Pharmacology Exam Review

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Feb 22, 2014 (3 years and 3 months ago)

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Pharmacology Exam Review

Ch. 1


Chemical name
: chemical structure


Code name
: experiential drug


Generic name:
Assigned by United States
Adopted Name Council, drug shows therapeutic
use and the manufacturer wishes to market the
drug


Trade name:
brand name or proprietary name


Official name
: experiential drug becomes
approved, generic name becomes official name


Ch. 1


FDA:
approval of drugs, lengthy, costly, research
phases


Orphan drugs
: rare disease drug, fewer than
200,000 people


Prescription
: includes:


Name/address/date


Rx, superscription


Inscription


Subscription


Sig, signature


Name of prescriber

Ch. 1


OTC
: without prescription


Know abbreviations
: QID, BID, TID, Q4…



Ch. 2


Agonist
: drug binds to a receptor creates an
effect


Antagonist
: blocks receptor effect


Bioavailibility
: amount of drug available for
action in systemic system


Drug administration routes:


Enteral (GI), Parenteral (IV), Transdermal,
inhalation, topical


Ch. 2


First pass effect:
initial metabolism in the liver
of a drug taken orally before the drug reaches
the systemic system


Hypersensitivity
: allergic/immune mediated
reaction to a drug, can be serious requiring
mechanical ventilation


Idiosyncratic effect:
unexpected reaction to
drug, other than a allergic reaction


Ch. 2


Pharmacodynamics
: mechanism of drug
action by which drug molecule causes effect;
after kinetic phase


Pharmacokinetics
: time course and disposition
based on absorption, distribution,
metabolism,
eliminitaion


Pharmacogentics
: genetic factors, influence
drug response

Ch
.

2


Synergism:
combined effect greater than
individual


Tachyphylaxis
: rapid decrease in response to a
drug


Tolerance
: decreased intensity of a drug


Pinocytosis
: substance goes into a cell by
process of membrane engulfment and
transport of the substance into the cell

Ch. 2


Metabolism
: liver primary site of metabolism
and biotransformation


Excretion
: Kidney primary site


Receptors:
linked to G proteins, cause both
constriction and dilation from
epinphrine

or
Ach stimulation


Ch. 3


Aerodynamic diameter of a particle:
determines deposition in airway


Dead volume
: amount of solution that
remains in a SVN after sputtering


HFA:
hydrofluoroalkane
, propellant for MDIs


Spacer, reservoir and holding chambers

Ch. 3


Aerosol delivery:


Advantages:


Smaller doses, rapid onset, targeted delivery, fewer side
effects, painless, lung provides portal to body


Disadvantages:


Many variables, dose reproducibility, difficult
coordination, lack of knowledge, lack of standardized
info, varying devices

Ch. 3


Mass Median Aerodynamic Diameter (MMAD)


Indicates where the mass of drug is centered in a
distribution of particle sizes


>10
nasopharngeal

and
oropharyngeal

regions


5
-
10 microns: central airways


2
-
5 microns: lower airway (bronchodilator range)


0.8
-
3 microns: small airways, alveoli

Ch. 3


Mechanisms of Deposition


Inertial impaction
: function of particle size and
velocity and increases with larger size and higher
velocities


Gravitational settling
: sedimentation, particle size
and time


Diffusion (Brownian motion):
affects particles less
than 1 micron


Ch. 3


Devices: DPI, MDI, SVN, USN, SPAG


USN: electric powered, piezoelectric principle,


SPAG:
Ribavirn


SVN: gas powered, uses a baffle to disperse particles
to form aerosol from liquid


Time: 10
-
15 minutes, decreases with higher flows,
flow set at 6
-
8 liters, volume 3
-
5 ml.


Advantages of SVN: can nebulize many drugs,
mixtures, minimal coordination, useful in old/young,
low inspiratory flows, modifiable doses


Disadvantages: expensive/cumbersome,
Tx

time
lengthy, variability in performance, contamination

Ch. 3


BAN:
Aeroclipse
, undiluted meds, shorter
tx

times


MDI
: drug,
propellent
, canister, valve, and mouth
piece. HFA, portable/compact, short
tx

time, hard
to coordinate, difficult to assess depletion, large
oral impaction w/o holding chamber. Shake
canister if not used frequently, may prime device,
recommend spacer/holding chamber over open
mouth


Breath actuated inhalers
:
Maxair

Ch. 3


Holding chamber:
one way valve/spacer, holds
the aerosol cloud until inspiration occurs,
decreases waste and oral impaction, reduce
electrostatic charge, do not wipe inside.


