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Pharmacology > Neuro/Psych drugs > Flashcards

Neuro/Psych drugs Flashcards

1
Q

Latanoprost (mechanism and use)

A

PGF2a -> increases outflow of aq humor

For glaucoma

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2
Q

Latanoprost (side effect)

A

Darkens color of iris (browning)

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3
Q

Morphine (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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4
Q

Morphine (3 uses)

A

Pain
Pulm edema
Used w/ other CNS depressants during general anesthesia

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5
Q

Morphine (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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6
Q

Fentanyl (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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7
Q

Fentanyl (3 uses)

A

Pain
Pulm edema
Used w/ other CNS depressants during general anesthesia

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8
Q

Fentanyl (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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9
Q

Codeine (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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10
Q

Codeine (2 uses)

A

Pain

Pulm edema

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11
Q

Codeine (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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12
Q

Loperamide (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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13
Q

Loperamide (3 uses)

A

Diarrhea
Pain
Pulm edema

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14
Q

Loperamide (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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15
Q

Methadone (mechanism)

A 
Opioid analgesics (mu receptor agonist) -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P
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16
Q

Methadone (3 uses)

A

Maintenance program for heroin addicts (b/c it has longer HL than heroin)
Pain
Pulm edema

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17
Q

Methadone (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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18
Q

Meperidine (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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19
Q

Meperidine (2 uses)

A

Pain

Pulm edema

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20
Q

Meperidine (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Reduces seizure threshold
Decrease dose w/ renal dysfx
Tolerance doesn’t develop to miosis and constipation

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21
Q

Dextromethorphan (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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22
Q

Dextromethorphan (3 uses)

A

Cough suppression
Pain
Pulm edema

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23
Q

Dextromethorphan (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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24
Q

Diphenoxylate (mechanism)

A

Opioid analgesics -> G protein linked -> opens K+ channels to increase efflux and closes Ca2+ channels in postsynaptic neurons -> decreases synaptic transmission
Inhibits release of ACh, NE, 5-HT, glutamate, substance P

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25
Q

Diphenoxylate (3 uses)

A

Diarrhea
Pain
Pulm edema

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26
Q

Diphenoxylate (side effects)

A

Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation

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27
Q

Butorphanol (mechanism)

A

Partial agonist at mu opioid receptor and agonist at kappa opioid receptor

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28
Q

Butorphanol (use)

A

Severe pain

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29
Q

Butorphanol (side effects)

A

Causes opioid withdrawal sx if also taking full opioid agonist
Overdose not easily reversed w/ naloxone
Less resp depression than full opioid agonists tho

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30
Q

Tramadol (mechanism)

A

Weak mu opioid agonist

Inhibits 5-HT and NE reuptake

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31
Q

Tramadol (use)

A

Chronic pain

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32
Q

Tramadol (3 side effects)

A

Decreases seizure threshold
Serotonin syndrome
Usual opioid side effects (resp depression, constipation, miosis)

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33
Q

Ethosuximide (mechanism)

A

Blocks thalamic T-type Ca2+ channels

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34
Q

Ethosuximide (use)

A

1st line for absence seizure

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35
Q

Ethosuximide (side effects)

A

EFGHIJ = Ethosuximide causes Fatigue, GI distress, Headache, Itching, stevens-Johnson syndrome

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36
Q

“-toin” (mechanism)

A

Phenytoin (PO), Fosphenytoin (IV)
Increases Na+ channel inactivation
Zero order kinetics

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37
Q

“-toin” (4 uses)

A

1st line for tonic-clonic seizure (like carbamazepine and valproic acid)
1st line prophylaxis for status epilepticus
Simple seizure, complex seizure

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38
Q

“-toin” (side effects)

A 
Megaloblastic anemia
Teratogen (fetal hydantoin syndrome)
SLE-like syndrome
Hirsutism
Gingival hyperplasia
Stevens-Johnson
Lymphadenopathy
Osteopenia
Induces P450
Neuro stuff: nystagmus, diplopia, ataxia, sedation, peripheral neuropathy
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39
Q

Carbamazepine (mechanism)

A

Increases Na+ channel inactivation

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40
Q

Carbamazepine (5 uses)

A 
1st line for trigeminal neuralgia
1st line for simple seizure
1st line for chronic seizure
1st line for tonic-clonic seizure (like phenytoin and valproic acid)
Bipolar (can use as monotherapy)
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41
Q

