IV - Topnotch Pharma Flash Cards - CNS Drugs Preview

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Flashcards in IV - Topnotch Pharma Flash Cards - CNS Drugs Deck (156):
1

bind GABA-A receptor subunits to increase frequency of chloride channel opening which causes membrane hyperpolarization

benzodiazepines (TOPNOTCH)

2

SE: anterograde amnesia, decreased psychomotor skills, unwanted daytime sedation, tolerance, dependence liability and rebound insomnia or anxiety

benzodiazepines (TOPNOTCH)

3

BZD that can be used for seizure disorders, Bipolar disorder and infantile spasm

Clonazepam (TOPNOTCH)

4

Why is Lorazepam preferred over Diazepam in status epilepticus

due to its long distribution halflife (TOPNOTCH)

5

date-rape drug

Flunitrazepam (TOPNOTCH)

6

BZD used for alcohol withdrawal

Diazepam and Chlordiazepoxide (TOPNOTCH)

7

antagonist at benzodiazepine sites on GABA-A receptor

Flumazenil (TOPNOTCH)

8

bind to GABA-A receptor sites to increase duration of chloride channel opening, block glutamic acid neurotransmission

barbiturates (TOPNOTCH)

9

which has greater dependence liability: barbiturates or benzodiazepine

barbiturates (TOPNOTCH)

10

Barbiturate with the highest lipid solubility

Thiopental (TOPNOTCH)

11

barbiturate for status epilepticus

Phenobarbital (TOPNOTCH)

12

SE: acute intermittent porphyria

barbiturates (TOPNOTCH)

13

High dose BZD and Barbs may suppress seizure but at the expenses of marked sedation EXCEPT for

Clonazepam and Phenobarbital (TOPNOTCH)

14

only interact with GABA-A receptors with alpha-1 subunit; For insomnia and sleep disorder esp when sleep onset is delayed

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

15

dependence liability and withdrawal symptoms is less than that of benzodiazepines

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

16

lack anti-convulsant, anti-anxiety and muscle relaxant effects, effects are reversed with Flumazenil, very rapid onset of action, may dec REM sleep

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

17

increasing use due to rapid onset with minimal effects on the sleep pattern and cause less daytime cognitive impairment as compared to BZD

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

18

partial agonist at 5-HT1A receptors and possibly D2 receptors, used For generalized anxiety disorders

Buspirone (TOPNOTCH)

19

slow onset of action (more than 1week), metabolized by CYP3A4, safe for pregnant patients

Buspirone (TOPNOTCH)

20

activates melatonin receptors (MT1 and MT2 receptors) in the suprachiasmatic nuclei in the CNS leading to dec latency of sleep onset

Ramelteon (TOPNOTCH)

21

block voltage-gated Na channel; DOC for generalized tonic-clonic seizures, DOC for partial seizures, can be used for migraine

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

22

SE: nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal hydantoin syndrome, abnormalities in Vit D metabolism

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

23

preferred in prolonged therapy for status epilepticus because it is less sedating

phenytoin (TOPNOTCH)

24

block voltage-gated Na channels and decreases glutamate release; DOC for trigeminal neuralgia, DOC for generalized tonic-clonic seizures, DOC for partial seizures, for bipolar disorders

Carbamazepine, Oxcarbazepine (TOPNOTCH)

25

SE: diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, Stevens-Johnson syndrome, erythematous rash, teratogen (spina bifida and craniofacial anomalies), hyponatremia

Carbamazepine, Oxcarbazepine (hyponatremia) (TOPNOTCH)

26

may be used for acute manic phase and as prophylaxis in the depressive phase

Carbamazepine, Oxcarbazepine (TOPNOTCH)

27

blocks high-frequency firing of neurons which modifies amino acid metabolism; DOC for bipolar disorder (acute mania), DOC for generalized tonic-clonic seizures and absence seizure, partial seizures, myoclonic seizures, also used for Bipolar disorders

Valproic acid (TOPNOTCH)

28

anti-manic that is CYP450 inhibitor

Valproic acid (TOPNOTCH)

29

for status epilepticus in children ; primary anticonvulsant in infants, children and pregnant patients

Phenobarbital (TOPNOTCH)

30

inhibit low threshold (T-type) Ca currents esp in thalamic neurons ; DOC for absence seizure

Ethosuximide, Phensuximide, Methsuximide (TOPNOTCH)

