By

P.SATHISH BABU
B- PHARMACY- V SEM
SRI RAMACHANDRA UNIVERSITY

HOSPITAL
PHARMACY
TRAINING
ASSIGNMENT
WORK

INTRODUCTION
Hospital pharmacy is a place
where we have scope to learn a lots of things. It has helped us
to train ourselves in lots of interdisciplinary phases of the
pharmacy. We really found it very helpful. Importance of
dispensing and things to be concentrated while we dispense in
such a big well developed locality where thousands of people
come every day. Though we felt that the training period was
less we had scope to learn a lot things. We thank the staff in
charge and the initiators for providing us such a good
opportunity to explore.
In this assignment I have
compiled a list of drugs available at Sri Ramachandra hospital
free pharmacy. These were the drugs what we dispensed
during our posting period. The monograph of the drugs
include the following categories:
The name and structure of the drug
IUPAC name and details about the molecule
The pharmacological action of the drug, synthesis and uses
Brand names of the particular drug available in the market
These details helps us to know
about the drugs and mode of action and their importance.
These drugs are found to be economically and medicinally

important. It is essential to know about all these as a

pharmacist.

TABLE OF CONTENTS

DIAZEPAM

DICLOFENAC

ENALAPRIL

GLIBENCLAMIDE (GLYNASE)

METFORMIN

PARACETAMOL

AMITRIPTYLINE

LEVOTHYROXINE

AMLODIPINE

CHLORTHALIDONE

MONOGRAPH OF DIAZEPAM

IUPAC: 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
FORMULA: C16H13ClN2O ; MOLECULAR MASS: 284.7 g/mol.

Diazepam is a medication of the benzodiazepine type. It is commonly used to

treat a range of conditions including anxiety, alcohol withdrawal syndrome, benzodiazepine
withdrawal syndrome, muscle spasms, seizures, trouble sleeping, and restless legs syndrome.
It may also be used to cause memory loss during certain medical procedures. It can be taken
by mouth, inserted into the rectum, injected into muscle, or injected into a vein. When given
into a vein effects begin in one to five minutes and last up to an hour. By mouth effects may
take 40 minutes to begin.
Common side effects include sleepiness and trouble with coordination. Serious side effects are
rare. They include suicide, decreased breathing, and an increased risk of seizures if used too
frequently in those with epilepsy. Occasionally excitement or agitation may occur. Long term
use can result in tolerance, dependence, and withdrawal upon dose reduction. Abrupt stopping
after long term use can be potentially dangerous. After stopping cognitive problems may
persist for six months or longer. They are not recommended during pregnancy or
breastfeeding. Its mechanism of action is by increasing the effect of the
neurotransmitter gamma-Amino butyric acid (GABA).

PHARMACOLOGY: Diazepam is a long-acting "classical" benzodiazepine. Diazepam

has anticonvulsant properties. Diazepam has no effect on GABA levels and no effect on
glutamate decarboxylase activity, but has a slight effect on gamma-amino butyric acid
transaminase activity. It differs from some other anticonvulsive drugs with which it was
compared. Benzodiazepines act via micro molar benzodiazepine binding sites
as Ca2+ channel blockers and significantly inhibit depolarization-sensitive Calcium uptake in
rat nerve cell preparations.
Diazepam inhibits acetylcholine release in mouse hippocampal synaptosomes. This has been
found by measuring sodium-dependent high-affinity choline uptake in mouse brain cells in
vitro, after pretreatment of the mice with diazepam in vivo. This may play a role in explaining
diazepam's anticonvulsant properties.
Diazepam binds with high affinity to glial cells in animal cell cultures. Diazepam at high doses
has been found to decrease histamine turnover in mouse brain via diazepam's action at the
benzodiazepine-GABA receptor complex. Diazepam also decreases prolactin release in rats.

