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MEDICINE YEAR 1 > PHARMACOLOGY > Flashcards

PHARMACOLOGY Flashcards

1
Q

what are the 4 drug targets ?

A

receptors, ion channels, enzymes, transport proteins

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2
Q

what is a drug

A

a chemical that affects physiological function in a specific way

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3
Q

what is affinity

A

the tendency of a ligand to bind to its receptor

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4
Q

what is an agonist

A

A ligand that binds to a receptor results in a biological response- evokes activation

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5
Q

what is an antagonist

A

A drug that reduces the action of another drug ( usually the agonist)

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6
Q

what is a partial agonist

A

An agonist that cannot produce as large an effect as can another agonist even with 100% receptor occupancy acting through the same receptors

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7
Q

what is efficacy

A

tendency for the agonist to activate the receptor to evoke a response

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8
Q

what is drug potency

A

conc . / amt of drug needed to produce a response

eg: EC50

explains drug activity, depends on receptor and tissue

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9
Q

what is dose

A

a specified quantity of drug administered

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10
Q

what causes adverse drug reactions?

A

High doses (leading to higher blood-plasma concentrations) can lead to the drug binding to ‘off targets’ and/or the appearance of adverse drug reactions.

This is because no drug is completely specific to a particular recpetor

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11
Q

disassociation equilibrium constan KA is

A

concentration of ligand required to occupy 50% of the receptors

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12
Q

Lower the Ka ___ the affinity for the receptor

A

Greater

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13
Q

when [A] = KA, pAR = ?

A

0.5

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14
Q

what is the Hill-Langmuir equation?

A

pAR = [A]/ KA + [A]

relationship between ligand concentration and receptor occupancy

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15
Q

what is chemical antagonism?

A

Chemical antagonism – the antagonist combines in solution directly with the chemical being antagonised

(e.g., chelating agents, used to treat lead poisoning, bind to heavy metals and form a less toxic chelate).

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16
Q

what is pharmacokinetic antagonism?

A

Pharmacokinetic antagonism – one drug reduces the effect of another drug by accelerating its metabolism or elimination

e.g., phenobarbitone increases hepatic metabolism of the anticoagulant drug warfarin)

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17
Q

what is physiological antagonism?

A

Physiological antagonism – Two agonists that produce opposing physiological actions and cancel each other out.

Each drug acts through its own receptors

(e.g., adrenaline relaxes bronchial smooth muscle reducing the bronchoconstriction of histamine)

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18
Q

what does Pindolol do?

drug

A

it is a partial agonist at beta1 and beta2 adrenoreceptors

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19
Q

what is Amitriptyline+ action, side effects

A

Tricyclic antidepressant
antagonist at : NET and SERT
side effects: sedation( H1 receptor blockade) ,dry mouth, constipation (ACh receptor blockade M1-M5)

nor-adrenaline transporter and serotonin transporter

Histamine H1 receptor and ACh M1-M5 receptor

20
Q

what is Salbutamol and what does it do? + what is it used for

A

agonist at β2 adrenoceptors (activates it)
bronchodilation,
used for asthma

21
Q

what is Propranolol

A

beta-blocker

reversible competivite antagonist at beta adreno receptors

22
Q

how long do ligand gated ion channels take to produce a cellular effect?

A

milliseconds

23
Q

how long do G-protein coupled receptors take to produce a cellular effect?

A

seconds

24
Q

how long do kinase-linked receptors take to produce a cellular effect?

A

hours

25
Q

how long do nuclear receptors take to produce a cellular effect?

A

hours

26
Q

drugs that act as agonists at nicotinic acetylcholine receptors

A

acetylcholine
nicotine
varenicline- partial agonist

27
Q

adrenoreceptors are what type of receptors?

A

G-protein coupled

28
Q

at alpha1 adrenoreceptor which Gprotein does what?

A

Gq protein

activates phospholipase C
increases IP3 and DAG, which increases CA+2 and stimulates MLCK activity

causes vasoconstriction

29
Q

in alpha2 adrenoreceptor which G-protein does what?

A

Gi protein

Inhibits adenylyl cylase
reduces cAMP, increases K+ channels, reduces Ca+2 channels

relaxation of GI tract

30
Q

in beta1 adrenoreceptor which G-protein does what?

A

Gs

stimulates adenylyl cylase (converts ATP to cAMP)
increases cAMP

Increased heart rate and cardiac muscle contraction

31
Q

in beta2 adrenoreceptor which G-protein does what?

A

Gs

stimulates adenylyl cylase (converts ATP to cAMP)
increases cAMP

bronchodilation

32
Q

in beta3 adrenoreceptor which G-protein does what?

A

Gs

stimulates adenylyl cylase (converts ATP to cAMP)
increases cAMP

thermogenesis in skeletal muscle, lipolysis

33
Q

what is theophylline?

A

Theophylline is a phosphodiesterase inhibitor
-Indicated for COPD

34
Q

what does Phosphodiesterase do to cAMP?

A

Phosphodiesterase terminates action of cAMP - makes it into AMP- which cant activate PKA to phosphorylate

35
Q

Steroid hormones are hydro____ (phillic/phobic)

A

hydrophobic/lipophilic

36
Q

what do thiazides do?

A

Thiazides are used to lower arterial blood pressure by blocking sodium

37
Q

what is hyponatremia? what hormone is released because of this?

A

hyponatremia- low levels of sodium
aldosterone is released in response to it- increases Na+ reabsorption

38
Q

the hormone aldosterone binds to what type of receptor?

A

nuclear receptors

39
Q

what type of drug is Ibuprofen

A

NSAID: non steroidal anti-inflammatory drug
cox-1,2 inhibitor

40
Q

on what enzyme does Ibuprofen act?

A

cyclo-oxygenase: cox-1,2

41
Q

how does Ibuprofen work?

A

it inhibits cox-1,2 enzymes, inhibits prostaglandins which decreases blood flow and causes vasodilation:
reduces pain and fever (pyrexia)

42
Q

t1/2 of Ibuprofen

A

1.2-2 hours in normal paitemt
3-3.4 hours of paitent with liver dysfunction

43
Q

side effects of Ibuprofen

A

irritation of GI tract, impairment of renal function

44
Q

what ion channel does amlodipine block?

A

calcium

45
Q

what is amlodipine used for?

A

angina, hypertension, reduces cardiac contractility

46
Q

what the t1/2 of amlodipine

A

40 hours, more than 50 in paitents with renal dysfunction

47
Q

what are the side effects of amlodipine?

A

not suitable for emergency, redces arterial blood pressure

MEDICINE YEAR 1 (6 decks)

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