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242 Cards in this Set

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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

is Vmax inversely or directly related to enzyme concentration

direct

what does a sigmoid enzyme kinetic curve indicate

cooperative kinetics like hemoglobin

what does a hyperbolic enzyme kinetic curve indicate

normal first order kinetics typical of most enzymes

what is the x axis on a lineweaver burke plot

1/substrate

what is the y axis on a lineweaver burke plot

1/V

what is the y intercept on a lineweaver burke plot

1/Vmax

what is the x intercept on a lineweaver burke plot

-1/Km

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors....




which resembles substrate

both competitive types

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors....




which are overcome by increased substrate

ONLY reversible competitive

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors....




which binds the active site

both competitive

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors....




which decrease Vmax

Irreversible competitive




Noncompetitive

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors....




which increase Km

ONLY reversible competitive

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors




which decrease efficacy

Irreversible competitiveNoncompetitive

amongst reversible competitive inhibitors, irreversible competitive inhibitors, and noncompetitive inhibitors




which decrease potency

reversible competitive

what are the only differences between competitive Irreversible inhibitor and noncompetitive

irreversible competitive binds at active site and resembles substrate

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

what is definition of Volume of Distribution in words

theoretical volume occupied by total amount of drug in body relative to its plasma concentration

How can you calculate Vd

plasma drug concentration= amount of drug in body/Vd

can drugs distribute to more than one or only one compartment?

multiple

what compartment are drugs with low Vd mainly in

blood

what kind of drugs have low Vd

large/charged molecules




protein bound drugs

what kind of drugs have medium Vd

small size




hyrdrophilic/charged

what compartment are drugs with medium Vd mainly in

ECF

what compartment are drugs with high Vd mianly in

all tissue including fat

what kind of drugs have high Vd

small fatty drugs espcecially bound to tissue protein

what is definition of clearance in words

volume of plasma cleared of drug per unit time

how does liver impact Vd

decreased protein synthesis by liver means decreased protein-drug binding leading to increased Vd

what three organ system defects can impact clearance

-heart


-liver


-kidney

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

what is loading dose calculation

Loading Dose= Target Plasma Concentration (Vd)/F

what is formula for calculation half life

t1/2= .693 Vd/Clearance

what does time to steady state depend on

t1/2

what is time to steady state independent of

dose/dosing frequency!

what is maintenance dose formula calculation

Target plasma concentration at steady state x Clearance x Dosage interval/F

what drugs have zero order kinetics

Phenytoin




Ethanol




Aspirin

how does concentration of drug in plasma change over time in zero order kinetics

falls linearly/constant value

how does concentration of drug in plasma change over time in first order kinetics

exponent decay

is netural or ionized drug form trapped in urine/cleared

ionized

is neutral or ionized drug form reabsorbed/retained

neutral

what are phase one drug metabolism products

slighlty polar, water soluble metabolites that are often still active

what reactions occur in phase I drug metabolism and using what system

-Reduction


-Oxidation


-Hydrolysis




Cyt P450

what phase of metabolism do old people lose first

I

what class of reactions occur in phase II of drug metabolism

conjugation

what product is obtained from phase II drug metabolism

very polar, inactive metabolites

what are the types of conjugation reactions done in phase II

Glucorinidation




Acetylation




Sulfation

is Vmax related to potency or efficacy or both

efficacy

is Km related to potency or efficacy or both

potency

do you want therapeutic index to be high or low for a safe drug

high

what are drugs with low therapeutic index (4)

