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170 Cards in this Set
- Front
- Back
Normal dopamine transmission removes the inhibition on the what via what?
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Thalams, via secreation of GABA, thus inhibited by GABA.
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After the Thalamus what happens with the transmission?
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Glutamatergic neuron transmission.
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What is the goal and strategies in the pharmacological Tx of Parkinsons?
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Goal = To restore normal functioning of the striatum. Strategies: 1. Restore DA levels to normal 2. Correct imbalance between ACh and DA in striatum and #. Directly stimulate striatal DA receptors with agonist drug.
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Parkinson's Drugs not in a specific class.
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Levadopa
Carbidopa Amantadine |
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Levadopa and Carbidopa
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Levadopa is given with carbidopa and entacapone to increase dopamine levels. Carbidopa is a dopa decarboxylase inhibitor, it inhibits the conversion of L-Dopa to Dopamine.
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Parkinson's COMT Inhibitors
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Entacapone and Tolcapone
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Entacapone and Tolcapone MOA
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Keep COMT inhibited so that it can't metabolized L-Dopa into Dopamine
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Parkinson's Dopamine Agonist
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Bromocriptine
Pramipexole Ropinirole Apomorphine Rotigotine Cabergoline |
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Bromocriptine
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Is an ergot derivative that acts as anb agonist at the D2 like family of DA receptors, some selectivity for D3
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Parmipexole
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Non-Ergot dopamine agonist that acts at the D2 and D3 receptors
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Ropinirole and Rotigotine
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Non-Ergot dopamine agonist at D2, D3 receptor. Rotigotine also at D1
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Apomorphine
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D1 and D2 dopamine agonist
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Cabergoline
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Long acting D2 receptor agonist
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MAOI Inhibitors
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Selegeline and Rasageline
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Selegeline and Rasageline
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Selective and IRREVERSIBLE MAO-B Inhibitors
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Parkinson's Anticholinergic Drugs
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Procyclidine, Trihexyphenidyl, Benztropine, Biperiden
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Procyclidine, Trihexyphenidyl, Benztropine, Biperiden MOA
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Block the effects of ACh in striatum restoring balance between DA and ACh
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Amantadine is what kind of drug and what is its MOA?
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It is an anti-viral drug, and its MOA is unknown
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Neuroleptic Drugs: Phenothiazines
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Prochlorperazine
Chlorpromazine Thioridazine Penphenazine Fluphenazine |
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Neuroleptic Drugs: Butyrophenones
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Haloperidol
Droperidol |
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Neuroleptic Drugs: Thioxanthines
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Thiothixine
Chlorprothixene |
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Neuroleptic Drugs: Atypical Anti-Psychotics
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Quietidine
Risperidone Clozapine Paliperidone Aripiprazole Pimozide Loxapine Olanzapine Olanzapine and Fluoxitine Melindone Ziprasidone |
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Neuroleptic Drugs: Bi-Polar
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Lithum
Valproic Acid Cabemazepine |
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Antipsychotic Drugs MOA
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Block D2 receptors but extent varies, alpha 1 and 5HT2 blockade is common, atypical antipsycholtics have affinity for 5HT2A receptors, less for D2 receptors
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Clozapine MOA
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D4 and 5HT2 Blocker
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Lithium MOA
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Decreases IP3 and DAG levelvs thus decreases PKC activity. Lithium inhibits enzymes of inositol recycling, uncouples G proteins at least explains some side effects. Polyuria is due to uncoupling of G protein from vasopression receptor. Hypothyroidism is due to uncoupling of TSH receptor.
