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CHEM358 Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Pharmacokinetics refers to the changing concentrations/ amounts of a drug and its ??? in blood plasma, urine and other body tissues and fluids

A

metabolites

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2
Q

Pharmacological and toxicological actions of drugs are primarily related to the ??? concentration of drugs

A

plasma

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3
Q

therapeutic failure of a drug occurs when there is not enough drug and plasma level is LESS than or MORE than (?) the MEC (minimal effective concentration)

A

less

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4
Q

a drug becomes toxic when there is too much drug/ too frequent and the plasma concentration levels are LESS or MORE than the MTC (minimal toxicity concentration)

A

More than

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5
Q

Therapeutic window: a range of doses which optimise between ??? and toxicity, achieving the greatest therapeutic benefit without resulting in unacceptable side-effects or toxicity.

A

efficacy

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6
Q

polymorphism is the ability of a ??? to exist in more than one crystalline form. the solubility and bioavailability is different according to each form

A

solid compound

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7
Q

LIBERATION or ABSORPTION is the process of release of drug from the formulation

A

Liberation

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8
Q

ABSORPTION or DISTRIBUTION is the process of a substance entering the blood circulation

A

ABSORPTION

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9
Q

DISTRIBUTION or METABOLISM is the irreversible transformation of parent compounds into daughter metabolites

A

Metabolism

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10
Q

ELIMINATION or DISTRIBUTION is the dispersion or dissemination of substances throughout the fluids and tissues of the body

A

distribution

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11
Q

ELIMINATION or TOXICITY is the elminiation of substances from the body

A

ELimination

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12
Q

TOXICITY or LIBERATION is the potential or real toxicity of the compound

A

Toxicity

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13
Q

drug administration can be parenteral through
- intra???
- intramuscular
- subcutaneous

A

intravenous

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14
Q

TRUE or FALSE: drug administration route depends on the properties of the drug (water/ lipid solubilities, ionisations etc) and the therapeutical objectives (rapid onset or long-term administration)

A

TRUE

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15
Q
  • Self-administrated;
  • Toxicities or overdose may be
    overcome with antidotes;
    these characteristics are advantages for ORAL or SUBLINGUAL administration of drugs?
A

ORAL

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16
Q
  • Rapid absorption;
  • Convenient administration;
  • Low incident of infection;
  • Avoidance of the harsh GI environment;
  • Avoidance of first-pass metabolism;
    these characteristics are advantages for ORAL or SUBLINGUAL administration of drugs?
A

SUBLINGUAL

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17
Q
  • Complicated drug-absorption pathway;
  • Exposed to the harsh gastrointestinal (GI) environment;
  • Undergoes first-pass metabolism before entering systemic circulation;
  • Not suitable for emergencies;
    these characteristics are disadvantages for ORAL or SUBLINGUAL administration of drugs?
A

ORAL

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18
Q
  • Interferes with eating, drinking, and talking,
    unsuitable for prolonged administration.
  • Can’t be used when patient is uncooperative or unconscious.
  • Smoking causes vasoconstriction of the blood vessels. This decreases absorption of medication.
    these characteristics are disadvantages for ORAL or SUBLINGUAL administration of drugs?
A

SUBLINGUAL

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19
Q

??? Tablets are a form of oral dosage that defines a drug that is embedded in inert “carrier” meshwork extended or targeted (intestinal) release;

A

Matrix tablets

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20
Q

what type of oral dosage form has an oblong casing made from gelatin, containing drug liquid, powder or granulated form

A

capsules

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21
Q

Eudragit is an example of a ??? tablet that is targeted for release at or above pH 7 and is hence coated in a wax-like coating of highly specialised polymers to protect the actual drug

A

coated tablet

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22
Q
  • Aqueous Solutions (with Sugar=Syrup)
  • Mostly for ??? use;
  • 20 drops = 1g;
  • Alcoholic Solutions (=Tinctures)
  • Often plant extracts;
  • 40 drops = 1g;
  • Suspensions: Insoluble drug particles in aqueous or lipophilic media;
A

paediatric use

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23
Q

Topical Administration is usually used for ??? effects

A

local

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24
Q

topical administration through skin is generally slow; enhanced by increased ???, by damage to stratum corneum, or by increased blood flow

A

lipophilicity

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25
Q

??? (DMSO) will readily penetrate the skin and carry the active ingredient along with it;

A

dimethylsulfoxide

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26
Q

TOPICAL or ORAL administration: Specific formulation determined by physicians/dermatologists
-based on skin type:
* dry vs oily
* young vs old
* intact vs injured
-based on drug properties
* hydrophilic vs lipophilic
* soluble vs insoluble

A

Topical

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27
Q

advantages of parenteral drugs are:
- Can achieve up to 100% “absorption”
- Drug directly enters the systemic circulation or other ??? tissues i.e. no first pass of metabolism or harsh GI environment
- Better bioavailability of hydrophilic drugs;

A

vascular

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28
Q

Disadvantages of ??? administration include:
- irreversible
may cause pain, fear, infections

A

parenteral administration

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29
Q

what type of parenteral administration is fastest acting, followed by intramuscular and then subcutaneous

A

intravenous

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30
Q
  • Ampules
  • Single use mostly with fracture ring
  • Single and Multiple-dose Vials
  • 10-100ml; Contain preservatives;
  • Cartridge ampules
  • Infusions
  • Solution administrated over an extended period of time

these are all types of what drug administration?

