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year 2 > Pharm Exam 2--opioids, anticonvulsants, NSAID, DMARD > Flashcards

Pharm Exam 2--opioids, anticonvulsants, NSAID, DMARD Flashcards

1
Q

**Morphine

A

STRONG AGONIST

  • binds to and stimulates ALL opiate receptors
  • -closes Ca++ channels on presynaptic (all)
  • –↓ ACh, NE, 5HT, *glutamate, *substance P
  • -Mu also open K+ on postsynaptic- hyperpolarize
  • -release HISTAMINE (orthostatic hypoTN)
  • administered in all routes
  • high first pass metabolism in liver
  • -3-glucuronide (50%): more potent analgesia > morphine
  • -6-glucuronide (5-15%): hyperalgesia, excitement, myoclonus
  • excreted primarily in urine as 3-glucuronide (renal problems metabolite accumulates?)

EFFECTS
-Analgesia: sensory & affective; (tolerance)-mu, kappa
-Sedation/mental clouding (tolerance)-mu
-Euphoria or dysphoria (kappa & delta) (tolerance)-mu
-Nausea: direct stim of CTZ (tolerance)
(Mu → side-effects)

  • Anti-tussive: lower doses
  • Respiratory depression: ↑ PaCO2
  • -good: pulm edema; bad: COPD, asthma, cor pulmonale
  • MIOSIS (no tolerance)
  • ↑ intracranial pressure: due to ↑ CO2 (vasodilate, ↑ flow)
  • ↓ body temp
  • Truncal rigidity
  • Cardiovascular: bradycardia (not direct), orthostatic hypoTN
  • GI: CONSTIPATION (no tolerance)
  • GU: retention
  • Uterus: relax
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2
Q

Hydromorphone (Dilaudid)

A

STRONG AGONIST

  • morphine derivative
  • more potent and as effective as morphine
  • *-used w/ Renal dysfunction–metabolites don’t accumulate
  • –like they will w/ Meperidine
  • *-less itching than morphine
  • slightly shorter DOA than morphine
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3
Q

Heroin

A

STRONG AGONIST

  • schedule I drug
  • easily passes BBB and is metabolized → morphine
  • 10x more potent than morphine
  • high abuse potential
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4
Q

Methadone (Dolophine)

A

STRONG AGONIST

  • *longer DoA than morphine
  • potent mu agonist
  • BLOCKS NMDA receptors– ↓ tolerance
  • ↓ reuptake of Monoamines
  • used in HARD TO TREAT pain (neuropathic, cancer)
  • tolerance & dependence occur more slowly
  • helps ↓ withdrawl symptoms in heroin addicts
  • more mild but longer withdrawl
  • absorbed more slowly → doesn’t produce high
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5
Q

Meperidine (Demerol)

A

STRONG AGONIST

  • short DoA (not for long term use)
  • antimuscarinic → tachycardia, dilates pupils
  • blocks reuptake of Serotonin (TCA or SSRI)
  • use in healthy pts and/or pts that have problems w/ other opiate agonists (NOT long term)
  • -too short DoA
  • -**metabolites (normeperidine) accumulate
  • -anxiety & **SEIZURES (w/ Renal failure cause seizures)
  • -OD can cause excitement and convulsion
  • euphoria → significant addiction potential
  • **doesnt suppres COUGH
  • **doesnt cause MIOSIS
  • do not use w/ MAOI (phenelzine, selegiline, linezolid)
  • -can cause serotonin syndrome

-reduces shivering (and other emergence symptoms?)

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6
Q

Fentanyl (Sublimaze) #

A

-preffered over morphine in anesthesia-

STRONG AGONIST

  • highly LIPID soluble
  • 100x more potent than morphine
  • shorter DoA and 1/2life than morphine or meperidine (abuse potential)
  • used to aid induction & maintenance of GA
  • supplement regional & spinal analgesia
  • -attenuate hemodynamic responses & maintain cardiac stability
  • -administered in various forms (transdermal, lozenges)
  • extensively metabolized by CYP3A4- significant interaction w/ inhibitors or inducers
  • tolerance and dependance less common

-truncal rigidity → NM blocker b/c hard to breat

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7
Q

Alfentanil / Sufentanil / Remifentabuk

A

STRONG AGONIST

  • primarily used in anesthesia
  • faster onset & shorter DoA than fentanyl
  • IV or epidural
  • undergoes liver biotransformation via CYP3A4
  • -interactions w/ agents that inhibit CYP3A4

-truncal rigidity

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8
Q

Hydrocodone (Codan)

+ acetaminophen = Vicodin

A

Moderate-to-Strong AGONIST

  • synthetic codeine derivative
  • undergoes complex hepatic metabolism:
  • -O & N demethylation
  • -6-keto reduction
  • –6-α and 6-β hydroxy active metabolites
  • *–some is converted to HYDROMORPHONE (CYP2D6)
  • inhibitors of CYP2D6 (quinidine & SSRI) reduce analgesia

