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NBDE II Board Busters > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

catecholamines pass the blood brain barrier well? poorly?

A

very poorly

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2
Q

acetylcholine affects what 2 receptors

A

nicotinic
muscarinic

secreted by cholinergic fibers

after a threshold stimulus, liberation of Ach alters the cell membrane’s permeability

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3
Q

epinephrine is a direct acting catecholamine and adrenergic agonist or antagonist?

A

AGONIST

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4
Q

norepinephrine is a direct acting catecholamine that works through which receptors in the CNS?

A

a1, a2, b-adrenergics

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5
Q

dopamine (intropin) is an immediate precursor to?

acts through which 2 subtype receptors?

A

NE

D1 - activates adenylyl cyclase
D2 - inhibits adenylyl cyclase

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6
Q

serotonin (5-hydroxytryptamine) works through at least 14 subreceptors __ type neurons

A

tryptominergic

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7
Q

the major inhibitory neurotransmitter in the CNS is

A

GABA

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8
Q

opioid peptides include (3)

A

beta-endorphin
enkephalines
dynorphin

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9
Q

these 2 nts have EXCITATORY effects on neurons everywhere in the CNS

A

glutamate

aspartate

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10
Q

catecholamines are a group of

A

sympathomimetic compounds

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11
Q

these 2 catecholamines stimulate the myocardium

A

epi

NE

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12
Q

clinically, epi is for

A

anaphylaxis, glaucoma, asthma, vasoconstriction to prolong anesthesia

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13
Q

clinically, norepi causes

A

vasoconstriction in hypotension

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14
Q

CNS stimulants include

  1. analeptics
  2. xanthines
  3. sympathomimetic amines
A
  1. analeptics - can overcome drug-induced RESPIRATORY DEPRESSION and hypnosis [metrazol, coramine, dopram, picrotoxin, strychnine]
  2. xanthines - improve mental ALERTNESS, reduce urge to sleep, elevate MOOD [caffeine, theophylline, theobromine]
  3. sympathomimetic amines - to treat NARCOLEPSY, OBESITY, ADHD [amphetamines, methylphenidate, phenmetrazine]
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15
Q

__ is the only xanthine important in asthma tx, by stimulating medulla respiratory centers to cause bronchial dilation

A

theophylline

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16
Q

caffeinism occurs if you intake > __ mg caffeine per day

A

600-750 (10 cups)

> 1000 mg is TOXIC

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17
Q

caffeine stimulates the CNS unequally, with the __ being the most excited, and __ least excited

A

CORTEX most,

spinal cord least

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18
Q

the Autonomic Nervous System (ANS) is an efferent motor system that fxns independent of consciousness and controls __

A

automatic VISCERAL fxns required for life

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19
Q

drugs block or mimic ANS transmitters to clinically modify what functions?

A

autonomic fxns like: cardiac and smooth muscle, vascular endothelium, exocrine glands, presynaptic nerve terminals)

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20
Q

ANS consists of 2 parts

A

sympathetic nervous system - response to STRESS, fight or flight

parasympathetic - at REST, rest and digest

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21
Q

SYMPATHETIC NERVOUS SYSTEM FUNCTION

A
  • epi released from adrenal medulla
  • HR incr (tachycardia)
  • CO, Bp, blood flows from skin and internal organs into SKELETAL MUSCLE
  • energy stores are mobilized
  • pupils dilate (MYDRIASIS
  • bronchioles dilate
  • FEAR activates ANS sympathetics -> HYPERTENSION (a1 adrenergic receptors cause arteriolar vasoconstriction)
  • DECR. salivation
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22
Q

PARASYMPATHETIC NERVOUS SYSTEM FUNCTION

A
  • effectors are activated as needed, does not discharge as a complete system
  • Cranial nerves with PS activity = 3, 7, 9, 10
  • MIOSIS (pupils constrict)
  • bradycardia
  • incr. salivation
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23
Q

