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Flashcards in Drugs Deck (163):
1

Levodopa

Dopaminergic Agent
Class: Dopamine (DA) precursor
MOA: Crosses BBB and is converted to dopamine--> improves nigrostriatal functioning
Given with carbidopa (as Sinemet);
Use: firstline treatment for Parkinson's unless patient is young (want to delay as long as possible)
SE: Dyskinesias; hypotension, nausea, anxiety, fatigue

Psychoses of dosed too high
MAO-A inhibitors are contraindicated
(except MAO-B, which only hits DA)

2

Carbidopa

Dopaminergic Agent
Class: Aromatic amino acid decarboxylase inhibitor
MOA: Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
Use: Parkinson's (given with Levadopa to
lower side effects)
SE: Dyskinesias, on-off phenomenon, ---

MAO-A inhibitors are contraindicated
(except MAO-B, which only hits DA)

3

Buproprion

Dopaminergic Agent
Class: Norepinephrinedopamine reuptake inhibitor (NDRI)
MOA: Blocks dopamine transporter (DAT) ->
increased dopamine in synapse
Use: Parkinson's (and depression, smoking cessation, weight loss)
SE: Insomnia, anxiety, agitation, nausea, dry mouth, sweating, palpitations, Mild increase in BP

4

dextroamphetamine
lisdexamfetamine

Dopaminergic Agent
Class: Stimulant
MOA: Blocks dopamine transporter (DAT); also increases VMAT2
Use: ADHD
Norepi and dopamine side effects; weight loss; addictive Psychosis at high doses

5

Modafinil; Armodafinil

Dopaminergic Agent
Stimulant
Increases histamine activity in the tuberomammilary nucleus; may block DAT
Fatigue due to narcolepsy, apnea, shiftwork disorder
SEs are Similar to, but less severe, than amphetamines, Addiction possible

6

Selegiline

Dopaminergic Agent
MAO-B inhibitor
Prevents breakdown of DA
Early Parkinson's; depression
Hypotension, dizziness, insomnia, weight gain Nausea, vomiting
For depression it comes in a patch called EMSAM

7

Rasagiline

Dopaminergic Agent
MAO-B inhibitor
Prevents breakdown of DA
Early Parkinson's
Hypotension, dizziness, insomnia, weight gain Nausea, vomiting

8

Tranylcypromine
Isocarboxazid
Phenelzine

Dopaminergic Agent
MAOI
Irreversibly inhibit both MAO-A and MAO-B
Depression
Hypotension, dizziness, insomnia, weight gain

Hypertensive crisis (with tyramine-rich foods); serotonin
syndrome (MAOI + SSRI)

9

Entacapone

Dopaminergic Agent
COMT inhibitor
Prevents breakdown of DA
Parkinson's
Nausea, fatigue DA side effects
Short-acting (2 hours)

10

Tolcapone

Dopaminergic Agent
COMT inhibitor
Prevents breakdown of DA
Parkinson's
Nausea, fatigue; liver failure, DA side effects
Use only if entacapone fails.

11

Bromocriptine

Dopaminergic Agent
Ergot D2 receptor
agonist Increases DA activity
Mild Parkinson's; Restless Leg Syndrome
hyperprolactinemia Mania, nausea, dizziness, fatigue Peripheral DA-like effects

Must be titrated slowly due to hypotension

12

Pramipexole ;
Ropinerole

Dopaminergic Agent
Selective D2 receptor agonist
Increases DA activity
Mild Parkinson's; Restless Leg Syndrome
Syndrome Mania, nausea, dizziness, fatigue Peripheral DA-like effects

Less effective with motor symptoms of PD

13

Apomorphine

Dopaminergic Agent
D2 receptor agonist
Increases DA activity
Mild Parkinson's; Restless Legs Syndrome
Mania, nausea, dizziness, fatigue Peripheral DA effects
Injectable only; serotonin receptor antagonists contraindicated (e.g., ondansetron)

14

Aripiprazole

Dopaminergic Agent
D2 & D3 receptor (partial) agonist I
ncreases DA activity
Schizophrenia; depression
Less side effects than other DA agonists;
akathisia

15

Amantadine

Dopaminergic Agent
Anti-viral
Stimulates D2 receptors, blocks DAT
Mild Parkinson's (2nd-line); influenza
Nausea, dizziness, psychosis, insomnia, seizures ---

Contraindicated in elderly with dementia (anticholinergic effects)

16

Reserpine

Dopaminergic Agent
Synapse depleter
Blocks VMAT (no release of monoamines
into synapses)
Use: Hypertension
SE: Depression

17

Tetrabenazine

Dopaminergic Agent
Synapse depleter
Blocks VMAT (no release of monoamines into synapses)
Huntington's Chorea,
Depression is a SE

18

Benztropine;
Trihexiphenidyl

Dopaminergic Agent
Anticholinergics
Antagonize the ACh muscarinic receptor
Early Parkinson's; reduce EPS parkinsonian side effects
Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)

Contraindicated in demented Parkinson's; abrupt discontinuation exacerbates symptoms

19

Diphenhydramine

Dopaminergic Agent
Antihistamine Anticholinergic properties Reduce EPS Parkinsonian side effects
Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)

20

Chlorpromazine;
Thioridazine

Dopaminergic Agent
First-generation antipsychotics (Low Potency)
Non-selective D2 receptor antagonism
Use: Psychosis (schizophrenia)
SE: EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism)
Tardive dyskinesia with chronic use
Little effect on negative symptoms of Schizophrenia

21

Fluphenazine;
Thiothixine ;
Haloperidol

Dopaminergic Agent
First-generation antipsychotics (High Potency)
Non-selective D2 receptor antagonism
Use: Psychosis (schizophrenia); movement disorder in Huntingtons
SE: EPS; NMS
Tardive dyskineasia with chronic use
Little effect on negative symptoms

22

Clozapine

Dopaminergic Agent
Second-Generation Antipsychotic
D2 (& D1, D4) receptor antagonist; 5HT2a receptor antagonist
Use: Refractory shizophrenia
Side effects similar to other "pines",
but also agranulocytosis (NMDA receptor antagonism?)
**Most metabolic risk of all
antipsychotics**, but little EPS/TD;
must monitor WBC bc of **agranulocytosis**

