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Principles Collated Flashcards > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Pharmacodynamics?

A

What a drug does to the body (drug and dynamics begin with d, drug first)

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2
Q

Pharmacokinetics?

A

What the body does to a drug

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3
Q

What are receptors?

A

Protein macromolecules

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4
Q

What is an agonist? What do they possess?

A

Drug that binds to a receptor to produce a cellular response
-Affinity & efficacy

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5
Q

What is affinity?

A

Strength of association between ligand and receptor

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6
Q

What is efficacy?

A

Ability of an agonist to evoke a cellular response

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7
Q

What is an antagonist?

A

Drug that blocks the actions of an agonist

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8
Q

Agonists posses affinity but lack efficacy. True or false?

A

TRUE

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9
Q

What do agonists possess?

A

Affinity NOT efficacy

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10
Q

What is competitive antagonism?

A

Binding of an agonist and antagonist occur at same time (orthosteric) site and is thus competitive

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11
Q

What does competitive antagonism cause?

A

Parallel rightward shift of agonist concentration response curve with no depression in maximal response
(Less potent but the same efficacy)

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12
Q

What is non-competitive antagonism?

A

Agonist binds to normal site and antagonist binds to separate (allosteric) site and is thus not competitive

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13
Q

When can activation occur in non-competitive antagonism?

A

CANNOT occur when antagonist is bound

however both may occupy site simultaneously without activating

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14
Q

What does non-competitive antagonism cause on a graph?

A

Depress the slope and maximum response curve BUT no rightwards shift
-LOWERs the efficacy, but potency stays the same

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15
Q

Graph of competitive and non competitive antagonism?

A
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16
Q

Absorption?

A

Process by which a drug enters the body from its site of administration

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17
Q

Distribution?

A

Process by which drug leaves circulation and enters tissues perfused by blood

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18
Q

Metabolism?

A

Process by which tissue enzymes catalyse chemical conversion of a drug to a more polar form that is more readily excreted from the body

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19
Q

Excretion?

A

Process that removes the drug from the body

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20
Q

Factors controlling drug absorption?

A
  • Solubility - must dissolve
  • Chemical stability -some drugs are destroyed by acid
  • Lipid to water partition of coefficient - Rate of diffusion increases with lipid solubility
  • Degree of ionisation - Only un-ionised forms readily diffuse across lipid bilayer
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21
Q

What does the degree of ionisation in drug absorption depend on?

A

pKa of the drug and the local pH

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22
Q

What is pKa?

A

pH at which 50% of the drug is ionized and 50% unionized

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23
Q

Henderson Hasselbalch equation?

A

pH-pKa= log (A-/AH) = acid

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24
Q

What type of substance is it if Ka is large?

A

Strong acid

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25
Q

What does henderson hasellbalch equation help you determine?

A

Determine how active a drug may be in the body

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26
Q

What is oral avilability?

A

Fraction of drug that reaches the systemic circulation after oral ingestion

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27
Q

What is systemic availability?

A

Fraction of drug that reaches the systemic circulation after absorption

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28
Q

Routes of administration of drugs?

A 
Enteral= oral, sublingual, rectal 
Parenteral= IV, Intramuscular and subcutaneous, topical
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29
Q

Volume of distribution? (Vd)

A

Volume into which a drug appears to be distributed with a concentrationWhat equal to that of plasma

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30
Q

Equation for setting up an IV?

A

Vd= dose/plasma concentration

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31
Q

What is MEC?

A

Minimum effective concentration

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32
Q

What is MTC?

A

Maximum tolerated concentration

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33
Q

What is the equation for therapeutic transfer?

A

MTC/MEC

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34
Q

What does it mean if the TR of a drug is very high?

A

The higher the TA the safer the drug

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35
Q

What is first order kinetics?

A
  • The rate of elimination of a drug is directly proportional to drug concentration
  • Half life of a drug in inversely proportional to elimination rate constant
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36
Q

How do you find the half life in first order kinetics?

A

T1/2 = 0.69/kel

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37
Q

What is clearance?

A

The volume of plasma cleared of drug in unit time

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38
Q

Equation for rate of elimination?

A

Rate of elimination = Clearance x plasma concentration

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39
Q

Equation for dosing to steady state?

A

Cpss = Maintenance dose rate/ clearance

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40
Q

When is Css reached?

A

Approx 5 half lives

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41
Q

What is a loading dose?

A

Initially higher dose of drug before stepping down to lower maintenance dose

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42
Q

Why is a loading dose used?

