Monograph
Monograph
BS PHARMACY 2F
DRUG
MONOGARPH
PREPARED BY:
KENNETH ANGELO C.
MANTIGUE
PHCHEM 205
Pharmaceutical & Medicinal
Organic Chemistry
TABLE OF
CONTENTS
Antibacterials 1
Anti Infectives 9
Anti Malarias 22
Antivirals 25
CNS Depressants 29
CNS Stimulants 37
Adrenergic Agents 43
Cholinergic Agents 48
Histamine & Antihistamine Agents 52
Diuretics 57
Cardiovascular Agents 61
Analgesic Agents 71
Cough Agents 76
Local Anesthetic Agents 80
Prostaglandins 85
Leukotrienes 90
Eicosanoids 92
Antineoplastic Agents 97
ANTI
BACTERIALS
Antibiotics specifically treat infections caused by bacteria, such as
Staph., Strep., or E. coli., and either kill the bacteria (bactericidal) or keep
it from reproducing and growing (bacteriostatic). Antibiotics do not work
against any viral infection.
1
Amoxicillin Trihydrate
C16H19N3O5S
Oxacillin
C19H19N3O5S
Color:
White
State/form:
Crystalline powder
MOA AND USES
Description:
Oxacillin is a penicillin antibiotic used to treat a number of Soluble in organic solvents such as
susceptible bacterial infections, particularly in staphylococci ethanol, DMSO, and dimethyl
formamide.
resistant infections. By binding to specific penicillin-binding
proteins (PBPs) located inside the bacterial cell wall, Oxacillin Melting point:
inhibits the third and last stage of bacterial cell wall synthesis 188 °C
Aztreonam
C13H17N5O8S2
State/form:
MOA AND USES Crystalline powder
Aztreonam is a beta-lactam antibiotic used to treat select Description:
aztreonam-sensitive gram-negative bacteria. The bactericidal It is soluble in organic solvents such
action of aztreonam results from the inhibition of bacterial cell as ethanol, DMSO, and dimethyl
wall synthesis due to a high affinity of aztreonam for penicillin- formamide (DMF).
binding protein 3 (PBP3). By binding to PBP3, aztreonam inhibits
the third and last stage of bacterial cell wall synthesis Melting point:
227 °C
2
Cephalexin
C16H17N3O4S
State/form:
MOA AND USES Crystalline powder
Erythromycin Estolate
C37H67NO13
State/form:
N/A
MOA AND USES
Description:
Erythromycin is used to treat certain infections caused by
Erythromycin estolate is freely
bacteria, such as infections of the respiratory tract, including soluble in organic solvents but
bronchitis, pneumonia, Legionnaires' disease (a type of lung practically insoluble in water.
infection), and pertussis; diphtheria (a serious infection in the
throat); sexually transmitted diseases (STD), including syphilis; Melting point:
and ear, intestine, gynecological, urinary tract, and skin 135-140°C
infections.
Netilmicin
C21H41N5O7
Color:
ON:
white
Netilmicin Sulfate
MOA AND USES State/form:
N/A
It’s used for the treatment of bacteremia, septicemia, and
respiratory tract infections, skin and soft-tissue infection, burns, Description:
wounds, and peri-operative infections caused by susceptible Soluble in water (288 mg/ml at 25° C),
strains. Acts with interference with the initiation complex, DMSO (<1 mg/ml at 25° C), and
misreading of mRNA so incorrect amino acids are inserted into the ethanol (<1 mg/ml at 25° C).
polypeptide leading to nonfunctional or toxic peptides and the
breakup of polysomes into nonfunctional monosomes, leaving the Melting point:
194-198° C
bacterium unable to synthesize proteins vital to its growth.
3
Rolitetracycline
C27H33N3O8
Bacitracin
C66H103N17O16S
Color:
ON: Colorless to light yellowish
Bacitracina
Bacitracin A State/form:
Solid
MOA AND USES
Description:
Bacitracin is a cyclic polypeptide antibiotic used to prevent very soluble in water and methanol;
wound infections, treat pneumonia and empyema in infants, and soluble in ethanol; slightly soluble in
acetone, benzene, and ether; and
treat skin and eye infections. Bacitracin binds to divalent metal practically insoluble in chloroform,
ions such as Mn(II), Co(II), Ni(II), Cu(II), or Zn(II).1 These complexes ether, and acetone
bind C55-isoprenyl pyrophosphate, preventing the hydrolysis of
a lipid dolichol pyrophosphate, which finally inhibits cell wall Melting point:
221 - 225 °C
synthesis.
