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MEDICINE YEAR 1 > PHARMACOLOGY > Flashcards

PHARMACOLOGY Flashcards

(47 cards)

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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

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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

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A

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

21
Q

what is Propranolol

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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?

23
Q

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

24
Q

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

25
how long do nuclear receptors take to produce a cellular effect?
hours
26
drugs that act as agonists at nicotinic acetylcholine receptors
acetylcholine nicotine varenicline- partial agonist
27
adrenoreceptors are what type of receptors?
G-protein coupled
28
at alpha1 adrenoreceptor which Gprotein does what?
Gq protein activates phospholipase C increases IP3 and DAG, which increases CA+2 and stimulates MLCK activity causes vasoconstriction
29
in alpha2 adrenoreceptor which G-protein does what?
Gi protein Inhibits adenylyl cylase reduces cAMP, increases K+ channels, reduces Ca+2 channels relaxation of GI tract
30
in beta1 adrenoreceptor which G-protein does what?
Gs stimulates adenylyl cylase (converts ATP to cAMP) increases cAMP Increased heart rate and cardiac muscle contraction
31
in beta2 adrenoreceptor which G-protein does what?
Gs stimulates adenylyl cylase (converts ATP to cAMP) increases cAMP bronchodilation
32
in beta3 adrenoreceptor which G-protein does what?
Gs stimulates adenylyl cylase (converts ATP to cAMP) increases cAMP thermogenesis in skeletal muscle, lipolysis
33
what is theophylline?
Theophylline is a phosphodiesterase inhibitor -Indicated for COPD
34
what does Phosphodiesterase do to cAMP?
Phosphodiesterase terminates action of cAMP - makes it into AMP- which cant activate PKA to phosphorylate
35
Steroid hormones are hydro____ (phillic/phobic)
hydrophobic/lipophilic
36
what do thiazides do?
Thiazides are used to lower arterial blood pressure by blocking sodium
37
what is hyponatremia? what hormone is released because of this?
hyponatremia- low levels of sodium aldosterone is released in response to it- increases Na+ reabsorption
38
the hormone aldosterone binds to what type of receptor?
nuclear receptors
39
what type of drug is Ibuprofen
NSAID: non steroidal anti-inflammatory drug cox-1,2 inhibitor
40
on what enzyme does Ibuprofen act?
cyclo-oxygenase: cox-1,2
41
how does Ibuprofen work?
it inhibits cox-1,2 enzymes, inhibits prostaglandins which decreases blood flow and causes vasodilation: reduces pain and fever (pyrexia)
42
t1/2 of Ibuprofen
1.2-2 hours in normal paitemt 3-3.4 hours of paitent with liver dysfunction
43
side effects of Ibuprofen
irritation of GI tract, impairment of renal function
44
what ion channel does amlodipine block?
calcium
45
what is amlodipine used for?
angina, hypertension, reduces cardiac contractility
46
what the t1/2 of amlodipine
40 hours, more than 50 in paitents with renal dysfunction
47
what are the side effects of amlodipine?
not suitable for emergency, redces arterial blood pressure

MEDICINE YEAR 1 (6 decks)

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