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general pharm


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define volume of distribution
amount of drug in body/plasma drug concentration
define clearance
rate of elimination of drug/plasma drug concentration
relate half life to volume of distribution and clearance
t1/2 = (0.7*Vd)/CL
how many half life would it take to reach 87.5% of steady-state concentration?
the XXXX of plasma protein-bound drugs is affected in liver and kidney disease
volume of distribution
loading dose calculation
target plasma concentration X volume of distribution / bioavailability
what is the bioavailability in an IV dose
maintenance dose calculation
target plasma concentration X clearance / bioavailability
does loading dose or maintenance dose change in impaired renal/hepatic function?
maintenance dose
define zero-order elimination
rate of elimination is constant regardless of drug concentration
how does the plasma drug concentration decrease with time in zero-order elimination?
give 3 examples of zero-order elimination drugs
ethanol, phenytoin, aspirin
define first-order elimination
rate of elimination is propotional to drug concentration
how does the plasma drug concentration decrease with time in first-order elimination?
what system is involved in phase I metabolism?
cytochrome p-450
what is the overall mechanism of phase II metabolism
what is yielded after phase I metabolism
slightly polar, water soluble metabolites that are often still active
what is yielded ater phase II metabolism?
very polar inactive metabolites that are renally excreted
what are 3 mechanisms of phase II metabolism
acetylation, sulfation, glucuronidation
what are 3 mechanisms of phase I metabolism
reduction, oxidation, hydrolysis
what phase of metabolism do elderly patients lose first?
phase I metaoblism
what effect does a competitive antagonist have on a dose-response curve?
shift to the right and decrease potency
what effect does a noncompetitive antagonist have on a dose-response curve?
shift downward. decrease efficacy
how is the Kd related to the EC50 in a system with spare receptors
Kd > EC50
define Kd
concentration of drugs required to bind 50% of receptor spots
what is the different between partial agonist and full agonist in a dose-response curve
partial agonist has lower maximal efficacy no matter how much dose is increased but both shift to left
how does a partial agonist compare with a full agonist in terms of potency?
could be less, more, or equally potent. potency = independent factor
define therapeutic index
median toxic dose / median effective dose
what is done in vitro studies?
production of compound
what is evaluated in animal testing (3)?
efficacy, selectivity, mechanism
what is evaluated in phase I clinical testing? (2)
is it safe? pharmocodynamics?
what is evaluated in phase II clinical testing
does it work in patients?
what is evaluated in phase III clinical testing?
does it work (double=blind)
what is evaluated in the marketing phase of drug development?
postmarketing surveillance
how long until patent expires and generics become available?
20 years
define drug efficacy
maximum effect that can be produced by drug
define drug potency
dose required to produce 50% of drug's maximal effect
define LD50
lethal dose in 50% of patients
how do you determine steady-state concentration of a drug?
dosing rate / clearance
name all of the p450 inducers
quinidine, barbituates, phenytoin, rifampin, griseofulvin, carbamazepine
name all of the p450 inhibitors
isoniazid, sulfonamides, cimetidine, ketoconazole, erythromycin, grapefruit juice, st. john's wort (inhibitors stop cyber-kids from eating grapefruits)
use for echinacea
common cold
ephedra toxicities
cns and cardiovascular stimulation, arryhtmias/strokes/seizures at high doses
use for feverfew
feverfew toxicities
mouth ulcers, antiplatelet actions
use for ginko
intermittent claudication
ginko toxicities
anxiety, antiplatelet
kava use
chronic anxiety
kava toxicities
sedaion, hepatotoxicity, phototoxicity, dermatotoxicity
milk thistle use
viral hepatitis
milk thistle toxicity
loose stool
saw palmetto use
benign prostatic hyperplasia
saw palmetto toxicities
decrease libido, hypertension
st. john's wort use
mild to moderate depression
st. john's wort toxicities
phototoxicity, seratonin syndrome with SSRIs, inhibit p-450 system
DHEA (dehydroepiandrosterone) use
improvement in females with AIDS/SLE
DHEA toxicities
androgenization in premenopause, estrogen effects in postmenopause, feminization in young men
melatonin use
jet lag insomnia
melatonin toxicities
sedation, suppress midcycle LH, hypoprolactinemia
what organella is cytochrome p-450 located in
smooth endoplasmic reticulum
henderson hasselbach equatoin
ph = pka + log (A-/HA)
is a weak acidic charged?
is a weak base charged?
does a charged or uncharged drug pass through membranes easier?
what effect does alcohol have in pharmacokinetics?
it will induces p450 system
how many 1/2 lives does it take to achieve steady state?

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