Comprehensive Pharmacology Summary

Drug
Antiepileptic:
Seizures:
Anticonvulsants
Carbamazepine
(drug of choice in
Parial
and tonic cloinc
seizures)
Phenytoin
Phosphenytoin
Oxcarbamazepine
Clonazepam
Ethosuximide (drug
of choice in
absence
seizures)
Felbamate
Gabapentin
Lamotrigine
Phenobarbital (drug
of choice of febrile
seizures and grand
mal seizures in
children)
Primidone
Tiagabine
Topimarate
Valproate
Sodium divalproex
Vigabatrin
Levetiractem

Mechanism of action
Many typical anticonvulsants
work by blocking
voltagesensitive sodium
channels in the brain.
Phenobarbital potentiates synaptic
inhibition through an action on
GABA receptor.
Ethosuximide inhibits calcium ion
influx through T type channels in
the thalmic neurons.
Gabapentin promotes the release of
GABA.
Absence seizures (sometimes
referred to as petit mal seizures)
involve an interruption to
consciousness where the person
experiencing the seizure seems to
become vacant and unresponsive
for a short period of time (usually
up to 30 seconds).
Slight muscle twitching may occur.
Tonic-clonic seizures (sometimes
referred to as grand mal seizures),
involve an initial contraction of the
muscles (tonic phase) which may
involve tongue biting, urinary
incontinence and the absence of
breathing.
Myoclonic seizures involve
sporadic muscle contraction and
can result in jerky movements of
muscles or muscle groups.
Atonic seizures involve the loss of
muscle tone, causing the person to
fall to the ground. These are
sometimes called 'drop attacks' but
should be distinguished from
similar looking attacks that may
occur in narcolepsy or cataplexy.

By: Mr Ednan and FPGEE October Group

Side effect
Carbamazepine: NV,
Jaundice, abdominal pain, pale
stool, darkened urine, unusual
bruising bleeding, fever, sore
throat, ulcer in the mouth,
dizziness, drowsiness,
unsteadiness.
Phenytoin: NV, swollen
gums, rash, swollen glands,
bleeding, jaundice, fever, sore
throat.
Phosphenytoin: Similar to
phenytoin.
Oxcarbazepine: NV,
dermatological reactions,
dizziness, somnolence,
headache, ataxia, fatigue,
cognitive symptoms, vertigo,
abdominal pain, abnormal
gait, tremor, diplopia,
nystagmus, abnormal vision.
Hyponatremia.
Clonazepam drowsiness,
ataxia, behavior disturbances
in children, hypersalivation,
bronchial hypersecretion,
anemia, leukopenia,
thrombocytopenia, respiratory
depression, anorexia, weight
loss.
Ethosuximide NV, fatigue,
headaches, drowsiness,
eosinophilia,
granulocytopenia, leukopenia,
blurred vision, hiccups,
confusion, urticaria, SSS, renal
damage, periorbital edema.
Felbamate: N, infection,
aplastic anemia, liver failure,
acne, insomnia, headache,
anxiety, hyperactivity, fatigue,

Interaction
Carbamazepine
Antiepileptic drugs,
antibiotics, isoniazid,
cimetidine,
propoxyphene,
diltiazem, verapamil,
CCB, warfarin, TCAs
and grapefruit juice.
Phenytoin
Antiepileptic drugs,
disulfiram, isoniazid,
chloramphenicol,
propoxyphene,
corticosteroids,
digitoxin, doxycycline,
estrogens, furosemide,
oral contraceptives,
quinidine, rifampin,
theophylline, vit D,
enteral nutritional
therapy, coumarin,
warfarin, TCAs,DM,
arthritis drugs.
Phosphenytoin
Amiodarone, quinidine.
Oxcarbazepine:
Phenytoin
phenobarbital, oral
contraceptive.
Clonazepam
Phenytoin, levodopa,
digoxin.
Ethosuximide
Carbamazepine,
valproic acid.
Felbamate:
Phenytoin,
carbamazepine.
Valproic acid.
Gabapentin Antacids,
cimetidine, oral

Contraindications:
Carbamazepine: CBC should be
monitored; can lower white blood
cell count.
Therapeutic drug monitoring is
required Caution: in patients with
bone marrow depression,
glaucoma and elderly.
REM dermatological reactions,
blood dyscrasias, suicidal thoughts
and behavior.
PhenytoinMyocardial insufficiency
hypotension, renal failure and
elderly.
Clonazepam
Caution: Patients with psychoses,
acute narrow-angle glaucoma, and
significant liver disease.
REM: withdrawal symptoms with
abrupt discontinuation, suicidal
thoughts and behavior.
Ethosuximide Avoid exposure to
sunlight and ultraviolet light and
alcoholic beverages
REM: Blood dyscrasias, systemic
lupus erythematosus, suicidal
thoughts and behavior. Hepatic
and renal toxicity.
Gabapentin
REM: Suicidal thoughts and
behavior.
Lamotrigine: Caution: in renal,
hepatic, or cardiac impairment.
Phenobarbital:
Caution in patients with hepatic
disease and elderly
Tiagabine:
To monitor: Periodic
ophthalmological. REM: Suicidal
thoughts, behavior.
Topimarate:
REM: Suicidal thoughts, behavior,

peripheral edema,
vasodilation, hypotension,
HTN, diplopia blurred vision,
anorexia, weight decrease, QT
prolongation and torsade de
pointes.
Gabapentin Somnolence,
dizziness, ataxia, nystagmus,
dyspepsia, dryness of mouth,
constipation, increased
appetite, diplopia, blurred
vision, CHF, HTN /
hypotension, dry skin, fungal
dermatitis, herpes infection,
SSS, DM.
Lamotrigine:
NV, dizziness, diplopia, ataxia,
blurred vision, rash, SSS,
photosensitization.
Phenobarbital: NV,
respiratory depression,
Withdrawal convulsions.
Tiagabine: Confusion,
dizziness, fatigue, GI upset,
mouth ulceration, and
anorexia, EEG abnormalities,
sudden unexpected death,
rash.
Topimarate: N, breast pain in
females, tremor, back pain,
chest pain, dyspepsia, leg
pain.
Valproic acid: NV, abdominal
pain, anoxia.
Vigabatrin:
Somnolence, fatigue, lightheadedness, peripheral
neuropathy, anemia,
depression.
Levetiracetam: Somnolence,
weakness, hostility, infection,
dizziness, depression,
nervousness, pruritis, skin
discoloration, rash, alopecia,

contraceptives.
Lamotrigine:
Carbamazepine,
phenobarbital,
primidone, valproic
acid.
Phenobarbital:
Antiepileptic drugs,
acetazolamide,
chloramphenicol,
cimetidine,
furosemide, rifampin,
pyridoxine, ethanol.
Tiagabine:
Phenobarbital,
phenytoin,
carbamazepine. Take
with food.
Topimarate:
Phenytoin,
carbamazepine.
Valproic acid:
Antiepileptic drugs,
aspirin, warfarin,
antacids.

teratogenic effects.
Vigabatrin: REM: Vision loss,
suicidal thoughts and behavior.

Antidepressants:
SSRIs
Fluoxetine (Prozac;
Sarafem)
Sertraline (Zoloft)
Escitalopram:
(Lexapro:Cipralex)
Citalopram(Celexa)
Fluvoxamine (Luvox)
Paroxetine (Paxil)

Selective
Norepinehprine
Reuptake
Inhibitor (SNRI)
Venlafaxine (effexor)

TCAs;
Antidepressants
amitriptyline (Elavil)
amoxapine (Asendin)
clomipramine
(Anafranil)
desipramine
(Norpramin)
doxepin (Adapin,
Sinequan)
imipramine (Tofranil)
nortriptyline
(Pamelor)
trimipramine
(Surmontil)
Tetracyclic
Antidepressant
Remeron
(Mirtazipine)

They act within the brain to

increase the amount of the
neurotransmitter, serotonin (5hydroxytryptamine or 5-HT), in
the synaptic gap by inhibiting
its reuptake (Reuptake is the
reabsorption of a neurotransmitter
by the molecular transporter of a
pre-synaptic neuron after it has
performed its function of
transmitting a neural impulse).
Venlafaxine is chemically unrelated
to other antidepressants, and
is categorized as a serotoninnorepinephrine reuptake inhibitor
(SNRI). It works by blocking the
transporter "reuptake" proteins
for key neurotransmitters
affecting mood, thereby leaving
more active in the synapse.
It was thought that tricylic
antidepressants work by
inhibiting the re-uptake of the
neurotransmitters
norepinephrine and serotonin
by nerve cells. However, this
response occurs immediately,
however mood does not lift for
around two weeks. It
is now thought that changes
occur in receptor sensitivity in
the cerebral cortex and
hippocampus.