23

Olanzapine ;
Quetiapine ;
Asenapine

Dopaminergic Agent
Second-Generation Antipsychotics
D2 receptor antagonist, 5HT2a receptor antagonist
Use: Psychosis, mania, agression
SE: Suicide risk in ages

24

Risperidone;
Ziprazidone;
Paliperidone;
Iloperidone;
Lurasidone

Dopaminergic Agent
Class: Second-Generation Antipsychotics
MOA: D2 receptor antagonist; but various other receptor agonism/antagonism
Use: Psychosis, mania, agression
SE: Suicide risk in ages

25

Pilocarpine HCl

Ocular Drug
Class: Direct muscarinic agonist
Use: Pupillary constriction, increased aqueous outflow
Treatment of glaucoma (both open angle and acute closed angle); cataract surgery
SE: Decreased vision when patient has cataracts due to miosis and headache, Bronchospasm, salivation, nausea, vomiting, diarrhea, abdominal pain, tenesmus, lacrimation, sweating

Used less frequently today due to side effects (SLUDGE)

26

Echothiophate

Ocular Drug
Indirect muscarinic agonist
Irreversibly binds cholinesterase
Use: Treatment of glaucoma ---
SE: Bronchospasm, salivation, nausea, vomiting, diarrhea, abdominal pain, tenesmus, lacrimation, sweating

Used less frequently today due to side effects

27

Atropine

Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Use: Improve discomfort during active eye inflammation (ueveitis)
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention

Very long acting so not used unless severe inflammation

28

Scopolamine

Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Improve discomfort during active eye inflammation (ueveitis) (also used to treat motion sickness)
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention

29

Tropicamide

Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Most commonly used cycloplegia for eye exams
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention

30

Edrophonium

Ocular Drug
Nm agonist
Destroys acetylcholinesterase
Use: Diagnose myasthenia gravis

31

Epinephrine

Ocular Drug
Direct adrenergic agonist
Dilation of episcleral vessels --> increased aqueous outflow
SE: Extrasystoles, palpitation, hypertension, myocardial infarction, trembling, paleness, sweating

32

Hydroxyamphetamine

Ocular Drug
Class: Indirect adrenergic agonist
MOA: Release NE
Use: Separates 1st and 2nd from 3rd order neuron dysfunction in Horner's syndrome; positive dilation means 1st or 2nd order, an ominous sign

33

Cocaine

Ocular Drug
Indirect adrenergic agonist
Prevent reuptake of NE
Use initially to confirm diagnosis of Horner's Syndrome

34

Phenylephrine

Ocular Drug
Direct α1-agonist ---
Use: Dilate pupil for eye exam and cataract surgery ---
Extrasystoles, palpitation, hypertension, myocardial infarction, trembling, paleness, sweating

Caution in elderly patients: at 10% can cause cardiac side effects

35

Brimondine tartrate

Direct α2-agonist
Suppresses aqueous humor production
through action of cAMP in non-pigmented
ciliary epithelium Primary agent for treatment of glaucoma --- ---
May cause follicular conjunctivitis;
use with MAOi can cause
fatigue/drowsiness

36

Timolol

Ocular Drug
β-blocker
Reduce intraocular pressure by reducing aqueous production at the ciliary process
Use: Second line treatment of glaucoma ---
Bradycardia, hypotension, syncope, palpitation, congestive heart failure, bronchospasm, mental confusion, depression, fatigue, lightheadedness, hallucinations, memory impairment, sexual dysfunction, hyperkalemia

Contraindicated in CHF, asthma; bradycardia over time may produce tachyphylaxis

37

Levobunolol

Ocular Drug
β-blocker
Reduce intraocular pressure by reducing aqueous production at the ciliary process
Use: Second line treatment of glaucoma ---
Bradycardia, hypotension, syncope, palpitation, congestive heart failure, bronchospasm, mental confusion, depression, fatigue, lightheadedness, hallucinations, memory impairment, sexual dysfunction, hyperkalemia

38

Betaxolol

β1-blocker
Reduce intraocular pressure by reducing
aqueous production at the ciliary process Second line treatment of glaucoma

39

Latanoprast

Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma
Eyelash growth, change in iris
color, intraocular inflammation
May cause cystoid macular edema in
cataract surgery and activate herpes

40

Travoprost

Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma Eyelash growth, change in iris color
May cause cystoid macular edema in
cataract surgery; more effective in
African Americans

41

Bimatoprost

Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma Eyelash growth, change in iris color
May cause cystoid macular edema in
cataract surgery and activate herpes

42

Unoprostone isopryl

Prostaglandin analog Increase uveoscleral outflow Glaucoma Eyelash growth, change in iris color Least effective overall

43

Nifedipine

Ca-channel blocker Increases ocular perfusion at nervehead Low-tension glaucoma Not widely used.

44

Dorzolamide HCl

Carbonic anhydrase
inhibitor
Reduce aqueous production via interfere
with the active transport of Na through Na-
K-ATPase pump Second line glaucoma therapy Red eyes, lid allergies
Contraindicated in sulfonamide
allergies

45

Acetazolamide

Carbonic anhydrase
inhibitor
Reduce aqueous production via interfere
with the active transport of Na through Na-
K-ATPase pump
Oral agent used for advanced glaucoma
and with cataract surgery
Paresthesia, fatigue, drowsiness,
depression, diarrhea, metaboliv
acidosis, electrolyte changes Anaphylaxis, blood dyscrasias
Used only if other topical therapy
fails.

