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117 Cards in this Set

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amount of drug in body/_______ = Vd
plasma drug concentration


(Vd is Volume of Distribution)
rate of elimination of drug/[plasma drug] = ?
CL (Clearance)
(.7)(Vd)/CL = ?
T 1/2
A drug infused at a constant rate reaches about 94% of steady state after _______ t 1/2s.
4
A loading dose is calculated using this formula.
Loading Dose = (Cp)(Vd)/F

(Cp = target plasma conc; F = bioavailability)
A maintenance dose is calculated using this formula.
(Cp)(CL)/F

(CL = Clearance)
Rate of elimination is proportional to _______ ______ in 1st order elimination.
drug concentration
In the case of EtOH, which is elimated by _____ order elimination, a constant amount of drug is eliminated per unit time.
zero
Phase ____ (I or II) reactions yield slightly polar metabolites that are often _____ (active or inactive)
I, active
Phase ____ (I or II) reactions yield very polar metabolites that are often _____ (active or inactive) and are excreted by the _______.
II, inactive, kidney
Phase II reactions are often of this type.
conjugation
Cytochrome P-450 is involved in _____ phase (I or II) reactions.
I
A drug patent lasts for _____ years after filing for application.
20
How many phases are there in drug development?
4
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 _____.
2,1,3,4
In a dose response curve, a competitive antagonist shifts the curve _____

a non-competitive antagonist shifts the curve ______.
right

down
What pharmacologic relationship would determine the existence of spare receptors?
EC50 is lower then Kd (EC50 is more to the left)
What does it mean if EC50 and Kd are equal?
The system does not have spare receptors
A partial agonist acts on the same receptor system as a full agonist? T/F
TRUE
What's the main difference between a partial agonist and a full agonist?
A partial agonist has a lower maximal efficacy.
Is a partial agonist less potent than a full agonist?
Not necessarily. It can be less, more or equally potent as a full agonist.
Equation for Half Life
T 1/2 = (0.7 x Vd)/CL
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%
How do the Loading and Maintenance doses change in a patient w/ Renal or Hepatic dysfunction?
Loading - unchanged


Maintenance - Decreased
Equation for Theraputic Index
TI = Toxic dose/Effective dose
Phase in clinical drug testing:

safety, pharmacokinetics
1
Phase in clinical drug testing:

Protocol, dose level, work on patients
2
Phase in clinical drug testing:

double blind study, efficacy, adverse effects
3
(3) drugs that use Zero-order elimination
Alcohol,

Aspirin,

Phenytoin
What phase of a reaction uses cytP-450?

What is the purpose of this phase?
Phase I

converts lipophilic to polar
What is the main focus of Phase II reactions?
Conjugation
When pH < pKa, what is more common?
(2)

which can pass through the membrane?
HA and BH+


HA passes thru the membrane (uncharged)
Definition:

Amount of the drug required for a given response
Potency
what is the first NT to everything?

the first receptor?
NT: ACh

Receptor: Nicotinic
what system does not have a synapse from the spinal cord to the tissue?
Somatic NS

(skeletal muscle)

ACh to Nicotinic receptor
what is the only sympathetic ACh?

what is the receptor?
Sweat gland


receptor: Muscarinic
what is the receptor for the Parasympathetic system at the tissue?
Muscarinic
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
what receptors use Gq as their second messenger?
(5)
HAVe 1 M&M:
H1
Alpha1
V1
M1
M3
what G-protein uses Phospholipase C?
Gq
what receptors use Gi as their second messenger?

action?
MAD 2s:
M2
Alpha2
D2

inhibits Adenylyl Cyclase
what receptor increases gastric acid secretion?
H2
Inhibits choline re-entering the presynaptic terminal
Hemicholinium
Inhibits ACh into vesicles
Vesamicol
Inhibits NE into vesicles
Reserpine
Inhibits release of ACh into synaptic membrane
Botulinum
Inhibits release of NE into synaptic membrane
Guanethidine
Promotes release of NE into synaptic membrane
Amphetamines
Inhibits reuptake of NE into presynaptic nerve
(2)
Cocaine

TCA
what receptor does NE act on in the presynaptic neuron as neg feedback to inhibit its release?
alpha-2
(3) Cholinomimetrics and use of each
Bethanechol - post-OP activates GI/GU

Carbachol - Glaucoma

Pilocarpine - Glaucoma
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
ACh receptor blocker used for Motion Sickness
Scopolamine

(DOC)
ACh receptor blocker used for Asthma/COPD
Ipratropium
what drug slows the HR at 0.5mg and increases it at >1.0mg?
Atropine

(muscarinic antagonist)
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
which NMJ (nicotinic) blocker also releases histamine?
Tubocurarine
Epinepherine effects on:

1. BP

2. HR

3. TPR
Epinepherine

BP: Inc Systolic, Dec Diastolic

HR: Inc (tachycardia)

TPR: Dec
NE effects on:

1. BP

2. HR

3. TPR
NE

BP: BIG INC in systolic and diastolic

HR: DECREASES

TPR: BIG INCREASE
Isoproterenol effects on:

1. BP

2. HR

3. TPR
Isproterenol

BP: Decrease in systolic and diastolic

HR: BIG INCREASE

TPR: BIG DECREASE
DOC for Shock to increase renal perfusion and for CHF to increase CO
Dopamine
DOC for CHF to increase CO w/o increasing oxygen demand
Dobutamine
Alpha agonist that is used for HTN w/ renal Dz
Clonidine
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
what occurs w/ BP if a-blocker is given before Isoproterenol?
No change!
what occurs w/ BP if a-blocker is given before Epinepherine?
Reverses the vasoconstriction effect of Epi and Decreases BP
which beta-blockers are beta1 selective?
if they start w/ A-M in alphabet

(except Labetalol - partial agonist)
what glaucoma drug should not be used in closed-angle glaucoma?
Epinepherine
Antidote/Tx for:

Salicylates
Alkalinize urine
Antidote/Tx for:

Anticholinesterases;
Organophosphates
(2)
Atropine,

Pralidoxime
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)
Antidote/Tx for:

Arsenic, gold, mercury
(2)
Dimercaprol,

Succimer (kids)
Antidote/Tx for:

Copper
Penicillamine
Antidote/Tx for:

Cyanide
(3)
Nitrite,

Hydrocobalamin,

Thiosulfate
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
Antidote/Tx for:

Opioids
(2)
Naloxone,

Naltrexone
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
Urine pH and drug elimination for:

Weak acids
alkalinize urine w/ Bicarb
Urine pH and drug elimination for:

Weak bases
Acidify urine w/ NH4Cl
What is the reversible cholinesterase inhibitor indicated for the Tx of Alzheimer's Dz?
Tacrine
what is the skeletal muscle relaxant that acts directly on the contractile mechanism of the muscle fiber?
Dantrolene
which Glaucoma agent acts by decreaseing production of aqueous humor?
Timolol
why is Epi mixed w/ anesthetics?
to retard the systemic absorption
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