31

blocks Ca channels, increases GABA release ; For neuropathic pain such as postherpetic neuralgia, partial seizures, migraine

Gabapentin, Pregabalin (TOPNOTCH)

32

structural analogues of GABA but does not activate GABA receptor directly ; also have the same effect on Ca currents like Ethosuximide

Gabapentin, Pregabalin (TOPNOTCH)

33

blocks Na and Ca channels and decreases glutamate, used for acute manic phase and as prophylaxis in the depressive phase

Lamotrigine (TOPNOTCH)

34

primarily undergoes glucuronidation reaction ; SE: dizziness, ataxia, nausea, rash, SJS / TEN

Lamotrigine (TOPNOTCH)

35

Bind synaptic protein selectively inhibiting hypersynchronization of epileptiform burst firing ; For generalized tonic-clonic seizures, partial seizures

Levetiracetam (TOPNOTCH)

36

not metabolized by CYP450 enzymes, eliminated in the kidneys in their unchanged form

Levetiracetam (TOPNOTCH)

37

multiple actions on synaptic function, probably via actions on phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic anhydrase)

Topiramate, Felbamate (TOPNOTCH)

38

also facilitate the inhibitory actions of GABA but its exact MOA is still unknown

Felbamate (TOPNOTCH)

39

Antiseizure drugs with the most number of MOA, undergo both hepatic and renal metabolism

Topiramate, Felbamate (TOPNOTCH)

40

Irreversibly inactivates GABA aminotransaminase (GABA-T) which terminates the action of GABA ; For GTC seizure

Vigabatrin (TOPNOTCH)

41

Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its reuptake, leading to prolongation of GABA effects ; For partial seizures

Tiagabine (TOPNOTCH)

42

SE: visual field defects

Vigabatrin (TOPNOTCH)

43

Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N receptors

Inhalational anesthetics (TOPNOTCH)

44

SE: megaloblastic anemia on prolonged exposure; Euphoria (laughing gas), bronchodilation

Nitrous Oxide (TOPNOTCH)

45

Lowest Potency (highest MAC) and least cardiotoxic

Nitrous Oxide (TOPNOTCH)

46

all inhaled anesthetcis cause bronchodilation except

Desflurane (TOPNOTCH)

47

SE: catecholamine-induced arrhythmias, peripheral vasodilation, bronchodilation

Isoflurane (TOPNOTCH)

48

SE: spike-and-wave activity in EEG, muscle twitching, breath-holding, myocardial depression, renal insufficiency (due to Flourine release), dec cardiac output, bronchodilation

Enflurane (TOPNOTCH)

49

has pungent odor which limits its use

Enflurane (TOPNOTCH)

50

SE: catecholamine-induced arrhythmias, myocardial depression, post-operative hepatitis, dec cardiac output, bronchodilation

Halothane (TOPNOTCH)

51

Highest potency and lowest MAC (very slow onset and recovery)

Methoxyflurane (TOPNOTCH)

52

a usual adjunct with inhalational anesthetics and IV opioids, has a slow onset but longer DOA

Midazolam (TOPNOTCH)

53

Blocks excitation by glutamate at NMDA receptors; For dissociative anesthesia (analgesia, amnesia and catatonia but with retained consciousness)

Ketamine (TOPNOTCH)

54

congener of Phencyclidine / angel dust

Ketamine (TOPNOTCH)

55

For general anesthesia to patients with limited cardiac or respiratory reserve

Etomidate (TOPNOTCH)

56

Interacts with mu, sigma, kappa receptors for endogenous opioid peptides ; For high risk patients who might not survive general anesthesia

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

57

SE: respiratory depression, chest wall rigidity (which may cause impaired ventilation) and constipation

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

58

Antidote is Naloxone / Naltrexone

Opioid toxicity (TOPNOTCH)

59

milk of anesthesia

Propofol, Fospropofol (TOPNOTCH)

60

Potentiates GABA-A receptors, blocks Na channels; For prolonged sedation esp in ICU patients and also in OPD surgeries

Propofol, Fospropofol (TOPNOTCH)

61

Blockade of Na channels slows which prevents axon potential propagation

Local Anesthetics (TOPNOTCH)

62

Shortest half-life among local anesthetics

Procaine (TOPNOTCH)

