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GER MS2 Unit 3 > Pharm > Flashcards

Pharm Flashcards

1
Q

Levodopa (L-DOPA) (Dopar)

A
  • class: dopamine precursor
  • crosses BBB→DA; improves nigrostriatal functioning
  • +carbidopa= first-line treatment for Parkinson’s (unless patient is young; delay use as long as possible)
  • side effects: dyskinesias; hypotension, nausea, anxiety, fatigue; psychoses if dosed too high
  • MAO-A inhibitors contraindicated (MAO-Bonly hits DA)
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2
Q

Carbidopa (Lodosyn)

A
  • class: aromatic AA decarboxylase inhibitor
  • inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
    • given with Levadopa to lower side effects
  • treats parkinson’s
  • side effects: dyskinesias, on-off phenomenon
  • MAO-A inhibitors contraindicated (MAO-B only hits DA)
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3
Q

Buproprion (Wellbutrin)

A
  • class: norepi-dopamine reuptake inhibitor (NDRI)
  • blocks DAT→ increased DA synthesis
  • treats: parkinson’s, SAD, good for patients with addictive behavior (maintain nicotine abstinence in quitting smokers);
  • side effects due to increased NE: insomnia, anxiety, agitation, nausea, dry mouth, sweating, palpitations; mild increase in BP
  • less pronounced DA side effects because it’s less aggressive in CNS and not 100% agonist
  • lowers seizure threshold
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4
Q

Modafinil

Armodafinil

A
  • class: stimulants
  • increases histamine activity in tuberomammilary nucleus; may block DAT
  • wake promoting; treats narcolepsy, apnea
  • side effects: similar to but less severe than amphetamines; less addictive than the phetamines
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5
Q

Selegiline (Eldepryl)

Rasagiline (Azilect)

A
  • class: MAO-B inhibitor (more relevant for DA)
  • prevents breakdown of DA
  • treats: early Parkinson’s
  • side effects: hypotension (due to NE→ a1), dizziness, insomnia, weight gain; N/V
  • selegiline: patch for depression too (EMSAM)
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6
Q

Tranylcypromine (Parnate)

Isocarboxazid (Marplan)

Phenelzine (Nardil)

A
  • class: MAOI
  • irreversibly inhibits MAO-A and MAO-B
  • treats depression
  • side effects: hypotension, dizziness, insomnia, weight gain
  • HTN crisis with tyramine rich foods
  • serotonin syndrome (MAOI + SSRI)
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7
Q

Entacapone (Comtan)

Tolcapone (Tasmar)

A
  • class: COMT inhibitor
  • prevents breakdown of DA
  • treats parkinson’s (good add on for other drugs)
  • side effects: nausea, fatigue; dopamine side effects
  • entacapone: short acting (2 hours)
  • tolcapone: use only if entacapone fails, risk of liver failure
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8
Q

Bromocriptine (Parlodel)

Pramipexole (Mirapex)

Ropinerole (Requip)

Apomorphine (Apokyn)

A
  • class: D2 receptor agonist
  • increases DA activity (phasic)
  • treats: mild/early parkinson’s, restless leg syndrome
  • side effects: mania, nausea, dizziness, fatigue; peripheral DA-like effects
  • less effective with motor symptoms of PD
  • bromocriptine: treats hyperprolactinemia; must be titrated slowly due to hypotension
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9
Q

Aripiprazole (Abilify)

A
  • class: D2 & D3 receptor (partial) agonist
  • increases DA activity (tonic)
  • treats: schizophrenia; depression
  • side effects: less side effects than other DA
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10
Q

Amantadine (Symmetrel)

A
  • class: antiviral
  • ? stimulates D2 receptors, blocks DAT; leads to DA release from terminal vesicles
  • treats: mild parkinson’s (2nd-line; not used much); influenza
  • side effects: nausea, dizziness, psychosis, insomnia, seizures
  • contraindicated in elderly with dementia (anticholinergic effects)
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11
Q

Reserpine

Tetrabenazine

A
  • class: synapse depleter
  • blocks VMAT (no release of monoamines into synapses)
  • reserpine: treats HTN
  • tetrabenazine: treats huntington’s
  • side effects: depression (lowers NA and DA)
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12
Q

Benztropine (Cogentin)

Trihexiphenidyl (Artane)

Diphenhydramine

A
  • benztropine, trihexiphenidyl: anticholinergics; contraindicated in parkinson’s dementia; abrupt discontinuation exacerbates symptoms
  • diphenhydramine: antihistamine
  • muscarinic receptor antagonist (inhibiting cholinergic tone in basal ganglia improves DA tone in nigrostriatal pathway)
  • treats: early parkinson’s, reduces EPS
  • side effects: dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations
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13
Q

