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122 Cards in this Set
- Front
- Back
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In a graph depicting Velocity (V) vs. [Substrate] ([S]), When is Km=[S]
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at 1/2 Vmax
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What is Km?
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Reflects the affinity of the enzyme for its substrate
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If you decrease the Km, what happens to the substrate affinity?
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The substrate affinity will increase
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Competitive Inhibitor or Noncompetitive Inhibitor: Resembles substrate
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CI
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Competitive Inhibitor or Noncompetitive Inhibitor: Overcome by increasing [S]
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CI
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Competitive Inhibitor or Noncompetitive Inhibitor: Bind active site
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CI
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Competitive Inhibitor vs Noncompetitive Inhibitor: Effect on Vmax
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CI: Unchanged
NCI: decreases |
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Competitive Inhibitor vs Noncompetitive Inhibitor: Effect on Km
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CI: Increases
NCI: Unchanged |
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Formula for volume of distribution (Vd=...)
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Vd= Amount of drug in body/[plasma drug]
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Clearance (CL)=....=.....
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rate of elimination/[plasma concentration]
= Vd x Ke(elimination constant) |
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t1/2=
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0.7 x Vd/CL
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What is the concentration (% eliminatedl) at 1, 2, 3, and 4 half lives?
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50%, 75%, 87.5%, 93.75%
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How do you calculate a loading dose?
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Loading Dose = Cp x (Vd/F) where Cp=target plasma [drug], Vd=Volume of dist., and F=bioavailability
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How do you calculate a maintenance dose?
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=Cp x (Clearance/F), where Cp=target plasma [drug] and F=bioavailability
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What and how would you change the dosing (maintenance vs. loading) in a pt with impaired renal or hepatic fxn?
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Loading dose unchanged, maintenance dose decreases
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What are three examples of drugs with zero order elimination
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Phenytoin
Ethanol Aspirin |
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What does the graph of Time vs. [plasma] look like in zero-order elimination? 1st order?
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zero - Line with a negative slope
1st - Negative curve w/ asymptote as it approaches a concentration of zero |
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What is Efficacy? 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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In a plot of Agonist Dose vs. % of maximum effect, what effect does a competitive antagonist have on a sigmoidal curve generated by an agonist
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Shifts the curve to the right, decreasing potency and increasing EC50
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In a plot of Agonist Dose vs. % of maximum effect, what effect does a noncompetitive antagonist have on a sigmoidal curve generated by an agonist
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Limits the percent of maximum effect, decreasing efficacy
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How do you calculate the therapeutic index?
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LD50/ED50 (Lethal dose for 50%/Effective dose for 50%)
TILE= TI=Ld/Ed |
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The therapeutic index can be determined by LD50/ED50. What does this mean practically?
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Safer Drugs have a high TI value
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A drug has a very high TI value, What does that mean
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Very safe to use - low effective does and need lots of it to kill your patient
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A drug has a very low TI value. What does that mean?
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Very narrow range between benefiting your patient and killing him.
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What type of Muscarinic receptor does the eye have? response?
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M3 - miosis
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What type of Muscarinic receptor does the Heart have (SA and AV nodes)? Effect?
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SA - M2 - Decrease HR
AV - M2 - Decrease Conduction velocity |
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What type of Muscarinic receptor do the lungs have? Effect?
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M3 - constriction and glandular secretion
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What type of Muscarinic receptor does the stomach, GI glands, and intestines have? Effect?
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M3 (stomach and intestine) and M1 (Glands) - Increase motility, secretion
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What type of Muscarinic receptor does the bladder have? Effect?
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M3 - Contraction (detrusor), relaxation (trigone/sphincter), voiding
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What type of Muscarinic receptor do most glands have? Effect?
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M3 - sweat (SNS), salivate, lacrimate
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What type of Muscarinic receptor does the endothelium of blood vessels have? Effect?
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M3 - Dialation (via NO)
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What receptor mechanism does M1 have?
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Gq coupled - PLC -> IP3, DAG, Ca2+
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Which muscarinic receptor type is a Gq coupled?
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M1 and M3
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What receptor mechanism does M3 have?
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Gq - PLC ->IP3, DAG, Ca2+
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What receptor mechanism does M2 have? Where is it found?