63

For local anesthesia, topical anesthesia

Benzocaine, Cocaine, Tetracaine (TOPNOTCH)

64

Use cautiously in sunburns, Topical only

Benzocaine (TOPNOTCH)

65

with intrinsic sympathomimetic activity so it does not need an alpha agonist (like epinephrine) to limit its systemic absorption

Cocaine (TOPNOTCH)

66

All local anesthetics are vasodilators EXCEPT

Cocaine (TOPNOTCH)

67

SE: light-headedness, sedation, restlessness, nystagmus, seizures, respiratory, CV depression, abuse liability, severe hypertension, cerebral hemorrhage, cardiac arrhythmia, MI

Cocaine (TOPNOTCH)

68

For local anesthesia, spinal anesthesia, epidural anesthesia, topical ophthalmic anesthesia

Tetracaine (TOPNOTCH)

69

Blockade of Na channels slows which prevents axon potential propagation; For local anesthesia, antiarrythmia (group 1B activity), used for post-MI and for digitalis toxicity

Lidocaine (TOPNOTCH)

70

For local anesthesia, dental anesthesia

Prilocaine (TOPNOTCH)

71

local anesthetic that can cause methemoglobinemia

Prilocaine (TOPNOTCH)

72

For local anesthesia, epidural anesthesia, intrathecal anesthesia

Bupivacaine (TOPNOTCH)

73

Use with caution in pregnant women and patients with cardiac disease (may cause heartblock, arrhyhtmia and hypotension)

Bupivacaine (TOPNOTCH)

74

Longest half-life among local anesthesia

Ropivacaine (TOPNOTCH)

75

Depolarizing Neuromuscular Blocker

Succinylcholine (TOPNOTCH)

76

Agonist at Ach-N receptors causing initial twitch then persistent depolarization

Succinylcholine (TOPNOTCH)

77

SE: muscle pain, hyperkalemia, increased intragastric pressure leading to regurgitation (aspiration), increased intraocular pressure, malignant hyperthermia

Succinylcholine (TOPNOTCH)

78

Metabolized by pseudocholinesterase ; may cause malignant hyperthermia if given together with inhaled anesthetics

Succinylcholine (TOPNOTCH)

79

a common SE for this group is Histamine release

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

80

Undergoes Hoffman elimination (rapid spontaneous breakdown)

Atracurium (TOPNOTCH)

81

converted to Laudanosine which can cause seizures

Atracurium (TOPNOTCH)

82

short-acting Non-Depolarizing Neuromuscular Blocker

Mivacurium (TOPNOTCH)

83

intermediate-acting Non-Depolarizing Neuromuscular Blocker ; Undergoes elimination in bile

Vecuronium (TOPNOTCH)

84

Suggamadex is a novel reversal agent for

Rocuronium (TOPNOTCH)

85

Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors; For skeletal muscle relaxation during intubation and general anesthesia

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

86

long-acting Non-Depolarizing Neuromuscular Blocker; may cause heart block

Pancuronium (TOPNOTCH)

87

Relatively contraindicated in myocardial ischemia; reverse effects with neostigmine

Tubocurarine (TOPNOTCH)

88

a dopamine precursor

Levodopa (TOPNOTCH)

89

inhibits peripheral metabolism via dopa decarboxylase

carbidopa (TOPNOTCH)

90

SE: GI upset (emesis), dyskinesia (choreoathetosis), behavioural changes (anxiety, agitation, confusion, delusion), on-off phenomena, wearing-off phenomena, postural hypotension, tachycardia

Levodopa-carbidopa (TOPNOTCH)

91

Partial agonist at dopamine D2 receptors in brain

Bromocriptine, Pergolide (TOPNOTCH)

92

For Parkinson's disease which is levodopa intolerance, hyperprolactinemia

Bromocriptine, Pergolide (TOPNOTCH)

93

SE: anorexia, n/v, dyskinesia, postural hypotension, behavioural changes, erythromelalgia, pulmonary infiltrate

Bromocriptine (TOPNOTCH)

94

Partial agonist at dopamine D3 receptors in brain

Pramipexole (TOPNOTCH)

95

SE: Contraindicated for patients with active peptic ulcer disease, psychotic illnesss or recent MI

Pramipexole, Ropinirole (TOPNOTCH)

96

Partial agonist at dopamine D3 receptors, antagonist at 5-HT and alpha adrenoceptors