First-generation antipsychotics (Low Potency)

A
  • Chlorpromazine, thioridazine
  • non-selective D2 receptor antagonism (also H1, anticholinergic, and a1 antagonism)
  • treats psychosis (schizophrenia)
  • side effects: EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism)
  • tardive dyskinesia with chronic use
  • little effect on negative symptoms
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14
Q

First-generation antipsychotics (High Potency)

A
  • Fluphenazine, thiothixine, haloperidol
  • non-selective D2 receptor antagonism
  • treats: psychosis (schizophrenia); movement disorder in Huntingtons
  • side effects: EPS; NMS (skeletal muscles microcontract→hyperthermia, muscle rigidity)
  • tardive dyskinesia with chronic use
  • little effect on negative symptoms
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15
Q

Second-Generation Antipsychotic (Low potency)

A
  • ‘pines: olanzapine, quetiapine, asenapine
  • D2 receptor antagonist, 5HT2a receptor antagonist
    • less EPS but more sedating
  • treats: psychosis, mania, agression
  • side effects: suicide risk in ages <25; metabolic syndrome; TD/EPS; stroke in dementia patients
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16
Q

Clozapine (Clozaril)

A
  • class: second generation antipsychotic (low potency)
  • D2 (& D1, D4) receptor antagonist; 5HT2a receptor antagonist
  • treats refractory shizophrenia (use if all else fails)
  • side effects: similar to other “pines”; agranulocytosis, most metabolic risk of all antipsychotics, but little EPS/TD; must monitor WBC
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17
Q

Second-Generation Antipsychotics (High Potency)

A
  • ‘dones: risperidone, ziprazidone, paliperidone, iloperidone, lurasidone
  • D2 receptor antagonist; but various other receptor agonism/antagonism
    • higher potency, more EPS
  • treats: psychosis, mania, agression
  • side effects: suicide risk in ages <25; metabolic syndrome; TD/EPS; stroke in dementia patient, fewer metabolic complications than ‘pines
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18
Q

Pilocarpine HCl (Salagen)

A
  • class: direct muscarinic agonist
  • pupillary constriction, increased aqueous outflow
  • treats: glaucoma (open angle and acute closed angle); cataract surgery
  • used infrequently due to side effects (decreased vision when patient has cataracts due to miosis, headache; SLUDGE)
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19
Q

AChEI

A
  • Edrophonium: short-acting, fast onset; used to diagnose myasthenia gravis
  • Echothiophate: irreversible, long acting; treats glaucoma
  • Neostigmine: MC used for reversal of NMB; more complete antagonism than edrophonium
  • Pyridostigmine: Longer acting than neostigmine, edrophonium
  • side effects: SLUDGE
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20
Q

Atropine

Scopolamine

A
  • class: antimuscarinic
  • pupillary dilatation; paralysis of ciliary body
  • treats: improve discomfort during active eye inflammation (ueveitis)
  • side effects: ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention
  • atropine: v. long acting so not used unless inflammation is severe
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21
Q

Tropicamide (Mydriacyl)

A
  • class: antimuscarinic
  • pupillary dilatation; paralysis of ciliary body
  • treats: MC used cycloplegia for eye exams
  • side effects: ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention
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22
Q

Epinephrine (Epinal)

A
  • class: direct adrenergic agonist
  • dilation of episcleral vessels→ increased aqueous outflow and a1 pupillary dilation
  • side effects: extrasystoles, palpitation, hypertension, myocardial infarction, trembling, paleness, sweating
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23
Q

Hydroxyamphetamine (Paredrine)

A
  • class: indirect adrenergic agonist
  • mechanism: release NE
  • separates 1st and 2nd from 3rd order neuron dysfunction in Horner’s syndrome (positive dilation means 1st or 2nd order)
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24
Q

Cocaine

A
  • class: indirect adrenergic agonist
  • blocks reuptake of DA, NE, 5HT
  • use to confirm diagnosis of Horner’s
  • topical anesthetic, combined vasoconstrictor and local anesthetic
  • side effects: sympathetic effects; paranoia, aggression
  • rapidly hydrolyzed by plasma cholinesterase
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25
Q

Phenylephrine (Neo-Synephrine)

A
  • class: direct α1-agonist
  • dilate pupil for eye exam and cataract surgery
  • side effects: extrasystoles, palpitation, HTN, myocardial infarction, trembling, paleness, sweating
  • caution in elderly patients: at 10% can cause cardiac side effects
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26
Q

Brimondine tartrate (Alphagan)

