Drugs Flashcards
What major neurodegenerative disorder is L-Dopa used in? What is the MOA of L-Dopa?
Parkinson’s
L-Dopa is able to cross the BBB - then converted into dopamine by aromatic L-amino-acid decarboxylase - allows the build up of dopamine
What disorder is Apomorphine used in? What is its MOA?
Parkinson’s
It is a dopamine D2 agonist
What disorder is Rotigotine used in? What is its MOA?
Parkinson’s
Dopamine receptor agonist
What disorder is Cabergoline used in? What is its MOA?
Parkinson’s
Long-acting dopamine receptor agonist - high affinity for D2 receptors
What disorder is Selegiline used in? What is its MOA?
Parkinson’s
Monoamine Oxidase B inhibitor - stops the metabolism of dopamine and enhances its activity in the substantia nigra
What disorder is Trihexyphenidyl used in? What is its MOA?
Parkinson’s
Selective M1 muscarinic ACh receptor antagonist - partially blocks cholinergic activity in the CNS
What disorder is Orphenadrine used in? What is its MOA?
Parkinson’s
Antagonist of NMDA receptor; also a muscarinic anticholinergic receptor antagonist
What are some of the side effects of trihexyphenidyl?
Mydriasis, dryness of mucous membranes and atonic bladder/bowel
What disorder is Procyclidine used in? What is its MOA?
Parkinson’s
Central muscarinic anticholinergic receptor antagonist
What disorder is Entacapone used in? What is its MOA?
Parkinson’s
Catechol-O-methyl transferase inhibitor - used to enhance the effects of L-Dopa (increase plasma levels of L-Dopa)
What disorder is Tolcapone used in? What is its MOA?
Parkinson’s
COMT inhibitor
What disorder is Tetrabenazine used in? What is its MOA?
Huntington’s
Vesicular amine transporter - depletes serotonin, noradrenaline and dopamine and inhibits the transmission of these
What movement disorder is Haloperidol used in? What is its MOA?
Huntington’s
Antidopaminergic/antipsychotic drug - affects the D2 receptors
What disorder is Olanzapine used in? What is its MOA?
Huntington’s
antidopaminergic/antipsychotic drug - antagonises d2 and 5HT2a receptors
What movement disorder is Imipramine used in? What is its MOA?
Huntington’s
Antidepressant (TCA) - inhibits neuronal uptake of serotonin and noradrenaline
What other conditions is Imipramine used in?
Depression and pain
What movement disorder is Amitriptyline used in? What is its MOA?
Huntington’s
TCA - inhibits the uptake of serotonin and noradrenaline
What other conditions is Amitriptyline used in?
Depression
Neuropathic or cancer pain
What are the side effects of amitriptyline?
Low BP confusion convulsions dilated pupils hallucinations
What receptor/s does morphine act on?
mu-opioid receptors
also binds to and inhibits GABA inhibitory interneurones
What receptor/s does Pethidine act on?
Kappa-opiate receptors (agonist) - it inhibits the release of nociceptive neurotransmitters
What receptor/s does Fentanyl act on?
Mostly an agonist for mu-opioid receptors
Also binds to kappa and delta receptors
What is methadone commonly used for and how does it work?
Synthetic opioid that is very similar to morphine (therefore mu agonist) and is used in opioid type drug dependency (such as heroin)
What receptor/s does Pentazocine act on?
Agonist at the kappa and sigma opioid receptors
weak antagonist action at the mu receptor
What receptor/s does Sufentanil act on?
binds to μ-opioid receptors
*works like other opioids by opening calcium-dependent potassium channels
What is the other name for paracetamol?
Acetaminophen
What is the MOA of paracetamol?
Reduces the active oxidised forms of COX-2
What is the other name for aspirin?
Acetylsalicylic acid
What is the MOA for aspirin?
Inhibits the COX1 and COX2 enzymes to decrease the formation of precursors of prostaglandins and thromboxanes
What is the MOA of Ibuprofen/diclofenac/ketoprofen?
Inhibits the COX1 and COX2 enzymes to decrease the formation of precursors of prostaglandins and thromboxanes
What conditions is Rofecoxib used in? What is the MOA?
Osteoarthritis, rheumatoid arthritis and acute pain
Inhibits COX-2
How does codeine (like most opioids) act as an analgesic?
Codeine’s analgesic effects are most likely due to conversion to morphine
Opioids close N-type voltage-operated calcium channels and open calcium-dependent inwardly rectifying potassium channels = hyperpolarisation + reduced neuronal excitability.
What condition/s is Carbamazepine used in?
Grand mal and psychomotor/focal seizures (epilepsy) and trigeminal neuralgia
**NOT used in absence seizures
What is the MOA of Carbamazepine?
inhibits sustained firing by blocking use-dependent sodium channels
Acts as an analgesic due to ability to block synaptic transmission in the trigeminal nucleus
What condition/s is sodium valproate used in?
Epilepsy - absence seizures, tonic clonic seizures (grand mal) and complex partial seizures
What is the MOA of sodium valproate?
inhibits sodium channels
inhibits GABA transaminase = increase in GABA (anticonvulsant)
What condition/s is Pregabalin used in?
Neuropathic pain, epilepsy, GAD
What is the MOA of Pregabalin?
Acts on the alpha2delta subunit of Ca2+ channels - inhibits release of monoamines
What condition/s is Duloxetine used in? What is its MOA?
Used for MDD, GAD and neuropathic pain
Inhibits the reuptake of serotonin and noradrenaline
What is Lignocaine/Lidocaine used for? What is its MOA?
Local anaesthetic and cardiac depressant (antiarrhythmia)
Stabilises the neuronal membrane by inhibiting ionic flux required for initiation and conduction of impulses
What is Bupivacaine used for? What is its MOA?
Local or regional anaesthesia/anaesthetic
Blocks the generation and conduction of nerve impulses - increases the threshold for electrical activation in the nerve
What is Prilocaine used for? What is its MOA?
Local anaesthetic
acts of sodium channels on neuronal cell membranes
What is Phenytoin used for? What is its MOA?
Tonic-clonic/grand mal and complex partial seizures
Acts on sodium channels on neuronal cell membranes - limits the spread of seizure activity and reduces seizure propagation
What is Lamotrigine used for?
Epilepsy and BPD
What is the MOA of Lamotrigine?
Inhibits voltage-sensitive sodium channels
Stabilises the neuronal membranes
Modulates presynaptic NT release of glutamate and aspartate
What other channel does Lamotrigine act on?
Ca2+ channels
What is Topiramate used for?
Control of partial seizures and grand mal seizures
Can also be used for migraine prevention
What is the MOA of Topiramate?
Blocks sodium channels
Augments GABAa
Inhibits glutamate AMPA/kainate signalling