Neuro Pharm Flashcards Preview

Boards > Neuro Pharm > Flashcards

Flashcards in Neuro Pharm Deck (147):
1

How do you treat essential tremor (postural tremor)?

Beta-blockers
Primidone (anti-convulsant)
ETOH (decreases tremor amplitude)

2

How do you precipitate Wernicke-Korsakoff syndrome?

Giving glucose without B1 to a B1 deficient patient

3

Treat subarachnoid hemorrhage?

Nimodipine (Ca channel blocker)

4

What is indicated in ischemic stroke?

tPA within 4.5 hours
as long as paint presents within 3 hours of onset & there is no major risk of hemorrhage

5

What are some ALS therapies?

Riluzole (decrease presynaptic glutamate release)
Baclofen (GABA-B agnoist to dec spasticity)

6

What is contraindicated in closed (narrow angle) glaucoma?

Epinephrine
(bc causes mydriasis)

7

How do you treat Dry ARMD (nonexudative age-related macular degeneration)?

prevent progression-- multivitamins & antioxidants

8

How do you treat Wet ARMD (exudative age-related macular degeneration)?

anti-VEGF injections or laser
(stops choroidal neovascularization)

9

How do you treat MS?

Beta-interferon
Natalizumab (monoclonal AB against alpha-4 integrin for cell adhesion)
Glatiramer (immune modulator)
Symptomatic Tx: 1) Baclofen (GABA-B agonist-- tx spasticity), 2) Muscarinic antagonist & catheterization (neurogenic bladder), 3) Opiods (pain)

10

How do you treat Guillain-Barre?

Respiratory ventilator support
Plasmapheresis
IV immune globulins

11

What is the DOC for partial (focal) seizures?

Carbemazepine

12

How do you treat cluster HA?

inhaled oxygen
sumatriptan

13

How do you treat migraine?

Abortive-- triptans
Prophylacitc-- propranolol, topiramate

14

What is the general mechanism of glaucoma drugs?

decrease amount of aqueous humor to decrease intraocular pressure

15

Which drug classes are used to treat glaucoma?

alpha-agonists
beta-blockers
diuretics
cholinomimetics
prostaglandin

16

Which alpha-agonists are used to treat glaucoma?

Epinepherine
Brimonidine (alpha 2)

17

What is the MOA of alpha-agonists in glaucoma?

decrease aqueous humor synthesis
(epi does so via vasoconstriction)

18

Side effects of alpha-agonists in glaucoma?

Mydriasis-- Epi is contraindicated in closed-angle glaucoma
blurry vision, ocular hyperemia, foreign body sensation, ocular allergic rxn, ocular pruritis

19

Which beta-blockers are used in glaucoma?

Timolol
Betaxolol
Carteolol

20

What is the MOA of beta-blockers in glaucoma treatment?

Dec aqueous humor synthesis
*no pupillary or vision change S/E

21

Which diuretic is used to treat glaucoma?

Acetazolamide

22

What is the MOA of acetazolamide?

dec aqueous humor synthesis via carbonic anhydrase inhibition
*no pupillary or vision change S/E

23

Which cholinomimetics are used to treat glaucoma?

Direct-- Pilocarpine, Carbachol
Indirect-- Physostigmine, Echothiphate

24

What is the MOA of cholinomimetics in glaucoma?

inc outflow of humor via contraction of ciliary muscle and opening of trabecular meshwork

25

Which cholinomimetic is very effective in emergencies?

Pilocarpine (direct cholinomimetic)
acts quickly at opening trabecular meshwork into canal of schlemm

26

What are the side effects of cholinomimetics in glaucoma?

Miosis
Cyclospasm (contraction of ciliary muscle)

27

Which prostaglandin is used in glaucoma?

Latanoprost (PGF-2-alpha)

28

What is the MOA of prostaglandin used in glaucoma?

inc outflow of aqueous humor

29

What is the S/E of prostaglandin in glaucoma?

Darkening of the iris (browning)

30

What are the common opioid analgesics?

Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan
Diphenoxylate

31

What is the MOA of opioid analgesics?

agonists at opioid receptors to modulate synaptic transmission
opens K channels & closes Ca channels to decrease synaptic transmission.
inhibits release of ACh, HE, 5-HT, glutamate, substance P

32

What are the opioid receptors?