A

Employed to decrease time to steady state for drugs with a long half-life

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43
Q

What is a half-life?

A

Time for the conc of a drug in plasma to half

44
Q

What is half-life dependant on?

A

Vd and Cl

45
Q

What does ADME stand for?

A

Absorption
Distribution
Metabolism
Excretion

46
Q

What is ADME?

A

Factors which influence drug disposition

47
Q

What does drug metabolism do?

A

Convert drugs to more polar metabolites not readily absorbed in renal tubules, facilitating excretion

48
Q

How many phases of drug metabolism?

A

2

49
Q

Phase 1 of drug metabolism?

A
  • Oxidation, reduction and hydrolysis

- Makes a drug more polar, adds a chemically reactive group permitting conjugation

50
Q

Where does phase 1 of drug metabolism occur?

A

RHS of liver

51
Q

Phase 2 of drug metabolism occurs on the RHS of the liver. True or False?

A

FALSE

LHS

52
Q

Phase 2 of drug metabolism?

A

Conjugation

-Adds an endogenous compound increasing polarity

53
Q

3 basic processes involved in renal excretion of drugs and drugs metabolites involved?

A
  1. Glomerular filtration
  2. Active tubular secretion
  3. Passive reabsorption
54
Q

What is glomerular filtration?

A
  • Occurs freely for most drugs
  • Drugs bound to large plasma proteins exist in blood in equilibrium between unbound and protein bound forms. ONLY unbound can enter filtrate via glomerular filtration
55
Q

What is active tubular secretion?

A

Epithelial cells of proximal tube contain 2 transporter systems which actively secrete drugs to lumen of nephron

56
Q

What does an organic anion transporter handle?

A

Acidic drugs like penicillins, uric acid, frusemide, thiazides

57
Q

What does an organic cation transporter handle?

A

Handles basic drugs

-Morphine

58
Q

What is the potentially most effective mechanism of drug elimination?

A

Active tubular secretion

59
Q

What is passive reabsorption across tubular epithlium?

A

Concentration of urine favours passive reabsorption of drugs across distal tubule by diffusion

60
Q

Which factors influence reabsorption in the third step of renal excretion of drugs?

A

Lipid solubility
Polarity
Urinary flow rate
Urinary pH= alkaline (increases excretion of acids) acidic (increases excretion of bases)

61
Q

What is depolarisation?

A

The membrane potential becomes less negative (or even positive)

62
Q

What is hyperpolarisation?

A

The membrane potential becomes more negative

63
Q

Which direction does Na flow in sodium channels?

A

Inwardly

64
Q

What is the driving force in sodium channels?

A

Vm-Ena (negative driving force causes the inward movement of sodium)

65
Q

Which way does K flow in potassium channels?

A

Outwardly (when positive)

The driving force is Vm-Ek

66
Q

Ion channels responsible for action potentials in neurones?

A

Voltage activated Na channels = depolarizing

Voltage activated K channels = Hyperpolarizing

67
Q

What are voltage activated Na/K channels activated by?

A

Membrane depolarization

-Na channels rapid, K channels slight delay

68
Q

What is positive feedback (upstroke of graph)?

A

Activation of Na channels is self-reinforcing, the opening of a few channels causes further depolarization

69
Q

How is the activation of K channels self-limiting?

A

The outward movement of K causes repolarisation which turns off the stimulus (negative feedback) downstroke of graph ad undershoot due to delayed closure of K channels

70
Q

What does an absolute refractory period mean?

A

No stimulus, however strong, can elicit a second AP

71
Q

Oligodendrocytes?

A

Produce myelinated cells in CNS (Shwann cells do it in PNS)

72
Q

What do astrocytes do/look like?

A

Support homeostasis and maintain BBB

Star shaped

73
Q

What are the macrophages of the CNS?

A

Microglia

74
Q

What do microglia do?

A

Immune surveillance

75
Q

Functions of the ANS?

A
  • Carries output from the CNS to the whole of the body other than skeletal muscle
  • Regulates visceral functions that are largely involuntary
  • Subdivided into sympathetic and parasympathetic
76
Q

What is main role of sympathetic nervous system?

A

Coordinates the body’s response to stress, associated with the fight, flight or fright reactions

77
Q

What is the pre-ganglionic neurone always in sympathetic system?

A

ACh

78
Q

What is noradrenaline in the sympathetic nervous system?

A

Post-ganglionic

79
Q

Where is the outflow of sympathetic?

