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All about: Moexipril Hydrochloride

Big Image Pronouncation: (moe-EX-ah-pril HIGH-droe-KLOR-ide)
Class: ACE inhibitor

Trade Names:
Univasc
- Tablets 7.5 mg
- Tablets 15 mg

Mechanism of Action

Pharmacology

Competitively inhibits angiotensin I-converting enzyme, preventing conversion of angiotensin I to angiotensin II, which is a potent vasoconstrictor and also stimulates aldosterone secretion from the adrenal cortex. This results in decrease in sodium and fluid retention, decrease in BP, and increase in diuresis.

Pharmacokinetics

Absorption

Moexipril is incompletely absorbed and the bioavailability is approximately 13%. Food markedly reduces absorption.

Distribution

Approximately 50% is protein bound and Vd is approximately 183 L.

Metabolism

Active metabolite is moexiprilat.

Elimination

Moexipril is excreted in urine (13%, 1% unchanged) and feces (53%, 1% unchanged). The t ½ is 2 to 9 hr, and the clearances are 441 mL/min (moexipril) and 232 mL/min (moexiprilat).

Onset

1 hr.

Peak

3 to 6 hr.

Duration

24 hr.

Special Populations

Renal Function Impairment

Effective elimination t ½ and AUC of moexipril and moexiprilat are increased with decreasing renal function.

Indications and Usage

Treatment of hypertension.

Contraindications

Hypersensitivity to ACE inhibitors; history of angioedema related to previous treatment with an ACE inhibitor.

Dosage and Administration

Adults Initial dose

PO 7.5 mg qd.

Maintenance

PO 7.5 to 30 mg/day in 1 or 2 divided doses; may add diuretic if needed and decrease dose.

Renal function impairment

Cautiously use 3.75 mg qd in patients with Ccr no more than 40 mL/min/1.73 m 2 . Dosage may be titrated up to a max of 15 mg/day.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F). Protect from moisture.

Drug Interactions

Capsaicin

Cough may be exacerbated.

Digoxin

May increase or decrease plasma digoxin levels.

Diuretics

Excessive reductions in BP may occur.

Indomethacin, salicylates (eg, aspirin)

Reduced hypotensive effects, especially in low-renin or volume-dependent hypertensive patients.

Lithium

Increased lithium levels and symptoms of lithium toxicity.

Phenothiazines

May increase the pharmacologic effect of moexipril.

Potassium-sparing diuretics, potassium preparations

May increase serum potassium levels.

Laboratory Test Interactions

False elevation of liver enzymes and uric acid may occur.

Adverse Reactions

CNS

Dizziness (4%); fatigue (2%).

Dermatologic

Rash (2%).

EENT

Pharyngitis (2%).

GI

Diarrhea (3%).

Hematologic-Lymphatic

Neutropenia; agranulocytosis.

Metabolic

Hyperkalemia.

Musculoskeletal

Myalgia (1%).

Respiratory

Cough (6%).

Miscellaneous

Flu syndrome (3%); flushing (2%); anaphylactoid reactions.

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.


Pregnancy

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

Lactation

Undetermined.

Children

Safety and efficacy not established.

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

In renal insufficiency, increased serum creatinine may occur due to inadequate renal perfusion; monitor renal function during first few weeks of therapy and adjust dosage carefully; for patients with Ccr less than 40 mL/1.73 m 2 , give an initial dose of 3.75 mg. Doses may be carefully titrated to max of 15 mg/day.

Hepatic Function

Hepatic failure has been associated with other ACE inhibitors. Patients who develop jaundice or marked elevations of liver enzymes should discontinue drug and receive medical follow-up.

Angioedema

Use with 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 the first dose, especially in severely salt- or volume-depleted patients or in those with heart failure. Minimize risk by discontinuing diuretics, decreasing dose, or increasing salt intake approximately 2 to 3 days prior to initiating drug.

Neutropenia/agranulocytosis

Has been reported with other ACE inhibitors. Risk appears greater in patients with renal dysfunction, heart failure, or immunosuppression.

Overdosage

Symptoms

Hypotension.

Patient Information

  • Explain name, dose, action, and potential side effects of drug.
  • Advise patient to take qd or bid as prescribed.
  • Advise patient to take medication 1 hr before or 2 hr after meals because food can reduce absorption and benefits of medication.
  • Advise patient to try to take each dose at about the same time each day.
  • Inform 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 BP medications 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 if abnormal measurements are 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 importance of other modalities on BP control: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
  • 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 to not take any prescription or OTC medications, potassium-containing salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.
  • Advise patient that follow-up visits and lab tests will be required to monitor therapy and to keep appointments.

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