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Quarter 4 > pharm exam 1 > Flashcards

pharm exam 1 Flashcards

1
Q

TCAs

antidepressant

A

Inhibit reuptake of NE and 5-HT

BUT also block alpha, histamine, and muscarinic receptors –> many SE

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2
Q

TCAs, careful with

A

SI, potential for OVERDOSE

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3
Q

TCAs are used minimally in depression, but also used for:

A

Chronic pain (TMJ)
Fibromyalgia
Enuresis (bedwetting)

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4
Q

TCA toxicity

A

Histamine rec block: drowsy, fatigue, sedation

Cholinergic rec block: blurry vision, tachycardia, urinary retention, dry mouth, memory loss

alpha rec block: cardiac arrhythmia, hypotension, reflex tachycardia

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5
Q

Other SE of TCA

A

Sexual dysfx
SIADH
Weight gain

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6
Q

Can TCA be used in pregnancy?

A

YES, surprisingly

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7
Q

Serious toxicity of TCA

A

Torsades de pointes!!!!!

prolonged QT
Met acidosis
Resp depression
Coma, shock

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8
Q

Tx of OD on TCA

A 
Cardiac monitor
Lavage
Charcoal
Mg, Isoproterenol, Cardiac pacing for Torsades de pointe
Lidocaine, Propranolol, Phenytoin

Na bicarb and KCl

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9
Q

TCAs are either

A

Tertiary or Secondary amaines

Tertiary cause more seizures and are more sedating

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10
Q

Tertiary amines (TCA)

A

Amitriptyline
Imapramine

block 5HT reuptake (seretonin)

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11
Q

Secondary amines (TCA)

A

Nortriptyline
Desipramine

block NE reuptake

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12
Q

SSRIs

A 
Fluoxetine
Sertraline
Paroxetine
Citalopram
Escitalopram
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13
Q

SSRIs

A 
Depression (DOC)
Panic disorder
OCD
Social anxiety
Bulimia
Alcoholism

Very safe therap window

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14
Q

SSRIs mild SE

A

GI, nausea, weight cange, anxiety, insomnia

Sexual disinterest*

Photosensitivity (LIMIT SUN EXP)

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15
Q

Fluoxetine

prototype SSRI

A

More drug intxns than other SSRIs

Impairs glucose levels, avoid in DIABETIC

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16
Q

Fluoxetine and Sertraline (SSRI) spec have SE of

A

Anxiety, insomnia

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17
Q

With SSRIs, be aware of what type of drug interaction?

A

Opoiods

  • pain med will not work
  • Serotonin synd
  • Inc risk Seizures
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18
Q

Avoid this SSRI if you are Diabetic

A

Fluoxetine (prozac)

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19
Q

DOC for Depression

A

Citalopram (celexa)

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20
Q

SNRI

Seretonin-NE reuptake inhibitor

A

Depression
Neuropathic pain*
Post menopause hot flashes

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21
Q

SNRI

A

Inhibit NE and 5-HT but cleaner than TCAs

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22
Q

SNRIs (2 drugs)

A

Venlafaxine

Duloxetine

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23
Q

Venlafaxine (SNRI)

A

may increase BP

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24
Q

Duloxetine (SNRI) bad SE

A

Hepatotoxicity

Glaucoma

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25
Q

MAOIs

A

Dirty drug

LAST CHOICE

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26
Q

MAOIs

A

Avoid foods w Tyramine (HTN crisis)

With basically any other drug, SEROTONIN SYNDROME (high fever)

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27
Q

MAOIS

A

irrev inhibit MAO which break down NE, DA, and 5-HT

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28
Q

MAO-A

A

inhibit NE, DA, and 5HT in CNS AND Periphery

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29
Q

MAO-B

A

DA in CNS only

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30
Q

MAOIs (2 drugs)

A

Phenelzine

Selegiline

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31
Q

Phenelzine (MAOI)

A

Use for depression that hasn’t responded to other drugs

inhibits both MAO-A and MAO-B

HTN CRISIS

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32
Q

Selegiline (MAOI)

A

Depression and
Parkinsons (lower dose)

MAO-B only

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33
Q

Buproprion

A

Use if pts are having sexual dysfx w other Antidepressant meds

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34
Q

Buproprion

A

inhibit DA reuptake

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35
Q

SE of Buproprion

A

Seizure
Anxiety, insomnia, restless, tremor, psychosis
Tachycardic

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36
Q

Buproprion is CONTRA in

A

Seizure pts

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37
Q

Other uses for Buproprion

A

ADHD
Alcoholism
Smoking

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38
Q

Mirtazapine

A

Good if pts have Insomnia, Anxiety, AND depression

DROWSY EFFECT

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39
Q

Mirtazapine

A

block pre-syn a2 which usually inhibits NE and 5HT release

Result: increased amounts of NE and 5HT

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40
Q

Mirtazapine

A

No bad SE like anxiety, insomnia, sexual dysfx

ONLY DROWSY

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41
Q

Atomoxetine

A

ADHD med
Increases memory/ attention

Good choice for addicts (no euphoria effect)

