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M.Phil. Preparatory Flashcards > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Why is powdered drug inconvenient?

A

Flavour issue and rots over time.

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2
Q

What’s effervescent?

A

Drugs when dissolved in water form bubbles, likely due to the presence of soda, bicarbonate etc.

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3
Q

Explain the subtypes of tablets.

A

Chewable, dispersible, sublingual, enteric, sustained or extended, controlled release tablets.

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4
Q

Capsules are made of?

A

Gelatin

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5
Q

What are spansules?

A

Extended release capsules

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6
Q

Is lozenge solid or liquid dosage and whats it’s nature of administration?

A

It’s solid dosage form and tablets like, retained in mouth

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7
Q

What are pesaries?

A

Solid dosage for vagina.

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8
Q

What are suppositories?

A

Cone-like dosage insertions for female vagina and urethra. Bougies and pessaries.

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9
Q

In what dosage is the drug dissolved in water?

A

Aqueous

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10
Q

Where is the aqueous drug applied?

A

Oral, topical or parenteral

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11
Q

Which liquid drug dosage needs preservatives?

A

Aqueous dosage form to improve shelf life.

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12
Q

In this dosage a emulsifying agent is needed

A

Suspension liquid dosage form.

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13
Q

Drugs with two immiscible liquid phases are called?

A

Suspension or emulsion

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14
Q

Why use suspended dosage form when other alternatives are present?

A

Because of chemical stability, poor drug solubility in water and when solubilizing agent is not applicable and due to controllable release nature.

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15
Q

What’s an emulsion and give an example?

A

Something that has two phases which don’t dissolve. Milk is a natural emulsion.

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16
Q

What’s antitussive drug?

A

Drug for cough prevention/relief

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17
Q

What drugs deteriorate in water and are coated with sweetening agent such as syrup?

A

Elixir

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18
Q

What’s linctus?

A

A syrup containing liquid drug for throat.

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19
Q

What dosage form is suitable for children?

A

Oral drops

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20
Q

Which drug form needs to be sterilized and isotonic in nature?

A

Eye drops

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21
Q

This dosage form can be a suspension, liquid or emulsion?

A

Lotion form of liquid dosage

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22
Q

What is liniment?

A

A liquid form counter-irritant lotion.

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23
Q

Where is an injection applied?

A

Sub cutaneous, Intra muscular or intra vascular

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24
Q

Why is suspension or oil form injection not suitable for IV?

A

They cause embolism (BV blockage) only aqueous solution is injected IV.

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25
Q

What are vials and ampoules?

A

Ampoules are sealed glass whereas vials are air tight drug container.

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26
Q

Can a vial also contain powdered form drug?

A

Yes.

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27
Q

What drug is supplied in pen injector or prefilled syringes and why?

A

Insulin. Convenient to use and safe administration.

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28
Q

What’s the difference between ointment and cream?

A

Cream is 50% water whereas ointment is 80% oil

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29
Q

Why is ointment not suitable for cosmetics?

A

Ointments have an oily base which is not suitable for cosmetics.

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30
Q

These dosage forms are non oily viscous substance which swells upon interacting with water?

A

Pastes

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31
Q

This dosage form is inside collapsible tubes?

A

Gels

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32
Q

What are gels made of?

A

Gelatin, etc

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33
Q

How would you apply a powdery drug designed for gaseous administration?

A

Mixed with a suitable propellant and inhaled as aerosol.

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34
Q

What device uses HFA

A

PMDI (Pressurized metered dose inhaler)

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35
Q

What is the difference between jet nebulizer and Rota haler?

A

Nebulizer uses air to convert drug into mist for inhalation whereas rotahaler uses the person’s own air flow to convert powdered drug into aerosol.

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36
Q

How does aerosol particle size effects it’s progress through the respiratory tract?

A

Smaller particle size goes up to the bronchioles whereas larger particle settle down anywhere in the RT.

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37
Q

What’s parenteral?

A

Administration of drug into the body other than the GIT tract or intestines.

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38
Q

Does local drug route also includes intra arterial and deep tissue? But why?

A

Yes, these applications have a localized effect and minimal systemic absorption or not at all.

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39
Q

What’s indomethacin and how’s it administrated?

A

It’s a suppository drug used for rheumatoid arthritis. Administrated via rectal route.

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40
Q

Name the Local routes.

A

O-GREEN-BUS-AI

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41
Q

What is enema?

A

Liquid form drug administration into the rectum.

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42
Q

What are the two types of enema?

A

Retention and evacuant enema

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43
Q

What does enteral mean?

A

Related to the intestinal pathway

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44
Q

What’s the most common route of drug administration?

A

Oral

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45
Q

What’s the main difference between systemic and local drug routes

A

Local drug routes have effect at the site of action with minimal systemic side effects whereas systemic routes involve the circulation and the effect might be more extensive then the latter.