4 types of drug-receptor binding

A
  1. ionic - from electrostatic attraction btw ions of opp. charge
  2. H bonds - btw polar (water) molecules
  3. Van der Waals - weak interactions when atoms close
  4. Hydrophobic - btw drug, receptor and aqueous environment
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24
Q

covalent bonds

A

sharing e- by pair of atoms, for structural integrity of molecules, NOT involved in drug-receptor rxns

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25
Q

4 families of physiologic receptors

A
  1. receptors as enzymes (cell surface protein kinases) - kinases work by phosphorylating proteins
  2. ion channels - drugs bind channels to cause opening or closing -> alters cell membrane potential
  3. G-protein coupled receptors - second messengers like cyclic AMP are produced to cause an effect in the cell
  4. Receptors in the cell nucleus - receptors for steroid hormones are soluble DNA-transcription factors in nucleus
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26
Q

alpha (a) receptors are primarily excitatory or inhibitory?

located where?

A

EXCITATORY

vascular smooth muscle, pre-synaptic nerve terminals, blood platelets, fat cells, CNS neurons

*exception, some a-receptors relax GI smooth muscle

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27
Q

2 types of alpha receptors

A
  1. post junctional a1 adrenergic (MORE COMMON)
    - radial smooth muscle in iris, arteries/arterioles/veins, GI tract
    - causes CONTRACTION and VASOCONSTRICTION
    - in arterioles of skin, mucosa, viscera, kidney
  2. pre-junctional a2 adrenergic
    - INHIBITS release of NE
    - on presynaptic nerve endings to stop NE release
    - on post-synaptic endings in CNS to DECR. sympathetic tone
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28
Q

what nts combine with both types of alpha receptors

A

epi and norepi

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29
Q

beta receptors are mainly responsible for excitatory or inhibitory effects?

A

INHIBITORY, like vasodilation and relaxation of respiratory smooth muscle

*exception: some mediate excitatory increases in heart’s force and rate of contraction

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30
Q

2 types of beta receptors

A
  1. post-junctional b1 adrenergic
    - in HEART myocardium cell, intestine smooth muscle, adipose tissue
    - NE and epi both bind to INCR. HR, CO, BP, force of contraction
  2. post-junctional b2 adrenergic (MOST COMMON)
    - in BRONCHIOLAR and VASCULAR smooth muscle
    - cause VASODILATION in bronchial and uterine muscle to cause relaxation
    - incr. blood glucose
    - ONLY EPI (NE combines weakly or not at all to these)
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31
Q

epi combines with __ receptors to vasodilate bronchioles and tx asthma?

A

b-2 adrenergic receptors

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32
Q

pharmacologic agonist

A

binds to physiologic receptors to cause specific cellular effects, a full response

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33
Q

pharmacologic antagonist

A

binds receptor, does not trigger effect

-agonist can’t reach receptor site

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34
Q

competitive antagonism is when?

non-competitive antagonism is when?

A
  • response CAN be achieved by increasing agonist dose

- NO response with increasing agonist

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35
Q

sympathomimetic agents (adrenergic AGONISTS) do what?

A

mimic effects of STIMULATION of organs/structures of the SYMPATHETIC nervous system

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36
Q

uses for adrenergic agonist therapy includes

A
  1. control hemorrhage - a1 vasoconstriction
  2. allergic shock (anaphylaxis) - a1 vasoconstriction, b2 airway dilation, b1 incr. cardiac output
  3. nasal decongestant - a1 vasoconstriction
  4. bronchial relxation/airway - b2 agonist
  5. cardiac stimulation - b1 agonist
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37
Q

__ is the prototypical adrenergic agonist

A

epi

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38
Q

in anaphylaxis, epi works on what receptors, doing what?

