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Neuro 1 > Pharm > Flashcards

Pharm Flashcards

1
Q

Vincristine

A

Chemotherapeutic drug that causes peripheral neuropathy due to microtubule damage

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2
Q

Bethanechol

A

Muscarinic antagonist for post operative ileus

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3
Q

Pilocarpine

A

Musacrinic agonist used to increase secretions in ppl with Sjögren’s syndrome

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4
Q

Tropicamide

A

Musacrinic antagonist producing mydriasis needed in eye exam

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5
Q

Ipratropium

A

Muscarinic antagonist for COPD

Bronchodilates and inhibits bronchial glands

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6
Q

Tolterodine

A

Muscarinic antagonist for urge incontinence

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7
Q

Side effects of muscarinic antagonists

A

Constipation

Dry eyes

Dry mouth

Urinary retention

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8
Q

Treatment for cholinergic excess

A

Atropine (muscarinic antagonist) and pralidoxime (chemical antagonist)

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9
Q

Cholinesterase Inhibitor Poisoning

A 
D-diarrhea
U-urination
M-miosis
B-bronchospasm
B-bradycardia
E-excitation (of skeletal muscles)
L-lacrimation
S-sweating
S-salivation

Respiratory failure and death

With cholinergic excess, muscarinic symptoms before nicotinic

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10
Q

Mechanism of Action: Local Anesthetic

A

Reversible blocks voltage-gated Na+ channels to inhibit impulse conduction along nerve axons

Does not change resting potential

Neutral form required to enter membrane, but charged form required for binding to channel site

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11
Q

Modulated Receptor Hypothesis

A

Local anesthetic binding is a function of the conformational state of the channel

LAs have higher affinity for receptors in activated and inactivated states than receptors in resting state

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12
Q

Frequency Dependent Block

A

Repeated depolarizations produce more effective anesthetic binding

Fibers that fire at a faster rate are more susceptible to effects of LAs

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13
Q

Vasoconstrictors and local anesthetics

A

Vasoconstrictors decrease absorption

Used with short and medium acting drugs to increase duration of local anesthesia by constricting blood vessels (concentrates drug where it is needed)

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14
Q

Elimination of Esters

A

Plasma pseudocholinesterase yields PABA and derivatives

PABA can cause allergic reaction

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15
Q

Elimination of Amides

A

Liver and cytochome P450

If impaired flow to liver, have increased amide serum concentration

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16
Q

Adverse effects-local anesthetics

A
  1. Systemic toxicity: first manifests as CNS toxicity, then cardiotoxicity
  2. Local neural toxicity: can cause membrane damage leading to death of neuron; motor and sensory loss are seen; transient neurologic symptoms
  3. Methemoglobinemia: prilocaine and metabolites act as oxidizing agent to convert hemoglobin2+ to 3+, which causes decrease oxygen delivery
  4. Allergies: PABA metabolite of esters can cause IgE mediated allergy
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17
Q

Cocaine

A

LA

Stimulant, vasoconstrictor

18
Q

Benzocaine

A

LA

MetHb potential

19
Q

Mepivacaine

A

LA

Lowest pKa of injectable LAs

Vasoconstrictor–>longer duration

20
Q

Prilocaine

A

LA

MetHb potential

21
Q

Bupivacaine

A

LA

Risk of cardiotoxicty

22
Q

Opioid receptor target

A

G-protein coupled receptors

Mu
Kappa
Delta

23
Q

Opioid Mechanism of Action

A

Inhibitory process

Opioid binds to receptor on presynaptic neuron which inhibits the formation of cAMP

Decreased cAMP causes Ca2+ channels to close, preventing transmission of AP and release of NT

Opioid also binds to receptor on post-synaptic neuron, causing K+ channels to open and hyperpolarization of the cell, thus decreasing the firing of the neuron and decreasing excitability/pain

24
Q

Acute effects of Opioids

A 
Analgesia 
Respiratory depression
Euphoria
Cough Suppression
Miosis
Constipation 
Increased intracranial pressure
25
Q

Euphoric effects of opioids

A

Decrease GABA in neuron

Increase dopamine release from neighboring neuron

26
Q

Opioid effect on CNS

A

Sedation

Toxicity: contraindicated for head injury because can cause increase intracranial pressure

Respiratory depression: decreased response to carbon dioxide causes CO2 to rise, leading to cerebral vasodilation and increased intracranial pressure
Give naloxone, not oxygen
Major cause of death from overdose

Cough suppression

Pupillary constriction (except meperidine) 
Miosis is visible sign of overdose

Nausea and vomiting

Muscle rigidity

27
Q

Meperidine

A

Opioid that causes mydriasis (contrary to the miosis caused by other opioids)

28
Q

Opioid effect on cardiovascular system

A

Minimal effects, but may cause bradycardia, vasodilation, and orthostatic hypertension

29
Q

Opioid effect on histamine release

A

Causes non-immunologic (non-allergic) release of histamine, including vasodilation and hypotension

Skin redness, urticaria, pruritus

30
Q

Opioid effect on smooth muscle

A

GI: decreases peristalsis, which can lead to constipation

Biliary: induce spasmodic effects which may lead to biliary colic

Urinary tract: anti-diuretic, so can cause urinary retention

31
Q

Methynaltrexone

A

Medication used to treat opioid-induced constipation

32
Q

Loperamide

A

Opioid used to treat diarrhea

33
Q

Diphenoxylate

A

Opioid used to treat diarrhea

34
Q

Opioid effect on pregnancy/neonate

A

Used to relieve pain in labor

Fetus may become opioid dependent in utero because it courses the placenta
May cause respiratory depression in baby

35
Q

Opioid Overdose

A

Classic triad:

  1. Miosis
  2. Respiratory depression
  3. Apnea, coma
36
Q

Mechanism of Action: Nalaxone

A

Rapidly reverses opioid overdose by competing for opioid receptors (mu, kappa, and delta)

Short half life

37
Q

Methadone

A

Full mu agonist: Competes with opioids for mu receptor binding

Long acting

38
Q

Mechanism of Action: Cholinergic Drugs

A
  1. Presynaptic transporter CHAT brings in choline and Na+
  2. ChAT assembles choline and acetyl CoA into acetylcholine
  3. ACh is packed into vesicle using VAT (vesicle associated transporter)
  4. Ca2+ channels open, allowing for an influx and exocytosis of vesicle
  5. ACh binds to receptor on post synaptic neuron
  6. ACh on autoreceptor is important negative feedback loop
  7. Excess ACh is degraded by AChE
39
Q

Nicotinic receptors

A

Ionotropic

5 subunits

Nm=muscle type (on skeletal muscle endplate)

Nn=neuronal type (on another neuron)

40
Q

Muscarinic Receptor

A

Metabotropic

7 transmembrane domains

M1, M3, and M5 rely on second messengers

M2 and M4 open K+ channels

Neuro 1 (7 decks)

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