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45 Cards in this Set
- Front
- Back
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Define: pharmacology
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Study of the interaction of chemical substances with living systems
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Define: drug
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Any substance that brings about a change in biologic function thru chemical reaction
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Define: receptor
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Specific regulatory molecule in biologic system upon which some drugs acts (activation or inhibition of normal body processes
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What is the therapeutic benefit of a drug?
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1. Derived by acting on processes within the patient, 2. derived by acting on processes directed at parasites infecting the patient
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Define: agonist
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Drug that binds to receptor + stimulates cellular activity
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Define: antagonist
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Drug that binds to receptors and inhibits the action of agonists(drugs or endogenous agents)
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Example of endogenous drugs?
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Hormones
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Example of exogenous drugs
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Xenobiotics (stranger)
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Example of toxin
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Dioxin
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Example of inorganic poison
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Lead, argon
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Advantage of small drugs
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Goes thru membranes (lipophilic), goes thru pores(if aqueous), distribution
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What is the molecular weight of the majority of drugs?
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100 or 1000
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What is the advantage of low molecular weight(ie Li)?
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Lower limit allows SPECIFICITY of drug interaction (can have a good fit for one type of receptor)
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What is the advantage of high molecular weight(ie alteplase [t-PA])?
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Upper limit determines extent of movement within the body(ie from administration site -> site of action)(alteplase - administed in blood and stays there b/c of its size)
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What concept explains drug to receptor interaction?
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Lock and key - only a few receptor types(lock) are likely to provide such a precise fit for a particular drug structure (key)
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Carvedilol has S and R enantiomers- what is the Kd for each?
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Beta-receptors - S = Kd = 0.4(potent beta-receptor blocker), R = Kd = 45nM (100x weaker beta-receptor blocker)
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Warfarin is given as a racemic mixture- what is the function or S and R enantiomer
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S enantiomer = 4x more potent than R; Interaction with binding site on Vitamin K epoxide reductase
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What is the cause of enzymes having different duration of action on enantiomers of the same drug?
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Enzymes are STEREOSELECTIVE
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Lower Kd = ie 0.4
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higher affinity for the receptor
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Higer kd = ie 45
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Lower affinity for the receptor
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What does pH (body compartments) do to a drug?
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Affects the ionization of drugs b/c drugs are weak acids/weak bases (each has a unique pK)
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What are the protein targets of drugs?
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1. Receptors, 2. enzymes, 3. carrier molecules, 4. ion channels, 5. structural proteins (colchicine binds to tubulin -> inhibits mitosis)
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What is the function of colchicine on mitosis?
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Colchicine binds to tubulin -> inhibits mitosis
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Define: receptors
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System of chemical communication that all multicellular organisms use to coordinate the activities of their cells and organs
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How many times does the receptor cross the cell membrane?
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7 transmembrane receptor
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What is an example of chemical antagonist?
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Protamine -> binds to heparin(anticoagulant) -> stops bleeding
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What is an example of physiologic antagonists?
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Adrenergic beta-blockers -> thyroid hormone -induced tachycardia
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What is an example of osmotic agents
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Mannitol -> for subarachnoid hemmorhage
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What is an example of DNA agents?
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Cancer chemotherapeutic agents
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Define: pharmacodynamic interactions
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Actions of drugs on the body
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Define: pharmacokinetic interactions
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Action of the body on the drug
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What is the function of fluoxetine?
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PROZAC = Anti-depressant
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Define: indication
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The basis for the initiation of treatment - ie fluoxetine = used for major depressive disorder
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What type of people are Propranolol contranidicated in?
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asthmatics
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Define: MOA
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Mechanism of action = how the drug works - includes sites where the drug acts and mechanism by which it produces effects(ie propranolol blocks -beta-adrenergic receptors in heart myocardium -> ↓ sympathetic-mediated contractile force -> used as anti-hypertensive agent)
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Define: side effect
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Undesired effects of drug - ie propranolol is good for anti-hypertensives but also blocks beta receptors in lungs -> broncho-constriction = bad for asthamtics/obstructive lung disorder patients
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Define: contraindication
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Condition that precludes safe use of drug(ie propanolol is contraindicated in asthamtics b/c beta-blockers also work on the lung and causes boncho-constriction
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What type of patient is atropine contraindicated in?
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Narrow-angle glaucoma
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What is the normal action of atropine
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Muscarinic blocker -> Produce mydriasis and cycloplegia prior to refraction, treat spastic disorders of GI and lower urinary tract, treat organophosphate poisoning, suppress respiratory secretion prior to surgery
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What are the adverse effects of cholinergic antagonists?
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Blurred vision, confusion, mydriasis, constipation, urinary retention
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What is the therapeutic use of scopolamine?
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In obstetrics w/morphine to produce amnesia + sedation, prevent motion sickness
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What is the therapeutic use of ipratropium
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Treat asthma
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What is the therapeutic use of trimethaphan
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Short-term treatment of hypertension
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What is the therapeutic use of mecamylamine
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Treatment of mederatly severe to severe hypertension
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What changes the effects of a drug?
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1. State of health = poor heath, cormorbidities,2. pediatric (incomplete tests), 3. geriatic = ↓ blood supply -> ↓ absorption & distribution, ↓ renal function -> ↑ half-life, ↓ liver function -> ↓ plasma protein binding & ↓ volume of distribution, 4. pharmacogenetics, 5. gender, 6. pregnancy
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