MBB1 Drugs- Vitor's Cards Flashcards
1
Q
Venlafaxine
A
Class: Antidepressants (SNRIs (Seretonin and NE reuptake inhibitors))
Mechanism of Action: -Inhibit SERT and NET -Mechanism for analgesic effects is uncertain
Indications: -Neuropathic pain -Anxiety (GAD) -Depression
Primary Adverse Effects: -GI disturbances -Sedation -Sexual dysfunction Other Comments: Bolded Drug: Duloxetine
2
Q
Capsaicin
A
Class: External analgesic Mechanism of Action: Depletes and prevents reaccumulation of substance P in peripheral sensory neurons Indications: Neuropathic pain Primary Adverse Effects: Other Comments:
3
Q
Bethanechol
A
Class: mAChR agonist
Mechanism of Action: Stimulates mAChR in bladder -> emptying
Indications: Neurogenic bladder due to spinal cord injury or autonomic neuropathy
Primary Adverse Effects: mAChR Agonist side effects: GI side effects, hypersalivation, lacrimation, urinary urgency
Other Comments: May cause bronchospasm and wheezing.
4
Q
Oxybutynin
A
Class: mAChR Antagonist
Mechanism of Action: Blocks mAChR in bladder -> less tone –> Less involuntary leakage
Indications: Neurogenic bladder due to spinal cord injury or MS
Primary Adverse Effects: mAChR antagonist side effects: Xerostomia, urinary retention, confusion, sedation
Other Comments:
5
Q
Tolterodine
A
Class: mAChR Antagonist Mechanism of Action: Blocks mAChR in bladder –> Less bladder tone –> Less incontinence Indications: Neurogenic bladder due to spinal cord injury or MS Primary Adverse Effects: mAChR antagonist side effects: Xerostomia, urinary retention, confusion, sedation Other Comments:
6
Q
Ephedrine
A
Class: Indirect sympathomimetics Mechanism of Action: Stimulate alpha1 receptors in bladder neck -> contraction -> more bladder storage capacity Indications: Neurogenic bladder due to spinal cord injury Primary Adverse Effects: alpha1 side effects: Increased HR and BP Other Comments:
7
Q
Prazosin
A
Class: alpha1 antagonist Mechanism of Action: Blocks alpha1 receptors in bladder neck –> relaxation –> Emptying Indications: Neurogenic bladder due to spinal cord injury or autonomic neuropathy Primary Adverse Effects: alpha1 antagonist side effects: Orthostatic hypotension Other Comments:
8
Q
Terazosin
A
Class: alpha1 antagonist Mechanism of Action: Blocks alpha1 receptors in bladder neck –> relaxation –> Emptying Indications: Neurogenic bladder due to spinal cord injury or autonomic neuropathy Primary Adverse Effects: alpha1 antagonist side effects: Orthostatic hypotension Other Comments:
9
Q
Mirabegron
A
Class: beta3 agonist Mechanism of Action: Stiulates beta3 receptors in bladder –> less bladder tone –> Less incontinence Indications: Overactive bladder Primary Adverse Effects: Increased BP, UTI, headache Other Comments: -Caution in patients with HTN
10
Q
Ondasetron
A
Class: 5-HT3 antagonists “Setrons” Mechanism of Action: Blocks 5-HT3 receptors on vagal afferents, GI tract, Chemoreceptor trigger zone, and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Radiation induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Minor side effects (headache, dizziness) -Long QT interval Other Comments:
11
Q
Dolasetron
A
Class: 5-HT3 antagonists “Setrons” Mechanism of Action: Blocks 5-HT3 receptors on vagal afferents, GI tract, Chemoreceptro trigger zone, and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Radiation induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Minor side effects (headache, dizziness) -Long QT interval Other Comments: Bolded Drug: Ondansetron
12
Q
Granisetron
A
Class: 5-HT3 antagonists “Setrons” Mechanism of Action: Blocks 5-HT3 receptors on vagal afferents, GI tract, Chemoreceptro trigger zone, and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Radiation induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Minor side effects (headache, dizziness) -Long QT interval Other Comments: Bolded Drug: Ondansetron
13
Q
Palonosetron
A
Class: 5-HT3 antagonists “Setrons” Mechanism of Action: Blocks 5-HT3 receptors on vagal afferents, GI tract, Chemoreceptro trigger zone, and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Radiation induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Minor side effects (headache, dizziness) Other Comments: -Bolded Drug: Ondansetron -Doesn’t cause Long QT interval
14
Q
Metoclopramide
A
Class: D2 Antagonists Mechanism of Action: Blocks D2 receptors in Chemoreceptor trigger zone and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Migrane induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Extrapyramidal signs -mAChR Antagonist side effects Other Comments: -Good “general purpose” antiemetics
15
Q
Prochlorperazine
A
Class: D2 Antagonists Mechanism of Action: Blocks D2 receptors in Chemoreceptor trigger zone and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Migrane induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Extrapyramidal signs -mAChR Antagonist side effects Other Comments: -Bolded Drug: Metoclopramide -Good “general purpose” antiemetics
16
Q
Promethazine
A
Class: D2 Antagonists Mechanism of Action: Blocks D2 receptors in Chemoreceptor trigger zone and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Migrane induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Extrapyramidal signs -mAChR Antagonist side effects Other Comments: -Bolded Drug: Metoclopramide -Good “general purpose” antiemetics
17
Q
Droperidol
A
Class: D2 Antagonists Mechanism of Action: Blocks D2 receptors in Chemoreceptor trigger zone and Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV -Migrane induced NV -Gastroenteritis induced NV Primary Adverse Effects: -Extrapyramidal signs -mAChR Antagonist side effects Other Comments: -Bolded Drug: Metoclopramide -Good “general purpose” antiemetics
18
Q
Scopolamine
A
Class: mAChR Antagonist Mechanism of Action: Blocks muscarinic receptor on vestibular afferents and Emetic center/Nucleus of solitary tract Indications: -Post-op induced NV -NV due to motion sickness or vestibular disorders -Vertigo Primary Adverse Effects: mAChR antagonists side effects Other Comments:
19
Q
Diphenhydramine
A
Class: H1 antihistamine (first generation) Mechanism of Action: Blocks H1 receptors on vestibular afferents and Emetic center/Nucleus of solitary tract Indications: -Post-op induced NV -NV due to motion sickness or vestibular disorders -Vertigo -Insomnia Primary Adverse Effects: H1 Antagonist side effects (sedation, drowsiness)mAChR antagonists side effects Other Comments: -Routine use for insomnia is not recommended
20
Q
Dimenhydrinate (NV)
A
Class: H1 antihistamine (first generation) Mechanism of Action: Blocks H1 receptors on vestibular afferents and Emetic center/Nucleus of solitary tract Indications: -Post-op induced NV -NV due to motion sickness or vestibular disorders -Vertigo Primary Adverse Effects: H1 Antagonist side effects (sedation, drowsiness)mAChR antagonists side effects Other Comments: Bolded Drug: Diphenhydramine
21
Q
Meclizine
A
Class: H1 antihistamine (first generation) Mechanism of Action: Blocks H1 receptors on vestibular afferents and Emetic center/Nucleus of solitary tract Indications: -Post-op induced NV -NV due to motion sickness or vestibular disorders -Vertigo Primary Adverse Effects: H1 Antagonist side effects (sedation, drowsiness)mAChR antagonists side effects Other Comments: Bolded Drug: Diphenhydramine
22
Q
Doxylamine
A
Class: H1 antihistamine (first generation) Mechanism of Action: Blocks H1 receptors on vestibular afferents and Emetic center/Nucleus of solitary tract Indications: -Post-op induced NV -NV due to motion sickness or vestibular disorders -pregnancy induced NV -Insomnia Primary Adverse Effects: mAChR antagonists side effects Other Comments: -Bolded Drug: Diphenhydramine -Approved for pregnancy induced NV -Routine use for insomnia is not recommended
23
Q
Aprepitant
A
Class: NK1 Antagonist Mechanism of Action: Blocks NK1 receptors in Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV -Post-op induced NV Primary Adverse Effects: GI side effects (diarrhea, discomfort), fatigue Other Comments:
24
Q
Netupitant
A
Class: NK1 Antagonist Mechanism of Action: Blocks NK1 receptors in Emetic center/Nucleus of solitary tract Indications: -Chemo-induced NV Primary Adverse Effects: GI side effects (constipation) Headache, weakness, fatigue Other Comments: -Only available as combination with Palonesetron (5-HT3 antagonist)
25
Dexamethasone
