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242 Cards in this Set
- Front
- Back
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inverse or direct relationship of Km to enzyme affinity for substrate |
since Km is the concentration of substrate at 1/2 Vmax Inverse relationship |
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is Vmax inversely or directly related to enzyme concentration |
direct |
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what does a sigmoid enzyme kinetic curve indicate |
cooperative kinetics like hemoglobin |
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what does a hyperbolic enzyme kinetic curve indicate |
normal first order kinetics typical of most enzymes
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what is the x axis on a lineweaver burke plot |
1/substrate |
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what is the y axis on a lineweaver burke plot |
1/V |
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what is the y intercept on a lineweaver burke plot |
1/Vmax |
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what is the x intercept on a lineweaver burke plot |
-1/Km |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors.... which resembles substrate |
both competitive types |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors.... which are overcome by increased substrate |
ONLY reversible competitive |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors.... which binds the active site |
both competitive |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors.... which decrease Vmax |
Irreversible competitive Noncompetitive |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors.... which increase Km |
ONLY reversible competitive |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors which decrease efficacy |
Irreversible competitiveNoncompetitive |
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amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors which decrease potency |
reversible competitive |
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what are the only differences between competitive Irreversible inhibitor and noncompetitive |
irreversible competitive binds at active site and resembles substrate |
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what is the definition of bioavailbility and what is the symbol used for it in pharmocokinetics |
F= fraction of administered drug that reaches systemic circulation unchanged.....so in IV injection, F=1 |
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what is definition of Volume of Distribution in words |
theoretical volume occupied by total amount of drug in body relative to its plasma concentration |
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How can you calculate Vd |
plasma drug concentration= amount of drug in body/Vd |
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can drugs distribute to more than one or only one compartment? |
multiple |
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what compartment are drugs with low Vd mainly in |
blood |
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what kind of drugs have low Vd |
large/charged molecules protein bound drugs |
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what kind of drugs have medium Vd |
small size hyrdrophilic/charged |
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what compartment are drugs with medium Vd mainly in |
ECF |
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what compartment are drugs with high Vd mianly in |
all tissue including fat |
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what kind of drugs have high Vd |
small fatty drugs espcecially bound to tissue protein |
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what is definition of clearance in words |
volume of plasma cleared of drug per unit time |
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how does liver impact Vd |
decreased protein synthesis by liver means decreased protein-drug binding leading to increased Vd |
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what three organ system defects can impact clearance |
-heart -liver -kidney |
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what does 4-5 half lives represent for a drug |
time is takes for a drug infused at a constant rate to reach steady state/time takes for a drug to be eliminated |
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what is loading dose calculation |
Loading Dose= Target Plasma Concentration (Vd)/F |
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what is formula for calculation half life |
t1/2= .693 Vd/Clearance |
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what does time to steady state depend on |
t1/2 |
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what is time to steady state independent of |
dose/dosing frequency! |
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what is maintenance dose formula calculation |
Target plasma concentration at steady state x Clearance x Dosage interval/F |
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what drugs have zero order kinetics |
Phenytoin Ethanol Aspirin |
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how does concentration of drug in plasma change over time in zero order kinetics |
falls linearly/constant value |
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how does concentration of drug in plasma change over time in first order kinetics |
exponent decay |
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is netural or ionized drug form trapped in urine/cleared |
ionized |
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is neutral or ionized drug form reabsorbed/retained |
neutral |
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what are phase one drug metabolism products |