-does have a direct action on Mu rececptors

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9
Q

Oxycodone (OxyContin)

+ acetaminophen = Percoset

A

Moderate-to-Strong AGONIST

  • similar to hydrocodone and morphine
  • treats cancer pain, posoperative, postextractional, and post partum pain
  • *Restless Leg and Tourettes syndromes
  • oral administration
  • distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, CNS
  • metabolized by liver excreted in urine
  • has direct action but requires metabolism via CYP2D6
  • -oxymorphone (SSRI will ↓)
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10
Q

Oxymorphone (Opana)

A

Moderate-to-Strong AGONIST

  • IF patient is on SSRI
  • active metabolite of oxycodone
  • effects similar to morphine or oxycodone
  • very potent
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11
Q

Codeine

A

MODERATE agonist & **Antitussive

  • at higher doses- analgesic and addictive properties
  • *-does not bind to Mu receptor-
  • -will not compete w/ strong agonists
  • partially metabolized to morphine by CYP2D6 (analgesic)
  • use caution w/ small children (<2 yrs)
  • frequently combined w/ aspirin or acetaminophen

-OD can cause excitement and convulsion

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12
Q

Tramadol (Ultram)

A

MODERATE agonist/ Multiple Actions

  • weak Mu agonist
  • inhibits reuptake of NE and 5HT
  • not completely inhibited by Naloxone
  • good analgeisa (codeine) w/ mild opioid like SE
  • combo w/ *antidepressants → *SEIZURES
  • should not be combined w/ TCA. SSRI, MAOI → serotonin syndrome
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13
Q

Buprenorphine (Buprenex)

A

MIXED agonist-antagonist

  • partial agonist at Mu & possibly Kappa receptors
  • less analgesia than morphine
  • **much less abuse potential than morphine
  • **Reduces drug craving in heroin addicts
  • IV, **sublingual, nasal
  • formulated w/ Naloxone which cannot be absorbed sublingually and prevents it from IV use
  • acts as antagonist if combined w/ strong agonist
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14
Q

Pentazocine (Talwin)

A

MIXED agonist-antagonist
-used for MODERATE pain

  • agonist at kappa** (analgesia)
  • *partial at mu
  • less sedation, respiratory depression, and GI effects
  • dysphoria*, CNS stim, hallucinations
  • can precipitate withdrawl syndrome

-combination w/ strong agonists is CI

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15
Q

Naloxone (Narcan)

A

PURE ANTAGONIST

  • DOC for opioid overdose
  • high 1st pass– usually given IV**
  • reverse respiratory depressant effects of opioids
  • short DoA**
  • can precipitate withdrawls in addicts
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16
Q

Naltrexone (ReVia)

A

ANTAGONIST

  • orally effective
  • long acting (24hrs)
  • prevents recovering addicts from getting high
  • must be detoxified (withdrawl) before therapy
  • ↓ craving in alcoholics
  • risk of HEPATOTOXICITY
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17
Q

Dextromethorphan

A

ANTITUSSIVE

  • blocks NMDA receptros (may ↑ morphine analgesic)
  • block neuronal uptake of 5HT
  • -combo w/ MAOI can cause serotonin syndrome
  • no analgesic effect
  • less constipation than codeine

-excess pure detromethorphan in powder can cause death, brain damage, seizures, loss of consciousness, irregular heart beat

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18
Q

Diphenoxylate plus atropine

A

ANTIDIARRHEAL

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19
Q

Loperamine (Imodium)

A

ANTIDIARRHEAL

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20
Q

-Tapentadol

A

MODERATE AGONIST/ Mutli Actions

  • similar to tramadol
  • mu receptor agonist
  • inhibits NE re-uptake (chronic & neuropathic pain)
  • stimulate α2
  • nausea, vomiting, sedation
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21
Q

–Nalmefene

A

ANTAGONIST

  • used for treatment of opioid OD
  • similar to naloxone but longer DoA
  • chronic treatment of alcoholism
  • LESS liver toxicity than Naltrexone
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22
Q

Esters

A
  • shorter DoA
  • ↑ degree of systemic toxicity
  • -PABA inhibits action of sulfonamides
  • rapidly metabolized by butyrylcholinesterase in plasma

Connects lipophilic group to ionizable group
-weak bases (pKa 8-9)
(Procaine, Tetracaine, Benzocaine, Cocaine)

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23
Q

Amide

A
  • longer DoA
  • ↓ degree of systemic toxicity
  • metabolized in liver (CYP450)

Connects lipophilic group to ionizable group
-weak bases (pKa 8-9)

