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Neuro > Drugs > Flashcards

Drugs Flashcards

1
Q

Morphine

A
  • subQ, im, oral
  • MOA: binds to plasma proteins, rapidly goes to highly perfused tissues, acts on MOP
  • metabolized to M3G (exerts excit. effects on GABA) and M6G (4-6x potency) - can accumulate in renal failure Px
  • excreted in urine (M3G and M6G b/c they’re polar)
  • cross tolerance: show reduced analgesia when treated with another opioid receptor agonist
  • closes Ca2+ channels on presyn (reduce NT release)
  • opens K+ channels on postsyn (hyperpolarize)
  • tolerance: only to analgesic and respiratory depressant effects (no tolerance develops to miosis or GI effects)
  • peak effect: 1 hr (im)
  • DOA: 3-4 hours
  • Better for continuous, dull pain than for sharp, intermittent pain
  • postoperative, acute MI, renal or biliary colic, pulmonary edema, chronic/terminal pain
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2
Q

Morphine Contraindications

A

Major: head injuries, seizure disorders, drunk (b/c of resp. effects)

Relative: asthma, renal insufficiency (b/c dec. RPF), Hx of abuse, liver disease

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3
Q

Methadone

A
  • strong opioid agonist
  • oral, iv, subQ, spinal, rectal
  • better bioavailability than morphine
  • slow onset, long half-life
  • metabolized by CYP3A4 and CYP2B6 (don’t use in Px with hepatic dysfunction)
  • high cross tolerance to heroin
  • ability to relieve difficult-to-treat pain (neuropathic, cancer)
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4
Q

Buprenorphine

A
  • MOP low dose: partial agonist
  • MOP high dose: antagonist
  • DOP and KOP: antagonist
  • slow dissociation from MOP (resistant to naloxone reversal)
  • Tx of moderate pain
  • sublingual
  • reduces craving for alcohol
  • good substitute for methadone for withdrawal syndrome prevention (safer, lower risk of illicit use)
  • used for opioid dependence, but at high doses it can act as an antagonist and precipitate withdrawal
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5
Q

Meperidine

A
  • STRONG agonist
  • 1/10 analgesic potency of morphine, less efficacious
  • antimuscarinic properties - result in tachycardia
  • less resp. depression in newborns (GOOD)
  • high addiction liability
  • short DOA
  • used for moderate-severe pain, adjunct for anesthesia
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6
Q

Fentanyl

A
  • STRONG agonist
  • iv, epidural, patch
  • 100x more potent than morphine
  • highly lipophilic, slowly metabolized
  • muscle rigidity can occur at high doses (use with an NMJ blocker)
  • patch used to treat chronic pain, adjuvant for anesthesia
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7
Q

Nitrous Oxide MOA

A
  • NMDA receptor inhibitor (glutamate gated)
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8
Q

Nalbuphine

A
  • strong MOP ANTAGonist
  • strong KOP AGonist
  • resp. doesn’t worsen past a certain threshold, but effects are difficult to reverse
  • Tx moderate pain
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9
Q

Codeine

A
  • WEAK agonist
  • anti-tussive
  • less constipation, sedation, respiratory depression
  • converted to morphine by CYP2D6
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10
Q

Oxycodone

A
  • WEAK agonist

    • acetominophen = percocet

+ aspirin = percodan

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11
Q

Tramadol

A
  • codeine analog (non-opioid analgesic)

  • MOP: weak agonist
  • MOA: inhibit serotonin reuptake (SERT) and NE transporter (NET)
  • Tx of mild-moderate pain
  • partially antagonized by naloxone
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12
Q

Tramadol Contraindications

A
  • don’t use in patients who are on medications that lower the seizure threshold
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13
Q

Naloxone

A
  • MOP, KOP, DOP: antagonist

  • rapidly blocks effects of morphine
  • iv
  • used to treat an acute overdose (DOA = 2 hours)
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14
Q

Naltrexone

A
  • MOP, KOP, DOP: antagonist

  • oral
  • 10 hour half-life
  • blocks effects of heroin for up to 48 hours
  • used to prevent relapse in chronic alcoholics (may cause release of beta endorphins)
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15
Q

Desflurane

A
  • general inhaled anesthetic
  • activates GABA-A receptor to be more sensitive to endogenous GABA –> leads to an increase in Cl- influx (hyperpolarization) and decreased neuronal activity
  • poor induction, but rapid recovery
  • medium muscle relaxation
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16
Q