slighlty polar, water soluble metabolites that are often still active |
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what reactions occur in phase I drug metabolism and using what system |
-Reduction -Oxidation -Hydrolysis Cyt P450 |
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what phase of metabolism do old people lose first |
I |
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what class of reactions occur in phase II of drug metabolism |
conjugation |
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what product is obtained from phase II drug metabolism |
very polar, inactive metabolites |
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what are the types of conjugation reactions done in phase II |
Glucorinidation Acetylation Sulfation |
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is Vmax related to potency or efficacy or both |
efficacy |
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is Km related to potency or efficacy or both |
potency |
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do you want therapeutic index to be high or low for a safe drug |
high |
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what are drugs with low therapeutic index (4) |
-warfarin -theophylline -digoxin -lithium |
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what kind of synapse present (postsynaptic receptor type and neurotransmitter used) at all autonomic nervous system connection between the preganglionic and postganglionic fiber |
Nicotinic Ach |
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what is special about sweat gland control |
Under SNS control but still uses muscarinic ACh receptor |
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what G protein class is alpha 1 |
q |
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what G protein class is alpha 2 |
i |
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what G protein class is Beta 1 |
s
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what G protein class is beta 2 |
s |
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what G protein class is M1 |
q |
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what G protein class is M2 |
i |
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what G protein class is M3 |
q |
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what G protein class is D1 |
s |
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what G protein class is D2 |
i |
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what G protein class is H1 |
q |
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what G protein class is H2 |
s |
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what G protein class is V1 |
q |
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what G protein class is V2 |
s |
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what are major functions of alpha1 |
-vasoconstriction via vascular smooth muscle contraction leading to increased BP -pupil dilation via contraction of radial pupillary dilator muscles -decreased voiding of bladder/GI do to contraction of sphincters |
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what are major functions of alpha 2 |
-decreased SNS outflow -decrease insulin release -decrease lipolysis -decrease aqueous humor production -increase platelet aggregation |
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what are major functions of beta 1 |
-increase HR -increase contractility -increase renin release -increase lipolysis |
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what are major functions of beta 2 |
-vasodilation leading to decreased BP -bronchodilation -increased lipolysis -increased insulin release -increase aqueous humor production -relaxation of ciliary muscles -relaxation of uterine tone |
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what are major functions of M1 |
-CNS -enteric nervous system |
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what are major functions of M2 |
-decreased HR -decrease atria contractility |
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what are major functions of M3 |
-bronchoconstriction -pupil constriction via contracting circular sphincter muscle -increased bladder/GI voiding by constraction of bladder -increased peristalsis -ciliary muscle contraction for accomodation -increased exocrine gland secretions from tears, saliva, gastric acid |
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what are major functions of D1 |
relax renal vasculature (increased RBF) |
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what are major functions of D2 |
modulate neurotransmitter release in brain |
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what are major functions of H1 |
-increased nasal/bronchial mucus production -increased vascular permeability -increased bronchiole contriction -itching -pain |
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what are major functions of H2 |
-increased gastric acid secretion |
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what are major functions of V1 |
-increased vasoconstriction via vascular smooth muscle contraction |
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what are major functions of V2 |
- increase water permeability of collecting ducts in kidney leading to water reabsorption |
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what is signal cascade following Gq stimulation |
PLC leading to cleaving of PIP2 into DAG and IP3... DAG activates PKC IP3 increases intracellular calcium leading to smoth muscle contraction |
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what is signal cascade following Gs stimulation |
increases adenyl cyclase activity leading to ATP to cAMP conversion cAMP activates PKA PKA INHIBITS myosin light chain kinase leading to vasodilation of smooth muscle PKA increases intracellular calcium in heart |
