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Physical Pharmacy (Lecture) > Complexation (Module 8) > Flashcards

Complexation (Module 8) Flashcards

1
Q

Characterizes the covalent and noncovalent interactions between two or more compounds that are capable of independent existence

A

Complexation

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2
Q

What happens to the physical and chemical properties of the complexing species once complexation occurs?

A

The properties are altered or changed.

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3
Q

Products of complexations (compounds formed from covalent and noncovalent interactions between two or more compounds that are capable of independent existence).

A

Complexes (coordination compounds)

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4
Q

Part of the complex that interacts with another molecule or substrate

A

Ligand

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5
Q

Forms another molecule with the ligand

A

Substrate

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6
Q

What happens during a covalent bond / interaction?

A

There is a sharing of electrons

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7
Q

List types of non covalent interactions

A

Van der Waals forces, Dipolar forces, Electrostatic forces, Hydrogen bonding, Charge transfer, Hydrophobic interactions

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8
Q

Results during a covalent interaction with a complex

A

Donor-acceptor mechanism or Lewis acid-base reaction

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9
Q

(Part of Lewis Electron Theory) molecule or ion that accepts an electron pair to form covalent bonds (electron acceptor)

A

Acid

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10
Q

(Part of Lewis Electron Theory) donates the pair of unshared electrons by which the base coordinates with an acid (electron donor)

A

Base

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11
Q

Formed from the combination of a Lewis Acid and a Lewis Base

A

Coordinate covalent bond

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12
Q

Properties that are altered in a complexing species once complexation occurs

A

Solubility, Stability, Partitioning, energy absorption and emission, conductance of the drug

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13
Q

Beneficial property of drug complexation (theophylline complexation with ethylenediamine to form aminophylline)

A

Enhanced aqueous solubility

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14
Q

Beneficial property of drug complexation (inclusion complexes of labile drugs with cyclodextrins)

A

Stability

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15
Q

Beneficial property of drug complexation (affect distribution of drug in body after systemic administration as a result of protein binding)

A

Optimization of delivery system (e.g ion-exchange resins)

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16
Q

In some instances, complexation can lead to…

A

Poor solubility (e.g tetracycline combines with calcium ions can lead to enlarging of its molecules, thus decreasing solubility)

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17
Q

Drug complexation with hydrophilic compounds also can enhance…

A

Excretion

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18
Q

How can drug molecules with hydrophilic compounds enhance excretion?

A

An increase of water solubility will lead to the body releasing enzymes that will convert the drug to a hydrophilic form -> hydrophilic drug will then be directly excreted by the kidneys

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19
Q

How can complexes alter the pharmacologic activity of the drug agent?

A

By inhibiting interactions with receptors

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20
Q

Type of complexation that is consisted of covalent interactions

A

Metal Ion Complexes (Coordination Complexes)

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21
Q

What are the classifications of Metal Ion Complexes?

A

Inorganic Type and Chelates

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22
Q

Type of complexation that is consisted of non covalent interactions

A

Organic Molecular Complexes and Inclusion/Occlusion compounds

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23
Q

What are the classifications of Organic Molecular Complexes?

A

Drug Complexes and Polymer Type

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24
Q

What are the classifications of Inclusion/Occlusion Compounds?

A

Channel lattice type, Layer type, Clathrates, Monomolecular type (Cyclodextrins)

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25
Q

Covalent interaction that is the product of a Lewis acid-base reaction (wherein neutral anions bond to a central metal atom)

A

Inorganic Type

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26
Q

Usually a non-metallic atom or ion that can donate an electron pair (lewis base)

A

Donor (ligand)

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27
Q

Constituent that accepts a share in the pair of electrons, is frequently a metallic ion, although can also be a neutral atom - electrons by which the base coordinates with an acid (lewis acid)

A

Acceptor (substrate)

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28
Q

Sample ligands

A

water, ammonia, and chloride ions

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29
Q

In K4[Fe(CN)6] , which is the ligand or lewis base?

A

CN - Cyanide

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30
Q

In K4[Fe(CN)6] , which is the acceptor or lewis acid?

A

Fe- - Iron

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31
Q

In K4[Fe(CN)6] , which neutralizes the complex compound?