Mu = morphine
delta = enkephalin
kappa = dynorphin

33

Clinical use of opioid analgesics?

pain
cough suppression (dextromethorphan)
diarrhea (loperamide & diphenoxylate)
acute pulmonary edema
maintenance for addicts (methadone)

34

Toxicity of opioid analgesics?

Addiction
Respiratory depression
constipation
miosis (pinpoint pupils)
additive CNS depression with other drugs (esp ETOH, BZD, Barbs)
NO tolerance to miosis & constipation

35

What is the antidote to opioid OD?

Naloxone or Naltrexone
(opioid receptor antagonists)

36

What is the MOA of Butorphanol?

Mu-opioid receptor partial agonist
Kappa-opioid receptor agonist

37

Clinical use of Butorphanol?

Analgeisa for severe pain (migraine, labor, etc)
causes less respiratory depression than full opioid agonists.

38

What is the toxicity of Butorphanol?

opioid withdrawal symptoms if also taking full opioid agonist (competition for opioid receptors)
OD not easily reversed with Naloxone

39

What is the MOA of Tramadol?

Very weak opioid agonist
inhibitis serotonin & NE reuptake

40

What is the clinical use of Tramadol?

chronic pain

41

What is the toxicity of Tramadol?

similar to opioids-- resp depression, miosis, constipation, etc.
decreases seizure threshold

42

Anti-epileptic drugs

Phenytoin
Carbamazepine
Lamotrigine
Gabapentin
Topiramate
Phenobarbital
Valproic Acid
Ethosuximide
Benzodiazepines (Diazepam or Lorazepam)
Tiagavine
Vigabatrin
Levetiraceteam

43

1st line for tonic-clonic?

Phenytoin
Carbamazepine
Valproic Acid

44

1st line for Complex partial?

Carbamazepine

45

1st line for simple partial?

carbamazepine

46

1st line for absence seizure?

ethosuximide

47

1st line for status epilepticus?

Acute tx-- loreazepam (or diazepam)
Prophylaxis-- phenytoin

48

MOA of Phenytoin?

inc Na channel inactivation (use-dependent blockade)
inhibits glutamate release from excitatory presynaptic neuron

49

Use of Phenytoin?

tonic-clonic (also simple partial, complex partial)
status epilepticus prophylaxis
*use Fosphenytoin if parenteral

Class 1B antiarrhythmic

50

MOA of Carbamazepine?

Inc Na channel inactivation

51

Use of Carbamazepine?

1st line for simple partial, complex partial, tonic-clonic, and trigeminal neuralgia

52

MOA of Lamotrigine?

blocks voltage-gated NA channels

53

Use of Lamotrigine?

Simple partial, complex partial, tonic-clonic

54

MOA of Gabapentin?

GABA analog
inhibits high-voltage-activated Ca channels

55

Use of Gabapentin?

simple partial, complex partial, tonic-clonic
peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder

56

MOA of Topiramate?

blocks Na channels
inc GABA action

57

Use of Topiramate?

simple partial, complex partial, tonic- clonic
migraine prevention

58

MOA of phenobarbital?

inc GABA-A Action

59

Use of Phenobarbital?

1st line in children w/ simple partial, complex partial, tonic-clonic

60

MOA of Valproic Acid?

inc Na channel inactivation
inc GABA concentration

61

Use of valproic acid?

1st line for tonic clonic
simple partial, complex partial, absence, and myoclonic seizures (can be used for all seizure types)

62

MOA of Ethosuximide?

blocks thalamic T-type Ca channels

63

Use of Ethosuximide?

absence seizures (1st line)

64

MOA of benzodiazepines in seizures?

inc GABA-A action

65

Use of Bezodiazepines in seizures?

