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117 Cards in this Set
- Front
- Back
amount of drug in body/_______ = Vd
|
plasma drug concentration
(Vd is Volume of Distribution) |
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rate of elimination of drug/[plasma drug] = ?
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CL (Clearance)
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(.7)(Vd)/CL = ?
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T 1/2
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A drug infused at a constant rate reaches about 94% of steady state after _______ t 1/2s.
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4
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A loading dose is calculated using this formula.
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Loading Dose = (Cp)(Vd)/F
(Cp = target plasma conc; F = bioavailability) |
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A maintenance dose is calculated using this formula.
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(Cp)(CL)/F
(CL = Clearance) |
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Rate of elimination is proportional to _______ ______ in 1st order elimination.
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drug concentration
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In the case of EtOH, which is elimated by _____ order elimination, a constant amount of drug is eliminated per unit time.
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zero
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Phase ____ (I or II) reactions yield slightly polar metabolites that are often _____ (active or inactive)
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I, active
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Phase ____ (I or II) reactions yield very polar metabolites that are often _____ (active or inactive) and are excreted by the _______.
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II, inactive, kidney
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Phase II reactions are often of this type.
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conjugation
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Cytochrome P-450 is involved in _____ phase (I or II) reactions.
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I
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A drug patent lasts for _____ years after filing for application.
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20
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How many phases are there in drug development?
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4
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Drugs are first tested in patients in phase _____ of clinical testing, pharmacokinetic safety is determined in phase ______ of clinical testing, double blind tests are done in phase ____ and post-market surveillance is done in phase _____.
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2,1,3,4
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In a dose response curve, a competitive antagonist shifts the curve _____
a non-competitive antagonist shifts the curve ______. |
right
down |
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What pharmacologic relationship would determine the existence of spare receptors?
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EC50 is lower then Kd (EC50 is more to the left)
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What does it mean if EC50 and Kd are equal?
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The system does not have spare receptors
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A partial agonist acts on the same receptor system as a full agonist? T/F
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TRUE
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What's the main difference between a partial agonist and a full agonist?
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A partial agonist has a lower maximal efficacy.
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Is a partial agonist less potent than a full agonist?
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Not necessarily. It can be less, more or equally potent as a full agonist.
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Equation for Half Life
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T 1/2 = (0.7 x Vd)/CL
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Percent of concentration in the following number of half lives:
1 2 3 3.3 |
1 = 50%
2 = 75% 3 = 87.5% 3.3 = 90% |
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How do the Loading and Maintenance doses change in a patient w/ Renal or Hepatic dysfunction?
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Loading - unchanged
Maintenance - Decreased |
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Equation for Theraputic Index
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TI = Toxic dose/Effective dose
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Phase in clinical drug testing:
safety, pharmacokinetics |
1
|
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Phase in clinical drug testing:
Protocol, dose level, work on patients |
2
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Phase in clinical drug testing:
double blind study, efficacy, adverse effects |
3
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(3) drugs that use Zero-order elimination
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Alcohol,
Aspirin, Phenytoin |
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What phase of a reaction uses cytP-450?
What is the purpose of this phase? |
Phase I
converts lipophilic to polar |
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What is the main focus of Phase II reactions?
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Conjugation
|
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When pH < pKa, what is more common?
(2) which can pass through the membrane? |
HA and BH+
HA passes thru the membrane (uncharged) |
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Definition:
Amount of the drug required for a given response |
Potency
|
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what is the first NT to everything?
the first receptor? |
NT: ACh
Receptor: Nicotinic |
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what system does not have a synapse from the spinal cord to the tissue?
|
Somatic NS
(skeletal muscle) ACh to Nicotinic receptor |
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what is the only sympathetic ACh?
what is the receptor? |
Sweat gland
receptor: Muscarinic |
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what is the receptor for the Parasympathetic system at the tissue?
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Muscarinic
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what are the Adverse Effects of Acetylcholine?
which is the only Nicotinic receptor response? |
DUMBBELSS:
Diarrhea, Urination, Miosis, Bradycardia, Bronchoconstriction, Excite skeletal muscle (N), Lacrimation, Sweat, Salivation |
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what receptors use Gq as their second messenger?