Mirtazapine is chemically unrelated

to other antidepressants. It is
thought to work by blocking
presynaptic alpha-2 adrenergic
receptors that normally inhibit
the release of the
neurotransmitters
norepinephrine and serotonin,

drowsiness, cough.
Fewer and less severe than
TCAs and MAOI.
Insomnia, GI effects (nausea,
vomiting),
sexual dysfunction, a nxiety
WITHDRAWL SYMPTOMS: On
abrupt discontinuation
nightmares and vivid dreams
so tapered dose needed

Metabolised by CYP450
and CYP2D6 so drug
interactions are
common

Similar to SSRIs
Also produce withdrawal
symptoms.

Substrates for CYP2D6

Produce
SEROTONIN
SYNDROME if given
with MAOIs or other
Serotonergic agents

Numerous adverse effects

limit their use
-Anticholinergic side effects:
Dry mouth, blurred vision,
constipation, urinary retention,
tachycardia
-Quinidine like arrhythmias
-Weight gain

Substrates of CYP 450

enzymes so many
interactions MAO
INHIBITORS,
ADRENERGIC AGENTS

-Weight gain, increased

appetite
-Sedation

Antipsychotic:
Schizophrenia
Typical
Antipsychotics
Chlorpromazine
Fluphenazine
Haloperidol
Thiothixene
Thioridazine
Trifluoperazine
Loxapine

Atypical
Antipsychotics
Clozapine (Clozaril)
Olanzapine (Zyprexa)
Quetiapine
(Seroquel)
Risperidone
(Risperidal)
DA
Schizophrenia
DA PD

Mood Stabilizers
Lithium carbonate.

thereby increasing active levels

in the synapse. Mirtazapine also
blocks post-synaptic 5-HT2 and 5HT3 receptorsan action which is
thought to enhance serotonergic
neurotransmission while causing a
low incidence of side effects.
These drugs are also referred to as
neuroleptic drugs, or simply
neuroleptics. Typical antipsychotics
are sometimes referred to as major
tranquilizers because some of
them can tranquilize and sedate
when taken in large doses. All
antipsychotic drugs tend to block
the D2 neuroreceptors in the
dopamine pathways in the
brain, so the normal effect of
dopamine release in the
relevant synapses is reduced.
It is the blockade of D2
receptors in the mesolimbic
pathway of the brain which is
thought to produce the
intended antipsychotic effect.
All atypical antipsychotics are FDA
approved for use in the treatment
of schizophrenia. Some carry FDA
approved indications for acute
mania, bipolar mania, psychotic
agitation, bipolar maintenance, and
other indications.
Modulation of the dopamine
neurotransmitter system is
necessary for antipsychotic
activity while D2 receptor
antagonism coupled with 5
HT2A receptor antagonism is
responsible for the atypicality
of atypical antipsychotics.
Mania describes a medical
condition characterized by severely
elevated mood.

Sedation, blurred vision,

constipation, dry mouth,
Extrapyramidal symptoms,
Lowered seizure threshold,
orthostatic hypotension,
hyperprolactinemia, moderate
weight gain, QT
prolongation,photosensitivity,
temperature dysregulation,
neuroleptic malignant
syndrome, sexual dysfunction,
elevated liver enzymes.
Sedation, extrapyramidal
symptoms (except Clozapine),
anticholinergic effects,
Lowered seizure threshold,
orthostatic hypotension,
hyperprolactinemia
(risperidal), moderate to
severe weight gain, QT
prolongation, diabetes
mellitus,
hypercholesterolemia,
neuroleptic malignant
syndrome, sexual dysfunction.
Agranulocytosis (Clozapine).

Li:Early: GI upset, nausea,

polydipsia, nocturia, dry
mouth, hand tremor,

Clozapine:
Complete blood count (CBC) must
be monitored.
Caution in patients at risk for
seizures or with a history of a
seizure disorder.

Increase Li levels:
ACEIs, ARAII, NSADs,
thiazides, dehydration,

Lithium: Acute renal failure,

women in their first trimester of
pregnancy, pregnancy, renal

Anticonvulsants:
Valproic acid,
Carbamazepine
Oxcarbazepine
Gabapentin
Lamotrigine
Topiramate

5-HT3 receptor
blockers
Antiemetic
Granisetron
Ondansetron (zofran)
Dolasetron (anzemet)

Other manic symptoms include

irritability, reduced need of
sleep, hypersexuality,
religiosity, hyperactivity,
talkativeness, flight-of-ideas,
and grandiose plans.
Acetylcholinesterase (AChE)
inhibition was thought to be
important because there is
selective loss of forebrain
cholinergic neurons as a result of
Alzheimer's. AChE-inhibitors
reduce the rate at which
acetylcholine (ACh) is broken
down and hence increase the
concentration of ACh in the
brain. Acetylcholinesteraseinhibitors seemed to modestly
moderate symptoms but do not
prevent disease progression
including cell death.
The NMDA receptor (NMDAR) is
an ionotropic receptor for
glutamate (NMDA is a name of its
selective specific agonist).
NMDARs play a critical role in
synaptic plasticity mechanisms and
thus are necessary for several
types of learning and memory.
5-HT3 receptor blockers
principally used as an antiemetic
(cancer). The 5-HT3 receptor is a
ligand-gated Na+ and K+ cation
channel, resulting in a direct
plasma membrane depolarization.

Metoclopramide (GIT

Metoclopramide is a

Alzheimers
Disease; Dementia
donepezil (Aricept)
galantamine
(Reminyl)
rivastigmine (Exelon)

Mematine (NMDA
receptor
Antagonist) A
novel drug

Lithium: blocks the enzyme

inositol 1 phosphatase which
affects neurotransmitters.
Anticonvulsants are most mood
stabilizers too. We revised them
before #1)

leukocytosis, polyuria.
Long term: Morphological
kidney changes, EKG changes,
bradycardia, weigth gain,
decreased libido,
hypothyroidism, rash, acne.
Toxicity: Severe drowsiness,
coarse hand tremor, muscle
twitching, seizures,
choreoathetosis, vomiting,
confusion, vertigo.

Nausea, diarrhea, vomiting,

anorexia, tremors,
bradycardia, and muscle
cramps.

Confusion, agitation,
restlessness.

Headache.
Dolasetron:
Electrocardiographic changes
(prolonged QT interval).
Antidopaminergic: Sedation,
diarrhea, and extrapyramidal

renal dysfunction,
Sodium los, and
fluoxetine.
Decrease Li levels:
Acetazolamide,
methylxanthines,
osmotic diuretics,
pregnancy (3third
trimester), sodium
supplements, urine
alkalinizers.
Others: Antipsychotics,
benzodiazepines,
Are substrates for
cytochrome P450
(except Rivastigmine).

impairment, cardiovascular
disease, dehydration, seizure
disorder, and thyroid disease.
Consider: age, weight, and renal
function

motility inhibitor;
Prokinetic)

1
0

Anti Migraine; 5 HT
Receptors
Agonists
(Triptans)
Sumatriptan (Imitrex)
5HTD1
Rizatriptan (Maxalt)
Naratriptan (Amerge)
Zolmitriptan (Zomig)
5HTB1/D1

1
1

Antiarrrhythmics
Class Ia agents
include quinidine,
procainamide and
disopyramide.
Class Ib agents
include lidocaine,
mexiletine, tocainide,
and phenytoin.
Class Ic agents
include encainide,
flecainide,
moricizine, and
propafenone.
Class II agents
include esmolol,
propranolol, and
metoprolol.
Class III agents
include amiodarone,
azimilide, bretylium,
clofilium, dofetilide,
ibutilide, sematilide,
and sotalol.

parasympa-thomimetic, and is
also a potent dopamine
antagonist that enters the central
nervous system. It is used for
gastric emptying in patients with
gastric motor failure (gastroparesis).
Triptans are a family of tryptamine
drugs used in the treatment of
migraine and cluster headaches.
Their action is attributed to their
binding to serotonin 5-HT1B and 5HT1D receptors in cranial
blood vessels (causing their
constriction) and subsequent

symptoms

Antiarrhythmic agents are a group

of drugs that are used to
suppress fast rhythms of the
heart (cardiac arrhythmias), such
as atrial fibrillation, atrial flutter,
ventricular tachycardia, and
ventricular fibrillation.
Class I agents interfere with
the sodium (Na+) channel,
which
prolongs the action potential
duration by slowing conduction
Class II agents are antisympathetic nervous system
agents. All agents in this class are
beta blockers. They act by
slowing conduction through the
AV node.
Class III agents affect potassium
(K+) influx. They prolong
repolarization.
Class IV agents affect the AV
node. They decrease
conduction through the AV

Quinidine, Torsades des

pointes, Cinchonism,
thrombocytopenic purpura,
NVD (nausea, vomiting,
diarrhea).
Procainamide: Lupus like
syndrome and hypersensitivity
reactions.
Disopyramide. Potent
anticholinergic effects, NVD.
Lidocaine:
CNS: Paresthesias, drowsiness,
confusion, restlessness at low
dose.
Seizures and disorientation at
high dose. Cardiac depression
arrhythmias if given by rapid
IV.
Flecainide: May worsen
arrhythmias.
Propranolol: Heart failure.
Depressed AV conduction.
Bronchospasm. Hypotension.
Amiodarone: Corneal

Paresthesias, flushing, feeling

of pressure, tightness or pain
in the chest, neck, and jaw
and headache (Naratriptan
lower).