A

a1 - vasoconstriction to incr. BP
b1 - incr. cardiac output
b2 - dilates bronchial tubes

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39
Q

bronchodilators (b2 agonists) to tx acute asthma include

A

epi
albuterol
salmeterol
metaproterenol

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40
Q

amionphylline is a theophylline compound used for

A

bronchodilation for asthma or COPD, RELAX bronchial smooth muscle, a CNS stimulant that tx asthma

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41
Q

epi, penylephrine, albuterol, and isoproternol are all __ agonists

A

adrenergic; bind to adrenergic receptors

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42
Q

Direct acting Sympathomimetic agents - interact with a or b receptors, can be receptor selective or non-selective

Include ->

A

phenylephrine - a1 selective agonist, nasal decongestant, mydriatic, tx chronic orthostatic hypotension, 100x less potent than epi

clonidine - a2 selective agonist, anti-hypertensive

dobutamine - b1 selective agonist

terbutaline - b2 selective agonist, tx COPD, bronchopasm

albuterol - b2 selective agonist, long term tx obstructive airway diseases, ER tx bronchospasm, delay premature delivery

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43
Q

epinephrine (adrenaline) is a vasoconstrictor and stimulates what receptors

A

a1,2
b1,2

direct acting agonist

actions: vasoconstriction, incr BP, bronchodilation (b2), decr. blood volume in nasal tissue, OPPOSITE effects of histamine

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44
Q

epi is contraindicated in pts with

common epi side effects

A

ANGINA, cause of cardistimulatory effects

headaches, agitation (anxiety), tachycardia

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45
Q

norepinephrine is a __ agonist

A

a1, 2

b1

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46
Q

isoproterenol is a __ agonist

A

b1,2

MOST POTENT BRONCHODILATOR

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47
Q

Indirect acting Sympathomimetic agents - cause release of stored NE at post-ganglionic nerve endings, similar to STIMULATING the SYMPATHETIC nervous system

includes these drugs:

A 
tyramine
amphetamine
methamphetamine
hydroxyamphetamine
methoxamine
ephadrine
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48
Q

DA, EPI, NE< isoproterenol and phenylephrine are used as pressor agents to?

A

maintain BP in vascular shock; bronchodilators for asthma attacks and anaphylactick shock

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49
Q

amphetamines

A

stimulate CNS and PND
increase systolic and diastolic bp
weak bronchodilator and respiratory stimulant

pass readily in CNS and cause rapid release of NE in brain

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50
Q

ADHD drugs

A 
methylphenidate (ritalin) - mild CNS stimulant
focalin - new form of above
concerta - long acting ritalin
Adderal (mixed amphetamine salts)
strattera (atemoxetine) - non-stimulant
metadate CR - controlled delivery
dextroamphetamine (dexedrine)
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51
Q

dextroamphetamine (dexedrine) is used to treat

A

narcolepsy

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52
Q

4 types of Sympatholytic agents (anti-adrenergic) that act in a way OPPOSITE to the sympathetic nervous system. 4 types that all treat hypertension are

A
  1. beta-adrenergic receptor blockers (b blockers)
  2. alpha-adrenergic receptor blockers (a blockers)
  3. centrally-acting anti-hypertensive agents (a 2 selective agonists)
  4. neuronal depleting agents
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53
Q

beta blockers treat?

side effects?

A

hypertension, angina, cardiac arrhythmias, MI, glaucoma, prophylaxis of migraine

weakness, drowsiness

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54
Q

propranolol, timolol, nadolol

A

block b1 and b2, so they are NON-selective beta blockers

propranolol is the drug of choice for adrenergically induced arrythmias

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55
Q

non-selective b blockers are contraindicated in pts with

A

asthma or other chronic obstructive airway disease -> cause fatal bronchospasm

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56
Q

acebutolol (sectral) is a

A

b1 selective antagonist, tx HTN and arrhythmias

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57
Q

metoprolol is a

A

competitive b1 cardioselective antagonist

tx HTN, acute angina pectoris, good after heart attack

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58
Q

atenolol (tenormin) is a

A

competitive b1 cardioselective antagonist

tx HTN, chronic angina pectoris, after MI, LONG PLASMA 1/2 life

excreted by kidneyes

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59
Q

___ and __ are longer acting and more predictable than propranolol, b1 selective so SAFER to use in pts with asthma or bronchitis

A

metoprolol

atenolol

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60
Q

a blockers can cause

A

tachycardia, lower BP, vasodilation, orthostatic hypotension

any alpha antagonist can cause EPI reversal

main effects - reduce BP, reflex tachycardia

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61
Q

a blockers act by?

major adverse effect is?