-warfarin


-theophylline


-digoxin


-lithium

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

what is special about sweat gland control

Under SNS control but still uses muscarinic ACh receptor

what G protein class is alpha 1

q

what G protein class is alpha 2

i

what G protein class is Beta 1

s


what G protein class is beta 2

s

what G protein class is M1

q

what G protein class is M2

i

what G protein class is M3

q

what G protein class is D1

s

what G protein class is D2

i

what G protein class is H1

q

what G protein class is H2

s

what G protein class is V1

q

what G protein class is V2

s

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

what are major functions of alpha 2

-decreased SNS outflow


-decrease insulin release


-decrease lipolysis


-decrease aqueous humor production


-increase platelet aggregation

what are major functions of beta 1

-increase HR


-increase contractility


-increase renin release


-increase lipolysis

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

what are major functions of M1

-CNS


-enteric nervous system

what are major functions of M2

-decreased HR


-decrease atria contractility

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

what are major functions of D1

relax renal vasculature (increased RBF)

what are major functions of D2

modulate neurotransmitter release in brain

what are major functions of H1

-increased nasal/bronchial mucus production


-increased vascular permeability


-increased bronchiole contriction


-itching


-pain

what are major functions of H2

-increased gastric acid secretion

what are major functions of V1

-increased vasoconstriction via vascular smooth muscle contraction

what are major functions of V2

- increase water permeability of collecting ducts in kidney leading to water reabsorption

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

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

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

what does hemicholinium do

inhibits uptake of choline into axon (step 1)

what does vesamicol do

inhibits packaging of ACh into vesicles

what does Botulinum toxin do

cleaves SNARE proteins preventing ACh release from vesicles into synapse

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

what is metyrosine action

prevent tyrosine to DOPA

what does reserpine do

prevents storage of MAOs into vesicles

what does bretylium/guanethidine do

prevent release of NE into synapse

what does amphetamine do

blocks reuptake of NE into terminal




leads to more release of NE into terminal

what does cocaine do

blocks reuptake of NE into terminal

what does TCA do

blocks reuptake of NE into terminal

what does angiotensin II do to noradrenergic terminal

increases release of NE into terminal

what are direct cholinomimetics

-Bethanechol


-Carbachol


-Methacholine


-Pilocarpine

what is clinical use of bethanechol

USED TO TREAT:


-post op ileus


-neurogenic ileus


-urinary retention

what is carbachol clinical use

USED FOR:


-constricting pupils


-relieving IOP in glaucoma

what is methacholine clinical use

asthma challenge test to diagnose

what is pilocarpine clinical use

-stimulate secretions like sweat/tears/saliva (might need for CF sweat test for example)


-glaucoma

what are indirect cholinomimetics mechanism of action

inhibit acetylcholinesterase

what are the indirect cholinomimetics

-STIGMINES


-Donepezil


-Galantamine


- Edrophonium

which indirect cholinomimetics does not have CNS penetration

Neostigmine




Pyridostigmine

what is the use of rivastigmine

alzheimers

what is use of edrophonium

-used to be used to diagnose myasthenia gravis since it is so short acting

what is use of neostigmine

-post op ileus


-neurogenenic ileus


-urinary retention


- post op reversal of NMJ blockade


-myasthenia gravis

what is use of physostimgine

fix anticholinergic/atropine overdose

what is use of pyridostigmine

-myasthenia gravis (long acting)



