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Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Amphetamine based stimulants examples

A

Amphetamine (Adderal)
Methylphenidate (Ritalin)

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2
Q

What are the indications of amphetamines

A

ADHD
Narcolepsy

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3
Q

Mechanism of action of amphetamine

A

Stimulates CNS through a sympathomimetic mechanism involving the enhanced release and reduced reuptake of NE and Dopamine

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4
Q

Adverse effects of ampthetamines

A

Photosensitivity( due to mydriasis)
Visual disturbance (paralyze accommodation)
Elevated BP(release NE stimulate A1)
Infection (fight flight-increased steroid release)
Headache

Serious side effects=
Dependency and abuse
Psychosis
Growth suppression
Heart failure
Stevens-johnson syndrome

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5
Q

Drug interaction between amphetamines and CAI (carbonic anhydrase inhibitors) (Diamox)

A

Renal excretion of amphetamine is decreased in alkaline urine

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6
Q

Dug interaction between amphetamines and sympathomimetic drugs eg phenylephrine

A

Hypertensive crisis
Arrhythmia

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7
Q

Dug interaction between amphetamines and ophthalmic B-blockers

A

Hypertensive crisis

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8
Q

Contraindications of amphetamines

A

Glaucoma

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9
Q

ADHD results from low levels of

A

Dopamine

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10
Q

Depression results from low levels of

A

NE and serotonin

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11
Q

SSRI (selective serotonin reuptake inhibitors) examples

A

Escitalopram
Sertraline
Fluoxetine

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12
Q

Escitalopram (SSRI) indication

A

Major depression
Generalized anxiety disorder

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13
Q

Escitalopram (SSRI) adverse effects

A

Common:

  • Dizziness

Distinguishing:

  • suicidal risk
  • serotonin syndrome(serious)
  • Neuroleptic malignant syndrome
  • Seizures

Ocular:

  • dry eye
  • Blur
  • Diplopia
  • Conjunctivitis
  • Ptosis
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14
Q

Drug interactions with SSRI’s (Escitalopram)

A

NSAIDS & Omega 3- hemorrhage risk (diminishing platelet aggregation)
Ophthalmic B-Blockers- reduced B-blocker metabolism (CYP450)

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15
Q

SNRI (Serotonin norepinephrine reuptake inhibitors) examples

A

Duloxetine
Venlaflaxine

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16
Q

Indication of SNRI’s

A

Depression
Anxiety
Diabetic neuropathic pain
Fibromyalgia

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17
Q

Adverse effects of SNRI’s

A

Common:
Blurred vision
Headache
Dizziness
Sweating
Erectile dysfunction
Orthostatic hypotension
Hypertension
Syncope
Yawning
Constipation

Distinguishing:
Serotonin syndrome
Hypersensitivity: Angioedema, Stevens-Johnsons

Ocular:
Glaucoma

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18
Q

Drug interactions with SNRI’s

A

Opioids- additive effect- shut down digestion
NSAID & Omega 3 - hemorrhage
Beta-blocker- reduced B-Blocker metabolism

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19
Q

Cautions for use of SNRI’s

A

Risk of bleeding
Angle closure glaucoma

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20
Q

TCADs (tricyclic antidepressants) examples

A

Imipramine
Amitriptyline
Clomipramine

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21
Q

Indications of trazodone(atypical antidepressant)

A

Major Depressive disorder
Insomnia

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22
Q

Examples of atypical antidepressants

A 
Trazodone 
Bupropion (wellbutrin, Zyban) 
Nefazadone
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23
Q

Mechanism of action of Trazodone (atypical antidepressant)

A

SSRI
A1 blocker
Seratonin 2a/c blocker (5-HT a/c)

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24
Q

Adverse effects of Trazodone (atypical antidepressant)

A

Common:
Headache
Dizziness
Blurred vision
Ocular irritation

Distinguishing:
Suicidal ideation
5-HT syndrome (serotonin syndrome)

CVS: hemorrhage

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25
Q

Drug interactions of Trazodone (Atypical antidepressant)

A

Cyclosporine, Macrolides(antibiotic),Azoles- QT prolongation & impaired hepatic metabolism
NSAID-hemorrhage

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26
Q

Mania is due to an excess of which neurotransmitters

A

NE, 5-HT and DA

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27
Q

Difference between D1 and D2 receptors

A

D1- stimulatory
D2- inhibitory

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28
Q

1st generation (typical) antipsychotics are antagonists of which receptor

A

Selective D2

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29
Q

2nd generation antipsychotics have selectivity for which receptors

A

Vary in selectivity for D2 and 5-HT2A- higher risk of metabolic side effects (hyperglycemia, dyslipidemia, weight gain)