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Opiods: Opiod Agonist
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Sufentanyl, Fentanyl, Alfentenil, Remifentanyl, Oxymorphone, Hydromorphone, Oxycodone, Diacetylmorphine(HEROIN), Methadone, Morphine, Normophine, Codeine, Propoxyphene, Tramadol
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Opiod Agonist MOA
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1. Direct Inhibition 2. Indirect Inhibition
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Opiod Agonist MOA
1. Direct Inhibition? |
Presynaptic and Postsynaptic
Presynaptic - Inhibit opening of voltage gated Ca channels which inhibits Ca entry and decreases NT release. Postsynaptic - Gi/Go activation causes opening of K channels leading to hyperpolarization. Gi/Go activation inhibits adenylate cyclase which decreases cAMP and PKA which decresaes phosphorylation of many cellular proteins including Na channels decreasing neuronal excitability |
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Opiod Agonist MOA
2. Indirect Inhibition |
Indirect inhibition of synaptic transmission release of engogenous opiopeptides thus causing even more inhibition.
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Opiod: Mixed Agonist/Antagonist and Partial Antagonist
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Pentazocine
Nalbuphine Butorphanol Buprenorphine |
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Opiod: Opiod Antagonist
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Naloxone
Naltrexone Nalmefene |
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Hematopoeisis: Iron Drugs
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Iron Dextram
Iron Sucrose Iron Gluconate |
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Hematopoeisis: Iron Chelators
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Deferoxamine
Deferasirox |
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MOA for Deferasirox
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Selective for Fe3+, binds 2:1 ratio and excretion is fecal.
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B-12 Deficiency Tx
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Cyanocobalamin
Hydroxocobalamin |
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Sickle Cell Anemia Tx
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Hydroxyurea
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MOA for Hydroxyurea?
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Unknown
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Hematopoeitic Growth Factors:
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Epoetin Alfa (Epogen, Procrit)
Darbepoetin Alfa (Aranesp) G-CSF (Filgastrin, Neupogen) Pegfilgastrin (Neulasta) GM-CSF (Sargramastin, Leukine) IL-II (Opreleukin, Neumega) Thrombopoeitin (Romiplastim, Nplate) |
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Erythropoeitin MOA
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Stimulate RBC production, binds to erythropoeitin receptors on red cell progenitor cells.
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Myeloid Growth Factors MOA
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Glycoproteins that stimulate the proliferation and differentiation of myeloid cell lines. Bind and activate cytokine receptors of the JAK/STAT superfamily.
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Granulocyte-Colony Stimulating Factor (Filgastrim, Neupogen) MOA
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Stimulates the proliferation and differentiation of cells committed to the neutrophil lineage, activates mature neutrophils, mobilzes hematopoeitic stem cells from bone marrow to peripheral blood.
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Granulocyte-Macrophage-Colony Stimulating Factor (Sargromastim, Leukine) MOA
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Stimulates the proliferation and stimulation of early and late granulocytic progenitor cells, erythroid, and megakayrocyte progenitors.
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Interleukin II (Oprelvekin, Neumega) MOA
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Stimulates the growth of megakaryocytic progenitors which increases platelets
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Antiplatelet Drugs:
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Aspirin and NSAIDS
ADP Inhibitors: Clopidigril and Toclipine Glycoprotein IIb/IIIa Inhibitors: Abciximab, Tirofiban, Eptifabitide Dipyridamole |
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Antiplatelet Drugs MOA: ADP Inhibitors - Ticlopidine and Clopidogrel
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Irreversible inhibitors of ADP binding to its receptor. Decrease ADP-mediated platelet aggregation.
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Antiplatelet Drugs MOA: Glycoprotein IIb/IIIa Inhibitors - abciximab, trofiban, and eptifibatide
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A cell surface receptor on platelets involved in platelet cross linking with fibrinogen for aggregation. GPIIb/IIIa inhibitors bind to this receptor and block fibrinogen from binding.
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Antiplatelet Drugs MOA: Dipyridamole
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Inhibits the uptake of adenosine into platelets, inhibits phosphodiesterase which then leads to increase cAMP, inhibits Thromboxane A2 synthesis.