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46
Q

Oral route is present in both systemic and local, what’s the main difference then?

A

Type of drugs used, Such as suspension in local oral route and vice-versa.

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47
Q

What are the enteral routes?

A

OSR

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48
Q

What are the parenteral routes?

A

I-I-T

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49
Q

Why is inhalation a parenteral route?

A

It does not involve the GIT tract but respiratory tract.

50
Q

Which drug route has both systemic and local effect?

A

Rectal (suppository and enema)

51
Q

What’s the difference between dermal and subcutaneous drug routes?

A

Dermal is beneath the skin epidermis whereas subcutaneous injected in the fat layer.

52
Q

What are the 6 injectable routes

A

IIIIIS

53
Q

What’s intra-articular

A

Joint injection

54
Q

What’s the route of choice in emergency?

A

IV

55
Q

What’s the sub arachnoid space and what route is administered for it?

A

Intrathecal route, space between brain layers

56
Q

Is transdermal patch a local route?

A

No, the medication in the patch gets absorbed by the skin and produces it’s effect systematically.

57
Q

What is ocusert and progestasert?

A

Former is used as counteraceptive and releases progesterone for birth control whereas the latter is used by glaucoma patient (eyelid).

58
Q

What’s the use of liposomes and monoclonal antibodies in drug delivery?

A

Liposome encapsulates the drug whereas antibodies deliver targeted drugs such as those involving anti-cancer drugs.

59
Q

What is drug eluting stunt and computerized miniature pump?

A

Stunts used in heart whereas CMP for insulin.

60
Q

What are the important steps of pharmacokinetics?

A

Absorption, distribution, metabolism, and excretion

61
Q

On what factor does filtration of drug depends?

A

Molecular size and weight

62
Q

Solid form is better absorbed then liquid form of drug?

A

No, liquid form is better absorbed.

63
Q

Do you think lipid soluble and unionized form of drugs absorb better than aqueous soluble drugs?

A

Yes, they’re permeable to the hydrophobic molecules.

64
Q

What is disintegration time?

A

Time taken by a drug to disintegrate into smaller particles.

65
Q

What’s dissolution time?

A

Time taken to dissolve in a solution.

66
Q

How does formulation affects drug bioavailability?

A

These mixtures might interfere with the absorption of the drug.

67
Q

Why is it not a good idea to give ionic drugs via the GI tract?

A

Not absorbed easily and hence needs to be given Parenterally.

68
Q

Where will weakly acidic drug and weakly basic get better absorbed?

A

Weakly acidic drug will work better at low PH whereas weakly basic at High PH solutions. Stomach and intestine respectively. They remain in unionized form, remember ionized form is not better absorbed.

69
Q

Strong acids and bases are good for drugs?

A

No, they’re not ideal because they always remain ionized at all PH.

70
Q

What is bioequivalent and bioinequivalent?

A

If two drugs have same bioavailability and the latter means two drugs with different BA.

71
Q

What drugs have 100% bioavailability?

A

Intravenously administered drugs as they are directly enter the systemic circulation.

72
Q

What is FPM?

A

First pass metabolism involves the oral route of drug administration, which is Gut-portal vein-liver-systemic circulation

73
Q

What cycling process increases the drug bioavailability inside the body?

A

Drug-liver-bile-enterocytes-liver

74
Q

What’s apparent volume of distribution

A

D = Drug in the body/drug inside the plasma

75
Q

What’s distribution of drug?

A

Exchange of drug between the body fluid compartments.

76
Q

In what condition can drug get stored inside the adipose tissue?

A

When the Fat: lean BM is very high.

77
Q

In what conditions will be Vd remain low?

A

Heavy mol wt drugs or any other factor that confines the drug to the vascular space.

78
Q

In what condition will Vd be High?

A

Uremia, over dosage, disorder, body mass, etc.

79
Q

What info does Vd gives if its 42L or 14-16L?

A

If its 42 it means it’s distributed in total body water whereas the latter would mean that it’s distributed in the ECF.

80
Q

What’s drug redistribution and what is it’s consequence?

A

Drug-Blood-Organ-Blood-Tissue(less perfused), terminates drug action.

81
Q

What is the drug nature required to cross the BBB?

A

The drug needs to be in unionized form + hydrophobic in nature.

82
Q

In what condition does the permeability of BBB increases for drugs that are not normally distributed through the plasma membrane?

A

When their is so diseases such as meningitis or encephalitis, etc.

83
Q

What type of compounds cannot cross the placental barrier?

A

High mol wt insulin etc. compounds and Quaternary compounds.

84
Q

To what type of plasma protein does acidic or basic drugs bind to?

A

Acidic binds to albumin and basic to alpha-acid glycoprotein.