Monoamine oxidase
inhibitors (MAOIs):
(excluding eletriptan,
frovatriptan, and
naratriptan).
Eletriptan:
ketoconazole,
itraconazole,
nefazodone,
troleandomycin,
clarithromycin,
nelfinavir, and
ritonavir.

Avoid in familial hemiplegic migraine,

basilar migraine, ischemic stroke,
uncontrolled hypertension, ischemic
heart disease, prinzmetal angina,
ischemic complications,
cerebrovascular or peripheral vascular
disease, renal or hepatic disease, nearterm prior exposure to ergots alkaloid
or other 5-HT agonists.

1
2

1
3

Class IV agents
include verapamil
and diltiazem.
Class V agents
include adenosine
and digoxin.

node.
Class V agents work by other or
unknown mechanisms.

Calcium Channel
Blockers
Dihydropyridine
calcium channel
blockers
Amlodipine besylate
(Norvasc)
Nicardipine (Cardene,
Carden SR)
Nifedipine (Procardia,
Adalat)
Nitrendipine (Cardif,
Nitrepin)
Nimodipine
(Nimotop)
Phenylalkylamine
calcium channel
blockers
Verapamil
hydrochloride (Calan)
Diltiazem
hydrochloride
(Cardizem)
Fibrates;Hyperchol
esterolemia
Clofibrate (largely
obsolete due to sideeffect
profile, e.g.
gallstones)
Gemfibrozil (e.g.
Lopid)
Fenofibrate
Bezafibrate (e.g.
Bezalip)

Calcium channel blockers work by

blocking voltage-sensitive
calcium channels in the heart
and in the blood vessels. This
prevents calcium levels from
increasing as much in the cells
when stimulated, leading to less
contraction. This decreases total
peripheral resistance by dilating
the blood vessels, and decreases
cardiac output by lowering the
force of contraction.
Because resistance and output
drop, so does blood pressure.
Unlike with beta-blockers, the heart
is still responsive to
sympathetic nervous system
stimulation, so blood pressure can
be
maintained more effectively

The fibrates are a class of

amphipathic carboxylic acids.
Fibrates increase the activity of
lipoprotein lipase, a plasma
enzyme that degrades
chylomicrons and VLDL.
Fibrates are structurally and
pharmacologically related to the
thiazolidinediones, a novel class of
anti-diabetic drugs that also act
on PPARs .Although less effective in
lowering LDL, fibrates
improve HDL and triglyceride

deposits (reversible)
Hypo or hyperthyroidism.
Photosensitivity.
Pulmonary fibrosis.
Sotalol: Arrhythmias.
Verapamil: Sinus
bradycardia.
AV block. GI upset.
Verapamil: Constipation,
hypotension, bradycardia,
edema, CHF, GI upset.
Diltiazen: Edema, headache,
dizziness, asthenia, Rash.
Nifedipine: MI, peripheral
edema, reflex tachycardia,
Headache, flushing, edema.

Fibrates:
Muscle damage when fibrate
added with statin.
Gallstone formation.
NVD.

levels, and seem to improve

insulin resistance when the
dyslipidemia is associated with
other features of Syndrome X
(hypertension and diabetes
mellitus type 2).

Statins
atorvastatin
(Lipitor)
fluvastatin (Lescol)
lovastatin
(Mevacor,
Altocor, not
marketed in the UK)
pravastatin
(Pravachol,
rosuvastatin
(Crestor)
simvastatin (Zocor)
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4

Diuretics
Osmotic diuretics
(e.g., mannitol)
Carbonic
anhydrase
inhibitors (e.g.,
acetazolamide,
dorzolamide)

Thiazides (e.g.,
hydrochlorothiazide,
bendroflumethiazide)

Statins are the most potent

cholesterol-lowering agents,
lowering LDL-cholesterol (so-called
"bad cholesterol") by 3050%.
However, they are less effective
than the fibrates in reducing
triglycerides and raising HDLcholesterol. Statins act by
competitively inhibiting 3hydroxy-3-methylglutaryl
coenzyme
A (HMG CoA) reductase, an
enzyme of the HMG-CoA
reductase pathway, the body's
metabolic pathway for the
synthesis of cholesterol.
Diuretic is any drug that tends to
increase the flow of urine from
the body (diuresis). They also
decrease the extracellular fluid
volume, and are primarily used to
produce a negative extracellular
fluid balance. Diuretics are used to
treat heart failure, liver
cirrhosis, hypertension and certain
kidney diseases. Some common
diuretics are caffeine, cranberry
juice and alcohol.

Thiazides are a class of drug that

promote water loss from the body
((diuretics)). They inhibit Na+/Clreabsorption from the
distal convoluted tubules in the
kidneys. Thiazides also cause

Statins: Myositis, CPK

elevation, rhabdomyolysis,
memory loss, high BP.

Osmotic Diuretics:
Headache, NV, Chills,
dizziness, polydipsia.
Carbonic Anhydrase
Inhibitors: Acidosis.
THIAZIDE DIURETICS:
Chlorothiazide: hypokalemia,
hyponatremia, hyperglycemia,
hiperuricemia,
hypercalcemia, oliguria,
anuria, decreased placental
flow.
Loop Diuretics:
Furosemide: Ototoxicity,
hypovolemia,
hypomagnesemia.
hypokalemia

Loop diuretics
(e.g., furosemide,
bumetanide,
ethacrynic acid)

Potassium-sparing
diuretics (e.g.,
spironolactone,
amiloride,
triamtrene)

1
5

Alpha Adrenergic
Receptor Blockers
Alfuzosin
Doxazosin
Terazosin
Prazosin
Tamsulosin

1
6

Anti Diabetic, Type

2
Thiazolidinediones
Rosiglitazone
(Avandia)
Pioglitazone (Actos)

loss of potassium and an

increase in serum uric acid.

hyponatremia, hyperglycemia,
sulfonamide allergy.

Loop diuretics act on the

Na+/K+/Cl- cotransporter in the
ascending loop of Henle to
inhibit sodium and chloride
reabsorption. Because
magnesium and calcium
reabsorption in the thick ascending
loop is dependent on sodium and
chloride concentrations, loop
diuretics also inhibit their
reabsorption. This raises the
osmotic pressure inside the loop,
driving more water into the filtrate
causing increased urine volume.
Potassium sparing diuretics work
by inhibiting sodium
reabsorption in the distal
convoluted tubules and
collecting ducts in the kidneys.
This promotes the loss of sodium
and water from the body, but
without depleting potassium.
In BPH, the prostate grows larger
and presses against the urethra
and bladder, interfering with the
normal flow of urine. It leads to
symptoms of urinary hesitancy,
frequent urination, increased risk of
urinary tract infections and urinary
retention. Alpha blockers are used
to block alpha 1 receptors that
mediate muscular activity in
the bladder neck, prostate and
prostatic capsule.
Thiazolidinediones are selective
agonists for nuclear peroxisome
proliferator-activated receptorgamma (PPAR). These drugs bind
to PPAR, which activates insulinresponsive genes that regulate
carbohydrate and lipid metabolism.

Ethacrynic acid:Most
ototoxic.

POTASSIUM SPARING
DIURETICS:
Hyperkalemia, sodium or
water depletion, patients with
DM may develop glucose
intolerance, endocrine
disturbances. Triamterene
will turn urine blue.

Postural hypotension on first

dose is sudden and severe,
sodium depletion, edema, dry
mouth, headaches,
nightmares, sexual
dysfunction,lethargy.

Not indicated for use in type 1

diabetes, exacerbate CHF,
edema, weight gain, increased
LFT.

