Pharmacology Drug Studies Flashcards

Question

Clorazepate

Answer 1

Generic: Clorazepate Brand: Tranxene Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: GAD Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid and well absorbed orally Metabolism: Hepatic Excretion: Primarily through urine Half-Life: 40-50 hours Dosage: 15-30mg/day Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 2

Generic: Diazepam Brand: Valium/Diastat Classification: Benzodiazepine, Antianxiety, Anticonvulsant MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Anxiety disorders, muscle spasms, seizure disorders, medication for procedures (sedation and amnesia). Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral, IV or IM. Pharmacokinetics: Absorption: Rapidly absorbed orally Metabolism: Hepatic via CYP2C19 and CYP3A4 Excretion: Primarily via urine Half-Life: 20-50 hours Dosage: 2-10mg orally, 2-4 times per day PRN. Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 3

Generic: Flurazepam Brand: Dalmane Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Insomnia Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral Pharmacokinetics: Absorption: Rapidly absorbed after oral administration Metabolism: Hepatic Excretion: Primarily through urine Half-Life: 2-3 hours Dosage: 15-30 mg PO qHs. Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 4

Generic: Lorazepam Brand: Ativan Classification: Benzodiazepine, Antianxiety MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Anxiety disorders, acute agitation, seizures, sedation for medical procedures. Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral, IV or IM. Pharmacokinetics: Absorption: Well absorbed orally Metabolism: Hepatic Excretion: Primarily in urine Half-Life: 10-20 hours Dosage: 1-3mg PO, 2-3 times per day, maximum 10mg/day. Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 5

Generic: Midazolam Brand: Versed Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Procedural sedation, seizures. Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: IV, IM, Oral, IN. Pharmacokinetics: Absorption: Rapid via IV and IM routes Metabolism: Hepatic (via CYP3A4) Excretion: Primarily via urine Half-Life: 1.5-3 hours Dosage: Initial: Under 50kg, 0,2 mg/kg (maximum 10 mg/dose), over 50kg under 70yrs, 10mg. over 50kg over 70 yrs 5mg. Additional if needed: Under 50kg, 0,1 mg/kg (maximum 5 mg/dose), over 50kg under 70yrs, 5mg. over 50kg over 70 yrs 2.5mg. Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 6

Generic: Nitrazepam Brand: Mogadon Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Insomnia, seizure disorders Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral Pharmacokinetics: Absorption: Well absorbed orally Metabolism: Hepatic (CYP3A4 involvement) Excretion: Primarily in urine Half-Life: 16-38 hours Dosage: 5-10mg PO qHs. Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 7

Generic: Oxazepam Brand: Serax Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Anxiety Disorders (Short-term treatment) Alcohol Withdrawal Syndrome Sedation (Pre-procedure or for insomnia) Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral Pharmacokinetics: Absorption: Rapidly absorbed following oral administration Metabolism: Hepatic Excretion: Primarily through urine Half-Life: 4-15 hours Dosage: 10-30 mg orally 2-3 times daily, max: 120 mg/day Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 8

Generic: Temazepam Brand: Restoril Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Insomnia Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Routes of Administration: Oral Pharmacokinetics: Absorption: Well absorbed orally Metabolism: Hepatic (CYP3A4) Excretion: Primarily in urine as metabolites Half-Life: 8-20 hours Dosage: 15mg PO qHs, max 30mg/day Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 9

Generic: Triazolam Brand: Halcion Classification: Benzodiazepine MOA: Enhances the effect of GABA, the brain's main inhibitory neurotransmitter resulting in reduced anxiety, sedation, muscle relaxation, anticonvulsant activity. Indications: Insomnia Contraindications: Hypersensitivity to benzodiazepines Severe respiratory insufficiency Sleep apnea syndrome Pregnancy Breastfeeding Routes of Administration: Oral Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract Metabolism: Hepatic (CYP3A4) Excretion: Primarily excreted in urine Half-Life: 1.5-5.5 hours Dosage: 0.125mg to 0.25mg PO qHs, max 0.5mg/day Adverse Effects: Drowsiness, dizziness, fatigue, confusion, memory impairment, depression, respiration depression, nausea, constipation. Drug Interactions: CNS Depressants (e.g., opioids, alcohol): Increased risk of respiratory depression and sedation Monitoring Parameters: Anxiety Symptoms: Assess for therapeutic effectiveness CNS Depression: Monitor for excessive sedation or confusion Respiratory Function: Watch for signs of respiratory depression

