BLOCK 13 Flashcards
what type of drug is Paclitaxal?
a microtubule stabilisation agent (antineoplastic
what is paclitaxals moa?
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
what type of drug is cisplatin?
an anti neoplastic alkylating agent
what is cisplatins moa?
either attachment of alkyl groups to DNA bases, crosslinking DNA or inducing the nucleotide mispairing
what type of drug is isoniazid?
a bactericicdal agent
what is isoniazid target?
mycobacterium (specifically M. tuberculosis, M. bovis and M. kansasii)
what is isoniazids moa?
once activated it inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall
what type of drug is ethambutol?
a bactericidl agent
what is ethambutol effective against?
actively growing mycobacterium
what is ethambutols moa?
inhibits arabinosyl transferases which inhibits bacterial cell wall production, increasing cell wall permeability
what is pyrazinamide used to treat?
mycobacterium tuberculosis (only active at slightly acid pH)
what is pyrazinamides moa?
interfering with fatty acid synthases, disrupting the membrane potential and energy production or binding to the ribosomal protein S1
what type of drug is salbutamol?
a beta 2 adrenergic agonist
what are salbutamols 2 isomers?
the R-isomer is levalbuterol and this is responsible for bronchodilation
the S-isomer increases bronchial reactivity
what is salbutamols moa?
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_
what type of drug is salmeterol?
a beta 2 adrenergic agonist
what is salmeterols moa?
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.
what is salmeterol used for?
prevention - when used regularly it decreases the number and severity of asthma attacks but it cannot relieve an attack that has alreasy started
whats the difference in duration of action between salmeterol and salbutamol?
salmeterol lasts 12 hours whilst salbutamol lasts 4-6
whats the difference between salmeterol and formoterol?
formoterol has a faster onset of action and is more potent
what type of drug is budesonide?
an anti-inflammatory corticosteroid
why does budesonide need to be formulated as an extended release tablet?
because it undergoes significant first pass elimination so this delays its release until exposure to the small intestine
what type of drug is montelukast?
a leukotriene receptor antagonist
what is montelukast used for?
as an alternative to anti-inflammatory medications in the management of asthma and exercise induced bronchospasm
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