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Anticoagulants: Oral and Parenteral
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Oral - Warfarin
Parenteral - 1. Unfractionated Heparin 2. LMW Heparin - Tinzaparin, Enoxaparin, Dalteparin and Danaparoid 3. Lepirudin or hirudin, desirudin, bivalrudin 4. Argatroban 5. Human recombinant antithrombin III: Endogenous Human Anticoagulant |
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Anticoagulants: Oral-Warfarin MOA
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Interferes with the vitamin K dependent y-carboxylation of glutamate residues on several clotting factors which renders them inactive.
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Anticoagulants: Unfractionated Heparin MOA
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Thrombin inhibitor, heparin binds to AT III and speeds up its activity.
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Anticoagulants: LMWH - Tinzaparin, Enoxaparin, Dalteparin, and Danaparoid MOA
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Preferentially inhibit factor Xa
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Anticoagulants: Direct Thrombin Inhibitors - Lepirudin MOA
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Lepirudin - binds and inactivates both fibrin bound thrombin and circulating thrombin
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Anticoagulants: Direct Thrombin Inhibitors - Desirudin MOA
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Desirudin - Similar to Lepirudin
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Anticoagulants: Direct Thrombin Inhibitors - Bivalirudin
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Bivalirudin - Similar to Lepirudin but synthetic - inhibits thrombin, reversible binding to thrombin.
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Anticoagulants: Argatroban MOA
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Argatroban MOA - Binds only to the active site of thrombin, not the exosite
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Thrombolytic Drugs:
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Tissue Plasminogen Activator t-PA
Streptokinase Anistreplase |
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Thrombolytic Drugs: Tissue Plasminogen Activator t-PA MOA
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Converts fibrin bound plasminogen to plasmin within clots
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Thrombolytic Drugs: Streptokinase MOA
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Forms a stable complex with plasminogen (1:1) exposing its proteolytic active site such that other plasminogen molecules get converted to plasmin
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Thrombolytic Drugs: Anistreplase MOA
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Is a prodrug converted to plasminogen, then plasmin
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Drugs for Bleeding Disorders:
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Vitamin K - Phytonadione or Menadione
Clotting Factors - Fresh frozen human plasma, factors VIII or IX Antiplasmin Agents - Aminocaproic Acid, Tranexamic Acid Protamine |
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Drugs for Bleeding Disorders - Antiplasmin Agents MOA
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Aminocaproic Acid, Tranexamic Acid - Inhibit conversion of Plasminogen to Plasmin
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Hypothalamic/Pituitary Hormones
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Oxytocin/Vasopressin
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Hypothalamic Hormones
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GHRH, Somatostatin, Thyrotropin Releasing Hormone, Corticotrophin Releasing Hormone, GnRH, LHRH Prolactin RH, Prolactin IH
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Somorelin does what?
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It is an analog for GHRH
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Octreotide is an analog for what?
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Somatostatin which inhibits release of GH, TSH, gastrin, glucagon, insulin, vasoactive intestinal peptide, GI motility, and sphlancnic blood blow.
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Proteirelin is an analog for what?
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TRH, this increases Thyroid Stimulating Release
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Gonadoralin and the synthetic Leuprolide
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Are analogs for Gonadotropin releasing hormone, they increase LH and FSH
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What are the GnRH analogs
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Nafarelin, goserelin and histrolin.
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What is a GnRH antagonist
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Ganirelix - prevents premature surges of LH
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Prolactin Inhibiting Hormone is?
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Dopamine - Inhibits Prolactin
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Growth hormone-Somatatropin analog
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Somatrem, Increases GH levels
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Anterior Pituitary Hormones are?
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GH, TSH, ACTH, FSH, LH
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TSH analog is
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Thyrotropin a - prompts iodine uptake in normal thyroid cells
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ACTH analog is?
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Cosyntropin - increases cortisol
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FSH analogs
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Follitropin B, Urofollitropin, Increases follicle development in females, and increases spermatogenesis in males.
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LH analog
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hCG human chorionic gonadotropin - is the major stimulate of gonadal steroid production.
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Oxytocin analog
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Syntocinon, increases uterine contraction and triggers milk ejection, increases post partum milk production
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ADH/Vasopression analog
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DDAVP - Desmopressin V2 recepotors in kidney, V1 receptors in vacular smooth muscle. Modified form of vasopression that has minimal activity at V1.