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what are steps of acetycholine release in from cholingergic nerve terminal |
1) choline taken up into axon terminal 2)choline combines with acetyl CoA to from acetylcholine 3) ACh packaged into vesicles 4)Calcium entry leads to ACh release from vesicles into synapse 5)ACh broken down by AChE |
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what does hemicholinium do |
inhibits uptake of choline into axon (step 1) |
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what does vesamicol do |
inhibits packaging of ACh into vesicles |
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what does Botulinum toxin do |
cleaves SNARE proteins preventing ACh release from vesicles into synapse |
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what are steps in creation and release of NE from noradrenergic terminal |
1)tyrosine taken up into nerve terminal 2)tyrosine --> DOPA 3)DOPA --> DA 4) DA--> NE 5) NE released into synapse upon Calcium entry 6) transporter takes NE back up into terminal |
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what is metyrosine action |
prevent tyrosine to DOPA |
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what does reserpine do |
prevents storage of MAOs into vesicles |
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what does bretylium/guanethidine do |
prevent release of NE into synapse |
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what does amphetamine do |
blocks reuptake of NE into terminal leads to more release of NE into terminal |
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what does cocaine do |
blocks reuptake of NE into terminal |
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what does TCA do |
blocks reuptake of NE into terminal |
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what does angiotensin II do to noradrenergic terminal |
increases release of NE into terminal |
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what are direct cholinomimetics |
-Bethanechol -Carbachol -Methacholine -Pilocarpine |
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what is clinical use of bethanechol |
USED TO TREAT: -post op ileus -neurogenic ileus -urinary retention |
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what is carbachol clinical use |
USED FOR: -constricting pupils -relieving IOP in glaucoma |
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what is methacholine clinical use |
asthma challenge test to diagnose |
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what is pilocarpine clinical use |
-stimulate secretions like sweat/tears/saliva (might need for CF sweat test for example) -glaucoma |
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what are indirect cholinomimetics mechanism of action |
inhibit acetylcholinesterase |
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what are the indirect cholinomimetics |
-STIGMINES -Donepezil -Galantamine - Edrophonium |
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which indirect cholinomimetics does not have CNS penetration |
Neostigmine Pyridostigmine |
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what is the use of rivastigmine |
alzheimers |
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what is use of edrophonium |
-used to be used to diagnose myasthenia gravis since it is so short acting |
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what is use of neostigmine |
-post op ileus -neurogenenic ileus -urinary retention - post op reversal of NMJ blockade -myasthenia gravis |
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what is use of physostimgine |
fix anticholinergic/atropine overdose |
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what is use of pyridostigmine |
-myasthenia gravis (long acting) |
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what conditions should you be cautious about using cholinomimetics in |
-asthma -COPD -peptic ulcers |
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what is parathion |
organophosphate |
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what are organophosphate mechanims |
irreversibly inhibit acetylcholinesterase |
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what is seen in organophosphate poisoning |
-Diarreah -Urination -Miosis -Bronchoconstriction/spasm -Bradycardia -Excitation of skeletal muscle/CNS -Increased Secretions of Lacrimation, Sweating, Salivation basically parasympathetic on overdrive plus sweating because that uses acetycholine too |
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what is treatment for organophosphate poisoning |
-atropine to act as competitive inhibitor -pralidoxime to regenerate AChE if given early |
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what are muscarinic antagonist drugs |
-atropine -homatropine -tropicamide -benztropine -glycopyrrolate -hyoscyamine -dicyclomine -ipratropium -tiotropium -oxybutynin -solifenacin -tolterodine -scopolamine |
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what is use of atropine/homatropine/tropicamide |
dilate eyes |
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what is use of benztropine |
parkinsons |
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what is use of glycopyrrolate |
- IV: preop reduction of airway secretion -oral: reduce drooling, treat peptic ulcers |
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what is use of hyoscyamine/dicyclomine |
antispastic for IBS |
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what is use of ipratropium/tiotropium |
asthma/COPD |
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what is use of oxybutynin/solifenacin/tolterodine |
treat overactive bladder/reduce bladder spasticity/urinary incontinence |
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what is use of scopolamine |
