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Pharmacology > CNS Drugs > Flashcards

CNS Drugs Flashcards

1
Q

Zolpidem

A

Z-Drug. Commonly associated with sleep related behaviors. Short duration of action.

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2
Q

Atomoxetine Indications

A

ADHD. Especially in addicts (doesn’t cause euphoria).

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3
Q

Parkinson’s Pathophysiology

A

Caused by a loss of DA neurons in the nigrostriatal system. Treatment must balance Ach and DA.

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4
Q

Cholinesterase Inhibitors MOA

A

Increase Ach in the nerve terminals. May slow the progression of Alzheimer’s.

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5
Q

Mepivacaine

A

Amide LA. Intermediate duration of action.

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6
Q

Eszopiclone

A

Z-Drug. Long half life. Used for long-term treatment.

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7
Q

Secobarbital

A

Barbituate

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8
Q

Smoking Cessation

A

Bupropion will treat nicotine craving.

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9
Q

DOC for Bipolar Disorder

A

Lithium

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10
Q

TCA MOA

A

Inhibit re-uptake of NE and 5HT. Also blocks alpha, histamine and Ach receptors. Dirty drugs!

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11
Q

Galantamine

A

Cholinesterase Inhibitor used in Alzheimer’s

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12
Q

Tigabine Indications

A

Adjunct for partial seizures.

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13
Q

Metratazpine MOA

A

Blocks presynaptic alpha 2 receptors. Increases the release of NE and 5HT.

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14
Q

Citalopram.

A

SSRI. DOC for depression. Low incidence of drug interactions.

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15
Q

Z-Drugs MOA

A

Sedative-hypnotics. Bind the GABA receptor to increase GABA mediated inhibition.

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16
Q

Alcohol MOA

A

Binds to GABAa receptrs to increase Cl influx and enhance GABA (inhibitory) transmisison. Increases beta-endorphins in the mesolimbic pathway.

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17
Q

Cocaine effects

A

CNS stimulant. Increased SNS tone. Alertness, euphoria, hyperactivity, tachycardia, vasoconstriction, HTN, hyperprexia.

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18
Q

Midazolam

A

Very short-acting Benzodiazepine. Used for anxiety disorders and short surgical procedures as anesthesia.

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19
Q

DOC for Partial Seizures

A

Carbamazepine

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20
Q

Vigabatrin Indications

A

Refractory complex partial seizures. West’s syndrome.

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21
Q

Carbamazepine Indications

A

DOC for partial seizures. Also used for Trigeminal neuralgia, TC seizures and Refractory cases of Bipolar disorder.

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22
Q

Disulfuram (antabuse) MOA

A

Inhibits aldehyde dehydrogenase. Causes build up of acetyldehyde (flusing, nausea, HA).

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23
Q

Ropinirole

A

DA D2 agonist. Used as monotherapy in mild Parkinson’s. Can cause sudden sleep during the day.

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24
Q

Korsakoff’s psychosis

A

Chronic disabling memory loss

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25
Q

Memantine

A

NMDA receptor antagonist, reduces excitotoxic effects of glutamate and slows degerneration. Used in the late stages of Alzheimer’s in combination with a Cholinesterase Inhibitor.

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26
Q

Lamotrigine Indications

A

Partial seizures, Bipolar Disorder (prevents relapse). May be effective at treating myoclonic and absence seizures in children.

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27
Q

Carbamazepine SE

A

Diplopia, ataxia, high risk of SJS, Teratogenic.

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28
Q

Valproic Acid Indications

A

Second line treatment of absence seizures. Myoclonic seizures, bipolar disorder (rapid cycling), Migraine prophyaxis, mixed seizures.

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29
Q

Levodopa (L-dopa) Contraindications

A

Psychosis, Cardiac disease, malignant melanoma. Don’r use with MAOIs (HTN crisis).

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30
Q

Pramipexole

A

DA D2 agonist. Used as monotherapy in mild Parkinson’s. Can cause sudden sleep during the day.

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31
Q

Olanzapine (Zyprexa)

A

Atypical Antipsychotic. Can also be used in bipolar disorder. Similar to clozapine without the risk of agranulocytosis. EPS is very rare. Contraindicated in DM due to hyperglycemia.

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32
Q

PCP/Ketamine

A

NMDA receptor antagonists. Developed as general dissociative anesthetics. Cause analgesia accompanied by aggression. Often produces psychosis (treat with haloperidol).

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33
Q

Botulinum Toxin

A

Direct acting muscle relaxant. Inhibits Ach release from the nerve at the junction. Very toxic in large amounts.

