Pharmacology Flashcards

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1
Q

what is the chemical name for aspirin?

A

acetylsalicylic acid

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2
Q

what substrate does the enzyme cyclooxygenase bind to?

A

long fatty acid chain, Arachidonic acid

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3
Q

adrenoceptors Bind to…

A

adrenaline and noradrenaline

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4
Q

True of False

most drugs bind reversibly to their receptors

A

True - ligand binding is governed by kinetics of association and dissociation.

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5
Q

what is Ec5o?

A

the effective concentration of ligand producing 50% of Emax maximal response.

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6
Q

what is potency?

A

ligand affinity + Efficacy

measure of a drug activity expresses in terms of amount required to produce an effect of a given intensity.

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7
Q

what is Efficacy?

A

how well as ligand-receptor complex causes a desired response.

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8
Q

what is radioligand binding?

A

allows quantification of ligand receptor affinity.

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9
Q

what is Bmax and Kd

A

Bmax - maximum binding capacity

Kd- dissociation constant - measure of ligand affinity

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10
Q

True or false

antagonists possess affinity and Efficacy (intrinsic Efficacy).

A

False

they possess affinity but lack intrinsic Efficacy.

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11
Q

what is the effect of presence of fixed concentration of competitive antagonists on concentration response curve?

A

rightward shift

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12
Q

what is signal transduction?

A

process by which a biological cell converts one kind of signal or stimulus into another.

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13
Q

what is a signalling scaffold?

A

the number of signalling molecules brought together in one place in the cell to communicate signalling from outside the cell to inside of the cell.

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14
Q

examples of therapeutic applications of drugs targeting GPCRs

A

depression, schizophrenia, acid reflux, nausea, hypertension, overactive bladder, asthma, chronic pain, glaucoma.

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15
Q

anti asthma drugs

A

beta adrenoceptor agonists

e.g salbutamol and salmeterol

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16
Q

analgesia/anaesthesia drugs

A

miu (u) opioid receptor agonists

e.g morphine and fentanyl

17
Q

cardiovascular drugs

A

beta adrenoceptor antagonists

e.g propranolol and atenolol

18
Q

neuroleptic drugs

A

D2 dopamine receptor antagonists

e.g Haloperidol and sulpiride

19
Q

structure of GPCRs

A

single polypeptide chain
7 TM regions
extracellular Na terminal
intracellular C terminal

20
Q

what are G proteins made up of?

A

1 alpha, 1 beta and 1 gamma subunits

21
Q

what is the enzymatic activity /action of phospholipipase C?

A

converts PIP2 (phosphatidyl inositol phosphate 2) into 》 IP3 (Inositol 1,4,5 triphosphate) + DAG (diacyl glycerol)

22
Q

stimulation of adenyl cyclamen leads to…

A

production of cyclic AMP, which leads to increased protein kinase A (PKA) activity.

Gas (G alpha s) coupled receptor
beta adrenoceptors
D1 dopamine receptors
H2 histamine receptors

23
Q

inhibition of adenylyl cyclase leads to…

A

Gai (G alpha i) coupled receptors interact with and inhibit adenylyl cyclase, therefore no ATP is produced and PKA activity is reduced.

alpha 2 adrenoceptors
D2 dopamine receptor
miu opioid receptor