-Lidocaine*, Prilocaine, Bupivacaine, Mepivacaine, Ropivacaine, Etidocaine, Articaine

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24
Q

Benzocaine

A

ESTER

  • TOPICAL ONLY: treat puritis in OTC, sunburn, minor burns
  • *very lipophilic
  • **pKa ~3.5- non-ionized at physiological pH

-potential link to met-Hb

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25
Q

Bupivicaine (Marcaine)

A

AMIDE

  • long DoA
  • **sensory before motor (more sensory than motor)
  • infiltration, spinal anesthesia, ***epidural
  • post-op pain control
  • **greater cardiotoxicity
  • -high affinity to resting cardiac Na channels
  • -reverse w/ lipids
  • -do NOT use for IV regional anesthesia
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26
Q

Etidocaine

A

AMIDE

  • long DoA
  • rarely used for infiltrative, peripheral, or epidural blocks
  • **motor before (or w/o) sensory block
  • may cause inverse differential block
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27
Q

Prilocaine

A

AMIDE

  • intermediate DoA
  • **Highest rate of clearance (careful w/ pts w/ liver damage)
  • metabolite may produce met-Hb
  • limited to dentistry due to met-Hb
  • do NOT use in pts w/
  • -cardiac or respiratory disease
  • -idiopathic/congenital met-Hb-emia
  • reverse w/ methylene blue
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28
Q

**Procaine

A

ESTER

  • used in infiltration anesthesia & *diagnostic blocks
  • short DoA
  • potency of others are RELATIVE to Procaine
  • PABA metabolic product → ↓ action sulfonamide
  • minimal systemic toxicity
  • no local irritation
  • available w/ or w/o epi (2x DoA)
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29
Q

Tetracaine

A

ESTER

  • *spinal anesthesia w/ dextrose (heavier than CSF)
  • used for ophthalmological
  • long DoA & slow onset of action
  • 16x more potent/toxic than procaine
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30
Q

**Lidocaine (Xylocaine)

A

AMIDE

  • infiltration & epidural anesthesia
  • intermediate DoA; potency of 4
  • rapid onset, minimal local irritation
  • some topical activity
  • **Transient neurological symptoms (transient pain, dysesthesia)
  • -if used as spinal anesthesia (NOT DOC for spinal)
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31
Q

Cocaine

A

ESTER

  • topical anesthesia of mucous membranes around URT
  • short acting
  • topical only
  • ↑ catecholamine in CNS and periphery
  • -vasoconstriction

NARCOTIC:

  • ↓ repuptake of DA (and NE)
  • energy burst, euphoria
  • stimulates SYMPATHETIC
  • -↑ HR, BP → cerebral hemorrhage
  • -mydriasis
  • -↓ appetite

-hyperthermia, seizures

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32
Q

Ropivicaine

A

AMIDE

  • high volume peripheral blocks & epidural
  • S-enatiomer of bupivicaine
  • **less cardiac toxicity
  • **less lipid soluble & cleared more rapidly
  • -adverse effects less likely
  • PHK similar to bupivicaine
  • minor vasoconstricting
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33
Q

Mepivacaine

A

AMIDE

  • peripheral nerve blocks
  • NOT used in labor → toxic to neonate
  • intermediate DoA
  • potency 2
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34
Q

Articaine

A

AMIDE

  • has additional ester group- esterases metabolize
  • -↓ half-life & systemic toxicity
  • widely used in dentistry
  • -large therapeutic window & low potential systemic toxic
  • -can inject more later
  • may devole persistent paresthesias
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35
Q

Dibucane

A

AMIDE

  • inhibits butyryl-AChase
  • Dibucaine numer shows activity of butyryl-AChease
  • differentiate b/w substitution mutations of butyryl-AChease
  • inhibits wild type (normal) MORE than mutated type
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36
Q

nicotine

A

(use and mechanism)
-Activates nicotinic receptors in CNS & periphery
PERIPHERY
–↑ Epi release
–↑ HR, BP
–↑ tone & activity of GI
CNS
–**↑ 5HT & DOPAMINE release (↑ DA → endogenous opioid)
–effects memory and learning (nicotinic receptors)
-induces CYP450

  • psychological & physical dependence; withdrawal
  • -Buproprion ↓ craving (receptors up-regulated)
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37
Q

marijuana

A

(effects and drawbacks w. chronic use, medical effects)

  • targets presynaptic cannabinoid receptor (CB1) to alter NTM release
  • inhibits ACh & glutamate release
  • -impairs memory & cognitive function of hippocampus

HARMFUL EFFECTS:

  • amotivational syndrome
  • ↓ testoserone
  • depression, paranoia, panic

MEDICAL EFFECTS

  • anti-emetic
  • analgesia
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38
Q

