Neurology/Psychiatry Drugs Flashcards
what is a dopamine precursor drug?
levodopa
what is the MoA for levodopa?
pro drug
crosses BBB and is converted to dopamine
striatal dopaminergic neurotransmission increased
what are the indications for levodopa?
PD
list some side effects of levodopa
Dyskinesia Compulsive disorders Hallucinations Nausea GI upset
what is important regarding pharmaco-kinetics/dynamics for levodopa?
Converted to dopamine in peripheries (which can cause the motor side effects)
Given with a dopamine decarboxylase inhibitor or COMT inhibitor to reduce these effects
Short half life – 50 to 90 mins
Rapidly absorbed from the proximal small intestine via the large neutral amino acid (LNAA) transport carrier system
what info should be given to patient before starting levodopa?
Dyskinesia common
Reduced efficacy over time
Avoid abrupt withdrawal
what are some dopamine agonists?
Apomorphine Pramipexole Bromocriptine Pergolide Rotigotine
what is the MoA for dopamine agonists?
Stimulate post synaptic dopamine receptors
Apomorphine: non selective D1 and D2 dopamine subfamily of receptors
Pramipexole: selective D3 receptor
what are the indications for dopamine agonists?
PD
list some side effects of dopamine agonists?
Apomorphine: pain at site of injection, nausea, vomiting
Pramipexole: hallucinations, nausea, drowsiness, involuntary movements
what is important regarding pharmaco-kinetics/dynamics for dopamine agonists?
Apomorphine: highly emetic, hence limited use. Short half life (40 mins). Needs to be via injection.
Pramipexole: Cimetidine increases its toxicity, long half life (8 hrs)
Dopamine Agonists have reduced efficacy over time
what info should be given to patient before starting a dopamine agonist?
Apomorphine can only be injected
Dopamine agonists are weaker then L-DOPA so treatment may be modified in time.
what is an example of a Catechol-o-methyl transferase Inhibitor (COMT)?
Entacapone
what are the indications for a COMT inhibitor?
Parkinson’s Disease in conjunction with L-DOPA and dopamine decarboxylase inhibitor
list the side effects of a COMT inhibitor?
Dyskinesia Nausea Abdominal pain Vomiting Dry mouth Dizziness
what is important regarding pharmaco-kinetics/dynamics for a COMT inhibitor?
Rapidly absorbed
Levodopa dose may need to be reduced by 10-30% when given with Entacapone
what info should be given to patient before starting a COMT inhibitor?
Urine may turn brown – normal
Could become lightheaded/dizzy while doing daily activities
Avoid abrupt withdrawal
give examples of an anti-epileptic drug?
Carbamazepine sodium valproate phenytoin Lamotrigrine Levetiracetam
what is the MoA for Carbamazepine?
Voltage gated Na+ channel blocker on pre-synaptic membrane
Blocks the Na+ influx; reduces neuronal excitability and decreases the action potential
what are the indications for Carbamazepine?
Epilepsy
Trigeminal Neuralgia
Neuropathic pain
list the side effects of Carbamazepine?
Dizziness Dry mouth Ataxia Fatigue Headache Diplopia Blurred vision Hyponatraemia Stevens-Johnson’s syndrome
what is important regarding pharmaco-kinetics/dynamics for Carbamazepine?
Response to the drug can be variable
Enzyme inducer of cytochrome P450; induces metabolism of itself
Interactions with other anti-convulsants
The transporter that can confer drug resistance is RALBP1
Grapefruit can significantly increase serum levels of this drug
HLA-B*1502 allele raises the risk for SJS; avoid in these patients
what info should be given to patient before starting Carbamazepine?
Avoid alcohol
Avoid grapefruit juice
what is the MoA of sodium valproate
Weak sodium ion channel blocker
Inhibitor of GABA degrading enzymes
Increased GABA stops action potential
what are the indications for sodium valproate
Epilepsy
Bipolar disorder
Depression
list the side effects of sodium valproate
Nausea Diarrhoea Gastric irritation Weight gain Hyponatraemia Behavioral disturbances Confusion Stevens-Johnson Syndrome