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30
Q

3rd generation antipsychotic acts as functionally selective drugs. True or false

A

True

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31
Q

1st generation antipsychotic examples

A

Haloperidol
Chlorpromazine
Thiorodazine

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32
Q

2nd generation antipsychotic examples

A

Quetiapine
Clozapine
Olanzapine
Risperidone
Ziprasidone
Iloperiodone

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33
Q

What was the first ever antipsychotic

A

Lithium

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34
Q

3rd generation antipsychotic examples

A

Aripiprazole (partial agonist of D2 and 5HT1A)
Brexpiprazole (partial agonist of D2,D3 and near full agonist of 5HT1A)

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35
Q

Indications of Quetiapine( 2nd gen antipsychotics)

A
  • Schizophrenia
  • Bipolar
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36
Q

Adverse effects of quetiapine

A

Common:

  • Headache
  • Anemia

Hypersensitivity:

  • Stevens-Johnsons

Muscular:

  • Extrapyramidal symptoms

Ocular:

  • Cataracts
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37
Q

Quetiapine (2nd gen antipsychotic) mechanism of action

A

Antagonizes D2 and 5HT2 receptors

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38
Q

Name a CNS drug which is associated with cataract formation

A

2nd gen antipsychotics eg Quetiapine
1st gen antipsychotics eg Haloperidol

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39
Q

Interactions with quetiapine(2nd gen antipsychotic)

A

Macrolides, Azoles, cyclosporine - Prolonged QT segment
Classic(sedating) antihistamines -additive CNS depression

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40
Q

1st gen antipsychotic side effects

A

Haloperidol:

  • Photosensitivity
  • Anticholinergic effects
  • Drowsiness
  • Anxiety
  • Cataracts
  • Retinopathy

Chlorpromazine&Thioridazine:

  • Blur
  • Ocular pigmentation
  • Jaundice
  • Photosentitivity
  • Cataracts
  • Retinopathy
  • Night blindness
  • Salt & pepper fundus
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41
Q

What drug is associated with salt and pepper fundus

A

Chlorpromazine/ Thioridazine

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42
Q

Adverse effects of lithium

A

Blurred vision
Seizures
Bradycardia
Idiopathic intracranial hypertension

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43
Q

Drug interactions with lithium

A

Caffeine and CAI - reduced lithium levels through diuresis
NSAIDs , tetracycline- increased lithium levels

44
Q

Alzheimers

A

Loss of cholinergic neurons

45
Q

Donepezil (Alzheimer therapy) indication

A

Alzheimer’s
Dementia

46
Q

Mechanism of action of Donepezil (Alzheimer’s therapy)

A

Indirect acting, reversibly binds to and activates acetylcholinesterase (AChE) resulting in a sustained acetylcholine response

47
Q

Adverse effects of Donepezil

A
  • Headache
  • Dizziness
  • Arthritis
    • Seizures
  • Dream disturbances
  • Hemolytic anemia
  • AV block (atrioventricular block)
  • Bradycardia
  • Syncope
48
Q

Drug interactions with Donepezil

A
  • Cholinergic agents(pilocarpine) - additive
  • NSAIDs- Hemorrhagic risk
  • Anticholinergics(atropine)- Antagonism
  • Macrolides& azoles- Reduced metabolism of donepezil
  • Dexamethasone- Enhanced metabolism of donepezil
  • Brimonidine & Timolol ophthalmic- Enhanced bradycardia and bronchospasm
  • Ester Anesthetics- Reduced metabolism of anesthetics
49
Q

Sinemet (Levodopa &Carbidopa) combination is indicated for

A

Parkinson’s

50
Q

Mechanism of action of Sinemet(Levodopa and carbidopa)

A

Levodopa is a DA precursor that unlike DA crosses the BBB to enhance DA synthesis

Carbidopa is an inhibitor of dopa decarboxylase (enzyme that degrades levodopa to dopamine), peripheral degradation prevents drug crossing BBB
(makes sure the levodopa enters cns)

51
Q

Adverse effects of sinemet(Levodopa&carbidopa)

A

Headache
Confusion
Psychosis(elevation of catecholamines)
Suicidal ideation
Hallucinations