MDMA

A

(mxn, effects, toxicity)

  • Blocks 5HT transporter (SERT)
  • ↑ 5HT release
  • ↑ postsnyaptic 5HT receptors (↑ 5HT all over brain)

-causes feelings of peace, empathy, acceptance

  • neruotoxic due to SERT inhib
  • can cause confusion, depression, anxiety, insomnia etc
  • death due to dehydration, hyperthermia, heart, kidney failure
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39
Q

LSD/Mescaline/Psilocybin

A

(basic mxn & effects)

  • Binds 5HT2 (Gq)
  • no effect on mesolimbic DA → no reinforcement/ dependence
  • profound CNS w/ minimal peripheral effects
  • euphoria
  • visual hallucinations, altered perceptions, synesthesia
  • labile mood (elation to fear)
  • Mescaline: peyote; less potent
  • Psilocybin: muschrooms
40
Q

PCP (Phencyclidine)

A

(basic mxn & effects)
-developed as a dissociative anesthetic

  • Targets NMDA/glutamate system
  • stimulant
  • depressant
  • hallucinogenic
  • analgesic
  • physically aggressive behavior
  • amnesia or personality changes
41
Q

ketamine

A

(basic mxn & effects)

  • targets NMDA/glutamate
  • causes feelings of floating or dissociation
  • sympathomimetic
42
Q

GHB

A

(basic mxn & effects)

  • targets GABA system; ↑ inhibition
  • effective in preventing memory storage
43
Q

Methamphetamine

A

-blocks VMAT and reverses DAT
→ ↑ DA (NE)

  • **neurotoxic effect → damage DA-ergic & 5HT-ergic
  • causes loss of DAT
  • cardiac toxicity- pulm edema, heart failure
  • formication- bugs under skin
  • Dependence and Tolerance occur rapidly
  • Dilated pupils
44
Q

Inhaled drugs & Amyl and Butyl nitrate

A
  • produce dizzines and intoxication
  • symptoms: burns on lips or chemical smell
  • Smooth muscle relaxants that cause euphoria
  • hypotension & reflex tachy
  • effects occur w/in 30 sec
45
Q

**Aspirin (acetylsalicylic acid, ASA)

A

NSAID (analgetic, antipyretic, antiinflammatory, anitplatelet)

-irreversible inhibitor of both COX-1 & COX-2

  • -analgetic: central & peripheral ↓ PG synthesis; prevents sens. of pain receptors
  • -antipyretic: acts at hypothalamic area ↓ fever & malaise
  • -antiinflammatory: ↓ PG; ↓ tissue damage
  • -antiplatelet: lack ability to make more COX; can’t activate or cause others to activate (lasts 8-10 days)
  • readily absorbed in stomach; ↑ [ ] in mucosal cells
  • hydrolyzed in plasma, liver, erythrocytes
  • **binds plasma proteins (50-90%); cometes w/ other drugs that bind–WARFARIN
  • low dose → 1st order; high dose → 0 order
  • excreted by kidneys: alkalize urine ↑ excretion;
  • -↓ GFR ↓ excretion

Adverse reactions: respiratory & metabolic, platelet, uric acid, lungs, GI tract, kidneys

46
Q

**Acetaminophen

A

(analgesic & antipyretic; NO anti-inflammatory)

  • -not effective anti-rheumatic
  • -equipotent to aspirin for anaglesia & antipyretic
  • not a COX inhibitor, preferred if patient has:
  • -allergic reaction to ASA
  • coagulation disorders (hemophilia)
  • peptic ulcers
  • gouty arthritis & taking uricosuric agents
  • metabolized by CYP2E1 in liver
  • -chronic et-OH can ↑ toxicity

overdose causes FATAL HEPATIC NECROSIS

  • -caused by hydroxylated intermediate metabolite
  • -uses up Glutathione
  • -↑ serum transaminase, LDH
  • -progress to encephalopathy, coma, death

Treat OD w/

  • N-acetylcysteine (w/in 10-12 hrs)
  • gastric empty (w/in 4 hours)
  • forced diuresis
  • hemodialysis
47
Q

Indomethacin (Indocin)

A

NSAID (analgetic, antipyretic, antiinflammatory)

  • *very potent anti-inflam & anti-rheumatic
  • -**worst side-effect profile–GI irritation
  • inhibits phospholipase A2
  • reduce PMN migration
  • used for patent ductus arteriosus

primary NSAID used in Gout

  • acute attacks of Gout** + colchicine
  • -aspirin or salicylate CI in gout → ↓ excretion
48
Q

Ketorolac (Toradol)

A

NSAID (analgetic, antipyretic, antiinflammatory)

  • VERY potent
  • analgesic in post-surgical pain (instead of opioids that cause constipation)
  • oral, IV, IM
  • after 5 days of use → frequent GI SE
49
Q

