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

Block 6 Drugs Flashcards

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

A

Acetylcholinesterase inhibitor

Dementia

22
Q

Galantamine

A

Acetylcholinesterase inhibitor

Dementia

23
Q

Rivastigmine

A

Acetylcholinesterase inhibitor

Dementia

24
Q

Neurotransmitter changes in Huntington’s

A

Increased dopamine

Reduced GABA

Reduced ACh

25
Q

Neurotransmitter changes in Alzheimer’s

A

Reduced ACh

26
Q

Neurotransmitter changes in Depression

A

Reduced NE

Reduced 5HT

Reduced dopamine

27
Q

Neurotransmitter changes in Schizophrenia

A

Reduce dopamine in mesocortical

Increased dopamine in mesolimbic

28
Q

Neurotransmitter changes in Anxiety

A

Increased NE

Reduced 5HT

Reduced GABA

29
Q

Neurotransmitter changes in Parkinson’s

A

Reduced dopamine

Increased 5HT

Increased ACh

30
Q

Haloperidol

A

Dopamine receptor antagonist

31
Q

Phenytoin

A

Increase Na+ channel inactivation

1st line for tonic-clonic Rx

1st line for status epilepticus prevention

32
Q

Cabamazepine

A

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
Q

Lamotrigine

A

Blocks voltage gated Na+ channels

Anti-convulsant

34
Q

Gabapentin

A

Designed as GABA analogue BUT action primarily inhibits high-voltage gated Ca2+ channels

Anti-convulsant

35
Q

Topiramate

A

Blocks Na+ channels

Increases GABA action

Anti-convulsant

36
Q

Phenobarbitol (Barbituates)

A

Increases GABAA action by increasing Cl- channel opening time -> reduce neuronal firing

Anti-convulsant

SE: tiredness, forgetfulness, confusion

37
Q

Ethosuximide

A

Blocks T-type thalamic Ca2+ channels at the presynaptic neurons (reduce Ca2+ entry)

Rx for generalised absence seizures

38
Q

Sodium valproate (Valproic acid)

A

Increased Na+ channel inactivation (weaker than phenytoin & carbamazepine)

Ca2+ channel blocker

Increases GABA concentration (unknown mechanism)

39
Q

Benzodiazepines

A

DIAZEPAM or LORAZEPAM

Increase GABAA action by increasing Cl- channel opening frequency

Anti-convulsant

SE: rapid tolerance

40
Q

Vigabatrin

A

Irreversibly inhibits GABA transaminase -> increases GABA concentration

Synthetic structural analogue of GABA

41
Q

Tiagabine

A

GAT1 (GABA transporter) inhibitor -> inhibits GABA reuptake -> increase extracellular GABA concentration

42
Q

Mechanism of Action of Antiepileptic Drugs

A
  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
Q

Usage for Anti-psychotics (Neuroleptics)

A

Treatment of psychosis and symptoms of schizophrenia

44
Q

Typical antipsychotic drugs

A

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
Q

Dopamine Receptors in the Brain

A
  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
Q

Atypical antipsychotic drugs

A

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
Q

Selective Serotonin Reuptake Inhibitors (SSRIs)

A

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
Q

Tricyclic Anti-depressants (TCAs)

A

Amitriptyline, imipramine

ALL TCAs end in ~IPRAMINE OR ~TRIPTYLINE

SEs ->
Tri-Cs: Convulsions, Coma, Cardiotoxicity

49
Q

Carbapenems

A

A class of beta-lactam antibiotics that render them highly resistant to beta-lactamases

Broad spectrum

Good for meningitis

~PENEMS

50
Q

Aminoglycosides

A

Effective against only certain types of bacteria

Narrow spectrum

~MYCIN, ~MICIN

STREPTOMYCIN, GENTAMICIN

Not suitable for meningitis

51
Q

Atypical Antidepressants

A

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
Q

Long Term Effects of Antidepressants

A
  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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