Block 3 Flashcards
(36 cards)
1
Q
Dopaminergics
A
- Used in basal ganglia disorders
- Generic drug names: Levadopa (L-dopa), pramipexole, ropinirole, rotigotine, apomorphine
- Mechanisms of action: L-dopa - dopamine precursor; All others mentioned - synthetic dopamine receptor agonists
2
Q
Dopa-decarboxylase (DDC) inhibitor
A
- Used in basal ganglia disorders
- Generic Drug Names: Carbidopa, Benserazide
- Mechanisms of action: these stop the breakdown of levodopa in the periphery by inhibiting dopa-decarboxylase
3
Q
COMT (catechol-O-methyl transferase) inhibitor
A
- Used in basal ganglia disorders
- Generic drug names: entacapone, tolcapone
- Mechanism of Action: these stop the breakdown of dopamine in the CNS ny inhibition of the COMT
4
Q
MAOB (monoamine oxidase, B form) inhibitor
A
- Used to treat basal ganglia disorders
- Generic Drug Names: rasagiline, selegiline
- Mechanism of Action: This stops the breakdown of dopamine in the CNS by inhibiting MAOIb
5
Q
Anticholinergics
A
- Used to treat basal ganglia disorders
- Generic Drug Names: procyclidine, trihexphenidyl, orphenadrine
- Mechanism of action: Muscarinic cholinergic receptor antagonist
6
Q
Anti-Parkinsonism
A
- Used to treat basal ganglia disorders
- Generic drug names: Amantidine
- Mechanism of Action: dopamine agonist, glutamate (NMDA) receptor antagonist
7
Q
Dopamine-depleting drugs
A
- Antipsychotics, used to treat basal ganglia disorders
- Generic drug names: tetrabenazine
- Mechanism of Action: VMAT (vesicular monoamine transport) inhibitor, preventing the uptake of dopamine into vesicles
8
Q
Weak analgesic/ antipyretic
A
- Analgesics - used to treat pain
- Generic Drug Name: Paracetamol
- Mechanism of action: Non-selective cyclo-oxygenase (COX) inhibitor - CNS
9
Q
Non-steroidal anti-inflammatory drugs (NSAIDs)
A
- Analgesic
- Generic drug names: Ibuprofen, Diclofenac, Naproxen
- Mechanism of Action: This is a non-selective COX inhibitor
10
Q
COX2-selective NSAIDs
A
- Analgesic
- Generic Drug Name: celecoxib, etoricoxib
- Mechanism of action: selective COX-2 inhibitor
11
Q
Weak opioid analgesics
A
- Analgesic
- Generic Drug Names: Codeine, Dihydrocodeine
- Mechanism of Action: Opioid receptor agonist
12
Q
Strong opioid analgesics
A
- Analgesics
- Generic Drug Names: morphine, diamorphine, methadone (long half-life), fentanyl (short-acting)
- Mechanism of action: opioid receptor agonist
13
Q
Partial/ mixed agonist-antagonist opioid analgesics
A
- Analgesic
- Generic Drug Name: Buprenorphine
- Mechanism of Action: Opioid receptor agonist/ antagonist
14
Q
Opioid receptor antagonists
A
- Analgesic
- Generic Drug Names: Naloxone
- Mechanism of Action: Opioid receptor antagonist
15
Q
Synthetic opioid
A
- Analgesic
- Generic Drug Name: Tramadol
- Mechanism of Action: Opioid receptor agonist and serotonin/ noradrenaline reuptake inhibitor
16
Q
Drugs used in the management of opioid addiction
A
- Analgesics
- Generic Drug Names: Methadone, Buprenorphine
- Mechanism of Action: Opioid receptor agonist, buprenorphine is also an antagonist
17
Q
Drugs used to treat neuropathic pain
A
- Analgesic
- Generic Drug Names: Tricyclic antidepressants - Gabapentin (AED), Pregabalin (AED), Carbamezapine
- Mechanism of Action: Gabapentin- inhibits VDCC, and increases GABA transmission, Pregabalin- inhibits VDCC, Carbamezapine- sodium channel blocker
18
Q
IMPORTANT
Tricyclic antidepressants
A
- Used in depression
- Generic Drug Names: Amitriptyline, nortriptyline- neuropathic pain, clomipramine
- Principle mechanism of action: Inhibits reuptake of serotonin and noradrenaline in the presynaptic membrane in pain sensory pathway. Higher doses used for depression.
- Side effects: may cause sedation/ sleepiness, mania, confusion, postural hypotension, visual problems - blurred vision, cardiac dysrhythmias, toxic in overdose, drug interactions with alcohol and aspirin
19
Q
IMPORTANT
Selective Serotonin Reuptake Inhibitors
A
- Most commonly used in depression
- First line gold standard
- Generic Drug Names: sertraline, citalopram, escitalopram, fluoxetine (Prozac) which has a slow onset and suicidal ideation prior to improvement
- Mechanism of Action: Inhibits 5-HT (serotonin) reuptake pump, so more serotonin in the post-synpatic cleft.
