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85 Cards in this Set
- Front
- Back
What is Km?
What is Vmax? |
Km - affinity of the enzyme for its substrate...as Km decreases...affinity increases
Vmax - enzyme concentration; maximum velocity that an enzyme can breakdown substrate...adding more substrate past this point will NOT speed up a reaction...since the enzymes are saturated |
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Competative Inhibition causes a change in Km or Vmax?
Noncompetative Inhibition causes a change in Km or Vmax? |
KoMpetative Inhibition = Km Increases (no change in Vmax)
NOn-Kompetative inhibition = NO Km increase (but increase in Vmax |
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What does the mnemonic ENVY mean?
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E - efficacy DECREASES
N - non-competative V - Vmax DECREASES Y - y-intercept (1/Vmax) |
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Volume of distribution (Vd) of plasma protein-bound drugs can be altered by ______ and ______ disease.
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Kidney (proteinuria = decrease protein in body)
Liver (decrease protein synthesis) |
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Low Vd (4-8L) distrubutes in the ______
High Vd (>body weight) distrubutes into _______ |
blood
all tissues |
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How many half lives does it take to reach steady state?
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Usually 5! (FA said 4-5....Goljan says 5)
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What is the clearance (CL) rate equation?
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(rate of drug elimination)/(plasma drug concentration)
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In renal and/or liver disease...how are maintenance and loading doses adjusted?
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Maintenance dose = decreased***
Loading dose = unchanged |
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A drug with a high Vd will require a high or low loading dose?
A drug with a high clearance rate will require a high or low maintenance dose? |
HIGH
HIGH |
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1st order drug elimination = constant ________ of drug eliminated per unit time
Zero order drug elimination = constant ________ of drug eliminated per unit time |
fraction
amount |
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Weak acids are get trapped in acidic or basic environments? Tx overdose of a weak acid with ________
Weak bases are get trapped in acidic or basic environments? Tx overdose of a weak base with ______ |
trapped in basic environments - tx overdose with bicarbonate (ionized = trapped in urine and cleared quickly)
Trapped in acidic environments - tx overdose with ammonium chloride (ionized = trapped in urine and cleared quickly) |
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Reduction, Oxidation, Hydrolysis .... phase I or II metabolism?
Acetylation, Glucuronidation, Sulfation .... phase I or II metabolism? |
Phase I
Phase II |
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Geriatric patients lose phase I or phase II metabolism first?
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Phase I first (reduction, oxidation, hydrolysis)
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Most important component of Phase I metabolism is _________
Most important component of Phase II metabolism is _________ |
cytochrome P450
conjugation |
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What is the difference between efficacy and potency?
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Efficacy - maximal effect a drug can produce
Potency - amount of drug needed for a given effect |
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A competitive antagonist decreases efficacy or potency?
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potency
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A noncompetitive antagonist decreases efficacy or potency?
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efficacy
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Give an example of a physiologic antagonism
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Pt who has asthma d/t muscarinic overactivity (contracts smooth m), EPI can act as a bronchodilator by stimulating B2 receptors
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Sweat glands are part of the SNS & are innervated by _______ fibers
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cholinergic (ACh binding to Mreceptors)
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What do these agents have in common?
Hemicholinium Vesamicol Botulinum |
All act to decrease cholinergic activity:
Hemicholinium - blocks reuptake of choline at the presynaptic nerve Vesamicol - blocks uptake of ACh into presynaptic vesicles Botulinum - blocks release of ACh from presynaptic nerve |
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What drug is used for postoperative and neurogenic ileus and urinary retention?
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Bethanechol ("activates Bower and Bladder smooth muscle"!)
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What is pilocarpine used for?
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potent stimulator of sweat, tears and saliva
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What is methacholine used for?
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Methacholine Challenge Test for dx of asthma!
-stimulates muscarinic receptors in airway when inhaled |
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What do the -stigmine drugs (ie. neostigmine) do?
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Indirect cholinomimetic agonists....work by blocking acetylcholinesterases
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Which drug is used for diagnosis of asthma?
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Methacholine
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Which drug is used for diagnosis of myasthenia gravis?
Which drug is used for treatment of myasthenia gravis? |
Edrophonium (extremely short acting)
Pyridostigmine (long acting) -both drugs block acetylcholinesterase! |
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With all cholinomimetic agents, what do you have to watch for?
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exacerbation of:
COPD asthma peptic ulcers (when giving to susceptible pt's) |
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Which two anticholinesterases are used for glaucoma?
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Physostigmine (crosses BBB)
Echothiophate |
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What's the antidote for an anticholinesterase drug?
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Atropine (M blocker) + pralidoxime (regenerates active AChE) -- remember 2PAM!?
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Atropine, homatropine, tropicamide are a muscarinic blocker that works in what organ system?
Also..what is it's clinical use? |
Organ system: eye
Clinical use: produce mydriasis (block PNS..so more SNS effect) and cycloplegia (loss of accomidation) |
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Benztropine is muscarinic blocker that works in what organ system?
Also..what is it's clinical use? |
CNS
Parkinson's dz ("PARK my BENZ") |
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Scopolamine is muscarinic blocker that works in what organ system?
Also..what is it's clinical use? |
CNS
motion sickness |
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Ipratroprium (bromide) is muscarinic blocker that works in what organ system?
Also..what is it's clinical use? |
Respiratory
Asthma, COPD ("I pray I can breath soon!") |
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Oxybutynin & glycopyrrolate are muscarinic blockers that works in what organ system?