Answer 10

Generic: Sildenafil Brand: Viagra (ED) or Revatio (PAH) Classification: PDE5 inhibitor, Vasodilator MOA: selectively inhibits phosphodiesterase type 5 (PDE5), an enzyme that degrades cyclic guanosine monophosphate (cGMP). cGMP levels increase, leading to smooth muscle relaxation and vasodilation. In Viagra, this enhances blood flow to the penis, improving erectile function. In Revatio, this leads to pulmonary vasodilation, reducing pulmonary arterial pressure. Indications: ED, PAH Contraindications: Use of Nitrates (e.g., nitroglycerin, isosorbide dinitrate/mononitrate) → Can cause severe hypotension. Severe Cardiovascular Disease (e.g., recent MI, stroke, unstable angina). Severe Hypotension (<90/50 mmHg). Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid; onset within 30-60 minutes (Viagra), best taken on an empty stomach. Metabolism: Hepatic (CYP3A4, CYP2C9). Excretion: Feces (~80%) and Urine (~13%) Half-Life: ~3-5 hours. Dosage: 50mg PO for Viagra, 20mg PO TID for Revatio Adverse Effects: Common: Headache, flushing, dyspepsia (indigestion), nasal congestion. Cardiovascular: Hypotension, dizziness, palpitations. Vision Changes Priapism (Prolonged Erection >4 hours): Medical emergency, requires immediate intervention. Severe Hypotension: If combined with nitrates or alpha-blockers. Drug Interactions: Nitrates (e.g., Nitroglycerin, Isosorbide Dinitrate/Mononitrate): Life-threatening hypotension. Alpha-Blockers (e.g., Tamsulosin, Doxazosin): Increased risk of hypotension. Monitoring Parameters: Blood Pressure: Monitor for hypotension, especially in patients with cardiac disease. Vision & Hearing Changes: Patients should report sudden vision loss or hearing impairment. Cardiac Function: Assess for angina or arrhythmias in at-risk patients. Response to Treatment: For Viagra, check for improved erectile function; for Revatio, assess for symptom improvement in PAH.

Answer 11

Generic: Vardenafil Brand: Levitra Classification: PDE5 inhibitor, Vasodilator MOA: selectively inhibits phosphodiesterase type 5 (PDE5), an enzyme that degrades cyclic guanosine monophosphate (cGMP). cGMP levels increase, leading to smooth muscle relaxation and vasodilation. Indications: ED Contraindications: Use of Nitrates (e.g., nitroglycerin, isosorbide dinitrate/mononitrate) → Can cause severe hypotension. Severe Cardiovascular Disease (e.g., recent MI, stroke, unstable angina). Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, onset within 30-60 minutes. Metabolism: Hepatic Excretion: Primarily fecal (91-95%), renal (~2-6%). Half-Life: 4-5 hours. Dosage: 10mg PO for max dose: 20mg/day Adverse Effects: Common: Headache, flushing, dyspepsia (indigestion), nasal congestion. Cardiovascular: Hypotension, dizziness, palpitations. Vision Changes Priapism (Prolonged Erection >4 hours): Medical emergency, requires immediate intervention. Drug Interactions: Nitrates (e.g., Nitroglycerin, Isosorbide Dinitrate/Mononitrate): Life-threatening hypotension. Alpha-Blockers (e.g., Tamsulosin, Doxazosin): Increased risk of hypotension. Monitoring Parameters: Blood Pressure: Monitor for hypotension, especially in patients with cardiac disease. Vision & Hearing Changes: Patients should report sudden vision loss or hearing impairment. Cardiac Function: Assess for angina, arrhythmias, or recent CV events. Response to Treatment: Evaluate for improved erectile function.