A
  • class: direct α2-agonist
  • suppresses aqueous humor production through cAMP in non-pigmented ciliary epithelium
  • primary agent for treatment of glaucoma
  • side effects: may cause follicular conjunctivitis; use with MAOi can cause fatigue/drowsiness
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27
Q

β-blockers used for treatment of glaucoma

A
  • Timolol: β-blocker; contraindicated in CHF, asthma
  • Levobunolol: β2-blocker
  • Betaxolol: β1-blocker; few side effects
  • mechanism: reduce intraocular pressure by reducing aqueous production at ciliary process
  • 2nd line treatment of glaucoma
  • side effects: bradycardia, hypotension, syncope, CHF, bronchospasm, sexual dysfunction, hyperkalemia
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28
Q

Nifedipine (Procardia)

A
  • class: Ca-channel blocker
  • mechanism: increases ocular perfusion at nervehead
  • treat low-tension glaucoma
  • not widely used
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29
Q

carbonic anhydrase inhibitors

A
  • interferes with active transport of Na through Na-K-ATPase pump→reduced aqueous production
  • dorzolamide, brinzolamide: 2nd line glaucoma therapy
    • side effects: red eyes, lid allergies
  • acetazolamide: oral agent for advanced glaucoma and with cataract surgery (only if topical therapy fails)
    • side effects: paresthesia, fatigue, drowsiness, depression, diarrhea, met. acidosis, electrolyte changes
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30
Q

MAOIs

A
  • tranylcypromine, phenelzine
  • irreversibly inhibit MAOa,b
  • treats: depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
  • important side effects: agitation (rare), delerium→ seizures; HTN crisis with tyramine-rich foods; serotonin syndrome (MAOI + SSRI)
  • other side effects: anticholinergic, orthostatic hypotension, sexual dysfunction, weight gain, sedation
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31
Q

Tricyclics

A
  • Desipramine
  • Imipramine: active metabolite desipramine
  • Amitriptyline (Elavil): active metabolite nortriptyline; high side effects
  • Nortriptyline
  • block reuptake of NE or 5-HT at varying potencies/ selectivity; also variably block muscarinic, a-adrenergic, DA, and histamine receptors
  • treats: depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
  • not very safe; rarely used
  • side effects: sympathomimetic (cardiac arrhythmias and conduction defects, especially at OD), antimuscarinic, orthostatic hypotension, sedation (additive with alcohol), seizures
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32
Q

SSRIs

A
  • Fluoxetine (Prozac): model drug; potent P450 inhibitor
  • Paroxetine: more selective for 5HT than fluoxetine; potent P450 inhibitor
  • Sertraline, escitalopram, citalopram
  • mechanism: inhibit reuptake of 5-HT (and NE to lesser extent)
  • treats: depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; pre-menstrual dystrophic disorder
  • fewer side effects than tricylics, mostly nausea, decreased sexual function
  • Serotonin syndrome (with MAOIs)
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33
Q

SNRIs

A
  • Duloxetine (Cymbalta)
  • Venlafaxine (Effexor): low risk of side effects
  • mechanism: inhibits reuptake of 5-HT and NE
  • treats: depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
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34
Q

Mirtazapine

A
  • 5HT2a antagonist; also inhibit 5HT reuptake
  • treats: depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
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35
Q

Lithium

A
  • mechanism unknown; Li depletes 2nd messengers IP3 and DAG, important in a-adrenergic and muscarinic-cholinergic transmission
  • treats: anti-manic/mood-stabilizing (bipolar); LT cluster headache prevention
  • side effects: drowsiness, weight gain, tremor, polydipsia, polyuria; high levels→neurotoxicity, cardiac toxicity, renal dysfunction
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36
Q

Nalmefene (Revex)

A
  • class: opiod antagonist
  • may produce a prolonged withdrawal state (N/V, piloerection, yawning)
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37
Q

N-acetylcysteine (Mucomyst)

A
  • class: antioxidant
  • mechanism: supplies sulfhydryl groups to glutathione; improves microcirculation, anti-inflammatory effect
  • treats: acetaminophen overdose
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38
Q

Fomepizole (Antizol)

A
  • mechanism: blocks alcohol dehydrogenase
  • treats: methanol & ethylene glycol poisoning
  • $$$$
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39
Q

Schedule I Hallucinogens

A
  • 5HT2A receptor agonist on Raphe cell body→ inhibition of Raphe Nuclei firing→ increased sensory input; partial dopamine agonist
  • LSD: model hallucinogen; limited studies in psychoanalysis, alcoholism, autistic children, and terminal cancer patients; oxidized in liver
    • bad trips (anxiety and panic attacks), flashbacks; no overdoses, birth defects, or chronic psychoses linked to LSD
  • Mescaline
  • Psilocybin
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40
Q