Isoflurane

A
  • general inhaled anesthetic
  • activates GABA-A receptor to be more sensitive to endogenous GABA –> leads to an increase in Cl- influx (hyperpolarization) and decreased neuronal activity
  • medium rate of onset and recovery
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17
Q

Sevoflurane

A
  • general inhaled anesthetic
  • activates GABA-A receptor to be more sensitive to endogenous GABA –> leads to an increase in Cl- influx (hyperpolarization) and decreased neuronal activity
  • rapid onset and recovery
  • used in children
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18
Q

Nitrous Oxide

A
  • general inhaled anesthetic
  • incomplete anesthetic
  • act via inhibition of the NMDA receptor (glutamate-gated)
  • rapid onset and recovery
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19
Q

Ketamine

A
  • general IV anesthetic
  • produces a dissociative anesthetic state
  • only IV to produce analgesia and amnesia
  • binds to phencyclidine site on NMDA receptors (NMDA antagonist)
  • cardiovascular stimulant: use for Px with cardiogenic or septic shock
  • increased cerebral blood flow
  • causes vivid dreams post-op (emergence phenomema), ↓ by pretreatment with midazolam
  • use in kids undergoing painful procedures
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20
Q

Propofol

A
  • general IV anesthetic
  • rapid onset and recovery
  • anti-emetic
  • used in outpatient surgery
  • used for induction and maintenance
  • negative inotropic properties (hypotension, decreased HR, SV)
  • can cause respiratory depression
  • decrease cerebral blood flow and ICP (used for comas)
  • commonly have pain at site of injection
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21
Q

Thiopental

A
  • general IV anesthetic - barbituate
  • rapid onset with BOLUS: crosses BBB because highly lipid soluble
  • rapidly diffuses out of BBB and distributes to muscle and fat
  • used for induction
  • causes a dose-dependent decrease in BP, SV, CO
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22
Q

Cocaine

A
  • local anesthetic (closes Na+ channels)
  • DOA: intermediate
  • use for procedures requiring vasoconstriction, laryngeal, nasal, and urogenital topical application
  • ester: more prone to hydrolysis, short DOA
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23
Q

Bupivacaine

A
  • local anesthetic (blocks Na+ channels)
  • amide: long DOA
  • use for longer duration procedures, infiltration, nerve block, epidural and spinal block
  • especially cardiotoxic
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24
Q

Tetracaine

A
  • high potency
  • ester: longer DOA than cocaine, but still short
  • use for spinal, epidural anesthesia, laryngeal and esophageal exams
25
Q

Lidocaine

A
  • local anesthetic - Block Nav1.8 channel (a voltage-gated Na channel in DRG)
  • amide: BUT short DOA…
  • short duration procedures
  • can be topical
  • toxicity: CNS excitation, but doesn’t affect heart
26
Q

Mepivacaine

A
  • local anesthetic (blocks Na+ channels)
  • amide: intermediate DOA
  • nerve block, epidural block
  • toxicity: CNS excitation, cardio collapse
27
Q

Ambroxol

A
  • Non-opioid analgesic
  • Block Nav1.8 channel (a voltage-gated Na channel in DRG) - similar to lidocaine
  • Treat inflammatory and neuropathic pain
28
Q

Capsaicin

A
  • non-opioid analgesic
  • Exhaust supply of Substance P in nerves
  • Acts via receptor TRPV1
  • Transdermal patches
29
Q

Gabapentin

A
  • GABA analog
  • blocks alpha-2-delta voltage-gated Ca channels
  • Treat neuropathic and inflammatory pain
  • 1,4,5,6,7 (partial seizure, trigeminal neuralgia, mood disorder, migraine (prophylactic), neuropathic pain
  • renal excretion! less D:D interactions
  • weight gain prominent, depression
30
Q

Pregabalin

A
  • GABA analog
  • blocks alpha-2-delta voltage-gated Ca channels
  • Treat partial seizures (ADJUNCT) and neuropathic pain
  • A LOT of weight gain
31
Q

Lamotrigine (Lamictal)

A
  • anticonvulsant
  • Blocks Na channel
  • Blocks N-type voltage-gated Ca channels
  • Decreases glutamate release
  • 1,2,3,4,5: partial, generalized, absence seizure, trigeminal neuralgia, mood disorder
  • Dizziness, nausea; diplopia; ataxia; rash (Stevens-Johnson)
  • Hepatic metabolism by glucuronidation
32
Q

Ethosuximide

A
  • anticonvulsant
  • treat **ABSENCE **
  • inhibits T-type Ca channels
  • No effect on hepatic microsomal enzymes
  • Monitor CBC, liver enzymes because it’s hepatically metabolized
33
Q