46

Brinzolamide

Carbonic anhydrase
inhibitor
Reduce aqueous production via interfere
with the active transport of Na through Na-
K-ATPase pump Second line glaucoma therapy Red eyes, lid allergies

47

Tranylcypromine;
Phenelzine

Antidepressant
Class: MAOI
MOA: Irreversibly inhibit both MAOa and MAOb
Use: Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism

Hypertensive crisis (with tyraminerich foods); serotonin syndrome (MAOI + SSRI); agitation (rare), delerium --> seizures
Anticholinergic, orthostatic hypotension, sexual dysfunction, weight gain, sedation

48

Desipramine;
Imipramine;
Amitriptyline;
Nortriptyline

Tricyclic Antidepressant
Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Sympathomimetic (cardiac arrhythmias and conduction defects, especially at OD)
Antimuscarinic, orthostatic hypotension, sedation (additive
with alcohol), seizures

Not very safe; rarely used anymore

49

Fluoxetine; Paroxetine

SSRI
Inhibit reuptake of 5-HT (and NE to lesser extent)
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; premenstrual dystrophic disorder
Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly nausea, decreased sexual
function

Fluoxetine and Paroxetine are Potent P450 inhibitors;
Fluoxetine forms active metabolite (norfluoxetine)

50

Paroxetine

SSRI
Inhibit reuptake of 5-HT (and NE to lesser extent)
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly
nausea, decreased sexual
function Potent P450 inhibitor

51

Sertraline

SSRI
Inhibit reuptake of 5-HT (and NE to lesser
extent)
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly
nausea, decreased sexual
functio

52

Escitalopram

SSRI
Inhibit reuptake of 5-HT (and NE to lesser
extent)
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly
nausea, decreased sexual
function

53

Citalopram

SSRI
Inhibit reuptake of 5-HT (and NE to lesser
extent)
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly
nausea, decreased sexual
function

54

Duloxetine

SNRI Inhibits reuptake of 5-HT and NE
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism

55

Venlafaxine

SNRI Inhibits reuptake of 5-HT and NE
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism

56

Bupropion

Atypical Blocks DA and NE reuptake
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism;
maintain nicotine abstinence in quitting
smokers Lowers seizure threshold

57

Mirtazapine

Atypical
5HT2a antagonists; also inhibit 5HT
reuptake
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism

58

Lithium

Unknown; lithium depletes secondary
messengers IP3 and DAG, important in aadrenergic
and muscarinic-cholinergic
transmission
Anti-manic/mood-stabilizing (bipolar);
long-term cluster headache prevention
If elevated levels: neurotoxicity,
cardiac toxicity, renal dysfunction
Drowsiness, weight gain, tremor,
polydipsia, polyuria
Nausea and vomiting early sign of
lithium OD; indomethacin and Nadepleting
diuretics should be avoided
(increase [Li])

59

Nalmefene

Opiod antagonist --- ---
May produce a prolonged
withdrawal state (nausea, vomiting,
piloerection, yawning)

60

N-acetylcysteine

Antioxidant
Supplies sulfhydryl groups to glutathione;
improves microcirculation, provides antiinflammatory
effect Acetaminophen overdose

61

Fomepizole

Blocks alcohol dehydrogenase Methanol & ethylene glycol poisoning --- --- Very expensive

62

Cocaine

CNS stimulant
Blocks reuptake of dopamine,
norepinephrine, and serotonin
Topical anesthetic, combined
vasoconstrictor and local anesthetic
Sympathetic effects; paranoia,
aggression ---
Rapidly hydrolyzed by plasma
cholinesterase; crack is the free base
form

63

LSD

Schedule I
Hallucinogen
Agonist at 5HT2A receptors on Raphe cell
body --> inhibition of Raphe Nuclei firing -->
increased sensory input; partial dopamine
agonist
Schedule I hallucinogen; model
hallucinogen against which all others
compared; limited studies in
psychoanalysis, alcoholism, autistic
children, and terminal cancer patients
Bad trips (anxiety attack, panic
attack), flashbacks, "street drug"
lifestyle; no overdoses, birth
defects, or chronic psychoses
linked to LSD ---
Oxidized in liver; cross tolerance with
mescaline and psilocybin

64

Mescaline

Schedule I
Hallucinogen
Agonist at 5HT2A receptors on Raphe cell
body --> inhibition of Raphe Nuclei firing -->
increased sensory input; partial dopamine
agonist --- ---
Cross tolerance with LSD and
psilocybin

65

Psilocybin

Schedule I
Hallucinogen
Agonist at 5HT2A receptors on Raphe cell
body --> inhibition of Raphe Nuclei firing -->
increased sensory input; partial dopamine
agonist --- --- ---
Cross tolerance with mescaline and
LSD

66

Phencyclidine

Dissociative (PCP)
anesthetic
Antagonist of ion channel associated with
NDMA receptor; agonist at mu opioid
receptors ---
Violent behavior, coma, seizures,
arrest; inexplicable psychoses
Dissociation, confusion, ataxia,
marked nystagmus
Long half-life due to being highly lipid
soluble and having active metabolites

67

Amphetamines

Indirect sympathomimetic (release biologic
amines from nerve terminals in periphery
and in CNS); dopamine most important Narcolepsy, ADHD
Vasospasm leading to possible
stroke or MI, arrhythmia, weight
loss (anorectic effect)
Tremor, anxiety, irritability,
confusion, possibly paranoid
state
Others: dextroamphetamine
(Dexedrine), methamphetamine
(Desoxyn), methylphenidate (Ritalin)

68

Marijuana

Cannabinoid
Hits cannabinoid receptors (CB1, CB2: Gprotein
coupled receptors)
Schedule I hallucinogen; anti-emetic,
anti-nausea, and appetite stimulate for
cancer chemotherapy and AIDS
patients; analgesic for neuropathic pain;
potentially: glaucoma, asthma,
anxiolytic, migraine, and multiple
sclerosis treatment
Vasodilation --> tachycardia,
dilation of conjunctival vessels,
bronchodilation, decreased
intraocular pressure, hunger
May impair reproductive function
in adolescents; heavy use may
impair development of very
young users; possible
respiratory damage due to tar
Active ingredient is delta-9-
tetrahydrocannabinol; metabolized
by P450, with chronic use inducing
enzyme; highly lipid soluble

69

Anandamide

Endogenous
cannabinoid
Hits cannabinoid receptors (CB1, CB2: Gprotein
coupled receptors) Endogenous cannabinoid

70

Dronabinol

Synthetic THC
Hits cannabinoid receptors (CB1, CB2: Gprotein
coupled receptors)
Schedule III drug; anti-emetic, antinausea,
and appetite stimulate for
cancer chemotherapy and AIDS
patients