52
Q

Indications of Bromocriptine

A

Parkinson’s
Acromegaly (developemental condition)
Hyperprolactinemia
Neuroleptic malignant Syndromes(over activity in muscles)

53
Q

Mechanism of action of Bromocriptine

A

Stimulates DA receptors
Inhibits anterior pituitary prolactin secretion

54
Q

Adverse effects of Bromicriptine

A

Headache
Dizziness
Nasal congestion(changes in vascular tone)
Visual disturbance
Seizures
Neuroleptic malignant syndrome if abrupt discontinuing
Hypertension
Orthostatic hypotension

55
Q

Drug interactions of Bromocriptine

A

Avoid:
Pseudoephedrine, epinephrine- additive hypertension

Monitor:
Cyclosporine(more oral)- levels of both drugs may rise

Caution:
Cetirizine -additive CNS depression
Macrolides, Azoles-elevated bromocriptine levels

56
Q

Contraindications for bromocriptine

A

Uncontrolled hypertension (HTN)

57
Q

Safinamide indications

A

Parkinson’s
Dystonia

58
Q

Mechanism of action of Safinamide

A

Selectively inhibits MAOb
Increasing extracellular DA in the striatum

59
Q

Adverse effects of Safinamide

A

HTN (hypertension)(elevate sympathetic activity)
Nausea
cough
Hallucinations
NMS (Neuroleptic malignant Syndrome) if abrupt discontinuation
Retinal degeneration(animal studies)

60
Q

Contraindications of Safinamide

A

Tramadol(opioid) - additive 5HT-syndrome risk

Monitor: (additive HTN)
Caffeine,
epinephrine,
Naphazoline ophthalmic
oxymetazoline opt
phenylephrine oph
pseudoephedrine

61
Q

Anxiolytics

A 
Majority of drugs in this class promote actions of GABA 
which is the CNS major inhibitory neurotransmitter
62
Q

________ is nr 1 stimulatory neurotransmitter
______ nr 1 inhibitory neurotransmitter in CNS

A

Glutamate is nr 1 stimulatory neurotransmitter in CNS
GABA is the nr 1 inhibitory neurotransmitter in CNS

63
Q

Anxiolytic/hypnotic drug classes

A

Benzodiazepines
Non-benzodiazepines
Barbiturates

64
Q

Intermediate acting Benzo’s

A

Alprazolam(low potency, high TI)
Lorazepam
Temazepam(low potency, igh TI)
Clonazepam(high potency and lower TI)

65
Q

Short acting Benzo’s

A

Midazolam
Triazolam

66
Q

Long acting benzo’s

A

Diazepam
Chlordiazepoxide(low potency, high TI)
Flurazepam

67
Q

Indications of Alprazolam(Benzo)

A

Anxiety
Panic disorder

68
Q

Mechanism of action of Alprazolam(Benzo)

A

Selectively binds to BZD(benzodiazepine) site on GABAa receptors, allosterically enhancing GABA affinity
Receptor activation opens ion channel leading to chloride influx or efflux and resultant hyperpolarization(inhibition)

69
Q

Does cocaine, benzo’s, amphetamines act directly or indirectly on receptors

A

Indirect

70
Q

Side effects of alprazolam(Benzo)

A
  • Diplopia
  • Drowsiness
  • Anterograde amnesia
  • Confusion
  • Dizziness
  • Hypotension
  • Steven’s-Johnson
  • Angioedema
71
Q

Drug interactions of Alprazolam(Benzo)

A

Cyclosporine, Azoles, Macrolides - reduced alprazolam metabolism
Chlorpheniramine, diphenhydramine, opioids -additive effect

72
Q

Contraindications of alprazolam(Benzo)

A

unstable Myasthenia gravis

73
Q

Non-benzo example

A

Zolpidem

74
Q

Indications of zolpidem

A

Insomnia

75
Q

Mechanism of action of zolpidem(non-benzo)

A

Selective agonist of GABAa-BZD-1 receptor

76
Q

Adverse effects of zolpidem

A

Headache
Sinusitis
Pharyngitis
Amnesia
Suicidal ideation
Aggression
Hallucinations
(Flippen verslawend! veronderstel om nie te wees)

77
Q

Drug interactions with zolpidem

A

Cyclosporine, Azoles - reduced metabolism of zolpidem
Classic antihistamines, opioids- additive

78
Q

Indications of phenobarbital(barbituate)

A

Seizure disorder
Status epilepticus
Sedation

79
Q

Mechanism of action of phenobarbital(barbituate)