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34
Q

Amitriptyline

A

TCA. Tertiary amine (primarily 5HT uptake).

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35
Q

Nigrostriatal DA Pathway

A

SN to the Striaturm. Motor. Parkinson’s (not enough DA) and the side effects of many antipsychotics.

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36
Q

Naltrexone Indications

A

Treatment of alcoholism and opiod addiction. Decreases craving.

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37
Q

Baclofen SE

A

Drowsiness, weakness. Respiratory depression with intrathecal administration (can reduce other SE and increase treatment).

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38
Q

Topiramate Indications

A

Partial and TC seizures. Migraine prevention.

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39
Q

Opiod MOA

A

Closes voltage gated Ca channels on presynaptic nerve terminals to decrease neurotransmitter release and neuronal activity. Decreases glutamate from the dorsal horn or the spinal cord to the brain. Mu receptors also open K channels to hyperpolarize the cell.

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40
Q

Alcohol Withdrawal Treatment

A

Hydration. Diazepam or chlordiazepoxide to prevent seizures/DTs. Lorazepam to treat seizures. Phenytoin is second line to treat seizures.

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41
Q

Pentazocine MOA

A

Mixed Opiod. Kappa agonist (dysphoria) and partial Mu agonist.

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42
Q

DOC for Depression

A

Citalopram

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43
Q

Topiramate MOA

A

Anti-convulsant. Blocks Na channels to potentiate GABA and block glutamate.

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44
Q

SNRI Indications

A

Depression, neuro pain, post menopausal hot flashes. Have more side effects than SSRIs.

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45
Q

Buproprion Contraindications

A

History of seizures.

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46
Q

Dantrolene

A

Direct acting Muscle Relaxant. Inhibits Ca release by blocking the RyR1 channel on the SR (interferes with excitation/contraction coupling). Used in neuroleptic malignant syndrome and malignant hyperthermia.

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47
Q

Vigabatrin SE

A

Visual field problems and retinal damage.

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48
Q

Gabapentin Indications

A

Adjunct use for partial and TC seizures. Neuropathic pain and Bipolar Disorder (rapid cycling).

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49
Q

Clonazepam MOA

A

Benzodiazapine. Stimulates GABA.

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50
Q

Ethosuximide Indications

A

DOC for absence seizures.

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51
Q

Buproprion Indications

A

Refractory depression (combined with SSRIs), ADHD, Alcoholism, smoking cessation (extended release). Causes less sexual dysfunction than the other antidepressants.

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52
Q

Trazodone Indications

A

Sleep aid and pain. Not useful in depression.

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53
Q

Amantadine

A

Antiviral that increases DA transmissioin and is used to treat early/mild cases of parkinson’s or as an adjunct to other treatment . Can cause livedo reticularis (red/blue spotting of skin).

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54
Q

Imipramine

A

TCA. Tertiary amine (primarily 5HT).

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55
Q

Oxymorphone

A

Moderate Opiod. Similar to oxycodone but doesn’t need to be activated by CYP2D6.

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56
Q

GHB

A

GABA receptor weak agonist. Developed as general dissociative anesthetics. Used as date rape drugs.

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57
Q

Carbamazepine MOA

A

Anticonvulsant. Blocks Na channels (decreases glutamate)

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58
Q

Amide Metabolism

A

Metabolized via CYP 450s. Can cause toxicity in patients with liver disease. Excreted by the kidneys.

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59
Q

PTSD Treatment

A

Anti-Depressants

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60
Q

Atomoxetine MOA

A

Selective NE reuptake inhibitor.

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61
Q

Gabapentin MOA

A

Anti-convulsant. GABA analogue.

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62
Q

Phenytoin/Fosphenytoin SE

A

Gingival hyperplasia. Risk of SJS. Teratogenicity.

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63
Q

Methanol Poisoning Treatment

A

Fomepizole (alcohol dehydrogenase inhibitor) can also use ethanol.

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64
Q

Meperidien (demerol) SE

A

Renal failure (don’t use longer than 48 hours), Seizures (due to metabolite normeperidine), Tachycardia. MAOI: serotonin syndrome. No antitussive effects.

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65
Q

Antipsychotic Drug Interactions

A

Sedative-Hypnotics: Increased Sedation Smoking: Induces CYP450s

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66
Q

Naltrexone MOA

A

Opiod receptor antagonist. Reduces craving. Long-acting.

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67
Q

SNRI MOA

A

Inhibits NE and 5HT reuptake

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68
Q

Fluphenazine

A

Classical Antipsychotic. Selective for DA D2 receptors. Less anticholinergic effects so higher risk of EPS.

