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PCOL Flashcards

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1
Q

M1

A

Gastric acid secretion, autonomic ganglia and major stim role in CNS; Gαq

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2
Q

M2

A

Slowing of heart rate; Gαi

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3
Q

M3

A

Smooth muscle contraction in gastrointestinal and respiratory tract, pupillary constriction in eye and activation of glands including stomach; Gαq

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4
Q

M4

A

(Gαi) and M5 (Gαq) (central nervous system)

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5
Q

α1

A

(vasoconstriction); Gα/q ∴ ↑PLC

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6
Q

α2

A

(inhibition of transmitter release); Gα/i ∴ ↓AC

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7
Q

β1

A

(↑ rate and force of contraction of heart); Gα/s ∴ ↑AC

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8
Q

β2

A

Relaxation of smooth muscle e.g. bronchiole); Gα/s ∴ ↑AC

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9
Q

β3

A

Relaxation of bladder smooth muscle); Gα/s ∴ ↑AC

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10
Q

Most things in sympathetic system receptors

A

Ach (nic) -> NA (a,b)

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11
Q

Sweat glands

A

Ach (nic) -> Ach (mus)

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12
Q

Adrenal Medulla

A

Ach (nic)

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13
Q

Parasympathetic receptors

A

Ach (nic) -> Ach (mus)

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14
Q

Gai

A

inhibits adenylate cyclase, reducing cAMP levels

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15
Q

Gaq

A

Activates phospholipase C (PLC)

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16
Q

Order that Noradrenaline is made In

A

Tyrosine, DOPA, Dopamine, Noradrenaline, Adrenaline

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17
Q

In vitro

A

Cells

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18
Q

In vivo

A

Whole animals

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19
Q

Order of discovery

A

High throughput screening, hit to lead, lead optimisation, candidate seeking, preclinical development

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20
Q

Down regulation

A

A decrease in the number of receptors on the cell surface due to prolonged exposure. This is longer term.

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21
Q

Tolerance

A

Reduced response to a drug after repeated use. This means more conc. is needed to get the same response. This can also lead to induction of enzymes leading to faster removal of drug.

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22
Q

Induction of enzyme

A

Increase in the number of enzymes

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23
Q

Desensitisation

A

Short-term reduction in the receptor responsiveness. It occurs rapidly and is reversible.

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24
Q

Affinity

A

The strength of binding of agonists to receptors. It is measured by the disociation constant (Ka mol/l) The higher the affinity the lower the Ka