what conditions should you be cautious about using cholinomimetics in

-asthma


-COPD


-peptic ulcers

what is parathion

organophosphate

what are organophosphate mechanims

irreversibly inhibit acetylcholinesterase

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

what is treatment for organophosphate poisoning

-atropine to act as competitive inhibitor


-pralidoxime to regenerate AChE if given early

what are muscarinic antagonist drugs

-atropine


-homatropine


-tropicamide


-benztropine


-glycopyrrolate


-hyoscyamine


-dicyclomine


-ipratropium


-tiotropium


-oxybutynin


-solifenacin


-tolterodine


-scopolamine

what is use of atropine/homatropine/tropicamide

dilate eyes

what is use of benztropine

parkinsons

what is use of glycopyrrolate

- IV: preop reduction of airway secretion


-oral: reduce drooling, treat peptic ulcers

what is use of hyoscyamine/dicyclomine

antispastic for IBS

what is use of ipratropium/tiotropium

asthma/COPD

what is use of oxybutynin/solifenacin/tolterodine

treat overactive bladder/reduce bladder spasticity/urinary incontinence

what is use of scopolamine

motion sickness

what is tetrodotoxin effect

binds sodium channels blocking action potentials

what is tetrodotoxin source

badly prepared pufferfish/fugu

what is ciguatoxin effect

opens sodium channels leading to depolarization

what can ciguatoxin poisoning confused with

cholinergic poisoning

what is specific finding of ciguatoxin

hot feels cold, cold feels hot

what is source of ciguatoxin

reef fish like brracudas, snappers, moray eel

what causes scombroid poisoning

dark meat fish consumption that are stored in warm temperatures leading to bacterial histidien decarboxylase convertion histidine to histamine

what is presentation of scombroid poisoning

anaphylaxis, can look like fish allergy

what are the direct sympathomimetics

-Epi


-NE


-DA


-Dobutamine


-Albuterol


-Salmeterol


-Isoproterenol


-Phenlephrine

what is major effect of albuterol/salmeterol

Beta 2

what is major effects of dobutamine

Beta2




Alpha

what is major effects of epi

more beta than alpha




Beta 2


Beta 1


Alpha

what are major effects of isoproterenol

nonselective beta

what is main effects of NE

alpha


beta 1

what is major phenylephrine effects

alpha 1

what are indirect sympathomimetics

-ephedrine


-amphetamine


-cocaine

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

what is effect of NE on BP and reflex impact on HR

increased BP (alpha mediated vasoconstriction) leading to reflex bradycardia

what is effect of isoproterenol on BP and reflex impact on HR

decreased BP (beta 2 mediated vasodilation) leading to reflex tachycardia

what are the sympatholytics mechanism

alpha 2 agonists (decreases sympathetic action because these are autoreceptors)

what are the sympatholytic drugs

-clonidine


-alpha methyldopa

what is use of clonidine

-ADHD


-Tourette's


-hypertensive crises sometimes when you want to be sure to keep RBF intact

what is alpha methyldopa tox

direct coombs test hemolysis




SLE like syndrome

what are the nonselective alpha blockers

phenoxybenzamine




phentolamine

which nonselective alpha blocker is irreversible

phenoxybenzamine

what is phenoxybenzamine use

preop pheochromocytoma to prevent hypertensive crisis

what is phentolamine use

MAOi patients who still want to eat tyramine foods

what are the alpha 1 selective blocking drugs

"-osin"




praz, teraz, doxaz, tamsul

what are the uses of alpha one selective blocks

-BPH urinary symptoms


-PTSD for prazosin


-hypertention except tamsulosin

what are the alpha2 selective blockers

mirtazapine

what is use of mirtazapine

depression, increase appetite

what effect does epinephrine have on BP at high dose

increased because net alpha vasoconstriction (alpha outweighs beta at high epi doses)

what effect does phenylephrine have on BP

increased (alpha effect)

what effect does epi have on BP in presence of alpha blockade

decreases because of unopposed beta 2 action

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

what are the beta blockers

olol

how do you know if a beta blocker is selective for beta 1

MOSTLY starting with letter A-M

how do you know if a beta blocker is nonselective (blocks 1 and 2)

MOSTLY starting with letters N-Z (nebivolol excecption)

what are nonselective alpha and beta blockers

labetalol


carvedilol

what beta blockers are actually nonselective partial agonists at beta receptor

acebutolol




pindolol

what is special about nebivolol

combines cardiac selective Beta 1 block with stimulation of Beta 3 leading to increased NO in vasculature

what are the applications of beta blockers

-angina


-MI


-SVT


-hypertension


-CHF


-Glaucoma

which beta blocker for glaucoma

timolol

which beta blocker for SVT

metoprolol


esmolol

how does beta blocker help angina

-decreased HR/contractility via B1 block leading to less myocardial oxygen demand