1
7

Sulfonylurea;
Antidiabetic
First generation:
Chlorpropamide
Tolbutamide
Tolazamide
Second
generation:
Glipizide , Gliclazide
Glibenclamide ,
Glimepiride
Glyburide

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8

Cancer
Alkylating Agents
Cisplatin,
Carboplatin,
Ifosfamide,
Chlorambucil,
Busulfan, Thiotepa.
Cyclophosphamide

Cancer;
Antimetabolites
5 Fluoro Uracil (5 FU)
Methotrexate,
Fludarabine

Thiazolidinediones require
insulin to be present for their
action. Thiazolidinediones exert
their principal effects by increasing
insulin sensitivity in peripheral
tissue but also may lower glucose
production by the liver.
Sulfonylureas bind to an ATPdependent K+ channel on the
cell membrane of pancreatic beta
cells. This inhibits a tonic,
hyperpolarizing outflux of
potassium, which causes the
electric potential over the
membrane to become more
positive. This depolarization opens
voltage-gated Ca2+ channels. The
rise in intracellular calcium
leads to increased fusion of
insulin granulae with the cell
membrane, and therefore increased
secretion of proinsulin.
Alkylating agents are so named
because of their ability to add
alkyl groups to many
electronegative groups
undervconditions present in
cells. They stop tumor growth
by crosslinking guanine
nucleobases in DNA doublehelix strands - directly
attacking DNA. This makes the
strands unable to uncoil and
separate.
Anti-metabolites masquerade as
purine or pyrimidine which
become the building blocks of DNA.
They prevent these
substances becoming incorporated
in to DNA during the "S"
phase (of the cell cycle),
stopping normal development and
division. An important example is 5-

Hypoglycemia, weight gain, GI

upset, headache, teratogenic.

Alkylating Agents
Cisplatin: Nephrotoxicity,
nausea and vomiting,
peripheral neuropathy,
myelosuppression, ototoxicity.
Carboplatin:
Myelosuppression, nausea and
vomiting, peripheral
neuropathy, ototoxicity.
Ifosfamide:
Myelosuppression,
hemorrhagic cystitis,
somnolence, confusion.
Chlorambucil:
Myelosuppression, pulmonary
fi brosis, hiperuricemia.
Busulfan:
Myelosuppression, pulmonary
fi brosis, aplastic anemia, skin
Hyperpigmentation. Thiotepa:
Myelosuppression, nausea and
vomiting, mucositis, skin

Alkylating agents:
Pregnancy, patients with bone
marrow suppression, Renal
disease(with cisplatin)
Platinum Analogs:
Hypersensitivity to
cisplatin/platinum products or
mannitol
Severe
myelosuppression/significant
bleeding

Antimetabolites:

Caner; Plant
alkaloids
Vincristine
Vinblastine

Cancer; Anti tumor

Antibiotics
Doxorubicin
Daunorubicin
Bleomycin
Actinomycin
plicamycin (Safe use
in pregnancy)

Fluoro Uracil (5FU), which inhibits

thymidylate synthase.
Fludarabine inhibits function of
multiple DNA polymerases, DNA
primase, DNA ligase I and is
S phase-specific. Methotrexate
(being folate antagosnist) inhibits
dihidrofolate reductase, enzyme
essential for purines and
pyrimidines synthesis.
These alkaloids are derived from
plants and block cell division
by preventing microtubule
synthesis and mitotic spindle
formation. These are vital for cell
division and without them it can
not occur. The main examples are
vinca alkaloids such as
vincristine, and vinblastine which
bind to specific sites on tubulin,
inhibiting the assembly of tubulin
into microtubules
They prevent cell division by
several ways: (1) binding to DNA
through intercalation between
two adjacent nucleotide bases
and making it unable to
separate, (2) inhibiting
ribonucleic
acid (RNA), preventing enzyme
synthesis, (3) interfering with
cell replication. Bleomycin acts in
unique way through oxidation
of a DNA-bleomycin-Fe(II) complex
and forming free radicals, which
induce damage and chromosomal
aberrations.

rashes. Cyclophosphamide:
Myelosuppression,
hemorrhagic cystitis,
immunosuppression, alopecia,
stomatitis, SIADH
Antimetabolites:
5 FU: Stomatitis,
myelosuppression, diarrhea,
nausea and vomiting,
cerebellar ataxia.
Methotrexate: Mucositis,
myelosuppression, pulmonary
fi brosis, hepatotoxicity,
nephrotoxicity, diarrhea, skin
erythema.
Fludarabine:
Myelosuppression, nausea and
vomiting, fever, malaise,
pulmonary infi ltrates.
Plant alkaloids:
Vincristine: Peripheral
neuropathy, paralytic ileus,
SIADH
Vinblastine: Myelosuppression,
paralytic ileus, alopecia,
nausea, stomatitis.
Antibiotics:
Daunorubicin:
Myelosuppression,
cardiotoxicity, stomatitis,
alopecia, nausea and
vomiting.
Bleomycin: Pneumonitis,
pulmonary fibrosis, fever,
anaphylaxis,
hyperpigmentation,
alopecia
Actinomycin: Bone marrow, a
cough, sore throat, pain,
passing urine or may feel cold
and shivery, anemia, bruising,
hair loss, skin changes.
Plicamycin: headache, NV,
vesicant, hepatic injury,

Ampicillin, aspirin,
Nsaids,
Cephalosporins.

Plant alkaloids:
Drugs known to inhibit
drug metabolism by
hepatic CYP 3A
subfamily. Vincristine
sulfate: Itraconazole.

Antibiotics:
Cyclophosphamide doxorubicin.

Plant Alkaloids: Demyelinating

form of CharcotMarieTooth
syndrome, pregnancy, significant
granulocytopenia, bacterial
infections.

Antibiotics: Hypersensitivity,
Children < 12 years, myeloid
malignancies, heart failure, atrial
arrhythmias, thromboembolic
disorders.
Caution: Major organ dysfunction.
Plicamycin: Breast feeding.

1
9

Immunosuppressa
nt, Eczema
Organ Transplant
Tacrolimus (Prograf,
Protopic)
Mycophenolate
mofetil (Cellcept)
Cyclosporine

2
0

Immunosuppressiv
e
Azathioprine

2
1

DMARD
gold salts (sodium
aurothiomalate,
auranofin)
D-penicillamine
chloroquine and
hydroxychloroquine
(antimalarials)

Tacrolimus s a macrolide antibiotic.

It acts by reducing peptidylprolyl
isomerase activity by binding
to the immunophilin
FKBP-12, creating a new complex.
This inhibits both Tlymphocyte
signal transduction and IL-2
transcription.
Cellcept is metabolised in the liver
to mycophenolic acid which
inhibits inosine
mononophosphate
dehydrogenase, the
enzyme which controls the rate
of synthesis of guanine
monophosphate in the de novo
pathway of purine synthesis
used in the proliferation of
lymphocytes.
Cyclocporine has same action as
Tacrolimus.
Azathioprine is used for
immunosuppression in organ
transplantation and
autoimmune disease such as
rheumatoid arthritis or Crohn's
disease. It is converted in the body
to 6mercaptopurine. Azathioprine acts
to inhibit purine synthesis
necessary for the proliferation
of cells, especially leukocytes and
lymphocytes.
Disease-modifying antirheumatic
drugs (DMARDs) are a category of
drugs used in many autoimmune
disorders to slow down disease
progression. They are used in
diseases such as Crohn's disease
and ulcerative colitis, lupus
erythematosus (SLE), idiopathic

Coagulation factors II, V, VII

and X. Azotemia, GIT
problems.
Tacrolimus: Nephrotoxicity,
neurotoxicity post transplant,
diabetes, hair loss.
Cyclosporine: Nephrotoxicity,
neurotoxicity hepatotoxicity,
hirsutism and gingival
hyperplasia.

Azathioprine: Bone marrow

suppression.

Methotrexate: Bone marrow

suppression, diarrhea,
mucositis.

Tacrolimus:
Antiepileptic drugs,
rifampin isoniazid,
azole antifungal
agents , macrolide
antibiotics,
calcium-channel
blockers, antiviral
agents

Xanthine oxidase
inhibitor, allopurinol,

Avoid Grape fruit

sulfasalazine (SSZ)
methotrexate (MTX)
azathioprine
cyclosporin A

2
3

Antithyroids
PTU
(propylthyouracil)
Tepazole
(methimazole)

thrombocytopenic purpura (ITP),

myasthenia gravis and various
others.
Methotrexate inhibits
dihydrofolate reductase, an
enzyme that is part of the
folate synthesis metabolic
pathway. Dihydrofolate reductase
catalyses the conversion of
dihydrofolate to the active
tetrahydrofolate. Methotrexate,
therefore, inhibits the synthesis
of DNA, RNA, thymidylates, and
proteins. Methotrexate is cell
cycle S-phase selective, and has a
greater negative effect on rapidly
dividing cells, which are replicating
their DNA, and thus inhibits the
growth and proliferation of these
cells.
Arava inhibits pyrimide
sysnthesis.
PPIs act by irreversibly blocking
the K/H ATPase or more
commonly just proton pump of
the gastric parietal cell. The
proton pump is the terminal stage
in gastric acid secretion, being
directly responsible for secreting
H+ ions into the gastric lumen,
making it an ideal target for
inhibiting acid secretion.
Both agents inhibit iodide
oxidation and iodorhiouracil
coupling but PTU only diminishes
peripheral deiodonation of T4 to
T3.