Also..what is it's clinical use? |
Genitourinary system
reduce urgency in mild cystitis & reduce bladder spasms |
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Methscopolamine & propantheline are muscarinic blockers that works in what organ system?
Also..what is it's clinical use? |
Genitourinary system
Peptic ulcer treatment |
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Drug reactions:
Atropine-like side effects (antimuscarinic) |
Tricyclic Antidepressants (TCA)
- major SE is antimuscarinic...largely with amitriptyline |
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Drug reactions:
dilated cardiomyopathy |
the -RUBICIN's
Doxorubicin Daunorubicin |
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Drug reactions:
Coronary vasospasm |
cocaine
sumatriptan (migrane drug which vasoconstricts - 5HT2 agonist) |
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Drug reactions:
Cutaneous flushing |
VANC
Vancomycin Adenosine Niacin Ca channel blockers |
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Drug reactions:
Torsades de pointes |
Class III (sotalol) antiarrhtym.
Class IA (quinidine) antiarrhtym. |
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Drug reactions:
Gray baby syndrome |
Chloramphenicol
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Drug reactions:
Pseudomembranous colitis |
Clindamycin
ampicillin |
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Drug reactions:
Hepatitis |
Isoniazid (INH)
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Drug reactions:
Adrenocortical insufficiency |
Glucocorticoid withdrawl (HPA suppression)
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Drug reactions:
Hot falshes |
tamoxifen
clomiphene |
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Drug reactions:
Hypothyroidism |
Lithium
Amiadarone |
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Drug reactions:
Gingival hyperplasia*** |
Phenytoin
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Drug reactions:
Gout |
Furosemide
Thiazides |
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Drug reactions:
Osteoporosis |
corticosteroids
Heparin |
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Drug reactions:
tendonitis, tendon rupture, cartilage damage (kids) |
Fluoroquinolones
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Drug reactions:
Fanconi syndrome |
Expired tetracyclines
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Drug reactions:
Hemorrhagic cystitis ALSO...what is coadministered to prevent this? |
Cyclophosphamide
Ifosfamide (coadministered with MESNA!) |
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Drug reactions:
Cinchonisms |
Quinidine
Quinine |
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Drug reactions:
Diabetes Insipidus |
Lithium
Demeclocycline |
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Drug reactions:
Parkinson-like syndromes (those that block dopamine) |
Haloperidol
Chlorpromazine Reserpine metoclopramide |
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Drug reactions:
Seizures |
buproprion
Imipenem/cilastatin Isoniazid (INH) |
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Drug reactions:
Tardive dyskinesia |
Antipsychotics!!!
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Drug reactions:
Disulfiram-like reactions |
METRONIDAZOLE
Certain cephalosporins Procarbazine 1st-generation sulfonylureas |
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Drug reactions:
Nephrotoxicity/neurotoxicity |
Polymyxins
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Drug reactions:
Nephrotoxicity/ototoxicity |
Aminoglycosides
Vancomycin Loop diuretics Cisplatin |
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What drug is used to tx chronic alcoholism? Why? What is it's MOA?
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Disulfiram
- used to tx chronic alcoholism, since it causes nasty SE like nausea, vomiting, headache & hypotension with even a little bit of alcohol. -MOA: blocks acetaldehyde dehydrogenase, which prevents the normal breakdown of acetylaldehyde into acetic acid..and thus acetylaldehyde builds up & causes SE |
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Drug name ending..name category:
-afil (sildenafil) |
erectile dysfunction
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Drug name ending..name category:
-ane (halothane) |
inhalational general anesthetic
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Drug name ending..name category:
-azepam (diazepam) |
benzodiazepine
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Drug name ending..name category:
-azine (chlorpromazine) |
phenothiazine (neuroleptic, antiemetic)
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Drug name ending..name category:
-azole (ketoconazole) |
antifungal
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Drug name ending..name category:
-barbital (phenobarbital) |
barbituates
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Drug name ending..name category:
-caine (lidocaine) |
local anesthetic
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Drug name ending..name category:
-cillin (methicillin) |
penicillin
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Drug name ending..name category:
-cycline (tetracycline) |
antibiotic (protein synthesis inhibitor)
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Drug name ending..name category:
-etine (Fluoxetine) |
SSRI
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Drug name ending..name category:
-ipramine (imipramine) |
TCA
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Drug name ending..name category:
-navir (saquinavir) |
Protease inhibitor
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Drug name ending..name category:
-olol (propranolol) |
beta-blocker
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Drug name ending..name category:
-operidol (haloperidol) |
butyrophenone (neuroleptic)
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Drug name ending..name category:
-oxin (digoxin) |
cardiac glycoside (inotropic agent)
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Drug name ending..name category:
-phylline (theophylline) |
methylxanthine
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Drug name ending..name category:
-pril (captopril) |
ACEI
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Drug name ending..name category:
-terol (albuterol) |
Beta2 agonists
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Drug name ending..name category:
-tidine (cimetidine) |
H2 blockers
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Drug name ending..name category:
-triptan (Sumatriptan) |
5HT(1B/1D agonists) migrane
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Drug name ending..name category:
-triptyline (amitriptyline) |
TCA
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Drug name ending..name category:
-tropin (somatoptropin) |
pituitary hormone
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Drug name ending..name category:
-zolam (alprazolam) |
benzodiazepine
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Drug name ending..name category:
-osin (prazosin) |
alpha1 blockers
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