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Flashcards in FA Neuro Pharm Deck (98):
1

Mu-opioid receptor partial agonist and kappa opioid receptor agonist; produces analgesia

Butophanol

2

Very weak opioid agonist; also inhibits serotonin and NE reuptake (used for chronic pain)

Tramadol

3

Facilitates GABAa action by increasing DURATION of Cl- channel opening, thus decreasing neuron firing (barbiturates increase duration). Contraindicated in porphyrias.

Barbituates

4

Facilitate GABAa action by increasing FREQUENCY of Cl- channel opening. Decrease REM sleep,

Benzos

5

Act via the BZ1 subtype of the GABA receptor. Effects reversed by flumazenil.

Nonbenzo hypnotics

6

Block Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons.

Local anesthetics

7

Prevents the release of Ca2+ from the SR of skeletal muscle

dantrolene

8

Selectively inhibits MAO-B, which preferentially metabolizes dopamine over norepinephrine and 5-HT, thereby increasing the availability of dopamine

Selegiline

9

NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+)

Memantine

10

AchE inhibitors

Donepezil, galantamine, rivastigmine

11

Inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release

Tetrabenzamine, reserpine

12

5-HT1B/1D agonist. Inhibits trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction. Half-life < 2 hrs

Sumatriptan

13

Increases Na+ channel inactivation, zero-order kinetics

Phenytoin

14

Increases Na+ channel inactivation

Carbamazepine

15

Increases Na+ channel inactivation, increases GABA concentration by inhibiting GABA transaminase

Valproic acid

16

Primarily inhibits high-voltage-activated Ca2+ channels; designed as GABA analog

Gabapentin

17

Blocks thalamic T-type Ca2+ channels

Ethosuximide

18

Increases GABAa action

Phenobarbital

19

Blocks Na+ channels and increases GABA action

Topiramate

20

Blocks voltage-gated Na+ channels

Lamotrigine

21

Unknown; may modulate GABA and glutamate release

Levetiracetam

22

Increases GABA by inhibiting reuptake

Tiagabine

23

Increases GABA by irreversibly inhibiting GABA transaminase

Vigabatrin

24

Decreases aqueous humor synthesis via vasoconstriction

Epinephrine

25

Tox: Mydriasis; do NOT use in closed-angle glaucoma

Epinephrine

26

Alpha2 agonist that decreases aqueous humor synthesis

Brimonidine

27

Tox: Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic run, ocular pruritus

Brimonidine

28

5 classes of drugs that can be used for glaucoma

1. alpha agonists
2. beta blockers
3. diuretics
4. cholinomimetics (direct and indirect)
5. prostaglandin

29

What beta blockers can be used for glaucoma?

Timolol, betaxolol, carteolol

30

What diuretic can be used for glaucoma?

Acetazolamide

31

What alpha agonists can be used for glaucoma?

Epinephrine, brimonidine

32

Decreases aqueous humor synthesis via inhibition of carbonic anhydrase

Acetazolamide

33

Two direct cholinomimetics that can be used for glaucoma

pilocarpine and carbachol

34

two indirect cholinomimetics that can be used for glaucoma

physostigmine and chothiophate

35

What drug do you use in a glaucomic emergency?

pilocarpine - very effective at opening meshwork into canal of Schlemm

36

What is the mechanisms of cholinomimetics in treatment of glaucoma?

Increased outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork

37

What are the side effects of cholinomimetics in treatment of glaucoma?

miosis and cyclospasm (contraction of ciliary muscle)

38

What prostaglandin is useful in glaucoma treatment?

Latanoprost (PGF2alpha)

39

what is the mechanism of latanoprost?

increased outflow of aqueous humor

40

tox latanoprost

darkens color of iris

41

agonist at mu receptors

morphine

42

agonist at delta receptors

enkephalin

43

agonist at kappa receptors

dynorphin

44

what opioid is used for cough suppression?

dextromethorphan

45

what opioid is used for diarrhea

loperamide, diphenoxylate

46

opioid analgesic mechs

act as agonists at opioid receptors to (open K+ channels, close Ca2+ channels) --> decreased synaptic transmission Inhibit release of ACh, NE, 5-HT, glutamate, substance P

47

opioid antidote

naloxone or naltrexone

48

Butorphanol mech

mu opioid PARTIAL receptor agonist and kappa opioid receptor agonist; produces analgesia

49

CU butorphanol

severe pain (migraine, labor); causes less respiratory depression that full opioid agonists

50

Butorphanol Tox

can cause opioid withdrawal sx is pt is also taking full opioid agonist (competition for opioid receipts). OD not easily reversed w. naloxone

51

Tramadol mech

very weak opioid agonst; also inhibits serotonin and NE reuptake (works on multiple NTs - "tram it all" in with tramadol).

