Ramipril: Difference between revisions
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==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. | |||
<u>Metabolism</u> | |||
Ramipril is almost completely metabolized to ramiprilat. | |||
<u>Elimination</u> | |||
Excretion of the metabolites is primarily renal. After multiple once-daily doses of ramipril, the effective half-life of ramiprilat was 13-17 hours. | |||
<u>Special population</u> | |||
<u>''Patients with renal impairment</u> | |||
Renal excretion of ramiprilat is reduced in patients with impaired renal function, and renal ramiprilat clearance is proportionally related to creatinine clearance. | |||
<u>''Patients with hepatic impairment</u> | |||
In patients with impaired liver function, the metabolism of ramipril to ramiprilat was delayed, and plasma ramipril levels in these patients were increased. | |||
Revision as of 01:43, 22 August 2022
Pronunciation
Ramipril 10mg
Ramipril 2.5mg
Ramipril 5mg
| Generic Name: | Ramipril |
|---|---|
| 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 |
|---|---|---|---|
| Ramipril Tablet 2.5mg | RAMI01 | P1S1S3 | TRITACE |
| Ramipril Tablet 5mg | RAMI02 | P1S1S3 | TRITACE |
Mechanism of Action
Ramipril 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. 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
Dosage
Depending on why you are taking ramipril, the usual starting dose is between 1.25mg and 2.5mg once a day.
- Hypertension – 2.5mg to 5mg once a day
- Heart failure – 5mg twice a day of 10mg once a day
- Kidney disease (nephropathy) – 5mg or 10mg once a day
The maximum dose is 5mg twice a day or 10mg 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 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, bronchitis, sinusitis |
| Eye disorders | Common | Visual disturbances including blurred vision |
| Ear disorders | Rare | tinnitus |
| Skin disorders | Common | Itching , rash |
| uncommon | angioedema | |
| Gastro-intestinal disorders | Common | Nausea, vomiting, diarrhoea, abdominal pain, dyspepsia, |
| Uncommon | Dry mouth, constipation | |
| Rare | pancreatitis | |
| rare | glossitis | |
| Cardiac disorders | Uncommon | Palpitations, tachycardia |
| Vascular disorder | common | Hypotension |
| Uncommon | flushing | |
| Rare | glossitis | |
| Vascular disorder | Common | Hypotension |
| Uncommon | flushing | |
| Rare | vasculitis | |
| Musculoskeletal disorders | Common | Muscle cramps |
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.