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69
Q

Meperidien (demerol) MOA

A

Opiod. Mu agonist plus NE/5HT reuptake inhibitor. Also blocks muscarinic receptors.

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70
Q

Diazepam

A

Long- acting Benzodiazepine. Used in anxiety disorders, status epilepticus, alcohol/barbituate withdrawal (prevents seizures) and as a muscle relaxant

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71
Q

Ester Metabolism

A

Metabolized via butyrulcholinesterases in the plasma. Shorter duration of action and increased systemic toxicity. excreted by the kidneys. Has PABA as a metabolite which can cause allergic reactions.

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72
Q

Donepezil

A

Cholinesterase Inhibitor used in Alzheimer’s

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73
Q

Levetricetam SE

A

Dizziness, ataxia, asthenia (weakness), minimal drug interactions.

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74
Q

Hydromorphone

A

Strong opiod

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75
Q

Morphine

A

Strong Opiod. Severe pain. Injected. Associated with itching and vomiting.

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76
Q

Trazodone MOA

A

Anti-depressant. 5HT receptor antagonist.

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77
Q

Chlorpromazine MOA

A

Classical antipsychotic. Blocks DA D2 receptors but also alpha adrenergic and Ach receptors.

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78
Q

Rasagiline SE

A

Causes insomnia (take in the morning). Don’t use with Merperidine (stupor, rigidity, agitation) or TCA/SSRIs (serotonin syndrome).

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79
Q

Benzocaine

A

Ester LA. Topical use only. Pka=3.5 so always in nonionized form.

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80
Q

Acute Alcohol Toxicity Presentation

A

Emesis, stupor, coma, respiratory depression, electrolyte imbalances, hypothermia, decreased BP and CO.

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81
Q

Diazepam MOA

A

Centrally acting muslce relaxant (benzodiazepine). GABAa medicated presynaptic inhibition of the spinal cord. Also used in anxiety disorders, status epilepticus, alcohol/barbituate withdrawal (prevents seizures)

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82
Q

Tramadol Drug interactions

A

Serotonin syndrome if combined with MAOIs, TCAs, SSRIs/ Seizures: antidepressants.

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83
Q

Barbituates SE

A

Low margin of safety! Drowsiness, respiratory depression. Paradoxical excitement. Causes euphoria (drug of abuse) Supra-additive effect with alcohol.

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84
Q

Methamphetamines

A

Increases the release of DA and NE in the basal ganglia.. Rapid physical and psychological dependence. Cardiac toxicity, odor (hyperthermia), meth mouth, meth bugs.

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85
Q

Lithium MOA

A

Suppresses second messengers. Not metabolized. Excreted by the kidneys.

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86
Q

Fluoxetine

A

SSRI. Inhibits CYP450 (drug interactions). Inhibits conversion of codeine to morphine. Impairs BGL in DM.

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87
Q

D2 agonist Side effects

A

Anorexia, N/V, GI upset, Dyskinesias, mental disturbance, decreased prolactin.

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88
Q

Thopental

A

Barbituate. Used for induction of anesthesia.

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89
Q

SSRI Drug Interactions

A

MAOIs: Serotonin syndrome St. Johns Wort: Serotonin syndrome Opiods: Fluoxetine inhibits the conversion of codeine to morphine. Tramadol: inhibits 5HT reuptake and can lead to seizures and serotonin syndrome.

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90
Q

Nitrous Oxide

A

Used as an inhalant. Chronic use causes peripheral neuropathy. Frequently abused by dentists.

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91
Q

Classic Antipsychotics MOA

A

“neuroleptics.” Block DA D2 receptors. Target the mesolimbic system so only alleviates positive symptoms.

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92
Q

Mesolimbic DA Pathway

A

From the VTA to the Limbic system. Emotion. Too much DA causes the positive symptoms of schizophrenia.

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93
Q

Cocaine overdose

A

V-tach and V-fib. Strokes, bleed, seizures.

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94
Q

Pentazocine Indications

A

Moderate pain. Useful in addicts (low abuse potential).

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95
Q

Fetal Alcohol syndrome

A

microceophaly, mental retardation, poor coordination, flat face, joint abnormalities, heart defects, impaired immune system.

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96
Q

Apomorphone

A

DA D2 agonist. Used as “rescue” for the on/off phenomenon in successful L-dopa therapy. Caused N/V give antiemetic (trimethobrinzamide) beforehand.

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97
Q

Metratazpine Indications

A

None of the side effects associated with SSRIs (blocks 5HT in other places). Useful in depression mixed with insomnia or anxiety.

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98
Q

Methadone Indications

A

Treatment for addicts (prevent withdrawal) and long term pain control.