A

competitively inhibiting catecholamines at the a receptor site -> blood vessels DILATE

hypotension

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62
Q

after vasovagal syncope, __ is the 2nd most likely cause of transient unconsciousness in the dental office

A

orthostatic hypotension

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63
Q

factors that can cause orthostatic hypotension include

A

drugs, bad postural reflex, pregnancy, Addison’s, CHRONIC ORTHOSTATIC HYPOTENSION (Shy-Drager Syndrome)

increases with age

also an adverse effect of NSAIDs

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64
Q

drugs that can cause orthostatic hypotension (5)

A
  1. antihypertensives
  2. phenothiazines
  3. tricyclic antidepressants
  4. narcotics
  5. antiparkinson drugs
65
Q

2 types of alpha blockers (selective and non-selective)

a1 to treat?

non-selectives do not treat what conditions?

A
  1. Selective a1 blockers - tx cardiac conditions (HTN, benign prostatic hyperplasia (BPH))
  2. Non-Selective block a1 and a2, NOT for cardiac conditions cause it can cause tachycardia. Used for pre-surgery mgmt of PHEOCHROMOCYTOMA and RAYNAUD’S PHENOMENON
66
Q

selective a1 blockers include (3)

A
  1. Doxazosin (cardura) - tx HTN, long duration of action
  2. Prazosin (minipress) - not used much
  3. Terazosin (Hytrin) - mild to mod HTN, and BPH
67
Q

non-selective a1 and a2 blockers include (2)

A
  1. Tolazine (Priscoline) - direct peripheral vasodilation, treats persistent pulmonary HTN of newborn
  2. PHentolamine HCl (Regiitine) and PHenoxybenzamine HCl (Dibenzylene) - manage pheochromocytoma (adrenal medulla tumor)
68
Q

pheochromocytoma is a tumor of the?

A

adrenal medulla

releases excess EPI and NE -> causes HTN, tachycardia, arrhythmias

69
Q

epi reversal is a predictable result of using epi with a pt who received what kind of drug?

A

alpha blocker

without blockers, epi and NE will cause BP to increase
after a blocker, the pressor effect of NE is reduced and EPi causes a fall in BP (because NE only stimulates a receptors and has no b2 effects)

after blocking a receptors, only b can be stimulated

70
Q

pressor response produces

A

increase in BP and is mediated by a receptors

-depressor response produces decr. bp, mediated by b2 receptors

71
Q

centrally acting anti-HTN agents are a2 selective agonists that

include (3)

A

reduce BP by reducing cardiac output, vascular resistance

  1. Clonidine - a2 selective, in combo with thiazide and hydralazine, relaxes blood vessels
  2. Guanfacine and Guanabenz - stimulate a2 to inhibit sympathetic outflow, reduce peripheral resistance
  3. Methyldopa - combine with diuretic to produce FALSE transmitter tat replaces NE, good to tx HTN in pts with RENAL DAMAGE
72
Q

adverse effects of methyldopa

A

orthostatic hypotension, bradycardia, sedation and fevere, GI colitis, hepatitis, cirrhosis

73
Q

neuronal depleting agents deplete

includes (2)

A

catecholamine (NE, EPI, serotonin)

  1. Reserpine blocks uptake of NE, EPI, serotonin
  2. Guanethidin - blocks release of NE
74
Q

a and b adrenergic blockers act by

A

competitive inhibition of postjunctional adrenergic receptors

75
Q

autonomic nervous system has __ fibers that secrete __, and __ fibers that secrete norepi, epi, or dopamine.

A

cholinergic fibers secrete acetylcholine

adrenergic fibers secrete norepi, epi, dopamine (catecholamines)

76
Q

cholinergic fibers (neurons) release/secrete __

2 kinds

A

ACh
-primary nt

  1. Preganglionic sympathetic & parasympathetic
  2. Postganglionic parasympathetic - a MUSCARINIC response
77
Q

postganglionic SYMPathetic fibers are what kind?

