PHARMACEUTICAL CHEMISTRY
Is the study of drugs, the changes it goes, and the
energy that accompanies these changes
MATTER
Anything that occupies space and has mass,
structure, changes that matters undergoes, and
involved in such changes or interactions
Classified as:
1. Physical
2. Chemical
ELEMENT
Simplest form of matter. Made up of 1 kind of material
or atom.
Classified as:
1. Metals: heat and electrical conductors, have luster,
ductile, malleable
2. Nonmetals: generally brittle and non-lustrous, poor
conductors of heat and electricity
3. Metalloids: border the line-2 sides Properties are
intermediate between metals and nonmetals
COMPOUNDS
A compound is a composed of two or more elements
united chemically in definite proportion
Classified as:
1. Based on chemical bond
2. Based on organic or inorganic
Based on chemical bond:
1. Ionic- compound that forms by transfer of electrons
2. Covalent- compound that forms by sharing of
electrons
Polar covalent
Non-polar covalent
3. Metallic- formed between atoms of metallic elements
Based on organic or inorganic:
1. Inorganic compound- compounds that contain other
elements and a few containing carbons and its salts.
2. Organic compound- compounds that contains carbon
atom in their molecules
MIXTURE
Composed of 2 or more substances that are not
chemically combined.
Classified according to:
1. Nature of particles
(heterogenous and homogenous)
2. Size of particles
(solution, coarse and colloid)
Process of separating component of mixtures:
1. Distillation- used if two liquids are mixed but have
different boiling points.
2. Filtration- use by means of filtration set-up
3. Centrifugation- process rely on densities. Speeding
up of settling process of a precipitate
4. Decantation- separation by means of the difference in
specific gravity or density of the components
5.
6.
PROPERTIES OF MATTER:
1. Intrinsic- INDEPENDENT of mass or amount
(ex. Density, sp.gr and melting point)
2. Extrinsic- DEPENDENT on mass or amount
(ex. Weight, volume, pressure and heat content)
CHANGES THAT MATTER UNDERGOES:
1. Physical Change- change in the physical properties of
substances
without
changing
its
chemical
composition.
(Example: Evaporation, pounding of chalk)
2. Chemical change- change in the chemical
composition and constitution of substance.
3. Nuclear Change
change in the structure, properties, composition of the
nucleus of an atom resulting in the transmutation of
the element into another element.
Types:
a. Nuclear fission- splitting of heavy atom
b. Nuclear fusion- union of light atoms
CHEMICAL REACTION
Reaction that occurs when the outermost or valence
electrons around the nucleus interacts.
Entails the removal of valence electrons, adding
electrons to a partly filled valence shell, or sharing a
pair of electrons between two atoms.
REACTANTS
substances that enter into a chemical reaction
PRODUCTS
substances that are formed after chemical reaction
LAW OF CONSERVATION OF MASS
[A]w [B]x
[NH3 ]
[N 2 ][H 2 ]3
[PCl3 ][Cl 2 ]
[PCl5 ]
TYPES OF EQUILIBRIA:
1. Homogenous equilibria- substances are all in the
same state of matter.
CH4(g) + H2O(g) CO(g) + 3H2(g);
CO(g) + H2O(g) CO2(g) + H2(g)
2. Heterogenous equilibria-substances are in different states.
CaCO3(s) CaO(s) + CO2(g);
2+
PbCl2(s) Pb (aq) + 2 Cl (aq)
2. Electronegativity
Left to right increases
Going up increases
3. Ionization Potential
Left to right increases
Going up increases
4. Electron affinity
Right to left increases
Top to bottom increases
Examples:
Cl(g) + e Cl (g)
Ar(g) + e Ar (g)
TERMINOLOGIES:
Ion- charged atom
Atomic number- Protons= Electrons
Mass number- Protons + Neutrons
HYDROGEN (H)
The lightest element
Element common to all acids
Not a member of the family.