DPI
: requires inspiratory flow of 30
-
90 L/min,
old/young may not be able to use


IPPB, Endotracheal tube administration, mask,
mouth piece.

Ch. 5


Ach
:
transmission stimulates
bronchoconstriction, muscle contraction.
Responds to
cholingergic
/nicotinic receptors.
Destroyed by cholinesterase. Blocked by anti
-
cholinergics
,
parasympatholytics


Adrenergic
: stimulates receptors for
norepinephrine/epinephrine. Beta agonist,
receptors alpha/betas, causes
bronchodilation
,
increased HR, alpha constriction

Ch. 5


Peripheral nervous system:
outside the CNS,
includes sensory/sympathetic and
parasympathetic nerves, Autonomic nervous
system (parasympathetic and sympathetic
branch)


Sympatholytic, sympathomimetic,
cholinergic, anticholinergic, antiadrenergic,
adrenergic,
parasympatholytic

Ch. 5


Efferent
: from brain to body


Afferent:
from body to brain


Cholinergic:
stimulated by Ach,
contraction…cholinesterase destroys
AcH


M1
-
3 in lungs, M3 when stimulated by Ach
causes constriction. M2 cholinesterase
decreases
AcH
.
Anticholinergics

block all M
receptors; all are G linked



Ch. 5


Anticholingerics
:


Atropine: blocks salivary glands, increases HR,
bronchodlation
, pupil construction


Atrovent


Tiotropium

Adrenergics
:


Alpha and Beta receptor stimulators (know what
each does)

Ch

6


Adrenergics
:
beta agonist, bronchodilators


Asthma paradox: increased asthma mortality
despite knowledge and
tachnology


cAMP
:
produced by Beta receptor stimulation,
from conversion of ATP by
adenly

cyclase


cGMP
: opposite effect of
cAMP
, causes
bronchoconstriction


Downregulation
: long term desensitization of
Beta receptors to beta agonists

Ch. 6


Fast acting
vs

long acting


Ultra short: Racemic, stridor/airway swelling


Adrenergics

are stereoisomers,
Levalbuterol

does
not have the S
-
isomer


Albuterol/Proventil/
ProAir
/
Ventoline


Beta receptors


SVN 0.5%
soln
, 0.5 ml, 2.5 mg, 0.63 mg, 1.25 mg,
TID/QID.


MDI (
proAIR
) 90
ug
/puff x 2 puffs


Onset 15 min, peak 30
-
60 min, duration 5
-
8 hours


Ch. 6


Beta 2 agonists cause:


Bronchial
smooth muscle relaxation


Inhibition of histamine release


Stimulation of
mucociliary

clearence


Are called
sympathomimimic

as they mimic
epinephrine, also called
adrenergics
, or beta
agonists


Adrenergic stimulation causes: Beta 1, Beta 2
and Alpha responses

Ch. 6


Racemic Epinephrine/
microNefrin
/Nephron


Alpha 1 and Beta receptors


Vasoconstriction for stridor


SVN 2.25% solution, 0.25
-
0.5 ml


Onset: 3
-
5 min, peak 5
-
20 min, duration: 0.5
-
2 hr


Increases HR,
bronchodilates

and
vasoconstricts


Side effects: HR increases, tremors, shakiness

Ch. 6


Levalbuterol
/
Xopenex


SVN: 0.31, 0.63, 1.25 mg TID


MDI: 45
ug
/puff x 2, q4
-
6


Same onset/peak/duration as albuterol


One less isomer than
albuterol

(no S
-
isomer)


Pure R
-
isomer of
racemic

albuterol


Side effects: tremor, less HR changes


Ch

6


Long acting (prophylactic)


Not for acute bronchospasm


Brovana
/
arfometerol
, SVN only


Formoterol
/
Foradil


Mixed with
Pulmicort

to make
symbicort


Dose 12
ug

BID


Salmeterol
/
Serevent


Mixed with
Flovent

to make
Advair


Dose DPI 50
ug
/BID


Onset 20 min, peak 5
-
6, duration 12
hrs




Ch. 6


Saligenin

agents
:
albuterol
, beta 2 preferential
drug


Short/long acting bronchodilators:
Have
antiinflammatory

effects, however not enough
to replace
antiinflammatory

drugs


Used in treatment of COPD, asthma


LABA prophylactic use, BID, stays attached to
beta receptor longer


Ch. 6

Mode of Action of
Adrenergics
:

Once attached to a β2 receptor in bronchial


smooth muscle the drug then attaches to the
intracellular Gs
protien

which stimulates
adenly

cyclase

to form
cAMP

from ATP which
then decreases Ca2+↓ and Myosin resulting
in SM relaxation .

