EXAM #3: REVIEW Flashcards Preview

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Flashcards in EXAM #3: REVIEW Deck (132):
1

What sedative drug classes are "selective" CNS depressants?

1) Barbiturates
2) Benzodiazepines
3) Ethanol

2

Outline the progression of dose-dependent effects seen with the sedative hypnotics.

1) Sedation
2) Sleepiness
3) Anesthesia
4) Coma
5) Respiratory depression/ death

3

List the six clinical indications for the sedative hypnotics.

1) Anxiety
2) Insomnia
3) Amnesia-induction
4) Seizures
5) Ethanol withdrawal
6) Muscle relaxation

4

What are the two suffixes associated with the Benzodiazepines?

- "zepam"
- "zolam"

5

What are the two benzodiazepines that undergo metabolism to weakly active, short lived metabolites with intermediate duration of action?

- Alprazolam
- Triazolam

6

What effects are associated with Alpha-1 GABA receptor agnoism?

1) Sedation
2) Anticonvulsant
3) Anterograde amnesia

7

What effect is associated with Alpha 2,3, and 5 GABA receptor agonism?

Anxiolysis

8

What are the five adverse effects associated with benzodiazepines?

1) Respiratory depression
2) Anterograde amnesia
3) Tolerance
4) Dependence
5) Withdrawal

9

What drug classes will cause additive CNS depression when combined with benzodiazepines?

1) Ethanol
2) Opoids
3) Anticonvulsants
4) Phenothiazine
5) Antihistamines
6) TCAs

10

List the four indications for Barbiturates.

1) Anticonvulsant
2) Sedative-hypnotic
3) Anesthesia
4) Medically induced coma

11

List the three common side effects of the MAOIs.

- Orthostatic hypotension
- Weight gain
- Sexual dysfunction

12

What are TCAs first line therapeutic agents for?

Chronic pain

13

What are TCAs second line therapeutic agents for?

Major depression

14

What TCA is used to treat neuropathic pain?

Desipramine

15

What TCA has the most sedative effects?

Amitriptytline

16

What is the MAJOR side effect to remember as being associated with the TCAs?

Cardiac toxicity i.e. induction of lethal cardiac arrhythmias

17

What are all of the side effects of the TCAs?

1) Cardiac toxicity
2) Orthostatic hypotension
3) Delirium in the elderly
4) Sexual dysfunction

18

What is important to remember about the safety of SSRIs compared to other antidepressants?

SSRIs are much safer than MAOIs or TCAs

19

What symptoms compose the triad of Serotonin Syndrome?

1) AMS
2) Autonomic hyperactivity
3) Neuromuscular abnormalities

20

What is the MOA of Venlafaxine?

SNRI

21

What receptor does Venlafaxine have its major effect on? Minor?

Major= SERT
Minor= NET

22

What is the clinical indication for Venlafaxine?

Severe Depression

23

What is the MOA of Duloxetine?

SNRI with balance SERT and NET inhibition

24

What is the primary clinical indication for Duloxetine?

Chronic pain (increasingly prescribed over the TCAs i.e. Desipramine)

25

What is the MOA of Trazadone?

Antihistamine (H1 antagonist)

26

What is the primary clinical indication for Trazadone?

Depression + insomnia (unlabeled)

27

What is the MOA of Buproprion?

1) NE/ DA reuptake inhibitors
2) Increases catecholamine release

28

What are the clinical indications for Bupropion?

1) Major depression
2) Smoking cessation

29

What drug class does Mirtazapine fall under?

TCA

30

What is the MOA of Mirtazapine?

1) TCA (SERT and NET inhibitor)
2) Alpha-2 antagonist
3) Antihistamine (H1)
4) 5-HT2/3 antagonist

31

List the three antidepressants that are potent CYP2D6 inhibitors.

- Paroxetine
- Fluoxetine
- Fluvoxamine

32

What two anticonvulsants are prescribed for Bipolar Disorder?

1) Valproate
2) Carbamazepine

33

What is the MOA of Lithium?

Decreases the post-synaptic response to NE and 5-HT by:
- Decreasing cAMP
- Decreasing IP3

34

What are the four major side effects associated with Lithium?

1) Tremors
2) Hypothyroid
3) Nephrogenic Diabetes Insipidus
4) Skin reactions

35

What is the most common type of partial seizures?

