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53 Cards in this Set

  • Front
  • Back
Alteplase
Largest Drug with a MW of 60,000 used to dissolve clots
Phenoxybenzamine
Noncompetitive antagonist of Norepinephrine which functions by blocking the alpha adrenoreceptors for it
Carvedilol
Nonselective Beta blocker used to treat congestive heart failure
Ketamine
An intravenous anesthetic which is still used as a racemic mixture
Gleevec
Drug developed by Novatis used to treat CML Chronic myelogenous leukemia
Atropine
Antagonist of acetylcholine that functions by blocking the acetylcholine receptor
Fick's Law
Law that describes diffusion
Form of transport responsible for Iron and Vit B12
Endocytosis
Equation of Fick's Law
Flux=(C1-C2) x Area x Perm Coeff x thickness^-1
Gout
Inflammatory reaction of tissues caused by buildup of uric acid in joints
E=?
(Emax)(c)/ (Ec50) + (c)
B=?
(Bmax)(c)/(Kd) + (c)
Myocardium has a large proportion of what?
Spare B-adrenoceptors
Schild Equation
C'/C = 1 + [I]/KI
Example of Chemical Antagonism
Heparin is a very negative anticoagulant and protamine sulfate is very positive so protamine can bind to heparin to inactivate it
Example of Physical Antagonism
Insulin which lowers blood sugar and glucocorticoids which increases it
Discovery of John Langley
Curare did not prevent electrical stimulation of muscle but blocked contraction triggered by nicotine
Discovery of Paul Ehrlich
Certain synthetic organic agents had antiparasitic effects while others with nearly identical structures did not
Isoproterenol
Beta-Adrenoreceptor agonist that mimics sympathetic stimulation to increase heart rate
NO mechanism of Action
Enters the cell via diffusion and activates guanylyl cyclase to produce cGMP
Which vitamins are lipid soluble?
Vit ADEK
Herceptin
a.k.a Trastuzumab used for anti-breast cancer treatment works by acting as antagonist of the Her2/neu receptor tyrosine kinase
Two types of EGFR-TK inhibitors used for cancer treatment
Gleevec by Novatis

and Herceptin by Genetech and Roche
Signaling path & Function of TGF-B
Ser/Thr Kinases & regulates growth and cell proliferation by blocking growth of many different cells
Path & Function of ANP
Ligand Regulated Guanylyl Cyclase receptors & Functions in regulating blood volume and vascular tone
What is the rate limiting step in second messenger signals?
Hydrolysis of GTP to GDP so does not matter if ligand is bound or not
Gs
Up Adenyl Cyclase to up cAMP and Ca++ channel
Gi
Downs Adenyl Cyclase & opens K++ channels to dec heart rate
Gq
Up IP3 DAG & Ups cytoplasmic Ca++
Receptor regulation mechanism in the B-Adrenoceptor
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
Substance that cleaves phosphates from Tails
Phophatase
Methylxanthine Drug Effects
Competitive inhibitors of PDE

Ups Alertness, secretion, enzymes, smooth muscle dialation treats asthma

Downs Na reabsorption, causes weak diuretics
PLC pathway and 3 ways to terminate it
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
Which 2 places have cGMP based signal transduction?
Intestinal Mucosa and Smooth Muscle
What does NO activate?
Diffuses into the cell and directly activates GC to produce cGMP
3 Norepinephrine Receptor Classes
B-adrenergic:Gs ups heart rate

a1-adrenergic:Gq vasoconstriction

a2-adrenergic: Gi opening of K+ gates and decreases heart rate
Tamoxifen
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
Nobel Prize winner for discovery of NO
Ferid Murad
Viagra Acts on what?
PDE subtype 5 to prevent cGMP from becoming GMP
what does clinical effect of a drug in patients depend on?
Maximal Efficacy

NOT POTENCY
TI=?
TD50/ED50
Idiosyncratic
Unusual response not seen in most PTs
Hyporeactive
Drug effect is smaller than expencted
Hypereactive
Drug effect is greater than expected
Hypersensitive
Allergic reaction to drug
Tolerance
Desensitization to drug due to prolonged administration
Tachyphylaxis
Abnormally rapid desensitization to drug
Saralasin
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
Clonidine
Agonist of a2-adregenic receptor to reduce BP so can cause hypertensive crisis if removed abruptly
Prazosin
a1-adrenergic receptor antagonist lowers BP by acting on vascular smooth muscle
Methotrexate
Drug that kills tumor cells by inhibiting dihydrofolate reductase but kills healthy cells too
Asprin
Cox 1&2 inhibitor that acts on cyclo-osygenase to reduce inflammation caused by archidonic acid
Vioxx
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