71

Nabilone

Synthetic THC
Hits cannabinoid receptors (CB1, CB2: Gprotein
coupled receptors)
Schedule II drug; treatment-resistant
nausea and vomiting, weight loss and
anorexia in AIDS patients --- ---
Less psychoactive side effects than
marijuana

72

Morphine

Opioid Mu-opioid receptor agonist
Severe analgesia, mood alteration,
antitussive, sedation
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
2 major active metabolites: M6
(more potent/active), M3 (little
affinity); intraspinal administration
possible

73

Codeine

Opioid
Mu-opioid receptor agonist (low receptor
affinity); demethylated to form morphine
(10% of oral ingestion, via CYP2D6)
Moderate analgesia, antitussive (found
in many cough medicines)
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
10% of Caucasians unable to convert
codeine to morphine (can still
experience side effects, though)

74

Tramadol

Opioid
Mu opioid receptor agonist (weak); some
NE/5HT uptake inhibition (leading to
analgesia); synthetic codeine analog Moderate (not severe) analgesia
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
1 metabolite: demethylated, more
potent analgesic

75

Fentanyl

Opioid
Mu-opioid receptor agonist (strong); highly
lipid-soluble
Severe analgesia after identification of
dose level via other opiod (e.g.,
morphine)
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
IV, transdermal; do not change dose
more than 1/week (long half-life);
intraspinal administration possible

76

Methadone

Opioid Mu-opioid receptor agonist
Chronic, severe pain; treatment of
heroin and opiod addicts
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
90% bound to plasma protein,
accumulates in tissues (thus,
extended duration of action); do not
change dose more than 1/week (long
half-life

77

Oxycodone

Opioid Mu-opioid receptor agonist Moderate to severe analgesia
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence Oxycontin is extended release

78

Meperidine

(Demerol) Opioid Mu-opioid receptor agonist Don't use this
Miosis, constipation, respiratory
depression; mental status changes
and seizures (normeperidine)
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence 1 metabolite: normeperidine

79

Propoxyphene

(Darvon) Opioid Mu-opioid receptor agonist (weak) Don't use this
Miosis, constipation, respiratory
depression; CNS toxicity
(norpropoxyphene)
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence
1 metabolite: norpropoxyphene (has
long half-life)

80

Loperamide

(Imodium) Opioid
Slows peristalsis via opioid receptors in
intestine, and possibly decreased GI
secretion Diarrhea
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence Meperidine congener

81

Diphenoxylate

(Lomotil) Opioid
Slows peristalsis via opioid receptors in
intestine, and possibly decreased GI
secretion Diarrhea
Miosis, constipation, respiratory
depression
Dry mouth, nausea/vomiting,
sedation, sweating; dreams,
dysphoria, delerium, myoclonus,
seizures, pruritis, urticaria,
urinary incontinence Meperidine congener

82

Naloxone

Opioid antagonist
Competitive mu-, delta-, and kappa-opioid
receptor antagonist
Acute opioid toxicity (depressed RR
best predicts reponse)
Can precipitate withdrawal (flu-like
symptoms of nausea, vomiting,
diarrhea; piloerection, yawning,
irritability) ---
Continuous parenteral infusion, as
lasts only 15-30 minutes (oral almost
completely metabolized by liver);
patient has normal mental status

83

Naltrexone

Opioid antagonist Mu-opioid receptor antagonist Alcoholism
May produce a prolonged
withdrawal state (nausea, vomiting,
piloerection, yawning

84

Diazepam

Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 43 hours (active
metabolites up to 100 hours)
Short-term depression treatment;
maintenance of bipolar; severe bipolar;
anticonvulsant; muscle relaxant ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

85

Chlordiazepoxide

(Librium) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 10 hours (active
metabolites up to 100 hours)
Short-term depression treatment;
maintenance of bipolar; severe bipolar ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

86

Lorazepam

(Ativan) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 14 hours
Short-term depression treatment;
maintenance of bipolar; severe bipolar;
sedation; anticonvulsant; prevent
withdrawal symptoms in alcoholics ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA; directly conjugated
into inactive metabolite

87

Flurazepam

(Dalmane) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 74 hours (active
metabolites up to 100 hours)
Short-term depression treatment;
maintenance of bipolar; severe bipolar ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

88

Alprazolam

(Xanax) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 12 hours
Short-term depression treatment;
maintenance of bipolar; severe bipolar;
sedation ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

89

Midazolam

(Versed) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 1.9 hours
Anesthesia (calming effects, production
of anterograde amnesia) ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

90

Triazolam

(Halcion) Benzodiazepine
GABAa agonist; binds between a1 and y2
subunits; half-life of 2.9 hours
Short-term depression treatment;
maintenance of bipolar; severe bipolar;
induce sleep ---
Daytime sedation and
drowsiness, anterograde
amnesia, synergistic depression
of CNS with other drugs,
pyschologic and physiologic
dependence (chronic use)
"Ceiling effect" due to augmenting
action of GABA

91

Zolpidem

(Ambien)
Non-benzodiazepine
receptor agonist BDZ-1 selective agonist
Sedation and hypnosis without muscle
relaxation or anticonvulsant activity
Sleep-walking; next morning
impairment

92

Flumazenil

(Romazicon)
Benzodiazepine
antagonist Competitive non-selective antagonist Benzodiazapine overdose
Withdrawal (may be lifethreatening);
seizures in mixed
overdoses ---
Non uniform in reversal of respiratory
depression

93

Thiopental

(Pentothal) Barbiturate
GABAa agonist (binds a or b subunit); highly
lipid soluble, fast-on, fast-off Induce anesthesia ---
Daytime sedation and
drowsiness, dose-dependent
depression of CNS, pyschologic
and physiologic dependence
(chronic use)
Abrupt withdrawal life-threatening;
redistribute from brain to muscle and
fat, metabolized by liver; dosed
based on lean body mass

94

Phenobarbitol

Barbiturate GABAa agonist (binds a or b subunit) Antiepileptic, anticonvulsant ---
Daytime sedation and
drowsiness, dose-dependent
depression of CNS, pyschologic
and physiologic dependence
(chronic use) Abrupt withdrawal life-threatening

