Pharmacology Flashcards
What class is carbamazepine
Na channel blocker
what is the indication of carbamazepine
Focal epileptic seizures
Trigeminal neuralgia
What are the side effects of carbamazepine
diplopia ataxia blood dycrasias tertogenic hyponatraemia
What drug class is phenytoin
Na channel blocker
What is the indication of phenytoin
Status epilepticus
What are the side effects of phenytoin
Gingival hyperplasia peripheral neuropathy nystagmus ataxia, sedation teratogenic enzyme inducer double vision hirsutism
what class is Lamotrigine
Na channel blocker
What is the indication of lamotrigine
Generalised and focal seizures
What are the side effects of lamotrigine
rash and steven johnson syndrome - therefore takes a long time to build up dose
NOT teratogenic
double vision
Drug class of Na valproate
Na channel blocker with increased GABA concentration
Indications of Na valproate
General epileptic seizures
Side effects of Na valproate
VALPROATE
Teratogenic Balding Fattening tremor ataxia liver dysfunction/toxicity oedema thrombocytopaenia enchephalopathy
what are the 5 mechanisms of action of analgesia
reduce inflammation at site of injury
suppressing nerve conduction
suppressing synaptic transmission
activating descending inhibitory controls
targeting ion channels upregulated (GABA) in nerve damage
what is the difference between opiates and opioids
opiates = plant based drug eg morphine opioid = any agent that acts upon opioid receptors eg morphine, endogenous substances like endorphins and enkephalins
where is periaqueductal grey found
midbrain
where is locus ceruleus found
pons
where is nucleus raphe magnus found
medulla
excitation of PAG causes profound analgesia/pain
analgesia
what substances are released from NRM
5HT and enkephalins
what substance is released from LC
NA
what happens when endogenous chemicals are released from the NRM and LC
they act on the dorsal horn of the spinal cord and inhibit nociceptive transmission
what type of receptor mediates opioid action
GPCR
what does GPCR signalling produce and what subunits are responsible
inhibition of voltage gated Ca channels to prevent release of neurotransmitter - Gi/o Bgamma subunit pre synaptically
opening of K channels to suppress excitation of post synaptic neuron - Gi/o Bgamma subunit
inhibition of adenylyl cyclase - Gi/o alpha subunit
what are the opioid receptos
mu
delta
kappa
adverse effects of opioids
addiction N+V respiratory depression postural hypotension constipation confusion, euphoria, dysphoria, hallucinations, myoclonus
what receptor do opioid agonists mostly work on
mu receptors
how is morphine metabolised
liver
methods of morphine administration
PO, SC, IM, IV, epidural, intrathecal
what is heroin
diamorphine
diamorphine has a rapid/slow onset of action when administered IV
rapid
codeine can be given IV, true or false
FALSE
only given orally
when is pethidine used
in acute pain eg labour
pethidine is suitable for chronic pain, true or false
false
it has a short duration
buprenorphine is a partial/full agonist
partial
tramadol is a weak/strong mu agonist
weak
how is tramadol administered
PO
in which neurological condition is tramadol contraindicated
epilepsy
methadone has a long/short half life making it effective as in drug withdrawal
long half life
how strong is etorphine
VERY
only used in large animals
fentanyl is used in chronic/acute pain states
chronic
pethidine should not be used in conjunction with MAO inhibitors, true or false
true
what is a neurotoxic metabolite of pethidine
norpethidine
what is naloxone
complete opioid mu receptor antagonist
how is naloxone administered
IM, IV, SC
what is naltrexone
opioid receptor antagonist
how is naltrexone administered
PO
naltrexone has a shorter half life than naloxone, true or false
false
half life of naltrexone is longer than that of naloxone
NSAIDs act centrally/peripherally
both!
what adverse effects arise from
COX 1 inhibition
COX 2 inhibition
COX 1 - Peptic ulcer disease
COX 2 - nephrotoxicity
selective COX 2 inhibitors are anti/pro thrombotic
PRO thrombotic - lead to heart disease
subtypes of ACh receptors
nicotinic
muscarinic
where are nicotinic receptors found
skeletal muscle parasympathetics sympathetics spinal cord NMJ
where are muscarinic receptors found
target organ
peripheral tissues
nicotinic receptors are ionotropic/metabotropic and are slow/fast
ionotropic
fast
muscarinic receptors are ionotropic/metabotropic and are slow/fast
metabotropic
slow
GABA a mediates
Cl-
GABA b mediates
K+
side effects of topiramate
cognitive problems
weight loss
what is the difference between nociceptive and neuropathic pain
nociceptive - response to painful stimulus with an intact nervous system
neuropathic - inappropriate response caused by dysfunctional nervous system