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Lisinoril Information and Side Effect

Lisinopril is a medication of the angiotensin-converting enzyme (ACE) inhibitor class used to treat high blood pressure, heart failure, and after heart attacks. For high blood pressure (hypertension) it is usually a first line treatment, although in black people calcium-channel blockers or thiazide diuretics work better. Hypertension, also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. Hypertension is risk to brain, hearth, blood vessel and kidneys. Lisinopril has been use to treat hearth failure in adult and improve health quality after hearth attack. Lisinopril is an ACE inhibitor, meaning it blocks the actions of angiotensin-converting enzyme (ACE) in the renin–angiotensin–aldosterone system (RAAS), preventing angiotensin I from being converted to angiotensin II. Angiotensin II is a potent direct vasoconstrictor and a stimulator of aldosterone release. Reduction in the amount of angiotensin II results in relaxation of the arterioles. 



Lisinopril is generic drug and available in several brands such as Zestril, Prinivil and Qbrelis.

Drug Fact

Class : ACE Inhibitor

Category : Prescription Drug

Uses : treat high blood pressure, heart failure, and after heart attacks

Consumed by : Adult and child with age 6 years or above

Pregnancy category :  D 

Category D: There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). There is no evidence of breast milk absorption. If you are breastfeeding, do not use this medication without first consulting your doctor 

Administration

May be taken with or without food.

Contraindications

History of angioedema related to previous ACE inhibitor treatment, hereditary or idiopathic angioedema. Concomitant use with aliskiren especially in patients with diabetes mellitus or renal impairment (GFR<60 mL/min/1.73 m2). Concomitant use with sacubitril. Pregnancy.

Special Precautions

Patient with severe aortic stenosis, hypertrophic cardiomyopathy, CV disease (e.g. ischaemic heart disease) collagen vascular disease, ascites, unstented unilateral and bilateral renal artery stenosis. Patients undergoing major surgery or during anaesthesia. Black race. Desensitisation treatment (e.g. hymenoptera venom). Renal and hepatic impairment. Lactation. Children.

Adverse Reactions

Significant: Hyperkalaemia, hypotension, cholestatic jaundice, chest pain, syncope, cough, haematologic effects (e.g. neutropenia, anaemia, thrombocytopenia).

Cardiac disorders: Tachycardia, palpitations.

Ear and labyrinth disorders: Tinnitus.

Gastrointestinal disorders: Nausea, diarrhoea, vomiting, abdominal pain, dry mouth, constipation.

General disorders and admin site conditions: Fatigue, asthenia.

Immune system disorders: Intestinal angioedema.

Investigations: Elevated serum creatinine, BUN increased.

Metabolism and nutrition disorders: Electrolyte imbalance.

Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.

Nervous system disorders: Headache, vertigo, paresthesia, taste disturbance, dizziness.

Psychiatric disorders: Hallucinations, mood alterations, sleep disturbance, drowsiness.

Renal and urinary disorders: Renal dysfunction, oliguria, anuria.

Reproductive system and breast disorders: Impotence, gynaecomastia.

Respiratory, thoracic and mediastinal disorders: Rhinitis, sinusitis, dyspnoea.

Skin and subcutaneous tissue disorders: Pruritus, rash, psoriasis.

Vascular disorders: Raynaud’s phenomenon, flushing.

Potentially Fatal: Anaphylactoid reactions (e.g. angioedema of face, lips, tongue, and extremities), arrhythmia, severe hypotension. Rarely, fulminant hepatic necrosis.

Patient Counseling Information

This drug may cause occasional dizziness, if affected, do not drive or operate machinery.

Monitoring Parameters

Monitor BP, heart rate, BUN, CBC with differential LFT, serum K, and creatinine levels. Assess for signs of angioedema.

Over dosage

Symptoms: Hypotension, circulatory shock, tachycardia, palpitations, bradycardia, hyperventilation, renal failure, electrolyte disturbances, anxiety, dizziness and cough. Management: Administer IV infusion NaCl 0.9%. May perform gastric lavage if ingestion is recent. If hypotension occurs, place the patient in shock position. May also consider administration of angiotensin II infusion and/or IV catecholamines.

Drug Interactions

Increased hypotensive effect with antihypertensives, diuretics. Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, amiloride), K supplements, and drugs affecting serum K concentrations (e.g. trimethoprim, ciclosporin). May increase hypoglycaemic effect with insulin and oral hypoglycaemics agents. Concomitant use with NSAIDs including selective COX-2 inhibitors may result to renal function deterioration and reduced antihypertensive effect. May increase serum levels and toxicity of lithium. Coadministration with parenteral gold (e.g. Na aurothiomalate, aurothioglucose) may cause nitritoid reaction characterized by facial flushing, nausea, vomiting, and hypotension. Increased risk of angioedema with mammalian target of rapamycin (mTOR) inhibitors (e.g. temsirolimus, sirolimus, everolimus), tissue plasminogen activators (e.g. alteplase), neprilysin inhibitors (e.g. sacubitril) and neutral endopeptidase (NEP) inhibitors (e.g. racecadotril).

Potentially Fatal: Increased risk of hypotension, hyperkalaemia, and changes in renal failure with aliskiren. Increased risk of angioedema with neprilysin inhibitors (e.g. sacubitril). May cause anaphylactoid reactions with dextran sulfate in LDL apheresis.

Lab Interference

May result to false-negative aldosterone/renin ratio (ARR).

Action

Description: Lisinopril, a peptidyl dipeptidase inhibitor, is an ACE inhibitor which prevents conversion of angiotensin I to angiotensin II, thereby increasing plasma renin activity and decreasing aldosterone secretion.

Onset: Within 1-2 hours.

Duration: 24 hours.

Pharmacokinetics:

Absorption: Slowly and incompletely absorbed from the gastrointestinal tract. Bioavailability: Approx 25%. Time to peak plasma concentration: Approx 7 hours.

Distribution: Crosses placenta.

Excretion: Mainly via urine (unchanged drug). Elimination half-life: 12 hours.

Chemical Structure




Storage

Store between 15-30°C. Protect from moisture.

ATC Classification

C09AA03 - lisinopril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.


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