95

Buspirone

No GABAa interaction; may be partial
agonist at 5HT1A Anxiolytic without marked sedation

96

Nitrous Oxide

Inorganic gas NMDA receptor antagonist
Mask induction in children; adjuvant to
volatile anesthetics, opioids
Post-operative nausea and
vomiting; inactivates vitamin B
(leading to abnormal embryonic
development, abortion);
accumulates in closed, aircontaining
spaces (bowel, middle
ear, pneumothoraces, air emboli)
because N2O insoluble in blood --- No muscle relaxation

97

Isoflurane

Volatile anesthetic Most potent
Gold standard for maintenance of
anesthesia
Pungent; dose dependent CNS
depression, increase in cerebral
blood flow and intracranial
pressure; dose dependent
decrease in systemic BP, decrease
in respiratory function; relaxes
skeletal muscle; increase in HR;
malignant hyperthermia

98

Desflurane

Volatile anesthetic
Least soluble, least potent (allows for rapid
emergence from anesthesia) Maintenance of anesthesia
Most pungent (airway irritation
symptoms); dose dependent CNS
depression, increase in cerebral
blood flow and intracranial
pressure; dose dependent
decrease in systemic BP, decrease
in respiratory function; relaxes
skeletal muscle; increase in HR;
malignant hyperthermia

99

Sevoflurane

Volatile anesthetic Less soluble, less potent (but not irritating)
Mask induction in children and adults;
maintenance of anesthesia
Can form CO if not combined with
CO2 correctly; dose dependent
CNS depression, increase in
cerebral blood flow and intracranial
pressure; dose dependent
decrease in systemic BP, decrease
in respiratory function; relaxes
skeletal muscle; malignant
hyperthermia

100

Methohexital

Barbiturates
GABAa receptor agonist, antagonist of
NMDA-glutamate receptor; produce
hypnosis & sedation, but is anti-analgesic Induce general anesthesia --- ---
Redistribute from brain to muscle and
fat, metabolized by liver; dosed
based on lean body mass

101

Propofol

Alkylphenol (a fatty
acid)
GABAa receptor agonist, antagonist of
NMDA-glutamate receptor; some a2
receptor activity; rapid onset and offset
Anti-emetic at low doses; induction and
maintenance of general anesthesia;
sedation in ICU, procedural sedation
Propofol infusion syndrome: being
given for several days leads to
metabolic acidosis,
rhabdomyolysis, heart & renal
failure, lowering of BP, bradycardia,
and death (likely due to fatty acid
oxidation)
Painful injection site; supports
bacterial growth
Administered IV in a lipid emulsion
(cause of pain); be aware of allergies
(egg and soy in emulsion); no
malignant hyperthermia

102

Etomidate

Carboxylated
imidazole GABAa receptor agonist (only D-isomer) Hypnosis; no analgesic activity
Pain on administration (due to
solvent, propylene glycol);
involuntary myoclonic movements
due to subcortical disinhibition (not
a seizure); post-operative nausea
and vomiting; single dose inhibits
cortisol synthesis ---
Minimal cardiorespiratory depression
(good agent in patients with minimal
cardiac reserve)

103

Ketamine

Phencyclidine
NMDA receptor antagonist, kappa opiate
agonist; leads to dose-dependent
unconsciousness, amnesia, analgesia
Sedative/anesthetic for
pediatric/developmentally delayed
patients; induction in patients with
reactive airway disease, hypovolemia
(trauma patients), cardiac disease; with
propofol for IV procedural sedation;
adjuvant during and after surgery to
reduce opiod use; part of multimodal
pain therapy regimen; depression
treatment
Stimulates sympathetic nervous
system outflow; increases cerebral
blood flow, ICP; emergence
delerium; nystagmus, lacrimation,
salivation, and dissociative
anesthesia ---
Racemic mixture (S more potent);
metabolized by P450 (norketamine, a
third to a fifth as effective); great
bronchodilator; contraindicated in
CAD patients and those with with
intracranial lesions

104

Dexmedetomidine

a2 adrenergic
agonist
Binds a2a and a2b in locus coeruleus and
spinal cord (produces sedation,
sympatholysis, and analgesia)
Awake intubations, awake craniotomies;
adjunct to general anesthesia in
patients susceptible to narcotic-induced
post-op respiratory depression;
withdrawal/detoxification
Limited respiratory depression
(wide safety margin) ---
Since GABA not hit, sedation is
easier to wake from and is similar to
non-REM sleep; FDA approved only
for ventilation of ICU patients for
under 24 hours

105

Succinylcholine

Depolarizing NMB
Divalent ACh molecule; attaches to all ACh
receptors, overstimulating them (first seen
as disorganized muscular contractions
(fasiculations), then paralysis) Skeletal muscle relaxant (intubation)
Malignant hyperthermia; cardiac
dysrhythmias, hyperkalemia,
increased intraocular pressure,
increased intracranial pressure
Increased intragastric pressure,
myalgias, masseter spasm
Hydrolyzed by pseudocholinesterase
(in plasma); blockade cannot be
reversed; only NMB with rapid onset
and ultra-short duration of action

106

Pancuronium

Amino steroid nondepolarizing
NMB
Competitive blockade of ACh (no
depolarization); vagolytic
Skeletal muscle relaxant; avoid in
patients with renal insufficiency Increase in HR ---
Only long acting non-depolarizing
agent; supplied as liquid; 80%
excreted unchanged in liver (low
metabolism in liver); reverse with
AChEI

107

Vecuronium

Amino steroid nondepolarizing
NMB
Competitive blockade of ACh (no
depolarization) Skeletal muscle relaxant No cardiovascular effects ---
Intermediate acting; supplied as a
powder (reconstitute); hepatic
metabolism, hepatic and renal
excretion; reverse with AChEI

108

Rocuronium

Amino steroid nondepolarizing
NMB
Competitive blockade of ACh (no
depolarization)
Skeletal muscle relaxant (can substitute
succinylcholine in rapid sequence
intubation) No cardiovascular effects ---
Intermediate acting; supplied as a
liquid; hepatic metabolism, hepatic
and renal excretion; can speed onset
with higher dose; reverse with AChEI

