Pharmaceutical Chemistry (Inorganic chemistry)

1. Prepared and UPDATED By:
Boy Sapphire, RPh. MS Pharm (CAR) 082015
Department of Pharmacy
School of Allied Medicine
Universidad de Zamboanga
Pharm Chem – 1:
ANTIOXIDANTS

2.  are molecules capable of inhibiting the
oxidation of other molecules.
They are substances that inhibit the destructive
effects of oxidation, e.g. in the body or in
foodstuffs or plastics
Aka: N_ _ _ _ _ _ E C _ _ _ _ _ _T
Aka: R _ _ _ _ _ _G A _ _ _T
ANTIOXIDANTS

3. OXIDATION  is a chemical reaction that transfers electrons from
a substance to an Oxidizing Agent.
Oxidation Reactions can produce free radicals. In turn, these
radicals can start chain reactions.When a Chain Reactions occur in a
Cell, it can cause damage or death (NECROSIS vs. APOPTOSIS).
When a Chain Reactions occur in purified Monomer, it produces a
Polymer Resin, such as a PLASTIC; a Synthetic Fiber; or an Oil Paint
Film.
ANTIOXIDANTS terminate these reactions by removing free radical
intermediates, and inhibit other oxidation reactions.They do this
by being oxidized themselves, an Antioxidants are often Reducing
Agents, such asThiols, Ascorbic acid or Polyphenols.
BASIC CONCEPTS:

4. Although Oxidation reactions are critical for life, they can also be
damaging; hence plants and animals maintain complex systems
of multiple types of antioxidants such as Glutathione,Vitamin C
andVitamin E, as well as enzymes such as Catalyses superoxide
dismutase and various peroxides. Low levels of Antioxidants , or
inhibition of the Antioxidant Enzymes , cause oxidative stress and
may damage or kill cells.
As Oxidative Stress appears to be an important of many human
diseases, the USE of Antioxidants in Pharmacology is intensively
studied, particularly as treatments for Stroke and Neurode-
generative Diseases. However, it is unknown whether Oxidative
Stress is the cause or the consequence of disease.
BASIC CONCEPTS:

5. Antioxidants are widely used as ingredients in dietary
supplements and have been investigated for the prevention of
diseases such as Cancers, Coronary Heart Disease and even
Attitude Sickness.
Although initial studies suggested that antioxidant
supplements might promote health, later large clinical trials did
not detect any benefit and suggested instead that excess
supplementation is harmful.
 In addition to these uses of natural antioxidants in medicine,
these compounds have many industrial uses, such as:
Preservatives in food and cosmetics; and preventing the
degradation of Rubber and Gasoline.
BASIC CONCEPTS:

6.  aka: N_ _ _ _ _ _ _ C _ _ _ _ _ _ _ s;
R__________________ A_ _ _ _s
 these substances prevent OXIDATION.
when combined with
STRONG OXIDIZING AGENTS –
will result to EXPLOSION.
ANTIOXIDANTS: BASIC CONCEPTS

7.  CONSIDERATIONS in the
USED of ANTIOXIDANTS:

INERT  Nonreactive:
 not readily changed by chemical or
biological reaction

NON-TOXIC
 NOT POISONOUS

SOLUBLE
 Capable of being Dissolved by Solvent.
ANTIOXIDANTS: BASIC CONCEPTS

8.  As part of their Adaptation from marine life, terrestrial
plants began producing non-marine antioxidants such
as ascorbic acid (Vitamin C), Polyphenols and
Tocopherols.
 Further development of angiosperm plants between
5o & 200 million years ago, particularly during the
Jurassic Period produced many antioxidant pigments
evolved during the late Jurassic period as chemical
defenses against reactive oxygen species produced
during photosynthesis.
HISTORY OF ANTIOXIDANTS:

9. The term ANTIOXIDANT originally was used to
refer specifically to a chemical that prevented the
consumption of oxygen.
In the late 19th and early 20th centuries, extensive
study was devoted to the uses of antioxidants in
important industrial processes, such as the
prevention of metal corrosion, the vulcanization of
rubber, and the polymerization of fuels in the
fouling of internal combustion engines.
HISTORY OF ANTIOXIDANTS:

10.  Early research on the role of Antioxidants in
biology focused on their use in preventing the
oxidation of unsaturated fats, which is the cause of
Rancidity. Antioxidant activity could be measured
simply by placing the fat in a closed container with
oxygen and measuring the rate of oxygen
consumption.
 However, it was identification of vitamins A, C & E
as antioxidants that revolutionized the field and led
to the realization of the importance of antioxidants
in the biochemistry of living organisms.
HISTORY OF ANTIOXIDANTS:

11.  The possible Mechanism Of Actions of
antioxidants were firsts explored when it was
recognized that a substance with antioxidant
activity is likely to be one that is itself readily
oxidized.
HISTORY OF ANTIOXIDANTS:

12.  Of Pharmaceutical Importance
 1. HYPOPHOSPHORUS ACID
C/F: HPH O ; or H PO₂ ₂ ₃ ₂
Antioxidant used for HydroIodic Syrup /
Hydriodic Syrup / HI Syrup.
2. SULFUR DIOXIDE (C/F: SO )₂

Used for Parenteral Preparations;

also as Fumigant.
INORGANIC ACID
ANTIOXIDANTS

13.  3. SODIUM BISULFITE
 Synonyms: Sulfurous acid,
monosodium salt; Sodium Hydrogen
Sulfite;
 Sodium Acid Sulfite; Leucogen
 Chemical Formula: NaHSO₃;
 antioxidant; antiseptic .
Uses-An Antioxidant and stabilizing Agent. Epinephrine
hydrochloride
Solutions may be stabilized by the addition of small
quantities
of the salt.
INORGANIC ACID
ANTIOXIDANTS

