Lopirel PLUS Tablet

What is Lopirel Plus?

Lopirel Plus is a fixed-dose combination antiplatelet medication containing Clopidogrel 75 mg and Aspirin 75 mg, manufactured by Incepta Pharmaceuticals Ltd. It is used to reduce the risk of myocardial infarction and stroke in patients with acute coronary syndrome, recent MI, recent stroke, or established peripheral arterial disease.

Indications

Acute Coronary Syndrome (ACS): Indicated to reduce the rate of myocardial infarction (MI) and stroke in patients with non-ST-segment elevation ACS (unstable angina/NSTEMI) and acute ST-elevation ACS (STEMI).
Recent MI, Recent Stroke, or Established Peripheral Arterial Disease: Indicated to reduce the rate of MI and stroke in these patients.

Pharmacology

Clopidogrel: A prodrug that inhibits platelet activation and aggregation through irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets. Dose-dependent inhibition is seen 2 hours after a single oral dose, reaching steady state between Day 3 and Day 7 with repeated 75 mg daily doses. Extensively metabolized by the liver; the main circulating metabolite (carboxylic acid derivative) has no antiplatelet effect and represents about 85% of circulating drug-related compounds. Approximately 50% is excreted in urine and 46% in faeces within 5 days. Elimination half-life of the main metabolite is 8 hours.
Aspirin: Inhibits platelet aggregation through irreversible inhibition of platelet cyclooxygenase, thereby blocking generation of thromboxane A2, a powerful inducer of platelet aggregation and vasoconstriction.

Dosage & Administration

The recommended dose of Clopidogrel is 75 mg once daily with or without food; no dosage adjustment is necessary for elderly or renally impaired patients. For acute coronary syndrome (unstable angina/non-Q-wave MI), initiate with a single 300 mg Clopidogrel loading dose, then continue at 75 mg once daily. Aspirin 75-325 mg once daily should be initiated and continued in combination with Clopidogrel. Most patients with ACS also receive heparin acutely.

Interaction

Aspirin: Does not modify Clopidogrel-mediated inhibition of ADP-induced platelet aggregation; Clopidogrel potentiates aspirin's effect on collagen-induced platelet aggregation.
Heparin: No dose modification needed; co-administration does not affect inhibition of platelet aggregation induced by Clopidogrel.
NSAIDs: Associated with increased occult gastrointestinal blood loss; co-administer with caution.
Warfarin: Safety of co-administration has not been established; undertake with caution.

Contraindications

Contraindicated in hypersensitivity to the drug substance or any component of the product, and in active pathological bleeding such as peptic ulcer or intracranial hemorrhage.

Side Effects

Lopirel Plus is generally well tolerated.

Pregnancy & Lactation

Clopidogrel: No adequate and well-controlled studies exist in pregnant women; use only if clearly needed, and only during the first and second trimesters. Unknown whether excreted in human breast milk.
Aspirin: Contraindicated during the third trimester of pregnancy. Known to be excreted in human milk. This drug should be discontinued during breastfeeding.

Precautions & Warnings

May prolong bleeding time. Thrombotic Thrombocytopenic Purpura (TTP) has been reported rarely following use. Reye's syndrome may develop in individuals with chicken pox, influenza, or flu symptoms. Hypersensitivity reactions including rash, angioedema, or hematologic reactions have been reported.

Use in Special Populations

Should not be given to children, particularly those under 12 years, unless expected benefits outweigh possible risks; Aspirin may contribute to Reye's syndrome in some children.

Overdose Effects

Clopidogrel overdose may lead to bleeding complications; platelet transfusion may help restore clotting ability. Moderate Aspirin intoxication may cause dizziness, headache, tinnitus, confusion, and gastrointestinal symptoms, treatable by inducing vomiting followed by gastric lavage if needed. Severe Aspirin intoxication can cause respiratory alkalosis, respiratory/metabolic acidosis, hyperthermia, perspiration, and dehydration, treatable with haemodialysis and symptomatic treatment.

Therapeutic Class

Anti-platelet Drug

Storage Conditions

Keep in a cool and dry place (below 30°C), protected from light and moisture. Keep out of reach of children.