Carbamazepine (side effecs)

A

Blood dyscrasias (agranulocytosis, aplastic anemia)
Liver toxicity
Teratogen (neural tube, craniofacial, fingernail hypoplasia, delay/growth)
SIADH (exaggerated response to ADH)
Stevens-Johnson
Induces P450
Neuro stuff: diplopia, ataxia

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42
Q

Valproic acid (mechanism)

A

Increases Na+ channel inactivation
Inhibits GABA transaminase -> reduces catabolism and increases GABA concentration
Blocks NMDA receptors in hippocampal neurons
Blocks K+ efflux

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43
Q

Valproic acid (6 uses)

A

1st line for tonic-clonic seizure (like phenytoin and carbamazepine)
Myoclonic seizures
Bipolar disorder (can use as monotherapy)
Simple seizure, complex seizure, absence seizure

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44
Q

Valproic acid (side effects)

A

Hepatotoxicity (rare but fatal, so measure LFTs)
Neural tube defects in fetus
Weight gain
GI distress, tremor

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45
Q

Gabapentin (mechanism)

A

Inhibits high-voltage-activated Ca2+ channels (but actually designed as GABA analog)

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46
Q

Gabapentin (4 uses)

A

Peripheral neuropathy
Postherpetic neuralgia
Migraine prophylaxis
Seizures: simple seizure, complex seizure

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47
Q

Gabapentin (2 side effects)

A

Sedation, ataxia

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48
Q

Topiramate (mechanism)

A

Blocks Na+ channels

Increases GABA action

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49
Q

Topiramate (2 uses)

A

Migraine prevention

Seizures: simple, complex, tonic-clonic

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50
Q

Topiramate (4 side effects)

A

Mental dulling
Kidney stones
Weight loss
Sedation

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51
Q

Lamotrigine (mechanism)

A

Blocks voltage-gated Na+ channels

Anticonvulsant mood stabilizer

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52
Q

Lamotrigine (2 uses)

A

Seizures: simple, complex, tonic-clonic, absence

Depressed phase of bipolar

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53
Q

Lamotrigine (side effect)

A

Stevens-Johnson (must be titrated slowly)

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54
Q

Levetiracetam (3 uses)

A

Seizures: simple, complex, tonic-clonic

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55
Q

Tiagabine (mechanism)

A

Inhibiting GABA reuptake

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56
Q

Tiagabine (2 uses)

A

Seizures: simple, complex

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57
Q

Vigabatrin (mechanism)

A

Irreversibly inhibits GABA transaminase -> reduces catabolism and increases GABA

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58
Q

Vigabatrin (2 uses)

A

Seizures: simple, complex

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59
Q

“-barbital” (mechanism)

A

Barbiturates: phenobarbital, pentobarbital, secobarbital
Increases duration of Cl- channel opening -> facilitates GABA-A action -> decreases neuron firing
Decrease in plasma conc is due to tissue redistribution NOT METABOLISM

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60
Q

“-barbital” (4 uses)

A

Anxiety
Seizures (1st line in neonates): simple, complex, tonic-clonic
Insomnia
Phenobarbital used for Crigler-Najjar syndrome type II (increases liver enzyme synthesis)

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61
Q

“-barbital” (side effects and antidotes)

A

Contraindicated in porphyria
Resp & cardiovascular & CNS depression (esp w/ alcohol)
Induces P450
Overdose tx: supportive + forced alkaline diuresis (diuretic + urinary alkalinization)

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62
Q

Thiopental (mechanism)

A

Barbiturate
Increases duration of Cl- channel opening -> facilitates GABA-A action -> decreases neuron firing
Decrease in plasma conc is due to tissue redistribution (to skeletal muscle and fat) NOT METABOLISM

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63
Q

Thiopental (4 uses)

A

Anesthesia induction & short surgical procedure (effects terminated by rapid redistribution into tissue and fat)
Anxiety
Seizures (1st line in neonates): simple, complex, tonic-clonic
Insomnia

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64
Q

Thiopental (side effects)

A

Contraindicated in porphyria
Resp & cardiovascular & CNS depression (esp w/ alcohol)
Decreases cerebral blood flow (unlike inhaled anesthetics)
Induces P450
Overdose tx: supportive

