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11001 > B1W5 > Flashcards

B1W5 Flashcards

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1
Q

Measured permeability approximates transport of drugs taking into consideration only (a) through the bilayer lipid membrane.

A

(a) passive transcellular drug diffusion

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2
Q

Some prediction of drug performance in vivo can be made based on…

A

In vitro evaluation of its permeability and solubility

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3
Q

Examples of biological barriers

A

GIT, BBB

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4
Q

Cellular membranes are the (a) that drugs have to cross to reach their (b)

A

(a) barriers (b) biological targets

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5
Q

Transport route of a drug

A

Extracellular fluid (aq) -> lipid membrane (org) -> intracellular fluid (aq)

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6
Q

What properties must a drug have to effectively travel to its site of action?

A

Must be sufficiently soluble in both aqueous and lipid phases

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7
Q

The properties of some (a) are thought to resemble those of lipid bilayer membranes.

A

(a) Organic solvents

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8
Q

Distribution of drugs into (a) simulates their ability to (b)

A

(a) hydrophobic organic media (b) passively diffuse across biological membranes

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9
Q

Definition of partitioning

A

The movement of organic compounds from one liquid to another

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10
Q

If an excess of an organic compound is added to a mixture of two immiscible liquids…

A

It will partition itself between the 2 liquids so that each becomes saturated

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11
Q

Partition coefficient definition

A

The ratio of concentration of compound in organic phase to the concentration in aqueous phase at equilibrium

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12
Q

P(true) =

A

C(org)/C(aq)

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13
Q

Molecular polarity is dependent on…

A
  • The difference in electronegaitivty between atoms in a compound
  • Asymmetry of the chemical structure
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14
Q

The Hansch-Fujita parameters (pi) describe…

A

The contribution of various functional groups to the lipophilicity of a compound

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15
Q

HF hydrophobic functional groups:

A
  • Halogens
  • Aliphatic hydrocarbons
  • Aromatic hydrocarbons
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16
Q

HF Hydrophilic functional groups

A
  • Hydroxyl
  • Carboxyl
  • Amine
  • Amide
  • Ether
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17
Q

Partition coefficient of a neutral compound

Changes with pH

A

Same at any pH

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18
Q

P(apparent) = ?

A

P(true) x f(unionised)

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19
Q

If drug is only absorbed in the small intestine and not the stomach…

A

It should be taken early

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20
Q

Components of a solution

A

A solution is a mixture of at least 2 components one of which is a solute and the other is a solvent

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21
Q

Definition of a solution

A

A system in which molecules of solutes are dispersed in a solvent vehicle

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22
Q

Definition of dissolution

A

The transfer of molecules from the solid state to the liquid state

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23
Q

Solubility definition

A

The maximum amount of a chemical substance that passed in solution at the equilibrium

