Neuro/Psych drugs Flashcards Preview

Pharmacology > Neuro/Psych drugs > Flashcards

Flashcards in Neuro/Psych drugs Deck (208):
1

Latanoprost (mechanism and use)

PGF2a -> increases outflow of aq humor
For glaucoma

2

Latanoprost (side effect)

Darkens color of iris (browning)

3

Morphine (mechanism)

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

4

Morphine (3 uses)

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

5

Morphine (side effects)

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

6

Fentanyl (mechanism)

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

7

Fentanyl (3 uses)

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

8

Fentanyl (side effects)

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

9

Codeine (mechanism)

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

10

Codeine (2 uses)

Pain
Pulm edema

11

Codeine (side effects)

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

12

Loperamide (mechanism)

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

13

Loperamide (3 uses)

Diarrhea
Pain
Pulm edema

14

Loperamide (side effects)

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

15

Methadone (mechanism)

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

16

Methadone (3 uses)

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

17

Methadone (side effects)

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

18

Meperidine (mechanism)

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

19

Meperidine (2 uses)

Pain
Pulm edema

20

Meperidine (side effects)

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

21

Dextromethorphan (mechanism)

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

22

Dextromethorphan (3 uses)

Cough suppression
Pain
Pulm edema

23

Dextromethorphan (side effects)

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

24

Diphenoxylate (mechanism)

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

25

Diphenoxylate (3 uses)

Diarrhea
Pain
Pulm edema

26

Diphenoxylate (side effects)

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

27

Butorphanol (mechanism)

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

28

Butorphanol (use)

Severe pain

29

Butorphanol (side effects)

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

30

Tramadol (mechanism)

Weak mu opioid agonist
Inhibits 5-HT and NE reuptake

31

Tramadol (use)

Chronic pain

32

Tramadol (3 side effects)

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

33

Ethosuximide (mechanism)

Blocks thalamic T-type Ca2+ channels

34

Ethosuximide (use)

1st line for absence seizure

35

Ethosuximide (side effects)

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

36

"-toin" (mechanism)

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

37

"-toin" (4 uses)

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

38

"-toin" (side effects)

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

39

Carbamazepine (mechanism)

Increases Na+ channel inactivation

40

Carbamazepine (5 uses)

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)

41

Carbamazepine (side effecs)

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

42

Valproic acid (mechanism)

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

43

Valproic acid (6 uses)

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

44

Valproic acid (side effects)

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

45

Gabapentin (mechanism)

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

46

Gabapentin (4 uses)

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

47

Gabapentin (2 side effects)

Sedation, ataxia

48

Topiramate (mechanism)

Blocks Na+ channels
Increases GABA action

49

Topiramate (2 uses)

Migraine prevention
Seizures: simple, complex, tonic-clonic

50

Topiramate (4 side effects)

Mental dulling
Kidney stones
Weight loss
Sedation

51

Lamotrigine (mechanism)

Blocks voltage-gated Na+ channels
Anticonvulsant mood stabilizer

52

Lamotrigine (2 uses)

Seizures: simple, complex, tonic-clonic, absence
Depressed phase of bipolar

53

Lamotrigine (side effect)

Stevens-Johnson (must be titrated slowly)

54

Levetiracetam (3 uses)

Seizures: simple, complex, tonic-clonic

55

Tiagabine (mechanism)

Inhibiting GABA reuptake

56

Tiagabine (2 uses)

Seizures: simple, complex

57

Vigabatrin (mechanism)

Irreversibly inhibits GABA transaminase -> reduces catabolism and increases GABA

58

Vigabatrin (2 uses)

Seizures: simple, complex

59

"-barbital" (mechanism)

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

60

"-barbital" (4 uses)

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

61

"-barbital" (side effects and antidotes)

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

62

Thiopental (mechanism)

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

63

Thiopental (4 uses)

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

64

Thiopental (side effects)

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

65

"-zepam" and "-zolam" (mechanism)

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

66

"-zepam" and "-zolam" (7 uses)

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)

67

"-zepam" and "-zolam" (side effects)

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

68

"-zepam" and "-zolam" (antidote)

Flumazenil (competitive antagonist)

69

Chlordiazepoxide (mechanism)

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

70

Chlordiazepoxide (5 uses)

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

71

Chlordiazepoxide (side effects)

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

72

Chlordiazepoxide (antidote)

Flumazenil (competitive antagonist)

73

Zolpidem (mechanism)

"Ambien"
Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

74

Zolpidem (2 uses)

Insomnia, helping you sleep "on an overnight flight to Australia"

75

Zolpidem (side effects)

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

76

Zolpidem (antidote)