1st line for acute status epilepticus
Use for eclampsia seizures (after 1st line MgSO4)

66

MOA of Tiagabine?

inhibits GABA reuptake

67

Use of Tiagabine?

simple & complex partial seizures

68

MOA of Vigabatrin?

irreversibly inhibits GABA transaminase to increase GABA

69

Use of Vigabatrin?

simple & complex partial seizures

70

MOA of Levetiracetam?

unknown
may modulate GABA and Glutamate release

71

Use of Levetiracetam?

simple & complex partial
tonic-clonic

72

Toxicity of benzodiazepines?

sedation
tolerance
dependence
induction of cytochrome p450

73

Toxicity of Carbamazepine?

Blood Dyscrasias (agranulocytosis & aplastic anemia)
Stevens-Johnson syndrome
Diplopia, Ataxia
liver toxicity
teratogenesis
induction of cytochrome p450
SIADH (dec Na)

74

Toxicity of Ethosuximide?

GI distress, fatigue, aggression
HA, uritcaria
Stevens-Johnson syndrome
may worsen generalized tonic-clonic seizures

75

Toxicity of Phenobarbital?

sedation
tolerance
dependence
induction of cytochrome p450

76

Toxicity of Phenytoin?

Gingival hyperplasia
Hirsutism/ Hypertrichosis
Teratogenesis (fetal hydantoin syndrome & inc risk of cleft palate)
Nystagmus & Diplopia (will develop tolerance)
megaloblastic anemia (dec folate absorption)
SLE-like syndrome
Ataxia
Sedation
induction of p450
lymphadenopathy
peripheral neuropathy
Stevens-Johnson syndrome

77

Toxicity of Valproic Acid?

Hepatotoxicty (rare but fatal-- measure LFTs)
Neural tube defects (spina bifida)-- Contra in pregnancy
GI distress
tremor, weight gain

78

Toxicity of Lamotrigine?

Stevens-Johnson syndrome
(increase dosage slowly)

79

Toxicity of Gabapentin?

Sedation
Ataxia

80

Toxicity of Topiramate

Weight loss = decreases appetite
Sedation
Kidney stones
Mental dulling

81

What are common barbiturates?

Phenobarbital
Pentobarbital
Thiopental
Secobarbital

82

What is the MOA of barbiturates?

facilitate GABA-A action by increasing DURATION of Cl channel opening thus decreasing neuron firing)

*BARBI (barbituates) likes it longer, BEN (benzodiazepines) wants it more often

83

What condition are barbiturates contraindicated in?

Porphyria

84

Clinical use of barbiturates?

sedative
(anxiety, seizures, insomnia, induction of anaesthesia-- thiopental)

85

Toxicity of Barbiturates?

Respiratory and cardiovascular depression (may be fatal)
CNS depression (exacerbated with BZD & ETOH use)
dependence
drug interactions (induces p450)

86

Antidote for Barbiturate OD?

supportive-- respiratory assistance & BP maintenance

87

What are common Benzodiazepines?

Diazepam
Lorazepam
Triazolam
Temazepam
Oxazepam
Midazolam
Chlordiazepoxide
Alprazolam

88

What is the MOA of Benzodiazepines?

facilitate GABA-A action by increasing the FREQUENCY of Cl channel opening
dec REM sleep
most have long-half lives

*Barbi likes it longer, Ben wants it more frequently

89

Short-half life benzodiazepines?

Triazolam
Oxazepam
Midazolam

*higher addictive potential

90

Clinical use of Benzodiazepines?

anxiety, spasticity, status epilepticus, detoxification (ETOH withdrawal/DT's), night terros, sleepwalking, general anethetic, hypnotic.

91

Toxicity of Benzodiazepines?

Dependence
additive CNS depression effects w/ ETOH & Barbs
Less coma & resp depression risk than Barbs

92

Antidone for OD?

Flumazenil
competitive antagonist at GABA benzodiazepine receptor

93

Nonbenzodiazepine Hypnotics

Zolpidem, Zaleplon, Eszopiclone

94

MOA of non-benzo hypnotics?

act via BZ-1 subtype of GABA receptor

95

clinical use of non-benzo hypnotics?

insomnia

96

Toxicity of non-benzo hyponotics?

ataxia, HA, confusion
rapid metab by liver enzymes = short duration of action
few amnestic events and modest day-after psychomotor depression
lower dependence risk than BZDs

97

Anesthetic drugs with low solubility in blood

rapid induction and recovery times
lower potency

98

Anesthetic drugs with high solubility in lipids

high potency = 1/ MAC
MAC = minimal alveolar concentration at which 50% of the population is anesthetized. varies with age

99

Inhaled anesthetics

halothane
enflurane
isoflurane
secoflurane
methoxyflurane
nitrous oxide

100

Effects of inhaled anesthetics?

unknown MOA
myocardial depression, respiratory depression, nausea/ emesis, inc cerebral blood flow (dec cerebral metabolic demand)

101

Toxicity of inhaled anesthetics?