Class: Glucocorticoids Mechanism of Action: Inhibits PLA2 --> -Decreased synthesis of eicosanoids -Decreased synthesis of cytokines -Decreased movement of leukocytes to areas of injury Anti-Inflamatory Effect -->Improved function of damaged BBB -Unsure of NV mechanism of action. Indications: -Chemo induced NV -Post-op induced NV -Vasogenic cerebral edema Primary Adverse Effects: Short periods of use: insomnia, behavior changes, peptic ulcers. Long periods of use: Metabolic side effects (redistribution of fat, acne, weight gain), Cushings Syndrome. Other Comments: -Used together with 5-HT3 antagonist and NK1 antagonist for Nausea/Vomiting
26
Dronabinol
Class: Cannabinoids Mechanism of Action: Stimulate CB1 receptors in Emetic center/Nucleus of solitary tract Indications: Chemo-induced NV Primary Adverse Effects: CNS side effects (vertigo, euphoria, anxiety, increase appetite) Other Comments:
27
Nabilone
Class: Cannabinoids Mechanism of Action: Stimulate CB1 receptors in Emetic center/Nucleus of solitary tract Indications: Chemo-induced NV Primary Adverse Effects: CNS side effects (vertigo, euphoria, anxiety, increase appetite) Other Comments:
28
Lorazepam
Class: BZDs Mechanism of Action: Bind to allosteric site on GABAA receptor -> GABA mediated IPSP -Mechanism as vestibular suppressant poorly understood Indications: -Chemo and post op induced NV -Vertigo -Seizure -Insomnia Primary Adverse Effects: Sedation, Motor impairment, Amnesia, dependence Other Comments: Bolded Drug: Benzodiazepines -Very effective against status epilepticus (seizure lasting longer than 5 min and/or repetitive seizures in which person does not go back to normal inbetween)
29
Alprazolam
Class: Benzodiazepines Mechanism of Action: Bind to allosteric site on GABAA receptor -> GABA mediated IPSP -Mechanism as vestibular suppressant poorly understood Indications: -Chemo and post op induced NV -Vertigo -Essential Tremor -Anxiety (GAD, panic disorder) -Insomnia Primary Adverse Effects: Sedation, Motor impairment, Amnesia, dependence Other Comments: Bolded Drug: Benzodiazepines
30
Pyridoxine (Vitamin B6)
Class: Alternative therapies for NV Mechanism of Action: ?? Indications: Any form of NV Primary Adverse Effects: Other Comments: -Good for pregnancy induced NV
31
Ginger
Class: Alternative therapies for NV Mechanism of Action: ?? Indications: Any form of NV Primary Adverse Effects: Other Comments: -Good for Pregnancy-induced NV
32
Disulfiram
Class: Aldehyde dehydrogenase inhibitor Mechanism of Action: Inhibits Alcohol dehydrogenase -> more acetaldehyde in blood -> Nausea/vomiting, headache, weakness Indications: Management of Ethanol use disorder Primary Adverse Effects: Acetaldehyde syndrome -> Nausea/vomiting, headache, weakness Other Comments: Bolded Drugs: Naltrexone, Acamprosate-Gives negative experience for drinking alcohol
33
Acamprosate
Class: GABA analog (not effective in receptor) Mechanism of Action: GABA analog (not effective in receptor) Indications: Management of ethanol use disorder Primary Adverse Effects: Diarrhea, nervousness, fatigue Other Comments:
34
Nicotine
Class: nAChR agonist Mechanism of Action: Suppression of withdrawal and cravings in pts with nicotine use Indications: Management of smoking cessation Primary Adverse Effects: Headache, appetite stimulation Other Comments: -Available as patches, lozenges, gum, inhaler
35
Varenicline
Class: nAChR partial agonist Mechanism of Action: Suppression of withdrawal and cravings in pts with nicotine use Indications: Management of smoking cessation Primary Adverse Effects: Headache, Nausea, Insomnia, agitation, depression Other Comments:
36
Bupropion
Class: NDRI (NE and DA reuptake inhibitor) Mechanism of Action: Inhibition of NET and DAT. Inhibiting DA reuptake heps with cravings in pts with nicotine use disorder. Inhibition of NE reuptake may relieve withdrawal symptoms Indications: -Management of smoking cessation -Depression -ADHD Primary Adverse Effects: Insomnia, Headache, Aitiation, Xerostomia Other Comments: -No sexual dysfunction-Risk of seizures -Not as efficacious as stimulants
37
Fluoxetine
Class: SSRI Mechanism of Action: Inhibits SERT Indications: -Anxiety (PTSD, OCD, social anxiety disorder, panic disorder) -Depression Primary Adverse Effects: GI side effects Sexual dysfunction Motor restlessness Other Comments: -Few side effects and good therapeutic window
38
Sertaline
Class: SSRI Mechanism of Action: Inhibits SERT Indications: Anxiety (PTSD, OCD, social anxiety disorder, panic disorder) Primary Adverse Effects: GI side effects Sexual dysfunction Motor restlessness Other Comments: Bolded Drug: Fluoxetine
39
Paroxetine
Class: SSRI Mechanism of Action: Inhibits SERT Indications: -Depression-Anxiety (PTSD, OCD, social anxiety disorder, panic disorder) Primary Adverse Effects: GI side effects Sexual dysfunction Motor restlessness Other Comments: Bolded Drug: Fluoxetine -Few side effects and good therapeutic window
40
Citalopram
Class: SSRI Mechanism of Action: Inhibits SERT Indications: -Depression-Anxiety (PTSD, OCD, social anxiety disorder, panic disorder) Primary Adverse Effects: GI side effects Sexual dysfunction Motor restlessness Other Comments: Bolded Drug: Fluoxetine
41
Benzodiazepines
Class: BZD Mechanism of Action: Bind to Allosteric site on GABAA receptors --> Increases GABA-mediated IPSPs -Mechanism as vestibular suppressant poorly understood Indications: -Anxiety (GAD, panic disorder) -Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, ect. -Essential Tremor -Chemo and post op induced NV -Vetigo -Seizures -IV Anesthetics - Preanesthetic sedation, Induction of general anesthesia, Conscious sedation -Insomnia Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: -Very effective against status epilepticus (seizure lasting longer than 5 min and/or repetitive seizures in which person does not go back to normal inbetween) -Slower sedation onset compared to Barbiturates (Thiopental) -Effects can be reversed with Flumazenil
42
Midazolam
Class: BZD Mechanism of Action: Bind to Allosteric site on GABAA receptors --> Increases GABA-mediated IPSPs Indications: -Anxiety (GAD, panic disorder) -IV Anesthetics - Preanesthetic sedation, Induction of general anesthesia, Conscious sedation Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: Bolded drug: Benzodiazepines -Slower sedation onset compared to Barbiturates (Thiopental) -Effects can be reversed with Flumazenil
43
Buspirone
Class: Partial agonist at 5-HT1A Mechanism of Action: Partial agonist at 5-HT1A Indications: Anxiety (GAD) Primary Adverse Effects: Dizziness, Non-specific chest pain Other Comments:
44
Imipramine
Class: TCAs (Tricyclic Antidepressants) Mechanism of Action: Inhibit NET and SERT Indications: Anxiety (Social anxiety disorder, panic disorder) Primary Adverse Effects: mAChR antagonist side effects.(zerostomia, urinary retention, confusion) alpha 2 antagonist side effects (orthostatic hypotension) H1 antagonist side effects (sedation, dizziness) Other Comments: -Bolded Drug: Amitriptyline Low therapeutic index. Overdose -> diagnostic triade (coma, seizures, ECG abnormalities)
45
Dextromethorphan + Quinidine
Class: Mechanism of Action: Dextromethorphan blocks NMDA receptors Quinidine blocks CYP2D6 --> Increases bioavailability of Dextromethorphan Indications: Pseudobulbar affect due to ALS (Spontaneous, exagerated expression of affect that may be incongruous with mood) Primary Adverse Effects: Nausea, headache, diarrhea, fatigue, dizziness Other Comments: Dextromethorphan has serotonergic effects and should be used cautiously or not at all with SSRIs
46
Sertraline
Class: SSRIs Mechanism of Action: Inhibit SERT Indications: -Depression Primary Adverse Effects: GI side effects Sexual Dysfunction Motor restlessness, Insomnia Other Comments: -Bolded Drug: Fluoxetine-Few side effects and good therapeutic window
47
Escitalopram
Class: SSRI Mechanism of Action: Inhibit SERT Indications: Depression Primary Adverse Effects: GI side effects Sexual dysfunction Motor restlesness, insomnia Other Comments: -Bolded Drug: Fluoxetine-Few side effects and good therapeutic window
48
Vortioxetine
Class: SSRI Mechanism of Action: Inhibit SERT, affects 5-HT receptors too Indications: Depression Primary Adverse Effects: GI side effect Other Comments: -Bolded Drug: Fluoxetine-Less likely to Cause sexual dysfunction
49
Desvenlafaxine
Class: SNRIs Mechanism of Action: Inhibit SERT and NET Indications: Depression Primary Adverse Effects: GI side effects Sexual dysfunction Sedation Other Comments: Bolded drug: Duloxetine
50
Levomilnacipran
Class: SNRIs Mechanism of Action: Inhibit SERT and NET Indications: Depression Primary Adverse Effects: GI side effects Sexual dysfunction Sedation Other Comments: Bolded drug: Duloxetine
51
Vilazodone