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Gi - Decrease adenylyl cyclase -> Decrease cAMP. Heart
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What receptor mechanism do Nn and Nm have?
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No 2nd messanger - Activation (opening) of Na/K channels
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Bethanechol: Class and Use
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Direct Muscarinic Agonist
Ileus and Urinary Retention |
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Methacholine: Class and Use
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Direct Muscarinic Agonist
Dx of Bronchial hyperreactivity |
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Pilocarpine: Class and Use
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Direct Muscarinic Agonist
Glaucoma, xersotomia (dry mouth in Sjogren's syndrome) |
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Carbachol: Class and Use
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Direct Muscarinic Agonist
Glaucoma |
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Neostigmine: Class and Use
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Indirect Muscurinic Agonist (AChEi)
Postop Ileus |
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Pyridostigmine: Class and Use
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Indirect Muscurinic Agonist (AChEi)
Tx of Myasthenia gravis |
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Edrophonium: Class and Use
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Indirect Muscurinic Agonist (AChEi)
Dx of Myasthenia Gravis |
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Physostigmine: Class and Use
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Indirect Muscurinic Agonist (AChEi)
Glaucoma and Atropine OD |
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Echothiophate
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Indirect Muscurinic Agonist (AChEi)
Glaucoma |
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Symptoms of Cholinesterase poisoning.
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DUMBLESS
Diarrhea, Urinatiopn, Miosis, Bronchospasm, Excitation, lacrimination, sweating, and salivation |
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Atropine: Class and use
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Muscarinic antagonist
Produce Mydriasis and cycloplegia |
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Benztropine: Class and use
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Muscarinic antagonist
Parkinson's |
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Scopolamine: Class and use
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Muscarinic antagonist
Motion sickness |
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Ipratropium: Class and use
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Muscarinic antagonist
Asthma, COPD |
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Oxybutynin: Class and use
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Muscarinic antagonist
Reduce bladder urgency and spasms |
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Methscopolamine: Class and use
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Muscarinic antagonist
Peptic Ulcer treatment |
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Contraindications of atropine
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Elderly (with glaucoma - angle closure)
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Hexamethonium: class and use
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Nicotinic antagonist. Smoking cessation
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Epinephrine stimulates what receptors?
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a1, a2, B1, B2 (low dose selective for B1)
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NE stimulates what receptors?
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a1, a2>B1
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Epinephrine: Use
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Anaphylaxis
Glaucoma (open angle) Hypotention |
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NE: Use
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Hypotention
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a1: target organs and action
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Eyes - mydriasis
Arterioles - Incr. TPR - Incr Diastole, incr. afterload Veins - Contration - incr. VR Liver - Incr. Glycogenolysis |
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a2 target organs and action
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Decreases central sympathetic output. Negative feedack for NE release
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B1 target organs and action
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SA node - (+) chronotroph (incr. HR)
AV node - (+) dromotropy (incr. velocity) Heart muscle - (+) inotropy (incr. contract) Kidney - Renin release |
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B2 target organs and action
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Blood vessels (all) - Vasodilation
Liver - Glycogenolysis |
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D1 (peripheral) - Target organs and action
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Vasodilation - Kidney - Incr. RBF, Incr GFR, Incr Na secretion
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Causal Agent(s): Atropine-like SEs
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Tricyclics
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Causal Agent(s): Coronary Vasospasm
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Cocaine, sumatriptan
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Causal Agent(s): Cutaneous flushing
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Niacin, CCBs, Adenosine, vancomycin
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Causal Agent(s): Dilated cardiomyopathy
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Doxorubicin (adriamycin), daunorubicin
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Causal Agent(s): Torsades de pointes
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Class III (sotalol), Class IA, cisapride
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Causal Agent(s): Agranulocytosis
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clozapine
Carbamazepine Colchicine propylthiouracil Methimazole |
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Causal Agent(s): Aplastic Anemia
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Chloramphenicol
Benzene NSAIDS propylthiouracil Methimazole |
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Causal Agent(s): Direct Coombs positive HA
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Methyldopa
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Causal Agent(s): Gray baby syndrome
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Chloramphenicol
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Causal Agent(s): Hemolysis in G6PD-deficient patients
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INH, Sulfonamides, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin (hemolysis IS PAIN)
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Causal agent(s): Megaloblastic anemia
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Phenytoin, Methotrexate, Sulfa drugs (having a blast with PMS)
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Causal agent(s): Cough
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ACE inhibitors
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Causal agent(s): Pulmonary fibrosis
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Bleomycin, busulfan, amiodarone
