Pharm3 - Week 1
Terms
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- Weird side effect of aspirin
- Tinnitus
- Ticlopidine
-
Hypercoagulability
Anti-PLATELET
Inhibits ADP from binding to platelet receptors -> v activation of GPIIb/IIIa - Dipyridamole
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Hypercoagulability
Anti-platelet
^ platelet cAMP levels -> inhibits platelet activation - Clopidogrel
-
Hypercoagulability
Anti-platelet
Inhibits ADP from binding to platelet receptors -> v activation of GPIIb/IIIa - Abciximab
- monoclonal antibody to GP IIb/IIIa receptor
- What can Vitamin E and Garlic cause in proper circumstances?
- Bleeding
- Warfarin MOA
- Antagonize Vitamin K, which makes Factors II, VII, IX, and X nonfuctional
-
What rate is used to measure monitor Warfarin?
What should the range be? -
INR (internal Normalized Ratio) = (partient's Prothrombin Time/mean normal PT in seconds)
2-3 - What interferes with Warfarin?
- Foods with Vitamin K and ginseng
- Heparin MOA
-
potentiate antithrombin III
inactivates IIa, IXa, Xa, XIa & XIIa
act in many steps to not get crosslinked fibrin - Enoxaparin
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Anticoagulant
Low Molecular Weight Heparin
Only inhibits Xa to inactivate thrombin - Major SE of Heparin (less so w/ LMWH)
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Heparin-Induced Thrombocytopenia (HIT)
v amount of platelet count - Lepirudin
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Direct Thrombin Inhibitor
1st line for HIT - Argatroban
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Direct Thrombin Inhibitor
1st line for HIT - Streptokindase
- Plasminogen Activator
- Urokinase
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Thrombolytic
Plasminogen Activator - Tranexamic Acid
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Procoagulant
Fibrinolysis inhibitors - Essential Nutrients for RBC production (erythropoiesis)?
- Folate, B12 & iron
- What nutrient is key for AA and purine synthesis?
- Folate
- Where is folate absorbed, stored and for how long?
- proximal jejunum; liver; 1-6 months
- Folate deficiency leads to?
-
1) MACROcytic/megaloblastic Anemia
2) Slow down nuclear replication -
*Methotrexate blocks what nutrient?
also oral contraceptives, Isoniazid, and Phenytoin and Trimethoprim block as well - Folate
- Wernicke-Korsakoff has what deficiency?
- Thiamine (B1)
- Pernicious Anemia
- Vitamin B12 deficiency
- Difference b/w Folate and Vitamin B12 (cobalamine) Megaloblastic anemia?
-
Vitamin B12 = neuroloical syndrome
-paresthesias
-weakness
-ataxia
Folate: no neurologic syndromes - Iron deficiency causes?
- MICROcytic anemia (too little cytoplasm
- What is an adequate measure of total body iron stores?
- Plasma Ferritin
- Do sickle cell patients have iron deiciency?
- No
- Transferrin
- ^ during v storage iron to ^ import of more iron from GI mucosa
- Weird SE of oral iron
- Black stool
- Acute iron toxicity causes?
- Necrosis of gut
- Do you give sickle cell patients iron?
- No, they do not have an Iron deficiency
- Erythropoietin
-
Main growth factor for Hematopoiesis
Produced by peritubular system of the kidney
Epo level drop = red cell production drop
Travels to BM & v apoptosis to ^ RBC - Thyroid System is directly triggered/impacted by what?
- Temperature
- Liothyronine
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T3
Used only in acute situations (ie Myxedema coma) b/c faster acting than T4 - Levothyroxine
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T4
Almost always the DOC for Hypothyroidism (except for acute situations -> T3) - Propothiouracil (PTU)
-
Anti-thyroid
Inhibits iodide organification
AND
Coupling of MIT & DIT
Conversion of T4 -> T3
FASTER onset than Methimazole but take 3x daily - Methimazole
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Anti-thyroid
ONLY Inhibits iodide organification (iodination of tyrosine in thyroglobulin)
SLOWER onset than Propothiouracil but only give 1x daily - B-Blockers' and Corticosteroids hormonal action
- Antagonize effects of thyroid hormone
-
Expression of Na/K ATPase is regulated hormonally by?
Thereby important in the metabolsm of ALL cells - T3
- Cretinism (short stature) is caused by?
- Lack of thyroid hormone during development
- Give high dose of iodide therapy 2 weeks prior to surgical storm?
- YES, shrinks thyroid making surgery easier
- Give high dose of iodide therapy prior to implantation of radioactive iodide?
