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Block 6-10 Drugs, PopMed & EBM > Block 6 Drugs > Flashcards

Block 6 Drugs Flashcards

(52 cards)

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1
Q

Neuroprotective drugs

A

Target cellular disturbances that lead to brain infarct after stroke.

Dixocilpine
Dextrophan
Lubeluzole
Riluzole
Nimodipine
Lifarizine
Tirilazad
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2
Q

Dizolcilpine, Dextrophan

A

Glutamate receptor antagonist

reduce glutamate excitotoxicity on AMPA & NMDA receptors

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3
Q

Lubeluzole, Riluzole

A

Voltage gated Na+ channel blockers

reducing collapse of Na+ gradient and reducing Na+ channel prolonged opening malfunction

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4
Q

Nimodipine, Lifarizine

A

Voltage gated Ca2+ channel blockers

reduce Ca2+ overload which is overstimulated by glutamate

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5
Q

Tirilazad

A

Free radical scavenger

reduce reperfusion injury due to production of highly toxic oxygen free radicals

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6
Q

Management of Meningitis

A

First line -> 3rd gen cephalosporin

ie:

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7
Q

3rd Generation Cephalosporins

Ceftriaxone, Cefotaxime

A

A class of beta-lactam antibiotics

Broad spectrum of activity

Disrupt synthesis of peptidoglycan bacterial cell wall layer

Increased activity against Gram-negative bacteria -> menningicocci, pneumococci, some strains of E.coli, Klebsiella, H.influenzae

Ceftriaxone only recommended Rx for gonnorhoeae in US since 08/12

First line for bacterial meningitis

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8
Q

Vancomycin

A

A type of glycopeptide antibiotic

Limited spectrum of activity

Inhibits peptidoglycan cell wall synthesis in bacteria

Principally effective against Gram-positive cocci ESPECIALLY pneumococci

Used as targeted treatment if bacterial culture proves positive for highly resistant pneumococci in meningitis

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9
Q

Ampicillin

A

Beta-lactam antibiotic

Successor to amoxicillin

Irreversible binding to bacterial transpepsidase which prevents cell wall synthesis

Used against Listeria Monocytogenes for neonate (<3 month) meningitis

(Listeria is not responsive to 3rd generation cephalosporins)

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10
Q

Sumatriptan

A

5HT(1D1D) agonist

Constricts arteriolar and capillary blood vessels in migraine

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11
Q

Pizotifen

A

5HT2 antagonist

Inhibits vasoconstriction that causes cerebral hypoperfusion which triggers a migraine

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12
Q

Natalizumab

A

Binds to alpha-4 integrin on lymphocytes, inhibiting their attachment to endothelial cells and diapedesis

MS therapy

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13
Q

L-dopa

A

Can cross BBB & converted to dopamine in dopaminergic nerves (and stored)

Rx for Parkinson’s

L-dopa can also be converted in serotonergic nerves but it cannot be stored -> sudden release into synapse -> excessive involuntary movements (dyskinesia) in 50% pats.

Usually given with Carbidopa (peripheral decarboxylase inhibitor)

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14
Q

Selegiline

A

MAO-B inhibitor

Inhibits conversion of dopamine into inactive metabolites (MAO-B targets dopamine over NA & 5HT specifically)

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15
Q

Parkinson’s Disease Drugs

A 
BALSA
Bromocriptine
Amantadine
Levodopa
Selegiline
Antimuscarinics
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16
Q

Dopamine receptor agonists

A

Ergots or non-ergots (preferred)

Ergots have more SEs eg: fibrotic side effects -> valvular heart fibrosis, pulmonary fibrosis
BROMOCRIPTINE, CABERGOLINE, PERGOLIDE

Non-ergots: PRAMIPEXOLE, APOMORPHINE

ALL dopamine agonists have increased risk of sedation and impulse control disorders

Patients who commence dopamine agonists rather than L-dopa enjoy a longer period (1-2 years) before the onset of motor fluctuations, even if they subsequently commence L-dopa

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17
Q

Monoamine oxidase inhibitors

A

Inhibitors of dopamine breakdown

MAO breaks down NA, 5HT & Dopamine ->

MAO-B favours breakdown of dopamine over others -> SELEGILINE (disproved to be effective for prevention of further exacerbation) & RASAGILINE

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18
Q

Catechol-O-methyl transferase (COMT) inhibitors

A

COMT breaks down extrasynaptic dopamine and increases the amount of L-dopa reaching the brain by approximately 30%

Used with Carbidopa and Levodopa -> increased delivery over a longer period of time -> reduce period that patients spend in their switched off and dyskinectic states