- Takes 2-4 weeks to work
- Side effects: nausea, sleep disorders, memory loss, sexual dysfunction - erectile dysfunction and delayed ejaculation, bleeding disorders - gastric bleeding
20
Q
IMPORTANT
Monoamine oxidase inhibitors (MAOIs)
A
- Used in depression
- Generic Drug Names: Moclobemide - less toxic than TCA and other older MAOIs
- Mechanism of Action: Monoamine oxidases are intracellular neuronal liver enzymes (phase 1 reaction) which inactivate monoamines (5-HT and NA). Stop breakdown of monoamines in CNS, so availability increases. Reversible inhibitor of monoamine oxidase A (RIMA)
- Side effects: cheese reaction - when the drug reacts with tyramine in some cheeses, can cause acute attack of hypertension, convulsions, similar to TCAs, constipation
21
Q
IMPORTANT
Atypical Antidepressants
A
-Used in depression
-Generic Drug Names: Venlafaxine, Reboxetine, Bupropion, Mirtazapine
-Mechanism of Action: Venlafaxine - Serotonin/Noradrenaline Reuptake Inhibitor, Reboxetine - Noradrenaline Reuptake Inhibitor, Bupropion - Noradrenaline/ Dopamine Reuptake Inhibitor, Mirtazapine - alpha-2 adrenergic antagonist. Inhibit the reuptake of NA in the presynaptic membrane.
-Side effects:
Reboxetine - palpitations, agitation
Venlafaxine - nausea, constipation, sweating
Bupropion - nausea, vomitting
22
Q
IMPORTANT
Mood Stabilisers
A
- Used in bipolar disorder
- Generic Drug Name: Lithium
- Mechanism of action: Precisely this is unknown
- Narrow therapeutic index
- Side effects: can affect both kidney and thyroid function, so regular blood tests are needed
23
Q
1st generation antipsychotics
A
- Antipsychotics
- Generic Drug Names: Chloropramazine, Haloperidol
- Mechanism of Action: Selective dopamine (D2) receptor antagonist
24
Q
2nd generation antipsychotics
A
- Antipsychotics
- Generic Drug Names: Risperidone, Clozapine
- Mechanism of Action: Serotonin (5HT2a) and dopamine (D2) antagonist
25
Anxiolytic-hypnotics/ sedatives
- Used to treat anxiety
- Generic Drug Names: SSRI, SNRI, zolpidem (Z-drug), temazepam (benzodiazepine), dexmedetomidine
- Mechanism of Action: SSRI/SNRI - 5HT1a partial agonist, zolpidem (Z-drug) - GABA PAM, temazepam (benzodiazepine) - GABA PAM, dexmedetomidine - alpha2-adrenergic receptor agonist
26
Symptom reduction (autonomic)
- Used to treat anxiety
- Generic Drug Names: Propanolol
- Mechanism of Action: beta-adrenergic antagonist (beta-blocker)
27
Anti-epilepsy drugs (AEDs)
- Used for epilepsy
- Generic Drug Names: Valproate, Lamotrigine, Carbemazepine, Ethusuximide
- Mechanism of Action: Sodium Channel Blockers except Ethusuximide which is a T-type calcium channel blocker
28
Benzodiazepines
- Used for epilepsy
- Generic drug names: Midazolam, Lorazepam, Diazepam
- Mechanism of Action: GABA PAM (gamma- subunit)
29
Benzodiazepine antagonist
- Used for epilepsy
- Generic Drug Name: Flumazenil
- Mechanism of Action: Competitive antagonist at benzodiazepine site
30
Barbiturates
- Used to treat epilepsy
- Generic Drug Names: Phenobarbital
- Mechanism of Action: GABA PAM (beta subunit)
31
Adjuncts
- Used to treat epilepsy
- Generic Drug Names: Vigabatrin, Tiagabine
- Mechanism of Action: Vigabatrin - inhibits GABA breakdown by GABA transminase, Tiagabine - GABA reuptake inhibitor
32
IMPORTANT
Anticholinesterases - cholinesterase inhibitors
- Used for mild to moderate dementia
- Generic Drug Names: Donepezil, Galantamine, Rivastigmine
- Mechanism of Action: Inhibitor of acetylcholinesterase (reversible). Prevent the breakdown of acetylcholine which is the most affected in AD.
33
IMPORTANT
Glutamate receptor antagonist
- Used in moderate to severe depression
- Generic Drug Name: Memantine
- Mechanism of Action: Alter disease progression by interfering with glutamate mediated cell death. NMDA type of glutamate receptor is involved in plasticity and allows calcium ions into the cell to trigger plastic changes, however is calcium levels are too high, this can lead to cell death, so blocking this receptor is thought to be neuroprotective, but it has a modest effect on the progression of dementia
34
Antimicrobial drugs
- Used for CNS infection and inflammation
- Generic Drug Name: Ceftriazone, Amoxicillin
- Mechanism of Action: Ceftriazone - inhibits synthesis of cell walls in bacteria, amoxicillin - inhibits cell lysis by blocking last stages of cell wall synthesis
35
Corticosteroids
- Used for CNS infection and inflammation
- Generic Drug Names: Dexamethasone
- Mechanism of Action: Glucocorticoid receptor agonist
36
What types of drugs elicit fewer side effects?
Broad spectrum drugs elicit fewer side effects