Answer 12

Generic: Tadalafil Brand: Cialis (ED) or Adcirca (PAH) Classification: PDE5 inhibitor, Vasodilator MOA: selectively inhibits phosphodiesterase type 5 (PDE5), an enzyme that degrades cyclic guanosine monophosphate (cGMP). cGMP levels increase, leading to smooth muscle relaxation and vasodilation. This enhances blood flow to the penis, improving erectile function. This also leads to pulmonary vasodilation, reducing pulmonary arterial pressure. Indications: ED, PAH Contraindications: Use of Nitrates (e.g., nitroglycerin, isosorbide dinitrate/mononitrate) → Can cause severe hypotension. Severe Cardiovascular Disease (e.g., recent MI, stroke, unstable angina). Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, onset within 30-60 minutes. Metabolism: Hepatic (CYP3A4). Excretion: Feces (~61%) and Urine (~36%). Half-Life: 17.5 hours (much longer than Sildenafil & Vardenafil). Dosage: 10mg PO for Cialis, 5mg PO DIE for Adcirca must be taken at same time each day. Adverse Effects: Common: Headache, flushing, dyspepsia (indigestion), nasal congestion. Cardiovascular: Hypotension, dizziness, palpitations. Vision Changes Priapism (Prolonged Erection >4 hours): Medical emergency, requires immediate intervention. Drug Interactions: Nitrates (e.g., Nitroglycerin, Isosorbide Dinitrate/Mononitrate): Life-threatening hypotension. Alpha-Blockers (e.g., Tamsulosin, Doxazosin): Increased risk of hypotension. Monitoring Parameters: Blood Pressure: Monitor for hypotension, especially in patients with cardiac disease. Vision & Hearing Changes: Patients should report sudden vision loss or hearing impairment. Cardiac Function: Assess for angina or arrhythmias in at-risk patients. Response to Treatment: For Cialis, check for improved erectile function; for Adcirca, assess for symptom improvement in PAH.

Answer 13

Generic: Clopidogrel Brand: Plavix Classification: Antiplatelet Agent MOA: Selectively inhibits the P2Y12 ADP receptor on platelets, preventing ADP-mediated platelet activation and aggregation. This results in reduced thrombus (clots) formation. Indications: Acute Coronary Syndrome (ACS) – Used in NSTEMI, STEMI, and unstable angina, often with aspirin. Recent Myocardial Infarction (MI) – Reduces the risk of recurrent MI. Recent Ischemic Stroke or Transient Ischemic Attack (TIA) – Prevents further thrombotic events. Peripheral Arterial Disease (PAD) – Improves blood flow and prevents clot formation. Stent Thrombosis Prevention (PCI with Stent Placement) – Given with aspirin (dual antiplatelet therapy). Contraindications: Active Bleeding (e.g., Peptic Ulcer, Intracranial Hemorrhage). Hypersensitivity to Clopidogrel or its components. Severe Hepatic Impairment (risk of bleeding complications) Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, peak effect in 2 hours. Excretion: Feces (~50%) and Urine (~50%). Dosage: Loading dose 300mg and then maintenance dose 75m DIE Adverse Effects: Bleeding (Most Common) – GI bleeding, epistaxis, easy bruising. Gastrointestinal Symptoms – Diarrhea, abdominal pain, dyspepsia. Skin Reactions – Rash, pruritus. Drug Interactions: NSAIDs & Anticoagulants (e.g., Warfarin, Heparin, DOACs): Increased bleeding risk. SSRIs & SNRIs (e.g., Fluoxetine, Sertraline): Increased bleeding tendency. Monitoring Parameters: Signs of Bleeding: Bruising, black/tarry stools, blood in urine, prolonged bleeding. Platelet Function (if needed): Verify antiplatelet effect in high-risk patients. Hemoglobin & Hematocrit: Monitor for anemia due to bleeding.

Answer 14

Generic: Ticlopidine Brand: Ticlid Classification: Antiplatelet Agent MOA: Selectively inhibits the P2Y12 ADP receptor on platelets, preventing ADP-mediated platelet activation and aggregation. This results in reduced thrombus (clots) formation. Indications: Prevention of Stroke in Patients with a History of TIA or Ischemic Stroke (when aspirin is not tolerated). Prevention of Stent Thrombosis After Coronary Stent Placement (used with aspirin). Alternative Antiplatelet for Patients Intolerant to Aspirin or Clopidogrel. Contraindications: Active Bleeding (e.g., Peptic Ulcer, Intracranial Hemorrhage). Severe Hepatic Impairment (risk of bleeding complications) Hypersensitivity to Ticlopidine. Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, peak effect in 1-3 hours. Duration: Antiplatelet effect lasts 7-10 days. Excretion: Feces (~60%) and Urine (~23%). Half-Life: ~30 hours Dosage: 250mg TID, with food. Adverse Effects: Bleeding (Most Common) – GI bleeding, epistaxis, easy bruising. Gastrointestinal Symptoms – Diarrhea, abdominal pain, dyspepsia. Skin Reactions – Rash, pruritus. Drug Interactions: NSAIDs & Anticoagulants (e.g., Warfarin, Heparin, DOACs): Increased bleeding risk. Monitoring Parameters: Complete Blood Count (CBC) with Differential Signs of Bleeding: Bruising, black/tarry stools, blood in urine.