SYNTHESIS:

MEDICINAL USES:

Treatment of anxiety, panic attacks, and states of agitation

Treatment of neurovegetative symptoms associated with vertigo

Treatment of the symptoms of alcohol, opiate, and benzodiazepine withdrawal

Short-term treatment of insomnia

Treatment of tetanus, together with other measures of intensive treatment

Adjunctive treatment of spastic muscular paresis (paraplegia/tetraplegia) caused by

cerebral or spinal cord conditions such as stroke, multiple sclerosis, or spinal cord injury
(long-term treatment is coupled with other rehabilitative measures)
Palliative treatment of stiff person syndrome

Pre- or postoperative sedation, anxiolysis and/or amnesia (e.g., before endoscopic or

surgical procedures)

Treatment of complications with a hallucinogen crisis and stimulant overdoses and

psychosis, such as LSD, cocaine, ormethamphetamine

Preventative treatment of oxygen toxicity during hyperbaric oxygen therapy

BRAND NAMES: Diastat, Valium.

MONOGRAPH OF DICLOFENAC

IUPAC: 2-(2,6-dichloranilino) phenylacetic acid.

FORMULA: C14H11Cl2NO2 ; MOLECULAR MASS: 296.148g/mol.
Diclofenac is a non steroidal anti-inflammatory drug (NSAID) taken or applied
to reduce inflammation and as an analgesic reducing pain in certain conditions. It is supplied
as or contained in medications under a variety of trade names. In the United Kingdom, United
States, India, and Brazil diclofenac may be supplied as either the sodium or potassium salt; in
China, it is most often supplied as the sodium salt, while in some other countries it is only
available as the potassium salt. Diclofenac is available as a generic drug in a number of

formulations, including diclofenac diethylamine, which is applied topically. Over-thecounter (OTC) use is approved in some countries for minor aches and pains and fever
associated with common infections.
PHARMACOLOGY:
The
primary
mechanism
responsible
for
its antiinflammatory, antipyretic,
and analgesic action
is
thought
to
be
inhibition
of prostaglandin synthesis by inhibition of cyclooxygenase (COX). It also appears to exhibit
bacteriostatic activity by inhibiting bacterial DNA synthesis.
Inhibition of COX also decreases prostaglandins in the epithelium of the stomach, making it
more sensitive to corrosion by gastric acid. This is also the main side effect of diclofenac.
Diclofenac has a low to moderate preference to block the COX2-isoenzyme (approximately
10-fold) and is said to have, therefore, a somewhat lower incidence of gastrointestinal
complaints than noted with indomethacin and aspirin.
The action of one single dose is much longer (6 to 8 hour) than the very short half-life of the
drug indicates. This could be partly because it persists for over 11 hours in synovial fluids.
Diclofenac may also be a unique member of the NSAIDs. Some evidence indicates it inhibits
the lipoxygenase pathways, thus reducing formation of the leukotrienes (also proinflammatory autacoids). It also may inhibit phospholipase A2 as part of its mechanism of
action. These additional actions may explain its high potency - it is the most potent NSAID on
a broad basis.
Marked differences exist among NSAIDs in their selective inhibition of the two subtypes of
cyclooxygenase, COX-1 and COX-2. Much pharmaceutical drug design has attempted to
focus on selective COX-2 inhibition as a way to minimize the gastrointestinal side effects of
NSAIDs such as aspirin. In practice, use of some COX-2 inhibitors with their adverse
effects has led to massive numbers of patient family lawsuits alleging wrongful death by heart
attack, yet other significantly COX-selective NSAIDs, such as diclofenac, have been well
tolerated by most of the population.
SYNTHESIS:

MEDICINAL USES:
Diclofenac is used to treat pain, inflammatory disorders, and dysmenorrhea.[4] Inflammatory
disorders may include musculoskeletal complaints, especially arthritis, rheumatoid
arthritis,polymyositis, dermatomyositis, osteoarthritis, dental pain, TMJ
pain, spondylarthritis, ankylosing spondylitis, gout attacks, and pain management in cases
of kidney stones and gallstones. An additional indication is the treatment of acute migraines.
Diclofenac is used commonly to treat mild to moderate postoperative or post-traumatic pain,
in particular when inflammation is also present, and is effective against menstrual pain
and endometriosis.
BRAND NAMES: Aclonac, Cataflam, Voltaren.