(5) |
HAVe 1 M&M:
H1 Alpha1 V1 M1 M3 |
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what G-protein uses Phospholipase C?
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Gq
|
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what receptors use Gi as their second messenger?
action? |
MAD 2s:
M2 Alpha2 D2 inhibits Adenylyl Cyclase |
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what receptor increases gastric acid secretion?
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H2
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Inhibits choline re-entering the presynaptic terminal
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Hemicholinium
|
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Inhibits ACh into vesicles
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Vesamicol
|
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Inhibits NE into vesicles
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Reserpine
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Inhibits release of ACh into synaptic membrane
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Botulinum
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Inhibits release of NE into synaptic membrane
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Guanethidine
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Promotes release of NE into synaptic membrane
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Amphetamines
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Inhibits reuptake of NE into presynaptic nerve
(2) |
Cocaine
TCA |
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what receptor does NE act on in the presynaptic neuron as neg feedback to inhibit its release?
|
alpha-2
|
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(3) Cholinomimetrics and use of each
|
Bethanechol - post-OP activates GI/GU
Carbachol - Glaucoma Pilocarpine - Glaucoma |
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Anticholinesterase used for post-OP activation of GI/GU, myasthinia gravis
what is it an antidote for? |
Neostigmine
antidote: Curarae (NMJ block) |
|
Anticholinesterase used for glaucoma and crosses BBB
what is it an Antidote for? |
Physostigmine
antidote: Atropine overdose |
|
(3) ACh receptor blockers
|
Atropine,
Scopalamine, Ipratropium |
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ACh receptor blocker used for Motion Sickness
|
Scopolamine
(DOC) |
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ACh receptor blocker used for Asthma/COPD
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Ipratropium
|
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what drug slows the HR at 0.5mg and increases it at >1.0mg?
|
Atropine
(muscarinic antagonist) |
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what are the AE of Atropine?
|
Opposite of DUMBBELSS:
Hot as hare, Dry as bone, Red as beet, Blind as Bat, Mad as hatter |
|
Insecticide antidote
|
Atropine
|
|
Nicotinic ACh receptor antagonist
use? |
Hexamethonium
use: prevents reflex bradycardia caused by NE |
|
drug used for intubation for its rapid onset and quick duration in causing flaccid paralysis
|
Succinylcholide
|
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which NMJ (nicotinic) blocker also releases histamine?
|
Tubocurarine
|
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Epinepherine effects on:
1. BP 2. HR 3. TPR |
Epinepherine
BP: Inc Systolic, Dec Diastolic HR: Inc (tachycardia) TPR: Dec |
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NE effects on:
1. BP 2. HR 3. TPR |
NE
BP: BIG INC in systolic and diastolic HR: DECREASES TPR: BIG INCREASE |
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Isoproterenol effects on:
1. BP 2. HR 3. TPR |
Isproterenol
BP: Decrease in systolic and diastolic HR: BIG INCREASE TPR: BIG DECREASE |
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DOC for Shock to increase renal perfusion and for CHF to increase CO
|
Dopamine
|
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DOC for CHF to increase CO w/o increasing oxygen demand
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Dobutamine
|
|
Alpha agonist that is used for HTN w/ renal Dz
|
Clonidine
|
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what occurs if atropine is given before NE?
|
Heart rate increases instead of decreases
|
|
a1-blocker for urinary retention in BPH and HTN
|
Prazosin
|
|
a2-blocker for depression
|
Mirtazapine
|
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what occurs w/ BP if a-blocker is given before Isoproterenol?
|
No change!
|
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what occurs w/ BP if a-blocker is given before Epinepherine?