Complex partial

36

What is an absence of Petit Mal seizure?

A seizure that is characterized by:
- Brief LOC
- Some motor signs/ automatisms

*More common in children

37

What are the three molecular events underlying EPSPs?

1) Na+ influx
2) Ca++ influx
3) Paroxysmal Depolarization

38

What drugs are best for treating absence/ petite mal seziures?

Ethosiximide
Valproate

39

What drugs are best for treating myoclonic seizures?

Clonazepam
Valproate

40

What drugs are best for treating Status Epilepticus?

Diazepam
Lorazepam
Phenytoin
Fos-phenytoin

41

List the adverse effects associated with anticonvulsant agents.

1) Sedation
2) Diplopia
3) Nystagmus
4) Ataxia
5) GI disturbances

42

What two things do you need to remember about anticonvulsant therapy in women?

1) Anticonvulsants decrease the efficacy of oral contraceptives
2) Anticonvulsants are teratogenic

43

What are the three elements of the Phenytoin MOA?

1) Na+ channel blocker
2) Enhanced GABA release
3) Decreased Glutamate release

*Generally prevents seizure propagation*

44

What are the clinical indications for Phenytoin?

1) Gran mal seizures
2) Partial seizures
3) Status epilepticus

45

What is the MOA of Carbamazepine in regards to its anticonvulsant effects? What drug class does Carbamazepine fall into?

Carbamazepine is TCA that also:
- Blocks Na+ channels --anticonvulsant

46

What is Oxcarbazepine?

Carbamazepine analog that has fewer side effects

47

List the clinical indications for Carbamazepine.

1) General (tonic-clonic) seizures
2) Partial seizures
3) Manic phase of bipolar phase (acute)

AND

4) TRIGEMINAL NEURALGIA

48

What unique side effect is associated with Carbamazepine?

SIADH

49

What are the clinical indications for phenobarital?

1) Neonatal seizures
2) Seizures in pregnancy
3) Status epilepticus

50

What is the unique side effect associated with Valproate?

Hepatotoxicicty

51

What is the MOA of Lamotrigine?

Na+ and Ca++ channel antagonist

52

What is the MOA of Felbamate?

Na+ and Glutamate receptor antagnoist

53

What are the adverse effects associated with Felbamate?

1) Aplastic anemia
2) Liver failure

54

What is the MOA of Tiagabine?

Inhibits GABA uptake

55

What is the difference between GABA-A and GABA-B receptors?

GABA-A= Cl- ion channel

GABA-B= GPCR that increases K+ conductance on stimulation

56

What are the six characteristics of an ideal anesthetic?

1) Unconsciousness
2) Amnesia
3) Analgesia
4) Skeletal muscle relaxation
5) Areflexia
6) Good minute-to-minute control

57

What are the four phases of anesthesia?

1) Induction
2) Maintenance
3) Emergence
4) Recovery

58

What are the stages of anesthesia?

1) Analgesia
2) Excitement
3) Surgical anesthesia
4) Medullary depression

59

What are the three general mechanisms of action of general anesthetics?

1) Increased GABA-A activity
2) Activation of K+ channels
3) Inhibition of NMDA receptors

60

What clinical scenario will cause a decreased MAC value?

Presence of CNS depressants

61

What are the three major drawbacks to NO?

1) Lack of potency (110% MAC value)
2) Diffusion hypoxia
3) Increased risk of spontaneous abortion

62

List the halogenated anesthetic agents.

1) Halothane
2) Enflurane
3) Isoflurane
4) Desflurane

63

What major adverse effect is associated with Halothane?

Hepatitis

64

What major side effect is associated with Enflurane?

CNS stimulant effects

65

What drug class does Thiopental fall into?

Barbiturate (used for anesthesia induction)

66

What is the MOA of Ketamine?

NMDA antagonist

67

What type of local anesthetic, protonated (LAH) or non protonated (LA) is more lipophilic? Which binds the internal portion of Na+ channels with higher affinity?

LA= more lipophilic
LAH+= binds Na+ channels with higher affinity (internally)

68

Which type of LA has a longer half-life, amides or ester?

Amides have a longer half-life

69

Which type of LA is metabolized in the liver? Blood?

- AmIdes-- with 2x i's--are metabolized in the lIver
- Esters-- with 1x i-- are metabolized in the blood

70

What is the Cm?