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65
Q

“-zepam” and “-zolam” (mechanism)

A

Benzodiazepines: short acting (ATrOM: alprazolam, triazolam, oxazepam, midazolam), medium acting (first 2 syllables sound like names: estazolam, lorazepam, temazepam), long acting (chlordiazepoxide, clorazepate, diazepam, flurazepam)
Increases frequency of Cl- channel opening -> facilitates GABA-A action -> decreases neuron firing

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66
Q

“-zepam” and “-zolam” (7 uses)

A

Benzodiazepines: short acting (ATrOM: alprazolam, triazolam, oxazepam, midazolam), medium acting (first 2 syllables sound like names: estazolam, lorazepam, temazepam), long acting (chlordiazepoxide, clorazepate, diazepam, flurazepam)
Anxiety
Spasticity
1st line for acute status epilepticus (lorazepam and diazepam)
Detoxification (esp in alcohol withdrawal - DTs)
Sleep stuff: night terror, sleepwalking, hypnotic
General anesthetic (amnesia, muscle relaxation; midazolam most common drug used for endoscopy)
Eclampsia seizure (1st line is MgSO4 tho)

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67
Q

“-zepam” and “-zolam” (side effects)

A

Benzodiazepines: short acting (ATrOM: alprazolam, triazolam, oxazepam, midazolam), medium acting (first 2 syllables sound like names: estazolam, lorazepam, temazepam), long acting (chlordiazepoxide, clorazepate, diazepam, flurazepam)
CNS depression (esp w/ alcohol)
Anterograde amnesia
Less risk of resp depression & coma compared to barbiturates
Short acting: higher risk of dependence but less risk of falls
Long acting: less risk of dependence but higher risk of falls

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68
Q

“-zepam” and “-zolam” (antidote)

A

Flumazenil (competitive antagonist)

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69
Q

Chlordiazepoxide (mechanism)

A 
Benzodiazepine
Increases frequency (instead of duration) of Cl- channel opening -> facilitates GABA-A action -> decreases neuron firing
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70
Q

Chlordiazepoxide (5 uses)

A

Anxiety
Spasticity
Detoxification (esp in alcohol withdrawal - DTs)
Sleep stuff: night terror, sleepwalking, hypnotic
General anesthetic (amnesia, muscle relaxation)

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71
Q

Chlordiazepoxide (side effects)

A

CNS depression (esp w/ alcohol)
Anterograde amnesia
Less risk of resp depression & coma compared to barbiturates
Dependence

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72
Q

Chlordiazepoxide (antidote)

A

Flumazenil (competitive antagonist)

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73
Q

Zolpidem (mechanism)

A

“Ambien”

Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

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74
Q

Zolpidem (2 uses)

A

Insomnia, helping you sleep “on an overnight flight to Australia”

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75
Q

Zolpidem (side effects)

A

Neuro stuff: ataxia, headaches, confusion
Rapid metab so short duration
The good: compared to older sedative-hypnotics, only modest day-after psychomotor depression and few amnestic effects and less dependence risk

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76
Q

Zolpidem (antidote)

A

Flumazenil (competitive antagonist)

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77
Q

Zaleplon (mechanism)

A

Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

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78
Q

Zaleplon (use)

A

Insomnia

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79
Q

Zaleplon (side effects)

A

Neuro stuff: ataxia, headaches, confusion
Rapid metab so short duration
The good: compared to older sedative-hypnotics, only modest day-after psychomotor depression and few amnestic effects and less dependence risk

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80
Q

Zaleplon (antidote)

A

Flumazenil (competitive antagonist)

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81
Q

Eszopiclone (mechanism)

A

Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

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82
Q

Eszopiclone (use)

A

Insomnia

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83
Q

Eszopiclone (side effects)

A

Neuro stuff: ataxia, headaches, confusion
Rapid metab so short duration
The good: compared to older sedative-hypnotics, only modest day-after psychomotor depression and few amnestic effects and less dependence risk

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84
Q

Eszopiclone (antidote)

A

Flumazenil (competitive antagonist)

85
Q

Halothane (mechanism and use)

A

Inhaled anesthetics -> myocardial/resp depression, nausea, increases cerebral blood flow (and decreases cerebral metabolic demand)
Preferred in asthma (along w/ sevoflurane) bc of its bronchodilation properties