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99
Q

Phenelzine

A

MAOI. Inhibits MAO-A and MAO-B. Drug of last choice for depression. Don’t eat dietary tyramine (HTN crisis).

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100
Q

Lidocaine

A

Amide LA. Rapid onset. Used for infiltrative and epidural blocks. Not for spinal blocks (risk of TNS). Also used as an anti arrhythmic.

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101
Q

Venlaxfaxine

A

SNRI. May increase BP.

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102
Q

Development of Opiod Tolerance

A

Occurs rapidly. NMDA antagonists may decrease the development of tolerance. No tolerance develops to miosis, constipation or seizures.

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103
Q

Ethosuximide MOA

A

Anti-convulsant. Inhibits T-type Ca channels

104
Q

Pharmacokinetic Alcohol Tolerance

A

Increased Alcohol metabolism because CYP2E1 is induced.

105
Q

Benzodiazepines and Alcohol

A

Supra additive effect.

106
Q

SSRI MOA

A

Selectively inhibit 5HT reuptake. Takes 2-3 weeks to have effects.

107
Q

Dextromethorphan MOA

A

Antitussive Opiod. Blocks NMDA and decreases 5HT reuptake.

108
Q

Dextromethorphan Indications

A

Cough suppression. Don’t’ use with MAOIs (serotonin syndrome)

109
Q

Levodopa (L-dopa) SE

A

Has peripheral effects of N/V. Effectiveness will decrease over time. Has no effect on progression.

110
Q

Benzodiazepines MOA

A

CNS depressant. GABAa agonist and increases the affinity for GABA (needs GABA) has ceiling effect.

111
Q

Methadone MOA

A

Opiod. Strong mu agonist that also blocks NMDA and NE/5HT reuptake. Long duration of action. Decreased tolerance.

112
Q

Cholinesterase Inhibitors SE

A

N/V, diarrhea, stomach cramps.

113
Q

Desipramine

A

TCA. Secondary amine (primarily NE)

114
Q

Duloxetine

A

SNRI. Hepatotoxicity.

115
Q

Quetiapine (Seroquel)

A

Atypical Antipsychotic. Used to promote sleep and for sleep maintenance. Similar to clozapine without risk of agranulocytosis. Very sedating. Does not elevate prolactin levels.

116
Q

SSRI SE

A

Mild compared to the TCAs. GI, weight change, CNS stimulation, Sexual dysfunction.

117
Q

Ramelteon Indications

A

Resets sleep-wake cycle. Good for use in addicts.

118
Q

Valproic Acid MOA

A

Anti-convulsant. Blocks Ca channels, Na channels, and may enhance GABA activity.

119
Q

Cocaine as LA

A

Ester LA. Inhibits Na channels secondary to effects on increases DA in the CNS. Used topically. Decreases dental bleeding.

120
Q

Clonazepam Indications

A

Absence and myoclonic seizures. West’s syndrome.

121
Q

Levodopa (L-dopa) Indications

A

Treats Parkinson’s by improving bradykinesia for the first 3-4 years.

122
Q

Effects of Opiods

A

Analgesia (develop tolerance), sedation, euphoria or dysphoria, histamine release (itching), emesis (esp. morphine), Antitussive (codeine and dextromethorphan), respiratory depression (useful in pulmonary edema), elevated intracranial pressure, Miosis (no tolerance), truncal rigidity (fentanyl), CONSTIPATION (no tolerance) Difficulty urinating.

123
Q

Z-Drugs Indications

A

Insomia. Sedation with no anxiolytic, anticonvulsant or muscle relaxant properties.

124
Q

Phenytoin/Fosphenytoin MOA

A

Anticonvulsants. Prolongs inactivation of Na channels (decreases glutamate).

125
Q

Nalaxone

A

Opiod antagonist. Short duration of action. DOC for opiod overdose. Inject until pupils dilate.

126
Q

Benzodiazepines Contraindications

A

Eldery, Sleep apnea, Pregnancy. Avoid abrupt withdrawla (rebound insomnia/anxiety).

127
Q

Topiramate SE

A

Acute myopia and glaucoma.

128
Q

Alprazolam

A

Intermediate-acting Benzodiazepine.

129
Q

Phenobarbital

A

Barbituate. Anticonvulsant (partial seizures and TC seizures). HUGE Inducer CYP 450s.

130
Q

Ramelteon MOA

A

Sedative-hypnotic. Melatonin analogue. No GABA effect.

131
Q

Pentobarbital

A

Barbituate

132
Q

Aripiprazole (Abilify) SE

A

Decreased esophageal motility. Low risk of EPS.

