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IMPORTANT DRUGS AND THEIR MECHANISM OF ACTIONS

No
1

Drugs and Therapeutic Class

Antiepileptic: Seizures: Anticonvulsants
Carbamazepine (drug of choice in Parial
and tonic cloinc seizures)
Oxcarbamazepine
Clonazepam
Ethosuximide (drug of choice in absence
seizures)
Felbamate
Phosphenytoin
Gabapentin
Lamotrigine
Phenobarbital (drug of choice of febrile
seizures and grand mal seizures in
children)
Phenytoin
Primidone
Tiagabine
Tpoimarate
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.

Antidepressants: SSRIs
Fluoxetine (Prozac; Sarafem)
Sertraline (Zoloft)
Escitalopram: (Lexapro:Cipralex)
Citalopram(Celexa)
Fluvoxamine (Luvox)
Paroxetine (Paxil)
Selective Norepinehprine Reuptake
Inhibitor (SNRI)
Venlafaxine (effexor)

They act within the brain to increase the amount of the

neurotransmitter, serotonin (5-hydroxytryptamine 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 serotonin-norepinephrine reuptake inhibitor
(SNRI). It works by blocking the transporter "reuptake"
proteins for key neurotransmitters affecting mood, thereby
leaving more active in the synapse.

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

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.

Tetracyclic Antidepressant
Remeron (Mirtazipine)

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, thereby
increasing active levels in the synapse. Mirtazapine also blocks

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post-synaptic 5-HT2 and 5-HT3 receptorsan action which is

thought to enhance serotonergic neurotransmission while causing
a low incidence of side effects.
6

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

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.

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

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.

DA Schizophrenia
DA PD
7

Mood Stabilizers
Lithium carbonate - Valproic acid,
divalproex sodium and sodium valproate.
Carbamazepine (Tegretol) - CBC should be
monitored; can lower white blood cell count.
Therapeutic drug monitoring is required.
Oxcarbazepine (Trileptal)
Gabapentin (Neurontin)
Lamotrigine (Lamictal)
Topiramate (Topamax)

Mania describes a medical condition characterised by severely

elevated mood. Lithium blocks the enzyme inositol 1
phosphatase which affects neurotransmitters.Most mood
stabilizers are anticonvulsants.
Other manic symptoms include irritability, reduced need of
sleep, hypersexuality, religiosity, hyperactivity, talkativeness,
flight-of-ideas, and grandiose plans.

Alzheimers Disease; Dementia

donepezil (Aricept)
galantamine (Reminyl)
rivastigmine (Exelon)

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
Acetylcholinesterase-inhibitors seemed to modestly moderate
symptoms but do not prevent disease progression including cell
death.

Mematine (NMDA receptor Antagonist) A

novel drug

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 Antagonists; Antiemetic

Granisetron
Ondansetron (zofran)
Dolasetron (anzemet)
Metoclopramide (GIT motility inhibitor;
Prokinetic)

Ondansetron is a 5-HT3 receptor antagonist 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 is a parasympathomimetic, 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).It is also useful for facilitating small bowel
intubation and as an antiemetic. Metoclopramide is indicated for
the prevention of nausea and vomiting associated with
emetogenic cancer chemotherapy and surgery. In addition,
metoclopramide is indicated for the treatment of
gastroesophageal reflux disease and gastroparesis as well as to
aid in intubation of the small intestine and in radiologic examination
of the upper gastrointestinal tract.

10

Anti Migraine; 5 HT Receptors Agonists

(Triptans)
Sumatriptan (Imitrex) 5HTD1
Rizatriptan (Maxalt)

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 5-HT1D receptors in cranial blood
vessels (causing their constriction) and subsequent inhibition of

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Naratriptan (Amerge)
Zolmitriptan (Zomig) 5HTB1/D1

pro-inflammatory neuropeptide release.

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

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 anti-sympathetic 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 node.
Class V agents work by other or unknown mechanisms.

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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)

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

13

Fibrates;Hypercholesterolemia
Clofibrate (largely obsolete due to side-effect
profile, e.g. gallstones)
Gemfibrozil (e.g. Lopid)
Fenofibrate
Bezafibrate (e.g. Bezalip)

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 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)

14

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 HDL-cholesterol. Statins act by
competitively inhibiting 3-hydroxy-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.