motion sickness |
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what is tetrodotoxin effect |
binds sodium channels blocking action potentials |
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what is tetrodotoxin source |
badly prepared pufferfish/fugu |
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what is ciguatoxin effect |
opens sodium channels leading to depolarization |
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what can ciguatoxin poisoning confused with |
cholinergic poisoning |
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what is specific finding of ciguatoxin |
hot feels cold, cold feels hot |
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what is source of ciguatoxin |
reef fish like brracudas, snappers, moray eel |
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what causes scombroid poisoning |
dark meat fish consumption that are stored in warm temperatures leading to bacterial histidien decarboxylase convertion histidine to histamine |
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what is presentation of scombroid poisoning |
anaphylaxis, can look like fish allergy |
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what are the direct sympathomimetics |
-Epi -NE -DA -Dobutamine -Albuterol -Salmeterol -Isoproterenol -Phenlephrine |
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what is major effect of albuterol/salmeterol |
Beta 2 |
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what is major effects of dobutamine |
Beta2 Alpha |
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what is major effects of epi |
more beta than alpha Beta 2 Beta 1 Alpha |
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what are major effects of isoproterenol |
nonselective beta |
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what is main effects of NE |
alpha beta 1 |
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what is major phenylephrine effects |
alpha 1 |
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what are indirect sympathomimetics |
-ephedrine -amphetamine -cocaine |
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what drug don't you give in cocaine intoxication and why |
NEVER give beta blocker because it will lead to unopposed alpha activation and extreme hypertension |
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what is effect of NE on BP and reflex impact on HR |
increased BP (alpha mediated vasoconstriction) leading to reflex bradycardia |
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what is effect of isoproterenol on BP and reflex impact on HR |
decreased BP (beta 2 mediated vasodilation) leading to reflex tachycardia |
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what are the sympatholytics mechanism |
alpha 2 agonists (decreases sympathetic action because these are autoreceptors) |
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what are the sympatholytic drugs |
-clonidine -alpha methyldopa |
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what is use of clonidine |
-ADHD -Tourette's -hypertensive crises sometimes when you want to be sure to keep RBF intact |
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what is alpha methyldopa tox |
direct coombs test hemolysis SLE like syndrome |
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what are the nonselective alpha blockers |
phenoxybenzamine phentolamine |
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which nonselective alpha blocker is irreversible |
phenoxybenzamine |
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what is phenoxybenzamine use |
preop pheochromocytoma to prevent hypertensive crisis |
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what is phentolamine use |
MAOi patients who still want to eat tyramine foods |
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what are the alpha 1 selective blocking drugs |
"-osin" praz, teraz, doxaz, tamsul |
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what are the uses of alpha one selective blocks |
-BPH urinary symptoms -PTSD for prazosin -hypertention except tamsulosin |
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what are the alpha2 selective blockers |
mirtazapine |
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what is use of mirtazapine |
depression, increase appetite |
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what effect does epinephrine have on BP at high dose |
increased because net alpha vasoconstriction (alpha outweighs beta at high epi doses) |
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what effect does phenylephrine have on BP |
increased (alpha effect) |
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what effect does epi have on BP in presence of alpha blockade |
decreases because of unopposed beta 2 action |
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what effect does phenylephrine have on BP in presence of alpha blockage |
none....alpha blocked....but unlike epi also does NOT decrease the BP since does not have beta 2 like epi |
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what are the beta blockers |
olol |
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how do you know if a beta blocker is selective for beta 1 |
MOSTLY starting with letter A-M |
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how do you know if a beta blocker is nonselective (blocks 1 and 2) |
MOSTLY starting with letters N-Z (nebivolol excecption) |
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what are nonselective alpha and beta blockers |
labetalol carvedilol |
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what beta blockers are actually nonselective partial agonists at beta receptor |
acebutolol pindolol |
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what is special about nebivolol |