86
Q

Halothane (side effects)

A 
Hepatotoxicity (massive hepatic necrosis)
Malignant hyperthermia (hereditary condition; treat w/ dantrolene)
87
Q

“-flurane” (mechanism and use)

A

Enflurane, isoflurane, sevoflurane, methoxyflurane
Inhaled anesthetics -> myocardial/resp depression, nausea, increases cerebral blood flow (and decreases cerebral metabolic demand)
Sevoflurane is preferred in asthma (along w/ halothane) bc of its bronchodilation properties

88
Q

“-flurane” (side effects)

A

Malignant hyperthermia (hereditary condition; treat w/ dantrolene)
Nephrotoxicity w/ methoxyflurane
Proconvulsant w/ enflurane

89
Q

Nitrous oxide (mechanism and use)

A

Inhaled anesthetics -> myocardial/resp depression, nausea, increases cerebral blood flow (and decreases cerebral metabolic demand)

90
Q

Nitrous oxide (side effects)

A 
Malignant hyperthermia (hereditary condition; treat w/ dantrolene)
Expansion of trapped gas in body cavity
91
Q

Ketamine (mechanism)

A

An arylcyclohexylamine; PCP analog that acts as dissociative anesthetics
Blocks NMDA receptor (noncompetitive antagonist of glutamate) -> cardiovascular stimulants and increases cerebral blood flow

92
Q

Ketamine (use)

A

IV ansthetic

93
Q

Ketamine (3 side effects)

A

Disorientation
Hallucination
Bad dreams

94
Q

Propofol (mechanism)

A

Potentiates GABA-A

95
Q

Propofol (use)

A

IV anesthetics -> sedation in ICU, rapid induction, short procedures
Less postop nausea than thiopental

96
Q

“-caine” (mechanism)

A 
Local anesthetics (esters have one I in the name, amides have 2 I's)
Blocks Na+ channels, prefers activated Na+ channels so most effective in rapidly firing neurons (small myelinated fibers > small unmyelinated fibers > large myelinated fibers > large unmyelinated fibers; SO affects pain before temp before touch before pressure)
Tertiary amines penetrate membrane in uncharged form then binds ion channels as charged form (so need to use more in infected/acidic tissue)
97
Q

“-caine” (2 uses)

A

Minor surgical procedure
Spinal anesthesia
Can be given w/ vasoconstrictor (epinephrine) to enhance local action

98
Q

“-caine” (side effects)

A

CNS excitation
Severe cardiovascular toxicity w/ bupivacaine
HTN, hypotension
Arrhythmias (cocaine)

99
Q

“-curium”, “-curonium”, and “-curarine” (mechanism)

A

Atracurium, mivacurium, pancuronium, vecuronium, rocuronium, tubocurarine
Non-depolarizing neuromuscular blockage (competitive antagonist at ACh receptors, selective for motor nicotinic receptors rather than autonomic)

100
Q

“-curium”, “-curonium”, and “-curarine” (use)

A

Muscle paralysis in surgery or mechanical ventilation

101
Q

“-curium”, “-curonium”, and “-curarine” (antidote)

A

AChEi, esp neostigmine (given w/ atropine), edrophonium

102
Q

Dantrolene (mechanism)

A

Prevents release of Ca2+ from sarcoplasmic reticulum of skeletal muscle

103
Q

Dantrolene (2 uses)

A

Malignant hyperthermia

Neuroleptic malignant syndrome (NMS)

104
Q

Bromocriptine (mechanism)

A

Ergot D2 agonist

105
Q

Bromocriptine (3 uses)

A

Parkinson (but non-ergot preferred)
Pituitary adenoma
Neuroleptic malignant syndrome (NMS)

106
Q

Pramipexole (mechanism)

A

Non-ergot dopamine agonist

107
Q

Pramipexole (use)

A

Parkinson

108
Q

Ropinirole (mechanism)

A

Non-ergot dopamine agonist (D2)

109
Q

Ropinirole (use)

A

Parkinson, restless leg syndrome

110
Q

Amantadine (mechanism)

A

Increases dopamine release

Prevents viral uncoating

111
Q

Amantadine (2 uses)

A

Parkinson

Antiviral against influenza A and rubella

112
Q

Amantadine (side effect)

A

Ataxia

113
Q

Carbidopa (mechanism)