Cefaclor
C15H14CIN3O4S
State/form:
MOA AND USES Dry powder
Clavulanate
C8H9NO5
ON: State/form:
Clavulanic acid powder
MOA AND USES
Description:
Clavulanic acid is a beta-lactamase inhibitor that is frequently The solubility of potassium
combined with [Amoxicillin] or [Ticarcillin] to fight antibiotic clavulanate in ethanol, 1-propanol, 1-
resistance by preventing their degradation by beta-lactamase butanol, between 273 K and 305 K
enzymes, broadening their spectrum of susceptible bacterial were measured using a laser
technique.
infections. Clavulanic acid is derived from the organism
Streptomyces clavuligerus.When it is combined with amoxicillin, Melting point:
clavulanic acid is frequently known as Augmentin, Co-Amoxiclav, 117.5 - 118 °C
or Clavulin.
Clindamycin
C18H33ClN2O5S
Gentamicin
C21H43N507
Melting point:
105 °C
Lincomycin
C18H34N2O6S
State/form:
MOA AND USES crystal
Linezolid is indicated in adults and children for the treatment of
infections caused by susceptible Gram-positive bacteria, Description:
including nosocomial pneumonia, community-acquired The aqueous solubility is
pneumonia, skin and skin structure infections, and vancomycin- approximately 3 mg/mL.
resistant Enterococcus faecium infections.
Melting point:
181.5-182.5 °C
Minocycline
C23H27N3O7
Mupirocin
C26H44O9
Polymyxin B Sulfate
C56H98N16O13
8
ANTI
INFECTIVES
They are drugs that are capable of acting against infection, either by
inhibiting the spread of an infectious agent or by killing the infectious
agent outright.
9
Benzalkonium chloride
C27H42ClNO2
Ethyl alcohol
C2H5OH
Boiling point:
78.5 °C
Flucytosine
C4H4FN3O
Color:
White
Hexachlorophene
C13H6CI6O2
Hexylresorcinol
C12H18O2
Isopropyl alcohol
(CH3)2CHOH
Boiling point:
82.3 °C
Metronidazole
C6H9N3O3
State/form:
MOA AND USES Crystalline powder
Povidone-iodine
C6H9I2NO
Pyrantel pamoate
C34H30N2O6S
Ciprofloxacin
C17H18FN3O3
Dapsone
C12H12N2O2S
State/form:
MOA AND USES Crystalline powder
Dapsone is used to treat leprosy (Hansen's disease) and to help
control dermatitis herpetiformis, a skin problem. It inhibits the Description:
synthesis of dihydrofolic acid through by competing with para- Soluble in alcohol, methanol,
aminobenzoic acid for the active site of dihydropteroate acetone, dilute hydrochloric acid.
synthetase Practically insoluble in water.
Melting point:
175-176 °C
Gentian violet
C25N3H30Cl
Ketoconazole
C26H28Cl2N4O4
Lindane
C6H6Cl6
State/form:
MOA AND USES Amorphous powder
Methylparaben
C8H8O3
Methylene blue
C16H18ClN3S
State/form:
MOA AND USES Crystalline solid
Nifurtimox is in a class of medications called antiprotozoals. It
works by killing the organism that can cause Chagas disease. Description:
Nitroreductase activity results in the formation of nitro anion Nifurtimox is poorly soluble in water.
radicals causing the formation of oxygen radicals that result in
decreased protein and nucleic acid synthesis, breakage of DNA, Melting point:
and inhibition parasite growth. 180 to 182 °C
Nitrofurantoin
C8H6N4O5
Nitromersol
C7H5HgNO3
State/form:
Solid granules or powder
Melting point:
N/A 18
Nystatin
C47H75NO17
Permethrin
C21H20Cl2O3
Rifampin
C43H58N4O12
State/form:
MOA AND USES Crystalline powder
Sulfamethoxazole and trimethoprim are antibiotics used in
combination to treat infections including urinary tract infections, Melting point:
middle ear infections (otitis media), and shigellosis (bacillary N/A
dysentery). It acts by inhibiting the synthesis of dihydrofolic
acid. Trimethoprim inhibits thymidine and DNA synthesis. These
two agents act synergistically in inhibiting folic acid synthesis.