A

parenteral

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31
Q

Rectal administration:
- minimises biotransformation by liver;
- prevents destruction by intestinal enzymes or low pH in stomach;
- erratic/incomplete absorption;
- suitable for persons with ??? and ???

A

nausea and vomiting.

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32
Q

Absorption: the transfer of a drug from its site of ??? to the bloodstream.

A

administration

33
Q

Drugs usually must cross at least one cell membrane from site of administration to
site of action. this occurs via
* Passive diffusion (water-soluble vs lipid soluble)
* Active transport
* Pinocytosis OR phagocytosis?

A

Pinocytosis

34
Q

TRUE or FALSE: most drugs can passively diffuse through aqueous pores

A

FALSE: most drugs CANNOT as the aqueous pores are too small

35
Q

Mechanisms for absorption of drugs includes passive diffusion through lipids, passive diffusion through aqueous pores, active transport, and ???

A

pinocytosis

36
Q

Factors influencing absorption- pH:
- many drugs are weak acids or bases, this affects the passage of an ??? drug through a membrane

A

uncharged

37
Q

pH equilibrium:
pKa = pH + log [protonated species] /[??? species]

A

non-protonated

38
Q

equilibrium of weak ???: pKa = pH + log [AH] / [A-]

A

acids

39
Q

equilibrium of weak ???: pKA = pH + log [BH+] / [B]

A

bases

40
Q

Factors influencing absorption: Blood flow to absorption site:
- Blood flow to the intestine is much GREATER or LESSER (?) than that to the stomach = absorption from the intestine is favoured over that from the stomach.

A

GREATER

41
Q

Factors influencing absorption: Total surface area available for absorption:
- SA of the intestine is about 1,000-fold of that of the ??? = absorption across the intestine is more efficient.

A

stomach

42
Q

Factors influencing absorption: Contact time at the absorption surface:
- a drug moves through GI tract very quickly (e.g. diarrhea), it is not well absorbed; the presence of food ??? the drug and slows gastric emptying = absorbed slowly.

A

dilutes

43
Q

Bioavailability: the fraction of the administrated drug that reaches the ??? circulation

A

systemic

44
Q

Factors influencing bioavailability include:
* ??? metabolism;
* Solubility of the drug;
* Chemical instability;
* Nature of the drug formulation;

A

First pass metabolism

45
Q

Amount of Drug absorbed into the systemic circulation = (S) x (F) x (D)
S: fraction of ??? drug in the formulation
F: bioavailability
D: dose - how much was administrated

A

active

46
Q

Determinants of Drug absorption from GIT:
* Dissolution
* Gastric emptying rate - affected by some drugs (e.g. metoclopramide)
* Intestinal motility – affected by drugs (Opiates, anticholinergics)
???
???
???

A
  • Disease states (e.g. gastroenteritis)
  • Drug interaction in the GI tract - food interactions (antibiotics)
  • Passage through gut wall
47
Q

Distribution: the process by which a drug REVERSIBLY or IREVERSIBLY (?) leaves the bloodstream and enters the interstitium (extracellular fluid) and/or the cells of the tissues.

A

reversibly

48
Q

distribution of drugs is affected by:
- blood flow
- capillary permeability
- binding of drugs to plasma ???

A

proteins

49
Q

Apparent Volume of Distribution: a hypothetic volume of ??? into which a drug is dispersed.

A

fluid

50
Q

Apparent Volume of Distribution:
Vd[ml or l] = Dose[mg] / Cp[mg/ml]
where Cp is the [???] after it has equilibrated in its distribution before significant fraction has been eliminated

A

drug in plasma

51
Q

Plasma compartment: a drug has a very large MW or binds exclusively to ???, is effectively trapped in plasma (vascular) compartment.
Ex: anticoagulant Heparin Vd=4L

A

plasma protein

52
Q

Extracellular fluids: a drug has a LOW or HIGH (?) MW and hydrophilic = can move through endothelia slit junction of capillaries into interstitial fluid.
Ex: antibiotic aminoglycoside Vd=14L

A

low

53
Q

drugs that act on total body water: a drug has a low MW and is HYDROPHOBIC or HYDROPHILIC. High lipid solubility
Ex: ethanol, Vd=42L

A

Hydrophobic

54
Q

TRUE or FALSE: Drugs do not penetrate uniformly throughout the body. Some tissues may behave similar and can be considered as a common compartment;