A

Inhibits peripheral DOPA decarboxylase inhibitor -> decreases peripheral metabolism of levodopa (so more levodopa reaches CNS and less systemic side effects)

114
Q

Carbidopa (use)

A

Parkinson (w/ l-dopa aka levodopa)

115
Q

Selegiline (mechanism)

A

Selective MAO-B inhibitor -> decreases central dopamine degradation (MAO-B prefers to metabolize dopamine over NE and 5-HT)
Irreversible

116
Q

Selegiline (3 uses)

A

Parkinson (adjunct to l-dopa)
Atypical depression
Anxiety

117
Q

“-capone” (mechanism)

A

Entacapone (peripheral COMT), tolcapone (central and peripheral COMT)
COMT inhibitors -> prevents l-dopa degradation so there’s more dopamine available

118
Q

“-capone” (use)

A

Parkinson

119
Q

L-dopa/levodopa (mechanism)

A

Increases dopamine level in brain (can cross BBB unlike dopamine)
Converted by dopa decarboxylase in CNS to dopamine

120
Q

L-dopa/levodopa (side effects)

A

Arrhythmias (from peripheral conversion to catecholamines)
Dyskinesia after administration (long-term use)
Akinesia between doses

121
Q

L-dopa/levodopa (use)

A

Parkinson

122
Q

Memantine (mechanism)

A

NMDA ANTAgonist

Helps prevent excitotoxicity (mediated by Ca2+)

123
Q

Memantine (use)

A

Alzheimer

124
Q

Memantine (side effects)

A

Dizziness, confusion, hallucinations

125
Q

Tetrabenazine (mechanism)

A

Inhibits VMAT (vesicular monoamine transporter) -> limits dopamine packaging and release

126
Q

Tetrabenazine (use)

A

Huntington

127
Q

Reserpine (mechanism)

A

Inhibits VMAT (vesicular monoamine transporter) -> limits dopamine packaging into presynaptic vesicles and release

128
Q

Reserpine (use)

A

Huntington

129
Q

Sumatriptan (mechanism)

A

5-HT(1B/1D) agonist -> inhibits trigeminal nerve activation, prevents vasoactive peptide release, induces vasoconstriction
Short HL

130
Q

Sumatriptan (2 uses)

A

Acute migraine

Cluster headache attacks

131
Q

Sumatriptan (3 side effects)

A 
Coronary vasospasm (don't use if CAD or Prinzmetal angina)
Mild tingling
HTN crisis (don't use if BP poorly controlled)
132
Q

Ergotamine (mechanism)

A

Partial agonist at tryptaminergic, dopaminergic, a-adrenergic

133
Q

Ergotamine (2 uses)

A

Vascular headache prevention

n/v

134
Q

Ergotamine (side effects)

A

Contraindicated in Prinzmetal angina (but doesn’t cause HTN crisis
Cyanosis, absent peripheral pulse, gangrene

135
Q

Methylsergide (mechanism)

A

Blocks serotonin

136
Q

Methylsergide (2 uses)

A

Vascular headache prevention

n/v

137
Q

Methylsergide (side effects)

A

FIBROSIS: retroperitoneal fibrosis, pleuropulmonary fibrosis, fibrotic thickening of cardiac valve

138
Q

Methylphenidate (mechanism)

A

Increases catecholamines at synaptic cleft (esp NE and dopamine)

139
Q

Methylphenidate (3 uses)

A

ADHD (main)
Narcolepsy
Appetite control

140
Q

“-tamine” (mechanism)

A

Dextroamphetamine, methamphetamine

Increases catecholamines at synaptic cleft (esp NE and dopamine)

141
Q

“-tamine” (3 uses)

A

ADHD
Narcolepsy
Appetite control

142
Q

Phentermine (mechanism)

A

Increases catecholamines at synaptic cleft (esp NE and dopamine)

143
Q

Phentermine (3 uses)

A

ADHD
Narcolepsy
Appetite control

144
Q

Haloperidol (mechanism)

A

Neuroleptics/typical antipsychotics

Blocks D2 receptor (thus increases cAMP)

145
Q

Haloperidol (5 uses)

A

Huntington
Schizophrenia (primarily positive sx), psychosis, acute mania
Tourette syndrome

146
Q

Haloperidol (side effects)