52

CU tramadol

chronic pain

53

Tramadol tox

opioid tox, decreases seizure threshold, serotonin syndrome

54

ethosuximide mech

blocks thalamic T-type Ca2+ channels

55

Tox ethosuximide

EFGHIJ
Ethosuximide causes Fatigue, GI distress, Headache, Itching, stevens-Johnson

56

barbiturate mech

facilitate GABA(A) action by increasing the DURATION of chloride channel opening, thus decreasing neuron firing (barbiDURATes increase DURATion). Contraindicated in porphyria

57

barbiturate CU

sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

58

barbiturate tox

respiratory and CV depression (can be fatal!); CNS depression (exacerbated by EtOH); dependence; drug interaxns (INDUCES P450!).

59

barbituate AD?

none! supprotive - assist respiration and maintain BP

60

phenobarbital, pentobarbital, thiopental, secobarbital

barbiturates

61

benzo mech

facilitate GABA(A) action by increasing FREQUENCY of chloride channel opening, decrease REM sleep

62

highest addictive potential, shortest acting benzos

Triazolam
Oxazepam
Midazolam

63

status epilepticus tx

lorazepam, diazepam

64

benzo AD

flumazenil

65

flumazenil mech

competitive antagonist at GABA benzo receptor

66

Non benzo hypnotic examples

Zolpidem
Zaleplon
Eszopiclone

67

Zolpidem mech

act via the BZ1 subtype of the GABA receptor

68

MAC =

miminal alvelolar concentration required to prevent 50% of subjects from moving in response to noxious stimulus (e.g. skin incision)

69

inhaled anesthetic with hepatotoxicity

halothane

70

inhaled anesthetic with nephrotoxicity

methoxyflurane

71

inhaled anesthetic that is proconvulsant

enflurane

72

inhaled anesthetic that can cause expansion of trapped gas in a body gravity?

nitrous oxide

73

the one inhaled anesthetic that doesn't cause malignant hyperthermia

nitrous oxide

74

what besides inhaled anesthetics can cause malignant hyperthermia

succinylcholine

75

tx malignant hypertension

dantolene

76

dantrolene mech

prevents the release of Ca2+ from SR of skeletal muscle

77

what causes neuroleptic malignant syndrome?

antipsychotic drugs

78

IV anesthetic barbiturate

thiopental

79

IV anesthetic benzo

midazolam

80

PCP analogs that act as dissociative anesthetics, Block NMDA receptors. CV stimulants. Cause disorientation, hallucination, and bad dreams. Increases cerebral BF

arylcyclohezylamines (ketamine)

81

Used for sedation in ICU, rapid anesthesia induction, and short procedures. Less post operative nausea than thiopental. Potentiates GABA(A).

Propofol

82

local anesthetic esters

procaine, cocaine, tetracaine

83

local anesthetic amides

lidocaine, mepivacaine, bupivacaine,

84

local anesthetic mechanism

blocks Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons. Teritiary amine local anesthetics penetrate membrane in uncharted form, then bind to ion channels in charged form.

85

Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction

succinylcholine (depolarizing nueromuscular blocking drug)

86

reversal of non depolarizing neuromuscular blockade?

neostigmine (must be given with atropine to prevent muscarinic effects such as bradycardia), edrophonium, and other cholinesterase inhibitors)

87

How to treat Parkinson dz?

BALSA
Bromocriptine
Amantadine
Levodopa w/ carbidopa
Selegiline (and COMT inhibitors)
Antimuscarinics

88

levodopa tox

arrythmias from increased peripheral formation of catecholamines. long term use can lead to dyskinesia following administration ("on off phenomenon"), akinesia between doses

89

how to treat alzheimers?

memantine (NMDA receptor antagonist)
AChE inhibitors (donepezil, galantamine, rivastigmine)

90

memantine tox

dizziness, confusion, hallucinations

91

AChE inhibitor tox

nausea, dizziness, insomnia

92

NT changes in HD?

decreased GABA and ACh,
Increased dopamine

93

HD tx

tetrabenazamine and reserpien;
haloperidol

94

tetrabenazine and reserpine mech

inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release

95

haloperidol mech

dopamine receptor antagonist

96

sumatriptan mech

5HT1b/1D agonist. INhibts trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction. Half-life < 2 hours

97

sumatriptan CU

acute migraine, cluster headache

98

sumatriptan tox

coronary vasospasm (contraindicated in pts with CAD or Prinzmetal), mild tingling.