2
4

Corticosteroids
Prednisone

Corticosteroids have potent antiinflammatory and

Leflunomide (Arava)

2
2

Proton Pump
Inhibitors (PPIs)
Omeprazole,
Lansoprazole,
Esomeprazole,
Pantoprazole,
Rabeprazole

Diarrhea, GI pain, headache.

Inhibit CYP2C19
Diazepam, warfarin,
phenytoin, clopidogrel,
theophylline

NV, dermatologic reactions,

headache, drowsiness,
paresthesia, vertigo, neuritis,
loss of taste, arthralgia,
myalgia. Severe:
Agranulocytosis,
granulocytopenia,
thrombocytopenia, drug fever,
hepatitis,
hypoprothrombinemia.
Suppress pituitaryadrenal
axis, peptic ulcer, GI

To monitor: Serum thyroid levels

and the FTI.FDA black box
warning: Severe liver injury and
acute liver failure (PTU)

Estrogens, oral
contraceptives,

Caution: Diabetes, adrenal

suppression, CHF, osteoporosis,

Methylprednisone
Dexamethasone

2
5

Anti obesity
Orlistat (Xenical)

2
6

OCPs
Birth Control Pills

2
7

Inflammatory
Bowel Disease

immunosuppressive
properties.They bind to
glucocorticoid
receptors altering DNA and
RNA translation causing drop in
circulating T lymphocytes. As a
consequence, corticosteroids
are widely used as drugs to treat
inflammatory conditions such as
arthritis or dermatitis, and as
adjunction therapy for
conditions such as autoimmune
diseases.
It works by inhibiting pancreatic
lipase, an enzyme that breaks
down fat in the intestine.
Without this enzyme, fat from the
diet is excreted undigested, and not
absorbed by the body.
The Pill works by preventing
ovulation, as well as making
the uterus less likely to accept
implantation of an embryo if
one is created, and thickens
the mucus in the cervix making
it more difficult for sperm to
reach any egg. Taken correctly, it
is the
single most reliable form of
reversible contraception. Most
brands use 20 to 40 micrograms of
ethinyloestradiol as the
estrogen component and either a
fixed or varying (the bi and
triphasic pills) amount of
progestogen as the
progesterone analogue. Most
progestagens are used for their
antiestrogenic properties in oral
contraceptives to avoid over
stimulation of the endometrium
which could lead to endometriosis.
Ulcerative colitis is an inflammatory
disease of the bowel, that usually

hemorrhage, ulcerative
esophagitis, acute
pancreatitis, weight gain,
osteoporosis, hyperglycemia,
acne, increased susceptibility
to infection, cushingoid moon
face, buffalo hump,
headache, vertigo, increased
intraocular, glaucoma,
cataracts intracranial
pressures, muscle weakness,
psychological disturbances,
edema, HTN.
GI (soft or liquid stools),
increased defecation, fecal
urgency, abdominal pain,
decreased absorption of
vitamins A, D, E, K, and betacarotene.
Relatively low: Most due to
estrogen component.
Cardiovascular both. Breast
fullness, depression, fluid
retention, headache, NV.
Carcinogenicity: Increased
incidence of cervical cancer,
induce other neoplasms.
Production of benign tumors,
hemorrhage, abnormal
glucose tolerance, weight gain
(nortestosterone) (less weight
gain drospirenone). Changes in
the serum lipoprotein profile.

itraconazole, macrolide
antibiotics,
cyclosporine,
potassium-depleting
diuretics, digitalis
glycosides.

Mesalamine (5 ASA):
Diarrhea, headache,

Mesalamine
Mercaptopurine,

myasthenia gravis, psychiatric

diseases.

Fish oil.

Cerebrovascular, thromboembolic
disease, estrogen dependent
neoplasms, liver disease, and
pregnancy. Age of 35 who are
heavy smokers.

Mesalamine Caution: rarely

exacerbation of IBD

(IBD)
Ulcerative Colitis and
Crohns Disease

Mesalamine (5
ASA) (Pentasa,
Asacol)
Olsalazine
olsalazine,
balsalazide

affects the distal end of the large

intestine and rectum. The main
difference between the two is the
location and nature of the
inflammatory changes in the gut.
Crohn's can affect any part of
the gastrointestinal tract, from
mouth to anus. Ulcerative
colitis, in contrast, is restricted
to the colon, and spares the
anus.
Mesalamine, also known as 5aminosalicylic acid (5-ASA), is an
anti-inflammatory drug used to
treat inflammation of the
rectum, mild to moderate
ulcerative colitis and
inflammation of the lower
colon.

abdominal pain, cramps,

flatulence, skin rash. Rarely
hepatotoxicity or acute or
chronic renal injury.

antacids or acid
lowering agents.

Sulfasalazine
Fever, dizziness, headache,
itching, rash, photosensitivity,
GI upset, nausea, vomiting,
diarrhea, reversible
oligospermia

Sulfasalazine
folic acid

Zafirlukast: Headache,
dizziness, nausea, diarrhea

Zafirlukast: Aspirin,
erythromycin,
theophylline,
terfenadine, warfarin,
dofetilide.

Sulfasalazine

2
8

Leukotriene
receptors
antagonists
(LTRA); Asthma
Zafirlukast
(Accolade)

Montelukast
(Singulair)

Sulfasalazine is a sulfa drug used

primarily in the treatment of
inflammatory bowel disease. It is a
5-acetylsalicyclic acid
derivative. It is also used for
rheumatoid arthritis.
Leukotrienes are autocrine and
paracrine eicosanoid lipid
mediators derived from
arachidonic acid by 5lipoxygenase.
Zafirlukast is an oral leukotriene
receptor antagonist (LTRA) for the
maintenance treatment of asthma.
Available as a tablet, it
blocks the action of leukotriene
C4 on its receptors, thus reducing
constriction of the airways,
build-up of mucus in the lungs and
inflammation of the breathing
passages.
Montelukast blocks the action
of leukotriene D4 on the

To monitor: for vasculitic rash,

eosinophilia, increasing
pulmonary, cardiac, and
neuropathic symptoms.

Montelukast: Avoid in patients

with phenylketonuria.
Montelukast: Headache,
dizziness, and dyspepsia.

Montelukast: Hepatic
enzyme inducers (e.g.,
rifampin,
phenobarbital).

2
9

Bisphosphonates
Alendronate
Risedidronte
etidronate

3
0

Influenza A and B
Tamiflu (Oseltamivir)
Zanamivir

3
1

Influenza A (Flu)
Amantadine

3
2

Anticoagulants
Warfarin
Phenindione

cysteinyl leukotriene receptor

CysLT1, thus inhibiting
bronchoconstriction.
Bisphosphonates inhibit
osteoclastic activity. They reduce
both the resorption and
formation of hydroxyapetite
crystals.
Oseltamivir is a neuraminidase
inhibitor used in the treatment of
and prophylaxis of both influenza A
and influenza B. Oseltamivir is
a prodrug, usually administered as
oseltamivir phosphate, with
the drug being converted heptically
to the active metabolite.
Influenza (or as it is commonly
known, the flu or the grippe) is a
contagious disease caused by an
RNA virus of the orthomyxoviridae
family. Amantadine inhibits
replication of the influenza A
virus by interfering with viral
attachment and
uncoating.
The oral anticoagulants are a class
of pharmaceuticals that act by
antagonizing the effects of
vitamin K. It is important to
note that they take at least 48
to 72 hours for the
anticoagulant effect to develop
fully. Vitamin K is converted to
vitamin K epoxide in the liver. This
epoxide is then reduced by the
enzyme epoxide reductase. The
reduced form of vitamin K
epoxide is necessary for the
synthesis of many coagulation
factors (II, VII, IX and X, as well
as protein C and protein S).
Warfarin inhibits the enzyme
epoxide reductase in the liver,

Well tolerated. GI irritation,

heartburn, esophageal
irritation. diarrhea, abdominal
pain, musculoskeletal pain.
Unusual jaw necrosis, atypical
fractures of the femur.
NV, self-injury, delirium
(pediatric).

Contraindicated in women with a

creatinine clearance less than 30
mL/min.

Ataxia, nightmares, insomnia,

depression, confusion,
dizziness, fatigue, anxiety,
headache. Anticholinergic
reactions.

Caution: Elderly patients,

impaired renal function.
To monitor: History of seizures or
psychiatric disorders.