Thimerosal
C9H9HgNaO2S
Undecylenic acid
C11H20O2
21
ANTI
MALARIALS
Antimalarial drugs are used for the treatment and prevention of malaria
infection. Most antimalarial drugs target the erythrocytic stage of
malaria infection, which is the phase of infection that causes
symptomatic illness.
22
Chloroquine
C18H26CIN3
Doxycycline
C22H24N2O8
24
ANTI
VIRALS
Antivirals are medications that help your body fight off certain viruses
that can cause disease. Antiviral drugs are also preventive. They can
protect you from getting viral infections or spreading a virus to others.
25
Acyclovir
C8H11N5O3
Idoxuridine
C9H11IN2O5
Zidovudine
C10H13N5O4
State/form:
Crystalline powder
MOA AND USES
Description:
By disrupting the enzyme's catalytic site, delavirdine binds
The aqueous solubility of delavirdine
directly to viral reverse transcriptase (RT) and inhibits the RNA- free base at 23°C is 2,942 mcg/mL at
dependent and DNA-dependent DNA polymerase activities. pH 1.0, 295 mcg/mL at pH 2.0, and
Delavirdine does not cure or prevent HIV infection or AIDS; 0.81 mcg/mL at pH 7.4.
however, it appears to prevent HIV from reproducing and delay
the immune system's deterioration. This may delay the onset of Melting point:
problems typically associated with HIV or AIDS 226 - 228 °C
Nevirapine
C15H14N4O
Ritonavir
C37H48N6O5S2
Melting point:
349.84 °C
Stavudine
C10H12N2O4
State/form:
Crystalline solid
MOA AND USES
Stavudine is converted to stavudine 5'-triphosphate, which Description:
competes for incorporation into viral DNA with thymidine 5'- The solubility of stavudine at 23° C is
triphosphate. Stavudine is utilized in combination with other approximately 83 mg/mL in water and
drugs to treat infections caused by the human 30 mg/mL in propylene glycol.
immunodeficiency virus (HIV).
Melting point:
159 - 160 °C
28
CNS
DEPRESSANTS
Central nervous system (CNS) depressants are drugs that can slow down
brain activity. A physician may prescribe CNS depressants to treat
anxiety, muscle tension, pain, insomnia, acute stress reactions, panic
attacks, and seizure disorders. In higher doses, some CNS depressants
may be used as general anesthetics.
29
Carbamazepine
C15H12N2O
ON: State/form:
CBZ Crystal
MOA AND USES
Description:
Na+ Channel Blocker It is practically insoluble in water and
Carbamazepine treats certain types of seizures (e.g., partial ether but soluble in acetone, alcohol,
carbon tetrachloride, chloroform,
seizures, tonic-clonic seizures) and bipolar disorder. It is also dimethylformamide dioxane, and
used to relieve pain caused by trigeminal neuralgia (tic propylene glycol
douloureux).
Melting point:
190 to 193°C
Diazepam
C16H13ClN2O
State/form:
MOA AND USES Solid crystals
GABA Stimulator
Diazepam is a benzodiazepine used to treat anxiety, acute Description:
alcohol withdrawal, and seizures, also used to relieve muscle Odorless, slightly bitter taste. The pH
spasms and to provide sedation before medical procedures. It is neutral.