Class: Dual-Action antidepressant Mechanism of Action: Inhibit SERT and partial 5-HT1A agonist Indications: Depression Primary Adverse Effects: GI side effects Other Comments: Must take with food
52
Trazodone
Class: Heterocyclic antidepressant Mechanism of Action: Blocks 5-HT2A and weakly inhibits SERT Indications: -Depression -Insomnia Primary Adverse Effects: -H1 antagonist side effects (Sedation) -Priapism (persistant abnormal erection) Other Comments:
53
Nefazodone
Class: Heterocyclic antidepressants Mechanism of Action: Blocks 5-HT2A and weakly inhibits SERT Indications: Depression Primary Adverse Effects: H1 antagonist side effects (Sedation) Hepatic failure Other Comments:
54
Mirtazapine
Class: Heterocyclic antidepressants Mechanism of Action: Blocks presynaptic alpha2, and regular 5-HT2A and 5-HT3 receptors Indications: Depression Primary Adverse Effects: H1 antagonist side effects (sedation) Other Comments:
55
Desipramine
Class: TCAs Mechanism of Action: Inhibit NET and SERT Indications: Depression Primary Adverse Effects: anticholinergic side effects (xerostomia, urinary retention, confusion) Other Comments: -Bolded Drug: Amitriptyline -Overdose -> DIagnostic triad (Coma, seizures, ECG abnormalities)
56
Nortriptyline
Class: TCAs Mechanism of Action: Inhibit NET and SERT Indications: Depression Primary Adverse Effects: anticholinergic side effects (xerostomia, urinary retention, confusion) Other Comments: -Bolded Drug: Amitriptyline -Overdose -> DIagnostic triad (Coma, seizures, ECG abnormalities)
57
Phenelzine
Class: MAO-B inhibitors Mechanism of Action: Inhibit MAO-B in brain --> Increase t1/2 of dopamine, NE and 5-HT in brain Indications: -Depression Primary Adverse Effects: Nausea, Headache, sexual dysfunction Other Comments: Bolded Drug: Selegiline
58
Tranylcypromine
Class: MAO-B inhibitors Mechanism of Action: Inhibit MAO-B in brain --> Increase t1/2 of dopamine, NE and 5-HT in brain Indications: -Depression Primary Adverse Effects: Nausea, Headache, sexual dysfunction Other Comments: Bolded Drug: Selegiline
59
Lithium
Class: Mood Stabilizers Mechanism of Action: Inhibits multiple enzmes involved in generation of second messengers. Indications: Bipolar Disorder Primary Adverse Effects: Tremor, Weight gain, Diabetes Insipidus, GI side effects Other Comments: -Good for acute mania
60
Divalproex
Class: Antiepileptics Mechanism of Action: Prolonged inactivated state of Na+ channels and blocks T-type Ca2+ channels Indications: -Bipolar Disorder -Seizure Primary Adverse Effects: Weight gain, tremor, Teratogenic effects Other Comments: -Effective against a variety of seizure types, but a lot of adverse effects
61
Valproic acid
Class: Antiepileptics Mechanism of Action: Prolonged inactivated state of Na+ channels and blocks T-type Ca2+ channels Indications: -Bipolar Disorder -Seizures Primary Adverse Effects: Weight gain, tremor, Teratogenic effects Other Comments: Bolded Drug: Divalproex -Effective against a variety of seizure types, but a lot of adverse effects
62
Lamotrigine
Class: Antiepileptics (2nd generation) Mechanism of Action: Prolonged inactivated state of Na+ channels Blocks T-type Ca2+ channels Inhibits Glutamatergic transmission Indications: -Bipolar Disorder -Seizures Primary Adverse Effects: Rash, ataxia, headache, diplopia Other Comments: -Very effective against primary generalized tonic-clonic seizures -Second line drug for absence seizures
63
Quetiapine
Class: Second-gen. Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Bipolar disorder -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments:
64
Clozapine
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Bipolar Disorder -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism -Agranulocytosis (lowered WBC count) Other Comments: Bolded Drug: Quetiapine (Bipolar, Schizophrenia), Aripiprazole (Schizophrenia)
65
Lurasidone
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Bipolar Disorder -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Quetiapine (Bipolar, Schizophrenia), Aripiprazole (Schizophrenia)
66
Fosphenytoin
Class: Antiepileptic (First generation) Mechanism of Action: Prolongs inacivated state of Na+ channels Indications: Seizures Primary Adverse Effects: -Acne -Facial coarsing -Teratogenic effects Other Comments: Bolded Drug: Phenytoin
67
Ethosuximide
Class: Blocks T-type Ca2+ Channels Mechanism of Action: Blocks T-type Ca2+ Channels Indications: Seizures Primary Adverse Effects: Sleep Disturbances, Rash Other Comments: -Effective only against absence seizures
68
Phenobarbital
Class: Barbituate Mechanism of Action: Binds to allosteric site on GABAA --> Increase GABA mediated IPSPs Indications: Seizures Primary Adverse Effects: Psychomotor impairment Tolerance and dependence Abuse potential Sedation Other Comments: -Good but not first line because of sedation
69
Oxcarbazepine
Class: 2nd gen Antiepileptic Mechanism of Action: Prolonged inactivated state of voltage-gated Na+ channels Indications: Seizures Primary Adverse Effects: Hyponatremia (worse than CBZ) Rash (Less than CBZ) Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam -Similar to CBZ with fewer drug interactions and side effects
70
Eslicarbazepine
Class: 2nd gen. Antiepileptic Mechanism of Action: Prolonged inactivated state of voltage-gated Na+ channels Indications: Seizures Primary Adverse Effects: Hyponatremia Rash Other Comments: Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, LevetiracetamIsomer of Oxcarbazepine
71
Zonisamide
Class: 2nd gen. antiepileptic Mechanism of Action: Prolonged inactivated state of voltage-gated Na+ channels, Blocks T-Type Ca2+ channels Indications: Seizures Primary Adverse Effects: Rash Kidney stones Weight loss Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam -Effective against variety of seizures
72
Felbamate
Class: 2nd gen. Antiepileptic Mechanism of Action: Prolonged inactivated state of voltage-gated Na+ channels Blocks NMDA receptor (Glutamate transmission) Indications: Seizures Primary Adverse Effects: Weight loss Insomnia Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam -3rd line drug b/c of possible rare side effects
73
Lacosamide
Class: 2nd gen. Antiepileptic Mechanism of Action: Prolonged inactivated state of voltage-gated Na+ channels Indications: Seizures Primary Adverse Effects: Headache Diplopia Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam
74
Tiagabine
Class: 2nd gen. Antiepileptic Mechanism of Action: Inhibits GABA uptake Indications: Seizures Primary Adverse Effects: Behavioral Disturbances Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam
75
Levetiracetam
Class: Antiepileptic (2nd gen) Mechanism of Action: Modifies exocytosis of glutamate and GABA Indications: Seizures Primary Adverse Effects: Psychosis Hallucinations Irritability Other Comments: -Used for all seizures -Second line for abscence seizures
76
Ezogabine
Class: Antiepileptic (2nd gen) Mechanism of Action: Opens voltage-gated K+ channels --> Stabilizes resting membrane potential --> less brain excitability -May enhance GABAergic transmission Indications: Seizures Primary Adverse Effects: Dizziness, fatigue, weakness, confusion, urinary retention Discoloration of skin, nails, sclera Vision loss, retinal abnormalities Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam Metabolized in liver but NOT by CYPs
77
Perampanal
Class: 2nd gen. Antiepileptic Mechanism of Action: Blocks AMPA receptor (Glutamate transmission) Indications: Seizures Primary Adverse Effects: Hostility, aggression Dizziness, vertigo, irritability, ataxia GI side effects, weight gain Other Comments: -Bolded Drugs: Lamotrigine, Topiramate, Gabapentin, Levetiracetam
78
Thiopental
Class: IV Anesthetic - Barbituate Mechanism of Action: Binds to allosteric site on GABAA --> Increases GABA-mediated IPSPs Indications: General Anesthesia Primary Adverse Effects: Respiratory and CV depression Hyperalgesic effects Other Comments: Rapid onset
79
Propofol
Class: IV Anesthetics - GABAA targeted anesthetics Mechanism of Action: Binds to unknown site on GABAA receptor --> Increases GABA mediated IPSPs Indications: General Anesthessa Induction of general anesthesia Primary Adverse Effects: Respiratory and CV depression (less than Thiopental) Other Comments: Rapid onset and offset Antiemetic properties
80
Etomidate
Class: IV Anesthetics - GABAA targeted anesthetics Mechanism of Action: Binds to unknown site on GABAA receptor --> Increases GABA mediated IPSPs Indications: General Anesthessa Induction of general anesthesia Primary Adverse Effects: Post-op nausea/vomiting Less synthesis of adrenal corticosteroids Other Comments: Rapid onset and offset
81
Flumazenil