Apomorphine (TOPNOTCH)

97

For off-periods of Parkinson's disease, alcoholism, opiate addiction, erectile dysfunction, alzheimer's disease

Apomorphine (TOPNOTCH)

98

Selective inhibitors of MAO type B leading to decreased degradation of dopamine, increases response to levodopa/carbidopa

Selegiline, Rasagiline (TOPNOTCH)

99

Block L-dopa metabolism by inhibiting catechol-O-methyltransferase in periphery and CNS, prolongs response to levodopa

Entacapone, Tolcapone (TOPNOTCH)

100

T or F: Entacapone only acts in the periphery while Tolcapone acts both in the periphery and CNS

TRUE (TOPNOTCH)

101

enhances dopaminergic transmission by unknown mechanism, maybe by influencing the synthesis, release or reuptake of dopamine

Amantadine (TOPNOTCH)

102

SE: behavioral changes (restlessness, agitation, insomnia, hallucination, psychosis), livedo reticularis, GI disturbances, urinary retention, postural hypotension, peripheral edema

Amantadine (TOPNOTCH)

103

Decrease the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

104

as adjunct for parkinson's disease and extrapyramidal symptoms caused by antipsychotics

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

105

Blocks D2 receptos more than 5-HT2 receptors

Typical Antipsyhotics (TOPNOTCH)

106

Typical Antipsychotic, SE: retinal deposits and arryhthmias

Thioridazine (TOPNOTCH)

107

has the Strongest autonomic effects; only antipsychotic with fatal overdose

Thioridazine (TOPNOTCH)

108

For schizophrenia and other psychotic disorders, huntington's disease and tourette's syndrome

Haloperidol, Droperidol (TOPNOTCH)

109

SE: extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, neuroleptic malignant syndrome

Haloperidol, Droperidol (TOPNOTCH)

110

Only antipsychotic that reduces the risk of suicide

Clozapine (TOPNOTCH)

111

For schizophrenia (refractory, suicidal) and other psychotic disorders

Clozapine (TOPNOTCH)

112

Blocks 5-HT2 receptors more than D2 receptors

Atypical Antipsychotics (TOPNOTCH)

113

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, hyperglycemia, hyperlipidemia, myocarditis, agranulocytosis, seizures, ileus, hypersalivation (sialotthea)

Clozapine (TOPNOTCH)

114

weight gain and hyperglycemia is prominent, safe in pregnancy

Olanzapine (TOPNOTCH)

115

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, somnolence, fatigue, sleep paralysis, hypnagogic hallucinations, cataracts, priapism, QT prolongation (TDP) ; safe in pregnancy

Quetiapine (TOPNOTCH)

116

Only antipsychotic approved for schizophrenia in the youth

Risperidone (TOPNOTCH)

117

Increased mortality in elderly patients with dementia-related psychosis ; can cause TDP

Ziprasidone (TOPNOTCH)

118

Least sedating atypical antipsychotics

Aripiprazole (TOPNOTCH)

119

Uncertain MOA but the proposed MOA is by inhibiting the enzyme involved in the recycling of neuronal membrane phosphoinositides which causes depletion of phosphatidylinositol bisphosphate, thus consequently decreasing IP3 and DAG leading to decreased neurotransmission

Lithium (TOPNOTCH)

120

SE: Tremor, sedation, ataxia, aphasia, thyroid enlargement, hypothyroidism, reversible nephrogenic diabetes insipidus, edema, acneiform skin eruption, leukocytosis, teratogen (ebstein's anomaly), bradycardia

Lithium (TOPNOTCH)

121

Block NE and 5-HT transporters leading to potentiation of NT action at postsynaptic receptors

Tricyclic Antidepressants (TOPNOTCH)

122

Tricyclic Antidepressants

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

123

For MDD (most effective), bipolar disorder, acute panic attacks, ADHD, chronic pain states, as sleeping aid, OCD ; this group is very useful for patients with psychomotor retardation, sleep disturbance, poor appetite and weight loss

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

124

3Cs of TCA overdose

Coma, Cardiotoxicity, Convulsions (TOPNOTCH)

125

longterm use may lead to down-regulation of Beta receptors leading to a decrease in BP and depression of cardiac conduction

Tricyclic Antidepressants (TOPNOTCH)

126

Inhibits neuronal reuptake of serotonin by inhibiting Serotonin Transporter (SERT)