combines cardiac selective Beta 1 block with stimulation of Beta 3 leading to increased NO in vasculature |
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what are the applications of beta blockers |
-angina -MI -SVT -hypertension -CHF -Glaucoma |
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which beta blocker for glaucoma |
timolol |
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which beta blocker for SVT |
metoprolol esmolol |
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how does beta blocker help angina |
-decreased HR/contractility via B1 block leading to less myocardial oxygen demand |
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how does beta blocker help MI |
decreases mortality |
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how does beta blocker help SVT |
decreases AV node conduction velocity |
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how does beta blocker help hypertension |
-decreases CO -decreases renin secretion |
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how does beta blocker help CHF |
decreases mortality |
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how does beta blocker help glaucoma |
decreased acqueous humor production |
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what is tox of beta blockers |
-impotence -bradycardia -AV block -HF -CNS adverse effects like sedation/seizure -dyslipidemia in metoprolol -asthma/COPD exacerbation |
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what is guideline for beta blocker use in diabetics |
concern of masking hypoglycemia but not contraindicated because benefits outweigh risks |
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acetaminophen antidote
|
N acetyl cysteine |
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organophosphate antidote |
atropine pralidoxine |
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anticholinergic antidote |
phsostigmine |
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benzos antidote |
flumazenil |
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beta blocker antidote |
glucagon |
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carbon monoxide antidote |
100% oxygen, hyperbaric oxygen |
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copper antidote |
penicillamine |
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arsenic antidote |
penicillamine |
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gold antidote |
penicillamine |
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cyanide antidote |
nitrite +thiosulfate hydroxyocobalmin |
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digoxin antidote |
anti dig Fab fragments |
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heparine antidote |
protamine sulfate |
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iron antidote |
deferoxamine deferasirox |
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lead antidote |
EDTA, dimercaprol, succimer, penicillamine |
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mercury antidote |
dimercaprol |
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methanol, ethylene glycol antidote |
fomepizole better than ethanol |
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methemoglobin antidote |
methylene blue, vit C |
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opioid antidote |
naloxone, naltrexone |
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salicylate antidote |
NaHCO3 to alkalnize urine |
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TCAs antidote |
NAHCO3, alkalinize plasma |
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tPA, streptokinase, urokinase antidote |
aminocaproic acid |
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warfarin antidote |
Vit K delayed fresh frozen plasma immediate |
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what drugs induce cyt P450 |
-Rifampin -Griseofulvin -Carbamazepine -Chornic alcohol -St. John's wort -Phenytoin -Phenobarbitol -Nevirapine |
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what drugs inhibit cyt P450 |
-Isoniazid -Acute Alcohol Abuse -Ritonavir - Amiodarone -Cimetidine -Ketoconazole -Sulfonamides -Grapefruit juice -Quinidine -Macrolides asides from azithromycin |
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what are sulfa drugs |
-start with sulf -probenecid -furosemide -acetazolamide -Celecoxib -thiazides |
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what drugs have adverse reaction of vasospasm |
-cocaine -sumitriptan -ergotalkaloids |
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what drugs have adverse reaction of cutaneous flushing |
-vancomycin -adenosine -Niacin -Calcium channel blockers |
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what drugs have adverse reaction of dilated cardiomyopathy |
-anthracyclines (doxorubicin) |
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how do prevent dilated cardiomyopathy in doxorubicin? |
dexrazoxane |
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what drugs have adverse reaction of torsdades de pointes |
-Class II antiarrhythmics -Class IA antiarrhthmics -marcolides -antipsychotics -TCAs |
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what drugs have adverse reaction of adrenal cortex insufficiency |
-glucocorticoid withdrawal! |
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what drugs have adverse reaction of hot flashes |
tamoxifen clomiphene |
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what drugs have adverse reaction of hyperglycemia |
-tacrolimus -protease inhibitors -niacine -HCTZ -corticosteroids |
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what drugs have adverse reaction of hypothyroidism |
-lithium -amiodarone -sulfonamides |
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what drugs have adverse reaction of acute cholestatic heptatis, jaundice |