Class: IV Anesthetics - BDZ antagonist Mechanism of Action: Antagonist at allosteric site on GABAA receptor Indications: Reversal of BDZ-induced sedation following surgery Primary Adverse Effects: Other Comments:
82
Sufentanil
Class: IV Anesthetics - Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: -General Anesthesia, Induction of general anesthesia Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: Bolded Drug: Fentanyl -Opioids --> Miosis (constricted pupils) -Excellent analgesia -Rapid anesthesia onset and offset
83
Remifentanil
Class: IV Anesthetics - Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: -General Anesthesia, Induction of general anesthesia Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: Bolded Drug: Fentanyl -Opioids --> Miosis (constricted pupils) -Excellent analgesia -Rapid anesthesia onset and offset
84
Ketamine
Class: IV Anesthetics - Dissociative anesthetics Mechanism of Action: NMDAR antagonist (Glutamate transmission) Indications: -General Anesthesia, Induction of general anesthesia Primary Adverse Effects: Dysphoria (Bad dreams, hallucinations) Nausea/Vomiting Increased Intracranial pressure Other Comments: Rapid onset Excellent Amnesia and Analgesia
85
Halothane
Class: Volatile anesthetic - Halogenated Hydrocarbons Mechanism of Action: Bind to unknown site on GABAA receptor --> More GABA mediated IPSPs. Also may have effects on glycine receptors, nAChRs, and/or K+ channels Indications: General Anesthesia Primary Adverse Effects: Respiratory and CV depression Sensitizes myocardium to EPI/NE --> arrhythmias Other Comments: Bolded Drug: Desflurane -Halothane Hepatitis Poor analgesia
86
Isoflurane
Class: Volatile anesthetic - Halogenated Hydrocarbons Mechanism of Action: Bind to unknown site on GABAA receptor --> More GABA mediated IPSPs. Also may have effects on glycine receptors, nAChRs, and/or K+ channels Indications: General Anesthesia Primary Adverse Effects: -Mild airway irritation -modest CV depression Other Comments: -Bolded Drug: Desflurane -No Hepatitis-More SKM relaxation than Halothane
87
Desflurane
Class: Volatile anesthetic - Halogenated Hydrocarbons Mechanism of Action: Bind to unknown site on GABAA receptor --> More GABA mediated IPSPs. Also may have effects on glycine receptors, nAChRs, and/or K+ channels Indications: General Anesthesia Primary Adverse Effects: Airway irritation Modest CV depression Other Comments: -Most rapid onset and offset of Halogenated hydrocarbons -No Hepatitis -Good SKM relaxation
88
Sevoflurane
Class: Volatile anesthetic - Halogenated Hydrocarbons Mechanism of Action: Bind to unknown site on GABAA receptor --> More GABA mediated IPSPs. Also may have effects on glycine receptors, nAChRs, and/or K+ channels Indications: General Anesthesia Primary Adverse Effects: Modest CV depression Other Comments: Bolded Drug: Desflurane -Similar to Desflurane but less irritating. -No Hepatitis -Nephrotoxic compound
89
Nitrous Oxide (N2O)
Class: Volatile anesthetic - Other general anesthetics Mechanism of Action: May act as NMDAR antagonist (Glutamate transmission) Indications: -General anesthesia in combo with other anesthetics -In low doses, analgesia in obstetrics Primary Adverse Effects: -Can expand air spaces in body (air emboli in blood, or pneumothorax) -Anemia, polyneuropathy Other Comments: -Low potency -Rapid onset and offset -Good analgesia -Minimum CV depression -Drug of abuse
90
Ether
Class: Volatile anesthetic - Other general anesthetics Mechanism of Action: Probably similaar to Halogenated hydrocarbons Indications: General anesthesia Primary Adverse Effects: Airway irritation --> Nausea/Vomiting Other Comments: Very slow onset/offset No CV depression Good analgesia and SKM relaxation
91
D-tubocurarine
Class: Competitive NMJ blocking agent (Natural alkaloid) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Releases histmine from mast cells Also can block NN receptors in peripheral ganglia Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Long duration of action Excreted unchanged by kidney, bile or liver
92
Atracurim
Class: Competitive NMJ blocking agent (Benzylisoquinolines) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Releases histmine from mast cells (less than D-Tubocurarine) Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid))-Intermediate duration of action
93
Cisatracurium
Class: Competitive NMJ blocking agent (Benzylisoquinolines) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Similar to Atracurium, but less likely to release histamine from mast cells
94
Mivacurium
Class: Competitive NMJ blocking agent (Benzylisoquinolines) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Short duration of action (hydrolized by BuChE)
95
Doxacurium
Class: Competitive NMJ blocking agent (Benzylisoquinolines) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Long Duration of Action -Excreted unchanged by kidney, bile or liver
96
Vecuronium
Class: Competitive NMJ blocking agent (Ammoniosteroid) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Other Comments: -Intermediate duration of action
97
Rocuronium
Class: Competitive NMJ blocking agent (Ammoniosteroid) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Rapid onset of action -Intermediat duration of action
98
Pancuronium
Class: Competitive NMJ blocking agent (Ammoniosteroid) Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: -Tachycardia Other Comments: -Bolded Drug: Vecuronium (Competitive NMJ blocking agent (Ammonio steroid)) -Long duration of action
99
Succinylcholine
Class: Depolarizing NMJ blocking agent Mechanism of Action: Block ACh binding site on NM receptor on motor end in SKM --> Prolonged depolarization of end plate --> Depolarization blockade Indications: Relaxation of SKM in anesthesiology Primary Adverse Effects: -Hyperkalemia in pts aking digoxin, K+-sparing drugs or with tissue injuries/burns -Malignant hyperthermia in susceptible patients Other Comments: Rapid onset of action Rapidly hydrolyzed by BuChE (Ultra short duration of action)
100
Temazepam
Class: BZD Mechanism of Action: Bind to Allosteric site on GABAA receptors --> Increases GABA-mediated IPSPs Indications: -Insomnia Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: -Bolded Drug: Benzodiazepines -Risk of tolerance and/or withdrawal
101
Triazolam
Class: BZD Mechanism of Action: Bind to Allosteric site on GABAA receptors --> Increases GABA-mediated IPSPs Indications: -Insomnia Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: -Bolded Drug: Benzodiazepines -Risk of tolerance and/or withdrawal
102
Zolpidem
Class: Non-BDZ hypnotics Mechanism of Action: Bind to allosteric site at or near BDZ GABAA receptor binding site-> GABA mediated IPSP Indications: Insomnia Primary Adverse Effects: Same as BDZ adverse effects but less frequent/severe Other Comments: Approved for long term use
103
Zaleplon
Class: Non-BDZ hypnotics Mechanism of Action: Bind to allosteric site at or near BDZ GABAA receptor binding site-> GABA mediated IPSP Indications: Insomnia Primary Adverse Effects: Same as BDZ adverse effects but less frequent/severe Other Comments: -Bolded Drug: Zolpidem
104
Eszopiclone
Class: Non-BDZ hypnotics Mechanism of Action: Bind to allosteric site at or near BDZ GABAA receptor binding site-> GABA mediated IPSP Indications: Insomnia Primary Adverse Effects: Same as BDZ adverse effects but less frequent/severe Other Comments: -Bitter aftertaste -Approved for long term use
105
Ramelteon
Class: Melatonin receptro agonist Mechanism of Action: Agonist at MT1 and MT2 melatonin receptors Indications: Insomnia Primary Adverse Effects: Other Comments: -Less efficacious than BDZs and non-BDZs -Lacks problematic adverse effects -Approved for long-term use -Only approved sedative-hypnotic that is not a scheduled substance
106
Suvorexant
Class: Orexin receptor antagonists Mechanism of Action: Antagonist at orexin receptors Indications: Insomnia Primary Adverse Effects: Daytime sedation Motor impairment Other Comments:
107
Doxepin
Class: TCA (Tricyclic antidepressant) Mechanism of Action: TCA: Inhibits NET and SERT Indications: Insomnia Primary Adverse Effects: mAChR antagonist side effects: (Xerostomia, urinary retention, confusion alpha 1 antagonist side effects: orthostatic hypotension H1 antagonist side effects: sedation, dizziness Cardiac arrhythmias Other Comments: Low therapeutic index Diagnostic triad: Coma, seizures, ECG abnormalities
108
Modafinil
Class: Stimulant Mechanism of Action: Poorly understood may inhibit DAT and NET Indications: Excessive sleepiness in patients with narcolepsy, shift-work sleep disorder, sleep apnea Primary Adverse Effects: Adverse psychiatric effects (anxiety, delusions, hallucinations) Other Comments:
109
Armodafinil
Class: Stimulant Mechanism of Action: Poorly understood may inhibit DAT and NET Indications: Excessive sleepiness in patients with narcolepsy, shift-work sleep disorder, sleep apnea Primary Adverse Effects: Adverse psychiatric effects (anxiety, delusions, hallucinations) Other Comments: Bolded Drug: Modafinil
110
Amphetamine
Class: Stimulant Mechanism of Action: Indirect sympathomimetic. Inhibits DAT, NET, SERT Indications: -Excessive sleepiness in pts with narcolepsy -ADHD Primary Adverse Effects: Sympathomimetic side effects: Increased BP, cardiac arrhythmias, abuse potential Other Comments: Modafinil has fewer adverse effects
111
Methylphenidate
Class: Stimulants Mechanism of Action: Inhibits DAT and NET Indications: -Excessive sleepiness in patients with narcolepsy -ADHD Primary Adverse Effects: Sympathomimetic side effects: Increased BP, cardiac arrhythmias Other Comments: Modafinil has fewer adverse side effects
112
Sodium Oxybate
Class: GABAB /GHB agonist Mechanism of Action: GABA analog. Agonist at GABAB and GHB receptors Indications: Excessive sleepiness in patients with narcolepsy Primary Adverse Effects: Deep sedation, dizziness, nausea, urinary incontinence Abuse potential Other Comments: -Combinatino with other CNS depressants is contraindicated
113
Atomoxetine
Class: Non-stimulants Mechanism of Action: Inhibits NET Indications: ADHD Primary Adverse Effects: Insomnia Anorexia GI side effects Other Comments: Not as efficacious as stimulants in most patients
114
Chlorpromazine
Class: Antipsychotics (1st gen) Mechanism of Action: Inhibits D2 Receptors Indications: -Schizophrenia Primary Adverse Effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism mAChR antagonist side effects: Xerostomia, urniary retention, constipation, confusion alpha1 antagonist side effects: orthostatic hypotension H1 antagonist side effects: Sedation, dizziness Other Comments: Bolded Drug: Haloperidol
115
Thioridazine
Class: Antipsychotics (1st gen) Mechanism of Action: Inhibits D2 Receptors Indications: -Schizophrenia Primary Adverse Effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism mAChR antagonist side effects: Xerostomia, urniary retention, constipation, confusion alpha1 antagonist side effects: orthostatic hypotension H1 antagonist side effects: Sedation, dizziness Other Comments: Bolded Drug: Haloperidol
116
Fluphenazine
Class: Antipsychotics (1st gen) Mechanism of Action: Inhibits D2 Receptors Indications: -Schizophrenia Primary Adverse Effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism mAChR antagonist side effects: Xerostomia, urniary retention, constipation, confusion alpha1 antagonist side effects: orthostatic hypotension H1 antagonist side effects: Sedation, dizziness Other Comments: Bolded Drug: Haloperidol
117
Aripiprazole
Class: Antipsychotics (2nd gen) Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments:
118
Olazapine
Class: Second-gen. Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: -H1 antagonist side effects: Sedation, dizziness, Weight gain -D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism -Metabolic syndrome Other Comments: Bolded Drugs: Quetiapine, Aripiprazole
119
Ziprasidone
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drugs: Quetiapine, Aripiprazole
120
Palperidone
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Quetiapine, Aripiprazole
121
Iloperidone
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Quetiapine, Aripiprazole
122
Asenapine
Class: Second-gen Antipsychotics Mechanism of Action: Blocks D2 and 5-HT2A receptors Indications: -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Quetiapine, Aripiprazole
123
Donepezil
Class: Anti-AChEs Mechanism of Action: Inhibits AChE -> more ACh in synapse --> Inreased cholinergic transmission in pathways from nucleus basalis to cortex and hippocampus Indications: Alzheimer's Disease Primary Adverse Effects: Cholinergic side effects: Diarrhea, nausea, escessive sweating, increased urinary frequency Other Comments:
124
Galantamine
Class: Anti-AChEs Mechanism of Action: Inhibits AChE -> more ACh in synapse --> Inreased cholinergic transmission in pathways from nucleus basalis to cortex and hippocampus Indications: Alzheimer's Disease Primary Adverse Effects: Cholinergic side effects: Diarrhea, nausea, escessive sweating, increased urinary frequency Other Comments: Bolded Drugs: Donepezil
125
Rivastigmine
Class: Anti-AChEs Mechanism of Action: Inhibits AChE -> more ACh in synapse --> Inreased cholinergic transmission in pathways from nucleus basalis to cortex and hippocampus Indications: Alzheimer's Disease Primary Adverse Effects: Cholinergic side effects: Diarrhea, nausea, escessive sweating, increased urinary frequency Other Comments: Bolded Drugs: Donepezil
126
Memantine
Class: NMDA receptor antagonist Mechanism of Action: Blocks NMDA receptors (Glutamate transmission) Indications: Alzheimer's Disease Primary Adverse Effects: Dizziness Other Comments: -Fewer side effects than Anti-AChEs -Recommended for pts with moderate-to-severe Alzheimer's disease -Often administered in combo with an anti-AChE
127
Mydriatic Drugs
Class: Mydriatic Mechanism of Action: mAChR (M3) antagonist or alpha1 agonist Indications: Dilates pupil to facilitate examination of retina Primary Adverse Effects: Other Comments:
128
Cycloplegic Drugs
Class: Cycloplegic Mechanism of Action: mAChR (M3) antagonist Indications: Paralyzes ciliary muscle to prevent accommodation. Helps assess visual acuity. Primary Adverse Effects: Other Comments:
129
Tropicamide
Class: Mydriatic and Cycloplegic Mechanism of Action: mAChR antagonist on pupillary constrictor muscles and ciliary muscle. Indications: Facilitation of ophthalmoscopy and refraction Primary Adverse Effects: Photosensitivity. Blurred vision. Systemic mAChR antagonist side effects e.g., Xerostomia (dry mouth), confusion Other Comments: Mydriatics can precipitate attacks of acute angle-closure Glaucoma.
130
Cyclopentolate
Class: Mydriatics and Cycloplegics Mechanism of Action: mAChR antagonist Indications: Primary Adverse Effects: Other Comments: Bolded Drug: Tropicamide (mAChR Antagonist) and Phenylephrine (alpha1 agonist)Opthalmological Diagnosis Other Bolded Drugs: Tropicamide
131
Phenylephrine
Class: Mydriatics Mechanism of Action: alpha1 agonist on pupillary dilator muscle Indications: Facilitation of ophthalmoscopy Primary Adverse Effects: Photosensitivity. Systemic alpha1 agonist side effects e.g. Increased BP. Other Comments: Mydriasis can precipitate attacks of acute angle-closure glaucoma
132
Benoxinate
Class: Ophthalmic anesthetics Mechanism of Action: Block voltage-gated Na+ channels in nerve Indications: Local anesthesia for eye Primary Adverse Effects: Stinging and local irritation Other Comments: Generally mixed with fluorescein (stains cornea and highlighs irregularities)
133
Mannitol
Class: Osmotic Diuretics Mechanism of Action: Increases ECFOSM --> moves fluid from ICF --> ECF Indications: Increased intracranial pressure Primary Adverse Effects: Overexpansion of ECF Electrolyte disturbances Other Comments:
134
Lidocaine
Class: Local Anesthetic (Amide) Mechanism of Action: Blocks voltage gated Na+ channels in nerve Indications: -Local Anesthesia -Neuropathic pain Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility Other Comments: -Analgesic effects occur at [Drug] below those required for local anesthesia -All forms of local anesthesia administration -More potent and longer acting than procaine -Amides metabolized in liver
135
Procaine
Class: Local Anesthetics (Esters) Mechanism of Action: Blocks voltage gated Na+ Channels Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hypersensitivity --> More common in Esters (metabolized derivatives can cause allergic reaction) Other Comments: -Bolded Drug: Lidocaine (Amide) -Infiltration, nerve block, and spinal anesthesia (not effective topically) -short duration (t1/2 ~ 30min) -Esters metabolized by plasma cholinesterases and liver esterases -PABA is formed during metabolism of esters -> antagonizes sulfonaminde antibiotics
136
Chloroprocaine
Class: Local Anesthetics (Esters) Mechanism of Action: Blocks voltage gated Na+ Channels Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hypersensitivity --> More common in Esters (metabolized derivatives can cause allergic reaction) Other Comments: -Bolded Drug: Lidocaine (Amide) -Infiltration and nerve block -short duration -Esters metabolized by plasma cholinesterases and liver esterases -PABA is formed during metabolism of esters -> antagonizes sulfonaminde antibiotics
