mix of drugs packaged in packets or sachets
active drug(s) combined witha binder and excipient. Mix is compressed into tablets by machine. Disc shaped
irritant tablets or those that would be destroyed by gastric acid that are coated with phenylsalicylate (salol) or other substance which is insoluble in acid but will dissolve in alkaline SI
mix of dugs and a sticky binder in form of ovoid or spherical mass provided with a glazed sugar coating
container made of mix of gelatin and glycerin and is suitable for drugs in powdered form and certain liquid drugs
large and cylindrical in shape; for horses and cattle
aqueous soln or suspension intended for oral administration. Aromatic water is added to prevent contamination with bacteria or mold
conical solid prep for intravaginal use in humans
conical solid prep given intrarectally for systemic effect in humans. Melts and releases active ingredients after being introduced into the body
semisolid prep for either external use or internal use
semisolid prep applied on the back of the tongue for a systemic effect
alcoholic liquid prep of nonvolatile substance either for external or internal use
alcoholic liquid prep of a volatile substance
aqueous suspension of insoluble solids and usually contains a dispering agent (gum tragacanth or methylcellulose) to delay settling. Bottle should contain phrase "shake well before use"
soln of medicinal agents, flavoring, and coloring agents in an 85% sucrose soln (more than 50% sucrose)
hydroalcoholic soln of medicinal agents that have been sweetened and flavored
oily substance dispersed in an aqueous medium with an emulsifying agent (gum acacia, lecithin, or methylcellulose)
obtained by poassing solvent over dried plant material (percolation) then evaporation of solvent or placing crude material in solvent until active substances are extracted (maceration).
extraction using cold water or warm water
extraction using boiling water
sterile solutinos or suspensions in an aqueous (sometimes an oil vehicle). Heat sterilized or filtered through Millipore filters. Some are unstable in soln and packaged aseptically in vials and then later reconstituted with sterile water immediately before use. Tablets for injections similar to powder in vials
repository forms (slow release form)
sustained release forms prolong effective drug conc. in body by providing for sustained release from dosage form
liquid or semisolid prep applied on skin with friction (rubbing); generally contains counterirritants used in chronic inflammation of muscles and tendons
soln or suspension of soothing substances to be applied on skin in acute inflamm. or to relieve pain
semisolid greasy prep in which drug is dissolved or dispensed in a suitable base
incorporates a drug in water-oil emulsion; water will evaporate following application leaving the drug and a thin film of oil on skin
mix of drugs in powder form for external use such as talc or starch as adsorbants
drug incorporated in a suitable solvent and packaged under pressure with a propellant such as fluorinated hydrocarbon or nitrogen
starch, sucrose, talc, polyvinylpyrrolidone (PVP) and resin
oral medication vehicles:
waters (peppermint water), syrup, elixir
sterile water, sterile saline, propylene glycol, polyethylene glycol, PVP, polysorbate 80 (Tween 80)
paraffin oil and wax, bees wax, Vaseline
1 oz = _____ drams
1 dram = ______ grains
60 grains (gr)
1 oz = ____ grains
1 oz x 8 drams/oz x 60 grains/drams= 480 grains
1 pint = _____ fluid ounces
16 fl. oz.
1 fl. oz. = ______ fluid drams
8 fluid drams
1 fluid dram = _____ minims (m)
1 gallon = ____ liters
1 L = ____ pints
1 kg = ____ lb
1 oz = ____ grams
1 fluid ounce = _____ mL
1 grain = _____ milligrams
1 mL =____ cc
study of movement of drugs across the biological membrane
transfer of a drug from site of administration to circulation
movement of drugs from blood to tissues
chemical alteration of the drug molecule in the body usually via enzymatic reactions within cells which will change the physiochemical properties of the drug and its pharmacological activity
removal or clearance of drug from the body
F%; fraction of the dose that reaches the systemic circulation
1st pass effect
drug biotransformation that significantly reduces quantity of the drug that reaches systemic circulation
resistance to ordinary dose of the drug
half the time the drug exists in the body
t1/2= 0.693/ Ke
how easily a drug enters lipid phase from aqueous solution; [oil]:[water] ratio
K is high= highly lipid soluble
K is low= poorly lipid soluble (unlikely to cross cell membrane)
a low K (partition coefficient) signifies what?
poorly lipid soluble
unlikely to cross cell membrane
specific type of endocytosis in which cell engulfs molecules of drugs in water
addition of an endogenous substrate to the drug or its metabolite (ex. glucuronidation)
acute tolerance to repeated administration of a drug
single nucleotide polymorphism
single NT substitution of one base for another that occurs in more than 1% of the population
what type of drug don't we give to lagomorphs?
why don't we give cats aspirin?
low amounts of glucuronyl transferase that metabolizes sialicylate via conjugation so aspirin is poorly metabolized
why don't we give cats acetominophen?
p450 produces NAPQ1 that lead to hepatotoxicity and nephrotoxicity
what happens to cats with opioids?
mydriasis (rather than miosis)
what is the only microsomal phase II reaction?
what are horses especially prone to with IM injections?
why don't we give dogs aspirin?
they have an aspirin hypersensitivity due to an accumulation of leukotrienes
why are NSAIDS especially bad when kidney function is lowered?
1. block Cox-1 found in arterioles, collecting ducts and glomeruli
•Therefore PGE-1 and PGI-2 and renin (vasodilatory) aren't made
•BP cannot be maintained and therefore decreased renal blood flow occurs
2. also block Cox-2 in the macula densa
•this secretes prostaglandin and increases if less tubular NaCl due to reduction in afferent arteriole pressure and decreased renin
•this also decreases blood flow in the kidney
why are NSAIDS bad w/ hypotension?