3 isotopes of Hydrogen:
1. Protium
2. Deuterium
3. Tritium
LITHIUM (Li)
The lightest metal
One of the bridge element
Used in batteries
Depressant and DOC for Mania
SODIUM (Na)
Major extracellular cation
COPPER (Cu)
Only reddish metal
Essential trace element
Occurs in the respiratory pigment hemocyanin and
cytochrome oxidase
Important alloys: Brass and Bronze
Toxicity: Willsons disease
Important Compounds:
1. Cu(AsO3)2.Cu(C2H3O2)2- Insecticide
2. CuSO4.5H2O- algaecide (ingredient in Bordeaux
mixture)
3. 64Cu isotope
SILVER (Ag)
Silver (Ag)
AKA: Argentum
Pcol action: Oligodynamic property
Toxicity: Argyria
Important Compounds:
1. AgNO3- treatment of warts and eye antiseptic
2. Ag(NH3)2NO3- Howes solution, dental protective
Ag proteinate:
1. Mild Ag proteinate- antiseptic for eye
2. Strong Ag proteinate- germicide for ear and throat
3. Colloidal Ag proteinate- general germicide
GOLD (Au)
AKA: Aurum, shining dawn
Most malleable and ductile of all metals
Best conductor of electricity
This metal can be dissolve using Aqua Regia and
Selenic acid
Important compounds:
1. Aurothioglucose IM
2. Gold Na Thiomalate (IM)
3. Auranofin (PO)
Antidote: Dimercaprol (BAL)
MAGENSIUM (Mg)
nd
2 most abundant intercellular cation
Metal component of chrolophyll
Important compounds:
1. Antacids & laxative (Oxides, carbonates)
2.
3.
4.
Anticonvulsant (SO4)
Lubricants (stearates)
Clarifying and filtering (silicates)
CALCIUM (Ca)
nd
2 most abundant cation in extracellular fluid
Cation of hydroxyapatite
Pcol action:
1. Blood coagulation factor
2. Important in muscle contraction
3. Release of neurotransmitters
4. Def state: osteoporosis, osteomalacia, ricketts
Important compounds:
1. CaCO3- antacids
2. CaCl2- calcium replenisher
3. Ca(OH)2- antacid & saponifying agent
4. CaO- component of Bordeaux mixture
5. Plaster of Paris and Gypsum
STRONTIUM (Sr)
Important compound:
SrCl2- temperature desensitizing agent
BARIUM (Ba)
The most active element of Group IIA
Toxicity: Baritosis
Important compound: BaSO4
RADIUM (Ra)
Only radioactive element of the group
Use for:
1. Cancer radiotherapy
2. Diagnostic purposes
ZINC (Zn)
Metal present in insulin
Essential component of carbonic anhydrase and other
enzymes
Deficiency: Parakeratosis
CADMIUM (Cd)
Pcol action: astringent
Other use: manufacture of stink bomb, found in street
lights
Poisoning: Itai- itai dx
MERCURY (Hg)
AKA: Quicksilver
Pcol action: Antiseptic, Treatment of syphilis,
Paraciticidal and fungicidal
Industrial use: thermometer and amalgams (alloy of
Hg)
Toxicity: Minamata
Boron (B)
A metalloid element of the group
Bonding of this element tends to be more covalent
than ionic
Use to inc. coefficient of expansion of glass
ALUMINUM (Al)
Most abundant metal
rd
3 most abundant element in the earths crust (in the
form of bauxite)
This metal is capable of forming covalent and ionic
bond
Pcol actions: astringent, antiperspirant, deodorant and
used for burn patients
GALLIUM (Ga)
Has the lowest melting point of all the metals
Pcol action: appers in transferring an iron transport
CHON useful in treating cancer related hypercalcemia
Industrial use: substitute for Hg in manufacture of arc
lamps
Toxicity: PLUMBISM
METALS IN METALLURGY:
THALLIUM (Tl)
toxic metal. Similar to arsenics
A.
B.