MONOGRAPH OF ENALAPRIL

IUPAC: (2S)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2yl]amino}propanoyl]pyrrolidine-2-carboxylic acid

FORMULA: C20H28N2O5 ; MOLECULAR MASS: 376.447 g/mol.

Enalapril is an angiotensin-converting-enzyme (ACE) inhibitor used in the treatment

of hypertension, diabetic nephropathy, and some types of chronic heart failure. ACE converts
the peptide hormone angiotensin I to angiotensin II. One of the actions of angiotensin II is the
vasoconstriction of blood vessels, resulting in an increase in blood pressure. ACE inhibitors
such as enalapril prevent this effect. Enalapril has been shown to lower the death rate in systolic
heart failure. Enalapril was the first member of the group known as the dicarboxylate-containing
ACE inhibitors.
PHARMACOLOGY: Normally, angiotensin I is converted to angiotensin II by angiotensinconverting enzyme (ACE). Angiotensin II constricts blood vessels, increasing blood pressure.
By inhibiting ACE, enalapril decreases levels of angiotensin II leading to less vasoconstriction
and decreased blood pressure.
SYNTHESIS:

MEDICINAL USES: Enalapril is used to treat hypertension, symptomatic heart failure, and
asymptomatic left ventricular dysfunction. It has been proven to protect the function of the
kidneys in hypertension, heart failure, and diabetes, and may be used in the absence of
hypertension for its kidney protective effects. It is widely used in chronic kidney failure.
BRAND NAMES: Vasotec

MONOGRAPH OF GLIBENCLAMIDE

IUPAC: 5-chloro-N-(4-[N-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-methoxybenzamide
FORMULA: C23H28ClN3O5S ; MOLECULAR MASS: 494.004g/mol.
Glibenclamide (AAN, BAN, INN), also known as glyburide (USAN), is
an antidiabetic drug in a class of medications known assulfonylureas, closely related

to sulfa drugs. It was developed in 1966 in a cooperative study between Boehringer

Mannheim and Hoechst.
It is sold in doses of 1.25, 2.5, and 5 mg, under the trade names Diabeta, Glynase, and
Micronase in the United States and Daonil, Semi-Daonil, and Euglucon in the United
Kingdom, and Delmide, Glybovin in India. It is also sold in combination with metformin
under the trade names Glucovance, Benimet, and Glibomet, as well as Glucored and Glucored
Forte (by Sun Pharmaceutical) in Russia, Belarus and other countries of the CIS.
PHARMACOLOGY: The drug works by binding to and activating the ATP-sensitive
potassium
channels (KATP)
inhibitory
regulatory
subunit sulfonylurea
receptor
1 (SUR1) in pancreatic beta cells. This inhibition causes cell membrane depolarization,
opening voltage-dependent calcium channels. This results in an increase in
intracellular calcium in the beta cell and subsequent stimulation of insulin release.
After a cerebral ischemic insult, the bloodbrain barrier is broken and glibenclamide can reach
the central nervous system. Glibenclamide has been shown to bind more efficiently to the
ischemic hemisphere. Moreover, under ischemic conditions SUR1, the regulatory subunit of
the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes,
endothelial cells and by reactive microglia.
MEDICINAL USES: It is used in the treatment of type 2 diabetes. As of 2011, it is one of
only two oral antidiabetics in the World Health Organization Model List of Essential
Medicines (the other being metformin). As of 2003, in the United States, it was the most
popular sulfonylurea. It is not as good as either metformin or insulin in those who
have gestational diabetes.
BRAND NAMES: Diabeta, Glynase, Micronase Daonil, Semi-Daonil, Euglucon, Delmide,
Glybovin Gilema
SYNTHESIS:

RESEARCH:
Glibenclamide improves outcome in animal stroke models by preventing brain swelling and
enhancing neuroprotection. A retrospective study showed, in type 2 diabetic patients already
taking glyburide, NIH stroke scale scores on were improved on discharge compared to
diabetic patients not taking glyburide.

