Pharm - Adrenergic/Cholinergic Effects, Movement Disorders, Analgesia Flashcards

1
Q

Adrenergic pathway in CNS

A

Norepinephrine distributed throughout brain; majority of noadrenergic neurons in locus ceruleus (sleep and arousal center)

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2
Q

Adrenergic receptors

A

G protein coupled

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3
Q

Cholinergic pathways in CNS

A

Mixture of both nicotinic and muscarinic

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4
Q

Ach and NE brain functions

A

Ach - motivation, learning, memory; NE - arousal, attention, vigilence, and memory; both involved with wakefullness and cognition

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5
Q

Antipsychotics

A

Work on many receptors in the brain (ex - muscarinic blockade, dopamine blockade); AE - xerostomia, constipation, Parkinson’s

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6
Q

Effects of antidepressants

A

Similar to antipsychotics but with CV involvement - hypotension, reflex tachycardia

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7
Q

Treatment for Parkinsonism

A

Benztropine, diphenhydramine, trihexyphenidyl

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8
Q

Receptors in amygdala

A

Alpha and beta 1 adrenergic receptors

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9
Q

PTSD treatment

A

Paroxetine and sertriline (SSRI), prazosin and propanolol (for amygdala)

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10
Q

Lipophilic drugs that have central effects

A

Propanolol and diphenhydramine

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11
Q

Pathogenesis of Parkinson’s

A

Indirect pathway predominates, loss of dopamine input from SNpc or blockade of dopamine receptors

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12
Q

Dopamine replacement therapy

A

Primary treatment, use when symptoms show functional impairment, levodopa used bc DA cannot cross BBB, fluctuations in response “on-off phenomena”

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13
Q

Stimulation of DA receptors

A

Activate D2 receptors to turn of indirect pathway

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14
Q

Drugs that stimulate DA receptors

A

Bromocriptine (D2 agonist/D1 partial agonist), apomorphine (D1/D2 agonist), Pramipexole (D2 selective), Ropinirole (D2 selective)

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15
Q

Enhancement of DA release

A

Amantadine

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16
Q

Inhibition of DA metabolism

A

Selegiline (selective MAO-B inhibitor), Rasagiline (inhibitor of MAO-B), Entacapone/tolcapone (selective inhibitors of COMT)

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17
Q

Muscarinic Antagonist for PD

A

To block cholinergic activation of striatum - benztropine, diphenhydramine, trihexyphenidyl

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18
Q

Treatment for Huntington’s

A

Reserpine and tetrabenazine (DA depleting), chlorpromazine and haloperidol (DA antagonist)

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19
Q

How opiates lead to death

A

Respiratory depression

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20
Q

How opioids works

A

Inhibition of calcium presynaptically, activation of potassium postsynaptically

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21
Q

What plays an important role in central sensitization

A

NMDA receptors

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22
Q

NMDA blockers

A

Ketamine and Dextromethorphan used prior to surgery to avoid sensitization

23
Q

Common features of opiates and adjunctive agents

A

Sedation

24
Q

Common feature of alpha 2 adrenergic agonists

A

Reduced sympathetic outflow; hypotension, bradycardia

25
Q

Opiate receptor subtypes

A

Delta, kappa, mu (OP 1,2,3 - think alphabetic order) - highest affinity for enkephalins, dynorphins, and endorphins, respectively

26
Q

Opiate agonists (mu receptor)

A

Morphine (kappa a little too), Hydromorphone, Oxymorphone, Methadone, Meperidine, Fentanyl, Remifentanil

27
Q

Partial agonists of mu

A

Codeine, Hydrocodone, Oxycodone, Pentazocine, Nalbuphine, Buprenorphine, Butorphanol (more kappa activity in these)

28
Q

Transdermal opiate delivery

A

Fentanyl patches

29
Q

Opiate with low oral bioavailability? High?

A

Low oral bioavailabiltiy - morphine; high - codeine, oxycodone

30
Q

Mechanism of desensitization

A

Some like morphine only activate G-protein signaling but fail to activate endocytosis (recycling of receptors); enkephalin does both

31
Q

Mediators of receptor internalization

A

GRK2 and beta arrestin (arrested for using opiate drugs!)

32
Q

Tolerance in opiate drug use

A

High tolerance to most things like analgesia (which sucks) and low tolerance to constipation and convulsions which are persistent (double sucks)

33
Q

Adverse effects of opiates that may need management

A

Nausea/vomiting, constipation, pruritis, respiratory depression, somnolence

34
Q

Classic triad of opiate overdose

A

coma, pinpoint pupils, respiratory depression

35
Q

Opiate antagonists

A

Naloxone, nalmefene, naltrexone (the longer the name the longer the action)

36
Q

Converted to morphine

A

Heroin and codeine

37
Q

Meperidine

A

Anticholinergic effects, not used commonly because of diverse effects

38
Q

Best opiate to use in treating opiate withdrawal

A

Methadone - really long half life

39
Q

Tramodol

A

Little effect on respiratory or CV systems; increased risk of hypoglycemia compared to codeine (mnemonic: tremor-dol; tremors bc of low sugar)

40
Q

Opiates used in renal insufficiency

A

Hydromorphone and fentanyl (no active metabolites)

41
Q

Strategy for management of poorly responsive pain

A

Opiate rotation

42
Q

Signs of opiate withdrawal

A

Agitation, diaphoresis, increased lacrimation, piloerection, dilated pupils

43
Q

Short-term treatment of opiate withdrawal

A

Methadone and clonidine

44
Q

Buprenorphine combination

A

Has naloxone that works only IV and not oral so it discourages abuse of the drug

45
Q

Opiate for pregnancy

A

Methadone

46
Q

Adverse effects of methadone

A

Constipation, drowsiness, prolonged QTc and arrhythmia

47
Q

Buprenorphine for opiate withdrawal

A

Precipitates withdrawal due to high affinity to receptors, long duration, ceiling effect (hard to overdose)

48
Q

Gabapentin/Pregabalin

A

Inhibits neuron excitation by binding to alpha2-delta subunit

49
Q

Lamotrigine/Carbamazepine

A

Block sodium channels

50
Q

Anti-tussive opiates

A

Codeine and Dextromethorphan

51
Q

Antidiarrheal opiates

A

Loperamide and Diphenoxylate

52
Q

Treatment for alcohol dependence and cravings

A

Naltrexone

53
Q

Surgical management of pain

A

Neuroablation (last resort)

54
Q

Opiate found combined with acetaminophen

A

Codeine, oxycodone, and hydrocodone