Phencyclidine (PCP)

A
  • class: dissociative anesthetic
  • mechanism: antagonist of ion channel associated with NDMA receptor; agonist at mu opioid receptors
  • side effects: 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
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41
Q

Amphetamines (Benzadrine)

Dextroamphetamine (Dexedrine)

Methamphetamine (Desoxyn)

Methylphenidate (Ritalin)

A
  • class: stimulants
  • mechanism: Blocks DAT, also increases VMAT2 (indirect sympathomimetic→ release biologic amines from nerve terminals in periphery and in CNS, esp. dopamine most important)
  • treats: narcolepsy, ADHD
  • side effects: vasospasm leading to possible stroke or MI, arrhythmia, weight loss (anorectic effect); tremor, anxiety, irritability, confusion, possible paranoia
42
Q

THC

A
  • mechanism: hits cannabinoid receptors (CB1, CB2: GPCRs)
  • Marijuana: cannabinoid, schedule I drug; antiemetic, antinausea, appetite stimulate for chemotherapy and AIDS; analgesic for neuropathic pain
    • potential use for glaucoma, asthma, anxiolytic, migraine, and MS
    • side effects: 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-THC (metabolized by P450); highly lipid soluble
  • Anandamide: endogenous cannabinoid
  • Dronabinol: synthetic THC; schedule III drug; antiemetic, antinausea, appetite stimulate for chemotherapy and AIDS patients
  • Nabilone: synthetic THC; schedule II drug; treatment-resistant N/V weight loss and anorexia in AIDS patients; less psychoactive side effects than marijuana
43
Q

Morphine

A
  • class: opioid; mu-opioid receptor agonist
  • treats: severe analgesia (step 3)
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V, 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
44
Q

Codeine

A
  • class: opioid; mu-opioid receptor agonist (low receptor affinity)
    • CYP2D6 polymorphisms: 10% of caucasians can’t convert to morphine (can still experience side effects)
  • treats: moderate analgesia (step 2), antitussive
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V
45
Q

Tramadol (Ultram)

A
  • class: opioid; mu-opioid receptor agonist (weak); some NE/5HT uptake inhibition (leading to analgesia)
  • treats: moderate analgesia (step 2)
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V
46
Q

Fentanyl (Duragesic)

A
  • class: opioid; mu-opioid receptor agonist (strong); highly lipid-soluble
  • treats: severe analgesia (step 3) after identification of dose level via other opiod (e.g., morphine)
    • IV, transdermal; do not change dose more than 1/week (long half-life); intraspinal administration possible
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V
47
Q

opioids

A
  • Codeine: step 2
  • Tramadol: step 2
  • Oxycodone: step 3 (+acetominophen=2)Morphine: step 3
  • Fentanyl: step 3
  • Methadone: step 3
  • Diphenoxylate
  • Loperamide
48
Q

Methadone (Methadose)

A
  • class: opioid
  • mu-opioid receptor agonist
  • treats: chronic, severe pain; treatment of heroin and opiod addicts
    • 90% bound to plasma protein, accumulates in tissues (extended duration of action); do not change dose more than 1/week (long half-life)
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
49
Q

Oxycodone

A
  • class: opioid
  • mu-opioid receptor agonist
  • treats: moderate to severe analgesia
    • oxycontin is extended release
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
50
Q

Loperamide (Imodium)

Diphenoxylate (Lomotil)

A
  • class: opioid
  • slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
  • treats diarrhea
  • side effects: miosis, constipation, respiratory depression; dry mouth, N/V sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
51
Q

Naloxone (Narcan)

A
  • class: opioid antagonist
  • competitive mu-, delta-, and kappa-opioid receptor antagonist
  • treats acute opioid toxicity (depressed RR best predicts reponse)
  • side effects: can precipitate withdrawal (flu-like symptoms of N/V/D, piloerection, yawning, irritability)
  • continuous parenteral infusion, as lasts only 15-30 minutes (oral almost completely metabolized by liver)
52
Q

Naltrexone (Revia)

A
  • class: opioid antagonist
  • mu-opioid receptor antagonist
  • treats alcoholism
  • may produce a prolonged withdrawal state (N/V, piloerection, yawning)
53
Q

Benzodiazepines

A
  • GABAa agonist; binds between a1 and y2 subunits;“ceiling effect” due to augmenting action of GABA
  • P450 metabolism
  • treats: depression (short-term); maintenance of bipolar; severe bipolar
  • side effects: daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)
  • Diazepam: muscle relaxant
  • Chlordiazepoxide
  • Flurazepam: longest t1/2
  • Lorazepam: prevent withdrawal symptoms in alcoholics, anticonvulsant, anxiety
  • Alprazolam: sedation, anxiety
  • Midazolam: anesthesia (calming effects, anterograde amnesia)
  • Triazolam: induces sleep
54
Q