A

K - Potassium

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32
Q

Number of ligands (lewis base) attached to the metal ion

A

Coordination number

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33
Q

Types of Ligands (determined from how many pairs of electrons are available for sharing)

A

Unidentate, Bidentate, and Polydentate

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34
Q

Type of ligand that has a single pair of electrons (basic group) for bonding with metal ion

A

Unidentate ligand

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35
Q

Type of ligand that has two donor sites that can share with a metal ion

A

Bidentate Ligand

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36
Q

Type of ligand that has multiple binding sites that can share with a metal ion

A

Polydentate or Multidentate Ligand

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37
Q

Compound containing a ligand (typically organic) bonded to a central metal atom at two or more points (multidentate ligand)

A

Chelate

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38
Q

Examples of naturally occurring chelates

A

Hemoglobin and Chlorophyll

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39
Q

Pharmaceutical chelates that have proven to be useful agents in the treatment of cancer

A

Cisplatin and Carboplatin (Platinum Complexes)

40
Q

The cobalt ion is situated in the center of the conjugated corrin ring structure

A

Cyanocobalamin (vitamin B12)

41
Q

Organic compounds that can assimilate and fic metallic ions and thus remove them from the body

A

Chelating agents

42
Q

What are chelating agents most especially useful for?

A

Helping in cases against poisoning and tissue damage from metals

43
Q

Good examples of chelating agents?

A

EDTA ethylenediamine tetra acetic acid and BAL, or British Anti-Lewisite

44
Q

How can chelating agents isolate and remove damage caused by metallic ions?

A

Through coordinate covalent bonds / lewis acid-base theory (chelating agents injected in the body have an open pair of electrons that the metals can bind to)

45
Q

Formed between a non covalent interaction between ligand and substrate

A

Organic Molecular Complexes

46
Q

(Example of Drug Complexes) forms insoluble complexes, making caffeine less soluble which provides caffeine in a form that masks its normal bitter taste

A

Caffeine + organic acid anions

47
Q

(Examples of Drug Complexes) insoluble complex or less soluble caffeine, masking bitter taste and converting the complex into a chewable caffeine tablet - this also provides the caffeine tablet an extended release form

A

Caffeine + gentisic acid (organic acid)

48
Q

(Examples of Drug Complexes) forms a complex that improves drug absorption and bioavailability - presence of sodium salicylate with benzocaine significantly influences the release of benzocaine

A

Benzocaine + sodium salicylate

49
Q

(Example of Polymer Type) comprised of Aerodine, Betadine

A

Povidone (polymer) + iodine = povidone - iodine

50
Q

What is Povidone (polyvinylpyrrolidone, PVD) commonly used for?

A

Used in the pharmaceutical industry as a synthetic polymer vehicle for dispersing and suspending drugs

51
Q

What does iodine do in the povidone - iodine complex?

A

An antiseptic that slows povidone’s release, thus reducing the drug’s painful effects

52
Q

Formed between interacting molecules in which guest molecules are entrapped in a host molecule through the unique molecular architecture of the host

A

Inclusion compounds or complexes

53
Q

Architecture of this type of Inclusion Compound forms channels that holds entrapped molecules

A

Channel Lattice Type

54
Q

Type of Channel Lattice Type that has crystals of complexing molecules within such channels.

A

Deoxycholic acid

55
Q

What compounds can Deoxycholic acid combine with? (e.g deoxycholic acid + camphor)

A

paraffins, organic acids, esters, ketones, and aromatic compounds

56
Q

Type of Channel Lattice type that has a channel-like structure enclosing unbranched paraffin, organic acids, alcohols, ketones

A

Urea and thiourea

57
Q

Type of Channel Lattice Type that has a channel-like complex that entraps iodine molecules within the spirals of the glucose residues

A

Starch-iodine (bluish black color indicates presence of glucose molecules)

58
Q

Architecture of this type of Inclusion Compound resembles that of stacked layers or levels

A

Layer Type

59
Q

Type of Layer Type compound complexes that entraps hydrocarbons, alcohols, and glycols between the layers of its lattices

A

Montmorillonite

60
Q

Type of Layer Type compound complexes that intercalates compounds between its lattices

A

Graphite

61
Q

Architecture of this Inclusion Compound resembles that of a cage-like lattice

A

Clathrates

62
Q

Type of Clathrate crystals that trap methanol, CO2, and HCL but not smaller and larger molecules

A

Hydroquinone

63
Q

Type of Clathrate that is a clathrate of water, isopropyl alcohol, and sodium warfarin

A

Warfarin sodium USP

64
Q

Architecture of this Inclusion compound is usually compounds of 6 molecules of glucose that forms a donut/cone shaped structure

A

Cyclodextrins (monomolecular inclusion compounds)

65
Q

Used to trap, stabilize, and solubilize sulfonamides, tetracyclines, morphine, aspirin, benzocaine, ephedrine, reserpine, and testosterone

A

Cyclodextrin (CD)

66
Q

How can Cyclodextrins effect labile complexes?