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42
Q

Atomoxetine

A

selective inhibitor of NE reuptake

SAFE and CLEAN drug

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43
Q

SE of Atomoxetine

A

GI distress
insomnia

Liver damage- but very rare

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44
Q

Trazadone

A

Sleep aid
Pain mgmt

NOT a good antidepressant

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45
Q

Trazadone

A

5HT2a receptor antagonist

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46
Q

Trazadone SE

use rather for sleep and pain

A

sedating
dizzy
Priapism- rare but serious!!! persistent and painful erection

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47
Q

Priapism

A

persistent and painful erection

SE of Trazadone

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48
Q

Mesolimbic pathway

A

VTA to Limbic system

Emotion
D2 receptors
Positive sx

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49
Q

Mesocortical pathway

A

VTA to frontal Cortex
D4, Seretonin 4a receptors
Negative sx

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50
Q

Nigrostriatal pathway

A

SN to Striatum

Motor control

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51
Q

Tuberofundibular pathway

A

Hypothalamus to pituitary

Prolactin

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52
Q

Neuroleptic Malignant syndrome

A

SE of Antipsychotic drugs
Muscle rigidity
change in BP, HR
Block of D2 receptors in Striatum and Hypoth

Tx: Dantrolene (muscle relaxant)

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53
Q

“positive” sx of psychotic disorders

A

D2 pathway, emotion
Overactive DA in Limbic system

Catatonic behavior, disorganized speech and thinking

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54
Q

“negative” sx of psychotic disorders

A

Underactive DA pathways in frontal Cortex

Depressed, withdrawing from activity

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55
Q

Chlorpromazine

A

“classical” antipsychotic

Use: Psychosis associated with Mania and Drugs of abuse

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56
Q

EPS

A

Extrapyramidal sx

acute dyskinesias and dystonic reactions, neuroleptic malignant synd, etc

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57
Q

Classic antipsychotics run the risk of

A

EPS

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58
Q

Chlorpromazine

A

low incidence of EPS compared to other classics

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59
Q

Chlorpromazine SE

A

Seizures
Retinal deposits (browning vision)
Sedation, blurry vision

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60
Q

Fluphenazine

A

similar to Chlorpromazine, selective for D2

Less anticholinergic effects, thus more EPS potential (bad)

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61
Q

Haloperidol

injected

A

Classic antipsychotic

for ACUTE situations to pull someone out of psychotic episode

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62
Q

Haloperidol SE

injected

A

Potent D2 blocker

no anticholinergic activity, HIGH EPS POTENTIAL (bad)

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63
Q

The 3 types of Classic Antipsychotics we talk about are

A

Chlorpromazine
Fluphenazine
Haloperidol

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64
Q

Atypical Antipsychotic means:

A

Block 5HT2a receptors AND D2, D4

Alleviate pos and neg sx of psychosis

Lower incidence of EPS

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65
Q

Clozapine

A

Drug of LAST choice out of Atypicals d/t SE of AGRANULOCYTOSIS

seizures
hypersalivation
dizzy
tachy
wt gain
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66
Q

If you are on Clozapine, what do you need to monitor daily

A

Blood to check for Agranulocytosis

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67
Q

DO NOT STOP what Atypical Antipsychotic drug abruptly?

A

Clozapine bc effects do not persist

unusual for antipsychotics

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68
Q

Olanzapine

A

A fairly safe Atypical Antipsychotic

Also used for Bipolar (w Lithium)

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69
Q

Olanzapine SE

A

“Zyprexa Diabetes”

caution of Hyperglycemia

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70
Q

Risperidone

A

DOC 1st choice for Schizophrenia

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71
Q

Risperidone

A

1st choice

EPS is very very rare

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72
Q

Risperidone SE

A

Hypotension
Wt gain
Insomnia
Lengthen QT interval*

BUT, overall pretty safe. 1st choice for Schizo

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73
Q

Ziprasidone

A

Antidepressant use

and
Tourettes
Acute mania

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74
Q

Ziprasidone

A

Prolong QT interval
Sedation
Hyperprolactinemia

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75
Q

Ziprasidone CONTRA

A

Seizure hx

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76
Q

Quetiapine

A

VERY SEDATING

Used to promote sleep

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77
Q

Good things about Quetiapine

A

No agranulocytosis

Doesn’t elevate prolactin

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78
Q

Aripiprazole unique trait

A

Dopamine system stabilizer

brings it back to natural levels

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79
Q

Aripiprazole SE

A

Hyperglycemia
Seizures
Sedation
Decreases esophogeal motility

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80
Q

Good things about Aripiprazole

A

no increase in prolactin

no effect on QT

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81
Q

Lurasidone

A

Depression associated w Bipolar

don’t know much about this drug, new

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82
Q

Lurasidone

A

new drug
hits 30 receptor subtypes

Monitor Blood for: Agranulocytosis and Neutropenia

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83
Q

Lithium

A

DOC for Bipolar

calming manic state

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84
Q

Lithium

A

Small therapeutic window

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85
Q

Lithium SE

A

Extremely TOXIC in OD
Can lead to Diabetes Insipidus
Competes w Na for reabsorption (watch salt intake)

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86
Q

Lithium CONTRA

A

Hypothyroid
Pregnancy
with NSAIDs

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87
Q

Valproic acid

A

Use for Rapid Cycling manic/depressive episodes

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88
Q

Valproic acid

A

Bipolar pts who do not respond to Lithium

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89
Q

Valproic acid

A

Anticonvulsant

mechanism unknown

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90
Q

Valproic acid SE

A

Surgical bleeding (dental)

GI, sedation, wt gain

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91
Q

Valproic Acid CONTRA

A

Pregnancy (remember, all anticonvulsants aren’t safe in pregnancy)

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92
Q

Gabapentin

A

Also used for rapid cycling

minimal drug interactions

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93
Q

Carbamazepine

A

Use: Refractory Bipolar disorder

used w Lithium

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94
Q

Carbamazepine SE

A

Induce CYP450

SJS/TEN risk!!!

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95
Q

Testing for human antigen required prior to using this to prevent SJS/TEN

A

Carbamazepine

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96
Q

Lamotrigine

A

prevention of Relapse following mania

Acute mania

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97
Q

Opioids work at the pre-syn and post-syn terminal

A

pre: decrease Ca, thus decrease neurotransmitter release (Glutamate and Substance P)
post: Mu agonist, hyperpolarize pain receptor and inhibiting the post-synaptic potential

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98
Q

Does neuropathic pain respond to opioids?

A

No

Gabapentin and Amitriptyline are better for neuropathic pain

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99
Q

What receptors are responsible for dysphoria? (bad)

A

Kappa

Delta

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100
Q

What do pupils look like with Opioids?

A

Constricted

may concert to dilation in comatose

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101
Q

Tolerance for Opioids develops after a few days, EXCEPT with

A

Miosis
Seizures
Constipation

tolerance never develops

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102
Q

Tolerance involves which parts of the nervous sytem

A

Thalamus

Spinal cord

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103
Q

Addiction involves

A

reward pathway

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104
Q

Overdose Triad of Opioids

A

Respiratory depression
Pinpoint pupils
CNS depression

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105
Q

Tx of Opioid OD

A

ABCs

Naloxone (Narcan)

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106
Q

MAOI and Opioids?

A

BAD NEWS BEARS

Seretonin Syndrome!!!

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107
Q

Drug intxns w Opioids

A 
Meperidine
Dextromethorphan
MAOI
SSRI
Antipsychotic
Sedative hypnotics
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108
Q

CONTRA to opioid use

A 
Partial agonist w full agonist
Pregnant
Head injury
Impaired lung, liver, or kidney fx
Some endocrine dz
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109
Q

Heroin and pregnancy

A

Can cross placental barrier

Cause respiratory depression and dependence in baby

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110
Q

Morphine

A

SEVERE pain, strong agonist

Stimulates ALL receptors

best effective when injected (high first pass if given orally)

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111
Q

Morphine dosing

A

Standard dose is 10 mg SubQ or IM

all other drugs based off of this

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112
Q

Hydromorphone (Dilaudid)

A

Mod-Severe pain

Good if pt has Renal dysfx

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113
Q

Hydromorphone (Dilaudid) is very similar to Morphine other than

A

Metabolites dont accumulate, less itching SE

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114
Q

Methadone (Dolophine)

A

Long term pain control
Maintenance tx of addicts
Low dose: prevent withdrawal
“Hard to treat” types of pain

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115
Q

Methadone (Dolophine

A

Mu agonist

Block NMDA

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116
Q

GOOD effect of Methadone

A

pts less likely to become tolerant to this

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117
Q

Meperidine

A

“odd duck” drug

Used in Obstetrics: less respiratory depression in babies

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118
Q

Meperidine

A

Mu agonist

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119
Q

Meperidine SE

A

Seizures
Tachycardia
Pupil dilation
*Seretonin synd if given w MAOI

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120
Q

Meperidine

A

Use in pregnancy!

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121
Q

Fentanyl (sublimaze)

A

Short surgical procedures
(with midazolam)
or
Longer surgeries

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122
Q

Fentanyl (Sublimaze)

A

Short duration! very lipid soluble

transdermal patch: slower release

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123
Q

Fentanyl (sublimaze) bad things/SE

A

Abuse potential is HIGH

Truncal rigidity

Drug intxns likely

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124
Q

In general, short acting drugs are

A

WORSE, higher risk for abuse potential

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125
Q

Hydrocodone (Vidocin)

A

Mod-severe pain
often combo w Acetaminophen

Does NOT work well w SSRI

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126
Q

“workhorse” opioid drugs

given often

A

Hydrocodone (vicodin)

Oxycodone (oxycontin)

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127
Q

Oxycodone

A

mod-severe pain

often combo w Acetaminophen (just like hydrocodone)

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128
Q

Oxycodone

A

huge drug of abuse

can be given in different forms to decrease abuse potential

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129
Q

Codeine

A

good cough suppressant (low dose)

mild-moderate pain

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130
Q

Codeine

A

converted to Morphine

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131
Q

Codeine CONTRA

A

children

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132
Q

Pentazoicne/Naloxene

A

moderate pain

Kappa agonist
Partial Mu agonist

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133
Q

Pentazocine/Naloxone

A

Dysphoria!!

recovering addicts or those afraid for abuse use this bc it has LOW abuse potential

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134
Q

Buprepnorphine

A

Use: maintenance tx of addiction
decreases craving
(combine w Naloxone)

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135
Q

Buprenorphine

A

Mu partial agonist

does NOT cause euphoria

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136
Q

Buprenorphine and pentazocine/Naloxone

A

Low abuse potential

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137
Q

Tramadol

A

Mild-moderate pain

Comb w Antidepressants to treat seizures

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138
Q

Tramadol

A

Weak Mu agonist

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139
Q

Tramadol SE

A

mild: dizzy, sedation, constipation, nausea

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140
Q

Tramadol CONTRA

A

with Antidepressants, can cause Serotonin syndrome and seizures

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141
Q

Dextromethorphan

A

Cough suppressant
Drug of abuse in teenagers

NOT a pain med

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142
Q

Dextromethorphan

A

blocks NMDA receptors

abuse potential

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143
Q

Anything with MAOIs

A

be cautious of Serotonin syndrome

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144
Q

Naloxone (Narcan)

A

DOC for Opioid overdose

now can be comb w some opioids to prevent abuse

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145
Q

Naloxone (Narcan)

A

Opioid antagonist

give until pupils dilate

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146
Q

How long is Naloxone (Narcan)’s duration?

A

Short! only 2 hours

Might have to give every couple hours until opioid wears off

Repeat dosing

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147
Q

Naltrexone

A

Another opioid antagonist

Tx of opioid addicts in Healthcare professionals

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148
Q

Naltrexone

A

Healthcare addicts

Recovering alcoholics

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149
Q

Naltrexone

A

Orally effective

24 hour long drug (why its good for healthcare, can last their whole shift)

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150
Q

Naltrexone SE/ CONTRA

A

Liver toxicity w chronic use

CONTRA hx of liver dz

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151
Q

Parkinsons

A

death of DA neurons in Substantia Nigra

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152
Q

Lewy bodies

A

clumps of a-synuclein and other proteins in nerve cells, associated with Parkinson’s

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153
Q

L dopa alone

A

end result: increase DA levels
Crosses BBB, then converted to DA

need high doses, only 1-3% gets into CNS

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154
Q

L dopa WITH Carbidopa

A

now 10% can get into CNS

bc Carbidopa inhibits dopa-decarboxylase, the enzyme that breaks L dopa down, inhibits SE also

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155
Q

SE of L-dopa/carbidopa

A 
N/v
Dyskinesa 
Hypotension
Arrhythmia
Depression, anxiety, agitation

Psychosis possible

156
Q

Imp drug combo considerations with L-dopa/carbidopa

A

with MAOI: HTN crisis

with Vit B6: decrease effectiveness of drug

157
Q

CONTA to L-dopa/carbidopa

A 
Psychosis
Closed glaucoma
Cardiac dz
active PUD
Malignant melanoma
158
Q

Considerations w L-dopa/Carbidpoa

A

pt compliance
Has to take med 3-4x per day

“on off phenomenon”

159
Q

On off phenomenon

A

Apomorphine used to treat

D2 receptor agonist, pulls people out of the off phase

160
Q

Selegiline

A

Parkinson tx

inhibits MAO-B in CNS (inhibits DA metabolsim)

161
Q

Selegiline SE

A

Insomnia

Severe HTN

162
Q

Selegiline CONTRA

A

do NOT combo with Meperidine: Seretonin Syndrome

163
Q

MAOB-I

Parkinson tx

A

Selegiline
Rasagiline
Safinamide

all inhibit MAO-B in the CNS only

which means does not affect DA in the periphery

164
Q

COMT inhibitors

A

Tolcapone

Entacapone

165
Q

Tolcapone

A

inhibit DA and L-dopa metabolism in CNS and periphery

166
Q

Tolcapone SE

A

Hepatic failure

167
Q

Entacapone SE

A

Orange urine

confusion, hypotension, abd pain, insomnia

168
Q

Stalevo

combo

A

L-dopa, Carbidopa, Entacapone

169
Q

Entacapone

A

inhibit DA and L-dopa metabolism in PERIPHERY only

170
Q

COMT

A

usually metabolizes L-dopa and DA, that is why inhibitors of these drugs help tx Parkinson

171
Q

DA receptor agonists

A

Bromocriptine
Ropinirole
Pramipexole
Rotigotine

continue to be effective as Parkinsons progresses bc act directly on receptors*

172
Q

First line therapy for Parkinson

A

DA receptor agonists

Bromo
Ropinirole
Pramipex
Rotigot

173
Q

Bromocriptine

A

can cause Erythromelalgia (vascular peripheral hand/feet spasm)

174
Q

Ropinirole and

Pramipexole

A

the “go to”

Monotherapy in Mild parkinson, soothing response to L-dopa in Late parkinson

175
Q

Ropinirole

A

DOC for restless leg syndrome (RLS)

176
Q

Pramipexole

A

FDA warning: Heart Failure

177
Q

Rotigotine

A

transdermal patch for Parkinson and Restless leg synd

178
Q

Apomorphine

A

Tx temporary relief “rescue” for off period in pts on optimized L-dopa

179
Q

Apomorphine SE

A

Nausea

take anti-emetic b4, like trimethobenzamide

180
Q

When giving anti-emetic with Apomorphine, avoid

A

targets to 5HT, like Ondansetron (can cause severe HTN, LOC)

blocks to D2 receptors, like Prochlorperazine

181
Q

SE of DA agonist

Bromocriptine
ROpinirole
Pramipexole
Rotigotine

A 
Anorexia, n/v
Postural hypotension (beg of tx)
Cardiac arrhytmias (DISCONTINUE if happens)
182
Q

What causes erythromelalgia

A

Bromocriptine

183
Q

Amantadine

A

increases DA neurotransmission

184
Q

Amantadine

A

Antiviral for flu

Early/mild Parkinson

185
Q

Amantadine SE

A

Livedo reticularis - reddish blue spotting of skin

186
Q

Amantadine overdose

A

Toxic psychosis

Convulsions

187
Q

Anticholinergics to treat Parkinson

A

Benztropine
Trihexyphenidyl

restores DA/Ach balance in striatum

188
Q

Benztropine

Trihexyphenidyl

A

modest anti-parkinson
Improve rigidity,t remor

Little effect on bradykinesia

189
Q

Benztropine

Trihexyph

A

usually used in addition to DA therapy

190
Q

Pimavanserin

A

Atypical Antipsychotic

For tx of psychosis and dellusions/hallucinations associated w Parkinson

191
Q

Pimavanserin mechanism

A

inverse agonist/antagonist for 5HT receptors

192
Q

Pimavanserin

A

NOT approved for tx of dementia assoc w Alzheimers, increases mortality

193
Q

do NOT use Pimavanserin in

A

Alzheimers

194
Q

B-amyloids and Tau proteins

A

plaques and tangles associated with Alzheimers

195
Q

What causes Alzheimers

A

degeneration of Cholinergic neurons

Neuronal atrophy

196
Q

Cholinesterase inhibitors for Alzheimers

A

Donepezil
Rivastigmine
Galnatamine

197
Q

ACHe Inhibitors for ALzheimers

A

taken once/day
Inc brain activity and improve fx

may slow progression of dz

198
Q

Memantine tx for Alzheimers

A

NMDA receptor antagonist,

reduces excitotoxic effect of glutamate and slow degeneration

199
Q

Memantine CONTRA

A

do not give WITH Meperidine

200
Q

Downfall of L-dopa for tx

A

Effectiveness goes down over time

Does not affect progression of dz; DA neurons continue to degenerate

201
Q

SE of Cholinesterase inhibitors

A

GI most common

n/v/d, stomach cramps

202
Q

Amphetamines

A

Adderall

Ritalin (methylphenidate)

203
Q

Amphetamines

  • adderal
  • ritalin
A

increase release of DA, reverse DA transport thru the DAT

204
Q

Bad things about Amphetamines (Adderall and Ritalin)

A

Increase BP
Pulmonary edema
Heart Failure

205
Q

Amphetamines

A 
Alertness
Euphoria
Excitement
Aggression
Paranoia
Delusions
206
Q

Meth

ICE, crystal meth

A

May produce Amphetamine psychosis

pale skin, body odor, hyperthermia, dental problems
“meth bugs”
“meth mouth”

207
Q

More serious SE of Meth

A

seizures, organ damage, stroke, heart attack

208
Q

Meth

ICE, crystal meth

A

Rapid physical and psychological dependence

209
Q

Chronic users of meth

A

Permanent damage to Noradrenergic and Serotonergic neurons, loss DA transport, Slow motor rxn, Memory loss, personality change

210
Q

Cocaine

A 
Alertnes
Euphoria
Anxiety
Hyperactivity
Tremor 
Twitch
Pupil DILATION
211
Q

Cocaine systemic effects

A 
tachycardia
vasoconstriction
HTN
bronchodilation
hyperpyrexia
212
Q

Medical use of cocaine

A

Local anesthetic

Vasoconstrictor

213
Q

Chronic use of cocaine

A 
Reduce brain activity
Anxiety
Insomnia
Paranoia
Hallucinate
Repetitive behavior
Nasal congestion
Perforated nasal septum
214
Q

Cocaine mechanism

A

inhibit DA reuptake

Physical and psychological dependence (severe withdrawal)

215
Q

Cocaine overdose/toxicity

A 
Ventricular tachy
V- Fib
Stroke
Cerebral hemorrhage
Seizure
216
Q

Tx for Cocaine withdrawal

A

Bromocriptine (decreases craving)

217
Q

Nicotine

A

Mild euphoria
Increased arousal
Appetite suppression

218
Q

Nicotine mechanism

A

Increase 5HT and DA release

intense psychological and physical dependence

219
Q

Nicotine withdrawal is so difficult partly because

A

Nicotinic receptors are in excess still 1 month after stopping

Normalize by 6-12 wks after

220
Q

Tx for Nicotine withdrawal

A

Replacement therapy
Bupropion
Varenicline
Behavioral tx

221
Q

NDMA “Ecstacy”

A

Feelings of peaceful
Empathy
Closeness
Trust, BUT

followed by: depression, confusion, anxiety, paranoi

222
Q

NDMA “ecstasy”

A

inc Serotonin activity by blocking reuptake AND stimulating receptors

223
Q

NDMA “ecstacy” SE

A

Hyperthermia
Dehydration
Kidney failure can –> DEATH
Memory loss

224
Q

Long term use of NDMA “Ecstacy”

A

Decrease level of Serotonin in Cerebral cortex

225
Q

Marijuana

A 
Mild euphoria
Well being
Altered sense of time
Difficult to concentrate
Introspection
Tranquility
226
Q

Marijuana SE

A

anxiety
dec memory
impaired reasoning
un-motivated

227
Q

Marijuana SE

A

Hyperemesis
Cyclic vomiting

Bronchial irritaiton
risk of CA
Decreased ovulation
Decreased Testosterone
Low birth weight
FETAL malformations
228
Q

Synthetic “cannabinoid” agonist

A

Psychoactive effects
Paranoid
hallucinate, mood swing, aggression, violent outburst, elevated HR and BP

not tested for human effects

229
Q

Mary J pharmaco

A

Very lipophilic, long 1/2 life, quickly absorbed

no physical dependence

230
Q

Mary J mechanism

A

Stimulate pre-syn CB1 receptors to inhibit Ach release

231
Q

LSD/ Mescaline/ Psilocybin

A

Euphoria
Visual hallucinate
“bad trips” flashbacks
Increase BP, HR, flushing, dilated pupils

232
Q

Synesthesia

A

LSD (and Mescaline/psilocybin)

Senses are all mixed up- colors are heard, sounds are seen

233
Q

LSD

A

acts on serotinin receptors in brain

NO dependance, does NOT stimulate DA pathways

234
Q

PCP (angel dust)

A

Developed as anesthetic
May cause analgesia WITH agression

often produces Psychosis

235
Q

PCP (angel dust)

Ketamine

A

NMDA antagonist

236
Q

How to treat Psychosis caused by PCP (angel dust)?

A

Haloperidol

237
Q

Ketamine and GHB

A

“date rape”

238
Q

GHB mechanism

A

weak GABA agonist

239
Q

Inhalants cause

A

toxicity in MANY organs

Lesions in brain white matter!

240
Q

Nitrous oxide

A

Peripheral neuropathy with chronic use

Frequently abused by DENTISTs

241
Q

Nitrous oxide

A

rapid, short acting pleasure

OD can be fatal

242
Q

Amyl/butyl nitrite

A

“poppers” “snappers”

Euphoria, light headed, blurry vision, HA, nausea, hypotension, tachycardia

Smooth muscle relaxant

243
Q

Naltrexone CONTRA

treat alcoholism, pt doesn’t even want it- curbs craving

A

Liver failure

causes hepatic damage

244
Q

Acamprosate

treat alcoholism

A

analog of GABA

restores normal balance of GABA and glutamate

245
Q

Disulfuram

treat alcoholism

A

acetaldehyde builds up, person feels awful BUT SE can be severe: vomiting, sweating, CP, hypotension, blurred vision, shock

246
Q

Topiramate

treat alcoholism

A

Anticonvulsant

mechanism not well understood

247
Q

Barbiturates

A

works INDEPENDENT of GABA

No ceiling effect, dangerous bc levels can just keep rising

248
Q

Barbiturates

“phenobarbitol”

A

Bind to GABA, stimulate Cl influx

249
Q

Barbiturates CONTRA

A

Porphyria (abnormal heme synthesis)

Pulmonary insufficiency

With other CNS drugs (supra-additive w alcohol)

250
Q

Benzos

“pam” mostly used for

A

Anxiety

Insomnia

251
Q

Benzos “pam” CONTRA

A

Pregnant
Sleep apnea
Elderly

252
Q

Benzos “pam” are safer because

A

Have ceiling effect

Dependent on GABA

253
Q

Do not stop ____ abruptly

A

Benzos “pam”

254
Q

Flurazepam and Temazepam

A

Insomnia

“hangover” drowsy effect

255
Q

Diazepam and Lorazepam use:

A

Status Epilepticus

256
Q

Midazopam

A

Short acting

Given IV b4 short procedures

257
Q

Flumazenil use

A

Hyperinsomnia (too much sleeping)

258
Q

Flumazenil

A

Benzo “pam” ANTAGONIST

competes w benzos for GABA spot

259
Q

Flumazenil (hyperinsomnia tx) CONTRA

A

Seizure hx

260
Q

The Z drugs for insomnia

A

Zolpidem
Zaleplon
EsZopiclone

261
Q

The Z drugs

A

bind to Benzo1 subtype of GABA

Strong and rapid sedative effects

High margin of safety; GOOD

262
Q

Morning drowsy is unlikely with the Z drugs (except Eszopliclone) because

A

they have a short duration of action

besides EsZ

263
Q

Suvorexant

insomnia tx

A

Orexin antagonist

264
Q

Caution w Suvorexant (insomnia tx)

A

Those w Depression, can worsen

265
Q

Suvorexant (insomnia tx) CONTRA

A

Narcolepsy

266
Q

Ramelteon mechanism

A

Melatonin analog

resets sleep/wake cycle

267
Q

Chloral hydrate

A

Children sedation during dental procedures

268
Q

Chloral hydrate

A

Children dental
nursing home
chronic care

269
Q

Chloral hydrate

A

converted to Trichloroethanol which acts similar to barbs on GABA receptor

LOW margin of safety (just like Barb)

270
Q

Chloral hydrate is dangerous d/t low margin of safety

A

Respiratory and vasomotor depression
Cardiac arrhythmia

Long term: liver damage, fatal intoxication

271
Q

Buspirone use

A

Generalized anxiety

272
Q

Buspirone

A

Relieves anxiety w/o causing sedation

Full agonist at 5HT1a presynaptic

Partial agonist at postsynaptic

273
Q

Tiagabine

anticonvulsant

A

block GABA reuptake

274
Q

Vigabatrin

A

Refractory partial

Infantile West spasm

275
Q

Vigabatrin

A

Inhibit GABA-T metabolism (breakdown)

276
Q

Vigabtrin SE

A

Visual field problems
Retinal damage
Agitate, confusion

277
Q

Infantile West synd tx

A

Clonazepam

Vigabatrin

278
Q

Long duration Benzos “pam”

A

Diazepam

Flurazepam

279
Q

Intermediate duration Benzos “pam”

A

Alprozolam
Oxazepam
Lorazepam

280
Q

Pregabalin (Lyrica)

A

Generalized anxiety disorder

Others:
Neuropathic pain
Fibromyalgia
Post op pain

281
Q

Pregabalin

A

GABA analog, binds to Ca channels

CONTRA: pregnancy

282
Q

Gabapentin (neurontin)

A

Adjunct partial and gen tonic-clonic seizure
Neuropathic pain
Bipolar (off label)

283
Q

Gabapentin

A

Gaba analog- increase GABA release

CONTRA: pregnancy

284
Q

Does Gabapentin have drug interactions?

A

NO

and Pregabalin has very little

285
Q

Phenobarbitol

A

Stimulate GABAa receptor, prolong opening of Cl channel

partial seizures
gen tonic-clonic

286
Q

Levetiracetam

A

Partial seizures
Myoclonic
Tonic clonic

287
Q

Levetiracetam mechanism

A

SV2A, bind synaptic vesicular protein

Minimal drug intxns, SAFE to use w others

288
Q

Phenytoin (dilantin)

A

Partial seizures

Gen tonic-clonic

289
Q

Phenytoin (dilantin) mechanism

A

prolongs inactivation of Na; decreases Glutamate activity

290
Q

Phenytoin pharmaco

A

1st order at low doses
Zero order at therapeutic and HIGH doses; small change in dose can cause BIG change in plasma levels

(Caution)

291
Q

Phenytoin (dilantin) SE

A

Gingival hyperplasia
Risk of SJS
CONTRA: pregnancy

292
Q

Carbamazepine

A

DOC for Partial seizures

293
Q

Carbamazepine other use (other than Partial seizures)

A

Trigeminal neuralgia

294
Q

Carbamazepine mechanism

A

Block Na channel; decrease Glutamate activity

295
Q

Carbamazepine SE

A

SJS risk, screen for HLAB1502 before use
Aplastic anemia and Agranulocytosis

CONTRA: pregnancy

296
Q

Lamotrigine

A

Inactivate Na channels; decrease Glutamate activity

used for Partial seizures, but NOT DOC (Carbamazepine is)

297
Q

Lamotrigine risk

A

SJS

Pregnancy CONTRA

298
Q

Topiratmate

A

Partial
Gen tonic-clonic
Migraine PREVENTION

299
Q

Topiramate

A

Block Na channe; decrease Glutamate

300
Q

Topiramate SE

A

Acute myopia

Glaucoma

301
Q

Levetiracetam

A

Minimal drug intxns

302
Q

Ethosuximide

A

DOC for Abscence seizures

303
Q

Ethosuximide mechanism

A

Inhibit low threshold Ca channels

304
Q

Ethosuximide SE

A

Hiccups!

305
Q

Ethosuximide’s metabolism is inhibited by

A

Valproic acid

306
Q

Valproic acid

A

Mixed seizures

bc mechanism blocks Ca and Na channels, may enhance GABA

307
Q

Valproic acid SE

A

Hepatotoxic (need to monitor LFTs)

CONTRA pregnancy

308
Q

Toxicity of all Anticonvulsants

A

Teratogenic; AVOID in pregnancy
Rebound seizures in withdrawal
OD CNS depression(rarely lethal, do NOT treat w CNS stimulant)
Suicidal thoughts

309
Q

SJS risk, those that block Na channels

A

Phenytoin
Lamotrigine
Carbamezapine*
Valproic acid

310
Q

Anticonvulstants cause what to be less effective

A

Birth control!

If pregnant, causes birth defects, congenital heart defects, neural tube defects

311
Q

Esters

A

shorter duration of action, but

increased TOXICITY

312
Q

Mechanism of anesthetics

A

Block Na channels

inhibit neuron firing

313
Q

Efficiency of anesthetic block is better in

A

Rapidly firing axons

314
Q

Anesthetic block is enhanced in

A

Elevated K+ bc the membrane is already depolarized

315
Q

Anesthetic block is diminished in

A

Elevated Ca++ bc the membrane is hyperpolarized

316
Q

Lipid solubility does what to the duration of anesthetic action?

A

More lipid soluble = longer duration of action

317
Q

Amides are metabolized in

A

Liver by CYP450

318
Q

Esters are metabolized in

A

Plasma by butylcholinesterase

319
Q

Have to caution with Liver damage with Amides or Esters?

A

Amides
met in the Liver

Toxicity is more likely in pt with Liver dz or Reduced Liver blood flow

320
Q

Methemoglobinemia

A

Prilocaine metabolite

321
Q

Allergic reactions are rare with Amides or Esters?

A

Rare with Amides

322
Q

Procaine- short duration of action

A

Diagnostic infilration nerve block

metabolite product PABA; allergic rxn and inhibit sulfa

323
Q

Tetracaine

A

Obhto (eye) use, retrobulbar procedure

and

Spinal anesthesia

324
Q

Benzocaine

A

Very lipophilic
always in Non-ionized form

Topical only; sunburn

325
Q

Cocaine

A

Reduce dental bleeding

CNS and CVD SE; caution

326
Q

Lidocaine- prototype AMIDE

A

Infiltration block
Epidural anesthesia

NOT for spinal block (risk of TNS)

327
Q

Prilocaine

A

Highes rate of clearance of Amides

328
Q

Prilocaine SE

A

Risk of Methemoglobinemia

Too much methemoglobin in blood, SOB, fatigue, dizzy, coma, death

Tx; methylene blue

329
Q

Prilocaine CONTRA

A

Cardiac or respiratory dz

330
Q

Prilocaine use

A

LARGELY LIMITED to DENTISTRY

331
Q

Bupivacaine

A

longer duration
post-op pain control
Spinal anesthesia, infiltration, epidural

GREATER cardiotoxicity than other amides

332
Q

Bupivacaine use

A

Epidural during LABOR

sensory> motor block, important for delivery

333
Q

Ropivacaine

A

S-enantiomer of Bupivacaine

less likely to have cardiac toxic SE, but still not DOC for birth bc has more effect on motor

334
Q

Ropivacaine use

A

peripheral and

epidural (not labor) nerve blocks

335
Q

Etidocaine

A

Inverse differential block,

meaning motor> sensory block

336
Q

Articaine

A

Widespread use in Dental medicine

337
Q

Articaine rare SE

A

Persistent paresthesia

338
Q

Dibucaine

A

test to measure butylcholinesterase activity

determines the ability to use Ester drugs

339
Q

Centrally acting spasmolytics

A

Baclofen
Cyclobenazprine
Diazepam
Tizanidine

340
Q

Direct acting spasmolytics

A

Dantrolene

Botox

341
Q

Diazepam affects all subtypes of GABA receptors

A

can be used as muscle relaxant, bu tproduces heavy sedation

342
Q

Baclofen

A

GABA-b receptor

stimulates open K channels- hyperpolarize

inhibit Ca influx

343
Q

Tizanidine

A

a2 agonist, inhibits BOTH pre and post synaptic spinal cord activity

chronic and acute muscle spasm

344
Q

Dantrolene

A

inhibit Ca release from SR

RYR1 channel

345
Q

Dantrolene use

A

Neuroleptic malignant syndrome

Malignant hyperthermia

346
Q

Botox

A

Small amts injected locally to control muscle spasm following Stroke or other neuro injury

347
Q

Ach

A

Alzheimers

348
Q

Dopamine (DA)

A

Parkinson’s

Schizophrenia

349
Q

GABA

A

Major inhibitory
Relieves anxiety, promotes sedation

Cl- channels

350
Q

Neuropeptide Y

A

food intake and fat storage

351
Q

Genetic link to Alcoholism is related to

A

increase in release of B-endorphins in the Dopamine reward pathway

352
Q

Genetic alcholism

A

B-endorphins

353
Q

Alcohol metabolism

Acute vs Chronic pathways

A

Acute: Alcohol DH

Chronic: MEOS and CYP2E1 now get activated as well
increases acetaminophen toxicity

354
Q

Alcohol does what to CYP2E1?

A

induces CYP2E1, meaning they now metabolize it quicker, leading to increased tolerance

355
Q

What happens to GABA and NMDA receptors in Alcoholics

A

Down regulate GABA

Up regulate NMDA

356
Q

An Alcoholic who is tolerant to Alcohol may also be tolerant to:

A

Benzos and Barbs

357
Q

Alcohol mechanism

A

Bind to GABAa- increase Cl- influx and enhance GABA transmission

Increase DA in Limbic area

358
Q

Alcohol leads to deficiencies in

A

Folate

Thiamine

359
Q

Wernicke Korsakoff syndrome

A 
Paralysis of eye
Ataxia
Confusion
Coma
Death

All d/t THIAMINE deficiency

360
Q

Korsakoff psychosis

A

Chronic disabling memory loss

361
Q

Best tx for Acute Anxiety (short term, self limiting)

A

Benzos “pam”

362
Q

Tx for Chronic/Generalized Anxiety

A

Buspirone

Benzos “pam”

363
Q

Kleine-Levin Syndrome

A

“sleeping beauty”
dissapears in teen years

sleeping for 24 hours at a time

364
Q

DOC for Enuresis/ bed wetting

A

TCAs (Tricyclic Antidepressants)

365
Q

Hydroxyzine

A

Antihistamine used as Anti-anxiety

1st gen Sedation

366
Q

How is Barbiturate toxicity eventually cleared?

A

Diuresis and Alkalization of URINE

otherwise, just treat supportively

367
Q

What is prescribed more for Anxiety/Insomnia?

Barbs or Benzos?

A

Benzos “pam”

368
Q

Traits about Diazepam and Lorazepam

A

DOC: Status Epileptius

Also, provide a tapered withdrawal (+ Chlordiazepoxide)

369
Q

Benzos “pam” contra

A

Pregnant
Old
Sleep apnea

370
Q

Barb contra

A

Porphyria
Pulm insufficiency
With other CNS depressants

371
Q

What can be given to reverse the effects of Midalozam? (a short acting Benzo)

A

Flumenazil- a Benzo antagonist

372
Q

Complex seizures are still <2 minutes

A

Altered or LOC

373
Q

Partial with secondary Tonic Clonic

A

LOC

muscle contraction w alternating contraction

374
Q

Tonic clonic (grand mal) seizure

A

<2 minutes

Start rigid, then tremor, then clonic jerking

LOC

375
Q

Absence seizure

A

10-30 seconda

Not as aware, but STILL CONSCIOUS

376
Q

Goal of seizure medicine in relation to GABA

A

Increase GABA

377
Q

Goal of seizure medicine in relation to Glutamate (NMDA)

A

Decrease NMDA (glutamate)

378
Q

Glutamate

A

Na and Ca channels

to treat seizure: inhibit these channels

379
Q

Common SE of seizure meds

A

Teratogenic

Hypersensitivity- SJS

380
Q

Anytime you are prolonging the inactivation of Na and Ca channels, you are

A

decreasing Glutamate activity

381
Q

Seizure meds affecting Na+ channels

A

Phenytoin
Carbamazepine
Lamotrigrine
Topiramate

382
Q

Seizure meds affecting Ca++ channels

A

Ethosuximide

Valproic acid

383
Q

Seizure meds affecting GABA channels

A 
Benzos
Barbs
Gabapentin
Pregabalin
Tiagabine
Vigabatrin
384
Q

SV2A

A

Levetiracetam

385
Q

Phenelzine

Selegiline

A

MAOIs

386
Q

Venlafaxine

Duloxetine

A

SNRIs

387
Q

Fluoxetine
Sertraline
Paroxetine
Citalopram

A

SSRIs

Quarter 4 (10 decks)

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