Zolpidem (Ambien)

A
  • class: non-benzodiazepine receptor agonist
  • BDZ-1 selective agonist
  • sedation and hypnosis without muscle relaxation or anticonvulsant activity (unlike the other benzos)
  • side effects: sleep-walking, next morning impairment
55
Q

Flumazenil (Romazicon)

A
  • class: competitive nonselective benzodiazepine antagonist
  • treats benzodiazapine overdose
  • side effects: withdrawal (may be life-threatening); seizures in mixed overdoses; non uniform in reversal of respiratory depression
56
Q

Barbiturates

A
  • GABAa agonist (binds a or b subunit)
  • Thiopental: highly lipid soluble, fast-on, fast-off (redistribute from brain to muscle and fat, metabolized by liver; dosed based on lean body mass); induces anesthesia
  • Methohexital: also antagonist of NMDA-glutamate receptor; induce general anesthesia (produce hypnosis & sedation, but is antianalgesic)
  • Phenobarbitol: antiepileptic, anticonvulsant
  • side effects: daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
  • abrupt withdrawal life-threatening
57
Q

Buspirone (Buspar)

A
  • may be partial agonist at 5HT1A, no GABAa interaction
  • anxiolytic without marked sedation
58
Q

Nitrous Oxide

A
  • class: inorganic gas
  • NMDA receptor antagonist
  • mask induction in children; adjuvant to volatile anesthetics, opioids
    • no muscle relaxation
    • v. insoluble/ works fast (don’t need much to create equilibrium)
  • side effects: postop N/V; inactivates B12 (abnormal embryonic development, abortion); accumulates in closed, air-containing spaces (bowel, middle ear, pneumothoraces, air emboli) because N2O insoluble in blood
59
Q

Volatile Anesthetics

A
  • Isoflurane: most potent; gold standard for maintenance; pungent; can increase HR, resistant to metabolism
  • Desflurane: least soluble, least potent (allows for rapid emergence from anesthesia); maintenance of anesthesia; most pungent (airway irritation)
  • Sevoflurane: 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
  • side effects: dose dependent CNS depression, increase in cerebral blood flow and ICP, decrease in BP, decrease in respiratory function; relaxes skeletal muscle; increase in HR; malignant hyperthermia
60
Q

Propofol

A
  • class: Alkylphenol (atty acid)
  • GABAa receptor agonist, antagonist of NMDA-glutamate receptor; some a2 receptor activity; rapid onset and offset
  • antiemetic at low doses; induction and maintenance of general anesthesia; sedation in ICU, procedural sedation; no malignant hyperthermia
  • Propofol infusion syndrome: use for several days→ met. acidosis, rhabdo, heart & renal failure, lowering of BP, bradycardia, and death
  • side effects: painful injection site (administer in lipid emulsion); supports bacterial growth
61
Q

Etomidate (Amidate)

A
  • class: carboxylated imidazole
  • GABAa receptor agonist (only D-isomer)
  • used for hypnosis; no analgesic activity; minimal cardiorespiratory depression (good for patients with minimal cardiac reserve)
  • side effects: pain on administration (due to solvent, propylene glycol); involuntary myoclonic movements due to subcortical disinhibition (not seizure); postop N/V; single dose inhibits cortisol synthesis
62
Q

Ketamine (Ketalar)

A
  • class: phencyclidine
  • NMDA receptor antagonist, kappa opiate agonist; leads to dose-dependent unconsciousness, amnesia, analgesia
    • ​dissociative (intact CN signs)
  • use for: sedative/anesthetic for: peds/delayed patients, induction in reactive airway disease (bronchodilates), hypovolemia (increases HR and systemic vascular resistance), cardiac disease; + propofol procedural sedation; adjuvant during/after surgery to reduce opiod use; part of multimodal pain therapy regimen; depression treatment
  • side effects: stimulates symp outflow; increases cerebral blood flow (ICP); emergence delerium;
  • metabolized by P450 (norketamine, less effective); contraindicated in CAD and those with intracranial lesions
63
Q

Dexmedetomidine (Precedex)

A
  • class: a2 adrenergic agonist
  • binds a2a and a2b in locus coeruleus and spinal cord (sedation, sympatholysis, and analgesia)
    • GABA not hit (easier to wake; similar to non-REM sleep); FDA approved only for ventilation of ICU patients for <24 hrs
  • awake intubations and craniotomies; adjunct to general anesthesia in patients susceptible to narcotic-induced post-op respiratory depression; withdrawal/ detox
  • limited respiratory depression (wide safety margin)
64
Q

