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122 Cards in this Set

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In a graph depicting Velocity (V) vs. [Substrate] ([S]), When is Km=[S]
at 1/2 Vmax
What is Km?
Reflects the affinity of the enzyme for its substrate
If you decrease the Km, what happens to the substrate affinity?
The substrate affinity will increase
Competitive Inhibitor or Noncompetitive Inhibitor: Resembles substrate
CI
Competitive Inhibitor or Noncompetitive Inhibitor: Overcome by increasing [S]
CI
Competitive Inhibitor or Noncompetitive Inhibitor: Bind active site
CI
Competitive Inhibitor vs Noncompetitive Inhibitor: Effect on Vmax
CI: Unchanged
NCI: decreases
Competitive Inhibitor vs Noncompetitive Inhibitor: Effect on Km
CI: Increases
NCI: Unchanged
Formula for volume of distribution (Vd=...)
Vd= Amount of drug in body/[plasma drug]
Clearance (CL)=....=.....
rate of elimination/[plasma concentration]
=
Vd x Ke(elimination constant)
t1/2=
0.7 x Vd/CL
What is the concentration (% eliminatedl) at 1, 2, 3, and 4 half lives?
50%, 75%, 87.5%, 93.75%
How do you calculate a loading dose?
Loading Dose = Cp x (Vd/F) where Cp=target plasma [drug], Vd=Volume of dist., and F=bioavailability
How do you calculate a maintenance dose?
=Cp x (Clearance/F), where Cp=target plasma [drug] and F=bioavailability
What and how would you change the dosing (maintenance vs. loading) in a pt with impaired renal or hepatic fxn?
Loading dose unchanged, maintenance dose decreases
What are three examples of drugs with zero order elimination
Phenytoin
Ethanol
Aspirin
What does the graph of Time vs. [plasma] look like in zero-order elimination? 1st order?
zero - Line with a negative slope
1st - Negative curve w/ asymptote as it approaches a concentration of zero
What is Efficacy? Potency?
Efficacy - Maximal effect a drug can produce
Potency - Amount of drug needed for a given effect
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
Shifts the curve to the right, decreasing potency and increasing EC50
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
Limits the percent of maximum effect, decreasing efficacy
How do you calculate the therapeutic index?
LD50/ED50 (Lethal dose for 50%/Effective dose for 50%)

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