A

adrenergic!! not cholinergic

78
Q

postganglionic sympathetic fibers that innervate sweat glands secrete

A

acetylcholine

79
Q

acetylcholine receptors are divided into 2 groups

A
  1. Muscarinic
    - autonomic effector cells in CNS (heart, vascular endotheliu, smooth muscle, prseynaptic nerve terminals, exocrine glands)
    - respond to MUSCARINE and ACh
  2. Nicotinic
    - in ganglia, skeletal muscle end plates, CNS
    - respond to NICOTINE and ACh
    - acts at neuromuscular jxn of skeletal muscle
80
Q

2 major nicotinic receptors

A
  1. at neuromuscular jxns at somatic nervous systems - where neuromuscular blockers work here
  2. at autonomic ganglia in both sympathetic and parasympathetic systems - ganglionic blockers work here
81
Q

ACh is the chemical mediator at:

A

all autonomic ganglia, parasympathetic postganglionic synapses, transmitter at neuromuscular junction in skeletal muscle and sweat glands

82
Q

ACh causes alteration in cell membrane permeability to produce these actions:

A

cholinergic drug actions - slow hear, miosis, simtulate bronchi, GI tract, gallbladder, bile duct, bladder, ureters, stimulate sweat + salivary + tear + bronchial glands

83
Q

cholinesterase inhibitors increase/decrease salivation?

A

increases cause it reduces acetylcholine metabolism

84
Q

overdose of cholinergic drugs cause

A

sweating, urination, bradycardia, copieous saliva

but NOT mydriasis (dilation)

85
Q

all __ receptors are CHOLINERGIC

A

M receptors

bind acetylcholine and are antagonized by ATROPINE

86
Q

3 classes of cholinergic agonists

A

choline esters

cholinergic alkaloids

cholinesterase inhibitors

-stimulate muscarinic sites by mimicking ACh, BUT if these are given before ACh, then the action of ACh is enhanced and prolonged

87
Q

indirect acting cholinergic agonists (cholinesterase inhibitors) act by

cause a __ effect

inhibit at what sites?

A

increase the effects of ACh in the autonomic nervous system and at neuromuscular junctions

cause a CHOLINERGIC EFFECT -> eventually causes muscle paralysis

they inhibit acetylcholinesterase at BOTH muscarinic and nicotinic sites

88
Q

indirect acting cholinergic agonists (cholinesterase inhibitors) include (4)

A
  1. edrophonium - good to dx myasthenia gravis
  2. neostigmine and pyridostigmine - tx myasthenia gravis, can reverse blockade
  3. malathion and parathion - insecticides
  4. physostigmine
89
Q

pralidoxime (protopam) is a cholinesterase reactivator used as an antidoe to reverse?

A

muscle paralysis due to organophosphate anticholinesterase pesticide poisoning

90
Q

symptoms of organophosphate poisoning

A

excess salivation, bronchoconstriciton, diarrhea, skeletal muscle fasciculations (twitching)

91
Q

organophosphates inhibit cholinesterase. 5 of them are

A
  1. isoflurophate and echothiophate - tx glaucoma
  2. malathion - insecticide
  3. parathion - insecticide
  4. tabun
  5. metrifonate - anthelmintic
92
Q

direct acting cholinergics are in 2 gruops

A
  1. choline ESTERS - decrease BP due to general vasodilation, flushing of skin, slow HR [carbachol to produce miosis, bethanecol for post-op ab distension and urinary retention]
  2. cholinergic ALKALOIDS
    - pilocarpine used as a MIOTIC and to tx open-angle glaucoma and xerostomia
93
Q

xerostima is caused by

A

meds, cancer therapy, Sjogren’s syndrome, head and neck trauma, bone marrow transplants, endocrine disorders, etc.