Levitiracetam (Keppra)

A
  • MOA unknown
  • adjunct for partial seizures; neuropathic pain
  • Favorite in hospital because renal excretion, no known interactions with other drugs
  • side effects: depression, irritability - don’t use in someone who is depressed
34
Q

Phenobarbital

A
  • binds GABA to enhance transmission; reduced excitatory synaptic responses
  • 1,2, status epilepticus (partial, generalized)
  • used more often in kids
  • cardiac and respiratory depression, hepatic failure, megaloblastic anemia
  • P450
  • long half-life
35
Q

Phenytoin

A
  • Blocks Na channel
  • Decreases synaptic release of glutamate
  • Partial, generalized seizures
  • Gingival hyperplasia; hirsutism (↑ hairiness); dizziness, nausea, vomiting; ataxia; diplopia; nystagmus; rash; blood dyscrasias; sensory neuropathy; teratogen
  • Induces cP450; dose-dependent hepatic metabolism
  • Zero-order kinetics
  • Slow and variable absorption so must measure plasma levels
36
Q

Topiramate

A
  • MOA unknown - does lots
  • Multiple seizure types; chronic migraines; bipolar disorder
  • Drowsiness; dizziness; ataxia; diplopia; confusion; behavioral/cognitive dysfunction; weight loss; kidney stones; metabolic acidosis
    
  • Also used to treat migraines
  • Inhibits cP450
  • Renal and hepatic elimination
37
Q

Valproate

A
  • Blocks voltage-gated Na ch.
  • Inhibits T-type Ca channels
  • Enhances GABA transmission
  • FIRST LINE GENERALIZED EPILEPSY (also used for Lennox Gastaut)
  • also used for chronic headaches and migraine prophylaxis
  • hepatically metabolized by glucouronidation (important for drug:drug interactions)
  • side effects: fat, bald, shaky, acute pancreatitis (check amylase, lipase), bone marrow suppression, hyperammonemia
38
Q

Carbamazepine

A
  • anticonvulsant
  • Blocks voltage-gated Na channels
  • Treat trigeminal neuralgia (“gold standard”)
  • also Tx partial seizure, mood disorders
  • induces own metabolism (P450)
  • side effects: aplastic anemia, stevens-johnson, thrombocytopenia
  • AVOID IN GENERALIZED SEIZURES - it will induce more
39
Q

Aspirin

A
  • Irreversibly inhibits COX-1 and COX-2 by covalent modification at active site
  • inhibits arachidonic acid binding COX-1; substrates bind COX-2 but no PGs produced
  • Antipyresis
  • Relief of low intensity pain
  • Anti-inflammatory
    (RA, OA, IBD)
  • Antithrombotic effects
  • reye’s syndrome toxicity in kids
  • uncouples ox phos - hypervent + resp alkalosis, metabolic acidosis; children may have hypovent + resp acidosis
40
Q

Clopidogrel

A
  • Inhibits ADP binding to P2Y12 receptors on platelets… dec. platelet aggregation and activation
  • Tx of acute coronary syndrome with ASA = 25-35% reduction in death or MI
  • Oral dosing
  • Prodrug, so slow onset but LONG DOA
  • TOX: neutropenia; GI effects; thrombotic thrombocytopenia purpura; bleeding
41
Q

Anticholinergics

  • atropine, etc
A
  • block effects of ACh
  • inhibit parasympathetics
  • atropine lowers organophosphate poisoning
42
Q

Diazepam (Valium)

A
  • long acting benzo
  • Tx of acute status epilepticus, seizure clusters, anxiety
  • enhances GABA-A - increased Cl- - decreased neuronal activity
43
Q

Midazolam (Versed)

A
  • general IV anesthetic (benzodiazepine)
  • H20 soluble
  • often used as a pre-anesthetic (before patient enters OR because it has sedative-anxiolytic properties)
  • slower onset, but effects last longer (just like klonopin vs. xanax)
  • little effect on cardio
44
Q

Lorazepam (Ativan)

A
  • intermediate acting benzo
  • enhanced GABA-A activation, increased flow of Cl- ions, so decreased activity of neurons in limbic, thalamic, and hypothalamic regions
  • Tx of acute status epilepticus, seizure clusters, anxiety
45
Q

