Topic 10 Pharma Flashcards
Intramuscular routes of administration should be used for what type of vehicle
suspensions / oily vehicles
subcutaneous routes of administration should be used for what type of vehicle
suspensions / pelletes
Buccal route of administration must be what
water / lipid soluble
how much of a drug is absorbed in 1-3 hours
75%
bases are proton
acceptors
what form of a drug can cross a cell membrane
un-ionised
Volume of plasma that accounts for total amount of drug
Volume of distribution
2 drug binding proteins
albumin
glycoproteins
how thick is a membrane
10nm
name 3 places where first pass metabolism occurs
intestines
liver
lung
Mucousal cells / pancreas secrete what that breaks down proteins?
Where are they found
digestive enzymes
intestinal lumen
the lung is the site of metabolism for what?
local hormones
what are the 3 phases of drug metabolism
oxidation/reduction/hydrolysis
conjugation
excretion
which phase of drug metabolism forms a reactive drug
oxidation/reduction/hydrolysis
in paracetamol, a conjugation reaction forms what 2 things
paracetamol glucuronide
paracetamol sulphate
oxidation of paracetamol forms what
NAPQI + Glutathione
bioavailability definition
proportion of a dose that reaches systemic circulation
what can creatinine clerance estimate
clearance of a drug filtered at glomerulus
what is the name of the esmitated creatinine clerance in ml/min
Cockcroft Gault
Cockcroft Gault equation
(140-age) x weight x constant
——————————————serum creatinine
- 23 creatinine clearance
1. 04 “
men
women
functional change to receptor upon binding of drug =
efficacy
dose of drug needed for biological effect =
potency
a non competitive antagonist binds to what
allosteric site
inactivating receptor
ligand gated ion channels (4)
glutamate
serotonin
dopamine
acetylchocline
name 3 molecules that bind to H2 receptors
histamine
acetylcholine
gastrin
what does h2 receptors activate
gastic / acid secretion
enchances cAMP
name 2 H2 receptor antagonists
what does this lead to
Ranitidine // Cimetidine
blocks H2
no cAMP
no acid
name 2 molecules that bind to receptor kinases
insulin
GF
thromboxanes are what
cytoprotective prostaglandings
aldosterone is released from what?
what does this lead to
adrenal cortex
increases water reabsorption
Decreases urine volume
increased BP
AG2 causes what
vasoconstriction
name 4 calcium channel blockers
amlodipine
diltiazem
verapamil
felodipine
calcium channel blockers bind to receptors where?
what does this cause
blocks receptors on SM
no influx of calcium
SM relaxation + low HR
Dihydropyridines Ca blocker class example (2)
what are they selective to
Amlopdipine
Felodpine
SM selective
Phenylalkylamine Ca blocker class example
what are they selective to
verapamil
selective myocardium
Benzothiazepine Ca blocker class example
What does it do
Diltiazem
Cardiac depressant + vasodilator
What do local anesthetics block?
what does this cause (2)
blocks Na+ channel
causes depression of excitation in nerve endings
inhibits conduction process in peripheral nerves
2 groups found on local anesthetics
lipid soluble hydrophobic aromatic group
charged hydrophilic amine group
local anesthetics are what
weak bases
Name 2 ester local anesthetics
cocaine
amethocaaine
ester local anesthetics are rapidly what?
what breakdown product do they form. what is this known for doing
rapidly hydrolysed
PABA = allergic reaction
Lignocaine
Bupivacaine
Prilocaine
are all types of what?
Amides local anesthetics
an adverse effect with the heart from local anesthetics is what?
myocardial depression + vasodilation
as Na+ blocked in conduction system
what can prolong the action of local anesthetics
addition of adrenaline
ED50 is what
dose that produces 50% of maximum response
Ceiling of a drug involves what?
lowest dose that produces maximal effect
Threshold of a drug involves what
dose that produces a just-noticeable effect
Agonist plus competitive antagonist graph
line will be identical but shifted right
Agonist plus irreversible antagonist graph
line shifted to bottom right
