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CNS Drugs > Mechanisms > Flashcards

Mechanisms Flashcards

1
Q

Opioids

A 
3 opioid receptors : mu , delta , kappa
Natural endogenous opioids are :
Enkephalins
Dynorohins
Endorphins

Endorphins act on u
Closing of voltage gated Ca channels and open K channels allowing efflux of K ions.

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2
Q

Opioids Adverse effects

A 
Nausea
Vomiting
Anti tussive
Respiratory depression
Immune Suppression
Constipation
Flushing (meperidine morphine)
Itching
Urinary retention
Dependence
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3
Q

Buprenorphine

A

Partial agonist of u rec
Antagonist of k and d rec

Produces partial effect thus less risk of abuse

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4
Q

Naloxone

A

Opioid antagonist

Morphine antidote

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5
Q

Anesthesia stages

A
  1. Induction
  2. Excitement
  3. Surgical Anesthesia
  4. Medullary paralysis
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6
Q

1st group Anesthesia

A

Etomidate
Propofol
Barbiturates

Unconsciousness more then analgesia
Act on GABA a
Hyperpolarization of resting potential . Open Cl channels, suppress neuronal excitability .

Used in Induction phase.

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7
Q

1st group Anesthesia Adverse effects

A

Etomidate
Renal suppression
Transient Skeletal muscle movements (myoclonus)

Propofol
Respiratory depression
Hypotension

Barbiturates
Bronchospasm
Respiratory depression

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8
Q

2nd group Anesthesia mech

A

Ketamine (IV)
Nitrous Oxide
Xenon
Cyclopropane

No effect on GABA
More Analgesia than unconsciousness

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9
Q

Ketamin

A

Act on N-methyl D aspartate rec NMDA

Inhibits NDMA receptors. Inhibit glutamate excitatory action

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10
Q

Xenon

Cyclopropane

A

Selectively inhibit NMDA

2 pore domain K channels . Efflux of K ions

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11
Q

2nd group adverse effects

A 
Ketamine:
Htn
tachy
Hypersalivation
Hallucinations
Delrium

Nitrous oxide , cyclopropane

Dizziness nausea vomit

Xenon: none

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12
Q

3rd group

A 
Halothane
Enflurane
Isoflurane
Sevoflurane
Desflurane

Act on all
GABA a, NMDA & 2 pore domain K channels and many other

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13
Q

3rd group side effects

A

Dose dependant hypotension
Low cardiac output
Arrhythmia hepatotoxicity (halothane)
Renal toxicity ( Sevoflurane)

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14
Q

Dexmedotomidine

A

Unique Anesthetic

Presynaptic a2 adrenergic rec

Brady
Hypotension

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15
Q

Local anesthetics mechanism

A

Bind to a site on voltage gated Na Channels prevention of Na Influx .

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16
Q

Local anesthetics adverse effects

A 
Systemic effects: 
Blurry vision
Light headedness
Seizure
Cardiac arrhythmia
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17
Q

Alzheimer’s drugs mechanisms

A

Anti cholinesterases

Rivastigmine ( both Acetyl and butyl cholinesterase)
Donapezil
Galantamine
Tacrine

Inhibit cholinesterase enzyme and promotes prolonged action of Ach

NMDA rec antagonist
Memantine

Abnormal B -amyloid accumulation may cause high levels of glutamate by inhibiting it’s uptake and triggering more release from glial cells.
Memantine binds to NMDA receptors and block excitatory action of glutamate by blocking Ca influx

18
Q

Side effects Alzheimer’s

A

Anti cholinesterase
SLUD
Brady
Weight loss

Memantine
Insomnia
Diarrhea
Headache

19
Q

Parkinson’s mechanism

A

Parkinson’s develops when neurons connecting substantia Niagra to striatum degenerate

Dopaminergic neurons originate in substantia niagra

Low dopamine causes more GABA & more Ach

Increase inhibition in thalamus and reduced excitatory input to motor cortex

20
Q

Parkinson’s drugs mechanisms

Pre BBB crossing

A

Tyrosine –th–> L-Dopa –AADC–> DOPAMINE
DOPAMINE released
Broken by MAO-B and COMPT

Levodopa (precursor of Dopamine) (BBB crossing)
Carbidopa (inhibits Dopamine Decarboxylase)
Entacapone (inhibits COMPT)

21
Q

Parkinson’s drugs mechanisms

Post BBB

A

Selegeline
Rasagiline

Inhibit MAO-B

Tolcapone: inhibits COMT

22
Q

Parkinson’s drug mechanism

Anti Muscarinic Agents

A

Benztropine
Biperidine
Procyclidine
Trihexphenidyl

23
Q

Parkinson’s drugs

Dopamine mimics

A 
Bromocriptin
Ropinorole
Pramipexole
Rotigotine
Apomorphine

Stimulate dopamine receptors to produce similar effects as dopamine

24
Q

Amantadine Parkinson’s

A

Facilitates pre synaptic dopamine release

Blocks Glutamate NMDA rec

25
Q

Parkinson’s drug Adverse effects

A 
Levo carbi
Nausea loss of appetite
Hypotension
Mental disturbance
Discolored urine
Selegeline rasagiline
Nausea
Insomnia
Dyskinesia
Hallucinations

Entacapone tolcapone
Diarrhea (tolcapone severe)
Hepatotoxic (tolca)
Discolored urine

Dopamine mimics
Nausea
Hypo
Daytime sleepiness
Mental disturbance
Bromocriptin (cardiac and pulmonary fibrosis)

Anticholinergic
Dry mouth
Constipation
Blurred vision

26
Q

Seizures classification

A 
Focal seizure (one hemisphere) 
May or may not be unconscious

Generalize
Both hemisphere
Always unconscious

27
Q

Why seizures happen?

