Pharma Mod 6

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Questions and Answers

What is a major adverse effect of fibrinolytic agents?

Increased blood pressure

Thrombosis of healthy blood vessels

Wound healing acceleration

Hemorrhage (correct)

What is the primary role of platelet aggregation inhibitors?

To enhance the formation of thrombus.

To decrease the action of signals promoting platelet aggregation. (correct)

To promote the conformational change of GP IIb/IIIa receptors.

To increase blood pressure during coagulation.

Which patients are contraindicated from using Alteplase?

Patients with high blood pressure

Patients with myocardial infarction

Patients with healing wounds (correct)

Patients with acute ischemic stroke

Which receptor is crucial for regulating platelet-platelet interaction?

GP IIb/IIIa receptor Signup and view all the answers

What is the primary use of Streptokinase?

Treatment of acute pulmonary embolism Signup and view all the answers

Which of the following agents is known to promote platelet activation?

Thromboxane A2 Signup and view all the answers

What is the mechanism of action of eptifibatide?

Binds to GP IIb/IIIa at the site for fibrinogen interaction Signup and view all the answers

What potential side effect is associated with aminocaproic acid and tranexamic acid?

Intravascular thrombosis Signup and view all the answers

Which of the following statements about dipyridamole is correct?

It is a coronary vasodilator used prophylactically. Signup and view all the answers

What is a characteristic of hemophilia?

Deficiency in plasma coagulation factors Signup and view all the answers

How does fibrinogen contribute to platelet aggregation?

By binding to GP IIb/IIIa receptors on two separate platelets. Signup and view all the answers

What mechanism do aspirin and other platelet aggregation inhibitors use?

Inhibition of cyclooxygenase-1 (COX-1). Signup and view all the answers

What is a major adverse effect of GP IIb/IIIa-receptor blockers?

Bleeding Signup and view all the answers

What common reaction may occur as a side effect of Streptokinase?

Rash and fever Signup and view all the answers

Which method is not typically used to treat severe hemorrhage?

Exercise therapy Signup and view all the answers

What is one of the therapeutic uses of platelet aggregation inhibitors?

For the treatment of occlusive cardiovascular diseases. Signup and view all the answers

Which anticoagulant functions by interfering with the synthesis of coagulation factors?

Warfarin Signup and view all the answers

How is the extrinsic pathway of coagulation initiated?

By activation of clotting Factor VII by tissue factor Signup and view all the answers

Which of the following best describes how platelet aggregation takes place?

It requires fibrinogen to link GP IIb/IIIa receptors on different platelets. Signup and view all the answers

Which enzyme is Alteplase derived from?

Serine protease from human melanoma Signup and view all the answers

Which statement correctly describes tirofiban?

It blocks the same site as eptifibatide but is not a peptide. Signup and view all the answers

What potential effect occurs when GP IIb/IIIa receptors are blocked?

Decreased platelet cross-linking and aggregation. Signup and view all the answers

What are the available formulations for GP IIb/IIIa blockers?

Only intravenous formulations Signup and view all the answers

Which of the following components is expressed by activated endothelial cells during vascular injury?

Tissue factor Signup and view all the answers

What is the effect of the combination of ezetimibe and simvastatin on LDL levels compared to simvastatin alone?

It lowers LDL levels more effectively. Signup and view all the answers

Which drug is included in the formulation that enhances LDL lowering?

Ezetimibe Signup and view all the answers

What is the primary purpose of the formulation of ezetimibe and simvastatin?

To lower LDL levels. Signup and view all the answers

Which antihyperlipidemic effect is primarily targeted by simvastatin?

Lowering LDL cholesterol Signup and view all the answers

What class of drugs does simvastatin belong to?

Statins Signup and view all the answers

In the context of treating hyperlipidemia, what is a common goal of statin therapy?

To lower LDL cholesterol levels Signup and view all the answers

What is one benefit of using ezetimibe in combination with statins?

Enhances efficacy in lowering LDL Signup and view all the answers

What role does ezetimibe play in lipid regulation?

It inhibits the absorption of cholesterol in the intestines. Signup and view all the answers

Which of the following is an adverse effect associated with the use of anticoagulants?

Bleeding disorders Signup and view all the answers

What is a contraindication for the use of warfarin?

Pregnancy Signup and view all the answers

What is the primary mechanism of action of coumarin anticoagulants like warfarin?

Inhibition of vitamin K functions Signup and view all the answers

In which scenario is thrombolytic therapy generally considered reliable?

When angioplasty is not an option Signup and view all the answers

What therapeutic condition is NOT mentioned as a use for warfarin?

Active infections Signup and view all the answers

What percentage of thrombolytic therapy outcomes are considered unsuccessful in infarcted arteries?

20% Signup and view all the answers

Which of these conditions indicates the need for anticoagulant therapy with a consideration for a patient's risk?

Acute myocardial infarction Signup and view all the answers

What is a potential outcome following the administration of thrombolytic drugs?

Lysis of both normal and pathologic thrombi Signup and view all the answers

What is a major adverse effect associated with bile acid sequestrants?

Gastrointestinal disturbances Signup and view all the answers

Which of the following is a contraindication for using ezetimibe?

Severe hepatic insufficiency Signup and view all the answers

How do bile acid sequestrants lower LDL cholesterol levels?

By binding bile acids in the intestine Signup and view all the answers

Which of the following statements regarding colesevelam is correct?

It causes fewer gastrointestinal side effects than cholestyramine or colestipol. Signup and view all the answers

What is the primary mechanism of action of ezetimibe?