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25
Specificity
The degree that a drug recognises a single target
26
Selectivity
Ability of an agonist to produce one effect over another
27
Partial agonist
Maximum response is not the maximum respnonse of the natural agonist
28
Intrinsic activity
Measure of agonistic activity. Full agonist= 1 partial agonist is less than this.
29
Inverse agonist
Puts the activity below the basal rate
30
Kd
This is a measure of affinity and its an equilibrium value of free vs bound drugs. K+1/ K-1
31
Hill Langumir equation
Pa= xA/ (xa+ ka) or 1/ ((kd/xa)+1) Xa= conc of ligand pa= proportion of receptors occupied.
32
Cooperativity
Measure of how much one ligand affects the binding of another ligand. Postive (slope of curve is greater than 1) and negative.
33
Response/ response max=
Xan/ (XAn+Ec50)
34
Scatchard Plot
Measure of Kd and Bmax. Bound x axis and Bound/free on Y. Kd is found by negative 1 over slope. Bmax is the x intercept
35
B max
This is a measure of the number of receptors
36
Non-polar aliphatic groups
Glycine, Alanine, Valine, Leucine, Methionine, Isoleucine
37
Glycine
Non-polar aliphatic
38
Alanine
Non-Polar aliphatic
39
Valine
Non-polar aliphatic
40
Leucine
Non-polar aliphatic
41
Methionine
Non-polar aliphatic
42
Isoleucine
Non-polar aliphatic
43
Aromatic R groups
Phenylalanine, Tyrosine, Tryptophan
44
Phenylalanine
Aromatic R Group
45
Tyrosine
Aromatic R group
46
Tryptophan
Aromatic R group
47
Polar uncharged groups
Serine, Threonine, Cysteine, Proline, Asparagine, Glutamine
48
Serine
Polar uncharged
49
Threonine
Polar uncharged
50
Cysteine
Polar uncharged
51
Proline
Polar uncharged
52
Asparagine
Polar uncharged
53
Glutamine
Polar uncharged
54
Postively charged R groups
Lysine, Arginine, Histidine
55
Lysine
Postively charged
56
Ariginine
Postively charged
57
Histidine
Postively charged
58
Negatively charged R groups
Aspartate, glutamate
59
Aspartate
Negavtively charged
60
Glutamate
Negatively charged
61
Henderson-Hasselbalch equation acidic
pH- pKa= log [A-]/[AH]
62
Henderson-Hasselbalch equation basic
pH-pka = log [B]/[BH+]
63
SLC transporters
Transport ions into the cell. (OATs and OCTS). They are secondary active transporters.
64
ABC transporters
Transport out of cells. (Pgp) Use active transport
65
Weakly acidic drug
A decrease in pH suppresses ionisation.
66
Stomach ph
2-2.5
67
Urine pH
5-8
68
Small intestine pH
7.5-8
69
Acetylcholinease substrates
Acetylcholine, Methacholine
70
Butyrylcholineastase substrates
Butyrylcholine, acetylcholine, benzylcholine, suxamethonium
71
Three resuides of Acetylcholineastase
Serine (1 alcohol), histidine (pent two nitrogens group) Glutamate (carboxyl group).
72
Ti index
= TD50/Ed50 higher means bigger theraputic window.
73
Clearance equations
Volume of blood per unit of time. Elimination rate (mg/h)= Cl total (l/h) * drug plasma (mg/l). Cl (l/h)= Dose (mg)/ (AUC (mg.h/l)
74
Steady state concentration (mg/l)
Dose rate (mg/h)/ Cl (l/h)
75
Vd equation
Dose (mg)/ C0 (mg/l)
76
IV first order elimination equation
ct= c0 * e^-kt k=cl/vd
77
AUC calculation
(t2-t1) * (c2+c1)/2
78
Phase 1 enzymes
Cytochrome P450
79
CyP3A4
Metabolises the most number of drugs and is not subject to polymorphism. Inhibited by grapefruit juice
80
Phase II metabolism
Very polar group added. UGTs (Glucuonidation) and SULTS (sulfation), Glatathuione.
81
Glomerular filtration
Removal of free drug at the glomerulus. Drugs are smaller than 40kda as they have to fit through slits.
82
Active tubular secretion
Drug from blood into Urine by tubular transport proteins. Can have competitve inhibition. Via SLC or ABC
83
Tubular reabsorption
Passive prcoess drug in urine difuses back into blood.
84
Effect of pH on tubular reabsorption
Only non ionsised drugs can leave. Acidic urine will ionise durgs so decreasing elimination, opposite for acidic drugs.
85
Phase I objectives
Pharmacokinetics, tolerability, side-effects. Done in a small number of healthy volunteers. What is a good dosage?
86
Phase I outcomes
Route of administration, freuency of dosing, Mechanism of action.
87
Phase II objectives
Does it do what it is supposed to do?, how does it affect the body, common ADRS.
88
Phase II outcomes
Confirmed efficacy, confirmed safety profile.
89
Phase III objectives
Does this drug work better than the best drug or placebo? Is it more safe?
90
Phase III outcomes
Confirmed effiacy, confirmed safety profile, is better than other drugs.
91
Single dose studies
Done in two species, informes overdose pharmacology, main source of PK data.
92
Repeat dose studies
Detect longer term effects, generally proposed clinical route, up to maximum tolerated dose.
93
Difference between single dose and repeat dose
Single dose only measures, mortality, clinical signs, body weight, food and water consumption, and necropsy.
94
Genotoxicity studies
A bacterial mutation test, a cytogenetic test, an in vivo test in rodent bone cells or a bacterial mutation test and an in vivo test with two tissues.
95
Ames test
See if the bacteria grow; if so then the drug can cause mutations and cancer. Salmonella that is histidine dependent is used. Rat liver and a histidine-deficient plate.
96
Choromosomal damage test
This uses a mouse lymphoma assay. L5178Y cells deificent in tk are used. If a mutationo occurs the cells can now metabolise triflourothymine and so DNA synthesis is interfaired with and the cell can no longer replicate
97
In vivo toxic test (Micronucleus)
Rodent given drug, harvest bone marrow, and examine for the presence of bits of DNA.
98
Staggered
Angle not near 0 H-H atoms
99
Eclipsed
Angle near 0
100
Anti
Bulky subsituants are 180
101
Gauche
Bulky subsituants are 60-90.
102

PCOL (1 decks)

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