- NO, b/c it would block the uptak of the radioactive iodide
- Calcitriol
-
1, 25-dihydroxy D3 (renal-activated form of Vitamin D)
stimulates the intestine to increase absoprtion of phosphate and calcium (esp in intestine, kidney, & bone -
For Hypocalcemia w/
Hepatic Failure - Give 25-Hydroxy D3
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For Hypocalcemia w/
Renal failure - Give 1,25-Dihydroxy D3
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For Hypocalcemia w/
Normal Renal and Hepatic fxn - Give vitamin D3
- Unlike thyroid hormone, effects of 1,25-Dihydroxy D3 not found all over the body but mostly in?
- Gut
- Calcitonin synthesized in?
- Thyroid gland
- Net affect of Vit D and Parathyroid hormone?
-
increasing Ca in
1)intestine
2)kidney
3)bone -
Biphosphonates are a class of drugs useful for? **ALENDRONATE**
Etidronate
Pamidronate
Pyrophosphate -
Treatment of Osteoporosis
**SE: Esophageal erosion** - Penicillin most useful for what bacteria?
- Gram +
- Main difference b/w Cycloserine and Penicillin?
- Cycloserine is REVERSIBLE and Penicillin is IRREVERSIBLE
- What are the 5 classes of immunosuppressnt agents?
-
1)T Cell blockers
2)Glucocorticoids
3)Cytotoxic drugs
4)Antibody reagents
5)Cytokine inhibitors - Cyclosporine
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Immunosuppressant - T-cell Blocker
Organ transplant, Autoimmune Dz (RA), & Psoriasis
Binds cyclophilin, and the cyclosporine=cyclophilin complex inhibits calcineurin (decrease in IL-2 production which is a T cell growth factor)
Narrow TI
SE: Nephrotoxicity, HT, CYP450 ACTIVATION! - Tacrolimus
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Immunosuppressant - T-cell Blocker
Organ Transplant
Binds FKBP, complex then inhibits calcineurin (decrease in IL-2 production which is a T cell growth factor)
MORE potent than cyclosporine
Narrow TI
SE: Nephrotoxicity, Neurotoxicity, Diarrhea, CYP450 ACTIVATION! - Sirolimus
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Immunosuppressant - T-cell Blocker
Organ Transplant, Antifungal agent
Binds FKBP, complex but DOES NOT inhibit calcineurin It inhibits signal pathway from IL-2 recepor to the DNA transcription --> decresed IL-2 responsiveness (v T cell
AND B cells growth)
SE: CYP450 ACTIVATION!
LESS NEPHROTOXICITY than Cyclosporine and Tacrolimus - Prednisone
-
Immunosuppressant - Glucocorticoid
Organ trasplant & Autoimmune Disease
Converts to Prednisolone
Antiinflammatory: ^ Neutrophils & v lymphocytes (B AND T cells) & cytokines in circulation
Pharmadynamic effect is longer than its pharacokinetic effect (short 1/2 life, longer effective duration)
SE: Adrenal insufficiency - Azathioprine
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Immunosuppresant - Cytotoxic Agent - PURINE
Organ Transplants, Auntoimmune DX (RA)
Adenine Analog - ANTAGONIST TO PURINE SYN which lymphocytes need for proliferation
Pharmadynamic effect is longer than its pharacokinetic effect
SE: v Renal and Hepatic fxn
** AVOID ALLOPURINOL Interaction -> inhibits xanthine oxidase which inactivates activity; THUS Allopurinol causes ^ levels of azathioprnie -> PANCYTOPENIA - Mycophenylate Mofetil
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Immunosuppresant - Cytotoxic Agent - PURINE
Organ Transplants
Inibits IMP Dehydrogenase -> inhibits de novo synthesis of Purines
Undergoes enterohepatic circulation --> inactive metabolites activated in liver
SE: GI upset, BM suppression & Infection risk - Cyclophosphamide
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Immunosuppresant - Cytotoxic Agent - Alkalating Agent
Interferes with DNA replication and transcription of RNA, thus disrupting nucleic acid function
SE: GI upset, cardiotoxicity BM suppression & NEOPLASIA (esp BLADDER cancer) - Leflunomide
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Immunosuppressant - Cyotoxic Agent - PYRIMIDINE
Used mainly for RA
SE: alopecia, N/V, diarrhea, rash - Antithymocyte Globulin
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Immunosuppresant - Antibody Reagent
Organ transplants
Purified Animal Gamma Globulin (mailinly IgG) against T lymphocytes
SE: Allergic Rxn - OKT3
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Immunosuppresant - Antibody Reagent
Organ transplants (ACUTE REJECTION)
Used in conjunction with Azahioprine & Corticosteroids
Murine monoclonal T3 antibody --> blocking fxn of all T cells
SE: Flu-like symptoms, HA, seizures, aseptic meningitis and encephalopathy - Basiliximab
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Immunosuppresant - Antibody Reagent
Organ transplants (ACUTE REJECTION)
Used in conjunction with Azahioprine & Corticosteroids
Monoclonal antibody from Human recombinant DNA - blocks CD 25 -> inhibits T Lymphocytes
SE: Hypersensitivity - Daclizumab
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Immunosuppresant - Antibody Reagent
Organ transplants (ACUTE REJECTION)
Used in conjunction with Azahioprine & Corticosteroids
Monoclonal antibody from Human recombinant DNA - blocks CD 25 -> inhibits T Lymphocytes
SE: Gi effects, HA, dizziness, otherwiise well tolerated compared to other agents - Etanercept
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Immunosuppressant: Cytokine Inhibitor
Autoimmune Dz (RA, Crohn's Dz)
Monoclonal IgG antibody from recombinant human DNA that binds specifically to TNF alpha --> Inhibition of inflammatory cascade
"EI EI LUPUUUUUUS"
"TNF-alpha now!"