Answer 15

Generic: Prasugrel Brand: Effient Classification: Antiplatelet Agent MOA: Selectively inhibits the P2Y12 ADP receptor on platelets, preventing ADP-mediated platelet activation and aggregation. This results in reduced thrombus (clots) formation. Indications: Acute Coronary Syndrome (ACS) with Percutaneous Coronary Intervention (PCI) – Reduces the risk of myocardial infarction (MI), stroke, and cardiovascular death. Prevention of Stent Thrombosis After Coronary Stent Placement (used with aspirin). Contraindications: Active Bleeding (e.g., Peptic Ulcer, Intracranial Hemorrhage). Severe Hepatic Impairment (risk of bleeding complications) History of Stroke or Transient Ischemic Attack (TIA). Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, peak effect in ~30 minutes. Excretion: Urine (~70%) and Feces (~30%). Dosage: 60mg once then 10mg DIE Adverse Effects: Bleeding (Most Common) – GI bleeding, epistaxis, easy bruising. Hypotension Drug Interactions: NSAIDs & Anticoagulants (e.g., Warfarin, Heparin, DOACs): Increased bleeding risk. SSRIs & SNRIs (e.g., Fluoxetine, Sertraline): Increased bleeding tendency. Monitoring Parameters: Signs of Bleeding: Bruising, black/tarry stools, blood in urine. Hemoglobin & Hematocrit: Monitor for anemia due to bleeding. Platelet Function (if needed): Verify antiplatelet effect in high-risk patients.

Answer 16

Generic: Ticagrelor Brand: Brilinta Classification: Antiplatelet Agent MOA: Selectively inhibits the P2Y12 ADP receptor on platelets, preventing ADP-mediated platelet activation and aggregation. This results in reduced thrombus (clots) formation. Indications: Acute Coronary Syndrome (ACS) (e.g., Unstable Angina, STEMI, NSTEMI) – Used with aspirin to reduce the risk of myocardial infarction (MI), stroke, and cardiovascular death. Prevention of Stent Thrombosis in PCI Patients – Used as part of dual antiplatelet therapy (DAPT). Secondary Prevention of Atherothrombotic Events – In patients with a history of MI. Contraindications: Active Bleeding (e.g., Peptic Ulcer, Intracranial Hemorrhage). Severe Hepatic Impairment (risk of bleeding complications) History of Stroke or Transient Ischemic Attack (TIA). Routes of Administration: Oral Pharmacokinetics: Absorption: Rapid, peak effect in ~1.5 hours. Excretion: Feces (~58%) and Urine (~26%). Metabolism: Liver (CYP3A4) Half-Life: ~7-9 hours Dosage: 180mg once then 90mg TID Adverse Effects: Bleeding (Most Common) – GI bleeding, epistaxis, easy bruising. Dyspnea (Shortness of Breath) – Reversible, typically mild, and dose-dependent. Bradycardia & Ventricular Pauses – Due to adenosine-like effects. Drug Interactions: NSAIDs & Anticoagulants (e.g., Warfarin, Heparin, DOACs): Increased bleeding risk. Monitoring Parameters: Signs of Bleeding: Bruising, black/tarry stools, blood in urine. Dyspnea Symptoms: Monitor for respiratory distress. Heart Rate & ECG: For bradycardia or pauses.

Answer 17

Generic: Warfarin Brand: Coumadin Classification: Anticoagulant, VKA MOA: Inhibits vitamin K epoxide reductase (VKORC1), preventing the activation of clotting factors II (prothrombin), VII, IX, and X. Indications: Prevention & Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE) Stroke Prevention in Atrial Fibrillation (AFib) Contraindications: Active Bleeding (e.g., GI Bleed, Intracranial Hemorrhage). Pregnancy (Teratogenic – Category X, except in mechanical heart valves). Severe Liver Disease (Impaired clotting factor synthesis). Uncontrolled Hypertension (Increased bleeding risk). Recent Surgery or Trauma (High risk of hemorrhage). Routes of Administration: Oral Pharmacokinetics: Absorption: Oral Metabolism: Liver Excretion: Urine & Feces Half-Life: ~36-42 hours. Dosage: Initial dose 5mg once daily and then maintenance dose of 2-10mg daily adjusted afterwards. Adverse Effects: Bleeding (Most Serious) – Includes intracranial, GI, or hematuria. Drug Interactions: Drugs That Increase Bleeding Risk: Aspirin, NSAIDs (Ibuprofen, Naproxen), Clopidogrel, Heparin, DOACs (Apixaban, Rivaroxaban). Monitoring Parameters: INR (International Normalized Ratio) – Most Important (Goal INR 2-3 in most cases). Signs of Bleeding (Bruising, Gum Bleeding, Blood in Urine/Stool).