A

Thoraco-lumbra (T1-L2)

80
Q

What does sympathetic do to

  • HR
  • Force of contraction ?
A

Increases them both

81
Q

What does the sympathetic system decrease?

A

-Mucous production

82
Q

What relaxes in a sympathetic response?

A
  • Bronchi relax

- Skeletal muscle relaxation

83
Q

GI motility is increased in sympathetic response. True or false?

A

False

Decreased and sphincters are constricted

84
Q

What type of response does ejaculation occur in?

A

Sympathetic

85
Q

What hormone is released in sympathetic response?

A

Adrenaline from adrenal gland

86
Q

Vasoconstriction occurs in sympathetic response. True or False?

A

True

87
Q

Role of parasympathetic response?

A

Coordinates the body’s basic homeostatic functions

88
Q

What is the neuro-transmitter use in parasympathetic response?

A

ACh for both pre/post ganglionic neurones

89
Q

Which cranial nerves are parasympathetic?

A

Cranial nerves 3, 7, 9, 10

90
Q

What does parasymp do to HR?

A

Decrease it

91
Q

Exaplain what happens to bronchi, mucous production, GI motility and blood vessels in parasympathetic?

A
  • Bronchoconstriction
  • Stimulates mucous production
  • Increased GI motility
  • Relaxed sphincters
  • NO effect on blood vessels/adrenal glands
92
Q

Which response does an erection occur in?

A

Parasympathetic

93
Q

Process of neurochemical transmission?

A
  1. precursor taken up
  2. Transmitter synthesized and stored
  3. AP depolarizes
  4. Calcium influx through voltage-activated channels
  5. Calcium induced release of transmitter
  6. Receptor activation
  7. Enzyme mediated inactivation of transmitter or re-uptake of transmitter
94
Q

How sympathetic chemical transmission works?

A

AP is from the CNS

  • Travels to pre-synaptic terminal of preganglionic neurone triggering Ca2+ entry and release ACh
  • ACh opens ligand-gated ion channel in the postganglionic neurone (this causes depolarization, and generation of AP that travel to pre-synaptic terminal of the neurone, triggering Ca2+ entry and release, usually of noradrenaline
95
Q

What activates G protein coupled receptors? (adrenorecptors)

A

Noradrenaline

96
Q

Differences between sympathetic and parasympathetic chemical transmission?

A

Parasympathetic

  • ACh always the transmitter used by postganglionic neurones
  • ACh activates the G protein coupled muscarnic acetylcholine receptors in target cell membrane
97
Q

What do ligand gated ion channels consist of?

A

Separate glycoprotein subunits forming a central, ion conducting channel

98
Q

What do Ligand-gated ion channels allow?

A

Rapid change in the permeability of membrane to certain ions

They can rapidly alter membrane potential

99
Q

Types of G protein coupled muscarinic ACh receptor subtypes at parasympathetic neuroeffector junctions?

A

M1-Gq= stimulates phospholipase C= increased stomach acid secretion

M2-Gi = Inhibition of adenylyl cyclase, opening of K+ channels- decreased HR

M3- Gq = stimulates phospholipase C= Increased saliva secretion and bronchoconstriction

100
Q

Types of G protein coupled muscarinic ACh receptor subtypes at sympathetic neuroeffector junctions?

A

B1- Gs = Stimulation of adenylyl cyclase = increased HR and force

B2- Gs = Stimulation of adenylyl cyclase- relaxation of bronchial and vascular smooth muscle

A1- Gq = Stimulation of phospholipase C = Contraction of vascular smooth muscle

A2-Gi = Inhibition of adenylyl cyclase = Inhibition of NA release

101
Q

What do amphetamines do?

A 
U1 substrate 
Inibits MAO (monoamine oxidase) 
Displaces NA into cytoplasm 
NA accumulates into synaptic cleft causing increased adrenoreceptor stimulation
102
Q

What is prazozin?

A

Vasodilator used as anti-hypertensive

Selective, competitive antagonist of a1

103
Q

What is atenolol?

A

Selective, competitive antagonist of B1

Used as an anti-anginal and anti-hypertensive agent

104
Q

What is salbutamol?

A

Selective against B2

Used as a bronchodilator in asthma

105
Q

What does atropine do?

A
  • Blocks parasympathetic division of ANS

- Used to reverse bradycardia post MI and in AChE poisoning

106
Q

What is atropine?

A

Competitive antagonist of muscarinic ACh receptors , does not block nicotinic ACh recpetors

Principles Collated Flashcards (13 decks)

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