•As hypotension sets in and NSAIDs are used , no renin is released from afferent arterioles
•Without renin, Angiotensinogen isn't changed into Angiotensin I or Angiotensin II
•Without Angiotensin II:
1. No cardiac and vascular hypertrophy
2. No systemic vasoconstriction
3. No increase blood volume
4. No pituitary release of ADH
5. No stimulation of Aldosterone release from adrenal cortex
1. Renal sodium and fluid retention
2. Hyperkalemia (leads to cardiac issues!!)
•No compensation for hyptension systemically (reduced blood flow) alters kidney function
•Decreased renal blood flow alters kidney functions and up to ischemia and necrosis if acute intoxication of NSAID
how might kidney or liver disease effect dosage?
kidney: main site of excretion
liver: main site of transformation/ metabolization and also main site of producer of proteins so will affect protein binding in the plasma
which factors effect drug dosages for the very young AND the old? (3)
decreased plasma protein binding
which factors only effect the very young for drug dosages? (2)
growth related sensitivity
which factors effect drug dosages only in the old? (2)
decrease in blood flow
change in body composition/ health
how might SNPs affect drugs?
linked SNPs- don't reside within genes/ affect protein function but correspond to a particular drug response
causative SNPs- affects protein function and possibly influencing person's response to medication
what is most likely the cause of idiosyncratic drug reactions?
reactive drug metabolites that induce cell damage and immune response
what are 2 examples of idiosyncratic reaction?
how does tolerance to beta-2 adrenergic drugs occur?
beta-2 receptors are down regulated and thus the effect of the drug is diminished
can you give repeated amounts of thiopental? why/why not?
no; risk of accumulation especially because of slow metabolism in addition to redistribution
1+1=2 with drug dosages
1+1>2 with drug dosages
one drug can increase the effect of another
how can effect of drug-drug interactions be toxic?
increases the dose of one of the drugs to a toxic level or cancel the effect of one of the drugs due to protein binding in the blood of an effect on metabolization pathways
how do drugs that induce loss of plasma protein binding lead to toxicity?
leads to increased effect of weakly bound drugs by freeing them
this leads to increased efficacy and possible toxicity
what is the strongest promoter of the p450 metabolization pathway?
when giving phenobarbitol, what must we remember?
it is the strongest promoter of p450 metabolization
leads to rapid disappearance of the effect of drugs that use this pathway
what does a carbonic anhydrase inhibitor (CAI) do for renal excretion?
it is a urine alkalinizer that enhances the excretion of weak acids (salicylate like aspirin)
which types of transport are non-saturable? which is saturable?
1. passive simple diffusion= non
2. passive channel-mediated diffusion= non
1. passive carrier mediated diffusion= saturable!
2. Active carrier mediated= saturable!
acute tolerance vs. tolerance
acute tolerance = tachyphylaxis and its due to repeated administration of a drug (happens w/in hours)
other tolerance is days-weeks
what are 2 mechanisms of tolerance?
induction of biotransforming enzymes
down regulation of receptors
what is the mechanism for tolerance to NE?
TYR (tyramine) displaces NE and thus makes NE inactive quickly; type of tachyphylaxis
what is dosage regimen dependent on? (4)
• Route of administration
• Frequency of administration
• Duration of administration
what can you acidify urine for ion trapping?
ammonium chloride or di-methionine (for weak basic drugs)
what can you alkalinize urine for ion trapping?
sodium bicarbonate, CAI
If it is only the nonionized form of a drug that can pass through membranes, which form of weak acid can go through? Weak base?
acid: RCOOH (protonated)
base: RNH2 (nonprotonated)
what are the natural state of the drug acted upon by the pH of the medium/environment? (ionizable sites)
RCOOH and RNH2 (nonionized forms)
define ionizable sites?
can accept or donate a proton to become charged
does protein binding happen only in the plasma?
only _____ drug exerts diffusion pressure across membranes
T/F: though a drug is bound to a protein it can be metabolized
false; it cannot be distributed, metabolized or excreted by glomerular filtration when bound
T/F: drugs cannot bind to glycoproteins or lipoproteins
acidic drugs mainly bind what in the plasma? basic drugs?
basic: acid alpha-1-glycoproteins
at steady state, are all forms of the drug in equilibrium?
no! only nonionized, free form is in equilibrium
what level of binding induces significant effect on the drug-drug interaction?
how does protein binding affect the half life of a drug?
prolongs the half life
how does high plasma binding affect drug concentration in the plasma vs. tissues?
keeps drug concentration in plasma high relative to the rest of the body
if a drug has high plasma protein binding, how does that affect Vd? what if it has high tissue protein binding?
plasma: apparent Vd is lessened (still possible to have a high distribution)
tissue: HIGH VOLUME OF DISTRIBUTION (Vd> total body water)
what is Tilmicosin? where does it accumulate/ why? what can you use to block accumulation?
Tilmicosin: weakly basic drug used to help treat pneumonias because it accumulates in the acidic lysosomes of phagocytes
accumulation would be blocked by agents known to decrease proton conc of lysosomes like chloroquine, ammonium chloride, and bafilomycin
filtration derives its energy from where?
passive facilitated diffusion derives its energy from where?
the concentration of solute (down its concentration gradient)
where does primary active transport derive its energy from? secondary?
primary: high energy phosphate bonds like ATP
secondary: stored energy in the Na+ electrochemical gradient created using ATP in primary active transport (symporters or antiporters)
6 things that affect drug absorption:
1. molecular size
2. lipid solubility
3. degree of ionization
4. dissolution in water
5. concentration at the absorption site
6. route of administration
3 factors that affect passive diffusion
1. concentration gradient (high to low)
2. lipid solubility (lipophilic moves faster)
3 degree of ionization (nonionized diffuse through)
the _____ the concentration of the drug, the faster the absorption