Also activate β receptors on mast cell
mb
. ,


thus used in prophylaxis of allergic asthma .


Ch. 6


Side effects:


Tremor, palpitations, headache, insomnia,
nervousness, dizziness, nausea, tolerance, loss of
bronchoprotection
,
hypokalemia
;
downregulation


Routes of administration with
adrenergics
:


Continuous SVN: severe asthma, 10
-
15 mg an
hour of
albuterol


SVN route the best route


Ch. 6


Respiratory assessment with
adrenergics
:


Assess effectiveness; peak flows


Breath sound change


Vital signs


A 20% change in HR from baseline may warrant a
change in therapy


Check glucose, potassium levels


Device education

Ch. 7


Anticholinergics
:
only two used for the
inhalation route:


Atrovent

(
Ipatropium

Bromide), 0.5 mg SVN, MDI
dose


Spiriva

(
Tiotropium

Bromide),
handihaler

dry
powder


Both have little systemic side effects


Use one or the other. Used for COPD and also
during asthmatic attacks

Ch. 7


Combivent
:
Combo of
Atrovent

and
Albuterol

in a MDI


Duoneb
: Combo of
Albuterol

and
Atrovent

in a
SVN


Give combos for synergetic effect


Atropine:
No longer aerosolized, used to
increase HR, dry mouth. Tertiary compound,
means it crosses BBB has systemic effects

Ch. 7


Spiriva


DPI, 18
ug
/inhalation, given QD


Onset 30 min, peak 3hr, duration 24 hrs


Atrovent
:


MDI (HFA)17
ug
/puff x 2 puffs, QID


Onset 15 min, peak 1
-
2 hr, duration 4
-
6 hrs


SVN 0.02% solution, 0.5 mg TID



Ch. 7


Mode of action of
anticholinergics


cGMP

inhibits constriction and mucus production


cGMP

acts as a secondary messenger much like
cAMP

but
instead of converting ATP,
cGMP

prevents
neurotransmitters from entering the bronchial smooth
muscle cell


Unlike
sympathometic

bronchodilators,
Atrovent
/
Spiriva

do not cross the blood brain barrier and thus have
essentially no systemic side effects (both are derivatives
of Atropine, but are quaternary amines)


Slower bronchodilator effects and less intense than
adrenergics


Ch. 7


Atrovent

is non selective M blocker


Quaternary
compund
, does not cross the BBB


Spiriva
: dissociates more slowly from M1 and M3
receptors. More selective than
Atrovent


M2: inhibits further
AcH

release


Cholinergic effects:
decrease HR,
miosis
,
contraction of lens, salivation, urination,
secretion of mucus,
bronchoconstriction


AcH

destroyed by cholinesterase

Ch. 7


Anticholinergic

effects:
increased HR, pupil
dilation, flattened lens (USE CAUTION WITH
ATROVENT WITH patients with Glaucoma),
drying of upper airway, urinary retention,
antidiarrheal
,
mucociliary

slowing


Adverse effects:
dry mouth, cough, avoid
spraying in eye

Ch. 8


Methylxanthines
: derived from
Xanthines
,
consist of Caffeine,
theophylline
, and
theobromine


Phosphodiesterase
: enzyme that inhibits
cAMP
.
Xanthine

believed to inhibit this
enzyme, thus increasing
bronchodilation


Uses:
Apnea/
bradycardias
; most common use
of
Xanthine
, in form of
Caffiene

for neonates




Ch. 8


Uses:

COPD as a weak bronchodilator,
increasing respiratory muscle strength,
increases contractility for patients on long
term mechanical ventilation (helps with
diaphragm wasting); respiratory muscle
endurance, central
ventilatory

drive,
cardiovascular effects by increasing CO, and
antiinflammatory

effects


Ch. 8


Theophylline
: lots of side effects, must keep in
narrow therapeutic range, headache, anxiety,
restlessness, nausea, anorexia, vomiting,
abdomial

pain,
hematemesis
,
tachypnea
,
palpitations, SVT, ventricular arrhythmias,
hypotension,
diruresis


Ch. 9


Abhesives
:
coating of film that
preventsor

reduces adhesion


Elasticity:
rheologic

property characteristic of
solids it is represented by the storage of
modulus G


Expectorant
: medication meant to increase
the volume or hydration of airway secretions