Succinylcholine (Anectine)

A
  • class: depolarizing NMB
  • divalent ACh molecule; attaches and overstimulates all ACh receptors (fasiculations→ paralysis)
  • used as a skeletal muscle relaxant (intubation)
  • side effects: 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
65
Q

non-depolarizing NMBs

A
  • competitive blockade of ACh (no depolarization)
  • skeletal muscle relaxant, reverse with AChEI
  • Pancuronium: vagolytic, avoid in patients with renal insufficiency; can increase HR; long acting, low liver metabolism
  • Vecuronium: no cardiovascular effects; hepatic and renal excretion
  • Rocuronium: can substitute succinylcholine in rapid sequence intubation, no cardiovascular effects; hepatic and renal excretion
  • Atracurium: use in patients with liver/renal dysfunction; leads to histamine release→ hypotension and tachycardia
  • Cis-atracurium: use in patients with liver/renal dysfunction; no histamine release; nonenzymatic degradation (hofman elimination)
66
Q

Sugammadex (Bridion)

A
  • class: selective relaxant binding agent
  • complexes with rocuronium, rendering it inactive; no effect on AChE
  • not yet FDA approved
  • side effects: decrease in BP, N/V, dry mouth
67
Q

Glycopyrrolate (Robinul)

A
  • class: anti-muscarinic
  • used for reversal of neuromuscular blockade’s muscaranic effects
  • side effects: DUMBELLS
68
Q

Ester anesthetics

A
  • used as local anesthesia, hydrolyzed by pseydocholinesterase (rapid)
  • reversibly inactivates intracellular portion of voltage-gated Na channel; blocks nociceptive nerve impulses
  • local side effects: transient neurologic symptoms (really bad pain), neuronal injury
  • Cocaine: many side effects due to action as a CNS stimulant
  • Benzocaine: risk of methemoglobinemia
  • Procaine
  • Tetracaine
  • Chlorprocaine: high pKa (not as potent)
  • systemic side effects (MC with long-acting 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
69
Q

Amide anesthetics

A
  • Lidocaine
  • Mepivacaine
  • Bupivacaine: highest cardiac toxicity potential
  • Ropivacaine: less potent than others (larger TI)
  • used as local anesthesia; transformed by hepatic carboxyl esterases and CYP450s (slow)
  • mechanism: reversibly inactivates intracellular portion of voltage-gated Na channel; blocks nociceptive nerve impulses; effects more rapidly firing neurons vs. resting neurons, smaller more myelinated nerves are blocked faster
  • local side effects: transient neurologic symptoms (really bad pain), neuronal injury
  • systemic side effects (MC with long-acting 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 (block Na channels in heart and increase myocardial contractility and vasodilation)
70
Q

IFN-betas for MS

A
  • inhibit T cell activation, shift reponse from Th1 to Th2; inhibit lymphocyte movement into CNS
  • treats RRMS; decrease acute attacks by 1/3 and significantly reduces new and enhacing MRI lesions
    • does not cross BBB (treats peripherally)
  • side effects: anemia, leukopenia, increase LFTs and hypothyroidism (monitor every 3 mo.); injection site reactions
  • IFN-beta-1a: available in low and high doses (high dose is 1st line; better than other IFNs and glatiramer acetate)
  • IFN-beta-1b: high dose, more efficacious than low dose IFN beta 1a
71
Q

Glatiramer acetate (Copaxone)

A
  • class: myelin basic protein analog
  • causes T-cell apoptosis (looks like MBP), induces anti-inflammatory Th2 cells (cytokine shift from Th1), induces Treg with induction of anergy
  • treats RRMS
  • active in CNS (decreases brain atrophy; no organ damage); try to use early; reduce relapse by 1/3, modest reduction in MRI lesion and reduction of atrophy, but no effect on disease progression
  • side effects: injection site rxn, anxiety attack-like reaction
72
Q

Natalizumab (Tysabri)

A
  • class: monoclonal antibody
  • binds VLA4 (integrin subunit), inhibiting leukocyte migration across BBB
  • treats: 2nd line therapy for RRMS (relapse reduction by 2/3)
    • most efficacious treatment for MS, 2nd line because it is also the most problematic
  • side effects: PML (JC virus); acute urticaria, systemic HSN infusion rxn; headache, dizziness, fatigue, arthralgia, rigors
73
Q

Fingolimod (Gilenya)