SSRI (TOPNOTCH)

127

SSRIs

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

128

DOC for OCD, for MDD, anxiety, panic attacks, phobias, PTSD, GAD, bulimia, premenstrual dysphoric disorder, alcohol dependence

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

129

This antidepressant group can decrease appetite leading to weight loss

SSRI (TOPNOTCH)

130

Inhibits neuronal reuptake of serotonin and norepinephrine by binding to transporters for both 5HT and NE

SNRI (TOPNOTCH)

131

SNRIs

Venlafaxine, Duloxetine, Desvenlafaxine (TOPNOTCH)

132

differ from TCA in lacking blockade of H1, M and alpha receptors ; Increased risk for suicide in children and adolescents

SNRIs (TOPNOTCH)

133

Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT transporters

Serotonin antagonist (TOPNOTCH)

134

Antidepressant Serotonin antagonist

Trazodone, Nefazodone (TOPNOTCH)

135

Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor, blocks dopamine D2 receptors

Tetracyclics: Amoxapine (TOPNOTCH)

136

Increases amine release from nerve endings by antagonism of presynaptic a2 adrenoceptors, also blocks serotonin 5-HT2A receptors

Tetracyclics: Mirtazapine (TOPNOTCH)

137

Inhibits neuronal reuptake of dopamine and norepinephrine, increase dopamine and norepinephrine activity

Tetracyclics: Bupropion (TOPNOTCH)

138

Inhibits MAO type A and type B, increases CNS levels of NE and serotonin

Phenelzine, tranylcypromine (TOPNOTCH)

139

MAO-B selective inhibitor

Selegiline (TOPNOTCH)

140

Triad of opioid overdose

miosis, coma, respiratory depression (TOPNOTCH)

141

Strong agonist at u receptors; For severe pain, pain associated with acute MI, for pulmonary edema

Morphine (TOPNOTCH)

142

morphine is metabolized in the body to _____ which has equal analgesic activity as morphine

morphine-6-glucuronide (TOPNOTCH)

143

Strong agonist at u receptors; For severe pain, adjunct in anesthesia, chronic pain and breakthrough cancer pain

Fentanyl (TOPNOTCH)

144

Strong agonist at u and k receptors, inhibits pain neurotransmission, muscarinic blocking actions; For moderate to severe pain, labor analgesia, spasmodic pain (biliary, renal), preoperative sedation

Meperidine (TOPNOTCH)

145

Only opioid that does not cause miosis and biliary contraction

Meperidine (TOPNOTCH)

146

opioid of choice for pain relief in pancreatitis

Meperidine (TOPNOTCH)

147

metabolized to normeperidine which can cause _____ therefore contraindicated in patients with ______

seizure, seizure disorder (TOPNOTCH)

148

full opioid agonist, Strong agonist at u receptors, inhibits pain neurotransmission, binds NMDA receptors and antagonizes the effects of glutamate; For moderate to severe pain, opioid dependence, opioid withdrawal

Methadone (TOPNOTCH)

149

used as maintenance therapy for opioid dependence

Methadone (TOPNOTCH)

150

Decreases sensitivity of cough receptors, depressing the medullary cough center through sigma receptors stimulation; For cough suppression

Dextrometorphan, codeine (TOPNOTCH)

151

codeine is metabolized by CYP2D6 to ______

morphine (TOPNOTCH)

152

SE: miosis, restlessness, respiratory depression, increased ICP, postural hypotension, urinary retention, pruritus, addiction liability

Opioid analgesics (TOPNOTCH)

153

Mixed Agonist-Antagonist: Strong agonist at k receptors, weak antagonist activity at u receptors

Nalbuphine, buprenorphine, butorphanol, pentazocine (TOPNOTCH)

154

Weak agonist at u receptors, inhibits pain neurotransmission; For mild to moderate pain, restless leg syndrome

Propoxyphene, levopropoxyphene, dextropropoxyphene (TOPNOTCH)

155

Competitively blocks u, sigma and k receptors, rapidly reverses effects of opioid agonists; For opioid overdose, opioid and alcohol dependence

Naloxone, naltrexone, nalmefene (TOPNOTCH)

156

Weak agonist at u receptors, inhibits neuronal reuptake of serotonin and norepinephrine; For moderate pain, chronic pain syndrome, neuropathic pain

Tramadol (TOPNOTCH)