Inhibition of cholesterol absorption in the intestine Signup and view all the answers

What effect do high doses of cholestyramine and colestipol have that colesevelam does not?

Impair absorption of fat-soluble vitamins Signup and view all the answers

In which patient population are bile acid sequestrants primarily indicated?

Patients with Type IIa and IIb hyperlipidemias Signup and view all the answers

What is the approximate reduction in LDL cholesterol that ezetimibe achieves?

17% Signup and view all the answers

Study Notes

Basic Pharmacology - Drugs Affecting the Blood and Antihyperlipidemic Drugs - Module 6

This module covers drugs used to treat thrombosis, bleeding, and anemia.

Drugs Affecting the Blood

Overview: Drugs are used in treating thrombosis, bleeding, and anemia.
Thrombosis: Formation of an unwanted blood clot within a blood vessel. Common thrombotic disorders include
- Acute myocardial infarction
- Deep-vein thrombosis
- Pulmonary embolism
- Acute ischemic stroke
Drugs used in treating Thrombosis: Anticoagulants and fibrinolytics
Hemostasis: Physiological process that stops bleeding at the site of injury while maintaining normal blood flow.
Bleeding Disorders: Include hemophilia (treated with Factor VIII) and vitamin K deficiency (treated with dietary supplements).
Anemias: Caused by nutritional deficiencies (iron deficiency anemia), or genetic disorders (sickle cell disease).

Thrombus vs Embolus

A thrombus is a clot that adheres to a vessel wall.
An embolus is a detached thrombus that floats in the blood.
Both can occlude blood vessels, depriving tissues of oxygen and nutrients.
Arterial thrombosis typically involves platelet-rich clots, often due to atherosclerosis.
Venous thrombosis involves fibrin-rich clots and is often associated with blood stasis.

Platelet Response to Vascular Injury

Physical trauma to the blood vessels initiates interactions between platelets, endothelial cells and the coagulation cascade.
A platelet-fibrin plug (clot) forms at the site of puncture.
Platelets monitor the integrity of the endothelium, circulating freely when there is no injury.

Drugs Affecting the Blood: Platelet Aggregation Inhibitors

These drugs decrease platelet aggregation by inhibiting chemical signals
The most important agent is the GP IIb/Illa receptor that ultimately regulates platelet interactions.
Fibrinogen binds to GP IIb/IIla receptors, contributing to platelet aggregation.
Inhibiting cyclooxygenase-1 (COX-1) or blocking GP IIb/IIIa or ADP receptors interferes with signals that induce platelet aggregation.
Therapeutic uses include prevention and treatment of cardiovascular diseases and as adjuncts to thrombolytic therapy in myocardial infarction.

Drugs Affecting the Blood: Anticoagulants

Mechanism: Affect clotting by inhibiting thrombin's action, or interfering with the synthesis of coagulation factors.
Heparin: Major antithrombotic for deep vein thrombosis and pulmonary embolism.
Low-molecular weight heparins (LMWHs): Advantageous over heparin in certain circumstances including injections.
Lepirudin: Directs thrombin antagonist, useful in HIT and thromboembolic disorders.
Argatroban: Direct thrombin inhibitor, utilized for treatment and prophylaxis of HIT and percutaneous coronary interventions.
Fondaparinux: Synthetic pentasaccharide that is used to prevent deep vein thrombosis.
Vitamin K antagonists (ex. warfarin): Used in prophylactically in patients with acute myocardial infarction, prosthetic valves or chronic atrial fibrillation

Drugs Affecting the Blood: Thrombolytics

Mechanism: Activate the conversion of plasminogen to plasmin, enabling fibrin breakdown and clot dissolution.
Alteplase (tPA): Treatment for acute myocardial infarction.
Streptokinase: For pulmonary embolism, acute myocardial infarction, or occluded access shunts.

Drugs Used to Treat Bleeding

Aminocaproic acid, tranexamic acid: Control fibrinolytic states and are oral active.
Protamine sulfate: Antagonizes Heparin's anticoagulant effects.
Vitamin K (phytonadione): Delays the response, if immediate hemostasis is needed use fresh frozen plasma.
Aprotinin: Serine protease inhibitor, and inhibits streptokinase.
Blood transfusions: Treatment option to replace blood loss.

Agents Used to Treat Anemia

Defined as having a below-normal plasma hemoglobin concentration or low total hemoglobin content.
- Deficiency may be due to chronic blood loss, bone marrow abnormalities, increased hemolysis, infections, or malignancy.
Iron: Stored as ferritin; deficiency can result from acute/chronic blood loss, growth periods and periods of heavy menstruation/pregnancy.
Folic Acid: Important for DNA synthesis; deficiency can lead to megaloblastic anemia, seen in pregnancy, alcoholism and those with malabsorption.
Vitamin B12: Necessary for DNA synthesis; Deficiency can lead to pernicious anemia.
Erythropoietin and darbepoetin: Used to treat anemia associated with end-stage renal disease, HIV infection or some cancers

Agents Used To Treat Sickle Cell Anemia

Hydroxyurea: May alleviate painful sickle-cell disease symptoms by increasing fetal hemoglobin levels.
It is used in treating chronic myelogenous leukemia and polycythemia vera.

Antihyperlipidemic Drugs

Elevated levels of LDL cholesterol, triacylglycerols, and low levels of HDL cholesterol are correlated with coronary heart disease incidence.
Other risk factors for CHD include smoking, hypertension, obesity, and diabetes.
Hyperlipidemias can also result from a single inherited gene defect or lifestyle factors, or combined.
Antihyperlipidemic drugs are required to lower lipid levels.

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