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

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 (e.g., hydrochlorothiazide,

bendroflumethiazide)

Thiazides are a class of drug that promote water loss from the
body ((diuretics)). They inhibit Na+/Cl- reabsorption from the
distal convoluted tubules in the kidneys. Thiazides also cause
loss of potassium and an increase in serum uric acid.

Loop diuretics (e.g., furosemide,

bumetanide, ethacrynic acid)

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

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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.

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17

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Potassium-sparing diuretics (e.g.,

spironolactone, amiloride, triamtrene)

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.

Alpha Adrenergic Receptor Blockers

Alfuzosin
Doxazosin
Terazosin
Prazosin
Tamsulosin

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.

Anti Diabetic, Type 2

Thiazolidinediones
Rosiglitazone (Avandia)
Pioglitazone (Actos)

Thiazolidinediones are selective agonists for nuclear peroxisome

proliferator-activated receptor-gamma (PPAR). These drugs bind to
PPAR, which activates insulin-responsive genes that regulate
carbohydrate and lipid metabolism. 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.

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

Sulfonylureas bind to an ATP-dependent 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.

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

Alkylating agents are so named because of their ability to add

alkyl groups to many electronegative groups under conditions
present in cells. They stop tumor growth by cross-linking
guanine nucleobases in DNA double-helix strands - directly
attacking DNA. This makes the strands unable to uncoil and
separate.

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

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-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.

Caner; Plant alkaloids

Vincristine
Vinblastine

Cancer; Anti tumor Antibiotics

Doxorubicin
Daunorubicin
Bleomycin
Actinomycin
plicamycin

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.

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US/CANADIAN PHARMACY EXAM

Immunosuppressant, Eczema
Organ Transplant
Tacrolimus (Prograf, Protopic)
Mycophenolate mofetil (Cellcept)

Cyclosporine
20

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Immunosuppressive
Azathioprine

DMARD
gold salts (sodium aurothiomalate, auranofin)
D-penicillamine
chloroquine and hydroxychloroquine
(antimalarials)
sulfasalazine (SSZ)
methotrexate (MTX)
azathioprine
cyclosporin A

Leflunomide (Arava)

EDNAN

Tacrolimus is 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 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.

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Proton Pump Inhibitors (PPIs)

Omeprazole, Lansoprazole,
Esomeprazole, Pantoprazole, Rabeprazole

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.

Antithyroids
PTU (propylthyouracil)
Tepazole (methimazole)

Both agents inhibit iodide oxidation and iodorhiouracil

coupling but PTU only diminishes peripheral deiodonation of T4 to
T3.

Corticosteroids
Prednisone
Methylprednisone
Dexamethasone

Corticosteroids have potent anti-inflammatory and

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.

Anti obesity
Orlistat (Xenical)

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.

OCPs
Birth Control Pills

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.

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Inflammatory Bowel Disease (IBD)

Ulcerative Colitis and Crohns Disease

EDNAN

Ulcerative colitis is an inflammatory disease of the bowel, that

usually 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 (5 ASA) (Pentasa, Asacol)

Sulfasalazine
Olsalazine

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Leukotriene receptors antagonists

(LTRA); Asthma
Zafirlukast (Accolade)

Montelukast (Singulair)

Mesalamine, also known as 5-aminosalicylic 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.
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 5-lipoxygenase.
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
cysteinyl leukotriene receptor CysLT1, thus inhibiting
bronchoconstriction.

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Bisphosphonates
Alendronate
Risedidronte
etidronate

Bisphosphonates inhibit osteoclastic activity. They reduce both

the resorption and formation of hydroxyapetite crystals.

30

Influenza A and B
Tamiflu (Oseltamivir)

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.

31

Influenza A (Flu)
Amantadine

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.

32

Anticoagulants
Warfarin
Phenindione

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, thereby inhibiting coagulation.
Common indications for warfarin use are atrial fibrillation,
artificial heart valves, deep venous thrombosis and pulmonary
embolism.