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Vasopression analog
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Aqueous vasopression
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Levadopa DDI
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Pyridoxiine, antipsychotic drugs, MAOIs - D/C at least two weeks prior to Tx with MAOIs
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Pramipexole DDI
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Cimetidine due to decreased renal tubular secretion, antipsychotic drugs
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Ropinirole DDI
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Ciprofloxacin, cimetidine, opioids, smoking increases clearance, food delays absorption, hepatic metabolism via CYP1A2
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Selegiline and Rasagiline DDI
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TCA, SSRIs, Meperidine, MAOIs - can lead to Seratonin Syndrome, hyperpyrexia, delirium, coma and death
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Rasagiline DDI
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Ciprofloxacin CYP1A2 inhibitor, inhibits metabolism and increases level of rasagiline two fold
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Anticholinergic DDI
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Other drugs with antimuscarinic activities
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Lithium DDI
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Plasma levels change with hydration status, dehydration, or patients taking diuretics increases lithium levels to toxicity. Thiazide diuretics, NSAIDS, decrease clearance toxicity. Theophyline increases Lithium's clearance rate. Antipsychotics increase risk of EPS, antimeitic effects of antipsychs can mask LI nausea. Li nausea is the first sign of Li intoxication. Increase dose during pregnancy, don't breast feed, decrease dose after birth.
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Meperedine DDI
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w/MAOIs death caused by hypertensive crisis and or serotonin syndrome. DDI with SSRI/TCA that can lead to serotonin syndrome
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Opioid DDI
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Other CNS depressants, ETOH, sedative hypnotics, anesthetics, antipsychotics, TCAs, antihistamines can have additive CNS depression
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Warfarin DDI
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Metabolized by CYP2C9, C19, 1A2, 3A4, and CYP450 inducers increase clearance, cause therapuetic failure (barbituates, CBZ, PHT), CYP450 inhibitors cause decreased clearance and bleeding. Warfarin is hihgly plasma protein bound, maintain consistent intake of dietary vitamin K and avoid NSAIDS and ASA, increased risk of GI bleed, avoid ETOH
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What is neuroleptic malignant syndrome?
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o Occurs with antipsychotics or an L-dopa drug holiday
o Fever, encephalopathy, unstable vitals, elevated enzymes, metabolic acidosis, rigidity of muscles |
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How do you treat it?
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o d/c neuroleptic, cool patient, give benzos, hydrate, alkalinize urine
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What 2 drugs are also used to treat hyperprolactinemia?
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o Bromocriptine and cabergoline
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What 2 drugs are also used to treat restless leg syndrome?
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o Pramipexole and Ropinirole
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Which drug must be given with an antiemetic?
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o Apomorpine
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Which 2 drugs cause heart valve problems?
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o Pergolide and cabergoline
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What 2 drugs are metabolized by CYP1A2?
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o Ropinirole and rasagiline
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What drug would increase their levels by inhibiting CYP1A2?
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o Ciprofloxacin
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Which drugs can be used alone to treat parkinsons initially?
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o Pramipexole, Ropinirole, selegiline, rasagiline
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Food delays the absorption of what 2 drugs?
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o L-dopa and ropinirole
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Which 2 drugs can cause arrhythmias?
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o L-dopa and amantadine
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• What 2 drugs are used for anti-emetics?
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o Prochlorperazine and droperidol
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• What drugs cause arrhythmias?
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o Thioridazine, Sertindole, Ziprasidone
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• What drugs are used for tourettes?
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o Pimozide (DOC), Haloperidol, Risperidone
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• What drugs block H1 receptors?
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o All atypicals (clozapine highly), and chlorpromazine
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• What are side effects common to older typical drugs?
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o Sedation, neuroleptic syndrome, extrapyramidal side effects, increased PRL secretion
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• What drugs are used to treat parkinsonian syndrome?