A
  • class: sphingosine-1-phosphate analog
  • prodrug; sequesters lymphocytes in secondary lymph organs via induction of intracellular internalization of receptors on lymphocytes (no effect on lymphocyte induction, proliferation, or memory function)
  • treats RRMS; better than low dose IFN
  • side effects: bradycardia and heartblock; macular edema, reduced FEV1, increased LFTs, lymphopenia, leukopenia, infections
  • Patients must be VZV immune before prescription
74
Q

Teriflunomide (Aubagio)

A
  • class: immunosuppressants
  • reduces T and B proliferation and function against autoantigens; preserves replication and function of cells living on salvage pathway (e.g., hematopoietic cells, memory cells)
  • treats RRMS; as good as IFNs but oral dosing
  • black box warnings: hepatotoxicity; teratogenicity (animal data)
75
Q

Dimethyl fumarate (Tecfidera)

A
  • neuroprotective (enhances Nrf2 pathway; some Th1→ Th2 shift)
  • treats RRMS; comparible to fingolimod (better than low dose IFN)
  • side effects: N/V/D, stomach pain, flushing, itching redness, rash
76
Q

Mitoxantrone (Novantrone)

A
  • class: anthracenedione
  • broad immune suppression and modulation of B cells, T cells and macrophages;
  • treats: SPMS, RRMS (2nd line); decreases frequency of clinical relapse, reduces disease progress, and reduces disability
  • side effects: dose-dependent cardiac toxicity (decreased LVEF, irreversible CHF); leukemia
77
Q

immunosuppressants for SPMS

A
  • treats SPMS (resistant, or as combination with other therapies)
  • side effects: systemic toxicity (monitor blood for changes)
  • Azathioprine
  • Methotrexate
  • Cyclophosphamide
  • Mycophenolate mofetil
78
Q

meds for acute MS attacks

A
  • 1st line= methylprednisone: corticosteroid (immunosuppressant)
    • short-term: insomnia, mood changes, fluid retention, epigastric pain, HTN
    • long-term: osteoporosis, cushingoid, secondary malignancies
  • 2nd line= plasmaphoresis
  • 3rd line= ACTH if patient is allergic to corticoseroids, poor IV access, MTP doesn’t work
79
Q

Voltage-gated Na channel stabilizer

A
  • stabilize inactive conformation of Na channel (nerve can still work but not repeatedly and v. fast)
  • side effects: rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs; can cause contraceptive failure
  • toxicity: dizzy drunk double vision
  • Phenytoin: less effective for absence (esp pediatric), myoclonic, atonic seizures; teratogen; gingival hyperplasia, hirsutism, lupus-like reaction
  • Carbamazepine: more effective for complex partial seizure than primary generalized; bipolar disorder; neuropathic pain; hepatic enzyme inducer (auto and hetero) so much increase dose
  • Oxcarbamazepine: more effective for complex partial seizure than primary generalized; bipolar disorder; neuropathic pain; fewer interactions/ less toxic than carba
  • Lamotrigine: primary generalized epilepsies, absence seizures; indicated in children; bipolar disorder; neuropathic pain; competes with valproate for excretion (synergism)
80
Q

Valproate (Depakote)

A
  • likely affects Na-gated channels and GABA system
  • treats: broad spectrum seizure treatment but not absence; IV for status epilepticus; bipolar treatment, migraine and long-term cluster headache prophylaxis
  • side effects: weight gain, hair loss, hyperammonemia (can be mitigated with oral carnitine), teratogenicity, blood dyscrasias; pancreatitis
81
Q

GABAergic anti-epileptics

A
  • vigabatrin: GABA transaminase binder (slows down intracellular breakdown of GABA); works on GABA-A
  • tigabine: GABA reuptake inhibitor; works on GABA-A
  • benzodiazapines: binds GABA-A in post synaptic membrane of inhibitory synapse); treasts status epilepticus; anesthesia
    • LT usefulness limited by tolerance
82
Q

Gabapentin

Pregabalin

A
  • class: GABA analog
  • block presynaptic influx of Ca
  • adjunct for partial complex epilepsy; more commonly used for neuropathic pain
  • gabapentin: v. safe (no metabolism or drug interaction so few side effects)
83
Q

Topiramate

A
  • class: glutamate receptor blockers
  • partial AMPA, Kainate Ca receptor blocker; 2ndary effect on voltage-gated Na and GABA system
  • treats partial onset seizures, 2ndary generalized seizures, generalized epilepsy, migraine and LT cluster headache prevention
  • side effects: mild met. acidosis→ resp. comp.→ mild alk→ Ca ionization→ tingling; kidney stones; weight loss; word-finding problems; acute angle-closure glaucoma
84
Q