109

Sugammadex

Selective relaxant
binding agent
Complexes with rocuronium, rendering it
inactive; no effect on AChesterase Immediate reversal of rocuronium
Decrease in blood presure, nausea
and vomiting, dry mouth --- Not yet FDA approved

110

Atracurium

Isoquinoline nondepolarizing
NMB
Competitive blockade of ACh (no
depolarization)
Skeletal muscle relaxant; use in patients
with liver or renal dysfunction
Histamine release (especially if
given as rapid IV bolus), with
resultant hypotension and
tachycardia ---
Undergoes spontaneous, nonenzymatic
degradation (Hofman
elimination); intermediate acting;
reverse with AChEI

111

Cis-atracurium

Isoquinoline nondepolarizing
NMB
Competitive blockade of ACh (no
depolarization)
Skeletal muscle relaxant; use in patients
with liver or renal dysfunction
Unlike atracurium, no histamine
release or downstream effects ---
Undergoes spontaneous, nonenzymatic
degradation (Hofman
elimination); intermediate acting;
reverse with AChEI

112

Edrophonium

AChE-I --- Reversal of NMB --- --- Short-acting, fast onset

113

Neostigmine

AChE-I ---
Reversal of NMB (most commonly
used) --- ---
More complete antagonism than
edrophonium

114

Pyridostigmine

AChE-I --- Reversal of NMB --- ---
Longer duration of action than
neostigmine, edrophonium

115

Glycopyrrolate

Anti-muscarinic ---
Reversal of neuromuscular blockade's
muscaranic effects DUMBELLS --- Could also use atropine

116

Cocaine; benzocaine
; procaine
; tetracaine;
chlorprocaine

Ester anesthetic
Binds reversibly to the intracellular portion of
the voltage-gated sodium channel and
inactivates it, and so blocks transmission of
nociceptive nerve impulses. Local anesthesia
Local: transient neurologic
symptoms (basically, really bad
pain), neuronal injury.
Systemic (more common with longacting
local anesthetics): circumoral
numbness, dizziness, tinnitis,
blurred vision, CNS excitation
(restlessness, agitation, seizures),
followed by CNS depression
(respiratory arrest,
unconsciousness); hypotension;
cardic toxicity with higher doses.
Methemoglobinemia (primarily
with benzocaine), allergic
reactions
Used less frequently than amides;
cocaine has many side effects due to
action as a CNS stimulant

117

Lidocaine;
mepivacaine;
bupivacaine;
ropivacaine

Amide anesthetic
Binds reversibly to the intracellular portion of
the voltage-gated sodium channel and
inactivates it, and so blocks transmission of
nociceptive nerve impulses. Local anesthesia
Local: transient neurologic
symptoms (basically, really bad
pain), neuronal injury.
Systemic (more common with longacting
local anesthetics): circumoral
numbness, dizziness, tinnitis,
blurred vision, CNS excitation
(restlessness, agitation, seizures),
followed by CNS depression
(respiratory arrest,
unconsciousness); hypotension;
cardic toxicity with higher doses.
Bupivicaine has highest cardiac
toxicity potential; ropivicaine less
potent than others (so larger
therapeutic index)

118

IFN-beta-1a

IFN-beta-1a
Many, potentially: inhibit T-cell activation,
shift from Th1 to Th2, inhibit lymphocyte
movement into CNS, anti-proliferative effect,
apoptosis of T-cells, anti-viral, IFN-g
antagonism RRMS
Mild anemia, increase LFT (monitor
every 6 mo.), hypothyroid; least
NAB formed
Flu-like, minor irritation at inject
site, anemia
Doesn't cross BBB; decreases
relapse rate by 1/3 and reduces MRI
lesions, with a trend toward
decreasing disability and brain
atrophy

119

Glatiramer acetate

Myelin basic protein
analog
Mixture of 4 AAs in myelin basic protein;
causes T-cell apoptosis (looks like MBP),
induces anti-inflammatory Th2 cells
(cytokine shift from Th1), induces Treg with
induction of anergy RRMS
Mild: injection site reaction, anxiety
attack-like reaction ---
Active in CNS (not peripherally); try
to use early; reduce relapse by 1/3,
modest reduction in MRI lesion and
reduction of atrophy, but no effect on
disease progression

120

Natalizumab

Monoclonal antibody
Binds VLA4 (integrin subunit), inhibiting
leukocyte migration across BBB RRMS (2nd line)
PML (JC virus); acute urticaria,
systemic hypersensitivity infusion
reaction
Headache, dizziness, fatigue,
arthralgia, rigors
Decrease relapse rate by 2/3, greatly
reduce MRI lesions; once/month;
antibodies to natalizumab cause it to
stop working; side effects more
common in patients positive for
neutralizing antibodies

121

Fingolimod

Sphingosine-1-
phosphate analog
Prodrug; sequesters circulating lymphocytes
in secondary lymphoid organs via induction
of intracellular internalization of receptors on
lymphocytes (no effect on lymphocyte
induction, proliferation, or memory function) RRMS
Bradycardia and heartblock (EKG
for first 6 hours); macular edema
(need opthalmology exam before
and after 3 months)
Reduced FEV1, increased LFTs,
lymphopenia, leukopenia,
asthenia, back pain, blurred
vision, headache dizziness,
infections
Patients must be VZV immune before
prescription; oral daily

122

Teriflunomide

Immunosuppressant
Selective dihydro-orotate dehydrogenase
inhibitor; blocks de novo pyramidine
synthesis, reducing T- and B-cell
proliferation and function against
autoantigens; preserves replication and
function of cells living on salvage pathway
(e.g., hematopoietic cells, memory cells) RRMS
Hepatotoxicity; teratogenicity
(animal data) --- Oral daily

123

Dimethyl fumarate

Enhances Nrf2 pathway; some Th1 -> Th2
sgift ---
N & V; diarrhea; stomach pain;
flushing Itching, redness, rash Oral BID