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o Benzotropine, trihexyphenidyl, amantidine
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• What drug is used to treat acute dystonic rxns (muscle spasms)?
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o Diphenyhydramine (benadryl)
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• What drug is used to treat neuroleptic malignant syndrome?
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o Bromocriptine
o DO NOT give dantrolene |
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• Which drugs is associated with impotence?
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o Thioridazine
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• What drug causes bone marrow suppression, agranulocytosis, and aplastic anemia?
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o Clozapine (take weekly WBC counts for 6 mo.)
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• What 2 drugs may improve negative schizophrenic symptoms?
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o Olanzapine, sertindole
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• What drug is used for refractory major depressive disorder?
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o Aripiprazole
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• Which drugs are given for agitation?
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o Haloperidol, olanzapine, ziprasidone
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• What drug is used for management of autism?
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o Risperidone
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• Which drug causes retinal deposits or “brown vision” at toxic levels?
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o Thioridazine
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• What are the therapeutic levels of lithium?
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o 0.8-1.2 mEq/L (>1.6 is intoxication)
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• What are the 4 endogenous opioid peptides?
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o Enkephalins, nociceptins, endorphins, endomorphins
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• What groups of peptides bind to Mu receptors?
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o Enkephalins and endomorphins, morphines and fentanyls
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• What binds to kappa receptors?
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o Dynorphins, morphine, nalmorphine
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• What drugs bind to the sigma site?
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o Pentazocine and nalorphine
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• What drug is the most euphoric?
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o Heroin
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• What is darvocet and what is a problem with it?
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o Propoxyphene + APAP, overdose is common
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• What is the main reason for deaths from opioid overdose?
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o Respiratory arrest, caution in patients with copd/asthma
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• Which opioids do not cause miosis?
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o Meperidene, amphetamine, cocaine
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• What symptoms of opioids do not develop tolerance?
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o Miosis, constipation
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• Which drugs cause the most histamine release?
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o Morpine, meperidine
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• What drug is used to reverse trunk muscle rigidity from fentanyl and others?
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o Naloxone
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• What drug is preferred during labor and why?
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o Meperidine because of less effect on uterine tone
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• Which drug is metabolized to a convulsant metabolite?
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o Meperidine converted to normeperidine
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• What is the DOC for opioid overdoses?
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o Naloxone
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• What drug is given PO for alcohol/opioid dependence?
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o Naltrexone
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• What are 3 antitussive drugs?
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o Codeine, hydrocodone, detromethorphan
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• What are 3 anti-diarrhea drugs?
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o Diphenoxylate, loperamide, deodorized tincture of opium
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• What drug is used for withdrawal management?
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o Methadone
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• What has to be prescribed with iron supplements?
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o Stool softeners
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• Which drug requires a small test dose due to anaphylaxis?
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o Iron dextran
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• What are cobalamins and what are they used for?
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o Isomers of B12, used for B12 deficiency
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• What are 4 reasons the folic acid cycle is important?
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o Synthesis of purines, DNA, methionine, and decreases levels of homocysteine (causes heart probs)
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• What 3 drugs cause folate deficiencies?
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o Methotrexate, trimethoprim, pyrimethamine
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• What are A.R.s of erythropoietin?
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o HTN, DVT, PE
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• What are myeloid growth factors (GCSF/GMCSF) used for?
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o Chemo induced neutropenia, any neutropenia, aplastic anemia
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• What are some A.R.s of GCSF?
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o Bone pain, hypersensitivity rxns, spenomegaly (long term use), rare nectrotizing vasculitis
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• Besides these what are A.R.s of GMCSF?
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o Flu symptoms, peripheral adema, pericardial/pleural effusion
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• What other growth factor increases fluid retention?
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o Interleukin 11/ oprelvekin (caution in CHF)
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• What kind of drugs are used to treat arterial thrombosis?
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o Antiplatelet agents
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• What drugs are used to treat venous thrombosis?
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o Anticoagulants
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• What are the types of antiplatelet drugs?
