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1
Q

Sumatriptan

A

Analgesic, HA abortive

MOA:

  • Serotonergic -> vasoconstricion
  • t1/2 = 2hrs

SE’s

  • Chest/neck tightness
  • flushing, sedation
  • Serotonin syndrome in SSRI/SNRI/MAOI/other triptans
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2
Q

Ergotamine Tartrate

A

Analgesic, HA abortive

MOA:

  • Sertonergic, adrenergic, dopaminergic - suppress neurogenic inflammation]
  • vasoconstriction

SE’s

  • Narrow therapeutic window
  • vasoconstriction
  • hallucinations
  • No Pregnancy
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3
Q

Dihydroergotamine

A

Analgesic, HA abortive

MOA:

  • Sertonergic, adrenergic, dopaminergic - suppress neurogenic inflammation]
  • vasoconstriction

SE’s

  • Narrow therapeutic window
  • vasoconstriction
  • hallucinations
  • No Pregnancy
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4
Q

Propranaolol

A

HA prophylaxis, Anyihypertensive, Beta-blocker

MOA:

  • Inhibits CSD
  • good for MVP, HTN, anxiety, tremor

SE’s

  • Bad w. depression, fibromyalgia, Raynaud’s, asthma
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5
Q

Amitriptyline

A

HA prophylaxis, Antidepressant

MOA

  • Tricyclic antidepressant

ClinUse:

  • good in sleep disturbance, neck pain, T-T headache
  • Inhibits CSD

SE’s

  • Weight gain, sedation, dry-mouth, orthostatic hypotension
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6
Q

Valproic acid

A

HA prophylaxis, Anticonvulsant, mood stabilizer

MOA:

  • not well understood
  • ?Na channel blocker, GABA, Ca, K effects?
  • Enhances GABA activity,
  • reduces excittory NT,
  • reduces serotonergic activity

Metabolism:

  • Hepatic metabolism
  • NOT inducer
  • T1/2 15h

Clin Use

  • PO/IV
  • All seizure types
  • Migraine
  • BPD

SE’s:

  • +++ Weight Gain; occasional
  • GI upset
  • menstrual problems,
  • Hair loss
  • thrombocytopenia
  • hepatic encephalopathy w/out elevated enzymes (elevated NH4+) Tx. carnatine
  • Birth defects (spina bifida)
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7
Q

Topiramate

A

HA prophylaxis, Anticonvulsant

MOA:

  • Multiple - Na channel blockade
  • GABA agonist
  • Glu antagonist
  • Reduces neuron firing in TNC & inhibits CSD

Met:

  • Renal excretion unchanged
  • t1/2 = 24h

Clin Use:

  • Broas specturm; no good vs absence
  • chronic migraine prophylaxis
  • neuropathic pain
  • weight loss

SE’s:

  • sedation
  • aphasias
  • parasthesias
  • nephroliths
  • glaucoma
  • weight loss
  • cognitive difficulty
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8
Q

Verapamil

A

HA prophylaxis, antihypertensive Ca entry blocker

MOA:

ClinUse:

SEs:

  • constipation
  • heart block
  • depression
  • weight gain
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9
Q

Lithium

A

HA prophylaxis, mood stabilizer

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10
Q

BoTox

A

HA prophylaxis

MOA:

  • Prevents synaptic vesicle fusion w/ nerve terminal;
  • prevenst ACh/Glu/CGRP release

ClinUse:

  • Best for chronic migraine

​SE’s:

  • Neck pain
  • weakness
  • ptosis, diplopia
  • Spock eyebrow
  • flu-like illness
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11
Q

Phenobarbital

A

Anticonvulsant, sedative-hypnotic

MOA

  • GABA agonist -> opens Cl channels -> hyperpolerization

Metabolism

  • 100 hr T1/2
  • Loading dose required
  • Hepatic metabolism and enzyme inducer

Clinical use

  • All seizure types except absence
  • PO/IV for status epilepticus

Side Effects

  • Hyperactivity in peds
  • Sedation in adults
  • Joint/CT problems
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12
Q

Phenytoin

A

Anticonvulsant

MOA

  • Blocks voltage gated Na channels

Metabolism

  • Hepatic met and Enzyme inducer
  • Zero order Kinetics at high doses; OD with small changes
  • T1/2 variable (6-24h)
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13
Q

Ethosuximide

A

Anticonvulsant

MOA:

  • Blocks T-type Ca channels

Metabolism;

  • hepatic metabolism
  • Mild hepatic induction

Clin Use

  • Absence Seizures
  • PO
  • 1st line by PCP

SE’s

  • Sedation
  • GI distress
  • behavior change
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14
Q