Warfarin:
Hemorrhage, skin lesions,
necrosis, purple toe syndrome,
alopecia.

Oseltamivir To monitor: Abnormal

behavior.
Caution: impaired renal function.
Zanamivir: Severe reactive
asthma or COPD

Warfarin: Numerous:
Inhibition of
metabolism: Acute
alcoholintoxication,
cimetidine,
chloramphenicol,
cotrimoxazole,
disulfiram,
metronidazole.
Stimulation : Chronic
alcohol, ingestion,
barbiturates,
glutethimide,
griseofulvin, rifampin
Antagonist: Spinach,
broccoli.
Additive effect:
Garlic.

Warfarin:
Pregnancy (X)
Black box warning for bleeding
risk.
Monitor and adjust the
anticoagulant effect.
To monitor: if necessary:
response with prothrombin
time/INR measurements.

Heparin:
Hypersensitive, bleeding disorders;
alcoholics; having or have had
recent surgery of the brain, eye,
spinal cord.

Heparin

3
3

Beta Blockers
Cardioselective
Acebutolol, Atenolol,
Betaxolol Bisoprolol,
Esmolol, Metoprolol
Nebivolol
Nonselective
Nadolol, propanolol,
Sotalol, Pindolol,

3
4

Biguanide;
Glucophage

thereby inhibiting coagulation.

Common indications for warfarin
use are atrial fibrillation,
artificial heart valves, deep
venous thrombosis and
pulmonary embolism.
Heparin works by potentiating
the action of antithrombin III, as
it is similar to the heparan sulfate
proteoglycans which are naturally
present on the cell membrane of
the endothelium.
Because antithrombin III
inactivates many coagulation
proteins, the process of
coagulation will slow down.
Beta blockers or beta-adrenergic
blocking agents are a class of drugs
used to treat a variety of
cardiovascular conditions and some
other diseases. Beta blockers block
the action of epinephrine and
norepinephrine on the adrenergic receptors in the
body (primarily in the heart,
peripheral blood vessels, bronchi,
pancreas, and liver). The hormones
and neurotransmitters stimulate
the sympathetic nervous system by
acting on these receptors.
Propanolol is used for social phobia.
Metformin is antihyperglycemic,
not hypoglycemic. It does not cause
insulin release from the pancreas
and generally does not cause
hypoglycemia, even in large doses.
Metformin has no significant effects
on the secretion of glucagon,
cortisol, growth hormone, or
somatostatin. Metformin reduces
glucose levels primarily by
decreasing hepatic glucose
production and by increasing insulin
action in muscle and fat.

To monitor:
The bleeding time.

Heparin: Hemorrhage,
Hypersensitivity reactions
(chills, fever, urticaria,
anaphylactic shock),
thrombosis,
thrombocytopenia,
osteoporosis, abnormal liver
function tests.

Heparin:
Protamine sulfate
(neutralization).

Propanolol:
Bronchoconstriction, sexual
impairment, disturbance in
metabolism, fasting
hypoglycemia.

Propanolol:
Cimetidine, fluoxetine,
paroxetine, ritonavir,
barbiturates,
phenytoin, rifampin

Propanolol: Asthma, COP.

Potential fatal lactic acidosis

(rarely).

Vitamin B12,
intravenous
radiographic contrast
agents.

Renal and/or hepatic disease,

acute myocardial infarction, severe
infection, or diabetic ketoacidosis.
Caution >80 years, history of
CHF, alcohol abuse.

3
5

Digitalis: Cardiac
Glycoside
Digoxin

3
6

Selective Estrogen
Receptor
Modulator
(SERM)
clomifene (an
ovulation)
raloxifene
(osteoporosis)
tamoxifen (breast
cancer)
toremifine (breast
cancer)

3
7

Antiretroviral
Drugs; HIV
Protease inhibitors
(PIs); HIV
Saquinavir, Ritonavir,

Digoxin inhibits the Na+-K+

ATPase pump in the
membranes of the heart cells
(myocytes). This causes an
increase in the
level of sodium ions in the
myocytes, which then leads to a
rise in the level of calcium ions.
This increased level of calcium
increases the contractility of the
myocardium (muscle of the heart).
Digoxin also decreases the
conduction of electrical
impulses through the AV node,
making it a commonly used drug in
controlling the heart rate during
atrial fibrillation or atrial flutter.
Selective estrogen receptor
modulator (SERMs) is a class of
medication that acts on the
estrogen receptor. A
characteristic
that distinguishes these substances
from receptor agonists and
antagonists is that their action is
different for various tissues,
thereby granting the possibility to
selectively inhibit or stimulate
estrogen-like action in various
tissues. There are three types of
estrogen receptors, which are
intracellular: ( homodimer),
( homodimer) and (- and receptor heterodimer). The receptor is generally stimulatory,
but the -receptor may inhibit
the -isoform as well as
suppressing transcription
independently
Protease inhibitors are a class of
medication used in viral infections.
They act by inhibiting specific
viral enzymes that are
essential to the viral life cycle by

N, headache, fatigue,
confusion, color perception
alteration, halos in dark
objects. Hypercalcemia and
hypomagnesemia. Ventricular
tachycardia.

Quinidine, verapamil,
amiodarone, K
depleting diuretics,
corticosteroids.

Clomiphene: Headach,
nausea, vasomotor flushes,
visual disturbances, ovarian
enlargement.
Toremifene: Endometrial
hyperplasia.
Raloxifene: Hot flashes, leg
cramps, deep vein thrombosis,
pulmonary embolism, retinal
vein thrombosis.

PIs:
Saquinavir: Prolongs PR and
QT interval, torsades de
pointes.
Ritonavir: GI intolerance,

Caution: Hypothyroidism, hypoxia,

renal failure, myocarditis.
To monitor: renal insufficiency and
dosage adjustment.

Raloxifene: women who will be

pregnant, history of
thromboembolic events.

PIs:
Warfarin.
Ritonavir:
inhibits many P450
isoenzymes

PIs: Simvastatin, lovastatin,

rifampin, cisapride, pimozide,
midazolam, triazolam, ergots,
alfuzosin, salmeterol, St. Johns
wort.

Indinavir, Nelfinavir

Reverse
Transcriptase
Inhibitors (RTIs)
Nucleoside Analog
Reverse
Transcriptase
Inhibitors (NARTIs) or
(NRTIs).
(Zidovudine,
didanosine,
Zalcitabine,
Stavudine,
Lamivudine,
Abacavir)
Non-Nucleoside
Reverse
Transcriptase
Inhibitors (NNRTIs)
(nevirapine:
Viramune, efavirenz:
Sustiva,
delavirdine:
Rescriptor)

cleaving viral proteins. Protease

inhibitors are molecules that
inhibit the function of
peptidases
and In medicine, protease inhibitor
is often used interchangeably with
alpha 1-antitrypsin.
Reverse Transcriptase Inhibitors
inhibit activity of reverse
transcriptase, a viral enzyme
HIV needs to reproduce. Lack of
this enzyme prevents HIV from
building DNA based on its RNA.

circumoral paresthesias,
hyperlipidemia,
hyperglycemia, fat
maldistribution, liver
function tests, taste
perversion.
Indinavir: Nephrolithiasis,
indirect hyperbilirubinemia,
hyperglycemia,
hyperlipidemia, fat
maldistribution,
headache, GI intolerance.
Nelfinavir: D, GI intolerance,
hyperlipidemia,
hyperglycemia, fat
maldistribution, pancreatitis,
PR interval prolongation.
RTIs
Zidovudine: Bone marrow
suppression, macrocytic
anemia, neutropenia,
headache, malaise, seizures,
anxiety, fever, rash,
symptomatic myopathy.
Didanosine: Reversible
peripheral neuropathy,
pancreatitis.
Stavudine: Reversible
peripheral neuropathy,
headache, rash, NVD. Fatal
episodes of pancreatitis.
Lamivudine: Minor.
Headache, fatigue, GI
reactions (NVD), dizziness,
neuropathy, insomnia.
NNRTIs
Nevirapine: SSS, N,
symptomatic hepatitis, fever,
headache.
Efavirenz: Insomnia,
dizziness, drowsiness,
nightmares, hallucinations,
rash, transaminases, GI
disturbances.

Indinavir: Atazanavir,
Vitamin C.
Nelfinavir Methadone.
RTIs
Zidovudine:
Cotrimoxazole,
atovaquone, valproic
acid, methadone,
probenecid, cytotoxic
drugs ganciclovir,
dapsone, ribavirin,
interferonalpha,Rifabut
in, rifampin.
Didanosine:
Zalcitabine:
Stavudine:
Zidovudine.
Lamivudine:
Cotrimoxazole,
emtricitabine.
Abacavir: Alcohol
NNRTIs
Rash, hepatotoxicity.
Nevirapine:
Methadone
Efavirenz: St. Johns
wort, levonorgestrel.
Delavirdine:
Alprazolam,
midazolam, triazolam,
simvastatin, lovastatin,
rifabutin, cisapride.
PPIs and H2-receptor
antagonists, St. Johns
wort, carbamazepine,
phenobarbital,
phenytoin, rifampin.