94
Q

cholinergics tx dry mouth by inducing salivation. cholinergics used are (2)

A
  1. pilocarpine (salagen) - cholinergic agonist and alkaloid, tx xerostomia caused by salivary gland hypofunction
  2. cevimeline (evoxac) tx xerostomia in pts with Sjogren’s
95
Q

cholinergic crisis symptoms

A

bradycardia, lacrimation, extreme salivation, vasodilation, muscle weakness

96
Q

typical cholinergic effects caused by stimulation of ACh (cholinergic) receptors are

A

salivation, miosis, excess sweating, flushing, incr. GI motility and bradycardia

97
Q

mecamylamine (inversine) is a __ blocking drug

A

nicotinic ganglion

98
Q

anti-cholinergic (anti-muscarinic) drugs produce opposite effects of cholinergics like

A

xerostomia (block postganglionic cholinergic fibers), mydriasis (dilation), anti-spasmodic, decr. GI motility, less gastric and salivary secretions, tachyardia

99
Q

anti-cholinergics are contraindicated in __ patients

A

GLAUCOMA, cardio probs, GI obstruction, asthma

100
Q

anticholinergics work by

therapy for:

A

preventing ACh from occupying the same receptor

Parkinson’s, motion sickness, bladder syndrome, traveler’s diarrhea

101
Q

anticholinergic/antimuscarinic drugs include

A 
glycopyrrolate - diarrhea, bladder
propantheline bromide - diarrhea
benzotropine - Parkinson's
trihexyphenidyl HCl - Parkinson's
atropine sulfate - causes mydriases, cycloplegia
scopolamine - reduces motion sickness
belladonna derivatives
102
Q

nicotinic receptor antagonists (nicotinic blockers) divided into

  1. Ganglionic blockers
  2. Neuromuscular blockers
A
  1. Ganglionic - not used cause of parasympathetic blockade that causes xerostomia, constipation, blurred vision, postuarl hypotension [mecamylamine, trimethaphan for HTN in emergency, cause fall in BP]
  2. Neuromuscular - complete skeletal muscle relaxation and helps in endotracheal intubation, interact with nicotinic receptors, danger is it can lead to paralysis
103
Q

2 classes of neuromuscular blockers include

A
  1. non-depolarizing (competitive) - cause paralysis [Tubocurare (curare] is the prototype]
    * Neostigmine/Pyridostigmine used to REVERSE paralysis
  2. depolarizing (non-competitive) - [Succinylcholine prototype], used in caution with pts with low pseudocholinesterase (can cause respiratory failure)
104
Q

Skeletal muscle spasmolytics (relaxants) are used for some CNS diseases like?

include (5)

A

multiple sclerosis, cerebral palsy, CVAs

  1. baclofen - derivative of GABA
  2. carisoprodol
  3. cyclobenzaprine
  4. methocarbamol
  5. quinine - nocturnal leg cramps
105
Q

bioavailability measures

A

rate and amount of therapeutically active drug that reaches systemic circulation

amt of drug absorbed/amt of drug administered

IV provides 100% bioavailability

106
Q

drug’s onset of action is primarily determined by rate of?

A

absorption

major effect of a drug is determined by how much is FREE IN PLASMA

107
Q

oral route of administration

A

safest and easiest

hepatic FIRST PASS metabolism, not for emergencies

drugs are absorbed best from the DUODENUM

108
Q

intramuscular injection

A
  • 5 min rapid onset
  • good for solutions too irritating to be subcutaneous
  • aqueous soln absorbs fast, and oily ones are slow
  • anterior thigh for kids
  • 1 inch deep for adults, 1/4 inch for kids
109
Q

subcutaneous injection

intra-arterial injection concern

A
  • 15 min onset, less rapid

- can burn

110
Q

intravenous injection

A
  • most RAPID onset

- 100% bioavailability, allows TITRATION

111
Q

inhalation

A
  • 5 min

- most frequent in pediatric pts

112
Q

patch delivery

A
  • in blood over 12-24 hrs

- SYSTEMIC effect

113
Q

distribution of a drug into tissue mainly depends on _

A

rate of blood flow to the tissue

-also gastric emptying time and degree of plasma protein binding (albumin) matters but not as much

