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Pharmacology > Exam 3 > Flashcards

Exam 3 Flashcards

1
Q

Phenobarbital

A
  • 1st anti-seizure;cheap/effective
  • MonoTx: Gen TC, Partial, IV for Status Epilepticus
  • Effect: Synaptic inhibition via GABA
  • SE: Sedation (adults), hyperactive (kids), increased Rx metabolism (CYP3A4 induction), minor rash
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2
Q

Phenytoin

A
  • MonoTx: Gen TC, Partial
  • Effect: Prolong rate of recovery for Na VG channels (longer inactive)
  • Mostly bound to protein
  • drug conc incr disproportionally to dosage
  • liver meta
  • SE: Warfarin meta affected; induction of CYP3A4; 20% gingival hyperplasia; minor rash
  • SJS: immune response; blistering; 5% mort; flu-like w/ fever - TX discont. RX; TEN is more severe SJS
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3
Q

Fosphenytoin

A

IV Prodrug for Status Epilepticus

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4
Q

Carbamazepine

A
  • MonoTx: Gen TC, Partial, Manic-Dep, Nocicep Pain
  • Effect: Prolong rate of recovery for Na VG channels (longer inactive)
  • Self-meta to 10,11 epoxide; wait 3 wks for level plasma conc.
  • Increase metabolism: phenobarbitol, phenytoin, valproic acid
  • SE: acute (stupor, coma, hyperirritable convulsions) and chronic (drowsy, vertigo, ataxia, blurred vision)
  • CYP3A4 induction
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5
Q

Oxcarbazepine

A
  • Mono/Adjunct Tx: Partial (Mono = 4-16yo)
  • Effect: Prolong rate of recovery for Na VG channels (longer inactive)
  • Prodrug -> active via liver; Inactive via glucoronide conj; renal excretion
  • NO SELF INDUCTION
  • SE: dizzy, nausea, somnolence, ataxia
  • CYP3A4 induction (less than carbamazepine)
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6
Q

Ethosuximide

A
  • MonoTx: Absence
  • Effect: Inhibit T-type Ca Channels
  • No plasma protein binding
  • few Rx interactions
  • 25% urine excretion
  • SE: nausea, vomit, anorexia, CNS: drowsy, lethargy, euphoria, SJS, aplastic anemia
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7
Q

Valproic Acid

A
  • BROAD SPECTRUM AED
  • MonoTx: Absence, myclonic, partial, TC, status epilepticus (IV)
  • Effect: inhibit T-type Ca channel, prolong inactivation Na VG, increase GABA synth (in vitro)
  • Plasma protein binding (most), half-life = 15 hrs (decrease with more AEDs)
  • SE: GI: nausea, anorexia; CNS: sedation, ataxia, tremor
  • Increase hepatic blood enzymes
  • Hepatic toxicity <2 yo (on multiple AEDs incl Valproic)
  • CYP2C9 inhibition -> increased conc. of phenytoin/phenobarb and displaces phenytoin from protein
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8
Q

Gabapentin

A
  • GABA bound to lipophilic ring = cross BBB but does NOT bind to GABA receptor
  • AdjunctiveTX: Partial (w/ or w/o gen 2˚ seizure) and neuropathic pain (mostly)
  • Effect: Bind L-type Ca channel; no change in Ca conductance
  • Excreted unchanged in urine (no meta); check renal fxn before using
  • SE: fatigue, ataxia
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9
Q

Lamotrigine

A
  • BROAD SPECTRUM AED
  • Mono/Adjunct TX: Partial, Gen TC, Lennox-Gastaut syndrome (LGS)
  • Effect: prolong rate of recovery Na VG (longer inactive); inhibit Ca (lesser effect)
  • 24-35 hr half-life; shorter with carba, pheno, and primidone (15 hr); reduces Valproate by 25%
  • SE: dizzy, ataxia, blurry vision, nausea; rash + SJS with other AEDs
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10
Q

