問題一覧
1
Study of pharmacotechnical factors in drug products
biopharmaceutics
2
Study of the process that a drug undergoes from the moment it enters the body until it leaves
pharmacokinetics
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The only biopharmaceutics process. Converting drug to its solution form. Highly modifiable. Primary determinant
liberation
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Rate and extent of drug entry into the systemic circulation
absorption
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Movement of drug from systemic circulation to different compartments
distribution
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A space in the body pertaining to organs and tissues deemed as kinetically homogenous (peripheral compartment)
compartment
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Joint space
intraarticular
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Intraosseus
bone
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Intraspinal
vertebral column
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Intrasynovial
joint fluid area
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Maximum therapeutic concentration
minimum toxic concentration
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High dosing frequency, risk of non compliance
immediate release
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Follows immediate release graph but allows for a second release. Fast onset
bimodal release
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Racemic. Equal portions of levo and dextro isomers
chirality
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Created a bigger compound, making it less soluble
complex formation
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Makes nonpolar drugs soluble in polar solvent
salt formation
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Davson and Danieli. 2 layers of phospholipid
unit membrane theory/lipid bilayer
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The lipid bilayer has proteins embedded in the matrix
fluid mosaic model
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Protein embedded are receptors and transporters
modified fluid mosaic
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Most common transport system but the slowest. Moves along conc. Gradient. No ATP and no carrier
passive diffusion
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Stereo-specific, competitive and saturable
carrier mediated
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Along the conc gradient. No ATP and needs carrier
facilitated diffusion
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Against the conc gradient. Needs ATP and carrier. Fastest.
active transport
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Moves via water filled pores, along the conc gradient. Used by electrolytes
convective transport
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Drug ions bind to endogenous ions to form a neutral complex
ion pair transport
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Envagenation of a cell membrane
vesicular transport
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The only significant endocytosis for drug transport
pinocytosis
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Weak acid in acidic environment
nonionized - absorbed
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Weak acid in basic environment
ionized- excreted
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Increase GET
decrease GER - decrease absorption
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Decrease GET
increase GER - increase absorption
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Same in all aspects but may differ in excipients, scoring, shape
pharmaceutical equivalent
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Same API but different dose or dosage form
pharmaceutical alternative
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Same safety and efficacy and safety. Biopharmaceutical equi. & bioequi
therapeutic equivalent
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Different API but same drug class
therapeutic alternative
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Allows exchange of nutrients between the mother and the fetus
placental barrier
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Most common endogenous amine for conjugation with organic acids
glycine
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Considered to be a minor pathway
methylation
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Majority of the drug products follows 1st order kinetics
true
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Volume of plasma cleared of the drug per unit time
clearance
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Rapidly achieves peak concetration
loading dose
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Drug concentration achieves a steady state in steps but reaches a point at which dose rate and clearance rate are equal
maintenance dose
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Main site of tubular reabsorption
proximal convoluted tubules
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Acetylsalicylic acid/aspirin, acetylcholilne, esters, amides
hydrolysis
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Prontozil, naloxon, chloramphenicol (nitro )
reduction
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Gray baby syndrom (chloramphenicol)
glucuronidation
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Benzoic acid
glycine conjugation
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Hydralazine, isoniazid, procainamide, sulfonamide
acetylation
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Fast acetylators
asians, eskimos
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Methyldopa, albuterol, terbutaline, acetaminophen, phenacetin
sulfation
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Catecholamines
methylation
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Main pathway of paracetamol
glucuronidation
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Valproic acid, ketoconazole, cimetidine, acute alcoholism, grape fruit juice, quinidine
enzyme inhibitors
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Phenytoin, phenobarbital, chronic alcoholism, st johns wort, charcoal broiled food, cigarette smoking
enzyme inducers
55
Chloramphenicol patient with a deficiency in nitro reduction
aplastic anemia