14.  4. NITROGEN  N₂
 aka – Molecular Nitrogen;
 Diatomic Nitrogen Gas
Used in H₂O₂ & Acetanilide Preparation that
functions as Negative Catalyst or AntiOxidant
5. SODIUM THIOSULFATE
 Na₂S₂O₃;
 ANTIDOTE for CYANIDE Poisoning
INORGANIC ACID
ANTIOXIDANTS

15.  BUTYLATED HYDROXYANISOLE
 Synonym: Phenol, O,l-dimethylethyl}-4-methoxy-, Tenox
BHA
 Chemical Structure:
 Uses: An Antioxidant in cosmetics and
pharmaceuticals, containing Fats and oils.
ORGANIC ACID ANTIOXIDANTS

16.  BUTYLATED HYDROXYTOLUENE
 Synonym: Phenol, 2,6-bis{1, 1-dimethylethyl)-4-methyl-,
Butylated Hydroxytoluene Crystalline; Tenox BHT
 Chemical Structure:
Uses:. Uses-An Antioxidant employed to retard oxidative
degradation of oils and fats in various Cosmetics and
pharmaceuticals.
ORGANIC ACID ANTIOXIDANTS

17. VITAMIN C  isWater Soluble. Because of this, it makes it
a great free radical scavenger in the body fluids such as the
blood. It has also been shown to guard against Atherosclerosis
by preventing damage to ArteryWalls.
VITAMIN E  prevents the Oxidation of Lipids (FATS). It
prevents the cell’s protective coatings from becoming rancid
as a result of the attack by free radicals. It also plays a role in
the prevention of cataracts caused by free radical damage.
COENZYME Q10  is a coenzyme produced in the body
that plays a vital role in the production of cellular energy. It is
also a fat soluble antioxidant that protects the fatty parts of
the cell from the free radicals. As we get older, our production
of CoQ10 decreases. That is why supplementation of CoQ10 is
important.
MOST IMPORTANT ANTIOXIDANTS

18. ALPHA-LIPOIC ACID
Research shows that Alpha LipoicAcid is one of the
Most Important Antioxidants, if not the most
important. Here’s is one of the many reasons why:
1. All cells have a fat barrier that keeps the water
soluble components that are inside the cell separate
from the water soluble components that are outside of
the cell. Other Antioxidants are either water soluble or
fat soluble but not both which means that they are not
able to access both the fatty and watery areas of the
cells.
MOST IMPORTANT OF ANTIOXIDANTS

19. ALPHA-LIPOIC ACID
2. Alpha Lipoic Acid however is both fat and water
soluble means that it can access both the fatty and
watery areas of the cells.This allows Alpha Lipoic acid
to deal with free radicals wherever they are.When you
read about all the things that Alpha Lipoic acid does, it
makes you want to ensure that you have adequate
amounts in your body at all times.
3. The body does not produce very large amounts
of Alpha Lipoic acid. Also, because it is found in only a
few foods, it makes sense to take Alpha-Lipoic Acid
supplements.
MOST IMPORTANT OF ANTIOXIDANTS

20. GLUTATHIONE
is a protein that is produced by the liver from the amino
acids glycine, glutamic acid and cysteine. Glutathione is the
cell’s main antioxidant. It is found in greater quantities in
the cell than any other antioxidant.
It has been discovered however that using glutathione
supplements may not be the best way to make sure you
have adequate levels of this very important antioxidant.
That is because it has been found that only very small
amounts of glutathione can pass intact from the digestive
tract all the way to the cells. It has been also found that one
of the best ways to assist the production of glutathione is
with Alpha Lipoic acid supplements.
MOST IMPORTANT OF ANTIOXIDANTS

21. CAROTENOIDS
These are fat soluble pigments that are found in
yellow, red, green and orange vegetable and fruits.
There are over 500 carotenoids found in nature but
the most studied have been alpha carotene, beta
carotene, Lycopene, Cryptoxanthin, Lutein and
Zeaxanthin.
 Because of some of the controversy that has
surrounded studies of beta carotene when beta
carotene has been tested on its own with non-
conclusive results.
MOST IMPORTANT OF ANTIOXIDANTS

22. FLAVONOIDS
are chemical compounds that plants to produce
to protect themselves from damage to their cells.
Plants produce them also to prevent against
bacteria and parasites.
Flavonoids are believed to reduce inflammation,
bolster immune function and improve memory and
concentration.
They are even used to treat attention deficit
disorder. Flavonoids are found in abundance in
plants, fruits and vegetables and plant based
beverages.
MOST IMPORTANT OF ANTIOXIDANTS

23. FLAVONOIDS
are chemical compounds that plants to produce
to protect themselves from damage to their cells.
Plants produce them also to prevent against
bacteria and parasites. Flavonoids are believed to
reduce inflammation, bolster immune function and
improve memory and concentration.
They are even used to treat attention deficit
disorder. Flavonoids are found in abundance in
plants, fruits and vegetables and plant based
beverages.
MOST IMPORTANT OF ANTIOXIDANTS

24. I. Look for the DESCRIPTIONs, MOAs & Use of Other
Substances: ANTIOXIDANTS:
A.Vitamin A H. POLYPHENOLS,
B.CATECHINS/CATECHOLS, I. PCO-Genols;
C.SELENIUM J. COPPER
D.Z I N C K. LYCOPENE
E. Co-Enzyme Q10. L. BROMOLEIN
F. XANTHONE Compds M. PHYCOCYANIN
G. CHLORPHYLL N. PHYCOERYTHRIN
II. Research on the different CONTAINERS used in
Pharmaceuticals: GiveTYPES & Representative Examples of each.
ASSIGNMENTS: Due on FRIDAY