Minimum anesthetic concentration for standard block in 50% of the population

71

List the amide type LAs.

Lidocaine
Bupivicaine
Ropivacaine
Articaine

72

List the ester type LAs.

Cocaine
Procaine
Tetracaine
Benzocaine
Chloroprocaine

73

What is the clinical utility of Benzocaine?

This is an ester-LA that has enhanced lipid solubility--it can be used topically

74

What is the clinical utility of Chloroprocaine?

This is an ester-LA that is used as an epidural agent in labor b/c:
- Low risk of systemic toxicity
- Low risk of fetal exposure

75

What is Exparel-Liposome? What is it used for?

- Encased Bupivacaine (amide LA) w/ extended half-life
- Provides up to 72 hours of post-op pain relief

76

What are the four clinical indications for antipsychotic medications?

1) Schizophrenia
2) Psychotic behavior
3) Severe mania
4) Antiemetic

77

List the typical antipsychotics.

Chlorpromazine
Thioridazine
Fluphenazine
Haloperiodol

78

List the atypical antipsychotics.

Clozapine
Olanzapine
Risperiodone
Aripiprazole
Quetiapine
Zisprasidone

79

What is the difference between the metabolism of the typical and atypical antipsychotics?

Typical= metabolism into an INACTIVE metabolite

Atypical= metabolism into an ACTIVE metabolite

80

What receptor/s is primarily antagonized by typical antipsychotics? Atypical?

Typical= D2
Atypical D2 + 5-HT2A

81

What antipsychotic is associated with high 5-HT2A affinity?

Clozapine

82

List the subtypes of extrapyramidal symptoms.

1) PD-like Syndrome
2) Akathesia
3) Dystonia
4) Tardive Dyskinesia

83

List the four most common reasons that patients will stop taking antipsychotics.

1) Lack of efficacy
2) Cannot tolerate side effects in general
3) Weight gain
4) Sexual dysfunction

84

List the five hallmark cognitive symptoms of AD.

1) Loss of short-term memory
2) Disorientation
3) The A's
- Aphasia
- Apraxia
- Agnosia

85

Describe the pathologic changes that underly the development of the AD phenotype specifically in regards to Beta-amyloid.

1) ABPP or Amyloid Precursor Protein is cleaved into Beta-Amyloid
2) There is an IMBALANCE between Beta-Amyloid production and clearance
3) Beta-amyloid accumulates and is TOXIC to neurons

86

What is the function of "Presenilin?"

Presenilin cleaves Amyloid Precursor Protein

87

What are the consequences of neurofibrillary tangles in AD?

1) Microtubular disintegration and instability
2) Collapse of the neuronal transport system
3) Altered neurotransmitter release
4) Cell death

88

List the four drugs that are used as first line agents in AD. What drug class do they belong to?

Cholinesterase inhibitors:
1) Tacrine
2) Donepezil
3) Rivastigmine
4) Galantamine

89

What adverse effect of Tacrine limits its clinical use today?

Hepatotoxicity

*Also has a v. short half-life and had to be dosed 4x per day

90

Which first line agent for AD can be given as a transdermal patch? What are the clinical implications?

Rivastigmine can be given transdermally
- Limits the adverse GI disturbances

91

What is the MOA of Memantine?

Non-competitive NMDA antagonist

92

What class of antidepressants are contraindicated in the treatment of depression in AD patients?

TCAs--alpha-1 effects have an increased risk for orthostatic hypotension and falls

93

What are the four cardinal symptoms of PD?

1) Bradykinesia
2) Muscular rigidity
3) Resting tremor
4) Postural instability

94

What are the adverse effects associated with L-DOPA administration in PD?

1) Dyskinesia
2) Response fluctuations
3) Postural hypotension/tachycardia
4) Behavioral disturbance
5) GI disturbances

95

What is the drug interaction between L-DOPA and the antipsychotics?

- L-DOPA is aiming to increase DA concentrations
- Antipsychotics are D2 ANTAGONISTS

Thus, the drugs counteract each other.

96

List three DA receptors agonists that are used to treat PD.

Pramipexole
Ropinirole
Apomorphine

97

List the two MAO-B receptor antagonists used to treat PD.

Rasagiline
Selegiline

98

List the two COMT inhibitors used to treat PD.

Entacapone
Tolcapone

99

What is the MOA of Amantadine to treat PD?

