#hematological agent

Brand Name: Plavix

Generic Available

Common Dosage Forms:

Tablets: 75 mg and 300 mg

FDA Interactions/Dosages:

For the reduction of atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease: The recommended dose is 75 mg once daily with or without food.

For the reduction of atherosclerotic events in patients with acute coronary syndrome including unstable angina and non-Q-wave myocardial infarction: Therapy should start with a 300 mg loading dose and then continued at 75 mg once a day. Aspirin (75 mg - 325 mg) should be initiated and continued in combination with clopidogrel. Most patients will also be treated acutely with heparin.

Pharmacology/Pharmacokinetics Clopidogrel is converted by CYP2C19 to its active metabolite which inhibits platelet aggregation by irreversibly modifying platelet receptors thereby selectively inhibiting the binding of adenosine diphosphate (ADP) to the receptor. This results in an inhiation of the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex and an inhibition of platelet aggregation. Patients who are CYP2C19 poor metabolizers can be identified through genotype testing. Clinical effects are seen 2 hours after an oral dose and a steady state of platelet aggregation occurs after 3 to 7 days. Clopidogrel and its active metabolite are bound to plasma proteins (98% and 94% respectively).

Drug Interactions: Use may predispose occult blood loss in patients taking NSAIDs. Clopidogrel inhibits CYP2C9 enzyme therefore it may interfere with the metabolism of phenytoin, tamoxifen, tolbutamide, warfarin, torsemide, fluvastatin, and NSAIDs. Omeprazole and esomeprazole may decrease effects.

Contraindications/Precautions: Contraindicated in active pathological bleeding such as peptic ulcer or intracranial hemorrhage. Use with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions. Use with caution in patients with severe hepatic disease. Rare cases of thrombotic thrombocytopenic purpura (TTP) have been reported in patients taking clopidogrel. Most TTP patients present with initial nonspecific complaints of fatigue, weakness, anorexia, nausea, diarrhea, and abdominal pain. Clopidogrel is excreted in breast milk of studied rats. DO NOT USE IN PATIENTS IDENTIFIED WITH TWO LOSS-OF-FUNCTION ALLELES OF THE CYP2C19 GENES. Pregnancy Category B.

Adverse Effects: Upper respiratory tract infection (8.7%), chest pain (8.3%), headache (7.6%), flu-like symptoms (7.5%), arthralgia (6.3%), dizziness (6.2%), back pain (5.8%), abdominal pain (5.6%), purpura (5.3%), dyspepsia (5.2%), diarrhea (4.5%), dyspnea (4.5%), rhinitis (4.2%), rash (4.2%), hypertension (4.3%), edema (4.1%), bronchitis, coughing, urinary tract infection, pruritus, depression, nausea, epistaxis, and fatigue (<4%).

Patient Consultation:

Contact your physician if the above side effects are severe or persistent.

Contact your physician if you notice any indication of infection including fever, chill, or sore throat (neutropenia) or signs of TTP including fatigue, weakness, anorexia, nausea, diarrhea, and abdominal pain.

Can be taken without regard to meals.

Bleeding time will be increased during therapy--report unusual bleeding to your physician.

Tell your physician and dentists about your therapy before elective surgery.

Do not exceed prescribed dosage; take medication only as directed.

Do not take over-the-counter omeprazole products wile on clopidogrel.

Common Brand Name: Eliquis

Common Dosage Forms:

Tablets: 2.5 mg and 5 mg

FDA Indications/Dosages:

For the reduction of risk of stroke and systemic embolism in nonvalvular atrial fibrillation: 5 mg twice daily. Use the 2.5 mg twice daily in patients with two of the following; age ≥ 80 years, weight ≤ 60 kg, or serum creatinine ≥ 1.5 mg/dL.

For the prophylaxis of DVT following hip or knee replacement surgery: 2.5 mg twice daily.

For the treatment of DVT and PE: 10 mg twice daily for 7 days followed by 5 mg twice daily.

Reduction in the risk of recurrent DVT and PE following initial therapy: 2.5 mg twice daily.

Pharmacology/Pharmacokinetics: Apixaban is a selective inhibitor of Factor Xa (FXa). Through inhibition of FXa, apixaban decreases thrombin and thrombus formation. Oral bioavailability is approximately 50% with no effect from food. Cmax occurs about 3 to 4 hours post oral dose and with an apparent half-life of 12 hours. Metabolism occurs in the liver primarily via CYP3A4. Renal elimination accounts for about 27% of  the total clearance.

Drug Interactions: Apixaban exposure is increased by strong dual inhibitors of CYP3A4 and P-gp such as ketoconazole, itraconazole, ritonavir, or clarithromycin. Exposure is decreased by CYP3A4 inducers such as rifampin, carbamazepine, phenytoin, and St. John’s Wort. Coadministration with anticoagulants and antiplatelets increases the risk of bleeding adverse effects.

Contraindications/Precautions: Contraindicated in patients with active pathological bleeding. PREMATURE DISCONTINUATION OF THERAPY INCREASES THE RISK OF THROMBOTIC EVENTS. USE CAUTION IN PATIENTS UNDERGOING SPINAL/EPIDURAL ANESTHESIA, ESPECIALLY THOSE WITH INDWELLING EPIDURAL CATHETERS. Not recommended for use in patients with prosthetic heart valves. Pregnancy Category B.

Adverse Effects: Adverse effects are uncommon and are primarily composed of bleeding events such as contusion, hemorrhage, hematoma, and gingival bleeding.

Patient Consultation:

May be taken without regard to food.

Do not discontinue without first consulting your physician.

Inform your physician of any upcoming surgical procedures.

Do not take aspirin, NSAIDs, or other drugs that increase your risk of bleeding.

Contact your physician if you experience any signs or symptoms of unusual bleeding such as nose bleeds, bleeding gums, pink or brown urine, red or black stools, coughing or vomiting blood, headaches, or dizziness.