124

Mitoxantrone

Anthracenedione
Broad immune suppression and modulation
of B cells, T cells and macrophages;
decreases frequency of clinical relapse,
reduces disease progress, and reduces
disability SPMS; RRMS (2nd line)
Dose-dependent cardiac toxicity
(decreased LVEF, irreversible
CHF); induction of acute leukemia
Nausea and vomiting, alopecia,
menstrual irregularities,
increased susceptibility to
infection IV; once/3 months

125

Azathioprine;
Methotrexate;
Cyclophosphamide;
Mycophenolate mofetil

Immunosuppressant Immunosuppressive
SPMS (resistant, or as combination with
other therapies)
Systemic toxicity: monitor blood for
changes

126

Methylprednisone

Corticosteroid
(immunosuppressant)
Unclear mechanism (suppress both B and T
cells, may reduce cytokine release)
Acute MS attack, SPMS; shortens acute
attack duration,speeds recovery ---
Short-term: insomnia, mood
changes, fluid retention,
epigastric pain, hypertension;
long-term: osteoporosis,
cushingoid, secondary
malignancies Given IV with oral prednisone taper

127

ACTH

Acute MS attack (if patient allergic to
corticosteroids, poor IV access); or if
Methylprednisone doesn't work

128

Plasmapharesis

Unclear mechanism Acute MS attack not responsive to Methylprednisone

129

Phenytoin

Voltage-gated Na
channel stabilizer
Stabilize inactive conformation of Na
channel
Less effective for absence (particular
pediatric), myoclonic, atonic seizures
Rash, gingival hyperplasia,
hirsutism, lupus-like reaction; can
cause contraceptive failure
Mild myelosuppression,
increased LFT; long-term:
cerebellar degeneration,
peripheral neuropathy,
osteoporosis
IV infusion limited by hypotension;
hepatic enzyme inducer (both autoand
hetero-inducer), highly protein
bound

130

Carbamazepine

Voltage-gated Na
channel stabilizer
Stabilize inactive conformation of Na
channel
More effective for complex partial
seizure than primary generalized;
bipolar disorder; neuropathic pain
Rash (rarely, Stevens-Johnson),
mild myelosuppression, mild
increase in LFTs; can cause
contraceptive failure ---
Hepatic enzyme inducer (both autoand
hetero-inducer); highly protein
bound; must increase dose in 1-2
wks due to autoinduction; side effects
likely due to epoxide metabolite

131

Oxcarbamazepine

Voltage-gated Na
channel stabilizer
Stabilize inactive conformation of Na
channel
More effective for complex partial
seizure than primary generalized;
bipolar disorder; neuropathic pain
Rash (rarely, Stevens-Johnson),
mild myelosuppression, mild
increase in LFTs; can cause
contraceptive failure ---
Designed to bypass carbamazepine
epoxide; less protein-bound, less
autoinduction, fewer interactions,
less toxic, longer half-life than
carbamazepine

132

Lamotrigine

Voltage-gated Na
channel stabilizer
Stabilize inactive conformation of Na
channel
Primary generalized epilepsies,
absence seizures; indicated in children;
bipolar disorder; neuropathic pain
Rash, (rarely, Stevens-Johnson):
slow initial titration important; may
lead to contraceptive failure ---
May exacerbate myoclonic seizures;
competes with valproic acid for
excretion (potential synergy); hepatic
enzyme inducer; not very protein
bound

133

Valproate

Unknown; likely affects Na-gated channels
and GABA system
Broad spectrum: absence, myoclonic,
tonic-clonic, primary generalized, partial
onset, and secondary generalized
seizures (but not absence seizures); IV
for status epilepticus; bipolar treatment,
migraine and long-term cluster
headache prophylaxis
Weight gain, hair turnover,
hyperammonemia (which can be
mitigated with oral carnitine),
teratogenicity, blood dyscrasias Pancreatitus

134

Vigabatrin

GABAergic antiepileptic
GABA transaminase binder (slows down
intracellular breakdown of GABA) Anti-epileptic --- --- Works on GABA-A

135

Tigabine

GABAergic antiepileptic
GABA reuptake inhibitor Anti-epileptic --- --- Works on GABA-A

136

Benzodiazapines

GABAergic antiepileptic
Bind GABA-A
Status epilepticus (refractory);
anesthesia Sedation ---
Long-term usefulness limited by
tolerance

137

Gabapentin

GABA analog Block presynaptic influx of Ca
Adjunct for partial complex epilepsy;
more commonly used for neuropathic
pain Sedation ---
Absorption limited by intestinal AA
transporter (there is a Tm); limited
protein binding; no metabolism or
drug interaction in humans (so few
side effects)

138

Pregabalin

GABA analog Block presynaptic influx of Ca
Adjunct for partial complex epilepsy;
more commonly used for neuropathic
pain

139

Topiramate

Glutamate Receptor Blocker
Partial AMPA, Kainate Ca receptor blocker;
secondary effect at voltage-gated Na
channel, GABA system
Partial onset seizures, secondary
generalized seizures, primary
generalized epilepsy; migraine
prevention, long-term prevention of
cluster headaches
Mild metabolic acidosis, kidney
stones (due to some carbonic
anhydrase activity); modest weight
loss; rare acute glaucoma; sedation Word-finding problems
Carbonic anhydrase activity leads to
mild metabolic acidosis, which leads
to respiratory compensation, which
leads to mild alkalosis, which leads to
calcium ionization, which leads to
tingling; treat with vitamin C (acidify
urine)

140

Felbamate

Glutamate Receptor Blocker
NMDA receptor blocker; secondary effect at
voltage-gated Na and Ca channels, GABA
system
Partial onset seizures with or without
secondary generalization; medically
refractory epilepsy
Uncommon but potentially fatal.
Aplastic anemia, acute hepatic
failure. Requires monitoring.