Benzodiazepines

A

Anxiolytic, sedative, amnestic, anticonvulsant, skeletal muscle relaxant

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15
Q

Carbamazepine

A

anticonvulsant, mood stabilizer

MOA:

  • Na channel blocker

Metabolism

  • hepatic met, enzyme inducer
  • short t1/2 = 12h
  • Levels increased by Ca channel blockers & macrolides

Clin Use:

  • Focal and 2nd generalized seizures
  • cheap
  • PO only
  • mood stabilizer for BPD, neuropathic pain, trigeminal neuralgia

SEs

  • Blurred vision
  • sedation
  • neutropenia
  • hyponatremia
  • weight gain
    *
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16
Q

Gabapentin

A

Anticonvulsant

MOA:

  • Increases GABA levels in brain
  • blocks Na post synaptically

Metabolism:

  • v. short T1/2
  • not metabolized/inducer/inhibitor
  • urinary excretion unchanged

Clin Use

  • peripheral neuropathy
  • partial & secondarily generalized seizures
  • PO only

SE’s

  • sedation (esp in elderly)
  • GI distress
  • pedal edema
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17
Q

Lamotrigine

A

Anticonvulsant, mood stabilizer

MOA:

  • blocks pre-synaptic Glu release
  • Blocks Na channel post synaptically

Metabolism:

  • Hepatic metabolism
  • Renal Excretion
  • t1/2 = 24h

Clin Use:

  • Broad specturm vs all seizure types
  • neuropathic pain
  • BPdisorder
  • PO only

SE’s:

  • Allergic rash
  • insomnia
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18
Q

Levetiracetam

A

Anticonvulsant

MOA:

  • Ca channel blocker
  • blocks vesicle exocytosis

Met:

  • Urinary excretion, unchanged
  • Not enzyme inducer
  • Not protein bound

ClinUse:

  • Broad spectrum, focal & generalized
  • equivelent PO/IV dosing
  • Favorite of hospitals

SE’s

  • Cognitive and Behavioral sx
    *
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19
Q

Aspirin

A

Analgesic, antipyretic, anti-inflammatory

MOA:

  • irreversibly inhibits COX
  • lasts 10-14 days in platelets
  • analgesia via COX-2
  • Side effects by COX-1

ClinUse

  • Very goor for inflammatory & somatic pain
  • NO 3rd trimester pregnant women
    • Close DA of fetus
    • APAP instead
  • Kids = APAP
  • Elderly
    • hypoalbuminemia -> toxicity, longer t1/2

ADR:

  • Reyes Syndrome in kids
  • Hepatotox

DDI:

  • Lithium
  • Warfarin
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20
Q

ibuprofen

A

Analgesic, antipyretic, anti-inflammatory

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21
Q

Naproxen

A

analgesic, antipyretic, anti-inflammatory

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22
Q

Oxaprozin

A

analgesic, antipyretic, anti-inflammatory

MOA:

  • concentrates in synovial fluid
  • Non-selective COX inhibitor
  • NFkB metalloprotease inhibitor
  • t1/2 = 40-60h

ClinUse:

  • Orthopedic pain
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23
Q

Meloxicam

A

analgesic, antipyretic, anti-inflammatory

Enolic Acid

MOA:

  • COX2 preferential
  • t1/2 =20h

Clinical Use

  • good for hepatic/renal fail; no need to adjust

AE:

  • Fewer GI effects than piroxicam, diclofenac, naproxen
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24
Q

Celecoxib

A

Analgesic, anti-inflammatory

MOA:

  • COX-2 selective inhibitor

ClinUse

  • Mild - Moderate Pain

AE’s:

  • GI bleed (less than non-selectives)
  • interacts w/ hepatic enzyme inducers
  • decreases ACE-I and diuretic effects
  • Increases Lithium levels
  • Contranidicate w/ sulfa allergy
  • No platelet effects
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25
Q

Ketorolac

A

Analgesic, anti-inflammatory

MOA:

  • Non-selective COX inhibitor

ClinUse:

  • Use for < 5 days
  • shrot term pain management
  • IV/PO
  • Good post op; very strong

AE:

  • Allergic rxns
  • GI effects
  • Hepatotox w/ APAP
  • renal failure
    *
26
Q

Indomethacin

A

NSAID

MOA:

  • Non-selective COX inhibitor
  • concentrates in joints

ClinUse:

  • Gout - couple of weeks
  • Osteoarthritis
  • PDA closure in neonates

AEs:

  • High side effects
  • short term only
27
Q

Diclofenac

A

NSAID

MOA:

  • COX-2 Selective
  • Concentrates in joints

ClinUse:

  • Post-op pain relief
  • Topical

AE:

  • monitor for hepatotox
28
Q

Acetaminophen

A

Analgesic, antiypyretic

APAP

MOA:

  • unclear mech
  • central prostaglandin synthesis
  • no-antiplatelet activity
  • active 4-6hrs

ClinUse:

  • Not Anti-Inflammatory
  • chronic pain, used w/ NSAIDS

AE’s:

  • Narrow therapeutic window
  • fatal hepatotox via glutathione depletion
  • depression, chronic pain, EtOH/drug use, multiple NSAID use
  • Hepatotox
  • No EtOH
29
Q

Morphine

A

Analgesic, drug of abuse

MOA:

  • mu opioid receptor agonist

ClinUse:

  • can be used w/ hepatic failure
    • prolonged t1/2
  • ​Avoid w/ GFR < 30ml/min
    • toxic metabolite accumulation

AEs:

  • Sedation confusion, constipation
  • resp depression, sexxual dysfunction
  • fracture, physical dependence
  • infection, tumor
  • Additeve w/ CNS depressants
  • MAOIs - severe/fatal rxn
30
Q

Meperidine

A

Analgesic

MOA:

  • mu opiod receptor agonist

ClinUse:

  • 10x as powerful as morphine
  • Not for routine use; severe pain

AEs:

  • Mydriasis (all others cause miosis
  • MAOI = fatal/severe rxn
  • ADRS of morphine + increased HR
31
Q

oxycodone

A

Analgesic

MOA:

  • mu opioid receptor agonist
  • equianalgesic to morphine
  • t1/2 = 2-3h
  • To oxymorphone 2D6
  • To noroxycodone 3A4

ClinUse:

  • acute pain

AE:

  • Additive w/ CNS depressants
  • abuse deterent formula
  • ADRS of morphine
    *
32
Q

Oxymorphone

A

Analgesic

MOA:

  • 2x morphine strength
  • metabolic end product of morphine

ClinUse:

  • Acute pain

AR:

  • high abuse potential
  • morphine like ARs
33
Q

Hydromorphone

A

Analgesic

MOA:

  • mu opiod agonist

ClinUse:

  • 7.5x potent as morphine
  • avoid sustained release w/ hepatic disease
  • not for renal disease;

ARs:

  • Morphine like
34
Q

Methadone

A

Opioid abuse

MOA:

  • mu opioid agonist (levo)
  • NMDA receptor antagonist (dextro)
  • SRI
  • t1/2 = 8- 47h

ClinUse:

  • Severe pain (chronic)
  • addiction
  • caution in elderly
  • dont increase more than q14day
  • variable potency - dose dependent

AR:

  • morphine ADRs
  • long QTc
  • arrhythmia
  • baseline EKG
35
Q

Fentanyl

A

analgesic

MOA:

  • mu opioid agonist

ClinUse:

  • 80x strong as morphine
  • patch for severe pain
  • liver disease decreases absorption
  • Ok renal disease

AE:

  • additive w/ CNS depressants
    *
36
Q

tramadol

A

analgesic

MOA:

  • modulation of nociception
  • inhibits NE/5HT reuptake

ClinUse:

  • Chronic pain

AE:

  • don’t combine w/ SRI’s (eg methadone or ADDs)
37
Q

Tapentadol

A

Analgesic

MOA:

  • modulation phase
  • inhibits NE/5HT reuptake

ClinUse:

  • severe pain
  • neuropathic pain (v.strong)

AE:

  • Morphine ADR
  • dont combine w/ SRIs (eg methadone ADDs)
38
Q

Naloxone

A

Opioide overdose

MOA:

  • competitivly blocks mu, kappa, delta opioid receptors

ClinUse:

  • rapidly reverse opiod agonists
  • opiod OD, dependence

AE:

  • can precipitate withdrawal in dependent persons
39
Q

Codeine

40
Q

Buprenorphine

41
Q

Marijuana

A

Pain, chronic pain, weight loss, Cancer, MS, HIV

42
Q

Bupivicaine

A

Long acting local anesthetic

MOA:

  • amide - binds Na channel of inner nerve membrane
  • closes Na channel -> no AP
  • Better in non-ionized form (not acidic places)
  • Best on narrow, heavily myelinated, rapid firing neurons
  • partial liver metabolism

​ClinUse:

  • Inj - long acting local anesthetic
  • w/ Epi for prolonged duration

AE:

  • Most toxic of the ‘caines
  • Cardiac arrest if IV
  • light headed, tinnitus, metallic taste
  • blurred vision, numbness, twitching
  • convulsions
  • Resuscitative equipment available
  • delay in mgmt => acidosis, cardiac arrest, death
  • longest acting 12-18h
    *
43
Q