erythromycin |
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what drugs have adverse reaction of diarrhea |
-metformin -erythromycin -colchicine -orlistat -acarbose |
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what drugs have adverse reaction of focal to massive hepatic necrosis |
-halothane -alpha amanitan in mushrooms -valproic acid -acetaminophen |
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what drugs have adverse reaction of hepatitis |
-rifampin -isoniazid -pyrazinamide -statins -fibrates |
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what drugs have adverse reaction of pancreatitis |
-didanosine -corticosteroids -alochol -valproic acid -azathioprine -diuretics |
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pseudomembranous colitis |
-clindamycin -ampicillin -cephalosporins |
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what drugs have adverse reaction of agranulocytosis |
-clozapine -carbamazepine -ganciclovir -colchicine -methimazole -propylthiouracil |
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what drugs have adverse reaction of aplastic anemia |
-methimazole
-propylthiouracil -carbamazepine -NSAIDs -benzene -chloramphenicol |
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what drugs have adverse reaction of direct coombs positive hemolytic anemia |
-methyldopa -penicillin |
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what drugs have adverse reaction of gray baby syndrome |
chloramphenicol |
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what drugs have adverse reaction of hemolysis in G6PD deficiency |
-INH -Sulfonamides -Dapsone -Primaquine -Aspirin -Ibuprofen -Nitrofurantoin |
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what drugs have adverse reaction of megaloblastic anemia |
-Phenytoin -Methotrexate -Sulfa drugs |
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what drugs have adverse reaction of thrombocytopenia |
Heparin |
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what drugs have adverse reaction of thrombotic complications |
-OCP -hormone replacement therapy |
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what drugs have adverse reaction of fat redistribution |
-protease inhibitors -glucorticoids |
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what drugs have adverse reaction of gingival hyperplasia |
-phenytoin -calcium channel block -cyclosporine |
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what drugs have adverse reaction of gout |
-pryazinamide -thiazide -furosemide -niacin -cyclosporine |
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what drugs have adverse reaction of myopathy |
-fibrates -niacine -colchine -hydroxychloroquine -interferon alpha -penicillamine -statins -glucocorticoids |
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what drugs have adverse reaction of osteoporosis |
corticosteroids heparin |
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what drugs have adverse reaction of photosensitivity |
-tetracycline -sulfonamides -amiodarone -5-FU |
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what drugs have adverse reaction of Steven Johnson syndrome rash |
-Antiepileptics esp. lamotrigine -allopurinol -sulfa drugs -penicillin |
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SLE like syndrome what drugs have adverse reaction of |
-sulfa drugs -hydralazine -INH -Procainamide -Phenytoin -Etanercept |
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what drugs have adverse reaction of teeth discoloration |
tetracyclines |
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what drugs have adverse reaction of tendonitis, tendon rupture, cartilage damage |
fluoroquinolones |
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what drugs have adverse reaction of parkinson like syndrome |
antipsychotics reserpine metocloproamide |
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what drugs have adverse reaction of sezirues |
-INH -Bupropion -Imipenem/cilastatin -enflurane |
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what drugs have adverse reaction of tardive dyskinesia |
-antipsychotics -metoclopromaide |
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what drugs have adverse reaction of diabetes insipidus |
-lithium -demeclocycline |
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what drugs have adverse reaction of fanconi syndrome |
expired tetracycline |
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what drugs have adverse reaction of hemorrhagic cystitis |
cyclophosphamide ifosfamide |
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what drugs have adverse reaction of interstitial nephritis |
methicillin NSAIDs furosemide |
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how can you prevent hemorrahgic cystitis in cyclophosphamide/ifosfamide |
give mesna |
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what drugs have adverse reaction of SIADH |
cyclophosphamide SSRIs carbamazepine |
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what drugs have adverse reaction of dry cough |
ACE inhibitors |
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what drugs have adverse reaction of pulmonary fibrosis |
-bleomycin -amiodarone -busulfan -methotrexate |
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what drugs have adverse reaction of antimuscarinic |
-atropine -TCA -H1 blocker -antipsychotics |
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what drugs have adverse reaction of disulfiram like reaction |
-metronidazole -cephalosporins -griseofulvin -procarbazine -1st gen sulfonylureas |
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what drugs have adverse reaction of nephrotoxicity/ototoxicity |
-vancomycin -aminoglycoside -loop diuretics -cisplatin (treat with amifostine) |