A

4 hrs: acute dystonia
4 days: akathisia (restlessness)
4 weeks: bradykinesia (parkinsonism)
4 mos: Tardive dyskinesia
NMS: about 7-10 days, think FEVER (Fever, Encephalopathy, Vitals unstable, Enzymes go up, Rigidity)
Long-term: hyperprolactinemia from antagonizing dopamine receptor

147
Q

Diphenhydramine (use)

A

Treats extrapyramidal side effects of typical antipsychotics like dyskinesias (along w/ benztropine)
Anaphylaxis (after pt is stabilized by epinephrine)

148
Q

“-azine” (mechanism)

A

Neuroleptics/typical antipsychotics

Blocks D2 receptor (thus increases cAMP)

149
Q

“-azine” (4 uses)

A

Schizophrenia (primarily positive sx), psychosis, acute mania
Tourette syndrome

150
Q

“-azine” (side effects)

A 
Low potency (Cheating Thieves are low): Chlorpromazine, Thioridazine -> anticholinergic, antihistamine, a1-blockade effects; corneal deposits w/ chlorpromazine; retinal deposits w/ thioridazine
High potency (Try to Fly High): Trifluoperazine, Fluphenazine, Haloperidol -> EPS sx (4 hrs: acute dystonia; 4 days: akathisia aka restlessness; 4 weeks: bradykinesia aka parkinsonism; 4 mos: tardive dyskinesia; NMS: about 7-10 days)
Long-term: hyperprolactinemia from antagonizing dopamine receptor
151
Q

“-apine” and “-idone” (mechanism)

A

Atypical antipsychotics -> varied effects on 5-HT2, dopamine, a, and H1 receptors

152
Q

“-apine” and “-idone” (5 uses)

A

Schizophrenia (both positive and negative sx, unlike typical antipsychotics which affect mostly positive sx)
Mood disorders: bipolar, depression, mania
OCD
Anxiety disorder
Tourette syndrome

153
Q

“-apine” and “-idone” (side effects)

A

“it’s atypical for Old Closets to Quietly Risper from A to Z”: Olanzapine, Clozapine, Quetiapine, Risperidone, Aripiprazole, Ziprasidone
Overall fewer side effects than traditional antipsychotics
Watch clozapine closely! -> weight gain (also in olanzapine), agranulocytosis (weekly WBC monitoring), seizures
Risperidone causes reproductive issues (increases prolactin and thus decreases GnRH, LH, FSH)
Ziprasidone prolongs QT

154
Q

Aripiprazole (mechanism)

A

Olanzapine, clozapine, quetiapine, risperidone, ziprasidone

Atypical antipsychotics -> varied effects on 5-HT2, dopamine, a, and H1 receptors

155
Q

Aripiprazole (5 uses)

A

Schizophrenia (both positive and negative sx, unlike typical antipsychotics which affect mostly positive sx)
Mood disorders: bipolar, depression, mania
OCD
Anxiety disorder
Tourette syndrome
Overall fewer side effects than traditional antipsychotics

156
Q

Lithium (mechanism)

A

Not established but possibly inhibits phosphoinositol casecade

157
Q

Lithium (2 uses)

A

Bipolar (mood stabilizer, blocks relapse and acute manic events)
SIADH

158
Q

Lithium (side effects)

A

Narrow therapeutic window
Tremor
Nephrogenic DI (antagonizing effects on ADH action in collecting duct system -> “renal tubular dysfx”)
Hypothyroidism
Pregnancy problems (Ebstein anomaly, malformation of great vessels)
Sedation, edema, heart block
Exclusively secreted by kidneys (most is reabsorbed at PCT following Na+ reabsorption)

159
Q

Buspirone (mechanism)

A

5-HT(1A) agonist

160
Q

Buspirone (use and side effects)

A

1st line for GAD -> takes 1-2 weeks to take effect
Doesn’t cause sedation, addiction, tolerance
Doesn’t interact w/ alcohol like barbiturates and benzos
Doesn’t cause sexual dysfx like SSRIs

161
Q

SSRIs (names)

A

“Flashbacks Paralyze Senior Citizens”

FLuoxetine, PARoxetine, SErtraline, CITalopram

162
Q

SSRIs (4 categories of uses)