works by enhancing the effects of a certain natural chemical in
the body (GABA). Melting point:
131.5 to 134.5 C
Enflurane
C3H2ClF5O
Boiling point:
56.5°C 30
Halothane
C2HBrClF3
State/form:
MOA AND USES Liquid
Halothane is a general inhalation anesthetic used for the
induction and maintenance of general anesthesia. Description:
HIGHLY VOLATILE COLORLESS
LIQUID WITH CHARACTERISTIC ODOR
Boiling point:
50°C
Ketamine
C13H16ClNO
Phenytoin
C15H12N2O2
Color:
ON: Yellow
Penthiobarbital
Thiopentone State/form:
hygroscopic powder
MOA AND USES
Description:
GABA-A Modulator At 20˚C, thiopental sodium is soluble
Thiopental is a barbiturate used to induce general anesthesia, in 1.5 parts of water. It is partially
soluble in alcohol and is practically
treat convulsions, and reduce intracranial pressure. insoluble in ether, benzene, and
petroleum ether.
Melting point:
158-160°C
Chlorpromazine
C17H19ClN2S
State/form:
MOA AND USES Oily liquid
Clozapine
C18H19ClN4
Melting point:
85-87 °C
Haloperidol
C21H23ClFNO2
State/form:
MOA AND USES Amorphous or micro-crystalline
powder
Dopamine 2 Receptor Antagonist
Haloperidol is used to treat psychotic disorders; is also used to Description:
control motor tics and verbal tics in adults and children who Freely sol in chloroform, methanol,
have Tourette's disorder. Haloperidol is also used to treat severe acetone, benzene, dil acids
behavioral problems such as explosive, aggressive behavior or
hyperactivity in children who cannot be treated with Melting point:
psychotherapy or with other medications 151.5 °C
Lamotrigine
C9H7Cl2N5
Color:
White to pale colored powder
State/form:
Crystals from isopropanol
MOA AND USES
Description:
Na+ Channel Blocker
Lamotrigine is very slightly soluble in
Lamotrigine is an anti-epileptic medication, also called an water (0.17 mg/mL at 25°C) and
anticonvulsant. Lamotrigine is used alone or with other slightly soluble in 0.1 M HCl (4.1
medications to treat epileptic seizures in adults and children. mg/mL at 25°C)
Lamotrigine is also used to delay mood episodes in adults with
bipolar disorder (manic depression). Melting point:
177-181°C
33
Lithium Carbonate
Li2CO3
Melting point:
723 °C
Lorazepam
C15H10Cl2N2O2
State/form:
solid-crystals
MOA AND USES
Description:
Lorazepam is used to treat anxiety disorders. It is also used for
Loprazepam is odourless or almost
short-term relief of the symptoms of anxiety or anxiety caused odourless. It is practically insoluble in
by depression. water; sparingly soluble in alcohol;
slightly soluble in chloroform.
Melting point:
166 - 168 °C
Loxapine
C18H18ClN3O
State/form:
Crystals, powder
MOA AND USES
Description:
GABA A Receptor Agonist Meprobamate has a low solubility in
Meprobamate is used to treat anxiety disorders or for short-term water, is resistant to gastric and
intestinal juices, and decreases
relief of the symptoms of anxiety in adults and children 6 years gastric motility; bezoar formation is
of age and older. Meprobamate is in a class of medications called more likely than with other sedative-
tranquilizers. It works by slowing activity in the brain to allow for hypnotics.
relaxation.
Melting point:
105 °C
Phenobarbital
C12H12N2O3
State/form:
MOA AND USES Crystals
Melting point:
174 °C
Remoxipride
C16H23BrN2O3
Color:
N/A
State/form:
MOA AND USES N/A
Melting point:
173° 35
Risperidone
C23H27FN4O2
State/form:
MOA AND USES Powder, crystals
Thioridazine
C21H26N2S2
State/form:
crystals
MOA AND USES
Description:
Thioridazine is used to treat the symptoms of schizophrenia in
Soluble in alcohol (1 in 6), chloroform
people who have already been treated with at least two other (1 in 0.81), ether (1 in 3); freely soluble
medications and have not been helped or who have experienced in dehydrated alcohol. Insoluble in
severe side effects. water
Melting point:
72-74 °C
36
CNS
STIMULANTS
A type of drug that increases the levels of certain chemicals in the brain
and increases alertness, attention, energy, and physical activity. CNS
stimulants also raise blood pressure and increase heart rate and
breathing rate.