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MONOGRAPH OF METFORMIN

IUPAC: N,N-Dimethylimidodicarbonimidic diamide

FORMULA: C4H11N5 ; MOLECULAR MASS: 129.16364g/mol.
Metformin is an oral antidiabetic drug in the biguanide class. It is the firstline drug of choice for the treatment of type 2 diabetes, in particular,
in overweight and obese people and those with normal kidney function. Its use in gestational
diabetes has been limited by safety concerns. It is also used in the treatment of polycystic
ovary syndrome, and has been investigated for other diseases where insulin resistance may be
an important factor. Metformin works by suppressing glucose production by the liver.
Limited evidence suggests metformin may prevent the cardiovascular and possibly the cancer
complications of diabetes. It helps reduce LDL cholesterol and triglyceride levels and is not
associated with weight gain; in some people, it promotes weight loss. Metformin is one of
only two oral antidiabetics in the World Health Organization Model List of Essential
Medicines (the other being glibenclamide).
PHARMACOLOGY: Metformin decreases hyperglycemia primarily by suppressing glucose
production by the liver (hepatic gluconeogenesis). The "average" person with type 2 diabetes
has three times the normal rate of gluconeogenesis; metformin treatment reduces this by over
one-third. The molecular mechanism of metformin is incompletely understood: inhibition of
the mitochondrial respiratory chain (complex I), activation of AMP-activated protein
kinase (AMPK), inhibition of glucagon-induced elevation of cyclic adenosine
monophosphate(cAMP), and consequent activation of protein kinase A (PKA), inhibition of
mitochondrial glycerophosphate dehydrogenase, and an effect on gut microbiota have been
proposed as potential mechanisms. Metformin and other biguanides may antagonize the action
of glucagon, thus reducing fasting glucose levels. Metformin also induces a profound shift in
the faecal microbial community profile in diabetic mice and this may contribute to its mode of
action possibly through an effect onglucagon-like peptide-1 secretion.

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MEDICINAL USES: Metformin is primarily used for type 2 diabetes, but is increasingly
being used in polycystic ovary syndrome, non-alcoholic fatty liver disease (NAFLD) and
premature puberty, three other diseases that feature insulin resistance; these indications are
still considered experimental. The benefit of metformin in NAFLD has not been extensively
studied and may be only temporary; although some randomized controlled trials have found
significant improvement with its use, the evidence is still insufficient.
BRAND NAMES: Glucophage
SYNTHESIS:

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MONOGRAPH OF PARACETAMOL

IUPAC: N-(4-hydroxyphenyl)ethanamide
N-(4-hydroxyphenyl)acetamide
FORMULA: C8H9NO2 ; MOLECULAR MASS: 151.163g/mol.
Paracetamol is classified as a mild analgesic. It is commonly used for the
relief of headaches and other minor aches and pains and is a major ingredient in
numerous cold and flu remedies. In combination with opioid analgesics, paracetamol can also
be used in the management of more severe pain such as post-surgical and cancer pain.
[13]
Though paracetamol is used to treat inflammatory pain, it is not generally classified as
an NSAID because it exhibits only weak anti-inflammatory activity.
While generally safe for use at recommended doses, even small overdoses can be fatal.
Compared to other over-the-counter pain relievers, paracetamol is significantly more toxic in
overdose but may be less toxic when used chronically at recommended doses. Paracetamol is
the active metabolite of phenacetin and acetanilide, both once popular as analgesics and
antipyretics in their own right. However, unlike phenacetin, acetanilide and their
combinations, paracetamol is not considered carcinogenic at therapeutic doses.
PHARMACOLOGY: The main mechanism proposed is the inhibition of
cyclooxygenase (COX), and recent findings suggest that it is highly selective for COX-2.
[84]
Because of its selectivity for COX-2 it does not significantly inhibit the production of the
pro-clotting thromboxanes.[84] While it has analgesic and antipyretic properties comparable to
those of aspirin or other NSAIDs, its peripheral anti-inflammatory activity is usually limited