137
Tetracaine
Class: Local Anesthetics (Esters) Mechanism of Action: Blocks voltage-gated Na+ channels in nerve Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hypersensitivity --> More common in Esters (metabolized derivatives can cause allergic reaction) Other Comments: -Bolded Drug: Lidocaine (Amide) -Spinal and Topical -10x more potent than procaine (b/c of hydrophobicity) -Esters metabolized by plasma cholinesterases and liver esterases -PABA is formed during metabolism of esters -> antagonizes sulfonaminde antibiotics
138
Benzocaine
Class: Local Anesthetics (Esters) Mechanism of Action: Blocks voltage gated Na+ Channels Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hypersensitivity --> More common in Esters (metabolized derivatives can cause allergic reaction) -Hematological -->Can cause methemoglobinemia Other Comments: -Bolded Drug: Lidocaine (Amide)-Widely used as topical OTC -Esters metabolized by plasma cholinesterases and liver esterases -PABA is formed during metabolism of esters -> antagonizes sulfonaminde antibiotics
139
Cocaine
Class: Local Anesthetics (Esters) Mechanism of Action: Blocks voltage gated Na+ Channels Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hypersensitivity --> More common in Esters (metabolized derivatives can cause allergic reaction) Other Comments: -Bolded Drug: Lidocaine (Amide) -Blocks NET ---> Sympathomimetic -Produces Hypertension -Esters metabolized by plasma cholinesterases and liver esterases -PABA is formed during metabolism of esters -> antagonizes sulfonaminde antibiotics
140
Bupivacaine
Class: Local Anesthetic (Amide) Mechanism of Action: Blocks voltage gated Na+ channels in nerve Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility Other Comments: -Bolded Drug: Lidocaine (Amide) -All forms of local anesthesia administration -Long duration of action (4-6 hours)-Amides metabolized in liver
141
Ropivacaine
Class: Local Anesthetic (Amide) Mechanism of Action: Blocks voltage gated Na+ channels in nerve Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility Other Comments: -Bolded Drug: Lidocaine (Amide) -All forms of local anesthesia administration -S-isomer of Bupivacaine, has less cardiac side effects -Amides metabolized in liver
142
Prilocaine
Class: Local Anesthetic (Amide) Mechanism of Action: Blocks voltage gated Na+ channels in nerve Indications: Local Anesthesia Primary Adverse Effects: -CNS effects in order of P[Drug] -->Restlessnss, tingling/numbness, tremors, convulsions, CNS depression, Respiratory arrest -Cardio effects (typically higher [drug] than CNS effects) -->Decreased excitability, conduction velocity, contractility -Hematology --> metabolized to o-toluidine --> Methemoglobinemia Other Comments: -Bolded Drug: Lidocaine (Amide) -Amides metabolized in liver
143
Dalfampridine
Class: Voltage gated K+ channel blockers Mechanism of Action: Blocks Kv channels --> prolongs AP --> Improved conduction in demyelinated fibers Indications: Multiple Sclerosis Primary Adverse Effects: Increased risk of seizures, urinary tract infections, insomnia, dizziness, headache, nausea Other Comments:
144
Acetazolamide
Class: Diuretics (Carbonic Acid Anhydrase Inhibitor) Mechanism of Action: CSF production involves secretion of HCO3- into CSF by Choroid plexus. Thus Carbonic Anhydrase Inhibitors lead to reduced CSF prduction Indications: Idiopathic intracranial hypertension Primary Adverse Effects: -Hypokalemia -Metabolic Acidosis Other Comments:
145
Furosemide
Class: Diuretics (Loop Diuretics) Mechanism of Action: Inhibits NKCC2 --> Less production of CSF Indications: Idiopathic intracranial pressure Primary Adverse Effects: -Hypokalemia -Metabolic alkalosis Other Comments: -Bolded Drug: Acetazolamide (Carbonic Anhydrase Inhibitor)
146
Diazepam
Class: BZD Mechanism of Action: Binds to allosteric site on GABAA receptor --> Increases GABA-mediated IPSPs -Mechanism as vestibular suppressant poorly understood Indications: -Spasticity due to cerebral palsy, MS, spinal cord injury, ect. -Anxiety (Gtroke, AD, panic disorder) -Vertigo -Seizures -IV Anesthetics - Preanesthetic sedation, Induction of general anesthesia, Conscious sedation Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: -Bolded Drugs: Benzodiazepines (Allosteric site (GABAA) --> Increases GABA-medated IPSP), Baclofen (GABAB Agonist), Tizanidine (Alpha2 agonist)-Most comony used Benzodiazepine as a spasmolytic -Very effective against status epilepticus (seizure lasting longer than 5 min and/or repetitive seizures in which person does not go back to normal inbetween) -Slower sedation onset compared to Barbiturates (Thiopental) -Effects can be reversed with Flumazenil
147
Baclefen
Class: Spasmolytic agent Mechanism of Action: Agonist at GABAB receptors --> Decreases exocytosis of excitatory NTs (glutamatergic) and increases inhibitory GABAnergic response Indications: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, ect. Primary Adverse Effects: SKM weakness, dizzines, drowsiness, depression, fatigue. Other Comments: -May have analgesic effects by inhibiting release of substance P in spinal cord -Less sedation than the Benzodiazepines -Less weakness than Dantrolene but more than tizanidine
148
Tizanidine
Class: Spasmolytic agent Mechanism of Action: Agonist at alpha2 receptors --> Less exocytosis of excitatory NT (Glutamatergic) in brain and spinal cord. Also may have post synaptic inhibitory effects. Indications: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, ect. Primary Adverse Effects: -SKM weakness (less than Baclofen) -alpha2 systemic side effects (hypotension, drowsiness, xerostomia Other Comments:
149
Dantrolene
Class: Spasmolytic agent Mechanism of Action: Blocks release of Ca2+ from sarcoplasmic reticulum in SKM. (blocks RyR1 and opening of channel) Indications: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, ect. Primary Adverse Effects: -SKM weakness (more than baclofen or tizanidine) -Hepatotoxicity Other Comments: -Bolded Drugs: Benzodiazepines (Allosteric site (GABAA) --> Increases GABA-medated IPSP), Baclofen (GABAB Agonist), Tizanidine (Alpha2 agonist)
150
Cyclobenzaprine
Class: Muscle Relaxants Mechanism of Action: Central effect in brain stem Indications: Acute muscle spasm due to local tissue injury, muscle sprains, etc. Primary Adverse Effects: -Drowsiness. -mAChR antagonist side effects (xerostomia), constipation, fonfusion, drowsiness Other Comments: -Limited efficacy: no more effective than NSAIDs -Risk of abuse
151
Carisoprodol
Class: Muscle Relaxants Mechanism of Action: Central effect in brain stem Indications: Acute muscle spasm due to local tissue injury, muscle sprains, etc. Primary Adverse Effects: -Drowsiness. -mAChR antagonist side effects (xerostomia), constipation, fonfusion, drowsiness Other Comments: -Bolded Drug: Cyclobenzaprine-Limited efficacy: no more effective than NSAIDs -Largest risk of Abuse
152
Chlorzoxasone
Class: Muscle Relaxants Mechanism of Action: Central effect in brain stem Indications: Acute muscle spasm due to local tissue injury, muscle sprains, etc. Primary Adverse Effects: -Drowsiness. -mAChR antagonist side effects (xerostomia), constipation, fonfusion, drowsiness Other Comments: -Bolded Drug: Cyclobenzaprine -Limited efficacy: no more effective than NSAIDs -Risk of abuse
153
Methocarbamol
Class: Muscle Relaxants Mechanism of Action: Central effect in brain stem Indications: Acute muscle spasm due to local tissue injury, muscle sprains, etc. Primary Adverse Effects: -Drowsiness. -mAChR antagonist side effects (xerostomia), constipation, fonfusion, drowsiness Other Comments: -Bolded Drug: Cyclobenzaprine -Limited efficacy: no more effective than NSAIDs -Risk of abuse
154
Orphenadrine
Class: Muscle Relaxants Mechanism of Action: Central effect in brain stem Indications: Acute muscle spasm due to local tissue injury, muscle sprains, etc. Primary Adverse Effects: -Drowsiness. -mAChR antagonist side effects (xerostomia), constipation, fonfusion, drowsiness Other Comments: -Bolded Drug: Cyclobenzaprine -Limited efficacy: no more effective than NSAIDs -Risk of abuse
155
Levodopa
Class: Dopamine Precursor Mechanism of Action: Converted into Dopamine Indications: -Parkinson's Disease -Dystonia Primary Adverse Effects: Nausea/vomiting and dyskinesia Other Comments: -Same as L-Dopa-Administered with Carbidopa (blocks formation of L-Dopa -->Dopamine outside of brain) -Can also be administered with Carbidopa + Entacapone (Inhibits breakdown of L-Dopa by COMT)
156
Carbidopa