A

SSRI
Depression (normally takes 4-8 weeks for antidepressants to have an effect)
Bulimia
Anxiety disorders: GAD, panic disorder, OCD, social phobias, PTSD
Premature ejaculation

163
Q

SSRIs (side effects)

A 
SSRI
Overall fewer than TCAs
Sexual dysfx
GI distress
Serotonin syndrome -> hyperthermia, confusion, myoclonus (contrast to NMS!), cardiovascular collapse, flushing, diarrhea, seizures -> treats w/ cyproheptadine
164
Q

Cyproheptadine (mechanism and use)

A

5-HT2 ANTAgonist (and antihistamine too)

Treat serotonin syndrome (from SSRIs, SNRIs, TCAs, MAO inhibitors)

165
Q

Venlafaxine (mechanism)

A

SNRI: inhibits reuptake of both 5-HT and NE

166
Q

Venlafaxine (2 uses)

A

Depression

Anxiety disorders: GAD, panic disorders

167
Q

Venlafaxine (side effects)

A

HTN, stimulant effects

Sedation, nausea

168
Q

Duloxetine (mechanism)

A

SNRI: inhibits reuptake of both 5-HT and NE

169
Q

Duloxetine (2 uses)

A

Depression

Diabetic peripheral neuropathy

170
Q

Duloxetine (side effects)

A

NE effects: HTN, stimulant effects

Sedation, nausea

171
Q

“-triptyline” and “-ipramine” (mechanism)

A

Amitriptyline, nortriptyline, imipramine, desipramine, clomipramine
TCA: presynaptic NONSELECTIVE monoamine reuptake -> blocks reuptake of both NE and 5-HT

172
Q

“-triptyline” and “-ipramine” (3 uses)

A

Major depression
OCD (clomipramine)
Fibromyalgia (amitriptyline)

173
Q

“-triptyline” and “-ipramine” (side effects)

A

Tri-C’s: Convulsion, Coma, Cardiotoxicity
WHAT KILLS YOU: blocks cardiac fast Na+ channels -> quinidine-like -> prolongs QRS and QT -> treat cardio stuff w/ NaHCO3
NE & serotonin effects: seizures, tremor, insomnia
Anti a-1 effect: l hypotension (anti-a1)
Anti-musca effects (think atropine overdose): so careful w/ BPH (causes urinary retention); 3rd gen like amitriptyline is worse at this than 2nd gen like nortriptyline, so use nortriptyline in elderly b/c less confusion and hallucinations
Anti H1 effects: sedation (desipramine better at this, but has a higher seizure incidence)

174
Q

Doxepin (mechanism)

A

TCA: presynaptic NONSELECTIVE monoamine reuptake -> blocks reuptake of both NE and 5-HT

175
Q

Doxepin (2 uses)

A

Major depression

Fibromyalgia

176
Q

Doxepin (side effects)

A

Tri-C’s: Convulsion, Coma, Cardiotoxicity
Blocks cardiac fast Na+ channels -> quinidine-like -> prolongs QRS and QT -> treat cardio stuff w/ NaHCO3
NE & serotonin effects: tremor & insomnia
Anti a-1 effect: postural hypotension (anti-a1)
Anti-musca effects (think atropine overdose): so careful w/ BPH (causes urinary retention); 3rd gen like amitriptyline is worse at this than 2nd gen like nortriptyline, so use nortriptyline in elderly b/c less confusion and hallucinations
Anti H1 effects: sedation (desipramine better at this, but has a higher seizure incidence)

177
Q

Amoxapine (mechanism)

A

TCA: blocks reuptake of both NE and 5-HT

178
Q

Amoxapine (2 uses)

A

Major depression

Fibromyalgia

179
Q

Amoxapine (side effects)

A

Tri-C’s: Convulsion, Coma, Cardiotoxicity
Blocks cardiac fast Na+ channels -> quinidine-like -> prolongs QRS and QT -> treat cardio stuff w/ NaHCO3
NE & serotonin effects: tremor & insomnia
Anti a-1 effect: postural hypotension (anti-a1)
Anti-musca effects (think atropine overdose): so careful w/ BPH (causes urinary retention); 3rd gen like amitriptyline is worse at this than 2nd gen like nortriptyline, so use nortriptyline in elderly b/c less confusion and hallucinations
Anti H1 effects: sedation (desipramine better at this, but has a higher seizure incidence)