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24
Q

Solubility dictates…

A

The rate of dissolution

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25
Subsequent addition of solid drug after solution is saturated is called...
Supersatured
26
Nature of solubility
A concentration
27
Steps to solubility
Remove a drug molecule from a crystal/solid particle -> create a hole in the solvent -> Insert the drug molecule in the solvent -> Create interaction between solvent and solute
28
Creation of cavity requires...
Energy
29
The larger the surface area of the drug...
The larger the cavity needed and the lower the solubility
30
Solubility and melting point
The lower the melting point, the easier it is to separate molecules of drugs, the higher the solubility
31
Henderson-Hasselbach equation for weak acid (in terms of solubility)
pH - pKa = log (S-S0/S0)
32
Isoelectric point definition
The pH at which the overall charge of the molecule is 0, i.e. it is a zwitterion
33
pI =
(pKa1+pKa2)/2
34
pH < pI -> drug behaves as...
base
35
pH > pI -> drug behaves as...
Acid
36
Point at which the solubility is the lowest
pI
37
How can drugs be formulated to improve their solubility?
By formulating as salts
38
Solubility will be affected by:
* Solid state of the drug * Polymorph type * Salts and counter ions * Composition of aqueous media * pH * Ionic strength * Temperature
39
Solubility depends on...
The interactions with the solvent
40
The human body is designed to (a) and (b)
(a) Take in nutrition (b) Stop bacterial infection
41
Benefits of the oral route
* Most common and simple * Convenient & safe * MR have the potential to tailor delivery * High surface area and excellent absorptive capacity
42
Problems with the oral route
* First-pass metabolism * Irreversible * Irritating to GI tract * Variability * Hostile env't * Lag time to effective concentration
43
Advantages of the buccal and sublingual administration
* Avoids first-pass * Used for prolonged release of pain medication
44
Problems with the buccal and sublingual pathway
Taste-masking
45
(a) administration is the most demanding for formulation as it has be (b)
(a) Occular (b) sterile and isotonic
46
Nasal administration is mainly used to treat...
Rhinitis
47
Rhinitis is usually treated by? | (RofA)
Nasal administration
48
Aural administration is generally used for...
Young children with otitis media
49
Young children with otitis media is treated with...
Aural administration
50
Forms of respiratory administration
Gaseous, mist or aerosol
51
Drug particle size is critical for (a) Too big leads to (b) Too small leads to (c) | In respiratory route
(a) adequate drug deposition (b) impact in the mouth (c) exhalation of the particles
52
Devices for respiratory route
* Pressurised metered-dose inhaler * Dry powder inhaler * Nebulizer
53
Advantages of respiratory route
* Many different devices to target different parts of the lung * Very large surface area * Possibility to deliver macromolecules * Fast relief treatment for asthma
54
Disadvantages of the respiratory route
* Patient has to be trained to use inhalers * Dry powder inhalers not suitable for children/patients with decreased lung capacity * Formulation is very difficult, as certain parameters have to be met most accurately * Unwanted systemic effect possible due to swallowing of drug after wrong administration
55
Three paranteral routes
* Intravenous * Intramuscular * Subcutaneous
56
All paranteral routes can be administered as (a) or (b)
(a) Bolus (b) Infusion
57
Advantages of parenteral route
* Rapid onset * Enters general circulation without hepatic passage * Can deliver proteins and macromolecules * Can be applied to unconscious patients with swallowing problems * Many different injection sites which allow pharmacokinetics to be controlled
58
Disadvantages of parenteral route
* Infection risk * Pain * Only liquid preparations can be administered * Some injections cannot be administered when patient moves * Irreversible administration
59
Forms of topical route
* Creams * Ointments * Gels * Patches
60
Advantages of topical route
* Non-invasive * Local treatments of ailments wihtout systemic effect * Additional treatment effect by application of cream or ointment
61
Disadvantages of topical route
* not very accurate dosing * Leave an oily feeling on skin * There can be a grade of systemic absorption * Absorption depends on the site of application
62
Rectal forms
Suppository/foams/enemas
63
Advantages of the rectal route
* Well-vascularised region * Avoids first-pass * Both local and systemic delivery
64
Properties affecting the choice of RofA
* Physical characteristics of the drug * Rate at which the drug is released/absorbed * Need to bypass hepatic metabolism and achieve high concentrations at particular sites * Therapeutic use of medicine
65
Function of protein is dependent on...
* Amino acid composition and sequence * Structure * Chemical properties of amino acids * PTM
66
Clockwise CORN
Levo
67
Anticlockwise CORN
Dextro
68
Left terminus
N
69
Right terminus
C
70
Why is the actual C-N bond length for peptide bond different and why is rotation restricted?
The C-N bond behaves partially like a double bond due to resonance stabilisation.
71
Nearly all amino acids prefer to be in (a) to avoid (b)
(a) trans conformation (b) steric constraint
72
(a) can go into both cis and trans but prefers (b)
(a) Proline (b) cis
73
Polarity of amino acids
7 are polar and 8 are non-polar
74
Charges of amino acids
2 are acidic and 3 are basic
75
Classification of amino acid side chains
* Aliphatic and non-polar * Basic and hydrophilic * Acidic and hydrophilic * Aromatic * Hydrophilic but neutral
76
Chirality in aliphatic side chains
* Gly has no chiral site * Ile has two chiral sites * the others have one
77
Side chain with highest pKa
Arg
78
Side chain fully protonated at pH 7
Lys
79
Which side chains usually have a negative charge?
Glu, Asp
80
Which side chain absorbs most in UV?
Trp
81
Aromatics are origin of protein (a) at (b) nm
(a) UV absorbance (b) 280
82
The (a) in proteins contributes to the overall (b) of a protein
(a) disulfide bridge (b) shape

11001 (8 decks)

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