Topiramate

A
  • BROAD SPECTRUM AED
  • Mono/Adjunct TX: Partial, Gen TC, Lennox-Gastaut syndrome (LGS)
  • Effect: inhibit Na and AMPA-kainate rec = enchance GABA
  • excreted unchanged in urine (mostly)
  • SE: ataxia, fatigue, somnolene, wt loss; decrease plasma estradiol/oral contracep conc.
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11
Q

Levetiracetam

A
  • Adjunct TX: partial, Gen TC (adult), mycolinc (kids), Status Epilepticus (IV)
  • Effect: inhibit presynaptic glutamate release
  • excreted unchanged in urine (mostly), no liver induction
  • Highest safety margin
  • rapid dose titration
  • SE: somnolence, dizzy, asthenia, no drug-drug interaction
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12
Q

Ergotamine tartrate

A
  • ACUTE TX MOD->SEV MIGRAINE
  • Ergot alkaloid from fungus (contaiminated Rye)
  • Oral, sublingual, suppository (sub/supp bypass portal circ); Max dose = 6mg/attack; 10mg/wk; HL ~ 2hr
  • Caffeine prolongs vasconstriction (VC) + inc GI abs
  • Liver meta; bile excrete
  • Effect: 5-HT1 stim + direct VC on dilated vessels -> dec pulsations -> dec neuro inflam via dec release of VD/pro inflam neuropeptides BUT also interacts with catecholamines, seratonin, and DA receptors
  • SE: nausea, vomiting, anorexia (CRTZ activation); TX w/ Metoclopramide (anti-emetic)
  • No erythromycin (interferes w/ liver meta of Ergot -> toxicity)
  • Contra: PVD (VC + partial a-adren/5-HT2 agonist); B-block prolong VC, CVD, sepsis, liver/kidney dz, preggo/breast feed
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13
Q

Dihydroergotamine

A
  • ACUTE TX MOD -> SEV MIGRAINE
  • semisynth ergot alkaloid
  • Liver meta, 10% urine excrete, rest in feces (bile)
  • Parenteral admin; incomplete GI absorption (new nasal spray, too)
  • Effects: 5-HT1 stim + direct VC on dilated vessels -> dec pulsations -> dec neuro inflam via dec release of VD/pro inflam neuropeptides BUT also interacts with catecholamines, seratonin, and DA receptors
  • SE: nausea/vomit -> CRTZ stim; transient bradycardia, leg weakness, vasospasm
  • Contra: CVD, sepsis, liver/kidney dz, arterial insuff., preggo/breast feed
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14
Q

Methysergide maleate

A
  • Prophylactic for migraine/cluster; only if other tx fails
  • Semisynth ergot; liver meta to active metabolite (methylergometrine)
  • oral w/ meals (vascular HA)
  • Effect: 5-HT1 agonist, 5-HT2 antagonist; 1-2d to protective blood level of active metabolite
  • SE:
    • Fibrosis: retroperitoneal ->obs urinary tract; pleuropulmonary; cardiac -> vascular shutdown; avoid by stopping drug 4 wks every 6 mo
    • CV: angina via VC/coronary insuff.
    • GI: nausea, vomit, dirrhea, heartburn
    • CNS: drowsy, insomnia, hyperactivity, LSD-like
  • Contra: CVD, fibrotic dz, liver/kidney dz, peptic ulcer, sepsis, preggos, kids
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15
Q

Sumatriptan

A
  • ACUTE TX MOD -> SEV MIGRAINE
  • 1st gen triptan
  • 5-HT derivative
  • SubQ or Oral
  • MAO-A meta, urine excrete
  • Effect: VC of diltated intracranial vessels and inhibit release of VD/proinflamm mediators from CN V; relief for nausea, vomiting, photophobia, phonophobia
  • SE: CV (coronary spasm, MI, vent arrythmias); SubQ -> MI .: not for pt w/ CAD; Not IV -> Vasospasm (or w/ ergot b/c inc vasospasm); injection site rxn; triptan symptoms (chest/throat tightness, difficulty breathing, panic/anxiety, paresthesias, heavy feeling)
  • Contra: MAOIs w/n 2 wks
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16
Q

