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DP FINAL EXAM cards
final final
172
Pharmacology
Graduate
04/30/2012

Additional Pharmacology Flashcards

 


 

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Term
myristyl alcohol
Definition
fatty alcohol
Term
cetyl alcohol
Definition
fatty alcohol
Term
stearyl alcohol
Definition
fatty alcohol
Term
mystric acid
Definition
fatty acid
Term
stearic acid
Definition
fatty acid
Term
oleic acid
Definition
fatty acid
Term
isopropyl myristate
Definition
fatty acid ester
Term
isopropyl palmitate
Definition
fatty acid ester
Term
glycerol
Definition
polyol
Term
propylene glycol
Definition
polyol
Term
polyethylene glycol
Definition
polyol
Term
sodium lauryl sulfate
Definition
anionic surfactant
Term
benzalkonium chloride
Definition
cationic surfactant
Term
lecithins
Definition
amphoteric surfactant
Term
spans
Definition
non ionic surfactant
Term
tweens
Definition
non ionic surfactant
Term
poloxamers
Definition
non ionic surfactant
Term
where can u apply androderm?
Definition
only scrotum
Term
where can u apply testoderm
Definition
anywhere
Term
acrylic psa
Definition
one of the matrix adhesive layer types
Term
silicone psa
Definition
one of the matrix adhesive layer types
Term
polyisobutyl
Definition
one of the matrix adhesive layer types
Term
ethylene vinyl acetate
Definition
non porous RATE CONTROLLING MEMBRANE copolymer
Term
Polyethylene/Polypropylene
Definition
MICROPOROUS Rate CONTROLLING MEMBRANE colpolymer
Term
Scopolamine
(Transderm Scop)
Definition
Adhesive Matrix
Term
Nitroglycerin
(Deponit)
Definition
Adhesive matrix
Term
Nitroglycerin
(Transderm- Nitro)
Definition
Reservoir system
Term
Clonidine
(Catapress TTS)
Definition
Reservoir system
Term
Estradiol
(Estraderm)
Definition
Reservoir system
Term
Estradiol
(Vivelle)
Definition
Adhesive matrix
Term
Estradiol
(Climara)
Definition
Adhesive matrix
Term
Testosterone
(Testoderm)
Definition
Adhesive matrix
Term
Testosterone
(Androderm)
Definition
Reservoir system
Term
Nicotine
(Habitrol)
Definition
Reservoir system
Term
Oxybutynin
(Oxytrol)
Definition
Adhesive matrix
Term
Methyl Phenidate
(Daytrana)
Definition
Adhesive matrix
Term
Fentanyl
(Duragesic)
Definition
Reservoir system
Term
Selegiline
(Emsam)
Definition
Adhesive matrix
Term
Rotigotine
(Neupro)
Definition
Adhesive matrix
Term
Rivastigmine
(Excelon)
Definition
Adhesive matrix
Term
lidocaine
Definition
neulagia herpes pain and iontophoresis enhanced drug
Term
tween 80
Definition
emulsifier
Term
trimethicilone + stearic acid =
Definition
emulsifier
Term
glycerin
Definition
levigating agent, preservative, emmolient
Term
soap
Definition
permeability enhancer
Term
methylcellulose
Definition
gelling agent
Term
ethyl alcohol
Definition
cosolvent for better dissolution
Term
sodium benzoate
Definition
buffer and preservative
Term
to prolong shelf life
Definition
freeze dry routinely
Term
lysine
Definition
amino acid solubility enhancer
Term
arginine
Definition
amino acid solubility enhancer
Term
sodium dodecyclsulfate
Definition
surfactant
Term
albumin
Definition
anti absorptionn / anti aggregation agent
Term
polysorbate 80
Definition
anti absorption/ anti aggregation agent
Term
phosphate
Definition
buffer component
Term
citrate
Definition
buffer component
Term
acetate
Definition
buffer component
Term
ascorbic acid
Definition
antioxidant
Term
sodium formaldehyde sulfoxylate
Definition
antioxidant
Term
methionine
Definition
antioxidant
Term
sodium thiosulfate
Definition
antioxidant
Term
phenylmercuric nitrate
Definition
preservative
Term
thermersol and alccohols
Definition
preservative
Term
methionine, cysteine molecular oxygen H2O2 aromatic aminoacids all undergo
Definition
Oxidation
Term
fridge or freeze proteins?
Definition
never FREEze only fridge
Term
2% water required for
Definition
dehydration. never completely dehydate 100% the biotech drugs
Term
p- hydroxy benzoic acids (parabens)
Definition
presservatives
Term
phenol
Definition
Preservative
Term
Benzyl alcohol
Definition
Preservative
Term
Chloro butanol
Definition
Preservative
Term
Saline
Definition
Osmotic bulking agent
Term
monosaccharide or disacchride
Definition
Osmotic bulking agent
Term
Sorbitol
Definition
Osmtic bulking agent
Term
sucrose, or dextrose or lactose
Definition
osmotic bulking agents
and STABILIZER
Term
PEG 400
Definition
Osmotic bulking agent
Term
mannitol
Definition
Osmotic bulking agent
Term
route ranking for protein peptides
Definition
IV > NASAL > SQ. ORal is a fail cuz it breaks before its absorbed.
Term
amount of AA for:
Ace inhibitors, TSH analogues
Definition
<8 AA
Term
amount of AA for:
Calcitonin, cyclosporin (only peptide with oral bioavialbility)
Definition
8-50 AA
Term
amount of AA for:
Insulin,GH, interferon
Definition
50-2500 AA
Term
bioavailability of peptides, hi or low?
Definition
low
Term
metabolism of peptides, fast or slow?
Definition
fast
Term
difference between protein and standardized synthetic drugs
Definition
proteins have specialized uptake and binding mech
Term
Most peptide drugs Vd is Big or Small?
Definition
Small < 0.2 L/Kg
Term
tPA Vd is big or small?
Definition
Large. one of the exceptions. 7.6 Vd cuz it has lots of binding sites to distribute to outside the plasma
Term
Gasatrin releasing factor Vd is big or small?
Definition
Large.
Term
small Vd is
Definition
Volume of distribution. means more drug is in the plasma
Term
Large Vd is
Definition
more drug outside plasma
Term
Small Vd + High Clearance = small or big t1/2
Definition
Short t1/2
Term
Erythropoiten t1/2 is small or larger?
Definition
LONG. 8 to 9 hours. it is the exception
Term
Vss and Vd area are 2x the Plasma Vd (which is Vc) for most peptide drugs.
what are the exceptions?
Definition
calcitonin
EPO
GH'
interferon
TNF
Term
PTS 1 - 2
Definition
Brain to blood Protein transport system
Term
PTS 3
Definition
Blood to brain Protein transport system
Term
PTS 4
Definition
Both blood to brain and brain to blood transport system
Term
four types of receptors: whats the ligand for alpha 2 Macroglobulin receptor?
Definition
interleukin 1 beta and TGF Beta
Term
four types of receptors: whats the ligand
for LDL receptor?
Definition
cyclosporine
Term
four types of receptors: whats the ligand
for Mannose Terminated Glycoprotein Receptor?
Definition
Renin
Term
four types of receptors: whats the ligand for (N acetyl galactosamine terminated asialo glycoprotein receptor ) AKA the GALACTOSE RECEPTOR?
Definition
tPA, Interferone, EPO
Term
sources of nonlinearity in Peptide PK?
Definition
receptor mediated endocytosis (saturatable)