37
Doxapram
C24H30N2O2
Description:
MOA AND USES Insoluble in ether
Doxapram produces respiratory stimulation mediated through
the peripheral carotid chemoreceptors. The physiologic effect of Melting point: 217-219°C
doxapram is by means of Increased Medullary Respiratory Drive.
Amphetamine
C9H13N
Methamphetamine
C10H15N
38
Phentermine
C10H15N
Tranylcypromine
C9H11N
Imipramine
C19H24N2
39
Desipramine
C18H22N2
Amitriptyline
C20H23N
Nortriptyline
C19H21N1
40
Doxepin
C19H21NO
Fluoxetine
C17H18F3NO
Buspirone
C21H31N5O2
41
Mirtazapine
C17H19N3
Bupropion
C13H18ClNO
Phenelzine
C8H12N2
42
ADRENERGIC
AGENTS
These drugs stop catecholamines from being released or stop them from
doing their job. These agents have different ways of doing what they do,
such as binding directly to or adrenoceptors or stopping sympathetic
activity in the periphery or the center of the body.
43
Metyrosine
C10H13NO3
State/form:
MOA AND USES Powder
Metyrosine inhibits tyrosine hydroxylase, which catalyzes the
first transformation in catecholamine biosynthesis, i.e., the Description:
conversion of tyrosine to dihydroxyphenylalanine (DOPA). It is Very slightly soluble
used to treat high blood pressure (hypertension) caused by a
disease called pheochromocytoma. Melting point:
315.5°C
Dipivefrin
C19H29NO5
Phenylephrine
C9H13NO2
Clonidine
C9H9Cl2N3
Propranolol
C16H21NO2
Dobutamine
C18H23NO3
State/form:
MOA AND USES Dextrose injection solution
Dobutamine directly stimulates beta-1 receptors of the heart to
increase myocardial contractility and stroke volume, resulting in Description:
increased cardiac output. Dobutamine is a medication that treats Soluble in water
heart failure by strengthening your heart muscle.
Melting point:
184-186°C
Prazosin
C19H21N5O4
47
CHOLINERGIC
AGENTS
Cholinergic medications are a category of pharmaceutical agents that
act upon the neurotransmitter acetylcholine, the primary
neurotransmitter within the parasympathetic nervous system (PNS).
48
Acetylcholine
C7H16NO2
Pilocarpine
C11H16N2O2
Physostigmine
C15H21N3O2
State/form:
MOA AND USES Microcrystalline powder
Physostigmine inhibits acetylcholinesterase, the enzyme
responsible for the breakdown of used acetylcholine. By Description:
interfering with the metabolism of acetylcholine, physostigmine Slightly soluble in water; soluble in
indirectly stimulates both nicotinic and muscarinic receptors
due to the consequential increase in available acetylcholine at alcohol, benzene, chloroform, oils
the synapse. Physostigmine is a medication most commonly
used to manage and treat antimuscarinic toxicity and glaucoma. Melting point:
105-106 °C
49
Atropine
C17H23NO3
Hyoscyamine
C17H23NO3
Biperiden
C12H29NO
Atracurium
C53H72N2O12+2
State/form:
Powder
MOA AND USES
Description:
Atracurium antagonizes the neurotransmitter action of Atracurium (besylate) is soluble in
acetylcholine by binding competitively with cholinergic receptor organic solvents such as ethanol,
DMSO, and dimethyl formamide
sites on the motor end-plate. Atracurium is indicated as an (DMF), which should be purged with
addition to general anesthesia to facilitate endotracheal an inert gas.
intubation and provide skeletal muscle relaxation during surgery
or mechanical ventilation. Melting point:
185 - 194 °C
51
HISTAMINE &
ANTIHISTAMINE
AGENTS
Histamine is an ingredient of topical drugs for the relief of joint pain or
muscle aches and pains. Histamine acts directly on the blood vessels to
dilate arteries and capillaries; this action is mediated by both H 1- and H
2-receptors. An antihistamine is a prescription or over-the-counter
medication that blocks some of what histamine does. “Anti” means
against, so antihistamines are medicines that work against or block
histamine.