Flumazenil (competitive antagonist)

77

Zaleplon (mechanism)

Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

78

Zaleplon (use)

Insomnia

79

Zaleplon (side effects)

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

80

Zaleplon (antidote)

Flumazenil (competitive antagonist)

81

Eszopiclone (mechanism)

Nonbenzo hypnotic: increases GABA activity (BZ1 receptor subtype)

82

Eszopiclone (use)

Insomnia

83

Eszopiclone (side effects)

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

84

Eszopiclone (antidote)

Flumazenil (competitive antagonist)

85

Halothane (mechanism and use)

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

Halothane (side effects)

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

87

"-flurane" (mechanism and use)

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

"-flurane" (side effects)

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

89

Nitrous oxide (mechanism and use)

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

90

Nitrous oxide (side effects)

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

91

Ketamine (mechanism)

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

92

Ketamine (use)

IV ansthetic

93

Ketamine (3 side effects)

Disorientation
Hallucination
Bad dreams

94

Propofol (mechanism)

Potentiates GABA-A

95

Propofol (use)

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

96

"-caine" (mechanism)

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

"-caine" (2 uses)

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

98

"-caine" (side effects)

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

99

"-curium", "-curonium", and "-curarine" (mechanism)

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

100

"-curium", "-curonium", and "-curarine" (use)

Muscle paralysis in surgery or mechanical ventilation

101

"-curium", "-curonium", and "-curarine" (antidote)

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

102

Dantrolene (mechanism)

Prevents release of Ca2+ from sarcoplasmic reticulum of skeletal muscle

103

Dantrolene (2 uses)

Malignant hyperthermia
Neuroleptic malignant syndrome (NMS)

104

Bromocriptine (mechanism)

Ergot D2 agonist

105

Bromocriptine (3 uses)

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

106

Pramipexole (mechanism)

Non-ergot dopamine agonist

107

Pramipexole (use)

Parkinson

108

Ropinirole (mechanism)

Non-ergot dopamine agonist (D2)

109

Ropinirole (use)

Parkinson, restless leg syndrome

110

Amantadine (mechanism)

Increases dopamine release
Prevents viral uncoating

111

Amantadine (2 uses)

Parkinson
Antiviral against influenza A and rubella

112

Amantadine (side effect)

Ataxia

113

Carbidopa (mechanism)

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

114

Carbidopa (use)

Parkinson (w/ l-dopa aka levodopa)

115

Selegiline (mechanism)

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

116

Selegiline (3 uses)

Parkinson (adjunct to l-dopa)
Atypical depression
Anxiety

117

"-capone" (mechanism)

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

118

"-capone" (use)

Parkinson

119

L-dopa/levodopa (mechanism)

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

120

L-dopa/levodopa (side effects)

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

121

L-dopa/levodopa (use)

Parkinson

122

Memantine (mechanism)

NMDA ANTAgonist
Helps prevent excitotoxicity (mediated by Ca2+)

123

Memantine (use)

Alzheimer

124

Memantine (side effects)

Dizziness, confusion, hallucinations

125

Tetrabenazine (mechanism)

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

126

Tetrabenazine (use)

Huntington

127

Reserpine (mechanism)

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

128

Reserpine (use)

Huntington

129

Sumatriptan (mechanism)

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

130

Sumatriptan (2 uses)

Acute migraine
Cluster headache attacks

131

Sumatriptan (3 side effects)

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

132

Ergotamine (mechanism)

Partial agonist at tryptaminergic, dopaminergic, a-adrenergic

133

Ergotamine (2 uses)

Vascular headache prevention
n/v

134

Ergotamine (side effects)

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

135

Methylsergide (mechanism)

Blocks serotonin

136

Methylsergide (2 uses)

Vascular headache prevention
n/v

137

Methylsergide (side effects)

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

138

Methylphenidate (mechanism)

Increases catecholamines at synaptic cleft (esp NE and dopamine)

139

Methylphenidate (3 uses)

ADHD (main)
Narcolepsy
Appetite control

140

"-tamine" (mechanism)

Dextroamphetamine, methamphetamine
Increases catecholamines at synaptic cleft (esp NE and dopamine)

141

"-tamine" (3 uses)

ADHD
Narcolepsy
Appetite control

142

Phentermine (mechanism)

Increases catecholamines at synaptic cleft (esp NE and dopamine)

143

Phentermine (3 uses)

ADHD
Narcolepsy
Appetite control

144

Haloperidol (mechanism)

Neuroleptics/typical antipsychotics
Blocks D2 receptor (thus increases cAMP)

145

Haloperidol (5 uses)

