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53 Cards in this Set
- Front
- Back
Alteplase
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Largest Drug with a MW of 60,000 used to dissolve clots
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Phenoxybenzamine
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Noncompetitive antagonist of Norepinephrine which functions by blocking the alpha adrenoreceptors for it
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Carvedilol
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Nonselective Beta blocker used to treat congestive heart failure
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Ketamine
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An intravenous anesthetic which is still used as a racemic mixture
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Gleevec
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Drug developed by Novatis used to treat CML Chronic myelogenous leukemia
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Atropine
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Antagonist of acetylcholine that functions by blocking the acetylcholine receptor
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Fick's Law
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Law that describes diffusion
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Form of transport responsible for Iron and Vit B12
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Endocytosis
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Equation of Fick's Law
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Flux=(C1-C2) x Area x Perm Coeff x thickness^-1
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Gout
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Inflammatory reaction of tissues caused by buildup of uric acid in joints
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E=?
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(Emax)(c)/ (Ec50) + (c)
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B=?
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(Bmax)(c)/(Kd) + (c)
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Myocardium has a large proportion of what?
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Spare B-adrenoceptors
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Schild Equation
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C'/C = 1 + [I]/KI
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Example of Chemical Antagonism
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Heparin is a very negative anticoagulant and protamine sulfate is very positive so protamine can bind to heparin to inactivate it
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Example of Physical Antagonism
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Insulin which lowers blood sugar and glucocorticoids which increases it
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Discovery of John Langley
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Curare did not prevent electrical stimulation of muscle but blocked contraction triggered by nicotine
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Discovery of Paul Ehrlich
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Certain synthetic organic agents had antiparasitic effects while others with nearly identical structures did not
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Isoproterenol
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Beta-Adrenoreceptor agonist that mimics sympathetic stimulation to increase heart rate
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NO mechanism of Action
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Enters the cell via diffusion and activates guanylyl cyclase to produce cGMP
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Which vitamins are lipid soluble?
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Vit ADEK
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Herceptin
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a.k.a Trastuzumab used for anti-breast cancer treatment works by acting as antagonist of the Her2/neu receptor tyrosine kinase
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Two types of EGFR-TK inhibitors used for cancer treatment
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Gleevec by Novatis
and Herceptin by Genetech and Roche |
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Signaling path & Function of TGF-B
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Ser/Thr Kinases & regulates growth and cell proliferation by blocking growth of many different cells
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Path & Function of ANP
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Ligand Regulated Guanylyl Cyclase receptors & Functions in regulating blood volume and vascular tone
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What is the rate limiting step in second messenger signals?
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Hydrolysis of GTP to GDP so does not matter if ligand is bound or not
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Gs
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Up Adenyl Cyclase to up cAMP and Ca++ channel
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Gi
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Downs Adenyl Cyclase & opens K++ channels to dec heart rate
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Gq
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Up IP3 DAG & Ups cytoplasmic Ca++
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Receptor regulation mechanism in the B-Adrenoceptor
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Ligand binding activates Gs-GTP and B-ARK aswell which phosphorylates cytoplasmic tail due to high amount of serine and threonine residues & causes binding of B-arr to block 3rd intracellular loop
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Substance that cleaves phosphates from Tails
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Phophatase
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Methylxanthine Drug Effects
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Competitive inhibitors of PDE
Ups Alertness, secretion, enzymes, smooth muscle dialation treats asthma Downs Na reabsorption, causes weak diuretics |
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PLC pathway and 3 ways to terminate it
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PLC hydrolyze PIP2 into DAG & IP3
IP3 causes release of calcium which binds to calmodulin to phosphorylate substrate DAG activates PKC which phosphorylates substrates aswell IP3 is rapidly dephosphorylated by phosphatases DAG is either dephosphorylated or deacylated to form archidonic acid Cell actively removes Ca+ from cytoplasm with pumps |
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Which 2 places have cGMP based signal transduction?
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Intestinal Mucosa and Smooth Muscle
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What does NO activate?
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Diffuses into the cell and directly activates GC to produce cGMP
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3 Norepinephrine Receptor Classes
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B-adrenergic:Gs ups heart rate
a1-adrenergic:Gq vasoconstriction a2-adrenergic: Gi opening of K+ gates and decreases heart rate |
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Tamoxifen
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Antagonist on estrogen receptors in breast tissue to prevent breast cancer
Agonist in estrogen receptors in bone to reduce osteoperosis Agonist on estrogen receptors in uterus causing cell proliferation leading to cancer |
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Nobel Prize winner for discovery of NO
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Ferid Murad
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Viagra Acts on what?
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PDE subtype 5 to prevent cGMP from becoming GMP
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what does clinical effect of a drug in patients depend on?
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Maximal Efficacy
NOT POTENCY |
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TI=?
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TD50/ED50
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Idiosyncratic
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Unusual response not seen in most PTs
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Hyporeactive
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Drug effect is smaller than expencted
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Hypereactive
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Drug effect is greater than expected
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Hypersensitive
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Allergic reaction to drug
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Tolerance
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Desensitization to drug due to prolonged administration
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Tachyphylaxis
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Abnormally rapid desensitization to drug
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Saralasin
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Weak partial agonist of angiotensin receptors which raises BP so will lower BP in HTN patients but will raise BP in patients with low levels of angiotensin
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Clonidine
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Agonist of a2-adregenic receptor to reduce BP so can cause hypertensive crisis if removed abruptly
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Prazosin
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a1-adrenergic receptor antagonist lowers BP by acting on vascular smooth muscle
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Methotrexate
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Drug that kills tumor cells by inhibiting dihydrofolate reductase but kills healthy cells too
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Asprin
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Cox 1&2 inhibitor that acts on cyclo-osygenase to reduce inflammation caused by archidonic acid
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Vioxx
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Drug that acts on Cox 2 inhibitor which like asprin acts on cyclo-oxygenase to lower inflammation but was pulled from marked because it caused heart problems
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