Diclofenac (Voltaren)

A

NSAID (analgetic, antipyretic, antiinflammatory)

  • potent COX inhibitor
  • mostly GI side effects
  • combine w/ misoprostol (PGE1 analog) → Arthrotec
  • -protects GI
50
Q

**Ibuprofen (Advil, Motrin)

A

NSAID (analgetic, antipyretic, antiinflammatory)

best adverse effect profile

  • first choice drug
  • lowest incidence of side-effects
  • treatment of RA and OA
  • combo w/ ASA ↓ effect
51
Q

Naproxen (Naprosyn)

A

NSAID (analgesic, antipyretic, antiinflammatory)

  • Longest lasting (fewest daily doses)
  • treat RA, OA, ankylosing spondylitis
  • extensively binds to *plasma proteins (anticoagulants, hypoglycemic agents)
  • MIGRAINE treatment
52
Q

Piroxicam

A

NSAID (analgetic, antipyretic, antiinflammatory)

  • inhibits PMN migration & lymphocyte function
  • ↓ oxygen radical production
  • long half-life
  • high incidence of GI SE
53
Q

Nabumetone

A

NSAID (analgetic, antipyretic, antiinflammatory)

-pro-drug that must be converted to active metabolite

54
Q

**Hydroxychloroquine

A

DMARD

  • Anti-muscarinic, anti-cholinesterase, anti-protease
  • inhibits PG synthesis
  • inhibits biosynthesis of mucopolysaccharide
  • inhibits responses to chemotactic stimuli & phagocytosis
  • stabilizes lysosomes
  • reacts w/ NA and tissue proteins

-High affinity for melanin–concentrates in epidermis and retina

  • toxicity: hemolysis (G6PD def), NADPH synthesis is hindered and can’t reduce met-Hb to Hb
  • ototoxicitym retinopathy, peripheral neruopathy
55
Q

**Sulfasalazine

A

DMARD

-metabolized to Mesalamine by intestinal bacteria
Mesalamine
-inhibits COX → inhibit AA metabolism
-inhibits lipoxygenase → inhibits LT synthesis

-was used to treat IBD

toxicity: GI and Rash,
- Hepatitis and Blood dycrasias are rare
- -monitor hepatitis & marrow suppression for first 2-3 weeks

56
Q

**Infliximab

A

DMARD–acts on TNF-α

  • Chimeric IgG1k MAb against TNF-α
  • treatment of Crohns & RA
  • -combined w/ methotrexate in RA

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

57
Q

**Adalimumab

A

DMARD–acts on TNF-α

  • Recombinant human IgG1 MAB
  • unlike Infliximab, approved for MONOTHERAPY in RA

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

58
Q

**Certolizumab pegol

A

DMARD–acts on TNF-α

-Humanized Ab that is POTENT neutralizer of TNF-α

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

59
Q

**Golimumab

A

DMARD–acts on TNF-α

-Human derived MAb against TNF-α

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

60
Q

**Entanercept

A

DMARD–acts on TNF-α

  • dimeric fusion protein– fake TNF-α receptor
  • -NOT a MAb
  • Binds and inactivates TNFα
  • doesn’t affect TNF production or serum levels

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

61
Q

**Leflunomide

A

DMARD–inhibitor of NA synthesis
-↓ immune reaction

-inhibits de novo PYRIMIDINE synthesis via
→ inhibit dihyroorotate dehydrogenase (DHODH)
-inhibits tyrosine kinase associated w/ cytokine and GF receptor
-inhibits induction of COX-2

-ORAL administation

62
Q

Mycophenolate mofetil

A

DMARD–inhibitor of NA synthesis
-↓ immune reaction

-inhibits lymphocyte PURINE synthesis
→ inhibits inosine monophosphate dehydrogenase

  • ORAL administration
  • prodrug for mycophenolic acid (MPA)
63
Q

**Anakinra

A

DMARD–interleukin receptor antagonist

  • recombinant IL-1 receptor antagonist (IL-1Ra)
  • improves swollen and painful joints
64
Q

**Toclizumab

A

DMARD–interleukin receptor antagonist

  • humanized MAb that inhibits IL-6 receptor
  • Adverse reaction similar to other immunosuppressants
65
Q

**Tofacitinib

A

DMARD–JAK inhibitor

  • primarily inhibits JAK1, JAK3, and some JAK2
  • may precipitate SERIOUS INFECTIONS and MALIGNANCY
66
Q

**Penicillamine

A

DMARD

  • Chelating agent effective in RA (and in Wilson’s disease)
  • inhibits collagen formation
  • ↓ CIRCULATING IgM rheumatoid factor but not absolute lvls
  • depresses T-cell activity but NOT B-cell

