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Advanced Pharmaceutical Discovery > Absorption > Flashcards

Absorption Flashcards

1
Q

Pharmacology consists of two processes

A

Pharmacokinetics and pharmacodynamics

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2
Q

Pharmacokinetics

A

how the body affects a specific drug after administration; BODY TO DRUG

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3
Q

Pharmacodynamics

A

How a drug affects the body system after administration; DRUG TO BODY; drug action

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4
Q

Processes of PK

A

ADME

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5
Q

Foundation to all ADME processes

A

Drug transport

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6
Q

Physicochemical determinants of drug passage

A

Membrane characteristics; drop properties

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7
Q

Mechanism of drug transport

A

passive diffusion; carrier-mediated transport; bulk flow; filtration, etc.

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8
Q

Membrane characteristics

A

Bilayer of amphipathic lipids and embedded proteins = barriers.

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9
Q

Drug properties

A

molecular weight, shape, and size; water solubility and lipid solubility; and ionization

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10
Q

Molecular weight, shape, and size

A

Small molecules - more chance of crossing membrane.

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11
Q

Lipid solubility

A

Movement directly through the lipid bilayer requires that the substance dissolve into the lipid bilayer

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12
Q

Partition coefficient (Kp)

A

solubility in lipid/solubility in water.

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13
Q

Relationship: lipid solubility and Kp

A

Increase LS, increase Kp

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14
Q

Relationship: Kp and Permeability

A

Increase Kp, increase permeability

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15
Q

Ionization: General rules

A

drugs usually exist in two forms: ionized and unionized.

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16
Q

Unionized drugs: diffusion

A

Can passively diffuse across membrane; the ratio of drug will indicate direction of passive diffusion.

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17
Q

Ionization: Factors

A

pH of hte medium; pKa of the drug.

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18
Q

Ionization: Acidic

A

Acidic drugs ionize more in basic medium; pH - pKa = log (ionized/nonionized)

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19
Q

Ionization: Basic

A

Ionize more in acidic medium; pH - pKA = log (nonionized/ionized).

20
Q

Henderson-Hasselbach Eqn

A

pH = pK + log (H+ acceptor/H+ donor).

21
Q

Mechanisms of Drug Transport: Transcellular

A

Passive diffusion, carrier-mediated transport (facilitated diffusion and active transport); ion-pair transport; endocytosis or pinocytosis.

22
Q

Mechanisms of Drug Transport: Paracellular transport

A

bulk flow; filtration

23
Q

Requirements of passive diffusion

A

drugs must be lipid soluble, unionized form, move according to a concentration gradient.

24
Q

Carrier mediated transport

A

Facilitated diffusion and active transport

25
Q

Facilitated diffusion

A

carrier needed (can be saturated), no energy required, move along concentration gradient

26
Q

Active Transport

A

carrier needed (can be saturated), energy required, move against concentration gradient.

27
Q

Bulk flow

A

move drug out of blood vessel

28
Q

Filtration

A

excrete drug

29
Q

Absorption

A

the rate and extent at which a drug leaves its site of administration; %Abs = % of first pass effect + %bioavail

30
Q

Bioavailability

A

the extent to which a drug reaches its site of action, or to a biological fluid (eg plasma) from which the drug has access to its site of action; not the same as abs.

31
Q

Factors affecting drug absorption

A

Dose, concentration, and rate of administration; dosage forms; physical and chemical properties of drugs; physiological factors; routes of drug administration.

32
Q

Dosage forms

A

Afx drug abs; depend on how well they can be dissolved (LIBERATION process)

33
Q

Factors affecting drug abs: physicochemical properties

A

acid or base; degree of ionization; molecular weight; lipid solubility or Kp

34
Q

Lipid solubility and Abs

A

Lower Kp = lower % absorbed.

35
Q

Factors affecting drugs abs: Physiological factors

A

Gastric motility; gastric emptying time; pH at the abs site; area of absorbing surface; blood flow; ingestion with or without food.

36
Q

Factors: Area of surface

A

Larger SA = more %abs.

37
Q

Oral (PO) Absorption Factors

A

dosage form, drug concentration, SA of abs, blood flow to GI, GI activity, food, bacteria in GI, first pass effect (hepatic metabolism; entero-hepatic cycle

38
Q

Parenteral administration

A

subcutaneous, intramuscular, intra-peritoneal; IV/Intra-artertial

39
Q

Parenteral administration: Subcutaneous abs

A

slow abs

40
Q

Parenteral administration: Intramuscular abs

A

fast abs

41
Q

Parenteral administration: Intraperitoneal abs

A

rapid, large abs

42
Q

Parenteral administration: IV, Intra-arterial abs

A

No abs

43
Q

Route: Pulmonary

A

Inhalation; absorbed by pulmonary epithelium and mucous membrane of respiratory tract.

Almost instaneous abs; avoids first-pass; local application

44
Q

ROA: Topical

A

Abs is proportional to SA; more rapid through burned/abraded skin; inflammation increases cutaneous BF and abs; enhanced by suspension in oily vehicle rubbing into skin

45
Q

ROA: Epicutaneous

A

local effect. no abs (frontline plus)

46
Q

Bioavailability (F)

A

Fraction of a dose that reaches the systemic circulation in a chemically unaltered form. NO UNITS (percentage or decimal).

47
Q

Incomplete Oral F

A
  1. Failure of dissolution, 2. chemical, enzymatic or bacterial attack, 3. failture of abs and pGP, 4. first pass metabolism in gut wall or liver.

Advanced Pharmaceutical Discovery (2 decks)

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