133
Q

Carisoprodol

A

Acute local muscle relaxant. Metabolized to meprobamate (similar to barbituates) drug of abuse (caution in addicts).

134
Q

Z-Drugs SE

A

Large margin of safety. Sleep related behaviors. Elderly may have confusion/memory loss. Rebound insomnia with abrupt withdrawal.

135
Q

Entacapone

A

COMT inhibitor. Inhibits DA and L-dopa metabolism. Increases the pool of L-dopa available for the drain. Causes an orange color in the urine.

136
Q

Acamprosate Indications

A

Treatment of Alcoholism. Decreases craving without liver toxicity.

137
Q

MAOIs SE

A

Orthostatic hypotension, weight gain, insomnia.

138
Q

Risperidone (Risperdal)

A

Atypical Antipsychotic. First line for psychosis. EPS and TD are rare.

139
Q

Nortriptyline

A

TCA. Secondary amine (primarily NE)

140
Q

Codeine MOA

A

Antitussive opiod. Has to be metabolized by CYP2D6 and converted into morphine.

141
Q

Flumazenil Indications

A

Reverses effects of Benzodiazepine. Especially used to reverse Midazolam in surgical procedures.

142
Q

DOC for absence seizures

A

Ethosuximide

143
Q

DOC for Status Epilepticus

A

Diazepam

144
Q

Clozapine

A

Atypical Antipsychotic. Last to choose due to the risk of agranulocytosis (have to monitor CBC closely). EPS and TD are very rare.

145
Q

Ropivacaine

A

Amide LA. Long duration of action. S-enantiomer of bupivacaine (better clearance and less cardiac issues). Causes vasoconstriction.

146
Q

Tuberoinfundibular DA Pathway

A

The hypothalamus to the pituitary (prolactin). Causes the side effects of many antipsychotics.

147
Q

TCA Drug Interactions

A

Metabolized by CYP2D6 MAOIs: Serotonin Syndrome. Potentiate the sedative effects of alcohol and CNS depressants. Potentiate anticholinergic drug effects.

148
Q

Alcohol Metabolism

A

Zero order (Rate is independent of concentration). Alcohol dehydrogenase is major enzyme. Secondary: MEOS and CYP2E1 (increases Acetaminophen toxicity), Induced with chronic consumption.

149
Q

Selegiline

A

MAOI. Only inhibits MAO-B. Increases DA in the brain. Used in Parkinson’s disease.

150
Q

DOC for Anxiety

A

Benzodiazepines

151
Q

Rivastigmine

A

Cholinesterase Inhibitor used in Alzheimer’s

152
Q

Lamotrigine Drug Interactions

A

Half life if DOUBLED with valproic acid.

153
Q

Procaine

A

Ester LA. Short duration of action. Used for diagnostic nerve blocks.

154
Q

Ethosuximide SE

A

Hiccups, SJS.

155
Q

Fosphenytoin

A

Injectable version of phenytoin.

156
Q

Temazepam

A

Benzodiazepine. Used for anxiety disorders and insomnia.

157
Q

Tizanidine

A

Centrally acting muscle relaxant. Alpha 2 receptor agonist. Used for muscle spasm with limited muscle weakness. Very sedating.

158
Q

Acamprosate MOA

A

Structural analogue of GABA. Restores balance between GABA and Glutamate.

159
Q

Metratazpine SE

A

Blocks histamine (drowsiness).

160
Q

Bupivacaine

A

Amide LA. Long duration of action. Used as epidural for labor/delivery. More potent sensory than motor block. High cardiotoxicity

161
Q

Rasagiline MOA

A

MAOI that inhibits DA metabolism especially by MAO-B in the CNS to increase DA in the striatal pathway.

162
Q

MAOIs MOA

A

Irreversibly inhibit MAO which metabolizes NE, DA and 5HT. MAO-A is in the CNS and periphery. MAO-B selectively metabolizes DA in the CNS.

163
Q

Levetricetam Indications

A

Partial and TC seizures. Also used for myoclonic seizures.

164
Q

Extrapyrimidal Symptoms (EPS)

A

Common side effect of antipsychotics (primarily classical). Due to blocking of the nigrostriatal DA pathway. Parkinson’s like side effects (tremor, dyskinesia, rigidity). Treat with an anticholinergic like benztropine to correct the imbalance of DA and Ach.

165
Q

MAOI Drug interactions

A

Serotonin syndrome with: meperidine, dextromethorphan, TCAs, SSRIs. Tramadol: Hyperpyrexia OTC cold meds (sympathomimetics): Severe HTN

166
Q

Alzheimer’s Pathophysiology

A

Degeneration of cholinergic neaurons. Beta-amyloid plaques and tau proteins.

