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PHARMACOLOGY 2 > BLOCK 13 > Flashcards

BLOCK 13 Flashcards

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1
Q

what type of drug is Paclitaxal?

A

a microtubule stabilisation agent (antineoplastic

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2
Q

what is paclitaxals moa?

A

binds to the beta subunit of tubulin causing hyperstabilization of the microtubule which prevents the cell from undergoing disassembly. This adversely affects cell function
also binds to Bcl-2 inducing apoptosis

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3
Q

what type of drug is cisplatin?

A

an anti neoplastic alkylating agent

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4
Q

what is cisplatins moa?

A

either attachment of alkyl groups to DNA bases, crosslinking DNA or inducing the nucleotide mispairing

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5
Q

what type of drug is isoniazid?

A

a bactericicdal agent

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6
Q

what is isoniazid target?

A

mycobacterium (specifically M. tuberculosis, M. bovis and M. kansasii)

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7
Q

what is isoniazids moa?

A

once activated it inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall

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8
Q

what type of drug is ethambutol?

A

a bactericidl agent

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9
Q

what is ethambutol effective against?

A

actively growing mycobacterium

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10
Q

what is ethambutols moa?

A

inhibits arabinosyl transferases which inhibits bacterial cell wall production, increasing cell wall permeability

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11
Q

what is pyrazinamide used to treat?

A

mycobacterium tuberculosis (only active at slightly acid pH)

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12
Q

what is pyrazinamides moa?

A

interfering with fatty acid synthases, disrupting the membrane potential and energy production or binding to the ribosomal protein S1

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13
Q

what type of drug is salbutamol?

A

a beta 2 adrenergic agonist

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14
Q

what are salbutamols 2 isomers?

A

the R-isomer is levalbuterol and this is responsible for bronchodilation
the S-isomer increases bronchial reactivity

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15
Q

what is salbutamols moa?

A

stimulates beta 2 adrenoreceptors leading to adenyl cyclase activation, increasig cAMP concentration and activating protein kinase A. This lowers intracellular Ca2+ concentrations causing smooth muscle relaxation
(it also inhibits the release of bronchoconstricting agents from mast cells_

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16
Q

what type of drug is salmeterol?

A

a beta 2 adrenergic agonist

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17
Q

what is salmeterols moa?

A

it binds to exosites near beta 2 adrenoreceptors in the lungs and bronchiolar smooth muscle which allows the active portion of the molecules to remain at the receptor site, continually binding and releasing.

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18
Q

what is salmeterol used for?

A

prevention - when used regularly it decreases the number and severity of asthma attacks but it cannot relieve an attack that has alreasy started

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19
Q

whats the difference in duration of action between salmeterol and salbutamol?

A

salmeterol lasts 12 hours whilst salbutamol lasts 4-6

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20
Q

whats the difference between salmeterol and formoterol?

A

formoterol has a faster onset of action and is more potent

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21
Q

what type of drug is budesonide?

A

an anti-inflammatory corticosteroid

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22
Q

why does budesonide need to be formulated as an extended release tablet?

A

because it undergoes significant first pass elimination so this delays its release until exposure to the small intestine

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23
Q

what type of drug is montelukast?

A

a leukotriene receptor antagonist

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24
Q

what is montelukast used for?

A

as an alternative to anti-inflammatory medications in the management of asthma and exercise induced bronchospasm

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25
what is montelukasts moa?
it selectively antagonizes leukotriene D4 at CysLT1 receptors, preventing airway oedema, smooth muscle contraction and enhanced secretion of thick, viscous mucus
26
what type of drug is ipratropium?
an anticholinergic agent
27
what is ipratropium used for?
as a bronchodilator in the management of cholinergic-mediated bronchospasm (associated with COPD)
28
what is ipratropiums moa?
it non-seletively inhibits muscarinic cholinergic receptors, resulting in a decrease in cGMP concentration. This causes a decrease in smooth muscle contraction
29
what type of drug is verapamil?
a class 4 anti-arrhythmia agent
30
what is verapamil moa?
in the heart it blocks L-type calcium chanells causing a reduction in ionotropy and chronotropy, reducing hR and BP
31
what type of drug is diltiazem?
a Ca2+ channel inhibitor
32
what is diltiazem used to treat?
hypertension, chronic stable angina pectoris and prinzmetals variant agina
33
what is diltiazem moa?
it inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes
34
what type of drug is atenolol?
a beta 1 selective antagonist
35
whats likely to be used instead of atenolol?
bisoprolol
36
what type of drug is atropine?
an antimuscarinic (M2) agent
37
what are the indications for atropine?
bradycardia
38
what type of drug is glyceryl trinitrate (GTN)?
a vasodilator
39
what is GTN given for?
angina pectoris or perioperative hypertension to produce controlled hypotension
40
what is glyceryl trinitrates moa?
its converted to nitric oxide which activates guanylate cyclase, stimulating the synthesis of cGMP which activates protein kinase G leading to dephosphorylation of myosin light chain causing decreased intracellular Ca2+ = smooth muscle relaxation and vasodilation
41
what type of drug is amiodarone?
``` a vaughan williams class 3 antiarrhythmic agent K+ channel blocker ```
42
what is amiodarones moa?
prolonging the myocardial cell action proteintial by blocking K+ channels duration or acting as a non-copeitiive alpha and beta adrenergic inhibitor
43
what type of drug is adenosine?
an endogenous nucleoside
44
what is adenosins moa?
actvating A1 and A2 adenosine receptors which causes inhibition of the slow inward calcium current and activation of adenylate cyclase in smooth muscle cells = relaxation
45
what is adenosine given for?
Rapid reversion to sinus rhythm of paroxysmal supraventricular tachycardias
46
what type of drug is lidocaine?
an anaesthetic agent class 1b
47
what is lidocaines moa?
blocks voltage sensitive Na+ channels during phase 0 of the cardiac action potential, slowing and depressing impulse conduction
48
what is lidocaine used to treat?
ventricular tachycarrhythmias assocated with MI
49
what class of drug is lidocaine?
a class 1 b sodium channel blocker/ anaesthetic agent
50
what is lidocaine moa?
blocks voltage sensitive Na+ channels during phase 0 of the cardiac action potential, thus slowing and depressing impulse conduction.
51
what is lidocaine used to treat
ventricular tachyarrythmias
52
what class of drug is quinidine?
class 1a antiarrthmic
53
what class of drug is procainamide?
class 1a anti arrhythmic
54
what class of drug is phenytoin (vaughan williams)?
class 1b antiarrythmic
55
what class of drug is flecainide (vaughan williams)?
class 1c antiarrythmic
56
what class of drug is propafenone (vaughan williams)?
class 1 c antiarrhytmic
57
what class of drug is verapamil (vaughan williams)?
class 4 antiarrythmic
58
what class of drug is sotalol (vaughan williams)?
class 3 antiarrythic
59
what class of drug is metoprolol (vaughan williams)?
class 2 antiarrythnic
60
what do class 1 antiarrythnics do?
block Na+ channels
61
what do class 2 antiarrythmics do?
block beta 1 receptors
62
what do class 3 antiarrythmics do?
block K+ channels
63
what do class 4 antiarrythmics do?
block Ca2+ channels

PHARMACOLOGY 2 (7 decks)

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