52
Diphenhydramine
C17H21NO
Meclizine
C25H27ClN2
Chlorpheniramine
C16H19ClN2
Melting point:
130 - 135 °C
53
Promethazine
C17H20N2S
Melting point: 60 °C
Fexofenadine
C32H39NO4
Loratadine
C22H23ClN2O2
Melting point:
134 - 136 °C
54
Cetirizine
C21H25ClN2O3
Cimetidine
C10H16N6S
Omeprazole
C17H19N3O3S
ON: Color:
Prilosec White to off-white
State/form:
MOA AND USES Crystalline powder
56
DIURETICS
Diuretics, often known as water pills, aid in the removal of salt (sodium)
and water from the body. The majority of these medications assist your
kidneys in releasing more sodium into your urine. The salt aids in the
removal of water from your blood, reducing the amount of fluid passing
through your veins and arteries.
.
57
Acetazolamide
C4H6N4O3S2
Furosemide
C12H11ClN2O5S
Ethacrynic acid
C13H12Cl2O4
58
Spironolactone
C24H32O4S
Triamterene
C12H11N7
Amiloride
C6H8ClN7O
60
CARDIO-
VASCULAR
AGENTS
The term "cardiovascular drugs" refers to a group of substances used to
treat various cardiac conditions, including hypertension, congestive heart
failure, angina, and arrhythmia.
61
Nitroglycerin
C3H5N3O9
Melting point: 14 °C
Isosorbide dinitrate
C6H8N2O8
Verapamil
C27H38N2O4
Nifedipine
C17H18N2O6
Aspirin
C9H8O4 or CH3COOC6H4COOH
Captopril
C9H15NO3S
Losartan
C22H23ClN6O
ON:
allisartan
State/form: Solid
Lortaan
MOA AND USES
Losartan is an antihypertensive nonpeptide angiotensin II
antagonist. Losartan and its active metabolite selectively and Description:
competitively block angiotensin II binding to the angiotensin I sparingly soluble in ethyl acetate,
(AT1) receptor after treatment. This inhibits angiotensin II's butyl acetate, and cyclohexane
vasoconstriction and aldosterone secretion, resulting in a drop in
blood pressure
Melting point: 184 °C
64
Reserpine
C33H40N2O9
Terazosin
C19H25N5O4
Methyldopa
C10H13NO4
Minoxidil
C9H15N5O
Digoxin
C41H64O14
ON:
Lanoxin State/form: Solid
12 beta-Hydroxy Digitoxin
Digacin Description:
MOA AND USES freely soluble in pyridine, slightly
soluble in 1:1 ethanol:water,
Digoxin is classified as a cardiac glycoside. Digoxin inhibits the chloroform, and practically insoluble
sodium potassium ATPase (ATPase) pump, raising intracellular in water and ether
calcium and improving cardiac contractility. This drug also works
directly on the atrioventricular node, inhibiting conduction and
Melting point: 230–265 °C
reducing conduction velocity
66
Clofibrate
C12H15ClO3
Cholestyramine
C27H47ClN2
Simvastatin
C25H38O5
Tolbutamide
C12H18N2O3S
Glipizide
C21H27N5O4S
Levothyroxine
C15H11I4NO4
Propylthiouracil
C7H10N2OS
70
ANALGESIC
AGENTS
Agents which selectively relieve pain by acting in the CNS or peripheral
pain mechanisms without significantly altering consciousness
71
Morphine
C17H19NO3
Codeine
C18H21NO3
Nalbuphine
C21H27NO4
ON: Color:
Nalbufina White to colorless
Intapan
State/form:
MOA AND USES solid
It interacts with an opiate receptor site in the CNS (probably in
or associated with the limbic system). Nalbuphine is used for the Description:
relief of moderate to severe pain, for pre-operatively analgesia, Its solubility is 35.5 mg/mL at 25 °C as
supplement to balance anesthesia, surgical anesthesia, and HCl salt
obstetrical analgesia.