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by several factors, one of which is the high level of peroxides present in inflammatory lesions.
However, in some circumstances, even peripheral anti-inflammatory activity comparable to
NSAIDs can be observed. the active metabolite but that this reactive compound should react
not only with the thiol in TRPA1 but also with any other suitably available nucleophile that it
happens to encounter. It is suggested that thiol groups in cysteine proteases, e.g. the proteases
that take part in the processing of procytokines, such as those generating IL-1 and IL-6,
might be the targets giving rise to overall analgesic effects.
MEDICINAL USES: Paracetamol is used for reducing fever in people of all ages
Paracetamol is used for the relief of pain, head ache, low back pain and post operative pain.
SYNTHESIS:

BRAND NAMES: Calpol, Dolo650, Palol, Ampar, Aldolol, etc.,

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MONOGRAPH OF AMITRIPTYLINE

IUPAC: 3-(10,11-Dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethylpropan-1amine
FORMULA: C20H23N ; MOLECULAR MASS: 277.403g/mol.
Amitriptyline is the most widely used tricyclic antidepressant (TCA).
Amitriptyline is chemically basic and is in the form of hydrochloride salt (pKa 9.4) in the
market. It is used to treat a number of mental disorders, including major depressive
disorder and anxiety, and less commonly psychosis, attention deficit hyperactivity disorder,
and bipolar disorder. Other uses include prevention of migraines, post herpetic
neuralgia, neuropathic pain such as fibromyalgia, and less commonly insomnia.
Side effects may include seizures, an increased risk of suicide in those less than 25 years of
age, urinary retention, and a number of heart issues. They should not be taken with MAO
inhibitors or cisapride. In the United States and Australia, they are pregnancy category C
which means that may cause problems during pregnancy. Use during breastfeeding does not
appear to be a problem.
PHARMACOLOGY: Amitriptyline acts primarily as a serotonin-norepinephrine reuptake
inhibitor, with strong actions on the serotonin transporter and moderate effects on
the norepinephrine transporter. It has negligible influence on the dopamine transporter and

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therefore does not affect dopamine reuptake, being nearly 1,000 times weaker on it than
on serotonin. It is metabolized to nortriptylinea more potent and selective norepinephrine
reuptake inhibitorwhich may complement its effects on norepinephrine reuptake.
MEDICINAL USES: Amitriptyline is used for a number of medical conditions
including major depressive disorder (MDD) which is its only FDA-labeled indication. This is
also a TGA- and MHRA-labelled indication. Some evidence suggests amitriptyline may have
superior efficacy compared to other antidepressants, including the selective serotonin reuptake
inhibitors (SSRIs), although it is rarely used as a first-line antidepressant nowadays due to its
high degree of toxicity in overdose and generally poorer tolerability than the newer
antidepressants such as the SSRIs and serotonin-norepinephrine reuptake inhibitors.
BRAND NAMES: Amitrip, Elevil, Endep, Levate
SYNTHESIS:

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MONOGRAPH OF LEVOTHYROXINE

IUPAC: (S)-2-Amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoic acid

FORMULA: C15H11I4NO4 ; MOLECULAR MASS: 776.87g/mol.
Levothyroxine (INN, USAN) or L-thyroxine is a synthetic thyroid hormone that is
chemically identical to thyroxine (T4), which is naturally secreted by the follicular cells of
the thyroid gland. It is used to treat thyroid hormone deficiency, and occasionally to prevent
the recurrence of thyroid cancer. Like its naturally secreted counterpart, levothyroxine is
a chiral compound in the L-form. The related drug dextrothyroxine (D-thyroxine) was used in
the past as a treatment for hypercholesterolemia (elevated cholesterol levels) but was
withdrawn due to cardiac side effects.
PHARMACOLOGY: Levothyroxine is a synthetic form of thyroxine (T4), an endogenous
hormone secreted by the thyroid gland, which is converted to its active metabolite, Ltriiodothyronine (T3). T4 and T3 bind to thyroid receptor proteins in the cell nucleus and
cause metabolic effects through the control of DNA transcription and protein synthesis.
MEDICINAL USES: Levothyroxine is typically used to treat hypothyroidism,[5] and is the
treatment of choice for patients with hypothyroidism, [6] who often require lifelong thyroid
hormone therapy.[7] It may also be used to treat goiter via its ability to lower thyroidstimulating hormone(TSH), a hormone that is considered goiter-inducing.
BRAND NAMES: Thyronorm
SYNTHESIS:

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MONOGRAPH OF AMLODIPINE

IUPAC: (RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4dihydropyridine-3,5-dicarboxylate

FORMULA: C H ClN O ; MOLECULAR MASS: 408.879g/mol.
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25

Amlodipine (as besylate, mesylate or maleate) is a medication used to lower blood

pressure and prevent chest pain. It belongs to a group of medications known
as dihydropyridine-type calcium channel blockers. Widening of these blood vessels lowers
blood pressure. In angina, amlodipine increases blood flow to the heart muscle to relieve pain
due to angina. It is on the World Health Organization's List of Essential Medicines, the most
important medications needed in a basic health system.
PHARMACOLOGY: Amlodipine inhibits calcium ions into vascular smooth muscle cells
and cardiac muscle cells. The contractile processes of cardiac muscle and vascular smooth

18

muscle are dependent upon the movement of extracellular calcium ions into these cells
through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes
selectively, with a greater effect on vascular smooth muscle cells. Negative inotropic effects
can be detected in vitro, but such effects have not been seen in intact animals at therapeutic
doses. Serum calcium concentration is not affected by amlodipine. Amlodipine is a peripheral
arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in
peripheral vascular resistance and reduction in blood pressure. As a calcium channel blocker,
amlodipine is expected to inhibit the currents of L-type Cav1.3 channels in the zona
glomerulosa.
MEDICINAL USES: Amlodipine is used in the management of hypertension[4] and coronary
artery disease.
BRAND NAMES: Norvasc

SYNTHESIS:

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MONOGRAPH OF CHLORTHALIDONE

IUPAC: (RS)-2-Chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1sulfonamide
FORMULA: C14H11ClN2O4S ; MOLECULAR MASS: 338.766g/mol.
Chlortalidone (INN/BAN) or chlorthalidone (USAN) is a diuretic drug used to
treat hypertension, originally marketed as Hygroton in the USA. It is described as a thiazide
diuretic (or, rather, a thiazide-like diuretic because it acts similarly to the thiazides but does
not contain the benzothiadiazine molecular structure). Compared with other medications of
the thiazide class, chlortalidone has the longest duration of action but a similar diuretic effect
at maximal therapeutic doses. It is often used in the management of hypertension and edema.
PHARMACOLOGICAL ACTION: Chlortalidone prevents reabsorption of sodium and
chloride by inhibiting the Na+/Cl symporter in the distal convoluted tubule. Thiazides and
related compounds also decrease the glomerular filtration rate, which further reduces the
drug's efficacy in patients with renal impairment (e.g. renal insufficiency). By increasing the
delivery of sodium to the distal renal tubule, chlortalidone indirectly increases potassium
excretion via the sodium-potassium exchange mechanism (i.e. apical ROMK/Na channels
coupled with basolateral NKATPases). This can result in hypokalemia and hypochloremia as

20

well as a mild metabolic alkalosis; however, the diuretic efficacy of chlortalidone is not
affected by the acid-base balance of the patient being treated.
Initially, diuretics lower blood pressure by decreasing cardiac output and reducing plasma and
extracellular fluid volume. Eventually, cardiac output returns to normal, and plasma and
extracellular fluid volume return to slightly less than normal, but a reduction in peripheral
vascular resistance is maintained, thus resulting in an overall lower blood pressure. The
reduction in intravascular volume induces an elevation in plasma renin activity and
aldosterone secretion, further contributing to the potassium loss associated with thiazide
diuretic therapy.
MEDICINAL USES: Diuretic, used to treat hypertension

SYNTHESIS:

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BIBLIOGRAPHY
www.wikipedia.org
www.google.com/patents
www.drugs.com

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THANK
YOU !!!

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