Answer 18

Generic: Acenocoumarol Brand: Sintrom Classification: Anticoagulant, VKA MOA: Inhibits vitamin K epoxide reductase (VKORC1), preventing the activation of clotting factors II (prothrombin), VII, IX, and X. Indications: Prevention & Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE) Stroke Prevention in Atrial Fibrillation (AFib) Contraindications: Active Bleeding (e.g., GI Bleed, Intracranial Hemorrhage). Pregnancy (Teratogenic – Category X, except in mechanical heart valves). Severe Liver Disease (Impaired clotting factor synthesis). Uncontrolled Hypertension (Increased bleeding risk). Recent Surgery or Trauma (High risk of hemorrhage). Routes of Administration: Oral Pharmacokinetics: Absorption: Oral Metabolism: Liver Excretion: Urine & Feces Half-Life: 8-12 hours Dosage: Initial dose 2-4mg once daily for two days and then maintenance dose of 1-8mg daily adjusted afterwards. Adverse Effects: Bleeding (Most Serious) – Includes intracranial, GI, or hematuria. Drug Interactions: Drugs That Increase Bleeding Risk: Aspirin, NSAIDs (Ibuprofen, Naproxen), Clopidogrel, Heparin, DOACs (Apixaban, Rivaroxaban). Monitoring Parameters: INR (International Normalized Ratio) – Most Important (Goal INR 2-3 in most cases). Signs of Bleeding (Bruising, Gum Bleeding, Blood in Urine/Stool).

Answer 19

Generic: Dabigatran Brand: Pradaxa Classification: Anticoagulant, DTI MOA: Directly inhibits thrombin (Factor IIa), a key enzyme in the coagulation cascade, preventing the conversion of fibrinogen to fibrin and the subsequent formation of thrombi (blood clots). Indications: Prevention of Stroke and Systemic Embolism in Non-Valvular Atrial Fibrillation (AFib). Treatment and Prevention of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Prevention of DVT and PE following hip replacement surgery. Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Hypersensitivity to Dabigatran or any of its components. Pregnancy (Category C) – Use only if clearly needed. Liver Disease with elevated liver enzymes or hepatic impairment. Routes of Administration: Oral Pharmacokinetics: Onset of Action: 1-3 hours after oral administration. Metabolism: Liver Excretion: Primarily renal (80%) Half-Life: 12-17 hours Dosage: 150mg TID, no need for adjustment. Adverse Effects: Bleeding (Most Serious): GI bleeding, intracranial hemorrhage, and hematuria. Gastrointestinal Symptoms: Dyspepsia, nausea, abdominal pain, and esophagitis. Allergic Reactions: Rash, pruritus, or rare anaphylactic reactions. Drug Interactions: Antiplatelet Drugs (Increased bleeding risk when combined): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Monitoring Parameters: Renal Function (Creatinine Clearance – CrCl). Signs of Bleeding (Bruising, GI bleeding, hematuria). Liver Function (ALT, AST). Hemoglobin and Hematocrit (for bleeding complications).

Answer 20

Generic: Rivaroxaban Brand: Xarelto Classification: Anticoagulant MOA: Directly inhibits Factor Xa, a crucial enzyme in the coagulation cascade that catalyzes the conversion of prothrombin to thrombin. Indications: Prevention of stroke and systemic embolism in non-valvular atrial fibrillation (AFib). Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Prevention of DVT and PE recurrence. Contraindications: Active Bleeding (e.g., gastrointestinal bleeding, intracranial hemorrhage). Hypersensitivity to Rivaroxaban or any of its components. Pregnancy (Category C) – Use only if clearly needed. Routes of Administration: Oral Pharmacokinetics: Absorption: Rivaroxaban has good bioavailability when taken with food. Metabolism: Primarily metabolized by liver Excretion: Primarily renal and in feces. Half-Life: 5-13 hours Dosage: 20mg once daily with food. Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Anemia (due to bleeding). Gastrointestinal Symptoms: Nausea, abdominal pain, dyspepsia. Drug Interactions: Antiplatelet Drugs (Increased bleeding risk when combined): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Monitoring Parameters: Signs of Bleeding (e.g., bruising, dark stools, hematuria). Hemoglobin/Hematocrit (for signs of blood loss).

