Ramipril

BRAND NAMES

Altace HCT – It contains the active ingredient of ramipril. It is available in the form of capsules used to treat heart attacks, stroke, or heart failure.

Altace- It contains the active ingredient of ramipril. It is available in capsules to treat high blood pressure by reducing or relaxing blood vessels.

MECHANISM OF ACTION

Ramipril and its active metabolite, ramiprilate, function as ACE inhibitors, inhibiting circulation and tissue ACE. The inhibition lowers angiotensin Ⅱ formulation. As a result, sympathetic activity reduces, as does sodium and water reabsorption by the kidneys. The smooth muscle in the arterioles relaxes, resulting in lower blood pressure. ACE also helps to break down bradykin, a vasopressor agent. The increased bradykinin levels induced by ACE inhibition may contribute to ramipril's therapeutic benefits.

PHARMACOKINETICS

Absorption

Ramipril is readily available in capsule or tablet form for oral administration. The maximum plasma concentration in the therapeutic window is typically reached within 1 hour. The bioavailability of ramipril is approximately 50% to 60%.

Distribution

Ramipril is predominantly metabolized to its active form, ramiprilat and both substances exhibit significant plasma protein binding. The plasma protein binding. 

Metabolism

Removing the ester group from ramipril converts it to its active metabolite, ramiprilat. Additionally, the glucuronidation of both ramipril and ramiprilate produces inactive metabolites. Ramipril is not a substrate, inhibitor, or inducer of cytochrome P450 enzymes. 

Excretion

Ramipril is primarily excreted from the body through urine and stool.

PHARMACODYNAMICS

AACE inhibitors impede the fast conversion of ATI to ATII and prevent RAAS-induced blood pressure rises. ACE is also involved in the enzymatic inactivation of bradykinin, a vasodilator. Inhibiting bradykinin deactivation raises bradykinin levels, which may prolong the benefits of ramiprilat by increasing vasodilation and lowering blood pressure.

DOSAGE AND ADMINISTRATION

Ramipril comes as a capsule to take by orally. It is usually taken once or twice a day with or without food. 

Ramipril is available in capsules with a strength of 1.25mg, 2.5 mg, 5mg, and 10mg.

DRUG INTERACTIONS

Drug interaction with ramipril may include

Severe heart failure – valsartan

Pain killers – aspirin, naproxen and ibuprofen

PDE5 inhibitors – sildenafil

Gout drugs – allopurinol

Anti-diabetics – sitagliptin, metaformin, and insulin

Diuretics – furosemide

Corticosteroids – prednisolone

Anti-counvulsant - pregabalin

CONTRAINDICATIONS

Other ACE inhibitors or drugs for hypersensitivity should not be taken with ramipril. In patients with diabetes or renal impairment, do not co-administer aliskiren. It is not advisable to take ramipril when expecting. Pregnancy-related oligohydramnios and malformations of the skull have been related to the concurrent use of an ACE inhibitor. 

SIDE EFFECTS

Side effects of ramipril may include

•        Cough

•        Dizziness

•        Headache

•        Stomach upset

•        Weakness

•        Excessive tiredness

Serious side effects may include

•        Hoarseness

•        Swelling of the face, throat, tongue, lips, eyes

•        Fever, sore throat and other infections

•        Yellowing of the skin or eye

OVERDOSE

Symptoms of overdose may include

•        Lightheadedness

•        Fainting

•        Peripheral vasodilation

•        Bradycardia

•        Electrolyte disturbances

•        Renal failure

TOXICITY

Ramipril overdose can lead to several hypotension, primarily attributed to vasodilation and effective hypovolemia. Monitoring the patients for at least 6 hours after the overdose is essential. If the blood pressure remains stable and normal during the first 6 hours after exposure, the patients can be considered for discharge.