Endo + Exo peptidase (saturatable)

Binding proteins (saturatable like tPA)


this makes it dose dependent
Term
DOSE depends on
Definition
hepatic and renal clearance

increasing the dose causes Vd to increase or decrease

increase dose increases t1/2
Term
if we increase the dose saturate the binding proteins in the PLASMA
what happens to Vd?
Definition
Vd Goes UP as we increase the dose
Term
if its not being bound in the plasma by binding proteins it will go in the DEEP COMPARTMENT periphery and saturates binding sites there. what happens to vD?
Definition
Vd goes down as we increase the dose
Term
suppositories are intended for
Definition
Insertion into rectum, vagina, urethra,

they melt or dissolve when inserted
Term
for suppositories, a decrease in particle size does what to absorption?
Definition
faster absorption
Term
1. Oleaginous Fatty Base name:
2. Melt fast or slow?
3. miscible or immiscible with rectal fluid?
4. absorption fast or slow?
5. fatty suppository based are better for what type of drugs?
Definition
1. cocoa butter
2.fast melt
3. Immiscible with rectal fluid
4. slow absoprtion
5. Water soluble drugs
Term
1. Water Soluble base name:
2. Melt fast or slow?
3. miscible or immiscible with rectal fluid?
4. absorption fast or slow?
5. fatty suppository based are better for what type of drugs?
Definition
1. PEG
2.dissolve fast
3. miscible with rectal fluid
4. slow absoprtion still
5. Lipid soluble drugs
Term
vaginal suppositories are what type of tablets?
Definition
Compressed tablets
Term
Pessaries
Water soluble bases prefered
Definition
Vaginal Suppositores 5grams
Term
Bougies
local effect
Definition
Urethral suppositores (3-6mm)
Term
polyoxyl 40 stearate
Definition
O/W surfactant for suppositories
Term
Glycerinated Gelatin
Definition
Water soluble base of glycerin water and gelatin.