A

Cyclodextrins can help encase the fragile complexes within itself and thus make it more stable in water

67
Q

What are the three types of Cyclodextrins?

A

α-cyclodextrin (alpha), β-cyclodextrin (beta), and γ-cyclodextrin (gamma)

68
Q

What types of Cyclodextrins are most useful for pharmacy?

A

Beta and Gamma cyclodextrins because they have a bigger cavity within them (seven and eight glucose units)

69
Q

Type of Cyclodextrin that increases reactivity

A

Gamma CD + Mitomycin C and Beta CD + indomethacin

70
Q

Type of Cyclodextrin that increases aqueous solubility

A

Cyclodextrin + retinoic acid

71
Q

Type of Cyclodextrin that increases in dissolution rate of famotidine and tolbutamide

A

CD + famotidine and CD + tolbutamide

72
Q

Type of Cyclodextrin that allows efficient transport of hormone into the circulation via sublingual route

A

Amorphous derivatives of Beta CD and Gamma CD + testosterone

73
Q

Type of Cyclodextrin that produce a sustained release effect

A

Water-soluble diltiazem (calcium channel blocker) and isosorbide dinitrate + ethylated Beta CD

74
Q

Type of Cyclodextrin that suppresses bitter taste in oral liquid suspensions

A

Femoxetine complex + Beta CD

75
Q

Plays an important role in the pharmacokinetic and pharmacodynamics of a drug

A

Drug-protein binding

76
Q

The binding of drugs can influence their actions in many ways, such as:

A

Facilitate the distribution of the drug throughout the body, inactivate the drug by decreasing free drug available for protein binding, retard the excretion of the drug

77
Q

What happens to highly protein-bound drugs once they enter the system?

A

They tend to remain mainly in the systemic circulation and have a relatively low volume of distribution as opposed to binding with adipose tissue

78
Q

Which between bound drugs or unbound drugs have a pharmacological effect?

A

The unbound drugs

79
Q

What does protein binding do to the biological half-life in the body?

A

It lengthens it

80
Q

What size of molecules can proteins interact with?

A

Small molecules as a result of H-bonding between donor and acceptor functional group in amino acid sequence

81
Q

Proteins interact with small molecules

A

H-bonding

82
Q

Occur between charge amino acids with oppositely charge ligand molecules

A

Electrostatic interactions

83
Q

Dipole-dipole, dipole induced dipole, dispersion forces

A

Van der Waals interactions

84
Q

Interfacial phenomenon that results of attraction between nonpolar (hydrophobic) groups with water molecules

A

Hydrophobic interaction

85
Q

Serves as an osmotic agent for the regulation of pressure differences between intracellular and extracellular fluids. It also has the ability to bind to many different types of molecules

A

Albumin

86
Q

Preferably binds with basic drugs

A

Alpha-acid glycoprotein

87
Q

Primarily responsible for the binding and transport of plasma lipids, where basic lipophilic drugs bind

A

Lipoproteins

88
Q

(Quiz) Included in the formulation of chewable caffeine tablets that is combines with caffeine to mask its bitter taste?

A

Gentisic acid

89
Q

(Quiz) Drugs that are NOT bound to proteins in the blood are…?

A

Active

90
Q

Phenobarbital is a drug that is weakly acidic, into which protein in the blood will it predominantly combine?

A

Albumin

91
Q

(Quiz) Drug that prevents ulcer that has insolubility problems, but when complexed with cyclodextrin, its solubility is enhances

A

Famotidine

92
Q

(Quiz) Has cage-like structures

A

Clathrates

93
Q

(Quiz) What inclusion compound is the starch-iodine complex classified?

A

Channel Lattice Type

94
Q

(Quiz) Metal ion found in chlorophyll

A

Magnesium

95
Q

(Quiz) Ligands that have two donor sites

A

Bidentate

96
Q

(Quiz) Bond involved in the binding of chelating agents with metal ions

A

Covalent bonding

Physical Pharmacy (Lecture) (3 decks)

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