Methylprednisolone (prednisone) and Dexamethasone

A
  • Immunosuppressive and anti-inflammatory effects (dec circulating immune cells, dec neutrophil adherence, inhibit histamine release; inhibit T > B lymphocytes)
  • Inhibit production of AA metabolites; induce lipocortin which inhibits PLA2
  • Inhibit cytokine production and release, acute phase reactants
  • DO NOT use oral form to treat optic neuritis!
  • Tx allergies, IBD, spinal cord compression (decreases swelling)
  • Effects not immediate (rely on gene transcription)
  • Short, intermediate, or long acting
  • Can be administered orally, topically, parenterally, or by inhalation
  • Withdraw: flare-up of underlying disease; acute adrenal insufficiency
46
Q

Fingolimod

A
  • Tx of MS
  • Retains certain WBC in lymph nodes to prevent their access to CNS
  • toxicity: abnormal liver enzymes
47
Q

Glatirimer Acetate

A
  • Tx of MS
  • Simulates myelin basic prot; binds to MHC II, competes with myelin antigens for presentation to T cells
  • Inhibits immune response to Myelin Basic Protein, leaves response to other Ag intact
  • subQ injection
48
Q

IFN-beta

A
  • Tx of relapsing-remitting MS
  • may cause skin reactions, influenza- like symptoms
  • may cause stimulation of NGF
49
Q

Natalizumab

A
  • Tx of MS
  • human mab that decreases lymphocyte migration to CNS
  • Reduce risk of progression and exacerbations
  • iv infusion every 4 weeks
  • toxicity: - ↑ risk for PML (progressive multifocal leukoencephalopathy); hepatotoxicity; increased risk of infections; various pains, headache
50
Q

Donepezil (Aricept) and Galantamine (Razadyne) and Rivastigmine

A
  • Tx of Alzheimer’s
  • AchE inhibitor (AD destroys cells that produce and use Ach, so want to ↑[Ach])
  • Mild to moderate symptoms; improves cognition, behavior, function
  • ↑ peripheral Ach function: nausea, vomiting, loss of appetite, diarrhea, in bowel movements
51
Q

Memantine

A
  • Tx of Alzheimer’s
  • NMDA antagonist (NMDA receptors necessary for learning and memory)
  • moderate to severe symptoms
  • No evidence it can prevent or slow neurodegeneration
52
Q

Amantadine

A
  • Tx of Parkinson’s
  • Blocks NMDA, weak inducer of DA release
  • Some stimulation of DA release from substantia nigra
  • Treat dyskinesias
  • Delirium
  • also used to treat influenza A
53
Q

Carbidopa-Levodopa

A
  • FIRST LINE Tx of Parkinson’s
  • Carbidopa inhibits DOPA-decarboxylase in the periphery = more levodopa in the brain
  • “Wears off”; abrupt on-off; esp. as course progresses
  • Nausea, orthostatic hypotension, hallucinations - Dyskinesias—risk linked to dose
  • Effects are dose-related
  • Less effective when taken with food containing proteins (eg with meal or milk) due to competition for uptake
  • No clear benefit in delaying tx as does not accelerate PD progression
  • Advantages over agonists: better PD control, cheaper and easier, fewer short term side effects
  • Also treat Restless Leg Syndrome
54
Q

Entacapone

A
  • Tx of Parkinson’s

– COMT inhibitor; ↓DA metabolism

  • Combine with L-DOPA to treat short-duration response
55
Q

Pramipexole (Mirapex) and Ropinarole

A
  • Tx of Parkinson’s
  • Dopamine agonist (D2)
  • Longer duration of action than L- DOPA but not as effective for motor symptoms
  • Start dose low, titrate up
  • Combine with L-DOPA to treat short-duration response
  • Low standing BP, hallucinations, dyskinesias, nausea, sleepiness, leg edema
  • Compulsive behaviors (12- 15%)
  • Rare= lung and cardiac valve fibrosis
  • Advantages over L-DOPA: less long term motor complications (dyskinesias), longer duration of action, extended release (once daily)
  • Also treat Restless Leg Syndrome
56
Q

Rasagiline and Selegeline

A
  • Tx of Parkinson’s
  • MAO-B inhibitor, so levels of DA increase in presynaptic cleft
  • avoid tyramine containing food
  • Combine with L-DOPA to treat short-duration response
57
Q

Sumatriptan

A
  • Tx of Migraines, cluster headaches
  • stimulates presynaptic 5-HT1D receptors (results in inhibition of vasodilation and inflammation of the dura)
  • CONTRAINDICATED in Px with coronary artery disease
58
Q

Amytryptaline

A
  • Tx of Migraine PROPHYLAXIS
  • Indirectly affect endogenous opioid pathway by activating descending 5HT pathway
  • Also use for fibromyalgia, shingles, diabetic neuropathy
59
Q

Propranolol

A
  • beta blocker
  • migraine prevention

Neuro (5 decks)

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