Gel:
macromolecular description of pseudo
-
plastic material viscosity and elasticity

Ch. 9


Mucin
: principle airway gel forming
mucins


Mucoactive

agent
: effect on mucus secretion


Mucokinetic

agent:
increases
ciliary

clearance
or respiratory mucus



Mucolytic

agent:
degrades polymers in
secretions


Mucoregulatory

agent
: reduces volume of
airway mucus secretion and appears to be
especially effective in
hypersecretory

states

Ch. 9


Know layers of mucosa (gel, sol layer, epithelial cells, cilia,
goblet cells, bronchial glands
-

produce most mucus)


Produce 100 ml of mucus daily


Acetylcysteine

(NAC):
Mucomyst
, 10%/20%, SVN 3
-
5 ml


Causes
bronchospasm
, give with bronchodilator


Rotten egg smell, nausea


Directly instilled, or aerosolized


Breaks down
sulfhydryl

groups for disulfide bonds of mucus


Given to COPD, pneumonia, congestion, acetaminophen
overdose


Incompatible with anti
-
biotics

(do not mix
mucomyst
)

Ch. 9


Factors affecting mucus transport:


COPD/CF


Airway drying


Narcotics


Artificial airways/suctioning


Cigarette smoke


Pollution


Hyperoxia
/hypoxia


Ch. 9


Food intake (milk) in particular does not increase
mucus


Adrenergics
: increase cilia beat and mucus
production


Cholinergics
:

increase
ciliary

beat and mucus


Anticholinergics
:
decrease cilia beat and decrease
mucus production


Xanthines
:
increase cilia beat and production


Steroids:
no effects on cilia, decrease mucus
production

Ch. 9


Sputum:
mucus plus oral secretions


Bronchorrhea
:
watery sputum


Asthma:
inflammation/increased mucus
production


CF:
impaired proteins, get frequent infections
such as pseudomonas, require
Dornase

Alfa.
Most congestion is not
mucin
, instead puss
from
neutrophil

degradation

Ch. 9


Physical properties of mucus include viscosity,
elasticity, cohesion, and
adhesity
.


Dornase

Alfa:


Pulmozyme

dose 2.5 mg


Given during infections with CF


Reduces extracellular DNA and F
-
actin

polymers,
reduces viscosity and adhesiveness of mucus


Does not cause
bronchospasm
, may cause
pharyngitis
,
laryngitis, rash, chest pain, conjunctivitis



Ch. 9


Expectorants:


Sodium
Bicarb
:
increases pH of mucus weakening
bonds lowering viscosity and elasticity, used
directly or aerosolized. Weak


Guaifesnsin
:
cilitoxic

when applied directly


Hypertonic Saline
: >0.9%, for induction of cough


Use adjunct therapy for mucus control


PEP, CPT, IPPB, Heated humidity, postural drainage,
Bronchodilators, Vest


Bland aerosols (without medications)

Ch. 10


Surfactant agents regulate surface tension in
films at gas
-
liquid interfaces, described by
LaPlace’s

Law


Surfactants are used are prophylactic or
rescue treatment for RDS


Used exogenous surfactants include:


Beractant

(
Survanta
),
Calfactant

(
infasurf
),
Poractant

alfa

(
Curosurf
)

Ch. 10


Surfactant is directly instilled into the airway
via
endotracheal

tube and adaptor, must
closely monitor patient for compliance
changes in order to prevent
pneumothorax


Surfactants used are all natural based


Surfactant is composed of:


85
-
90% lipids and 10% Proteins


Exogenous surfactant enter into the alveolar pool
and replace deficient natural surfactant



Ch. 11


Adrenal cortical hormone:
chemicals secreted by
the adrenal cortex (steroids)


Endogenous
: made within body


Exogenous
: outside body


IgE
: immune antibody, increased with allergen


Prostglandin
: hormone type substances
circulating in body


Steroids:
Glucocorticoids

or corticosteroids,
antiinflammatory

effect


Ch. 11


Adrenal cortical hormones: adrenal cortex
secretes natural
antiinflammatories
. Secreted
at the
hypothlamic

pituritary

adrenal (HPA)
axis portion of the adrenal gland


Indications:


COPD


Asthma (moderate/severe persistent); must also
give a LABA with steroid. Commonly
Advair

or
Symbicort


Ch. 11


Corticosteroids secreted by the adrenal cortex
include
glucocorticoids

(
cortisol
),
minaerlocorticoids

(
aldosterone
), and the
androgen estrogen hormones


Beclomethasone
:


QVAR, MDI 40 or 80, 160
ug
/puff, BID


Rinse mouth after all steroids to prevent thrush

Ch. 11


Fluticasone

(
Flovent
);
MDI 44, 110 and 220
ug
/puff,
BID; DPI 50, 100, 250; combined with
Serevent

to make
Advair
, doses 500/50, 250/50, 100/50


Budesonide

(
Pulmicort
);
only
nebulized

steroid,
respules

SVN 0.25
-
0.5 mg;
tubahaler

DPI 200
ug
/actuation BID; mixed with
foradil

to make
Symbicort
, MDI doses 80/4.5, 160/4.5 BID


Mometasone

(
Asmanex
);
Twisthaler

DPI, 220
ug
; BID


Flunisolide

(
Aerospan
);


MDI 80
ug
/puff, BID

Ch. 11


Hypothalamic Pituitary Adrenal Axis (HPA):
controls endogenous steroids, may be
suppressed/affected with exogenous steroid use.
Cortisol

release causes breakdown of
carbohydrates, fats, and proteins to make glucose
for energy. Side effect of systemic steroid is
steroid diabetes


Diurnal Steroid Cycle
: levels of natural steroids
follow a daily or diurnal rhythm. Give exogenous
steroids following normal cycle of release


Ch. 11


Inflammatory response:
Redness, flare, wheal,
increased vascular permeability,
leukocytic

infiltration,
phagocytosis
, mediator cascade


Mode of action:
upregulation

of
antiinflammatory

proteins and
downregulation

of
proinflammatory

proteins


Systemic Steroids
(Prednisone/
Salmederol
), are
potent, given following or during COPD or asthma
exacerbation and several days after, continued
use leads to many side effects

Ch. 11


Systemic side effects:


HPA suppression


Immunosuppressant, WBC affected


Psychiatric reactions


Myopathy

of skeletal muscle


Fluid retention


Moon face, osteoporosis


Increased WBC


Increased glucose levels


Ch. 11


Minimize oral side effects with use of holding
chamber, rinsing mouth after use


Inhaled steroids may cause oral
candidiasis

(thrush), hoarseness, cough,
bronchoconstriction

Ch. 12


Antiluekotrienes
:
agents that block
inflammatory mediators, do not prevent mast
cell
degranulation


Mast cell inhibitors
: prevent
degranulation
, do
not stop mediators once release


Both used in extrinsic asthma as a
prophylactic treatment; typically mild or
moderate persistent asthma

Ch. 12


Allergic response in airway caused by
IgE

mediated mast cell release of mediators


Cromolyn

sodium
(
Intal
); MDI 800
ug
/actuation,
SVN 20 mg QID


Nedocromil

sodium
(
Tilade
); MDI 1.75
mg/actuation QID


Leukotrienes
:
Zafirkulast

(
accolate
),
Montelukast

(
Sinuglair
),
Zileuton

(
Zyflo
); ALL tablets


Omalizumab

(
Xolair
):
allergy shot, Q
-

every 4
weeks

Ch. 12


MOA of
Intal
: inhibits mediator release by
preventing calcium influx necessary for extrusion
of mast cell


Intal

has no antagonist effect on chemical
mediators themselves


Does not operate through
cAMP

system, no
bronchodilation


Does not prevent
Ige

antibody formation on Mast
cell


Do not replace inhaled steroids with mast cell
inhibitors suddenly as the HPA will be affected

Ch. 12


Tilade
: prevents mast cell release but also
esionphil
, histamine,
trypase

and others


Can inhibit
esionphil

chemotaxis

and adhesion

Ch. 13


PCP:
interstitial plasma cell pneumonia
affecting
immunocompromised
, particularly
HIV/AIDS.


Pentamindine

(
Nebupent
)
indicated as a
prophylactic for patients susceptible to PCP.
Should be given once a month in a scavenger
nebulizer, 300 mg in 6ml water


Know side effects of each
antiinfective


Ch. 13


Ribavirn

(
Virazole
):
for treatment of RSV/
Hep

C, given with SPAG, multiple side effects


Tobramycin

(
Tobi
),
300 mg, for CF patients, or
anyone with pseudomonas. Strict dosing and
frequency
requirments


Zanamivir

(
relenza
):
influenza


Amphotericin

B:
antifungal drugs is indicated
after a lung transplant



Extra Credit will come from


Ch. 14


General pharmacology