Increased DA release

100

What adverse effect is associated with Amantadine?

Livedo Reticularis

101

List the two anticholinergic agents used to treat PD.

Benztropine
Trihexyphenidyl

102

Name the three endogenous opioids.

Endorphins
Enkephalins
Dynorphins

103

What is the difference between Mu1 and Mu2 receptors?

Mu1= outside the CNS
Mu2= inside the CNS

104

How does agonism of Mu opioid receptors produce analgeisa?

1) Mu opioid receptors are GPRCs coupled to Gi subunits
2) Activation causes decreased adenylyl cyclase
3) Decreased adenylyl cyclase causes decreased cAMP

The final result is LESS intracellular Ca++ and increased K+ conductance i.e. INHIBITION

105

List five clinical indications for opioids.

1) Analgesia
2) Anesthesia
3) Anti-tussive
4) Anti-diarrheal
5) Acute pulmonary edema

106

What class of drugs are contraindicated with opioids?

MAOIs

107

List the "strong" opioids.

Morphine
Hydromorphone
Oxymorphone
Methadone
Fentanyl
Sufentanil
Meperidine
Heroin

108

List the mixed opioid agonist-antagonists.

Bupreneorphine
Butorphanol
Nalbuphine
Pentazocine

109

List the "other" opoid agonists.

Dextromethorphan
Diphenoxylate
Loperamide
Tramadol

110

What effects will CNS stimulants produce?

1) Alterness
2) Productivity and motivation
3) Arousal
4) Euphoria
5) Nervousness and anxiety

111

What is Methylxanthine?

- CNS/ Respiratory stimulant
- Derivative of xanthine

112

What are the clinical indications for Theophylline?

- COPD
- Asthma

*Note that this drug has bronchodilator properties*

113

List the sympathomimetic amide stimulants.

1) Amphetamine analogs including:
- Methamphetamine
- Dexamphetamine
- Methylphenidate
2) Cocaine
3) Modafinil
4) Atomoxetine

114

How are the amide psychomotor stimulants metabolized?

1) MAO
2) CYP p450

115

What classes of drugs will have adverse interactions with CNS stimulants?

MAOIs
SSRIs

116

List the CNS related side effects seen with the psychomotor stimulants.

Euphoria
Dysphoria
Insomnia
Irritability
Tremor
Headache
Anorexia

117

List the stimulant drugs that are used to treat ADHD.

Methylphenidate
Amphetamine salts (adderall)
Dextroamphetamine

118

List the non-stimulant drugs that can be prescribed for ADHD.

1) Atomoxetine
2) Clonidine
3) Modafininl
4) Antidepressants
- TCAs
- MAOIs
- Bupropion

119

List the psychological manifestations of drug withdrawal.

- Dysphoria
- Depression
- Anxiety
- Craving
- Psychosis

120

What are the three drugs "targets" of the VTA?

1) Gi GPCRs that inhibit GABA
2) Inonotropic DA receptors
3) DA uptake transporter

121

What drugs act on ionotropic DA receptors in the VTA?

1) Benzodiazepines
2) Nicotine
3) Alcohol

122

What is the MOA of GHB?

Disinhibition of GABA-B receptors in the VTA

123

What are the side effects associated with Methamphetamine use?

Methamphetamine is sympathomimetic, thus:
- Mydriasis
- Tachycardia
- Hypertension

124

What is the MOA of MDMA?

1) SERT Antagonism
2) Increases the release of 5-HT

125

Wha toxicity is associated with MDMA?

Acute hyperthermia and dehydration

126

List the Psychedelcis.

1) LSD
2) Psilocybin
3) Ketamine
4) Phecyclidine

127

What is the MOA of LSD and Psilocybin?

- Increase glutamate release
- 5-HT2A agonist

128

What is the MOA of Ketamine and PCP?

NMDA antagonists

129

What is the RR of opioid addiction?

4

130

List the four most commonly abused opioids.

1) Codeine
2) Heroin
3) Morphine
4) Oxycodone

131

What is the MOA of euphoria seen in opioid use?

1) Activation of Mu opioid receptors
2) Inhibition of GABAnergic neurons in the VTA

Result in disinhibition of VTA DA neurons

132

What is the MOA of THC?

Blocks GABA-A receptors on DA neurons in the VTA

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