180
Q

Tranylcypromine (mechanism)

A

Nonselective MAO inhibitor (so increases NE, 5-HT, dopamine)

Irreversible

181
Q

Tranylcypromine (2 uses)

A

Atypical depression

Anxiety

182
Q

Tranylcypromine (side effects)

A

HTN crisis (esp w/ ingestion of tyramine like wine and cheese)
CNS stimulation
Don’t use w/ SSRIs, TCA, St. John’s wort, meperidine, dextromethorphan -> prevents serotonin syndrome

183
Q

Phenelzine (mechanism)

A

Nonselective MAO inhibitor (so increases NE, 5-HT, dopamine)

Irreversible

184
Q

Phenelzine (2 uses)

A

Atypical depression

Anxiety

185
Q

Phenelzine (side effects)

A

HTN crisis (esp w/ ingestion of tyramine like wine and cheese)
CNS stimulation
Don’t use w/ SSRIs, TCA, St. John’s wort, meperidine, dextromethorphan -> prevents serotonin syndrome

186
Q

Isocarboxazid (mechanism)

A

Nonselective MAO inhibitor (so increases NE, 5-HT, dopamine)

187
Q

Isocarboxazid (2 uses)

A

Atypical depression

Anxiety

188
Q

Isocarboxazid (side effects)

A

HTN crisis (esp w/ ingestion of tyramine like wine and cheese)
CNS stimulation
Don’t use w/ SSRIs, TCA, St. John’s wort, meperidine, dextromethorphan -> prevents serotonin syndrome

189
Q

Bupropion (mechanism and 3 uses)

A

Atypical antidepressant
Presynaptic selective NE reuptake inhibitor -> increases NE and dopamine
For smoking cessation and hypoactive sexual disorder
NO sexual side effects so can use as alternate/adjunct of SSRIs

190
Q

Bupropion (side effects)

A

Seizure in bulimic pts
Stimulant effects (tachycardia, insomnia)
Headache
NO sexual side effects like SSRIs

191
Q

Trazodone (mechanism)

A

Atypical antidepressant

Blocks 5-HT2 and a1 receptors

192
Q

Trazodone (use)

A

Insomnia

It’s an atypical antidepressant, but high doses needed for antidepressant effects

193
Q

Trazodone (side effects)

A

Priapism
Postural hypotension
Sedation, nausea

194
Q

Primidone (use and side effect)

A

Anticonvulsant and essential tremor (so use this in pts w/ seizures AND essential tremor who also has asthma so you know can’t use B blocker)
Sedation
Metabolites are phenobarbital and phenylethylmalonamide -> measure phenobarbital activity in blood if wanna know activity

195
Q

Benzoate (use)

A

Hyperammonemia (binds AA and leads to excretion)

196
Q

Phenylbutyrate (use)

A

Hyperammonemia (binds AA and leads to excretion)

197
Q

“-triptyline” and “-ipramine” (antidote)

A

Sodium bicarbonate -> corrects cardiotoxicity (QRS and QT prolongation, hypotension)

198
Q

Beclofen (mechanism and use)

A

GABA-B agonist at the level of spinal cord

Muscle relaxant -> for spastic conditions (?)

199
Q

Tolcapone (side effect)

A

Hepatotoxicity (not in encapone)

200
Q

Buprenorphine (mechanism)

A

Partial agonist at opioid u receptors

201
Q

Pentazocine (mechanism)

A

Partial agonist and weak ANTAgonist at opioid u receptors

202
Q

Rilouzole (mechanism and use)

A

Decreases presynaptic glutamate release

For ALS

203
Q

Baclofen (mechanism and use)

A

GABA-B receptor agonist -> decreases muscle spasticity

For MS

204
Q

Natalizumab (mechanism and 2 uses)

A

Mechanism: integrin receptor antagonist

For MS & crohn

205
Q

Natalizumab (side effect)

A

Increased risk of PML

206
Q

Atracurium (side effect)

A

Seizure

H1-releasing -> BP falls, flushing, bronchoconstriction

207
Q

Guanethidine (mechanism)

A

Inhibits NE release

208
Q

Modafinil (mechanism and use)

A

Non-amphetamine stimulant thought to enhance dopaminergic signaling
1st line for narcolepsy (2nd line is amphetamine)

Pharmacology (12 decks)

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