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85 Cards in this Set

  • Front
  • Back
What is Km?

What is Vmax?
Km - affinity of the enzyme for its substrate...as Km decreases...affinity increases

Vmax - enzyme concentration; maximum velocity that an enzyme can breakdown substrate...adding more substrate past this point will NOT speed up a reaction...since the enzymes are saturated
Competative Inhibition causes a change in Km or Vmax?

Noncompetative Inhibition causes a change in Km or Vmax?
KoMpetative Inhibition = Km Increases (no change in Vmax)

NOn-Kompetative inhibition = NO Km increase (but increase in Vmax
What does the mnemonic ENVY mean?
E - efficacy DECREASES
N - non-competative
V - Vmax DECREASES
Y - y-intercept (1/Vmax)
Volume of distribution (Vd) of plasma protein-bound drugs can be altered by ______ and ______ disease.
Kidney (proteinuria = decrease protein in body)
Liver (decrease protein synthesis)
Low Vd (4-8L) distrubutes in the ______

High Vd (>body weight) distrubutes into _______
blood

all tissues
How many half lives does it take to reach steady state?
Usually 5! (FA said 4-5....Goljan says 5)
What is the clearance (CL) rate equation?
(rate of drug elimination)/(plasma drug concentration)
In renal and/or liver disease...how are maintenance and loading doses adjusted?
Maintenance dose = decreased***

Loading dose = unchanged
A drug with a high Vd will require a high or low loading dose?

A drug with a high clearance rate will require a high or low maintenance dose?
HIGH

HIGH
1st order drug elimination = constant ________ of drug eliminated per unit time

Zero order drug elimination = constant ________ of drug eliminated per unit time
fraction

amount
Weak acids are get trapped in acidic or basic environments? Tx overdose of a weak acid with ________

Weak bases are get trapped in acidic or basic environments? Tx overdose of a weak base with ______
trapped in basic environments - tx overdose with bicarbonate (ionized = trapped in urine and cleared quickly)

Trapped in acidic environments - tx overdose with ammonium chloride (ionized = trapped in urine and cleared quickly)
Reduction, Oxidation, Hydrolysis .... phase I or II metabolism?

Acetylation, Glucuronidation, Sulfation .... phase I or II metabolism?
Phase I

Phase II
Geriatric patients lose phase I or phase II metabolism first?
Phase I first (reduction, oxidation, hydrolysis)
Most important component of Phase I metabolism is _________

Most important component of Phase II metabolism is _________
cytochrome P450

conjugation
What is the difference between efficacy and potency?
Efficacy - maximal effect a drug can produce

Potency - amount of drug needed for a given effect
A competitive antagonist decreases efficacy or potency?
potency
A noncompetitive antagonist decreases efficacy or potency?
efficacy
Give an example of a physiologic antagonism
Pt who has asthma d/t muscarinic overactivity (contracts smooth m), EPI can act as a bronchodilator by stimulating B2 receptors
Sweat glands are part of the SNS & are innervated by _______ fibers
cholinergic (ACh binding to Mreceptors)
What do these agents have in common?

Hemicholinium
Vesamicol
Botulinum
All act to decrease cholinergic activity:

Hemicholinium - blocks reuptake of choline at the presynaptic nerve
Vesamicol - blocks uptake of ACh into presynaptic vesicles
Botulinum - blocks release of ACh from presynaptic nerve
What drug is used for postoperative and neurogenic ileus and urinary retention?
Bethanechol ("activates Bower and Bladder smooth muscle"!)
What is pilocarpine used for?
potent stimulator of sweat, tears and saliva
What is methacholine used for?
Methacholine Challenge Test for dx of asthma!

-stimulates muscarinic receptors in airway when inhaled
What do the -stigmine drugs (ie. neostigmine) do?
Indirect cholinomimetic agonists....work by blocking acetylcholinesterases
Which drug is used for diagnosis of asthma?
Methacholine
Which drug is used for diagnosis of myasthenia gravis?

Which drug is used for treatment of myasthenia gravis?
Edrophonium (extremely short acting)

Pyridostigmine (long acting)

-both drugs block acetylcholinesterase!
With all cholinomimetic agents, what do you have to watch for?
exacerbation of:
COPD
asthma
peptic ulcers

(when giving to susceptible pt's)
Which two anticholinesterases are used for glaucoma?
Physostigmine (crosses BBB)
Echothiophate
What's the antidote for an anticholinesterase drug?
Atropine (M blocker) + pralidoxime (regenerates active AChE) -- remember 2PAM!?
Atropine, homatropine, tropicamide are a muscarinic blocker that works in what organ system?

Also..what is it's clinical use?
Organ system: eye

Clinical use: produce mydriasis (block PNS..so more SNS effect) and cycloplegia (loss of accomidation)
Benztropine is muscarinic blocker that works in what organ system?

Also..what is it's clinical use?
CNS

Parkinson's dz ("PARK my BENZ")
Scopolamine is muscarinic blocker that works in what organ system?

Also..what is it's clinical use?
CNS

motion sickness
Ipratroprium (bromide) is muscarinic blocker that works in what organ system?

Also..what is it's clinical use?
Respiratory

Asthma, COPD ("I pray I can breath soon!")
Oxybutynin & glycopyrrolate are muscarinic blockers that works in what organ system?