167
Q

Trihexyphenidyl

A

Muscarinic receptor antagonist, restores Ach and DA balance. Used as an adjunct to improve rigidity and tremor.

168
Q

Cocaine MOA

A

Inhibits DA reuptake and secondarily inhibits Na channels.

169
Q

Lamotrigine MOA

A

Anti-convulsant. Inactivation of Na channels.

170
Q

Baclofen MOA

A

Centrally acting muscle relaxant. GABAb agonist (opens K channels causing hyperpolarization) and decreases presynaptic Ca influx (decreases neurotransmitter release).

171
Q

Tigabine MOA

A

Anti-convulsant. Inhibits the reuptake of GABA via GAT1. Short half life. Few drug interactions.

172
Q

DOC for restless leg syndrome

A

Ropinirole

173
Q

Reward Pathway

A

Mesolimbic DA pathway. VTA to the NAc to the prefrontal cortex. All drugs of abuse release DA in the accumbens.

174
Q

Buprenorphine Indications

A

Maintenance treatment of opiod addiction (decreases cravings).

175
Q

Effects of Alcohol

A

CNS: disinhibition, mild euphoria, depressant and sedation. Smooth Muscle: Vasodilation (hypothermia) Heart: Depression of myocardial contractility Kidney: Decreases ADH (Diuresis).

176
Q

Lorazepam

A

Intermediate-acting Benzodiazepine. Used for anxiety disorders and status epilepticus.

177
Q

Barbituate Overdose and Treatment

A

Coma, respiratory depression. Treated by supportive care and alkalizing the urine. Don’t use stimulants.

178
Q

Pharmacodynamic Alcohol Tolerance

A

Down- regulation of GABA receptors and Up-regulation of NMDA receptors (blackout amnesia). Causes Withdrawal symptoms.

179
Q

LSD

A

Act on 5HT receptors in the brain. Doesn’t cause addiction. Euphoria, visual hallucinations, synesthesia.

180
Q

Trazodone SE

A

Sedations, priapism, liver failure.

181
Q

Bath Salts

A

Synthetic Cannabinoid agonist. Has psychoactive properties. Elevated HR and BP.

182
Q

Flurazepam

A

Long-acting Benzodiazepine. Used for anxiety disorders, alcohol/barbituate withdrawal and insomnia.

183
Q

Prochlorpromazine

A

Classical antipsychotic. Same as Chlorpromazine. Used as an antiemetic.

184
Q

Tramadol MOA

A

Moderate Opiod. Weak mu agonist. Inhibits NE/5HT reuptake.

185
Q

Parkinson’s Presentation

A

Bradykinesia (slow movement), Muscle rigidity, resting tremors, impairment of posture balance and gait.

186
Q

Cocaine long term side effects

A

Overall reduction in brain activity. Sever craving. Physical and physiological dependence.

187
Q

Etidocaine

A

Amide LA. Intermediate duration of action. Inverse differential block (causes motor block before or even without sensory block).

188
Q

Hydrocodone

A

Moderate Opiod. Activated by CYP2D6 (variable metabolizers.

189
Q

Buspirone Indications

A

Relieves anxiety with no sedation. Good to use in addicts.

190
Q

Flumazenil Contraindications

A

History of seizures or chronic alcohol abuse.

191
Q

Paroxetine

A

SSRI. Used for OCD and Social Anxiety.

192
Q

Flumazenil MOA

A

Benzodiazepine antagonist

193
Q

Neuroleptic Malignant Syndrome (NMS)

A

Life threatening side effect. Muscle rigidity, hyperprexia. Caused by blockade of DA D2 receptors in the striatum and hypothalamus. Treat with dantrolene.

194
Q

Ziprisadone (Geodon)

A

Atypical Antipsychotic. Used for tourette’s and acute mania. Prolongs QT interval and causes sedation.

195
Q

Nicotine

A

Activates nicotinic receptors in the CNS increases 5HT and DA. Intense psychological and physical dependence. Induces CYP450s.

196
Q

Fentanyl

A

Strong, very potent opiod. Used in short surgical procedures. Truncal rigidity (rapid IV).

197
Q

Levetricetam MOA

A

Anti-convulsant. Binds synaptic vsicular protein (SV2A) to decrease glutamate and increase GABA release.

198
Q

Lithium SE

A

Diabetes insipidus. Small therapeutic window (Extremely toxic in overdose).

199
Q

Chlordiazepoxide

A

Long-acting Benzodiazepine. Used in anxiety disorders and alcohol/barbituate withdrawal (prevent seizures).