High incidence of adverse reactions:

  • thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia
  • AI diseases: SLE-like, pemphigus, Goodpasture, Myasthenia graves, polymyositis, stenosing alveoli’s
  • alteration in TASTE
  • ↑ risk in pts >65
67
Q

Zileuton

Zafirlukast & montelukast

A

lipoxygenase inhibitor

LT receptor inhibitor
-effective against asthma

68
Q

Latanoprost

A
  • 1st line treatment of glaucoma
  • ↑ resorption of aqueous humor
  • changes color of light blue eyes
  • PGF2α
69
Q

**Celecoxib

A
  • reversible inhibition of COX-2 (PGI2)
  • ↓ potential for gastropathy & GI bleed
  • ↑ risk of CVD due to ↑ ratio of TXA2 → vasoconstriction and platelet activation

CI: GI disease, asthma, pregnancy, renal failure, sulfonamide hsn.

70
Q

**Arhrotec

A

-combo of diclofenac & misoprostol

Diclofenac-NSAID
Misoprostol- PGE1 analog- protects GI

71
Q

**Rituximab

A

DMARD- inhibitor of B-cell diff

  • chimeric MAb against CD20 on pre-B & mature B-cell (>90% B-cell NHL)
  • CD20 NOT found on: hematopoietic SC, pro B-celll, normal plasma cell, or other normal tissue

General Adverse effect themes:

1) Injection: irritation & pain
2) CI in children & pregnancy: don’t know effects yet
3) Immunosuppresion: ↑ risk of infections & cancer
- Hypersensativity: murine protein ↑ chance

72
Q

**Abatacept

A

DMARD- inhibitor T-cell activation & B-cell diff.

  • fully human recombinant fusion protein
  • costimulatory or 2nd signal BLOCKER of T-cell activation
  • -↓ host defense against infections and malignancies
73
Q

ASA adverse reactions & contraindications

A
  • Initially ↑ respiration → respiratory alkalosis,
  • then ↓ respiration → metabolic & respiratory acidosis

Warfarin + ASA:

1) inhibits platelet aggregation/coagulation (8-10 days)
2) displaces warfarin for PP– 2% change = 2x [ ]

Uric acid: ASA competes w/ reabsorption

  • ↓ excretion of UA & ↑ blood [ ]; exacerbates gout
  • very high [ ] ↓ UA secretion

Lungs: blocks PG pathway which ↑ LT pathway → asthma

GI tract: ↑ acid production → ulceration & bleeding
-salicylates ↓ secretion of protective mucus

Kidneys: ↓ PG allows ↑ vasoconstriction (ATII, NE, ADH)
-renal damage, failure; interstitial nephritis, nephrotic syndrome

Salicylism: (large repeated doses) dizziness, ringing ears, visual & hearing problems. Maybe skin eruptions, CNS problems

Reye’s syndrome: cerebral edema in children w/ viral infections (uncouples oxidative phosphrylation in hepatic mitochondria)

Contraindications

  • Dont take aspirin for ~week before pregnancy or elective surgery
  • ↓ dose w/ oral anticoagulants, hypoglycemic agents
  • bleeding condition
74
Q

Typical non-specific NSAID toxicities

A
  • GI - pain, bleeding, ulcer, pancreatitis, diarrhea
  • CNS - headache, dizziness, confusion, depression
  • Lung - bronchoconstriction
  • Bone marrow - agranulocytosis, aplastic anemia
  • Nephrotoxicity - acute renal failure, interstitial nephritis, nephrotic syndrome
  • Hepatotoxicity - enzyme elevation, hepatitis
  • Hypersensitivity reactions
75
Q

Sulindac (Clinoril)

A

NSAID (analgetic, antipyretic, antiinflammatory)

  • less nephrotoxic
  • SEVERE GI effects including pancreatitis
76
Q

**Gold salts

A

DMARD
-inhibit phagocytosis, proteolytic enzymes of PMN

TOXICITY: bone marrow damage

77
Q

**Colchicine

A

Acute attack of Gout

  • inhibits phagocytosis of urate by PMN
  • -binds tubulin→ inhibits microtubular assembly
  • -helps terminate inflammatory process of ACUTE attack
  • inhibits formation of LTB4
  • -inhibits leukocyte migration
  • effective only against gouty arthritis
  • no effect on rate excretion
  • no analgesic effect, no effect on COX
  • SE: **DIARRHEA. nausea, vomiting, abdominal pain
  • combine w/ indomethacin?
78
Q

**Probenecid (Benemid)

A

Hyperuricemia- uricosuric agent

  • reduces pool of uric acid by ↓ re-uptake in kidney (blocks organic anion transporter)
  • -prevent crystal formation and acute attack
  • wait 2-3 weeks after acute attack
  • **decreases excretion of many acidic compounds:
  • -*penicillin, NSAIDs glucuronides

