Lisinopril is a prescription medication used primarily to treat high blood pressure (hypertension), heart failure, myocardial infarction, and diabetic neuropathy and to improve survival after a heart attack. It belongs to a class of drugs called ACE inhibitors (Angiotensin-Converting Enzyme inhibitors). Lisinopril received its initial approval from the U.S. Food and Drug Administration (FDA) in 1988. It was introduced to the market under the brand name Prinivil by Merck and Zestril by AstraZeneca. In 1995, the FDA approved additional tablet strengths of Zestril, including 2.5 mg, 10 mg, 20 mg, and 40 mg formulations.

BRAND NAMES:

Zestril-The main active ingredient in Zestril is Lisinopril, which is available in tablets in strengths of 2.5mg, 10mg, 20mg, and 40mg.

Prinivil- These are available in tablets with strengths 5mg, 10mg, and 20mg containing Lisinopril as the main active ingredient.

MECHANISM OF ACTION:

Lisinopril functions as a competitive inhibitor of angiotensin-converting enzyme (ACE), hindering the conversion of angiotensin I into angiotensin II, a potent vasoconstrictor. The reduction in angiotensin II levels leads to decreased aldosterone secretion, which in turn lowers sodium reabsorption in the renal collecting ducts and reduces potassium excretion. Consequently, this may cause a slight increase in serum potassium levels.

PHARMACOKINETICS:

Absorption: Lisinopril has low bioavailability, ranging from 10% to 30%. The time to peak concentration can vary from 6 to 8 hours. Food does not affect the Lisinopril.

Distribution:  The volume of distribution for Lisinopril is ˜0.5-0.8 L/kg.

Metabolism: It is not metabolized in the liver.

Elimination: Lisinopril is mainly excreted unchanged in the urine.

PHARMACODYNAMICS:

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor with effects primarily on the renin-angiotensin-aldosterone system (RAAS), which regulates blood pressure, fluid balance, and vascular resistance.

DOSAGE AND ADMINISTRATION:

Lisinopril is available as 2.5mg, 5mg, 10mg, 20mg, 30mg, and 40mg oral tablets and as a 1mg/ml oral solution. The dose recommended for patients depends on various health conditions.

  • For Hypertension, in adults, the recommended initial dose is 10 mg daily, which gradually can be increased up to 40 mg daily.
  • If adequate blood pressure control is not achieved with Lisinopril alone, a low-dose diuretic can be added.
  • For Heart failure, the recommended initial dose is 2.5mg daily, with a maximum daily dose of 40mg.
  • For Myocardial Infarction, the recommended initial dose is 2.5 to 5 mg daily, with a slow titration to 40 mg daily.
  • For Diabetes and Hypertension, the recommended initial dose is 2.5 to 10 mg daily, depending on blood pressure, and slowly titrated to a maximum daily dose of 40 mg.

DRUG INTERACTIONS:

While taking Lisinopril, it is needed to discuss with the doctor if the patient is taking any other medicines for other health conditions. This is because few medicines interact with Lisinopril and can cause adverse effects. Below are the medicines that should be avoided while taking Lisinopril.

  • Heart Failure Medicines: Sacubitril, Valsartan
  • Anti-diabetic Medicines: Sitagliptin, Metformin, Insulin glargine.
  • Erectile Dysfunction: Sildenafil
  • Anti-gout Medicines: Allopurinol
  • Depression medicines: Lithium supplements
  • Anti-hypertensive medication: Aliskiren
  • NSAIDS: Aspirin, naproxen, indomethacin, ibuprofen

FOOD INTERACTIONS:

Avoid taking alcohol.

CONTRAINDICATIONS:

Lisinopril is contraindicated in patients with angioedema, congestive heart failure, anti-hemodialysis, low blood pressure, Hyperkalemia, liver diseases, and kidney dysfunction.

ADVERSE EFFECTS:

  • Hyperkalemia
  • Hypotension
  • Sinusitis
  • Dizziness
  • Nausea
  • Headache
  • Weakness
  • Kidney problems
  • Muscle pain
  • Skin rash
  • Diarrhea
  • Chest pain

OVERDOSE:

Taking an overdose of Lisinopril can cause severe toxic effects like

  • Severe hypotension
  • Dizziness or fainting
  • Bradycardia
  • Shock
  • Acute kidney injury
  • Hyperkalemia
  • Fatigue, confusion, or weakness
Image
76547-98-3
CAS Number
76547-98-3 (freebase)
Alternate CAS Number
3915-83-7 (2HCl salt) ; 328395-62-6 (Hydrate salt)
CAS Number
83915-83-7 (2HCl salt)
CAS Number
328395-62-6 (Hydrate salt)
CAS Number
104-15-4;
Alternate CAS Number
6106-44-8 (Potassium salt)
CAS Number
85955-59-5(freebase)
Alternate CAS Number
1356019-70-9(Na Salt)
CAS Number
STD- 76547-98-3: IMP-G- 1356839-89-8