Also..what is it's clinical use?
Genitourinary system

reduce urgency in mild cystitis & reduce bladder spasms
Methscopolamine & propantheline are muscarinic blockers that works in what organ system?

Also..what is it's clinical use?
Genitourinary system

Peptic ulcer treatment
Drug reactions:

Atropine-like side effects (antimuscarinic)
Tricyclic Antidepressants (TCA)
- major SE is antimuscarinic...largely with amitriptyline
Drug reactions:

dilated cardiomyopathy
the -RUBICIN's

Doxorubicin
Daunorubicin
Drug reactions:

Coronary vasospasm
cocaine
sumatriptan (migrane drug which vasoconstricts - 5HT2 agonist)
Drug reactions:

Cutaneous flushing
VANC

Vancomycin
Adenosine
Niacin
Ca channel blockers
Drug reactions:

Torsades de pointes
Class III (sotalol) antiarrhtym.
Class IA (quinidine) antiarrhtym.
Drug reactions:

Gray baby syndrome
Chloramphenicol
Drug reactions:

Pseudomembranous colitis
Clindamycin
ampicillin
Drug reactions:

Hepatitis
Isoniazid (INH)
Drug reactions:

Adrenocortical insufficiency
Glucocorticoid withdrawl (HPA suppression)
Drug reactions:

Hot falshes
tamoxifen
clomiphene
Drug reactions:

Hypothyroidism
Lithium
Amiadarone
Drug reactions:

Gingival hyperplasia***
Phenytoin
Drug reactions:

Gout
Furosemide
Thiazides
Drug reactions:

Osteoporosis
corticosteroids
Heparin
Drug reactions:

tendonitis, tendon rupture, cartilage damage (kids)
Fluoroquinolones
Drug reactions:

Fanconi syndrome
Expired tetracyclines
Drug reactions:

Hemorrhagic cystitis

ALSO...what is coadministered to prevent this?
Cyclophosphamide
Ifosfamide

(coadministered with MESNA!)
Drug reactions:

Cinchonisms
Quinidine
Quinine
Drug reactions:

Diabetes Insipidus
Lithium
Demeclocycline
Drug reactions:

Parkinson-like syndromes (those that block dopamine)
Haloperidol
Chlorpromazine
Reserpine
metoclopramide
Drug reactions:

Seizures
buproprion
Imipenem/cilastatin
Isoniazid (INH)
Drug reactions:

Tardive dyskinesia
Antipsychotics!!!
Drug reactions:

Disulfiram-like reactions
METRONIDAZOLE
Certain cephalosporins
Procarbazine
1st-generation sulfonylureas
Drug reactions:

Nephrotoxicity/neurotoxicity
Polymyxins
Drug reactions:

Nephrotoxicity/ototoxicity
Aminoglycosides
Vancomycin
Loop diuretics
Cisplatin
What drug is used to tx chronic alcoholism? Why? What is it's MOA?
Disulfiram
- used to tx chronic alcoholism, since it causes nasty SE like nausea, vomiting, headache & hypotension with even a little bit of alcohol.
-MOA: blocks acetaldehyde dehydrogenase, which prevents the normal breakdown of acetylaldehyde into acetic acid..and thus acetylaldehyde builds up & causes SE
Drug name ending..name category:

-afil (sildenafil)
erectile dysfunction
Drug name ending..name category:

-ane (halothane)
inhalational general anesthetic
Drug name ending..name category:

-azepam (diazepam)
benzodiazepine
Drug name ending..name category:

-azine (chlorpromazine)
phenothiazine (neuroleptic, antiemetic)
Drug name ending..name category:

-azole (ketoconazole)
antifungal
Drug name ending..name category:

-barbital (phenobarbital)
barbituates
Drug name ending..name category:

-caine (lidocaine)
local anesthetic
Drug name ending..name category:

-cillin (methicillin)
penicillin
Drug name ending..name category:

-cycline (tetracycline)
antibiotic (protein synthesis inhibitor)
Drug name ending..name category:

-etine (Fluoxetine)
SSRI
Drug name ending..name category:

-ipramine (imipramine)
TCA
Drug name ending..name category:

-navir (saquinavir)
Protease inhibitor
Drug name ending..name category:

-olol (propranolol)
beta-blocker
Drug name ending..name category:

-operidol (haloperidol)
butyrophenone (neuroleptic)
Drug name ending..name category:

-oxin (digoxin)
cardiac glycoside (inotropic agent)
Drug name ending..name category:

-phylline (theophylline)
methylxanthine
Drug name ending..name category:

-pril (captopril)
ACEI
Drug name ending..name category:

-terol (albuterol)
Beta2 agonists
Drug name ending..name category:

-tidine (cimetidine)
H2 blockers
Drug name ending..name category:

-triptan (Sumatriptan)
5HT(1B/1D agonists) migrane
Drug name ending..name category:

-triptyline (amitriptyline)
TCA
Drug name ending..name category:

-tropin (somatoptropin)
pituitary hormone
Drug name ending..name category:

-zolam (alprazolam)
benzodiazepine
Drug name ending..name category:

-osin (prazosin)
alpha1 blockers