A

TRUE

55
Q

One compartment distribution kinetics:
When a drug is ??? Or ??? passive diffusion is responsible for this, drug transport is often first order; i.e. rate is proportional to concentration gradient

A

absorption or elimination

56
Q

One compartment distribution kinetics:
Cp = Cp(0) exp(-kel . t)
OR
ln Cp = ln Cp(0) - kelt
where Kel = elimination rate constant

A

yup

57
Q

One compartment distribution kinetics:
zero-order kinetics = the rate of the
process is INDEPENDENT or DEPENDANT (?) of the drug’s concentration;
Cp = Cp(0) - kelt

A

independent

58
Q

Most drugs follow first order kinetics
(only three drugs follow zero order kinetics for elimination: ethanol, high concentration of phenytoin, ???)

A

aspirin

59
Q

TRUE or FALSE:
Two Compartment Kinetics: absorption and elimination are to and from compartment 1

A

TRUE

60
Q

Binding of drugs to plasma proteins (usually albumin) is reversible and may show low or high capacity. Bound drugs are pharmacologically ACTIVE or INACTIVE (?)

A

INactive

61
Q

Albumin has the strongest affinities for anionic drugs (weak acids) or ??? drugs.

A

hydrophobic

62
Q

Clinical importance of drug displacement:
1. Warfarin (class I) is highly bound to albumin- only small fraction is free.
2. If a sulfonamide antibiotic (Class II) is administered, it displaces warfarin from albumin = rapid INCREASE or DECREASE (?) in concentration of free warfarin in plasma

A

increase

63
Q

Class I or Class II (?) drugs: Dose is less than available binding sites

A

Class I

64
Q

Class I or Class II (?): dose is greater than available binding sites

A

Class II

65
Q

Drug Metabolism- the process of transformation of lipophilic drugs into more polar, readily excretable products- happens in which organse?

A

Liver
Kidney
Intestines

66
Q

Phase I of drug metabolism: convert lipophilic molecules into POLAR or NON-POLAR (?) molecules by adding or unmasking a polar functional group, such as -OH, -SH, -NH2, -COOH etc via oxidation, reduction, and hydrolysis etc.

A

POLAR

67
Q

TRUE or FALSE: Phase I or drug metabolism may increase, decrease, or leave unaltered the drug’s pharmacological activity;

A

TRUE

68
Q

Metabolism Phase I - Oxidation
- Oxygen is incorporated into the drug molecule (e.g. hydroxylation)
- Oxidation causes loss of part of the drug molecule (e.g. oxidative ???, dealkylation)

A

deamination

69
Q

Metabolism Phase I - Oxidation
Microsomal ??? Oxidase (MFOs):
1. Flavoprotein, aka NADPH-cytochrome c reductase: Flavin mononucleotide (FMN) and Flavin adenine dinucletotide (FAD);
2. Cytochrome P450: located in most cells (primarily liver and GI tract) light absorption at 450 nm when complexed with CO; hemoprotein: an iron atom alternating between Ferrous (Fe2+) and Ferric (Fe3+) states;

A

Mixed Function

70
Q

Most common inhibition of Cytochrome P450 is through competition for the same ???
= serious adverse events.

A

isozyme

71
Q

TRUE or FALSE: Numerous drugs have shown to inhibit one or more of the CYP dependent transformation pathways of warfarin (anticoagulant). e.g. omeprazole (gastroesophageal reflux etc)

A

TRUE

72
Q

if metabolite from Phase I is sufficiently polar, drug can be excreted by kidney. Usually NOT the case and metabolites are ??? hence phase II

A

lipophilic

73
Q

Phase II of drug metabolism: a subsequent conjugation reaction with an endogenous substrate = polar, usually more water soluble compounds that are often therapeutically ACTIVE or INACTIVE?

A

inactive

74
Q

what type of phase II conjugation reaction is most important and products are often excreted in bile, requires enzyme UDP-glucuronosyltransferase?

A

glucuronidation (conjugation to α-d-glucuronic acid)

75
Q

the sole determinant of the rate that a drug reaches the steady-state is ???

A

t1/2 (half life)

76
Q

Empirical PK-Lipinski’s Rule of Five: describes molecular properties important for a drug’s pharmacokinetics in human body. However, the rule does not predict if a compound is pharmacologically ???

A

active.

77
Q

Empirical PK-Lipinski’s Rule of Five
- 5 hydrogen bond donors (N or O atoms with one or more hydrogen atoms)
- 10 hydrogen bond acceptors (N or O atoms)
- ??? 500 daltons
- An octanol-water partition coefficient log P not greater than 5

A

Molecular weight

78
Q

Pharmacogenomics: the whole genome application of pharmacogenetics, which deals with SINGLE or MULTIPLE (?) gene interactions with drugs

A

single

CHEM358 Pharmacology (11 decks)

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