Exam 4 Flashcards
3 Short-Medium acting Glucocorticoids
Hydrocortisone
Prednisone
Methylprednisolone
Intermediate Acting Glucocorticoid
Triamcinolone
Long acting Glucocorticoid
Dexamethasone
2 Glucocorticoid synthesis inhibitors/antagonists
Metyrapone
Ketoconazole
Mineralocorticoid agonist
Fludrocortisone
Mineralocorticoid antagonist
Spironolactione
4 Glucocorticoids Used to Treat Asthma
Prednisone, Methylprednisolone, Triamcinolone, Dexamethasone
All the ones we know minus hydrocortisone
Steroid Tx for Cerebral Edema
Prednisone
Steroid Tx for Bacterial Meningitis
Dexamethasone
Steroid Tx for Collagen Disorders (SLE, Polymyalgia rheumatica, myositis)
Prednisone, Methylprednisolone, Triamcinolone, Dexamethasone
All the ones we know minus hydrocortisone, same as for asthma
Steroid Tx for Hematological Disorders (Autoimmune hemolytic anemia, Thrombocytopenia purpura)
Prednisone, Triamcinolone, Dexamethasone
Asthma/Collagen drugs minus Methylprednisone
Steroid Tx for Idiopathic Nephrotic Syndrome
Methylprednisolone
Steroid Tx for pulmonary sarcoidosis
Prednisone
Steroid Tx for Respiratory Distress Syndrome in the premature neonate
Dexamethasone
Describe Hydrocortisone, Prednisone, Triamcinolone, and Dexamethasone in terms of their Anti-inflammatory properties and mineralocorticoid potency.
Hydrocortisone has low AI potency and High mineralocorticoid potency.
Prednisone has medium AI potency and Moderate mineralocorticoid potency.
Triamcinolone has Medium AI potency and no mineralocorticoid potency
Dexamethasone has very high AI potency and no mineralocorticoid potency.
Fludrocortisone
Mineralocorticoid agonist
Has both mineral/glucocorticoid properties.
Tx for adrenocortical insufficiency associated with mineralocorticoid deficiency.
Metyrapone
Inhibitor of cortisol and aldosterone synthesis
Inhibits CYP11B1
Cushing’s Tx
Ketoconazole
Blocks all steroid synthesis by inhibiting CYP17 and at higher concentrations CYP11A1.
Most effective inhibitor in tx of Cushing’s
Typically used before Metyrapone with Metyrapone added if necessary (they exhibit synergism)
Also an antifungal agent
Spironolactone
Mineralocorticoid antagonist
Tx for hyperaldosteronism
Given before adrenal adenoma surgery to normalize potassium.
Cosyntropin
Synthetic ACTH
Used to test adrenal function.
Aspirin
Cyclooxygenase inhibitor
Suppresses of Thromboxane, which is a proaggregatory substance produced by platelets.
The effect is irreversible and lasts as long as the affected platelet is alive.
Used to prevent MI, ischemic strokes.
Used after CABG to prevent graft occlusion.
160-325 mg/day is antiplatelet dose
GI side effects
May effect hemostasis in surgery (more bleeding)
May cause problems in pregnancy.
Heparin
Antigoagulant via binding to Lysine residues of Antithrombin III (a protease inhibitor) and accelerating its activity.
AT III inactivates Xa and Thrombin, preventing conversion of fibrinogen to fibrin.
Also inhibits platelet function (can cause thrombocytopenia)
Its a mix of mucopolysaccharides that is synthesized in mast cells, especially in the lungs.
Administered by IV and works rapidly.
Used to treat MI, during heart surgery with extracorporeal circulation, and to keep CV catheters patent.
Better than oral anticoagulants during pregnancy.
Usage monitored by PTT, APTT.
Quite a few side effects…
Antidote to OD is Protamine sulfate.
Protamine sulfate
Strongly basic proteins originally harvested from fish sperm
Binds to Heparin due to its positive charge and reverses its effect immediately.
Lasts about 2 hours.
Too much can have anticoagulant activity of its own.
Less effective at inhibiting low molecular weight heparin.
Side effects include transient hypotension and allergic reactions (fish allergy?)
Warfarin
Oral anticoagulant.
Blocks Vitamin K in the liver, inhibiting the synthesis of clotting factors.
Works slower than heparin because clotting factors already in blood are unaffected.
Used to prevent thromboembolism in patients with chronic conditions (A fib, prosthetic valves, indwelling venous catheters, etc.)
Also used as part of chemo for some cancer treatments.
Risk of bleeding, hypertension, soft tissue necrosis, GI problems.
Dont give it to pregnant patients. It will cross the placenta and severely mess up the fetus. Use heparin instead if necessary.
Aspirin may intensify its affect.
Corticosteroids or too much vitamin K may decrease its affect.
Too much can be reversed with Vitamin K and FFP.
Lepirudin
Thrombin inhibitor
Yeast polypeptide
IV injected, very short halflife.
Used as an anticoagulant in patients with heparin-induced thrombocytopenia.
Side effects include hypersensitivities, bleeding, may affect fetus.
No antidote for OD.
Alteplase
tPA
Serine protease
Activates fibrin bound plasminogen to plasmin.
Can be reversed with Aminocaproic acid
Aminocaproic acid
Reverses alteplase (tPA)
Factor VIII
Antihemophilic factor
Treats hemophilia A, which is a factor VIII deficiency
Clopidogrel
Oral antiplatelet
Inhibits platelet aggregation
Inhibits the irreversible binding of ADP to the ADP receptor
Platelets exposed to clopidogrel are thus effected for their entire lifespan.
Used to prevent MI, stroke in high risk patients
Dipyramidamole
Blocks platelet adhesion to the subendothelium by inhibiting phosphodiesterase, increasing cAMP
Tirofiban
Antagonist of the platelet glycopritein IIb/IIIa receptor.
Inhibits platelet aggregation.
B12 and Folate
Treatment for megaloblastic anemia
Pernicious anemia is an example
Megaloblastic because cells lack the nutrients that allow them to divide. They just get larger.