Lisinopril

Cardiovascular Drug

Drug class: Angiotensin Converting Enzyme Inhibitors, ACEI

Lisinopril (ZESTRIL)（中文: 賴諾普利）

Pronunciation

Lisinopril 10mg

Lisinopril 20mg

Lisinopril 5mg

Common Strengths of Lisinopril

Lisinopril is available in the following strengths:

• 5 mg
• 10 mg
• 20 mg

Drug Trade Names of Lisinopril

The brand names for lisinopril is Zestril.

Mechanism of Action

Lisinopril is an angiotensin-1 converting enzyme (ACE inhibitor).

The beneficial effects of ACE inhibitors appear to result primarily from the suppression of the plasma renin-angiotensin-aldosterone system.

Renin is synthesized by the kidneys and released into the circulation where it converts angiotensinogen to angiotensin-I. Angiotensin-I is then converted by angiotensin converting enzyme to angiotensin-II. Angiotensin-II is a potent vasoconstrictor responsible for arterial vasoconstriction and increased blood pressure, as well as for stimulation of the adrenal gland to secrete aldosterone.

Inhibition of ACE results in decreased plasma angiotensin-II, which leads to decreased vasopressor activity and to reduced aldosterone secretion. The latter decrease may result in an increase in serum potassium concentration. Lisinopril is used in the treatment of hypertension and heart failure. It also improves your survival if you are taking it after a recent heart attack of heart failure.

It works by widening your blood vessels and making it easier for your heart to pump blood around your body. It can also be used for diabetic kidney disease, to slow down the disease.

Route of Administration

Lisinopril is administered orally in a single daily dose. The absorption of Lisinopril tablet is not affected by food.

Dosage

• Hypertension
  • Adult: Initially 10 mg once daily; maintenance 20 mg once daily; maximum 80 mg/day.
• Heart failure
  • Adult: Initially 2.5 mg once daily, increased in steps of up to 10 mg at least every 2 weeks; maximum 35 mg per day if tolerated.
• Diabetic kidney disease
  • 10 mg to 20 mg once daily

The antihypertensive effects of lisinopril are seen within 1 to 2 hours of a single oral dose and the maximum effect occurs after about 6 hours, although the full effect may not develop for several weeks during chronic dosing.

The haemodynamic action lasts for about 24 hours after once-daily dosing.

Side Effects

Frequency	Adverse reactions
Common (≥1/100 to <1/10)	Dizziness
	Headache
	Dry
	Itickly (non-productive) cough
	Dyspnoea
	Vomiting
	Diarrhoa
	Hypotension
Uncommon (≥1/1,000 to <1/100)	Confusion
	Sleep disturbances
	Itching or a mild skin rash
	Nausea
	Abdominal pain and indigestion
	Palpitations
	Tachycardia
	Raynaud's syndrome
Rare (≥1/10,000 to <1/1,000)	Alopecia
	Oedema of the face, extremities, lips, tongue, glottis and/or larynx
	Dry mouth
Very Rare (<1/10,000)	Glossitis
	Pancreatitis

Pharmacokinetics

• Following oral administration of lisinopril, peak serum concentrations occur within about 7 hours, although there was a trend to a small delay in time taken to reach peak serum concentrations in acute myocardial infarction patients.
• Lisinopril absorption is not affected by the presence of food.
• Lisinopril does not undergo metabolism and is excreted entirely unchanged into the urine.
• On multiple dosing lisinopril has an effective half-life of 12.6 hours.
• The clearance of lisinopril in healthy subjects is approximately 50 mL/min.

Renal Impairment

Impaired renal function decreases elimination of lisinopril, which is excreted via the kidneys, but this decrease becomes clinically important only when the glomerular filtration rate is below 30 mL/min.

Drug Management

Safety

Your very first dose may make you feel dizzy, so it is best to take it at bedtime. After the first dose, if you do not feel dizzy, you can take lisinopril at any time of day. Try to take it at the same time every day.

Pregnancy

Should be avoided in pregnancy unless essential.

Breast Feeding

• Should avoid in the few weeks after delivery, particularly in preterm infants
  • risk of profound neonatal hypotension
• Can be used in mothers breast-feeding older infants if essential.

Renal Impairment

• If eGFR 31-80 mL/minute/1.73 m²
  • Max. initial doses 5-10 mg daily. (max. 40 mg daily)
• If eGFR 10-30 mL/minute/1.73 m²
  • 2.5 – 5 mg daily (max. 40 mg daily)
• If eGFR < 10 mL/minute/1.73 m²
  • 2.5 mg daily

Monitoring Requirements

Renal function and electrolytes should be checked before starting ACE inhibitors (or increasing the dose) and monitored during treatment (more frequently if side effects mentioned are present).

Drug Interactions

• Diuretics
  • Prior treatment with high dose diuretics may result in volume depletion and a risk of hypotension when initiating therapy with Lisinopril.
• Potassium sparing diuretics (triamterene, amiloride and spironolactone) or potassium supplement
  • May cause significant increase in serum potassium.

Caution

• Concomitant diuretics
  • First dose hypotension (especially in patients taking high doses of diuretics, on a low-sodium diet, on dialysis, dehydrated , or with heart failure)
• Use with care in those with a history of angioedema
• Use with care in patients with severe or symptomatic aortic stenosis (risk of hypotension)

FAQs

How should I take the tablet?

Your doctor may advise you to take your first dose before bedtime, because it can make you dizzy. After the first dose, if you do not feel dizzy, you can take the tablet at any time of day. Try to take it at the same time every day. You can take lisinopril with or without food. Swallow the tablet whole with a drink of water.

What should I avoid while taking?

Should avoid potassium rich foods as lisinopril has the capacity to increase potassium level in the blood. High levels of potassium can lead to irregular heartbeat. It is better to avoid potassium-rich foods like bananas.

What happens if I miss a dose?

If you forget to take a dose and you usually take lisinopril

• Once a day: Take it as soon as you remember unless it is less than 12 hours until your next dose. In this case leave out the missed dose and take your next dose at the usual time

Never take 2 doses to make up for a forgotten one.