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Causal agent(s): Acute cholestatic hepatitis
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Macrolides
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Causal agent(s): Focal to massive hepatic necrosis
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Halothane, valproic acid, acetaminophen, Amanita phalloides
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Causal agent(s): Hepititis
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INH
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Causal agent(s): Pseudomembranous colitis
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Clindamycin, ampicillin
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Causal agent(s): Adrenocortical insufficiency
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Glucocorticoid withdrawl
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Causal agent(s): Gynecomastia
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Spironolactone, Digitalis, Cimetidine, Alcohol, estrogens, Ketoconazole (Some Drugs Create Awesome Knockers)
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Causal agent(s): Hot flashes
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Tamoxifen, Clomiphene
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Causal agent(s): Gingival Hyperplasia
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Phenytoin
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Causal agent(s): Gout
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Furosemide, thiazides
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Causal agent(s): Osteoporosis
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Corticosteroids, heparin
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Causal agent(s): Photosensitivity
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Sulfonamides, Amiodarone, Tetracycline (SAT for a photo)
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Causal agent(s): Rash (Stevens- Johnson syndrome)
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Ethosuximide
Lamotrigine Carbamazepine Phenobarbital phenytoin sulfa drugs penicillin allopurinol |
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Causal agent(s): SLE-like syndrome
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Hydralazine, INH, Procainamide, Phenytoin (it's not HIPP to have lupus)
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Antidote for: Acetaminophen
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N-acetylcysteine
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Antidote for: Salicylates
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NaHCO3 (alkalinize urine)
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Antidote for: Amphetamines
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NH4Cl (acidify urine)
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Antidote for: Anticholinesterases, organophosphates
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Atropine, pralidoxime
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Antidote for: Antimuscarinic, anticholinergics
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Physostigmine salicylate
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Antidote for: B Blockers
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Glucagon
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Antidote for: Iron
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Deferoxamine
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Antidote for: Lead
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CaEDTA, dimercaprol, succimer, penicillamine
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Antidote for: Mercury, arsenic gold
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Dimercaprol (BAL), succimer
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Antidote for: Copper, arsenic, gold
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Penicillamine
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Antidote for: Cyanide
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Nitrite, hydroxocobalamin, thiosulfate
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Antidote for: Methemoglobin
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Methylene blue
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Antidote for: Methanol, ethylene glycol
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Ethanol, dialysis, fomepizole
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Antidote for: Opiods
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Naloxone/naltrexone
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Antidote for: Benzodiazepines
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Flumazenil
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Antidote for: TCAs
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NaHCO3 (serum alkalinization)
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Antidote for: Heparin
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Protamine
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Antidote for: Warfarin
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Vitamin K, Fresh Frozen Plasma
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Antidote for: tPA, streptokinase
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Aminocaproic Acid
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Antidote for: Theophylline
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B-blocker
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Causal agent(s): Fanconi's syndrome
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Expired Tetracycline
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Causal agent(s): Interstitial Nephritis
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Methicillin, NSAIDS, furosemide
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Causal agent(s): Hemorrhagic cystitis
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Cyclophosphamide, isosfamide
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Causal agent(s): Cinchonism
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Quinidine and quinine
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Causal agent(s): Diabetes insipidus
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Lithium, demeclocycline
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Causal agent(s): Parkinson-like symptoms
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Haloperidol, chlorpromazine, reserpine, metoclopramide
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Causal agent(s): Seizures
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Bupropion, imipenem/cilastatin, INH
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Causal agent(s): Tardive dyskinesia
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Antipsychotics
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Causal agent(s): Disulfram-like rxn
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Metronidazole, cephalosporins, procarbazine, 1st gen sulfonylureas
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Causal agent(s): Nephrotoxicity/Neurotoxicity
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Polymyxins
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Causal agent(s): Nephrotoxicity/ototoxicity
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Aminoglycosides
Vancomycin Loop diuretics Cisplatin |
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c-ANCA
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Wegener's
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p-ANCA
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Microscopic polyangitis, churg-strauss
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