how does beta blocker help MI

decreases mortality

how does beta blocker help SVT

decreases AV node conduction velocity

how does beta blocker help hypertension

-decreases CO


-decreases renin secretion

how does beta blocker help CHF

decreases mortality

how does beta blocker help glaucoma

decreased acqueous humor production

what is tox of beta blockers

-impotence


-bradycardia


-AV block


-HF


-CNS adverse effects like sedation/seizure


-dyslipidemia in metoprolol


-asthma/COPD exacerbation

what is guideline for beta blocker use in diabetics

concern of masking hypoglycemia but not contraindicated because benefits outweigh risks

acetaminophen antidote

N acetyl cysteine

organophosphate antidote

atropine


pralidoxine

anticholinergic antidote

phsostigmine

benzos antidote

flumazenil

beta blocker antidote

glucagon

carbon monoxide antidote

100% oxygen, hyperbaric oxygen

copper antidote

penicillamine

arsenic antidote

penicillamine

gold antidote

penicillamine

cyanide antidote

nitrite +thiosulfate




hydroxyocobalmin

digoxin antidote

anti dig Fab fragments

heparine antidote

protamine sulfate

iron antidote

deferoxamine




deferasirox

lead antidote

EDTA, dimercaprol, succimer, penicillamine

mercury antidote

dimercaprol

methanol, ethylene glycol antidote

fomepizole better than ethanol

methemoglobin antidote

methylene blue, vit C

opioid antidote

naloxone, naltrexone

salicylate antidote

NaHCO3 to alkalnize urine

TCAs antidote

NAHCO3, alkalinize plasma

tPA, streptokinase, urokinase antidote

aminocaproic acid

warfarin antidote

Vit K delayed


fresh frozen plasma immediate

what drugs induce cyt P450

-Rifampin


-Griseofulvin


-Carbamazepine


-Chornic alcohol


-St. John's wort


-Phenytoin


-Phenobarbitol


-Nevirapine



what drugs inhibit cyt P450

-Isoniazid


-Acute Alcohol Abuse


-Ritonavir


- Amiodarone


-Cimetidine


-Ketoconazole


-Sulfonamides


-Grapefruit juice


-Quinidine


-Macrolides asides from azithromycin

what are sulfa drugs

-start with sulf


-probenecid


-furosemide


-acetazolamide


-Celecoxib


-thiazides

what drugs have adverse reaction of vasospasm

-cocaine


-sumitriptan


-ergotalkaloids

what drugs have adverse reaction of cutaneous flushing

-vancomycin


-adenosine


-Niacin


-Calcium channel blockers

what drugs have adverse reaction of dilated cardiomyopathy

-anthracyclines (doxorubicin)



how do prevent dilated cardiomyopathy in doxorubicin?

dexrazoxane

what drugs have adverse reaction of torsdades de pointes

-Class II antiarrhythmics


-Class IA antiarrhthmics


-marcolides


-antipsychotics


-TCAs

what drugs have adverse reaction of adrenal cortex insufficiency

-glucocorticoid withdrawal!