Melting point:
230 °C as HCl salt
72
Tramadol
C16H25NO2
Propoxyphene
C22H29NO2
Mefenamic acid
C15H15NO2
State/form:
Solid crystalline powder
MOA AND USES
Description:
Mefenamic Acid is an anthranilic acid and non-steroidal anti- In water, at pH 7.1, solubility is
inflammatory drug (NSAID) with anti-inflammatory, antipyretic 0.0041 g/100mL (at 25 °C), 0.008
and analgesic activities. Mefenamic acid inhibits the activity of g/100 ML (at 37 °C); soluble in
the enzymes cyclo-oxygenase I and II, resulting in a decreased solution of alkali hydroxides;
sparingly soluble in ether,chloroform;
formation of precursors of prostaglandins and thromboxanes.
slightly soluble in ethanol
The resulting decrease in prostaglandin synthesis, by
prostaglandin synthase, is responsible for the therapeutic Melting point:
effects of mefenamic acid. 230-231 °C 73
Indomethacin
C19H16ClNO4
State/form:
MOA AND USES crystalline powder
Melting point:
160 °C
Sulindac
C20H17FO3S
ON: Color:
Sulindacum Yellow
Imbaral
State/form:
MOA AND USES solid
Sulindac is used for acute or long-term use in the relief of signs
and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing Description:
spondylitis, acute painful shoulder (acute subacromial Solubility in water is 3000 mg/L at pH
bursitis/supraspinatus tendinitis), and acute gouty arthritis. 7
Melting point:
183 °C
Ibuprofen
C13H18O2
Celecoxib
C17H14F3N3O2S
State/form:
MOA AND USES Solid
Celecoxib is a non-steroidal anti-inflammatory drug (NSAID)
selectively for inhibition of cycloxgenase -2 (Cox-2), which is Description:
widely used in the therapy of arthritis. It is used to treat Poorly soluble in water
osteoarthritis, rheumatoid arthritis, acute pain, menstrual
symptoms, and to reduce polyps is familial adenomatous Melting point:
polyposis. 157-159 °C
Acetaminophen
C8H9NO2
76
Bromhexine
C14H20Br2N2
Ambroxol
C13H18Br2N2O
Acetylcysteine
C5H9NO3S
Salbutamol
C13H21NO3
Dextromethorphan
C18H25NO
ON State/form:crystalline powder
DXM
MOA AND USES Description: soluble in water
Dextromethorphan is a levorphanol derivative and codeine
analog commonly used as a cough suppressant and also a drug Melting point: 109-111 °C
of abuse. Although similar in structure to other opioids, it has
minimal interaction with opioid receptors. Dextromethorphan
exhibits antitussive activity and is devoid of analgesic or
addictive property. This agent crosses the blood-brain-barrier
and activates sigma opioid receptors on the cough center in the
central nervous system, thereby suppressing the cough reflex.
78
Erdosteine
C8H11NO4S2
Guaifenesin
C10H14O4
79
LOCAL
ANESTHETIC
AGENTS
Local anesthesia, also called local anesthetic, is usually a one-time
injection of medicine that numbs a small area of the body. It is used for
procedures such as performing a skin biopsy or breast biopsy, repairing a
broken bone, or stitching a deep cut.
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Cocaine
C17H21NO4
Procaine
C13H20N2O2C13H20N2O2
Tetracaine
C15H24N2O2
81
Lidocaine
C14H22N2O
Bupivacaine
C18H28N2O
Benzocaine
C9H11NO2
O Articaine
C13H20N2O3S
S
OCH 3 BRAND NAMES/ OTHER NAMES PHYSICOCHEMICAL PROPERTIES
BN Molecular weight: 284.38
NH Septocaine
O Color: Clear
NH
State/form: Injectable solution
Mepivacaine
C15H22N2O
83
Prilocaine
C13H20N2O
84
PROSTA-
GLANDINS
One of several hormone-like substances made by the body. Different
prostaglandins control blood pressure, contraction of smooth muscles,
and other processes within tissues where they are made.
85
Carboprost tromethamine
C25H47NO8
Misoprostol
C22H38O5
State/Form:
MOA AND USES Oil
Misoprostol is a synthetic prostaglandin E1 analog that inhibits
basal and nocturnal gastric acid secretion through direct Description:
stimulation of prostaglandin E1 receptors on parietal cells in the The solubility of misoprostol in PBS,
stomach. pH 7.2, is approximately 1.6 mg/ml.