–should NOT be used in acute attack → ineffective & may precipitate an attack

79
Q

**Allopurinol (Zyloprim)

A

Hyperuricemia- Xanthine oxidase inhibitor

  • decreases the formation of uric acid
  • -blocks metabolism of xanthine and hypoxanthine
  • metabolized by liver → oxipurinol (active compound)

SE: vasculitis, agranulocytosis, hsn rxn

-initially may provoke attack– prophylaxis w/ colchicine

DRUG INTERACTIONS:

  • ↑ effect of chemo mercaptopurines 6MP and azathioprine
  • ↓ activation of fluorouracil 5FU → ↓ effect
  • ↓ metabolism of Warfarin & Probenecid

-should NOT be used in acute attack → ineffective & may precipitate an attack

80
Q

*Febuxostat (Uloric)

A

Hyperuricemia- Xanthine oxidase inhibitor

81
Q

**Rasburicase (Fasturtec)

A

Hyperuricemia- enzyme converting uric acid to *allantoin

  • recombinant form of urate oxidase (humans lack)
  • -allantoin is readily excreted
  • b/c it is a non-human protein HSN run occur
  • -can probably only use drug once
82
Q

**Sumatriptan (-triptans)

A

5-HT agonists- migraine symptoms

  • constricts mostly the large intracranial arteries
  • -highly selective for 5HT-*D receptors– on intracranial vessels (AV anastomoses)
  • may ↓ release of neuropeptide-mediated inflammatory substance

-NOT an analgesic– direct vasoconstriction ↓ pain

SE: VASOSPASM- coronary aa.(angina, MI), peripheral ischemia
-rare cardiac arrhythmias–vent tachy/fib, arrest, death)

CI: any vascular disease, renal impairment, breast feeding, HTN

83
Q

**Ergotamine tartrate

A

5-HT agonists- migraine symptoms

-causes vasoconstriction like -triptans , but less specific

  • partial agonist at 5-HT receptors in certain blood vessels
  • partial agonist at α1
  • -antagonist of 5-HT in SM
  • -poor agonist/antagonist in CNS
  • more potent vasoconstrictor than -triptans
  • ergotism: vasoconstriction + CNS

-pts w/ peripheral vascular disease should avoid

84
Q

Migraine prophylaxis

A 
Valproic Acid: block Na channels, ↑ GABA, ↓  NMDA
Topiramate: block Na channels, ↑ GABA, ↓  NMDA
Botox
ATII receptor blocker (-sartans)
Β-blocker- Propranolol
Clonidine
CCB- Verapamil
Antidepressants- Amitriptyline
85
Q

**Nitrous Oxide

A

Inhaled general anesthetic (properties & toxicities)

-blocks NMDA

  • reduces hypotension**
  • little respiratory depression
  • Fast onset and recovery
  • second gas effect**→ ↑ rate of induction
  • **GOOD ANALGESIA (cannot produce anesthesia)
  • no renal or liver toxicity
  • diffusion hypoxia
  • replaces any trapped gas (nitrogen) → expands
  • -Caution occluded middle ear/eustacian tube, pneumothorax, loop of intestine, lung or renal cysts
  • DO NOT USE after EYE SURGERY (3 months) → irreversible loss of vision

-**neurophathy w/ chronic exposure
-inactivates Methionine synthase → ↓ DNA syntheses
→ ↓ WBC and RBC megaloblastic anemia

86
Q

**Halothane

A

Inhaled general anesthetic (toxicities)

-slow induction rapid awakening

  • *-Immune response (Cl- & Br-),
  • *-hepatitis (Cl- & Br-)
  • *-malignant hyperthermia (w/ succinylcholine)
  • *-cardiovascular problems- ↓ CO and arrhythmia
  • *-miscarriage
  • significant uterine relaxation (prolong delivery
  • ↓ renal function and urine flow
  • **depresses myocardium → ↓ CO
  • sensitization to catecholamines → arrhythmias
87
Q

**Isoflurane

A

Inhaled general anesthetic (advantages/popularity)

  • *-MOST COMMONLY USED
  • *-HEPATIC and RENAL toxicity NONEXISTANT
  • *-useful in neurosurgery
  • *-low toxicity

MAC 1.17
blood/gas 1.46

  • induction & emergence > halothane or enflurane
  • vasodilation
  • ↓ BP (↓ w/ NOs), ↓ respiration
  • **↑ HR (prevent w/ opioids)
  • *-pungent odor

-high [ ] → uterine relaxation
-dilates cerebral vasculature → ↑ pressure
-↓ cerebral metabolic 02 use → neurosurgery
(Propofol ↓ BF)