Ketamine

A

Sedative hypnotic

44
Q

Nitrous oxide

A

dissocidative anesthetic

45
Q

Sevoflurane

A

General anesthetic

46
Q

Isoflurane

A

General anesthetic

47
Q

Propofol

A

General anesthetic

MOA:

  • lipid soluble IV agent
  • GABAa potentiation
  • blocks Na channels
  • impacts endocannabinoid system

ClinUse:

  • IV short acting anesthetic
  • anti-emetic
  • euphoria
  • Aseptic technique - susceptible to bacterial contamination
  • single use parenteral

AE:

  • injection site pain
  • apnea
  • decreased CO
  • hypotension
48
Q

Midazolam

A

Conscious sedation

MOA:

  • GABAa potentiation; enhances effects

ClinUse:

  • IV bzd - for hospital sedation
  • General anesthetic adjuvant
  • 15-20min duration

AE:

  • resp depression
  • addiction, tolerence (error risk)
  • CV depression
  • caution with ER formulation
49
Q

Etomidate

A

sedative-hypnotic

MOA:

  • GABAa modulator at B3 subunits
  • Hepatic metabolism

ClinUse:

  • IV general anesthetic
  • non-analgesia
  • t1/2= 75min

AE:

  • CV and resp depression
  • skeletal muscle movements
  • laryngospasm
  • shock
50
Q

Remifentanil

A

Analgesic

MOA:

  • Opioid receptor agonist

ClinUse:

  • IV - opioid
  • analgesic and sedative
  • short acting - t1/2 = 4min
  • immdiate emmergence
51
Q

Lidocaine

A

Local anesthetic

MOA:

  • medium-acting
  • amide - binds Na channel of inner nerve membrane
  • closes Na channel -> no AP
  • Better in non-ionized form (not acidic places)
  • Best on narrow, heavily myelinated, rapid firing neurons

ClinUse:

  • local anesthesia
  • Epi to prolong action

AEs:

  • seizures
52
Q

Phenobarbital

A

Anticonvulsant, sedative-hypnotic

MOA

  • GABA agonist -> opens Cl channels -> hyperpolerization

Metabolism

  • 100 hr T1/2
  • Loading dose required
  • Hepatic metabolism and enzyme inducer

Clinical use

  • All seizure types except absence
  • PO/IV for status epilepticus

Side Effects

  • Hyperactivity in peds
  • Sedation in adults
  • Joint/CT problems
53
Q

Tetracaine

A

Local Anesthetic

MOA:

  • amide - binds Na channel of inner nerve membrane
  • closes Na channel -> no AP
  • Better in non-ionized form (not acidic places)
  • Best on narrow, heavily myelinated, rapid firing neurons
  • AChE metabolism

​ClinUse:

  • Inj - long acting local anesthetic
  • w/ Epi for prolonged duration
54
Q

Chloroprocaine

A

Local Anesthetic

Short-acting

MOA:

  • amide - binds Na channel of inner nerve membrane
  • closes Na channel -> no AP
  • Better in non-ionized form (not acidic places)
  • Best on narrow, heavily myelinated, rapid firing neurons
  • metabolized by AChE

​ClinUse:

  • Inj - short acting local anesthetic
  • w/ Epi for prolonged duration
  • short acting; 30-60mins

AE:

  • safest ‘caine
    *
55
Q

Sucinylcholine

A

Depolarizing neuromuscular blockade

MOA:

ClinUse:

  • Induction agent
  • facilitate paralysis for intubation

AEs:

  • Disassociate them first
56
Q

Rocuronium

A

Non-depolarizing neuromuscular blockade

MOA

ClinUse:

  • Intubation
  • surgical paralysis

AEs:

  • disassociate first
57
Q

Desflurane

A

General anesthetic

MOA:

  • inhaled hydrocarbon

ClinUse:

  • surgical anesthetic

AEs:

  • delayed emergence
  • delirium
  • N/V
58
Q

Dexmetomidine

A

Anesthetic adjunct

MOA:

  • a2 agonist
  • dose dependent analgesia and sedation

ClinUse:

  • Reduce side effects from high-dose inhalation agents
  • can be used alone for minor procedures

AEs:

*

59
Q

Isoflurane

A

General anesthetic

MOA:

  • inhaled hydrocarbon

ClinUse:

  • surgical anesthetic

AEs:

  • delayed emergence
  • delirium
  • N/V
60
Q

Sevoflurane

A

General anesthetic

MOA:

  • inhaled hydrocarbon

ClinUse:

  • surgical anesthetic

AEs:

  • delayed emergence
  • delirium
  • N/V
61
Q

Neostigmine

A

Paralytic reversal

MOA:

ClinUse:

  • Reverses muscle relaxants

AEs:

Pharm II (3 decks)

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