200
Q

Amphetamine MOA

A

Increase release of DA by reversing DA transport through the DAT.

201
Q

Effect of Chronic Alcohol Abuse

A

Liver: cirrhosis, alcoholic hepatitis, Liver cancer Malnutrition: Folate and Thiamine CNS effects, Cardiomyopathy, Mild Anemia, Sexual dysfunctioin, respiratory infections (immunosuppressed), Skeletal muscle atrophy, hypothermia, teratogenicity (fetal alcohol syndrome)

202
Q

General Side Effects of Antipsychotics

A

Decreased seizure threshold, Anticholinergic effects, EPS, Tardive Dyskinesia, NMS.

203
Q

St. John’s Wort Drug Interactions

A

Don’t combine with other anti-depressants due to serotonin syndrome.

204
Q

TCA SE

A

Caused by blocking alpha (cardiac depression, arrhythmias), histamine (drowsiness) and Ach (antichol effects) receptors. Weight gain. Analgesia. SIADH. Sexual dysfunction. Decreased seizure threshold. No euphoria (low abuse potential). Can be used in pregnancy.

205
Q

Bromocriptine

A

Ergot derivative that acts as a DA D2 agonist. Side effect of erythromelalgia. Can be used to decrease craving for cocaine.

206
Q

Chloral Hydrate

A

Sedative-Hypnotic. Not highly recommended (low margin of safety) but extremely cheap. Often used in nursing homes.

207
Q

Lamotrigine SE

A

Dizziness, HA, N/V, SJS, rash, teratogenic.

208
Q

Barbituates Contraindications

A

Pulmonary insufficiency, Porphyria (increases porphyrin synthesis).

209
Q

Levodopa (L-dopa) MOA

A

Replacement therapy for Parkinson’s. L-dopa can cross the BBB where it is converted into DA (only 1-3% gets into the brain).

210
Q

Barbituates MOA

A

CNS depressant (hypnosis). GABAa agonist. Binds the receptor and increases the duration of GABA action. Occurs Independent of GABA. No ceiling effect (Low margin of safety).

211
Q

Metaxalone methocarbamol

A

Acute local muscle relaxant.

212
Q

Zaleplone

A

Z-Drug. Short duration of action.

213
Q

Benzotropine

A

Muscarinic receptor antagonist, restores Ach and DA balance. Used as an adjunct to improve rigidity and tremor.

214
Q

TCA Indications

A

Chronic TMJ pain, Fibromyalgia, Depression (last drug of choice).

215
Q

Articaine

A

Amide LA that also has an ester group so metabolized via plasma esterases. Used commonly in dentistry.

216
Q

Buproprion MOA

A

Anti-depressant. Inhibits DA reuptake (little NE and 5HT).

217
Q

Tardive Dyskinesia (TD)

A

Side effect of antipsychotics (least likely to occur with clozapine and olanzapine) especially after long term treatment. Chreiform, uncontrolled jerky movements.

218
Q

Methanol Poisoning Presentation

A

Visual disturbances (being in a snow storm), formaldehyde on breath. Severe metabolic acidosis.

219
Q

Wernicke-korsakoff syndrome

A

paralysis of eye muscles, ataxia, confusion, coma and dearh. Due to thiamine deficiency.

220
Q

Disulfuram (antabuse) Indications

A

Treatment of alcoholism. Not often used. Dangerous.

221
Q

Mesocortical DA Pathway

A

VTA to the frontal cortex. Cognition and Emotion. Not enough DA causes the negative symptoms of schizophrenia.

222
Q

Prilocaine

A

Amide LA. Immediate duration of action. Has the highest rate of clearance of the amides. Risk of methemoglobinemia.

223
Q

Local Anesthetics Transport Across the Membrane

A

Local Anesthetics are weak bases. Must be nonionized to cross the cell membrane. The closer their Pka is to 7.4 the higher concentration is nonionized so the faster it is transported. Inflammation (more acidic) decreases onset of action and bicarb increases the onset of action.

224
Q

Atypical Antipsychotics MOA

A

Blocks 5HT2a and DA D2 and D4 receptors. Targets the mesocortical and mesolimbic systems. Alleviates both positive and negative symptoms.

225
Q

Carbidopa MOA

A

Inhibits dopa-decarboxylase in the periphery. Combined with L-Dopa to decrease the peripheral effects (N/V).

226
Q

Treatment of Anxiety in Children

A

Anti-Depressants

227
Q

Lithium Drug interactions

A

NSAIDs: Increase toxicity. Diueretics: Alter clearance. Competes with Na for reabsorption in the kidney. Decreased Na causes increased lithium toxicity. Increased Na causes an increased excretion of lithium. Increased Lithium causes hyponatremia.