114
Q

most drugs travel through blood by binding to __

A

albumin

115
Q

physiochemical properties of drugs that influence their passage across membranes are

A

lipid solubility, degree of ionization, molecular size, molecular shape

116
Q

most drugs are absorbed by what kind of transport

A

facilitated diffusion

driving force is concentration difference

117
Q

biotransformation of drugs in the liver in 2 phases

A

Phase I - P450 system

Phase II - conjugation

118
Q

DEA Schedule I drugs

A

not for medical use, can’t be prescribed

119
Q

DEA Schedule II drugs

A

strong potential for ABUSE or ADDICTION, but have legitimate medical use

amphetamines, morphine, cocaine, pentoarbital, oxycodone, methadone, codein

need rx, can be prescribed but not refilled, can’t be called in

120
Q

DEA Schedule III

A

written rx signed, can call in, can have refills

analgesic combos

121
Q

DEA Schedule IV

A

diazepam (valium), lorazepam, triazolam, xanax

122
Q

who determines which drugs can be sold by rx?

A

FDA

123
Q

allergic rxns to anesthetics is more common with what kind?

__ is the component of local anesthetics that causes allergy

A

esters (not amides)

bisulfites

124
Q

mechanism of local anesthetics

A

decrease Na+ uptake through sodium channels, decreases nerve’s excitability and impulses fail to propagate

NO effect on K+

125
Q

when tissues are normal (pH = 7.4), what % of the local anesthetic is in free base form? (non-ionized)

A

10-20%

enough to penetrate nerve to cause anesthesia

126
Q

the lower the drug’s pKa, and higher the pH of the solution or injected tissue, the MORE or LESS free base avail?

A

MORE

127
Q

potential action of locals depends on the ability of

A

the SALT to liberate the FREE BASE (active form)

128
Q

esters are metabolized in the __

amides in the __

A

plasma

liver

129
Q

esters mainly avail as

A

topicals

PROCAINE (novocaine) one of the originals

130
Q

the only local anesthetic that increases the pressor activity of EPI and NE is

A

cocaine

  • ester
  • causes definite vasoconstriction
131
Q

amides

A

used with caution or not at all in pts with compromised liver
-metabolized by P450 enzymes

132
Q

the only amid local anesthetic metabolized int he bloodstream is

A

articaine (septocaine)

contraindicated in pts sensitive to amides or sodium bisulfite

max dose 7 mg/ kg

133
Q

prilocaine (citanest)

A
  • causes less vasodilation than lido
  • less potent than lido

not for pts with liver disease, hypoxic conditions

metabolized into orthotoluidine -> can produce methemoglobinemia

134
Q

bupivacaine (marcaine)

A

longest duration of action of any local anesthetic

135
Q

lidocaine (xylocaine)

A

anti-arrhythmic agent in the ventricle
-decreases cardiac excitability

lido + mepi most likely to show cross-allergy

136
Q

mepivacaine (carbocaine)

A

equal to lido in efficacy and used without EPI

TOXIC to neonates

short lasting

137
Q

max. lido dose in kids

max. in adults

A

in kids, by weight, 4.4 mg/kg

in adults, 300 mg

138
Q

chloral hydrate

A

only non-barbiturate sedative-hypnotic indicated in dentistry

  • used orally for anxious kids
  • kids will get excited and irritable before sedation
  • DOES NOT RELIEVE PAIN
139
Q

nitrous oxide must be coupled with __ % oxygen

A

20

140
Q

nitrous is contraindicated for

A

upper respiratory infxns, emphysema, bronchitis, 1st trimester of pregnancy, autistic pts (communication difficult), NEVER on pts with contagious disease

