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CNS > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What blocks the effects of opioids?

A

Naloxone

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2
Q

Describe opioid receptors

A

g-protein coupled receptors [Go/Gi]

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3
Q

What are the main analgesic opioids?

A

μ [Mu] agonists

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4
Q

Activation of opioid receptors produces …?

A

Inhibits adenylyl cyclase → Increases cGMP → pKA

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5
Q

List opioids that are Mu agonists

A

Morphine
Codeine
Prthidine
Fentanyl

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6
Q

List Mu antagonists

A

Naloxone

Naltrexone

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7
Q

What drug of abuse is a mu agonist?

A

Heroin [diamorphine]

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8
Q

What are the MOA of opioids?

A

Inhibits adenylyl cyclase → reduced cGMP → reduced pKA → no phosphyrlazation of channels

Activation of K conductance → hyper polarization

Inhibition of Ca conductance → reduced Ca entry into neurons → Reduced NT release and synaptic transmission

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9
Q

Side effects of opioids?

A 
Respiratory distress (→ death)
Constipation 
Pupilary contraction 
Bronchoconstriction 
Hypotension 
Pruritis
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10
Q

Which opioid is used to treat diarrhea?

A

Loperamide

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11
Q

What reverses tolerance to Opioids?

A

NMDA receptor antagonists

Ketamine
Dextromethorphan

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12
Q

What treats opioids dependance?

A

Methadone

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13
Q

Indications of weak opioids

A

Mild inflammatory arthritic pain, used in conjunctions with NSAIDs

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14
Q

Indications of strong opoids

A

Severe acute pain
Cancer pain
Back pain
Severe arthritis

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15
Q

Side effects of Morphine

A 
Cough Suppression 
Constipation 
Euphoria
Analgesia 
Sedation 
Dependence 
Tolerance
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16
Q

What form of morphine is the most potent?

A

M6G is more potent than morphine

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17
Q

Indications of Codeine

A

Coughing

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18
Q

MOA of Tramadol

A

Serotonin and NA re-uptake inhibitor [SNRI}

[partial Mu agonists]

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19
Q

Contraindications of Tramadol

A

Suicidal patients

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20
Q

What does Tramadol interact with?

A 
Alcohol 
Narcotics 
Sedative
Anxiolytics
Anti-depressants
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21
Q

What blocks the effects of Tramadol?

A

Naloxone [partially]

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22
Q

Side effect of Pethidine

A

Bronchoconstriction

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23
Q

Contraindications of Pethidine

A

Asthmatics

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24
Q

What is the hard life of Fentanyl?

A

3-6 hrs. in the plasma

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25
Q

Route of Administration of Fentanyl?

A

Sublingual

Transdermal

26
Q

Route of Administration of Codeine

A

Oral

27
Q

Route of Administration of Morphine

A

IV
IM
Orally
Epidural route

28
Q

MOA of Methadone

A

NMDA receptor Antagonists

29
Q

What is used for treating addicts?

A

Methadone

30
Q

MOA of Naloxone

A

Mu antagonists

31
Q

What treats morphine dependence?

A

Morphine

32
Q

MOA of Naltrexone

A

Mu antagonists

33
Q

Duration of Naloxone and Naltrexone

A

naltrexone has a longer duration of action

34
Q

What role does GABA play in pain?

A

No role, rather it plays a role in epilepsy and anxiety

35
Q

What are orphan receptor?

A

receptors that don’t have an affinity for opioid ligands

36
Q

Administration of morphine in RVM

A

Suppresses ON cells
Activates Off cells
Neutral cells

37
Q

What degrades 5HT in systole?

A

Monoamine Oxidase and Aldehyde Dehydrogenase

38
Q

What NT crosses BBB?

A

Tryptophan

39
Q

What is the role of Reserpine?

A

Transports of NA into vesicles

40
Q

What is the biochemical basis of depression?

A

Deficiency of monoamines [NA and 5HT]

41
Q

What is the biochemical basis of mania?

A

Overproduction of Monoamines [NA and 5HT]

42
Q

What effects do antidepressants produce in children >18 yrs?

A

Insomnia
Aggression
Worsening of Suicidal thoughts

43
Q

How can antidepressants induce seizures ?

A

Its lowers seizure threshold

44
Q

Onset of Antidepressants?

A

Beneficial effects within 2 weeks, maladaptive changes are produced earlier than beneficial

45
Q

MOA of imipramine

A

Inhibits neuronal re-uptake of NA and Serotonin into presynaptic nerve terminals

Block 5HT, alpha Adrenergic, histamine and muscrainic receptors

46
Q

Indications of imipramine

A

Moderate-severe depression

Panic/Anxiety attacks

47
Q

Side effects of imipramine

A 
Weight gain 
Orthostatic Hypotension
Dizziness
Reflex Tachycardia
Arrhythmia
Sudden death
Blurred vision
Dry mouth 
Urinary retention 
Constipation
48
Q

What drug interactions with imipramine produces toxic sedations?

A

Ethanol

CNS depressants

49
Q

What drug interactions with imipramine produces potentiation effects?

A

Direct acting adrenergic drugs

50
Q

What drug interaction with imipramine blocks its effect?

A

Indirect acting adrenergic drugs

51
Q

What precautions must be taken before prescribing imipramine?

A

Bipolar disorders [unmasks mania]

Suicidal patients [narrow TI]

52
Q

What drugs is a TCAs?

A

Imipramine

53
Q

What drugs are SSRIs?

A

Fluoxetine

Citalopram

54
Q

MOA of SSRIs

A

selectively inhibits serotonin re-uptake, and at higher doses can affect Na

55
Q

Indications of SSRIs

A 
Moderate depression
Bulimia nervosa
OCD
Anorexia 
Panic disorders

[dose reduced in hepatically impaired patients]

56
Q

Side effects of SSRIs

A

Anticholinergic ad cardiotoxic effects

57
Q

Half life of Fluoxetine

A

7-15 days

58
Q

Side effects of Fluoxetine

A 
Nauseas
Anxiety 
Insomnia
Weight loss/Anorexia
Tremors
Sexual Dysfunction 
Seizures [overdose]
59
Q

MOA of Fluoxetine

A

Antagonist at 5HT2C and weak NA re-uptake inhibitor at higher doses

60
Q

MOA of SNRIs?

A

Inhibits reuptake of 5HT and NA

61
Q

What drugs are SNRIs?

A

Venlafaxine and Duloxetine

CNS (10 decks)

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