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o COX inhibitors, ADP inhibitors, glycoprotein IIb/IIIa inhibitors
|
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• What drugs are used only acutely after angioplasties?
|
o Abciximab, eptifibatide, tirofiban
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• What drug is used for cardiac perfusion tests?
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o Dipyridamole (it’s a vasodilator)
|
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• How does warfarin work?
• How is this treated? o Immediately stop heparin/LMWH and provide anticoagulation if necessary o Do not give heparin or warfarin • What anticoagulants can be used in these patients? o Fondaparinux, Argatroban, lepirudin, bivalirudin, danaparoid (outside U.S.) • What conditions are contraindicated for LMWH and Fondaparinux? o Patients with epidurals and intrathecal catheters • What drug is used for disseminated intravascular coagulation (DIC)? o Antithrombin III • How do thrombolytic drugs work? o Convert plasminogen to plasmin to split clots • What is a A.R. of streptokinase? o Systemic fibrinolysis, antigenic responses • What can be given to patients with hemophilia? o Clotting factors VIII, IX, fresh frozen plasma, aminocaproic acid, and tranexamic acid • T/F do LMWH require lab monitoring? o False • What drugs increase INR when given with warfarin? o Amiodarone, azithromycin, bactrim, ciprofloxacin, dexamethasone, antiarrhythmics, cephalosporins, nsaids, pain relievers, statins • What drugs decrease INR when given with warfarin? o Anti-thyroids, barbiturates, OCPs |
o Blocks vit. K action on clotting factors = inactivates them
o Interferes with clotting factors 2,7,9,10 o Interferes with protein C and protein S |
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• What does it mean for warfarin to be a category X drug?
|
o Causes severe birth defects such as bleeding and bone defects
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• How is warfarin toxicity reversed (also if INR >9)?
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o Vitamin K, fresh frozen plasma, factor IX
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• What enzymes metabolize warfarin?
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o CYP2C9, 2C19, 1A2, 3A4
o CYP450 inducers increase clearance = decrease INR o CYP450 inhibitors cause decreased clearance = increase INR • Other DDIs with warfarin are? o PPB drugs, NDAIDs, ASA, EtOH |
|
• What drug is given for heparin overdoses?
|
o Protamine
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• How does heparin work?
|
o Binds to ATIII leading to thrombin inactivation
|
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• How do you monitor Warfarin levels?
|
o PT/INR tests
|
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• How do you monitor heparin levels?
|
o PT tests
|
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• How do LMWH work?
|
o Inhibit factor Xa
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ARTICLE:
• What is heparin induced thrombocytopenia? |
o Unfractionated Heparin binds to platelet factor 4 (PF4) on some cells causing antibodies to be made, leading to thrombin generation and thrombosis
|
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• How is this treated?
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o Immediately stop heparin/LMWH and provide anticoagulation if necessary
o Do not give heparin or warfarin |
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• What anticoagulants can be used in these patients?
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o Fondaparinux, Argatroban, lepirudin, bivalirudin, danaparoid (outside U.S.)
|
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• What conditions are contraindicated for LMWH and Fondaparinux?
|
o Patients with epidurals and intrathecal catheters
|
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• What drug is used for disseminated intravascular coagulation (DIC)?
|
o Antithrombin III
|
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• How do thrombolytic drugs work?
|
o Convert plasminogen to plasmin to split clots
|
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• What is a A.R. of streptokinase?
|
o Systemic fibrinolysis, antigenic responses
|
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• What can be given to patients with hemophilia?
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o Clotting factors VIII, IX, fresh frozen plasma, aminocaproic acid, and tranexamic acid
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• T/F do LMWH require lab monitoring?
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o False
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• What drugs increase INR when given with warfarin?
|
o Amiodarone, azithromycin, bactrim, ciprofloxacin, dexamethasone, antiarrhythmics, cephalosporins, nsaids, pain relievers, statins
|
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• What drugs decrease INR when given with warfarin?
|
o Anti-thyroids, barbiturates, OCPs
|