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Foundations > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

what causes a parallel right shift in the response curve with no depression?

A

reversible competitive antagomism

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2
Q

what do nuclear receptors do?

A

regulate gene transcription

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3
Q

which drugs can act as agonists at the acetylcholine receptors (nAchRs) ?

A

acetylcholine
nicotine
varenicline

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4
Q

which kind of receptor is involved in signal amplification?

A

G protein coupled receptor

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5
Q

what is occupying alpha binding site when there is no signalling?

A

GDP

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6
Q

what hydrolyses GTP to GDP + Pi when turning signal off?

A

alpha subunit

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7
Q

what does alpha 1 do?

A

blood vessel vasoconstriction

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8
Q

what does alpha 2 do?

A

presynaptic inhibition of noradrenaline in CNS
GI tract relaxation
Decrease in persistalsis

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9
Q

what does beta 3 do?

A

thermogenesis in skeletal muscle
lipolysis

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10
Q

what does beta 1 do?

A

inc. heart rate & cardiac muscle contraction
tachycardic response

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11
Q

what does beta 2 do?

A

bronchodilation
inc. heart rate & cardiac muscle contraction (lesser extent than Beta 1)

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12
Q

what can activate cyclic AMP (cAMP) second messenger pathway?

A

G-protein coupled receptors

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13
Q

state the selectivity & extent of agonist of nicotine, varenicline & acetylcholine

A

nicotine: full agonist, selective
varenicline: partial agonist, selective
acetylcholine: full agonist, non-selective

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14
Q

greater pKi means greater or lesser affinity for receptor?

A

greater

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15
Q

lower KA means greater or lesser affinity for receptor?

A

greater

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16
Q

what does the Hill-Langmuir equation model?

A

relationship between ligand concentration and receptor occupancy

17
Q

what is EC50?

A

concentration of agonist that elicits half maximal effect

18
Q

what does non-competitive agonism do to the sigmoidal curve?

A

depresses the slope & maximum response curve
no right shift

19
Q

what is pKa?

A

pH at which 50% of the drug is ionised and 50% is unionised

20
Q

what is bioavailability (F)?

A

how available to exert effect, the amount of drug that eventually reaches systemic circulation

21
Q

what is the bioavailability calculation?

A

quantity of drug reaching systemic circulation (AUC) / Quantity of drug administered (dose)

22
Q

what can clearance be broken down into?

A

renal (CLR)
hepatic (CLH)
other elimination routes (CLO)
total clearance (CLT)

23
Q

how do you calculate clearance? (CL)

A

rate of drug elimination/ [drug] plasma

24
Q

what is first order kinetics?

A

initially, the rate of drug elimination increases as drug plasma increases (follows Michaelis-Menten kinetics)

25
Q

what is zero order kinetics?

A

when elimination rate (RE) reaches Vmax
when elimination mechanisms become more saturated and reach Vmax
e.g. with ethanol

26
Q

what is clearance?

A

the volume of blood removed of a drug per unit of time

27
Q

what is the dosage rate calculation?

A

[drug]plasma x CL

28
Q

what is steady state?

A

when rate of drug administration (R0) = Rate of elimination (RE)

29
Q

what is the drug half-life calculation?

A

t1/2 = 0.693 x Vd / CL

30
Q

what is antagonism?

A

when the antagonist forms a covalent bond with the receptor, permanently preventing the
agonist from binding and activating the receptor

31
Q

which bonds are susceptible to hydrolysis?

A

ester
amide

32
Q

what are two drugs that can go directly into Phase II metabolism?

A

codeine
morphine

33
Q

what is phase I oxidation accomplished by?

A

cytochrome P450 enzymes
(family of microsomal haem proteins)

34
Q

what happens in nuclear receptors once hormone is bound to receptor?

A

-activated hormone-receptor complex forms within cell
-the complex binds to DNA & activated specific genes
-gene activation leads to production of key proteins

Foundations (15 decks)

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