Zolmitriptan

A
  • 2nd gen triptan
  • Effect: trigeminovascular system (direct VC, inhibit release of VD/proinflamm mediators) and inhibit pain transmission from trigeminal nuc (high lipid solubility)
  • longer half-life than Sumatriptan
  • Contra: use w/ MAOI
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17
Q

Metoclopramide

A
  • DA agonist
  • TX acute migraine unresponsive to sumatriptan, DHE, or oral analgesics
  • relieve HA and anti-emetic
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18
Q

Prochlorperazine

A
  • DA agonist
  • TX acute migraine unresponsive to sumatriptan, DHE, or oral analgesics
  • relieve HA and anti-emetic
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19
Q

Midrin

A
  • TX MILD -> MOD MIGRAINE
  • As effective as oral Ergot., less SEs
  • 2 caps immediately, and 1/hr until no HA (>6/d)
  • Isometheptene -> a/B adren activity (mild VC)
  • dichloralphenazone -> sedative
  • Acetaminophen
  • Contra: glacucoma, renal dz, HTN, heart/liver dz, MAOIs
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20
Q

Propranalol, timolol, atenolol, metropolol, nadolol

A
  • NOT partial agonists
  • Prophylaxis
  • SE:
    • fatigue
    • cold extremities
    • dizzy
    • CNS SE (vivid dreams, nightmares, insomnia, depression)
    • Nadalol/Atenolol - less CNS effects than Propr
  • Contra: asthmatics/DM; VC may enhance effect of ergotamine
21
Q

Amitrptyline

A
  • Effect: downreg centreal 5-HT2 + adrenergic receptors; ind of antidepressant effects
  • Prophylaxis
  • SE
    • Anticholinergic (dry mouth, blurry vision, urine retention, cardiac arrhythmia)
  • Contra: glaucoma, BPH, heart dz
22
Q

Valproate, topiramate, gabapentin

A
  • Prophylaxis (dec frequency by 50% in most pts)
  • Effect: inc GABA transmission, mod glutamate channel activity, and inibiting Na/Ca channels
  • SE: nausea, vomit, weakness, wt gain, tremor, hair loss, hepatic tox (rare)
  • Contra: liver dz, thrombocytopenia
  • Valproic Acid: neural tube defects
  • Topiramate/Gabapentin effective tx
    • Top SE: paresthesia, fatigue, anorexia, diarrhea, wt loss, memory problems, nausea
    • Gaba SE: somnolence, asthenia, dizzy
23
Q

Migraine Triggers

A
  • Weather change
  • Alcohol
  • Chocolate
  • Tyramine (cheese, sour cream, wine, beer, liver, bananas, avocado, chocolate, yogurt, bean pods)
24
Q

Morphine

(Mechanism)

A
  • active moiety: phenyl-N-methyl piperidine
  • antagonist activity: allyl/methylcclopropyl @ p 17
  • acts on limbic system -> mod perception of pain .: pain does not evoke anxiety, fear, panic, or suffering
  • acts on SC/thalamus -> mod physio pain
  • dec sensitivity of noci fields
  • effective against: dull, constant, visceral pain
  • No LoC @ therapeutic dose
  • Agonist on receptors for endorphins/enkephalins/dynorphins -> mod pain processing
  • strong u agonist, mod k agonist, weak d agonist
25
Q

Morphine

(Actions/Effects/SE)