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

146

Haloperidol (side effects)

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

Diphenhydramine (use)

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

148

"-azine" (mechanism)

Neuroleptics/typical antipsychotics
Blocks D2 receptor (thus increases cAMP)

149

"-azine" (4 uses)

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

150

"-azine" (side effects)

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

"-apine" and "-idone" (mechanism)

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

152

"-apine" and "-idone" (5 uses)

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

"-apine" and "-idone" (side effects)

"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

Aripiprazole (mechanism)

Olanzapine, clozapine, quetiapine, risperidone, ziprasidone
Atypical antipsychotics -> varied effects on 5-HT2, dopamine, a, and H1 receptors

155

Aripiprazole (5 uses)

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

Lithium (mechanism)

Not established but possibly inhibits phosphoinositol casecade

157

Lithium (2 uses)

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

158

Lithium (side effects)

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

Buspirone (mechanism)

5-HT(1A) agonist

160

Buspirone (use and side effects)

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

SSRIs (names)

"Flashbacks Paralyze Senior Citizens"
FLuoxetine, PARoxetine, SErtraline, CITalopram

162

SSRIs (4 categories of uses)

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

SSRIs (side effects)

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

Cyproheptadine (mechanism and use)

5-HT2 ANTAgonist (and antihistamine too)
Treat serotonin syndrome (from SSRIs, SNRIs, TCAs, MAO inhibitors)

165

Venlafaxine (mechanism)

SNRI: inhibits reuptake of both 5-HT and NE

166

Venlafaxine (2 uses)

Depression
Anxiety disorders: GAD, panic disorders

167

Venlafaxine (side effects)

HTN, stimulant effects
Sedation, nausea

168

Duloxetine (mechanism)

SNRI: inhibits reuptake of both 5-HT and NE

169

Duloxetine (2 uses)

Depression
Diabetic peripheral neuropathy

170

Duloxetine (side effects)

NE effects: HTN, stimulant effects
Sedation, nausea

171

"-triptyline" and "-ipramine" (mechanism)

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

172

"-triptyline" and "-ipramine" (3 uses)

Major depression
OCD (clomipramine)
Fibromyalgia (amitriptyline)

173

"-triptyline" and "-ipramine" (side effects)

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

Doxepin (mechanism)

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

175

Doxepin (2 uses)

Major depression
Fibromyalgia

176

Doxepin (side effects)

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

Amoxapine (mechanism)

TCA: blocks reuptake of both NE and 5-HT

178

Amoxapine (2 uses)

Major depression
Fibromyalgia

179

Amoxapine (side effects)

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

Tranylcypromine (mechanism)

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

181

Tranylcypromine (2 uses)

Atypical depression
Anxiety

182

Tranylcypromine (side effects)

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

Phenelzine (mechanism)

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

184

Phenelzine (2 uses)

Atypical depression
Anxiety

185

Phenelzine (side effects)

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

Isocarboxazid (mechanism)

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

187

Isocarboxazid (2 uses)

Atypical depression
Anxiety

188

Isocarboxazid (side effects)

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

Bupropion (mechanism and 3 uses)

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

Bupropion (side effects)

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

191

Trazodone (mechanism)

Atypical antidepressant
Blocks 5-HT2 and a1 receptors

192

Trazodone (use)

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

193

Trazodone (side effects)

Priapism
Postural hypotension
Sedation, nausea

194

Primidone (use and side effect)

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

Benzoate (use)

Hyperammonemia (binds AA and leads to excretion)

196

Phenylbutyrate (use)

Hyperammonemia (binds AA and leads to excretion)

197

"-triptyline" and "-ipramine" (antidote)

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

198

Beclofen (mechanism and use)

GABA-B agonist at the level of spinal cord
Muscle relaxant -> for spastic conditions (?)

199

Tolcapone (side effect)

Hepatotoxicity (not in encapone)

200

Buprenorphine (mechanism)

Partial agonist at opioid u receptors

201

Pentazocine (mechanism)

Partial agonist and weak ANTAgonist at opioid u receptors

202

Rilouzole (mechanism and use)

Decreases presynaptic glutamate release
For ALS

203

Baclofen (mechanism and use)

GABA-B receptor agonist -> decreases muscle spasticity
For MS

204

Natalizumab (mechanism and 2 uses)

Mechanism: integrin receptor antagonist
For MS & crohn

205

Natalizumab (side effect)

Increased risk of PML

206

Atracurium (side effect)

Seizure
H1-releasing -> BP falls, flushing, bronchoconstriction

207

Guanethidine (mechanism)

Inhibits NE release

208

Modafinil (mechanism and use)

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