Ramipril

Cardiovascular Drug

Drug class: Angiotensin Converting Enzyme Inhibitors, ACEI

Ramipril (TRITACE)（中文：雷米普利）

Pronunciation

Ramipril 10mg

Ramipril 2.5mg

Ramipril 5mg

Common Strengths of Ramipril

Ramipril is available in the following strengths:

• 2.5 mg
• 5 mg

Drug Trade Names of Ramipril

The brand names for metoprolol is Tritace.

Mechanism of Action

Ramipril is an inhibitor of angiotensin 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.

Ramipril is used in the treatment of hypertension and heart failure. Ramipril helps to reduce the risk of future strokes and heart attacks. It also improves your survival if you are taking it following for heart attack or after a heart attack.

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.

Route of Administration

Ramipril is administered orally in a single daily dose.

Dosages

Depending on why you are taking ramipril, the usual starting dose is between 1.25mg and 2.5mg once a day.

• Hypertension
  • 2.5 mg to 5 mg once a day
• Heart failure
  • 5 mg twice a day or 10 mg once a day
• Kidney disease (nephropathy)
  • 5 mg or 10 mg once a day

The maximum dose is 5 mg twice a day or 10 mg once a day.

When will I feel better?

The antihypertensive effect becomes apparent 1 to 2 hours after oral administration. The peak effect of a single dose is usually reached 3 to 6 hours after oral administration. The antihypertensive effect of a single dose usually lasts for 24 hours. The maximum antihypertensive effect of continued treatment with ramipril is generally apparent after 3 to 4 weeks. If you are taking Ramipril for heart failure, it may take weeks, even months, before you feel better.

Side Effects

Frequency	Adverse reactions
Common (≥1/100 to <1/10)	Dizziness
	Headache
	Vertigo
	Dry
	Tickly (non-productive) cough
	Dyspnoea
	Bronchitis
	Sinusitis
	Itching
	Rash
	Nausea
	Vomiting
	Diarrhea
	Abdominal pain
	Dyspepsia
	Hypotension
	Muscle cramps
Uncommon (≥1/1,000 to <1/100)	Visual disturbances including blurred vision
	Angioedema
	Dry mouth
	Constipation
	Palpitations
	Tachycardia
	Flushing
Rare (≥1/10,000 to <1/1,000)	Confusion
	Tinnitus
	Glossitis
	Vasculitis

Pharmacokinetics

Following oral administration ramipril is rapidly absorbed from the gastrointestinal tract: peak plasma concentration is reached within 1 hour. Based on urinary recovery, the extent of absorption is at least 56% and is not significantly influenced by the presence of food in the gut. The bioavailability of the active metabolite ramiprilat after oral administration of 2.5 mg and 5 mg ramipril is 45%.

Peak plasma concentrations of ramiprilat are reached 2-4 hours after ramipril intake. Steady state plasma concentrations of ramiprilat after once daily dosing with the usual doses of ramipril are reached by about the fourth day of treatment.

Metabolism

• Ramipril is almost completely metabolized to ramiprilat.

Elimination

• Excretion of the metabolites is primarily renal. After multiple once-daily doses of ramipril, the effective half-life of ramiprilat was 13-17 hours.

Special population

• Patients with renal impairment
  • Renal excretion of ramiprilat is reduced in patients with impaired renal function, and renal ramiprilat clearance is proportionally related to creatinine clearance.
• Patients with hepatic impairment
  • In patients with impaired liver function, the metabolism of ramipril to ramiprilat was delayed, and plasma ramipril levels in these patients were increased.

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 ramipril in the morning.

Pregnancy

Should be avoided in pregnancy unless essential.

Breast Feeding

Not recommnded.

Hepatic Impairment

• Max. daily dose 2.5mg.
• Ramipril is a prodrug and requires close monitoring in patients with hepatic impairment.

Renal Impairment

• If eGFR 31-60 ml/minute/1.73 m2
  • Max. daily dose 5mg
• If eGFR < 30ml/minute/1.73 m2
  • Max. initial dose 1.25 mg once daily (do not exceed 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 Ramipril.
• 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 hyperkalemia

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?

You will usually take ramipril once or twice a day. Swallow ramipril tablet whole with a drink of water, with or without food. 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 ramipril at the same time every day.

What should I avoid while taking?

Should avoid potassium rich foods: ramipril 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 ramipril:

• 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.
• Twice a day: Take it as soon as you remember unless it is less than 4 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.