Introduction Flashcards
golden period for giving pralidoxime
6-8 hours
smallest drug by MW
lithium
largest drug by MW
alteplase
excretion of a weak base may be accelerated by acidifying urine with
ammonium chloride
drug w/ no oral form, undergoes 100% 1st pass effect
nitroglycerin
drugs with IM=oral bioavailability
Metronidazole, Clindamycin
vessel in superomedial aspect of buttocks
sup.gluteal n.
vessel in inferomedial aspect of buttocks
sciatic nerve
blood vessels passed by SL drugs
lingual vein-internal jugular v-brachiocephalic/innominate v-SVC-RA
rectal vein responsible for partial first-pass effect on rectal (suppository) route
superior rectal vein-> inferior mesenteric vein–> portal vein
topical route, poorest ability to evaporate, better for chronic inflammation
ointment
topical route, greatest ability to evaporate, better for acute inflammation
tinctures
binding of acidic drugs
albumin
binding of basic drugs
orosomucoid
known teratogenic effect of methimazole
cutis aplasia
DOC for hyperthyroid pregnant
PTU
this drug undergoes elimination without metabolism
lithium
rate of elimination is proportionate to the concentration
first-order elimination
rate of elimination is constant regardless of concentration
zero-order elimination
concentration decreases linearly
zero-order
concentration decreases exponentially
first-order
occurs when drugs have saturated their elimination mechanisms
zero-order elimination
drugs with zero-order elimination
warfarin, heparin, aspirin, tolbutamide, phenytoin, ethanol, theophylline (WHATPET)
dose at which 50% of maximal effect is reached
potency (EC50)
concentration required to bind 50% of the receptors
Kd
minimum dose required to produce a specified response is determined in each member of a population
quantal dose-response curve
determines median effective (ED50), median toxic (TD50) and median lethal dose (LD50)–> three potency variables
quantal dose-response curve
formula for therapeutic index
median toxic dose/median effective dose
measures drug efficacy
graded dose-response curve
nonselective alpha antagonist, serves as a noncompetetive/irreversible antagonist which is the DOC for pheochromocytoma
phenoxybenzamine
binding to a different receptor, producing an effect opposite to the drug it is antagonizing
physiologic antagonists
physiologic antagonist of histamine
epinephrine
physiologic antagonist of thyroid hormone
propranolol
chemical antagonist for lead poisoning
dimercaprol
reduces constitutive activity
inverse agonist
drugs displaying tachyphylaxis
metoclopromide, ephedrine, dobutamine, LSD, calcitonin, nitroglycerin, nicotine, hydralazine, desmopressin
continuous activation may lead to depletion of essential substrates
tolerance
nitroglycerin tolerance can be reversible by administration of
glutathione
infrequently observed response
idiosyncratic drug response
example of idiosyncratic drug response- aplastic anemia
chloramphenicol
example of idiosyncratic drug response- cataracts
allopurinol
formula for apparent volume of distribution
amount of drug in tissue/ plasma drug concentration
formula for clearance
rate of elimination/plasma concentration
formula for half-life
0.693x Vd/CL
bioavailability is determined by computing
AUC
maintenance dose computation
clearance x desired plasma concentration / bioavailability
loading dose computation
Vd x desired plasma concentration / bioavailability
phase 1/phase 2 reaction? hydrolysis
phase 1
phase 1/phase 2 reaction? oxidation
phase 1
phase 1/phase 2 reaction? reduction
phase 1
phase 1/phase 2 reaction? deamination
phase 1
phase 1/phase 2 reaction? dealkylation
phase 1
phase 1/phase 2 reaction? dehydrogenation
phase 1
phase 1/phase 2 reaction? gluocoronidation
phase 2
phase 1/phase 2 reaction? acetylation
phase 2
phase 1/phase 2 reaction? glutathione conjugation
phase 2
phase 1/phase 2 reaction? glycine conjugation
phase 2
phase 1/phase 2 reaction? sulfation
phase 2
phase 1/phase 2 reaction? methylation
phase 2
teratogenic effect: ACEI
fetal renal damage
teratogenic effect: antiepileptic drugs
NTDs
teratogenic effect: phenytoin
fetal hydantoin syndrome
teratogenic effect: oral hypoglycemic agents
neonatal hypoglycemia
teratogenic effect: barbiturates
neonatal dependence
teratogenic effect: DES
vaginal clear cell adenoCA
teratogenic effect: ethanol
fetal alcohol syndrome
teratogenic effect: Lithium
Ebstein’s anomaly
teratogenic effect: isotretinoin
craniofacial malformations
teratogenic effect: iodide
congenital hypothyroidism
teratogenic effect: misoprostol
Mobius sequence
teratogenic effect: penicillamine
cutis laxa
teratogenic effect: thalidomide
phocomelia
teratogenic effect: smoking
IUGR
teratogenic effect: tetracycline
tooth discoloration
teratogenic effect: streptomycin
ototoxicity
teratogenic effect: sulfonamides
kernicterus
teratogenic effect: fluoroquinolones
cartilage damage
teratogenic effect: warfarin
1st tri: chondrodysplasia, 2nd: CNS malformations, 3rd: bleeding diatheses
standard in vitro test for mutagenicity
Ames test
in vivo mutagenicity test in mice
Dominant lethal test
trial among normal human volunteers
phase 1 trial
evaluation of a drug in a moderate number of patients
phase 2 trial
large design involving many patients
phase 3 trial
compares therapy with the gold standard
phase 3 trial
postmarketing surveillance phase
phase 4 trial
detects toxicities that occur infrequently
phase 4 trial
comparable bioavailability and similar times to achieve peak blood concentrations
bioequivalence
drug for a rare disease (affecting <200,000)
orphan drug