A

Convey synaptic inhibition to sensory cortex and to cerebellar and motor activities ,produces sedation, hypnosis and anesthesia

Enhances GABA effects at GABAa receptor

80
Q

Adverse effects of phenobarbital

A

Drowsiness
Nausea and vomitting
Respiratory depression
Hypersensitivity: Steven’s-Johnsons, angioedema,
Blood dyscrasias
Withdrawal symptoms if abrupt discontinuation

81
Q

Drug interactions of phenobarbital

A
  • Acetaminophen(paracetamol)-phenobarbital enhances acetaminophen metabolism leading to metabolic toxicity risk
  • Opioids-phenobarbital enhances acetaminophen metabolism leading to metabolic toxicity risk
  • Erythromycins(macrolides), tetracyclines, steroids- enhanced metabolism by phenobarbital
  • Azole antifungals- enhanced metabolism by phenobarbital
  • Classic antihistamines- additive cns depression
  • Lidocaine topical- increased methemoglobinemia risk
82
Q

Contraindications of phenobarbital

A

Respiratory dysfunction

83
Q

Indications of phenytoin

A

Seizure disorders
Status epilepticus

84
Q

Mechanism of action of phenytoin

A

Modulates neuronal voltage-dependant sodium and calcium chanels

85
Q

Adverse effects of phenytoin

A
  • Nystagmus
  • Blur
  • Headache
  • Pancytopenia (lower than normal red&white blood cells and platelets in blood)
  • Hypersensitivity- stevens johnsons, TEN (rare life threatening skin condition)
  • Lupus
86
Q

Drug interactions with phenytoin

A

Acetaminophen- induced hepatic metabolism by phenytoin metabolite toxicity riak with repeated dosing

Erythromycin,azoles,opiods,steroids- induced hepatic metabolism by phenytoin

Antihistamines-additive cns depression

Topical lidocaine- increased methemoglobinemia risk

Acyclovir- reduced phenytoin levels

87
Q

Contraindications of phenytoin

A

Caution in diabetes

88
Q

Examples of muscle relaxants

A

Cyclobenzaprine
Tizanidine

89
Q

Indication of cyclobenzaprine and tizanidine

A

Muscle spasm
Fibromyalgia

90
Q

Mechanism of action of cyclobenzaprine

A

Central acting: potentiates NE and stimulates serotonin receptors

91
Q

Mechanism of action of tizanidine

A

Central acting: binds to presynaptic alpha 2 adrenergic receptors, inhibits neurotransmitter release

92
Q

Adverse effects of cyclobenzaprine symptoms

A

Blur
Headache
Hypersensitivity
Myocardial infarction

93
Q

Adverse effects of tizanidine

A

Hypotension
Blur
Syncope
Bradycardia
Hypersensitivity stevens johnsons

94
Q

Drug interactions of cyclobenzaprine

A

Avoid anticholinergics- additive effects
Avoid serotonergic agents - additive effects, risk of serotonin syndrome

95
Q

Drug interactions of tizanidine

A

Ciprofloxacin- reduces tizanidine metabolism leading to a rise in levels with routine dosing

96
Q

Adverse effects of cyclobenzaprine

A

Blur
Headache
Hypersensitivity
Myocardial infarction

97
Q

Adverse effects of tizanidine

A

Hypotension
Blur
Syncope
Bradycardia
Hypersensitivity stevens johnsons

98
Q

Drug interactions with cyclobenzaprine

A

Avoid Anticholinergics- additive effects

Avoid serotogenic agents- additive effects, riak of serotonin syndrome

99
Q

Contraindications of cyclobenzaprine

A

CNS depressant use
Narrow angles
Elevated IOP

100
Q

Contraindications of tizanidine

A

CNS depressant use

101
Q

ADHD is characterized by low/high levels of which neurotransmitter

A

Low dopamine

102
Q

Depression is characterized by low/high levels of which neurotransmitters

A

Low Norepinephrine and low serotonin

103
Q

Mania/psychosis is characterized by low/high levels of which neurotransmitters

A

High Dopamine, high Norepinephrine and high Serotonin

104
Q

Alzheimers is characterized by low/high levels of which neurotransmitters

A

Low Acetylcholine and high Glutamine

105
Q

Parkinsons is characterized by low/high levels of which neurotransmitters

A

Low Dopamine , high Acetylcholine

106
Q

Anxiety is characterized by low/high levels of which neurotransmitter

A

Low GABA

Pharmacology (19 decks)

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