85
Q

What form of the drug in blood acts as inert form/storage form.

A

When it binds to a carrier protein.

86
Q

Tightly bound drugs with blood protein have high Vd?

A

No, it’s actually low. Drug metabolism is delayed due to plasma proteins.

87
Q

What happens in diseases state to drug in blood?

A

Albumin is low and drug is in it’s free form causing toxicity.

88
Q

Can multiple proteins bind to a same site in blood protein?

A

Yes they can in fact displace each other in the process.

89
Q

What is biotransformation?

A

Drug chemical alteration.

90
Q

What are some scenarios if a drug is not inactivated in metabolism?

A

active to inactive, active to active metabolite, pro drug or inactive drug to active metabolite.

91
Q

Explain example of a prodrug

A

Levodopa crosses the BBB and gets converted into dopamine, Normally dopamine cannot cross the BBB but the prodrug does.

92
Q

What are the advantages of prodrug?

A

Bioavailability, drug delivery, taste, action extension

93
Q

Which is synthetic and non-synthetic metabolism pathway of drugs?

A

Phase 1 is non synthetic and phase 2 synthetic

94
Q

What enzyme carries the oxidation reaction in drug metabolism?

A

CYP450 isoenzymes of the Liver ER.

95
Q

What enzyme carries out 50% of drug biotransformation?

A

CYP3A4/5

96
Q

What are the reactions of phase 1 metabolism of drugs?

A

OR-HCD -polar molecules excreted directly in urine.

97
Q

Do the phase reactions of drug take place in order?

A

No, they take place randomly and some drugs can even get metabolized without these two reactions.

98
Q

What happens in phase 2 reaction?

A

It’s synthetic and a lipophilic molecule is usually conjugated with another one such as amino acids, H2SO4, and glucuronic acid etc.

99
Q

What are the two enzyme groups of drug metabolism?

A

Microsomal and non microsomal

100
Q

What drug inactivation does not involve enzyme?

A

Hoffman reaction

101
Q

Inducers of enzyme increase what?

A

Microsomal enzymes

102
Q

Non microsomal enzymes are inducible or not?

A

No they cannot be induced

103
Q

Whats the formula of drug excretion by kidney?

A

Net renal excretion = (GF+TS)-TRB

104
Q

Explain the drug dynamics of glomerulus

A

Non bind drugs pass through the big pores easily. It only depends on the protein drug affinity and blood flow

105
Q

What is the type of drug reabsorption in renal tubules?

A

Passive diffusion, PH dependent

106
Q

What’s the nature of tubular excretion?

A

Active transport based, promotes drug-protein disassociation.

107
Q

What are the two important transporters in kidney for drug excretion?

A

OAT and OCT organic acid and base antiporters respectively.

108
Q

What are the important pharmacokinetic parameters

A

Bioavailability, half life, Vd, and clearance

109
Q

What’s clearance?

A

volume of drug cleared from plasma in a unit time.

110
Q

What happens in First order kinetics?

A

Drug is cleared in a constant with constant CL per unit time, only applicable when drug does not cause saturation. Conc dependent

111
Q

What is zero order kinetics in drug metabolism?

A

Drug is cleared constantly irrespective of the concentration. CL decreases with increase in concentration.

112
Q

What is also called as capacity limiting or Michalis Menten elimination?

A

Zero order elimination of drug

113
Q

The plasma plot for drug elimination is slightly curved?

A

Because the saturation of drug causes the first order clearance to convert into zero order. Since the body can metabolize a particular amount of drug at a time any further dosing will cause drug plasma concentration to increase

114
Q

How many slopes are in the drug elimination curve

A

Two (alpha and beta)

115
Q

Which slope corresponds to elimination and half life and which one corresponds with drug distribution.

A

Beta corresponds with elimination and half life of elimination whereas alpha with the other.

116
Q

What should be done to prevent Clearance from decreasing?

A

Administer drug according to the half life of the drug in plasma, at 4-5 half life the slope will attain plateau.

117
Q

What is loading and maintenance dose?

A

Loading dose or series of dose given to attain a desired effect in a short period of time. Maintenance does is given in specific intervals according to drug half life. The former gives a declining slope whereas the latter a steady state slope.

118
Q

What is plateau principle

A

Drug is administered until it achieves a constant steady range with input = elimination

119
Q

Loading dose is not governed by?

A

CL or half life since they are not considered when applying the dose.

120
Q

On what parameter does steady state dosage depends

A

F, V, and CL

121
Q

What is the importance of TDM

A

Helps in monitoring the kinetics of a drug in plasma and thus helps in adjusting the drug dosage according to nature of patients.

122
Q

When is plasma concentration surveillance of no use?

A

When drug is of hit and run in nature, drug response is easily calculated, Drug with irreversible action

M.Phil. Preparatory Flashcards (8 decks)

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