Class: Mechanism of Action: Blocks formation of L-Dopa -->Dopamine outside of brain Indications: Always used in conjunction with Levodopa for Parkinson's Disease and/or Dystonia Primary Adverse Effects: Other Comments: -Increases bioavailability of L-Dopa
157
Entacapone
Class: Mechanism of Action: Inhibits breakdown of L-Dopa by COMT outside of the brain Indications: Can be used with Levodopa + Carbidopa for Parkinson's Disease and/or Dystonia Primary Adverse Effects: Other Comments: -Increases bioavailability of L-Dopa
158
Ropinirole
Class: Dopamine Agonists Mechanism of Action: Stimulate DA receptors (mainly D2 in striatum) Indications: Parkinson's Disease Primary Adverse Effects: -Nausea/vomiting and dyskinesia -behavioral effects, daytime sleepiness, disorders of impulse control Other Comments: -Used for PD therapy in early stages or as an adjunct to Levodopa/Carbidopa in later stages. -Less effective than Levodopa in controlling Parkinsonism -Less likely to cause dyskinesia and motor fluctuations than levodopa
159
Pramipexole
Class: Dopamine Agonists Mechanism of Action: Stimulate DA receptors (mainly D2 in striatum) Indications: Parkinson's Disease Primary Adverse Effects: -Nausea/vomiting and dyskinesia -behavioral effects, daytime sleepiness, disorders of impulse control Other Comments: -Bolded Drug: Ropinirole
160
Rotigotine
Class: Dopamine Agonists Mechanism of Action: Stimulate DA receptors (mainly D2 in striatum) Indications: Parkinson's Disease Primary Adverse Effects: -Nausea/vomiting and dyskinesia -behavioral effects, daytime sleepiness, disorders of impulse control Other Comments: -Bolded Drug: Ropinirole
161
Apomorphine
Class: Dopamine Agonists Mechanism of Action: Stimulate DA receptors (mainly D2 in striatum) Indications: Parkinson's Disease Primary Adverse Effects: -Nausea/vomiting and dyskinesia -behavioral effects, daytime sleepiness, disorders of impulse control Other Comments: -Bolded Drug: Ropinirole -Administered SC as rescue medication
162
Trihexyphenidyl
Class: mAChR Antagonist Mechanism of Action: Blocks mAChRs in Striatum Indications: -Parkinson's Disease -Drug induced Extrapyramidal symptomes (EPS) Primary Adverse Effects: mAChR Antagonist systemic side effects: Xerostomia, urinary retention, constipation, confusion, drosiness Other Comments: -Used for treating tremors, but not better than other drugs for that. -Not recommended for elderly patients
163
Benztropine
Class: mAChR Antagonist Mechanism of Action: Blocks mAChRs in Striatum Indications: -Parkinson's Disease -Drug induced Extrapyramidal symptomes (EPS) Primary Adverse Effects: mAChR Antagonist systemic side effects: Xerostomia, urinary retention, constipation, confusion, drosiness Other Comments: -Bolded Drug: Trihexyphenidyl -Used for treating tremors, but not better than other drugs for that. -Not recommended for elderly patients
164
Selegiline
Class: MAO-B inhibitors Mechanism of Action: Inhibit MAO-B in brain --> Increase t1/2 of dopamine, NE and 5-HT in brain Indications: -Parkinson's Disease -Depression Primary Adverse Effects: Nausea, Headache, sexual dysfunction Other Comments: -Rasagiline (not bolded) is more potent for Parkinson's Disease
165
Rasagiline
Class: MAO-B inhibitors Mechanism of Action: Inhibit MAO-B in brain --> Increase t1/2 of dopamine in brain Indications: Parkinson's Disease Primary Adverse Effects: Nausea, Headache Other Comments: -Bolded drug: Selegiline-Rasagiline is more potent than Selegiline
166
Amantadine
Class: NMDAR Antagonist Mechanism of Action: Uncertain. -may lessen glutamatergic transmission in basal ganglia -may increase dopamine release, lower reuptake, or stimulate DA receptors Indications: Parkinson's Disease Primary Adverse Effects: Dizziness, confusion, nausea, dermatologic reactions Other Comments: -Used as monotherapy in early stages of PD, or as an adjunct in later stages
167
Tetrabenazine
Class: VMAT2 Antagonist Mechanism of Action: Inhibits uptake of Dopamine into synaptic vesicles --> depletion of neuronal Dopamine (In Basal Ganglia) Indications: Chorea, Tics Primary Adverse Effects: Depression, Drowsiness/fatigue, Parkinsonian syndrome Other Comments:
168
Haloperidol
Class: Antipsychotics (1st gen) Mechanism of Action: Inhibits D2 Receptors in Basal Ganglia Indications: -Chorea, Tics -Schizophrenia Primary Adverse Effects: D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism mAChR antagonist side effects: Xerostomia, urniary retention, constipation, confusion alpha1 antagonist side effects: orthostatic hypotension H1 antagonist side effects: Sedation, dizziness Other Comments:
169
Risperidone
Class: Antipsychotics (2nd gen) Mechanism of Action: Inhibits D2 Receptors in Basal Ganglia and 5-HT2A Indications: -Chorea, Tics -Bipolar Disorder -Schizophrenia Primary Adverse Effects: H1 antagonist side effects: Sedation, dizziness, Weight gain D2 antagonist side effects: Extrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Haloperidol (Chorea, Tics), Quetiapine (Bipolar, Schizophrenia), Aripiprazole (Schizophrenia) -Second Generation Antipsychotic -Causes fewer EPS than Haloperidol and usually beter tolerated
170
Olanzapine
Class: Antipsychotics Mechanism of Action: Inhibits D2 Receptors in Basal Ganglia and 5-HT2A Indications: -Chorea, Tics -Bipolar Disorder Primary Adverse Effects: Weight gainExtrapyramidal symptomes (EPS) ex. Dystonia, Akathisia (inner restlessness), and Parkinsonism Other Comments: Bolded Drug: Haloperidol (Chorea, Tics), Quetiapine (Bipolar) -Second Generation Antipsychotic
171
Guanfacine
Class: Alpha2 agonist Mechanism of Action: May reduce activity of noradrenergic neurons in Locus Ceruleus Indications: Tics Primary Adverse Effects: Sedation, Xerostomia, Constipation Other Comments: -Bolded Drug: Clonidine-Used mainly in patients with prominent behavioral problems (e.g. impulse control deficits and rage attacks -Contraindicated in patients with Depression
172
Botulinum Toxin
Class: Muscle Relaxant Mechanism of Action: Blocks exocytosis of ACh from cholinergic nerve terminals at NMJ -> Localized muslce paralysis Indications: -Tics Neurogenic bladder due to spinal cord injury or MS Primary Adverse Effects: -Injection site reactions. Weakness of injected muscle and/or adjacent muscles -UTI, urinary retention, hematuria Other Comments: Injected directly into detrusor muscle for Neurogenic bladder
173
Propranolol
Class: Beta Antagonist Mechanism of Action: Blocks beta receptor effects in brain and SKM Indications: Essential Tremor (ET) Primary Adverse Effects: Beta antagonist side effects (decreased HR, AV block, hypotension, imparied peripheral circulation) Other Comments: -Can also be used to decrease Physiological tremor caused by performance anxiety -High lipid solubility --> Penetrates BBB easily -Non-selective (acts on both beta 1 and 2)
174
Primidone
Class: Antiepileptic drugs Mechanism of Action: Metabolized to phenobarbital --> binds to allosteric site on GABAA --> More GABA mediated IPSPs Indications: -Essential Tremors (ET) -Seizures Primary Adverse Effects: Depression, drowsiness/fatigue, nausea Other Comments: -Good but not first line for Seizures b/c of sedation
175
Gabapentin
Class: Antiepileptic Drugs (2nd gen.)/Anticonvulsant Mechanism of Action: Binds to alpha2gamma subunit of voltage-gated Ca2+ channels May decrease glutamate and/or enhance GABA release -mechanism for effectiveness in ET is uncertain -mechanism for analgesic effects in uncertian Indications: -Essential Tremors (ET) -Neuropathic pain -Seizure Primary Adverse Effects: Ataxia sedation in adults Hyperactivity in children headache weight gain Other Comments: -Better efficacy in treatment for neuropathic pain than seizures -Excreted unchanged by the kidney, no hepatic metabolism
176
Clonazepam
Class: BZD Mechanism of Action: Binds to allosteric site on GABAA receptor --> Increases GABA-mediated IPSPs Indications: -Anxiety (GAD, panic disorder) -Essential Tremor -Vertigo -Seizures Primary Adverse Effects: -Sedation -Motor Impairment -Amnesia -Physical dependence Other Comments: Bolded Drug: Benzodiazepines -Very effective against status epilepticus (seizure lasting longer than 5 min and/or repetitive seizures in which person does not go back to normal inbetween)
177
Ibuprofen
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -May cause hypersensitivity reactions
178
Asprin
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -Bolded Drug: Ibuprofen -May cause hypersensitivity reactions
179
Naproxen
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -Bolded Drug: Ibuprofen -May cause hypersensitivity reactions
180
Indomethacin
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -Bolded Drug: Ibuprofen -May cause hypersensitivity reactions