Important compounds:
1. CO2- Resp. stimulant, treatment of acne, warts and
eczema
2. CO3- antacid, pharmaceutical aid
3. CO- toxic form of carbon, has 210x greater affinity to
hemoglobin than O2
4. Activate charcoal
SILICON (Si)
nd
2 most abundant element in the earths crust.
A tetravalent metalloid. It is less reactive than its
analog carbon.
Toxicity: Silicosis
Forms of Silicon:
1. Talc
Softest mineral known
2. Glass
Generic term used to identify vitreous silicate
material prepared by fusing base (Na2CO3 and
CaCO3) with pure silica.
Substances added to glass: MnO2, Borates, K ion, Pb
1)
2)
3)
4)
5)
Misch metal:
Pewter metal:
Solder metal:
Rose metal:
Litophone:
70%Cs + 30%Fe
80%Sn + 20%Pb
50%Sb + 50%Sn
25%Sn + 25%Pb + 50%Bi
30%ZnS + 70%BaS
OXYGEN (O)
Aka: empyreal air
The most abundant element in the earths crust
Discovered by Joseph Priestly
Pcol use: tx of hypoxia/asphyxia
It is a component of Artificial air
Container: Green
FLUORINE (F)
Exists as a pale yellow gas
The most electronegative element of the periodic
table
Fluoride compounds are use as anti-cariogenic
agents
Excessive amount in drinking water results to
fluorosis
Important compounds:
1. Fluorides- anti-cariogenic
2. Freons- refrigerant, aerosol propelant
SULFUR (S)
Aka: brimstone, shubari and enemy of Copper
It occurs on the earths crust as a free element or in
combined form as metal sulfides and sulfates.
Most sulfur compounds have a strong odor
Forms of Sulfur:
1. Monoclinic- rhombic sulfur that is heated to a temperature
of 96C.
2. Mobile sulfur- monoclinic that is melted at a temperature of
113C
3. Viscous sulfur- result of continued heating of mobile sulfur
4. Amorphous sulfur- viscous that is cooled rapidly by
immersion in cold water.
5. Rhombic sulfur
Important Compounds:
1. Elemental sulfur- fungicidal
2. Sublimed sulfur- cathartic
3. Precipitated sulfur- scabicide
4. Sulfurated potash- tx for psoriasis
5. White Lotion USP- scabicidal
6. Sodium metabisulfite- antioxidant, preservative
SELENIUM (Se)
Aka: Selene, Moon
An essential trace element
Promotes absorption of Vitamin E
Important compounds:
1. Selenomethionine
2. SeS2- tx of sebborheic dermatitis
TELLURIUM (Te)
Occur much less abundant than sulfur. It is found
along with sulfur in metal sulfides and are recovered
in some quantity from Pb and Cu refining process.
POLONIUM (Po)
Occurs only in the form of radioisotopes as a result of
decay of the actinide elements.
CHROMIUM GROUP (GROUP VIB )
Chromium (Cr), Molybdenum (Mo), Tungsten (W), and
Uranium (U)
CHROMIUM (Cr)
Comes from the Greek word chroma
CHLORINE (Cl)
Aka: dephlogesticated muriatic acid air
Element with greenish yellow gas with a very
suffocating odor
Discovered by a swedish chemist, Carl Wilhelm
Scheele
Important compounds:
1. Chlorides- electrolyte replenisher
2. Hypochlorites- bleaching agent
3. HCl- treatment of achlorhydria
BROMINE (Br)
A fuming reddish brown liquid in room temperature,
corrosive and toxic
Bromine comes from the Greek word bromos
meaning strong smelling
Bromide compounds have sedative and CNS
depressant action
Poisoning: Brominism (NaCl and Ammonia)
IODINE (I)
Exists as a brown solid at room temperature
Elemental Iodine is known as one of the oldest known
germicides in use today.
Pcol action: component of thyroxine and
triiodothyroxine
Iodide compounds have an expectorant action.
