Drugs Flashcards
Carbidopa
decarboxylase inhibitor (with levadopa as mechanism for reduced conversion to dopamine outside BBB)
Causes nausea due to stimulation of the chemoreceptor trigger zone
Beserazide
decarboxylase inhibitor (with levadopa as mechanism for reduced peripheral dopamine conversion)
Causes nausea due to stimulation of the chemoreceptor trigger zone
Ropinirole
Dopamine agonist
Side effects: Impulse control disorders, excessive sleepiness, hallucinations
Selegeline
MOA-B inhibitor
Tolcapone
COMT inhibitor
Pramipexole
Dopamine agonist
Side effects: Impulse control disorders, excessive sleepiness, hallucinations
Amantadine
In PD, increases dopamine release and inhibits uptake
Side effects: ataxia, slurred speech, confusion, dizziness
Memantine
NMDA antagonist
Stimulate Mu Opioid Receptors
- Decreased neuronal excitability (by increasing K+ conductance) and decreased release of neurotransmitters (decreases Ca2+ influx)
Descending Inhibitory pathways
- Stimulate the periaqueductal gray
- Inhibit the substantia gelatinosa of the SC (Lamina II)
Limbic System
- Reduces the anxiety of pain.
Moderate Alzheimers (intolerant to Acetylcholinesterase Inhibitor)
Add on drug with Acetylcholinesterase Inhibitors for moderate to severe
Monotherapy in severe Alzheimers
Side effects: Constipation, nausea, respiratory, depression and sleepiness.
Tramadol
Weak Opioid via Oral administration
Acts on mu opioid receptors
Interacts with monoaminergic systems
Used for: Post-operative pain or low back pain
Side effects: Nausea, Vomiting, Sweating, Itching, Constipation
In seizures can lower seizure threshold so only used if necessary
Morphine
Strong Opioid via Oral, IV, subcutaneous administration
Used for: Post-operative pain, patient controlled analgesia, major trauma
Side effects: Sedation, respiratory depression, constipation, addiction
Methadone
Strong Opioid via Oral administration
Used for: Opioid dependence treatment, chronic pain
Side effects: Addiction, sedation, respiratory depression
Baclofen
GABA receptor Agonist
Can treat MS, Spinal cord Injuries, Cerebral Palsy
Aspirin
Irreversibly binds to COX
Warfarin
Anti-coagulant binds to factors II, VII, IX, X (mnemonic 1972)
Side effects: Haemorrhage, teratogenic (can be used in breastfeeding), skin necrosis, purple toes
Rasagaline
MOAb inhibitor
Prevent conversion of Dopamine to DOPAC (in presynaptic neurones)
Tolcapone
COMT inhibitor
Prevent degradation from DOPAC to Homovanillic acid
Tetrabanazine
Inhibits vesicular storage of dopamine by irreversibly inhibiting Vesicular Monoamine Trasnporter VMAT2
Used in Huntingtons
Amantadine
Inhibition of amine uptake, inhibition of MOA activity, release of dopamine from monoaminergic terminals
Levadopa
Dopaminergic neurones uptake Levadopa, converted by the enzyme DOPA decarboxylase to dopamine
Rotigotine
Post-Synaptic Dopamine Receptor Agonist
Non-selective between D1 and D2. Can be given as a transdermal patch
Chlorpromazine
Post-Synaptic Dopamine Receptor Antagonist
Higher affinity for D2 than D1
Used to treat schizophrenia
Side effects:
Extrapyramidal effects:
- Tardive dyskinesia, Dystonia, Parkinsonism, Bradykinesia, Tremor
Weight gain, Postural hypotension, blurred vision, Dry mouth
Haloperidol
Post-Synaptic Dopamine Receptor Antagonist
Higher affinity for D2 than D1
Used to treat schizophrenia
Clozapine
Post-Synaptic Dopamine Receptor Antagonist
Higher affinity for D2 than D1
Used to treat schizophrenia
Paracetamol
Analgesic
Anti-pyretic and analgesic
Decreases prostaglandin E2-induced reduction (reduce prostaglandins)
Inhibits reuptake of endogenous cannabinoids
Side effects: Nausea and GI bleeding
Ibuprofen
NSAID
analgesic and anti-inflammatory
Inhibits activity of COX-1 and COX-2 enzymes
Decreases prostaglandin formation and recruitment of leucocytes
Reduces sensitization
Travel across BBB to have same effect on prostaglandin synthesis in the CNS
Side effects: Long term use can lead to peptic ulcers
Diclofenac
NSAID
Inhibit the formation of prostaglandins (longer acting than ibuprofen)
Inhibiting phospholipase A2 and reductions in arachidonic acid
Side effects: higher risk of CV complications
Contraindicated in people with IHD and stroke
Amitriptyline
Tricyclic Anti-depressant
Inhibits reuptake of amines Inhibits sodium channels L-type Ca2+ channels Subtypes of K+ channels Acts on NDMA receptors
Overdose = cardiotoxicity
Side effects: Weight gain appetite changes Muscle stiffness, constipation, urinary retention, dry mouth Postural hypotension Nausea nervousness, dizziness
Pregabalin
Anticonvulsant
Binding to Alpha-2-Delta-1 subunit of N-type voltages gated Ca2+ channels
Reduction in Ca2+ entry = decreased release of neurotransmitters
Side effects:
Drowsiness, dizziness and headaches
Uncommon -
Peripheral oedema, visual problems, weight gain, confusion
Phenytoin
Anti-epileptic
Bind to the inner pore of the Na+ channel in its inactivated state, leads to an increased refractory period
T-type Ca2+ channels: require less depolarization to be activated
L-type Ca2+ channels: allow post-depolarization calcium influx and are slowly inactivated. Inhibiting these channels causes inhibition of calcium influx post-depolarization.
