Neuro/Psych drugs Flashcards
1
Q
Latanoprost (mechanism and use)
A
PGF2a -> increases outflow of aq humor
For glaucoma
2
Q
Latanoprost (side effect)
A
Darkens color of iris (browning)
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
4
Q
Morphine (3 uses)
A
Pain
Pulm edema
Used w/ other CNS depressants during general anesthesia
5
Q
Morphine (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
7
Q
Fentanyl (3 uses)
A
Pain
Pulm edema
Used w/ other CNS depressants during general anesthesia
8
Q
Fentanyl (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
10
Q
Codeine (2 uses)
A
Pain
Pulm edema
11
Q
Codeine (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
13
Q
Loperamide (3 uses)
A
Diarrhea
Pain
Pulm edema
14
Q
Loperamide (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
16
Q
Methadone (3 uses)
A
Maintenance program for heroin addicts (b/c it has longer HL than heroin)
Pain
Pulm edema
17
Q
Methadone (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
19
Q
Meperidine (2 uses)
A
Pain
Pulm edema
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
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
22
Q
Dextromethorphan (3 uses)
A
Cough suppression
Pain
Pulm edema
23
Q
Dextromethorphan (side effects)
A
Opioid overdose stuff (resp depression, constipation, miosis)
Tolerance doesn’t develop to miosis and constipation
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
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)