Important compounds:
1. Povidone-Iodine
2. Strong Iodine solution
3. Iodine tincture
ASTATINE (At)
The only metallic halogen
The only synthetic
The only radioactive halogen
(MANGANESE GROUP (GROUP VIIB)
Manganese (Mn), Technetium (Tc), and Rhenium (Re)
General Properties:
MANGANESE (Mn)
A silvery gray metal that resembles iron.
This element occurs mainly as the oxide (MnO2) in
nature.
Compounds with 2+ oxidation state is a good
reducing agent and MnO4 (permanganates) are good
oxidizing agent.
Pcol action: cofactor in protein synthesis, and
important in activation of pyruvate carboxylase (vital
role in human metabolic function)
Industrial use: production of metal alloys
Poisoning: Parkinson-like symptoms
Important compound of Mn:
1) KMnO4- oxidizing agent and antiseptic (0.02%) and
as a gastric lavage for various alkaloidal poisoning.
Identification tests for Mn:
1) H2S: salmon or flesh colored ppt. of MnS
2) NaBiO3: purple solution of HMnO4
TECHNETIUM (Tc)
Came from the greek word technetos
st
It was the 1 element produced artificially
Use: preparation of radiopharmaceuticals
NOBLE GASES (GROUP VIIIA)
Helium (He), Neon (Ne), Argon (Ar), Krypton (Kr), Xenon
(Xe) and Radon (Rn)
General Properties:
This element are inactive. It maybe explained on the
basis of their atomic structure. Helium (2e) and the
rest have (8e) in outermost shell.
st
IRON (Fe)
Fe meaning ferrum
The first production of this metal started from the
middle bronze age.
It is not found free in nature, the chief source in
industry is hematite.
The sulfide form, Fe2S3 looks similar to gold.
COBALT (Co)
In nature, cobalt is usually found associated with
arsenical ores.
Most ores of this element contains water of hydration
and are red in color.
Elemental component of Vit. B12
Pcol action: essential in development of erythrocyte
and hemoglobin
Deficiency of cobalt: Megaloblastic anemia
Identification tests:
1) NH4OH: pink ppt. of Co(OH)2 which dissolves upon
addition of an excess reagent forming
2) KNO2, HAc: yellow ppt. of K3Co(NO2)6
NICKEL (Ni)
Aka: old nicks copper
Metal use in fake/fancy jewelries
Important compound: Nickel pectinate- tx of diarrhea
Identification tests:
1) NH4OH: green ppt. of Ni(OH)2 which dissolves in
excess reagent
2) Dimethylglyoxime, NH3: red ppt.
OSMIUM (Os)
Heaviest/ densest metal
Important compounds:
1) Osmic acid
2) Osmium tetroxide- used in microorganism staining
PLATINUM (Pt)
Industrial use: catalyst in finely divided steel
Pharmaceutical products available:
1) Cisplatin
2) Carboplatin
Fluoride- anticariogenic
Bromide- sedative, CNS depressant and hypnotic
Arsenic- depressant for epilepsy and used to treat
leukemia
4) Lithium- diuretic and used in manic-depressive
disorder
5) Gold- used in rheumatism and SLE
6) Aluminum- astringent, antiseptic and deodorant
7) Silver- antiseptic, astringent (irritant to corrosive)
8) Mercury- diuretic, antiseptic, parasiticide and
fungicide
9) Strontium- sedative, treatment of osteoporosis,
dentrifice and tooth temperature desensitizing agent
10) Chromium- play some role in glucose tolerance of
some diabetics, old people and malnourished people
1)
2)
3)
PHYSIOLOGICAL BUFFERS
Carbonic acid & Bicarbonate- Primary buffer of ECF
Phosphate & Dihydrogen Phosphate- Urinary buffer/
also a buffer of ICF
Hemoglobin & Proteins- Primary buffer of ICF
PREPARED BY:
DAN LESTER P. BACALZO, RPH
Instructor-College of Pharmacy