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Reverses the vasoconstriction effect of Epi and Decreases BP
|
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which beta-blockers are beta1 selective?
|
if they start w/ A-M in alphabet
(except Labetalol - partial agonist) |
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what glaucoma drug should not be used in closed-angle glaucoma?
|
Epinepherine
|
|
Antidote/Tx for:
Salicylates |
Alkalinize urine
|
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Antidote/Tx for:
Anticholinesterases; Organophosphates (2) |
Atropine,
Pralidoxime |
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Antidote/Tx for:
Antimuscarinic; Anticholinergic agents |
Physostigmine
|
|
Antidote/Tx for:
beta-blockers |
Glucagon
|
|
Antidote/Tx for:
Digitalis (4) |
Stop Dig,
normalize K, Lidocaine, Magnesium |
|
Antidote/Tx for:
Iron |
Deferoxamine
|
|
Antidote/Tx for:
Lead (3) |
CaEDTA,
Dimercaprol, Succimer (kids) |
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Antidote/Tx for:
Arsenic, gold, mercury (2) |
Dimercaprol,
Succimer (kids) |
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Antidote/Tx for:
Copper |
Penicillamine
|
|
Antidote/Tx for:
Cyanide (3) |
Nitrite,
Hydrocobalamin, Thiosulfate |
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Antidote/Tx for:
Methemoglobin |
Methylene Blue
|
|
Antidote/Tx for:
Carbon Monoxide |
100% O2
(or hyperbaric O2) |
|
Antidote/Tx for:
Methanol, Ethylene glycol (antifreeze) (2) |
Ethanol,
Fomepizole |
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Antidote/Tx for:
Opioids (2) |
Naloxone,
Naltrexone |
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Antidote/Tx for:
Benzodiazepines |
Flumazenil
|
|
Antidote/Tx for:
TCAs |
NaHCO3
|
|
Antidote/Tx for:
Heparin |
Protamine
|
|
Antidote/Tx for:
Warfarin (2) |
Vitamin K,
FFP |
|
Antidote/Tx for:
tPA, Streptokinase |
Aminocaproic acid
|
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Urine pH and drug elimination for:
Weak acids |
alkalinize urine w/ Bicarb
|
|
Urine pH and drug elimination for:
Weak bases |
Acidify urine w/ NH4Cl
|
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What is the reversible cholinesterase inhibitor indicated for the Tx of Alzheimer's Dz?
|
Tacrine
|
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what is the skeletal muscle relaxant that acts directly on the contractile mechanism of the muscle fiber?
|
Dantrolene
|
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which Glaucoma agent acts by decreaseing production of aqueous humor?
|
Timolol
|
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why is Epi mixed w/ anesthetics?
|
to retard the systemic absorption
|
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which muscles are most affected by tubocurarine?
|
fine movement muscles (head, neck, face)
|
|
what is the alpha receptor-assoc eye muscle?
|
Radial muscle
|
|
what agent for bronchial asthma causes tremor?
|
Salmeterol
(b-agonist) |
|
what ANS drug class masks hypoglycemia in treated diabetics?
how? |
b-blockers
blocks catecholamines, which stimulate Glyconeogenesis |
|
(2) MAO inhibitors that are used for depression
|
Tranylclpromine,
Phenelzine sulfate |
|
DOC for thyroid storm
|
Propranolol
|
|
Definition:
two drugs act on the same tissue via independent receptors resulting in effects in the opposite direction |
Physiologic antagonist
|
|
Definition:
when two drugs combine and the activity of one or both drugs is blocked |
Chemical antagonist
|
|
equation for the Elimination constant
(2) |
Ke = 0.7/half-life = CL/Vd
|
|
when calculating an IV dosage, what needs to be remembered?
|
multiply drug (mg/kg) by weight (kg)
|
|
(2) equations for Extraction ratio
|
ER = (Ci-Co)/Ci = CL/Q
|
|
Which is not absorbed well in the stomach:
Aspirin (pKa = 3) or Propranolol (pka = 9.4)? |
Propranolol
|
|
the AE of convulsions are MC w/ what drug?
|
Strychnine
|
|
what drug can cause Hypocalemic Tetany?
|
Edetate Disodium (Na-EDTA)
|
|
what mineral toxicity can decrease Amylase secretion?
|
Zinc
|
|
AE of drug is Congenital goiter, Hypothyroidism
|
Methimazole
|
|
AE of drug is Agenesis of fetal kidneys
|
Chlorambucil
|