Felbamate

A
  • class: glutamate receptor blocker
  • NMDA receptor blocker; 2ndary effect at voltage-gated Na and Ca, GABA system
  • treats: partial onset seizures w/or w/out 2nd generalization, medically refractory epilepsy
  • side effects: uncommon but potentially fatal (aplastic anemia, acute hepatic failure); requires monitoring
85
Q

Levetiracetam

A
  • class: synaptic vesicle binder
  • binds synaptic vesicle protein 2→ less NT release
  • treats: partial onset seizures, 2ndary generalized seizures
  • side effects: irritability
86
Q

Ethosuximide

A
  • class: voltage-gated Ca channel blocker
  • blocks T-type Ca channels in thalamocortical circuits
  • treats: absence seizures only; neuropathic pain
  • side effects: nausea, irritability
  • readly absorbed, minimal 1st pass metabolism
87
Q

Butalbital

A
  • class: barbiturate
  • acute treatment of migraines; use when more traditional therapies unavailable or contraindicted (no RCT show efficacy)
  • side effects: drowsiness, dizziness; risk of overuse and withdrawal)
  • use limited to 2-3x /week
88
Q

opioids for headache treatment

A
  • acute treatment of migraines, patients with infrequent headaches; generally for patients who wake up with a headache
  • side effects: drowsiness, constipatient
  • physical dependence w/chronic use (rebound headaches); use <3x/week
  • pregnant women may use codeine or meperidine with caution
89
Q

corticosteroids for headache treatment

A

used for acute treatment of migraines, prolonged headache syndromes; rescue treatment of cluster headache; avoid chronic use

90
Q

ergot alkaloids for headache treatment

A
  • ergotamine, DHE
  • vasoconstriction possible; act as 5HT agonist in trigem vascular pathway
  • contraindicated in: women planning pregnancy, uncontrolled HTN, sepsis, renal or hepatic failure, vascular disease
91
Q

triptans for headache treatment

A
  • selective 5HT1 b-d agonists (blocks peptide release); penetrate CNS, constriction of extracerebral intracranial vessels, inhibition of trigem vascular system
  • used for acute treatment of migraines (premier option); photo/phonophobia, N/V, acute treatment of cluster headaches (subQ)
  • side effects: flushing, tingling, noncardiac chest discomfort
  • contraindicated in: vascular disease, inctrolled HTN, complicated migraine
92
Q

onabotulinum toxin A

A
  • prevention of migraines; unknown mechanism (possibly decreased afferent stimulation of trigem. vascular system or downreg of sensory and parasymp receptors)
  • injection site pain (specific injection site protocol is FDA approved)
93
Q

TCAs for headache treatment

A
  • used for migraine and tension headache prevention
  • side effects: dry mouth, constipation, weight gain, cardiac toxicity, orthostatis hypotension
94
Q

SSRIs for headache treatment

A
  • migraine and tension headache prevention; treatment for coexisting depression and chronic daily headache
  • side effects: weight gain, sexual dysfunction, headache
95
Q

ß-blockers for headache treatment

A
  • only propranolol and timolol are FDA approved for migraine prevention
    • nadolol and atenolol sometimes preferred for long half-life and tolerability
  • side effects: drowsiness, dpression, decreased libido, hypotension, memory disturbance
  • contrindicated in asthma, diabetes, CHF, or Raynaud’s
96
Q

verapamil

A
  • Ca channel blocker for migraine prevetion (esp. in prolongued/disabling aura or complicated migraine); LT prevention of cluster headaches
  • side effects: constipation dizziness
97
Q

Dextroamphetamine

Lisdexamfetamine

A
  • class: stimulant
  • mechanism: blocks DAT (may actuall reverse it); increases VMAT2
  • treats: ADHD
  • side effects due to NE and DA; addictive
98
Q

prostaglandin analogs

A
  • latanoprast, travorprost, bimatoprost, unoprostone isopryl (least effective)
  • increase uveoscleral outflow (no effect on aqueous or trabecular flow)
  • primary agent for glaucoma
  • side effects: eyelash grow, iris color change, may cause cystoid macular edema in cataract surgery and activate herpes
99
Q

AChE inhibitors for Alzheimer’s Disease

A
  • tacrine: AChE and BuChE inhibition; can raise transaminase
  • donepezil: mild-severe AD
  • rivastigmine: not metabolized by P450 (hydrolyzed by cholinesterases)
  • galantamine: AChE inhibition, allosteric modulator of N receptors
  • side effects: N/V, sleep disturbance
100
Q

Memantine

A
  • partial antagonist of NMDA receptor
  • used for severe AD
  • side effects: dizziness, confusion, headache, constipation
  • excreted unchanged in urine

GER MS2 Unit 3 (4 decks)

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