Caution antiepileptic drugs,

erectile dysfunction drugs,
colchicine, azole antifungals.
Saquinavir: Trazodone.
RTIs
Dose adjustment in renal
dysfunction (except abacavir).
Black box warning: Potential
lactic acidosis and severe
hepatomegaly with steatosis.
Didanosine:
Zalcitabine:
Lamivudine:
Black box warning: acute
exacerbations of hepatitis B.
Abacavir:
Black box warning:
hypersensitivity.
NNRTIs
Nevirapine: OCPs, efavirenz,
atazanavir, ritonavir, ketoconazole,
rifampin, St. Johns wort. Black
box warning: hepatic necrosis
Efavirenz: 1 trimester of
pregnancy, childbearing, unreliable
contraception, cisapride,
midazolam, triazolam, ergot
derivatives.

Delavirdine: N, rash, SSS,

headache.
3
8

Antituberculosis
Rifampin

Rifampicin inhibits DNAdependent RNA polymerase in

bacterial cells by binding its beta
subunit, thus preventing
transcription of messenger RNA
(mRNA) and subsequent
translation to proteins.

Rifampin: Serious
hepatotoxicity, skin rash,
drowsiness, headache, fatigue,
confusion, NV, abdominal pain.
Colors urine, sweat, tears,
saliva, feces orange-red.
Influenza-like syndrome.

Isoniazid

Isoniazid inhibits the mycolic

acid cell wall synthesis via
oxygen-dependent pathways,
such as the catalase-peroxidase
reaction.

Isoniazid: Skin rash, fever,

jaundice, peripheral neuritis,
Blood dyscrasias, GI (NV,
epigastric distress).
CNS toxicity (insomnia,
restlessness, hyperreflexia,
convulsions. Hepatitis).

3
9

Vancomycin
(Vancocin)
The drug of choice
and last resort where
other antibiotics are
not effective.

Fever, chills, phlebitis, red man

syndrome (flushing), shock,
hearing loss, renal failure.

Amino glycosides:
ototoxicity and
nephrotoxicity

4
0

Metronidazole
(Flagyl)

Vancomycin is an antibiotic used in

the prophylaxis and treatment of
infections caused by Grampositive bacteria. Vancomycin
acts
by inhibiting proper cell wall
synthesis in Gram-positive
bacteria. Vancomycin needs to be
given intravenously (IV) for
systemic therapy since it does not
cross through the intestinal lining. It
is a large hydrophilic molecule
which partitions poorly
across the gastrointestinal mucosa.
The only indication for oral
vancomycin therapy is in the
treatment of pseudomembranous
colitis, where it must be given
orally to get to reach the site of
infection in the colon.
Metronidazole is an antibiotic and
antiparasitic drug classified as a
nitroimidazole. It inhibits
nucleic acid synthesis and is
used for the treatment of infections

GIT(NAUSEA,VOMITING,ABDO
MINAL CRAMP)
METALIC TESTE,ORAL
YEAST INFECTION
(MONILIASIS)

WITH ALCOHOL
~FROM DISULFIRAM
LIKE EFFECT

Rifabutin &
rifapentine. (Newer)

Rifampin: CS, WARF,

OCPs, quinidine,
digitoxin, PIs, NNRTIs,
KCZ, verapamil,
methadone, OADs,
CYA, dapsone, Cam,
BARB. Probenecid.
ASA.
Isoniazid: PHT,
Antacids (Aluminum),
CBZ, cycloserine,
SSRIs, ethionamide,
meperidine.

Rifampin:
To monitor: Liver function tests.
Isoniazid:
Monitor: CBC, liver function.
Caution: Age, diabetes, HIV,
uremia, alcoholism, malnutrition,
pregnancy, seizure disorder

involving anaerobic bacteria as

well as protozoal infections.
Conditions it is useful in include:
giardiasis, amoebiasis,
Trichomonas vaginalis
infections, bacterial vaginosis,
pseudomembranous colitis,
Helicobacter pylori infections,
and acne rosacea.
The polyenes bind with sterols in
the fungal cell wall, principally
ergosterol. This causes the cell's
contents to leak out and the
cell dies. Human (and other
animal) cells contain cholesterol
rather than ergosterol so are much
less susceptible.
The imidazole and triazole
groups of antifungal drugs
inhibit
the enzyme cytochrome P450
14-demethylase. This enzyme
converts lanosterol to ergosterol,
and is required in fungal cell wall
synthesis. These drugs also block
steroid synthesis in humans.
Allylamines inhibit the enzyme
squalene epoxidase, another
enzyme required for ergosterol
synthesis

,NEUROTOXICOLOGIC
PROBLEM
(DIZZINESS,VERTIGO AND
NUMBNESS)

4
1

Polyene Antibiotics
Imidazole
(Miconazole,Ketocona
zole
Clotrimazole
,Econazole,
Mebendazole
,Oxiconazole
Thiabendazole
,Tiaconazole)
Triazole
(Fluconazole
,Itraconazole)
Allyalamine
(Terbinafine; Lamisil)

ALLERGY,GIT DISTURBANCE ,
GYNECOMASTIA AND
IMPOTANCE.
HEPATIC DYSFUNCTION AND
LIVER MICROSOMAL ENZYME
INHIBITOR
OTHER AZOLES~ LESS SIDE
EFFECT
FLUCONAZOLE~ NO
ENDOCRINE SIDE EFFECT

4
2

Quniolones and
Fluoroquinolones
Antibiotics
Ciprofloxacin (Cipro)
Levofloxacin
(Levaquin)
Norfloxacin (Noroxin)
Ofloxacin (Floxin)
Moxifloxacin (Avelox)
Gatifloxacin (tequin)

Quinolones and fluoroquinolones

form a group of broad-spectrum
antibiotics. They are derived from
nalidixic acid.
Quinolones act by inhibiting the
bacterial DNA gyrase enzyme.
This way they inhibit nucleic acid
synthesis and act
bacteriocidically.

GIT(NAUSEA,VOMITING,DIARR
HEA)
CNS(DIZZINESS,HEADACHE,SE
IZURE)
PHOTOTOXICITY
GATIFLOXACIN~ DIABETES
GREPAFLOXACIN~
PROLONGED QTINTERVAL
TROVAFLOXACIN~ FETAL
LIVER DAMAG

THEOPHYLLINE~
INCREASE
CIPROFLOXACINE
CONCENTRATION
DECREASE CATIONS
( AL,Mg,Ca,Zn,Fe)
ABSORPTION

4
3

Macrolides
Antibiotics

The mechanism of action of the

macrolides is inhibition of

GIT:(NAUSEA,VOMITING
,DIARRHIEA)

MICROSOMAL
ENZYME INHIBITER

(erythromycin
,clarithromycin
azithromycin
roxithromycin)
The macrolides are a
group of drugs
(typically antibiotics)
whose activity stems
from the presence of
a macrolide ring, a
large lactone ring
to which one or
more
deoxy sugars,
usually cladinose and
desosamine, are
attached. The
lactone ring can be
either 14, 15 or 16membered.
Macrolides belong to
the polyketide class
of
natural products.

bacterial protein synthesis by

binding reversibly to the
subunit 50S of the bacterial
ribosome, thereby inhibiting
translocation of peptidyl-tRNA.
This action is mainly bacteriostatic,
but can also be bactericidal in high
concentrations.
Macrolides tend to accumulate
within leukocytes, and are therefore
actually transported into the site of
infection.
Macrolides are used to treat
infections such as respiratory
tract infections and soft tissue
infections. Beta-hemolytic
streptococci, pneumococci,
staphylococci and enterococci are
usually susceptible to macrolides.
Unlike penicillin, macrolides
have shown effective against
mycoplasma, mycobacteria, some
rickettsia and chlamydia.

LIVER: CHOLESTATIC
JAUNDICE
OTOTOXCIT

~INCREASE
WARFARINE TOXICITY

4
4

Aminoglycosides
Amikacin,
gentamicin,
kanamycin,
neomycin,
streptomycin, and
tobramycin.

OTOTOXICITY
,NEPHROTOXICITY ,SKELETAL
MUSCLE RELAXANT ,ALLERGIC
REACTION

CEPHALOSPORINS,
POLYMYXINS AND
FUROSAMDE.