141
Q

drug of choice against syncope is

A

inhaled ammonia

-irritates trigem nerve sensory endings

142
Q

inhalation agents

A
  1. isoflurane - for old ppl, safe for heart disease
  2. halothane, enflurance - decreases cardiac output, halothane sensitizes heart to catecholamines (risk of ventricular arrhytmia); enflurane is CNS irritant so avoid in pts with seizures

lipophilic moleculres

143
Q

IV agents, classes

A
  1. Barbiturates
  2. Benzodiazepines
  3. Neuroleptanalgesics
  4. Others
144
Q

Barbitruates (2)

A
  1. thiopental (pentothal) - MOST COMMON, ultrashort acting

2. methohexital (brevital) - outpatient, rapid recovery, short acting

145
Q

Benzodiazepines do not provide anesthesia, provide anterograde amnesia, and include

A
  1. midazolam (versed) - pt groggy, preferred to diazpema because more water soluble
  2. diazepam (valium) and lorazepam (ativan) - ANTI ANXIETY, contraindicated in pts with narrow angle glaucoma. diazepam for cerebral palsy and status epilepticus
  3. flumazenil -benzodiazepine antagonist for recovery
  4. alprazolam (xanax) - anxioloytic effects in pts with agoraphobia
146
Q

__ and __ are benzodiazepines that provide preop sedation but are more irritating

A

lorazepam (ativan) and diazepam (valim)

147
Q

__ are the most effective oral sedative drugs in dentistry

A

benzodiazepines

  • used for anxiety and sleep disorders
  • dont’ use during pregnancy
148
Q

Neuroleptanalgesics are neruoleptic-opiod combos that combine __ and __

A

Fentanyl and Droperidol

Fentanyl - opioid used as premed or adjunct to inhalation agents, used with droperidal and NO.

149
Q

opioid adverse effects are reversed and recovery hastened by admin of

A

Naloxone (Narcan)

-opioid antagonist

150
Q

Propofol (Diprivan)

A

IV anesthetic, metabolized in liver

  • respiratory depressant
  • doesn’t increase intracranial pressure
  • safer for pregnant women, less likely to cause bronchospasms
  • contraindicated in kids, caution if pt has hypotension
151
Q

etimodate (amidate) andvantage is

A

minimal respiratory and cardiovascular depressant effects

  • no alnalgesic effects
  • no hypotension or significant HR effects
152
Q

ketamine

A

for DISSOCIATIVE ANESTHESIA

  • cause catatonia, amnesia, analgesia without loss of consciousness
  • antagonist at NMDA receptor to block excitatory effects
  • not good for adults, better in kids
153
Q

only anesthetic that acts as a cardiovascular stimulant is

A

KETAMINE

154
Q

benzodiazepines, barbiturates and narcotic analgesics all produces

A

SEDATION and can cause physiologic dependence

-FLUMAZENIL is a benzodiazepine antagonist used to REVERSE benzo overdose

155
Q

tranquilizer is a drug that promotes tranquility by

A

calming, soothing, quieting, or pacifying WITHOUT sedation or depressant effects

major ones = anti-psychotics
minor ones = anti-anxiety (benzos)

156
Q

Benzodiazepines (minor tranquilizers)

how does it work? what nt?

bad effects are?

A

anti-anxiety, induce sleep (sedative-hypnotic), anti-convulsant, skeletal muscle relaxant

work by DEPRESSING LIMBIC SYSTEM and RETICULAR FORMATION through potentiation of GABA

adverse effects - CNS depression, GI disturbances, hypotension, ataxia, muscle relaxation, NEVER take with alcohol

157
Q

benzodiazepines taken orally are

A

chlordiaepoxide (librium)
lorazepam (ativan)
alprazolam (xanax)
diazepam (valium)

158
Q

benzodiazepines rx as HYPNOTICS for insomnia include

A
  1. Flurazepam (Dalmane)
  2. Temazepam
  3. Triazolam (Halcion) - metab by liver by P450 isoform CYP 3A4 (avoid in pts taking inhibitors for that); antifungals can also elevate triazolam levels
159
Q

Midazolam (versed)

A

a benzodiazepine in liquid form for pre-op sedation of kids, and injectable for IV.

NBDE II Board Busters (11 decks)

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