181
Ketorolac
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -Bolded Drug: Ibuprofen -May cause hypersensitivity reactions
182
Diclofenac
Class: NSIADs Mechanism of Action: Inhibit COX --> Less synthesis of PGs Indications: Mild-to-moderate pain, pyrexia (Fever), Inflammation Primary Adverse Effects: -GI Side effects (PGs have protective properties in GI) -Less platelet aggregation -> More bleeding -Less RBF, GFR in pts with Renal problems Other Comments: -Bolded Drug: Ibuprofen -May cause hypersensitivity reactions
183
Acetominophen
Class: "NSAIDs" Mechanism of Action: Small amount of COX inhibition, but not really known Indications: Mild-to-moderate pain, pyrexia (Fever) Primary Adverse Effects: Hepatotoxicity of recommended doses are exceeded Other Comments: -Recommended over other NSAIDs for mild-to-moderate pain and pyrexia b/c of LOW risk of adverse GI, Hematologic, and Renal Effects
184
Morphine
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Opioids --> Miosis (constricted pupils)
185
Fentanyl
Class: IV Anesthetics - Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: -Moderate-to-severe pain -General Anesthesia, Induction of general anesthesia Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Opioids --> Miosis (constricted pupils) -Excellent analgesia -Rapid anesthesia onset and offset
186
Methadone
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: -Moderate-to-severe pain -Management of opioid use disorder (supress withdrawal symptoms) Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Opioids --> Miosis (constricted pupils)
187
Codeine
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: -Converted into Morphine -Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Codeine is frequently administered in combination with NSAIDs-Opioids --> Miosis (constricted pupils)
188
Hydromorphone
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Bolded Drugs: Morphine, Fentanyl, Methadone, Codeine -Opioids --> Miosis (constricted pupils)
189
Hydrocodone
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Bolded Drugs: Morphine, Fentanyl, Methadone, Codeine -Hydrocodone frequently administered with NSAIDs -Opioids --> Miosis (constricted pupils)
190
Meperidine
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Seizures (specific to Meperidine)-Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Bolded Drugs: Morphine, Fentanyl, Methadone, Codeine -Meperidine forms pro-convulsant --> Seizures -Opioids --> Miosis (constricted pupils)
191
Oxycodone
Class: Opioid analgesic (full Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: Moderate-to-severe pain Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Bolded Drugs: Morphine, Fentanyl, Methadone, Codeine -Frequently administered with NSAIDs -Opioids --> Miosis (constricted pupils)
192
Buprenorphine
Class: Opioid analgesic (partial Mu agonist) Mechanism of Action: Stimulates Mu receptor in amygdala, substantia nigra, periaqueductal gray area, rostroventral meulla, and spinal cord. -> Act to inhibit activation of neuron Indications: -Moderate-to-severe pain -Opioid use disorder (suppression of withdrawal symptomes) Primary Adverse Effects: -Sedation -Respiratory depression (less responsiveness to CO2) -Constipation -Nausea/vomiting -Urinary retention -Histamine release -> Allergic symptomes -Neuroendocrine effects -Psychological dependence and abuse Other Comments: -Opioids --> Miosis (constricted pupils)
193
Butorphanol
Class: Opioid analgesic (full Kappa agonist) Mechanism of Action: Stimulates Kappa receptors Indications: Moderate-to-severe pain Primary Adverse Effects: -Drowsiness -Weakness -Sweating -Psychotomimetic side effects Other Comments: -Opioids --> Miosis (constricted pupils)
194
Naloxone
Class: Opioid Antagonists Mechanism of Action: Blocks all Opioid receptors Indications: -Opioid overdose -Managment of Opioid use disorder Primary Adverse Effects: Other Comments: Naltrexone has greater oral efficacy and longer duration of action than Naloxone
195
Naltrexone
Class: Opioid Antagonists Mechanism of Action: Blocks all opioid receptors Indications: Opioid overdose -Management of Opioid and Ethanol use disorder Primary Adverse Effects: Nausea Headache, dizziness Other Comments: -Naltrexone has greater oral efficacy and longer duration of action than Naloxone -Can cause hepatotoxicity -May inhibit reward mechanisms of food intake
196
Tramadol
Class: Miscellaneous Analgesics Mechanism of Action: -Weakly stimulate Mu opioid recpetors. -Weakly inhibit NET and SERT (NE and Seretonin transporters for reuptake) Indications: Moderate pain Primary Adverse Effects: -Dizziness -Nausea/vomiting -Constipation Other Comments: -Lowers Seizure threshold
197
Clonidine
Class: Alpha2 agonist Mechanism of Action: -Stimulates alpha2 receptors in brain/spinal cord -May reduce activity of noradrenergic neurons in Locus Ceruleus Indications: -Post-op pain management -Neuropathic pain -Tics -ADHD Primary Adverse Effects: Alpha2 side effects: Sedation, hypotension, dry mouth Other Comments: -Used mainly in patients with prominent behavioral problems (e.g. impulse control deficits and rage attacks -Contraindicated in patients with Depression -Not as efficacious as simulants for ADHD
198
Dexmedetomidine
Class: alpha2 agonist Mechanism of Action: Stimulate alpha2 in brain/spinal cord Indications: -post-op pain management -Neuropathic pain Primary Adverse Effects: alpha2 side effects: sedation, hypotension, dry mouth Other Comments: Bolded Drug: Clonidine
199
Tapentadol
Class: Miscellaneous analgesics Mechanism of Action: -Weakly stimulates Mu opioid receptors. -Weakly inhibit NET and SERT (NE and Seretonin transporters for reuptake) Indications: Moderate-to-severe apin Primary Adverse Effects: Nausea/Vomiting Other Comments: -Bolded Drug: Tramadol
200
Ziconotide
Class: N-type Ca2+ channel blocker Mechanism of Action: Blocks N-type Ca2+ channels in spinal cord Indications: -Severe pain -Neuropathic pain Primary Adverse Effects: -Severe psychiatric Symptoms -Impaired cognition, hallucinations Other Comments: -Intrathecal administration only
201
Pregabalin
Class: Anticonvulsants/Antiepileptic (2nd gen) Mechanism of Action: Binds to alpha2gamma subunit of voltage-gated Ca2+ channels May decrease glutamate and/or enhance GABA release -Mechanism for analgesic effect is uncertain Indications: -Neuropathic pain -Seizures Primary Adverse Effects: -Ataxia -Sedation -Weight gain Other Comments: Bolded Drug: Gabapentin (Neuropathic pain, Seizures), Lamotrigine (Seizures), Topiramate (Seizures), Levetiracetam (Seizures)-Greater efficacy in treatment for neuropathic pain than seizures. -Excreted unchanged by kidney.
202
Topiramate
Class: Anticonvulsant/Antiepileptic (2nd gen) Mechanism of Action: -Prolongs inactivated state of Na+ channels. -Enhances GABAergic transmission -Blocks AMPA receptor (Glutamte transmission) Indications: -Neuropathic pain -Essential Tremors (ET) -Seizures Primary Adverse Effects: -Cognition problems -Weight loss -Metabolic acidosis (CAI activity) -Teratogenic effects Other Comments:
203
Carbamazepine
Class: Anticonvulsants/Antiepileptic (first generation) Mechanism of Action: Prolongs inacivated state of Na+ channels Indications: -Neuropathic pain -Bipolar Disorder -Seizures Primary Adverse Effects: -Blurred vision -Hyponatremia -Teratogenic effects Other Comments: -Particularly useful for Trigeminal neuralgia
204
Phenytoin
Class: Anticonvulsant/Antiepileptic (first generation) Mechanism of Action: Prolongs inacivated state of Na+ channels Indications: -Neuropathic pain -Seizures Primary Adverse Effects: -Acne -Facial coarsing -Teratogenic effects Other Comments: -No longer first line AED
205
Amitriptyline
Class: TCAs (Tricyclic Antidepressants) Mechanism of Action: -Inhibit NET and SERT (NE and Seretonin transporters for reuptake) -Mechanism for analgesic uncertain Indications: -Neuropathic pain -Depression -Anxiety (Social anxiety disorder, panic disorder) Primary Adverse Effects: -mAChR antagonist side effects: Xerostomia, urinary retention, sedation... -alpha1 antagonist side effects: postural hypotension -H1 antagonist side effects: Sedation, dizziness... -Cardiac arrhythmias Other Comments: -Low therapeutic index. -Overdose -> Diagnostic triad (Coma, Seizures, ECG abnormalities)
206
Duloxetine
Class: Antidepressants (SNRIs (Seretonin and NE reuptake inhibitors)) Mechanism of Action: -Inhibit SERT and NET -Mechanism for analgesic effects is uncertain Indications: -Neuropathic pain -Anxiety (GAD) -Depression Primary Adverse Effects: -GI disturbances -Sedation -Sexual dysfunction Other Comments:
