drug list Flashcards
1
Q
what’s the first antisense drug to be approved by FDA?
A
vitravene
2
Q
what’s used in the treatment of CMV retinitis?
A
vitravene
3
Q
what is only effective in about 20% of patients that overexposes HER2 receptor?
A
Herceptin
4
Q
Herceptin aka
A
trastuzamab
5
Q
what is a metastatic breast cancer treatment ?
A
Herceptin
6
Q
what drug may lead to cardio toxicity and ADRs?
A
Herceptin
7
Q
following patient testing what’s one of the first drugs to be prescribed for patients with breast cancer?
A
Herceptin
8
Q
what are the two MOA of Herceptin?
A
1 prevent HER2 receptor from releasing growth signals
2 it will tell your immune cells to target cells with HER@ receptor
9
Q
what happens in the absence of Herceptin?
A
HER2 cancer cells release excess growth signals for proliferation
10
Q
what drug is metabolized by isoenzyme CYP2D6?
A
debrisoquine
11
Q
what kind of drug is debrisoquine?
A
antihypertensive
12
Q
what alter metabolism of debrisoquine?
A
SNPs in the isoenzyme
13
Q
what drugs follow zero order kinetics?
A
ethanol and aspirin
14
Q
ethanol is excreted in …
A
sweat
15
Q
what’s penicillin?
A
an acidic antibiotic
16
Q
how are penicillin and aspirin excreted?
A
via proximal tubular secretion (renal excretion)
17
Q
what is used in the excretion of penicillin and aspirin?
A
anion transport system
18
Q
what may prolong effects of penicillin?
A
competition for secretion with probenecid
19
Q
what is aspirin?
A
acidic salicylate
20
Q
what is given to prevent gout?
A
aspirin is given to compete with uric acid during distal tubular active reabsorption
21
Q
what drugs are alkylating agents ?
A
cyclophosphamide and thio-TEPA
22
Q
cyclophosphamide and thio-TEPA MOA
A
creates highly reactive carbonium ion which alkylates guanine at N-7 position
23
Q
what prodrug is acts on S/G2 phase and G2/M phase?
A
cyclophosphamide
24
Q
what activates cyclophosphamide?
A
CYTP450
25
what drug is used for treatment of chronic lymphatic leukemia?
cyclophosphamide
26
what drug is used for treatment of breast and ovarian cancer?
cyclophosphamide
27
what drug is used in the management of rheumatic disorders and autoimmune nephritis?
cyclophosphamide
28
what are the adverse effects associated with cyclophosphamide and thio-TEPA ?
myelosuppression
nausea and vomitting
teratogenesis
gonadal atrophy
29
what drugs carry risk of leukomegenesis and resistance?
cyclophosphamide and thio-TEPA
30
what drug is aka as ethyleneammonium?
thio-TEPA
31
how is thio-TEPA activated?
its converted into its active metabolite try ethylene phosphor amide by liver MFO
32
what's used in the treatment of bladder cancer?
thio-TEPA
33
what are antimetabolites used to treat cancer?
methotrexate (MTX) and 5-fluorouracil (5-FU)
34
what drug is a folic acid antagonist?
methotrexate (MTX)
35
what does methotrexate (MTX) do?
irreversibly inhibits DHFR which is needed for thymidine and purine synthesis
36
what drug is a prymidine antagonist?
5-fluorouracil (5-FU)
37
what drug is a thymine analogue that has a fluorine group instead of a methyl group?
5-fluorouracil (5-FU)
38
what does 5-fluorouracil (5-FU) do?
its active metabolite 5-dUMP inhibits DNA synthesis and 5-dUTP when incorporated into RNA prevents its function
39
what's used in treatment of solid tumors?
5-fluorouracil (5-FU)
40
what's used in treatment of breast tumors?
5-fluorouracil (5-FU)
41
what's used in collateral tumors and gastric tumors?
5-fluorouracil (5-FU)
42
what's used in the treatment of squamous cell tumors of the head and neck?
5-fluorouracil (5-FU)
43
what are adverse effects of methotrexate (MTX) and 5-fluorouracil (5-FU)?
```
myelosuppresion
severe leukopenia
bone marrow aplasia
hepatotoxicity
thrombocytopenia
gi disturbances
crystal urea
```
44
what drugs are G1/S and S/G2 specific?
methotrexate (MTX) and 5-fluorouracil (5-FU)
45
what drugs intercalate btwn bps --> topoismoerase ii inhibited and free radicals fare formed --> inhibition of. dna synthesis and cause strand incision?
Doxorubicin and Actinomycin D
46
what drug is an anthracycline?
Doxorubicin
47
how does Doxorubicin work?
```
It gets reduced by CYTP450
reductase into a reduced
metabolite and a
superoxide ion hydrogen
peroxide, which breaks the
strands in DNA
```
48
what drugs may lead to severe cardiac toxicity and serious pulmonary and mucocutaneous reactions because of their free radical formation?
Doxorubicin and Actinomycin D
49
what are the adverse effects of Doxorubicin and Actinomycin D?
Cardiac toxicity
Severe pulmonary and mucocutaneous reactions
Bone marrow depression
Severe and prolonged Myelosuppression
Total alopecia
50
It is a cell cycle specific
| drug: G1/S and G2/M
Actinomycin D
51
It’s used to treat
gestational and pediatric
tumors (Ewing Sarcoma
and Wilms Tumor)
Actinomycin D
52
It intercalates DNA and
inhibits DNA and mRNA
synthesis.
Actinomycin D
53
what drug causes excess hypotension in poor metabolizers ?
Debrisoquine
54
what drug is an antidepressant?
paroxetine
55
what affects response of paroxetine?
Its response is affected by
SNPs in the Serotonin 2A
receptor.
56
whats the purpose of paroxetine?
It is a serotonin reuptake
| inhibitor.
57
what was found in patients taking paroxetine?
```
They found that depressed
patients with the C/C
genotype for the serotonin
2A receptor were more
likely to discontinue the
use of Paroxetine then the
T/C and T/T genotype.
```
58
name an endogenous adrenergic
| agonist
nora
59
what are the Direct-acting adrenergic
| agonist?
```
Nora
phenylephrine
clonidine
isoprenaline
dobutamine
salbutamol
```
60
what receptors does NA act on?
alpha 1 and alpha 2
61
NA is a catecholamine what does that mean?
can't be ingested orally bc it will be digested by MAO and COMT before it reaches systemic circulation ( short DOA)
cannot pass the BBB so minimal effect on CNS
62
what blocks release of NA from presynaptic neuron?
guanthedine
63
what direct acting adrenergic agonists are sympathomimetic?
phenylephrine
clonidine
dobutamine
salbutamol
64
true or false phenylephrine can be given orally.
true
65
what drug is a selective alpha 1 adrenergic agonist?
phenylephrine
66
what drug causes vasoconstriction?
phenylephrine
67
what drug is used as a nasal decongestant?
phenylephrine
68
why is phenylephrine used as a nasal decongestant?
acts on alpha 1 receptors on bvs of nasal mucosa to relieve congestion by inducing vasoconstriction
69
what is a selective alpha 2 adrenergic agonist ?
clonidine
70
what is used to treat hypertension by inhibiting sympathetic outflow leading to decreased blood pressure?
clonidine
71
what inhibits NA release ?
clonidine
72
what drugs are catecholamines ?
NA
| isoprenaline
73
what drug is a nonselective beta agonist?
isoprenaline
74
what is the effect when isoprenaline acts on B1 receptors?
increase renin release and contractility and rate of heart
75
what is the effect when isoprenaline acts on B2 receptors?
bronchodilation and peripheral vasodilation
76
what drug is a selective b1 adrenergic agonist?
dobutamine
77
what drug increases cardiac output and contractility of heart?
dobutamine
78
whats useful in Tx of CHF by increasing cardiac output?
dobutamine
79
how does dobutamine indirectly increase heart rate?
increase release of renin from kidneys promoting release of angiotensin II which brings up heart rate
80
what drug is a selective B2 adrenergic agonist?
salbutamol
81
whats used in the treatment of asthma for its bronchodilator effect?
salbutamol
82
whats used in the treatment of premature labor because it relaxes the smooth muscles of the uterus?
salbutamol
83
what drug is a nonselective alpha adrenergic blocker?
phentolamine
84
whats used to treat hypertensive crisis cause by phaeochromocytoma?
phentolamine
85
phentolamine ...... until tumor ( phaeochromocytoma) is removed.
release of catecholamines
86
whats a selective alpha 1 adrenergic antagonist ?
prazosin
87
whats used in treatment of primary hypertension?
prazosin
88
what is used to treat benign symptoms of prostatic hyperplasia?
prazosin
89
how does prazosin treat benign symptoms of prostatic hyperplasia?
prevents contraction of urinary smooth muscles and bladder neck allowing urine to pass easily and reducing lower UT symptoms
90
what drug is a nonselective beta antagonists?
propranolol
91
It is a selective B1
| adrenergic agonist
Dobutamine
92
It increases the cardiac
output and contractility of
the heart.
Dobutamine
93
• It is useful in the
treatment of CHF by
increasing the CO.
Dobutamine
94
```
It also can increase the
release of renin from the
kidneys promoting the
release of angiotensin II
which brings up the heart
rate.
```
Dobutamine
95
It is a selective B2
| adrenergic agonist
Salbutamol
96
```
Used in the treatment of
Asthma for its
bronchodilator effect and
in the treatment of
premature labor (relaxes
the smooth muscles of the
uterus).
```
Salbutamol
97
```
Non
-selective alpha
-
adrenergic blocker (Acts
on both alpha 1 and alpha
2)
```
Phentolamine
98
```
It is used to treat
hypertensive crises caused
by phaeochromocytoma
(which is a tumor of the
adrenal glands that
secretes excess
catecholamines)
```
Phentolamine
99
__________ prevents
the release of
catecholamines until the
tumor is removed.
Phentolamine
100
Selective alpha 1
| adrenergic antagonist
Prazosin
101
It is useful in the
treatment of primary
hypertension.
Prazosin
102
```
It is used to treat
symptoms of benign
prostatic hyperplasia. It
prevents contractions of
the urinary smooth
muscles and bladder neck
allowing the urine to pass
easily and reducing lower
UT symptoms.
```
Prazosin
103
```
Non
-selective beta
-
adrenergic antagonist
(blocks beta 1 and beta 2).
```
Propranolol
104
• It blocks the effects of
catecholamines on the
heart and blood vessels.
Propranolol
105
```
Is used to treat angina
pectoris
- chest pain caused
by lack of O2 to the heart
(because of increased
blood flow). _________
decreases the CO and BP
allowing time for the blood
to pass through the heart.
```
Propranolol
106
```
Considered as a first line
treatment for
hypertension and can be
used in combination with
other blood pressure
lowering drugs to
maximize the affect.
```
Propranolol
107
```
It is also proven to have a
protective affect in
patients who have had a
MI (prevents them from
getting it a second time so
its protective on the heart)
```
Propranolol
108
```
It is also used in the
treatment of
hyperthyroidism (which
can cause tachycardia and
anxiety)
```
Propranolol
109
It can also decrease the bp
by decreasing the CO and
renin release.
Propranolol
110
AE: Since it is non
-selective
it may cause
bronchospasm in patients
who have asthma.
Propranolol
111
AE: It may also lead to
cardiac depression and
signs of HF.
Propranolol
112
```
It is used in the treatment
of hypertension and may
be used in combo with
other blood pressure
lowering drugs.
```
Atenolol
113
used in the
treatment of angina
pectoris.
Atenolol
114
It is used to treat MI
| protective effect
Atenolol
115
used to treat
| hyperthyroidism
Atenolol
116
AE : cardiac depression and HF
Atenolol
117
• It also decreases bp by
decreasing the CO and
renin release.
Atenolol
118
It blocks the effect of
catecholamines on the
heart and blood vessels.
Atenolol
119
Indirect acting adrenergic agonists
```
cocaine
tricyclic antidepressants
amphetamine
tyramine
MAO inhibitors
```
120
direct acting adrenergic agonists
dopamine
epinephrine
isoproterenol
121
mixed action adrenergic agonists
ephedrine
122
It inhibits neuronal uptake
| uptake 1
cocaine
| tricyclic antidepressant
123
```
It increases the amount of
NA in synaptic gap and
thus promotes increased
activation of adrenergic
receptors (both
```
cocaine
| tricyclic antidepressant
124
tricyclic antidepressant
Imiprimane
125
It blocks the release of NA
| into synaptic space.
Guanethidine
126
Noradrenergic neuron
| blocking drug
Guanethidine
127
Drugs that act on
noradrenergic nerve
terminals
Reserpine
128
It blocks the transport of
NA into synaptic vesicles,
thus depleting the stores.
Reserpine
129
It is not used clinically.
Reserpine
130
```
It does not bind to a
receptor instead it
displaces NA from the
vesicles to cause NA
release.
```
Amphetamine
131
```
MOA: it enters the nerve
terminal via uptake 1 and
enters the synaptic vesicle
in exchange for NA. This
causes NA to accumulate
presynaptically and some
of it will be broken down
by MAO, while the rest of
it will be released into the
synaptic cleft to act on
adrenergic receptors.
```
Amphetamine
132
It acts in a similar way to
amphetamine (ya3ny it
displaces NA from its
vesicle)
Tyramine
133
It can cause severe
hypertension in patients
who take MAO inhibitors.
Tyramine
134
It is naturally broken down
by MAO (you can see why
MAO inhibitors are a
problem)
Tyramine
135
A protein found in cheese
| products
Tyramine
136
It is involved in the cheese
| reaction.
Tyramine
137
```
Mixed acting adrenergic
agonist (ya3ny it can
increase the amount of NA
released or it can bind to
the receptors and activate
them directly)
```
Ephedrine
138
Non-catecholamine
Ephedrine
139
It is the major
neurotransmitter of the
PSNS
Acetylcholine
140
It is an endogenous and direct acting
| cholinergic agonist
Acetylcholine
141
It is involved in the PSNS and
acts on nicotinic or
muscarinic receptors.
Acetylcholine
142
Typically acts on skeletal
muscles in the somatic
efferent pathway
Acetylcholine
143
```
It is the major
neurotransmitter in all
presynaptic neurons of the
PNS and is only active in the
PSNS post-synaptically.
```
Acetylcholine
144
Heart: decreases CO
and rate of the heart
Blood vessels:
vasodilation and
decreased blood
pressure
Acetylcholine
145
GI: stimulates
salivary and
intestinal secretion
and gastric motility
Acetylcholine
146
Lungs: it induces
bronchiolar
secretion and
bronchoconstriction.
Acetylcholine
147
```
Genitourinary tract:
it increases the
detrusor urinae
muscle tone for
expulsion of urine.
```
Acetylcholine
148
Eye: muscle
contraction for near
vision and pupil
constriction (miosis)
Acetylcholine
149
It is broken down by
| acetylcholinesterase
Acetylcholine
150
It activates all cholinergic
receptors (muscarinic and
nicotinic receptors)
Acetylcholine
151
```
It is not used therapeutically
because of its multiplicity of
action and its rapid
degradation by
acetylcholinesterase.
```
Acetylcholine
152
It is a type of choline ester
(direct
-acting cholinergic
agonist)
Acetylcholine
153
It is only clinically used for its
miotic effects in cataract
surgery.
Acetylcholine
154
It is contraindicated in: People with coronary
insufficiency because it causes hypotension
and people with Hyperthyroidism
(atrial arrythmias)
Acetylcholine
155
It is contraindicated in: People with Asthma or Peptic ulcers
Acetylcholine
156
It is an alkaloid found in
| Atropa Belladona
Atropine
157
```
It blocks all types of
muscarinic receptors (It does
not affect nicotinic receptors)
```
Atropine
158
At low doses it has no effect
| on the CNS
Atropine
159
```
At high doses it causes
excitation effects on the CNS
(hallucinations,
disorientation, and
restlessness)
```
Atropine
160
It is a cholinergic
antagonist --> binds competitively and
reversibly
Atropine
161
```
Eye: mydriasis
(persistent)
Antispasmodic:
relaxes GIT and
bladder
```
Atropine
162
```
Antisecretory: it
prevents secretion
from upper and
lower respiratory
tract prior to
surgery
```
Atropine
163
surgery
o Used to treat
anticholinesterase
Atropine
164
```
Adverse effects:
Dry mouth
Blurred vision
Tachycardia
Constipation
Confusion (CNS)
```
Atropine
165
in surgery its used as a pre anesthetic to prevent salivary and bronchiolar secretions
Atropine
166
```
Ophthalmology: It is
used to induce
mydriasis, to dilate
the pupil, and
paralyze the eye
lens for examination
(long
-lasting effects)
```
Atropine
167
Antidote: treatment
of
anticholinesterase
poisoning
Atropine
168
Treatment of GIT
| cramps
Atropine
169
Treatment of
Parkinson’s disease
and tardive
dyskinesia
Atropine
170
Treatment of sinus
bradycardia after an
MI
Atropine
171
Its use is contraindicated in
children because it increases
their body temperature.
Atropine
172
It can be used in conjunction
with pralidoxime to treat
organophosphate poisoning.
Atropine
173
It is used in the treatment of
Parkinsonism and tardive
dyskinesia
Benztropine
174
It is a cholinergic
antagonist that only acts on muscarinic
receptors
Benztropine
175
It blocks the release of
acetylcholine from the
presynaptic cholinergic
neurons.
Botulinum Toxin
176
A bacterial toxin
Botulinum Toxin
177
It is an indirect
| -acting cholinergic agonist and anticholinesterase
Echothiophate
178
It is an organophosphate
Echothiophate
179
It is irreversible and long
| -acting
Echothiophate
180
Typically used in the
preparation of war gases and
pesticides
Echothiophate
181
It may be used to treat
glaucoma (but not as a first
choice).
Echothiophate
182
```
what causes these side effects?
Respiratory
depression (very
dangerous)
Agitation
Confusion
Vomiting, colic, and
diarrhea
```
Echothiophate
183
```
what causes these side effects?
Constricted pupils
that are unresponsive to light
Sweating and salivation
Bronchoconstriction
```
Echothiophate
184
```
what causes this side effects?
CNS: It may cause
demyelination,
which causes
sensory loss and
respiratory
paralysis.
```
Echothiophate
185
When used in combo with a
NMB it may lead to
prolonged and excessive
muscular (skeletal) paralysis
Gentamicin
186
It prevents the release of
| acetylcholine
Gentamicin
187
It may be used in combo with
vecuronium= blocks nicotinic
receptors
Gentamicin
188
its an Aminoglycoside
Gentamicin
189
```
Blocks the choline uptake
(rate limiting step) (prevents
the entry of choline to the
presynaptic membrane via
choline carrier) → inhibits
acetylcholine synthesis →
Blocks cholinergic
transmission.
```
Hemicholinum
190
Blocker of Cholinergic
| transmission
Hemicholinum
191
Cholinergic antagonist acts on muscarinic
| receptors
Ipratropium
192
It is a quaternary nitrogen
| compound
Ipratropium
193
Used to treat chronic
bronchitis and asthma; it
relaxes smooth muscles.
Ipratropium
194
It binds competitively and
reversibly
It is inhaled
Ipratropium
195
```
It inhibits plasma
cholinesterases from
metabolizing another NMB=
Suxamethonium (prolonging
its duration of action)
```
Neostigmine
196
Reversible and long
-acting
anticholinesterase
Neostigmine
197
It is used to reverse
| competitive NMB
Neostigmine
198
Used in the treatment of
paralytic ileus and bladder
atony
Neostigmine
199
It is also used in the
treatment of myasthenia
gravis
Neostigmine
200
```
It leads to the AE mentioned
earlier for
anticholinesterases (all
except confusion, agitation,
and respiratory depression)
```
Neostigmine
201
Used to treat glaucoma
because it’s only
administered on the eyes
Physostigmine
202
Used as an antidote for
| atropine poisoning
Physostigmine
203
Used in the treatment of
| Alzheimer’s disease
Physostigmine
204
```
It may cause agitation,
confusion and respiratory
depression (along with the
other side effects on
anticholinesterases)
```
Physostigmine
205
It is a naturally occurring
| alkaloid
Pilocarpine
206
It has a longer DOA than
acetylcholine
It specifically acts on
muscarinic receptors
Pilocarpine
207
used to treat glaucoma
Pilocarpine
208
```
contraindicated in the following : -
Coronary insufficiency (hypotension)
Hyperthyroidism
(atrial arrythmias)
Peptic ulcer
Asthma
```
Pilocarpine
209
At therapeutic dose it is a
depressant in the CNS: it
leads to sedation, drowsiness
and amnesia
Scopolamine
210
It is also an antiemetic • It has a longer DOA than
| acetylcholine
Scopolamine
211
It also has a greater overall
effect on the CNS than
acetylcholine
Scopolamine
212
```
AKA: Hyoscine
It’s another type of plant
product
It is a muscarinic
antagonist
```
Scopolamine
213
It is used in the treatment of motion sickness
Scopolamine
214
It is uses as a
adjunct with
anesthesia
Scopolamine
215
```
It also blocks short
term memory
(useful so that the
patient can’t
remember the
surgery)
```
Scopolamine
216
AE: very similar to Atropine
```
dry mouth
blurred vusuin
constipation
tachycardia
confusion
```
Scopolamine
217
in Surgery: it is used as a pre-anesthetic to prevent salivary and bronchiolar secretions
Scopolamine
218
It is also used in the
treatment of GIT
cramps.
Scopolamine
219
Blocks the storage of
| acetylcholine
Vesamicol
220
Blocker of cholinergic
| transmission
Vesamicol
221
```
It has a longer DOA than
acetylcholine
It is selective to muscarinic
receptors
It is used to treat paralytic
ileus and urinary retention
```
Bethanechol
222
Direct-acting cholinergic agonist
It is a choline ester
(synthetic ester of
choline)
Bethanechol
223
It increases the release of
acetylcholine from
presynaptic cholinergic
neurons
Latrotoxin
224
It is also found in spider
venom
• Typically known as Black
Widow Toxin
Latrotoxin
225
It is used in the treatment of
| organophosphate poisoning
Pralidoxime
226
May be used in conjugation
with Atropine
• It reactivates cholinesterases
Pralidoxime
227
• Oxime compound
Pralidoxime
228
Reactivates enzymes
inactivated by
phosphorylation.
Pralidoxime
229
It is a competitive NMB
| It is non-depolarizing
```
Suxamethonium
Rocuronium
Mivacurium
Tubocurarine
Vecuronium
```
230
```
It competes with
acetylcholine to bind to
nicotinic receptors
• It is clinically important
• It is an active drug
```
Mivacurium
231
It is useful in patients
suffering from kidney
disease because it cannot
be excreted by the kidneys
Mivacurium
232
It is rapidly hydrolyzed by
plasma cholinesterase
(short acting)
Mivacurium
233
```
Only causes mild or
transient histamine
release and hypotension
No effect on muscarinic
receptors
```
Mivacurium
234
```
It is of clinically important
use
• It has an intermediate
duration of action (30-40
minutes).
```
Rocuronium
235
It has no ganglionic block
or histamine release
• It does not act on
muscarinic receptors
Rocuronium
236
No tachycardia
| • Its onset is rapid (1 -2 minutes)
Rocuronium
237
```
It is used in
electroconvulsive therapy
to reduce trauma
• It is also used in rapid
endotracheal intubation.
```
Suxamethonium
238
```
It is used in
electroconvulsive therapy
to reduce trauma
• It is also used in rapid
endotracheal intubation.
```
Suxamethonium
239
It is the only depolarizing
NMB used clinically.
Its onset of action is rapid
(1 minute).
Suxamethonium
240
```
MOA: It behaves like
acetylcholine; it binds to
the nicotinic receptor and
induces contraction.
However, it is not
susceptible to
acetylcholinesterases. This
means that it persists for a
longer period of time on
the receptor leading to
sustained muscular
contraction and
depolarization that leads
to inactivation of the
receptor and relaxation of
the muscle. It actually
produces transient
twitching (fasciculation)
before causing the block.
```
Suxamethonium
241
```
It is short acting in its
nature (5 minutes) as it is
digested rapidly by plasma
cholinesterases. However,
at the NMJ it must be
redistributed to the
plasma (no plasma
cholinesterases at the
NMJ)
```
Suxamethonium
242
```
Its use is contraindicated
in people with a deficiency
or defective plasma
cholinesterases because its
duration of action is
prolonged (prolonged
neuromuscular paralysis)
```
Suxamethonium
243
```
AE associated with
o Depression of
respiration
o Post -operative pain
o Hyperkalemia which can cause cardiac arrythmias
o Malignant hyperthermia
o Prolonged muscle paralysis and apnea (in plasma
cholinesterase deficient
patients= paralyzes diaphragm)
```
Suxamethonium
244
```
side effects = Bradycardia
(muscarinic
agonist effect)
o Increased
intraocular
pressure
(nicotinic agonist
effect on
extraocular
muscles)
```
Suxamethonium
245
```
Its effect can be enhanced
by neostigmine blocking
the plasma cholinesterases
as it is a an
anticholinesterase
```
Suxamethonium
246
Non -competitive NMB
• It is depolarizing in its
nature
• AKA: succinylcholine
Suxamethonium
247
Competitive NMB • Non-depolarizing • Alkaloid
Tubocurarine
248
It is a prototype • It is not clinically used
because of its lack of
selectivity and multiple
side effects
Tubocurarine
249
```
It leads to histamine
release, which causes
bronchoconstriction and
and hypotension
• It also leads to ganglionic
block
```
Tubocurarine
250
It is only important
because it was one of the
first NMB to ever be
introduced to medicine
Tubocurarine
251
It is clinically important
It has an intermediate duration of action (30-40 minutes)
It has a rapid onset ( 1-2 minutes)
Vecuronium
252
It does not promote
histamine release
It does not cause ganglionic block (so it doesn’t act on muscarinic receptors= no tachycardia)
Vecuronium
253
It may lead to prolonged
muscle paralysis when
administered with
gentamicin.
Vecuronium
254
```
It is used against gram -ve
bacteria.
It is bactericidal against
streptococci but
bacteriostatic against
enterococci.
```
Penicillins
255
Some bacteria produce B-
lactamase and are
resistant to it
Penicillins
256
Closely related to penicillin
• Some bacteria that
produce B-lactamase are
also resistant
Cephalosporins
257
If a patient has an allergy
towards penicillin= he
should not take it
Cephalosporins
258
It may cause kidney
| damage.
Cephalosporins
259
They inhibit folic acid
synthesis
They cause kernicterus in
neonates
Sulfonamides
260
During pregnancy, they
lead to neonatal jaundice
and hemolytic anemia
Sulfonamides
261
They prevent bacterial
DNA synthesis (since they
need folic acid for
synthesis)
Sulfonamides
262
It interferes with cell
division (selective toxicity
to bacteria and not
humans)
Sulfonamides
263
It is prototypic of
Sulfonamides
```
• It is active against gram
+ve and
-ve bacteria
• It helped overcome an
outbreak of meningitis
• It also inhibits folic acid
synthesis in bacteria
```
Sulfanilamide
264
```
Prototypic of an
aminoglycoside
• It was especially designed
against the penicillin
resistant gram-ve bacteria
```
Streptomycin
265
It inhibits the 30s
ribosomal subunit in
bacterial species= inhibits
protein synthesis
Streptomycin
266
```
Since its an
aminoglycoside, it requires
an oxygen dependent
transport mechanism=
anaerobes are inherently
resistant to it
```
Streptomycin
267
```
Some bacteria, becomes
resistant to it
because their DNA is
altered= Ribosome
altered.
• It may lead to kidney
damage in the fetus and
hearing problems.
```
Streptomycin
268
```
Their uptake may be
reduced by bacterial
mechanisms which
promote the outflux of
antibiotics.
• They are used as a
bacteriostatic agent in
pneumococcal infections
```
Tetracyclines
269
In pregnancy and
breastfeeding= weak bone
and teeth formation
Tetracyclines
270
```
Isolated from
streptomyces organism
• It is active against gram
+ve and
-ve bacteria,
ricketssia, and some
protozoa
```
Chlortetracycline
271
```
It is active against gram
-ve and gram +ve bacteria
• It was found to cause
aplastic anemia, so it is not
widely used anymore
(unless person is resistant
to other drugs)
```
Chloramphenicol
272
```
It inhibits the 50s
ribosomal subunit of
bacteria (inhibiting protein
synthesis)
• It may cause gray baby
syndrome
• It is metabolized by the
liver (may lead to toxicity
in those patients who have
liver damage)
```
Chloramphenicol
273
Metabolized by liver
enzymes and may lead to
toxicity if liver function is
impaired
Erythromycin
Clarithromycin
Rifampin
274
```
Leads to kidney damage
and hearing problems
when taken in pregnancy
and breast feeding
• Anaerobes are resistant to
it because it requires an
oxygen dependent
transport mechanism
```
Aminoglycosides
275
Vinka Alkaloids (Taxens= have the
```
same MOA= prevent
polymerization)
MOA: They are tubulin
-binding agents
- arrest the cell in G2/M
phase by preventing the formation
of the mitotic filament for nuclear
and cell division
```
Vinblastine
276
It is obtained from the
Vinca Rosa
• It’s mostly used in combo
with other drugs
Vinblastine
277
It’s used with cisplatin and
bleomycin = to treat
metastatic testicular and
prostate cancer.
Vinblastine
278
AE:
Severe neurotoxicity
Foot drop
Ataxia
Vinblastine
| Vincristine
279
```
It is obtained from the
Vinca Rosa
• It is often used in combo
with other drugs
• It is used with prednisone=
treats childhood leukemia
```
Vincristine
280
It is used against a wide
range of neoplasms.
• It’s a cell cycle non-specific drug
Cisplatin
281
MOA: They bind to guanine in DNA
| and RNA and the interaction is stabilized by hydrogen bonding, which causes unwinding and shortening of the DNA helix.
Cisplatin
| Carboplatin
282
```
It is given intravenously as
a first line treatment for:
o Testicular cancer
o Ovarian cancer
o Bladder cancer
o Melanoma
o And a number of
other solid tumors
```
Cisplatin
283
```
AE:
o Severe nausea
o Nephrotoxicity
o Vomiting
o Little
myelosuppression.
```
Cisplatin
| Carboplatin
284
```
Used in the treatment of a
wide variety of neoplasms
• It has a similar spectrum of
action to cisplatin.
However, it is only used as
a second-line drug for
ovarian cancer.
```
Carboplatin
285
```
Estrogen
• It inhibits the effects of
endogenous androgens
• It is used in the treatment
of androgen-dependent
metastatic prostatic
carcinoma
```
Diethylstilbestrol
286
Hormone
MOA: Several types of hormone-
dependent cancers respond to their antagonist hormones as treatment.
Diethylstilbestrol
Fluoxymesterone
Tamoxifen
Anastrozole
287
```
AE:
o CVD=
cerebrovascular
and cardiac
complications
o Male breast
carcinoma
```
Diethylstilbestrol
288
```
Androgen
• It’s MOA in breast cancer is
very similar to estrogens
• AE:
o Hepatic toxicity
o Virilizing effects
```
Fluoxymesterone
289
Sex hormone antagonist
• It antagonizes the ERs of
estrogen sensitive cancer
cells
Tamoxifen
290
```
It is used in the treatment
of ER sensitive breast
carcinomas and progestin
resistant endometrial
cancer
```
Tamoxifen
291
```
AE:
o Hot flushes
o Venous
thrombosis
o Vaginal bleeding
```
Tamoxifen
292
```
Aromatase inhibitor
• The aromatase reaction is
responsible for the extra-
adrenal estrogen synthesis
from androstenedione in
post-menstrual women.
```
Anastrozole
293
```
It is used as a first line
treatment for breast cancer
in post-menopausal women
to decrease estrogen
production.
```
Anastrozole
294
AE:
o Bone pain
o Peripheral edema
Anastrozole
295
```
There are many neoplastic
cells that require
asparagine to grow faster.
• L-asparaginase catalyzes
the deamination of
Asparagine to aspartate
and ammonia.
```
Asparaginase
296
```
It is used in the treatment
of childhood acute
lymphatic leukemia (in
combo therapy)
• AE: Acute Pancreatitis
```
Asparaginase
297
```
It is used as an inhibitor of
the tyrosine kinase activity
of the protein product
produced by the BCR-Abl
oncogene.
• Used in the treatment of
chronic myeloid leukemia.
```
Imatinib
298
Half life in neonates= 2.2-5
hours
```
• Half life in adults= 0.9-2.2
hrs
• Due to the lack of
development in fetal liver
metabolizing enzymes, its
half life is prolonged.
```
Acetaminophen
299
```
Its hazardous in cases of
low blood flow because its
distribution relies on
increased blood flow
• Its elimination is slower in
neonates because their
GFR and tubular secretion
is very low.
```
Gentamicin
300
```
It is a hydrophilic drug, so
its volume of distribution
is high in neonates
(because neonates have a
greater water: body fat
ratio)
```
Gentamicin
301
```
Its renal clearance is low
• Its half life is prolonged in
geriatric age due to
impaired renal function
and clearance= could be
very toxic if not adjusted.
```
Gentamicin
302
```
It is highly bound to
plasma proteins
• It should bind to serum
albumin, but because of
lower serum
concentrations of
albumin= its free fraction
in plasma will go up (in old
age)
• The loading dose=
decreases in elderly
```
Warfarin
303
It is less effective in old
people because of the
reduced number of
receptors and affinity.
B1- agonists
304
```
Uses:
o In the treatment
of anaphylactic
shock
o Severe
hypertension
o Atrioventricular
blockage
o Refractory HF
```
B1- agonists
305
```
It increases the myocardial
O2 demand= Elderly may
suffer from cardiac
arrythmias and angina,
especially if they have
CAD.
```
B1- agonists
306
```
These are substances which
activate receptors on the heart and
kidney to allow increased heart rate
and contractility and increased
secretion of renin.
```
B1- agonists
307
```
These drugs are used in
the treatment of:
o Cardiac
arrythmias
o CHF
o Angina
o HTN
o MI
```
B- blockers
308
```
In elderly, it may lead to an
undue-blockade of
sympathetic influences on
the heart= bradycardia,
hypotension, and Heat
failure
• In elderly, it may also lead
to an AV-nodule
conduction block
```
B- blockers
309
```
They are CVS drugs that
can lead to (especially in
those patients suffering
from arryythmia, type 2
DM, and gout):
o Hyperglycemia
o Hyperuricemia
o Hypokalemia
```
B- blockers
310
```
It should not be used in
elderly patients suffering
from any obstructive
airway disease (it will lead
to bronchoconstriction)
```
B- blockers
311
These substances block the actions of adrenergic agonists on the heart,
smooth muscles of the lungs, and fat cells.
B- blockers
312
```
It is hazardous in neonates
because of decreased
blood flow to the site of
administration
• Half life in neonates= 60-
70 hrs
• Half life in adults= 30-60
hrs
```
Digoxin
313
```
It is rapidly eliminated in
toddlerhood because of
increased GFR
• Absorption of it is delayed
by increased gastric
emptying
• It’s renal clearance is low
```
Digoxin
314
Its vd in geriatrics is low
because of decreased lean
body mass in old age (this
```
is because digoxin needs
to bind to the muscles in
order to exert its action).
• Digoxin’s half
-life is
prolonged in elderly
patients because of
decreased renal
clearance= dose needs to
be adjusted.
```
Digoxin
315
```
It is a CVS drug and it can
lead to toxic
arrhythmogenic action=
you need to decrease the
dose to decrease the
effect in elderly.
```
Digoxin
316
```
It’s ability to bind to
plasma proteins in
neonates is low.
• Reduced by MFO (mixed
function oxidases) and has
a long elimination half life
in neonates (their liver
enzymes are not as
developed)
• Half-life in neonates: 25-100 hrs
• Half-life in adults= 40-50hrs
```
Diazepam
317
```
It’s a hydrophobic drug so
its vd is decreased in
neonates (because they
have a high water: body
fat ratio)
• In elderly, due to increased
fat stores, its volume of
distribution is high
(because it’s a lipophilic
drug)
```
Diazepam
318
```
Due to decreased amount
of albumin in elderly, the
percentage of unbound or
free drugs increase (its Vd
is increased and so is its
action)
• Because of decreased liver
enzyme function in the
elderly, their half life is
prolonged (phase I
reactions are altered)
```
Diazepam
319
Because it’s a CNS drug=
ataxia (especially in elderly
because its half life is
prolonged)
Diazepam
320
```
Can only be given as a
treatment if the toxicant
was ingested less than an
hour ago
• It works against
hydrophobic toxicants
```
Activated charcoal
321
```
Can only be given as a
treatment if the toxicant
was ingested less than an
hour ago
• It works against
hydrophobic toxicants
```
Activated charcoal
322
```
It is not used for corrosives
MDAC can be used to
enhance the elimination of
a toxicant, but this is
mainly used if the patient
took a life threatening
amount of drug that can
be removed well by
charcoal.
```
Activated charcoal
323
```
Used in decontamination
from a toxicant
• Used in enhancing the
elimination of a toxicant
by metabolism
```
Activated charcoal
324
```
Toxicodynamic effect: It
causes antimuscarinic
syndrome, which is
characterized by
hypertension, tachycardia,
hyperthermia, and
mydriasis, and urinary
retention (toxic
syndrome).
```
Atropine
325
```
It can be used as an
antidote in
anticholinesterase
poisoning. It acts as this by
blocking the receptors
preventing acetylcholine
from binding (if there’s too
much of it).
```
Atropine
326
It is also used as an
| antidote for OP’s.
Atropine
327
```
It produces a very toxic
metabolite that is
metabolized by N-acetylcysteine
• Its antidote is N
-acetylcysteine.
```
Acetaminophen
328
```
Since it is an alcohol, the
general agreement is that
as its dosage increase, its
response increases and
causes an elevated anion
gap.
```
Ethanol
| Methanol
329
```
It completes with
methanol to bind to ADH.
It does this to prevent the
formation of methanol’s
toxic metabolite.
```
Ethanol
330
```
The mechanism is
competitive inhibition
• It acts as an antidote
against methanol and
ethylene glycol
```
Ethanol
331
```
It produces a toxic
metabolite when it binds
to ADH
• Its actions are terminated
by ethanol (its antidote)
```
Methanol
332
```
Given to comatose
patients mainly
Used in stabilization and
supportive care of the
intoxicated patient
```
Dextrose
333
```
In its poisoning state it
causes an elevated anion
gap
• It is treated using sodium
bicarbonate, which
enhances its elimination
through the kidneys
```
Salicylates
334
Hemodialysis may also
| enhance its elimination
Salicylates
335
It induces emesis
(although apomorphine is
parenterally preferred)
It is used to
decontaminate the GI
Syrup of Ipecac
336
It is contraindicated in
people who are:
```
o Unconscious
patients or
experiencing
convulsions
o Corrosives
o Drugs that induce
```
Syrup of Ipecac
337
It treats patients suffering
from poisoning by
acetaminophen’s toxic
N-acetylcystine
338
```
It enhances urinary
excretion of acidic drugs
mainly by altering the pH
of the urine (makes it
more alkaline to ionize
acidic drugs like aspirin,
enhancing its excretion).
```
Sodium bicarbonate
339
AKA: NaHCO3
• It is used as a measure to
enhance drug elimination
Sodium bicarbonate
340
```
It leads to an augmented
adverse drug reaction
• Leads to bradycardia
• It can also lead to chest
pain if abruptly stopped.
```
Atenolol
341
```
It causes an augmented
adverse drug reaction
• It causes dry skin and
constipation and
tachycardia.
```
Atropine
342
```
It leads to an immunogenic
bizarre adverse drug
reaction
• Immunogenic= allergic
reactions
• It causes pulmonary
reactions
• It causes skin reactions
```
aspirin
343
```
It can lead to an
augmented adverse drug
reaction when given in the
form of an injection
• Hypoglycemia (since it
brings down blood
glucose)
```
Insulin
344
Result in bizarre adverse
drug reactions
```
• These reactions are
immunogenic in nature.
• They bind to tissue
proteins forming
immunogens
• They also cause allergic
reactions: skin reactions
and anaphylactic shock.
```
Pencillins
345
```
It leads to a bizarre
adverse drug reaction
• The reaction is genetic in
nature.
• It leads to prolonged
paralysis and apnea in
patients who are deficient
in plasma cholinesterases.
```
Suxamethonium
346
```
It results in a bizarre
adverse drug reaction
• The reaction is genetic in
nature
• It’s been shown that it may
lead to hemolytic anemia
in those patients who are
deficient in G6PD.
• It typically affects black
males (10%) and
Mediterraneans.
```
Primiquine
347
```
It leads to bizarre adverse
drug reactions
• These reactions are also
genetic in their nature
• It tends to affect people
who are slow-acetylators
(so they have a
polymorphism in
metabolism of acetyaltors)
```
Isoniazid
348
It induces peripheral
neuropathy in people who
are deficient in N-acetyltransferase
Isoniazid
349
```
It causes delayed adverse
drug reactions
• These reactions are
typically congenital in
nature and can be severe
```
Warfarin
350
It causes a craniofacial
| abnormality- nasal hypoplasia
Warfarin
351
It causes delayed adverse
drug reactions
• It is mainly congenital in
nature and is very severe
• It causes deformed limbs
in the infant
Thalidomide
352
It is susceptible to drug interactions
because it has a low therapeutic
range.
Digoxin
353
Its absorption is altered by an increase in the gastric pH caused by
antacids.
Ketoconazole
354
```
If the antacids contain
aluminum or calcium, they
can chelate tetracycline
and reduce its absorption
and effectiveness.
```
Antacids
355
It can be displaced from plasma
binding proteins causing an
increase in its effect= you would
see excess bleeding.
Aspirin
356
```
In cases of aspirin toxicity,
you would want to
increase the renal
excretion. To prevent
tubular reabsorption, you
make the urine more
alkaline to increase the
chances of aspirin being
ionized.
```
Aspirin
357
```
When administered with
Warfarin, it poses an
increased risk of bleeding
(additivism=
pharmacodynamic affect)
• When administered with
garlic or ginkgo will cause
increased bleeding.
```
Aspirin
358
It can be displaced from the plasma
binding protein leading to an
increase in its effect= you would
see excess bleeding.
Warfarin
359
In the presence of
phenobarbital, it becomes
rapidly metabolized
reducing its effectiveness.
Warfarin
360
```
When administered with
aspirin, it increases the risk
of bleeding
(pharmacodynamic
effect=additivism)
• When administered with
garlic or ginkgo may lead
to increased bleeding.
```
Warfarin
361
In the presence of
phenobarbital, it becomes
rapidly metabolized
reducing its effectiveness.
Cimetidine
362
Cytochrome p450 isoenzyme
inhibitor
Cimetidine
363
Cytochrome p450 isoenzyme inhibitor
Cimetidine
364
If iron contains aluminum or
calcium it will form a complex with
tetracycline reducing its
Iron
365
```
It is an inducer of the
cytochrome p450 phase 1
reaction enzymes
• When administered it
accelerates the
metabolism of many other
drugs.
• Warfarin’s effectiveness is
reduced in the presence of
phenobarbital because of
its increased metabolism.
```
Phenobarbital
366
When administered with Penicillin,
it inhibits its active secretion
allowing it to stay longer in the
circulation (beneficial)
Probenecid
367
```
Normally administered to
treat asthma by relaxing
the smooth muscles in the
bronchioles
• When administered with a
b-blocker (antagonist), its
effects are reduced.
```
Salbutamol
368
```
Its excretion is increased
by making the urine more
alkaline
• Aspirin is an example of a
salicylate
```
• When administered with
garlic and ginkgo it may
lead to excess bleeding
Salicylates
369
```
Drugs like iron and
antacids that contain
calcium or aluminum can
form chelates with
tetracycline reducing its
absorption and
effectiveness.
```
Tetracyclines
370
```
When administered with
milk products, which are
high in calcium, it results in
decreased absorption of
tetracycline (because it is
chelated)
```
Tetracyclines
371
```
When administered with
aminoglycosides it will inhibit cell
wall synthesis allowing for
increased penetration of the cell
wall by aminoglycosides.
(syngergistic)
• Administered to treat
against Staph. Aureus
infections.
```
Penicillin
372
When administered with NA, it
inhibits the reuptake of NA allowing
NA to persist longer in the synaptic
cleft (potentiating its affect)
Cocaine
373
When administered with
acetylcholinesterases, its affect is
potentiated, as it will persist longer
in the synaptic cleft.
Acetylcholine
374
```
Tyramine is an important
dietary protein that is
needed for the formation
of NA
• When a person consumes
a tyramine rich diet and is
taking monoamine oxidase
inhibitors (phenelzine), the
chances of developing
hypertensive crisis are
high.
```
Tyramine
375
```
It is involved in dietary
drug interactions
• It is very important in
those patients who
consume high amounts of
cheese, particularly
because of the presence of
```
Tyramine within these
cheese products
Phenelzine
376
When tyramine is
consumed in the presence
of phenelzine it may lead
to a hypertensive crisis.
Phenelzine
377
```
It has a pharmacodynamic
drug interaction affect
• The effect is potentiation
• It allows for prolonged
action of acetylcholine by
inhibition of
acetylcholinesterases.
```
Physostigmine
378
```
It causes increased gastric
emptying= increased
absorption of drugs (not
sure about this).
• Thus, it can lead to
pharmacokinetic drug
interactions
• It does so by altering the
gastrointestinal absorption
of drugs.
```
Bethanecol
379
```
It inhibits the metabolism
of some drugs like calcium
channel blockers
(antihypertensives).
• This leads to hypotension
because the calcium
channel blockers cannot
be metabolized due to the
blockage of the intestinal
CYP3A4.
```
Grapefruit juice