BASE IS HYDROSCOPIC

gives prolonged action and does NOT LEAK
Term
Fatty bases require fridge or not?
Definition
Fridge
Term
water soluble bases require fridge or not
Definition
No fridge
Term
Fusion lubricants:
1.cocoa butter
Definition
glycerin
Term
Fusion lubricants
1. PEG
Definition
Mineral oil
Term
why should u not cool suppositories by fusion to rapidly?
Definition
contraction
Term
U shape
Definition
= temp too high or over filling or cool too rapidly
Term
name the suppository manufacturer problem:
hollow nose suppository =
Definition
excess lubricant like mineral oil forms a ball at the bottom and displaces the tip.
Term
name the suppository manufacturer problem:

drug settled at nose tip
Definition
didnt stirr and base solidified, insoluble drug. drug not soluble in base and u heat it up and poured it too late cuz stopped stirring. like bismuth
keep stirring till just pourable to prevent this settling tip breaks off easily.
Term
name the suppository manufacturer problem:
layered streaks of drug in suppository=
Definition
didnt pour continously
Term
name the suppository manufacturer problem:

circular o shaped hole in suppository base top:
Definition
put in ice bath and it contracts real hard. so you have that hole.
Term
split in half suppository:
Definition
inssuficient mold lubrication.
Term
silicone dioxide in hydromorphone
Definition
Suspending agent to prevent drug from going into tip of suppository
Term
White Wax
Definition
Used as a stiffening agent but the promethazine probably is one of those drugs that lower the cocoa butter melting point and that means the cocoa butter would not be solid at room temperature ever. So the white wax gives you a solid suppository still. But if you do too much then the drug will now slowly release cuz its too stiff
Term
Butylated hydroxyANISOLE
Definition
Antioxidant
Term
shape and dimensions of dosage for dinoprostone give what benefit?
Definition
Larger surface area
Term
Evacuation Enema
Definition
cleanse bowel
Term
Retention Enema
Definition
local effect or systemic absorption
Term
how many years to develop biotech drugs?
5 or 7 or 12 or 15 years?
Definition
7
Term
advantage of biotech drugs
Definition
cheap
Term
disadavantage of biotech vs traditional
Definition
less stable
Term
What is the Cloning Process:
Definition
 Gene of interest is cut out with restriction enzymes (RE)
 Host plasmid (circular chromosome) is cut with same REs
 Gene is inserted into plasmid and ligated with ligase
 New engineered plasmid inserted into bacterium
Term
PCR process
Definition
• First, DNA is denatured to separate strands
• Next, primer is hybridized (specific location) on each DNA strand
• Finally, DNA polymerase enzyme is added for extension of the primer along the DNA strand to copy the target nucleic acid sequence
• Repeat as desired
Term
Sense Sequence:
Definition
Nucleotide chain that contains the information for protein synthesis
Term
o Antisense Sequence
Definition
Complimentary (to sense sequence) nucleotide chain
 Antisense drugs recognize and bind to the nucleotide sense sequence of specific mRNA molecules preventing synthesis of unwanted proteins and actually destroying the sense molecules in the process.
Term
magic number of aminoacids that higher or lower tells if peptide or protein
Definition
40
Term
proteins at their isoelectric point in terms of stability and solubility?
Definition
most stable
least soluble
Term
glycosilation linkages
Definition
for biodistribution of proteins
d
Term
aspartyl prolyl linkages
Definition
vulnerable to hydrolysis and occur in acid ph hi temp
Term
denaturation occurs by
Definition
high temp
shearing
shaking
pressure
Term
o Non-Ionic Surfactants and Cylcodextrins:
Definition
Inhibit protein aggregation and precipitation
o
Term
Addition of Sugars (Dextran):
Definition
Displace water and reduce microbial growth
Term
o Co-Solvents: (i.e. Glycerol, Polyethylene)
Definition
Have a stabilizing effect
Term
Conversion of a solid to a gas (lyophilization or sublimation)
Definition
Freeze drying
Term
atomize protein solution and particles and dry in air stream
Definition
Spray dry
Term
benefit of freeze dry
Definition
cost effective and prolongs shelf life
Term
benefit of spray dry
Definition
better particle control and enhanced flow. good for non paraenteral
Term
• Becaplermin (Regranex
Definition
CARBOXYMeTHLCELLULOSE gel for Diabetic foot ulcer
Term
Dornase alfa
Definition
inhalataion for cystic fibrosis
Term
Exubera
Definition
Nonivasive Insulin
Term
Fomivirsen
Definition
Phophorthiate 2nd line treatment for cytalomeagovirus retinitis
Term
Size dependant protein peptide elimination route:

<0.5
Definition
liver, blood (HYDROLYSIS)
Term
Size dependant protein peptide elimination route:

0.5-1
Definition
Carrier mediated elimination LIVER more specific
Term
Size dependant protein peptide elimination route:

1-50
Definition
Kidney GFR filtration FLUID endocytosis
Term
Size dependant protein peptide elimination route:

50- 200
Definition
Opsonization Receptor mediated
Term
Size dependant protein peptide elimination route:

>400
Definition
Phagocytosis
Term
kidney metabolism data
Definition
 Must be less than 60kDa to filter through Glomerulus
• < 5kDa undergo hydrolysis (Bradykinin, Angiotensin)
• > 5kDa endocytosis (to be digested)
Term
liver metabolism data
Definition
• Small Proteins and Peptides:
o Diffuse or Carrier transport to cytosol or Endoplasmic Reticulum
o Metabolized by proteases (calpains) and endo-/exopeptidases
• Large Proteins and Peptides:
o Passive Diffusion or adhere to hepatocytes membrane
 Then fluid or receptor mediated endocytosis
Term
drug absorption limiting barrier
Definition
stratum corneum
Term
skin layer resistance
Definition
SC > epidermis > dermis
Term
advantage of Matrix
and disadvantage
Definition
sleek thin, daily or multiple day application.

Dis: less control on release rate (rate limiting)
Term
Advantage and disadvantage of Reservoir
Definition
good for POTENT drugs
Release rate controlled

Bad: rupture of control membrane leads to dose dumping
Term
FRANZ vertical diffusion
Definition
Used for patch formulations, ointments, solutions and suspensions
Term
horizontal diffusion cell
Definition
used for Liquid preparations (solution suspensions ONLY
Term
o AKo = CpVdKel
Definition
 A: Area of applicable system
 Ko: Target Delivery Rate of the drug
 Cp: Plasma Concentration
 Vd: Volume of Distribution
 Kel: Elimination Rate from Plasma
Term
o Flux (J) = (DKC)/h
 Flux (J): The amount of drug transported through a unit of skin per unit of time
 D: Diffusion coefficient of the drug
 K: Partition Coefficient
 C: Drug concentration in the vehicle or delivery system
 h: Thickness of skin

SKIN enhancers
Definition
 Increase drug permeability (DK) in the stratum Corneum
• Act as solvents to dissolve the skin lipids or denature skin proteins
 Increasing the drug Solubility (C) in the Transdermal formulation (Patch)
Term
• Skin Penetration Enhancers:
o Work by

3 things
Definition
 Disrupting the order of the stratum Corneum lipids
 Interaction with cellular proteins
 Increasing the solubility of the drug in the topical/Transdermal formulation
Term
• Unlike synthetic drugs, it is better to give protein and peptide drugs at _______ doses, over a ______ period of time to see a more dramatic result.
Definition
lower doses

longer periods
Term
 Attachment of PEG to Protein/Peptide:
Definition
• Larger and more hydrophilic
• Discourages hepato-uptake
• Blocks receptor-mediated endocytosis (decreases clearance)
• Decreases distribution (V)
Term
 Carbohydrate addition or change:
Definition
• May hide from receptor-mediated endocytosis (May decrease Clearance)
o Have to be careful not to affect target/receptor interactions
 Cross-linking Carbohydrates may help
Term
o PK-PD model is used to understand the time course of concentrations and effects
o Standard Drugs: Desire constant drug plasma concentration to get constant effects
 This may not be desired with peptide and protein drugs

BECAUSE
Definition
They stimulate or mimic physiological effects and Protein PEPTIDE metabolism, elimination and binding all happen in one spot at one time
Term
 TPA: Alteplase (rh-t-PA):
• Rapid metabolism, Deactivation by PAI-1

so whats great about Tenecteplase?
Definition
 Tenecteplase: TPA variant
• Increased (3-10 Times) Potency
• Decreased (6-8 fold) in Clearance
• Higher fibrin specificity
• Resistant to PAI-1
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