Answer 21

Generic: Edoxaban Brand: Savaysa Classification: Anticoagluant MOA: Selectively inhibits Factor Xa, an enzyme in the coagulation cascade that converts prothrombin to thrombin Indications: Prevention of stroke and systemic embolism in non-valvular atrial fibrillation (AFib). Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Prevention of recurrent DVT and PE. Contraindications: Active Bleeding (e.g., gastrointestinal bleeding, intracranial hemorrhage). Hypersensitivity to Edoxaban or any of its components. Pregnancy (Category C) – Use only if clearly needed. Routes of Administration: Oral Pharmacokinetics: Absorption: Edoxaban has a high bioavailability (~62%) when taken orally. Metabolism: Minimal hepatic metabolism Excretion: Primarily renal (50-60%), with some fecal elimination. Half-Life: 10-14 hours Dosage: 60mg once daily. Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Anemia (due to bleeding). Gastrointestinal Issues: Nausea, dyspepsia, abdominal pain. Drug Interactions: Antiplatelet Drugs (Increased bleeding risk when combined): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Monitoring Parameters Renal Function Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 22

Generic: Apixaban Brand: Eliquis Classification: Anticoagulant MOA: Selectively inhibits Factor Xa, a key enzyme in the coagulation cascade that converts prothrombin to thrombin Indications: Prevention of stroke and systemic embolism in non-valvular atrial fibrillation (AFib). Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Prevention of recurrent DVT and PE. Contraindications: Active Bleeding (e.g., gastrointestinal bleeding, intracranial hemorrhage). Hypersensitivity to Eliquis or any of its components. Pregnancy (Category C) – Use only if clearly needed. Routes of Administration: Oral Pharmacokinetics: Absorption: Apixaban has high bioavailability (~50%) when taken orally. Metabolism: Primarily metabolized by liver Excretion: Primarily renal (27%) and fecal (63%). Half-Life: 12 hours Dosage: 5mg TID. Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Anemia (due to bleeding). Gastrointestinal Issues: Nausea, dyspepsia, abdominal pain. Drug Interactions: Antiplatelet Drugs (Increased bleeding risk when combined): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Monitoring Parameters Renal Function Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 23

Generic: Enoxaparine Brand: Lovenox Classification: Anticoagulant MOA: Binds to and enhances the activity of antithrombin III, which inhibits Factor Xa and Factor IIa (thrombin), preventing the formation of fibrin and clot formation. Indications: Prevention of Deep Vein Thrombosis (DVT) Treatment of DVT with or without pulmonary embolism (PE). Prevention of ischemic complications of unstable angina and non-Q-wave myocardial infarction (MI). Acute ST-segment elevation myocardial infarction (STEMI) with fibrinolytics. Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Severe Thrombocytopenia (low platelet count). Hypersensitivity to enoxaparin, heparin, or pork products. Routes of Administration: SC or IV Pharmacokinetics: Absorption: Rapidly absorbed after subcutaneous injection with bioavailability of about 90%. Metabolism: Primarily non-hepatic (no significant hepatic metabolism). Excretion: Renal (primarily unchanged in urine). Half-Life: 4.5 hours Dosage: 40mg SC once daily Adverse Effects: Bleeding (Most Common and Serious): May cause GI bleeding, intracranial hemorrhage, and hematoma. A decrease in platelet count can occur, especially in patients with a history of heparin-induced thrombocytopenia (HIT). Injection Site Reactions Drug Interactions: Antiplatelet Drugs (Increased bleeding risk): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Other Anticoagulants: Warfarin or direct thrombin inhibitors can increase bleeding risk when combined with enoxaparin. Monitoring Parameters: Platelet Count (especially for signs of heparin-induced thrombocytopenia). Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 24