ENTACAPONE

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19
Q

Amantadine

A

Non-selective NMDA receptor antagonist
May also increase dopamine release

Treatment of dyskinesias

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20
Q

Memantine

A

NMDA type glutamate receptor antagonists

Helps prevent dizziness & excitotoxicity

Used in Alzheimer’s dementia

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21
Q

Donepizil

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A

Acetylcholinesterase inhibitor

Dementia

22
Q

Galantamine

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A

Acetylcholinesterase inhibitor

Dementia

23
Q

Rivastigmine

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A

Acetylcholinesterase inhibitor

Dementia

24
Q

Neurotransmitter changes in Huntington’s

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A

Increased dopamine

Reduced GABA

Reduced ACh

25
Neurotransmitter changes in Alzheimer's
Reduced ACh
26
Neurotransmitter changes in Depression
Reduced NE Reduced 5HT Reduced dopamine
27
Neurotransmitter changes in Schizophrenia
Reduce dopamine in mesocortical Increased dopamine in mesolimbic
28
Neurotransmitter changes in Anxiety
Increased NE Reduced 5HT Reduced GABA
29
Neurotransmitter changes in Parkinson's
Reduced dopamine Increased 5HT Increased ACh
30
Haloperidol
Dopamine receptor antagonist
31
Phenytoin
Increase Na+ channel inactivation 1st line for tonic-clonic Rx 1st line for status epilepticus prevention
32
Cabamazepine
Increase Na+ channel inactivation 1st line for simple seizures 1st line for complex seizures 1st line for tonic-clonic seizures 1st line for trigeminal neuralgia
33
Lamotrigine
Blocks voltage gated Na+ channels Anti-convulsant
34
Gabapentin
Designed as GABA analogue BUT action primarily inhibits high-voltage gated Ca2+ channels Anti-convulsant
35
Topiramate
Blocks Na+ channels Increases GABA action Anti-convulsant
36
Phenobarbitol (Barbituates)
Increases GABAA action by increasing Cl- channel opening time -> reduce neuronal firing Anti-convulsant SE: tiredness, forgetfulness, confusion
37
Ethosuximide
Blocks T-type thalamic Ca2+ channels at the presynaptic neurons (reduce Ca2+ entry) Rx for generalised absence seizures
38
Sodium valproate (Valproic acid)
Increased Na+ channel inactivation (weaker than phenytoin & carbamazepine) Ca2+ channel blocker Increases GABA concentration (unknown mechanism)
39
Benzodiazepines
DIAZEPAM or LORAZEPAM Increase GABAA action by increasing Cl- channel opening frequency Anti-convulsant SE: rapid tolerance
40
Vigabatrin
Irreversibly inhibits GABA transaminase -> increases GABA concentration Synthetic structural analogue of GABA
41
Tiagabine
GAT1 (GABA transporter) inhibitor -> inhibits GABA reuptake -> increase extracellular GABA concentration
42
Mechanism of Action of Antiepileptic Drugs
1. Enhance Na+ channel inactivation -> PHENYTOIN, CARBAMAZEPINE, LAMOTRIGINE, TOPIRAMATE 2. Increase GABA action -> BENZOS, BARBITUATES 3. Inhibit excitatory amino acid release (block Ca2+ or K+) -> VALPROATE, ETHOSUXIMIDE, GABAPENTIN 4. Reduce GABA reuptake -> TIAGABINE 5. Inhibit GABA breakdown -> VIGABATRIN
43
Usage for Anti-psychotics (Neuroleptics)
Treatment of psychosis and symptoms of schizophrenia
44
Typical antipsychotic drugs
All anti-psychotic drugs are dopamine receptor 2 antagonists HALOPERIDOL + ~AZINES ie: CHLORPROMAZINE, THIORIDAZINE Reduce positive symptoms of schizophrenia but have little effect on negative symptoms SEs: movement disorders, endocrine effects
45
Dopamine Receptors in the Brain
1. D1 like receptors (D1 & D5) ACTIVATE AC -> Inc. cAMP 2. D2 like receptors (D2,D3,D4) INHIBIT AC -> reduce cAMP AUTORECEPTORS - when activated prevents further release of dopamine Role of antipsychotics -> antagonistic to D2 receptors
46
Atypical antipsychotic drugs
Second generation anti-psychotics OLANZAPINE, CLOZAPINE, QUETIAPINE, RISPERIDONE, ARIPIPRAZOLE, ZIPRASIDONE It's atypical for old closets to quietly risper from A to Z Reduce positive AND negative symptoms of schizophrenia Fewer SEs than typicals Effective in treatment resistant patients (approx. 30% of pats.)
47
Selective Serotonin Reuptake Inhibitors (SSRIs)
Fluoxetine, Paroxetine, Sertraline, Citalopram Flashbacks paralyze senior citizens Short Term: Highly selective 5-HT presynaptic reuptake blockade -> increase levels in synapse Fewer SEs than TCAs SE: CNS (confusion, anxiety) & Gastrointestinal (nausea, vomiting, anorexia)
48
Tricyclic Anti-depressants (TCAs)
Amitriptyline, imipramine ALL TCAs end in ~IPRAMINE OR ~TRIPTYLINE SEs -> Tri-Cs: Convulsions, Coma, Cardiotoxicity
49
Carbapenems
A class of beta-lactam antibiotics that render them highly resistant to beta-lactamases Broad spectrum Good for meningitis ~PENEMS
50
Aminoglycosides
Effective against only certain types of bacteria Narrow spectrum ~MYCIN, ~MICIN STREPTOMYCIN, GENTAMICIN Not suitable for meningitis
51
Atypical Antidepressants
alpha-adrenoceptor antagonist: Mirtazapine -> increases NA & 5-HT release (5-HT1 over 2 & 3) NRI: Reboxetine -> highly selective blockade of NA reuptake -> increase NA levels (no effect on histamine & mACh levels) SNRIs: Venlafaxine, Duloxetine
52
Long Term Effects of Antidepressants
1. Down-regulate post-synaptic NA &/ 5-HT2 receptors (less sensitive) 2. Increase activity/sensitivity of post-synaptic 5-HT1 receptors in hippocampus (except MAO-Is which downregulate 5-HT1) 3. Decrease activity/sensitivity of presynaptic alpha2 adrenoceptors &/ 5-HT1 receptors -> increase in monoamine release

Block 6-10 Drugs, PopMed & EBM (6 decks)

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