A
  • Analgesia (see mech card)
  • Sedation and mental clouding - “floating/dream-like but normally aroused”; help sleep by pain removal NOT depression
    • OD situation: sedation -> hypnosis/stupor -> coma -> death
  • Relief of anxiety and apprehension
  • Euphoria (usually)/Dysphoria (occasionally; more common in the ladies)
  • Nausea - CRTZ stim but eventual tolerance
  • Respiratory Depression - dec CO2 sens in medulla; major toxic effect -> OD death
    • Partial relief to acute PE -> dec awareness of resp distress; + VD -> dec pre-/afterload
  • Pupil constriction: “pin point” -> OD sign
  • Antitussive effect: medulla
  • Histamine release -> aggre asthma/COPD or cause itching; Tx w/ H1 antagonist (dephenhydramine) or naloxone
  • Dec seizure threshold
  • Endocrine changes: dec sec gonadotropins, corticosteroids, prolactin; mentrual change (women) + impotence (men)
  • SM: incr tone circ sm and dec propulsive movement of long m.
    • dec GI motility (constipation), urine retention, bronchoconstriction, incr biliary pressure (bile duct constrict)
  • CV: ortho hypotension (histamine release); cute VD (histamine release), incr CSF (CO2 incr + cerebral VD)
  • Skeletal M. rigidity -> high dose
  • Immunosupp: chronic usage
26
Q

Morphine

(dose/admin route/interactions)

A
  • SEVERE PAIN
  • IM/IV; oral available but not as effective b/c 1st pass meta; 90% urine excrete in 24h
  • Dose: 10 mg SC/IM or 10-30 mg P.O; higher may be needed
  • Important: infusion/autoinjector; PCA (reduces usage of drug); spinal analgesia
  • 4-6h duration
  • crosses placenta
  • Interactions:
    • additive w/ CNS depressants, MAOIs (hyperpyrexia), abuse w/ amphetamines/cocaine, combo w/ other drugs for enhanced analgesia, antihistamines (enhance analgesic effect -> not used anymore), tricyclics (enhanced analagesic effect)
27
Q

Codeine

A
  • MILD->MOD
  • Oral
  • 1/12 as potent as morphine; 30-60 mg P.O
  • antitussive
  • Codeine weak opioid but when demethylated -> forms morphine -> effects
28
Q

Hydromorphone

A
  • similar to morphine; more potent
  • Trauma, post-op, interchangeable w/ morphine
29
Q

Oxycodone

A
  • MOD->SEV
  • morphine/codeine mix
  • oral
  • OxyContin = sustained release; widely abused; “Hillbilly Heroin”
30
Q

Hydrocodone

A
  • MILD -> MOD
  • similar to codeine/oxycodone
  • Oral combo w/ acetaminophen
  • antitussive
  • widely prescribed
31
Q

Meperidine

A
  • MOD -> SEV
  • synthetic
  • oral/parenteral
  • 1/10 as potent as morphine
  • Used in Obstetrics (doesn’t effect fetus as much)
  • use for acute not chronic (build up of metabolite -> seizures)
  • Rx interaction w/ MAOI/SSRI
32
Q

Heroin

A
  • more potent/more euphoric than morphine; 4-6hr duration
  • abuse
  • injection, snorting, smoking
33
Q

Methadone

A
  • Oral; less 1st pass than morphine
  • Low euphoria, long duration (12-24hr)
  • analgesic (acute), tx opioid addiction (chronic use)
34
Q

Fentanyl

A
  • NOT oral -> 1st pass
  • potent u agonist
  • parenterally (surgery), transdermal (chronic pain), lozenge (breakthrough tx)
  • fentanyl + droperidol -> neuroleptic analgesia (for Dx/minor surgeries)
  • fentanyl + droperidol + NO -> neuroleptic anesthesia
35
Q

Pentazocine

A
  • Mixed
  • k agonist, partial u (antagonist @ high dose)
  • less effective, less sedation/resp dep, less physical dependence
  • more CNS stim (hallucinations)
  • precipitate withdrawl in addicts
  • Pentazocine + nalaxone (NX) reduce IV abuse
36
Q