A

Too much Glutamate can cause abnormal influx of Na ions (AMPA rec) & Ca ions (NMDA rec) . GABA a opens Cl channels and influx of Cl ions can neutralize it. But if Little or no GABA. Seizures.

28
Q

Epilepsy drugs mechanisms

Na Channel blockers

A 
Carbamazepine
Oxcarbazepine
Lamotrigine
Phenytoin
Topiramate 
Valproic Acid
Zonisamide
29
Q

Epilepsy drugs

Ca channel blockers

A

High voltage activated Ca channel blockers
Lamotrigine
Topiramate

T-type Ca ch blocker
Valproic Acid
Zonisamide

30
Q

Epilepsy drugs

Ca ch subunit

A

Gabapentin
Pregabalin
Act on HVA Ca ch subunit alpha2 delta1

31
Q

Levetriacetam
Felbamate
Epilepsy

A

Binds to SV2A protein in walls of glutamate containing vesicles. Glutamate release impaired

Felbamate: blocks NMDA rec

32
Q

Anti epilepsy
Barbiturates
Benzodiazepines

A

Act on GABA rec
Prolongs opening of Cl channels
Inhibitory action

33
Q

Antiepleptics drugs

GABA

A

Tigabine (GAT1 inhibitor)
Inhibits GABA transporter and blocks GABA reuptake

Vigabatrin
Inhibits GABA aminotransferase (GABA-T) which catabolizes GABA. Thus GABA conc is increased.

34
Q

Antiepleptics

Side effects

A

All
Sedation
Dizziness

Carbamazepine oxcarbazepine
Hyponatremia

Vigabatrin lamotrigine
Visual disturbances

phenytoin
Double vision
Gingival hyperplasia
Hirsutism

Zonisamide topiramate
Cognitive disturbance
Wt loss (topiramate)

Valproic Acid
Wt gain

pregabalin gabapentin
peripheral edema
Hepatotoxic

Felbamate
Rare aplastic anemia

35
Q

Dopamine hypothesis

A

Mesolimbic pathway (⬆️ Dopamine) (hallucinations)

Mesocortical pathway (⬇️ Dopamine) (social withdrawal, no motivation)

Nigrostriatal pathway . ⬆️ Dopamine hyperkinetic movement dyskinesia ⬇️ Dopamine dystonia Parkinson

Tubero infundibular pathway.
Dopamine here inhibits prolactin

36
Q

Antipsychotics

1st generation

A

D2 blockers in all 4 pathways

So mesocortical dopamine ⬇️⬇️⬇️ social withdrawal, no energy, sad

Nigrostriatal Dopamine ⬇️⬇️⬇️ tremors, muscles rigidity

Tuberoinfundibular Dopamine ⬇️⬇️⬇️ gynecomastia, galactorrhea, sexual dysfunction

37
Q

Antipsychotics
1st generation
Typicals

A 
High potency
Haloperidol
Flupenazine
Prochlorperazine
Trifluoperazine

Low potency
Chlorpromazine
Bind to other receptors a B adrenergic and Histamine receptors causing more side effects

38
Q

Antipsychotics
2nd generation
Atypicals

A

D2 blockers and 5HT2A serotonin receptors

Reduced side effects

Aripiprazole
Clozapine
Lurasidine
Olanzapine
Quetiapine
Risperidone
ziprasidone
39
Q

2nd generation antipsychotics side effects

A

5HT2A blockers Clozapine, Olanzapine
Hyperglycemia
Hyperlipidemia

H1 blockers Clozapine Quetiapine:
Sleepiness
Wt gain

a1 blockers Clozapine Risperidone
Orthostatic Hypotension

Risperidone extrapyridimal side effects. Hyperprolactinemia

Clozapine Agranulocytosis

40
Q

Benzodiazepines

A

Mechanisms:
Act between gamma and alpha subunits of GABA a receptors and increase GABA binding to the receptors. Cl channels frequency increases and Cl influx happens

Adverse effects
Dizziness
Drowsiness
⬇️Motor coordination
⬇️ Alertness
41
Q

Barbiturates

A

Mechanisms
Bind to GABA a receptors between a and b subunits. They keep the Cl channels open for long period of time. In high doses they become GABA mimics as well.

Side effects
Dizziness
Lightheaded
Respiratory depression
Narrow therapeutic index
Overdose coma death
42
Q

Non benzodiazepines hypnotics

A

Selectively bind to a1 subunit in GABA A receptors
a1 subunit GABA A receptors are involved in sleep
While a2 & a3 subunit receptors are involved in anxiety control.
Thus these hypnotics only induce sleep not anxiolytics

Side effects
Memory loss
Day time sedation
Cognitive impairment
⬇️Motor function

Zolpidem
Zalpelon
Eszopiclone

CNS Drugs (9 decks)

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