  • does NOT depress myocardium or sensitize to catecholamines (Halothane)
  • vasodilation could cause coronary steal
88
Q

**Sevoflurane

A

Inhaled general anesthetic (advantage/popularity)

MAC 1.80
blood/gas 0.69 (low solubility = easy control)

  • *-SAFEST drug for cardiovascular disease
  • *-LEAST respiratory irritation
  • **cardiac and respiratory depression minimal
  • least irritating, minimal odor → induction
  • -used in CHILDREN
  • rapid effect (0.69)
  • ↑ cerebral blood flow (prevent w. hyperventilation)
  • metabolized to Fl- → kidney damage (rare)
  • Compound A → kidney (degradation in machine)
89
Q

**Desflurane

A

Inhaled general anesthetic

MAC 6.60
blood/gas 0.42

  • Rapid EMERGENCE
  • *-pungent odor, irritates airways
  • similar circulatory effects as Isoflurane
  • -↓ BP, ↑ HR
  • ↓↓↓ respiration (& Propofol)
90
Q

**Thiopental

A

IV general anesthetic– Barbituate

  • INDUCTION & short procedures not involving severe pain
  • -NO analgesic activity
  • ↓ cerebral O2 requirement → used w/ head trauma
  • heart and respiratory depression possible
  • CI in PORPHYRIA (↑ porphyrin synthesis)
91
Q

**Midazolam

A

IV general anesthetic–bezodiazepine

  • Sedation, anxiety relief, anterograde amnesia
  • pre-anesthetic and induction (given IV)
  • minor surgies w/ fentanyl
  • reverse with flumazenil

-highly lipid soluble (rapid onset & short DoA)

92
Q

**Propofol (Diprivan)

A

IV general anesthetic (effects, uses, SE, advantages)
DOC for most anesthetic procedures

  • -**induces as rapid as thipental
  • -**emergence is 10x faster
  • used for induction and maintenance
  • used in critical care settings
  • available as emulsion w/ albumin → **allergic reactions
  • -painful when injected (prodrug fospropofol ↓ pain)
  • SEVERE respiratory depressant (must monitor)
  • vasodilation but blunts baroreflex (no ↑ in HR)
  • -made worse by opioids
  • **least likely to cause nausea & vomiting
  • **↓ cerebral blood flow metabolism * IC pressure (neurosurgery) (isoflurane ↑ blood flow)
  • safe in pregancny
  • Propofol infusion syndrome: young puts w/ head trauma
  • metabolic acidosis, hyperlipidemia, rhabdomyolysis, enlarged liver

-facilitates action of GABA at GABAa
highly lipid soluble (rapid onset & short DoA)

93
Q

Etomidate

A

IV general anesthetic

-MAIN USE- anesthesia in patients at risk of HYPOTENSION

  • facilitates action of GABA by ↑ available receptors
  • -may disperse endogenous inhibitors
  • half life constant
  • likely to cause vomiting and cause
  • ↓ seizure threshold
  • hiccups
94
Q

**Ketamine

A

IV general anesthetic

  • blocks NMDA receptors
  • catatonic state: no response to noxious stimuli, eyes open, respiration maintained
  • Dissociative anesthesia: profound analgesia and superficial level of sleep
  • LITTLE respiratory depression– bronchodilation
  • Sympathomimetic: ↑ HR and BP
  • no nausea or vomitting
  • Emergence delirum: bizzare dreams, hallucinations, psychosis
  • ↓ w/ benzos
  • ↑ cerebral blood flow and intracranial pressure
95
Q

General Anesthetics EFFECTS

A

EFFECTS of GENERAL ANESTHETICS
-amnesia, analgesia, unconsciousness, ↓ autonomic response, immobility in response to pain

  • ↓ BP & HR: vasodilation, cardiac depression, ↓ baroreflexes, ↓ SNS tone
  • ↓ respiratory drive (gag, cough, LES)
  • ↓ metabolism in brain
  • ↑ intracranial pressure: ↑ blood flow from vasodilation
  • hypothermia
  • nausea & vomiting (relived 5ht3 agonist ondansetron)
  • HTN & tachy on emergence
96
Q

Enflurane

A

Inhaled general anesthetic (JUST KNOW NAME)

MAC 1.63
blood/gas 1.90

  • more rapid induction than halo thane
  • muscle relaxation and analgesia
  • depress respiration
  • uterine relaxation

-may produce fluoride → reversible kidney damage (rare)

97
Q

list LA in order from shorts acting/least lipid soluble to longest/most lipid soluble

A 
Procaine         1     Short
Cocaine          2    Med
Mepivicaine    2    Med
Lidocaine        4    Med
(Prilocaine)
Tetracaine      16    Long
Bupivicaine    16    Long
Ropivicaine    16    Long
Etidocaine

year 2 (15 decks)

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