Butorphanol

A
  • similar to pentazocine, parenterally/intranasally
37
Q

Buprenorphine

A
  • partial u agonist (antagonist @ high dose)
  • very low abuse potential, less analgesic effect
  • dec Rx craving in addicts
  • some contain nalaxone to prevent IV abuse
  • injection, sublingual, intranasally, transdermal
  • “Office based” tx for addiction
38
Q

Tramadol

A
  • MILD->MOD
  • weak u agonist
  • inhibit NE/5-HT reuptake like tricyclics
  • mild SEs (similar to morphine)
  • low abuse/addiction (but still present)
39
Q

Naloxone

A
  • Tx OD; reverse resp dep
  • parenterally (not oral b/c first pass)
  • combo w/ oral narcotics to prevent abuse
  • short action (1-2 hr)
  • precipitate withdrawl
40
Q

Naltrexone

A
  • Oral, long lasting (24hr)
  • “immunize” addicts = no “high”
  • Heptatox risk
  • pt compliance = problem
  • Dec EtOH craving in alcoholics = main use now
41
Q

Methylnaltrexone

A
  • quaternary salt of naltrexone
  • tx/prevent constipation (opioid use)
  • parenterally
  • tx post-op paralytic ileus
42
Q

Alvimopan

A
  • similar to methylnaltrexone but oral efficacy
43
Q

NSAIDs (Indomethacin, Ibuprofen, Ketorolac)

A
  • antiinflammatory
  • can stop gout attack
  • inhibit PG synth
  • SE: GI irritation (inhibits protective mech in stomach -> acid irritation); caution w/ peptic ulcer
    • indomethacin = CNS effects (HA, drowsy, dizzy, confusion)
  • Ketoralac = IM, tx severe/acute attacks
  • avoid use w/ aspirin (biphasic effect on uric acid secr.)
44
Q

Corticosteroids (Prednisone and methylprednisone)

A
  • quick/effective but immunosuppression
45
Q

Colchicine

A
  • antiinflammatory specific for gout; not widely used anymore
  • Oral/IV (acute attack); low/less frequent dose = prevent recurrence
  • binds tubulin -> prevents polymerization -> decr leukocyte migration/phago/mitosis
  • inhibits prodution/release of proinflamm glycoproteins from neutrophils
  • SE: GI (Severe; NVD), OD (severe burning, throat pain, bloody diarrhea and CNS dep.), transient leukopenia, agranulocytosis, aplastic anemia, alpecia, myopathies/neuropathies (chronic use)
46
Q

Allopurinol

A
  • Effect: inhibitxanthine oxidase -> decr uric acid formation (keeps from forming .: facilitates dissolution)
  • reduces gout attack potential (not acute tx)
  • SE: initial incr in gout attacks; elevated liver enzymes, allergic rxn (skin)
  • Drug interactions: incr half-life/effect of probenecid; inhib hepatic meta of some drugs; incr half-life theophyline
  • Surgery -> cell lysis -> purine release -> gout attack (tx w/ allo)
47
Q

Febuxostat

A
  • xanthine oxidase inhibitor
  • SE: less skin problems/allergic rxns; elevated liver enzymes
  • high cost
  • beneficial if allopurinol failure
48
Q

Probenecid

A
  • Oral (2-4hr; elim 5-8hr)
  • Chronic NOT acute tx
  • Effect: inhibits secretion/reabsorption of organic acids -> net effect = uric acid excretion
  • SE: GI upset (caution w/ peptic ulcer); skin rash, OD CNS effects (seizure/death), incr kidney stone effect
  • Contra: gouty nephropathy
  • Rx interactions: salicylates, inhib rx excretion (penicillin, methotrexate, NSAIDS, rifampin in bile)
49
Q

Acetaminophen

A
  • inhibit PG @ CNS not PNS
  • NO antiinflamm
  • NO GI SEs
  • SE: hepatotox @ high dose

Pharmacology (3 decks)

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