Hepatotoxicity (halothane)
nephrotoxicity (methoxyflurane)
proconvulsant (enflurane)
malignant hyperthermia (all but nitrous oxide-- rare & life-threatening, inherited susceptibility)
expansion of trapped gas in body cavity (Nitrous oxide)

102

IV anesthetics?

Barbiturates (Thiopental)
Benzodiazepines (Midazolam)
Arylcyclohexylamines (ketamine-- PCP analogs)
Opioids (morphine & fentayl)
Propofol

103

Thiopental

barbiturate anesthetic
high potency-- high lipid solubility & rapid entry into brain
used for induction of anesthesia & short surgical procedures
effects terminated by rapid redistribution into tissue & fat
decreased cerebral blood flow

104

Midazolam

most common drug used in endoscopy
used adjunctively with gas anesthetics & narcotics
may cause severe post-op respiratory depression, dec BP (tx OD w/ Flumazenil) and amnesia

105

Ketamine/ PCP analogs

dissociative anesthetics
block NMDA receptors
Cardiovascular stimulants
cause disorientation, hallucination, and bad dreams
inc cerebral blood flow

106

Morphine & Fentanyl

used with other CNS depressants in general anesthesia

107

Propofol

sedation in ICU
rapid induction of anesthesia
short procedure anesthesia
less post-op nausea than thiopental
potentiates GABA-A

108

Local anesthetics

2 classes:
1) esters--- procaine, cocaine, tetracaine
2) amides--- lidocaine, mepivacaine, bupivacaine (all have 2 I's in name)

*if ester allergy, give amide

109

MOA of local anesthetics

blocks Na channels by dividing into specific receptors on inner portion of channel
preferentially bind to activated Na channels-- so most effective in rapidly firing neurons
tertiary amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form

110

Order of nerve blockade in local anesthetics?

small-diameter fibers > large-diameter fibers
myelinated fibers > nonmyelinated fibers
*size predominates over myelination status
sm myelinated > sm unmyelinated > lg myelinated > lg unmyelinated

111

Order of loss of sensations in local anesthetic?

1) pain
2) temperature
3) touch
4) pressure

112

What happens when you give local anesthetic at an infected tissue?

infected tissue is acidic
anesthetic is alkaline and charged (therefore cannot penetrate membrane as effectively)
*must give more anesthetic at infected tissues

113

What can you combine with local anesthetics to enhance local action?

vasoconstrictors (epinephrine)
decreases bleeding, increases anesthesia locally by decreasing systemic concentration

114

Clinical use of local anesthetics?

Minor surgical procedures
Spinal anesthesia

115

Toxicity of local anesthetics?

CNS excitation
severe cardiovascular toxicity (bupivacaine)
hypertension, hypotension & arrhythmias (cocaine)

116

What are neuromuscular blockade drugs used for?

muscle paralysis in surgery or mechanical ventilation
selective for motor nicotinic receptor (not autonomic)

117

What are the two types of neuromuscular blockade drugs?

Depolarizing (succinylcholine)
Nondepolarizing (Tubocurarine, etc)

118

What is the common depolarizing NM blocking drug?

Succinylcholine
(strong Ach receptor agonist)

119

What is the MOA of succinylcholine?

produces sustained depolarization and prevents muscle contraction

120

How does blockade reversal occur in succinylcholine?

2 phases:
Phase I-- prolonged deloparization.
no antidone. block potentiated by cholinesterase inhibitors.
Phase II-- repolarized but blocked (ACh receptors are available but desensitized)
antidote = neostigmine (cholinesterase inhibitors)

121

Complication of succinylcholine?

hypercalcemia
hyperkalemia
malignant hyperthermia

122

Common Non-depolarizing NM blocking drugs?