4
5

Finasteride
(Propecia):
Antiandrogen
5 alpha reductase
inhibitor

Aminoglycosides are a group of

antibiotics that are effective against
certain types of bacteria.
Aminoglycosides work by
binding to the bacterial 30S
ribosomal subunit, causing
misreading of t-RNA, leaving
the bacterium unable to
synthesize proteins vital to its
growth. Aminoglycosides are
useful primarily in infections
involving aerobic, Gram-negative
bacteria, such as Pseudomonas,
Acinetobacter, and Enterobacter.
Finasteride acts by inhibiting 5alpha reductase, the enzyme
the converts testosterone to
dihydrotestosterone. It is used in
benign prostate hyperplasia (BPH)

allergic reaction, male breast

cancer, Less serious side
effects (impotence, abnormal
ejaculation, swelling in hands
or feet,

4
6

4
7

Flutamide
Bicalutamide
(Casodex)
Nilutamide
(Anandron)
Tetracyclines
Doxycylcine
Demeclomycin
Minocycline

in low doses, and in prostate cancer

in higher doses. It is registered in
many countries for malepattern
baldness.

swelling or tenderness in
breasts, dizziness)

Tetracyclines bind to 30S subunit

of bacterial ribosome, blocking
aminosyl transfer RNA on the
receptor site on the m RNA
ribosomal complex

eta Lactam
Antibiotics
Penicillins
Cephalosporins
First generation
cephalosporins
cephalexin
,cephalothin
cephazolin
Second generation
cephalosporins
cefaclor ,cefuroxime
cefamandole
Second generation
cephamycins
Moderate
spectrum with
anti-anaerobic
activity.
cefotetan , cefoxitin
Third generation
cephalosporins
Broad spectrum.
ceftriaxone ,
cefotaxime
Broad spectrum
with anti-

-lactam antibiotics are a broad

class of antibiotics including
penicillin derivatives,
cephalosporins, monobactams,
carbapenems and -lactamase
inhibitors; basically anyantibiotic
agent which contains a -lactam
nucleus in its molecular structure.
-lactam antibiotics were mainly
active only against
Gram-positive bacteria, the
development of broad-spectrum lactam antibiotics active against
various Gram-negative organisms
has increased the usefulness of the
-lactam antibiotics. All - lactam
antibiotics are bactericidal, and act
by inhibiting the synthesis of
the peptidoglycan layer of
bacterial cell walls.
The peptidoglycan layer is
important for cell wall
structural
integrity, especially in Grampositive organisms. The final
transpeptidation step in the
synthesis of the peptidoglycan is

GIT(ANOREXIA,EPIGASTRIC
PAIN, ABDOMINAL DISTENTION
,PERIANAL
IRRITATION),CLACIFIED
TISSUE,FETAL HEPATOTOXICITY
PHOTOSENSITIVTY,
AZOTEMIA,FAN-CNI
SYNDROME(TETRACYCLINE~E
PITETRACYCLINE~ LEADE TO
NAUSEA ,VOMITING,POLYURIA,
POLYDIPSIA,PROTEINEURIA
,ACIDOSIS AND GLYCOSURIA
Penicillins: Hypersensitivity
reactions (urticarial, vesicular,
bullous, scarlatiniform,
maculopapular. Thrombopenic
purpura, fever, eosinophilia,
angioedema, serum sickness).
Anaphylaxis: (severe
hypotension,
bronchoconstriction, nausea,
vomiting, abdominal pain, and
extreme weakness).GI
distress, bone marrow
suppression, superinfection.
Cephalosporins:
Hypersensitivity (See for
penicillins), NVD,
superinfection, nephrotoxicity,
Clostridium difficileinduced
colitis.
Cefoperazone, cefmetazole,
cefotetan: bleeding diatheses.

Penicillins:
Probenecid.
Antagonism:
Erythromycins,
tetracyclines, or
chloramphenicol.
Parenteral products
contain either
potassium, sodium.
Cephalosporins:
Cross-sensitivity with
penicillin.Probenecid
(except ceftazidime).
Alcohol consumption:
cefmetazole,
cefotetan,
cefoperazone.
Antacids Cefaclor
extended-release
tablets, cefdinir,
cefpodoxime.
H2-antagonists:
cefpodoxime &
cefuroxime.
Iron supplements and
iron-fortified foods:
cefdinir

Penicillins:
A positive history for reactions
Renal impairment.
Procaine hypersensitivity is a
contraindication to the use of
procaine penicillin G.
Cephalosporins:
Ceftriaxone: Newborns receiving
concurrent administration of
calcium containing solutions.
IV calcium-containing solutions.

Carbapenems:
Cross-sensitivity reactions those
are allergic to penicillin or
cephalosporins

Pseudomonas
activity.
ceftazidime
Fourth generation
cephalosporins
cefepime
Carbapenems

4
8

Analgesics:
Narcotics
Endogenous
opioids
Opioid-peptides that
are produced in the
body:endorphins
dynorphins
enkephalins
Opium alkaloids
Phenanthrenes
naturally occurring in
opium:morphine
,codeine
thebaine
Semisynthetic
derivatives
diamorphine
(heroin) , oxycodone
hydrocodone
,dihydrocodeine
hydromorphone
,oxymorphone
Synthetic opioids
Phenylheptylamine
s
methadone
levomethadyl
acetate
hydrochloride
Phenylpiperidines
pethidine
(meperidine)
fentanyl , alfentanil
sufentanil

facilitated by transpeptidases
known as penicillin binding proteins
(PBPs). Inhibition of PBPs may also
lead to the activation of autolytic
enzymes in the bacterial cell wall.
-lactam antibiotics are indicated
for the prophylaxis and treatment
of bacterial infections caused by
susceptible organisms.
An opioid is any agent that binds to
opioid receptors found principally in
the central nervous system and
gastrointestinal tract. There are
four broad classes of opioids:
endogenous opioid peptides,
produced in the body; opium
alkaloids, such as morphine
(the prototypical opioid) and
codeine; semi-synthetic opioids
such as heroin and oxycodone; and
fully synthetic opioids such as
pethidine and methadone that have
structures unrelated to the opium
alkaloids.
There are at least three major
classes of opioid receptors: ,
and
. These are all G-protein
coupled receptors acting on
GABAergic neurotransmission.
The receptor (the represents
morphine) is perhaps the most
important being responsible for
most of the analgesic and other
major pharmacological effects
as well as many of the adverse
effects of opioids.
Opioid overdose can be rapidly
reversed with any of several opioid
antagonists such as naloxone.
These competitive antagonists are
drugs that bind to the -opioid
receptors with higher affinity than
agonists but do not activate them.

Carbapenems: NVD,
pseudomembranous colitis,
seizures, dizziness,
hypotension.

NV, constipation (e.g.,

codeine), sedation, respiratory
depression, anticholinergic
effects (dry mouth and urinary
retention), hypersensitivity,
CNS excitation.
Tolerance (increase doses),
dependence (physical
dependence), withdrawal
symptoms.

Cephalosporins: may
cause false-positive
glycosuria results.

CNS depressants (e.g.,

alcohol, anesthetics,
antidepressants,
antihistamines,
barbiturates,
benzodiazepines,
phenothiazines). MAO
inhibitors.

To monitor: Respiratory rate,

warned about driving or operating
machinery.

4
9

Diphenylpropylami
ne derivatives
propoxyphene
dextropropoxyphene
Benzomorphan
derivatives
pentazocine ,
phenazocine
Oripavine
derivatives
buprenorphine
Morphinan
derivatives
butorphanol,
nalbufine
tramadol, loperamide
diphenoxylate
Opioid antagonists
naloxone , naltrexone
Gout
Colchicine

Allopurinol

The main clinical indications of

opioids include; moderate-tosevere acute pain and chronic
pain cough (mainly codeine)
diarrhea (mainly loperamide and
diphenoxylate used therapeutically)
relief of severe dyspnoea (e.g.
lung cancer, terminal COPD)

Colchicine inhibits the

cytoskeleton by binding to
tubulin, one of the main
constituents of microtubules.
Allopurinol is used for long term
treatment. Allopurinol treatment
should not be initiated during an
attack of gout, as it can then
worsen the attack. In humans,
xanthine oxidase is normally
found
in the liver and not free in the
blood. Because xanthine oxidase is
a metabolic pathway for uric acid
formation, the xanthine oxidase
inhibitor allopurinol is used in
the treatment of gout.

Colchicine:
NVD, abdominal pain,
myopathy, neutropenia,
aplastic anemia, alopecia.

Allopurinol: Hypersensitivity
runs in skin. Acute attacks of
gout. Colchicine and NSAIDS:
NV.

Pregnancy.
Caution: hepatic, renal, or
cardiovascular disease.

Allopurinol
6-mercaptopurine,
azathioprine.