what drugs have adverse reaction of hot flashes

tamoxifen


clomiphene

what drugs have adverse reaction of hyperglycemia

-tacrolimus


-protease inhibitors


-niacine


-HCTZ


-corticosteroids

what drugs have adverse reaction of hypothyroidism

-lithium


-amiodarone


-sulfonamides

what drugs have adverse reaction of acute cholestatic heptatis, jaundice

erythromycin

what drugs have adverse reaction of diarrhea

-metformin


-erythromycin


-colchicine


-orlistat


-acarbose

what drugs have adverse reaction of focal to massive hepatic necrosis

-halothane


-alpha amanitan in mushrooms


-valproic acid


-acetaminophen

what drugs have adverse reaction of hepatitis

-rifampin


-isoniazid


-pyrazinamide


-statins


-fibrates

what drugs have adverse reaction of pancreatitis

-didanosine


-corticosteroids


-alochol


-valproic acid


-azathioprine


-diuretics

pseudomembranous colitis

-clindamycin


-ampicillin


-cephalosporins

what drugs have adverse reaction of agranulocytosis

-clozapine


-carbamazepine


-ganciclovir


-colchicine


-methimazole


-propylthiouracil

what drugs have adverse reaction of aplastic anemia

-methimazole

-propylthiouracil


-carbamazepine


-NSAIDs


-benzene


-chloramphenicol

what drugs have adverse reaction of direct coombs positive hemolytic anemia

-methyldopa


-penicillin

what drugs have adverse reaction of gray baby syndrome

chloramphenicol

what drugs have adverse reaction of hemolysis in G6PD deficiency

-INH


-Sulfonamides


-Dapsone


-Primaquine


-Aspirin


-Ibuprofen


-Nitrofurantoin

what drugs have adverse reaction of megaloblastic anemia

-Phenytoin


-Methotrexate


-Sulfa drugs

what drugs have adverse reaction of thrombocytopenia

Heparin

what drugs have adverse reaction of thrombotic complications

-OCP


-hormone replacement therapy

what drugs have adverse reaction of fat redistribution

-protease inhibitors


-glucorticoids

what drugs have adverse reaction of gingival hyperplasia

-phenytoin


-calcium channel block


-cyclosporine

what drugs have adverse reaction of gout

-pryazinamide


-thiazide


-furosemide


-niacin


-cyclosporine

what drugs have adverse reaction of myopathy

-fibrates


-niacine


-colchine


-hydroxychloroquine


-interferon alpha


-penicillamine


-statins


-glucocorticoids

what drugs have adverse reaction of osteoporosis

corticosteroids


heparin

what drugs have adverse reaction of photosensitivity

-tetracycline


-sulfonamides


-amiodarone


-5-FU



what drugs have adverse reaction of Steven Johnson syndrome rash

-Antiepileptics esp. lamotrigine


-allopurinol


-sulfa drugs


-penicillin

SLE like syndrome what drugs have adverse reaction of

-sulfa drugs


-hydralazine


-INH


-Procainamide


-Phenytoin


-Etanercept

what drugs have adverse reaction of teeth discoloration

tetracyclines

what drugs have adverse reaction of tendonitis, tendon rupture, cartilage damage

fluoroquinolones

what drugs have adverse reaction of parkinson like syndrome

antipsychotics


reserpine


metocloproamide

what drugs have adverse reaction of sezirues

-INH


-Bupropion


-Imipenem/cilastatin


-enflurane

what drugs have adverse reaction of tardive dyskinesia

-antipsychotics


-metoclopromaide

what drugs have adverse reaction of diabetes insipidus

-lithium


-demeclocycline

what drugs have adverse reaction of fanconi syndrome

expired tetracycline

what drugs have adverse reaction of hemorrhagic cystitis

cyclophosphamide




ifosfamide

what drugs have adverse reaction of interstitial nephritis

methicillin


NSAIDs


furosemide

how can you prevent hemorrahgic cystitis in cyclophosphamide/ifosfamide

give mesna

what drugs have adverse reaction of SIADH

cyclophosphamide


SSRIs


carbamazepine

what drugs have adverse reaction of dry cough

ACE inhibitors

what drugs have adverse reaction of pulmonary fibrosis

-bleomycin


-amiodarone


-busulfan


-methotrexate

what drugs have adverse reaction of antimuscarinic

-atropine


-TCA


-H1 blocker


-antipsychotics

what drugs have adverse reaction of disulfiram like reaction

-metronidazole


-cephalosporins


-griseofulvin


-procarbazine


-1st gen sulfonylureas

what drugs have adverse reaction of nephrotoxicity/ototoxicity

-vancomycin


-aminoglycoside


-loop diuretics


-cisplatin (treat with amifostine)