fainting, swelling of the face, lips, eyelids, or tongue, difficulty breathing.
  • Instruct patient to inform health care provider if a persistent cough develops while taking this medication.
  • Caution patient not to take any prescription or OTC medications, potassium-containing salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.

Copyright © 2009 Wolters Kluwer Health.

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