141

Levetiracetam

Synaptic vesicle
binder
Binds synaptic vesicle protein 2, leading to
less NT release
Partial onset seizures, secondary
generalized seizures; maybe primary
generalized epilepsy
Well tolerated; sedation, mostly;
rarely, irritability, aphasia,
thrombocytopenia

142

Ethosuximide

Voltage-gated Ca
channel blocker
Blocks T-type Ca-channels in thalamocortical
circuits
Absence seizures only (and neuropathic
pain)
Nausea (transient), sedation,
irritability ---
Readily absorbed, minimal first pass
metabolism; not protein bound

143

Aspirin,
acetaminophen,
naproxen,
indomethacin,
piroxicam, diclofenac,
ibuprofen

Analgesic NSAIDs Inhibition of COX-1 and COX-2
Acute treatment of moderate migraines;
acute treatment of tension headaches GI disturbances ---
Excedrin (combination of aspirin,
acetaminophen, and caffeine) is
particularly effective

144

Butalbital

Barbiturate ---
Acute treatment of migraines; use when
more traditional therapies unavailable or
contraindicated Drowsiness, dizziness --- Use limited to 2-3 times per week

145

Codeine, meperidine,
oxycodone,
butorphanol

Opioids ---
Acute treatment of migraines; patients
with infrequent headaches; generally,
for patients who wake up with a
headache
Drowsiness, constipation,
respiratory depression, itching,
miosis, urinary retention, euphoria
Physical dependence w/ chronic
use.
Use less than 2 days per week;
pregnant women may use codeine or
meperidine with caution

146

Prednisone;
dexamethasone

Corticosteroids ---
Acute treatment of migraines; migraine,
prolonged headache syndromes (e.g.,
status migrainosus); rescue treatment of
cluster headache --- --- Avoid chronic use

147

Ergotamine

Ergot alkaloid
Vasoconstriction possibly; may also act as a
5HT agonist in trigeminovascular pathway Acute treatment of migraines
Nausea, dizziness, paresthesia,
chest pain, abdominal cramps ---
Contraindicated in women planning
pregnancy, uncontrolled HTN,
sepsis, renal or hepatic failure,
vascular disease

148

Dihydroergotamine

Ergot alkaloid
Vasoconstriction possible; mainly act as a
5HT agonist in trigeminovascular pathway
Acute treatment of migraines; less likely
to cause rebound headache than
ergotamine; acute treatment of cluster
headaches; short-term prevention of
cluster headaches (along with steroids)
Nausea (less likely than
ergotamine), dizziness,
paresthesia, chest pain, abdominal
cramps ---
Contraindicated in women planning
pregnancy, uncontrolled HTN,
sepsis, renal or hepatic failure,
vascular disease; injectable

149

Sumatriptan

Selective 5HT1b-d agonists; penetration of
CNS, constriction of extracerebral
intracranial vessels, inhibition of
trigeminovascular system
Acute treatment of migraines (premier
option); also effective for
photo/phonophobia, nausea and
vomiting; acute treatment of cluster
headaches
Flushing, tingling, dizziness, chest
discomfort (noncardiac) ---
Contraindicated in vascular disease
(including Prinzmetal), uncontrolled
HTN, complicated migraine;
injectable (suma)

150

Onabotulinum toxin A

Mechanisms unknown (possibly decreased afferent
stimulation of trigeminovascular system, or
downregulation of sensory and
parasympathetic receptors)
Preventive treatment of chronic
migraine headaches ---
Injection site pain, headache,
neck weakness, ptosis
FDA approved specific injection site
protocol followed.

151

Amitriptyline,
protriptyline,
nortriptyline

Tri-cyclic
antidepressants
(TCA) ---
Migraine prevention, tension headache
prevention
Dry mouth, constipation, weight
gain, cardiac toxicity, orthostatic
hypotension

152

Fluoxetine, paroxetine,
sertraline

SSRIs ---
Migraine prevention, tension headache
prevention; treatment for coexistant
depression and chronic daily headache
Weight gain, sexual dysfunction,
headache

153

Propranolol, timolol,
nadolol, atenolol

Beta-blockers ---
Migraine prevention [Only propranolol
and timolol FDA approved, but
nadolol and atenolol sometimes
preferred for their longer half-life and
tolerability.]
Drowsiness, depression, decreased
libido, hypotension, memory
disturbance ---
Contraindicated in asthma,
diabetes, CHF, or Raynaud's

154

Verapamil

Calcium Channel
Blockers ---
Migraine prevention; particularly useful
in prolonged or disabling aura, or
complicated migraine syndromes (e.g.,
hemiplegic migarine); long-term
prevention of cluster headaches Constipation, dizziness

155

Valproic acid

Antiepileptic Migraine prevention
Hepatotoxicity, pancreatitis, blood
dyscrasias, sedation, hair loss,
weight gain, tremor, decreasing
cognition

156

Topiramate

Antiepileptic Migraine prevention
Kidney stones, decresing cognition,
parestesias, weight loss acute angle-closure glaucoma

157

Oxygen

Acute treatment of cluster headaches --- ---
Rebound can occur when oxygen
stopped

158

Lithium

Alters circadian rhythm (?) Cluster headache prevention
Weakness, nausea, thirst, tremor,
lethargy, blurred vision & slurred
speech Confusion, nystagmus
Must monitor blood levels; do not use
with indomethacin or Na-depleting
diuretics

159

Tacrine

AChE inhibitor Inhibits AChE and BuChE Mild to moderate Alzheimers Transaminase elevation
Nausea, vomiting, diarrhea,
abdominal cramping
Metabolized by P450; dosed 4/day;
now obsolete

160

Donepezil

AChE inhibitor Inhibits AChE
Mild to moderate Alzheimers; severe
Alzheimers ---
Nausea, vomiting, sleep
disturbance Metabolized by P450; dosed 1/day

161

Rivastigmine

AChE inhibitor Inhibits AChE and BuChE Mild to moderate Alzheimers ---
Nausea, vomiting, sleep
disturbance
Hydrolyzed by cholinesterases;
dosed 2/day

162

Galantamine

AChE inhibitor
Inhibits AChE; allosteric modulator of
nicotinic receptors Mild to moderate Alzheimers ---
Nausea, vomiting, sleep
disturbance
Metabolized by P450; dosed 2/day
(1/day for ER strength)

163

Memantine

Partial antagonist of NMDA receptor Severe Alzheimers ---
Dizziness, confusion, headache,
constipation
Excreted unchanged in urine; dosed
2/day

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