228
Q

Phenytoin/Fosphenytoin Metabolism

A

Metabolized by and induces and inhibits CYP450s. First order elimination at low doses, Zero order elimination at therapeutic doses.

229
Q

Carbidopa SE

A

Postural hypotension, Arrhythmias, HTN, Dyskinesias

230
Q

Aripiprazole (Abilify) MOA

A

Atypical Antipsychotic. Partial agonist for DA D2 and 5HT1a. Antagonist for 5HT2a. “DA system stabilizer” acitvate receptors when DA is too low and blocks them if DA is too high.

231
Q

Acute Alcohol Toxicity Treatment

A

Manage respirations and prevent emesis. Seizures: Lorazepam or phenytoin.

232
Q

Local Anesthetics General MOA

A

Block Na channels to inhibit neuronal firing. Higher affinity for channels in activated or inactivated state, not in resting state. Block in more effective in rapidly firing axons. Elevated Ca will diminish the block and elevated K will increase the block.

233
Q

Sertraline

A

SSRI. Preferred in the elderly. Least drug interactions of the SSRIs.

234
Q

Cocaine Addiction treatment

A

Bromocriptine can decrease craving.

235
Q

Ramelteon SE

A

Drowsiness, dizziness, nausea. Additive sedation with alcohol.

236
Q

Buprenorphine MOA

A

Mixed Opiod. Partial Mu agonist with some Kappa. Often mixed with naloxone (inhibits effects if injected).

237
Q

SSRI Indications

A

Depression, panic disorder, bulimia, alcoholism, and depression in children.

238
Q

Valproic Acid SE

A

Alopecia, hepatotoxictiy, teratogenic.

239
Q

Alcohol Withdrawal Presentation

A

Mild anxiety, irritability, insomnia, nausea, tachycardia. Hallucinations, DTs, seizures, hypotension, arrhythmias.

240
Q

Buspirone MOA

A

Sedative-hypnotic. Partial agonist at postsynaptic 5HT (inhibits signaling) and full agonist at presynaptic 5HT (decreases release of 5HT).

241
Q

Acute Local Muscle Relaxant MOA

A

Acts at the brain stem to decrease neuronal activity in the spinal cord.

242
Q

Gabapentin Metabolism

A

First order elimination. Excreted by the kidneys. Negligible drug interactions.

243
Q

MDMA (ecstasy)

A

Increases 5HT by blocking reuptake and stimulating 5HT receptors. Not addictive because doesn’t effect DA. Leads to hyperthermia and dehydration. Can have persistent memory loss.

244
Q

Chlorpromazine SE

A

High anticholinergic effects so low risk of EPS. Retinal deposits and decreased seizure threshold.

245
Q

Phenytoin/Fosphenytoin Indications

A

Partial and TC seizures.

246
Q

Tetracaine

A

Ester LA. 16x more potent that procaine. Ophthalmologic use (retrobulbar).

247
Q

Oxycodone

A

Moderate Opiod. Activated by CYP2D6 (variable metabolizers.

248
Q

Dibucaine

A

Dibucaine number test to determine butyrylcholinesterase activity to identify mutations or deficiencies.

249
Q

Marijuana (THC)

A

Targets presynaptic cannabinoid (CB1) receptors and inhibits neurotransmitter release (Ach and glutamate). No physiologic dependence but psychological dependence is possible. Amotivational syndrome.

250
Q

Naltrexone SE

A

Liver damage. Don’t use in patients with liver failure. Will precipitate with chronic opiod users.

251
Q

Opiod Drug Interactions

A

Seadtive-hypnotics: CNS and respiratory depression Antipsychotics: sedation and respiratory depression MAOIs: meperidine and dextro can cause serotonin syndrome. Fluoxetine: inhibits metabolsim of coedine to morphine.

252
Q

Cyclobenzaprine

A

Acute local muscle relaxant. Has antimuscarinic action so causes sedation.

253
Q

Oxazepam

A

Intermediate-acting Benzodiazepine.

254
Q

Vigabatrin MOA

A

Anti-convulsant. Irreversibly inhibits AB transaminase (GABA-T) to decrease GABA metabolism.

255
Q

Benzodiazepines SE

A

CNS depression (tolerance will develop), paradoxical excitement (elderly), Sleep related behaviors. High abuse potential.

256
Q

Halperidol

A

Classical Antipsychotic. Injected for acute psychosis. No anticholinergic effects so high risk of EPS.

Pharmacology (24 decks)

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