Heparin

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Beta Blockers
Cardioselective
Acebutolol, Atenolol, Betaxolol Bisoprolol,
Esmolol, Metoprolol Nebivolol

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

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Nonselective
Nadolol, propanolol, Sotalol, Pindolol,

Biguanide; Glucophage
34

EDNAN

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.
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.

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Digitalis: Cardiac Glycoside

Digoxin

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Selective Estrogen Receptor Modulator

(SERM)
clomifene (an ovulation)
raloxifene (osteoporosis)
tamoxifen (breast cancer)
toremifine (breast cancer)

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

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Antiretroviral Drugs; HIV

Protease inhibitors (PIs); HIV
Saquinavir, Ritonavir, Indinavir, Nelfinavir

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 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 (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)
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Antituberculosis
Rifampin
Isoniazid

39

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

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.

Rifampicin inhibits DNA-dependent RNA polymerase in bacterial

cells by binding its beta subunit, thus preventing transcription of
messenger RNA (mRNA) and subsequent translation to proteins.
Isoniazid inhibits the mycolic acid cell wall synthesis via
oxygen-dependent pathways, such as the catalase-peroxidase
reaction.
Vancomycin is an antibiotic used in the prophylaxis and treatment
of infections caused by Gram-positive 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.

ZALJALAALE WAL IKRAM

US/CANADIAN PHARMACY EXAM

EDNAN

40

Metronidazole (Flagyl)

Metronidazole is an antibiotic and antiparasitic drug classified

as a nitroimidazole. It inhibits nucleic acid synthesis and is
used for the treatment of infections 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.

41

Polyene Antibiotics
Imidazole (Miconazole,Ketoconazole
Clotrimazole ,Econazole, Mebendazole
,Oxiconazole
Thiabendazole ,Tiaconazole)
Triazole (Fluconazole ,Itraconazole)

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

Allyalamine (Terbinafine; Lamisil)

42

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.

43

Macrolides Antibiotics
(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 16-membered.
Macrolides belong to the polyketide class of
natural products.

The mechanism of action of the macrolides is inhibition of

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.

44

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

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.

45

Finasteride (Propecia): Antiandrogen

5 alpha reductase inhibitor
Flutamide
Bicalutamide (Casodex)
Nilutamide (Anandron)

Finasteride acts by inhibiting 5-alpha reductase, the enzyme

the converts testosterone to dihydrotestosterone. It is used in
benign prostate hyperplasia (BPH) in low doses, and in prostate
cancer in higher doses. It is registered in many countries for malepattern baldness.

46

Tetracyclines
Doxycylcine
Demeclomycin
Minocycline

Tetracyclines bind to 30S subunit of bacterial ribosome, blocking

aminosyl transfer RNA on the receptor site on the m RNA
ribosomal complex

ZALJALAALE WAL IKRAM

US/CANADIAN PHARMACY EXAM

EDNAN

47

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-Pseudomonas
activity.
ceftazidime
Fourth generation cephalosporins
cefepime
Carbapenems

-lactam antibiotics are a broad class of antibiotics including

penicillin derivatives, cephalosporins, monobactams,
carbapenems and -lactamase inhibitors; basically any
antibiotic 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 Gram-positive organisms. The final
transpeptidation step in the synthesis of the peptidoglycan is
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.

48

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
Phenylheptylamines
methadone
levomethadyl acetate hydrochloride
Phenylpiperidines
pethidine (meperidine)
fentanyl , alfentanil
sufentanil
Diphenylpropylamine derivatives
propoxyphene
dextropropoxyphene
Benzomorphan derivatives
pentazocine , phenazocine
Oripavine derivatives
buprenorphine
Morphinan derivatives
butorphanol, nalbufine
tramadol, loperamide
diphenoxylate
Opioid antagonists
naloxone , naltrexone

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.
Common ADRs include: nausea and vomiting, drowsiness, dry
mouth, miosis, orthostatic hypotension, urinary retention, and
constipation
The main clinical indications of opioids include;
moderate-to-severe 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)

49

Gout
Colchicine

Colchicine inhibits the cytoskeleton by binding to tubulin, one

of the main constituents of microtubules.

Allopurinol

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.