Melting Point:
261-263°C
Sulprostone
C23H31NO7S
State/Form
MOA AND USES Solid
Sulprostone is a prostaglandin analogue used to treat post-
partum hemorrhaging, induce medical abortion, and induce Description:
labour in instances of in utero fetal death. Sulprostone has been Soluble in methyl acetate
used in trials studying Abortion, Induced.
Melting Point:
79.25°C
86
Treprostinil
C23H34O5
Melting Point:
90-100°C
Bimatoprost
C25H37NO4
Epoprostenol
C20H32O5
Limaprost
C22H36O5
State/form:
Solid
Description:
MOA AND USES Its water solubility is 0.0248 mg/mL
Limaprost is used for the improvement of various ischemic
symptoms such as ulcer, pain and feeling of coldness associated Melting point:
with thromboangiitis obliterans as well as improvement of 100 - 103 °C
subjective symptoms (pain and numbness of lower legs) and gait
ability associated with acquired lumbar spinal canal stenosis (in
patients with bilateral intermittent claudication showing normal
SLR test result).
Dinoprostone
C20H32O5
State/form:
Liquid
Description:
MOA AND USES Its water solubility is 0.0306 mg/mL
Unoprostone is a prostaglandin analogue used to lower
intraocular pressure in patients with open-angle glaucoma or
ocular hypertension who are clinically unresponsive to other
ocular antihypertensive agents.
89
LEUKO-
TRIENES
They can help prevent breathing problems associated with allergies,
asthma and chronic obstructive pulmonary disease. Examples include
montelukast, zafirlukast and zileuton.
90
Montelukast
C35H36ClNO3S
Zafirlukast
C31H33N3O6S
Zileuton
C11H12N2O2S
Description:
MOA AND USES Practically insoluble in water (0.5
Zileuton is an antiinflammatory leukotriene pathway inhibitor mg/ml)
classified as an inhibitor of the enzyme 5-lipoxygenase that is
used in the treatment of asthma and allergic rhinitis. Zileuton has Melting point:
been linked to rare cases of drug induced liver disease and is 144.2-145.2 °C
considered to be contraindicated in patients with active liver
disease.
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EICOSA-
NOIDS
Eicosanoids are potent chemical messengers that have well-established
roles in regulation of inflammation, immunity, platelet aggregation,
smooth muscle contraction and renal function
92
Celecoxib
C17H14F3N3O2S
ON State/form: Solid
Celebra
Onsenal Description: Soluble in DMSO at 200
MOA AND USES mg/mL; soluble in ethanol at 100
mg/mL; very poorly soluble in water;
Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is a maximum solubility in plain water is
nonsteroidal anti-inflammatory drug (NSAID) which is known for estimated to be about 10-50 µM;
its decreased risk of causing gastrointestinal bleeding compared buffers, serum, or other additives
to other NSAIDS.16 It is used to manage symptoms of various may increase or decrease the
types of arthritis pain and in familial adenomatous polyposis aqueous solubility
(FAP) to reduce precancerous polyps in the colon.
Melting point: 157-159 °C
Rofecoxib
C17H14O4S
State/form: Solid
Aspirin
C9H8O4
Ibuprofen
C13H18O2
Naproxen
C14H14O3
State/form: Solid
Diclofenac
C14H11Cl2NO2
Beclomethasone
C28H37ClO7
96
ANTI
NEOPLASTIC
AGENTS
Antineoplastic drugs are medications used to treat cancer. Other names
for antineoplastic drugs are anticancer, chemotherapy, chemo, cytotoxic,
or hazardous drugs.
97
Cyclophosphamide
C7H15Cl2N2O2P
Ifosfamide
C7H15Cl2N2O2P
Thiotepa
C6H12N3PS
Busulfan
C6H14O6S2
Carmustine
C5H9Cl2N3O2
State/form: Liquid
Carboplatin
C6H12N2O4Pt
Altretamine
C9H18N6
101
PHCHEM 205
Pharmaceutical & Medicinal
Organic Chemistry