Generic: Dalteparine Brand: Fragmin Classification: Anticoagulant MOA: Enhances the activity of antithrombin III, leading to the inhibition of Factor Xa and Factor IIa (thrombin). Indications: Prevention of Deep Vein Thrombosis (DVT) in patients undergoing hip or knee replacement surgery, abdominal surgery, or medical patients with restricted mobility. Treatment of DVT with or without pulmonary embolism (PE). Prevention of ischemic complications of unstable angina and non-Q-wave myocardial infarction (MI). Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Severe Thrombocytopenia (low platelet count). Hypersensitivity to dalteparin, heparin, or pork products. Routes of Administration: SC or IV Pharmacokinetics: Absorption: Dalteparin is rapidly absorbed after subcutaneous injection, with a bioavailability of around 90%. Metabolism: Primarily non-hepatic, meaning it is not significantly metabolized in the liver. Excretion: Renal (about 60% is excreted unchanged in urine). Half-Life: 3-5 hours Dosage: 2,500 to 5,000 IU SC once daily. Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Injection Site Reactions: Pain, bruising, or hematoma at the injection site. Drug interactions: Antiplatelet Drugs (Increased bleeding risk): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Other Anticoagulants (Increased bleeding risk): Warfarin, rivaroxaban, dabigatran, apixaban. Monitoring Parameters: Platelet Count Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 25

Generic: Fondaparinux Brand: Arixtra Classification: Anticoagulant MOA: Selectively inhibits Factor Xa by binding to antithrombin III (ATIII). This inactivates Factor Xa, preventing the conversion of prothrombin to thrombin, which is essential for clot formation. Indications: Prevention of Deep Vein Thrombosis (DVT) in patients undergoing hip or knee replacement surgery or abdominal surgery. Treatment of DVT and Pulmonary Embolism (PE) (in combination with warfarin or other anticoagulants for long-term management). Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Hypersensitivity to fondaparinux or other heparins. Severe thrombocytopenia (low platelet count) or a history of heparin-induced thrombocytopenia (HIT). Routes of Administration: SC or IV Pharmacokinetics: Absorption: Rapidly absorbed after subcutaneous injection, with high bioavailability (100%). Metabolism: No significant hepatic metabolism. Excretion: Renal (80% of the drug is excreted unchanged in the urine). Half-Life: 17-21 hours Dosage: 2.5mg SC once daily Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Thrombocytopenia (Rare): May cause a decrease in platelet count, though less common than heparin-induced thrombocytopenia (HIT). Injection Site Reactions: Pain, bruising, or hematoma at the injection site, though less common than with unfractionated heparin. Anemia Drug Interactions: Antiplatelet Drugs (Increased bleeding risk): Aspirin, NSAIDs, Clopidogrel, Ticagrelor – Increased bleeding risk when combined with fondaparinux. Other Anticoagulants (Increased bleeding risk): Warfarin, rivaroxaban, dabigatran, apixaban. Thrombolytics (e.g., tPA, streptokinase, urokinase) should be used cautiously with fondaparinux due to increased bleeding risk. Monitoring Parameters: Platelet Count (especially for signs of heparin-induced thrombocytopenia). Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 26

Generic: Tinzaparine Brand: Innohep Classification: Anticoagulant MOA: Enhances the activity of antithrombin III, which inactivates Factor Xa and Factor IIa (thrombin). Indications: Prevention of Deep Vein Thrombosis (DVT) in patients undergoing hip or knee replacement surgery or abdominal surgery. Treatment of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Severe Thrombocytopenia (low platelet count). Hypersensitivity to tinzaparin, heparin, or pork products. Routes of Administration: SC or IV Pharmacokinetics: Absorption: Rapid absorption after subcutaneous injection, with high bioavailability. Metabolism: Non-hepatic. Excretion: Renal (about 60% of the drug is excreted unchanged). Half-Life: 3-4 hours Dosage: 50 IU/kg SC once daily. Adverse Effects: Bleeding (Most Common and Serious): Can cause GI bleeding, intracranial hemorrhage, and hematoma. Injection Site Reactions: Pain, bruising, or hematoma at the injection site. Drug Interactions: Antiplatelet Drugs (Increased bleeding risk): Aspirin, NSAIDs, Clopidogrel, Ticagrelor. Other Anticoagulants (Increased bleeding risk): Warfarin, rivaroxaban, dabigatran, apixaban. Thrombolytics (e.g., tPA, streptokinase, urokinase) should be used cautiously with tinzaparin. Monitoring Parameters: Platelet Count (especially for signs of heparin-induced thrombocytopenia). Signs of Bleeding (unusual bruising, blood in stool or urine, nosebleeds). Hemoglobin/Hematocrit (to monitor for bleeding complications).

