Drugs for Coagulation Disorders Flashcards
antipyretic, anti-inflammatory, ANTI-PLATELET, analgesic
prevents arterial thrombosis; used for inflammatory disorders
uncoupler of oxidative phosphorylation in ETC
SE: hypersensitivity
aspirin/acetylsalicylic acid/ASA
toxic and lethal dose of ASA/aspirin
toxic dose: 150 mg/kg
lethal dose: 500 mg/kg
acid-base disorder in aspirin intoxication
adults: respiratory alkalosis with HAGMA
children: HAGMA
ASA intoxication in children
considered idiosyncratic
Reye Syndrome
Samter Triad of ASA intoxication
asthma
aspirin sensitivity
nasal polyps
GpIIb/IIIa inhibitor
prevents vessel restenosis, reinfarction, death
Abciximab
Eptifibatide, Tirofiban
ADP inhibitor
reduces platelet aggregation
prevention and treatment of arterial thrombosis
has additive effects with aspirin
Clopidogrel
Ticlopidine (parent coumpound; has more GI and hema SE)
Prasugel
PDE inhibitor increases cAMP (which is an anti-aggregant) for intermittent claudication
Dipyrimadole (has little or no benefit)
Cilostazol (contraindicated in heart failure)
2 major types of anti-coagulants:
indirect thrombin inhibitors: ?
direct thrombin inhibitors: ?
indirect thrombin inhibitors: heparin, enoxaparin (LMWH), coumarin derivatives (warfarin)
direct thrombin inhibitors: lepirudin
heparin antidote
protamine sulfate
laboratory tests to evaluate coagulation pathways
intrinsic pathway: PTT
extrinsic pathway: PT
indirect thrombin inhibitor; anticoagulant
activates antithrombin III
for deep venous thrombosis, pulmonary embolism, myocardial infarction
monitor with aPTT (N = 1.5 - 2.5)
heparin
indirect thrombin inhibitor; anticoagulant
factor Xa selective
for deep venous thrombosis, pulmonary embolism, myocardial infarction
SE: less risk of thrombocytopenia
does NOT require aPTT monitoring
protamine sulfate is only partially effective in reversing effects
Enoxaparin
Dalteparin, Tinzaparin, Danaparoid, Fondaparinux
direct thrombin inhibitor; anticoagulant
for heparin-induced thrombocytopenia
monitor effect with aPTT
NO REVERSAL AGENT EXISTS
Lepirudin
Desirudin, Bivalirudin, Argatroban, Dabigatran
oral direct Factor Xa inhibitor
Rivaroxaban
Apixaban
anticoagulant
for chronic anticoagulation EXCEPT in pregnancy
monitor effects with PT
NARROW THERAPEUTIC WINDOW
active ingredient in most rat poisons (racumin)
Warfarin
Dicumarol
Anisindione
SE: warfarin-induced skin necrosis (for protein C & S deficiencies)
antidote for warfarin
Vit. K (slow) vs. FFP (fast)
what is prothrombotic first before it works as an anticoagulant?
warfarin
requires elimination of preformed clotting factors (8-60 hrs)
hence heparin bypasses initial prothrombotic effect of warfarin (skin necrosis)
what increases clearance and reduces anticoagulant effect?
cytochrome P450-inducers
what reduces clearance and increases anticoagulant effect?
cytochrome P450-inhibitors
cytochrome P450-inducers
Ethanol Barbiturates Phenytoin Rifampicin Griseofulvin Carbamazepine St. John's Wort/Smoking
cytochrome P450-inhibitors
Isoniazid Sulfonamides Cimetidine Ketoconazole Erythromycin Grapefruit juice Ritonavir Amiodarone Quinidine
antidote
chemical antagonist
partially reverses effects of LMWH
protamine sulfate
tissue plasminogen activator analog
thrombolytic
for acute MI, ischemic stroke, pulmonary embolism
antidote: AMINOCAPROIC ACID
Alteplase
anistreplase, reteplase, streptokinase, tenecteplase, urokinase
loss of effectiveness (on 2nd use) and allergic reactions may be observed with STREPTOKINASE
contraindication to thrombolysis
- history of cerebrovascular hemorrhage at any time
- non-hemorrhagic stroke or other cerebrovascular event within past year
- marked hypertension (>180/110 mmHg) at any time during acute presentation
- suspicion of aortic dissection
- active internal bleeding (except menses)
prothrombotic antiplasmin aminocaproic acid inhibits tPA CONTRAINDICATED IN DIC
Tranexamic Acid
antidote
prevention of hemorrhagic diathesis in newborns
SE: severe infusion reaction (dyspnea, chest and back pain)
Vitamin K1 = Phytonadione
Vitamin K2 = Menaquinone
Vitamin L3 = Menadione –> SHOULD NEVER BE USED IN THERAPEUTICS (INEFFECTIVE)
ADH agonist
vasopressin V2 receptor agonist
increases factor VIII activity of patients with mild hemophilia A or von Willebrand disease
Desmopressin
Vasopressin
antiplasmin
serine protease inhibitor
for post-op or intra-op bleeding
REMOVED IN 2007 FROM MARKET DUE TO MORTALITY
Aprotinin
other drugs used for coagulation disorders
antihemophilic factor
anti-inhibitor coagulant complex
anti-thrombin III
factor VIIa, VIII, IX complex
