培哚普利
培哚普利 (Perindopril) 是 血管緊張素轉換酶抑制劑(Angiotensin-converting enzyme inhibitor, ACEI)
作用來自對 「腎素-血管緊張素-醛固酮 (RAA) 系統」的抑制。
腎素 (renin) 是一種由腎臟合成的酶並釋放到血液循環中，將血管緊張素原 (angiotensinogen) 轉化為血管緊張素-I (angiotensin-I)。然後血管緊張素-I (angiotensin-I) 被血管緊張素轉化酶 (angiotensin-converting enzyme, ACE) 轉化為血管緊張素-II (angiotensin-II)。血管緊張素-II 是一種高效的血管收縮劑，負責動脈血管收縮和血壓升高以及刺激腎上腺分泌醛固酮 (aldosterone)。
ACE 的抑制導致血管緊張素-II 水平降低，從而導致血壓降低和醛固酮分泌減少。後者的降低導致血清鉀濃度增加。
用於治療高血壓和心力衰竭。有助於降低中風和心臟病發作的風險。在心臟手術後服用，還可以提高生存率。這是透過擴張血管，讓心臟更容易將血液泵送到身體周圍，改善心力衰竭的症狀。
可單獨使用或與其他抗高血壓藥物聯合使用，例如吲達帕胺 (indapamide)。
給藥途徑: 培哚普利 (Perindopril) 是口服每日一次。
| Generic Name 藥物學名 | Perindopril |
|---|---|
| Class: | Cardiovascular Drug |
| Subclass: | ACE inhibitor |
| HK Legal Classification香港法律藥物分類 | P1S1S3 |
Drug Names
| Generic Name 藥物化學名稱 | HA Code 藥物代碼 | HK Legal Classification香港法律藥物分類 | Brand Name 品牌名稱 |
|---|---|---|---|
| Perindopril Tertbutylamine Tab 2mg | PERI28 | P1S1S3 | ACERTIL AR Tablet 5mg
ACERTIL AR Tablet 10mg ACERTIL PLUS TAB 2.5mg/0.625mg (perindopril arginine 5 mg, indapamide 0.625mg) 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) |
| Perindopril Tertbutylamine Tab 4mg | PERI17 | P1S1S3 | |
| Perindopril Arginine Tab 5mg | PERI29 | P1S1S3 | |
| Perindopril Arginine Tab 10mg |
Mechanism of Action
The beneficial effects of ACE inhibitors appear to result primarily from the suppression of the plasma renin-angiotensin-aldosterone (RAA) system. Renin is an enzyme 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 (ACE) 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 level, which leads to decreased vasopressor activity and to reduced aldosterone secretion. The latter decrease results 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 agents 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 effects.
If you are taking perindopril for heart failure, it may take weeks, even months, before you feel better.
Side Effects
The following definitions of frequencies are used:
Very common ≥ 1/10
Common ≥ 1/100 to < 1/10
Uncommon ≥ 1/1,000 to < 1/100
Rare ≥ 1/10,000 to < 1/1,000
Very rare < 1/10,000
| 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 | |
| Very rare | Glossitis, pancreatitis | |
| Cardiac disorders | Uncommon | Palpitations, tachycardia |
| Vascular disorders | 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 is reached within 1 hour. The plasma half-life of perindopril is about 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 Perindopril should be avoided in pregnancy.
BREAST FEEDING Perindopril is not recommended.
HEPATIC IMPAIRMENT Perindopril is a prodrug, and its use 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 Perindopril.
Potassium sparing diuretics (triamterene, amiloride and spironolactone) or potassium supplement: may cause significant increase in serum potassium levels, resulting in hyperkalaemia.
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)
- Use with care in patients with bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney (risk of acute renal failure)
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 and 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: perindopril 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:
- 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 dose.