Answer 27

Generic: Heparine Sodique Brand: Heparin Classification: Anticoagulant MOA: Enhances the activity of antithrombin III, which inhibits several clotting factors, particularly Factor Xa and Factor IIa (thrombin). Indications: Prophylaxis and Treatment of Deep Vein Thrombosis (DVT). Pulmonary Embolism (PE). Prevention of thrombus formation during open-heart surgery and vascular surgery. Acute Coronary Syndrome (ACS), including unstable angina and non-ST-segment elevation myocardial infarction (NSTEMI). Prevention of clotting in patients undergoing dialysis or blood transfusions. Use as an adjunctive agent in in vitro studies or in laboratory procedures. Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Severe Thrombocytopenia (low platelet count). Hypersensitivity to heparin or pork products. History of Heparin-induced Thrombocytopenia (HIT). Severe hypertension or other conditions with high bleeding risk. Routes of Administration: SC or IV Pharmacokinetics: Absorption: Heparin is rapidly absorbed after subcutaneous injection but has variable absorption rates depending on the site of injection and patient factors. Onset of Action: Immediate (IV), 20-30 minutes after subcutaneous injection. Metabolism: Non-hepatic Excretion: Renal Half-Life: 1-2 hours Dosage: 5,000 IU every 8-12 hours Adverse Effects: Bleeding (Most Common and Serious): The most common side effect, ranging from minor bruising to life-threatening hemorrhage. Heparin-induced Thrombocytopenia (HIT) Injection site reactions (pain, redness, hematoma). Drug Interactions: Antiplatelet Agents (Increased bleeding risk): Aspirin, NSAIDs, Clopidogrel, Ticagrelor – These increase the risk of bleeding when combined with heparin. Other Anticoagulants (Increased bleeding risk): Warfarin, rivaroxaban, dabigatran, apixaban – Combined use increases the risk of bleeding. Thrombolytics (e.g., tPA, streptokinase, urokinase) should be used cautiously with heparin due to increased bleeding risk. Corticosteroids: May increase the risk of bleeding by affecting platelet function. Monitoring Parameters: Activated Partial Thromboplastin Time (aPTT) – The most important test to monitor for therapeutic levels of heparin (usually 1.5-2.5 times normal value). Platelet Count – To monitor for heparin-induced thrombocytopenia (HIT). Hemoglobin and Hematocrit – To detect bleeding complications. Signs of Bleeding – Watch for unusual bruising, blood in stool or urine, and nosebleeds.

Answer 28

Generic: Danaparoide Brand: Orgaran Classification: Anticoagulant MOA: Inhibits Factor Xa and to a lesser extent, Factor IIa (thrombin). It binds to antithrombin III to inactivate Factor Xa and other clotting factors. Indications: Prevention of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE) in patients at risk. Treatment of Acute Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE). Heparin-induced Thrombocytopenia (HIT): Danaparoid is an alternative anticoagulant in patients with HIT or HIT with thrombosis (HITT). Contraindications: Active Bleeding (e.g., GI bleeding, intracranial hemorrhage). Severe Thrombocytopenia (low platelet count). Hypersensitivity to danaparoid or any of its components. History of heparin-induced thrombocytopenia (HIT), unless used as an alternative. Routes of Administration: SC or IV Pharmacokinetics: Absorption: Danaparoid is well-absorbed after subcutaneous injection, with high bioavailability. Onset of Action: Effects are seen within 2-4 hours of subcutaneous administration. Metabolism: Non-hepatic, mainly cleared through the kidneys. Excretion: Renal, with significant renal excretion Half-Life: 25 hours Dosage: 1500 IU once daily Adverse Effects: Bleeding (Most Common and Serious): The most significant risk of danaparoid therapy is bleeding, especially in patients with other risk factors for bleeding. Monitor for unusual bruising, blood in stool or urine, nosebleeds. Heparin-induced Thrombocytopenia (HIT): Although danaparoid is used as an alternative to heparin in HIT, monitor platelet counts regularly. The incidence of HIT is lower with danaparoid compared to heparin. Injection site reactions (pain, bruising, or redness). Drug Interactions: Other Anticoagulants (Increased bleeding risk): Warfarin, enoxaparin, rivaroxaban, dabigatran, apixaban, and other antiplatelet agents may increase the bleeding risk when used together. Monitor INR if used concomitantly with warfarin. Thrombolytic Therapy: When used with thrombolytics (e.g., tPA, streptokinase), bleeding risk is significantly increased. Use with caution. Monitoring Parameters: Platelet Count – To monitor for heparin-induced thrombocytopenia (HIT) or other thrombocytopenia. Signs of Bleeding – Watch for unusual bruising, blood in stool or urine, and nosebleeds. Anti-Xa levels (especially when used as an alternative to heparin in HIT).