Tubocurarine
Atracurium
Mivacurium
Pancuronium
Vecuronium
Rocuronium

123

MOA of non-depolarizing NM blocking drugs?

competitive antagonists-- compete with ACh for receptors

124

Reversal of blockade by non-depolarizing NM blocking drugs?

neostigmine & edrophonium
(cholinesterase inhibitors)

125

MOA of Dantrolene?

prevents Ca release from sarcoplasmic reticulum of skeletal muscle

126

Clinical use of Dantrolene?

Treats malignant hyperthermia
(rare, but life-threatening S/E of succinylcholine & inhalation anesthetics-- except N2O.
Neuroleptic Malignant Syndrome (toxicity of antipsychotic drugs)

127

General Parkinson's Disease Drug strategies:

dopamine agonists
increase dopamine release
prevent dopamine breakdown
curb excess cholinergic activity

128

Dopamine agonists used in Parkinsons?

Bromocriptine* (ergot)
pramipexole
ropinirole (non-ergot)
(non-ergots are preferred)

129

Agents that Increase Dopamine release in Parkinsons?

Amantadine* (inc dopa release & also antiviral against influenza A & rubella)
L-dopa/Carbidopa* (converted to dopamine in CNS)

130

Agents that prevent Dopa breakdown in parkinsons?

Selegiline* (selective MAO-B inhibitor)
Entacapone, Tolcapone (COMT inhibitors-- prevent L-Dopa degradation = inc dopamine availability)

131

Agents that curb excess cholinergic activity in Parkinsons?

Benzotropine
(antimuscarininc that improves tremor & rigidity but has little effect on bradykinesia)

*PARK your mercedes-BENZ here.

132

Typical regimen in Parkinson's Disease?

Bromocriptine
Amantadine
Levodopa (+ Carbidopa)
Selegiline
Antimuscarinics

*BALSA

133

Toxicity associated with Amantadine?

ataxia

134

MOA of Levodopa/Carbidopa?

increases level of dopamine in the brain
unlike dopa, L-dopa can cross BBB and is converted by dopa decarboxylase in CNS to dopamine.
Carbidopa = peripheral decarboxylase inhibitor
given with L-dopa to increase brain bioavailability and limit peripheral side effects

135

Toxicity of Levodopa/Carbidopa?

Arrhythmias-- bc inc peripheral formation of catecholamines
Long term use = dyskinesia following administration & akinesia between doses

136

MOA of selegiline?

Selective inhibits MAO-B (which preferentially metabolizes dopamine over NE & 5-HT) = increase availability of dopamine

137

Toxicity of selegiline?

may enhance adverse effects of L-dopa (arrhythmia & dyskinesia with long term use)

138

Alzheimer's Drugs

Memantine
Donepezil, Galantamine, Rivastigmine

139

MOA of Memantine?

un-competitive NMDA receptor antagonist
helps prevent excitotoxicity (mediated by Ca & glutamate)

140

Toxicity of Memantine?

Dizzyness
Confusion
Hallucination

141

MOA of Dopepezil, Galantamine & Rivastigmine?

Acetylcholinesterase inhibitors = keep ACh levels up

142

Toxicity of Acetylcholinesterase inhibitors in Alzheimer's dz?

Nausea, diarrhea
dizziness, insomnia, urinary incontinence

143

Huntington's Treatment?

Tetrabenazine & Reserpine = inhibit VMAT (limit dopamine vesicle packaging & release)
Haloperidol- dopamine receptor antagonist

144

Sumatripin MOA

5-HT (1B/1D) agonist
inhibits trigeminal nerve activation
prevents vasoactive peptide release
induces vasoconstriction
half-life < 2 hrs

145

Clinical use of Sumatriptin?

Cluster HA attack
Acute Migraine

146

Toxicity of Sumatripin?

coronary vasospasm (CONTRA in CAD or Prinzmetal's Angina)
mild tingling

147

What is the MOA of alpha methyl tyrosine?

Inhibits tyrosine hydroxylase decreasing conversion of tyrosine to DOPA thereby inhibiting the rate-limiting step in catecholamine synthesis