SE: Infusion reactions, Upper respiratory infecions, LUPUS-llike syn - Infliximab
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Immunosuppressant: Cytokine Inhibitor
Autoimmune Dz (RA, Crohn's Dz)
Monoclonal IgG antibody from recombinant human DNA that binds specifically to TNF alpha --> Inhibition of inflammatory cascade
SE: Infusion reactions, Upper respiratory infecions, LUPUS-llike syn
"EI EI LUPUUUUUUS"
"TNF-alpha now!" - IV Immunoglobulin
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Immunostimulant
Used for Primary immune deficiency (ie AIDS)
Contain no IgM, variable IgA, and normal IgG
SE: allergic rxn -> anaphylaxis - INF Gamma 1B
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Immunostimulant
Prevention of infection in Chronic Granulomatous Dz - INF Beta 1a/b
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Immunostimulant
Used to reduce the severity of MS attacks - INF Alpha 2a/b
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Immunostimulant
Used in Hepatitis, HPV, Kaposi's sarcoma - IL-2
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Immunostimulant
stimulates T helper and T cytotoxic cells
HIGHLY TOXIC w/ life-threatening cardiotoxicity, pulmonary edema and renal toxicity - Levamisole
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Immunostimulant
Used in Hodgkin's Dz, RA, & Colorectal cancer
Causes macrophages and T cells to secrete cytokines and other factors suppressing tumor growth - St John's Wort
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Treat Depression
Can bind FXR receptor and activate CYP450 system - ^ metabolism of drugs such as cyclosporin & theophylline
DO NOT TAKE with MAO INHIBITORS - Echinacea
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Common Cold
DO NOT TAKE with IMMUNOSUPPRESSANTS (ie corticosteriods) - Saw Palmetto
- Treat BPH
- Cranberry Exract
- Treat UTI
- Ginkgo Biloba
- Treat Anxiety/Stress & Memory Loss
- Black Cohosh
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Treat Menopause
Contains isoflavones - *Grape Seed Extract
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Neuroprotective
high antioxidants - Garlic
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Contains *INDOLE-3-CARBINOL (found in broccili; anticancer properties) & *ALLICIN - both antioxidants
DO NOT TAKE with NSAIDs - Evening Primrose
- DO NOT TAKE with Anti-convulsants
- Ginseng
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Energy
DO NOT TAKE with NSAIDs - Yohimbe
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Depression
MAO inhibitor
TOXIC - PSYCHOSIS - Comfrey
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Demulcent
TOXIC - Hepatotoxicity - Chaparral
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Antibiotic
contains anti-oxidants
TOXIC - Hepatotoxicity - *Genistein
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also Red Clover & Kudzu
Soy products
An isoflavone resembling 17B-estradiol binding estrogen receptor SELECTIVELY in bone, brain, and CV system
Polyphenols have ANTIOXIDANT properties; may enhance cell viablilty/logevity by enhancing certian de-acetylases - Chinese Red Rice
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Treat hypercholesteremia
fungus that contains statins -> inhibition of HMG CoA Reductase - Tissue Plasminogen Activator
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U: Hypercoagulability
Thrombolytic (most common)
-specific for clot-bound plasma - What kind of iron is direcly absorbed?
-
Meat iron
Iron from other food sources must be reduced to ferrous to form Fe2+ before it can be actively tranproted into intestinal mucosa