Perindopril

Pronunciation

Perindopril 4mg (ACERTIL 4mg)

Generic Name:	Perindopril
Class:	Cardiovascular Drug
Subclass:	ACE inhibitor
Legal Classification:	P1S1S3

Drug Names

Generic Name 藥物化學名稱	HA Code 藥物代碼	Legal Classification法律藥物分類	Brand Name 品牌名稱
Perindopril Tertbutylamine Tab 2mg	PERI28	P1S1S3	ACERTIL AR Tablet 5mg
Perindopril Tertbutylamine Tab 4mg	PERI17	P1S1S3	ACERTIL AR Tablet 10mg
Perindopril Arginine Tab 5mg	PERI29	P1S1S	ACERTIL PLUS TAB 2.5mg/0.625mg (perindopril arginine 5 mg, indapamide 0.625mg)
Perindopril Arginine Tab 10mg			ACERTIL PLUS TAB 5MG/1.25MG (perindopril arginine 5 mg, indapamide 1.25mg)
			ACERTIL PLUS TAB 10mg/2.5mg (perindopril arginine 10 mg, indapamide 2.5mg)

Mechanism of Action

Perindopril is an inhibitor of angiotensin-I 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. Perindopril is used in the treatment of hypertension and heart failure. Perindopril helps to reduce the risk of future strokes and heart attacks. It also improves your survival if you are taking it following a heart attack or heart surgery. It works by widening your blood vessels and making it easier for your heart to pump blood around your body. This can improve the symptoms of heart failure.

Perindopril can be used alone or in combination with other antihypertensive agent such as indapamide.

Route of Administration

Perindopril is administered orally in a single daily dose

Dosage

Dose for perindopril Tertbutylamine

• Hypertension - 4mg once a day (the maximum dose is 8 mg once daily)
• Heart failure – 4mg once a day
• After a heart attack – 8mg once a day

Dose for perindopril Arginine

• Hypertension - 5mg once a day (the maximum dose is 10 mg once daily)
• Heart failure – 5mg once a day
• After a heart attack – 10mg once a day

When will I feel better?

Perindopril starts to work within a few hours to reduce high blood pressure, but it may take up to a month to achieve its full effect.

If you are taking perindopril for heart failure, it may take weeks, even months, before you feel better.

Side Effects

System Organ Class	Frequency	Adverse reactions
Nervous system disorder	Common	Dizziness, headache, vertigo
	Uncommon	Confusion
Respiratory disorders	Common	Dry, tickly (non-productive) cough, dyspnoea
Eye disorders	Common	Visual disturbances
Ear disorders	Common	tinnitus
Skin disorders	Common	Itching , rash
	uncommon	oedema of the face, extremities, lips, tongue, glottis, and/or larynx
Gastro-intestinal disorders	Common	Nausea, vomiting, diarrhoea, abdominal pain, dyspepsia, constipation
	Uncommon	Dry mouth
	Rare	pancreatitis
	Very rare	Glossitis, pancreatitis
		Cardiac disorders	Uncommon	Palpitations, tachycardia
		Vascular disorder	common	Hypotension
		Uncommon	vasculitis
		Rare	flushing
Musculoskeletal disorders	Common	Muscle cramps
General disorder	Common	asthenia

Pharmacokinetics

Perindopril acts through its active metabolite, perindoprilat.

After oral administration, the absorption of perindopril is rapid and the peak concentration complete within 1 hour. The plasma half-life of perindopril is equal to 1 hour.

Perindopril is a pro-drug. About 27 % of the total quantity of perindopril absorbed is converted into perindoprilat, the active metabolite. The peak plasma concentration of perindoprilat is achieved within 3 to 4 hours.

As ingestion of food decreases conversion to perindoprilat, hence bioavailability, perindopril should be administered orally in a single daily dose in the morning before breakfast.

Elimination

Perindopril is eliminated in the urine and the half-life of the unbound fraction is approximately 17 hours, resulting in steady state within 4 days.

Special population

Elimination of perindoprilat is decreased in the elderly, and also in patients with heart or renal failure. Dosage adjustment in renal insufficiency is desirable depending on the degree of impairment (creatinine clearance).

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 perindopril in the morning.

PREGNANCY should be avoided in pregnancy unless essential.

BREAST FEEDING not recommended.

HEPATIC IMPAIRMENT Perindopril is a prodrug and requires close monitoring in patients with hepatic impairment.

RENAL IMPAIRMENT

For perindopril tertbutylamine:

Max. initial dose 2mg once daily if eGFR 31-60 ml/minute/1.73 m2

2 mg once daily on alternate days if eGFR 15-30 ml/minute/1.73 m2

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 Interaction:

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.

Co-trimoxazole (trimethoprim/sulfamethoxazole): taking concomitant co-trimoxazole may be at increased risk for hyperkalaemia

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)

FAQ

How should I take the tablet?

You will usually take perindopril once a day.

Swallow perindopril tablet whole with a drink of water.

Your doctor may suggest that you take your first dose before bedtime because it can make you feel dizzy. After the very first dose, if you do not feel dizzy, take perindopril in the morning, ideally 30 to 60 minutes before breakfast.

What should I avoid while taking?

Should avoid potassium rich foods: 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 happen if I miss a dose?

If you forget to take a dose and you usually take perindopril:

• 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.